Page last updated: 2024-12-06

oxazolidin-2-one

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Description

Oxazolidin-2-ones are a class of heterocyclic compounds that have gained significant attention in medicinal chemistry due to their diverse pharmacological properties. They are commonly synthesized through a variety of methods, including the reaction of an amino alcohol with a carbonyl compound, or by ring-closing metathesis. Oxazolidin-2-ones have been shown to exhibit a wide range of biological activities, including antimicrobial, antiviral, and anti-inflammatory effects. They have also been explored as potential therapeutic agents for the treatment of various diseases, such as cancer, diabetes, and Alzheimer's disease. The unique structural features of oxazolidin-2-ones, particularly their ability to interact with biological targets via hydrogen bonding and other non-covalent interactions, make them attractive candidates for drug discovery. Their importance lies in their potential applications in various fields, including medicine, agriculture, and materials science. Extensive research is conducted to investigate their synthesis, structure-activity relationships, and biological effects, with the goal of developing novel and effective therapeutic agents.'

Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

oxazolidinone : An oxazolidine containing one or more oxo groups. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID73949
CHEMBL ID1867161
CHEBI ID1237
MeSH IDM0249955

Synonyms (60)

Synonym
carbamic acid, .gamma.-lactone
oxazolidin-2-one
nsc-38240
nsc38240
2-oxazolidone
1,3-oxazolidin-2-one
nsc35382
nsc-35382
wln: t5mvotj
oxazolidone
einecs 207-840-9
ai3-38980
nsc 35382
brn 0106251
carbamic acid, (2-hydroxyethyl)-, gamma-lactone
oxazolidinone
inchi=1/c3h5no2/c5-3-4-1-2-6-3/h1-2h2,(h,4,5
oxazolidine,2-one
497-25-6
2-oxazolidinone
C06695
2-oxazolidinone, 98%
smr000857362
MLS001335929
MLS001335930
O0188
AKOS000119963
51667-26-6
A827830
2h-oxazol-2-id-4-one;oxazolidin-2-one
CHEBI:1237 ,
HMS2231L03
4-27-00-02516 (beilstein handbook reference)
z4d49w92pp ,
unii-z4d49w92pp
oxazolidinones
FT-0613254
hydroxy-oxazoline
2-oxo-1,3-oxazolidine
oxazolodinone
oxazolidine-2-one
W-106010
CHEMBL1867161
carbamic acid, (2-hydroxyethyl)-, .gamma.-lactone
2-oxazolidine
2-oxotetrahydro-1,3-oxazole
mfcd00005268
DTXSID2074326
CS-W007548
2-oxazolidinon
F0001-1296
SY003480
Q425555
hydroxyoxazoline
STL183293
STR03231
AMY39498
C93484
EN300-19697
Z104474784

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Adverse experiences reported are generally dose related, mild to moderate and resolve spontaneously."( Clinical safety of 311C90: aggregated data from patients and volunteers to date.
Earl, NL, 1996
)
0.29
" Safety assessments include electrocardiograms, the frequency, intensity and duration of adverse experiences, and routine haematology, urinalysis and clinical chemistry measures."( Evaluation of the long-term safety and efficacy of 311C90 in the treatment of migraine.
Geraud, GE, 1996
)
0.29
" These results suggest that T-794 is an effective and particularly safe antidepressant and that it may make an important contribution in the treatment of depressive disorders."( In vivo characterization of T-794, a novel reversible inhibitor of monoamine oxidase-A, as an antidepressant with a wide safety margin.
Iwata, H; Katayama, T; Kato, M; Matsuoka, Y; Narita, H; Yamamura, M, 1998
)
0.3
" The most frequent adverse effects were nausea and dizziness."( [Safety profile of 311C90 (zolmitriptan)].
Morales Asín, F, 1998
)
0.3
" Linezolid is well tolerated: the most common adverse events (gastrointestinal effects, headache) are reported in frequencies similar to those reported for comparator agents."( Efficacy and safety of linezolid in the treatment of skin and soft tissue infections.
Hau, T, 2002
)
0.31
"8%) of the 191 episodes of infection, patients experienced one or more adverse events or exhibited one or more abnormal laboratory results; in 35 (18."( The efficacy and safety of linezolid as treatment for Staphylococcus aureus infections in compassionate use patients who are intolerant of, or who have failed to respond to, vancomycin.
Birmingham, MC; Forrest, A; Moise, PA; Schentag, JJ, 2002
)
0.31
" Linezolid was well-tolerated in this patient population, with an overall adverse event rate of 17."( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
0.32
"Linezolid was safe and effective in treating resistant Gram-positive infections in neutropenic cancer patients."( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
0.32
"Clinical trials have shown that linezolid (600 mg twice daily in adults) is safe and generally well tolerated for up to 28 days."( Safety and tolerability of linezolid.
French, G, 2003
)
0.32
" Drug-related adverse events were primarily transient."( Worldwide assessment of linezolid's clinical safety and tolerability: comparator-controlled phase III studies.
Cammarata, S; Hafkin, B; Isturiz, R; Le, V; Oliphant, TH; Remington, J; Rubinstein, E; Smith, LG; Standiford, HC, 2003
)
0.32
" Because of the increasing use of linezolid, it is important to review the common adverse events (AEs) associated with its use in children with the use of data from clinical trials."( Safety and tolerability of linezolid in children.
Bruss, JB; Edge-Padbury, B; Goldfarb, J; Kaplan, SA; Naberhuis-Stehouwer, S; Saiman, L; Wible, K, 2003
)
0.32
"Linezolid was safe and well-tolerated in pediatric patients with community-acquired pneumonia, otitis media, SSSIs and infections caused by Gram-positive resistant pathogens."( Safety and tolerability of linezolid in children.
Bruss, JB; Edge-Padbury, B; Goldfarb, J; Kaplan, SA; Naberhuis-Stehouwer, S; Saiman, L; Wible, K, 2003
)
0.32
" However, the apparent increase in observed adverse events, particularly bone marrow suppression, seen with prolonged administration, means that treatment of such patients must be undertaken with careful surveillance, at least until these complications are better understood."( The safety and efficacy of linezolid in orthopaedic practice for the treatment of infection due to antibiotic-resistant organisms.
Giannoudis, PV; Harwood, PJ, 2004
)
0.32
" Overall, adverse events occurred in 32."( Zolmitriptan nasal spray exhibits good long-term safety and tolerability in migraine: results of the INDEX trial.
Charlesworth, BR; Diener, HC; Dowson, AJ; Färkkilä, M; Gawel, M; Green, J; Hansen, SB, 2005
)
0.33
" Seven of 10 patients experienced serious adverse events, which led to withdrawal of linezolid in all seven."( Efficacy and safety of linezolid in multidrug resistant tuberculosis (MDR-TB)--a report of ten cases.
Brubakk, O; Sandven, P; von der Lippe, B, 2006
)
0.33
" Adverse hematological events have been reported."( Possibly linezolid-induced peripheral and central neurotoxicity: report of four cases.
Biron, F; Boibieux, A; Chidiac, C; Ferry, T; Issartel, B; Petiot, P; Peyramond, D; Ponceau, B; Simon, M, 2005
)
0.33
"Two de novo peripheral neuropathies and one worsening of a preexisting toxic neuropathy have been observed."( Possibly linezolid-induced peripheral and central neurotoxicity: report of four cases.
Biron, F; Boibieux, A; Chidiac, C; Ferry, T; Issartel, B; Petiot, P; Peyramond, D; Ponceau, B; Simon, M, 2005
)
0.33
" Close neurological monitoring should be recommended in prolonged linezolid therapy and coadministration of a serotonin reuptake inhibitor or antihistamine should be avoided to limit neurological adverse events."( Possibly linezolid-induced peripheral and central neurotoxicity: report of four cases.
Biron, F; Boibieux, A; Chidiac, C; Ferry, T; Issartel, B; Petiot, P; Peyramond, D; Ponceau, B; Simon, M, 2005
)
0.33
" Patients were also evaluated for adverse drug reactions due to linezolid."( The effectiveness and safety of oral linezolid for the primary and secondary treatment of osteomyelitis.
Aneziokoro, CO; Cannon, JP; Lentino, JR; Pachucki, CT, 2005
)
0.33
" Distribution of adverse events, including reported hematologic events, was similar between groups, except that linezolid was associated with fewer drug-related adverse events (52 [17."( Efficacy and safety of linezolid compared with vancomycin in a randomized, double-blind study of febrile neutropenic patients with cancer.
Hartman, CS; Jaksic, B; Leonard, LB; Martinelli, G; Perez-Oteyza, J; Tack, KJ, 2006
)
0.33
"We requested from the US Food and Drug Administration all postmarketing adverse event reports regarding linezolid that included serotonin toxicity or any report describing cognitive or behavioral symptoms and autonomic and neuromuscular excitability."( Serotonin toxicity associated with the use of linezolid: a review of postmarketing data.
Adra, M; Gillman, PK; Lawrence, KR, 2006
)
0.33
" Thirteen patients required an intervention to prevent permanent impairment or required hospitalization for the adverse event."( Serotonin toxicity associated with the use of linezolid: a review of postmarketing data.
Adra, M; Gillman, PK; Lawrence, KR, 2006
)
0.33
" Assessment of causality using the Naranjo adverse drug reaction probability scale revealed a probable relationship between this adverse drug event and linezolid therapy."( Bell's palsy associated with linezolid therapy: case report and review of neuropathic adverse events.
Bruno-Murtha, LA; Thai, XC, 2006
)
0.33
" New rare adverse events are likely to follow."( Tongue discoloration in an elderly kidney transplant recipient: Treatment-related adverse event?
Amir, KA; Arsura, EL; Balogun, SA; Bobba, RK; Clarke, B; Evans, JM; Nagy-Agren, S, 2006
)
0.33
" Based on the Naranjo probability scale, the calculated score for tongue discoloration as a drug-related adverse event was 7 out of a maximum score of 13 points, designating it as a probable cause."( Tongue discoloration in an elderly kidney transplant recipient: Treatment-related adverse event?
Amir, KA; Arsura, EL; Balogun, SA; Bobba, RK; Clarke, B; Evans, JM; Nagy-Agren, S, 2006
)
0.33
" We present this case to increase clinicians' awareness of the potential adverse event."( Tongue discoloration in an elderly kidney transplant recipient: Treatment-related adverse event?
Amir, KA; Arsura, EL; Balogun, SA; Bobba, RK; Clarke, B; Evans, JM; Nagy-Agren, S, 2006
)
0.33
" The aim of this study was to evaluate the influences of pyridoxine, rifampin, and renal function on hematological adverse events."( Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
Bové, A; García, S; Marcos, M; Martínez, JA; Martínez, JC; Mensa, J; Ortega, M; Peñarroja, G; Soriano, A, 2007
)
0.34
" The most common adverse events were thrombocytopenia (n = 5) and anemia (n = 5), necessitating treatment discontinuation in 3 patients."( Efficacy and safety of linezolid for Gram-positive orthopedic infections: a prospective case series.
Hamilton, CW; Rao, N, 2007
)
0.34
"The optic nerve is quite vulnerable to the toxic effect of drugs."( [Toxicity of recent and less recent drugs on the optic nerve. Does Viagra cause blindness?].
Cordonnier, M, 2007
)
0.34
" However, haematological toxic effects of linezolid frequently limit its prolonged use, especially in patients with poor marrow reserves such as those with cancer receiving chemotherapy."( The role of vitamin B6 in the prevention of haematological toxic effects of linezolid in patients with cancer.
Adachi, J; Chemaly, RF; Hachem, R; Raad, I; Rolston, K; Ying, J; Youssef, S, 2008
)
0.35
" We found no significant differences in the rate of haematological toxic effects between the two patient groups."( The role of vitamin B6 in the prevention of haematological toxic effects of linezolid in patients with cancer.
Adachi, J; Chemaly, RF; Hachem, R; Raad, I; Rolston, K; Ying, J; Youssef, S, 2008
)
0.35
"Damage of the optic nerve (optic neuropathy) may be caused, apart from other reasons, by an adverse drug effect."( [Adverse effect optic neuropathy].
Martini, BC, 2008
)
0.35
"Tigecycline is safe and effective in hospitalized patients with serious infection caused by MRSA."( Efficacy and safety of tigecycline compared with vancomycin or linezolid for treatment of serious infections with methicillin-resistant Staphylococcus aureus or vancomycin-resistant enterococci: a Phase 3, multicentre, double-blind, randomized study.
Babinchak, T; Beuran, M; Bochan, M; Cooper, CA; Dartois, N; Dimov, R; Dukart, G; Ellis-Grosse, EJ; Fichev, G; Florescu, I; Gandjini, H; Razbadauskas, A, 2008
)
0.35
"Since linezolid was licensed, rare-but-serious adverse events caused by inhibition of mitochondrial protein synthesis have been identified."( Toxicity of extended courses of linezolid: results of an Infectious Diseases Society of America Emerging Infections Network survey.
Beekmann, SE; Gilbert, DN; Polgreen, PM, 2008
)
0.35
" Anacetrapib was well tolerated, and the incidence of adverse events was similar for placebo and all active treatment groups."( Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib as monotherapy and coadministered with atorvastatin in dyslipidemic patients.
Bloomfield, D; Carlson, GL; Littlejohn, TW; McKenney, JM; Mitchel, Y; Pasternak, RC; Sapre, A; Sisk, CM; Tribble, D, 2009
)
0.35
"To review the literature (including latest publications) about the adverse events of linezolid and its overall safety."( Update on the safety of linezolid.
Falagas, ME; Metaxas, EI, 2009
)
0.35
"The range of adverse events of linezolid is growing; new ones, such as nephro-toxicity and Bell's palsy, have been reported."( Update on the safety of linezolid.
Falagas, ME; Metaxas, EI, 2009
)
0.35
" Our findings demonstrate no adverse effect on the times to neutrophil or platelet engraftment with linezolid use."( Hematologic safety profile of linezolid in the early periengraftment period after allogeneic stem cell transplantation.
Chou, J; Chung, D; Cohen, N; Heller, G; Mihu, CN; Papanicolaou, GA; Seo, SK, 2009
)
0.35
" The main adverse events were thrombocytopenia grade 1-3 and anemia grade 2-3 (four and two patients, respectively)."( Efficacy and safety of linezolid in immunocompromised children with cancer.
Chatzi, F; Chrousos, G; Karamolegou, K; Moschovi, M; Santou, A; Tourkantoni, N; Trimis, G; Tsotra, M, 2010
)
0.36
"Linezolid may be another effective and safe therapy to treat infections from resistant Gram-positive bacteria in immunocompromised children, even in young ages."( Efficacy and safety of linezolid in immunocompromised children with cancer.
Chatzi, F; Chrousos, G; Karamolegou, K; Moschovi, M; Santou, A; Tourkantoni, N; Trimis, G; Tsotra, M, 2010
)
0.36
" Adverse events were similar to each drug's established safety profile."( Efficacy and safety of linezolid versus vancomycin for the treatment of complicated skin and soft-tissue infections proven to be caused by methicillin-resistant Staphylococcus aureus.
Baruch, AM; Bhattacharyya, H; Dryden, MS; Itani, KM; Kunkel, MJ; Weigelt, JA, 2010
)
0.36
" Sustained pain-free response with no adverse events has been recommended as a composite endpoint which measures the efficacy and tolerability attributes that patients desire."( Sustained pain freedom and no adverse events as an endpoint in clinical trials of acute migraine treatments: application to patient-level data from a trial of the CGRP receptor antagonist, telcagepant, and zolmitriptan.
Assaid, C; Dodick, DW; Ho, TW; Kost, J; Lines, C, 2011
)
0.37
" Endpoints were 2-24-hour sustained pain freedom and no adverse events from 0-24 hours (SPF24NAE), 2-24 hour sustained pain relief and no adverse events from 0-24 hours (SPR24NAE), pain freedom at 2 hours and no adverse events from 0-24 hours (PF2NAE), and pain relief at 2 hours and no adverse events from 0-24 hours (PR2NAE)."( Sustained pain freedom and no adverse events as an endpoint in clinical trials of acute migraine treatments: application to patient-level data from a trial of the CGRP receptor antagonist, telcagepant, and zolmitriptan.
Assaid, C; Dodick, DW; Ho, TW; Kost, J; Lines, C, 2011
)
0.37
" All doses were safe and well tolerated."( Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis.
Bedarida, G; Campbell, S; Jakubiec, W; Kumar, V; Ladutko, L; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, A; Wallis, RS; Zhu, T, 2011
)
0.37
" The primary end points were the percent change from baseline in LDL cholesterol at 24 weeks (HDL cholesterol level was a secondary end point) and the safety and side-effect profile of anacetrapib through 76 weeks."( Safety of anacetrapib in patients with or at high risk for coronary heart disease.
Ashraf, TB; Barter, P; Brinton, EA; Cannon, CP; Dansky, HM; Davidson, M; Gibbons, P; Gotto, AM; Liu, SX; Mitchel, Y; Shah, S; Stepanavage, M; Zafarino, J, 2010
)
0.36
"Treatment with anacetrapib had robust effects on LDL and HDL cholesterol, had an acceptable side-effect profile, and, within the limits of the power of this study, did not result in the adverse cardiovascular effects observed with torcetrapib."( Safety of anacetrapib in patients with or at high risk for coronary heart disease.
Ashraf, TB; Barter, P; Brinton, EA; Cannon, CP; Dansky, HM; Davidson, M; Gibbons, P; Gotto, AM; Liu, SX; Mitchel, Y; Shah, S; Stepanavage, M; Zafarino, J, 2010
)
0.36
" TP was safe and well tolerated at all dose levels."( Phase 2, randomized, double-blind, dose-ranging study evaluating the safety, tolerability, population pharmacokinetics, and efficacy of oral torezolid phosphate in patients with complicated skin and skin structure infections.
Bien, P; Bulitta, JB; Corey, GR; DeAnda, C; Mehra, P; Prokocimer, P; Surber, J, 2011
)
0.37
" We did not observe any further adverse events, especially no severe neurological complications (e."( Efficacy and safety of linezolid in liver transplant patients.
Juntermanns, B; Kaiser, GM; Mathe, Z; Paul, A; Radunz, S; Saner, FH; Treckmann, J, 2011
)
0.37
" However, little is known about the mechanism of this side effect and the exposure-response relationship."( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
0.37
"Spontaneous reports in the United States Food and Drug Administration Adverse Event Reporting System (AERS) database generated between November 1, 1997, and December 21, 2008."( Potential for linezolid-related blindness: a review of spontaneous adverse event reports.
Aitken, SL; Brown, J; van Manen, RP, 2011
)
0.37
" A limitation of AERS is the lack of a quantitative exposure estimate to put rare adverse events of the AERS, such as linezolid-related blindness, into perspective."( Potential for linezolid-related blindness: a review of spontaneous adverse event reports.
Aitken, SL; Brown, J; van Manen, RP, 2011
)
0.37
" Nausea and vomiting were the most common adverse events."( Randomized, double-blind, phase II, multicenter study evaluating the safety/tolerability and efficacy of JNJ-Q2, a novel fluoroquinolone, compared with linezolid for treatment of acute bacterial skin and skin structure infection.
Almenoff, J; Andrae, D; Covington, P; Davenport, JM; Liverman, L; McIntyre, G; O'Riordan, W, 2011
)
0.37
"3%) patients due to adverse reactions."( Linezolid: an effective, safe and cheap drug for patients failing multidrug-resistant tuberculosis treatment in India.
Bali, RK; Behera, D; Caminero, JA; Gupta, S; Jaiswal, A; Singla, N; Singla, R, 2012
)
0.38
" The exact proportions of serious and minor adverse events determined by linezolid were 21."( Efficacy and safety of linezolid in the treatment of extensively drug-resistant tuberculosis.
Gu, J; Hao, XH; Liu, YD; Sun, H; Tangg, SJ; Xiao, HP; Yao, L; Zhang, Q; Zheng, LH, 2011
)
0.37
" All reported adverse events were evaluated for serotonin toxicity using exact and surrogate terms consistent with Sternbach Criteria and Hunter Serotonin Toxicity Criteria."( Comparison of serotonin toxicity with concomitant use of either linezolid or comparators and serotonergic agents: an analysis of Phase III and IV randomized clinical trial data.
Butterfield, JM; Huang, DB; Lawrence, KR; Lodise, TP; Reisman, A; Thompson, CA, 2012
)
0.38
" No patients in either group were reported to have adverse events identified as serotonin toxicity."( Comparison of serotonin toxicity with concomitant use of either linezolid or comparators and serotonergic agents: an analysis of Phase III and IV randomized clinical trial data.
Butterfield, JM; Huang, DB; Lawrence, KR; Lodise, TP; Reisman, A; Thompson, CA, 2012
)
0.38
" However, prolonged linezolid treatment (>14 days) is considered to increase the risk of hematological adverse events."( Immediate hematological toxicity of linezolid in healthy volunteers with different body weight: a phase I clinical trial.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Guo, D; Liang, B; Liu, Y; Vouloumanou, EK; Wang, R, 2012
)
0.38
" Only two patients (both teen-aged) encountered linezolid-related adverse effects (13 %, 2/16)."( Safety and efficacy of linezolid in 16 infants and children in Japan.
Hasegawa, N; Iketani, O; Iwata, S; Kudo, M; Mori, T; Shimada, H; Shimojima, N; Shinjoh, M; Sugita, K; Takahashi, T; Watanabe, K; Yamagishi, H, 2012
)
0.38
" Adverse events were observed in 63 (58."( Efficacy, safety and tolerability of linezolid containing regimens in treating MDR-TB and XDR-TB: systematic review and meta-analysis.
Alffenaar, JW; Anger, HA; Caminero, JA; Castiglia, P; Centis, R; D'Ambrosio, L; De Lorenzo, S; Ferrara, G; Koh, WJ; Migliori, GB; Schecter, GF; Shim, TS; Singla, R; Skrahina, A; Sotgiu, G; Spanevello, A; Udwadia, ZF; Villar, M; Zampogna, E; Zellweger, JP; Zumla, A, 2012
)
0.38
" Adverse events were reported in 46 (41."( A randomized, evaluator-blind, phase 2 study comparing the safety and efficacy of omadacycline to those of linezolid for treatment of complicated skin and skin structure infections.
Arbeit, RD; Draper, MP; Hait, H; Noel, GJ; Tanaka, SK, 2012
)
0.38
"Literature was accessed via MEDLINE/PubMed and Google Scholar (both through February 2013) using the search terms linezolid, serotonin syndrome, serotonin toxicity, and adverse reaction."( Clinical relevance of linezolid-associated serotonin toxicity.
Maynor, LM; Woytowish, MR, 2013
)
0.39
" However, the safe upper threshold level for LNZ plasma trough concentrations (Cmin values) has not been defined with certainty."( Linezolid plasma concentrations and occurrence of drug-related haematological toxicity in patients with gram-positive infections.
Baldelli, S; Cattaneo, D; Clementi, E; Cordier, L; Cozzi, V; Fucile, S; Gulisano, C; Merli, S; Orlando, G; Rizzardini, G, 2013
)
0.39
" ANA was well tolerated, and dose-dependent relationships for adverse events were not observed across treatment groups."( Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib in Japanese patients with dyslipidemia.
Kikuchi, M; McCrary Sisk, C; Nakagomi, M; Numaguchi, H; Shirakawa, M; Surks, HK; Tamura, S; Teramoto, T, 2013
)
0.39
" Clinical success, microbiologic success, and adverse events (AEs) were evaluated."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
" This study of hospitalized patients revealed comparably low frequencies of adverse events potentially related to ST among patients who received linezolid or vancomycin."( Comparative evaluation of serotonin toxicity among veterans affairs patients receiving linezolid and vancomycin.
Lazariu, V; Lodise, TP; McNutt, LA; Patel, N; Rivera, A; Tristani, L; Vandewall, H, 2013
)
0.39
" The most common adverse event was headache, with no observed relationship between dose or treatment duration and adverse events."( Cadazolid, a novel antibiotic with potent activity against Clostridium difficile: safety, tolerability and pharmacokinetics in healthy subjects following single and multiple oral doses.
Baldoni, D; Dingemanse, J; Gutierrez, M; Timmer, W, 2014
)
0.4
"1%, with an acceptable side-effect profile, in patients with or at high risk for coronary heart disease in the Determining the Efficacy and Tolerability of CETP Inhibition With Anacetrapib (DEFINE) trial."( Evaluation of lipids, drug concentration, and safety parameters following cessation of treatment with the cholesteryl ester transfer protein inhibitor anacetrapib in patients with or at high risk for coronary heart disease.
Barter, P; Brinton, EA; Cannon, CP; Dansky, HM; Davidson, M; Gotto, AM; Kher, U; Li, XS; Mitchel, Y; Moon, JE; Shah, S; Vaidya, S, 2014
)
0.4
" Myelosuppression and monoamine oxidase inhibition (MAOI) are key independent causes for limiting adverse effects in therapy with the sole approved drug of this class, linezolid."( New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
Gordeev, MF; Yuan, ZY, 2014
)
0.4
" Treatment with linezolid was not associated with more adverse effects in general (OR = 0."( Efficacy and safety of linezolid for the treatment of infections in children: a meta-analysis.
Apostolidou-Kiouti, F; Haidich, AB; Ioannidou, M; Niopas, I; Roilides, E, 2014
)
0.4
" No clinically important abnormalities in liver enzymes, blood pressure, electrolytes, or adverse experiences were observed during the extension."( Lipids, safety parameters, and drug concentrations after an additional 2 years of treatment with anacetrapib in the DEFINE study.
Barter, P; Brinton, EA; Cannon, CP; Chatterjee, MS; Dansky, HM; Gotto, AM; Kher, U; Li, XS; Liu, Y; Mitchel, Y; Moon, JE; Shah, S; Vaidya, S, 2014
)
0.4
" GSK1322322 administration was associated with mild-to-moderate drug-related adverse events, most commonly, nausea, vomiting, diarrhea, and headache."( Safety, tolerability, and efficacy of GSK1322322 in the treatment of acute bacterial skin and skin structure infections.
Corey, R; Dumont, E; Jones, LS; Kurtinecz, M; Naderer, OJ; O'Riordan, WD; Zhu, JZ, 2014
)
0.4
"Linezolid induced black hairy tongue is a rare benign reversible side effect of linezolid therapy."( Linezolid induced black hairy tongue: a rare side effect.
Abdulla, FM; Aijazi, I,
)
0.13
" Azithromycin was not associated with excess serious adverse events (SAEs)."( Efficacy and safety of World Health Organization group 5 drugs for multidrug-resistant tuberculosis treatment.
Butler-Laporte, G; Menzies, D; Winters, N, 2015
)
0.42
"Oxazolidinone pharmacology including structure-activity relationships, mode of action, pharmacokinetics, drug-drug interactions, and adverse drug reactions is reviewed."( Drug-drug interactions and safety of linezolid, tedizolid, and other oxazolidinones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.42
" There were no differences between the groups in the proportion of patients who discontinued drug due to an adverse event or abnormalities in liver enzymes, creatinine kinase, blood pressure, electrolytes or adjudicated cardiovascular events."( Efficacy and safety of the cholesteryl ester transfer protein inhibitor anacetrapib in Japanese patients with heterozygous familial hypercholesterolemia.
Arai, H; Blaustein, RO; Daida, H; Ikewaki, K; Johnson-Levonas, AO; Kakikawa, T; Maeda, Y; Nakagomi, M; Numaguchi, H; Shirakawa, M; Teramoto, T; Vaidya, S, 2016
)
0.43
" Oral MRX-I was well tolerated at single doses of up to 1,200 and 800 mg q12h for up to 28 days; all adverse events were mild to moderate in severity, and there was no drug discontinuation due to adverse events."( Single- and Multiple-Dose Study To Determine the Safety, Tolerability, Pharmacokinetics, and Food Effect of Oral MRX-I versus Linezolid in Healthy Adult Subjects.
Eckburg, PB; Ge, Y; Hafkin, B, 2017
)
0.46
" Systemic adverse events were consistent with previous triptan trials, and included dizziness, paresthesia, muscle tightness, and nausea, all of which occurred in < 5% of patients in any group."( Randomized, double-blind, placebo-controlled, parallel-group, multi-center study of the safety and efficacy of ADAM zolmitriptan for the acute treatment of migraine.
Brandes, JL; Kellerman, DJ; Kudrow, DB; Schmidt, PC; Spierings, EL; Tepper, SJ; Weintraub, J, 2018
)
0.48
" High rates of adverse reactions including myelosuppression have been reported for existing oxazolidinones, limiting their long-term use."( Safety, tolerability and pharmacokinetics of 21 day multiple oral administration of a new oxazolidinone antibiotic, LCB01-0371, in healthy male subjects.
Cho, YL; Choi, Y; Chung, JY; Jang, IJ; Jang, K; Kim, A; Lee, SW; Nam, H; Yu, KS, 2018
)
0.48
"LCB01-0371 was generally safe and well tolerated up to 1200 mg BID for 7 days."( Multiple-dose Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Oral LCB01-0371 in Healthy Male Volunteers.
Bae, KS; Cho, YL; Cho, YS; Lim, HS; Nam, HS, 2018
)
0.48
" Adverse events (AEs) were identified from patients' medical records and laboratory data."( Safety and Tolerability of More than Six Days of Tedizolid Treatment.
Calabuig Muñoz, E; Castells Lao, G; Isernia, V; López Suñé, E; Mensa Pueyo, J; Mensa Vendrell, M; Morata Ruiz, L; Moreno Nuñez, L; Oltra Sempere, MR; Pasquau Liaño, J; Pedro-Botet Montoya, ML; Reynaga Sosa, EA; Salavert Lletí, M; Sequera Arquelladas, S; Soriano Viladomiu, A; Tasias Pitarch, M; Yuste Ara, JR, 2020
)
0.56
" Treatment-emergent adverse events were balanced between treatment groups (tedizolid, 14."( Safety and Efficacy of Oral and/or Intravenous Tedizolid Phosphate From a Randomized Phase 3 Trial in Adolescents With Acute Bacterial Skin and Skin Structure Infections.
Antadze, T; Bradley, JS; Broyde, N; Butterton, JR; Chou, MZ; De Anda, CS; Kim, JY; Ninov, B; Sears, PS; Tayob, MS, 2021
)
0.62
" Most participants (96%) experienced at least 1 adverse event, the vast majority of which concerned the application site, and > 95% of which were mild."( Long term safety, tolerability, and efficacy of intracutaneous zolmitriptan (M207) in the acute treatment of migraine.
Elbuluk, N; Foreman, PK; Friedman, DI; Hindiyeh, N; Kellerman, DJ; Nahas, SJ; Schmidt, P, 2021
)
0.62
"The majority of participants experienced cutaneous adverse reactions such as application site erythema, swelling, and bleeding, and most reactions were scored as mild."( Long term safety, tolerability, and efficacy of intracutaneous zolmitriptan (M207) in the acute treatment of migraine.
Elbuluk, N; Foreman, PK; Friedman, DI; Hindiyeh, N; Kellerman, DJ; Nahas, SJ; Schmidt, P, 2021
)
0.62
"BackgroundTo investigate the adverse event (AE) profile of tedizolid and linezolid in post-marketing surveillance."( Serious adverse events with tedizolid and linezolid: pharmacovigilance insights through the FDA adverse event reporting system.
De Ponti, F; Fusaroli, M; Gatti, M; Moretti, U; Poluzzi, E; Raschi, E, 2021
)
0.62
" There were no significant effects on non-vascular mortality, site-specific cancer, or other serious adverse events."( Long-term safety and efficacy of anacetrapib in patients with atherosclerotic vascular disease.
Angermann, C; Armitage, J; Baigent, C; Barter, P; Baxter, A; Blaustein, R; Bowman, L; Braunwald, E; Brenner, S; Cannon, C; Chen, F; Chen, Y; Chen, Z; Collins, R; Dayanandan, R; DeLucca, P; Ertl, G; Fabbri, G; Fajardo-Moser, M; Goodenough, R; Goto, S; Gray, A; Hao, D; Haynes, R; Herrington, W; Hill, M; Hopewell, JC; Knott, C; Landray, M; Lay, M; Liu, J; Lucci, D; Macdonnell, S; Maggioni, A; Mihaylova, B; Mitchel, Y; Mosegaard, S; Murphy, K; Sammons, E; Stevens, W; Tobert, J; Valdes-Marquez, E; Wallendszus, K; Wanner, C; Wincott, E; Wiviott, S; Wuhan, B; Zhang, H, 2022
)
0.72
"The beneficial effects of anacetrapib on major coronary events increased with longer follow-up, and no adverse effects emerged on non-vascular mortality or morbidity."( Long-term safety and efficacy of anacetrapib in patients with atherosclerotic vascular disease.
Angermann, C; Armitage, J; Baigent, C; Barter, P; Baxter, A; Blaustein, R; Bowman, L; Braunwald, E; Brenner, S; Cannon, C; Chen, F; Chen, Y; Chen, Z; Collins, R; Dayanandan, R; DeLucca, P; Ertl, G; Fabbri, G; Fajardo-Moser, M; Goodenough, R; Goto, S; Gray, A; Hao, D; Haynes, R; Herrington, W; Hill, M; Hopewell, JC; Knott, C; Landray, M; Lay, M; Liu, J; Lucci, D; Macdonnell, S; Maggioni, A; Mihaylova, B; Mitchel, Y; Mosegaard, S; Murphy, K; Sammons, E; Stevens, W; Tobert, J; Valdes-Marquez, E; Wallendszus, K; Wanner, C; Wincott, E; Wiviott, S; Wuhan, B; Zhang, H, 2022
)
0.72
" The frequency of treatment-emergent adverse events was comparable between the two groups."( A Phase III multicentre, randomized, double-blind trial to evaluate the efficacy and safety of oral contezolid versus linezolid in adults with complicated skin and soft tissue infections.
Huang, H; Yuan, H; Yuan, Z; Zhang, Y; Zhao, X, 2022
)
0.72
" Safety outcomes included assessment of treatment-emergent adverse events."( Efficacy and safety of tedizolid for the treatment of ventilated gram-positive hospital-acquired or ventilator-associated bacterial pneumonia in Japanese patients: Results from a subgroup analysis of a phase 3, randomized, double-blind study comparing ted
De Anda, C; Fujimi, S; Kusachi, S; Mikamo, H; Nagashima, M; Oshima, N; Takase, A, 2022
)
0.72
"Linezolid is an effective, but toxic anti-tuberculosis drug that is currently recommended for the treatment of drug-resistant tuberculosis."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91
"DECODE is an innovative dose-finding trial, designed to support exposure-response modelling for safe and effective dose selection."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91
" Linezolid may be a good option for treating bone and joint infections, but there is an increased risk of potential serious adverse drug events (ADEs) when used for more than 28 days."( Prolonged use of linezolid in bone and joint infections: a retrospective analysis of adverse effects.
Goosen, J; Heesterbeek, P; Jager, N; Spijkers, K; Telgt, D; Veerman, K, 2023
)
0.91
" Severe cytopenia, according to the Common Terminology Criteria for Adverse events (CTCA), was observed in four patients and was reversible after discontinuation of linezolid."( Prolonged use of linezolid in bone and joint infections: a retrospective analysis of adverse effects.
Goosen, J; Heesterbeek, P; Jager, N; Spijkers, K; Telgt, D; Veerman, K, 2023
)
0.91
" The primary efficacy endpoint was pain freedom at 2 h, and the primary safety endpoint was adverse events (AEs)."( Efficacy and safety of intranasal agents for the acute treatment of migraine: a systematic review and network meta-analysis.
Duan, S; Li, G; Liu, L; Liu, Z; Ren, Z; Wang, Z; Xia, H; Zhu, T, 2023
)
0.91
" Zavegepant nasal spray 10 mg had the fewest adverse side effects."( Efficacy and safety of intranasal agents for the acute treatment of migraine: a systematic review and network meta-analysis.
Duan, S; Li, G; Liu, L; Liu, Z; Ren, Z; Wang, Z; Xia, H; Zhu, T, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
" No differences were observed in the pharmacokinetic parameters with the increase of the dose."( Toloxatone pharmacokinetics in the plasma and cerebrospinal fluid of the rabbit.
Lamiable, D; Leon, A; Vistelle, R; Wiczewski, M; Zinsou, M, 1992
)
0.28
" This pharmacodynamic interaction could be explained by an increase in tyramine systemic bioavailability in the presence of toloxatone."( Pharmacokinetic and pharmacodynamic interaction between toloxatone, a new reversible monoamine oxidase-A inhibitor, and oral tyramine in healthy subjects.
D'Estanque, J; Ego, D; Funck-Brentano, C; Jaillon, P; Provost, JC; Rovei, V, 1992
)
0.28
" MD 770222, which is also a selective and reversible inhibitor of MAO A although less potent than cimoxatone, is the major plasma metabolite and its plasma elimination half-life is about three times longer than cimoxatone."( Pharmacokinetic and relative bioavailability studies of cimoxatone in humans.
Kendall, MJ; Mitchard, M; Rovei, V; Strolin Benedetti, M, 1984
)
0.27
" The pharmacokinetic and tolerability profiles of single oral doses from 1-50 mg 311C90 were investigated in 12 healthy male volunteers in a double-blind, placebo-controlled, dose-escalating study."( The tolerability and pharmacokinetics of the novel antimigraine compound 311C90 in healthy male volunteers.
Churchus, R; On, N; Phillips, S; Posner, J; Rolan, P; Seaber, E, 1996
)
0.29
" There was no evidence of significant changes in the pharmacokinetic parameters of zomitriptan or its metabolites after the last dose compared to the first, except for an expected rise in peak concentrations and a small, apparent increase in the amount of drug excreted in urine and hence in CLR."( The pharmacokinetics and effects on blood pressure of multiple doses of the novel anti-migraine drug zolmitriptan (311C90) in healthy volunteers.
Dixon, R; Gibbens, M; Gillotin, C; Peck, RW; Posner, J, 1997
)
0.3
" Pharmacodynamic measures included oscillometric blood pressure, systolic blood pressure at the toe and arm using a strain gauge technique, stroke volume and cardiac output using bioimpedance cardiography, high-resolution ultrasound to measure brachial arterial diameter and a novel Doppler method to measure blood flow velocity."( Peripheral vascular effects and pharmacokinetics of the antimigraine compound, zolmitriptan, in combination with oral ergotamine in healthy volunteers.
Dixon, RM; Evans, DH; Meire, HB; On, N; Posner, J; Rolan, PE; Watt, H, 1997
)
0.3
" On average, 75% of its eventual Cmax is achieved within 1 h of dosing."( The clinical pharmacokinetics of zolmitriptan.
Dixon, R; Warrander, A, 1997
)
0.3
" Blood pressure, heart rate, ECG, and central nervous system effects were monitored, and pharmacokinetic parameters of zolmitriptan and its metabolites calculated."( The pharmacodynamics and pharmacokinetics of the 5HT1B/1D-agonist zolmitriptan in healthy young and elderly men and women.
Dixon, RM; Jackson, SH; Layton, GR; Peck, RW; Posner, J; Rolan, PE; Seaber, EJ; Weatherley, BC, 1998
)
0.3
" Zolmitriptan plasma concentrations were higher in women than in men, with higher values of AUC and Cmax and lower total clearance in women."( Pharmacokinetics and pharmacodynamics of zolmitriptan in patients with mild to moderate hypertension: a double-blind, placebo-controlled study.
Cleary, EW; Dilzer, SC; Huffman, CS; Lasseter, KC; Smith, DA; Watkins, S, 1998
)
0.3
" The metabolism of zolmitriptan was reduced in patients with severe hepatic impairment compared with healthy subjects, resulting in higher peak plasma concentrations (47%), increased exposure (226%), and prolonged half-life (157%)."( Effect of hepatic impairment on the pharmacokinetics of zolmitriptan.
Delvaux, M; Dixon, R; French, S; Kemp, J; Leclerc, V; Rautureau, J; Sellers, M, 1998
)
0.3
" Cmax and AUC of oral zolmitriptan were dose-proportional and there was a 13 and 16% fall in mean zolmitriptan Cmax and AUC, respectively, when administered after food."( The absolute bioavailability and effect of food on the pharmacokinetics of zolmitriptan in healthy volunteers.
Allanson, J; Hefting, NR; Jonkman, JH; Peck, RW; Seaber, EJ; Smith, DA; Sollie, FA; van Lier, JJ; Wemer, J, 1998
)
0.3
" Pharmacokinetic data demonstrate that coadministration of linezolid and aztreonam does not alter the disposition of either agent under single-dose conditions."( A pharmacokinetic evaluation of concomitant administration of linezolid and aztreonam.
Hopkins, NK; Jungbluth, GL; Sisson, TL, 1999
)
0.3
" A mean peak concentration in plasma of 18."( Pharmacokinetics and tissue penetration of linezolid following multiple oral doses.
Andrews, J; Ashby, J; Ellis, R; Gee, T; Marshall, G; Wise, R, 2001
)
0.31
" The authors present data evaluating the pharmacokinetic and pharmacodynamic responses to coadministration of oral linezolid with sympathomimetics (pseudoephedrine and phenylpropanolamine) and a serotonin reuptake inhibitor (dextromethorphan)."( Linezolid: pharmacokinetic and pharmacodynamic evaluation of coadministration with pseudoephedrine HCl, phenylpropanolamine HCl, and dextromethorpan HBr.
Antal, EJ; Batts, DH; Hendershot, PE; Hopkins, NK; Welshman, IR, 2001
)
0.31
" Pharmacokinetic parameters were assessed using noncompartmental methods."( Age and sex effects on the pharmacokinetics of linezolid.
Hopkins, NK; Jungbluth, GL; Sisson, TL, 2002
)
0.31
" The pharmacodynamic activity and in vivo efficacy of linezolid were compared to those of ceftriaxone in an immunocompetent rat model of pneumococcal pneumonia."( Pharmacodynamic activity and efficacy of linezolid in a rat model of pneumococcal pneumonia.
Gentry-Nielsen, MJ; Olsen, KM; Preheim, LC, 2002
)
0.31
"In this study, our objective was to determine the steady-state intrapulmonary concentrations and pharmacokinetic parameters of orally administered linezolid in healthy volunteers."( Intrapulmonary pharmacokinetics of linezolid.
Conte, JE; Golden, JA; Kipps, J; Zurlinden, E, 2002
)
0.31
" There were no significant differences in terminal elimination half-life between days 1 and 7 (9."( Single- and multiple-dose pharmacokinetics of linezolid and co-amoxiclav in healthy human volunteers.
Borner, K; Burkhardt, O; Köppe, P; Lode, H; Nord, CE; Pletz, MW; von der Höh, N, 2002
)
0.31
" Plasma levels were maintained at a plateau between 1 and 6 hours postdose, then decreased with a half-life of approximately 3 hours."( Preliminary studies of the pharmacokinetics and tolerability of zolmitriptan nasal spray in healthy volunteers.
Dixon, R; Nairn, K; Seaber, E; Yates, R, 2002
)
0.31
" Of the patient covariates considered (age, sex, ideal body weight, baseline serum albumin, hepatic or renal dysfunction, underlying malignancy, organ transplantation, surgical status, global severity of illness, site of infection, route of administration, and location of care [intensive-care unit, general floor, or outpatient]), only normalized creatinine clearance (CL(CR)) and body weight explained significant portions of the variance and were incorporated into the pharmacokinetic model."( Population pharmacokinetics of linezolid in patients treated in a compassionate-use program.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.32
" The plasma-ear fluid pharmacodynamic profile associated with linezolid efficacy was a T>MIC of >/=42%, a C(max)/MIC ratio of >/=3."( Pharmacokinetics and efficacy of linezolid in a gerbil model of Streptococcus pneumoniae-induced acute otitis media.
Biermacher, JJ; Humphrey, WR; Jensen, JL; Kuo, MS; Richards, IM; Schaadt, RD; Shattuck, MH; Smith, DP; Zielinski, RJ; Zurenko, GE, 2003
)
0.32
" Non-compartmental pharmacokinetic analyses were used to describe the disposition of linezolid."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.32
" Mean clearance, half-life and volume of distribution were similar irrespective of dose for both the oral and intravenous routes."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.32
" Plasma samples for population pharmacokinetic analysis were collected."( Safety, efficacy and pharmacokinetics of linezolid for treatment of resistant Gram-positive infections in cancer patients with neutropenia.
Birmingham, MC; Forrest, A; Meagher, AK; Noskin, GA; Rayner, CR; Schentag, JJ; Smith, PF, 2003
)
0.32
"Potential alternatives, including linezolid, adjunctive rifampin, and moxifloxacin, were evaluated against vancomycin-tolerant (P9802-020) and vancomycin-susceptible clinical isolates of Streptococcus pneumoniae in an in vitro pharmacodynamic model."( Linezolid and vancomycin, alone and in combination with rifampin, compared with moxifloxacin against a multidrug-resistant and a vancomycin-tolerant Streptococcus pneumoniae strain in an in vitro pharmacodynamic model.
Cha, R; Rybak, MJ, 2003
)
0.32
" Serial blood samples for assessment of the pharmacokinetic parameters of linezolid and its two inactive metabolites were collected on days 1 and 8, whereas vitamin concentrations were measured prior to and after the vitamin intake on these days."( The pharmacokinetics of linezolid are not affected by concomitant intake of the antioxidant vitamins C and E.
Antal, EJ; Francom, SF; Gordi, T; Hong, C; Hopkins, NJ; Slatter, JG; Tan, LH, 2003
)
0.32
" Therefore it is important to determine the specific pharmacokinetic characteristics for individual drugs in pediatric patients so that appropriate age-specific dosage regimens can be developed and evaluated in clinical trials."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
0.32
" Children younger than 12 years of age have a smaller area under the drug concentration-time curve, a faster clearance and a shorter elimination half-life than adults."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
0.32
" The elimination half-life of linezolid is 5-7 hours, and twice-daily administration of 400-600 mg provides steady-state concentrations in the therapeutic range."( Clinical pharmacokinetics of linezolid, a novel oxazolidinone antibacterial.
Jungbluth, GL; Stalker, DJ, 2003
)
0.32
" aureus (VRSA), an in vitro pharmacodynamic model with simulated endocardial vegetations incorporating protein and a high inoculum was used to simulate daptomycin, linezolid, quinupristin-dalfopristin, and vancomycin against the Michigan VRSA strain."( Bactericidal activities of daptomycin, quinupristin-dalfopristin, and linezolid against vancomycin-resistant Staphylococcus aureus in an in vitro pharmacodynamic model with simulated endocardial vegetations.
Brown, WJ; Cha, R; Rybak, MJ, 2003
)
0.32
" Plasma concentrations were obtained and a multicompartmental pharmacokinetic model was fitted."( Clinical pharmacodynamics of linezolid in seriously ill patients treated in a compassionate use programme.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.32
"Modelled pharmacodynamic outcomes of efficacy included probabilities of eradication and clinical cure (multifactorial logistic regression, nonparametric tree-based modelling, nonlinear regression) and time to bacterial eradication (Kaplan-Meier and Cox proportional hazards regression)."( Clinical pharmacodynamics of linezolid in seriously ill patients treated in a compassionate use programme.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.32
" Pharmacokinetic parameters were estimated using standard noncompartmental methods."( Linezolid pharmacokinetics in adult patients with cystic fibrosis.
Bosso, JA; Flume, PA; Gray, SL, 2004
)
0.32
"To compare the pharmacodynamic profiles of linezolid, levofloxacin, and vancomycin against clinical strains of Streptococcus pneumoniae, including vancomycin-tolerant and fluoroquinolone-resistant isolates."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.32
"In vitro pharmacodynamic model."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.32
"An in vitro pharmacodynamic model was used to simulate standard dosing regimens of linezolid, levofloxacin, and vancomycin against the isolates 79, R921, and P9802-020."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.32
"The pharmacokinetic parameters of DA-7867, a new oxazolidinone, were compared after intravenous and oral administration at a dose of 10 mg x kg(-1) to control rats and rats with protein-calorie malnutrition (rats with PCM)."( Effects of protein-calorie malnutrition on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats.
Bae, SK; Kim, WB; Kwon, JW; Lee, MG; Lee, SJ, 2004
)
0.32
" Allometric scaling has previously been used as an effective tool for the prediction of human pharmacokinetic data."( Prediction of clinical pharmacokinetic parameters of linezolid using animal data by allometric scaling: applicability for the development of novel oxazolidinones.
Bhamidipati, RK; Dravid, PV; Mullangi, R; Srinivas, NR, 2004
)
0.32
"To determine the pharmacokinetic characteristics of linezolid and teicoplanin in critically ill patients."( Pharmacokinetic studies of linezolid and teicoplanin in the critically ill.
Aarons, L; Cepeda, JA; Kibbler, C; MacGowan, A; Nalda-Molina, R; Shaw, S; Shulman, R; Singer, M; Tobin, C; Whitehouse, T; Wilson, AP, 2005
)
0.33
"The aim of this study was to compare the activity of linezolid and vancomycin in an in vitro pharmacodynamic model to assess potential differences in activity against biofilm-embedded organisms."( Antibacterial activity of linezolid and vancomycin in an in vitro pharmacodynamic model of gram-positive catheter-related bacteraemia.
Coyle, EA; Lewis, RE; Prince, RA; Raad, II; Wiederhold, NP, 2005
)
0.33
"Single-lumen central venous catheters colonized with biofilm-embedded Staphylococcus aureus, Staphylococcus epidermidis or vancomycin-resistant Enterococcus faecium (VRE) were treated with simulated clinical dosing regimens of linezolid 600 mg every 12 h or vancomycin 1 g every 12 h in a one-compartment in vitro pharmacodynamic model."( Antibacterial activity of linezolid and vancomycin in an in vitro pharmacodynamic model of gram-positive catheter-related bacteraemia.
Coyle, EA; Lewis, RE; Prince, RA; Raad, II; Wiederhold, NP, 2005
)
0.33
" The assay method was successfully applied to a pharmacokinetic study of DRF-6196 in mice."( Validation of a simple bioanalytical method for the determination of DRF-6196, a novel oxazolidinone, in mouse plasma: application to a single-dose pharmacokinetic study.
Bhamidipati, RK; Dravid, PV; Mullangi, R; Srinivas, NR, 2005
)
0.33
"To determine the steady-state plasma pharmacokinetic variables and epithelial lining fluid concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia."( Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC; Toutain, J, 2005
)
0.33
" After 2 days of therapy, the steady-state plasma pharmacokinetic variables and epithelial lining fluid concentrations of linezolid were determined by high-performance liquid chromatography."( Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC; Toutain, J, 2005
)
0.33
" Pharmacokinetic parameters derived from noncompartmental and compartmental analysis incorporating linear and nonlinear elimination pathways were compared between groups: F, Ka, Vs, K23, K32, Vmax, Km, and K20 (bioavailability, absorption rate constant, volume of central compartment normalized to body weight, intercompartmental rate constants, maximum velocity, Michaelis-Menten constant, and elimination rate constant, respectively)."( Absolute bioavailability and pharmacokinetics of linezolid in hospitalized patients given enteral feedings.
Beringer, P; Gill, M; Gurevitch, M; Hoem, N; Louie, S; Nguyen, M; Wong-Beringer, A, 2005
)
0.33
" Aqueous and serum levels of linezolid were assayed by high performance liquid chromatography, and a pharmacokinetic curve constructed from the pooled results."( The pharmacokinetics of linezolid in the non-inflamed human eye.
Jenkins, DR; Lovering, A; Prydal, JI; Watts, A, 2005
)
0.33
"The pharmacokinetic parameters of DA-7867 were compared after intravenous and oral administration at a dose of 10 mg/kg to control rats and rats with acute renal failure induced by uranyl nitrate (rats with U-ARF)."( Effects of acute renal failure on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats.
Bae, SK; Kim, WB; Kwon, JW; Lee, I; Lee, MG, 2006
)
0.33
"Several antibiotics show significant pharmacokinetic interactions when they are given orally concomitantly with antacids."( Lack of pharmacokinetic interaction between linezolid and antacid in healthy volunteers.
Drewe, J; Grunder, G; Krähenbühl, S; Maier, T; Vollenweider, F; Zysset-Aschmann, Y, 2006
)
0.33
"The pharmacokinetic parameters of DA-7867 were compared after intravenous and oral administration at a dose of 10 mg/kg in control rats and in rats with water deprivation for 72 h (rat model of dehydration)."( Effects of water deprivation for 72 hours on the pharmacokinetics of DA-7867, a new oxazolidinone, in rats.
Bae, SK; Kim, YC; Kwon, JW; Lee, I; Lee, JK; Lee, MG; Yoo, M, 2006
)
0.33
" The comparison of pharmacokinetic and clinical data available from different formulations of zolmitriptan contributes both to the understanding of its mode of action and the characteristics required of an acute migraine treatment if it is to meet patient needs."( Zolmitriptan intranasal: a review of the pharmacokinetics and clinical efficacy.
Goadsby, PJ; Yates, R, 2006
)
0.33
" The method was successfully applied to a pharmacokinetic study of zolmitriptan after an oral administration of 5 mg zolmitriptan to 20 healthy volunteers."( Determination of zolmitriptan in human plasma by liquid chromatography-tandem mass spectrometry method: application to a pharmacokinetic study.
Chen, X; Jin, F; Liu, D; Luan, Y; Zhong, D, 2006
)
0.33
"We inoculated an in vitro pharmacodynamic model simultaneously with clinical isolates of methicillin-resistant Staphylococcus aureus and an enterocin-producing enterococcus (vancomycin-resistant Enterococcus faecalis, ampicillin susceptible) at 7 log10 CFU/ml to examine enterocin effects and antimicrobial activity on staphylococci."( Impact of Enterococcus faecalis on the bactericidal activities of arbekacin, daptomycin, linezolid, and tigecycline against methicillin-resistant Staphylococcus aureus in a mixed-pathogen pharmacodynamic model.
Chin, JN; LaPlante, KL; Leuthner, KD; Rybak, MJ, 2006
)
0.33
" Individual compartmental pharmacokinetic (PK) analysis was performed using WinNonlin."( Pharmacokinetics of unbound linezolid in plasma and tissue interstitium of critically ill patients after multiple dosing using microdialysis.
Buerger, C; Dehghanyar, P; Joukhadar, C; Kloft, C; Plock, N, 2006
)
0.33
"The pharmacokinetic profile of linezolid in cerebrospinal fluid (CSF) in five neurointensive care patients with staphylococcal ventriculitis was studied."( Pharmacokinetics of intravenous linezolid in cerebrospinal fluid and plasma in neurointensive care patients with staphylococcal ventriculitis associated with external ventricular drains.
Beer, R; Brenneis, C; Broessner, G; Engelhardt, KW; Georgopoulos, A; Helbok, R; Kaehler, ST; Lackner, P; Pfausler, B; Schmutzhard, E, 2007
)
0.34
" Optimal pharmacokinetic (PK)/pharmacodynamic (PD) indices have been described for the antimicrobial efficacy of linezolid (area under the concentration-time curve over 24 h at steady state divided by the MIC, >100; the cumulative percentage of a 24-h period that the drug concentration exceeds the MIC under steady-state PK conditions, >85)."( Pharmacokinetic/pharmacodynamic factors influencing emergence of resistance to linezolid in an in vitro model.
Boak, LM; Li, J; Nation, RL; Rayner, CR, 2007
)
0.34
"To compare pharmacodynamic indices and minimal inhibitory concentrations for vancomycin, gatifloxacin, moxifloxacin, linezolid, and combined quinupristin and dalfopristin for historic and current human coagulase-negative staphylococcus (CoNS) endophthalmitis isolates."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Peak concentration (C(max)) was defined as the maximum attainable aqueous concentration using topical or oral therapy, or both."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
"The objective of this study was to evaluate a physiologically based pharmacokinetic (PBPK) approach for predicting the plasma concentration-time curves expected after intravenous administration of candidate drugs to rodents."( Evaluation of a basic physiologically based pharmacokinetic model for simulating the first-time-in-animal study.
Burton, PS; Crivori, P; Germani, M; Poggesi, I; Rocchetti, M; Smith, ME; Wilson, AG, 2007
)
0.34
" The pharmacokinetic parameters of DA-7218 and DA-7157 were evaluated after intravenous (5, 10 and 20 mg kg(-1)) and oral (20, 50 and 100 mg kg(-1)) administration of DA-7218 to rats."( Pharmacokinetics of DA-7218, a new oxazolidinone, and its active metabolite, DA-7157, after intravenous and oral administration of DA-7218 and DA-7157 to rats.
Bae, SK; Lee, MG; Rhee, JK; Shin, KN; Yang, SH; Yoo, M, 2007
)
0.34
" Therefore, a population pharmacokinetic analysis using NONMEM was performed to thoroughly understand the pharmacokinetics of unbound linezolid in plasma."( Does linezolid inhibit its own metabolism? Population pharmacokinetics as a tool to explain the observed nonlinearity in both healthy volunteers and septic patients.
Buerger, C; Joukhadar, C; Kljucar, S; Kloft, C; Plock, N, 2007
)
0.34
" Pharmacodynamic targets included an AUC/MIC >82."( Pharmacodynamic comparison of linezolid, teicoplanin and vancomycin against clinical isolates of Staphylococcus aureus and coagulase-negative staphylococci collected from hospitals in Brazil.
Kiffer, CR; Kuti, JL; Mendes, CM; Nicolau, DP, 2008
)
0.35
" The aim of this study was to assess the feasibility of the microdialysis technique to cancellous bone for single dose pharmacokinetic investigations of the anti-infective linezolid."( Pharmacokinetics of linezolid in bone tissue investigated by in vivo microdialysis.
Arpi, M; Buerger, C; Emmertsen, KJ; Joukhadar, C; Kloft, C; Plock, N; Riegels-Nielsen, P; Stolle, LB, 2008
)
0.35
"Simulating the average non-protein-bound (free) human serum drug concentration-time profiles for linezolid in an in vitro pharmacodynamic model, we characterized the pharmacodynamic parameter(s) of linezolid predictive of kill and for prevention of resistance in Bacillus anthracis."( Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
Brown, DL; Drusano, GL; Heine, HS; Kim, K; Kinzig-Schippers, M; Liu, W; Louie, A; Sörgel, F; VanScoy, B, 2008
)
0.35
"The aim of this study was to develop an integrated system for in vitro pharmacodynamic modelling of antimicrobials with greater flexibility, easier control and better accuracy than existing in vitro models."( Development of an integrated semi-automated system for in vitro pharmacodynamic modelling.
Berejnaia, O; Conway, D; Giacobbe, RA; Kath, GS; Racine, F; Wang, L; Wismer, MK, 2008
)
0.35
" The system was validated by pharmacokinetic simulations of linezolid 600 mg infusion."( Development of an integrated semi-automated system for in vitro pharmacodynamic modelling.
Berejnaia, O; Conway, D; Giacobbe, RA; Kath, GS; Racine, F; Wang, L; Wismer, MK, 2008
)
0.35
"The aim of the study was to assess the biliary penetration of linezolid and the probabilities of attaining optimal pharmacodynamic exposure against vancomycin-resistant enterococci (VRE) in the bile of liver transplant (LTx) patients who received linezolid for the treatment of multidrug-resistant Gram-positive hospital infections."( Biliary penetration and pharmacodynamic exposure of linezolid in liver transplant patients.
Adani, GL; Baccarani, U; Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Tavio, M; Viale, P, 2009
)
0.35
" Biliary penetration of linezolid was calculated as the ratio between Cmin in bile and in plasma."( Biliary penetration and pharmacodynamic exposure of linezolid in liver transplant patients.
Adani, GL; Baccarani, U; Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Tavio, M; Viale, P, 2009
)
0.35
"83) enabled achievement of optimal theoretical pharmacodynamic exposure against VRE in bile (Cmin>2 mg/L) on all of the occasions."( Biliary penetration and pharmacodynamic exposure of linezolid in liver transplant patients.
Adani, GL; Baccarani, U; Della Rocca, G; Furlanut, M; Lugano, M; Pavan, F; Pea, F; Tavio, M; Viale, P, 2009
)
0.35
" There are no published pharmacokinetic (PK) and pharmacodynamic (PD) data for linezolid in children with CF."( Pharmacokinetics and pharmacodynamics of linezolid in children with cystic fibrosis.
Ahmad, N; Brown, ME; Jafri, HS; McCracken, GH; Murphey, DK; Prestidge, CB; Salvatore, CM; Sanchez, PJ; Santos, RP; Siegel, JD; Urbancyzk, B, 2009
)
0.35
" Linezolid has a favorable pharmacokinetic profile."( Association of pharmacokinetic and pharmacodynamic aspects of linezolid with infection outcome.
Falagas, ME; Kioumis, I; Vardakas, KZ, 2009
)
0.35
" Non-compartmental analyses were used to describe the pharmacokinetic disposition of linezolid."( Pharmacokinetic evaluation of linezolid in patients with major thermal injuries.
Birraux, G; Bret, P; Hovsepian, L; Le Floch, R; Lovering, AM; Stephanazzi, J; Vinsonneau, C, 2009
)
0.35
"The rational selection of antibiotics for the treatment of meningitis must take into account several criteria, among which their intrinsic activity against the causative bacteria, and their pharmacokinetic and pharmacodynamic properties."( [Pharmacodynamics of antibiotics in CSF: principles and consequences (predictive factors of efficacy)].
Tulkens, PM; Van Bambeke, F,
)
0.13
" Although linezolid has been approved worldwide, the Japanese pharmacokinetic (PK) profile has not been characterized in detail."( Population pharmacokinetic analysis of linezolid in patients with infectious disease: application to lower body weight and elderly patients.
Abe, S; Chiba, K; Cirincione, B; Grasela, TH; Ito, K; Suwa, T, 2009
)
0.35
" Because of the likely use of anacetrapib with hydroxy-3-methylglutaryl coenzyme A reductase inhibitors, we aimed to evaluate the potential for a pharmacokinetic interaction with simvastatin."( Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.
Bieberdorf, FA; Chodakewitz, J; Garg, A; Jin, B; Keshavarz, SS; Krishna, R; Wagner, JA, 2009
)
0.35
"There appears to be no clinically meaningful effect of anacetrapib on the pharmacokinetic parameters of simvastatin."( Assessment of a pharmacokinetic and pharmacodynamic interaction between simvastatin and anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.
Bieberdorf, FA; Chodakewitz, J; Garg, A; Jin, B; Keshavarz, SS; Krishna, R; Wagner, JA, 2009
)
0.35
"In an in vitro pharmacodynamic model, linezolid attenuated the activity of aztreonam and ceftazidime against Escherichia coli."( Evaluating aztreonam and ceftazidime pharmacodynamics with Escherichia coli in combination with daptomycin, linezolid, or vancomycin in an in vitro pharmacodynamic model.
LaPlante, KL; Sakoulas, G, 2009
)
0.35
" Torezolid (TR-700) is a novel methyltetrazolyl oxazolidinone with potentially different cellular pharmacokinetic properties."( Cellular pharmacokinetics and intracellular activity of torezolid (TR-700): studies with human macrophage (THP-1) and endothelial (HUVEC) cell lines.
Appelbaum, PC; Lemaire, S; Tulkens, PM; Van Bambeke, F, 2009
)
0.35
" The goal of the present study was to develop a general pharmacokinetic (PK)-pharmacodynamic (PD) model that allows the characterization and comparison of the in vitro activities of oxazolidinones, determined in time-kill curve experiments, against MRSA."( Pharmacokinetic-pharmacodynamic modeling of the in vitro activities of oxazolidinone antimicrobial agents against methicillin-resistant Staphylococcus aureus.
Abbanat, D; Barbour, A; Derendorf, H; Manitpisitkul, P; Sabarinath, SN; Schmidt, S; Sha, S, 2009
)
0.35
"Anacetrapib was rapidly absorbed, with peak concentrations occurring at approximately 4 h post-dose and an apparent terminal half-life ranging from approximately 9 to 62 h in the fasted state and from approximately 42 to approximately 83 h in the fed state."( Single-dose pharmacokinetics and pharmacodynamics of anacetrapib, a potent cholesteryl ester transfer protein (CETP) inhibitor, in healthy subjects.
Al-Huniti, N; Archer, L; Bergman, AJ; Chavez-Eng, C; Chen, J; Cote, J; Dykstra, K; Garg, A; Gottesdiener, K; Hilliard, D; Jin, B; Krishna, R; Laethem, T; Lasseter, KC; Lutz, R; Panebianco, D; Snyder, K; Van Bortel, L; Van Dyck, K; Van Hoydonck, P; Wagner, JA, 2009
)
0.35
" The pharmacokinetic parameters, their variability, and possible covariates were analyzed using NONMEM."( Pharmacokinetics of linezolid in septic patients with and without extended dialysis.
Haefeli, WE; Hempel, G; Hoppe-Tichy, T; Lichtenstern, C; Ober, MC; Saleh, S; Schwenger, V; Sonntag, HG; Swoboda, S; Weigand, MA, 2010
)
0.36
" The mean half-life and apparent oral clearance were decreased for the combination treatment compared with linezolid alone."( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism.
Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011
)
0.37
" Pharmacokinetic indices (Cmax, Cmin, Tmax, AUC) were determined for plasma and ventricular fluid (VF) after the first and last doses."( Pharmacokinetics and distribution of linezolid in cerebrospinal fluid in children and adolescents.
Damle, B; Levy, G; Nachman, S; Yogev, R, 2010
)
0.36
"In study 1, after the last dose, the mean Cmax values for plasma and VF were 10."( Pharmacokinetics and distribution of linezolid in cerebrospinal fluid in children and adolescents.
Damle, B; Levy, G; Nachman, S; Yogev, R, 2010
)
0.36
"This open-label, prospective pharmacokinetic study evaluated two doses (300 and 600 mg) of linezolid in MDR-TB patients, who received linezolid as part of their treatment."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
0.36
" The present article reviews the pharmacokinetic properties of vancomycin, linezolid, tigecycline and daptomycin."( Comparison of the pharmacokinetic properties of vancomycin, linezolid, tigecyclin, and daptomycin.
Derendorf, H; Estes, KS, 2010
)
0.36
" Using 603 platelet counts from 45 patients, a PPK/PD analysis with a semimechanistic pharmacodynamic model described the relationship between linezolid exposure and platelet counts quantitatively, and the newly constructed model was validated using external data (776 platelet counts from 60 patients)."( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
0.37
" Single-dose pharmacokinetic studies were conducted in mice for TR-701/700."( In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model.
Drusano, GL; Kulawy, R; Liu, W; Louie, A, 2011
)
0.37
" Population pharmacokinetic analyses were performed by nonlinear mixed-effects modeling using a previously described 2-compartment model with time-dependent clearance inhibition."( Pharmacokinetics of intravenous and oral linezolid in adults with cystic fibrosis.
Keel, RA; Kloft, C; Knauft, RF; Kuti, JL; Muhlebach, M; Nicolau, DP; Pope, JS; Schaeftlein, A, 2011
)
0.37
" This review examines pharmacokinetic data relating to linezolid use in different patient groups (obesity, enteral feeding, renal failure, neonates, and paediatrics) and in different clinical conditions (sepsis syndrome, skin and soft tissue infection, diabetic foot infection, pneumonia, bone and joint infection, infection of the central nervous system, eye infection, and neutropenic sepsis)."( Linezolid pharmacokinetics and pharmacodynamics in clinical treatment.
Dryden, MS, 2011
)
0.37
" The purpose of the current study was to describe the pharmacokinetic profile and determine the level of penetration of linezolid into healthy thigh tissue and infected wound tissue of the same extremity in 9 diabetic patients with chronic lower limb infections by use of in vivo microdialysis."( Determination of tissue penetration and pharmacokinetics of linezolid in patients with diabetic foot infections using in vivo microdialysis.
Kuti, JL; Nicolau, DP; Shepard, A; Wiskirchen, DE, 2011
)
0.37
" WHAT THIS STUDY: ADDS • This is the first study to show that there is no clinically meaningful pharmacokinetic interaction between anacetrapib and warfarin."( Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects.
Ali, M; Connolly, SM; Cote, J; Degroot, B; Garg, A; Krishna, R; Li, S; Liu, Y; Maes, A; Stoch, SA; Stypinski, D; Wagner, JA, 2012
)
0.38
" After warfarin concentrations and prothrombin time were measured, standard pharmacokinetic, pharmacodynamic and statistical (linear mixed effects model) analyses were applied."( Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects.
Ali, M; Connolly, SM; Cote, J; Degroot, B; Garg, A; Krishna, R; Li, S; Liu, Y; Maes, A; Stoch, SA; Stypinski, D; Wagner, JA, 2012
)
0.38
" The results showed increased clearance of linezolid and a reduced serum concentration compared to population pharmacokinetic parameters, with trough levels below the 90% minimum inhibitory concentration."( Evaluation of the pharmacokinetics of linezolid in an obese Japanese patient.
Hiraki, Y; Kamimura, H; Karube, Y; Kobayashi, T; Matsumoto, K; Mizoguchi, A; Morita, K; Sadoh, S; Sakamoto, S; Tsuji, Y; Yukawa, E, 2012
)
0.38
"Our study shows that the continuous infusion of 1200 mg of linezolid daily in critically ill patients with VAP provides satisfactory pharmacokinetic results, with a linezolid alveolar diffusion of 100% and concentrations exceeding almost twice the susceptibility breakpoint for Staphylococcus aureus (4 mg/L) in both serum and ELF for 100% of the time."( Alveolar diffusion and pharmacokinetics of linezolid administered in continuous infusion to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Bouvet, L; Breilh, D; Caillault-Sergent, A; Djabarouti, S; Guillaume, C; Rimmelé, T; Saux, MC; Xuereb, F, 2012
)
0.38
"The methodology included the following steps: acquisition of microbiological and pharmacokinetic data, Monte Carlo simulation, estimation of the probability of target attainment (PTA), and calculation of the cumulative fraction of response (CFR)."( Pharmacokinetic-pharmacodynamic evaluation of daptomycin, tigecycline, and linezolid versus vancomycin for the treatment of MRSA infections in four western European countries.
Betriu, C; Canut, A; Gascón, AR; Isla, A, 2012
)
0.38
" These data highlight the importance of pharmacokinetic confirmation in each model."( Pharmacokinetics and pulmonary disposition of tedizolid and linezolid in a murine pneumonia model under variable conditions.
Crandon, JL; Keel, RA; Nicolau, DP, 2012
)
0.38
" Pharmacokinetic parameters may vary as a consequence of gender differences, inter- and intra-subjects variability and delivery system."( Pharmacokinetic evaluation of zolmitriptan for the treatment of migraines.
Casolla, B; D'Alonzo, L; Lionetto, L; Martelletti, P; Mastropietri, F; Negro, A; Simmaco, M, 2012
)
0.38
" Pharmacokinetic analyses were conducted using compartmental and noncompartmental methods."( Pharmacokinetics of intravenous linezolid in moderately to morbidly obese adults.
Bhalodi, AA; Kuti, JL; Nicolau, DP; Papasavas, PK; Tishler, DS, 2013
)
0.39
"The objective was to evaluate the pharmacokinetic and pharmacodynamic properties of a single intravenous fixed dose compared with a weight-adjusted dose of linezolid."( Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Karageorgopoulos, DE; Liang, B; Wang, R, 2013
)
0.39
" A Monte Carlo simulation was used to evaluate the probability of pharmacodynamic target attainment (PTA)."( Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Karageorgopoulos, DE; Liang, B; Wang, R, 2013
)
0.39
" Log-transformed anacetrapib AUC0-∞ and Cmax were analyzed by a linear mixed effects model."( Effects of Rifampin, a potent inducer of drug-metabolizing enzymes and an inhibitor of OATP1B1/3 transport, on the single dose pharmacokinetics of anacetrapib.
Anderson, MS; Auger, P; Cote, J; Gutstein, DE; Hohnstein, A; Johnson-Levonas, AO; Liu, Y; Rasmussen, S; Stypinski, D, 2013
)
0.39
"From the pharmacodynamic perspective (serum concentrations), vancomycin tolerance should include MBC/MIC ≥8 since strains exhibiting this ratio showed bacteriostatic profiles similar to those obtained with isolates with MBC/MIC ratios of 16 or 32."( Influence of the MBC/MIC ratio on the antibacterial activity of vancomycin versus linezolid against methicillin-resistant Staphylococcus aureus isolates in a pharmacodynamic model simulating serum and soft tissue interstitial fluid concentrations reported
Aguilar, L; Alou, L; Cafini, F; Gimenez, MJ; Gomez-Lus, ML; Gonzalez, N; Prieto, J; Sevillano, D, 2013
)
0.39
" The population pharmacokinetic (PPK) of linezolid was investigated in MRSA infected patients with renal dysfunction."( Population pharmacokinetic analysis of linezolid in low body weight patients with renal dysfunction.
Hiraki, Y; Kamimura, H; Karube, Y; Matsumoto, K; Mizoguchi, A; Morita, K; To, H; Tsuji, Y; Yukawa, E, 2013
)
0.39
" The validated method was applied to assay real plasma samples used for pharmacokinetic studies and therapeutic drug monitoring of the selected drugs."( Simultaneous quantification of linezolid, tinidazole, norfloxacin, moxifloxacin, levofloxacin, and gatifloxacin in human plasma for therapeutic drug monitoring and pharmacokinetic studies in human volunteers.
Helmy, SA, 2013
)
0.39
"This assay method was valid within a wide range of plasma concentrations and may be proposed as a suitable method for pharmacokinetic studies, therapeutic drug monitoring implementation, and routine clinical applications, especially for some populations of patients who receive a combination of these drugs."( Simultaneous quantification of linezolid, tinidazole, norfloxacin, moxifloxacin, levofloxacin, and gatifloxacin in human plasma for therapeutic drug monitoring and pharmacokinetic studies in human volunteers.
Helmy, SA, 2013
)
0.39
"A Monte Carlo simulation involving 10000 subjects was used to analyze the pharmacokinetic parameters and microbiological data of linezolid for an effectiveness evaluation at the corresponding AUC24/MIC values (area under the serum concentration-time curve over 24h/minimum inhibitory concentration)."( Developments in the pharmacokinetic/pharmacodynamic index of linezolid: a step toward dose optimization using Monte Carlo simulation in critically ill patients.
Chen, L; Dong, H; Dong, Y; Sun, J; Wang, T; Xie, J; Zhao, Y, 2014
)
0.4
" A detailed in vitro structure-activity relationship of 1a in CLL compared to that of 22 synthetic analogues is described along with preliminary in vivo pharmacokinetic and metabolism studies on the most potent compounds."( Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies.
Castro, JE; Choi, MY; Molinski, TF; Stout, EP, 2014
)
0.4
" Multiple administrations of linezolid led to disappearance of significant differences in Cmax and AUC0-8 between plasma, inflamed, and non-inflamed tissue."( Target site pharmacokinetics of linezolid after single and multiple doses in diabetic patients with soft tissue infection.
Burian, A; Eslam, RB; Frenzel, D; Hammer, A; Kloft, C; Matzneller, P; Minichmayr, IK; Oesterreicher, Z; Sauermann, R; Vila, G; Zeitlinger, M, 2014
)
0.4
" The relationships between the plasma concentrations of U-480 and U-603 and intracellular whole-blood bactericidal activity (WBA) in ex vivo cultures were examined using a direct competitive population pharmacokinetic (PK)/pharmacodynamic 4-parameter sigmoid model."( Population pharmacokinetic/pharmacodynamic analysis of the bactericidal activities of sutezolid (PNU-100480) and its major metabolite against intracellular Mycobacterium tuberculosis in ex vivo whole-blood cultures of patients with pulmonary tuberculosis.
Diacon, A; Friedrich, SO; Wallis, RS; Zhu, T, 2014
)
0.4
"2 × Cmin + 134."( Analysis of thrombocytopenic effects and population pharmacokinetics of linezolid: a dosage strategy according to the trough concentration target and renal function in adult patients.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2014
)
0.4
" Intensive structure-activity relationship (SAR) and structure-pharmacokinetic relationship (SPR) studies on this new series led to the discovery of compound 11a: a highly potent, selective, direct, and orally bioavailable FXa inhibitor with excellent in vivo antithrombotic efficacy and preferable pharmacokinetic profiles."( Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.
Chen, X; Chu, W; Ding, S; Gong, G; Guo, B; Sun, P; Wang, H; Wang, Y; Xue, T; Yang, Y; Zhou, Y, 2014
)
0.4
"We performed a retrospective study of patients whose plasma C(min) and Cmax levels were measured during linezolid treatment."( Pharmacokinetic/pharmacodynamic evaluation of linezolid in hospitalized paediatric patients: a step toward dose optimization by means of therapeutic drug monitoring and Monte Carlo simulation.
Cojutti, P; Crichiutti, G; Isola, M; Maximova, N; Pea, F, 2015
)
0.42
"Linezolid pharmacokinetic profile in pediatric patients has not been fully characterized, and the dose needed to achieve a pharmacokinetic-pharmacodynamic (PK-PD) target has yet to be established because its efficacy is associated with the area under the plasma drug concentration-time curve (AUC24)/minimum inhibitory concentration (MIC) ratio."( Linezolid dosage in pediatric patients based on pharmacokinetics and pharmacodynamics.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2015
)
0.42
" To evaluate the potential of the novel oxazolidinone tedizolid to cause similar side effects, nonclinical and pharmacokinetic assessments were conducted."( Nonclinical and pharmacokinetic assessments to evaluate the potential of tedizolid and linezolid to affect mitochondrial function.
Das, D; Fiedler-Kelly, J; Flanagan, S; Hosako, H; McKee, EE; Passarell, J; Prokocimer, P; Radovsky, A; Tulkens, PM, 2015
)
0.42
" As a continuous, growth-control-normalised pharmacodynamic measure, the relative bacterial reduction (RBR) was introduced and derived."( Concentration-response studies and modelling of the pharmacodynamics of linezolid: Staphylococcus aureus versus Enterococcus faecium.
Derendorf, H; Kloft, C; Michael, J; Scheerans, C; Wicha, SG, 2015
)
0.42
"Anacetrapib, a cholesterol ester transfer protein (CETP) inhibitor, has been reported to have longer elimination half-life after longer treatment."( Assessment of the persistence of anacetrapib and evacetrapib concentrations using two pharmacokinetic modeling approaches.
Friedrich, S; Hall, SD; Ke, AB; Mantlo, N; Rotelli, M; Small, DS, 2015
)
0.42
"To evaluate the pharmacokinetic and pharmacodynamic (PK/PD) results of three different infusion time regimens of single doses of 600 mg linezolid in healthy Han Chinese volunteers."( Pharmacokinetic/pharmacodynamic research on three different infusion time regimens of linezolid in healthy Chinese volunteers.
Bai, N; Cai, Y; Liang, B; Liu, X; Wang, J; Wang, R, 2015
)
0.42
" No significant difference was found in pharmacokinetic parameters among the three different infusion regimens."( Pharmacokinetic/pharmacodynamic research on three different infusion time regimens of linezolid in healthy Chinese volunteers.
Bai, N; Cai, Y; Liang, B; Liu, X; Wang, J; Wang, R, 2015
)
0.42
"Limited pharmacokinetic sampling strategy may be useful for predicting the area under the curve (AUC) for triptans and may have clinical utility as a prospective tool for prediction."( Intranasal Pharmacokinetic Data for Triptans Such as Sumatriptan and Zolmitriptan Can Render Area Under the Curve (AUC) Predictions for the Oral Route: Strategy Development and Application.
Srinivas, NR; Syed, M, 2016
)
0.43
" We review its pharmacokinetic properties."( Pharmacokinetic drug evaluation of anacetrapib for the treatment of dyslipidemia.
Borghi, C; Cicero, AF, 2017
)
0.46
" There are no studies describing the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" Herein, we described the preparation, pharmacokinetic properties, tissue distribution, efficacy and toxicity of PZ-M."( Improving the pharmacokinetics and tissue distribution of pyrinezolid by self-assembled polymeric micelles.
Deng, Y; Guo, G; He, G; Li, X; Li, Z; Long, H; Luo, Y; Mei, L; Sang, Z; Wang, Z; Yang, T; Zheng, Y; Zhou, L, 2017
)
0.46
" These antimicrobial agents exhibit a favourable pharmacokinetic profile with an excellent bioavailability and a good tissue and organ penetration."( Clinical Pharmacokinetics and Pharmacodynamics of Oxazolidinones.
Muller, L; Roberts, JA; Roger, C, 2018
)
0.48
"7), and peak concentration was 38."( Steady state pharmacokinetics of cycloserine in patients on terizidone for multidrug-resistant tuberculosis.
Court, R; de Vries, N; Gumbo, T; Harding, J; Maartens, G; McIlleron, H; Stewart, A; Wiesner, L, 2018
)
0.48
" The non-clinical pharmacokinetic profiles of rovatirelin, a novel thyrotropin-releasing hormone (TRH) analogue, were investigated in vivo and in vitro."( Non-clinical pharmacokinetic profiles of rovatirelin, an orally available thyrotropin-releasing hormone analogue.
Abe, Y; Endo, T; Harada, H; Kobayashi, K; Oota, E; Takeda, H, 2019
)
0.51
" Although there was no apparent race-related pharmacokinetic effect, attenuation of the lipid response was observed in black subjects."( Pharmacokinetics and Pharmacodynamics of Anacetrapib in Black and White Healthy Subjects.
Corr, C; Cote, J; Gheyas, F; Gutstein, DE; Krishna, R; Liu, Y; Wagner, J, 2018
)
0.48
" The goal of this investigation was to evaluate the pharmacokinetics, pharmacodynamics, safety, and tolerability of multiple-dose LCB01-0371 as well as the pharmacokinetic characteristics of a new 400-mg tablet formulation."( Multiple-dose Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Oral LCB01-0371 in Healthy Male Volunteers.
Bae, KS; Cho, YL; Cho, YS; Lim, HS; Nam, HS, 2018
)
0.48
" The method was successfully applied to evaluate the possible conversion of WCK 3023 to RE in rat serum samples during pre-clinical pharmacokinetic studies."( Chiral separation and thermodynamic investigation of WCK 3023: A novel oxazolidinone antibacterial agent, application to pre-clinical pharmacokinetic study.
Ahirrao, V; Jadhav, R; Patel, A; Patil, K; Patil, V; Rane, V; Yeole, R, 2019
)
0.51
"This study assessed the tolerability and pharmacokinetic (PK) properties of a new-generation oxazolidinone, contezolid (MRX-I), and its major inactive metabolite, M2, after single oral administrations of 800, 1200, and 1600 mg in the fed state, and compared the efficacy of 3 dosing regimens in the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infection based on PK/pharmacodynamic (PD) analysis."( Tolerability and Pharmacokinetics of Contezolid at Therapeutic and Supratherapeutic Doses in Healthy Chinese Subjects, and Assessment of Contezolid Dosing Regimens Based on Pharmacokinetic/Pharmacodynamic Analysis.
Cao, G; Chen, Y; Guo, B; Guo, Y; Hu, F; Wang, Y; Wu, H; Wu, J; Wu, X; Yu, J; Yuan, H; Zhang, J; Zhu, D, 2019
)
0.51
", responsible for antiviral antiendotoxin activity; however, few pharmacokinetic studies have been conducted."( Metabolic profiles and pharmacokinetics of goitrin in rats through liquid chromatography combined with electrospray ionization-tandem mass spectrometry.
Han, H; Li, J; Shi, Y; Wang, R; Wang, Z; Xu, Y; Yang, L, 2019
)
0.51
" The nasal spray was prepared from Zolmitriptan loaded chitosan nanoparticles and evaluated for pharmacokinetic properties."( Pharmacokinetic study and brain tissue analysis of Zolmitriptan loaded chitosan nanoparticles in rats by LC-MS method.
Bukka, R; Khezri, FANZ; Lakshmi, CSR; Nargund, SL; Nidhi, M, 2020
)
0.56
" The resulting optimized compound, BAY1217224, has reached first clinical trials, which have confirmed the desired pharmacokinetic properties."( Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
Allerheiligen, S; Gericke, KM; Gnoth, M; Heitmeier, S; Hillig, RC; Hillisch, A; Lienau, P; Puetter, V; Roehrig, S; Schaefer, M; Schulz, S; Tersteegen, A, 2020
)
0.56
" The incorporation of the NLCs in in situ gelling hard gelatin capsules fulfilled a dual function in increasing permeability, as well as sustaining the pharmacodynamic effect."( Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles - Formulation and Pharmacodynamic Assessment.
Awadeen, RH; Boughdady, MF; Meshali, MM, 2020
)
0.56
" To support the use of tedizolid phosphate in adolescents with ABSSSIs, a population pharmacokinetic (PK) model, developed using adult and pediatric data, was updated to include PK data from a phase 3 clinical trial (PN012) that evaluated the safety and efficacy of once-daily oral or intravenous 200-mg tedizolid phosphate treatment in adolescents (12 to <18 years) with ABSSSIs, along with emerging data from a phase 1 trial (PN013) in children (2 to <12 years)."( Population Pharmacokinetics, Exposure-Response, and Probability of Target Attainment Analyses for Tedizolid in Adolescent Patients with Acute Bacterial Skin and Skin Structure Infections.
Broyde, N; Chou, MZ; De Anda, CS; Duval, V; Feng, HP; Guiastrennec, B; Hardalo, C; Li, D; Ouerdani, A; Rizk, ML; Sabato, PE; Sears, PS, 2021
)
0.62
" The aim of the review was to summarize and critically review the key pharmacokinetic and pharmacodynamic aspects of tedizolid."( Pharmacokinetics and Pharmacodynamics of Tedizolid.
Iqbal, K; Milioudi, A; Wicha, SG, 2022
)
0.72

Compound-Compound Interactions

ExcerptReferenceRelevance
" Zolmitriptan, at eight times the likely therapeutic dose, was generally well tolerated both alone and in combination with ergotamine."( Peripheral vascular effects and pharmacokinetics of the antimigraine compound, zolmitriptan, in combination with oral ergotamine in healthy volunteers.
Dixon, RM; Evans, DH; Meire, HB; On, N; Posner, J; Rolan, PE; Watt, H, 1997
)
0.3
" When combined with gentamicin (MIC/4 concentration), rapid bactericidal action was observed against all streptococci tested, but not against the staphylococci."( AZD2563, a new oxazolidinone: bactericidal activity and synergy studies combined with gentamicin or vancomycin against staphylococci and streptococcal strains.
Anderegg, TR; Deshpande, LM; Jones, RN, 2002
)
0.31
"The in vitro activity of the oxazolidinone linezolid was studied alone and in combination with three antibiotics acting on different cellular targets."( In vitro activity of linezolid alone and in combination with gentamicin, vancomycin or rifampicin against methicillin-resistant Staphylococcus aureus by time-kill curve methods.
Bugnon, D; Caillon, J; Donnio, PY; Jacqueline, C; Le Mabecque, V; Miegeville, AF; Potel, G, 2003
)
0.32
"The activities of linezolid, an oxazolidinone antibacterial agent active against gram-positive organisms, alone and in combination with 35 antimicrobial agents were tested in vitro against methicillin-sensitive (n = 1 to 2 strains) and methicillin-resistant (n = 8 to 10) Staphylococcus aureus strains; vancomycin-sensitive (n = 6) and vancomycin-resistant (n = 6 to 8) Enterococcus faecalis strains; vancomycin-sensitive (n = 5) and vancomycin-resistant (n = 6) Enterococcus faecium strains; penicillin-sensitive (n = 2 to 5), penicillin-intermediate (n = 5 to 6), and penicillin-resistant (n = 5 to 6) Streptococcus pneumoniae strains; Escherichia coli (n = 6); and Klebsiella pneumoniae (n = 6)."( In vitro activities of linezolid combined with other antimicrobial agents against Staphylococci, Enterococci, Pneumococci, and selected gram-negative organisms.
Sweeney, MT; Zurenko, GE, 2003
)
0.32
"A rat model was used to investigate the efficacy of linezolid, alone or in combination with levofloxacin and vancomycin, in the prevention of vascular prosthetic graft infection resulting from methicillin-resistant Staphylococcus epidermidis with intermediate resistance to glycopeptides."( Prophylactic efficacy of linezolid alone or combined with levofloxacin and vancomycin in a rat subcutaneous pouch model of graft infection caused by Staphylococcus epidermidis with intermediate resistance to glycopeptides.
Cirioni, O; D'Amato, G; Del Prete, MS; Ghiselli, R; Giacometti, A; Mocchegiani, F; Orlando, F; Saba, V; Scalise, G; Silvestri, C, 2003
)
0.32
" The purpose of this study was to evaluate the in vivo activity of linezolid combined with gentamicin using a methicillin-resistant Staphylococcus aureus (MRSA) endocarditis experimental model."( In vivo efficacy of linezolid in combination with gentamicin for the treatment of experimental endocarditis due to methicillin-resistant Staphylococcus aureus.
Asseray, N; Batard, E; Bugnon, D; Caillon, J; Dube, L; Jacqueline, C; Kergueris, MF; Le Mabecque, V; Potel, G, 2004
)
0.32
"Indifference or moderate antagonism of linezolid combined with other antibiotics in vitro and in vivo have mainly been reported in the literature."( In vitro and in vivo synergistic activities of linezolid combined with subinhibitory concentrations of imipenem against methicillin-resistant Staphylococcus aureus.
Batard, E; Bugnon, D; Caillon, J; Jacqueline, C; Kergueris, MF; Le Mabecque, V; Miegeville, AF; Navas, D; Potel, G, 2005
)
0.33
" Linezolid is a weak monoamine oxidase inhibitor and has been reported to interact with selective serotonin reuptake inhibitors (SSRIs)."( Drug interactions between linezolid and selective serotonin reuptake inhibitors: case report involving sertraline and review of the literature.
Andrus, MR; Byrd, DC; Clark, DB, 2006
)
0.33
"Linezolid in combination with ertapenem showed in vitro synergy against methicillin-resistant Staphylococcus aureus strains."( In vitro and in vivo assessment of linezolid combined with ertapenem: a highly synergistic combination against methicillin-resistant Staphylococcus aureus.
Batard, E; Bugnon, D; Caillon, J; Grossi, O; Jacqueline, C; Le Mabecque, V; Miegeville, AF; Potel, G, 2006
)
0.33
" To explore strategies to overcome resistance development, we studied the effects of rifalazil in combination with several different antibiotics in an in vitro time-kill model, against both log phase and stationary phase Staphylococcus aureus cells."( Enhanced activity of rifalazil in combination with levofloxacin, linezolid, or mupirocin against Staphylococcus aureus in vitro.
Murphy, CK; Osburne, MS; Rothstein, DM, 2006
)
0.33
"The objective of this paper was to investigate the in vitro effects of linezolid combined with five antistaphylococcal antibiotics--doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin--upon methicillin-susceptible Staphylococcus aureus (MSSA)."( In vitro activity of linezolid in combination with doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin against methicillin-susceptible Staphylococcus aureus.
Cantón, E; Colombo Gainza, E; Gil Brusola, A; Gobernado, M; Ortiz Estévez, R; Sahuquillo Arce, JM, 2006
)
0.33
" The objective of this study was also to determine the effects of the interaction of linezolid when it was combined with rifampicin and test this effect against strains of methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis."( Linezolid alone and in combination with rifampicin prevents experimental vascular graft infection due to methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis.
Baltalarli, A; Duver, H; Goksin, I; Kaan Inan, B; Kaleli, I; Onem, G; Ozcan, V; Sacar, M; Sacar, S; Turgut, H, 2007
)
0.34
" This study describes the synergistic activity of oritavancin in combination with gentamicin, linezolid, moxifloxacin, or rifampin in time-kill studies against methicillin-susceptible, vancomycin-intermediate, and vancomycin-resistant Staphylococcus aureus."( Assessment by time-kill methodology of the synergistic effects of oritavancin in combination with other antimicrobial agents against Staphylococcus aureus.
Arhin, FF; Belley, A; McKay, GA; Moeck, G; Neesham-Grenon, E; Parr, TR, 2008
)
0.35
"The knowledge about efficacy of linezolid alone or in combination with rifampin in device infections is limited."( Efficacy of linezolid alone and in combination with rifampin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Domenech, A; Euba, G; Gudiol, F; Murillo, O; Tubau, F; Verdaguer, R, 2008
)
0.35
"Linezolid alone showed moderate efficacy, whereas its combination with rifampin prevented the emergence of rifampin resistance."( Efficacy of linezolid alone and in combination with rifampin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Domenech, A; Euba, G; Gudiol, F; Murillo, O; Tubau, F; Verdaguer, R, 2008
)
0.35
"We investigated the activity of linezolid, alone and in combination with rifampin (rifampicin), against a methicillin-resistant Staphylococcus aureus (MRSA) strain in vitro and in a guinea pig model of foreign-body infection."( Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
Baldoni, D; Haschke, M; Rajacic, Z; Trampuz, A; Zimmerli, W, 2009
)
0.35
" In vitro, fosfomycin showed a synergistic effect when combined with the other antimicrobials tested."( Efficacy of fosfomycin and its combination with linezolid, vancomycin and imipenem in an experimental peritonitis model caused by a Staphylococcus aureus strain with reduced susceptibility to vancomycin.
Ariza, J; Cabellos, C; Domínguez, MA; Fernández, R; Gudiol, F; Pachón-Ibáñez, ME; Ribes, S; Tubau, F, 2011
)
0.37
" The aim of this study was to evaluate the efficacies of daptomycin at usual and high doses (equivalent to 6 and 10 mg/kg of body weight/day, respectively, in humans) and in combination with rifampin and to compare the activities to those of conventional anti-MRSA therapies."( Efficacy of usual and high doses of daptomycin in combination with rifampin versus alternative therapies in experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
Ariza, J; Cabellos, C; Cabo, J; Euba, G; Garrigós, C; Murillo, O; Tubau, F; Verdaguer, R, 2010
)
0.36
" Treatment with linezolid combined with TMP-SMZ resulted in a clear clinical improvement and bacterial clearance."( Linezolid combined with trimethoprim-sulfamethoxazole therapy for the treatment of disseminated nocardiosis.
Li, H; Shen, Q; Zhou, H; Zhou, J, 2011
)
0.37
" When combined with 8 mg/L rifampicin, MBECs for ciprofloxacin and linezolid dropped to 16-32 mg/L for the four isolates tested."( Effectiveness of ciprofloxacin or linezolid in combination with rifampicin against Enterococcus faecalis in biofilms.
Holmberg, A; Mörgelin, M; Rasmussen, M, 2012
)
0.38
"Serotonin syndrome can be a rare but life-threatening condition that is commonly the result of a drug-drug interaction causing excessive serotonin activity."( Probable drug-drug interaction leading to serotonin syndrome in a patient treated with concomitant buspirone and linezolid in the setting of therapeutic hypothermia.
Morrison, EK; Rowe, AS, 2012
)
0.38
" We carried out this study to determine the mutant prevention concentration (MPC) of linezolid when combined with minocycline against VRE strains, to determine the mechanism of drug resistance in vitro, and to provide a theoretical basis for the rational use of drugs against VRE."( Antimicrobial activity of linezolid combined with minocycline against vancomycin-resistant Enterococci.
Jiang, TT; Li, L; Su, JR; Wu, J, 2013
)
0.39
" decreased dramatically when combined with minocycline, and vice versa."( Antimicrobial activity of linezolid combined with minocycline against vancomycin-resistant Enterococci.
Jiang, TT; Li, L; Su, JR; Wu, J, 2013
)
0.39
" coli and MRSA when ranalexin was used in combination with antibiotics, even at concentrations of 1/4 MIC or 1/2 MIC of ranalexin, respectively."( Secretory ranalexin produced in recombinant Pichia pastoris exhibits additive or synergistic bactericidal activity when used in combination with polymyxin B or linezolid against multi-drug resistant bacteria.
Aleinein, RA; Schäfer, H; Wink, M, 2014
)
0.4
"The objective of this paper was to investigate the in vitro effects of fosfomycin combined with linezolid against methicillin-resistant Staphylococcus aureus (MRSA)."( In vitro activity of fosfomycin in combination with linezolid against clinical isolates of methicillin-resistant Staphylococcus aureus.
De-feng, L; Dong, W; Falagas, ME; Karageorgopoulos, DE; Rui, W; Xu-hong, Y, 2014
)
0.4
"Ion mobility was performed on stored plasma samples collected from patients before and after treatment with anacetrapib alone (150 and 300 mg/d) or in combination with atorvastatin (20 mg/d) in a previously conducted 8-week phase IIb study."( Changes in LDL particle concentrations after treatment with the cholesteryl ester transfer protein inhibitor anacetrapib alone or in combination with atorvastatin.
Dansky, HM; Johnson-Levonas, AO; Krauss, RM; Liu, Y; Pinto, CA,
)
0.13
"Warfarin is known to interact with many drugs; however, there are currently no descriptions of an interaction with linezolid in the literature."( Potential drug interaction between warfarin and linezolid.
Arima, C; Hidaka, H; Kakuma, T; Masunaga, K; Miura, M; Naito, T; Qin, L; Sakai, Y; Watanabe, H, 2015
)
0.42
"Oxazolidinone pharmacology including structure-activity relationships, mode of action, pharmacokinetics, drug-drug interactions, and adverse drug reactions is reviewed."( Drug-drug interactions and safety of linezolid, tedizolid, and other oxazolidinones.
Douros, A; Grabowski, K; Stahlmann, R, 2015
)
0.42
"Rifampin (RIF) plus clarithromycin (CLR) for 8 weeks is now the standard of care for Buruli ulcer (BU) treatment, but CLR may not be an ideal companion for rifamycins due to bidirectional drug-drug interactions."( Oxazolidinones Can Replace Clarithromycin in Combination with Rifampin in a Mouse Model of Buruli Ulcer.
Almeida, DV; Converse, PJ; Grosset, JH; Lee, J; Li, SY; Nuermberger, EL; Omansen, TF, 2019
)
0.51
" Zoliflodacin was evaluated alone or combined with ceftriaxone, cefixime, spectinomycin, gentamicin, tetracycline, cethromycin or sitafloxacin in chequerboard assays, time-kill curve analysis and selection-of-resistance studies."( In vitro antimicrobial combination testing of and evolution of resistance to the first-in-class spiropyrimidinetrione zoliflodacin combined with six therapeutically relevant antimicrobials for Neisseria gonorrhoeae.
Alirol, E; Drusano, G; Foerster, S; Golparian, D; Neely, M; Piddock, LJV; Unemo, M, 2019
)
0.51
"Zoliflodacin alone or in combination with all six antimicrobials showed rapid growth inhibition against all examined strains."( In vitro antimicrobial combination testing of and evolution of resistance to the first-in-class spiropyrimidinetrione zoliflodacin combined with six therapeutically relevant antimicrobials for Neisseria gonorrhoeae.
Alirol, E; Drusano, G; Foerster, S; Golparian, D; Neely, M; Piddock, LJV; Unemo, M, 2019
)
0.51
"Zoliflodacin, alone or in combination with sexually transmitted infection therapeutic antimicrobials, rapidly kills gonococci with infrequent resistance emergence."( In vitro antimicrobial combination testing of and evolution of resistance to the first-in-class spiropyrimidinetrione zoliflodacin combined with six therapeutically relevant antimicrobials for Neisseria gonorrhoeae.
Alirol, E; Drusano, G; Foerster, S; Golparian, D; Neely, M; Piddock, LJV; Unemo, M, 2019
)
0.51
" Delpazolid is administered in combination with bedaquiline, delamanid and moxifloxacin."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91

Bioavailability

The transepithelial passage of the orally bioavailable antibacterial agent oxazolidin-2-one (OXa) and 10 derivatives has been studied with human intestinal (Caco-2) and canine renal (MDCK) cell lines grown on polycarbonate filters. An ultra-high performance liquid chromatography/tandem mass spectrometry (UPLC-MS/MS) method has been developed to support a clinical study.

ExcerptReferenceRelevance
" This pharmacodynamic interaction could be explained by an increase in tyramine systemic bioavailability in the presence of toloxatone."( Pharmacokinetic and pharmacodynamic interaction between toloxatone, a new reversible monoamine oxidase-A inhibitor, and oral tyramine in healthy subjects.
D'Estanque, J; Ego, D; Funck-Brentano, C; Jaillon, P; Provost, JC; Rovei, V, 1992
)
0.28
" Although cimoxatone solubility in water is only 5 ppm, the drug appears to be well absorbed as indicated by the tight conformity of the pharmacokinetic parameters."( Pharmacokinetic and relative bioavailability studies of cimoxatone in humans.
Kendall, MJ; Mitchard, M; Rovei, V; Strolin Benedetti, M, 1984
)
0.27
" The original drug tested here, (5R)-3-[2-(3-cyanopropyl)benzothiazol-6-yl]-5-methoxymethyl-2-oxaz olidinone (ER-4539), exhibited strong MAO-A inhibitory activity in vitro, but its bioavailability in rat was very low."( Application of pharmacokinetic studies to a novel antidepressant, E2011.
Akasaka, K; Horie, T; Kagaya, T; Kubota, A; Nagato, S; Naitoh, T, 1994
)
0.29
"The Upjohn oxazolidinones, U-100592 and U-100766, are orally bioavailable synthetic antimicrobial agents with spectra of activity against antibiotic-susceptible and -resistant gram-positive pathogens."( In vivo activities of U-100592 and U-100766, novel oxazolidinone antimicrobial agents, against experimental bacterial infections.
Barbachyn, MR; Brickner, SJ; Ford, CW; Hamel, JC; Hutchinson, DK; Moerman, JK; Stapert, D; Wilson, DM; Yancey, RJ, 1996
)
0.29
"The transepithelial passage of the orally bioavailable antibacterial agent oxazolidin-2-one (OXa) and 10 derivatives has been studied with human intestinal (Caco-2) and canine renal (MDCK) cell lines grown on polycarbonate filters."( Transport of the antibacterial agent oxazolidin-2-one and derivatives across intestinal (Caco-2) and renal (MDCK) epithelial cell lines.
Guba, W; Islam, K; Ranaldi, G; Sambuy, Y; Seneci, P, 1996
)
0.8
" It is rapidly absorbed, with 75% of maximal plasma concentration (Cmax) attained within 1 hour and good absolute oral bioavailability (approximately 40%)."( 311C90: increasing the options for therapy with effective acute antimigraine 5HT1B/1D receptor agonists.
Ferrari, MD, 1997
)
0.3
"Two open studies in healthy volunteers were conducted to determine the absolute bioavailability and metabolic disposition of zolmitriptan (311C90), a novel 5HT1D agonist for the acute treatment of migraine."( The absolute bioavailability and metabolic disposition of the novel antimigraine compound zolmitriptan (311C90).
Chittick, G; Dixon, RM; Gibbens, M; Leavens, WJ; Liptrot, J; On, N; Pack, RW; Posner, J; Rolan, PE; Seaber, E, 1997
)
0.3
" Zolmitriptan has suitable bioavailability for an acute oral migraine treatment and there are no significant unidentified metabolites in man."( The absolute bioavailability and metabolic disposition of the novel antimigraine compound zolmitriptan (311C90).
Chittick, G; Dixon, RM; Gibbens, M; Leavens, WJ; Liptrot, J; On, N; Pack, RW; Posner, J; Rolan, PE; Seaber, E, 1997
)
0.3
" In healthy volunteers it is rapidly and extensively absorbed and has favorable oral bioavailability (approximately 40%) which is not affected by concomitant food intake."( The clinical pharmacokinetics of zolmitriptan.
Dixon, R; Warrander, A, 1997
)
0.3
"Concomitant administration of zolmitriptan and paracetamol resulted in a slight increase in bioavailability of zolmitriptan and a reduced rate and extent of paracetamol absorption."( The novel anti-migraine compound zolmitriptan (Zomig 311C90) has no clinically significant interactions with paracetamol or metoclopramide.
Layton, G; Peck, RW; Posner, J; Ridout, G; Seaber, EJ, 1997
)
0.3
"At therapeutic doses zolmitriptan has good oral bioavailability in healthy volunteers and has dose-proportional pharmacokinetics that are not affected by food to any clinically relevant extent."( The absolute bioavailability and effect of food on the pharmacokinetics of zolmitriptan in healthy volunteers.
Allanson, J; Hefting, NR; Jonkman, JH; Peck, RW; Seaber, EJ; Smith, DA; Sollie, FA; van Lier, JJ; Wemer, J, 1998
)
0.3
"Zolmitriptan is a new serotonergic agonist with excellent oral bioavailability exhibiting a potent symptomatic antimigraine effect."( [Mechanism of action of zolmitriptan].
Pascual, J, 1998
)
0.3
"Zolmitriptan (previously known as 311C90) is a serotoninergic 5-HT1B/D agonist with high oral bioavailability with a double, central and peripheral, action mechanism."( [Clinical efficacy of zolmitriptan in migraine].
Leira, R; Noya, M, 1998
)
0.3
" Linezolid, the oxazolidinone which has been selected for clinical development, has near complete oral bioavailability plus favourable pharmacokinetic and toxicity profiles."( Oxazolidinones: a review.
Diekema, DI; Jones, RN, 2000
)
0.31
" Zolmitriptan introduced in 1994 is an agonists of 5-HT 1B/1D receptor, is active both peripherally and centrally, is well absorbed from the digestive tract and has a good bioavailability index /40%/."( [Emergency treatment of migraine attacks with particular reference to agonists of 5-HT1B/1D receptor].
Prusiński, A, 1999
)
0.3
" It has good pharmacokinetics, with equal bioavailability by both oral and intravenous routes and no need for dose adjustment in patients with renal impairment."( Linezolid.
French, G,
)
0.13
" Linezolid has almost 100% bioavailability and the area under the plasma concentration curve is identical after oral and iv."( Linezolid--a review of the first oxazolidinone.
Norrby, R, 2001
)
0.31
" Linezolid may be administered either intravenously or orally with oral bioavailability of approximately 100% and limited adverse effects."( The oxazolidinones as a new family of antimicrobial agent.
Marchese, A; Schito, GC, 2001
)
0.31
" The objectives of this study were twofold: (1) to compare the absorption of linezolid tablets given immediately following a high-fat meal with the absorption of tablets administered while fasting, and (2) to assess the bioavailability of a 375-mg oral dose given while fasting relative to a 375-mg dose of linezolid sterile solution given intravenously."( Linezolid absolute bioavailability and the effect of food on oral bioavailability.
Hopkins, NK; Jungbluth, GL; Sisson, TA; Stalker, DJ; Welshman, IR, 2001
)
0.31
" Linezolid is a parenteral agent that also possesses near-complete oral bioavailability plus favourable pharmacokinetic and toxic effect profiles."( Oxazolidinone antibiotics.
Diekema, DJ; Jones, RN, 2001
)
0.31
" It is well absorbed with high bioavailability that allows conversion to oral therapy as soon as the patient is clinically stable."( Linezolid: its role in the treatment of gram-positive, drug-resistant bacterial infections.
Ament, PW; Horne, JP; Jamshed, N, 2002
)
0.31
" bioavailability of > 95% in rat and dog, and > 70% in mouse."( Pharmacokinetics, toxicokinetics, distribution, metabolism and excretion of linezolid in mouse, rat and dog.
Adams, LA; Bush, EC; Chiba, K; Daley-Yates, PT; Feenstra, KL; Koike, S; Ozawa, N; Peng, GW; Sams, JP; Schuette, MR; Slatter, JG; Yamazaki, S, 2002
)
0.31
" LZD is rapidly absorbed following oral administration and bioavailability when compared with intravenous administration is almost 100%."( [Antimicrobial and clinical effect of linezolid (ZYVOX), new class of synthetic antibacterial drug].
Hashimoto, M; Irinoda, K; Nomura, S, 2002
)
0.31
" Oral bioavailability in humans was determined to be 100% and twice daily dosing in humans resulted in blood levels which even at trough values were in excess of the MIC90 for significant Gram-positive pathogens."( The discovery of linezolid, the first oxazolidinone antibacterial agent.
Barbachyn, MR; Ford, CW; Zurenko, GE, 2001
)
0.31
" Virtually complete oral bioavailability allows for 1:1 conversion between the intravenous and oral dosage forms."( Linezolid: an oxazolidinone antimicrobial agent.
Paladino, JA, 2002
)
0.31
" The almost-complete bioavailability of linezolid permits oral administration."( Quinupristin-dalfopristin and linezolid: evidence and opinion.
Eliopoulos, GM, 2003
)
0.32
"Linezolid, an oxazolidinone antibiotic, has 100% oral bioavailability and favorable activities against gram-positive pathogens including multidrug-resistant staphylococci, enterococci, and pneumococci."( Worldwide assessment of linezolid's clinical safety and tolerability: comparator-controlled phase III studies.
Cammarata, S; Hafkin, B; Isturiz, R; Le, V; Oliphant, TH; Remington, J; Rubinstein, E; Smith, LG; Standiford, HC, 2003
)
0.32
" Finally, these predicted values were compared to previously measured bioavailability data in the rat in order to estimate oral absorption properties."( Predicting oral absorption of drugs: a case study with a novel class of antimicrobial agents.
Adams, WJ; Biermacher, JJ; Burton, PS; Day, JS; Friis, JM; Hilgers, AR; Hosley, JD; Jensen, JL; Palandra, J; Shobe, EM; Sims, SM; Smith, DP, 2003
)
0.32
"A reasonably good correlation between predicted dose absorbed and bioavailability was observed for most of the compounds."( Predicting oral absorption of drugs: a case study with a novel class of antimicrobial agents.
Adams, WJ; Biermacher, JJ; Burton, PS; Day, JS; Friis, JM; Hilgers, AR; Hosley, JD; Jensen, JL; Palandra, J; Shobe, EM; Sims, SM; Smith, DP, 2003
)
0.32
" Linezolid has complete bioavailability in parenteral and oral administration, is well tolerated and shows little toxicity, thus favoring a shortened hospital stay, improving the patient's quality of life and reducing social costs."( Treatment of gram-positive surgical sepsis: role of the oxazolidinones.
Carnuccio, P; Colizza, S; Cucchiara, G; Rodio, F; Rossi, S, 2003
)
0.32
" Oral linezolid has excellent bioavailability and activity against MRSA and MR-CoNS and offers the potential for outpatient treatment of MRSA and MR-CoNS infections."( Early switch and early discharge opportunities in intravenous vancomycin treatment of suspected methicillin-resistant staphylococcal species infections.
Goetz, MB; Parodi, S; Rhew, DC,
)
0.13
" Also, some nasal preparations have significant adverse effects or are not well absorbed and therefore do not work consistently; others are more challenging to administer as a result of their delivery apparatus."( Intranasal medications for the treatment of migraine and cluster headache.
Bigal, ME; Rapoport, AM; Sheftell, FD; Tepper, SJ, 2004
)
0.32
" Linezolid possesses a high activity against all multiresistant gram-positive cocci, favourable pharmacokinetics, a good safety profile, a complete bioavailability after and administration permitting switch therapy, a low capacity of inducing resistance, and both clinical and microbiologic efficacy as demonstrated by a number of clinical trials conducted on thousands of patients."( [The role of linezolid in the therapy of infections caused by multiresistant gram-positive cocci].
Corti, G; Paradisi, F, 2004
)
0.32
" The compound's excellent oral bioavailability and reasonable safety profile, along with the increasing incidence of resistant infections, means that linezolid offers a valuable alternative to more traditional therapies such as vancomycin."( The safety and efficacy of linezolid in orthopaedic practice for the treatment of infection due to antibiotic-resistant organisms.
Giannoudis, PV; Harwood, PJ, 2004
)
0.32
" The excellent bioavailability after oral administration (almost 100%) makes it suitable for outpatient treatment and treatment by general practitioners."( [Linezolid, an agent from a new class of antibiotics].
Bernards, AT; Kuijper, EJ; Schippers, EF, 2004
)
0.32
" The proposed method enables the unambiguous identification and quantification of zolmitriptan for pharmacokinetic, bioavailability or bioequivalence studies."( Quantification of zolmitriptan in plasma by high-performance liquid chromatography-electrospray ionization mass spectrometry.
Li, W; Mao, G; Tian, Y; Xu, F; Zhang, Z, 2004
)
0.32
"Linezolid is an oxazolidinone antimicrobial with excellent oral bioavailability and tissue penetration and is active against multidrug-resistant skin/soft tissue pathogens."( Pharmacokinetics and pharmacodynamics of linezolid in obese patients with cellulitis.
Citron, DM; Goldstein, EJ; Havlichek, DH; Kak, V; Peloquin, CA; Schooley, SL; Stein, GE; Tyrrell, KL, 2005
)
0.33
" With an excellent oral bioavailability and acceptable safety profile, linezolid offers a valuable alternative to more traditional therapies, such as glycopeptides."( Role of linezolid in the treatment of orthopedic infections.
Bassetti, D; Bassetti, M; Beltrame, A; Di Biagio, A; Righi, E; Rosso, R, 2005
)
0.33
" Therefore, the bioavailability of linezolid administered enterally in the presence of enteral feedings in hospitalized patients was examined."( Absolute bioavailability and pharmacokinetics of linezolid in hospitalized patients given enteral feedings.
Beringer, P; Gill, M; Gurevitch, M; Hoem, N; Louie, S; Nguyen, M; Wong-Beringer, A, 2005
)
0.33
" Linezolid is a pararental drug that also possesses near-complete oral bioavailability and a favourable pharmacokinetic profile."( Oxazolidinones--a new class of broad-spectrum chemotherapeutics.
Pasternak, K; Sztanke, K; Sztanke, M, 2004
)
0.32
" The oral bioavailability of linezolid is approximately 100%, thus allowing sequential intravenous-to-oral administration without changing the drug or dosage regimen."( Linezolid: a pharmacoeconomic review of its use in serious Gram-positive infections.
Figgitt, DP; Plosker, GL, 2005
)
0.33
"The aim of this study was to determine the bioavailability of a novel oxazolidinone, DRF-6196, in mice and rats following intravenous (i."( Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid.
Bhamidipati, R; Das, J; Dravid, PV; Mullangi, R; Narasimhulu, PC; Srinivas, NR; Tvrs, S; Venkatesh, P,
)
0.13
" With its oral bioavailability profiles, it obviously holds great promise."( In vitro activity of linezolid and other antibiotics against Gram-positive bacteria from the major teaching hospitals in Kuwait.
Al Sweih, N; Jamal, W; Mokaddas, E; Phillips, OA; Rotimi, VO, 2005
)
0.33
" Prosthesis retention, in conjunction with debridement and prolonged (for at least 3 months) oral antibiotic therapy, can be an alternative for early postoperative or late acute haematogenous infections, when the duration of symptoms is less than 1 month, the implant is stable, and the pathogen is relatively avirulent and sensitive to an orally well absorbed antibiotic."( Management of infections of osteoarticular prosthesis.
Barberán, J, 2006
)
0.33
" Linezolid is a new antibiotic with high bioavailability and an outstanding safety profile, synergistic with imipenem, which may deserve a place in the armamentarium for severe pneumonia in children."( Effectiveness of linezolid and imipenem association in the treatment of severe community-acquired pneumonia in children: two case reports.
Caillon, J; Christophe Roze, J; Denizot, S; Godon, N; Gras-Le Guen, C; Podevin, G; Potel, G, 2006
)
0.33
" Linezolid is the first of a new class of antimicrobial agents known as the oxazolidinones with activity against gram-positive bacteria similar to that of vancomycin and yet its oral bioavailability allows for enteral administration."( Preliminary experience with the use of oral linezolid in infants for the completion of antibiotic therapy in the outpatient setting after admission to the pediatric intensive care unit.
Sullivan, J; Tobias, JD,
)
0.13
" Linezolid is well absorbed in the intestinal system."( [Linezolid in the treatment of antibiotic-resistant gram-positive infections of the musculoskeletal system].
Jahoda, D; Landor, I; Nyc, O; Pokorný, D; Sosna, A, 2006
)
0.33
" Pharmacocinetics studies have shown that linezolid has an excellent bioavailability allowing a fast relay per os."( [Linezolid: antibacterial activity, clinical efficacy and resistance].
Bourgeois-Nicolaos, N; Butel, MJ; Doucet-Populaire, F; Piriou, O,
)
0.13
" It is well absorbed with high bioavailability after oral administration and generally well tolerated."( [Linezolid--novel antibiotic for the treatment of gram-positive bacterial infections].
Jankowski, A; Stefanik, W, 2006
)
0.33
"Linezolid is an attractive alternative for orthopedic infections because of oral bioavailability and activity against methicillin-resistant staphylococci and vancomycin-resistant enterococci."( Efficacy and safety of linezolid for Gram-positive orthopedic infections: a prospective case series.
Hamilton, CW; Rao, N, 2007
)
0.34
" Furthermore, in vivo efficacies and pharmacokinetic properties of the selected compounds were also disclosed herein; the selected compounds showed reasonable bioavailability as well as in vivo efficacy comparable to that of linezolid."( Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
Chen, Y; Fan, H; Ji, R; Jiang, Z; Yang, Y; Zhang, S; Zhong, D, 2008
)
0.35
"The excellent oral bioavailability and the Gram-positive antimicrobial spectrum make linezolid an attractive antibiotic for treatment of osteoarticular infections."( Experience with linezolid therapy in children with osteoarticular infections.
Chen, CJ; Chiu, CH; Huang, YC; Lee, ZL; Lin, TY; Yang, WE, 2007
)
0.34
" Burned crop residues may effectively adsorb pesticides and thus influence their bioavailability in agricultural soils."( Burned rice straw reduces the availability of clomazone to barnyardgrass.
Liu, W; Sheng, GD; Xu, C, 2008
)
0.35
" It has an excellent bioavailability both intravenously and orally and a very good safety profile both in adults and in children."( Linezolid in children: recent patents and advances.
Velissariou, IM, 2007
)
0.34
"We have developed a first generation of hybrid sparsomycin-linezolid compounds into a new family of orally bioavailable biaryloxazolidinones that have activity against both linezolid-susceptible and -resistant gram-positive bacteria as well as the fastidious gram-negative bacteria Haemophilus influenzae and Moraxella catarrahalis."( Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
Bhattacharjee, A; Chen, S; Chen, Y; Duffy, E; Farmer, J; Goldberg, J; Hanselmann, R; Ippolito, JA; Johnson, G; Lou, R; Orbin, A; Oyelere, A; Salvino, J; Springer, D; Tran, J; Wang, D; Wu, Y; Zhou, J, 2008
)
0.35
" We aimed to assess the clinical profile of MK-0974 (telcagepant), an orally bioavailable antagonist of CGRP receptor."( Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial.
Assaid, C; Dodick, DW; Fan, X; Ferrari, MD; Froman, S; Galet, V; Ho, TW; Koppen, H; Kost, J; Leibensperger, H; Lines, C; Winner, PK, 2008
)
0.35
" The availability of intravenous and oral formulations, with near 100% bioavailability of the latter, is hoped to facilitate the management of multiply drug-resistant Gram-positive infections."( Linezolid: a review of safety and tolerability.
Rubinstein, E; Vinh, DC, 2009
)
0.35
" Anacetrapib exhibited a low clearance in both species and a moderate oral bioavailability of approximately 38% in rats and approximately 13% in monkeys."( Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys.
Bradley, S; Braun, MP; Chen, Q; Dean, DC; Doss, G; Hartmann, G; Ho, JZ; Kumar, S; Pereira, A; Tan, EY; Tang, W; Zhang, AS, 2010
)
0.36
" The compound was well absorbed and exhibited approximately linear pharmacokinetics in the oral dose range of 100 to 1000 mg in human."( Preclinical and clinical evidence for the collaborative transport and renal secretion of an oxazolidinone antibiotic by organic anion transporter 3 (OAT3/SLC22A8) and multidrug and toxin extrusion protein 1 (MATE1/SLC47A1).
Adams, WJ; Balogh, LM; Brayman, TG; Cox, SR; Kumar, V; Lai, Y; Sampson, KE; Stevens, JC, 2010
)
0.36
" PNU-100480 doses to 1000 mg were well absorbed and showed approximately proportional increases in exposures of parent and metabolites."( Pharmacokinetics and whole-blood bactericidal activity against Mycobacterium tuberculosis of single doses of PNU-100480 in healthy volunteers.
Campbell, S; Dimitrova, D; Friedland, G; Jakubiec, WM; Kumar, V; Ladutko, L; Li, X; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, AM; Wallis, RS, 2010
)
0.36
" Moreover, the availability of intravenous and oral formulation with an excellent bioavailability of the latter, is hoped to facilitate the management of these infections."( [Linezolide in paediatrics].
Ménager, C; Moulin, F, 2010
)
0.36
" The population pharmacokinetic model described differences between the liquid-filled capsule used in phase I and phase IIb and the hot-melt extruded (HME) tablet formulation introduced in phase III, allowing for bridging of the two formulations, and quantified the complex relationship of apparent anacetrapib bioavailability with subject meal intake."( Model-based development of anacetrapib, a novel cholesteryl ester transfer protein inhibitor.
Bergman, AJ; Dockendorf, MF; Dykstra, K; Green, M; Krishna, R; Wagner, JA, 2011
)
0.37
" It is unique amongst antibiotics active against most multiply-resistant Gram-positive bacteria in that there is an oral preparation with 100% bioavailability and an extensive volume of distribution."( Linezolid pharmacokinetics and pharmacodynamics in clinical treatment.
Dryden, MS, 2011
)
0.37
"Fusidic acid (CEM-102), an orally bioavailable fusidane antibiotic with a unique mode of action, is under development for treatment of acute gram-positive bacterial skin and skin structure infections, including those caused by methicillin-susceptible and methicillin-resistant Staphylococcus aureus and streptococci."( A randomized, double-blind phase 2 study comparing the efficacy and safety of an oral fusidic acid loading-dose regimen to oral linezolid for the treatment of acute bacterial skin and skin structure infections.
Clark, K; Corey, GR; Craft, JC; Das, A; Degenhardt, TP; Fernandes, P; Moriarty, SR; Scott, D; Still, JG, 2011
)
0.37
" This compound also showed excellent pharmacokinetic profiles, with a half-life of more than 5 h as well as an oral bioavailability of 81% in rats."( Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
Fan, H; Gao, S; Guo, B; He, H; Huang, Y; Wang, H; Xin, Q; Yang, Y, 2011
)
0.37
" Its current oral therapies present drawbacks such as slow onset of action, low bioavailability and large inter-subject variability."( Fast relief from migraine attacks using fast-disintegrating sublingual zolmitriptan tablets.
Mahmoud, AA; Salah, S, 2012
)
0.38
"Tedizolid will provide a useful addition to the antimicrobial armamentarium, particularly in complicated skin and skin structure infections, due to its high oral bioavailability and once-daily dosing."( Tedizolid (TR-701): a new oxazolidinone with enhanced potency.
Corey, GR; Kanafani, ZA, 2012
)
0.38
" Parametric population pharmacokinetic analysis was used to evaluate bioavailability and the influence of total body weight (TBW) on pharmacokinetic parameters."( Oral bioavailability of linezolid before and after Roux-en-Y gastric bypass surgery: is dose modification necessary in obese subjects?
Ameri, D; Hamilton, R; Pai, MP; Thai, XC, 2013
)
0.39
"The bioavailability of linezolid is not impaired by RYGBS."( Oral bioavailability of linezolid before and after Roux-en-Y gastric bypass surgery: is dose modification necessary in obese subjects?
Ameri, D; Hamilton, R; Pai, MP; Thai, XC, 2013
)
0.39
"Linezolid may be an interesting alternative for prosthetic joint infection (PJI) due to its bioavailability and its antimicrobial spectrum."( Linezolid in late-chronic prosthetic joint infection caused by gram-positive bacteria.
Ariza, J; Cobo, J; del Toro, MD; Euba, G; Jover-Sáenz, A; Lora-Tamayo, J; Palomino, J; Riera, M; Rodríguez-Pardo, D, 2013
)
0.39
" This study was conducted to evaluate the pharmacokinetics (PKs) and relative bioavailability of suspension (reference) and tablet (test) formulations of Linezolid (LZD)."( Pharmacokinetics and relative bioavailability evaluation of linezolid suspension and tablet formulations.
Helmy, SA, 2013
)
0.39
" In order to further support the development of anacetrapib, we prepared [M + 6]MK-0859, which was required in support of an absolute bioavailability study of the active pharmaceutical ingredient (API)."( Synthesis of stable isotope labeled anacetrapib, its major metabolites and [(14) C]anacetrapib.
Kuethe, JT; Quinn, CA; Royster, P; Soli, ED, 2013
)
0.39
" Of primary importance when treating cSSTIs is the agent's clinical efficacy against the causative pathogens, as well as its bioavailability in the skin and associated structures."( European perspective and update on the management of complicated skin and soft tissue infections due to methicillin-resistant Staphylococcus aureus after more than 10 years of experience with linezolid.
Baguneid, M; Bassetti, M; Bouza, E; Dryden, M; Nathwani, D; Wilcox, M, 2014
)
0.4
" The high oral bioavailability of linezolid makes it an attractive oral alternative to glycopeptides and its use has increased in the last decade."( Clinical experience with linezolid for the treatment of orthopaedic implant infections.
García-Ramiro, S; Martínez-Pastor, JC; Mensa, J; Morata, L; Soriano, A; Tornero, E, 2014
)
0.4
"4% coefficient of variation), and absolute bioavailability was high (86%)."( Tedizolid population pharmacokinetics, exposure response, and target attainment.
Fiedler-Kelly, J; Flanagan, S; Lu, Q; Ludwig, E; Passarell, J; Prokocimer, P, 2014
)
0.4
" Intensive structure-activity relationship (SAR) and structure-pharmacokinetic relationship (SPR) studies on this new series led to the discovery of compound 11a: a highly potent, selective, direct, and orally bioavailable FXa inhibitor with excellent in vivo antithrombotic efficacy and preferable pharmacokinetic profiles."( Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.
Chen, X; Chu, W; Ding, S; Gong, G; Guo, B; Sun, P; Wang, H; Wang, Y; Xue, T; Yang, Y; Zhou, Y, 2014
)
0.4
" In this study, we formulate a Zolmitriptan (ZT) & ketorolac tromethamine (KT) loaded thermo reversible in-situ mucoadhesive intranasal gel (TMISG) formulation which gels at the nasal mucosal temperature and contains a bioadhesive polymer (Xyloglucan) that lengthens the residence time will enhance the bioavailability of the combinational drugs."( Optimization of combinational intranasal drug delivery system for the management of migraine by using statistical design.
Garg, T; Goyal, AK; Kumar, A; Rath, G; Sarma, GS, 2015
)
0.42
" The results revealed that the absolute bioavailability was about 63%."( Drug in Adhesive Patch of Zolmitriptan: Formulation and In vitro /In vivo Correlation.
Fang, L; Liu, C, 2015
)
0.42
" The compound also demonstrated high oral bioavailability (F = 99."( Discovery of a Teraryl Oxazolidinone Compound (S)-N-((3-(3-Fluoro-4-(4-(pyridin-2-yl)-1H-pyrazol-1-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)acetamide Phosphate as a Novel Antimicrobial Agent with Enhanced Safety Profile and Efficacies.
Ang, W; Chang, Y; Chen, G; Li, G; Liu, Y; Long, H; Luo, Y; Sang, Z; Tang, J; Wang, Z; Wei, Y; Yang, S; Yang, T; Yang, X; Zhang, J, 2015
)
0.42
" Oxazolidinones represent synthetic anti-bacterial agents with unique mechanism of action having wide spectrum of activity, oral bioavailability and well established SAR."( Oxazolidinones as Anti-tubercular Agents: Discovery, Development and Future Perspectives.
Chakraborti, AK; Dhameliya, TM; Jadhavar, PS; Vaja, MD, 2015
)
0.42
"Zolmitriptan is the drug of choice for migraine, but low oral bioavailability (<50%) and recurrence of migraine lead to frequent dosing and increase in associated side effects."( Poloxamer 407-based intranasal thermoreversible gel of zolmitriptan-loaded nanoethosomes: formulation, optimization, evaluation and permeation studies.
Dhamecha, D; Jalalpure, S; Shahi, S; Shelke, S, 2016
)
0.43
" The absolute bioavailability of zolmitriptan is about 40% for oral administration; due to hepatic first metabolism."( Trans-nasal zolmitriptan novasomes: in-vitro preparation, optimization and in-vivo evaluation of brain targeting efficiency.
Abd-Elal, RM; Bendas, ER; Rashed, HM; Shamma, RN, 2016
)
0.43
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" The addition of other orally bioavailable anti-staphylococcal agents to tedizolid may be unlikely to improve killing but further research is warranted to assess the impact of these combinations on resistance prevention, or against biofilm-embedded organisms."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" Oral MRX-I was associated with a greater bioavailability and exposure when administered with food, and minimal accumulation of MRX-I occurred after multiple-dose administration."( Single- and Multiple-Dose Study To Determine the Safety, Tolerability, Pharmacokinetics, and Food Effect of Oral MRX-I versus Linezolid in Healthy Adult Subjects.
Eckburg, PB; Ge, Y; Hafkin, B, 2017
)
0.46
" In vivo studies show that PZ-M possess prolonged blood circulation time and increased oral bioavailability compared with free PZ."( Improving the pharmacokinetics and tissue distribution of pyrinezolid by self-assembled polymeric micelles.
Deng, Y; Guo, G; He, G; Li, X; Li, Z; Long, H; Luo, Y; Mei, L; Sang, Z; Wang, Z; Yang, T; Zheng, Y; Zhou, L, 2017
)
0.46
"Zolmitriptan (ZT) is a well-tolerated drug in migraine treatment suffering from low bioavailability due to low amount of the drug that reaches the brain after oral and nasal delivery."( Brain targeting efficiency of antimigrain drug loaded mucoadhesive intranasal nanoemulsion.
Abdou, EM; Kandil, SM; Miniawy, HMFE, 2017
)
0.46
" Moreover, adding a substituent into the upper phenyl moiety further enhanced the intrinsic activity, which led to the discovery of 5-[(4S,5S)-5-(4fluorophenyl)-4-methyl-2-oxo-1,3-oxazolidin-3-yl]benzene-1,3-dicarbonitrile (4S,5S)-5n, endowed with excellent D5D binding affinity, cellular activity, and high oral bioavailability in a mouse."( Discovery of 3,5-Diphenyl-4-methyl-1,3-oxazolidin-2-ones as Novel, Potent, and Orally Available Δ-5 Desaturase (D5D) Inhibitors.
Andou, T; Fujimoto, J; Hara, R; Hayashi, R; Iida, K; Imanishi, M; Kawamoto, T; Kubo, K; Maekawa, T; Masada, S; Matsui, J; Matsunaga, N; Miyahisa, I; Nagase, H; Noguchi, N; Okamoto, R; Takagahara, S; Tamura, YO; Tohyama, K, 2017
)
0.72
" These antimicrobial agents exhibit a favourable pharmacokinetic profile with an excellent bioavailability and a good tissue and organ penetration."( Clinical Pharmacokinetics and Pharmacodynamics of Oxazolidinones.
Muller, L; Roberts, JA; Roger, C, 2018
)
0.48
"The aim was to prepare an optimized zolmitriptan (ZT)-loaded transfersome formulation using Box-Behnken design for improving the bioavailability by nasal route for quick relief of migraine and further to compare with a marketed nasal spray."( Development of zolmitriptan transfersomes by Box-Behnken design for nasal delivery: in vitro and in vivo evaluation.
Dudhipala, N; Narala, A; Pitta, SK; Veerabrahma, K, 2018
)
0.48
"9-mg zolmitriptan was delivered with high efficiency (85%) and high absolute bioavailability (77%)."( Pharmacokinetics and Skin Tolerability of Intracutaneous Zolmitriptan Delivery in Swine Using Adhesive Dermally Applied Microarray.
Ameri, M; Diep, AN; Hochart, G; Lewis, H; Nguyen, J; Queja, A, 2018
)
0.48
" Bioavailability studies performed in humans demonstrated that dissolution was the rate limiting step for bioavailability of the drug and one of the test products had significantly improved bioavailability compared to the marketed product Skelaxin®."( Development of a Clinically Relevant Dissolution Method for Metaxalone Immediate Release Formulations Based on an IVIVC Model.
Cetina-Čižmek, B; Filipović-Grčić, J; Khan, MZI; Radić, M; Špoljarić, D; Vuletić, L, 2018
)
0.48
"2% SLS (USP apparatus 2 at 50 rpm) is clinically relevant to predict bioavailability of the drug and is superior to the USP method in terms of the Quality by Design (QbD) concept."( Development of a Clinically Relevant Dissolution Method for Metaxalone Immediate Release Formulations Based on an IVIVC Model.
Cetina-Čižmek, B; Filipović-Grčić, J; Khan, MZI; Radić, M; Špoljarić, D; Vuletić, L, 2018
)
0.48
" However, there are limited published data on the impact of nanoparticle size on bioavailability in vivo and, to our knowledge, there have been no published examples looking at the impact of differential size of in situ-generated nanoparticles from an ASD."( Effect of Amorphous Nanoparticle Size on Bioavailability of Anacetrapib in Dogs.
Galipeau, K; Harmon, P; Kesisoglou, F; Okoh, G; Wang, M; Xu, W, 2019
)
0.51
"Despite the high bioavailability of oxazolidinones, we were not able to find evidence that its use was associated with a decrease of mortality or hospital length of stay (due to early discharge) of patients with skin and skin structure infections."( Evidence Associated with the Use of Oxazolidinones for the Treatment of Skin and Skin Structure Infections: A Retrospective Study.
Antão, HS; Froes, F; Gonçalves-Pereira, J; Guimarães, JP; Santos, FP, 2019
)
0.51
"Despite extensive research on small molecule thrombin inhibitors for oral application in the past decades, only a single double prodrug with very modest oral bioavailability has reached human therapy as a marketed drug."( Design, Synthesis, and Pharmacological Characterization of a Neutral, Non-Prodrug Thrombin Inhibitor with Good Oral Pharmacokinetics.
Allerheiligen, S; Gericke, KM; Gnoth, M; Heitmeier, S; Hillig, RC; Hillisch, A; Lienau, P; Puetter, V; Roehrig, S; Schaefer, M; Schulz, S; Tersteegen, A, 2020
)
0.56
" The validated method was successfully applied to pharmacokinetic and bioavailability studies of OTB-658 in cynomolgus monkeys and the absolute bioavailability of OTB-658 was 25."( Simultaneous determination of a novel oxazolidinone anti-tuberculosis OTB-658 and its metabolites in monkey blood by LC-MS/MS.
Huang, H; Jiang, J; Li, Y; Liu, X; Liu, Y; Sheng, L; Wang, B; Zhang, D, 2021
)
0.62
"Zolmitriptan is a widely used antimigraine drug, and its brain targeting by nasal route in the form of mucoadhesive nanoparticles is more effective in migraine treatment as it provides fast relief and good bioavailability as compared to its oral drug delivery."( Evaluation of Brain Targeting Potential of Zolmitriptan Mucoadhesive Nanoparticles for Intranasal Drug Delivery.
Jha, S; Mishra, D, 2022
)
0.72
" Oxazolidinone antibiotics such as linezolid have excellent oral bioavailability and provide coverage against MRSA infections."( The Novel Oxazolidinone TBI-223 Is Effective in Three Preclinical Mouse Models of Methicillin-Resistant Staphylococcus aureus Infection.
Archer, NK; Dikeman, DA; Fotouhi, N; Gordon, O; Gough, E; Kaushik, A; Miller, LS; Mumtaz, M; Nuermberger, EL; Orlando, N; Ortines, RV; Patel, AM; Upton, AM; Wang, Y; Youn, C; Zhang, J, 2022
)
0.72

Dosage Studied

ExcerptRelevanceReference
" Repeated dosing for 14 days did not enhance MAO-A inhibition."( SR 95191, a selective inhibitor of type A monoamine oxidase with dopaminergic properties. II. Biochemical characterization of monoamine oxidase inhibition.
Bizière, K; Kan, JP; Mouget-Goniot, C; Steinberg, R; Worms, P, 1987
)
0.27
"A single oral dosage of furaltadone and nitrofurazone (14."( Some pharmacokinetic data about furaltadone and nitrofurazone administered orally to preruminant calves.
Aerts, MM; Degen, M; Driessens, F; Nouws, JF; Vree, TB, 1987
)
0.27
"5 ng/ml of tyramine in 1 ml of human plasma and is thus suitable for monoamine oxidase inhibitor studies involving oral dosing with tyramine."( Measurement of tyramine in human plasma, utilising ion-pair extraction and high-performance liquid chromatography with amperometric detection.
Brown, MJ; Causon, RC, 1984
)
0.27
" Less than 2% of the parent drug was present in the urine of animals dosed either intravenously or intramammarily."( In vivo and in vitro pharmacokinetics and fate of furaltadone in meat- and milk-producing animals.
Bevill, RF; Ng, LL; Perkins, EG, 1984
)
0.27
" The adverse experience and efficacy profile appears to be consistent with previous 311C90 studies and this dosing regimen of 311C90 was well tolerated during multiple exposures."( Evaluation of the long-term safety and efficacy of 311C90 in the treatment of migraine.
Geraud, GE, 1996
)
0.29
" The dosing regimen was well tolerated during multiple exposures."( 311C90: long-term efficacy and tolerability profile for the acute treatment of migraine. International 311C90 Long-Term Study Group.
Zagami, AS, 1997
)
0.3
" After the last 10 mg dose, mean dosing interval zolmitriptan AUC was 80."( The pharmacokinetics and effects on blood pressure of multiple doses of the novel anti-migraine drug zolmitriptan (311C90) in healthy volunteers.
Dixon, R; Gibbens, M; Gillotin, C; Peck, RW; Posner, J, 1997
)
0.3
" faecalis sera from patients dosed with either drug were generally inhibitory at the peak timepoint, but at trough only linezolid exhibited a persistent effect."( Serum inhibitory titers and serum bactericidal titers for human subjects receiving multiple doses of the antibacterial oxazolidinones eperezolid and linezolid.
Batts, DH; Daley-Yates, PT; Pawsey, SD; Schaadt, RD; Stalker, DJ; Zurenko, GE, 1997
)
0.3
" Plasma concentrations are sustained for 4 to 6 h after dosing with single or multiple peaks in the plasma concentration-time profile, reflecting continued absorption down the gastrointestinal tract."( The clinical pharmacokinetics of zolmitriptan.
Dixon, R; Warrander, A, 1997
)
0.3
"5 mg dose was on the shoulder of the dose-response curve (2-h headache response rate 64%), showing similar efficacy to the 5 mg dose (67%)."( Zolmitriptan (Zomig, 311C90), a novel dual central and peripheral 5HT1B/1D agonist: an overview of efficacy.
Sawyer, J; Schoenen, J, 1997
)
0.3
" It is therefore unlikely that the pharmacokinetic changes will lead to clinically important changes in pharmacological effects and dosage adjustment of zolmitriptan is not required in patients taking propranolol for migraine prophylaxis."( The interaction between propranolol and the novel antimigraine agent zolmitriptan (311C90).
Dixon, R; Gillotin, CG; Layton, G; Peck, RW; Posner, J; Seaber, EJ; Weatherley, BC, 1997
)
0.3
" In young subjects, concentrations were higher in women than in men, but the differences were insufficient to justify dosage adjustment."( The pharmacodynamics and pharmacokinetics of the 5HT1B/1D-agonist zolmitriptan in healthy young and elderly men and women.
Dixon, RM; Jackson, SH; Layton, GR; Peck, RW; Posner, J; Rolan, PE; Seaber, EJ; Weatherley, BC, 1998
)
0.3
" Patients with moderate hepatic impairment require no dosage adjustment, but the recommended daily intake of zolmitriptan may need to be reduced in patients with severe hepatic impairment."( Effect of hepatic impairment on the pharmacokinetics of zolmitriptan.
Delvaux, M; Dixon, R; French, S; Kemp, J; Leclerc, V; Rautureau, J; Sellers, M, 1998
)
0.3
" A dose-response study was performed with PNU-100480 and linezolid (both at 25, 50, and 100 mg/kg of body weight)."( Activities of several novel oxazolidinones against Mycobacterium tuberculosis in a murine model.
Chase, S; Cynamon, MH; Klemens, SP; Sharpe, CA, 1999
)
0.3
" At a dosage of 100 mg/kg/day, linezolid treatment led to an approximately 100-fold reduction in viable cells per gram of abscess."( Activities of the oxazolidinones linezolid and eperezolid in experimental intra-abdominal abscess due to Enterococcus faecalis or vancomycin-resistant Enterococcus faecium.
Eliopoulos, GM; Moellering, RC; Schülin, T; Thauvin-Eliopoulos, C, 1999
)
0.3
" Headache response rates and pain-free response rates were assessed within two hours of dosing with zolmitriptan, and response rates were compared across migraines with and without a history of aura, and associated or not with menses."( Zolmitriptan provides consistent migraine relief when used in the long-term.
Edvinsson, L; Geraud, G; Korczyn, A; Mauskop, A; Pfaffenrath, V; Tuchman, M, 1999
)
0.3
" 1 mirogram/ml at 16 to 17 h after orogastric dosing at 25 mg/kg."( Efficacy of linezolid in experimental otitis media.
Albut, R; Figueira, M; Pelton, SI; Stalker, D, 2000
)
0.31
" Unpublished clinical data, adverse effects, and dosing information were abstracted from product labeling."( Linezolid for the treatment of resistant gram-positive cocci.
Bain, KT; Wittbrodt, ET, 2001
)
0.31
" Results of PAE testing support twice-daily dosing of linezolid in humans."( Post-antibiotic growth suppression of linezolid against Gram-positive bacteria.
Giles, C; Munckhof, WJ; Turnidge, JD, 2001
)
0.31
" Two weeks treatment of E2011 alone at an oral dosage of 150 mg/kg induced hepatocellular changes characterized by nuclear enlargement."( Protection from drug-induced hepatocellular changes by pretreatment with conjugating enzyme inhibitors in rats.
Aoki, T; Hosokawa, S; Sagami, F; Sato, G; Tsukidate, K, 2001
)
0.31
") dosed linezolid and intravenously (i."( Efficacy of linezolid in treatment of experimental endocarditis caused by methicillin-resistant Staphylococcus aureus.
Batts, DH; Buchanan, LV; Dailey, CF; Dileto-Fang, CL; Ford, CW; Gibson, JK; Oramas-Shirey, MP, 2001
)
0.31
" We demonstrated equivalence of intravenous and oral dosing in this patient, suggesting that oral linezolid may be an excellent alternative to intravenous vancomycin for CF patients infected with MRSA."( Successful treatment of methicillin-resistant Staphylococcus aureus pulmonary infection with linezolid in a patient with cystic fibrosis.
Blumberg, EA; Ferrin, M; Meagher, A; Zuckerman, JB, 2002
)
0.31
" Blood and urine samples were collected until 48 h after dosing and assayed for linezolid concentrations using a validated high-performance liquid chromatography method."( Age and sex effects on the pharmacokinetics of linezolid.
Hopkins, NK; Jungbluth, GL; Sisson, TL, 2002
)
0.31
"9, respectively, and the percentage of time the drug remained above the MIC for the 12-h dosing interval was 100%; the corresponding ratios in ELF were 120 and 16."( Intrapulmonary pharmacokinetics of linezolid.
Conte, JE; Golden, JA; Kipps, J; Zurlinden, E, 2002
)
0.31
" Dosage reductions are not necessary, even in severe renal impairment, but about one third of the dose is eliminated during dialysis."( [New treatment option for gram-positive infections in critically ill patients - overview over linezolid].
Krueger, WA; Unertl, KE, 2002
)
0.31
"This phase II study investigated the efficacy, tolerability and dose-response relationship of oral zolmitriptan in the treatment of a single migraine attack in Japanese patients."( Zolmitriptan is effective and well tolerated in Japanese patients with migraine: a dose-response study.
Fukuuchi, Y; Itoyama, Y; Iwata, M; Morimatsu, M; Nakashima, K; Sakai, F; Sobue, G; Tashiro, K; Tsuji, S, 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
" Results are in agreement with the assumption of a limited accumulation of linezolid under the dosage regimen given."( Single- and multiple-dose pharmacokinetics of linezolid and co-amoxiclav in healthy human volunteers.
Borner, K; Burkhardt, O; Köppe, P; Lode, H; Nord, CE; Pletz, MW; von der Höh, N, 2002
)
0.31
" A rabbit endocarditis model was used to compare the in vivo activities of different linezolid regimens mimicking intermittent dosing of 10 mg/kg of body weight every 12 h for 5 days or continuous (constant-rate) infusion of a daily dose of 20 mg/kg (for 5 days) or 40 mg/kg (for 3 and 5 days) and the activities of intermittent dosing and continuous infusion of vancomycin (for 5 days)."( In vivo efficacy of continuous infusion versus intermittent dosing of linezolid compared to vancomycin in a methicillin-resistant Staphylococcus aureus rabbit endocarditis model.
Batard, E; Boutoille, D; Bugnon, D; Caillon, J; Hamel, A; Jacqueline, C; Kergueris, MF; Perez, L; Potel, G, 2002
)
0.31
" Oral bioavailability in humans was determined to be 100% and twice daily dosing in humans resulted in blood levels which even at trough values were in excess of the MIC90 for significant Gram-positive pathogens."( The discovery of linezolid, the first oxazolidinone antibacterial agent.
Barbachyn, MR; Ford, CW; Zurenko, GE, 2001
)
0.31
"Patients received linezolid in a dosage of 600 mg intravenously (iv) and/or orally twice daily."( The efficacy and safety of linezolid as treatment for Staphylococcus aureus infections in compassionate use patients who are intolerant of, or who have failed to respond to, vancomycin.
Birmingham, MC; Forrest, A; Moise, PA; Schentag, JJ, 2002
)
0.31
" Drug concentration and half-life were adjusted to simulate clinical dosing (600 mg twice daily) of linezolid."( Comparison of linezolid activities under aerobic and anaerobic conditions against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecium.
Gunderson, BW; Hovde, LB; Ibrahim, KH; Peloquin, CA; Rotschafer, JC, 2003
)
0.32
" Virtually complete oral bioavailability allows for 1:1 conversion between the intravenous and oral dosage forms."( Linezolid: an oxazolidinone antimicrobial agent.
Paladino, JA, 2002
)
0.31
" Its elimination half-life allows dosing twice per day, and alteration of drug dosage is not required in patients with impaired renal or hepatic function."( Linezolid: the first oxazolidinone antimicrobial.
Moellering, RC, 2003
)
0.32
" The potential for alternative day or thrice weekly dosing with teicoplanin may offer further cost advantages whilst maintaining equivalent clinical effectiveness."( Cost-minimization analysis and audit of antibiotic management of bone and joint infections with ambulatory teicoplanin, in-patient care or outpatient oral linezolid therapy.
Ajdukiewicz, K; Barlow, GD; Clift, B; Davey, P; France, AJ; Gray, K; Morrison, J; Nathwani, D, 2003
)
0.32
"0 mg/L) for the majority of the 12 h dosing interval."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.32
"Oral and intravenous linezolid exhibit linear pharmacokinetics, with concentrations remaining above the target MIC90 for most of the dosing interval."( Pharmacokinetics and tolerance of single- and multiple-dose oral or intravenous linezolid, an oxazolidinone antibiotic, in healthy volunteers.
Batts, DH; Hopkins, NK; Jungbluth, GL; Stalker, DJ, 2003
)
0.32
" Terminal phase tissue residue and excretion data were compared to data from rats dosed orally with [(14)C]sodium acetate."( Assessment of radioactive residues arising from radiolabel instability in a multiple dose tissue distribution study in rats.
Chiba, K; Courtney, M; Easter, JA; Fate, GD; Johnson, MG; Jones, BW; Koets, MD; Norris, LR; Sams, JP; Slatter, JG, 2003
)
0.32
"Ten adult patients undergoing bronchoscopy for diagnostic purposes were given oral linezolid at a dosage of 600 mg twice a day for a total of six doses."( Intrapulmonary penetration of linezolid.
Andrews, J; Honeybourne, D; Jevons, G; Tobin, C; Wise, R, 2003
)
0.32
" teicoplanin) dosed per approved prescription information."( Hospital resource use and cost of treatment with linezolid versus teicoplanin for treatment of serious gram-positive bacterial infections among hospitalized patients from South America and Mexico: results from a multicenter trial.
Balan, DA; Li, JZ; López, H; Mozaffari, E; Rittenhouse, BE; Tang, T; Vidal, G; Willke, RJ; Zitto, T, 2003
)
0.32
" We conclude that no adjustment of the linezolid dosage is needed in subjects with renal dysfunction or subjects on hemodialysis."( Pharmacokinetics of linezolid in subjects with renal dysfunction.
Aronoff, GR; Batts, DH; Brier, ME; Hopkins, NK; Jungbluth, GL; O'Grady, M; Ryan, KK; Stalker, DJ, 2003
)
0.32
" Therefore it is important to determine the specific pharmacokinetic characteristics for individual drugs in pediatric patients so that appropriate age-specific dosage regimens can be developed and evaluated in clinical trials."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
0.32
"Because of the higher clearance and lower area under the drug concentration-time curve, a shorter dosing interval for linezolid is required for children younger than 12 years of age to produce adequate drug exposure against target Gram-positive pathogens."( Linezolid pharmacokinetics in pediatric patients: an overview.
Hopkins, NK; Jungbluth, GL; Welshman, IR, 2003
)
0.32
" Dosing frequency (two to three times daily) varied depending on age and clinical diagnosis."( Safety and tolerability of linezolid in children.
Bruss, JB; Edge-Padbury, B; Goldfarb, J; Kaplan, SA; Naberhuis-Stehouwer, S; Saiman, L; Wible, K, 2003
)
0.32
" The nonlinearity is not relevant over the therapeutic dosage range."( Clinical pharmacokinetics of linezolid, a novel oxazolidinone antibacterial.
Jungbluth, GL; Stalker, DJ, 2003
)
0.32
" Evaluation of the pharmacokinetic data would appear to support the use of linezolid dosing regimens currently approved for infants and young children in neonates with postnatal age greater than 7 days."( Impact of ontogeny on linezolid disposition in neonates and infants.
Abdel-Rahman, SM; Bruss, JB; Grzebyk, RP; Hopkins, NK; Jungbluth, GL; Kearns, GL; Van Den Anker, JN; Welshman, IR, 2003
)
0.32
" Chance of success in bacteraemia, LRTI and SSSI also appear to be higher when concentrations remain above the MIC for the entire dosing interval."( Clinical pharmacodynamics of linezolid in seriously ill patients treated in a compassionate use programme.
Birmingham, MC; Forrest, A; Meagher, AK; Rayner, CR; Schentag, JJ, 2003
)
0.32
"A simple, selective, precise, and stability-indicating high-performance thin layer chromatographic method of analysis of Linezolid both as a bulk drug and in formulations was developed and validated in pharmaceutical dosage form."( Stability indicating HPTLC determination of linezolid as bulk drug and in pharmaceutical dosage form.
Agrawal, H; Kaul, N; Mahadik, KR; Paradkar, AR, 2003
)
0.32
"The pharmacokinetics of many drugs are altered in patients with cystic fibrosis (CF), often necessitating different dosage requirements than those used in non-CF patients."( Linezolid pharmacokinetics in adult patients with cystic fibrosis.
Bosso, JA; Flume, PA; Gray, SL, 2004
)
0.32
"An in vitro pharmacodynamic model was used to simulate standard dosing regimens of linezolid, levofloxacin, and vancomycin against the isolates 79, R921, and P9802-020."( Linezolid, levofloxacin, and vancomycin against vancomycin-tolerant and fluoroquinolone-resistant Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Akins, RL; Cha, R; Rybak, MJ, 2003
)
0.32
" The appearance of increasing antimicrobial resistance can challenge the efficacy of these drugs when concentrations do not exceed the MIC for 40% to 50% of the dosing interval."( Basic pharmacodynamics of antibacterials with clinical applications to the use of beta-lactams, glycopeptides, and linezolid.
Craig, WA, 2003
)
0.32
" Mean levels exceed the required MIC for the treatment of MRSA for >80% of the dosing period for serum and the majority of the dosing period for sputum."( Serum and sputum concentrations following the oral administration of linezolid in adult patients with cystic fibrosis.
Conway, S; Denton, M; Etherington, C; Hulme, B; Peckham, DG; Saralaya, D; Tobin, CM, 2004
)
0.32
" AZD2563 is a novel oxazolidinone that has activity similar to linezolid and the potential for extended dosing intervals."( Preliminary susceptibility testing guidelines for AZD2563, a long-acting oxazolidinone.
Anderegg, TR; Jones, RN, 2004
)
0.32
"At the conclusion of this learning activity, participants should be familiar with the modes of action, clinical indications, dosage regimens, and contraindications and cautions for several novel antibacterial agents for skin and skin structure infections."( Novel antibacterial agents for skin and skin structure infections.
Schweiger, ES; Weinberg, JM, 2004
)
0.32
" This suggests that Skelaxin Tablets should be considered a delayed release dosage form."( Comparison of the dissolution of metaxalone tablets (Skelaxin) using USP Apparatus 2 and 3.
Amann, A; Cacace, J; Reilly, EE, 2004
)
0.32
" The findings of these studies collectively suggest that once-daily dosing of telavancin may provide an effective approach for the treatment of clinically relevant infections with gram-positive organisms."( Pharmacodynamics of telavancin (TD-6424), a novel bactericidal agent, against gram-positive bacteria.
Hegde, SS; Judice, JK; Kaniga, K; McCullough, J; Obedencio, G; Pace, J; Reyes, N; Shaw, JP; Skinner, R; Thomas, R; Vanasse, N; Wiens, T, 2004
)
0.32
" It is not known whether dosage adjustments are necessary in patients treated with continuous renal replacement therapies."( Elimination of linezolid by an in vitro extracorporeal circuit model.
Hansen, M; Hoffmann, E; Krueger, WA; Schroeder, TH; Stephan, M; Unertl, K, 2004
)
0.32
" It exhibits good penetration into pulmonary, as well as skin and related structure tissues, and does not require dosage adjustment in hepatic or renal dysfunction."( A review of linezolid: the first oxazolidinone antibiotic.
Dotter, B; Madaras-Kelly, K; Stevens, DL, 2004
)
0.32
" Human therapeutic dosing regimens for nafcillin, daptomycin, vancomycin, linezolid, and gentamicin were simulated."( Impact of high-inoculum Staphylococcus aureus on the activities of nafcillin, vancomycin, linezolid, and daptomycin, alone and in combination with gentamicin, in an in vitro pharmacodynamic model.
LaPlante, KL; Rybak, MJ, 2004
)
0.32
" Serum levels exceeded the breakpoint of 4 mg/L for the entire dosing interval in all subjects (400 mg dose every 12 h) with an AUC/MIC of 399."( Pharmacokinetic studies of linezolid and teicoplanin in the critically ill.
Aarons, L; Cepeda, JA; Kibbler, C; MacGowan, A; Nalda-Molina, R; Shaw, S; Shulman, R; Singer, M; Tobin, C; Whitehouse, T; Wilson, AP, 2005
)
0.33
"Linezolid dosage at 600 mg every 12 h was adequate in the critically ill without need for adjustment for renal function."( Pharmacokinetic studies of linezolid and teicoplanin in the critically ill.
Aarons, L; Cepeda, JA; Kibbler, C; MacGowan, A; Nalda-Molina, R; Shaw, S; Shulman, R; Singer, M; Tobin, C; Whitehouse, T; Wilson, AP, 2005
)
0.33
"Single-lumen central venous catheters colonized with biofilm-embedded Staphylococcus aureus, Staphylococcus epidermidis or vancomycin-resistant Enterococcus faecium (VRE) were treated with simulated clinical dosing regimens of linezolid 600 mg every 12 h or vancomycin 1 g every 12 h in a one-compartment in vitro pharmacodynamic model."( Antibacterial activity of linezolid and vancomycin in an in vitro pharmacodynamic model of gram-positive catheter-related bacteraemia.
Coyle, EA; Lewis, RE; Prince, RA; Raad, II; Wiederhold, NP, 2005
)
0.33
" The venlafaxine dosage was decreased to 150 mg/day, and symptoms gradually abated over 36 hours."( Serotonin toxicity associated with concomitant use of linezolid.
Bergeron, L; Boulé, M; Perreault, S, 2005
)
0.33
"Clinicians should pay special attention to patients treated with serotonergic drugs, especially those receiving dosages in the higher end of the normal range who are prescribed linezolid, and consider tapering or reducing the dosage of serotonergic drugs for the duration of antibiotic therapy."( Serotonin toxicity associated with concomitant use of linezolid.
Bergeron, L; Boulé, M; Perreault, S, 2005
)
0.33
" The aim of this prospective, single-centre, open-label, two-arm study was to investigate the pharmacokinetics of linezolid during continuous venovenous haemofiltration (CVVH) in critically ill patients and to derive a dosage recommendation."( Multiple-dose pharmacokinetics of linezolid during continuous venovenous haemofiltration.
Heinz, G; Jaeger, W; Karth, GD; Kornek, GV; Locker, GJ; Meyer, B; Nikfardjam, M; Thalhammer, F, 2005
)
0.33
" These data suggest that a schedule of 600 mg linezolid at least twice daily may also be an appropriate dosing for patients with severe Gram-positive infections undergoing CVVH with both types of membranes."( Multiple-dose pharmacokinetics of linezolid during continuous venovenous haemofiltration.
Heinz, G; Jaeger, W; Karth, GD; Kornek, GV; Locker, GJ; Meyer, B; Nikfardjam, M; Thalhammer, F, 2005
)
0.33
" This suggests that a dosage of 600 mg administered intravenously twice daily to critically ill patients with Gram-positive ventilator-associated pneumonia would achieve success against organisms with minimum inhibitory concentrations as high as 2-4 mg/L in both plasma and epithelial lining fluid."( Pharmacokinetics and intrapulmonary concentrations of linezolid administered to critically ill patients with ventilator-associated pneumonia.
Allaouchiche, B; Boselli, E; Breilh, D; Chassard, D; Djabarouti, S; Rimmelé, T; Saux, MC; Toutain, J, 2005
)
0.33
" Because the vitreous concentrations appeared to exponentially trend upward with time and 33% of the late group achieved sufficient MIC90 levels for the common pathogens found in postoperative endophthalmitis, adequate concentrations might be achieved with an altered dosing regimen to achieve higher serum steady state levels."( Human vitreous distribution of linezolid after a single oral dose.
Ciulla, TA; Comer, GM; Peloquin, C; Wheeler, J,
)
0.13
" The oral bioavailability of linezolid is approximately 100%, thus allowing sequential intravenous-to-oral administration without changing the drug or dosage regimen."( Linezolid: a pharmacoeconomic review of its use in serious Gram-positive infections.
Figgitt, DP; Plosker, GL, 2005
)
0.33
"v) and oral dosing and to compare the pharmacokinetics with those obtained following linezolid dosing."( Assessment of oral bioavailability and preclinical pharmacokinetics of DRF-6196, a novel oxazolidinone analogue, in comparison to linezolid.
Bhamidipati, R; Das, J; Dravid, PV; Mullangi, R; Narasimhulu, PC; Srinivas, NR; Tvrs, S; Venkatesh, P,
)
0.13
" The objective of phase two was to investigate patients' dosing patterns, satisfaction and preference following open-label treatment with the nasal spray."( Treatment satisfaction with zolmitriptan nasal spray for migraine in a real life setting: results from phase two of the REALIZE study.
Aschoff, J; Charlesworth, BR; Gawel, M; May, A, 2005
)
0.33
" Treatment with linezolid at a dosage of 10 mg/kg every 8 h intravenously for a duration of 16 days and 14 days, respectively, was well tolerated and led to complete clinical recovery and clearance of the organism from all body sites."( Linezolid treatment of glycopeptide-resistant Enterococcus faecium in very low birth weight premature neonates.
Bauer, K; Groll, AH; Hoehn, R; Schaefer, V; Schloesser, RL, 2006
)
0.33
" This may be due to the poor penetration of vancomycin into the lung, and alternate dosing regimens to increase tissue levels need to be further studied."( Methicillin-Resistant S. aureus Ventilator-Associated Pneumonia: Strategies to Prevent and Treat.
Lam, AP; Wunderink, RG, 2006
)
0.33
" Our findings emphasise the importance of optimal dosage of linezolid to prevent the emergence of resistance."( Emergence of linezolid-resistant Staphylococcus aureus during treatment of pulmonary infection in a patient with cystic fibrosis.
Andrade, SS; Barth, AL; Gales, AC; Lutz, L; Machado, A; Sader, HS, 2006
)
0.33
" Recurrence rates 2-24 h after dosing were 32."( Efficacy and tolerability of almotriptan versus zolmitriptan for the acute treatment of menstrual migraine.
Acuto, G; Allais, G; Benedetto, C; Bussone, G; Cabarrocas, X; Esbri, R, 2006
)
0.33
" It does not appear that supplemental dosing of linezolid is necessary in patients undergoing CVVHDF."( Clearance of linezolid via continuous venovenous hemodiafiltration.
Assaly, R; Malhotra, D; Mauro, LS; Peloquin, CA; Schmude, K, 2006
)
0.33
" Based on the model-predicted unbound concentrations in ISF, a scheme of more-frequent daily dosing of linezolid for some critically ill patients might be taken into consideration to avoid subinhibitory unbound concentrations in the infected tissue."( Pharmacokinetics of unbound linezolid in plasma and tissue interstitium of critically ill patients after multiple dosing using microdialysis.
Buerger, C; Dehghanyar, P; Joukhadar, C; Kloft, C; Plock, N, 2006
)
0.33
"Although daily-half doses of linezolid were effective in patients with intractable or extensive MDR-TB, this dosage regimen did not reduce long-term use-related side effects, such as peripheral and optic neuropathy."( Efficacy and tolerability of daily-half dose linezolid in patients with intractable multidrug-resistant tuberculosis.
Hong, SB; Kim, DS; Kim, MN; Kim, WD; Kim, WS; Koh, Y; Lee, SD; Lim, CM; Oh, YM; Park, IN; Shim, TS, 2006
)
0.33
" The serum and CSF linezolid concentrations exceeded the pharmacodynamic breakpoint of 4 microg/ml for susceptible target pathogens for the entire dosing interval in the majority of patients."( Serum and cerebrospinal fluid concentrations of linezolid in neurosurgical patients.
Anagnostaki, M; Baltopoulos, G; Boutzouka, E; Markantonis, SL; Myrianthefs, P; Panidis, D; Vlachos, K, 2006
)
0.33
" Urine samples were taken every 2 h during the whole dosing interval of the particular antibiotic."( Urinary bactericidal activity of oral antibiotics against common urinary tract pathogens in an ex vivo model.
Bedenic, B; Bubonja, M; Budimir, A; Topic, M, 2006
)
0.33
" Once-a-week dosing with dalbavancin may obviate the need for the continued presence of IV lines in some patients, which could translate into fewer local infections and blood stream infections and which could facilitate transfer of the patients to skilled nursing facilities."( Dalbavancin: a review for dermatologists.
Scheinfeld, N, 2006
)
0.33
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Linezolid, active against methicillin-resistant strains and available in oral and intravenous dosage forms, is a potential alternative to vancomycin for the treatment of PJIs."( Linezolid versus vancomycin for prosthetic joint infections: a cost analysis.
Cheung, KW; Hui, M; Lee, GC; So, RK; You, JH, 2007
)
0.34
" aregenerative anemia, neutropenia and thrombopenia, developed 3 weeks and 5 weeks after initiating linezolid therapy at a conventional dosage (600 mg bid)."( Linezolid-related pancytopenia in organ-transplant patients: report of two cases.
Faguer, S; Fillola, G; Guitard, J; Kamar, N; Rostaing, L, 2007
)
0.34
" Furthermore, bactericidal activity (titres > or = 1:2) was observed for at least 6 h (50% of the dosing interval) against four of these five strains."( Linezolid tissue penetration and serum activity against strains of methicillin-resistant Staphylococcus aureus with reduced vancomycin susceptibility in diabetic patients with foot infections.
Havlichek, DH; Missavage, A; Peloquin, CA; Schooley, S; Stein, GE, 2007
)
0.34
" The proposed methods have been applied successfully for the analysis of the drug in its dosage forms."( Extractive spectrophotometric methods for determination of zolmitriptan in tablets.
Aydogmus, Z; Inanli, I,
)
0.13
" The patient did not respond to 5 days of appropriately dosed linezolid and daptomycin and remained bacteremic because abscess drainage was not an option in this case and the continuous, high-grade MRSA bacteremia continued despite appropriate therapy."( Methicillin-resistant Staphylococcus aureus (MRSA) mitral valve acute bacterial endocarditis (ABE) in a patient with Job's syndrome (hyperimmunoglobulin E syndrome) successfully treated with linezolid and high-dose daptomycin.
Cunha, BA; Kodali, V; Krol, V,
)
0.13
" In response, some clinicians increased vancomycin dosing to >or=4 g/day."( Larger vancomycin doses (at least four grams per day) are associated with an increased incidence of nephrotoxicity.
Drusano, GL; Graves, J; Lodise, TP; Lomaestro, B, 2008
)
0.35
" Therefore, a correct dosing regimen for the time-dependent molecules (i."( [Pharmacological rationale for choice of antibiotics for intraabdominal infections].
Mazzei, T; Novelli, A, 2008
)
0.35
" The lower dosage for the pharmacodynamically optimized regimen may decrease drug toxicity."( Use of an in vitro pharmacodynamic model to derive a linezolid regimen that optimizes bacterial kill and prevents emergence of resistance in Bacillus anthracis.
Brown, DL; Drusano, GL; Heine, HS; Kim, K; Kinzig-Schippers, M; Liu, W; Louie, A; Sörgel, F; VanScoy, B, 2008
)
0.35
" However, in the current study we show LZD accumulation occurring with repeated dosing during hemodialysis in a 64-year-old man receiving hemodialysis treatment."( Pharmacokinetics of repeated dosing of linezolid in a hemodialysis patient with chronic renal failure.
Hayashi, W; Hiraki, Y; Kamimura, H; Kamohara, R; Karube, Y; Mizoguchi, A; Tsuji, Y, 2008
)
0.35
" Extrapolation of these results to humans suggests the feasibility of delivering therapeutic amounts of zolmitriptan at faster rates than those from existing dosage forms."( Controlled non-invasive transdermal iontophoretic delivery of zolmitriptan hydrochloride in vitro and in vivo.
Kalia, YN; Patel, SR; Sharma, A; Zhong, H, 2009
)
0.35
" However, our drug level results suggest that further investigation is needed to determine the optimal dosing of linezolid in treatment of central nervous system infection in pediatric patients."( Successful treatment of vancomycin-resistant enterococcal ventriculitis in a pediatric patient with linezolid.
Maranich, AM; Rajnik, M, 2008
)
0.35
" aureus strains was studied by in vitro simulation of 5-day antibiotic dosing over a wide range of AUC(24)/MIC ratios."( Linezolid pharmacodynamics with Staphylococcus aureus in an in vitro dynamic model.
Firsov, AA; Lubenko, IY; Portnoy, YA; Smirnova, MV; Strukova, EN; Vostrov, SN; Zinner, SH, 2009
)
0.35
" Linezolid was administered intravenously at a dosage of 10 mg/kg every 8 h and then orally."( Pharmacokinetics and tolerance of linezolid for meticillin-resistant Staphylococcus aureus mediastinitis in paediatric patients.
Fujita, N; Hamaoka, K; Kato, R; Kokufu, T; Kosaka, T; Shime, N; Sugioka, N, 2009
)
0.35
"Linezolid clearance is enhanced in children with CF requiring a higher dosage regimen."( Pharmacokinetics and pharmacodynamics of linezolid in children with cystic fibrosis.
Ahmad, N; Brown, ME; Jafri, HS; McCracken, GH; Murphey, DK; Prestidge, CB; Salvatore, CM; Sanchez, PJ; Santos, RP; Siegel, JD; Urbancyzk, B, 2009
)
0.35
" These changes are of sufficient magnitude that linezolid concentrations may be sub-therapeutic in some patients and we suggest that the dosage interval may need to be decreased in this patient population."( Pharmacokinetic evaluation of linezolid in patients with major thermal injuries.
Birraux, G; Bret, P; Hovsepian, L; Le Floch, R; Lovering, AM; Stephanazzi, J; Vinsonneau, C, 2009
)
0.35
"48, %T(MSW) (% of the dosing interval that concentrations fall in the MSW)=40%] and ATCC 51299 and GP32 (AUC/MIC=30."( In vitro analysis of resistance selection by linezolid in vancomycin-susceptible and -resistant Enterococcus faecalis and Enterococcus faecium.
Allen, GP; Bierman, BC, 2009
)
0.35
" We conclude that pharmacokinetics of linezolid are altered in burn patients, in a magnitude sufficient that linezolid concentration may be subtherapeutic in some patients and we suggest that the dosage interval may need to be decreased in this patient population."( [Pharmacokinetic evaluation of linezolid in patients with major thermal injuries].
Arnould, JF; Birraux, G; Bret, P; Hovsepian, L; Le Floch, R; Lovering, AM; Stephanazzi, J; Vinsonneau, C, 2010
)
0.36
" The dosage of linezolid was 600 mg daily."( Linezolid in the treatment of multidrug-resistant tuberculosis.
Flood, J; Mase, S; Raftery, A; Schecter, GF; Scott, C; True, L, 2010
)
0.36
" This study was limited due to an inability to assess for the effects of hetero-resistance and appropriate vancomycin dosing on outcomes."( Efficacy and safety of linezolid in methicillin-resistant Staphylococcus aureus (MRSA) complicated skin and soft tissue infection (cSSTI): a meta-analysis.
Bounthavong, M; Hsu, DI, 2010
)
0.36
" The best method of managing linezolid dosage in such a complex group of patients, whose physiology can vary daily, would be to use therapeutic drug monitoring."( Pharmacokinetics of linezolid in septic patients with and without extended dialysis.
Haefeli, WE; Hempel, G; Hoppe-Tichy, T; Lichtenstern, C; Ober, MC; Saleh, S; Schwenger, V; Sonntag, HG; Swoboda, S; Weigand, MA, 2010
)
0.36
" Overall, it appears that anacetrapib exhibits a low-to-moderate degree of absorption after oral dosing and majority of the absorbed dose is eliminated via oxidation to a series of hydroxylated metabolites that undergo conjugation with glucuronic acid before excretion into bile."( Pharmacokinetics, metabolism, and excretion of anacetrapib, a novel inhibitor of the cholesteryl ester transfer protein, in rats and rhesus monkeys.
Bradley, S; Braun, MP; Chen, Q; Dean, DC; Doss, G; Hartmann, G; Ho, JZ; Kumar, S; Pereira, A; Tan, EY; Tang, W; Zhang, AS, 2010
)
0.36
"95 but appeared not clinically relevant because it did not result in different dosing advice."( Limited sampling strategies for therapeutic drug monitoring of linezolid in patients with multidrug-resistant tuberculosis.
Alffenaar, JW; Kosterink, JG; Proost, JH; Uges, DR; van Altena, R; van der Werf, TS, 2010
)
0.36
" Recently, the therapeutic efficacy of vancomycin in the treatment of hospitalized patients with MRSA infections has been questioned due to the emergence of MRSA strains with reduced susceptibility to vancomycin together with concerns related to inadequate dosing and poor tissue penetration of the drug."( The importance of tissue penetration in achieving successful antimicrobial treatment of nosocomial pneumonia and complicated skin and soft-tissue infections caused by methicillin-resistant Staphylococcus aureus: vancomycin and linezolid.
Stein, GE; Wells, EM, 2010
)
0.36
" Linezolid demonstrates adequate penetration into lung and other soft issues with sustained concentrations above the minimum inhibitory concentrations for susceptible pathogens, including MRSA, for the majority of the dosing interval."( The importance of tissue penetration in achieving successful antimicrobial treatment of nosocomial pneumonia and complicated skin and soft-tissue infections caused by methicillin-resistant Staphylococcus aureus: vancomycin and linezolid.
Stein, GE; Wells, EM, 2010
)
0.36
" As a consequence, studies have recommended higher doses or more frequent dosing or both for some antibiotics in patients with major burns, but data are lacking for many of the antibiotics reserved for treatment of life-threatening infections."( Potential subtherapeutic linezolid and meropenem antibiotic concentrations in a patient with severe burns and sepsis.
Allen, JM; Davies, JG; Dheansa, BS; Donaldson, PM; Hallam, MJ; Hanlon, GW; James, SE,
)
0.13
" Due to its bacteriostatic property, the cumulative percentages of the dosing interval during which the drug concentration exceeded the MIC (T > MIC), 66."( Activity of linezolid in an in vitro pharmacokinetic-pharmacodynamic model using different dosages and Staphylococcus aureus and Enterococcus faecalis strains with and without a hypermutator phenotype.
Arpin, C; Ba, BB; Bikie Bi Nso, B; Dubois, V; Quentin, C; Saux, MC, 2010
)
0.36
" In Group 2, eyes were dosed in accordance with a keratitis protocol (1 drop of 2 mg/mL every 15 minutes for 1 hour)."( Ocular penetration of topically applied linezolid in a rabbit model.
Bourcier, T; Dory, A; Gaucher, D; Jehl, F; Lefevre, S; Prevost, G; Saleh, M; Sauer, A; Speeg-Schatz, C, 2010
)
0.36
" When coadministered with rifampin, area under the plasma concentration-time curve over the dosing interval and maximum concentration values for linezolid were reduced approximately 32% and 21%, respectively."( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism.
Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011
)
0.37
"8 g/kg in a within-subject, counterbalanced dosing design."( Zolmitriptan and human aggression: interaction with alcohol.
Gowin, JL; Lane, SD; Moeller, FG; Swann, AC, 2010
)
0.36
"A 5-mg dose of zolmitriptan effectively reduced alcohol-related aggression in an acute dosing protocol, demonstrating an interaction of 5-HT and alcohol in human aggressive behavior."( Zolmitriptan and human aggression: interaction with alcohol.
Gowin, JL; Lane, SD; Moeller, FG; Swann, AC, 2010
)
0.36
" No electroactive interferences from the excipients and endegenous substances were found in the pharmaceutical dosage form and the biological sample, respectively."( Anodic voltammetry of zolmitriptan at boron-doped diamond electrode and its analytical applications.
Canbaz, D; Uslu, B, 2010
)
0.36
" Linezolid was administered intravenously twice daily at a dosage of 600 mg."( Linezolid concentrations in infected soft tissue and bone following repetitive doses in diabetic patients with bacterial foot infections.
Joukhadar, C; Mauric, O; Popovic, M; Scharnagl, E; Schintler, MV; Spendel, S; Traunmüller, F, 2010
)
0.36
" However, in vitro dose-response curves for bone chips impregnated with different kinds of antibiotics are not available."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" In a separate experiment, in vitro dose-response curves were established for bone chips impregnated with cefazolin and vancomycin solutions at five different concentrations."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" The in vitro dose-response curves show that the free-zone diameter increases logarithmically with antibiotic concentration."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" The in vitro dose-response curve can be used to determine the optimal concentration(s) for local application."( Impregnation of bone chips with antibiotics and storage of antibiotics at different temperatures: an in vitro study.
Bloem, RM; Buma, P; Mathijssen, NM; Petit, PL; Pilot, P; Schreurs, BW, 2010
)
0.36
" Nearly 70% of the respondent hospitals reported having a vancomycinspecific dosing or monitoring guideline in place."( Hospital policies and practices on prevention and treatment of infections caused by methicillin-resistant Staphylococcus aureus.
Hennenfent, J; Lambert, BL; McBride, MV; Rodvold, KA; Schiff, G; Schumock, GT; Trese, AM; Tverdek, F; Yang, Y, 2010
)
0.36
" An optimal antibacterial effect is achieved when plasma drug concentrations are above the minimum inhibitory concentration (MIC) [T>MIC] for the entire length of treatment and the ratio between the area under the plasma concentration-time curve (AUC) and the MIC (AUC/MIC) is greater than 100, as is most commonly obtained with administration of the standard dosage of linezolid 600 mg twice daily."( Pharmacological issues of linezolid: an updated critical review.
Danesi, R; Del Tacca, M; Di Paolo, A; Guidotti, E; Malacarne, P, 2010
)
0.36
" A dosage regimen of 10mg/kg body weight given either orally or intravenously every 8h in infants aged >or=1 week and the same dose given every 12h in infants <1 week was shown to be safe and effective with a mean treatment duration of 10-28 days."( Linezolid treatment of nosocomial bacterial infection with multiresistant Gram-positive pathogens in preterm infants: a systematic review.
Kocher, S; Müller, W; Resch, B, 2010
)
0.36
" In order to reduce its adverse effects and maintain efficacy, we investigated whether linezolid in a reduced dosage resulted in drug serum concentrations exceeding a ratio of the in vitro minimum inhibitory concentration (MIC) to the area under the serum concentration-time curve (AUC) over 24 hours (AUC(24)) [AUC(24)/MIC] of >100."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
0.36
" Larger numbers of patients should be studied to confirm the efficacy of the linezolid 300 mg twice-daily dosage in MDR-TB or XDR-TB treatment."( Comparison of the pharmacokinetics of two dosage regimens of linezolid in multidrug-resistant and extensively drug-resistant tuberculosis patients.
Alffenaar, JW; Filguera, P; Harmelink, IM; Kosterink, JG; Molenaar, E; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D; Wessels, AM, 2010
)
0.36
"The objective of the present retrospective observational study carried out in patients receiving a standard dosage of linezolid and undergoing routine therapeutic drug monitoring (TDM) was to assess the interindividual variability in plasma exposure, to identify the prevalence of attainment of optimal pharmacodynamics, and to define if an intensive program of TDM may be warranted in some categories of patients."( Therapeutic drug monitoring of linezolid: a retrospective monocentric analysis.
Cojutti, P; Cristini, F; Franceschi, L; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2010
)
0.36
" Further investigation into β-lactam dosing strategies against different BORSA strains is warranted in order to avoid possible therapy failure."( Diminished in vitro antibacterial activity of oxacillin against clinical isolates of borderline oxacillin-resistant Staphylococcus aureus.
Beisser, PS; Croes, S; Deurenberg, RH; Neef, C; Stobberingh, EE; Terporten, PH, 2010
)
0.36
"Despite the growing epidemic of obesity in the United States, dosing medications in such patients remains poorly studied and understood."( Pharmacotherapy in the critically ill obese patient.
Medico, CJ; Walsh, P, 2010
)
0.36
" There were no hematologic or other safety signals during 28 days of dosing at 600 mg twice daily."( Biomarker-assisted dose selection for safety and efficacy in early development of PNU-100480 for tuberculosis.
Bedarida, G; Campbell, S; Jakubiec, W; Kumar, V; Ladutko, L; Miller, PF; Mitton-Fry, M; Paige, D; Silvia, A; Wallis, RS; Zhu, T, 2011
)
0.37
" Linezolid was given at a dosage of 600 mg, iv, q12h."( [Clinical analysis of 102 blood disease patients with gram positive cocci infection treated with Linezolid].
Fu, R; Guan, J; Liang, Y; Liu, H; Qu, W; Ruan, EB; Shao, ZH; Song, J; Wang, GJ; Wang, HQ; Wang, XM; Wu, YH; Xing, LM, 2010
)
0.36
" The obtained results should be considered for future studies of formulation of structurally related TOZs in oral dosage forms."( Assessment of the stability of novel antibacterial triazolyl oxazolidinones using a stability-indicating high-performance liquid chromatography method.
Abdel-Hamid, ME; Phillips, OA; Sharaf, LH; Varghese, R, 2011
)
0.37
" For a successful therapy it is of vital importance that these compounds are used judiciously and dosed appropriately."( Comparison of the pharmacokinetic properties of vancomycin, linezolid, tigecyclin, and daptomycin.
Derendorf, H; Estes, KS, 2010
)
0.36
" Their mechanism of action, potential for significant raising of HDL-C, once-daily dosing regimen, and favorable lipid-altering effects when added to hydroxymethylglutaryl-CoA reductase inhibitors are key elements."( Anacetrapib and dalcetrapib: two novel cholesteryl ester transfer protein inhibitors.
Miyares, MA, 2011
)
0.37
"To address issues of antibiotic dosing during sustained low-efficiency dialysis by using available pharmacokinetic data, intermittent and continuous renal replacement therapy dialysis guidelines, and our experience with sustained low-efficiency dialysis."( Antibiotic dosing during sustained low-efficiency dialysis: special considerations in adult critically ill patients.
Bogard, KN; Erwin, MW; Fuller, PD; Olsen, KM; Peterson, NT; Plumb, TJ, 2011
)
0.37
"Published clinical trials, case reports, and reviews of antibiotic dosing in humans during sustained low-efficiency dialysis."( Antibiotic dosing during sustained low-efficiency dialysis: special considerations in adult critically ill patients.
Bogard, KN; Erwin, MW; Fuller, PD; Olsen, KM; Peterson, NT; Plumb, TJ, 2011
)
0.37
" Appropriate dose and calculation of dosing intervals is essential to provide adequate antibiotic therapy in these patients."( Antibiotic dosing during sustained low-efficiency dialysis: special considerations in adult critically ill patients.
Bogard, KN; Erwin, MW; Fuller, PD; Olsen, KM; Peterson, NT; Plumb, TJ, 2011
)
0.37
" This stresses the importance of an optimal dosing of the antibiotic when SCVs are present."( Intra- and extracellular activities of dicloxacillin and linezolid against a clinical Staphylococcus aureus strain with a small-colony-variant phenotype in an in vitro model of THP-1 macrophages and an in vivo mouse peritonitis model.
Frimodt-Møller, N; Hughes, D; Lemaire, S; Sandberg, A; Tulkens, PM; Van Bambeke, F; von Eiff, C, 2011
)
0.37
" The present population pharmacokinetic/pharmacodynamic (PPK/PD) study was undertaken to elucidate the factors that determine linezolid levels, the relationship between exposure to linezolid and a decrease in platelet counts, and appropriate dosage adjustments based on exposure levels."( Population pharmacokinetic and pharmacodynamic analysis of linezolid and a hematologic side effect, thrombocytopenia, in Japanese patients.
Higuchi, S; Hirota, T; Horii, T; Ieiri, I; Isagawa, S; Ogawa, K; Otsubo, K; Sasaki, T; Takane, H, 2011
)
0.37
" Dose fractionation studies showed that AUC/MIC was the pharmacodynamic index linked with efficacy, indicating that once-daily dosing in humans is feasible."( In vivo pharmacodynamics of torezolid phosphate (TR-701), a new oxazolidinone antibiotic, against methicillin-susceptible and methicillin-resistant Staphylococcus aureus strains in a mouse thigh infection model.
Drusano, GL; Kulawy, R; Liu, W; Louie, A, 2011
)
0.37
" difficile epidemic strains (ribotypes 027 and 106) and linezolid was dosed to achieve human gut concentrations."( Evaluation of linezolid for the treatment of Clostridium difficile infection caused by epidemic strains using an in vitro human gut model.
Baines, SD; Freeman, J; Hobbs, JK; Huscroft, GS; Lovering, AM; Noel, AR; O'Connor, R; Todhunter, SL; Wilcox, MH, 2011
)
0.37
" difficile PCR ribotype 106 viable counts declined at a faster rate than those of PCR ribotype 027 following dosing with linezolid, but cytotoxin titres declined at a similar rate to an untreated control."( Evaluation of linezolid for the treatment of Clostridium difficile infection caused by epidemic strains using an in vitro human gut model.
Baines, SD; Freeman, J; Hobbs, JK; Huscroft, GS; Lovering, AM; Noel, AR; O'Connor, R; Todhunter, SL; Wilcox, MH, 2011
)
0.37
" Monte Carlo simulation was performed to assess the activities of the linezolid dosing regimens against 42 contemporary MRSA isolates recovered from CF patients."( Pharmacokinetics of intravenous and oral linezolid in adults with cystic fibrosis.
Keel, RA; Kloft, C; Knauft, RF; Kuti, JL; Muhlebach, M; Nicolau, DP; Pope, JS; Schaeftlein, A, 2011
)
0.37
" Appropriate linezolid dosage and hospital infection control measures are essential to avoid the spread of linezolid resistance."( Clinical experience with linezolid in infants and children.
Garazzino, S; Tovo, PA, 2011
)
0.37
" Adequate dosing of these agents is emphasized to minimize the potential for paradoxical induction of virulence."( Antivirulence potential of TR-700 and clindamycin on clinical isolates of Staphylococcus aureus producing phenol-soluble modulins.
Synold, T; Wong-Beringer, A; Yamaki, J, 2011
)
0.37
" These results demonstrated that the submicron emulsion preparation of ZT was a relatively safe dosage form for rapid and effective intranasal delivery of ZT."( Preparation and evaluation of zolmitriptan submicron emulsion for rapid and effective nasal absorption in beagle dogs.
Cai, C; Gu, P; He, H; Qi, N; Tang, X; Yu, C; Zhang, W, 2011
)
0.37
" Hourly plasma and dialysate samples were obtained over a 12-h dosing interval following 3 to 4 doses of linezolid (600 mg intravenously every 12 h)."( Determination of tissue penetration and pharmacokinetics of linezolid in patients with diabetic foot infections using in vivo microdialysis.
Kuti, JL; Nicolau, DP; Shepard, A; Wiskirchen, DE, 2011
)
0.37
"5, 1 (end of infusion), 2, 4, 8, 12, and 24 h after intravenous dosing of linezolid 600 and 1,200 mg."( Lack of an effect of standard and supratherapeutic doses of linezolid on QTc interval prolongation.
Alvey, C; Choo, HW; Cuozzo, C; Damle, B; Kirby, D; Labadie, RR; Riley, S, 2011
)
0.37
" In summary, these findings point to highly variable PK/PD properties of linezolid in severely ill patients, providing the rationale for targeting linezolid dosage to each individual patient's specific properties."( Clinical pharmacokinetic/pharmacodynamic profile of linezolid in severely ill intensive care unit patients.
Dong, H; Dong, Y; Lei, J; Li, H; Sun, J; Wang, M; Wang, X; Xing, J; You, H; Zhu, H, 2011
)
0.37
" Three dosing regimens were simulated with each drug alone: linezolid (AUC(24)/MIC 30, 60 and 200 h-L30, L60 and L200, respectively) and doxycycline (AUC(24)/MIC 90, 180 and 520 h - D90, D180 and D520, respectively) and in combination: linezolid plus doxycycline (L30+D90; L60+D180 and L200+D520)."( The antistaphylococcal pharmacodynamics of linezolid alone and in combination with doxycycline in an in vitro dynamic model.
Dovzhenko, SA; Firsov, AA; Kobrin, MB; Portnoy, YA; Smirnova, MV; Strukova, EN; Zinner, SH, 2011
)
0.37
"We evaluated the possible association between trough linezolid (LZD) concentrations and platelet counts using a dose-response curve with a logit model equation."( Correlation between serum linezolid concentration and the development of thrombocytopenia.
Hiraike, M; Hiraki, Y; Kamimura, H; Karube, Y; Matsumoto, K; Misumi, N; Morita, K; Tsuji, Y, 2012
)
0.38
" Thus, no dosage adjustment for digoxin is necessary when co-administered with anacetrapib."( Lack of an effect of anacetrapib on the pharmacokinetics of digoxin in healthy subjects.
Ali, M; Connolly, SM; DeGroot, B; Garg, A; Gendrano, IN; Krishna, R; Li, S; Liu, Y; Maes, A; Stoch, SA; Stypinski, D; Wagner, JA, 2011
)
0.37
" An early and adequate antibiotic treatment at correct dosage is extremely important."( [Antibiotic dose adjustment in the treatment of MRSA infections in patients with acute renal failure undergoing continuous renal replacement therapies].
Carcelero, E; Soy, D, 2012
)
0.38
" A drug interaction study for warfarin with a novel CETP inhibitor is expected to be helpful in defining dosing regimens."( Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects.
Ali, M; Connolly, SM; Cote, J; Degroot, B; Garg, A; Krishna, R; Li, S; Liu, Y; Maes, A; Stoch, SA; Stypinski, D; Wagner, JA, 2012
)
0.38
" Thus, no dosage adjustment for warfarin is necessary when co-administered with anacetrapib."( Lack of a meaningful effect of anacetrapib on the pharmacokinetics and pharmacodynamics of warfarin in healthy subjects.
Ali, M; Connolly, SM; Cote, J; Degroot, B; Garg, A; Krishna, R; Li, S; Liu, Y; Maes, A; Stoch, SA; Stypinski, D; Wagner, JA, 2012
)
0.38
" Early initiated continuous monitoring of hematological values and linezolid dosage adjustment for body weight are recommended."( Immediate hematological toxicity of linezolid in healthy volunteers with different body weight: a phase I clinical trial.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Guo, D; Liang, B; Liu, Y; Vouloumanou, EK; Wang, R, 2012
)
0.38
" Plasma samples were collected over the dosing interval, and participants were randomized to undergo bronchoalveolar lavage (BAL) at 2, 6, 12, or 24 h after the last dose."( Pulmonary disposition of tedizolid following administration of once-daily oral 200-milligram tedizolid phosphate in healthy adult volunteers.
Housman, ST; Kuti, JL; Nicolau, DP; Pope, JS; Russomanno, J; Salerno, E; Shore, E, 2012
)
0.38
"My general pharmacokinetic scaling theory is discussed for the important matter of determining pediatric dosing for existing and new therapeutic drugs when optimal, or near-optimal, dosing for adults is known."( Scaling adult doses of antifungal and antibacterial agents to children.
Dawson, TH, 2012
)
0.38
" No significant differences were detected in the subgroup efficacy analysis (daily linezolid dosage ≤ 600 mg versus >600 mg)."( Efficacy, safety and tolerability of linezolid containing regimens in treating MDR-TB and XDR-TB: systematic review and meta-analysis.
Alffenaar, JW; Anger, HA; Caminero, JA; Castiglia, P; Centis, R; D'Ambrosio, L; De Lorenzo, S; Ferrara, G; Koh, WJ; Migliori, GB; Schecter, GF; Shim, TS; Singla, R; Skrahina, A; Sotgiu, G; Spanevello, A; Udwadia, ZF; Villar, M; Zampogna, E; Zellweger, JP; Zumla, A, 2012
)
0.38
" Dosage adjustments were performed when C(min) ≥10 mg/L and/or AUC₂₄ ≥400 mg/L · h."( Therapeutic drug monitoring may improve safety outcomes of long-term treatment with linezolid in adult patients.
Cojutti, P; Del Pin, B; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2012
)
0.38
" Dosage adjustments were needed in 40% versus 0% of patients in the linezolid group (n = 35) versus the linezolid + rifampicin group (n = 10), respectively."( Therapeutic drug monitoring may improve safety outcomes of long-term treatment with linezolid in adult patients.
Cojutti, P; Del Pin, B; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2012
)
0.38
" Thus, more aggressive vancomycin dosing has the potential to improve efficacy."( Treatment of methicillin-resistant Staphylococcus aureus ventilator-associated pneumonia with high-dose vancomycin or linezolid.
Boucher, BA; Christopher Wood, G; Croce, MA; Fabian, TC; Hamilton, LA; Magnotti, LJ; Martin, JB; Swanson, JM, 2012
)
0.38
" Detailed stability exercises including drug stability in blood, hemolyzed, lipemic and normal plasma were conducted to extend the method applicability in vast majority of clinical studies using 800 mg metaxalone extended release oral dosage form."( Metaxalone estimation in biological matrix using high-throughput LC-MS/MS bioanalytical method.
Goswami, D; Gurule, S; Khuroo, A; Monif, T; Saha, A; Vats, P, 2012
)
0.38
" In a recent prospective, randomized, open-label, comparator-controlled, multicenter, phase 4 clinical trial in adults with complicated skin and soft tissue infections (cSSTIs) caused by methicillin-resistant Staphylococcus aureus (MRSA), linezolid achieved clinical and microbiologic success comparable to appropriately dosed intravenous vancomycin."( Clinical efficacy of oral linezolid compared with intravenous vancomycin for the treatment of methicillin-resistant Staphylococcus aureus-complicated skin and soft tissue infections: a retrospective, propensity score-matched, case-control analysis.
Baruch, AM; Bhattacharyya, H; Biswas, P; Itani, KM; Reisman, A, 2012
)
0.38
" The aggressive vancomycin dosing regimens are still associated with unacceptable high microbiological failure rates and it is not currently possible to achieve probability of target attainment at higher vancomycin MICs of 2 mg/l."( Does resistance in severe infections caused by methicillin-resistant Staphylococcus aureus give you the 'creeps'?
Brink, AJ, 2012
)
0.38
"Continued monitoring of patients on aggressive vancomycin dosing schedules is advised."( Does resistance in severe infections caused by methicillin-resistant Staphylococcus aureus give you the 'creeps'?
Brink, AJ, 2012
)
0.38
"The optimal dosage of linezolid to avoid hematologic toxicity is unknown."( A reduced linezolid dosage maintains favorable efficacy with minimal hematologic toxicity in a methicillin-resistant Staphylococcus aureus-infected patient with renal insufficiency.
Anraku, Y; Horio, M; Kawaguchi, T; Miyakawa, T; Mizuta, H; Ohmura, T; Okada, T; Saito, H; Taguchi, K, 2013
)
0.39
" Linezolid remains costly, and a reduced dosage and duration may result in fewer adverse events and lower cost."( Linezolid-containing regimens for the treatment of drug-resistant tuberculosis in South African children.
Hallbauer, UM; Hesseling, AC; Rose, PC; Schaaf, HS; Seddon, JA, 2012
)
0.38
" The areas under the curve for the 12-h dosing interval (AUCτ) were similar between moderately obese and morbidly obese groups: 130."( Pharmacokinetics of intravenous linezolid in moderately to morbidly obese adults.
Bhalodi, AA; Kuti, JL; Nicolau, DP; Papasavas, PK; Tishler, DS, 2013
)
0.39
" Dose-response data were analyzed by a maximum effect (E(max)) model using nonlinear regression."( Inoculum effects of ceftobiprole, daptomycin, linezolid, and vancomycin with Staphylococcus aureus and Streptococcus pneumoniae at inocula of 10(5) and 10(7) CFU injected into opposite thighs of neutropenic mice.
Andes, DR; Craig, WA; Lee, DG; Murakami, Y, 2013
)
0.39
"Our findings suggest that a weight-adjusted, 10 mg/kg regimen of linezolid may be more appropriate than fixed dosing for patients of different body weight."( Weight-adjusted versus fixed dose of linezolid for Chinese healthy volunteers of higher and lower body weight: a Phase I pharmacokinetic and pharmacodynamic study.
Bai, N; Cai, Y; Chai, D; Falagas, ME; Karageorgopoulos, DE; Liang, B; Wang, R, 2013
)
0.39
" All of the five subjects who were examined 1 week after dosing with zolmitriptan showed higher BP ND post drug administration compared with baseline."( A PET study with [11C]AZ10419369 to determine brain 5-HT1B receptor occupancy of zolmitriptan in healthy male volunteers.
Farde, L; Halldin, C; Jučaite, A; Kanes, S; McCarthy, DJ; Nord, M; Stenkrona, P; Varnäs, K, 2013
)
0.39
" In a suspected case, the doctor was recommended to discontinue, decrease the dosage or keep the drug under observation; and a follow-up of the patient's platelet count was made in order to classify the relationship between the drug and thrombocytopenia."( [Incidence of drug-induced thrombocytopenia in hospitalized patients].
Álvarez-Arroyo, L; Delgado-Sánchez, O; Seco-Melantuche, R,
)
0.13
" The doctor was recommended to discontinue the drug (2), decrease the dosage (3) or keep it under observation (3), with 100% acceptance."( [Incidence of drug-induced thrombocytopenia in hospitalized patients].
Álvarez-Arroyo, L; Delgado-Sánchez, O; Seco-Melantuche, R,
)
0.13
" Further studies are required to evaluate whether therapeutic drug monitoring-guided dosage adjustment of linezolid decreases the adverse effects while maintaining treatment efficacy in patients with renal dysfunction."( High plasma linezolid concentration and impaired renal function affect development of linezolid-induced thrombocytopenia.
Hatakeyama, S; Hisaka, A; Moriya, K; Nukui, Y; Okamoto, K; Suzuki, H; Yamamoto, T; Yata, N; Yotsuyanagi, H, 2013
)
0.39
"We evaluated treatment with linezolid, dosed at 800 mg once daily for 1 to 4 months as guided by sputum culture status and tolerance and then at 1,200 mg thrice weekly until ≥ 1 year after culture conversion, in addition to individually optimized regimens among 10 consecutive patients with extensively drug-resistant tuberculosis or fluoroquinolone-resistant multidrug-resistant tuberculosis."( Can intermittent dosing optimize prolonged linezolid treatment of difficult multidrug-resistant tuberculosis?
Chan, RC; Chang, KC; Chau, CH; Cheung, SW; Leung, CC; Tam, CM; Wen, PK; Yew, WW, 2013
)
0.39
" This open-label, fixed-sequence, 3-period study was intended to evaluate the potential of anacetrapib to be a victim of OATP1B1/3 inhibition and strong CYP3A induction using acute and chronic dosing of rifampin, respectively, as a probe."( Effects of Rifampin, a potent inducer of drug-metabolizing enzymes and an inhibitor of OATP1B1/3 transport, on the single dose pharmacokinetics of anacetrapib.
Anderson, MS; Auger, P; Cote, J; Gutstein, DE; Hohnstein, A; Johnson-Levonas, AO; Liu, Y; Rasmussen, S; Stypinski, D, 2013
)
0.39
" Linezolid was given intravenously (IV) at a dosage of 600 mg q12h and vancomycin IV at 500 mg q6h."( Vancomycin versus linezolid in the treatment of methicillin-resistant Staphylococcus aureus meningitis.
Arda, B; Aydemir, S; Bardak-Ozcem, S; Dalbasti, T; Pullukcu, H; Ruksen, M; Sipahi, H; Sipahi, OR; Turhan, T; Ulusoy, S; Yurtseven, T; Zileli, M, 2013
)
0.39
"Limited data on linezolid dosing in the morbidly obese population show lower serum drug concentrations than those in nonobese patients, but no clinical failure has been reported when treating MRSA skin and soft tissue infections or MRSA tracheitis."( Subtherapeutic linezolid concentrations in a patient with morbid obesity and methicillin-resistant Staphylococcus aureus pneumonia: case report and review of the literature.
Lee, KB; Muzevich, KM, 2013
)
0.39
"The oral liquid formulations poses an alternative way in providing medications to pediatric patients, geriatric patients, patients with feeding tubes, and patients who cannot swallow solid dosage forms."( Pharmacokinetics and relative bioavailability evaluation of linezolid suspension and tablet formulations.
Helmy, SA, 2013
)
0.39
" In vivo dose-response studies demonstrated that oral linezolid administration sufficiently decreased bronchoalveolar lavage fluid levels of IFN-γ at day 7 postinfluenza infection in a dose-dependent manner."( Linezolid decreases susceptibility to secondary bacterial pneumonia postinfluenza infection in mice through its effects on IFN-γ.
Birket, SE; Breslow-Deckman, JM; Feola, DJ; Garvy, BA; Ho, TN; Hoskins, SN; Mattingly, CM, 2013
)
0.39
"This work describes a simple and sensitive method for simultaneous determination of zolmitriptan, naproxen and propranolol in their dosage forms using HPLC."( A rapid and sensitive HPLC assay of some concomitant anti-migraine drugs.
El-Kadi, AO; Lotfy, HM; Michael, AM; Rezk, MR; Shehata, MA, 2014
)
0.4
" Because there are physiologic, pharmacologic, and dosing differences related to weight, it is important to evaluate the impact of weight on antimicrobial agents to optimize clinical outcomes."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
"We analyzed data from 2 clinical trials of patients randomized to receive a fixed dose of linezolid or weight-based dosing of vancomycin for the treatment of cSSSIs or NP caused by MRSA."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
" Among patients with cSSSIs, clinical success rates at the study end with fixed-dose linezolid were similar across all weight quartiles and similar to weight-based dosing of vancomycin for Q1-3."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
"Except for Q4 within the vancomycin-treated patients for MRSA cSSSI, the efficacy of fixed-dosed linezolid and weight-based dosing of vancomycin was maintained across all weight quartiles and MRSA infection types."( Impact of weight on treatment efficacy and safety in complicated skin and skin structure infections and nosocomial pneumonia caused by methicillin-resistant Staphylococcus aureus.
Barreto, JN; Huang, DB; Morrow, LE; Puzniak, LA, 2013
)
0.39
" We evaluated the efficacy of two cadazolid dosing regimens (250 versus 750 mg/L twice daily for 7 days) to treat simulated CDI."( In vitro activity of cadazolid against clinically relevant Clostridium difficile isolates and in an in vitro gut model of C. difficile infection.
Athanasiou, A; Baines, SD; Chilton, CH; Crowther, GS; Freeman, J; Locher, HH; Todhunter, SL; Wilcox, MH, 2014
)
0.4
"Bioadhesive nasal dosage forms are an attractive method for overcoming rapid mucociliary clearance transport in the nose and for delivering the drug directly to brain."( Formulation and evaluation of chitosan-chondroitin sulphate based nasal inserts for zolmitriptan.
Kaur, G; Kaur, K, 2013
)
0.39
" A microemulsion-based technology has various advantages over other technically complex dosage forms."( Duel-acting subcutaneous microemulsion formulation for improved migraine treatment with zolmitriptan and diclofenac: formulation and in vitro-in vivo characterization.
Christie, M; Dubey, R; Martini, LG, 2014
)
0.4
"The effects of pressure, temperature, time, concentration and dosage of alcohol were studied by single factor analysis and orthogonal test."( [The extraction technology of epigoitri from isatidis radix by supercritical CO2 fluid].
Liu, CY; Liu, LM; Nian, SH; Yang, LF, 2013
)
0.39
"The optimized conditions were as follows: The pressure was 20 MPs, the temperature was 50 degrees C, the time was 2 h, concentration of alcohol was 100%, dosage was 80 mL."( [The extraction technology of epigoitri from isatidis radix by supercritical CO2 fluid].
Liu, CY; Liu, LM; Nian, SH; Yang, LF, 2013
)
0.39
" In such cases, we suggest optimized adjustment of the linezolid dosage regimen."( Developments in the pharmacokinetic/pharmacodynamic index of linezolid: a step toward dose optimization using Monte Carlo simulation in critically ill patients.
Chen, L; Dong, H; Dong, Y; Sun, J; Wang, T; Xie, J; Zhao, Y, 2014
)
0.4
" Model parameters were used to simulate in vivo activity after oral dosing with sutezolid at 600 mg twice a day (BID) and 1,200 mg once a day (QD)."( Population pharmacokinetic/pharmacodynamic analysis of the bactericidal activities of sutezolid (PNU-100480) and its major metabolite against intracellular Mycobacterium tuberculosis in ex vivo whole-blood cultures of patients with pulmonary tuberculosis.
Diacon, A; Friedrich, SO; Wallis, RS; Zhu, T, 2014
)
0.4
" This study was aimed to evaluate whether standard dosing of linezolid leads to therapeutic serum concentrations in critically ill patients."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
0.4
"In this prospective observational study, 30 critically ill adult patients with suspected infections received standard dosing of 600 mg linezolid intravenously twice a day."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
0.4
" The findings suggest that therapeutic drug monitoring of linezolid might be helpful for adequate dosing of linezolid in critically ill patients."( Variability of linezolid concentrations after standard dosing in critically ill patients: a prospective observational study.
Bruegel, M; Döbbeler, G; Frey, L; Grabein, B; Holdt, LM; Hornuss, C; Maier, B; Nagel, D; Neugebauer, C; Teupser, D; Vogeser, M; Weig, T; Zander, J; Zoller, M, 2014
)
0.4
" This recommended initial dosage and subsequent dosage adjustment for the target concentration range should avoid adverse events, thereby enabling effective linezolid-based therapies to be continued."( Analysis of thrombocytopenic effects and population pharmacokinetics of linezolid: a dosage strategy according to the trough concentration target and renal function in adult patients.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2014
)
0.4
"To report on linezolid exposure in a paediatric population who routinely underwent therapeutic drug monitoring (TDM) for dosage optimization and to assess the factors affecting interpatient variability."( Pharmacokinetic/pharmacodynamic evaluation of linezolid in hospitalized paediatric patients: a step toward dose optimization by means of therapeutic drug monitoring and Monte Carlo simulation.
Cojutti, P; Crichiutti, G; Isola, M; Maximova, N; Pea, F, 2015
)
0.42
" Simulations showed a PTA of ≥ 90% with the current dosing regimens in both groups only for pathogens with an MIC ≤ 1 mg/L."( Pharmacokinetic/pharmacodynamic evaluation of linezolid in hospitalized paediatric patients: a step toward dose optimization by means of therapeutic drug monitoring and Monte Carlo simulation.
Cojutti, P; Crichiutti, G; Isola, M; Maximova, N; Pea, F, 2015
)
0.42
" TDM is a diagnostic standard for the individualization of polypharmcotherapy based on validated analytical methods (in particular LC-MS/MS and HPLC-methods) in order to optimize dosing and drug safety."( [Therapeutic Drug Monitoring of antiinfectives in intensive care medicine].
Adam, R; Michels, G; Müller, C; Nosseir, NS; Pfister, R; Wiesen, MH, 2014
)
0.4
" Administration of higher than standard doses of linezolid and therapeutic drug monitoring should therefore be considered as options to optimise linezolid dosing in critically ill patients with CNS infections."( Plasma and cerebrospinal fluid concentrations of linezolid in neurosurgical critically ill patients with proven or suspected central nervous system infections.
Alvarez-Lerma, F; Basas, M; Campillo, N; Ferrández, O; Grau, S; Horcajada, JP; Lipman, J; Luque, S; Roberts, JA, 2014
)
0.4
"The minimum inhibitory concentrations (MICs) of vancomycin and norvancomycin for half of the isolates decreased below the susceptibility break point, and the MIC of linezolid for one isolate was decreased to the blood and epithelial lining fluid concentration using the current dosing regimen."( Colistin and anti-Gram-positive bacterial agents against Acinetobacter baumannii.
Bai, Y; Di, X; Liu, B; Liu, Y; Wang, J; Wang, R; Zhang, X, 2014
)
0.4
" The present study aimed to define the pharmacokinetic parameters of intravenous linezolid in pediatric patients and assess the rationale for the approved dosage recommendations."( Linezolid dosage in pediatric patients based on pharmacokinetics and pharmacodynamics.
Ikawa, K; Matsumoto, K; Morikawa, N; Shigemi, A; Takeda, Y; Takeshita, A; Watanabe, E; Yokoyama, Y, 2015
)
0.42
" The main objective of this review is to compare the relative efficacies, dosing strategies, and side-effect profiles of quinupristin-dalfopristin, linezolid, and daptomycin for VRE bacteremia in the pediatric population."( Optimizing therapy for vancomycin-resistant enterococcal bacteremia in children.
Hsu, AJ; Tamma, PD, 2014
)
0.4
" aureus RMs (resistant to 2× and 4×MIC but not 8× and 16×MIC) were enriched at ratios of the 24-h area under the concentration-time curve (AUC24) to the MIC that provide linezolid concentrations between the MIC and MPC for 100% (AUC24/MIC, 60 h) and 86% (AUC24/MIC, 120 h) of the dosing interval."( In vitro resistance studies with bacteria that exhibit low mutation frequencies: prediction of "antimutant" linezolid concentrations using a mixed inoculum containing both susceptible and resistant Staphylococcus aureus.
Edelstein, MV; Firsov, AA; Golikova, MV; Portnoy, YA; Romanov, AV; Strukova, EN; Zinner, SH, 2015
)
0.42
" The extent of this variability makes the case for therapeutic drug monitoring since an area under the inhibitory curve greater than 80 to 120 and the time above the minimum inhibitory concentration over the entire dosing interval strongly correlate with linezolid treatment efficacy."( Therapeutic drug monitoring: linezolid too?
Brink, AJ; Richards, GA, 2014
)
0.4
" Therapeutic drug monitoring dosage adjustments may be especially useful in patients with renal dysfunction and severe MRSA infection."( Treatment of mediastinitis due to methicillin-resistant Staphylococcus aureus in a renal dysfunction patient undergoing adjustments to the linezolid dose.
Ashizawa, N; Fukahara, K; Nagura, S; Narukawa, M; Obi, H; Ota, Y; Tashiro, M; To, H; Tsuji, Y; Yamamoto, Y; Yoshimura, N, 2015
)
0.42
" A higher dosage of the drug showed a higher accumulation in these bacteria in a dosing range of 5-50 ng/mL."( Thinking outside the "bug": a unique assay to measure intracellular drug penetration in gram-negative bacteria.
Isabella, V; Joubran, C; Miller, A; Miller-Vedam, L; Nayar, A; Tentarelli, S; Zhou, Y, 2015
)
0.42
" Dosing ETX0914 in human volunteers showed sufficient exposure and minimal adverse effects to expect a highly efficacious anti-gonorrhea therapy."( Responding to the challenge of untreatable gonorrhea: ETX0914, a first-in-class agent with a distinct mechanism-of-action against bacterial Type II topoisomerases.
Alm, RA; Barvian, K; Basarab, GS; Doig, P; Galullo, V; Gardner, H; Gowravaram, M; Huband, M; Kern, GH; Kimzey, A; Kutschke, A; Lahiri, SD; Lawrence, K; McNulty, J; Morningstar, M; Mueller, JP; Newman, JV; Perros, M; Schuck, VJ; Singh, R; Tommasi, R; Vishwanathan, K; Walkup, G, 2015
)
0.42
" Each dosage of cadazolid resulted in a lower recurrence rate than with vancomycin (18."( Multicenter, Double-Blind, Randomized, Phase 2 Study Evaluating the Novel Antibiotic Cadazolid in Patients with Clostridium difficile Infection.
Buitrago, M; Charef, P; Cornely, OA; Gerding, DN; Kracker, H; Louie, T; Nord, CE; Talbot, GH; Wilcox, M, 2015
)
0.42
" Increasing the dosage regimen can be applied to ceftriaxone and azithromycin, but the emergence of high-level resistance has already been reported."( New treatment options for infections caused by increasingly antimicrobial-resistant Neisseria gonorrhoeae.
Chong, Y; Lee, H; Lee, K, 2016
)
0.43
" Mice were dosed orally with 10 mg/kg anacetrapib daily for 42 days."( Disposition into Adipose Tissue Determines Accumulation and Elimination Kinetics of the Cholesteryl Ester Transfer Protein Inhibitor Anacetrapib in Mice.
Burton, A; Chavez-Eng, C; Gheyas, F; Gutstein, D; Hartmann, G; Jackson, T; Johns, D; Kumar, S; Lederman, H; Lutz, R; Mitra, K; Shen, X, 2016
)
0.43
"Zolmitriptan is the drug of choice for migraine, but low oral bioavailability (<50%) and recurrence of migraine lead to frequent dosing and increase in associated side effects."( Poloxamer 407-based intranasal thermoreversible gel of zolmitriptan-loaded nanoethosomes: formulation, optimization, evaluation and permeation studies.
Dhamecha, D; Jalalpure, S; Shahi, S; Shelke, S, 2016
)
0.43
" The role of individualized drug dosing regimens for other oxazolidinones remains to be proven."( Drug monitoring and individual dose optimization of antimicrobial drugs: oxazolidinones.
Alffenaar, JW; Cattaneo, D; Neely, M, 2016
)
0.43
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
"The inverted U-shaped, methamphetamine dose-response function for intake on the fixed ratio 5 schedule was shifted downward by CP 94,253 both before and after abstinence."( Preclinical Evidence That 5-HT1B Receptor Agonists Show Promise as Medications for Psychostimulant Use Disorders.
Cotter, AR; Garcia, R; Leslie, K; Neisewander, JL; Olive, MF, 2017
)
0.46
" Consumption of a traditional Japanese breakfast prior to dosing increased the plasma pharmacokinetics of anacetrapib in Japanese subjects compared with fasted conditions, to a similar extent as in white subjects."( Pharmacokinetics and Pharmacodynamics of Anacetrapib Following Single Doses in Healthy, Young Japanese and White Male Subjects.
Cote, J; Denker, AE; Gheyas, F; Krishna, R; Laterza, O; Liu, Y; Ruckle, JL; Wagner, JA, 2018
)
0.48
" This newer oxazolidinone offers the advantages of once-daily dosing and a better safety profile in healthy volunteer studies (fewer gastrointestinal and haematological side effects)."( Clinical Pharmacokinetics and Pharmacodynamics of Oxazolidinones.
Muller, L; Roberts, JA; Roger, C, 2018
)
0.48
" Serial blood samples for PK analysis were collected up to 12 h after dosing on day 21."( Safety, tolerability and pharmacokinetics of 21 day multiple oral administration of a new oxazolidinone antibiotic, LCB01-0371, in healthy male subjects.
Cho, YL; Choi, Y; Chung, JY; Jang, IJ; Jang, K; Kim, A; Lee, SW; Nam, H; Yu, KS, 2018
)
0.48
"Thirty-two healthy male subjects received BID 400-1600 mg multiple oral dosing of LCB01-0371 (200-mg tablet or 400-mg tablet) for 7 days, and 6 subjects received an 800-mg single oral dose of LCB01-0371 (400-mg tablet)."( Multiple-dose Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Oral LCB01-0371 in Healthy Male Volunteers.
Bae, KS; Cho, YL; Cho, YS; Lim, HS; Nam, HS, 2018
)
0.48
" A tedizolid dose of 200 mg/day or 700 mg twice a week is recommended for testing in patients; the intermittent tedizolid dosing schedule could be much safer than daily linezolid."( The Sterilizing Effect of Intermittent Tedizolid for Pulmonary Tuberculosis.
Cirrincione, K; Deshpande, D; Dheda, K; Gumbo, T; Lee, PS; Nuermberger, E; Srivastava, S, 2018
)
0.48
"This study assessed the tolerability and pharmacokinetic (PK) properties of a new-generation oxazolidinone, contezolid (MRX-I), and its major inactive metabolite, M2, after single oral administrations of 800, 1200, and 1600 mg in the fed state, and compared the efficacy of 3 dosing regimens in the treatment of methicillin-resistant Staphylococcus aureus (MRSA) infection based on PK/pharmacodynamic (PD) analysis."( Tolerability and Pharmacokinetics of Contezolid at Therapeutic and Supratherapeutic Doses in Healthy Chinese Subjects, and Assessment of Contezolid Dosing Regimens Based on Pharmacokinetic/Pharmacodynamic Analysis.
Cao, G; Chen, Y; Guo, B; Guo, Y; Hu, F; Wang, Y; Wu, H; Wu, J; Wu, X; Yu, J; Yuan, H; Zhang, J; Zhu, D, 2019
)
0.51
" Steady-state concentrations of contezolid following the 3 dosing regimens (800, 1200, and 1600 mg q12h) were simulated by employing a newly developed 2-compartmental PK model."( Tolerability and Pharmacokinetics of Contezolid at Therapeutic and Supratherapeutic Doses in Healthy Chinese Subjects, and Assessment of Contezolid Dosing Regimens Based on Pharmacokinetic/Pharmacodynamic Analysis.
Cao, G; Chen, Y; Guo, B; Guo, Y; Hu, F; Wang, Y; Wu, H; Wu, J; Wu, X; Yu, J; Yuan, H; Zhang, J; Zhu, D, 2019
)
0.51
" To our knowledge, this is the first PK study to predict that a dosing regimen of 800 mg q12h of oral contezolid is sufficient for treating MRSA infection, with a MIC of ≤4 mg/L."( Tolerability and Pharmacokinetics of Contezolid at Therapeutic and Supratherapeutic Doses in Healthy Chinese Subjects, and Assessment of Contezolid Dosing Regimens Based on Pharmacokinetic/Pharmacodynamic Analysis.
Cao, G; Chen, Y; Guo, B; Guo, Y; Hu, F; Wang, Y; Wu, H; Wu, J; Wu, X; Yu, J; Yuan, H; Zhang, J; Zhu, D, 2019
)
0.51
" [D-Val5]NPS dosing at 20 nmol and SHA 68 dosing at 50 mg/kg significantly decreased the number of visits to the 2 odorants interchanged spatially, switched odorants, in recall trial, and simultaneously reduced the percentage of Fos-ir in NPSR-ir neurons, which were densely distributed in the anterior olfactory nucleus, piriform cortex, subiculum, presubiculum, and parasubiculum."( Neuropeptide S Displays as a Key Neuromodulator in Olfactory Spatial Memory.
Cai, CC; Chen, HL; Cong, CY; Cui, GF; Dong, CY; Hou, YP; Kong, XP; Li, J; Ren, YL; Shao, YF; Wang, C; Xie, JF; Xin, L, 2020
)
0.56
" Another goal was to evaluate the 2 dosing regimens against methicillin-resistant Staphylococcus aureus infections based on PK/PD analysis."( Population Pharmacokinetics Study of Contezolid (MRX-I), a Novel Oxazolidinone Antibacterial Agent, in Chinese Patients.
Cao, G; Chen, Y; Guo, B; Li, L; Wu, H; Wu, J; Wu, X; Yuan, H; Zhang, J; Zhang, Y; Zhao, M, 2020
)
0.56
"The aim of this study is to investigate the influence of hard capsule shells on the possibility of non-invasive monitoring and authentication of medicines presented in capsules dosage form."( Influence of the quality of capsule shell on the non-invasive monitoring of medicines using Terizidone as an example.
Balyklova, KS; Demkin, NA; Pomerantsev, AL; Rodionova, OY; Titova, AV, 2021
)
0.62
" Clinical investigations with daily doses of 200 mg for 6 days showed non-inferiority to twice-daily dosing of linezolid 600 mg for 10 days in patients with acute bacterial skin and skin-structure infections."( Pharmacokinetics and Pharmacodynamics of Tedizolid.
Iqbal, K; Milioudi, A; Wicha, SG, 2022
)
0.72
"This study aimed to build a population pharmacokinetic (PopPK) model for contezolid tablet (MRX-I) in healthy subjects and adults with complicated skin and soft-tissue infections (cSSTIs) to further evaluate the efficacy and safety of contezolid and recommend the optimal dosing regimen based on pharmacokinetic/pharmacodynamic (PK/PD) analysis."( Clinical Pharmacology and Utility of Contezolid in Chinese Patients with Complicated Skin and Soft-Tissue Infections.
Cao, G; Chen, Y; Guo, B; Huang, H; Li, Y; Wu, H; Wu, J; Wu, X; Yang, W; Yu, J; Yuan, H; Yuan, Z; Zhang, J; Zhang, Y, 2022
)
0.72
" The dosage was selected based on mouse pharmacokinetic analysis of both linezolid and TBI-223, as well as measurement of the MICs."( The Novel Oxazolidinone TBI-223 Is Effective in Three Preclinical Mouse Models of Methicillin-Resistant Staphylococcus aureus Infection.
Archer, NK; Dikeman, DA; Fotouhi, N; Gordon, O; Gough, E; Kaushik, A; Miller, LS; Mumtaz, M; Nuermberger, EL; Orlando, N; Ortines, RV; Patel, AM; Upton, AM; Wang, Y; Youn, C; Zhang, J, 2022
)
0.72
" Randomized controlled trials (RCTs) using intranasal agents (no restrictions on dose, formulation, dosing regimen or timing of the first dose) to treat adult patients with acute migraine were included."( Efficacy and safety of intranasal agents for the acute treatment of migraine: a systematic review and network meta-analysis.
Duan, S; Li, G; Liu, L; Liu, Z; Ren, Z; Wang, Z; Xia, H; Zhu, T, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
metaboliteAny intermediate or product resulting from metabolism. The term 'metabolite' subsumes the classes commonly known as primary and secondary metabolites.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
oxazolidinoneAn oxazolidine containing one or more oxo groups.
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency112.20200.354828.065989.1251AID504847
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency35.48130.050127.073689.1251AID588590
gemininHomo sapiens (human)Potency0.23440.004611.374133.4983AID624296; AID624297
VprHuman immunodeficiency virus 1Potency0.89131.584919.626463.0957AID651644
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency39.81073.981146.7448112.2020AID720708
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (10)

Processvia Protein(s)Taxonomy
adaptive immune responseRap guanine nucleotide exchange factor 4Homo sapiens (human)
G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayRap guanine nucleotide exchange factor 4Homo sapiens (human)
calcium-ion regulated exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of exocytosisRap guanine nucleotide exchange factor 4Homo sapiens (human)
insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
positive regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of synaptic vesicle cycleRap guanine nucleotide exchange factor 4Homo sapiens (human)
Ras protein signal transductionRap guanine nucleotide exchange factor 4Homo sapiens (human)
regulation of insulin secretionRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
guanyl-nucleotide exchange factor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
cAMP bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
protein-macromolecule adaptor activityRap guanine nucleotide exchange factor 4Homo sapiens (human)
small GTPase bindingRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
cytosolRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
hippocampal mossy fiber to CA3 synapseRap guanine nucleotide exchange factor 4Homo sapiens (human)
plasma membraneRap guanine nucleotide exchange factor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (13)

Assay IDTitleYearJournalArticle
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (4,186)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990212 (5.06)18.7374
1990's218 (5.21)18.2507
2000's1775 (42.40)29.6817
2010's1718 (41.04)24.3611
2020's263 (6.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 22.55

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index22.55 (24.57)
Research Supply Index8.46 (2.92)
Research Growth Index5.21 (4.65)
Search Engine Demand Index25.99 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.55)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials347 (7.93%)5.53%
Reviews542 (12.39%)6.00%
Case Studies563 (12.87%)4.05%
Observational9 (0.21%)0.25%
Other2,915 (66.61%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]