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piperidines

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Description

Piperidines: A family of hexahydropyridines. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID44237242
MeSH IDM0016885

Synonyms (1)

Synonym
piperidines

Research Excerpts

Overview

Piperidines are a relatively novel class of calcium channel blockers. They act at a unique receptor site associated with the calcium channel alpha1 subunit.

ExcerptReferenceRelevance
"Piperidines are a relatively novel class of calcium channel blockers which act at a unique receptor site associated with the calcium channel alpha1 subunit. "( Cytoplasmic determinants of piperidine blocking affinity for N-type calcium channels.
Zamponi, GW, 1999
)
1.75

Toxicity

ExcerptReferenceRelevance
"Sufentanil (R 30 730), N-[4-methoxymethyl)-1-[2-(2-thienyl)ethyl]-4-piperidinyl]-N-phenylpropanamide, is a chemically novel, highly potent and extremely safe intravenous morphine-like agent in laboratory animals."( Sufentanil, a very potent and extremely safe intravenous morphine-like compound in mice, rats and dogs.
Janssen, PA; Niemegeers, CJ; Schellekens, KH; Van Bever, WF, 1976
)
0.26
"3-dihydro-2H-benzimidazol-2-one (domperidone), which in contrast to available anti-emetics does not provoke extrapyramidal or adrenolytic adverse effects, also enhances gastric emptying motility."( Domperidone, a novel and safe gastrokinetic anti-nauseant for the treatment of dyspepsia and vomiting.
Broekaert, A; Heykants, J; Jageneau, A; Janssen, PA; Laduron, P; Marsboom, R; Niemegeers, CJ; Reyntjens, AJ; Schellekens, KH; Van Nueten, JM, 1978
)
0.26
" There were no major adverse reactions associated with risperidone use, but it was noted to reduce the signs of tardive dyskinesia."( Risperidone: clinical safety and efficacy in schizophrenia.
Borison, RL; Diamond, BI; Meibach, RC; Pathiraja, AP, 1992
)
0.28
" Nausea and constipation occurred significantly more often with paroxetine, but only 9% of paroxetine patients dropped out of the study due either in whole or in part to an adverse effect."( The safety and efficacy of paroxetine compared with placebo in a double-blind trial of depressed outpatients.
Claghorn, JL, 1992
)
0.28
" Furthermore, paroxetine is relatively safe in overdose and has very little anticholinergic activity."( The safety profile of paroxetine.
Blumhardt, CL; Boyer, WF, 1992
)
0.28
"Compared to traditional neuroleptics, most of the new antipsychotics are characterized by a low extrapyramidal side effect (EPS) liability and varying antipsychotic efficacy."( New antipsychotics: classification, efficacy, and adverse effects.
Gerlach, J, 1991
)
0.28
" In Purkinje fibers exposed to toxic concentrations of ouabain, R 56865 (1 microM) reduced the delayed after depolarization (DAD) amplitude and inhibited triggered activity."( Investigation of electrophysiologic mechanisms for the antiarrhythmic actions of R 56865 in cardiac glycoside toxicity.
Damiano, BP; Stump, GL; Yagel, SK, 1991
)
0.28
" Mild adverse reactions were reported in 6 out of 23 cisapride-treated patients and in 10 out of 20 clebopride-treated patients who completed the study."( Clinical efficacy and safety of cisapride and clebopride in the management of chronic functional dyspepsia: a double-blind, randomized study.
D'Angelo, V; Manzi, G; Mazzacca, G; Minieri, M; Piai, G; Sabbatini, F, 1991
)
0.28
"3 microM and 9 microM, respectively, against the toxic action of 100 microM glutamate."( Excitatory amino acid neurotoxicity at the N-methyl-D-aspartate receptor in cultured neurons: protection by SKF 10,047.
Feuerstein, G; Lysko, PG, 1990
)
0.28
"Loperamide is a safe and effective antidiarrheal for the treatment of acute diarrhea."( Safety and efficacy of loperamide.
Ericsson, CD; Johnson, PC, 1990
)
0.28
" However, a comparison of the relative toxic effects of MDMA and MBDB indicates that MBDB may be slightly less neurotoxic."( Neurotoxic effects of the alpha-ethyl homologue of MDMA following subacute administration.
Johnson, MP; Nichols, DE, 1989
)
0.28
" The central monoamine stores of rats were significantly decreased with reserpine (5 mg/kg) prior to toxic injections of MDMA."( Reserpine does not prevent 3,4-methylenedioxymethamphetamine-induced neurotoxicity in the rat.
Hekmatpanah, CR; McKenna, DJ; Peroutka, SJ, 1989
)
0.28
"Cisapride has not been found to have a significant frequency of adverse reactions, except for diarrhoea which occurs in about 4% of individuals taking the drug."( How safe and acceptable is cisapride?
Bennett, JR, 1989
)
0.28
"Drug-induced hematological disorders appear as a rare but serious side effect of the drugs use."( [Hematologic toxicity of antidepressive agents].
Galbaud du Fort, G,
)
0.13
" Treatment effects on vital signs, laboratory tests, a mood evaluation test, electrocardiograms (ECGs), and reported adverse experiences were monitored."( Safety evaluation of ritanserin--an investigational serotonin antagonist.
Barone, JA; Bierman, RH; Colaizzi, JL; Cornish, JW; Drake, ND; Hsuan, A, 1986
)
0.27
"N-Chloropiperidine (NCP) has been reported to be both toxic and mutagenic in a wide range of in vitro and in vivo genotoxicity assays, however, few experimental details or numerical data have been presented to support these claims."( N-chloropiperidine and calcium hypochlorite: possible examples of toxicity-dependent clastogenicity in vitro.
Ashby, J; Callander, RD; Mohammed, R, 1987
)
0.27
" However, at this dose level vadocaine is apparently safe and its antitussive properties seem promising enough for further evaluation."( First human studies on the safety and antitussive activity of vadocaine hydrochloride.
Karttunen, P; Männistö, PT; Tukiainen, H; Uusitupa, M, 1988
)
0.27
" On the basis of these results, a 300 mg dose of vadocaine appears to be safe in man in all respects."( Assessment of the safety margin of vadocaine hydrochloride in man.
Helin, M; Karttunen, P; Silvasti, M; Tukiainen, H; Uusitupa, M, 1988
)
0.27
" This dual action negates most of the toxic effects of the compound in vivo."( Neurotoxicity of dipiperidinoethane due to in vivo conversion to a selective cholinesterase inhibitor.
Baron, BM; Kashman, Y; Sokolovsky, M, 1985
)
0.27
" These results emphasize the need for pilot toxicity studies, especially when components of the test system are varied, to assess the effect of drug concentration on the toxic response."( Alterations of drug-induced toxicity in the mouse lymphoma assay by a rat hepatic microsomal metabolizing system (S-9).
Oldham, JW; Paulson, JD; Preston, RF; Pritchard, JF, 1984
)
0.27
" The most frequently reported extracardiac adverse experiences were dizziness (30%) and visual disturbances (28%), often occurring in tandem."( Extracardiac adverse effects of flecainide.
Gentzkow, GD; Sullivan, JY, 1984
)
0.27
" Chronic administration of flecainide did not produce chronic toxic changes in either species."( Chronic oral toxicity and oncogenicity studies of flecainide, an antiarrhythmic, in rats and mice.
Case, MT; Sibinski, LJ; Steffen, GR, 1984
)
0.27
"Piperine is acutely toxic to mice, rats and hamsters."( Acute and subacute toxicity of piperine in mice, rats and hamsters.
Glinsukon, T; Piyachaturawat, P; Toskulkao, C, 1983
)
0.27
" Other adverse effects were assessed using the UKU Side Effects Scale."( Extrapyramidal side effects and tolerability of risperidone: a review.
Owens, DG, 1994
)
0.29
" Orthostatic hypotension, dizziness, and somnolence were the most commonly reported adverse events."( Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic.
Brecher, MB; Chi, E; Grasing, K; Hubbard, JW; Sainati, SM, 1995
)
0.29
" We found no major difference between non-elderly and elderly depressed patients as concerns efficacy, total incidence of adverse findings or safety parameters such as laboratory values and heart rate."( Are there any differences in the safety and efficacy of brofaromine and imipramine between non-elderly and elderly patients with major depression?
Möller, HJ; Müller, H; Volz, HP, 1995
)
0.29
" Piperine itself was not toxic to the cells up to a concentration of almost 100 microM."( Piperine, a major ingredient of black and long peppers, protects against AFB1-induced cytotoxicity and micronuclei formation in H4IIEC3 rat hepatoma cells.
Reen, RK; Singh, J; Wiebel, FJ, 1994
)
0.29
" Using a potent and selective ligand of sigma binding sites, 6-[6-(4-hydroxypiperidinyl)hexyloxy]-3-methylflavone (NPC 16377), we further investigated the influence of sigma ligands on additional behavioral and toxic effects of cocaine in mice."( Effects of the selective sigma receptor ligand, 6-[6-(4-hydroxypiperidinyl)hexyloxy]-3-methylflavone (NPC 16377), on behavioral and toxic effects of cocaine.
Ferkany, J; Hickey, P; Katz, JL; Menkel, M; Pontecorvo, M; Terry, P; Witkin, JM, 1993
)
0.29
" Using inhibition of D-amphetamine-stimulated locomotion in mice as a measure of potential antipsychotic efficacy, MDL 100,907 showed a superior CNS safety index relative to the reference compounds, haloperidol, clozapine, risperidone, ritanserin, and amperozide, in each of five tests for side effect potential, including measures of ataxia, general depressant effects, alpha 1-adrenergic antagonism, striatal D2 receptor antagonism, and muscle relaxation."( Preclinical characterization of the potential of the putative atypical antipsychotic MDL 100,907 as a potent 5-HT2A antagonist with a favorable CNS safety profile.
Baron, BM; Carr, AA; Chaney, SF; Elands, J; Feldman, DJ; Frank, RA; Johnson, MP; Kehne, JH; McCarty, DR; McCloskey, TC; Poirot, M; Senyah, Y; Siegel, BW; van Giersbergen, PL; Widmaier, C, 1996
)
0.29
" This column will review the mechanism of action of cisapride, the drug's metabolism and reported cardiac adverse effects with intravenous cisapride."( Cardiac toxicity with cisapride.
Farrington, E,
)
0.13
" The popularity of the newer H1 antihistamines is due to their ability to provide relief from allergic symptoms without the undesirable side effect of sedation commonly associated with first generation H1 receptor antagonists such as diphenhydramine and promethazine."( Comparative analysis of the cardiotoxicity proclivities of second generation antihistamines in an experimental model predictive of adverse clinical ECG effects.
del Prado, M; Egan, RW; Hey, JA; Kreutner, W; Sherwood, J, 1996
)
0.29
" The incidence of treatment-emergent adverse events with all three dosages of donepezil (64-68%) was comparable to that observed with placebo (65%)."( The efficacy and safety of donepezil in patients with Alzheimer's disease: results of a US Multicentre, Randomized, Double-Blind, Placebo-Controlled Trial. The Donepezil Study Group.
Friedhoff, LT; Rogers, SL,
)
0.13
"The clinical study population showed a significantly younger age profile than the PEM population and excluded patients with serious disease; however, both studies showed similar patterns of adverse events."( A comparison of two cohort studies evaluating the safety of cisapride: Prescription-Event Monitoring and a large phase IV study.
Mann, RD; Pearce, GL; Tooley, PJ; Wager, E; Wilton, LV, 1997
)
0.3
"Both studies showed cisapride to be generally safe and well tolerated."( A comparison of two cohort studies evaluating the safety of cisapride: Prescription-Event Monitoring and a large phase IV study.
Mann, RD; Pearce, GL; Tooley, PJ; Wager, E; Wilton, LV, 1997
)
0.3
" Putrescine was moderately toxic but only at 500 microM concentration."( Neurotoxicity of polyamines and pharmacological neuroprotection in cultures of rat cerebellar granule cells.
Ciani, E; Contestabile, A; Dall'Olio, R; Gandolfi, O; Sparapani, M, 1997
)
0.3
" Adverse experiences, predominantly lightheadedness and dizziness, were reported by subjects receiving doses of lubeluzole greater than or equal to 10 mg."( The safety and tolerability of single intravenous doses of lubeluzole (Prosynap) in healthy volunteers.
Crabbé, R; Gheuens, J; Hantson, L; Tritsmans, L; Van Rooy, P, 1997
)
0.3
" Piperine at 60 microM completely counteracted cytotoxicity and formation of MN by 10 microM AFB1 and reduced the toxic effects of 20 microM AFB1 by > 50%."( Piperine inhibits aflatoxin B1-induced cytotoxicity and genotoxicity in V79 Chinese hamster cells genetically engineered to express rat cytochrome P4502B1.
Reen, RK; Singh, J; Wiebel, FJ, 1997
)
0.3
" The majority of adverse experiences were mild to moderate and resolved during treatment."( Safety and pharmacokinetics of the neuroprotective drug lubeluzole in patients with ischemic stroke.
De Keyser, J; Franke, CL; Gheuens, J; Hantson, L; Schellens, RL; Tritsmans, L; Van de Velde, V; van Gorp, J; Van Peer, A; Woestenborghs, R,
)
0.13
" Adverse experiences were similar in all three treatment groups except that superficial thrombophlebitis was more frequent in the lubeluzole 10-mg group."( Cardiovascular safety of lubeluzole (Prosynap(R)) in patients with ischemic stroke.
Diener, HC; Haan, J; Hacke, W; Hantson, L; Hennerici, M; Lees, KR; Timmerhuis, T,
)
0.13
" Because the catechol was generally less toxic than the O-methylated product, species that eliminate zamifenacin primarily as the catechol or its conjugate may be less affected by the potential hepatotoxicity of the methylated product."( In vitro toxicity of zamifenacin (UK-76,654) and metabolites in primary hepatocyte cultures.
Amacher, DE; Beaumont, K; Charuel, C; Comby, P; Fasulo, LM, 1998
)
0.3
" Overall, the incidence of adverse events was similar for both treatment groups."( Efficacy and safety of levocabastine nasal spray for seasonal allergic rhinitis.
Dolen, J; Hampel, FC; Holton, D; Karcher, K; Martin, BG; Travers, S,
)
0.13
"To assess the incidence of adverse events in postmenopausal women treated with raloxifene compared with placebo, hormone replacement therapy (HRT), or unopposed estrogen."( Adverse events reported by postmenopausal women in controlled trials with raloxifene.
Davies, GC; Huster, WJ; Lakshmanan, M; Lu, Y; Plouffe, L, 1999
)
0.3
" Incidence and severity of all treatment-emergent adverse events, defined as events that first occurred or worsened during treatment, were compared among groups in each of the databases."( Adverse events reported by postmenopausal women in controlled trials with raloxifene.
Davies, GC; Huster, WJ; Lakshmanan, M; Lu, Y; Plouffe, L, 1999
)
0.3
"Discontinuation rates overall, and those related to adverse events, were not significantly different between treatment groups in any database."( Adverse events reported by postmenopausal women in controlled trials with raloxifene.
Davies, GC; Huster, WJ; Lakshmanan, M; Lu, Y; Plouffe, L, 1999
)
0.3
"Raloxifene had an adverse event profile distinct from HRT and unopposed estrogen and was well tolerated by postmenopausal women."( Adverse events reported by postmenopausal women in controlled trials with raloxifene.
Davies, GC; Huster, WJ; Lakshmanan, M; Lu, Y; Plouffe, L, 1999
)
0.3
" No serious adverse events occurred, and study treatments were well tolerated with a low incidence of central nervous system-related adverse events and headache."( A 12-week, placebo-controlled study of the efficacy and safety of ebastine, 10 and 20 mg once daily, in the treatment of perennial allergic rhinitis. Multicentre Study Group.
Bousquet, J; Gaudaño, EM; Palma Carlos, AG; Staudinger, H, 1999
)
0.3
" The most common adverse event in the phase II studies was hypoglycaemia."( Preclinical and clinical studies on safety and tolerability of repaglinide.
Schatz, H, 1999
)
0.3
"In light of our previous SAR studies on nitroxides acting as less toxic anticancer agents, antioxidants and radioprotectors, we designed and tested, in vivo an in vitro, a new triradical spin trap -N,N',N"-tris-(l-oxyl-2,2,6,6-tetramethylpiperidine-4-yl)-1,3, 5-tnazine-2,4,6-triamine (TTT)."( TTT, a novel free radical spin trap, induces apoptosis in sarcoma Yoshida cells in vivo: comparative investigations of its cytotoxicity in vitro.
Koceva-Chyła, A; Kochman, A; Metodiewa, D; Skolimowski, J,
)
0.13
" The most common adverse events were related to the nervous and digestive systems, and were generally mild and transient, resolving without the need for dose modifications."( Long-term efficacy and safety of donepezil in the treatment of Alzheimer's disease: final analysis of a US multicentre open-label study.
Doody, RS; Ieni, JR; Pratt, RD; Rogers, SL, 2000
)
0.31
"We report the safe use of remifentanil as part of the anaesthetic technique in a patient undergoing major head and neck surgery who was being treated for depressive illness with the non-specific monoamine oxidase inhibitor (MAOI) phenelzine."( Safe use of remifentanil in a patient treated with the monoamine oxidase inhibitor phenelzine.
Gillies, MA; James, KS; Ure, DS, 2000
)
0.31
" Results from the present study suggest a better therapeutic index for the nimesulide-piperine combination indicating that this combination would further reduce the frequency of adverse effects associated with nimesulide alone."( Comparative anti-nociceptive, anti-inflammatory and toxicity profile of nimesulide vs nimesulide and piperine combination.
Bansal, P; Bhardwaj, RK; Gupta, SK; Velpandian, T, 2000
)
0.31
"5% ophthalmic solution instilled four times daily is effective and safe in reducing the signs and symptoms of seasonal allergic conjunctivitis."( Efficacy and safety of ketorolac tromethamine 0.5% and levocabastine 0.05%: a multicenter comparison in patients with seasonal allergic conjunctivitis.
Donshik, PC; Pearlman, D; Pinnas, J; Raizman, MB; Tauber, J; Tinkelman, D; Walters, TR,
)
0.13
" The incidence of drug-related adverse events was 10% (14/136) in the donepezil and 8% (10/131) in the placebo group; no significant difference was seen between the two groups."( Clinical efficacy and safety of donepezil on cognitive and global function in patients with Alzheimer's disease. A 24-week, multicenter, double-blind, placebo-controlled study in Japan. E2020 Study Group.
Hasegawa, K; Homma, A; Imai, Y; Kameyama, M; Nishimura, T; Takeda, M; Udaka, F,
)
0.13
" In conclusion, Rf appears to be safe and effective for the treatment of acute pain in the very young child submitted to craniosynostosis repair."( Safety and efficacy of remifentanil in craniosynostosis repair in children less than 1 year old.
Chiaretti, A; Ciano, F; Di Rocco, C; Piastra, M; Pietrini, D; Polidori, G; Savioli, A; Velardi, F, 2000
)
0.31
" It is reported to have a relatively favourable side-effect profile."( Adverse effects associated with the use of donepezil in general practice in England.
Dunn, NR; Pearce, GL; Shakir, SA, 2000
)
0.31
" The results clearly confirmed that the toxic effect could result either from the presence or structure of substituent(s) at position 4 of the free radical piperidine moiety."( Tempicol-3, a novel piperidine-N-oxide stable radical and antioxidant, with low toxicity acts as apoptosis inducer and cell proliferation modifier of Yoshida Sarcoma cells in vivo.
Gwoździnski, K; Głebska, J; Jóźwiak, Z; Koceva-Chyła, A; Kochman, A; Metodiewa, D,
)
0.13
" The most common adverse events were associated with the nervous and digestive systems and were generally mild and transient; 17% of patient discontinuations were associated with adverse events."( Open-label, multicenter, phase 3 extension study of the safety and efficacy of donepezil in patients with Alzheimer disease.
Doody, RS; Geldmacher, DS; Gordon, B; Perdomo, CA; Pratt, RD, 2001
)
0.31
"Donepezil is an effective and safe drug for the long-term symptomatic treatment of mild to moderately severe AD for up to 144 weeks (2."( Open-label, multicenter, phase 3 extension study of the safety and efficacy of donepezil in patients with Alzheimer disease.
Doody, RS; Geldmacher, DS; Gordon, B; Perdomo, CA; Pratt, RD, 2001
)
0.31
" No clinically important adverse events were observed."( Effect of a platelet-activating factor receptor antagonist, E5880, on cerebral vasospasm after aneurysmal subarachnoid hemorrhage--open clinical trial to investigate efficacy and safety.
Endo, S; Hirashima, Y; Kobayashi, N; Nukui, H; Takaku, A, 2001
)
0.31
" No serious adverse events were reported, all adverse events were related to nasal symptoms."( Comparative efficacy and safety of azelastine and levocabastine nasal sprays in patients with seasonal allergic rhinitis.
Baehre, M; Falser, N; Rahlfs, VW; Wober, W, 2001
)
0.31
" Both remifentanil and fentanyl were well-tolerated, with reported adverse events typical of mu-opioid agonists."( Remifentanil and fentanyl during anaesthesia for major abdominal and gynaecological surgery. An open, comparative study of safety and efficacy.
Appelgren, L; Camu, F; Doenicke, A; Helmers, JH; Holgersen, O; Mann, C; Noronha, D; Sneyd, JR; Upadhyaya, BK, 2001
)
0.31
" ERA-923 was well tolerated, and adverse events were mild and reversible."( Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women.
Burghart, PH; Cotreau, MM; Dykstra, KH; Gandhi, T; Gutierrez, M; Park, Y; Schwertschlag, US; Stonis, L; Xu, J, 2002
)
0.31
" Safety was monitored by physical examinations, vital signs, clinical laboratory tests, electrocardiograms (ECGs), and treatment-emergent adverse events (AEs)."( A randomized, double-blind, placebo-controlled study of the efficacy and safety of donepezil in patients with Alzheimer's disease in the nursing home setting.
Cummings, JL; Katz, IR; Mintzer, J; Perdomo, CA; Schwam, EM; Tariot, PN; Whalen, E, 2001
)
0.31
" Overall, the incidence of adverse events was similar but greater in the remifentanil group with respect to shivering (P<0."( Comparative efficacy and safety of remifentanil and fentanyl in 'fast track' coronary artery bypass graft surgery: a randomized, double-blind study.
Blake, D; Demeyere, R; Dybvik, T; Herregods, L; Kirnö, K; MacAdams, C; Moerman, A; Möllhoff, T; Shaikh, S, 2001
)
0.31
" The antitumor and toxic effects are mediated in part by different mechanisms, thus, permitting a selective inhibition of certain side effects."( BGP-15 - a novel poly(ADP-ribose) polymerase inhibitor - protects against nephrotoxicity of cisplatin without compromising its antitumor activity.
Berente, Z; Bernath, S; Gallyas, F; Jaszlits, L; Literati-Nagy, P; Osz, E; Rabloczky, G; Racz, I; Sumegi, B; Tory, K, 2002
)
0.31
" brasiliensis alkaloids have a potent toxic activity."( Antibacterial activity against resistant bacteria and cytotoxicity of four alkaloid toxins isolated from the marine sponge Arenosclera brasiliensis.
Berlinck, RG; de Moraes, MO; Fortier, SC; Nascimento, GG; Pessoa, C; Torres, YR, 2002
)
0.31
" Rivastigmine was generally well tolerated, the most common adverse events being nausea and vomiting, consistent with reports from previous clinical studies."( Efficacy and safety of rivastigmine in patients with Alzheimer's disease who failed to benefit from treatment with donepezil.
Auriacombe, S; Loria-Kanza, Y; Pere, JJ; Vellas, B, 2002
)
0.31
"The correlates of dropout, efficacy, and adverse events in the treatment of Alzheimer's disease (AD) with acetylcholinesterase inhibitors (ChEI) are unclear."( Correlates of dropout, efficacy, and adverse events in treatment with acetylcholinesterase inhibitors in Korean patients with Alzheimer's disease.
Kim, JM; Shin, IS; Yoon, JS, 2002
)
0.31
" There were also no significant differences in the percentages of patients experiencing adverse events between the ebastine with and without food groups."( A double-blind, placebo-controlled study of the efficacy and safety of ebastine 20 mg once daily given with and without food in the treatment of seasonal allergic rhinitis.
Frank, H; George, G; Gillen, M; Lim, J; Rohatagi, SS, 2002
)
0.31
" Adverse events, physical examinations and clinical laboratory tests were assessed."( Donepezil: tolerability and safety in Alzheimer's disease.
Ieni, JR; Perdomo, CA; Pratt, RD; Surick, IW, 2002
)
0.31
"To compare the frequency of adverse effects of remifentanil and fentanyl in a large and diverse patient population."( A comparison of the remifentanil and fentanyl adverse effect profile in a multicenter phase IV study.
Fleisher, LA; Joshi, GP; Twersky, RS; Warner, DS, 2002
)
0.31
", opioid-related) adverse effects were recorded."( A comparison of the remifentanil and fentanyl adverse effect profile in a multicenter phase IV study.
Fleisher, LA; Joshi, GP; Twersky, RS; Warner, DS, 2002
)
0.31
" There were no significant differences between the two drugs with respect to other adverse events (i."( A comparison of the remifentanil and fentanyl adverse effect profile in a multicenter phase IV study.
Fleisher, LA; Joshi, GP; Twersky, RS; Warner, DS, 2002
)
0.31
"In the doses used, both remifentanil and fentanyl have a similar frequency of adverse effects except for the higher frequency of hypotension associated with the use of remifentanil."( A comparison of the remifentanil and fentanyl adverse effect profile in a multicenter phase IV study.
Fleisher, LA; Joshi, GP; Twersky, RS; Warner, DS, 2002
)
0.31
" Quaternary piperidine derivatives IIIf and IIIg and also non-quaternary piperidine derivatives IIIb, IIIe, IIIc and IIId were more toxic than 5-fluorouracil in brine shrimp bioassay."( Toxicity of some bis Mannich bases and corresponding piperidinols in the brine shrimp (Artemia salina) bioassay.
Erciyas, E; Gul, HI; Gul, M,
)
0.13
" No serious or severe adverse events were reported."( Safety and pharmacokinetics of ReN1869: a first human dose study in healthy subjects after single-dose administration.
Gerrits, M; Ingwersen, SH; Skrumsager, BK, 2003
)
0.32
"The type and severity of adverse events during repaglinide treatment were similar to the run-in period."( Safety and efficacy of repaglinide in type 2 diabetic patients with and without impaired renal function.
Hasslacher, C, 2003
)
0.32
" Adverse events (predominantly headache, nervousness, and somnolence) were minor and comparable for all treatment groups."( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil.
Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003
)
0.32
"We conducted a comparative retrospective study of the tolerance and the adverse events (AE) of two AChEI in a group of patients with very slight and mild probable AD over a 6 month period."( [Tolerance and adverse events of treatment with acetylcholinesterase inhibitors in a clinical sample of patients with very slight and mild Alzheimer s disease over a six-month period].
Fajardo-Tibau, C; Garre-Olmo, J; Gelada-Batlle, E; Hernández-Ferràndiz, M; López-Pousa, S; Lozano-Gallego, M; Morante-Muñoz, V; Turon-Estrada, A; Vilalta-Franch, J,
)
0.13
" 2 Delta(9)-and Delta(8)-tetrahydrocannabinol (THC) were toxic when added directly to SH-SY5Y neuroblastoma cells."( Reduction of human monocytic cell neurotoxicity and cytokine secretion by ligands of the cannabinoid-type CB2 receptor.
Bissonnette, CJ; Klegeris, A; McGeer, PL, 2003
)
0.32
" In all five studies, most adverse events were related to hypoglycemia, as expected in a normal population given a blood glucose regulator."( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide.
Hansen, KT; Hatorp, V; Thomsen, MS, 2003
)
0.32
" Histamine was applied at 10(-9),10(-8), 10(-7),10(-6), and 10(-5) M for 16 h into the cultures and the highest dose was found to be the most toxic one."( Contribution of the histaminergic receptor subtypes to histamine-induced cerebellar granular neurotoxicity.
Buyukokuroglu, ME; Gepdiremen, A; Hacimuftuoglu, A; Suleyman, H,
)
0.13
" The type and frequency of adverse events were similar across treatment groups."( Efficacy and safety of ketotifen eye drops in the treatment of seasonal allergic conjunctivitis.
Cooper, C; Kidd, M; Lanz, R; McKenzie, SH; Steven, I, 2003
)
0.32
" Our previous experiments have proved the toxic effects of Tinuvin 770 on isolated rat cardiomyocytes."( Comparative study on cardiotoxic effect of Tinuvin 770: a light stabilizer of medical plastics in rat model.
Hubay, M; Járay, J; Kovács, A; Merkely, B; Soós, P; Sótonyi, P; Szentmáriay, I; Zima, E, 2004
)
0.32
" Tolerability and safety were assessed by monitoring adverse events, physical examinations, vital signs, clinical laboratory test abnormalities and ECG findings throughout the study."( Efficacy and safety of donepezil in patients with Alzheimer's disease: results of a global, multinational, clinical experience study.
Bahra, R; Baloyannis, S; Boada-Rovira, M; Brodaty, H; Cras, P; Emre, M; Zhang, R, 2004
)
0.32
"9%) patients completed the study; 59 (5%) patients discontinued because of adverse events."( Efficacy and safety of donepezil in patients with Alzheimer's disease: results of a global, multinational, clinical experience study.
Bahra, R; Baloyannis, S; Boada-Rovira, M; Brodaty, H; Cras, P; Emre, M; Zhang, R, 2004
)
0.32
" Finally, no apparent difference was noted in the safety of ebastine between patients with hepatic insufficiency and healthy subjects as assessed by evaluation of adverse events, vital signs and laboratory parameters."( Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.
Dilzer, SC; Lasseter, KC; Noveck, RJ; Vargas, R; Waldman, S, 2004
)
0.32
"Bolus injection could potentially be a safe and effective means of administering remifentanil in clinical situations requiring a brief period of intense analgesia."( Remifentanil by bolus injection: a safety, pharmacokinetic, pharmacodynamic, and age effect investigation in human volunteers.
Egan, TD; Kern, SE; Muir, KT; White, J, 2004
)
0.32
" Safety and tolerability were assessed using telemetry, Holter monitoring, surface ECG, vital signs, safety laboratories, and adverse event reports."( Single oral dose safety, tolerability, and pharmacokinetics of PNU-96391 in healthy volunteers.
Adams, G; Azie, NE; Bombardt, PA; Donaldson, K; Francom, SF; Rodríguez, CA; Staton, BA, 2004
)
0.32
" There were no statistically significant differences between the renal function groups in the incidence of adverse events, and no deaths were attributable to remifentanil use."( Offset of pharmacodynamic effects and safety of remifentanil in intensive care unit patients with various degrees of renal impairment.
Albrecht, S; Bach, V; Bodenham, A; Bonde, J; Breen, D; Kessler, P; Shaikh, S; Wilmer, A, 2004
)
0.32
" Overall, all treatments were safe and well tolerated."( Efficacy and safety of ebastine 20 mg compared to loratadine 10 mg once daily in the treatment of seasonal allergic rhinitis: a randomized, double-blind, placebo-controlled study.
Hampel, F; Howland, W; Ratner, P; Van Bavel, J, 2004
)
0.32
" There was no significant difference among all groups in the number of patients who reported adverse events."( A randomized, double-blind, placebo-controlled study comparing the efficacy and safety of ebastine (20 mg and 10 mg) to loratadine 10 mg once daily in the treatment of seasonal allergic rhinitis.
Hampel, F; Howland, W; Ratner, P; Van Bavel, J, 2004
)
0.32
"6 %)treatment was withdrawn because of mostly gastrointestinal adverse events."( Effectiveness and safety of cholinesterase inhibitors in elderly subjects with Alzheimer's disease: a "real world" study.
Bardelli, F; Bencini, F; Biagini, CA; Caleri, V; Cantini, C; Cavallini, MC; Marini, M; Masotti, G; Mecacci, R; Mossello, E; Razzi, E; Sarcone, E; Tilli, S; Tonon, E, 2004
)
0.32
" Analgesia-based sedation with remifentanil was very effective, well tolerated and had a similar adverse event and haemodynamic profile to those of hypnotic-based regimens when used in critically ill neuro-intensive care unit patients for up to 5 days."( Safety and efficacy of analgesia-based sedation with remifentanil versus standard hypnotic-based regimens in intensive care unit patients with brain injuries: a randomised, controlled trial [ISRCTN50308308].
Karabinis, A; Kirkham, AJ; Komnos, A; Mandragos, K; Soukup, J; Speelberg, B; Stergiopoulos, S, 2004
)
0.32
" Data both from clinical trials and studies in routine clinical practice have shown that donepezil is associated with a low incidence of GI adverse events (AEs) that is comparable with placebo."( The safety and tolerability of donepezil in patients with Alzheimer's disease.
Ham, RJ; Jackson, S; Wilkinson, D, 2004
)
0.32
" Safety was evaluated by physical and laboratory evaluations and the monitoring of adverse events (AEs)."( Concurrent administration of donepezil HCl and sertraline HCl in healthy volunteers: assessment of pharmacokinetic changes and safety following single and multiple oral doses.
Cullen, EI; Kumar, D; Nagy, CF; Perdomo, CA; Pratt, RD; Wason, S, 2004
)
0.32
" Safety assessments included monitoring adverse events, and the Unified Parkinson's Disease Rating Scale (UPDRS) motor examination."( Concurrent administration of donepezil HCl and levodopa/carbidopa in patients with Parkinson's disease: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Hahne, WA; Kirby, L; Kumar, D; Okereke, CS; Pratt, RD, 2004
)
0.32
" The number of PD patients who experienced at least one adverse event during the study (13/25) was higher when they received donepezil HCl than when they received placebo (5/25), but was the same as healthy subjects who received donepezil HCl only (13/26)."( Concurrent administration of donepezil HCl and levodopa/carbidopa in patients with Parkinson's disease: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Hahne, WA; Kirby, L; Kumar, D; Okereke, CS; Pratt, RD, 2004
)
0.32
" Co-administration of the two drugs led to a small increase in adverse events compared with administration of levodopa/carbidopa alone in PD patients."( Concurrent administration of donepezil HCl and levodopa/carbidopa in patients with Parkinson's disease: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Hahne, WA; Kirby, L; Kumar, D; Okereke, CS; Pratt, RD, 2004
)
0.32
" The most common adverse event in both treatment groups was diarrhoea (6/16 risperidone + donepezil HCl patients and 9/16 donepezil HCl only subjects)."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.32
" elegans strain PC72 (lacZ, heat shock protein-16 [hsp-16] construct) was used as a report organism for toxic effects."( Caenorhabditis elegans as model system for rapid toxicity assessment of pharmaceutical compounds.
Dengg, M; van Meel, JC,
)
0.13
" These results suggest that donepezil exerts a neuroprotective effect by reducing the amount of the toxic form of Abeta fibrils in septal neuron cultures."( Protective effect of donepezil against Abeta(1-40) neurotoxicity in rat septal neurons.
Akasofu, S; Kimura, M; Ogura, H; Sawada, K, 2005
)
0.33
" The LD50 of (+)-D-ammodendrine in mice was determined to be 94."( Ammodendrine and N-methylammodendrine enantiomers: isolation, optical rotation, and toxicity.
Chang, CW; Gardner, DR; Garrossian, M; Lee, ST; Molyneux, RJ; Panter, KE; Pfister, JA, 2005
)
0.33
" This review will concentrate on the adverse effects of remifentanil given by bolus injection, either alone or in the context of a background infusion."( The safety of remifentanil by bolus injection.
Egan, TD; Richardson, SP, 2005
)
0.33
" Their use is frequently associated with dose-limiting adverse effects."( Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.
Berzsenyi, P; Farkas, S; Kárpáti, E; Kocsis, P; Tarnawa, I,
)
0.13
" For detecting side effect liability (ataxia, sedation, impairment of voluntary motor functions), (1) the rota-rod test, (2) measurement of spontaneous motility, (3) the weight-lifting test and (4) the thiopental sleep test were used."( Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.
Berzsenyi, P; Farkas, S; Kárpáti, E; Kocsis, P; Tarnawa, I,
)
0.13
"Therapeutic indices calculated from the results of these in vivo experiments for the clinically used muscle relaxants are in agreement with their adverse effect profiles in humans."( Simple pharmacological test battery to assess efficacy and side effect profile of centrally acting muscle relaxant drugs.
Berzsenyi, P; Farkas, S; Kárpáti, E; Kocsis, P; Tarnawa, I,
)
0.13
"To provide a systematic review of the best quality evidence of the effects of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in people with mild to moderately-severe AD."( A systematic review of the clinical effectiveness of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in Alzheimer's disease.
Clegg, A; Green, C; Kirby, J; Loveman, E; Payne, E; Picot, J; Takeda, A, 2006
)
0.33
" Adverse events were generally related to the gastrointestinal system, with a tendency for these to be more common in the treatment arms."( A systematic review of the clinical effectiveness of donepezil, rivastigmine and galantamine on cognition, quality of life and adverse events in Alzheimer's disease.
Clegg, A; Green, C; Kirby, J; Loveman, E; Payne, E; Picot, J; Takeda, A, 2006
)
0.33
" Twenty-four drug-related adverse events were recorded of which four were regarded as serious."( Efficacy and safety of high-dose cabergoline in Parkinson's disease.
Ludolph, A; Odin, P; Oehlwein, C; Polzer, U; Renner, R; Schüler, P; Shing, M; Storch, A; Werner, G, 2006
)
0.33
" Moreover, NMDAR involvement causes the fatal activation of calpain, which, in turn, degrades tau protein into a 17-kDa peptide and possibly other highly toxic N-terminal peptides."( NMDA receptor mediates tau-induced neurotoxicity by calpain and ERK/MAPK activation.
Amadoro, G; Calissano, P; Canu, N; Cestari, V; Ciotti, MT; Costanzi, M, 2006
)
0.33
" After providing evidence that the cardiovascular liabilities were not a function of MCHr1 antagonism, continued screening identified the chromone-substituted aminopiperidine amides as a class of MCHr1 antagonists that demonstrated a safe cardiovascular profile at high drug concentrations in both plasma and brain."( Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Brodjian, S; Campbell, TJ; Collins, CA; Dayton, BD; Freeman, JC; Fryer, RM; Gao, J; Hernandez, L; Iyengar, R; Judd, AS; Kym, PR; Lynch, JK; Marsh, KC; Mulhern, M; Napier, JJ; Polakowski, JS; Preusser, LC; Reilly, RM; Reinhart, GA; Segreti, JA; Sham, HL; Souers, AJ; Vasudevan, A; Wagaw, SH; Wodka, D; Zhao, G, 2006
)
0.33
" Donepezil is expected to be therapeutically useful and safe in treating DLB patients, indicating marked improvements in behavioral and psychological symptoms of dementia (BPSD) rather than in cognitive deficit, without deteriorating parkinsonism."( Efficacy and safety of donepezil in patients with dementia with Lewy bodies: preliminary findings from an open-label study.
Iseki, E; Kosaka, K; Mori, E; Mori, S, 2006
)
0.33
" Adverse events were monitored up to 30 days after the last dose of study drug was administered."( A double-blind, randomized, placebo-controlled phase III study of the safety of alvimopan in patients who undergo simple total abdominal hysterectomy.
Coleman, RL; Du, W; Fort, JG; Gabriel, K; Guerrieri, JP; Herzog, TJ; Techner, L; Wallin, B, 2006
)
0.33
"Overall, the most common adverse events were nausea, vomiting, and constipation; < 5% of patients discontinued use because of adverse events."( A double-blind, randomized, placebo-controlled phase III study of the safety of alvimopan in patients who undergo simple total abdominal hysterectomy.
Coleman, RL; Du, W; Fort, JG; Gabriel, K; Guerrieri, JP; Herzog, TJ; Techner, L; Wallin, B, 2006
)
0.33
" One hundred and thirteen adverse drug reactions (ADRs) were reported, with the most frequently specified being diarrhoea (10), abdominal pain (10) and nausea/vomiting (9)."( Safety profile of repaglinide as used in general practice in England: results of a prescription-event monitoring study.
Marshall, V; Shakir, S; Wilton, L, 2006
)
0.33
" Mild and transient adverse events were observed in 6% of akatinol memantine group."( [Clinical efficacy and safety of akatinol memantine in treatment of mild to moderate Alzheimer disease: a donepezil-controlled, randomized trial].
Hu, HT; Ji, CJ; Tang, HC; Wang, YH; Xu, T; Yao, JL; Yu, HZ; Zhang, ZX, 2006
)
0.33
"As a safe and effective medicine, akatinol memantine, which has a similar effect as donepezil for AD, can remarkably improve the cognition, behavior, and mood of AD patients."( [Clinical efficacy and safety of akatinol memantine in treatment of mild to moderate Alzheimer disease: a donepezil-controlled, randomized trial].
Hu, HT; Ji, CJ; Tang, HC; Wang, YH; Xu, T; Yao, JL; Yu, HZ; Zhang, ZX, 2006
)
0.33
"0 mug per intravenous injection, based on the combined no observable adverse effect levels (NOAEL, mg/m(2)) measured in these species."( Preclinical acute toxicity studies and dosimetry estimates of the novel sigma-1 receptor radiotracer, [18F]SFE.
Chang, RC; Mirsalis, JC; Ng, H; Schindler-Horvat, J; Stabin, MG; Waterhouse, RN; Zhao, J,
)
0.13
" Donepezil was well tolerated; 51% of patients experienced adverse events, most commonly diarrhea (5."( Safety and efficacy of donepezil in African Americans with mild-to-moderate Alzheimer's disease.
Goldman, R; Griffith, P; Lichtenberg, P; Payne-Parrish, J, 2006
)
0.33
"These results suggest that donepezil is effective and safe in treating African Americans with mild-to-moderate AD, and support the value of FOME in assessing efficacy in AD trials in diverse populations."( Safety and efficacy of donepezil in African Americans with mild-to-moderate Alzheimer's disease.
Goldman, R; Griffith, P; Lichtenberg, P; Payne-Parrish, J, 2006
)
0.33
" Overall, 85% of patients experienced at least one adverse event (AE)."( Efficacy and safety of donepezil over 3 years: an open-label, multicentre study in patients with Alzheimer's disease.
Burns, A; Gauthier, S; Perdomo, C, 2007
)
0.34
"These results support the conclusion that donepezil is safe and effective for the long-term treatment of patients with mild to moderate AD."( Efficacy and safety of donepezil over 3 years: an open-label, multicentre study in patients with Alzheimer's disease.
Burns, A; Gauthier, S; Perdomo, C, 2007
)
0.34
" The cytotoxicity of FC-TEMPO in the high metastatic lung carcinoma cells (95-D) showed that it markedly inhibited the viability of cancer cells in a dose-dependent manner, while it was less toxic to a normal human cell line."( Cytotoxicity of a newly synthesized nitroxide derivative of 4-ferrocenecarboxyl-2,2,6,6-tetramethylpiperidine-1-oxyl in high metastatic lung tumor cells.
Han, J; Lan, MB; Li, CL; Liu, JW; Miao, LD; Tang, W; Wu, Y, 2006
)
0.33
" Patients were treated every 21 days until progression or intolerable adverse events (AEs)."( A phase II study of the safety and efficacy of the multidrug resistance inhibitor VX-710 combined with doxorubicin and vincristine in patients with recurrent small cell lung cancer.
Gandhi, L; Harding, MW; Johnson, BE; Langer, CJ; Lynch, TJ; Moore, M; Neubauer, M; Ross, HJ, 2007
)
0.34
" The incidence of adverse events was comparable in both groups."( Fast-track cardiac anesthesia: efficacy and safety of remifentanil versus sufentanil.
Conzen, P; Lison, S; Schill, M, 2007
)
0.34
"Remifentanil for fast-track cardiac anesthesia provided safe and stable operating conditions and facilitated earlier tracheal extubation."( Fast-track cardiac anesthesia: efficacy and safety of remifentanil versus sufentanil.
Conzen, P; Lison, S; Schill, M, 2007
)
0.34
"Cardiovascular disorders are the most frequently reported adverse effects of drugs used to treat Alzheimer's disease."( Anti-Alzheimer drugs: life-threatening adverse effects.
, 2007
)
0.34
" In addition, no differences were observed in the safety of ebastine between patients with renal impairment and healthy subjects when assessing adverse events, vital signs, laboratory parameters or ECGs."( Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.
Noveck, RJ; Preston, RA; Swan, SK, 2007
)
0.34
" The side effects were mild, transient, and consistent with the adverse events noted with cholinesterase inhibitors."( Preliminary study of the safety and efficacy of donepezil hydrochloride in children with Down syndrome: a clinical report series.
Crissman, BG; Dawson, D; Eells, R; Heller, JH; Kishnani, PS; Li, J; Spiridigliozzi, GA; Sullivan-Saarela, JA, 2007
)
0.34
" Treatment-emergent adverse events (AEs) were observed for 54."( Efficacy and safety of donepezil in patients with schizophrenia or schizoaffective disorder: significant placebo/practice effects in a 12-week, randomized, double-blind, placebo-controlled trial.
Buchanan, RW; Goldman, R; Kane, JM; Keefe, RS; Li, C; Malhotra, AK; Meltzer, HY; Murthy, A; Sovel, M, 2008
)
0.35
" Trial methods, clinical characteristics, outcomes, and adverse events were extracted and checked."( Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis of randomised controlled trials.
Kavirajan, H; Schneider, LS, 2007
)
0.34
" Compared with placebo, more dropouts and adverse events (anorexia, nausea, vomiting, diarrhoea, and insomnia) occurred with the cholinesterase inhibitors, but not with memantine."( Efficacy and adverse effects of cholinesterase inhibitors and memantine in vascular dementia: a meta-analysis of randomised controlled trials.
Kavirajan, H; Schneider, LS, 2007
)
0.34
"The combination of repaglinide, metformin and bedtime NPH is safe and effective and it provides better postprandial blood glucose control."( Safety and efficacy of repaglinide in combination with metformin and bedtime NPH insulin as an insulin treatment regimen in type 2 diabetes.
Civera, M; Martínez, I; Merchante, A; Salvador, M; Sanz, J, 2008
)
0.35
"Ebastine is safe and effective in preventing the symptoms of ACU."( Acquired cold urticaria symptoms can be safely prevented by ebastine.
Magerl, M; Maurer, M; Metz, M; Schmolke, J; Siebenhaar, F; Zuberbier, T, 2007
)
0.34
" Thus, developing safe NMDAR antagonists is of high therapeutic interest."( Comparison of the pharmacological properties of GK11 and MK801, two NMDA receptor antagonists: towards an explanation for the lack of intrinsic neurotoxicity of GK11.
Becerril Ortega, J; Buisson, A; Crouzin, N; Desmadryl, G; Hirbec, H; Privat, A; Teigell, M; Vandame, D, 2007
)
0.34
"Since the prevalence of obesity continues to increase, there is a demand for effective and safe anti-obesity agents that can produce and maintain weight loss and improve comorbidity."( Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials.
Astrup, A; Bartels, EM; Bliddal, H; Christensen, R; Kristensen, PK, 2007
)
0.34
" Rimonabant caused significantly more adverse events than did placebo (OR=1."( Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials.
Astrup, A; Bartels, EM; Bliddal, H; Christensen, R; Kristensen, PK, 2007
)
0.34
"Our findings suggest that 20 mg per day rimonabant increases the risk of psychiatric adverse events--ie, depressed mood disorders and anxiety-despite depressed mood being an exclusion criterion in these trials."( Efficacy and safety of the weight-loss drug rimonabant: a meta-analysis of randomised trials.
Astrup, A; Bartels, EM; Bliddal, H; Christensen, R; Kristensen, PK, 2007
)
0.34
" Generally, rimonabant has been well tolerated, with a primary side effect of nausea."( Cannabinoid-1 receptor blockade in cardiometabolic risk reduction: safety, tolerability, and therapeutic potential.
Cannon, CP; Steinberg, BA, 2007
)
0.34
" At 1 year, adverse events more frequently reported with rimonabant were gastrointestinal, neurological, and psychiatric in nature."( Efficacy and safety of rimonabant for improvement of multiple cardiometabolic risk factors in overweight/obese patients: pooled 1-year data from the Rimonabant in Obesity (RIO) program.
Després, JP; McCarthy, C; Pi-Sunyer, X; Scheen, A; Van Gaal, L, 2008
)
0.35
" Rimonabant was generally well tolerated, with more frequently reported adverse events being gastrointestinal, neurological, and psychiatric in nature."( Efficacy and safety of rimonabant for improvement of multiple cardiometabolic risk factors in overweight/obese patients: pooled 1-year data from the Rimonabant in Obesity (RIO) program.
Després, JP; McCarthy, C; Pi-Sunyer, X; Scheen, A; Van Gaal, L, 2008
)
0.35
" Higher doses of donepezil, if safe and well tolerated, might provide further benefits for patients with AD."( Safety and tolerability of donepezil at doses up to 20 mg/day: results from a pilot study in patients with Alzheimer's disease.
Corey-Bloom, J; Doody, RS; Ieni, J; Li, H; Schindler, R; Zhang, R, 2008
)
0.35
" Primary outcome measures were tolerability (as determined by monitoring of discontinuations, dose modifications and adverse events) and safety (as determined by adverse event monitoring, physical examinations, clinical laboratory tests and ECGs)."( Safety and tolerability of donepezil at doses up to 20 mg/day: results from a pilot study in patients with Alzheimer's disease.
Corey-Bloom, J; Doody, RS; Ieni, J; Li, H; Schindler, R; Zhang, R, 2008
)
0.35
"No patients withdrew from the study and there were no serious adverse events or deaths."( Safety and tolerability of donepezil at doses up to 20 mg/day: results from a pilot study in patients with Alzheimer's disease.
Corey-Bloom, J; Doody, RS; Ieni, J; Li, H; Schindler, R; Zhang, R, 2008
)
0.35
"In this small pilot study of patients with mild-to-moderate AD already stabilized on donepezil 10 mg/day, doses of 15 and 20 mg/day of donepezil appeared safe and well tolerated."( Safety and tolerability of donepezil at doses up to 20 mg/day: results from a pilot study in patients with Alzheimer's disease.
Corey-Bloom, J; Doody, RS; Ieni, J; Li, H; Schindler, R; Zhang, R, 2008
)
0.35
" Patients exposed to 3 dose ranges of iloperidone, another antipsychotic, or placebo were compared on rates of serious adverse events (SAEs), adverse events (AEs), extrapyramidal symptoms, akathisia, prolactin, weight and metabolic parameters, QTc, and other standard safety parameters."( Safety profile of iloperidone: a pooled analysis of 6-week acute-phase pivotal trials.
Cutler, AJ; Polymeropoulos, MH; Weiden, PJ; Wolfgang, CD, 2008
)
0.35
" The most common adverse events were insomnia (18."( Long-term efficacy and safety of iloperidone: results from 3 clinical trials for the treatment of schizophrenia.
Di Marino, M; Kane, JM; Laska, E; Lauriello, J; Wolfgang, CD, 2008
)
0.35
" The most frequent adverse events were infections and gastrointestinal (abdominal pain, diarrhea, dyspepsia, and vomiting)."( Phase 1 dose-escalation study of CP-690 550 in stable renal allograft recipients: preliminary findings of safety, tolerability, effects on lymphocyte subsets and pharmacokinetics.
Brennan, D; Chan, G; Chow, V; Gaston, R; Krishnaswami, S; Mendez, R; Ni, G; Pescovitz, MD; Pirsch, J; Swan, S; van Gurp, E; Wang, C; Weimar, W, 2008
)
0.35
" Across trials, the incidence of adverse events was generally lowest for donepezil and highest for rivastigmine."( Efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer's disease: a systematic review and meta-analysis.
Gartlehner, G; Hansen, RA; Jonas, DE; Moore, CG; Morgan, LC; Webb, AP, 2008
)
0.35
" Overall, incidences of adverse events (67."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin in patients with type 2 diabetes and inadequate glycemic control: a randomized, double-blind, placebo-controlled study.
DeFronzo, RA; Fleck, PR; Mekki, Q; Wilson, CA, 2008
)
0.35
" Masitinib was generally well tolerated, with mild (grade I) or moderate (grade II) diarrhea or vomiting as the most common adverse events."( Masitinib is safe and effective for the treatment of canine mast cell tumors.
Devauchelle, P; Dubreuil, P; Hahn, KA; Hermine, O; Kinet, JP; Leblanc, A; Legendre, A; Leventhal, PS; Moussy, A; Ogilvie, G; Oglivie, G; Palmerini, F; Powers, B; Rusk, T,
)
0.13
"Masitinib is safe and effective at delaying tumor progression in dogs presenting with recurrent or nonresectable grade II or III nonmetastatic MCT."( Masitinib is safe and effective for the treatment of canine mast cell tumors.
Devauchelle, P; Dubreuil, P; Hahn, KA; Hermine, O; Kinet, JP; Leblanc, A; Legendre, A; Leventhal, PS; Moussy, A; Ogilvie, G; Oglivie, G; Palmerini, F; Powers, B; Rusk, T,
)
0.13
" plus single-dose insulin glargine regimen was safe for low-risk type 2 diabetic patients who insisted on fasting during Ramadan."( Repaglinide plus single-dose insulin glargine: a safe regimen for low-risk type 2 diabetic patients who insist on fasting in Ramadan.
Bakiner, O; Bozkirli, E; Demirag, NG; Ertorer, ME; Tutuncu, NB, 2009
)
0.35
" Most patients tolerated the treatment well, with only 2 discontinuing because of adverse events."( Effectiveness and safety of donepezil in Hispanic patients with Alzheimer's disease: a 12-week open-label study.
Kassalow, LM; Li, H; Lopez, OL; Mackell, JA; McRae, T; Sun, Y; Xu, Y, 2008
)
0.35
" Overall, adverse events (AEs) observed with alogliptin were not substantially different from those observed with placebo."( Efficacy and safety of adding the dipeptidyl peptidase-4 inhibitor alogliptin to metformin therapy in patients with type 2 diabetes inadequately controlled with metformin monotherapy: a multicentre, randomised, double-blind, placebo-controlled study.
Ellis, GC; Fleck, PR; Mekki, Q; Nauck, MA; Wilson, CA, 2009
)
0.35
"Alogliptin is an effective and safe treatment for type 2 diabetes when added to metformin for patients not sufficiently controlled on metformin monotherapy."( Efficacy and safety of adding the dipeptidyl peptidase-4 inhibitor alogliptin to metformin therapy in patients with type 2 diabetes inadequately controlled with metformin monotherapy: a multicentre, randomised, double-blind, placebo-controlled study.
Ellis, GC; Fleck, PR; Mekki, Q; Nauck, MA; Wilson, CA, 2009
)
0.35
" The incidence of treatment emergent adverse events was similar for bilastine (20."( Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients.
Bachert, C; Dimitrov, V; Gorina, MM; Ivan, P; Kuna, P; Loureiro, A; Sanquer, F; van de Heyning, P, 2009
)
0.35
"Bilastine 20 mg once daily was efficacious, safe and not different from desloratadine 5 mg once daily in the treatment of SAR symptoms."( Comparison of the efficacy and safety of bilastine 20 mg vs desloratadine 5 mg in seasonal allergic rhinitis patients.
Bachert, C; Dimitrov, V; Gorina, MM; Ivan, P; Kuna, P; Loureiro, A; Sanquer, F; van de Heyning, P, 2009
)
0.35
"Biochemically validated 4-week continuous abstinence at end-of-treatment (weeks 6-9; primary end-point); 7-day point prevalence abstinence at weeks 9 and 24; sustained abstinence (weeks 6-24); change in body weight; and adverse events."( A randomized controlled trial of adding the nicotine patch to rimonabant for smoking cessation: efficacy, safety and weight gain.
Chang, Y; Dale, LC; Gonzales, D; Lawrence, D; Rigotti, NA, 2009
)
0.35
" Serious adverse event rates did not differ between groups."( A randomized controlled trial of adding the nicotine patch to rimonabant for smoking cessation: efficacy, safety and weight gain.
Chang, Y; Dale, LC; Gonzales, D; Lawrence, D; Rigotti, NA, 2009
)
0.35
"The Leipzig fast-track protocol for cardio-anesthesia including the central elements of switching opiate therapy to remifentanil and switching patient recovery to a special post-anesthesia recovery and care unit, shortened therapy times, is safe and economically effective."( [Leipzig fast-track protocol for cardio-anesthesia. Effective, safe and economical].
Ender, J; Fassl, J; Funkat, AK; Häntschel, D; Scholz, M; Sommer, M; Wittmann, M, 2009
)
0.35
" Adverse events were consistent with the known donepezil safety profile."( Long-term safety and efficacy of donepezil in patients with severe Alzheimer's disease: results from a 52-week, open-label, multicenter, extension study in Japan.
Arimoto, I; Asada, T; Homma, A; Imai, Y; Iwamoto, T; Koma, H; Ohbayashi, T; Shigeta, M; Tago, H; Takase, T; Takita, M, 2009
)
0.35
"Donepezil is effective and safe for symptomatic treatment of severe AD for at least 1 year."( Long-term safety and efficacy of donepezil in patients with severe Alzheimer's disease: results from a 52-week, open-label, multicenter, extension study in Japan.
Arimoto, I; Asada, T; Homma, A; Imai, Y; Iwamoto, T; Koma, H; Ohbayashi, T; Shigeta, M; Tago, H; Takase, T; Takita, M, 2009
)
0.35
"To investigate spontaneous reports of TdP present in the public version of the FDA Adverse Event Reporting System (AERS) in the light of what is already known on their TdP-liability."( Drug-induced torsades de pointes: data mining of the public version of the FDA Adverse Event Reporting System (AERS).
De Ponti, F; Moretti, U; Poluzzi, E; Raschi, E, 2009
)
0.35
" Cases were represented by TdP reports, whereas non-cases were all reports of adverse drug reactions other than TdP."( Drug-induced torsades de pointes: data mining of the public version of the FDA Adverse Event Reporting System (AERS).
De Ponti, F; Moretti, U; Poluzzi, E; Raschi, E, 2009
)
0.35
"Large spontaneous reporting databases represent an important source for signal detection of rare adverse drug reactions (ADR), such as TdP."( Drug-induced torsades de pointes: data mining of the public version of the FDA Adverse Event Reporting System (AERS).
De Ponti, F; Moretti, U; Poluzzi, E; Raschi, E, 2009
)
0.35
"Remifentanil is safe and highly effective for pain control during percutaneous transhepatic biliary drainage."( Safety and effectiveness of analgesia with remifentanil for percutaneous transhepatic biliary drainage.
Bae, JI; Lee, HS; Park, AW; Park, NS; Won, JH, 2009
)
0.35
" Adverse events occurred in 205 (77%) patients in the single-dose oral casopitant mesylate group and 203 (75%) patients in the 3-day intravenous and oral casopitant mesylate group compared with 194 (73%) of patients in the control group."( Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenic chemotherapy: a randomised, double-blind, placebo-contr
Aziz, Z; Grunberg, SM; Guckert, M; Herrstedt, J; Lane, S; Rolski, J; Russo, MW; Strausz, J; Wissel, P; Wright, O, 2009
)
0.35
" Safety was assessed according to adverse events (AEs), laboratory tests and electrocardiograms."( Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo for the symptomatic treatment of seasonal allergic rhinitis: a randomized, double-blind, parallel-group study.
Agache, I; Bachert, C; Fouquert, L; Kuna, P; Nowacki, Z; Roger, A; Sologuren, A; Valiente, R; van Cauwenberge, P, 2009
)
0.35
"The objective of this article was to estimate the risk of discontinuation due to adverse events in trials of orlistat, sibutramine and rimonabant."( Discontinuation due to adverse events in randomized trials of orlistat, sibutramine and rimonabant: a meta-analysis.
DeSantis, SM; Johansson, K; Neovius, K; Neovius, M; Rössner, S, 2009
)
0.35
" Multiple mechanisms concur in generating the damage, but activation of oxidative stress may contribute to the final toxic effect."( The non-peptidyl low molecular weight radical scavenger IAC protects human pancreatic islets from lipotoxicity.
Boggi, U; Bonamassa, B; Canistro, D; D'Aleo, V; Del Guerra, S; Del Prato, S; Filipponi, F; Lupi, R; Martano, M; Paolini, M; Soleti, A; Valgimigli, L, 2009
)
0.35
" It may potentially have a lower incidence of adverse events than other antipsychotic agents."( The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study.
Garcia, E; Nakamura, H; Peris, F; Robert, M; Sato, N; Terazawa, Y, 2009
)
0.35
" Patients were assessed weekly for clinical efficacy, adverse events, extrapyramidal symptoms (EPS) and drug compliance, and were assessed biweekly for other safety variables."( The efficacy and safety of blonanserin compared with haloperidol in acute-phase schizophrenia: a randomized, double-blind, placebo-controlled, multicentre study.
Garcia, E; Nakamura, H; Peris, F; Robert, M; Sato, N; Terazawa, Y, 2009
)
0.35
"To determine the efficacy, safety, and tolerability of 3 different dosages of CP-690,550, a potent, orally active JAK inhibitor, in patients with active rheumatoid arthritis (RA) in whom methotrexate, etanercept, infliximab, or adalimumab caused an inadequate or toxic response."( The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo.
Bloom, BJ; Breedveld, FC; Burgos-Vargas, R; Coombs, JH; Fletcher, MP; Gruben, D; Kremer, JM; Krishnaswami, S; Wilkinson, B; Zerbini, CA; Zwillich, SH, 2009
)
0.35
" The most common adverse events reported were headache and nausea."( The safety and efficacy of a JAK inhibitor in patients with active rheumatoid arthritis: Results of a double-blind, placebo-controlled phase IIa trial of three dosage levels of CP-690,550 versus placebo.
Bloom, BJ; Breedveld, FC; Burgos-Vargas, R; Coombs, JH; Fletcher, MP; Gruben, D; Kremer, JM; Krishnaswami, S; Wilkinson, B; Zerbini, CA; Zwillich, SH, 2009
)
0.35
"Acetylcholinesterase inhibitors (AChIs) are widely used in the treatment of mild-to-moderate Alzheimer's disease (AD), but their cholinergic effects could generate adverse side effects in the cardiovascular system."( Donepezil-induced adverse side effects of cardiac rhythm: 2 cases report of atrioventricular block and Torsade de Pointes.
Hiramatsu, Y; Koga, S; Tanaka, A, 2009
)
0.35
" Adverse event rates were comparable to AD studies."( The efficacy, safety, and tolerability of donepezil for the treatment of young adults with Down syndrome.
Capone, GT; Handen, BL; Heller, JH; Kishnani, PS; McRae, T; Richardson, S; Seltzer, B; Sommer, BR; Spiridigliozzi, GA, 2009
)
0.35
" There appears to be a dose relationship for adverse events such as dizziness, somnolence and dry mouth; for example NNH vs."( Iloperidone for schizophrenia: a review of the efficacy and safety profile for this newly commercialised second-generation antipsychotic.
Citrome, L, 2009
)
0.35
" Although, the response to bronchoconstriction in dogs and rats was different from humans, the two species presented ventilatory changes that highlight the potential adverse effect of test articles."( Respiratory safety pharmacology: positive control drug responses in Sprague-Dawley rats, Beagle dogs and cynomolgus monkeys.
Authier, S; Gauvin, D; Legaspi, M; Troncy, E, 2009
)
0.35
" The incidences of overall adverse events and hypoglycemia were similar across treatment groups, but cardiac events occurred more often with active treatment than placebo."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin added to pioglitazone in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled study.
Fleck, PR; Mekki, Q; Pratley, RE; Reusch, JE; Wilson, CA, 2009
)
0.35
"Galantamine, a centrally acting cholinesterase (ChE) inhibitor and a nicotinic allosteric potentiating ligand used to treat Alzheimer's disease, is an effective and safe antidote against poisoning with nerve agents, including soman."( Effectiveness of donepezil, rivastigmine, and (+/-)huperzine A in counteracting the acute toxicity of organophosphorus nerve agents: comparison with galantamine.
Adler, M; Akkerman, M; Albuquerque, EX; Aracava, Y; Pereira, EF, 2009
)
0.35
" Adverse event reporting with arzoxifene was similar to that with raloxifene, as were hot flush and night sweat reporting."( Effects of arzoxifene on bone, lipid markers, and safety parameters in postmenopausal women with low bone mass.
Cox, DA; Downs, RW; Dowsett, SA; Ghosh, A; Harper, K; Moffett, AM, 2010
)
0.36
" Relative risks (RR) with 95% confidence interval for relevant adverse events and number needed to harm was calculated."( Systematic review and meta-analysis on the adverse events of rimonabant treatment: considerations for its potential use in hepatology.
Bedogni, G; Chavez-Tapia, NC; Crocè, LS; Masutti, F; Tellez-Avila, FI; Tiribelli, C, 2009
)
0.35
"Rimonabant is associated with an increased risk of adverse events."( Systematic review and meta-analysis on the adverse events of rimonabant treatment: considerations for its potential use in hepatology.
Bedogni, G; Chavez-Tapia, NC; Crocè, LS; Masutti, F; Tellez-Avila, FI; Tiribelli, C, 2009
)
0.35
" Safety was assessed according to adverse events, laboratory tests and electrocardiograms."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010
)
0.36
" Comparison with levocetirizine indicated both treatments to be equally efficacious as well as equally safe and well tolerated as compared with placebo."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010
)
0.36
"Bilastine 20 mg is a novel effective and safe treatment option for the management of CU."( Comparison of the efficacy and safety of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic idiopathic urticaria: a multi-centre, double-blind, randomized, placebo-controlled study.
Antépara, I; Bogacka, E; Jáuregui, I; Medina, I; Oanta, A; Uhl, P; Valiente, R; Wesel, F; Zuberbier, T, 2010
)
0.36
" Fewer donepezil-treated subjects withdrew due to adverse events (AEs) compared with rivastigmine and galantamine-treated subjects."( Safety and tolerability of donepezil, rivastigmine and galantamine for patients with Alzheimer's disease: systematic review of the 'real-world' evidence.
Kelly, S; Lockhart, IA; Mitchell, SA, 2009
)
0.35
" Adverse events (AEs) were recorded throughout."( Safety and tolerability of donepezil in mild cognitive impairment: open-label extension study.
Doody, RS; Ferris, S; Gao, J; Goldman, R; Murthy, AK; Salloway, S, 2010
)
0.36
"The objective was to investigate the frequency of adverse events (AE) as a cause for discontinuation of donepezil treatment for Alzheimer's dementia (DAT) in a geriatric memory unit."( [Adverse events causing discontinuation of donepezil for Alzheimer's dementia].
Carøe, TK; Moe, C, 2009
)
0.35
" Safety outcomes included adverse events (AEs), discontinuations caused by AEs and serious AEs (SAEs)."( Safety and tolerability of rivastigmine transdermal patch compared with rivastigmine capsules in patients switched from donepezil: data from three clinical trials.
Farlow, MR; Meng, X; Olin, JT; Sadowsky, CH, 2010
)
0.36
"A synopsis of the unique pharmacokinetic properties of remifentanil and its action on major organ systems will provide insight on the safe and effective use of the drug in a variety of clinical settings."( Remifentanil, a different opioid: potential clinical applications and safety aspects.
Manolaraki, M; Paspatis, GA; Stroumpos, C, 2010
)
0.36
" The most common suspected adverse events were nausea, vomiting, rash, diarrhoea, peripheral oedema, anaemia, lymphopenia, thrombocytopenia, pyrexia, neutropenia, asthenia, leucopenia, and abdominal pain, and most were of grades 1-2 severity."( Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer.
Deplanque, G; Hammel, P; Hermine, O; Kinet, JP; Levy, P; Mitry, E; Mornex, F; Moussy, A; Raymond, E; Rougier, P; Seitz, JF, 2010
)
0.36
"Repaglinide is considered a safe drug; adverse events are mild to moderate which includes hypoglycemia, headache, nausea, vomiting, diarrhea and dyspepsia as similar to sulphonylureas."( Repaglinide induced acute hepototoxicity.
Jaiswal, S; McNamee, W; Mehta, R; Musuku, M; Tran, L,
)
0.13
"The authors aimed to test the hypothesis that xenon anesthesia limits adverse hypotensive effects of losartan during acute hemorrhage."( Xenon/remifentanil anesthesia protects against adverse effects of losartan on hemodynamic challenges induced by anesthesia and acute blood loss.
Boemke, W; Francis, RC; Klein, A; Philippi-Höhne, C; Pickerodt, PA; Reyle-Hahn, MS, 2010
)
0.36
" All active doses seemed to be well tolerated; headache, dizziness, and constipation were the most frequently reported adverse events."( Phase II study to evaluate the safety and efficacy of the oral neurokinin-1 receptor antagonist casopitant (GW679769) administered with ondansetron for the prevention of postoperative and postdischarge nausea and vomiting in high-risk patients.
Blackburn, L; Chung, F; Johnson, B; Kutsogiannis, DJ; Lane, SR; Levin, J; Pergolizzi, JV; Singla, NK; Singla, SK, 2010
)
0.36
" Information regarding safety of triptans while breastfeeding is limited but also reassuring, as the minimal amounts excreted into the milk are insufficient to cause any adverse effects on the breastfeeding infant."( Safety of triptans for migraine headaches during pregnancy and breastfeeding.
Bozzo, P; Duong, S; Einarson, A; Nordeng, H, 2010
)
0.36
" Safety was assessed by adverse events (AEs) and laboratory tests."( Efficacy and safety of donepezil in patients with Alzheimer's disease in assisted living facilities.
Gao, J; Mackell, J; Richardson, S; Rosenblatt, A, 2010
)
0.36
" While initial attempts to target this system using the cannabinoid receptor inverse agonist rimonabant were successful in producing modest weight loss and improving obesity-related metabolic complications in humans, adverse central nervous system side effects precluded introduction of this drug into clinical practice."( Rehashing endocannabinoid antagonists: can we selectively target the periphery to safely treat obesity and type 2 diabetes?
Patti, ME, 2010
)
0.36
" Bepotastine has negligible affinity for receptors associated with undesirable adverse effects, including histamine H(3), α(1)-, α(2)-, and β-adrenergic, serotonin (5-HT(2)), muscarinic, and benzodiazepine receptors."( Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate.
Gow, JA; Klier, SM; McCue, SL; McNamara, TR; Salapatek, AM; Williams, JI, 2010
)
0.36
"Due to psychiatric adverse effects, 50% of subjects in the rimonabant group withdrew, and the study was terminated early (N=10) for safety concerns."( Psychiatric adverse effects of rimonobant in adults with Prader Willi syndrome.
Angulo, MA; Christos, PJ; Hogg, JE; Lipman, EG; Motaghedi, R; Vogiatzi, MG,
)
0.13
" The tolerability profile of iloperidone is noteworthy in terms of modest weight gain, no medically important changes in lipid and glucose, little in the way of prolactin elevation, and an absence of extrapyramidal adverse effects, including akathisia."( Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion.
Citrome, L, 2010
)
0.36
" The present study investigates the molecular etiology of haloperidol neurotoxicity and the role of curcumin, a well-known anti-oxidant, in ameliorating these adverse effects."( Protective effect of curcumin and its combination with piperine (bioavailability enhancer) against haloperidol-associated neurotoxicity: cellular and neurochemical evidence.
Bishnoi, M; Chopra, K; Kulkarni, SK; Rongzhu, L, 2011
)
0.37
" The most frequent adverse events (AEs) for CP-945,598 were: diarrhea, nausea, nasopharyngitis, and headache."( Efficacy and safety of CP-945,598, a selective cannabinoid CB1 receptor antagonist, on weight loss and maintenance.
Aronne, LJ; Chew, RD; England, RD; Finer, N; Fountaine, RJ; Hollander, PA; Klioze, SS; Obourn, JD; Powell, CM, 2011
)
0.37
" Finally, we demonstrated that slices from mice heterozygous for NR2B receptor) in the forebrain are not susceptible to the toxic effects of Aβ(1-42) oligomers but express normal LTP (138 ± 6%)."( Therapeutic significance of NR2B-containing NMDA receptors and mGluR5 metabotropic glutamate receptors in mediating the synaptotoxic effects of β-amyloid oligomers on long-term potentiation (LTP) in murine hippocampal slices.
Deussing, JM; Hasenjäger, A; Parsons, CG; Rammes, G; Sroka-Saidi, K, 2011
)
0.37
"The objective of this study was to determine if healthy cats can tolerate administration of masitinib without clinically relevant adverse effects."( Safety of masitinib mesylate in healthy cats.
Cohen, N; Daly, M; Hermine, O; Moussy, A; Nabity, M; Sheppard, S; Wilson, H,
)
0.13
" An increase in serum creatinine concentration and adverse gastrointestinal effects were noted in some cats."( Safety of masitinib mesylate in healthy cats.
Cohen, N; Daly, M; Hermine, O; Moussy, A; Nabity, M; Sheppard, S; Wilson, H,
)
0.13
" The proportion of women reporting ≥ 1 adverse event did not differ between treatment groups, nor did vaginal bleeding."( Arzoxifene versus raloxifene: effect on bone and safety parameters in postmenopausal women with osteoporosis.
Alam, J; Cox, DA; Dowsett, SA; Kendler, DL; Palacios, S; Stock, J; Zanchetta, J, 2012
)
0.38
" The primary outcome measure was the incidence of adverse events."( Safety and effectiveness of donepezil on behavioral symptoms in patients with Alzheimer disease.
Agüera, L; Carrasco, MM; Gil, P; Leon, T; Moríñigo, A,
)
0.13
"In the present study, AC927 (1-(2-phenethyl)piperidine oxalate), a selective sigma receptor ligand, was tested against the behavioral and toxic effects of cocaine in laboratory animals."( Effects of the selective sigma receptor ligand, 1-(2-phenethyl)piperidine oxalate (AC927), on the behavioral and toxic effects of cocaine.
Coop, A; Fantegrossi, WE; Katz, JL; Li, SM; Matsumoto, RR, 2011
)
0.37
" In this review, we argue that identification of high-risk individuals by a combination of genomic screening, previous risk phenotype, and environmental risk factors offers a promising method for the safe use of centrally acting CB₁ receptor antagonists."( Personalized medicine can pave the way for the safe use of CB₁ receptor antagonists.
Bagdy, G; Hunyady, L; Juhasz, G; Lazary, J, 2011
)
0.37
"Safety analyses comprised examination of the incidence, severity, and timing of treatment-emergent adverse events (AEs) and their relationship to treatment initiation; changes in weight, electrocardiogram, vital signs, and laboratory parameters; and the incidence of premature study discontinuation."( Safety and tolerability of donepezil 23 mg in moderate to severe Alzheimer's disease.
Bibbiani, F; Brand-Schieber, E; Farlow, M; Hsu, T; Moline, M; Satlin, A; Veloso, F; Yardley, J; Zou, H, 2011
)
0.37
" Their known adverse effects include bradycardia."( Bradycardia due to cholinesterase inhibitors: identify adverse effects and take them into account.
, 2011
)
0.37
" Safety endpoints were the occurrence of adverse events, vital sign measurements, physical examination and ECG findings, and laboratory test results recorded over the entire 52-week period."( Efficacy and safety of alogliptin in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, dose-ranging comparison with placebo, followed by a long-term extension study.
Fujita, T; Hirayama, M; Hiroi, S; Kaku, K; Seino, Y, 2011
)
0.37
" The incidence of adverse events with alogliptin over 52 weeks was not dose-dependent and was lower than with voglibose."( Efficacy and safety of alogliptin in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, dose-ranging comparison with placebo, followed by a long-term extension study.
Fujita, T; Hirayama, M; Hiroi, S; Kaku, K; Seino, Y, 2011
)
0.37
" The present paper summarizes the occurrence of alkaloids in the food chain, their mode of action and possible adverse effects including a safety assessment."( Alkaloids in the human food chain--natural occurrence and possible adverse effects.
Dusemund, B; Koleva, II; Rietjens, IM; Soffers, AE; van Beek, TA, 2012
)
0.38
"While new anticancer angiogenesis inhibitors present a well-tolerated safety profile, they are not without adverse events."( [Dermatologic side effects induced by new angiogenesis inhibitors].
Chevreau, C; Cottura, E; Garrido-Stowhas, I; Sibaud, V, 2011
)
0.37
" In addition, bilastine was shown to be safe and well-tolerated over a 1-year treatment period."( Efficacy and safety of bilastine 20 mg compared with cetirizine 10 mg and placebo in the treatment of perennial allergic rhinitis.
Mullol, J; Sastre, J; Valero, A; Valiente, R, 2012
)
0.38
"In randomized clinical trials, adverse events (AEs) are reported for the drug under evaluation and compared with the placebo group."( A systematic review of adverse events in the placebo arm of donepezil trials: the role of cognitive impairment.
Amanzio, M; Benedetti, F; Vase, L, 2012
)
0.38
" Vandetanib was associated with more frequent adverse events."( Efficacy and safety of vandetanib, a dual VEGFR and EGFR inhibitor, in advanced non-small-cell lung cancer: a systematic review and meta-analysis.
Bai, C; He, J; Li, H; Qin, Y; Song, H; Wang, C; Wei, L; Wu, C; Wu, M; Xu, J; Zhang, X; Zhu, T, 2011
)
0.37
"Donepezil is a widely used cholinesterase inhibitor for the treatment of Alzheimer's disease (AD), however its cholinergic adverse side effects on the cardiovascular system are still unclear."( Cardiac safety of donepezil in elderly patients with Alzheimer disease.
Aydemir, E; Bozoglu, E; Isik, AT; Yay, A; Yildiz, GB, 2012
)
0.38
" The safety evaluation included adverse events, visual acuity, intra-ocular pressure and study drug drop sensation."( [Safety and efficacy of a new preservative-free levocabastine ophthalmic solution (Levofree®) using the conjunctival provocation test].
Allaire, C; Bassols, A; Siou-Mermet, R, 2012
)
0.38
" The incidence of adverse events was lower with the preservative-free solution than with the preserved suspension."( [Safety and efficacy of a new preservative-free levocabastine ophthalmic solution (Levofree®) using the conjunctival provocation test].
Allaire, C; Bassols, A; Siou-Mermet, R, 2012
)
0.38
" Rates of treatment-emergent adverse events (AEs) were higher for donepezil 23 mg/day with memantine (80."( Efficacy and safety of donepezil 23 mg versus donepezil 10 mg for moderate-to-severe Alzheimer's disease: a subgroup analysis in patients already taking or not taking concomitant memantine.
Doody, RS; Farlow, MR; Geldmacher, DS; Mackell, J; Moline, M; Sun, Y, 2012
)
0.38
" Donepezil 23 mg was generally safe and well tolerated among patients receiving donepezil alone and among patients receiving a combination of donepezil and memantine therapy."( Efficacy and safety of donepezil 23 mg versus donepezil 10 mg for moderate-to-severe Alzheimer's disease: a subgroup analysis in patients already taking or not taking concomitant memantine.
Doody, RS; Farlow, MR; Geldmacher, DS; Mackell, J; Moline, M; Sun, Y, 2012
)
0.38
" The primary endpoint during the long-term extension phase was adverse events."( Efficacy and safety of alogliptin added to metformin in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label, long-term extension study.
Hirayama, M; Hiroi, S; Kaku, K; Miyata, Y; Seino, Y, 2012
)
0.38
" Incidences of adverse effects were comparable between groups, with no increases in hypoglycaemia."( Efficacy and safety of alogliptin added to metformin in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label, long-term extension study.
Hirayama, M; Hiroi, S; Kaku, K; Miyata, Y; Seino, Y, 2012
)
0.38
"5 and 25 mg once daily was safe and effective when added to metformin (500 or 750 mg/day) in Japanese patients with inadequately controlled type 2 diabetes on metformin alone."( Efficacy and safety of alogliptin added to metformin in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label, long-term extension study.
Hirayama, M; Hiroi, S; Kaku, K; Miyata, Y; Seino, Y, 2012
)
0.38
" With respect to effects on embryofoetal development in rabbits, bilastine at 400 mg/kg/day (the highest dose evaluated) was assessed to be the no observed adverse effects level."( Preclinical toxicity profile of oral bilastine.
Arteche, JK; Casadesus, A; Lucero, ML; Sommer, EW, 2012
)
0.38
" Safety analyses comprised examination of the incidence, severity, and timing of treatment-emergent adverse events (AEs); changes in weight, electrocardiogram, vital signs, and laboratory parameters; and discontinuation due to AEs."( Long-term safety and tolerability of donepezil 23 mg in patients with moderate to severe Alzheimer's disease.
Mackell, J; Moline, M; Salloway, S; Tariot, P; Yardley, J, 2012
)
0.38
" However, donepezil appeared to be safe and well tolerated."( Effectiveness and safety of donepezil in boys with fragile x syndrome: a double-blind, randomized, controlled pilot study.
Arya, R; Chauhan, S; Chowdhury, MR; Dwivedi, SN; Gulati, S; Gupta, N; Gupta, YK; Kabra, M; Kalra, V; Sahu, JK; Sapra, S, 2013
)
0.39
" In this context, newer SGAs were developed to further improve the adverse effect burden of available agents."( Body weight and metabolic adverse effects of asenapine, iloperidone, lurasidone and paliperidone in the treatment of schizophrenia and bipolar disorder: a systematic review and exploratory meta-analysis.
Correll, CU; De Hert, M; Detraux, J; Sweers, K; van Winkel, R; Yu, W, 2012
)
0.38
" Adverse events were more common with donepezil but mostly mild/moderate in severity."( Donepezil in Parkinson's disease dementia: a randomized, double-blind efficacy and safety study.
Dubois, B; Emre, M; Gray, J; Hsu, T; Katzenschlager, R; Lees, AJ; Moline, ML; Pourcher, E; Schumann, G; Swartz, J; Thomas, G; Tolosa, E, 2012
)
0.38
" The most frequently reported adverse events (AEs) were infections and infestations: 22·4% (2 mg twice daily), 20·4% (5 mg twice daily), 36·7% (15 mg twice daily) and 32·0% (placebo)."( Efficacy and safety of tofacitinib, an oral Janus kinase inhibitor, in the treatment of psoriasis: a Phase 2b randomized placebo-controlled dose-ranging study.
Buonanno, M; Gupta, P; Harness, JA; Krishnaswami, S; Langley, RG; Menter, A; Papp, KA; Strober, B; Tan, H; Wolk, R, 2012
)
0.38
" The absorption of bilastine is fast, linear and dose-proportional; it appears to be safe and well tolerated at all doses levels in healthy population."( Safety profile of bilastine: 2nd generation H1-antihistamines.
Scaglione, F, 2012
)
0.38
" Treatment-emergent adverse events (TEAEs), most mild to moderate in severity, included headache (13."( Long-term safety and tolerability of iloperidone: results from a 25-week, open-label extension trial.
Cutler, AJ; Kalali, AH; Kunovac, J; Mattingly, GW; Meng, X, 2013
)
0.39
" Adverse event (AE) occurrence was similar across treatment groups."( A randomized phase 2a efficacy and safety trial of the topical Janus kinase inhibitor tofacitinib in the treatment of chronic plaque psoriasis.
Bissonnette, R; Bolduc, C; Khan, S; Lamba, M; Lan, S; Papp, K; Ports, WC, 2013
)
0.39
" Any adverse events (AEs) were recorded."( One-year safety and tolerability profile of pridopidine in patients with Huntington disease.
Bright, J; de Yebenes, JG; Ivkovic, J; Landwehrmeyer, B; Prang, A; Reilmann, R; Rembratt, A; Rosser, A; Squitieri, F, 2013
)
0.39
"This study provides Class IV evidence that pridopidine (≤90 mg/day) is generally safe and well-tolerated in patients with Huntington disease for up to 1 year."( One-year safety and tolerability profile of pridopidine in patients with Huntington disease.
Bright, J; de Yebenes, JG; Ivkovic, J; Landwehrmeyer, B; Prang, A; Reilmann, R; Rembratt, A; Rosser, A; Squitieri, F, 2013
)
0.39
" Serious adverse events (AEs) occurring in 20/37 patients included neutropenia (n = 5), diarrhea (n = 4), pulmonary embolism (n = 3), and simultaneous dehydration, acute renal failure, and febrile neutropenia (n = 2)."( A phase I trial to determine the safety, pharmacokinetics, and pharmacodynamics of intercalated BMS-690514 with paclitaxel/carboplatin (PC) in advanced or metastatic solid malignancies.
Adjei, AA; Belani, CP; Chow, LQ; Dy, GK; Fortin, C; Gupta, A; Jonker, DI; Laurie, SA; Nicholas, G; Park, JS; Patricia, D; Sbar, EI; Zhang, S, 2013
)
0.39
"We evaluated the incidence of CV events in patients treated with alogliptin, placebo or comparator antihyperglycaemic drugs in the clinical trial database for alogliptin using the composite major adverse cardiovascular event (MACE) endpoints of CV death, non-fatal myocardial infarction and non-fatal stroke."( Cardiovascular safety of the dipetidyl peptidase-4 inhibitor alogliptin in type 2 diabetes mellitus.
Fleck, P; Hisada, M; Menon, V; Munsaka, M; Pratley, R; White, WB; Wilson, C, 2013
)
0.39
" Our results suggest that GluN2B antagonists may represent valuable alternatives to unspecific NMDAR antagonists with robust antidepressant efficacy and a more favorable side-effect profile."( Pharmacological blockade of GluN2B-containing NMDA receptors induces antidepressant-like effects lacking psychotomimetic action and neurotoxicity in the perinatal and adult rodent brain.
Dormann, C; Gass, P; Inta, D; Köhr, G; Lima-Ojeda, JM; Pfeiffer, N; Sprengel, R; Vogt, MA, 2013
)
0.39
" In Aβ42-induced toxic conditions, each PP2A and GSK-3β activity measured at different times showed time-dependent reverse pattern toward the direction of accelerating neuronal deaths with the passage of time."( Neuroprotective effects of donepezil against Aβ42-induced neuronal toxicity are mediated through not only enhancing PP2A activity but also regulating GSK-3β and nAChRs activity.
Kim, SH; Kim, SM; Koh, SH; Ku, SK; Maurice, T; Noh, MY, 2013
)
0.39
" There was no significant imbalance in the incidence of adverse events (AEs) by onset time, and delayed AE onset induced by the long-term administration of donepezil was unlikely to appear."( Long-term safety and efficacy of donepezil in patients with dementia with Lewy bodies: results from a 52-week, open-label, multicenter extension study.
Hashimoto, M; Ikeda, M; Iseki, E; Kosaka, K; Matsukawa, N; Matsuo, K; Mori, E; Nakagawa, M, 2013
)
0.39
" Outcomes of interest include 20% and 50% improvement in the American College of Rheumatology Scale (ACR20 and ACR50) response rates, rates of infection, the number of immunological/haematological adverse events (AEs), deranged laboratory results (hepatic, renal, haematological tests and lipoprotein level) and the incidence of drug withdrawal."( Efficacy and safety of tofacitinib in the treatment of rheumatoid arthritis: a systematic review and meta-analysis.
Chan, EW; Chui, CS; He, Y; Lau, WC; Man, KK; Wong, AY; Wong, IC; Worsley, AJ, 2013
)
0.39
" Given the potential for long-term vandetanib therapy in this setting, in addition to treatment for disease-related symptoms, effective management of related adverse events (AEs) is vital to ensure patient compliance and maximize clinical benefit with vandetanib therapy."( Vandetanib in advanced medullary thyroid cancer: review of adverse event management strategies.
Capdevila, J; Filetti, S; Grande, E; Kreissl, MC; Newbold, K; Reinisch, W; Robert, C; Schlumberger, M; Tolstrup, LK; Zamorano, JL, 2013
)
0.39
" Presently only Memantine is considered a safe NMDAR antagonist and is used clinically."( Development of NMDAR antagonists with reduced neurotoxic side effects: a study on GK11.
Hirbec, H; Nesic, O; Perez-Polo, R; Prieto-Cappellini, M; Privat, A; Teigell, M; Ulmann, L; Vandame, D; Vignon, J, 2013
)
0.39
"As life expectancy increases, it is imperative that health care providers recognize the importance of safe medication use within an aging geriatric population."( Donepezil 23 mg: a brief insight on efficacy and safety concerns.
Nguyen, MD; Salbu, RL, 2013
)
0.39
" The drug was safe and well tolerated in healthy Chinese males."( The pharmacokinetic and safety profiles of blonanserin in healthy Chinese volunteers after single fasting doses and single and multiple postprandial doses.
Chen, R; Chen, X; Hu, P; Jiang, J; Liu, H; Wang, H; Zhong, W; Zhou, Y, 2014
)
0.4
" Overall incidence of adverse events was similar among treatment groups."( Efficacy and safety evaluation of HSD-1 inhibitor ABT-384 in Alzheimer's disease.
Greco, N; Katz, DA; Lenz, RA; Liu, W; Marek, GJ; Meier, A; Zhang, W, 2014
)
0.4
" The safety endpoints consisted of the incidence of hypoglycemia and other adverse events."( [The design and baseline characteristics of a phase III study to evaluate the efficacy and safety of alogliptin versus placebo in type 2 diabetes mellitus in Mainland China].
Bu, RF; Gu, W; Han, P; Ji, QH; Jiang, ZS; Lei, MX; Li, CJ; Li, L; Li, WH; Li, XF; Li, XJ; Li, ZF; Liu, JD; Liu, XM; Liu, Y; Liu, ZM; Lu, JM; Lü, XF; Pan, CY; Peng, YD; Qu, S; Shi, BY; Song, QH; Xu, XJ; Xue, YM; Yan, L; Yang, JK; Zeng, JE; Zheng, BZ, 2013
)
0.39
"To assess the effects of tofacitinib on T lymphocytes in RA patients with a special focus on efficacy and infectious adverse events (iAEs)."( Effects of tofacitinib on lymphocytes in rheumatoid arthritis: relation to efficacy and infectious adverse events.
Fukuyo, S; Hirata, S; Kubo, S; Maeshima, K; Saito, K; Sonomoto, K; Suzuki, K; Tanaka, Y; Yamaoka, K, 2014
)
0.4
" Alogliptin appears to be weight neutral and is relatively well tolerated with few adverse effects."( Alogliptin: safety, efficacy, and clinical implications.
Cole, SW; Marino, AB, 2015
)
0.42
"Alogliptin alone or in combination with other antidiabetic agents has shown a significant reduction in HbA1c while remaining safe and tolerable."( Alogliptin: safety, efficacy, and clinical implications.
Cole, SW; Marino, AB, 2015
)
0.42
" As a result, we proposed tetrahydroquinazoline-type derivative as a safe and effective antimalarial candidate."( Synthesis of febrifugine derivatives and development of an effective and safe tetrahydroquinazoline-type antimalarial.
Hariguchi, N; Horoiwa, S; Kasahara, R; Kikuchi, H; Matsumoto, M; Oshima, Y, 2014
)
0.4
" Compared with placebo, more dropouts and adverse events occurred with the cholinesterase inhibitors, but not with memantine."( Efficacy and safety of donepezil, galantamine, rivastigmine, and memantine for the treatment of Alzheimer's disease: a systematic review and meta-analysis.
Jiang, T; Meng, XF; Tan, CC; Tan, L; Tan, MS; Wang, C; Wang, HF; Yu, JT; Zhu, XC, 2014
)
0.4
" Treatment discontinuation due to adverse events was more common in Arm A compared to Arm B (42 vs."( A randomized phase II efficacy and safety study of vandetanib (ZD6474) in combination with bicalutamide versus bicalutamide alone in patients with chemotherapy naïve castration-resistant prostate cancer.
Azad, AA; Beardsley, EK; Chi, KN; Chin, J; Ellard, SL; Hotte, SJ; Klotz, L; Kollmannsberger, C; Mukherjee, SD, 2014
)
0.4
" Primary endpoints were adverse events (AE) and laboratory safety data."( Safety and efficacy of tofacitinib, an oral janus kinase inhibitor, for the treatment of rheumatoid arthritis in open-label, longterm extension studies.
Benda, B; Curtis, JR; Gruben, D; Komuro, Y; Lee, EB; Nakamura, H; Nduaka, CI; Riese, RJ; Silverfield, J; Soma, K; Wang, L; Wollenhaupt, J; Wood, SP; Zwillich, SH, 2014
)
0.4
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" The most common adverse events were grade 1/2 and included asthenia (N = 5), constipation (N = 4), diarrhoea (N = 3), back pain (N = 3) and cancer pain (N = 3)."( Safety, tolerability and anti-tumour activity of the androgen biosynthesis inhibitor ASP9521 in patients with metastatic castration-resistant prostate cancer: multi-centre phase I/II study.
Baron, B; Baskin-Bey, E; De Bono, JS; Fizazi, K; Heeringa, M; Holtkamp, GM; James, ND; Jones, RJ; Loriot, Y; Molife, RL; Omlin, A; Ouatas, T; Van den Brande, J, 2014
)
0.4
" Visual analogue scale (VAS), requirement of fentanyl and flurbiprofen, and the incidence of remifentanil-related adverse effects (respiratory depression, nausea, vomiting, pruritus) were examined at 3 hourly intervals for 12 hours."( [Efficacy and safety of remifentanil-based regimen for postoperative pain management in abdominal surgery patients: a double-blind study with low-dose remifentanil infusion of 0.02 microg x kg(-1) x min(-1)].
Hirano, H; Kaida, T; Machino, A; Nagasaka, Y; Shirasaki, R; Wakamatsu, M, 2014
)
0.4
" No adverse events including respiratory depression occurred throughout the study in both groups."( [Efficacy and safety of remifentanil-based regimen for postoperative pain management in abdominal surgery patients: a double-blind study with low-dose remifentanil infusion of 0.02 microg x kg(-1) x min(-1)].
Hirano, H; Kaida, T; Machino, A; Nagasaka, Y; Shirasaki, R; Wakamatsu, M, 2014
)
0.4
"02 microg x kg(-1) x min(-1) can safely be used without any serious adverse events, while it may not be enough for postoperative analgesia."( [Efficacy and safety of remifentanil-based regimen for postoperative pain management in abdominal surgery patients: a double-blind study with low-dose remifentanil infusion of 0.02 microg x kg(-1) x min(-1)].
Hirano, H; Kaida, T; Machino, A; Nagasaka, Y; Shirasaki, R; Wakamatsu, M, 2014
)
0.4
" Alectinib was well tolerated, with the most common adverse events being fatigue (14 [30%]; all grade 1-2), myalgia (eight [17%]; all grade 1-2), and peripheral oedema (seven [15%] grade 1-2, one [2%] grade 3)."( Safety and activity of alectinib against systemic disease and brain metastases in patients with crizotinib-resistant ALK-rearranged non-small-cell lung cancer (AF-002JG): results from the dose-finding portion of a phase 1/2 study.
Azada, MC; Boisserie, F; Chiappori, AA; Di Laurenzio, L; Gadgeel, SM; Gandhi, L; Garcia, L; Golding, S; Lee, RM; Morcos, PN; Ou, SH; Riely, GJ; Sato, J; Tanaka, T; West, HL; Yokoyama, S; Yu, L, 2014
)
0.4
" Incidences of adverse effects were comparable between groups, with no relevant increases in hypoglycemia or weight gain seen."( Efficacy and safety of alogliptin added to insulin in Japanese patients with type 2 diabetes: a randomized, double-blind, 12-week, placebo-controlled trial followed by an open-label, long-term extension phase.
Kaku, K; Kanoo, T; Katou, M; Mori, M; Seino, Y, 2014
)
0.4
" 25 patients (seven taking placebo and 18 taking idalopirdine) discontinued treatment because of adverse events, the difference between groups being mainly due to asymptomatic transient increases in transaminase concentrations in some idalopirdine-treated patients."( Safety and efficacy of idalopirdine, a 5-HT6 receptor antagonist, in patients with moderate Alzheimer's disease (LADDER): a randomised, double-blind, placebo-controlled phase 2 trial.
Colding-Jørgensen, E; Wilkinson, D; Windfeld, K, 2014
)
0.4
" Observed signs and symptoms such as tachycardia (112 bpm), hypertension (220/125 mmHg), echolalia, confusion, agitation, opisthotonus, nystagmus and amnesia were consistent with phencyclidine-induced adverse effects."( Acute toxicity associated with the recreational use of the novel dissociative psychoactive substance methoxphenidine.
Ceschi, A; Degrandi, C; Hofer, KE; Müller, DM; Rauber-Lüthy, C; Wahl, S; Zürrer-Härdi, U, 2014
)
0.4
" Common adverse events (AEs) were also studied."( Efficacy and safety of angiogenesis inhibitors in advanced non-small cell lung cancer: a systematic review and meta-analysis.
Chen, Y; Hong, S; Luo, S; Tan, M; Wang, S; Zhang, L, 2015
)
0.42
"BRAF inhibitor (BRAFi) and MEK inhibitor (MEKi) frequently cause cutaneous adverse events."( Comparative profile of cutaneous adverse events: BRAF/MEK inhibitor combination therapy versus BRAF monotherapy in melanoma.
Algazi, A; Chong, K; Choudhry, A; Daud, A; Johnston, K; Meier, M; Ortiz-Urda, S; Osella-Abate, S; Posch, C; Quaglino, P; Rappersberger, K; Sanlorenzo, M; Vujic, I, 2014
)
0.4
" Patient characteristics, and the occurrence and severity of cutaneous adverse events, are described."( Comparative profile of cutaneous adverse events: BRAF/MEK inhibitor combination therapy versus BRAF monotherapy in melanoma.
Algazi, A; Chong, K; Choudhry, A; Daud, A; Johnston, K; Meier, M; Ortiz-Urda, S; Osella-Abate, S; Posch, C; Quaglino, P; Rappersberger, K; Sanlorenzo, M; Vujic, I, 2014
)
0.4
"The development of cutaneous adverse events was significantly less frequent (P = ."( Comparative profile of cutaneous adverse events: BRAF/MEK inhibitor combination therapy versus BRAF monotherapy in melanoma.
Algazi, A; Chong, K; Choudhry, A; Daud, A; Johnston, K; Meier, M; Ortiz-Urda, S; Osella-Abate, S; Posch, C; Quaglino, P; Rappersberger, K; Sanlorenzo, M; Vujic, I, 2014
)
0.4
"Combination regimen with BRAFi and MEKi shows fewer cutaneous adverse events and longer cutaneous adverse event-free interval compared with BRAFi monotherapy."( Comparative profile of cutaneous adverse events: BRAF/MEK inhibitor combination therapy versus BRAF monotherapy in melanoma.
Algazi, A; Chong, K; Choudhry, A; Daud, A; Johnston, K; Meier, M; Ortiz-Urda, S; Osella-Abate, S; Posch, C; Quaglino, P; Rappersberger, K; Sanlorenzo, M; Vujic, I, 2014
)
0.4
"No serious adverse events were recorded following any dose in either the able-bodied group or the SCI group."( Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers.
Brown, DJ; Ellis, AG; Frauman, AG; Furness, JB; Millard, M; Zeglinski, PT, 2015
)
0.42
"Capromorelin at the doses tested was safe and well tolerated in both SCI and able-bodied participants and also showed similar pharmacokinetics with dose-dependent increases in concentration and drug exposure."( Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers.
Brown, DJ; Ellis, AG; Frauman, AG; Furness, JB; Millard, M; Zeglinski, PT, 2015
)
0.42
" However, few studies focused on the risk and adverse events (AEs) of combined targeted therapy."( Safety profile of combined therapy inhibiting EFGR and VEGF pathways in patients with advanced non-small-cell lung cancer: A meta-analysis of 15 phase II/III randomized trials.
Huang, J; Ji, LJ; Liu, H; Liu, Y; Ma, W; Qi, X; Xu, M; Zhu, Y, 2015
)
0.42
"The standards of care for Alzheimer's disease, acetylcholinesterase inhibitors such as donepezil (Aricept®), are dose-limited due to adverse side-effects."( Improved cognition without adverse effects: novel M1 muscarinic potentiator compares favorably to donepezil and xanomeline in rhesus monkey.
Cannon, CE; Dancho, M; Koser, A; Kuduk, SD; Puri, V; Renger, JJ; Uslaner, JM; Vardigan, JD; Wittmann, M, 2015
)
0.42
" Six tofacitinib patients experienced treatment-related serious adverse events (AEs)."( Efficacy and safety of tofacitinib as monotherapy in Japanese patients with active rheumatoid arthritis: a 12-week, randomized, phase 2 study.
Nakamura, H; Takeuchi, T; Tanaka, Y; Toyoizumi, S; Yamanaka, H; Zwillich, S, 2015
)
0.42
" Increased patient awareness about safe usage is important as well as more training with regards to traditional medicine."( Anti-staphylococcal, anti-HIV and cytotoxicity studies of four South African medicinal plants and isolation of bioactive compounds from Cassine transvaalensis (Burtt. Davy) codd.
Aiyegoro, OA; Mthethwa, NS; Obi, LC; Oyedeji, BA, 2014
)
0.4
" Predose and postdose safety assessments included orthostatic vital signs; 6-lead continuous telemetry monitoring (approximately 16 h predose to 24 h postdose); 12-lead electrocardiograms (ECGs); clinical chemistry, hematology, coagulation, and urinalysis; psychomotor functioning (using the Wayne Saccadic Fixator (WSF)); and adverse events."( A Double-Blind, Placebo-Controlled Trial to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of JDTic.
Buda, JJ; Carroll, FI; Kosten, TR; Swearingen, D; Walters, BB, 2015
)
0.42
" Mild to moderate adverse events were observed, with no evidence of exposure dependence up to 500 mg (fed)."( Safety, Tolerability and Pharmacokinetic and Pharmacodynamic Learnings from a Double-Blind, Randomized, Placebo-Controlled, Sequential Group First-in-Human Study of the TRPV1 Antagonist, JNJ-38893777, in Healthy Men.
De Meulder, M; Jun, C; Manitpisitkul, P; Mayorga, A; Moyer, JA; Romano, G; Shalayda, K, 2015
)
0.42
" In contrast, the safety based on the number of withdrawals due to adverse events did not differ significantly among the seven interventions."( Comparative efficacy and safety of tofacitinib, with or without methotrexate, in patients with active rheumatoid arthritis: a Bayesian network meta-analysis of randomized controlled trials.
Bae, SC; Lee, YH; Song, GG, 2015
)
0.42
" The most frequent adverse events (any grade) were diarrhea (70%), infusion-related reaction (45%), and peripheral sensory neuropathy (44%)."( Safety and activity of BTK inhibitor ibrutinib combined with ofatumumab in chronic lymphocytic leukemia: a phase 1b/2 study.
Andritsos, LA; Blum, KA; Byrd, JC; Flynn, JM; Grever, MR; Hall, N; Heerema, NA; Jaglowski, SM; James, DF; Johnson, AJ; Jones, JA; Lozanski, G; Maddocks, KJ; Munneke, B; Nagar, V; Neuenburg, JK; Ruppert, AS; Smucker, K; Stefanos, M; West, JS; Woyach, JA, 2015
)
0.42
"To establish the mortality risk and adverse events associated with the use of atypical antipsychotic medications in people with Parkinson disease psychosis (PDP) in a clinically defined trial cohort."( Impact of Current Antipsychotic Medications on Comparative Mortality and Adverse Events in People With Parkinson Disease Psychosis.
Ballard, C; Burn, DJ; Coate, B; Corbett, A; Isaacson, S; Mills, R; Pahwa, R; Rascol, O; Williams, H, 2015
)
0.42
"Safety assessments at 2 weeks; 1, 3, 6, 9, and 12 months; and every 6 months thereafter, including evaluation of adverse events (AEs), vital signs, weight, physical examinations, 12-lead electrocardiograms, clinical laboratory tests (serum chemistry, hematology, and urinalysis), and the Unified Parkinson's Disease Rating Scale Parts II and III (UPDRS-II+III, activities of daily living and motor impairment, respectively)."( Impact of Current Antipsychotic Medications on Comparative Mortality and Adverse Events in People With Parkinson Disease Psychosis.
Ballard, C; Burn, DJ; Coate, B; Corbett, A; Isaacson, S; Mills, R; Pahwa, R; Rascol, O; Williams, H, 2015
)
0.42
" Efficacy endpoints and incidence rates of adverse events (AEs) of special interest were assessed."( Efficacy and safety of tofacitinib following inadequate response to conventional synthetic or biological disease-modifying antirheumatic drugs.
Bananis, E; Burmester, G; Charles-Schoeman, C; Fleischmann, R; Hendrikx, T; Kwok, K; Nash, P; Soma, K; Zerbini, CA, 2016
)
0.43
" The overall incidence rates of treatment-emergent adverse events were similar among the treatment groups."( Efficacy and safety of pioglitazone added to alogliptin in Japanese patients with type 2 diabetes mellitus: a multicentre, randomized, double-blind, parallel-group, comparative study.
Igeta, M; Kaku, K; Katou, M; Ohira, T; Sano, H, 2015
)
0.42
" Discontinuation of ibrutinib is rarely due to adverse events related to the drug."( The clinical safety of ibrutinib in chronic lymphocytic leukemia.
Molica, S, 2015
)
0.42
"Ibrutinib is associated with bleeding-related adverse events of grade ≤ 2 in severity, and infrequently with grade ≥ 3 events."( Incidence and risk factors of bleeding-related adverse events in patients with chronic lymphocytic leukemia treated with ibrutinib.
Cullinane, AM; Farooqui, MZ; Herman, SE; Holland, SM; Lipsky, AH; Lozier, JN; Marti, G; Martyr, S; Nghiem, K; Niemann, CU; Saba, N; Soto, S; Sun, C; Tian, X; Uzel, G; Valdez, J; Wiestner, A, 2015
)
0.42
" For adverse events of special interest, data on tofacitinib 5 or 10 mg BID or placebo were pooled from six PII and five PIII randomised studies."( Efficacy and safety of tofacitinib in US and non-US rheumatoid arthritis patients: pooled analyses of phase II and III.
Cohen, SB; Fleischmann, R; Koenig, A; Kwok, K; Mebus, CA; Riese, R; Wang, L,
)
0.13
" Incidence rates for adverse events of special interest were similar between the US and ROW PII/PIII populations."( Efficacy and safety of tofacitinib in US and non-US rheumatoid arthritis patients: pooled analyses of phase II and III.
Cohen, SB; Fleischmann, R; Koenig, A; Kwok, K; Mebus, CA; Riese, R; Wang, L,
)
0.13
" The most common (≥ 20% patients) adverse events were neutropenia, anemia, nasopharyngitis, increased bilirubin, and rash."( Safety and tolerability of ibrutinib monotherapy in Japanese patients with relapsed/refractory B cell malignancies.
Aoki, T; Ishizawa, K; Morishita, T; Munakata, W; Ogura, M; Suzuki, T; Takahara, S; Tobinai, K; Uchida, T; Ushijima, Y, 2016
)
0.43
" In particular, adverse events (AEs) that have been of interest for the DPP-4 class of drugs, such as the risk of major cardiovascular (CV) events and acute pancreatitis, will be investigated in detail."( Alogliptin for the treatment of type 2 diabetes: a drug safety evaluation.
Seino, Y; Yabe, D, 2016
)
0.43
"This survey analyzes two national pharmacovigilance databases in order to determine the major adverse reactions observed with the use of cholinesterase inhibitors in dementia."( Adverse Effects of Cholinesterase Inhibitors in Dementia, According to the Pharmacovigilance Databases of the United-States and Canada.
Abagyan, R; Ali, TB; Chen, WY; Reilly, BM; Schleret, TR, 2015
)
0.42
"Both rapamycin (RAPA) and cyclosporin A (CsA) are commonly used for immunosuppression, however their adverse side effects limit their application."( Halofuginone Synergistically Enhances Anti-Proliferation of Rapamycin in T Cells and Reduces Cytotoxicity of Cyclosporine in Cultured Renal Tubular Epithelial Cells.
Chu, TL; Du, C; Guan, Q; Nguan, CY, 2015
)
0.42
" Withdrawals due to adverse events and number of patients experiencing nausea, vomiting, diarrhoea and dizziness were examined as safety profiles."( The comparative efficacy and safety of cholinesterase inhibitors in patients with mild-to-moderate Alzheimer's disease: a Bayesian network meta-analysis.
Kobayashi, H; Nakagawa, R; Ohnishi, T; Yoshizawa, K, 2016
)
0.43
" In contrast, the safety based on the number of withdrawals due to adverse events did not differ significantly among the treatment options."( Comparative efficacy and safety of tocilizumab, rituximab, abatacept and tofacitinib in patients with active rheumatoid arthritis that inadequately responds to tumor necrosis factor inhibitors: a Bayesian network meta-analysis of randomized controlled tri
Bae, SC; Lee, YH, 2016
)
0.43
"Tocilizumab 8 mg was the second-line non-TNF biologic with the highest performance regarding an early good response based on ACR20 response rate and acceptable safety profile, followed by rituximab, abatacept and tofacitinib in patients with RA and an inadequate response to anti-TNF therapy, and none of these treatments were associated with a significant risk of withdrawal due to adverse events."( Comparative efficacy and safety of tocilizumab, rituximab, abatacept and tofacitinib in patients with active rheumatoid arthritis that inadequately responds to tumor necrosis factor inhibitors: a Bayesian network meta-analysis of randomized controlled tri
Bae, SC; Lee, YH, 2016
)
0.43
" The percentage of subjects who experienced all adverse events including hypoglycemia with alogliptin were comparable to those with placebo."( [Efficacy and safety of alogliptin in treatment of type 2 diabetes mellitus: a multicenter, randomized, double-blind, placebo-controlled phase III clinical trial in mainland China].
Bu, R; Gu, W; Han, P; Ji, Q; Jiang, Z; Lei, M; Li, C; Li, L; Li, W; Li, X; Li, Z; Liu, J; Liu, X; Liu, Y; Liu, Z; Lu, J; Lyu, X; Pan, C; Peng, Y; Qu, S; Shi, B; Song, Q; Xu, X; Xue, Y; Yan, L; Yang, J; Zeng, J; Zheng, B, 2015
)
0.42
" We report a serious side effect of ibrutinib potentially attributable to interaction with the moderate CYP3A4 inhibitor verapamil."( Adverse event potentially due to an interaction between ibrutinib and verapamil: a case report.
Bilbault, P; Gourieux, B; Lambert Kuhn, E; Levêque, D; Lioure, B, 2016
)
0.43
"This is the first description of a serious side effect of ibrutinib likely due to an interaction with the CYP3A4 inhibitor verapamil."( Adverse event potentially due to an interaction between ibrutinib and verapamil: a case report.
Bilbault, P; Gourieux, B; Lambert Kuhn, E; Levêque, D; Lioure, B, 2016
)
0.43
" Adverse events occurred in 83% of patients through Week 52, including four (4."( Oral tofacitinib efficacy, safety and tolerability in Japanese patients with moderate to severe plaque psoriasis and psoriatic arthritis: A randomized, double-blind, phase 3 study.
Asahina, A; Etoh, T; Igarashi, A; Imafuku, S; Nagaoka, M; Ohtsuki, M; Saeki, H; Shibasaki, Y; Tomochika, Y; Toyoizumi, S, 2016
)
0.43
" Serious adverse events and discontinuations because of adverse events were reported in less than 11% of patients over 33 months of tofacitinib exposure."( Tofacitinib, an oral Janus kinase inhibitor, for the treatment of chronic plaque psoriasis: Long-term efficacy and safety results from 2 randomized phase-III studies and 1 open-label long-term extension study.
Feldman, SR; Gardner, A; Gupta, P; Krueger, JG; Langley, RG; Luo, Y; Mallbris, L; Mebus, C; Papp, KA; Tan, H; Tatulych, S; Thaci, D; Torii, H; Tyring, S; Wolk, R, 2016
)
0.43
" Safety evaluations included treatment-emergent adverse events (TEAEs), laboratory tests, cardiac safety (ECG recordings) and somnolence/sedation using the Pediatric Sleep Questionnaire (PSQ)."( Safety and tolerability of bilastine 10 mg administered for 12 weeks in children with allergic diseases.
Kiss, I; Kuna, P; Novák, Z; Tortajada-Girbés, M; Valiente, R; Yáñez, A, 2016
)
0.43
"The analysis of adverse events plays an important role in the benefit assessment of drugs."( Biometrical issues in the analysis of adverse events within the benefit assessment of drugs.
Beckmann, L; Bender, R; Lange, S, 2016
)
0.43
" ABT-126 was generally well tolerated; the most common adverse events were agitation, constipation, diarrhea, fall, and headache."( Efficacy and Safety of ABT-126 in Subjects with Mild-to-Moderate Alzheimer's Disease on Stable Doses of Acetylcholinesterase Inhibitors: A Randomized, Double-Blind, Placebo-Controlled Study.
Florian, H; Gault, LM; Gauthier, S; Lin, Y; Lipschitz, S; Meier, A; Othman, AA; Robieson, WZ; Tang, Q, 2016
)
0.43
" Common adverse events in the SR 23 mg group were decreased appetite, vomiting, diarrhea, and contusion."( Efficacy and Safety of Sustained Release Donepezil High Dose versus Immediate Release Donepezil Standard Dose in Japanese Patients with Severe Alzheimer's Disease: A Randomized, Double-Blind Trial.
Atarashi, H; Homma, A; Kubota, N; Nakai, K; Takase, T, 2016
)
0.43
" The rate of adverse events was 86."( Clinical study of repaglinide efficacy and safety in type 2 diabetes mellitus patients with blood glucose levels inadequately controlled by sitagliptin.
Hanafusa, T; Hotta, N; Ioriya, K; Kageyama, S; Kaku, K; Kawamori, R, 2016
)
0.43
" We here document the possible mechanism of tofacitinib in patiens with RA, shedding light upon a characteristic adverse event, herpes zoster."( Relevance of involvement of tofacitinib in T cell subsets to clinical courses and adverse events in patients with rheumatoid arthritis.
Sonomoto, K; Tanaka, Y, 2015
)
0.42
" Forty-nine treatment-emergent all-causality adverse events (AEs) were observed; nausea and headache were the most frequently reported."( Safety, tolerability, and pharmacokinetics of single oral doses of tofacitinib, a Janus kinase inhibitor, in healthy volunteers.
Boy, M; Chan, G; Chow, V; Krishnaswami, S, 2015
)
0.42
" All treatments were well tolerated, and adverse event incidence was similar across the treatment groups."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.43
" A similar percentage of patients experienced drug-related, treatment-emergent adverse events in the alogliptin and placebo arms."( Efficacy and safety of alogliptin in patients with type 2 diabetes mellitus: A multicentre randomized double-blind placebo-controlled Phase 3 study in mainland China, Taiwan, and Hong Kong.
Chan, J; Han, P; Hsieh, AT; Ji, Q; Li, C; Li, W; Lu, J; Pan, C; Yang, J; Zeng, J, 2017
)
0.46
" Incidence rates (IRs; patients with event/100 patient-years) of adverse events (AEs) of special interest were reported."( Tofacitinib, an oral Janus kinase inhibitor, for the treatment of Latin American patients with rheumatoid arthritis: Pooled efficacy and safety analyses of Phase 3 and long-term extension studies.
Cardiel, MH; Citera, G; García, EG; Goecke, A; Jaller, JJ; Kwok, K; Lomonte, ABV; Miranda, P; Radominski, SC; Rojo, R; Velez, P; Xibillé, D,
)
0.13
" Therefore, CV adverse events (AEs), and blood pressure and lipid level changes, in tofacitinib-treated patients with RA were evaluated."( Cardiovascular safety findings in patients with rheumatoid arthritis treated with tofacitinib, an oral Janus kinase inhibitor.
Boy, M; Charles-Schoeman, C; Geier, J; Gonzalez-Gay, MA; Kwok, K; Riese, R; Soma, K; Wicker, P; Zuckerman, A, 2016
)
0.43
" CV events, including major adverse CV events (MACE: CV death and non-fatal CV events) and congestive heart failure (CHF), were assessed by a blinded adjudication committee."( Cardiovascular safety findings in patients with rheumatoid arthritis treated with tofacitinib, an oral Janus kinase inhibitor.
Boy, M; Charles-Schoeman, C; Geier, J; Gonzalez-Gay, MA; Kwok, K; Riese, R; Soma, K; Wicker, P; Zuckerman, A, 2016
)
0.43
" To characterise the relative safety profile of tofacitinib to biologic disease-modifying antirheumatic drugs (bDMARDs), the accrued patient-years (pt-yrs) of exposure needed in an RA clinical trial programme to detect a potential increase in risk of specific adverse events (AEs) was determined."( Use of a risk characterisation approach to contextualise the safety profile of new rheumatoid arthritis treatments: a case study using tofacitinib.
Anisfeld, A; Chen, C; Chen, Y; Curtis, JR; Geier, J; Krishnaswami, S; Strengholt, S; Zhang, R, 2017
)
0.46
" Adverse events (AEs) were reported by 17."( Long-term safety and efficacy of bilastine following up to 12 weeks or 52 weeks of treatment in Japanese patients with allergic rhinitis: Results of an open-label trial.
Gotoh, M; Ohashi, Y; Okubo, K; Saito, A; Togawa, M, 2017
)
0.46
" Monitoring by means of the bispectral index (BIS) has shown its utility in reducing the use of drugs and their adverse events in general anesthesia, but evidence in prolonged sedation is insufficient."( Bispectral Index Monitoring Reduces the Dosage of Propofol and Adverse Events in Sedation for Endobronchial Ultrasound.
Bello, S; Chacón, E; De Pablo, F; Júdez, D; Martínez Ubieto, J; Mincholé, E; Pascual, A; Quesada, N, 2016
)
0.43
"A randomized cohort study of 90 patients with mediastinal lymph node involvement and/or lung or mediastinal lesions for whom EBUS was indicated, comparing the modified observer's assessment of alertness/sedation scale clinical evaluation (n = 45) versus the BIS evaluation (n = 45) of sedation with propofol-remifentanil, was conducted in order to evaluate the clinical parameters, doses used, adverse events, and tolerance of the procedure."( Bispectral Index Monitoring Reduces the Dosage of Propofol and Adverse Events in Sedation for Endobronchial Ultrasound.
Bello, S; Chacón, E; De Pablo, F; Júdez, D; Martínez Ubieto, J; Mincholé, E; Pascual, A; Quesada, N, 2016
)
0.43
" Significantly fewer overall adverse events were recorded in the BIS group and included desaturation, hypotension, and bradypnea."( Bispectral Index Monitoring Reduces the Dosage of Propofol and Adverse Events in Sedation for Endobronchial Ultrasound.
Bello, S; Chacón, E; De Pablo, F; Júdez, D; Martínez Ubieto, J; Mincholé, E; Pascual, A; Quesada, N, 2016
)
0.43
"BIS monitoring of sedation in EBUS makes it possible to reduce the dosage of propofol, thereby shortening the waking time and reducing adverse events."( Bispectral Index Monitoring Reduces the Dosage of Propofol and Adverse Events in Sedation for Endobronchial Ultrasound.
Bello, S; Chacón, E; De Pablo, F; Júdez, D; Martínez Ubieto, J; Mincholé, E; Pascual, A; Quesada, N, 2016
)
0.43
" The bilastine treatments were safe and well tolerated."( Efficacy and safety of bilastine in Japanese patients with chronic spontaneous urticaria: A multicenter, randomized, double-blind, placebo-controlled, parallel-group phase II/III study.
Furue, M; Hide, M; Saito, A; Togawa, M; Yagami, A, 2017
)
0.46
" A total of 8/16 patients (50%) had at least one grade 3 adverse event (AE), and 5 (31."( Efficacy and safety of ibrutinib in Japanese patients with relapsed or refractory mantle cell lymphoma.
Choi, I; Fukuhara, N; Hatake, K; Ishikawa, T; Kinoshita, T; Kitano, T; Maruyama, D; Matsuno, Y; Nagai, H; Nishikawa, T; Nishikori, M; Shibayama, H; Takahara, S; Tobinai, K; Uchida, T, 2016
)
0.43
" The most common adverse events in vandetanib-treated patients are: diarrhea, rash, folliculitis, nausea, QTc prolongation, hypertension and fatigue."( The safety and efficacy of vandetanib in the treatment of progressive medullary thyroid cancer.
Antonelli, A; Baldini, E; Biricotti, M; Fallahi, P; Ferrari, SM; Materazzi, G; Miccoli, P; Ulisse, S, 2016
)
0.43
" Adverse events were limited to mild emesis and loose stools in all groups and excess salivation among some dogs receiving higher capromorelin doses."( Evaluation of the safety in dogs of long-term, daily oral administration of capromorelin, a novel drug for stimulation of appetite.
Armintrout, G; Huebner, M; Rausch-Derra, LC; Rhodes, L; Zollers, B, 2017
)
0.46
" Adverse events were limited to grade I and II infections."( Safety and efficacy of the JAK inhibitor tofacitinib citrate in patients with alopecia areata.
Cerise, JE; Chen, JC; Christiano, AM; Craiglow, BG; Jabbari, A; Kennedy Crispin, M; King, BA; Ko, JM; Li, S; Marinkovich, MP; Oro, AE; Shankar, G; Urban, JR; Winge, MC, 2016
)
0.43
"At the dose and duration studied, tofacitinib is a safe and effective treatment for severe AA, though it does not result in a durable response."( Safety and efficacy of the JAK inhibitor tofacitinib citrate in patients with alopecia areata.
Cerise, JE; Chen, JC; Christiano, AM; Craiglow, BG; Jabbari, A; Kennedy Crispin, M; King, BA; Ko, JM; Li, S; Marinkovich, MP; Oro, AE; Shankar, G; Urban, JR; Winge, MC, 2016
)
0.43
" All patients experienced at least one adverse event (AE), and 7 patients (50%) experienced grade ≥3 AEs."( SAFETY AND TOLERABILITY OF VANDETANIB IN JAPANESE PATIENTS WITH MEDULLARY THYROID CANCER: A PHASE I/II OPEN-LABEL STUDY.
Horiuchi, K; Ito, Y; Komoda, M; Okamoto, T; Rito, K; Takahashi, S; Todo, T; Tomomatsu, J; Tsuji, A; Uchino, K, 2017
)
0.46
" The overall frequency of adverse events was similar among the groups."( Randomized, double-blind, phase III study to evaluate the efficacy and safety of once-daily treatment with alogliptin and metformin hydrochloride in Japanese patients with type 2 diabetes.
Kaku, K; Katou, M; Kinugawa, Y; Nishiyama, Y; Sumino, S, 2017
)
0.46
" Safety was consistent with prior experience for each drug, with infusion reactions the most prevalent adverse event."( Ublituximab (TG-1101), a novel glycoengineered anti-CD20 antibody, in combination with ibrutinib is safe and highly active in patients with relapsed and/or refractory chronic lymphocytic leukaemia: results of a phase 2 trial.
Brooks, HD; Burke, JM; Fanning, S; Farber, CM; Greenwald, DR; Klein, L; Kolibaba, KS; Mahadevan, D; Miskin, HP; Schreeder, MT; Sharman, JP; Sportelli, P; Weiss, MS, 2017
)
0.46
"To determine possible differences in serious adverse effects among the 10 currently approved biological and targeted synthetic DMARDs (b/ts-DMARDs) for RA."( Risk of serious adverse effects of biological and targeted drugs in patients with rheumatoid arthritis: a systematic review meta-analysis.
Bliddal, H; Boers, M; Brock, B; Christensen, R; Dossing, A; Eric Furst, D; Heller Asmussen, K; Luta, G; Schjødt Jørgensen, T; Tarp, S; Tarp, U; Thirstrup, S, 2017
)
0.46
" Network meta-analyses using mixed-effects Poisson regression models were conducted to calculate rate ratios for serious adverse events (SAEs) and deaths between each of the 10 drugs and control (i."( Risk of serious adverse effects of biological and targeted drugs in patients with rheumatoid arthritis: a systematic review meta-analysis.
Bliddal, H; Boers, M; Brock, B; Christensen, R; Dossing, A; Eric Furst, D; Heller Asmussen, K; Luta, G; Schjødt Jørgensen, T; Tarp, S; Tarp, U; Thirstrup, S, 2017
)
0.46
" In a well-matched series of 540 patients undergoing transsphenoidal surgery, remifentanil was found to be a safe anesthetic adjunct."( Safety of remifentanil in transsphenoidal surgery: A single-center analysis of 540 patients.
Aglio, LS; Burke, WT; Castlen, JP; Cote, DJ; King, CH; Laws, ER; Smith, TR; Zaidi, HA, 2017
)
0.46
" Incidence rates (IRs; patients with event/100 patient-years) and 95% CIs are reported for adverse events (AEs) of interest."( Long-term safety of tofacitinib for the treatment of rheumatoid arthritis up to 8.5 years: integrated analysis of data from the global clinical trials.
Charles-Schoeman, C; Cohen, SB; Curtis, JR; DeMasi, R; Geier, J; Kwok, K; Lee, EB; Mariette, X; Nash, P; Riese, R; Tanaka, Y; Thirunavukkarasu, K; Wang, L; Winthrop, KL; Wollenhaupt, J, 2017
)
0.46
" IRs for discontinuation due to adverse events, serious infections, tuberculosis, all herpes zoster (HZ), serious HZ, malignancies (excluding non-melanoma skin cancer) and major adverse cardiovascular events were numerically lower for LA versus RoW patients; IR for mortality was numerically higher."( Safety of Tofacitinib in the Treatment of Rheumatoid Arthritis in Latin America Compared With the Rest of the World Population.
Alvarez-Moreno, C; Cardiel, MH; Castañeda, OM; Castelli, G; Citera, G; García, EG; Jaller, JJ; Kwok, K; Mysler, E; Ponce de Leon, D; Radominski, SC; Rillo, O; Rojo, R; Romero, FJ; Salinas, A, 2017
)
0.46
" Twenty-nine patients with serious adverse events (SAEs) were reported in donepezil (n = 11) and placebo groups (n = 18) (p = 0."( Efficacy and Safety of Donepezil in Chinese Patients with Severe Alzheimer's Disease: A Randomized Controlled Trial.
Doody, RS; Jia, J; Jia, L; Li, F; Liang, J; Shi, L; Tang, Y; Wei, C; Zhou, A, 2017
)
0.46
" The incidences of adverse events (AEs) were 29."( Efficacy and safety of metformin and sitagliptin based triple antihyperglycemic therapy (STRATEGY): a multicenter, randomized, controlled, non-inferiority clinical trial.
Bi, Y; Engel, SS; Ji, L; Ji, Q; Jia, W; Lu, J; Mao, A; Mu, Y; Ran, X; Weng, J; Xu, W; Yang, W; Yao, B; Zeng, L; Zhao, B; Zhao, J; Zhou, Z; Zhu, D, 2017
)
0.46
" Specifically, we cover cardiovascular, gastrointestinal, hepatic, musculoskeletal, and respiratory adverse events."( Safety of alectinib for the treatment of metastatic ALK-rearranged non-small cell lung cancer.
Ou, SH; Zhu, V, 2017
)
0.46
" Anesthesia onset time, total number of intraoperative children movements, hemodynamics (heart rate, arterial pressure, pulse oxygen saturation (SpO2), respiratory rate), total cumulative dose of dexmedetomidine and remifentanil, the amount of midazolam and lidocaine, time to first dose of rescue midazolam and lidocaine, postoperative recovery time, adverse events, bronchoscopist satisfaction score were recorded."( The safety and efficacy of dexmedetomidine-remifentanil in children undergoing flexible bronchoscopy: A retrospective dose-finding trial.
Jin, S; Li, X; Li, Y; Wang, X; Zhang, D, 2017
)
0.46
" Information on individual adverse events, reported by phone by the village distributors, was obtained through home visits."( Safety of a topical insect repellent (picaridin) during community mass use for malaria control in rural Cambodia.
Coosemans, M; Durnez, L; Heng, S; Mean, V; Polo, K; Sluydts, V; Tho, S; van Griensven, J, 2017
)
0.46
"Of the 41 adverse events notified by phone by the village distributors, there were 22 adverse reactions, 11 cases of repellent abuse (6 accidental, 5 suicide attempts) and 8 non-related events."( Safety of a topical insect repellent (picaridin) during community mass use for malaria control in rural Cambodia.
Coosemans, M; Durnez, L; Heng, S; Mean, V; Polo, K; Sluydts, V; Tho, S; van Griensven, J, 2017
)
0.46
" With remarkable efficacy, good oral bioavailability, and modest adverse events profile, ibrutinib use is likely to continue to increase."( Ibrutinib in CLL: a focus on adverse events, resistance, and novel approaches beyond ibrutinib.
Kaur, V; Swami, A, 2017
)
0.46
" These toxic effects were attenuated by CB1R knockout or CB1R antagonists."( Genetic or pharmacological depletion of cannabinoid CB1 receptor protects against dopaminergic neurotoxicity induced by methamphetamine in mice.
Dang, DK; Jang, CG; Jeong, JH; Kim, HC; Ledent, C; Mai, AT; Nabeshima, T; Nah, SY; Onaivi, ES; Shin, EJ; Yamamoto, T, 2017
)
0.46
" Clinical disease activity indicated by disease activity score (DAS)28-ESR, the simplified disease activity index, and the clinical disease activity index as well as adverse events (AEs) were evaluated."( Efficacy and safety at 24 weeks of daily clinical use of tofacitinib in patients with rheumatoid arthritis.
Aramaki, T; Eguchi, K; Fukui, S; Hirai, Y; Horai, Y; Ichinose, K; Iwamoto, N; Kawakami, A; Kawashiri, SY; Koga, T; Nakamura, H; Nishino, A; Origuchi, T; Shimizu, T; Takatani, A; Tamai, M; Terada, K; Tsuji, S; Ueki, Y; Umeda, M, 2017
)
0.46
" Safety, including incidence rates (IRs; patients with events/100 patient-years) for adverse events (AEs) of special interest, was assessed throughout the studies."( Tofacitinib, an oral Janus kinase inhibitor, in patients from Mexico with rheumatoid arthritis: Pooled efficacy and safety analyses from Phase 3 and LTE studies.
Abud-Mendoza, C; Burgos-Vargas, R; Cardiel, M; Fan, H; García, E; Mahgoub, E; Pacheco-Tena, C; Pascual-Ramos, V; Rahman, M; Rojo, R; Santana, K; Xibillé, D,
)
0.13
" Based on a previous clinical trial, body weight of less than 55 kg is a risk factor for adverse events with donepezil 23 mg/d treatment in global population."( Adverse Events With Sustained-Release Donepezil in Alzheimer Disease: Relation to Body Mass Index.
Bae, JN; Carroll, BJ; Han, C; Jung, YE; Kang, HS; Kim, BJ; Kim, BS; Kim, DK; Kim, JL; Kim, KW; Kim, SG; Kim, SY; Kim, YH; Lee, C; Lee, DW; Lee, JY; Lee, K; Lee, SY; Lee, YM; Moon, SW; Myung, W; Ryu, SH; Shin, IS; Yu, H, 2017
)
0.46
" After screening, we analyzed a final cohort of 166 patients who received donepezil 23 mg/d for 24 weeks to compare the occurrence of treatment-emergent adverse events (TEAEs) between patients with high versus low body mass index (BMI) based on the World Health Organization overweight criteria for Asian populations (23 kg/m)."( Adverse Events With Sustained-Release Donepezil in Alzheimer Disease: Relation to Body Mass Index.
Bae, JN; Carroll, BJ; Han, C; Jung, YE; Kang, HS; Kim, BJ; Kim, BS; Kim, DK; Kim, JL; Kim, KW; Kim, SG; Kim, SY; Kim, YH; Lee, C; Lee, DW; Lee, JY; Lee, K; Lee, SY; Lee, YM; Moon, SW; Myung, W; Ryu, SH; Shin, IS; Yu, H, 2017
)
0.46
"Treatment-emergent adverse events were reported by 79."( Adverse Events With Sustained-Release Donepezil in Alzheimer Disease: Relation to Body Mass Index.
Bae, JN; Carroll, BJ; Han, C; Jung, YE; Kang, HS; Kim, BJ; Kim, BS; Kim, DK; Kim, JL; Kim, KW; Kim, SG; Kim, SY; Kim, YH; Lee, C; Lee, DW; Lee, JY; Lee, K; Lee, SY; Lee, YM; Moon, SW; Myung, W; Ryu, SH; Shin, IS; Yu, H, 2017
)
0.46
" Severe adverse events (AEs) (grade ≥ 3) based on the ALK-TKI type were analysed."( Pooled safety analyses of ALK-TKI inhibitor in ALK-positive NSCLC.
Chen, CL; Hu, H; Tang, Y; Weng, DS; Xia, JC; Zhang, XF; Zhou, ZQ; Zhu, Q, 2017
)
0.46
"ALK-TKIs were safe for ALK-positive patients."( Pooled safety analyses of ALK-TKI inhibitor in ALK-positive NSCLC.
Chen, CL; Hu, H; Tang, Y; Weng, DS; Xia, JC; Zhang, XF; Zhou, ZQ; Zhu, Q, 2017
)
0.46
" In total, 23 (6%) of 384 patients receiving tofacitinib monotherapy, 26 (7%) of 376 patients receiving tofacitinib plus methotrexate, and 36 (9%) of 386 patients receiving adalimumab plus methotrexate discontinued due to adverse events."( Efficacy and safety of tofacitinib monotherapy, tofacitinib with methotrexate, and adalimumab with methotrexate in patients with rheumatoid arthritis (ORAL Strategy): a phase 3b/4, double-blind, head-to-head, randomised controlled trial.
DeMasi, R; Fleischmann, R; Hall, S; Kivitz, AJ; Krishnaswami, S; Luo, Z; Menon, S; Mojcik, C; Moots, RJ; Mysler, E; Smolen, JS; Soma, K; Takiya, L; Tatulych, S; Zhang, R, 2017
)
0.46
" The spleen cells appear more susceptible to the adverse effects of DLM than thymus cells."( Mechanism of deltamethrin induced thymic and splenic toxicity in mice and its protection by piperine and curcumin: in vivo study.
Kumar, A; Sasmal, D; Sharma, N, 2018
)
0.48
" It is also essential to carefully monitor patients using TKI regarding possible adverse effects, which should be properly managed when occurring."( Medullary thyroid carcinoma - Adverse events during systemic treatment: risk-benefit ratio.
Maciel, LMZ; Magalhães, PKR,
)
0.13
" Acetylcholinesterase inhibitors (AChEIs) aim to provide symptomatic benefit for cognitive decline, however these drugs are not without adverse events (AEs)."( Acetylcholinesterase inhibitors for treating dementia symptoms - a safety evaluation.
Bradley, J; Chan, P; Herrmann, N; Lanctôt, K; Mohammad, D, 2017
)
0.46
" Adverse events (AEs) including cytokine release syndrome AEs (CytoRS-AEs) and nasal symptoms were assessed."( Safety and pharmacodynamics of intranasal GSK2245035, a TLR7 agonist for allergic rhinitis: A randomized trial.
Ellis, AK; Lee, LA; Powley, W; Quint, D; Tsitoura, DC, 2017
)
0.46
" Grade 3 or higher adverse events (AEs) occurred in 40% of patients, 6% of patients had treatment withdrawn on account of AEs, and 33% had AEs leading to dose interruptions/modification."( Pooled Systemic Efficacy and Safety Data from the Pivotal Phase II Studies (NP28673 and NP28761) of Alectinib in ALK-positive Non-Small Cell Lung Cancer.
Ahn, JS; Balas, B; Barlesi, F; Bordogna, W; Crino, L; Dansin, E; De Petris, L; Dingemans, AC; Gadgeel, S; Gandhi, L; Golding, S; Govindan, R; Kim, DW; Lena, H; Morcos, PN; Ou, SI; Popat, S; Shaw, AT; Yang, JC; Zeaiter, A, 2017
)
0.46
" Lasmiditan penetrates the blood-brain barrier and CNS associated adverse events are common, but mostly in mild to moderate severity."( The safety and efficacy of the 5-HT 1F receptor agonist lasmiditan in the acute treatment of migraine.
Israel, H; Neeb, L; Raffaelli, B; Reuter, U, 2017
)
0.46
" Adverse events (AEs), laboratory values, and electrocardiography were monitored throughout."( Safety and Exploratory Efficacy at 36 Months in Open-HART, an Open-Label Extension Study of Pridopidine in Huntington's Disease.
Abler, V; Auinger, P; Gandhi, S; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Papapetropoulos, S, 2017
)
0.46
"Pridopidine 45 mg BID was generally safe and tolerable in HD subjects over 36 months."( Safety and Exploratory Efficacy at 36 Months in Open-HART, an Open-Label Extension Study of Pridopidine in Huntington's Disease.
Abler, V; Auinger, P; Gandhi, S; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Papapetropoulos, S, 2017
)
0.46
" Serious adverse events occurred in 3 patients in the tofacitinib group (5."( The Safety and Immunogenicity of Live Zoster Vaccination in Patients With Rheumatoid Arthritis Before Starting Tofacitinib: A Randomized Phase II Trial.
Biswas, P; Choy, EH; Hodge, JA; Mojcik, CF; Nduaka, CI; Needle, E; Passador, S; Rigby, WF; Soma, K; Winthrop, KL; Wouters, AG, 2017
)
0.46
" Vaccination appeared to be safe in all of the patients except 1 patient who lacked preexisting VZV immunity."( The Safety and Immunogenicity of Live Zoster Vaccination in Patients With Rheumatoid Arthritis Before Starting Tofacitinib: A Randomized Phase II Trial.
Biswas, P; Choy, EH; Hodge, JA; Mojcik, CF; Nduaka, CI; Needle, E; Passador, S; Rigby, WF; Soma, K; Winthrop, KL; Wouters, AG, 2017
)
0.46
" Common adverse events were falls (21 [23%] of 90 participants in the pimavanserin group vs 21 [23%] of 91 in the placebo group), urinary tract infections (20 [22%] vs 25 [28%]), and agitation (19 [21%] vs 13 [14%])."( Evaluation of the safety, tolerability, and efficacy of pimavanserin versus placebo in patients with Alzheimer's disease psychosis: a phase 2, randomised, placebo-controlled, double-blind study.
Ballard, C; Banister, C; Coate, B; Cummings, J; Demos, G; Khan, Z; Owen, R; Stankovic, S; Youakim, JM, 2018
)
0.48
"Bilastine had a good safety profile and was well tolerated in terms of adverse events, laboratory parameters and vital signs."( Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients.
Biffi, A; Demonte, A; Fainello, M; Fernando, F; Guanti, MB; Liberati, S; Pepe, P, 2018
)
0.48
" The safety profile of bilastine in clinical trials of allergic rhinoconjunctivitis or urticaria, assessed by type and frequency of adverse events (AE), was similar to that of placebo."( Open-label safety assessment of bilastine in elderly patients with allergic rhinoconjunctivitis and/or urticaria.
Cordón, E; Del Mar Forés, M; Fernández, S; Labeaga, L; Riesgo, SE; Ruiz-Miján, M; Senán, MR; Sologuren, A; Viñas, R, 2018
)
0.48
"Vandetanib, a multi-kinase inhibitor used for the treatment of various cancers, has been reported to induce several adverse cardiac effects."( Electrophysiological mechanisms of vandetanib-induced cardiotoxicity: Comparison of action potentials in rabbit Purkinje fibers and pluripotent stem cell-derived cardiomyocytes.
Byun, B; Chae, JH; Hyun, SA; Kim, KS; Lee, HA, 2018
)
0.48
" As such, we assessed disproportionate reporting of major adverse cardiac events (MACE) among reports for DPP-4i submitted to the FDA Adverse Event Reporting System (FAERS) from 2006 to 2015."( Cardiovascular safety signals with dipeptidyl peptidase-4 inhibitors: A disproportionality analysis among high-risk patients.
Alexander, GC; Baksh, SN; McAdams-DeMarco, M; Segal, JB, 2018
)
0.48
"3 million adverse event reports, 13."( Cardiovascular safety signals with dipeptidyl peptidase-4 inhibitors: A disproportionality analysis among high-risk patients.
Alexander, GC; Baksh, SN; McAdams-DeMarco, M; Segal, JB, 2018
)
0.48
" Treatment-emergent adverse events were reported in 33."( A Randomized, Single-Center, Double-Blind, Placebo-Controlled Multiple-Dose Phase 1 Study to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of Imarikiren in Healthy Adult Nonelderly and Elderly Male Subjects.
Hashimoto, T; Kagawa, T; Koumura, E; Matsuno, K; Nakamichi, H; Tanaka, S, 2018
)
0.48
" The adverse drug effects and discontinuation rates were investigated with self-reported complaint after starting or increasing anti-dementia drugs."( Safety and Efficacy of Anti-dementia Agents in the Extremely Elderly Patients with Dementia.
Cho, AH; Kim, JS; Lim, EY; Yang, DW, 2018
)
0.48
" The adverse drug effects were observed in 26 (33."( Safety and Efficacy of Anti-dementia Agents in the Extremely Elderly Patients with Dementia.
Cho, AH; Kim, JS; Lim, EY; Yang, DW, 2018
)
0.48
"The use of anti-dementia agents in the oldest old dementia patients may be safe and effective as the younger old dementia patients."( Safety and Efficacy of Anti-dementia Agents in the Extremely Elderly Patients with Dementia.
Cho, AH; Kim, JS; Lim, EY; Yang, DW, 2018
)
0.48
" DS-2969b was safe and well tolerated at all dose levels examined."( A Phase I, Single-Ascending-Dose Study in Healthy Subjects to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of DS-2969b, a Novel GyrB Inhibitor.
Dennie, J; Gajee, R; Inoue, S; Masuda, N; Pav, J; Senaldi, G; Uchiyama, M; Vandell, AG; Yamada, M; Zamora, C; Zhang, G, 2018
)
0.48
" In the pivotal ENGOT-OV16/NOVA trial, the dose reduction rate due to treatment-emergent adverse event (TEAE) was 68."( Safety and dose modification for patients receiving niraparib.
Berek, JS; Berton-Rigaud, D; Colombo, N; Ellard, S; Ghatage, P; Gonzalez-Martin, A; Guo, W; Hazard, S; Ledermann, J; Lesoin, A; Madry, R; Mahner, S; Matulonis, UA; Mirza, MR; Peen, U; Pineda, M; Redondo, A; Reinthaller, A; Rosengarten, O; Sehouli, J; Vergote, I, 2018
)
0.48
" Adverse events (AEs) are reported up to month 66 and laboratory data up to month 54."( Tofacitinib in patients with moderate-to-severe chronic plaque psoriasis: long-term safety and efficacy in an open-label extension study.
Bakos, N; Bissonnette, R; Gardner, AC; Harper, MK; Korman, NJ; Ports, WC; Tallman, A; Tan, H; Tsai, TF; Valdez, H; Valenzuela, F, 2018
)
0.48
" Adverse events (AEs) and serious AEs were reported in 82·5% and 13·7% of patients, respectively; 13·9% of patients discontinued owing to AEs; and 29 patients died."( Tofacitinib in patients with moderate-to-severe chronic plaque psoriasis: long-term safety and efficacy in an open-label extension study.
Bakos, N; Bissonnette, R; Gardner, AC; Harper, MK; Korman, NJ; Ports, WC; Tallman, A; Tan, H; Tsai, TF; Valdez, H; Valenzuela, F, 2018
)
0.48
" Frequencies of adverse events (AEs), serious AEs, and discontinuations due to AEs were similar for tofacitinib and placebo at month 3; serious infection events were more frequent for tofacitinib."( Tofacitinib 5 mg Twice Daily in Patients with Rheumatoid Arthritis and Inadequate Response to Disease-Modifying Antirheumatic Drugs: A Comprehensive Review of Phase 3 Efficacy and Safety.
Bensen, W; Bird, P; El-Zorkany, B; Kaine, J; Manapat-Reyes, BH; Pascual-Ramos, V; Soma, K; Thirunavukkarasu, K; Witcombe, D; Zhang, R, 2019
)
0.51
" The most common adverse events reported after MGV354 administration were conjunctival and ocular hyperemia."( A Randomized, Controlled Phase I/II Study to Evaluate the Safety and Efficacy of MGV354 for Ocular Hypertension or Glaucoma.
Adams, C; Grosskreutz, C; He, Y; Huttner, K; Kolega, R; Mogi, M; Newton, R; Ni, X; Peace, J; Prasanna, G; Sall, K; Seaman, J; Stacy, R; Wald, M; Walters, T; Watts, J; Wirta, D; Yan, JH, 2018
)
0.48
" Across both study parts, the number of subjects with treatment-emergent adverse events ranged from 0 to 3 per group with no dependency on dose."( Pharmacokinetics, Pharmacodynamics and Safety of a Single Dose of Imarikiren, a Novel Renin Inhibitor, in Healthy Male Subjects.
Kagawa, T; Koumura, E; Kuroda, S; Matsuno, K; Nakamichi, H; Tanaka, S, 2018
)
0.48
" Higher percentages of adverse events were detected in groups 2 (31."( Efficacy and safety of resveratrol, an oral hemoglobin F-augmenting agent, in patients with beta-thalassemia intermedia.
Bordbar, M; Eshghi, P; Haghpanah, S; Hoormand, M; Karimi, M; Zarei, T; Zekavat, O, 2018
)
0.48
" Piperine has been determined safe under conditions of intended use as a flavoring substance by regulatory and scientific expert bodies."( Absence of adverse effects following administration of piperine in the diet of Sprague-Dawley rats for 90 days.
Aubanel, M; Bastaki, M; Bauter, M; Cachet, T; Demyttenaere, J; Diop, MM; Harman, CL; Hayashi, SM; Krammer, G; Li, X; Llewellyn, C; Mendes, O; Renskers, KJ; Schnabel, J; Smith, BPC; Taylor, SV, 2018
)
0.48
"Active inflammatory bowel disease increases the risk of adverse pregnancy outcomes."( Outcomes of Pregnancies With Maternal/Paternal Exposure in the Tofacitinib Safety Databases for Ulcerative Colitis.
Baumgart, DC; Clowse, MEB; Dubinsky, MC; Feldman, SR; Graham, D; Jones, TV; Lawendy, N; Mahadevan, U; Marren, A; Su, C; Zhang, H, 2018
)
0.48
" Outcomes from tofacitinib rheumatoid arthritis (RA), psoriasis, and psoriatic arthritis interventional studies, and RA noninterventional postapproval safety studies, spontaneous adverse event reporting, and registry data are also reported."( Outcomes of Pregnancies With Maternal/Paternal Exposure in the Tofacitinib Safety Databases for Ulcerative Colitis.
Baumgart, DC; Clowse, MEB; Dubinsky, MC; Feldman, SR; Graham, D; Jones, TV; Lawendy, N; Mahadevan, U; Marren, A; Su, C; Zhang, H, 2018
)
0.48
" Although generally well tolerated, here we describe our institutional experience of unique adverse effects encountered with the use of ibrutinib in patients with B-cell lymphomas."( Case series of unique adverse events related to the use of ibrutinib in patients with B-cell malignancies-A single institution experience and a review of literature.
Albrethsen, M; Chilkulwar, A; Faisal, MS; Fazal, S; Khattab, A; Sadashiv, S; Shaikh, H, 2019
)
0.51
"This is a retrospective observational study done at a tertiary care facility, to evaluate adverse events in patients with B-cell malignancies on treatment with ibrutinib between 2014 and 2018."( Case series of unique adverse events related to the use of ibrutinib in patients with B-cell malignancies-A single institution experience and a review of literature.
Albrethsen, M; Chilkulwar, A; Faisal, MS; Fazal, S; Khattab, A; Sadashiv, S; Shaikh, H, 2019
)
0.51
"We found 10 patients with unique adverse events related to ibrutinib."( Case series of unique adverse events related to the use of ibrutinib in patients with B-cell malignancies-A single institution experience and a review of literature.
Albrethsen, M; Chilkulwar, A; Faisal, MS; Fazal, S; Khattab, A; Sadashiv, S; Shaikh, H, 2019
)
0.51
" The aim of this narrative review is to summarize the data concerning the drugs' basic mechanisms and clinical trial results in order to inform clinicians about the serious and non-serious adverse events associated with JAK inhibitors."( Adverse events, clinical considerations and management recommendations in rheumatoid arthritis patients treated with JAK inhibitors.
Atzeni, F; Gerratana, E; Marino, F; Masala, IF; Nucera, V; Sangari, D; Sarzi-Puttini, P; Talotta, R, 2018
)
0.48
"We conducted an integrated safety analysis to characterize the frequency, severity, natural history, and outcomes of adverse events (AEs) with ibrutinib versus comparators."( Safety Analysis of Four Randomized Controlled Studies of Ibrutinib in Patients With Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma or Mantle Cell Lymphoma.
Barr, PM; Burger, JA; Chang, S; Coutre, S; Cramer, P; Dilhuydy, MS; Fraser, G; Graef, T; Hess, G; Hillmen, P; Howes, A; James, DF; Liu, E; Moreno, C; O'Brien, S; Patel, K; Styles, L; Tedeschi, A; Valentino, R; Vermeulen, J, 2018
)
0.48
" The most frequent class of adverse events was infections and infestations."( Tofacitinib, an oral Janus kinase inhibitor, in patients from Brazil with rheumatoid arthritis: Pooled efficacy and safety analyses.
Akylbekova, EL; Brenol, CV; de Leon, DP; García, EG; Lomonte, ABV; Marcolino, FMD; Radominski, SC; Rojo, R; Zerbini, CAF, 2018
)
0.48
" Data suggest that immune-related adverse events (irAEs) are associated with clinical benefit in patients treated with immunotherapy and that response to BRAF/MEK therapy may have an underlying immune mechanism."( Possible immune adverse events as predictors of durable response to BRAF inhibitors in patients with BRAF V600-mutant metastatic melanoma.
Asher, N; Baruch, EN; Ben-Betzalel, G; Boursi, B; Markel, G; Schachter, J; Shapira-Frommer, R; Steinberg-Silman, Y, 2018
)
0.48
" Safety assessments included incidence rates (IRs) for serious adverse events (SAEs), discontinuations due to AEs, serious infection events, and herpes zoster (HZ), and were evaluated throughout the duration of the Phase 3 studies."( A pooled analysis of the safety of tofacitinib as monotherapy or in combination with background conventional synthetic disease-modifying antirheumatic drugs in a Phase 3 rheumatoid arthritis population.
Bananis, E; Cohen, S; Connell, CA; Fan, H; Fleischmann, R; Haraoui, B; Kaine, J; Keystone, E; Kivitz, AJ; Takiya, L; van Vollenhoven, RF, 2018
)
0.48
" No significant differences were observed in the incidence of serious adverse events after treatment with tofacitinib + MTX, baricitinib + MTX, adalimumab + MTX, or placebo + MTX."( Comparison of the efficacy and safety of tofacitinib and baricitinib in patients with active rheumatoid arthritis: a Bayesian network meta-analysis of randomized controlled trials.
Bae, SC; Lee, YH, 2019
)
0.51
"In RA patients with an inadequate response to DMARDs or biologics, tofacitinib 10 mg + MTX and baricitinib 4 mg + MTX were the most efficacious interventions and were not associated with a significant risk of serious adverse events."( Comparison of the efficacy and safety of tofacitinib and baricitinib in patients with active rheumatoid arthritis: a Bayesian network meta-analysis of randomized controlled trials.
Bae, SC; Lee, YH, 2019
)
0.51
" Imarikiren was safe and well-tolerated, regardless of the severity of RI or HI."( Pharmacokinetics and Safety After a Single Dose of Imarikiren in Subjects with Renal or Hepatic Impairment.
Aso, M; Itou, M; Kagawa, T; Kobayashi, T; Koumura, E; Kuroda, S; Matsuno, K; Saiki, T; Sakaki, M; Sano, Y; Shimasaki, Y; Shimizu, K, 2018
)
0.48
" Although memantine monotherapy and combination therapy are associated with a few individual adverse events such as somnolence, it is well-tolerated and its safety (all-cause discontinuation) is comparable or superior to that of the placebo (agitation)."( The efficacy and safety of memantine for the treatment of Alzheimer's disease.
Ikuta, T; Iwata, N; Kishi, T; Matsunaga, S; Nomura, I; Okuya, M; Sakuma, K, 2018
)
0.48
" The discontinuation rate due to adverse events (AEs) was pooled to evaluate their safety."( The efficacy and safety of ALK inhibitors in the treatment of ALK-positive non-small cell lung cancer: A network meta-analysis.
Fan, J; Fong, T; Luo, P; Xia, Z; Zhang, J, 2018
)
0.48
" This study employs bioactive surfactants in the common safe doses to improve PIP targeting to the brain."( Oral Brain-Targeted Microemulsion for Enhanced Piperine Delivery in Alzheimer's Disease Therapy: In Vitro Appraisal, In Vivo Activity, and Nanotoxicity.
Abdallah, OY; Abdelmonsif, DA; Elnaggar, YSR; Etman, SM, 2018
)
0.48
"This case emphasizes the uncommon adverse effect of the anaplastic lymphoma kinase-targeted therapy alectinib causing acute renal failure manifesting as acute tubular necrosis."( Alectinib (Alecensa)-induced reversible grade IV nephrotoxicity: a case report and review of the literature.
Morcus, R; Onukogu, I; Ramachandran, P; Spinowitz, B; Tahir, M; Wang, JC, 2018
)
0.48
" TKIs also act systemically causing various adverse events (AEs)."( Pazopanib, Cabozantinib, and Vandetanib in the Treatment of Progressive Medullary Thyroid Cancer with a Special Focus on the Adverse Effects on Hypertension.
Bauer, J; Grimm, D; Grosse, J; Infanger, M; Kopp, S; Krüger, M; Milling, RV; Wehland, M, 2018
)
0.48
"The signal is defined as "reported information on a possible causal relationship between an adverse event and a drug, of which the relationship is unknown or incompletely documented previously"."( Novel Adverse Events of Iloperidone: A Disproportionality Analysis in US Food and Drug Administration Adverse Event Reporting System (FAERS) Database.
Beulah, TE; Maheswari, E; Singh, H; Subeesh, V; Swaroop, AM, 2019
)
0.51
"To detect novel adverse events of iloperidone by disproportionality analysis in FDA database of Adverse Event Reporting System (FAERS) using Data Mining Algorithms (DMAs)."( Novel Adverse Events of Iloperidone: A Disproportionality Analysis in US Food and Drug Administration Adverse Event Reporting System (FAERS) Database.
Beulah, TE; Maheswari, E; Singh, H; Subeesh, V; Swaroop, AM, 2019
)
0.51
" We consider DECs for disproportionality analysis only if a minimum of ten reports are present in database for the given adverse event and which were not detected earlier (in clinical trials)."( Novel Adverse Events of Iloperidone: A Disproportionality Analysis in US Food and Drug Administration Adverse Event Reporting System (FAERS) Database.
Beulah, TE; Maheswari, E; Singh, H; Subeesh, V; Swaroop, AM, 2019
)
0.51
" The result requires an integration of further clinical surveillance for the quantification and validation of possible risks for the adverse events reported of iloperidone."( Novel Adverse Events of Iloperidone: A Disproportionality Analysis in US Food and Drug Administration Adverse Event Reporting System (FAERS) Database.
Beulah, TE; Maheswari, E; Singh, H; Subeesh, V; Swaroop, AM, 2019
)
0.51
" The network meta-analysis is applied to compare the efficacies and adverse events of five targeted agents (erlotinib, gefitinib, vandetanib, dacomitinib, and icotinib) for advanced or metastatic NSCLC."( Efficacy and adverse events of five targeted agents in the treatment of advanced or metastatic non-small-cell lung cancer: A network meta-analysis of nine eligible randomized controlled trials involving 5,059 patients.
Li, XF; Liu, GF; Miao, YY; Yu, SN; Zhang, SH, 2019
)
0.51
" Incidence rates for adverse events of special interest in tofacitinib-treated patients were similar to the global population."( Efficacy and Safety of Tofacitinib in Chinese Patients with Rheumatoid Arthritis.
An, Y; Bao, CD; Chen, ZW; Gu, JR; Hwang, LJ; Kremer, J; Li, ZG; Liu, Y; Wang, L; Wu, QZ; Xu, HJ; Zhao, DB, 2018
)
0.48
" Incidence rates (IRs; patients with events per 100 patient-years of exposure) were evaluated for select adverse events."( Safety of Tofacitinib for Treatment of Ulcerative Colitis, Based on 4.4 Years of Data From Global Clinical Trials.
Chan, G; D'Haens, GR; Friedman, GS; Jones, T; Lawendy, N; Moscariello, M; Panés, J; Pedersen, R; Sandborn, WJ; Sands, BE; Su, C, 2019
)
0.51
"In the maintenance cohort, IRs for select adverse events were similar among treatment groups, except for a numerically higher IR of herpes zoster infection among patients who received tofacitinib 5 mg twice daily (2."( Safety of Tofacitinib for Treatment of Ulcerative Colitis, Based on 4.4 Years of Data From Global Clinical Trials.
Chan, G; D'Haens, GR; Friedman, GS; Jones, T; Lawendy, N; Moscariello, M; Panés, J; Pedersen, R; Sandborn, WJ; Sands, BE; Su, C, 2019
)
0.51
" In comparison to systemic application, metformin displayed the most adverse effects in vitro in nearly all analyses, interestingly at serum equivalent concentrations."( Side effects of frequently used oral antidiabetics on wound healing in vitro.
Bachmann, HS; Besser, M; Koester, V; Severing, AL; Stuermer, EK; Terberger, N, 2019
)
0.51
"8% of patients treated with a combination of a sulfonylurea and insulin knew this side effect of the OAD."( Hypoglycemic side effects of sulfonylureas and repaglinide in ageing patients - knowledge and self-management.
Harsch, IA; Kaestner, RH; Konturek, PC, 2018
)
0.48
" The most common adverse events (AEs) included diarrhea, hypocalcemia, asthenia, QTc prolongation, hypokalemia and keratopathy, all at generally higher incidence with 300 vs 150 mg (Part A)."( Safety and efficacy of two starting doses of vandetanib in advanced medullary thyroid cancer.
Dedecjus, M; Druce, M; Elisei, R; Gagel, RF; Hu, MI; Kapiteijn, E; Krajewska, J; Locati, L; Pacini, F; Popovtzer, A; Weiss, R, 2019
)
0.51
" The most frequent adverse events across all groups were diarrhoea, vomiting, nasopharyngitis, falls, headache, insomnia, and anxiety."( Safety and efficacy of pridopidine in patients with Huntington's disease (PRIDE-HD): a phase 2, randomised, placebo-controlled, multicentre, dose-ranging study.
Borowsky, B; Eyal, E; Grachev, ID; Gross, N; Hayden, M; Kieburtz, K; Landwehrmeyer, GB; Langbehn, D; McGarry, A; Papapetropoulos, S; Reilmann, R; Savola, JM; Schubert, R; Squitieri, F; Wickenberg, AT, 2019
)
0.51
" Adverse events (AEs) of special interest were based on the known safety profile of poly(ADP-ribose) polymerase inhibitors."( Efficacy and safety of niraparib as maintenance treatment in older patients (≥ 70 years) with recurrent ovarian cancer: Results from the ENGOT-OV16/NOVA trial.
Banerjee, S; Bover, I; Dørum, A; Fabbro, M; Follana, P; Goffin, F; Harter, P; Hazard, SJ; Hellman, K; Mahner, S; Matulonis, UA; Mirza, MR; Moore, KN; Pineda, MJ; Provencher, D; Shapira-Frommer, R; Tinker, AV; Tognon, G; Vázquez, IP; Wenham, RM, 2019
)
0.51
" The most common all-grade adverse events were diarrhoea (47 [33%] of 141 patients), neutropenia (44 [31%]), and fatigue (37 [26%])."( Safety and activity of ibrutinib in combination with nivolumab in patients with relapsed non-Hodgkin lymphoma or chronic lymphocytic leukaemia: a phase 1/2a study.
Alvarez, J; Avivi, I; Balasubramanian, S; Ben-Yehuda, D; Bosch, F; Brody, J; Buglio, D; Caballero Barrigón, MD; Carpio, C; Ceulemans, R; Cordoba, R; de Jong, J; Demirkan, F; Ferhanoglu, B; Fourneau, N; Hellmann, A; Hodkinson, BP; Horowitz, NA; Jurczak, W; Kuss, B; Lopez-Guillermo, A; Ma, DDF; Marlton, P; Nagler, A; Ozcan, M; Schaffer, M; Streit, M; Wang, SS; Wrobel, T; Yağci, M; Younes, A, 2019
)
0.51
" Both groups had similar rates of adverse events and serious infections."( Long-term safety and tolerability of oral tofacitinib in patients with Crohn's disease: results from a phase 2, open-label, 48-week extension study.
Chan, G; D'Haens, GR; Higgins, PDR; Maller, E; Mele, L; Moscariello, M; Niezychowski, W; Panés, J; Su, C; Wang, W, 2019
)
0.51
" Clinical efficacy, structural progression, and treatment-emergent adverse events were evaluated."( Tofacitinib in Combination With Methotrexate in Patients With Rheumatoid Arthritis: Clinical Efficacy, Radiographic, and Safety Outcomes From a Twenty-Four-Month, Phase III Study.
Cardiel, MH; Cohen, S; Connell, CA; Fleischmann, R; Gruben, D; Keystone, E; Kremer, J; Nash, P; Song, YW; Strand, V; Tanaka, Y; Tegzová, D; van der Heijde, D; Wallenstein, G; Zerbini, CAF, 2019
)
0.51
"Vemurafenib and cobimetinib are extremely effective in treating V600E-mutated metastatic melanoma, but their use is associated with toxic cardiac effects."( Cardiac toxicity of combined vemurafenib and cobimetinib administration
.
Eleftheriou, G; Fiocchi, R; Gallo, M; Gori, M; Taddei, F; Trevisani, L, 2019
)
0.51
"This study aimed to evaluate the impact of early adverse events on overall survival (OS), progression-free survival (PFS) and objective response within a pooled secondary analysis of participants treated with first-line vemurafenib or vemurafenib plus cobimetinib in the clinical trials BRIM3 and coBRIM."( Effect of early adverse events on response and survival outcomes of advanced melanoma patients treated with vemurafenib or vemurafenib plus cobimetinib: A pooled analysis of clinical trial data.
Hopkins, AM; Rowland, A; Sorich, MJ; Van Dyk, M, 2019
)
0.51
" The primary endpoint was the incidence of adverse drug reactions (ADR), which are important identified risks for alectinib in Japanese patients."( Safety and effectiveness of alectinib in a real-world surveillance study in patients with ALK-positive non-small-cell lung cancer in Japan.
Gemma, A; Ishii, T; Kusumoto, M; Masuda, N; Ohe, Y; Yamada, I; Yamamoto, N, 2019
)
0.51
" We observed no significant differences in the incidence of serious adverse events after treatment with tofacitinib 10 mg, apremilast 30 mg, tofacitinib 5 mg, apremilast 20 mg, or placebo."( Comparison of the Efficacy and Safety of Tofacitinib and Apremilast in Patients with Active Psoriatic Arthritis: A Bayesian Network Meta-Analysis of Randomized Controlled Trials.
Lee, YH; Song, GG, 2019
)
0.51
"In patients with active psoriatic arthritis, tofacitinib 10 mg and apremilast 30 mg were the most efficacious interventions and were not associated with a significant risk of serious adverse events."( Comparison of the Efficacy and Safety of Tofacitinib and Apremilast in Patients with Active Psoriatic Arthritis: A Bayesian Network Meta-Analysis of Randomized Controlled Trials.
Lee, YH; Song, GG, 2019
)
0.51
" Here side effects of ibrutinib have been summarized and important considerations in the management of these adverse events have been reviewed."( Management of adverse effects/toxicity of ibrutinib.
Paydas, S, 2019
)
0.51
" Safety data pooled over 92 months from one P1, four P2, six P3, and two LTE studies for all tofacitinib doses (N = 1464) included incidence rates (IRs) (patients with events/100 patient-years) for adverse events (AEs) of special interest."( Efficacy and safety of tofacitinib for the treatment of rheumatoid arthritis in patients from the Asia-Pacific region: Post-hoc analyses of pooled clinical study data.
Chen, C; Kwok, K; Lee, EB; Liu, Y; Llamado, LJ; Luo, Y; Sugiyama, N; Tanaka, Y; Tsai, WC; Wang, L; Yamanaka, H; Yoo, HJ, 2019
)
0.51
" Overall, 52% of patients discontinued (24% due to adverse events [AEs] and 4% due to insufficient clinical response); the safety profile remained consistent with that observed in prior phase 1, 2, 3, or LTE studies."( Safety and efficacy of tofacitinib for up to 9.5 years in the treatment of rheumatoid arthritis: final results of a global, open-label, long-term extension study.
Cohen, S; Curtis, JR; DeMasi, R; Kwok, K; Lazariciu, I; Lee, EB; Mojcik, C; Silverfield, J; Soma, K; Strengholt, S; Terry, K; Wang, L; Wollenhaupt, J, 2019
)
0.51
" 19 and 37%, 50 and 40%, and 0 and 0% of patients in groups A and B, treated with crizotinib, ceritinib, and alectinib, respectively, developed high-grade adverse events."( Efficacy and Safety of ALK Tyrosine Kinase Inhibitors in Elderly Patients with Advanced ALK-Positive Non-Small Cell Lung Cancer: Findings from the Real-Life Cohort.
Allen, AM; Bar, J; Bedas, A; Dudnik, E; Maimon Rabinovich, N; Mishaeli, M; Peled, N; Rotem, O; Shochat, T; Zer, A, 2019
)
0.51
"In the elderly, crizotinib, ceritinib, and alectinib treatments are associated with similar efficacy but different safety profiles; alectinib is associated with a lower rate of high-grade adverse events and a lower treatment discontinuation rate."( Efficacy and Safety of ALK Tyrosine Kinase Inhibitors in Elderly Patients with Advanced ALK-Positive Non-Small Cell Lung Cancer: Findings from the Real-Life Cohort.
Allen, AM; Bar, J; Bedas, A; Dudnik, E; Maimon Rabinovich, N; Mishaeli, M; Peled, N; Rotem, O; Shochat, T; Zer, A, 2019
)
0.51
" In clinical trials, the most common digestive adverse events were nausea, vomiting, and diarrhoea."( Severe gastrointestinal toxicity of MEK inhibitors.
Allayous, C; Allez, M; Ballon, A; Baroudjian, B; Bertheau, P; Delyon, J; Eftekhari, P; Lebbé, C; Lourenço, N; Mourad, N; Pagès, C, 2019
)
0.51
" For safety, the incidence of adverse reactions was statistically significantly higher for tofacitinib compared with placebo."( Efficacy and safety of tofacitinib for the treatment of chronic plaque psoriasis: a systematic review and meta-analysis.
Chen, Z; Tian, F; Xu, T, 2019
)
0.51
"Treatment of chronic plaque psoriasis with tofacitinib is effective, but there may be more adverse reactions."( Efficacy and safety of tofacitinib for the treatment of chronic plaque psoriasis: a systematic review and meta-analysis.
Chen, Z; Tian, F; Xu, T, 2019
)
0.51
" Treatment-emergent adverse events (occurring within 48 hours of first dose) were considered in the analyses."( Safety findings from Phase 3 lasmiditan studies for acute treatment of migraine: Results from SAMURAI and SPARTAN.
Buchanan, AS; Doty, EG; Dowsett, SA; Krege, JH; Liffick, E; Rizzoli, PB; Wang, J, 2019
)
0.51
" There were no deaths; serious adverse events were reported for seven patients (placebo, n = 2 [0."( Safety findings from Phase 3 lasmiditan studies for acute treatment of migraine: Results from SAMURAI and SPARTAN.
Buchanan, AS; Doty, EG; Dowsett, SA; Krege, JH; Liffick, E; Rizzoli, PB; Wang, J, 2019
)
0.51
"As a centrally-penetrant drug, lasmiditan use was associated with neurologic treatment-emergent adverse events; most were mild or moderate in severity and self-limiting."( Safety findings from Phase 3 lasmiditan studies for acute treatment of migraine: Results from SAMURAI and SPARTAN.
Buchanan, AS; Doty, EG; Dowsett, SA; Krege, JH; Liffick, E; Rizzoli, PB; Wang, J, 2019
)
0.51
" Emerging real-world-data shows similar response and survival, but higher discontinuation rates due to adverse events (AEs)."( Safety and efficacy analysis of long-term follow up real-world data with ibrutinib monotherapy in 58 patients with CLL treated in a single-center in Greece.
Angelopoulou, M; Bitsani, C; Dimou, M; Iliakis, T; Kalyva, S; Koudouna, A; Kyrtsonis, MC; Panayiotidis, P; Papaioannou, P; Pardalis, V; Tsaftaridis, P; Vassilakopoulos, TP, 2019
)
0.51
" In the integrated analysis (ibrutinib treatment up to 43 months), the most common adverse events (AEs) were primarily grade 1/2; diarrhea (n = 173, 52% any-grade; n = 15, 5% grade 3) and fatigue (n = 119, 36% any-grade; n = 10, 3% grade 3)."( Long-term safety of single-agent ibrutinib in patients with chronic lymphocytic leukemia in 3 pivotal studies.
Barr, PM; Barrientos, JC; Burger, JA; Byrd, JC; Chang, S; Coutre, SE; Dean, JP; Devereux, S; Furman, RR; Ghia, P; Hillmen, P; James, DF; Kipps, TJ; Moreno, C; O'Brien, SM; O'Dwyer, M; Robak, T; Schuh, A; Valentino, R, 2019
)
0.51
" No significant differences were observed in the incidence of serious adverse events after treatment with tofacitinib + MTX, upadacitinib + MTX, adalimumab + MTX, or placebo + MTX."( Comparison of the efficacy and safety of tofacitinib and upadacitinib in patients with active rheumatoid arthritis: A Bayesian network meta-analysis of randomized controlled trials.
Choi, SJ; Lee, YH; Song, GG, 2019
)
0.51
"In RA patients with an inadequate response to cs- or b-DMARDs, upadacitinib 15 mg + MTX and upadacitinib 30 mg + MTX were the most efficacious interventions and were not associated with significant risks of serious adverse events."( Comparison of the efficacy and safety of tofacitinib and upadacitinib in patients with active rheumatoid arthritis: A Bayesian network meta-analysis of randomized controlled trials.
Choi, SJ; Lee, YH; Song, GG, 2019
)
0.51
"Cutaneous immune-related adverse events (irAEs) are a known consequence of immune checkpoint inhibitor (ICI) therapy and may exhibit a spectrum of morphologic features both clinically and histologically."( Lichenoid dermatitis from immune checkpoint inhibitor therapy: An immune-related adverse event with mycosis-fungoides-like morphologic and molecular features.
Aung, PP; Cabanillas, ME; Curry, JL; Duke, T; Duvic, M; Grabell, DA; Huen, A; Nagarajan, P; Prieto, VG; Tang, S; Tetzlaff, MT; Torres-Cabala, CA; Yao, JC; Zuo, Z, 2019
)
0.51
" All adverse events (AEs) reported were mild to moderate in severity."( Pharmacokinetics, Safety and Tolerability of JNJ-56136379, a Novel Hepatitis B Virus Capsid Assembly Modulator, in Healthy Subjects.
Berke, JM; Biewenga, J; De Zwart, L; Jessner, W; Snoeys, J; Talloen, W; van den Boer, M; Vandenbossche, J; Yogaratnam, J, 2019
)
0.51
" The frequencies of adverse events were similar between the two groups."( Efficacy and safety of tipepidine as adjunctive therapy in children with attention-deficit/hyperactivity disorder: Randomized, double-blind, placebo-controlled clinical trial.
Akhondzadeh, S; Bagheri, S; Dehbozorghi, S; Mohammadi, MR; Moradi, K; Shokraee, K, 2019
)
0.51
" The most common adverse events were nausea (rimegepant n=11 [2%]; placebo n=3 [<1%]) and urinary tract infection (rimegepant n=10 [1%]; placebo n=4 [1%])."( Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial.
Conway, CM; Coric, V; Croop, R; Forshaw, M; Goadsby, PJ; Lipton, RB; Stock, DA; Stock, EG, 2019
)
0.51
" Rates of adverse events were similar for patients using and not using preventive medications."( Efficacy and safety of lasmiditan in patients using concomitant migraine preventive medications: findings from SAMURAI and SPARTAN, two randomized phase 3 trials.
Ailani, J; Baygani, S; Hundemer, HP; Krege, JH; Loo, LS; Port, M; Schim, J, 2019
)
0.51
" In patients whose first dose was lasmiditan, the incidence of treatment emergent adverse events (TEAEs) reported after the second dose was similar whether second dose was lasmiditan or placebo."( Effect of a rescue or recurrence dose of lasmiditan on efficacy and safety in the acute treatment of migraine: findings from the phase 3 trials (SAMURAI and SPARTAN).
Case, MG; Dowsett, SA; Krege, JH; Loo, LS; Plato, BM; Raskin, J; Turner, IM, 2019
)
0.51
" Overall, treatment-emergent adverse events (TEAEs) were similar to those in the single-attack studies and included dizziness (18."( Interim results of a prospective, randomized, open-label, Phase 3 study of the long-term safety and efficacy of lasmiditan for acute treatment of migraine (the GLADIATOR study).
Brandes, JL; Case, M; Khanna, R; Klise, S; Krege, JH; Kudrow, D; Pearlman, EM; Raskin, J; Vasudeva, R, 2019
)
0.51
" Safety assessments included treatment-emergent adverse events (TEAEs)."( Efficacy and safety of blonanserin transdermal patch in patients with schizophrenia: A 6-week randomized, double-blind, placebo-controlled, multicenter study.
Agarkov, A; Correll, CU; Cosca, R; Higuchi, T; Inoue, Y; Ishigooka, J; Iwata, N; Kane, JM; Kim, WH; Lin, SK; Matsui, T; Sato, T; Suchkov, Y; Sulaiman, AH; Wang, L; Watabe, K; Yoon, BH, 2020
)
0.56
"There are limited data on treatment patterns, adverse events (AEs), and economic burden in younger, commercially insured patients treated for mantle cell lymphoma (MCL)."( Treatment patterns, adverse events, healthcare resource use and costs among commercially insured patients with mantle cell lymphoma in the United States.
Burudpakdee, C; Kabadi, SM; Near, A; Wada, K, 2019
)
0.51
" The most frequent treatment-emergent adverse events (AEs) in patients with FL and DLBCL, respectively, were diarrhea (16 [59%]; 16 [47%]), fatigue (12 [44%]; 16 [47%]), nausea (9 [33%]; 12 [35%]), peripheral edema (7 [26%]; 13 [38%]), decreased appetite (8 [30%]; 11 [32%]), neutropenia (6 [22%]; 11 [32%]), and vomiting (5 [19%]; 12 [35%])."( Safety and activity of ibrutinib in combination with durvalumab in patients with relapsed or refractory follicular lymphoma or diffuse large B-cell lymphoma.
Goy, A; Guan, S; Herrera, AF; Hill, JS; Kwei, K; Liu, EA; Mehta, A; Pagel, JM; Phillips, T; Ramchandren, R; Svoboda, J, 2020
)
0.56
" Common grade ≥3 adverse events (AEs) included neutropenia (13%), pneumonia (12%), hypertension (8%), anemia (7%), and hyponatremia (6%); occurrence of most events as well as discontinuations due to AEs decreased over time."( Long-term efficacy and safety of first-line ibrutinib treatment for patients with CLL/SLL: 5 years of follow-up from the phase 3 RESONATE-2 study.
Bairey, O; Barr, PM; Burger, JA; Coutre, SE; Dai, S; Dean, JP; Devereux, S; Ghia, P; Grosicki, S; Hillmen, P; Kipps, TJ; Lal, I; McCarthy, H; Moreno, C; Offner, F; Owen, C; Robak, T; Simpson, D; Tedeschi, A, 2020
)
0.56
" The incidence and severity of adverse events (AEs) were meticulously recorded in each case."( Tofacitinib in Pediatric Psoriasis: An Open-Label Trial to Study Its Safety and Efficacy in Children.
AlMutairi, N; Nour, T, 2020
)
0.56
" -Conclusion: The treatment with tofacitinib was safe and well tolerated, and led to significant improvement of their disease and quality of life as reflected in CDLQI scores."( Tofacitinib in Pediatric Psoriasis: An Open-Label Trial to Study Its Safety and Efficacy in Children.
AlMutairi, N; Nour, T, 2020
)
0.56
" We retrieved evidence on treatment-related grade III/IV adverse events, progression-free survival (PFS) and overall survival (OS)."( A systematic literature review and network meta-analysis of effectiveness and safety outcomes in advanced melanoma.
Franken, MG; Gheorghe, M; Haanen, JBAG; Leeneman, B; Uyl-de Groot, CA; van Baal, PHM, 2019
)
0.51
" Outcomes assessed included overall response rate (ORR), complete response (CR) rate, overall survival (OS), progression-free survival (PFS), and adverse events."( Matching-adjusted Indirect Comparisons of the Efficacy and Safety of Acalabrutinib Versus Other Targeted Therapies in Relapsed/Refractory Mantle Cell Lymphoma.
Abhyankar, S; Kabadi, SM; Signorovitch, J; Song, J; Telford, C; Yao, Z; Zhao, J, 2019
)
0.51
" Safety was assessed through adverse event (AE) reporting."( Pooled overall survival and safety data from the pivotal phase II studies (NP28673 and NP28761) of alectinib in ALK-positive non-small-cell lung cancer.
Ahn, JS; Balas, B; Barlesi, F; Bordogna, W; Crino, L; Dansin, E; De Petris, L; Dingemans, AM; Gadgeel, SM; Govindan, R; Kim, DW; Léna, H; Mitry, E; Morcos, PN; Müller, B; Ou, SI; Popat, S; Shaw, AT; Yang, JC, 2020
)
0.56
" In both ethnicities, most adverse events were mild."( Phase 1 Dose-Escalation Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of Tofacitinib in Japanese Healthy Volunteers.
Krishnaswami, S; Miyoshi, S; Nakamura, H; Toyoizumi, S; Zwillich, SH, 2020
)
0.56
" Adverse events occurred in 14 (37%) patients, including 6 severe adverse events and three herpes zoster infections."( Real-world evidence of tofacitinib effectiveness and safety in patients with refractory ulcerative colitis.
Abitbol, V; Amiot, A; Bouguen, G; Bouhnik, Y; Carbonnel, F; Dib, N; Fumery, M; Laharie, D; Lair-Mehiri, L; Pariente, B; Peyrin-Biroulet, L; Roblin, X; Rosa, I; Simon, M; Stefanescu, C; Treton, X; Vaysse, T; Viennot, S, 2020
)
0.56
" Thus, the developed pH sensitive lipoplexes promises to be a potential tumor targeting and safe delivery system than Lipofectamine® 2000."( Exploring the potential of novel pH sensitive lipoplexes for tumor targeted gene delivery with reduced toxicity.
Banerjee, SK; Chaudhari, D; Jain, S; Katare, PB; Katiyar, SS; Kuche, K; Kumar, Y; Swami, R, 2020
)
0.56
" No significant differences were observed in the incidence of serious adverse events after treatment with tofacitinib + MTX, filgotinib + MTX, adalimumab + MTX, or placebo + MTX."( Comparison of the efficacy and safety of tofacitinib and filgotinib in patients with active rheumatoid arthritis: a Bayesian network meta-analysis of randomized controlled trials.
Lee, YH; Song, GG, 2020
)
0.56
"In patients with RA exhibiting an inadequate response to cs- or bDMARDs, tofacitinib 10 mg + MTX and filgotinib 200 mg + MTX were the most efficacious interventions and risks of serious adverse events did not differ between tofacitinib and filgotinib groups."( Comparison of the efficacy and safety of tofacitinib and filgotinib in patients with active rheumatoid arthritis: a Bayesian network meta-analysis of randomized controlled trials.
Lee, YH; Song, GG, 2020
)
0.56
" Drug-induced IgA vasculitis has been previously described for anti-tumor necrosis factor-(TNF)α therapies, but this is the first report of this adverse effect with anti-JAK therapy."( IgA Vasculitis Developed as an Adverse Effect of Tofacitinib Taken for Rheumatoid Arthritis.
Hayashi, S; Itoh, I; Iwano, M; Kasuno, K; Kimura, H; Ojima, T; Shimizu, H; Takahashi, N; Yamamoto, C, 2020
)
0.56
" Safety outcomes included adverse events and serious adverse events."( Efficacy and safety of biologic agents and tofacitinib in moderate-to-severe ulcerative colitis: A systematic overview of meta-analyses.
Bonovas, S; Danese, S; Evripidou, D; Nikolopoulos, GK; Pantavou, K; Peyrin-Biroulet, L; Piovani, D; Yiallourou, AI, 2019
)
0.51
" Safety analyses indicated no increased rates of adverse events, except for infliximab."( Efficacy and safety of biologic agents and tofacitinib in moderate-to-severe ulcerative colitis: A systematic overview of meta-analyses.
Bonovas, S; Danese, S; Evripidou, D; Nikolopoulos, GK; Pantavou, K; Peyrin-Biroulet, L; Piovani, D; Yiallourou, AI, 2019
)
0.51
"Biologics and tofacitinib are efficacious and safe for treating UC."( Efficacy and safety of biologic agents and tofacitinib in moderate-to-severe ulcerative colitis: A systematic overview of meta-analyses.
Bonovas, S; Danese, S; Evripidou, D; Nikolopoulos, GK; Pantavou, K; Peyrin-Biroulet, L; Piovani, D; Yiallourou, AI, 2019
)
0.51
" Safety endpoints included the incidence of adverse events (AEs), treatment-related AEs, extrapyramidal AEs [also assessed using the change in Drug-Induced Extrapyramidal Symptoms Scale (DIEPSS) score], the use of any concomitant antiparkinsonian drugs, and skin-related AEs, including skin irritation."( Long-Term Safety and Efficacy of Blonanserin Transdermal Patches in Japanese Patients with Schizophrenia: A 52-Week Open-Label, Multicenter Study.
Higuchi, T; Ishigooka, J; Iwata, N; Kanamori, Y; Matsumoto, M; Nakamura, H; Naoi, I, 2020
)
0.56
"Blonanserin transdermal patches are safe and effective in the long-term treatment of schizophrenia."( Long-Term Safety and Efficacy of Blonanserin Transdermal Patches in Japanese Patients with Schizophrenia: A 52-Week Open-Label, Multicenter Study.
Higuchi, T; Ishigooka, J; Iwata, N; Kanamori, Y; Matsumoto, M; Nakamura, H; Naoi, I, 2020
)
0.56
" The primary outcome was incidence rates of adverse events (AEs) and serious AEs."( Safety of Janus Kinase Inhibitors in Patients With Inflammatory Bowel Diseases or Other Immune-mediated Diseases: A Systematic Review and Meta-Analysis.
Bonovas, S; Danese, S; Lasa, JS; Olivera, PA; Peyrin-Biroulet, L, 2020
)
0.56
"We explore factors that may have contributed to differences in treatment-emergent adverse events in the phase 2 and phase 3 lasmiditan clinical trials."( Issues Impacting Adverse Event Frequency and Severity: Differences Between Randomized Phase 2 and Phase 3 Clinical Trials for Lasmiditan.
Berg, PH; Hundemer, HP; Khanna, R; Krege, JH; Kudrow, D; Ossipov, MH; Pozo-Rosich, P, 2020
)
0.56
"Our objective was to compare the incidence rates (IRs) of adverse events in tofacitinib clinical trials and real-world observational data for alternative treatments."( An Integrated Analysis of the Safety of Tofacitinib in Psoriatic Arthritis across Phase III and Long-Term Extension Studies with Comparison to Real-World Observational Data.
Azevedo, VF; Biswas, P; Burmester, GR; Curtis, JR; FitzGerald, O; Hendrikx, T; Jones, T; Kanik, KS; Menon, S; Palmetto, N; Rigby, WFC; Rojo, R; Wang, C; Winthrop, KL; Yun, H, 2020
)
0.56
" IRs for serious infections (SIEs; requiring hospitalization), herpes zoster (HZ), malignancies (excluding non-melanoma skin cancer [NMSC]), NMSC, and major adverse cardiovascular events (MACE) across cohorts were qualitatively compared."( An Integrated Analysis of the Safety of Tofacitinib in Psoriatic Arthritis across Phase III and Long-Term Extension Studies with Comparison to Real-World Observational Data.
Azevedo, VF; Biswas, P; Burmester, GR; Curtis, JR; FitzGerald, O; Hendrikx, T; Jones, T; Kanik, KS; Menon, S; Palmetto, N; Rigby, WFC; Rojo, R; Wang, C; Winthrop, KL; Yun, H, 2020
)
0.56
" Moreover, no treatments were found to increase the occurrence of adverse events when compared with placebos, except infliximab."( Comparative of the Effectiveness and Safety of Biological Agents, Tofacitinib, and Fecal Microbiota Transplantation in Ulcerative Colitis: Systematic Review and Network Meta-Analysis.
Chen, LH; Guo, B; Li, BZ; Li, XM; Lufumpa, E; Meng, X; Zhou, HY, 2021
)
0.62
" Safety was assessed by monitoring, laboratory and physical examinations, vital signs, and recording adverse events (AEs)."( Safety, pharmacokinetics and pharmacodynamics of branebrutinib (BMS-986195), a covalent, irreversible inhibitor of Bruton's tyrosine kinase: Randomised phase I, placebo-controlled trial in healthy participants.
Catlett, IM; Girgis, IG; Grasela, DM; He, B; Kundu, S; Liu, A; Nowak, M; Zheng, N, 2020
)
0.56
" By measuring the antinociceptive and respiratory depressant effects of these ligands, we showed that the low intrinsic efficacy of opioid ligands can explain an improved side effect profile."( Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists.
Alamein, C; Canals, M; Christie, MJ; Connor, M; Fritzwanker, S; Gillis, A; Gondin, AB; Grimsey, NL; Halls, ML; Kassiou, M; Katte, TA; Kellam, B; Kliewer, A; Krasel, C; Lane, JR; Lim, HD; Manandhar, P; Reekie, T; Sanchez, J; Santiago, M; Schmiedel, F; Schulz, S, 2020
)
0.56
" Tofacitinib 5 mg, filgotinib 200 mg, and placebo showed a significantly lower serious adverse event rate than upadacitinib 15 mg."( Comparative efficacy and safety of tofacitinib, baricitinib, upadacitinib, and filgotinib in active rheumatoid arthritis refractory to biologic disease-modifying antirheumatic drugs.
Lee, YH; Song, GG, 2021
)
0.62
" The purpose of this study was to describe treatment patterns, adverse events (AEs), and economic burden among treated patients with CLL."( Real-World Treatment Patterns, Adverse Events, Resource Use, and Costs Among Commercially Insured, Younger Patients with Chronic Lymphocytic Leukemia in the USA: A Retrospective Cohort Study.
Burudpakdee, C; Kabadi, SM; Near, A; Wada, K, 2020
)
0.56
"Single doses of SUVN-G3031 up to 20 mg and multiple doses up to 6 mg once daily were found to be safe and well tolerated in healthy young adults."( Safety, Tolerability, and Pharmacokinetics of SUVN-G3031, a Novel Histamine-3 Receptor Inverse Agonist for the Treatment of Narcolepsy, in Healthy Human Subjects Following Single and Multiple Oral Doses.
Bhyrapuneni, G; Goyal, VK; Jetta, S; Mohammed, AR; Muddana, NR; Mudigonda, K; Nirogi, R; Palacharla, VRC; Pandey, SK; Ravula, J; Shinde, A, 2020
)
0.56
"SUVN-G3031 was found to be safe and well tolerated in healthy human subjects without any effect of age, gender, and food on the pharmacokinetics and safety profile."( Safety, Tolerability, and Pharmacokinetics of SUVN-G3031, a Novel Histamine-3 Receptor Inverse Agonist for the Treatment of Narcolepsy, in Healthy Human Subjects Following Single and Multiple Oral Doses.
Bhyrapuneni, G; Goyal, VK; Jetta, S; Mohammed, AR; Muddana, NR; Mudigonda, K; Nirogi, R; Palacharla, VRC; Pandey, SK; Ravula, J; Shinde, A, 2020
)
0.56
" Due to increasing use, characterization of their true adverse event profile is critical."( Pulmonary adverse events of small molecule JAK inhibitors in autoimmune disease: systematic review and meta-analysis.
Barnes, H; Glaspole, IN; Key, S; Khoo, JK; Östör, AJ, 2020
)
0.56
"We performed a systematic review and meta-analysis of all published trial data on the pulmonary and serious adverse effects of smTKIs in autoimmune disease."( Pulmonary adverse events of small molecule JAK inhibitors in autoimmune disease: systematic review and meta-analysis.
Barnes, H; Glaspole, IN; Key, S; Khoo, JK; Östör, AJ, 2020
)
0.56
" The risk of any serious pulmonary adverse events is low."( Pulmonary adverse events of small molecule JAK inhibitors in autoimmune disease: systematic review and meta-analysis.
Barnes, H; Glaspole, IN; Key, S; Khoo, JK; Östör, AJ, 2020
)
0.56
" Incidence rates (IRs; patients with events/100 patient-years) for adverse events of special interest (AESIs) were assessed throughout."( Tofacitinib in the treatment of Indian patients with rheumatoid arthritis: A post hoc analysis of efficacy and safety in Phase 3 and long-term extension studies over 7 years.
Adhav, C; Chandrashekara, S; Chopra, A; Kadel, JK; Kwok, K; Pandya, S; Rao, UR; Santos Estrella, P; Sharma, R; Shobha, V; Thorat, AV; Veeravalli, SCM; Wagh, S; Wouters, A; Yu, W, 2020
)
0.56
" No significant differences were observed in the incidence of serious adverse events after treatment with tofacitinib+MTX, peficitinib+MTX, adalimumab+MTX, or placebo+MTX."( Comparison of the efficacy and safety of tofacitinib and peficitinib in patients with active rheumatoid arthritis: A Bayesian network meta-analysis of randomized controlled trials.
Lee, YH; Song, GG, 2020
)
0.56
"In patients with RA with an inadequate response to DMARDs, tofacitinib 10 mg+MTX and peficitinib 150 mg+MTX were the most efficacious interventions and were not associated with a significant risk of serious adverse events."( Comparison of the efficacy and safety of tofacitinib and peficitinib in patients with active rheumatoid arthritis: A Bayesian network meta-analysis of randomized controlled trials.
Lee, YH; Song, GG, 2020
)
0.56
" However, the number of patients who experienced serious adverse events did not differ significantly between the JAK inhibitors, except for tofacitinib 5 mg, and placebo."( Comparative efficacy and safety of tofacitinib, baricitinib, upadacitinib, filgotinib and peficitinib as monotherapy for active rheumatoid arthritis.
Gyu Song, G; Ho Lee, Y, 2020
)
0.56
" American College of Rheumatology 20%, Health Assessment Questionnaire-Disability Index, adverse events, risk for infection, venous thromboembolic events, and malignancy were calculated."( Efficacy and Safety of Tofacitinib, Baricitinib, and Upadacitinib for Rheumatoid Arthritis: A Systematic Review and Meta-Analysis.
Davis, JM; Luo, F; Matteson, EL; Murad, MH; Sun, L; Vassallo, R; Wang, F; Wang, S, 2020
)
0.56
" Pain free and pain relief, global impression (very much/much better), and no/mild disability at 2 h in efficacy; total treatment-emergent adverse events (TEAEs), dizziness, nausea, fatigue, paraesthesia and somnolence in safety were extracted from the included studies."( Short-term efficacy and safety of lasmiditan, a novel 5-HT
Chen, J; Deng, D; Hou, M; Li, C; Li, J; Wang, X; Xing, H; Zhang, P, 2020
)
0.56
"This meta-analysis suggests that lasmiditan is effective for the acute treatment of migraine with a higher incidence of CNS-related adverse reactions compared with placebo."( Short-term efficacy and safety of lasmiditan, a novel 5-HT
Chen, J; Deng, D; Hou, M; Li, C; Li, J; Wang, X; Xing, H; Zhang, P, 2020
)
0.56
" Adverse events, concomitant medications, vital signs, laboratory values, and ECG data were monitored."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
0.56
" Pridopidine remained safe and well tolerated over the 60-month interval."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
0.56
"The 45 mg BID pridopidine dosage remained safe and tolerable over 60 months."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
0.56
" This study aims to evaluate the different efficacies of alectinib and crizotinib on progression-free survival (PFS), central nervous system (CNS) progression and adverse events (AEs) in NSCLC patients with ALK-positive."( Effect of alectinib versus crizotinib on progression-free survival, central nervous system efficacy and adverse events in ALK-positive non-small cell lung cancer: a systematic review and meta-analysis.
Wang, WJ; Xiang, RL; Xiang, ZJ; Yang, JH; Yang, YL, 2020
)
0.56
"6 % patients experienced ≥ grade 3 adverse events and serious adverse events."( Efficacy and safety of ibrutinib in diffuse large B-cell lymphoma: A single-arm meta-analysis.
Fang, H; Feng, Y; Hou, K; Huang, L; Jia, Y; Shao, S; Yu, Z, 2020
)
0.56
" Patient characteristics, ibrutinib use and adverse drug reactions (ADRs) were collected from medical records."( Patterns of use and safety of ibrutinib in real-life practice.
Allouchery, M; Delaunay, P; Delwail, V; Guidez, S; Lafay-Chebassier, C; Pérault-Pochat, MC; Salvo, F; Tomowiak, C, 2021
)
0.62
" Animal studies show no evidence of adverse effects on pre- or post-natal development after administration of vedolizumab and ustekinumab."( Safety of New Biologics (Vedolizumab and Ustekinumab) and Small Molecules (Tofacitinib) During Pregnancy: A Review.
Chaparro, M; Gisbert, JP, 2020
)
0.56
" Safety was assessed by recording drug-related adverse events, biochemical investigations, and electrocardiogram, along with tolerability and compliance."( Effectiveness, safety, and tolerability of bilastine 20 mg vs levocetirizine 5 mg for the treatment of chronic spontaneous urticaria: A double-blind, parallel group, randomized controlled trial.
Biswas, D; Chowdhury, SN; Das, A; Ghosh, S; Podder, I; Sengupta, S, 2020
)
0.56
"DFN-15 treatment may be effective and safe for pain control in migraine patients."( The Efficacy and Safety of DFN-15 for the Treatment of Migraine: A Meta-Analysis of Randomized Controlled Studies.
Chen, Y; Deng, Y; Peng, Z; Yang, H,
)
0.13
" Safety was evaluated from adverse events (AEs), clinical laboratory results, motor symptoms, electrocardiograms (ECG), and mortality."( Long-term evaluation of open-label pimavanserin safety and tolerability in Parkinson's disease psychosis.
Abler, V; Azulay, JP; Ballard, CG; Demos, G; Fernandez, HH; Ferreira, JJ; Ilic, TV; Isaacson, S; Kreitzman, DL; Liu, IY; Norton, JC; Stankovic, S, 2020
)
0.56
" In this review, the authors briefly discuss schizophrenia and its treatment, before they discuss properties of iloperidone, its indications, approval process, and adverse effects."( An update on the efficacy and safety of iloperidone as a schizophrenia therapy.
Asamoah, AL; Gosal, R; Grossberg, GT; Nair, A; Salem, A, 2020
)
0.56
"Among 66 patients who received ≥1 dose of study drug, all experienced an adverse event (AE)."( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors.
Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021
)
0.62
" We report here 13 additional patients with migraine who simultaneously used rimegepant and either erenumab, fremanezumab, or galcanezumab and assess the rate of on-treatment adverse events (AEs)."( Safety of Rimegepant, an Oral CGRP Receptor Antagonist, Plus CGRP Monoclonal Antibodies for Migraine.
Berman, G; Conway, CM; Coric, V; Croop, R; Halverson, P; Kudrow, D; Lipton, RB; Lovegren, M; Thiry, AC, 2020
)
0.56
" Safety, including collection of adverse events and the Mini-Mental State Examination (MMSE) and Movement Disorder Society-sponsored revision of the Unified Parkinson's Disease Rating Scale Part III (MDS-UPDRS III) scores, was assessed in patients who received ≥1 pimavanserin dose."( An Open-Label, 8-Week Study of Safety and Efficacy of Pimavanserin Treatment in Adults with Parkinson's Disease and Depression.
Abler, V; Aldred, JL; Alva, G; Cantillon, M; Coate, B; DeKarske, D; Jacobi, L; Norton, JC; Nunez, R, 2020
)
0.56
" Twenty-one of 47 patients experienced 42 treatment-emergent adverse events; the most common by system organ class were gastrointestinal (n = 7; 14."( An Open-Label, 8-Week Study of Safety and Efficacy of Pimavanserin Treatment in Adults with Parkinson's Disease and Depression.
Abler, V; Aldred, JL; Alva, G; Cantillon, M; Coate, B; DeKarske, D; Jacobi, L; Norton, JC; Nunez, R, 2020
)
0.56
" The pooled incidence of partial response (PR), stable disease (SD), TKI-related adverse events (AEs), and pooled median progression-free survival (PFS) were calculated with 95% confidence intervals (CI)."( Comparative efficacy and safety of tyrosine kinase inhibitors for thyroid cancer: a systematic review and meta-analysis.
Chino, T; Ito, KI; Ito, T; Kanai, T; Maeno, K; Oba, T; Ono, M; Shimizu, T; Soma, A, 2020
)
0.56
" Serious, related, unexpected adverse events requiring intervention had a low incidence and were largely due to predictable effects of the drugs being administered."( The safety profile and effectiveness of propofol-remifentanil mixtures for total intravenous anesthesia in children.
Bagshaw, O; Baxter, A; Brooks, P; Marriott, D; McCormack, J, 2020
)
0.56
" The safety analysis based on serious adverse events, adverse events (AEs), and withdrawals due to AEs revealed no statistically significant differences between the respective intervention groups."( Comparative study of the efficacy and safety of tofacitinib, baricitinib, upadacitinib, and filgotinib versus methotrexate for disease-modifying antirheumatic drug-naïve patients with rheumatoid arthritis.
Lee, YH; Sung, YK, 2021
)
0.62
" Adverse events, reasons for switching, and discontinuation were also determined."( Efficacy, retention, and safety of tofacitinib in real-life: Hur-bio monocentric experience
Akdoğan, A; Apraş Bilgen, ŞŞ; Bilgin, E; Bölek, EÇ; Ceylan, F; Duran, E; Ertenli, Aİ; Farisoğullari, B; Kalyoncu, U; Karadağ, Ö; Kiliç, L; Kiraz, S; Yardimci, GK, 2021
)
0.62
" The most common infectious and laboratory adverse events were herpes zoster infection (3."( Efficacy, retention, and safety of tofacitinib in real-life: Hur-bio monocentric experience
Akdoğan, A; Apraş Bilgen, ŞŞ; Bilgin, E; Bölek, EÇ; Ceylan, F; Duran, E; Ertenli, Aİ; Farisoğullari, B; Kalyoncu, U; Karadağ, Ö; Kiliç, L; Kiraz, S; Yardimci, GK, 2021
)
0.62
"These data demonstrate the importance of appropriate dose reduction according to toxicity criteria and support the safe long-term use of niraparib for maintenance treatment in patients with recurrent ovarian cancer."( Long-term safety in patients with recurrent ovarian cancer treated with niraparib versus placebo: Results from the phase III ENGOT-OV16/NOVA trial.
Barceló, IB; Benigno, B; Berton-Rigaud, D; Bessette, P; Buscema, J; de Jong, FA; du Bois, A; Dørum, A; Gupta, D; Herráez, AC; Herrstedt, J; Kalbacher, E; Lau, S; Ledermann, JA; Levy, T; Lorusso, D; Mahner, S; Matulonis, UA; Mirza, MR; Rimel, BJ; Vergote, I; Wang, P, 2020
)
0.56
" This study was designed to comprehensively assess the adverse events of AKI in real-world patients receiving small-molecule PKIs using the Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS)."( Assessment of acute kidney injury related to small-molecule protein kinase inhibitors using the FDA adverse event reporting system.
Fan, Q; Li, Q; Liu, F; Ma, J; Zhang, B; Zhao, B, 2020
)
0.56
"Among the 462,020 adverse event reports for small-molecule PKIs, 9970 (2."( Assessment of acute kidney injury related to small-molecule protein kinase inhibitors using the FDA adverse event reporting system.
Fan, Q; Li, Q; Liu, F; Ma, J; Zhang, B; Zhao, B, 2020
)
0.56
" Incidence rates (IRs; patients with events/100 patient-years [PY]; 95% CIs) of first-time occurrences were obtained for adverse events (AEs) of interest."( Long-term safety of tofacitinib up to 9.5 years: a comprehensive integrated analysis of the rheumatoid arthritis clinical development programme.
Biswas, P; Charles-Schoeman, C; Chen, C; Cohen, SB; Curtis, JR; Kwok, K; Lee, EB; Madsen, A; Mariette, X; Nash, P; Shapiro, A; Tanaka, Y; Wang, L; Winthrop, KL; Wollenhaupt, J, 2020
)
0.56
" In contrast, the number of patients with serious adverse events (SAEs) or withdrawals due to AEs did not differ significantly among the 4 treatment options."( Relative efficacy and safety of tofacitinib for treating psoriasis: A Bayesian network meta-analysis of randomized controlled trials.
Lee, YH; Song, GG, 2021
)
0.62
" Most common adverse events (AEs) leading to prior KI discontinuation were rash (27%), arthralgia (18%), and atrial fibrillation (16%)."( Phase 2 study of the safety and efficacy of umbralisib in patients with CLL who are intolerant to BTK or PI3Kδ inhibitor therapy.
Barr, PM; Barrientos, JC; Brander, DM; Cheson, BD; Dorsey, C; Flinn, IW; Fonseca, GA; Ghosh, N; Hamadeh, IS; Kambhampati, S; Lamanna, N; Lansigan, F; LaRatta, N; Luning Prak, ET; Mato, AR; Miskin, HP; Pagel, JM; Paskalis, D; Pu, JJ; Rai, KR; Reeves, JA; Roeker, L; Schuster, SJ; Sitlinger, A; Skarbnik, AP; Sportelli, P; Svoboda, J; Tsao, P; Weiss, MS; Weissbrot, H, 2021
)
0.62
" Safety evaluations included the incidence of treatment-emergent adverse events (TEAEs), including serious TEAEs."( Phase 2 single-arm study on the efficacy and safety of niraparib in Japanese patients with heavily pretreated, homologous recombination-deficient ovarian cancer.
Aoki, D; Hamanishi, J; Harano, K; Hasegawa, K; Hirasawa, T; Hori, K; Kase, Y; Komiyama, S; Kondo, E; Matsuura, M; Nakai, H; Nakamura, H; Nakamura, T; Okamoto, A; Sakata, J; Soeda, J; Sugiyama, T; Sumino, S; Suri, A; Tabata, T; Takehara, K; Takekuma, M; Yanagida, S; Yokoyama, Y, 2021
)
0.62
" Adverse drug reactions, such as akathisia and extrapyramidal symptoms, were common in all surveillances."( Safety and effectiveness of oral blonanserin for schizophrenia: A review of Japanese post-marketing surveillances.
Inoue, Y; Nakamura, H; Tsuchimori, K, 2021
)
0.62
" Symptomatic hypoglycemia, pancreatitis, skin disorders of non-extrinsic origin, severe infections, and cancer were collected as major adverse events (AEs)."( Long-term safety and efficacy of alogliptin, a DPP-4 inhibitor, in patients with type 2 diabetes: a 3-year prospective, controlled, observational study (J-BRAND Registry).
Abiko, A; Araki, E; Fujimoto, S; Fujiwara, M; Hayashi, M; Inagaki, N; Kadowaki, T; Katagiri, H; Miyoshi, H; Nakamura, J; Naruse, K; Nishimura, R; Okada, Y; Shikata, K; Shimada, A; Shimomura, I; Tanizawa, Y; Ueki, K; Watada, H; Yamada, Y; Yamazaki, T, 2021
)
0.62
"Alogliptin as a representative of DPP-4 inhibitors was safe and durably efficacious when used alone or with other OHAs for patients with type 2 diabetes in the real world setting."( Long-term safety and efficacy of alogliptin, a DPP-4 inhibitor, in patients with type 2 diabetes: a 3-year prospective, controlled, observational study (J-BRAND Registry).
Abiko, A; Araki, E; Fujimoto, S; Fujiwara, M; Hayashi, M; Inagaki, N; Kadowaki, T; Katagiri, H; Miyoshi, H; Nakamura, J; Naruse, K; Nishimura, R; Okada, Y; Shikata, K; Shimada, A; Shimomura, I; Tanizawa, Y; Ueki, K; Watada, H; Yamada, Y; Yamazaki, T, 2021
)
0.62
"All three topical ophthalmic medications used in the study are safe and effective in the treatment of allergic conjunctivitis."( Comparative analysis of safety and efficacy of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% in allergic conjunctivitis.
Ayyappanavar, S; Gangasagara, SB; Jayanthi, CR; Kumar, K; Mittal, P; Preethi, B; Rathod, BLS; Sridhar, S, 2021
)
0.62
" The primary endpoint (incidence of grade 3 or 4 thrombocytopenia-related events within 30 days after initial niraparib administration) was justified by the incidences of a global pivotal phase 3 study and its post-hoc safety analysis on thrombocytopenia, the major hematological adverse event of niraparib."( Phase 2 single-arm study on the safety of maintenance niraparib in Japanese patients with platinum-sensitive relapsed ovarian cancer.
Hamanishi, J; Hasegawa, K; Itamochi, H; Kase, Y; Matsumoto, T; Matsuura, M; Miura, K; Nagao, S; Nakai, H; Sumino, S; Suri, A; Takehara, K; Takeshima, N; Tanaka, N; Tokunaga, H; Ushijima, K; Watari, H; Yokoyama, Y, 2021
)
0.62
" Mucositis was the most common adverse event (67%), followed by diarrhea, fatigue, alopecia, anorexia, constipation, and nausea."( Aurora kinase A inhibitor, LY3295668 erbumine: a phase 1 monotherapy safety study in patients with locally advanced or metastatic solid tumors.
Batist, G; Bouganim, N; Chu, QS; de la Peña, A; Fortier, C; Hui, YH; Kremer, JD; Lithio, A; Smith, PS; Stille, JR; Yuen, E; Zaknoen, S, 2021
)
0.62
" Only 1 adverse event was reported: mild rhinorrhea in a participant with moderate hepatic impairment."( Single-Dose Pharmacokinetics and Safety of Atogepant in Adults With Hepatic Impairment: Results From an Open-Label, Phase 1 Trial.
Boinpally, R; Borbridge, L; Butler, M; Jakate, A; Periclou, A, 2021
)
0.62
"Limited published real-world data describe adverse events (AEs) among patients treated for mantle-cell lymphoma (MCL)."( Adverse Events and Economic Burden Among Patients Receiving Systemic Treatment for Mantle Cell Lymphoma: A Real-World Retrospective Cohort Study.
Byfield, SD; Kabadi, SM; LE, L; Olufade, T, 2021
)
0.62
" One patient in Cohort 2 discontinued due to adverse events."( Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine.
Dennehy, EB; Kerr, L; Khanna, R; Komori, M; Nery, ESM; Tsai, M; Wilbraham, D; Winner, P, 2021
)
0.62
" The number of patients with dose-limiting toxicities in cycle 1 and number with treatment-emergent adverse events were primary endpoints."( The safety, tolerability and pharmacokinetics of niraparib in Japanese patients with solid tumours: results of a phase I dose-escalation study.
Iwasa, S; Kase, Y; Kitano, S; Kondo, S; Koyama, T; Sato, J; Shibaki, R; Shimizu, T; Shimomura, A; Sumino, S; Suri, A; Tamura, K; Yamamoto, N; Yonemori, K, 2021
)
0.62
" All patients in both cohorts developed treatment-emergent adverse events."( The safety, tolerability and pharmacokinetics of niraparib in Japanese patients with solid tumours: results of a phase I dose-escalation study.
Iwasa, S; Kase, Y; Kitano, S; Kondo, S; Koyama, T; Sato, J; Shibaki, R; Shimizu, T; Shimomura, A; Sumino, S; Suri, A; Tamura, K; Yamamoto, N; Yonemori, K, 2021
)
0.62
" VAN + EV combination is safe and active in refractory solid tumors."( Safety and activity of vandetanib in combination with everolimus in patients with advanced solid tumors: a phase I study.
Amini, B; Bhatt, T; Cascone, T; Conley, AP; Drobnitzky, N; Falchook, GS; Fu, S; Hess, KR; Heymach, JV; Hong, DS; Janku, F; Karp, D; Meric-Bernstam, F; Naing, A; Piha-Paul, SA; Ryan, AJ; Sacks, RL; Sherman, SI; Subbiah, IM; Subbiah, V, 2021
)
0.62
"2%) had grade 3/4 treatment-emergent adverse events, the most common being thrombocytopenia (26."( Niraparib with androgen receptor-axis-targeted therapy in patients with metastatic castration-resistant prostate cancer: safety and pharmacokinetic results from a phase 1b study (BEDIVERE).
Bradic, B; Chi, KN; De Meulder, M; Espina, BM; Francis, P; Graff, JN; Hayreh, V; Hazra, A; Lattouf, JB; Mamidi, RNVS; Posadas, EM; Rezazadeh Kalebasty, A; Saad, F; Shore, ND; Yu, A; Zhu, E, 2021
)
0.62
"Secukinumab, ixekizumab, and tofacitinib were effective in PsA patients with inadequate response to TNF inhibitors, without serious adverse event risks."( Comparative efficacy and safety of secukinumab, ixekizumab, and tofacitinib in patients with active psoriatic arthritis showing insufficient response to tumor necrosis factor inhibitors.
Lee, YH; Song, GG, 2021
)
0.62
" Adverse events (AEs) were mild in intensity, and dose-dependent increase in AE prevalence was not apparent."( Safety, tolerability, pharmacokinetics, pharmacodynamics, bioavailability and food effect of single doses of soticlestat in healthy subjects.
Affinito, J; Chen, G; Cwik, M; Faessel, H; Merlo Pich, E; Wang, S, 2021
)
0.62
" No significant differences were noted in the incidence of serious adverse events (SAEs) after tofacitinib+MTX, mavrilimumab+MTX, or placebo+MTX."( Comparison of the efficacy and safety of tofacitinib and mavrilimumab in patients with active rheumatoid arthritis: A Bayesian network meta-analysis of randomized controlled trials.
Lee, YH; Sung, YK, 2021
)
0.62
" Grade greater than or equal to 3 adverse events occurred in 34."( Efficacy and Safety of Niraparib as Maintenance Treatment in Patients With Extensive-Stage SCLC After First-Line Chemotherapy: A Randomized, Double-Blind, Phase 3 Study.
Ai, X; Chen, G; Cui, J; Ding, C; Dong, X; Gao, B; He, J; Hu, C; Hu, X; Huang, C; Jiang, L; Li, J; Li, X; Li, Y; Liao, W; Liu, A; Liu, C; Liu, X; Liu, Z; Lu, S; Ma, Z; Pan, Y; Shi, J; Song, Y; Wang, K; Wang, M; Wang, W; Xiong, J; Yang, N; Zhang, B; Zhang, D; Zhang, H; Zhang, X; Zhang, Y; Zhao, J; Zhou, J, 2021
)
0.62
"Cardiovascular adverse events (CVAEs) associated with BRAF inhibitors alone versus combination BRAF/MEK inhibitors are not fully understood."( Cardiovascular adverse events associated with BRAF versus BRAF/MEK inhibitor: Cross-sectional and longitudinal analysis using two large national registries.
Al-Kindi, S; Barnholtz-Sloan, JS; de Lima, M; Dowlati, A; Fradley, MG; Guha, A; Gutierrez, JM; Jain, C; Jain, P; Lenihan, D; Oliveira, GH, 2021
)
0.62
" We utilized the cross-sectional FDA's Adverse Events Reporting System (FAERS) and longitudinal Truven Health Analytics/IBM MarketScan database from 2011 to 2018."( Cardiovascular adverse events associated with BRAF versus BRAF/MEK inhibitor: Cross-sectional and longitudinal analysis using two large national registries.
Al-Kindi, S; Barnholtz-Sloan, JS; de Lima, M; Dowlati, A; Fradley, MG; Guha, A; Gutierrez, JM; Jain, C; Jain, P; Lenihan, D; Oliveira, GH, 2021
)
0.62
"4%) were cardiovascular adverse events (mortality rate 19%)."( Cardiovascular adverse events associated with BRAF versus BRAF/MEK inhibitor: Cross-sectional and longitudinal analysis using two large national registries.
Al-Kindi, S; Barnholtz-Sloan, JS; de Lima, M; Dowlati, A; Fradley, MG; Guha, A; Gutierrez, JM; Jain, C; Jain, P; Lenihan, D; Oliveira, GH, 2021
)
0.62
" Response and adverse events (AEs) were analyzed by Response Evaluation Criteria in Solid Tumors v1."( The efficacy and safety of niraparib for ovarian cancer: a single-center observational study from China.
Chen, X; Cheng, X; Dai, Z; Gu, H; Guo, W; Ni, J; Wang, Y; Xu, X; Zhao, Q; Zhou, R, 2021
)
0.62
" Leg swelling was observed as a new adverse event."( The efficacy and safety of niraparib for ovarian cancer: a single-center observational study from China.
Chen, X; Cheng, X; Dai, Z; Gu, H; Guo, W; Ni, J; Wang, Y; Xu, X; Zhao, Q; Zhou, R, 2021
)
0.62
" The pooled estimate of incidence rate of adverse events was 53."( Effectiveness and safety of tofacitinib for the treatment of ulcerative colitis: A single-arm meta-analysis of observational studies.
Macaluso, FS; Maida, M; Orlando, A; Ventimiglia, M, 2022
)
0.72
"To analyse adverse events (AEs) of special interest across tofacitinib clinical programmes in rheumatoid arthritis (RA), psoriatic arthritis (PsA), ulcerative colitis (UC) and psoriasis (PsO), and to determine whether the incidence rates (IRs; unique patients with events per 100 patient-years) of these events are consistent across diseases."( Adverse events of special interest in clinical trials of rheumatoid arthritis, psoriatic arthritis, ulcerative colitis and psoriasis with 37 066 patient-years of tofacitinib exposure.
Burmester, GR; Cohen, SB; Jones, TV; Madsen, A; Nash, P; Papp, K; Sands, BE; Stockert, L; Tan, H; Valdez, H, 2021
)
0.62
" The tofacitinib is found to be safe in SLE meeting study's primary endpoint."( Phase 1 double-blind randomized safety trial of the Janus kinase inhibitor tofacitinib in systemic lupus erythematosus.
Apps, R; Babyak, AL; Biancotto, A; Biehl, AJ; Brooks, SR; Carlucci, PM; Chen, J; Cheung, F; Davis, M; Diamond, B; Gadina, M; Gazaniga, N; Giudice, V; Goel, RR; Gregersen, P; Gupta, S; Hasni, SA; Kaplan, MJ; Kotliarov, Y; Li, X; Lu, S; MacKay, M; Manna, Z; Mehta, NN; Naqi, M; O'Shea, JJ; Ochoa-Navas, I; Playford, MP; Poncio, E; Remaley, AT; Shi, R; Shi, Y; Stagliano, K; Temesgen-Oyelakin, Y; Thomas, D; Tsai, WL; Vian, L; Wang, X; Zhou, H, 2021
)
0.62
" Adverse events (AEs), serious AEs and discontinuations due to AEs were reported by 362 (52."( Efficacy and safety of tofacitinib modified-release 11 mg once daily plus methotrexate in adult patients with rheumatoid arthritis: 24-week open-label phase results from a phase 3b/4 methotrexate withdrawal non-inferiority study (ORAL Shift).
Cohen, SB; Diehl, A; Germino, R; Haraoui, B; Keystone, EC; Liu, S; Lukic, T; Menon, S; Mysler, E; Pope, J; Shi, H; Stockert, L, 2021
)
0.62
" Adverse drug reactions were recorded for each subject during drug administration and follow-up visits."( Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.
Abad-Santos, F; Arranz, P; Belmonte, C; Elgezabal, L; Fernández, N; Hernández, G; Martín-Vilchez, S; Mejía-Abril, G; Ochoa, D; Román, M, 2021
)
0.62
" Adverse events were mild and transient, consisting mainly of dysgeusia."( Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.
Abad-Santos, F; Arranz, P; Belmonte, C; Elgezabal, L; Fernández, N; Hernández, G; Martín-Vilchez, S; Mejía-Abril, G; Ochoa, D; Román, M, 2021
)
0.62
" Outcomes included sustained pain freedom and -relief 2-48 hours post-dose, and adverse events."( Comparative efficacy and safety of rimegepant, ubrogepant, and lasmiditan for acute treatment of migraine: a network meta-analysis.
Coric, V; Croop, R; Dabirvaziri, P; Deighton, A; Harris, L; Johnston, K; L'Italien, G; Moren, J; Popoff, E; Thiry, A, 2022
)
0.72
" However, lasmiditan 200 mg was also associated with higher rates of adverse events, particularly somnolence and dizziness."( Comparative efficacy and safety of rimegepant, ubrogepant, and lasmiditan for acute treatment of migraine: a network meta-analysis.
Coric, V; Croop, R; Dabirvaziri, P; Deighton, A; Harris, L; Johnston, K; L'Italien, G; Moren, J; Popoff, E; Thiry, A, 2022
)
0.72
"This was a randomized, double-blind, placebo-controlled trial in 42 (to deliver 36 with combination treatment) healthy elderly subjects investigating the effects of oral HTL0018318 15 and 25 mg given alone and combined with donepezil 10 mg at steady state on adverse events (AEs), vital signs, saliva production, sleep quality, pulmonary function, subjective feelings, and pharmacokinetics."( Safety and Pharmacokinetics of HTL0018318, a Novel M
Bakker, C; Cross, DM; Dickinson, S; Groeneveld, GJ; Klaassen, ES; Labots, G; Liptrot, J; Tasker, T; van der Aart, J, 2021
)
0.62
" There was no consistent trend between BMI and adverse events."( The impact of body mass index on efficacy and safety in the tofacitinib OCTAVE ulcerative colitis clinical programme.
Farraye, FA; Judd, DT; Kotze, PG; Lawendy, N; Moore, GT; Mundayat, R; Qazi, T; Sharma, PP, 2021
)
0.62
" No serious adverse events, no case of herpes zoster, but two cases of deep vein thrombosis were seen."( Efficacy and Safety of Tofacitinib for Treatment of Moderate to Severe Active Ulcerative Colitis: First Report from Iran.
Alatab, S; Anushiravani, A; Jameshorani, M; Malekzadeh, MM; Naserinejad, S; Nateghi Beige, H; Sadeghi, A; Sima, AR; Vahedi, H, 2021
)
0.62
" Target drug-associated AKI signals were detected by reporting odds ratio (ROR) derived from report data in the Food and Drug Administration Adverse Events Reporting System database."( BRAF/MEK inhibitor-associated nephrotoxicity in a real-world setting and human kidney cells.
Hotta, Y; Kataoka, T; Kimura, K; Mori, N; Sanagawa, A; Tohkin, M; Tomita, N, 2021
)
0.62
"Ibrutinib has superior progression-free survival compared with bendamustine plus rituximab (BR) in older CLL patients, however, differences in treatment duration, six monthly BR cycles versus continuous ibrutinib, complicate adverse event (AE) comparisons."( Adverse event burden in older patients with CLL receiving bendamustine plus rituximab or ibrutinib regimens: Alliance A041202.
Abramson, JS; Bartlett, NL; Booth, AM; Brander, DM; Brown, JR; Byrd, JC; Coutre, S; Ding, W; Erba, H; Kuzma, CS; Larson, RA; Little, RF; Litzow, M; Mandrekar, SJ; Nattam, S; Owen, C; Ruppert, AS; Smith, SE; Stone, RM; Woyach, JA, 2021
)
0.62
" The primary outcome was nezulcitinib safety and tolerability assessed from treatment-emergent adverse events (TEAEs)."( Phase I study in healthy participants to evaluate safety, tolerability, and pharmacokinetics of inhaled nezulcitinib, a potential treatment for COVID-19.
Bourdet, DL; Colley, K; Lo, A; Pfeifer, ND; Singh, D, 2021
)
0.62
" Based on therapeutic drug monitoring of cyclosporin A plasma level, the dose of cyclosporine A has been adjusted to achieve a safe and effective therapeutic level in terms of both cancer treatment and kidney transplant condition."( Drug interaction profile of TKI alectinib allows effective and safe treatment of ALK+ lung cancer in the kidney transplant recipient.
Bilek, O; Borilova, S; Holanek, M; Jurica, J; Kazda, T; Kiss, I; Poprach, A; Selingerova, I; Stepankova, S; Vasina, J; Zdrazilova-Dubska, L, 2021
)
0.62
" Adverse events (AEs) were reported in 36."( Safety and Efficacy of Tofacitinib in Combination With Biologic Therapy for Refractory Crohn's Disease.
Barahimi, M; Clark-Snustad, KD; Harper, J; Jacobs, J; Kamp, KJ; Lee, SD; Singla, A, 2022
)
0.72
"These post hoc analyses evaluated the incidence of treatment-emergent adverse events (TEAEs) in elderly (≥65 years of age) versus nonelderly (<65 years of age) lasmiditan-treated patients."( Tolerability and Safety of Lasmiditan Treatment in Elderly Patients With Migraine: Post Hoc Analyses From Randomized Studies.
Ahmed, Z; Baygani, SK; Dong, Y; Hauck, PM; Hochstetler, HM; Khanna, R; Martin, VT, 2021
)
0.62
"The occurrence of adverse events was revealed as a major cause of ibrutinib failure in the real-world."( Keeping a balance in chronic lymphocytic leukemia (CLL) patients taking ibrutinib: ibrutinib-associated adverse events and their management based on drug interactions.
Baek, DW; Cho, HJ; Kim, J; Lee, JM; Moon, JH; Sohn, SK, 2021
)
0.62
" Outcomes of interest included: serious adverse event (SAE), discontinuation due to adverse event (AE), interruption of treatment due to AE, dose reduction due to AE, and specific grade 1-5 AEs."( Comparative safety and tolerability of approved PARP inhibitors in cancer: A systematic review and network meta-analysis.
Cai, Z; Cao, D; Chang, C; Jiang, Z; Liu, C; Mu, M; Shen, C; Yin, X; Yin, Y; Zhang, B; Zhang, L; Zhao, Z, 2021
)
0.62
" While 176 adverse events (AEs) were reported in 74 (54."( Efficacy and Safety of Ibrutinib Therapy in Patients with Chronic Lymphocytic Leukemia: Retrospective Analysis of Real-Life Data
Akay, OM; Akdeniz, A; Akpınar, S; Aydoğdu, İ; Baştürk, A; Batur, DS; Berber, İ; Çekdemir, D; Çetin, G; Davulcu, EA; Demircioğlu, S; Deveci, B; Dinçyürek, HD; Doğu, MH; Durusoy, SS; Ertop, Ş; Ferhanoğlu, B; Güneş, AK; Gürkan, E; İlhan, G; Kaya, E; Kızıklı, A; Kurtoğlu, E; Mehtap, Ö; Okan, V; Okay, M; Özcan, MA; Özcan, Ö; Özet, G; Özkocamaz, V; Pepedil Tanrıkulu, F; Sahip, B; Saydam, G; Sayınalp, N; Seyhanlı, A; Sönmez, M; Terzi, H; Tombak, A; Turgut, B; Uçar, MA; Ümit, EG; Ünal, A; Yavaşoğlu, İ; Yıldırım, R; Yılmaz, M, 2021
)
0.62
"This real-life analysis confirms the favorable efficacy and safety profile of long-term ibrutinib treatment while emphasizing the potential adverse impacts of poorer ECOG performance status, heavy treatment prior to ibrutinib, and advanced Rai stage on patient compliance, treatment response, and survival outcomes."( Efficacy and Safety of Ibrutinib Therapy in Patients with Chronic Lymphocytic Leukemia: Retrospective Analysis of Real-Life Data
Akay, OM; Akdeniz, A; Akpınar, S; Aydoğdu, İ; Baştürk, A; Batur, DS; Berber, İ; Çekdemir, D; Çetin, G; Davulcu, EA; Demircioğlu, S; Deveci, B; Dinçyürek, HD; Doğu, MH; Durusoy, SS; Ertop, Ş; Ferhanoğlu, B; Güneş, AK; Gürkan, E; İlhan, G; Kaya, E; Kızıklı, A; Kurtoğlu, E; Mehtap, Ö; Okan, V; Okay, M; Özcan, MA; Özcan, Ö; Özet, G; Özkocamaz, V; Pepedil Tanrıkulu, F; Sahip, B; Saydam, G; Sayınalp, N; Seyhanlı, A; Sönmez, M; Terzi, H; Tombak, A; Turgut, B; Uçar, MA; Ümit, EG; Ünal, A; Yavaşoğlu, İ; Yıldırım, R; Yılmaz, M, 2021
)
0.62
" Safety assessments included adverse events and laboratory parameters."( Efficacy and safety of tofacitinib by background methotrexate dose in psoriatic arthritis: post hoc exploratory analysis from two phase III trials.
Azevedo, VF; FitzGerald, O; Kivitz, AJ; Nash, P; Pang, S; Takiya, L; Wang, C, 2022
)
0.72
" Secondary outcomes included clinical response, steroid free remission, and adverse events (AEs)."( Effectiveness and Safety of Tofacitinib for Ulcerative Colitis: Systematic Review and Meta-analysis.
Bain, PA; El-Dallal, M; Feuerstein, JD; Haq, Z; Said, H; Systrom, HK; Taneja, V; Tripathi, K; Wang, LF; Zhou, Y,
)
0.13
"Donepezil 23 mg is considered for Alzheimer's disease (AD) to optimize cognitive benefits; however, increased adverse events (AEs) can negatively influence drug adherence."( Effects of Body Weight on the Safety of High-Dose Donepezil in Alzheimer's Disease: Post hoc Analysis of a Multicenter, Randomized, Open-Label, Parallel Design, Three-Arm Clinical Trial.
Han, HJ; Hong, YJ; Kim, HJ; Kim, S; Kwon, M; Lee, JH; Lee, Y; Park, KW; Yang, DW; Youn, YC, 2021
)
0.62
" The most common grade 3 adverse events were rash/pruritis/dermatitis (19%), diarrhea (11%), hyperglycemia (11%), and hypertension (11%)."( Phase I/Ib Study of the Efficacy and Safety of Buparlisib and Ibrutinib Therapy in MCL, FL, and DLBCL with Serial Cell-Free DNA Monitoring.
Batlevi, CL; De Frank, S; Drullinsky, P; Gerecitano, JF; Hamilton, A; Hamlin, PA; Horwitz, SM; Kumar, A; Matasar, MJ; Michaud, L; Moskowitz, A; Moskowitz, CH; Nakajima, R; Nichols, C; Rademaker, J; Salles, G; Schöder, H; Seshan, V; Stewart, CM; Straus, D; Tsui, DWY; Whiting, K; Younes, A; Zelenetz, AD, 2022
)
0.72
" Post-marketing surveillance (PMS) is an important part of monitoring adverse events (AEs)."( Worldwide post-marketing safety surveillance experience with tofacitinib in ulcerative colitis.
Danese, S; Jones, TV; Koram, N; Kwok, KK; Modesto, I; Ng, SC; Rubin, DT; Vermeire, S, 2022
)
0.72
"Lasmiditan with the 50 mg, 100 mg, and 200 mg doses are effective and safe in acute migraine treatment."( The Effect and Safety of 5-HT
Chen, C; Dong, C; Dong, X; Gu, P; Wan, Q; Wang, T; Wu, Q, 2021
)
0.62
" In all subjects dosed with telacebec (10 to 800 mg), telacebec was well tolerated and did not lead to any significant or serious adverse events."( Safety, Tolerability, and Pharmacokinetics of Telacebec (Q203), a New Antituberculosis Agent, in Healthy Subjects.
Ahn, J; Choi, J; Hutchings, J; Jeon, Y; Kang, H; Kim, J; Nam, K; Park, D; Shin, BS; Shin, S; van Niekerk, C, 2022
)
0.72
" We constructed a pooled safety analysis to better understand zanubrutinib-associated treatment-emergent adverse events (TEAEs) and identify treatment-limiting toxicities."( Pooled safety analysis of zanubrutinib monotherapy in patients with B-cell malignancies.
Chan, WY; Cohen, A; Cull, G; D'Sa, S; Dimopoulos, M; Du, C; Garcia-Sanz, R; Gottlieb, D; Guo, H; Huang, J; Ji, M; Jurczak, W; Li, J; Marlton, P; Munoz, J; Novotny, W; Opat, S; Owen, R; Phillips, T; Qiu, L; Roberts, AW; Song, Y; Tam, CS; Tedeschi, A; Trotman, J; Xu, W; Zhou, L; Zhu, H; Zhu, J, 2022
)
0.72
" The incidences of treatment-emergent serious adverse events (SAEs) were - placebo, n=2 (0."( Safety findings from CENTURION, a phase 3 consistency study of lasmiditan for the acute treatment of migraine.
Ardayfio, PA; Bragg, S; Doty, EG; Dowsett, SA; Krege, JH; Ruff, D; Schwedt, T; Tassorelli, C, 2021
)
0.62
"1%) experienced grade ≥3 treatment-related adverse events (TRAE), leading to discontinuation in 27 patients (10."( Tepotinib Efficacy and Safety in Patients with MET Exon 14 Skipping NSCLC: Outcomes in Patient Subgroups from the VISION Study with Relevance for Clinical Practice.
Berghoff, K; Bestvina, CM; Britschgi, C; Bruns, R; Chen, YM; Cho, BC; Cortot, AB; Felip, E; Garassino, MC; Gottfried, M; Griesinger, F; Heymach, J; Iams, WT; Johnson, M; Kim, HR; Le, X; Mazieres, J; Otto, G; Paik, PK; Park, K; Patel, JD; Raskin, J; Sakai, H; Schumacher, KM; Sikoglu, E; Smit, EF; Thomas, M; Veillon, R; Viteri, S; Yang, JC, 2022
)
0.72
"Immune checkpoint inhibitors (ICIs) have demonstrated marked efficacy in some cancer patients, but they may cause various severe immune-related adverse events."( Severe Skin Toxicity Caused by Sequential Anti-PD-1 Antibody and Alectinib in Non-small-cell Lung Cancer: A Report of Two Cases and a Literature Review.
Hattori, Y; Murayama, T; Nishiyama, A; Satouchi, M; Takeuchi, S; Tanimoto, A; Yano, S, 2022
)
0.72
" Eligible studies reported at least one of the following outcomes: progression free survival (PFS), overall survival (OS), objective response rate (ORR), or adverse events of grade 3 or higher (Grade ≥ 3 AEs)."( Comparative efficacy and safety of first-line treatments for advanced non-small cell lung cancer with ALK-rearranged: a meta-analysis of clinical trials.
Chang, XS; Chen, YD; Ding, KL; Liu, YF; Liu, YH; Ma, HC; Xiao, ZZ; Yu, YY; Zhang, HB; Zhao, WJ; Zhou, R; Zhu, YJ, 2021
)
0.62
" On the other hand, ceritinib showed the highest rate of severe adverse events (60%)."( Comparative efficacy and safety of first-line treatments for advanced non-small cell lung cancer with ALK-rearranged: a meta-analysis of clinical trials.
Chang, XS; Chen, YD; Ding, KL; Liu, YF; Liu, YH; Ma, HC; Xiao, ZZ; Yu, YY; Zhang, HB; Zhao, WJ; Zhou, R; Zhu, YJ, 2021
)
0.62
" Incidence rates (unique patients with events/100 patient-years) for adverse events of special interest were calculated; ≤7."( Safety and efficacy of tofacitinib for treatment of ulcerative colitis: final analysis of OCTAVE Open, an open-label, long-term extension study with up to 7.0 years of treatment.
Damião, AOMC; Danese, S; Dotan, I; Guo, X; Hart, A; Judd, DT; Lawendy, N; Loftus, EV; Modesto, I; Panés, J; Sandborn, WJ; Su, C; Wang, W, 2022
)
0.72
"Adverse events were generally mild, but one case of fatal suspected unexpected serious adverse reaction occurred."( Safety and efficacy of the mRNA BNT162b2 vaccine against SARS-CoV-2 in five groups of immunocompromised patients and healthy controls in a prospective open-label clinical trial.
Akber, M; Aleman, S; Bergman, P; Blennow, O; Blixt, L; Bogdanovic, G; Buggert, M; Chen, MS; Chen, P; Friman, G; Gomez, AC; Hansson, L; Hober, S; Lindgren, G; Ljunggren, HG; Ljungman, P; Loré, K; Mielke, S; Muschiol, S; Nilsson, P; Nordlander, A; Norlin, AC; Nowak, P; Österborg, A; Smith, CIE; Söderdahl, G; Thalme, A; Valentini, D; Vesterbacka, J; Wahren-Borgström, E; Wullimann, D, 2021
)
0.62
"The results showed that the mRNA BNT162b2 vaccine was safe in immunocompromised patients."( Safety and efficacy of the mRNA BNT162b2 vaccine against SARS-CoV-2 in five groups of immunocompromised patients and healthy controls in a prospective open-label clinical trial.
Akber, M; Aleman, S; Bergman, P; Blennow, O; Blixt, L; Bogdanovic, G; Buggert, M; Chen, MS; Chen, P; Friman, G; Gomez, AC; Hansson, L; Hober, S; Lindgren, G; Ljunggren, HG; Ljungman, P; Loré, K; Mielke, S; Muschiol, S; Nilsson, P; Nordlander, A; Norlin, AC; Nowak, P; Österborg, A; Smith, CIE; Söderdahl, G; Thalme, A; Valentini, D; Vesterbacka, J; Wahren-Borgström, E; Wullimann, D, 2021
)
0.62
" Three patients experienced grade 3 treatment-related adverse events: pneumonitis related to alectinib, proteinuria related to bevacizumab, and hypertension related to bevacizumab."( Safety and activity of alectinib plus bevacizumab in patients with advanced ALK-rearranged non-small-cell lung cancer: a phase I/II study.
Azzoli, CG; Dagogo-Jack, I; Gainor, JF; Kennedy, E; Kuberski, H; Lennes, I; Lin, JJ; Muzikansky, A; Sequist, LV; Shaw, AT; Stober, LL; Wanat, AC, 2022
)
0.72
" There were adverse events in a quarter of the patients; only four were severe and led to treatment discontinuation."( Efficacy and safety of tofacitinib in the treatment of ulcerative colitis: real-life experience in Andalusia.
Argüelles Arias, F; Fernández Cano, MC; Gallardo Sánchez, F; González García, J; Hernández Martínez, A; Lázaro Sáez, M; Marín Pedrosa, S; Martín Rodríguez, MDM; Navajas Hernández, P; Núñez Ortiz, A; Olmedo Martín, R; Vázquez Morón, JM, 2022
)
0.72
" In total, 45 treatment-emergent adverse events (TEAEs) were reported; most (91%) were transient and mild in intensity."( Pharmacokinetics, pharmacodynamics and safety assessment of multiple doses of soticlestat in healthy volunteers.
Affinito, J; Chen, G; Cwik, M; Faessel, HM; Merlo Pich, E; Wang, S, 2022
)
0.72
" The discharge time, consumption of propofol and opioid, adverse events, diagnostic accuracy, and sensitivity and specificity for malignancy, were compared."( Efficacy and safety of remifentanil for endoscopic ultrasound-guided tissue acquisition: a single center retrospective study.
Huang, CH; Huang, HH; Lin, PL; Lin, YJ; Wang, YC, 2022
)
0.72
" The consumption of propofol, adverse events, diagnostic accuracy, sensitivity, and specificity for malignancy in the alfentanil group were not significantly different from those in the remifentanil group."( Efficacy and safety of remifentanil for endoscopic ultrasound-guided tissue acquisition: a single center retrospective study.
Huang, CH; Huang, HH; Lin, PL; Lin, YJ; Wang, YC, 2022
)
0.72
" Tofacitinib, 10 mg was well-tolerated and was devoid of any serious adverse event."( An Evaluation of Efficacy and Safety of Tofacitinib, A JAK Inhibitor in the Management of Hospitalized Patients with Mild to Moderate COVID-19 - An Open-Label Randomized Controlled Study.
Cs, G; Es, SS; M, G; Murugesan, H; Nasreen, HS; Ravi, S; Santhanam, S, 2022
)
0.72
"05) in outcomes of adverse events between atogepant and placebo."( The efficacy and safety of atogepant for the prophylactic treatment of migraine: evidence from randomized controlled trials.
Dai, Q; Meng, J; Tao, X; Wang, W; Wang, Z; Yan, Z; Zhou, Q, 2022
)
0.72
" The outcomes of the meta-analysis included cognitive function, global assessment, and the incidence of adverse events and serious adverse events."( Compared of efficacy and safety of high-dose donepezil vs standard-dose donepezil among elderly patients with Alzheimer's disease: a systematic review and meta-analysis.
Han, Y; Liu, H; Liu, Y; Wang, H; Zhao, J; Zong, Y, 2022
)
0.72
" The primary endpoints were change in HbA1c versus baseline, and the incidence of gastrointestinal adverse events (AEs)."( Efficacy and safety of alogliptin versus acarbose in Chinese type 2 diabetes patients with high cardiovascular risk or coronary heart disease treated with aspirin and inadequately controlled with metformin monotherapy or drug-naive: A multicentre, randomi
Gao, B; Gao, W; Ji, Q; Wan, H; Xu, F; Zhang, X; Zhou, R, 2022
)
0.72
" Pruritus, number, diameter, duration and frequency of wheals, and adverse reactions were assessed."( Efficacy and safety of ebastine dose escalation in chronic urticaria: A prospective study.
Chen, Q; Hao, F; Li, S; Qian, T; Song, Z; Zhang, D, 2022
)
0.72
" The most common treatment-emergent adverse events were nausea, constipation, and upper respiratory infection."( Atogepant for Migraine Prevention: A Systematic Review of Efficacy and Safety.
Balasundaram, MK; Singh, A, 2022
)
0.72
" Most common (≥20%) all-grade adverse events (AEs) were neutrophil count decreased (46."( Zanubrutinib in relapsed/refractory mantle cell lymphoma: long-term efficacy and safety results from a phase 2 study.
Feng, R; Gao, S; Guo, H; Hu, J; Huang, J; Ji, J; Jin, J; Kim, P; Lv, F; Novotny, W; Song, Y; Wu, B; Xu, W; Yang, H; Yu, Y; Zhang, H; Zhou, J; Zhou, K; Zhou, L; Zhu, J; Zou, D, 2022
)
0.72
"The increasing indications and addition of newer agents to clinical practice and emergence of BTK inhibitor-related cardiac adverse events have complicated the management decisions for utilization of this class of therapy."( Cardiotoxicity of BTK inhibitors: ibrutinib and beyond.
Awan, FT; Christensen, BW; Zaha, VG, 2022
)
0.72
"The newer BTK inhibitor acalabrutinib represents a new standard of care in front-line chronic lymphocytic leukemia (CLL) given the results of the ELEVATE-RR trial demonstrating comparable efficacy and a more favorable toxicity profile especially with regard to cardiac adverse events as compared to ibrutinib."( Cardiotoxicity of BTK inhibitors: ibrutinib and beyond.
Awan, FT; Christensen, BW; Zaha, VG, 2022
)
0.72
" Moreover, incidence of adverse events, changes in endocrine and metabolic profiles, renal, hepatic and sexual functions and extrapyramidal symptoms will be strictly monitored and recorded."( Effectiveness and safety of blonanserin for improving social and cognitive functions in patients with first-episode schizophrenia: a study protocol for a prospective, multicentre, single-arm clinical trial.
Bo, Q; Deng, H; Hu, S; Inoue, Y; Lei, L; Liu, Z; Pu, C; Sheng, J; Wang, L; Wu, B; Yang, F; Yu, X, 2022
)
0.72
" We report detailed analyses of adverse events of clinical interest (AECIs) in VISION, including edema, a class effect of MET inhibitors."( Safety of Tepotinib in Patients With MET Exon 14 Skipping NSCLC and Recommendations for Management.
Baijal, S; Berghoff, K; Britschgi, C; Cortot, AB; Felip, E; Griesinger, F; Jr, GC; Le, X; Melosky, B; Otto, G; Paik, PK; Park, K; Sakai, H; Sedova, M; Smit, EF; Veillon, R; Wu, YL, 2022
)
0.72
" We investigated the incidence of serious adverse events (SAEs) in patients with UC using tofacitinib from the National Health Insurance Service database."( The Comparative Risk of Serious Adverse Events With Tofacitinib and TNF Inhibitors in Patients With Ulcerative Colitis: The Korean Experience as Revealed by a National Database.
Jung, SH; Seo, GH, 2022
)
0.72
" The 28-day toxicity study highlighted the tolerability of repeated dose administration without adverse effects."( Sex-divergent expression of cytochrome P450 and SIRTUIN 1-7 proteins in toxicity evaluation of a benzimidazole-derived epigenetic modulator in mice.
Falasca, M; Kaur, G; Lee, YT; Mok, PY; Oon, CE; Sreenivasan, S; Tan, YJ, 2022
)
0.72
" Safety was assessed according to adverse events, laboratory tests, vital signs, body weight, and 12-lead electrocardiogram."( Efficacy and Safety of Difelikefalin in Japanese Patients With Moderate to Severe Pruritus Receiving Hemodialysis: A Randomized Clinical Trial.
Gejyo, F; Narita, I; Okamura, S; Oya, N; Takahashi, N; Tsubakihara, Y; Uchiyama, T, 2022
)
0.72
" Side-effect prevalence was higher in the LEF group (11 (31."( Efficacy and safety of tofacitinib versus leflunomide with glucocorticoids treatment in Takayasu arteritis: A prospective study.
Chen, H; Dai, X; Ding, Z; Ji, Z; Jiang, L; Jin, X; Kong, X; Ma, L; Wang, J; Wu, S, 2022
)
0.72
" We retrospectively analysed records (demographic and clinical information, haematology and biochemistry, adverse events) of patients prescribed generic tofacitinib from a single centre in Mumbai, India."( Real-world evidence of the effectiveness and safety of generic tofacitinib in rheumatoid arthritis patients: a retrospective, single-centre analysis from Western India.
Amin, S; Khenat, A; Malandkar, M; Phatak, S, 2022
)
0.72
" The incidence of treatment-related adverse events (AEs) was also assessed."( The efficacy and safety of tofacitinib, peficitinib, solcitinib, baricitinib, abrocitinib and deucravacitinib in plaque psoriasis - A network meta-analysis.
Guo, L; Jiang, X; Wang, L; Zhang, L, 2022
)
0.72
" Common nonhematologic adverse events were fatigue (56%), nausea (53%), anorexia (41%), and diarrhea (41%) and were mostly low grade."( Selinexor Combined with Ibrutinib Demonstrates Tolerability and Safety in Advanced B-Cell Malignancies: A Phase I Study.
Baker, S; Bhat, S; Byrd, JC; Canfield, D; Cempre, CB; Fu, Q; Hu, B; Huang, Y; Jaglowski, SM; Lapalombella, R; Lockman, H; Rogers, KA; Ruppert, AS; Shah, H; Stephens, DM; Vadeboncoeur, R; Walker, JS; Woyach, JA, 2022
)
0.72
" One tool for this combat is repellents; however, these products are composed of different toxic agents."( Use of 2D and co-culture cell models to assess the toxicity of zein nanoparticles loading insect repellents icaridin and geraniol.
Abrantes, DC; Bilesky-José, N; Fraceto, LF; Germano-Costa, T; Guilger-Casagrande, M; Lima, R; Maruyama, CR; Oliveira, JL; Pasquoto-Stigliani, T; Rogério, CB, 2022
)
0.72
" LC-MS/MS analysis revealed that the reduction in the magnitude of adverse effects was the result of the ability to release HF from the HFm core in a slow and sustained manner."( Halofuginone micelle nanoparticles eradicate Nrf2-activated lung adenocarcinoma without systemic toxicity.
Baird, L; Miyata, K; Naito, M; Panda, H; Saito, R; Suzuki, M; Uruno, A; Wen, H; Yamamoto, M, 2022
)
0.72
" Interstitial lung disease is the most common adverse event leading to discontinuation of alectinib."( Evaluation of Lung Toxicity Related to the Treatment With Alectinib Using a Pharmacovigilance Database.
Sato, J; Shimizu, T; Uchida, M; Wakabayashi, H, 2022
)
0.72
" These results will be useful for monitoring adverse events associated with the use of alectinib."( Evaluation of Lung Toxicity Related to the Treatment With Alectinib Using a Pharmacovigilance Database.
Sato, J; Shimizu, T; Uchida, M; Wakabayashi, H, 2022
)
0.72
" This study evaluated the risk of serious adverse events (SAEs) associated with individual ChEIs in older adults with dementia and also examined sex-based and dose-based effects on this risk."( Risk of Serious Adverse Events Associated With Individual Cholinesterase Inhibitors Use in Older Adults With Dementia: A Population-Based Cohort Study.
Aparasu, RR; Chatterjee, S; Chen, H; Johnson, ML; Masurkar, PP; Sherer, JT, 2022
)
0.72
" Proportions and IRs (unique patients with events/100 patient-years) were calculated for adverse events (AEs) of special interest."( Safety and efficacy of long-term tofacitinib treatment in East Asian patients with ulcerative colitis in OCTAVE Open.
Arai, S; Hibi, T; Hisamatsu, T; Hoshi, M; Kim, HJ; Matsuoka, K; Shi, N; Tabira, J; Toyoizumi, S; Woo, JS; Ye, BD; Yuasa, H, 2022
)
0.72
"In controlled clinical trials, compared with placebo, a significantly greater proportion of participants using lasmiditan to treat a migraine attack achieved 2-h pain freedom (PF) and experienced ≥ 1 treatment-emergent adverse event (TEAE)."( The Association Between the Occurrence of Common Treatment-Emergent Adverse Events and Efficacy Outcomes After Lasmiditan Treatment of a Single Migraine Attack: Secondary Analyses from Four Pooled Randomized Clinical Trials.
Dong, Y; Doty, EG; Hake, AM; Hauck, PM; Komori, M; Krege, JH; Lipton, RB, 2022
)
0.72
" Adverse events occurred in 74."( Efficacy and safety of ibrutinib in relapsed/refractory CLL and SLL in Japan: a post-marketing surveillance.
Akizuki, R; Fujino, A; Nomura, F; Omi, A; Tsujioka, S, 2022
)
0.72
" Safety assessments included incidence of treatment-emergent adverse events (TEAEs)."( A phase 2, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of soticlestat as adjunctive therapy in pediatric patients with Dravet syndrome or Lennox-Gastaut syndrome (ELEKTRA).
Arkilo, D; Asgharnejad, M; Dlugos, D; Hahn, CD; Hsiao, S; Jiang, Y; Villanueva, V; Zolnowska, M, 2022
)
0.72
" Toxic effects of the combination of ibrutinib and cetuximab have been reported in a patient with metastatic CRC."( Ibrutinib and panitumumab used in combination safely in a patient with metachronous colorectal cancer and chronic lymphocytic leukemia.
Araz, M; Artaç, M; Çeneli, Ö; Karaağaç, M; Karakurt Eryilmaz, M; Korkmaz, M, 2022
)
0.72
"This article provides nurse-specific recommendations for identification and management of tepotinib adverse events (AEs)."( Tepotinib: Management of Adverse Events in Patients With MET Exon 14 Skipping Non-Small Cell Lung Cancer.
Ahn, L; Alexander, T; Berghoff, K; Lemmens, L; Vlassak, S, 2022
)
0.72
" The incidence of treatment-emergent adverse events (TEAEs), their severity, and incidence by treated attacks for frequently reported TEAEs (≥ 5%) were evaluated."( Safety Findings in Lasmiditan as a Novel Acute Treatment of Migraine in Chinese Patients: A Post Hoc Analysis of the Randomized Controlled Phase 3 CENTURION Trial.
Dong, Z; Ji, F; Liu, H; Luo, G; Pan, X; Xu, Y; Yang, X; Yu, S; Zhong, S; Zhou, J, 2022
)
0.72
" No deaths and no study drug-related treatment emergent serious adverse events (TESAEs) were reported."( Safety Findings in Lasmiditan as a Novel Acute Treatment of Migraine in Chinese Patients: A Post Hoc Analysis of the Randomized Controlled Phase 3 CENTURION Trial.
Dong, Z; Ji, F; Liu, H; Luo, G; Pan, X; Xu, Y; Yang, X; Yu, S; Zhong, S; Zhou, J, 2022
)
0.72
" We also synopsize and discuss the cardiovascular adverse effects related to other more selective BTK inhibitors, which may guide the selection of appropriate BTK inhibitors."( Ibrutinib-Associated Cardiotoxicity: From the Pharmaceutical to the Clinical.
Dong, R; Lin, N; Tan, B; Yan, Y; Zeng, X, 2022
)
0.72
" Despite a growing number of studies on its safety and efficacy, there is still a lack of clarity, especially in the pediatric population, in treatment considerations such as proper dosage, treatment duration, side-effect profile, and therapeutic strategies to guide clinicians."( Efficacy and safety of tofacitinib for treatment of alopecia areata in children: A systematic review and meta-analysis.
Barough, MS; Behrangi, E; Goodarzi, A; Hejazi, P; Khoramdad, M; Koltapeh, MP, 2022
)
0.72
"5-15 mg daily (especially 5 mg twice daily) oral formulation or 2% topical solution can be regarded as a viable alternative or adjunct to the conventional treatment options for moderate to severe forms of alopecia areata in children owing to its acceptable efficacy and side-effect profile."( Efficacy and safety of tofacitinib for treatment of alopecia areata in children: A systematic review and meta-analysis.
Barough, MS; Behrangi, E; Goodarzi, A; Hejazi, P; Khoramdad, M; Koltapeh, MP, 2022
)
0.72
" However, drug-induced pneumonitis is an uncommon but threatening adverse effect found in patients treated with both capmatinib and tepotinib."( Safety of Tepotinib Challenge after Capmatinib-Induced Pneumonitis in a Patient with Non-Small Cell Lung Cancer Harboring MET Exon 14 Skipping Mutation: A Case Report.
Chang, JW; Tseng, LW; Wu, CE, 2022
)
0.72
" This analysis assessed age as a risk factor for adverse events of special interest (AESI) in the tofacitinib UC clinical program."( Assessment of Safety and Efficacy of Tofacitinib, Stratified by Age, in Patients from the Ulcerative Colitis Clinical Program.
Bressler, B; Francisconi, C; Jones, T; Judd, DT; Lawendy, N; Lichtenstein, GR; Loftus, EV; Salese, L; Sawyerr, G; Shi, H; Su, C; Vermeire, S, 2023
)
0.91
"Age was assessed as a risk factor for adverse events of special interest in the tofacitinib ulcerative colitis clinical program."( Assessment of Safety and Efficacy of Tofacitinib, Stratified by Age, in Patients from the Ulcerative Colitis Clinical Program.
Bressler, B; Francisconi, C; Jones, T; Judd, DT; Lawendy, N; Lichtenstein, GR; Loftus, EV; Salese, L; Sawyerr, G; Shi, H; Su, C; Vermeire, S, 2023
)
0.91
"Ibrutinib, a first-class Bruton tyrosine kinase inhibitor, is known to be associated with adverse bleeding events and has been recently approved for the treatment of relapse Waldenström macroglobulinemia (WM)."( Successful and safe response to ibrutinib alone in treating relapsed Waldenström macrogobulinemia and related acquired von Willebrand syndrome: an option to consider.
Bauters, A; Butelet, A; Chauvet, P; de Charette, M; Dupont, A; Jeanpierre, E; Nudel, M; Poulain, S; Srour, M; Susen, S, 2022
)
0.72
"One-third of patients with UC treated with tofacitinib achieved clinical remission with few serious adverse events."( REMIT-UC: Real-World Effectiveness and Safety of Tofacitinib for Moderate-to-Severely Active Ulcerative Colitis: A Canadian IBD Research Consortium Multicenter National Cohort Study.
Bessissow, T; Bressler, B; Jairath, V; Khandelwal, Y; Loomes, D; Ma, C; Murthy, SK; Narula, N; Panaccione, R; Peerani, F; Reise-Filteau, M; Sedano, R; Starkey, SY; Tsai, C; Wong, ECL; Xiao, Y, 2023
)
0.91
" In SH-SY5Y neuroblastoma cell lines they exhibited a neuroprotective effect against rotenone- and NMDA-mediated toxic insults."( Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents.
Bedeschi, M; Collina, S; Denora, N; Dondio, G; Franchini, S; Linciano, P; Marino, N; Marsala, A; Miserocchi, G; Peviani, M; Rossi, D; Rossino, G; Sorbi, C; Tesei, A, 2023
)
0.91
" Incidence of adverse events (AEs)/serious AEs (M0-3): 68."( Efficacy and safety of tofacitinib in Chinese patients with active psoriatic arthritis: a phase 3, randomised, double-blind, placebo-controlled study.
Dina, O; Gunay, LM; Hu, J; Jiang, Z; Kanik, K; Kinch, C; Leng, X; Li, J; Lin, W; Liu, J; Liu, S; Liu, Y; Tan, W; Wan, W; Wang, C; Xu, J; Zeng, X; Zhang, Z, 2023
)
0.91
" Data on efficacy and safety are presented with the main focus on treatment-related hypertension, a well-known adverse effect (AE) of these TKIs."( Cabozantinib, Vandetanib, Pralsetinib and Selpercatinib as Treatment for Progressed Medullary Thyroid Cancer with a Main Focus on Hypertension as Adverse Effect.
Grimm, D; Højer Wang, L; Infanger, M; Kreissl, MC; Wehland, M; Wise, PM, 2023
)
0.91
"5, or 5 mg/kg of AdipoRon without adverse effects."( The Safety of Adiponectin Receptor Agonist AdipoRon in a Rabbit Model of Arthrofibrosis.
Abdel, MP; Berry, DJ; Bettencourt, JW; Carstens, MF; Dudakovic, A; Gow, C; Limberg, AK; Morrey, ME; Payne, AN; Salmons, HI; Sanchez-Sotelo, J, 2023
)
0.91
"In this study, we fill this gap in knowledge by updating the safety profile of ubrogepant and rimegepant via disproportionality analysis in the Food and Drug Administration (FDA) Adverse Event Reporting System (FAERS), a US-based database registering spontaneous reports."( Ubrogepant and rimegepant: signal detection using spontaneous reports of adverse events from the Food and Drug Administration Adverse Event Reporting System.
Battini, V; Carnovale, C; Clementi, E; Sessa, M,
)
0.13
" Ten disproportionality signals for ubrogepant and 25 disproportionality signals for rimegepant were identified; these were mostly related to psychiatric, neurological, gastrointestinal, skin, vascular, and infectious type of adverse events."( Ubrogepant and rimegepant: signal detection using spontaneous reports of adverse events from the Food and Drug Administration Adverse Event Reporting System.
Battini, V; Carnovale, C; Clementi, E; Sessa, M,
)
0.13
" The incidence of adverse events at application site in the continuation group over 52 weeks was 56."( Efficacy and Safety of a Transdermal Donepezil Patch in Patients with Mild to Moderate Alzheimer's Disease: Open-Label, Extension Study.
Aoki, H; Ishikawa, I; Kikuchi, T; Kim, R; Nakamura, Y; Nishiyama, K; Omori, T, 2023
)
0.91
" No severe adverse events were observed in either group."( Efficacy and Safety of Tofacitinib in Patients with Polymyalgia Rheumatica (EAST PMR): An open-label randomized controlled trial.
Chen, C; Chen, W; Jiang, M; Liang, J; Lin, J; Ma, X; Ren, C; Sun, C; Sun, Y; Wu, J; Xiao, L; Xu, B; Xu, D; Yang, F; Ye, Z; Yu, Y, 2023
)
0.91
"Remifentanil appears to be effective and safe in the short term in preterm and full-term neonates."( Fetal, Preterm, and Term Neonate Exposure to Remifentanil: A Systematic Review of Efficacy and Safety.
Aubelle, MS; Chollat, C; Maroni, A, 2023
)
0.91
" However, as they are associated with many adverse events (AEs), it is important to be aware of their safety and toxicity profiles."( Safety of PARP inhibitors as maintenance therapy in ovarian cancer.
Casartelli, C; Cecere, SC; Forte, M; Pignata, S; Pisano, C,
)
0.13
"4% (6/64) discontinued due to adverse events."( Long-Term Safety, Tolerability, and Efficacy of a Transdermal Donepezil Patch in Patients with Severe Alzheimer's Disease.
Aoki, H; Ishikawa, I; Kikuchi, T; Kim, R; Nakamura, Y; Narita, K; Nishiyama, K, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" The pharmacokinetic parameters were not found to be dose dependent in the range investigated, but it was not possible to decide whether the bioavailability was dependent on the dose."( Pharmacokinetics of femoxetine in man.
Bechgaard, E; Christensen, JA; Larsson, H; Lund, J; Molander, L, 1979
)
0.26
" The pharmacokinetic studies revealed a dose dependent systemic availability, a rather slow elimination (t1-z2 = approximately 16 hrs), a good fit to one compartment open model, and an almost complete metabolism of the substance."( Paroxetine: pharmacokinetics, tolerance and depletion of blood 5-HT in man.
Bechgaard, E; Christensen, JA; Fabricius, J; Lomholt, B; Lund, J, 1979
)
0.26
"A pharmacokinetic study of the antidiarrheal agent loperamide hydrochloride (Imodium) was conducted in six male subjects."( Human pharmacokinetics and comparative bioavailability of loperamide hydrochloride.
Fuller, BL; Killinger, JM; Weintraub, HS, 1979
)
0.26
" A comparison of the pharmacokinetic and metabolic behaviour of piprozoline in rats, dogs and humans showed that it was similar in all three species."( [Metabolism and pharmacokinetics of piprozoline in the rat, dog and man. 1. Studies with the radioactively-labeled substance].
Bode, R; Hodenberg, AV; Poisson, A; Schauerte, E; Vollmer, KO, 1977
)
0.26
" In all cases, metabolite I was eliminated from the plasma with a half-life of approx."( [Metabolism and pharmacokinetics of piprozoline in rat, dog and man. 3rd communication: Determination of piprozoline and metabolite I in plasma and urine (author's transl)].
Ehret, I; Gladigau, V, 1977
)
0.26
" There are marked pharmacokinetic differences between F and M, probably related to their physical properties."( Pharmacokinetics of flavoxate in rats.
Cova, A; Magistretti, MJ; Setnikar, I, 1975
)
0.25
"This work deals with the pharmacodynamic problem of relating a drug effect E(t) to an observable pharmacokinetic (PK) predictor variable r(t), which may be a venous and/or arterial drug level, some other PK variable, or a drug infusion scheme."( Pharmacodynamic system analysis of the biophase level predictor and the transduction function.
Modi, NB; Veng-Pedersen, P, 1992
)
0.28
" Based on pharmacokinetic considerations, the dosage of pirmenol is unlikely to differ in young and elderly subjects."( Pharmacokinetics of pirmenol in young and elderly subjects.
Beasley, M; Bland, R; Campbell, AJ; Edwards, IR; Ferry, DG; Gazeley, L, 1992
)
0.28
" These results regarding the pharmacokinetic parameters of BM 12."( Pharmacokinetics of the organic nitrates trans-2-amino-2-methyl-N-(4- nitroxycyclohexylmethyl)-propionamide in dogs, and of 4-(2-nitroxyethyl)-piperidine in dogs and in monkeys.
Bartsch, W; Neidlein, R; Pressmar, F; Strein, K, 1992
)
0.28
" The plasma elimination half-life of heptacaine was 133 min and its biological availability of 52% was comparable to other agents of the class."( Pharmacokinetics of heptacaine, a novel potent local anaesthetic agent, after rectal administration to rats.
Divisová, D; Durisová, M; Faberová, V; Trnovec, T,
)
0.13
"The pharmacokinetic properties of the newer specific serotonin (5-HT) reuptake inhibitors are reviewed."( Pharmacokinetics of the selective serotonin reuptake inhibitors.
DeVane, CL, 1992
)
0.28
" In nearly all extensive metabolizers the concentration-dose data were best described by a pharmacokinetic model assuming elimination by at least two kinetically distinct processes, one a high-affinity saturable process and one a low-affinity linear process."( Pharmacokinetics of the selective serotonin reuptake inhibitor paroxetine: nonlinearity and relation to the sparteine oxidation polymorphism.
Brøsen, K; Gram, LF; Sindrup, SH, 1992
)
0.28
"The pharmacokinetic parameters of oral diphemanil methylsulphate have been evaluated in six healthy male volunteers."( Pharmacokinetics of diphemanil methylsulphate in healthy subjects.
d'Athis, P; Olive, G; Pello, JY; Pons, G; Rey, E; Vidal, AM, 1992
)
0.28
" Mean pirmenol concentration-time curves and pharmacokinetic parameters, including elimination rate constant, were not significantly altered by concomitant administration of cimetidine."( Effect of cimetidine administration on the pharmacokinetics of pirmenol.
Bockbrader, HN; Cetnarowski-Cropp, AB; Chang, T; Goldfarb, AL; Lebsack, ME; Radulovic, LL; Sedman, AJ; Stringer, KA, 1992
)
0.28
" The pharmacodynamic effect of cisapride was measured by means of radionuclide gastric emptying."( Pharmacokinetics and pharmacodynamics of cisapride in patients undergoing hemodialysis.
Bares, R; Dakshinamurty, KV; Gladziwa, U; Ittel, TH; Klotz, U; Seiler, KU; Sieberth, HG, 1991
)
0.28
" Its pharmacokinetic parameters were obtained from the rabbit plasma level-time curve measured."( [RP-HPLC determination of 1-(p-methylphenyl-2-(2-piperidinoacetyl- 1,2,3,4-tetrahydroisoquinoline hydrochloride in rabbit plasma and its pharmacokinetic parameters].
Cheng, WB; Qin, ZL; Xie, XY; Zhou, ZS, 1991
)
0.28
" An earlier tmax and a higher Cmax and AUC were observed in the subjects who received piperine and propranolol."( Effect of piperine on bioavailability and pharmacokinetics of propranolol and theophylline in healthy volunteers.
Bano, G; Bedi, KL; Johri, RK; Raina, RK; Sharma, SC; Zutshi, U, 1991
)
0.28
" The regular hemodialysis sessions every 2-3 days did not affect the elimination rate of ritanserin, as the terminal half-life in these patients (39 +/- 23 hr) is similar to that in healthy volunteers (41 +/- 14 hr)."( Pharmacokinetics of ritanserin in patients undergoing hemodialysis.
Heykants, J; Huang, ML; Koch, S; Kokot, F; Kuska, J; Van Peer, A; Zazgornik, J, 1991
)
0.28
" The time courses of biperiden concentration in plasma, brain, and fat were simulated using a physiological pharmacokinetic model."( Effect of fat tissue volume on the distribution kinetics of biperiden as a function of age in rats.
Ichimura, F; Nakashima, E; Yokogawa, K,
)
0.13
" Gastric secretion inhibition over the 90 min of IGT correlated with peak concentration exclusively for the subpopulation with peak occurrence at T 150."( [Plasma pharmacokinetics of roxatidine in the healthy man: correlation with gastric antisecretory effect].
Bonfils, S; Chen, WW; Kolsky, H; Lewin, MJ, 1990
)
0.28
" We observed great interindividual differences in the pharmacokinetic behaviour."( [Pharmacokinetics (rats and rabbits) of N-methyl-4- piperidinylbenzilate (Po)3].
Gabrio, T; Göber, B; Höhn, H, 1990
)
0.28
" Loratadine was rapidly absorbed and the decline of plasma concentrations after attainment of the Cmax was biexponential in all subjects."( Pharmacokinetics of loratadine in patients with renal insufficiency.
Halstenson, CE; Hilbert, J; Matzke, GR; Opsahl, JA; Perentesis, G; Radwanski, E; Zampaglione, N, 1990
)
0.28
" Also, steady-state pharmacokinetic parameters are not predictable from single-dose data."( A review of the metabolism and pharmacokinetics of paroxetine in man.
Greb, WH; Haddock, RE; Kaye, CM; Langley, PF; Mellows, G; Tasker, TC; Zussman, BD, 1989
)
0.28
"To evaluate the pharmacokinetic properties, efficacy, and tolerability of paroxetine in elderly depressed patients, a clinical study was set up--initially at Aalborg Psychiatric Hospital in Denmark, and subsequently at the University Hospital in Linköping, Sweden."( Paroxetine: pharmacokinetic and antidepressant effect in the elderly.
Fjord-Larsen, T; Lundmark, J; Manniche, PM; Mengel, H; Møller-Nielsen, EM; Pauser, H; Scheel Thomsen, I; Wålinder, J, 1989
)
0.28
" After pretreatment with cimetidine, the plasma clearances (CL) of AP and TMO were significantly lower and the elimination half-life (t1/2) of AP was significantly increased."( The effect of roxatidine acetate and cimetidine on hepatic drug clearance assessed by simultaneous administration of three model substrates.
Nakamura, K; Tanaka, E, 1989
)
0.28
"The effects of a new H2-receptor antagonist, roxatidine acetate, have been investigated in both clinical and pharmacodynamic trials in Europe and the United States."( Safety and efficacy of roxatidine acetate. Evidence from pharmacodynamic and clinical trials.
Bender, W; Labs, R; Merki, HS, 1989
)
0.28
"This article reviews the published and unpublished results of pharmacokinetic studies with roxatidine acetate in healthy volunteers of different ethnic origins, patients with various degrees of renal impairment, patients on maintenance hemodialysis, lactating women, and elderly patients."( Pharmacokinetic characteristics of roxatidine.
Bender, W; Brockmeier, D, 1989
)
0.28
" The peak concentrations of vadocaine were achieved at 1 h both after the tablet and the solution and there were no statistically significant differences in serum concentrations or in pharmacokinetic parameters."( The single dose and steady-state pharmacokinetics of a vadocaine tablet in healthy human volunteers.
Hänninen, U; Karttunen, P; Mykkänen, M; Silvasti, M; Tukiainen, H; Välttilä, S, 1989
)
0.28
"Biotransformation and Pharmacokinetics of Bamipine in Rats/2nd Communication: Pharmacokinetic studies (Part I)."( [Biotransformation and pharmacokinetics of bamipine in rats. 2. Studies of the pharmacokinetics (1.)].
Kleiser, M; Neidlein, VR, 1987
)
0.27
" The pharmacokinetics of carebastine were linear over the dose range studied and the terminal elimination half-life was 10."( The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
Liminana, R; Meredith, PA; Reid, JL; Vincent, J, 1988
)
0.27
" In common with many other prodrugs, the parent substance is not detectable in either plasma or urine and therefore all pharmacokinetic studies have been evaluated using measurements of roxatidine."( Pharmacokinetics of roxatidine in healthy volunteers.
Collins, JD; Pidgen, AW, 1988
)
0.27
" Plasma and urine samples were collected throughout the study for the pharmacokinetic assessment."( The pharmacodynamics and pharmacokinetics of multiple doses of the new H2-receptor antagonist, roxatidine acetate, in healthy men.
Ho, I; Lassman, HB; Puri, SK; Sabo, R; Scheffler, MR, 1988
)
0.27
" During steady-state therapy the elimination half-life (24."( Blood pressure reduction and pharmacokinetics of ketanserin in hypertensive patients.
Hedner, T; Persson, B; Pettersson, A, 1986
)
0.27
" Concentrations of loratadine in the disposition phase were fitted to a biexponential equation and those of descarboethoxyloratadine to either a monoexponential or biexponential equation for pharmacokinetic analysis."( The pharmacokinetics of loratadine in normal geriatric volunteers.
Hilbert, J; Moritzen, V; Parks, A; Perentesis, G; Radwanski, E; Symchowicz, S; Zampaglione, N,
)
0.13
" On the other hand, the elimination half-life of antiarrhythmic agents that have a large volume of distribution and are highly cleared by the liver may be twice as long in patients with CHF compared with normal subjects."( Effects of congestive heart failure on the pharmacokinetics and pharmacodynamics of antiarrhythmic agents.
Echt, DS; Roden, DM; Woosley, RL, 1986
)
0.27
"Lorcainide, a new antiarrhythmic agent currently undergoing clinical trial, has been pentadeuterated and the usefulness of this labelled compound in pharmacokinetic and metabolism studies has been investigated in dogs."( The use and limitations of deuterated lorcainide in metabolism and pharmacokinetic studies.
Gelijkens, CF; Heykants, J; Knaeps, A; Lenoir, H; Van Peer, A; Woestenborghs, R, 1985
)
0.27
" Individual plasma level-time curves fitted to an open three compartment model and a half-life of 17."( Bioavailability and pharmacokinetics of ketanserin in elderly subjects.
Kurowski, M, 1985
)
0.27
" The author summarizes the hemodynamic and pharmacokinetic studies of pirmenol noting that its effects are relatively independent of potassium concentration."( Clinical pharmacology and pharmacokinetics of pirmenol.
Reiter, MJ, 1988
)
0.27
" This method was used to establish the pharmacokinetic profiles of I and PK following a single oral administration of I (100 mg) in 8 healthy volunteers."( HPLC determination of indalpine and its major metabolite in human plasma and a pharmacokinetic application.
Caillé, G; Demontigny, C; Tawashi, M; Toupin, L; Vézina, M,
)
0.13
" The terminal plasma half-life of cisapride was about 1-2 h in the rat and about 4-10 h in the rabbit and dog."( Pharmacokinetics and tissue distribution of the new gastrokinetic agent cisapride in rat, rabbit and dog.
Geerts, R; Hendriks, R; Heykants, J; Michiels, M; Monbaliu, J; Woestenborghs, R, 1987
)
0.27
" The number of compartments in the preferred pharmacokinetic model of biperiden changed from three (for normal rats) to two (for fasted rats)."( Effects of fasting on biperiden pharmacokinetics in the rat.
Hashimoto, T; Ichimura, F; Nakashima, E; Tsuji, A; Yamana, T; Yokogawa, K, 1987
)
0.27
"The pharmacodynamic and kinetic profiles of two oral biperiden formulations (tablet with instant-release and sugar-coated tablet with slow-release) were studied in a total of 12 healthy subjects after the administration of a 4 mg dose and compared in part to placebo."( Pharmacokinetic-dynamic study on different oral biperiden formulations in volunteers.
Brode, E; Crema, A; Greger, G; Grimaldi, R; Hollmann, M; Müller-Peltzer, H; Perucca, E, 1987
)
0.27
"After oral application pharmacokinetic parameters of N-phenyl-N-benzyl-4-amino-1-methylpiperidin (bamipine) were investigated."( [Biotransformation and pharmacokinetics of bamipine in rats. 2. Pharmacokinetics (P 2)].
Kleiser, M; Neidlein, R, 1987
)
0.27
" The mean half-life of elimination was 10."( Pharmacodynamics and pharmacokinetics of oral pirmenol.
Ellenbogen, KA; Kates, RE; McCarthy, EA; Pritchett, EL; Roark, SF; Sintetos, AL; Smith, MS; Smith, WM, 1987
)
0.27
" An open two-compartment pharmacokinetic model was conferred to the data."( Pharmacokinetics of the new local anaesthetic N-[2-(2-Heptyloxyphenylcarbamoyloxy)ethyl]piperidinium chloride in rats and mice.
Bezek, S; Durisovă, M; Kállay, Z; Scasnár, V; Trnovec, T, 1987
)
0.27
"The influence of cardiac function as measured by the left ventricular ejection fraction on the pharmacokinetic variables of a new antiarrhythmic drug, lorcainide, was investigated in 20 cardiac patients."( Pharmacokinetic implications of lorcainide therapy in patients with normal and depressed cardiac function.
Fraker, TD; Somani, P; Temesy-Armos, PN, 1987
)
0.27
" It can be given either intravenously or orally and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration."( Flecainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Heel, RC; Holmes, B, 1985
)
0.27
" Some pharmacokinetic parameters (e."( Pharmacokinetics of 3H-pipethiaden after single oral and intravenous administration in rats.
Franc, Z; Lapka, R; Smolik, S, 1985
)
0.27
" However the plasma elimination of flecainide was found to be inversely proportional to urinary pH and the volunteers' mean elimination half-life ranged between 10."( Flecainide pharmacokinetics in healthy volunteers: the influence of urinary pH.
Johnston, A; Turner, P; Warrington, S, 1985
)
0.27
" Plasma concentration declined with a mean terminal half-life of 15."( Pharmacokinetics and pharmacodynamics of the 5-HT2 receptor antagonist ketanserin in man.
Jähnchen, E; Kirch, W; Meinertz, T; Mosler, A; Trenk, D,
)
0.13
" It can be given either intravenously or orally, and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration."( Lorcainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Brogden, RN; Eiriksson, Ce, 1984
)
0.27
"This article reviews clinical pharmacokinetic data on 8 new antiarrhythmic agents."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
"We have examined the analysis of pharmacodynamic data in normal subjects receiving propranolol, flecainide or the two together."( Application of second-order polynomial equations to the study of pharmacodynamic interactions: the effect of flecainide acetate and propranolol on cardiac output and vascular resistance.
Berry, DA; Borrell, G; Holtzman, JL; Kvam, DC; Mottonen, L, 1984
)
0.27
" The elimination half-life of femoxetine was within the normal limits in most of the patients."( Femoxetine clearance in patients with liver cirrhosis.
Hansen, BA; Keiding, S; Lund, J; Mengel, H, 1984
)
0.27
" The terminal elimination half-life (term."( Pharmacokinetics of ketanserin in man.
Klotz, U; Okonkwo, PO; Reimann, IW, 1983
)
0.27
" Blood, plasma and free drug concentrations declined biexponentially after cessation of a 150-mg infusion (n = 4), with a terminal half-life of 7-9."( Pirmenol, a new antiarrhythmic agent: initial study of efficacy, safety and pharmacokinetics.
Baker, JT; Hammill, SC; Hindman, MC; Pritchett, EL; Routledge, PA; Shand, DG, 1982
)
0.26
" After a rapid initial decrease radioactivity was eliminated with a half-life of 8-10 hours."( On the pharmacokinetics of domperidone in animals and man II. Tissue distribution, placental and milk transfer of domperidone in the Wistar rat.
Hendriks, R; Heykants, J; Michiels, M, 1981
)
0.26
" Following are the mean pharmacokinetics of risperidone and risperidone + 9-OH-risperidone: area under the plasma concentration curve (AUC) from 0 to 96 hours; 278."( Pharmacokinetics of risperidone in chronic schizophrenic patients.
Borison, RL; Diamond, B; Meibach, RC; Pathiraja, A, 1994
)
0.29
" Risperidone can be characterized as a potent D2 antagonist with predominant 5HT2 antagonistic activity and optimal pharmacokinetic properties."( Survey on the pharmacodynamics of the new antipsychotic risperidone.
Awouters, FH; Dugovic, C; Leysen, JE; Meert, TF; Megens, AA; Niemegeers, CJ; Schotte, A, 1994
)
0.29
" Most traditional antipsychotic drugs have similar pharmacokinetic profiles that differ from the newer agents in several key respects."( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs.
DeVane, CL, 1995
)
0.29
" Two studies on iloperidone evaluated its safety and tolerability, made a preliminary pharmacokinetic assessment of single 3- and 5-mg doses, and determined the effect of food on its tolerability and pharmacokinetics in healthy volunteers after single 3-mg doses."( Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic.
Brecher, MB; Chi, E; Grasing, K; Hubbard, JW; Sainati, SM, 1995
)
0.29
" Because of its unique metabolic pathway (among this group of drugs) and rapid clearance, remifentanil represents a new pharmacokinetic class of opioid."( Remifentanil pharmacokinetics and pharmacodynamics. A preliminary appraisal.
Egan, TD, 1995
)
0.29
" The terminal elimination half-life ranged from 50 to 83 min."( Dose and species dependent pharmacokinetics of a novel sigma receptor antagonist, DuP 734.
Kapil, RP; Lam, GN, 1995
)
0.29
" Risperidone half-life was about 3 hours in extensive metabolizers and 22 hours in poor metabolizers."( Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects.
De Coster, R; Heykants, J; Huang, ML; Jansen, AA; Jonkman, JH; Van Peer, A; Visscher, HW; Woestenborghs, R; Zylicz, Z, 1993
)
0.29
" The aim of this study was to characterize in detail the pharmacokinetic profile of remifentanil in healthy male volunteers."( The pharmacokinetics of the new short-acting opioid remifentanil (GI87084B) in healthy adult male volunteers.
Egan, TD; Fiset, P; Hermann, DJ; Lemmens, HJ; Muir, KT; Shafer, SL; Stanski, DR, 1993
)
0.29
" The raw pharmacokinetic data were analyzed using three different parametric compartmental modeling methods (traditional two-stage, naive pooled data, and NONMEM)."( The pharmacokinetics of the new short-acting opioid remifentanil (GI87084B) in healthy adult male volunteers.
Egan, TD; Fiset, P; Hermann, DJ; Lemmens, HJ; Muir, KT; Shafer, SL; Stanski, DR, 1993
)
0.29
" The terminal half-life of remifentanil ranged from 10 to 21 min."( Pharmacokinetics of remifentanil (GI87084B) and its major metabolite (GI90291) in patients undergoing elective inpatient surgery.
Hoke, JF; Hug, CC; Muir, KT; Sebel, PS; Westmoreland, CL, 1993
)
0.29
" The decreased urinary excretion most likely contributed to the prolonged half-life (from 36 hours to 95 hours) and increased area under the plasma concentration-time curve (+56%) in the patients with renal insufficiency as compared with the healthy volunteers."( Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency.
Heykants, J; Huang, ML; Stephen, A; Van Peer, A; Woestenborghs, R; Zazgornik, J, 1993
)
0.29
" The Cmax of carebastine in guinea pigs (2820 ng/ml) was markedly higher than that in rats (311 ng/ml), dogs (465 ng/ml) and monkeys (1036 ng/ml)."( Comparative pharmacokinetics of the histamine H1-receptor antagonist ebastine and its active metabolite carebastine in rats, guinea pigs, dogs and monkeys.
Fujii, T; Matsuda, M; Mizuki, Y; Sakashita, M; Sekine, Y; Yamaguchi, T, 1994
)
0.29
" The Cmax and AUC of carebastine increased in proportion to the dose."( Pharmacokinetics of the H1-receptor antagonist ebastine and its active metabolite carebastine in healthy subjects.
Fujii, T; Hashizume, T; Matsuda, M; Nakashima, M; Sakashita, M; Sekine, Y; Uematsu, T; Yamaguchi, T, 1994
)
0.29
" This assay was used for a pharmacokinetic study in five subjects after administration of a single dose of 60 mg of terfenadine."( A preliminary pharmacokinetic study of the enantiomers of the terfenadine acid metabolite in humans.
Khalil, SK; Surapaneni, S, 1994
)
0.29
" Its pharmacokinetic parameters are known for adults but not for infants."( [Pharmacokinetics of diphemanil methylsulfate in infants].
Chéron, G; d'Athis, P; Olive, G; Pons, G; Rey, E; Vidal, AM, 1994
)
0.29
"The relatively long half-life of diphemanil methylsulfate allows this drug to be given every 8 hours."( [Pharmacokinetics of diphemanil methylsulfate in infants].
Chéron, G; d'Athis, P; Olive, G; Pons, G; Rey, E; Vidal, AM, 1994
)
0.29
" Mean plasma elimination half-life values of carebastine ranged from 10 to 14 hours."( Pharmacokinetics and pharmacodynamics of ebastine in children.
Simons, FE; Simons, KJ; Watson, WT, 1993
)
0.29
" Pharmacokinetic analyses indicate nonlinearity of 349U85 and 661U88, suggestive of saturation of metabolism and large interindividual variability in maximum plasma drug concentration and area under the plasma concentration-time curve."( Pharmacokinetics and pharmacodynamics of a new cardiotonic vasodilator agent, 349U85, in normal subjects.
Brown, AR; Clifton, GD; Fleck, RJ; Harrison, MR; Long, RA; Rolleri, RL; Welch, RM; Weller, S; Wermeling, DP, 1994
)
0.29
" The plasma elimination half-life of the beta-phase (t 1/2 beta) and time to maximum peak plasma concentration (tmax) were significantly longer in the elderly than in the young: t 1/2 beta, 103."( Comparison of the pharmacokinetics of E2020, a new compound for Alzheimer's disease, in healthy young and elderly subjects.
Hasegawa, J; Kamakura, H; Mihara, M; Morishita, N; Ohnishi, A; Tanaka, T; Tomono, Y; Yamazaki, K, 1993
)
0.29
" In man, the di-cationic disobutamide was slowly eliminated with a mean terminal phase half-life of 54 +/- 18 h, a value > 7 times longer than disopyramide."( Importance of pharmacokinetic and physicochemical data in the discovery and development of novel anti-arrhythmic drugs.
Cook, CS; Karim, A; McDonald, SJ, 1993
)
0.29
" Three separate studies were conducted to evaluate the safety and to establish the pharmacokinetic profile of E2020 after oral administration to healthy male subjects."( Pharmacokinetics of E2020, a new compound for Alzheimer's disease, in healthy male volunteers.
Hasegawa, J; Mihara, M; Morishita, N; Ohnishi, A; Shimamura, Y; Tomono, Y; Yamazaki, K, 1993
)
0.29
" The mean pharmacokinetic parameters of oral diphemanil methylsulphate in infants were similar to those in adults."( Pharmacokinetics of diphemanil methylsulphate in infants.
Chéron, G; d'Athis, P; Olive, G; Pons, G; Rey, E; Vidal, AM, 1993
)
0.29
"The linear and predictable pharmacokinetic properties of the histamine H1-receptor antagonist levocabastine make it particularly suitable for intranasal or ocular treatment of allergic rhinoconjunctivitis."( The pharmacokinetic properties of topical levocabastine. A review.
Heykants, J; Meuldermans, W; Snoeck, E; Van de Velde, V; Van Peer, A; Woestenborghs, R, 1995
)
0.29
" Cimetidine significantly decreased the total body clearance and extended the plasma half-life of theophylline, but did not change its volume of distribution."( Drug interactions between theophylline and H2-antagonists, roxatidine acetate hydrochloride and cimetidine: pharmacokinetic analysis in rats in vivo.
Furuhata, M; Nagai, N; Ogata, H, 1995
)
0.29
" During and after the infusion, arterial blood was obtained for pharmacokinetic analyses, and the ventilatory response to a hypercarbic challenge was assessed."( Pharmacokinetics and pharmacodynamics of remifentanil in volunteer subjects with severe liver disease.
Connors, PM; Dershwitz, M; Dienstag, JL; Hoke, JF; Michałowski, P; Muir, KT; Rosow, CE, 1996
)
0.29
"There were no differences in any of the pharmacokinetic parameters for remifentanil or GR90291 between the two groups."( Pharmacokinetics and pharmacodynamics of remifentanil in volunteer subjects with severe liver disease.
Connors, PM; Dershwitz, M; Dienstag, JL; Hoke, JF; Michałowski, P; Muir, KT; Rosow, CE, 1996
)
0.29
" The observed half-life was used to provide an estimate of in vivo blood metabolic clearance of the compound."( The pharmacokinetics and extra-hepatic clearance of remifentanil, a short acting opioid agonist, in male beagle dogs during constant rate infusions.
Chism, JP; Rickert, DE, 1996
)
0.29
" This semicompartmental solution does not require the specification of a compartmental model for the pharmacokinetic response and may offer an advantage when model misspecification is present in using standard compartmental models."( A semicompartmental modeling approach for pharmacodynamic data assessment.
Karim, A; Kowalski, KG, 1995
)
0.29
" 230 l), and the half-life was slightly increased (19."( Influence of age, frailty and liver function on the pharmacokinetics of brofaromine.
Antonin, KH; Bergmann, W; Bieck, P; Degel, F; Fuchs, L; Platt, D; Zeeh, J, 1996
)
0.29
" The context-sensitive half-life remains very short (3 to 4 minutes), independent of the duration of infusion."( The pharmacokinetics of remifentanil.
Hug, CC; Michelsen, LG, 1996
)
0.29
" Population pharmacokinetic and pharmacodynamic modeling was performed using the software package NONMEM."( Influence of age and gender on the pharmacokinetics and pharmacodynamics of remifentanil. I. Model development.
Billard, V; Egan, TD; Gambus, PL; Hermann, DJ; Hoke, JF; Lemmens, HJ; Mandema, JW; Minto, CF; Moore, KH; Muir, KT; Schnider, TW; Shafer, SL; Youngs, E, 1997
)
0.3
"This study identified (1) an effect of age on the pharmacokinetics and pharmacodynamics of remifentanil; (2) an effect of lean body mass on the pharmacokinetic parameters; and (3) no influence of gender on any pharmacokinetic or pharmacodynamic parameter."( Influence of age and gender on the pharmacokinetics and pharmacodynamics of remifentanil. I. Model development.
Billard, V; Egan, TD; Gambus, PL; Hermann, DJ; Hoke, JF; Lemmens, HJ; Mandema, JW; Minto, CF; Moore, KH; Muir, KT; Schnider, TW; Shafer, SL; Youngs, E, 1997
)
0.3
" In a companion article, the authors developed complex population pharmacokinetic and pharmacodynamic models that incorporated age and lean body mass (LBM) as significant covariates and characterized intersubject pharmacokinetic and pharmacodynamic variability."( Pharmacokinetics and pharmacodynamics of remifentanil. II. Model application.
Minto, CF; Schnider, TW; Shafer, SL, 1997
)
0.3
"Based on the typical pharmacokinetic and pharmacodynamic parameters, nomograms for bolus dose and infusion rates at each age and LBM were derived."( Pharmacokinetics and pharmacodynamics of remifentanil. II. Model application.
Minto, CF; Schnider, TW; Shafer, SL, 1997
)
0.3
" This remains true even when interindividual pharmacokinetic and pharmacodynamic variability are incorporated in the analysis."( Pharmacokinetics and pharmacodynamics of remifentanil. II. Model application.
Minto, CF; Schnider, TW; Shafer, SL, 1997
)
0.3
" Remifentanil was rapidly eliminated, with a terminal half-life of 6 min, compared with 19 min for GR90291 and alfentanil."( Comparative pharmacokinetics and pharmacodynamics of remifentanil, its principle metabolite (GR90291) and alfentanil in dogs.
Cunningham, F; Hoffman, WE; Hoke, JF; James, MK; Muir, KT, 1997
)
0.3
" The antiarrhythmic response of coronary artery ligated dogs to pirmenol was described by a sigmoid Emax model, and no statistically significant differences were observed in the pharmacodynamic parameters [i."( Pharmacokinetics and pharmacodynamics of pirmenol enantiomers in coronary artery ligated dogs.
Chang, T; Janiczek, N; Mertz, TE; Smith, DE; Ventura, A, 1997
)
0.3
" The ideal therapy for GORD will have linear pharmacokinetics, a relatively long plasma half-life (t1/2), a duration of action allowing once daily administration, and a stable effect independent of interactions with food, antacids and other drugs."( Pharmacokinetic optimisation in the treatment of gastro-oesophageal reflux disease.
Berstad, A; Hatlebakk, JG, 1996
)
0.29
" Pharmacokinetic parameters evaluated after administration of single intravenous and oral doses were very similar and the ANOVA analysis did not show any statistically significant differences for t1/2, Cmax, V or AUC (normalised)."( A method using a liquid chromatographic-electrospray-mass spectrometric assay for the determination of antimigraine compounds: preliminary pharmacokinetics of MDL 74,721, sumatriptan and naratriptan, in rabbit.
David, M; Duléry, BD; Huebert, ND; Petty, MA; Schoun, J, 1997
)
0.3
" Pharmacokinetic evaluation of SB 223412 in rat and dog indicated low plasma clearance, oral bioavailability and high and sustained plasma concentrations after 4 to 8 mg/kg oral dosages."( Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Brawner, ME; Elshourbagy, NA; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Martin, LD; Medhurst, AD; Potts, W; Sarau, HM; Schmidt, DB; Webb, EF, 1997
)
0.3
" Information on serum/plasma concentration, bioavailability and half-life can often aid the discovery process by selecting those candidates with the desired pharmacokinetic parameters."( Pharmacokinetic screening for the selection of new drug discovery candidates is greatly enhanced through the use of liquid chromatography-atmospheric pressure ionization tandem mass spectrometry.
Bryant, MS; Korfmacher, WA; Lin, CC; Nardo, C; Nomeir, AA; Wang, S, 1997
)
0.3
" The pharmacokinetics of remifentanil were fit using a one-compartment pharmacokinetic model."( Pharmacokinetics and pharmacodynamics of remifentanil in persons with renal failure compared with healthy volunteers.
Connors, PM; Dershwitz, M; Glass, PS; Hoke, JF; Malthouse-Dufore, S; Martel, D; Michałowski, P; Muir, KT; Rosow, CE; Rubin, N; Shlugman, D, 1997
)
0.3
" Pharmacokinetic analysis revealed a modest, but significant (up to 40%) elevation in the area under the plasma concentration-time curve during 6 h of the drug administration, and a reduction in L-734,217 plasma clearance and volumes of distribution, in the anesthetized dogs."( Effects of pentobarbital on pharmacokinetics and pharmacodynamics of a potent fibrinogen receptor antagonist, L-734,217, in dogs.
Cook, JJ; Ellis, JD; Hand, EL; Holahan, MA; Prueksaritanont, T; Sitko, GR; Stranieri, MT, 1997
)
0.3
" We performed pharmacokinetic simulations to estimate the effect site concentrations of propofol and remifentanil as the infusion rates were modulated to meet the dynamic sedation and analgesic needs of the operation."( Remifentanil and propofol combination for awake craniotomy: case report with pharmacokinetic simulations.
Egan, TD; Johnson, KB, 1998
)
0.3
" A linked sigmoid Emax PK-PD model was used and the pharmacodynamic parameters were not statistically different."( The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat.
Eddington, ND; Haidar, SH; Hoke, JF; Liang, Z; Moreton, JE; Muir, KT, 1997
)
0.3
"At the doses tested, there is no pharmacokinetic or pharmacodynamic interaction between remifentanil and esmolol in the rat."( The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat.
Eddington, ND; Haidar, SH; Hoke, JF; Liang, Z; Moreton, JE; Muir, KT, 1997
)
0.3
" Pharmacokinetic studies were performed in 24 patients."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3
" The pharmacokinetic parameters of doxorubicin in this study were close to those usually described and were not influenced by escalation of the S9788 dose."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3
" After intravenous administration the half-life was short in all three animal species, due to a small volume of distribution and a relatively high clearance."( Animal pharmacokinetics of inogatran, a low-molecular-weight thrombin inhibitor with potential use as an antithrombotic drug.
Bredberg, U; Eriksson, UG; Regårdh, CG; Renberg, L; Teger-Nilsson, AC, 1998
)
0.3
" Drug interactions with cholinesterase inhibitors may occur by pharmacokinetic or pharmacodynamic mechanisms."( Pharmacokinetics and drug interactions of cholinesterase inhibitors administered in Alzheimer's disease.
Crismon, ML,
)
0.13
" Based on extensive assessment of the drug's pharmacokinetic profile, the currently approved initial oral dosing regimen for cisapride is 10 mg QID."( Pharmacokinetic profile of cisapride 20 mg after once- and twice-daily dosing.
Clyde, C; Herron, J; Lee, P; Mechlinski, W; Pesco-Koplowitz, L; Zhou, H,
)
0.13
" Each subject's pharmacokinetic parameters were estimated by fitting a two-compartment model to the concentration versus time curves."( Remifentanil pharmacokinetics in obese versus lean patients.
Egan, TD; Gupta, SK; Huizinga, B; Jaarsma, RL; Muir, KT; Sperry, RJ; Yee, JB, 1998
)
0.3
" The individual pharmacokinetic parameters of a two-compartment model were not significantly different between the obese versus lean cohorts (unless normalized to TBW)."( Remifentanil pharmacokinetics in obese versus lean patients.
Egan, TD; Gupta, SK; Huizinga, B; Jaarsma, RL; Muir, KT; Sperry, RJ; Yee, JB, 1998
)
0.3
"The essential findings of the study are that remifentanil's pharmacokinetics are not appreciably different in obese versus lean subjects and that remifentanil pharmacokinetic parameters are therefore more closely related to LBM than to TBW."( Remifentanil pharmacokinetics in obese versus lean patients.
Egan, TD; Gupta, SK; Huizinga, B; Jaarsma, RL; Muir, KT; Sperry, RJ; Yee, JB, 1998
)
0.3
" Following the infusion, plasma lubeluzole concentrations decayed biphasically, with a mean distribution half-life (t1/2alpha) of 30 to 65 minutes and a mean terminal half-life (t1/2beta) of 15 to 24 hours."( Pharmacokinetics of lubeluzole (Prosynap) after single intravenous doses in healthy subjects.
Crabbe, R; Hantson, L; Heykants, J; Van de Velde, V; Van Osselaer, N; Van Peer, A; Woestenborghs, R, 1998
)
0.3
"The aim of this study was to characterize the pharmacokinetic and pharmacodynamic profile of donepezil HCl, a chemically distinct and specific acetylcholinesterase (AChE) inhibitor for the treatment of Alzheimer's disease, following administration of single oral doses."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following single oral doses.
Friedhoff, LT; Rogers, SL, 1998
)
0.3
" Pharmacodynamic activity was determined by the radioenzymatic measurement of erythrocyte membrane acetylcholinesterase (rbc-AChE) inhibition."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following single oral doses.
Friedhoff, LT; Rogers, SL, 1998
)
0.3
"The pharmacokinetic disposition of donepezil was observed to be both linear and dose proportional following single-dose administration."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following single oral doses.
Friedhoff, LT; Rogers, SL, 1998
)
0.3
" The extended half-life of donepezil makes it suitable for once-daily dosing."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following single oral doses.
Friedhoff, LT; Rogers, SL, 1998
)
0.3
" Pharmacodynamic activity was determined by the radioenzymatic measurement of erythrocyte membrane acetylcholinesterase (rbc-AChE) inhibition."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following multiple oral doses.
Cooper, NM; Friedhoff, LT; Lee, JN; Pederson, JE; Rogers, SL; Sukovaty, R, 1998
)
0.3
"The pharmacokinetic disposition of donepezil was observed to be dose proportional."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following multiple oral doses.
Cooper, NM; Friedhoff, LT; Lee, JN; Pederson, JE; Rogers, SL; Sukovaty, R, 1998
)
0.3
" The half-life of donepezil makes it suitable for once-daily dosing."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following multiple oral doses.
Cooper, NM; Friedhoff, LT; Lee, JN; Pederson, JE; Rogers, SL; Sukovaty, R, 1998
)
0.3
" The pharmacodynamic parameters, Emin, Emax and Ess, were 62."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following evening administration.
Friedhoff, LT; Rogers, SL; Tiseo, PJ, 1998
)
0.3
"The measured pharmacokinetic and pharmacodynamic parameters for both 5 and 10 mg day(-1) donepezil administered in the evening are in good agreement with previous results obtained with morning administration, indicating no time of dosing effect."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following evening administration.
Friedhoff, LT; Rogers, SL; Tiseo, PJ, 1998
)
0.3
" Pharmacokinetic comparisons were made between groups for the day 1 and day 7 profiles."( Concurrent administration of donepezil HCl and cimetidine: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.3
"On both day 1 and day 7, a statistically significant difference was observed between the donepezil and the donepezil + cimetidine groups in terms of the Cmax and AUC(0-24) values for donepezil."( Concurrent administration of donepezil HCl and cimetidine: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.3
"Co-administration of donepezil HCl (5 mg) and cimetidine (800 mg) did not produce clinically significant changes in the pharmacokinetic profiles of either drug."( Concurrent administration of donepezil HCl and cimetidine: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.3
" Pharmacokinetic comparisons were made between treatment groups for the day 1 and day 7 profiles."( Concurrent administration of donepezil HCl and ketoconazole: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.3
"On both day 1 and day 7, a statistically significant difference was observed between the donepezil and the donepezil + ketoconazole treatment groups in terms of Cmax and AUC(0-24) of donepezil."( Concurrent administration of donepezil HCl and ketoconazole: assessment of pharmacokinetic changes following single and multiple doses.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.3
"Concurrent administration of donepezil HCl does not alter the pharmacokinetic profile of theophylline following multiple-dose administration of both drugs in healthy volunteers."( Concurrent administration of donepezil HCl and theophylline: assessment of pharmacokinetic changes following multiple-dose administration in healthy volunteers.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
"25 mg) produced no changes in the pharmacokinetic profile of either drug."( Concurrent administration of donepezil HCl and digoxin: assessment of pharmacokinetic changes.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ, 1998
)
0.3
"The aim of the study was to examine the pharmacokinetic and pharmacodynamic profiles of single doses of warfarin (25 mg) following administration alone, and in combination with multiple doses of donepezil HCl (10 mg day(-1)) in healthy volunteers."( The effect of multiple doses of donepezil HCl on the pharmacokinetic and pharmacodynamic profile of warfarin.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
" Pharmacokinetic parameters were assessed for both (R)- and (S)-warfarin concentrations in plasma, and pharmacodynamic analyses utilizing prothrombin time were undertaken."( The effect of multiple doses of donepezil HCl on the pharmacokinetic and pharmacodynamic profile of warfarin.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
" Warfarin pharmacodynamic parameters, Rmax and AUC(PT), were also unchanged by concomitant administration ofdonepezil."( The effect of multiple doses of donepezil HCl on the pharmacokinetic and pharmacodynamic profile of warfarin.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
"Concurrent administration of donepezil HCl does not alter the pharmacokinetic or pharmacodynamic profile of single doses of warfarin in healthy volunteers."( The effect of multiple doses of donepezil HCl on the pharmacokinetic and pharmacodynamic profile of warfarin.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
"The aim of this study was to evaluate the pharmacokinetic profile of donepezil HCl (5 mg) in patients with impaired hepatic function, following the administration of single oral doses."( An evaluation of the pharmacokinetics of donepezil HCl in patients with impaired hepatic function.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ; Vargas, R, 1998
)
0.3
"This was an open-label, non-randomized study comparing the pharmacokinetic profile of donepezil in male volunteers with chronic compensated cirrhosis of the liver (n = 10) to that in healthy age- and sex-matched controls (n = 10)."( An evaluation of the pharmacokinetics of donepezil HCl in patients with impaired hepatic function.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ; Vargas, R, 1998
)
0.3
" Blood samples for pharmacokinetic measurements were taken at specified intervals for 17 days post-dose."( An evaluation of the pharmacokinetics of donepezil HCl in patients with moderately to severely impaired renal function.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
"There were no statistical differences between the two groups for any of the pharmacokinetic parameters evaluated (ANOVA)."( An evaluation of the pharmacokinetics of donepezil HCl in patients with moderately to severely impaired renal function.
Foley, K; Friedhoff, LT; Tiseo, PJ, 1998
)
0.3
"The purpose of this study was to investigate the in vivo pharmacodynamics and the pharmacodynamic interactions of remifentanil and its major metabolite, GR90291, in a rat electroencephalographic model."( The comparative pharmacodynamics of remifentanil and its metabolite, GR90291, in a rat electroencephalographic model.
Cox, EH; Danhof, M; Gubbens-Stibbe, JM; Langemeijer, MW; Muir, KT, 1999
)
0.3
" The mean terminal half-life was approximately 45 and 44 hours, respectively."( Lack of effect of erythromycin and ketoconazole on the pharmacokinetics and pharmacodynamics of steady-state intranasal levocabastine.
Grover, M; Hall, N; Hassell, A; Hunt, T; Lee, P; Mechlinski, W; Pesco-Koplowitz, L; Smith, R; Travers, S; Wiesinger, B; Zhou, H, 1999
)
0.3
" No drug was administered on study day 2 because of pharmacokinetic sampling."( Pharmacokinetics and electrocardiographic effect of ebastine in young versus elderly healthy subjects.
Argenti, D; Garcia, J; Heald, D; Huang, MY; Wilson, J, 1998
)
0.3
"The objective of this work was to assess the pharmacokinetics of napsagatran, a low molecular weight thrombin inhibitor, after intravenous administration in a variety of laboratory animals, and prospectively to help design the first pharmacokinetic studies in man."( Interspecies pharmacokinetic comparisons and allometric scaling of napsagatran, a low molecular weight thrombin inhibitor.
Gianni, A; Girometta, MA; Guenzi, A; Lavé, T; Portmann, R; Schenker, G; Schmitt, M, 1999
)
0.3
" Pharmacokinetic profiles, including area under the curve (AUC), log(AUC), maximal concentration (Cmax), log(Cmax), time to maximal concentration (Tmax), and half-life (T(1/2)), were determined at completion of the single- and multiple-dose regimens (days 1 and 9, respectively)."( Pharmacokinetic profiles of repaglinide in elderly subjects with type 2 diabetes.
Hatorp, V; Huang, WC; Strange, P, 1999
)
0.3
" Particular emphasis was placed on intersubject variability of the pharmacokinetic and pharmacodynamic parameters of Ro 44-3888."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" Part II, a double-blind, placebo-controlled, parallel-group study, addressed the intersubject variability of pharmacokinetic and pharmacodynamic parameters of the active principle at a sibrafiban dose achieving an intermediate effect."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" The interindividual coefficients of variation of the integrated pharmacokinetic and pharmacodynamic parameters (AUC and AUE) were below 20%, thus lying well within the pre-set level of acceptance."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
"With a low intersubject variability of its pharmacokinetic and pharmacodynamic parameters, linear pharmacokinetics and pharmacodynamic effects closely related to its plasma concentrations, Ro 44-3888 has good pharmacological prerequisites for a well controllable therapy of secondary prevention of arterial thrombosis in patients with acute coronary syndrome."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" This difference may greatly affect the estimation of pharmacokinetic and pharmacodynamic parameters."( Influence of arteriovenous sampling on remifentanil pharmacokinetics and pharmacodynamics.
Egan, TD; Hermann, DJ; Muir, KT, 1999
)
0.3
"To assess the effects of sampling site on the pharmacokinetic and pharmacodynamic characteristics of remifentanil."( Influence of arteriovenous sampling on remifentanil pharmacokinetics and pharmacodynamics.
Egan, TD; Hermann, DJ; Muir, KT, 1999
)
0.3
" Pharmacokinetic parameters estimated from venous and arterial data differed significantly."( Influence of arteriovenous sampling on remifentanil pharmacokinetics and pharmacodynamics.
Egan, TD; Hermann, DJ; Muir, KT, 1999
)
0.3
" When designing studies to measure the acute time course (ie, non-steady state) of concentration and effect, the potential effects of sampling site on pharmacokinetic and pharmacodynamic characteristics must be carefully considered, particularly when the arteriovenous drug concentration difference is large."( Influence of arteriovenous sampling on remifentanil pharmacokinetics and pharmacodynamics.
Egan, TD; Hermann, DJ; Muir, KT, 1999
)
0.3
"In this open-label, single-center, pharmacokinetic study of repaglinide, 12 healthy volunteers (6 men, 6 women) were enrolled in each of 2 groups (total, 24 volunteers)."( Repaglinide pharmacokinetics in healthy young adult and elderly subjects.
Hatorp, V; Huang, WC; Strange, P, 1999
)
0.3
"It has previously been reported that a 3-(3-(piperazin-1-yl)propyl)indole series of 5-HT1D receptor ligands have pharmacokinetic advantages over the corresponding 3-(3-(piperidin-1-yl)propyl)indole series and that the reduced pKa of the piperazines compared to the piperidines may be one possible explanation for these differences."( Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
Beer, MS; Broughton, HB; Castro, JL; Cheng, SK; Collins, I; Goodacre, SC; Heald, A; Locker, KL; MacLeod, AM; Morrison, D; Moyes, CR; O'Connor, D; Pike, A; Rowley, M; Russell, MG; Sohal, B; Stanton, JA; Thomas, S; van Niel, MB; Verrier, H; Watt, AP, 1999
)
0.48
" Remifentanil's rapid onset-rapid offset pharmacokinetic profile enabled precise control of the level of opioid effect."( Remifentanil for conscious sedation and analgesia during awake fiberoptic tracheal intubation: a case report with pharmacokinetic simulations.
Egan, TD; Reusche, MD, 1999
)
0.3
" Of the many trihalobenzocycloheptapyridine analogues prepared, we have identified several which inhibit FPT and cellular proliferation at single-digit nanomolar concentrations and which have good pharmacokinetic properties in mice."( Identification of pharmacokinetically stable 3, 10-dibromo-8-chlorobenzocycloheptapyridine farnesyl protein transferase inhibitors with potent enzyme and cellular activities.
Afonso, A; Alvarez, C; Bishop, WR; Carr, D; Chao, J; del Rosario, J; Deskus, J; Doll, RJ; Ganguly, AK; Girijavallabhan, VM; Heimark, L; James, L; Kirschmeier, P; Lalwani, T; Liu, M; Mallams, AK; Njoroge, FG; Pinto, P; Pramanik, B; Remiszewski, S; Rossman, RR; Taveras, AG; Vaccaro, CJ; Vibulbhan, B; Wang, L, 1999
)
0.3
" Slight but significant differences of some pharmacokinetic parameters were observed between genders."( Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part I: Pharmacokinetics and tissular distribution in Sprague-Dawley rats.
Buzas, A; Duchêne, P; Houin, G; Ladure, P; Merour, JY; Ollivier, R; Tran, G, 1999
)
0.3
" One young subject was excluded from the pharmacokinetic analyses owing to an insufficient urine collection."( Comparison of pharmacokinetics of NS-105, a novel agent for cerebrovascular disease, in elderly and young subjects.
Isawa, S; Kumagai, Y; Miyatake, S; Mukai, H; Murasaki, M; Yokota, S, 1999
)
0.3
" The focus was on the pharmacokinetics, the metabolism, the dose dependency and gender differences of the pharmacokinetic parameters of BM 113 and its main desacetylated metabolite, BM 212."( Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part III: Pharmacokinetics, metabolism, dose dependency and gender effect after single or repeated administration to human healthy volunteers.
Buzas, A; Duchêne, P; Houin, G; Ladure, P; Laneury, JP; Merour, JY; Ollivier, R; Tran, G, 1999
)
0.3
" The Cmax and AUC0-infinity of radioactivity concentration were proportional to the dose for 1-100 mg/kg of 14C-NS-105."( Pharmacokinetics of NS-105, a novel cognition enhancer. 1st communication: absorption, metabolism and excretion in rats, dogs and monkeys after single administration of 14C-NS-105.
Ago, M; Morino, A; Mukai, H; Sugimoto, T, 1999
)
0.3
" Values for AUC and Cmax were significantly higher in CLD patients compared with healthy subjects, and the MRT was prolonged in CLD patients."( Single-dose pharmacokinetics of repaglinide in subjects with chronic liver disease.
Christensen, MS; Hatorp, V; Haug-Pihale, G; Walther, KH, 2000
)
0.31
" There were no significant differences between the pharmacokinetic parameters of repaglinide when given as monotherapy and when administered concurrently with cimetidine."( Drug interaction studies with repaglinide: repaglinide on digoxin or theophylline pharmacokinetics and cimetidine on repaglinide pharmacokinetics.
Hatorp, V; Thomsen, MS, 2000
)
0.31
"We conducted a phase I, multicenter, parallel-group, pharmacokinetic comparison trial with single and multiple doses of repaglinide in subjects with various degrees of renal impairment."( Pharmacokinetics of repaglinide in subjects with renal impairment.
Andersen, MP; Hatorp, V; Huang, WC; Marbury, TC; Nielsen, KK; Ruckle, JL; Strange, P, 2000
)
0.31
" Using published pharmacokinetic values for remifentanil and the method of collapsing hysteresis loops, the authors estimated the effect-site equilibration rate constant (k(eo)), the effect-site concentration producing 50% respiratory depression (EC50), and the shape parameter of the concentration-response curve (gamma)."( The pharmacodynamic effect of a remifentanil bolus on ventilatory control.
Babenco, HD; Conard, PF; Gross, JB, 2000
)
0.31
"The addition of ticlopidine/aspirin to sibrafiban did not significantly alter the pharmacokinetic parameters of Ro 44-3888."( Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin.
Birnböck, H; Chung, J; Ensor, H; Ertel, SI; Lausecker, B; Machin, SJ; MacKie, IJ; Wittke, B, 2000
)
0.31
"This study shows a significant pharmacodynamic interaction between sibrafiban and ticlopidine/aspirin."( Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin.
Birnböck, H; Chung, J; Ensor, H; Ertel, SI; Lausecker, B; Machin, SJ; MacKie, IJ; Wittke, B, 2000
)
0.31
" No pharmacodynamic interaction was seen with coadministration of heparin."( Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered GP IIb/IIIa antagonist, following coadministration of aspirin and heparin.
Modi, NB; Novotny, W; Reimann, JD, 2000
)
0.31
" The influence of CO on pharmacokinetic and pharmacodynamic parameters of rocuronium in patients was evaluated using a recirculatory pharmacokinetic model."( Recirculatory pharmacokinetics and pharmacodynamics of rocuronium in patients: the influence of cardiac output.
Boer, F; Bovill, JG; Burm, AG; Kuipers, JA; Olofsen, E, 2001
)
0.31
" For drugs with a fast onset of effect, a recirculatory model, which includes CO, can give a good description of the relation between concentration and effect, in contrast to a conventional compartmental pharmacokinetic model."( Recirculatory pharmacokinetics and pharmacodynamics of rocuronium in patients: the influence of cardiac output.
Boer, F; Bovill, JG; Burm, AG; Kuipers, JA; Olofsen, E, 2001
)
0.31
" Pharmacokinetic parameters were estimated using a three-compartment model."( Influence of hemorrhagic shock on remifentanil: a pharmacokinetic and pharmacodynamic analysis.
Egan, TD; Hamber, EA; Johnson, KB; Kern, SE; Kohnstamm, KM; McJames, SW, 2001
)
0.31
"A single-agent dose-escalating phase I and pharmacokinetic study on the farnesyl transferase inhibitor SCH 66336 was performed to determine the safety profile, maximum-tolerated dose, and recommended dose for phase II studies."( Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH 66336 given twice daily to patients with advanced solid tumors.
Awada, A; Cutler, DL; de Jonge, MJ; Eskens, FA; Faber, MN; Hanauske, AR; Luyten, GP; Piccart, M; Sparreboom, A; Statkevich, P; Verweij, J, 2001
)
0.31
" Pharmacokinetic sampling was performed on days 1 and 15."( Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH 66336 given twice daily to patients with advanced solid tumors.
Awada, A; Cutler, DL; de Jonge, MJ; Eskens, FA; Faber, MN; Hanauske, AR; Luyten, GP; Piccart, M; Sparreboom, A; Statkevich, P; Verweij, J, 2001
)
0.31
"The terminal half-life of sabeluzole was significantly prolonged in subjects with severe hepatic dysfunction vs healthy subjects (respectively 39."( Pharmacokinetics of sabeluzole and dextromethorphan oxidation capacity in patients with severe hepatic dysfunction and healthy volunteers.
Blin, O; Bouhours, P; Lacarelle, B; Le Moing, JP; Levron, JC; Micallef, J; Nataf, MB; Pageaux, GP, 2001
)
0.31
" The pharmacodynamic data, ex vivo platelet aggregation, were described with the use of a direct effect inhibitory sigmoidal model with a baseline."( A population pharmacokinetic-pharmacodynamic and logistic regression analysis of lotrafiban in patients.
Aluri, J; Chapelsky, M; Granett, J; Mould, D; Samuels, R; Swagzdis, J, 2001
)
0.31
"The pharmacokinetic parameters of napsagatran were not significantly influenced by co-administration of warfarin."( The effect of warfarin on the pharmacokinetics and pharmacodynamics of napsagatran in healthy male volunteers.
Burggraaf, J; Cohen, AF; Faaij, RA; Goggin, T; Guenzi, A; Kroon, JM; Schoemaker, RC; van Griensven, JM, 2001
)
0.31
"Warfarin has no effect on the pharmacokinetics of napsagatran, but has a marked influence on the pharmacodynamic parameters (APTT, PT) of napsagatran."( The effect of warfarin on the pharmacokinetics and pharmacodynamics of napsagatran in healthy male volunteers.
Burggraaf, J; Cohen, AF; Faaij, RA; Goggin, T; Guenzi, A; Kroon, JM; Schoemaker, RC; van Griensven, JM, 2001
)
0.31
"Mean area under the curve and Cmax values on Day 1 and Day 5 were similar for ebastine but approximately doubled for carebastine due to its longer half-life."( Effect of age and gender on the pharmacokinetics of ebastine after single and repeated dosing in healthy subjects.
Aubeneau, M; Gillen, M; Jan, C; Jensen, BK; Pandit, B; Rhodes, G; Rohatagi, S, 2001
)
0.31
" Specifically, certain metabolic parameters (ie, half-life and route of metabolism/elimination) can affect a drug's tolerability and become important when a switch from one agent to another is contemplated."( Pharmacokinetic profiles of current therapies for Alzheimer's disease: implications for switching to galantamine.
Farlow, MR, 2001
)
0.31
" In the group of patients with severe renal dysfunction, the main pharmacokinetic finding was a longer half-life after multiple dosing."( Single- and multiple-dose pharmacokinetics of repaglinide in patients with type 2 diabetes and renal impairment.
Abbasi, I; Hasslacher, C; Hatorp, V; Sattler, K; Schumacher, S; Sieber, J; Weise, D, 2001
)
0.31
"The dose-dependency of budipine pharmacokinetic characteristics was studied."( Dose linearity and steady state pharmacokinetics of the new antiparkinson agent budipine after oral administration.
Bethke, TH; Hauschke, D; Heinze, H; Merz, M; Seiberling, M; Wurst, W; Zech, K, 2001
)
0.31
" A pharmacokinetic study was performed in rabbits and tissue distribution studies were carried out in rats."( Pharmacokinetics and tissue distribution of piperine in animals after i.v. bolus administration.
Mada, SR; Sunkara, G; Vobalaboina, V, 2001
)
0.31
" Relationships between pharmacokinetic variables and each parameter related to hepatic functions were also investigated."( Pharmacokinetics of roxatidine acetate in patients with chronic liver disease.
Takase, S; Tsutsumi, M; Ueshima, Y, 2001
)
0.31
"There was no difference in the pharmacokinetic variables and serum levels of roxatidine between chronic hepatitis and healthy controls."( Pharmacokinetics of roxatidine acetate in patients with chronic liver disease.
Takase, S; Tsutsumi, M; Ueshima, Y, 2001
)
0.31
" This study showed the absence of any pharmacokinetic difference between the two enantiomers when administered individually, and no enantiomeric inversion."( Pharmacokinetics of gacyclidine enantiomers in plasma and spinal cord after single enantiomer administration in rats.
D'Arbigny, P; Dukic, S; Hoizey, G; Kaltenbach, ML; Lamiable, D; Millart, H; Vistelle, R, 2001
)
0.31
" Arterial blood samples were collected and analyzed by mass spectroscopy to determine remifentanil pharmacokinetic profiles."( Pharmacokinetics of remifentanil in anesthetized pediatric patients undergoing elective surgery or diagnostic procedures.
Davis, PJ; Dear Gd, GL; Ginsberg, B; Henson, LG; Huffman, C; McGowan, FX; Muir, KT; Ross, AK; Stiller, RD, 2001
)
0.31
" A preliminary pharmacokinetic study was carried out in mice by administering phenytoin (10 mg) orally, with or without piperine (0."( Piperine in food: interference in the pharmacokinetics of phenytoin.
Bhardwaj, RK; Gupta, SK; Jaiswal, J; Jasuja, R; Velpandian, T,
)
0.13
" Phase I and II clinical trials demonstrated donepezil's favorable pharmacokinetic, pharmacodynamic and safety profile."( Donepezil for Alzheimer's disease: pharmacodynamic, pharmacokinetic, and clinical profiles.
Homma, A; Shigeta, M, 2001
)
0.31
" In addition, pharmacokinetic analysis showed that a high-fat breakfast increased the extent of absorption."( Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women.
Burghart, PH; Cotreau, MM; Dykstra, KH; Gandhi, T; Gutierrez, M; Park, Y; Schwertschlag, US; Stonis, L; Xu, J, 2002
)
0.31
"To develop a predictive population pharmacokinetic/ pharmacodynamic (PK/PD) model for repaglinide (REP), an oral hypoglycemic agent, using artificial neural networks (ANNs)."( Modeling the pharmacokinetics and pharmacodynamics of a unique oral hypoglycemic agent using neural networks.
Fossler, MJ; Haidar, SH; Hussain, AS; Johnson, SB, 2002
)
0.31
"A two-compartment pharmacokinetic model provided an adequate fit for individual patient data."( End-stage renal failure reduces central clearance and prolongs the elimination half life of remifentanil.
Dahaba, AA; List, WF; Oettl, K; Reibnegger, G; von Klobucar, F, 2002
)
0.31
" The pharmacokinetic profile of repaglinide and the improvements in post-prandial hyperglycaemia and overall glycaemic control make repaglinide suitable for administration preprandially, with the opportunity for flexible meal arrangements, including skipped meals, without the risk of hypoglycaemia."( Clinical pharmacokinetics and pharmacodynamics of repaglinide.
Hatorp, V, 2002
)
0.31
" This article presents the latest information on their pharmacokinetic properties and pharmacodynamic activity."( Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors.
Jann, MW; Shirley, KL; Small, GW, 2002
)
0.31
" The temporal profile of the effect site concentration of remifentanil, estimated from a pharmacokinetic model, was incorporated into a linear model of the fMRI data."( Combining fMRI with a pharmacokinetic model to determine which brain areas activated by painful stimulation are specifically modulated by remifentanil.
Bantick, S; Painter, D; Ploghaus, A; Rapeport, G; Rogers, R; Tracey, I; Williams, P; Wise, RG, 2002
)
0.31
" We conducted a phase I trial and pharmacokinetic study of flavopiridol given as a 72-h continuous intravenous infusion repeated every 2 weeks."( Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol.
Alberti, D; Arzoomanian, R; Bailey, HH; Binger, K; Cleary, JF; Dresen, A; Feierabend, C; Marnocha, R; Simon, K; Thomas, JP; Tutsch, KD; Wilding, G, 2002
)
0.31
" Additional postinfusion pharmacokinetic sampling was done at the 40 and 50 mg/m(2)/24 h dose levels."( Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol.
Alberti, D; Arzoomanian, R; Bailey, HH; Binger, K; Cleary, JF; Dresen, A; Feierabend, C; Marnocha, R; Simon, K; Thomas, JP; Tutsch, KD; Wilding, G, 2002
)
0.31
" The terminal half-life at the MTD was 26."( Phase I clinical and pharmacokinetic trial of the cyclin-dependent kinase inhibitor flavopiridol.
Alberti, D; Arzoomanian, R; Bailey, HH; Binger, K; Cleary, JF; Dresen, A; Feierabend, C; Marnocha, R; Simon, K; Thomas, JP; Tutsch, KD; Wilding, G, 2002
)
0.31
" Although they are commonly administered together for clinical anesthesia, their pharmacokinetic interaction has not been investigated so far."( Non-steady state analysis of the pharmacokinetic interaction between propofol and remifentanil.
Bertaccini, E; Bouillon, T; Bruhn, J; Park, S; Radu-Radulescu, L; Shafer, S, 2002
)
0.31
" After having established the individual population models for both drugs and an exploratory analysis for hypothesis generation, pharmacokinetic interaction was identified by including an interaction term into the population model and comparing the value of the objective function in the presence and absence of the respective term."( Non-steady state analysis of the pharmacokinetic interaction between propofol and remifentanil.
Bertaccini, E; Bouillon, T; Bruhn, J; Park, S; Radu-Radulescu, L; Shafer, S, 2002
)
0.31
" Pharmacokinetic profiles, including area under the curve (AUC0-t), maximum serum concentration (Cmax), time to Cmax (tmax), and half-life (t1/2), were determined for each dose of repaglinide."( Pharmacokinetics of repaglinide in healthy caucasian and Japanese subjects.
Chassard, D; Evène, E; Jørgensen, M; Nielsen, KK; Thomsen, MS, 2003
)
0.32
" The parameters Cmax and AUC increased proportionally with dose level, whereas all other pharmacokinetic parameters were independent of the dose."( Safety and pharmacokinetics of ReN1869: a first human dose study in healthy subjects after single-dose administration.
Gerrits, M; Ingwersen, SH; Skrumsager, BK, 2003
)
0.32
" Roxifiban has pharmacokinetic and pharmacodynamic properties believed to be more favorable than the earlier oral agents."( Effects of glycoprotein IIb/IIIa antagonists on platelet activation: development of a transfer method to mimic peak to trough receptor occupancy.
Billheimer, JT; He, B; Seiffert, D; Spitz, SM; Stern, AM, 2002
)
0.31
"To investigate the enantioselective pharmacokinetic process of benproperine in healthy volunteers."( [Enantioselective pharmacokinetics of benproperine in healthy volunteers].
Chen, XY; Du, ZM; Kang, Y; Zhong, DF, 2000
)
0.31
" The treatment ratios of Cmax and associated 90% CIs for risperidone active moiety (ratio = 114."( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil.
Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003
)
0.32
" The improved bioavailability is reflected in various pharmacokinetic parameters viz."( Effect of co-administration of piperine on pharmacokinetics of beta-lactam antibiotics in rats.
Dhuley, JN; Hiwale, AR; Naik, SR, 2002
)
0.31
"Knowledge of the pharmacodynamic interaction between remifentanil and propofol is important to permit optimal dosage strategies."( Modelling the pharmacodynamic interaction between remifentanil and propofol by EEG-controlled dosing.
Albrecht, S; Fechner, J; Hering, W; Ihmsen, H; Palmaers, T; Schüttler, J, 2003
)
0.32
"Within the studied concentration range, remifentanil and propofol showed an additive type of pharmacodynamic interaction on the electroencephalogram."( Modelling the pharmacodynamic interaction between remifentanil and propofol by EEG-controlled dosing.
Albrecht, S; Fechner, J; Hering, W; Ihmsen, H; Palmaers, T; Schüttler, J, 2003
)
0.32
" Both drugs were dosed and titrated based on computer-assisted pharmacokinetic models to maintain constant plasma concentrations."( Pharmacokinetic-based total intravenous anaesthesia using remifentanil and propofol for surgical myocardial revascularization.
De Cosmo, D; De Stefani, R; Guarracino, F; Penzo, D; Vardanega, A, 2003
)
0.32
" Additionally, a pharmacodynamic study was performed."( Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
Calvo, R; de la Fuente, L; Jauregizar, N; Quintana, A; Raczka, E; Suarez, E,
)
0.13
"Both pharmacokinetic changes (decreased volume of distribution and clearance and increased elimination half-life) and pharmacodynamic alterations (decrease in total and unbound EC(50)) may be responsible for the different responses to lerisetron observed in old rats."( Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
Calvo, R; de la Fuente, L; Jauregizar, N; Quintana, A; Raczka, E; Suarez, E,
)
0.13
" Compared to administration of repaglinide alone, concomitant ketoconazole increased mean AUC0-infinity for repaglinide by 15% and mean Cmax by 7%."( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide.
Hansen, KT; Hatorp, V; Thomsen, MS, 2003
)
0.32
" The apparent elimination half-life (T1/2) of LOR was (6+/-4) h, and that of DCL was (13."( Pharmacokinetics of loratadine and its active metabolite descarboethoxyloratadine in healthy Chinese subjects.
Chen, XY; Dong, YM; Zhang, YF; Zhong, DF, 2003
)
0.32
"To simulate the time course of drug effect, it is sometimes necessary to combine the pharmacodynamic parameters from an integrated pharmacodynamic-pharmacodynamic study (e."( Using the time of maximum effect site concentration to combine pharmacokinetics and pharmacodynamics.
Gregg, KM; Henthorn, TK; Minto, CF; Schnider, TW; Shafer, SL, 2003
)
0.32
"The naive approach to combining separate pharmacokinetic and pharmacodynamic studies is to simply take the k(e0) from the pharmacodynamic study and apply it naively to the pharmacokinetic study of interest."( Using the time of maximum effect site concentration to combine pharmacokinetics and pharmacodynamics.
Gregg, KM; Henthorn, TK; Minto, CF; Schnider, TW; Shafer, SL, 2003
)
0.32
"T(peak) is a useful pharmacodynamic parameter and can be used to link separate pharmacokinetic and pharmacodynamic studies."( Using the time of maximum effect site concentration to combine pharmacokinetics and pharmacodynamics.
Gregg, KM; Henthorn, TK; Minto, CF; Schnider, TW; Shafer, SL, 2003
)
0.32
"This study determined the pharmacokinetic profile of single-dose loratadine-ambroxol hydrochloride combination therapy versus each component given separately."( Pharmacokinetic properties of single-dose loratadine and ambroxol alone and combined in tablet formulations in healthy men.
Alcántar, F; Herrera, J; Morales, JM; Rodríguez, JM; Rosete, R; Villacampa, J, 2003
)
0.32
" Comparison of the effective half-life of ebastine and carebastine between groups did not show relevant differences."( Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.
Dilzer, SC; Lasseter, KC; Noveck, RJ; Vargas, R; Waldman, S, 2004
)
0.32
" Pharmacokinetic parameters obtained by simultaneous modelling of remifentanil and RA data were statistically compared between the two groups."( Pharmacokinetics of remifentanil and its major metabolite, remifentanil acid, in ICU patients with renal impairment.
Albrecht, S; Bach, V; Bodenham, A; Bonde, J; Breen, D; Fisher, G; Kessler, P; Kirkham, A; Pitsiu, M; Wilmer, A, 2004
)
0.32
"Although RA accumulates in patients with moderate/severe renal impairment, pharmacokinetic modelling predicts that RA concentrations during a 9 microg kg(-1) h(-1) remifentanil infusion for up to 15 days would not exceed those reported in the present study, for which no associated prolongation of mu-opioid effects was observed."( Pharmacokinetics of remifentanil and its major metabolite, remifentanil acid, in ICU patients with renal impairment.
Albrecht, S; Bach, V; Bodenham, A; Bonde, J; Breen, D; Fisher, G; Kessler, P; Kirkham, A; Pitsiu, M; Wilmer, A, 2004
)
0.32
"Although remifentanil's short-acting pharmacokinetic profile makes it well suited for procedures during which a brief period of intense analgesia is required, setting up an infusion pump for brief procedures is inconvenient."( Remifentanil by bolus injection: a safety, pharmacokinetic, pharmacodynamic, and age effect investigation in human volunteers.
Egan, TD; Kern, SE; Muir, KT; White, J, 2004
)
0.32
" A population pharmacokinetic model was constructed using non-linear, mixed-effects modelling techniques based on arterial blood samples."( Remifentanil by bolus injection: a safety, pharmacokinetic, pharmacodynamic, and age effect investigation in human volunteers.
Egan, TD; Kern, SE; Muir, KT; White, J, 2004
)
0.32
" The pharmacokinetic simulations illustrated the potential utility of bolus-dose remifentanil."( Remifentanil by bolus injection: a safety, pharmacokinetic, pharmacodynamic, and age effect investigation in human volunteers.
Egan, TD; Kern, SE; Muir, KT; White, J, 2004
)
0.32
" Pharmacokinetic parameters were determined by model-independent techniques."( Single oral dose safety, tolerability, and pharmacokinetics of PNU-96391 in healthy volunteers.
Adams, G; Azie, NE; Bombardt, PA; Donaldson, K; Francom, SF; Rodríguez, CA; Staton, BA, 2004
)
0.32
"This open label, multicentre study was conducted to assess the times to offset of the pharmacodynamic effects and the safety of remifentanil in patients with varying degrees of renal impairment requiring intensive care."( Offset of pharmacodynamic effects and safety of remifentanil in intensive care unit patients with various degrees of renal impairment.
Albrecht, S; Bach, V; Bodenham, A; Bonde, J; Breen, D; Kessler, P; Shaikh, S; Wilmer, A, 2004
)
0.32
"Remifentanil was well tolerated, and the offset of pharmacodynamic effects was not prolonged either as a result of renal dysfunction or prolonged infusion up to 72 hours."( Offset of pharmacodynamic effects and safety of remifentanil in intensive care unit patients with various degrees of renal impairment.
Albrecht, S; Bach, V; Bodenham, A; Bonde, J; Breen, D; Kessler, P; Shaikh, S; Wilmer, A, 2004
)
0.32
" By allometric scaling of in vivo animal data, clearance of PNU-96391 in humans was over-predicted by 4-fold, half-life was under-predicted by 3-fold, and volume of distribution was accurately predicted."( Comparison of prediction methods for in vivo clearance of (S,S)-3-[3-(methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride, a dopamine D2 receptor antagonist, in humans.
Black, ML; Duncan, JN; Toth, LN; Yamazaki, S, 2004
)
0.32
"The purpose of this investigation was to describe the pharmacodynamic interaction between propofol and remifentanil for probability of no response to shaking and shouting, probability of no response to laryngoscopy, Bispectral Index (BIS), and electroencephalographic approximate entropy (AE)."( Pharmacodynamic interaction between propofol and remifentanil regarding hypnosis, tolerance of laryngoscopy, bispectral index, and electroencephalographic approximate entropy.
Andresen, C; Bouillon, TW; Bruhn, J; Cohane, C; Radulescu, L; Shafer, SL; Shafer, TJ, 2004
)
0.32
" The pharmacodynamic synergy of opioids and hypnotics was investigated using a volunteer study paradigm."( A response surface analysis of propofol-remifentanil pharmacodynamic interaction in volunteers.
Egan, TD; Kern, SE; White, JL; Xie, G, 2004
)
0.32
" The purpose of this study was to describe the pharmacodynamic interaction of remifentanil and propofol when used in combination for esophagogastroduodenoscopy in pediatric patients."( Determination of the pharmacodynamic interaction of propofol and remifentanil during esophagogastroduodenoscopy in children.
Drover, DR; Hammer, GB; Litalien, C; Shafer, SL; Wellis, V, 2004
)
0.32
" Propofol was administered via a target-controlled infusion system using the STANPUMP software based on a pediatric pharmacokinetic model."( Determination of the pharmacodynamic interaction of propofol and remifentanil during esophagogastroduodenoscopy in children.
Drover, DR; Hammer, GB; Litalien, C; Shafer, SL; Wellis, V, 2004
)
0.32
" The objectives of this study were (1) to evaluate the pharmacokinetic (PK) effects of administering nitroxide covalently bound to HBOCs compared to those of free nitroxide coadministered with HBOCs and (2) to elucidate the effects of differing molecular weight HBOCs on the PK of bound nitroxide in a conscious guinea pig model of 25% blood exchange transfusion."( Polynitroxyl hemoglobin: a pharmacokinetic study of covalently bound nitroxides to hemoglobin platforms.
Buehler, PW; Gulati, A; Haney, CR; Hsia, CJ; Ma, L, 2004
)
0.32
"To determine whether an in vivo pharmacokinetic interaction exists between memantine and the acetylcholinesterase (AChE) inhibitor donepezil."( Lack of pharmacokinetic or pharmacodynamic interaction between memantine and donepezil.
Abramowitz, WT; Periclou, AP; Rao, N; Sherman, T; Ventura, D, 2004
)
0.32
" Assessments included pharmacokinetic as well as safety parameters."( Lack of pharmacokinetic or pharmacodynamic interaction between memantine and donepezil.
Abramowitz, WT; Periclou, AP; Rao, N; Sherman, T; Ventura, D, 2004
)
0.32
"Data from 19 subjects who completed the study indicated no significant pharmacokinetic interactions between a single dose of memantine and multiple doses of donepezil."( Lack of pharmacokinetic or pharmacodynamic interaction between memantine and donepezil.
Abramowitz, WT; Periclou, AP; Rao, N; Sherman, T; Ventura, D, 2004
)
0.32
"The pharmacokinetic and pharmacodynamic data from this study indicated a lack of interaction between memantine and donepezil, suggesting that memantine and donepezil may be safely and effectively used in combination."( Lack of pharmacokinetic or pharmacodynamic interaction between memantine and donepezil.
Abramowitz, WT; Periclou, AP; Rao, N; Sherman, T; Ventura, D, 2004
)
0.32
" Bezafibrate and fenofibrate had no significant effect on the peak concentration (Cmax) of repaglinide."( Lack of effect of bezafibrate and fenofibrate on the pharmacokinetics and pharmacodynamics of repaglinide.
Backman, JT; Kajosaari, LI; Laitila, J; Neuvonen, M; Neuvonen, PJ, 2004
)
0.32
"To characterize the pharmacokinetic, pharmacodynamic and safety profiles of donepezil in subjects with moderate renal impairment and matched healthy controls during single-dose and multiple-dose phases."( Steady-state pharmacokinetics and safety of donepezil HCl in subjects with moderately impaired renal function.
Bolton, WK; Cullen, EI; Gutierrez, MJ; Hutman, HW; Kumar, D; Marbury, TC; Nagy, CF; Pratt, RD, 2004
)
0.32
" The pharmacokinetic and pharmacodynamic parameters of donepezil were determined for up to 144 h after the first dose and 168 h after the last dose."( Steady-state pharmacokinetics and safety of donepezil HCl in subjects with moderately impaired renal function.
Bolton, WK; Cullen, EI; Gutierrez, MJ; Hutman, HW; Kumar, D; Marbury, TC; Nagy, CF; Pratt, RD, 2004
)
0.32
"The co-administration of once-daily oral donepezil HCl 5 mg for 15 days and once-daily oral sertraline HCl (50 mg for 5 days increased to 100 mg for 10 days) did not result in any clinically meaningful pharmacokinetic interactions, and no unexpected AEs were observed."( Concurrent administration of donepezil HCl and sertraline HCl in healthy volunteers: assessment of pharmacokinetic changes and safety following single and multiple oral doses.
Cullen, EI; Kumar, D; Nagy, CF; Perdomo, CA; Pratt, RD; Wason, S, 2004
)
0.32
" Plasma concentrations of thioridazine were measured after each dose, and pharmacokinetic parameters were determined."( Repeated dosing with donepezil does not affect the safety, tolerability or pharmacokinetics of single-dose thioridazine in young volunteers.
Boyce, M; Dunn, K; Johnston, A; Ravic, M; Warrington, S, 2004
)
0.32
" Blood samples were collected before, during and after the 15 doses of donepezil HCl for pharmacokinetic (PK) assessments."( Concurrent administration of donepezil HCl and levodopa/carbidopa in patients with Parkinson's disease: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Hahne, WA; Kirby, L; Kumar, D; Okereke, CS; Pratt, RD, 2004
)
0.32
" Pharmacokinetic parameters (C(max), t(max) and AUC) were assessed from plasma drug concentrations measured in blood collected before, during and after administration (for 12 h after risperidone on days 0 and 7, and for 24 h after donepezil HCl on day 7)."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.32
" Pharmacokinetic parameters for risperidone and 9-OH risperidone were not altered in patients with schizophrenia after 7 days of donepezil HCl administration (AUC(0-12 h) standardized by dose: risperidone = 59."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.32
"A nonlinear mixed-effects modelling approach was used to analyse pharmacokinetic and pharmacodynamic data from two Phase I studies of a platelet activating factor (PAF) antagonist under development for the treatment of seasonal allergic rhinitis."( A pharmacokinetic/pharmacodynamic model for a platelet activating factor antagonist based on data arising from Phase I studies.
Aarons, L; Brearley, C; Evans, L, 2005
)
0.33
"Ketoconazole altered the pharmacokinetic profiles of both ebastine and loratadine although the effect was greater for the former drug."( Co-administration of ketoconazole with H1-antagonists ebastine and loratadine in healthy subjects: pharmacokinetic and pharmacodynamic effects.
Chaikin, P; Gillen, MS; Malik, M; Pentikis, H; Rhodes, GR; Roberts, DJ, 2005
)
0.33
"The area under the plasma concentration-time curve from time 0 to infinity [AUC(0-infinity)] and peak concentration in plasma (Cmax) of repaglinide varied 16."( Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics.
Backman, JT; Daly, AK; Eichelbaum, M; Kajosaari, LI; Kivistö, KT; Leathart, JB; Neuvonen, M; Neuvonen, PJ; Niemi, M, 2005
)
0.33
" The analysis was based on phase I pharmacokinetic naratriptan data, sumatriptan pharmacodynamic data, and naratriptan preclinical (animal) potency information, together with general knowledge as to how migraine affects oral absorption."( Uncertainty analysis in pharmacokinetics and pharmacodynamics: application to naratriptan.
Aarons, L; Gueorguieva, I; Nestorov, IA; Rowland, M, 2005
)
0.33
"A previously developed pharmacokinetic (PK)/pharmacodynamic (PD) model for naratriptan disposition and effect was used."( Uncertainty analysis in pharmacokinetics and pharmacodynamics: application to naratriptan.
Aarons, L; Gueorguieva, I; Nestorov, IA; Rowland, M, 2005
)
0.33
" The assay method also shows good specificity to donepezil enantiomers, and it could be successfully applied to its pharmacokinetic studies and to therapeutic drug monitoring."( Stereoselective HPLC assay of donepezil enantiomers with UV detection and its application to pharmacokinetics in rats.
Abdine, HH; Aboul-Enein, HY; Al-Quadeb, BT; Nakashima, K; Radwan, MA, 2006
)
0.33
" These molecules also exhibit superior pharmacological and pharmacokinetic parameters, relative to all GlyT1 inhibitors of the spiropiperidine family, culminating in the identification of 16b with an oral bioavailability of approximately 60%."( 4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.
Alberati, D; Hainzl, D; Jolidon, S; Kurt, A; Pinard, E; Thomas, AW; Zimmerli, D, 2006
)
0.33
" The mean plasma drug concentrations at different time points and the pharmacokinetic parameters before and after piperine administration were compared by Student's t-test."( Effect of piperine on the steady-state pharmacokinetics of phenytoin in patients with epilepsy.
Hota, D; Kharbanda, P; Pandhi, P; Pattanaik, S; Prabhakar, S, 2006
)
0.33
" For pharmacokinetic analysis plasma sampling was performed during the first and second course and assayed using a validated high-performance liquid chromatographic assay with mass spectrometric detection."( Phase I and pharmacokinetic study of halofuginone, an oral quinazolinone derivative in patients with advanced solid tumours.
de Jonge, MJ; Dumez, H; Lacombe, D; Marréaud, S; Punt, CJ; Snyder, D; van Oosterom, A; Verweij, J; Yamaguchi, T; Yarkoni, S, 2006
)
0.33
" Plasma concentration, FXa activity, and coagulation parameters were used to monitor the pharmacokinetic (PK) and pharmacodynamic (PD) profiles of PD 0313052."( Formulation modifications of PD 0313052, a direct Factor Xa Inhibitor, alter pharmacokinetics and pharma-codynamics following subcutaneous administration to rabbits.
A Perrin, L; Chi, L; Gibson, G; Janiczek, N; Juneau, P; Leadley, R; Peng, YW; Ross, D, 2006
)
0.33
" The validated LC/MS/MS method was applied to a pharmacokinetic study in which healthy Chinese volunteers each received a single oral dose of 5 mg donepezil hydrochloride."( Rapid and sensitive determination of donepezil in human plasma by liquid chromatography/tandem mass spectrometry: application to a pharmacokinetic study.
Liao, Q; Liu, D; Wan, J; Xie, Z; Xu, X; Yao, M, 2006
)
0.33
" The developed assay method was successfully applied to a pharmacokinetic study in human volunteers after oral administration of roxatidine acetate hydrochloride at a dose of 75 mg."( Determination of roxatidine in human plasma by liquid chromatography/electrospray mass spectrometry and application to a clinical pharmacokinetic study.
Balthasar, JP; Choi, JW; Hong, DK; Kim, JJ; Shin, BS; Yoo, SD, 2007
)
0.34
"In this study, the development and validation of a high-performance liquid chromatography (HPLC) assay for determination of repaglinide concentration in human plasma for pharmacokinetic studies is described."( Method development and validation of repaglinide in human plasma by HPLC and its application in pharmacokinetic studies.
Gan, SH; Imran, A; Ismail, Z; Ruzilawati, AB; Wahab, MS, 2007
)
0.34
" grapefruit juice) may cause pharmacokinetic interactions."( Drug-drug and food-drug pharmacokinetic interactions with new insulinotropic agents repaglinide and nateglinide.
Scheen, AJ, 2007
)
0.34
" The aim of this study was to evaluate the ability of an artificial neural network (ANN) to predict ApEn overshoot and to evaluate the predictive performance of the pharmacokinetic model, and pharmacodynamic models of ANN with respect to data used."( Population pharmacokinetic and pharmacodynamic models of remifentanil in healthy volunteers using artificial neural network analysis.
Bae, KS; Kang, SH; Kern, SE; Kim, DH; Kim, KM; Lee, H; Lee, SH; Linares, O; Noh, GJ; Poynton, MR, 2007
)
0.34
" A total of 1077 measured remifentanil concentrations and ApEn data, and a total of 24 509 predicted concentrations and ApEn data were used in the pharmacodynamic model A and B of ANN, respectively."( Population pharmacokinetic and pharmacodynamic models of remifentanil in healthy volunteers using artificial neural network analysis.
Bae, KS; Kang, SH; Kern, SE; Kim, DH; Kim, KM; Lee, H; Lee, SH; Linares, O; Noh, GJ; Poynton, MR, 2007
)
0.34
" Pharmacokinetic parameters for these groups were calculated and compared with one another."( Interaction study of aspirin or clopidogrel on pharmacokinetics of donepezil hydrochloride in rats by HPLC-fluorescence detection.
Aboul-Enein, HY; Nakashima, K; Nishiwaki, J; Ohwaki, Y; Wada, M; Yamane, T, 2007
)
0.34
" Pharmacokinetic sampling was measured up to 216 hours after single oral/nasogastric doses of ACP-103 and after the last dose of once-daily oral administration of ACP-103 for 14 days."( Pharmacokinetics, tolerability, and safety of ACP-103 following single or multiple oral dose administration in healthy volunteers.
Davis, RE; Mant, TG; Robbins-Weilert, D; van Kammen, DP; Vanover, KE; Weiner, DM; Wilbraham, DG, 2007
)
0.34
" The aim of this study was to compare the pharmacokinetic and pharmacodynamic properties of lafutidine and famotidine following postprandial oral administration."( Pharmacokinetic and pharmacodynamic properties of lafutidine after postprandial oral administration in healthy subjects: comparison with famotidine.
Hayato, S; Ikawa, K; Morikawa, N; Shimatani, T; Tazuma, S, 2007
)
0.34
" Comparison of the plasma exposure and the elimination half-life of ebastine and carebastine between groups showed no significant differences."( Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.
Noveck, RJ; Preston, RA; Swan, SK, 2007
)
0.34
" No clinically important pharmacokinetic or safety differences were observed between patients with renal impairment and healthy subjects with normal renal function."( Pharmacokinetics and safety of ebastine in healthy subjects and patients with renal impairment.
Noveck, RJ; Preston, RA; Swan, SK, 2007
)
0.34
"To evaluate the population pharmacokinetic characteristics of cilobradine including a covariate analysis based on six phase I trials and to assess the predictive performance of the model developed."( Population Pharmacokinetic Data Analysis of Cilobradine, an I f Channel Blocker.
Fliss, G; Kloft, C; Schaefer, HG; Staab, A; Tillmann, C; Trommeshauser, D, 2008
)
0.35
" We describe an asleep-awake-asleep technique with propofol and remifentanil infusions, with pharmacokinetic simulation to predict the effect-site concentrations and to modulate the infusion rates of both drugs, and bispectral index (BIS) monitoring."( Propofol and remifentanil effect-site concentrations estimated by pharmacokinetic simulation and bispectral index monitoring during craniotomy with intraoperative awakening for brain tumor resection.
Beiras, A; Lobo, F, 2007
)
0.34
"A dose-escalation phase I and pharmacokinetic study of the farnesyltransferase inhibitor lonafarnib (SCH66336) was conducted in children with recurrent or progressive CNS tumors."( Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Cons
Banerjee, A; Belasco, JB; Blaney, SM; Boyett, JM; Broniscer, A; Frank, E; Geyer, JR; Goldman, S; Gururangan, S; Kieran, MW; Kirschmeier, P; Kun, LE; Onar, A; Packer, RJ; Phillips, P; Pollack, IF; Statkevich, P; Turner, CD; Yver, A; Zhu, Y, 2007
)
0.34
" We have investigated the replacement or the modification of this group, and we suggest that the pKa of this part of the molecules influences both the antiviral activity and the pharmacokinetic profile."( Selection of a respiratory syncytial virus fusion inhibitor clinical candidate, part 1: improving the pharmacokinetic profile using the structure-property relationship.
Andries, K; Arnoult, E; Bonfanti, JF; Doublet, F; Fortin, J; Gevers, T; Guillemont, J; Janssens, F; Janssens, P; Lacrampe, J; Muller, P; Queguiner, L; Sommen, C; Szel, H; Timmerman, P; Wigerinck, P; Willebrords, R; Wuyts, K, 2007
)
0.34
" Pharmacokinetic data suggest an increase in the plasma Css in relation to the escalation of FK866."( The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor.
Burk, K; Hanauske, AR; Holen, K; Hollywood, E; Saltz, LB, 2008
)
0.35
" Blood samples were collected from 1 to 144 hours post-dose for pharmacokinetic analysis."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.34
" Nine of the 19 patients completed both treatment cycles and were used for pharmacokinetic assessment."( Effect of food on the pharmacokinetics of lonafarnib (SCH 66336) following single and multiple doses.
Cutler, DL; Statkevich, P; Zhu, Y, 2007
)
0.34
" Intrasubject variability in the pharmacokinetic parameters was less pronounced after multiple dosing (17%) than that after single dosing (33%) of lonafarnib."( Effect of food on the pharmacokinetics of lonafarnib (SCH 66336) following single and multiple doses.
Cutler, DL; Statkevich, P; Zhu, Y, 2007
)
0.34
" Css is strongly affected by weight and age with Minto's pharmacokinetic parameters of remifentanil."( [Pharmacokinetic simulations of remifentanil].
Kazama, T; Masui, K, 2007
)
0.34
"This study describes a pharmacodynamic model during general anaesthesia in children relating the bispectral index (BIS) response to the anaesthetic dosing of propofol, fentanyl, and remifentanil."( Pharmacodynamic modelling of the bispectral index response to propofol-based anaesthesia during general surgery in children.
Ammon, C; Fechner, J; Ihmsen, H; Jeleazcov, C; Schmidt, J; Schüttler, J; Schwilden, H, 2008
)
0.35
" The pharmacodynamic parameters were estimated by non-linear regression analysis."( Pharmacodynamic modelling of the bispectral index response to propofol-based anaesthesia during general surgery in children.
Ammon, C; Fechner, J; Ihmsen, H; Jeleazcov, C; Schmidt, J; Schüttler, J; Schwilden, H, 2008
)
0.35
" We performed in vitro characterization of the device before developing a population pharmacokinetic model for sevoflurane administration with the AnaConDa, and retrospectively testing its performance (internal validation)."( Population pharmacokinetics of sevoflurane in conjunction with the AnaConDa: toward target-controlled infusion of volatiles into the breathing system.
Bouillon, T; Enlund, M; Kietzmann, D; Meineke, I; Züchner, K, 2008
)
0.35
" The individual pharmacokinetic parameters were obtained and tested for covariate relationships."( Population pharmacokinetics of sevoflurane in conjunction with the AnaConDa: toward target-controlled infusion of volatiles into the breathing system.
Bouillon, T; Enlund, M; Kietzmann, D; Meineke, I; Züchner, K, 2008
)
0.35
"In vitro studies assessed the contribution of the device to the pharmacokinetic model."( Population pharmacokinetics of sevoflurane in conjunction with the AnaConDa: toward target-controlled infusion of volatiles into the breathing system.
Bouillon, T; Enlund, M; Kietzmann, D; Meineke, I; Züchner, K, 2008
)
0.35
" The apparent volume of distribution of the central compartment, the apparent volume of distribution at steady state, the clearance, and the terminal half-life (median [range]) were 1,596 (1,164 to 2,111) and 567 (278 to 641) mL/kg, 7,632 (2,284 to 76,039) and 1,651 (446 to 29,229) mL/kg, 766 (408 to 1,473) and 371 (197 to 472) mL/min/kg, and 17."( Pharmacokinetics of remifentanil in conscious cats and cats anesthetized with isoflurane.
Brosnan, RJ; Pypendop, BH; Siao, KT; Stanley, SD, 2008
)
0.35
"This study was conducted to evaluate the pharmacokinetic (PK), pharmacodynamic (PD), and tolerability profiles and explore the efficacy of multiple oral doses of alogliptin in patients with T2D."( Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Mekki, QA; Wann, ER, 2008
)
0.35
" Blood and urine were collected over 72 hours after dosing for pharmacokinetic analysis and determination of plasma DPP-4 inhibition and active glucagon-like peptide -1(GLP-1) concentrations."( Pharmacokinetics, pharmacodynamics, and tolerability of single increasing doses of the dipeptidyl peptidase-4 inhibitor alogliptin in healthy male subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Mekki, QA; Wann, ER, 2008
)
0.35
" Optimization of the most tractable hits gave a series of compounds showing inhibition of cholesterol biosynthesis at 2mg/kg in the rat with distinct pharmacokinetic profiles."( Design and evaluation of a novel series of 2,3-oxidosqualene cyclase inhibitors with low systemic exposure, relationship between pharmacokinetic properties and ocular toxicity.
Bouillot, A; Boullay, AB; Coste, H; Dodic, N; Donche, F; Fouchet, MH; Issandou, M; Junot, C; Magny, SD; Martin, C; Potvain, F; Walker, M, 2008
)
0.35
" This method has the lowest lower limit of quantitation (LLOQ) reported to date for flavopiridol, and it allows for more accurate determination of terminal phase concentrations and improved pharmacokinetic parameter estimation in patients receiving an active dosing schedule of flavopiridol."( Development and validation of a sensitive liquid chromatography/mass spectrometry method for quantitation of flavopiridol in plasma enables accurate estimation of pharmacokinetic parameters with a clinically active dosing schedule.
Albanese, KA; Byrd, JC; Dalton, JT; Farley, KL; Grever, MR; Johnston, JS; Lin, TS; Phelps, MA; Rozewski, DM, 2008
)
0.35
" The additional pharmacodynamic benefit of the combination dose was not because of an alteration in the pharmacokinetics of either agent but is likely the result of the complementary mechanisms of pharmacologic action of the two drugs."( Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret.
Bambal, R; Davis, CB; Gontarek, RR; Han, C; King, AG; Mencken, T; Minthorn, E; Rominger, D; Shu, A, 2008
)
0.35
"The purpose of this study was to estimate the pharmacokinetic parameters and tissue distribution of positively charged stearylamine (LN-P-SA) and pegylated lipid nanospheres (LN-P-PEG) of piperine in BALB/c mice."( Pharmacokinetics and tissue distribution of piperine lipid nanospheres.
Veerareddy, PR; Vobalaboina, V, 2008
)
0.35
"The aim of this study was to construct the population pharmacokinetic model in Chinese adult patients and to characterize the factors that affect the parameters of remifentanil pharmacokinetics."( Population pharmacokinetics study of remifentanil in Chinese adult patients determined by an LC-MS/MS method.
Duan, L; Yang, L; Zhai, S; Zhang, C; Zhang, L; Zhang, X, 2008
)
0.35
" Meanwhile, population modeling was performed using the NONMEM (nonlinear mixed-effect modeling) program with a 2-compartment pharmacokinetic model."( Population pharmacokinetics study of remifentanil in Chinese adult patients determined by an LC-MS/MS method.
Duan, L; Yang, L; Zhai, S; Zhang, C; Zhang, L; Zhang, X, 2008
)
0.35
" The population pharmacokinetic results indicated that total bilirubin, age, alkaline phosphatase activity and gender significantly affected the parameters of remifentanil."( Population pharmacokinetics study of remifentanil in Chinese adult patients determined by an LC-MS/MS method.
Duan, L; Yang, L; Zhai, S; Zhang, C; Zhang, L; Zhang, X, 2008
)
0.35
" The population model was acceptable and would be helpful for clinicians to assess the remifentanil pharmacokinetic parameters based on patient's specific demographic characteristics."( Population pharmacokinetics study of remifentanil in Chinese adult patients determined by an LC-MS/MS method.
Duan, L; Yang, L; Zhai, S; Zhang, C; Zhang, L; Zhang, X, 2008
)
0.35
" The present method was successfully applied to the pharmacokinetic study of donepezil after oral dose of donepezil hydrochloride (10 mg tablet) to male healthy volunteers."( Hydrophilic interaction chromatography-tandem mass spectrometry of donepezil in human plasma: application to a pharmacokinetic study of donepezil in volunteers.
Ji, HY; Kim, HY; Lee, HS; Lee, HW; Lee, KC; Lee, MH; Park, EJ; Park, ES, 2008
)
0.35
" Our data suggest that thioperamide, at least at 10 mg/kg, increases cocaine-induced locomotion through the combination of pharmacokinetic effects and the blockade of H3 receptors located on non-histaminergic neurons."( Effects of the H3 receptor inverse agonist thioperamide on cocaine-induced locomotion in mice: role of the histaminergic system and potential pharmacokinetic interactions.
Alleva, L; Brabant, C; Grisar, T; Jatlow, P; Lakaye, B; Lin, JS; Ohtsu, H; Picciotto, MR; Quertemont, E; Tirelli, E, 2009
)
0.35
"The AUC(0-infinity) and Cmax of repaglinide were 32% (P=0."( Effects of the SLCO1B1*1B haplotype on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide.
Backman, JT; Kalliokoski, A; Neuvonen, PJ; Niemi, M, 2008
)
0.35
" We now report full pharmacokinetic (PK) data, correlations of PK with clinical outcomes, and final response and progression-free survival (PFS)."( Clinical response and pharmacokinetics from a phase 1 study of an active dosing schedule of flavopiridol in relapsed chronic lymphocytic leukemia.
Blum, KA; Brooker-McEldowney, M; Byrd, JC; Dalton, JT; Farley, KL; Fischer, B; Grever, MR; Heerema, NA; Hurh, E; Jarjoura, D; Johnson, AJ; Lin, TS; Mitchell, SM; Moran, ME; Phelps, MA; Rozewski, DM; Schaaf, LJ; Wu, D, 2009
)
0.35
" The pharmacokinetic properties of the compounds were predicted by the physico-chemical parameters."( [Physico-chemical profiling of centrally acting molecules for prediction of pharmacokinetic properties].
Deák, K, 2008
)
0.35
" The discovery of 4,4-disubstituted piperidine inhibitors of GlyT1 which exhibit improved pharmacokinetic properties, including oral bioavailability, is discussed."( Discovery of GlyT1 inhibitors with improved pharmacokinetic properties.
Gibson, C; Hartman, GD; Jacobson, MA; Kinney, GG; Leister, WH; Lemaire, W; Lindsley, CW; Ma, BK; O'Brien, J; Pettibone, DJ; Polsky-Fisher, SL; Smith, S; Sur, C; Tiller, PR; Williams, DL; Wisnoski, DD; Wolkenberg, SE; Zhao, Z, 2009
)
0.35
" Log-transformed area under the curve (AUC) and Cmax were statistically analyzed by performing an analysis of variance."( Effect of casopitant, a novel NK-1 antagonist, on the pharmacokinetics of dolasetron and granisetron.
Adams, LM; Johnson, B; Kirby, LC; Lebowitz, P; Stoltz, R; Yue, L; Zhang, K, 2009
)
0.35
"The primary objective of this study was to demonstrate the use of stable isotope (SI)-labeled compound as an approach for pharmacokinetic analysis such as fraction absorbed, hepatic extraction ratio, and fraction metabolized from the parent drug to a metabolite."( Application of stable isotope methodology in the evaluation of the pharmacokinetics of (S,S)-3-[3-(methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride in rats.
Bower, J; Heath, TG; Kimoto, E; Romero, D; Skaptason, J; Toth, LN; Yamazaki, S, 2009
)
0.35
" The pharmacokinetic parameters were compared by Students t-test."( Pharmacokinetic interaction of single dose of piperine with steady-state carbamazepine in epilepsy patients.
Hota, D; Kharbanda, P; Pandhi, P; Pattanaik, S; Prabhakar, S, 2009
)
0.35
" Cmax and C2 values tended to increase whereas C0 remained unaffected."( Rimonabant affects cyclosporine a, but not tacrolimus pharmacokinetics in renal transplant recipients.
Amundsen, R; Asberg, A; Bergan, S; Hartmann, A; Midtvedt, K; Robertsen, I; Vethe, NT, 2009
)
0.35
" Population pharmacokinetic modeling was performed using nonlinear mixed-effects modeling (NONMEM)."( Population pharmacokinetics of remifentanil in patients undergoing orthotopic liver transplantation.
Bi, SS; Duan, LP; Lu, W; Yang, L; Zhai, SD; Zhang, LP; Zhang, XH, 2009
)
0.35
" The pharmacokinetic parameters were not influenced by age, gender, operative phase, blood temperature, rehydration volume, or blood loss volume during sampling."( Population pharmacokinetics of remifentanil in patients undergoing orthotopic liver transplantation.
Bi, SS; Duan, LP; Lu, W; Yang, L; Zhai, SD; Zhang, LP; Zhang, XH, 2009
)
0.35
" Here, we report the results of a preliminary pharmacokinetic study of masitinib in cats which showed a good bioavailability of ~60% in both sexes."( Pharmacokinetics of masitinib in cats.
Bader, T; Bellamy, F; Hermine, O; Moussy, A, 2009
)
0.35
" Potential pharmacokinetic (PK) drug-drug interactions of alogliptin with pioglitazone or glyburide were evaluated in healthy adults."( Coadministration of pioglitazone or glyburide and alogliptin: pharmacokinetic drug interaction assessment in healthy participants.
Fleck, P; Karim, A; Laurent, A; Mekki, Q; Munsaka, M; Wann, E, 2009
)
0.35
"To model the pharmacokinetic and pharmacodynamic relationship of bilastine, a new histamine H(1) receptor antagonist, from single- and multiple-dose studies in healthy adult subjects."( Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.
de la Fuente, L; Jauregizar, N; Leal, N; Lucero, ML; Rodríguez, M; Sologuren, A, 2009
)
0.35
"The pharmacokinetic model was developed from different single-dose and multiple-dose studies."( Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.
de la Fuente, L; Jauregizar, N; Leal, N; Lucero, ML; Rodríguez, M; Sologuren, A, 2009
)
0.35
"Pharmacokinetic and pharmacodynamic relationships of bilastine were reliably described with the use of an indirect response pharmacodynamic model; this led to an accurate prediction of the pharmacodynamic activity of bilastine."( Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine.
de la Fuente, L; Jauregizar, N; Leal, N; Lucero, ML; Rodríguez, M; Sologuren, A, 2009
)
0.35
" Pharmacokinetic analysis revealed that PF-00885706 has a low to moderate volume of distribution and the complete absorption in dogs."( Pharmacological characterization and determination of pharmacokinetic and pharmacodynamic relationship of PF-00885706, a novel partial agonist selective for the 5-HT(4) receptor.
Eda, H; Kimura, N; Komada, T; Matsuura, T; Mikami, T; Nakai, Y; Ohmi, T; Sakakibara, M; Sugimoto, H; Suzuki, K; Toga, T, 2009
)
0.35
"The aim of this study was to examine the pharmacokinetic and pharmacodynamic profile of propofol during propofol remifentanil and propofol - alfentanil anaesthesia, when monitored by SFx."( Pharmacokinetics and pharmacodynamics of propofol during propofol-alfentanil and propofol-remifentanil total intravenous anaesthesia monitored by spectral frequency index.
Bienert, A; Grabowski, T; Grzeskowiak, E; Kusza, K; Zaba, Z, 2009
)
0.35
" The remifentanil and alfentanil groups were compared in relation to pharmacokinetic and pharmacodynamic parameters of propofol and a t-test was used for statistical analysis."( Pharmacokinetics and pharmacodynamics of propofol during propofol-alfentanil and propofol-remifentanil total intravenous anaesthesia monitored by spectral frequency index.
Bienert, A; Grabowski, T; Grzeskowiak, E; Kusza, K; Zaba, Z, 2009
)
0.35
" We demonstrate the feasibility of our approach with the development of a system that synthesizes pharmacokinetic pathways."( Synthesis of pharmacokinetic pathways through knowledge acquisition and automated reasoning.
Anwar, S; Baral, C; Hakenberg, J; Liang, S; Tari, L, 2010
)
0.36
" This study investigated (1) the effect of food on alogliptin pharmacokinetics and tolerability and (2) pharmacokinetic interactions between alogliptin and metformin or cimetidine and tolerability of alogliptin when administered with either drug."( Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Li, X; Mekki, Q; Wann, E, 2010
)
0.36
" Pharmacokinetic parameters were determined after the last dose in each period."( Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Li, X; Mekki, Q; Wann, E, 2010
)
0.36
"In a previous article, we showed that the pharmacokinetic set of remifentanil used for target-controlled infusion (TCI) might be biased in obese patients because it incorporates flawed equations for the calculation of lean body mass (LBM), which is a covariate of several pharmacokinetic parameters in this set."( Predictive performance of the 'Minto' remifentanil pharmacokinetic parameter set in morbidly obese patients ensuing from a new method for calculating lean body mass.
Albertin, A; Aldegheri, G; Di Candia, D; Gigli, F; La Colla, G; La Colla, L; Porta, A, 2010
)
0.36
" The intervention included manually controlled continuous infusion of remifentanil during the surgery and analysis of arterial blood samples to determine the arterial remifentanil concentration, to be compared with concentrations predicted by either the unadjusted or the adjusted pharmacokinetic set."( Predictive performance of the 'Minto' remifentanil pharmacokinetic parameter set in morbidly obese patients ensuing from a new method for calculating lean body mass.
Albertin, A; Aldegheri, G; Di Candia, D; Gigli, F; La Colla, G; La Colla, L; Porta, A, 2010
)
0.36
" The performance (in terms of the MDPE and MDAPE) of the corrected pharmacokinetic set was better than that of the uncorrected one."( Predictive performance of the 'Minto' remifentanil pharmacokinetic parameter set in morbidly obese patients ensuing from a new method for calculating lean body mass.
Albertin, A; Aldegheri, G; Di Candia, D; Gigli, F; La Colla, G; La Colla, L; Porta, A, 2010
)
0.36
"This study compared the blood concentrations of remifentanil obtained in a previous clinical investigation with the predicted remifentanil concentrations produced by different pharmacokinetic models: a non-linear mixed effects model created by the software NONMEM; an artificial neural network (ANN) model; a support vector machine (SVM) model; and multi-method ensembles."( Machine learning methods applied to pharmacokinetic modelling of remifentanil in healthy volunteers: a multi-method comparison.
Boo, YK; Choi, BM; Hong, SO; Kang, SH; Kim, YM; Noh, GJ; Park, IS; Poynton, MR,
)
0.13
" Through integration of in vitro and in vivo pharmacokinetic data and antitumor efficacy in nude mice, human pharmacokinetics and efficacious doses were projected for BMS-690514."( Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2.
Christopher, L; Gavai, A; Marathe, P; Rodrigues, D; Sleczka, B; Tang, Y; Wong, T; Zhang, H, 2010
)
0.36
"To estimate population pharmacokinetic parameters of repaglinide in 121 healthy Malaysian volunteers."( Population pharmacokinetic modelling of repaglinide in healthy volunteers by using Non-Parametric Adaptive Grid Algorithm.
Gan, SH; Mohd Suhaimi, AW; Ruzilawati, AB, 2010
)
0.36
" The parametric Iterative Two-Stage Bayesian Population Model (it2b) program followed by the Non-Parametric Adaptive Grid (npag) program was used to determine a population pharmacokinetic modelling of repaglinide."( Population pharmacokinetic modelling of repaglinide in healthy volunteers by using Non-Parametric Adaptive Grid Algorithm.
Gan, SH; Mohd Suhaimi, AW; Ruzilawati, AB, 2010
)
0.36
"In this first report, specifically on the population pharmacokinetic modelling of repaglinide, the data generated should help us to better understand appropriate dosage-regimens for the drug."( Population pharmacokinetic modelling of repaglinide in healthy volunteers by using Non-Parametric Adaptive Grid Algorithm.
Gan, SH; Mohd Suhaimi, AW; Ruzilawati, AB, 2010
)
0.36
"04) and the mean half-life was 33."( CYP3A4 genetic polymorphism influences repaglinide's pharmacokinetics.
Gan, SH; Ruzilawati, AB, 2010
)
0.36
" Pharmacokinetic parameters were determined using noncompartmental methods."( Pharmacokinetics of vandetanib in subjects with renal or hepatic impairment.
Langmuir, P; Martin, P; Molz, KH; Oliver, S; Read, J; Smith, R; Weil, A, 2010
)
0.36
"The purpose of this review is to examine published non-clinical literature on the antihistamine bepotastine besilate, including pharmacokinetic and pharmacologic properties."( Non-clinical pharmacology, pharmacokinetics, and safety findings for the antihistamine bepotastine besilate.
Gow, JA; Klier, SM; McCue, SL; McNamara, TR; Salapatek, AM; Williams, JI, 2010
)
0.36
" Diclazuril and halofuginone resulted in a significant short distribution half-life (t(½α)) (7."( Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone.
Amer, AM; Atef, M; El-Gendi, AY; Kamel, GM, 2010
)
0.36
" Oral administration of 13 1-aryl-3-(1-acylpiperidin-4-yl)urea inhibitors in mice revealed substantial improvements in pharmacokinetic parameters over previously reported 1-adamantylurea based inhibitors."( 1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain.
Hammock, BD; Inceoglu, B; Jones, PD; Liu, JY; Morisseau, C; Rose, TE; Sanborn, JR, 2010
)
0.36
" A two-compartment population pharmacokinetic model estimating oral clearance, between-patient variability in oral clearance, central volume of distribution, and residual variability in combination with historical estimates of first-order absorption rate constant, intercompartmental clearance, and peripheral volume of distribution adequately described the sparse MPA data."( Population pharmacokinetic analysis of mycophenolic acid coadministered with either tasocitinib (CP-690,550) or tacrolimus in adult renal allograft recipients.
Busque, S; Chan, G; Krishnaswami, S; Lamba, M; Melcher, M; Tafti, B, 2010
)
0.36
" Blood samples were obtained for pharmacokinetic and pharmacodynamic studies."( A dose-finding, pharmacokinetic and pharmacodynamic study of a novel schedule of flavopiridol in patients with advanced solid tumors.
Arbogast, D; Baiocchi, R; Bekaii-Saab, T; Byrd, JC; Campbell, A; Doyle, A; Grever, MR; Lai, JP; Lustberg, ME; Ni, W; Phelps, MA; Ramaswamy, B; Shah, MH; Wei, L; Wilkins, D; Wolfson, A, 2012
)
0.38
"To describe the pharmacodynamic interaction between propofol and remifentanil in suppressing somatic and hemodynamic responses to electrical tetanus stimuli (ETS) during induction of intravenous anesthesia with response surface method."( [Pharmacodynamic interaction between propofol and remifentanil on the tolerance response to electrical tetanus stimuli].
Bi, SS; Guo, XY; Lu, W; Wei, B; Yang, L; Zhang, LP, 2010
)
0.36
" The pharmacodynamic interaction between propofol and remifentanil was analyzed by response surface method."( [Pharmacodynamic interaction between propofol and remifentanil on the tolerance response to electrical tetanus stimuli].
Bi, SS; Guo, XY; Lu, W; Wei, B; Yang, L; Zhang, LP, 2010
)
0.36
"Response surface method characterized the pharmacodynamic interactions between propofol (0-9 mg/L) and remifentanil (0-10 μg/L) qualitatively and quantitatively."( [Pharmacodynamic interaction between propofol and remifentanil on the tolerance response to electrical tetanus stimuli].
Bi, SS; Guo, XY; Lu, W; Wei, B; Yang, L; Zhang, LP, 2010
)
0.36
"Response surface method can analyze the pharmacodynamic interactions qualitatively and quantitatively."( [Pharmacodynamic interaction between propofol and remifentanil on the tolerance response to electrical tetanus stimuli].
Bi, SS; Guo, XY; Lu, W; Wei, B; Yang, L; Zhang, LP, 2010
)
0.36
"the purpose of this review is to describe the pharmacokinetic profile of iloperidone and its clinical implications in the treatment of schizophrenia."( Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion.
Citrome, L, 2010
)
0.36
"time to peak plasma concentration occurs in 2 - 4 h but elimination half-life is 18 h for extensive CYP2D6 metabolizers and 33 h for poor CYP2D6 metabolizers, suggesting that once or twice daily dosing would be feasible."( Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion.
Citrome, L, 2010
)
0.36
" As many promising targeted therapies affect kinase activity of specific enzymes involved in cancer transformation, H1 phosphorylation can serve as potential pharmacodynamic marker for drug activity within the cell."( Assaying pharmacodynamic endpoints with targeted therapy: flavopiridol and 17AAG induced dephosphorylation of histone H1.5 in acute myeloid leukemia.
Byrd, JC; Freitas, MA; Grever, M; Harshman, SW; Liu, S; Marcucci, G; Ren, C; Sallans, L; Wang, L; Xu, H, 2010
)
0.36
" Intravenous and oral 6-h blood sampling profiles in old (30 months old) and young (7 months old) rats revealed pharmacokinetic changes similar to those in humans with an approximately 40% increase in C(max) of galantamine and prolonged t(1/2) (1."( Pharmacokinetic and pharmacodynamic properties of cholinesterase inhibitors donepezil, tacrine, and galantamine in aged and young Lister hooded rats.
Aw, CC; Browne, ER; Chen, CP; Goh, CW; Lee, JH, 2011
)
0.37
" The proposed method was successfully applied for the estimation of the drug in real time plasma samples for pharmacokinetic studies."( A rapid and sensitive LC-MS/MS method for quantification of donepezil and its active metabolite, 6-o-desmethyl donepezil in human plasma and its pharmacokinetic application.
Damaramadugu, R; Inamadugu, JK; Karra, VK; Kondreddy, N; Pilli, NR; Rao, JV, 2011
)
0.37
" The physicochemical properties of MNP001, including solubility, pKa, Log P, plasma protein binding and plasma/blood partitioning, were determined to support the pharmacokinetic characterization."( Preclinical pharmacokinetics and metabolism of MNP001, a piperidine analog of 3-carbamyl compounds.
Fox, LM; Wang, D; Xia, B, 2011
)
0.37
" Then selected volunteers took part in the clinical pharmacokinetic study, receiving 2 mg repaglinide."( Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers.
Chen, X; Fan, H; Fang, F; Han, D; He, J; Li, N; Li, T; Lu, Y; Qiu, Z; Sun, W; Yu, Y; Zhao, D; Zheng, J, 2011
)
0.37
"SLCO1B1*1B/*1B genotype is associated with reduced pharmacokinetic exposure after a single dose oral administration of 2 mg repaglinide, including decreased AUC(0-∞) and increased clearance of repaglinide."( Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers.
Chen, X; Fan, H; Fang, F; Han, D; He, J; Li, N; Li, T; Lu, Y; Qiu, Z; Sun, W; Yu, Y; Zhao, D; Zheng, J, 2011
)
0.37
" Pharmacokinetic parameters were determined using non-compartmental methods."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
0.37
" The pharmacokinetics of vandetanib in Chinese, Western, and Japanese patients were compared through a combined population pharmacokinetic model."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
" Population pharmacokinetic analysis suggests that vandetanib pharmacokinetics appear to be comparable in Chinese, Western, and Japanese patients."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
"The pharmacokinetic properties of vandetanib in these Chinese patients were characterized by low plasma clearance of approximately 8 L/h, a long half-life of approximately 8 to 10 days, and an accumulation of approximately 8-fold to 15-fold on multiple dosing."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
"The purpose of this study was to compare the pharmacokinetic characteristics of orally disintegrating (test) and conventional (reference) donepezil formulations to satisfy the regulatory requirement for marketing."( Pharmacokinetic comparison of orally disintegrating and conventional donepezil formulations in healthy Korean male subjects: a single-dose, randomized, open-label, 2-sequence, 2-period crossover study.
Kim, C; Kim, KA; Lim, JL; Park, JY, 2011
)
0.37
" Pharmacokinetic parameters, including C(max) and AUC, were determined by noncompartmental analysis."( Pharmacokinetic comparison of orally disintegrating and conventional donepezil formulations in healthy Korean male subjects: a single-dose, randomized, open-label, 2-sequence, 2-period crossover study.
Kim, C; Kim, KA; Lim, JL; Park, JY, 2011
)
0.37
" No significant differences in pharmacokinetic parameters between the 2 formulations were observed."( Pharmacokinetic comparison of orally disintegrating and conventional donepezil formulations in healthy Korean male subjects: a single-dose, randomized, open-label, 2-sequence, 2-period crossover study.
Kim, C; Kim, KA; Lim, JL; Park, JY, 2011
)
0.37
"This study found that the test and reference formulations met the regulatory criteria for pharmacokinetic equivalence in these fasting healthy Korean male subjects."( Pharmacokinetic comparison of orally disintegrating and conventional donepezil formulations in healthy Korean male subjects: a single-dose, randomized, open-label, 2-sequence, 2-period crossover study.
Kim, C; Kim, KA; Lim, JL; Park, JY, 2011
)
0.37
"In all subjects, SJW had no effect on the total area under the plasma concentration-time curve from time zero to infinity (AUC(∞)), the peak plasma concentration (C(max)) or the elimination half-life (t(½)) of repaglinide."( The pregnane X receptor agonist St John's Wort has no effects on the pharmacokinetics and pharmacodynamics of repaglinide.
Chen, WQ; Fan, L; Guo, D; Liu, YL; Liu, ZQ; Sheng, D; Tan, ZR; Zhang, W; Zhou, G; Zhou, HH, 2011
)
0.37
"Drug development is a high-risk and high failure enterprise, and studies that provide an early read on the pharmacodynamic activity of novel compounds could save time and money, increasing the efficiency of the drug development process."( The scopolamine model as a pharmacodynamic marker in early drug development.
Abi-Saab, W; Baker, JD; Lenz, RA; Locke, C; Mohler, EG; Rueter, LE; Saltarelli, MD; Wesnes, K, 2012
)
0.38
"Preclinical and clinical experiments were designed to examine the utility of the scopolamine-induced cognitive impairment model in predicting pharmacodynamic signals of putatively procognitive compounds, utilizing the acetylcholinesterase inhibitor donepezil for illustration."( The scopolamine model as a pharmacodynamic marker in early drug development.
Abi-Saab, W; Baker, JD; Lenz, RA; Locke, C; Mohler, EG; Rueter, LE; Saltarelli, MD; Wesnes, K, 2012
)
0.38
"These findings suggest that reversal of scopolamine-induced cognitive impairment is a viable model for predicting pharmacodynamic signals of procognitive compounds in both animals and humans."( The scopolamine model as a pharmacodynamic marker in early drug development.
Abi-Saab, W; Baker, JD; Lenz, RA; Locke, C; Mohler, EG; Rueter, LE; Saltarelli, MD; Wesnes, K, 2012
)
0.38
" Venous blood samples were taken prior to and following oral dosing up to 24 h for a pharmacokinetic study of casopitant concentration in plasma."( A pharmacokinetic PET study of NK₁ receptor occupancy.
Bani, M; Cunningham, VJ; Fernandes, SA; Gomeni, R; Gunn, RN; Rabiner, EA; Ratti, E; Zamuner, S, 2012
)
0.38
" Despite high metabolic stability, pharmacokinetic evaluation revealed poor mice exposure; therefore, a second phase of optimization was required."( Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors.
Baulard, AR; Blondiaux, N; Brodin, P; Christophe, T; Déprez, B; Desroses, M; Flament, MP; Flipo, M; Jeon, HK; Lecat-Guillet, N; Leroux, F; Locht, C; Mathys, V; Piveteau, C; Siepmann, J; Soror, SH; Villemagne, B; Villeret, V; Willand, N; Wintjens, R; Wohlkönig, A, 2012
)
0.38
" The influence of continuous (body weight, age, blood pressure, heart rate and blood oxygenation, serum protein, the erythrocyte count, hemoglobin and hematocrit, serum creatinine and creatinine clearance) and categorical (gender and the type of opioid) covariates on the pharmacokinetic and pharmacodynamic parameters was investigated."( Influence of demographic factors, basic blood test parameters and opioid type on propofol pharmacokinetics and pharmacodynamics in ASA I-III patients.
Bienert, A; Grześkowiak, E; Kusza, K; Marciniak, R; Wiczling, P; Wolc, A; Zaba, C; Zaba, Z, 2011
)
0.37
" Blood samples were collected for pharmacokinetic analysis for up to 28 days after the dose (Studies A and B) and 42 days after the dose (Study C)."( Pharmacokinetics of vandetanib: three phase I studies in healthy subjects.
Clarke, D; Giles, P; Hutchison, M; Kennedy, SJ; Martin, P; Oliver, S; Partridge, E, 2012
)
0.38
" Pharmacokinetic parameters were consistent across all studies (Studies A and C, vandetanib 800 mg: geometric mean CL/F, 13."( Pharmacokinetics of vandetanib: three phase I studies in healthy subjects.
Clarke, D; Giles, P; Hutchison, M; Kennedy, SJ; Martin, P; Oliver, S; Partridge, E, 2012
)
0.38
" The pharmacokinetic parameters of repaglinide and blood glucose concentrations were also determined in rats after oral (0."( Effects of efonidipine on the pharmacokinetics and pharmacodynamics of repaglinide: possible role of CYP3A4 and P-glycoprotein inhibition by efonidipine.
Choi, DH; Choi, JS; Li, C, 2012
)
0.38
" We constructed physiologically based pharmacokinetic (PBPK) models for 3 nonrenally eliminated drugs (sildenafil, repaglinide, and telithromycin)."( Evaluation of exposure change of nonrenally eliminated drugs in patients with chronic kidney disease using physiologically based pharmacokinetic modeling and simulation.
Abernethy, DR; Arya, V; Atkinson, AJ; Berglund, EG; Grillo, JA; Huang, SM; Lesko, LJ; Pang, KS; Reynolds, KS; Song, P; Sugiyama, Y; Vieira, Mde L; Wu, TC; Zhang, L; Zhao, P; Zheng, JH, 2012
)
0.38
" In a single-dose pharmacokinetic (PK) study in pediatric patients aged between 6 and 14 years with acid-related diseases, 37."( Pharmacokinetics of the H(2) blocker roxatidine acetate hydrochloride in pediatric patients, in comparison with healthy adult volunteers.
Azuma, R; Kawashima, H; Miyazawa, K; Nagao, K; Nakamura, H; Sato, I, 2012
)
0.38
"The predictive power of using in vitro systems in combination with physiologically based pharmacokinetic (PBPK) modeling to elucidate the relative importance of metabolism and carrier-mediated transport for the pharmacokinetics was evaluated using repaglinide as a model compound and pig as the test system."( The pharmacokinetics and hepatic disposition of repaglinide in pigs: mechanistic modeling of metabolism and transport.
Bredberg, U; Lennernäs, H; Sjögren, E, 2012
)
0.38
" The mean AUCs and peak plasma concentration were higher in subjects with the 521TC allele than in those with the OATP1B1 521TT allele, and the OATP1B1 388A allele is associated with a reduced trend of pharmacokinetic exposure; however, these trends were not statistically significant."( The Influence of MDR1 G2677T/a genetic polymorphisms on the pharmacokinetics of repaglinide in healthy Chinese volunteers.
Cui, YM; Xiang, Q; Yan, L; Zhao, X; Zhou, Y, 2012
)
0.38
"We attempted to establish and validate an in vivo pharmacodynamic (PD) rabbit model to screen tachykinin NK(2) receptor (NK(2)-R) antagonists using pharmacological and pharmacokinetic (PK)/PD analyses."( Establishment and validation of a rabbit model for in vivo pharmacodynamic screening of tachykinin NK2 antagonists.
Fujioka, Y; Imanishi, A; Inatomi, N; Kamiguchi, H; Kawamoto, M; Matsumoto-Okano, S; Miura, K; Nishikawa, Y; Tanaka, T; Tsukimi, Y; Yamaguchi, M, 2012
)
0.38
" Pharmacokinetic-pharmacodynamic (PK-PD) modeling was used to relate GDC-0973 plasma and tumor concentrations, tumor pharmacodynamics and antitumor efficacy to establish pharmacokinetic endpoints and predict active doses in the clinic."( Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.
Aftab, BT; Aoyama, R; Belvin, M; Choo, EF; Del Rosario, G; Hoeflich, KP; Lam, ST; Lee, L; Li, C; Martini, JF; Peterson, A; Prescott, J; Shi, Y; Vernillet, L; Ware, JA; Wong, H; Yu, P, 2012
)
0.38
"GDC-0973 showed a sustained tumor pharmacodynamic response due to longer residence in tumor than in plasma."( Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.
Aftab, BT; Aoyama, R; Belvin, M; Choo, EF; Del Rosario, G; Hoeflich, KP; Lam, ST; Lee, L; Li, C; Martini, JF; Peterson, A; Prescott, J; Shi, Y; Vernillet, L; Ware, JA; Wong, H; Yu, P, 2012
)
0.38
" Pharmacokinetic (PK) plasma samples are generally taken from a parallel group of animals to avoid disruption of the behavioral pharmacodynamic (PD) endpoint."( Evaluation of an innovative population pharmacokinetic-based design for behavioral pharmacodynamic endpoints.
Laird, JM; Lessard, E; Martino, G; Viberg, A, 2012
)
0.38
" The aim of this study was to determine whether a commercially available curcuminoid/piperine extract alters the pharmacokinetic disposition of probe drugs for these enzymes in human volunteers."( Effect of a herbal extract containing curcumin and piperine on midazolam, flurbiprofen and paracetamol (acetaminophen) pharmacokinetics in healthy volunteers.
Badmaev, V; Court, MH; Greenblatt, DJ; Hanley, MJ; Harmatz, JS; Hazarika, S; Majeed, M; Masse, G; Volak, LP, 2013
)
0.39
"To examine individual patient's demographic parameters and clinical variables related to return of consciousness (ROC) and the pharmacodynamic relationship between propofol effect-site concentration (C(e)) and ROC from propofol-remifentanil anesthesia."( A pharmacodynamic analysis of factors affecting recovery from anesthesia with propofol-remifentanil target controlled infusion.
Han, DW; Kang, YR; Koo, BN; Lee, JH; Lee, JR; Noh, GJ, 2012
)
0.38
" Pharmacodynamic modeling incorporating covariates was performed using NONMEM (Nonlinear Mixed Effects Modeling) VII software."( A pharmacodynamic analysis of factors affecting recovery from anesthesia with propofol-remifentanil target controlled infusion.
Han, DW; Kang, YR; Koo, BN; Lee, JH; Lee, JR; Noh, GJ, 2012
)
0.38
"Age significantly affects the relationship between propofol C(e) and ROC, and pharmacodynamic modeling including age could lead to better predictions of ROC during emergence from propofol-remifentanil anesthesia."( A pharmacodynamic analysis of factors affecting recovery from anesthesia with propofol-remifentanil target controlled infusion.
Han, DW; Kang, YR; Koo, BN; Lee, JH; Lee, JR; Noh, GJ, 2012
)
0.38
" The developed assay was applied to a pharmacokinetic study in rats."( LC-MS/MS-ESI method for simultaneous quantitation of metformin and repaglinidie in rat plasma and its application to pharmacokinetic study in rats.
Giri, S; Mullangi, R; Pawar, G; Rajagopal, S; Sharma, K; Yadam, S, 2013
)
0.39
" In vitro studies have shown that pridopidine is a substrate for the P450 cytochrome 2D6 enzyme (CYP2D6), and clinical data show that the half-life of pridopidine is different following single dosing versus at steady state."( Pharmacokinetic and tolerability profile of pridopidine in healthy-volunteer poor and extensive CYP2D6 metabolizers, following single and multiple dosing.
Gundorf Drewes, P; Lindskov Krog, P; Osterberg, O; Rembratt, Å; Schultz, A; Timmer, W, 2013
)
0.39
" Pharmacodynamic monitoring offers a unique tool to evaluate the biologic effects of immunosuppressive drugs."( Pharmacodynamic analysis of tofacitinib and basiliximab in kidney allograft recipients.
Baan, CC; Chan, G; Kho, MM; Mol, WM; Quaedackers, ME; Vafadari, R; Weimar, W, 2012
)
0.38
" This involved further structural exploration directed at reducing metabolism and leading to the identification of compound 60 with a greatly improved in vivo pharmacokinetic profile."( Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H₁ antagonists. Part II: optimising in vivo clearance.
Alcaraz, L; Bahl, A; Beaton, H; Bowers, K; Collington, J; Denton, R; Donald, D; Furber, M; Kinchin, E; Luckhurst, C; MacDonald, C; Rigby, A; Riley, R; Soars, M; Springthorpe, B; Webborn, P, 2012
)
0.38
" The complex pharmacokinetic and pharmacogenetic properties and the unfavourable short and long term risk profile of glibenclamide and glimepiride raise the question whether their use can be justified any longer."( CYP2C metabolism of oral antidiabetic drugs--impact on pharmacokinetics, drug interactions and pharmacogenetic aspects.
Beil, W; Holstein, A; Kovacs, P, 2012
)
0.38
" In normal and streptozotocin induced diabetic rats the combination of glimepiride with piperine increased all the pharmacokinetic parameters, such as Cmax, AUC0-n, AUCtotal, t1/2, and MRT, and decreased the clearance, Vd, markedly as compared with the control group."( Effect of piperine on the pharmacokinetics and pharmacodynamics of glimepiride in normal and streptozotocin-induced diabetic rats.
Rani, TS; Sujatha, S; Veeresham, C, 2012
)
0.38
"Conventional mammillary models are frequently used for pharmacokinetic (PK) analysis when only blood or plasma data are available."( Applications of minimal physiologically-based pharmacokinetic models.
Cao, Y; Jusko, WJ, 2012
)
0.38
"The purpose of this study was to investigate the potential pharmacokinetic interactions with natural products (such as piperine (PIP), gallic acid (GA) and cinnamic acid (CA)) and rosuvastatin (RSV) (a specific breast cancer resistance protein, BCRP substrate) in rats."( Effects of piperine, cinnamic acid and gallic acid on rosuvastatin pharmacokinetics in rats.
Basu, S; Jana, S; Patel, H; Patel, VB, 2013
)
0.39
" TLS grading was modeled with logistic regression as a pharmacodynamic endpoint."( A pharmacokinetic/pharmacodynamic model of tumor lysis syndrome in chronic lymphocytic leukemia patients treated with flavopiridol.
Blum, KA; Byrd, JC; Grever, MR; Ji, J; Johnson, AJ; Mould, DR; Phelps, MA; Poi, M; Ruppert, AS; Zhao, Y, 2013
)
0.39
"Gender was the most significant pharmacokinetic covariate, with females displaying higher flavo-G exposure than males."( A pharmacokinetic/pharmacodynamic model of tumor lysis syndrome in chronic lymphocytic leukemia patients treated with flavopiridol.
Blum, KA; Byrd, JC; Grever, MR; Ji, J; Johnson, AJ; Mould, DR; Phelps, MA; Poi, M; Ruppert, AS; Zhao, Y, 2013
)
0.39
" Donepezil, galantamine and rivastigmine are acetylcholinesterase inhibitors with different pharmacodynamic and pharmacokinetic profiles."( Pharmacodynamic, pharmacokinetic and pharmacogenetic aspects of drugs used in the treatment of Alzheimer's disease.
Eap, CB; Noetzli, M, 2013
)
0.39
"The aim of the study was to better understand blonanserin population pharmacokinetic (PK) characteristics in Chinese healthy subjects."( Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake.
Li, FF; Li, X; Liu, X; Lu, W; Luo, FT; Ni, XJ; Qiu, C; Shang, DW; Wang, XP; Wen, YG; Xie, HZ; Zhang, M, 2013
)
0.39
" Using a LC-MS/MS assay validated in cell medium, cellular pharmacokinetic studies revealed that in cells overexpressing the P-gp intracellular concentrations of vandetanib were decreased compared to parental cell line."( Influence of the multidrug transporter P-glycoprotein on the intracellular pharmacokinetics of vandetanib.
Bidart, JM; Broutin, S; Deroussent, A; Farinotti, R; Gil, S; Jovelet, C; Paci, A, 2013
)
0.39
"The in vivo preclinical pharmacodynamic profile of TD-1211, a selective opioid receptor antagonist currently under development for the treatment of opioid-induced constipation, was compared to that of the clinically studied opioid antagonists, naltrexone, alvimopan, and ADL 08-0011 (the primary active metabolite of alvimopan)."( The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity.
Armstrong, SR; Beattie, DT; Campbell, CB; Hegde, SS; Long, DD; Richardson, CL; Tsuruda, PR; Vickery, RG, 2013
)
0.39
"Only one kind of synthesized alkaloid, piperlonguminine, was used to understand the interference of the other alkaloids in pharmacokinetic study using HPLC/UV in rat plasma after oral administration."( LC analysis and pharmacokinetic study of synthetic piperlonguminine in rat plasma after oral administration.
Baigude, H; Borjihan, G; Sarnaizul, E, 2013
)
0.39
" The validated method has been successfully applied to a human pharmacokinetic study of iloperidone and two active metabolites, P88 and P95, after oral administration of 4mg iloperidone tablets in 12 healthy Chinese volunteers."( Simultaneous determination of iloperidone and its two active metabolites in human plasma by liquid chromatography-tandem mass spectrometry: application to a pharmacokinetic study.
Fan, Y; He, X; Jia, M; Li, J; Li, W; Liu, M; Zhou, Y, 2013
)
0.39
"The effect of pitavastatin and SLCO1B1 genetic background on the pharmacokinetic and pharmacodynamic properties of repaglinide was investigated."( Effect of pitavastatin in different SLCO1B1 backgrounds on repaglinide pharmacokinetics and pharmacodynamics in healthy Chinese males.
Chen, XP; Fu, ZM; Huang, LH; Huang, YY; Huang, ZJ; Liu, C; Song, M; Tan, HY; Tan, ZR; Yang, GP; Yuan, H; Zhu, J, 2013
)
0.39
" The aim of the analyses was to develop a population pharmacokinetic model to describe the pharmacokinetics of JNJ-37822681 in healthy subjects and patients with schizophrenia and to identify covariates of interest."( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy.
Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013
)
0.39
" Nonlinear mixed effects modeling of pooled data was conducted using NONMEM(®) to estimate population pharmacokinetic parameters and the effect of covariates on these parameters."( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy.
Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013
)
0.39
" The estimated pharmacokinetic parameters for the phase IIb study were similar to those observed in the phase IIa study."( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy.
Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013
)
0.39
"The population pharmacokinetic model of JNJ-37822681 successfully described the pharmacokinetics of JNJ-37822681 and allowed the reliable determination of individual exposure parameters in a phase IIb study."( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy.
Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013
)
0.39
" This method was applied to quantify samples obtained from the pharmacokinetic and brain penetration studies in male wistar rats."( LC-MS/MS method for the determination of pitolisant: application to rat pharmacokinetic and brain penetration studies.
Ajjala, DR; Bhyrapuneni, G; Jonnala, MR; Kandikere, V; Muddana, NR; Nirogi, R; Pantangi, HR; Vurimindi, H, 2013
)
0.39
"The pharmacokinetic parameters including AUC and T1/2 were significantly different among the PXR genotype groups."( PXR polymorphisms and their impact on pharmacokinetics/pharmacodynamics of repaglinide in healthy Chinese volunteers.
Du, QQ; He, L; Jiang, XH; Wang, L; Wang, ZJ, 2013
)
0.39
" Blood and urine samples were collected from pre-dose up to 72 h post-dose for bilastine pharmacokinetic analysis."( Evaluation of the single-dose pharmacokinetics of bilastine in subjects with various degrees of renal insufficiency.
Dilzer, SC; La Noce, A; Lasseter, KC; Sologuren, A, 2013
)
0.39
" No significant differences among groups in median time to reach Cmax (tmax) or in the mean terminal disposition rate constants for bilastine were found."( Evaluation of the single-dose pharmacokinetics of bilastine in subjects with various degrees of renal insufficiency.
Dilzer, SC; La Noce, A; Lasseter, KC; Sologuren, A, 2013
)
0.39
"Using Schnider's pharmacokinetic model, propofol pharmacodynamics were modelled during total intravenous anaesthesia."( Modelling propofol pharmacodynamics using BIS-guided anaesthesia.
León, A; Martín-Mateos, I; Méndez Pérez, JA; Reboso, JA, 2013
)
0.39
" Terminal phase half-life (t1/2 ) increased with severity of renal impairment."( Pharmacokinetics of tofacitinib, a janus kinase inhibitor, in patients with impaired renal function and end-stage renal disease.
Boy, M; Chan, G; Chow, V; Krishnaswami, S; Wang, C, 2014
)
0.4
" Here, we analyzed the occupancy of 5-HT1A receptors in living Sprague-Dawley rat brains by a novel candidate drug for OAB, E2110, using positron emission tomography (PET) imaging, and assessed the utility of a receptor occupancy (RO) assay to establish a pharmacodynamic index translatable between animals and humans."( A small-animal pharmacokinetic/pharmacodynamic PET study of central serotonin 1A receptor occupancy by a potential therapeutic agent for overactive bladder.
Higuchi, M; Ishihara, H; Maeda, J; Nakatani, Y; Sakai, M; Suhara, T; Suzuki, M; Takenaka, O; Tokunaga, M; Yoshinaga, T; Zhang, MR, 2013
)
0.39
" Pharmacokinetic parameters, including maximum plasma concentration (C(max)) and area under the plasma concentration-time curve (AUC), were calculated."( Pharmacokinetic comparisons of bepotastine besilate and bepotastine salicylate in healthy subjects.
Kim, KA; Park, JY, 2013
)
0.39
" All pharmacokinetic parameters of bepotastine exhibited no significant differences between the two formulations."( Pharmacokinetic comparisons of bepotastine besilate and bepotastine salicylate in healthy subjects.
Kim, KA; Park, JY, 2013
)
0.39
"64 mg (test) formulations have comparable pharmacokinetic characteristics and that these two formulations meet the regulatory criteria for bioequivalence."( Pharmacokinetic comparisons of bepotastine besilate and bepotastine salicylate in healthy subjects.
Kim, KA; Park, JY, 2013
)
0.39
"Allometric exponents in population pharmacokinetic analysis are regularly used but the issue of fixing or estimating an allometric exponent remains controversial."( A population pharmacokinetic model of remifentanil in pediatric patients using body-weight-dependent allometric exponents.
Mahmood, I; Staschen, CM, 2013
)
0.39
" A population pharmacokinetic approach was taken to describe drug clearance by the following BDE equation: CL=CLpop(BW/14."( A population pharmacokinetic model of remifentanil in pediatric patients using body-weight-dependent allometric exponents.
Mahmood, I; Staschen, CM, 2013
)
0.39
" Pharmacodynamic analyses of ChEIs provide paradoxical observations."( Pharmacodynamics of cholinesterase inhibitors suggests add-on therapy with a low-dose carbamylating inhibitor in patients on long-term treatment with rapidly reversible inhibitors.
Darreh-Shori, T; Hosseini, SM; Nordberg, A, 2014
)
0.4
" The mean elimination half-life of blonanserin (7."( The pharmacokinetic and safety profiles of blonanserin in healthy Chinese volunteers after single fasting doses and single and multiple postprandial doses.
Chen, R; Chen, X; Hu, P; Jiang, J; Liu, H; Wang, H; Zhong, W; Zhou, Y, 2014
)
0.4
" The pharmacokinetic parameters of repaglinide and blood glucose concentrations were also determined in rats after oral (0."( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine.
Choi, DH; Choi, I; Choi, JS, 2013
)
0.39
"A population pharmacokinetic study was performed including data from 129 older patients treated with donepezil."( Population pharmacokinetic approach to evaluate the effect of CYP2D6, CYP3A, ABCB1, POR and NR1I2 genotypes on donepezil clearance.
Alnawaqil, AM; Bula, C; Csajka, C; Eap, CB; Ebbing, K; Eyer, S; Gaillard, M; Giannakopoulos, P; Guidi, M; Michon, A; Noetzli, M; Stancu, I; Thomazic, V; von Gunten, A; Wilhelm, L; Zumbach, S, 2014
)
0.4
"The pharmacokinetic parameters of donepezil were well described by the developed population model."( Population pharmacokinetic approach to evaluate the effect of CYP2D6, CYP3A, ABCB1, POR and NR1I2 genotypes on donepezil clearance.
Alnawaqil, AM; Bula, C; Csajka, C; Eap, CB; Ebbing, K; Eyer, S; Gaillard, M; Giannakopoulos, P; Guidi, M; Michon, A; Noetzli, M; Stancu, I; Thomazic, V; von Gunten, A; Wilhelm, L; Zumbach, S, 2014
)
0.4
" During pseudo-steady-state anesthesia, the pharmacodynamic measures were obtained before and after a series of noxious and nonnoxious stimulations."( A response surface model approach for continuous measures of hypnotic and analgesic effect during sevoflurane-remifentanil interaction: quantifying the pharmacodynamic shift evoked by stimulation.
Eleveld, DJ; Hannivoort, LN; Heyse, B; Luginbühl, M; Proost, JH; Struys, MM; Vereecke, HE, 2014
)
0.4
"By combining pre- and poststimulation data, interaction models for BIS, SE, and RE demonstrate a consistent influence of "stimulation" on the pharmacodynamic relationship between sevoflurane and remifentanil."( A response surface model approach for continuous measures of hypnotic and analgesic effect during sevoflurane-remifentanil interaction: quantifying the pharmacodynamic shift evoked by stimulation.
Eleveld, DJ; Hannivoort, LN; Heyse, B; Luginbühl, M; Proost, JH; Struys, MM; Vereecke, HE, 2014
)
0.4
"To investigate the effect of OATP1B1 genotype as a covariate on repaglinide pharmacokinetics and drug-drug interaction (DDIs) risk using a reduced physiologically-based pharmacokinetic (PBPK) model."( Reduced physiologically-based pharmacokinetic model of repaglinide: impact of OATP1B1 and CYP2C8 genotype and source of in vitro data on the prediction of drug-drug interaction risk.
Galetin, A; Gertz, M; Houston, JB; Säll, C; Tsamandouras, N, 2014
)
0.4
" Four of the five commercially available DPP-4 inhibitors are subject to significant renal clearance, and pharmacokinetic studies in people with renal impairment have led to lower recommended doses based on creatinine clearance in order to prevent drug accumulation."( Dipeptidyl peptidase-4 inhibitors: pharmacokinetics, efficacy, tolerability and safety in renal impairment.
Davis, TM, 2014
)
0.4
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" This method is sufficient for pharmacokinetic studies of vandetanib in small animals and may be applied to human pharmacokinetic studies."( Validation of a high-performance liquid chromatographic ultraviolet detection method for the quantification of vandetanib in rat plasma and its application to pharmacokinetic studies.
Bu, Q; Cao, Z; Cui, D; Lin, H; Xu, Y; Zhao, Y,
)
0.13
"The study aims to establish a method for simultaneous determination of repaglinide and pravastatin sodium in rat plasma by LC-MS/MS and to study its pharmacokinetic interactions."( [Simultaneous determination of repaglinide and pravastatin sodium in rat plasma by LC-ms/MS and its application on pharmacokinetic interactions study].
Huang, J; Ma, YR; Rao, Z; Wei, YH; Wu, XA; Zhang, GQ; Zhou, Y, 2014
)
0.4
" Then, the pharmacokinetic profiles of linarin in rats after oral administration of linarin (50 mg/kg) alone and in combination with piperine (20 mg/kg) were determined using a validated LC-MS/MS method."( Effects of piperine on the intestinal permeability and pharmacokinetics of linarin in rats.
Di, X; Feng, X; Liu, Y; Wang, X, 2014
)
0.4
" Finally, the applicability of this assay has been successfully demonstrated in vivo pharmacokinetic and in vitro metabolism studies in Sprague-Dawley rat."( Pharmacokinetic and metabolism studies of rohitukine in rats by high performance liquid-chromatography with tandem mass spectrometry.
Balaramnavar, VM; Bhatta, RS; Chandasana, H; Chhonker, YS; Gaikwad, AN; Kanojiya, S; Kumar, D; Mishra, SK; Saxena, AK; Srivastava, S, 2014
)
0.4
" To evaluate the pharmacokinetic interactions between Pro and Rem, we developed and validated a method combining high-performance liquid chromatography with tandem mass spectrometry for simultaneous determination of Pro and Rem."( Simultaneous determination of propofol and remifentanil in rat plasma by liquid chromatography-tandem mass spectrometry: application to preclinical pharmacokinetic drug-drug interaction analysis.
El Hamd, MA; Ikeda, R; Kawakami, S; Kuroda, N; Nakashima, K; Wada, M, 2015
)
0.42
"Obesity is associated with important physiologic changes that can potentially affect the pharmacokinetic (PK) and pharmacodynamic (PD) profile of anesthetic drugs."( Performance of propofol target-controlled infusion models in the obese: pharmacokinetic and pharmacodynamic analysis.
Cortínez, LI; Crovari, F; De la Fuente, N; Eleveld, DJ; Ibacache, M; Oliveros, A; Sepulveda, P; Solari, S, 2014
)
0.4
" We used brain microdialysis to shed light on this aspect of the pharmacokinetic and to correlate these findings with Minto's model."( No correlation between remifentanil blood, cerebrospinal fluid and cerebral extracellular fluid levels and TCI prediction: a pharmacokinetic study.
Del Gaudio, A; Mastronardi, P; Mincolelli, G; Piacevoli, Q; Tonti, MP; Wouters, G, 2015
)
0.42
" The predictive performance of the Minto pharmacokinetic parameter set was evaluated by examining the performance error."( No correlation between remifentanil blood, cerebrospinal fluid and cerebral extracellular fluid levels and TCI prediction: a pharmacokinetic study.
Del Gaudio, A; Mastronardi, P; Mincolelli, G; Piacevoli, Q; Tonti, MP; Wouters, G, 2015
)
0.42
" Vandetanib + digoxin increased digoxin area under the concentration-time curve from zero to the last quantifiable concentration (AUC0-last) and Cmax by 23 and 29 %, respectively, versus digoxin alone, with only a 9 % decrease in CLR."( Pharmacokinetic evaluations of the co-administrations of vandetanib and metformin, digoxin, midazolam, omeprazole or ranitidine.
Johansson, S; Leese, PT; Li, Y; Lisbon, E; Martin, P; Mathews, D; Oliver, S; Read, J; Steinberg, M, 2014
)
0.4
" The floating time and accumulative release amount as evaluation indexes were utilized to perform pre-experiment screening and single-factor test, respectively, while central composite design response surface method was applied for formulation optimization, followed by in vivo pharmacokinetic study in beagles after oral administration for floating tablets and commercial tablets used as the control."( Preparation and pharmacokinetics study on gastro-floating sustained-release tablets of troxipide.
Gao, Y; Pan, WS; Wang, M; Wang, Z; Yang, X; Yang, Y; Ye, T; Yin, F, 2015
)
0.42
" The validated assay was applied to derive the pharmacokinetic parameters for MTX and TFB post-dosing of MTX and TFB orally and intravenously to rats."( A validated LC-MS/MS assay for simultaneous quantification of methotrexate and tofacitinib in rat plasma: application to a pharmacokinetic study.
Dhiman, V; Dixit, A; Giri, K; Mullangi, R; Sharma, K; Zainuddin, M, 2015
)
0.42
" We developed a population pharmacokinetic (PK) model for ibrutinib in patients."( Population pharmacokinetic model of ibrutinib, a Bruton tyrosine kinase inhibitor, in patients with B cell malignancies.
Advani, R; Byrd, JC; de Jong, J; De Nicolao, G; de Trixhe, XW; Loury, D; Marostica, E; McGreivy, J; O'Brien, S; Poggesi, I; Sukbuntherng, J; Vermeulen, A, 2015
)
0.42
" EEG is a potentially useful technique in drug development for measuring the pharmacodynamic (PD) effects of a centrally acting compound and hence to assess the likelihood of success of a novel drug based on pharmacokinetic-pharmacodynamic (PK-PD) principles."( Extracting drug mechanism and pharmacodynamic information from clinical electroencephalographic data using generalised semi-linear canonical correlation analysis.
Berry, E; Brain, P; Diukova, A; Hall, JE; Ivarsson, M; Jolly, A; Strimenopoulou, F; Wilson, FJ; Wise, RG, 2014
)
0.4
" Sustained drug releases profiles over 10h and a reduced influence of medium pHs on release were achieved with the optimized formulation; moreover, the in vivo performance of extended release formulation was also examined, and better absorption, a one-fold decrease in Cmax, a two-fold increase of Tmax and a prolonged hypoglycemic effect compared to the marketed product were observed."( Matrix tablets for sustained release of repaglinide: Preparation, pharmacokinetics and hypoglycemic activity in beagle dogs.
He, W; Huang, S; Wu, M; Yin, L, 2015
)
0.42
"Following initial screening and baseline blood collections, participants received ascending oral doses (20, 50 and then 100 mg at least 1-week apart) of capromorelin after pre-dose blood collection, followed by blood collections over the following 12 h for pharmacokinetic analysis and 1-week and 4-week follow-up blood collections for safety evaluations."( Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers.
Brown, DJ; Ellis, AG; Frauman, AG; Furness, JB; Millard, M; Zeglinski, PT, 2015
)
0.42
" Pharmacokinetic behaviour was broadly similar between groups, with both exhibiting dose-dependent increases in Cmax and AUC0-∞."( Pharmacokinetics of the ghrelin agonist capromorelin in a single ascending dose Phase-I safety trial in spinal cord-injured and able-bodied volunteers.
Brown, DJ; Ellis, AG; Frauman, AG; Furness, JB; Millard, M; Zeglinski, PT, 2015
)
0.42
" In the pharmacokinetic studies in mice, rats and dogs, favorable pharmacokinetic profiles and good oral bioavailability were observed for AV560."( [Antiviral activity in vitro and pharmacokinetics of HCV entry inhibitor AVR560].
Bulanova, EA; Bychko, VV; Ezhova, EV; Iamanushkin, PM; Ivashchenko, AA; Ivashchenko, AV; Koriakova, AG; Korzinov, OM; Mit'kin, OD; Vyshemirskaia, PV, 2014
)
0.4
"05) increase in the maximum plasma concentration (Cmax), the mean area under the plasma concentration-time curve (AUC), and the elimination half-life (t1/2) of domperidone as compared to those obtained for domperidone alone."( Effect of piperine, a major component of black pepper, on the pharmacokinetics of domperidone in rats.
Alhumayyd, MS; Almotrefi, AA; Bukhari, IA, 2014
)
0.4
" The analytical method was applied to support a pharmacokinetic study of simultaneous estimation of lenalidomide, ibrutinib, and its active metabolite PCI-45227 in Wistar rat."( Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: application to a pharmacokinetic study.
Govindarajulu, B; Rangasamy, M; Thappali, S; Vakkalanka, S; Veeraraghavan, S; Viswanadha, S, 2015
)
0.42
" The validated HPLC method was successfully applied to a pharmacokinetic study in rats."( Development and validation of a RP-HPLC method for the quantitation of tofacitinib in rat plasma and its application to a pharmacokinetic study.
Dhiman, V; Giri, KK; Mullangi, R; S, VK; Sharma, K; Zainuddin, M, 2015
)
0.42
" When corrected for repeated dosing, pharmacokinetic parameters in healthy participants and patients were comparable."( The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia.
Byrd, JC; Chauhan, V; de Jong, J; Hellemans, P; James, D; Jiao, J; Loury, DJ; Mannaert, E; Murphy, J; O'Brien, S; Skee, D; Sukbuntherng, J, 2015
)
0.42
"There have been no pharmacokinetic parameters and blood-brain equilibration rate constant (k e0) of propofol obtained in a single population of children, by which propofol can be administered using a target effect-site concentration controlled infusion."( Population pharmacokinetic and pharmacodynamic model of propofol externally validated in children.
Byon, HJ; Choi, BM; Kim, HS; Lee, EK; Lee, HG; Lee, SH; Noh, GJ, 2015
)
0.42
" Pharmacokinetic parameters were obtained by noncompartmental analysis."( Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.
Bae, KS; Choi, HY; Choi, YK; Hong, D; Jeon, HS; Kim, SS; Kim, YH; Lee, SH; Lim, HS, 2015
)
0.42
" Median time to Cmax was ~74-76 hours (~2-4 hours after patch removal), and mean t1/2β was ~63."( Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.
Bae, KS; Choi, HY; Choi, YK; Hong, D; Jeon, HS; Kim, SS; Kim, YH; Lee, SH; Lim, HS, 2015
)
0.42
" Pharmacokinetic analysis of the donepezil patch demonstrated linear kinetics."( Single dose pharmacokinetics of the novel transdermal donepezil patch in healthy volunteers.
Bae, KS; Choi, HY; Choi, YK; Hong, D; Jeon, HS; Kim, SS; Kim, YH; Lee, SH; Lim, HS, 2015
)
0.42
" Following intravenous administration of DL76 at the dose of 3 mg/kg, pharmacokinetic parameters were calculated using non-compartmental analysis."( Pharmacokinetics and tissue distribution of the new non-imidazole histamine H3 receptor antagonist 1-[3-(4-tert-butylphenoxy) propyl]piperidine in rats.
Kiec-Kononowicz, K; Kryczyk, A; Lazewska, D; Szafarz, M; Wyska, E, 2015
)
0.42
" Serial plasma and urine samples (collected over 120 h post-dose) were analyzed using LC-MS/MS for pharmacokinetic evaluations."( Safety, Tolerability and Pharmacokinetic and Pharmacodynamic Learnings from a Double-Blind, Randomized, Placebo-Controlled, Sequential Group First-in-Human Study of the TRPV1 Antagonist, JNJ-38893777, in Healthy Men.
De Meulder, M; Jun, C; Manitpisitkul, P; Mayorga, A; Moyer, JA; Romano, G; Shalayda, K, 2015
)
0.42
" No clinically relevant pharmacokinetic interactions between the two agents have been described and the fixed-dose combination has shown bioequivalence with alogliptin and pioglitazone given separately."( Pharmacokinetics and clinical evaluation of the alogliptin plus pioglitazone combination for type 2 diabetes.
Scheen, AJ, 2015
)
0.42
"We performed population pharmacokinetic (PK) analysis of a novel transdermal donepezil patch in healthy subjects who participated in a phase I trial."( Therapeutic dosage assessment based on population pharmacokinetics of a novel single-dose transdermal donepezil patch in healthy volunteers.
Bae, KS; Choi, HY; Hong, D; Kim, SS; Kim, YH; Lim, HS, 2015
)
0.42
" There was a 37% decrease in Cmax and a 16% decrease in AUC (0-∞) following administration of danirixin in the presence of food."( The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)--a selective CXCR2 antagonist --in healthy adult subjects.
Bloomer, JC; Carpenter, DC; Connolly, P; Cooray, H; Lazaar, AL; Miller, BE; Mistry, S; Smart, K; Tal-Singer, R, 2015
)
0.42
" The pharmacokinetic profiles of emodin after oral administration of emodin (20mg/kg) alone and in combination with piperine (20mg/kg) to rats were investigated via a validated LC/MS/MS method."( Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats.
Di, X; Liu, Y; Wang, X, 2015
)
0.42
" NONMEM was used for pharmacokinetic analysis."( Population pharmacokinetics and dosing implications for cobimetinib in patients with solid tumors.
Bruno, R; Budha, NR; Choong, N; Dresser, M; Eppler, S; Hack, SP; Han, K; Jin, JY; Marchand, M; Musib, L; Tikoo, N, 2015
)
0.42
"A population pharmacokinetic model was developed for cobimetinib in cancer patients."( Population pharmacokinetics and dosing implications for cobimetinib in patients with solid tumors.
Bruno, R; Budha, NR; Choong, N; Dresser, M; Eppler, S; Hack, SP; Han, K; Jin, JY; Marchand, M; Musib, L; Tikoo, N, 2015
)
0.42
"2h, Cmax 25."( Metabolism and pharmacokinetics of 8-hydroxypiperidinylmethyl-baicalein (BA-j) as a novel selective CDK1 inhibitor in monkey.
Guo, HM; Ju, XL; Li, HL; Li, J; Sun, XD; Sun, YM; Xie, AY; Zhang, SX; Zheng, Y; Zou, L, 2015
)
0.42
"The availability of intravenous and oral pharmacokinetic data in animals enabled the allometry scaling of 6 DPP-IV inhibitors."( Retrospective and Prospective Human Intravenous and Oral Pharmacokinetic Projection of Dipeptidyl peptidase-IV Inhibitors Using Simple Allometric Principles - Case Studies of ABT-279, ABT-341, Alogliptin, Carmegliptin, Sitagliptin and Vildagliptin.
Bhamidipati, RK; Gilibili, RR; Mullangi, R; Srinivas, NR, 2015
)
0.42
" Finally, the assay was used for a pharmacokinetic study of plasma levels in treated FVB mice."( Liquid chromatography-tandem mass spectrometric assay for the simultaneous determination of the irreversible BTK inhibitor ibrutinib and its dihydrodiol-metabolite in plasma and its application in mouse pharmacokinetic studies.
Beijnen, JH; Rood, JJM; Schellens, JHM; Schinkel, AH; Sparidans, RW; van Hoppe, S, 2016
)
0.43
"To explore the pharmacokinetic properties of icariin (ICA) and icariside II (ICA II) following intragastric and intravenous administration in rats, a rapid and sensitive method by using ultra-performance liquid chromatography-tandem mass spectroscopy (UPLC-MS/MS) was developed and validated for the simultaneous quantification of ICA and ICA II in rat plasma."( Comparative Pharmacokinetics Study of Icariin and Icariside II in Rats.
Cheng, T; Ding, Y; Lu, L; Zhang, T; Zhang, Y; Zhao, Y, 2015
)
0.42
" These pharmacokinetic characteristics in animals were also confirmed in the clinical studies."( Pharmacokinetics of TAK-475, a Squalene Synthase Inhibitor, in Rats and Dogs.
Asahi, S; Ebihara, T; Kondo, T; Moriwaki, T; Tagawa, Y; Teshima, K, 2016
)
0.43
"Herein, we report the gram-scale synthesis, pharmacokinetic profile and CNS distribution of (R)-RC-33 in the mouse to determine the most suitable dosage schedule for in vivo administration."( Toward the identification of neuroprotective agents: g-scale synthesis, pharmacokinetic evaluation and CNS distribution of (R)-RC-33, a promising SIGMA1 receptor agonist.
Bigogno, C; Canta, A; Cavaletti, G; Collina, S; Corbo, M; Curti, D; Dondio, G; Malacrida, A; Marra, A; Oggioni, N; Peviani, M; Pignataro, L; Rossi, D, 2016
)
0.43
"(R)-RC-33 shows a similar pharmacokinetic profile and a better CNS distribution when compared with PRE-084."( Toward the identification of neuroprotective agents: g-scale synthesis, pharmacokinetic evaluation and CNS distribution of (R)-RC-33, a promising SIGMA1 receptor agonist.
Bigogno, C; Canta, A; Cavaletti, G; Collina, S; Corbo, M; Curti, D; Dondio, G; Malacrida, A; Marra, A; Oggioni, N; Peviani, M; Pignataro, L; Rossi, D, 2016
)
0.43
" Camicinal was well absorbed, exhibiting linear and approximately dose-proportional pharmacokinetic characteristics and a clear exposure-response relationship with gastric emptying."( The pharmacodynamics, safety and pharmacokinetics of single doses of the motilin agonist, camicinal, in type 1 diabetes mellitus with slow gastric emptying.
Alpers, DH; Barton, ME; Dukes, GE; Hacquoil, K; Hellström, PM; Johnson, LV; Richards, DB; Sanger, GJ; Tack, J, 2016
)
0.43
" Camicinal was well tolerated and exhibited similar pharmacokinetic characteristics in diabetic patients to those previously reported in healthy volunteers."( The pharmacodynamics, safety and pharmacokinetics of single doses of the motilin agonist, camicinal, in type 1 diabetes mellitus with slow gastric emptying.
Alpers, DH; Barton, ME; Dukes, GE; Hacquoil, K; Hellström, PM; Johnson, LV; Richards, DB; Sanger, GJ; Tack, J, 2016
)
0.43
" An extended-release (XR) formulation has been designed to provide a once-daily (QD) dosing option to patients to achieve comparable pharmacokinetic (PK) parameters to the twice-daily immediate-release (IR) formulation."( Extended-Release Once-Daily Formulation of Tofacitinib: Evaluation of Pharmacokinetics Compared With Immediate-Release Tofacitinib and Impact of Food.
Alvey, C; Fletcher, T; Kushner, J; Lamba, M; Stock, TC; Wang, R, 2016
)
0.43
" In-vivo pharmacokinetic studies in rats showed that optimized SNEDDS I1 controlled the absorption of IBR compared with IBR suspension."( Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system.
Ezzeldin, E; Iqbal, M; Shakeel, F, 2016
)
0.43
" In subjects with moderate hepatic impairment, the geometric mean AUCinf and Cmax of tofacitinib were increased (90% confidence intervals of percentage increase) by approximately 65% (25%, 117%) and 49% (12%, 97%), respectively."( The effect of mild and moderate hepatic impairment on the pharmacokinetics of tofacitinib, an orally active Janus kinase inhibitor.
Alvey, CW; Chan, G; Krishnaswami, S; Lamba, M; Lawendy, N; Wang, R, 2014
)
0.4
" Mean half-life was similar in the presence and absence of tofacitinib: 13."( Evaluation of the Effect of Tofacitinib on the Pharmacokinetics of Oral Contraceptive Steroids in Healthy Female Volunteers.
Alvey, CW; Krishnaswami, S; Menon, S; Petit, W; Riese, R; Shi, H; Wang, R, 2016
)
0.43
" Plasma pharmacokinetic studies of single-dose NSC23925b alone or in combination with paclitaxel or doxorubicin were conducted in male BALB/c mice and Sprague-Dawley rats."( Pharmacokinetics and tolerability of NSC23925b, a novel P-glycoprotein inhibitor: preclinical study in mice and rats.
Choy, E; Duan, Z; Gao, Y; Hornicek, FJ; Mankin, HJ; Shen, JK; Zhang, Z, 2016
)
0.43
"The purpose of this study was to investigate potential systemic pharmacokinetic interactions between intranasal fluticasone furoate (FF) and levocabastine (LEVO) when delivered simultaneously via a metered atomizing spray pump."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.43
"These results suggest that in healthy subjects, for LEVO, there is no pharmacokinetic interaction with FF when delivered as FF/LEVO FDC."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.43
"The pharmacokinetic parameters like peak plasma concentration (Cmax), area under the plasma concentration time profile (AUC) and elimination half life of repaglinide were significantly (p<0."( Altered pharmacokinetics and pharmacodynamics of repaglinide by ritonavir in rats with healthy, diabetic and impaired hepatic function.
Goud, T; Maddi, S; Nayakanti, D; Thatipamula, RP, 2016
)
0.43
" The pharmacokinetic profile of DTX was exceptionally improved by the conjugation, in general, and coadministration with piperine, in specific vis-à-vis plain drug."( Conjugation of Docetaxel with Multiwalled Carbon Nanotubes and Codelivery with Piperine: Implications on Pharmacokinetic Profile and Anticancer Activity.
Arora, S; Bhushan, S; Guru, SK; Katare, OP; Kiran, C; Kumar, D; Kumar, M; Kumar, P; Raza, K; Sharma, G, 2016
)
0.43
"Accompanied by significant improvements of modeling techniques and computational methods in medical sciences, the last thirty years saw the flourishing of pharmacokinetic models for applications in the pharmacometric field."( Innovations and Improvements in Pharmacokinetic Models Based on Physiology.
Abbiati, RA; Manca, D, 2017
)
0.46
" Four major points are detailed: (i) the mathematical formulation of the model, which allows modulating its complexity as a function of the administration route and active principle; (ii) a dedicated parameter of the PBPK model quantifies the drugprotein binding, which affects the active principle distribution; (iii) the gall bladder compartment and the bile enterohepatic circulation process; (iv) the coupling of the pharmacokinetic and pharmacodynamic models to produce an overall understanding of the drug effects on mammalian body."( Innovations and Improvements in Pharmacokinetic Models Based on Physiology.
Abbiati, RA; Manca, D, 2017
)
0.46
"A physiologically based pharmacokinetic (PBPK) model was developed for cobimetinib using in vitro data."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
"The PBPK model described cobimetinib pharmacokinetic profiles after both intravenous and oral administration of cobimetinib well and accurately simulated the itraconazole-cobimetinib DDI."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
" In addition, co-administration of rebaudioside A with repaglinide in rats did not lead to AUC and Cmax changes of repaglinide."( CYP2C8-mediated interaction between repaglinide and steviol acyl glucuronide: In vitro investigations using rat and human matrices and in vivo pharmacokinetic evaluation in rats.
Li, J; Lu, J; Wang, M; Wang, Y; Xu, Y; Zhang, H; Zhou, D, 2016
)
0.43
"Based on ibrutinib pharmacokinetics and potential sensitivity towards CYP3A4-mediated drug-drug interactions (DDIs), a physiologically based pharmacokinetic approach was developed to mechanistically describe DDI with various CYP3A4 perpetrators in healthy men under fasting conditions."( Ibrutinib Dosing Strategies Based on Interaction Potential of CYP3A4 Perpetrators Using Physiologically Based Pharmacokinetic Modeling.
De Jong, J; de Zwart, L; Mannaert, E; Monshouwer, M; Snoeys, J; Sukbuntherng, J, 2016
)
0.43
" The pharmacokinetic and pharmacodynamic profiles were compared with those reported in Caucasian subjects."( Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects.
Nagashima, H; Rodríguez, M; Togawa, M; Yamaya, H, 2016
)
0.43
"Bilastine exhibits similar single- and multiple-dose pharmacokinetic and pharmacodynamic characteristics in healthy Japanese subjects compared with those observed in Caucasian subjects in previous studies."( Pharmacokinetics, Pharmacodynamics and Population Pharmacokinetic/Pharmacodynamic Modelling of Bilastine, a Second-Generation Antihistamine, in Healthy Japanese Subjects.
Nagashima, H; Rodríguez, M; Togawa, M; Yamaya, H, 2016
)
0.43
" This work describes the isolation and characterization of the individual isomers of 1 and shows that these display stereospecific pharmacokinetic and pharmacodynamic features."( The Oncolytic Efficacy and in Vivo Pharmacokinetics of [2-(4-Chlorophenyl)quinolin-4-yl](piperidine-2-yl)methanol (Vacquinol-1) Are Governed by Distinct Stereochemical Features.
Bernlind, A; Ernfors, P; Färnegårdh, K; Granath, M; Gravenfors, Y; Hammarström, LG; Harmel, RK; Kitambi, SS; Lehmann, F; Lundin, G; Ringom, R; Roddis, Y; Svensson, PH; Wennman, D, 2016
)
0.43
" In a search for KOR antagonists that do not accumulate in the brain, we compared single doses of five methylated JDTic analogs (RTI-97, -194, -212, -240, and -241) for reversal of U50,488 diuresis and pharmacokinetic (PK) properties."( Pharmacodynamic Relationships between Duration of Action of JDTic-like Kappa-Opioid Receptor Antagonists and Their Brain and Plasma Pharmacokinetics in Rats.
Carroll, FI; Fennell, TR; Howard, JL; Owens, SM; Pollard, GT; Snyder, RW, 2016
)
0.43
" To determine the rate of DPP-4 inhibition induced by these inhibitors, pharmacokinetic and pharmacodynamic parameters were used to theoretically examine the relationship between the rate of DPP-4 inhibition and clinical efficacy following the administration of four different DPP-4 inhibitors (sitagliptin, vildagliptin, alogliptin, linagliptin) by focusing on the increase in the level of glucagon-like peptide-1 (GLP-1) induced by their administration."( Evaluation of drug efficacy of DPP-4 inhibitors based on theoretical analysis with pharmacokinetics and pharmacodynamics.
Kimura, K; Takayanagi, R; Uchida, T; Yamada, Y, 2017
)
0.46
"We report a case of Pisa syndrome (PS) due to the acetylcholinesterase inhibitor donepezil which may have been precipitated by pharmacokinetic interactions with commonly used medications."( Pisa syndrome due to donepezil: pharmacokinetic interactions to blame?
Cunningham, E; McGuinness, B; Passmore, AP; Pollock, D, 2017
)
0.46
" Here, we review the available literature on the pharmacokinetic and pharmacodynamic properties of these novel agents to guide the reader in the appropriate use of ibrutinib, idelalisib, and venetoclax."( Pharmacokinetic and Pharmacodynamic Considerations in the Treatment of Chronic Lymphocytic Leukemia: Ibrutinib, Idelalisib, and Venetoclax.
Hill, BT; Waldron, M; Winter, A, 2017
)
0.46
" This manuscript outlines a nonclinical approach comprising multiple biopharmaceutical, in vitro and physiologically based pharmacokinetic model (PBPK) modelling studies to enable selection of an alternative salt form for danirixin (DNX, GSK1325756), a pharmaceutical agent being developed for chronic obstructive pulmonary disease (COPD)."( Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations.
Ambery, C; Bloomer, JC; Connolly, P; Garden, H; Henley, N; Hodnett, N; Keel, S; Kreindler, JL; Lazaar, AL; Lloyd, RS; Matthews, W; Miller, BE; Yonchuk, J, 2017
)
0.46
" The predictive performance of three published pharmacokinetic models was evaluated."( Population pharmacokinetics of intravenous acetaminophen in Japanese patients undergoing elective surgery.
Hasegawa, M; Imaizumi, T; Iseki, Y; Mogami, M; Murakawa, M; Obara, S, 2017
)
0.46
" In the present study, a physiologically-based pharmacokinetic model was applied to compare the pharmacokinetics of tofacitinib in Japanese and Caucasians to assess the potential impact of ethnicity on the dosing regimen in the two populations."( Application of Physiologically-Based Pharmacokinetic Modeling for the Prediction of Tofacitinib Exposure in Japanese.
Hirai, M; Kurebayashi, Y; Suzuki, M; Tse, S, 2017
)
0.46
"Pharmacokinetic and pharmacodynamic models are used to predict and explore drug infusion schemes and their resulting concentration profiles for clinical application."( An Allometric Model of Remifentanil Pharmacokinetics and Pharmacodynamics.
Absalom, AR; Eleveld, DJ; Olofsen, E; Proost, JH; Struys, MMRF; Vereecke, H; Vuyk, J, 2017
)
0.46
"Remifentanil pharmacokinetic data were obtained from three previously published studies of adults and children, one of which also contained pharmacodynamic data from adults."( An Allometric Model of Remifentanil Pharmacokinetics and Pharmacodynamics.
Absalom, AR; Eleveld, DJ; Olofsen, E; Proost, JH; Struys, MMRF; Vereecke, H; Vuyk, J, 2017
)
0.46
" The final pharmacokinetic model uses age, weight, and sex as covariates."( An Allometric Model of Remifentanil Pharmacokinetics and Pharmacodynamics.
Absalom, AR; Eleveld, DJ; Olofsen, E; Proost, JH; Struys, MMRF; Vereecke, H; Vuyk, J, 2017
)
0.46
"The influence of obesity on the pharmacokinetic (PK) behavior of remifentanil is incompletely understood."( Disposition of Remifentanil in Obesity: A New Pharmacokinetic Model Incorporating the Influence of Body Mass.
Drover, DR; Egan, TD; Kim, TK; La Colla, L; Mertens, M; Minto, CF; Obara, S; Vuyk, J, 2017
)
0.46
"To establish the in silico ocular pharmacokinetic modeling for eye drops, and to simulate the dose regimen for FK962 in human choroid/retinal diseases."( In Silico Ocular Pharmacokinetic Modeling: Delivery of Topical FK962 to Retina.
Azuma, M; Kishimoto, Y; Kozai, S; Mori, A; Ohtori, A; Shearer, TR; Yabuta, C, 2017
)
0.46
" As a validation, we perform mechanistic pharmacokinetic modeling for SLCO1B1 (encoding OATP1B1) and ABCG2 (encoding BCRP) genotyped pharmacokinetic data from 18 clinical studies with healthy Caucasian and/or Asian subjects."( Explaining Ethnic Variability of Transporter Substrate Pharmacokinetics in Healthy Asian and Caucasian Subjects with Allele Frequencies of OATP1B1 and BCRP: A Mechanistic Modeling Analysis.
Barton, HA; Li, R, 2018
)
0.48
"Simulations based on the current hypothesis reasonably describe SLCO1B1 and ABCG2 genotyped pharmacokinetic time course data for five transporter substrates (atorvastatin, pitavastatin, pravastatin, repaglinide, and rosuvastatin) in Caucasian and Asian populations."( Explaining Ethnic Variability of Transporter Substrate Pharmacokinetics in Healthy Asian and Caucasian Subjects with Allele Frequencies of OATP1B1 and BCRP: A Mechanistic Modeling Analysis.
Barton, HA; Li, R, 2018
)
0.48
" 18F-Fluoro-deoxy-glucose positron emission tomography (18F-FDG PET) is a non-invasive pharmacodynamic imaging biomarker that has become an integral part of drug development."( The use of 18F-Fluoro-deoxy-glucose positron emission tomography (18F-FDG PET) as a non-invasive pharmacodynamic biomarker to determine the minimally pharmacologically active dose of AZD8835, a novel PI3Kα inhibitor.
Barjat, H; Ble, FX; Emmas, SA; Hancox, U; Hudson, K; Lawrie, E; Maynard, J; Polanska, UM; Pritchard, A, 2017
)
0.46
"Our pre-clinical studies support the use of 18F-FDG PET imaging as a sensitive and non- invasive pharmacodynamic biomarker (understanding the role of PI3K signalling in glucose uptake) for AZD8835 with a decrease in 18F-FDG uptake observed at only two hours post treatment."( The use of 18F-Fluoro-deoxy-glucose positron emission tomography (18F-FDG PET) as a non-invasive pharmacodynamic biomarker to determine the minimally pharmacologically active dose of AZD8835, a novel PI3Kα inhibitor.
Barjat, H; Ble, FX; Emmas, SA; Hancox, U; Hudson, K; Lawrie, E; Maynard, J; Polanska, UM; Pritchard, A, 2017
)
0.46
" The aims of this work are to propose and validate a physiologically based pharmacokinetic model capable to predict both the pharmacokinetics and pharmacodynamics of remifentanil, and to take into account the inter-individual differences among the patients (such as height and body mass)."( A physiologically-based model to predict individual pharmacokinetics and pharmacodynamics of remifentanil.
Abbiati, RA; Cascone, S; Lamberti, G; Manca, D; Piazza, O, 2018
)
0.48
" Pharmacokinetic parameters were estimated by non-compartmental analysis and compared between periods by standard average bioequivalence ANOVA."( Effects of food and grapefruit juice on single-dose pharmacokinetics of blonanserin in healthy Chinese subjects.
Hu, HT; Hu, JQ; Lu, HY; Ni, XJ; Peng, H; Qiu, C; Shang, DW; Shen, LF; Wang, ZZ; Wen, YG; Zhang, M; Zhang, YF, 2018
)
0.48
" To elucidate on-target and pharmacodynamic effects of acalabrutinib, we evaluated several laboratory endpoints, including proteomic changes, chemokine modulation and impact on cell migration."( Pharmacodynamics and proteomic analysis of acalabrutinib therapy: similarity of on-target effects to ibrutinib and rationale for combination therapy.
Ayres, ML; Balakrishnan, K; Cheung, JP; Gandhi, V; Gay, J; Ivan, C; Keating, MJ; Lamothe, B; Marszalek, JR; Morse, J; Nelson, M; Patel, VK; Wierda, WG, 2018
)
0.48
" Therefore, a strategy with a combination of physiologically based pharmacokinetic (PBPK) modeling and limited clinical trials focused on generating informative data for modeling was made to ensure extrapolation ability of DDI risk."( Model-Based Assessments of CYP-Mediated Drug-Drug Interaction Risk of Alectinib: Physiologically Based Pharmacokinetic Modeling Supported Clinical Development.
Cleary, Y; Fowler, S; Gertz, M; Morcos, PN; Parrott, N; Phipps, A; Youdim, K; Yu, L, 2018
)
0.48
" The method was validated and successfully applied to everted sac and pharmacokinetic studies in rats."( HPLC Estimation, Ex vivo Everted Sac Permeability and In Vivo Pharmacokinetic Studies of Darunavir.
Sangave, PC; Suvarna, VM, 2018
)
0.48
" The main objective of the present study was to investigate the effect of alcohol on the pharmacokinetic properties of blonanserin and its metabolite N-deethyl blonanserin in healthy Chinese male subjects under fasting conditions."( Effects of Alcohol on the Pharmacokinetics of Blonanserin and N-Deethylated Blonanserin in Healthy Chinese Subjects.
Chen, Y; Deng, S; Hu, J; Lu, H; Ni, X; Peng, H; Shang, D; Wang, Z; Wen, Y; Zhang, M; Zhang, Y; Zhu, X, 2018
)
0.48
" In treatment A, average values of AUC0-24h, AUC0-∞, and Cmax were 3178 ng/h/L, 3879 ng/h/L, and 492 ng/L for blonanserin, and 1932 ng/h/L, 4208 ng/h/L, and 137 ng/L for N-deethylated blonanserin, respectively."( Effects of Alcohol on the Pharmacokinetics of Blonanserin and N-Deethylated Blonanserin in Healthy Chinese Subjects.
Chen, Y; Deng, S; Hu, J; Lu, H; Ni, X; Peng, H; Shang, D; Wang, Z; Wen, Y; Zhang, M; Zhang, Y; Zhu, X, 2018
)
0.48
" The proposed method was successfully applied for pharmacokinetic study in beagle dogs."( Simultaneous determination of zidebactam and cefepime in dog plasma by LC-MS/MS and its application to pre-clinical pharmacokinetic study.
Chavan, R; Patel, M; Patil, K; Tambe, H; Yeole, R; Zope, V, 2018
)
0.48
"The use of conventional pharmacokinetic parameters sets 'models' derived from nonobese patients has proven inadequate to administer intravenous anesthetics in the obese population and is commonly associated with higher than anticipated plasma propofol concentrations when used with target (plasma or effect site) controlled infusion pumps."( Advances in pharmacokinetic modeling: target controlled infusions in the obese.
Anderson, BJ; Cortínez, LI, 2018
)
0.48
" Newer pharmacokinetic models, determined from obese patient data, have been developed for propofol and remifentanil using allometric concepts and comprehensive size descriptors."( Advances in pharmacokinetic modeling: target controlled infusions in the obese.
Anderson, BJ; Cortínez, LI, 2018
)
0.48
" Post-marketing studies provided additional pharmacokinetic information on their pharmacokinetic parameters."( Clinical Pharmacokinetics of Anaplastic Lymphoma Kinase Inhibitors in Non-Small-Cell Lung Cancer.
Hirota, T; Ieiri, I; Muraki, S, 2019
)
0.51
"We analyzed torsadogenic and pharmacokinetic profile of E-4031 using chronic atrioventricular block dogs."( Analysis of torsadogenic and pharmacokinetic profile of E-4031 in dogs bridging the gap of information between in vitro proarrhythmia assay and clinical observation in human subjects.
Ando, K; Chiba, K; Goto, A; Hagiwara-Nagasawa, M; Izumi-Nakaseko, H; Naito, AT; Sugiyama, A, 2018
)
0.48
"A three-compartment joint parent-metabolite population pharmacokinetic model was developed using concentrations of remifentanil and its metabolite remifentanil acid from two trials."( Population Pharmacokinetic Modelling for Estimation of Remifentanil Metabolic-Ratio Using Non-steady-State Concentrations under Rapidly Adaptive Dosing.
Chen, C; Simeoni, M, 2018
)
0.48
" Eligible studies reported data from pharmacokinetic evaluations of repaglinide in healthy adults according to different categories of CYP2C8 and SLCO1B1 genetic polymorphisms."( Effects of CYP2C8 and SLCO1B1 Genetic Polymorphisms on Repaglinide Pharmacokinetics: A Systematic Review and Meta-Analysis.
Chen, S; Cui, Y; Ma, L; Mu, G; Xiang, Q; Xie, Q; Zhang, Z; Zhou, S, 2019
)
0.51
"001) and Cmax (SMD: -0."( Effects of CYP2C8 and SLCO1B1 Genetic Polymorphisms on Repaglinide Pharmacokinetics: A Systematic Review and Meta-Analysis.
Chen, S; Cui, Y; Ma, L; Mu, G; Xiang, Q; Xie, Q; Zhang, Z; Zhou, S, 2019
)
0.51
"Physiologically based pharmacokinetic (PBPK) models often include several sets of correlated parameters, such as organ volumes and blood flows."( Accounting for inter-correlation between enzyme abundance: a simulation study to assess implications on global sensitivity analysis within physiologically-based pharmacokinetics.
Darwich, AS; Magni, P; Melillo, N; Rostami-Hodjegan, A, 2019
)
0.51
" Here, we describe the pharmacokinetic (PK) observations, along with modeling to further explore the interaction between ibrutinib and rituximab."( Systemic Exposure of Rituximab Increased by Ibrutinib: Pharmacokinetic Results and Modeling Based on the HELIOS Trial.
Avigdor, A; Bartlett, N; Cramer, P; de Jong, J; De Nicolao, G; Demirkan, F; Dilhuydy, MS; Fraser, G; Ganguly, S; Goy, A; Howes, A; Lavezzi, SM; Loscertales, J; Mahler, M; Neyens, M; Poggesi, I; Rule, S; Salman, M; Samoilova, O, 2019
)
0.51
" Herein, pharmacokinetic properties regarding lipophilicity, plasma protein binding (PPB) and metabolism are analyzed."( Pharmacokinetic properties of enantiomerically pure GluN2B selective NMDA receptor antagonists with 3-benzazepine scaffold.
Ametamey, SM; Börgel, F; Galla, F; Lehmkuhl, K; Schepmann, D; Wünsch, B, 2019
)
0.51
" In the present work, we investigated possible interactions of this novel drug with ATP-binding cassette (ABC) drug efflux transporters and cytochrome P450 (P450) biotransformation enzymes that play significant roles in the phenomenon of multidrug resistance (MDR) of cancer cells as well as in pharmacokinetic drug-drug interactions."( Interactions of Alectinib with Human ATP-Binding Cassette Drug Efflux Transporters and Cytochrome P450 Biotransformation Enzymes: Effect on Pharmacokinetic Multidrug Resistance.
Ceckova, M; Hofman, J; Kammerer, S; Küpper, JH; Novotna, E; Sorf, A; Staud, F; Sucha, S; Vagiannis, D, 2019
)
0.51
" The pharmacokinetic properties of DL0410 were analyzed by liquid chromatography‑mass spectrometry at oral doses of 25, 50 and 100 mg/kg and intravenous dose of 5 mg/kg."( Pharmacokinetics, excretion and metabolites analysis of DL0410, a dual‑acting cholinesterase inhibitor and histamine‑3 receptor antagonist.
Du, G; Liu, A; Pang, X; Song, J; Wang, L; Wu, S; Zhao, Y, 2019
)
0.51
" We previously constructed a physiologically-based pharmacokinetic (PBPK) model of rifampicin accounting for the components for the induction of cytochrome P450 (CYP) 3A/CYP2C9 and the inhibition of organic anion transporting polypeptide 1B (OATP1B)."( Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for Predicting Interactions With Drugs and an Endogenous Biomarker via Complex Mechanisms Including Organic Anion Transporting Polypeptide 1B Induction.
Asaumi, R; Imawaka, H; Kusuhara, H; Lee, W; Menzel, K; Nunoya, KI; Sugiyama, Y, 2019
)
0.51
" The objective of this study was to investigate the pharmacokinetic (PK) profile and tolerability of IDP-73152 and the effect of food after a single oral administration."( Pharmacokinetics and tolerability of IDP-73152 mesylate after a single oral administration under fasted and fed conditions in healthy volunteers.
An, KM; Jung, J; Lee, HS; Lee, M; Park, SI; Shin, D; Yu, KS, 2019
)
0.51
" However, there is limited pharmacokinetic information on this compound, especially its distribution in neuronal tissue and its route of excretion."( Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.
Anukunwithaya, T; Junsaeng, D; Khemawoot, P; Likhitwitayawuid, K; Songvut, P; Sritularak, B, 2019
)
0.51
"The addition of piperine could enhance some of the pharmacokinetic properties of oxyresveratrol via both intravenous and oral administration."( Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.
Anukunwithaya, T; Junsaeng, D; Khemawoot, P; Likhitwitayawuid, K; Songvut, P; Sritularak, B, 2019
)
0.51
" The method was applied in the analysis of the plasma, brain, and urine samples collected during pharmacokinetic studies in healthy male and female Sprague Dawley rats."( Bioanalytical method development and validation of MES207, a neuropeptide FF receptor antagonist, and its application in preclinical pharmacokinetics.
Avery, BA; Harrison, S; Kamble, SH; King, TI; McCurdy, CR; Mesangeau, C; Mottinelli, M; Roewekamp, AC; Sharma, A, 2019
)
0.51
"A new series of Proteolysis Targeting Chimeras (PROTACs) targeting Bruton's Tyrosine Kinase (BTK) was synthesized, with the goal of improving the pharmacokinetic properties of our previously reported PROTAC, MT802."( Design, synthesis and biological evaluation of Proteolysis Targeting Chimeras (PROTACs) as a BTK degraders with improved pharmacokinetic properties.
Buhimschi, AD; Crews, CM; Hines, J; Jaime-Figueroa, S; Toure, M, 2020
)
0.56
"Of the 25 enrolled patients, 24 were included in the pharmacokinetic analysis."( Pharmacokinetics of pitolisant in children and adolescents with narcolepsy.
Duvauchelle, T; Franco, P; Jacqz-Aigrain, E; Lecendreux, M; Plazzi, G; Robert, P; Schwartz, JC, 2020
)
0.56
" The sustained release capsule formulation was developed and characterized for physicochemical and pharmacokinetic properties."( Evaluation of rohitukine-enriched fraction of Dysoxylum binectariferum Hook.f. (leaves) as anti-arthritic phytopharmaceutical candidate: Chemical standardization, in-vivo validation, formulation development and oral pharmacokinetics.
Bharate, SB; Bharate, SS; Bhurta, D; Gandhi, SG; Gupta, M; Jaglan, S; Kumar, A; Kumar, V; Singh, D; Vishwakarma, RA, 2020
)
0.56
" The aim of this work is to develop a population pharmacokinetic model for ibrutinib and its dihydrodiol metabolite to quantify pharmacokinetic inter- and intra-individual variability, to evaluate the impact of several covariates on ibrutinib pharmacokinetic parameters, and to examine the relationship between exposure and clinical outcome."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
" Pharmacokinetic blood samples were taken from months 1 to 12 after inclusion."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
"A total of 89 patients and 1501 plasma concentrations were included in the pharmacokinetic analysis."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
"We present the first population pharmacokinetic model describing ibrutinib and dihydrodiol-ibrutinib concentrations simultaneously."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
" Assessment of the drug-drug interaction potential suggests that tofacitinib, baricitinib and upadacitinib generally show a favourable disposition with no perpetrator activity; however, as victim drugs, they show subtle pharmacokinetic differences that may be considered during polypharmacy."( Critical Assessment of Pharmacokinetic Drug-Drug Interaction Potential of Tofacitinib, Baricitinib and Upadacitinib, the Three Approved Janus Kinase Inhibitors for Rheumatoid Arthritis Treatment.
Babu, RJ; Dash, RP; Madgula, LMV; Srinivas, NR; Thomas, JA; Veeravalli, V, 2020
)
0.56
" This study aimed to predict the impact of drug-drug interactions and renal or hepatic impairment on tofacitinib pharmacokinetics using a physiologically based pharmacokinetic (PBPK) model."( Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure and Support Dosing Recommendations for Potential Drug-Drug Interactions or in Special Populations: An Example Using Tofacitinib.
Dowty, ME; Gupta, P; Krishnaswami, S; Menon, S; Tse, S, 2020
)
0.56
" Values for total clearance of compounds from plasma should be one of the most important pharmacokinetic parameters for predictions."( Predicted values for human total clearance of a variety of typical compounds with differently humanized-liver mouse plasma data.
Ito, S; Iwamoto, K; Kamimura, H; Mizunaga, M; Nakayama, K; Negoro, T; Nishiwaki, M; Nomura, Y; Suemizu, H; Yamazaki, H; Yoneda, N, 2020
)
0.56
" Secondary objectives included analysis of pharmacokinetic parameters, MAPK and PI3K pathway alterations, changes in tissue biomarkers, and preliminary anti-tumor efficacy."( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors.
Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021
)
0.62
" No pharmacokinetic interactions were identified."( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors.
Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021
)
0.62
" Nonetheless, pharmacodynamic analyses indicated target engagement and suggest rationale for further exploration of cobimetinib or ipatasertib in combination with other anticancer agents."( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors.
Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021
)
0.62
" However, a lack of systematic metabolic, pharmacokinetic and pharmacological studies limits its clinical use."( Metabolites profiling and pharmacokinetics of troxipide and its pharmacodynamics in rats with gastric ulcer.
Chen, B; Gao, J; Guo, H; Tang, J; Yan, Z; Zhou, C, 2020
)
0.56
"We fitted a population pharmacokinetic model to ampreloxetine plasma concentrations from single- and multiple-ascending dose trials in healthy subjects and two phase II studies in adult subjects with attention-deficit/hyperactive disorder or fibromyalgia at doses of 2-50 mg."( Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain.
Baldwin, RM; Bourdet, DL; Graham, RA; Kanodia, J; Lo, A, 2021
)
0.62
" The terminal half-life was 30-40 h, resulting in sustained drug concentrations for the entire 24-h dosing interval at steady state."( Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain.
Baldwin, RM; Bourdet, DL; Graham, RA; Kanodia, J; Lo, A, 2021
)
0.62
"The population pharmacokinetic model effectively described the plasma concentration-time profile of ampreloxetine after single and multiple doses."( Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain.
Baldwin, RM; Bourdet, DL; Graham, RA; Kanodia, J; Lo, A, 2021
)
0.62
"In our present experiment, the aim of this paper was to develop and fully validate an accurate and simple ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) assay for simultaneous quantification of acalabrutinib, ibrutinib, and their metabolites (ACP-5862 and PCI-45227) in beagle dog plasma and to survey the pharmacokinetic study of all analytes in beagle dogs."( Simultaneous measurement of acalabrutinib, ibrutinib, and their metabolites in beagle dog plasma by UPLC-MS/MS and its application to a pharmacokinetic study.
Jiang, Z; Lin, G; Shi, L; Wang, Y; Zhang, Y, 2020
)
0.56
" The objective of this analysis was to develop a population pharmacokinetic (PK) model to characterize the PKs of zanubrutinib and identify the potential impact of intrinsic and extrinsic covariates on zanubrutinib PK."( Population Pharmacokinetic Analysis of the BTK Inhibitor Zanubrutinib in Healthy Volunteers and Patients With B-Cell Malignancies.
Gao, Y; Jindal, A; Liu, L; Ou, YC; Sahasranaman, S; Tang, Z; Tariq, B; Wang, K, 2021
)
0.62
"To evaluate the pharmacokinetics and bioequivalence of tofacitinib citrate using pharmacokinetic parameters, a single-dose, randomized-sequence, two-way crossover study of tofacitinib citrate test (T) and reference (R) formulations, with a 4-day washout period, was performed."( Evaluation of tofacitinib citrate bioequivalence based on pharmacokinetic parameters in healthy Chinese subjects.
Hu, W; Lu, C; Wang, X; Yang, Y; Yu, B; Zhang, X, 2021
)
0.62
" The pharmacokinetic (PK) interactions studies on co-administration of ATR (8."( Pharmacokinetics and Pharmacodynamic Herb-Drug Interaction of Piperine with Atorvastatin in Rats.
Choudhary, DC; Nagrik, SS; Raje, A; Thomas, AB, 2021
)
0.62
" Atogepant was rapidly absorbed (median time to maximum plasma concentration, ∼2 hours) with an apparent terminal elimination half-life of ∼11 hours."( Single-Dose Pharmacokinetics and Safety of Atogepant in Adults With Hepatic Impairment: Results From an Open-Label, Phase 1 Trial.
Boinpally, R; Borbridge, L; Butler, M; Jakate, A; Periclou, A, 2021
)
0.62
"5-2 h post dose and then declined, with a terminal half-life of approximately 4 h in both cohorts."( Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine.
Dennehy, EB; Kerr, L; Khanna, R; Komori, M; Nery, ESM; Tsai, M; Wilbraham, D; Winner, P, 2021
)
0.62
"Niraparib (200 or 300 mg/day) was tolerable and had a favourable pharmacokinetic profile in Japanese patients with advanced solid tumours."( The safety, tolerability and pharmacokinetics of niraparib in Japanese patients with solid tumours: results of a phase I dose-escalation study.
Iwasa, S; Kase, Y; Kitano, S; Kondo, S; Koyama, T; Sato, J; Shibaki, R; Shimizu, T; Shimomura, A; Sumino, S; Suri, A; Tamura, K; Yamamoto, N; Yonemori, K, 2021
)
0.62
"A population pharmacokinetic modeling approach was applied to 39 healthy subjects."( Population Pharmacokinetics of Ibrutinib in Healthy Adults.
Al-Ghazawi, M; Najib, N; Najib, O; Saleh, MI; Salem, I, 2021
)
0.62
" Ex vivo pharmacodynamic data from phase 1 healthy volunteers clinically confirmed JAK1 selectivity of filgotinib."( JAK selectivity and the implications for clinical inhibition of pharmacodynamic cytokine signalling by filgotinib, upadacitinib, tofacitinib and baricitinib.
Campigotto, F; Di Paolo, JA; Galien, R; Meng, A; Murray, B; Traves, PG, 2021
)
0.62
" Serial blood and urine samples were collected for pharmacokinetic and pharmacodynamic assessments."( Safety, tolerability, pharmacokinetics, pharmacodynamics, bioavailability and food effect of single doses of soticlestat in healthy subjects.
Affinito, J; Chen, G; Cwik, M; Faessel, H; Merlo Pich, E; Wang, S, 2021
)
0.62
" The aim of the present study was to evaluate the pharmacokinetic (PK) interaction between FOT and MET in healthy subjects after multiple-dose administration."( Safety and pharmacokinetic interaction between fotagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin in healthy subjects.
Ding, Y; Li, C; Li, Y; Sun, H; Wang, M; Wu, M; Zhang, H; Zheng, W, 2021
)
0.62
" Using predictive physiologically-based pharmacokinetic (PBPK) models in the evaluation of the PK of alectinib, ruxolitinib, and panobinostat exposures in the presence of cancer, RIP, and HIP can help in using optimal doses with lower toxicity in these populations."( Physiologically-based pharmacokinetic model for alectinib, ruxolitinib, and panobinostat in the presence of cancer, renal impairment, and hepatic impairment.
Abu Kassab, HT; Abu Kwiak, AD; Abu Laila, SS; Abu Shameh, AJ; Al-Daoud, NM; Alhazabreh, MK; Alsmadi, MM; Alzughoul, SB; Jaber, SA; Jaradat, MM, 2021
)
0.62
" A population pharmacokinetic (popPK) model of tedatioxetine and its CYP2D6-dependent metabolite was developed based on pharmacokinetic data from 578 subjects."( Cytochrome P450 2D6 genotype-phenotype characterization through population pharmacokinetic modeling of tedatioxetine.
Areberg, J; Brøsen, K; Frederiksen, T; Schmidt, E; Stage, TB, 2021
)
0.62
"Accurately predicting the pharmacokinetics of compounds that are transporter substrates has been notoriously challenging using traditional in vitro systems and physiologically based pharmacokinetic (PBPK) modeling."( Improving the Translation of Organic Anion Transporting Polypeptide Substrates using HEK293 Cell Data in the Presence and Absence of Human Plasma via Physiologically Based Pharmacokinetic Modeling.
Bowman, CM; Chen, B; Chen, Y; Cheong, J; Liu, L; Mao, J, 2021
)
0.62
" Oral tofacitinib undergoes extensive hepatic metabolism and has numerous drug interactions and a half-life of 3 hours necessitating twice daily dosing."( Sublingual tofacitinib for alopecia areata: a roll-over pilot clinical trial and analysis of pharmacokinetics.
Bokhari, L; Lai, VWY; Sinclair, R, 2021
)
0.62
" This methodology was effectively used to estimate Pimavanserin in vivo human (K2EDTA) plasma concentration for a clinical pharmacokinetic study."( A Fully Validated UHPLC-MS/MS Method for the Estimation of Pimavanserin in Human (K2EDTA) Plasma and its Application to a Clinical Pharmacokinetic Study.
Aalapati, KK; Patnaik, RS; Singh, A, 2022
)
0.72
" HTL0018318 and donepezil do not demonstrate pharmacokinetic or pharmacodynamic interactions, indicating that HTL0018318 can be safely administered in combination with donepezil."( Safety and Pharmacokinetics of HTL0018318, a Novel M
Bakker, C; Cross, DM; Dickinson, S; Groeneveld, GJ; Klaassen, ES; Labots, G; Liptrot, J; Tasker, T; van der Aart, J, 2021
)
0.62
" The pharmacokinetic and pharmacodynamic data of acalabrutinib were also discussed."( Assessing the pharmacokinetics of acalabrutinib in the treatment of chronic lymphocytic leukemia.
Li, J; Miao, Y; Xu, W, 2021
)
0.62
" We hypothesized that the oral bioavailability of ibrutinib is limited by CYP3A isoform-mediated metabolism, and that this pathway can be inhibited to improve the pharmacokinetic properties of ibrutinib."( Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition.
Baker, SD; Byrd, JC; Eisenmann, ED; Fu, Q; Garrison, DA; Jin, Y; Muhowski, EM; Sparreboom, A; Uddin, ME; Weber, RH; Woyach, J, 2021
)
0.62
" Pharmacokinetic parameters were analyzed with noncompartmental methods."( Pharmacokinetics and Bioequivalence Studies of Roxatidine Acetate Hydrochloride Sustained-Release Capsule in Healthy Chinese Subjects.
Fan, X; Li, X; Li, Y; Tu, S; Xiao, G; Xu, B; Yuan, F; Zhang, P, 2022
)
0.72
" Here, we report safety, tolerability, pharmacokinetic and pharmacodynamic outcomes from a phase I, randomized, double-blind, placebo-controlled, multiple-rising-dose study of soticlestat in healthy adults."( Pharmacokinetics, pharmacodynamics and safety assessment of multiple doses of soticlestat in healthy volunteers.
Affinito, J; Chen, G; Cwik, M; Faessel, HM; Merlo Pich, E; Wang, S, 2022
)
0.72
"5 hour, and soticlestat elimination half-life was approximately 4 hours."( Pharmacokinetics, pharmacodynamics and safety assessment of multiple doses of soticlestat in healthy volunteers.
Affinito, J; Chen, G; Cwik, M; Faessel, HM; Merlo Pich, E; Wang, S, 2022
)
0.72
"The pharmacokinetic and pharmacodynamic profiles of soticlestat characterized here provided a data-driven rationale for clinical trial dose selection."( Pharmacokinetics, pharmacodynamics and safety assessment of multiple doses of soticlestat in healthy volunteers.
Affinito, J; Chen, G; Cwik, M; Faessel, HM; Merlo Pich, E; Wang, S, 2022
)
0.72
" An established physiologically-based pharmacokinetic (PBPK) modeling framework for age-dependent simulations was utilized."( Physiologically-Based Pharmacokinetic Modelling to Investigate Baricitinib and Tofacitinib Dosing Recommendations for COVID-19 in Geriatrics.
Chan, ECY; Wang, Z, 2022
)
0.72
" Objectives of this population pharmacokinetic (PK) analysis were to evaluate the dose-exposure relationship of tepotinib and its major circulating metabolite, MSC2571109A, and to identify the intrinsic/extrinsic factors that are predictive of PK variability."( Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, including data from the VISION study.
Girard, P; Jonsson, EN; Papasouliotis, O; Strotmann, R; Xiong, W, 2022
)
0.72
" Tepotinib has a long effective half-life of ~ 32 h."( Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, including data from the VISION study.
Girard, P; Jonsson, EN; Papasouliotis, O; Strotmann, R; Xiong, W, 2022
)
0.72
"Co-intake of ATR with Acai berry resulted in slight decrease in Cmax from 41."( Investigation of the effect of Acai berry on the pharmacokinetics of Atorvastatin, Alogliptin and Empagliflozin: a herb-drug interaction study.
Nanjappan, SK; Ravichandiran, V; Somabattini, RA, 2022
)
0.72
"There was a significant change in the AUC0-t and Cmax of ATR, ALO and EMPA after co-administration with Acai berry."( Investigation of the effect of Acai berry on the pharmacokinetics of Atorvastatin, Alogliptin and Empagliflozin: a herb-drug interaction study.
Nanjappan, SK; Ravichandiran, V; Somabattini, RA, 2022
)
0.72
" Zanubrutinib was given to mice intragastrically at 30 mg/kg to determine its pharmacokinetic parameters."( Quantitative evaluation and pharmacokinetic characteristics of the irreversible BTK inhibitor zanubrutinib in mouse plasma using LC-MS/MS.
Cheng, K; Feng, W; Kou, J; Li, M; Wei, J; You, H, 2022
)
0.72
" This analysis aimed to develop pharmacokinetic (PK) and pharmacodynamic (PD; BTK occupancy [BTKO]) models of evobrutinib and simulate PK and BTKO profiles under alternative dosing regimens."( Population pharmacokinetic and pharmacodynamic modeling of evobrutinib in healthy adult participants.
Dyroff, M; Girard, P; Mitchell, D; Papasouliotis, O, 2022
)
0.72
"The population pharmacokinetic (PK) and exposure-response (E-R) analyses for the safety of ibrutinib for the treatment of chronic graft-versus-host disease (cGVHD) is presented."( Population Pharmacokinetic and Exposure-Safety Analyses of Ibrutinib for the Treatment of Chronic Graft-Versus-Host Disease.
Atluri, H; Iwaki, Y; Mita, S; Ogawa, T, 2023
)
0.91
" The interaction between propofol and remifentanil was explored using the principles of the general pharmacodynamic interaction (GPDI) model."( Pharmacodynamic mechanism-based interaction model for the haemodynamic effects of remifentanil and propofol in healthy volunteers.
Colin, PJ; Eleveld, DJ; Koomen, JV; Struys, MMRF; Su, H, 2023
)
0.91
" The GPDI model provided a good framework for characterising the pharmacodynamic interaction between remifentanil and propofol on haemodynamic properties."( Pharmacodynamic mechanism-based interaction model for the haemodynamic effects of remifentanil and propofol in healthy volunteers.
Colin, PJ; Eleveld, DJ; Koomen, JV; Struys, MMRF; Su, H, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"The effects of single oral doses of terfenadine, diphenhydramine and placebo, alone or in combination with diazepam or alcohol, on psychomotor performance and subjective feelings were evaluated in a double-blind, crossover study in 20 normal male volunteers."( Effects of terfenadine and diphenhydramine alone or in combination with diazepam or alcohol on psychomotor performance and subjective feelings.
Hüther, KJ; Koch-Weser, J; Lundt, PV; Moser, L, 1978
)
0.26
"Apomorphine in combination with a peripheral dopamine receptor blocker (domeperidone) was administered to four parkinsonian patients in a double-blind placebo-controlled study."( Therapeutic efficacy of apomorphine combined with an extracerebral inhibitor of dopamine receptors in Parkinson's disease.
Corsini, GU; Del Zompo, M; Gessa, GL; Mangoni, A, 1979
)
0.26
" When 'C7/3-phthalimido-propyl' was combined with competitive antagonists such as (+)-benzetimide, atropine or homatropine the degree of antagonism was greater than expected for combination of 2 competitive antagonists."( Antimuscarinic action of an alkane-bis-ammonium compound alone and in combination with (+)-benzetimide.
Mitchelson, F,
)
0.13
"The effects on gastric emptying and gastrointestinal symptoms of treatment with cisapride alone and in combination with domperidone were investigated in 25 patients with chronic idiopathic dyspepsia."( Effect of treatment with cisapride alone or in combination with domperidone on gastric emptying and gastrointestinal symptoms in dyspeptic patients.
Iishi, H; Nakaizumi, A; Okuda, S; Tatsuta, M, 1992
)
0.28
"The antihypertensive effect of ketanserin in combination with beta-adrenergic blockade was assessed in a double-blind crossover (4 weeks) manner in 10 patients with essential hypertension."( Antihypertensive properties of ketanserin in combination with beta-adrenergic blocking agents.
Hedner, T; Persson, B, 1985
)
0.27
"The long-term safety and efficacy of ketanserin in the treatment of essential hypertension was assessed in monotherapy or in combination with the beta-blocker, metoprolol."( Long-term safety and efficacy of ketanserin in essential hypertension: ketanserin versus or in combination with metoprolol.
Mauersberger, H, 1986
)
0.27
"), but exerted a marked inhibition of muricide when combined with the above serotonin antagonists."( Anti-serotonin action in combination with noradrenaline-stimulating action is important for inhibiting muricide in midbrain raphe-lesioned rats.
Ohno, M; Takao, K; Ueki, S; Yamamoto, T, 1988
)
0.27
"The antihypertensive properties of ketanserin, a 5-HT2 receptor antagonist, was investigated in combination with beta-adrenoceptor blockade."( Ketanserin in combination with beta-adrenergic receptor blocking agents in the treatment of essential hypertension.
Hedner, T; Persson, B, 1984
)
0.27
" Using the unique features of column-switching HPLC combined with MS/MS, it was possible to develop the method in a short period of time."( Column-switching high-performance liquid chromatography combined with ionspray tandem mass spectrometry for the simultaneous determination of the platelet inhibitor Ro 44-3888 and its pro-drug and precursor metabolite in plasma.
Hopfgartner, G; Husser, C; Zell, M, 1997
)
0.3
" Volatile anesthetics are commonly combined with opioids."( Drug interactions: volatile anesthetics and opioids.
Gan, TJ; Ginsberg, B; Glass, PS; Howell, S, 1997
)
0.3
" We conclude that S9788 administered at the doses and schedule used in this study results in relevant plasma concentrations in humans and can safely be administered in combination with doxorubicin."( Phase IB study of doxorubicin in combination with the multidrug resistance reversing agent S9788 in advanced colorectal and renal cell cancer.
Backx, A; Bleiberg, H; De Mulder, PH; Gerard, B; Hecquet, B; Lucas, C; Punt, CJ; Tueni, E; Van Oosterom, AT; Voest, EE, 1997
)
0.3
"The objectives of this phase I study were to evaluate the toxic effects and the maximum tolerated dose (MTD) of S9788, a new modifier of multidrug resistance (MDR), when given alone and in combination with doxorubicin to patients with advanced solid tumors; to achieve a potentially active plasma concentration of S9788; and to study the pharmacokinetics of both drugs."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3
" S9788 was given alone as a 30-min infusion at day 1 and in combination with a 50-mg/m2 bolus of doxorubicin at days 8 and 29."( Phase I clinical and pharmacokinetic study of S9788, a new multidrug-resistance reversal agent given alone and in combination with doxorubicin to patients with advanced solid tumors.
Ardiet, C; Barbet, N; Bastian, G; Catimel, G; Clavel, M; Dumortier, A; Evene, E; Foy, M; Froudarakis, M; Grossin, F; Guastalla, JP; Lucas, C; Mazier, B; Négrier, S; Rebattu, P; Sarkany, M; Tranchand, B, 1998
)
0.3
"To evaluate the feasibility of administering biricodar (VX-710; Incel, Vertex Pharmaceuticals Inc, Cambridge, MA), an agent that modulates multidrug resistance (MDR) conferred by overexpression of both the multidrug resistance gene product (MDR1) P-glycoprotein and the MDR-associated protein (MRP) in vitro, in combination with paclitaxel."( Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP.
Aylesworth, C; Campbell, E; Chaturvedi, P; Drengler, R; Eckhardt, SG; Hammond, L; Harding, MW; Kraynak, M; Rowinsky, EK; Smith, L; Stephenson, J; Villalona, M; Von Hoff, DD; Wang, YM, 1998
)
0.3
" In combination with paclitaxel, biologically relevant VX-710 plasma concentrations are achieved and sustained for 24 hours, which simulates optimal pharmacologic conditions required for MDR reversal in vitro."( Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP.
Aylesworth, C; Campbell, E; Chaturvedi, P; Drengler, R; Eckhardt, SG; Hammond, L; Harding, MW; Kraynak, M; Rowinsky, EK; Smith, L; Stephenson, J; Villalona, M; Von Hoff, DD; Wang, YM, 1998
)
0.3
" For clinical use remifentanil must be combined with another anaesthetic agent."( [Remifentanil in gynecologic laparoscopy. A comparison of consciousness and circulatory effects of a combination with desflurane and propofol].
Bauer, C; Berg, K; Biedler, A; Langhammer, A; Larsen, R; Wilhelm, W, 1998
)
0.3
"25 microgram/kg/min) was combined with either desflurane (0."( [Remifentanil in gynecologic laparoscopy. A comparison of consciousness and circulatory effects of a combination with desflurane and propofol].
Bauer, C; Berg, K; Biedler, A; Langhammer, A; Larsen, R; Wilhelm, W, 1998
)
0.3
"Remifentanil in combination with either desflurane or propofol, used for general anaesthesia during gynaecological laparoscopy, will facilitate a smooth haemodynamic course as well as a rapid emergence thereafter."( [Remifentanil in gynecologic laparoscopy. A comparison of consciousness and circulatory effects of a combination with desflurane and propofol].
Bauer, C; Berg, K; Biedler, A; Langhammer, A; Larsen, R; Wilhelm, W, 1998
)
0.3
" When eliprodil was combined with an ineffective dose of L-701,324 (2."( Anticonvulsant effects of eliprodil alone or combined with the glycineB receptor antagonist L-701,324 or the competitive NMDA antagonist CGP 40116 in the amygdala kindling model in rats.
Ebert, U; Löscher, W; Wlaź, P, 1999
)
0.3
" Control of pH was used in combination with surfactants (polysorbate 20 and polysorbate 80), cosolvents (ethanol and propylene glycol), as well as uncharged and anionic complexing agents [hydroxypropyl beta-cyclodextrin (HPbetaCD) and sulfobutyl ether beta-cyclodextrin (SBEbetaCD)] to solubilize flavopiridol."( Solubilization of flavopiridol by pH control combined with cosolvents, surfactants, or complexants.
Li, P; Tabibi, SE; Yalkowsky, SH, 1999
)
0.3
" No direct drug-drug interactions were found in these studies, suggesting that repaglinide may be coprescribed with cimetidine, digoxin, or theophylline at the dosage used for monotherapy."( Drug interaction studies with repaglinide: repaglinide on digoxin or theophylline pharmacokinetics and cimetidine on repaglinide pharmacokinetics.
Hatorp, V; Thomsen, MS, 2000
)
0.31
"We describe the target-controlled administration of propofol and remifentanil, combined with monitoring of the bispectral index, during an awake craniotomy for removal of a left temporo-parietal tumour near the motor speech centre."( Target-controlled infusion of propofol and remifentanil combined with bispectral index monitoring for awake craniotomy.
Bonhomme, V; Born, JD; Brichant, JF; Dewandre, PY; Hans, P; Maertens de Noordhoudt, A, 2000
)
0.31
" Concentrations of the active metabolite of sibrafiban, Ro 44-3888, in plasma and urine were determined by column-switching liquid chromatography combined with tandem mass spectrometry."( Pharmacokinetics and pharmacodynamics of sibrafiban alone or in combination with ticlopidine and aspirin.
Birnböck, H; Chung, J; Ensor, H; Ertel, SI; Lausecker, B; Machin, SJ; MacKie, IJ; Wittke, B, 2000
)
0.31
"Remifentanil anesthesia, combined with small-dose propofol, desflurane, or sevoflurane, enables predictably fast and smooth early recovery after ear, nose, and throat surgery."( Recovery after anesthesia with remifentanil combined with propofol, desflurane, or sevoflurane for otorhinolaryngeal surgery.
Loop, T; Priebe, HJ, 2000
)
0.31
" The antiemetic efficacy of NK1 receptor antagonists against chemotherapy-induced emesis is, however, enhanced when combined with a 5-HT3 receptor antagonist."( Comparison of the neurokinin-1 antagonist GR205171, alone and in combination with the 5-HT3 antagonist ondansetron, hyoscine and placebo in the prevention of motion-induced nausea in man.
Clemes, SA; House, F; Palmer, JL; Reid, K; Somal, HS; Stott, JR; Troakes, C; Wright, RJ, 2000
)
0.31
"The enhancement of NK1 receptor antagonist antiemetic activity through combination with a 5-HT3 receptor antagonist is not replicated in motion-induced nausea."( Comparison of the neurokinin-1 antagonist GR205171, alone and in combination with the 5-HT3 antagonist ondansetron, hyoscine and placebo in the prevention of motion-induced nausea in man.
Clemes, SA; House, F; Palmer, JL; Reid, K; Somal, HS; Stott, JR; Troakes, C; Wright, RJ, 2000
)
0.31
"The purpose of this cardiac fast-track study was to evaluate the use of remifentanil (R) combined with intrathecal (IT) morphine as an alternative to sufentanil (S) during desflurane anesthesia with respect to postoperative pain control."( Fast-track cardiac anesthesia: use of remifentanil combined with intrathecal morphine as an alternative to sufentanil during desflurane anesthesia.
Bossard, R; Chi, L; Douning, LK; Latham, P; Morse, L; Shi, C; White, PF; Zarate, E, 2000
)
0.31
"As part of a cardiac fast-tracking program involving desflurane anesthesia, the use of intrathecal morphine in combination with a remifentanil infusion provided improved postoperative pain control, compared with IV sufentanil alone."( Fast-track cardiac anesthesia: use of remifentanil combined with intrathecal morphine as an alternative to sufentanil during desflurane anesthesia.
Bossard, R; Chi, L; Douning, LK; Latham, P; Morse, L; Shi, C; White, PF; Zarate, E, 2000
)
0.31
"32-10 mg/kg) was administered with scopolamine (0."( Effects of the cannabinoid ligand SR 141716A alone or in combination with delta9-tetrahydrocannabinol or scopolamine on learning in squirrel monkeys.
Moerschbaecher, JM; Nakamura-Palacios, EM; Winsauer, PJ, 2000
)
0.31
"Both fentanyl and the newer opioid remifentanil, when each is combined with isoflurane and propofol, allowed for fast-track cardiac anesthesia."( A randomized double-blinded multicenter comparison of remifentanil versus fentanyl when combined with isoflurane/propofol for early extubation in coronary artery bypass graft surgery.
Bowdle, TA; Bukenya, D; Cheng, D; Hillel, Z; Hogue, C; Howie, MB; Newman, MF; Pierce, ET, 2001
)
0.31
" In contrast, SR 141716 in combination with naloxone had a significantly supra-additive anorectic action."( Effects of the cannabinoid receptor antagonist SR 141716, alone and in combination with dexfenfluramine or naloxone, on food intake in rats.
Mukherjee, M; Robertson, K; Rowland, NE, 2001
)
0.31
" Propofol and remifentanil are known to reduce intraocular pressure (IOP), but no information is available regarding the effects of sevoflurane combined with remifentanil on IOP."( Intraocular pressure more reduced during anesthesia with propofol than with sevoflurane: both combined with remifentanil.
Auffarth, G; Böttiger, BW; Klett, J; Martin, E; Polarz, H; Schäfer, R; Völcker, HE, 2002
)
0.31
"In patients undergoing cataract surgery under general anesthesia with tracheal intubation, anesthetic regimens with propofol as well as with sevoflurane, both combined with remifentanil, decrease IOP significantly."( Intraocular pressure more reduced during anesthesia with propofol than with sevoflurane: both combined with remifentanil.
Auffarth, G; Böttiger, BW; Klett, J; Martin, E; Polarz, H; Schäfer, R; Völcker, HE, 2002
)
0.31
"This study examined the intra-operative and postoperative characteristics of a remifentanil infusion alone, or intermittent fentanyl bolus admistration combined with a propofol infusion, for the anaesthetic management of patients undergoing shock wave lithotripsy."( A comparison of anaesthetic techniques for shock wave lithotripsy: the use of a remifentanil infusion alone compared to intermittent fentanyl boluses combined with a low dose propofol infusion.
Blanc, I; Brauer, P; Burmeister, MA; Graefen, M; Standl, TG; Wintruff, M, 2002
)
0.31
"To compare the effect on glycemic control and weight gain of repaglinide versus metformin combined with bedtime NPH insulin in patients with type 2 diabetes."( Repaglinide versus metformin in combination with bedtime NPH insulin in patients with type 2 diabetes established on insulin/metformin combination therapy.
Furlong, NJ; Hardy, KJ; Hulme, SA; O'Brien, SV, 2002
)
0.31
"The efficacy and safety of ebastine 20 mg once daily given with and without food were compared in patients ages 12 to 70 years with seasonal allergic rhinitis (SAR) caused by mountain cedar allergen."( A double-blind, placebo-controlled study of the efficacy and safety of ebastine 20 mg once daily given with and without food in the treatment of seasonal allergic rhinitis.
Frank, H; George, G; Gillen, M; Lim, J; Rohatagi, SS, 2002
)
0.31
" In current experiments, the authors investigated its neuroprotective effect alone and in combination with recombinant tissue plasminogen activator (rt-PA) in thromboembolic focal cerebral ischemia in rats."( Reduced brain infarct volume and improved neurological outcome by inhibition of the NR2B subunit of NMDA receptors by using CP101,606-27 alone and in combination with rt-PA in a thromboembolic stroke model in rats.
Hussain, M; Li, Q; Shuaib, A; Yang, T; Yang, Y, 2003
)
0.32
"The data in this study suggested that postischemia treatment with CP-101,606-27 is neuroprotective in the current stroke model; however, the authors also note that although rt-PA may offer modest protection when used alone, combination with CP-101,606-27 did not appear to enhance its effects."( Reduced brain infarct volume and improved neurological outcome by inhibition of the NR2B subunit of NMDA receptors by using CP101,606-27 alone and in combination with rt-PA in a thromboembolic stroke model in rats.
Hussain, M; Li, Q; Shuaib, A; Yang, T; Yang, Y, 2003
)
0.32
" Therefore, its combination with acetylcholinesterase inhibitors (AChEIs) is anticipated."( Tolerability of memantine in combination with cholinesterase inhibitors in dementia therapy.
Hartmann, S; Möbius, HJ, 2003
)
0.32
" The present study tested the effect of different selective 5-HT(1A) receptor antagonists (WAY 100635, NAD-299, p-MPPI and LY 426965) in combination with a SSRI (paroxetine), on postsynaptic 5-HT function measured by increased expression of the immediate early gene, Arc."( Effect of different 5-HT1A receptor antagonists in combination with paroxetine on expression of the immediate-early gene Arc in rat brain.
Gray, K; Newson, M; Pei, Q; Sharp, T; Sprakes, M; Tordera, R, 2003
)
0.32
" The use of irinotecan together with raltitrexed is also being investigated, as is its combination with oxaliplatin."( Irinotecan in metastatic colorectal cancer: dose intensification and combination with new agents, including biological response modifiers.
Ducreux, M; Köhne, CH; Schwartz, GK; Vanhoefer, U, 2003
)
0.32
" gliclazide combined with bedtime NPH insulin in patients with Type 2 diabetes inadequately controlled with oral hypoglycaemic therapy [HbA1c>7."( Comparison of repaglinide vs. gliclazide in combination with bedtime NPH insulin in patients with Type 2 diabetes inadequately controlled with oral hypoglycaemic agents.
Furlong, NJ; Hardy, KJ; Hulme, SA; O'Brien, SV, 2003
)
0.32
"Over 13 weeks, both repaglinide and gliclazide, when combined with bedtime NPH insulin produce similar significant improvements in glycaemic control (-1%) and similar weight gain."( Comparison of repaglinide vs. gliclazide in combination with bedtime NPH insulin in patients with Type 2 diabetes inadequately controlled with oral hypoglycaemic agents.
Furlong, NJ; Hardy, KJ; Hulme, SA; O'Brien, SV, 2003
)
0.32
" In this study we examined midazolam and clonidine for premedication in combination with target controlled infusion anaesthesia (TCI) in patients undergoing orthopaedic shoulder surgery and analysed the effects on the peri- and postoperative course."( [Comparison of premedication with clonidine and midazolam combined with TCI for orthopaedic shoulder surgery].
Dietrich, PJ; Grottke, O; Krause, TH; Müller, J; Wappler, F, 2003
)
0.32
"Premedication with the alpha(2)-adrenoceptor agonist clonidine is as good as with benzodiazepines in combination with TCI."( [Comparison of premedication with clonidine and midazolam combined with TCI for orthopaedic shoulder surgery].
Dietrich, PJ; Grottke, O; Krause, TH; Müller, J; Wappler, F, 2003
)
0.32
" The activity of FTi SCH66336, alone or in combination with paclitaxel, gemcitabine, and radiotherapy, was examined in 3 cell lines, A-549, LX-1 and CaLu-6, by colorimetric MTT assay."( In vitro study of farnesyltransferase inhibitor SCH 66336, in combination with chemotherapy and radiation, in non-small cell lung cancer cell lines.
Ardizzoni, A; De Cupis, A; Favoni, RE; Loprevite, M; Mazzanti, P; Scolaro, T; Semino, C, 2004
)
0.32
" These results demonstrate that the PET imaging technique with specific labeled compounds in combination with microdialysis and a behavioral cognition task could be a useful method to clarify the mechanism of drugs in the living brains of experimental animals."( Effects of acute acetylcholinesterase inhibition on the cerebral cholinergic neuronal system and cognitive function: Functional imaging of the conscious monkey brain using animal PET in combination with microdialysis.
Fukumoto, D; Kakiuchi, T; Nishiyama, S; Ohba, H; Sato, K; Tsukada, H, 2004
)
0.32
" The present findings suggest that NK1 receptor antagonists, when combined with a SSRI, augment 5-HT release by modulating substance P/5-HT interactions in the dorsal raphe nucleus."( Blockade of substance P (neurokinin 1) receptors enhances extracellular serotonin when combined with a selective serotonin reuptake inhibitor: an in vivo microdialysis study in mice.
De Felipe, C; Froger, N; Gardier, AM; Guiard, BP; Guilloux, JP; Hunt, SP; Lanfumey, L; Przybylski, C; Seif, I, 2004
)
0.32
"Docetaxel combined with 72-hour flavopiridol was not feasible because of dose-limiting neutropenia."( Phase I trial of the cyclin-dependent kinase inhibitor flavopiridol in combination with docetaxel in patients with metastatic breast cancer.
Berman, A; Brahim, JS; Chow, C; Figg, WD; Parr, AL; Sparreboom, A; Steinberg, SM; Swain, SM; Tan, AR; Yang, X; Zhai, S, 2004
)
0.32
"To investigate the efficacy and safety of repaglinide alone and in combination with metformin therapy."( The efficacy of repaglinide monotherapy and in combination with metformin in Indonesian type 2 diabetes mellitus patients.
Luthariana, L; Soegondo, S; Subekti, I,
)
0.13
"treatment with repaglinide alone and in combination with metformin was efficacious in glycaemic control in OAD-naive or previous users."( The efficacy of repaglinide monotherapy and in combination with metformin in Indonesian type 2 diabetes mellitus patients.
Luthariana, L; Soegondo, S; Subekti, I,
)
0.13
" We investigated the activity of ZD6474 in combination with SC-236, a selective COX-2 inhibitor, to determine the antitumor activity of the simultaneous blockade of EGFR, COX-2, and VEGF functions."( Antitumor activity of ZD6474, a vascular endothelial growth factor-2 and epidermal growth factor receptor small molecule tyrosine kinase inhibitor, in combination with SC-236, a cyclooxygenase-2 inhibitor.
Bianco, R; Bianco, RA; Ciardiello, F; De Vita, F; Fontanini, G; Martinelli, E; Morgillo, F; Romano, M; Tortora, G; Troiani, T; Tuccillo, C, 2005
)
0.33
" As ciproxifan and thioperamide are inhibitors of cytochrome P450 enzymes, responsible for metabolizing risperidone and haloperidol, the possibility that the augmentation of antipsychotics by imidazoles resulted from drug-drug interactions was tested."( Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs.
Ballard, ME; Cowart, M; Decker, MW; Esbenshade, TA; Faghih, R; Fox, GB; Hancock, AA; Pan, L; Roberts, S; Rueter, LE; Zhang, M, 2005
)
0.33
"One of the emerging problems concerning the use of antiangiogenic drugs, when used in combination with certain chemotherapy regimens, is enhanced rates and severity of adverse clotting events."( In vitro procoagulant activity induced in endothelial cells by chemotherapy and antiangiogenic drug combinations: modulation by lower-dose chemotherapy.
du Manoir, J; Francia, G; Hicklin, DJ; Kerbel, RS; Ma, L; Rak, J; Viloria-Petit, A, 2005
)
0.33
"The aim of this prospective, randomized, double-blind study was to determine the effects of adding nitrous oxide on sevoflurane requirement for blunting sympathetic responses after surgical incision combined with two different target-controlled concentrations of remifentanil (1 and 3 ng mL(-1)) in female."( The effect of adding nitrous oxide on MAC of sevoflurane combined with two target-controlled concentrations of remifentanil in women.
Albertin, A; Bergonzi, PC; Casati, A; Lombardo, F; Moizo, E; Torri, G, 2005
)
0.33
"Flavopiridol, a cyclin-dependent kinase inhibitor, transcription inhibitor, and DNA-interacting agent, was combined with cisplatin or carboplatin to establish toxicities, evaluate pharmacokinetics, and examine its effects on patient cancers and levels of selected polypeptides in patient peripheral blood mononuclear cells (PBMC)."( Phase 1 trial of flavopiridol combined with cisplatin or carboplatin in patients with advanced malignancies with the assessment of pharmacokinetic and pharmacodynamic end points.
Adjei, AA; Ames, MM; Atherton, PJ; Bible, KC; Daiss, MK; Erlichman, C; Isham, CR; Kaufmann, SH; Lee, YK; Lensing, JL; Nelson, SA; Piens, J; Reid, JM; Rubin, J; Rubin, SL; Sloan, JA, 2005
)
0.33
" Flavopiridol combined with carboplatin resulted in unexpectedly high toxicities and one treatment-related death."( Phase 1 trial of flavopiridol combined with cisplatin or carboplatin in patients with advanced malignancies with the assessment of pharmacokinetic and pharmacodynamic end points.
Adjei, AA; Ames, MM; Atherton, PJ; Bible, KC; Daiss, MK; Erlichman, C; Isham, CR; Kaufmann, SH; Lee, YK; Lensing, JL; Nelson, SA; Piens, J; Reid, JM; Rubin, J; Rubin, SL; Sloan, JA, 2005
)
0.33
"Reality orientation therapy combined with cholinesterase inhibitors has not been evaluated in patients with Alzheimer's disease."( Reality orientation therapy combined with cholinesterase inhibitors in Alzheimer's disease: randomised controlled trial.
Bartorelli, L; Bernabei, R; Carbone, G; Frisoni, GB; Giacobini, E; Lambertucci, P; Onder, G; Silveri, MC; Zanetti, O, 2005
)
0.33
" Therefore, drug therapy targeted to VEGF receptors and EGFRs, when combined with radiotherapy (RT), may improve tumor control and provide wider applicability."( ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinase activity in combination with radiotherapy.
Bianco, C; Ciardiello, F; Dimery, I; Frederick, B; Gustafson, D; Raben, D, 2006
)
0.33
" In this clinical study we investigated the performance of propofol TCI in combination with remifentanil."( The performance of a target-controlled infusion of propofol in combination with remifentanil: a clinical investigation with two propofol formulations.
Brauer, U; Frenkel, C; Hoeft, A; Kiefer, N; Knüfermann, P; Scholz, M; Wietasch, JK; Zinserling, J, 2006
)
0.33
"To evaluate the preemptive effects of diclofenac sodium, in combination with remifentanil and ketamine."( The preemptive use of diclofenac sodium in combination with ketamine and remifentanil does not enhance postoperative analgesia after laparoscopic gynecological procedures.
Aypar, U; Canbay, O; Celebi, N; Coskun, F; Karakas, O; Peker, L, 2006
)
0.33
"This study compared the efficacy and safety profile of remifentanil and sufentanil in combination with propofol for anesthesia in adult patients undergoing nonemergency intracranial surgery."( Comparison of the time to extubation after use of remifentanil or sufentanil in combination with propofol as anesthesia in adults undergoing nonemergency intracranial surgery: a prospective, randomized, double-blind trial.
Blanchet, B; Coste, J; Disdet, M; Djian, MC; Gury, C; Joly, LM; Pesce, F; Raggueneau, JL; Roux, FX; Sermet, A; Vazquez, V, 2006
)
0.33
"In these adults undergoing nonemergency intracranial surgery, there was no significant difference in extubation time between those receiving remifentanil and sufentanil infusions adjusted based on hemodynamic parameters in combination with propofol administered by TCI."( Comparison of the time to extubation after use of remifentanil or sufentanil in combination with propofol as anesthesia in adults undergoing nonemergency intracranial surgery: a prospective, randomized, double-blind trial.
Blanchet, B; Coste, J; Disdet, M; Djian, MC; Gury, C; Joly, LM; Pesce, F; Raggueneau, JL; Roux, FX; Sermet, A; Vazquez, V, 2006
)
0.33
"This randomized prospective study with blinded postanesthesia care unit (PACU) observers compared the recovery profiles in morbidly obese patients who received sevoflurane or desflurane for maintenance of anesthesia in combination with a remifentanil target controlled infusion (TCI)."( Postoperative results after desflurane or sevoflurane combined with remifentanil in morbidly obese patients.
De Baerdemaeker, LE; Den Blauwen, NM; Herregods, LL; Jacobs, S; Mortier, EP; Pattyn, P; Struys, MM, 2006
)
0.33
"50 morbidly obese patients scheduled for laparoscopic gastric banding were included to receive BIS-guided sevoflurane or desflurane anesthesia with BIS-triggered inhalation boli in combination with remifentanil TCI."( Postoperative results after desflurane or sevoflurane combined with remifentanil in morbidly obese patients.
De Baerdemaeker, LE; Den Blauwen, NM; Herregods, LL; Jacobs, S; Mortier, EP; Pattyn, P; Struys, MM, 2006
)
0.33
" ZD6474 in combination with oxaliplatin has synergistic antiproliferative properties in human colorectal cancer cell lines in vitro when oxaliplatin is administered before ZD6474."( Sequence-dependent inhibition of human colon cancer cell growth and of prosurvival pathways by oxaliplatin in combination with ZD6474 (Zactima), an inhibitor of VEGFR and EGFR tyrosine kinases.
Ciardiello, F; Eckhardt, SG; Lockerbie, O; Morrow, M; Troiani, T, 2006
)
0.33
"To observe the impacts of doxapram on anesthetic efficacy and respiratory and circulatory functions during anesthesia with remifentanil given by target-controlled infusion (TCI) combined with propofol in painless artificial abortion."( [Clinical observation of target-controlled remifentanil infusion combined with propofol and doxapram in painless artificial abortion].
Dong, T; Li, JX; Liu, JH; Tan, ZM, 2006
)
0.33
"Doxapram may attenuate respiratory and circulatory depression during anesthesia with remifentanil given by TCI combined with propofol in painless artificial abortion, and provide comparable anesthetic efficacy."( [Clinical observation of target-controlled remifentanil infusion combined with propofol and doxapram in painless artificial abortion].
Dong, T; Li, JX; Liu, JH; Tan, ZM, 2006
)
0.33
" This effect was less pronounced when FK866 was used in combination with another alkylating agent, melphalan."( Chemopotentiating effects of a novel NAD biosynthesis inhibitor, FK866, in combination with antineoplastic agents.
Azzam, K; Hasmann, M; Nüssler, V; Pelka-Fleischer, R; Pogrebniak, A; Schemainda, I, 2006
)
0.33
"This review describes the current knowledge on drug-drug and food-drug interactions with repaglinide and nateglinide."( Drug-drug and food-drug pharmacokinetic interactions with new insulinotropic agents repaglinide and nateglinide.
Scheen, AJ, 2007
)
0.34
" A Phase II study was designed to evaluate VX-710 in combination with doxorubicin and vincristine in patients with sensitive, recurrent small cell lung cancer (SCLC)."( A phase II study of the safety and efficacy of the multidrug resistance inhibitor VX-710 combined with doxorubicin and vincristine in patients with recurrent small cell lung cancer.
Gandhi, L; Harding, MW; Johnson, BE; Langer, CJ; Lynch, TJ; Moore, M; Neubauer, M; Ross, HJ, 2007
)
0.34
"To study the efficacy and safety of Reinhartdt and sea cucumber capsule (RSC) combined with donepezil in treating Alzheimer's disease (AD), and its effect on thyroid function axis."( [Clinical study of Reinhartdt and sea cucumber capsule combined with donepezil in treating Alzheimer's disease].
Liang, LZ; Yan, YX; Zhou, ZL, 2007
)
0.34
"Sixty-eight patients were randomly assigned to the RSC group, the Donepezil group and the combined treatment group, who were treated for 3 and 6 months with RSC, Donepezil and RSC combined with Donepezil, respectively."( [Clinical study of Reinhartdt and sea cucumber capsule combined with donepezil in treating Alzheimer's disease].
Liang, LZ; Yan, YX; Zhou, ZL, 2007
)
0.34
"RSC combined with Donepezil in treating AD is effective and safe with no evident adverse reaction, better than single drug treatment, which may be through influencing the metabolism of thyroid hormones to improve the cognition function of AD patients."( [Clinical study of Reinhartdt and sea cucumber capsule combined with donepezil in treating Alzheimer's disease].
Liang, LZ; Yan, YX; Zhou, ZL, 2007
)
0.34
" Vandetanib has demonstrated enhanced efficacy in combination with radiation therapy (RT) in human tumor models."( Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
Frederick, B; Gustafson, DL; Merz, AL; Raben, D, 2008
)
0.35
" These effects were also observed in vivo, where the combination with piplartine but not piperine with 5-FU led to a higher tumor growth inhibition."( In vitro and in vivo antitumor effect of 5-FU combined with piplartine and piperine.
Alves, AP; Bezerra, DP; Costa-Lotufo, LV; de Alencar, NM; de Castro, FO; de Moraes, MO; Elmiro, FJ; Lima, MA; Lima, MW; Mesquita, RO; Pessoa, C; Silveira, ER, 2008
)
0.35
"Cholinesterase inhibitors (ChEIs) could be involved in several drug-drug interactions (DDIs) because of their complex pharmacodynamic and/or pharmacokinetic properties."( Drug interactions with cholinesterase inhibitors: an analysis of the French pharmacovigilance database and a comparison of two national drug formularies (Vidal, British National Formulary).
Bagheri, H; Lapeyre-Mestre, M; Montrastruc, JL; Sommet, A; Tavassoli, N, 2007
)
0.34
"This in vivo study was designed to determine the optimal doses and schedules of vandetanib, a dual epidermal growth factor receptor (EGFR)-vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan in a murine xenograft model of human colon cancer."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
"The greatest antitumor efficacy was observed in the groups receiving the highest dose of vandetanib given continuously (concurrent schedule), alone or in combination with irinotecan."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
"These data suggest that higher, sustained concentrations of vandetanib (versus intermittent), alone and in combination with irinotecan, result in optimal antitumor efficacy in this model and may have implications for the design of future clinical studies with this drug."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
" The effect of ZD6474, a potent inhibitor of VEGF-receptor-2, was evaluated in combination with either radiotherapy or temozolomide."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
" ZD6474 30 mg/kg was given alone or in combination with radiotherapy 12 Gy x 1 or with temozolomide 100 mg/kg for 3 days."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
"ZD6474 in combination with radiotherapy significantly decreased tumour area by 66% compared with controls whereas the combination with temozolomide decreased tumour area by 74%."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
"ZD6474 in combination with two standard modalities in the treatment of malignant glioma, radiotherapy and chemotherapy, markedly decreased the growth of an intracerebral experimental glioma."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
"To compare the effect of remifentanil combined with desflurane or isoflurane on the quality of the operative field and surgical conditions, blood loss, and recovery during tympanoplasty or endoscopic sinus surgery."( Hypotensive anaesthesia with remifentanil combined with desflurane or isoflurane in tympanoplasty or endoscopic sinus surgery: a randomised, controlled trial.
Gursoy, S; Kaygusuz, K; Kol, IO; Mimaroglu, C; Yildirim, A, 2008
)
0.35
"To compare the effects of fentanyl or remifentanil in combination with midazolam on hemodynamic parameters, pain, and satisfaction profile in cataract surgery."( Remifentanil versus fentanyl in combination with midazolam for retrobulbar block in cataract surgery.
Bahadir, M; Cok, OY; Ertan, A, 2008
)
0.35
"Many drugs have been reported to interact with repaglinide in patients with type 2 diabetes mellitus, resulting in hypoglycemia."( Severe hypoglycemia from clarithromycin-repaglinide drug interaction.
Khamaisi, M; Leitersdorf, E, 2008
)
0.35
" alone and in combination with at least one dose of rimonabant."( Apparent affinity estimates of rimonabant in combination with anandamide and chemical analogs of anandamide in rhesus monkeys discriminating Delta9-tetrahydrocannabinol.
McMahon, LR, 2009
)
0.35
" Here, we report that AKR-501 in combination with TPO has additive effect on megakaryocytopoiesis."( AKR-501 (YM477) in combination with thrombopoietin enhances human megakaryocytopoiesis.
Abe, M; Fukushima-Shintani, M; Hirayama, F; Iwatsuki, Y; Kawasaki, T; Sugasawa, K; Suzuki, K, 2008
)
0.35
"The aim of this study was to evaluate the safety and tolerability of escalating doses of flavopiridol/ paclitaxel/carboplatin in patients with advanced-stage non-small-cell lung cancer (NSCLC) as well as the pharmacokinetics and activity of flavopiridol when used in combination with paclitaxel/carboplatin."( Phase I study of flavopiridol in combination with Paclitaxel and Carboplatin in patients with non-small-cell lung cancer.
Bukowski, RM; Cogswell, J; Fidias, P; George, S; Kasimis, BS; Schwarzenberger, P; Shapiro, GI, 2008
)
0.35
" These results provide a strong argument for using alogliptin in combination with pioglitazone."( The dipeptidyl peptidase-4 inhibitor alogliptin in combination with pioglitazone improves glycemic control, lipid profiles, and increases pancreatic insulin content in ob/ob mice.
Asakawa, T; Kataoka, O; Moritoh, Y; Odaka, H; Takeuchi, K, 2009
)
0.35
"To compare the hemodynamics and post-anesthetic recovery of total intravenous anesthesia (TIVA) with remifentanil or fentanyl combined with propofol administered by target controlled infusion (TCI) in neurosurgery."( [Remifentanil and fentanyl combined with propofol administered by target controlled infusion in neurosurgery].
Bai, N; Cheng, Z; Guo, Q; Wang, Y; Yang, S, 2009
)
0.35
"TIVA with remifentanil or fentanyl combined with propofol administered by TCI in neurosurgical operation can provided steadible hemodynamics."( [Remifentanil and fentanyl combined with propofol administered by target controlled infusion in neurosurgery].
Bai, N; Cheng, Z; Guo, Q; Wang, Y; Yang, S, 2009
)
0.35
" The purpose of this study was to evaluate the use of either desflurane or propofol, both combined with remifentanil, in patients with MG undergoing a video-assisted thoracoscopic-extended thymectomy (VATET)."( The use of desflurane or propofol in combination with remifentanil in myasthenic patients undergoing a video-assisted thoracoscopic-extended thymectomy.
Benigni, A; Bortolotti, G; Carrara, B; Giardini, D; Gritti, P; Khotcholava, M; Lanterna, LA; Sonzogni, V, 2009
)
0.35
" The time-to-awakening, post-operatory pH and base excess were significantly different in the two groups, with a decreasing mean arterial pressure in the group administered with desflurane."( The use of desflurane or propofol in combination with remifentanil in myasthenic patients undergoing a video-assisted thoracoscopic-extended thymectomy.
Benigni, A; Bortolotti, G; Carrara, B; Giardini, D; Gritti, P; Khotcholava, M; Lanterna, LA; Sonzogni, V, 2009
)
0.35
" In this study, the effects of insulin glargine (IG) in combination with repaglinide or acarbose on glycemic parameters were investigated."( The investigation of the efficacy of insulin glargine on glycemic control when combined with either repaglinide or acarbose in obese Type 2 diabetic patients.
Duran, C; Ercan, I; Ersoy, C; Erturk, E; Guclu, M; Imamoglu, S; Kiyici, S; Selimoglu, H; Tuncel, E, 2009
)
0.35
" The in vivo pharmacokinetics revealed that curcumin entrapped nanoparticles demonstrate at least 9-fold increase in oral bioavailability when compared to curcumin administered with piperine as absorption enhancer."( Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer.
Ankola, DD; Beniwal, V; Kumar, MN; Shaikh, J; Singh, D, 2009
)
0.35
"To observe clinical therapeutic effect of acupuncture combined with Yizhi Jiannao Granules for treatment of Alzheimer's disease and its effects on intelligence, daily life and social activity ability."( [Clinical observation on acupuncture combined with Yizhi Jiannao granules for treatment of Alzheimer's disease].
Dong, KL; Peng, XW, 2009
)
0.35
"Acupuncture combined with Yizhi Jiannao Granules has a significant therapeutic effect on Alzheimer's disease, which is better than that of Yizhi Jiannao Granules or Aricept."( [Clinical observation on acupuncture combined with Yizhi Jiannao granules for treatment of Alzheimer's disease].
Dong, KL; Peng, XW, 2009
)
0.35
" Potential pharmacokinetic (PK) drug-drug interactions of alogliptin with pioglitazone or glyburide were evaluated in healthy adults."( Coadministration of pioglitazone or glyburide and alogliptin: pharmacokinetic drug interaction assessment in healthy participants.
Fleck, P; Karim, A; Laurent, A; Mekki, Q; Munsaka, M; Wann, E, 2009
)
0.35
" With 20 microgram/ml remifentanil in normal saline, postoperative PCA was administered with a background infusion at 2 ml/h following 2 ml as a loading dose and 1ml demand dose with a 3-minute lockout period."( Remifentanil combined with low-dose ketamine for postoperative analgesia of lower limb fracture: a double-blind, controlled study.
Deng, GF; Tian, B; Wang, S; Zhang, SG; Zheng, JP, 2009
)
0.35
"This randomized, double-blind, dose-ranging, placebo-controlled, phase 2 trial evaluated the neurokinin-1 receptor antagonist casopitant mesylate in combination with ondansetron/dexamethasone (ond/dex) for the prevention of chemotherapy-induced nausea and vomiting (CINV) related to moderately emetogenic chemotherapy (MEC)."( Phase 2 trial results with the novel neurokinin-1 receptor antagonist casopitant in combination with ondansetron and dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in cancer patients receiving moderately emetogenic chemothera
Albert, I; Arpornwirat, W; Bandekar, RR; Grunberg, SM; Hansen, VL; Levin, J, 2009
)
0.35
" The recommended phase II dose of flavopiridol was 45 mg/m in combination with irinotecan and gemcitabine every 2 weeks."( A phase I study of flavopiridol in combination with gemcitabine and irinotecan in patients with metastatic cancer.
Chyi Lee, F; Fekrazad, HM; Rabinowitz, I; Royce, M; Smith, HO; Verschraegen, CF, 2010
)
0.36
"The every 2 week dosing is well tolerated with a phase II recommended dose of 45 mg/m of flavopiridol in combination with irinotecan (80 mg/m) and gemcitabine (800 mg/m)."( A phase I study of flavopiridol in combination with gemcitabine and irinotecan in patients with metastatic cancer.
Chyi Lee, F; Fekrazad, HM; Rabinowitz, I; Royce, M; Smith, HO; Verschraegen, CF, 2010
)
0.36
" We assessed the effects of rimonabant, alone and in combination with fenofibrate or ezetimibe, on adipokine levels in obese/overweight patients with dyslipidemia."( Effects of rimonabant, as monotherapy and in combination with fenofibrate or ezetimibe, on plasma adipokine levels: a pilot study.
Derdemezis, CS; Elisaf, M; Florentin, M; Liberopoulos, EN; Tellis, CC; Tselepis, A, 2010
)
0.36
" This study investigated (1) the effect of food on alogliptin pharmacokinetics and tolerability and (2) pharmacokinetic interactions between alogliptin and metformin or cimetidine and tolerability of alogliptin when administered with either drug."( Pharmacokinetics of alogliptin when administered with food, metformin, or cimetidine: a two-phase, crossover study in healthy subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Li, X; Mekki, Q; Wann, E, 2010
)
0.36
" Consequently, we studied intraoperative urinary output of two groups, patients administered with remifentanil and those without remifentanil administration."( [Comparison of urinary output during general anesthesia, between patients administered with remifentanil and those without remifentanil administration].
Hara, M; Kawaguchi, M; Kawai, M; Maseki, M; Nakata, J; Takahashi, T; Teramoto, Y; Yamaguchi, S, 2010
)
0.36
"We compared urinary output during general anesthesia, of 327 patients administered with remifentanil (Group R) and 314 patients without remifentanil administration (Group NR) retrospectively."( [Comparison of urinary output during general anesthesia, between patients administered with remifentanil and those without remifentanil administration].
Hara, M; Kawaguchi, M; Kawai, M; Maseki, M; Nakata, J; Takahashi, T; Teramoto, Y; Yamaguchi, S, 2010
)
0.36
"We found a significance difference in urinary output during anesthesia, between patients administered with remifentanil and those without remifentanil administration."( [Comparison of urinary output during general anesthesia, between patients administered with remifentanil and those without remifentanil administration].
Hara, M; Kawaguchi, M; Kawai, M; Maseki, M; Nakata, J; Takahashi, T; Teramoto, Y; Yamaguchi, S, 2010
)
0.36
" Compared with standard practice, targeting an Entropy or BIS value of 50 did not result in a reduction of propofol consumption during general anaesthesia combined with regional anaesthesia as performed by an experienced anaesthesiologist in orthopaedic patients."( The Entropy Module and Bispectral Index as guidance for propofol-remifentanil anaesthesia in combination with regional anaesthesia compared with a standard clinical practice group.
Bruhn, J; Ellerkmann, RK; Hoeft, A; Riese, G; Soehle, M; Wirz, S; Zinserling, J, 2010
)
0.36
" This study evaluates the therapeutic potential of masitinib in pancreatic cancer, as a single agent and in combination with gemcitabine."( Masitinib combined with standard gemcitabine chemotherapy: in vitro and in vivo studies in human pancreatic tumour cell lines and ectopic mouse model.
Bader, T; Bertucci, F; Castéran, N; Dubreuil, P; Finetti, P; Hanssens, K; Hermine, O; Humbert, M; Iovanna, J; Letard, S; Mansfield, CD; Moussy, A, 2010
)
0.36
"In vitro investigation of pharmacokinetic drug-drug interactions (DDIs) has officially been part of the regulatory pathway for new drugs in the USA since the publication of an FDA guidance on the subject in 1997."( The nasty surprise of a complex drug-drug interaction.
Bode, C, 2010
)
0.36
"To investigate the killing effect of ZD6474 combined with adriamycin (ADM) on MCF-7 human breast cancer cells."( [Inhibitory effect of ZD6474 combined with adriamycin on MCF-7 human breast cancer cells in vitro].
He, BF; Luo, RC; Miao, JX; Ruan, J; Shen, J; Zhao, P; Zheng, H, 2010
)
0.36
"To evaluate the efficacy and safety of masitinib combined with gemcitabine in patients with advanced pancreatic cancer."( Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer.
Deplanque, G; Hammel, P; Hermine, O; Kinet, JP; Levy, P; Mitry, E; Mornex, F; Moussy, A; Raymond, E; Rougier, P; Seitz, JF, 2010
)
0.36
"Twenty-two non-randomised patients with unresectable, locally advanced (n = 9) or metastatic pancreatic cancer (n = 13) received oral masitinib (9 mg/kg/day) combined with standard gemcitabine."( Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer.
Deplanque, G; Hammel, P; Hermine, O; Kinet, JP; Levy, P; Mitry, E; Mornex, F; Moussy, A; Raymond, E; Rougier, P; Seitz, JF, 2010
)
0.36
"The efficacy and safety of masitinib combined with gemcitabine are encouraging, with extended survival and median TTP that support initiation of a phase 3 trial."( Safety and activity of masitinib in combination with gemcitabine in patients with advanced pancreatic cancer.
Deplanque, G; Hammel, P; Hermine, O; Kinet, JP; Levy, P; Mitry, E; Mornex, F; Moussy, A; Raymond, E; Rougier, P; Seitz, JF, 2010
)
0.36
"This Phase I study investigated the safety, tolerability, and pharmacokinetics of vandetanib when administered with either gemcitabine plus cisplatin (GC) or vinorelbine plus cisplatin (VC) in patients with previously untreated locally advanced or metastatic non-small cell lung cancer."( A phase I study of Vandetanib in combination with vinorelbine/cisplatin or gemcitabine/cisplatin as first-line treatment for advanced non-small cell lung cancer.
Blackhall, FH; Kennedy, SJ; Milenkova, T; Nicolson, M; O'brien, M; Schmid, P; Taylor, P; Thatcher, N, 2010
)
0.36
"In this study, in patients with previously untreated advanced non-small cell lung cancer, vandetanib 100 mg/d in combination with either VC or GC was not tolerated."( A phase I study of Vandetanib in combination with vinorelbine/cisplatin or gemcitabine/cisplatin as first-line treatment for advanced non-small cell lung cancer.
Blackhall, FH; Kennedy, SJ; Milenkova, T; Nicolson, M; O'brien, M; Schmid, P; Taylor, P; Thatcher, N, 2010
)
0.36
"Patients with type 2 diabetes mellitus (T2DM) are generally treated with many pharmacological compounds and are exposed to a high risk of drug-drug interactions."( Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions.
Scheen, AJ, 2010
)
0.36
" A two-compartment population pharmacokinetic model estimating oral clearance, between-patient variability in oral clearance, central volume of distribution, and residual variability in combination with historical estimates of first-order absorption rate constant, intercompartmental clearance, and peripheral volume of distribution adequately described the sparse MPA data."( Population pharmacokinetic analysis of mycophenolic acid coadministered with either tasocitinib (CP-690,550) or tacrolimus in adult renal allograft recipients.
Busque, S; Chan, G; Krishnaswami, S; Lamba, M; Melcher, M; Tafti, B, 2010
)
0.36
" We report a case of a 45-year-old woman with DM who underwent laparotomy for uterine cancer under general anesthesia combined with epidural anesthesia."( [Successful management of a patient with myotonic dystrophy under total intravenous anesthesia with propofol, remifentnil and rocuronium bromide, combined with epidural anesthesia].
Hirai, A; Nakanishi, T; Nishihama, M; Shimosaka, M; Uchikado, M; Uehara, A, 2010
)
0.36
"The purpose of this study was to determine the ability of radiation therapy (RT) combined with the tyrosine kinase inhibitors (TKI) vandetanib (antiepidermal growth factor receptor [EGFR] plus antivascular endothelial growth factor receptor [anti-VEGFR]) and cediranib (anti-VEGFR) to inhibit glioblastoma multiforme (GBM) growth."( Epidermal growth factor receptor expression modulates antitumor efficacy of vandetanib or cediranib combined with radiotherapy in human glioblastoma xenografts.
Daroczi, B; Dicker, AP; Lawrence, YR; Liu, Y; Wachsberger, PR; Xu, X, 2012
)
0.38
" In U87MG EGFR-null cells, TKI combined with radiation was no better than radiation therapy alone."( Epidermal growth factor receptor expression modulates antitumor efficacy of vandetanib or cediranib combined with radiotherapy in human glioblastoma xenografts.
Daroczi, B; Dicker, AP; Lawrence, YR; Liu, Y; Wachsberger, PR; Xu, X, 2012
)
0.38
" Hence EGFR status plays a major role in determining a tumor's in vivo response to radiation combined with TKI, supporting a "personalized" approach to GBM management."( Epidermal growth factor receptor expression modulates antitumor efficacy of vandetanib or cediranib combined with radiotherapy in human glioblastoma xenografts.
Daroczi, B; Dicker, AP; Lawrence, YR; Liu, Y; Wachsberger, PR; Xu, X, 2012
)
0.38
"To further explore the mechanism underlying the interaction between repaglinide and gemfibrozil, alone or in combination with itraconazole."( Repaglinide-gemfibrozil drug interaction: inhibition of repaglinide glucuronidation as a potential additional contributing mechanism.
Chen, W; Gan, J; Gao, L; Hong, Y; Humphreys, WG; Li, W; Rodrigues, AD; Shen, H; Tang, Y; Tian, Y; Zhang, H; Zhang, Y, 2010
)
0.36
"to investigate the antitumor effects on ovarian cancer using recombinant adenoviruses expressing autocatalytic caspase-3 driven by amplified human telomerase reverse transcriptase promoter (AdHTVP2G5-rev-casp3) combined with flavopiridol."( [Synergism of antitumor effects on ovarian carcinoma using autocatalytic caspase-3 combined with flavopiridol].
Shen, K; Song, Y; Xu, F, 2010
)
0.36
"following the treatment with AdHTVP2G5-rev-casp3 combined with flavopiridol, cell survival rate was measured by cell counting kit 8; cell apoptotic rate and cell cycle distribution were detected by flow cytometry."( [Synergism of antitumor effects on ovarian carcinoma using autocatalytic caspase-3 combined with flavopiridol].
Shen, K; Song, Y; Xu, F, 2010
)
0.36
" The levels of serum ALT and AST were not significantly elevated and no obvious lesions were found in any organs in treatments with AdHTVP2G5-rev-casp3 of low doses combined with flavopiridol."( [Synergism of antitumor effects on ovarian carcinoma using autocatalytic caspase-3 combined with flavopiridol].
Shen, K; Song, Y; Xu, F, 2010
)
0.36
"Vandetanib at doses of 100 mg and 300 mg daily in combination with capecitabine and oxaliplatin was well tolerated."( A phase I trial of vandetanib combined with capecitabine, oxaliplatin and bevacizumab for the first-line treatment of metastatic colorectal cancer.
Cabebe, EC; Fisher, GA; Sikic, BI, 2012
)
0.38
"Exposure to vandetanib, as assessed by AUC(504) in healthy subjects, was reduced by around 40% when a single dose was given in combination with the potent CYP3A4 inducer rifampicin."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
0.37
"Low-flow sevoflurane anesthesia combined with remifentanil regimen in patients undergoing tympanoplasty surgery resulted in a faster early recovery and decreased sevoflurane consumption."( Evaluation of recovery and anesthetic gas consumption using remifentanil combined with low-flow sevoflurane anesthesia in tympanoplasty.
Demircioglu, Rİ; Gozdemir, M; Kınacı, S; Kurtaran, H; Muslu, B; Sert, H; Usta, B, 2011
)
0.37
"We gave general anesthesia to a patient with scoliosis combined with central core disease (CCD)."( [Anesthetic management for a patient with scoliosis combined with central core disease].
Ishikawa, K; Nagata, H; Ookawa, H; Suzuki, T; Tamura, Y; Yamada, N, 2011
)
0.37
"In Japanese patients with active RA with an inadequate response to MTX, tofacitinib in combination with MTX over 12 weeks was efficacious and had a manageable safety profile."( Phase II study of tofacitinib (CP-690,550) combined with methotrexate in patients with rheumatoid arthritis and an inadequate response to methotrexate.
Nakamura, H; Suzuki, M; Tanaka, Y; Toyoizumi, S; Zwillich, SH, 2011
)
0.37
"We have investigated in vitro effects of anticancer therapy with the histone deacetylase inhibitor (HDACi) 4-phenylbutyrate (4-PB) combined with receptor tyrosine kinase inhibitors (RTKi) gefitinib or vandetanib on the survival of glioblastoma (U343MGa) and medulloblastoma (D324Med) cells."( Enhanced effects by 4-phenylbutyrate in combination with RTK inhibitors on proliferation in brain tumor cell models.
Baryawno, N; Ekström, TJ; Johnsen, JI; Larsson, C; Marino, AM; Sofiadis, A; Vukojević, V, 2011
)
0.37
"The aim of this research is to determine efficacy and safety of repaglinide alone and in combination with metformin in Chinese subjects with type 2 diabetes naive to oral antidiabetes therapy."( Randomized study of repaglinide alone and in combination with metformin in Chinese subjects with type 2 diabetes naive to oral antidiabetes therapy.
Bu, R; Liu, J; Ning, G; Su, Q; Wang, W, 2011
)
0.37
" The primary objective of this open-label phase I trial was to determine the maximum tolerated dose (MTD) and recommended dose (RD) of vandetanib in combination with gemcitabine in patients with unresectable, locally advanced or metastatic pancreatic adenocarcinoma (PAC)."( Phase I dose-finding study of vandetanib in combination with gemcitabine in locally advanced unresectable or metastatic pancreatic adenocarcinoma.
Cerny, T; De Dosso, S; Koeberle, D; Renggli, V; Saletti, P; Sessa, C, 2011
)
0.37
"Vandetanib 100 mg/day is the RD in combination with gemcitabine in the treatment of patients with advanced PAC."( Phase I dose-finding study of vandetanib in combination with gemcitabine in locally advanced unresectable or metastatic pancreatic adenocarcinoma.
Cerny, T; De Dosso, S; Koeberle, D; Renggli, V; Saletti, P; Sessa, C, 2011
)
0.37
"To observe the effects of remifentanil combined with naloxone on human sperm motility in vitro and to investigate its possible mechanism."( [Effects of remifentanil combined with naloxone on human sperm motility].
Hu, YP; Li, Q; Wang, XH; Wang, YJ; Wang, ZP; Xu, B, 2011
)
0.37
" Anesthesia was maintained with either propofol or etomidate combined with remifentanil."( Comparison of the effects of etomidate and propofol combined with remifentanil and guided by comparable BIS on transcranial electrical motor-evoked potentials during spinal surgery.
Cheng, H; Han, RQ; Liu, HY; Qiao, H; Wang, MR; Zeng, HY, 2012
)
0.38
"46) ng·mL-1 when used in combination with midazolam and topical lidocaine."( The optimal effect site concentration of remifentanil in combination with intravenous midazolam and topical lidocaine for awake fibreoptic nasotracheal intubation in patients undergoing cervical spine surgery.
Chang, CH; Kim, HS; Kwak, YL; Lee, JW; Shim, YH; Song, JW, 2012
)
0.38
"The aim of the study was to assess the efficacy and tolerability of alogliptin combined with pioglitazone in metformin-treated type 2 diabetic patients."( Efficacy and tolerability of the DPP-4 inhibitor alogliptin combined with pioglitazone, in metformin-treated patients with type 2 diabetes.
Burant, CF; DeFronzo, RA; Fleck, P; Mekki, Q; Pratley, RE; Wilson, C, 2012
)
0.38
"5 or 25 mg qd) alone or combined with pioglitazone (15, 30, or 45 mg qd) in 1554 patients on stable-dose metformin monotherapy (≥1500 mg) with inadequate glycemic control."( Efficacy and tolerability of the DPP-4 inhibitor alogliptin combined with pioglitazone, in metformin-treated patients with type 2 diabetes.
Burant, CF; DeFronzo, RA; Fleck, P; Mekki, Q; Pratley, RE; Wilson, C, 2012
)
0.38
"Compared with the donepezil treatment in the patients with mild-to-moderate AD, our results suggest that donepezil combined with natural hirudin may improve the treatment effects in the ADL, BPSD and cognition of the patients."( Donepezil combined with natural hirudin improves the clinical symptoms of patients with mild-to-moderate Alzheimer's disease: a 20-week open-label pilot study.
Li, DQ; Yang, H; Zhou, YP, 2012
)
0.38
"We aimed to observe the emergence characteristics of children tracheally extubated in deep anesthesia with sevoflurane or sevoflurane in combination with low-dose remifentanil."( Tracheal extubation of deeply anesthetized pediatric patients: a comparison of sevoflurane and sevoflurane in combination with low-dose remifentanil.
Hu, C; Li, W; Shen, X, 2012
)
0.38
"Low-dose remifentanil in combination with sevoflurane provided rapid recovery and was safe for deep tracheal extubation in deep anesthesia in pediatric patients."( Tracheal extubation of deeply anesthetized pediatric patients: a comparison of sevoflurane and sevoflurane in combination with low-dose remifentanil.
Hu, C; Li, W; Shen, X, 2012
)
0.38
" Promising preliminary antitumor activity warrants further evaluation of lonafarnib in combination with paclitaxel and trastuzumab in Her2-positive breast cancer."( Phase I study of lonafarnib (SCH66336) in combination with trastuzumab plus paclitaxel in Her2/neu overexpressing breast cancer: EORTC study 16023.
Awada, A; Beijnen, JH; Diéras, V; Govaerts, AS; Huitema, AD; Kerklaan, BM; Le Tourneau, C; Marreaud, S; Mergui-Roelvink, M; Milojkovic Kerklaan, B; Piccart-Gebhart, MJ; Rosing, H; Schellens, JH, 2013
)
0.39
"To evaluate the cost effectiveness of genetic screening for the apolipoprotein (APOE) ε4 allele in combination with preventive donepezil treatment in comparison with the standard of care for amnestic mild cognitive impairment (AMCI) patients in Canada."( Genetic testing in combination with preventive donepezil treatment for patients with amnestic mild cognitive impairment: an exploratory economic evaluation of personalized medicine.
Beca, J; Black, S; Djalalov, S; Hoch, JS; Moretti, M; Musa, Z; Saposnik, G; Siminovitch, K; Yong, J, 2012
)
0.38
"Using presently available clinical evidence, this exploratory study illustrates that genetic testing combined with preventive donepezil treatment for AMCI patients may be economically attractive."( Genetic testing in combination with preventive donepezil treatment for patients with amnestic mild cognitive impairment: an exploratory economic evaluation of personalized medicine.
Beca, J; Black, S; Djalalov, S; Hoch, JS; Moretti, M; Musa, Z; Saposnik, G; Siminovitch, K; Yong, J, 2012
)
0.38
"Quantitative prediction of complex drug-drug interactions (DDIs) is challenging."( Mechanistic modeling to predict the transporter- and enzyme-mediated drug-drug interactions of repaglinide.
El-Kattan, AF; Goosen, TC; Kimoto, E; Kumar, V; Lai, Y; Varma, MV, 2013
)
0.39
" We designed this study to investigate whether epidural anaesthesia with a goal-directed approach, when combined with general anaesthesia, improved haemodynamic stability in elderly patients undergoing major abdominal surgery."( Epidural anaesthesia with goal-directed administration of ropivacaine improves haemodynamic stability when combined with general anaesthesia in elderly patients undergoing major abdominal surgery.
Xiao, WP; Yun, X; Zhou, QH, 2013
)
0.39
" (Amaranthaceae) root alone and in combination with piperine in treating ulcerative colitis (UC) in mice."( Amaranthus roxburghianus root extract in combination with piperine as a potential treatment of ulcerative colitis in mice.
Bhawar, SB; Ingale, JM; Nirmal, SA; Pattan, SR, 2013
)
0.39
" In conclusion, p38 MAPK phosphorylation may be a prognostic marker for high-grade glioma patients, and vandetanib combined with a p38 MAPK inhibitor may be useful combination chemotherapy for glioma patients."( Vandetanib combined with a p38 MAPK inhibitor synergistically reduces glioblastoma cell survival.
Alafuzoff, I; Bergqvist, M; Blomquist, E; Edqvist, PH; Ekman, S; Gullbo, J; Jaiswal, A; Johansson, F; Lennartsson, J; Navani, S; Pontén, F; Popova, S; Sooman, L; Tsakonas, G, 2013
)
0.39
"The aim of this study was to investigate and evaluate the safety, recovery time, and side effects of general anesthesia with different doses of etomidate emulsion combined with remifentanil."( Clinical study of etomidate emulsion combined with remifentanil in general anesthesia.
Huang, M; Jiang, R; Weng, D; Yang, C; Zhan, R, 2013
)
0.39
"Continuous infusion of etomidate emulsion at 10 μg · kg(-1) · minute(-1) combined with remifentanil during anesthesia has the advantages of hemodynamic stability, quick wake-up, and few adverse reactions."( Clinical study of etomidate emulsion combined with remifentanil in general anesthesia.
Huang, M; Jiang, R; Weng, D; Yang, C; Zhan, R, 2013
)
0.39
"To evaluate the efficacy and safety of tofacitinib in combination with nonbiologic DMARDs."( Tofacitinib in combination with nonbiologic disease-modifying antirheumatic drugs in patients with active rheumatoid arthritis: a randomized trial.
Bradley, J; Fleischmann, R; Genovese, M; Gruben, D; Hall, S; Isaacs, JD; Koncz, T; Kremer, J; Krishnaswami, S; Li, ZG; Martin-Mola, E; Riese, R; Wallenstein, G; Zwillich, SH, 2013
)
0.39
"Given increased knowledge from molecular biology and pharmacology, it is apparent that multiple factors can interact to produce clinically meaningful differences in a drug's effect in specific individuals (i."( Complexities of personalized medicine: how genes, drug-drug interactions, dosing schedules, and other factors can combine to produce clinically meaningful differences in a drug's effect.
Preskorn, SH, 2013
)
0.39
" In this study we addressed the potential of NAD(+) depletion as an anti-cancer strategy and assessed the combination with radiation."( NAD⁺ depletion by APO866 in combination with radiation in a prostate cancer model, results from an in vitro and in vivo study.
Floot, B; van Triest, B; Vens, C; Verheij, M; Zerp, SF, 2014
)
0.4
" Thus, changes in CB1r function - alone and in combination with cocaine - affected stereotyped vigilance-related behaviors in this NHP, further implicating the eCB system in the neurobiological mechanisms of cocaine addiction."( Cannabinoid type-1 receptor ligands, alone or in combination with cocaine, affect vigilance-related behaviors of marmoset monkeys.
Barros, M; Cagni, P; de Jesus, AG; Melo, GC, 2014
)
0.4
"To investigate the effect of OATP1B1 genotype as a covariate on repaglinide pharmacokinetics and drug-drug interaction (DDIs) risk using a reduced physiologically-based pharmacokinetic (PBPK) model."( Reduced physiologically-based pharmacokinetic model of repaglinide: impact of OATP1B1 and CYP2C8 genotype and source of in vitro data on the prediction of drug-drug interaction risk.
Galetin, A; Gertz, M; Houston, JB; Säll, C; Tsamandouras, N, 2014
)
0.4
"A new method orthogonal projection to latent structures (O-PLS) combined with artificial neural networks is investigated for non-destructive determination of ebastine powder via near-infrared (NIR) spectroscopy."( Orthogonal projection to latent structures combined with artificial neural networks in non-destructive analysis of ebastine powder.
Ibrahim, FA; Wahba, ME, 2014
)
0.4
" remifentanil in combination with an inhaled anesthetic to facilitate tracheal extubation of deeply anesthetized adults after otologic surgery are investigated."( Sevoflurane in combination with remifentanil for tracheal extubation after otologic surgery.
Hu, C; Shen, X; Ye, M; Yu, H, 2014
)
0.4
"Sevoflurane combined with remifentanil provided rapid recovery and appeared to be safe for deep-anesthesia tracheal extubation in adult patients after otologic surgery."( Sevoflurane in combination with remifentanil for tracheal extubation after otologic surgery.
Hu, C; Shen, X; Ye, M; Yu, H, 2014
)
0.4
"To explore the clinical anesthesia value of transcutaneous acupoint electrical stimulation (TAES) combined with general intravenous anesthesia in endoscopic bilateral thyroidectomy patients."( [The anesthesiologic value of transcutaneous acupoint electrical stimulation combined with general intravenous anesthesia in endoscopic thyroidectomy patients: a clinical study].
Li, YL; Wang, MX; Wu, XY; Yan, YN, 2014
)
0.4
"High EGFR gene copy number or activating EGFR mutations may identify patient subgroups who receive increased clinical benefit from vandetanib in combination with docetaxel in second-line NSCLC."( EGFR biomarkers predict benefit from vandetanib in combination with docetaxel in a randomized phase III study of second-line treatment of patients with advanced non-small cell lung cancer.
Herbst, RS; Heymach, JV; Johnson, BE; Lockwood, SJ; Ryan, AJ, 2014
)
0.4
"To explore the feasibility and safety of dexmedetomidine combined with remifentanil for lower eyelid blepharoplasty."( [Efficacy of dexmedetomidine combined with remifentanil for lower eyelid blepharoplasty].
Chen, H; Li, X; Wu, M, 2014
)
0.4
" Local anesthesia by lidocaine (1%) combined with midazolam (0."( [Efficacy of dexmedetomidine combined with remifentanil for lower eyelid blepharoplasty].
Chen, H; Li, X; Wu, M, 2014
)
0.4
"Dexmedetomidine combined with remifentanil is practical and safe."( [Efficacy of dexmedetomidine combined with remifentanil for lower eyelid blepharoplasty].
Chen, H; Li, X; Wu, M, 2014
)
0.4
" Each dog went through all three anaesthetic protocols, which were propofol alone (group P) and propofol combined with dexmedetomidine (3 µg/kg/h, group PD) or remifentanil (18 µg/kg/h, group PR)."( [Evaluation of heart rate variability for monitoring the depth of anaesthesia in dogs. Investigations based on total intravenous anaesthesia using propofol alone or in combination with dexmedetomidine or remifentanil].
Bergfeld, C; Beyerbach, M; Kästner, SB; Voigt, AM, 2015
)
0.42
" We aimed to compare mortality and cardiovascular risk among users of metformin in combination with pharmacologically different ISs."( Metformin in combination with various insulin secretagogues in type 2 diabetes and associated risk of cardiovascular morbidity and mortality--a retrospective nationwide study.
Andersson, C; Fosbøl, EL; Gislason, G; Køber, L; Mogensen, UM; Scheller, NM; Schramm, TK; Torp-Pedersen, C; Vaag, A, 2015
)
0.42
"Most ISs in combination with metformin were associated with similar mortality and cardiovascular risk."( Metformin in combination with various insulin secretagogues in type 2 diabetes and associated risk of cardiovascular morbidity and mortality--a retrospective nationwide study.
Andersson, C; Fosbøl, EL; Gislason, G; Køber, L; Mogensen, UM; Scheller, NM; Schramm, TK; Torp-Pedersen, C; Vaag, A, 2015
)
0.42
"We compared the effect of propofol and sevoflurane combined with remifentanil under comparable bispectral index (BIS) levels on transcranial electric motor-evoked potentials (TceMEPs) and somatosensory-evoked potentials (SSEPs) during brainstem surgery."( Comparison of the Effects of Propofol and Sevoflurane Combined With Remifentanil on Transcranial Electric Motor-evoked and Somatosensory-evoked Potential Monitoring During Brainstem Surgery.
Doménech-Asensi, P; Falcón-Araña, L; Fuentes-García, D; Hernández-Palazón, J; Izura, V; Piqueras-Pérez, C, 2015
)
0.42
"Both sevoflurane and propofol at low dosages combined with remifentanil under comparable BIS values and partial muscle relaxation can be used when monitoring of TceMEPs and SSEPs is required for brainstem surgery."( Comparison of the Effects of Propofol and Sevoflurane Combined With Remifentanil on Transcranial Electric Motor-evoked and Somatosensory-evoked Potential Monitoring During Brainstem Surgery.
Doménech-Asensi, P; Falcón-Araña, L; Fuentes-García, D; Hernández-Palazón, J; Izura, V; Piqueras-Pérez, C, 2015
)
0.42
" We investigated the efficacy of the histone deacetylase (HDAC) inhibitor vorinostat combined with one of several B-cell receptor (BCR) signaling inhibitors on MCL cell death and the underlying mechanisms, using MCL cell lines."( The synergistic effect of BCR signaling inhibitors combined with an HDAC inhibitor on cell death in a mantle cell lymphoma cell line.
Hagiwara, K; Iida, H; Kunishima, S; Miyata, Y; Nagai, H; Naoe, T, 2015
)
0.42
"To evaluate the effects of a constant rate infusion of remifentanil, alone or in combination with ketamine, in healthy cats anesthetized with isoflurane."( Clinical effects of a constant rate infusion of remifentanil, alone or in combination with ketamine, in cats anesthetized with isoflurane.
Aucoin, M; Burns, PM; Monteiro, BP; Moreau, M; Simon, BT; Steagall, PV, 2015
)
0.42
" We report the first bench-to-bedside evidence that RET inhibitor combined with an mTOR inhibitor is active against brain-metastatic RET-rearranged lung cancer and the first evidence of blood-brain barrier penetration."( Systemic and CNS activity of the RET inhibitor vandetanib combined with the mTOR inhibitor everolimus in KIF5B-RET re-arranged non-small cell lung cancer with brain metastases.
Ali, SM; Berry, J; Cascone, T; Guha-Thakurta, N; Heymach, JV; McMahon, C; Miller, V; Pai, S; Roxas, M; Subbiah, IM; Subbiah, V; Tang, Z, 2015
)
0.42
" Therefore, the present study tested whether full FAAH inhibition combined with partial MAGL inhibition would produce sustained antinociceptive effects with minimal cannabimimetic side effects."( Full Fatty Acid Amide Hydrolase Inhibition Combined with Partial Monoacylglycerol Lipase Inhibition: Augmented and Sustained Antinociceptive Effects with Reduced Cannabimimetic Side Effects in Mice.
Abdullah, RA; Cravatt, BF; Ghosh, S; Grim, TW; Hruba, L; Kinsey, SG; Lichtman, AH; Liu, QS; McMahon, LR; Merritt, CR; Selley, DE; Sim-Selley, LJ; Wise, LE, 2015
)
0.42
" We here compare bortezomib with carfilzomib and LU-102 in MM and MCL in vitro with regard to their effects on pIκB/NF-κB signaling and their cytotoxic activity in combination with ibrutinib."( The novel β2-selective proteasome inhibitor LU-102 decreases phosphorylation of I kappa B and induces highly synergistic cytotoxicity in combination with ibrutinib in multiple myeloma cells.
Bader, J; Besse, L; de Bruin, G; Driessen, C; Geurink, PP; Kisselev, AF; Kraus, J; Kraus, M; Liu, N; Overkleeft, H, 2015
)
0.42
" Anti-CD20 antibodies have improved response and progression-free survival (PFS) when combined with chemotherapy."( Safety and activity of BTK inhibitor ibrutinib combined with ofatumumab in chronic lymphocytic leukemia: a phase 1b/2 study.
Andritsos, LA; Blum, KA; Byrd, JC; Flynn, JM; Grever, MR; Hall, N; Heerema, NA; Jaglowski, SM; James, DF; Johnson, AJ; Jones, JA; Lozanski, G; Maddocks, KJ; Munneke, B; Nagar, V; Neuenburg, JK; Ruppert, AS; Smucker, K; Stefanos, M; West, JS; Woyach, JA, 2015
)
0.42
" The present study examined the synergistic effect of low doses of FA combined with subthreshold dose of piperine, a bioavailability enhancer, on depression-like behaviors in mice, and investigated the possible mechanism."( Synergistic antidepressant-like effect of ferulic acid in combination with piperine: involvement of monoaminergic system.
Chen, J; Chen, L; Chen, R; Huang, W; Li, G; Pan, J; Reed, M; Ruan, L; Wang, R; Xie, X; Xu, Y; Yan, Q; Zhang, M, 2015
)
0.42
" Although curcumin caused already significant effects, the combination with piperine completely suppressed the osteoclastogenesis by decreasing the TRAP activity and inhibiting the expression of the specific osteoclast markers TRAP, cathepsin K, and calcitonin receptor."( Curcumin in Combination with Piperine Suppresses Osteoclastogenesis In Vitro.
Geurtsen, W; Leyhausen, G; Martins, CA; Volk, J, 2015
)
0.42
"We demonstrated that curcumin combined with piperine suppressed the osteoclastogenesis in vitro without causing cytotoxic effects in periodontal ligament cells."( Curcumin in Combination with Piperine Suppresses Osteoclastogenesis In Vitro.
Geurtsen, W; Leyhausen, G; Martins, CA; Volk, J, 2015
)
0.42
"The objective of this study was to evaluate the hemodynamic effects of target-controlled infusion (TCI) of propofol alone or in combination with a constant-rate infusion (CRI) of remifentanil."( Hemodynamic effects of target-controlled infusion of propofol alone or in combination with a constant-rate infusion of remifentanil in dogs.
Aguiar, AJ; Beier, SL; Massone, F; Mattoso, CR; Vianna, PT, 2015
)
0.42
" In other words, the tissue distribution of drugs can be influenced by drug-drug interaction (DDI) at efflux transporters in certain tissues (local DDI) without any apparent change in plasma concentration (systemic DDI)."( Local Drug-Drug Interaction of Donepezil with Cilostazol at Breast Cancer Resistance Protein (ABCG2) Increases Drug Accumulation in Heart.
Nakanishi, T; Shinozaki, K; Takeuchi, R; Tamai, I, 2016
)
0.43
"Ibrutinib combined with rituximab is active and well tolerated in patients with relapsed or refractory mantle cell lymphoma."( Ibrutinib in combination with rituximab in relapsed or refractory mantle cell lymphoma: a single-centre, open-label, phase 2 trial.
Addison, A; Badillo, M; Champlin, R; Chen, W; Chuang, H; DeLa Rosa, M; Fayad, L; Hagemeister, F; Lam, L; Lee, H; Li, S; Medeiros, LJ; Nomie, K; Oki, Y; Romaguera, J; Samaniego, F; Santos, D; Turturro, F; Wagner-Bartak, N; Wang, ML; Westin, J; Young, KH; Zhang, H; Zhang, L; Zhao, D, 2016
)
0.43
"Between Sept 19, 2012, and Jan 21, 2014, 578 eligible patients were randomly assigned to ibrutinib or placebo in combination with bendamustine plus rituximab (289 in each group)."( Ibrutinib combined with bendamustine and rituximab compared with placebo, bendamustine, and rituximab for previously treated chronic lymphocytic leukaemia or small lymphocytic lymphoma (HELIOS): a randomised, double-blind, phase 3 study.
Avigdor, A; Balasubramanian, S; Bartlett, NL; Chanan-Khan, A; Cramer, P; Demirkan, F; Dilhuydy, MS; Fraser, G; Goy, A; Grosicki, S; Hallek, M; Howes, A; Janssens, A; Karlsson, C; Loscertales, J; Mahler, M; Mato, A; Mayer, J; Panagiotidis, P; Pavlovsky, MA; Phelps, C; Pristupa, A; Pylypenko, H; Rule, S; Salman, M; Samoilova, O; Silva, RS; Sun, S; Villa, D, 2016
)
0.43
" This phase I study evaluated the safety profile of vandetanib in combination with standard doses of gemcitabine and capecitabine in order to determine the maximum tolerated dose (MTD)."( Phase I trial of vandetanib in combination with gemcitabine and capecitabine in patients with advanced solid tumors with an expanded cohort in pancreatic and biliary cancers.
Bradshaw-Pierce, EL; Eckhardt, SG; Eppers, S; Freas, E; Kane, MA; Kessler, ER; Leong, S; Lieu, CH; Messersmith, WA; Nallapreddy, S; O'byrant, CL; Pitts, TM; Spratlin, J; Weekes, C, 2016
)
0.43
" To create a safer clozapine-like drug, we tested whether the antipsychotic iloperidone, a drug that combines a weak dopamine D2 receptor blockade and a potent norepinephrine alpha-2 receptor blockade would reduce alcohol drinking, and whether its effect on alcohol drinking could be increased if combined with an agent to facilitate norepinephrine activity."( Effects of iloperidone, combined with desipramine, on alcohol drinking in the Syrian golden hamster.
Green, AI; Khokhar, JY, 2016
)
0.43
" Tofacitinib can be administered as a monotherapy or in combination with conventional synthetic disease-modifying antirheumatic drugs (DMARDs)."( Initial Experience With Tofacitinib in Clinical Practice: Treatment Patterns and Costs of Tofacitinib Administered as Monotherapy or in Combination With Conventional Synthetic DMARDs in 2 US Health Care Claims Databases.
Curtis, JR; Gerber, R; Gruben, D; Harnett, J; Koenig, A, 2016
)
0.43
" A clinical drug-drug interaction (DDI) study with the potent CYP3A4 inhibitor itraconazole resulted in an approximately sevenfold increase in cobimetinib exposure."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
" To alleviate the pill burden and swallowing difficulties associated with the condition, a fixed drug combination of extended-release memantine and donepezil was developed."( Memantine and donepezil: a fixed drug combination for the treatment of moderate to severe Alzheimer's dementia.
Owen, RT, 2016
)
0.43
" Nevertheless, the effect of such drug combination usage on the in vivo exposure of PIP has not been investigated due to lack of assay for the simultaneous determination of PIP and other drugs such as DOX."( Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats.
Chow, MSS; Lam, CWK; Li, C; Ren, T; Wang, Q; Zhang, Y; Zuo, Z, 2016
)
0.43
"In this double-blind, randomised, placebo-controlled, multicentre study, adult patients (aged ≥18 years) with histologically confirmed BRAF(V600) mutation-positive unresectable stage IIIC or stage IV melanoma were randomly assigned (1:1) using an interactive response system to receive cobimetinib (60 mg once daily for 21 days followed by a 7-day rest period in each 28-day cycle) or placebo, in combination with oral vemurafenib (960 mg twice daily)."( Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial.
Ascierto, PA; Atkinson, V; Chang, I; de la Cruz-Merino, L; Demidov, L; Di Giacomo, AM; Dréno, B; Dutriaux, C; Garbe, C; Hsu, JJ; Koralek, DO; Larkin, J; Liszkay, G; Mandalà, M; McArthur, GA; Ribas, A; Rooney, I; Stroyakovskiy, D; Thomas, L; Wongchenko, M; Yan, Y, 2016
)
0.43
"These data confirm the clinical benefit of cobimetinib combined with vemurafenib and support the use of the combination as a standard first-line approach to improve survival in patients with advanced BRAF(V600)-mutant melanoma."( Cobimetinib combined with vemurafenib in advanced BRAF(V600)-mutant melanoma (coBRIM): updated efficacy results from a randomised, double-blind, phase 3 trial.
Ascierto, PA; Atkinson, V; Chang, I; de la Cruz-Merino, L; Demidov, L; Di Giacomo, AM; Dréno, B; Dutriaux, C; Garbe, C; Hsu, JJ; Koralek, DO; Larkin, J; Liszkay, G; Mandalà, M; McArthur, GA; Ribas, A; Rooney, I; Stroyakovskiy, D; Thomas, L; Wongchenko, M; Yan, Y, 2016
)
0.43
" Here, we report in vivo data for OTX015 in combination with the histone deacetylase inhibitor vorinostat, the Bruton's tyrosine kinase inhibitor ibrutinib, the anti-CD20 monoclonal antibody rituximab, and the mTOR inhibitor everolimus in a diffuse large B cell lymphoma model."( Bromodomain inhibitor OTX015 (MK-8628) combined with targeted agents shows strong in vivo antitumor activity in lymphoma.
Bernasconi, E; Bertoni, F; Cascione, L; Cvitkovic, E; Gaudio, E; Odore, E; Ponzoni, M; Rezai, K; Rinaldi, A; Riveiro, E; Stathis, A; Tarantelli, C; Zucca, E, 2016
)
0.43
"The study showed that intraoperative glucose infusion suppressed lipolysis and proteolysis in patients anesthetized with remifentanil in combination with sevoflurane during surgery of >6 hours in length."( Effect of Intraoperative Glucose Infusion on Catabolism of Adipose Tissue and Muscle Protein in Patients Anesthetized With Remifentanil in Combination With Sevoflurane During Major Surgery: A Randomized Controlled Multicenter Trial.
Hayashi, H; Ichinose, H; Kamada, Y; Sawada, A; Sumita, S; Yamakage, M, 2016
)
0.43
" We present results from 3 fixed-sequence studies evaluating drug-drug interactions for alectinib through CYP3A."( Clinical Drug-Drug Interactions Through Cytochrome P450 3A (CYP3A) for the Selective ALK Inhibitor Alectinib.
Bogman, K; Bordogna, W; Cleary, Y; Dall, G; De Petris, L; Guerini, E; Martin-Facklam, M; Morcos, PN; Phipps, A; Viteri, S; Yu, L, 2017
)
0.46
" We compared patient-reported outcomes (PROs) in patients with RA treated with tofacitinib or placebo in combination with conventional disease-modifying antirheumatic drugs (DMARDs)."( Tofacitinib in Combination With Conventional Disease-Modifying Antirheumatic Drugs in Patients With Active Rheumatoid Arthritis: Patient-Reported Outcomes From a Phase III Randomized Controlled Trial.
Gruben, D; Kremer, JM; Krishnaswami, S; Strand, V; Wallenstein, GV; Zwillich, SH, 2017
)
0.46
"In a 12-month, phase III randomized controlled trial (ORAL Sync), patients (n = 795) with active RA and previous inadequate response to therapy with ≥1 conventional or biologic DMARD were randomized 4:4:1:1 to tofacitinib 5 mg twice daily (BID), tofacitinib 10 mg BID, placebo advanced to 5 mg BID, or placebo to 10 mg BID, in combination with stable background DMARD therapy."( Tofacitinib in Combination With Conventional Disease-Modifying Antirheumatic Drugs in Patients With Active Rheumatoid Arthritis: Patient-Reported Outcomes From a Phase III Randomized Controlled Trial.
Gruben, D; Kremer, JM; Krishnaswami, S; Strand, V; Wallenstein, GV; Zwillich, SH, 2017
)
0.46
"Patients with active RA treated with tofacitinib combined with background conventional DMARD therapy reported sustained, significant, and clinically meaningful improvements in PROs versus placebo."( Tofacitinib in Combination With Conventional Disease-Modifying Antirheumatic Drugs in Patients With Active Rheumatoid Arthritis: Patient-Reported Outcomes From a Phase III Randomized Controlled Trial.
Gruben, D; Kremer, JM; Krishnaswami, S; Strand, V; Wallenstein, GV; Zwillich, SH, 2017
)
0.46
" Curcumin (CMN) in combination with bioenhancer piperine (PP) in 6-hydroxydopamine-induced Parkinsonian rats was used to investigate the antioxidant, neuromodulatory and neuroprotective mechanisms."( Neuroprotective potential of curcumin in combination with piperine against 6-hydroxy dopamine induced motor deficit and neurochemical alterations in rats.
Kumar, P; Singh, S, 2017
)
0.46
" Ublituximab in combination with ibrutinib resulted in rapid and high response rates."( Ublituximab (TG-1101), a novel glycoengineered anti-CD20 antibody, in combination with ibrutinib is safe and highly active in patients with relapsed and/or refractory chronic lymphocytic leukaemia: results of a phase 2 trial.
Brooks, HD; Burke, JM; Fanning, S; Farber, CM; Greenwald, DR; Klein, L; Kolibaba, KS; Mahadevan, D; Miskin, HP; Schreeder, MT; Sharman, JP; Sportelli, P; Weiss, MS, 2017
)
0.46
" We aimed to systematically screen for drugs that interact with the five most commonly used secretagogues-glipizide, glyburide, glimepiride, repaglinide, and nateglinide-to cause serious hypoglycemia."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
" We first predicted the drug-drug interaction potential based on the pharmacokinetics of each secretagogue-precipitant pair."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
"We predicted 34 pharmacokinetic drug-drug interactions with the secretagogues, nine moderate and 25 weak."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
"The self-controlled case series design has the potential to be widely applicable to screening for drug-drug interactions that lead to adverse outcomes identifiable in healthcare databases."( Biomedical Informatics Approaches to Identifying Drug-Drug Interactions: Application to Insulin Secretagogues.
Bilker, WB; Brensinger, CM; Chiang, C; Han, X; Hennessy, S; Leonard, CE; Li, L, 2017
)
0.46
" In the drug combination studies, intrathecal coadministration of BRL52537 with pregabalin or A804598 exhibited synergistic interactions, and other drugs combinations showed additivity."( Isobolographic Analysis of Drug Combinations With Intrathecal BRL52537 (κ-Opioid Agonist), Pregabalin (Calcium Channel Modulator), AF 353 (P2X3 Receptor Antagonist), and A804598 (P2X7 Receptor Antagonist) in Neuropathic Rats.
Han, JH; Jung, YH; Kim, YC; Kim, YO; Yoon, MH, 2017
)
0.46
" The aim of the study was to evaluate whether dipeptidyl peptidase-4 (DPP-4) inhibitor alogliptin (ALO) alone or in combination with pioglitazone (PIO) improves β-cell function along with insulin resistance (IR) in metformin (MET) treated obese women with PCOS with persistent IR."( Add on DPP-4 inhibitor alogliptin alone or in combination with pioglitazone improved β-cell function and insulin sensitivity in metformin treated PCOS.
Goricar, K; Janez, A; Jensterle, M, 2017
)
0.46
"ALO alone and in combination with PIO improved IR along with dynamic IS and meal related β-cell function when added to MET treated PCOS."( Add on DPP-4 inhibitor alogliptin alone or in combination with pioglitazone improved β-cell function and insulin sensitivity in metformin treated PCOS.
Goricar, K; Janez, A; Jensterle, M, 2017
)
0.46
"Of 495 patients recruited to the study, 493 patients received treatment and constituted the safety population (cobimetinib combined with vemurafenib, 247; vemurafenib, 246)."( Incidence, course, and management of toxicities associated with cobimetinib in combination with vemurafenib in the coBRIM study.
Ascierto, PA; Dréno, B; Grob, JJ; Hauschild, A; Hsu, JJ; Koralek, DO; Larkin, J; McArthur, GA; McKenna, EF; Ribas, A; Rooney, I; Thomas, L, 2017
)
0.46
"These data indicate that most AEs arising from treatment with cobimetinib combined with vemurafenib generally occur early in the treatment course, are mild or moderate and are manageable by patient monitoring, dose modification and supportive care."( Incidence, course, and management of toxicities associated with cobimetinib in combination with vemurafenib in the coBRIM study.
Ascierto, PA; Dréno, B; Grob, JJ; Hauschild, A; Hsu, JJ; Koralek, DO; Larkin, J; McArthur, GA; McKenna, EF; Ribas, A; Rooney, I; Thomas, L, 2017
)
0.46
"Quantitative analysis of transporter- and enzyme-mediated complex drug-drug interactions (DDIs) is challenging."( Quantitative Analysis of Complex Drug-Drug Interactions Between Repaglinide and Cyclosporin A/Gemfibrozil Using Physiologically Based Pharmacokinetic Models With In Vitro Transporter/Enzyme Inhibition Data.
Kim, SJ; Sugiyama, Y; Toshimoto, K; Yao, Y; Yoshikado, T, 2017
)
0.46
"A total of 334 participants with Alzheimer's disease will be randomly assigned to either an electroacupuncture combined with donepezil group or a donepezil group with a ratio of 1:1."( The effect of electroacupuncture combined with donepezil on cognitive function in Alzheimer's disease patients: study protocol for a randomized controlled trial.
Bin, L; Feng, Q; Liu, Z; Peng, W; Xu, M; Zhou, J, 2017
)
0.46
"This study aims to describe the administration of propofol in combination with remifentanil for the induction of general anesthesia during cesarean section (CS)."( Propofol in combination with remifentanil for cesarean section: Placental transfer and effect on mothers and newborns at different induction to delivery intervals.
He, K; Hu, L; Pan, J; Shu, S; Wang, R; Yu, J; Zhang, S, 2017
)
0.46
"It is safe to administer propofol in combination with remifentanil by continuous infusion after the bolus dose for the induction of anesthesia during cesarean section."( Propofol in combination with remifentanil for cesarean section: Placental transfer and effect on mothers and newborns at different induction to delivery intervals.
He, K; Hu, L; Pan, J; Shu, S; Wang, R; Yu, J; Zhang, S, 2017
)
0.46
" Quercetin (QC) in combination with piperine (bioenhancer) acts as potential antioxidant, anti-inflammatory and neuroprotective against 6-OHDA rat model of PD."( Piperine in combination with quercetin halt 6-OHDA induced neurodegeneration in experimental rats: Biochemical and neurochemical evidences.
Kumar, P; Singh, S, 2018
)
0.48
" Alectinib and its major active metabolite M4 exhibited drug-drug interaction (DDI) potential through cytochrome P450 (CYP) enzymes CYP3A4 and CYP2C8 in vitro."( Model-Based Assessments of CYP-Mediated Drug-Drug Interaction Risk of Alectinib: Physiologically Based Pharmacokinetic Modeling Supported Clinical Development.
Cleary, Y; Fowler, S; Gertz, M; Morcos, PN; Parrott, N; Phipps, A; Youdim, K; Yu, L, 2018
)
0.48
" We investigate, as an example, the impact of CYP3A4-CYP2C8 intercorrelation on the predicted interindividual variabilities of clearance and drug-drug interactions (DDIs) for repaglinide using physiologically based pharmacokinetic (PBPK) modelling."( Implications of intercorrelation between hepatic CYP3A4-CYP2C8 enzymes for the evaluation of drug-drug interactions: a case study with repaglinide.
Achour, B; Backman, JT; Darwich, AS; Doki, K; Rostami-Hodjegan, A; Tornio, A, 2018
)
0.48
" We conducted a single-center phase 1 study evaluating dose-escalated ibrutinib, in a 3-by-3 design, in combination with rituximab, ifosfamide, carboplatin, and etoposide (R-ICE) in physiologically transplant-eligible rel/ref DLBCL patients."( A phase 1 study of ibrutinib in combination with R-ICE in patients with relapsed or primary refractory DLBCL.
Courtien, AI; Devlin, SM; Drullinsky, P; Gerecitano, J; Kumar, A; Matasar, MJ; McCall, SJ; Miller, ST; Moskowitz, CH; Noy, A; Palomba, ML; Portlock, CS; Sauter, CS; Schoder, H; Straus, DJ; Younes, A; Zelenetz, AD, 2018
)
0.48
" For the first time, this study was aimed to evaluate the effect of topical piperine combined with narrowband ultraviolet B (NB-UVB) on vitiligo treatment."( The effect of topical piperine combined with narrowband UVB on vitiligo treatment: A clinical trial study.
Abadi, A; Hoormand, M; Shafiee, A; Shahidi-Dadras, M, 2018
)
0.48
" We evaluated the safety, tolerability, and pharmacokinetic properties of GDC-0575 alone and in combination with gemcitabine."( Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in patients with refractory solid tumors.
Blackwood, EM; Cousin, S; DuPree, K; Epler, J; Hamilton, E; Hollebecque, A; Infante, JR; Italiano, A; Lauchle, JO; LoRusso, PM; Lu, X; Mahrus, S; Moein, A; Moore, KN; Murray, ER; Peale, FV; Postel-Vinay, S; Schutzman, JL; Shapiro, GI; Soria, JC; Tagen, M; Tolaney, S; Toulmonde, M, 2018
)
0.48
"In this phase I open-label study, in the dose escalation stage, patients were enrolled in a GDC-0575 monotherapy Arm (1) or GDC-0575 combination with gemcitabine Arm (2) to determine the maximum tolerated dose."( Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in patients with refractory solid tumors.
Blackwood, EM; Cousin, S; DuPree, K; Epler, J; Hamilton, E; Hollebecque, A; Infante, JR; Italiano, A; Lauchle, JO; LoRusso, PM; Lu, X; Mahrus, S; Moein, A; Moore, KN; Murray, ER; Peale, FV; Postel-Vinay, S; Schutzman, JL; Shapiro, GI; Soria, JC; Tagen, M; Tolaney, S; Toulmonde, M, 2018
)
0.48
" No pharmacokinetic drug-drug interaction was observed between GDC-0575 and gemcitabine."( Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in patients with refractory solid tumors.
Blackwood, EM; Cousin, S; DuPree, K; Epler, J; Hamilton, E; Hollebecque, A; Infante, JR; Italiano, A; Lauchle, JO; LoRusso, PM; Lu, X; Mahrus, S; Moein, A; Moore, KN; Murray, ER; Peale, FV; Postel-Vinay, S; Schutzman, JL; Shapiro, GI; Soria, JC; Tagen, M; Tolaney, S; Toulmonde, M, 2018
)
0.48
"GDC-0575 can be safely administered as a monotherapy and in combination with gemcitabine; however, overall tolerability with gemcitabine was modest."( Phase I study of the checkpoint kinase 1 inhibitor GDC-0575 in combination with gemcitabine in patients with refractory solid tumors.
Blackwood, EM; Cousin, S; DuPree, K; Epler, J; Hamilton, E; Hollebecque, A; Infante, JR; Italiano, A; Lauchle, JO; LoRusso, PM; Lu, X; Mahrus, S; Moein, A; Moore, KN; Murray, ER; Peale, FV; Postel-Vinay, S; Schutzman, JL; Shapiro, GI; Soria, JC; Tagen, M; Tolaney, S; Toulmonde, M, 2018
)
0.48
" JZL alone or in combination with r-tPA, but not r-tPA, reduced brain edema, infarct volume, brain levels of TNF-α, MMP9, and also improved behavioral tests."( Monoacylglycerol Lipase Inhibitor is Safe when Combined with Delayed r-tPA Administration in Treatment of Stroke.
Allahtavakoli, M; Hakimizadeh, E; Rahmani, MR; Shamsizadeh, A, 2018
)
0.48
" The results of the systematic review showed that piperine has promising anti-TB activity, mainly when combined with antimicrobials, and plays an important role as an EP inhibitor."( Promising Antituberculosis Activity of Piperine Combined with Antimicrobials: A Systematic Review.
Almeida, AL; Barros, ILE; Caleffi-Ferracioli, KR; Campanerut-Sá, PAZ; Canezin, PH; Cardoso, RF; Hegeto, LA; Nakamura de Vasconcelos, SS; Perez de Souza, J; Scodro, RBL; Siqueira, VLD; Teixeira, JJV,
)
0.13
"Pooled data from six double-blind, randomized controlled Phase 3 studies of tofacitinib 5 and 10 mg BID in patients with RA were analyzed for safety and stratified by administration as monotherapy (ORAL Solo: NCT00814307 and ORAL Start: NCT01039688) or in combination with csDMARDs (ORAL Sync: NCT00856544, ORAL Standard: NCT00853385, ORAL Scan: NCT00847613, and ORAL Step: NCT00960440), and by glucocorticoid use at baseline."( A pooled analysis of the safety of tofacitinib as monotherapy or in combination with background conventional synthetic disease-modifying antirheumatic drugs in a Phase 3 rheumatoid arthritis population.
Bananis, E; Cohen, S; Connell, CA; Fan, H; Fleischmann, R; Haraoui, B; Kaine, J; Keystone, E; Kivitz, AJ; Takiya, L; van Vollenhoven, RF, 2018
)
0.48
" Therefore, a clinical drug-drug interaction (DDI) study to evaluate the effects of evocalcet on the pharmacokinetics (PKs) of probe substrates for CYP isozymes (CYP1A2, CYP2B6, CYP2C8, CYP2C9, and CYP3A) was conducted in healthy male volunteers using a novel cocktail combination."( Assessment of CYP-Mediated Drug Interactions for Evocalcet, a New Calcimimetic Agent, Based on In Vitro Investigations and a Cocktail Study in Humans.
Akizawa, T; Endo, Y; Fukagawa, M; Kannami, A; Maeda, H; Nagata, Y; Nakamura, H; Narushima, K; Ohtsuka, S; Shimazaki, R; Shiramoto, M; Uchimura, T, 2019
)
0.51
" The recommended phase 2 dose of umbralisib when given in combination with ibrutinib was 800 mg once daily."( Umbralisib in combination with ibrutinib in patients with relapsed or refractory chronic lymphocytic leukaemia or mantle cell lymphoma: a multicentre phase 1-1b study.
Arnason, JE; Bazemore, J; Boruchov, AM; Brown, JR; Davids, MS; Fisher, DC; Francoeur, K; Hellman, JM; Jacobsen, ED; Jacobson, CA; Kim, HT; Maegawa, R; Miskin, HP; Nicotra, A; Rueter, J; Savell, A; Sportelli, P; Stampleman, L, 2019
)
0.51
" The aim of this study was to assess the safety and activity of ibrutinib in combination with nivolumab in patients with relapsed or refractory B-cell malignant diseases."( Safety and activity of ibrutinib in combination with nivolumab in patients with relapsed non-Hodgkin lymphoma or chronic lymphocytic leukaemia: a phase 1/2a study.
Alvarez, J; Avivi, I; Balasubramanian, S; Ben-Yehuda, D; Bosch, F; Brody, J; Buglio, D; Caballero Barrigón, MD; Carpio, C; Ceulemans, R; Cordoba, R; de Jong, J; Demirkan, F; Ferhanoglu, B; Fourneau, N; Hellmann, A; Hodkinson, BP; Horowitz, NA; Jurczak, W; Kuss, B; Lopez-Guillermo, A; Ma, DDF; Marlton, P; Nagler, A; Ozcan, M; Schaffer, M; Streit, M; Wang, SS; Wrobel, T; Yağci, M; Younes, A, 2019
)
0.51
" The primary objective of part A (dose escalation) was to assess the safety of daily oral ibrutinib (420 mg or 560 mg) in combination with intravenous nivolumab (3 mg/kg every 2 weeks) to ascertain a recommended phase 2 dose in patients with relapsed or refractory high-risk chronic lymphocytic leukaemia or small lymphocytic lymphoma (del17p or del11q), follicular lymphoma, or diffuse large B-cell lymphoma."( Safety and activity of ibrutinib in combination with nivolumab in patients with relapsed non-Hodgkin lymphoma or chronic lymphocytic leukaemia: a phase 1/2a study.
Alvarez, J; Avivi, I; Balasubramanian, S; Ben-Yehuda, D; Bosch, F; Brody, J; Buglio, D; Caballero Barrigón, MD; Carpio, C; Ceulemans, R; Cordoba, R; de Jong, J; Demirkan, F; Ferhanoglu, B; Fourneau, N; Hellmann, A; Hodkinson, BP; Horowitz, NA; Jurczak, W; Kuss, B; Lopez-Guillermo, A; Ma, DDF; Marlton, P; Nagler, A; Ozcan, M; Schaffer, M; Streit, M; Wang, SS; Wrobel, T; Yağci, M; Younes, A, 2019
)
0.51
" This study confirmed that the Inje cocktail approach was able to detect relevant drug-drug interactions impacting further development of ASP8477 and future therapeutic use."( A Cocktail Interaction Study Evaluating the Drug-Drug Interaction Potential of the Perpetrator Drug ASP8477 at Multiple Ascending Dose Levels.
Collins, C; Ernault, E; Fuhr, R; Gangaram-Panday, S; Passier, P; Treijtel, N; van Bruijnsvoort, M, 2019
)
0.51
"Ibrutinib alone or in combination with cytarabine or azacitidine demonstrated an acceptable safety profile."( Clinical Experience With Ibrutinib Alone or in Combination With Either Cytarabine or Azacitidine in Patients With Acute Myeloid Leukemia.
Cortes, JE; Graef, T; Jonas, BA; Luan, Y; Stein, AS, 2019
)
0.51
" The aim of this study was to characterize the metabolites of AdipoRon in rat and human liver microsomes using ultra-high performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry (UPLC-Q-Exactive-Orbitrap-MS) together with data processing techniques including extracted ion chromatograms and a mass defect filter."( Characterization of the metabolite of AdipoRon in rat and human liver microsomes by ultra-high-performance liquid chromatography combined with Q-Exactive Orbitrap tandem mass spectrometry.
Ge, Y; Li, X; Liu, Q; Yu, Y; Zhang, Y, 2019
)
0.51
" This study investigated the effect of CMG002 alone and in combination with sorafenib on HCC in vitro and vivo."( Preclinical efficacy of a novel dual PI3K/mTOR inhibitor, CMG002, alone and in combination with sorafenib in hepatocellular carcinoma.
Hwang, SG; Kim, JS; Kim, MN; Lee, SM, 2019
)
0.51
" Treatment with CMG002 for 4 weeks alone and in combination with sorafenib strongly inhibited tumor growth."( Preclinical efficacy of a novel dual PI3K/mTOR inhibitor, CMG002, alone and in combination with sorafenib in hepatocellular carcinoma.
Hwang, SG; Kim, JS; Kim, MN; Lee, SM, 2019
)
0.51
" The aim of this study was to investigate the pharmacokinetic profiles of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats."( Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.
Anukunwithaya, T; Junsaeng, D; Khemawoot, P; Likhitwitayawuid, K; Songvut, P; Sritularak, B, 2019
)
0.51
"Male Wistar rats were administered with oxyresveratrol 10 mg/kg, oxyresveratrol 10 mg/kg plus piperine 1 mg/kg via intravenous or oxyresveratrol 100 mg/kg, oxyresveratrol 100 mg/kg plus piperine 10 mg/kg via oral gavage."( Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.
Anukunwithaya, T; Junsaeng, D; Khemawoot, P; Likhitwitayawuid, K; Songvut, P; Sritularak, B, 2019
)
0.51
"The combination with piperine had shown a significantly higher maximum concentration in plasma approximately 1500 μg/L within 1-2 h after oral dosing, and could increase oral bioavailability of oxyresveratrol approximately 2-fold."( Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.
Anukunwithaya, T; Junsaeng, D; Khemawoot, P; Likhitwitayawuid, K; Songvut, P; Sritularak, B, 2019
)
0.51
" This study was carried out to investigate the effect of piperine and quercetin alone or in combination with marbofloxacin on CYP3A37 and MDR1 mRNA expression levels in liver and intestine of broiler chicken."( Effect of piperine and quercetin alone or in combination with marbofloxacin on CYP3A37 and MDR1 mRNA expression levels in broiler chickens.
Mathapati, BS; Modi, CM; Patel, HB; Patel, UD, 2019
)
0.51
" Therefore, the present study was designed to evaluate the neuroprotective effect of quercetin in combination with piperine against rotenone- and iron supplement-induced model of PD."( Neuroprotective Effect of Quercetin in Combination with Piperine Against Rotenone- and Iron Supplement-Induced Parkinson's Disease in Experimental Rats.
Raj, K; Sharma, S; Singh, S, 2020
)
0.56
"We evaluated ibrutinib, a once-daily inhibitor of Bruton's tyrosine kinase, combined with bortezomib and dexamethasone in patients with relapsed or relapsed/refractory multiple myeloma who had received 1-3 prior therapies."( A phase 2 study of ibrutinib in combination with bortezomib and dexamethasone in patients with relapsed/refractory multiple myeloma.
Anagnostopoulos, A; Briso, EM; Cascavilla, N; Dobkowska, E; García Sanz, R; Hajek, R; Hauns, B; Lee, Y; Martin Sánchez, J; Oriol, A; Ozcan, M; Pour, L; Špička, I; Terjung, A, 2020
)
0.56
"Ibrutinib combined with bortezomib and dexamethasone elicited clinical responses."( A phase 2 study of ibrutinib in combination with bortezomib and dexamethasone in patients with relapsed/refractory multiple myeloma.
Anagnostopoulos, A; Briso, EM; Cascavilla, N; Dobkowska, E; García Sanz, R; Hajek, R; Hauns, B; Lee, Y; Martin Sánchez, J; Oriol, A; Ozcan, M; Pour, L; Špička, I; Terjung, A, 2020
)
0.56
" This study assessed the in vitro and in vivo functionality of CAR T cells transduced to express the anti-CD19 CAR of liso-cel in combination with ibrutinib or acalabrutinib."( Antitumor Potency of an Anti-CD19 Chimeric Antigen Receptor T-Cell Therapy, Lisocabtagene Maraleucel in Combination With Ibrutinib or Acalabrutinib.
Baturevych, A; Clouser, CR; Hause, RJ; Johnstone, TG; Jones, JC; Krejsa, CM; Ponce, R; Ports, MO; Qin, JS; Ragan, SP; Salmon, RA, 2020
)
0.56
"Rash is one of the most common severe adverse events associated with use of vemurafenib for the treatment of melanoma, either as monotherapy or in combination with cobimetinib."( Risk factors for severe rash with use of vemurafenib alone or in combination with cobimetinib for advanced melanoma: pooled analysis of clinical trials.
Hopkins, AM; Kichenadasse, G; Rathod, AD; Rowland, A; Sorich, MJ, 2020
)
0.56
"Females had approximately two-fold increased risk of developing severe rash compared to males in clinical trials of vemurafenib alone or in combination with cobimetinib."( Risk factors for severe rash with use of vemurafenib alone or in combination with cobimetinib for advanced melanoma: pooled analysis of clinical trials.
Hopkins, AM; Kichenadasse, G; Rathod, AD; Rowland, A; Sorich, MJ, 2020
)
0.56
"Administration of finerenone 20 mg once daily confers no risk of clinically relevant drug-drug interactions with substrates of cytochrome P450 enzymes."( Results from Drug-Drug Interaction Studies In Vitro and In Vivo Investigating the Effect of Finerenone on the Pharmacokinetics of Comedications.
Bairlein, M; Gerisch, M; Heinig, R; Loewen, S; Nagelschmitz, J, 2020
)
0.56
"This study was devised to investigate if P-glycoprotein (P-gp) mediated the drug-drug interaction (DDI) between genistein and repaglinide."( Molecular pharmacokinetic mechanism of the drug-drug interaction between genistein and repaglinide mediated by P-gp.
Huo, X; Jin, H; Liu, K; Ma, X; Meng, Q; Sun, H; Sun, P; Tan, A; Wang, C; Wu, J; Zhu, Y, 2020
)
0.56
" Pharmacokinetic parameters of cobimetinib and GDC-0994 given in combination were similar to those previously observed in monotherapy studies, so that there was no evidence of drug-drug interaction."( A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors.
Burris, H; Dokainish, H; Lockhart, A; LoRusso, P; Mueller, L; Murray, E; Park, E; Sarkar, I; Shapiro, G; Singh, J; Tagen, M; Weekes, C, 2020
)
0.56
" Pharmacokinetic data did not show evidence of a drug-drug interaction."( A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors.
Burris, H; Dokainish, H; Lockhart, A; LoRusso, P; Mueller, L; Murray, E; Park, E; Sarkar, I; Shapiro, G; Singh, J; Tagen, M; Weekes, C, 2020
)
0.56
" To our knowledge, no published or ongoing trial is trying to answer the question if patient can benefit from a potentially complete resection combined with PARPi maintenance in OC patients with secondary recurrence."( A phase II trial of cytoreductive surgery combined with niraparib maintenance in platinum-sensitive, secondary recurrent ovarian cancer: SGOG SOC-3 study.
Ai, Z; Bao, W; Chen, X; Feng, Y; Gao, W; Huang, H; Jia, H; Jiang, R; Jiang, W; Li, J; Li, Y; Liu, J; Luan, Y; Shi, T; Teng, Y; Wang, X; Wu, S; Yin, S; Yu, A; Zang, R; Zhang, J; Zhang, P; Zhang, W; Zhang, Y; Zhu, J; Zhu, T; Zhu, Y, 2020
)
0.56
" This review aimed to critically assess the drug-drug interaction potential of tofacitinib, baricitinib and upadacitinib and provide a balanced perspective for choosing the most appropriate Janus kinase inhibitor based on the needs of patients with rheumatoid arthritis including co-medications and renal/hepatic impairment status."( Critical Assessment of Pharmacokinetic Drug-Drug Interaction Potential of Tofacitinib, Baricitinib and Upadacitinib, the Three Approved Janus Kinase Inhibitors for Rheumatoid Arthritis Treatment.
Babu, RJ; Dash, RP; Madgula, LMV; Srinivas, NR; Thomas, JA; Veeravalli, V, 2020
)
0.56
" This study aimed to predict the impact of drug-drug interactions and renal or hepatic impairment on tofacitinib pharmacokinetics using a physiologically based pharmacokinetic (PBPK) model."( Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure and Support Dosing Recommendations for Potential Drug-Drug Interactions or in Special Populations: An Example Using Tofacitinib.
Dowty, ME; Gupta, P; Krishnaswami, S; Menon, S; Tse, S, 2020
)
0.56
" High-dose chemotherapy regimens such as DA-EPOCH should be administered to young patients in combination with rituximab."( Chidamide combined with ibrutinib improved the prognosis of primary bone marrow diffuse large B cell lymphoma.
Chen, Z; Li, Y; Tian, C, 2020
)
0.56
" After incubation for 2 h, the samples were pretreated and analyzed using liquid chromatography combined with diode-array detection and high-resolution mass spectrometry (LC/DAD-HRMS)."( Identification of the metabolites of piperine via hepatocyte incubation and liquid chromatography combined with diode-array detection and high-resolution mass spectrometry.
Li, M; Li, Y; Tang, J; Wang, Z; Wen, M, 2020
)
0.56
" However, BTKi have a range of drug-drug and drug-food interactions, which may alter drug efficacy and/or increase toxicity."( Drug interactions with Bruton's tyrosine kinase inhibitors: clinical implications and management.
Fancher, KM; Pappacena, JJ, 2020
)
0.56
"Antipsychotics are often used in combination with other psychotropic drugs to treat a variety of psychiatric disorders, as well as in combination with other drugs taken by patients with co-morbidities."( Asenapine and iloperidone decrease the expression of major cytochrome P450 enzymes CYP1A2 and CYP3A4 in human hepatocytes. A significance for drug-drug interactions during combined therapy.
Danek, PJ; Daniel, WA; Wójcikowski, J, 2020
)
0.56
" Here, M-134, a recently developed HDAC6 inhibitor, was examined for its therapeutic potential when combined with tofacitinib in a rat model of RA."( M-134, a novel HDAC6-selective inhibitor, markedly improved arthritic severity in a rodent model of rheumatoid arthritis when combined with tofacitinib.
Bae, D; Baek, J; Choi, Y; Ha, N; Lee, J; Park, J; Son, W; Suh, D, 2021
)
0.62
" The biotransformation was executed at a temperature of 37°C for 60 min, and the samples were analyzed by ultra-high performance liquid chromatography combined with high-resolution mass spectrometry (UHPLC-HRMS) operated in positive electrospray ionization mode."( Identification of the metabolites of tofacitinib in liver microsomes by liquid chromatography combined with high resolution mass spectrometry.
Dong, Z; Liu, P; Wu, S, 2021
)
0.62
" These variants were subsequently combined with replacement of the cysteine 481 residue to which irreversible inhibitors, such as ibrutinib, acalabrutinib and zanubrutinib, bind."( BTK gatekeeper residue variation combined with cysteine 481 substitution causes super-resistance to irreversible inhibitors acalabrutinib, ibrutinib and zanubrutinib.
Berglöf, A; Estupiñán, HY; Mohammad, DK; Schaafsma, GCP; Shi, Y; Smith, CIE; Vihinen, M; Wang, Q; Yu, L; Zain, R; Zhou, L, 2021
)
0.62
" The model was developed based on physicochemical and in vitro parameters, as well as clinical data, including pharmacokinetic data in patients with B-cell malignancies and in healthy volunteers from two clinical drug-drug interaction (DDI) studies of zanubrutinib as a victim of CYP modulators (itraconazole, rifampicin) or a perpetrator (midazolam)."( Comprehensive PBPK model to predict drug interaction potential of Zanubrutinib as a victim or perpetrator.
Gao, Y; Liu, D; Ou, YC; Sahasranaman, S; Wang, K; Yao, X; Zhang, M, 2021
)
0.62
" He was placed on intravenous immunoglobulin (IVIg) in combination with ibrutinib."( [Intravenous immunoglobulin in combination with ibrutinib for the treatment of IgM-type M protein associated peripheral neuropathy complicated with chronic lymphocytic leukemia].
Kawano, K; Kawano, Y; Miyazaki, Y; Ohtsuka, E; Saburi, M; Sakata, M; Takata, H; Uchida, H, 2021
)
0.62
" The highest tested dose of ibrutinib, 560 mg once daily, was combined with a fixed dose of pembrolizumab 200 mg every 3 weeks for the phase 2 portion."( A phase 1/2 trial of ibrutinib in combination with pembrolizumab in patients with mismatch repair proficient metastatic colorectal cancer.
Carballido, E; Imanirad, I; Kim, DW; Kim, RD; Martinez, M; Mehta, R; Schell, MJ; Strosberg, J; Tan, E; Yu, J; Zhou, JM, 2021
)
0.62
" Herein, we investigated the effects of the two drugs on UDP-glucuronosyltransferase (UGT) activities to evaluate their potential risk for drug-drug interactions (DDIs) via UGT inhibition."( Comparison of the drug-drug interactions potential of ibrutinib and acalabrutinib via inhibition of UDP-glucuronosyltransferase.
Cao, J; Fan, X; Jiang, L; Liu, Y; Wang, X; Wang, Z; Xia, Y; Yan, M, 2021
)
0.62
"In patients treated with tofacitinib in combination with a biologic, no new safety signals were observed."( Safety and Efficacy of Tofacitinib in Combination With Biologic Therapy for Refractory Crohn's Disease.
Barahimi, M; Clark-Snustad, KD; Harper, J; Jacobs, J; Kamp, KJ; Lee, SD; Singla, A, 2022
)
0.72
" In subsequent drug combination experiments, tepotinib synergistically reversed daunorubicin and mitoxantrone resistance in cells with ABCB1 and ABCG2 overexpression, respectively."( Tepotinib Inhibits Several Drug Efflux Transporters and Biotransformation Enzymes: The Role in Drug-Drug Interactions and Targeting Cytostatic Resistance In Vitro and Ex Vivo.
Budagaga, Y; Hanke, I; Hofman, J; Kammerer, S; Küpper, JH; Morell, A; Novotná, E; Rozkoš, T; Skarka, A; Vagiannis, D; Zhang, Y, 2021
)
0.62
" We hypothesized that a tailored treatment with ibrutinib in combination with rituximab (IR) could obtain significant responses in these patients."( Ibrutinib in Combination With Rituximab for Indolent Clinical Forms of Mantle Cell Lymphoma (IMCL-2015): A Multicenter, Open-Label, Single-Arm, Phase II Trial.
Aymerich, M; Beà, S; Campo, E; Casanova, M; Cortés-Romera, M; de la Cruz, F; de la Fuente, A; García Sanz, R; Giné, E; González Barca, E; González-López, TJ; Jiménez Ubieto, A; López Jimenez, J; López-Guillermo, A; Marín-Niebla, A; Martín García-Sancho, A; Medina Herrera, A; Muntañola, A; Nadeu, F; Rodríguez, S; Rotger, A; Setoain, X; Terol, MJ, 2022
)
0.72
" We administered tofacitinib combined with leflunomide to a 38-year-old female patient who presented with PsA and IgA nephropathy."( Tofacitinib combined with leflunomide for treatment of psoriatic arthritis with IgA nephropathy: a case report with literature review.
Ci, X; Du, X; Li, L; Lu, X; Luo, M; Wu, L; Xue, H, 2022
)
0.72
"To explore the effects of systematic diet education combined with multidisciplinary nursing on nutritional status and calcium and phosphorus metabolism in patients with diabetic kidney disease (DKD) in uremic phase after treatment with alogliptin."( Effects of Systematic Diet Education Combined with Multidisciplinary Nursing on Nutritional Status and Calcium and Phosphorus Metabolism in Patients with Diabetic Kidney Disease in Uremic Phase after Treatment with Alogliptin.
Guo, N; Li, N; Liu, K; Sun, H; Zhao, Y, 2022
)
0.72
" The combination group received systematic dietary education combined with multidisciplinary nursing after the medication, and the conventional group received conventional intervention."( Effects of Systematic Diet Education Combined with Multidisciplinary Nursing on Nutritional Status and Calcium and Phosphorus Metabolism in Patients with Diabetic Kidney Disease in Uremic Phase after Treatment with Alogliptin.
Guo, N; Li, N; Liu, K; Sun, H; Zhao, Y, 2022
)
0.72
"With conspicuous intervention effect, systematic diet education combined with multidisciplinary nursing is a reliable method that can improve the nutritional status and levels of calcium and phosphorus metabolism, enhance treatment compliance, and reduce anxiety."( Effects of Systematic Diet Education Combined with Multidisciplinary Nursing on Nutritional Status and Calcium and Phosphorus Metabolism in Patients with Diabetic Kidney Disease in Uremic Phase after Treatment with Alogliptin.
Guo, N; Li, N; Liu, K; Sun, H; Zhao, Y, 2022
)
0.72
"To explore the effect of resveratrol (RES) combined with donepezil hydrochloride on inflammatory factor level and cognitive function level of patients with Alzheimer's disease (AD)."( Effect of Resveratrol Combined with Donepezil Hydrochloride on Inflammatory Factor Level and Cognitive Function Level of Patients with Alzheimer's Disease.
Fang, X; Wang, L; Zhang, J; Zhao, J, 2022
)
0.72
" This study was conducted to explore the clinical effects of repaglinide combined with exercise rehabilitation on improving the blood glucose of patients with diabetes."( Clinical Effects of Exercise Rehabilitation Combined with Repaglinide in the Treatment of Diabetes.
Li, Y; Wang, X; Zhang, Y, 2022
)
0.72
" First three groups were treated with Acai berry (PO; 250 mg/kg); fourth, fifth and sixth groups received sodium CMC (vehicle) for 10 days and on eleventh day, first and fourth groups were administered with ATR (PO; 10 mg/kg); second and fifth groups with ALO (PO; 25 mg/kg) and third and sixth groups received EMPA (PO; 25 mg/kg)."( Investigation of the effect of Acai berry on the pharmacokinetics of Atorvastatin, Alogliptin and Empagliflozin: a herb-drug interaction study.
Nanjappan, SK; Ravichandiran, V; Somabattini, RA, 2022
)
0.72
"Cobimetinib combined with vemurafenib was available in France in 2015 through a 'Temporary Authorization for Use' program (TAU, preapproval access pending its marketing on 2016) for patients with v-raf murine sarcoma viral oncogene homolog B1-mutant advanced melanoma."( Survival in adult patients with BRAFV600 mutation-positive advanced melanoma: a noninterventional ambispective study of patients with cobimetinib combined with vemurafenib during the French early access program: MELANIS study.
Duval-Modeste, AB; El Adaoui, L; Lelarge, Y; Mateus, C; Meyer, N; Niarra, R; Pérol, D, 2022
)
0.72
"In order to investigate the effect of remifentanil combined with propofol on awakening of craniotomy for tumor, a retrospective analysis is conducted."( The Efficacy of Remifentanil Combined with Propofol in Craniotomy for Tumor Was Evaluated by Wake Quality, Hemodynamics, and Adverse Reactions.
Chen, J; Han, Y; Zhou, Q, 2022
)
0.72
" This study aimed to evaluate the analgesic effects and safety of CSA using different doses of remifentanil combined with dexmedetomidine during peritoneal dialysis catheter insertion."( Conscious sedation anesthesia using different doses of remifentanil combined with dexmedetomidine for peritoneal dialysis catheter implantation.
Ding, J; Fang, X; Liu, K; Ren, X; Wang, M; Yang, Q; Yao, L, 2023
)
0.91
"07 μg/kg/min) combined with dexmedetomidine achieved satisfactory anesthetic effects with fewer adverse drug reactions during PD catheter implantation, indicating its potential for use in patients undergoing PD catheter placement."( Conscious sedation anesthesia using different doses of remifentanil combined with dexmedetomidine for peritoneal dialysis catheter implantation.
Ding, J; Fang, X; Liu, K; Ren, X; Wang, M; Yang, Q; Yao, L, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
"Following oral administration of the 14C-labeled title compound to male mice, the drug was well absorbed and rapidly distributed throughout the body."( The disposition of threo-alpha-(2-piperidyl)-2-trifluoromethyl-6-(4-trifluoromethylphenyl)-4-pyridinemethanol phosphate in mice.
Chung, H; Gillum, HH; Rozman, RS,
)
0.13
"Following oral administration of 14C-labeled mefloquine hydrochloride to female mice, the drug was well absorbed and distributed throughout the body."( The absorption, distribution, and excretion in mice of the antimalarial mefloquine, erythro-2,8-bis(trifluoromethyl)-alpha-(2-piperidyl)-4-quinolinemethanol hydrochloride.
Koby, R; Molek, NA; Rozman, RS,
)
0.13
" The pharmacokinetic parameters were not found to be dose dependent in the range investigated, but it was not possible to decide whether the bioavailability was dependent on the dose."( Pharmacokinetics of femoxetine in man.
Bechgaard, E; Christensen, JA; Larsson, H; Lund, J; Molander, L, 1979
)
0.26
"Penfluridol, 1-[4,4-bis(4-fluorophenyl)butyl]-4-[4-chloro-3-(trifluoromethyl)phenyl]-4-piperidinol, was well absorbed by the rat, rabbit, dog, and man after single oral doses of drug in solution."( The comparative metabolism and disposition of penfluridol-3H in the rat, rabbit, dog, and man.
Cressman, WA; Grindel, JM; Migdalof, BH,
)
0.13
" Comparison of the area under the curves during steady state (ss) indicated a complete bioavailability of multiple oral doses."( Disposition and antiarrhythmic effect of lorcainide.
Heimburg, P; Klotz, U; Müller-Seydlitz, P, 1979
)
0.26
" In 4 of the healthy volunteers, the bioavailability of a single 100mg(n = 2) and 150mg (n = 2) oral dose was determined."( Pharmacokinetics of lorcainide in man: a new antiarrhythmic agent.
Heimburg, P; Klotz, U; Müller-Seydlitz, P,
)
0.13
" Derivatives of the spiroindenepiperidine ring system, these compounds include L-366,509, an orally bioavailable OT antagonist with good in vivo duration."( Orally active, nonpeptide oxytocin antagonists.
DiPardo, RM; Evans, BE; Gilbert, KF; Gould, NP; Hobbs, DW; Leighton, JL; Lundell, GF; Pettibone, DJ; Rittle, KE; Veber, DF, 1992
)
0.28
" Preclinical studies in the rat have shown the drug to be well absorbed and extensively metabolized."( Quantitative determination of CGS 18102A, a new anxiolytic, in human plasma using capillary gas chromatography/mass spectrometry.
Hayes, MJ; Leal, M; Powell, ML,
)
0.13
" The total bioavailability of BM 12."( Pharmacokinetics of the organic nitrates trans-2-amino-2-methyl-N-(4- nitroxycyclohexylmethyl)-propionamide in dogs, and of 4-(2-nitroxyethyl)-piperidine in dogs and in monkeys.
Bartsch, W; Neidlein, R; Pressmar, F; Strein, K, 1992
)
0.28
" The peak plasma concentration of disopyramide in association with cisapride oral administration was significantly higher, and the apparent absorption rate constant and lag time of disopyramide were about 2-fold higher and 2-fold shorter, respectively, than for disopyramide alone."( Effects of cisapride on gastrointestinal motor activity and gastric emptying of disopyramide.
Akima, M; Azumi, T; Fukuzaki, H; Inatome, T; Kuroda, T; Nakamura, H; Takanashi, H; Yogo, K; Yoshihara, Y, 1992
)
0.28
" The well known bioavailability parameters of absorption and the area under the curve of the fractional absorbed time profiles up to 30 min were used as an index of gastric emptying."( Influence of cisapride, metoclopramide and loperamide on gastric emptying of normal volunteers as measured by means of the area under the curve of the cumulative fraction absorbed-time profiles of paracetamol.
Moncrieff, J; Sommers, DK; van Wyk, M, 1992
)
0.28
" They are well absorbed orally but exhibit an extensive first-pass extraction in the liver."( Pharmacokinetics of the selective serotonin reuptake inhibitors.
DeVane, CL, 1992
)
0.28
" Paroxetine is well absorbed from the gastrointestinal tract and undergoes first-pass metabolism that is partially saturable."( The pharmacologic profile of paroxetine, a new selective serotonin reuptake inhibitor.
Johnson, AM; Tulloch, IF, 1992
)
0.28
"The effect of piperine on the bioavailability and pharmacokinetics of propranolol and theophylline has been examined in a crossover study."( Effect of piperine on bioavailability and pharmacokinetics of propranolol and theophylline in healthy volunteers.
Bano, G; Bedi, KL; Johri, RK; Raina, RK; Sharma, SC; Zutshi, U, 1991
)
0.28
" The bioavailability of A10 capsules was determined with tritium-labelled A10 in rabbits."( Studies of the release rate and bioavailability of antineoplaston A10 capsule.
Wang, H; Xu, W; Yuan, Y, 1990
)
0.28
"The comparative bioavailability of cisapride as a 30 mg suppository and three 5 mg oral tablets was investigated in 12 non-smoking, healthy male volunteers."( Comparative bioavailability of a cisapride suppository and tablet formulation in healthy volunteers.
Gelin-Friberg, A; Hedner, J; Hedner, T; Heykants, J; Huang, ML; Van de Poel, S; Van Peer, A; Woestenborghs, R, 1990
)
0.28
" The drugs were quantitated in samples from bioavailability studies performed in dogs."( Determination of a new anti-allergenic agent, 1-[4-[3-[4-[bis-(4-fluorophenyl)hydroxymethyl]-1-piperidinyl] propoxy]-3-methoxyphenyl]ethanone, and its active acidic metabolite in plasma by high-performance liquid chromatography.
Cheng, LK; Greene, SV; Krebs, HA; Lemieux, RE, 1990
)
0.28
" Systemic oral bioavailability averaged 87% in humans."( Preclinical and clinical pharmacokinetics of pirmenol.
Chang, T, 1987
)
0.27
" bioavailability and a relatively long duration of action."( Pharmacology of risperidone (R 64 766), a new antipsychotic with serotonin-S2 and dopamine-D2 antagonistic properties.
Awouters, F; Janssen, PA; Meert, TF; Megens, AA; Niemegeers, CJ; Schellekens, KH, 1988
)
0.27
"Paroxetine is well absorbed from the gastrointestinal tract, and appears to undergo first-pass metabolism which is partially saturable."( A review of the metabolism and pharmacokinetics of paroxetine in man.
Greb, WH; Haddock, RE; Kaye, CM; Langley, PF; Mellows, G; Tasker, TC; Zussman, BD, 1989
)
0.28
" analysis of spiked samples demonstrated the good accuracy and precision of the method, which is suitable for use in pharmacokinetic and bioavailability studies."( Determination of the new monoamine oxidase inhibitor brofaromine and its major metabolite in biological material by gas chromatography with electron-capture detection.
Degen, PH; Keller, B; Schneider, W, 1989
)
0.28
" Loperamide is well absorbed after oral administration and extensively metabolized."( Loperamide--an opiate receptor agonist with gastrointestinal motility effects.
Mellstrand, T, 1987
)
0.27
" ratios indicate that, relative to ranitidine, the bioavailability of AY-29,315 by the oral route was low, particularly in the dog."( Antisecretory and antiulcer activities of a potent new histamine H2-receptor antagonist with an intermediate duration of action.
Borella, L; Failli, A; Grimes, D; Mir, GN; Rimele, TJ; Russell, J, 1988
)
0.27
" Furthermore, there was no interference in the bioavailability of roxatidine acetate 150 mg daily when administered alone or in combination with a meal or antacids."( Interaction of roxatidine acetate with antacids, food and other drugs.
Labs, RA, 1988
)
0.27
" Relative bioavailability of conjugated tyramine was elevated sixfold by brofaromine and 11."( Monoamine oxidase inhibition by phenelzine and brofaromine in healthy volunteers.
Antonin, KH; Bieck, PR; Firkusny, L; Nilsson, E; Schick, C; Schulz, R; Schwenk, M; Wollmann, H, 1989
)
0.28
" Bioavailability ranged between 15 and 60%, indicating a substantial first-pass effect."( Blood pressure reduction and pharmacokinetics of ketanserin in hypertensive patients.
Hedner, T; Persson, B; Pettersson, A, 1986
)
0.27
" Gastric emptying after each premedication was assessed indirectly from the rate of absorption of oral paracetamol."( Comparison of the effect of cisapride and metoclopramide on morphine-induced delay in gastric emptying.
Bamber, PA; Nimmo, WS; Rowbotham, DJ, 1988
)
0.27
" According to these findings in the dog, the use of deuterated lorcainide in human bioavailability and metabolism studies is probably of limited value."( The use and limitations of deuterated lorcainide in metabolism and pharmacokinetic studies.
Gelijkens, CF; Heykants, J; Knaeps, A; Lenoir, H; Van Peer, A; Woestenborghs, R, 1985
)
0.27
"The bioavailability of ketanserin has been examined in a cross-over experiment in 21 elderly subjects (aged 59-72 years) by administration of tablets (40 mg), solution (40 mg) and injectable solution (10 mg)."( Bioavailability and pharmacokinetics of ketanserin in elderly subjects.
Kurowski, M, 1985
)
0.27
" Compared with intravenous administration, the absolute bioavailability of oral cisapride was 23% in rats and 53% in the dog for the drug given in solution."( Pharmacokinetics and tissue distribution of the new gastrokinetic agent cisapride in rat, rabbit and dog.
Geerts, R; Hendriks, R; Heykants, J; Michiels, M; Monbaliu, J; Woestenborghs, R, 1987
)
0.27
"Relative bioavailability of the investigational gastrointestinal stimulant agent cisapride after oral administration was determined in healthy men."( Bioavailability of three oral dosage forms of cisapride, a gastrointestinal stimulant agent.
Barone, JA; Bierman, RH; Colaizzi, JL; Heykants, J; Huang, YC; Kerr, DA; Long, JF; Van Peer, A; Woestenborghs, R, 1987
)
0.27
" The initial rate of absorption of diazepam contained in the drink was increased by C (AUC 0-1 h C: 328 micrograms h l-1, P: 253 micrograms h l-1, but there was no change in overall bioavailability."( The action of cisapride on gastric emptying and the pharmacodynamics and pharmacokinetics of oral diazepam.
Bateman, DN, 1986
)
0.27
" The bioavailability of muscular injection was unity."( Fundamental pharmacokinetic properties of biperiden: tissue distribution and elimination in rabbits.
Ichimura, F; Nakashima, E; Yamana, T; Yokogawa, K, 1986
)
0.27
" The observed interaction can be explained by an increase in bioavailability or, more probably, by a decrease in biotransformation of flecainide in the presence of cimetidine."( Altered pharmacokinetics of oral flecainide by cimetidine.
de Schepper, PJ; Tjandra-Maga, TB; van Hecken, A; van Melle, P; Verbesselt, R, 1986
)
0.27
" Orally administered ketanserin was well absorbed and almost completely metabolized in both species."( Excretion and biotransformation of ketanserin after oral and intravenous administration in rats and dogs.
Hendrickx, J; Heykants, J; Hurkmans, R; Knaeps, F; Lauwers, W; Meuldermans, W; Swysen, E; Woestenborghs, R,
)
0.13
" The mean absolute bioavailability for the oral dose was 87%."( Pharmacokinetics and efficacy of pirmenol hydrochloride in the treatment of ventricular dysrhythmia.
Chang, T; Goldberg, AD; Goldstein, S; Johnson, EL; Lee, TG; Serkland, MT; Toole, JG; Yakatan, GJ,
)
0.13
" Flecainide pharmacokinetics are suitable for oral use but encainide disposition is complex with variable bioavailability and active metabolites that contribute substantially to activity."( Clinical profiles of newer class I antiarrhythmic agents--tocainide, mexiletine, encainide, flecainide and lorcainide.
Pottage, A, 1983
)
0.27
" Lorcainide is also a class Ic antiarrhythmic drug, the bioavailability of which is nonlinear."( Clinical pharmacokinetics of the newer antiarrhythmic agents.
Gillis, AM; Kates, RE,
)
0.13
"Lorcainide is a new type 1 antiarrhythmic drug that is well absorbed orally, with bioavailability increasing with both dose and continued administration."( Pharmacology of lorcainide.
Keefe, DL, 1984
)
0.27
"A new benzothiophene-derived antiestrogen (LY156758) when orally administered was well absorbed in rats and monkeys while approx."( Disposition and metabolism of a new benzothiophene antiestrogen in rats, dogs and monkeys.
Lindstrom, TD; Whitaker, GW; Whitaker, NG, 1984
)
0.27
" In control rats, the total blood clearance of lorcainide was 30 ml/kg/min and the bioavailability was 14%."( Effect of enzyme induction on the disposition of lorcainide in rats following intravenous and oral administration.
Jähnchen, E; Plänitz, V, 1984
)
0.27
" A substantial first-pass effect led to a bioavailability of about 50% (range: 27-69%)."( Pharmacokinetics of ketanserin in man.
Klotz, U; Okonkwo, PO; Reimann, IW, 1983
)
0.27
" The tablet gave a longer lag time and a slower absorption rate than the solution."( Biovailability and pharmacokinetics of femoxetine.
Lange, J; Lund, J; Mengel, H, 1983
)
0.27
"To determine whether the antidiarrheal effect of loperamide is due to an effect on intestinal motor function or to an acceleration of the rate of absorption by the intestine (as has been suggested recently), we studied absorption during experimental diarrhea produced by the rapid intragastric infusion of electrolyte solution."( Mechanism of the antidiarrheal effect of loperamide.
Fordtran, JS; Morawski, SG; Santa Ana, CA; Schiller, LR, 1984
)
0.27
" The drug is well absorbed by the oral route and its elimination half-life is long when compared with other substances."( Lorcainide (R 15 889), a first review.
Amery, WK; Gough, DA; Heykants, JJ; Janssen, PA; Oettel, P; Towse, G; Xhonneux, R, 1981
)
0.26
"The pharmacokinetics and bioavailability of domperidone, a novel gastrokinetic, were studied in healthy male subjects by comparing plasma concentrations and urinary excretion following intravenous, intramuscular, oral and rectal administration."( On the pharmacokinetics of domperidone in animals and man. IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration.
Hendriks, R; Heykants, J; Meuldermans, W; Michiels, M; Reyntjens, H; Scheygrond, H, 1981
)
0.26
"3:1, suggesting that hepatic metabolism of perhexiline may be saturable and that the bioavailability of perhexiline is dose dependent."( High-performance liquid chromatographic assay of perhexiline maleate in plasma.
Drummer, OH; Goble, AJ; Horowitz, JD; Louis, WJ; Morris, PM, 1981
)
0.26
" The results suggest that these acrids have the capacity to increase the bioavailability of certain drugs."( Scientific evidence on the role of Ayurvedic herbals on bioavailability of drugs.
Atal, CK; Rao, PG; Zutshi, U, 1981
)
0.26
"The in vitro fate of an ester prodrug, glycovir, was studied to determine if the species differences in the bioavailability of pharmacologically active SC-48334 observed after glycovir administration and not observed after SC-48334 administration is due to species differences in ester hydrolysis rate or species differences in absorption of the prodrug itself, and to determine the site(s) of ester hydrolysis which contributes most to species differences in the bioavailability of SC-48334 if any."( Species dependent esterase activities for hydrolysis of an anti-HIV prodrug glycovir and bioavailability of active SC-48334.
Cook, CS; Karabatsos, PJ; Karim, A; Schoenhard, GL, 1995
)
0.29
" After SC-48334 administration, SC-48334 was rapidly and similarly well absorbed in all species."( Species dependent esterase activities for hydrolysis of an anti-HIV prodrug glycovir and bioavailability of active SC-48334.
Cook, CS; Karabatsos, PJ; Karim, A; Schoenhard, GL, 1995
)
0.29
"The species differences in bioavailability of SC-48334 with the prodrug were due to species differences in hydrolysis rates of the prodrug in small intestinal mucosa."( Species dependent esterase activities for hydrolysis of an anti-HIV prodrug glycovir and bioavailability of active SC-48334.
Cook, CS; Karabatsos, PJ; Karim, A; Schoenhard, GL, 1995
)
0.29
" The newer antipsychotic agents clozapine and risperidone are also well absorbed and undergo extensive presystemic elimination."( Brief comparison of the pharmacokinetics and pharmacodynamics of the traditional and newer antipsychotic drugs.
DeVane, CL, 1995
)
0.29
" Iloperidone was well absorbed orally in fasted subjects."( Safety, tolerability, and effect of food on the pharmacokinetics of iloperidone (HP 873), a potential atypical antipsychotic.
Brecher, MB; Chi, E; Grasing, K; Hubbard, JW; Sainati, SM, 1995
)
0.29
" The oral bioavailability of BMS-184111 was found to be 10% after administration of the free base and 23% after administration of the hydrochloride salt."( In vivo disposition and in vitro metabolism of an anxiolytic compound, BMS-184111, in rats.
Catt, JD; Knipe, JO; Mattson, RJ; McGoff, KB; Rourick, R; Volk, KJ; Yeleswaram, K, 1995
)
0.29
" Risperidone absolute oral bioavailability was 66%."( Pharmacokinetics of the novel antipsychotic agent risperidone and the prolactin response in healthy subjects.
De Coster, R; Heykants, J; Huang, ML; Jansen, AA; Jonkman, JH; Van Peer, A; Visscher, HW; Woestenborghs, R; Zylicz, Z, 1993
)
0.29
" The absorption rate constant was increased significantly after multiple administration as compared to that of single administration."( Effect of oral multiple-dose administration of anti-inflammatory flurbiprofen chimera drug on gastric lesion, other toxicities and disposition kinetics.
Fukuhara, A; Imai, T; Inoue, K; Otagiri, M, 1995
)
0.29
" Tanaka, Yakuzaigaku, accepted) was evaluated by the dissolution test and its bioavailability in beagle dogs was determined."( Evaluation of a pharmaceutical preparation of 2-[4-(p-fluorobenzoyl)-piperidin-1-yl]-2'-acetonaphthone hydrochloride with enhanced dissolution rate.
Tanaka, T; Tokumura, T, 1994
)
0.29
" These effects would be expected to increase the initial rate of absorption of orally administered drugs, but reduce total bioavailability of the agents."( Pharmacokinetic drug interactions with gastrointestinal motility modifying agents.
Greiff, JM; Rowbotham, D, 1994
)
0.29
" Comparison of the parenteral and enteral potencies indicated that FRG-8813 has a lower bioavailability than famotidine and cimetidine in rats and dogs."( Gastric antisecretory effect of FRG-8813, a new histamine H2 receptor antagonist, in rats and dogs.
Chida, Y; Inaba, N; Ohnishi, H; Onodera, S; Shibata, M; Yamaura, T, 1993
)
0.29
" The absorption was complete with an oral bioavailability of 92-131%."( Metabolism and disposition of EXP631--a novel antidepressant analgesic.
Burcham, DL; Huang, SM; Quon, CY; Wong, YN, 1993
)
0.29
" The new OT antagonist L-367,773 (35) is shown to be an orally bioavailable agent with good duration in vivo and to inhibit OT-stimulated uterine contractions effectively in several in vitro and in vivo models."( Nanomolar-affinity, non-peptide oxytocin receptor antagonists.
Bock, MG; Carroll, LA; Evans, BE; Gilbert, KF; Leighton, JL; Lundell, GF; Pawluczyk, JM; Rittle, KE; Williams, PD; Young, MB, 1993
)
0.29
" The absolute bioavailability of bidisomide was 45-62% which is lower than that of disopyramide (60-90%)."( Importance of pharmacokinetic and physicochemical data in the discovery and development of novel anti-arrhythmic drugs.
Cook, CS; Karim, A; McDonald, SJ, 1993
)
0.29
" These compounds are structurally related to the 1-(4-piperidyl)-2(1H)-quinolinones, including OPC-21268, an orally bioavailable AVP V1 antagonist with high V1 specificity."( Orally active, nonpeptide vasopressin V1 antagonists. A novel series of 1-(1-substituted 4-piperidyl)-3,4-dihdyro-2(1H)-quinolinone.
Chihara, T; Kondo, K; Miyamoto, H; Mori, T; Nakaya, K; Ogawa, H; Tominaga, M; Yabuuchi, Y; Yamamura, Y; Yamashita, H, 1993
)
0.29
"The effect of food on the bioavailability of brofaromine hydrochloride was investigated in a randomized cross-over study."( Influence of food on the disposition of the monoamine oxidase-A inhibitor brofaromine in healthy volunteers.
Cardot, JM; Czendlik, C; Degen, PH; Dieterle, W, 1993
)
0.29
" Tetrazole 19 inhibits radiation-induced emesis in the ferret with high potency when administered both subcutaneously and orally, has a long duration of action, and has high oral bioavailability in the dog."( Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity.
Armour, DR; Bays, DE; Evans, B; Giblin, GM; Heron, N; Hubbard, T; Liang, K; Middlemiss, D; Mordaunt, J; Ward, P, 1995
)
0.29
" The bioavailability of parent LY255582 was < 1% in both the rat and the dog, primarily because of extensive first-pass metabolism."( Disposition of the opioid antagonist, LY255582, in rats and dogs.
Catlow, J; Chay, SH; Johnson, T; Pohland, RC; Swanson, SP, 1995
)
0.29
" Long half life and oral bioavailability would be desirable for prophylactic treatment of thrombotic disorders."( Synthesis and characterisation of novel thrombin inhibitors based on 4-amidinophenylalanine.
Czech, J; Dickneite, G; Hoffmann, D; Koschinsky, R; Reers, M; Stüber, W, 1995
)
0.29
" dose ratio was approximately one, suggesting that LY353433 was well absorbed with excellent pharmacodynamics in the rat."( LY353433, a potent, orally effective, long-acting 5-HT(4) receptor antagonist: comparison to cisapride and RS23597-190.
Bloomquist, W; Calligaro, DA; Cohen, I; Cohen, ML; Schaus, JM; Susemichel, AD; Thompson, DC, 1996
)
0.29
" The amphiphilic compound exhibits virtually no systemic bioavailability despite proteolytic stability and proven enteral absorption."( First-pass elimination of a peptidomimetic thrombin inhibitor is due to carrier-mediated uptake by the liver. Interaction with bile acid transport systems.
Dickneite, G; Eckhardt, U; Petzinger, E; Reers, M; Stüber, W, 1996
)
0.29
" In animal studies, L-368,899 was shown to be a potent and selective OT antagonist and was orally bioavailable in rats, dogs and chimpanzees."( Progress in the development of oxytocin antagonists for use in preterm labor.
Bock, MG; Evans, BE; Guidotti, M; Harrell, CM; Jasper, JR; Lis, EV; O'Brien, JA; Pettibone, DJ; Reiss, DR; Woyden, CJ, 1995
)
0.29
" The effect of food on their bioavailability is similar."( Modulation of insulin secretion in non-insulin-dependent diabetes mellitus by two novel oral hypoglycaemic agents, NN623 and A4166.
Kikuchi, M, 1996
)
0.29
" The striking potency of these agents, their bioavailability and the dissociation of neurotrophic from immunosuppressant actions argue for their therapeutic relevance in the treatment of neurodegenerative diseases."( Neurotrophic actions of nonimmunosuppressive analogues of immunosuppressive drugs FK506, rapamycin and cyclosporin A.
Connolly, MA; Dawson, TM; Hamilton, GS; Hester, L; Snyder, SH; Steiner, JP; Valentine, HL, 1997
)
0.3
" dose both probably due to extensive and rapid metabolism of the parent drugs as suggested by the low values for bioavailability (range 13."( A method using a liquid chromatographic-electrospray-mass spectrometric assay for the determination of antimigraine compounds: preliminary pharmacokinetics of MDL 74,721, sumatriptan and naratriptan, in rabbit.
David, M; Duléry, BD; Huebert, ND; Petty, MA; Schoun, J, 1997
)
0.3
" In conscious rats and dogs, naratriptan has high oral bioavailability (71% and 95%, respectively)."( Naratriptan: biological profile in animal models relevant to migraine.
Beattie, DT; Connor, HE; Feniuk, W; Humphrey, PP; North, PC; Oxford, AW; Saynor, DA, 1997
)
0.3
" Following oral administration to animals, metabolic clearance resulted in decreased bioavailability due to first-pass metabolism in rat and mouse."( Pharmacokinetics and metabolism of zamifenacin in mouse, rat, dog and man.
Beaumont, KC; Causey, AG; Coates, PE; Smith, DA, 1996
)
0.29
" Pharmacokinetic evaluation of SB 223412 in rat and dog indicated low plasma clearance, oral bioavailability and high and sustained plasma concentrations after 4 to 8 mg/kg oral dosages."( Nonpeptide tachykinin receptor antagonists: I. Pharmacological and pharmacokinetic characterization of SB 223412, a novel, potent and selective neurokinin-3 receptor antagonist.
Brawner, ME; Elshourbagy, NA; Foley, JJ; Giardina, GA; Griswold, DE; Hay, DW; Martin, LD; Medhurst, AD; Potts, W; Sarau, HM; Schmidt, DB; Webb, EF, 1997
)
0.3
" Compound 36 is an antagonist of hD4 receptors with good oral bioavailability of 38%, a half life of 2 h, and brain levels 10-fold higher than plasma levels."( 4-Heterocyclylpiperidines as selective high-affinity ligands at the human dopamine D4 receptor.
Baker, R; Ball, R; Broughton, HB; Collins, I; Davey, WB; Emms, F; Freedman, SB; Leeson, PD; Marwood, R; Patel, S; Ragan, CI; Rowley, M, 1997
)
0.66
" Coadministration of sucralfate leads to a 44% decrease in the bioavailability of sparfloxacin."( Pharmacokinetics of sparfloxacin and interaction with cisapride and sucralfate.
Borner, K; Geerdes-Fenge, HF; Koeppe, P; Lode, H; Rau, M; Vöckler, J; Zix, JA, 1997
)
0.3
" Information on serum/plasma concentration, bioavailability and half-life can often aid the discovery process by selecting those candidates with the desired pharmacokinetic parameters."( Pharmacokinetic screening for the selection of new drug discovery candidates is greatly enhanced through the use of liquid chromatography-atmospheric pressure ionization tandem mass spectrometry.
Bryant, MS; Korfmacher, WA; Lin, CC; Nardo, C; Nomeir, AA; Wang, S, 1997
)
0.3
" However, NAPAP and other benzamidine derivatives do not show favorable pharmacological properties; above all, they have very low systemic bioavailability after oral administration."( Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.
Hauptmann, J; Prasa, D; Stürzebecher, J; Vieweg, H; Wikström, P, 1997
)
0.3
"59 ng/ml, and bioavailability +/- SD was 29."( Pharmacokinetics and suggested oral dosing regimen of cisapride: a study in healthy cats.
Boothe, DM; Herndon, S; LeGrange, SN; Willard, MD,
)
0.13
" Increasing bioavailability has been achieved with greater lipophilicity and thus the potential for greater activity in the central nervous system."( Inhibition of trigeminal neurones after intravenous administration of naratriptan through an action at 5-hydroxy-tryptamine (5-HT(1B/1D)) receptors.
Goadsby, PJ; Knight, Y, 1997
)
0.3
" This may be due to poor bioavailability during a migraine attack."( Ineffectiveness of neurokinin-1 antagonist in acute migraine: a crossover study.
Goldstein, DJ; Mathew, NT; Saper, JR; Silberstein, SD; Stoltz, R; Wang, O, 1997
)
0.3
" Donepezil has a relative bioavailability of 100% following oral administration and is not affected by the presence of food."( Donepezil use in Alzheimer disease.
Barner, EL; Gray, SL, 1998
)
0.3
" The oral bioavailability of inogatran was incomplete, presumably due to a low membrane permeability, and dose dependent."( Animal pharmacokinetics of inogatran, a low-molecular-weight thrombin inhibitor with potential use as an antithrombotic drug.
Bredberg, U; Eriksson, UG; Regårdh, CG; Renberg, L; Teger-Nilsson, AC, 1998
)
0.3
" Bidisomide AUC was decreased since it was well absorbed in the upper but not lower small intestine."( Reduced systemic availability of an antiarrhythmic drug, bidisomide, with meal co-administration: relationship with region-dependent intestinal absorption.
Cook, C; Fleisher, D; Kararli, T; Karim, A; Kirchhoff, C; Pao, LH; Truelove, J; Zhou, SY, 1998
)
0.3
" All three showed excellent oral bioavailability in vivo in nude mice and cynomolgus monkeys and exhibited excellent antitumor efficacy against a series of tumor cell lines when dosed orally in nude mice."( Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridi
Bishop, WR; Bryant, MS; Carr, DM; Catino, JJ; Chen, J; Chen, KJ; Dell, J; Doll, RJ; Ganguly, AK; Girijavallabhan, VM; Kirschmeier, P; Korfmacher, WA; Lee, S; Li, Z; Lin, CC; Lipari, P; Liu, M; Mallams, AK; Nardo, C; Nomeir, AA; Patton, R; Petrin, J; Rossman, RR; Wang, L; Wang, S, 1998
)
0.3
" Bioavailability was calculated to be 20."( Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa.
Hirayama, F; Hisamichi, N; Kawasaki, T; Kayama, M; Koshio, H; Mano, Y; Matsumoto, Y; Sakai, Y; Sato, K; Taniuchi, Y, 1998
)
0.3
" It is shown to enhance the bioavailability of various structurally and therapeutically diverse drugs."( Permeability characteristics of piperine on oral absorption--an active alkaloid from peppers and a bioavailability enhancer.
Bedi, KL; Khajuria, A; Zutshi, U, 1998
)
0.3
" The bioavailability of MK-499 was high in dogs (100%) but low in rats (17%)."( Metabolism of MK-499, a class III antiarrhythmic agent, in rats and dogs.
Arison, BH; Duncan, CA; Greber, T; Olah, TV; Slaughter, DE; Vickers, S; Vyas, KP, 1998
)
0.3
" Pharmacokinetic studies of MDL 100,907 in rats and dogs show that the drug is well absorbed but undergoes extensive first-pass metabolism to an active metabolite (MDL 105,725)."( Investigation of the CNS penetration of a potent 5-HT2a receptor antagonist (MDL 100,907) and an active metabolite (MDL 105,725) using in vivo microdialysis sampling in the rat.
Heath, TG; Scott, DO, 1998
)
0.3
" cannot be utilised because of poor bioavailability due to its rapid metabolism in the liver and intestinal wall."( Influence of piperine on the pharmacokinetics of curcumin in animals and human volunteers.
Joseph, T; Joy, D; Majeed, M; Rajendran, R; Shoba, G; Srinivas, PS, 1998
)
0.3
" The results showed that huperzine A had high bioavailability and more selective inhibition on AChE activity in cortex and hippocampus."( Comparative studies of huperzine A, E2020, and tacrine on behavior and cholinesterase activities.
Cheng, DH; Tang, XC, 1998
)
0.3
" Thirdly, oral bioavailability has been achieved while maintaining selectivity and efficacy through the incorporation of progressively less basic P1 groups."( Thrombin inhibitor design.
Naylor-Olsen, AM; Sanderson, PE, 1998
)
0.3
" In mouse, rat, and monkey systems, SCH 66336 has excellent oral bioavailability and pharmacokinetic properties."( Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.
Bishop, WR; Bryant, MS; Catino, JJ; Chen, J; Dell, J; Doll, RJ; Ferrari, E; Girijavallabhan, VM; Korfmacher, WA; Lee, S; Lin, CC; Lipari, P; Liu, M; Malkowski, M; Mallams, AK; Nielsen, L; Njoroge, FG; Nomeir, AA; Prioli, N; Remiszewski, S; Sinha, D; Syed, J; Taveras, AG; Wang, L; Yaremko, B, 1998
)
0.3
" The relative bioavailability of repaglinide (AUC(tablet)/AUC(oral solution)) was 110% (95% CI, 103%-117%)."( Bioavailability of repaglinide, a novel antidiabetic agent, administered orally in tablet or solution form or intravenously in healthy male volunteers.
Hatorp, V; Oliver, S; Su, CA, 1998
)
0.3
" It was concluded that repaglinide is rapidly absorbed and eliminated in healthy subjects when administered orally or intravenously under fasting conditions, and that the total availability of repaglinide is similar in the tablet and oral solution formulations, though that the rate of absorption is slower for the tablet formulation."( Bioavailability of repaglinide, a novel antidiabetic agent, administered orally in tablet or solution form or intravenously in healthy male volunteers.
Hatorp, V; Oliver, S; Su, CA, 1998
)
0.3
"The objective of the study was to investigate the mechanisms behind increased bioavailability of an enzymatically stable thrombin inhibitor, inogatran, after coadministration with a trypsin inhibitor, aprotinin."( Inhibition of binding of an enzymatically stable thrombin inhibitor to lumenal proteases as an additional mechanism of intestinal absorption enhancement.
Lindfors, L; Sjöström, M; Ungell, AL, 1999
)
0.3
" There was a 5-fold increase in the bioavailability of inogatran in the presence of aprotinin."( Inhibition of binding of an enzymatically stable thrombin inhibitor to lumenal proteases as an additional mechanism of intestinal absorption enhancement.
Lindfors, L; Sjöström, M; Ungell, AL, 1999
)
0.3
" Limited oral bioavailability or excessive production costs have prevented these inhibitors from becoming new antihypertensive drugs."( Renin inhibition by substituted piperidines: a novel paradigm for the inhibition of monomeric aspartic proteinases?
Binggeli, A; Breu, V; Bur, D; Clozel, JP; D'Arcy, A; Dorn, A; Fischli, W; Grüninger, F; Güller, R; Hirth, G; M ller, M; Märki, H; Mathews, S; Oefner, C; Ridley, RG; Stadler, H; Vieira, E; Wilhelm, M; Winkler, F; Wostl, W, 1999
)
0.59
"The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none."( Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
Assié, MB; Bonnaud, B; Cosi, C; Funes, P; Jubault, N; Kleven, M; Koek, W; Vacher, B, 1999
)
0.3
" In the present study, SCH 66336, an orally bioavailable nonpeptide tricyclic farnesyltransferase inhibitor, was tested against a large variety of human tumors to define its preclinical activity profile, utilizing the human tumor cloning assay."( Activity of SCH 66336, a tricyclic farnesyltransferase inhibitor, against human tumor colony-forming units.
Bishop, WR; Izbicka, E; Lawrence, RA; Petit, T; Von Hoff, DD; Weitman, S, 1999
)
0.3
" The bioavailability of Z-300 was 52% after the oral administration of Z-300, 3 mg/kg."( Pharmacokinetics of a new histamine H2-receptor antagonist, Z-300, in rat and dog.
Furuta, S; Hirabayashi, N; Imamura, F; Ito, T; Kawamata, H; Matsuki, Y; Sano, H; Sugimoto, T; Suzuki, M, 1999
)
0.3
" The incorporation of fluorine was found to significantly reduce the pKa of the compounds, and this reduction of basicity was shown to have a dramatic, beneficial influence on oral absorption, although the effect on oral bioavailability could not always be accurately predicted."( Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles.
Beer, MS; Broughton, HB; Castro, JL; Cheng, SK; Collins, I; Goodacre, SC; Heald, A; Locker, KL; MacLeod, AM; Morrison, D; Moyes, CR; O'Connor, D; Pike, A; Rowley, M; Russell, MG; Sohal, B; Stanton, JA; Thomas, S; van Niel, MB; Verrier, H; Watt, AP, 1999
)
0.3
"Two studies were performed to characterize the influence of food on the bioavailability of the current formulation of ebastine tablets."( The effect of food on the bioavailability of ebastine.
Dorr, MB; Heald, DL; Huang, MY; Pentikis, HS,
)
0.13
" Central bioavailability was gauged indirectly by determining anticonvulsant activity in a mouse maximal electroshock (MES) assay."( 4-Hydroxy-1-[2-(4-hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidine: a novel, potent, and selective NR1/2B NMDA receptor antagonist.
Bigge, CF; Boxer, PA; Cai, SX; Coughenour, LL; Espitia, SA; Hawkinson, JE; Keana, JF; Konkoy, CS; Rock, DM; Tran, M; Weber, E; Whittemore, ER; Wise, LD; Woodward, RM; Zhou, ZL, 1999
)
0.3
"5-fold higher than in wild-type mice, suggesting increased bioavailability of SP."( Neutral endopeptidase (EC 3.4.24.11) terminates colitis by degrading substance P.
Barbara, G; Bunnett, NW; Collins, SM; Figini, M; Geppetti, P; Gerard, C; Gerard, N; Grady, EF; Qiu, B; Sturiale, S, 1999
)
0.3
" Nevertheless, one compound (13), PNU-103657, possessed oral bioavailability in rats approaching that of the structurally related NNRTI drug delavirdine which is currently on the market for the treatment of HIV infection."( Synthesis and structure-activity relationships of the (alkylamino)piperidine-containing BHAP class of non-nucleoside reverse transcriptase inhibitors: effect of 3-alkylpyridine ring substitution.
Adams, WJ; Friis, JM; Genin, MJ; Kopta, LA; May, PD; Olmsted, RA; Poel, TJ; Romero, DL; Thomas, RC; Voorman, RL; Yagi, Y, 1999
)
0.3
" Pharmacokinetic studies demonstrated that BX 471 was orally active with a bioavailability of 60% in dogs."( Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1.
Bauman, JG; Buckman, B; Dunning, L; Ghannam, A; Harvey, S; Hesselgesser, J; Ho, E; Islam, I; Liang, M; Mallari, C; May, K; Monahan, S; Morrissey, MM; Ng, HP; Oanh, H; Perez, HD; Rosser, M; Shaw, K; Shen, J; Snider, RM; Subramanyam, B; Taub, D; Vergona, R; Wei, GP; Xu, W; Zhao, Z, 2000
)
0.31
" Preliminary pharmacokinetic studies conducted by us suggested the increased bioavailability of nimesulide co-administered with piperine."( Comparative anti-nociceptive, anti-inflammatory and toxicity profile of nimesulide vs nimesulide and piperine combination.
Bansal, P; Bhardwaj, RK; Gupta, SK; Velpandian, T, 2000
)
0.31
" Pyridinyloxazole 11 showed a promising in vivo profile with bioavailability of 64% and ED50 in rat collagen induced arthritis of 10 mg/kg po bid."( SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.
Buhl, T; Di Padova, FE; Feifel, R; Gram, H; Hiestand, P; Manning, U; Revesz, L; Zimmerlin, AG, 2000
)
0.31
"1% when administered intravenously at 30 microg/kg to the chronically hypoxic rats and had an apparent oral bioavailability of about 19."( 4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Adachi, H; Ishibashi, K; Ishihara, H; Kabasawa, Y; Kakiki, M; Kodama, K; Matsukura, M; Miyazaki, K; Nishino, M; Ozaki, H; Takase, Y; Watanabe, N, 2000
)
0.31
" Thus few novel analogues as CYP inactivators have been synthesized which may have important consequences in pharmacokinetics and bioavailability of drugs."( Structure-activity relationship of piperine and its synthetic analogues for their inhibitory potentials of rat hepatic microsomal constitutive and inducible cytochrome P450 activities.
Dhar, KL; Jamwal, DS; Koul, JL; Koul, S; Reen, RK; Singh, J; Singh, K; Taneja, SC, 2000
)
0.31
" Oral bioavailability in rodents is in the region of 20%."( Flavopiridol, the first cyclin-dependent kinase inhibitor to enter the clinic: current status.
Kelland, LR, 2000
)
0.31
" The ability of halofuginone to interfere with key events in neovascularization, together with its oral bioavailability and safe use as an anti-parasitic agent, make it a promising drug for further evaluation in the treatment of a wide range of diseases associated with pathological angiogenesis."( Halofuginone: a potent inhibitor of critical steps in angiogenesis progression.
Aingorn, E; Dou, HL; Elkin, M; Hemo, I; Miao, HQ; Nagler, A; Pines, M; Reich, R; Vlodavsky, I, 2000
)
0.31
"2nM), selective (>800 fold over h5-HT2C and hD2 receptors) antagonist at the h5-HT2A receptor with oral bioavailability in rats."( 3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
Bourrain, S; Crawforth, J; Goodacre, S; Herbert, R; Hutson, P; Marwood, R; Maxey, R; O'Connor, D; Patel, S; Rowley, M, 2000
)
0.31
" We developed a series of ACAT inhibitors that preferentially inhibited macrophage ACAT relative to hepatic or intestinal ACAT based on in vitro assays and ex vivo bioavailability studies."( Preferential pharmacological inhibition of macrophage ACAT increases plaque formation in mouse and rabbit models of atherogenesis.
Bellamy, F; Binet, J; Edgar, AD; Guffroy, C; Laugel, T; Legendre, C; Matsukura, T; Matsuura, A; Ohbayashi, S; Ortuno, JC; Padovani, P; Perrey, S; Tanaka, T, 2001
)
0.31
" Improvements could be made to oral bioavailability in this series by reduction of the pK(a) of the basic nitrogen, by adding a fluorine atom to the piperidine ring, leading to 3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole (17)."( 3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Castro, JL; Crawforth, J; Goodacre, S; Hallett, DJ; Hitzel, L; Hutson, PH; MacLeod, AM; Marwood, R; Moyes, C; O'Connor, D; Patel, S; Rowley, M; Sparey, TJ; Szeto, N; Thomas, S, 2001
)
0.31
" Piperine (1) is an alkaloidal constituent of black and long peppers recently established as a bioavailability enhancer of drugs and other substances."( Antidiarrhoeal activity of piperine in mice.
Bajad, S; Bedi, KL; Johri, RK; Singla, AK, 2001
)
0.31
" Clinical trials are now required, but are hindered by a paucity of cannabinoids of suitable bioavailability and therapeutic ratio."( Cannabinoids and pain.
Rice, AS, 2001
)
0.31
" Compound 1, which has good oral bioavailability in rats, dogs, and monkeys, is proposed as a potential therapeutic agent for the treatment of HIV-1 and has entered human clinical trials."( Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
Baroudy, BM; Clader, JW; Cox, K; Endres, M; Greenlee, WJ; Palani, A; Shapiro, S; Strizki, J, 2001
)
0.31
" Of these, 35, which showed the highest oral bioavailability in vivo in rats, was resolved into its two isomers 36 and 37."( Improvement in the selectivity and metabolic stability of the serotonin 5-HT(1A) ligand, S 15535: a series of cis- and trans-2-(arylcycloalkylamine) 1-indanols.
Bertrand, M; Charlot, V; Dekeyne, A; Despaux, N; Genissel, P; Giraud, H; Goument, B; Millan, MJ; Newman-Tancredi, A; Nisole, C; Peglion, JL, 2002
)
0.31
" Bioavailability lacking in the parent, 1-(2-(2,4-difluorophenyl)ethyl)-4-(phenylsulfonyl)piperidine (12), was introduced by using stability toward rat liver microsomes as a predictor of bioavailability."( 4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Bentley, G; Blurton, P; Bristow, LJ; Burkamp, F; Castro, JL; Chapman, K; Cheng, SK; Clarkson, R; Cook, GP; Fletcher, SR; Hutson, PH; MacLeod, AM; Marwood, R; O'Connor, D; Patel, S; Shepheard, S; Spinks, D; Tudge, M; van Niel, MB, 2002
)
0.65
"4) and good oral bioavailability in rat and dog (> 80 and > 50%, respectively)."( Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.
Curwen, JO; Dukes, M; Hennequin, LF; Johnstone, C; Kendrew, J; Ogilvie, DJ; Plé, PA; Stokes, ES; Thomas, AP; Wedge, SR, 2002
)
0.31
" The best compound in this series was sulfamoylacetic acid derivative (YM-60828) which was a potent, selective and orally bioavailable FXa inhibitor and was chosen for clinical development."( The discovery of YM-60828: a potent, selective and orally-bioavailable factor Xa inhibitor.
Hirayama, F; Hisamichi, N; Katayama, N; Kawasaki, T; Koshio, H; Kurihara, H; Matsumoto, Y; Sakai-Moritani, Y; Sato, K; Taniuchi, Y; Yanagisawa, I, 2002
)
0.31
" It may be less well absorbed and/or less effective than Clozaril, although evidence is conflicting."( Advances in atypical antipsychotics for the treatment of schizophrenia: new formulations and new agents.
Albert, MJ; Baldessarini, RJ; Centorrino, F; Kelleher, JP, 2002
)
0.31
"Piperine, a major alkaloid of black and long peppers has been reported to act as bioavailability enhancer of several drugs by inhibiting drug metabolising enzymes and/or by increasing oral absorption."( Simple high-performance liquid chromatography method for the simultaneous determination of ketoconazole and piperine in rat plasma and hepatocyte culture.
Bajad, S; Bedi, KL; Johri, RK; Singh, J; Singh, K, 2002
)
0.31
"We previously reported the discovery of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1'-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4'-methyl-1,4'-bipiperidine N-oxide 1 (SCH 351125) as an orally bioavailable human CCR5 antagonist for the treatment of HIV-1 infection."( Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.
Bara, T; Baroudy, BM; Clader, JW; Cox, K; Greenlee, WJ; Josien, H; Palani, A; Shapiro, S; Strizki, JM, 2002
)
0.31
" Notably, these compounds show a high bioavailability and a remarkable preference for the brain vs."( AF150(S) and AF267B: M1 muscarinic agonists as innovative therapies for Alzheimer's disease.
Bar-Ner, RH; Brandeis, R; Fisher, A; Kliger-Spatz, M; Marcovitch, I; Natan, N; Pittel, Z; Sonego, H,
)
0.13
"Different experimental formulations based on aqueous and oily systems, water miscible solvents, and solid dispersions were investigated for their potential to increase the oral bioavailability (F) of two novel piperidine renin inhibitors (Ro-X1: (R)-1-methoxy-3-[(3S,4R,5R)-4-[4-[3-(2-methoxy-benzyloxy)-propoxy]-phenyl]- 5-(4-methoxy-naphthalen-2-ylmethoxy)-piperidin-3-yloxy]-propan-2-ol; Ro-X2: (R)-3-[(3S,4R,5R)-4-[4-[3-(2-methoxy-benzyloxy)-propoxy]-phenyl]-5-(4- methoxy-naphthalen-2-ylmethoxy)-piperidin-3-ylmethoxy]-propane-1,2-diol) in dogs compared to their administration as acidic aqueous solution."( Preformulation approaches to improve the oral bioavailability of two novel piperidine renin inhibitors in dog.
Bittner, B; Chou, R; Lavé, T; Morgenroth, B; Schleimer, M; Zell, M, 2002
)
0.31
"Orally administered astemizole is well absorbed but undergoes an extensive first-pass metabolism to O-desmethylastemizole."( Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole.
Hirama, T; Matsubara, T; Matsumoto, S; Nagata, K; Yamazoe, Y, 2002
)
0.31
" The 4-aminopentamethylpiperidine naphthyridinone 5, which was designed to block metabolism at major 'hot spots', combined excellent inhibitory potency with good oral bioavailability in the rat."( p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.
Doherty, JB; Hop, CE; Hunt, JA; Ita, I; Kallashi, F; Kumar, S; McCormick, SX; O'Keefe, SJ; O'Neill, EA; Pivnichny, JV; Porter, G; Ruzek, RD; Sinclair, PJ; Thompson, JE; Wang, Z; Woods, A; Zaller, DM, 2003
)
0.32
" enhanced bioavailability of beta lactam antibiotics, amoxycillin trihydrate and cefotaxime sodium significantly in rats."( Effect of co-administration of piperine on pharmacokinetics of beta-lactam antibiotics in rats.
Dhuley, JN; Hiwale, AR; Naik, SR, 2002
)
0.31
" A series of potent and orally bioavailable CCR5 antagonists containing symmetrical 2,6-dimethyl isonicotinamides and 2, 6-dimethyl pyrimidines amides were generated with enhanced affinity for the CCR5 receptor."( Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.
Baroudy, BM; Clader, JW; Cox, K; Greenlee, WJ; McCombie, S; Palani, A; Shapiro, S; Strizki, J; Vice, S, 2003
)
0.32
" The discovery process of new chemical leads for an orally bioavailable inhibitor of human inducible NOS (iNOS) is reported."( Design and synthesis of inhibitors of inducible nitric oxide synthase. Discovery of a new chemical lead with potential for oral bioavailability.
Fujii, A; Hirai, K; Hisaichi, K; Kawanaka, Y; Kobayashi, K; Komeno, M; Kusuda, S; Murota, M; Naka, M; Nakai, H; Nishiyama, T; Tatsumi, T; Toda, M, 2003
)
0.32
"The method is sensitive, simple and rapid, so, it can meet the need of the studies on the pharmacokinetics and bioavailability of donepezil."( [Determination of donepezil in human plasma by HPLC-MS].
Chi, YM; Li, W; Lu, YH; Wen, HM; Zhang, ZX, 2003
)
0.32
"Potential of piperine, an active alkaloid of black and long peppers, to increase the bioavailability of drugs in humans is of great clinical significance owing to its omnipresence in food."( Characterization of a new rat urinary metabolite of piperine by LC/NMR/MS studies.
Bajad, S; Bedi, KL; Coumar, M; Khajuria, R; Suri, OP, 2003
)
0.32
" The relative bioavailability of the donepezil capsule was 102% +/- 11%."( [Bioequivalence of donepezil capsule and tablet in human].
Bian, XJ; Ding, L; Hao, XY; Li, LM; Zhang, SQ, 2003
)
0.32
" Pempidine is well absorbed from the gastro-intestinal tract as judged by (a) the low ratio (6."( Pharmacological properties of pempidine (1:2:2:6:6-pentamethylpiperidine), a new ganglion-blocking compound.
CORNE, SJ; EDGE, ND, 1958
)
0.24
" All were well absorbed when administered orally."( The pharmacological actions of pempidine and its ethyl homologue.
DUNLOP, D; FARRINGTON, JA; SPINKS, A; YOUNG, EH, 1958
)
0.24
"In this population of healthy mate volunteers, results showed the bioavailability of loratadine and ambroxol from the new formulation and did not show impairment of absorption when the drugs were formulated in a combination tablet."( Pharmacokinetic properties of single-dose loratadine and ambroxol alone and combined in tablet formulations in healthy men.
Alcántar, F; Herrera, J; Morales, JM; Rodríguez, JM; Rosete, R; Villacampa, J, 2003
)
0.32
" Although SR 140 333 increased the absorption rate from the jejunum in animals infused intra-arterially with 5-HT, 5-HT itself did not cause a significant reduction in absorption."( Effects of tachykinins and 5-hydroxytryptamine on intestinal secretion.
Coupar, IM; Di Iulio, JL, 2003
)
0.32
"Arzoxifene (ARZ) is a selective estrogen receptor (ER) modulator with greater bioavailability than raloxifene which is being developed as treatment for breast cancer."( Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model.
A'Hern, R; Detre, S; Dowsett, M; Johnston, SR; Riddler, S; Salter, J, 2003
)
0.32
" Donepezil is well absorbed orally, unaffected by food or by time of administration; it reaches therapeutic levels in doses of 5-10 mg/day and peak plasma concentrations are obtained 3-4 h after oral administration."( Donepezil: a clinical review of current and emerging indications.
Rogers, SJ; Román, GC, 2004
)
0.32
"Anthranilamide analogues such as 23 are potent and highly selective muscarinic M2 antagonists that also show good oral bioavailability and in vivo activity."( Muscarinic M2 antagonists: anthranilamide derivatives with exceptional selectivity and in vivo activity.
Billard, W; Binch, H; Chen, LY; Clader, JW; Crosby, G; Duffy, RA; Ford, J; Greenlee, WJ; Kozlowski, JA; Lachowicz, JE; Li, S; Liu, C; McCombie, SW; Vice, S; Zhou, G, 2004
)
0.32
" This compound is a potent CCR5 antagonist showing good in vitro antiviral activity against HIV-1, an excellent selectivity profile, and good oral bioavailability in three animal species."( Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Carella, A; Carver, G; Chapman, KT; Danzeisen, R; DeMartino, JA; Emini, EA; Gould, SL; Hale, JJ; Hazuda, D; Holmes, K; Kessler, J; Kwei, GY; Lineberger, J; Lynch, CL; Lyons, K; Malkowitz, L; Miller, MD; Mills, SG; Pivnichny, JV; Schleif, WA; Shah, S; Shen, DM; Shu, M; Siciliano, SJ; Springer, MS; Willoughby, CA, 2004
)
0.32
" Limited oral bioavailability of AC-90179 likely reflects rapid metabolism rather than poor absorption."( Pharmacological characterization of AC-90179 [2-(4-methoxyphenyl)-N-(4-methyl-benzyl)-N-(1-methyl-piperidin-4-yl)-acetamide hydrochloride]: a selective serotonin 2A receptor inverse agonist.
Andersson, CM; Bradley, SR; Brann, MR; Davis, RE; Hacksell, U; Harvey, SC; Kold, H; Makhay, M; Son, T; Spalding, TA; Tolf, BR; Vanover, KE; Veinbergs, I; Weiner, DM, 2004
)
0.32
" We have developed orally bioavailable pyridazinyl oxime ethers that are as potent as pirodavir."( In vitro activity of expanded-spectrum pyridazinyl oxime ethers related to pirodavir: novel capsid-binding inhibitors with potent antipicornavirus activity.
Barnard, DL; Hubbard, VD; Reece, PA; Sidwell, RW; Smee, DF; Tucker, SP; Watson, KG, 2004
)
0.32
" Optimization of the lead benzylic methyl compound 3 led to the methoxymethyl analogue 30, which had excellent receptor selectivity and oral bioavailability in rats and monkeys."( Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly sele
Baroudy, BM; Cox, K; Labroli, MA; Lachowicz, J; McCombie, SW; Nazareno, D; Steensma, RW; Strizki, JM; Tagat, JR; Varty, G; Watkins, R; Xiao, Y, 2004
)
0.32
" Previously, we reported the bioavailability of EGCG in rats (1."( Piperine enhances the bioavailability of the tea polyphenol (-)-epigallocatechin-3-gallate in mice.
Hong, J; Kim, DH; Lambert, JD; Mishin, VM; Yang, CS, 2004
)
0.32
" Agonistic 5-HT(1A) receptor activity was confirmed in vivo in the ultrasonic vocalization test, and the results suggest that the introduction of the carboxamide residue leads to better bioavailability than the corresponding methyl ether."( Indolebutylamines as selective 5-HT(1A) agonists.
Bartoszyk, GD; Böttcher, H; Greiner, HE; Heinrich, T; Seyfried, CA; Van Amsterdam, C, 2004
)
0.32
" These results suggest that YM598 has high selectivity for native human ETA against ETB receptors, and that YM598 is superior to atrasentan as an ETA receptor antagonist with regard to pharmacological bioavailability in rats."( Superiority of YM598 over atrasentan as a selective endothelin ETA receptor antagonist.
Fujimori, A; Fujiyasu, N; Miyata, K; Noguchi, Y; Ohtake, A; Sasamata, M; Sato, S; Sudoh, K; Ukai, M; Yuyama, H, 2004
)
0.32
" These data indicate that ET-1-induced vasoconstriction may be increased in the diabetic rat basilar artery, and that this hyper-reactivity to ET-1 may be due to an overproduction of ET-1, an up-regulation of ET(A)/ET(B) receptors, and a defect in the bioavailability of NO."( Mechanisms underlying enhanced contractile response to endothelin-1 in diabetic rat basilar artery.
Kamata, K; Kobayashi, T; Matsumoto, T; Yoshiyama, S, 2004
)
0.32
" In a pharmacokinetic experiment carried out in rats, 29 displayed an interesting profile, with a bioavailability of 49%."( Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands.
Bischoff, SF; Buhl, T; Floersheim, P; Fournier, B; Geiser, M; Halleux, C; Kallen, J; Keller, H; Ramage, P; Renaud, J, 2005
)
0.33
" The potency of 32 for mouse CCR3 (chemotaxis IC(50) = 41 nM) and its oral bioavailability in mice (20% F ) were adequate to assess the efficacy in animal models of allergic airway inflammation."( Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
Covington, M; Das, AM; Davies, P; De Lucca, GV; Decicco, CP; Duncia, JV; Emmett, G; Gardner, DS; Graden, DM; Kim, UT; Ko, SS; Liauw, A; Newton, RC; Santella, JB; Solomon, KA; Stowell, NC; Trainor, GL; Vargo, BJ; Wacker, DA; Wadman, EA; Wang, Z; Welch, PK; Yeleswaram, S; Zheng, C, 2005
)
0.33
" X-ray structure driven template modification and exchange of the benzamidine to optimize potency and pharmacokinetic properties gave selective, potent and orally bioavailable 4-(3-aminomethyl phenyl)piperidinyl-1-amides."( Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Aldous, S; Astles, P; Cairns, J; Czekaj, M; Davidson, J; Dupuy, A; Eastwood, P; Engers, D; Fenton, G; Gardyan, M; Giardino, O; Guilloteau, JP; Harrison, T; Houille, O; Kwong, J; Levell, J; Liang, G; Lim, HK; Luo, Y; Maignan, S; Mathew, R; McCarthy, C; Merriman, G; Morley, A; Pauls, H; Pribish, J; Rebello, S; Romano, J; Shen, L; Sides, K; Smith, K; Tsay, J; Wang, J; Watson, S; Whiteley, B, 2005
)
0.33
" In particular, one analog (74, DPP-IV IC50=26 nM) exhibited good oral bioavailability and acceptable half-life in the rat, albeit with rather high clearance."( Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.
Ashton, WT; Dong, H; Doss, GA; He, H; Leiting, B; Lyons, KA; Marsilio, F; Patel, RA; Sisco, RM; Thornberry, NA; Weber, AE; Wu, JK, 2005
)
0.57
" These results suggest that YM598 has a high selectivity for native human ETA receptors against ETB receptors, and that YM598 is superior to atrasentan as an ETA receptor antagonist, with regard to pharmacological bioavailability in rats."( Pharmacological characterization of YM598, a selective endothelin-A receptor antagonist.
Fujimori, A; Miyata, K; Noguchi, Y; Ohtake, A; Sasamata, M; Sato, S; Sudoh, K; Ukai, M; Yuyama, H, 2004
)
0.32
" ZD6474 is an orally bioavailable inhibitor of VEGF receptor-2 tyrosine kinase activity that in preclinical studies has been shown to inhibit both VEGF-induced signalling in endothelial cells and tumour-induced angiogenesis."( ZD6474--a novel inhibitor of VEGFR and EGFR tyrosine kinase activity.
Ryan, AJ; Wedge, SR, 2005
)
0.33
" The designed system, combining excellent buoyant ability and suitable drug release pattern, could possibly be advantageous in terms of increased bioavailability of repaglinide."( Calcium silicate based microspheres of repaglinide for gastroretentive floating drug delivery: preparation and in vitro characterization.
Agrawal, GP; Awasthi, AM; Jain, NK; Jain, SK, 2005
)
0.33
"SAR and DMPK studies led to the identification of substituted N-alkyl-N-[1-(3,3-diphenylpropyl)piperidin-4-yl]-2-phenylacetamides as potent and orally bioavailable ligands for the human CCR5 chemokine receptor."( Modulators of the human CCR5 receptor. Part 2: SAR of substituted 1-(3,3-diphenylpropyl)-piperidinyl phenylacetamides.
Cooper, AE; Cumming, JG; Grime, K; Logan, CJ; McLaughlin, S; Oldfield, J; Shaw, JS; Tucker, H; Whittaker, D; Winter, J, 2005
)
0.33
" 55 was highly active in several functional assays, showed excellent oral bioavailability in rat and monkey models, and showed complete inhibition of agonist-induced ex vivo platelet aggregation in cynomolgus monkeys after oral administration."( Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents.
Agans-Fantuzzi, J; Ahn, HS; Asberom, T; Boykow, G; Bryant, M; Chackalamannil, S; Chintala, M; Clasby, M; Czarniecki, M; Doller, D; Foster, C; Greenlee, WJ; Lau, J; Tsai, H; Xia, Y, 2005
)
0.33
"4-(1-Benzo[1,3]dioxol-5-ylmethylpiperidine-4-ylmethyl)-6-chlorochromen-2-one (7) is a potent, orally bioavailable melanin concentrating hormone receptor 1 (MCHr1) antagonist that causes dose-dependent weight loss in diet-induced obese mice."( Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Blackburn, C; Brodjian, S; Brown, J; Brune, M; Bush, E; Che, JL; Collins, CA; Cullis, C; Dayton, BD; Falls, D; Fey, T; Freeman, J; Fry, D; Gao, J; Geddes, B; Govek, E; Hernandez, L; Iyengar, R; Judd, AS; Knourek-Segel, V; Kym, PR; Lai, SJ; LaMarche, MJ; Lynch, JK; Marsh, K; Marsilje, T; McDowell, C; Mulhern, M; Patane, M; Preusser, LC; Reinhart, GA; Roses, J; Sells, T; Sham, HL; Shapiro, R; Souers, AJ; Vasudevan, A; Wodka, D; Zhao, G, 2005
)
0.33
" These additives increased intestinal permeability (P(app)) and absorption rate constant (K(a)) up to two and fourfold, respectively."( In situ and in vivo efficacy of peroral absorption enhancers in rats and correlation to in vitro mechanistic studies.
Chawla, HP; Panchagnula, R; Sharma, P; Varma, MV,
)
0.13
" The proposed method enables the unambiguous identification and quantification of lafutidine for pharmacokinetic, bioavailability or bioequivalence studies."( Simple, sensitive and rapid LC-ESI-MS method for the quantitation of lafutidine in human plasma--application to pharmacokinetic studies.
Chen, WD; Li, H; Liang, Y; Liu, XD; Wang, GJ; Xie, L; Xiong, Y, 2006
)
0.33
" Grapefruit juice increased the bioavailability of repaglinide, suggesting significant intestinal elimination of the drug which was assumed to be primarily mediated by CYP3A4 in the gut."( The impact of CYP2C8 polymorphism and grapefruit juice on the pharmacokinetics of repaglinide.
Bidstrup, TB; Brøsen, K; Damkier, P; Ekblom, M; Karlsson, A; Olsen, AK, 2006
)
0.33
" Oral bioavailability was low in rats (10%) but significantly higher in dogs (52%) and monkeys (26%)."( Preclinical pharmacokinetics and metabolism of a potent non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase.
Bishop, A; Bonelli, F; Di Marco, A; Fiore, F; Giuliano, C; Gonzalez-Paz, O; Harper, S; Laufer, R; Marcucci, I; Migliaccio, G; Monteagudo, E; Narjes, F; Pacini, B; Padron Velazquez, J; Rowley, M,
)
0.13
" The apparent absorption rate constant (ka) of [(14)C]bepotastine in the small intestine was greatly increased by cyclosporin A and verapamil, especially in the distal portion, and the site-specific absorption of [(14)C]bepotastine disappeared."( Effect of P-glycoprotein on intestinal absorption and brain penetration of antiallergic agent bepotastine besilate.
Fukuda, H; Kamikozawa, Y; Ohashi, R; Sugiura, M; Tamai, I; Yabuuchi, H, 2006
)
0.33
" One of these compounds, 13g, shows modest oral bioavailability in rats."( A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Askew, BC; Biddlecome, G; Biswas, K; Chen, JJ; D'Amico, DC; Fotsch, C; Groneberg, RD; Han, NB; Hsieh, FY; Johnson, E; Kamassah, A; Kumar, G; Lester-Zeiner, D; Liu, Q; Mareska, DA; Ng, G; Riahi, BB; Wang, YJ; Yang, K; Zhan, J; Zhu, J, 2006
)
0.33
"6% oral bioavailability in rats."( Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N'-(4-(2-methylpropyloxy)phenylmethyl) carbamide (2R,3R)-dihydroxybutanedioate (2:1) (ACP-103), a novel 5-hydroxytryptamine(2A) receptor inverse agonist.
Andersson, CM; Brann, MR; Burstein, ES; Davis, RE; Del Tredici, AL; Gardell, LR; Geyer, MA; Harvey, SC; Lameh, J; Makhay, M; Ott, TR; Piu, F; Powell, SB; Schiffer, HH; Schlienger, N; Son, TY; Thygesen, MB; Tolf, BR; Uldam, AK; Vanover, KE; Veinbergs, I; Weiner, DM, 2006
)
0.33
" These molecules also exhibit superior pharmacological and pharmacokinetic parameters, relative to all GlyT1 inhibitors of the spiropiperidine family, culminating in the identification of 16b with an oral bioavailability of approximately 60%."( 4-Substituted-8-(1-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with superior pharmacological and pharmacokinetic parameters.
Alberati, D; Hainzl, D; Jolidon, S; Kurt, A; Pinard, E; Thomas, AW; Zimmerli, D, 2006
)
0.33
" We attempted to replicate the effects previously reported with SNAP-7941 and expanded the investigation to three other orally bioavailable MCH-1 receptor antagonists with good brain penetration."( Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety.
Basso, AM; Bratcher, NA; Brune, ME; Collins, CA; Cowart, MD; Esbenshade, TA; Fox, GB; Gallagher, KB; Hancock, AA; Iyengar, R; Kym, PR; Rueter, LE; Schmidt, M; Souers, AJ; Sun, M; Vasudevan, A; Zhao, C, 2006
)
0.33
"Piperine, the active principle of Piper longum, Piper nigrum and Zingiber officinalis, has been reported to enhance the oral bioavailability of phenytoin in human volunteers."( Effect of piperine on the steady-state pharmacokinetics of phenytoin in patients with epilepsy.
Hota, D; Kharbanda, P; Pandhi, P; Pattanaik, S; Prabhakar, S, 2006
)
0.33
" Antagonist 26 was shown to have good oral bioavailability in rats."( Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Ayala, JM; Cascierri, MA; Maccoss, M; Marino, D; Mills, SG; Parsons, W; Pasternak, A; Vicario, PP; Yang, L, 2006
)
0.33
"To assess the single-dose absolute oral bioavailability of traxoprodil in healthy male volunteers phenotyped as either CYP2D6 extensive or poor metabolisers."( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers.
Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006
)
0.33
"In poor metabolisers (n = 6), oral bioavailability was approximately 80% and was consistent with a liver extraction ratio of approximately 20% (plasma clearance of approximately 4 mL/min/kg) indicating near complete absorption."( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers.
Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006
)
0.33
" In extensive metabolisers, the oral bioavailability was nonlinear and dose-dependent, while in poor metabolisers, oral bioavailability appeared to be linear and dose-independent."( Absolute oral bioavailability of traxoprodil in cytochrome P450 2D6 extensive and poor metabolisers.
Benincosa, LJ; Crownover, PH; Diringer, K; Gibbs, MA; Russell, T; Taylor, TJ; Venkatakrishnan, K; Wilner, K, 2006
)
0.33
"Alvimopan is a selective, competitive mu-opioid receptor antagonist with limited oral bioavailability which may be used to reduce length of post-operative ileus."( Meta-analysis: Alvimopan vs. placebo in the treatment of post-operative ileus.
Cornish, J; Darzi, AW; Tan, EK; Tekkis, PP, 2007
)
0.34
"A postoperative decrease in the gastric emptying (GE) rate may delay the early start of oral feeding and alter the bioavailability of orally administered drugs."( The effect of anesthetic technique on early postoperative gastric emptying: comparison of propofol-remifentanil and opioid-free sevoflurane anesthesia.
Lövqvist, A; Thörn, SE; Walldén, J; Wattwil, L; Wattwil, M, 2006
)
0.33
" However, in cats by intraduodenal administration and in mice by oral administration its duration of action was much longer and its functional bioavailability much higher than of the other two drugs."( Silperisone: a centrally acting muscle relaxant.
Farkas, S,
)
0.13
" The meal-related timing of administration of glinides and the potential influence of food and meal composition on their bioavailability may be important."( Drug-drug and food-drug pharmacokinetic interactions with new insulinotropic agents repaglinide and nateglinide.
Scheen, AJ, 2007
)
0.34
"Lonafarnib is an orally bioavailable nonpetidomimetic farnesyl transferase inhibitor with significant activity against BCR-ABL-positive cell lines and primary human chronic myeloid leukemia (CML) cells."( Phase 1 study of lonafarnib (SCH 66336) and imatinib mesylate in patients with chronic myeloid leukemia who have failed prior single-agent therapy with imatinib.
Cortes, J; Daley, GQ; Ferrajoli, A; Jabbour, E; Kantarjian, H; Koller, C; O'Brien, S; Statkevich, P; Verstovsek, S; Zhu, Y, 2007
)
0.34
"Lonafarnib is an orally bioavailable farnesyltransferase inhibitor."( Enhancement of the antitumor activity of tamoxifen and anastrozole by the farnesyltransferase inhibitor lonafarnib (SCH66336).
Basso, AD; Black, S; Kirschmeier, P; Liu, G; Liu, M; Long, BJ; Marrinan, CH; Robert Bishop, W; Taylor, SA, 2007
)
0.34
" The MCH1 receptor antagonists 5m and (S)-6b show reasonable pharmacokinetic profiles (rat bioavailability = 48 and 81%, respectively)."( Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Andersen, K; Chen, CA; Craig, DA; Daniewska, I; De Leon, J; Forray, C; Hegde, LG; Jiang, Y; Kong, R; Li, B; Lu, K; Marzabadi, MR; Wetzel, JM; Wolinsky, TD, 2007
)
0.34
" There are indications that piperine inhibits, rather than stimulates, drug metabolism in most cases, thus increasing the bioavailability and effect of some drugs."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.34
"This pilot study provided evidence for enhanced bioavailability of nevirapine when administered with piperine."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.34
"The objective was to determine whether food affects the pharmacokinetics and safety of lonafanib, an orally bioavailable farnesyl transferase inhibitor that is under clinical evaluation for the treatment of various hematologic malignancies and solid tumors."( Effect of food on the pharmacokinetics of lonafarnib (SCH 66336) following single and multiple doses.
Cutler, DL; Statkevich, P; Zhu, Y, 2007
)
0.34
" Piperine has been documented to enhance the bioavailability of a number of therapeutic drugs as well as phytochemicals by this very property."( Black pepper and its pungent principle-piperine: a review of diverse physiological effects.
Srinivasan, K, 2007
)
0.34
"Previously, we identified cyclohexane diamine derivative 1 as orally bioavailable factor Xa inhibitor."( Design, synthesis, and biological activity of piperidine diamine derivatives as factor Xa inhibitor.
Mochizuki, A; Naito, H; Nakamoto, Y; Ohta, T; Uoto, K, 2008
)
0.35
" Computational chemistry was employed to analyze the three-dimensional geometries of these dispirotriheterocycles, as well as to generate chemoinformatic bioavailability data."( Design and synthesis of propeller-shaped dispiroisoxazolinopiperidinochromanones.
Carpenter, RD; DeBerdt, PB; Fettinger, JC; Holden, JB; Kurth, MJ; Milinkevich, KA; Min, T; Tantillo, DJ; Willenbring, D,
)
0.13
" The optimized formulation was evaluated for preclinical bioavailability and antihypertensive efficacy using albino rat model."( Transdermal therapeutic system of enalapril maleate using piperidine as penetration enhancer.
Ahmad, FJ; Ali, MM; Aqil, M; Chowdhary, I; Sultana, Y; Talegaonkar, S, 2008
)
0.35
"Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa."( Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.
Chang, CH; Cheney, DL; Corte, JR; Fang, T; Gauuan, JF; Hadden, M; Han, W; He, K; Hu, Z; Jiang, XJ; Knabb, RM; Lam, PY; Li, YL; Luettgen, JM; Morin, PE; Orton, D; Pinto, DJ; Rendina, AR; Wexler, RR; Wong, PC, 2008
)
0.35
" Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys was 45%, 86%, and 72% to 88%, respectively."( Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys.
Asakawa, T; Christopher, RJ; Kassel, DB; Lee, B; Shi, L; Takeuchi, K, 2008
)
0.35
" AUC(0-72h) or even AUC(0-48h), can be adequately used in assessing the relative bioavailability of long terminal half-life drugs."( The use of truncated area under the curves in the bioequivalence evaluation of long half-life drugs. Studies with donepezil and memantine.
Erkent, U; Koytchev, R, 2008
)
0.35
" Preliminary structure-activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors."( Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors.
Camp, HS; Cao, N; Collins, CA; Janis, RS; Liu, B; Liu, G; Liu, M; Nelson, LT; Serby, MD; Sham, HL; Smith, HT; Suhar, TS; Surowy, TK; Szczepankiewicz, BG; Xin, Z; Zhao, H, 2008
)
0.35
"The present study was designed to investigate the involvement of monoaminergic system(s) in the antidepressant activity of curcumin and the effect of piperine, a bioavailability enhancer, on the bioavailability and biological effects of curcumin."( Antidepressant activity of curcumin: involvement of serotonin and dopamine system.
Bhutani, MK; Bishnoi, M; Kulkarni, SK, 2008
)
0.35
" Compound 30 showed good oral bioavailability and brain penetration across species."( Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels.
Adarayan, ED; Ballard, JE; Barrow, JC; Bock, MG; Bunting, PB; Connolly, TM; DiLella, AG; Doran, SM; Fox, SV; Graufelds, VK; Hartman, GD; Koblan, KS; Kraus, RL; Kuo, Y; Lindsley, CW; Magee, MM; Marino, MJ; Nuss, CE; Prueksaritanont, T; Renger, JJ; Reynolds, IJ; Rittle, KE; Schlegel, KA; Shipe, WD; Shu, Y; Tang, C; Uebele, VN; Vargas, HM; Woltmann, RF; Yang, FV; Yang, ZQ; Zrada, MM, 2008
)
0.64
" ASP8497 exhibited good oral bioavailability with potent inhibition of plasma DPP-IV activity."( Evaluation of the antidiabetic effects of dipeptidyl peptidase-IV inhibitor ASP8497 in streptozotocin-nicotinamide-induced mildly diabetic mice.
Hayakawa, M; Matsuyama-Yokono, A; Nakano, R; Shibasaki, M; Someya, Y; Tahara, A, 2009
)
0.35
" Piperine could significantly enhance the oral bioavailability of carbamazepine, possibly by decreasing the elimination and/or by increasing its absorption."( Pharmacokinetic interaction of single dose of piperine with steady-state carbamazepine in epilepsy patients.
Hota, D; Kharbanda, P; Pandhi, P; Pattanaik, S; Prabhakar, S, 2009
)
0.35
" The in vivo pharmacokinetics revealed that curcumin entrapped nanoparticles demonstrate at least 9-fold increase in oral bioavailability when compared to curcumin administered with piperine as absorption enhancer."( Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer.
Ankola, DD; Beniwal, V; Kumar, MN; Shaikh, J; Singh, D, 2009
)
0.35
" Here, we report the results of a preliminary pharmacokinetic study of masitinib in cats which showed a good bioavailability of ~60% in both sexes."( Pharmacokinetics of masitinib in cats.
Bader, T; Bellamy, F; Hermine, O; Moussy, A, 2009
)
0.35
"Masitinib is a potent and selective tyrosine kinase inhibitor targeting KIT that is active, orally bioavailable in vivo, and has low toxicity."( Masitinib (AB1010), a potent and selective tyrosine kinase inhibitor targeting KIT.
Arock, M; Auclair, C; Borge, L; Castéran, N; Ciufolini, M; Dubreuil, P; Gros, L; Hajem, B; Hermine, O; Humbert, M; Lermet, A; Letard, S; Leventhal, PS; Mansfield, CD; Moussy, A; Sippl, W; Voisset, E, 2009
)
0.35
"001), with an enormous reduction in the oral bioavailability of ebastine and significantly reduced histamine-induced skin reactions."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
0.36
"We have recently discovered imidazo[1,5-c]imidazol-3-one derivative 1 as a potent, selective, and orally bioavailable factor Xa (FXa) inhibitor."( Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.
Fujimoto, T; Kawamura, M; Konishi, N; Kubo, K; Tada, N; Takagi, T; Tobisu, M, 2009
)
0.35
" In addition, this compound exhibited good oral bioavailability and demonstrated plasma triglyceride lowering effects in Zucker fatty rats in a dose-dependent manner after a 7-day oral administration (qd)."( Novel benzoylpiperidine-based stearoyl-CoA desaturase-1 inhibitors: Identification of 6-[4-(2-methylbenzoyl)piperidin-1-yl]pyridazine-3-carboxylic acid (2-hydroxy-2-pyridin-3-ylethyl)amide and its plasma triglyceride-lowering effects in Zucker fatty rats.
Deguchi, T; Kiyotsuka, Y; Konishi, M; Kurata, H; Kurikawa, N; Miyazawa, Y; Ogata, T; Ohsumi, J; Okuyama, R; Takagi, T; Ueno, Y; Uto, Y; Wakimoto, S; Watanabe, N, 2010
)
0.36
" Variation of the linker group between the piperidine and the lipophilic substituent identified 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as potent and orally bioavailable inhibitors of PKB."( Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).
Aherne, GW; Caldwell, JJ; Cheung, KM; Collins, I; Davies, TG; de Haven Brandon, A; Eccles, SA; Fazal, L; Garrett, MD; Henley, A; Hunter, LJ; McHardy, T; Raynaud, FI; Rowlands, M; Ruddle, R; Seavers, L; Taylor, K; Valenti, M, 2010
)
0.36
" The oral bioavailability of BMS-690514 was 78% in mice, approximately 100% in rats, 8% in monkeys, and 29% in dogs."( Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2.
Christopher, L; Gavai, A; Marathe, P; Rodrigues, D; Sleczka, B; Tang, Y; Wong, T; Zhang, H, 2010
)
0.36
" Scanning electronic microscopy of the intestinal villi in these spice treatments revealed alterations in the ultrastructure, especially an increase in microvilli length and perimeter which would mean a beneficial increase in the absorptive surface of the small intestine, providing for an increased bioavailability of micronutrients."( Beneficial influence of dietary spices on the ultrastructure and fluidity of the intestinal brush border in rats.
Prakash, UN; Srinivasan, K, 2010
)
0.36
" The relative bioavailability of repaglinide from its liquisolid compact formula was found to be increased significantly in comparison to that of the marketed tablet."( Bioavailability and biological activity of liquisolid compact formula of repaglinide and its effect on glucose tolerance in rabbits.
Arafa, NM; El-Houssieny, BM; Wahman, L, 2010
)
0.36
" Overall, the results from these studies suggested that BMS-690514 was well absorbed and highly metabolized through multiple pathways in these preclinical species."( Metabolism and disposition of [14C]BMS-690514 after oral administration to rats, rabbits, and dogs.
Allentoff, A; Caceres-Cortes, J; Chando, T; Christopher, LJ; Ekhato, IV; Hong, H; Humphreys, WG; Iyer, RA; Roongta, V; Su, H; Sun, H, 2010
)
0.36
" SAR studies, driven primarily by in vitro liver microsomal stability assessment, identified compound 10b, which displayed improved oral bioavailability and lower intrinsic clearance."( The synthesis and biological evaluation of quinolyl-piperazinyl piperidines as potent serotonin 5-HT1A antagonists.
Abou-Gharbia, MA; Adedoyin, A; Andree, TH; Aschmies, SH; Asselin, M; Bach, AC; Beyer, C; Bicksler, JJ; Childers, WE; Chong, DC; Comery, TA; Day, M; Grauer, SM; Grosu, GT; Harrison, BL; Havran, LM; Hirst, WD; Hughes, ZA; Huselton, C; Kagan, N; Kleintop, T; Magolda, R; Marathias, V; Platt, B; Pulicicchio, C; Robichaud, AJ; Rosenzweig-Lipson, S; Sabb, AL; Shen, Z; Smith, DE; Sukoff-Rizzo, SJ; Sullivan, KM; Zhang, MY, 2010
)
0.6
" The marked effect of food on the bioavailability of blonanserin should be taken into account in its dosing schedules."( Effect of dose timing in relation to food intake on systemic exposure to blonanserin.
Inoue, Y; Kaneko, S; Saruwatari, J; Yasui-Furukori, N, 2010
)
0.36
" The bioavailability of fexofenadine was increased by approximately 2-folds via the concomitant use of piperine."( Effect of piperine, a major component of black pepper, on the intestinal absorption of fexofenadine and its implication on food-drug interaction.
Han, HK; Jin, MJ, 2010
)
0.36
" Piperine (20 mg/kg orally) was administered along with curcumin to enhance the bioavailability of the latter up to 20-fold more."( Antioxidant potential of curcumin against oxidative insult induced by pentylenetetrazol in epileptic rats.
Jyothy, A; Munshi, A; Nehru, B; Sharma, V, 2010
)
0.36
" Enhanced bioavailability of curcumin was evidenced when the same was orally administered concomitant with piperine."( Tissue distribution & elimination of capsaicin, piperine & curcumin following oral intake in rats.
Srinivasan, K; Suresh, D, 2010
)
0.36
"Considerable difference exists in the bioavailability of the three test compounds."( Tissue distribution & elimination of capsaicin, piperine & curcumin following oral intake in rats.
Srinivasan, K; Suresh, D, 2010
)
0.36
"A series of phenyl piperidine alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing of MMP-1 and MMP-14 (MT1-MMP) and exhibit oral bioavailability in rats."( Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
Becker, DP; Boehm, TL; Carroll, JN; DeCrescenzo, GA; Fletcher, TR; Hockerman, SL; Kolodziej, SA; McDonald, JJ; Mischke, DA; Munie, GE; Rico, JG; Stehle, NW; Swearingen, C, 2010
)
0.36
" Oral bioavailability was improved by using syringe feeding with donepezil but not galantamine."( Alternative method of oral dosing for rats.
Atcha, Z; Aw, CC; Browne, ER; Goh, CW; Lim, JS; Neo, AH; Pemberton, DJ; Rourke, C, 2010
)
0.36
"Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin subtype-4 receptor (MC4R) agonists are disclosed."( Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
Bakshi, RK; Ball, RG; Chen, AS; Chen, HY; Dellureficio, JP; Dobbelaar, PH; Fong, TM; Guo, L; He, S; Hong, Q; Jian, T; Liu, J; MacIntyre, DE; MacNeil, T; Martin, WJ; Nargund, RP; Peng, Q; Sebhat, IK; Strack, AM; Tamvakopoulos, C; Tang, R; Tsou, NN; Weinberg, DH; Wyvratt, MJ; Ye, Z, 2010
)
0.36
" In summary, BMS-690514 was well absorbed and extensively metabolized via multiple metabolic pathways in humans, with excretion of drug-related radioactivity in both bile and urine."( Metabolism and disposition of [14C]BMS-690514, an ErbB/vascular endothelial growth factor receptor inhibitor, after oral administration to humans.
Allentoff, A; Christopher, LJ; Clemens, PL; Harbison, CT; Heller, K; Hong, H; Humphreys, WG; Iyer, RA; Roongta, V; Su, H; Sun, H; Vakkalagadda, BJ; Wong, T; Zhang, S, 2010
)
0.36
" Thus, it was concluded that DH ODTs with masked taste were obtained by Eudragit EPO-based microspheres, drug loaded microspheres neither decreased the bioavailability nor delayed the release of DH."( Preparation and evaluation of taste-masked donepezil hydrochloride orally disintegrating tablets.
Choi, HG; Kang, JH; Woo, JS; Yan, YD; Yong, CS, 2010
)
0.36
" Systemic bioavailability was 22."( Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone.
Amer, AM; Atef, M; El-Gendi, AY; Kamel, GM, 2010
)
0.36
"Repaglinide (RPG) is an oral hypoglycemic agent with excellent bioavailability (90-98%) and a short plasma half-life (2-6 h)."( Repaglinide-loaded long-circulating biodegradable nanoparticles: rational approach for the management of type 2 diabetes mellitus.
Jain, S; Saraf, S, 2009
)
0.35
" A two-compartment population pharmacokinetic model estimating oral clearance, between-patient variability in oral clearance, central volume of distribution, and residual variability in combination with historical estimates of first-order absorption rate constant, intercompartmental clearance, and peripheral volume of distribution adequately described the sparse MPA data."( Population pharmacokinetic analysis of mycophenolic acid coadministered with either tasocitinib (CP-690,550) or tacrolimus in adult renal allograft recipients.
Busque, S; Chan, G; Krishnaswami, S; Lamba, M; Melcher, M; Tafti, B, 2010
)
0.36
" One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat."( Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.
Horiguchi, M; Kimura, H; Masui, Y; Nakagawa, T; Nakahira, H; Nishio, Y; Ono, M; Sakai, M; Sugaru, E; Tosaki, S, 2010
)
0.36
" MNP001 exhibited a rapid absorption, broad distribution, slow systemic clearance and a low but pharmacologically relevant oral bioavailability in rats."( Preclinical pharmacokinetics and metabolism of MNP001, a piperidine analog of 3-carbamyl compounds.
Fox, LM; Wang, D; Xia, B, 2011
)
0.37
" Pharmacokinetic studies have determined that iloperidone is well absorbed orally, with a bioavailability of 96%."( Iloperidone: A new drug for the treatment of schizophrenia.
Arif, SA; Mitchell, MM, 2011
)
0.37
" Analog 20q displayed both good DPP-4 potency and selectivity against other proteases, while derivative 20k displayed long half life and modest oral bioavailability in rat."( Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.
Ashton, W; Caldwell, CG; Chen, P; He, H; Lyons, KA; Thornberry, NA; Weber, AE; Wu, JK, 2011
)
0.57
" Etoposide presents low bioavailability with wide inter-, and intra-patient variability after oral dosing."( Involvement of P-glycoprotein and CYP 3A4 in the enhancement of etoposide bioavailability by a piperine analogue.
Gupta, PN; Javed, S; Johri, RK; Koul, S; Najar, IA; Sharma, SC; Singh, GD, 2011
)
0.37
"P-glycoprotein (Pgp or ABCB1) is an ABC transporter protein involved in intestinal absorption, drug metabolism, and brain penetration, and its inhibition can seriously alter a drug's bioavailability and safety."( A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.
Broccatelli, F; Carosati, E; Cruciani, G; Frosini, M; Goracci, L; Neri, A; Oprea, TI, 2011
)
0.37
" A liquid chromatography-tandem mass spectrometry method was applied to determine the oral bioavailability of ethyl piperate."( Contribution of carboxylesterase in hamster to the intestinal first-pass loss and low bioavailability of ethyl piperate, an effective lipid-lowering drug candidate.
Bao, N; Borjihan, G; Hu, M; Jia, J; Li, S; Lu, Y; Ma, Y; Wang, Y; Yang, D; Yu, C, 2011
)
0.37
"25 and the relative bioavailability of the test formulation was 96."( Bioequivalence study of two tablet formulations containing rimonabant 20 mg in healthy Indian subjects.
Bhaumik, U; Chakrabarty, US; Das, A; Nandi, U; Pal, TK, 2011
)
0.37
"There is currently a need for a better understanding of the mechanisms of food-drug interaction as well as the clinical implication to maximize the effectiveness and applicability of black pepper or its active component, piperine, as a bioavailability enhancer in the clinical arena."( The effects of black pepper on the intestinal absorption and hepatic metabolism of drugs.
Han, HK, 2011
)
0.37
" The information provided is used to assess the clinical significance of black pepper and piperine and optimize their effectiveness as a bioavailability enhancer."( The effects of black pepper on the intestinal absorption and hepatic metabolism of drugs.
Han, HK, 2011
)
0.37
" Furthermore, the effective formulation strategy for the optimization of the pharmacokinetic characteristics of dietary components is crucial to improve their in vivo performance and ultimately maximize their effectiveness as a bioavailability enhancer."( The effects of black pepper on the intestinal absorption and hepatic metabolism of drugs.
Han, HK, 2011
)
0.37
" Vandetanib reduces constitutive NO production and increases blood pressure, yet flow-stimulated NO bioavailability was preserved."( Contrary effects of the receptor tyrosine kinase inhibitor vandetanib on constitutive and flow-stimulated nitric oxide elaboration in humans.
Beckman, JA; Burstein, HJ; Dallabrida, SM; Hannagan, K; Ismail, NS; Mayer, EL; Redline, WM; Rupnick, MA, 2011
)
0.37
" Solid lipid nanoparticles were prepared by modified solvent injection method for oral delivery to improve the bioavailability of RG, an antidiabetic drug."( Studies on binary lipid matrix based solid lipid nanoparticles of repaglinide: in vitro and in vivo evaluation.
Jain, A; Rawat, MK; Singh, S, 2011
)
0.37
"The purpose of this work was to develop prolonged release binary lipid matrix-based solid lipid nanoparticles (SLN) of repaglinide (RG) for oral intestinal delivery and to improve the bioavailability of RG."( In vivo and cytotoxicity evaluation of repaglinide-loaded binary solid lipid nanoparticles after oral administration to rats.
Jain, A; Rawat, MK; Singh, S, 2011
)
0.37
" Further fine-tuning of the substituent pattern in the sulfonamide paved the way to enhancing potency and bioavailability and minimizing hERG inhibition, resulting in discovery of clinical compound 122 (GSK163929)."( Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.
Anderson, DL; Aquino, C; Chauder, BA; Duan, M; Ferris, R; Kazmierski, WM; Kenakin, T; Koble, CS; Lang, DG; McIntyre, MS; Peckham, J; Spaltenstein, A; Svolto, A; Watson, C; Wheelan, P; Wire, MB; Youngman, M, 2011
)
0.37
" The initial absence of oral bioavailability was successfully tackled by moving the basic nitrogen of the spiro-4-piperidyl moiety towards the electron-deficient pyrrolepyridinedione core, thereby reducing the pK(a) and improving Caco-2 permeability."( Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Barf, T; Borsboom, J; de Kimpe, V; de Roos, J; de Wit, J; de Zwart, E; Dulos, J; Hoogenboom, N; Jaeger, M; Kaptein, A; Kazemier, B; Leandro-Garcia, P; Oubrie, A; Schultz-Fademrecht, C; van de Kar, B; van Hoek, M; van Zeeland, M; Versteegh, J; Vogel, G; Wijnands, F, 2011
)
0.37
" However, the poor in vivo bioavailability of resveratrol due to its rapid metabolism is being considered as a major obstacle in translating its effects in humans."( Enhancing the bioavailability of resveratrol by combining it with piperine.
Ahmad, N; Bailey, HH; Johnson, JJ; Mukhtar, H; Nihal, M; Scarlett, CO; Siddiqui, IA, 2011
)
0.37
"Our study demonstrated that piperine significantly improves the in vivo bioavailability of resveratrol."( Enhancing the bioavailability of resveratrol by combining it with piperine.
Ahmad, N; Bailey, HH; Johnson, JJ; Mukhtar, H; Nihal, M; Scarlett, CO; Siddiqui, IA, 2011
)
0.37
"An oral bioavailability issue encountered during the course of lead optimization in the renin program is described herein."( Impact of passive permeability and gut efflux transport on the oral bioavailability of novel series of piperidine-based renin inhibitors in rodents.
Bleasby, K; Chefson, A; Chen, A; Dubé, D; Ducharme, Y; Fournier, PA; Gagné, S; Gallant, M; Grimm, E; Hafey, M; Han, Y; Houle, R; Lacombe, P; Laliberté, S; Lévesque, JF; MacDonald, D; Mackay, B; Papp, R; Tschirret-Guth, R, 2011
)
0.37
" Studies on PAR2 have relied heavily upon activating effects of proteases and peptide agonists that lack stability and bioavailability in vivo."( Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110).
Barry, GD; Cotterell, AJ; Fairlie, DP; Halili, MA; Le, GT; Lohman, RJ; Suen, JY, 2012
)
0.38
" MK-6096 is an orally bioavailable potent and selective reversible antagonist of OX(1)R and OX(2)R currently in clinical development for insomnia."( Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia.
Breslin, MJ; Coleman, PJ; Cox, CD; Cui, D; Doran, SM; Fox, SV; Garson, SL; Gotter, AL; Harrell, CM; Reiss, DR; Renger, JJ; Schreier, JD; Stevens, J; Tannenbaum, PL; Winrow, CJ, 2012
)
0.38
" By inhibiting the metabolism of drugs, piperine improves the bioavailability of drugs."( Influence of piperine on ibuprofen induced antinociception and its pharmacokinetics.
Durga, KD; Mullangi, R; Padmavathi, Y; Reddy, BM; Venkatesh, S, 2011
)
0.37
"The poly-(ADP-ribose) polymerase (PARP) inhibitor, MK-4827, is a novel potent, orally bioavailable PARP-1 and PARP-2 inhibitor currently in phase I clinical trials for cancer treatment."( MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation.
Ang, KK; Buchholz, T; Buser-Doepner, C; Mason, KA; Mathur, A; Milas, L; Toniatti, C; Valdecanas, D; Wang, L, 2012
)
0.38
" Together, these data suggest that CP-945,598 is well absorbed and eliminated largely by CYP3A4/3A5-catalyzed metabolism."( Excretion, metabolism, and pharmacokinetics of 1-(8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl)-4-(ethylamino)piperidine-4-carboxamide, a selective cannabinoid receptor antagonist, in healthy male volunteers.
Liras, J; Miao, Z; Prakash, C; Sun, H, 2012
)
0.38
"01 for 3 mg/kg) increased the absolute bioavailability (AB) of repaglinide by 51."( Effects of efonidipine on the pharmacokinetics and pharmacodynamics of repaglinide: possible role of CYP3A4 and P-glycoprotein inhibition by efonidipine.
Choi, DH; Choi, JS; Li, C, 2012
)
0.38
" In vivo pharmacokinetic study in rats showed that immediate and complete release of repaglinide from the solid dispersion resulted in rapid absorption that significantly increased the bioavailability and the maximum plasma concentration over repaglinide raw material."( In vitro and in vivo studies on a novel solid dispersion of repaglinide using polyvinylpyrrolidone as the carrier.
Chen, XJ; Huang, SJ; Liu, QW; Yin, LF; Zhang, Q; Zhang, SH; Zhu, CL, 2012
)
0.38
" In rats and dogs, [(14)C]GDC-0973 was well absorbed (fraction absorbed, 70-80%)."( Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.
Aoyama, RG; Belvin, M; Boggs, J; Choo, EF; Deng, Y; Hoeflich, KP; Johnston, SH; Kassees, R; Ly, J; Martini, JF; Merchant, M; Orr, C; Plise, E; Ramaiya, A; Robarge, K, 2012
)
0.38
"9 mg/kg body weight) or the combination of the both - piperine was used in this combination to enhance the bioavailability of EGCG."( Green tea polyphenol epigallocatechin-3-gallate shows therapeutic antioxidative effects in a murine model of colitis.
Brückner, M; Domschke, W; Kucharzik, T; Lügering, A; Westphal, S, 2012
)
0.38
" Furthermore, it was found to be efficacious in the double transgenic rat hypertension model and show good to moderate oral bioavailability in two animal species."( 3,4-Diarylpiperidines as potent renin inhibitors.
Arbour, M; Aspiotis, R; Cauchon, E; Chen, A; Dubé, D; Falgueyret, JP; Fournier, PA; Gallant, M; Grimm, E; Han, Y; Juteau, H; Lacombe, P; Liu, S; Mellon, C; Ramtohul, Y; Simard, D; St-Jacques, R; Tsui, GC, 2012
)
0.78
" Exploration of the structure-activity relationships of 4 led to the identification of a potent and orally bioavailable TRPM8 antagonist, tetrahydroisoquinoline 87."( Fused piperidines as a novel class of potent and orally available transient receptor potential melastatin type 8 (TRPM8) antagonists.
Bartberger, MD; Bo, Y; Chen, J; Correll, TL; Deng, H; Gavva, NR; Gore, V; Klionsky, L; Lehto, SG; Ma, V; Nishimura, N; Norman, MH; Tamayo, NA; Tang, P; Wang, W; Youngblood, B, 2012
)
0.86
"Pharmacokinetic results show that FLAP has high bioavailability (> 75%), long T1/2 (> 260 min), and short peak time (<20 min)."( Disposition of orally administered a promising chemotherapeutic agent flavopiridol in the intestine.
Feng, Q; Li, Y; Liu, W; Liu, X; Liu, Z; Xia, B; Zhou, Q, 2013
)
0.39
"FLAP possesses high oral bioavailability and good absorption in the intestine, in which FLAP may be subjected to a P-gp efflux."( Disposition of orally administered a promising chemotherapeutic agent flavopiridol in the intestine.
Feng, Q; Li, Y; Liu, W; Liu, X; Liu, Z; Xia, B; Zhou, Q, 2013
)
0.39
" These results were discussed considering that curcumin may not be well absorbed and it did not reach a level high enough in vivo to overcome the severe hypercholesterolemia and oxidative stress produced by the PC-rich diet."( Effect of curcumin on LDL oxidation in vitro, and lipid peroxidation and antioxidant enzymes in cholesterol fed rabbits.
Kummerow, FA; Mahfouz, MM; Zhou, Q, 2011
)
0.37
"Vandetanib (an orally bioavailable VEGFR-2 and EGFR tyrosine kinases inhibitor) was combined at 100 mg, 200 mg, or 300 mg daily with standard dosed cetuximab and irinotecan (3+3 dose-escalation design)."( Phase I study of cetuximab, irinotecan, and vandetanib (ZD6474) as therapy for patients with previously treated metastastic colorectal cancer.
Abrams, TA; Ancukiewicz, M; Blaszkowsky, L; Chan, JA; Duda, DG; Elliott, M; Enzinger, PC; Goldstein, M; Jain, RK; Kulke, MH; Meyerhardt, JA; Regan, E; Schrag, D; Wolpin, BM; Zhu, AX, 2012
)
0.38
" By inhibiting the metabolism of drugs, piperine improves the bioavailability of drugs."( Effect of piperine on antihyperglycemic activity and pharmacokinetic profile of nateglinide.
Bommineni, MR; Mullangi, R; Nadipelli, M; Sama, V; Yenumula, P, 2012
)
0.38
" Incorporation of a 1,2,4-oxadiazole linker and substitution of the pendant phenyl ring led to the discovery of orally bioavailable analogues that showed efficient NR2B receptor occupancy in rats."( Discovery of 3-substituted aminocyclopentanes as potent and orally bioavailable NR2B subtype-selective NMDA antagonists.
Bednar, RA; Cunningham, ME; Dilella, AG; Fandozzi, C; Fay, JF; Kelly, MJ; Koblan, KS; Layton, ME; Liang, A; Lis, EV; McDonald, TP; Mosser, SD; Reiss, DR; Rodzinak, KJ; Sanderson, PE; Seabrook, GR; Trainor, N; Urban, MO; Wang, H; Yergey, J; Young, SD, 2011
)
0.37
" Piperine is known to enhance the bioavailability of curcumin, as a substrate of P-gp by at least 2000%."( A plausible explanation for enhanced bioavailability of P-gp substrates in presence of piperine: simulation for next generation of P-gp inhibitors.
Godbole, MM; Misra, K; Singh, DV, 2013
)
0.39
"This study investigated the effect of piperine on the gene expression of P-glycoprotein (P-gp) as well as pregnane-X-receptor (PXR) activity and also its implication on the bioavailability of diltiazem, a P-gp substrate."( Repeated dosing of piperine induced gene expression of P-glycoprotein via stimulated pregnane-X-receptor activity and altered pharmacokinetics of diltiazem in rats.
Han, HK; Kang, KW; Qiang, F, 2012
)
0.38
" Furthermore, the bepotastine salicylate-loaded tablet was prepared by the wet granulation method, and the dissolution and bioavailability in beagle dogs were evaluated compared to the bepotastine besilate-loaded commercial product."( Development of novel bepotastine salicylate salt bioequivalent to the commercial bepotastine besilate in beagle dogs.
Cho, KH; Choi, HG, 2013
)
0.39
" Recent advancement in bioavailability enhancement of drugs by compounds of herbal origin has produced a revolutionary shift in the way of therapeutics."( A comprehensive review on pharmacotherapeutics of herbal bioenhancers.
Awale, MM; Chauhan, BN; Dudhatra, GB; Kamani, DR; Kumar, A; Modi, CM; Mody, SK; Patel, HB, 2012
)
0.38
" Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation."( The discovery of CCR3/H1 dual antagonists with reduced hERG risk.
Bahl, A; Barton, P; Bowers, K; Brough, S; Evans, R; Luckhurst, CA; Mochel, T; Perry, MW; Rigby, A; Riley, RJ; Sanganee, H; Sisson, A; Springthorpe, B, 2012
)
0.38
" The results clearly suggest that piperine enhanced the bioavailability of curcumin and potentiated its protective effects against CUS induced cognitive impairment and associated oxidative damage in mice."( Piperine potentiates the protective effects of curcumin against chronic unpredictable stress-induced cognitive impairment and oxidative damage in mice.
Kumar, A; Rinwa, P, 2012
)
0.38
" Compound 8 has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow."( Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in c
Browning, M; Chen, L; Conway, CM; Denton, R; Dubowchik, GM; Houston, JG; Keavy, D; Kostich, W; Lentz, KA; Luo, G; Macor, JE; Santone, KS; Schartman, R; Signor, L; Tong, G, 2012
)
0.38
" The results revealed that a combination of glimepiride with piperine led to the enhancement of the bioavailability of glimepiride by inhibiting the CYP2C9 enzyme, which suggested that piperine might be beneficial as an adjuvant to glimepiride in a proper dose, in diabetic patients."( Effect of piperine on the pharmacokinetics and pharmacodynamics of glimepiride in normal and streptozotocin-induced diabetic rats.
Rani, TS; Sujatha, S; Veeresham, C, 2012
)
0.38
"A transdermal delivery system is warranted for repaglinide (RPG) which possesses half-life of 1 h and oral bioavailability of 56%."( A study on ethosomes as mode for transdermal delivery of an antidiabetic drug.
Bodade, SS; Chaudhari, PD; Kamble, MS; Shaikh, KS, 2013
)
0.39
"In view of the wide-spread deficiency of iron and zinc in populations dependent on plant foods, it is desirable to improve the bioavailability of the same."( Enhanced intestinal uptake of iron, zinc and calcium in rats fed pungent spice principles--piperine, capsaicin and ginger (Zingiber officinale).
Prakash, UN; Srinivasan, K, 2013
)
0.39
" (3S,5R)-12 showed oral bioavailability in rats and demonstrated blood pressure lowering activity in the double-transgenic rat model."( A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Baeschlin, DK; Breitenstein, W; Cumin, F; Ehrhardt, C; Francotte, E; Geisse, S; Gerhartz, B; Hartwieg, JC; Hassiepen, U; Jacoby, E; Klumpp, M; Kosaka, T; Krömer, M; Maibaum, J; Marzinzik, A; Ostermann, N; Ottl, J; Richert, P; Rigel, DF; Ruedisser, S; Sedrani, R; Trappe, J; Vangrevelinghe, E; Wagner, T; Webb, RL, 2013
)
0.62
"In this study, we used cubic nanoparticles containing piperine to improve the oral bioavailability of PPD and to enhance its absorption and inhibit its metabolism."( Enhanced oral absorption of 20(S)-protopanaxadiol by self-assembled liquid crystalline nanoparticles containing piperine: in vitro and in vivo studies.
Cheng, XD; Jia, XB; Jin, X; Li, SL; Sun, E; Tan, XB; You, M; Zhang, ZH, 2013
)
0.39
"The increased bioavailability of PPD-cubosome loaded with piperine is due to an increase in absorption and inhibition of metabolism of PPD by cubic nanoparticles containing piperine rather than because of improved release of PPD."( Enhanced oral absorption of 20(S)-protopanaxadiol by self-assembled liquid crystalline nanoparticles containing piperine: in vitro and in vivo studies.
Cheng, XD; Jia, XB; Jin, X; Li, SL; Sun, E; Tan, XB; You, M; Zhang, ZH, 2013
)
0.39
" bioavailability yet retaining its potency."( Systemic bile acid sensing by G protein-coupled bile acid receptor 1 (GPBAR1) promotes PYY and GLP-1 release.
Alvarez Sanchez, R; Beauchamp, J; Conde-Knape, K; Dehmlow, H; Iglesias, A; Mattei, P; Raab, S; Sewing, S; Sprecher, U; Ullmer, C, 2013
)
0.39
" In contrast to the orally bioavailable agonist RO5527239, we show that tauro-RO5527239 triggers PYY release only when applied intravenously."( Systemic bile acid sensing by G protein-coupled bile acid receptor 1 (GPBAR1) promotes PYY and GLP-1 release.
Alvarez Sanchez, R; Beauchamp, J; Conde-Knape, K; Dehmlow, H; Iglesias, A; Mattei, P; Raab, S; Sewing, S; Sprecher, U; Ullmer, C, 2013
)
0.39
" The aim of this trial was to study the absolute oral bioavailability of bilastine in humans."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013
)
0.39
"Oral bioavailability of bilastine was 60."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013
)
0.39
" The absolute oral bioavailability was moderate."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013
)
0.39
"To prepare curcumin-piperine (Cu-Pi) nanoparticles by various methods and to study the effect of various manufacturing parameters on Cu-Pi nanoparticles and to identify a suitable method for the preparation of Cu-Pi nanoparticles to overcome oral bioavailability and cancer cell targeting limitations in the treatment of cancer."( Preparation and characterization of curcumin-piperine dual drug loaded nanoparticles.
Kathiresan, K; Krishnan, K; Manavalan, R; Moorthi, C, 2012
)
0.38
" This dual nanoparticulate drug delivery system appears to be promising to overcome oral bioavailability and cancer cell targeting limitations in the treatment of cancer."( Preparation and characterization of curcumin-piperine dual drug loaded nanoparticles.
Kathiresan, K; Krishnan, K; Manavalan, R; Moorthi, C, 2012
)
0.38
" This coamorphous system provides a feasible way to process drugs with low solubility into substances with enhanced dissolution and stabilized amorphous state that could be conducive to greater bioavailability than the crystalline drug."( Coamorphous repaglinide-saccharin with enhanced dissolution.
Gao, Y; Liao, J; Qi, X; Zhang, J, 2013
)
0.39
" However, in addition to its culinary uses, pepper has important medicinal and preservative properties, and, more recently, piperine has been shown to have fundamental effects on p-glycoprotein and many enzyme systems, leading to biotransformative effects including chemoprevention, detoxification, and enhancement of the absorption and bioavailability of herbal and conventional drugs."( Piper nigrum and piperine: an update.
Goswami, TK; Meghwal, M, 2013
)
0.39
" The dichotomous effects of PIP on induction of CYP3A4 and MDR1 expression observed here and inhibition of their activity reported elsewhere challenges the potential use of PIP as a bioavailability enhancer and suggests that caution should be taken in PIP consumption during drug treatment in patients, particularly those who favor daily pepper spice or rely on certain pepper remedies."( Piperine activates human pregnane X receptor to induce the expression of cytochrome P450 3A4 and multidrug resistance protein 1.
Chai, SC; Chen, T; Lin, W; Ong, SS; Schuetz, EG; Wang, YM; Wu, J, 2013
)
0.39
" Significant covariates were sex and bioavailability on apparent clearance and food intake on the absorption rate constant."( Population pharmacokinetics of JNJ-37822681, a selective fast-dissociating dopamine D₂-receptor antagonist, in healthy subjects and subjects with schizophrenia and dose selection based on simulated D₂-receptor occupancy.
Hoeben, E; Mannaert, E; Neyens, M; Schmidt, M; Vermeulen, A, 2013
)
0.39
" Based on in vivo hypoglycemic results, bioavailability parameters like AUC, AUMC, Cmax, Tmax, MRT, t1/2 and relative bioavailability were found to be 2218."( Optimization and charaterization of repaglinide biodegradable polymeric nanoparticle loaded transdermal patchs: in vitro and in vivo studies.
Reddy, KR; Sakthivel, S; Swetha, C; Vijayan, V, 2013
)
0.39
" Bioflavonoids like quercetin are reported to have poor bioavailability and limited therapeutic potential against stress induced neurological disorders."( Quercetin along with piperine prevents cognitive dysfunction, oxidative stress and neuro-inflammation associated with mouse model of chronic unpredictable stress.
Kumar, A; Rinwa, P, 2017
)
0.46
" The present study investigated the synergistic antidepressant-like effect of trans-resveratrol and piperine, a bioavailability enhancer, in mice and explored the possible mechanism."( Piperine potentiates the antidepressant-like effect of trans-resveratrol: involvement of monoaminergic system.
Chen, Z; Huang, W; Li, G; Lin, M; Pan, J; Wang, Q; Wu, F; Wu, S; Xie, X; Xu, Y; Yan, Q; Yu, X, 2013
)
0.39
" Since cobimetinib exhibited absorption variability in cancer patients, a series of single-dose studies in healthy subjects were conducted to determine absolute bioavailability and elucidate potential effects of formulation, food, and elevated gastric pH on cobimetinib bioavailability."( Absolute bioavailability and effect of formulation change, food, or elevated pH with rabeprazole on cobimetinib absorption in healthy subjects.
Chan, IT; Choo, E; Deng, Y; Dresser, MJ; Eppler, S; Musib, L; Rooney, I, 2013
)
0.39
" Vandetanib, also known as ZD6474, is an orally bioavailable small molecule tyrosine kinase inhibitor of multiple growth factors that is an antagonist of the vascular endothelial growth factor receptor-2 (VEGFR-2)."( Specific binding of modified ZD6474 (Vandetanib) monomer and its dimer with VEGF receptor-2.
Kim, YS; Li, F; Li, Z; O'Neill, BE, 2013
)
0.39
" We also describe an orally bioavailable ABHD6 inhibitor, KT185, that displays excellent selectivity against other brain and liver serine hydrolases in vivo."( Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6).
Chang, JW; Cravatt, BF; Hsu, KL; Pugh, H; Speers, AE; Tsuboi, K; Whitby, LR, 2013
)
0.39
" The controlled dual release of curcumin and piperine from the G/SF microspheres would prolong their half-life, provide the optimal concentrations for therapeutic effects at a target site, and improve the bioavailability of curcumin."( The development of injectable gelatin/silk fibroin microspheres for the dual delivery of curcumin and piperine.
Damrongsakkul, S; Kanokpanont, S; Ratanavaraporn, J, 2014
)
0.4
" Interestingly, piperine also plays a vital role in increasing the bioavailability of many drugs which again is a promising property."( Piperine production by endophytic fungus Colletotrichum gloeosporioides isolated from Piper nigrum.
Chithra, S; Jasim, B; Jyothis, M; Radhakrishnan, EK; Sachidanandan, P, 2014
)
0.4
" Bruton's tyrosine kinase (BTK) shows constitutive activity in CLL and is the target of irreversible inhibition by ibrutinib, an orally bioavailable kinase inhibitor that has shown outstanding activity in CLL."( Bruton's tyrosine kinase (BTK) function is important to the development and expansion of chronic lymphocytic leukemia (CLL).
Bojnik, E; Buggy, JJ; Byrd, JC; Chang, BY; Davis, ME; Dubovsky, JA; Efremov, DG; Gobessi, S; Goettl, VM; Harrington, BK; Johnson, AJ; Laurenti, L; MacMurray, J; Ruppert, AS; Smith, LL; Smucker, KA; Stefanovski, MR; Towns, WH; Woyach, JA, 2014
)
0.4
" The potential of NLC for improving the oral bioavailability of ILO was also evaluated."( Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement.
Mandpe, L; Pokharkar, V, 2015
)
0.42
"30-fold increase in oral bioavailability of ILO NLC as compared with ILO pure drug suspension."( Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement.
Mandpe, L; Pokharkar, V, 2015
)
0.42
"The NLC formulation remarkably improved the oral bioavailability of ILO and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs."( Quality by design approach to understand the process of optimization of iloperidone nanostructured lipid carriers for oral bioavailability enhancement.
Mandpe, L; Pokharkar, V, 2015
)
0.42
"Here we show a curcumin encapsulated lipopolymeric hybrid nanoparticle formulation which could protect against QT prolongation and also render increased bioavailability and stability thereby overcoming the limitations associated with curcumin."( Mitigating prolonged QT interval in cancer nanodrug development for accelerated clinical translation.
Helson, L; Mukerjee, A; Ranjan, AP; Vishwanatha, JK, 2013
)
0.39
"Alogliptin is a selective, orally bioavailable inhibitor of the enzymatic activity of dipeptidyl peptidase-4 (DPP-4)."( Alogliptin: A new dipeptidyl peptidase-4 inhibitor for the management of type 2 diabetes mellitus.
Erowele, G; Ndefo, UA; Okoli, O, 2014
)
0.4
" This study suggested that food intake not only increases the bioavailability of blonanserin but differently affects the pharmacokinetics of its metabolites as well."( The pharmacokinetic and safety profiles of blonanserin in healthy Chinese volunteers after single fasting doses and single and multiple postprandial doses.
Chen, R; Chen, X; Hu, P; Jiang, J; Liu, H; Wang, H; Zhong, W; Zhou, Y, 2014
)
0.4
"The aim of this study was to investigate the effects of nifedipine on the bioavailability and pharmacokinetics of repaglinide in rats."( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine.
Choi, DH; Choi, I; Choi, JS, 2013
)
0.39
" Nifedipine also increased the absolute bioavailability (AB) of repaglinide by 50."( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine.
Choi, DH; Choi, I; Choi, JS, 2013
)
0.39
"Nifedipine enhanced the oral bioavailability of repaglinide, which may be mainly attributable to inhibition of CYP3A4-mediated metabolism of repaglinide in the small intestine and/or in the liver and to inhibition of the P-gp efflux transporter in the small intestine and/or reduction of total body clearance by nifedipine."( Effects of nifedipine on the pharmacokinetics of repaglinide in rats: possible role of CYP3A4 and P-glycoprotein inhibition by nifedipine.
Choi, DH; Choi, I; Choi, JS, 2013
)
0.39
" Thus, it may be useful for prolonged drug release in stomach to improve the bioavailability and reduced dosing frequency."( Gastroretentive mucoadhesive tablet of lafutidine for controlled release and enhanced bioavailability.
Patil, S; Talele, GS, 2015
)
0.42
" A significantly decreased Cmax, prolonged Tmax and satisfactory bioavailability of the osmotic pump tablet were obtained, and a good in vivo-in vitro correlation of the two drugs was also established."( Controlled release of metformin hydrochloride and repaglinide from sandwiched osmotic pump tablet.
He, W; Jin, Z; Qin, C; Wang, G; Wu, M; Yin, L; Zhang, Q; Zhu, C, 2014
)
0.4
"In this study, curcumin was designed into the nanoformulation called cubosome with piperine in order to improve oral bioavailability and tissue distribution of curcumin."( Preparation, characterisation and evaluation of curcumin with piperine-loaded cubosome nanoparticles.
Fu, JW; Huang, DE; Shi, ZQ; Sun, DM; Tu, YS; Yao, N; Zhang, JJ, 2014
)
0.4
" The pharmacokinetic test revealed that the cubosome could improve the oral bioavailability significantly compared to the suspension of curcumin with piperine and be mainly absorbed by the spleen."( Preparation, characterisation and evaluation of curcumin with piperine-loaded cubosome nanoparticles.
Fu, JW; Huang, DE; Shi, ZQ; Sun, DM; Tu, YS; Yao, N; Zhang, JJ, 2014
)
0.4
" A new generic formulation of bepotastine has been developed in China, and information concerning bioavailability and pharmacokinetic properties in the Chinese population has not been reported."( Comparative fasting bioavailability of 2 bepotastine formulations in healthy male Chinese volunteers: an open-label, randomized, single-dose, 2-way crossover study.
Hu, X; Liu, J; Shentu, J; Wu, G; Wu, L; Zhai, Y; Zheng, Y; Zhou, H; Zhu, M, 2014
)
0.4
"The aim of the present study was to compare the bioavailability and pharmacokinetic properties of 2 tablet formulations of bepotastine, the 10-mg generic formulation (test) and a branded formulation (reference), in healthy male Chinese volunteers to obtain registration approval of the test formulation."( Comparative fasting bioavailability of 2 bepotastine formulations in healthy male Chinese volunteers: an open-label, randomized, single-dose, 2-way crossover study.
Hu, X; Liu, J; Shentu, J; Wu, G; Wu, L; Zhai, Y; Zheng, Y; Zhou, H; Zhu, M, 2014
)
0.4
" In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of SEDDS on the bioavailability and intestinal absorption of piperine."( Enhanced oral bioavailability of piperine by self-emulsifying drug delivery systems: in vitro, in vivo and in situ intestinal permeability studies.
Cui, C; Ji, H; Li, X; Liu, H; Qin, M; Shao, B; Tang, J; Wang, Z; Wu, L, 2015
)
0.42
" Providing high bioavailability and a very long half-time, donepezil is regarded as effective and well tolerable in Alzheimer's disease patients, even in difficult clinical conditions such as hepatic or renal impairment."( Pharmacokinetic and pharmacodynamic evaluation of donepezil for the treatment of Alzheimer's disease.
Prvulovic, D; Schneider, B, 2014
)
0.4
"Although linarin possesses diverse pharmacological activities, its poor oral bioavailability has been a concern for further development."( Effects of piperine on the intestinal permeability and pharmacokinetics of linarin in rats.
Di, X; Feng, X; Liu, Y; Wang, X, 2014
)
0.4
" This lack of cognitive effects may be due to low bioavailability and, in turn, reduced bioefficacy of resveratrol in vivo."( Effects of resveratrol alone or in combination with piperine on cerebral blood flow parameters and cognitive performance in human subjects: a randomised, double-blind, placebo-controlled, cross-over investigation.
Dew, TP; Haskell, CF; Kennedy, DO; Reay, JL; Wightman, EL; Williamson, G, 2014
)
0.4
" Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability."( Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Achar, V; Arora, U; Awasthy, D; Bharath, S; Bheemarao, U; Chinnapattu, M; Coulson, M; de Sousa, SM; Ganguly, S; Gaonkar, S; Ghosh, A; Hameed P, S; Hoffner, S; Humnabadkar, V; Kaur, P; Kumar K N, M; Kumar, CN; Madhavapeddi, P; Manjrekar, P; Menasinakai, S; Mukherjee, K; Nandishaiah, R; Narayan, C; Panduga, V; Patil, V; Puttur, J; Raichurkar, A; Ramya, VK; Reddy, J; Rudrapatana, S; Sambandamurthy, VK; Shanbhag, G; Sharma, S; Sharma, U; Shinde, V; Solapure, S; Waterson, D; Werngren, J, 2014
)
0.4
" A pharmacokinetic study of compound 1 in vivo revealed good bioavailability and brain penetration in rats."( Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M(4) muscarinic acetylcholine receptor agonists.
Enomoto, T; Kitamura, A; Kiyoshi, A; Konishi, Y; Matsuda, H; Nakako, T; Ochi, Y; Sakai, M; Sumiyoshi, T; Suwa, A; Takai, K; Uematsu, Y; Uruno, Y, 2014
)
0.4
" Hybridization of compound 2 with the HTS hit compound 5 followed by optimization of the N-substituents of 7-azaindoline led to identification of compound 1, which showed highly selective M1 and M4 mAChRs agonistic activity, weak human ether-a-go-go related gene inhibition, and good bioavailability in multiple animal species."( Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists.
Enomoto, T; Hashimoto, G; Inoue, Y; Kitamura, A; Kiyoshi, A; Konishi, Y; Matsuda, H; Nakako, T; Nishikawa, H; Sakai, M; Sumiyoshi, T; Suwa, A; Takai, K; Uematsu, Y; Uruno, Y, 2014
)
0.4
"The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy."( Role of herbal bioactives as a potential bioavailability enhancer for Active Pharmaceutical Ingredients.
Alexander, A; Kumari, L; Qureshi, A; Saraf, S; Sharma, M; Vaishnav, P, 2014
)
0.4
" The bioavailability of ASP9521 after oral administration (1 mg/kg) was 35 %, 78 % and 58 % in rats, dogs and monkeys, respectively."( In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
Azami, H; Baskin-Bey, E; Enjo, K; Furutani, T; Heeringa, M; Kamiyama, Y; Kikuchi, A; Kuromitsu, S; Niimi, T; Ouatas, T; Watanabe, K, 2014
)
0.4
"ASP9521 is a potent, selective, orally bioavailable AKR1C3 inhibitor."( In vitro and in vivo characterisation of ASP9521: a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
Azami, H; Baskin-Bey, E; Enjo, K; Furutani, T; Heeringa, M; Kamiyama, Y; Kikuchi, A; Kuromitsu, S; Niimi, T; Ouatas, T; Watanabe, K, 2014
)
0.4
"ET-1 stimulates ETA -mediated NADPH oxidase-dependent ROS generation, which inhibits endothelial NO bioavailability and contributes to ET-1-induced contraction in healthy penile arteries."( Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from insulin-resistant obese rats: role of ET(A) and ET(B) receptors.
Benedito, S; García-Sacristán, A; Hernández, M; Martínez, P; Muñoz, M; Prieto, D; Sánchez, A, 2014
)
0.4
" Modulation of PXR transactivation has revealed the selective and orally bioavailable CCR1 antagonist BMS-817399 (29), which entered clinical trials for the treatment of rheumatoid arthritis."( Discovery of the CCR1 antagonist, BMS-817399, for the treatment of rheumatoid arthritis.
An, Y; Barrish, JC; Briceno, SW; Caceres-Cortes, J; Camac, DM; Caporuscio, C; Carter, PH; Cavallaro, C; Cvijic, ME; Davies, P; Dhar, M; Duncia, JV; Foster, WR; Gardner, DS; Grafstrom, RR; Hynes, J; Khan, JA; Liu, R; Patel, SR; Rose, AV; Santella, JB; Tebben, AJ; Vickery, RD; Watson, AJ; Wu, H; Yang, G; Yarde, M, 2014
)
0.4
" The present study aimed to investigate the efficacy of short-term supplementation with curcuminoids (co-administered with piperine to enhance the bioavailability of curcuminoids) in alleviating systemic oxidative stress and clinical symptoms, and improvement of health-related quality of life (HRQoL) in subjects suffering from chronic pulmonary complications due to SM exposure who are receiving standard respiratory treatments."( Effects of Curcuminoids-Piperine Combination on Systemic Oxidative Stress, Clinical Symptoms and Quality of Life in Subjects with Chronic Pulmonary Complications Due to Sulfur Mustard: A Randomized Controlled Trial.
Ghanei, M; Hajhashemi, A; Panahi, Y; Sahebkar, A, 2016
)
0.43
" The results indicated that the floating sustained-release tablets held a better capability for floating and drug release and more satisfactory pharmacokinetic parameters, such as a lower Cmax, a prolonged Tmax, but an equivalent bioavailability calculated by AUC0-24 compared to commercial tablets."( Preparation and pharmacokinetics study on gastro-floating sustained-release tablets of troxipide.
Gao, Y; Pan, WS; Wang, M; Wang, Z; Yang, X; Yang, Y; Ye, T; Yin, F, 2015
)
0.42
" The fasting state was characterized by a 67 % relative bioavailability compared with the meal conditions used in the trials and administration after a high-fat meal."( Population pharmacokinetic model of ibrutinib, a Bruton tyrosine kinase inhibitor, in patients with B cell malignancies.
Advani, R; Byrd, JC; de Jong, J; De Nicolao, G; de Trixhe, XW; Loury, D; Marostica, E; McGreivy, J; O'Brien, S; Poggesi, I; Sukbuntherng, J; Vermeulen, A, 2015
)
0.42
" Low permeability was a general feature of this series, however oral bioavailability could be achieved through the use of ester prodrugs."( Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists.
Andrés, M; Buil, MA; Calbet, M; Casado, O; Castro, J; Eastwood, PR; Eichhorn, P; Ferrer, M; Forns, P; Moreno, I; Petit, S; Roberts, RS, 2014
)
0.4
"The therapeutic efficacy of repaglinide (RPG) is limited by the low and variable oral bioavailability owing to its limited aqueous solubility."( Preparation, characterization and in vivo evaluation of formulation of repaglinide with hydroxypropyl-β-cyclodextrin.
Cao, W; He, Z; Liu, M; Sun, Y, 2014
)
0.4
"Knowing that curcumin has low bioavailability when administered orally, and that piperine has bioenhancer activity by inhibition of hepatic and intestinal biotransformation processes, the aim of this study was to investigate the antidiabetic and antioxidant activities of curcumin (90 mg/kg) and piperine (20 or 40 mg/kg), alone or co-administered, incorporated in yoghurt, in streptozotocin (STZ)-diabetic rats."( Piperine, a natural bioenhancer, nullifies the antidiabetic and antioxidant activities of curcumin in streptozotocin-diabetic rats.
Arcaro, CA; Assis, RP; Baviera, AM; Brunetti, IL; Costa, PI; Gutierres, VO; Moreira, TF, 2014
)
0.4
" In vivo HS-72 is well-tolerated, showing bioavailability and efficacy, inhibiting tumor growth and promoting survival in a HER2+ model of breast cancer."( Identification of an allosteric small-molecule inhibitor selective for the inducible form of heat shock protein 70.
Alwarawrah, Y; Bodoor, K; Brodsky, JL; Carlson, DA; Darr, DB; Gobillot, TA; Haystead, TA; Howe, MK; Hughes, PF; Hunter, LM; Jaeger, AM; Jordan, JL; Loiselle, DR; Molzberger, ET; Spector, NL; Thiele, DJ, 2014
)
0.4
" In the pharmacokinetic studies in mice, rats and dogs, favorable pharmacokinetic profiles and good oral bioavailability were observed for AV560."( [Antiviral activity in vitro and pharmacokinetics of HCV entry inhibitor AVR560].
Bulanova, EA; Bychko, VV; Ezhova, EV; Iamanushkin, PM; Ivashchenko, AA; Ivashchenko, AV; Koriakova, AG; Korzinov, OM; Mit'kin, OD; Vyshemirskaia, PV, 2014
)
0.4
" Almost 10 (TD-A) and 15 (TD-B)-fold enhancement in the oral bioavailability of nanocrystals was observed regardless of the fasted/fed state compared to pure repaglinide."( Ultra rapidly dissolving repaglinide nanosized crystals prepared via bottom-up and top-down approach: influence of food on pharmacokinetics behavior.
Gadadare, R; Mandpe, L; Pokharkar, V, 2015
)
0.42
" Piperine, one of the main constituents of black pepper, is known to increase the bioavailability of curcuminoids in mouse and human studies when consumed with turmeric."( Turmeric and black pepper spices decrease lipid peroxidation in meat patties during cooking.
Heber, D; Henning, SM; Huang, J; Lee, RP; Li, Z; Zerlin, A; Zhang, Y, 2015
)
0.42
" The results show that Cur-PIP-SMEDDS can increase the solubility and stability of curcumin significantly, in the expectation of enhancing the bioavailability of it."( [Optimization and characterization of curcumin-piperine dual drug loaded self-microemulsifying drug delivery system by simplex lattice design].
Dai, JD; Jiang, QL; Li, QP; Zhai, WW, 2014
)
0.4
"Data from the clinical absolute bioavailability (F) study with cobimetinib suggested that F was lower than predicted based on its low hepatic extraction and good absorption."( Use of transgenic mouse models to understand the oral disposition and drug-drug interaction potential of cobimetinib, a MEK inhibitor.
Choo, EF; DeMent, K; Ly, J; Messick, K; Qin, A; Takahashi, R; Woolsey, S, 2015
)
0.42
" Ibrutinib is an orally bioavailable and highly specific BTK inhibitor that was recently approved for treatment of patients with recurrent CLL and mantle cell lymphoma (MCL)."( Mechanisms of ibrutinib resistance in chronic lymphocytic leukaemia and non-Hodgkin lymphoma.
Lynn Wang, Y; Smith, SM; Zhang, SQ; Zhang, SY, 2015
)
0.42
" Further optimization of the pharmacokinetic (PK) properties afforded MK-8267 as a potent, orally bioavailable and brain penetrant KSP inhibitor which showed anti-tumor activity in preclinical xenograft models."( Discovery of novel spiro 1,3,4-thiadiazolines as potent, orally bioavailable and brain penetrant KSP inhibitors.
Allbritton, O; Angeles, AR; Basso, AD; Dai, C; Gray, K; Liang, L; Liu, M; Mansoor, UF; Siddiqui, MA; Tang, H; Vitharana, D; Yang, L, 2015
)
0.42
" The crystalline form of the compound is found to be low bioavailable, therefore attempts have been made to improve its bioavailability through polymorphic transformation and salt formation."( Synthesis and Biological Studies of a Novel CB1 Antagonist.
Banerjee, K; Jain, M; Joharapurkar, A; Patel, H; Srivastava, B; Vallabh, A, 2016
)
0.43
" A new fixed-dose combination (FDC) capsule containing 28 mg memantine extended release (ER) and 10 mg donepezil was evaluated for bioequivalence with co-administered commercially available memantine ER and donepezil, and for bioavailability with regard to food intake."( A novel once-daily fixed-dose combination of memantine extended release and donepezil for the treatment of moderate to severe Alzheimer's disease: two phase I studies in healthy volunteers.
Boinpally, R; Chen, L; Hofbauer, RK; McClure, N; Periclou, A; Zukin, SR, 2015
)
0.42
" There was no significant food effect on the bioavailability of the FDC components."( A novel once-daily fixed-dose combination of memantine extended release and donepezil for the treatment of moderate to severe Alzheimer's disease: two phase I studies in healthy volunteers.
Boinpally, R; Chen, L; Hofbauer, RK; McClure, N; Periclou, A; Zukin, SR, 2015
)
0.42
"An FDC capsule containing 28 mg memantine ER and 10 mg donepezil is bioequivalent to commercially available memantine ER and donepezil, and bioavailability is not affected by food intake or sprinkling of capsule contents on applesauce."( A novel once-daily fixed-dose combination of memantine extended release and donepezil for the treatment of moderate to severe Alzheimer's disease: two phase I studies in healthy volunteers.
Boinpally, R; Chen, L; Hofbauer, RK; McClure, N; Periclou, A; Zukin, SR, 2015
)
0.42
"P-glycoprotein (P-gp) efflux is the major cause of multidrug resistance (MDR) in tumors when using anticancer drugs, moreover, poor bioavailability of few drugs is also due to P-gp efflux in the gut."( Co-delivery of rapamycin- and piperine-loaded polymeric nanoparticles for breast cancer treatment.
Domb, AJ; Katiyar, SS; Khan, W; Muntimadugu, E; Rafeeqi, TA, 2016
)
0.43
"Emodin (1,3,8-trihydroxy-6-methylanthraquinone) has been widely used as a traditional medicine and was shown to possess a multitude of health-promoting properties in pre-clinical studies, but its bioavailability was low due to the extensive glucuronidation in liver and intestine, hindering the development of emodin as a feasible chemopreventive agent."( Effect of piperine on the bioavailability and pharmacokinetics of emodin in rats.
Di, X; Liu, Y; Wang, X, 2015
)
0.42
" The present study examined the synergistic effect of low doses of FA combined with subthreshold dose of piperine, a bioavailability enhancer, on depression-like behaviors in mice, and investigated the possible mechanism."( Synergistic antidepressant-like effect of ferulic acid in combination with piperine: involvement of monoaminergic system.
Chen, J; Chen, L; Chen, R; Huang, W; Li, G; Pan, J; Reed, M; Ruan, L; Wang, R; Xie, X; Xu, Y; Yan, Q; Zhang, M, 2015
)
0.42
" Piperine, an alkaloid present in black pepper, seems to enhance the bioavailability and activity of curcumin."( Curcumin in Combination with Piperine Suppresses Osteoclastogenesis In Vitro.
Geurtsen, W; Leyhausen, G; Martins, CA; Volk, J, 2015
)
0.42
" Phyllanthin along with piperine (a nutraceutical bioenhancer) was formulated as a mixed micellar lipid formulation (MMLF) in the present study and investigated to resolve the low bioavailability and enhance hepatoprotective effects on oral administration."( Antioxidant and hepatoprotective effects of mixed micellar lipid formulation of phyllanthin and piperine in carbon tetrachloride-induced liver injury in rodents.
Mishra, SH; Nagar, PA; Rajpara, A; Sethiya, NK; Shah, P, 2015
)
0.42
" It has been proved that curcumin is poorly absorbed while piperine is a bioavailability-enhancer."( Combination of curcumin and piperine prevents formation of gallstones in C57BL6 mice fed on lithogenic diet: whether NPC1L1/SREBP2 participates in this process?
Li, M; Li, Y; Tian, Y; Wu, S, 2015
)
0.42
" The present study was designed to investigate the absolute bioavailability (F) of ibrutinib in the fasting and fed state and assess the effect of grapefruit juice (GFJ) on the systemic exposure of ibrutinib in order to determine the fraction escaping the gut (Fg ) and the fraction escaping hepatic extraction (Fh ) in the fed state."( Stable isotope-labelled intravenous microdose for absolute bioavailability and effect of grapefruit juice on ibrutinib in healthy adults.
de Jong, J; de Vries, R; de Zwart, L; Hellemans, P; Jiao, J; Mannaert, E; Murphy, J; Skee, D; Smit, JW; Snoeys, J; Sukbuntherng, J; Vliegen, M, 2016
)
0.43
"CEP-32215 is a new, potent, selective, and orally bioavailable inverse agonist of the histamine H3 receptor (H3R) with drug-like properties."( 3-(1'-Cyclobutylspiro[4H-1,3-benzodioxine-2,4'-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist.
Aimone, LD; Ator, MA; Bacon, ER; Gruner, JA; Hudkins, RL; Marino, MJ; Mathiasen, JR; Raddatz, R; Williams, M, 2016
)
0.43
" It also enhances the bioavailability of phytochemicals and drugs."( Energetics, Thermodynamics, and Molecular Recognition of Piperine with DNA.
Haridas, M; Haris, P; Mary, V; Sudarsanakumar, C, 2015
)
0.42
" Orally bioavailable inhibitors of spleen tyrosine kinase, Bruton's tyrosine kinase, or PI3Kδ, induce high rates of durable responses."( The role of B-cell receptor inhibitors in the treatment of patients with chronic lymphocytic leukemia.
Wiestner, A, 2015
)
0.42
" In vivo pharmacokinetic testing revealed that inverse agonist 8c is orally bioavailable and has vastly reduced brain penetration compared to rimonabant."( Pyrazole antagonists of the CB1 receptor with reduced brain penetration.
Amato, G; Bortoff, K; Fulp, A; Maitra, R; Seltzman, H; Snyder, R; Wiethe, R; Zhang, Y, 2016
)
0.43
" In the present study, an attempt was made to study the brain bioavailability of commonly used anti-Alzheimer drug donepezil (DNP) liposomal formulation by intranasal route in rats."( Preparation, characterization, and in vivo evaluation of intranasally administered liposomal formulation of donepezil.
Al Asmari, AK; Fatani, A; Tariq, M; Ullah, Z, 2016
)
0.43
" In present study, we assessed the effects of trans-resveratrol used in combination with piperine, commonly known as a bioavailability enhancer, on chronic unpredictable mild stress-induced depressive-like behaviors and relevant molecular targets."( Piperine potentiates the effects of trans-resveratrol on stress-induced depressive-like behavior: involvement of monoaminergic system and cAMP-dependent pathway.
An, Y; Lin, M; Pan, J; Wang, G; Wu, F; Xu, X; Xu, Y; Yu, Y; Zhang, C, 2016
)
0.43
" Study B assessed the effect of a high-fat meal on the bioavailability of tofacitinib from the XR formulation."( Extended-Release Once-Daily Formulation of Tofacitinib: Evaluation of Pharmacokinetics Compared With Immediate-Release Tofacitinib and Impact of Food.
Alvey, C; Fletcher, T; Kushner, J; Lamba, M; Stock, TC; Wang, R, 2016
)
0.43
"These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy."( Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system.
Ezzeldin, E; Iqbal, M; Shakeel, F, 2016
)
0.43
"The effect of single and multiple doses of a herbal preparation Trikatu was studied on the bioavailability and pharmacokinetics of carbamazepine in rabbits."( EFFECT OF TRIKATU, AN AYURVEDIC PRESCRIPTION ON THE PHARMACOKINETIC PROFILE OF CARBAMAZEPINE IN RABBITS.
Bhargava, VK; Garg, SK; Karan, RS, 1999
)
0.3
"We combine quantum chemical and molecular docking techniques to provide new insights into how piperine molecule in various forms of pepper enhances bioavailability of a number of drugs including curcumin in turmeric for which it increases its bioavailability by a 20-fold."( Quantum Chemical and Docking Insights into Bioavailability Enhancement of Curcumin by Piperine in Pepper.
Balasubramanian, K; Das, S; Patil, VM, 2016
)
0.43
" The systemic exposure level and bioavailability after oral administration of 43 were also good in dog."( Piperidine derivatives as nonprostanoid IP receptor agonists 2.
Hayashi, R; Ishigaki, T; Isogaya, M; Ito, H; Miyamoto, M; Morita, Y, 2016
)
0.43
" As the majority of data were below the assay sensitivity for FF, any potential differences in the bioavailability of FF when delivered alone or as FF/LEVO FDC could not be established."( Pharmacokinetics, Safety, and Tolerability of Once-Daily Intranasal Fluticasone Furoate and Levocabastine Administered Alone or Simultaneously as fluticasone Furoate/Levocabastine Fixed-Dose Combination.
Allen, A; Bareille, P; Burns, O; Gupta, A; Hughes, S; Miller, SR; Murdoch, RD, 2016
)
0.43
" The absolute bioavailability of alectinib was moderate at 36."( Absorption, distribution, metabolism and excretion (ADME) of the ALK inhibitor alectinib: results from an absolute bioavailability and mass balance study in healthy subjects.
Bogman, K; Guerini, E; Heinig, K; Katsuki, H; Kawashima, K; Martin-Facklam, M; Moore, DJ; Morcos, PN; Muri, D; Nieforth, K; Phipps, A; Sato, M; Whayman, M; Yu, L, 2017
)
0.46
"These results demonstrated that increasing the bioavailability of piperine may be achieved as demonstrated by findings in this study."( Hot melt extrusion as an approach to improve solubility, permeability and oral absorption of a psychoactive natural product, piperine.
Alshehri, S; Alsheteli, A; Alsulays, B; Ashour, EA; Feng, X; Gryczke, A; Kolter, K; Langley, N; Majumdar, S; Repka, MA, 2016
)
0.43
" Besides, the reported pharmacokinetics of PIP varied a lot without appropriate bioavailability determined from the same dose."( Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats.
Chow, MSS; Lam, CWK; Li, C; Ren, T; Wang, Q; Zhang, Y; Zuo, Z, 2016
)
0.43
" Hence, in order to enhance the bioavailability of curcumin, we combined it with the bioavailability enhancers like piperine and quercetin."( Influence of piperine and quercetin on antidiabetic potential of curcumin.
Chintamaneni, M; Invally, M; Kaur, G, 2016
)
0.43
"071 μM), selective and orally bioavailable small-molecule SHP2 inhibitor, SHP099, that stabilizes SHP2 in an auto-inhibited conformation."( Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.
Acker, MG; Antonakos, B; Chan, HM; Chen, CH; Chen, YN; Chen, Z; Cooke, VG; Deng, Z; Dobson, JR; Fei, F; Fekkes, P; Firestone, B; Fodor, M; Fortin, PD; Fridrich, C; Gao, H; Garcia-Fortanet, J; Grunenfelder, D; Hao, HX; Ho, S; Hsiao, K; Jacob, J; Kang, ZB; Karki, R; Kato, M; Keen, NJ; La Bonte, LR; LaMarche, MJ; Larrow, J; Lenoir, F; Liu, G; Liu, S; Majumdar, D; Meyer, MJ; Palermo, M; Perez, L; Price, E; Pu, M; Quinn, C; Ramsey, T; Sellers, WR; Shakya, S; Shultz, MD; Slisz, J; Stams, T; Venkatesan, K; Wang, P; Warmuth, M; Williams, S; Yang, G; Yuan, J; Zhang, JH; Zhu, P, 2016
)
0.43
"Molecularly targeted agents that are designed to target specific lesions have been proven effective as clinical cancer therapies; however, most currently available therapeutic agents are poorly water-soluble and require oral administration, thereby resulting in low bioavailability and a high risk of side effects due to dose intensification."( iRGD-Decorated Polymeric Nanoparticles for the Efficient Delivery of Vandetanib to Hepatocellular Carcinoma: Preparation and in Vitro and in Vivo Evaluation.
Li, J; Liu, Z; Lu, D; Wang, H; Wang, J; Wei, X; Xie, H; Xu, X; Zheng, S; Zhuang, R, 2016
)
0.43
" Although donepezil is approved for use in patients and selective for inhibiting acetylcholinesterase over BuChE, no studies have reported cocaine bioavailability in human subjects receiving donepezil."( Cocaine cardiovascular effects and pharmacokinetics after treatment with the acetylcholinesterase inhibitor donepezil.
DeSouza, C; Grasing, K; Mathur, D; Moody, DE; Newton, TF; Sturgill, M, 2016
)
0.43
" Clinically significant changes in cocaine bioavailability and cardiovascular effects do not occur following this dose of donepezil."( Cocaine cardiovascular effects and pharmacokinetics after treatment with the acetylcholinesterase inhibitor donepezil.
DeSouza, C; Grasing, K; Mathur, D; Moody, DE; Newton, TF; Sturgill, M, 2016
)
0.43
" The modulation of donepezil release from MIPs-based formulations using oil vehicles may contribute to decrease its side effects, possibly regulating its absorption rate in the gastrointestinal tract."( Molecularly imprinted microparticles in lipid-based formulations for sustained release of donepezil.
Carvalho, FC; de Araújo, MB; de Figueiredo, EC; Pereira, GR; Ruela, AL, 2016
)
0.43
" In dog, 14 had oral bioavailability (74%), clearance (3."( Characterization of 3,3-dimethyl substituted N-aryl piperidines as potent microsomal prostaglandin E synthase-1 inhibitors.
Antonysamy, S; Bhattachar, SN; Chandrasekhar, S; Fisher, MJ; Fretland, AJ; Gooding, K; Harvey, A; Hughes, NE; Kuklish, SL; Luz, JG; Manninen, PR; McGee, JE; Navarro, A; Norman, BH; Partridge, KM; Quimby, SJ; Schiffler, MA; Sloan, AV; Warshawsky, AM; York, JS; Yu, XP, 2016
)
0.68
" The present study involves formulation of curcumin and piperine coloaded glyceryl monooleate (GMO) nanoparticles coated with various surfactants with a view to enhance the bioavailability of curcumin and penetration of both drugs to the brain tissue crossing the BBB and to enhance the anti-parkinsonism effect of both drugs in a single platform."( Delivery of Dual Drug Loaded Lipid Based Nanoparticles across the Blood-Brain Barrier Impart Enhanced Neuroprotection in a Rotenone Induced Mouse Model of Parkinson's Disease.
Das, M; Kundu, P; Sahoo, SK; Tripathy, K, 2016
)
0.43
" Compound 14 demonstrated excellent selectivity over other aspartyl proteases and moderate oral bioavailability in rats."( Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors.
Behnke, CA; Imaeda, Y; Kanagawa, R; Kondo, M; Kubo, K; Kuroita, T; Sanada, T; Snell, G; Suzuki, S; Tarui, N; Tawada, M; Tomimoto, M, 2016
)
0.43
"Curcumin (CUR) is known to exert numerous health-promoting effects in pharmacological studies, but its low bioavailability hinders the development of curcumin as a feasible therapeutic agent."( Selective reduction in the expression of UGTs and SULTs, a novel mechanism by which piperine enhances the bioavailability of curcumin in rat.
Cai, D; Chen, Y; Chen, Z; Gan, H; Huang, D; Huang, X; Sun, D; Yao, N; Zeng, Q; Zeng, X; Zhang, C; Zhao, Z; Zhong, G; Zhuo, J, 2017
)
0.46
"The results suggest that altered pharmacokinetics and enhanced bioavailability of FEX might be attributed to PIP-mediated inhibition of P-gp drug efflux."( The influence of piperine on the pharmacokinetics of fexofenadine, a P-glycoprotein substrate, in healthy volunteers.
Bedada, SK; Boga, PK, 2017
)
0.46
"GDC-0425 [5-((1-ethylpiperidin-4-yl)oxy)-9H-pyrrolo[2,3-b:5,4-c']dipyridine-6-carbonitrile] is an orally bioavailable small-molecule inhibitor of checkpoint kinase 1 that was investigated as a novel cotherapy to potentiate chemotherapeutic drugs, such as gemcitabine."( Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450.
Chen, Y; Halladay, JS; Hop, CE; Khojasteh, SC; Ma, S; Siu, M; Takahashi, RH, 2017
)
0.46
"The current study addressed the hypothesis that the local decrease in endothelin-1 (ET-1) bioavailability during sustained flow increases contributes to endothelium-dependent, flow-mediated dilatation (FMD) of conduit arteries and is altered in presence of cardiovascular risk factors."( Physiological role of endothelin-1 in flow-mediated vasodilatation in humans and impact of cardiovascular risk factors.
Bellien, J; Duflot, T; Gutierrez, L; Iacob, M; Joannidès, R; Monteil, C; Rémy-Jouet, I; Richard, V; Roche, C; Thuillez, C; Vendeville, C, 2017
)
0.46
"Curcumin is a well-established cardioprotective phytoconstituent, but the poor bioavailability associated with it is always a matter of therapeutic challenge."( Cardioprotective effect of curcumin and piperine combination against cyclophosphamide-induced cardiotoxicity.
Bhattacharjee, A; Chakraborty, M; Kamath, JV,
)
0.13
" The oral bioavailability of domperidone is very low due to its rapid first pass metabolism in the intestine and liver."( Enhanced Oral Bioavailability of Domperidone with Piperine in Male Wistar Rats: Involvement of CYP3A1 and P-gp Inhibition.
Athukuri, BL; Neerati, P, 2017
)
0.46
" The oral pharmacokinetics of domperidone was evaluated by conducting oral bioavailability study in rats."( Enhanced Oral Bioavailability of Domperidone with Piperine in Male Wistar Rats: Involvement of CYP3A1 and P-gp Inhibition.
Athukuri, BL; Neerati, P, 2017
)
0.46
"Piperine enhanced the oral bioavailability of domperidone by inhibiting CYP3A1 and P-gp in rats."( Enhanced Oral Bioavailability of Domperidone with Piperine in Male Wistar Rats: Involvement of CYP3A1 and P-gp Inhibition.
Athukuri, BL; Neerati, P, 2017
)
0.46
"We previously reported that piperine, an active alkaloidal principal of black and long peppers, enhances drug bioavailability by inhibiting drug metabolism."( Piperine Decreases Binding of Drugs to Human Plasma and Increases Uptake by Brain Microvascular Endothelial Cells.
Dubey, RK; Imthurn, B; Leeners, B; Merki-Feld, GS; Rosselli, M, 2017
)
0.46
" Grapefruit juice increased bioavailability and may have reduced systemic clearance of blonanserin."( Effects of food and grapefruit juice on single-dose pharmacokinetics of blonanserin in healthy Chinese subjects.
Hu, HT; Hu, JQ; Lu, HY; Ni, XJ; Peng, H; Qiu, C; Shang, DW; Shen, LF; Wang, ZZ; Wen, YG; Zhang, M; Zhang, YF, 2018
)
0.48
" Venetoclax is a selective, orally bioavailable inhibitor of BCL-2 active in previously treated patients with relapsed or refractory chronic lymphocytic leukaemia."( Venetoclax for chronic lymphocytic leukaemia progressing after ibrutinib: an interim analysis of a multicentre, open-label, phase 2 trial.
Barr, PM; Byrd, JC; Cheson, BD; Choi, M; Chyla, B; Coutre, S; Davids, MS; Furman, RR; Humerickhouse, RA; Jones, JA; Lamanna, N; Mato, AR; Potluri, J; Salem, AH; Verdugo, M; Wierda, WG; Woyach, J; Zhou, L, 2018
)
0.48
" Consequently, there is a great interest in the application of piperine as an alternative medicine or bioavailability enhancer."( Piperine-mediated drug interactions and formulation strategy for piperine: recent advances and future perspectives.
Back, SY; Han, HK; Kim, HY; Lee, SH, 2018
)
0.48
" Rifampicin, which is very effective against Mycobacterium tuberculosis, in both the phases of treatment, has certain concerns, which includes, decreased bioavailability with chronic use and hepatotoxicity."( A Randomized, Controlled, Phase III Clinical Trial to Evaluate the Efficacy and Tolerability of Risorine with Conventional Rifampicin in the Treatment of Newly Diagnosed Pulmonary Tuberculosis Patients.
Jagannath, K; Patel, A; Patel, M; Patel, N; Vora, A, 2017
)
0.46
" Lonafarnib is an orally bioavailable nonpeptide tricyclic farnesyltransferase inhibitor with excellent pharmacokinetic and safety profile."( Lonafarnib synergizes with azoles against Aspergillus spp. and Exophiala spp.
Gao, L; He, C; Qiao, J; Sun, Y; Zheng, W, 2018
)
0.48
"Alcohol increased the bioavailability of blonanserin and N-deethyl blonanserin in healthy subjects and the marked effect of alcohol on blonanserin bioavailability should be taken into consideration in deciding dosing schedules in clinical therapy."( Effects of Alcohol on the Pharmacokinetics of Blonanserin and N-Deethylated Blonanserin in Healthy Chinese Subjects.
Chen, Y; Deng, S; Hu, J; Lu, H; Ni, X; Peng, H; Shang, D; Wang, Z; Wen, Y; Zhang, M; Zhang, Y; Zhu, X, 2018
)
0.48
" However, the oral bioavailability of Rh2 is low, with P-glycoprotein (P-gp) and CYP3A4 being reported to be the main factors."( Enhancement of oral bioavailability and immune response of Ginsenoside Rh2 by co-administration with piperine.
Jiang, XH; Jin, ZH; Liu, H; Qiu, W; Wang, L, 2018
)
0.48
" The bioavailability (BA) of TAK-272 after oral administration to rats and monkeys was low, especially in fasted monkeys, and the systemic exposure of TAK-272 was highly variable in monkeys."( Differences in nonclinical pharmacokinetics between species and prediction of human pharmacokinetics of TAK-272 (SCO-272), a novel orally active renin inhibitor.
Ebihara, T; Jinno, F; Nishihara, M; Tagawa, Y; Takahashi, J, 2018
)
0.48
" Raloxifene's oral bioavailability was determined in a series of pharmacokinetic experiments using the freely moving rat model."( The Effect of Piperine Pro-Nano Lipospheres on Direct Intestinal Phase II Metabolism: The Raloxifene Paradigm of Enhanced Oral Bioavailability.
Aldouby Bier, G; Cherniakov, I; Domb, AJ; Hoffman, A; Izgelov, D, 2018
)
0.48
" Although we cannot exclude issues on bioavailability and in vivo efficacy of the used compounds, we hypothesize that extracellular TG1/TG2 activity is of greater importance than (intra-)cellular activity in mouse EAE pathology."( Characterization of Transglutaminase 2 activity inhibitors in monocytes in vitro and their effect in a mouse model for multiple sclerosis.
Bol, JGJM; Brevé, JJP; Chrobok, NL; Drukarch, B; El Alaoui, S; Jongenelen, CA; van Dam, AM; Wilhelmus, MMM, 2018
)
0.48
" Since 3 showed unacceptably low bioavailability (BA) in rats, structural modification, using SBDD and focused on physicochemical properties was conducted to improve its PK profile while maintaining renin inhibitory activity."( Discovery of benzimidazole derivatives as orally active renin inhibitors: Optimization of 3,5-disubstituted piperidine to improve pharmacokinetic profile.
Behnke, CA; Fukase, Y; Imaeda, Y; Iwanaga, K; Kajimoto, Y; Kanagawa, R; Kondo, M; Kuroita, T; Kusumoto, K; Matsuda, K; Snell, G; Taya, N; Tokuhara, H; Watanabe, K, 2018
)
0.48
" Piperine is also known to increase the bioavailability of dietary components, including curcumin."( Piperine potentiates curcumin-mediated repression of mTORC1 signaling in human intestinal epithelial cells: implications for the inhibition of protein synthesis and TNFα signaling.
Hage, DS; He, B; Kaur, H; Moreau, R; Rodriguez, E; Zhang, C, 2018
)
0.48
"The objective of the study was to improve the bioavailability of poorly soluble repaglinide (RPG) by preparing nanosuspension with poloxamer 188 using high pressure homogenization (HPH)."( Preparation, Characterization and In Vivo Assessment of Repaglinide Nanosuspension for Oral Bioavailability Improvement.
Bari, SB; Zawar, LR, 2018
)
0.48
" Further, the dried aqueous suspensions were evaluated for drug content, solubility, in vitro dissolution, oral bioavailability study and stability study."( Preparation, Characterization and In Vivo Assessment of Repaglinide Nanosuspension for Oral Bioavailability Improvement.
Bari, SB; Zawar, LR, 2018
)
0.48
"The outcomes of the study revealed significant enhancement in dissolution rate and oral bioavailability of RPG due to size reduction to nano range by HPH."( Preparation, Characterization and In Vivo Assessment of Repaglinide Nanosuspension for Oral Bioavailability Improvement.
Bari, SB; Zawar, LR, 2018
)
0.48
" This phenomenon was replicated during in vivo pharmacokinetic studies, whereby the bioavailability of simple clay-based lipid formulations was decreased relative to controls."( Montmorillonite and Laponite Clay Materials for the Solidification of Lipid-Based Formulations for the Basic Drug Blonanserin: In Vitro and in Vivo Investigations.
Cuyckens, F; Dening, TJ; Holm, R; Prestidge, CA; Rao, S; Thomas, N; van Looveren, C, 2018
)
0.48
" All compounds displayed favourable ADME findings which predict good oral bioavailability of these derivatives."( Quinoline containing chalcone derivatives as cholinesterase inhibitors and their in silico modeling studies.
Farooq Rizvi, SU; Iqbal, J; Najam-Ul-Haq, M; Shah, HS; Shah, MS, 2018
)
0.48
" However, IBR is insoluble at neutral pH and can dissolve only at low pH: thus, commercial IBR products present poor bioavailability and weakened in vivo antitumor activity."( Novel Self-Assembled Ibrutinib-Phospholipid Complex for Potently Peroral Delivery of Poorly Soluble Drugs with pH-Dependent Solubility.
Deng, Y; Hu, L; Lai, C; Li, C; Liu, M; Liu, X; Lu, M; Luo, X; Qiu, Q; Song, Y; Zhang, H; Zheng, H, 2018
)
0.48
" We here use a comprehensive set of in vitro and in vivo models to study the brain penetration and oral bioavailability of AZD2461."( ABCB1 Attenuates the Brain Penetration of the PARP Inhibitor AZD2461.
Beijnen, JH; Buil, LCM; Çitirikkaya, CH; de Gooijer, MC; Hermans, J; van Tellingen, O, 2018
)
0.48
" These studies demonstrated that NPT200-11 is orally bioavailable and brain penetrating and established target plasma and brain exposures for future studies of potential therapeutic benefit."( The small molecule alpha-synuclein misfolding inhibitor, NPT200-11, produces multiple benefits in an animal model of Parkinson's disease.
Bonhaus, D; Khan, A; Koike, MA; Masliah, E; Price, DL; Rockenstein, E; Wrasidlo, W, 2018
)
0.48
" The present study aimed to develop nanocrystalline solid dispersions (NSD) of HRN and evaluating the oral bioavailability in rats."( Nanocrystalline solid dispersions (NSD) of hesperetin (HRN) for prevention of 7, 12-dimethylbenz[a]anthracene (DMBA)-induced breast cancer in Sprague-Dawley (SD) rats.
Bansal, AK; Navik, U; Sheokand, S, 2019
)
0.51
"Although silybin serves as a well-known hepatoprotective agent with prominent anti-inflammatory, anti-oxidant and anti-fibrotic activities, its low bioavailability limits its application in the treatment of chronic liver diseases."( Piperine enhances the bioavailability of silybin via inhibition of efflux transporters BCRP and MRP2.
Bi, X; Liu, Z; Qu, B; Xie, Y; Yuan, Z; Zhou, H, 2019
)
0.51
"We hypothesized that inhibiting efflux transporter(s) and/or glucuronidation by piperine might enhance the bioavailability and efficacy of silybin."( Piperine enhances the bioavailability of silybin via inhibition of efflux transporters BCRP and MRP2.
Bi, X; Liu, Z; Qu, B; Xie, Y; Yuan, Z; Zhou, H, 2019
)
0.51
" This review also highlights the importance of the nanoformulation of such bioactive phytochemicals that could enhance their bioavailability by providing an efficient targeted delivery system with a reduced systemic dose while resulting in a more efficient dosing at the target site."( Combating breast cancer using combination therapy with 3 phytochemicals: Piperine, sulforaphane, and thymoquinone.
Aumeeruddy, MZ; Mahomoodally, MF, 2019
)
0.51
" Further SAR studies resulted in the discovery of the most potent modulator D11 that showed good oral bioavailability and significant in vivo therapeutic effects."( Phenotypic Screening-Based Identification of 3,4-Disubstituted Piperidine Derivatives as Macrophage M2 Polarization Modulators: An Opportunity for Treating Multiple Sclerosis.
Che, J; Dong, X; Gai, R; He, Q; Hu, Y; Lin, S; Tian, T; Wang, J; Weng, Q; Yang, B; Zhan, W; Zhang, Z; Zheng, J, 2019
)
0.51
" Ibrutinib is an orally bioavailable bruton tyrosine kinase inhibitor (BTKi) and forms an irreversible covalent bound to BTK at the Cysteine-481 residue."( Management of adverse effects/toxicity of ibrutinib.
Paydas, S, 2019
)
0.51
" Curcumin is a dietary phytochemical with hepatoprotective activities, though its low bioavailability is considered as a major challenge for clinical applications."( Curcuminoids plus piperine improve nonalcoholic fatty liver disease: A clinical trial.
Ahamdi, N; Ganjali, S; Majeed, M; Panahi, Y; Sahebkar, A; Valizadegan, G, 2019
)
0.51
"The aim of the present study was to develop modified nanoemulsions to improve the oral bioavailability and pharmacokinetics of a poor water-soluble drug, repaglinide (RPG)."( Improved oral bioavailability of repaglinide, a typical BCS Class II drug, with a chitosan-coated nanoemulsion.
Hamidi, M; Karami, Z; Nasihatsheno, N; Saghatchi Zanjani, MR, 2020
)
0.56
" Thus, the present study aimed to formulate piperine into a more solubilized form to enhance its oral bioavailability and facilitate its development as a potential anti-epileptic treatment."( Piperine-loaded nanoparticles with enhanced dissolution and oral bioavailability for epilepsy control.
Cheng, Y; Ho, NJ; Hu, M; Leung, SSY; Ren, T; Shek, TL; Xiao, M; Zhang, C; Zuo, Z, 2019
)
0.51
" Tofacitinib PK was described using a one-compartment disposition model parameterized in terms of apparent oral clearance (CL/F) and apparent volume of distribution (V/F) with first-order absorption rate (Ka) and a lag time."( Population pharmacokinetics of tofacitinib in patients with psoriatic arthritis
.
Deng, C; Kanik, KS; Menon, S; Nicholas, T; Wang, Q; Xie, R, 2019
)
0.51
" The in vivo pharmacokinetics studies showed relative bioavailability of the PEV loaded gel as 62% and 166% when compared to the oral drug and gel without vesicles respectively."( Transdermal lipid vesicular delivery of iloperidone: Formulation, in vitro and in vivo evaluation.
Bhasin, B; Londhe, VY, 2019
)
0.51
" Previously, we reported that lonafarnib, an orally bioavailable non-peptide inhibitor targeting farnesyltransferase, synergizes with sorafenib against the growth of HCC cells."( The combination of lonafarnib and sorafenib induces cyclin D1 degradation via ATG3-mediated autophagic flux in hepatocellular carcinoma cells.
Chen, D; Huang, Y; Lian, Y; Wang, J; Wei, H; Zeng, G, 2019
)
0.51
" These results suggest that MST may be effective in enhancing the bioavailability of ginkgolide A in GBE."( Mixing Ginkgo biloba Extract with Sesame Extract and Turmeric Oil Increases Bioavailability of Ginkgolide A in Mice Brain.
Ayaki, I; Iwamoto, K; Kawamoto, H; Matsumura, S; Moriyama, T; Takeshita, F; Zaima, N, 2019
)
0.51
" The rate of absorption and extent of exposure were reduced by food intake."( Pharmacokinetics and tolerability of IDP-73152 mesylate after a single oral administration under fasted and fed conditions in healthy volunteers.
An, KM; Jung, J; Lee, HS; Lee, M; Park, SI; Shin, D; Yu, KS, 2019
)
0.51
"The combination with piperine had shown a significantly higher maximum concentration in plasma approximately 1500 μg/L within 1-2 h after oral dosing, and could increase oral bioavailability of oxyresveratrol approximately 2-fold."( Comparative pharmacokinetics of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats.
Anukunwithaya, T; Junsaeng, D; Khemawoot, P; Likhitwitayawuid, K; Songvut, P; Sritularak, B, 2019
)
0.51
"Although N-methyl-d-aspartate receptor antagonists are hopeful therapeutic agents against cerebral ischemia/reperfusion (I/R) injury, effective approaches are needed to allow such agents to pass through the blood-brain barrier, thus increasing bioavailability of the antagonists to realize secure treatment."( Suppression of Cerebral Ischemia/Reperfusion Injury by Efficient Release of Encapsulated Ifenprodil From Liposomes Under Weakly Acidic pH Conditions.
Agato, Y; Asai, T; Fukuta, T; Ishii, T; Kikuchi, T; Koide, H; Oku, N; Shimizu, K; Yanagida, Y, 2019
)
0.51
" Naturally available phyto chemicals like piperine and quercetin as well as some floroquinolones are known to inhibit MDR1 and CYP3A37 activity and increases bioavailability of co-administered drugs."( Effect of piperine and quercetin alone or in combination with marbofloxacin on CYP3A37 and MDR1 mRNA expression levels in broiler chickens.
Mathapati, BS; Modi, CM; Patel, HB; Patel, UD, 2019
)
0.51
"The oral bioavailability of ibrutinib is low and variable, mainly due to extensive first-pass metabolism by cytochrome P450 (CYP) 3A4."( Itraconazole Increases Ibrutinib Exposure 10-Fold and Reduces Interindividual Variation-A Potentially Beneficial Drug-Drug Interaction.
Backman, JT; Elonen, E; Neuvonen, M; Neuvonen, PJ; Niemi, M; Olkkola, AM; Tapaninen, T; Tornio, A, 2020
)
0.56
" However, this route of administration passes through the body's first-pass metabolism which reduces the drugs' bioavailability and toxicates the liver and kidneys."( Active pulmonary targeting against tuberculosis (TB) via triple-encapsulation of Q203, bedaquiline and superparamagnetic iron oxides (SPIOs) in nanoparticle aggregates.
Ab Rahman, N; Loo, SCJ; Ostrovski, Y; Pethe, K; Poh, W; Sznitman, J, 2019
)
0.51
"1 L/h), and a poor oral bioavailability (1."( Bioanalytical method development and validation of MES207, a neuropeptide FF receptor antagonist, and its application in preclinical pharmacokinetics.
Avery, BA; Harrison, S; Kamble, SH; King, TI; McCurdy, CR; Mesangeau, C; Mottinelli, M; Roewekamp, AC; Sharma, A, 2019
)
0.51
" Moreover, the biosafety of the ternary formulation was the same as that of IBR while the in vitro performance advantage of the ternary formulation was converted into higher bioavailability in vivo experiments."( Microcrystalline cellulose as an effective crystal growth inhibitor for the ternary Ibrutinib formulation.
Gan, N; Li, H; Peng, X; Suo, Z; Tang, P; Wei, X; Zhang, M; Zhao, L, 2020
)
0.56
" However, the poor water solubility coupled with low bioavailability may inevitably hinder the application of Pip in the clinical setting."( Piperine fast disintegrating tablets comprising sustained-release matrix pellets with enhanced bioavailability: formulation,
Adu-Frimpong, M; Deng, W; Gu, Z; Xu, X; Yu, J; Zhou, G; Zhu, Y, 2020
)
0.56
"It is feasible to deliver a cytotoxic concentration of piperine to TNBC cells via NPs with the potential for improved bioavailability and solubility in biological fluids."( Delivery of Apoptosis-inducing Piperine to Triple-negative Breast Cancer Cells
Hoskin, DW; Rad, JG, 2020
)
0.56
" However, low bioavailability and severe nephrotoxicity are among the major shortcomings of AmB-based therapy."( Efficient antileishmanial activity of amphotericin B and piperine entrapped in enteric coated guar gum nanoparticles.
Goyal, N; Gupta, KC; Karthik, R; Pant, AB; Ray, L; Singh, SP; Srivastava, V, 2021
)
0.62
"5-fold increase in oral bioavailability of CBD compared to control group without piperine."( The effect of piperine on oral absorption of cannabidiol following acute vs. chronic administration.
Domb, AJ; Hoffman, A; Izgelov, D, 2020
)
0.56
" This open-label, phase I study in healthy volunteers (EudraCT 2013-003226-86) investigated its mass balance (part A) and absolute bioavailability (part B)."( Open-label, single-center, phase I trial to investigate the mass balance and absolute bioavailability of the highly selective oral MET inhibitor tepotinib in healthy volunteers.
Becker, A; Johne, A; Meyring, M; Scheible, H; van Lier, JJ; Wolna, P, 2020
)
0.56
" Unfortunately, this novel compound has poor aqueous solubility and bioavailability that limit its pharmaceutical effects."( Preparation of curcumin-poly (allyl amine) hydrochloride based nanocapsules: Piperine in nanocapsules accelerates encapsulation and release of curcumin and effectiveness against colon cancer cells.
Baydoun, E; Borjac, J; Moubarak, A; Patra, D; Slika, L, 2020
)
0.56
" The results also conclude that addressing the bioavailability of resveratrol using it in combination with piperine does not prove more efficacious in preventing lupus-associated pathologies than resveratrol alone."( Prophylactic effect of resveratrol and piperine on pristane-induced murine model of lupus-like disease.
Bhatnagar, A; Pannu, N, 2020
)
0.56
" The combination of paclitaxel (PTX) and piperine (PIP) may improve the bioavailability of paclitaxel for cancer therapy."( EGFR Targeted Paclitaxel and Piperine Co-loaded Liposomes for the Treatment of Triple Negative Breast Cancer.
Agrawal, N; Burande, AS; Jha, A; Mahto, SK; Mehata, AK; Muthu, MS; Poddar, S; Shaik, A; Viswanadh, MK, 2020
)
0.56
" It is a small synthetic molecule administered orally, with a fast bioavailability and elimination rate, predictable pharmacokinetics and lack of immunogenicity, which are convenient characteristics for both efficacy and safety."( Pharmacology and safety of tofacitinib in ulcerative colitis.
Domènech, E; Esplugues, JV; López-Sanromán, A, 2021
)
0.62
" Our prior murine modeling research observed enhanced resveratrol bioavailability with piperine co-administration."( A randomized, double-blind, dose-ranging, pilot trial of piperine with resveratrol on the effects on serum levels of resveratrol.
Ahmad, N; Bailey, HH; Havinghurst, T; Johnson, JJ; Kim, K; Lozar, T; Scarlett, CO; Wollmer, BW, 2021
)
0.62
"Low bioavailability of anti-diabetic drugs results in the partial absorption of the drug as they are mainly absorbed from the stomach and the lower part of the GIT."( Repaglinide and Metformin-Loaded Amberlite Resin-Based Floating Microspheres for the Effective Management of Type 2 Diabetes.
Jain, AK; Jain, SK; Mishra, K; Sahu, P, 2021
)
0.62
" Furthermore, in silico study showed excellent D4 bioavailability in oral administration."( The critical role of piperamide derivative D4 in the regulation of inflammatory response by the microglia and astrocytic glial cells.
Frycz, BA; Kaur, J; Shahbazi, S; Zakerali, T, 2020
)
0.56
" The present article provides a comprehensive review of PIP research in the last years concerning its chemical properties, synthesis, absorption, metabolism, bioavailability and toxicity."( Piperine: Chemical, biological and nanotechnological applications.
Araujo, VH; Chorilli, M; Quijia, CR, 2021
)
0.62
" Curcumin and piperine (1-piperoylpiperidine) interact to each other and form a π-π intermolecular complex which enhance the bioavailability of curcumin by inhibition of glucuronidation of curcumin in liver."( Therapeutic Approach against 2019-nCoV by Inhibition of ACE-2 Receptor.
Kumar, D; Kumar, G; Singh, NP, 2021
)
0.62
"Supersaturated silica-lipid hybrids have previously demonstrated improved in vitro solubilisation and in vivo oral bioavailability of poorly water-soluble drugs, however were only fabricated using a single lipid (LFCS type I formulations) and were not compared to their liquid precursors."( The Influence of Solidification on the in vitro Solubilisation of Blonanserin Loaded Supersaturated Lipid-Based Oral Formulations.
Meola, TR; Müllertz, A; Møller, A; Prestidge, CA; Schultz, HB, 2021
)
0.62
" The aim of this study was to investigate the impact of surfactant composition and surface charge of niosomes in enhancing oral bioavailability of repaglinide (REG) as a BCS II model drug."( The Impact of Surfactant Composition and Surface Charge of Niosomes on the Oral Absorption of Repaglinide as a BCS II Model Drug.
Bolourchian, N; Dadashzadeh, S; Haeri, A; Shahhosseni, S; Yaghoobian, M, 2020
)
0.56
"The modulatory effects of piperine on drug metabolizing enzymes play an important role in the control of pharmacokinetic and the bioavailability properties of the administered drugs."( The functional effects of piperine and piperine plus donepezil on hippocampal synaptic plasticity impairment in rat model of Alzheimer's disease.
Ashrafpoor, M; Esfahani, DE; Nazifi, M; Oryan, S, 2021
)
0.62
" This method has been used to quantitate these compounds in samples such as human intestinal epithelial cell lysates and mouse plasma or GI tissues in research aimed at examining the bioavailability of curcumin in the presence of piperine."( Analysis of curcumin and piperine in biological samples by reversed-phase liquid chromatography with multi-wavelength detection.
Bi, C; Hage, DS; Juritsch, AF; Kaur, H; Li, Z; Moreau, R; Rodriguez, EL; Woolfork, AG; Zhang, C, 2021
)
0.62
" However, its bioavailability in the cerebrospinal fluid (CSF) in humans has not been fully elucidated."( Activity and bioavailability of tepotinib for leptomeningeal metastasis of NSCLC with MET exon 14 skipping mutation.
Makiguchi, T; Nakagawa, J; Niioka, T; Taima, K; Tanaka, H; Tasaka, S, 2021
)
0.62
" However, its low bioavailability and long term exposure related cardiovascular side effects, limit its clinical application."( Piperine and Celecoxib synergistically inhibit colon cancer cell proliferation via modulating Wnt/β-catenin signaling pathway.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Srivastava, S; Wahajuddin, M, 2021
)
0.62
"The effect of PIP on the oral bioavailability of CXB in mice was investigated using HPLC analysis."( Piperine and Celecoxib synergistically inhibit colon cancer cell proliferation via modulating Wnt/β-catenin signaling pathway.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Srivastava, S; Wahajuddin, M, 2021
)
0.62
"PIP as a bioenhancer increased the oral bioavailability of CXB (129%)."( Piperine and Celecoxib synergistically inhibit colon cancer cell proliferation via modulating Wnt/β-catenin signaling pathway.
Chaturvedi, S; Dewangan, J; Divakar, A; Kumar, S; Mishra, S; Rath, SK; Srivastava, S; Wahajuddin, M, 2021
)
0.62
" Finally, SIAIS001 exhibited good oral bioavailability in Pharmacokinetics study."( Structure-based discovery of SIAIS001 as an oral bioavailability ALK degrader constructed from Alectinib.
Jiang, B; Kong, Y; Liu, H; Qu, X; Ren, C; Song, X; Sun, N; Yang, X; Zhong, H, 2021
)
0.62
"Iloperidone (IL) is practically insoluble in water and has significant first-pass metabolism, resulting in low oral bioavailability in humans (36%)."( Pharmacokinetic and pharmacodynamic studies of iloperidone-loaded lipid nanoemulsions via oral route of administration.
Narala, A; Suram, D; Veerabrahma, K, 2021
)
0.62
" The main objective of this research work was to improve the aqueous solubility and oral bioavailability of EBT by preparing EBT-loaded bilosomes (EBT-PC-SDC-BS)."( Improvement of solubility and dissolution of ebastine by fabricating phosphatidylcholine/ bile salt bilosomes.
Abbas, G; Ibrahim, HM; Ikram, M; Inam, S; Iqbal, MS; Irfan, M; Islam, N; Khan, IU; Mushtaq, M; Rasul, A; Rehman, MU; Syed, HK; Zahoor, AF, 2020
)
0.56
" Subsequently, nine healthy subjects received soticlestat tablets under fed and fasting conditions to assess the relative oral bioavailability and effects of food."( Safety, tolerability, pharmacokinetics, pharmacodynamics, bioavailability and food effect of single doses of soticlestat in healthy subjects.
Affinito, J; Chen, G; Cwik, M; Faessel, H; Merlo Pich, E; Wang, S, 2021
)
0.62
"The markedly low oral bioavailability of domperidone (anti-emetic drug) is associated with rapid first-pass metabolism in the intestine and liver."( Piperine phytosomes for bioavailability enhancement of domperidone.
Ghori, MU; Hussain, T; Irfan, M; Islam, N; Khan, IU; Mushtaq, M; Shahzad, Y; Yousaf, AM, 2022
)
0.72
"Alogliptin (ALG), an inhibitor of dipeptidylpeptidase-4, is used in the management of type 2 diabetes mellitus, and has a high absorption rate (>60-71%), despite its low lipophilicity (logP=-1."( Intestinal Absorption of Alogliptin Is Mediated by a Fruit-Juice-Sensitive Transporter.
Abe, M; Ishii, M; Kikuchi, T; Morimoto, K; Ogihara, T; Oikawa, E; Sasaki, M; Tomita, M, 2021
)
0.62
"This was an open-label, single-centre, phase I, bioavailability clinical trial."( Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation.
Abad-Santos, F; Arranz, P; Belmonte, C; Elgezabal, L; Fernández, N; Hernández, G; Martín-Vilchez, S; Mejía-Abril, G; Ochoa, D; Román, M, 2021
)
0.62
" KIN-8194 demonstrated excellent bioavailability and pharmacokinetic parameters, with good tolerance in rodent models at pharmacologically achievable and active doses."( The HCK/BTK inhibitor KIN-8194 is active in MYD88-driven lymphomas and overcomes mutated BTKCys481 ibrutinib resistance.
Anderson, KC; Buhrlage, SJ; Cameron, M; Castillo, JJ; Che, J; Chen, JG; Demos, MG; Gray, NS; Guerrera, ML; Hunter, ZR; Kofides, A; Liu, X; Meid, K; Munshi, M; Munshi, NC; Patterson, CJ; Tan, L; Treon, SP; Tsakmaklis, N; Wang, J; Xu, L; Yang, G, 2021
)
0.62
" In this work, we expand on the protective effects of AdipoRon in pancreatic β-cells and examine how structural modifications could affect the activity, pharmacokinetics, and bioavailability of this small molecule."( PEGylated AdipoRon derivatives improve glucose and lipid metabolism under insulinopenic and high-fat diet conditions.
Ghazvini Zadeh, E; Gordillo, R; Guo, Z; Joffin, N; Li, WH; Onodera, T; Scherer, PE; Xu, P; Yu, B, 2021
)
0.62
" Eight of these drugs inhibited the activity of the SARS-CoV-2 main protease, 3CLpro, with the most potent being masitinib, an orally bioavailable tyrosine kinase inhibitor."( Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2.
Azizi, SA; Baker, SC; Botten, JW; Brooke, CB; Bruce, EA; Chen, S; DeMarco, JK; Dickinson, BC; Drayman, N; Dvorkin, S; Firpo, MR; Froggatt, HM; Furlong, K; Han, KY; Heaton, NS; Jedrzejczak, R; Joachimiak, A; Jones, KA; Kathayat, RS; Lee, H; Maltseva, NI; Mastrodomenico, V; Meyer, B; Missiakas, D; Mounce, BC; Muñoz-Alía, MÁ; Nair, V; Nicolaescu, V; O'Brien, A; Palmer, KE; Randall, G; Schmidt, MM; Schuster, B; Severson, WE; Tan, K; Tay, S; Tomatsidou, A; Vignuzzi, M, 2021
)
0.62
" Furthermore, the nanoformulations studied to increase ibrutinib bioavailability are reported."( Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective.
Brullo, C; Russo, E; Spallarossa, A; Tasso, B; Villa, C, 2021
)
0.62
" PK studies were conducted to determine raloxifene oral bioavailability at different ages."( Age-and Region-Dependent Disposition of Raloxifene in Rats.
Du, T; Etim, I; Gao, S; Hu, M; Liang, D; Sun, R; Zheng, Z, 2021
)
0.62
" PK studies showed that the oral bioavailability of raloxifene is age dependent."( Age-and Region-Dependent Disposition of Raloxifene in Rats.
Du, T; Etim, I; Gao, S; Hu, M; Liang, D; Sun, R; Zheng, Z, 2021
)
0.62
"These findings suggested that raloxifene metabolism in the duodenum was significantly slower at young age in rats, which increased the oral bioavailability of raloxifene."( Age-and Region-Dependent Disposition of Raloxifene in Rats.
Du, T; Etim, I; Gao, S; Hu, M; Liang, D; Sun, R; Zheng, Z, 2021
)
0.62
" It was thought that the intake of bromelain could result in a decrease in the bioavailability of ALC, CER, and CRZ due to bromelain-induced alkalizing effect following digestion."( Development and validation of UPLC-MS/MS method for the simultaneous quantification of anaplastic lymphoma kinase inhibitors, alectinib, ceritinib, and crizotinib in Wistar rat plasma with application to bromelain-induced pharmacokinetic interaction.
Alanazi, AA; Almomen, A; Alzoman, NZ; Maher, HM; Shehata, SM, 2021
)
0.62
" We demonstrate that prophylactic and post-exposure therapeutic treatment with an orally bioavailable small-molecule polymerase inhibitor, ERDRP-0519, prevents measles disease in squirrel monkeys (Saimiri sciureus)."( Small-molecule polymerase inhibitor protects non-human primates from measles and reduces shedding.
Anderson, DE; Cox, RM; Kolkykhalov, AA; Mankertz, A; Natchus, MG; Pfaller, CK; Pfeffermann, K; Plemper, RK; Plesker, R; Santibanez, S; Sticher, ZM; von Messling, V; Wittwer, K; Wolf, JD, 2021
)
0.62
" We confirmed dominant role of ETA receptors in regulation of blood pressure and renal hemodynamics in normotensive and hypertensive rats and provided novel evidence for the role of ETA in control of intrarenal NO bioavailability in salt-dependent and spontaneous hypertension."( Effects of systemic and renal intramedullary endothelin-1 receptor blockade on tissue NO and intrarenal hemodynamics in normotensive and hypertensive rats.
Bądzyńska, B; Hojná, S; Kompanowska-Jezierska, E; Sadowski, J; Vaneckova, I, 2021
)
0.62
" In this work, the bioavailability and biological activities of piperine were presented and discussed."( A review on the bioavailability, bio-efficacies and novel delivery systems for piperine.
Cao, Y; Ho, CT; Huang, Q; Lu, M; Song, M; Xiao, J; Zhang, W; Zheng, Q, 2021
)
0.62
" In the present review, the chemistry and bioavailability of PIP, its molecular targets in BC, and nanotechnological strategies are discussed."( Piperine for treating breast cancer: A review of molecular mechanisms, combination with anticancer drugs, and nanosystems.
Chorilli, M; Quijia, CR, 2022
)
0.72
" The effect of spices on carotenoids' bioavailability is validated with active spice principles."( Turmeric, red pepper, and black pepper affect carotenoids solubilized micelles properties and bioaccessibility: Capsaicin/piperine improves and curcumin inhibits carotenoids uptake and transport in Caco-2 cells.
Ambedkar, R; Baskaran, V; Hanumanthappa, M; Lakshminarayana, R; Perumal, MK; Shilpa, S; Shwetha, HJ, 2021
)
0.62
"The findings indicated that the combination of PIP and UA is an effective strategy in enhancing the bioavailability and hepatoprotective potential of UA."( Synergistic effect of ursolic acid and piperine in CCl
Biswas, S; Haldar, PK; Kar, A; Mukherjee, PK; Sharma, N, 2021
)
0.62
" However, ibrutinib has very low oral bioavailability that contributes to significant variability in systemic exposure between patients, and this has the potential to affect both efficacy and toxicity."( Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition.
Baker, SD; Byrd, JC; Eisenmann, ED; Fu, Q; Garrison, DA; Jin, Y; Muhowski, EM; Sparreboom, A; Uddin, ME; Weber, RH; Woyach, J, 2021
)
0.62
" The novel combination of ATZ and PIP was proposed to enhance the bioavailability of both the compounds."( Simultaneous Method Development and Validation of Anastrozole Along with Piperine: Degradation Studies and Degradants Characterization Using LC-QTOF-ESI-MS Along with In-silico ADMET Predictions.
Alexander, A; Gajbhiye, R; Kumar, P; Mehta, P; Murty, US; Pawar, SD; Ravichandiran, V; Sarmah, B; Susanna, KJ, 2022
)
0.72
" In mice, we found tofacitinib bioavailability was 37% in both male and female mice; using these data we formulated mouse containing low and high doses of tofacitinib and found that the drug suppressed peripheral NK cell levels in a dose-dependent manner."( Tofacitinib Suppresses Natural Killer Cells
Famie, JP; Feldman, EL; Figueroa-Romero, C; Goutman, SA; Monteagudo, A; Murdock, BJ; Pacut, C; Piecuch, CE; Teener, SJ; Webber-Davis, IF, 2022
)
0.72
" However, its extensive first-pass metabolism, short-life life, and low oral bioavailability confined its medical application."( Calcium Ion-Sodium Alginate-Piperine-Based Microspheres: Evidence of Enhanced Encapsulation Efficiency, Bio-Adhesion, Controlled Delivery, and Oral Bioavailability of Isoniazid.
Jain, SP; Pandharinath, RR; Pethe, AM; Pingale, PL; Telange, DR, 2022
)
0.72
" The bioavailability of tepotinib was shown to be dose dependent, although bioavailability decreased primarily at doses above the therapeutic dose of 500 mg."( Population pharmacokinetic analysis of tepotinib, an oral MET kinase inhibitor, including data from the VISION study.
Girard, P; Jonsson, EN; Papasouliotis, O; Strotmann, R; Xiong, W, 2022
)
0.72
" Bioavailability increased by 49% with food compared with when fasted."( Population pharmacokinetic and pharmacodynamic modeling of evobrutinib in healthy adult participants.
Dyroff, M; Girard, P; Mitchell, D; Papasouliotis, O, 2022
)
0.72
" During its clinical development, a stable isotopologue of ibrutinib was required for the assessment of the drug's absolute oral bioavailability via intravenous microdosing."( Carbon-13 labeling of ibrutinib for human microdosing.
Gong, Y; Salter, R, 2023
)
0.91
" However, poor oral bioavailability and permeability of curcumin are a major challenge for formulation scientists."( Formulation and Development of Curcumin-Piperine-Loaded S-SNEDDS for the Treatment of Alzheimer's Disease.
Ahmad, S; Hafeez, A, 2023
)
0.91

Dosage Studied

ExcerptRelevanceReference
" 4 The dose-response curve for the pressor action of Wy 20051 was potentiated in reserpine-treated anaesthetized rats."( The evaluation of the novel pressor activity of gamma-piperidinobutyramide (WY 20051, DF480).
Alps, BJ; Devoy, PW; Waterfall, JF, 1976
)
0.26
" On the last three dosage schedules inhibition persisted for at least 12 h after the final dose."( Inhibitory activity of terfenadine on histamine-induced skin wheals in man.
Barraud, N; Burke, JT; Hüther, KJ; Koch-Weser, J; Renftle, G, 1977
)
0.26
" At least 90% of the radioactivity in the tissues at 2 hr after dosing was identified as parent compound by thin-layer chromatography."( The disposition of threo-alpha-(2-piperidyl)-2-trifluoromethyl-6-(4-trifluoromethylphenyl)-4-pyridinemethanol phosphate in mice.
Chung, H; Gillum, HH; Rozman, RS,
)
0.13
" The treatment comprised four periods in which the maximum tolerated daily dosage, the optimal weekly dosage (mean: 20."( Clinical experiments with the new oral long-acting neuroleptic clopimozide (R 29 764).
Floru, L; Tegeler, J, 1978
)
0.26
" 6 In isolated strips of cat splenic capsule, piperoxan produced a shift to the right of the dose-response curve to noradrenaline with no change of the maximum response."( The effects of piperoxan on uptake of noradrenaline and overflow of transmitter in the isolated blood perfused spleen of the cat.
Blakeley, AG; Summers, RJ, 1978
)
0.26
" At both 24 and 48 hr after dosing the majority of radiolabel remaining in the body was in the form of parent drug."( The absorption, distribution, and excretion in mice of the antimalarial mefloquine, erythro-2,8-bis(trifluoromethyl)-alpha-(2-piperidyl)-4-quinolinemethanol hydrochloride.
Koby, R; Molek, NA; Rozman, RS,
)
0.13
" The dosage level was, on weight basis, a little higher than the standard dosage for adults."( The protective effect of a new agent, ketotifen syrup, in the treatment of childhood asthma.
Lykkegaard Nielsen, EA; Osterballe, O, 1979
)
0.26
" Furthermore, the enhanced toxicity of pilocarpine caused by bamipine in a defined dosage range is antagonized by biperiden in a dose related manner."( [Central and peripheral interactions of the antiparkinson agent biperiden and the antihistaminic bamipin on the rat excited by pilocarpine].
Hofmann, HP; Kreiskott, H, 1978
)
0.26
"In a preliminary study which lasted 14 weeks, an anti-anginal preparation, perhexiline maleate (Pexid), was prescribed in a dosage of 200 mg twice a day to 7 patients who were suffering from cardiac arrhythmias associated with ischaemic heart disease."( The anti-arrhythmic effects of perhexiline maleate in patients with ischaemic heart disease.
Gitlin, N, 1975
)
0.25
" Although a relatively high chosen dosage of ketotifen was given, it does not seem capable of inhibiting mediator release from the bronchial mast-cells as DSCG does."( [Protection from exertion-induced bronchial asthma with disodium cromoglycate (DSCG) (cromolyn, lomudal, intal) and with ketotifen (zaditen). Doubly crossed double-blind study ].
Gmür, H; Scherrer, M, 1979
)
0.26
"Using measures of locomotor activity and stereotypy, dose-response curves to several psychomotor stimulant drugs were obtained on rats reared in deprived or normal environments."( The effects of psychomotor stimulants on stereotypy and locomotor activity in socially-deprived and control rats.
Iversen, SD; Morgan, MJ; Robbins, TW; Sahakian, BJ, 1975
)
0.25
" Statistical tests of parallelism revealed a significant difference between the log dose-response curves of Sch 15280 and ephedrine but not between those of Sch 15280, atropine and aminophylline."( Experimental study of a potential anti-asthmatic agent: SCH 15280.
Adams, GK; Bleidt, B; Diamond, L; Williams, B, 1975
)
0.25
" At this dosage schedule, delayed-type hypersensitivity responses to the same antigen were not affected."( Effect of mefloquine on the immune response in mice.
Ferrante, A; O'Keefe, DE; Rowan-Kelly, B; Thong, YH, 1979
)
0.26
" Its effect (in the dosage used) on the tyramine dose--pressor response and NA dose--pressor response tests were less than those of amitryptyline."( Antidepressant evaluation and the pharmacological actions of FG4963 in depressive patients.
Coppen, A; Ghose, K; Gupta, R; Lund, J, 1977
)
0.26
" In acute diarrhoea, loperamide provides more rapid control of symptoms than diphenoxylate when given in a flexible dosage according to unformed bowel movements, and in single dose studies 4mg loperamide has a much longer duration of effect than 5mg diphenoxylate."( Loperamide: a review of its pharmacological properties and therapeutic efficacy in diarrhoea.
Avery, GS; Brogden, RN; Heel, RC; Speight, TM, 1978
)
0.26
" The mean dosage of Penfluirdol was 22 up to 28 mg per week."( [Penfluridol. Results of a year-long clinical trial].
Woggon, B, 1978
)
0.26
" After the single intravenous dose total plasma clearance (Cl) ranged from 570 to 1670 ml/min (988 +/- 425 ml/min) while after multiple dosing Cl decreased to 666 +/- 27 ml/min."( Disposition and antiarrhythmic effect of lorcainide.
Heimburg, P; Klotz, U; Müller-Seydlitz, P, 1979
)
0.26
" This frequency of dosing is consistent with the pharmacokinetic behavior of the drug in man, and does not appear to result in any inappropriate accumulation of the drug in patients."( Penfluridol: a neuroleptic drug designed for long duration of action.
Grindel, JM; Heykants, JJ; Janssen, PA; Migdalof, BH, 1979
)
0.26
" Excretion of approximately 1 per cent of the dose in the urine as unchanged loperamide after seven days was observed independent of the particular dosage form that was administered."( Human pharmacokinetics and comparative bioavailability of loperamide hydrochloride.
Fuller, BL; Killinger, JM; Weintraub, HS, 1979
)
0.26
" The solvent systems and spray reagents described should be useful for the identification of these drugs in various dosage forms."( TLC differentiation of butyrophenone and diphenylbutylpiperidine compounds from phenothiazine derivatives.
Pluym, A, 1979
)
0.26
" In the course of the chronic experiments, in the highest dosage group of rats a slight sedation and a decrease of body weight gain and food intake could be observed."( [Toxicological study on piprozoline (author's transl)].
Herrmann, M; Leuschner, F; Wiegleb, J, 1977
)
0.26
"Studies of hexobarbital sleeping time in rats showed that only a very high dosage of ethyl(Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)-acetate (piprozoline, Gö 919, Problin) (500 mg/kg) produced a weak interaction with the metabolism of hexobarbital; no signs of any induction of the oxidative enzyme system were observed until 4 days after pre-treatment with 3 X 250 mg/kg."( [Studies on the influence of piprozoline on the microsomal enzyme system of the rat liver (author's transl)].
Friedrich, G; Vollmer, KO, 1977
)
0.26
" Side-effects, which mainly occurred during the last weeks of the experiment in the highest dosage group, were most probably due to the exhaustion of the fluid and especially of the electrolyte reserves of the animals."( [Toxicological studies on Etozolin (author's transl)].
Herrmann, M; Leuschner, F; Wiegleb, J, 1977
)
0.26
" Diarrhea was controlled with a median dosage of three capsules (6 mg total dose) and a range of two to 12 capsules."( The control of acute diarrhea in a large industrial plant.
Martins, JK; Roedl, G, 1978
)
0.26
" In healthy subjects, gastrointestinal symptoms limited single-day dosage of WR 122,455 to 800 mg and WR 171,669 to 1,260 mg."( Evaluation of two phenanthrenemethanols for antimalarial activity in man: WR 122,455 and WR 171,669.
Arnold, J; Canfield, CJ; Rinehart, J, 1976
)
0.26
" For penfluridol, a significant correlation between dosage and plasma level and also between dosage and changes in psychopathology as regards factor 5 in the Märtens & Jonsson S scale which comprises the items most characteristic of a schizophrenic syndrome, was found."( Penfluridol and thiothixene. Dosage, plasma levels and changes in psychopathology.
Edenius, B; Jacobsson, L; Kettner, B; Magnusson, KE; Mattsson, B; Mjörndal, T; Oreland, L; Perris, C; Rapp, W; Villemoes, P; von Knorring, L, 1976
)
0.26
" This study indicates that low doses of piperazinedione can produce variable and severe myelosuppression when used in combination with other myelosuppressive agents, and that only small increments in dosage may produce marked increases in the degree of myelosuppression."( Severe myelosuppression from piperazinedione, (NSC No. 135758), cyclophosphamide plus dimethyl-triazeno-imidazole carboxamide (DTIC).
Klahr, C; Presant, CA, 1977
)
0.26
" The optimal dosage range for severely ill schizophrenic patients appears to be between 100 and 600 mg once monthly."( Pipotiazine palmitate: an evaluation of a new long acting intramuscular antipsychotic agent in severely ill schizophrenic patients.
Bishop, G; Gallant, DM; Guerrero-Figueroa, R; Mielke, D; Oelsner, T, 1975
)
0.25
" The same dosage (in 70% of the patients from 40 to 80 mg) of penfluridol was used per week as was employed for flupenthixol decanoate per fortnight."( Peroral and parenteral administration of long-acting neuroleptics: a double-blind study of penfluridol compared to flupenthixol decanoate in the treatment of schizophrenia.
Gerlach, J; Kramp, P; Kristjansen, P; Lauritsen, B; Lühdorf, K; Munkvad, I, 1975
)
0.25
" The data obtained from this study have tended to confirm the impression of previous investigators that penfluridol, administered in a dosage of 40 to 80 mg on a once-a-week basis in a single dose, compares favorably with the antipsychotic activity of those neuroleptics requiring administration on a daily basis."( Penfluridol: a long-acting oral neuroleptic. A controlled study.
Kurland, AA; Ota, KY; Slotnick, VB,
)
0.13
"Twenty-two hospitalized schizophrenic patients, participating in a large-scale phase II double-blind dose-effect study (30, 60, and 120 mg weekly) of penfluridol, a new diphenylbutylpiperidine neuroleptic, were maintained on a regular dosage regimen for 13 wk."( Penfluridol steady-state kinetics in psychiatric patients.
Albert, JM; Bertrand, M; Cooper, SF; Dugal, R, 1975
)
0.25
" In this dosage it was found that the peak effect of the two drugs was the same but that the effect of rimiterol was less prolonged than that of sulbutamol."( Comparison between the bronchodilator and cardiovascular effects of inhaling 0.5 mg. rimiterol ('Pulmadil') and 0.2 mg. salbutamol.
Bianco, S; Kamburoff, PL; Prime, FJ, 1975
)
0.25
" The log dose-response curve of ergotamine was bell-shaped."( Analysis of ergotamine - 5-HT interaction on the isolated rat stomach preparation.
Frankhuijzen, AL, 1975
)
0.25
" Cebocephaly, harelip/cleft palate, exencephaly, and a cranial bled were the common deformities produced by dosing on the seventh day of gestation."( Teratogenic effects of cyclopamine and jervine in rats, mice and hamsters.
Keeler, RF, 1975
)
0.25
" For the inhibition of the hypotensive action of clonidine by protriptyline a parallel shift of the dose-response curve was obtained, indicating the possibility of a competitive antagonism."( Interaction between centrally acting hypotensive drugs and tricyclic antidepressants.
van Zwieten, PA, 1975
)
0.25
" There were controlled: blood-pressure, pulse, respiration, common dosing of the narcotica, dosing of the analgetica, and the patients' post-operative condition."( [Clinical studies on the use of neuroleptanalgesia in Wertheim's abdominal radical surgery].
Krafft, W; Laube, R; Schmidt, D, 1975
)
0.25
"), the respondings were inhibited in proportion to the dosage except in DRL performance, in which only correct response rate decreased at 8 mg/kg."( [Effects of penfluridol, a psychotropic agent, on operant behavior of rats].
Kuribara, H; Okuizumi, K; Shirota, M; Tadokoro, S, 1975
)
0.25
" All these antagonists caused a concentration-dependent rightward shift of the dose-response curve for carbachol-stimulated amylase release without altering the maximal response."( Characterization of muscarinic receptor subtypes on rat pancreatic acini: pharmacological identification by secretory responses and binding studies.
Kashima, K; Kataoka, K; Kato, M; Kuriyama, K; Ohkuma, S, 1992
)
0.28
" In dose-response studies, ifenprodil attenuated the NMDA-induced increase in medium GABA at all ages tested with an Imax of 10 microM."( Developmental differences in antagonism of NMDA toxicity by the polyamine site antagonist ifenprodil.
Nicklas, WJ; Zeevalk, GD, 1992
)
0.28
" The dose-response curve for AVP was shifted to the right in parallel by OPC-31260 but not by OPC-21268."( Potent antagonistic action of OPC-31260, a vasopressin V2 receptor antagonist, on [Arg8]vasopressin-induced vasoconstriction in isolated simian femoral arteries.
Chiba, S; Tsukada, M, 1992
)
0.28
" Estradiol also shifted the dose-response curve for GnRH-stimulated inositol phosphate (IP) accumulation rightward, increasing the EC50 for this GnRH effect by approximately 20-fold."( Estradiol regulates gonadotropin-releasing hormone receptor number, growth and inositol phosphate production in alpha T3-1 cells.
Gröner, I; McArdle, CA; Poch, A; Schomerus, E, 1992
)
0.28
" Combinations of ZOL and 2DG produced supraadditive antinociception, even though ZOL failed to significantly shift the 2DG dose-response curve to the left."( Potentiation of 2-deoxy-D-glucose antinociception, but not hyperphagia by zolantidine, a histamine (H2) receptor antagonist.
Bodnar, RJ; Hough, LB; Koch, JE, 1992
)
0.28
"Irreversible inactivation of striatal D2 dopamine (DA) autoreceptors with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) or inactivation of striatal guanine nucleotide binding proteins (G proteins) with pertussis toxin (PT) shifted the dose-response curve for N-n-propylnorapomorphine (NPA)-mediated inhibition of gamma-butyrolactone (GBL)-induced elevation of L-3,4-dihydroxyphenylalanine (L-DOPA) to the right, with a decrease in the maximum response."( The effects of pertussis toxin on dopamine D2 and serotonin 5-HT1A autoreceptor-mediated inhibition of neurotransmitter synthesis: relationship to receptor reserve.
Bohmaker, K; Bordi, F; Meller, E, 1992
)
0.28
"Akin to receptor inactivation with phenoxybenzamine (PBZ) (1 microM, 1 hr), treatment of anterior pituitary cells with 17 beta-estradiol (10 nM, 3 days) right-shifted the dose-response curve for inhibition of prolactin (PRL) secretion by the full agonist R-(-)-N-n-propylnorapomorphine (NPA) and reduced the maximal effect [EC50 (pM) and percent maximal effect: control, 25."( Comparative effects of receptor inactivation, 17 beta-estradiol and pertussis toxin on dopaminergic inhibition of prolactin secretion in vitro.
Bohmaker, K; Diamond, J; Lieu, HD; Meller, E; Puza, T, 1992
)
0.28
"The effects of cisapride, given orally at standard therapeutic dosage (10 mg tds), on proximal small bowel interdigestive motility in ten healthy volunteers was assessed by prolonged ambulatory manometry."( Assessment by prolonged ambulatory manometry of the effect of oral cisapride on proximal small bowel inter-digestive motility.
Benson, MJ; Castillo, FD; Deeks, JJ; Wingate, DL, 1992
)
0.28
" Based on pharmacokinetic considerations, the dosage of pirmenol is unlikely to differ in young and elderly subjects."( Pharmacokinetics of pirmenol in young and elderly subjects.
Beasley, M; Bland, R; Campbell, AJ; Edwards, IR; Ferry, DG; Gazeley, L, 1992
)
0.28
" At a higher concentration (20 microM), effects of RP 62719 on inotropy and lusitropy were less marked, thus accounting for the bell-shaped form of the dose-response curve."( Positive inotropic effects of RP 62719, a new pure class III antiarrhythmic agent, on guinea pig myocardium.
Beregi, JP; Chemla, D; Coudray, N; Escande, D; Lecarpentier, Y; Mery, P; Mestre, M, 1992
)
0.28
" The muscarinic antagonists pirenzepine, (+-)-5,11-dihydro-11-[[[2-[2-((dipropylamino)methyl)-1-piperidinyl] ethyl]amino]-carbonyl]-6H-pyrido(2,3-b)(1,4)-benzodiazepin-6-one (AF-DX 384), 11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11-dihydro- 6H-pyrido(2,3-b)(1,4)-benzodiazepin-6-one (AQ-RA 741), p-fluorohexahydro-sila-difenidol (p-F-HHSiD), 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP) and (R)- and (S)-hexahydro-difenidol [(R)-HHD, (S)-HHD] shifted the muscarine, methacholine or carbachol dose-response curve to the right in a competitive manner."( Characterization of muscarinic receptors mediating vasodilation in guinea-pig ileum submucosal arterioles by the use of computer-assisted videomicroscopy.
Bungardt, E; Feifel, R; Lambrecht, G; Moser, U; Mutschler, E; Surprenant, A; Tacke, R; Vockert, E, 1992
)
0.28
" Log ID50s calculated for the antagonists from the dose-response curves were found to correlate significantly with the log Kis of the antagonists for the muscarinic M3 receptor subtype."( Pressor response to posterior hypothalamic administration of carbachol is mediated by muscarinic M3 receptor.
Martin, JR, 1992
)
0.28
"The dose regimen for paroxetine in the treatment of depression has been well established through a number of individual dosing studies and analyses from the worldwide clinical data base."( Optimal dose regimen for paroxetine.
Dunbar, GC; Dunner, DL, 1992
)
0.28
" The nausea rarely leads to drug discontinuation or even dosage reduction."( An overview of paroxetine.
Boyer, WF; Feighner, JP, 1992
)
0.28
" One female in the high dosage group died on Gestation Day 12."( Evaluation of teratogenic potential of N-formylpiperidine in rats.
Alvarez, L; Johannsen, FR; Nair, RS, 1992
)
0.28
" In tissues precontracted with methacholine, 11-([[2-(diethylamino)methyl]-1-piperidinyl]acetyl)5,11- dihydro-6H-pyrido[2,3-6][1,4]benzodiazepine-6-one (AF-DX 116), a selective M2 antagonist, shifted dose-response curves to both isoproterenol and forskolin significantly to the left."( M2 muscarinic receptors inhibit isoproterenol-induced relaxation of canine airway smooth muscle.
Fernandes, LB; Fryer, AD; Hirshman, CA, 1992
)
0.28
" 4-PIOL antagonized the response to isoguvacine with a parallel shift to the right of the dose-response curve."( Electrophysiological studies of the GABAA receptor ligand, 4-PIOL, on cultured hippocampal neurones.
Falch, E; Kristiansen, U; Krogsgaard-Larsen, P; Lambert, JD, 1991
)
0.28
" Following BMY-25368 administration, hydrogen ion concentration was decreased and mean pH was higher than baseline values in a dose-response pattern."( Effects of a histamine type-2 receptor antagonist (BMY-25368) on gastric secretion in horses.
Dreyfuss, DJ; Orsini, JA; Spencer, PA; Uhlman, R; Vecchione, J, 1991
)
0.28
" The importance of the time of dosing of potent, long-acting H2 blockers for optimal suppression of intragastric acidity is unknown."( Is the time of dosing of a potent long-acting H2-receptor antagonist critical? Twenty-four-hour pH measurements with SKF-94482.
Merki, HS; Wilder-Smith, CH, 1991
)
0.28
" Furthermore, pretreatment with the drug did not affect the dose-response curve for the inhibitory effects of the DA receptor agonist apomorphine or the mixed DA agonist/sigma-receptor ligand (+)-3-(3-hydroxyphenyl)-N-1-propyl)piperidine ((+)-3-PPP)."( Sigma-receptors: implication for the control of neuronal activity of nigral dopamine-containing neurons.
Engberg, G; Wikström, H, 1991
)
0.28
" The dose-response curve of haloperidol remained virtually unchanged, apparently because of the potent dopamine-D2 antagonism associated with these doses which may block the potentiating effect of apomorphine."( Functional interaction between serotonin-S2 and dopamine-D2 neurotransmission as revealed by selective antagonism of hyper-reactivity to tryptamine and apomorphine.
Awouters, F; Janssen, PA; Megens, AA; Niemegeers, CJ, 1990
)
0.28
" Low concentrations of pirenzepine (10(-8) M), produced a rightward shift in the dose-response curve to McN, without inhibiting responses to carbachol."( Functional subtyping of muscarinic receptors on canine esophageal mucosa.
Donoff, B; Lad, R; Rangachari, PK, 1991
)
0.28
" Cisapride dosage adjustment or substitution after hemodialysis is not necessary."( Pharmacokinetics and pharmacodynamics of cisapride in patients undergoing hemodialysis.
Bares, R; Dakshinamurty, KV; Gladziwa, U; Ittel, TH; Klotz, U; Seiler, KU; Sieberth, HG, 1991
)
0.28
"In order to elucidate the interaction between cyproheptadine (CPH) and tipepidine (TP), the disposition of CPH and its metabolites from plasma and the hepatic drug metabolizing enzyme activities in rats dosed singly or repeatedly were investigated."( Drug interaction between cyproheptadine and tipepidine. Effect of single and repeated administrations.
Fujii, Y; Iwaki, M; Ogiso, T; Tanino, T; Yamashita, K, 1991
)
0.28
" Alinidine (10(-6) M) shifted the dose-response curves of acetylcholine and carbachol to the right, but it did not affect those for isosorbide dinitrate, isoproterenol and adenosine."( Anti-muscarinic effect of alinidine on acetylcholine-induced vasodilation in isolated and perfused dog coronary arteries.
Chiba, S; Furukawa, Y; Nakane, T, 1991
)
0.28
"5 mg/kg body weight) of the compound administered on days 1, 2 or 3 of pregnancy or multiple dosing (0."( Biological profile of 2-[4-(2-N-piperidinoethoxy) phenyl]-3-phenyl (2H) benzo (b) pyran--a potent antiimplantation agent in rat.
Dhar, JD; Duran, S; Kapil, RS; Setty, BS, 1991
)
0.28
" Plasma concentrations of paroxetine at steady state (8-147 ng/ml) were in the normal range for a 30-mg daily dosing regimen."( No influence of the antidepressant paroxetine on carbamazepine, valproate and phenytoin.
Andersen, BB; Dam, M; Kristensen, HB; Lund, J; Mengel, H; Mikkelsen, M; Pedersen, B; Vesterager, A,
)
0.13
" A clear dose-response relationship was found for ritanserin with higher doses evoking increased duration of slow wave sleep."( A dose-response study examining the effects of ritanserin on human slow wave sleep.
Idzikowski, C; James, RJ; Mills, FJ, 1991
)
0.28
" Post-evening meal (PEM) dosing of H2-receptor antagonists appears to be a rational method of suppressing late evening gastric acidity, but on balance the symptomatic response of twice daily dosing is superior to once daily dosing."( Reflux esophagitis.
Nio, CY; Schotborgh, RH; Tytgat, GN, 1990
)
0.28
" Oxotremorine-induced tremor and salivation in mice were delayed after extremely high dosage of levocabastine; however, these were much less effective than those seen after diphenhydramine and ketotifen."( Central effect of the potent long-acting H1-antihistamine levocabastine.
Aoki, I; Kamei, C; Tasaka, K; Tsujimoto, S; Yoshida, T, 1990
)
0.28
" On day 1 and 15 of dosing with each regimen, each subject's 24-h ambulatory intragastric acidity was measured by radiotelemetry and 24-h plasma gastrin profiles were derived from hourly venous blood samples."( The effects of 15 days of dosing with placebo, sufotidine 600 mg nocte or sufotidine 600 mg twice daily upon 24-hour intragastric acidity and 24-hour plasma gastrin.
Holmfield, JH; Johnston, D; Primrose, JN; Rogers, MJ, 1990
)
0.28
" In neither study were there any significant differences between the acid secretory dose-response curves to histamine in control and test animals."( Chronic administration of H2-antagonists does not alter gastric secretory responses to histamine, or the antisecretory activity of sufotidine.
Humphray, JM; Reeves, JJ; Stables, R, 1990
)
0.28
"; this dosage could be changed if necessary."( "Prokinetic" treatment of constipation-predominant irritable bowel syndrome: a placebo-controlled study of cisapride.
Milo, R; Toussaint, J; Van Eeghem, P; Van Outryve, M, 1991
)
0.28
" Dose-response curves were constructed, and the IC50s determined for 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP), pirenzepine (PRZ) and 11-2[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11,-dihydro- 6H-pyrido[2,3-b] [1,4]benzodiazepin-6-one (AF-DX 116) were 72 nM, 385 nM, and 24 microM, respectively."( Activation of the pharmacologically defined M3 muscarinic receptor depolarizes hippocampal pyramidal cells.
Alger, BE; Pitler, TA, 1990
)
0.28
" The volume of distribution (Vd) was evaluated in the rats by intravenous dosage of 150 mg/kg of 3H-A10 dissolved in dimethyl sulfoxide."( Pharmacokinetic study of radioactive antineoplaston A10 in rats and mice.
Wang, H; Xu, W; Yuan, Y, 1990
)
0.28
" The primary adverse events associated with serotonin reuptake inhibitors involve the gastrointestinal system, although side effects may be less frequent at lower dosage levels."( Clinical overview of serotonin reuptake inhibitors.
Rickels, K; Schweizer, E, 1990
)
0.28
" All the antagonists shifted the methacholine dose-response curve to the right in a parallel and concentration-dependent fashion, yielding Schild plots with slopes not significantly different from unity."( Characterization of the muscarinic receptor subtype involved in phosphoinositide metabolism in bovine tracheal smooth muscle.
Elzinga, CR; Meurs, H; Roffel, AF; Zaagsma, J, 1990
)
0.28
" Thioperamide did not alter the dose-response curve to exogenous histamine (0."( Histamine H3 receptors modulate antigen-induced bronchoconstriction in guinea pigs.
Barnes, PJ; Ichinose, M, 1990
)
0.28
"The pathophysiology, diagnosis, and treatment of diabetic gastroparesis are reviewed, and the mechanisms of action, pharmacokinetics, clinical efficacy, adverse effects, and dosage of metoclopramide, domperidone, and cisapride are described."( Use of metoclopramide, domperidone, and cisapride in the management of diabetic gastroparesis.
Brown, CK; Khanderia, U, 1990
)
0.28
" Dose-response curves for inhibition of choline transport by A-5 and HC-3 were not changed by a 24-hr pre-exposure of the cells to each inhibitor."( Characterization of the effect of two 4-methyl piperidine derivatives of hemicholinium-3, A-4 and A-5, on choline transport.
Long, JP; Sheff, KY; Yorek, MA, 1990
)
0.28
" We conclude that in the dosage used, long-term treatment with cisapride appears to improve chronic abdominal symptoms in patients with cystic fibrosis and DIOS, but fails to abolish the need for intestinal lavage."( Effects of cisapride in patients with cystic fibrosis and distal intestinal obstruction syndrome.
Corey, M; Durie, PR; Ellis, L; Koletzko, S; Spino, M; Stringer, DA, 1990
)
0.28
" Scopolamine hydrobromide reinstated contralateral placing errors in infarcted rats at a dosage that did not affect neurologically intact rats."( Ionic channels, cholinergic mechanisms, and recovery of sensorimotor function after neocortical infarcts in rats.
De Ryck, M; Duytschaever, H; Janssen, PA; Pauwels, PJ, 1990
)
0.28
" Chickens (9/10) and quails (8/10) dosed at 50 mg/kg body weight were affected, and several birds of each species died (2/10 and 5/10, respectively)."( Comparative toxicity of coniine, an alkaloid of Conium maculatum (poison hemlock), in chickens, quails, and turkeys.
Frank, AA; Reed, WM,
)
0.13
" However, in goats gavaged with fresh Conium plant, fetal movement was inhibited for only about 5 hours after each individual dosage and gradually returned to control levels 12 hours after dosing."( Multiple congenital contractures (MCC) and cleft palate induced in goats by ingestion of piperidine alkaloid-containing plants: reduction in fetal movement as the probable cause.
Bunch, TD; Callan, RJ; Keeler, RF; Panter, KE; Sisson, DV, 1990
)
0.28
" 24 h treatment of pituitary cell cultures with increasing concentrations of Phr led to a stimulatory effect on GnRH-stimulated LH secretion an effect that occurred at 10 microM got maximal at 100 microM and was lost at higher concentrations resulting in a bell-shaped dose-response curve."( Weak estrogenic activity of phenol red in the pituitary gonadotroph: re-evaluation of estrogen and antiestrogen effects.
Emons, G; Knuppen, R; Ortmann, O; Sturm, R, 1990
)
0.28
"In the spontaneously hypertensive rat (SHR), ketanserin and the ketanserin analogues R56413 and ritanserin were studied with regard to their ability to reduce the blood pressure in conscious rats and shift the dose-response curves for phenylephrine and serotonin (5-HT) in pithed rats after acute administration."( Antihypertensive effects of ketanserin in the spontaneously hypertensive rat: mode of action.
Gradin, K; Hedner, T; Persson, B; Pettersson, A, 1985
)
0.27
" The dose-response curve of blood pressure against rate of phenylephrine infusion was shifted to the right in keeping with alpha 1-adrenergic antagonism; the degree of shift was small compared with that after prazosin."( Ketanserin and alpha 1-adrenergic antagonism in humans.
Ball, SG; Robertson, JI; Zabludowski, JR, 1985
)
0.27
" Dosage in excess of 60 mg of Kn per day caused troublesome central nervous system symptoms or headache in some patients."( Clinical studies with ketanserin in hypertension.
Brown, SA; Simpson, FO; Spears, GF; Waal-Manning, HJ, 1985
)
0.27
" In vitro dose-response curves suggested that prolonged ketanserin intake results in a higher "sensitivity" of the platelets to serotonin rather than a refractoriness of the platelets to ketanserin."( Platelet hypersensitivity to serotonin after prolonged ketanserin intake?
Amery, A; Arnout, J; Deckmyn, H; Fiocchi, R; Lijnen, P; Van Russelt, M; Vermylen, J, 1985
)
0.27
" Bucindolol caused a parallel shift to the right of the dose-response curves for both serotonin (5-HT) and phenylephrine (PE), indicating competitive antagonism."( Bucindolol has serotonin and alpha-adrenoceptor blocking properties.
Marwood, JF; Stokes, GS, 1985
)
0.27
" 4-DAMP (10(-9) to 10(-6) M) caused a progressive parallel rightward shift in the acetylcholine dose-response curve without a change in maximal amylase release."( Muscarinic receptor subtypes on rat pancreatic acini: secretion and binding studies.
Louie, DS; Owyang, C, 1986
)
0.27
" produced a two-fold shift to the right of the dose-response curve of locally infused 5-hydroxytryptamine (5-HT) but increased only slightly the ED50 of locally infused pizotifen."( Pizotifen, an antimigraine drug with venoconstrictor activity in vivo.
Müller-Schweinitzer, E,
)
0.13
" At a daily dosage of 200 to 400 mg, pirmenol was effective in suppressing VPCs."( A multicenter dose-response study of pirmenol hydrochloride in patients with ventricular premature contractions.
Farnham, DJ, 1987
)
0.27
" Whereas the blood pressure reduction to acute administration of ketanserin was directly related to its ability to shift the dose-response curve of phenylephrine (alpha 1-adrenergic blockade), the same relationship was not apparent following chronic treatment with ketanserin."( Antihypertensive effects of ketanserin and ritanserin in the spontaneously hypertensive rat.
Gradin, K; Hedner, T; Persson, B; Pettersson, A, 1988
)
0.27
" Cumulative dose-response curves were constructed for either cinanserin or 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) in animals that had received a maximal hypotensive dose of prazosin that had, in addition to decreasing blood pressure, decreased heart rate and background activity in all three nerves."( Are drugs that act both on serotonin receptors and alpha 1-adrenoceptors more potent hypotensive agents than those that act only on alpha 1-adrenoceptors?
Ramage, AG, 1988
)
0.27
"The possible neurotoxic effects of the alpha-ethyl homologue of MDMA, N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), were examined following a regimen of twice daily dosing for four days."( Neurotoxic effects of the alpha-ethyl homologue of MDMA following subacute administration.
Johnson, MP; Nichols, DE, 1989
)
0.28
" Elimination half-lives also showed variability between these elderly patients, but tended to be longer after cessation of multiple dosing than after a single dose."( Paroxetine: pharmacokinetic and antidepressant effect in the elderly.
Fjord-Larsen, T; Lundmark, J; Manniche, PM; Mengel, H; Møller-Nielsen, EM; Pauser, H; Scheel Thomsen, I; Wålinder, J, 1989
)
0.28
" The often discussed intrinsic estrogen activity of the antiestrogens was present only in the highest dosage tested of tamoxifen."( Antiestrogen and antiandrogen administration reduce bone mass in the rat.
Bauss, F; Feldmann, S; Lempert, UG; Minne, HW; Parvizi, S; Pfeifer, M; Ziegler, R, 1989
)
0.28
"Evening dosing has become standard for H2 receptor antagonists, because available agents inhibit nocturnal basal acid secretion more effectively than daytime stimulated secretion."( Do H2 receptor antagonists have to be given at night? A study of the antisecretory profile of SKF 94482, a new H2 receptor antagonist which has a profound effect on daytime acidity.
Burget, DW; Chiverton, SG; Hunt, RH, 1989
)
0.28
" The absence of a depression of the maximum of the dose-response curve of ST 587 and the very moderate attenuation of the maximal B-HT 920-induced increase in diastolic blood pressure (BP) confirms the lack of major calcium entry blocking properties of R 56865 for alpha-adrenoceptor-activated calcium channels in vitro."( Interaction between R 56865 and alpha-adrenoceptors in the pithed rat.
Fruh, C; Koch, P; Peters, T; Schneider, J; Wilffert, B; Wilhelm, D,
)
0.13
" Its dose-response curve was bell-shaped with maximal effects at a dose of 100 micrograms/kg."( Occurrence of yawning and decrease of prolactin levels via stimulation of dopamine D2-receptors after administration of SND 919 in rats.
Domae, M; Furukawa, T; Matsumoto, S; Nagashima, M; Shirakawa, K; Yamada, K, 1989
)
0.28
" Dinnertime dosing of cimetidine appears to be a rational method of suppressing late-evening gastric acidity."( Drug therapy of reflux oesophagitis: an update.
Tytgat, GN, 1989
)
0.28
", was not greater than that of placebo, and dose-response as well as longer term trials are necessary to determine the clinical efficacy of this medication."( Effect of six weeks of treatment with cisapride in gastroparesis and intestinal pseudoobstruction.
Abell, TL; Brown, ML; Camilleri, M; Hench, V; Malagelada, JR; Zinsmeister, AR, 1989
)
0.28
" CGS 19755 was studied using single and cumulative dosing procedures up to a dose of 10."( The competitive N-methyl-D-aspartate (NMDA) antagonist CGS 19755 attenuates the rate-decreasing effects of NMDA in rhesus monkeys without producing ketamine-like discriminative stimulus effects.
France, CP; Ornstein, P; Woods, JH, 1989
)
0.28
" In "endogenous" depression, a statistically significant linear dose-response relationship was found in all the efficacy variables assessed."( Therapeutic and side-effect profile of a selective and reversible MAO-A inhibitor, brofaromine. Results of dose-finding trials in depressed patients.
Delini-Stula, A; Heath, WR; Schiwy, W, 1989
)
0.28
" Plasma cisapride concentrations were measured before and after dosing on both study days."( Effect of cisapride on postprandial gastro-oesophageal reflux.
Dent, J; Downton, J; Holloway, RH; Mitchell, B, 1989
)
0.28
" 4-DAMP, atropine, and pirenzepine caused a progressive parallel rightward shift in the dose-response curve of pancreatic secretion for bethanechol."( Subtypes of muscarinic receptors in pancreatic exocrine secretion in anesthetized dog.
Chiba, S; Haruta, K; Homma, N; Horiuchi, A; Iwatsuki, K; Yonekura, H, 1989
)
0.28
"The effects of roxatidine acetate hydrochloride and cimetidine during multiple dosing on the pharmacokinetics of theophylline was studied in nine healthy volunteers, five smokers and four non-smokers, in comparison with placebo treatment."( Effects of roxatidine acetate hydrochloride and cimetidine on the pharmacokinetics of theophylline in healthy subjects.
Aoi, R; Ishioka, T; Ogata, H; Takeuchi, H; Yoshimura, N, 1989
)
0.28
" Power increases, observed mainly in the alpha-1 and beta-2 bands, became decreases in several bands when the dosage was raised to 8 mg/kg."( Effects of the antiparkinson drug budipine on EEG activity in unrestrained rats.
Dimpfel, W; Menge, HG; Spüler, M, 1989
)
0.28
" The dose-response kinetics with four doses of bethanechol with and without somatostatin showed inhibition of a non-competitive type for gastric acid secretion and of a competitive type for antral motility with regard to amplitude."( Effect of somatostatin on bethanechol-stimulated gastric acid secretion and gastric antral motility in dogs with gastric fistula.
Andersen, D; Bech, K; Ladegaard, L, 1985
)
0.27
" Serious adverse reactions necessitate a change in antiarrhythmic therapy, as opposed to lowering drug dosage to an ineffective level."( Antiarrhythmic drug therapy. Recent advances and current status.
Somberg, J, 1985
)
0.27
" The data in this study show that ketanserin as an antihypertensive agent is as effective as prazosin, but in contrast requires no titration of dosage and better compliance can be expected with twice daily rather than three times daily dosing."( Moderate essential hypertension control: a double-blind crossover study between a serotonin antagonist and a post-synaptic alpha-blocker.
Fisher, R; Gruebel, B; Koehle, W; Rosenthal, J, 1986
)
0.27
" Dosage adjustment of TZU-0460 is necessary in renal failure."( Pharmacokinetics of TZU-0460, a new H2-receptor antagonist, in patients with impaired renal function.
Hara, H; Hattori, N; Ishida, Y; Nakamura, S; Ohta, H; Satoh, S; Takabatake, T; Ushiogi, Y; Yamamoto, Y, 1986
)
0.27
" In blood-perfused hindquarters of anaesthetized rats, pretreated with reserpine, pressor dose-response curves to norepinephrine and 5-HT were shifted to a higher dose range."( Pharmacological profile of a new potent 5-hydroxytryptamine (5-HT2) alpha 1-receptor antagonist.
Beckmann, R; Gerbling, KP; Loge, O; Maass, B; Müller, B; Schneider, HH; Schröder, G; Schulz, BG; Seidelmann, D; Stürzebecher, CS, 1988
)
0.27
" The kinetics and effects of ebastine 10 and 50 mg were studied after oral dosing in healthy subjects."( The pharmacokinetics, antihistamine and concentration-effect relationship of ebastine in healthy subjects.
Liminana, R; Meredith, PA; Reid, JL; Vincent, J, 1988
)
0.27
" In rats single or repeated dosing with roxatidine acetate did not influence drug metabolising enzymes in the liver nor did the drug show antiandrogenic activity in long term animal studies."( A review of the animal pharmacology of roxatidine acetate.
Bickel, M; Herling, AW; Scholtholt, J, 1988
)
0.27
"In a series of double-blind randomised studies in normal volunteers with continuous intragastric pH monitoring, the effects of different dosage regimens of roxatidine acetate, a new H2-receptor antagonist, were compared with placebo and ranitidine."( The effects of roxatidine acetate on 24-hour intragastric acidity. Investigations in healthy volunteers and comparison with ranitidine and placebo.
Kaufmann, D; Kempf, M; Merki, HS; Neumann, J; Röhmel, J; Scheurle, E; Walt, RP; Witzel, L, 1988
)
0.27
" After 14 days' treatment with roxatidine acetate substantial reductions in ulcer sizes had been obtained, in addition to healing rates of 87 to 89%, with no significant differences between the dosage regimens."( A comparison of roxatidine acetate 150 mg once daily and 75 mg twice daily in duodenal ulcer healing.
Hentschel, E; Schütze, K, 1988
)
0.27
" Therefore, the same dosage schedule as in uraemia may be applied in patients with dialysis."( Pharmacokinetics of histamine (H2)-receptor antagonists, including roxatidine, in chronic renal failure.
Brockmeier, D; Lameire, N; Rosenkranz, B, 1988
)
0.27
"In 10 healthy male volunteers a dose-response study was carried out with roxatidine acetate, 75, 150, 300, and 600 mg, and placebo on food-stimulated gastric acid secretion (intragastric titration (IGT]."( Inhibition of food-stimulated acid secretion (intragastric titration) by roxatidine acetate. Dose-response study.
Bonfils, S; Chen, WW; Vatier, J, 1988
)
0.27
" In three double-blind randomized studies in normal volunteers the effects of different dosage regimens of roxatidine acetate were compared with placebo and ranitidine."( Assessment of intragastric acidity in man: modern aspects, reproducibility of intragastric pH-monitoring, and pharmacodynamic results obtained with H2-receptor antagonists.
Kaufmann, D; Kempf, M; Merki, HS; Muessig, V; Neumann, J; Roehmel, J; Scheurle, E; Walt, RP; Witzel, L, 1988
)
0.27
"In a series of double-blind randomized studies in normal volunteers using continuous intragastric pH monitoring, the effects of different dosage regimens of roxatidine, a new H2-receptor antagonist, were compared with placebo and ranitidine."( The effects of roxatidine acetate (HOE-760) on 24-hour intragastric acidity in healthy volunteers: comparison with ranitidine and placebo.
Kaufmann, D; Kempf, M; Merki, HS; Müssig, V; Neumann, J; Röhmel, J; Scheurle, E; Walt, RP; Witzel, L, 1988
)
0.27
" At a dosing regimen of KET that inhibited the 5-HT-induced platelet shape change in platelet-rich plasma and the 5-HT-induced increase in perfusion pressure in isolated lungs, KET did not affect the elevation in lung weight or the increased accumulation of 125I-albumin in the lung tissue of MCTP-treated rats."( Monocrotaline pyrrole-induced cardiopulmonary toxicity is not altered by metergoline or ketanserin.
Ganey, PE; Hadley, KB; Roth, RA; Sprugel, KH, 1986
)
0.27
" In the intact animal it may cause increases or decreases of blood pressure and in isolated blood vessels contraction or relaxation depending on the species and vascular bed studied, the route of administration and the dosage used."( Serotonin and the blood vessel wall.
Lüscher, TF; Vanhoutte, PM, 1986
)
0.27
" After placebo dosing for 2 weeks, active drug was given double-blind in two 4-week phases."( Ketanserin and prazosin: a comparison of antihypertensive and biochemical effects.
Marwood, JF; Mennie, BA; Stokes, GS, 1986
)
0.27
" This selectivity for 5-HT uptake was maintained after oral dosing for 14 days."( Biochemical effects of the antidepressant paroxetine, a specific 5-hydroxytryptamine uptake inhibitor.
Johnson, AM; Nelson, DR; Thomas, DR, 1987
)
0.27
"0 hour after dosing and the milk Cmax was 29."( Excretion of loratadine in human breast milk.
Affrime, MB; Hilbert, J; Perentesis, G; Radwanski, E; Symchowicz, S; Zampaglione, N, 1988
)
0.27
" Each drug was administered for 6 weeks after a 1 week run-in period at a daily dosage of 30 mg for paroxetine or 60 mg for mianserin."( Paroxetine in the treatment of depression. A double-blind multicenter study versus mianserin.
Mertens, C; Pintens, H, 1988
)
0.27
" 5-HT agonists stimulated [3H]inositol phosphate accumulation in a dose-related but biphasic manner and only the high-affinity component of the dose-response curve was sensitive to antagonists."( 5-Hydroxytryptamine-stimulated inositol phospholipid hydrolysis in rat cerebral cortex slices: pharmacological characterization and effects of antidepressants.
Kendall, DA; Nahorski, SR, 1985
)
0.27
" The effects of REM parameters are correlated with the dosage and the plasma concentration of the substance."( Effects of brofaremine (CGP 11 305A), a short-acting, reversible, and selective inhibitor of MAO-A on sleep, nocturnal penile tumescence and nocturnal hormonal secretion in three healthy volunteers.
Benkert, O; Holsboer, F; Steiger, A, 1987
)
0.27
" decreased responding to a level significantly below baseline, thus resulting in a biphasic dose-response curve."( Anxiolytic-like action of the 3-PPP enantiomers in the Vogel conflict paradigm.
Carlsson, A; Engel, JA; Hjorth, S, 1987
)
0.27
"The effect of single and repeated dosing of paroxetine on the in vivo noradrenaline uptake process, as determined by tyramine pressor response tests, was evaluated in normal healthy subjects."( A comparison of the effect of paroxetine and amitriptyline on the tyramine pressor response test.
Hassan, SM; Turner, P; Wainscott, G, 1985
)
0.27
"01); twice daily dosage appeared satisfactory."( Ketanserin in essential hypertension: a double-blind, placebo-controlled study.
Cameron, HA; Ramsay, LE, 1985
)
0.27
" When a dose-response was determined by administering each dose in a single bolus injection, apomorphine and (+)-3-PPP produced dose-related inhibitions of fast-firing dopaminergic neurons, with the largest dose of each compound completely inhibiting nearly all cells tested."( Effects of intraperitoneal administration of apomorphine and the isomers of 3-(1-propyl-3-piperidinyl)phenol on the firing activity of substantia nigra dopamine neurons: comparison of agonist efficacies and development of acute tolerance.
Christoffersen, CL; Meltzer, LT, 1988
)
0.27
" The dose-response curve of ifenprodil tartrate was shifted to the left by pre-incubation in calcium hopantenate."( A possible mechanism on the potentiating vascular effect of coadministration of ifenprodil tartrate and calcium hopantenate: a study in the internal carotid artery.
Honda, H; Irino, O; Iwata, T; Izumisawa, M; Matsuda, H; Shibuya, T; Shimura, H; Tsuji, H; Watanabe, Y, 1988
)
0.27
" Based on these findings, pirmenol dosage adjustment will be required when pirmenol is given to patients concurrently receiving rifampin."( Enhanced pirmenol elimination by rifampin.
Cetnarowski, AB; Chang, T; Goldfarb, A; Lebsack, ME; Sedman, AJ; Stringer, KA, 1988
)
0.27
" The favorable pharmacokinetics of pirmenol permit dosage at less frequent intervals than with procainamide, quinidine, disopyramide."( Clinical pharmacology and pharmacokinetics of pirmenol.
Reiter, MJ, 1988
)
0.27
" Two potent, selective and competitive NMDA antagonists, cis-4-(phosphonomethyl)-2-piperidine-carboxylic acid (CGS 19755) and 4-(3-phosphonopropyl)-2-piperazine-carboxylic acid (CPP), were characterized in the gerbil ischemia model with respect to dose-response and time course effects."( The N-methyl-D-aspartate antagonists CGS 19755 and CPP reduce ischemic brain damage in gerbils.
Boast, CA; Etienne, PE; Gerhardt, SC; Lehmann, J; Liebman, JM; Pastor, G, 1988
)
0.27
" Active treatment was given in low dosage (4 mg nocte)."( Loperamide treatment of the irritable bowel syndrome.
Hovdenak, N, 1987
)
0.27
"Delayed gastric emptying is supposed to affect glycemic control in diabetic patients by relative over dosing of insulin to blood glucose level due to delayed absorption of nutrients."( [Effect of cisapride on delayed gastric emptying in diabetic patients].
Goto, Y; Hongo, M; Lin, YF; Okuyama, S; Satake, K; Toyota, T; Ujiie, H, 1988
)
0.27
" Neither was any dose-response relationship noted."( First human studies on the safety and antitussive activity of vadocaine hydrochloride.
Karttunen, P; Männistö, PT; Tukiainen, H; Uusitupa, M, 1988
)
0.27
" Its twice daily dosage schedule and demonstrated efficacy in suppression of ventricular ectopy suggest that it will be a valuable agent in the therapy of ventricular arrhythmias."( Flecainide: a new agent for the treatment of ventricular arrhythmias.
Grubb, BP; Tilley-Gray, B, 1986
)
0.27
" Analysis of the data suggests that the dose-response relationship depends on age in a way that would be consistent with a shift in the dose-response curve with increasing age."( Maturational age affects pirenperone dose-response pattern.
Dillehay, M; Goodrich, C, 1987
)
0.27
" In a similar study in beagle dogs, pirmenol was tolerated clinically at a dosage up to 30 mg/kg/day."( Preclinical toxicology of pirmenol hydrochloride.
de la Iglesia, FA; Martin, RA, 1987
)
0.27
" The dosage was 200 or 250 mg (both 3 times/day) in 2 and 5 patients, respectively."( Electrocardiographic and electrophysiologic effects of pirmenol in ventricular tachycardia.
Cameron, J; Estes, NA; Gold, R; Haffajee, C; Mack, K; Marshall, M; Salem, DN, 1987
)
0.27
" Pirmenol was administered in a 100 mg, 150 mg or 200 mg twice daily dosing schedule."( Preliminary study of pirmenol in the treatment of ventricular arrhythmias.
Algarra Vidal, FJ; Gimeno Gascon, JV, 1987
)
0.27
" All patients not responding to treatment in the first hour were given a repeat dosage and observed for the following 3 hours."( Treatment of postoperative gastrointestinal atony.
Boghaert, A; de Coster, M; Dehertog, P; Michiels, G; Verlinden, M, 1987
)
0.27
" Time course and dose-response studies of estradiol stimulation were carried out in ovariectomized animals and were consistent with a direct action for estrogen."( Direct action of 17 beta-estradiol on mouse mammary ducts analyzed by sustained release implants and steroid autoradiography.
Daniel, CW; Silberstein, GB; Strickland, P, 1987
)
0.27
" The results of the study indicate that the tablet and suspension dosage forms of cisapride are bioequivalent to the reference solution."( Bioavailability of three oral dosage forms of cisapride, a gastrointestinal stimulant agent.
Barone, JA; Bierman, RH; Colaizzi, JL; Heykants, J; Huang, YC; Kerr, DA; Long, JF; Van Peer, A; Woestenborghs, R, 1987
)
0.27
" Patients were initially treated orally in the hospital with 100 mg twice daily; dosage was titrated upward as needed at 4-day intervals to a maximal dose of 200 mg twice daily."( Treatment of resistant ventricular tachycardia with flecainide acetate. Flecainide Ventricular Tachycardia Study Group.
, 1986
)
0.27
" Reducing the dosage abolished the arrhythmia."( Exercise-induced ventricular tachycardia as a manifestation of flecainide toxicity.
Follath, F; Hoffmann, A; Wenk, M, 1986
)
0.27
" These adverse events were also dependent on dosing regimen."( Classification by type of ventricular arrhythmia predicts frequency of adverse cardiac events from flecainide.
Anderson, JL; Gentzkow, GD; Morganroth, J, 1986
)
0.27
" Thirty patients were discharged from the hospital receiving flecainide at a mean (+/- SD) dosage of 315 +/- 76 mg/d and 26 of these patients attained a mean trough plasma drug level of 567 +/- 254 ng/mL."( Flecainide in the treatment of nonsustained ventricular tachycardia.
Chapman, PD; Dougherty, AH; Kim, SS; Lal, R; Naccarelli, GV; Rinkenberger, RL; Ruffy, R; Schechtman, KB; Troup, PJ, 1986
)
0.27
" Only one of eight postinfarction dogs tested remained noninducible throughout the pirmenol dosing schedule."( Electrophysiologic actions of pirmenol in dogs with recent myocardial infarction.
DiCarlo, LA; Hassan, T; Lucchesi, BR; Lynch, JJ; Montgomery, DG, 1986
)
0.27
" After 6 weeks of treatment with a daily dosage of 600 mg femoxetine or 150 mg amitriptyline, no statistically significant differences between the 2 treatment groups were observed, either when using the HDS or the clinical global assessment scale."( Femoxetine and amitriptyline in general practice: a randomized double-blind group comparison.
Jeppesen, K; Skrumsager, BK, 1986
)
0.27
" The present experiments extend these findings by providing dose-response data on the effects of scopolamine and Ditran on neocortical activity in relation to behavior in the rat."( Joint cholinergic-serotonergic control of neocortical and hippocampal electrical activity in relation to behavior: effects of scopolamine, ditran, trifluoperazine and amphetamine.
Stewart, DJ; Vanderwolf, CH, 1986
)
0.27
" The dose-response curves for the phenethylamine hallucinogens were shifted significantly to the right and to a greater degree than were those for the indolealkylamine hallucinogens."( The 5HT2 antagonist pirenperone reverses disruption of FR-40 by hallucinogenic drugs.
Mokler, DJ; Rech, RH; Stoudt, KW, 1985
)
0.27
" It can be given either intravenously or orally and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration."( Flecainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Heel, RC; Holmes, B, 1985
)
0.27
" The study consisted of an initial 1-week, placebo-controlled, baseline period followed by two 12-day, randomized, crossover, double-blind treatment periods with incremental dosage and 1 month of placebo between drug periods."( Efficacy of flecainide in the management of ventricular arrhythmias: comparative study with amiodarone.
Bertolasi, CA; Dubner, SJ; Elencwajg, BD; Mendelzon, R; Palma, S; Ramos, A, 1985
)
0.27
" Plasma concentrations increased linearly with the cumulative flecainide dosage in both groups."( Hemodynamic dose-response effects of flecainide in acute myocardial infarction with and without left ventricular decompensation.
Frais, MA; Hafizullah, M; Jackson, N; Reynolds, G; Silke, B; Taylor, SH; Verma, SP, 1985
)
0.27
" The elimination half-life ranges from 12-27 hours in patients with normal renal function, allowing convenient dosing regimens of 100-200 mg twice daily in most patients."( Flecainide: a new prototype antiarrhythmic agent.
Anderson, JL; Nappi, JM,
)
0.13
" Flecainide is rapidly and completely absorbed after oral administration and has a 13-hour elimination half-life, allowing for twice-daily dosing regimens."( Flecainide: a new class Ic antidysrhythmic.
Smith, GH, 1985
)
0.27
"Flecainide was initially prescribed at a dose of 200 mg twice daily, but after early toxicity in patients with ventricular tachycardia (VT), the dosage was reduced to 100 mg twice daily."( Flecainide: long-term treatment using a reduced dosing schedule.
Flowers, D; Miura, D; O'Gallagher, D; Somberg, JC; Torres, V, 1985
)
0.27
" The above-mentioned cytostatic and cytotoxic effects of CP-46,665 were dependent on dosage and incubation time."( Cytotoxicity of the alkyl-linked lipoidal amine 4-aminomethyl-1-[2,3-(di-n-decyloxy)-n-propyl]-4-phenylpiperidine (CP-46,665) in cells from human tumors and leukemias.
Berdel, WE; Fink, U; Rastetter, J; Reichert, A; Schick, HD; Ulm, K, 1985
)
0.27
" At the dosage administered, propranolol alone had no antiarrhythmic effect."( Antiarrhythmic therapy with flecainide in combination and comparison with propranolol.
Scheininger, M; Stern, H; Theisen, F; Theisen, K, 1985
)
0.27
" The influence of changes in urinary pH on the pharmacokinetics of flecainide will contribute to the normal variability in flecainide serum concentrations seen in patients and should be considered in patients who have adverse reactions to the drug at low dosage or who fail to respond at high doses."( Flecainide pharmacokinetics in healthy volunteers: the influence of urinary pH.
Johnston, A; Turner, P; Warrington, S, 1985
)
0.27
" Midazolam (10(-7)-10(-5) M) potentiated responses to all three agonists to a similar extent with a shift to the left of the dose-response curve."( Modulation of the responses to the GABA-mimetics, THIP and piperidine-4-sulphonic acid, by agents which interact with benzodiazepine receptors. An electrophysiological study on cultured mouse neurones.
Jensen, MS; Lambert, JD, 1984
)
0.27
" None of the terfenadein dosage schedules up to 200 mg tid caused sedation significantly different from that of placebo."( Clinical investigation of terfenadine, a non-sedating antihistamine.
Brandon, ML; Weiner, M, 1980
)
0.26
" Ketotifen in the higher dosage caused a slight reduction in salbutamol usage and a modest improvement in breathing in patients not already receiving inhaled corticosteroids."( Ketotifen in adult asthma.
Dyson, AJ; Mackay, AD, 1980
)
0.26
" Each dopamine antagonist displaced the dose-response curve for dopamine-induced suppression of prolactin release to the right in a parallel manner."( Chlorpromazine, haloperidol, metoclopramide and domperidone release prolactin through dopamine antagonism at low concentrations but paradoxically inhibit prolactin release at high concentrations.
Besser, GM; Delitala, G; Grossman, A; Stubbs, WA; Yeo, T, 1980
)
0.26
") elicited yawning in rats and the dose-response curves of all 3 compounds showed a bell-shaped form."( Effects of apomorphine, TL-99 and 3-PPP on yawning in rats.
Boissard, CG; Delini-Stula, A; Mogilnicka, E, 1984
)
0.27
" If side effects intervene that may cause continued therapy to be intolerable, changing the antiarrhythmic agent, as opposed to decreasing the dosage to an ineffective range, may be appropriate."( New directions in antiarrhythmic drug therapy.
Somberg, JC, 1984
)
0.27
" In po dosed bile-cannulated rats, 57% was excreted with the bile within 24 hr, whereas about 30 to 40% of the biliary radioactivity was subjected to enterohepatic circulation."( Excretion and biotransformation of ketanserin after oral and intravenous administration in rats and dogs.
Hendrickx, J; Heykants, J; Hurkmans, R; Knaeps, F; Lauwers, W; Meuldermans, W; Swysen, E; Woestenborghs, R,
)
0.13
" Ketotifen markedly differs in this respect, inhibiting according to a bell-shaped dose-response curve and at concentrations closely comparable to that of DSCG."( Inhibition of allergen-mediated histamine release from human cells by ketotifen and oxatomide. Comparison with other H1 antihistamines.
Radermecker, M, 1981
)
0.26
" The likelihood of side effects may be decreased by using this dosage regimen."( Therapy of angina pectoris with low-dose perhexiline.
Horgan, JH; O'Callaghan, WG; Teo, KK,
)
0.13
" Loperamide, in the dosage used in this study, appears to have no significant effect on the course of acute gastro-enteritis in early childhood."( Loperamide in the treatment of acute gastroenteritis in early childhood. Report of a two centre, double-blind, controlled clinical trial.
Broadhead, R; Gangal, RN; Hendrickse, RG; Jaswal, OP; Owens, JR, 1981
)
0.26
" Atropine caused a dose-dependent rightward shift in the dose-response curves of inhibitory and excitatory effects of the two muscarinic agonists."( Pharmacologic identification, activation and antagonism of two muscarine receptor subtypes in the lower esophageal sphincter.
Gilbert, R; Goyal, RK; Rattan, S, 1984
)
0.27
"In a randomized double-blind cross-over trial, the effectiveness of lorcainide at a dosage of three times 100 mg/d by mouth was compared with that of a placebo for the treatment of subjectively disturbing stable ventricular extrasystoles (VES), using 48-hour continuous ECG monitoring."( [Lorcainide in stable ventricular extrasystole. A double-blind study with 48-hour continuous ECG recording].
Buss, J; Geiger, S; Gores, D; Heene, DL; Stegaru, B, 1984
)
0.27
" (10 mg) do not affect the pressor dose-response curve to phenylephrine."( Antihypertensive properties of ketanserin (R 41 468).
Janssen, PA; Symoens, J; Van Nueten, JM; Vanhoutte, PM, 1983
)
0.27
" Agonist-antagonist interactions were studied by pretreating the vessels with methysergide, ketanserin and phentolamine and then establishing the dose-response curves to 5-HT or noradrenaline (NA)."( Tryptaminergic receptors in the bovine pulmonary vasculature: effects of ketanserin.
Eyre, P; Ogunbiyi, PO, 1984
)
0.27
"Ketanserin, a new 5-hydroxy-tryptamine antagonist, was given at three different dosage levels (double-blind, randomized) in a dose finding study for 2 months to 31 patients with mild to moderately severe essential hypertension."( Ketanserin in hypertension. Early clinical evaluation and dose finding study of a new 5-HT2 receptor antagonist.
Andrén, L; Dahlöf, B; Eggertsen, R; Hansson, L; Svensson, A, 1983
)
0.27
" Twice-daily dosing with 100 to 200 mg usually provides effective therapy."( A proposal for the clinical use of flecainide.
Anderson, JL; Crevey, BJ; Stewart, JR, 1984
)
0.27
" For patients with ventricular premature complexes, the half-life is longer (mean 20 hours), and twice-daily oral dosage is effective."( Metabolism of flecainide.
Conard, GJ; Ober, RE, 1984
)
0.27
"Symptom scores, stool data, and the transit of a standard, solid meal were measured in 28 patients with irritable bowel syndrome (IBS) during baseline conditions and after five weeks of treatment with placebo and loperamide, given as a flexible dosage regime in the form of a double-blind, cross-over trial."( Role of loperamide and placebo in management of irritable bowel syndrome (IBS).
Barends, D; Cann, PA; Holdsworth, CD; Read, NW, 1984
)
0.27
" It can be given either intravenously or orally, and its pharmacokinetic properties allow relatively long (12 hours) dosing intervals with oral administration."( Lorcainide. A preliminary review of its pharmacodynamic properties and therapeutic efficacy.
Brogden, RN; Eiriksson, Ce, 1984
)
0.27
"Measurement of drug levels is becoming increasingly popular to optimise the dosage of various drugs."( Reliability of antiarrhythmic drug plasma concentration monitoring.
Follath, F; Ganzinger, U; Schuetz, E,
)
0.13
" A single dosage (0."( Synthetic immunomodulators for prevention of fatal infections in a burned guinea pig model.
Alexander, JW; Gonce, SJ; Loose, LD; Miskell, P; Stinnett, JD; Tenney, CL, 1983
)
0.27
" It may therefore be possible to reduce the incidence of these complications by adapting dosage to the patient's clinical state and to the serum drug levels."( [Flecainide: a new antiarrhythmic agent].
Coumel, P; Leclercq, JF, 1983
)
0.27
" All drugs have been shown to inhibit specifically the locomotor activity potentiating effect of LSD in a low dosage range (0."( Effects of atypical antidepressants on LSD potentiated apomorphine hypermotility in rats.
Fink, H; Gold, R; Morgenstern, R, 1980
)
0.26
" It is metabolized through the liver, and patients with significant liver disease will require dosage reduction."( Pharmacology of lorcainide.
Keefe, DL, 1984
)
0.27
"0 mg/kg); dose-response curves for LY136596 were shifted to the right in a parallel manner by increasing doses of LY136595."( Quantitative analysis of the interaction between the agonist and antagonist isomers of picenadol (LY150720) on electric shock titration in the squirrel monkey.
Carter, RB; Dykstra, LA, 1984
)
0.27
" For example, M-methyl-4-piperidinol benzylate applied in a wide dosage range induced motor hyperactivity without affecting the short-term memory, whereas tropine phenylcyclopentylglycolate provoked motor hyperactivity and memory disorders at equal doses."( [Comparative study of the effect of 3 M-cholinergic blockaders on memory and motor activity in rats].
Sprints, AM; Vinogradov, VV; Zhirova, ND,
)
0.13
"Blood pressure and heart rate, supine and standing, were studied in patients with essential hypertension during 8 weeks of oral therapy with two dosage schedules of ketanserin, 40 mg once and twice daily."( Ketanserin, a novel 5-hydroxytryptamine antagonist: monotherapy in essential hypertension.
Berglund, G; Hedner, T; Persson, B, 1983
)
0.27
" Lever pressing for intracranial self-stimulation (ICSS) was attenuated in a dose-related fashion by TL-99 and 3-PPP, with relatively shallow dose-response relationships."( Avoidance and ICSS behavioral models dissociate TL-99 and 3-PPP from dopamine receptor antagonists.
Fenton, HM; Gerhardt, S; Hall, NR; Liebman, JM; Neale, R; Noreika, L, 1983
)
0.27
" Three dosage levels were tested: 15, 30 and 60 mg/a day in 3 divided doses."( Pilot study of a specific serotonergic antagonist, pirenperone, in the treatment of anxiety disorders.
Ansseau, M; Doumont, A; Gelders, Y; Thiry, D,
)
0.13
" Only minor quantitative differences were observed between intravenously and orally dosed animals, and between male and female rats."( Excretion and metabolism of lorcainide in rats, dogs and man.
Hendrickx, J; Heykants, J; Hurkmans, R; Lauwers, W; Meuldermans, W; Swysen, E; Thijssen, J,
)
0.13
") was administered at 30 min intervals on four experimental days: no pretreatment; after prazosin 1 mg/kg and infusion; after pharmacological 'total' autonomic effector block (TAB) and with repeated three point methoxamine dose-response lines."( Haemodynamic response to ketanserin in rabbits with Page hypertension: comparison with prazosin.
Angus, JA; Wright, CE, 1983
)
0.27
" Placebo was then reinstituted and after arrhythmia had recurred, the patients were discharged on the effective dosage to return to the clinic for evaluation 7 and 14 days later."( Flecainide dose-response relations in stable ventricular arrhythmias.
Duff, HJ; Roden, DM; Siddoway, LA; Woosley, RL, 1984
)
0.27
" Minor dosage adjustments were made during early outpatient therapy in 5 patients."( Experience with electrophysiologically guided therapy of ventricular tachycardia with flecainide: summary of long-term follow-up.
Anderson, JL, 1984
)
0.27
" These data suggest that renal disease should not alter either the dose or the dosing interval of lorcainide."( Lorcainide kinetics and protein binding in patients with end-stage renal disease.
Gupta, RK; King, P; Shapiro, RS; Simon, V; Somani, P; Stockard, H, 1984
)
0.27
" 3 On a dosage basis, encainide was seven times, lorcainide fourteen times and ORG 6001 twice as potent as lignocaine in raising VFT."( Antifibrillatory efficacy of encainide, loracainide and ORG 6001 compared with lignocaine in isolated hearts of rabbits and guinea-pigs.
Almotrefi, AA; Baker, JB, 1981
)
0.26
" The extended half-life of this new agent (about 20 hours in cardiac patients) may allow a convenient twice-daily dosage schedule."( Use of flecainide acetate in the treatment of premature ventricular contractions.
Abate, C; Abitbol, H; Beilis, P; Califano, JE; Castellanos, H, 1983
)
0.27
" Its favorable pharmacokinetics with an average plasma half-time of about 20 hours allows in most patients twice daily dosing (Duff et al."( Flecainide-induced aggravation of ventricular tachycardia.
Hohnloser, S; Hust, MH; Just, H; Wollschläger, H; Zeiher, A, 1983
)
0.27
"Halofuginone lactate, given once orally at a dosage rate of 1,2 mg/kg body mass on the 1st, 3rd or 5th days of fever, resulted in the recovery of only 1 out of 5 splenectomized cattle."( Chemotherapy of Theileria parva lawrencei infections in cattle with halofuginone.
De Vos, AJ; Roos, JA, 1983
)
0.27
" Domperidone was taken at a dosage of 10 mg tablets 4-times daily."( Use of the peripheral dopamine antagonist, domperidone, in the management of gastro-intestinal symptoms in patients with irritable bowel syndrome.
Milo, R, 1980
)
0.26
" Twice-daily dosing (average daily dose 436 mg) completely suppressed all ventricular ectopic activity in five of 11 patients; average suppression in the 11 patients was 96."( Suppression of ventricular ectopic depolarizations by flecainide acetate, a new antiarrhythmic agent.
Asinger, RW; Conard, GJ; Granrud, G; Haugland, JM; Hodges, M; Krejci, J; Mikell, FL, 1982
)
0.26
" Combination of the two drugs permitted rapid increase in bromocriptine dosage from 22."( Bromocriptine and domperidone in the treatment of Parkinson disease.
Agid, Y; Illas, A; Lhermitte, F; Quinn, N, 1981
)
0.26
") dosing and there was a prolonged increase during 8 min."( [Influence of 3-(3, 4, 5-trimethoxybenzamido) piperidine (KU-54) on gastric mucosal blood flow (author's transl)].
Abe, Y; Irikura, T, 1980
)
0.26
" Two oral dosage forms were studied: 10-mg tablets and a 10-mg/ml oral solution."( On the pharmacokinetics of domperidone in animals and man. IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration.
Hendriks, R; Heykants, J; Meuldermans, W; Michiels, M; Reyntjens, H; Scheygrond, H, 1981
)
0.26
"Blood pressure and pulse rate were studied in 20 Parkinsonian patients on no treatment, and during treatment with bromocriptine (mean dosage 148 mg/day) as the sole anti-Parkinsonian therapy."( Bromocriptine in Parkinson's disease: a study of cardiovascular effects.
Agid, Y; Illas, A; Lhermitte, F; Quinn, N, 1981
)
0.26
"Stimulation of complex dosage regimens for drugs with multicompartmental kinetics is described using the method of separate exponentials."( The method of separate exponentials: a simple aid to devising intravenous drug-loading regimens.
Bjornsson, TD; Desjardins, RE; Hammill, SC; Pritchett, EL; Shand, DG, 1981
)
0.26
" After acquisition, the quipazine and ketanserin dose-response curves were found to be orderly and reproducible."( Neurochemical and behavioral evidence that quipazine-ketanserin discrimination is mediated by serotonin2A receptor.
Barrett, RJ; Sanders-Bush, E; Smith, RL, 1995
)
0.29
" produced a rightward parallel shift of the dose-response curves for AVP in a dose-dependent manner."( OPC-21268 antagonizes arginine vasopressin-induced vasoconstrictor response in the spinally-anesthetized dog.
Chihara, T; Mori, T; Nakamura, S; Onogawa, T; Tominaga, M; Yabuuchi, Y; Yamamura, Y; Yamashita, T, 1995
)
0.29
" SR 48968 (10(-6) M shifted the [Pro9]SP dose-response curve but did not modify the septide dose-response curve."( Involvement of septide-sensitive tachykinin receptors in inositol phospholipid hydrolysis in the rat urinary bladder.
Beaujouan, JC; Glowinski, J; Saffroy, M; Torrens, Y, 1995
)
0.29
" This article discusses the relevant clinical considerations in switching neuroleptics and proposes practical guidelines on issues such as dosing and course of therapy with risperidone."( Clinical considerations in the use of risperidone.
Remington, GJ, 1993
)
0.29
" Agents were compared over dosage ranges that produced maximal increases in QTc interval and monophasic action potential duration (MAPD)."( Comparative assessment of ibutilide, D-sotalol, clofilium, E-4031, and UK-68,798 in a rabbit model of proarrhythmia.
Brunden, MN; Buchanan, LV; Gibson, JK; Kabell, G, 1993
)
0.29
" Dose-response analysis of receptor occupancy revealed risperidone demonstrated higher binding affinity for 5-HT2 than for D2, while the reverse was observed with haloperidol."( In vivo dopamine-D2 and serotonin-5-HT2 receptor binding study of risperidone and haloperidol.
Kido, H; Mori, H; Sakamoto, H; Shiba, K; Sumiyoshi, T; Suzuki, K; Urasaki, K; Yamaguchi, N; Yokogawa, K, 1994
)
0.29
" Risperidone was found to have a curvilinear dose-response curve with an optimum effect of 4 mg day on the negative, anxious/depressive and cognitive factors and with an optimum effect of 8 mg day on the positive and excited factors."( Changes in single symptoms and separate factors of the schizophrenic syndrome after treatment with risperidone or haloperidol.
Lindström, E; von Knorring, L, 1994
)
0.29
" Risperidone is 4-10 times less potent than haloperidol as a central D2 antagonist in rats and it differs from haloperidol by the following characteristics: predominant 5-HT2 antagonism; LSD antagonism; effects on sleep; smooth dose-response curves for D2 antagonism; synergism of combined 5-HT2/D2 antagonism; pronounced effects on amphetamine-induced oxygen consumption; increased social interaction; and pronounced effects on dopamine (DA) turnover."( Survey on the pharmacodynamics of the new antipsychotic risperidone.
Awouters, FH; Dugovic, C; Leysen, JE; Meert, TF; Megens, AA; Niemegeers, CJ; Schotte, A, 1994
)
0.29
" At a dosage of 4 to 8 mg/day, risperidone is comparable to 10 mg/day of haloperidol."( A risk-benefit assessment of risperidone in schizophrenia.
Curtis, VA; Kerwin, RW, 1995
)
0.29
" Recent research has underscored the need for optimum dosing strategies."( Antipsychotic medication in the treatment of schizophrenia.
Kane, JM, 1995
)
0.29
" In patients in whom low-to-moderate dosage is effective, there should be fewer and less severe adverse effects with risperidone than with haloperidol."( Risperidone: review and assessment of its role in the treatment of schizophrenia.
Cardoni, AA, 1995
)
0.29
" In anaesthetized guinea-pigs, RS 39604 antagonized the contractile effect of 5-HT in the proximal colon by producing parallel, dextral displacement of the dose-response curve to 5-HT."( RS 39604: a potent, selective and orally active 5-HT4 receptor antagonist.
Bonhaus, DW; Clark, RD; Eglen, RM; Hegde, SS; Johnson, LG; Leung, E, 1995
)
0.29
" Changes in the dosage of cisapride should be further evaluated."( The effects of cisapride on the quality and tolerance of colonic lavage: a double-blind randomized study.
Berner, JS; Korsten, MA; Rajendran, SK; Reiser, JR; Rosman, AS, 1995
)
0.29
" Thus, we have compared the actions of the selective neurokinin 1 (NK1) (CP-99,994) and neurokinin 2 (NK2) (SR-48,968) receptor antagonists against dose-response curves (DRC) induced by intravenously administered substance P (SP), neurokinin A (NKA), neurokinin B (NKB), beta Ala8-NKA (4-10),Sar9-Met(O2)11SP, and single dose (intravenous) challenge with resiniferatoxin (RTX), a capsaicin-like sensory neurotoxin, leukotriene D4 (LTD4) and antigen."( NK1 and NK2 receptors mediate tachykinin and resiniferatoxin-induced bronchospasm in guinea pigs.
Champion, E; Foulon, DM; Jones, TR; Masson, P; Rodger, IW, 1993
)
0.29
" Oxotremorine generated dose-response curves that were similar in both the circular and longitudinal vectors and intermediate to those previously reported for carbachol and aceclidine."( The effect of muscarinic agonists and selective receptor subtype antagonists on the contractile response of the isolated rhesus monkey ciliary muscle.
Gabelt, BT; Kaufman, PL; Poyer, JF, 1994
)
0.29
" The antiischemic and antiarrhythmic dose-response curves were superimposable, suggesting a common mechanism of action."( Attenuation by R 56865, a novel cytoprotective drug, of regional myocardial ischemia- and reperfusion-induced electrocardiographic disturbances in anesthetized rabbits.
De Courtois, F; John, GW; Le Grand, B; Pouget, G; Verscheure, Y, 1995
)
0.29
" As in a pilot study with six patients (CLCR < or = 17 ml min-1) the recommended dosage regimen (75 mg 48 h-1) was unable to maintain gastric pH > 4 for more than 6 h, daily nocturnal intake of 75 mg roxatidine acetate appears appropriate to elevate gastric pH > 4 for a sufficient period of time."( Pharmacokinetics and pharmacodynamics of roxatidine in patients with renal insufficiency.
Gladziwa, U; Klotz, U; Sieberth, HG; Wagner, S, 1995
)
0.29
"To determine the stability of cisapride in a liquid dosage form stored in plastic bottles at 2 temperatures."( Stability of cisapride in a liquid dosage form at two temperatures.
Hipple, TF; Morosco, RS; Nahata, MC, 1995
)
0.29
"Prosidol, a new Russian narcotic analgesic, was used in various dosage forms (buccal and oral tablets, injection solution) in 113 cancer patients for the treatment of chronic pain, as a component of total anesthesia, and for postoperative analgesia."( [First experience in the use of a new Russian narcotic analgesic prosidol in oncology].
Beresnev, VA; Loseva, NA; Novikov, GA; Osipova, NA; Prokhorov, BM; Smolina, TA; Vetsheva, MS; Zemskaia, SIu,
)
0.13
" Group A patients took nearly the maximum dosage of cisapride tablets allowed during follow-up (3."( Cisapride in chronic idiopathic constipation: can the colon be re-educated? Bavarian Constipation Study Group.
Müller-Lissner, SA, 1995
)
0.29
"To extend and confirm previous data, we examined the effects of raloxifene on the proximal tibia of ovariectomized rats, aged 6 months, longitudinally and cross-sectionally by computed tomography (pQCT) and then compared the effects to those of orally dosed estrogen."( Longitudinal and cross-sectional analysis of raloxifene effects on tibiae from ovariectomized aged rats.
Bryant, HU; Kim, J; Sato, M; Short, LL; Slemenda, CW, 1995
)
0.29
" This suggests that remifentanil may not need to be dosed according to body weight in adult patients."( Pharmacokinetics of remifentanil (GI87084B) and its major metabolite (GI90291) in patients undergoing elective inpatient surgery.
Hoke, JF; Hug, CC; Muir, KT; Sebel, PS; Westmoreland, CL, 1993
)
0.29
" The measured reduction in dopamine D2 receptor density after EEDQ was of the same magnitude as the reduction in receptor number predicted from the EEDQ induced shift in the dose-response curve of the full dopamine D2 receptor agonist NPA."( A high dose of EEDQ reduces pituitary dopamine D2 receptor density and the prolactin suppressive potency of agonists.
Ekman, A; Eriksson, E, 1993
)
0.29
" Although the 6-hour hemodialysis procedure starting 4 hours after dosing eliminated 10% of the oral dose, the terminal half-life and the total area under the plasma concentration-time curve did not differ significantly between the hemodialysis and the nonhemodialysis patients."( Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency.
Heykants, J; Huang, ML; Stephen, A; Van Peer, A; Woestenborghs, R; Zazgornik, J, 1993
)
0.29
"We determined the possible benefits of a new opioid, trefentanil, relative to fentanyl and alfentanil using high-resolution pharmacokinetic-pharmacodynamic modeling and computer simulations of clinical dosing scenarios."( Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil.
Dyck, JB; Lemmens, HJ; Shafer, SL; Stanski, DR, 1994
)
0.29
" Finally, we used computer simulations to predict offset of opioid effects of trefentanil, fentanyl, and alfentanil when given in different dosing schemes."( Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil.
Dyck, JB; Lemmens, HJ; Shafer, SL; Stanski, DR, 1994
)
0.29
"We suggest that high-resolution pharmacokinetic-pharmacodynamic studies and computer simulations of clinical dosing scenarios may have significant usefulness in appreciating differences between new and established drugs in early phase I studies."( Pharmacokinetic-pharmacodynamic modeling in drug development: application to the investigational opioid trefentanil.
Dyck, JB; Lemmens, HJ; Shafer, SL; Stanski, DR, 1994
)
0.29
" The results of the trial are compared with other trials of monoamine oxidase inhibitors in this patient group and the possible reasons for the lack of a clear dose-response relationship are discussed."( Brofaromine in non-endogenous major depressed inpatients--results of a preliminary dose-finding trial versus tranylcypromine.
Bellaire, J; Heimann, H; Laux, G; Möller, HJ; Volz, HP, 1994
)
0.29
" In experiment 1, steers were dosed with 0, 25, or 50 micrograms."( Effects of slaframine and 4-diphenylacetoxy-N-methylpiperidine methiodide (4DAMP) on pancreatic exocrine secretion in the bovine.
Croom, WJ; Hagler, WM; Harmon, DL; Krehbiel, CR; St Jean, G; Walker, JA, 1994
)
0.29
" In its presence, the dose-response curve for RP 67580 was dose-dependently shifted to the left."( The glycine B receptor partial agonist, (+)-HA966, enhances induction of antinociception by RP 67580 and CP-99,994.
Millan, MJ; Seguin, L, 1994
)
0.29
" The pharmacokinetics of carebastine were linear and dose independent in the dosage range studied."( Pharmacokinetics and pharmacodynamics of ebastine in children.
Simons, FE; Simons, KJ; Watson, WT, 1993
)
0.29
" Twelve healthy subjects received a single 20 mg dose of ebastine on day 2 of a multiple oral dosing regimen of either cimetidine (400 mg three times daily and 800 mg in the evening on the day preceding ebastine administration and 400 mg four times daily on the 2 following days) or placebo in a randomised cross-over design."( Cimetidine does not influence the metabolism of the H1-receptor antagonist ebastine to its active metabolite carebastine.
Breimer, DD; Bruno, R; Cohen, AF; Reinhoudt, JF; Schoemaker, HC; Van Rooij, J, 1993
)
0.29
" Cisapride, at the dosage given, confers only modest benefit."( Small bowel motility following major intra-abdominal surgery: the effects of opiates and rectal cisapride.
Benson, MJ; Castillo, FD; Deeks, JJ; Roberts, JP; Rogers, J; Williams, NS; Wingate, DL, 1994
)
0.29
"Randomized, double-blind, parallel, dose-response study."( Picenadol in a large multicenter dental pain study.
Brunelle, RL; Cooper, SA; Desjardins, PJ; Gallegos, LT; Gaston, GW; George, RE; Goldstein, DJ; Jeffers, GE; Reynolds, DC,
)
0.13
" These effects occurred with litoxetine blood concentrations ranging from 3 to 7 ng ml-1 with the 10 mg dosage and from 8 to 18 ng ml-1 with the 25 mg dosage."( EEG profile of litoxetine after single and repeated administration in healthy volunteers.
Bianchetti, G; Court, LA; Dubruc, C; Morselli, PL; Patat, A; Rosenzweig, P; Thébault, JJ; Trocherie, S, 1994
)
0.29
" The NK1 antagonist (+/-)-CP96345 was found to cause, at a maximally tolerated dose of 9 mumol/kg, an approximate 10-fold rightward shift of the dose-response curves for selective NK1 agonists substance P (SP), [Sar9,Met(O2)11]SP and Ac-[Arg6,Sar9,Met(O2)11]SP6-11 without altering responses to selective NK2 agonists neurokinin A (NKA), [Nle10]NKA4-10 or [beta-Ala8]NKA4-10."( Differential blockade by tachykinin NK1 and NK2 receptor antagonists of bronchoconstriction induced by direct-acting agonists and the indirect-acting mimetics capsaicin, serotonin and 2-methyl-serotonin in the anesthetized guinea pig.
Buckner, CK; Campbell, J; Dea, D; Krell, RD; Lengel, D; Liberati, N; Miller, S; Shenvi, A; Stinson-Fisher, C, 1993
)
0.29
"The aim of this study was to determine the optimal dosage regimen of cisapride for the treatment of idiopathic gastroparesis."( The effect of different dosage schedules of cisapride on gastric emptying in idiopathic gastroparesis.
Barbara, L; Corbelli, C; Corinaldesi, R; Marengo, M; Monetti, N; Rea, E; Stanghellini, V; Tosetti, C, 1993
)
0.29
"100 mg kg-1 and with a dosage interval of 12 hours should improve pulmonary function."( Comparison of three metrenperone dosage regimens inhibiting the 5-hydroxytryptamine-induced pulmonary dysfunction in cattle.
Amory, H; Desmecht, DJ; Lekeux, PM; Linden, AS; Rollin, FA, 1993
)
0.29
" Conversely, SR-48,968 antagonized the bronchoconstrictor response to Nle10-NKA[4-10], right-shifting the dose-response curve by 2 log units, but had no effect on Sar9, Met(O2)11-SP-induced bronchoconstriction."( Tachykinin receptor antagonists inhibit hyperpnea-induced bronchoconstriction in guinea pigs.
Alger, LE; Garland, A; Gitter, B; Howbert, JJ; Jordan, JE; Kao, BM; Leff, AR; Necheles, J; Rodger, IW; Solway, J, 1993
)
0.29
" Gallbladder contractility, measured in vitro in response to CCK, decreased 23% in animals on the 1% cholesterol diet; cisapride restored the CCK dose-response curve to normal."( Cisapride improves gallbladder contractility and bile lipid composition in an animal model of gallstone disease.
Shaffer, EA; Xu, QW, 1993
)
0.29
" Our results suggest that brofaromine at the clinically used dosage of 150 mg/day does indeed inhibit 5-HT uptake, as evidenced by measurements of 3H-paroxetine binding to platelets."( Serotonin uptake inhibition by the monoamine oxidase inhibitor brofaromine.
Feldtrauer, JJ; Germer, M; Graf, T; Howald, H; Waldmeier, PC, 1993
)
0.29
" stephensi Liston, and Phlebotomus papatasi (Scopoli) using a dose-response testing procedure on human volunteers."( Laboratory evaluation of repellents against four anopheline mosquitoes (Diptera: Culicidae) and two phlebotomine sand flies (Diptera: Psychodidae).
Coleman, RE; Glass, JA; Laughinghouse, A; Perkins, PV; Robert, LL; Roberts, LW; Seeley, DC; Wirtz, RA, 1993
)
0.29
" The dosage of cisapride ranges from 5mg 3 times daily to 20mg twice daily."( A risk-benefit assessment of cisapride in the treatment of gastrointestinal disorders.
Coremans, G; Janssens, J; Tack, J, 1995
)
0.29
" Early evening or bedtime dosing with roxatidine 150 mg resulted in similar 4- to 8-week rates of duodenal ulcer healing."( Double-blind, randomized trial of roxatidine 150 mg in the early evening versus bedtime administration in the short-term treatment of duodenal ulcer.
Bianchi Porro, G; Canali, A; Lazzaroni, M, 1995
)
0.29
", approximately 35% [CR+PR] in unselected patients), although dosage regimens of the new antiestrogens are higher than the 20 mg tamoxifen required daily."( Alternate antiestrogens and approaches to the prevention of breast cancer.
Jordan, VC, 1995
)
0.29
" R56865 was given before ischemia and with the onset of reperfusion, applying different dosing schedules, including an initial loading dose."( R56865 is antifibrillatory in reperfused ischemic guinea-pig hearts, even when given only during reperfusion.
Guttmann, I; Mozes, A; Scheufler, E; Wilffert, B, 1995
)
0.29
" Further studies are needed to evaluate the most effective dosage regimen for the treatment of constipation and to compare the efficacy and cost-efficiency of cisapride with those of conventional therapy."( Cisapride for the treatment of chronic idiopathic constipation.
Beckwith, JV; Gardner, VY; Heyneman, CA, 1995
)
0.29
" Therefore, it is difficult to accurately compare the ETA activity of selective ETA receptor antagonists (BQ 123 and BMS 182874) with mixed ETA/ETB antagonists (SB 209670 and bosentan) on the cumulative dose-response curve to ET-1."( Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats.
Brazdil, R; Brown, TJ; Flynn, DA; Roach, AG; Sargent, CA, 1995
)
0.29
" dosing with responses returning to control by 16 hr, indicative of long duration receptor blockade."( LY353433, a potent, orally effective, long-acting 5-HT(4) receptor antagonist: comparison to cisapride and RS23597-190.
Bloomquist, W; Calligaro, DA; Cohen, I; Cohen, ML; Schaus, JM; Susemichel, AD; Thompson, DC, 1996
)
0.29
" In experiment 1, a dose-response curve was performed."( Vesamicol, an acetylcholine uptake blocker in presynaptic vesicles, suppresses rapid eye movement (REM) sleep in the rat.
Jimenez-Anguiano, A; Salin-Pascual, RJ, 1995
)
0.29
" Airway hyperresponsiveness was evidenced by significant shifts to the left of dose-response curves for intravenous acetylcholine (ACh) without a change in maximum responses to ACh."( The tachykinin NK2 receptor antagonist SR 48968 inhibits citric acid-induced airway hyperresponsiveness in guinea pigs.
Advenier, C; Emonds-Alt, X; Girard, V; Yavo, JC, 1996
)
0.29
" Five weeks of oral dosing confirmed that ethynyl estradiol, tamoxifen, and raloxifene are potent inhibitors of the loss in volumetric bone mineral density (BMD, mg/cc) induced by ovariectomy, as measured by computed tomography."( Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats.
Bryant, HU; Rippy, MK; Sato, M, 1996
)
0.29
"1 microM), shifted the dose-response curve for muscarine-induced adrenaline secretion to the right."( Muscarinic receptor subtypes mediating catecholamine secretion and increase in intracellular Ca2+ concentration in adrenal chromaffin cells of the guinea pig.
Asano, T; Ito, S; Nakazato, Y; Ohta, T; Otsuguro, K, 1995
)
0.29
"Twenty-four patients with healed duodenal ulcer were dosed according to a balanced incomplete-block design, with two of the following regimens: placebo, roxatidine 150 mg at 07."( Twenty-four-hour intragastric acidity following early evening or bedtime administration of roxatidine in duodenal ulcer patients.
Bargiggia, S; Bensi, G; Bianchi Porro, G; Canali, A; Lazzaroni, M; Sangaletti, O, 1996
)
0.29
" Selective PAF, TXA2 and 5HT antagonists (WEB 2086, sulotroban and MCI-9042) clearly inhibited both the shape change and the aggregation induced by the appropriate agonist; in each case the effect of the antagonist was to move the dose-response curve to the right."( Studies on the effects of agonists and antagonists on platelet shape change and platelet aggregation in whole blood.
Heptinstall, S; Lösche, W; Sanderson, HM; Vickers, J, 1996
)
0.29
" L-734,217 in dogs was unaffected by dosage form or food."( Nonpeptide glycoprotein IIb/IIIa inhibitors. 8. Antiplatelet activity and oral antithrombotic efficacy of L-734,217.
Cook, JJ; Drag, MD; Duggan, ME; Gehret, JR; Gould, RJ; Hand, EL; Hartman, GD; Holahan, MA; Ihle, NC; Kothstein, T; Lyle, EA; Lynch, JJ; McCormick, GY; Perkins, JJ; Ramjit, DR; Sitko, GR; Stranieri, MT; Stupienski, RF; Wallace, AA, 1996
)
0.29
" Repeated administration of BTCP dose-dependently produced leftward and downward shifts of the cocaine dose-response curve."( Effects of repeated administration of N-[1-(2-benzo(b)-thiophenyl)cyclohexy]piperidine and cocaine on locomotor activity in C57BL/6 mice.
Kamenka, JM; Kleven, MS; Koek, W; Prinssen, EP; Vignon, J, 1996
)
0.29
" The reversal of scopolamine-induced impairment was characterized by the presence of an inverted U-shaped dose-response curve."( An inverted U-shaped curve for heptylphysostigmine on radial maze performance in rats: comparison with other cholinesterase inhibitors.
Braida, D; Griffini, P; Lamperti, M; Maggi, A; Paladini, E; Sala, M, 1996
)
0.29
" For these reasons, we carried out a prospective pharmacodynamic investigation in 48 patients with endoscopically proven duodenal ulcer using the well-established once daily dosing schedule of H2 blockers."( Absence of tolerance in duodenal ulcer patients treated for 28 days with a bedtime dose of roxatidine or ranitidine.
Belicchi, M; Celle, G; Cutela, P; Di Mario, F; Ferrana, M; Malesci, A; Mela, GS; Savarino, V; Termini, R; Vigneri, S; Zentilin, P, 1996
)
0.29
" Defining this interaction provides a basis for more rational dosing schemes when such combinations are used for anesthesia and allows the anesthetic potency of remifentanil relative to other opioids to be determined."( Reduction of isoflurane minimal alveolar concentration by remifentanil.
Glass, PS; Hoke, JF; Kapila, A; Lang, E; Sebel, PS; Shlugman, D, 1996
)
0.29
" The appropriate use of prokinetic agents in these groups requires an understanding of the unique dosage considerations that may be necessary to ensure safe, effective therapy."( Use of prokinetic agents in special populations.
Horn, JR, 1996
)
0.29
"After once-daily oral dosing in ovariectomized rats, raloxifene (LY139481) hydrochloride produced dose- and time-dependent reductions in serum cholesterol and high-density lipoprotein-cholesterol."( Hypocholesterolemic activity of raloxifene (LY139481): pharmacological characterization as a selective estrogen receptor modulator.
Bean, JS; Bensch, WR; Bryant, HU; Cole, HW; Cullinan, GJ; Glasebrook, AL; Kauffman, RF; Monroe, A; Phillips, DL; Roudebush, RE, 1997
)
0.3
" In the present article, the authors determined whether remifentanil dosing should be adjusted according to age and LBM, or whether these covariate effects were overshadowed by the interindividual variability present in the pharmacokinetics and pharmacodynamics."( Pharmacokinetics and pharmacodynamics of remifentanil. II. Model application.
Minto, CF; Schnider, TW; Shafer, SL, 1997
)
0.3
"Based on the EEG model, age and LBM are significant demographic factors that must be considered when determining a dosage regimen for remifentanil."( Pharmacokinetics and pharmacodynamics of remifentanil. II. Model application.
Minto, CF; Schnider, TW; Shafer, SL, 1997
)
0.3
" We report here three structural classes of 8-chlorobenzocycloheptapyridines as novel, nonpeptidic, nonsulfhydryl FPT inhibitors having antitumor activity in mice when dosed orally."( Antitumor 8-chlorobenzocycloheptapyridines: a new class of selective, nonpeptidic, nonsulfhydryl inhibitors of ras farnesylation.
Alvarez, C; Bishop, WR; Bryant, MS; Carr, D; Catino, J; Doll, RJ; Ganguly, AK; James, L; Kaminski, JJ; King, I; Kirschmeier, P; Li, Z; Lin, CC; Liu, M; Mallams, AK; Nardo, C; Njoroge, FG; Petrin, J; Remiszewski, SW; Rossman, RR; Snow, ME; Taveras, AG; Vibulbhan, B; Wang, S; Wong, J, 1997
)
0.3
" Similar dose-response activity was obtained for a control group consisting of six patients undergoing resection for colorectal carcinoma."( Abnormalities in the contractile properties of colonic smooth muscle in idiopathic slow transit constipation.
Gillespie, JI; Slater, BJ; Varma, JS, 1997
)
0.3
" Rapid biotransformation to minimally active metabolites results in short and predictable duration of action with no accumulation of effect on repeated dosing or with continuous infusion."( [Is remifentanil an ideal opioid for anesthesiologic management in the 21st century?].
Scholz, J; Steinfath, M, 1996
)
0.29
" This potentiation is dose-dependent at doses between 1 and 1000 micrograms/kg, IV but bell-shaped dose-response curves are obtained."( Effects of low and high doses of selective sigma ligands: further evidence suggesting the existence of different subtypes of sigma receptors.
Bergeron, R; Debonnel, G, 1997
)
0.3
" Diphemanil at progressive dosage was later introduced safely in two of these infants."( [Does stopping of oral feeding favour the occurrence of auriculoventricular block in premature infants treated with diphemanil?].
Autret, E; Blond, MH; Chantepie, A; Favre, A; Gold, F; Guérois, M; Ramponi, N; Rondeau, C, 1997
)
0.3
" The dosage could be doubled after 4 weeks."( Double-blind study of the effect of cisapride on constipation and abdominal discomfort as components of the irritable bowel syndrome.
Brandstätter, G; Dragosics, B; Hentschel, E; Judmaier, G; Schütze, K, 1997
)
0.3
" Guinea-pigs were dosed subcutaneously (s."( Central antitussive activity of the NK1 and NK2 tachykinin receptor antagonists, CP-99,994 and SR 48968, in the guinea-pig and cat.
Bolser, DC; DeGennaro, FC; Hey, JA; McLeod, RL; O'Reilly, S, 1997
)
0.3
" Following screening and placebo washout, patients received brofaromine (a combined MAO-A inhibitor/5-HT transport inhibitor) or placebo in a flexible dosing design."( Pharmacotherapy of post-traumatic stress disorder with a novel psychotropic.
Arbus, P; Crocq, L; Herlobsen, P; Katz, RJ; Lingjaerde, O; Lopez, G; Lott, MH; Loughrey, GC; MacFarlane, DJ; McIvor, R,
)
0.13
" In this situation, the selection of a correct assay dosage to study the MDR modulation mechanism was a problem."( Simultaneous determination of cytotoxic (adriamycin, vincristine) and modulator of resistance (verapamil, S 9788) drugs in human cells by high-performance liquid chromatography and ultraviolet detection.
Atassi, G; Dubois, J; Hanocq, M; Tassin, JP, 1997
)
0.3
" During general anaesthesia, any dosage of remifentanil may be used without undue lengthening of emergence times."( Remifentanil: when and how to use it.
Servin, F, 1997
)
0.3
" Dose-response curves were constructed using the putatively selective antagonists pirenzepine (M1), gallamine (M2) and 4-DAMP (M3: 4-diphenyl-acetoxy-N-methylpiperidine) and compared with the non-selective blocker, atropine."( Functional characterization of peripheral muscarinic subtypes in anesthetized cats.
Koss, MC, 1997
)
0.3
"In an international, multicentre, double-blind trial, to document the therapeutic equivalence of two dosing regimens of cisapride on endoscopic healing and symptom improvement in patients with proven reflux oesophagitis grade I or II (Savary-Miller)."( Comparison of two dosing regimens of cisapride in the treatment of reflux oesophagitis.
Bedogni, G; Bigard, MA; Hentschel, E; Hinojosa, J; Schütze, K; Van Waes, L, 1997
)
0.3
"High cisapride dosage in preterm, newborns and infants seems to favor QT prolongation which is reversible when dosage is reduced or drug is stopped."( [Long QT syndrome under cisapride in neonates and infants].
Aujard, Y; Bedu, A; Casasoprana, A; Cézard, JP; Denjoy, I; Faure, C; Lupoglazoff, JM, 1997
)
0.3
" Linkage to cisapride was probable, promoted by high dosage and cisapride metabolism inhibition by ranitidine, but its plasma concentration was not measured."( [Syncope with long QT interval in a 39 day-old infant treated with cisapride].
Autret, E; Champel, V; Jonville-Bera, AP; Olivier, C; Valdes, L, 1997
)
0.3
"This case report stresses the problem of cisapride dosage in infants and the question of an interaction between cisapride and ranitidine."( [Syncope with long QT interval in a 39 day-old infant treated with cisapride].
Autret, E; Champel, V; Jonville-Bera, AP; Olivier, C; Valdes, L, 1997
)
0.3
"8 mL, resulting in an inadvertent, 10-fold, iatrogenic, dosing error."( Cisapride poisoning.
Gibly, RL; Kloster, J; Osterloh, J; Theodorou, AA; Walter, FG, 1997
)
0.3
" After the baseline scan each subject was studied three times post dosing at various time points."( Time course of 5-HT2A receptor occupancy in the human brain after a single oral dose of the putative antipsychotic drug MDL 100,907 measured by positron emission tomography.
Dannals, RF; Gründer, G; Howard, DR; Offord, SJ; Ravert, HT; Salzmann, JK; Szymanski, S; Wilson, PD; Wong, DF; Yokoi, F, 1997
)
0.3
" Through an understanding of the pharmacodynamic interaction of volatile anesthetics with opioids and the pharmacokinetic processes responsible for the recovery from drug effect, optimal dosing schemes can thus be developed."( Drug interactions: volatile anesthetics and opioids.
Gan, TJ; Ginsberg, B; Glass, PS; Howell, S, 1997
)
0.3
" Dose-response curves to (+)-WIN 55212 and CP 55940 were shifted to the right, with no reduction of maximal response, by pretreatment with SR141716A (31."( Inhibition by cannabinoid receptor agonists of acetylcholine release from the guinea-pig myenteric plexus.
Coutts, AA; Pertwee, RG, 1997
)
0.3
" Because plasma levels of total raloxifene were low relative to clinical values in postmenopausal women, dose-response data for raloxifene are required."( Raloxifene inhibits aortic accumulation of cholesterol in ovariectomized, cholesterol-fed rabbits.
Bjarnason, NH; Byrjalsen, I; Christiansen, C; Haarbo, J; Kauffman, RF, 1997
)
0.3
" The thrombin inhibitors were given intravenously, and complete concentration- and/or dose-response curves were constructed."( The importance of enzyme inhibition kinetics for the effect of thrombin inhibitors in a rat model of arterial thrombosis.
Deinum, J; Elg, M; Gustafsson, D, 1997
)
0.3
" Two groups of rats were dosed with remifentanil [25 micrograms/kg/min (n = 8)] and remifentanil plus esmolol [25 and 200 mg/kg/min (n = 7)] for 20 min."( Evaluating a possible pharmacokinetic interaction between remifentanil and esmolol in the rat.
Eddington, ND; Haidar, SH; Hoke, JF; Liang, Z; Moreton, JE; Muir, KT, 1997
)
0.3
" We therefore compared two dosage regimens of cisapride with placebo over a period of 6 months in patients with evidence of gastrooesophageal reflux, initially treated with antisecretory medication, with regard to maintaining symptom relief and satisfaction with treatment."( The effect of cisapride in maintaining symptomatic remission in patients with gastro-oesophageal reflux disease.
Carling, L; Hatlebakk, JG; Johnsson, F; Thøgersen, T; Vilien, M; Wetterhus, S, 1997
)
0.3
" Cisapride mixed with propylene glycol and administered rectally at a dosage of 1 mg/kg is poorly and incompletely absorbed."( Pharmacokinetics of cisapride in horses after intravenous and rectal administration.
Bowman, KF; Cook, G; Papich, MG; Roberts, MC, 1997
)
0.3
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, and dosage and administration of donepezil are reviewed."( Donepezil: an anticholinesterase inhibitor for Alzheimer's disease.
Shintani, EY; Uchida, KM, 1997
)
0.3
" At dosing and at predetermined intervals beginning 30 minutes postdose, patients recorded migraine pain severity, clinical disability, and presence of associated migraine symptoms."( Naratriptan is effective and well tolerated in the acute treatment of migraine. Results of a double-blind, placebo-controlled, parallel-group study. Naratriptan S2WA3001 Study Group.
Asgharnejad, M; Elkind, A; Klassen, A; Laurenza, A; Webster, C,
)
0.13
" The design of succinic acid esters of high insulinotropic potential might thus allow efficient stimulation of insulin secretion in non-insulin-dependent diabetes, without requiring unpractical high dosage and without running the risk of an undesirable increase in gluconeogenesis."( Stimulation of insulin release and potentiation of the insulinotropic action of antidiabetic agents by 1,2,3-tri(methylsuccinyl)glycerol ester in anaesthetized rats.
Björkling, F; García-Martínez, JA; Malaisse, WJ; Valverde, I; Villanueva-Peñacarrillo, ML, 1997
)
0.3
" Each rat was dosed with REMI (15 micrograms/kg/min), and REMI & ES (15 micrograms/kg/min and 600 micrograms/kg/min) for 21 minutes in a random crossover design."( The pharmacokinetics and electroencephalogram response of remifentanil alone and in combination with esmolol in the rat.
Eddington, ND; Haidar, SH; Hoke, JF; Liang, Z; Moreton, JE; Muir, KT, 1997
)
0.3
" In the PK/PD cohort of TIMI 12, 106 patients were randomized to receive one of seven dosing regimens of sibrafiban, ranging from 5 mg daily to 10 mg twice daily for 28 days."( Randomized trial of an oral platelet glycoprotein IIb/IIIa antagonist, sibrafiban, in patients after an acute coronary syndrome: results of the TIMI 12 trial. Thrombolysis in Myocardial Infarction.
Ault, K; Borzak, S; Braunwald, E; Cannon, CP; Feldman, R; Hamilton, SA; Henry, TD; McCabe, CH; Mueller, HS; Novotny, WF; Palmeri, ST; Rothman, JM; Tischler, MD, 1998
)
0.3
"The oral glycoprotein IIb/IIIa antagonist sibrafiban achieved effective, long-term platelet inhibition with a clear dose-response but at the expense of a relatively high incidence of minor bleeding."( Randomized trial of an oral platelet glycoprotein IIb/IIIa antagonist, sibrafiban, in patients after an acute coronary syndrome: results of the TIMI 12 trial. Thrombolysis in Myocardial Infarction.
Ault, K; Borzak, S; Braunwald, E; Cannon, CP; Feldman, R; Hamilton, SA; Henry, TD; McCabe, CH; Mueller, HS; Novotny, WF; Palmeri, ST; Rothman, JM; Tischler, MD, 1998
)
0.3
"Our study shows clearly that the efficacy of a single therapeutic dosage of cetirizine is consistently good for suppression of cutaneous reactivity to histamine in healthy volunteers."( Consistency of the efficacy of cetirizine and ebastine on skin reactivity.
Benabdesselam, O; Frossard, N; Melac, M; Pauli, G, 1998
)
0.3
" All three showed excellent oral bioavailability in vivo in nude mice and cynomolgus monkeys and exhibited excellent antitumor efficacy against a series of tumor cell lines when dosed orally in nude mice."( Inhibitors of farnesyl protein transferase. 4-Amido, 4-carbamoyl, and 4-carboxamido derivatives of 1-(8-chloro-6,11-dihydro-5H-benzo[5,6]- cyclohepta[1,2-b]pyridin-11-yl)piperazine and 1-(3-bromo-8-chloro-6,11- dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridi
Bishop, WR; Bryant, MS; Carr, DM; Catino, JJ; Chen, J; Chen, KJ; Dell, J; Doll, RJ; Ganguly, AK; Girijavallabhan, VM; Kirschmeier, P; Korfmacher, WA; Lee, S; Li, Z; Lin, CC; Lipari, P; Liu, M; Mallams, AK; Nardo, C; Nomeir, AA; Patton, R; Petrin, J; Rossman, RR; Wang, L; Wang, S, 1998
)
0.3
"We evaluated the efficacy and safety of a twice-daily dosage regimen of cisapride 20 mg in relieving the symptoms of mild-moderate gastroesophageal reflux disease (GERD) in patients with moderate intensity heartburn and no history of erosive esophagitis."( Cisapride 20 mg b.i.d. provides symptomatic relief of heartburn and related symptoms of chronic mild to moderate gastroesophageal reflux disease. CIS-USA-52 Investigator Group.
Castell, DO; Clyde, C; Hasner, D; Lambert, R; Patterson, D; Sigmund, C; Zeldis, JB, 1998
)
0.3
" The reversal of scopolamine-induced impairment was characterized by an inverted U-shaped dose-response curve."( Long-lasting antiamnesic effect of a novel anticholinesterase inhibitor (MF268).
Braida, D; Colibretti, L; Griffini, P; Lamperti, M; Paladini, E; Sala, M, 1998
)
0.3
" Based on extensive assessment of the drug's pharmacokinetic profile, the currently approved initial oral dosing regimen for cisapride is 10 mg QID."( Pharmacokinetic profile of cisapride 20 mg after once- and twice-daily dosing.
Clyde, C; Herron, J; Lee, P; Mechlinski, W; Pesco-Koplowitz, L; Zhou, H,
)
0.13
" Capsaicin (10(-6) M) caused relaxation and desensitization that was overcome by long recovery periods and substance P dosing (10(-8) M)."( Activation of non-adrenergic non-cholinergic inhibitory pathways by endogenous and exogenous tachykinins in the ferret lower oesophageal sphincter.
Blackshaw, LA; Lynn, PA; Smid, SD; Templeman, R, 1998
)
0.3
" Using a dosing regimen known to produce pharmacological and behavioral tolerance, mice were treated with Delta9-tetrahydrocannabinol (Delta9-THC) twice a day for 1 wk."( CB1 receptor antagonist precipitates withdrawal in mice exposed to Delta9-tetrahydrocannabinol.
Cook, SA; Lowe, JA; Martin, BR, 1998
)
0.3
" It is tempting to speculate that these characteristics will make remifentanil an easy drug to titrate, and that clinicians will not need to consider patient covariates such as advanced age when choosing a dosing regimen."( The role of newer opioids in geriatric anesthesia.
Shafer, SL, 1998
)
0.3
" The dose-response relationship and possible tachyphylaxis were tested for each chemical."( Activation of neurons in rat trigeminal subnucleus caudalis by different irritant chemicals applied to oral or ocular mucosa.
Carstens, E; Handwerker, HO; Kuenzler, N, 1998
)
0.3
" Neither dosage of lubeluzole had any statistically or clinically relevant effects on the QTc."( Cardiovascular safety of lubeluzole (Prosynap(R)) in patients with ischemic stroke.
Diener, HC; Haan, J; Hacke, W; Hantson, L; Hennerici, M; Lees, KR; Timmerhuis, T,
)
0.13
" The simulations illustrated that remifentanil pharmacokinetics are not grossly different in obese versus lean subjects and that TBW based dosing in obese patients can result in excessively high remifentanil concentrations."( Remifentanil pharmacokinetics in obese versus lean patients.
Egan, TD; Gupta, SK; Huizinga, B; Jaarsma, RL; Muir, KT; Sperry, RJ; Yee, JB, 1998
)
0.3
" Clinically this means that remifentanil dosing regimens should be based on ideal body weight (or LBM) and not TBW."( Remifentanil pharmacokinetics in obese versus lean patients.
Egan, TD; Gupta, SK; Huizinga, B; Jaarsma, RL; Muir, KT; Sperry, RJ; Yee, JB, 1998
)
0.3
" Pretreatment with BQ123, an ETA receptor selective antagonist, shifted the dose-response curve to the right, whereas pretreatment with BQ788, an ETB receptor selective antagonist, showed little effect."( Studies on the endothelin-1-induced contraction of rat granulation tissue pouch mediated by myofibroblasts.
Goto, T; Ohtsuki, I; Yanaga, F, 1998
)
0.3
" Both dosage regimens were well tolerated; no clinically significant changes in laboratory or vital sign parameters were observed in any subject."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following evening administration.
Friedhoff, LT; Rogers, SL; Tiseo, PJ, 1998
)
0.3
"The measured pharmacokinetic and pharmacodynamic parameters for both 5 and 10 mg day(-1) donepezil administered in the evening are in good agreement with previous results obtained with morning administration, indicating no time of dosing effect."( Pharmacokinetic and pharmacodynamic profile of donepezil HCl following evening administration.
Friedhoff, LT; Rogers, SL; Tiseo, PJ, 1998
)
0.3
" These results suggest that the administration of donepezil to patients with hepatic disease in clinical practice should not require any dosing modifications."( An evaluation of the pharmacokinetics of donepezil HCl in patients with impaired hepatic function.
Friedhoff, LT; Perdomo, CA; Tiseo, PJ; Vargas, R, 1998
)
0.3
"To estimate the optimum dosing regimen and delivery system for remifentanil, a new opioid, using computer simulations based on information from pharmacokinetic and pharmacodynamic models available for fentanyl, alfentanil and remifentanil, as well as from clinical trials of fentanyl and alfentanil."( [Characterization of dose profile of remifentanil with computer simulation: comparative study with fentanyl and alfentanyl].
Gambús, PL; Minto, CF; Schnider, TW, 1998
)
0.3
" Dosing guidelines for remifentanil, fentanyl and alfentanil were estimated for three methods of administration (bolus, bolus + variable continuous infusion or constant continuous infusion)."( [Characterization of dose profile of remifentanil with computer simulation: comparative study with fentanyl and alfentanyl].
Gambús, PL; Minto, CF; Schnider, TW, 1998
)
0.3
" The results are fairly consistent with clinical evidence, demonstrating the power of pharmacokinetic and pharmacodynamic models for rationally establishing opioid dosing guidelines."( [Characterization of dose profile of remifentanil with computer simulation: comparative study with fentanyl and alfentanyl].
Gambús, PL; Minto, CF; Schnider, TW, 1998
)
0.3
" The implications of tailoring repaglinide treatment to meals were examined in a study where repaglinide was dosed either morning and evening, or with each main meal (i."( Repaglinide--prandial glucose regulator: a new class of oral antidiabetic drugs.
Owens, DR, 1998
)
0.3
" PD, SB, and BQ produced parallel concentration-dependent rightward shifts in the S6c dose-response curve in the kidney."( PD 142893, SB 209670, and BQ 788 selectively antagonize vascular endothelial versus vascular smooth muscle ET(B)-receptor activity in the rat.
Cheng, XM; Haleen, SJ; Keiser, JA; Schroeder, RL, 1998
)
0.3
" Furthermore, its long half-life supports a simple and convenient once-daily dosing regimen."( Clinical profile of donepezil in the treatment of Alzheimer's disease.
Doody, RS, 1999
)
0.3
" The results indicate that dimaprit, an H2 agonist, facilitated retention (25 and 50 pg) with a U-shaped dose-response curve typical of drugs acting at postsynaptic receptors."( Effect of histamine H2 and H3 receptor modulation in the septum on post-training memory processing.
Flood, JF; Morley, JE; Uezu, K, 1998
)
0.3
"), which facilitates histamine release, significantly shifted the methamphetamine dose-response curve to the left when tested together with different doses of methamphetamine and markedly extended the time-course of methamphetamine's discriminative-stimulus effects."( Potentiation of the discriminative-stimulus effects of methamphetamine by the histamine H3 receptor antagonist thioperamide in rats.
Goldberg, SR; Munzar, P; Nosál, R, 1998
)
0.3
" Brain tissue sodium content was significantly reduced at the dosage of 300 mg/kg (P<0."( Treatment of brain edema with a nonpeptide arginine vasopressin V1 receptor antagonist OPC-21268 in rats.
Bemana, I; Nagao, S, 1999
)
0.3
" Hypothermia shifted the dose-response curves to the right for the negative chronotropic and inotropic effects of verapamil and for the negative chronotropic and positive inotropic effects of zatebradine, but not for the negative chronotropic and positive inotropic effects of E-4031."( Effects of low temperature on the chronotropic and inotropic responses to zatebradine, E-4031 and verapamil in isolated perfused dog atria.
Chiba, S; Furukawa, Y; Hoyano, Y; Kasama, M; Oguchi, T, 1998
)
0.3
" Our results indicated that acute exercise induced the following effects: (1) the dose-response curves of ACh and CLO shifted to the left; (2) the high-affinity M3 binding sites increased in number but not in affinity; (3) the alpha2 binding sites decreased in number but increased in affinity."( Acute exercise enhances receptor-mediated endothelium-dependent vasodilation by receptor upregulation.
Chen, H; Cheng, L; Hsu, L; Jen, CJ; Lin, MT; Yang, C, 1999
)
0.3
" Our results demonstrate that the HSN tumour vasculature is selectively responsive to IRL 1620 at doses > 1 nmol kg(-1) compared with the majority of normal tissues with the exception of the small intestine, and that only the tumour response is highly sensitive to BQ-788 antagonism, under the experimental dosing regime investigated."( Modification of blood flow in the HSN tumour and normal tissues of the rat by the endothelin ET(B) receptor agonist, IRL 1620.
Bell, KM; Chaplin, DJ; Poole, BA; Prise, VE; Tozer, GM, 1999
)
0.3
" Dose-response curves were obtained for the effects of several 5-HT2 receptor antagonists on response magnitude."( Effect of 5-HT2 receptor antagonists on a cranial nerve reflex in the rabbit: evidence for inverse agonism.
Harvey, JA; Hood, H; Romano, AG; Welsh, SE, 1999
)
0.3
" The newer mast-cell stabilizing agent nedocromil sodium has a similar safety profile to sodium cromoglycate, but is more potent and has a more convenient twice-daily dosing regimen."( Treating severe eye allergy.
Verin, P, 1998
)
0.3
" Twelve-lead electrocardiography was performed before dosing on day 1 and repeated 4 hours postdose on days 1, 5, and 10."( Pharmacokinetics and electrocardiographic effect of ebastine in young versus elderly healthy subjects.
Argenti, D; Garcia, J; Heald, D; Huang, MY; Wilson, J, 1998
)
0.3
" Major reasons for noncompliance among these patients were an absence of symptoms and an inconvenient dosage schedule."( Compliance with therapy for ulcer disease: clinical experience and review of the literature.
Battaglia, G; Bo, ND; DiMario, F; Ferrana, M; Mela, GS; Pilotto, A; Salandin, S; Savarino, V; Vianello, F; Vigneri, S,
)
0.13
" This large trial uses twice daily dosage regimens to produce the plasma concentrations which were associated with less bleeding in the earlier dose-ranging trial."( Sibrafiban.
Dooley, M; Goa, KL, 1999
)
0.3
" The mean log(AUC) values after multiple dosing were significantly higher than the values obtained after a single dose."( Pharmacokinetic profiles of repaglinide in elderly subjects with type 2 diabetes.
Hatorp, V; Huang, WC; Strange, P, 1999
)
0.3
" Emesis induced by RS14203 exhibited a dose-response relationship but no such relationship was seen for R-rolipram or CT-2450."( Emesis induced by inhibitors of type IV cyclic nucleotide phosphodiesterase (PDE IV) in the ferret.
Choudhury, I; Robichaud, A; Rodger, IW; Tattersall, FD, 1999
)
0.3
" A dose-response effect was evident, with the 10 mg/day donepezil group demonstrating greater benefits in all outcome measures than the 5 mg/day group."( The effects of donepezil in Alzheimer's disease - results from a multinational trial.
Burns, A; Friedhoff, LT; Gauthier, S; Hecker, J; Möller, HJ; Petit, H; Rogers, SL; Rossor, M,
)
0.13
" These benefits, as well as a simple, once-daily dosing regimen, make donepezil a viable therapeutic option for AD patients."( Clinical benefits of a new piperidine-class AChE inhibitor.
Doody, RS, 1999
)
0.3
" At the higher doses, ADP-induced platelet aggregation was almost completely inhibited while a clear dose-response could be observed with TRAP-induced inhibition of platelet aggregation at sibrafiban doses of 5 to 12 mg."( Pharmacokinetics and pharmacodynamics of Ro 44-3888 after single ascending oral doses of sibrafiban, an oral platelet aggregation inhibitor, in healthy male volunteers.
Goggin, T; Machin, SJ; Mackie, IJ; Timm, U; Wittke, B; Zell, M, 1999
)
0.3
" There was no obvious synergistic or antagonistic toxicity when flavopiridol was combined with radiotherapy or cisplatin dosed at the IC50 despite the observation that radiotherapy and flavopiridol led to more profound G2/M arrest than either agent alone."( In vitro evaluation of flavopiridol, a novel cell cycle inhibitor, in bladder cancer.
Astumian, M; Chien, M; Liebowitz, D; Rinker-Schaeffer, C; Stadler, WM, 1999
)
0.3
" Methysergide counteracted the effect of thioperamide in the open-field test only at a high dosage (50 mg/kg)."( Combined action of thioperamide plus scopolamine, diphenhydramine, or methysergide on memory in mice.
Di Carlo, G; Ghi, P; Molinengo, L, 1999
)
0.3
" A flexible preprandial only dosing regimen of repaglinide significantly lowers the risk of hypoglycaemia if a meal is missed or postponed."( Repaglinide: a new short-acting insulinotropic agent for the treatment of type 2 diabetes.
Owens, DR, 1999
)
0.3
" Once-daily dosing resulted in high peak-trough excursions in active drug concentrations: trough concentrations were 21% +/- 6% of peak."( Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered IIb/IIIa antagonist, in patients with acute coronary syndrome.
Braunwauld, E; Cannon, CP; Modi, NB; Novotny, W; Reimann, JD, 1999
)
0.3
" They both potentiated the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease, dosed at 10 mg/kg ip, but 48 was not active at 30 mg/kg po."( Subtype-selective N-methyl-D-aspartate receptor antagonists: synthesis and biological evaluation of 1-(arylalkynyl)-4-benzylpiperidines.
Bigge, CF; Boxer, PA; Cai, SX; Gregory, TF; Hawkinson, JE; Konkoy, CS; Meltzer, LT; Serpa, K; Whittemore, ER; Wise, LD; Woodward, RM; Wright, JL; Zhou, ZL, 1999
)
0.51
" Treatment of Chinese hamster ovary (CHO) cells expressing the cannabinoid CB1 receptor with the cannabinoid CP 55,940, {(-)-cis-3-[2-hydroxy-4-(1,1-dimethylheptyl)phenyl]-trans-4-(3-hyd roxypropyl) cyclohexan-1-ol} resulted in cyclic AMP accumulation in a dose-response manner, an accumulation blocked by the cannabinoid CB1 receptor-specific antagonist SR 141716A, {N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-me thyl-1H-pyrazole-3-carboxamide hydrochloride}."( Dual intracellular signaling pathways mediated by the human cannabinoid CB1 receptor.
Calandra, B; Carillon, C; Delpech, M; Ferrara, P; Kernéis, A; Le Fur, G; Portier, M; Shire, D, 1999
)
0.3
" One of the most important and difficult steps in the drug development process is defining the dose-response relationship."( The role of positron emission tomography in the drug development of M100907, a putative antipsychotic with a novel mechanism of action.
Nyberg, S; Offord, SJ; Wong, DF, 1999
)
0.3
"To report toxicity resulting from donepezil administration following a tenfold dosing error."( Donepezil overdose: a tenfold dosing error.
Edwards, R; Klein-Schwartz, W; Shepherd, G,
)
0.13
"A tenfold dosing error caused donepezil toxicity."( Donepezil overdose: a tenfold dosing error.
Edwards, R; Klein-Schwartz, W; Shepherd, G,
)
0.13
", but without changing the maximum response or the bell-shaped nature of the dose-response curve for granisetron."( 5-HT4 receptor antagonism potentiates inhibition of intestinal allodynia by 5-HT3 receptor antagonism in conscious rats.
Banner, SE; Sanger, GJ; Smith, MI, 1999
)
0.3
" Studies were carried out in control animals and after dosing with phenserine, a selective centrally active AChE inhibitor; neostigmine, a peripheral cholinesterase inhibitor; and a combination of the two drugs."( Simplified methods for in vivo measurement of acetylcholinesterase activity in rodent brain.
Kilbourn, MR; Sherman, PS; Snyder, SE, 1999
)
0.3
" Nonetheless, our data show that the postoperative requirement for these rapidly acting drugs is qualitatively similar to that for other opioids in that dosage escalation does not occur."( Lack of rapid development of opioid tolerance during alfentanil and remifentanil infusions for postoperative pain.
Checketts, MR; Kenny, GN; Schraag, S, 1999
)
0.3
" HPLC dosage of BM 212, using a specific method, showed that BM 212 represented 62% of the urine radioactivity."( Pharmacokinetics, metabolism and bioavailability of the new anti-allergic drug BM 113. Part III: Pharmacokinetics, metabolism, dose dependency and gender effect after single or repeated administration to human healthy volunteers.
Buzas, A; Duchêne, P; Houin, G; Ladure, P; Laneury, JP; Merour, JY; Ollivier, R; Tran, G, 1999
)
0.3
" Within 96 h of dosing with (14)C-repaglinide, 90% of the administered dose appeared in the faeces and 8% was excreted in urine."( Absorption, metabolism and excretion of a single oral dose of (14)C-repaglinide during repaglinide multiple dosing.
De Merbel, NC; Hansen, KT; Hatorp, V; Jonkman, JH; Kramer Nielsen, K; Oosterhuis, B; van Heiningen, PN; van Lier, JJ, 1999
)
0.3
"After oral dosing with repaglinide, the mean peak plasma concentration was rapidly attained and, thereafter, plasma concentrations decreased promptly."( Absorption, metabolism and excretion of a single oral dose of (14)C-repaglinide during repaglinide multiple dosing.
De Merbel, NC; Hansen, KT; Hatorp, V; Jonkman, JH; Kramer Nielsen, K; Oosterhuis, B; van Heiningen, PN; van Lier, JJ, 1999
)
0.3
" When dosed orally, this compound potentiates the effects of L-DOPA in the 6-hydroxydopamine-lesioned rat, a model of Parkinson's disease."( Discovery of subtype-selective NMDA receptor ligands: 4-benzyl-1-piperidinylalkynylpyrroles, pyrazoles and imidazoles as NR1A/2B antagonists.
Boxer, PA; Gregory, TF; Meltzer, LT; Serpa, KA; Wise, LD; Wright, JL, 1999
)
0.3
"Our study shows clearly that the efficacy of a single therapeutic dosage of cetirizine is greater and consistently better than that of ebastine for suppression of cutaneous reactivity to histamine 4 h after treatment in healthy volunteers."( Consistency and efficacy of cetirizine (10 mg) versus ebastine (20 mg) at 4 h on skin reactivity.
Benabdesselam, O; Duvernelle, C; Frossard, N; Melac, M; Pauli, G; Purohit, A, 1999
)
0.3
" Dosage requirements, vital functions, oxygen saturation (as achieved by pulse oximetry, psO(2)), adverse drug effects and the level of sedation (LOS 1-5; 1 = asleep/unarousable, 4 = calm/awake) were recorded."( [Remifentanil for oocyte retrieval: A new single-agent monitored anaesthesia care technique].
Biedler, A; Fleser, R; Grüness, V; Hammadeh, ME; Wilhelm, W, 1999
)
0.3
" In this dose-response study, we evaluated the efficacy of a remifentanil infusion in maintaining hemodynamic stability during intracranial surgery under desflurane anesthesia."( The use of a remifentanil infusion for hemodynamic control during intracranial surgery.
Gesztesi, Z; Mootz, BL; White, PF, 1999
)
0.3
" The dose-response relations for extracellular Mg2+ blockade of INMDA indicated a high affinity binding of Mg2+ to NMDA receptors at membrane potentials more negative than -60 mV, independent of postnatal age."( Early postnatal switch in magnesium sensitivity of NMDA receptors in rat CA1 pyramidal cells.
Kirson, ED; Konnerth, A; Schirra, C; Yaari, Y, 1999
)
0.3
" It is therefore used in a meal-related dosing regimen; repaglinide is taken with each main meal."( Repaglinide--a new compound for the treatment of patients with type 2 diabetes.
Wolffenbuttel, BH, 1999
)
0.3
" The dose-response curve of WIN55212-2 is shifted parallel to the right by SR141716A."( Involvement of cannabinoid receptors in the intraocular pressure-lowering effects of WIN55212-2.
Slowey, CA; Song, ZH, 2000
)
0.31
" The first large-scale study designed to evaluate the efficacy of Aricept administered at a daily dosage of 5 to 10 mg was conducted over 14 weeks."( [Cholinergic hypothesis and Alzheimer's disease: the place of donepezil (Aricept)].
Bertogliati, C; Gokalsing, E; Robert, PH, 1999
)
0.3
" Initial studies determined the dose-response relationship for each of the two drugs given intraperitoneally twice a day, while monitoring systolic arterial pressure (SAP), mean arterial pressure (MAP) and heart rate (HR) measured by the tail-cuff method."( Kappa-opioid receptors behind the blood-brain barrier are involved in the anti-hypertensive effects of systemically administered kappa-agonists in the conscious spontaneously hypertensive rat.
Ingenito, AJ; Shen, S, 1999
)
0.3
" There was no dose-response relation for Vf (10."( Rate of CSF formation and resistance to reabsorption of CSF during sevoflurane or remifentanil in rabbits.
Artru, AA; Momota, T, 2000
)
0.31
" Beyond the dosing site, cystic degeneration of the liver was described in 2-year 200-mg KBR 3023/kg body wt/day males."( Chronic toxicity and carcinogenicity testing in the Sprague-Dawley rat of a prospective insect repellant (KBR 3023) using the dermal route of exposure.
Christenson, WR; Croutch, C; Lake, SG; Sangha, GK; Sheets, LP; Wahle, BS, 1999
)
0.3
" No direct drug-drug interactions were found in these studies, suggesting that repaglinide may be coprescribed with cimetidine, digoxin, or theophylline at the dosage used for monotherapy."( Drug interaction studies with repaglinide: repaglinide on digoxin or theophylline pharmacokinetics and cimetidine on repaglinide pharmacokinetics.
Hatorp, V; Thomsen, MS, 2000
)
0.31
" Although adjustment of starting doses of repaglinide is not necessary for renal impairment or renal failure, severe impairment may require more care when upward adjustments of dosage are made."( Pharmacokinetics of repaglinide in subjects with renal impairment.
Andersen, MP; Hatorp, V; Huang, WC; Marbury, TC; Nielsen, KK; Ruckle, JL; Strange, P, 2000
)
0.31
" Compound 11a also potentiated the effects of L-DOPA in a rat model of Parkinson's disease (the 6-hydroxydopamine-lesioned rat), dosed at 30 mg/kg orally."( Subtype-selective N-methyl-D-aspartate receptor antagonists: benzimidazalone and hydantoin as phenol replacements.
Meltzer, LT; Schelkun, RM; Serpa, K; Whittemore, ER; Wise, LD; Woodward, RM; Yuen, PW, 2000
)
0.31
" Donepezil (5 and 10 mg) is an agent with a simple once-daily dosage schedule which improves cognition and global clinical function in the short (up to 24 weeks) and long term (up to about 1 year) in patients with mild to moderate Alzheimer's disease."( Donepezil: a review of its use in Alzheimer's disease.
Dooley, M; Lamb, HM, 2000
)
0.31
" On the basis of these results, a dosing regimen was selected for the phase III Blockage of the Glycoprotein IIb/IIIa Receptor to Avoid Vascular Occlusion (BRAVO) trial based on pharmacodynamics and drug tolerability."( Design of the blockade of the glycoprotein IIb/IIIa receptor to avoid vascular occlusion (BRAVO) trial.
Amarenco, P; Califf, R; Chan, R; Davis, S; Diener, HC; Easton, JD; Ferguson, J; Fitzgerald, D; Graffagnino, C; Granett, J; Harrington, R; Ilson, B; Koudstaal, PJ; Samuels, R; Shuaib, A; Theroux, P; Topol, EJ; Van de Werf, F; Willerson, JT, 2000
)
0.31
" Ifenprodil dose-response curves for all receptors were biphasic."( Electrophysiological analysis of NMDA receptor subunit changes in the aging mouse cortex.
Kuehl-Kovarik, MC; Magnusson, KR; Partin, KM; Premkumar, LS, 2000
)
0.31
"We examined the effects of Delta 9-tetrahydrocannabinol (Delta 9-THC), (R)-(+)-arachidonyl-1'-hydroxy-2'-propylamide ((R)-methanandamide, AM 356), SR 141716, and d-amphetamine on fixed-ratio (FR) responding maintained by food in rats before and during daily dosing with Delta 9-THC."( Effects of Delta 9-tetrahydrocannabinol, (R)-methanandamide, SR 141716,and d-amphetamine before and during daily Delta 9-tetrahydrocannabinol dosing.
Goutopoulos, A; Järbe, TU; Lamb, RJ; Lin, S; Makriyannis, A, 2000
)
0.31
" In the REM groups, the dosage of PRO (75 microg."( Recovery after anesthesia with remifentanil combined with propofol, desflurane, or sevoflurane for otorhinolaryngeal surgery.
Loop, T; Priebe, HJ, 2000
)
0.31
"Overall, 451 patients with a recent cardiovascular or cerebrovascular acute ischemic event were randomized in a double-blind fashion to 1 of 5 dosing regimens for 12 weeks: placebo or 5, 20, 50, or 100 mg lotrafiban, both twice daily with 300 to 325 mg/d aspirin."( Dose-finding, safety, and tolerability study of an oral platelet glycoprotein IIb/IIIa inhibitor, lotrafiban, in patients with coronary or cerebral atherosclerotic disease.
Armstrong, PW; Califf, RM; Card, T; Chan, R; Graffagnino, C; Granett, J; Harrington, RA; Joseph, DM; Kereiakes, DJ; Samuels, R; Sigmon, KN; Topol, EJ; Van De Werf, F, 2000
)
0.31
" Linking up with the previous studies, the paper investigated the effects of two auxiliary substances--cellulose derivatives (hydroxyethylcellulose, methylcellulose)--and their concentration on the pharmaceutical availability of the potential drug XX B from the dosage form."( [Effect of macromolecular substances on pharmaceutical availability of a potential local anesthetic].
Svehlová, E, 2000
)
0.31
" The pharmacokinetic profile of R is organ-independent and the dosing regimen must be regulated in elderly patients by reducing the bolus and infusion doses, and in obese subjects by calculating the intravenous dosages as a function of age and lean body mass."( [Remifentanil in anesthesia and intensive care].
Cafiero, T; De Cillis, P; Mastronardi, P, 2000
)
0.31
" In studies in mesenteric artery rings suspended in myographs, we observed a leftward shift in the dose-response curve for ET-1 after selective blockade of ET(B) receptors with BQ-788 in 3- but not 35-day-old swine."( Endothelin-mediated vasoconstriction in postischemic newborn intestine.
Miller, CE; Nankervis, CA; Schauer, GM, 2000
)
0.31
" On the other hand, lubeluzole treatment by the current dosage schedule was not associated with a significant safety problem."( Lubeluzole in acute ischemic stroke treatment: A double-blind study with an 8-hour inclusion window comparing a 10-mg daily dose of lubeluzole with placebo.
Cortens, M; Diener, HC; Ford, G; Grotta, J; Hacke, W; Kaste, M; Koudstaal, PJ; Wessel, T, 2000
)
0.31
" However, these trials employed fixed dosing and mealtime regimens, so repaglinide was not used as intended."( Prandial glucose regulation with repaglinide: its clinical and lifestyle impact in a large cohort of patients with Type 2 diabetes.
Bauer, C; Dieken, ML; Frank, M; Landgraf, R, 2000
)
0.31
" However, the incidence of intraoperative adverse events and other postoperative sequelae, recovery times, pain and nausea visual analog scale scores, opioid analgesic dosage requirements in the postanesthetic care unit, and satisfaction survey responses were similar between groups."( A comparison of the cost-effectiveness of remifentanil versus fentanyl as an adjuvant to general anesthesia for outpatient gynecologic surgery.
Beers, RA; Calimlim, JR; Camporesi, EM; Esposito, BF; Uddoh, E, 2000
)
0.31
" The MOR internalization is dose-dependent, with a similar dose-response to that observed for opioid-induced increases in potassium conductance."( Postsynaptic signaling via the [mu]-opioid receptor: responses of dorsal horn neurons to exogenous opioids and noxious stimulation.
Abbadie, C; Basbaum, AI; Marek, K; Trafton, JA, 2000
)
0.31
" A comparable bell-shaped dose-response relation was seen in the social exploration test in rats."( NKP608: a selective NK-1 receptor antagonist with anxiolytic-like effects in the social interaction and social exploration test in rats.
Brugger, F; Gentsch, C; Hauser, K; Ofner, S; Schilling, W; Vassout, A; Veenstra, S, 2000
)
0.31
" The present study investigated the dose-response characteristics of donepezil, tacrine, rivastigmine and metrifonate in inducing tremor, lacrimation, salivation and hypothermia and the duration of action of these compounds in Lister hooded rats."( Comparison of donepezil-, tacrine-, rivastigmine- and metrifonate-induced central and peripheral cholinergically mediated responses in the rat.
Dronfield, S; Egan, K; Green, AR; Marsden, CA, 2000
)
0.31
"25 microgram/kg/min, or sufentanil (S-group) 1 microgram/kg before surgery with dosage adjustments according to haemodynamic parameters."( [Endocrine stress parameters during TIVA with remifentanil or sufentanil].
Bastian, C; Brockmann, C; Raasch, W, 2000
)
0.31
" This compound has excellent oral activity at 4 h after oral dosing (1 mg/kg), inhibiting methacholine-induced bronchoconstriction in dogs, and may be useful in clinical situations in which M(3) over M(2) selectivity is desirable."( A potent, long-acting, orally active (2R)-2-[(1R)-3, 3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: novel muscarinic M(3) receptor antagonist with high selectivity for M(3) over M(2) receptors.
Hasegawa, T; Hirose, H; Kakikawa, T; Kawakami, K; Kimura, T; Kobayashi, K; Mase, T; Mitsuya, M; Noguchi, K; Numazawa, T; Ogino, Y; Ohtake, N; Sato, A; Satoh, A, 2000
)
0.31
" The dose-response relationship and the effective dose for at least 50% of the subjects (ED(50)) were determined."( The effect of remifentanil on the heat pain threshold in volunteers.
Brannath, W; Felleiter, P; Gustorff, B; Hoerauf, KH; Kress, HG; Nahlik, G; Spacek, A, 2001
)
0.31
" When injected alone, SR141716A produced, with the highest dosage used, a significant reduction in the latency of the NR."( Metabotropic and NMDA glutamate receptors participate in the cannabinoid-induced antinociception.
Berrino, L; de Novellis, V; Maione, S; Marabese, I; Oliva, P; Palazzo, E; Rossi, F, 2001
)
0.31
" Constant infusion of physostigmine at a dosage of 250 microg/kg/min produced an identical increase in radioligand binding."( Acetylcholinesterase inhibition increases in vivo N-(2-[18F]fluoroethyl)-4-piperidyl benzilate binding to muscarinic acetylcholine receptors.
Kilbourn, MR; Sherman, PS; Skaddan, MB; Snyder, SE, 2001
)
0.31
"SCH 66336 can be administered safely using a continuous oral bid dosing regimen."( Phase I and pharmacokinetic study of the oral farnesyl transferase inhibitor SCH 66336 given twice daily to patients with advanced solid tumors.
Awada, A; Cutler, DL; de Jonge, MJ; Eskens, FA; Faber, MN; Hanauske, AR; Luyten, GP; Piccart, M; Sparreboom, A; Statkevich, P; Verweij, J, 2001
)
0.31
" In order to maximize and prolong positive drug effects, it is important to start early and adjust dosage during the treatment."( Cholinesterase inhibitors stabilize Alzheimer's disease.
Giacobini, E, 2000
)
0.31
"This double-blind randomized placebo-controlled parallel group study assessed the efficacy and safety (with particular regard to body weight and hypoglycemia) of repaglinide when used in a flexible mealtime dosing regimen in a situation close to everyday clinical practice."( Flexible meal-related dosing with repaglinide facilitates glycemic control in therapy-naive type 2 diabetes.
Dedov, I; Frandsen, KB; Gomis, R; Moses, RG; Schlienger, JL, 2001
)
0.31
" Patients were free to choose a flexible meal pattern, adjusting the dosing schedule from two to four preprandial doses per day in accordance with a "one meal, one dose; no meal, no dose" principle."( Flexible meal-related dosing with repaglinide facilitates glycemic control in therapy-naive type 2 diabetes.
Dedov, I; Frandsen, KB; Gomis, R; Moses, RG; Schlienger, JL, 2001
)
0.31
"Mealtime dosing with repaglinide is effective in improving overall glycemic control in type 2 diabetic patients for which control is suboptimal using diet alone."( Flexible meal-related dosing with repaglinide facilitates glycemic control in therapy-naive type 2 diabetes.
Dedov, I; Frandsen, KB; Gomis, R; Moses, RG; Schlienger, JL, 2001
)
0.31
" Vascular segments were obtained in 34 patients who had undergone revascularization procedures, and isometric dose-response curves (DRCs) were constructed using the isolated tissue bath procedure as follows: 1) cumulative DRCs to norepinephrine; and 2) DRCs to acetylcholine (ACh) and sodium nitroprusside in the absence and presence of bosentan, BQ-123, or BQ-788."( Augmentation of endothelial function by endothelin antagonism in human saphenous vein conduits.
Anderson, TJ; Dumont, AS; Lovren, F; McNeill, JH; Sutherland, GR; Triggle, CR; Verma, S, 2001
)
0.31
" Although careful titration of repaglinide dose is recommended for patients with mild to moderate renal impairment, no dosage adjustment is otherwise needed in the elderly."( Repaglinide: prandial glucose regulation in clinical practice.
McDougall, A; Owens, DR, 2000
)
0.31
" Double-blind, active-comparator studies have shown repaglinide to have an antidiabetic efficacy that is at least equivalent to sulphonylureas, even when food intake and dosing intervals were controlled according to the requirements of sulphonylureas."( A review of clinical experience with the prandial glucose regulator, repaglinide, in the treatment of type 2 diabetes.
Moses, R, 2000
)
0.31
" In a placebo-controlled cross-over study, we investigated the effect of SR 48968C, administrated orally once-daily in a dosage of 100 mg during 9 days, on airway responsiveness to adenosine 5'-monophosphate (AMP) in 12 allergic asthmatic patients."( The NK-2 receptor antagonist SR 48968C does not improve adenosine hyperresponsiveness and airway obstruction in allergic asthma.
Kraan, J; Postma, DS; Vink-Klooster, H, 2001
)
0.31
" Additionally, AH11110A enhanced the general contractility of rat vas deferens, produced a bell-shaped dose-response curve of vasodilation in perfused rat kidney, and its antagonism in most other tissues was not simply competitive."( Failure of AH11110A to functionally discriminate between alpha(1)-adrenoceptor subtypes A, B and D or between alpha(1)- and alpha(2)-adrenoceptors.
Eltze, M; Grebe, T; König, H; Ullrich, B, 2001
)
0.31
" This study was designed to evaluate the dose-response effect of lanepitant in patients with daily moderate to severe, bilateral, distal neuropathic pain."( Dose-response study of the analgesic effect of lanepitant in patients with painful diabetic neuropathy.
Gitter, BD; Goldstein, DJ; Iyengar, S; Wang, O,
)
0.13
" h/mL, the severity of adverse bleeding events increased considerably; this suggested that dosing recommendations should be generated to minimize the likelihood of patients having an area under the plasma concentration-time curve from 0 to 24 hours in excess of this value."( A population pharmacokinetic-pharmacodynamic and logistic regression analysis of lotrafiban in patients.
Aluri, J; Chapelsky, M; Granett, J; Mould, D; Samuels, R; Swagzdis, J, 2001
)
0.31
" Plasma insulin-like growth factor-I (IGF-I) was elevated progressively over a 5-d course of daily oral dosing in dogs."( Preclinical pharmacology of CP-424,391, an orally active pyrazolinone-piperidine [correction of pyrazolidinone-piperidine] growth hormone secretagogue.
Carpino, PA; Chidsey-Frink, K; DaSilva-Jardine, PA; Lefker, BA; Lu, B; MacLean, DB; Mullins, MA; Nettleton, DO; Ng, O; Nickerson, DF; Pan, LC; Pettersen, JC; Pirie, CM; Ragan, JA; Tess, DA; Thompson, DD; Toler, SM, 2001
)
0.31
"0 mg/kg) produced a rightward shift in the (+)-7-OH-DPAT dose-response curve."( Antagonism of the discriminative stimulus effects of (+)-7-OH-DPAT by remoxipride but not PNU-99194A.
Baker, LE; Christian, AJ; Goodwin, AK, 2001
)
0.31
" Notably, the interaction isobole of the (clinically readily available) infusion rates provides a useful dosing recommendation for the coadministration of propofol and remifentanil during maintenance of anesthesia."( Propofol and remifentanil pharmacodynamic interaction during orthopedic surgical procedures as measured by effects on bispectral index.
Bouillon, T; Cuhls, M; Hoeft, A; Könen-Bergmann, M; Röpcke, H, 2001
)
0.31
"The goals of this study were to determine the CDB-4022 dose-response relationship for induction of acute decreases in testicular weight and germ cell depopulation in rats; establish the threshold dose of CDB-4022 required to induce infertility; and investigate whether CDB-4022-induced testicular damage could be prevented by a GnRH agonist (Lupron Depot)."( Lupron depot prevention of antispermatogenic/antifertility activity of the indenopyridine, CDB-4022, in the rat.
Blye, RP; Hild, SA; Meistrich, ML; Reel, JR, 2001
)
0.31
"The pharmacodynamics and dose-response relationship of repaglinide, a novel oral hypoglycemic agent, were evaluated in steady-state treatment of patients with type 2 diabetes."( Pharmacokinetics, pharmacodynamics, and dose-response relationship of repaglinide in type 2 diabetes.
Goldberg, RB; Graf, RJ; Huang, WC; Marbury, TC; Polvino, W; Schwartz, SL; Strange, P; Weston, I, 1999
)
0.3
"5 mg, 1 mg, 2 mg, and 4 mg) was compared to that of placebo in a double-blind, randomized, parallel-group, 4-week dose-response clinical trial in 143 patients."( Pharmacokinetics, pharmacodynamics, and dose-response relationship of repaglinide in type 2 diabetes.
Goldberg, RB; Graf, RJ; Huang, WC; Marbury, TC; Polvino, W; Schwartz, SL; Strange, P; Weston, I, 1999
)
0.3
" A well-defined dose-response relationship was observed for BGmean and FSG values."( Pharmacokinetics, pharmacodynamics, and dose-response relationship of repaglinide in type 2 diabetes.
Goldberg, RB; Graf, RJ; Huang, WC; Marbury, TC; Polvino, W; Schwartz, SL; Strange, P; Weston, I, 1999
)
0.3
" If necessary, the dosis should be progressively increased, depending on the individual response, up to 4 mg before meal (maximal daily dosage of 16 mg), in order to optimize blood glucose control."( [Pharma-clinics. Medication of the month. Repaglinide (NovoNorm)].
Scheen, AJ, 2001
)
0.31
"3 and 1 mg/kg) produced rightward shifts in the Delta9-THC dose-response curve for Delta9-THC-appropriate responding and for (R)-methanandamide-appropriate responding (surmountable antagonism)."( (R)-methanandamide and Delta 9-THC as discriminative stimuli in rats: tests with the cannabinoid antagonist SR-141716 and the endogenous ligand anandamide.
Järbe, TU; Lamb, RJ; Lin, S; Makriyannis, A, 2001
)
0.31
"Pharmacokinetics of roxatidine acetate is affected by hepatic function, and the dosage of roxatidine acetate for patients with liver disease, especially cirrhosis, should be modified."( Pharmacokinetics of roxatidine acetate in patients with chronic liver disease.
Takase, S; Tsutsumi, M; Ueshima, Y, 2001
)
0.31
" Recovery profile was assessed by recording time spent in the postanesthesia care unit and step-down recovery unit, number and timing of adverse events, timing and dosage of rescue medications, and time to eligibility for discharge (to home or to hospital room)."( Hemodynamics and emergence profile of remifentanil versus fentanyl prospectively compared in a large population of surgical patients.
Fleisher, LA; Hogue, S; Jamerson, B; Twersky, RS; Warner, DS, 2001
)
0.31
" The desensitization was dose-dependent, and it shifted the oxytocin and ACTH dose-response curves of 8-OH-DPAT to the right (increased ED(50)) with no change in their maximal responses (E(max))."( Characterization of the functional heterologous desensitization of hypothalamic 5-HT(1A) receptors after 5-HT(2A) receptor activation.
Battaglia, G; D'Souza, D; Garcia, F; Muma, NA; Raap, DK; Van de Kar, LD; Zhang, Y, 2001
)
0.31
") caused dose-dependent rightward shift in the pressor dose-response curve induced by B-HT 920."( alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator.
Hashimoto, A; Imaizumi, T; Kambe, T; Kishi, M; Mori, T; Nakazawa, T; Orito, K, 2001
)
0.31
" Dosage was titrated against clinical response to perioperative stimulation and the infusion was terminated at the end of the operation."( Effect of age on recovery from remifentanil anaesthesia.
Hung, CT; Lai, A, 2001
)
0.31
" However, considering the selected dosing regimen, recovery times were significantly shorter for children after TIVA."( [Propofol-remifentanil versus sevoflurane-remifentanil for anesthesia for pediatric procedures in infants, children and adolescents].
Albrecht, S; Carbon, R; Fechner, J; Fritsch, B; Rösch, W; Schmidt, J; Schmitz, B, 2001
)
0.31
" The ET-1 dose-response was biphasic in normal muscles."( Myocardial contractile responsiveness to endothelin-1 in the post-infarction rat model of heart failure: effects of chronic quinapril.
Cernacek, P; Nguyen, QT; Picard, P; Qi, XL; Rouleau, JL; Sia, YT; Sirois, M; Stewart, DJ; Wei, G, 2001
)
0.31
"5 mg/kg), dipentylphthalate (DPP; 2200 mg/kg; a Sertoli cell toxicant), or vehicle and were necropsied 3, 6, or 12 h after dosing to determine acute effects."( Disruption of spermatogenesis and Sertoli cell structure and function by the indenopyridine CDB-4022 in rats.
Blye, RP; Hild, SA; Larner, JM; Reel, JR, 2001
)
0.31
" Dose-response analysis showed that both flavopiridol and roscovitine reversibly suppressed HIV-1 transcription in podocytes in vitro at an IC(50) of 25 nM and 3 microM, respectively."( Suppression of HIV-1 expression by inhibitors of cyclin-dependent kinases promotes differentiation of infected podocytes.
Gelman, IH; Klotman, PE; Nelson, PJ, 2001
)
0.31
" However, plasma concentrations increased from the first minute after intranasal dosing suggesting that sumatriptan and naratriptan are absorbed into the general systemic circulation from the nasal cavity in rats in a first-order fashion with no lag time."( Intranasal absorption of sumatriptan and naratriptan: no evidence of local transfer from the nasal cavities to the brain arterial blood in male rats.
Deprez, S; Einer-Jensen, N; Larsen, L; Schwartz, S; Starns, E, 2001
)
0.31
" dosing and 15-16% and 16% of the administered dose within 24 and 48 h, respectively, after oral dosing."( Pharmacokinetics and tissue distribution of halofuginone (NSC 713205) in CD2F1 mice and Fischer 344 rats.
Covey, JM; Egorin, MJ; Eiseman, JL; Hamburger, DR; Parise, RA; Stecklair, KP, 2001
)
0.31
" If mean arterial pressure (MAP) increased >80 mm Hg during maximal dosage of isoflurane or remifentanil, labetalol was administered."( Remifentanil provides hemodynamic stability and faster awakening time in transsphenoidal surgery.
Cozzi, S; Gemma, M; Losa, M; Mortini, P; Narcisi, S; Soldarini, A; Tommasino, C, 2002
)
0.31
" When multiple dosages of a drug were tested, the results of the highest approved dosage were used."( Oral antihyperglycemic therapy for type 2 diabetes: scientific review.
Inzucchi, SE, 2002
)
0.31
"), showed an anxiogenic-like effect that reached a maximum with the dosage of 5 mg/kg."( Mouse light/dark box test reveals anxiogenic-like effects by activation of histamine H1 receptors.
Bartolini, A; Ipponi, A; Malmberg-Aiello, P; Schunack, W,
)
0.13
" The purpose of this pharmacodynamic study was to validate a prandial regimen of repaglinide by comparing meal-related dosing with a regimen in which the same total daily dose was divided into only two doses at morning and evening meals."( Optimizing insulin secretagogue therapy in patients with type 2 diabetes: a randomized double-blind study with repaglinide.
Andersen, PH; Jønler, M; Lund, S; Pørksen, N; Schmitz, O, 2002
)
0.31
"These data support the strategy of mealtime dosing with repaglinide."( Optimizing insulin secretagogue therapy in patients with type 2 diabetes: a randomized double-blind study with repaglinide.
Andersen, PH; Jønler, M; Lund, S; Pørksen, N; Schmitz, O, 2002
)
0.31
" Overall, ERA-923 was safe and well tolerated in postmenopausal women dosed for 28 days."( Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women.
Burghart, PH; Cotreau, MM; Dykstra, KH; Gandhi, T; Gutierrez, M; Park, Y; Schwertschlag, US; Stonis, L; Xu, J, 2002
)
0.31
" The U-shaped dose-response relationship and the time dependency of the effect of thioperamide indicated that the drug acts on mechanisms involved in memory consolidation."( Histamine H3-receptor blockade in the rat nucleus basalis magnocellularis improves place recognition memory.
Ferretti, C; Gamalero, R; Ghi, P; Orsetti, M, 2002
)
0.31
" Dosing of mice with LY303870, a neurokinin-1 receptor antagonist, reduced the severity of IBD, and treatment of mice with preexisting IBD allowed partial healing of lesions."( Treatment with neurokinin-1 receptor antagonist reduces severity of inflammatory bowel disease induced by Cryptosporidium parvum.
Akili, D; Harp, JA; Palmer, MV; Sonea, IM, 2002
)
0.31
"The objective of this study was to determine a dosing regimen for remifentanil-sevoflurane anaesthesia that achieves an optimal balance between quality of anaesthesia and time to recovery."( Remifentanil-sevoflurane anaesthesia for laparoscopic cholecystectomy: comparison of three dose regimens.
Bencini, AF; Ephraim, EP; Frietman, RC; Houweling, PL; Mulder, PG; van Delden, PG; van Niekerk, J; van Stolk, MA; Verheijen, R; Wajer, OJ, 2002
)
0.31
" Female rhesus macaques were ovariectomized and orally dosed with vehicle, estradiol 17beta, raloxifene or arzoxifene once per day by sipper bottles for 30 days."( Effects of oral estrogen, raloxifene and arzoxifene on gene expression in serotonin neurons of macaques.
Bethea, CL; Michelson, D; Mirkes, SJ; Su, A, 2002
)
0.31
"The short onset and offset of remifentanil may allow for accurate dosing of sedative effect with few side-effects and rapid recovery."( Remifentanil sedation compared with propofol during regional anaesthesia.
Aitkenhead, A; Hanson, AL; Lauwers, MH; Martisson, S; Marty, J; Merle, JC; Raeder, JC; Reite, K; Servin, FS; Wattwil, M; Wostyn, L, 2002
)
0.31
"The optimization of oral dosage form formulation has been developed for N-4472, N-[2-(3,5-di-tert-butyl-4-hydroxyphenethyl)-4,6-difluorophenyl]-N'-[4-(N-benzylpiperidyl)] urea, which was a poorly water-soluble drug having a lipid-lowering effect."( Improvement of physicochemical properties of N-4472 part I formulation design by using self-microemulsifying system.
Itoh, K; Oguchi, T; Tozuka, Y; Yamamoto, K, 2002
)
0.31
" The first series of experiments was designed to determine if Delta(9)-THC-mediated changes in cerebral metabolism followed a clear dose-response relationship."( Dose-dependent effects of Delta9-tetrahydrocannabinol on rates of local cerebral glucose utilization in rat.
Freedland, CS; Miller, MD; Porrino, LJ; Whitlow, CT, 2002
)
0.31
"Cholinesterase inhibitors (ChEIs) are dosed in two phases for the treatment of dementia, an initial dose-escalation phase to achieve a therapeutic dose and a maintenance phase where the therapeutic dose is given for long-term therapy."( The tolerability and safety of cholinesterase inhibitors in the treatment of dementia.
Inglis, F, 2002
)
0.31
" Beneficial effects in other similar patients or at higher dosage cannot be excluded."( An N-of-1 randomized controlled trial ('N-of-1 trial') of donepezil in the treatment of non-progressive amnestic syndrome.
Grimley Evans, J; Price, JD, 2002
)
0.31
" Further investigation into flavopiridol as a clinical agent should focus on alternative dosing schedules and the compound's potential use in combination chemotherapeutic regimens."( Seventy-two hour continuous infusion flavopiridol in relapsed and refractory mantle cell lymphoma.
Howard, OM; Kim, HH; Lin, TS; Neuberg, DS; Shipp, MA, 2002
)
0.31
" After Ramadan, patients resumed their regular meal pattern and treatment dosage for 4 weeks."( Repaglinide versus glibenclamide treatment of Type 2 diabetes during Ramadan fasting.
Mafauzy, M, 2002
)
0.31
" Improvement in behavioural symptoms also occurs, but without a dose-response relationship."( Clinical pharmacokinetics and pharmacodynamics of cholinesterase inhibitors.
Jann, MW; Shirley, KL; Small, GW, 2002
)
0.31
" Both medications were administered open label according to recommended dosing regimens from the respective product labelling available during the conduct of the study."( A multinational, randomised, 12-week, comparative study of donepezil and rivastigmine in patients with mild to moderate Alzheimer's disease.
Bahra, RS; Bullock, R; Engelbrecht, I; Hock, C; Hopker, SW; Ieni, JR; Maud, CM; Passmore, AP; Potocnik, FC; Smith, R; Wilkinson, DG,
)
0.13
" There were, however, no adverse cardiovascular or CNS side-effects seen at this dosing level."( Pharmacological characterization of Ro 63-1908 (1-[2-(4-hydroxy-phenoxy)-ethyl]-4-(4-methyl-benzyl)-piperidin-4-ol), a novel subtype-selective N-methyl-D-aspartate antagonist.
Alanine, A; Bourson, A; Buttelmann, B; Fischer, G; Gill, R; Heitz, MP; Kemp, JA; Kew, JN; Levet-Trafit, B; Lorez, HP; Malherbe, P; Miss, MT; Mutel, V; Pinard, E; Roever, S; Schmitt, M; Trube, G; Wybrecht, R; Wyler, R, 2002
)
0.31
" Both compounds maintained responding with sigmoidal or biphasic dose-response functions (0."( Reinforcing strength of a novel dopamine transporter ligand: pharmacodynamic and pharmacokinetic mechanisms.
Kozikowski, A; Ordway, GA; Paul, IA; Petukhov, P; Ranaldi, R; Wang, Z; Woolverton, WL, 2002
)
0.31
" When used in a flexible dosing regime in a large cohort of patients, it is associated with better glycaemic control, a reduction in HbA1c, weight loss and improved quality of life compared to sulphonylureas."( Insulin secretagogues.
Davies, MJ, 2002
)
0.31
"In direct head-to-head comparative clinical trials, oral rizatriptan 10 mg enabled more migraine sufferers to function normally at 2 h after dosing than oral sumatriptan, naratriptan, and zolmitriptan."( Restoring migraine sufferers' ability to function normally: a comparison of rizatriptan and other triptans in randomized trials.
Bussone, G; D'Amico, D; Gerth, W; Lines, CR; McCarroll, KA, 2002
)
0.31
" Repeat oral dosing of 4 in dogs for 29 days (6 mg/kg) resulted in a significant down-regulation of the post dose GH response and a 60 and 40% increase in IGF-1 levels relative to pre-dose levels at the 8- and 24-h post dose time points."( Discovery and biological characterization of capromorelin analogues with extended half-lives.
Carpino, PA; Chidsey-Frink, KL; Cook, ER; DaSilva-Jardine, PA; DeNinno, SL; DiBrino, JN; Hada, WA; Hadcock, JR; Inthavongsay, J; Lefker, BA; Lewis, SK; Mangano, FM; Mullins, MA; Murray, MC; Ng, O; Nickerson, DF; Pan, LC; Pettersen, JC; Pirie, CM; Ragan, JA; Rose, CR; Tess, DA; Thompson, DD; Toler, SM; Wilson, TC; Wright, AS; Yu, L; Zawistoski, MP, 2002
)
0.31
"As a result of the higher incidence of adverse respiratory effects with remifentanil and similar sedative effects, propofol is preferable for sedation during cervical plexus block in elderly patients with comorbid disease at the dosage used."( Remifentanil or propofol for sedation during carotid endarterectomy under cervical plexus block.
Deusch, E; Fitzgerald, RD; Jellinek, H; Krenn, H; Oczenski, W, 2002
)
0.31
" It seems that remifentanil dosage does not need to be changed in patients with butyrylcholinesterase deficiency."( In vitro remifentanil metabolism: the effects of whole blood constituents and plasma butyrylcholinesterase.
Davis, PJ; Egan, TD; McGowan, FX; Muir, KT; Stiller, RL; Wilson, AS, 2002
)
0.31
" More importantly, even millimolar concentrations of CX516 did not influence the dose-response relation for CX546, suggesting the possibility that they bind to different sites."( Benzamide-type AMPA receptor modulators form two subfamilies with distinct modes of action.
Arai, AC; Kessler, M; Lynch, G; Rogers, G; Xia, YF, 2002
)
0.31
" SCH 66336 can be safely administered using a continuous oral OD dosing regimen."( Phase I and pharmacological study of the oral farnesyltransferase inhibitor SCH 66336 given once daily to patients with advanced solid tumours.
Awada, A; Bleiberg, H; Cutler, DL; Eskens, FA; Faber, MN; Fumoleau, P; Piccart, M; Statkevich, P; van der Gaast, A; Verweij, J; Wanders, J, 2002
)
0.31
" A pre-defined dosing algorithm permitted initial titration of the opioids to predetermine the optimal level of sedation and pain score."( Remifentanil vs morphine for patients in intensive care unit who need short-term mechanical ventilation.
Chinachoti, T; Kessler, P; Kirkham, A; Werawatganon, T, 2002
)
0.31
" The dose-response relationship indicated that percent drug lever responding was dose-dependent."( Discriminative stimulus properties of 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane [(+/-)DOI] in C57BL/6J mice.
Barrett, RJ; Sanders-Bush, E; Smith, RL, 2003
)
0.32
" Concurrent dosing of dihydrocodeine and ebastine produced a significant place preference."( Effects of second generation of histamine H1 antagonists, cetirizine and ebastine, on the antitussive and rewarding effects of dihydrocodeine in mice.
Kamei, J; Miyata, S; Morita, K; Onodera, K, 2003
)
0.32
"The anesthetic management of a 58 year-old-male suffering from idiopathic pulmonary fibrosis associated with a previous experience of altered dose-response relationship to muscle relaxants is reported."( [Tracheal intubation in a case of idiopathic pulmonary fibrosis using remifentanil and propofol without muscle relaxants].
Burrelli, R; Cafiero, T; Gargiulo, G; Mastronardi, P, 2002
)
0.31
"We determined the effect of a cannabinoid CB1 receptor antagonist (AM-251; N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide) on food intake, body weight and adipose tissue mass in Western diet-induced obese (DIO) mice using a chronic, interrupted, oral dosing paradigm."( Antiobesity effects of chronic cannabinoid CB1 receptor antagonist treatment in diet-induced obese mice.
Black, SC; Hildebrandt, AL; Kelly-Sullivan, DM, 2003
)
0.32
" The results indicate that no clinically meaningful drug interactions occurred between risperidone 1 mg daily and donepezil 5 mg daily at steady state, and therefore no dosage adjustment is required when both drugs are combined with the dosage regimen studied."( Pharmacokinetic and safety assessments of concurrent administration of risperidone and donepezil.
Jia, X; Parier, JL; Pesco-Koplowitz, L; Xie, C; Zhao, Q, 2003
)
0.32
" The present study indicates that clinically relevant concentrations of the tested thrombin inhibitors interfere with endothelial-mediated APC generation, which may offer an explanation for the lack of a dose-response effect in clinical trials with thrombin inhibitors."( Inhibition of endothelial cell-mediated generation of activated protein C by direct and antithrombin-dependent thrombin inhibitors.
Frebelius, S; Jansson, K; Linder, R; Swedenborg, J, 2003
)
0.32
"Lean and obese Zucker rats were orally dosed with SR 141716 (3, 10, 30 mg/kg PO), sibutramine (5 mg/kg PO) or vehicle for one week."( Preferential effects of the cannabinoid CB1 receptor antagonist, SR 141716, on food intake and body weight gain of obese (fa/fa) compared to lean Zucker rats.
Dourish, CT; Kennett, GA; Vickers, SP; Webster, LJ; Wyatt, A, 2003
)
0.32
"To identify the remifentanil dosing regimen providing safe and optimal anesthetic conditions during coronary artery bypass graft surgery and to evaluate postoperative recovery characteristics."( Comparison of three remifentanil dose-finding regimens for coronary artery surgery.
Howie, MB; Hug, CC; Jopling, MW; Michelsen, LG; Porembka, DT; Shaikh, S; Warren, SM, 2003
)
0.32
"Within subjects, latencies were most consistent from infusion to infusion at unit doses on the descending limb of the dose-response curve."( Variability of drug self-administration in rats.
Katz, JL; Panlilio, LV; Pickens, RW; Schindler, CW, 2003
)
0.32
"1-1 microM), which correlates with the cerebrospinal fluid concentration of the drug at the recommended daily dosage of 16 to 24 mg."( Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.
Albuquerque, EX; Christner, C; Fehrenbacher, A; Höffle, A; Jostock, R; Lübbert, H; Ludwig, J; Maelicke, A; Pereira, EF; Radina, M; Samochocki, M; Ullmer, C; Zerlin, M, 2003
)
0.32
" If the combination is considered necessary, repaglinide dosage should be greatly reduced and blood glucose concentrations carefully monitored."( Effects of gemfibrozil, itraconazole, and their combination on the pharmacokinetics and pharmacodynamics of repaglinide: potentially hazardous interaction between gemfibrozil and repaglinide.
Backman, JT; Neuvonen, M; Neuvonen, PJ; Niemi, M, 2003
)
0.32
" The prandial glucose regulator repaglinide has been studied in combination with metformin (an inhibitor of hepatic glucose production), neutral protamine Hagedorn (NPH)-insulin (which has a long duration of effect, but at the risk of early hypoglycaemia and late hyperglycaemia in the dosing interval) and three thiazolidinediones (TZDs--troglitazone, rosiglitazone and pioglitazone, which stimulate nuclear receptors to increase insulin sensitivity and reduce insulin resistance) in patients whose diabetes was inadequately controlled by previous monotherapy or combination therapy."( Repaglinide in combination therapy.
Moses, R, 2002
)
0.31
" Dose-response studies indicated that c-Fos protein expression was induced at doses (0."( The novel analgesic and high-efficacy 5-HT1A receptor agonist, F 13640 induces c-Fos protein expression in spinal cord dorsal horn neurons.
Besson, JM; Buritova, J; Colpaert, F; Tarayre, JP, 2003
)
0.32
" It is currently debated if the steep ascending part of the biphasic dose-response curve typically obtained in multiple-dosing lever-press-based operant conditioning procedures represents a satiety-driven, all-or-none response or if the response is gradual and tightly adjusted to the various doses of the reinforcer."( Opioids, cocaine, and food change runtime distribution in a rat runway procedure.
Saria, A; Sturm, K; Wakonigg, G; Zernig, G, 2003
)
0.32
" In conclusion, this study shows that, at the end of the conventional dosing interval, ebastine 10 mg and cetirizine 10 mg once daily in repeated doses suppressed the histamine wheal more effectively than did loratadine 10 mg once daily or fexofenadine 60 mg twice daily."( Inhibition of the histamine wheal by ebastine compared with cetirizine, fexofenadine and loratadine at steady state.
Boyce, M; Carey, W; Luria, X; Warrington, S, 2002
)
0.31
"Knowledge of the pharmacodynamic interaction between remifentanil and propofol is important to permit optimal dosage strategies."( Modelling the pharmacodynamic interaction between remifentanil and propofol by EEG-controlled dosing.
Albrecht, S; Fechner, J; Hering, W; Ihmsen, H; Palmaers, T; Schüttler, J, 2003
)
0.32
" Both drugs were dosed and titrated based on computer-assisted pharmacokinetic models to maintain constant plasma concentrations."( Pharmacokinetic-based total intravenous anaesthesia using remifentanil and propofol for surgical myocardial revascularization.
De Cosmo, D; De Stefani, R; Guarracino, F; Penzo, D; Vardanega, A, 2003
)
0.32
" A mixed-effects population study was carried out in order to analyze the sparse data and to create covariate models which could be used to derive dosage recommendations."( Age-related changes in pharmacokinetics and pharmacodynamics of lerisetron in the rat: a population pharmacokinetic model.
Calvo, R; de la Fuente, L; Jauregizar, N; Quintana, A; Raczka, E; Suarez, E,
)
0.13
" In conclusion, flexible mealtime dosing with oral medication appears to be well accepted by pharmacotherapy-naïve patients with Type 2 diabetes."( The effect of prandial glucose regulation with repaglinide on treatment satisfaction, wellbeing and health status in patients with pharmacotherapy naïve Type 2 diabetes: a placebo-controlled, multicentre study.
Bech, P; Gomis, R; Moses, R, 2003
)
0.32
" Profiles of blood glucose concentration following repaglinide dosing were altered by less than 8% by both ketoconazole and rifampicin."( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide.
Hansen, KT; Hatorp, V; Thomsen, MS, 2003
)
0.32
" A cumulative dose-response relationship was observed between longer-term sustained donepezil use and delay of NHP."( Donepezil is associated with delayed nursing home placement in patients with Alzheimer's disease.
Geldmacher, DS; Ieni, JR; Mastey, V; McRae, T; Provenzano, G, 2003
)
0.32
" This includes the anaesthesia induction sequence, the choice and dosage of anaesthetics when used as adjuncts to remifentanil, and even more, the proper planning of postoperative pain management."( [Remifentanil. An update].
Kreuer, S; Larsen, R; Wilhelm, W; Wrobel, M, 2003
)
0.32
" In this study, our aim was to determine an appropriate dosage regimen of remifentanil for awake nasotracheal fiberoptic intubation."( Awake nasotracheal fiberoptic intubation: patient comfort, intubating conditions, and hemodynamic stability during conscious sedation with remifentanil.
Andel, D; Gonano, C; Holzer, A; Illievich, UM; Machata, AM; Spiss, CK; Zimpfer, M, 2003
)
0.32
" We show that at therapeutic dosage (or at micromolar range), flavopiridol almost completely prevents colchicine-induced apoptosis in cerebellar granule neurones."( Neuroprotective action of flavopiridol, a cyclin-dependent kinase inhibitor, in colchicine-induced apoptosis.
Bravo, R; Bruna, A; Caelles, C; Camarasa, J; Camins, A; Canudas, AM; Escubedo, E; Jiménez, A; Jorda, EG; Pallàs, M; Pubill, D; Verdaguer, E, 2003
)
0.32
" In two experiments using Aedes aegypti, one using a single identical dose and one with varying doses used to develop a dose-response curve, SS220 was as effective as Deet and both compounds were more effective than Bayrepel."( Synthesis and repellent efficacy of a new chiral piperidine analog: comparison with Deet and Bayrepel activity in human-volunteer laboratory assays against Aedes aegypti and Anopheles stephensi.
Debboun, M; Khrimian, A; Klun, JA; Kramer, M; Margaryan, A, 2003
)
0.32
"Increased dosage was necessary only for 10 min during the procedure."( Efficacy and safety of continuous intravenous infusion of remifentanil in preterm infants undergoing laser therapy in retinopathy of prematurity: clinical experience.
Bocci, MG; Conti, G; Ferro, G; Lepore, D; Mercurio, G; Molle, F; Papacci, P; Sammartino, M, 2003
)
0.32
" This comparison suggests that 25 mg of picenadol is a more acceptable dosage since both 25 and 50 mg were effective dosages."( Intramuscular picenadol in patients with postoperative pain.
Brunelle, RL; George, RE; Goldstein, DJ; Zimmerman, DM, 1993
)
0.29
" Some differences in side-effects at equi-analgesic dosage were observed, particularly a reduction in histamine release."( Pharmacological actions of two new pethidine analogues.
LISTER, RE, 1960
)
0.24
"2% in oxygen and nitrous oxide and the opioid dosing was titrated to autonomic responses."( Remifentanil infusion for cleft palate surgery in young infants.
Dagher, C; Desjeux, L; Gall, O; Murat, I; Roulleau, P, 2003
)
0.32
" A small but significant effect on uterine wet weight was noted with raloxifene dosed at 1 mg/kg."( Effects of SP500263, a novel selective estrogen receptor modulator, on bone, uterus, and serum cholesterol in the ovariectomized rat.
Anderson, DW; Bhagwat, SS; Brady, H; Gayo-Fung, LM; Leisten, J; Lipps, SG; McKie, JA; O'Leary, E; Patnaik, N; Stein, B; Sutherland, MK, 2003
)
0.32
" Dose-response curves for buprenorphine-induced antinociception display ceiling effects or are bell shaped, which have been attributed to the partial agonist activity of buprenorphine at opioid receptors."( Buprenorphine-induced antinociception is mediated by mu-opioid receptors and compromised by concomitant activation of opioid receptor-like receptors.
Bryant, CD; Carroll, FI; Eitan, S; Evans, CJ; Kieffer, BL; Lutfy, K; Maidment, NT; Saliminejad, N; Takeshima, H; Walwyn, W; Yang, YC, 2003
)
0.32
" Moreover, the CB1 antagonists right-shifted A1 agonist dose-response curves without affecting maximal responses, suggesting competitive mode of antagonist action."( An optimized approach to study endocannabinoid signaling: evidence against constitutive activity of rat brain adenosine A1 and cannabinoid CB1 receptors.
Järvinen, T; Laitinen, JT; Niemi, R; Saario, SM; Savinainen, JR, 2003
)
0.32
"The dose-response curve for the effect of volatile anesthetics on the somatosensory evoked potential (SEP) is well described, but for propofol, the large dose segment of the curve is undefined."( Propofol suppresses the cortical somatosensory evoked potential in rats.
Cronin, AJ; DiVittore, NA; Kreiser, S; Li, BH; Li, DP; Logginidou, HG; Lohmann, JS; Schuler, HG, 2003
)
0.32
"3 nM for this subtype (compared to NR1(A)/2A: 35 microM and NR1(A)/2C>100 microM) and was active in rat at a relatively low dosage (10mg/kg po)."( Synthesis, radiosynthesis and in vivo evaluation of 5-[3-(4-benzylpiperidin-1-yl)prop-1-ynyl]-1,3-dihydrobenzoimidazol-2-[(11)C]one, as a potent NR(1A)/2B subtype selective NMDA PET radiotracer.
Besret, L; Bottlaender, M; Bramoullé, Y; Coulon, C; Dollé, F; Kassiou, M; Lagnel, B; Ottaviani, M; Roger, G; Valette, H, 2003
)
0.32
" It is important to prevent dosing errors in cooperation with medical providers, patients and families."( [A case of acute cholinergic adverse effects induced by donepezil overdose: a follow-up of clinical course and plasma concentration of donepezil].
Fukuhara, Y; Kowa, H; Nakashima, K; Wada, K; Yano, H, 2003
)
0.32
" For this purpose, 129/SVE and C57BL/6 male mice were acutely dosed intraperitoneally (i."( Antidepressant-like and anorectic effects of the cannabinoid CB1 receptor inverse agonist AM251 in mice.
Fleischer, R; Rocha, BA; Rosko, KM; Shearman, LP; Tong, XS; Wang, J; Xu, S, 2003
)
0.32
" Coadministration of lonafarnib could thus reduce chemotherapy dosage and hence produce lower exposure to normal cells and less undesired toxicity."( The farnesyl protein transferase inhibitor lonafarnib (SCH66336) is an inhibitor of multidrug resistance proteins 1 and 2.
Johnson, WW; Wang, EJ, 2003
)
0.32
"A simple, precise and rapid RP-HPLC method was developed for the determination of repaglinide in pharmaceutical dosage forms."( Determination of repaglinide in pharmaceutical formulations by HPLC with UV detection.
Gandhimathi, M; Ravi, TK; Renu, SK, 2003
)
0.32
"In this 12-week, open-label, multicentre trial, patients with probable mild-to-moderate Alzheimer's disease received donepezil 5 mg/day for 28 days, after which the dosage was increased to 10 mg/day according to the investigating clinician's judgement."( Efficacy and safety of donepezil in patients with Alzheimer's disease: results of a global, multinational, clinical experience study.
Bahra, R; Baloyannis, S; Boada-Rovira, M; Brodaty, H; Cras, P; Emre, M; Zhang, R, 2004
)
0.32
" Side effects were associated with dosage increases."( Randomized placebo-controlled trial of donepezil in cognitive impairment in Parkinson's disease.
Brandt, J; Grill, S; Leroi, I; Lyketsos, CG; Marsh, L; Reich, SG; Thompson, R, 2004
)
0.32
" However, variable tolerability in our sample underscores the need for careful monitoring when prescribing donepezil to patients with PD, especially with dosage increases."( Randomized placebo-controlled trial of donepezil in cognitive impairment in Parkinson's disease.
Brandt, J; Grill, S; Leroi, I; Lyketsos, CG; Marsh, L; Reich, SG; Thompson, R, 2004
)
0.32
" Increased remifentanil dosage was associated with reduced plasma cortisol during surgery (P<0."( Effect of remifentanil infusion rate on stress response to the pre-bypass phase of paediatric cardiac surgery.
Cooper, R; Nolan, J; Rogers, CA; Weale, NK; Wolf, AR, 2004
)
0.32
" Pioglitazone dosage was fixed at 30 mg per day."( Treatment of type 2 diabetes with a combination regimen of repaglinide plus pioglitazone.
Gooch, B; Greco, S; Hale, PM; Hassman, DR; Jain, R; Jovanovic, L; Khutoryansky, N, 2004
)
0.32
" Nevertheless, the dosage used in severely impaired patients (10mg daily) was half that used in patients with mild to moderate impairment, and any comedication did not include drugs affecting liver function; in clinical practice, both these factors should be taken into account."( Pharmacokinetics and safety of ebastine in patients with impaired hepatic function compared with healthy volunteers: a phase I open-label study.
Dilzer, SC; Lasseter, KC; Noveck, RJ; Vargas, R; Waldman, S, 2004
)
0.32
" Dose-response curves for tremor (central effect) and salivation (peripheral effect) showed that donepezil and icopezil possess a more favourable therapeutic index than the nonselective inhibitors, tacrine and heptylphysostigmine."( Pharmacology of selective acetylcholinesterase inhibitors: implications for use in Alzheimer's disease.
Chapin, D; Hubbard, ST; Jones, SB; Liston, DR; Nason, D; Nielsen, JA; Ramirez, A; Shalaby, IA; Villalobos, A; White, WF, 2004
)
0.32
" However, combined oral dosing of nalmefene and subthreshold doses of AM251, a cannabinoid CB1 receptor inverse agonist, led to a significant reduction in food intake in both lean and diet-induced obese (DIO) mice."( Synergistic effects of cannabinoid inverse agonist AM251 and opioid antagonist nalmefene on food intake in mice.
Chen, RZ; Fong, TM; Huang, RR; MacNeil, DJ; Shen, CP, 2004
)
0.32
" In contrast, continuous treatment of mice bearing established GEO xenografts with ZD6474 resulted in efficient tumor growth inhibition for the entire duration of dosing (up to 150 days)."( Antitumor activity of ZD6474, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in human cancer cells with acquired resistance to antiepidermal growth factor receptor therapy.
Bianco, AR; Bianco, R; Caputo, R; Ciardiello, F; Damiano, V; De Placido, S; De Vita, F; Melisi, D; Tortora, G; Troiani, T, 2004
)
0.32
" Activities of daily living and social behaviour: On the Instrumental Activity of Daily Living (IADL) scale, there was no statistically significant difference between the groups taking donepezil 5mg per day donepezil and placebo, but the group taking 10 mg of donepezil a day showed benefit compared with placebo There were statistically significant benefit for donepezil at either dosage compared with placebo on the Alzheimer's Disease Functional Assessment and Change Scale (ADFACS)."( Donepezil for vascular cognitive impairment.
Birks, J; Malouf, R, 2004
)
0.32
" Fentanyl was similar, probably because the dosing algorithm demanded frequent monitoring and adjustment, thereby preventing over-sedation."( Remifentanil versus fentanyl for analgesia based sedation to provide patient comfort in the intensive care unit: a randomized, double-blind controlled trial [ISRCTN43755713].
Bonome, C; Cross, MH; Kirkham, AJ; López, A; Morrison, L; Muellejans, B, 2004
)
0.32
" According to a logistic regression model fitted to the experimental data, the dose-response relationship for the two repellents was the same within each species, thus pooled ED values were assessed for each mosquito separately."( Evaluation of the sensitivity of Aedes aegypti and Anopheles gambiae complex mosquitoes to two insect repellents: DEET and KBR 3023.
Badolo, A; Costantini, C; Ilboudo-Sanogo, E; Ouédraogo, AP, 2004
)
0.32
" Moreover, increasing doses of carbidopa significantly shifted the inhibitory dose-response effect of delta-9-THC in protecting shrews from 5-HTP-induced emesis to the left."( Central and peripheral mechanisms contribute to the antiemetic actions of delta-9-tetrahydrocannabinol against 5-hydroxytryptophan-induced emesis.
Darmani, NA; Johnson, JC, 2004
)
0.32
" Ang II was administered ip at a dosage of 640 ng/kg."( Angiotensin II-induced insulin resistance is enhanced in adrenomedullin-deficient mice.
Ando, K; Asano, T; Fujita, T; Itakura, K; Matsui, H; Ogihara, T; Qingyou, X; Shimosawa, T; Xing, G, 2004
)
0.32
" The Narcotrend monitor can make a significant contribution to the improvement of the quality of anaesthesia by adjusting the dosage of hypnotics to individual patient needs."( The Narcotrend Index: classification algorithm, correlation with propofol effect-site concentrations, and comparison with spectral parameters.
Beger, FA; Grouven, U; Schultz, A; Schultz, B, 2004
)
0.32
" Fentanyl and sufentanil require higher hypnotic dosage (halogenated agents, propofol) and remifentanil is accompanied by greater volumes of fluid infusion."( [Opioid anesthetics (sufentanil and remifentanil) in neuro-anaesthesia].
Garnier, F; Viviand, X, 2004
)
0.32
" We also show that it is not necessary to administer Arz and 268 continuously during tumor progression to prevent cancer in the rat model because dosing of these drugs in combination for relatively short periods, each followed by drug-free rests, is highly effective."( The selective estrogen receptor modulator arzoxifene and the rexinoid LG100268 cooperate to promote transforming growth factor beta-dependent apoptosis in breast cancer.
Berchuck, A; Heyman, RA; Krajewski, S; Lamph, WW; Liby, K; Reed, JC; Rendi, MH; Risingsong, R; Royce, DB; Sporn, MB; Suh, N; Williams, CR, 2004
)
0.32
"The pharmacokinetics of YM466, a selective inhibitor for factor Xa, was investigated after single intravenous and oral dosing to rats and dogs."( Pharmacokinetics of YM466, a new factor Xa inhibitor, in rats and dogs.
Kamimura, H; Mano, Y; Usui, T,
)
0.13
" Rupatadine is a new second generation H(1)-antihistamine with once-daily dosing that may provide better control of symptoms than the currently used H(1)-receptor blockers because of its dual pharmacological profile (anti-PAF and anti-H(1))."( Rupatadine 10 mg and ebastine 10 mg in seasonal allergic rhinitis: a comparison study.
Castillo, JA; De Molina, M; Guadaño, EM; Meseguer, J; Picado, C; Serra-Batlles, J; Valero, A, 2004
)
0.32
" Eighty-eight patients were randomly assigned to receive repaglinide and 87 patients to glyburide, with a titration period of 6 to 8 weeks for optimization of drug dosage and a subsequent 12-month treatment period."( Regression of carotid atherosclerosis by control of postprandial hyperglycemia in type 2 diabetes mellitus.
Esposito, K; Giugliano, D; Marfella, R; Nappo, F, 2004
)
0.32
"Oxidation presents a constant challenge for formulation scientists trying to develop stable dosage forms."( Antioxidant-accelerated oxidative degradation: a case study of transition metal ion catalyzed oxidation in formulation.
Carter, JC; Hong, J; Lee, E; Masse, JA; Oksanen, DA, 2004
)
0.32
" A prospective, randomized, placebo-controlled clinical trial with standard timing, dosage and treatment duration is recommended to further evaluate treatment efficacy."( The effects of Donepezil on traumatic brain injury acute rehabilitation outcomes.
Cornis-Pop, M; Gibellato, M; Jena, T; Lew, H; Seel, R; Silver, T; Walker, W, 2004
)
0.32
" In a dose-dependent manner, both the intraperitoneal and oral route of administration resulted in similar ex vivo binding curves and tele-methylhistamine dose-response curves despite the route of administration."( Central H3R activation by thioperamide does not affect energy balance.
Alexander-Chacko, J; Cramer, JW; Dill, MJ; Gadski, R; Pickard, RT; Shepperd, ML; Sindelar, DK; Smith, DP, 2004
)
0.32
"The authors estimated the effects of each of the three commonly used drugs for Alzheimer disease (donepezil, galantamine, and rivastigmine) in terms of predefined clinical outcomes and trial completion rates, by dosing level, and described differences among them."( Metaanalysis of randomized trials of the efficacy and safety of donepezil, galantamine, and rivastigmine for the treatment of Alzheimer disease.
Ames, D; Clayton, T; Lai, R; Ritchie, CW,
)
0.13
" This was prevented by ormeloxifene and the effect, though apparently more in females supplemented with higher dose of ormeloxifene, was not always significantly different and clear dose-response was not evident until BMD data was evaluated on T-/Z-score basis."( In vitro anti-resorptive activity and prevention of ovariectomy-induced osteoporosis in female Sprague-Dawley rats by ormeloxifene, a selective estrogen receptor modulator.
Arshad, M; Ghosh, R; Sawlani, V; Sengupta, S; Sharma, S; Singh, MM, 2004
)
0.32
" Beginning on day 22, the donepezil dosage was doubled for 22 days to the target dose of 10 mg once daily, with the last donepezil dose concomitantly administered with memantine 10 mg on day 43."( Lack of pharmacokinetic or pharmacodynamic interaction between memantine and donepezil.
Abramowitz, WT; Periclou, AP; Rao, N; Sherman, T; Ventura, D, 2004
)
0.32
" The variability associated with the dose-response analysis was attributable primarily to subject age, such that older monkeys required higher doses of donepezil."( Donepezil-induced improvement in delayed matching accuracy by young and old rhesus monkeys.
Buccafusco, JJ; Terry, AV, 2004
)
0.32
" Dosage requirements, blood pressure, heart rate, oxygen saturation (pulse oxymetry, SaO2) and the level of analgesia were recorded every 3 minutes."( [Remifentanil analgesia for aspiration of follicles for oocyte retrieval].
Arndt, M; Kreienmeyer, J; Nöldge-Schomburg, GF; Vagts, DA, 2004
)
0.32
" At concentrations that include their prescribed dosage ranges, donepezil (1-1000 nM) and galantamine (50-1000 nM) increase action potential-dependent dopamine release."( Cholinergic drugs for Alzheimer's disease enhance in vitro dopamine release.
Dani, JA; Zhang, L; Zhou, FM, 2004
)
0.32
" This was also supported by the finding that no metabolites were observed in bile and urine after oral dosing of (14)C-YM466."( Absorption, distribution, metabolism and excretion of YM466, a novel factor Xa inhibitor, in rats.
Kamimura, H; Mano, Y; Nakamura, E; Sonoda, T; Usui, T, 2004
)
0.32
" Three head-to-head trials of ChEIs in the treatment of AD have been published to date, but are limited due to their open-label design, rates of titration, and the drug dosage levels utilised."( The benefits and risks associated with cholinesterase inhibitor therapy in Alzheimer's disease.
Herrmann, N; Lanctôt, KL; Thompson, S, 2004
)
0.32
" The dose-response of BIS values and desflurane concentrations was not uniform: two patients showed increasing BIS values with increasing desflurane concentrations, while in three patients BIS values remained unchanged."( Comparison of BIS and AAI as measures of anaesthetic drug effect during desflurane-remifentanil anaesthesia.
Bauer, C; Bruhn, J; Kreuer, S; Larsen, R; Wilhelm, W, 2004
)
0.32
" In conclusion, the duration of action of cisatracurium was prolonged in morbidly obese patients when dosed according to RBW compared with a control group of normal weight patients."( The effects of cisatracurium on morbidly obese women.
Gullo, A; Leykin, Y; Lomangino, G; Lucca, M; Marzano, B; Pellis, T, 2004
)
0.32
" In contrast to nicotine replacement therapy and bupropion, SR141716 did not have nicotine-like discriminative effects and did not alter the dose-response curve for nicotine discrimination."( Rimonabant, a CB1 antagonist, blocks nicotine-conditioned place preferences.
Goldberg, SR; Le Foll, B, 2004
)
0.32
" Although insomnia and other sleep disorders have been reported following administration of donepezil, lengthening the time period before increasing the dose of donepezil from 5 to 10 mg day(-1) or switching to morning dosing can reduce these events to the levels of placebo-treated patients."( The safety and tolerability of donepezil in patients with Alzheimer's disease.
Ham, RJ; Jackson, S; Wilkinson, D, 2004
)
0.32
"These results indicate that the pharmacokinetics of donepezil are not altered after dosing to steady state, and that donepezil can be administered safely to subjects with moderate renal impairment."( Steady-state pharmacokinetics and safety of donepezil HCl in subjects with moderately impaired renal function.
Bolton, WK; Cullen, EI; Gutierrez, MJ; Hutman, HW; Kumar, D; Marbury, TC; Nagy, CF; Pratt, RD, 2004
)
0.32
" In consecutive dosing periods separated by washout periods of > or = 3 weeks, healthy volunteers received either oral donepezil HCI 5 mg once daily for 15 days, oral sertraline HCl 50 mg once daily for 5 days followed by 10 days of once-daily sertraline HCl 100 mg, or the simultaneous administration of oral donepezil HCl and sertraline HCl."( Concurrent administration of donepezil HCl and sertraline HCl in healthy volunteers: assessment of pharmacokinetic changes and safety following single and multiple oral doses.
Cullen, EI; Kumar, D; Nagy, CF; Perdomo, CA; Pratt, RD; Wason, S, 2004
)
0.32
"Repeated dosing with donepezil, 5 mg daily for 2 weeks, had no significant effect on the safety, tolerability or pharmacokinetics of thioridazine."( Repeated dosing with donepezil does not affect the safety, tolerability or pharmacokinetics of single-dose thioridazine in young volunteers.
Boyce, M; Dunn, K; Johnston, A; Ravic, M; Warrington, S, 2004
)
0.32
"Twenty-five patients with PD who were taking physician-optimized doses of levodopa/carbidopa (with daytime dosing intervals of 4-8 h) were administered once-daily doses of either donepezil HCl (5 mg) or placebo for 15 days, in two treatment periods, separated by a washout of at least 2 weeks."( Concurrent administration of donepezil HCl and levodopa/carbidopa in patients with Parkinson's disease: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Hahne, WA; Kirby, L; Kumar, D; Okereke, CS; Pratt, RD, 2004
)
0.32
"These results suggest that once-daily dosing of 5 mg donepezil HCl does not alter the PK of risperidone in patients with schizophrenia."( Concurrent administration of donepezil HCl and risperidone in patients with schizophrenia: assessment of pharmacokinetic changes and safety following multiple oral doses.
Cullen, EI; Khan, A; Kumar, D; Perdomo, CA; Pratt, RD; Preskorn, SH; Reyes, JF, 2004
)
0.32
"In drug-naive individuals with Type 2 diabetes, similar HbA(1c) levels are achieved with repaglinide when dosing is adjusted according to either post-prandial or pre-prandial levels."( Pre-prandial vs. post-prandial capillary glucose measurements as targets for repaglinide dose titration in people with diet-treated or metformin-treated Type 2 diabetes: a randomized controlled clinical trial.
Garon, J; Gerstein, HC; Joyce, C; Rolfe, A; Walter, CM, 2004
)
0.32
" Nefiracetam has been shown to potentiate ACh currents in the alpha4beta2 receptor of rat cortical neurons with a bell-shaped dose-response relationship and the maximum effect at 1 nM."( Mechanisms of action of cognitive enhancers on neuroreceptors.
Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2004
)
0.32
" Higher dosages often did not exert beneficial effects in accordance with inverted U-shaped dose-response curves described for cholinomimetics."( Symptomatic effect of donepezil, rivastigmine, galantamine and memantine on cognitive deficits in the APP23 model.
Abramowski, D; De Deyn, PP; Staufenbiel, M; Van Dam, D, 2005
)
0.33
" The results were used to simulate a 320-mg twice-daily dosing regimen."( A pharmacokinetic/pharmacodynamic model for a platelet activating factor antagonist based on data arising from Phase I studies.
Aarons, L; Brearley, C; Evans, L, 2005
)
0.33
" Moreover, the cocaine dose-response curve was flattened in the knockout group, suggesting that the differences observed between genotypes were related to changes in the reinforcing efficacy of the training dose of cocaine."( Lack of CB1 cannabinoid receptor impairs cocaine self-administration.
Ledent, C; Maldonado, R; Mendizábal, V; Parmentier, M; Robledo, P; Soria, G; Touriño, C; Valverde, O, 2005
)
0.33
" For each compound, in vitro dose-response assays were conducted with compounds applied to cloth positioned over blood reservoirs covered with Baudruche membrane against Aedes aegypti."( A new in vitro bioassay system for discovery of novel human-use mosquito repellents.
Debboun, M; Klun, JA; Kramer, M, 2005
)
0.33
"Ghrelin, GHRP-6, and capromorelin accelerated gastric emptying in an equipotent manner, with bell-shaped dose-response relationships."( Gastric motor effects of peptide and non-peptide ghrelin agonists in mice in vivo and in vitro.
De Smet, B; Depoortere, I; Kitazawa, T; Peeters, TL; Verbeke, K, 2005
)
0.33
"54 mg kg-1 D-1 dosage as a positive control drug, DZXYS in 12."( [Protective effect of Danzhi-xiaoyao San on rat brain energy or material metabolism (correction of matebolism) dealt with D-galactose].
Cai, DY; Chen, JX; Huang, QF; Sun, LP; Wang, X; Zhang, JJ; Zhang, W, 2005
)
0.33
" Upon examining the effect of increasing concentrations of TB-1-099 on the apparent K(d) and B(max) of [(125)I]RTI-55 binding to hSERT, we found that TB-1-099 decreased the B(max) in a dose-dependent manner and affected the apparent K(d) in a manner well described by a sigmoid dose-response curve."( Studies of the biogenic amine transporters. XI. Identification of a 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR12909) analog that allosterically modulates the serotonin transporter.
Boos, TL; Calhoun, WJ; Dersch, CM; Greiner, E; Jacobson, AE; Nightingale, B; Rice, KC; Rothman, RB, 2005
)
0.33
" The author provides information on recommended dosing for all three medications, noting that cholinesterase inhibitors must be titrated carefully."( Cholinesterase inhibitors in the treatment of dementia.
Ellis, JM, 2005
)
0.33
"Once-daily oral dosing of ZD6474 at 300 mg/day is generally well tolerated in patients with advanced solid tumors, and this dose is being investigated in phase II trials."( Clinical evaluation of ZD6474, an orally active inhibitor of VEGF and EGF receptor signaling, in patients with solid, malignant tumors.
Barge, A; Basser, R; de Boer, R; Eckhardt, SG; Green, M; Holden, SN; Hurwitz, HI; Rischin, D; Rosenthal, MA; Wheeler, C, 2005
)
0.33
" However, the dose-response curve against dermorphine inhibition of the response to CCK-8 was bell-shaped and the highest SR concentration also significantly decreased the mu-withdrawal response."( Involvement of the cannabinoid CB1 receptor in the opioid inhibition of the response to cholecystokinin and acute withdrawal response.
Amico, MC; Morrone, LA; Palmery, M; Romanelli, L; Tucci, P; Valeri, P, 2005
)
0.33
" Consistent with inhibition of angiogenesis, once-daily oral dosing of ZD6474 produced significant broad-spectrum antitumour activity in a panel of histologically diverse human tumour xenografts."( ZD6474--a novel inhibitor of VEGFR and EGFR tyrosine kinase activity.
Ryan, AJ; Wedge, SR, 2005
)
0.33
" The assay was applied to a pharmacokinetic study in mice to determine dosing schedules that would approximate therapeutic ZD6474 levels determined in humans."( Rapid and sensitive LC/MS/MS analysis of the novel tyrosine kinase inhibitor ZD6474 in mouse plasma and tissues.
Bradshaw, EL; Gustafson, DL; Long, ME; Zirrolli, JA, 2005
)
0.33
" Furthermore, WIN 55,212-2 at a dosage of 8 nmol/rat decreased RVM ON-cell (57+/-7%) and increased OFF-cell ongoing activities (26+/-4%)."( Periaqueductal grey CB1 cannabinoid and metabotropic glutamate subtype 5 receptors modulate changes in rostral ventromedial medulla neuronal activities induced by subcutaneous formalin in the rat.
de Novellis, V; Maione, S; Marabese, I; Mariani, L; Palazzo, E; Rossi, F; Scafuro, M; Vita, D, 2005
)
0.33
"Flavopiridol as a single agent in the above dosing schedule appears to have minimal activity as second-line chemotherapy of endometrial adenocarcinoma."( A phase II evaluation of flavopiridol as second-line chemotherapy of endometrial carcinoma: a Gynecologic Oncology Group study.
Blessing, JA; Burger, R; Grendys, EC; Hoffman, J, 2005
)
0.33
" Dose-response curve for a beta-adrenergic agonist isoproterenol was constructed in the presence and absence of a CB-1 antagonist AM251 (1 microM)."( Role of endocannabinoids in the pathogenesis of cirrhotic cardiomyopathy in bile duct-ligated rats.
Baik, SK; Gaskari, SA; Lee, SS; Li, Y; Liu, H; Moezi, L, 2005
)
0.33
" Interestingly, the same dosage regimen significantly increased the social interaction time in rats, suggesting an additional potential anxiolytic activity."( Preclinical pharmacology of F-98214-TA, a novel potent serotonin and norepinephrine uptake inhibitor with antidepressant and anxiolytic properties.
Artaiz, I; Castro, E; Del Olmo, E; Díaz, A; Innerárity, A; Labeaga, L; Orjales, A; Pazos, A; Pena, R; Ruiz-Ortega, JA; Zazpe, A, 2005
)
0.33
" Initially, we established a dose-response relationship for the acute and chronic haloperidol and DOI-induced HTR."( Effects of donepezil, nicotine and haloperidol on the central serotonergic system in mice: implications for Tourette's syndrome.
Hayslett, RL; Tizabi, Y, 2005
)
0.33
" The dosage of propofol, desflurane, and sevoflurane, obtained with a value of bispectral index (BIS) 40, was kept unchanged throughout the course, and remifentanil was titrated to maintain controlled hypotension: systolic arterial blood pressure 70 to 90 mmHg and mean arterial blood pressure 50 to 65 mmHg."( Hypotensive anesthesia and recovery of cognitive function in long-term craniofacial surgery.
Caverni, V; Favaro, R; Pinto, G; Rosa, G; Tordiglione, P, 2005
)
0.33
"Gastroretentive dosage forms have potential for use as controlled-release drug delivery systems."( Calcium silicate based microspheres of repaglinide for gastroretentive floating drug delivery: preparation and in vitro characterization.
Agrawal, GP; Awasthi, AM; Jain, NK; Jain, SK, 2005
)
0.33
" Consistent with its long duration of action, alvimopan has a slow dissociation rate from the micro opioid receptor compared to other shorter acting antagonists and may be more potent if administered prior to dosing with exogenous opioids."( [(3)H]Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists.
Cassel, JA; Daubert, JD; DeHaven, RN, 2005
)
0.33
" Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice."( Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Brodjian, S; Brune, M; Bush, E; Collins, CA; Dayton, B; Engstrom, KM; Falls, DH; Freeman, JC; Gao, J; Hernandez, LE; Kym, PR; Lynch, JK; Marsh, KC; Mulhern, MM; Shapiro, RD; Souers, AJ; Vasudevan, A; Verzal, MK; Wagaw, SH; Wodka, D, 2005
)
0.33
") dosing in rats, six of eight drugs produced dose- and time-related antinociception on both the tail flick and hot plate tests over a nearly eight-fold range of potencies."( Antinociceptive, brain-penetrating derivatives related to improgan, a non-opioid analgesic.
Hough, LB; Lu, Q; Montero, MJ; Nalwalk, JW; Shan, Z; Svokos, K; Wentland, MP, 2005
)
0.33
" The investigation of the beta-sulfones subsequently led to the discovery of hitherto unknown alpha-sulfone hydroxamates that are superior to the corresponding beta-sulfones in potency for target MMPs, selectivity vs MMP-1, and exposure when dosed orally."( Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.
Barta, TE; Becker, DP; Bedell, LJ; Boehm, TL; Carron, CP; Decrescenzo, GA; Freskos, JN; Funckes-Shippy, CL; Getman, DP; Heintz, R; Hockerman, S; Howard, SC; Li, MH; McDonald, JJ; Mehta, PP; Munie, GE; Swearingen, CA; Villamil, CI, 2005
)
0.33
" The effect of AM 251 of food intake and body weight was examined in daily (1 mg kg(-1)) and 5-day (5 mg kg(-1)) dosing schedules."( AM 251 produces sustained reductions in food intake and body weight that are resistant to tolerance and conditioned taste aversion.
Chambers, AP; Koopmans, HS; Pittman, QJ; Sharkey, KA, 2006
)
0.33
"Pharmacodynamic assessments of lymphocyte activation, function, proliferation and phenotype were performed in three settings: in vitro in whole blood isolated from untransplanted cynomolgus monkeys (cynos), in vivo in blood from untransplanted cynos dosed with CP-690,550 for 8 days, and in vivo in blood from transplanted cynos immunosuppressed with CP-690,550."( Effects of JAK3 inhibition with CP-690,550 on immune cell populations and their functions in nonhuman primate recipients of kidney allografts.
Aalami, O; Borie, DC; Campbell, A; Changelian, PS; Flores, MG; Paniagua, R; Reitz, BA; Rousvoal, G; Si, MS; Zhang, S, 2005
)
0.33
" Similar results were observed in animals dosed with CP-690,550."( Effects of JAK3 inhibition with CP-690,550 on immune cell populations and their functions in nonhuman primate recipients of kidney allografts.
Aalami, O; Borie, DC; Campbell, A; Changelian, PS; Flores, MG; Paniagua, R; Reitz, BA; Rousvoal, G; Si, MS; Zhang, S, 2005
)
0.33
" After the dose-response curve was obtained, the author measured the inotropic response to 1 micromol/L of isoproterenol in the presence of the cumulative dose of remifentanil."( Effects of remifentanil on the contractility of failing human heart muscle.
Moravec, CS; Ogletree, ML; Sprung, J, 2005
)
0.33
" The observed side effects appear amenable to improvements upon alteration of dosing strategies."( Combined use of the JAK3 inhibitor CP-690,550 with mycophenolate mofetil to prevent kidney allograft rejection in nonhuman primates.
Ball, DJ; Borie, DC; Brissette, WH; Campbell, A; Changelian, PS; Elliott, EA; Flores, MG; Higgins, JP; Kudlacz, EM; Larson, MJ; Reitz, BA; Rousvoal, G; Zhang, S, 2005
)
0.33
"The short onset and offset of remifentanil may allow for accurate dosing of sedative effect with few side-effects and rapid recovery."( Remifentanil versus propofol sedation for peribulbar anesthesia.
Aypar, U; Dal, D; Demirtaş, M; Irkeç, M; Sahin, A, 2005
)
0.33
" Dose-response studies with 6-hydroxydopamine revealed that the application of 200 microg per animal caused hypokinetic signs (decreased ambulatory activity, increased inactivity, and reduced motor coordination), which paralleled several signs of degeneration of nigrostriatal dopaminergic neurons (dopamine depletion in the caudate-putamen, and decreased mRNA levels for tyrosine hydroxylase and superoxide dismutase-1 and -2 in the substantia nigra)."( Effects of rimonabant, a selective cannabinoid CB1 receptor antagonist, in a rat model of Parkinson's disease.
de Miguel, R; Fernández-Ruiz, J; García-Arencibia, M; González, S; Ramos, JA; Scorticati, C, 2006
)
0.33
"2 mM) shifted the Ca++ dose-response curves to the right, similar to that produced by verapamil (0."( Synthesis and smooth muscle-selective relaxant activity of a piperidine analogue: 1-(4'-fluorophenacyl)-4-hydroxy-4-phenyl-piperidinium chloride.
Aftab, MT; Ghayur, MN; Gilani, AH; Saify, ZS; Taqvi, SI, 2006
)
0.33
" These results indicate that the endogenous OFQ/N system is differentially involved in morphine tolerance development and establishment of opiate dependence, depending on the specific morphine dosage regimen."( Endogenous orphanin FQ/nociceptin is involved in the development of morphine tolerance.
Chung, S; Civelli, O; Pohl, S; Reinscheid, RK; Zeng, J, 2006
)
0.33
" The incorporation of an empirical approach to dosing in mouse models of cancer in preclinical studies may allow for better prediction of clinical efficacy for ZD6474 alone and in combination with other therapeutic modalities based on equivalent drug exposure."( Tissue distribution and metabolism of the tyrosine kinase inhibitor ZD6474 (Zactima) in tumor-bearing nude mice following oral dosing.
Bradshaw-Pierce, EL; Gustafson, DL; Merz, AL; Zirrolli, JA, 2006
)
0.33
" The drug was administered at a dosage of 5 mg/day for 1 month and 10 mg/day for the following 7 months, as tolerated."( Cardiovascular effects and risk of syncope related to donepezil in patients with Alzheimer's disease.
Bordier, P; Garrigue, S; Gencel, L; Lafitte, A; Lanusse, S; Margaine, J; Robert, F, 2006
)
0.33
" MR signal from fluorine-containing tecastemizole-related moieties was observed in situ only at day 8 in the liver of three of five subjects dosed at 270 mg/day."( Magnetic resonance spectroscopy for measuring the biodistribution and in situ in vivo pharmacokinetics of fluorinated compounds: validation using an investigation of liver and heart disposition of tecastemizole.
Bolo, NR; Frederick, B; Hashoian, R; Hirashima, F; Hsu, R; Hwang, J; Jones, S; Koch, P; Lyoo, IK; Maier, G; Nassar, L; Renshaw, PF; Schneider, E; Sung, Y; Villafuerte, RA; Wilkinson, S, 2006
)
0.33
"Short-acting agents for neuromuscular block (NMB) require frequent dosing adjustments for individual patient's needs."( Model-based control of neuromuscular block using mivacurium: design and clinical verification.
Leibundgut, D; Pfister, CA; Schumacher, PM; Stadler, KS; Wirz, R; Zbinden, AM, 2006
)
0.33
" Moreover, dose-response curves of the agonists showed that mu and CB1 receptors mediating inhibition of [3H]glutamate release display a non-additive interaction, whereas these receptors synergistically interact regarding their inhibitory control of [3H]GABA release."( Interactions between CB1 cannabinoid and mu opioid receptors mediating inhibition of neurotransmitter release in rat nucleus accumbens core.
De Vries, TJ; Hogenboom, F; Schoffelmeer, AN; Wardeh, G, 2006
)
0.33
" Diet-induced obese (DIO) rats were dosed with rimonabant (3, 10 mg/kg PO once daily) and matched with pair-fed controls."( The cannabinoid CB1 receptor inverse agonist, rimonabant, modifies body weight and adiponectin function in diet-induced obese rats as a consequence of reduced food intake.
Benwell, KR; Clifton, PG; Kennett, GA; Misra, A; Revell, DF; Sellwood, DM; Thornton-Jones, ZD; Vickers, SP, 2006
)
0.33
"This study compared dosing and utilization patterns of the cholinesterase inhibitors (ChEIs) donepezil, rivastigmine, and galantamine in the nursing home setting."( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis.
Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006
)
0.33
" The mean daily dosage of donepezil was above the effective dose throughout the study period, whereas the mean daily dosage was below the effective dose for the first 3 months with rivastigmine and did not approach the effective dose for galantamine until month 12."( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis.
Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006
)
0.33
"The results of this study suggest that early effective dosing occurred more often with donepezil than with rivastigmine or galantamine in these nursing home residents."( Patterns of cholinesterase-inhibitor use in the nursing home setting: a retrospective analysis.
Dybicz, SB; Erwin, WG; Keohane, DJ; McRae, T; Shah, SN, 2006
)
0.33
"To examine the effects of the histamine H(2)-receptor antagonist, lafutidine, at clinical dosage (10 mg tablet after a standardized meal) on plasma levels of the gastrointestinal peptides, calcitonin gene-related peptide (CGRP), somatostatin and gastrin."( Calcitonin gene-related peptide and somatostatin releases correlated with the area under the lafutidine concentration-time curve in human plasma.
Azuma, Y; Ikawa, K; Inoue, M; Morikawa, N; Shimatani, T, 2006
)
0.33
"Lafutidine at clinical dosage increases plasma CGRP and the somatostatin."( Calcitonin gene-related peptide and somatostatin releases correlated with the area under the lafutidine concentration-time curve in human plasma.
Azuma, Y; Ikawa, K; Inoue, M; Morikawa, N; Shimatani, T, 2006
)
0.33
" SR 141716 elicited a significant increase in paw tremors in mice that were repeatedly dosed with either marijuana or Delta(9)-THC."( SR 141716 (Rimonabant) precipitates withdrawal in marijuana-dependent mice.
Harloe, JP; Lichtman, AH; Martin, BR; Varvel, SA; Wilson, DM, 2006
)
0.33
") on plasma corticosterone 60 min postinjection were retained after subchronic dosing (5 days, once daily) in mice."( Cannabinoid CB1 receptor antagonism modulates plasma corticosterone in rodents.
Degroot, A; Nomikos, GG; Wade, MR, 2006
)
0.33
" Total codeine dosage was also similar, except at 4 h postoperatively when it was higher in the block group."( A comparison between scalp nerve block and morphine for transitional analgesia after remifentanil-based anesthesia in neurosurgery.
Ayoub, C; Boudreault, D; Chouinard, P; Girard, F; Moumdjian, R; Ruel, M, 2006
)
0.33
" Disease dynamics must be considered to evaluate treatment response adequately and optimise the dosing regimen in migraine."( A model-based approach to treatment comparison in acute migraine.
Danhof, M; Della Pasqua, O; Maas, HJ, 2006
)
0.33
" Problems with potency of CX516 in other studies have suggested dosing may have been inadequate for therapeutic effect and thus it remains unclear whether modulation of AMPA-mediated neurotransmission is a viable therapeutic strategy for the treatment of FXS."( Effect of CX516, an AMPA-modulating compound, on cognition and behavior in fragile X syndrome: a controlled trial.
Berry-Kravis, E; Block, SS; Cogswell, J; Cook, E; Decle, P; Guter, S; Hagerman, R; Jardini, T; Johnson, SA; Krause, SE; Lara, R; Leurgans, S; Maino, D; Potanos, K; Salt, J; Weinberg, D; Wuu, J, 2006
)
0.33
"05-5pmol) induced anxiolytic-like effects with bell-shaped dose-response curves, the higher doses being ineffective."( Anxiolytic-like effect of cannabinoids injected into the rat dorsolateral periaqueductal gray.
Aguiar, DC; Guimarães, FS; Moreira, FA, 2007
)
0.34
"Patients enrolled in the present study had a 6-week single-blind placebo washout period followed by treatment with donepezil 5 mg/day for 6 weeks with an optional increase in dosage to 10 mg/day between weeks 6 and 32."( Efficacy and safety of donepezil over 3 years: an open-label, multicentre study in patients with Alzheimer's disease.
Burns, A; Gauthier, S; Perdomo, C, 2007
)
0.34
" Monkeys (four per group) were dosed via nasogastric tube for 7 d with l-CDB-4022 at 12."( Development of l-CDB-4022 as a nonsteroidal male oral contraceptive: induction and recovery from severe oligospermia in the adult male cynomolgus monkey (Macaca fascicularis).
Attardi, BJ; Hess, RA; Hild, SA; Koduri, S; Marshall, GR; Plant, TM; Ramaswamy, S; Reel, JR; Schlatt, S; Simorangkir, DR, 2007
)
0.34
" dosing of a novel MCHR1 antagonist, N-[3-(1-{[4-(3,4-difluorophenoxy)-phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847), in three mouse models predictive of antidepressant/anxiolytic-like activity: novelty suppressed feeding (NSF) in 129S6/SvEvTac mice and light/dark paradigm (L/D) and forced swim test (FST) in BALB/cJ mice."( Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocam
Craig, DA; David, DJ; Dong, D; Gerald, CP; Hegde, LG; Hen, R; Holick, KA; Klemenhagen, KC; Marzabadi, MR; Mendez, I; Ping, XI; Santarelli, L; Saxe, MD; Swanson, CJ; Zhong, H, 2007
)
0.34
"05); the dose-response curve was shifted to the left in the obese."( Effects of cannabinoid receptors on skeletal muscle oxidative pathways.
Cameron-Smith, D; Cavuoto, P; Hatzinikolas, G; McAinch, AJ; Wittert, GA, 2007
)
0.34
"The pharmacology, pharmacokinetics, clinical efficacy, safety, drug interactions, and dosage and administration of rimonabant in the treatment of obesity and related metabolic factors are reviewed."( Rimonabant: a novel selective cannabinoid-1 receptor antagonist for treatment of obesity.
Patel, PN; Pathak, R, 2007
)
0.34
" This study aimed to evaluate the schedule-dependent interaction of clinically relevant dosing of vandetanib with RT in human head and neck cancer models that had been characterized as EGFR positive (EGFR+) or negative (EGFR-) in order to begin differentiating vandetanib and RT interactions at the level of antitumor (EGFR) or antivascular (VEGFR2) activities."( Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
Frederick, B; Gustafson, DL; Merz, AL; Raben, D, 2008
)
0.35
" Vandetanib was dosed at 30 mg kg(-1) day(-1) based on pharmacokinetic studies in nude mice showing that this dose results in drug exposure similar to that seen in humans at clinical doses."( Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
Frederick, B; Gustafson, DL; Merz, AL; Raben, D, 2008
)
0.35
" That some patients still yielded to acute organophosphate poisoning despite repeated dosing of atropine suggests that cellular mechanisms that are independent of muscarinic receptor activation may also be engaged in organophosphate poisoning."( Muscarinic receptor-independent activation of cyclic adenosine monophosphate-dependent protein kinase in rostral ventrolateral medulla underlies the sympathoexcitatory phase of cardiovascular responses during mevinphos intoxication in the rat.
Chan, SH; Chang, AY; Tsai, CY; Wu, CH, 2007
)
0.34
" An unexpectedly large placebo effect, inadequate dosage (mean 120 mg/day), and inadequate power may have contributed to lack of demonstrable benefit."( Quetiapine for agitation or psychosis in patients with dementia and parkinsonism.
Cummings, J; Kurlan, R; Raman, R; Thal, L, 2007
)
0.34
" Near-maximal inhibition of c-Met activity for the full dosing interval was necessary to maximize the efficacy of PF-2341066."( An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms.
Alton, G; Arango, ME; Bender, SL; Christensen, JG; Cui, JJ; Koudriakova, TB; Kung, PP; Lee, JH; Li, Q; Los, G; McDonnell, SR; Mroczkowski, B; Nambu, MD; Yamazaki, S; Zou, HY, 2007
)
0.34
" Further investigation would be required to determine whether individual patients, or those with particular epilepsy syndromes, might benefit from donepezil or other acetylcholinesterase inhibitors, or if a higher dosage might be effective."( A randomized, double-blind, placebo-controlled trial of donepezil to improve memory in epilepsy.
Choi, H; Hamberger, MJ; Hirsch, LJ; Palmese, CA; Scarmeas, N; Weintraub, D, 2007
)
0.34
" Excretion of radioactivity was rapid and nearly complete within 48 h after dosing in both species."( Metabolism, distribution and excretion of a selective N-methyl-D-aspartate receptor antagonist, traxoprodil, in rats and dogs.
Butler, T; Cui, D; Potchoiba, MJ; Prakash, C, 2007
)
0.34
"Inter- and intra-individual variability of the loratadine (LOR) metabolism in Caucasian subjects was assessed during a bioequivalence study for two pharmaceutical formulations (solid oral dosage forms) containing 10 mg of the active substance."( Validated ion pair liquid chromatography/fluorescence detection method for assessing the variability of the loratadine metabolism occurring in bioequivalence studies.
David, V; Medvedovici, A; Sora, DI; Udrescu, S, 2007
)
0.34
" Nevertheless, whereas in the case of donepezil there seems to be a positive relation between the maximum dosage and response, for galanthamine doses above 24 mg/day do not seem to offer any improvement."( [Galanthamine versus donepezil in the treatment of Alzheimer's disease].
Garre-Olmo, J; López-Pousa, S; Vilalta-Franch, J,
)
0.13
" Furthermore, it has been shown that improved clinical efficacy can be attained with an increased dosage of 20 mg daily in comparison to the usual dosage of 10 mg/day without increasing the rate of side effects."( [New generation antihistamines as monotherapy or in combination. What is the relevance for daily clinical routine for allergic rhinoconjunctivitis].
Köberlein, J; Mösges, R, 2007
)
0.34
" A leftward shift in the dose-response curve was observed following WIN55,212-2 relative to morphine treatment."( Activation of cannabinoid CB1 and CB2 receptors suppresses neuropathic nociception evoked by the chemotherapeutic agent vincristine in rats.
Hohmann, AG; Makriyannis, A; Rahn, EJ, 2007
)
0.34
" CD1 mice were dosed either acutely or chronically with either antidepressants or 5-HT receptor subtype selective antagonists."( Hippocampal Bcl-2 expression is selectively increased following chronic but not acute treatment with antidepressants, 5-HT(1A) or 5-HT(2C/2B) receptor antagonists.
Hutson, PH; Murray, F, 2007
)
0.34
" Therefore, the model can serve as a tool to simulate and evaluate different dosing regimens for further clinical trials."( Population Pharmacokinetic Data Analysis of Cilobradine, an I f Channel Blocker.
Fliss, G; Kloft, C; Schaefer, HG; Staab, A; Tillmann, C; Trommeshauser, D, 2008
)
0.35
" Tolerability can be increased by use of flexible dosing and efficacy is likely to be enhanced by increasing the length of the trial from six to 12 months and by enriching the sample with subjects more likely to decline during the trial."( Key lessons learned from short-term treatment trials of cholinesterase inhibitors for amnestic MCI.
Correia, S; Richardson, S; Salloway, S, 2008
)
0.35
"25-1 mg/kg) did not alter the dose-response curve of nicotine, while DOI (0."( Effects of the serotonin 5-HT2A and 5-HT2C receptor ligands on the discriminative stimulus effects of nicotine in rats.
Filip, M; McCreary, AC; Przegaliński, E; Zaniewska, M, 2007
)
0.34
"We assessed the minimal remifentanil dosage required for tracheal tube tolerance in awake and spontaneously breathing patients after major abdominal surgery."( Remifentanil for tracheal tube tolerance: a case control study.
Fässler, K; Gonano, C; Gustorff, B; Illievich, UM; Machata, AM; Spiss, CK, 2007
)
0.34
" Data were also collected on post-treatment weight gain, and, as prolonged appetite suppression has been found after single dosing with compounds of this series, rats were reassessed (drug-free) for food intake 7 days after initial testing."( Grooming, scratching and feeding: role of response competition in acute anorectic response to rimonabant in male rats.
Blundell, JE; Rodgers, RJ; Tallett, AJ, 2007
)
0.34
" Because a) the mechanism of action of improgan remains unknown and b) this drug may indirectly activate cannabinoid CB(1) receptors, the effects of the CB(1) antagonist/inverse agonist rimonabant (SR141716A) and 3 congeners with varying CB(1) potencies were studied on improgan antinociception after intracerebroventricular (icv) dosing in rats."( Significance of cannabinoid CB1 receptors in improgan antinociception.
Abood, ME; Gehani, NC; Hough, LB; Martin, BR; Nalwalk, JW; Razdan, RK; Sun, X; Wentland, M, 2007
)
0.34
"Although pain and satisfaction scores were similar in both groups, the regimen used in Group A was associated with fewer side effects compared to the Group B dosing regimen."( Remifentanil patient-controlled analgesia for labour: optimizing drug delivery regimens.
Balki, M; Bernstein, P; Carvalho, JC; Dhumne, S; Kasodekar, S, 2007
)
0.34
" When administered 20 min before acquisition, memantine elicited an inverted U-shape dose-response relationship, with low doses (0."( The uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist memantine prolongs spatial memory in a rat delayed radial-arm maze memory task.
Lichtman, AH; Wise, LE, 2007
)
0.34
" This review focuses on a novel dosing regimen that has achieved significant clinical activity in relapsed, poor-risk chronic lymphocytic leukemia."( Flavopiridol in the treatment of chronic lymphocytic leukemia.
Byrd, JC; Christian, BA; Grever, MR; Lin, TS, 2007
)
0.34
"Binding to human plasma proteins reduces free flavopiridol concentration and makes continuous intravenous infusion dosing ineffective."( Flavopiridol in the treatment of chronic lymphocytic leukemia.
Byrd, JC; Christian, BA; Grever, MR; Lin, TS, 2007
)
0.34
" Repaglinide has primarily a role in the treatment of T2DM when metformin cannot be used due to adverse effects, when metformin fails to adequately control blood glucose levels, when there is a need for flexible dosing (i."( Defining the role of repaglinide in the management of type 2 diabetes mellitus: a review.
Birkeland, KI; Johansen, OE, 2007
)
0.34
" In a series of follow-up studies using hallucinogen-induced head twitch response and phencyclidine-induced hyperlocomotion, it was additionally discovered that the repeated dosing regimen required for discrimination training attenuated the behavioral effects of the mGlu2/3 receptor agonist LY379268."( Chronic phenethylamine hallucinogen treatment alters behavioral sensitivity to a metabotropic glutamate 2/3 receptor agonist.
Benneyworth, MA; Sanders-Bush, E; Smith, RL, 2008
)
0.35
" Further in-depth studies in a large number of patients receiving different dosage regimens are required to confirm these results and further our understanding of a possible clinical advantage arising from the bioenhancement capabilities of piperine in the treatment of HIV infection."( Influence of piperine on the pharmacokinetics of nevirapine under fasting conditions: a randomised, crossover, placebo-controlled study.
Kasibhatta, R; Naidu, MU, 2007
)
0.34
" Intrasubject variability in the pharmacokinetic parameters was less pronounced after multiple dosing (17%) than that after single dosing (33%) of lonafarnib."( Effect of food on the pharmacokinetics of lonafarnib (SCH 66336) following single and multiple doses.
Cutler, DL; Statkevich, P; Zhu, Y, 2007
)
0.34
" These dosing schedules resulted in significant effects on tumor vasculature, with decreased volume transfer constants, area under the curve, and permeability surface factor as well as increased gadolinium clearance after 30 days of treatment."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
" Selected compounds showed significant reduction of Abeta levels upon oral dosing in a transgenic murine model of Alzheimer's disease."( Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
Chu, I; Clader, JW; Del Vecchio, RA; Favreau, L; Greenlee, WJ; Hyde, LA; McBriar, MD; Nomeir, AA; Parker, EM; Pissarnitski, DA; Song, L; Zhang, L; Zhao, Z, 2008
)
0.35
" However, fentanyl concentration decreases quite rapidly and patients may need repeated dosing until analgesia is attained."( [Postoperative analgesia after remifentanil].
Kiyama, S, 2007
)
0.34
" After extinction of responding with saline self-administration, dose-response studies showed that cocaine reliably and dose dependently maintained responding greater than saline in all wild-type mice but in none of the D1 receptor knock-out mice."( Lack of self-administration of cocaine in dopamine D1 receptor knock-out mice.
Berkowitz, JS; Caine, SB; Gabriel, KI; Gold, LH; Koob, GF; Thomsen, M; Tonegawa, S; Xu, M; Zhang, J, 2007
)
0.34
" This dosing regimen was supported by the pharmacokinetic profile of JNJ 26993135, along with the demonstration of the inhibition of ex vivo production of LTB(4) in whole blood following oral administration."( Attenuation of inflammation and cytokine production in rat colitis by a novel selective inhibitor of leukotriene A4 hydrolase.
Berko, A; Dunford, PJ; Fourie, AM; Horvath, K; Lundeen, KA; Posa, A; Riley, JP; Varga, C; Whittle, BJ, 2008
)
0.35
" The most frequently reported adverse events were abdominal pain, nausea, and diarrhea, occurring more frequently in the higher dosage groups."( Alvimopan, a peripherally acting mu-opioid receptor (PAM-OR) antagonist for the treatment of opioid-induced bowel dysfunction: results from a randomized, double-blind, placebo-controlled, dose-finding study in subjects taking opioids for chronic non-cance
Carter, E; Irving, G; Jansen, JP; Kleoudis, C; Lasko, B; Morlion, B; Mortensen, E; Peppin, J; Pierce, A; Snidow, J; Webster, L, 2008
)
0.35
" The mean therapeutic dosage of insulin glargine in group A was 14."( Therapeutic options for elderly diabetic subjects: open label, randomized clinical trial of insulin glargine added to oral antidiabetic drugs versus increased dosage of oral antidiabetic drugs.
Alagona, C; Chiavetta, A; Fedele, V; Leotta, C; Lorenti, I; Luca, S; Papa, G; Pezzino, V; Piro, S; Purrello, F; Rabuazzo, AM; Spadaro, L, 2008
)
0.35
" Compound 11a possessed desirable pharmaceutical properties, including excellent brain exposure and long brain half-life following oral dosing to mice."( Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.
Andresson, T; Bedell, L; Bjornsson, JM; Bragason, G; Burghes, AH; Butchbach, ME; Coovert, DD; Gurney, ME; Haraldsson, M; Keyvan, M; Mishra, R; Pai, G; Palomo, M; Pease, B; Rao, M; Singh, J; Thosteinsdottir, M; Thurmond, J, 2008
)
0.35
" twice daily) and alcohol dose-response curves were carried out on firing rate of BLA neurons 24 hours following the last injection of the cannabinoid agonist."( Alcohol inhibits spontaneous activity of basolateral amygdala projection neurons in the rat: involvement of the endocannabinoid system.
Luchicchi, A; Perra, S; Pillolla, G; Pistis, M, 2008
)
0.35
" At week 6 of randomization, the dosage of donepezil was increased to 10 mg/d."( A double-blind, placebo-controlled trial of donepezil for the treatment of menopause-related cognitive loss.
Devi, G; Khosrowshahi, L; Laakso, UK; Massimi, S; Schultz, S, 2007
)
0.34
" Animals dosed with CP-690550 (15 mg/kg/d) during the period of antigen sensitization and boost demonstrated marked reductions in BAL eosinophils and levels of IL-13 and eotaxin following ovalbumin aerosol exposure."( The JAK-3 inhibitor CP-690550 is a potent anti-inflammatory agent in a murine model of pulmonary eosinophilia.
Andresen, C; Changelian, P; Conklyn, M; Kudlacz, E; Whitney-Pickett, C, 2008
)
0.35
"7s during this dosing protocol."( Antinociceptive effects of high-dose remifentanil in male methadone-maintained patients.
Bochner, F; Hay, JL; Somogyi, AA; White, JM, 2008
)
0.35
"This study describes a pharmacodynamic model during general anaesthesia in children relating the bispectral index (BIS) response to the anaesthetic dosing of propofol, fentanyl, and remifentanil."( Pharmacodynamic modelling of the bispectral index response to propofol-based anaesthesia during general surgery in children.
Ammon, C; Fechner, J; Ihmsen, H; Jeleazcov, C; Schmidt, J; Schüttler, J; Schwilden, H, 2008
)
0.35
" Because fat oxidation measured by indirect calorimetry increased immediately after dosing in the postprandial state, the acute effect of rimonabant on lipolysis was investigated in postprandial male rats."( Increased energy expenditure contributes more to the body weight-reducing effect of rimonabant than reduced food intake in candy-fed wistar rats.
Elvert, R; Haschke, G; Herling, AW; Kilp, S; Kramer, W, 2008
)
0.35
" Additionally, it was investigated whether the effect of a fixed dosage of propofol on the attained depth of hypnosis during induction of anaesthesia is different in male and female patients."( Comparison of Narcotrend Index, Bispectral Index, spectral and entropy parameters during induction of propofol-remifentanil anaesthesia.
Grouven, U; Kneif, T; Schultz, A; Schultz, B; Siedenberg, M, 2008
)
0.35
"In children, as in adults, BIS values were highly correlated with the corresponding Ct or Cm of propofol following classical E(max) dose-response curves."( The relationship between bispectral index and propofol during target-controlled infusion anesthesia: a comparative study between children and young adults.
Constant, I; De-Smet, T; Girault, L; Louvet, N; Murat, I; Piat, V; Rigouzzo, A; Seeman, R; Servin, F, 2008
)
0.35
" We studied the effect of dosing interval on the extent of the gemfibrozil-repaglinide interaction."( The effect of gemfibrozil on repaglinide pharmacokinetics persists for at least 12 h after the dose: evidence for mechanism-based inhibition of CYP2C8 in vivo.
Backman, JT; Kalliokoski, A; Laitila, J; Neuvonen, M; Neuvonen, PJ; Niemi, M; Tornio, A, 2008
)
0.35
" A statistically significant dose-response relationship was demonstrated with the SIB and CIBIC-plus."( Donepezil treatment of patients with severe Alzheimer's disease in a Japanese population: results from a 24-week, double-blind, placebo-controlled, randomized trial.
Arimoto, I; Asada, T; Homma, A; Imai, Y; Iwamoto, T; Koma, H; Ohbayashi, T; Shigeta, M; Tago, H; Takita, M, 2008
)
0.35
"This study confirmed the effectiveness of donepezil 10 mg/day in patients with severe AD and demonstrated a significant dose-response relationship."( Donepezil treatment of patients with severe Alzheimer's disease in a Japanese population: results from a 24-week, double-blind, placebo-controlled, randomized trial.
Arimoto, I; Asada, T; Homma, A; Imai, Y; Iwamoto, T; Koma, H; Ohbayashi, T; Shigeta, M; Tago, H; Takita, M, 2008
)
0.35
" On day 14, mean peak DPP-4 inhibition ranged from 94% to 99%, and mean inhibition at 24 hours after dosing ranged from 82% to 97% across all alogliptin doses."( Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Mekki, QA; Wann, ER, 2008
)
0.35
" The PK and PD profiles of multiple doses of alogliptin in this study supported use of a once-daily dosing regimen."( Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor alogliptin: a randomized, double-blind, placebo-controlled, multiple-dose study in adult patients with type 2 diabetes.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Mekki, QA; Wann, ER, 2008
)
0.35
" Blood and urine were collected over 72 hours after dosing for pharmacokinetic analysis and determination of plasma DPP-4 inhibition and active glucagon-like peptide -1(GLP-1) concentrations."( Pharmacokinetics, pharmacodynamics, and tolerability of single increasing doses of the dipeptidyl peptidase-4 inhibitor alogliptin in healthy male subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Mekki, QA; Wann, ER, 2008
)
0.35
" Across alogliptin doses, mean peak DPP-4 inhibition ranged from 93% to 99%, and mean inhibition at 24 hours after dosing ranged from 74% to 97%."( Pharmacokinetics, pharmacodynamics, and tolerability of single increasing doses of the dipeptidyl peptidase-4 inhibitor alogliptin in healthy male subjects.
Christopher, R; Covington, P; Davenport, M; Fleck, P; Karim, A; Mekki, QA; Wann, ER, 2008
)
0.35
" It has been reported that remifentanil is suitable because of its wide dosage window with respect to recording MEP."( [Anesthetic management of a case of craniotomy using TCI of remifentanil with intraoperative monitoring of motor evoked potential].
Ito, T; Iwasaki, H; Kunisawa, T; Nagashima, M; Omachi, H; Ozaki, Y; Suzuki, A; Takahata, O, 2008
)
0.35
"CBD injected into the dlPAG produced anxiolytic-like effects in the EPM with a bell-shaped dose-response curve."( Involvement of 5HT1A receptors in the anxiolytic-like effects of cannabidiol injected into the dorsolateral periaqueductal gray of rats.
Campos, AC; Guimarães, FS, 2008
)
0.35
" Clinicians should be aware of this possible clarithromycin-repaglinide interaction; in particular, in elderly patients with type 2 diabetes who are taking repaglinide and begin clarithromycin therapy, blood glucose levels should be monitored closely for potential dosage adjustment of repaglinide."( Severe hypoglycemia from clarithromycin-repaglinide drug interaction.
Khamaisi, M; Leitersdorf, E, 2008
)
0.35
" Ablation of peripheral NK1 receptors attenuated the ability of GR73632 to induce a maximal frequency of emesis and shifted its percent animals vomiting dose-response curve to the right."( Utilization of the least shrew as a rapid and selective screening model for the antiemetic potential and brain penetration of substance P and NK1 receptor antagonists.
Abad, J; Darmani, NA; Ramirez, J; Ray, AP; Thrush, GR; Wang, Y, 2008
)
0.35
" This method has the lowest lower limit of quantitation (LLOQ) reported to date for flavopiridol, and it allows for more accurate determination of terminal phase concentrations and improved pharmacokinetic parameter estimation in patients receiving an active dosing schedule of flavopiridol."( Development and validation of a sensitive liquid chromatography/mass spectrometry method for quantitation of flavopiridol in plasma enables accurate estimation of pharmacokinetic parameters with a clinically active dosing schedule.
Albanese, KA; Byrd, JC; Dalton, JT; Farley, KL; Grever, MR; Johnston, JS; Lin, TS; Phelps, MA; Rozewski, DM, 2008
)
0.35
" The effects of chronic dosing of SCH 221510 were also assessed."( The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510).
Carey, GJ; Coffin, VL; Cohen-Williams, ME; Fawzi, AB; Graziano, MP; Ho, GD; Hodgson, RA; Lu, SX; Matasi, J; Morgan, CA; Smith-Torhan, A; Tulshian, D; Varty, GB; Zhang, H, 2008
)
0.35
" Our results indicate clearly a dose-response blockade of extinction induced by AM251 injected into the striatum but a facilitation of extinction when administered into the hippocampus."( Impairment of endocannabinoids activity in the dorsolateral striatum delays extinction of behavior in a procedural memory task in rats.
Méndez-Díaz, M; Montes-Rodriguez, CJ; Prospéro-García, O; Rueda-Orozco, PE; Soria-Gomez, E, 2008
)
0.35
"To better understand the mechanisms involved in cannabinoid modulation of vocal behavior, we have investigated the dose-response relationship between systemic cannabinoid exposure and changes in neuronal activity (as indicated by expression of the transcription factor, c-Fos) within telencephalic brain regions, with established involvement in song learning and/or control."( CB(1) cannabinoid receptor activation dose dependently modulates neuronal activity within caudal but not rostral song control regions of adult zebra finch telencephalon.
Soderstrom, K; Tian, Q, 2008
)
0.35
" The interaction was observed after administration of DHQ and 3M-GBP combination at fixed dose ratios of 1:10 and 1:30 and the dose-response curves shifted approximately 13- and 17-fold leftward, respectively, from the theoretical additive values."( Synergy between a NR2B receptor antagonist DHQ and 3-methyl-gabapentin in mice with neuropathic pain.
Hizue, M; Imai, A; Toide, K, 2008
)
0.35
" The increased responding observed in the MW group compared with the control and MD groups resulted in an upward shift in the remifentanil dose-response curve, an effect that was expressed only after repeated exposure to the contingency, demonstrating that morphine withdrawal ultimately enhances the reinforcing effects of remifentanil."( Morphine deprivation increases self-administration of the fast- and short-acting mu-opioid receptor agonist remifentanil in the rat.
Cooper, ZD; Shi, YG; Truong, YN; Woods, JH, 2008
)
0.35
" Phase I studies have established that it is suitable for once-daily oral dosing at a dose of up to 300 mg."( Dual targeting of the vascular endothelial growth factor receptor and epidermal growth factor receptor pathways with vandetinib (ZD6474) in patients with advanced or metastatic non-small cell lung cancer.
Natale, RB, 2008
)
0.35
" In summary, these data suggest that alogliptin is a potent and highly selective DPP-4 inhibitor with demonstrated efficacy in Zucker fa/fa rats and potential for once-daily dosing in humans."( Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys.
Asakawa, T; Christopher, RJ; Kassel, DB; Lee, B; Shi, L; Takeuchi, K, 2008
)
0.35
" dosing to the ferret, casopitant was rapidly absorbed, with plasma and brain concentrations being approximately equal at 2 h postdose."( Pharmacokinetics and brain penetration of casopitant, a potent and selective neurokinin-1 receptor antagonist, in the ferret.
Bambal, R; Davis, CB; Gontarek, RR; Han, C; King, AG; Mencken, T; Minthorn, E; Rominger, D; Shu, A, 2008
)
0.35
" A first-derivative UV spectroscopic method was developed for the determination of repaglinide in tablet dosage form and for dissolution testing."( A comparative study of first-derivative spectrophotometry and column high-performance liquid chromatography applied to the determination of repaglinide in tablets and for dissolution testing.
AlKhalidi, BA; AlKhatib, HS; Bustanji, Y; Mohammad, M; Shtaiwi, M,
)
0.13
" Dose-response analyses were performed for various 5-HT(2A) antagonist reference agents, providing receptor occupancy ED(50) values in conjunction with plasma and brain concentration levels."( Validation of a rat in vivo [(3)H]M100907 binding assay to determine a translatable measure of 5-HT(2A) receptor occupancy.
Bowman, C; Buchholz, L; Buist, S; Campbell, JE; Galvan, B; Grimwood, S; Henry, B; Knauer, CS; Osgood, S; Shahid, M; Wong, EH, 2008
)
0.35
" immediately after each dosing of 5-FU significantly reversed the delay in healing by 5-FU, and this effect was attenuated by the chemical ablation of capsaicin-sensitive afferent neurons."( Impairment by 5-fluorouracil of the healing of gastric lesions in rats: effect of lafutidine, a histamine H2 receptor antagonist, mediated by capsaicin-sensitive afferent neurons.
Amagase, K; Hayashi, S; Komatsu, Y; Kotani, T; Murashima, Y; Nakagiri, A; Takeuchi, K, 2009
)
0.35
" The results showed that piperine at all dosage range used in this study possessed anti-depression like activity and cognitive enhancing effect at all treatment duration."( Piperine, the potential functional food for mood and cognitive disorders.
Chonpathompikunlert, P; Muchimapura, S; Priprem, A; Tankamnerdthai, O; Wattanathorn, J, 2008
)
0.35
" RI was compared to the ARB, candesartan (3 mg/kg/day PO), and to the ACEI, enalapril (60 mg/kg/day PO) in a 4-week dosing paradigm."( A nonpeptide, piperidine renin inhibitor provides renal and cardiac protection in double-transgenic mice expressing human renin and angiotensinogen genes.
Carlson, T; Kowala, MC; Leadley, R; Major, TC; Okerberg, C; Olszewski, B; Ostroski, R; Rosebury, W; Schroeder, R, 2008
)
0.35
" We determine the effects of sub-chronic dosing of ChEIs on alpha7 and non-alpha7 nAChRs and determine if differences can be observed between them."( Effects of cholinesterase inhibitors on rat nicotinic receptor levels in vivo and in vitro.
Reid, RT; Sabbagh, MN, 2008
)
0.35
" Furthermore, a dose-response analysis (3, 10, 30 mg/kg) revealed a clear dose-dependent efficacy of the drug: 3 mg/kg was without effect, whilst 10 mg/kg led to an intermediate enhancement in performance."( The glycine transporter 1 inhibitor SSR504734 enhances working memory performance in a continuous delayed alternation task in C57BL/6 mice.
Feldon, J; Singer, P; Yee, BK, 2009
)
0.35
" Docetaxel may exert antiangiogenic effects if dosed so plasma levels are maintained at low nanomolar concentrations over a prolonged time."( Pharmacokinetic-directed dosing of vandetanib and docetaxel in a mouse model of human squamous cell carcinoma.
Bradshaw-Pierce, EL; Gustafson, DL; Raben, D; Steinhauer, CA, 2008
)
0.35
" Dose-response curves of donepezil effect both on I (C) and I (K) were shifted right along horizontal axis when donepezil was applied in combination with TEA."( The binding of donepezil with external mouth of K+-channels of molluscan neurons.
Bukanova, JV; Marchenko, EV; Rossokhin, AV; Skrebitsky, VG; Solntseva, EI, 2009
)
0.35
" The dosage rose to 10 mg daily for another 6 weeks before a 2-week course of cognitive training and was maintained for the remainder of a year."( Acetylcholinesterase inhibitor in combination with cognitive training in older adults.
Ashford, JW; Friedman, L; Hoblyn, J; Kraemer, HC; Mumenthaler, MS; Noda, A; Yesavage, JA, 2008
)
0.35
" SERMs known to cause ovarian cysts upregulate Cyp17a1 after only 4 days of dosing and suppression of the HPO axis prevented this regulation, indicating that ovarian expression of Cyp17a1 was secondary to SERM's effect on the brain."( Development of an early biomarker for the ovarian liability of selective estrogen receptor modulators in rats.
Azam, F; Chennathukuzhi, VM; Harris, HA; Huselton, C; Jelinsky, SA; Mekonnen, B; Negahban, A; Patel, VS; Schelling, SH; Winneker, RC; Zhang, X, 2008
)
0.35
" When rats were dosed with indinavir as a P450 3A probe substrate, plasma exposure to indinavir increased three-fold following pretreatment with 1, consistent with drug-drug interaction projections based on the k(inact) and K(I) parameters for 1 in rat liver microsomes."( Assessing and minimizing time-dependent inhibition of cytochrome P450 3A in drug discovery: a case study with melanocortin-4 receptor agonists.
Baillie, TA; Bakshi, RK; Chen, Q; Dean, DC; Miller, RR; Nargund, RP; Ngui, J; Stearns, RA; Tang, W; Wang, RW, 2008
)
0.35
" Also, a dose-response relationship was established between the dose of cyclosporin A and the brain uptake of [(123)I]R91150 in mice."( Effect of cyclosporin A administration on the biodistribution and multipinhole muSPECT imaging of [123I]R91150 in rodent brain.
Blanckaert, P; Burvenich, I; De Bruyne, S; De Vos, F; Moerman, L; Staelens, S; Wyffels, L, 2009
)
0.35
" Ebastine provides efficacy throughout the 24-h dosing interval with once-daily administration and clinical benefit is seen from the first day of treatment."( Ebastine in allergic rhinitis and chronic idiopathic urticaria.
Sastre, J, 2008
)
0.35
" The present study directly addresses the hypothesis that MC4R activation may ameliorate ischemic brain injury by assessing the efficacy of a novel small molecule MC4R agonist RY767, administered in a pharmacokinetically guided and pharmacologically validated dosing regimen, in a rat stroke model of transient middle cerebral artery occlusion (tMCAO)."( Lack of protection with a novel, selective melanocortin receptor subtype-4 agonist RY767 in a rat transient middle cerebral artery occlusion stroke model.
Fong, T; Lynch, J; Nargund, R; Pollard, P; Regan, C; Reynolds, I; Shepherd, C; Strack, A; Weinberg, D; Ye, Z, 2009
)
0.35
" The dosage of the narcotic, changes of both blood pressure and heart rate during operation, before and after extubation and the pain degree, etc."( [Observation on therapeutic effect of compound anesthesia of transcutaneous electrical point stimulation and Remifentanil].
Hong, H; Ou, JY; Wang, WL; You, YY, 2008
)
0.35
"(1) The dosage of Isoflurane, (0."( [Observation on therapeutic effect of compound anesthesia of transcutaneous electrical point stimulation and Remifentanil].
Hong, H; Ou, JY; Wang, WL; You, YY, 2008
)
0.35
"Compound anesthesia of transcutaneous electrical point stimulation and Remifentanil can reduce the dosage of narcotics, shorten the time of palinesthesia and effectively prevent and treat acute pain after Remifentanil anesthesia."( [Observation on therapeutic effect of compound anesthesia of transcutaneous electrical point stimulation and Remifentanil].
Hong, H; Ou, JY; Wang, WL; You, YY, 2008
)
0.35
" Despite its utility, adverse effects may occur with high or prolonged propofol dosing regimens including delayed awakening."( Effects of dexmedetomidine on propofol and remifentanil infusion rates during total intravenous anesthesia for spine surgery in adolescents.
Anderson, J; Hoernschemeyer, DG; Ngwenyama, NE; Tobias, JD, 2008
)
0.35
"1 mg/kg) each shifted the dose-response curves of DOM, 2C-T-7, and DPT rightward in a parallel manner."( Discriminative stimulus effects of 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane in rhesus monkeys: antagonism and apparent pA2 analyses.
France, CP; Li, JX; Rice, KC, 2009
)
0.35
" Additionally, 57 inhibited the related receptor, VEGF receptor I (VEGFR-1), and showed excellent exposure when dosed orally to female CD-1 mice."( Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2.
Balagtas, C; Bohlen, P; Doody, JF; Duncton, MA; Hadari, YR; Katoch-Rouse, R; Kawakami, JK; Kiselyov, AS; Kussie, P; Milligan, DL; Mitelman, S; Patel, SN; Piatnitski Chekler, EL; Rolster, RL; Sherman, D; Smith, LM; Surguladze, D; Tonra, JR; Wang, Y; Wong, WC, 2009
)
0.35
", the compound consistently increased anxiety parameters in all of the three different anxiety tests applied, while a lower dosage of 1mg/kg had no such effect."( Modulation of anxiety by acute blockade and genetic deletion of the CB(1) cannabinoid receptor in mice together with biogenic amine changes in the forebrain.
Hasenöhrl, RU; Ledent, C; Molleman, A; Thiemann, G; Watt, CA, 2009
)
0.35
" INTERVENTION/PARTICIPANTS: A total of 395 men and women aged 65-84 yr were randomized for an intended 2 yr of treatment to four dosing groups (10 mg three times/week, 3 mg twice a day, 10 mg each night, and 10 mg twice a day) or placebo."( Effects of an oral growth hormone secretagogue in older adults.
Blackman, MR; Ettinger, MP; Hoffman, AR; Landschulz, W; Lyles, K; MacLean, D; Merriam, GR; Morey, MC; Petrie, CD; Salvatori, R; Taylor, A; Wei, JY; White, HK, 2009
)
0.35
" Tumor regression was observed following twice daily dosing of AT7519 in the HCT116 and HT29 colon cancer xenograft models."( Biological characterization of AT7519, a small-molecule inhibitor of cyclin-dependent kinases, in human tumor cell lines.
Cross, DM; Feltell, RE; Lewis, EJ; Lyons, JF; Smith, DM; Squires, MS; Thompson, NT; Wallis, NG, 2009
)
0.35
" An adaptive design was employed to concentrate dosage assignments at or near the MTD."( An adaptive first in man dose-escalation study of NGX267: statistical, clinical, and operational considerations.
Ivanova, A; Murphy, M, 2009
)
0.35
" Subsequently, the effects of a 1-week chronic daily dosing of DPP-IV inhibitors and sulfonylureas were investigated."( Antidiabetic effects of dipeptidyl peptidase-IV inhibitors and sulfonylureas in streptozotocin-nicotinamide-induced mildly diabetic mice.
Hayakawa, M; Matsuyama-Yokono, A; Nakano, R; Shibasaki, M; Shiraki, K; Someya, Y; Tahara, A, 2009
)
0.35
" MTEP also decreased cocaine self-administration without a clear graded dose-response profile and did not modify SCM-reinforced responding."( Dissociation of the effects of MTEP [3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]piperidine] on conditioned reinstatement and reinforcement: comparison between cocaine and a conventional reinforcer.
Baptista, MA; Dayas, CV; Martin-Fardon, R; Weiss, F, 2009
)
0.35
" Kestine in dosage of 10 mg a day was prescribed in duration of 10 days."( [Avene-50 and Ebastine in treatment and prevention of photodermatosis].
Dundua, MM; Tsiskarishvili, NI; Tsiskarishvili, NV, 2009
)
0.35
"), dose-dependently produced rightward shifts of the dose-response curve of Ro 64-6198-induced antinociception."( Behavioral effects of a synthetic agonist selective for nociceptin/orphanin FQ peptide receptors in monkeys.
Fantegrossi, WE; Galuska, CM; Ko, MC; Prinssen, EP; Wichmann, J; Woods, JH, 2009
)
0.35
" Further studies should address the optimization of dosing and lock out setting."( Remifentanil vs. meperidine for patient-controlled analgesia during colonoscopy: a randomized double-blind trial.
Agostoni, M; Alberto, TP; Antonio, F; Facciorusso, A; Fanti, L; Gambino, G; Gemma, M; Giorgio, T; Giulia, G; Guslandi, M; Marco, G; Mario, G; Massimo, A; Testoni, PA; Torri, G, 2009
)
0.35
" Intermittent dosing of lonafarnib (5 days on then 5 days off) coadministered with docetaxel produced similar regressions in hormone-refractory 22Rv1 tumors."( Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.
Bishop, WR; Hsieh, Y; Kirschmeier, P; Liu, G; Long, BJ; Marrinan, CH; Taylor, SA, 2009
)
0.35
"The efficacy of twice-daily dosing of a repaglinide/metformin FDC tablet was non-inferior to that of three-times-daily dosing."( Twice-daily and three-times-daily dosing of a repaglinide/metformin fixed-dose combination tablet provide similar glycaemic control.
Lewin, A; Lyness, W; Raskin, P; Reinhardt, R, 2009
)
0.35
" In an ex vivo occupancy assay, Compound A dosed orally to rats caused a concentration dependent inhibition of the specific binding of [(125)I]-S36057 to rat caudate putamen."( Localisation of melanin-concentrating hormone receptor 1 in rat brain and evidence that sleep parameters are not altered despite high central receptor occupancy.
Able, SL; Clarke, TL; Duckworth, JM; Fish, RL; Ivarsson, M; Katugampola, SD; McCourt, C; Napier, C, 2009
)
0.35
" Masitinib was administered orally to 43 patients who had inadequate response to DMARDs, at initial randomised dosing levels of 3 and 6 mg/kg per day over a 12-week period."( Masitinib in the treatment of active rheumatoid arthritis: results of a multicentre, open-label, dose-ranging, phase 2a study.
Bourgeois, P; Dubreuil, P; Flipo, RM; Gaudin, P; Gineste, P; Guy, L; Hermine, O; Le Loët, X; Mansfield, CD; Mariette, X; Moussy, A; Sibilia, J; Tebib, J, 2009
)
0.35
" The main metabolite detected in urine after intravenous dosing was characterized as a dihydrohydroxy S-mercapturic acid conjugate."( Metabolism-related liabilities of a potent histone deacetylase (HDAC) inhibitor and relevance of the route of administration on its metabolic fate.
Fiore, F; Fonsi, M; Jones, P; Kinzel, O; Laufer, R; Monteagudo, E; Rowley, M, 2009
)
0.35
" The recommended dosage of alvimopan is 12 mg administered with a sip of water 30 minutes to five hours before surgery, followed by 12 mg twice daily beginning the day after surgery for a maximum of seven days, 15 total doses, or until discharge."( Alvimopan for postoperative ileus.
Bream-Rouwenhorst, HR; Cantrell, MA, 2009
)
0.35
"This study in swine assessed BIS stability in response to decreases and increases in cardiac output under two propofol/remifentanil dosage combinations, both producing the same depth of surgical anaesthesia."( BIS response to tamponade and dobutamine in swine varies with hypnotic/opiate ratio.
Beydon, L; Cailleux, A; Chazot, T; Desfontis, JC; Dussaussoy, C; Ferec, S; Fischler, M; Ganster, F; Gautier, F; Gogny, M; Liu, N; Petres, J,
)
0.13
" In a nonrandomized, single-sequence study (study II), participants (n = 24 completed) received a single 5-mg dose of the sulfonylurea glyburide, alone and after 8 days of dosing with alogliptin 25 mg qd."( Coadministration of pioglitazone or glyburide and alogliptin: pharmacokinetic drug interaction assessment in healthy participants.
Fleck, P; Karim, A; Laurent, A; Mekki, Q; Munsaka, M; Wann, E, 2009
)
0.35
"00; the alvimopan cost at the upper limit of allowed dosing was $937."( Economic analysis of alvimopan in North American Phase III efficacy trials.
Bell, TJ; Delaney, CP; Kraft, MD; Poston, SA; Senagore, AJ; Techner, L, 2009
)
0.35
"There is preliminary evidence that concurrent administration of some antidepressant medications may be useful in the highly treatment resistant patient, though due attention should be given to potential risks in combining these with ECT; reduction of the treatment frequency to twice a week; hyperventilation prior to each treatment; and the use of remifentanil to minimise the dosage of induction anaesthetics with anticonvulsant properties, may be useful strategies to enhance seizure production in cases where a high or rapidly rising seizure threshold is a major impediment to ECT treatment."( The difficult-to-treat electroconvulsive therapy patient - Strategies for augmenting outcomes.
Kaill, A; Loo, CK; Paton, P; Simpson, B, 2010
)
0.36
"0 mg/kg doses, 30 min before testing produced anxiolytic-like effects in an increasing dose-response manner as measured by the percentage of open arm time and percentage of open arm entries."( Anxiolytic-like effects of the neurokinin 1 receptor antagonist GR-205171 in the elevated plus maze and contextual fear-potentiated startle model of anxiety in gerbils.
Corsi, M; Davis, M; Heldt, SA; Ratti, E; Ressler, KJ; Trist, D, 2009
)
0.35
"Pharmacokinetic studies in obese patients suggest that dosing of rocuronium should be based on ideal body weight (IBW)."( Should dosing of rocuronium in obese patients be based on ideal or corrected body weight?
Claudius, C; Jenstrup, MT; Lund, J; Meyhoff, CS; Rasmussen, LS; Sørensen, AM; Viby-Mogensen, J, 2009
)
0.35
"In obese patients undergoing gastric banding or gastric bypass, rocuronium dosed according to IBW provided a shorter duration of action without a significantly prolonged onset time or compromised conditions for tracheal intubation."( Should dosing of rocuronium in obese patients be based on ideal or corrected body weight?
Claudius, C; Jenstrup, MT; Lund, J; Meyhoff, CS; Rasmussen, LS; Sørensen, AM; Viby-Mogensen, J, 2009
)
0.35
" The buprenorphine-induced inverted U-shaped dose-response curve for antinociception may be due to NOP receptor activation, given that, in the presence of the NOP receptor antagonist, 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J113397), or in NOP receptor knockout mice, buprenorphine has a steeper dose-response curve and acts as a full agonist."( Nociceptin/orphanin FQ receptor activation attenuates antinociception induced by mixed nociceptin/orphanin FQ/mu-opioid receptor agonists.
Jiang, F; Khroyan, TV; Polgar, WE; Toll, L; Zaveri, NT, 2009
)
0.35
"Simple and rapid stability-indicating HPLC methods were developed for the individual analysis of aconitine (ACN) and piperine (PIN) in Mahamrutynjaya rasa, an herbal dosage form containing Aconitum ferox, Piper nigrum, and Piper longum in combination."( Stability-indicating reversed-phase liquid chromatographic methods for the determination of aconitine and piperine in a polyherbal formulation.
Pathak, A; Rai, P; Rajput, SJ,
)
0.13
" Patient's reaction score at laryngoscopy and an Observer's Assessment of Alertness/Sedation Scale (OAA/S) were used to determine whether the remifentanil dosage regimen was accepted."( Median effective dose of remifentanil for awake laryngoscopy and intubation.
Liao, X; Liu, Y; Luo, MP; Xu, YC; Xue, FS; Yang, QY; Zhang, YM, 2009
)
0.35
" In mouse models, following chronic treatment with delta9-tetrahydrocannabinol (THC), administration of the selective cannabinoid CB1 receptor antagonist SR141716 (rimonabant) elicited varying behavioral responses, depending on mouse strain and dosing regimen."( Hyperlocomotion and paw tremors are two highly quantifiable signs of SR141716-precipitated withdrawal from delta9-tetrahydrocannabinol in C57BL/6 mice.
Cowan, A; Huang, P; Liu-Chen, LY; Unterwald, EM, 2009
)
0.35
" The recommended dosage of 100 mg twice daily with food was well tolerated."( Phase I study of the safety, tolerability, and pharmacokinetics of oral CP-868,596, a highly specific platelet-derived growth factor receptor tyrosine kinase inhibitor in patients with advanced cancers.
Cohen, RB; Eder, JP; Guo, F; Lewis, LD; Lewis, NL; Olszanski, AJ; Pierce, KJ; Reddy, NJ, 2009
)
0.35
" Thus, a strong CYP2C8 inhibitory effect persisted even after gemfibrozil and gemfibrozil 1-O-beta-glucuronide concentrations had decreased to less than 1% of their maximum (24-h dosing interval)."( CYP2C8 activity recovers within 96 hours after gemfibrozil dosing: estimation of CYP2C8 half-life using repaglinide as an in vivo probe.
Backman, JT; Honkalammi, J; Kurkinen, KJ; Neuvonen, M; Neuvonen, PJ; Niemi, M; Tornio, A, 2009
)
0.35
" In initial phase I studies using a continuous infusion dosing schedule in a variety of malignancies, no clinical activity was observed."( Flavopiridol in chronic lymphocytic leukemia: a concise review.
Byrd, JC; Christian, BA; Grever, MR; Lin, TS, 2009
)
0.35
" A dose-response effect was observed for donepezil, with the highest-dose group at greatest risk (HR=2."( Cholinesterase inhibitors and incidence of bradycardia in patients with dementia in the veterans affairs new England healthcare system.
Cantor, MD; Farwell, W; Hernandez, RK; Lawler, EV, 2009
)
0.35
" An open-label, sequential drug interaction study was conducted in 45 participants who received twice-daily dosing of alvimopan with and without ciprofloxacin."( The effects of a short course of antibiotics on alvimopan and metabolite pharmacokinetics.
Ameen, V; Dukes, GE; Hewens, DA; Johnson, BM; Kelleher, DL; Schmith, VD; Vasist, LS; Young, MA, 2010
)
0.36
" 30 min prior to the acquisition trial of the NOR task animals were dosed with either vehicle, CX546 (10, 40 or 80 mg/kg) or CX516 (0."( Positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors reverses sub-chronic PCP-induced deficits in the novel object recognition task in rats.
Damgaard, T; Grayson, B; Hansen, SL; Larsen, DB; Neill, JC; Plath, N, 2010
)
0.36
" The antihistamine response after ebastine dosing would be decreased following rifampin pretreatments."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
0.36
"A PK/PD model was built that linked the dosing regimen of a compound to the inhibition of tumor growth in mouse xenograft models."( Preclinical pharmacokinetic/pharmacodynamic models to predict synergistic effects of co-administered anti-cancer agents.
Ashwell, S; Brassil, PJ; Dai, J; Garner, CE; Gönen, M; Goteti, K; Kern, SE; Moustakas, DT; Schwartz, GK; Utley, L; Zabludoff, S, 2010
)
0.36
" When Model II was applied to the antitumor activity of irinotecan and flavopiridol combination therapy, the modeling was able to reproduce the optimal dosing interval between administrations of the compounds."( Preclinical pharmacokinetic/pharmacodynamic models to predict synergistic effects of co-administered anti-cancer agents.
Ashwell, S; Brassil, PJ; Dai, J; Garner, CE; Gönen, M; Goteti, K; Kern, SE; Moustakas, DT; Schwartz, GK; Utley, L; Zabludoff, S, 2010
)
0.36
"05) tests as compared to those dosed with the vehicle."( Metabolic profiling of rat brain and cognitive behavioral tasks: potential complementary strategies in preclinical cognition enhancement research.
Atcha, Z; Aw, CC; Browne, ER; Chan, EC; Chen, WS; Goh, CW; Goh, DP; Neo, AH; New, LS, 2009
)
0.35
" For the second test, novel object recognition (NOR), a separate batch of rats, had the same sub-chronic PCP dosing regime and washout period."( Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms.
Arnt, J; Bang-Andersen, B; Brennum, LT; Grayson, B; Idris, N; Neill, J; Witten, LM, 2010
)
0.36
" In vivo binding studies showed that the dose-response relationship for sertindole in this study most closely correlates with affinity for 5-HT(6) receptor in vivo binding in striatum, although contribution from binding to 5-HT(2A) receptors in vivo in cortex may also provide an important mechanism."( Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms.
Arnt, J; Bang-Andersen, B; Brennum, LT; Grayson, B; Idris, N; Neill, J; Witten, LM, 2010
)
0.36
" Factors that may contribute to poor compliance and persistence with current osteoporosis therapies include drug intolerance, complexity of dosing regimens, and poor understanding of the relative benefit and risk with treatment."( Current and emerging pharmacologic therapies for the management of postmenopausal osteoporosis.
Lewiecki, EM, 2009
)
0.35
" The same sequence of experiments was repeated in the isolated heart model using the maximal protective dose of remifentanil from the dose-response studies."( Remifentanil post-conditioning attenuates cardiac ischemia-reperfusion injury via kappa or delta opioid receptor activation.
Irwin, MG; Jiang, LL; Li, R; Wong, GT, 2010
)
0.36
" Donepezil was orally given at a dosage of 5 mgxkg(-1)xday(-1)."( Anti-Alzheimer's drug, donepezil, markedly improves long-term survival after chronic heart failure in mice.
Ando, M; Arikawa, M; Handa, T; Kakinuma, Y; Katare, RG; Sasaguri, S; Sato, T; Yamasaki, F, 2009
)
0.35
"The every 2 week dosing is well tolerated with a phase II recommended dose of 45 mg/m of flavopiridol in combination with irinotecan (80 mg/m) and gemcitabine (800 mg/m)."( A phase I study of flavopiridol in combination with gemcitabine and irinotecan in patients with metastatic cancer.
Chyi Lee, F; Fekrazad, HM; Rabinowitz, I; Royce, M; Smith, HO; Verschraegen, CF, 2010
)
0.36
" After cerebral infarction, intravenous dosing of saline had no effect on these parameters."( Ameliorating effects of cloperastine on dysfunction of the urinary bladder caused by cerebral infarction in conscious rats.
Shirasaki, T; Soeda, F; Takahama, K; Yamamoto, G, 2009
)
0.35
" The dose-response curve for ET-1 was shifted to the left in the diabetics, so that at some lower doses of ET-1 the vasoconstriction was greater than in the controls."( Diabetes-associated changes and role of N epsilon-(carboxymethyl)lysine in big ET-1-induced coronary vasoconstriction.
Kamata, K; Kobayashi, T; Matsumoto, T; Ozawa, Y; Taguchi, K, 2010
)
0.36
" The results showed that piperine at all dosage range used in this study significantly improved memory impairment and neurodegeneration in hippocampus."( Piperine, the main alkaloid of Thai black pepper, protects against neurodegeneration and cognitive impairment in animal model of cognitive deficit like condition of Alzheimer's disease.
Chonpathompikunlert, P; Muchimapura, S; Wattanathorn, J, 2010
)
0.36
"Streptozotocin-induced diabetic mice were treated with N-(piperidin-1-yl)-5-(4-iodophenyl)-1-(2,3-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (AM251), a selective CB1-receptor antagonist, at the dosage of 1 mg x kg(-1) x day(-1) via intraperitoneal injection for 14 weeks."( Cannabinoid receptor 1 blockade ameliorates albuminuria in experimental diabetic nephropathy.
Barutta, F; Corbelli, A; Di Marzo, V; Gambino, R; Gruden, G; Mastrocola, R; Perin, PC; Pinach, S; Rastaldi, MP, 2010
)
0.36
" The results were tested against the concentration addition reference model using dose-response surface analyses."( Pesticide cocktails can interact synergistically on aquatic crustaceans.
Cedergreen, N; Nørgaard, KB, 2010
)
0.36
"The results of the binary dose-response surface studies showed that mixtures with prochloraz increased toxicity up to 12-fold compared with what was expected using the reference model concentration addition (CA)."( Pesticide cocktails can interact synergistically on aquatic crustaceans.
Cedergreen, N; Nørgaard, KB, 2010
)
0.36
"The time and the dosage of etomidate necessary to loss consciousness were greater in group F ((70."( Peri-intubation hemodynamic changes during low dose fentanyl, remifentanil and sufentanil combined with etomidate for anesthetic induction.
Sun, L; Zhang, GH, 2009
)
0.35
" Intravenous atropine could prevent a fall in HR, but not a fall in BP, during induction of intravenous anesthesia with propofol and remifentanil of our dosing regimen."( Can intravenous atropine prevent bradycardia and hypotension during induction of total intravenous anesthesia with propofol and remifentanil?
Ariyama, J; Hayashida, M; Kitamura, A; Maruyama, K; Nakagawa, H; Nishikawa, Y, 2010
)
0.36
" Dose-response studies of G-1 vs 17beta-estradiol in isolated islets at 1 or 12 mM glucose showed an almost identical pattern in that both compounds increased insulin and inhibited glucagon and somatostatin secretion."( Activation of G protein-coupled receptor 30 modulates hormone secretion and counteracts cytokine-induced apoptosis in pancreatic islets of female mice.
Amisten, S; Balhuizen, A; Kumar, R; Lundquist, I; Salehi, A, 2010
)
0.36
"Combinations of non-steroidal anti-inflammatory drugs (NSAIDs) and cannabinoids are promising because of their potential synergistic effects in analgesia, resulting in a reduction in dosage and minimizing adverse reactions."( The antinociceptive effect of acetylsalicylic acid is differently affected by a CB1 agonist or antagonist and involves the serotonergic system in rats.
Filaferro, M; Frigeri, C; Pini, LA; Ruggieri, V; Sandrini, M; Vitale, G, 2010
)
0.36
" Monkeys were dosed orally with either vehicle (n = 7) or CP-900691 (3 mg/kg, n = 7) daily for 6 weeks."( A selective peroxisome proliferator-activated receptor alpha agonist, CP-900691, improves plasma lipids, lipoproteins, and glycemic control in diabetic monkeys.
Auerbach, BJ; Francone, OL; Harwood, HJ; Kavanagh, K; Royer, LJ; Shadoan, MK; Wagner, JD; Ward, GM; Zhang, L, 2010
)
0.36
" This discrepancy may be explained by the subtherapeutic dosage used in the pharmacokinetic study."( Symptomatic hypoglycemia associated with trimethoprim/sulfamethoxazole and repaglinide in a diabetic patient.
Blondel, E; Fonrose, X; Mallaret, MP; Roustit, M; Villier, C, 2010
)
0.36
" Further trials are required to evaluate ideal dosing regimens and combinations of agents for use with remifentanil in neonates."( Remifentanil for endotracheal intubation in neonates: a randomised controlled trial.
AlFaleh, K; Choong, K; Doucette, J; Gray, S; Paes, B; Rich, B; Verhey, L, 2010
)
0.36
" FAAH(-/-) mice dosed subchronically with equi-active maximally effective doses of AEA or THC displayed greater rightward shifts in THC dose-effect curves for antinociception, catalepsy, and hypothermia than in AEA dose-effect curves."( FAAH-/- mice display differential tolerance, dependence, and cannabinoid receptor adaptation after delta 9-tetrahydrocannabinol and anandamide administration.
Abdullah, RA; Cravatt, BF; Falenski, KW; Lichtman, AH; Schlosburg, JE; Selley, DE; Sim-Selley, LJ; Smith, TH; Thorpe, AJ, 2010
)
0.36
" The incidence of extrapyramidal symptoms appears to be low across all dosage ranges; however, akathisia may be more frequent with higher doses."( Iloperidone for the treatment of schizophrenia.
Caballero, J; Marino, J, 2010
)
0.36
" We reviewed our experience to determine the dose-response relationship and apparent perioperative safety profile of adenosine in intracranial aneurysm patients."( Adenosine-induced flow arrest to facilitate intracranial aneurysm clip ligation: dose-response data and safety profile.
Avram, MJ; Batjer, HH; Bebawy, JF; Bendok, BR; Gupta, DK; Hemmer, LB; Koht, A; Zeeni, C, 2010
)
0.36
"The aim of the present study was to determine the dosage of remifentanil that must be added to thiopental 5 mg kg(-1) to provide excellent intubating conditions in 95% of patients."( What is the optimal remifentanil dosage for providing excellent intubating conditions when coadministered with thiopental? A prospective randomized dose-response study.
Allaouchiche, B; Boselli, E; Bouvet, L; Chassard, D; Rousson, D; Stoian, A, 2010
)
0.36
"The dosage of remifentanil providing excellent intubating conditions in 95% of patients when coadministered with thiopental 5 mg kg(-1) in healthy premedicated female patients undergoing elective surgery was more than 7 microg kg(-1)."( What is the optimal remifentanil dosage for providing excellent intubating conditions when coadministered with thiopental? A prospective randomized dose-response study.
Allaouchiche, B; Boselli, E; Bouvet, L; Chassard, D; Rousson, D; Stoian, A, 2010
)
0.36
" V concentrations higher than previously reported with oral dosing were achieved."( A phase I pharmacokinetic study of pulse-dose vorinostat with flavopiridol in solid tumors.
Ames, MM; Cane, LM; Carvajal, RD; Dials, HJ; Dickson, MA; Gonen, M; Grant, S; Lefkowitz, RA; McGovern, RM; Rathkopf, DE; Reid, JM; Roberts, JD; Schwartz, GK, 2011
)
0.37
"Ratios and 90% confidence intervals of the geometric means compared with the fasting condition indicated that the maximum concentrations of blonanserin (C(max)) significantly increased with dosing 30 min before meal intake, and 30 min and 2 and 4 h after meal intake, yielding by 330%, 239%, 272%, and 138%, respectively."( Effect of dose timing in relation to food intake on systemic exposure to blonanserin.
Inoue, Y; Kaneko, S; Saruwatari, J; Yasui-Furukori, N, 2010
)
0.36
" The marked effect of food on the bioavailability of blonanserin should be taken into account in its dosing schedules."( Effect of dose timing in relation to food intake on systemic exposure to blonanserin.
Inoue, Y; Kaneko, S; Saruwatari, J; Yasui-Furukori, N, 2010
)
0.36
" Repeated (3 days) daily dosing of ABT-107 increased extracellular cortical acetylcholine in rats, whereas acute administration increased cortical extracellular signal-regulated kinase and cAMP response element-binding protein phosphorylation in mice, neurochemical and biochemical events germane to cognitive function."( In vivo pharmacological characterization of a novel selective alpha7 neuronal nicotinic acetylcholine receptor agonist ABT-107: preclinical considerations in Alzheimer's disease.
Anderson, DJ; Bitner, RS; Browman, K; Buccafusco, J; Bunnelle, WH; Decker, MW; Drescher, KU; Gopalakrishnan, M; Kohlhaas, KL; Markosyan, S; Marsh, KC; Nikkel, AL; Radek, R, 2010
)
0.36
" The aim of this study was to assess an alternative oral dosing method that could reduce the distress and morbidity associated with standard gavage techniques."( Alternative method of oral dosing for rats.
Atcha, Z; Aw, CC; Browne, ER; Goh, CW; Lim, JS; Neo, AH; Pemberton, DJ; Rourke, C, 2010
)
0.36
"With the objective to achieve prolonged drug release, especially for the treatment of diabetes mellitus, and thereby to reduce the side effects of administration of conventional dosage form, repaglinide loaded PMMA nanoparticles have been formulated."( In vitro characterization and invivo toxicity study of repaglinide loaded poly (methyl methacrylate) nanoparticles.
Dhana Lekshmi, UM; Kishore, N; Poovi, G; Reddy, PN, 2010
)
0.36
"A simple RP-HPLC method was developed and validated for the determination of rimonabant in a pharmaceutical dosage form."( Validated stability-indicating RP-HPLC method for the determination of rimonabant in a pharmaceutical dosage form.
Arend, MZ; Dalmora, SL; Hurtado, FK; Ravanello, A; Rolim, CM; Wrasse, M,
)
0.13
" In the present study, 9 dogs were treated with a single dose of the γ-secretase modulator E2012, the γ-secretase inhibitor LY450139, or vehicle with a dosing interval of 1 week."( Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.
Andreasson, U; Blennow, K; Borghys, H; Gustavsson, MK; Mercken, M; Portelius, E; Van Broeck, B; Zetterberg, H, 2010
)
0.36
"5% bepotastine besilate at 15 minutes and 8 hours after dosing for CAC-induced nasal congestion, rhinorrhea, ear or palate pruritus, nasal pruritus, and summed nonocular composite symptom (NOCS) scores and also at 16 hours after dosing for nasal congestion and rhinorrhea."( Bepotastine besilate ophthalmic solution for the relief of nonocular symptoms provoked by conjunctival allergen challenge.
Abelson, MB; Gomes, PJ; Gow, JA; McNamara, TR; Torkildsen, GL; Williams, JI, 2010
)
0.36
" Dependence was established using a noncontingent morphine dosing procedure that has been previously verified to maintain dependence while allowing for daily behavioral observation during a withdrawn state."( Reinforcer-dependent enhancement of operant responding in opioid-withdrawn rats.
Cooper, ZD; Shi, YG; Woods, JH, 2010
)
0.36
"Morphine withdrawal enhanced remifentanil self-administration, resulting in an upward and rightward shift of the descending limb of the dose-response curve, and increased operant responding for both food reinforcers."( Reinforcer-dependent enhancement of operant responding in opioid-withdrawn rats.
Cooper, ZD; Shi, YG; Woods, JH, 2010
)
0.36
" For 10 mg and 5 mg donepezil once-daily dosing, the estimated forgiveness of donepezil was 80% and 90% daily compliance or two and one dosage omissions at steady state, respectively."( Compliance assessment of ambulatory Alzheimer patients to aid therapeutic decisions by healthcare professionals.
Freiberg, I; Kloft, C; Scheerans, C; Schmidt-Pokrzywniak, A; Schwalbe, O; Stang, A, 2010
)
0.36
" The effect of tipepidine was significant even at a dosage as small as 5 mg/kg."( The potent inhibitory effect of tipepidine on marble-burying behavior in mice.
Honda, S; Kawaura, K; Shirasaki, T; Soeda, F; Takahama, K, 2011
)
0.37
" No increase in lipolytic activity was found after 3 weeks of repeated dosing as measured by microdialysis in adipose tissue whereas acute administration of 10mg/kg produced a significant increase in microdialysate levels of glycerol illustrating an acute stimulation of lipolysis."( Effect of the cannabinoid receptor-1 antagonist rimonabant on lipolysis in rats.
Hansen, HS; Johansen, T; Malmlöf, K; Mølhøj, S; Schweiger, M; Zimmermann, R, 2010
)
0.36
" Following oral dosing the tested drug absorbed with t(½ab) of 41."( Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone.
Amer, AM; Atef, M; El-Gendi, AY; Kamel, GM, 2010
)
0.36
" The time to loss of consciousness (LOC), intubation time, intubation score, anesthetic dosage and adverse effects were recorded."( [Comparison of sevoflurane and propofol in combined anesthesia induction with remifentanil for tracheal intubation with fiberoptic bronchoscope].
Cao, LH; Huang, W; Lin, WQ; Tan, HY; Zeng, WA; Zhong, ZJ, 2010
)
0.36
" A cautious dosing and titration schedule is recommended at the initiation of therapy due to the potential for orthostatic hypotension and dizziness."( Iloperidone for the treatment of schizophrenia.
Bishop, DL; Bishop, JR, 2010
)
0.36
" The dosage of ChEI treatment could possibly lead to a different functional outcome."( Long-term outcome and prediction models of activities of daily living in Alzheimer disease with cholinesterase inhibitor treatment.
Londos, E; Minthon, L; Wallin, ÅK; Wattmo, C,
)
0.13
" Tests assessed the dose-response functions of ∆⁹-THC and the time course for rimonabant in its ability to block the discriminative stimulus effects of ∆⁹-THC."( Antagonism of ∆⁹-THC induced behavioral effects by rimonabant: time course studies in rats.
Gifford, RS; Järbe, TU; Makriyannis, A, 2010
)
0.36
" The effects of the phenethylamine hallucinogen R(-)-2,5-dimethoxy-4-iodoamphetamine (DOI) on head-twitch behavior were studied over a range of doses in the mouse, generating a characteristic biphasic dose-response curve."( Interaction of 5-HT2A and 5-HT2C receptors in R(-)-2,5-dimethoxy-4-iodoamphetamine-elicited head twitch behavior in mice.
Cohen, MS; Fantegrossi, WE; Henson, CM; Rice, KC; Simoneau, J; Woods, JH; Zimmerman, SM, 2010
)
0.36
" Surface-modified NPs could be used to improve patient compliance with drug treatment as a result of decreased dosing frequency."( Repaglinide-loaded long-circulating biodegradable nanoparticles: rational approach for the management of type 2 diabetes mellitus.
Jain, S; Saraf, S, 2009
)
0.35
"Based on the promising activity and tolerability of flavopiridol administered with a pharmacokinetically-derived dosing schedule in chronic lymphocytic leukemia (CLL), we conducted a phase I study using this schedule in patients with advanced solid tumors."( A dose-finding, pharmacokinetic and pharmacodynamic study of a novel schedule of flavopiridol in patients with advanced solid tumors.
Arbogast, D; Baiocchi, R; Bekaii-Saab, T; Byrd, JC; Campbell, A; Doyle, A; Grever, MR; Lai, JP; Lustberg, ME; Ni, W; Phelps, MA; Ramaswamy, B; Shah, MH; Wei, L; Wilkins, D; Wolfson, A, 2012
)
0.38
" Flavopiridol PK was notably different, and there was a higher frequency of CKRS, despite prophylactic steroids, seen in this patient group compared to previous studies with CLL using a similar dosing schedule."( A dose-finding, pharmacokinetic and pharmacodynamic study of a novel schedule of flavopiridol in patients with advanced solid tumors.
Arbogast, D; Baiocchi, R; Bekaii-Saab, T; Byrd, JC; Campbell, A; Doyle, A; Grever, MR; Lai, JP; Lustberg, ME; Ni, W; Phelps, MA; Ramaswamy, B; Shah, MH; Wei, L; Wilkins, D; Wolfson, A, 2012
)
0.38
" This case series aimed to examine whether the aggressive dosing of remifentanil, exerting both depressor and bradycardic actions with short durations, is applicable for hemodynamic control during pheochromocytoma resection."( [Successful anesthetic management of three patients receiving pheochromocytoma resection using extremely high-dose remifentanil infusion].
Masuda, R; Serada, K; Shimoyama, Y; Suzuki, T, 2010
)
0.36
" Each patient received single-dose administration on day 1, cycle 1 then switched to a twice daily (BID) dosing regimen on days 2-14 of a 28-day cycle; subsequent cycles continued BID dosing on days 1-14."( Phase I and pharmacokinetic study of lonafarnib, SCH 66336, using a 2-week on, 2-week off schedule in patients with advanced solid tumors.
Castaneda, C; Cutler, DL; Hurwitz, HI; Kaufmann, SH; Meadows, KL; Morse, MA; Petros, WP; Statkevich, P; Truax, R; Zhu, Y, 2011
)
0.37
"The MTD and recommended phase II dose is 200 mg BID on days 1-14 of a 28-day dosing regimen."( Phase I and pharmacokinetic study of lonafarnib, SCH 66336, using a 2-week on, 2-week off schedule in patients with advanced solid tumors.
Castaneda, C; Cutler, DL; Hurwitz, HI; Kaufmann, SH; Meadows, KL; Morse, MA; Petros, WP; Statkevich, P; Truax, R; Zhu, Y, 2011
)
0.37
" The distribution and metabolism of casopitant were studied in both species evaluating the accumulation of drug-related material (DRM) after repeat dosing and its potential relationship with pathological findings observed in myocardium."( Tissue distribution and characterization of drug-related material in rats and dogs after repeated oral administration of casopitant.
Bordini, E; Cufari, D; Ferrari, L; Martinucci, S; Miraglia, L; Pagliarusco, S; Pellegatti, M, 2011
)
0.37
"time to peak plasma concentration occurs in 2 - 4 h but elimination half-life is 18 h for extensive CYP2D6 metabolizers and 33 h for poor CYP2D6 metabolizers, suggesting that once or twice daily dosing would be feasible."( Iloperidone: chemistry, pharmacodynamics, pharmacokinetics and metabolism, clinical efficacy, safety and tolerability, regulatory affairs, and an opinion.
Citrome, L, 2010
)
0.36
" A limiting factor in its drug development has been the high dosage required in human clinical trials."( The binding of flavopiridol to blood serum albumin.
Baumli, S; Johnson, L; Myatt, D; Siligardi, G, 2010
)
0.36
" When administered with a pharmacokinetically (PK)-directed dosing schedule, flavopiridol exhibited striking activity in patients with refractory chronic lymphocytic leukemia."( Flavopiridol pharmacogenetics: clinical and functional evidence for the role of SLCO1B1/OATP1B1 in flavopiridol disposition.
Ahn, S; Byrd, JC; Dai, Z; Dalton, JT; Farley, KL; Grever, MR; Jarjoura, D; Ji, J; Johnson, AJ; Li, X; Lin, TS; Ni, W; Papp, A; Phelps, MA; Sadee, W, 2010
)
0.36
" Blood samples were collected at the end of the dosing period for reproductive hormone analysis."( Effects of an antagonist of neurokinin receptors 1, 2 and 3 on reproductive hormones in male beagle dogs.
Enright, BP; LaBrie, F; Leach, MW; Losco, PE; McIntyre, BS; Pelletier, G, 2010
)
0.36
" A higher oral dosage was suggested to have a better therapeutic response in reported results, but the plasma concentration of donepezil was not examined with respect to the therapeutic outcomes in those studies."( Plasma concentration of donepezil to the therapeutic response of Alzheimer's disease in Taiwanese.
Chen, SH; Chou, MC; Lai, CL; Liu, CK; Wu, SL; Yang, YH, 2011
)
0.37
"there was no significant cell-killing effects or apoptosis in AO cells following treatments with AdHTVP2G5-rev-casp3 or flavopiridol at low dosage alone (apoptotic rate all < 11%), whereas significant synergism of their sequential combination was observed in AO cells."( [Synergism of antitumor effects on ovarian carcinoma using autocatalytic caspase-3 combined with flavopiridol].
Shen, K; Song, Y; Xu, F, 2010
)
0.36
" Pharmacokinetics demonstrated a dose-response for total and unbound plasma flavopiridol unrelated to total protein, albumin, peripheral blast count, or toxicity."( Phase 1 and pharmacokinetic study of bolus-infusion flavopiridol followed by cytosine arabinoside and mitoxantrone for acute leukemias.
Alino, K; Bagain, L; Blackford, A; Briel, J; Carraway, H; Doyle, LA; Gore, SD; Greer, JM; Joseph, B; Karp, JE; Levis, MJ; Mackey, K; McDevitt, MA; Moton-Nelson, D; Resar, LS; Rudek, MA; Smith, BD; Wright, JJ; Zhao, M, 2011
)
0.37
" The mean pain and pain relief scores were similar during the two different dosing regimens."( Timing of intravenous patient-controlled remifentanil bolus during early labour.
Akural, EI; Alahuhta, S; Ohtonen, P; Ranta, P; Raudaskoski, T; Tekay, A; Volmanen, PV, 2011
)
0.37
" Iloperidone has established tolerability at recommended dosages of up to 24 mg daily; however, the dosage must be slowly increased over seven days, and twice-daily administration is required to avoid orthostatic hypotension."( Iloperidone: A new drug for the treatment of schizophrenia.
Arif, SA; Mitchell, MM, 2011
)
0.37
" The IC(50) value of SB-612111 estimated from dose-response curves is 87."( Quantitative study of the antagonistic effect of (-)-cis-1-Methyl-7-[[4-(2,6-dichlorophenyl)piperidin-1-yl]methyl]-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111) on nociceptin/orphanin FQ-mediated potassium channel activation in rat periaqueducta
Chiou, LC; Jiang, F; Liao, YY, 2011
)
0.37
" Patients were randomized to 1 of 4 dosing cohorts: 1) 30 mg/m², 100 mg; 2) 36 mg/m², 100 mg; 3) 30 mg/m², 150 mg; or 4) 36 mg/m², 150 mg of DTX intravenously weekly, LNF orally twice daily, respectively."( Farnesyl transferase expression determines clinical response to the docetaxel-lonafarnib combination in patients with advanced malignancies.
Bender, L; Chanel-Vos, C; Escuin, D; Fanucchi, MP; Gal, A; Giannakakou, P; Harvey, RD; Kauh, J; Khuri, FR; Kutner, M; Marcus, A; Pan, L; Ramalingam, SS; Saba, N; Shin, DM, 2011
)
0.37
" When it was administered with cocaine, AC927 shifted the cocaine dose-response curve to the left, suggesting an enhancement of the discriminative stimulus effects of cocaine."( Effects of the selective sigma receptor ligand, 1-(2-phenethyl)piperidine oxalate (AC927), on the behavioral and toxic effects of cocaine.
Coop, A; Fantegrossi, WE; Katz, JL; Li, SM; Matsumoto, RR, 2011
)
0.37
"The aim of this study was to assess human striatal dopamine receptor 2 (D(2)) and cortical 5-hydroxytryptamine receptor 2A (5-HT(2A)) occupancy of SB-773812 to demonstrate brain penetration and binding to the target receptors and assess the pharmacokinetics-receptor occupancy relationship over time to aid dose selection and dosage regimen, in preparation for the phase II trials."( Contribution of SPECT measurements of D2 and 5-HT2A occupancy to the clinical development of the antipsychotic SB-773812.
Bullich, S; Burgess, C; Catafau, AM; Gray, F; Merlo-Pich, E; Nucci, G, 2011
)
0.37
" In patients with schizophrenia, D(2) occupancy levels induced by a single dose were maintained over time, indicating that once-daily dosing regimens are appropriate."( Contribution of SPECT measurements of D2 and 5-HT2A occupancy to the clinical development of the antipsychotic SB-773812.
Bullich, S; Burgess, C; Catafau, AM; Gray, F; Merlo-Pich, E; Nucci, G, 2011
)
0.37
" Both of the formulations were administered orally as a single dose with a 45-day washout period between two dosing sessions."( Bioequivalence study of two tablet formulations containing rimonabant 20 mg in healthy Indian subjects.
Bhaumik, U; Chakrabarty, US; Das, A; Nandi, U; Pal, TK, 2011
)
0.37
", dose, dosing regimen, genetic variation and species)."( The effects of black pepper on the intestinal absorption and hepatic metabolism of drugs.
Han, HK, 2011
)
0.37
" Iloperidone and asenapine are dosed twice daily, in contrast to lurasidone, which is dosed once daily with food."( Iloperidone, asenapine, and lurasidone: a brief overview of 3 new second-generation antipsychotics.
Citrome, L, 2011
)
0.37
"05-10 μg/mouse) produced antidepressant-like effect dose-dependently, whereas influenced the MBB in a biphasic manner (produced a U-shaped dose-response curve)."( Involvement of endocannabinoids in antidepressant and anti-compulsive effect of fluoxetine in mice.
Jain, NS; Manna, SS; Umathe, SN, 2011
)
0.37
" The initial cohort was dosed at 100 mg every other day."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
" Prescribing information recommends a starting dosage of 1 mg twice daily and then titrated over 7 days to reach a target dosage of 12 to 24 mg/d."( Iloperidone for the management of adults with schizophrenia.
Crabtree, BL; Montgomery, J, 2011
)
0.37
" Slow initial titration and twice-daily dosing are potential disadvantages."( Iloperidone for the management of adults with schizophrenia.
Crabtree, BL; Montgomery, J, 2011
)
0.37
"5% compared with placebo for the treatment of ocular itching and conjunctival hyperemia (redness) using the conjunctival allergen challenge (CAC) model of allergic conjunctivitis when dosed 16 h before a CAC test."( Prolonged effectiveness of bepotastine besilate ophthalmic solution for the treatment of ocular symptoms of allergic conjunctivitis.
Abelson, MB; Gomes, PJ; Gow, JA; Kennedy, KS; McNamara, TR; Torkildsen, GL; Williams, JI, 2011
)
0.37
" Eligible subjects (n=107) aged 10 years and older with a history of allergic conjunctivitis who had a reproducible positive reaction to a CAC were enrolled and dosed with test agent."( Prolonged effectiveness of bepotastine besilate ophthalmic solution for the treatment of ocular symptoms of allergic conjunctivitis.
Abelson, MB; Gomes, PJ; Gow, JA; Kennedy, KS; McNamara, TR; Torkildsen, GL; Williams, JI, 2011
)
0.37
"0 mg of remifentanil during a 50-minute surgical procedure as a result of a dosage miscalculation."( Delayed awakening following inadvertent high-dose remifentanil infusion in a 13 year old patient.
Barak, M; Danino, J; Greenberg, Z, 2011
)
0.37
" Broad variability in study design, selection and dosing of anesthetics, electrode placement, and limited examination of potentially relevant variables such as age, sex, concomitant medications; and stimulus parameters attenuate the certainty of these results."( Remifentanil: a review of its use in electroconvulsive therapy.
Chen, ST, 2011
)
0.37
" Patients had an option to continue in a 40-week, open-label extension study, with those originally randomized to alogliptin remaining on the same dosage regimen while patients treated with placebo were randomly allocated to alogliptin 12."( Efficacy and safety of alogliptin added to pioglitazone in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label long-term extension study.
Hirayama, M; Hiroi, S; Itayasu, T; Kaku, K; Seino, Y, 2011
)
0.37
" The antiemetic dose-response curves of tropisetron against both emetogens were U-shaped probably because larger doses of this antagonist behave as a partial agonist."( Synergistic antiemetic interactions between serotonergic 5-HT3 and tachykininergic NK1-receptor antagonists in the least shrew (Cryptotis parva).
Alkam, T; Amos, B; Chebolu, S; Darmani, NA, 2011
)
0.37
"A Bayesian nonlinear longitudinal Emax model for a binary endpoint was used to characterize the dose-response relationship for a new treatment of rheumatoid arthritis."( A case study of model-based Bayesian dose response estimation.
French, J; Gruben, D; Tan, H; Thomas, N, 2011
)
0.37
" Chronic treatment with the CB1 receptor antagonist SR141716 (5 daily dosing of 30mg/kg) did not change innate resistance to audiogenic seizures in non-epileptic rats but reverted acquired seizure resistance in rats which lost their epileptic sensitivity with repeated testing."( Pro-epileptic effects of the cannabinoid receptor antagonist SR141716 in a model of audiogenic epilepsy.
Shatskova, AB; van Rijn, CM; Vinogradova, LV, 2011
)
0.37
"We conducted a phase I clinical trial of the combination of SCH 66336 with temozolomide administered on the standard 5-day dosing schedule."( A phase I trial of the farnesyl transferase inhibitor, SCH 66336, with temozolomide for patients with malignant glioma.
Coan, AD; Desjardins, A; Friedman, AH; Friedman, HS; Herndon, JE; Peters, KB; Reardon, DA; Threatt, S; Vredenburgh, JJ, 2011
)
0.37
"0]hexane-4,6-dicarboxylic acid (LY379268) (0-3 mg/kg, subcutaneously) prevented cocaine seeking induced by footshock stress following the same dose-response function."( (-)-2-oxa-4-aminobicylco[3.1.0]hexane-4,6-dicarboxylic acid (LY379268) and 3-[(2-methyl-1,3-thiazol-4-yl)ethynyl]piperidine (MTEP) similarly attenuate stress-induced reinstatement of cocaine seeking.
Martin-Fardon, R; Weiss, F, 2012
)
0.38
" Four of eight participants receiving rimonabant (none of two receiving placebo) had greater cortisol concentrations 2 hours after dosing (at 11:30) than at 08:00, while normal diurnal variation should have peak concentrations at 08:00."( CB1 - cannabinoid receptor antagonist effects on cortisol in cannabis-dependent men.
Baumann, MH; Bonnet, D; Darwin, WD; Goodwin, RS; Gorelick, DA; Huestis, MA; Kelly, DL; Ortemann-Renon, C; Schroeder, JR; Schwilke, E; Schwope, DM, 2012
)
0.38
"In view of its favorable pharmacological and clinical characteristics, bilastine is likely to have particular benefit in urticaria for which guidelines recommend increasing the dosage of H(1)-antihistamines up to fourfold if standard dosing is ineffective."( Safety and efficacy of bilastine: a new H(1)-antihistamine for the treatment of allergic rhinoconjunctivitis and urticaria.
Church, MK, 2011
)
0.37
" Sigmoidal dose-response curves were plotted and IC(50) values were estimated."( In vitro and in situ evaluation of herb-drug interactions during intestinal metabolism and absorption of baicalein.
Fong, YK; Li, CR; Lin, G; Wang, S; Wo, SK; Zhang, L; Zhou, L; Zuo, Z, 2012
)
0.38
" Oral administration of IAC dosed at 50 and 100 mg/kg was able to significantly prevent gastric ulceration induced by indomethacin and by stress."( Further evidence of the antiulcer activity of IAC, a novel free radical scavenger.
Baraldi, M; Carnevale, G; Zanoli, P; Zavatti, M, 2011
)
0.37
" Experiment 1 tested the effects of 5 mg/per day dosage on cognitive and EEG markers at 6-hour, 2-week and 4-week follow-ups."( Donepezil impairs memory in healthy older subjects: behavioural, EEG and simultaneous EEG/fMRI biomarkers.
Balsters, JH; Bokde, AL; Brennan, S; Cassidy, SM; Delmonte, S; Fagan, AJ; Galli, A; Kilcullen, SM; Lai, R; Laruelle, M; Lawlor, B; Martin, MP; Meaney, JF; O'Connell, RG; Robertson, IH; Upton, N, 2011
)
0.37
" Dosed alone, compound 64 suppressed extinction of conditioned freezing (10 mg/kg) and rapid eye movement (REM) sleep (30 mg/kg), consistent with previous reports for rimonabant, although for REM sleep, compound 64 was greater than threefold less potent than for metabolic effects."( Characterization of a novel, brain-penetrating CB1 receptor inverse agonist: metabolic profile in diet-induced obese models and aspects of central activity.
Chaperon, F; Chen, YA; Commerford, SR; Dardik, B; Gerber, SP; Gromada, J; He, X; Hollenbeck, T; Jacobson, LH; Jaton, AL; Liu, H; McNamara, P; Nguyen-Tran, V; Schwartzkopf, C; Seidel, HM; Teixeira, S, 2011
)
0.37
" There were no significant differences between the extrapleural and epidural block groups with regard to VAS at rest and during movement assessed at 4, 12, 24, 36, and 48 hours after surgery, dosage of intravenous morphine (extrapleural: 12."( Comparison of the analgesic effects of continuous extrapleural block and continuous epidural block after video-assisted thoracoscopic surgery.
Endo, S; Endo, T; Hotta, K; Inoue, S; Sata, N; Seo, N; Taira, K; Takeuchi, M, 2011
)
0.37
" Change of LTP by donepezil treatment had a bell-shaped dose-response curve."( Donepezil in a narrow concentration range augments control and impaired by beta-amyloid peptide hippocampal LTP in NMDAR-independent manner.
Bukanova, JV; Kapai, NA; Skrebitsky, VG; Solntseva, EI, 2012
)
0.38
" If an increase in thermal threshold was found, naltrexone administration was repeated at decreasing intervals in the next experiment (all cats were not used for all dosing intervals)."( Use of naltrexone to antagonize high doses of remifentanil in cats: a dose-finding study.
Brosnan, RJ; Ilkiw, JE; Pypendop, BH, 2011
)
0.37
" Venous blood samples were taken prior to and following oral dosing up to 24 h for a pharmacokinetic study of casopitant concentration in plasma."( A pharmacokinetic PET study of NK₁ receptor occupancy.
Bani, M; Cunningham, VJ; Fernandes, SA; Gomeni, R; Gunn, RN; Rabiner, EA; Ratti, E; Zamuner, S, 2012
)
0.38
" All patients continued to receive a stable dosage of MTX."( A phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) versus placebo in combination with background methotrexate in patients with active rheumatoid arthritis and an inadequate response to methotrexate alone.
Cohen, S; Connell, CA; French, JL; Gomez-Reino, J; Gruben, D; Kanik, KS; Kremer, JM; Krishnaswami, S; Pascual-Ramos, V; Wallenstein, G; Wilkinson, BE; Zwillich, SH, 2012
)
0.38
"In patients with active RA in whom the response to MTX has been inadequate, the addition of tofacitinib at a dosage ≥3 mg twice daily showed sustained efficacy and a manageable safety profile over 24 weeks."( A phase IIb dose-ranging study of the oral JAK inhibitor tofacitinib (CP-690,550) versus placebo in combination with background methotrexate in patients with active rheumatoid arthritis and an inadequate response to methotrexate alone.
Cohen, S; Connell, CA; French, JL; Gomez-Reino, J; Gruben, D; Kanik, KS; Kremer, JM; Krishnaswami, S; Pascual-Ramos, V; Wallenstein, G; Wilkinson, BE; Zwillich, SH, 2012
)
0.38
"Toxicological effects of repeat dosing were assessed in naïve monkeys."( Investigation of mechanism of drug-induced cardiac injury and torsades de pointes in cynomolgus monkeys.
Albassam, M; Frantz, C; Gralinski, MR; Guo, L; Kolaja, KL; Ly, J; Misner, DL; Senese, PB, 2012
)
0.38
"A dose-response curve of the repinotan effects on spontaneous minute ventilation during continuous remifentanil infusion in anesthetized rats was established to identify moderate doses: (1) tail-flick reflex latencies to assess nociception were recorded until 60 min after cessation of a continuous remifentanil infusion with or without a concomitant moderate repinotan dose (10 μg/kg), and (2) remifentanil boluses (2."( Selective 5-HT(1A)-R-agonist repinotan prevents remifentanil-induced ventilatory depression and prolongs antinociception.
Boettcher, MF; Guenther, U; Hoeft, A; Huse, D; Putensen, C; Theuerkauf, NU; Wensing, G, 2012
)
0.38
" Iloperidone 4-8, 10-16, and 20-24 mg/day (all dosed twice daily) were compared with placebo."( Efficacy of iloperidone in the short-term treatment of schizophrenia: a post hoc analysis of pooled patient data from four phase III, placebo- and active-controlled trials.
Citrome, L; Hochfeld, M; Meng, X; Stahl, SM, 2012
)
0.38
" The objective of this model-based meta-analysis was to describe the time course of HbA1c response after dosing with alogliptin (ALOG), saxagliptin (SAXA), sitagliptin (SITA), or vildagliptin (VILD)."( Quantitative model of the relationship between dipeptidyl peptidase-4 (DPP-4) inhibition and response: meta-analysis of alogliptin, saxagliptin, sitagliptin, and vildagliptin efficacy results.
Barbee, T; Correa, I; Fredrickson, J; Gibbs, JP; Gibbs, MA; Lin, SL; Smith, B, 2012
)
0.38
" Taken together, we herein report a novel oral allosteric CCR8 antagonist with predicted low once-daily dosing capable of potent inhibition of both human T cell and DC functions."( Orally bioavailable allosteric CCR8 antagonists inhibit dendritic cell, T cell and eosinophil migration.
Connolly, S; Rosendahl, A; Skrinjar, M, 2012
)
0.38
" Three-day repeat dosing of the intranasal solution GSK1004723 1,000 μg also demonstrated a statistically significant attenuation of nasal symptoms, but was less than seen with cetirizine and GSK835726 and caused initial nasal discomfort."( The efficacy and tolerability of two novel H(1)/H(3) receptor antagonists in seasonal allergic rhinitis.
Ambery, C; Daley-Yates, P; McQuade, B; Oliver, A; Sweeney, L; Watson, J, 2012
)
0.38
" The present study illustrated the potential of nanoemulsion dosage form in improving biopharmaceutic performance of piperine and guggul sterone."( Development and validation of HPLC method for simultaneous estimation of piperine and guggulsterones in compound Unani formulation (tablets) and a nanoreservoir system.
Ahmad, S; Ali, I; Arif Zaidi, SM; Baboota, S; Kamal, YT; Mohammed Musthaba, S; Parveen, R; Siddiqui, KM; Singh, M, 2012
)
0.38
"Teriflunomide - a dihydroorotate dehydrogenase (DHODH) inhibitor; AL8697 - a selective p38 MAPK inhibitor; and tofacitinib - a Janus kinase (JAK) inhibitor; were selected as representatives of their class and dose-response studies carried out using a therapeutic 10-day administration scheme in arthritic rats."( Profiling of dihydroorotate dehydrogenase, p38 and JAK inhibitors in the rat adjuvant-induced arthritis model: a translational study.
Balagué, C; Godessart, N; Pont, M; Prats, N, 2012
)
0.38
" Midazolam pharmacokinetics were assessed over 24 h following single dose 2 mg administration prior to administering tofacitinib and after twice daily dosing of tofacitinib 30 mg for 6 days."( Lack of effect of tofacitinib (CP-690,550) on the pharmacokinetics of the CYP3A4 substrate midazolam in healthy volunteers: confirmation of in vitro data.
Alvey, C; Dowty, ME; Fahmi, OA; Gupta, P; Krishnaswami, S; Riese, RJ; Walsky, RL; Wang, R, 2012
)
0.38
" The dosage was one tablet/day (5 mg) for the first two weeks and two tablets/day (10 mg) for the last two weeks."( Beneficial effect of donepezil on obstructive sleep apnea: a double-blind, placebo-controlled clinical trial.
Guilleminault, C; Moraes, W; Poyares, D; Sukys-Claudino, L; Tufik, S, 2012
)
0.38
" In the phase I study, doxorubicin and flavopiridol were administered on two flavopiridol schedules; a 1-hour bolus and split dosing as a 30-minute bolus followed by a 4-hour infusion."( The cyclin-dependent kinase inhibitor flavopiridol potentiates doxorubicin efficacy in advanced sarcomas: preclinical investigations and results of a phase I dose-escalation clinical trial.
Carvajal, RD; D'Adamo, DR; de Stanchina, E; Dickson, MA; Keohan, ML; Luke, JJ; Maki, RG; Musi, E; Schwartz, GK; Singer, S, 2012
)
0.38
" Results of studies examining the effects of multiple repeat dosing suggest that the CYP2D6 enzyme is at least partly inactivated by pridopidine."( The dopaminergic stabilizer pridopidine is to a major extent N-depropylated by CYP2D6 in humans.
Bertilsson, L; Helldén, A; Johansson, P; Panagiotidis, G; Tedroff, J; Waters, N; Waters, S, 2012
)
0.38
" On the other hand, the optimal combination and dosage of these drugs, selection of the apropriate biomarker and better understanding of the conflicting role of PDGFR and FGFR signaling in angiogenesis remain future challenges."( [Possibilities for inhibiting tumor-induced angiogenesis: results with multi-target tyrosine kinase inhibitors].
Döme, B; Török, S, 2012
)
0.38
"This sequence of dosage and symptoms suggests acetylcholinesterase inhibition was the trigger for release of these memories, which are otherwise mostly chronically repressed in this individual."( Case report: Post-traumatic memories triggered by donepezil in a dose-dependent pattern.
Wolff, ML, 2012
)
0.38
" CBF was measured by laser Doppler from rat cerebral cortex after 8 weeks of daily oral dosing of these drugs."( Bacopa monnieri increases cerebral blood flow in rat independent of blood pressure.
Chootip, K; Ingkaninan, K; Kamkaew, N; Norman Scholfield, C; Taepavarapruk, N, 2013
)
0.39
"0) on stable donepezil dosing participated in two task-related fMRI sessions consisting of a face-name paired associative encoding memory paradigm 24 weeks apart during a randomized placebo-controlled pharmaco-fMRI drug study."( Tracking cognitive change over 24 weeks with longitudinal functional magnetic resonance imaging in Alzheimer's disease.
Atri, A; Deluca, AN; Diamond, EL; McLaren, DG; Mitchell, MB; O'Brien, JL; Rentz, DM; Sperling, RA; Sreenivasan, A; Van Dijk, KR, 2012
)
0.38
" The X-ray crystallography studies have been revealed that Alogliptin binds to DPP-IV active site by non-covalently and provides sustained reduction of plasma DPP-IV activity as well as lowering of blood glucose, in drug-naive patients with T2DM and inadequate glycemic control, once daily oral dosing regimen with varying levels of doses ranging from 25-800 mg."( Novel serine protease dipeptidyl peptidase IV inhibitor: alogliptin.
Agrawal, R; Bahare, RS; Dikshit, SN; Ganguly, S; Jain, P, 2012
)
0.38
" Follow-up dose-response studies revealed that 12 of the 13 known EGFR inhibitors in the library were confirmed as hits."( A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery.
Antczak, C; Bhinder, B; Calder, PA; Djaballah, H; Mahida, JP, 2012
)
0.38
" During the experiments, animals were dosed intravenously with the CB1 receptor antagonist rimonabant (0."( Cannabinoid receptors mediate methamphetamine induction of high frequency gamma oscillations in the nucleus accumbens.
Cheer, JF; Glick, SD; Morra, JT, 2012
)
0.38
" Frequent dosing of the antagonist results in side effects like sedation and cardiovascular toxicity."( In silico ligand based design of indolylpiperidinyl derivatives as novel histamine H(1) receptor antagonists.
Pal, M; Paliwal, S; Singh, S, 2012
)
0.38
" Instead, selective serotonin 2A receptor (5HT(2A)R) antagonists ketanserin and MDL-11939 replicate the effect of SGAs, repressing the activity in WT mice at a dosage that fails to suppress the activity of Egr3(-/-) mice."( Reduced levels of serotonin 2A receptors underlie resistance of Egr3-deficient mice to locomotor suppression by clozapine.
Elizalde, DI; Gallitano, AL; González-Maeso, J; Ingram, WM; Janowski, SA; Kamel, CM; Kozlenkov, A; Levine, S; Lish, JR; Resnik, J; Shoker, J; Williams, AA, 2012
)
0.38
"Vandetanib (an orally bioavailable VEGFR-2 and EGFR tyrosine kinases inhibitor) was combined at 100 mg, 200 mg, or 300 mg daily with standard dosed cetuximab and irinotecan (3+3 dose-escalation design)."( Phase I study of cetuximab, irinotecan, and vandetanib (ZD6474) as therapy for patients with previously treated metastastic colorectal cancer.
Abrams, TA; Ancukiewicz, M; Blaszkowsky, L; Chan, JA; Duda, DG; Elliott, M; Enzinger, PC; Goldstein, M; Jain, RK; Kulke, MH; Meyerhardt, JA; Regan, E; Schrag, D; Wolpin, BM; Zhu, AX, 2012
)
0.38
" Previous nonclinical reports supporting oral dosing have utilized liquid chromatography tandem mass spectrometry (LC/MS/MS) to quantify donepezil concentrations in plasma."( Dried blood spot analysis of donepezil in support of a GLP 3-month dose-range finding study in rats.
Arjmand, FM; Diehl, L; Huang, B; Lucke, RM; Meier-Davis, SR; Meng, M; Nagata, T; Shudo, J; Wen, J; Yuan, W,
)
0.13
" A refined dosing strategy was applied for a muscarinic agonist, AZD6088, using the rat spinal nerve ligation heat hyperalgesia model."( Evaluation of an innovative population pharmacokinetic-based design for behavioral pharmacodynamic endpoints.
Laird, JM; Lessard, E; Martino, G; Viberg, A, 2012
)
0.38
" The large (n=331), randomized, double-blind, multinational ZETA trial compared vandetanib at a dosage of 300 mg once daily with placebo in patients with unresectable, locally advanced or metastatic, hereditary or sporadic, medullary thyroid cancer."( Vandetanib: in medullary thyroid cancer.
Frampton, JE, 2012
)
0.38
"Using models of respiratory compromise, loss of response to esophageal instrumentation, and loss of responsiveness, the authors explored through simulation published dosing schemes for endoscopy using propofol alone and in combination with selected opioids."( A simulation study of common propofol and propofol-opioid dosing regimens for upper endoscopy: implications on the time course of recovery.
Egan, TD; Johnson, KB; LaPierre, CD; Randall, BR, 2012
)
0.38
"Four published dosing regimens of propofol alone or in combination with opioids were used to predict the probability of loss of response to esophageal instrumentation for a 10-min procedure and the probability of respiratory compromise and return of responsiveness once the procedure had ended."( A simulation study of common propofol and propofol-opioid dosing regimens for upper endoscopy: implications on the time course of recovery.
Egan, TD; Johnson, KB; LaPierre, CD; Randall, BR, 2012
)
0.38
" Further study is needed to determine whether these results concerning mechanism and dosage can be the basis for prevention of the development of CIS in at risk populations."( Prevention of the phencyclidine-induced impairment in novel object recognition in female rats by co-administration of lurasidone or tandospirone, a 5-HT(1A) partial agonist.
Adelekun, AE; Hannaway, KE; Horiguchi, M; Jayathilake, K; Meltzer, HY, 2012
)
0.38
"The purpose of this study was to develop an injectable depot liposphere delivery system with high loading capacity for controlled delivery of donepezil to decrease dosing frequency and increase patient compliance."( Biodegradable donepezil lipospheres for depot injection: optimization and in-vivo evaluation.
Elsayed, I; Elshafeey, AH; Yehia, SA, 2012
)
0.38
" In vitro studies have shown that pridopidine is a substrate for the P450 cytochrome 2D6 enzyme (CYP2D6), and clinical data show that the half-life of pridopidine is different following single dosing versus at steady state."( Pharmacokinetic and tolerability profile of pridopidine in healthy-volunteer poor and extensive CYP2D6 metabolizers, following single and multiple dosing.
Gundorf Drewes, P; Lindskov Krog, P; Osterberg, O; Rembratt, Å; Schultz, A; Timmer, W, 2013
)
0.39
"Application of Narcotrend monitor in monitoring the depth of anesthesia in severely burned patients during perioperative period with TCI of remifentanil hydrochloride and propofol is beneficial to reducing dosage of narcotics and shortening duration of recovery from anesthesia, and it can accurately predict the level of consciousness of patients at the time of withdrawal of anesthesia."( [Application of Narcotrend-assisted anesthesia in-depth monitor during escharectomy and skin transplantation in burn patients with target-controlled infusion of remifentanil hydrochloride and propofol].
Guo, ZG; Hao, JH; Lü, XL; Su, XJ; Wang, XY, 2012
)
0.38
" Mini-Mental State Examination and Alzheimer's Disease Assessment Scale (ADAS) scores were determined before and after the donepezil dosage increase."( Efficacy of a high dosage of donepezil for Alzheimer's disease as examined by single-photon emission computed tomography imaging.
Abe, S; Fujii, H; Iwamoto, T; Kanaya, K; Koizumi, K; Sakai, M, 2012
)
0.38
"After the donepezil dosage increase, adverse effects associated with gastrointestinal symptoms were observed in one patient, and irritability was observed in three."( Efficacy of a high dosage of donepezil for Alzheimer's disease as examined by single-photon emission computed tomography imaging.
Abe, S; Fujii, H; Iwamoto, T; Kanaya, K; Koizumi, K; Sakai, M, 2012
)
0.38
"Increasing the donepezil dosage from 5 mg/day to 10 mg/day is effective for the treatment of AD."( Efficacy of a high dosage of donepezil for Alzheimer's disease as examined by single-photon emission computed tomography imaging.
Abe, S; Fujii, H; Iwamoto, T; Kanaya, K; Koizumi, K; Sakai, M, 2012
)
0.38
"To improve the analgesic efficiency and to simplify the administration of remifentanil for systemic analgesia in labour, we contrived a modified delivery regimen with a specific infusion profile and variable dosing and conducted a single-blind randomised crossover study to compare it with the previous 'classical' regimen."( Modified patient-controlled remifentanil bolus delivery regimen for labour pain*.
Ban, B; Jost, A; Kamenik, M, 2013
)
0.39
" Acute dosing of vortioxetine inhibited neuronal firing activity more potently than fluoxetine."( The rapid recovery of 5-HT cell firing induced by the antidepressant vortioxetine involves 5-HT(3) receptor antagonism.
Bétry, C; Ebert, B; Etiévant, A; Haddjeri, N; Pehrson, AL; Sánchez, C, 2013
)
0.39
" Thirty-two patients with recurrent glioblastoma multiforme (GBM) and 32 patients with recurrent anaplastic gliomas (AGs) were treated in the phase II trial, at a dosage of 300 mg/day on 28-day cycles."( A phase I/II trial of vandetanib for patients with recurrent malignant glioma.
Fine, HA; Iwamoto, FM; Kreisl, TN; McNeill, KA; Shih, J; Sul, J, 2012
)
0.38
" A1120 dosing in mice induced 75% reduction in serum RBP4, which correlated with reduction in visual cycle retinoids and ocular levels of lipofuscin fluorophores."( A1120, a nonretinoid RBP4 antagonist, inhibits formation of cytotoxic bisretinoids in the animal model of enhanced retinal lipofuscinogenesis.
Allikmets, R; Dobri, N; Kong, J; Liu, Z; Ma, JX; Moiseyev, G; Petrukhin, K; Qin, Q; Sparrow, JR; Yamamoto, K, 2013
)
0.39
" While longer randomized controlled trials, increase dosage and selected groups of patients at different stage of cognitive impairment may provide a better understanding of the potential for this drug in addressing cognitive deficits, results to date have not been encouraging."( Assessing the prospect of donepezil in improving cognitive impairment in patients with schizophrenia.
Henderson, DC; Thakurathi, N; Vincenzi, B, 2013
)
0.39
"Adjusting the remifentanil dosage according to the SPI in outpatient anaesthesia reduced the consumption of both remifentanil and propofol and resulted in faster recovery."( Surgical pleth index-guided remifentanil administration reduces remifentanil and propofol consumption and shortens recovery times in outpatient anaesthesia.
Bauer, M; Bergmann, I; Crozier, TA; Göhner, A; Hesjedal, B; Hinz, JM; Popov, AF; Wiese, CH, 2013
)
0.39
" Humans dosed orally with MK-5757 showed reduced [(18)F]MK-0911 tracer concentration in brain proportional with MK-5757 dose and plasma level."( Evaluation of [¹⁸F]MK-0911, a positron emission tomography (PET) tracer for opioid receptor-like 1 (ORL1), in rhesus monkey and human.
Bi, S; Bormans, G; Burns, HD; Cho, W; Cook, JJ; de Groot, T; de Hoon, J; De Lepeleire, I; Depré, M; Egan, M; Eng, W; Gibson, RE; Hargreaves, RJ; Hostetler, ED; Joshi, AD; Kawamoto, H; Krause, SM; O'Malley, S; Ohta, H; Okamoto, O; Ozaki, S; Patel, S; Reynders, T; Riffel, K; Ryan, C; Sanabria-Bohórquez, S; van Laere, K, 2013
)
0.39
"4 μM, while in other cells it augmented the current with a bell-shaped dose-response curve."( Donepezil in low micromolar concentrations modulates voltage-gated potassium currents in pyramidal neurons of rat hippocampus.
Bukanova, JV; Skrebitsky, VG; Solntseva, EI, 2013
)
0.39
" However, these agents differ from one another in terms of formulations, pharmacokinetics, and dosing and nonmetabolic adverse effect profile."( Asenapine, iloperidone and lurasidone: critical appraisal of the most recently approved pharmacotherapies for schizophrenia in adults.
Bobo, WV, 2013
)
0.39
" In a comparison of the relative potency of each drug at different dosing ranges, tacrolimus had the strongest Th1 inhibitory effect (median inhibition of interferon-γ at 97."( Comparison of the effect of standard and novel immunosuppressive drugs on CMV-specific T-cell cytokine profiling.
Broscheit, C; Egli, A; Humar, A; Kumar, D; O'Shea, D, 2013
)
0.39
"This Phase 2b study assessed three tofacitinib dosage regimens vs."( Tofacitinib (CP-690,550), an oral Janus kinase inhibitor, improves patient-reported outcomes in a phase 2b, randomized, double-blind, placebo-controlled study in patients with moderate-to-severe psoriasis.
Harness, J; Mamolo, C; Menter, A; Tan, H, 2014
)
0.4
"Ethosomal system can successfully deliver RPG transdermally; sustain its effect and thus reduce its dosing frequency."( A study on ethosomes as mode for transdermal delivery of an antidiabetic drug.
Bodade, SS; Chaudhari, PD; Kamble, MS; Shaikh, KS, 2013
)
0.39
" In slices from Ts65Dn mice, a Down syndrome model with excess inhibition and cognitive impairment, acutely applied Ro25-rescued long-term potentiation (LTP) and gamma oscillation deficits, whereas prolonged dosing induced persistent rescue of LTP."( GluN2B antagonism affects interneurons and leads to immediate and persistent changes in synaptic plasticity, oscillations, and behavior.
Deng, L; Hanson, JE; Luu, T; Meilandt, WJ; Scearce-Levie, K; Shamloo, M; Sheng, M; Weber, M; Wu, T; Zhou, Q, 2013
)
0.39
" In a dose-response study the 5-HT2A agonist (±)-2,5-dimethoxy-4-iodoamphetamine hydrochloride (DOI) (25 nM to 5 μM) protected against serum deprivation cytotoxicity."( 5-HT2A serotonin receptor agonist DOI alleviates cytotoxicity in neuroblastoma cells: role of the ERK pathway.
Grünblatt, E; Marinova, Z; Walitza, S, 2013
)
0.39
" The purpose of this study is to predict the dosing time-dependent pharmacokinetic interactions of repaglinide with rifampicin, using mechanistic models."( Quantitative prediction of repaglinide-rifampicin complex drug interactions using dynamic and static mechanistic models: delineating differential CYP3A4 induction and OATP1B1 inhibition potential of rifampicin.
Bi, YA; El-Kattan, AF; Fahmi, OA; Goosen, TC; Lai, Y; Lam, JL; Lin, J; Rotter, CJ; Varma, MV, 2013
)
0.39
" The results can be used for simulation in further clinical trial and optimize individual dosage regimens using a Bayesian methodology in patients."( Population pharmacokinetics of blonanserin in Chinese healthy volunteers and the effect of the food intake.
Li, FF; Li, X; Liu, X; Lu, W; Luo, FT; Ni, XJ; Qiu, C; Shang, DW; Wang, XP; Wen, YG; Xie, HZ; Zhang, M, 2013
)
0.39
" The 90 mg/day dosage appears worthy of further study."( A randomized, double-blind, placebo-controlled trial of pridopidine in Huntington's disease.
, 2013
)
0.39
"A phase I dose escalation study was performed to determine the maximum tolerated dose (MTD) of intercalated dosing of BMS-690514, a reversible oral panHER/VEGF receptor inhibitor, combined with paclitaxel/carboplatin (PC) in advanced solid tumors."( A phase I trial to determine the safety, pharmacokinetics, and pharmacodynamics of intercalated BMS-690514 with paclitaxel/carboplatin (PC) in advanced or metastatic solid malignancies.
Adjei, AA; Belani, CP; Chow, LQ; Dy, GK; Fortin, C; Gupta, A; Jonker, DI; Laurie, SA; Nicholas, G; Park, JS; Patricia, D; Sbar, EI; Zhang, S, 2013
)
0.39
"The present study was aimed to characterize the anticonvulsant effects of piperine in combination with well established antiepileptic drug (AED) phenytoin, in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for non-parallel dose-response relationship curves (DRRCs)."( Combination therapy of piperine and phenytoin in maximal electroshock induced seizures in mice: isobolographic and biochemical analysis.
Khanam, R; Pillai, KK; Saraogi, P; Vohora, D, 2013
)
0.39
"Bilastine (Bilaxten™) is a novel non-sedating H1 receptor antagonist (antihistamine) developed in the dosage form of oral tablets and indicated for the treatment of allergic rhinitis (seasonal and perennial) and urticaria."( Oral availability of bilastine.
Azanza, JR; Gómez-Guiu, A; Ortega, I; Sádaba, B; Valiente, R, 2013
)
0.39
"7-fold over vehicle) upon oral dosing of 27 at 300 mg/kg."( Rational design and binding mode duality of MDM2-p53 inhibitors.
Bartberger, MD; Beck, HP; Canon, J; Chen, A; Chow, D; Correll, TL; Gonzalez-Lopez de Turiso, F; Huang, X; Julian, LD; Kayser, F; Lo, MC; Long, AM; McMinn, D; Medina, JC; Oliner, JD; Olson, SH; Osgood, T; Powers, JP; Rew, Y; Saiki, AY; Schneider, S; Shaffer, P; Sun, D; Xiao, SH; Yakowec, P; Yan, X; Ye, Q; Yu, D; Zhao, X; Zhou, J, 2013
)
0.39
" First-choice treatment continues to be centred on the second-generation H1 antihistamines, including a wide group of drugs with a better therapeutic index (or risk:benefit ratio) than the classic ones, even in the high, off-label dosage occasionally required in chronic urticaria."( Bilastine for the treatment of urticaria.
Bartra, J; Dávila, I; del Cuvillo, A; Ferrer, M; Jáuregui, I; Montoro, J; Mullol, J; Sastre, J; Valero, A, 2013
)
0.39
" Demographic variables, quantity and rate of prescriptions, dosage forms and strengths were analyzed."( [Drugs used for cognitive impairment. Analysis of 1.5 million prescriptions in Argentina].
Arizaga, RL; Demey, I; Rojas, G, 2013
)
0.39
" In mouse hippocampal slices, sunifiram at 10-100 nM significantly enhanced LTP in a bell-shaped dose-response relationship which peaked at 10 nM."( Novel nootropic drug sunifiram enhances hippocampal synaptic efficacy via glycine-binding site of N-methyl-D-aspartate receptor.
Fukunaga, K; Moriguchi, S; Narahashi, T; Tanaka, T, 2013
)
0.39
"Mice were treated using a repeated dosing paradigm and body temperatures recorded."( σ Receptor antagonist attenuation of methamphetamine-induced neurotoxicity is correlated to body temperature modulation.
Coop, A; Matsumoto, RR; McCurdy, CR; Robson, MJ; Seminerio, MJ, 2013
)
0.39
" Remifentanil gives rapid effect, shortens the duration of mechanical ventilation, reduces the dosage of propofol, and has no severe adverse effect."( [Remifentanil for analgesia and sedation in mechanically ventilated patients in intensive care unit].
Liu, KB; Ma, Y; Wang, DH; Xia, R, 2013
)
0.39
" Furthermore there are other factors such as succinylcholines use when fast intubation is needed, the wrong myorelaxant and dosage choice."( [Modern approach to the neuromuscular blocking agents use in pediatric patients].
Agavelyan, EG; Stepanenko, SM,
)
0.13
" (clinical periods, late donepezil treatment) with the dosage of 1, 2 and 4 mg/kg/d respectively and the treatments persisted throughout the experiments."( The anti-inflammatory effect of donepezil on experimental autoimmune encephalomyelitis in C57 BL/6 mice.
Chen, S; Chen, X; Jiang, Y; Kang, Z; Liu, M; Liu, Y; Ma, L; Ma, X; Peng, F; Pi, R; Wang, Q; Wu, A; Zhu, C; Zhu, D; Zou, Y, 2013
)
0.39
"Because cognitive function showed improvement after increasing the dose of donepezil, the dosage of this drug should probably be adjusted based on the overall severity of Alzheimer's disease as well as the progression of cognitive dysfunction."( Efficacy of increasing donepezil in mild to moderate Alzheimer's disease patients who show a diminished response to 5 mg donepezil: a preliminary study.
Hashimoto, M; Honda, K; Ikeda, M; Kaneda, K; Ogawa, Y; Yatabe, Y; Yuuki, S, 2013
)
0.39
" Nonlinear regression analysis was used to describe the dose-response relationships for the aepEX, the BIS, and propofol plasma concentrations (Cp)."( Evaluation of the aepEX™ monitor of hypnotic depth in pediatric patients receiving propofol-remifentanil anesthesia.
Cheung, YM; Hoeks, SE; Scoones, GP; Stolker, RJ; Weber, F, 2013
)
0.39
" ZC88 significantly inhibited the tumor growth in nude mice at a dosage with slight influence on the cardiac QT interval."( ZC88, a novel 4-amino piperidine analog, inhibits the growth of neuroblastoma cells through blocking hERG potassium channel.
Hua, N; Liu, X; Ma, X; Sun, H; Wei, X; Yan, H; Zhang, C; Zhang, S; Zheng, J, 2013
)
0.39
" In case of orally disintegrating tablet (ODT) containing bitter medicine, in vitro and in vivo disintegration is also importance for dosage performance."( In vitro and in vivo correlation of disintegration and bitter taste masking using orally disintegrating tablet containing ion exchange resin-drug complex.
Cao, QR; Cho, SM; Cui, JH; Kim, JI; Lee, BJ; Oh, E, 2013
)
0.39
" Research into aspects of pharmacokinetics and efficacy and adverse effect profiles of bilastine in children under 12 years of age is needed as are dose-response assessments and studies planned rigorously with the aim of assessing quality of life effects."( Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria.
Wolthers, OD, 2013
)
0.39
" However, additional research is necessary to identify the optimal dosing schedule, as well as patients most likely to benefit from BTK inhibition."( Ibrutinib and novel BTK inhibitors in clinical development.
Akinleye, A; Chen, Y; Liu, D; Mukhi, N; Song, Y, 2013
)
0.39
" We conducted a Phase I dose-escalation study to determine the maximum tolerated dose (MTD) for single-agent flavopiridol administered on a pharmacokinetically derived hybrid dosing schedule to patients with relapsed and refractory non-Hodgkin's lymphoma."( Flavopiridol can be safely administered using a pharmacologically derived schedule and demonstrates activity in relapsed and refractory non-Hodgkin's lymphoma.
Andritsos, L; Baiocchi, R; Benson, DM; Blum, KA; Byrd, JC; Christian, B; Flynn, J; Grever, MR; Jones, JA; Penza, S; Phelps, MA; Poi, M; Porcu, P; Rupert, AS, 2014
)
0.4
" Further, MFZ 10-7 appeared to be more potent than MTEP in inducing downward shifts in the cocaine dose-response curve, but less effective than MTEP in attenuating sucrose-induced reinstatement of sucrose-seeking behavior."( A novel mGluR5 antagonist, MFZ 10-7, inhibits cocaine-taking and cocaine-seeking behavior in rats.
Bi, GH; Gardner, EL; Keck, TM; Newman, AH; Srivastava, R; Wang, XF; Xi, ZX; Yang, HJ; Zhang, HY; Zou, MF, 2014
)
0.4
" PK data were obtained from blood and dialyzate (patients with ESRD only) samples prior and subsequent to dosing and/or hemodialysis (patients with ESRD only)."( Pharmacokinetics of tofacitinib, a janus kinase inhibitor, in patients with impaired renal function and end-stage renal disease.
Boy, M; Chan, G; Chow, V; Krishnaswami, S; Wang, C, 2014
)
0.4
" The variables discussed include dose, dosing schedule, genes, drug-drug interactions, and other medical factors."( Complexities of personalized medicine: how genes, drug-drug interactions, dosing schedules, and other factors can combine to produce clinically meaningful differences in a drug's effect.
Preskorn, SH, 2013
)
0.39
" There are often patients who desire extensive liposuction on approximately 30% of total body surface area, which means the lidocaine total dose might be over the dosing recommendation."( Safe extensive tumescent liposuction with segmental infiltration of lower concentration lidocaine under monitored anesthesia care.
Cao, WG; Jiang, ZH; Li, SL; Liu, LN; Wang, G, 2015
)
0.42
"9nM) showed a good pharmacokinetic profile upon oral dosing at 10mg/kg in Sprague-Dawley (SD) rats."( Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists.
Bhosale, VM; Chaudhari, SS; Gudi, GS; Kadam, AB; Karnik, PV; Khairatkar-Joshi, N; Mukhopadhyay, I; Raghuram, A; Rao, SS; Sangana, RR; Thomas, A; Vaiyapuri, TS; Wale, DP, 2013
)
0.39
" The main differences between the five gliptins on the market include: potency, target selectivity, oral bioavailability, long or short half-life, high or low binding to plasma proteins, metabolism, presence of active or inactive metabolites, excretion routes, dosage adjustment for renal and liver insufficiency, and potential drug-drug interactions."( Dipeptidyl peptidase-4 inhibitors in type 2 diabetes therapy--focus on alogliptin.
Capuano, A; Esposito, K; Giugliano, D; Maiorino, MI; Rossi, F; Sportiello, L, 2013
)
0.39
"7 % high dose), while both TGF-β3 dosage groups showed no significant change (65."( Preliminary results of antiscarring therapy in the prevention of postendoscopic esophageal mucosectomy strictures.
Chak, A; Cipriano, C; Lash, RH; Marks, JM; Ponsky, JL; Schomisch, SJ; Wu, Y, 2014
)
0.4
" Treatment lasted 8 weeks: 3 weeks of flexible dosing according to investigator's judgment (10 mg, 20 mg, or 40 mg a day of pitolisant; 100 mg, 200 mg or 400 mg a day of modafinil) followed by 5 weeks of stable dosing."( Pitolisant versus placebo or modafinil in patients with narcolepsy: a double-blind, randomised trial.
Arnulf, I; Bassetti, C; Dauvilliers, Y; Ding, CL; Lammers, GJ; Lecomte, JM; Lehert, P; Mayer, G; Rodenbeck, A; Schwartz, JC, 2013
)
0.39
" Notably, cells aligned on the biomimetic platform responded detectably down to a dosage of 3 nM E-4031, which is lower than the IC50 in the hERG channel assay."( Integrated platform for functional monitoring of biomimetic heart sheets derived from human pluripotent stem cells.
Chen, A; Fowlkes, C; Grosberg, A; Khine, M; Lee, E; Santiago, K; Tu, R, 2014
)
0.4
" Participants were assigned to receive 3 weeks of oral dosing with placebo or fluoxetine, 40 mg per day."( Central 5-HT4 receptor binding as biomarker of serotonergic tonus in humans: a [11C]SB207145 PET study.
Baaré, WF; Fisher, PM; Frokjaer, VG; Haahr, ME; Jensen, CG; Knudsen, GM; Lehel, S; Madsen, K; Mahon, BM; Norremolle, A; Rabiner, EA, 2014
)
0.4
"The mean (SD) blonanserin dosage was 14."( Blonanserin, a novel antipsychotic, is suitable for treating schizophrenia associated with hyperprolactinemia: a case series.
Horiuchi, F; Kawabe, K; Ueno, S,
)
0.13
"A critical piece in the translation of preclinical studies to clinical trials is the determination of dosing regimens that allow maximum therapeutic benefit with minimum toxicity."( Preclinical to clinical translation of tofacitinib, a Janus kinase inhibitor, in rheumatoid arthritis.
Dowty, ME; Ghosh, S; Jesson, MI; Kishore, N; Krishnaswami, S; Lee, J; Meyer, DM, 2014
)
0.4
" The approved dosing regimen includes an initial dose prior to surgery and 12 mg twice daily after surgery for up to 7 days; however, there are no human studies evaluating the need for the preoperative dose."( Efficacy of alvimopan following bowel resection: a comparison of two dosing strategies.
Brock, G; Cox, M; Pass, LA; Scherrer, N; Truelove, D; Winegar, B, 2013
)
0.39
"Patients receiving the approved alvimopan dosing regimen experienced the most rapid recovery of gastrointestinal function."( Efficacy of alvimopan following bowel resection: a comparison of two dosing strategies.
Brock, G; Cox, M; Pass, LA; Scherrer, N; Truelove, D; Winegar, B, 2013
)
0.39
"To review the pharmacology, pharmacokinetics, efficacy and safety, dosage administration, and adverse effects of tofacitinib for rheumatoid arthritis (RA) treatment."( Tofacitinib: The First Janus Kinase (JAK) inhibitor for the treatment of rheumatoid arthritis.
Bandy, JL; Boyce, EG; O'Dell, KM; Vyas, D, 2013
)
0.39
" The Food and Drug Administration's recent approval of the increased dosage strength, donepezil 23 mg, previously only available in 5 mg and 10 mg strengths, has raised efficacy and safety concerns."( Donepezil 23 mg: a brief insight on efficacy and safety concerns.
Nguyen, MD; Salbu, RL, 2013
)
0.39
" Alogliptin does not require any dosage adjustment when coadministered with ketoconazole, fluconazole, gemfibrozil, warfarin, metformin, glyburide, and pioglitazone."( Alogliptin: A new dipeptidyl peptidase-4 inhibitor for the management of type 2 diabetes mellitus.
Erowele, G; Ndefo, UA; Okoli, O, 2014
)
0.4
" Compound 6s demonstrated free-plasma exposures above the IC50 (∼50×) with a brain-to-plasma ratio of ∼3 following intravenous dosing in mice."( Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.
Bernstein, PR; Brown, DG; Cacciola, J; Dasser, M; Edwards, PD; Folmer, JJ; Giguère, P; Griffin, A; Groblewski, T; Labrecque, D; Lazor, LA; Lévesque, C; Mauger, R; Potts, WM; Pourashraf, M; Santhakumar, V; Scott, C; Sydserff, S; Sylvester, M; Throner, SR; Tremblay, MC; Wesolowski, S, 2014
)
0.4
" In each treatment group, the baseline characteristics including age, gender, body mass index, diabetes duration, HbA1c, fasting plasma glucose, body weight, daily dosage of metformin and daily dosage of pioglitazone were all well balanced."( [The design and baseline characteristics of a phase III study to evaluate the efficacy and safety of alogliptin versus placebo in type 2 diabetes mellitus in Mainland China].
Bu, RF; Gu, W; Han, P; Ji, QH; Jiang, ZS; Lei, MX; Li, CJ; Li, L; Li, WH; Li, XF; Li, XJ; Li, ZF; Liu, JD; Liu, XM; Liu, Y; Liu, ZM; Lu, JM; Lü, XF; Pan, CY; Peng, YD; Qu, S; Shi, BY; Song, QH; Xu, XJ; Xue, YM; Yan, L; Yang, JK; Zeng, JE; Zheng, BZ, 2013
)
0.39
" Plasma renin activity remained suppressed during the 24-hour dosing interval at all doses."( Multiple ascending dose study with the new renin inhibitor VTP-27999: nephrocentric consequences of too much renin inhibition.
Azizi, M; Balcarek, J; Bryson, C; Danser, AH; Garrelds, IM; Gregg, R; Griffith, SG; McGeehan, G; Ménard, J; Reeves, RA; Sevá Pessôa, B, 2014
)
0.4
" Thus, it may be useful for prolonged drug release in stomach to improve the bioavailability and reduced dosing frequency."( Gastroretentive mucoadhesive tablet of lafutidine for controlled release and enhanced bioavailability.
Patil, S; Talele, GS, 2015
)
0.42
" All subjects also received omeprazole 20 mg each morning beginning 4 days prior to the first treatment period and continuing through danirixin dosing in the final treatment period."( The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers.
Ambery, CL; Bloomer, JC; Connolly, P; Lazaar, AL; Miller, BE; Mistry, S; Sanderson, D; Shreeves, T; Smart, K; Smith, R, 2014
)
0.4
" All patients were titrated on iloperidone to 6mg BID by Day 4, then flexibly dosing between 6 and 12mg BID, as needed."( A trial evaluating gradual- or immediate-switch strategies from risperidone, olanzapine, or aripiprazole to iloperidone in patients with schizophrenia.
Alva, G; Brams, M; Citrome, L; Glick, ID; Hochfeld, M; Jackson, R; Kianifard, F; Mattingly, G; Meng, X; Pestreich, L; Weiden, PJ; Winseck, A, 2014
)
0.4
" In literature, there is no research investigating the effect of lidocaine infusion on remifentanil and anesthetic dosage used in hypotensive anesthesia."( Impact of perioperative lidocaine infusion and bis monitorization on remifentanil dosage in hypotensive anesthesia.
Aypar, U; Erden, A; Uzun, S; Yuce, Y, 2014
)
0.4
"kg(-1) bolus dosage given in 10 minutes."( Impact of perioperative lidocaine infusion and bis monitorization on remifentanil dosage in hypotensive anesthesia.
Aypar, U; Erden, A; Uzun, S; Yuce, Y, 2014
)
0.4
" RO by donepezil was calculated from a modified Lassen plot, and ED50 was estimated from the sigmoidal dose-response curves obtained when the RO was plotted against log donepezil dose."( Dose-dependent sigma-1 receptor occupancy by donepezil in rat brain can be assessed with (11)C-SA4503 and microPET.
Dierckx, RA; Elsinga, PH; Ishiwata, K; Luurtsema, G; Nyakas, CJ; Ramakrishnan, NK; Schepers, M; van Waarde, A; Visser, AK, 2014
)
0.4
" Donepezil dosage was then increased to 10 mg/day for 12 weeks."( Effects of donepezil dose escalation in Parkinson's patients with dementia receiving long-term donepezil treatment: an exploratory study.
Hattori, N; Ishikawa, K; Kubo, S; Mizuno, Y; Motoi, Y, 2014
)
0.4
" Designing a controlled release dosage form of the drug is required to maintain its therapeutic blood level and to eliminate its adverse effects, particularly the hypoglycaemia."( Preparation and evaluation of a controlled drug release of repaglinide through matrix pellets: in vitro and in vivo studies.
Minaiyan, M; Pendar, Y; Tabbakhian, M; Tavakoli, N, 2014
)
0.4
"Inclusion criteria were double-blind, placebo-controlled trials of any length comparing patients diagnosed with probable Alzheimer disease (according to the NINCDS-ADRDA/DSM-III/IV criteria) taking any dosage of donepezil."( The effect of funding sources on donepezil randomised controlled trial outcome: a meta-analysis.
Abrahams, S; Della Sala, S; Killin, LO; Russ, TC; Starr, JM, 2014
)
0.4
" The propofol dosage required for anesthetic maintenance was 29% (with a 95% confidence interval, 18-40) lower in patients given dexmedetomidine (2."( Dexmedetomidine reduces propofol and remifentanil requirements during bispectral index-guided closed-loop anesthesia: a double-blind, placebo-controlled trial.
Augé, M; Bonnet, F; Chazot, T; Dardelle, D; Fischler, M; Laloë, PA; Le Guen, M; Liu, N; Sessler, DI; Tounou, F; Tuil, O, 2014
)
0.4
" The best dosage of this drug for postoperative analgesia remains to be elucidated."( [Efficacy and safety of remifentanil-based regimen for postoperative pain management in abdominal surgery patients: a double-blind study with low-dose remifentanil infusion of 0.02 microg x kg(-1) x min(-1)].
Hirano, H; Kaida, T; Machino, A; Nagasaka, Y; Shirasaki, R; Wakamatsu, M, 2014
)
0.4
" In dose-response tests, the widely used repellents N,N-diethyl-3-methyl benzamide (deet) and 1-methyl-propyl-2-(hydroxyethyl)-1-piperidinecarboxylate (picaridin) were applied to filter paper strips and challenged by ticks at 10, 20, 30, 40, and 120 min after application."( Solvent, drying time, and substrate affect the responses of lone star ticks (Acari: Ixodidae) to the repellents deet and picaridin.
Bedoukian, RH; Carroll, JF; Kramer, M, 2014
)
0.4
" We used piperidine18 (Pip18), a potent and selective GluN2B-NMDAR antagonist with favorable pharmacokinetic properties, for long-term dosing in AD mouse models."( Chronic GluN2B antagonism disrupts behavior in wild-type mice without protecting against synapse loss or memory impairment in Alzheimer's disease mouse models.
Gogineni, A; Hanson, JE; Herrington, J; Meilandt, WJ; Reynen, P; Scearce-Levie, K; Weimer, RM; Zhou, Q, 2014
)
0.4
" It also reduce the dosage of anesthetics and improve the safety of anesthesia."( [The anesthesiologic value of transcutaneous acupoint electrical stimulation combined with general intravenous anesthesia in endoscopic thyroidectomy patients: a clinical study].
Li, YL; Wang, MX; Wu, XY; Yan, YN, 2014
)
0.4
" The dosage for anesthesia maintenance, recovery time of awareness, extubation time, incidences of nausea, vomiting and chill and irritation of urethral catheters were observed and recorded."( [Effects of assisted-electroacupuncture on recovery of fast tracking anesthesia in mPCNL].
Chen, YH; Lin, CQ; Luo, FR; Ou, JY; Xie, LC; Yan, J; Yang, YB; Zhang, CZ; Zhang, SL; Zhong, SQ, 2014
)
0.4
"The assisted-electroacupuncture anesthesia could reduce the dosage of remifentanil and sevoflurane in mPCNL fast tracking anesthesia in urinary surgery, reduce the incidences of nausea, vomiting, chill and irritation of urethral catheters during recovery stage, and prompt recovery of mPCNL patients."( [Effects of assisted-electroacupuncture on recovery of fast tracking anesthesia in mPCNL].
Chen, YH; Lin, CQ; Luo, FR; Ou, JY; Xie, LC; Yan, J; Yang, YB; Zhang, CZ; Zhang, SL; Zhong, SQ, 2014
)
0.4
"129 patients were treated at ten dosing regimens combining vemurafenib and cobimetinib: 66 had recently progressed on vemurafenib and 63 had never received a BRAF inhibitor."( Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study.
Boasberg, P; Chan, I; Chmielowski, B; Choong, N; Daud, A; Flaherty, L; Gajewski, TF; Gonzalez, R; Hamid, O; Kee, D; Lewis, K; Logan, T; McArthur, GA; Musib, L; Pavlick, A; Puzanov, I; Ribas, A; Yin, M, 2014
)
0.4
" Dose-response relationships and association with inflammation (C-reactive protein (CRP)) were explored using Phase 2 data and confirmed with Phase 3 data."( Changes in serum creatinine in patients with active rheumatoid arthritis treated with tofacitinib: results from clinical trials.
Boy, MG; Hutmacher, MM; Isaacs, JD; Kowalski, K; Krishnaswami, S; Lan, S; Menon, S; Nduaka, C; Riese, R; Zuckerman, A, 2014
)
0.4
"The present results suggest that a clinical dosage of DPZ accelerates angiomyogenesis by directly acting on both endothelial and satellite cells."( Donepezil can improve ischemic muscle atrophy by activating angiomyogenic properties of satellite cells.
Arikawa, M; Doi, Y; Hoshino, E; Iiyama, T; Kakinuma, Y; Kitaoka, H; Kubo, T; Noguchi, T; Okazaki, K; Sato, T, 2014
)
0.4
" In these animal models, the dose-response curve for LPS was too steep to allow use in survival studies and no changes in the N/OFQ system occurred within 24h."( Exploring LPS-induced sepsis in rats and mice as a model to study potential protective effects of the nociceptin/orphanin FQ system.
Bath, MF; Lambert, DG; Stover, CM; Thomas, RC; Thompson, JP, 2014
)
0.4
" Whether repeated dosing would achieve greater protection remains to be examined."( Endocannabinoid degradation inhibition improves neurobehavioral function, blood-brain barrier integrity, and neuroinflammation following mild traumatic brain injury.
Impastato, RA; Katz, PS; Molina, PE; Rogers, EK; Sulzer, JK; Teng, SX, 2015
)
0.42
" Patients receiving alvimopan received a preoperative dose of 12 mg perorally and then were dosed twice daily for 7 days or until first bowel movement."( Effect of alvimopan on return of bowel function after robot-assisted radical cystectomy.
Chan, K; Heinlen, JE; Kawachi, M; Lau, C; Ruel, N; Tobis, S; Wilson, T, 2014
)
0.4
" We also demonstrate that upon acute and chronic dosing in rats, 43, a potent cyclopentyl fused pyrrolidine antagonist, reduced circulating plasma RBP4 protein levels by approximately 60%."( Design, synthesis, and evaluation of nonretinoid retinol binding protein 4 antagonists for the potential treatment of atrophic age-related macular degeneration and Stargardt disease.
Barnes, KD; Chen, P; Cioffi, CL; Conlon, MP; Cywin, CL; Dobri, N; Freeman, EE; Golden, KC; Johnson, G; Kitchen, DB; Martin, WH; Michelotti, E; Pearson, PG; Petrukhin, K; Qin, Q; Racz, B; Schwarz, DM; Stafford, DG; Zhu, L, 2014
)
0.4
"Active-phase dosing of DORA-22 induced consistent effects on sleep architecture in mice, rats, dogs, and rhesus monkeys; attenuation of active wake was accompanied by increases in both non-rapid eye movement (NREM) and rapid eye movement (REM) sleep."( Differential sleep-promoting effects of dual orexin receptor antagonists and GABAA receptor modulators.
Coleman, PJ; Fox, SV; Garson, SL; Gotter, AL; Kuduk, SD; McDonald, T; Munden, RL; Renger, JJ; Stevens, J; Tannenbaum, PL; Tye, SJ; Uslaner, JM; Winrow, CJ; Yao, L, 2014
)
0.4
" Pharmacokinetic findings with the current dosing regimen were consistent with the comparable literature and the hybrid dosing regimen."( Phase I trial of bortezomib (PS-341; NSC 681239) and "nonhybrid" (bolus) infusion schedule of alvocidib (flavopiridol; NSC 649890) in patients with recurrent or refractory indolent B-cell neoplasms.
Baz, RC; Bose, P; Colevas, AD; Coppola, D; Dawson, J; Doyle, LA; Figg, WD; Grant, S; Hogan, KT; Holkova, B; Honeycutt, C; Kang, L; Kmieciak, M; Peer, CJ; Perkins, EB; Ramakrishnan, V; Roberts, JD; Roodman, GD; Sankala, H; Shrader, E; Stuart, RK; Sullivan, D; Tombes, MB; Wan, W; Weir-Wiggins, C; Wellons, M, 2014
)
0.4
" As the nonhybrid regimen is less cumbersome than the previous hybrid dosing schedule regimen, the current schedule is recommended for successor studies."( Phase I trial of bortezomib (PS-341; NSC 681239) and "nonhybrid" (bolus) infusion schedule of alvocidib (flavopiridol; NSC 649890) in patients with recurrent or refractory indolent B-cell neoplasms.
Baz, RC; Bose, P; Colevas, AD; Coppola, D; Dawson, J; Doyle, LA; Figg, WD; Grant, S; Hogan, KT; Holkova, B; Honeycutt, C; Kang, L; Kmieciak, M; Peer, CJ; Perkins, EB; Ramakrishnan, V; Roberts, JD; Roodman, GD; Sankala, H; Shrader, E; Stuart, RK; Sullivan, D; Tombes, MB; Wan, W; Weir-Wiggins, C; Wellons, M, 2014
)
0.4
" We conclude that endogenous N/OFQ functionally opposes DOP transmission in substantia nigra reticulata and that NOP receptor antagonists might be used in combination with DOP receptor agonists to reduce their dosage while maintaining their full therapeutic efficacy."( Stimulation of δ opioid receptor and blockade of nociceptin/orphanin FQ receptor synergistically attenuate parkinsonism.
Ledonne, A; Mabrouk, OS; Mercuri, N; Morari, M; Viaro, R; Volta, M, 2014
)
0.4
"A new HPLC method for separation and determination of impurities in paracetamol, codeine phosphate hemihydrate and pitophenone hydrochloride in the presence of fenpiverinium bromide in combined suppository dosage form was developed and validated."( Separation and determination of impurities in paracetamol, codeine and pitophenone in the presence of fenpiverinium in combined suppository dosage form.
Coufal, P; Hanzlík, P; Jedlička, A; Vojta, J, 2015
)
0.42
"Drug-interaction experiments, supplemented by dose-response data, examined the effects of these compounds on locomotor activity, on striatal levels of dopamine and 3,4-dihydroxyphenylacetic acid (DOPAC), and on levels of activity-regulated cytoskeleton-associated (Arc) gene expression in the striatum and frontal cortex of male Sprague-Dawley rats."( Co-administration of the Dopaminergic Stabilizer Pridopidine and Tetrabenazine in Rats.
Klamer, D; Ponten, H; Waters, N; Waters, S, 2014
)
0.4
" Analysis of anti-CD20 mediated activation of natural killer cells isolated from patients on continued oral ibrutinib treatment suggested that repeated drug dosing inhibits these cells in vivo."( Ibrutinib interferes with the cell-mediated anti-tumor activities of therapeutic CD20 antibodies: implications for combination therapy.
Beurskens, FJ; Breij, EC; Da Roit, F; Engelberts, PJ; Golay, J; Gritti, G; Introna, M; Parren, PW; Rambaldi, A; Taylor, RP, 2015
)
0.42
" The present research work pertains to the preparation of transdermal patches of donepezil with the objective to improve its patient compliance, therapeutic efficacy and to reduce the frequency of dosing and side effects as well as to avoid its extensive first pass metabolism."( Formulation and evaluation of transdermal patches of donepezil.
Argade, NS; Dua, K; Madan, JR, 2015
)
0.42
" This dosing schedule is being further evaluated in multiple phase II studies."( A Phase I study of cyclin-dependent kinase inhibitor, AT7519, in patients with advanced cancer: NCIC Clinical Trials Group IND 177.
Chen, EX; Hirte, H; Hotte, S; Lovell, S; Lyons, J; McIntosh, L; Seymour, L; Siu, LL; Squires, M; Turner, S, 2014
)
0.4
" In a recently published phase 3 trial (RESONATE) that compared ibrutinib and ofatumumab for the treatment of relapsed and refractory chronic lymphocytic leukemia or small lymphocytic lymphoma, ibrutinib at the daily dosage of 420 mg demonstrated a significantly higher overall response rate (43% in ibrutinib vs."( A review of a novel, Bruton's tyrosine kinase inhibitor, ibrutinib.
Kim, SS; Lee, CS; Rattu, MA, 2016
)
0.43
"3-10 µg/kg/infusion) generated a biphasic dose-response curve, characteristic of drugs with reinforcing properties."( Effects of the NOP agonist SCH221510 on producing and attenuating reinforcing effects as measured by drug self-administration in rats.
Ko, MC; Lagorio, CH; Sukhtankar, DD, 2014
)
0.4
" Lethality was increased by AM251 with the higher dosage of PO, but no lethality was noted with either dosage of CPO, with or without AM251."( The cannabinoid receptor antagonist AM251 increases paraoxon and chlorpyrifos oxon toxicity in rats.
Liu, J; Pope, C, 2015
)
0.42
"3, 1, and 3 mg/kg) enhanced cumulative food intake during the first 12 h with a dome-shaped dose-response relationship in freely fed rats, with the most effective dose being 1 mg/kg."( Differential modulation of endogenous cannabinoid CB1 and CB2 receptors in spontaneous and splice variants of ghrelin-induced food intake in conscious rats.
Chen, CY; Chi, CW; Li, CP; Ting, CH, 2015
)
0.42
"The amount of propofol-remifentanil administered by the controller is consistent with current knowledge, propofol is best dosed using TBW whereas remifentanil is best dosed using IBW."( Feasibility of closed-loop co-administration of propofol and remifentanil guided by the bispectral index in obese patients: a prospective cohort comparison.
Assenzo, V; Chazot, T; Cocard, V; Fischler, M; Journois, D; Le Guen, M; Liu, N; Lory, C; Sessler, DI, 2015
)
0.42
" Vandetanib and sirolimus were orally administered on a continuous daily dosing schedule in escalating dose cohorts."( Vandetanib plus sirolimus in adults with recurrent glioblastoma: results of a phase I and dose expansion cohort study.
Batchelor, TT; Beroukhim, R; Betensky, RA; Chheda, MG; Chi, AS; Drappatz, J; Eichler, AF; Gerstner, ER; Hochberg, FH; Norden, AD; Wen, PY; Yang, D, 2015
)
0.42
"Flavopiridol or AdHTVP2G5-rev-casp3 at low dosage alone was mildly cytotoxic in vitro with a viability rate of 86."( Sequential combination therapy with flavopiridol and autocatalytic caspase-3 driven by amplified hTERT promoter synergistically suppresses human ovarian carcinoma growth in vitro and in mice.
Shen, K; Song, Y; Xia, Z; Xin, X; Zhai, X, 2014
)
0.4
"To explore the neuromuscular effects of cisatracurium besylate in morbidly obese patients when dosed according to real body weight under total intravenous anesthesia with propofol."( [Neuromuscular effects of cisatracurium besylate in obese patients].
Geng, Z; Wu, X, 2014
)
0.4
"When dosed according to real body weight, onset time of cisatracurium is shorter while clinical duration and recovery index are prolonged in morbidly obese patients compared with normal weight counterparts."( [Neuromuscular effects of cisatracurium besylate in obese patients].
Geng, Z; Wu, X, 2014
)
0.4
" No significant differences in Remifentanil dosing were observed in the four groups."( Navigator® and SmartPilot® View are helpful in guiding anesthesia and reducing anesthetic drug dosing.
Cirillo, V; De Robertis, E; Desantis, O; Iacono, C; Piazza, O; Romano, GM; Servillo, G; Tufano, R; Zito Marinosci, G, 2015
)
0.42
"Bilastine PECsw was calculated using the maximum daily dosage (20 mg), assuming that all administered bilastine was released into the aquatic environment."( Bilastine: an environmental risk assessment.
Ledo, F; Lucero, ML; Peither, A, 2015
)
0.42
" The rationale for the higher dose formulation was the expected increase in acetylcholinesterase inhibition given the dose-response relationship of donepezil, with the benefits of the higher dose being most apparent in patients with more advanced AD."( Donepezil across the spectrum of Alzheimer's disease: dose optimization and clinical relevance.
Dash, A; Jeong, SK; Kim, BC; Lee, JH; Park, KW, 2015
)
0.42
"6 mg/kg) served as a discriminative stimulus in both genotypes, with similar THC dose-response curves between groups."( Phenotypic assessment of THC discriminative stimulus properties in fatty acid amide hydrolase knockout and wildtype mice.
Vann, RE; Walentiny, DM; Wiley, JL, 2015
)
0.42
"Ibrutinib administered in fasted condition reduces exposure to approximately 60 % as compared with dosing in proximity to food-intake, regardless of timing/type of meal."( The effect of food on the pharmacokinetics of oral ibrutinib in healthy participants and patients with chronic lymphocytic leukemia.
Byrd, JC; Chauhan, V; de Jong, J; Hellemans, P; James, D; Jiao, J; Loury, DJ; Mannaert, E; Murphy, J; O'Brien, S; Skee, D; Sukbuntherng, J, 2015
)
0.42
" The visual analog scale (VAS) score, PCA dosage administered, and postoperative nausea and vomiting (PONV) were recorded at the time of discharge from the PACU (T1) and at 2 (T2), 8 (T3), 24 (T4), and 48 hours (T5) after surgery."( Dexmedetomidine versus remifentanil in postoperative pain control after spinal surgery: a randomized controlled study.
Hwang, W; Joo, J; Lee, J; Park, J, 2015
)
0.42
" Using extracellular field recordings in rat hippocampal slices, we show that a single dose of the non-selective NMDA receptor antagonist ketamine or CP-101,606, a selective antagonist of the NR2B subunit of the NMDA receptor, enhances hippocampal synaptic plasticity induced with high frequency stimulation (HFS) 24h after dosing - a time at which plasma concentrations of the drug are no longer detectable in the animal."( Effect of acute NR2B antagonist treatment on long-term potentiation in the rat hippocampus.
Bristow, LJ; Graef, JD; Kiss, L; Li, YW; Luan, FN; Luchetti, D; Newberry, K; Newton, A; Pieschl, R; Schaeffer, E; Shields, E; Simmermacher, J, 2015
)
0.42
" Thus, optimal neprilysin inhibitor dosing reveals additional cardioprotective effects on top of AT1 receptor blockade in renin-dependent hypertension."( Optimum AT1 receptor-neprilysin inhibition has superior cardioprotective effects compared with AT1 receptor blockade alone in hypertensive rats.
Batenburg, WW; Bhaggoe, UM; Clahsen-van Groningen, MC; de Vries, R; Domenig, O; Friesema, EC; Garrelds, IM; Hoorn, EJ; Jan Danser, AH; Leijten, FP; Poglitsch, M; Roksnoer, LC; van Veghel, R, 2015
)
0.42
" We reviewed articles analyzing AOT and/or OIH by remifentanil and focused on the following issues: (1) evidence of remifentanil inducing AOT and/or OIH and (2) importance of AOT and/or OIH in considering the reduction of remifentanil dosage or adopting preventive modulations."( Remifentanil-acute opioid tolerance and opioid-induced hyperalgesia: a systematic review.
Bergese, SD; Kim, SH; Soghomonyan, S; Stoicea, N,
)
0.13
" These findings are consistent with the hypothesis that the inability of memantine, AZD6765 (lanicemine) and MK-0657 to reproduce the rapid and robust antidepressant effects of ketamine in the clinic result from insufficient dosing rather than a difference in mechanism of action among these NMDAR antagonists."( Effect of NMDAR antagonists in the tetrabenazine test for antidepressants: comparison with the tail suspension test.
Czekaj, J; Kos, T; Popik, P; Skolnick, P, 2015
)
0.42
" To constitute morphine tolerance, we used a 3 day cumulative dosing regimen."( Attenuation of morphine antinociceptive tolerance by cannabinoid CB1 and CB2 receptor antagonists.
Altun, A; Bagcivan, I; Durmus, N; Gursoy, S; Ozdemir, E; Yildirim, K, 2015
)
0.42
" Diminished dosing may also offer stable hemodynamics, even during sternotomy and sternal retraction."( The effect of two different doses of remifentanil on postoperative pain and opioid consumption after cardiac surgery--a randomized controlled trial.
Florkiewicz, P; Lahtinen, P; Musialowicz, T; Pitkänen, O, 2015
)
0.42
"Total remifentanil dosing was 64 μg/kg in the higher and 22 μg/kg in the lower dosing group during the 3-h cardiac operations."( The effect of two different doses of remifentanil on postoperative pain and opioid consumption after cardiac surgery--a randomized controlled trial.
Florkiewicz, P; Lahtinen, P; Musialowicz, T; Pitkänen, O, 2015
)
0.42
"The treatment of newly diagnosed type 2 diabetes mellitus is diverse, with no clear consensus regarding the initial drug regimen or dosing to achieve optimal glycemic control."( Getting to goal in newly diagnosed type 2 diabetes using combination drug "subtraction therapy".
George, TM; Jennings, AS; Jennings, JS; Lovett, AJ, 2015
)
0.42
" We also studied the optimal dosage regimen with repeated patch application for achieving a therapeutic range using a PK simulation model."( Therapeutic dosage assessment based on population pharmacokinetics of a novel single-dose transdermal donepezil patch in healthy volunteers.
Bae, KS; Choi, HY; Hong, D; Kim, SS; Kim, YH; Lim, HS, 2015
)
0.42
"Combining two standard-of-care medications for Alzheimer's disease (AD) into a single once-daily dosage unit may improve treatment adherence, facilitate drug administration, and reduce caregiver burden."( A novel once-daily fixed-dose combination of memantine extended release and donepezil for the treatment of moderate to severe Alzheimer's disease: two phase I studies in healthy volunteers.
Boinpally, R; Chen, L; Hofbauer, RK; McClure, N; Periclou, A; Zukin, SR, 2015
)
0.42
" Current immunosuppression protocols include a combination of calcineurin inhibitors, such as tacrolimus, and antiproliferative agents (most commonly mycophenolate mofetil), with or without different dosing regimens of corticosteroids."( Current State of Immunosuppression: Past, Present, and Future.
Karam, S; Wali, RK, 2015
)
0.42
" Therefore, increasing the dosage of donepezil is a safe and effective treatment for patients with DLB who experience a relapse of BPSD."( Increased dosage of donepezil for the management of behavioural and psychological symptoms of dementia in dementia with Lewy bodies.
Ino, T; Kosaka, K; Manabe, Y; Yamanaka, K, 2016
)
0.43
" Dose-response curves (0."( Drinking sucrose or saccharin enhances sensitivity of rats to quinpirole-induced yawning.
Bentley, TA; France, CP; Kilborn, DJ; Koek, W; Serafine, KM, 2015
)
0.42
"To test the hypothesis that intranasal levocabastine (LEVO) may provide benefits as a oncedaily treatment in allergic rhinitis (AR), this non-inferiority study compared the effect at steady state of once- and twice-daily dosing with LEVO on allergen-induced nasal symptoms in AR patients."( Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Bareille, P; Gupta, A; Ignar, D; Mark, S; Miller, SR; Murdoch, RD; Patel, P; Salapatek, AM, 2015
)
0.42
"82), demonstrating noninferiority between the two LEVO dosing regimens by meeting the pre-specified criterion of an upper limit of 95% CI<1."( Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Bareille, P; Gupta, A; Ignar, D; Mark, S; Miller, SR; Murdoch, RD; Patel, P; Salapatek, AM, 2015
)
0.42
"The results of this study support the hypothesis that at steady state LEVO 200 µg taken once-daily provides similar benefit to LEVO 200 µg dosed twice-daily."( Once-daily dosing of levocabastine has comparable efficacy to twice-daily dosing in the treatment of allergic rhinitis assessed in an allergen challenge chamber.
Bareille, P; Gupta, A; Ignar, D; Mark, S; Miller, SR; Murdoch, RD; Patel, P; Salapatek, AM, 2015
)
0.42
" Cobimetinib was administered orally, once daily on either a 21-day-on/7-day-off, 14-day-on/14-day-off or 28-day-on schedule in a 28-day dosing cycle as single agent or in combination with vemurafenib."( Population pharmacokinetics and dosing implications for cobimetinib in patients with solid tumors.
Bruno, R; Budha, NR; Choong, N; Dresser, M; Eppler, S; Hack, SP; Han, K; Jin, JY; Marchand, M; Musib, L; Tikoo, N, 2015
)
0.42
" To constitute morphine analgesic tolerance, a 3-day cumulative dosing regimen was used."( The effects of endocannabinoid receptor agonist anandamide and antagonist rimonabant on opioid analgesia and tolerance in rats.
Altun, A; Bagcivan, I; Durmus, N; Gursoy, S; Ozdemir, E; Yildirim, K, 2015
)
0.42
" In the systematic review, we describe possible modes of application, dosage and side-effects for mother, fetus/ newborn."( The analgesic efficacy of remifentanil for labour. Systematic review of the recent literature.
Harazim, H; Huser, M; Janku, P; Jarkovsky, J; Kosinova, M; Littnerova, S; Stourac, P, 2016
)
0.43
" Due to the convenient dosing regimen, it is expected to be widely used in the clinical setting."( First novel once-weekly DPP-4 inhibitor, trelagliptin, for the treatment of type 2 diabetes mellitus.
Kaku, K, 2015
)
0.42
" Cohort 1 (n = 3) consisted of two phases, a single-dose (140 and 280 mg) phase and a multiple-dose (420 mg) phase of ibrutinib; cohort 2 (n = 6) included multiple doses of ibrutinib 560 mg; and cohort 3 (n = 6) included only patients with chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) dosed at ibrutinib 420 mg."( Safety and tolerability of ibrutinib monotherapy in Japanese patients with relapsed/refractory B cell malignancies.
Aoki, T; Ishizawa, K; Morishita, T; Munakata, W; Ogura, M; Suzuki, T; Takahara, S; Tobinai, K; Uchida, T; Ushijima, Y, 2016
)
0.43
"Herein, quantitation aspects of a fully automated autosampler/HPLC-MS/MS system applied for unattended droplet-based surface sampling of repaglinide dosed thin tissue sections with subsequent HPLC separation and mass spectrometric analysis of parent drug and various drug metabolites were studied."( Quantitation of repaglinide and metabolites in mouse whole-body thin tissue sections using droplet-based liquid microjunction surface sampling-high-performance liquid chromatography-electrospray ionization tandem mass spectrometry.
Chen, W; Gan, J; Kertesz, V; Van Berkel, GJ; Wang, L, 2016
)
0.43
"Medline and Embase databases were searched for randomized studies, evaluating the intraoperative use of remifentanil (>2 h) versus another analgesic or a different dosage of remifentanil, and reporting acute postoperative pain parameters such as postoperative pain scores, hyperalgesia, acute opioid tolerance, or analgesics requirements."( Is Intraoperative Remifentanil Associated With Acute or Chronic Postoperative Pain After Prolonged Surgery? An Update of the Literature.
Ahlers, SJ; Dahan, A; de Hoogd, S; Hamilton-Ter Brake, TA; Knibbe, CA; Tibboel, D; van de Garde, EM; van Dongen, EP, 2016
)
0.43
" Strychnine, an inhibitor of glycine receptor activity, reversed the threshold elevation at a subconvulsive dosage (0."( A Highly Selective Inhibitor of Glycine Transporter-1 Elevates the Threshold for Maximal Electroshock-Induced Tonic Seizure in Mice.
Cai, Y; Cheng, W; Cui, L; Li, K; Liang, G; Tao, H; Xian, W; Yin, M; Zhao, B; Zhao, J, 2016
)
0.43
" The model may be useful for identifying optimal dosing schedules for these drugs in a combination that provides adequate sedation but avoids respiratory depression."( Modeling Respiratory Depression Induced by Remifentanil and Propofol during Sedation and Analgesia Using a Continuous Noninvasive Measurement of pCO2.
Borrat, X; Castells, A; Castellví-Bel, S; Gambús, PL; Hannam, JA; Jensen, EW; Muñoz, J; Pedroso, A; Trocóniz, IF; Valencia, JF, 2016
)
0.43
" The present paper addresses the effects on vigilance states of the mGluR2 positive allosteric modulator (PAM) JNJ-40411813 at different circadian times in rats and after afternoon dosing in humans."( Translational neurophysiological markers for activity of the metabotropic glutamate receptor (mGluR2) modulator JNJ-40411813: Sleep EEG correlates in rodents and healthy men.
Ahnaou, A; Cid, JM; de Boer, P; Drinkenburg, WH; Huysmans, H; Kemp, JA; Lavreysen, H; Macdonald, GJ; Raeymaekers, L; Sinha, V; Van De Casteele, T; Van Nueten, L, 2016
)
0.43
" Dose-response curves had inverted U shapes, with peak response rates occurring at a dose of 10 μg/kg/injection."( Self-administration of the anandamide transport inhibitor AM404 by squirrel monkeys.
Goldberg, SR; Justinova, Z; Makriyannis, A; Redhi, GH; Scherma, M; Schindler, CW; Vadivel, SK, 2016
)
0.43
" Consistent with this, AZD8835 demonstrated antitumor efficacy in corresponding breast cancer xenograft models when dosed continuously."( Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers.
Avivar-Valderas, A; Cosulich, SC; Cruzalegui, F; Cumberbatch, M; Delpuech, O; Dudley, P; Ellston, R; Green, S; Hancox, UJ; Hanson, L; Hudson, K; Jones, A; McEwen, R; Morentin Gutierrez, P; Nikolaou, M; Polanska, UM; Trigwell, C; Ward, L, 2016
)
0.43
" Target engagement was confirmed in humans following single intranasal doses of 32 of ≥20 ng, and reproducible pharmacological response was demonstrated following repeat intranasal dosing at weekly intervals."( Discovery of 6-Amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one (GSK2245035), a Highly Potent and Selective Intranasal Toll-Like Receptor 7 Agonist for the Treatment of Asthma.
Ahmed, M; Ball, DI; Biggadike, K; Coe, DM; Dalmas Wilk, DA; Edwards, CD; Gibbon, BH; Hardy, CJ; Hermitage, SA; Hessey, JO; Hillegas, AE; Hughes, SC; Lazarides, L; Lewell, XQ; Lucas, A; Mallett, DN; Price, MA; Priest, FM; Quint, DJ; Shah, P; Sitaram, A; Smith, SA; Stocker, R; Trivedi, NA; Tsitoura, DC; Weller, V, 2016
)
0.43
"Herein, we report the gram-scale synthesis, pharmacokinetic profile and CNS distribution of (R)-RC-33 in the mouse to determine the most suitable dosage schedule for in vivo administration."( Toward the identification of neuroprotective agents: g-scale synthesis, pharmacokinetic evaluation and CNS distribution of (R)-RC-33, a promising SIGMA1 receptor agonist.
Bigogno, C; Canta, A; Cavaletti, G; Collina, S; Corbo, M; Curti, D; Dondio, G; Malacrida, A; Marra, A; Oggioni, N; Peviani, M; Pignataro, L; Rossi, D, 2016
)
0.43
" Pivotal study participants could enroll into the long-term extension where they received tofacitinib at 10 mg BID for 3 months, after which dosing could be 5 or 10 mg BID."( Tofacitinib, an oral Janus kinase inhibitor, for the treatment of chronic plaque psoriasis: Long-term efficacy and safety results from 2 randomized phase-III studies and 1 open-label long-term extension study.
Feldman, SR; Gardner, A; Gupta, P; Krueger, JG; Langley, RG; Luo, Y; Mallbris, L; Mebus, C; Papp, KA; Tan, H; Tatulych, S; Thaci, D; Torii, H; Tyring, S; Wolk, R, 2016
)
0.43
"After intrathecally injecting the rats with five different doses of each drug, the dose-response curves of ifenprodil and bupivacaine were constructed to obtain the 50% effective dose (ED50)."( Ifenprodil for prolonged spinal blockades of motor function and nociception in rats.
Chen, YW; Chiu, CC; Hung, CH; Wang, JJ; Wang, JN, 2016
)
0.43
" Considering that a 10 mg/day dose is approved for SAD in Japan, the present findings suggest that IR 10 mg/day donepezil is the optimal dosage for Japanese patients with SAD."( Efficacy and Safety of Sustained Release Donepezil High Dose versus Immediate Release Donepezil Standard Dose in Japanese Patients with Severe Alzheimer's Disease: A Randomized, Double-Blind Trial.
Atarashi, H; Homma, A; Kubota, N; Nakai, K; Takase, T, 2016
)
0.43
" An extended-release (XR) formulation has been designed to provide a once-daily (QD) dosing option to patients to achieve comparable pharmacokinetic (PK) parameters to the twice-daily immediate-release (IR) formulation."( Extended-Release Once-Daily Formulation of Tofacitinib: Evaluation of Pharmacokinetics Compared With Immediate-Release Tofacitinib and Impact of Food.
Alvey, C; Fletcher, T; Kushner, J; Lamba, M; Stock, TC; Wang, R, 2016
)
0.43
" Patients received once-daily vandetanib (planned dosing levels of 100, 200, and 300 mg) with concomitant daily radiotherapy (1."( Induction Therapy for Locally Advanced, Resectable Esophagogastric Cancer: A Phase I Trial of Vandetanib (ZD6474), Paclitaxel, Carboplatin, 5-Fluorouracil, and Radiotherapy Followed by Resection.
Astsaturov, IA; Berger, AC; Boland, PM; Burtness, BA; Cheng, JD; Cohen, SJ; Cooper, HS; Davey, M; Lebenthal, A; Meyer, JE; Neuman, T; Olszanski, AJ; Scott, WJ, 2017
)
0.46
"Standard methods for meta-analysis of dose-response data in epidemiology assume a model with a single scalar parameter, such as log-linear relationships between exposure and outcome; such models are implicitly unbounded."( Methods for meta-analysis of pharmacodynamic dose-response data with application to multi-arm studies of alogliptin.
Aronson, JK; Langford, O; Stevens, RJ; van Valkenhoef, G, 2018
)
0.48
" These findings were replicated by subchronic dosing studies in non-human primates, where cerebrospinal fluid levels of apoE and amyloid-β peptides were increased concomitantly with an improved peripheral lipid profile relative to that of nonselective compounds."( Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.
Ballard, J; Bennett, DJ; Bilodeau, MT; Brnardic, E; Chen, Z; Cooke, AJ; Cosden, M; DiMuzio, J; Fradera, X; Holahan, M; Kim, Y; Klein, DJ; Li, J; Li, Y; Lu, J; Maxwell, J; Meissner, R; Michener, MS; Nanda, KK; Parthasarathy, G; Rada, V; Renger, J; Rudd, MT; Stachel, SJ; Suon, S; Szczerba, P; Uebele, VN; Uslaner, JM; Wessner, K; Wu, Z; Wuelfing, P; Yuan, Y; Zerbinatti, C, 2016
)
0.43
" Preclinical pharmacokinetic studies have demonstrated that most of the dosed TAK-475 was hydrolyzed to M-I during the absorption process and the concentrations of M-I in the liver, the main organ of cholesterol biosynthesis, were much higher than those in the plasma after oral administration to rats."( Characterization of Transporters in the Hepatic Uptake of TAK-475 M-I, a Squalene Synthase Inhibitor, in Rats and Humans.
Asahi, S; Ebihara, T; Kondo, T; Moriwaki, T; Moriya, Y; Tagawa, Y; Takeuchi, T, 2016
)
0.43
"Compared with the C group, mean remifentanil dosage was significantly higher in the T group (3."( Effects of indexes of consciousness (IoC1 and IoC2) monitoring on remifentanil dosage in modified radical mastectomy: a randomized trial.
Wang, X; Wu, G; Yu, A; Yu, J; Zhang, L; Zhang, Z, 2016
)
0.43
"IoC1-targeted propofol dosing does not seem to be significantly different to hemodynamic-based monitoring, whereas IoC2 monitoring can increase remifentanil dosage during modified radical mastectomy, but the anesthetic process is more controllable and total adverse events are reduced, which improves the controllability of anesthesia."( Effects of indexes of consciousness (IoC1 and IoC2) monitoring on remifentanil dosage in modified radical mastectomy: a randomized trial.
Wang, X; Wu, G; Yu, A; Yu, J; Zhang, L; Zhang, Z, 2016
)
0.43
"IoC1-targeted propofol dosing does not seem to be significantly different to hemodynamic-based monitoring, whereas IoC2 monitoring can increase remifentanil dosage during modified radical mastectomy, but the anesthetic process is more controllable and total adverse events are reduced, which improves the controllability of anesthesia."( Effects of indexes of consciousness (IoC1 and IoC2) monitoring on remifentanil dosage in modified radical mastectomy: a randomized trial.
Wang, X; Wu, G; Yu, A; Yu, J; Zhang, L; Zhang, Z, 2016
)
0.43
"Studies have reported that co-adjuvant remifentanil can enhance electroconvulsive therapy (ECT) seizure quality, putatively by allowing a reduction in the dosage of the main anaesthetic agents, as the latter have anticonvulsant properties."( Does remifentanil improve ECT seizure quality?
Bassa, A; Gálvez, V; Hadzi-Pavlovic, D; Loo, CK; MacPherson, R; Marroquin-Harris, M; Tor, PC, 2016
)
0.43
"The dosage of remifentanil used in observation group was (98."( [The influence of the sedation based on remifentanil analgesia on the occurrence of delirium in critically ill patients].
An, Y; Feng, Y; Liu, D; Lyu, J, 2015
)
0.42
" Chronic dosing may exacerbate the emergence of drug resistance, with resistant mutations already observed in ibrutinib-treated patients."( Investigational Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis.
Norman, P, 2016
)
0.43
" Recurrent dosing of RPG before each meal is burdensome remedy."( Nanoemulsion: for improved oral delivery of repaglinide.
Akhtar, J; Aqil, M; Fareed, S; Khalid, M; Siddiqui, HH, 2016
)
0.43
" Unfortunately these molecules cause a gastric enteropathy after chronic dosing in rats."( Imidazopyridine and Pyrazolopiperidine Derivatives as Novel Inhibitors of Serine Palmitoyl Transferase.
Adams, LA; Brozinick, JT; Estridge, T; Genin, MJ; Gonzalez Valcarcel, IC; Hawkins, E; Holloway, WG; Lamar, J; Mosior, M; Reynolds, VL; Seng, T; Weidner, J; Weller, J; Yurek, D, 2016
)
0.43
" The DDI risk for cobimetinib with other CYP3A4 inhibitors and inducers needs to be assessed in order to provide dosing instructions."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
"This study demonstrates the value of using PBPK simulation to assess the clinical DDI risk inorder to provide dosing instructions with other CYP3A4 perpetrators."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
0.43
"Two patients diagnosed with long-term AU were prescribed tofacitinib citrate at a dosage of 5 mg twice daily and observed for eight months."( Efficacy of tofacitinib in treatment of alopecia universalis in two patients.
Abramovits, W; Carviel, JL; Gupta, AK, 2016
)
0.43
"Trelagliptin (SYR-472), a novel dipeptidyl peptidase-4 inhibitor, shows sustained efficacy by once-weekly dosing in type 2 diabetes patients."( Trelagliptin (SYR-472, Zafatek), Novel Once-Weekly Treatment for Type 2 Diabetes, Inhibits Dipeptidyl Peptidase-4 (DPP-4) via a Non-Covalent Mechanism.
Grimshaw, CE; Jennings, A; Kamran, R; Kinugawa, Y; Kosaka, T; Koumura, E; Nishigaki, N; Sano, H; Shi, L; Takeuchi, K; Tani, A; Ueno, H, 2016
)
0.43
"Objective Switching from sulfonylureas to repaglinide in patients with type 2 diabetes improves glycemic control; however, the optimal dosage has not been fully evaluated."( Effect of Switching from Sulphonylurea to Repaglinide Twice or Three Times Daily for 4 Months on Glycemic Control in Japanese Patients with Type 2 Diabetes.
Aoki, K; Kamiko, K; Kamiyama, H; Nakajima, S; Shinoda, K; Taguri, M; Terauchi, Y, 2016
)
0.43
"Flexible dosing of iloperidone for maintenance-phase therapy, with a modal dose of 12 mg/day was effective in preventing relapse in subjects previously stabilized on iloperidone."( A Randomized Trial of Iloperidone for Prevention of Relapse in Schizophrenia: The REPRIEVE Study.
Ahmed, S; Han, G; Mancione, L; Manning, R; Mayo, MG; Ryan, JM; Weiden, PJ; Wolfgang, CD, 2016
)
0.43
"The present research project involves development and validation of a stability-indicating HPTLC method for the estimation of naratriptan-HCl in their pharmaceutical dosage forms and its content uniformity testing."( Development and Validation of Stability-Indicating HPTLC Method for Estimation of Naratriptan Hydrochloride in Its Pharmaceutical Dosage Form and Its Content Uniformity Testing.
Bodiwala, KB; Chotalia, J; Marolia, BP; Prajapati, PB; Shah, SA, 2016
)
0.43
" Dose reductions due to adverse reactions occurred in 12% of patients, whereas 27% of patients had alectinib dosing interrupted for adverse reactions."( FDA Approval: Alectinib for the Treatment of Metastatic, ALK-Positive Non-Small Cell Lung Cancer Following Crizotinib.
Agarwal, R; Blumenthal, GM; Chen, H; Davis, G; Gieser, G; He, K; Helms, W; Keegan, P; Larkins, E; McKee, AE; Pazdur, R; Ringgold, K; Shord, S; Stephens, O; Yu, J; Zahalka, E; Zhao, H, 2016
)
0.43
"We enrolled 136 subjects and the sum of TNSS on Day 1 of the three active treatments was significantly lower than that of placebo and was maintained up to 26 h after the first dosing (Day 2)."( Therapeutic effect of bilastine in Japanese cedar pollinosis using an artificial exposure chamber (OHIO Chamber).
Hashiguchi, K; Okubo, K; Saito, A; Togawa, M; Wakabayashi, KI, 2017
)
0.46
" Propofol group (n = 25): propofol-remifentanil regimenand the dosage was adjusted to maintain the bispectral index (BIS) between 40 and 50."( Effects of Dexmedetomidine on motor- and somatosensory-evoked potentials in patients with thoracic spinal cord tumor: a randomized controlled trial.
Gelb, AW; Guo, L; Han, R; Li, Y; Meng, L; Peng, Y; Qiao, H, 2016
)
0.43
" This prescribing could have been due to the complexity of different dosing requirements, or a lack of awareness of the need for dose adjustment of most DPP-4 inhibitors in patients with renal impairment."( Demographic and Clinical Characteristics of Patients With Type 2 Diabetes Mellitus Initiating Dipeptidyl Peptidase 4 Inhibitors: A Retrospective Study of UK General Practice.
Bingham-Gardiner, P; Bolodeoku, J; Hassan, SW; Lee, S; Scowcroft, A; Spencer, W; Tebboth, A, 2016
)
0.43
"BIS monitoring of sedation in EBUS makes it possible to reduce the dosage of propofol, thereby shortening the waking time and reducing adverse events."( Bispectral Index Monitoring Reduces the Dosage of Propofol and Adverse Events in Sedation for Endobronchial Ultrasound.
Bello, S; Chacón, E; De Pablo, F; Júdez, D; Martínez Ubieto, J; Mincholé, E; Pascual, A; Quesada, N, 2016
)
0.43
" More importantly, compound 3k also strongly blocked tumor growth with the dosage of 30 mg/kg/day, and subsequent mechanism exploration suggested that this series of compounds took effect mainly through angiogenesis signaling pathways."( Discovery and Optimization of N-Substituted 2-(4-pyridinyl)thiazole carboxamides against Tumor Growth through Regulating Angiogenesis Signaling Pathways.
Chen, Y; Dong, Y; Jiang, Z; Li, Y; Pei, H; Peng, Y; Shao, T; Sun, Z; Tang, W; Wang, J; Yi, Z; Zhou, W, 2016
)
0.43
" There is no consensus regarding the optimal administration, dosing strategy, or requirements for maternal monitoring, which may pose a patient safety issue."( A Survey of Intravenous Remifentanil Use for Labor Analgesia at Academic Medical Centers in the United States.
Aaronson, J; Abramovitz, S; Landau, R; Smiley, R; Tangel, V, 2017
)
0.46
"5 %); this was significantly higher vs vehicle for both dosage regimens."( Treatment of plaque psoriasis with an ointment formulation of the Janus kinase inhibitor, tofacitinib: a Phase 2b randomized clinical trial.
Bissonnette, R; Draelos, Z; Feldman, SR; Gooderham, M; Iversen, L; Mamolo, C; Papp, KA; Ports, WC; Purohit, V; Soung, J; Wang, C, 2016
)
0.43
"In addition, the data were also gathered on the dosage of ephedrine and atropine were used, as well as the intraoperative awareness in the patients who were followed up on the first day after the operation."( [Impact of dexmedetomidine-sevoflurane anesthesia on intraoperative wake-up test in children patients undergoing scoliosis surgery].
An, HX; Quan, LX; Wang, DX, 2016
)
0.43
"Extended-release (XR) formulations enable less frequent dosing vs."( Model-Informed Development and Registration of a Once-Daily Regimen of Extended-Release Tofacitinib.
Conrado, D; Cook, J; Dikranian, A; Dowty, ME; Furst, DE; Hutmacher, MM; Krishnaswami, S; Lamba, M; Nduaka, C; Stock, T, 2017
)
0.46
"HCl) for the treatment of migraine and is available in tablet dosage forms for oral administration."( Oral transmucosal delivery of naratriptan.
Lane, ME; Sattar, M, 2016
)
0.43
" In an attempt to find the mechanism by which piperine enhances the bioavailability of curcumin, the dosage ratio (CUR: PIP) and pre-treatment with piperine were hypothesized as key factors for improving the bioavailability in this combination."( Selective reduction in the expression of UGTs and SULTs, a novel mechanism by which piperine enhances the bioavailability of curcumin in rat.
Cai, D; Chen, Y; Chen, Z; Gan, H; Huang, D; Huang, X; Sun, D; Yao, N; Zeng, Q; Zeng, X; Zhang, C; Zhao, Z; Zhong, G; Zhuo, J, 2017
)
0.46
"In all 5 studies, tofacitinib was administered at a dosage of 5 mg twice daily or 10 mg twice daily, either as monotherapy or with background methotrexate or other conventional synthetic disease-modifying antirheumatic drugs."( Brief Report: Remission Rates With Tofacitinib Treatment in Rheumatoid Arthritis: A Comparison of Various Remission Criteria.
Aletaha, D; Gruben, D; Krishnaswami, S; Mebus, C; Smolen, JS; Zwillich, SH, 2017
)
0.46
" This is supposed to explain the bell-shaped dose-response curve for anandamide in preclinical models."( A dual inhibitor of FAAH and TRPV1 channels shows dose-dependent effect on depression-like behaviour in rats.
Joca, SRL; Kirkedal, C; Liebenberg, N; Moreira, F; Wegener, G, 2017
)
0.46
" On the basis of the relationship shown, changes in clinical efficacy in association with dose change were examined in order to discuss clinical dosage from the standpoint of proper usage."( Evaluation of drug efficacy of DPP-4 inhibitors based on theoretical analysis with pharmacokinetics and pharmacodynamics.
Kimura, K; Takayanagi, R; Uchida, T; Yamada, Y, 2017
)
0.46
" Averaged for the three compounds, the quantity for the double room was 21-fold higher than for the double cage, which required again a 9-fold higher dosage than the Y-olfactometer."( Evaluation of Clove Oil, Icaridin, and Transfluthrin for Spatial Repellent Effects in Three Tests Systems Against the Aedes aegypti (Diptera: Culicidae).
Frohberger, S; Nentwig, G; Sonneck, R, 2017
)
0.46
" Treatment lasted for 7 weeks: 3 weeks of flexible dosing decided by investigators according to efficacy and tolerance (5 mg, 10 mg, or 20 mg oral pitolisant), followed by 4 weeks of stable dosing (5 mg, 10 mg, 20 mg, or 40 mg)."( Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial.
Dauvilliers, Y; Jankovic, S; Krylov, S; Lecomte, I; Lecomte, JM; Lehert, P; Mikhaylov, V; Poverennova, I; Schwartz, JC; Sonka, K; Szakacs, Z, 2017
)
0.46
" In a regulatory repeat-dose toxicity study violent episodes of "muscle spasms" were observed in Wistar rats, daily dosed with the CB1 receptor antagonist SLV326 during 5 months."( Cannabinoid antagonist SLV326 induces convulsive seizures and changes in the interictal EEG in rats.
de Bruin, N; Heijink, L; Kruse, C; Lüttjohann, A; Perescis, MF; van Luijtelaar, G; van Rijn, CM; Vinogradova, L, 2017
)
0.46
"This systematic review shows that while JAK inhibitors hold promise for many skin disorders, there are still gaps regarding the correct dosing and safety profile of these medications for dermatologic indications."( Janus kinase inhibitors in dermatology: A systematic review.
Ramot, Y; Shreberk-Hassidim, R; Zlotogorski, A, 2017
)
0.46
" There was extensive variation in remifentanil dosing (0."( Remifentanil for procedural sedation: a systematic review of the literature.
Kisilewicz, M; Rosenberg, H; Vaillancourt, C, 2017
)
0.46
" Physicians should exert caution when using remifentanil in the absence of published standardised dosing protocols in light of frequently reported paediatric respiratory depression."( Remifentanil for procedural sedation: a systematic review of the literature.
Kisilewicz, M; Rosenberg, H; Vaillancourt, C, 2017
)
0.46
" The fetal-to-maternal (F/M) ratio of remifentanil concentration at various dosing regimens is useful to manage remifentanil effects."( Influence of maternal remifentanil concentration on fetal-to-maternal ratio in pregnant ewes.
Fukumori, R; Masui, K; Nagao, Y; Sago, H; Sarentonglaga, B; Sato, M; Sumikura, H; Yamaguchi, M, 2017
)
0.46
" An integrated analysis was conducted to evaluate dosage optimality for tofacitinib in patients with moderate-to-severe plaque psoriasis and the impact of body weight on optimality in this patient population."( Evaluating Dosage Optimality for Tofacitinib, an Oral Janus Kinase Inhibitor, in Plaque Psoriasis, and the Influence of Body Weight.
Gupta, P; Hutmacher, MM; Ito, K; Krishnaswami, S; Mebus, C; Papp, K; Rottinghaus, ST; Tan, H; Valdez, H; Wolk, R, 2017
)
0.46
" In a number of patients we examined the effect of repeated injections in order to estimate the dose-response curve."( Pharmacodynamics of remifentanil. Induced intracranial spike activity in mesial temporal lobe epilepsy.
Brennum, J; Derm, L; Hogenhaven, H; Jespersen, B; Kjaer, TW; Lee, AP; Madsen, FF; Moltke, FB, 2017
)
0.46
"Aggregate data model-based meta-analysis is a regression approach to compare the dose-response and/or time-course across different treatments using summary level data from the literature."( Quantitative Evaluations of Time-Course and Treatment Effects of Systemic Agents for Psoriasis: A Model-Based Meta-Analysis.
Ahadieh, S; Checchio, T; Gupta, P; Ito, K; Kaur, M; Krishnaswami, S; Mandema, J; Puig, L; Tallman, A; Tan, H; Valdez, H; Wolk, R, 2017
)
0.46
" In the present study, a physiologically-based pharmacokinetic model was applied to compare the pharmacokinetics of tofacitinib in Japanese and Caucasians to assess the potential impact of ethnicity on the dosing regimen in the two populations."( Application of Physiologically-Based Pharmacokinetic Modeling for the Prediction of Tofacitinib Exposure in Japanese.
Hirai, M; Kurebayashi, Y; Suzuki, M; Tse, S, 2017
)
0.46
"A new model estimated from a large, diverse data set provides the PK foundation for remifentanil dosing calculations in adult obese and elderly patients."( Disposition of Remifentanil in Obesity: A New Pharmacokinetic Model Incorporating the Influence of Body Mass.
Drover, DR; Egan, TD; Kim, TK; La Colla, L; Mertens, M; Minto, CF; Obara, S; Vuyk, J, 2017
)
0.46
" The optimized methods were compared using one-way analysis of variance (ANOVA) and proved to be accurate for assay of the investigated drugs in their pharmaceutical dosage form."( Comparative study between different simple methods manipulating ratio spectra for the analysis of alogliptin and metformin co-formulated with highly different concentrations.
Ayoub, BM; Hassan, MA; Mowaka, S; Zaghary, WA, 2017
)
0.46
" It provides recommendations regarding when to continue, when to withhold, and when to restart these medications, and the optimal perioperative dosing of glucocorticoids."( 2017 American College of Rheumatology/American Association of Hip and Knee Surgeons Guideline for the Perioperative Management of Antirheumatic Medication in Patients With Rheumatic Diseases Undergoing Elective Total Hip or Total Knee Arthroplasty.
Abdel, MP; Brause, B; Chen, AF; Dasa, V; George, M; Gewurz-Singer, O; Giles, JT; Gililland, J; Goodman, M; Goodman, SM; Guyatt, G; Hurley-Rosenblatt, A; Johnson, B; Kirou, K; Lee, S; Losina, E; MacKenzie, R; Mandl, LA; Michaud, K; Mikuls, T; Miller, AS; Mont, MA; Russell, L; Sah, A; Sculco, P; Singh, JA; Sporer, S; Springer, B; Stryker, L; Turgunbaev, M; Yates, A, 2017
)
0.46
" It provides recommendations regarding when to continue, when to withhold, and when to restart these medications, and the optimal perioperative dosing of glucocorticoids."( 2017 American College of Rheumatology/American Association of Hip and Knee Surgeons Guideline for the Perioperative Management of Antirheumatic Medication in Patients With Rheumatic Diseases Undergoing Elective Total Hip or Total Knee Arthroplasty.
Abdel, MP; Brause, B; Chen, AF; Dasa, V; George, M; Gewurz-Singer, O; Giles, JT; Gililland, J; Goodman, M; Goodman, SM; Guyatt, G; Hurley-Rosenblatt, A; Johnson, B; Kirou, K; Lee, S; Losina, E; MacKenzie, R; Mandl, LA; Michaud, K; Mikuls, T; Miller, AS; Mont, MA; Russell, L; Sah, A; Sculco, P; Singh, JA; Sporer, S; Springer, B; Stryker, L; Turgunbaev, M; Yates, A, 2017
)
0.46
" To select sub-efficacious doses of both drugs, dose-response studies were first performed on the scopolamine-induced deficits of spontaneous alternation in the Y-maze task and of acquisition and retrieval processes in a passive avoidance task."( Co-modulation of an allosteric modulator of nicotinic receptor-cholinesterase inhibitor (galantamine) and a 5-HT4 receptor agonist (RS-67333): effect on scopolamine-induced memory deficit in the mouse.
Boulouard, M; Dauphin, F; Freret, T; Hamidouche, K; Lecouflet, P; Lelong-Boulouard, V, 2017
)
0.46
"Our results suggest that the developed formulation has a potential to replace the current daily dosing regimen to a less frequent dosing schedule."( Long Acting Ionically Paired Embonate Based Nanocrystals of Donepezil for the Treatment of Alzheimer's Disease: a Proof of Concept Study.
Arya, A; Banala, VT; Mishra, PR; Mishra, S; Mitra, K; Mittapelly, N; Pandey, G; Sharma, S; Shukla, S; Thalla, M, 2017
)
0.46
" elegans dosage compensation and demonstrated H4K20me1's pivotal role in regulating higher-order chromosome structure and X-chromosome-wide gene expression."( Dynamic Control of X Chromosome Conformation and Repression by a Histone H4K20 Demethylase.
Anderson, EC; Bian, Q; Brejc, K; King, DS; Kranzusch, PJ; Meyer, BJ; Preston, CG; Uzawa, S; Wheeler, BS, 2017
)
0.46
" Acquisition of self-administration and responding during increasing fixed ratio requirements were assessed, and a dose-response curve was generated."( Effects of environmental enrichment on self-administration of the short-acting opioid remifentanil in male rats.
Bardo, MT; Beckmann, JS; Chow, JJ; Hofford, RS, 2017
)
0.46
" Patients in these studies received tofacitinib dosed at 1-30 mg twice daily or 20 mg once daily, as monotherapy or with conventional synthetic disease-modifying antirheumatic drugs."( Lymphoma in the Tofacitinib Rheumatoid Arthritis Clinical Development Program.
Biswas, P; Boy, MG; Chen, C; Kwok, K; Mariette, X, 2018
)
0.48
" All patients used a stable dosage of MTX, steroids, and statins or lipid-lowering drugs."( Tofacitinib improves atherosclerosis despite up-regulating serum cholesterol in patients with active rheumatoid arthritis: a cohort study.
Amano, K; Hatta, K; Kanazawa, T; Kume, K; Kuwaba, N; Ohta, H; Yamada, S, 2017
)
0.46
" Subgroup analysis suggested that the increased risk of all-grade rash was clear across all subgroups, including first-line/second-line therapy, phase 2/phase 3 trial, sample size 200, a dosage of 100 or 300 mg, and monotherapy/combination therapy."( Risk of rash associated with vandetanib treatment in non-small-cell lung cancer patients: A meta-analysis of 9 randomized controlled trials.
Hou, S; Li, Y; Liu, Q; Liu, Y; Qi, M; Shao, L; Zhang, J, 2017
)
0.46
" Fifteen patients (five groups; 3 per group) completed dosing as follows: (1) LNF 200 mg twice-daily (BID; 12 weeks); (2) LNF 300 mg BID (12 weeks); (3) LNF 100 mg thrice-daily (5 weeks); (4) LNF 100 mg BID + pegylated interferon alfa (PEG-IFNα) 180 μg once-weekly (QW; 8 weeks); and (5) LNF 100 mg BID + ritonavir (RTV) 100 mg once-daily (QD; 8 weeks)."( Optimizing lonafarnib treatment for the management of chronic delta hepatitis: The LOWR HDV-1 study.
Bozdayi, AM; Çalişkan, A; Glenn, JS; Heller, T; Idilman, R; Kalkan, Ç; Karakaya, F; Karatayli, E; Karatayli, S; Keskin, O; Koh, C; Yurdaydin, C, 2018
)
0.48
" CPD-4645 (10 mg/kg, subcutaneously) or vehicle was dosed 1 and 7 h after status epilepticus onset in video-electroencephalography (EEG) recorded mice."( Inhibition of monoacylglycerol lipase terminates diazepam-resistant status epilepticus in mice and its effects are potentiated by a ketogenic diet.
Butler, CR; Guilmette, E; Pauletti, A; Piro, JR; Porcu, L; Rizzi, M; Salamone, A; Samad, TA; Sheehan, MJ; Terrone, G; Vezzani, A; Villa, BR, 2018
)
0.48
"Eligible subjects were randomly assigned to one of six treatment sequences and received multiple ascending doses of ASP8477, duloxetine, and placebo over three treatment periods (each consisting of 21-day dosing separated by 14-day washout periods)."( A Randomized, Double-Blind, Placebo- and Active Comparator-Controlled Phase I Study of Analgesic/Antihyperalgesic Properties of ASP8477, a Fatty Acid Amide Hydrolase Inhibitor, in Healthy Female Subjects.
Passier, P; Reeh, P; Schaffler, K; Yassen, A, 2018
)
0.48
" However, a high dosage is related to hemodynamic abnormalities such as hypotension and bradycardia."( Effects of remifentanil with or without midazolam pretreatment on the 95% effective dose of propofol for loss of consciousness during induction: A randomized, clinical trial.
Han, DW; Kim, NY; Ko, SH; Koh, JC; Park, J; You, AH, 2017
)
0.46
" Patients with rapidly progressing disease received an accelerated dosing schedule (to 400 mg per day by week 3)."( Venetoclax for chronic lymphocytic leukaemia progressing after ibrutinib: an interim analysis of a multicentre, open-label, phase 2 trial.
Barr, PM; Byrd, JC; Cheson, BD; Choi, M; Chyla, B; Coutre, S; Davids, MS; Furman, RR; Humerickhouse, RA; Jones, JA; Lamanna, N; Mato, AR; Potluri, J; Salem, AH; Verdugo, M; Wierda, WG; Woyach, J; Zhou, L, 2018
)
0.48
" Given that piperine inhibits or stimulates the activity of metabolic enzymes and transporters depending on the treatment conditions, the clinical significance of piperine-drug interactions should be assessed by varying the dose, dosing frequency, and the duration of treatment."( Piperine-mediated drug interactions and formulation strategy for piperine: recent advances and future perspectives.
Back, SY; Han, HK; Kim, HY; Lee, SH, 2018
)
0.48
"Alcohol increased the bioavailability of blonanserin and N-deethyl blonanserin in healthy subjects and the marked effect of alcohol on blonanserin bioavailability should be taken into consideration in deciding dosing schedules in clinical therapy."( Effects of Alcohol on the Pharmacokinetics of Blonanserin and N-Deethylated Blonanserin in Healthy Chinese Subjects.
Chen, Y; Deng, S; Hu, J; Lu, H; Ni, X; Peng, H; Shang, D; Wang, Z; Wen, Y; Zhang, M; Zhang, Y; Zhu, X, 2018
)
0.48
" However, a dose-response study evaluating DON after a controlled cortical impact (CCI) injury in rats did not reveal cognitive benefits."( Systemic administration of donepezil attenuates the efficacy of environmental enrichment on neurobehavioral outcome after experimental traumatic brain injury.
Bondi, CO; Bou-Abboud, CE; Cheng, JP; Day-Cooney, J; Folweiler, KA; Kline, AE; Leary, JB; Memarzadeh, K; Tehranian-DePasquale, R; Yelleswarapu, NK, 2018
)
0.48
" The proposed method is applicable for the analysis of six pharmaceutical dosage forms namely, Nesina®, Actos®, Glucophage®, Oseni®, Kazano® and Actoplus MET® tablets."( A guide for using experimental design in chromatographic method development: applied to the analysis of selected anti-diabetic pharmaceutical combinations.
Abdel-Aziz, O; Ayoub, BM, 2016
)
0.43
"The pharmacology, pharmacokinetics, clinical efficacy, safety and tolerability, dosage and administration, and place in therapy of alectinib for treatment of patients with non-small-cell lung cancer (NSCLC) are reviewed."( Alectinib for advanced
Ly, AC; Olin, JL; Smith, MB, 2018
)
0.48
" There was no inducibility difference after chronic dosing with washout."( Increased Susceptibility for Atrial and Ventricular Cardiac Arrhythmias in Mice Treated With a Single High Dose of Ibrutinib.
Jones, DL; Tuomi, JM; Xenocostas, A, 2018
)
0.48
" Using an in vitro experimental approach, the physiological role of the airway epithelium on smooth muscle relaxation has been investigated by analyzing the dose-response curves for carbachol- or histamine-induced contractions on epithelium intact versus denuded tracheal tissue."( Relaxant effect of ghrelin on guinea pig isolated tracheal smooth muscle: role of epithelial NO and PGE
Al-Ayed, MSZ, 2018
)
0.48
" The additive and synergistic inhibition of this combination additionally supports a therapeutic strategy involving lower dosing of each drug to reduce potential side effects."( Additive and synergistic inhibition of mantle cell lymphoma cell growth by combining olaparib with ibrutinib.
Curtis, A; Rajan, S; Rueter, J; Shopland, L; Zhang, R, 2018
)
0.48
" Ocular safety tolerability, exposure, and efficacy studies were conducted in rabbit and monkey models following topical ocular dosing of MGV354."( A Novel Selective Soluble Guanylate Cyclase Activator, MGV354, Lowers Intraocular Pressure in Preclinical Models, Following Topical Ocular Dosing.
Adams, C; Ehara, T; Ferrara, L; Ghosh, M; Kim, S; Li, B; McAllister, C; Mogi, M; Newton, R; Ng, CTH; Prasanna, G; Rice, DS; Stacy, R; Topley, T; Towler, C; Xiang, C; Yang, L, 2018
)
0.48
" The MGV354-induced IOP lowering was sustained up to 7 days following once-daily dosing in a monkey model of glaucoma and was greater in magnitude compared to Travatan (travoprost)-induced IOP reduction."( A Novel Selective Soluble Guanylate Cyclase Activator, MGV354, Lowers Intraocular Pressure in Preclinical Models, Following Topical Ocular Dosing.
Adams, C; Ehara, T; Ferrara, L; Ghosh, M; Kim, S; Li, B; McAllister, C; Mogi, M; Newton, R; Ng, CTH; Prasanna, G; Rice, DS; Stacy, R; Topley, T; Towler, C; Xiang, C; Yang, L, 2018
)
0.48
" The method applied for biowaiver study of Donepezil Hydrochloride (DH) as a representative model was done by comparing two different dosage forms containing 5mg DH per tablet as an application of a developed chemometric method for correcting interferences as well as for the assay and dissolution testing in its tablet dosage form."( Chemometrics-assisted spectrophotometric green method for correcting interferences in biowaiver studies: Application to assay and dissolution profiling study of donepezil hydrochloride tablets.
Elmallah, OA; Haggag, RS; Korany, MA; Mahgoub, H; Ragab, MAA, 2018
)
0.48
"Applied dosage is one important variable in determining the persistence of a repellent experienced by users but the maximum concentration in current picaridin formulation is <30%w/v."( Mosquito repellents for the traveller: does picaridin provide longer protection than DEET?
Goodyer, L; Schofield, S, 2018
)
0.48
"The low permeability of anti-malarial drugs must be borne in mind during development of effective dosage regimens of new drugs."( Absorptive and Secretory Transport of Selected Artemisinin Derivatives Across Caco-2 Cell Monolayers.
Gouws, C; Hamman, J; Haynes, RK; Heyns, J; Willers, C; Wong, HN, 2018
)
0.48
"This was an open-label, multicenter, phase-1 study to evaluate the drug interaction between steady-state ibrutinib and moderate (erythromycin) and strong (voriconazole) CYP3A inhibitors in patients with B-cell malignancies and to confirm dosing recommendations."( A drug-drug interaction study of ibrutinib with moderate/strong CYP3A inhibitors in patients with B-cell malignancies.
Chauhan, V; Córdoba, R; de Jong, J; De Wilde, S; de Zwart, L; Hellemans, P; Jiao, J; Manikhas, G; Masterson, T; Myasnikov, A; Osmanov, D; Ouellet, D; Panizo, C; Patricia, D; Snoeys, J; Sukbuntherng, J, 2018
)
0.48
" The analysis suggested no dosing modifications for age, body weight, sex, race, ethnicity, baseline PASI, or CRP based on the magnitude of exposure change."( Pharmacokinetic Characteristics of Tofacitinib in Adult Patients With Moderate to Severe Chronic Plaque Psoriasis.
Gupta, P; Ito, K; Krishnaswami, S; Langley, R; Ma, G; Rottinghaus, S; Strober, B; Tallman, A; Valdez, H; Wolk, R; Xie, R, 2018
)
0.48
" In this study, we have examined whether a prodrug design that targets arthritic joints would enhance Tofa's therapeutic efficacy, which may provide an opportunity for future development of safer Tofa dosing regimens."( Development of a Janus Kinase Inhibitor Prodrug for the Treatment of Rheumatoid Arthritis.
Galdamez, J; Goldring, SR; Lele, SM; Liu, Y; Mikuls, TR; Purdue, PE; Soni, DM; Wang, D; Wang, X; Wei, X; Wu, J; Zhao, G, 2018
)
0.48
" A separate dosing regimen was used to determine whether the drugs induced pharmacologic tolerance."( A bivalent compound targeting CCR5 and the mu opioid receptor treats inflammatory arthritis pain in mice without inducing pharmacologic tolerance.
Akgün, E; Auger, JL; Binstadt, BA; Dutta, R; Lunzer, MM; Portoghese, PS, 2018
)
0.48
" These findings suggest deterioration of the humoral immune system is associated with progressive CLL and altering the dosing of IgRT to achieve higher than conventional IgG target levels may have therapeutic activity."( Association of blood IgG with tumor necrosis factor-alpha and clinical course of chronic lymphocytic leukemia.
Huang, J; Lazarus, A; Norris, P; Shi, Y; Spaner, DE; Venema, R; Wang, G, 2018
)
0.48
" This drug is commonly prescribed either in a 5-mg or in a10-mg dosage twice daily."( Adverse drug events associated with 5mg versus 10mg Tofacitinib (Janus kinase inhibitor) twice daily for the treatment of autoimmune diseases: A systematic review and meta-analysis of randomized controlled trials.
Huang, F; Luo, ZC, 2019
)
0.51
" To test this postulate, a pilot study (NCT02801578) was designed to systematically reduce ibrutinib dosing within the same patient with CLL over the course of three 28-day cycles."( A pilot study of lower doses of ibrutinib in patients with chronic lymphocytic leukemia.
Bose, P; Chen, LS; Cruz, ND; Feng, S; Gandhi, V; Huang, X; Jain, N; Jiang, Y; Keating, MJ; Kroll, MH; Qiao, W; Thompson, PA; Wierda, WG; Wu, Q, 2018
)
0.48
" In a cisplatin-based study, rats were dosed daily for 3 days (0."( Ghrelin agonist HM01 attenuates chemotherapy-induced neurotoxicity in rodent models.
Alberti, P; Canta, A; Cavaletti, G; Chiorazzi, A; Farah, MH; Fumagalli, G; Gadiano, AJ; Liu, Y; Meregalli, C; Monza, L; Pietra, C; Polydefkis, M; Pozzi, E; Rais, R; Rodriguez-Menendez, V; Slusher, BS; Vornov, JJ; Wozniak, KM; Wu, Y, 2018
)
0.48
" Fatigue is a common adverse event during treatment with these and other TKIs and a common cause of drug discontinuation or dosage reduction."( Primary Adrenal Insufficiency During Lenvatinib or Vandetanib and Improvement of Fatigue After Cortisone Acetate Therapy.
Colombo, C; De Leo, S; Di Stefano, M; Fugazzola, L; Persani, L; Vannucchi, G, 2019
)
0.51
"We show that the occurrence of PAI may be a common cause of fatigue during lenvatinib and vandetanib treatment, and we therefore recommend testing adrenal function for a prompt start of replacement therapy to avoid treatment discontinuation, dosage reduction, and potentially severe PAI complications."( Primary Adrenal Insufficiency During Lenvatinib or Vandetanib and Improvement of Fatigue After Cortisone Acetate Therapy.
Colombo, C; De Leo, S; Di Stefano, M; Fugazzola, L; Persani, L; Vannucchi, G, 2019
)
0.51
"As oral targeted agents, such as ibrutinib, become more widely used, understanding the impact of suboptimal dosing on overall survival (OS) and progression-free survival (PFS) outside of clinical trials is imperative."( Ibrutinib Dose Adherence and Therapeutic Efficacy in Non-Hodgkin Lymphoma: A Single-Center Experience.
Baloga, E; Baran, AM; Barr, PM; Casulo, C; Friedberg, JW; Helber, M; Moore, J; Reagan, P; Williams, AM; Zent, CS, 2019
)
0.51
" Compared with placebo, more patients dosed with lasmiditan 200 mg were free of headache pain at 2 hours after dosing (32."( Lasmiditan is an effective acute treatment for migraine: A phase 3 randomized study.
Berg, PH; Dozier, G; Kuca, B; Lipton, RB; Silberstein, SD; Wietecha, L, 2018
)
0.48
"Lasmiditan dosed at 200 and 100 mg was efficacious and well tolerated in the treatment of acute migraine among patients with a high level of cardiovascular risk factors."( Lasmiditan is an effective acute treatment for migraine: A phase 3 randomized study.
Berg, PH; Dozier, G; Kuca, B; Lipton, RB; Silberstein, SD; Wietecha, L, 2018
)
0.48
" Alectinib was then resumed at half dosage without further complications."( Successful re-introduction of alectinib after inducing interstitial lung disease in a patient with lung cancer.
Dasanu, CA; Hwang, A; Iskandar, A, 2019
)
0.51
"Intra-DMH anandamide treatment yielded a U-shaped dose-response curve with no effect of the lowest (0."( Opposing roles of dorsomedial hypothalamic CB1 and TRPV1 receptors in anandamide signaling during the panic-like response elicited in mice by Brazilian rainbow Boidae snakes.
Coimbra, NC; Dos Anjos-Garcia, T, 2019
)
0.51
" Additionally, debate exists regarding the recommended dosing strategy for ibrutinib for this indication with disease remission demonstrated at 560 mg and 420 mg."( Ibrutinib for the treatment of Bing-Neel syndrome, a complication of Waldenström macroglobulinemia: Patient case report.
Arnall, JR; Hartsell, L; Janes, A; Larck, C; Park, S, 2019
)
0.51
" This review also highlights the importance of the nanoformulation of such bioactive phytochemicals that could enhance their bioavailability by providing an efficient targeted delivery system with a reduced systemic dose while resulting in a more efficient dosing at the target site."( Combating breast cancer using combination therapy with 3 phytochemicals: Piperine, sulforaphane, and thymoquinone.
Aumeeruddy, MZ; Mahomoodally, MF, 2019
)
0.51
" In most patients, cobimetinib was dosed once daily orally for 21 days on, 7 days off."( Phase Ib study of atezolizumab combined with cobimetinib in patients with solid tumors.
Bang, YJ; Bendell, J; Cha, E; Chee, CE; Chow, LQM; Das Thakur, M; Desai, J; Foster, P; Gainor, JF; Goh, BC; Hellmann, MD; Hernandez, G; Jamal, R; Kim, TW; Lee, CB; Miller, WH; Oh, DY; Pitcher, B; Siu, LL; Solomon, BJ; Wongchenko, MJ, 2019
)
0.51
" Three dosage cohorts were studied over a 28-day period (20 mg, 40 mg and 80 mg once daily)."( The oral Janus kinase/spleen tyrosine kinase inhibitor ASN002 demonstrates efficacy and improves associated systemic inflammation in patients with moderate-to-severe atopic dermatitis: results from a randomized double-blind placebo-controlled study.
Bhatia, N; Bissonnette, R; Denis, L; Dhawan, S; Forman, S; Fowler, J; Guttman-Yassky, E; Lee, M; Maari, C; Pariser, D; Pavel, AB; Rao, N; Sofen, H; Song, T; Tyring, S; Usansky, H; Zammit, DJ; Zook, M, 2019
)
0.51
" Efficacy analyses were additionally done in all dosed patients with measurable disease at baseline."( Niraparib monotherapy for late-line treatment of ovarian cancer (QUADRA): a multicentre, open-label, single-arm, phase 2 trial.
Azodi, M; Berek, JS; Chan, JK; Cloven, N; Cristea, M; DiSilvestro, P; Fleming, GF; Geller, MA; Li, Y; Luptakova, K; Matei, DE; Matulonis, UA; Miller, DS; Monk, BJ; Moore, KN; Oza, AM; Rimel, BJ; Secord, AA; Sun, K; Wahner Hendrickson, AE, 2019
)
0.51
" Animals dosed with tofacitinib citrate demonstrated marked reductions in BAL eosinophils and total protein concentrations following HDM challenge."( Preformulation and Evaluation of Tofacitinib as a Therapeutic Treatment for Asthma.
Addison, KJ; Ledford, JG; Myrdal, PB; Vallorz, E; Younis, US, 2019
)
0.51
"5 mL; n = 7), dosed once every 24 hours for 21 days."( Long-term cardiovascular effects of vandetanib and pazopanib in normotensive rats.
Carter, JJ; Cooper, SL; March, J; Woolard, J, 2019
)
0.51
" Steady-state vemurafenib concentrations were evaluated according to vemurafenib dosing and concomitant ARA use across treatment cohorts in a subset of patients from BRIM-7 and coBRIM with available concentration data."( Effect of concomitant dosing with acid-reducing agents and vemurafenib dose on survival in patients with BRAF
Ascierto, PA; Dréno, B; Flaherty, KT; Hauschild, A; Larkin, J; Lewis, K; McArthur, GA; McKenna, E; Mun, Y; Ribas, A; Zhu, Q, 2019
)
0.51
" Dosing adjustments for renal impairment were derived from a separate phase 1 study."( Population pharmacokinetics of tofacitinib in patients with psoriatic arthritis
.
Deng, C; Kanik, KS; Menon, S; Nicholas, T; Wang, Q; Xie, R, 2019
)
0.51
"Different JAKis modulated distinct cytokine pathways to varying degrees, and no agent potently or continuously inhibited an individual cytokine signaling pathway throughout the dosing interval."( Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations.
Byers, NL; Higgs, RE; Lee, J; Macias, WL; McInnes, IB; Na, S; Ortmann, RA; Rocha, G; Rooney, TP; Taylor, PC; Wehrman, T; Zhang, X; Zuckerman, SH, 2019
)
0.51
" The established PBPK model was capable of accurately predicting complex rifampicin-induced alterations in the profiles of glibenclamide, repaglinide, and coproporphyrin I (an endogenous biomarker of OATP1B activities) with various dosing regimens."( Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for Predicting Interactions With Drugs and an Endogenous Biomarker via Complex Mechanisms Including Organic Anion Transporting Polypeptide 1B Induction.
Asaumi, R; Imawaka, H; Kusuhara, H; Lee, W; Menzel, K; Nunoya, KI; Sugiyama, Y, 2019
)
0.51
"Once daily oral mesalamine dosing is equivalent to split dosing in mild-moderate UC."( Maneuvering Clinical Pathways for Ulcerative Colitis.
Dassopoulos, T; Johnson, CM; Linzay, CD, 2019
)
0.51
" This beneficial effect possibly results from selective JAK/STAT-blockade by adequate tofacitinib dosage with inhibition of pro-inflammatory responses and permission of a balance-shift toward regulatory pathways."( Tofacitinib Reprograms Human Monocytes of IBD Patients and Healthy Controls Toward a More Regulatory Phenotype.
Bettenworth, D; Cordes, F; Foell, D; Kessel, C; Lenker, E; Schmidt, HH; Spille, LJ; Varga, G; Weinhage, T, 2020
)
0.56
" Dosing regimens of cefepime and zidebactam alone and in combination that achieved epithelial lining fluid (ELF) exposures in mice approximating human ELF exposures after doses of 2 g of cefepime/1 g of zidebactam every 8 h (1 h infusion) were utilized; controls were vehicle-dosed."( Efficacy of human-simulated bronchopulmonary exposures of cefepime, zidebactam and the combination (WCK 5222) against MDR Pseudomonas aeruginosa in a neutropenic murine pneumonia model.
Abdelraouf, K; Kidd, JM; Nicolau, DP, 2020
)
0.56
" These measures were equivalent to those obtained after 6 days of daily dosing by tofacitinib."( Quantitative tracking of inflammatory activity at the peak and trough plasma levels of tofacitinib, a Janus kinase inhibitor, via in vivo
Abria, C; Chaudhari, AJ; Harmany, ZT; Kundu-Raychaudhuri, S; Raychaudhuri, S; Raychaudhuri, SP; Smith, CM, 2019
)
0.51
" These measures were equivalent to those obtained after 6 days of daily dosing by tofacitinib."( Quantitative tracking of inflammatory activity at the peak and trough plasma levels of tofacitinib, a Janus kinase inhibitor, via in vivo
Abria, C; Chaudhari, AJ; Harmany, ZT; Kundu-Raychaudhuri, S; Raychaudhuri, S; Raychaudhuri, SP; Smith, CM, 2019
)
0.51
"For patients with UC, flexible maintenance dosing therapy may confer advantages for safety, efficacy, costs and patient preference."( Efficacy and safety of tofacitinib dose de-escalation and dose escalation for patients with ulcerative colitis: results from OCTAVE Open.
Armuzzi, A; Bressler, B; Chan, G; Colombel, JF; Danese, S; Lawendy, N; Lindsay, JO; Maller, E; Marren, A; Marshall, JK; Panés, J; Salese, L; Sandborn, WJ; Sands, BE; Su, C; Tsilkos, K; Zhang, H, 2020
)
0.56
" Clinical trials addressing its efficacy and the optimal dosing schedule in the present context are underway, and results are eagerly awaited."( Alectinib activity in chemotherapy-refractory metastatic RET-rearranged non-small cell lung carcinomas: A case series.
Alessi, JVM; de Galiza Barbosa, F; Feher, O; Gongora, ABL; Katz, A; Oliveira, LJC; Ribeiro, MFSA; Sacardo, KP; Shimada, AK; Zucchetti, BM, 2020
)
0.56
" Submaximal ibrutinib dosing will have to be further systematically evaluated."( Descriptive analysis of dosing and outcomes for patients with ibrutinib-treated relapsed or refractory chronic lymphocytic leukemia in a Canadian centre.
Banerji, V; Brown, K; Bucher, O; Dawe, DE; Dhaliwal, DH; Geirnaert, M; Hibbert, I; Johnston, JB; Uminski, K, 2019
)
0.51
"5 ml of pristane and after 2 months they were orally dosed with resveratrol combinations for 4 months."( Combinatorial therapeutic effect of resveratrol and piperine on murine model of systemic lupus erythematosus.
Bhatnagar, A; Pannu, N, 2020
)
0.56
" The animals were dosed through oral gavage (50 mg/kg) and intravenously (2."( Bioanalytical method development and validation of MES207, a neuropeptide FF receptor antagonist, and its application in preclinical pharmacokinetics.
Avery, BA; Harrison, S; Kamble, SH; King, TI; McCurdy, CR; Mesangeau, C; Mottinelli, M; Roewekamp, AC; Sharma, A, 2019
)
0.51
" In addition, BGT-1 deficiency or dosing with NNC 05-2090 stimulated the expression of the anti-apoptotic gene, c-Met in the liver, suggesting the involvement of c-Met in the function on hepatocytes of BGT-1 apoptosis."( Betaine/GABA transporter-1 (BGT-1) deficiency in mouse prevents acute liver failure in vivo and hepatocytes apoptosis in vitro.
Ci, L; Fei, J; Huang, F; Huang, Q; Li, Q; Liu, Z; Lu, T; Shen, R; Shi, J; Sun, R; Wan, Z; Wang, Z; Yang, H; Yang, X; Zhang, M, 2020
)
0.56
"The dose-response relationships of antipsychotic drugs for schizophrenia are not well defined, but such information would be important for decision making by clinicians."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" Dose-response curves were constructed with random-effects dose-response meta-analyses and a spline model."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" For some drugs, higher than currently licensed doses might be tested in further trials, because their dose-response curves did not plateau."( Dose-Response Meta-Analysis of Antipsychotic Drugs for Acute Schizophrenia.
Crippa, A; Davis, JM; Leucht, S; Orsini, N; Patel, MX; Siafis, S, 2020
)
0.56
" Other endpoints included total Drug Attitude Inventory 10 (DAI-10) scores, EuroQol-5 Dimension (EQ-5D) effect values, and a patient questionnaire about the dosage form."( Long-Term Safety and Efficacy of Blonanserin Transdermal Patches in Japanese Patients with Schizophrenia: A 52-Week Open-Label, Multicenter Study.
Higuchi, T; Ishigooka, J; Iwata, N; Kanamori, Y; Matsumoto, M; Nakamura, H; Naoi, I, 2020
)
0.56
" In phase 3, patients recorded in electronic diaries whether they experienced unusual feelings after dosing with lasmiditan that they had not felt with a migraine before, and were contacted to determine if an AE had occurred."( Issues Impacting Adverse Event Frequency and Severity: Differences Between Randomized Phase 2 and Phase 3 Clinical Trials for Lasmiditan.
Berg, PH; Hundemer, HP; Khanna, R; Krege, JH; Kudrow, D; Ossipov, MH; Pozo-Rosich, P, 2020
)
0.56
" Volinanserin also increased PPI in control and MK-801-treated mice, presenting an inverted U-shaped dose-response curve."( Effects of combined 5-HT
Cardoso, AR; Castro, NG; Hammes, CSO; Macena, MV; Marques, AM; Neves, GA; Pinheiro, FML, 2020
)
0.56
" The findings suggested that the DDI between genistein and repaglinide is mediated by P-gp, and a dosage adjustment may be needed when they are co-administered in a clinical setting."( Molecular pharmacokinetic mechanism of the drug-drug interaction between genistein and repaglinide mediated by P-gp.
Huo, X; Jin, H; Liu, K; Ma, X; Meng, Q; Sun, H; Sun, P; Tan, A; Wang, C; Wu, J; Zhu, Y, 2020
)
0.56
"Despite strong preclinical rationale, combined cobimetinib-mediated MEK inhibition and GDC-0994-mediated ERK inhibition was not tolerable on two 28-day dosing schedules in which GDC-0994 was given for 21 days continuously and cobimetinib administered over 21 days either continuously or intermittently."( A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors.
Burris, H; Dokainish, H; Lockhart, A; LoRusso, P; Mueller, L; Murray, E; Park, E; Sarkar, I; Shapiro, G; Singh, J; Tagen, M; Weekes, C, 2020
)
0.56
"Cobimetinib and GDC-0994 were administered orally on two separate dosing schedules."( A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors.
Burris, H; Dokainish, H; Lockhart, A; LoRusso, P; Mueller, L; Murray, E; Park, E; Sarkar, I; Shapiro, G; Singh, J; Tagen, M; Weekes, C, 2020
)
0.56
" However, overlapping AEs and cumulative toxicity could not be adequately managed on either dosing schedule, restricting the ability to further develop this combination."( A Phase Ib Study to Evaluate the MEK Inhibitor Cobimetinib in Combination with the ERK1/2 Inhibitor GDC-0994 in Patients with Advanced Solid Tumors.
Burris, H; Dokainish, H; Lockhart, A; LoRusso, P; Mueller, L; Murray, E; Park, E; Sarkar, I; Shapiro, G; Singh, J; Tagen, M; Weekes, C, 2020
)
0.56
" A link between the dosing compartment and the dihydrodiol-ibrutinib central compartment was added to assess for high first-pass hepatic metabolism."( Population Pharmacokinetics of Ibrutinib and Its Dihydrodiol Metabolite in Patients with Lymphoid Malignancies.
Allal, B; Chatelut, E; De Barros, S; Despas, F; Dupré, L; Gallais, F; Obéric, L; Protin, C; Quillet-Mary, A; Thomas, F; White-Koning, M; Ysebaert, L, 2020
)
0.56
" While the dosage of tofacitinib needs to be adjusted for patients with moderate hepatic impairment status, it is not the case for either baricitinib or upadacitinib."( Critical Assessment of Pharmacokinetic Drug-Drug Interaction Potential of Tofacitinib, Baricitinib and Upadacitinib, the Three Approved Janus Kinase Inhibitors for Rheumatoid Arthritis Treatment.
Babu, RJ; Dash, RP; Madgula, LMV; Srinivas, NR; Thomas, JA; Veeravalli, V, 2020
)
0.56
"To assess the efficacy and safety profiles of different dosing regimens of tofacitinib, baricitinib, and upadacitinib, novel selective oral Janus activated kinase inhibitors, in rheumatoid arthritis (RA)."( Efficacy and Safety of Tofacitinib, Baricitinib, and Upadacitinib for Rheumatoid Arthritis: A Systematic Review and Meta-Analysis.
Davis, JM; Luo, F; Matteson, EL; Murad, MH; Sun, L; Vassallo, R; Wang, F; Wang, S, 2020
)
0.56
"The 45 mg BID pridopidine dosage remained safe and tolerable over 60 months."( Additional Safety and Exploratory Efficacy Data at 48 and 60 Months from Open-HART, an Open-Label Extension Study of Pridopidine in Huntington Disease.
Abler, V; Auinger, P; Gandhi, S; Geva, M; Gordon, MF; Grachev, ID; Hayden, M; Kieburtz, K; McGarry, A; Mehra, M; Papapetropoulos, S; Savola, JM, 2020
)
0.56
"9% (15/101) in the 40 mg group, and no dose-response relationship was found."( Randomised clinical trial: minesapride vs placebo for irritable bowel syndrome with predominant constipation.
Fukudo, S; Hamatani, T; Inada, H; Kazumori, K; Miwa, H; Nakada, Y, 2020
)
0.56
" This approach may also be useful in predicting pharmacokinetics under untested or complex situations (eg, when a combination of intrinsic and extrinsic factors may impact pharmacokinetics) when conducting clinical studies may be difficult, in response to health authority questions regarding dosing in special populations, or for labeling discussions."( Application of Physiologically Based Pharmacokinetic Modeling to Predict Drug Exposure and Support Dosing Recommendations for Potential Drug-Drug Interactions or in Special Populations: An Example Using Tofacitinib.
Dowty, ME; Gupta, P; Krishnaswami, S; Menon, S; Tse, S, 2020
)
0.56
" Combination dosage forms of various API incorporating piperine as a bio-enhancer can be a potential area of thrust for upcoming drug design and development."( Propitious Profile of Peppery Piperine.
Aggarwal, G; Bakshi, H; Dhingra, GA; Nagpal, M; Singh, M, 2021
)
0.62
"This Phase Ib study explored combination dosing of the allosteric MEK1/2 inhibitor cobimetinib and the ATP-competitive pan-AKT inhibitor ipatasertib."( A phase Ib open-label dose escalation study of the safety, pharmacokinetics, and pharmacodynamics of cobimetinib (GDC-0973) and ipatasertib (GDC-0068) in patients with locally advanced or metastatic solid tumors.
Bendell, JC; Chan, IT; Chang, I; Cho, DC; LoRusso, P; Meng, RD; Musib, L; Patel, P; Sanabria-Bohorquez, S; Shapiro, GI; Wongchenko, M; Yan, Y, 2021
)
0.62
" In the meantime, gabapentin appears to be the most evidence-based widely available uremic pruritus treatment, as long as care is taken with dosing and monitoring of side-effects."( Recent advances in the treatment of uremic pruritus.
Collister, D; Rigatto, C; Trachtenberg, AJ, 2020
)
0.56
" In determining which patients should be offered front-line maintenance PARP inhibitors, and which agent to use, there are multiple factors to consider, including FDA indication, dosing preference, toxicity, risks versus benefits for each patient population, and cost."( Movement of Poly-ADP Ribose (PARP) Inhibition into Frontline Treatment of Ovarian Cancer.
Coleman, RL; Onstad, M; Westin, SN, 2020
)
0.56
" The terminal half-life was 30-40 h, resulting in sustained drug concentrations for the entire 24-h dosing interval at steady state."( Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain.
Baldwin, RM; Bourdet, DL; Graham, RA; Kanodia, J; Lo, A, 2021
)
0.62
" Population pharmacokinetic/pharmacodynamic analysis justified using a fixed dosing regimen with no dose adjustments across a broad population and can be used to inform dosing strategies in future clinical studies."( Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain.
Baldwin, RM; Bourdet, DL; Graham, RA; Kanodia, J; Lo, A, 2021
)
0.62
" However, multiple dosing may not be widely applicable in the field."( Reduced treatment frequencies with bumped kinase inhibitor 1369 are effective against porcine cystoisosporosis.
Choi, R; Greber, P; Hulverson, MA; Joachim, A; Michaels, SA; Ojo, KK; Ruttkowski, B; Shrestha, A; Van Voorhis, WC; Whitman, GR, 2020
)
0.56
" Zolpidem has been marketed in new dosage forms that include sublingual tablets and oral spray formulations."( New pharmacologic agents for insomnia and hypersomnia.
Earl, DC; Van Tyle, KM, 2020
)
0.56
"Recent advancements in the treatment of insomnia includes agents with novel mechanisms, new indications, and new dosage forms."( New pharmacologic agents for insomnia and hypersomnia.
Earl, DC; Van Tyle, KM, 2020
)
0.56
"Rimegepant ODT is an efficacious migraine treatment option with a novel mechanism of action, convenient dosage form, and limited adverse effect profile."( Rimegepant Orally Disintegrating Tablet for Acute Migraine Treatment: A Review.
Cope, NE; DeFalco, AP; Lazim, R, 2021
)
0.62
" Remifentanil delivery is inflexible and dosing cannot be adjusted to the clinical need and responses of individual patients."( De-mystifying the "Mixifusor".
Absalom, AR; Rigby-Jones, AE; Robert Sneyd, J; Rushton, AR, 2020
)
0.56
" Ibrutinib is currently not available in a liquid oral dosage form."( Ibrutinib treatment via alternative administration in a patient with chronic lymphocytic leukemia and dysphagia.
Arnall, JR; DiSogra, KY; Janes, A; Moore, DC; Park, SI; Tran, T, 2021
)
0.62
" Drug bioavailability of anti-diabetic drugs can be significantly increased by prolonging gastric retention time through gastro-retentive dosage form such as floating microspheres."( Repaglinide and Metformin-Loaded Amberlite Resin-Based Floating Microspheres for the Effective Management of Type 2 Diabetes.
Jain, AK; Jain, SK; Mishra, K; Sahu, P, 2021
)
0.62
" Dosed with normal/high fat food the selected formulation showed comparable exposure and a modest increase in DNX systemic PK was observed with PPI dependent on meal type."( Negative Food Effect of Danirixin: Use of PBPK Modelling to Explore the Effect of Formulation and Meal Type on Clinical PK.
Ambery, C; Bloomer, JC; Butler, JM; Charles, SJ; D'Amico, D; Donald, A; Hingle, MI; Lloyd, RS; Miller, B; Paul, A; Tal-Singer, R; Zhu, X, 2020
)
0.56
" Phase II study was conducted to examine the effects of TS-141 30 (once a day), 60 (once a day), 120 mg (60 mg twice a day), or placebo, that is within the exposure in the maximum dosage of Asverin, in children and adolescents with ADHD, and was designed as an 8-week treatment, randomized, parallel group, double-blind, placebo-controlled trial recruiting 6-17-year-old children and adolescents diagnosed with ADHD."( Using the drug repositioning approach to develop a novel therapy, tipepidine hibenzate sustained-release tablet (TS-141), for children and adolescents with attention-deficit/hyperactivity disorder.
Iwamori, S; Mizuno-Yasuhira, A; Nishino, I; Okada, T; Saito, K; Saito, T; Shinoda, S; Tomoda, A; Umeuchi, H; Urano, H; Yamashita, Y, 2020
)
0.56
" An optimized dose-response curve is then presented, introducing (±) amphetamine hydrochloride (0."( A Molecularly Imprinted Polymer-based Dye Displacement Assay for the Rapid Visual Detection of Amphetamine in Urine.
Arreguin-Campos, R; Caldara, M; Cleij, TJ; Diliën, H; Eersels, K; Heidt, B; Jimenez-Monroy, KL; Lowdon, JW; Rogosic, R; van Grinsven, B, 2020
)
0.56
" Potentially, lower IFN-α and IP-10 levels as well as once-weekly intranasal dosing vs daily subcutaneous or intramuscular dosing with recombinant type I IFNs could explain the lack of pregnancy effects; however, there was an undesired impact on offspring immune function."( GSK2245035, a TLR7 agonist, Does Not Increase Pregnancy Loss in Cynomolgus Monkeys.
Baker, A; Bray, M; Hillegas, AE; Maier, CC; Phadnis-Moghe, AS; Posobiec, LM; Price, MA; Stanislaus, DJ, 2021
)
0.62
" Remarkably, acute dosing limited to the first 3 d of life significantly enhanced survival in two severe SMA mice models, easing the burden on neonates and demonstrating the compound as suitable for evaluation of follow-on therapies without potential drug-drug interactions."( Short-duration splice promoting compound enables a tunable mouse model of spinal muscular atrophy.
Androphy, EJ; Hodgetts, KJ; Lorson, CL; Lusic, H; Osman, EY; Quist, KM; Rietz, A, 2021
)
0.62
"Investigation of the effect of infliximab, adalimumab, ixekizumab, secukinumab and tofacitinib on Health-Related Quality of Life (HRQOL) measured by the DLQI in adult plaque psoriatic patients with respect to the patients' race, type of used agent/placebo, agent's dosage and treatment duration as well as the DLQI score prior to and after commencement of treatment."( The effects of selected biologics and a small molecule on Health-Related Quality of Life in adult plaque psoriasis patients: A systematic review and meta-analysis.
Bartosińska, J; Karpińska-Mirecka, A; Krasowska, D, 2020
)
0.56
" Remarkably, both contractility (impedance) and extracellular field potentials (EFPs) could be detected from the actively beating spheroids over long durations and after automated dosing with pharmacological agents."( A Scalable Approach Reveals Functional Responses of iPSC Cardiomyocyte 3D Spheroids.
Burnham, MP; Fertig, N; Haddrick, M; Harvey, R; Sargeant, R, 2021
)
0.62
" Herein we evaluate the effects of acute and repeated dosing of SR-17018, oxycodone and morphine in additional models of pain-related behaviors."( Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain.
Acevedo-Canabal, A; Bannister, TD; Bohn, LM; Cameron, MD; Grim, TW; Kennedy, NM; Pantouli, F; Schmid, CL, 2021
)
0.62
" A once-per-day dosing regimen may be recommended as clinically efficacious."( Safety, Pharmacokinetics, and Pharmacodynamics of a Dipeptidyl Peptidase-4 Inhibitor: A Randomized, Double-Blinded, Placebo-Controlled Daily Administration of Fotagliptin Benzoate for 14 Days for Type 2 Diabetes Mellitus.
Ding, YH; Li, QQ; Li, XJ; Li, Y; Sun, HG; Wu, M; Zhang, H; Zhu, XX, 2021
)
0.62
" Individualized niraparib dosing is effective and safe and should be considered standard practice in this setting."( Niraparib maintenance therapy in patients with platinum-sensitive recurrent ovarian cancer using an individualized starting dose (NORA): a randomized, double-blind, placebo-controlled phase III trial
Abulizi, G; An, RF; Chen, LP; Chen, QH; Cui, H; Gao, YN; Hao, M; Hou, JM; Huang, XH; Huang, Y; Kong, BH; Li, GL; Liu, JH; Liu, ZL; Lou, G; Lu, WG; Lu, X; Mirza, MR; Tian, XF; Wang, DB; Wang, J; Wang, K; Wang, L; Wen, H; Wu, LY; Wu, XH; Yan, XJ; Yang, HY; Yang, JX; Yin, RT; Zhang, C; Zhang, Y; Zhou, Q; Zhu, JQ, 2021
)
0.62
"The PK results support weight-based dosing of lasmiditan in pediatric patients with migraine and no new safety or tolerability issues were identified."( Pharmacokinetics, Safety, and Tolerability of Lasmiditan in Pediatric Patients with Migraine.
Dennehy, EB; Kerr, L; Khanna, R; Komori, M; Nery, ESM; Tsai, M; Wilbraham, D; Winner, P, 2021
)
0.62
" This is different from optimal dosing identified for other indications and dosing of remifentanil should be specific to the clinical context in which it is used."( Study to evaluate the optimal dose of remifentanil required to ensure apnea during magnetic resonance imaging of the heart under general anesthesia.
Arnold, P; Cowen, R; Davis, A; Hampson, LV; Jaki, T; Kaleem, M; Sanaulla, S; Tan, J; Wadsworth, I; Williams, A, 2021
)
0.62
" The data have implications for developing novel, non-prostaglandin therapeutics for IOP-lowering and cytoprotective effects with the possibility of an eye drop dosing regimen of once every 3 days for patients with glaucoma."( Nanoencapsulated hybrid compound SA-2 with long-lasting intraocular pressure-lowering activity in rodent eyes.
Acharya, S; Behera, S; Chaphalkar, RM; Ellis, DZ; Kodati, B; Krishnamoorthy, RR; Millar, JC; Nguyen, KT; Nguyen, T; Stankowska, DL, 2021
)
0.62
"The model can be used to simulate clinical trials or various dosing scenarios."( Population Pharmacokinetics of Ibrutinib in Healthy Adults.
Al-Ghazawi, M; Najib, N; Najib, O; Saleh, MI; Salem, I, 2021
)
0.62
" Thus, the glucocorticoid dosage was successfully tapered low enough until no side effects were observed."( Two cases of rheumatoid arthritis complicated by organising pneumonia successfully treated with tofacitinib therapy.
Kameoka, J; Kodera, T; Oka, Y; Shirota, Y; Takeda, T; Tsutsumi, T, 2021
)
0.62
" Participants recorded their response to treatment prior to dosing and for 48 h postdose."( Phase 2 randomized placebo-controlled study of lasmiditan for the acute treatment of migraine in Japanese patients.
Homma, G; Katagiri, H; Komori, M; Sakai, F; Takeshima, T; Tanji, Y, 2021
)
0.62
" A statistically significant linear dose-response relationship for pain freedom was achieved at 2 h by a Cochran-Armitage trend test (p < 0."( Phase 2 randomized placebo-controlled study of lasmiditan for the acute treatment of migraine in Japanese patients.
Homma, G; Katagiri, H; Komori, M; Sakai, F; Takeshima, T; Tanji, Y, 2021
)
0.62
"Antiviral efficacy of DS003 was assessed in mucosal tissue explants (ecto-cervical, penile and colorectal) and in trans-infection models (co-cultures of dendritic or mucosal migratory cells with CD4+ T cells) with several dosing times (2, 24 h and sustained) and in combination with a fusion inhibitor."( The entry inhibitor DS003 (BMS-599793): a BMS-806 analogue, provides superior activity as a pre-exposure prophylaxis candidate.
Aldon, Y; Armanasco, N; Harman, S; Herrera, C; Nuttall, J; Rogers, P; Shattock, RJ; Stieh, D; Ziprin, P, 2021
)
0.62
"The objective of this study was to evaluate bilastine dosing recommendations in older adults and overcome the limitation of insufficient data from phase I studies in this underrepresented population."( Application of a dual mechanistic approach to support bilastine dose selection for older adults.
Campo, C; García-Bea, A; Kim, C; Leal, N; Lo Re, V; Lukas, JC; Rodriguez, M; Schmidt, S; Suarez, E; Vozmediano, V, 2021
)
0.62
" According to a literature review, no UV-visible spectrophotometric method has been reported yet for simultaneous estimation of montelukast sodium and bilastine in their combined pharmaceutical dosage forms."( Risk Assessment-Based Enhanced Analytical Quality-by-Design Approach to Eco-Friendly and Economical Multicomponent Spectrophotometric Methods for Simultaneous Estimation of Montelukast Sodium and Bilastine.
Mishra, A; Prajapati, P; Surati, P; Tamboli, J, 2021
)
0.62
"The developed and validated methods were applied for assay of combined pharmaceutical dosage forms of montelukast sodium and bilastine and results were found to be in good agreement with their label claims."( Risk Assessment-Based Enhanced Analytical Quality-by-Design Approach to Eco-Friendly and Economical Multicomponent Spectrophotometric Methods for Simultaneous Estimation of Montelukast Sodium and Bilastine.
Mishra, A; Prajapati, P; Surati, P; Tamboli, J, 2021
)
0.62
" An assay of combined tablet dosage forms of montelukast sodium and bilastine was then carried out using the developed methods."( Risk Assessment-Based Enhanced Analytical Quality-by-Design Approach to Eco-Friendly and Economical Multicomponent Spectrophotometric Methods for Simultaneous Estimation of Montelukast Sodium and Bilastine.
Mishra, A; Prajapati, P; Surati, P; Tamboli, J, 2021
)
0.62
" SCO-267 is safe and well tolerated and exhibits once-daily oral dosing potential."( SCO-267, a GPR40 Full Agonist, Stimulates Islet and Gut Hormone Secretion and Improves Glycemic Control in Humans.
Kagawa, T; Kobayashi, A; Matsuoka, O; Moritoh, Y; Nishizaki, H; Watanabe, M, 2021
)
0.62
" Here, we used mouse footpad infection models in immunocompetent BALB/c and immunocompromised SCID-beige mice to compare different Q203 doses, different dosing schedules, and treatment durations ranging from 1 day to 2 weeks, on long-term outcomes."( Impact of Dose, Duration, and Immune Status on Efficacy of Ultrashort Telacebec Regimens in Mouse Models of Buruli Ulcer.
Almeida, DV; Converse, PJ; Komm, O; Nuermberger, EL; Omansen, TF, 2021
)
0.62
" This method was successfully applied to pure form, tablet dosage form, spiked human (urine and plasma)."( Development of novel univariate and multivariate validated chemometric methods for the analysis of dasatinib, sorafenib, and vandetanib in pure form, dosage forms and biological fluids.
Abdelhameed, AS; Alanazi, AM; AlRabiah, H; Alruqi, OS; Attia, MI; Attwa, MW, 2022
)
0.72
" Here, we show that cantils (previously known as nubbins) arise as one of the many phenotypic consequences of aneuploidy resulting from chromosome dosage imbalances in Arabidopsis polyaneuploids despite normal reproductive transition in long-day photoperiods."( Cantil - a new organ or a morphological oddity?
Bondada, R; Kulaar, DS; Maruthachalam, R; Siddiqi, I, 2021
)
0.62
"A set of six clinical samples from an ongoing phase I trial dosing patients with chronic lymphocytic leukemia (CLL) with TG-1701, a novel irreversible and highly specific BTKi, were characterized by phosphoproteomic and RNA sequencing (RNA-seq) analysis."( Antitumor Activity of the Novel BTK Inhibitor TG-1701 Is Associated with Disruption of Ikaros Signaling in Patients with B-cell Non-Hodgkin Lymphoma.
Armengol, M; Bech-Serra, JJ; Blecua, P; Bosch, F; De La Torre, C; Esteller, M; Fernández-Serrano, M; Menéndez, P; Miskin, H; Musulen, E; Normant, E; Profitós Pelejà, N; Reyes-Garau, D; Ribeiro, ML; Roué, G; Santos, JC; Sedó Mor, A; Vinyoles, M, 2021
)
0.62
" A weight- and platelet count-based individualised dosage regimen introduced during the trial (and subsequently approved) appeared to improve haematological tolerability."( Niraparib: A Review in First-Line Maintenance Therapy in Advanced Ovarian Cancer.
Lee, A, 2021
)
0.62
" Starting treatment at a personalised lower dosage may also reduce the likelihood of adverse drug reactions."( Niraparib: A Review in First-Line Maintenance Therapy in Advanced Ovarian Cancer.
Lee, A, 2021
)
0.62
" In all subjects dosed with telacebec (10 to 800 mg), telacebec was well tolerated and did not lead to any significant or serious adverse events."( Safety, Tolerability, and Pharmacokinetics of Telacebec (Q203), a New Antituberculosis Agent, in Healthy Subjects.
Ahn, J; Choi, J; Hutchings, J; Jeon, Y; Kang, H; Kim, J; Nam, K; Park, D; Shin, BS; Shin, S; van Niekerk, C, 2022
)
0.72
" We sought to identify the optimal dosing combination, based on efficacy and toxicity, utilizing a continual reassessment method of 6 combinations of IBR (280 mg, 420 mg, and 560 mg by mouth daily) and VEN (max dose of 200 mg and 400 mg by mouth daily)."( Dose-finding study of ibrutinib and venetoclax in relapsed or refractory mantle cell lymphoma.
Budde, LE; Chen, RW; Cohen, JB; Kahl, BS; Petroni, GR; Portell, CA; Varhegyi, NE; Wages, NA; Williams, ME, 2022
)
0.72
" Ruxolitinib dosing was based on a previous phase I trial."( Janus kinases restrain chronic lymphocytic leukemia cells in patients on ibrutinib: Results of a phase II trial.
Gallagher, J; Luo, Y; Shi, Y; Spaner, DE; Tsui, H; Wang, G, 2021
)
0.62
" Previous preclinical studies suggested that an intermittent dosing of these drugs could delay the emergence of resistance."( Intermittent BRAF inhibition in advanced BRAF mutated melanoma results of a phase II randomized trial.
Arance, A; Basterretxea, L; Bellido, L; Berciano-Guerrero, MA; Berrocal, A; Campos, B; Cerezuela, P; de la Cruz, L; Diaz Beveridge, R; Drozdowskyj, A; Espinosa, E; Gonzalez-Cao, M; Lopez-Martin, JA; Mayo de Las Casas, C; Molina, MA; Montagut, C; Muñoz-Couselo, E; Ochenduszko, S; Oramas, J; Puertolas, T; Rodriguez, D; Villanueva, MJ, 2021
)
0.62
" The starting dosage of 20 mg of pimavanserin or placebo could be adjusted to 34 mg or 10 mg within the first 8 weeks of the study, after which dosage remained stable until the end of the study."( Pimavanserin for negative symptoms of schizophrenia: results from the ADVANCE phase 2 randomised, placebo-controlled trial in North America and Europe.
Abbs, B; Arango, C; Bugarski-Kirola, D; Fava, M; Liu, IY; Nasrallah, H; Stankovic, S, 2022
)
0.72
" However, given the small effect size, further investigation with optimised dosing is warranted to determine the clinical significance of this effect."( Pimavanserin for negative symptoms of schizophrenia: results from the ADVANCE phase 2 randomised, placebo-controlled trial in North America and Europe.
Abbs, B; Arango, C; Bugarski-Kirola, D; Fava, M; Liu, IY; Nasrallah, H; Stankovic, S, 2022
)
0.72
"To analyze alogliptin in its pharmaceutical dosage forms and human plasma, a sensitive, inexpensive, simple, and precise spectrofluorimetric method was developed and tested."( Hantzsch condensation reaction as a spectrofluorometric method for determination of alogliptin, an antidiabetic drug, in pure form, tablet form, and human and rat plasma.
Gahlan, AA; Haredy, AM; Taher, MA; Tammam, AS, 2022
)
0.72
" Managing type-2 diabetes mellitus with repaglinide is considered a burdensome therapy, as it requires frequent dosing of repaglinide before each meal to maintain its therapeutic plasma concentration due to its short plasma half-life of approximately one hour."( A Review on Recent Controlled Release Strategies for Oral Drug Delivery of Repaglinide (a BCS Class II Drug).
Abdalhafez, A; Abu-Zaid, A; Albetawi, S, 2021
)
0.62
" • Dosing up from tofacitinib 5 to 10 mg BID was associated with improved efficacy up to 12 months versus staying on 5 mg BID, and dosing down from 10 to 5 mg BID was not generally associated with a significant loss of efficacy."( Effect of dose adjustments on the efficacy and safety of tofacitinib in patients with rheumatoid arthritis: a post hoc analysis of an open-label, long-term extension study (ORAL Sequel).
Cohen, SB; Furst, DE; Killeen, T; Kwok, K; Mueller, RB; Schulze-Koops, H; von Kempis, J; Wang, L, 2022
)
0.72
"The first phase 2a trial showed a correlation between dosage and bacterial load in patient sputum, which should be confirmed using a direct measurement method such as colony-forming unit counting."( Telacebec: an investigational antibacterial for the treatment of tuberculosis (TB).
Lee, BS; Pethe, K, 2022
)
0.72
", dysphagia) occur in up to 40% of the adult general population, particularly among the elderly prescribed solid oral dosage forms."( In Vitro Stability and Recovery Studies of Pimavanserin in Water and in Different Vehicles Orally Administered.
Adegbenle, YH; Bokser, AD; Norton, JC; Stoisavljevic, V, 2022
)
0.72
" Subsequently, radiotelemetry was used to continuously measure body temperature and locomotor activity before (baseline), during, and after the 5-day dosing regimens."( Evidence for spontaneous cannabinoid withdrawal in mice.
Bergman, J; Iliopoulos-Tsoutsouvas, C; Makriyannis, A; Nikas, SP; Papanastasiou, I; Paronis, C, 2022
)
0.72
" Ibrutinib dosing was held (≥7 days) for 79 patients and reduced for 31 patients because of AEs; these AEs resolved or improved in 85% (67 of 79) and 90% (28 of 31) of patients, respectively."( Up to 8-year follow-up from RESONATE-2: first-line ibrutinib treatment for patients with chronic lymphocytic leukemia.
Bairey, O; Barr, PM; Burger, JA; Coutre, SE; Dearden, C; Ghia, P; Grosicki, S; Hillmen, P; Hsu, E; Kipps, TJ; Li, JY; McCarthy, H; Moreno, C; Offner, F; Owen, C; Robak, T; Szoke, A; Tedeschi, A; Zhou, C, 2022
)
0.72
" In addition, baricitinib has recently received Emergency Use Authorization from the US Food and Drug Administration, although the instruction provided dosing information only for adults."( Physiologically-Based Pharmacokinetic Modelling to Investigate Baricitinib and Tofacitinib Dosing Recommendations for COVID-19 in Geriatrics.
Chan, ECY; Wang, Z, 2022
)
0.72
" Despite no reported efficacy of extended-release formulations in refractory BD yet, such a dosage form has pharmacokinetic parameters that are comparable to those of conventional immediate-release formulations."( Extended-release tofacitinib for refractory Behçet disease: A case report.
Hsu, SM; Wang, CR; Wong, TW, 2022
)
0.72
" The dose-response curves showed that the anticonvulsant activity of pitolisant changed in a dose-dependent manner."( Anticonvulsant activity of the histamine H3 receptor inverse agonist pitolisant in an electrical kindling model of epilepsy.
Beheshti, S; Wesal, MW, 2022
)
0.72
"These analyses provide important quantitative pharmacologic support for benefit/risk assessment of the 500 mg/day dosage of tepotinib as being appropriate for the treatment of NSCLC harboring METex14 skipping alterations."( Exposure-response analyses for the MET inhibitor tepotinib including patients in the pivotal VISION trial: support for dosage recommendations.
Berghoff, K; Dong, J; Girard, P; Goteti, K; Hietala, SF; Johne, A; Nyberg, J; Papasouliotis, O; Strotmann, R; Venkatakrishnan, K; Xiong, W, 2022
)
0.72
"Male and female hRAMP1 mice were dosed with compound or vehicle and challenged with a charcoal meal suspension via oral gavage."( Characterization of transit rates in the large intestine of mice following treatment with a CGRP antibody, CGRP receptor antibody, and small molecule CGRP receptor antagonists.
Heinz, BA; Huang, X; Johnson, KW; Li, B; Li, X; Yu, J, 2022
)
0.72
"The structures of the isolated compounds 1 and 2 were identified by NMR and HRESIMS analyses, and their antiviral activity against CHIKV was assessed by a dose-response assay employing BHK-21 cells and CHIKV-nanoluc, a recombinant virus carrying the nanoluciferase gene reporter."( In vitro antiviral activity of piperidine alkaloids from Senna spectabilis flowers on Chikungunya virus infection.
da Silva Bolzani, V; Danuello, A; Freitas, TR; Jardim, ACG; Martins, DOS; Novais, RM; Pivatto, M; Santos, IA, 2022
)
0.72
" Oral administration of tofacitinib, a JAK inhibitor, was not associated with clinical or macroscopic effects on bone growth and development in a rat juvenile animal study (JAS) with tofacitinib dosing starting on postnatal day (PND) 21."( Lack of direct bone effect of tofacitinib, a JAK inhibitor, in juvenile rats and evaluation of the association between offspring growth and femur length.
Bowman, CJ; Campion, SN; Cappon, GD; Catlin, NR; Coder, PS; Davis, S; Hollingshead, BD; Millard, C; Nowland, WS; Potter, DM; Radi, ZA; Stethem, CM, 2022
)
0.72
"To examine published evidence on the two tofacitinib dosing strategies used in UC treatment, including expert interpretation of the data and how they could inform clinical practice."( Review article: guide to tofacitinib dosing in patients with ulcerative colitis.
Dubinsky, MC; Irving, PM; Leung, Y, 2022
)
0.72
"05) for pain freedom at 2 h post dose across all patient subgroups and lasmiditan doses, except for CVRF (100 mg and 200 mg), migraine with aura (50 mg), triptan response (50 mg), and time to dosing (200 mg)."( Efficacy of Lasmiditan Across Patient and Migraine Characteristics in Japanese Patients with Migraine: A Secondary Analysis of the MONONOFU Trial.
Komori, M; Ozeki, A; Takeshima, T; Tanji, Y; Tatsuoka, Y, 2022
)
0.72
" This analysis aimed to develop pharmacokinetic (PK) and pharmacodynamic (PD; BTK occupancy [BTKO]) models of evobrutinib and simulate PK and BTKO profiles under alternative dosing regimens."( Population pharmacokinetic and pharmacodynamic modeling of evobrutinib in healthy adult participants.
Dyroff, M; Girard, P; Mitchell, D; Papasouliotis, O, 2022
)
0.72
"2,3 The goal of this study is to investigate the long-term response of recalcitrant DM to oral and topical tofacitinib at varied dosing regimens."( A Retrospective Review of Tofacitinib in the Treatment of Refractory Dermatomyositis.
Eason, C; Elston, D; Plante, J; Robinson, I; Santa Lucia, G, 2022
)
0.72
" However, the appropriate donepezil dosage is still a matter of debate."( The measured CSF/plasma donepezil concentration ratio but not individually measured CSF and plasma concentrations significantly increase over 24 h after donepezil treatment in patients with Alzheimer's disease.
Angelucci, F; Dlabkova, A; Hort, J; Karasova, JZ; Kuca, K; Novotny, M; Pavelek, Z; Pejchal, J; Valis, M, 2023
)
0.91
" Such dosing regimen provides optimal conditions for reducing hemodynamic response to laryngoscopy and EI."( Effect of different doses of remifentanil on the cardiovascular response after endotracheal intubation: a randomized double-blind study.
Galambos, IF; Krtinic, D; Pap, D; Preveden, M; Radovanovic, D; Stanisavljevic, S; Vickovic, S; Videnovic, J; Videnovic, N; Zdravkovic, R, 2023
)
0.91
" In particular, we observed a correlation between ubrogepant dosage and muscle strain and between Body Mass Index (BMI) and liver function values."( Ubrogepant and rimegepant: systematic review, meta-analysis, and meta-regression of clinical studies.
Dong, G; Kjærgaard, NA; Sessa, M; Shakibfar, S, 2023
)
0.91
" We induced experimental colitis by transfer of CD4+CD25- isolated T cells into RAG2-/- (T and B cell deficient) mice and treated these mice with tofacitinib for 5-6 weeks either with a dosage of 10 or 40 mg/kg body weight immediately after CD4+ transfer or started treatment after first symptoms of disease for several weeks."( Tofacitinib fails to prevent T cell transfer colitis in mice but ameliorates disease activity.
Hriczko, JT; Ohl, K; Pappas, A; Schippers, A; Subramanyam, SH; Tenbrock, K; Wagner, N, 2023
)
0.91
" In Group P, remifentanil dosage during general anesthesia was determined according to pupil dilation reflex; in Group C, it was adjusted according to hemodynamic changes."( Pupillary monitoring decreases remifentanil consumption during laparoscopic uterine surgery and improves postoperative recovery.
Chen, C; Li, H; Li, N; Wang, Y; Wu, H; Yan, S; Yang, Y; Yu, L; Yu, Y; Zhang, Z, 2023
)
0.91
"Patient 1 underwent a trial of Tofacitinib at a dosage of 5 mg twice daily for one month, with notable improvement."( Case Report: Morbihan disease treated with tofacitinib successfully.
Cai, SQ; Chi, CC; Li, ZY, 2023
)
0.91
" The mean dosage of glucocorticoids was 34."( Efficacy and Safety of Tofacitinib in Anti-Melanoma Differentiation-Associated 5 Gene Antibody-Positive Dermatomyositis.
Duan, J; Li, S; Lu, X; Wang, G; Wang, J; Zhang, L, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (38,512)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906865 (17.83)18.7374
1990's5853 (15.20)18.2507
2000's10111 (26.25)29.6817
2010's12161 (31.58)24.3611
2020's3522 (9.15)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 69.90

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index69.90 (24.57)
Research Supply Index10.72 (2.92)
Research Growth Index4.69 (4.65)
Search Engine Demand Index130.83 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (69.90)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5,221 (12.98%)5.53%
Reviews3,071 (7.63%)6.00%
Case Studies1,854 (4.61%)4.05%
Observational130 (0.32%)0.25%
Other29,959 (74.46%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]