Carbamazepine is an anticonvulsant medication used to treat epilepsy, bipolar disorder, and neuropathic pain. It is synthesized through a multi-step process involving the reaction of 2-acetyl-1,3-cyclohexanedione with benzoyl chloride. Carbamazepine exerts its therapeutic effects by modulating the activity of voltage-gated sodium channels in the brain, thereby reducing neuronal excitability and preventing seizures. Its importance lies in its efficacy in treating various neurological conditions, making it a widely prescribed drug. The study of carbamazepine focuses on understanding its mechanism of action, optimizing its therapeutic use, and developing novel anticonvulsants with improved safety and efficacy. Research is also being conducted to explore its potential in treating other disorders, such as migraine, trigeminal neuralgia, and anxiety.'
Carbamazepine: A dibenzazepine that acts as a sodium channel blocker. It is used as an anticonvulsant for the treatment of grand mal and psychomotor or focal SEIZURES. It may also be used in the management of BIPOLAR DISORDER, and has analgesic properties.
carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant.
ID Source | ID |
---|---|
PubMed CID | 2554 |
CHEMBL ID | 108 |
CHEBI ID | 3387 |
SCHEMBL ID | 21639 |
SCHEMBL ID | 19838283 |
MeSH ID | M0003328 |
Synonym |
---|
BIDD:GT0479 |
MLS001074172 |
AB00051931-17 |
AB00051931-18 |
BRD-K71799949-001-06-7 |
lexin |
g-32883 |
5-carbamyldibenzo(b,f)azepine |
biston |
g 32883 |
tegretol |
stazepine |
nsc169864 |
carbazepine |
finlepsin |
tegretal |
5h-dibenz[b,f]azepine-5-carboxamide |
carbamezepine |
neurotol |
nsc-169864 |
5-carbamyl-5h-dibenzo(b,f)azepine |
5-carbamoyl-5h-dibenz[b,f]azepine |
wln: t c676 bnj bvz |
5-carbamoyl-5h-dibenzo(b,f)azepine |
carbamazepen |
geigy 32883 |
5-carbamoyldibenzo(b,f)azepine |
karbamazepin |
MLS000069652 , |
DIVK1C_003750 |
DIVK1C_000388 |
KBIO1_000388 |
5h-dibenzo[b,f]azepine-5-carboxamide |
EU-0100292 |
carbamazepina [inn-spanish] |
carbatrol |
nsc 169864 |
telesmin |
brn 1246090 |
equetro |
timonil |
carbamazepinum [inn-latin] |
bipotrol |
hsdb 3019 |
tegretol-xr |
epitol |
amizepin |
einecs 206-062-7 |
CDS1_002710 |
SPECTRUM_000096 |
OPREA1_790775 |
PRESTWICK_104 |
cas-298-46-4 |
NCGC00015234-02 |
lopac-c-4024 |
NCGC00015234-01 |
BSPBIO_000203 |
PRESTWICK3_000052 |
PRESTWICK2_000052 |
SPECTRUM5_000936 |
CBCHROMO1_000350 |
LOPAC0_000292 |
BSPBIO_001929 |
CHEMDIV1_018966 |
NCGC00023877-03 |
BIM-0050280.0001 |
298-46-4 |
C06868 |
carbamazepine |
benzo[b][1]benzazepine-11-carboxamide |
carbamazepine, meets usp testing specifications |
5-carbamoyl-5h-dibenz(b,f)azepine |
5h-dibenz(b,f)azepine-5-carboxamide |
DB00564 |
carbamazepine (jp17/usp/inn) |
equetro (tn) |
D00252 |
tegretol (tn) |
CBZ , |
IDI1_000388 |
NCGC00023877-06 |
NCGC00023877-08 |
NCGC00023877-05 |
STK177357 |
smr000058201 |
KBIO2_005652 |
KBIOGR_000724 |
KBIO2_003084 |
KBIO2_000516 |
KBIO3_001149 |
KBIOSS_000516 |
SPBIO_000170 |
SPECTRUM2_000125 |
PRESTWICK1_000052 |
SPECTRUM4_000262 |
NINDS_000388 |
SPBIO_002124 |
PRESTWICK0_000052 |
SPECTRUM3_000325 |
SPECTRUM1500159 |
BPBIO1_000225 |
NCGC00023877-04 |
NCGC00015234-03 |
NCGC00023877-07 |
MLS001055475 |
smr001227191 |
carbamazepine anhydrous |
spd-417 |
tegretol cr |
trimonil |
neurotop retard |
carbamazepine, powder |
NCGC00015234-07 |
HMS2090M07 |
HMS2091O19 |
C 4024 |
carbamazepina |
carbamazepinum |
carnexiv |
CHEBI:3387 , |
carbamazepin |
NCGC00015234-13 |
stazepin |
sirtal |
carbamazepine extended release |
neurotop |
karbelex |
CHEMBL108 , |
HMS501D10 |
HMS640O02 |
HMS1568K05 |
HMS1920I17 |
bdbm50003659 |
dibenzo[b,f]azepine-5-carboxylic acid amide(carbamazepine) |
teril |
NCGC00015234-11 |
AKOS003235644 |
HMS3260L06 |
HMS3259B21 |
HMS2095K05 |
HMS3039K09 |
dibenzo[b,f]azepine-5-carboxamide |
tox21_300195 |
NCGC00259822-01 |
tox21_202273 |
NCGC00253982-01 |
2-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaene-2-carboxamide |
11-benzo[b][1]benzazepinecarboxamide |
A820074 |
nsc-755920 |
pharmakon1600-01500159 |
nsc755920 |
MLS002548877 |
dtxsid4022731 , |
tox21_110104 |
dtxcid902731 |
HMS2233G16 |
carbatrol extended-release |
carbamazepine [usan:usp:inn:ban:jan] |
33cm23913m , |
unii-33cm23913m |
CCG-38931 |
NCGC00015234-12 |
NCGC00015234-05 |
NCGC00015234-04 |
NCGC00015234-09 |
NCGC00015234-06 |
NCGC00015234-15 |
NCGC00015234-10 |
NCGC00015234-14 |
NCGC00015234-08 |
NCGC00015234-16 |
calepsin |
carbelan |
FT-0602927 |
LP00292 |
carbamazepine [jan] |
carbamazepinum [who-ip latin] |
carbamazepine [mart.] |
carbamazepine [ep monograph] |
carbamazepine [usp monograph] |
carbamazepine [who-dd] |
carbamazepine [usp impurity] |
carbamazepine [mi] |
carbamazepine [who-ip] |
carbamazepine [usp-rs] |
carbamazepine [inn] |
carbamazepine [hsdb] |
carbamazepine [vandf] |
carbamazepine [usan] |
carbamazepine [orange book] |
oxcarbazepine impurity a [ep impurity] |
EPITOPE ID:174842 |
S1693 |
HMS3372J13 |
gtpl5339 |
HY-B0246 |
NC00679 |
SCHEMBL21639 |
tox21_110104_1 |
NCGC00015234-19 |
KS-5146 |
NCGC00260977-01 |
tox21_500292 |
F0348-2551 |
Q-200792 |
carbamazepine, british pharmacopoeia (bp) reference standard |
5h-dibenz[b,f]azepine-5-carboxamine |
5h-dibenzo[b,f]azepine-5-carboxamide # |
5-carbomoyl-5h-dibenzo(b,f)azepine |
iminostilbene-n-carboxamide |
AB00051931_20 |
AB00051931_19 |
OPERA_ID_72 |
mfcd00005073 |
FT-0696814 |
AKOS025397243 |
5h-dibenzo[b,f]azepine-5-carboximidic acid |
STL453548 |
carbamazepine, european pharmacopoeia (ep) reference standard |
carbamazepine, analytical standard |
AC-9538 |
sr-01000000229 |
SR-01000000229-2 |
carbamazepine, united states pharmacopeia (usp) reference standard |
HMS3657G03 |
AC2074 |
2-azatricyclo[9.4.0.0,3,8]pentadeca-1(15),3,5,7,9,11,13-heptaene-2-carboxamide |
EN300-21678 |
carbamazepine, pharmaceutical secondary standard; certified reference material |
carbamazepine 1.0 mg/ml in methanol |
SR-01000000229-7 |
SR-01000000229-4 |
SBI-0050280.P004 |
carbmazepine |
HMS3712K05 |
SY002823 |
SCHEMBL19838283 |
SW220141-1 |
(z)-5h-dibenzo[b,f]azepine-5-carboxamide |
cbz;nsc 169864 |
BCP21380 |
5h-dibenzo[b,f]azepine-5-carboxamide;oxcarbazepine impurity a |
Q410412 |
5h-dibenz(b,f)azepine-5-carboxamide maleic acid |
carbamazepine host structure with oxalic acid removed |
carbamazepine host structure with maleic acid removed |
carbamazepine host structure with 4-hydroxybenzoic acid removed |
carbamazepine host structure with dl-tartaric acid removed |
5h-dibenz(b,f)azepine-5-carboxamide dl-tartaric acid |
5h-dibenz(b,f)azepine-5-carboxamide oxalic acid |
carbamazepine (carbatrol) |
n6w , |
SDCCGSBI-0050280.P005 |
NCGC00015234-33 |
HMS3747E03 |
dibenzo[b,f]azepine-5-carboxylic acid amide |
NCGC00015234-18 |
BC166161 |
Z104508594 |
5h-dibenzo(b,f)azepin-5-carboxamide |
carbamazepine er |
5h-dibenzo(b,f)azepine-5-carboxamide |
carbamazepina (inn-spanish) |
carbamazepineer |
carbamazepine (usp-rs) |
oxcarbazepine impurity a (ep impurity) |
carbamazepine (usp monograph) |
carbamazepine (usp impurity) |
carbamazepinum (inn-latin) |
tegretolxr |
carbamazepine (usan:usp:inn:ban:jan) |
carbamazepine (ep monograph) |
n03af01 |
carbamazepine (mart.) |
carbamazepine, 1mg/ml in methanol |
Carbamazepine (CBZ) is a widely used anticonvulsant with a low molecular weight that allows for extracorporeal removal of free drug by both dialytic and hemoperfusion techniques. It is used to treat epilepsy, bipolar disorder, trigeminal neuralgia and chronic pain.
Carbamazepine (CBZ) has a narrow therapeutic concentration range, and therapeutic drug monitoring (TDM) is necessary for its safe and effective individualized medication. It has a long history of successful use in epilepsy and has a safety profile that is well characterised.
Carbamazepine (CBZ) has been used successfully in the treatment of different movement disorders and was recently reported to be effective for nonhereditary chorea. It has been shown to induce several P450 cytochromes including CYP3A4 and CYP1A2.
Excerpt | Reference | Relevance |
---|---|---|
"Carbamazepine (CBZ) has a narrow therapeutic concentration range, and therapeutic drug monitoring (TDM) is necessary for its safe and effective individualized medication. " | ( A Rapid Therapeutic Drug Monitoring Strategy of Carbamazepine in Serum by Using Coffee-Ring Effect Assisted Surface-Enhanced Raman Spectroscopy. Li, D; Li, X; Lu, F; Yuan, Y; Zhao, Y; Zhu, Q, 2022) | 2.42 |
"Carbamazepine has a long history in psychiatry and neurology. " | ( Carbamazepine extended-release capsules: a new treatment option for bipolar I disorder. Weisler, RH, 2005) | 3.21 |
"Carbamazepine (CBZ) has a long history of successful use in epilepsy and, therefore, has a safety profile that is well characterised. " | ( Practical considerations for carbamazepine use in bipolar disorder. Dostrow, V; Fuller, MA; Gazda, TD; Gupta, S, 2006) | 2.07 |
"Carbamazepine has an important and still evolving place in the treatment of acute mania and long-term prophylaxis." | ( Thirty years of clinical experience with carbamazepine in the treatment of bipolar illness: principles and practice. Ballenger, JC; Ketter, TA; Post, RM; Uhde, T, 2007) | 1.33 |
"Carbamazepine has a unique spectrum of clinical efficacy in paroxysmal pain syndromes and epilepsy, as well as in affective illness. " | ( Biochemical effects of carbamazepine: relationship to its mechanisms of action in affective illness. Ballenger, JC; Gold, PW; Post, RM; Rubinow, DR; Uhde, TW, 1983) | 2.02 |
"Carbamazepine (CBZ) has a narrow therapeutic concentration range, and therapeutic drug monitoring (TDM) is necessary for its safe and effective individualized medication. " | ( A Rapid Therapeutic Drug Monitoring Strategy of Carbamazepine in Serum by Using Coffee-Ring Effect Assisted Surface-Enhanced Raman Spectroscopy. Li, D; Li, X; Lu, F; Yuan, Y; Zhao, Y; Zhu, Q, 2022) | 2.42 |
"Carbamazepine (CBZ) has been commonly implicated in SJS." | ( Combination of Steven-Johnson syndrome and neuroleptic malignant syndrome following carbamazepine therapy: a rare occurrence. Dubey, P; Gandhi, P; Panagariya, A; Sannegowda, RB; Sharma, B, 2013) | 1.34 |
"Carbamazepine (CBZ) has been reported as the most common culprit drug for Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) in several Asian countries including Thailand. " | ( Association between HLA-B*1502 and carbamazepine-induced severe cutaneous adverse drug reactions in a Thai population. Aungaree, T; Auvichayapat, N; Chen, P; Chen, WH; Choonhakarn, C; Jantararoungtong, T; Khunarkornsiri, U; Konyoung, P; Kulkantrakorn, K; Lin, SY; Pavakul, K; Phonhiamhan, S; Piyatrakul, N; Pongpakdee, S; Tassaneeyakul, W; Tiamkao, S; Yodnopaglaw, P, 2010) | 2.08 |
"Carbamazepine has demonstrated safety, tolerability and efficacy in treatment of moderate to severe symptoms of alcohol withdrawal in the inpatient setting. " | ( The role of carbamazepine and oxcarbazepine in alcohol withdrawal syndrome. Barrons, R; Roberts, N, 2010) | 2.18 |
"As carbamazepine has shown antinociceptive properties in a variety of experimental and clinical settings, in the present study, we evaluated its potential antiallodynic effects on postoperative pain in naïve and morphine-dependent rats." | ( Carbamazepine potentiates morphine analgesia on postoperative pain in morphine-dependent rats. Moini Zanjani, T; Naseri, K; Sabetkasaei, M; Saghaei, E, 2012) | 2.34 |
"Carbamazepine (CBZ) has been used in the treatment of bipolar disorder, both in acute mania and maintenance therapy, since the early 1970s. " | ( Carbamazepine treatment of bipolar disorder: a retrospective evaluation of naturalistic long-term outcomes. Chen, CH; Lin, SK, 2012) | 3.26 |
"Carbamazepine which has been used as an anticonvulsivant for many years, has more recently been advocated for the control of aggressive behavior in epileptic and non epileptic populations. " | ( [Carbamazepine and aggressive behavior: a review]. Colonna, L; Thibaut, F, ) | 2.48 |
"Carbamazepine has been reported to exacerbate seizures in children with primary generalized epilepsy and epilepsy with mixed seizure types. " | ( Carbamazepine-induced seizures: a case report and review of the literature. Alsaadi, TM; Gansaeuer, M, 2002) | 3.2 |
"Carbamazepine has shown reasonable antimanic properties, but its use has been limited because of enzyme-inducing effects. " | ( Acute antimanic efficacy and safety of oxcarbazepine in an open trial with an on-off-on design. Amann, B; Dittmann, S; Frye, MA; Grunze, H; Hummel, B; Schaefer, M; Stampfer, R; Sterr, A; Walden, J, 2002) | 1.76 |
"Carbamazepine has been used to treat mania for over 2 decades. " | ( A multicenter, randomized, double-blind, placebo-controlled trial of extended-release carbamazepine capsules as monotherapy for bipolar disorder patients with manic or mixed episodes. Kalali, AH; Ketter, TA; Weisler, RH, 2004) | 1.99 |
"Carbamazepine has not been shown to be more effective than lithium or valproate, and it can cause serious adverse effects." | ( Extended-release carbamazepine (Equetro) for bipolar disorder. , 2005) | 1.39 |
"Carbamazepine has also been shown to induce the hepatic synthesis of sex hormone-binding globulin, thus reducing free serum testosterone levels and possibly causing erectile dysfunction (ED) in some men; these effects have not been observed with oxcarbazepine." | ( Amelioration of erectile dysfunction following a switch from carbamazepine to oxcarbazepine: recent clinical experience. Sachdeo, R; Sathyan, RR, 2005) | 1.29 |
"Carbamazepine has a long history in psychiatry and neurology. " | ( Carbamazepine extended-release capsules: a new treatment option for bipolar I disorder. Weisler, RH, 2005) | 3.21 |
"Carbamazepine (CBZ) has a long history of successful use in epilepsy and, therefore, has a safety profile that is well characterised. " | ( Practical considerations for carbamazepine use in bipolar disorder. Dostrow, V; Fuller, MA; Gazda, TD; Gupta, S, 2006) | 2.07 |
"Carbamazepine has shown rather modest benefit in reducing withdrawal severity, although it did significantly improve drug-free outcome." | ( Pharmacological interventions for benzodiazepine mono-dependence management in outpatient settings. Auriacombe, M; Denis, C; Fatséas, M; Lavie, E, 2006) | 1.06 |
"Carbamazepine has been shown to be very persistent in sewage treatment, as well as ground water." | ( Sorption-desorption of carbamazepine from irrigated soils. Adamsen, FJ; Williams, CF, ) | 1.16 |
"Carbamazepine, which has been used as an anti-epileptic drug in clinic for many years, is currently recognized as a histone deacetylase inhibitor (HDI), most of which showed anti-tumor characteristics. " | ( [Inhibitory effect of carbamazepine on proliferation of estrogen-dependent breast cancer cells]. Cai, L; Meng, QW; Sui, GJ; Sun, LC; Xi, YH; Zhao, CH, 2006) | 2.09 |
"Carbamazepine has an important and still evolving place in the treatment of acute mania and long-term prophylaxis." | ( Thirty years of clinical experience with carbamazepine in the treatment of bipolar illness: principles and practice. Ballenger, JC; Ketter, TA; Post, RM; Uhde, T, 2007) | 1.33 |
"Carbamazepine has proven to be both efficacious and safe in the treatment of this condition." | ( [Sydenham's chorea: report of a case treated with carbamazepine with excellent clinical response]. Cabacas García, A; García González, MM; Mayol Canals, L; Vázquez Ruiz, M; Villalobos Arévalo, P, 2007) | 1.31 |
"Carbamazepine, which has been used in the treatments of epilepsy, is often found in the environment. " | ( Identification of fungal metabolites of anticonvulsant drug carbamazepine. Hur, HG; Kang, SI; Kang, SY, 2008) | 2.03 |
"Carbamazepine has a unique spectrum of clinical efficacy in paroxysmal pain syndromes and epilepsy, as well as in affective illness. " | ( Biochemical effects of carbamazepine: relationship to its mechanisms of action in affective illness. Ballenger, JC; Gold, PW; Post, RM; Rubinow, DR; Uhde, TW, 1983) | 2.02 |
"Carbamazepine has recently been reported to have therapeutic potential in mania. " | ( Carbamazepine and haloperidol v placebo and haloperidol in excited psychoses. A controlled study. Belmaker, RH; Bental, E; Klein, E; Lerer, B, 1984) | 3.15 |
"Carbamazepine has been used in the treatment of temporal lobe epilepsy since 1963. " | ( Carbamazepine in the treatment of aggressive behavior in schizophrenic patients: a case report. Dupont, D; Yassa, R, 1983) | 3.15 |
"Carbamazepine has this characteristic common with antidepressant drugs." | ( Behavioral effects of carbamazepine after single and repeated administration in emotionally labile subjects. Ehrhardt, KJ; Janke, W; Münch, U, 1983) | 1.3 |
"Carbamazepine serum levels have been determined by gas-liquid chromatography in 24 children and 26 adults with epilepsy on chronic carbamazepine treatment. " | ( Dose-dependency of the ratio between carbamazepine serum level and dosage in patients with epilepsy. Kumps, AH, 1981) | 1.98 |
"CBZ (Carbamazepine) blood levels have been detected in a heterogeneous group of epileptic patients taking several other antiepileptic drugs." | ( [Clinicopharmacologic study of blood carbamazepine levels in a group of epileptic patients]. Ermani, M; Giaretta, D; Paleari, C; Pellegrini, A; Testa, G, ) | 0.86 |
"Carbamazepine (CBZ) has been used in the treatment of alcohol withdrawal (AW). " | ( Prolonged treatment with carbamazepine increases the stimulatory effects of ethanol in mice. Andreatini, R; Camarini, R; Monteiro, MG, ) | 1.88 |
"Carbamazepine has been reported to decrease agitation associated with various psychiatric disorders and to reduce neuroleptic side effects." | ( Effect of carbamazepine on agitation in Alzheimer's inpatients refractory to neuroleptics. Lemke, MR, 1995) | 1.41 |
"Carbamazepine (CBZ) has been successfully employed in a variety of neurological and psychiatric disorders. " | ( Signs and symptoms of carbamazepine overdose. Schmidt, S; Schmitz-Buhl, M, 1995) | 2.05 |
"Carbamazepine has no effect on the EEG, in epilepsies with atypical course (atypical benign partial epilepsy, Landau-Kleffner syndrome, epilepsy with continuous spikes and waves during slow sleep [CSWS]) carbamazepine usually has no effect either on the seizures or on the EEG, on the contrary, in some cases both may even get worse." | ( Treatment of "benign" partial epilepsies of childhood, including atypical forms. Gross-Selbeck, G, 1995) | 1.01 |
"Carbamazepine (CBZ) has been reported to exacerbate some seizure types in children. " | ( EEG changes and seizure exacerbation in young children treated with carbamazepine. Arora, MS; Sher, PK; Talwar, D, ) | 1.81 |
"Carbamazepine (CBZ) has been reported to have an antidiuretic action, though it is not known how it produces this effect. " | ( Fluid retention and cardiomegaly associated with carbamazepine in an epileptic child. Atalay, S; Gürer, YK; Karademir, S; Oner, A, 1993) | 1.98 |
"Carbamazepine has selectively relieved the tic douloureux, while lithium has completely controlled the cluster headache." | ( Relief of cluster-tic syndrome by the combination of lithium and carbamazepine. Berciano, J; Pascual, J, 1993) | 1.25 |
"Carbamazepine has been used in adults and children for over 30 years. " | ( Treatment of neonatal seizures with carbamazepine. al Hifzi, I; Khan, M; Majeed-Saidan, M; Singh, B; Singh, P, 1996) | 2.01 |
"Carbamazepine has been shown to induce several P450 cytochromes including CYP3A4 and CYP1A2. " | ( A pharmacokinetic interaction between carbamazepine and olanzapine: observations on possible mechanism. Bergstrom, RF; Gilfillan, DJ; Lucas, RA, 1998) | 2.01 |
"Carbamazepine (CBZ) has been widely used for treatment of manic states. " | ( Carbamazepine suppresses methamphetamine-induced Fos expression in a regionally specific manner in the rat brain. Possible neural substrates responsible for antimanic effects of mood stabilizers. Fujiwara, Y; Hamamura, T; Kuroda, S; Lee, Y; Miki, M; Ohashi, K, 2000) | 3.19 |
"Carbamazepine has been used successfully in the treatment of different movement disorders and was recently reported to be effective for nonhereditary chorea. " | ( Successful treatment of rheumatic chorea with carbamazepine. Amir, J; Harel, L; Straussberg, R; Volovitz, B; Zecharia, A, 2000) | 2.01 |
"Carbamazepine (CBZ) has been extensively used in the treatment of epilepsy, as well as in the treatment of neuropathic pain and affective disorders. " | ( Mechanisms of action of carbamazepine and its derivatives, oxcarbazepine, BIA 2-093, and BIA 2-024. Ambrósio, AF; Carvalho, AP; Carvalho, CM; Soares-Da-Silva, P, 2002) | 2.06 |
"Carbamazepine has been found to crystallize as a new polymorph that is stable at room temperature. " | ( Form IV of carbamazepine. Kampf, JW; Lang, M; Matzger, AJ, 2002) | 2.15 |
"Carbamazepine (CBZ) has shown contradictory results and in a previous study, our results were negative." | ( Effects of carbamazepine on dexamethasone suppression and sleep electroencephalography in borderline personality disorder. Bobes, J; De la Fuente, JM; Mendlewicz, J; Vizuete, C, 2002) | 1.43 |
"Oral carbamazepine has been shown to have antidiuretic activity in seven out of nine patients with neurohypophyseal diabetes insipidus. " | ( Treatment of diabetes insipidus with carbamazepine. Wales, JK, 1975) | 1.04 |
"Carbamazepine has been reported to decrease urine output and increase urinary concentration in patients with diabetes insipidus. " | ( Effects of carbamazepine on the water permeability and short-circuit current of the urinary bladder of the toad and the response to vasopressin, adenosine 3',5'-cyclic phosphate and theophylline. Meier, KE; Mendoza, SA, 1977) | 2.09 |
"Carbamazepine has recently been introduced for the treatment of generalized tonic-clonic and partial seizures." | ( Recent advances in drug therapy for epilepsy. Bruni, J, 1979) | 0.98 |
"Carbamazepine (CBZ) has become a commonly used antiepileptic agent in the pediatric population. " | ( Carbamazepine dosing for pediatric seizure disorders: the highs and lows. Gilman, JT, 1991) | 3.17 |
"2. Carbamazepine has useful sedating, antianxiety, and antidepressant properties that make it an effective treatment for manic psychosis." | ( Carbamazepine treatment of psychosis. Implications for patient welfare and nursing practice. Del Medico, VJ; Dilsaver, SC; Norris, AE, 1990) | 2.24 |
"Carbamazepine has been found to be relatively free of such effects, and would be an optimum alternative if seizure control were comparable." | ( Carbamazepine replacement of phenytoin, phenobarbital and primidone in a rehabilitation setting: effects on seizure control. Glenn, MB; Singer, WD; Whyte, J; Wroblewski, BA, ) | 2.3 |
"Carbamazepine (CBMZP) has been implicated as an inhibitor of the activities of 5-aminolaevulinic acid dehydratase (ALA-D) and uroporphyrinogen I synthetase (URO-S). " | ( Protoporphyrinaemia and decreased activities of 5-aminolevulinic acid dehydrase and uroporphyrinogen I synthetase in erythrocytes of a Vitamin B6-deficient epileptic boy given valproic acid and carbamazepine. Carson, R; Haust, HL; Peter, F; Poon, HC; VanDeWetering, C, 1989) | 1.91 |
"Carbamazepine has been reported to decrease symptoms in patients with aggression, dyscontrol syndromes, schizophrenia, and alcohol withdrawal syndrome, but few of these studies have been controlled, comparative trials; carbamazepine may be useful in patients with these disorders who do not respond to conventional therapies." | ( Use of carbamazepine in psychiatric disorders. Birkhimer, LJ; Curtis, JL; Jann, MW, ) | 1.31 |
"Carbamazepine, in contrast, has rather a stimulatory action." | ( [Modification of psychophysical performance of the human by anticonvulsants]. Meyer, FP; Walther, H, 1987) | 0.99 |
"Carbamazepine has been utilized both as an anticonvulsant and as a psychotropic drug for the treatment of complex partial seizures and various mood and other emotional disorders such as the episodic dyscontrol syndrome. " | ( Carbamazepine regulates feline aggression elicited from the midbrain periaqueductal gray. Edinger, HM; Shaikh, MB; Siegel, A, 1988) | 3.16 |
"Carbamazepine has been shown to enhance dopaminergic agonist behavioral effects, but not to displace [3H]spiroperidol binding. " | ( Effect of carbamazepine on dopamine release and reuptake in rat striatal slices. Barros, HM; Braz, S; Leite, JR, ) | 1.98 |
"Carbamazepine has been shown to have complex actions on multiple neurotransmitter and neuromodulator systems, and it is possible that paradoxical effects of this nature may occur in susceptible individuals, as has been found with other sedative and anticonvulsant agents." | ( Manic state with carbamazepine therapy of seizures. Drake, ME; Peruzzi, WT, 1986) | 1.33 |
Carbamazepine can produce hydrophobic interactions to affect the phospholipid bilayer and work on specific proteins to disfunction the cell membrane. It is known to produce the side effect of euphoria.
Excerpt | Reference | Relevance |
---|---|---|
"Carbamazepine may cause clinical effects such as dizziness and nystagmus. " | ( Assessment of vestibulo-ocular reflex with video head impulse test in epilepsy patients undergoing carbamazepine monotherapy. Adiguzel, A; Demir, I, 2023) | 2.57 |
"Carbamazepine can cause hypersensitivity reactions in ~10% of patients. " | ( Evaluation of clinical and genetic factors in the population pharmacokinetics of carbamazepine. Carr, DF; Maggs, JL; Marson, AG; Meng, X; Park, BK; Pertinez, H; Pirmohamed, M; Yip, VLM, 2021) | 2.29 |
"Carbamazepine can produce hydrophobic interactions to affect the phospholipid bilayer and work on specific proteins to disfunction the cell membrane." | ( Molecular toxicity of triclosan and carbamazepine to green algae Chlorococcum sp.: A single cell view using synchrotron-based Fourier transform infrared spectromicroscopy. An, C; Chen, X; Huang, G; Liu, X; Weger, H; Xin, X; Yao, Y; Zhang, P, 2017) | 1.45 |
"Carbamazepine is known to produce the side effect of euphoria. " | ( A Clinical Study of Toxication Caused by Carbamazepine Abuse in Adolescents. Chen, YL; Li, JJ; Liu, CF; Wang, LJ; Xu, W; Zhao, Y, 2018) | 2.19 |
"Carbamazepine alone did not increase neurodegeneration when given in doses up to 50 mg/kg, but it induced significant cell death at 100 mg/kg." | ( Antiepileptic drug-induced neuronal cell death in the immature brain: effects of carbamazepine, topiramate, and levetiracetam as monotherapy versus polytherapy. Gale, K; Kim, J; Kondratyev, A, 2007) | 1.29 |
"Carbamazepine did not inhibit the specific binding of [125I]triiodothyronine into the nuclei of intact fibroblasts, suggesting that it does not interact with thyroid hormone receptors in this system and is unlikely to do so in vivo." | ( Carbamazepine does not interact with thyroid hormone receptors in human fibroblasts. Eil, C; Joffe, RT; Post, RM, 1984) | 2.43 |
"Carbamazepine was of lower potency (Ki = 112 microM) as an inhibitor of the binding of the putative A2 adenosine agonist [3H]5'-N-ethylcarboxamidoadenosine." | ( Interactions of the anticonvulsant carbamazepine with adenosine receptors. 1. Neurochemical studies. Davies, LP; Johnston, GA; Skerritt, JH, 1983) | 1.26 |
"Carbamazepine does not inhibit cocaine-induced motor activity or the development of behavioral sensitization in the rat." | ( Differential effects of carbamazepine and lithium on sensitization and kindling. Pert, A; Post, RM; Weiss, SR, 1984) | 1.3 |
"Carbamazepine (C) can cause a characteristic hypersensitivity reaction (CHS¿. " | ( [Carbamazepine hypersensitivity symptoms]. Ivry, S; Shteinmintz, D; Tabenkin, H, 2000) | 2.66 |
"Carbamazepine (CBZ) can produce serious side-effects such as hepatitis, LES, agranulocytosis, aplastic anaemia and skin eruptions. " | ( [Skin rash induced by carbamazepine. Description of 2 clinical cases]. Azzini, M; Garavelli, PL, ) | 1.89 |
"The carbamazepine induced increase in brain adenosine receptors in all these areas persisted unabated at 1 and 5 days as well as 2, 4, and 8 weeks following termination of carbamazepine treatment, suggesting a relatively permanent alteration of the adenosine receptor by this drug." | ( Persistent upregulation of brain adenosine receptors in response to chronic carbamazepine treatment. Marangos, PJ; Montgomery, P; Patel, J; Post, RM; Weiss, SR, 1987) | 0.98 |
"Carbamazepine was found to cause statistically significant, but clinically insubstantial, decreases in white blood cell indexes." | ( Hematological effects of carbamazepine in patients with affective illness. Joffe, RT; Post, RM; Roy-Byrne, PP; Uhde, TW, 1985) | 1.29 |
Carbamazepine treatment could delay the disease onset and extend life span of SOD1-G93A mice by about 14.5% and 13.9%, respectively. Carbamazepines is a protective factor against uncontrolled seizures for EAF.
We evaluated the efficacy, development of adverse effects, and possible correlation between the plasma concentration of carbamazepine (CBZ) and its major metabolite, carbamazepsine-10,11-epoxide (CBZE) In a group of epileptic patients in whom selective increases in CBZ doses were made, four out of the seven patients developed moderate-t.
The influence of progabide, a new antiepileptic drug, on the pharmacokinetic profiles of phenobarbital, phenytoin, carbamazepine, and valproic acid was evaluated.
The study investigated the neuronal protective effect of SXC combined with carbamazepine (CBZ) on epilepsy and cognitive impairment in kainic acid-kindled SD rats.
Excerpt | Reference | Relevance |
---|---|---|
" The animals were given either CBZ alone or in combination with diltiazem and plasma samples were collected at different time intervals." | ( Elevation of carbamazepine plasma levels by diltiazem in rabbits: a potentially important drug interaction. al-Humayyd, MS, 1990) | 0.65 |
"To assess the roles of substance P in neurologic or psychiatric illnesses, effects of acute or chronic (40- or 80-day dietary) treatment with trihexyphenidyl and carbamazepine alone or in combination with haloperidol on substance P content were investigated in the rat brain." | ( Effects of chronic treatment with trihexyphenidyl and carbamazepine alone or in combination with haloperidol on substance P content in rat brain: a possible implication of substance P in affective disorders. Mataga, N; Mitsushio, H; Takashima, M; Toru, M, 1988) | 0.72 |
" Serum triiodothyronine (T3) and T4 by radioimmunoassay showed that PTU alone and in combination with Li lowered serum T4, while a high level of T4 by its supplement was suppressed by co-administration of Li." | ( Effect of lithium carbonate administration singly or in combination with some psychotropic drugs on the radioiodide uptake by mouse thyroid. Akamatsu, S; Kamata, N; Kawada, J; Kurata, M; Kuwae, T; Minakuchi, K; Nishida, M; Takasugi, M; Teraoka, K, 1989) | 0.28 |
" Purely additive interactions were found for the anticonvulsant effect when valproate was combined with carbamazepine as well as with phenobarbital." | ( Anticonvulsant potency and neurotoxicity of valproate alone and in combination with carbamazepine or phenobarbital. Bourgeois, BF, 1988) | 0.71 |
" Drug-drug interactions with carbamazepine include several types." | ( Clinically significant carbamazepine drug interactions: an overview. Pippenger, CE, 1987) | 0.87 |
" However, its apparent synergism with carbamazepine and phenytoin combined with its low incidence of serious side effects make baclofen a valuable adjunct in the treatment of refractory trigeminal neuralgia." | ( Treatment of trigeminal neuralgia: use of baclofen in combination with carbamazepine. Baker, KA; Lilly, GE; Taylor, JW, ) | 0.64 |
" Phenytoin in combination with other drugs (anticonvulsives, antibiotics etc." | ( [Effects of drug interaction in infancy (author's transl)]. Alterthum, K; Bauer, P; Stünkel, S; Windorfer, A, 1980) | 0.26 |
"Steady state carbamazepine (CBZ) plasma concentrations were similar in 15 epileptics receiving monotherapy and in 24 patients taking CBZ in combination with one other anticonvulsant." | ( Carbamazepine 10, 11 epoxide concentrations in epileptics on carbamazepine alone and in combination with other anticonvulsants. Brodie, MJ; Forrest, G; Rapeport, WG, 1983) | 2.08 |
"Valproic acid undergoes drug-drug interactions with most of the commonly used anticonvulsants." | ( Drug interactions with valproic acid. Koch, KM; Levy, RH, 1982) | 0.26 |
" Brief information on the following reports of drug-drug interactions is given in this article with the intention of giving these reports wider publicity and, possibly, encouraging further observation and research to establish or disprove their validity in a larger and wider range of patients or volunteer subjects." | ( Early reports on drug interactions. D'Arcy, PF, 1983) | 0.27 |
" It is often necessary to have lithium combined with other psychopharmacological agents when efforts are aimed at either enhancing a less-than-optimal therapeutic effect or treating other symptoms as well." | ( [Drug combinations of lithium: reasons and limitations]. Lagomarsino, AJ, 1993) | 0.29 |
" Monitering of BUP and its metabolites may ultimately prove useful in guiding clinicians dosing decisions, especially when mood stabilizers are combined with other psychotropic drugs in refractory bipolar patients." | ( Bupropion and anticonvulsant drug interactions. Lamparella, V; Masand, PS; Popli, AP; Tanquary, J, 1995) | 0.29 |
"2 years, 1,594 (31%) had at least one interacting drug combination according to the Swedish National Formulary." | ( Potential drug--drug interactions in 5,125 mostly elderly out-patients in Gothenburg, Sweden. Bergendal, L; Friberg, A; Schaffrath, A, 1995) | 0.29 |
" Because of its widespread and long term use, carbamazepine is frequently prescribed in combination with other drugs, leading to the possibility of drug interactions." | ( Clinically significant pharmacokinetic drug interactions with carbamazepine. An update. Perucca, E; Pisani, F; Spina, E, 1996) | 0.79 |
" Patients received phenobarbitone as monotherapy or in combination with either of the antiepileptic drugs carbamazepine or valproic acid." | ( Detection of a drug-drug interaction on population-based phenobarbitone clearance using nonlinear mixed-effects modeling. Aoyama, T; Higuchi, S; Ohdo, S; To, H; Yukawa, E, 1998) | 0.51 |
" There were no statistically significant differences in carbamazepine, carbamazepine epoxide, and phenytoin pharmacokinetic parameters when either drug was administered alone or in combination with tiagabine." | ( Lack of pharmacokinetic drug interactions between tiagabine and carbamazepine or phenytoin. Boellner, SW; Cao, GX; Cato, A; Guenther, HJ; Gustavson, LE; Qian, JX; Sommerville, KW, 1998) | 0.79 |
" Subjects were treated with carbamazepine combined with placebo for 21 days and subsequently with carbamazepine combined with mirtazapine for another 7 days (Study A) or with mirtazapine combined with placebo for 7 days and subsequently mirtazapine combined with carbamazepine for another 21 days (Study B)." | ( Drug-drug interaction studies with mirtazapine and carbamazepine in healthy male subjects. Maris, F; Sitsen, J; Timmer, C, ) | 0.68 |
" Other agents frequently used as mood stabilizers in monotherapy and in combination with lithium are valproate and carbamazepine." | ( Drug interactions of lithium and other antimanic/mood-stabilizing medications. Dunner, DL, 2003) | 0.53 |
"Our objective was to evaluate the drug-drug interactions of oxcarbazepine with coadministered antiepileptic drugs in children." | ( Pharmacokinetic drug interactions in children taking oxcarbazepine. D'souza, J; Hossain, M; Milosavljev, S; Sallas, WM, 2003) | 0.32 |
" Carbamazepine, phenobarbital, or phenytoin administered with oxcarbazepine increased the apparent clearance of 10-monohydroxy metabolite by 31% to 35%, whereas carbamazepine levels decreased by 15% and phenobarbital levels increased by 14%." | ( Pharmacokinetic drug interactions in children taking oxcarbazepine. D'souza, J; Hossain, M; Milosavljev, S; Sallas, WM, 2003) | 1.23 |
"This study was aimed at evaluating the body temperature of mice following the injection of LY 300164, an AMPA/kainate receptor antagonist, alone or in combination with carbamazepine or diphenylhydantoin." | ( Influence of LY 300164 alone or in combination with carbamazepine or diphenylhydantoin on the body temperature in mice. Czuczwar, SJ; Luszczki, JJ; Swiader, MJ; Wierzchowska-Cioch, E; Zwolan, A, 2004) | 0.77 |
" Patients received PGB, 600 mg/day (200 mg q8h) for 7 days, in combination with their individualized maintenance monotherapy with valproate (VPA), phenytoin (PHT), lamotrigine (LTG), or carbamazepine (CBZ)." | ( Pregabalin drug interaction studies: lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and valproate in patients with partial epilepsy. Alvey, CW; Bockbrader, HN; Brodie, MJ; Bron, NJ; Gibson, GL; Hounslow, NJ; Posvar, EL; Randinitis, EJ; Wesche, DL; Wilson, EA, 2005) | 0.75 |
" PGB may be added to VPA, LTG, PHT, or CBZ therapy without concern for pharmacokinetic drug-drug interactions." | ( Pregabalin drug interaction studies: lack of effect on the pharmacokinetics of carbamazepine, phenytoin, lamotrigine, and valproate in patients with partial epilepsy. Alvey, CW; Bockbrader, HN; Brodie, MJ; Bron, NJ; Gibson, GL; Hounslow, NJ; Posvar, EL; Randinitis, EJ; Wesche, DL; Wilson, EA, 2005) | 0.56 |
" Drug-drug interactions (DDIs) caused by induction of CYP3A4 can result in decreased exposure to coadministered drugs, with potential loss of efficacy." | ( Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction. de Morais, SM; Fahmi, OA; Liras, JL; Maurer, TS; Mills, JB; Ripp, SL; Trevena, KA, 2006) | 0.33 |
" Variables included in the analysis were age, gender, and concomitant treatment with a total of 41 drugs most often used in combination with quetiapine." | ( Quetiapine and drug interactions: evidence from a routine therapeutic drug monitoring service. Castberg, I; Skogvoll, E; Spigset, O, 2007) | 0.34 |
" On the basis of our data and pharmacokinetic considerations, the majority of drugs commonly used in psychiatry can safely be given in combination with quetiapine." | ( Quetiapine and drug interactions: evidence from a routine therapeutic drug monitoring service. Castberg, I; Skogvoll, E; Spigset, O, 2007) | 0.34 |
"In patients receiving carbamazepine alone or in combination with other drugs, administration of clarithromycin led to a transitory overdosage (ataxia, dizziness, diplopia, nausea, vomiting, drowsiness)." | ( [Carbamazepine and clarithromycin: a clinically relevant drug interaction]. Coubes, P; Crespel, A; Gélisse, P; Halaili, E; Hillaire-Buys, D; Jean-Pastor, MJ; Vespignan, H, 2007) | 1.56 |
"The present study describes a new analytical approach for the detection and characterization of chemically reactive metabolites using glutathione ethyl ester (GSH-EE) as the trapping agent in combination with hybrid triple quadrupole linear ion trap mass spectrometry." | ( Screening and characterization of reactive metabolites using glutathione ethyl ester in combination with Q-trap mass spectrometry. Fitch, WL; Wen, B, 2009) | 0.35 |
"Our results showed that the efficacy of carbamazepine combined with Flunarizine Hydrochloride is similar to that of the control group." | ( [Efficacy of carbamazepine combined with flunarizine hydrochloride for treating tinnitus]. Kong, X; Li, N; Ma, F; Xin, Y; Zhao, Y, 2008) | 0.98 |
" Pharmacokinetic parameters were measured, including dose and trough blood levels (C(0)), area under the serum concentration-time curve from 0 to 12 hours (AUC(0-12h)), and apparent clearance of oral FK506 (CL/F) for FK506 alone (about 3 months before starting CBZ) and combined with CBZ (11 days and about 3 months after starting CBZ)." | ( Drug interaction between tacrolimus and carbamazepine in a Japanese heart transplant recipient: a case report. Kato, TS; Komamura, K; Kotake, T; Mano, A; Morishita, H; Nakatani, T; Ochi, H; Oda, N; Okada, H; Sakai, M; Takada, M; Wada, K, 2009) | 0.62 |
" Food and Drug Administration draft drug interaction guidance as CYP3A4 inducers for clinical drug-drug interaction (DDI) studies." | ( Simulation of clinical drug-drug interactions from hepatocyte CYP3A4 induction data and its potential utility in trial designs. Hayashi, M; Shou, M; Skiles, GL; Xu, Y; Zhou, Y, 2011) | 0.37 |
" The analytical method utilized pressurized liquid extraction (PLE) combined with silica gel cleanup, gel permeation chromatography, and gas chromatography ion-trap tandem mass spectrometry." | ( Simultaneous analysis of select pharmaceuticals and personal care products in fish tissue using pressurized liquid extraction combined with silica gel cleanup. Chambliss, CK; Mottaleb, MA; Subedi, B; Usenko, S, 2011) | 0.37 |
" To demonstrate a case of a 15 year old girl suffering from refractory epilepsy with underlying focal cortical dysplasia (FCD), whose seizure deterioration was most probably associated with drug-drug interactions between prescribed common antiepileptic drugs, namely valproic acid, phenobarbital or the prodrug primidon and carbamazepine." | ( Antiepleptic drug interactions: a clinical case demonstration. Klapková, E; Komárek, V; Tesfaye, H; Tesfayeová, A, 2011) | 0.54 |
" When prescribing these drugs to patients of this age bracket, treatment should be based not only on the diagnosis and seizure type but also on the propensity of the drugs for adverse effects and their drug-drug interactions." | ( Choice of antiepileptic drugs for the elderly: possible drug interactions and adverse effects. Dostic, M; Jankovic, SM, 2012) | 0.38 |
"This article reviews antiepileptic drugs currently used for treating the elderly and highlights the adverse effects and potential drug-drug interactions for these treatments." | ( Choice of antiepileptic drugs for the elderly: possible drug interactions and adverse effects. Dostic, M; Jankovic, SM, 2012) | 0.38 |
" While the majority of antiepileptic drugs interact with other drugs, hepatic enzymes and plasma proteins, a few newer antiepileptic drugs are free from such interactions (e." | ( Choice of antiepileptic drugs for the elderly: possible drug interactions and adverse effects. Dostic, M; Jankovic, SM, 2012) | 0.38 |
" The cases were categorized into OXC monotherapy (n = 78), OXC in combination with EIAED (n = 73), and OXC in combination with non-EIAED (n = 103)." | ( Drug interaction and pharmacokinetic modeling of oxcarbazepine in korean patients with epilepsy. Hong, SB; Huh, W; Joo, EY; Kim, JR; Kim, SR; Ko, JW; Lee, SY; Park, KJ; Seo, DW, ) | 0.13 |
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions." | ( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012) | 0.38 |
"This paper describes the determination of carbamazepine (CBZ) in human plasma using ion chromatography combined with online electrochemical derivatization and fluorescence detection." | ( Ion chromatography combined with online electrochemical derivatization and fluorescence detection for the determination of carbamazepine in human plasma. Chen, D; Li, L; Subhani, Q; Wu, S; Xu, W; Yang, B; Zhu, Y, 2012) | 0.85 |
" In the treatment group, 30 patients were administered with local intramuscular injections of botulinum toxin A and oral carbamazepine 100 mg/time, 3 times a day for 60 days." | ( Efficacy of carbamazepine combined with botulinum toxin a in the treatment of blepharospasm and hemifacial spasm. Hong, YC; Hu, YF; Li, XH; Lin, SC; Liu, JB; Liu, LY, 2012) | 0.97 |
" While grapefruit juice has been extensively studied with respect to its drug-drug interaction potential, numerous other fruit juices such as cranberry juice, orange juice, grape juice, pineapple juice and pomegranate juice have also been investigated for its potential to show drug-drug interaction of any clinical relevance." | ( Is pomegranate juice a potential perpetrator of clinical drug-drug interactions? Review of the in vitro, preclinical and clinical evidence. Srinivas, NR, 2013) | 0.39 |
" For patients who used CBZ in combination with an enzyme-inducing antiepileptic drug (AED: PHT or PB), individuals carrying the CYP3A5*1 allele (CYP3A5 expressers) showed a trend of having higher CBZ clearance and lower dose-adjusted CBZ level as compared to individuals carrying the CYP3A5*3 allele, even though no statistical significance was recorded." | ( Effect of CYP3A5 genotypes on the pharmacokinetics of carbamazepine when used as monotherapy or co-administered with phenytoin, phenobarbital or valproic acid in Thai patients. Panomvana, D; Towanabut, S; Traiyawong, T, 2013) | 0.64 |
"When CBZ was used in combination with enzyme-inducing AED, CYP3A5 expressers yielded a trend toward greater susceptibility to change in CBZ clearance and showed lower dose-adjusted CBZ levels compared to CYP3A5 non-expressers." | ( Effect of CYP3A5 genotypes on the pharmacokinetics of carbamazepine when used as monotherapy or co-administered with phenytoin, phenobarbital or valproic acid in Thai patients. Panomvana, D; Towanabut, S; Traiyawong, T, 2013) | 0.64 |
" Little is known about pomalidomide's potential for drug-drug interactions (DDIs); as pomalidomide clearance includes hydrolysis and cytochrome P450 (CYP450)-mediated hydroxylation, possible DDIs via CYP450 and drug-transporter proteins were investigated in vitro and in a clinical study." | ( Pomalidomide: evaluation of cytochrome P450 and transporter-mediated drug-drug interaction potential in vitro and in healthy subjects. Assaf, M; Hoffmann, M; Kasserra, C; Kumar, G; Li, Y; Liu, L; Palmisano, M; Wang, X, 2015) | 0.42 |
" This study was designed to evaluate the bidirectional carbamazepine-armodafinil pharmacokinetic drug-drug interaction." | ( Evaluation of the potential for pharmacokinetic drug-drug interaction between armodafinil and carbamazepine in healthy adults. Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015) | 0.88 |
" Preferred binding of PGS at the allosteric site and a stronger preference for CBZ binding at the productive site give rise to a nontrivial drug-drug interaction." | ( Mechanism of drug-drug interactions mediated by human cytochrome P450 CYP3A4 monomer. Baylon, JL; Denisov, IG; Grinkova, YV; Sligar, SG; Tajkhorshid, E, 2015) | 0.42 |
"Solidified floating organic drop microextraction (SFODME) in combination with high performance liquid chromatography was used for separation/preconcentration and determination of carbamazepine (CBZ) in human plasma and urine samples." | ( Solidified floating organic drop microextraction combined with high performance liquid chromatography for the determination of carbamazepine in human plasma and urine samples. Abbasi, B; Asadi, M; Dadfarnia, S; Haji Shabani, AM, 2015) | 0.82 |
" In addition, carbamazepine and carbamazepine 10, 11-epoxide concentrations were determined using a reference liquid chromatography combined with a tandem mass spectrometry (LC/MS/MS) reference method in another 15 specimens." | ( Effect of Carbamazepine 10, 11-Epoxide on Serum Carbamazepine Measurement Using a New CMIA Assay: Comparison of Values Obtained by Using PETINIA, CEDIA and Liquid Chromatography Combined with Tandem Mass Spectrometry. Dasgupta, A; Davis, B; Johnson-Davis, KL; Slawson, MH, 2016) | 1.2 |
"The combination of anticonvulsant mood stabilizers with antipsychotic drugs may lead to clinically relevant drug-drug interactions." | ( Pharmacokinetic Drug-Drug Interactions of Mood Stabilizers and Risperidone in Patients Under Combined Treatment. Gründer, G; Haen, E; Hiemke, C; Lammertz, SE; Paulzen, M; Schoretsanitis, G; Schruers, KR; Stegmann, B, 2016) | 0.43 |
"This study evaluated the protective effects of CDDP alone and in combination with carbamazepine (CBZ) on kainic acid-induced TLE and cognitive impairment in rats." | ( Protective effect of compound Danshen (Salvia miltiorrhiza) dripping pills alone and in combination with carbamazepine on kainic acid-induced temporal lobe epilepsy and cognitive impairment in rats. Cao, B; Chen, M; Dang, X; Han, S; Jia, C; Jiao, H; Liu, Y; Niu, Q; Wei, L, 2018) | 0.92 |
"CDDP combined with CBZ significantly decreased seizure severity and frequency (p < 0." | ( Protective effect of compound Danshen (Salvia miltiorrhiza) dripping pills alone and in combination with carbamazepine on kainic acid-induced temporal lobe epilepsy and cognitive impairment in rats. Cao, B; Chen, M; Dang, X; Han, S; Jia, C; Jiao, H; Liu, Y; Niu, Q; Wei, L, 2018) | 0.69 |
"This study investigates the neuronal protective effect of SXC combined with carbamazepine (CBZ) on epilepsy and cognitive impairment in kainic acid-kindled SD rats." | ( Neuronal protective effect of Songling Xuemaikang capsules alone and in combination with carbamazepine on epilepsy in kainic acid-kindled rats. Chen, M; Jia, C; Jiao, H; Wei, L; Yang, H; Yin, W; Zhang, R, 2019) | 0.97 |
"The present study aims to evaluate the efficacy of selenium (Se) alone or combined with carbamazepine (CBZ) against the adverse effects induced by the chemoconvulsant pentylenetetrazole (PTZ) in the cortex of adult male rats." | ( Electrophysiological and Neurochemical Assessment of Selenium Alone or Combined with Carbamazepine in an Animal Model of Epilepsy. Aboul Ezz, HS; Ali, MA; Mohammed, HS; Zedan, A, 2020) | 1 |
" Hence, potential drug-drug interactions (DDIs) may occur between these 2 drugs and antiretrovirals." | ( Drug-Drug Interactions Between Antiretrovirals and Carbamazepine/Oxcarbazepine: A Real-Life Investigation. Atzori, C; Baldelli, S; Cattaneo, D; Cozzi, V; Filice, C; Fusi, M; Gervasoni, C; Micheli, V, 2020) | 0.81 |
" Brivaracetam does not interact with most metabolizing enzymes and drug transporters, and therefore does not interfere with drugs that use these metabolic routes." | ( A review of the drug-drug interactions of the antiepileptic drug brivaracetam. Chanteux, H; Gidal, B; Laloyaux, C; Moseley, BD; Nicolas, JM; Stockis, A, 2020) | 0.56 |
" In particular, carbamazepine (CBZ) is of high potential to interact with concurrent treatment of Chinese Medicine." | ( Herb-drug interaction of gastrodiae rhizoma on carbamazepine: A pharmacokinetic study in rats. Chook, P; Koon, CM; Leung, H; Leung, PC; Leung, TWH; Mok, VCT; Schachter, S; Yip, KL; Zhou, X, 2020) | 1.16 |
" Due to its widespread use and CYP3A4-mediated metabolism, there is concern regarding drug-drug interactions (DDIs), particularly a suboptimal LNG exposure when co-administered with CYP3A4 inducers, potentially leading to unintended pregnancies." | ( Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling. Chaturvedula, A; Cicali, B; Cristofoletti, R; Hoechel, J; Lingineni, K; Schmidt, S; Vozmediano, V; Wendl, T; Wiesinger, H, 2021) | 0.62 |
" Carbamazepine combined with valproic acid significantly increased epoxide levels in milk and maternal serum but not in breastfed infants." | ( Therapeutic monitoring of carbamazepine and its active metabolite during the 1st postnatal month: Influence of drug interactions. Brozmanova, H; Grundmann, M; Kacirova, I, 2021) | 1.83 |
" Pharmacokinetic drug-drug interactions (DDIs) between antiseizure medications (ASMs) and anti-infectives can occur and influence their efficacy or cause toxicity." | ( A review of pharmacokinetic drug interactions between antimicrobial and antiseizure medications in children. Lattanzi, S; Zaccara, G, 2021) | 0.62 |
" The purpose of this review is to present data from the last few years on drug-drug interactions among of AEDs, as well as AEDs with other drugs, nutrients and food." | ( Pharmacokinetic Drug-Drug Interactions among Antiepileptic Drugs, Including CBD, Drugs Used to Treat COVID-19 and Nutrients. Główka, AK; Główka, FK; Karaźniewicz-Łada, M; Mikulska, AA, 2021) | 0.62 |
" Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model." | ( Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model. Alves, G; Falcão, A; Fortuna, A; Meirinho, S; Rodrigues, M, 2022) | 0.72 |
" A limited fraction of potential drug-drug interactions (DDIs) have been or can ethically be studied in clinical trials, leaving the vast majority unexplored." | ( General Framework to Quantitatively Predict Pharmacokinetic Induction Drug-Drug Interactions Using In Vitro Data. Akpan, A; Bearon, R; Grañana-Castillo, S; Hodge, D; Khoo, S; Pham, T; Siccardi, M; Williams, A, 2023) | 0.91 |
"Chronic oral anticancer therapies, are increasingly prescribed and present new challenges including the enhanced risk of overlooked drug-drug interactions (DDIs)." | ( The use of therapeutic drug monitoring to highlight an over-looked drug-drug interaction leading to imatinib treatment failure. Buonadonna, A; Canil, G; Cecchin, E; Dalle Fratte, C; Gagno, S; Guardascione, M; Orleni, M; Posocco, B; Roncato, R; Toffoli, G; Zanchetta, M, 2023) | 0.91 |
" Drug-drug interactions were evaluated though Lexicomp." | ( The use of therapeutic drug monitoring to highlight an over-looked drug-drug interaction leading to imatinib treatment failure. Buonadonna, A; Canil, G; Cecchin, E; Dalle Fratte, C; Gagno, S; Guardascione, M; Orleni, M; Posocco, B; Roncato, R; Toffoli, G; Zanchetta, M, 2023) | 0.91 |
"The purpose of this study was to detect the changes of P-Glycoprotein (P-GP) expression in rat brain microvessel endothelial cell line RBE4 after the action of Tetramethylpyrazine (TMP) on Carbamazepine (CBZ), so as to clarify the potential mechanism of TMP combined with CBZ against intractable epilepsy drug resistance." | ( Study on the reversal of epileptic drug resistance by tetramethylpyrazine in combination with carbamazepine through modulation of P-Glycoprotein expression in rat brain microvessel endothelial cell. Deng, Y; Li, Y; Liu, J; Liu, W; Qian, X; Wang, J; Xiao, G; Yan, J; Ye, J; Zhong, N, 2023) | 1.32 |
Carbamazepine is an antiepileptic drug having low bioavailability due to its hydrophobic nature. absorption appeared to be delayed in alcoholics, both after debauche and withdrawal, but its bioavailability did not seem to be reduced.
Excerpt | Reference | Relevance |
---|---|---|
", 1974), the problem of its low bioavailability in solid form and its short half-life in monkey were addressed." | ( Carbamazepine revisited in a monkey model. Congdon, WC; DuCharme, LL; Levy, RH; Lockard, JS; Patel, IH, 1979) | 1.7 |
" However, if AUC0 leads to 72 was calculated instead of AUC0 leads to infinity, the preparation A gave the significantly lower bioavailability than the other compounds." | ( Bioavailability of four different pharmaceutical preparations of carbamazepine. Iisalo, E; Mäntylä, R; Pynnönen, S, 1978) | 0.5 |
" New knowledge of the pharmacokinetics of phenytoin has led to a better understanding of the drug's bioavailability and uses." | ( Recent advances in drug therapy for epilepsy. Bruni, J, 1979) | 0.26 |
"A comparative bioavailability study was performed using two commercially available types of carbamazepine tablets, by statistical analysis of serum levels and other bioavailability parameters." | ( Comparative bioavailability of two commercial preparations of carbamazepine tablets. Aaltonen, R; Anttila, M; Kahela, P; Panelius, M; Tikkanen, R; Yrjänä, T, 1979) | 0.72 |
" There were some suggestions of impaired bioavailability of the drug when given in tablet form." | ( The pharmacokinetics of carbamazepine. Cotter, LM; Eadie, MJ; Hooper, WD; Lander, CM; Smith, GA; Tyrer, JH, 1977) | 0.56 |
"The bioavailability of two preparations of carbamazepine--the tablet and a new syrup-was studied in 9 adult male volunteers by measuring saliva and serum levels." | ( Pharmacokinetic comparison of tablet and suspension dosage forms of carbamazepine. Friel, P; Leal, K; Pearmain, J; Remick, R; Troupin, AS; Wada, JA, 1978) | 0.76 |
"Differences in the bioavailability after administration of two pure carbamazepine samples that were different in particle sizes have been found." | ( The relative bioavailability and pharmacokinetics of carbamazepine. Richter, K; Terhaag, B, 1978) | 0.74 |
" Areas under the plasma level curves, absorption rate constants and times to achieve peak plasma levels showed little difference between the two preparations." | ( The comparative bioavailability of carbamazepine in 100 mg and 200 mg tablets. Eadie, MJ; Hooper, WD; Smith, GA; Tyrer, JH; Werth, B, ) | 0.41 |
" The absorption rate and fraction are very much dependent on the pharmaceutical preparation, and changes of brand may alter the plasma level of phenytoin in spite of unaltered dose." | ( Clinical pharmacokinetics of anticonvulsants. Dam, M; Hvidberg, EF, 1976) | 0.26 |
"The bioavailability of commercial carbamazepine talbets with and without meals was compared to a propylene glycol solution respect to extent of absorption in 6 normal humans after a dose of 6 MG/KG." | ( Pharmacokinetics of carbamazepine in normal man. Green, JR; Levy, RH; Neal, JM; Pitlick, WH; Troupin, AS, 1975) | 0.86 |
" It was concluded that the pharmaceutical formulation of carbamazepine tablets limits the bioavailability of the drug, and that problems may arise if the bioavailability of the drug is to be increased." | ( The bioavailability of carbamazepine. Cotter, LM; Eadie, MJ; Hooper, WD; Smith, G; Tyrer, JH, 1975) | 0.81 |
"The comparative bioavailability and steady state fluctuations resulting from the administration of Tegretol 200 mg commercial tablets and carbamazepine OROS controlled delivery tablets were investigated in 22 adult and 12 pediatric epileptic patients." | ( Comparative bioavailability and steady state fluctuations of Tegretol commercial and carbamazepine OROS tablets in adult and pediatric epileptic patients. Garnett, WR; Kochak, GM; Levy, RH; Mangat, S; Thakker, KM, 1992) | 0.71 |
" Through pharmacokinetic analyses, the decreased AUC and increased Vz/f were attributed to decreased bioavailability of phenytoin when CBZ was co-administered." | ( Effect of single- and multiple-dose carbamazepine on the pharmacokinetics of diphenylhydantoin. Huang, JD; Lai, ML; Lin, TS, 1992) | 0.56 |
"A bioavailability study of two commercial carbamazepine sustained-release formulations was carried out in 14 healthy male subjects in order to compare plasma concentration/time profiles and to determine the relative bioavailability of carbamazepine (CBZ)." | ( Investigation of the bioequivalence of two carbamazepine sustained-release formulations in healthy subjects. Düsing, R; Frercks, HJ; Lührmann, B; Schulz, HU, 1992) | 0.81 |
" Carbamazepine absorption appeared to be delayed in alcoholics, both after debauche and withdrawal, but its bioavailability did not seem to be reduced." | ( Carbamazepine kinetics and adverse effects during and after ethanol exposure in alcoholics and in healthy volunteers. Andersson, K; Lidén, A; Melander, A; Sternebring, B, 1992) | 2.64 |
" The results indicate that OCBZ, like most antiepileptic drugs (AEDs), decreases the bioavailability of EE and LNG, perhaps by affecting metabolism or protein binding." | ( Possible interaction between oxcarbazepine and an oral contraceptive. Haring, P; Klosterskov Jensen, P; Menge, GP; Saano, V; Svenstrup, B, ) | 0.13 |
"The bioavailability of three lots of a generic 200-mg carbamazepine tablet, which had been withdrawn from the market, was compared to the bioavailability of one lot of the innovator product in 24 healthy volunteers." | ( The bioinequivalence of carbamazepine tablets with a history of clinical failures. Jarvi, EJ; Meyer, MC; Pelsor, FR; Shah, VP; Straughn, AB; Wood, GC, 1992) | 0.84 |
"The bioavailability and serum level fluctuations of three carbamazepine (CBZ, CAS 298-46-4) slow release preparations marketed in Germany were compared in patients with epilepsy." | ( Steady state concentrations and diurnal fluctuations of carbamazepine in patients after different slow release formulations. May, T; Schreiber, G; Tiska, G; Wolf, P, 1992) | 0.77 |
" Since praziquantel, the drug used to treat neurocysticercosis, undergoes extensive liver first-pass metabolism, we carried out a prospective study to verify whether there was a decrease in oral bioavailability induced by carbamazepine and phenytoin." | ( Phenytoin and carbamazepine decreased oral bioavailability of praziquantel. Bittencourt, PR; Diekmann, HW; Fernandes, AG; Gracia, CM; Jung, W; Martins, R, 1992) | 0.83 |
"In order to compare the multiple-dose bioavailability of carbamazepine (CBZ) from 2 slow-release preparations, Neurotol slow and Tegretol Retard, a single-blind, randomized, cross-over study was carried out." | ( Comparative bioavailability of carbamazepine from two slow-release preparations. Anttila, M; Heinonen, EH; Nyman, L; Reunanen, M, 1992) | 0.81 |
"A bioavailability study with three test batches of a sustained release formulation of carbamazepine, which differed only in their in vitro dissolution profiles, was performed in 18 healthy subjects to compare the respective plasma concentration profiles and to determine the relative bioavailability of carbamazepine (CBZ)." | ( Investigations into the relative bioavailability of carbamazepine after single oral administration of three test batches of a carbamazepine-containing sustained release formulation in healthy subjects. Czaja, J; Düsing, R; Frecks, HJ; Grunwald, F; Lührmann, B; Schulz, HU, 1992) | 0.76 |
" Bioavailability tests (single dosage, crossover design) and several investigations into the dissolution profile were carried out on three test batches of a sustained release carbamazepine preparation (Timonil 300 retard)." | ( Pharmaceutical and biopharmaceutical quality of a sustained release carbamazepine preparation: a contribution to quality assurance. Czaja, J; Düsing, R; Grunwald, F; Schulz, HU, 1992) | 0.71 |
"The in-vitro dissolution profiles of two carbamazepine formulations (Tegretol and a generic carbamazepine) have been assessed and the bioavailability of carbamazepine compared in 12 epileptic children at steady-state." | ( Dissolution and relative bioavailability of two carbamazepine preparations for children with epilepsy. Aleksandrowicz, J; Bowmer, CJ; Cawood, A; Forsythe, WI; Hartley, R, 1991) | 0.8 |
" No significant changes were determined for fraction of absorbed dose, volume of distribution, absorption rate constant, and elimination rate constant." | ( Increased carbamazepine plasma concentrations after fluoxetine coadministration. Carter, JG; D'Mello, AP; D'Souza, MJ; Grimsley, SR; Jann, MW, 1991) | 0.68 |
" The bioavailability of CBZ from the two preparations was similar." | ( Treatment of epilepsy in mentally retarded patients with a slow-release carbamazepine preparation. Anttila, M; Heinonen, E; Kaski, M; Sivenius, J; Tuominen, J, 1991) | 0.51 |
" Estimates for volume of distribution, rates of absorption and elimination, and bioavailability could not be pursued rigorously." | ( Postinduction carbamazepine clearance in an adult psychiatric population. Crismon, ML; Godley, PJ; Martin, ES, 1991) | 0.64 |
" Mean concentration values also differed significantly, which is explained by a somewhat reduced bioavailability (22% less) of the slow-release formulation." | ( Diurnal variation of carbamazepine and carbamazepine-10,11-epoxide in plasma and saliva in children with epilepsy: a comparison between conventional and slow-release formulations. Arvidsson, J; Eeg-Olofsson, O; Grahn, PA; Gylje, H; Larsson, C; Nilsson, HL; Norén, L; Tonnby, B, 1990) | 0.6 |
"The bioavailability of carbamazepine from 4 commercially available products was evaluated in 12 healthy volunteers." | ( [Carbamazepine: the bioavailability of 4 oral pharmaceutical products]. Biagini, L; Chávez, H; Galdames, D; Passalacqua, A; Saavedra, I, 1990) | 1.5 |
"The bioavailability of carbamazepine from two products (Ethical Generics and Ciba-Geigy) and their efficacy with regard to seizure control and incidence of side-effects were compared in 23 children with tonic-clonic or complex partial seizures." | ( Breakthrough seizures with generic carbamazepine: a consequence of poorer bioavailability? Aleksandrowicz, J; Bowmer, CJ; Forsythe, WI; Hartley, R; McLain, B; Ng, PC, 1990) | 0.87 |
" There was no significant difference in bioavailability between the 2 preparations." | ( Multiple-dose pharmacokinetic study with a slow-release carbamazepine preparation. Anttila, M; Heinonen, E; Hokkanen, E; Järvensivu, P; Lehto, H; Reunanen, M, 1990) | 0.53 |
" The relative bioavailability of CBZ suspension with enteral feeding administration was 90." | ( Effects of enteral tube feeding on the absorption and pharmacokinetic profile of carbamazepine suspension. Bass, J; Holcombe, BJ; Miles, MV; Tennison, MB; Thorn, MD, ) | 0.36 |
" CBZ-CR fulfils the criteria for a controlled-release preparation with comparable apparent bioavailability to CBZ-C." | ( A double-blind comparison of conventional and controlled-release carbamazepine in healthy subjects. Brodie, MJ; Butler, E; Larkin, JG; McLellan, A; Munday, A; Sutherland, M, 1989) | 0.51 |
" The relative degree of bioavailability of Amizepin amounted to 98% of that of Tegretol." | ( [Evaluation of the biological availability of 2 carbamazepine preparations]. Kuran, W; Niedzielska, K; Rosnowska, M, ) | 0.39 |
" The bioavailability was reduced by colestipol 80%, by cholestyramine 95% and by activated charcoal 99." | ( Effects of resins and activated charcoal on the absorption of digoxin, carbamazepine and frusemide. Hirvisalo, EL; Kivistö, K; Neuvonen, PJ, 1988) | 0.51 |
"The relative bioavailability of carbamazepine mixture was studied after oral and rectal administration to healthy subjects." | ( Bioavailability of rectally administered carbamazepine mixture. Neuvonen, PJ; Tokola, O, 1987) | 0.82 |
" Most oral formulations of carbamazepine are well absorbed with high bioavailability." | ( Clinical pharmacokinetics and pharmacological effects of carbamazepine and carbamazepine-10,11-epoxide. An update. Bertilsson, L; Tomson, T, ) | 0.67 |
"Differences in product formulations have been shown to affect the therapeutic response by altering the relative bioavailability and pharmacokinetics of a drug." | ( A comparative bioavailability study of carbamazepine tablets and a chewable tablet formulation. Comstock, TJ; Garnett, WR; Maas, B; Pellock, JM, 1987) | 0.54 |
" Bioavailability of prednisolone after the oral administration of prednisone and methylprednisolone ranged from 86% to 104% during anticonvulsant therapy." | ( Prednisolone and methylprednisolone kinetics in children receiving anticonvulsant therapy. Bartoszek, M; Brenner, AM; Szefler, SJ, 1987) | 0.27 |
"The palatability of five flavored and unflavored extemporaneous carbamazepine 20-mg/mL oral suspensions was tested, and the bioavailability of the unflavored suspension relative to that of the tablet used in its manufacture was determined in a randomized, crossover study of 12 healthy volunteers." | ( Palatability and relative bioavailability of an extemporaneous carbamazepine oral suspension. Bloomer, D; Dupuis, LL; MacGregor, D; Soldin, SJ, 1987) | 0.75 |
" The likely causes of this fact were: too low doses prescribed (55% of the patients were given doses below the generally recommended), lower bioavailability of PHT (27% of patients had no therapeutic level of the drug in the serum, despite doses exceeding 5 mg/kg); or drug interaction." | ( [Characteristics of the clinical features and pharmacological treatment of epileptics with frequent seizures]. Buksowicz, C; Horyd, W; Koziak, M; Kuran, W; Lipczyńska-Lojkowska, W; Niedzielska, K; Witkowska-Olearska, K, ) | 0.13 |
"070); Ka, the first-order absorption rate constant (0." | ( Simultaneous first- and zero-order absorption of carbamazepine tablets in humans. Chan, KK; Riad, LE; Sawchuk, RJ; Wagner, WE, 1986) | 0.53 |
"The bioavailability of dexamethasone (DEX) has recently been demonstrated to be a critical factor in determining Dexamethasone Suppression Test (DST) status in psychiatric patients." | ( Dexamethasone bioavailability: implications for DST research. Lowy, MT; Meltzer, HY, 1987) | 0.27 |
" The drug's absorption rate increased and its peak plasma levels occurred earlier." | ( Intermittent carbamazepine intoxication possibly related to altered absorption characteristics of the drug. Eadie, MJ; Hooper, WD, 1987) | 0.64 |
" Like tetracycline, erythromycin also appears to have the potential for increasing the bioavailability of digoxin in patients who excrete high amounts of reduced digoxin metabolites, apparently through destruction of the gut flora that form these compounds." | ( Pharmacokinetic interactions of the macrolide antibiotics. Ludden, TM, ) | 0.13 |
" The mechanisms responsible for these effects have not been elucidated and possibly include decreased bioavailability or compliance, increased metabolic clearance, or decreased plasma protein binding." | ( Effects of pregnancy on antiepileptic drug utilization. Levy, RH; Yerby, MS, 1985) | 0.27 |
"A comparative bioavailability study of carbamazepine (CBZ) in tablets and a syrup preparation was carried out in six volunteers, using a crossover design." | ( Simultaneous plasma carbamazepine and carbamazepine-epoxide concentrations in pharmacokinetic and bioavailability studies. Dickinson, RG; Eadie, MJ; Hooper, WD; King, AR; Patterson, M, 1985) | 0.86 |
"During a carbamazepine (CBZ) relative bioavailability study involving tablets and a syrup preparation, salivary drug concentrations appeared disproportionately high relative to simultaneous plasma drug concentrations in the first 2-3 h after oral drug intake." | ( Fallacious results from measuring salivary carbamazepine concentrations. Dickinson, RG; Eadie, MJ; Hooper, WD; King, AR, 1985) | 0.95 |
"The bioavailability and central side effects of five carbamazepine tablets with different rates of absorption were investigated in nine healthy volunteers in a randomized cross-over study using single doses of 400 mg." | ( Bioavailability and central side effects of different carbamazepine tablets. Neuvonen, PJ, 1985) | 0.77 |
"The relative bioavailability of an investigational carbamazepine suspension was studied following rectal administration in human volunteers." | ( Relative bioavailability of rectally administered carbamazepine suspension in humans. Cloyd, JC; Graves, NM; Jones-Saete, C; Kriel, RL, ) | 0.64 |
" Carbamazepine is well absorbed and largely metabolized." | ( Pharmacokinetics of antiepileptic drugs. Neuvonen, PJ; Tokola, RA, 1983) | 1.18 |
"The relative bioavailability of an investigational carbamazepine suspension was studied following rectal administration in dogs." | ( Bioavailability of rectally administered carbamazepine suspension in dogs. Cloyd, JC; Graves, NM; Kriel, RL, 1983) | 0.78 |
"The comparative bioavailability of two commercial carbamazepine tablets (Finlepsin and Tegretol) was investigated." | ( Comparative bioavailability of two carbamazepine tablets. Glende, M; Hüller, H; Mai, I; Migulla, H; Prümke, J; Schumann, G, 1983) | 0.8 |
" The absolute bioavailability was determined by administering formulations A or B intravenously." | ( Intramuscular absorption of carbamazepine in rhesus monkeys. Levy, RH; Patel, IH, 1980) | 0.56 |
"The Michaelis-Menten pharmacokinetics and bioavailability of phenytoin were evaluated in children." | ( Plasma levels and pharmacokinetics of antipileptic drugs in children. Miura, H, 1981) | 0.26 |
"079 day-1), or absorption rate constant (14." | ( Effect of erythromycin on carbamazepine kinetics. Bell, RD; Ludden, TM; Wong, YY, 1983) | 0.57 |
" An antacid did not affect the bioavailability of single CBZ doses given to three subjects and was therefore used to neutralize gastric juice when administering CBZ-E." | ( Single-dose kinetics and metabolism of carbamazepine-10,11-epoxide. Bertilsson, L; Tomson, T; Tybring, G, 1983) | 0.54 |
" Absolute bioavailability of IM PB was 101 +/- 11%." | ( Kinetics of phenobarbital in normal subjects and epileptic patients. Comfort, CP; Friel, PN; Kaluzny, SP; Levy, RH; Wilensky, AJ, 1982) | 0.26 |
" Accordingly, carbamazepine had a more rapid absorption rate from F-CBZ, DAK than from Tegretol in a comparative absorption test involving single-dose administration of 200 mg to 8 healthy volunteers." | ( Carbamazepine: a clinical biopharmaceutical study. Christiansen, J; Dam, M; Helles, A; Jaegerskou, A; Kristensen, CB; Schmiegelow, M, 1981) | 2.07 |
" Bioavailability of CBZ was reduced by 29% in the presence of AMP, while that of SV was increased by about 8%." | ( Aminophylline alters pharmacokinetics of carbamazepine but not that of sodium valproate--a single dose pharmacokinetic study in human volunteers. David, J; Joseph, T; Kulkarni, C; Vaz, J, 1995) | 0.56 |
" This reflects either an induction of CsA hepatic metabolism or a reduced systemic bioavailability (possible induction of pre-hepatic metabolism) by concurrent use of carbamazepine." | ( Effects of carbamazepine on cyclosporine metabolism in pediatric renal transplant recipients. Cooney, GF; Dunn, SP; Goldsmith, B; Kaiser, B; Mochon, M, ) | 0.72 |
"The relative bioavailability of three carbamazepine generics available in Turkey, were investigated in 5 healthy male volunteers." | ( Pharmacokinetics of carbamazepine. Part I: A new bioequivalency parameter based on a relative bioavailability trial. Ertaş, M; Kayali, A; Tuğlular, I, ) | 0.73 |
"27 l/kg in a typical 33-kg patient, assuming that the bioavailability of orally administered zonisamide is 100%." | ( Population analysis of the dose-dependent pharmacokinetics of zonisamide in epileptic patients. Hashimoto, Y; Hori, R; Odani, A; Okuno, T; Tanigawara, Y; Yasuhara, M, 1994) | 0.29 |
"The extent of absorption of carbamazepine from a 2-hydroxypropyl-beta-cyclodextrin/carbamazepine complex was significantly greater and the rate of absorption was faster when compared with an immediate-release carbamazepine tablet in the dog." | ( Oral pharmacokinetics of carbamazepine in dogs from commercial tablets and a cyclodextrin complex. Betlach, CJ; Bodor, N; Gonzalez, MA; McKiernan, BC; Neff-Davis, C, 1993) | 0.88 |
" The effect of such variations on tablet efficacy cannot be ascertained in the absence of bioavailability data." | ( In vitro evaluation of carbamazepine 200 mg tablets. Kibwage, IO; Nguyo, M, 1993) | 0.6 |
" This reduction in FEL bioavailability is much smaller than that observed after co-administration of carbamazepine (CBZ) (i." | ( Influence of single and repeated doses of oxcarbazepine on the pharmacokinetic profile of felodipine. Bendoni, L; Gangemi, PF; Menge, GP; Monza, GC; Schwabe, S; Zaccara, G, 1993) | 0.5 |
" Plasma carbamazepine concentration data were obtained from an open, steady-state, crossover bioavailability study in which 494 measurements were obtained from 13 patients, with an equal number of samples per patient for each dosage form." | ( Bioavailability of controlled release carbamazepine estimated by mixed effect modelling. Ludden, TM; Miller, R, 1993) | 0.99 |
" The absorption rate constant (Ka), steady-state volume of distribution (Vdss) and total clearance (CL) were computed with the APIS software using 31 blood level profiles from 23 patients who were divided into four groups: patients receiving CBZ-CO in polytherapy, the same patients switched to CBZ-CR in the same polytherapy conditions, patients receiving CBZ-CO in monotherapy and patients receiving CBZ-CR in monotherapy." | ( Steady state pharmacokinetics of conventional versus controlled-release carbamazepine in patients with epilepsy. Bonneton, J; Dravet, C; Genton, P; Iliadis, A; Mesdjian, E; Viallat, D, 1993) | 0.52 |
" The absorption rate constant (Ka), apparent steady state volume of distribution (Vdss/F), and apparent total clearance (CL/F) were computed with the APIS software using blood level profiles from 34 patients divided into four groups: patients receiving either CBZ-CO or CBZ-CR in monotherapy, or CBZ-CO or CBZ-CR in comedication with PB." | ( Steady state pharmacokinetics of carbamazepine-phenobarbital interaction in patients with epilepsy. Barra, Y; Bonneton, J; Genton, P; Iliadis, A; Mesdjian, E; Sennoune, S, 1996) | 0.58 |
" The absolute bioavailability of CBZ from the tablets was approximately 25%." | ( Intravenous and oral pharmacokinetic evaluation of a 2-hydroxypropyl-beta-cyclodextrin-based formulation of carbamazepine in the dog: comparison with commercially available tablets and suspensions. Anderson, WR; Bodor, N; Brewster, ME; Cheung, B; Derendorf, H; Estes, KS; Meinsma, D; Moreno, D; Pablo, L; Pop, E; Sawchuk, R; Webb, AI, 1997) | 0.51 |
"To compare the bioavailability of three generic brands of carbamazepine tablets with that of a proprietary brand in adult patients with epilepsy." | ( Comparative study of bioavailability and clinical efficacy of carbamazepine in epileptic patients. Amornpichetkoon, M; Kaojarern, S; Silpakit, O, 1997) | 0.78 |
"The bioavailability of two generic brands of carbamazepine tablets (Carmapine and Carzepine) and the proprietary brand (Tegretol) were equivalent in this sample of adult patients with epilepsy." | ( Comparative study of bioavailability and clinical efficacy of carbamazepine in epileptic patients. Amornpichetkoon, M; Kaojarern, S; Silpakit, O, 1997) | 0.8 |
" This problem was considered with regard to carbamazepine 400 retard AWD (test) whose bioavailability relative to a listed reference (Tegretal 400 retard) was studied in 2 randomized, open, crossover studies both with 18 healthy volunteers of Caucasian origin (20-36 years, 61." | ( A single and multiple dose bioavailability study with carbamazepine 400 mg retard tablets with reference to enzyme autoinduction and circadian time differences. Franke, G; Hoffmann, A; Hoffmann, C; Möritz, KU; Siegmund, W; Terhaag, B; Zschiesche, M, 1997) | 0.81 |
"Carbamazepine 400 retard AWD tablets were bioequivalent to reference with regard to extent and rate of absorption after both single and multiple dose administration." | ( A single and multiple dose bioavailability study with carbamazepine 400 mg retard tablets with reference to enzyme autoinduction and circadian time differences. Franke, G; Hoffmann, A; Hoffmann, C; Möritz, KU; Siegmund, W; Terhaag, B; Zschiesche, M, 1997) | 1.99 |
" The rate of absorption of slow-release carbamazepine, as reflected by HVD, appeared to be unchanged in the presence of food." | ( Influence of food on the bioavailability of a carbamazepine slow-release formulation. Retzow, A; Schulz, HU; Schürer, M, 1997) | 0.82 |
" Also, the plasma t 1/2 (of carbamazepine was prolonged by two folds and bioavailability reduced by about 32% in presence of caffeine." | ( Influence of caffeine on pharmacokinetic profile of sodium valproate and carbamazepine in normal human volunteers. David, J; Joseph, T; Kulkarni, C; Vaz, J, 1998) | 0.83 |
"The additional parameters examined may supplement the traditional single-point parameters, Cmax and tmax, for assessment of rate of absorption and the flatness of the concentration curve." | ( Criteria to assess in vivo performance and bioequivalence of generic controlled-release formulations of carbamazepine. Bialer, M; Houle, JM; Levitt, B; Moros, D; Munsaka, MS; Yacobi, A, 1998) | 0.51 |
"To examine the effect of grapefruit juice on the bioavailability of carbamazepine in patients with epilepsy." | ( Effect of grapefruit juice on carbamazepine bioavailability in patients with epilepsy. Bhargava, VK; Garg, SK; Kumar, N; Prabhakar, SK, 1998) | 0.82 |
"Grapefruit juice increases the bioavailability of carbamazepine by inhibiting CYP3A4 enzymes in gut wall and in the liver." | ( Effect of grapefruit juice on carbamazepine bioavailability in patients with epilepsy. Bhargava, VK; Garg, SK; Kumar, N; Prabhakar, SK, 1998) | 0.84 |
" The new parameters showed that CBZ 600 granulate has similar rate of absorption as the two 600 mg CR tablets, but its extent of absorption was lower." | ( Existing and new criteria for bioequivalence evaluation of new controlled release (CR) products of carbamazepine. Arcavi, L; Bialer, M; Laor, A; Levitt, B; Moros, D; Sussan, S; Volosov, A; Yacobi, A, 1998) | 0.52 |
" After its oral administration to dogs, the absolute bioavailability was 78." | ( Stereoselective pharmacokinetic analysis of the antiepileptic 10-hydroxycarbazepine in dogs. Bialer, M; Sintov, A; Volosov, A, 1999) | 0.3 |
" The newer anticonvulsants felbamate, lamotrigine, topiramate, and tiagabine have different hepatically-mediated drug-drug interactions, while the renally excreted gabapentin lacks hepatic drug-drug interactions but may have reduced bioavailability at higher doses." | ( Metabolism and excretion of mood stabilizers and new anticonvulsants. Corá-Locatelli, G; Frye, MA; Ketter, TA; Kimbrell, TA; Post, RM, 1999) | 0.3 |
" They had been tested in a randomised, fourway cross-over bioavailability study in healthy volunteers." | ( In vitro/in vivo correlations of dissolution data of carbamazepine immediate release tablets with pharmacokinetic data obtained in healthy volunteers. Barends, DM; Lake, OA; Olling, M, 1999) | 0.55 |
" Bioavailability tests were carried out at a dose of either 40 mg/body or 200 mg/body." | ( Physicochemical properties and bioavailability of carbamazepine polymorphs and dihydrate. Itai, S; Ito, S; Kobayashi, Y; Yamamoto, K, 2000) | 0.56 |
"To assess the bioavailability of carbamazepine from two brands of carbamazepine--Tegretol 200 and Zen-200." | ( Comparison of absorption rate and bioavailability of two brands of carbamazepine. Bhatt, AD; Bolar, HV; Desai, ND; Gupta, C; Kamat, DV; Revankar, SN; Sane, SP, 1999) | 0.82 |
"A two-way randomised cross-over bioavailability of carbamazepine was carried out in twelve healthy male volunteers." | ( Comparison of absorption rate and bioavailability of two brands of carbamazepine. Bhatt, AD; Bolar, HV; Desai, ND; Gupta, C; Kamat, DV; Revankar, SN; Sane, SP, 1999) | 0.79 |
"A three-way randomized cross-over bioavailability study was carried out using CBZ 200 mg tablets of conventional and two controlled release formulations in twelve healthy volunteers." | ( Comparative bioavailability study of a conventional and two controlled release oral formulations of Tegretol (carbamazepine)--200 mg. Bhatt, AD; Bolar, HV; Desai, ND; Revankar, SN; Sane, SP; Tipnis, HP, 1999) | 0.52 |
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents." | ( QSAR model for drug human oral bioavailability. Topliss, JG; Yoshida, F, 2000) | 0.31 |
"Polymorphs of a compound have solid crystalline phases with different internal crystal lattices; in pharmaceuticals, differences due to polymorphism and pseudopolymorphism can affect bioavailability and effective clinical use." | ( Solid-state study of polymorphic drugs: carbamazepine. Ferioli, V; Ficarra, R; Gamberini, G; Gamberini, MC; Rustichelli, C; Tommasini, S, 2000) | 0.57 |
" The concepts of bioavailability and bioequivalence require further consideration." | ( Is generic prescribing acceptable in epilepsy? Besag, FM, 2000) | 0.31 |
" The clinical significance of the time-dependent influence of PTX on the rate of absorption of CBZ will be revealed upon extension of the study to patients." | ( Time-dependent influence of pentoxifylline on the pharmacokinetics of orally administered carbamazepine in human subjects. Boinpally, RR; Devaraj, R; Poondru, S; Yamsani, MR, 2001) | 0.53 |
" The results suggest that co-administration of Mentat could improve the effectiveness of anti-epileptic drugs due to the increased bioavailability of the latter." | ( Pharmacokinetic interactions of Mentat with carbamazepine and phenytoin. Gopumadhavan, S; Mitra, SK; Rafiq, M; Sundaram, R; Tripathi, M; Venkataranganna, MV, ) | 0.39 |
" Statistical analysis of pharmacokinetic parameters confirmed that the carbamazepine:PEG 6000 binary systems displayed higher bioavailability of the drug than the pure carbamazepine." | ( In vitro and in vivo evaluation of carbamazepine-PEG 6000 solid dispersions. Arnaud, P; Chemtob, C; Dugue, J; Toscani, S; Zerrouk, N, 2001) | 0.82 |
" OXC has a high bioavailability and is 40% protein-bound." | ( [Oxcarbazepine]. Arroyo, S, 2001) | 0.31 |
"This paper describes a graphical model for simplifying in vitro absorption, metabolism, distribution, and elimination (ADME) data analysis through the estimation of oral bioavailability (%F) of drugs in humans and other species." | ( Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. Hwang, KK; Mandagere, AK; Thompson, TN, 2002) | 0.31 |
" In rectal-resected rabbits, the bioavailability of CBZ and the plasma level of CBZ-E after rectal administration were significantly lower than those in normal rabbits, and furthermore these values after intracolostomal administration to colostoma-constructed rabbits tended to be lower than those in rectal-resected ones." | ( Decreased bioavailability of carbamazepine suppository after its intrarectal and intracolostomal administration to rectal-resected or colostoma-constructed rabbits. Fujimoto, S; Kintsuji, S; Nagasawa, K; Nakanishi, H; Yamamoto, R, 2002) | 0.61 |
" Data thus obtained suggested that honey decreases the bioavailability of carbamazepine." | ( Effect of honey on carbamazepine kinetics in rabbits. Abraham, BK; Adithan, C; Asad, M; Koumaravelou, K; Shashindran, CH, 2002) | 0.87 |
" The goal of the study was to compare the bioavailability after single doses and at steady state of the FMI versus CMF and CTF as well." | ( Oxcarbazepine final market image tablet formulation bioequivalence study after single administration and at steady state in healthy subjects. D'Souza, J; Flesch, G; Hossain, M; Souppart, C; Tudor, D, 2002) | 0.31 |
"Oxcarbazepine (trileptal) oral suspension has been reformulated and a study was performed to compare the bioavailability after single doses and at steady state of the current and former oral suspension versus the marketed film-coated tablets and to compare the bioavailability of the current and former oral suspension." | ( Assessment of the bioequivalence of two oxcarbazepine oral suspensions versus a film-coated tablet in healthy subjects. Bonner, J; Camisasca, R; Denouel, J; Flesch, G; Tudor, D, 2003) | 0.32 |
" The bioavailability of the oral formulation of oxcarbazepine is high (>95%)." | ( Clinical pharmacokinetics of oxcarbazepine. Korn-Merker, E; May, TW; Rambeck, B, 2003) | 0.32 |
" Concurrent ingestion of the herbal tea prepared from Cassia auriculata flowers with carbamazepine may therefore influence the bioavailability of the prescribed drug and hence its therapeutic potential." | ( Possible interaction of herbal tea and carbamazepine. Chackrewarthi, S; Munasinghe, TM; Senarath, S; Thabrew, MI, 2003) | 0.81 |
" Cassia auriculata tea has therefore the potential to influence the bioavailability of carbamazepine, and hence its therapeutic actions." | ( The effects of Cassia auriculata and Cardiospermum halicacabum teas on the steady state blood level and toxicity of carbamazepine. Chackrewarthi, S; Munasinghe, J; Senarath, S; Thabrew, I, 2004) | 0.76 |
"The bioavailability of a carbamazepine:beta-cyclodextrin (CBZ:betaCD) complex from hydroxypropylmethylcellulose (HPMC) matrix tablets was evaluated in beagle dogs." | ( Bioavailability of carbamazepine:beta-cyclodextrin complex in beagle dogs from hydroxypropylmethylcellulose matrix tablets. Bassani, VL; Bertuol, JB; Dalla Costa, T; Groch, KR; Koester, LS; Mayorga, P; Moellerke, R; Xavier, CR, 2004) | 0.96 |
" In this study, it was found that a high fat diet increases the bioavailability of phenytoin and carbamazepine in New Zealand white rabbits." | ( Influence of high fat diet (butter) on pharmacokinetics of phenytoin and carbamazepine. Garg, SK; Malhotra, S; Sidhu, S, 2004) | 0.77 |
" However, both binary and ternary approaches were considered suitable techniques to improve the release rate and potentially the in vivo bioavailability of poorly soluble drugs that had previously exhibited slow or incomplete release from SR beads." | ( Effect of SBE7-beta-cyclodextrin complexation on carbamazepine release from sustained release beads. Macrae, RJ; Smith, JS; Snowden, MJ, 2005) | 0.58 |
" However, to estimate additional pharmacokinetic model parameters (eg, the absorption rate constant and V(d)), it would be necessary to combine sparse TDM data with additional well-timed samples." | ( Development of a population pharmacokinetic model for carbamazepine based on sparse therapeutic monitoring data from pediatric patients with epilepsy. Carlsson, KC; Glauser, T; Hoem, NO; Vinks, AA, 2005) | 0.58 |
"05) in extent of bioavailability between the liquid suppository and oral suspension as indicated by the values of AUC(0 - infinity), 17." | ( Thermally reversible in situ gelling carbamazepine liquid suppository. El-Kamel, A; El-Khatib, M, ) | 0.4 |
"Enteric microparticles were prepared by a novel microencapsulation method in order to improve the oral bioavailability of lipophilic drugs." | ( Encapsulation of lipophilic drugs within enteric microparticles by a novel coacervation method. Bodmeier, R; Dong, W, 2006) | 0.33 |
" The high surface area and good wettability of the microparticles, the non-crystalline state of the drug in the matrix and the fast dissolution rate contributed to a significantly enhanced oral bioavailability from the microparticles when compared to the physical mixture." | ( In vitro and in vivo evaluation of carbamazepine-loaded enteric microparticles. Bodmeier, R; Dong, WY; Maincent, P, 2007) | 0.62 |
"Carbamazepine is a poor water soluble drug and its bioavailability is limited by dissolution rate." | ( Evaluation of in vitro-in vivo correlation and anticonvulsive effect of carbamazepine after cogrinding with microcrystalline cellulose. Adibkia, K; Anoush, M; Barzegar-Jalali, A; Barzegar-Jalali, M; Hanaee, J; Nayebi, AM; Sistanizad, M; Valizadeh, H, 2006) | 2.01 |
" In vitro dissolution, which is considered as an estimate of bioavailability demonstrated an initial dissolution of CBZ significantly greater in the treated physical mixtures of PVP10k:CBZ than the initial dissolution of the corresponding untreated physical mixtures and pure untreated CBZ." | ( Effect of n-scCO(2) on crystalline to amorphous conversion of carbamazepine. Needham, TE; Nunes, AC; Ugaonkar, S, 2007) | 0.58 |
" Finally, comparison of oral bioavailability of 1 with Tegretol tablets in dogs shows the co-crystal to be a viable alternative to the anhydrous polymorph in formulated solid oral products." | ( Performance comparison of a co-crystal of carbamazepine with marketed product. Almarsson, O; Guzmán, H; Haley, S; Hickey, MB; Morrisette, SL; Peterson, ML; Remenar, JF; Scoppettuolo, LA; Tawa, MD; Vetter, A; Zaworotko, MJ; Zhang, Z, 2007) | 0.6 |
" Relative bioavailability was calculated and the C(max) and AUCs were compared using Wilcoxon signed-rank tests." | ( Relative bioavailability, metabolism and tolerability of rectally administered oxcarbazepine suspension. Clemens, PL; Cloyd, JC; Kriel, RL; Remmel, RP, 2007) | 0.34 |
"Monohydroxy derivative bioavailability following rectal administration of oxcarbazepine suspension is significantly lower than following oral administration, most likely because of poor oxcarbazepine water solubility." | ( Relative bioavailability, metabolism and tolerability of rectally administered oxcarbazepine suspension. Clemens, PL; Cloyd, JC; Kriel, RL; Remmel, RP, 2007) | 0.34 |
"Interindividual variability in intestinal absorption and bioavailability might contribute to inadequate control of seizures under treatment with carbamazepine and phenytoin." | ( Intestinal expression of cytochrome P450 enzymes and ABC transporters and carbamazepine and phenytoin disposition. Fried, M; Fritschy, JM; Kullak-Ublick, GA; Mueller, S; Pauli-Magnus, C; Simon, C; Stieger, B; Wieser, HG, 2007) | 0.77 |
" Preliminary results from 60 patients on PHT therapy (41 elderly, mean age 76 years; 19 younger adults, mean age 41 years) indicate that PHT bioavailability did not differ between the two age groups; however, absorption and elimination half-lives were more variable in the elderly patients." | ( Factors affecting antiepileptic drug pharmacokinetics in community-dwelling elderly. Birnbaum, AK; Cloyd, JC; Marino, S, 2007) | 0.34 |
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects." | ( Hologram QSAR model for the prediction of human oral bioavailability. Andricopulo, AD; Moda, TL; Montanari, CA, 2007) | 0.34 |
" Additionally, bioavailability of controlled-release relative to immediate-release tablets was assessed." | ( Population pharmacokinetic model of carbamazepine derived from routine therapeutic drug monitoring data. Grabnar, I; Miljković, B; Mrhar, A; Pokrajac, M; Velicković, R; Vucićević, K, 2007) | 0.61 |
"Carbamazepine and dipyridamole are class II compounds (BCS) whose oral bioavailability is limited by poor solubility." | ( Melt extrusion and spray drying of carbamazepine and dipyridamole with polyvinylpyrrolidone/vinyl acetate copolymers. Forster, AH; James, MB; Patterson, JE; Rades, T, 2008) | 2.07 |
" The bioavailability of CBZ formulations and Tegretol CR 200 were evaluated in beagle dogs." | ( Formulation, release characteristics and bioavailability study of oral monolithic matrix tablets containing carbamazepine. Almurshedi, AS; Barakat, NS; Elbagory, IM, 2008) | 0.56 |
" Carbamazepine (CBZ) is an anticonvulsant which is useful in controlling neuropathic pain, and it is currently administered by peroral route, although its absorption and bioavailability is limited due to various factors." | ( Carbamazepine transbuccal delivery: the histo-morphological features of reconstituted human oral epithelium and buccal porcine mucosae in the transmucosal permeation. Campisi, G; Florena, AM; Giannola, LI; Lo Muzio, L; Paderni, C; Saccone, R; Siragusa, MG; Tripodo, C, ) | 2.48 |
" Regardless of the differences observed in vitro, the predicted pharmacokinetic profiles were similar in the extent of drug exposure (AUC) while there were certain differences in parameters defining the drug absorption rate (C(max)t(max))." | ( Justification of biowaiver for carbamazepine, a low soluble high permeable compound, in solid dosage forms based on IVIVC and gastrointestinal simulation. Homsek, I; Kovacević, I; Langguth, P; Parojcić, J; Tubić-Grozdanis, M, ) | 0.42 |
" Piperine could significantly enhance the oral bioavailability of carbamazepine, possibly by decreasing the elimination and/or by increasing its absorption." | ( Pharmacokinetic interaction of single dose of piperine with steady-state carbamazepine in epilepsy patients. Hota, D; Kharbanda, P; Pandhi, P; Pattanaik, S; Prabhakar, S, 2009) | 0.82 |
" In conclusion, berberine produced a dose-dependent increased bioavailability of digoxin and cyclosporine A by inhibition of intestinal P-gp." | ( Effect of berberine on the pharmacokinetics of substrates of CYP3A and P-gp. Jiang, XH; Jin, JX; Ju, Y; Liu, CX; Qiu, W, 2009) | 0.35 |
" Results of our work suggest that P-glycoprotein (P-gp) overexpression by repetitive seizures induced by MP administration does not modify brain bioavailability of carbamazepine." | ( Differential hippocampal pharmacokinetics of phenobarbital and carbamazepine in repetitive seizures induced by 3-mercaptopropionic acid. Girardi, E; Gonzalez, NN; Höcht, C; Lazarowski, A; Mayer, MA; Opezzo, JA; Taira, CA, 2009) | 0.79 |
" Drug properties such as flowability, dissolution, hardness and bioavailability may be affected by crystallinity behaviours of drugs." | ( Improvement of physicomechanical properties of carbamazepine by recrystallization at different pH values. Javadzadeh, Y; Khoei, NS; Mohammadi, A; Nokhodchi, A, 2009) | 0.61 |
"Formation of a solid solution of a drug in a water-soluble polymer is one of the primary techniques used to improve the dissolution rate and thus bioavailability of a poorly water-soluble drug." | ( Nanoscale thermal analysis of pharmaceutical solid dispersions. Bunker, M; Chen, X; Parker, AP; Patel, N; Roberts, CJ; Zhang, J, 2009) | 0.35 |
" The AUC(tau,ss) and C(max,ss) point estimates (combined vs sole treatment) showed relative bioavailability of approximately 100% for both drugs." | ( No pharmacokinetic interaction between lacosamide and carbamazepine in healthy volunteers. Cawello, W; Eggert-Formella, A; Nickel, B, 2010) | 0.61 |
" SCY-635 was shown to be orally bioavailable in multiple animal species and produced blood and liver concentrations of parent drug that exceeded the 50% effective dose determined in the bicistronic con1b-derived replicon assay." | ( SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro. Erdmann, F; Fischer, G; Harris, R; Hopkins, S; Huang, Z; Murray, MG; Ribeill, Y; Scorneaux, B; Smitley, C; Wring, S, 2010) | 0.36 |
" Furthermore, current water quality monitoring does not differentiate between soluble and colloidal phases in water samples, hindering our understanding of the bioavailability and bioaccumulation of pharmaceuticals in aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" Such strong pharmaceutical/colloid interactions may provide a long-term storage of pharmaceuticals, hence, increasing their persistence while reducing their bioavailability in the environment." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" As aquatic colloids are abundant, ubiquitous, and highly powerful sorbents, they are expected to influence the bioavailability and bioaccumulation of such chemicals by aquatic organisms." | ( Colloids as a sink for certain pharmaceuticals in the aquatic environment. Maskaoui, K; Zhou, JL, 2010) | 0.36 |
" The relative bioavailability of S-SMEDDS formulation of CBZ was evaluated in beagle dogs compared with a commercial tablet." | ( Studies on preparation of carbamazepine (CBZ) supersaturatable self-microemulsifying (S-SMEDDS) formulation and relative bioavailability in beagle dogs. Jin, Y; Quan, DQ; Zhang, N; Zhang, W, 2011) | 0.67 |
" Piperine (20 mg/kg orally) was administered along with curcumin to enhance the bioavailability of the latter up to 20-fold more." | ( Antioxidant potential of curcumin against oxidative insult induced by pentylenetetrazol in epileptic rats. Jyothy, A; Munshi, A; Nehru, B; Sharma, V, 2010) | 0.36 |
"Since polymorphs exhibit differences in chemical and physicochemical stability, characteristics, and dissolution rate of the bulk powder, they may significantly affect on the bioavailability of pharmaceutical compounds." | ( Determination of carbamazepine polymorphic contents in double-layered tablets using transmittance- and reflectance-near-infrared spectroscopy involving chemometrics. Fukui, Y; Otsuka, M, 2010) | 0.7 |
" The overall absolute oral bioavailability of CBZ from N-Gly-CBZ was determined to be 41 ± 14% in three rats." | ( In vitro and in vivo evaluation of a novel water-soluble N-glycyl prodrug (N-GLY-CBZ) of carbamazepine. Hemenway, JN; Stella, VJ, 2010) | 0.58 |
" The bioavailability of such a drug is limited by the dissolution rate." | ( Impairment of the in vitro release of carbamazepine from tablets. Hadzidedić, S; Uzunović, A; Vranić, E, 2010) | 0.63 |
"The aim of the present study was to present new evidence supporting the use of saliva as a biological fluid in relative bioavailability studies." | ( The use of saliva as a biological fluid in relative bioavailability studies: comparison and correlation with plasma results. Conforti, P; Fagiolino, P; Ruiz, ME; Volonté, MG, 2010) | 0.36 |
" Carbamazepine interacts with zolpidem in healthy volunteers and lowers its bioavailability by about 57%." | ( Pharmacokinetic interaction between zolpidem and carbamazepine in healthy volunteers. Bâldea, I; Leucuţa, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011) | 1.53 |
"T Carbamazepine interacts with ivabradine in healthy volunteers, and lowers its bioavailability by about 80%." | ( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers. Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011) | 1.34 |
" Tablets of the resulting complex were prepared using direct compression method and the bioavailability was evaluated in beagle dogs using a UPLC/MS/MS method." | ( In vitro and in vivo evaluation of novel immediate release carbamazepine tablets: complexation with hydroxypropyl-β-cyclodextrin in the presence of HPMC. Cai, C; Kou, W; Liu, J; Wang, H; Xu, S; Yang, D; Zhang, T, 2011) | 0.61 |
" This study was performed to characterize the disposition of the two enantiomers of MHD after oral and intravenous administration and to estimate the bioavailability of MHD after a single oral dose administration of OXC compared to a single intravenous administration of MHD." | ( Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. Czendlik, C; Flesch, G; Lloyd, P; Renard, D, 2011) | 0.37 |
"The dissolution behavior and bioavailability of carbamazepine (CBZ) is rate-limited by formation of carbamazepine dihydrate (CBZ-D) in dissolution fluids." | ( Influence of Simulated Gastrointestinal Fluids on Polymorphic Behavior of Anhydrous Carbamazepine Form III and Biopharmaceutical Relevance. Bhise, SB; Rajkumar, M, ) | 0.61 |
" Several in vitro and in vivo studies have shown significant improvement in dissolution and bioavailability of CBZ." | ( Review of solubilization techniques for a poorly water-soluble drug: carbamazepine. Apte, S; Madhusudan Rao, Y; Pavan Kumar, M; Srawan Kumar, GY, ) | 0.37 |
" Separate absorption rate constants were modelled for the two formulations." | ( Population pharmacokinetics of steady-state carbamazepine in Egyptian epilepsy patients. Bewernitz, M; Derendorf, H; El Desoky, ES; Hamdi, MM; Sabarinath, SN, 2012) | 0.64 |
"Species differences in the oral pharmacokinetics and absolute bioavailability (F ( abs )) of carbamazepine polymorphs (form I and form III) and dihydrate were studied." | ( Pharmacokinetics of carbamazepine polymorphs and dihydrate in rats, related to dogs and humans. Cheng, G; Liu, Y; Ren, J; Tian, Y; Wang, Y; Xu, C; Yan, J; Zou, M, 2011) | 0.89 |
" Therefore, electrospray technology has the potential to produce pharmaceutical dosage forms with enhanced bioavailability and can readily be integrated in a continuous pharmaceutical manufacturing process." | ( Production and characterization of carbamazepine nanocrystals by electrospraying for continuous pharmaceutical manufacturing. Myerson, AS; Rutledge, GC; Trout, BL; Wang, M, 2012) | 0.66 |
" Compared with fast-release commercial carbamazepine tablets, drug release from the liquisolid capsules was greatly improved, and the bioavailability of the liquisolid preparation was enhanced by 182." | ( In vitro and in vivo evaluation of ordered mesoporous silica as a novel adsorbent in liquisolid formulation. Chen, B; Li, G; Pan, X; Peng, X; Quan, G; Wang, R; Wang, Z; Wu, C; Xu, Y, 2012) | 0.65 |
" Because the long-term management of epilepsy is attained by means of orally administered AEDs, investigation of their potential to be well absorbed at the intestinal level is mandatory." | ( Evaluation of the permeability and P-glycoprotein efflux of carbamazepine and several derivatives across mouse small intestine by the Ussing chamber technique. Alves, G; Falcão, A; Fortuna, A; Soares-da-Silva, P, 2012) | 0.62 |
" However, few studies have assessed the bioavailability of pharmaceuticals to fish in natural waters." | ( Bioavailability of pharmaceuticals in waters close to wastewater treatment plants: use of fish bile for exposure assessment. Brozinski, JM; Kronberg, L; Lahti, M; Oikari, A; Segner, H, 2012) | 0.38 |
" Moreover, the impact of body weight, absorption rate and co-therapy with other antiepileptic drugs (phenytoin, phenobarbital and valproic acid) on the dosage recommendation was investigated in the event of poor compliance." | ( The effect of poor compliance on the pharmacokinetics of carbamazepine and its epoxide metabolite using Monte Carlo simulation. Ding, JJ; Jiao, Z; Wang, Y; Zhang, YJ, 2012) | 0.62 |
" Patient body weight, absorption rate and co-therapy with phenytoin, phenobarbital and valproic acid had no significant impact on the dose recommendation." | ( The effect of poor compliance on the pharmacokinetics of carbamazepine and its epoxide metabolite using Monte Carlo simulation. Ding, JJ; Jiao, Z; Wang, Y; Zhang, YJ, 2012) | 0.62 |
" Gender differences were also observed for CBZ-10,11-epoxide concentration, being bioavailability the main parameter responsible for this difference." | ( Usefulness of salivary drug monitoring for detecting efflux transporter overexpression. Fagiolino, P; Lazarowski, A; Maldonado, C; Orozco-Suárez, S; Ruiz, ME; Vázquez, M; Volonté, MG, 2013) | 0.39 |
" Both CBZ and PHT would modify their bioavailability and clearance by inducing efflux transporter throughout chronic treatments, from the first dose to multiple dose administration." | ( Usefulness of salivary drug monitoring for detecting efflux transporter overexpression. Fagiolino, P; Lazarowski, A; Maldonado, C; Orozco-Suárez, S; Ruiz, ME; Vázquez, M; Volonté, MG, 2013) | 0.39 |
" Whereas, increased Cmax, absorption rate measured by the time to Cmax (Tmax), and prolongation of the terminal elimination half-life (T1/2) were observed after the co-administration with Lepidium sativum." | ( Lepidium sativum but not Nigella sativa affects carbamazepine disposition in an animal model. Al-Jenoobi, FI; Al-Mohizea, AM; Al-Suwayeh, SA; Alam, MA; Alkharfy, KM; Khan, RM; Korashy, HM; Muzaffar, I, 2013) | 0.65 |
" Age was a significant factor contributing to pharmacokinetic variability in individuals using LTG, OXC, and CBZ with increasing clearance as a function of bioavailability (Cl/F) over age 18, a maximum Cl/F at 33years (CBZ) and 36 years (LTG and OXC), and a gradual decrease of Cl/F towards older age." | ( The impact of age on lamotrigine and oxcarbazepine kinetics: a historical cohort study. Lindhout, D; Sander, JW; Wegner, I; Wilhelm, AJ, 2013) | 0.39 |
" When considering particularly the pharmacokinetics during the development of oral antiepileptic drugs (AEDs), one of the most prominent goals is designing compounds with good bioavailability and brain penetration." | ( Pharmacokinetics, brain distribution and plasma protein binding of carbamazepine and nine derivatives: new set of data for predictive in silico ADME models. Alves, G; Falcão, A; Fortuna, A; Soares-da-Silva, P, 2013) | 0.63 |
" Furthermore, comparisons of in vitro and in vivo data of MCC with a conventional product highlighted its capability to attain higher bioavailability and more controlled release trends." | ( In vivo and ex vivo evaluation of a multi-particulate composite construct for sustained transbuccal delivery of carbamazepine. Adeleke, OA; Choonara, YE; Du Toit, LC; Pillay, V, 2014) | 0.61 |
"The occurrence of polymorphic transitions is a serious problem for pharmaceutical companies, because it can affect the bioavailability of the final product." | ( Simultaneous quantification of three polymorphic forms of carbamazepine in the presence of excipients using Raman spectroscopy. Carneiro, R; Farias, M, 2014) | 0.65 |
" Increase in the bioavailability of both diclofenac and carbamazepine following multiple GFJ ingestion was revealed." | ( Evidence of reduced oral bioavailability of paracetamol in rats following multiple ingestion of grapefruit juice. Alhussainy, TM; Arafat, TA; Idkaidek, NM; Ismail, OA; Qinna, NA, 2016) | 0.68 |
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates." | ( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. Bharate, SS; Vishwakarma, RA, 2015) | 0.42 |
" These two groups had equivalent maximum drug concentration and bioavailability levels." | ( [Study of Preparation and Utility of Suppository Containing Carbamazepine Tablet for Hospital Use in Rabbits]. Arai, N; Fukushima, A; Inoue, Y; Kanamoto, I; Kimura, M; Murata, I; Saito, A, 2015) | 0.66 |
" Studies in albino rabbits show correspondingly better bioavailability of F1-F3 than Epitol." | ( The development of carbamazepine-succinic acid cocrystal tablet formulations with improved in vitro and in vivo performance. Hussain, I; Sun, CC; Ullah, M, 2016) | 0.76 |
"Transformation of the solid-state form of a drug compound in the lumen of the gastrointestinal tract may alter the drug bioavailability and in extreme cases result in patient fatalities." | ( Anhydrate to hydrate solid-state transformations of carbamazepine and nitrofurantoin in biorelevant media studied in situ using time-resolved synchrotron X-ray diffraction. Arnfast, L; Boetker, JP; Boyd, BJ; Doreth, M; Hawley, A; Khan, J; Loebmann, K; Madsen, C; Müllertz, A; Rades, T; Raijada, D; Rantanen, J; Thomas, D, 2016) | 0.68 |
" Due to their surface active properties, PC forms bilayers at the aqueous interface, thereby enabling encapsulated drug to benefit from better bioavailability and stability." | ( Identifying lipidic emulsomes for improved oxcarbazepine brain targeting: In vitro and rat in vivo studies. Awad, GA; El-Zaafarany, GM; Mansour, S; Soliman, ME, 2016) | 0.43 |
"The effect of single and multiple doses of a herbal preparation Trikatu was studied on the bioavailability and pharmacokinetics of carbamazepine in rabbits." | ( EFFECT OF TRIKATU, AN AYURVEDIC PRESCRIPTION ON THE PHARMACOKINETIC PROFILE OF CARBAMAZEPINE IN RABBITS. Bhargava, VK; Garg, SK; Karan, RS, 1999) | 0.74 |
" Upon exposure to carbamazepine at 1 μg/L, the hatching rate, body length, swim bladder appearance and yolk sac absorption rate were significantly increased." | ( Environmental concentration of carbamazepine accelerates fish embryonic development and disturbs larvae behavior. Cheng, J; Qiang, L; Rotchell, JM; Yi, J; Zhou, J; Zhu, X, 2016) | 1.05 |
" Oral bioavailability of carbamazepine in children is about 75-85%, and it is approximately 75-85% bound to plasma proteins." | ( Pharmacokinetics and Pharmacogenetics of Carbamazepine in Children. Djordjevic, N; Jankovic, SM; Milovanovic, JR, 2017) | 1.02 |
" Co-administration of verapamil resulted in a modest increase of the apparent bioavailability of oxcarbazepine by 12% (10-28), but did not affect parent or metabolite clearances." | ( Population pharmacokinetics of oxcarbazepine and its metabolite 10-hydroxycarbazepine in healthy subjects. Alexandre Junior, V; Antunes, NJ; Coelho, EB; Della Pasqua, O; Lanchote, VL; Takayanagui, OM; Tozatto, E; van Dijkman, SC; van Hasselt, JGC; Wichert-Ana, L, 2017) | 0.46 |
" In soils amended with biosolids and irrigated with TWW, the bioavailability of carbamazepine for plant uptake was moderately decreased as compared to plants grown in soils irrigated with TWW alone." | ( Composted biosolids and treated wastewater as sources of pharmaceuticals and personal care products for plant uptake: A case study with carbamazepine. Ben Mordechay, E; Chefetz, B; Chen, Y; Shenker, M; Tarchitzky, J, 2018) | 0.91 |
" Based on a phase I trial and pooled data from 2 open-label bioavailability studies comparing oral with IV dosing, there was no noted indication of loss of seizure control in patients switched to short-term replacement antiepileptic drug therapy with IV carbamazepine." | ( Intravenous Carbamazepine for Adults With Seizures. DeFalco, AP; Tillery, EE; Vickery, PB, 2018) | 1.04 |
"05) improvement in bioavailability of CBZ." | ( RELATIVE BIOAVAILABILITY STUDY OF SUCCINIC ACID COCRYSTAL TABLET AND MARKETED CONVENTIONAL IMMEDIATE RELEASE TABLET FORMULATION OF CARBAMAZEPINE 200 MG IN RABBITS. Hussain, I; Murtaza, G; Ullah, M, 2016) | 0.64 |
"83-fold improved bioavailability compared to conventional drug suspension and Tegretol™ suspension respectively." | ( Multifunctional carbamazepine loaded nanostructured lipid carrier (NLC) formulation. Abdel-Bakky, MS; Ali, HM; Badran, MM; Elmowafy, M; Ibrahim, HM; Shalaby, K, 2018) | 0.83 |
" Although these findings suggest that iron ions reduce the oral bioavailability of carbamazepine, the influence of confounders cannot be excluded." | ( Drug interactions with carbamazepine: An ever expanding list? Perucca, E, 2018) | 1.02 |
" Taking into consideration that GSH conjugation is, in general, a detoxification pathway, these results suggest that under hyperoxia/oxidative stress conditions the bioavailability of the parent drug may be compromised." | ( The first-line antiepileptic drug carbamazepine: Reaction with biologically relevant free radicals. Antunes, AMM; Charneira, C; Marques, MM; Martins, IL; Morello, J; Nunes, J; Pereira, SA; Telo, JP, 2018) | 0.76 |
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
" A PEG400-based formulation was studied for five doses of the lipophilic drug carbamazepine, accounting for biorelevant dissolution of the dose in the GIT, and in-vivo bioavailability in rats." | ( The solubility, permeability and the dose as key factors in formulation development for oral lipophilic drugs: Maximizing the bioavailability of carbamazepine with a cosolvent-based formulation. Beig, A; Dahan, A; Fine-Shamir, N; Miller, JM, 2020) | 0.99 |
" It is characterized by a variable bioavailability and by the presence of different polymorphs." | ( Use of calcium carbonate as an excipient for release of poorly water soluble drugs: The case of carbamazepine. Ambrogi, V; Bini, M; Corneli, C; Donnadio, A; Ricci, P, 2020) | 0.78 |
" The effects of small molecular weight carriers such as amino acids (glycine, L-threonine; L-lysine and aspartic acid) on solubilization and enhancing bioavailability of Carbamazepine (Car) were investigated and compared to the more known excipients cyclodextrins (β-CD, HPβ-CD and γ-CD)." | ( Comparative studies of the effects of novel excipients amino acids with cyclodextrins on enhancement of dissolution and oral bioavailability of the non-ionizable drug carbamazepine. Abdelkader, H; Abou-Taleb, HA; Fathalla, Z, 2020) | 0.95 |
" To defeat this issue, it was planned to develop polymeric liposome formulations that are using for their bioavailability and enhancer impact in oral epilepsy treatment." | ( Chitosan-coated liposome-containing carbamazepine and coenzyme Q10: design, optimization and evaluation. Sağıroğlu, AA, 2021) | 0.9 |
" The role of different physicochemical processes in bioaccumulation of carbamazepine in fruits is investigated through Global Sensitivity Analysis, which shows how soil hydraulic properties and soil solute sorption regulate transpiration streams and bioavailability of carbamazepine." | ( On the Use of Mechanistic Soil-Plant Uptake Models: A Comprehensive Experimental and Numerical Analysis on the Translocation of Carbamazepine in Green Pea Plants. Brunetti, G; Fér, M; Grabic, R; Klement, A; Kodešová, R; Nikodem, A; Šimůnek, J; Švecová, H, 2021) | 1.06 |
" Nevertheless, the oral absolute bioavailability of carbamazepine lies between 70 and 78% and both in vivo and in vitro data support the classification of carbamazepine as a highly permeable drug." | ( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Carbamazepine. Abrahamsson, B; Cristofoletti, R; Dressman, JB; García, MA; Groot, DW; Langguth, P; Mehta, M; Parr, A; Polli, JE; Shah, VP; Tomakazu, T, 2021) | 1.11 |
" Among these pollutants, the surface-active substances have been suggested to enhance the bioavailability of other ECs." | ( The effect of PFOs on the uptake and translocation of emerging contaminants by crops cultivated under soil and soilless conditions. Beltrán, EM; Fernández-Torija, C; García-Hortigüela, P; González-Doncel, M; Pablos, MV; Porcel, MÁ, 2021) | 0.62 |
"Carbamazepine (CBZ) is an antiepileptic drug having low bioavailability due to its hydrophobic nature." | ( Fabrication of Carbamazepine Cocrystals: Characterization, Amirzada, MI; Asad, MHHB; Hussain, I; Mannan, A; Shafique, M; Wasim, M, 2021) | 2.42 |
"Incorporating the amorphous drug in polymeric components has been demonstrated as a feasible approach to enhance the bioavailability of poorly water-soluble drugs." | ( Role of polymers in the physical and chemical stability of amorphous solid dispersion: A case study of carbamazepine. Bu, T; Li, J; Li, T; Pan, H; Wang, H; Yu, D; Zhang, X; Zhou, W, 2022) | 0.94 |
" The most common method to facilitate drug administration in dysphagia patients is to mix the powdered drug with a small amount of thickened water, however little is known about the effects of this method on in vivo bioavailability of drugs." | ( Do Thickening Agents Used in Dysphagia Diet Affect Drug Bioavailability? Erdem, ÇE; Eroğlu, H; Eylem, CC; Gökmen-Özel, H; Ilgaz, F; Nemutlu, E; Timur, SS, 2022) | 0.72 |
" 1-H-benzotriazole, carbamazepine, citalopram, lamotrigine, sucralose, tramadol, and venlafaxine (>80 % frequency of appearance in effluents) were assessed with respect to their bioavailability in soil as part of different scenarios of irrigation with reclaimed water following a qualitative approach." | ( Multiclass target analysis of contaminants of emerging concern including transformation products, soil bioavailability assessment and retrospective screening as tools to evaluate risks associated with reclaimed water reuse. Beretsou, VG; Fatta-Kassinos, D; Lundy, L; Manoli, K; Michael, C; Nika, MC; Revitt, DM; Sui, Q; Thomaidis, NS, 2022) | 1.04 |
"Reversible interactions between drugs and humic acid in water can be an important factor in determining the bioavailability and effects of these pharmaceuticals as micropollutants in the environment." | ( Preparation of entrapment-based microcolumns for analysis of drug-humic acid interactions by high-performance affinity chromatography. Hage, DS; Iftekhar, S; Poddar, S; Rauhauser, M; Snow, DD, 2023) | 0.91 |
" In this study, we integrated bioavailability measurements into persistence testing of pollutants in soil to show that it is the key to have a more realistic environmental risk assessment (ERA)." | ( Integrating bioavailability measurements in persistence testing of partially biodegradable organic chemicals in soil. Fernández-López, C; Hennecke, D; Ortega-Calvo, JJ; Posada-Baquero, R, 2024) | 1.44 |
The effect of once daily dosage of carbamazepine on fit frequency, electroencephalogram (EEG), behaviour and 24-hour drug levels were compared with those following 2 to 3 divided daily doses treatment.
Excerpt | Relevance | Reference |
---|---|---|
" The one statistically significant interaction found was that in which phenytoin dosage decreased plasma carbamazepine concentrations." | ( Interactions between anticonvulsants. Eadie, MJ; Lander, CM; Tyrer, JH, 1975) | 0.47 |
" A single daily dose of carbamazepine is insufficient; 2 doses per day are appropriate in most cases, but some patients may benefit from more frequent dosing to avoid side-effects." | ( Clinical pharmacokinetics of carbamazepine. Bertilsson, L, ) | 0.73 |
" Serum drug concentrations were measured during 4 dosing intervals, once before and 3 times after beginning carbamazepine." | ( Effects of carbamazepine on valproic acid kinetics in normal subjects. Bowdle, TA; Cutler, RE; Levy, RH, 1979) | 0.86 |
" The half-life for elimination was much shorter than those already described even in multiple dosing epileptic adult patients." | ( Pharmacokinetics of carbamazepine in the neonate and in the child. Aicardi, J; d'Athis, P; de Lauture, D; Dulac, O; Olive, G; Rey, E, 1979) | 0.58 |
" In all three patients carbamazepine was introduced and gradually increased to a maximum dosage of 25 mg/kg of body weight per day." | ( Dystonia associated with carbamazepine administration: experience in brain-damaged children. Crosley, CJ; Swender, PT, 1979) | 0.87 |
"Carbamazepine concentrations in plasma during repetitive oral dosing were analyzed by means of a nonlinear, variable parameter, regression program (VARPARM) assuming dose-to-dose changes in the apparent elimination rate constant of the drug." | ( Time course of carbamazepine self-induction. Colburn, WA; Gibaldi, M; McNamara, PJ, 1979) | 2.06 |
"The applicability of a pharmacokinetic model for drug interactions by enzyme induction was tested by chronic dosing situation using carbamazepine (Tegretol) as the inducer and clonazepam (Clonopin) as the drug affected." | ( Time-course of interaction between carbamazepine and clonazepam in normal man. Cutler, RE; Lai, AA; Levy, RH, 1978) | 0.74 |
" Monitoring plasma concentrations may lead to adaptations of the choice of the drug and of the dosage regimen." | ( Kinetics of drug interactions in the treatment of epilepsy. Guelen, P; Knop, H; Schobten, F; van der Kleijn, E; Vree, T; Westenberg, H, 1978) | 0.26 |
" The nystagmus disappeared when phenytoin dosage was reduced." | ( Downbeat nystagmus due to anticonvulsant toxicity. Alpert, JN, 1978) | 0.26 |
" Blood levels of primidone decreased during pregnancy and rose postpartum requiring dosage adjustments." | ( Carbamazepine levels in pregnancy and lactation. Blake, DA; Freeman, JM; Luff, RD; Niebyl, JR, 1979) | 1.7 |
" In the literature, most cases of leukopenia secondary to carbamazepine are transient and benign, but any increase in dosage of the drug warrants a close follow-up of blood counts even if previous blood counts were normal." | ( Severe leukopenia secondary to carbamazepine administration. Gerber, JG; Nies, AS; Stiles, G, 1979) | 0.79 |
" The initial dosage of 6 mg/kg DPH or 15 mg/kg CARB was corrected according to the serum values aiming at therapeutic intervals of 8-16 mg/1 DPH and 6-10 mg/1 CARB." | ( A comparative controlled study between carbamazepine and diphenylhydantoin in psychomotor epilepsy. Kühl, V; Lund, M; Olsen, PZ; Simonsen, N; Wendelboe, J, 1976) | 0.52 |
" Combined treatment with other anticonvulsant drugs decreases the half-life and more frequent dosing may be necessary." | ( Clinical pharmacokinetics of anticonvulsants. Dam, M; Hvidberg, EF, 1976) | 0.26 |
" Reduction in antiepileptic drug dosage should be carried out as a stepwise procedure over a period of about 2 years." | ( [A discussion of the curability of childhood epilepsies (author's transl)]. Groh, C, 1975) | 0.25 |
" As the patient acquires greater tolerance the dosage may be gradually increased." | ( Adverse reactions to carbamazepine (tegretol). Al-Ubaidy, SS; Nally, FF, 1976) | 0.57 |
" The presence of immunological defects was independent of the dosage of drug, its serum concentration, the duration of therapy and the sex of the subject." | ( Depression of immune competence by phenytoin and carbamazepine. Studies in vivo and in vitro. Forbes, IJ; Sorrell, TC, 1975) | 0.51 |
" This combined drug therapy proved effective in all three cases: the good antidiuretic effect of chlorpropamide at high dosage is impaired by hypoglycaemia; the combination of carbamazepine allowed the dosage of chlorpropamide to be decreased without impairment of the obtained antidiuretic effect and with avoidance of hypoglycaemia and other side effects." | ( [Treatment of central diabetes insipidus with a combination of chlorpropamide and carbamazepine (author's transl)]. Stögmann, W, 1975) | 0.67 |
" On the basis of these considerations and clinical reports describing the use of these drugs, we make dosage recommendations to enable the practitioner to individualize therapeutic regimens." | ( Drugs used in the management of trigeminal neuralgia. Patsalos, PN; Zakrzewska, JM, 1992) | 0.28 |
" Neither dosage nor serum levels of CBZ were in a higher range." | ( Asterixis induced by carbamazepine therapy. Leblhuber, F; Rittmannsberger, H, 1992) | 0.6 |
" Tegretol commercial tablets were dosed according to previously established clinical regimens of 400 to 2000 mg daily doses divided into four equal or unequal intervals." | ( Comparative bioavailability and steady state fluctuations of Tegretol commercial and carbamazepine OROS tablets in adult and pediatric epileptic patients. Garnett, WR; Kochak, GM; Levy, RH; Mangat, S; Thakker, KM, 1992) | 0.51 |
" The usual phenytoin (PHT) dosage in adults is 4-6 mg/kg per day, but children may need a dosage three to five times higher." | ( Metabolism of antiepileptic medication: newborn to elderly. Leppik, IE, 1992) | 0.28 |
"A patient with epilepsy controlled by carbamazepine developed a carbamazepine neurotoxic reaction after being given an increased dosage of diltiazem hydrochloride as adjunctive therapy." | ( Carbamazepine neurotoxic reaction after administration of diltiazem. Grossman, E; Maoz, E; Rosenthal, T; Thaler, M, 1992) | 2 |
" At the end of the study, all but one of the children (and their parents) opted to receive CBZ-CR for ease of dosage administration and overall satisfaction." | ( Carbamazepine (CBZ) controlled release compared with conventional CBZ: a controlled study of attention and vigilance in children with epilepsy. Brouwer, OF; Edelbroek, PM; Heyer, A; Jennekens-Schinkel, A; Lanser, JB; Liauw, L; Peters, AC; Pieters, MS; Stijnen, T, ) | 1.57 |
" After reaching steady-state conditions by repeated administration of warfarin, the prothrombin time (Quick value) was assessed before and after single (600 mg) and multiple dosing (450 mg twice daily in 1 week) of OCBZ." | ( Oxcarbazepine does not affect the anticoagulant activity of warfarin. Klosterskov Jensen, P; Krämer, G; Menge, GP; Stoll, KD; Tettenborn, B, ) | 0.13 |
" The result showed that both drugs were effective in most cases at modest dosage without causing notable psychological effects 12 months into treatment." | ( Psychological effects of sodium valproate and carbamazepine in epilepsy. Stores, G; Styles, E; Williams, PL; Zaiwalla, Z, 1992) | 0.54 |
" Regular 2 weekly follow up for a minimum period of 2 months was done, after altering the drug dosage and bringing plasma level(s) within therapeutic range." | ( "An analysis of epileptic patients nonresponsive to drugs". Joshi, MV; Karande, SC; Kshirsagar, NA; Shah, PU, 1992) | 0.28 |
" A good relationship was found between the in vivo parameters and the in vitro dissolution results for the four dosage forms." | ( The bioinequivalence of carbamazepine tablets with a history of clinical failures. Jarvi, EJ; Meyer, MC; Pelsor, FR; Shah, VP; Straughn, AB; Wood, GC, 1992) | 0.59 |
" Significant clinical tolerance to side effects developed within 20 to 33 h after CBZ-CR dosage during a period in which the mean CBZ blood levels remained virtually unchanged." | ( Effect of acute doses of controlled-release carbamazepine on clinical, psychomotor, electrophysiological, and cognitive parameters of brain function. Bartel, PR; Becker, P; Blom, M; Erasmus, S; Griesel, D; Sommers, DK; van der Meyden, CH, ) | 0.39 |
" Each patient received 90-day supplies of Epitol or Tegretol and placebo, which replaced the usual dosage of the alternate product." | ( Therapeutic bioequivalency study of brand name versus generic carbamazepine. Anderson, RL; Dean, JC; Oles, KS; Penry, JK; Riela, AR; Smith, LD, 1992) | 0.52 |
" In particular, the TTV values were virtually unaffected by OXC administration, while the effects of CBZ on both variables were particularly evident at 8 and 10 h after dosing which correspond to the time at which the plasma concentrations of CBZ and of its 10,11-epoxide reach the peak." | ( Effects of oxcarbazepine and carbamazepine on the central nervous system: computerised analysis of saccadic and smooth-pursuit eye movements. Gangemi, PF; Massi, S; Messori, A; Monza, GC; Parigi, A; Valenza, T; Zaccara, G, 1992) | 0.57 |
" After a 4-week baseline period, patients were treated for 4 weeks with weekly ADD 94057 dosage escalations." | ( Pharmacokinetic and dose tolerability study of ADD 94057 in comedicated patients with partial seizures. Cereghino, JJ; Laxer, KD; Manning, LW; McCormick, C; Pledger, GW; Sahlroot, JT; Taylor, MR; Whitley, L, ) | 0.13 |
"In 3 patients the addition of fluvoxamine to a constant dosage of carbamazepine (CZP) caused a substantial rise of plasma CZP accompanied by symptoms of intoxication." | ( Interaction between carbamazepine and fluvoxamine. Fritze, J; Lanczik, M; Unsorg, B, 1991) | 0.84 |
" CBZ absorption can also be somewhat altered in children and may be related in part to the dosage form used in small children." | ( Carbamazepine dosing for pediatric seizure disorders: the highs and lows. Gilman, JT, 1991) | 1.72 |
" A dosing schedule for CBZ administration has been proposed with administration of 75% of the maintenance dose during the first week and the full CBZ maintenance dose from the beginning of the second week of CBZ therapy." | ( Changes in carbamazepine plasma concentrations in psychiatric patients during treatment. Kanarkowski, R; Lehmann, W; Matkowski, K; Rybakowski, J, ) | 0.52 |
" Plasma concentrations of paroxetine at steady state (8-147 ng/ml) were in the normal range for a 30-mg daily dosing regimen." | ( No influence of the antidepressant paroxetine on carbamazepine, valproate and phenytoin. Andersen, BB; Dam, M; Kristensen, HB; Lund, J; Mengel, H; Mikkelsen, M; Pedersen, B; Vesterager, A, ) | 0.39 |
" Carbamazepine in moderate dosage adversely affected memory, but sodium valproate and phenytoin did not." | ( Cognitive impairment in new cases of epilepsy randomly assigned to carbamazepine, phenytoin and sodium valproate. Berg, I; Butler, R; Forsythe, I; McGuire, R, 1991) | 1.43 |
"01) in serum CBZ concentration were substantially less with CBZ-CR and were similar to those calculated during a 6 or 8 hourly dosage interval with conventional CBZ (fluctuation 33 +/- 3%, variation 42 +/- 5%)." | ( Monotherapy with conventional and controlled-release carbamazepine: a double-blind, double-dummy comparison in epileptic patients. Blacklaw, J; Brodie, MJ; Butler, E; Gillham, RA; McKee, PJ, 1991) | 0.53 |
" Only one subject tolerated discontinuation of CBZ; the other three had dosage reductions of 33, 54, and 63%." | ( Discontinuation of phenytoin and carbamazepine in patients receiving felbamate. Graves, NM; Holmes, GB; Leppik, IE; Marienau, K; Remmel, RP; Wagner, ML, ) | 0.41 |
"We describe the case of a 26 years old woman in chronic therapy with phenobarbital, carbamazepine, valproic acid (VPA) and clonazepam who showed a hyperammonemic encephalopathy after an increase in dosage of VPA." | ( State of stupor from valproic acid during chronic treatment: case report. Buffa, C; Gentile, S; Ravetti, C; Sacerdote, I, 1991) | 0.51 |
" Steady-state trough CBZ serum concentrations, CBZ dosing history, concomitant drug administration, and other data from 45 patients were collected retrospectively." | ( Postinduction carbamazepine clearance in an adult psychiatric population. Crismon, ML; Godley, PJ; Martin, ES, 1991) | 0.64 |
" The mean felbamate dosage was 2,300 mg/d." | ( Felbamate for partial seizures: results of a controlled clinical trial. Bertram, E; Cereghino, JJ; Dreifuss, FE; Drury, I; Graves, NM; Jacobs, MP; Leppik, IE; Pledger, GW; Santilli, N; Tsay, JY, 1991) | 0.28 |
" In order to use these effectively, the critical care nurse must be aware of the indications and controversies surrounding their use, the patho-physiologic conditions that impact on the disposition, and appropriate dosing and monitoring of these agents in the critical care setting." | ( Anticonvulsants: pharmacotherapeutic issues in the critically ill patient. Dupuis, RE; Miranda-Massari, J, 1991) | 0.28 |
" CBZ and Li were given for four weeks using a fixed-flexible method at an equipotent dose ratio of 1:1, starting from an initial dosage of 400 mg with a maximum dosage of 1200 mg." | ( Comparison of the antimanic efficacy of carbamazepine and lithium carbonate by double-blind controlled study. Hazama, H; Inanaga, K; Itoh, H; Okuma, T; Otsuki, S; Sarai, K; Takahashi, R; Watanabe, S; Yamashita, I, 1990) | 0.55 |
" Phenytoin (PHT) dosage had to be increased in 85% of pregnancies in which the drug was received, carbamazepine (CBZ) dosage in 70%, and phenobarbital (PB) or methylphenobarbital (MPB) dosage in 85%, in an attempt to prevent or correct a fall in plasma concentrations of the respective drugs as pregnancy progressed." | ( Plasma antiepileptic drug concentrations during pregnancy. Eadie, MJ; Lander, CM, ) | 0.35 |
"The inhibitory effect of stiripentol (STP) on disposition of carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZE) was quantitated to establish CBZ dosage reduction guidelines for future clinical add-on efficacy trials of STP." | ( Carbamazepine dose requirements during stiripentol therapy: influence of cytochrome P-450 inhibition by stiripentol. Eddy, AC; Kerr, BM; Levy, RH; Martinez-Lage, JM; Tor, J; Viteri, C, ) | 1.82 |
" dosing schedule of the controlled-release (CR) preparation without a detrimental effect on seizure frequency or adverse effects." | ( A comparison of the efficacy and tolerability of controlled-release carbamazepine with conventional carbamazepine. Bruni, J; Dhalla, Z; Sutton, J, 1991) | 0.52 |
" The most common adverse effects are neurological and dose-related, and occur in up to 50% of patients treated, usually on dosage initiation or dose elevation." | ( Risk-benefit assessment of carbamazepine in children. Pellock, JM; Seetharam, MN, ) | 0.43 |
" The daily dosage of 50 mg/kg (maximum 3,000 mg) FBM per day was well tolerated by all 28 patients who completed the study." | ( Felbamate: a clinical trial for complex partial seizures. Balish, M; Bromfield, E; Devinsky, O; Ito, B; Nice, F; Porter, RJ; Raubertas, RF; Reeves, P; Theodore, WH, ) | 0.13 |
" In order to define the minimal dosage of fentanyl required, the MD was titrated according to increases or decreases in the heart rate and/or mean arterial pressure exceeding 15 per cent of baseline ward values." | ( Anticonvulsant therapy increases fentanyl requirements during anaesthesia for craniotomy. Modica, PA; Spitznagel, EL; Tempelhoff, R, 1990) | 0.28 |
" Blood and urine samples in the studies were collected during a dosing interval at steady state." | ( Effects of polytherapy with phenytoin, carbamazepine, and stiripentol on formation of 4-ene-valproate, a hepatotoxic metabolite of valproic acid. Acheampong, A; Anderson, GD; Baillie, TA; Friel, PN; Guyot, M; Levy, RH; Loiseau, P; Rettenmeier, AW; Tor, J; Wilensky, AJ, 1990) | 0.55 |
" Individual dosage adjustment is preferably based on clinical judgment rather than on published therapeutic ranges." | ( [High-dose monotherapy in intractable epilepsy]. Peng, SM; Wu, JZ, 1990) | 0.28 |
" The twice-a-day dosage should result in better compliance and consequently in a better quality of treatment in the long term." | ( [Comparative open trial of carbamazepine and slow-release carbamazepine in epilepsy in adults]. Remy, C, 1990) | 0.58 |
" This article reviews the indications, dosing regimens, and potential side effects of the drugs used for the treatment of trigeminal and glossopharyngeal neuralgia, posttherapeutic neuralgia, temporal arteritis, and migraine based on the clinical pharmacology of these drugs, so that the most appropriate treatment for each patient can be chosen on a sound, rational basis." | ( Clinical pharmacology of drugs used to treat head and face pain. Fromm, GH, 1990) | 0.28 |
" The daily dose and dosing frequency of CBZ were kept the same as before the study." | ( Differences in side effects between a conventional carbamazepine preparation and a slow-release preparation of carbamazepine. Ben-Menachem, E; Bengtsson, E; Heinonen, E; Persson, LI, 1990) | 0.53 |
" The serum levels for effective and safe dosage have been determined when these drugs are used alone." | ( Avoiding neurotoxicity with lithium-carbamazepine combinations. Hollister, LE; Kishimoto, A; McGinness, J, 1990) | 0.55 |
" Vegetative and neurotoxic effects most commonly occur in the beginning of therapy, after increasing the dosage and in case of intoxication." | ( [Carbamazepine in the treatment of psychiatric diseases: effects and side effects]. Rittmannsberger, H, 1990) | 1.19 |
" The imipramine dosage was significantly higher in the combined treatment group than in the imipramine-only group." | ( Possible influence of carbamazepine on plasma imipramine concentrations in children with attention deficit hyperactivity disorder. Brown, CS; Cold, JA; Froemming, JH; Jabbour, JT; Self, TH; Wells, BG, 1990) | 0.59 |
" Eighty-four patients had been established on treatment with a single anticonvulsant drug (35 carbamazepine (CBZ), 30 sodium valproate (VPA), 19 phenytoin (PHT)) at unaltered dosage for the previous 3 months." | ( Cognitive function in adult epileptic patients established on anticonvulsant monotherapy. Brodie, MJ; Butler, E; Gillham, RA; Larkin, JG; Wiedmann, KD; Williams, N, 1990) | 0.5 |
" These findings should therefore be considered when defining dosage regimens or interpreting serum drug concentrations." | ( Analysis of the factors influencing anti-epileptic drug concentrations--valproic acid. Aoyama, T; Higuchi, S; Hirata, K; Ieiri, I; Yamada, H, 1990) | 0.28 |
"The teratogenicity of carbamazepine (CBZ) was investigated in Sprague-Dawley CD rats at doses of 0, 200, 400, and 600 mg/kg administered by gavage in corn oil on days 7-18 of gestation in a dosage volume of 2 ml/kg." | ( Teratogenicity of carbamazepine in rats. Acuff, KD; Minck, DR; Vorhees, CV; Weisenburger, WP, 1990) | 0.93 |
" During a dosing interval, no significant differences were observed with respect to trough or peak serum concentrations of CBZ and CBZ-10,11-epoxide (CBZ-E), the active metabolite." | ( A comparative pharmacokinetic study of conventional and chewable carbamazepine in epileptic patients. Patsalos, PN, 1990) | 0.52 |
" We conclude that the AccuLevel assay is a simple, reliable method for determining CBZ concentration in a small volume of whole blood and is an acceptable alternative for assessment of CBZ therapy and individualization of CBZ dosage in the physician's office or emergency room." | ( Comparison of a noninstrumented immunoassay for carbamazepine to high performance liquid chromatography and fluorescence polarization immunoassay. Cochran, EB; Cramer, JA; Denio, LS; Drake, ME; Massey, KL; Phelps, SJ; Toftness, BR, ) | 0.39 |
" Dosing was single blind." | ( Carbamazepine-10,11-epoxide in epilepsy. A pilot study. Almkvist, O; Bertilsson, L; Nilsson, BY; Svensson, JO; Tomson, T, 1990) | 1.72 |
" Mean VPA dosage was 16." | ( The effect of carbamazepine on valproic acid disposition in adult volunteers. Abbott, FS; Burton, RW; Farrell, K; Kassahun, K; Orr, JM; Panesar, SK, 1989) | 0.64 |
" The technique is simple and rapid: 4 anticonvulsants are simultaneously extracted and dosed, valproic acid, only has to be dosed lonely." | ( [Plasma determination of 7 common drugs by high performance liquid chromatography]. Baty, C; Jambou, J; Leducq, B; Richard, L, 1989) | 0.28 |
"The in vitro recovery of three different dosage forms of carbamazepine (CBZ) when dispersed in gastric or intestinal fluids, in the presence or absence of Ensure was determined." | ( In vitro recovery of carbamazepine from ensure. Friesen, E; Kassam, RM; Locock, RA, ) | 0.7 |
" When the drug was repeatedly coadministered with DPH or CBZ, the initial VPA elimination from plasma up to 1 h after dosing was less than with VPA alone, while PB significantly enhanced the disappearance of VPA." | ( Effects of anticonvulsants on plasma levels and entero-hepatic circulation of valproic acid and on hepatic drug metabolizing enzyme activities in rats. Horibe, Y; Ito, Y; Iwaki, M; Ogiso, T; Yoneda, I, 1989) | 0.28 |
" We report here the results of dose-response studies (0." | ( In vitro effect of lithium on carbamazepine-induced inhibition of murine and human bone marrow-derived granulocyte-macrophage, erythroid, and megakaryocyte progenitor stem cells. Gallicchio, VS; Hulette, BC, 1989) | 0.57 |
" The dose-response curve of PHT was described as a first-order reaction with Kd = 37 microM; 100 microM CBZ was equally as effective 100 microM PHT." | ( Phenytoin and carbamazepine: potential- and frequency-dependent block of Na currents in mammalian myelinated nerve fibers. Grigat, G; Schwarz, JR, ) | 0.49 |
" However, the effect of carbamazepine (100 microM) on the respective dose-response curves suggests that the mechanism of inhibition of the carbachol response differs from the inhibition of the histamine and veratrin responses." | ( Inhibition of agonist-stimulated inositol lipid metabolism by the anticonvulsant carbamazepine in rat hippocampus. Logan, SD; McDermott, EE, 1989) | 0.81 |
" These results support the increased use of dosing aids for PHT that may help clinicians more accurately choose PHT doses and estimate time to steady state." | ( Dosing accuracy of antiepileptic drug regimens as determined by serum concentrations in outpatient epilepsy clinic patients. Privitera, MD, 1989) | 0.28 |
" All patients required a PHT dosage decrease of 10-30% during active FBM treatment to maintain stable concentrations." | ( Effect of felbamate on phenytoin and carbamazepine serum concentrations. Fuerst, RH; Graves, NM; Holmes, GB; Leppik, IE, ) | 0.4 |
" After 2 weeks' treatment, CBZ daytime levels measured as area under the concentration-time curve over a dosage interval were 7% lower with CBZ-CR, but this difference was not statistically significant." | ( A double-blind comparison of conventional and controlled-release carbamazepine in healthy subjects. Brodie, MJ; Butler, E; Larkin, JG; McLellan, A; Munday, A; Sutherland, M, 1989) | 0.51 |
" In all cases, the pimozide dosage was progressively reduced until the minimal effective dose was reached." | ( Pimozide therapy for trigeminal neuralgia. Acosta, E; Amat, J; Arocha, L; Cabrera, A; Gómez, F; Lechin, AE; Lechin, F; Lechin, ME; van der Dijs, B; Villa, S, 1989) | 0.28 |
" VPA was started in increasing dosage until infantile spasms were controlled or a maximum dose of 100 mg/kg/day was reached." | ( Therapy of infantile spasms with valproate: results of a prospective study. Michael, T; Nau, H; Siemes, H; Spohr, HL, ) | 0.13 |
" Two patients with mild symptoms were rechallenged with a lower verapamil dosage (120 mg twice a day) and showed similar rises in CBZ concentration and recurrent neurotoxic symptoms." | ( Verapamil potentiates carbamazepine neurotoxicity: a clinically important inhibitory interaction. Brodie, MJ; Macphee, GJ; McInnes, GT; Thompson, GG, 1986) | 0.59 |
" Frequency and extent of increased activity of gamma-GT were highly related to daily dosage in both preparations." | ( The influence of long-term anticonvulsant therapy with diphenylhydantoin and carbamazepine on serum gamma-glutamyltransferase, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase. Aldenhövel, HG, 1988) | 0.5 |
" Frequency and extent of increased activity of gamma-GT were highly related to daily dosage in both preparations." | ( [Altered gamma-glutamyltransferase, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase serum activities in long-term anticonvulsive therapy--comparison of diphenylhydantoin and carbamazepine]. Aldenhövel, HG, 1988) | 0.46 |
" Serum concentration values obtained after 1 week of monotherapy, using our dosing regimen, can be used to predict directly the dosing rate needed to obtain a specific serum concentration in most patients." | ( Time course of carbamazepine autoinduction. The VA Cooperative Study No.118 Group. Browne, TR; Collins, JF; Mikati, MA, 1989) | 0.63 |
"Most of the side effects associated with carbamazepine (Tegretol, USP, Geigy Pharmaceuticals) therapy are mild, transient, and reversible with an adjustment in dosage or rate of dosage increase." | ( Carbamazepine side effects in children and adults. Pellock, JM, 1987) | 1.98 |
" We report on a case of cardiac arrhythmia during low dosage therapy of post-herpetic neuralgia with Carbamazepine and Amitriptyline in a patient with chronic renal rejection and cirrhosis." | ( [Acute cardiotoxicity of tricyclic compounds: remarks on a clinical case]. Arisi, L; Paganelli, E, 1988) | 0.49 |
"The aim of the present work was to assess the forecasting efficiency of methods of dosage individualization for carbamazepine according to mean population pharmacokinetic parameters (method 1) and from information relating to one (method 2) or more (method 3) measured steady-state serum drug levels in 344 epileptic patients." | ( Contribution of serum level monitoring in the individualization of carbamazepine dosage regimens. Alonso Gonzalez, AC; Dominguez-Gil Hurle, A; Garcia Sanchez, MJ, 1988) | 0.72 |
"Safety and efficacy studies of new antiepileptic drugs require strict adherence to prescribed dosage regimens." | ( Compliant populations: variability in serum concentrations. Graves, NM; Holmes, GB; Leppik, IE, 1988) | 0.27 |
" In the case of diazepam, clonazepam, ethosuximide or trimethadione, the TE/TF ratio was decreased dose-dependently, but the slope of the dose-response regression line was less steep than that obtained by the administration of PB, PNT, CBZ, VPA or primidone." | ( [The correlation between concentrations of anticonvulsive drugs in the brain and various parameters of maximal electroshock seizures in mice]. Kishita, C, 1986) | 0.27 |
" The two cortical sites were distinguished by significantly different dose-response curve slopes for the suppression of afterdischarge duration by PHT, CBZ and VPA, which suggests more than one mechanism of action for these drugs." | ( Differential antiepileptic sensitivity between cortical sites in the rat. Iragui, VJ; Kalichman, MW; Moss, KA, ) | 0.13 |
" Based on these observations, suggestions have been made for rescheduling the dosage of the drug in PEM." | ( Pharmacokinetics of carbamazepine in protein energy malnutrition. Bano, G; Raina, RK; Sharma, DB, 1986) | 0.59 |
" One group (n = 6) received sodium valproate (1,100 mg/day) for 2 weeks, while the other group (n = 6) was given, for the same period, a dosage of VPM (1,200 mg/day) expected to produce VPA levels equivalent to those achieved with valproate." | ( Sodium valproate and valpromide: differential interactions with carbamazepine in epileptic patients. Fazio, A; Gitto, C; Oteri, G; Perucca, E; Pisani, F; Ruello, C; Russo, F, ) | 0.37 |
" The incidence of side effects was similar in both treatment groups, and side effects generally responded well to dosage reduction." | ( The comparative efficacy and safety of carbamazepine versus lithium: a randomized, double-blind 3-year trial in 83 patients. Akiskal, HS; Cassano, GB; Lazzerini, F; Lenzi, A; Placidi, GF, 1986) | 0.54 |
" The latter must be compensated for by planned dosage increases to maintain therapeutic plasma steady-state levels during the first 2 or 3 months of treatment." | ( Carbamazepine efficacy in adults with partial and generalized tonic-clonic seizures. Rangel, R; Wilder, BJ, 1987) | 1.72 |
" We founded a good relationship between PRI dosage and PB plasma levels." | ( [Usefulness of the evaluation of plasma levels of primidone and phenobarbital]. Franzoni, E; Govoni, M; Mambelli, M; Masoni, P, ) | 0.13 |
" In response to the effects of enzyme induction, valproate dosage may need to be doubled to maintain therapeutic serum levels." | ( Pharmacologic interactions between valproate and other drugs. Bourgeois, BF, 1988) | 0.27 |
" In each patient, the average unbound fraction for a dosing interval increased with increase in sodium valproate dose." | ( Changes in clearance of sodium valproate with changes in dose. Bury, RW; Fullinfaw, RO; Kilpatrick, CJ; Moulds, RF, 1987) | 0.27 |
"This preliminary clinical study describes the pharmacokinetic characteristics of flunarizine (FLN) following single and multiple dosing in epileptic patients receiving comedication." | ( Pharmacokinetic profile of flunarizine after single and multiple dosing in epileptic patients receiving comedication. Barber, K; Cereghino, JJ; Di Giorgio, C; Kapetanovic, IM; Kupferberg, HJ; Lau, M; Norton, L; Torchin, CD; Treiman, DM; Whitley, L, ) | 0.13 |
" By using Neurotol slow instead of a conventional CBZ preparation, Tegretol, it is evidently possible to reduce the dosing frequency from 3 times a day to twice daily administrations." | ( Reduction of dosing frequency of carbamazepine with a slow-release preparation. Anttila, M; Heinonen, E; Järvensivu, P; Lehto, H; Riekkinen, P; Sivenius, J; Ylinen, A, ) | 0.41 |
"The aim of the present work was to analyse the predictive capacity of different optimization methods for carbamazepine dosage regimens according to population pharmacokinetic parameters and/or serum levels data." | ( Comparison of methods of carbamazepine dosage, individualization in epileptic patients. Alonso, AC; Dominguez-Gil, A; Garcia, MJ; Matesanz, C; Maza, A; Santos, D, 1988) | 0.79 |
" However, carbamazepine dosage must be carefully monitored because low initial doses are equivalent to higher later doses, and the drug's addition to a regimen of other drugs may increase carbamazepine's serum levels." | ( Fundamentals of carbamazepine use in neuropsychiatry. Neppe, VM; Tucker, GJ; Wilensky, AJ, 1988) | 1.02 |
" Also, dosage requirements increase in the presence of other drugs that are enzyme inducers." | ( Clinical pharmacokinetics of carbamazepine. Kerr, BM; Levy, RH, 1988) | 0.57 |
" Saturation, or zero-order, kinetics accounts for nonlinear increases in drug concentration with dosage increase." | ( Clinically significant carbamazepine drug interactions: an overview. Pippenger, CE, 1987) | 0.58 |
" Aspects of monitoring, such as range of therapeutic plasma levels, dosage regimen and adverse effects, are discussed." | ( Lithium in depression: a review of the antidepressant and prophylactic effects of lithium. Johnson, GF, 1987) | 0.27 |
" These results suggest that flurithromycin can inhibit the conversion of CBZ to CBZ-E, although, at the dosage tested, the magnitude of this effect was significantly smaller than that observed after administration of erythromycin in the same subjects." | ( Effect of flurithromycin, a new macrolide antibiotic, on carbamazepine disposition in normal subjects. Amione, C; Barzaghi, N; Crema, F; Faja, A; Gatti, G; Leone, L; Monteleone, M; Perucca, E, 1988) | 0.52 |
" Dosage of both drugs was within the usual range." | ( Carbamazepine and benzodiazepines in combination--a possibility to improve the efficacy of treatment of patients with 'intractable' infantile spasms? Groh, C; Lischka, A; Müller, R; Tatzer, E, 1987) | 1.72 |
" In some patients, with pronounced fluctuation of plasma concentrations during the dosage interval, side effects may be avoided by more frequent dosing." | ( Clinical pharmacokinetics and pharmacological effects of carbamazepine and carbamazepine-10,11-epoxide. An update. Bertilsson, L; Tomson, T, ) | 0.38 |
" The toxicity resolved when the carbamazepine dosage was decreased 62 percent." | ( Elevated serum carbamazepine concentrations following diltiazem initiation. Carter, BL; Eimer, M, 1987) | 0.91 |
" Differences in CBZ and CBZ-E disposition between day and night dosing were minor." | ( Intradose and circadian variation in circulating carbamazepine and its epoxide in epileptic patients: a consequence of autoinduction of metabolism. Brodie, MJ; Butler, E; Macphee, GJ, ) | 0.39 |
"Evaluating in 62 children aged from 4 months to 14 years (mean age 3 years 7 months) the correlation between the carbamazepine dosage (carbamazepine was given as the only drug in 21 cases, and as one of several drugs in 41) the authors failed to find a simple correlation." | ( [Carbamazepine dosage and its blood serum level in children]. Czochańska, J; Losiowski, Z; Prokopczyk, J; Zimak, J, ) | 1.25 |
" Most practitioners agree that, because of carbamazepine's relatively short half-life, the total dosage should be administered in at least two divided doses." | ( How to initiate and maintain carbamazepine therapy in children and adults. Porter, RJ, 1987) | 0.83 |
" Psychomotor testing and blood sampling for total and free plasma CBZ, and CBZ 10, 11 epoxide concentration were performed at 10, 12, 14, 16, 18 and 34 h after oral dosing (23." | ( Effect of carbamazepine on psychomotor performance in näive subjects. Agnew, E; Brodie, MJ; Goldie, C; Laidlaw, J; MacPhee, GJ; Potter, L; Roulston, D, 1986) | 0.67 |
"Serious side effects may result from the concurrent administration of the usual dosage of carbamazepine and dextropropoxyphene." | ( Interaction between carbamazepine and dextropropoxyphene. Chang, CM; Chin, D; Huang, CY; Woo, E; Yu, YL, 1986) | 0.82 |
" These findings suggest that the dosage of zonisamide in epileptic patients might need to be varied depending on the comedication." | ( Comparative pharmacokinetics of zonisamide (CI-912) in epileptic patients on carbamazepine or phenytoin monotherapy. Buchanan, RA; Friel, PN; Levy, RH; McLean, JR; Ojemann, LM; Shastri, RA; Wilensky, AJ, 1986) | 0.5 |
" The most common of these causes include malpractice of the dosage build-up in the absence of the clinical effect, polytherapy--not infrequently with drugs of the same chemical group, and insufficient attention to the potentiating drug interaction." | ( [Phenomenon of "paradoxical poisoning" during antiepileptic therapy]. Geladze, TSh, 1986) | 0.27 |
" Failure to distinguish carbamazepine-induced cardiac syncope from epileptic attacks may lead to an increase in dosage and aggravation of syncope." | ( Sick sinus syndrome aggravated by carbamazepine therapy for epilepsy. Hewetson, KA; Ritch, AE; Watson, RD, 1986) | 0.86 |
" Data were excluded for patients who required dosage adjustments because of toxicity or seizures." | ( Effect of influenza vaccine on serum anticonvulsant concentrations. Fidone, GS; Jann, MW, 1986) | 0.27 |
" The provision of appropriate support services (assay results and dosage advice) to specialist epilepsy clinics allows improvement in the management of epilepsy." | ( Availability of drug assay results and dosage advice improves antiepileptic care in a specialist neurology outpatient clinic. Gilligan, BS; Harrison, PM; Heinzow, U; Horne, M; Ioannides-Demos, LL; McLean, AJ; Tong, N; Wodak, J, 1985) | 0.27 |
" Concurrent administration of triacetyloleandomycin with drugs whose metabolism is known to be affected or that could potentially be affected should be avoided unless appropriate adjustments in dosage are made." | ( Pharmacokinetic interactions of the macrolide antibiotics. Ludden, TM, ) | 0.13 |
" When the different dosage regimens (4 mg/kg, 6 mg/kg and 8 mg/kg) were compared at 6 and 12 months after treatment, the 6 mg/kg regimen was found to be more effective than the 4 mg/kg regimen in reducing the microfilarial count, and it produced fewer adverse reactions than the 8 mg/kg regimen." | ( The efficacy of annual single-dose treatment with diethylcarbamazine citrate against diurnally subperiodic bancroftian filariasis in Samoa. Kimura, E; Penaia, L; Spears, GF, 1985) | 0.27 |
" Acute intraperitoneal administration of the other drugs revealed VPA to be an effective anticonvulsant agent, whereas ethosuximide and diazepam were ineffective at dosage levels that are normally effective in mice as determined by classical testing methods such as electroshock and chemoshock." | ( Seizure control following administration of anticonvulsant drugs in the quaking mouse. Abbott, LC; Bennett, GD; Finnell, RH; Taylor, SM, 1985) | 0.27 |
"Fifty-nine patients with chronic generalized tonic-clonic or partial seizures refractory to the maximally tolerated daily dosage of single-drug therapy with carbamazepine, phenytoin, phenobarbital, or primidone subsequently received single-drug therapy with another one of these primary anticonvulsant drugs." | ( Alternative single anticonvulsant drug therapy for refractory epilepsy. Richter, K; Schmidt, D, 1986) | 0.47 |
" This experience suggests that, in therapeutic drug monitoring, salivary CBZ concentrations for at least 2 h after dosage may lead to invalid conclusions about simultaneous plasma CBZ concentrations." | ( Fallacious results from measuring salivary carbamazepine concentrations. Dickinson, RG; Eadie, MJ; Hooper, WD; King, AR, 1985) | 0.53 |
" The results demonstrate the bioequivalence of the dosage forms with respect to the extent of absorption, and similar steady-state concentrations of carbamazepine in plasma can be expected." | ( Bioequivalence of carbamazepine chewable and conventional tablets: single-dose and steady-state studies. Chan, KK; Gerardin, A; Hall, NR; LeSher, AR; Redalieu, E; Sawchuk, RJ; Thompson, TA; Wagner, WE; Weeks, BJ, 1985) | 0.8 |
" If the rats are dosed with carbamazepine during their epilepsy this memory deficit is abolished." | ( Antiepileptic and antiamnesic effect of carbamazepine in experimental limbic epilepsy. Brown, J; Hawkins, CA; Mellanby, J, 1985) | 0.83 |
" The importance of adequate dosage and duration in any treatment trial are emphasized, and the evidence in support of combined antidepressants, lithium-antidepressant combinations, the addition of triiodothyronine or tryptophan, the use of anticonvulsants, and the use of vanadium inactivators, is evaluated." | ( Pharmacological strategies in depression. Barnes, TR; Katona, CL, 1985) | 0.27 |
"Antipyrine total clearance and the formation clearance of its major metabolites were studied in normal, healthy male volunteers before and after multiple dosing for approximately three weeks with phenytoin (six subjects) and carbamazepine (six subjects)." | ( Antipyrine metabolite kinetics in healthy human volunteers during multiple dosing of phenytoin and carbamazepine. Hopkins, K; Houston, JB; Morselli, PL; Rowland, M; Shaw, PN; Thiercelin, JF, 1985) | 0.67 |
" We found a noticeable relationship between conduction velocity slowing and daily dosage for CBZ only." | ( Anticonvulsant therapy and its possible consequences on peripheral nervous system: a neurographic study. Faedda, MT; Geraldini, C; Sideri, G, 1984) | 0.27 |
" CBZ initial daily dosage of 400 mg was increased by a similar amount every second week to a maximum of 1,200 mg." | ( Treatment of intractable neurogenic pain with carbamazepine. Agnew, E; Brodie, MJ; McCubbin, TD; Rapeport, WG; Rogers, KM, 1984) | 0.53 |
" Neuroleptic medications are still the mainstay of treatment, but recent studies suggest new approaches to dosage and to the treatment of acute psychosis." | ( The pharmacologic treatment of schizophrenia: a progress report. Baldessarini, RJ; Donaldson, SR; Gelenberg, AJ, 1983) | 0.27 |
" The results show that all three of these anticonvulsants depress postjunctional sensitivity to released acetylcholine producing parallel dose-response curves for MEPP amplitude inhibition." | ( Differential effects of the anticonvulsants phenobarbital, ethosuximide and carbamazepine on neuromuscular transmission. Alderdice, MT; Trommer, BA, 1980) | 0.49 |
" Carbamazepine dosage was adjusted individually to provide serum levels within therapeutic range." | ( [Seizure prevention using carbamazepine following severe brain injuries]. Glötzner, FL; Haubitz, I; Kapp, G; Miltner, F; Pflughaupt, KW, 1983) | 1.48 |
" When binding is altered, the total concentration no longer reflects the amount of pharmacologically active drug in the plasma: this may mislead the clinician into making inappropriate dosage adjustments." | ( Free level monitoring of antiepileptic drugs. Clinical usefulness and case studies. Perucca, E, 1984) | 0.27 |
" In the dosage used, l-tryptophan was tolerated well by these children, and seizure frequency, as a whole, remained unaltered." | ( l-Tryptophan in hyperactive child syndrome associated with epilepsy: a controlled study. Ghose, K, 1983) | 0.27 |
" Conversely, anticonvulsants may influence the dosage requirements of oral anticoagulants by inducing their metabolism." | ( Interactions between anticonvulsants and other commonly prescribed drugs. Kutt, H, 1984) | 0.27 |
" Significant positive correlations were found between the dosage of CBZ, DPH, PMD and PB and both indices of enzyme induction." | ( A comparative study of the relative enzyme inducing properties of anticonvulsant drugs in epileptic patients. Hedges, A; Makki, KA; Perucca, E; Richens, A; Ruprah, M; Wilson, JF, 1984) | 0.27 |
"The objective of this investigation was to study the teratogenic effects of dosage levels and time of administration of three anticonvulsant drugs (carbamazepine [CMZ], sodium valproate [NaV], and diphenylhydantoin [DPH]) on craniofacial development in the CD-1 mouse fetus." | ( Teratogenic effects of dosage levels and time of administration of carbamazepine, sodium valproate, and diphenylhydantoin on craniofacial development in the CD-1 mouse fetus. Eluma, FO; Hayes, TG; Paulson, RB; Sucheston, ME, 1984) | 0.7 |
" Fluctuations in carbamazepine concentrations were 79% +/- 29% higher than trough levels on a twice-daily dosage schedule and 40% +/- 13% higher during four-times-a-day administration." | ( Interdosage fluctuations in plasma carbamazepine concentration determine intermittent side effects. Tomson, T, 1984) | 0.88 |
" On a three-times-daily or four-times-daily dosing schedule, both total and free carbamazepine levels fluctuated considerably (on an average, 41 and 45%, respectively, around the mean)." | ( Diurnal fluctuations in free and total steady-state plasma levels of carbamazepine and correlation with intermittent side effects. Albani, F; Ambrosetto, G; Baruzzi, A; Contin, M; Cortelli, P; Perucca, E; Riva, R, 1984) | 0.73 |
" Fifty-one percent of the 53 patients receiving phenytoin were completely controlled at either below or above the 10 to 20 micrograms/ml range, suggesting that individual dosage adjustment is preferably based on clinical judgment rather than numerical limits of published therapeutic ranges." | ( Therapeutic plasma levels of phenytoin, phenobarbital, and carbamazepine: individual variation in relation to seizure frequency and type. Haenel, F; Schmidt, D, 1984) | 0.51 |
" dosing schedule, total plasma levels of CBZ and CBZ-E fluctuated to a similar extent (average 34% and 29%, respectively)." | ( Free and total plasma concentrations of carbamazepine and carbamazepine-10,11-epoxide in epileptic patients: diurnal fluctuations and relationship with side effects. Albani, F; Ambrosetto, G; Baruzzi, A; Contin, M; Cortelli, P; Gobbi, G; Perucca, E; Procaccianti, G; Riva, R, 1984) | 0.54 |
" Doses of l-baclofen one fifth its equivalent racemic dosage produced a much greater enhancement of segmental inhibition." | ( Effect of baclofen enantiomorphs on the spinal trigeminal nucleus and steric similarities of carbamazepine. Chang, CH; Fromm, GH; Sax, M; Terrence, CF; Yoo, CS, 1983) | 0.49 |
" Relatively large fluctuations were observed for both CBZ (mean, 57%; range, 32-100%) and EP (mean, 97%; range, 19-189%) during a dosage interval." | ( Fluctuations in salivary carbamazepine and carbamazepine-10,11-epoxide concentrations during the day in epileptic children. Aman, MG; Paxton, JW; Werry, JS, 1983) | 0.57 |
" She was found to be taking a subtherapeutic dosage of carbamazepine; induction of therapeutic blood levels of carbamazepine resulted in improvement in the interictal EEG, decreased duration and intensity of affect during the epileptic attacks, and a normalization of behavioral and emotional functioning during the interictal period." | ( Effects of carbamazepine on interictal psychopathology in TLE with ictal fear. Hermann, BP; Melyn, M, 1984) | 0.9 |
"The incidence of malformations in fetal mice exposed to phenytoin depends on drug dosage and the strain of mice." | ( Teratogenic effects of anticonvulsants. Paulson, GW; Paulson, RB, 1981) | 0.26 |
" Carbamazepine in the dosage of 200-600 mg was administered for 1 year." | ( A preliminary double-blind study on the efficacy of carbamazepine in prophylaxis of manic-depressive illness. Hazama, H; Inanaga, K; Mori, A; Okuma, T; Otsuki, S; Sarai, K; Takahashi, R; Watanabe, S, 1981) | 1.42 |
" Fortunately, the drugs used by the majority of these patients are readily measured in plasma, and in most cases the plasma concentration is a valid measure of the appropriateness of the dosage of drug administered." | ( Antiepileptic therapeutic drug monitoring. Cohan, SL, 1981) | 0.26 |
" New antiepileptic drugs have improved medical management, and technical and theoretical advances in pharmacokinetics have permitted physicians to design balanced dosing for individual patients." | ( Recent developments in the diagnosis and therapy of epilepsy. Crandall, PH; Engel, J; Sterman, MB; Troupin, AS; Wasterlain, CG, 1982) | 0.26 |
" A cross-sectional analysis of items such as designs, patient sampling principles, recording of effect parameters and side effects, concomitant treatments, and statistical evaluations demonstrated that cross-over designs, investigating fixed dosage schedules, were extensively used." | ( Controlled trials in epilepsy: a review. Bentsen, KD; Flachs, H; Gram, L; Parnas, J, 1982) | 0.26 |
" However, displacement alone, unlike induced metabolism, should not affect the drug's dose-response relationship." | ( Drug interactions with valproic acid. Koch, KM; Levy, RH, 1982) | 0.26 |
"Levels of carbamazepine and its -10,11-epoxide metabolite were measured in plasma and CSF of affectively ill patients treated only with carbamazepine for an average of 33 days at an average dosage of 1,055 mg/day." | ( Carbamazepine and its -10,11-epoxide metabolite in plasma and CSF. Relationship to antidepressant response. Ballenger, JC; Bunney, WE; Chatterji, DC; Greene, RF; Post, RM; Uhde, TW, 1983) | 2.11 |
" After dosing with CBZ-E, peak plasma concentrations of the parent compound were reached within 2 hr." | ( Single-dose kinetics and metabolism of carbamazepine-10,11-epoxide. Bertilsson, L; Tomson, T; Tybring, G, 1983) | 0.54 |
"The effect of dosage frequency of carbamazepine (CBZ) (brand name Tegretol) on pseudo-steady state drug serum levels were studied in 14 male (16-18 years) epileptics." | ( Effect of dosage frequency of carbamazepine on drug serum levels in epileptic patients. Christfides, JA; Fry, DE; Ghose, K, 1983) | 0.83 |
"The effect of once daily dosage of carbamazepine on fit frequency, electroencephalogram (EEG), behaviour and 24-hour drug levels were compared with those following 2 to 3 divided daily doses treatment." | ( Once daily dosage versus divided daily doses of carbamazepine therapy in epileptic patients: a pilot study. Christofides, JA; Dawson, M; Fry, DE; Ghose, K, 1981) | 0.8 |
" Fifty-three patients were tested using the EMIT assay system, and a questionnaire was used to compare the physicians' choice of drug dosage and appointment interval before and after each patient result was available." | ( Evaluation of the provision of rapid drug plasma assays in an outpatient anticonvulsant clinic. Fullinfaw, R; King, J; Marty, J; Trembath, P; Tuckett, R, 1981) | 0.26 |
" Extemporaneously compounded suspensions of carbamazepine in HUP-A or in simple syrup can be used for patients who require a liquid dosage form." | ( Stability of extemporaneous suspensions of carbamazepine. Akers, MJ; Burckart, GJ; Hammond, RW, 1981) | 0.79 |
" The aim was to study diurnal pain distribution, its relation to CBZ dosing and plasma concentration and the effect of decreasing the dose." | ( Trigeminal neuralgia: time course of pain in relation to carbamazepine dosing. Ekbom, K; Tomson, T, 1981) | 0.51 |
"We describe a procedure for determining 2-ethyl-2-phenylmalonamide (I) in serum of epilepsy patients dosed with primidone (II) for seizure control, by extracting the sample with chloroform under basic conditions, with use of an internal standard, 2-ethyl-2-(p-tolyl)malonamide, and without derivative formation." | ( Monitoring 2-ethyl-2-phenylmalonamide in serum by gas-liquid chromatography: application to retrospective study in epilepsy patients dosed with primidone. Haidukewych, D; Rodin, EA, 1980) | 0.26 |
" The relationship appeared to be linear over the dosage range examined (600 to 1400mg in most patients)." | ( Effect of dose increments on serum carbamazepine concentration in epileptic patients. Bittencourt, P; Perucca, E; Richens, A, ) | 0.41 |
" Despite the significant dialysis clearance, a dosage regimen adjustment may not be necessary because of the long elimination half-life of carbamazepine of 35 hr compared to the short length of the usual hemodialysis treatment of 3-5 hr." | ( Hemodialysis clearance and total body elimination of carbamazepine during chronic hemodialysis. Bruni, J; Lee, CS; Marbury, TC; Perchalski, RJ; Wang, LH, 1980) | 0.71 |
" This anti-MES activity is achieved with nontoxic doses, with the optimal effect recorded in rats dosed orally with anti-MES ED50 and protective index (PI) values of 25." | ( Comparative anticonvulsant activity and neurotoxicity of 4-amino-N-(2,6-dimethylphenyl)phthalimide and prototype antiepileptic drugs in mice and rats. Bailleux, V; Hamoir, G; Nuyts, JP; Poupaert, JH; Stables, JP; Vallée, L; Vamecq, J, 1995) | 0.29 |
" CBZ dosage was decreased, with prompt resolution of symptoms." | ( Oculogyric crisis induced by carbamazepine. Barkley, GL; Gorman, M, 1995) | 0.58 |
" Even though the mean daily dosage of CsA was consistently higher in the carbamazepine group than in the control group (16." | ( Effects of carbamazepine on cyclosporine metabolism in pediatric renal transplant recipients. Cooney, GF; Dunn, SP; Goldsmith, B; Kaiser, B; Mochon, M, ) | 0.75 |
"Plasma carbamazepine (CBZ) and carbamazepine-10,11-epoxide (CBZ-E) concentrations were measured in 160 epileptic patients in order to determine the effect of factors such as age, daily dosing schedule, formulation, and combination with other antiepileptic drugs on these concentrations in relation to the daily dose." | ( Factors influencing plasma concentrations of carbamazepine and carbamazepine-10,11-epoxide in epileptic children and adults. Bonato, PS; Campos, GM; Lanchote, VL; Rodrigues, I, 1995) | 1.01 |
" for 10 days) on the steady-state plasma concentrations of Oxcarbazepine (OXC), its active metabolite 10, 11-dihydro-10-hydroxy-carbazepine (MHD) and the corresponding diol (DHD) were studied in a randomized, double-blind cross-over placebo-controlled trial in 6 epileptic patients stabilized on a fixed dosage of OXC." | ( Effects of the antidepressant drug viloxazine on oxcarbazepine and its hydroxylated metabolites in patients with epilepsy. Artesi, C; Di Perri, R; Fazio, A; Oteri, G; Perucca, E; Pisani, F; Xiao, B, 1994) | 0.29 |
" Fifty-two children between the age of 2 weeks and 15 years were treated with CBZ (mean dosage 17 mg/kg body weight) either as mono- (n = 36) or in polytherapy (n = 16)." | ( The metabolization of carbamazepine to CBZ-10,11-epoxide in children from the newborn age to adolescence. Hannak, D; Haug, C; Korinthenberg, R, 1994) | 0.6 |
" Extreme interindividual differences in both dosage and length of stay help in elucidating the apparently contradictory results of comparative investigations with small patient groups." | ( [General practice of acute inpatient treatment of mania. Retrospective comparative study of 100 patients at each of 2 psychiatric centers]. Adler, L; Hajak, G; Koller, M; Langer, C; Lehmann, K; Nordeck, I; Thomas, RS; Ulrich, M, 1994) | 0.29 |
" Because a drug interaction was suspected, the carbamazepine dosage was decreased during treatment, and serum levels were measured 3 to 5 days after change in therapy." | ( Clarithromycin-carbamazepine interaction in a clinical setting. Fris, J; O'Connor, NK, ) | 0.74 |
"Despite decreasing the dosage of carbamazepine by 30 to 40 percent, the serum levels of this drug increased in all of our patients while taking clarithromycin, including 3 patients who developed toxic serum levels of carbamazepine." | ( Clarithromycin-carbamazepine interaction in a clinical setting. Fris, J; O'Connor, NK, ) | 0.77 |
" If clinical judgment suggests clarithromycin should be used, however, we suggest decreasing the dosage of carbamazepine by 30 to 50 percent, monitoring the serum drug levels closely, and warning the patient about the signs and symptoms of carbamazepine toxicity." | ( Clarithromycin-carbamazepine interaction in a clinical setting. Fris, J; O'Connor, NK, ) | 0.7 |
"min-1), the glucuronides of oxcarbazepine and its monohydroxy-metabolite are likely to accumulate during repeated administration, and dosage adjustment of oxcarbazepine in these patients could not be proposed from this single administration study." | ( The effect of renal impairment on the pharmacokinetics of oxcarbazepine and its metabolites. Aldigier, JC; Darragon, T; Godbillon, J; Hillion, D; Jungers, P; Kourilsky, O; Lecaillon, JB; Menard, F; Meyer, P; Rouan, MC, 1994) | 0.29 |
" In this case, it seems necessary to diminish the interval between injections than to give higher dosage in order to maintain plasma concentrations." | ( Do enzyme inducers modify haloperidol decanoate rate of release? Agenet, C; Barges-Bertocchio, MH; Levron, JC; Pupeschi, G, 1994) | 0.29 |
" The dosage was increased when she developed generalized tonic-clonic seizures and she is currently maintained on a maximal dose of a controlled release formulation." | ( Case summary: Kate. Ebbing, A; Kirkham, FJ, 1994) | 0.29 |
" Neuroleptic dosing of manic patients is probably too high and exposes patients to an unnecessary risk of side effects including tardive dyskinesia." | ( Treatment approaches for acute mania. Chou, JC; Sweeney, EA; Tuma, I, 1993) | 0.29 |
"We have determined the cumulative dose-response relationship for vecuronium from the evoked compound electromyogram of the hypothenar muscles in eight patients who were receiving carbamazepine." | ( Influence of carbamazepine on the dose-response relationship of vecuronium. Ebrahim, Z; Whalley, DG, 1994) | 0.85 |
" An understanding of the underlying pharmacokinetic processes, including the need of most elderly patients for lower doses and longer dosing intervals, permits more effective management of therapy and reduces the risk for adverse reactions." | ( Antiepileptics in the elderly. Pharmacoepidemiology and pharmacokinetics. Cloyd, JC; Lackner, TE; Leppik, IE, 1994) | 0.29 |
" Each patient received an individualized loading dose and maintenance dosage targeted at a 60-ng/ml plasma FNR concentration." | ( Flunarizine for treatment of partial seizures: results of a concentration-controlled trial. Drake, ME; Mikati, M; Olson, L; Pellock, JM; Pledger, GW; Sackellares, JC; Sahlroot, JT; Treiman, DM; Tsay, JY; Wright, FS, 1994) | 0.29 |
" A recent panel study suggests that determination of CYP1A2 activity with the caffeine test may be very useful for the dosing of clozapine." | ( Fluvoxamine inhibition and carbamazepine induction of the metabolism of clozapine: evidence from a therapeutic drug monitoring service. Bertilsson, L; Bondesson, U; Jerling, M; Lindström, L, 1994) | 0.59 |
" Six patients were receiving CBZ monotherapy, and 12 patients were treated with an additional antiepileptic drug (AED) maintained at baseline dosage during CBZ taper." | ( Relationship of carbamazepine reduction rate to seizure frequency during inpatient telemetry. Blaxton, TA; Lynch, B; Malow, BA; Mikati, MA, ) | 0.48 |
" Recommendations are made for a higher initial dosage regime for sodium valproate in partial seizures." | ( A multicentre comparative trial of sodium valproate and carbamazepine in adult onset epilepsy. Adult EPITEG Collaborative Group. Cartlidge, NE; Davidson, DL; Easter, DJ; Richens, A, 1994) | 0.53 |
" Dose-response curves were constructed for the ability of theophylline to produce tonic seizures in animals pre-treated with vehicle or several adenosine A1 receptor agonists." | ( Adenosine receptors are not involved in theophylline-induced seizures. Hornfeldt, CS; Larson, AA, 1994) | 0.29 |
" Consequently, the controlled trial was designed to account for this interaction by reducing the phenytoin dosage by approximately 20% during the felbamate treatment period and using matching placebo capsules to maintain the blind." | ( Dosage adjustments in response to monitored plasma concentrations: can unblinded staff adhere to objective criteria? Pledger, GW; Sahlroot, JT, 1994) | 0.29 |
" The usually administered dosage of OCBZ is approximately 50% higher than that of CBZ." | ( Oxcarbazepine: clinical development program. Schwabe, S, 1994) | 0.29 |
"A retrospective study of 113 patients treated with a sustained-release form of valproate (SRF-VPA), known as the "chrono" formulation in most European countries, led to the following conclusions: Patients treated with the old VPA formulation could immediately receive the same daily dosage of SRF-VPA without loss of seizure control when administered as a single evening dose." | ( A retrospective study of 113 epileptic patients treated with sustained-release valproate. Despland, PA, 1994) | 0.29 |
" Dosage was kept constant unless poor seizure control prompted an increase." | ( Epilepsy and pregnancy: a prospective study of seizure control in relation to free and total plasma concentrations of carbamazepine and phenytoin. Ekqvist, B; Lindbom, U; Sundqvist, A; Tomson, T, ) | 0.34 |
" No dosage adjustment is necessary when GBP and CBZ or VPA are coadministered." | ( Lack of interaction of gabapentin with carbamazepine or valproate. Bockbrader, HN; Chang, T; Erdman, GR; Leppik, IE; Posvar, EL; Radulovic, LL; Sedman, AJ; Uthman, BM; Wilder, BJ, ) | 0.4 |
" CBZ-CR and PHT were administered to 42 adult patients (21 each) at a dosage of 20 mg/kg with a minimum and maximum dosage of 1,200 and 1,600 mg in patients weighting < 60 and > 80 kg, respectively." | ( Acute oral loading of carbamazepine-CR and phenytoin in a double-blind randomized study of patients at risk of seizures. Kruger, AJ; Müller, FO; Rabie, W; Schall, R; Van Der Meyden, CH, ) | 0.45 |
"Patients in whom carbamazepine (CBZ) monotherapy is discontinued for preoperative EEG/video monitoring often display toxicity if their previous maintenance dosage is resumed, even after a few days without CBZ." | ( Rapid reversibility of autoinduction of carbamazepine metabolism after temporary discontinuation. Bourgeois, BF; Lüders, HO; Schäffler, L, ) | 0.74 |
" Creatinine concentrations should not be considered when dosage adjustments of renally eliminated drugs are being calculated for patients with such metabolic interferences." | ( Creatinine metabolism impairment by an anticonvulsant drug, phenacemide. Baltassat, P; Cahen, R; Francois, B; Louisot, P; Martin, A, 1994) | 0.29 |
" Median AUCs of CBZ, VPA and PHT during a dosage interval did not differ significantly after treatment with OXC and placebo." | ( A double-blind, placebo-controlled interaction study between oxcarbazepine and carbamazepine, sodium valproate and phenytoin in epileptic patients. Blacklaw, J; Brodie, MJ; Connelly, D; Forrest, G; Gillham, RA; McKee, PJ; Walker, SM, 1994) | 0.52 |
" In patients, linear and dose-proportional kinetics with no autoinduction of metabolism simplify OCBZ dosage adjustment." | ( Clinical pharmacology and pharmacokinetics of oxcarbazepine. Dieterle, W; Flesch, G; Lloyd, P, 1994) | 0.29 |
" The recommended dosage of OCBZ as monotherapy for adults with epilepsy is 600-1,200 mg orally per day but may be higher in patients with refractory seizures and in patients requiring combination therapy." | ( Practical aspects of oxcarbazepine treatment. Dam, M, 1994) | 0.29 |
" We collected dosage interval urine samples from three groups of 10 valproate patients: (1) valproate monotherapy, (2) valproate with carbamazepine, and (3) valproate with phenytoin." | ( Interaction between valproate and branched-chain amino acid metabolism. Acheampong, AA; Anderson, GD; Levy, RH, 1994) | 0.49 |
" To compare the two formulations at the same doses and dose schedules, the study design had to be open, within-patient, with an initial 4 week period to individually adjust the dosage schedule with conventional CBZ followed by a 4 week period in which the CR formulation was substituted for conventional CBZ at the same daily dose and given by the same schedule." | ( Daily fluctuation of plasma levels with conventional and controlled-release carbamazepine: correlation with adverse effects. Bareggi, SR; Guizzaro, A; Monza, CG; Parisi, A; Pirola, R; Tata, MR, 1994) | 0.52 |
" The population pharmacokinetic parameters of zonisamide will be useful for designing dosage regimens in epileptic patients." | ( Population analysis of the dose-dependent pharmacokinetics of zonisamide in epileptic patients. Hashimoto, Y; Hori, R; Odani, A; Okuno, T; Tanigawara, Y; Yasuhara, M, 1994) | 0.29 |
" Its pharmacological properties and side-effects are well known and very effective dosage schedules already exist." | ( [Carbamazepine in treatment of alcohol withdrawal syndrome--an overview of current research]. Thome, J; Vince, GH; Wiesbeck, GA, 1994) | 1.2 |
" Six dogs were dosed orally in a two-way crossover study in which the tablet was compared with an equivalent dose of the complex in solution." | ( Oral pharmacokinetics of carbamazepine in dogs from commercial tablets and a cyclodextrin complex. Betlach, CJ; Bodor, N; Gonzalez, MA; McKiernan, BC; Neff-Davis, C, 1993) | 0.59 |
" Doubling the daily carbamazepine dosage did not yield quantifiable serum concentrations." | ( Unmasking the significant enzyme-inducing effects of phenytoin on serum carbamazepine concentrations during phenytoin withdrawal. Abou-Elkair, M; Chapron, DJ; LaPierre, BA, 1993) | 0.84 |
" The t 1/2 and AUC values of PB were significantly increased by ZNS coadministration, and a significant decrease in the Vd/F value of PHT was observed after multiple dosing of ZNS." | ( Pharmacokinetic interaction of zonisamide in rats. Effect of zonisamide on other antiepileptics. Fukuchi, H; Kimura, M; Kimura, Y; Kitaura, T; Miyake, K; Tanaka, N, 1993) | 0.29 |
" After an 8-week baseline period, a single-dose pharmacokinetic study was performed for each patient to calculate a loading dose and maintenance dosage necessary to achieve a target plasma FNR concentration of 30 ng/ml." | ( Increasing plasma concentration tolerability study of flunarizine in comedicated epileptic patients. Cereghino, JJ; DeGiorgio, C; Pledger, GW; Treiman, DM; Tsay, JY, ) | 0.13 |
" Blood samples for measurement of FEL and its pyridine metabolite (determined by gas-chromatography) were drawn just before dosing and at 2, 4, 6, 8, 10, 12, and 24 h after dosing on days 5, 6, and 13." | ( Influence of single and repeated doses of oxcarbazepine on the pharmacokinetic profile of felodipine. Bendoni, L; Gangemi, PF; Menge, GP; Monza, GC; Schwabe, S; Zaccara, G, 1993) | 0.29 |
" We conclude that OPT is a simple yet useful program to derive individual and population pharmacokinetic parameters for CBZ for use in dosage adjustments." | ( Estimation of population pharmacokinetics for carbamazepine in Malaysian patients using the OPT computer program. Ismail, R; Rahman, AF, 1993) | 0.54 |
" Plasma carbamazepine concentration data were obtained from an open, steady-state, crossover bioavailability study in which 494 measurements were obtained from 13 patients, with an equal number of samples per patient for each dosage form." | ( Bioavailability of controlled release carbamazepine estimated by mixed effect modelling. Ludden, TM; Miller, R, 1993) | 0.99 |
" Monitering of BUP and its metabolites may ultimately prove useful in guiding clinicians dosing decisions, especially when mood stabilizers are combined with other psychotropic drugs in refractory bipolar patients." | ( Bupropion and anticonvulsant drug interactions. Lamparella, V; Masand, PS; Popli, AP; Tanquary, J, 1995) | 0.29 |
" Although it had been suggested by several authors that the measurement of carbamazepine in hair might provide a better index of individual dosage history than the plasma level assays, the deviations observed in this study led to the conclusion that hair samples are not suitable for evaluating the quantity of drug consumed." | ( Testing human hair for carbamazepine in epileptic patients: is hair investigation suitable for drug monitoring? Kintz, P; Mangin, P; Marescaux, C, 1995) | 0.83 |
" Cognitive function testing was performed on Day 1 before carbamazepine dosing (baseline), Day 15 (carbamazepine alone), and Day 32 (carbamazepine plus sertraline or placebo)." | ( Absence of a sertraline-mediated effect on the pharmacokinetics and pharmacodynamics of carbamazepine. Dewland, PM; Muirhead, DC; Rapeport, WG; Tanner, T; Wesnes, K; Williams, SA, 1996) | 0.76 |
" TPM was added to the baseline antiepileptic drug (AED) at a dosage of up to 800 mg/day, after which the baseline drug was discontinued, when possible." | ( Drug interaction profile of topiramate. Bourgeois, BF, 1996) | 0.29 |
" All the drugs can be conveniently given as a twice daily dosage apart from gabapentin, which has a short half-life and a midday dose is needed." | ( Clinical pharmacokinetics of newer antiepileptic drugs. Lamotrigine, vigabatrin, gabapentin and oxcarbazepine. Binnie, CD; Elwes, RD, 1996) | 0.29 |
" Less than 8% of drug was excreted in the urine for each dosing regimen." | ( Bioactivation of carbamazepine in the rat in vivo. Evidence for the formation of reactive arene oxide(s). Madden, S; Maggs, JL; Park, BK, 1996) | 0.63 |
" The daily dosage of each drug was held constant during treatment of the obesity." | ( Clearance of phenytoin and valproic acid is affected by a small body weight reduction in an epileptic obese patient: a case study. Ashikari, Y; Chiba, S; Kodama, Y; Kuranari, M; Sakata, T; Takeyama, M, 1996) | 0.29 |
" Because dosage in general was moderate and serum levels were within therapeutic boundaries in most cases, the symptom seemed to have been caused by an interaction of drugs rather than by a single agent." | ( Asterixis induced by psychotropic drug treatment. Rittmannsberger, H, 1996) | 0.29 |
" With increasing carbamazepine dosage (1) carbamazepine overall plasma apparent clearance (CL/F), (2) plasma clearance of carbamazepine to urinary carbamazepine-10,11-epoxide, (3) plasma clearance of carbamazepine-10,11-epoxide to urinary unconjugated carbamazepine-10,11-trans-diol and (4) plasma clearances of carbamazepine to urinary 2- and 3-hydroxy carbamazepine all increased." | ( Dose-dependent metabolism of carbamazepine in humans. Bernus, I; Dickinson, RG; Eadie, MJ; Hooper, WD, 1996) | 0.92 |
" A patient was only considered twice if his comedication or OCBZ dosage had been changed." | ( Fluctuations of 10-hydroxy-carbazepine during the day in epileptic patients. May, TW; Rambeck, B; Sälke-Kellermann, A, 1996) | 0.29 |
" A drug concentration, however, can only be regarded as a guide around which to alter the dosage according to the patient's clinical condition." | ( Optimisation of antiepileptic drug therapy. The importance of serum drug concentration monitoring. Yukawa, E, 1996) | 0.29 |
"l-1 and the dosage of CBZ should simultaneously be decreased in steps by more than 50% to minimize the change in CBZ plasma concentration." | ( Effect of stiripentol on carbamazepine plasma concentration and metabolism in epileptic children. Chiron, C; d'Athis, P; Dulac, O; Olive, G; Pous, G; Renard, F; Rey, E; Tran, A; Vauzelle-Kervroedan, F, 1996) | 0.6 |
" When PB in the dosage of 30-60 mg/d was used in combination with PHT the above mentioned changes were not observed." | ( Brainstem auditory evoked potentials in epileptics on different anti-epileptic drugs. Gupta, HL; Mukhopadhyay, S; Panjwani, U; sel Vamurthy, W; Singh, SH; Thakur, L, 1996) | 0.29 |
" During this pregnancy the patient took a reduced dosage of carbamazepine." | ( Fetal malformations in an epileptic pregnant woman treated with carbamazepine. Caradonna, F; Caruso, G; Ceci, O; Clemente, R; Ferreri, R; Loizzi, P, 1996) | 0.77 |
" All patients received a drug dosage to ensure adequate plasma concentration and satisfactory seizure control." | ( The effect of chronic carbamazepine, valproic acid and phenytoin medication on the periodontal condition of epileptic children and adolescents. Borowicz-Andrzejewska, E; Borysewicz-Lewicka, M; Galas-Zgorzalewicz, B; Zgorzalewicz, M, ) | 0.45 |
" Both dosage regimens of lamotrigine were well tolerated." | ( A randomised open multicentre comparative trial of lamotrigine and carbamazepine as monotherapy in patients with newly diagnosed or recurrent epilepsy. Dam, M; Reunanen, M; Yuen, AW, 1996) | 0.53 |
" Phenobarbital cotreatment (45 mg/kg/day) with OXC (1100 mg/kg/day) did not lead to changes in the incidence of malformation when compared with OXC (1100 mg/kg/day) dosed alone." | ( Teratogenicity of carbamazepine-10, 11-epoxide and oxcarbazepine in the SWV mouse. Amore, BM; Bennett, GD; Finnell, RH; Kalhorn, TF; Nelson, SD; Skiles, GL; Slattery, JT; Wlodarczyk, B, 1996) | 0.63 |
" Based on this approach, liquid dosage forms were configured for both parenteral and oral use." | ( Intravenous and oral pharmacokinetic evaluation of a 2-hydroxypropyl-beta-cyclodextrin-based formulation of carbamazepine in the dog: comparison with commercially available tablets and suspensions. Anderson, WR; Bodor, N; Brewster, ME; Cheung, B; Derendorf, H; Estes, KS; Meinsma, D; Moreno, D; Pablo, L; Pop, E; Sawchuk, R; Webb, AI, 1997) | 0.51 |
" Therefore, when using surfactants in dissolution media for in vitro testing of dosage forms, consideration must be given to the level of impurities present so that the results are consistent and reliable." | ( Dissolution media for in vitro testing of water-insoluble drugs: effect of surfactant purity and electrolyte on in vitro dissolution of carbamazepine in aqueous solutions of sodium lauryl sulfate. Amidon, GL; Crison, JR; Weiner, ND, 1997) | 0.5 |
" Irrespective of the drug used, optimal clinical management requires individualization of dosage and dosing schedules based on careful evaluation of clinical response and sound knowledge of the pharmacokinetics and interaction potential of the individual compounds." | ( Established antiepileptic drugs. Perucca, E, 1996) | 0.29 |
" Specific indications and dosage schedules have been provided." | ( New antiepileptic drugs. Brodie, MJ; Wilson, EA, 1996) | 0.29 |
"028), indicating that the model proposed for CL can be used to make accurate dosage recommendations." | ( Carbamazepine population pharmacokinetics in children: mixed-effect models. Delgado Iribarnegaray, MF; Domínguez-Gil, A; Falcão, AC; García Sánchez, MJ; Otero, MJ; Santo Bueldga, D, 1997) | 1.74 |
" Sectional hair analysis of a patient on a constant dosage of CBZ demonstrates an exponential decrease in hair concentrations of CBZ and CBZ-diol with increasing distance from the root, probably caused by shampooing." | ( High-performance liquid chromatographic determination of carbamazepine and metabolites in human hair. Brekelmans, GJ; Edelbroek, PM; Rademaker, RV; Saris, LA; van der Linden, GJ, 1997) | 0.54 |
" With a view to better defining the drug's dose-response relationships in the presence of concomitant alternative antiepileptic drugs." | ( Plasma concentrations of vigabatrin in epileptic patients. López, E; Quintana, B; Rodriguez, I; Sánchez-Alcaraz, A, 1996) | 0.29 |
" Dosage should be individualized, based on withdrawal severity measured by withdrawal scales, comorbid illness, and history of withdrawal seizures." | ( Pharmacological management of alcohol withdrawal. A meta-analysis and evidence-based practice guideline. American Society of Addiction Medicine Working Group on Pharmacological Management of Alcohol Withdrawal. Mayo-Smith, MF, 1997) | 0.3 |
" Thus, the dosage of digitoxin appears to be fully compensated during concomitant use of phenobarbital, but obviously deserves attention during concomitant use of phenytoin or carbamazepine." | ( [Serum digitoxin in concomitant use of antiepileptics in routine therapy]. Aass, H; Johannessen, SI; Osnes, JB; Skomedal, T; Stokke, KT, 1997) | 0.49 |
" Our data indicate the possible use of hair testing as a marker of the dosage history of patients under long-term treatment with CBZ." | ( Carbamazepine levels in the hair of patients under long-term treatment: a preliminary study. Kourtopoulos, H; Paritsis, N; Psillakis, TK; Tsatsakis, AM; Tzatzarakis, M, 1997) | 1.74 |
" Thus the performance of the Bayesian dosing program is acceptable when two feedback concentrations are known, and seems able to help the clinician adjust carbamazepine dosage in an outpatient population." | ( Predictions of carbamazepine concentrations using a Bayesian program (PKS System, Abbott): a retrospective evaluation in an outpatient population. Boulieu, R; Fischer, C; Gaulier, JM; Mauguiere, F, 1997) | 0.85 |
" Results of outcome measures, including time to exit, completion rate, and mean time on monotherapy, showed no significant differences among dosage groups." | ( Gabapentin monotherapy: II. A 26-week, double-blind, dose-controlled, multicenter study of conversion from polytherapy in outpatients with refractory complex partial or secondarily generalized seizures. The US Gabapentin Study Group 82/83. Abou-Khalil, B; Beydoun, A; Cantrell, D; Fischer, J; Garofalo, E; Greiner, M; Harden, C; Hayes, A; Labar, DR; Pierce, M; Ramsay, RE; Sackellares, JC; Uthman, BM, 1997) | 0.3 |
" The LTG dosage was increased step by step until clinical response or side effects were observed." | ( No increase in carbamazepine-10,11-epoxide during addition of lamotrigine treatment in children. Boreus, LO; Eriksson, AS, 1997) | 0.65 |
" The first appears to involve a nonspecific manifestation of drug intoxication; seizure-worsening in this context is usually reversible by dosage reduction or elimination of unnecessary polypharmacy." | ( Antiepileptic drugs as a cause of worsening seizures. Avanzini, G; Dulac, O; Gram, L; Perucca, E, 1998) | 0.3 |
"A new capsule dosage form of carbamazepine (CBZ) has been developed, consisting of three different types of beads (immediate-release, extended-release, and enteric-release) that may be taken sprinkled on food or swallowed for easy administration." | ( Pharmacokinetic evaluation of twice-daily extended-release carbamazepine (CBZ) and four-times-daily immediate-release CBZ in patients with epilepsy. Belendiuk, GW; Couch, RA; Garnett, WR; Levy, B; McLean, AM; Pellock, JM; Rudnic, EM; Zhang, Y, 1998) | 0.83 |
"Results of the development of a solid dosage form containing 200 mg Carbamazepine (CBZ) are presented." | ( [Influence of different auxiliary materials on the dissolution of carbamazepine from solid dosage forms]. Jeköné, BZ, 1998) | 0.77 |
" For comparison of drug potencies, doses increasing seizure thresholds by 20 or 50% were calculated from dose-response curves." | ( Anticonvulsant drug effects in the direct cortical ramp-stimulation model in rats: comparison with conventional seizure models. Krupp, E; Löscher, W, 1998) | 0.3 |
" During the course of the double blind trials, the problem of different therapeutic dosages of psychotropic drugs between Japan and Western countries emerged; that is, the doses of chlorpromazine and lithium carbonate, which were used as the control drugs to carbamazepine in the two double-blind group-comparison studies in Japan, were both much lower than the dosage used in most of the Western countries." | ( A history of investigation on the mood stabilizing effect of carbamazepine in Japan. Kishimoto, A; Okuma, T, 1998) | 0.72 |
" We propose that individual dosage adjustment in VPA + CBZ polytherapy should be combined with monitoring of relevant enzyme activities in serum." | ( Valproate and carbamazepine comedication changes hepatic enzyme activities in sera of epileptic children. Cepelak, I; Lenicek, J; Mandusić, A; Rekić, B; Zanić Grubisić, T, 1998) | 0.66 |
" Both CBZ and CBZ-epoxide (CBZ-E) blood levels were elevated, and the symptoms resolved quickly when CBZ dosage was reduced and CLB discontinued." | ( Carbamazepine intoxication with negative myoclonus after the addition of clobazam. Genton, P; Mesdjian, E; Nguyen, VH, 1998) | 1.74 |
"The aim of our work was to define the kinetic profile of carbamazepine (CBZ), in order to improve on dosing schedules through a Bayesian approach." | ( Kinetic profile of carbamazepine in an adult Portuguese outpatient population. Almeida, AM; Caramona, MM; Costa, IM; Falcão, AC; Leitão, F; Sales, F; Santos, J, 1998) | 0.87 |
"Our results provide specific data on CBZ disposition in a Portuguese population and given the wide variability in the literature values, our data may help improve dosing of CBZ in Portuguese patients." | ( Kinetic profile of carbamazepine in an adult Portuguese outpatient population. Almeida, AM; Caramona, MM; Costa, IM; Falcão, AC; Leitão, F; Sales, F; Santos, J, 1998) | 0.63 |
" The results showed that autoinduction of carbamazepine metabolism under the chosen dosage regimen was complete within 14 days after start of treatment and that the criteria for bioequivalence were met." | ( Bioavailability study of two carbamazepine containing sustained release formulations after multiple oral dose administration. Blume, H; Evers, G; Mazur, D; Retzow, A; Schug, B; Wangemann, M, 1998) | 0.86 |
"Patients taking CBZ entered a 4-week run-in period to stabilise their dosage regimen to Tegretol tablets and blinded capsules containing Tegretol tablets." | ( Adjustment of carbamazepine dose to offset the effects of the interaction with remacemide hydrochloride in a double-blind, multicentre, add-on drug trial (CR2237) in refractory epilepsy. Jamieson, V; Lucas, SB; Mawer, GE; Wild, JM, 1999) | 0.66 |
"CBZ dosage reductions ranging from 14 to 50% were required by 63% of patients who received REM." | ( Adjustment of carbamazepine dose to offset the effects of the interaction with remacemide hydrochloride in a double-blind, multicentre, add-on drug trial (CR2237) in refractory epilepsy. Jamieson, V; Lucas, SB; Mawer, GE; Wild, JM, 1999) | 0.66 |
" In those patients who use these drugs at increased dosage levels or for long periods, the possibility of tubular dysfunction may be increased, and these dysfunctions may manifest in clinical symptoms." | ( N-acetyl-beta-glucosaminidase and beta-galactosidase activity in children receiving antiepileptic drugs. Cenani, A; Cengiz, M; Cengiz, S; Seven, M; Yüksel, A, 1999) | 0.3 |
" Twelve adult patients with seizures controlled by an individualized fixed dosage of antiepilepsy medication (carbamazepine or phenytoin) participated in each study." | ( Lack of pharmacokinetic drug interactions between tiagabine and carbamazepine or phenytoin. Boellner, SW; Cao, GX; Cato, A; Guenther, HJ; Gustavson, LE; Qian, JX; Sommerville, KW, 1998) | 0.75 |
" dosing with CBTL or TXR." | ( Controlled, multidose, pharmacokinetic evaluation of two extended-release carbamazepine formulations (Carbatrol and Tegretol-XR). Evans, G; Limsakun, T; Mason, DH; Stevens, RE, 1998) | 0.53 |
"Plasma concentrations of lamotrigine, an antiepileptic drug obtained in three adult controlled clinical trials conducted in the United States were pooled and analyzed using NONMEM, a population pharmacokinetic computer program, to facilitate development of dosing guidelines." | ( Population pharmacokinetics of lamotrigine adjunctive therapy in adults with epilepsy. Chen, C; Cox, E; Fiedler-Kelly, J; Grasela, TH; Risner, ME; Womble, GP, 1999) | 0.3 |
" Transfected cells were dosed with several known inducers of CYP3A4 and the levels of SPAP were measured." | ( A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human CYP3A4 gene in vitro. Gibson, GG; Goldfarb, PS; Gray, TJ; Ogg, MS; Tarbit, M; Williams, JM, 1999) | 0.3 |
" Dose-response relationships are quantitatively different among the models." | ( Carbamazepine pharmacokinetics-pharmacodynamics in genetically epilepsy-prone rats. Birkhahn, D; Burk, A; Dailey, JW; Graumlich, JF; Jobe, PC; McLaughlin, RG; Shah, N, 1999) | 1.75 |
" When it recurred, pain was less intense and was better controlled with a reduced dosage of carbamazepine." | ( Surgical treatment of trigeminal neuralgia. Hong-Sai, L, 1999) | 0.52 |
" Dose-response inhibition curves determined on the control receptor and on ADNFLE-mutant receptors showed a greater sensitivity of the mutants to CBZ, with median inhibitory concentrations (IC50s) in the range of the antiepileptic plasma levels of CBZ." | ( Mutated nicotinic receptors responsible for autosomal dominant nocturnal frontal lobe epilepsy are more sensitive to carbamazepine. Bertrand, D; Bertrand, S; Picard, F; Steinlein, OK, 1999) | 0.51 |
" Following a short titration period, the dosage was individualised for each patient while maintaining the blind over the next 24 weeks." | ( Multicentre, double-blind, randomised comparison between lamotrigine and carbamazepine in elderly patients with newly diagnosed epilepsy. The UK Lamotrigine Elderly Study Group. Brodie, MJ; Giorgi, L; Overstall, PW, 1999) | 0.54 |
" Valproate, when the proper therapeutic dosage was belatedly realized, was seen as a superior treatment for generalized and partial epilepsies." | ( Clinical experience with new antiepileptic drugs: antiepileptic drugs in Europe. Loiseau, PJ, 1999) | 0.3 |
" Because dosing is often modest, cost should rarely be the overriding factor in choosing a drug for a patient with newly diagnosed epilepsy in the developed world." | ( Monostars: an aid to choosing an antiepileptic drug as monotherapy. Brodie, MJ, 1999) | 0.3 |
" The gabapentin dosage was titrated to effective tolerated dose up to 2400 mg/day." | ( Gabapentin as adjunctive therapy for partial seizures. Bruni, J, 1999) | 0.3 |
" Seizures became diurnal and frequent, not modified by carbamazepine (CBZ) or valproate (VPA) but responding to VPA and lamotrigine (LTG) with recommended dosage schedules for this combination." | ( Paradoxic reaction to lamotrigine in a child with benign focal epilepsy of childhood with centrotemporal spikes. Boyd, S; Catania, S; Cross, H; de Sousa, C, 1999) | 0.55 |
" Further studies are required to establish its role and the optimal dosage regimen of charcoal to be administered." | ( Position statement and practice guidelines on the use of multi-dose activated charcoal in the treatment of acute poisoning. American Academy of Clinical Toxicology; European Association of Poisons Centres and Clinical Toxicologists. , 1999) | 0.3 |
" However, despite increasing the dosage of CBZ, rats experienced more behavioral seizures during the second week after TNTX injection." | ( Insights into the tetanus toxin model of early-onset epilepsy from long-term video monitoring during anticonvulsant therapy. Anderson, AE; Hrachovy, RA; Lee, I; Rashid, S; Swann, JW, 1999) | 0.3 |
" Nefazodone 200 mg twice daily was added to the dosing regimen from days 40 to 44, and a subsequent 0- to 48-hour pharmacokinetic analysis was performed on day 44." | ( Carbamazepine-nefazodone interaction in healthy subjects. Cheuvart, B; Cosson, JP; Decourt, JP; Girault, J; Ingrand, I; Istin, B; Laroudie, C; Salazar, DE, 2000) | 1.75 |
" In one group, dosage was adjusted to achieve serum AED concentration within a target range (10-20 microg/ml for PHT, 15-40 microg/ml for PB, 4-11 microg/ml for CBZ, and 40-100 microg/ml for VPA), whereas in the other group, dosage was adjusted on clinical grounds." | ( A multicenter randomized controlled trial on the clinical impact of therapeutic drug monitoring in patients with newly diagnosed epilepsy. The Italian TDM Study Group in Epilepsy. Bartoli, A; Cian, P; Fattore, C; Gatti, G; Jannuzzi, G; Monaco, F; Perucca, E, 2000) | 0.31 |
" After lamotrigine was added for better seizure control and the dosage of gabapentin was tapered, anorgasmia improved." | ( Improved sexual function in three men taking lamotrigine for epilepsy. Carwile, ST; Husain, AM; Miller, PP; Radtke, RA, 2000) | 0.31 |
"Determining antiepileptic drug (AED) concentration in biological fluids and calculating its dosage on this basis is a long-term method in the treatment of epilepsy." | ( [Therapeutic antiepileptic drug monitoring: thirteen years of experience in the Laboratory of Clinical Neuropharmacology in the Chair and Department of Developmental neurology]. Galas-Zgorzalewicz, B; Steinborn, B, 2000) | 0.31 |
" Everyone received a drug dosage which gave an adequate therapeutic plasma concentration and satisfactory seizure control." | ( [Bimodal evoked potentials during long-term therapy with conventional or slow release preparations of carbamazepine and valproic acid in children and adolescents with epilepsy]. Zgorzalewicz, M, 2000) | 0.52 |
" When alternate drug therapy is not possible, dosage adjustments, therapeutic drug monitoring, and careful clinical observation may help reduce adverse clinical consequences." | ( Carbamazepine--indinavir interaction causes antiretroviral therapy failure. Brinkman, K; Burger, DM; Hekster, YA; Hugen, PW; Koopmans, PP; Schuurman, R; ter Hofstede, HJ, 2000) | 1.75 |
" We report 11 MS patients with trigeminal neuralgia (TN): 6 intolerant to a therapeutic dosage of CBZ, showing serious adverse effects and subsequently treated with a combination of low-dose CBZ and gabapentin (GBP) (group 1); 5 treated with lamotrigine (LMT), showing adverse effects and subsequently treated with GBP (group 2)." | ( Low-dose gabapentin combined with either lamotrigine or carbamazepine can be useful therapies for trigeminal neuralgia in multiple sclerosis. Leandri, M; Mancardi, GL; Messmer Uccelli, M; Solaro, C; Uccelli, A, 2000) | 0.55 |
" Weighting the data for per-patient dosage values fails to discern a color effect." | ( Is a "color effect" demonstrated for hair analysis of carbamazepine? Mieczkowski, T, 2000) | 0.56 |
" After discontinuing RTV and reducing the dosage of CBZ, the serum concentration of CBZ returned to the optimal range, symptoms subsided, and liver function returned to baseline." | ( Potential interaction between ritonavir and carbamazepine. Feldman, MD; Fujii, T; Kato, Y; Kayser, SR; Mizoguchi, N; Takata, N; Ueda, K, 2000) | 0.57 |
" The wide variation in dose-response and dose-toxicity relationships may reflect different neurobiologies causing refractory epilepsy and differential efficacy of AED combinations." | ( Topiramate in refractory epilepsy: a prospective observational study. Brodie, MJ; Sills, GJ; Stephen, LJ, 2000) | 0.31 |
"To evaluate plasma homocysteine (Hcy) concentrations in children receiving sodium valproate (VPA) and carbamazepine (CBZ), monotherapy, in comparison with healthy control subjects and to determine the possible relationship between Hcy levels and dosage and plasma concentrations of the antiepileptic drugs." | ( Hyperhomocysteinemia in children treated with sodium valproate and carbamazepine. Chiarelli, F; Giuva, T; Morgese, G; Pascarella, R; Trotta, D; Verrotti, A, 2000) | 0.76 |
" TPM is introduced at 25 mg and increased with weekly 25mg/d increments to a minimum dosage of 200 mg/d." | ( A multicenter, randomized clinical study to evaluate the effect on cognitive function of topiramate compared with valproate as add-on therapy to carbamazepine in patients with partial-onset seizures. Aldenkamp, AP; Baker, G; Chadwick, D; Cooper, P; de Haan, GJ; Doelman, J; Duncan, R; Gassmann-Mayer, C; Hughson, C; Hulsman, J; Mulder, OG; Overweg, J; Pledger, G; Rentmeester, TW; Riaz, H; Wroe, S, 2000) | 0.51 |
"The goal of the study was to evaluate the safety and efficacy of a broad oxcarbazepine (OXC) dosage range (600, 1200, and 2400 mg/d) as adjunctive therapy for uncontrolled partial seizures and to determine the relationship between trough plasma 10-monohydroxy derivative concentrations and OXC safety and efficacy." | ( Oxcarbazepine placebo-controlled, dose-ranging trial in refractory partial epilepsy. Barcs, G; D'Souza, J; Elger, CE; Flesch, G; Kramer, L; Moore, A; Scaramelli, A; Stefan, H; Sturm, Y; Walker, EB, 2000) | 0.31 |
"Carbatrol, a new dosage form of carbamazepine (CBZ), was developed consisting of three different types of pellets (immediate release, controlled release, and enteric release)." | ( The influence of food on the bioavailability of a twice-daily controlled release carbamazepine formulation. Browne, S; Couch, R; Halstenson, C; McLean, A; Slaughter, E; Zhang, Y, 2001) | 0.82 |
"The study was conducted in 16 controlled and 15 uncontrolled adult epileptic patients receiving CBZ monotherapy for the previous 3 or more months, without any dosage change." | ( Association of drug levels & pharmacokinetics of carbamazepine with seizure control. Puri, V; Tripathi, KD; Vasudev, A, 2000) | 0.56 |
" Similarly, valproate combined with antipsychotics provided greater improvement in mania than antipsychotic medication alone and resulted in lower dosage of the antipsychotic medication." | ( Novel treatments for bipolar disorder. Bowden, CL, 2001) | 0.31 |
" Therefore, despite considerable reductions in total serum levels of IMI and DMI, but when the unchanged free fraction concentration of these compounds is maintained, a dosage elevation of IMI does not seem to be necessary after CBZ addition to TCA therapy." | ( Pharmacokinetic interaction between imipramine and carbamazepine in patients with major depression. Szymura-Oleksiak, J; Wasieczko, A; Wyska, E, 2001) | 0.56 |
"The main advantages of solid dispersions (the drug could be maintained in a bioavailable form, dosage reduction and cleaner manufacturing conditions) provide scope for the continued interest in field." | ( Computer supported studies on design and evaluation of solid dispersions of carbamazepine. Boral, A; Das, B; Ghosh, LK; Gupta, BK; Ray, S, ) | 0.36 |
" In particular, the gas antisolvent crystallisation technique (GAS), using supercritical carbon dioxide as processing medium, has been considered to prepare an enhanced release dosage form for of the poorly soluble carbamazepine, employing PEG 4000 as a hydrophilic carrier." | ( Processing of carbamazepine-PEG 4000 solid dispersions with supercritical carbon dioxide: preparation, characterisation, and in vitro dissolution. Filipović-Grcić, J; Kikic, I; Moneghini, M; Perissutti, B; Voinovich, D, 2001) | 0.86 |
" The dosage of other mood stabilizer drugs remained unchanged throughout the 6-week follow-up." | ( [Effectiveness and safety of topiramate in treatment-resistant bipolar disorder]. Arrufat, E; García-Castrillón, A; García-Parés, G; Gilabert, A; Luna, MJ; Rodríguez, A; Vieta, E, ) | 0.13 |
" The correlation between carbamazepine clearance and patient-specific characteristics may thus allow dosage adjustment to be made to achieve target steady-state plasma concentrations." | ( Population pharmacokinetics of carbamazepine in Singapore epileptic patients. Chan, E; Hue, SS; Lee, HS, 2001) | 0.9 |
" Rates of metabolism in children may be much faster than in nonelderly adults, requiring dosing adjustments to ensure enough medication is used to control seizures." | ( Treatment of epilepsy in 3 specialized populations. Leppik, IE, 2001) | 0.31 |
" The authors conclude that it is unnecessary to adjust the oxcarbazepine dosage when performing single-volume plasma exchanges or even multiple exchanges during an extended period." | ( Removal of 10-hydroxycarbazepine by plasmapheresis. Balslev, T; Christensen, J; Dam, M; Heinsvig, EM; Poulsen, JH; Villadsen, J, 2001) | 0.31 |
"The aim of this study was to define the pharmacokinetic profile of free carbamazepine (F-CBZ) in adult Omani epileptic patients in order to improve on dosing schedules through population pharmacokinetic analysis using the NONMEM program." | ( Population pharmacokinetics of free carbamazepine in adult Omani epileptic patients. Aarons, L; Ahmed, IA; Deleu, D, 2001) | 0.82 |
"Steady-state trough F-CBZ serum concentrations, carbamazepine (CBZ) dosing history and associated information were collected prospectively." | ( Population pharmacokinetics of free carbamazepine in adult Omani epileptic patients. Aarons, L; Ahmed, IA; Deleu, D, 2001) | 0.84 |
" However, CL increased as a function of dosing rate and consequently was modelled as a linear function of steady-state concentration." | ( Population pharmacokinetics of free carbamazepine in adult Omani epileptic patients. Aarons, L; Ahmed, IA; Deleu, D, 2001) | 0.59 |
"In order to establish steady-state dosage regimens, a population pharmacokinetic model is proposed, based on the patient's dose, to estimate the individual CL for an Omani epileptic patient receiving CBZ in monotherapy." | ( Population pharmacokinetics of free carbamazepine in adult Omani epileptic patients. Aarons, L; Ahmed, IA; Deleu, D, 2001) | 0.59 |
" Dosage can be increased by 8-10 mg/kg/day in weekly increments if necessary for seizure control." | ( Recommendations on the clinical use of oxcarbazepine in the treatment of epilepsy: a consensus view. Arroyo, S; Baulac, M; Dam, M; Dulac, O; Friis, ML; Kälviäinen, R; Krämer, G; Pedersen, B; Sachdeo, R; Schmidt, D; van Parys, J, 2001) | 0.31 |
" Although structurally similar to carbamazepine, significant differences exist in the pharmacokinetics, drug interaction potential, adverse-effect profile, and dosage and titration between these two agents, and they should be considered distinct therapeutic agents." | ( Oxcarbazepine in the treatment of epilepsy. Glauser, TA, 2001) | 0.59 |
"The aim of this research was to use a ram extruder to prepare directly a fast release dosage form with uniform shape and density, containing carbamazepine (C) as a water-insoluble drug and polyethylene glycol 4000 (PEG) as a low melting binder." | ( Preparation of extruded carbamazepine and PEG 4000 as a potential rapid release dosage form. Newton, JM; Perissutti, B; Podczeck, F; Rubessa, F, 2002) | 0.82 |
" According to the literature, OCBZ is regarded as effective in acute mania and appears to reduce the dosage of neuroleptics required for the treatment of affective and schizoaffective disorders." | ( Oxcarbazepine in affective and schizoaffective disorders. Dietrich, DE; Emrich, HM; Kropp, S, 2001) | 0.31 |
" An exchange in a dosage ratio of 1:1-1:1." | ( [Ad hoc change from carbamazepine to oxcarbazepine--effectiveness and tolerance. A retrospective analysis]. Homberg, V; Kowalik, A; Schulze-Bonhage, A, 2001) | 0.63 |
" Patients were first treated with oxcarbazepine 1200 +/- 600 mg daily dosage (mean +/- SD) and subsequently with surgery of their choice." | ( Long-term cohort study comparing medical (oxcarbazepine) and surgical management of intractable trigeminal neuralgia. Patsalos, PN; Zakrzewska, JM, 2002) | 0.31 |
"The individualization of carbamazepine (CBZ) dosage regimen based on estimation of pharmacokinetic (PK) parameters and measurement of serum drug concentration in epileptic patients can help to control epilepsy." | ( Bayesian estimation of six different sets of carbamazepine pharmacokinetic parameters in Egyptian adult epileptic patients. EL Desoky, ES; Kandil, MR, 2002) | 0.88 |
"To compare the effects of carbamazepine, remacemide, and placebo on actual driving performance during a 12-day incremental dosing regimen." | ( A comparative study of the effects of carbamazepine and the NMDA receptor antagonist remacemide on road tracking and car-following performance in actual traffic. Lamers, J; Lewis, M; Lockton, A; Mobbs, E; Muntjewerff, D; Ramaekers, G; Sanders, N; Verhey, F, 2002) | 0.89 |
" Blood and saliva samples were taken simultaneously at 0 hours and 24 hours of CBZ dosing from 31 epileptic patients, receiving CBZ monotherapy for three or more months." | ( Correlation of serum and salivary carbamazepine concentration in epileptic patients: implications for therapeutic drug monitoring. Puri, V; Tripathi, KD; Vasudev, A, 2002) | 0.59 |
" The authors assessed eight patients on CBZ monotherapy (CBZ extended-release capsules) at a mean dosage of 625 +/- 253 mg/day (range, 400-1,200 mg/day) for at least 1 year." | ( Carbamazepine-risperidone interactions in patients with epilepsy. Monaco, F; Mula, M, ) | 1.57 |
" Age at onset, duration of epilepsy, seizure type, seizure frequency, localisation, years on CBZ, and CBZ dosage were not related to cognitive functioning or HRQOL." | ( Cognition and health-related quality of life in a well-defined subgroup of patients with partial epilepsy. Adèr, HJ; Engelberts, NH; Heimans, JJ; Jolles, J; Kasteleijn-Nolst Trenité, DG; Klein, M; van Boxtel, MP; van der Ploeg, HM, 2002) | 0.31 |
" The aim of this study was to develop and validate a HPLC method allowing simultaneous dosage of oxcarbazepine, 10-hydroxycarbamazepine, epoxycarbamazepine, carbamazepine, phenobarbital and phenytoïn." | ( LC determination of oxcarbazepine and its active metabolite in human serum. Levert, H; Odou, P; Robert, H, 2002) | 0.52 |
" Patients were switched to controlled-release CBZ and the dosage was slowly adjusted." | ( [A practical study of the efficacy of a delayed-action preparation of carbamazepine (Tegretol CR 400) in the treatment of patients with partial epilepsy ]. Janković, SM; Lević, Z; Sokić, DV; Vojvodić, NM, ) | 0.37 |
" conventional carbamazepine had better efficiency, based on an excellent tolerance, favorable daily dosage and superior compliance." | ( [A practical study of the efficacy of a delayed-action preparation of carbamazepine (Tegretol CR 400) in the treatment of patients with partial epilepsy ]. Janković, SM; Lević, Z; Sokić, DV; Vojvodić, NM, ) | 0.73 |
"The purpose of this study was to investigate the relationship of changes in the enzyme-inducing anticonvulsant daily dosage (drug score) to variations in urinary D-glucaric acid excretion and gamma-glutamyltransferase and beta-glucuronidase serum activities." | ( Relationship between changes in drug score, D-glucaric acid excretion, and gamma-glutamyltransferase and beta-glucuronidase serum activities during anticonvulsant treatment. Fernández, MP; Hermida, J; Tutor, JC, 2002) | 0.31 |
"Proper formulation is an important aspect of any dosage form design." | ( Compatibility studies between carbamazepine and tablet excipients using thermal and non-thermal methods. Joshi, BV; Patil, VB; Pokharkar, VB, 2002) | 0.6 |
" Adjusting the maintenance dosage of H(2)-histamine antagonists has been recommended in elderly patients since age-related reduction in renal plasma flow, glomerular filtration rate and renal tubular function may be present, which can in turn elevate histamine levels in plasma and cerebrospinal fluid." | ( H(2)-histamine antagonist (famotidine) induced adverse CNS reactions with long-standing secondary mania and epileptic seizures. Bergemann, N; Diebold, K; Mundt, C; Roesch-Ely, D; Sartor, K; von Einsiedel, RW, 2002) | 0.31 |
" dosing with either Carbatrol (extended-release beads) or Tegretol-XR (an osmotic pump tablet, an Oros tablet) using compartmental method." | ( Reanalysis of carbamazepine and carbamazepine-epoxide pharmacokinetics after multiple dosing of extended release formulation. Dechasathian, S; Konsil, J; Mason, DH; Stevens, RE, ) | 0.49 |
" When compared to published literature of single dose data, the investigation of CBZ and CBZ-E pharmacokinetics from this study suggested that autoinduction might occur by the fifth day of dosing and might partly contribute to the sigmoidal shape of CBZ-E profiles." | ( Reanalysis of carbamazepine and carbamazepine-epoxide pharmacokinetics after multiple dosing of extended release formulation. Dechasathian, S; Konsil, J; Mason, DH; Stevens, RE, ) | 0.49 |
" Subsequent experience suggests that dosage needs were overestimated." | ( Low-dose topiramate in adults with treatment-resistant partial-onset seizures. Gassmann-Mayer, C; Guberman, A; Neto, W, 2002) | 0.31 |
" After dosage of 800 mg of carbamazepine in 2/7 volunteers the finding was unchanged, in 3/7 second stage disturbance was found and in 2/7 third stage of disturbance in the smooth tracking test was found." | ( [The smooth tracking test and rotation stimulation test in disorders of the vestibular system caused by carbamazepine]. Canji, K; Jovićević, J; Kljajić, V; Milosević, D; Savović, S; Vlaski, L, ) | 0.64 |
" lower dosage in Japan, emerged and caused the delay of publication of our results in Western journals." | ( [A history of investigation on the mood-stabilizing effect of carbamazepine in Japan]. Okuma, T, 2002) | 0.56 |
" Dosage of OXC, serum levels of the active metabolite of OXC, antiepileptic comedication or patients' age and gender were of no predictive value for the development of hyponatremia." | ( Oxcarbazepine-induced hyponatremia and the regulation of serum sodium after replacing carbamazepine with oxcarbazepine in children. Boenigk, HE; Holtmann, M; Korn-Merker, E; Krause, M; Opp, J; Tokarzewski, M, 2002) | 0.54 |
"This work describes a new approach to prepare a fast-release dosage form for carbamazepine (CBZ), involving the use of melt granulation process in high shear mixer for the production of tablets." | ( Formulation design of carbamazepine fast-release tablets prepared by melt granulation technique. Moneghini, M; Perissutti, B; Rubessa, F; Voinovich, D, 2003) | 0.86 |
"A population pharmacokinetic model was proposed to estimate the individual CL for Chinese patients receiving CBZ in terms of patient's dose, TBW, and comedications to establish a priori dosage regimens." | ( Population pharmacokinetics of carbamazepine in Chinese epilepsy patients. Hu, M; Jiao, Z; Shi, XJ; Zhang, JH; Zhong, MK, 2003) | 0.6 |
" Additional supporting findings demonstrated that 43-71% of patients with partial onset, generalized or undetermined epilepsy were seizure free after oxcarbazepine monotherapy (mean dosage 27." | ( Oxcarbazepine: a review of its use in children with epilepsy. Bang, L; Goa, K, 2003) | 0.32 |
" For those who were treated, they were easily controlled on a low dose of carbamazepine (median dosage of 12." | ( Benign childhood epilepsy with centrotemporal spikes: a study of 50 Chinese children. Chan, KY; Ma, CK, 2003) | 0.55 |
" Although its half-life is relatively short (6 to 8 hours), its duration of action is longer than anticipated from its pharmacokinetics in plasma, and a twice-daily dosing regimen is adequate to produce the desired response." | ( The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come? Johannessen, SI; Perucca, E, 2003) | 0.32 |
"This study is the open-label extension phase that followed a multicenter, randomized, double-blind, dose-response clinical study of OXC monotherapy in patients with medically refractory partial epilepsy." | ( Sustained efficacy and long-term safety of oxcarbazepine: one-year open-label extension of a study in refractory partial epilepsy. Beydoun, A; D'Souza, J; Kutluay, E; McCague, K; Sachdeo, RC, 2003) | 0.32 |
" The drug dosage reduction lasted from 3 to 24 months." | ( [Treatment termination in children with idiopathic generalized epilepsy and cryptogenic focal epilepsy]. Marszał, E; Szwed-Białozyt, B, 2003) | 0.32 |
" Although few studies are available, extrapolations from research in young people and elderly patients without dementia provide several recommendations for the management of seizures in patients with dementia: exclude symptomatic causes of seizures before committing to antiepileptic drug therapy; treat after a first seizure if there is evidence of focal neurological involvement or a risk of recurrent seizures; use antiepileptic drugs with minimal cognitive adverse effects, such as carbamazepine, valproic acid, gabapentin and lamotrigine; and use the lowest possible dosage and monitor antiepileptic drug levels, where possible." | ( Seizures in elderly patients with dementia: epidemiology and management. Lim, G; Mendez, M, 2003) | 0.48 |
" Hill slope coefficients for the tested anticonvulsants indicate that the dose-response curve was less steep for gabapentin than for phenytoin, carbamazepine and ethosuximide." | ( Potent analgesic effects of anticonvulsants on peripheral thermal nociception in rats. Jevtovic-Todorovic, V; Rastogi, AJ; Todorovic, SM, 2003) | 0.52 |
" Computer simulations were carried out to investigate the effect of missing or delaying doses of carbamazepine extended-release capsules (CBZ-ERC) on plasma CBZ levels and the optimal dosing strategy to return plasma concentrations to therapeutic levels." | ( Simulation of the effect of patient nonadherence on plasma concentrations of carbamazepine from twice-daily extended-release capsules. Clausen, S; Garnett, WR; McLean, AM; Tulloch, SJ; Zhang, Y, 2003) | 0.77 |
" Patients were converted during an =8-week Escalation/Taper Phase from their prestudy antiepileptic drug (carbamazepine, phenytoin, or valproate) to lamotrigine via a protocol-specified dosing algorithm or to conventional therapy via standard dosing guidelines." | ( Lamotrigine monotherapy compared with carbamazepine, phenytoin, or valproate monotherapy in patients with epilepsy. Hammer, AE; Kaminow, L; Schimschock, JR; Vuong, A, 2003) | 0.8 |
" Additional supporting findings demonstrated that 43-71% of patients with partial onset, generalised or undetermined epilepsy were seizure free after oxcarbazepine monotherapy (mean dosage 27." | ( Spotlight on oxcarbazepine in epilepsy. Bang, LM; Goa, KL, 2004) | 0.32 |
"The quality and performance of a solid oral dosage form depends on the choice of the solid phase, the formulation design, and the manufacturing process." | ( Phase transformation considerations during process development and manufacture of solid oral dosage forms. Law, D; Qiu, Y; Schmitt, EA; Zhang, GG, 2004) | 0.32 |
" Three decision trees for solid oral dosage forms or liquid suspensions are provided for evaluating when and how polymorphs of drug substances should be monitored and controlled in ANDA submissions." | ( Regulatory considerations of pharmaceutical solid polymorphism in Abbreviated New Drug Applications (ANDAs). Adams, RC; Furness, MS; Gill, DS; Holcombe, FO; Raw, AS; Yu, LX, 2004) | 0.32 |
" However, there is no information available on the number of therapeutic abortions, or the different types of epilepsy or drug dosage in the two treatment groups." | ( Major malformations in infants exposed to antiepileptic drugs in utero, with emphasis on carbamazepine and valproic acid: a nation-wide, population-based register study. Källén, B; Wide, K; Winbladh, B, 2004) | 0.55 |
" Reduction in VPA dosage in the third patient produced no improvement." | ( Reversible parkinsonism with normal beta-CIT-SPECT in patients exposed to sodium valproate. Clough, P; Duncan, S; Easterford, K; Fallon, K; Kellett, M, 2004) | 0.32 |
"Carbatrol (CBR) is a new multiple-unit, sustained-release dosage form of carbamazepine (CBZ) developed by Pharmavene." | ( A multicenter, placebo-controlled, double-blind study of efficacy of a new form of carbamazepine (Carbatrol) in refractory epileptic patients. Boćkowski, L; Jedrzejczak, J; Kułak, W; Majkowski, J; Smigielska-Kuzia, J; Sobaniec, W, ) | 0.59 |
" Although a high inter-subject variability was observed, the results pointed to the feasibility of using betaCD in order to modulate CBZ release and absorption, as well as to reduce the drug dosage maintaining the same plasma levels." | ( Bioavailability of carbamazepine:beta-cyclodextrin complex in beagle dogs from hydroxypropylmethylcellulose matrix tablets. Bassani, VL; Bertuol, JB; Dalla Costa, T; Groch, KR; Koester, LS; Mayorga, P; Moellerke, R; Xavier, CR, 2004) | 0.65 |
" It is also recommended to avoid saliva collection within 8 hours after OXC dosing to allow complete absorption and transformation of the parent drug." | ( Feasibility and limitations of oxcarbazepine monitoring using salivary monohydroxycarbamazepine (MHD). Baumann, RJ; DeGrauw, TJ; Fakhoury, TA; Grim, SA; Miles, MV; Ryan, MA; Strawsburg, RH; Tang, PH, 2004) | 0.55 |
"The aims of our study were to evaluate whether deficits in color vision exist in epileptic adolescents, to study if monotherapy with valproic acid (VPA) and carbamazepine (CBZ) can affect color vision, and to determine the possible relationship between abnormal color vision tests and AEDs dosage and their serum concentrations." | ( Color vision in epileptic adolescents treated with valproate and carbamazepine. Chiarelli, F; Gallenga, PE; Lobefalo, L; Morgese, G; Priolo, T; Rapinese, M; Trotta, D; Verrotti, A, 2004) | 0.76 |
" Pearson's correlation test was performed to correlate chromatic sense and perimetric data and AEDs dosage and serum concentrations." | ( Color vision in epileptic adolescents treated with valproate and carbamazepine. Chiarelli, F; Gallenga, PE; Lobefalo, L; Morgese, G; Priolo, T; Rapinese, M; Trotta, D; Verrotti, A, 2004) | 0.56 |
" Within each of 4 dosage groups of 8 healthy male adult subjects, 2 subjects were randomized to receive placebo, and the remaining 6 subjects were randomized to receive BIA 2-093 (200 mg bid, 400 mg qd, 800 mg qd, and 1200 mg qd) for 8 days." | ( Safety, tolerability, and pharmacokinetic profile of BIA 2-093, a novel putative antiepileptic, in a rising multiple-dose study in young healthy humans. Almeida, L; Soares-da-Silva, P, 2004) | 0.32 |
" Two hours after a documented overdosage of more than 100 tablets oxcarbazepine, the serum level of the parent compound was 10-fold higher than the therapeutic dosage (31." | ( Severe overdosage with the antiepileptic drug oxcarbazepine. Cilissen, J; De Heer, F; Janknegt, R; L'Ortije, WH; Nel, JE; van Opstal, JM, 2004) | 0.32 |
" Based on an expected maximum drug release criterion of 85% in a reasonable time, at a relatively slow drug release rate and within a dosing interval, a spindle speed of 25 rpm was found to be the most appropriate." | ( Choice of rotation speed (rpm) for bio-relevant drug dissolution testing using a crescent-shaped spindle. Qureshi, SA, 2004) | 0.32 |
" CBZ, PB, OXC, and VPA displayed a dose-response relation." | ( Fracture risk associated with use of antiepileptic drugs. Mosekilde, L; Rejnmark, L; Vestergaard, P, 2004) | 0.32 |
" ZNS was initiated at 2mg/kg; daily dosage was doubled at weekly intervals to achieve maintenance dosage (8." | ( Zonisamide monotherapy with once-daily dosing in children with cryptogenic localization-related epilepsies: clinical effects and pharmacokinetic studies. Miura, H, 2004) | 0.32 |
" A small dosage of carbamazepine was remarkably effective in stopping the attacks." | ( Kinesigenic attacks with ictal electroencephalographic abnormalities. Akiyama, T; Kobayashi, K; Ohtsuka, Y; Oka, E, 2004) | 0.65 |
" Based on the lack of clinically relevant in vitro and in vivo effects, adjustment of carbamazepine dosing should not be required with concomitant zonisamide administration." | ( Carbamazepine pharmacokinetics are not affected by zonisamide: in vitro mechanistic study and in vivo clinical study in epileptic patients. Bergen, D; Garnett, W; Grundy, JS; Levy, RH; Mather, G; Ragueneau-Majlessi, I; Rosenfeld, W; Shah, J, 2004) | 1.99 |
"Various extended release carbamazepine (CBZ) formulations have been developed previously, in order to reduce the frequency of dosing in chronic therapy and to decrease the variability in drug plasma concentration." | ( Study of in-vitro release characteristics of carbamazepine extended release semisolid matrix filled capsules based on Gelucires. Abdallah, OY; Daabis, NA; El Massik, MA; Galal, S, 2004) | 0.89 |
"Eleven medication-naive patients, diagnosed with acute paranoid psychosis with associated EEG abnormalities, were divided into two treatment groups: sole fluphenazine group, with flexible dosing of 5-10 mg/day (n=6), and carbamazepine group (n=5) with the addition of carbamazepine (600 mg/day) to fluphenazine treatment." | ( Carbamazepine for acute psychosis with EEG abnormalities. Damjanović, A; Ivković, M; Marinković, D; Paunović, VR, ) | 1.76 |
"This article reviews preclinical and clinical data on the efficacy and tolerability of these 4 AEDs in the management of neuropathic pain, as well as the pharmacokinetics, drug-interaction potential, adverse effects, and dosing of these agents, with an emphasis on their use in older individuals." | ( Oxcarbazepine, topiramate, zonisamide, and levetiracetam: potential use in neuropathic pain. Guay, DR, 2003) | 0.32 |
" Although race and sex appear to influence delavirdine pharmacokinetics, men and women and patients of different races should receive similar mg/kg dosage regimens." | ( Population pharmacokinetics of delavirdine and N-delavirdine in HIV-infected individuals. Dicenzo, R; DiFrancesco, R; Fischl, M; Forrest, A; Friedland, G; Morse, GD; Para, M; Pollard, R; Shelton, M; Smith, PF, 2005) | 0.33 |
" Because of the differences among inter-individuals in the metabolic clearance of these drugs and their toxicity at certain levels of concentration in serum, the dosage should be regulated to maintain a therapeutic blood drugs level." | ( [Simultaneous analysis of theophylline, phenobarbital, amobarbital and carbamazepine in serum by high performance liquid chromatography]. Duan, S; Fu, S; Ren, Q, 1997) | 0.53 |
" These results provide evidence of a drug target polymorphism associated with the clinical use of AEDs and set the stage for a prospective evaluation of how pharmacogenetic diagnostics can be used to improve dosing decisions in the use of phenytoin and carbamazepine." | ( Genetic predictors of the maximum doses patients receive during clinical use of the anti-epileptic drugs carbamazepine and phenytoin. Cavalleri, GL; Depondt, C; Goldstein, DB; Sander, JW; Schorge, S; Sen, A; Shorvon, SD; Sisodiya, SM; Soranzo, N; Tate, SK; Thom, M; Wood, NW, 2005) | 0.72 |
"OXC, at a dosage of 900-1,200 mg/day, was administered for 5 consecutive weeks to 25 outpatients, 10 men and 15 women, aged 25 to 64 years, with bipolar or schizoaffective disorder." | ( Plasma concentrations of risperidone and olanzapine during coadministration with oxcarbazepine. Cacciola, M; D'Arrigo, C; La Torre, D; Migliardi, G; Pacetti, M; Rosaria Muscatello, M; Spina, E; Zoccali, R, 2005) | 0.33 |
" Carbamazepine at a dosage of 800 mg daily was the most effective medication used." | ( Auditory hallucinations after right temporal gyri resection. Brennan, DM; Stewart, B, 2005) | 1.24 |
" Detoxification followed a predefined dosage scheme." | ( Scheme-based benzodiazepine detoxification with oxcarbazepine -- a case report. Croissant, B; Diehl, A; Grosshans, M; Klein, O; Mann, K, 2005) | 0.33 |
" However, adverse event occurrence can be correlated to fluctuations in plasma drug levels that occur with varying dosing regimens of the many AEDs." | ( Carbamazepine extended-release capsules vs. oxcarbazepine: computer simulations of the effect of missed doses on drug plasma concentrations. Ahmad, A; Garnett, WR, 2005) | 1.77 |
" Histidine at a specific dosage range might serve as a beneficial adjuvant for the clinical treatment of epilepsy, especially when accompanied by impaired spatial memory." | ( Histidine enhances carbamazepine action against seizures and improves spatial memory deficits induced by chronic transauricular kindling in rats. Chen, Z; Jin, CL; Li, Q; Liu, LY; Xu, LS; Yang, LX; Zhu-Ge, ZB, 2005) | 0.66 |
" The medication dosage varied from 1 to 20 mg/kg daily." | ( [The efficacy of topiramate (topamax) in the treatment of resistant epilepsy in children]. Belousova, ED; Dorofeeva, MIu; Ermakov, AIu, 2005) | 0.33 |
" Linear regression analysis of dose-response relationship between the doses of 2-PMPA and their corresponding threshold values allowed the calculation of threshold increasing dose by 20% (TID20), which was 109." | ( 2-phosphonomethyl-pentanedioic acid (glutamate carboxypeptidase II inhibitor) increases threshold for electroconvulsions and enhances the antiseizure action of valproate against maximal electroshock-induced seizures in mice. Czuczwar, SJ; Luszczki, JJ; Mohamed, M, 2006) | 0.33 |
" A rectal dosage form of CBZ is not commercially available, although it is of particular interest when oral administration is impossible." | ( Thermally reversible in situ gelling carbamazepine liquid suppository. El-Kamel, A; El-Khatib, M, ) | 0.4 |
" Clinical heterogeneity was assessed by reviewing differences across trials in characteristics of randomized patients, dosing protocols and trial design." | ( Oxcarbazepine versus phenytoin monotherapy for epilepsy. Marson, AG; Muller, M; Williamson, PR, 2006) | 0.33 |
" In both instances, the carbamazepine dosage was decreased by 33%, which resulted in resolution of symptoms." | ( Carbamazepine toxicity induced by lopinavir/ritonavir and nelfinavir. Bates, DE; Herman, RJ, 2006) | 2.08 |
" Carbamazepine toxicity may be prevented by reducing the carbamazepine dosage by 25-50% when protease inhibitors are introduced." | ( Carbamazepine toxicity induced by lopinavir/ritonavir and nelfinavir. Bates, DE; Herman, RJ, 2006) | 2.69 |
" Because the dosing frequency of a particular medication can affect adherence rates, this important aspect of treatment must be taken into account." | ( Safety and efficacy of carbamazepine extended-release capsules in patients with bipolar disorder: QD vs BID. Ginsberg, LD, 2006) | 0.64 |
"The assessment compared qd dosing of CBZ-ERC with twice-daily (bid) dosing by matching the charts of the 23 study subjects to those of 23 similar control patients who had been taking CBZ-ERC dosed bid." | ( Safety and efficacy of carbamazepine extended-release capsules in patients with bipolar disorder: QD vs BID. Ginsberg, LD, 2006) | 0.64 |
"These findings suggest that CBZ-ERC dosed qd is comparable in efficacy, safety, and tolerability to CBZ-ERC dosed bid for patients with bipolar disorder." | ( Safety and efficacy of carbamazepine extended-release capsules in patients with bipolar disorder: QD vs BID. Ginsberg, LD, 2006) | 0.64 |
" Our results showed that age-related influences in CBZ pharmacokinetics in elderly patients should be considered in the optimal planning of CBZ dosage regimens." | ( Population pharmacokinetic modelling of carbamazepine in epileptic elderly patients: implications for dosage. Belousov, YB; Bondareva, IB; Guekht, AB; Gusev, EI; Jelliffe, RW; Melikyan, EG, 2006) | 0.6 |
" This formulation allows twice-daily dosing and minimizes plasma carbamazepine fluctuations." | ( Extended-release carbamazepine for acute bipolar mania: a review. Owen, RT, 2006) | 0.91 |
"A total of 116 outpatients 7 to 18 years of age with bipolar I disorder, manic or mixed, were recruited at 20 centers in the United States and randomly assigned to receive 7 weeks of double-blinded, flexibly dosed treatment with oxcarbazepine (maximum dose 900-2400 mg/day) or placebo." | ( A double-blind, randomized, placebo-controlled trial of oxcarbazepine in the treatment of bipolar disorder in children and adolescents. Berv, D; D'Souza, J; Emslie, GJ; Findling, RL; Kowatch, RA; Lehman, RB; Linden, D; McCague, K; Wagner, KD; Wamil, A; Wilens, TE, 2006) | 0.33 |
" The aims of our study were to evaluate whether color vision and macular function are impaired in epileptic adolescents, to study if the monotherapy with valproic acid (VPA) and carbamazepine (CBZ) can affect color vision and macular function and to determine the possible relationship between color vision, retinal function and antiepileptic drugs (AEDs) dosage and their serum concentrations." | ( Color vision and macular recovery time in epileptic adolescents treated with valproate and carbamazepine. Chiarelli, F; Gallenga, PE; Iannetti, P; Lobefalo, L; Spalice, A; Tocco, AM; Verrotti, A, 2006) | 0.75 |
" At baseline (day 1) mean dosage given was 796 for tiapride and 543 mg for carbamazepine." | ( Treatment of alcohol withdrawal syndrome with a combination of tiapride/carbamazepine: results of a pooled analysis in 540 patients. Barth, T; de Groot, M; Franz, M; Kienast, T; Reinert, T; Richter, C; Sander, G; Schmidt, P; Soyka, M, 2006) | 0.8 |
"Phenytoin dosing is critical in cancer patients as to decreased absorption secondary to chemotherapy-induced gastrointestinal toxicity, increased phenytoin metabolism in the liver secondary to chemotherapy, extreme patient profile that falls outside the predicted pharmacokinetic population, frequent hypoalbuminaemia and polydrug treatment." | ( Interactions of serum albumin, valproic acid and carbamazepine with the pharmacokinetics of phenytoin in cancer patients. Beijnen, JH; Boogerd, W; Huitema, AD; Joerger, M; Schellens, JH; van der Sande, JJ, 2006) | 0.59 |
" However, it provides a valuable aid to decision-making with regard to first-time dosing in children and study design." | ( Prediction of the clearance of eleven drugs and associated variability in neonates, infants and children. Johnson, TN; Rostami-Hodjegan, A; Tucker, GT, 2006) | 0.33 |
" For Treatment A carbamazepine was added in a dosage for targeted plasma levels of 4-6 mg/L." | ( Carbamazepine for prevention of oxaliplatin-related neurotoxicity in patients with advanced colorectal cancer: final results of a randomised, controlled, multicenter phase II study. Adelsberger, H; Bredenkamp, R; Eckel, F; Erdmann, J; Kullmann, F; Lersch, C; Mayr, M; Obermeier, F; Quasthoff, S; Schmelz, R; Schmid, RM; Stock, K; von Delius, S; Wagenpfeil, S, 2007) | 2.12 |
" Also discussed are findings concerning the continuation of acute treatments, including antidepressants, into the maintenance phase; dosage adjustments for maintenance treatment; the rationale for combination treatments; and implications of comorbid substance abuse and strategies for its management." | ( Maintenance treatment of bipolar disorder: Applying research to clinical practice. Chou, JC; Fazzio, L, 2006) | 0.33 |
" For these older drugs it has been common practice to adjust the dosage to achieve a serum drug concentration within a predefined 'therapeutic range', representing an interval where most patients are expected to show an optimal response." | ( Pharmacokinetic variability of newer antiepileptic drugs: when is monitoring needed? Johannessen, SI; Tomson, T, 2006) | 0.33 |
"The objective of this study was to compare the efficacy and safety of a chronotherapeutic dosing schedule of phenytoin and carbamazepine versus a conventional dosing schedule for the treatment of tonic-clonic epileptic patients." | ( Chronotherapeutic dose schedule of phenytoin and carbamazepine in epileptic patients. Mahesh, SD; Sangle, S; Yegnanarayan, R, 2006) | 0.8 |
"To characterize the possible pharmacokinetic interaction between the new antiepileptic and CNS drug RWJ-333369 and carbamazepine (CBZ) following multiple dosing in healthy subjects." | ( Pharmacokinetic interaction study between the new antiepileptic and CNS drug RWJ-333369 and carbamazepine in healthy adults. Bialer, M; Chien, S; Doose, DR; Novak, G; Solanki, B; Verhaeghe, T; Yao, C, 2006) | 0.76 |
"At steady-state following multiple dosing, RWJ-333369 peak plasma concentration (C(max)) and area under the concentration-time-curve within the dosing interval (AUCss) increased in proportion to dose." | ( Pharmacokinetic interaction study between the new antiepileptic and CNS drug RWJ-333369 and carbamazepine in healthy adults. Bialer, M; Chien, S; Doose, DR; Novak, G; Solanki, B; Verhaeghe, T; Yao, C, 2006) | 0.55 |
" Measuring antiepileptic drug levels in body fluids (therapeutic drug monitoring) is frequently used to optimise drug dosage for individual patients." | ( Therapeutic monitoring of antiepileptic drugs for epilepsy. Dahl, ML; Kimland, E; Tomson, T, 2007) | 0.34 |
" In this open study, 180 patients with newly-diagnosed, untreated epilepsy were randomised to treatment with the antiepileptic drug selected by their physician either with or without therapeutic drug serum level monitoring as an aid to dosage adjustments." | ( Therapeutic monitoring of antiepileptic drugs for epilepsy. Dahl, ML; Kimland, E; Tomson, T, 2007) | 0.34 |
" The oral delivery of the anti-psychotic agent carbamazepine was facilitated by preparing a non-disintegrating floating dosage form which can increase its absorption in the stomach by increasing the drug's gastric residence time." | ( Design and in vitro evaluation of floating drug delivery system for an antipsychotic agent: a technical report. Kar, M; Reddy, MS, ) | 0.39 |
" If a seizure occurred within 26 weeks of stabilization, dosage was increased incrementally to a maximum of levetiracetam 1,500 mg twice daily or carbamazepine 600 mg twice daily." | ( Comparison of levetiracetam and controlled-release carbamazepine in newly diagnosed epilepsy. Ben-Menachem, E; Brodie, MJ; Meencke, HJ; Perucca, E; Ryvlin, P, 2007) | 0.79 |
"Levetiracetam and controlled-release carbamazepine produced equivalent seizure freedom rates in newly diagnosed epilepsy at optimal dosing in a setting mimicking clinical practice." | ( Comparison of levetiracetam and controlled-release carbamazepine in newly diagnosed epilepsy. Ben-Menachem, E; Brodie, MJ; Meencke, HJ; Perucca, E; Ryvlin, P, 2007) | 0.86 |
" Carbamazepine (CBZ) and phenobarbital (PHB) during pregnancy should be used at the lowest dosage compatible with maternal disease." | ( Unilateral multicystic dysplastic kidney in infants exposed to antiepileptic drugs during pregnancy. Carta, M; Cimador, M; Corsello, G; De Grazia, E; Di Pace, MR; Giuffrè, M; Sergio, M, 2007) | 1.25 |
"OXC at a dosage of 1500-1800 mg/day might be beneficial in terms of alcohol relapse prevention." | ( High and low dosage oxcarbazepine versus naltrexone for the prevention of relapse in alcohol-dependent patients. Andreoli, S; Di Nicola, M; Janiri, L; Martinotti, G; Moroni, N; Pozzi, G; Romanelli, R, 2007) | 0.34 |
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process." | ( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential. Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A, ) | 0.13 |
" The discontinuation or dosage decrease of carbamazepine or oxcarbazepine may be associated with a slow increase of lamotrigine levels over several weeks and thus increase risk of lamotrigine toxicity that may manifest as oral ulcers." | ( Two case reports of oral ulcers with lamotrigine several weeks after oxcarbazepine withdrawal. de Leon, J; O'Neill, A, 2007) | 0.6 |
" The present case suggests that complete atrioventricular block may occur long after initiation of carbamazepine therapy in an older woman even if the daily dosage or the serum concentration of carbamazepine is low." | ( Intermittent complete atrioventricular block after long term low-dose carbamazepine therapy with a serum concentration less than the therapeutic level. Ide, A; Kamijo, Y, 2007) | 0.79 |
" Differences in outcome compared with previous trials may be related to different dosing rates and use of a sustained-release formulation for CBZ." | ( An international multicenter randomized double-blind controlled trial of lamotrigine and sustained-release carbamazepine in the treatment of newly diagnosed epilepsy in the elderly. Gjerstad, L; Isojärvi, J; Perucca, E; Saetre, E, 2007) | 0.55 |
" The mean dosage of OXC was 1033 mg daily." | ( Oxcarbazepine for treating paroxysmal painful symptoms in multiple sclerosis: a pilot study. Mancardi, GL; Restivo, D; Solaro, C; Tanganelli, P, 2007) | 0.34 |
" More certainly, they minimise concentration-related adverse effects, and the dosing flexibility and consistency of plasma concentrations may simplify the management of antiepileptic drug therapy." | ( Extended-release formulations for the treatment of epilepsy. Bialer, M, 2007) | 0.34 |
"A growing concern for the biopharmaceutical characterization of pharmaceutical products increased the interest in the evaluation and identification of physicochemical properties of drugs and dosage forms that govern its biological performance." | ( Biopharmaceutical characterization of carbamazepine immediate release tablets. In vitro-in vivo comparison. Cvetkovic, N; Djuric, Z; Homsek, I; Parojcic, J; Popadic, D, 2007) | 0.61 |
" Seven healthy volunteers were dosed with carbamazepine over 16 consecutive days." | ( Pharmacodynamics of carbamazepine-mediated induction of CYP3A4, CYP1A2, and Pgp as assessed by probe substrates midazolam, caffeine, and digoxin. Cederberg, J; Dahl, ML; Karlsson, MO; Magnusson, MO; Sandström, R, 2008) | 0.93 |
" Steady-state carbamazepine plasma concentrations determined by homogenous enzyme immunoassay technique, dosing history including cotherapy, schedule of blood sampling, and patients' demographic characteristics were collected retrospectively from patients' chart histories." | ( Population pharmacokinetic model of carbamazepine derived from routine therapeutic drug monitoring data. Grabnar, I; Miljković, B; Mrhar, A; Pokrajac, M; Velicković, R; Vucićević, K, 2007) | 0.98 |
" Compound 4 had good efficacy (52% and 41% reversal of allodynia at 2 and 4h post-dose, respectively) in the Chung rat spinal nerve ligation (SNL) model of neuropathic pain when dosed orally at 10mg/kg." | ( Imidazopyridines: a novel class of hNav1.7 channel blockers. Abbadie, C; Dean, B; Duffy, JL; Felix, JP; Garcia, ML; Hoyt, SB; Jochnowitz, N; Kaczorowski, GJ; Karanam, BV; Li, X; London, C; Lyons, KA; Martin, WJ; McGowan, E; Parsons, WH; Priest, BT; Smith, MM; Tschirret-Guth, R; Warren, VA; Williams, BS, 2008) | 0.35 |
"Two spectrophotometric methods are proposed for the assay of oxcarbazepine (OXC) in bulk and dosage forms using Folin-Ciocalteu phenol reagent (FCP) and 3-methyl-2-benzothiazolinone hydrazine hydrochloride (MBTH) as reagents." | ( Use of Folin-Ciocalteu phenol reagent and 3-methyl-2-benzothiazolinone hydrazine hydrochloride in the determination of oxcarbazepine in pharmaceuticals. Gandhimathi, M; Ravi, TK, 2008) | 0.35 |
" Comparison of isotherms for the target compounds to those for other conventional micropollutants suggested that naproxen and carbamazepine could be effectively removed by applying the same dosage utilized to remove odorous compounds (geosmin and MIB) at very low concentrations." | ( Adsorption characteristics of selected pharmaceuticals and an endocrine disrupting compound-Naproxen, carbamazepine and nonylphenol-on activated carbon. Huck, PM; Peldszus, S; Yu, Z, 2008) | 0.77 |
"Non-depressed outpatients with DSM-IV PG received flexibly dosed extended release carbamazepine in a prospective 10-week open-label trial following a two-week observation period." | ( Extended release carbamazepine in the treatment of pathological gambling: an open-label study. Allen, J; Black, DW; Shaw, MC, 2008) | 0.91 |
" The isobolographic analysis for parallel and nonparallel dose-response effects was used in the mouse maximal electroshock seizure (MES) model for evaluation of pharmacodynamic interaction." | ( Isobolographic characterization of interactions of retigabine with carbamazepine, lamotrigine, and valproate in the mouse maximal electroshock-induced seizure model. Czuczwar, SJ; Luszczki, JJ; Raszewski, G; Wu, JZ, 2009) | 0.59 |
"Drugs were tested in a repeated dosing paradigm (four daily injections)." | ( Experimental studies of potential analgesics for the treatment of chemotherapy-evoked painful peripheral neuropathies. Bennett, GJ; Naso, L; Xiao, W, ) | 0.13 |
"The objective of the study was to examine the negative impact of valproates on haemostasis and peripheral blood count in children and to analyse whether these disturbances were dependent on the dosage of valproates and drug level in blood." | ( [Impact of valproates on haemostasis and blood cell count in children]. Igrutinović, Z; Marković, S; Obradović, S; Vuletić, B, ) | 0.13 |
" These disturbances are in correlation with the dosage and the level of the medicine in blood." | ( [Impact of valproates on haemostasis and blood cell count in children]. Igrutinović, Z; Marković, S; Obradović, S; Vuletić, B, ) | 0.13 |
" Drug dosage and blood drug level are correlated with their negative impact on haemostasis parameters." | ( [Impact of valproates on haemostasis and blood cell count in children]. Igrutinović, Z; Marković, S; Obradović, S; Vuletić, B, ) | 0.13 |
" The detoxification program followed an outlined dosage scheme with oxcarbazepine increase and benzodiazepine tapering." | ( Oxcarbazepine in rapid benzodiazepine detoxification. Croissant, B; Diehl, A; Grosshans, M; Mann, K, 2008) | 0.35 |
"Oxcarbazepine is used in lower doses than recommended and the dosing is not adjusted for weight." | ( [Utilization of carbamazepine and oxcarbazepine in pediatric patients with partial epilepsy in Spain. An observational study]. Carreño, M; Rufo Campos, M, ) | 0.48 |
" Subsequent dosage adjustments were allowed while maintaining the blind." | ( The cognitive and psychomotor effects of remacemide and carbamazepine in newly diagnosed epilepsy. Dean, AD; Edgar, C; Wesnes, KA; Wroe, SJ, 2009) | 0.6 |
" His skin signs appeared 1 day after the last dosage increment." | ( Toxic epidermal necrolysis in a child after carbamazepine dosage increment. Akman, M; Bicer, S; Hatipoglu, S; Sevketoglu, E, 2009) | 0.61 |
" A significant decrease of ratio plasma concentration of 10-monohydroxy derivate (MHD) of oxcarbazepine to dosage was found by 26." | ( Seizure deterioration in women treated with oxcarbazepine during pregnancy. Hansen-Schwartz, J; Petrenaite, V; Sabers, A, 2009) | 0.35 |
" In some cases, this may affect the individual dosage adjustment and subsequent treatment." | ( A high-performance liquid chromatography method for the determination of carbamazepine and carbamazepine-10,11-epoxide and its comparison with chemiluminescent immunoassay. Leite, CE; Lunardelli, A; Petersen, GO; Thiesen, FV, 2009) | 0.58 |
"In this 12 week, randomized, double-blind pilot study, 60 patients diagnosed with acute mania (DSM-IV) and a baseline Young Mania Rating Scale (YMRS) score of 20 or more received flexibly dosed oxcarbazepine (1,000-2,400 mg/day) or divalproex (750-2,000 mg/day)." | ( Comparative efficacy and safety of oxcarbazepine versus divalproex sodium in the treatment of acute mania: a pilot study. Chopra, D; Gupta, NK; Kakkar, AK; Kataria, D; Rehan, HS; Unni, KE, 2009) | 0.35 |
" These findings showed that with a much lower dosage of the drugs, which is suggested in texts can lead to an appropriate blood level of CBZ and VPA for controlling the epileptic seizures." | ( An experimental design for finding of minimum dosage of carbamazepine and valproate in preventing of seizure attacks. Nobahar, M; Samaei, A; Vafaei, AA, 2009) | 0.6 |
" On the other hand, we found a gene dosage effect for mouse Sp4 gene in the modulation of sensorimotor gating, a putative endophenotype for both schizophrenia and bipolar disorder." | ( Transcription factor SP4 is a susceptibility gene for bipolar disorder. Geyer, MA; Greenwood, TA; Guo, S; He, L; Kelsoe, JR; Tang, W; Zhou, X, 2009) | 0.35 |
" Fifty-one patients received carbamazepine as a monotherapy in dosage 300-1200 mg/day, 21 patients were treated with oxcarbazepine in dosage 600-1500 mg daily." | ( [Comparison of efficacy of trileptal (oxcarbazepine) and carbamazepine in the treatment of temporal epilepsy]. Basamygin, AV; Kalinin, VV; Polianskiĭ, DA; Sokolova, LV; Zemlianaia, AA; Zheleznova, EV, 2008) | 0.88 |
" A vaginal dosage form of carbamazepine is not commercially available." | ( Design and in vitro evaluation of a novel vaginal drug delivery system based on gelucire. Geeta, MP; Madhabhai, MP, 2009) | 0.65 |
" They were divided in two groups: Group A--21 person who prophylactically took a daily dosage of 400 mg Carbamezepin and during acute pain attacks Naproksen; and group B--19 persons who prophylactically took daily dosage of 400 mg Carbamezepin." | ( Analysis of the electroencephalogram and pain characteristic in patients before and after carbamazepine treatment. Alicajic, F; Babic, N; Fajkic, A; Huseinagic, S; Music, M; Sivic, S; Toromanovic, S, 2008) | 0.57 |
" We then administered codeine, which alleviated the pain; an increase in the dosage led to complete pain remission." | ( [Opioid effectiveness for neuropathic pain in a patient with glossopharyngeal neuralgia]. Hirano, T; Kouzaki, Y; Otsuka, T; Takita, T; Tawara, S; Uchino, M, 2009) | 0.35 |
" No single demographic or genetic variable was of sufficient strength to independently influence carbamazepine dosing requirements." | ( Genetic variants in microsomal epoxide hydrolase influence carbamazepine dosing. Brodie, MJ; Butler, E; Hitiris, N; Makmor-Bakry, M; Sills, GJ; Wilson, EA, ) | 0.59 |
" A large-scale prospective investigation of genetic influences on drug dosing strategies in epilepsy, with specific focus on whole gene variability for those proteins involved in the pharmacokinetics and pharmacodynamics of antiepileptic agents, is warranted." | ( Genetic variants in microsomal epoxide hydrolase influence carbamazepine dosing. Brodie, MJ; Butler, E; Hitiris, N; Makmor-Bakry, M; Sills, GJ; Wilson, EA, ) | 0.37 |
" Since carbamazepine was discontinued and had been prescribed for bipolar disorder, his olanzapine dosage was increased, and trazodone was added at bedtime for insomnia." | ( Carbamazepine-induced hyperammonemia. Adams, EN; Lizer, MH; Marks, A, 2009) | 2.25 |
" Pharmacokinetic parameters, area under the concentration-time curve during a dosage interval at steady state (AUC(tau,ss)), and maximum steady-state plasma drug concentration during a dosage interval (C(max,ss)) of lacosamide, carbamazepine, and carbamazepine-10,11-epoxide were measured and compared for each drug alone and together." | ( No pharmacokinetic interaction between lacosamide and carbamazepine in healthy volunteers. Cawello, W; Eggert-Formella, A; Nickel, B, 2010) | 0.79 |
" However, no significant correlation was found between the extents of pain by visual analog score or between the daily dosage of carbamazepine and the NVC volume measured by MR cisternography." | ( Relationship between the curative effects of carbamazepine administration and the neurovascular compression volume of the trigeminal nerve measured using magnetic resonance cisternography. Imamura, Y; Kito, S; Matsumoto-Takeda, S; Morimoto, Y; Nakanishi, O; Oda, M; Sakamoto, E; Shiiba, S; Tanaka, T; Wakasugi-Sato, N, ) | 0.6 |
" In the treatment phase, carbamazepine was dosed 100 mg three times daily (for a total daily dose of 300 mg) for 7 days, and on Day 7, a single 60-mg dose of fexofenadine was coadministered with a 100-mg dose of carbamazepine." | ( Effects of the P-glycoprotein inducer carbamazepine on fexofenadine pharmacokinetics. Akamine, Y; Kaneko, S; Uno, T; Yamada, S; Yasui-Furukori, N, 2009) | 0.93 |
" Analysis of the log dose-response curves for oxcarbazepine or gabapentin in a presence of amitriptyline and oxcarbazepine or gabapentin applied alone, revealed a synergism in oxcarbazepine-amitriptyline and additivity in gabapentin-amitriptyline combination." | ( Analysis of the antinociceptive interactions in two-drug combinations of gabapentin, oxcarbazepine and amitriptyline in streptozotocin-induced diabetic mice. Bosković, B; Micov, AM; Prostran, MS; Stepanović-Petrović, RM; Tomić, MA; Ugresić, ND; Vucković, SM, 2010) | 0.36 |
" TDM requests, interpretation and dosage adjustment recommendations were mainly responsible by residents." | ( Effect of pharmacist participation in the health care team on therapeutic drug monitoring utilization for antiepileptic drugs. Faroongsarng, D; Kaewpibal, P; Ratanajamit, C; Setthawacharavanich, S, 2009) | 0.35 |
"The aim of this study was to characterize the anticonvulsant effects of 1-methyl-1,2,3,4-tetrahydroisoquinoline (MeTHIQ--an endogenous parkinsonism-preventing substance) in combination with four second-generation antiepileptic drugs (AEDs: lamotrigine [LTG], oxcarbazepine [OXC], pregabalin [PGB], and topiramate [TPM]) in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for parallel and non-parallel dose-response relationship curves (DRRCs)." | ( Interactions of 1-methyl-1,2,3,4-tetrahydroisoquinoline with lamotrigine, oxcarbazepine, pregabalin, and topiramate in the mouse maximal electroshock-induced seizure model: a type I isobolographic analysis. Antkiewicz-Michaluk, L; Czuczwar, SJ; Luszczki, JJ; Raszewski, G, 2010) | 0.36 |
" On the other hand, simulations indicated that at least 2 weeks of dosing would be needed to detect the potent inhibition of CYP3A (maximal ~40% decrease in 4βHC plasma levels)." | ( Does the long plasma half-life of 4beta-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric? Rodrigues, AD; Yang, Z, 2010) | 0.36 |
"To characterize the anticonvulsant effects of pregabalin (PGB - a third-generation antiepileptic drug) in combination with carbamazepine (CBZ - a classical antiepileptic drug) in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for non-parallel dose-response relationship curves (DRRCs)." | ( Interaction of pregabalin with carbamazepine in the mouse maximal electroshock-induced seizure model: a type I isobolographic analysis for non-parallel dose-response relationship curves. Luszczki, JJ, 2010) | 0.85 |
"We administered oxcarbazepine at a dosage of 1200 mg/d, and this subject improved both in hair pulling and in eating behaviors with no relapse after 9 months." | ( Oxcarbazepine for the treatment of trichotillomania. Gastaldi, F; Leombruni, P, ) | 0.13 |
" Additional information about gender, age, co-medication and dosage was obtained." | ( Individual clearance and therapeutic drug monitoring of quetiapine in clinical practice. Haen, E; Hajak, G; Hausner, H; Köstlbacher, A; Wittmann, M, 2010) | 0.36 |
" In three trials, carbamazepine failed to reduce alcohol withdrawal symptoms possibly as a result of delayed administration, inadequate dosage or inadequate sample size." | ( The role of carbamazepine and oxcarbazepine in alcohol withdrawal syndrome. Barrons, R; Roberts, N, 2010) | 1.07 |
" Results of our study show the positive correlation between dosage and serum concentration of CBZ." | ( Carbamazepine and lamotrigine plasma concentrations in epileptic patients during optimising therapy. Bauer, S; Islami, H; Krasniqi, S; Neziri, B, 2010) | 1.8 |
", lamotrigine [LTG], oxcarbazepine [OXC] and topiramate [TPM]) in the mouse maximal electroshock (MES)-induced seizure model by using the type I isobolographic analysis for non-parallel dose-response relationship curves (DRRCs)." | ( Additive interactions of pregabalin with lamotrigine, oxcarbazepine and topiramate in the mouse maximal electroshock-induced seizure model: a type I isobolographic analysis for non-parallel dose-response relationship curves. Czuczwar, SJ; Filip, D; Luszczki, JJ, 2010) | 0.36 |
" Dosing and plasma levels of levetiracetam and concomitant antiepileptic drugs were reviewed retrospectively." | ( Age and comedications influence levetiracetam pharmacokinetics in children. Dahlin, MG; Ohman, I; Wide, K, 2010) | 0.36 |
" The results of the IV dosing pharmacokinetics investigation were consistent with N-Gly-CBZ acting as a prodrug with rapid and complete conversion to CBZ in vivo." | ( In vitro and in vivo evaluation of a novel water-soluble N-glycyl prodrug (N-GLY-CBZ) of carbamazepine. Hemenway, JN; Stella, VJ, 2010) | 0.58 |
" The degree of decline in serum sodium concentration was significantly negatively correlated with the dosage of OXC." | ( Risk factors of oxcarbazepine-induced hyponatremia in patients with epilepsy. Chang, WN; Chuang, YC; Lai, SL; Lin, CH; Lu, CH; Tsai, MH; Tsai, NW; Tseng, YL; Wang, FJ, ) | 0.13 |
" Improvement was noted after the drug dosage was reduced." | ( Respiratory alkalosis and metabolic acidosis in a child treated with sulthiame. Garty, BZ; Hoffer, V; Scheuerman, O; Tirosh, I; Weissbach, A, 2010) | 0.36 |
"The derived models describe well VPA clearance in terms of characteristics of Serbian pediatric and adult epileptic patients, offering a basis for rational individualization of VPA dosage regimens." | ( Factors influencing valproate pharmacokinetics in children and adults. Jankovic, S; Jankovic, SM; Milovanovic, JR, 2010) | 0.36 |
" Therefore, the patient's daily dosage of oxcarbazepine and phenytoin were reduced." | ( Phenytoin toxicity secondary to an oxcarbazepine-phenytoin 2C19 interaction. Kane, AJ; Soskin, DP; Stern, TA, ) | 0.13 |
"Many investigators agree that appropriate rational utilization of therapeutic drug monitoring (TDM) with Bayesian feedback dosage adjustment facilitates epilepsy treatment with carbamazepine (CBZ) and/or valproate (VPA) by increasing the seizure control and safety, as well as by reducing treatment costs." | ( Predictability of individualized dosage regimens of carbamazepine and valproate mono- and combination therapy. Andreeva, OV; Bondareva, IB; Bondareva, KI; Jelliffe, RW, 2011) | 0.81 |
"Our validation results suggest good predictive performance of the population models developed earlier, and quite acceptable predictions of future AED serum levels for individualized dosage regimens of CBZ and VPA therapy in real clinical settings." | ( Predictability of individualized dosage regimens of carbamazepine and valproate mono- and combination therapy. Andreeva, OV; Bondareva, IB; Bondareva, KI; Jelliffe, RW, 2011) | 0.62 |
"0 g/L) PAC dosage could be attributed to the fact that carbamazepine is relatively more hydrophobic than sulfamethoxazole, which subsequently resulted in its higher adsorption affinity toward PAC." | ( Simultaneous activated carbon adsorption within a membrane bioreactor for an enhanced micropollutant removal. Hai, FI; Li, X; Nghiem, LD, 2011) | 0.62 |
" In case of breakthrough seizures or increased seizure frequency, dosage adjustment of both drugs may be required." | ( Drug monitoring of lamotrigine and oxcarbazepine combination during pregnancy. de Haan, GJ; Edelbroek, P; Lindhout, D; Sander, JW; Wegner, I, 2010) | 0.36 |
" In the process of introduction and increase in the dosage of VPA, an aggravation of epileptic discharges, especially a dramatic increase in diffuse spike-waves during sleep, was observed." | ( [Aggravation of epilepsy by valproate sodium in a child with cryptogenic localization-related epilepsy]. Ohtsuka, Y; Watanabe, K; Watanabe, Y, 2011) | 0.37 |
" C3H/HeOuJ mice were dosed by oral gavage with diclofenac (DF), APAP, AMAP, OFLX, MET, or CMZ." | ( Oral exposure to drugs with immune-adjuvant potential induces hypersensitivity responses to the reporter antigen TNP-OVA. Bleumink, R; Boon, L; Fiechter, D; Hassing, I; Kwast, LM; Ludwig, IS; Pieters, RH, 2011) | 0.37 |
" To optimize the dose regimens of these inducers for use in DDI studies, their effect at various doses and dosing durations on the area under the curve (AUC) of multiple probe substrates was simulated using a population-based simulator." | ( Simulation of clinical drug-drug interactions from hepatocyte CYP3A4 induction data and its potential utility in trial designs. Hayashi, M; Shou, M; Skiles, GL; Xu, Y; Zhou, Y, 2011) | 0.37 |
" Plasma TRP/LNAAS ratios increased 2- to 3-fold after dosing with ALAC (250 mg/kg/day) for 7 and 14 days, respectively." | ( Preclinical activity profile of α-lactoalbumin, a whey protein rich in tryptophan, in rodent models of seizures and epilepsy. Citraro, R; De Fazio, S; De Sarro, G; Mainardi, P; Perucca, E; Raggio, R; Russo, E; Scicchitano, F, 2011) | 0.37 |
" Stabilization of CBZ form I in in vitro and in vivo conditions using pharmaceutical polymers in dosage form may bring better clinical outcomes than present-day therapies." | ( Influence of Simulated Gastrointestinal Fluids on Polymorphic Behavior of Anhydrous Carbamazepine Form III and Biopharmaceutical Relevance. Bhise, SB; Rajkumar, M, ) | 0.36 |
" The disease occurred after one to four years of drug therapy, at dosage of 100 mg/day." | ( Dupuytren's contracture as result of prolonged administration of phenobarbital. Cordova, A; Moschella, F; Tripoli, M, 2011) | 0.37 |
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts." | ( FDA-approved drug labeling for the study of drug-induced liver injury. Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011) | 0.37 |
"0μg/mL, and areas under the plasma concentration-time curve over the dosing interval (AUC(0-24)) were 132." | ( Pharmacokinetics of eslicarbazepine acetate at steady-state in adults with partial-onset seizures. Almeida, L; Elger, C; Falcão, A; Halász, P; Perucca, E; Soares-da-Silva, P, 2011) | 0.37 |
"The derived models describe well CBZ clearance in terms of Serbian pediatric and adult epileptic patient characteristics, offering a basis for rational individualization of CBZ dosage regimens." | ( Factors influencing carbamazepine pharmacokinetics in children and adults: population pharmacokinetic analysis. Jankovic, SM; Milovanovic, JR, 2011) | 0.69 |
" Mean dosage of oxcarbazepine was 1,230 mg/day (min 600, max 2,100 mg/day)." | ( Oxcarbazepine monotherapy in patients with brain tumor-related epilepsy: open-label pilot study for assessing the efficacy, tolerability and impact on quality of life. Dinapoli, L; Fabi, A; Maschio, M; Muti, P; Pace, A; Sperati, F; Vidiri, A, 2012) | 0.38 |
"Individualization of carbamazepine (CBZ) dosage regimen in patients with epilepsy based on based on therapeutic drug monitoring (TDM) followed by estimation of pharmacokinetic (PK) parameters can help in better control of epilepsy." | ( Population pharmacokinetics of steady-state carbamazepine in Egyptian epilepsy patients. Bewernitz, M; Derendorf, H; El Desoky, ES; Hamdi, MM; Sabarinath, SN, 2012) | 0.96 |
" Another PK study to better define the effect of different covariates would improve on the model for dosage individualization." | ( Population pharmacokinetics of steady-state carbamazepine in Egyptian epilepsy patients. Bewernitz, M; Derendorf, H; El Desoky, ES; Hamdi, MM; Sabarinath, SN, 2012) | 0.64 |
" Forty adult patients were studied and oxcarbazepine was administered orally at a single loading dosage of 30 mg/kg." | ( Efficacy, tolerability, and pharmacokinetics of oxcarbazepine oral loading in patients with epilepsy. Cho, JY; Chu, K; Gu, N; Jang, IJ; Kim, DW; Kim, HS; Lee, SK; Oh, J; Yoon, SH; Yu, KS, 2012) | 0.38 |
" However, in order to make further recommendations regarding the choice and dosing regimens of antiepileptic drugs in elderly patients, more extensive clinical research in this specific population is necessary." | ( Choice of antiepileptic drugs for the elderly: possible drug interactions and adverse effects. Dostic, M; Jankovic, SM, 2012) | 0.38 |
" The dosage was adjusted according to the level of pain control and side-effects." | ( Use of single- and multi-drug regimens in the management of classic (idiopathic) trigeminal neuralgia: an 11-year experience at a single Sri Lankan institution. Ariyawardana, A; Pallegama, R; Ranasinghe, A; Sitheeque, M, 2012) | 0.38 |
" Therefore, electrospray technology has the potential to produce pharmaceutical dosage forms with enhanced bioavailability and can readily be integrated in a continuous pharmaceutical manufacturing process." | ( Production and characterization of carbamazepine nanocrystals by electrospraying for continuous pharmaceutical manufacturing. Myerson, AS; Rutledge, GC; Trout, BL; Wang, M, 2012) | 0.66 |
" Daily fluctuations in serum levels of carbamazepine and carbamazepine-10,11-epoxide did not appear to be related to the dosage schedule, but some patients tended to have lower fluctuations when the carbamazepine was given more frequently." | ( CSF concentrations and serum protein binding of carbamazepine and carbamazepine-10,11-epoxide in epileptic patients. Bakke, J; Gerna, M; Johannessen, SI; Morselli, PL; Strandjord, RE, 1976) | 0.78 |
" Sex and racial differences in clearance may contribute to variable dosing requirements and clinical response." | ( Steady-state carbamazepine pharmacokinetics following oral and stable-labeled intravenous administration in epilepsy patients: effects of race and sex. Birnbaum, AK; Brundage, RC; Cloyd, JC; Conway, JM; Gross, CR; Leppik, IE; Marino, SE; Mishra, U; Musib, LC; Pennell, PB; Ramsay, RE; Rarick, JO; White, JR, 2012) | 0.75 |
" LGI1 gene dosage was performed by real-time quantitative PCR (qPCR)." | ( LGI1 microdeletion in autosomal dominant lateral temporal epilepsy. Barozzi, C; Cubeddu, T; de Falco, A; de Falco, FA; Errichiello, L; Fanciulli, M; Michelucci, R; Nobile, C; Rampazzo, A; Rigon, L; Santulli, L; Striano, P; Striano, S; Tomasi, L; Uzzau, S, 2012) | 0.38 |
" The smaller peak-to-trough fluctuation of eslicarbazepine in CSF (a measure of sustained delivery to the brain) than in plasma supports once-daily dosing of ESL." | ( Steady-state plasma and cerebrospinal fluid pharmacokinetics and tolerability of eslicarbazepine acetate and oxcarbazepine in healthy volunteers. Almeida, L; Falcão, A; Nunes, T; Rocha, JF; Soares-da-Silva, P, 2013) | 0.39 |
" The primary study variable was to assess the maximum tolerated dosage with OXC-MR and OXC-IR." | ( [Slow release versus immediate release oxcarbazepine in difficult-to-treat focal epilepsy: a multicenter, randomized, open, controlled, parallel group phase III study]. Elger, CE; Hueber, R; Paulus, W; Schulze-Bonhage, A; Stefan, H; Steinhoff, BJ; Wangemann, M, 2012) | 0.38 |
" The initial dosage of 900 mg, 1,200 mg or 1,500 mg OXC was increased every 5 days by 300 mg up to a maximum daily dosage of 2,700 mg." | ( [Slow release versus immediate release oxcarbazepine in difficult-to-treat focal epilepsy: a multicenter, randomized, open, controlled, parallel group phase III study]. Elger, CE; Hueber, R; Paulus, W; Schulze-Bonhage, A; Stefan, H; Steinhoff, BJ; Wangemann, M, 2012) | 0.38 |
" The maximum mean daily OXC dosage at the end of the study period was 1,950 mg with OXC-MR and thus statistically significantly higher than in OXC-IR group (1,650 mg, p = 0." | ( [Slow release versus immediate release oxcarbazepine in difficult-to-treat focal epilepsy: a multicenter, randomized, open, controlled, parallel group phase III study]. Elger, CE; Hueber, R; Paulus, W; Schulze-Bonhage, A; Stefan, H; Steinhoff, BJ; Wangemann, M, 2012) | 0.38 |
" In spite of a higher mean daily dosage adverse events and especially CNS-related adverse events occurred less often than with OXC-IR." | ( [Slow release versus immediate release oxcarbazepine in difficult-to-treat focal epilepsy: a multicenter, randomized, open, controlled, parallel group phase III study]. Elger, CE; Hueber, R; Paulus, W; Schulze-Bonhage, A; Stefan, H; Steinhoff, BJ; Wangemann, M, 2012) | 0.38 |
"Here, we aim to evaluate Gelucire 44/14 as non-ionic surface-active excipient to produce immediate-release solid dosage forms for poorly water-soluble drugs." | ( Gelucire 44/14 based immediate release formulations for poorly water-soluble drugs. da Fonseca Antunes, AB; De Geest, BG; Remon, JP; Vervaet, C, 2013) | 0.39 |
" In addition, there appeared to be a dose-response relationship between stroke risk and PHT prescriptions." | ( Comparative stroke risk of antiepileptic drugs in patients with epilepsy. Hsieh, CY; Lai, EC; Lin, SJ; Yang, YH, 2013) | 0.39 |
"The objective of the present study was the development and the in vitro evaluation of extended release multiparticulate dosage forms with carbamazepine, starting from drug crystals of established granulometry as cores and using Eudragit NE aqueous dispersions as coating film polymer in a bottom spray fluid bed coating system." | ( Development and in vitro evaluation of multiparticulate sustained release carbamazepine formulation. Leucuţa, SE; Tomuţă, I, ) | 0.56 |
" Moreover, the impact of body weight, absorption rate and co-therapy with other antiepileptic drugs (phenytoin, phenobarbital and valproic acid) on the dosage recommendation was investigated in the event of poor compliance." | ( The effect of poor compliance on the pharmacokinetics of carbamazepine and its epoxide metabolite using Monte Carlo simulation. Ding, JJ; Jiao, Z; Wang, Y; Zhang, YJ, 2012) | 0.62 |
"The purpose of this research work was the realization of a bi-layered mucoadhesive dosage form intended for carbamazepine sublingual administration and planned in order to obtain a unidirectional drug release and diffusion only across buccal mucosa avoiding the liberation in the buccal environment." | ( Preformulation studies of mucoadhesive tablets for carbamazepine sublingual administration. Pagano, C; Perioli, L, 2013) | 0.85 |
" These technologies extend the dosing interval such that dosing frequency can be minimized, which may improve patient adherence." | ( Extended-release antiepileptic drugs: a comparison of pharmacokinetic parameters relative to original immediate-release formulations. Hovinga, CA; Leppik, IE, 2013) | 0.39 |
" Ecotoxicity was shown to increase in parallel with carbamazepine degradation indicating that the mixture of degradation products formed was more toxic than the parent compound, and all three ecotoxicity endpoints were still inhibited >60% relative to control populations upon dosing with 90+min UV-treated carbamazepine solution." | ( Ecotoxicity of carbamazepine and its UV photolysis transformation products. Andersen, HR; Donner, E; Heath, E; Kosjek, T; Kusk, KO; Ledin, A; Qualmann, S; Revitt, DM, 2013) | 0.99 |
" Mean PGB dosage was 279 mg/day." | ( Effect of pregabalin add-on treatment on seizure control, quality of life, and anxiety in patients with brain tumour-related epilepsy: a pilot study. Carapella, CM; Dinapoli, L; Fabi, A; Maschio, M; Pace, A; Pompili, A; Sperati, F; Vidiri, A, 2012) | 0.38 |
"Hot-melt extrusion (HME) is a dust- and solvent-free continuous process enabling the preparation of a variety of solid dosage forms containing solid dispersions of poorly soluble drugs into thermoplastic polymers." | ( Preparation of carbamazepine-Soluplus solid dispersions by hot-melt extrusion, and prediction of drug-polymer miscibility by thermodynamic model fitting. Djuric, Z; Djuris, J; Ibric, S; Kachrimanis, K; Nikolakakis, I, 2013) | 0.74 |
"The dissolution enhancement advantages inherent to amorphous solid dispersions systems are often not fully realized once they are formulated into a solid dosage form." | ( The use of inorganic salts to improve the dissolution characteristics of tablets containing Soluplus®-based solid dispersions. Hughey, JR; Keen, JM; Kolter, K; Langley, N; McGinity, JW; Miller, DA, 2013) | 0.39 |
" The stable-labeled intravenous dosing methodology enabled the estimation of the CBZ clearance (CL) and volumes of distribution." | ( Population pharmacokinetics of unbound and total drug concentrations following intravenously administered carbamazepine in elderly and younger adult patients with epilepsy. Ahmed, GF; Birnbaum, AK; Brundage, RC; Cloyd, JC; Leppik, IE; Marino, SE; Pennell, PB; Ramsay, RE, 2013) | 0.6 |
" We planned to include trials of oxcarbazepine compared with placebo or any other intervention, regardless of administration route, dosage or length of treatment." | ( Oxcarbazepine for neuropathic pain. Chen, N; He, L; Wu, F; Yang, M; Zhou, M; Zhu, C, 2013) | 0.39 |
" The mean area under the curve (AUC)ss,0-τ (in μmol h/L) following the last dose of an 8-day repeated dosing was 1156." | ( Pharmacokinetics and tolerability of eslicarbazepine acetate and oxcarbazepine at steady state in healthy volunteers. Almeida, L; Bialer, M; Elger, C; Falcão, A; Nunes, T; Soares-da-Silva, P; Vaz-da-Silva, M, 2013) | 0.39 |
"Oral loading of oxcarbazepine suspension followed by maintenance dosing is well tolerated and effective in steadily achieving the therapeutic level of MHD in selected patients with epilepsy." | ( Usefulness of oral loading of oxcarbazepine suspension in selected patients with epilepsy. Cho, JY; Chu, K; Gu, N; Jang, IJ; Kim, DW; Lee, H; Lee, SK; Na, HJ; Yoon, SH; Yu, KS, 2013) | 0.39 |
"Two reviewers independently extracted the following data: study design, eligibility criteria, diagnostic criteria, patient demographics, genotype distribution, HLA-B genotyping technique, selection of cases and controls, dosage of carbamazepine and duration of use, and results of Hardy-Weinberg equilibrium in the control group." | ( Relationship between the HLA-B*1502 allele and carbamazepine-induced Stevens-Johnson syndrome and toxic epidermal necrolysis: a systematic review and meta-analysis. Chaiyakunapruk, N; Lohitnavy, M; Somkrua, R; Tangamornsuksan, W; Tassaneeyakul, W, 2013) | 0.83 |
" Chlorination was relatively not effective for the removal of micropollutants due to the lower chlorine dosage (2 mg L(-1)), lower contact time (1h), and already lower levels of micropollutants at the chlorination stage at WTP." | ( Occurrence and removal of selected micropollutants in a water treatment plant. Jo, BI; Nam, SW; Yoon, Y; Zoh, KD, 2014) | 0.4 |
"5%) obtained moderate relief (good), and was under control with carbamazepine at a dosage of 600 mg/d." | ( Use of electrophysiological monitoring in selective rhizotomy treating glossopharyngeal neuralgia. Chai, Y; Chen, M; Zhang, W, 2014) | 0.64 |
" The numerical density of Leydig cells and hormone dosage were obtained." | ( Carbamazepine-exposure during gestation and lactation affects pubertal onset and spermatic parameters in male pubertal offspring. Andretta, RR; de Oliva, SU; Miraglia, SM; Okada, FK; Paccola, CC; Stumpp, T, 2014) | 1.85 |
" The mean dosage of AED for valproate was 498 mg/day and carbamazepine was 555 mg/day." | ( Malformation in index pregnancy in women with epilepsy is not followed by recurrence in subsequent pregnancy. Begum, S; Sarma, SP; Thomas, SV, 2013) | 0.64 |
" The dosage regimen should be adjusted accordingly to gain a better clinical outcome." | ( Effect of CYP3A5 genotypes on the pharmacokinetics of carbamazepine when used as monotherapy or co-administered with phenytoin, phenobarbital or valproic acid in Thai patients. Panomvana, D; Towanabut, S; Traiyawong, T, 2013) | 0.64 |
"The LTG population pharmacokinetic model developed in this study may be a reliable method for individualising the LTG dosing regimen in paediatric and young adult patients on combination therapy during therapeutic drug monitoring." | ( Pharmacokinetics of lamotrigine in paediatric and young adult epileptic patients--nonlinear mixed effects modelling approach. Brzaković, B; Kovačević, SV; Martinović, Ž; Miljković, B; Pokrajac, M; Prostran, M; Vučićević, K, 2014) | 0.4 |
" We examined the HLA-A/HLA-B genotypes, gene dosage, and drug dosage effects." | ( Genotype-phenotype association between HLA and carbamazepine-induced hypersensitivity reactions: strength and clinical correlations. Chang, PY; Chang, WC; Chang, YG; Chen, DP; Chen, MJ; Chung, WH; Ho, HC; Hsiao, YH; Hsih, MS; Hui, RC; Hung, SI; Lin, JY; Wu, T; Wu, TL; Yang, CH, 2014) | 0.66 |
" No gene dosage or CBZ dosage effects was observed." | ( Genotype-phenotype association between HLA and carbamazepine-induced hypersensitivity reactions: strength and clinical correlations. Chang, PY; Chang, WC; Chang, YG; Chen, DP; Chen, MJ; Chung, WH; Ho, HC; Hsiao, YH; Hsih, MS; Hui, RC; Hung, SI; Lin, JY; Wu, T; Wu, TL; Yang, CH, 2014) | 0.66 |
" At least, three possible interpretations of the measured carbamazepine concentrations were addressed: (1) decrease in administration in the more recent period; (2) increase of body weight due to growing, so the same dosage will result in lower concentrations in hair; and (3) sweat contamination from the mother at the time the girl is with her in bed, the older hair being in contact longer with the bedding." | ( Interpretation of hair findings in children: about a case involving carbamazepine. Kintz, P, 2014) | 0.88 |
" Simulations of carbamazepine dosing regimen based on the pharmacokinetic parameters of this patient were performed to allow individualization of drug therapy." | ( Slow carbamazepine clearance in a nonadherent Malay woman with epilepsy and thyrotoxicosis. Hui-Ping Khor, A; Lim, KS; Lo, YL; Ng, CC; Yeap, LL, 2014) | 1.26 |
" Once-daily dosing was not associated with any new safety signals." | ( Efficacy and safety of extended-release oxcarbazepine (Oxtellar XR™) as adjunctive therapy in patients with refractory partial-onset seizures: a randomized controlled trial. Baroldi, P; Brittain, ST; French, JA; Johnson, JK, 2014) | 0.4 |
" The history of CBZ therapy before MVD, pre-operative dosage of CBZ, and the D-value of CBZ blood concentrations demonstrated statistic differences between the patients with CAWR and those without CAWR." | ( Withdrawal reaction of carbamazepine after neurovascular decompression for trigeminal neuralgia: a preliminary study. Chai, Y; Chen, MJ; Guo, ZL; Li, YW; Zhang, WH; Zhang, WJ, 2014) | 0.71 |
"It is strongly suggested that CAWR is dependent on the pre-operative dosage and the changing rate of pre- and post-operative CBZ blood concentrations." | ( Withdrawal reaction of carbamazepine after neurovascular decompression for trigeminal neuralgia: a preliminary study. Chai, Y; Chen, MJ; Guo, ZL; Li, YW; Zhang, WH; Zhang, WJ, 2014) | 0.71 |
" This method was successfully applied in pharmacokinetic study of acetylcorynoline after intravenous administration of single dosage 3 mg/kg in rats." | ( Gradient elution liquid chromatography mass spectrometry determination of acetylcorynoline in rat plasma and its application to a pharmacokinetic study. Cai, J; Lin, C; Ma, J; Wang, X; Wen, C, 2014) | 0.4 |
" A properly modulation of the drug dosage allowed pain relief to be achieved." | ( Typical trigeminal neuralgia by an atypical compression: case report and review of the literature. Cacciola, F; Caruso, G; Giambartino, F; Grasso, G; Passalacqua, M; Tomasello, F, 2014) | 0.4 |
" Testing of biological activity revealed limited potential for resistance to these agents, low toxicity, and highly effective in vivo activity, even with low dosing regimens." | ( Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines. Burda, WN; Fleeman, R; Manetsch, R; Shaw, LN; Van Horn, KS, 2014) | 0.4 |
" The CBZ removal efficiency was enhanced with the increase of RSB dosage without pH control." | ( Biosorption of clofibric acid and carbamazepine in aqueous solution by agricultural waste rice straw. Chen, X; Dai, C; Liu, Z; Zhang, J; Zhang, Y; Zhou, X, 2013) | 0.67 |
" Simulations demonstrated that twice-daily dosing offered little advantage in further flattening the concentration-time profile of perampanel in the adherent patient." | ( The practical impact of altered dosing on perampanel plasma concentrations: pharmacokinetic modeling from clinical studies. Fain, R; Ferry, J; Gidal, BE; Hussein, Z; Laurenza, A; Majid, O; Yang, H; Zhu, J, 2014) | 0.4 |
" The results from the study can help inform dosing regimens in pediatrics using the quetiapine XR formulation." | ( Development of physiologically based pharmacokinetic model to evaluate the relative systemic exposure to quetiapine after administration of IR and XR formulations to adults, children and adolescents. Bui, KH; Johnson, TN; Zhou, D, 2014) | 0.4 |
" Comparisons were made between the groups based on the age of onset, seizure frequency before treatment, time interval between seizure onset and treatment start, time interval between the two EEGs, oxcarbazepine dosage at the follow-up electroencephalography, occurrence of daytime seizures, and seizure control." | ( Changes in current-source density of interictal spikes in benign epilepsy of childhood with centrotemporal spikes following treatment with oxcarbazepine. Jung, S; Kim, YS; Kwon, OY; Yeom, JS, 2014) | 0.4 |
" This model may be very useful for establishing individual dosage guidelines of OXC in Chinese children with epilepsy." | ( Population pharmacokinetics of oxcarbazepine active metabolite in Chinese children with epilepsy. Liu, ZS; Peng, J; Wang, Y; Xu, H; Zhang, HN, 2014) | 0.4 |
" The reproducibility of oral dosing was confirmed by the fact that the results obtained in both the experiments had negligible errors." | ( Oral dosing in adult zebrafish: proof-of-concept using pharmacokinetics and pharmacological evaluation of carbamazepine. Banote, RK; Chatti, K; Chaudhari, GH; Kirla, KT; Kulkarni, P; Oruganti, S; Rao, P; Sripuram, V; Sultana, R, 2014) | 0.62 |
"6 months, 27% of responders to CBZ incurred in undesired effects to a level that caused interruption of treatment or a dosage reduction to an unsatisfactory level." | ( Natural history and outcome of 200 outpatients with classical trigeminal neuralgia treated with carbamazepine or oxcarbazepine in a tertiary centre for neuropathic pain. Cruccu, G; Di Stefano, G; La Cesa, S; Truini, A, 2014) | 0.62 |
"Nineteen patients completed the desensitization protocol to a target dosage over 2-5 months." | ( Human leukocyte antigen genotypes and trial of desensitization in patients with oxcarbazepine-induced skin rash: a pilot study. Kang, ES; Lee, B; Lee, J; Lee, M; Yu, HJ, 2014) | 0.4 |
" Patients continued their randomized treatment, with dosing adjusted according to tolerability/response (zonisamide 200-500 mg/day; carbamazepine 400-1,200 mg/day)." | ( Long-term safety and efficacy of zonisamide versus carbamazepine monotherapy for treatment of partial seizures in adults with newly diagnosed epilepsy: results of a phase III, randomized, double-blind study. Baulac, M; Giorgi, L; Patten, A, 2014) | 0.86 |
" Microcosms were assembled in a factorial design containing algae and mayfly nymphs native to central Indiana and dosed with environmentally relevant concentrations of carbamazepine." | ( The effects of the pharmaceutical carbamazepine on life history characteristics of flat-headed mayflies (Heptageniidae) and aquatic resource interactions. Bernot, MJ; Bernot, RJ; Jarvis, AL, 2014) | 0.88 |
"These results suggest that up to a 50% decrease of vilazodone dosage should be considered when it is given in combination with strong CYP3A4 inhibitors; conversely, increasing the vilazodone dosage up to a maximum of 80 mg/d should be considered when it is given in combination with strong CYP3A4 inducers." | ( Influence of CYP3A4 induction/inhibition on the pharmacokinetics of vilazodone in healthy subjects. Boinpally, R; Gad, N; Gupta, S; Periclou, A, 2014) | 0.4 |
"The present study aimed to establish population pharmacokinetic model for phenobarbital (PB), examining and quantifying the magnitude of PB interactions with other antiepileptic drugs concomitantly used and to demonstrate its use for individualization of PB dosing regimen in adult epileptic patients." | ( Nonlinear mixed effects modelling approach in investigating phenobarbital pharmacokinetic interactions in epileptic patients. Golubović, B; Jovanović, M; Kovačević, SV; Martinović, Ž; Miljković, B; Prostran, M; Vučićević, K, 2015) | 0.42 |
"Developed population PB model may be used in estimating individual CL/F for adult epileptic patients and could be applied for individualizing dosing regimen taking into account dose-dependent effect of concomitantly given VPA." | ( Nonlinear mixed effects modelling approach in investigating phenobarbital pharmacokinetic interactions in epileptic patients. Golubović, B; Jovanović, M; Kovačević, SV; Martinović, Ž; Miljković, B; Prostran, M; Vučićević, K, 2015) | 0.42 |
" Furthermore, the proposed population pharmacokinetic model of VPA can be used to design rational dosage regimens to achieve desirable serum concentrations." | ( A population pharmacokinetic model of valproic acid in pediatric patients with epilepsy: a non-linear pharmacokinetic model based on protein-binding saturation. Ding, J; Jiao, Z; Li, X; Lin, W; Miao, L; Wang, C; Wang, Y; Zhao, L; Zhao, Z, 2015) | 0.42 |
" Subjects assigned to group 1 received a dose of carbamazepine (200 mg) alone and a dose after pretreatment with daily dosing of armodafinil (titrated to 250 mg/d)." | ( Evaluation of the potential for pharmacokinetic drug-drug interaction between armodafinil and carbamazepine in healthy adults. Bond, M; Darwish, M; Hellriegel, ET; Robertson, P; Yang, R, 2015) | 0.89 |
"In personalized medicine and patient-centered medical treatment individual dosing of medicines is crucial." | ( Development of sustained and dual drug release co-extrusion formulations for individual dosing. Breitkreutz, J; Laukamp, EJ; Thommes, M; Voorspoels, J; Vynckier, AK, 2015) | 0.42 |
" The blood samples were collected after CBZ dosing at predetermined time intervals and analyzed by LC-MS/MS." | ( Effect of resveratrol on the pharmacokinetics of carbamazepine in healthy human volunteers. Bedada, SK; Nearati, P, 2015) | 0.67 |
" To improve on drug compliance attending physicians need to prescribe more of the relatively cheaper AED like the phenobarbitone and to optimize drug dosage before switching to another." | ( A 3 year audit of adult epilepsy care in a Nigerian tertiary hospital (2011-2013). Ademiluyi, BA; Alaofin, WA; Bello, HA; Busari, K; Desalu, OO; Sanya, EO; Wahab, KW, ) | 0.13 |
" The final PPK model was demonstrated to be suitable and effective and it can be used to evaluate the pharmacokinetic parameters of MHD in Chinese patients with epilepsy and to choose an optimal dosage regimen of oxcarbazepine on the basis of these parameters." | ( Population pharmacokinetic modeling of oxcarbazepine active metabolite in Chinese patients with epilepsy. Hao, G; Lv, C; Xu, W; Yu, Y; Zhang, Q, 2016) | 0.43 |
"A sensitive and simple spectrofluorimetric method has been developed and validated for the determination of the anti-epileptic drug carbamazepine (CBZ) in its dosage forms." | ( Validated spectrofluorimetric method for the determination of carbamazepine in pharmaceutical dosage forms after reaction with 4-chloro-7--nitrobenzo-2-oxa-1,3-diazole (NBD-Cl). Askar, H; El-Enany, N; Walash, MI, 2015) | 0.86 |
"Patients receiving a stable oral dosage of carbamazepine were switched to an intravenous (IV) carbamazepine formulation solubilized in a cyclodextrin matrix (at a 70% dosage conversion) for either a 15- or a 30-min infusion every 6 h for up to 7 days and then switched back." | ( Intravenous carbamazepine as short-term replacement therapy for oral carbamazepine in adults with epilepsy: Pooled tolerability results from two open-label trials. Bekersky, I; Biton, V; Cloyd, J; Dheerendra, S; Halford, JJ; Kalu, U; Klein, P; Lee, D; Peng, G; Tolbert, D, 2015) | 1.06 |
"In this phase 1, open-label study, adult patients with epilepsy on a stable oral carbamazepine dosage (400-2,000 mg/day) were converted to intravenous carbamazepine (administered at 70% of the oral dosage)." | ( Bioequivalence of oral and intravenous carbamazepine formulations in adult patients with epilepsy. Bekersky, I; Biton, V; Cloyd, J; Drummond, R; Lee, D; Tolbert, D; Walzer, M; Wesche, D, 2015) | 0.91 |
" The mean daily oral and intravenous carbamazepine dosage for 64 PK-evaluable patients with normal renal function was 962." | ( Bioequivalence of oral and intravenous carbamazepine formulations in adult patients with epilepsy. Bekersky, I; Biton, V; Cloyd, J; Drummond, R; Lee, D; Tolbert, D; Walzer, M; Wesche, D, 2015) | 0.96 |
" Hence, oxcarbazepine can be generally applied using the same dosage and administration for the treatment of partial onset seizures in pediatric patients, regardless of ethnicity." | ( Population pharmacokinetic analysis for 10-monohydroxy derivative of oxcarbazepine in pediatric epileptic patients shows no difference between Japanese and other ethnicities. Bouillon, T; Fink, M; Hirota, T; Sugiyama, I; Suzuki, H; Yamaguchi, M, 2015) | 0.42 |
"To assess efficacy/tolerability of ezogabine (EZG)/retigabine (RTG) in combination with specified monotherapy antiepileptic drug (AED) treatments in adults with uncontrolled partial-onset seizures using a flexible dosing regimen." | ( Efficacy and safety of ezogabine/retigabine as adjunctive therapy to specified single antiepileptic medications in an open-label study of adults with partial-onset seizures. Brandt, C; Daniluk, J; DeRossett, S; Edwards, S; Lerche, H; Lotay, N, 2015) | 0.42 |
"NCT01227902 was an open-label, uncontrolled study of flexibly dosed EZG/RTG." | ( Efficacy and safety of ezogabine/retigabine as adjunctive therapy to specified single antiepileptic medications in an open-label study of adults with partial-onset seizures. Brandt, C; Daniluk, J; DeRossett, S; Edwards, S; Lerche, H; Lotay, N, 2015) | 0.42 |
"EZG/RTG was effective as adjunctive therapy to CBZ/OXC, LTG, LEV, and VPA, using a flexible dosing regimen, in adults with partial-onset seizures; safety and tolerability were consistent with that previously observed." | ( Efficacy and safety of ezogabine/retigabine as adjunctive therapy to specified single antiepileptic medications in an open-label study of adults with partial-onset seizures. Brandt, C; Daniluk, J; DeRossett, S; Edwards, S; Lerche, H; Lotay, N, 2015) | 0.42 |
" Furthermore, two interactions between these genes were associated with the lnCDR and the maintenance dosage of CBZ, respectively." | ( Association between PK/PD-involved gene polymorphisms and carbamazepine-individualized therapy. Hong, Z; Jiao, Z; Ma, CL; Wu, XY; Wu, ZY; Zhong, MK, 2015) | 0.66 |
"Hypromellose is a hydrophilic polymer widely used in immediate- and modified-release oral pharmaceutical dosage forms." | ( A New Extrudable Form of Hypromellose: AFFINISOL™ HPMC HME. Huang, S; Keen, JM; McGinity, JW; O'Donnell, KP; Rickard, MA; Williams, RO, 2016) | 0.43 |
"The occurrence of AEs is significantly (and non-linearly) dependent on MHD serum level, whereas the dependence of OXC dosage is less distinctive." | ( Relationship between mono-hydroxy-carbazepine serum concentrations and adverse effects in patients on oxcarbazepine monotherapy. May, TW; Sattler, A; Schaefer, M, 2015) | 0.42 |
" This necessitates their robust stabilization in order for successful use in a tablet dosage form." | ( The development of carbamazepine-succinic acid cocrystal tablet formulations with improved in vitro and in vivo performance. Hussain, I; Sun, CC; Ullah, M, 2016) | 0.76 |
" Patients resistant to CBZ treatment showed increased dosage of CBZ (657 ± 285 vs 489 ± 231 mg/day; P<0." | ( Polymorphic Variants of SCN1A and EPHX1 Influence Plasma Carbamazepine Concentration, Metabolism and Pharmacoresistance in a Population of Kosovar Albanian Epileptic Patients. Beretta, G; Daci, A; Govori, V; Krasniqi, S; Norata, GD; Shala, A; Vllasaliu, D, 2015) | 0.66 |
" Patients were on stable TPM dosing regimen for at least 7 days; therefore, steady-state was assumed." | ( Application of Counter-propagation Artificial Neural Networks in Prediction of Topiramate Concentration in Patients with Epilepsy. Erić, S; Grabnar, I; Jovanović, M; Kuzmanovski, I; Miljković, B; Prostran, M; Sokić, D; Vovk, T; Vučićević, K, 2015) | 0.42 |
"Individual dosing of medicines is relevant for paediatrics, geriatrics and personalised medicine." | ( Micropellet-loaded rods with dose-independent sustained release properties for individual dosing via the Solid Dosage Pen. Breitkreutz, J; Knop, K; Laukamp, EJ; Thommes, M, 2016) | 0.43 |
"31) for area under the curve from time zero to the end of the dosing interval (AUC(0-τ)), maximum observed plasma concentration (Cmax), and plasma concentration at the end of the dosing interval (Cτ), respectively." | ( Effect of carbamazepine on dolutegravir pharmacokinetics and dosing recommendation. Borland, J; Choukour, M; Jerva, F; Patel, J; Piscitelli, S; Song, I; Weller, S; Wynne, B, 2016) | 0.84 |
" This population PK model can be applied for optimizing topiramate dosage regimens in actual clinical practice." | ( Factors influencing topiramate clearance in adult patients with epilepsy: A population pharmacokinetic analysis. Bae, EK; Jang, IJ; Kim, TJ; Lee, J; Lee, KJ; Lee, SK; Moon, J; Shin, D; Shin, JW; Shin, YW, 2016) | 0.43 |
" Type I isobolographic analysis for parallel dose-response relationship curves (DRRCs) was used to analyze the 3-drug combination." | ( Isobolographic Analysis of Interaction for Three-Drug Combination of Carbamazepine, Phenobarbital and Topiramate in the Mouse Maximal Electroshock-Induced Seizure Model. Luszczki, JJ, 2016) | 0.67 |
"Psychoactive pharmaceuticals have been found as teratogens at clinical dosage during pregnancy." | ( Maternal exposure to carbamazepine at environmental concentrations can cross intestinal and placental barriers. Aho, K; Bearden, S; Finney, B; Huber, DP; Kaushik, G; Thomas, MA; Zarbalis, KS, 2016) | 0.75 |
" During and after the experimental process, CBZ did not significantly affect the efficiency of the MBR system, and the quality of the effluent was not affected by the dosing of CBZ in terms of COD and nitrogen removal." | ( Carbamazepine behaviour and effects in an urban wastewater MBR working with high sludge and hydraulic retention time. González-Pérez, DM; Nieto, MÁ; Pérez, JI, 2016) | 1.88 |
" The ultimate goal of this research is to improve the compliance of patients through a dosage form that provides a zero-order drug release profile for anti-epileptic drugs, so as to achieve therapeutic doses and minimize side effects." | ( Three-Dimensional Printing of Carbamazepine Sustained-Release Scaffold. Chia, SM; Kang, L; Lim, SH; Yap, KY, 2016) | 0.72 |
" In this phase IIIb, prospective, multicenter, open-label, single-arm trial (NCT01375374), the serum concentrations of CYP-related reproductive hormones, thyroid hormones, and lipids were assessed in otherwise healthy male patients with focal seizures (N=11), before and after a switch from CBZ (600-1200mg/day at baseline) to lacosamide (target dose: 400mg/day by the end of titration) as adjunctive treatment to the nonenzyme-inducing AED levetiracetam (LEV, stable dosage of >1000mg/day throughout)." | ( Changes in hormone and lipid levels in male patients with focal seizures when switched from carbamazepine to lacosamide as adjunctive treatment to levetiracetam: A small phase IIIb, prospective, multicenter, open-label trial. Brandt, C; De Backer, M; Dedeken, P; Eckhardt, K; Elger, CE; Elmoufti, S; Rademacher, M; Tennigkeit, F, 2016) | 0.65 |
" Patients were switched because they experienced persistent seizures with OXC but were unable to tolerate increased OXC dosing due to adverse events." | ( Overnight switching from oxcarbazepine to eslicarbazepine acetate: an observational study. Höfler, J; Kalss, G; Kirschner, M; Kuchukhidze, G; Leitinger, M; Rohracher, A; Schmid, E; Steinhoff, BJ; Trinka, E; Wendling, AS, 2017) | 0.46 |
" There is no need to limit brivaracetam dosing when used concomitantly with carbamazepine." | ( Pharmacokinetic interaction of brivaracetam on carbamazepine in adult patients with epilepsy, with and without valproate co-administration. Brodie, MJ; Sargentini-Maier, ML; Stockis, A, 2016) | 0.92 |
" Further development of MT as a single unit or multicompartment prolonged-release new dosage form especially suitable for children has been justified." | ( Prolonged-release minitablets with carbamazepine - preliminary observations in vitro. Anna, M; Anna, S; Dagmara, D; Dzajkowska, M; Hanna, K; Maja, S; Malgorzata, S, 2017) | 0.73 |
" Pharmacokinetics of carbamazepine in children is age and body weight dependent and highly variable due to influence of dosing regimen and co-medication." | ( Pharmacokinetics and Pharmacogenetics of Carbamazepine in Children. Djordjevic, N; Jankovic, SM; Milovanovic, JR, 2017) | 1.04 |
" The dosage of PB was ranked first followed by that of CBZ and finally by the VPA." | ( [Therapeutic drug monitoring of three antiepileptic drugs - Back on twenty years of experience]. Badrane, N; Bencheikh, RS; Moussa, LA; Ouammi, L; Serragui, S; Tanani, DS; Zalagh, F, 2016) | 0.43 |
" Moreover, this study revealed that CBZ dosage was related to toxicity in mice." | ( Evaluating the Effectiveness of GTM-1, Rapamycin, and Carbamazepine on Autophagy and Alzheimer Disease. Che, H; Fu, P; Gao, Y; Pan, Y; Wang, L; Wang, R; Zhang, L, 2017) | 0.7 |
" A population pharmacokinetic (PPK) analysis was performed to improve the topiramate dosage adjustment for individualized treatment." | ( Population Pharmacokinetics of Topiramate in Japanese Pediatric and Adult Patients With Epilepsy Using Routinely Monitored Data. Ikeda, A; Ito, S; Matsubara, K; Sugimoto, M; Takeuchi, M; Yamamoto, S; Yano, I; Yonezawa, A, 2017) | 0.46 |
" Simulations based on the final model showed that dosage adjustments allometrically scaling to body weight can equalize the serum concentrations in children of various ages and adults." | ( Population Pharmacokinetics of Topiramate in Japanese Pediatric and Adult Patients With Epilepsy Using Routinely Monitored Data. Ikeda, A; Ito, S; Matsubara, K; Sugimoto, M; Takeuchi, M; Yamamoto, S; Yano, I; Yonezawa, A, 2017) | 0.46 |
" Dosage adjustments based on body weight and concomitant antiepileptic drug help obtain the dosage of topiramate necessary to reach an effective concentration in each individual." | ( Population Pharmacokinetics of Topiramate in Japanese Pediatric and Adult Patients With Epilepsy Using Routinely Monitored Data. Ikeda, A; Ito, S; Matsubara, K; Sugimoto, M; Takeuchi, M; Yamamoto, S; Yano, I; Yonezawa, A, 2017) | 0.46 |
" We sought to determine whether there were regions in the dosage range of commonly used AEDs that were associated with superior efficacy in patients with refractory epilepsy." | ( Association between antiepileptic drug dose and long-term response in patients with refractory epilepsy. Castagna, CE; Miller, AB; Poolos, NP; Story, TJ; Williams, S, 2017) | 0.46 |
"The aims of the study were to develop a population pharmacokinetic model of orally administered brivaracetam in paediatric patients and to provide dosing suggestions." | ( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years. Schoemaker, R; Stockis, A; Wade, JR, 2017) | 0.46 |
" Simulations were performed to investigate dosing regimens." | ( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years. Schoemaker, R; Stockis, A; Wade, JR, 2017) | 0.46 |
" Data suggest no need to change brivaracetam dosing when used concomitantly with carbamazepine, phenobarbital or valproate." | ( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years. Schoemaker, R; Stockis, A; Wade, JR, 2017) | 0.68 |
" This improvement is more pronounced if the OXC-related AEs are most evident following morning dosing of OXC." | ( Transition from oxcarbazepine to eslicarbazepine acetate: A single center study. Mäkinen, J; Peltola, J; Rainesalo, S, 2017) | 0.46 |
" These techniques have encountered challenges in analyzing the constitution of polymorphs in the presence of other components commonly found in pharmaceutical dosage forms." | ( Investigation of the Sensitivity of Transmission Raman Spectroscopy for Polymorph Detection in Pharmaceutical Tablets. Anderson, CA; Bondi, RW; Drennen, JK; Feng, H; Igne, B, 2017) | 0.46 |
" Epidemiologic data, type of epilepsy, etiology, the age of seizure onset, duration of epilepsy, intractable epilepsy, and number and dosage of AEDs were recorded." | ( Effects of antiepileptic drugs on thyroid hormone function in epilepsy patients. Chuang, MJ; Chuang, YC; Fu, TY; Lu, YT; Shih, FY; Tsai, MH; Tsai, WC, 2017) | 0.46 |
"Nonadherence to prescribed dosing regimens is a significant problem in the treatment of pediatric and adult chronic epilepsy, and can result in severe consequences to patient outcomes." | ( The impact of nonadherence to antiseizure drugs on seizure outcomes in an animal model of epilepsy. Glauser, TA; Modi, AC; Rausch, JR; Steve White, H; Thomson, KE, 2017) | 0.46 |
"In study 1, three different patterns of nonadherence were modeled in newly diagnosed epileptic rats treated with carbamazepine: perfect adherence (100% of pellets contained carbamazepine), variable nonadherence (50% of pellets contained carbamazepine with different dosing patterns between animals), and complete nonadherence (0% of pellets contained carbamazepine)." | ( The impact of nonadherence to antiseizure drugs on seizure outcomes in an animal model of epilepsy. Glauser, TA; Modi, AC; Rausch, JR; Steve White, H; Thomson, KE, 2017) | 0.67 |
"To review the pharmacology, pharmacokinetics, efficacy, safety, dosage and administration, potential drug-drug interactions, and place in therapy of the intravenous (IV) formulation of carbamazepine (Carnexiv) for the treatment of seizures in adult patients." | ( Intravenous Carbamazepine for Adults With Seizures. DeFalco, AP; Tillery, EE; Vickery, PB, 2018) | 1.05 |
" The polymeric carriers are long known to manipulate this conversion during dissolution to parent crystalline drug, which may hinder or accelerate the dissolution process if used in a dosage form." | ( Improved in vitro and in vivo performance of carbamazepine enabled by using a succinic acid cocrystal in a stable suspension formulation. Bin Asad, MHH; Hasan, SMF; Hussain, I; Shah, MR; Ullah, M, 2017) | 0.71 |
" For this dosage form, the product quality is related amongst others to the drug content." | ( Inline UV/Vis spectroscopy as PAT tool for hot-melt extrusion. Berghaus, A; Prill, S; Thommes, M; Wesholowski, J, 2018) | 0.48 |
" Oxcarbazepine dosage was found to linearly correlate with AEP and ABNAS scores, better than carbamazepine dosage." | ( Adverse effects of anti-epileptics in trigeminal neuralgiform pain. Cregg, R; Lee, G; O'Keeffe, AG; Reading, J; Tentolouris-Piperas, V; Zakrzewska, JM, 2018) | 0.7 |
" The purpose of this review is to provide an up-to-date evidence summary of the incidence and outcomes of seizures following an SAH as well as the use of different AEDs post-SAH in order to evaluate the need for seizure prophylaxis, the choice of AEDs, and their dosing considerations in SAH patients." | ( Seizures and Choice of Antiepileptic Drugs Following Subarachnoid Hemorrhage: A Review. Buxton, J; Mahmoud, SH, 2017) | 0.46 |
" Idiosyncratic DILI is most often unrelated to pharmacological effects or the dosing amount of a drug." | ( Role of cytochrome P450-mediated metabolism and involvement of reactive metabolite formations on antiepileptic drug-induced liver injuries. Sasaki, E; Yokoi, T, 2018) | 0.48 |
" Chronic water borne exposures of adult zebrafish to 10 μg/L of GEM and CBZ were conducted and the dosing was confirmed by chemical analysis of water as 17." | ( Gemfibrozil and carbamazepine decrease steroid production in zebrafish testes (Danio rerio). Fraz, S; Lee, AH; Wilson, JY, 2018) | 0.83 |
"The present investigation was undertaken with an objective of formulating sustained release microspheres of oxcarbazepine (OXC), an anti-epileptic drug, to overcome poor patient compliance and exposure to high doses associated with currently marketed OXC dosage forms." | ( COLOCASIA ESCULENTA CORMS MUCILAGE-ALGINATE MICROSPHERES OF OXCARBAZEPINE: DESIGN, OPTIMIZATION AND EVALUATION. Ahmad, J; Bashir, S; Ghumman, SA; Hameed, H; Khan, IU, 2017) | 0.46 |
"Evidence for the comparative teratogenic risk of antiepileptic drugs is insufficient, particularly in relation to the dosage used." | ( Comparative risk of major congenital malformations with eight different antiepileptic drugs: a prospective cohort study of the EURAP registry. Battino, D; Bonizzoni, E; Craig, J; Lindhout, D; Perucca, E; Sabers, A; Thomas, SV; Tomson, T; Vajda, F, 2018) | 0.48 |
"This formulation reduced systemic exposure to carbamazepine over 1,000-fold relative to traditional analgesic dosing regimens." | ( Opiate-Free Pain Therapy Using Carbamazepine-Loaded Microparticles Provides Up to 2 Weeks of Pain Relief in a Neuropathic Pain Model. Dai, H; Doherty, C; Gulati, A; Holzhaus, K; Khalil, A; Mehta, N; Mercedes, G; Reynolds, FM; Tilley, DM, 2018) | 1.03 |
"In the therapeutic drug monitoring group, clinicians had access to clinical findings and monthly serum AED levels to guide AED dosage adjustment for seizure control." | ( AntiEpileptic drug Monitoring in PREgnancy (EMPiRE): a double-blind randomised trial on effectiveness and acceptability of monitoring strategies. Bagary, M; Coleman, J; D'Amico, M; Denny, E; Dodds, J; Eldridge, S; Greenhill, L; Hard, K; Kelso, A; Khan, KS; Marlin, N; McCorry, D; Middleton, L; Moss, N; Newton, S; Pirie, A; Pullen, A; Rikunenko, R; Roberts, T; Rogozińska, E; Thangaratinam, S; Weckesser, A, 2018) | 0.48 |
" In the present study, we investigated whether the pharmacokinetic profile of orally administered carbamazepine (CBZ) is altered by a treatment with SA immediately before and after dosing of the drug." | ( Alterations in Pharmacokinetics of Orally Administered Carbamazepine in Rats Treated with Sodium alginate: Possible Interaction between Therapeutic Drugs and Semi-solid Enteral Nutrients. Hatsuda, Y; Ito, A; Mukai, J; Myotoku, M; Nagai, K; Nishimura, I; Omotani, S; Teramachi, H, 2019) | 0.98 |
" The review presents the current published data on the incidence of seizures in pregnant women, specificity of therapy with antiepileptic drugs (AEDs), frequency of fetal malformations in pregnant women taking AEDs regularly and their dependence on the frequency, dosage and nature of therapy." | ( [Modern aspects of antiepileptic therapy during pregnancy]. Kispayeva, TT; Nurakhmetova, AS, ) | 0.13 |
" When sodium channel blockers cannot reach full dosage because of side effects, an add-on treatment with lamotrigine or baclofen should be considered." | ( Current and Innovative Pharmacological Options to Treat Typical and Atypical Trigeminal Neuralgia. Cruccu, G; Di Stefano, G; Truini, A, 2018) | 0.48 |
"The aim of this study was to demonstrate the usefulness of the time domain nuclear magnetic resonance (TD-NMR) method to characterize the crystalline state of active pharmaceutical ingredients (APIs) containing solid dosage forms." | ( Hayashi, Y; Hirai, D; Kosugi, A; Kumada, S; Okada, K; Onuki, Y, 2019) | 0.51 |
" Inclusion criteria included residency in a nursing home for at least 2 months, age 65 years or older, a stable dosing regimen of CBZ for at least 4 weeks (considered steady state), available CBZ concentration, and complete information regarding all co-medications." | ( Iron supplements in nursing home patients associated with reduced carbamazepine absorption. Ahn, JE; Bathena, SPR; Birnbaum, AK; Brundage, RC; Conway, JM; Leppik, IE, 2018) | 0.72 |
"Results from this pharmacokinetic study indicate that use of iron supplementation is associated with a reduction in absorption of CBZ and may need to be considered when dosing CBZ in patients taking iron supplementation." | ( Iron supplements in nursing home patients associated with reduced carbamazepine absorption. Ahn, JE; Bathena, SPR; Birnbaum, AK; Brundage, RC; Conway, JM; Leppik, IE, 2018) | 0.72 |
" Subsequently, nanoparticles were spray-dried and tableted to provide a differentiated solid dosage form." | ( Rethinking carbamazepine oral delivery using polymer-lipid hybrid nanoparticles. Ana, R; Falcão, A; Fortuna, A; Mendes, M; Pais, A; Sousa, J; Vitorino, C, 2019) | 0.9 |
" A new dosing strategy combining the dosage guideline and Bayesian method is proposed to individualise OXC regimens." | ( Population pharmacokinetics of oxcarbazepine active metabolite in Chinese paediatric epilepsy patients and its application in individualised dosage regimens. Jiao, Z; Li, XW; Lin, WW; Lin, XH; Rao, X; Wang, CL; Zeng, DY; Zhang, J, 2019) | 0.51 |
"A PPK model was established to estimate individual MHD clearance in paediatric patients taking OXC to develop individualised OXC dosing regimens for Chinese paediatric epilepsy patients." | ( Population pharmacokinetics of oxcarbazepine active metabolite in Chinese paediatric epilepsy patients and its application in individualised dosage regimens. Jiao, Z; Li, XW; Lin, WW; Lin, XH; Rao, X; Wang, CL; Zeng, DY; Zhang, J, 2019) | 0.51 |
" In the clinical setting, these findings can help to estimate LTG concentrations and adjust dosage and evaluate adverse drug reactions." | ( The influence of concomitant antiepileptic drugs on lamotrigine serum concentrations in Northwest Chinese Han population with epilepsy. Han, X; Huang, J; Lv, J; Ma, L; Nie, X; Peng, L; Wang, J; Xia, L; Zan, X, 2019) | 0.51 |
" The MHD plasma concentration was detected by high-performance liquid chromatography and then standardized through dosage and body weight." | ( Comparison of oxcarbazepine efficacy and MHD concentrations relative to age and BMI: Associations among ABCB1, ABCC2, UGT2B7, and SCN2A polymorphisms. Chen, X; Fang, S; Gong, Z; Ma, H; Qian, L; Wei, J; Xu, Z; Yan, Y; Yang, X; Zeng, S, 2019) | 0.51 |
"22) with evidence of a dose-response relationship for carbamazepine." | ( Use of antiepileptic drugs and risk of skin cancer: A nationwide case-control study. Kristensen, KB; Pedersen, SA; Pottegård, A; Schmidt, SAJ, 2020) | 0.81 |
" Collectively, healthcare providers should take these factors in consideration for optimal valproic acid dosage regimen." | ( Estimation of apparent clearance of valproic acid in adult Saudi patients. Alandas, N; Alqahtani, S; Alsultan, A, 2019) | 0.51 |
" There was no change in open-field test activity following acute or chronic oral dosing of 75 mg/kg CBZ compared to a pretreatment baseline (P > 0." | ( The pharmacokinetics of oral carbamazepine in rats dosed using an automated drug delivery system. Hill, AC; Rower, JE; White, HS, 2019) | 0.81 |
"Five groups of each of 12 female rats were orally dosed daily for 8 weeks with either carbamazepine (CBZ) (60 mg/kg), eslicarbazepine (ESL) (80 mg/kg), valproic acid (VPA) (300 mg/kg), levetiracetam (LEV) (50 mg/kg) or saline (control (CTL))." | ( Effects of carbamazepine, eslicarbazepine, valproic acid and levetiracetam on bone microarchitecture in rats. Andersen, NB; Diemar, SS; Ding, M; Eiken, P; Ellegaard, M; Jørgensen, NR; Sejling, AS, 2020) | 1.17 |
" Thus, this study offers a potentially effective means of transforming poorly water soluble BCS Class II APIs into fast dissolving solid dosage NP-carrier composites, whereby the surface properties of the carrier particle can be tuned with prior knowledge of the zeta potential of the API nanoparticles." | ( Modification of the zeta potential of montmorillonite to achieve high active pharmaceutical ingredient nanoparticle loading and stabilization with optimum dissolution properties. Davern, P; Hodnett, BK; Hudson, S; Kumar, A, 2020) | 0.56 |
"To determine the degree of cross-contamination and to validate a cleaning process for an Automated Personalised Dosing System (APDS), respecting the permitted residue transfer limits." | ( Determination of the cross-contamination and validation of the cleaning process for an automated personalised dosing system. Beobide Telleria, I; Ferro Uriguen, A; Martínez Arrechea, S; Miró Isasi, B; Sampedro Yangüela, C; Urretavizcaya Anton, M, 2022) | 0.72 |
" This might endow the formulator flexibility in the design and dosage form with less bulky economic and more patient friendly solid platform for those epileptic patients and/or elderly patients that can experience difficulty in swallowing and need rapid onset of action." | ( Comparative studies of the effects of novel excipients amino acids with cyclodextrins on enhancement of dissolution and oral bioavailability of the non-ionizable drug carbamazepine. Abdelkader, H; Abou-Taleb, HA; Fathalla, Z, 2020) | 0.75 |
" Logistic regression analysis showed that carbamazepine dosage had a statistically significant relationship with a decreasing rate of patient-recognized depression occurring during pregnancy and topiramate dosage with an increasing rate." | ( Antiepileptic drugs and depression during pregnancy in women with epilepsy. Eadie, MJ; Graham, JE; Hitchcock, AA; Horgan, D; Lander, CM; Mitchell, J; O'Brien, TJ; Vajda, FJE, 2020) | 0.82 |
"6%), major side effects caused treatment interruption or dosage reduction to an unsatisfactory level." | ( Real-world effectiveness and tolerability of carbamazepine and oxcarbazepine in 354 patients with trigeminal neuralgia. Cruccu, G; De Stefano, G; Di Lionardo, A; Di Pietro, G; Di Stefano, G; Leone, C; Mollica, C; Sgro, E; Truini, A, 2021) | 0.88 |
"Literature relevant to assessing whether BCS-based biowaivers can be applied to immediate release (IR) solid oral dosage forms containing carbamazepine as the single active pharmaceutical ingredient are reviewed." | ( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Carbamazepine. Abrahamsson, B; Cristofoletti, R; Dressman, JB; García, MA; Groot, DW; Langguth, P; Mehta, M; Parr, A; Polli, JE; Shah, VP; Tomakazu, T, 2021) | 1.06 |
"This is a retrospective data analysis of 646 consecutive AED-naive patients aged 1-88 years treated with CBZ, LTG, or LEV between 2006 and 2012 with dosing adjustments permitted during the first 6 months." | ( Effectiveness at 24 Months of Single-Source Generic Carbamazepine, Lamotrigine, or Levetiracetam in Newly Diagnosed Focal Epilepsy. Chayasirisobhon, S; Gurbani, A; Gurbani, S; Pietzsch, E; Spurgeon, B; Tovar, S, 2020) | 0.81 |
" It affects drug manufacturing, development processes, and the stability of pharmaceutical dosage forms." | ( The impact of carbamazepine crystallinity on carbamazepine-loaded microparticle formulations. Chatterjee, B; Doolaanea, AA; Hadi, HA; Mawazi, SM, 2021) | 0.98 |
" To facilitate this, manufacturers have developed a strict re-challenge dosing regimen to facilitate successful reintroduction of lamotrigine." | ( Lamotrigine and Stevens-Johnson Syndrome Prevention. Crane, E; Edinoff, AN; Fitz-Gerald, MJ; Gennuso, SA; Kaye, AD; Kaye, AM; Kaye, JS; Kaye, RJ; Lewis, K; Nguyen, LH; Pierre, SS; Urits, I; Varrassi, G; Viswanath, O, 2021) | 0.62 |
" Similar dose-related responses were seen following the week-long dosing protocol for carbamazepine, phenobarbital, and phenytoin, and these responses were associated with drug levels that were in the human therapeutic range." | ( Chronic limbic epilepsy models for therapy discovery: Protocols to improve efficiency. Bertram, EH; Edelbroek, P, 2021) | 0.84 |
"002), and daily dosage (> 1,000 mg/d; OR = 19." | ( Investigation of the risk of valproic acid-induced tremor: clinical, neuroimaging, and genetic factors. Huang, S; Jian, S; Kang, H; Kirsch, HE; Lan, L; Li, C; Wang, M; Zhao, X; Zhou, Q; Zhu, S, 2022) | 0.72 |
"In this study, we examined whether the pharmacokinetic profiles of sodium valproate (SVA), levetiracetam (LEV), and carbamazepine (CBZ) are affected by altering the dosing time of RACOL®-NF Semi Solid for Enteral Use (RASS), a prescribed semi-solid formula." | ( Effects of concurrent and staggered dosing of semi-solid enteral nutrients on pharmacokinetic behavior of antiepileptic drugs after oral administration in rats. Fukuno, S; Hatsuda, Y; Iwanami, Y; Konishi, H; Myotoku, M; Nagai, K; Omotani, S; Ryuno, Y, 2021) | 0.83 |
"There was no difference in pharmacokinetic characteristics of SVA and LEV when the dosing time of RASS was altered." | ( Effects of concurrent and staggered dosing of semi-solid enteral nutrients on pharmacokinetic behavior of antiepileptic drugs after oral administration in rats. Fukuno, S; Hatsuda, Y; Iwanami, Y; Konishi, H; Myotoku, M; Nagai, K; Omotani, S; Ryuno, Y, 2021) | 0.62 |
"We concluded that the pharmacokinetic profiles of CBZ, but not SVA and LEV, after its oral administration are affected by the dosing time of RASS, but staggered administration of CBZ and RASS prevented their interaction." | ( Effects of concurrent and staggered dosing of semi-solid enteral nutrients on pharmacokinetic behavior of antiepileptic drugs after oral administration in rats. Fukuno, S; Hatsuda, Y; Iwanami, Y; Konishi, H; Myotoku, M; Nagai, K; Omotani, S; Ryuno, Y, 2021) | 0.62 |
" In this article, we describe a case of a 40-year-old female who presented to a local emergency department with focal neurological deficits after repeated supratherapeutic dosing of carbamazepine." | ( Neurologic toxicity of carbamazepine in treatment of trigeminal neuralgia. Birdsong, S; Bridwell, RE; Brown, S; Clerkin, S; Long, B, 2022) | 1.22 |
" For 25 years, this author has focused on a circumscribed type of precision medicine: personalized dosing using pharmacokinetic mechanisms to stratified patients." | ( Precision psychiatry: The complexity of personalizing antipsychotic dosing. de Leon, J, 2022) | 0.72 |
"In the present study, we examined the effects of concurrent and staggered dosing of PG-soft ace-MP TM (PG), novel semi-solid enteral nutrients, on the pharmacokinetics of orally administered carbamazepine (CBZ) in rats due to the high possibility of drug interaction during the absorption process." | ( Influence of concurrent and staggered dosing of semi-solid nutrients on the pharmacokinetics of orally administered carbamazepine in rats. Fukuno, S; Hatsuda, Y; Konishi, H; Kuroda, H; Miura, T; Moriwaki, R; Myotoku, M; Nagai, K; Omotani, S, 2022) | 1.12 |
"Swallowing oral solid dosage forms is challenging in patients with dysphagia who are at risk of aspiration or choking." | ( Do Thickening Agents Used in Dysphagia Diet Affect Drug Bioavailability? Erdem, ÇE; Eroğlu, H; Eylem, CC; Gökmen-Özel, H; Ilgaz, F; Nemutlu, E; Timur, SS, 2022) | 0.72 |
"This review aims to identify the optimal therapeutic dosage of anti-epileptic drugs in terms of efficacy and safety in patients with multiple comorbidities." | ( Individualizing doses of antiepileptic drugs. Burchiani, B; Di Cara, G; Liparoti, G; Mencaroni, E; Tripodi, D; Verrotti, A, 2022) | 0.72 |
"Orthokine injection led to consistent pain relief and reduced carbamazepine dosage in patients with trigeminal neuralgia, with acceptable safety." | ( Autologous conditioned serum (Orthokine) injection for treatment of classical trigeminal neuralgia: results of a single-center case series. Aghamohammadi, D; Dolatkhah, N; Eslampour, Y; Shakouri, SK; Sharifi, S, 2022) | 0.96 |
"Pharmacogenomics (PGx) is a research area aimed at identifying genetic factors that are associated with drug responses, including drug efficacy, adverse drug reactions, and the appropriate drug dosage on a case-to-case basis." | ( Avoidance of cutaneous adverse drug reactions induced by antiepileptic drugs based on pharmacogenomics. Mushiroda, T, 2023) | 0.91 |
" As a general rule, these interactions can be managed by careful evaluation of clinical response and, when indicated, individualized dosage adjustments guided by measurement of drugs serum concentrations, especially if pharmacokinetic interactions may cause any change in seizure control or signs of toxicity." | ( Pharmacokinetic Interactions Between Antiseizure and Psychiatric Medications. Franco, V; Zaccara, G, 2023) | 0.91 |
"Carbamazepine (CBZ), a drug prescribed to prevent seizures in people with epilepsy, has a narrow therapeutic range such that patients would greatly benefit from personalized drug dosage recommendations." | ( Comparison of signal enhancement strategies for carbamazepine detection in undiluted human saliva using an electrochemical sensor with stencil-printed carbon electrodes. Downs, C; Fu, E; Wentland, L, 2022) | 2.42 |
" Inclusion criteria were monotherapy of CBZ in adequate dosage for epilepsy treatment and RCT duration of ≥3 months." | ( Anti-seizure efficacy and retention rate of carbamazepine is highly variable in randomized controlled trials: A meta-analysis. Hoppe, C; Olaciregui-Dague, K; Schmid, M; Surges, R; Weinhold, L, 2022) | 0.98 |
" In this communication, we describe eight patients undergoing sleeve gastrectomy (SG) and treated with CBZ, including therapeutic drug monitoring (TDM) and dosage adjustments at different timeframes before vs." | ( Carbamazepine Therapy After Bariatric Surgery: Eight Sleeve Gastrectomy Cases and Review of the Literature. Dahan, A; Lavon, O; Margolin, N; Porat, D, 2022) | 2.16 |
" Mytilus galloprovincialis were exposed to environmental levels of CBZ and VAL dosed alone or in combination: measurement of drug bioaccumulation was integrated with changes in the whole transcriptome and responsiveness of various biochemical and cellular biomarkers." | ( Mixtures of environmental pharmaceuticals in marine organisms: Mechanistic evidence of carbamazepine and valsartan effects on Mytilus galloprovincialis. d'Errico, G; Gorbi, S; Mezzelani, M; Milan, M; Peruzza, L; Regoli, F, 2023) | 1.13 |
"A correlative, multiscale imaging methodology for visualising and quantifying the morphology of solid dosage forms by combining ptychographic X-ray computed nanotomography (PXCT) and scanning small- and wide-angle X-ray scattering (S/WAXS) is presented." | ( Multiscale X-ray imaging and characterisation of pharmaceutical dosage forms. Abrahmsén-Alami, S; Diaz, A; Govender, R; Holler, M; Larsson, A; Liebi, M; Matic, A; Menzel, A; Olsson, M; Sadd, M, 2023) | 0.91 |
"97%), switching to or adjusting carbamazepine dosage (27." | ( The impact of a newly established specialized pediatric epilepsy center in Tanzania: An observational study. Aricò, M; Di Noia, SP; Kalolo, A; Mabusi, MS; Mastrangelo, M; Pisani, F, 2023) | 1.19 |
" Among the symptomatic treatments with anticonvulsants, carbamazepine was the most efficacious anticonvulsant in treatment of IS, with an average effective dosing of 480 mg/day (carbamazepine was used in 32." | ( Systematic Review of the Clinical Characteristics and Management of Isaac Syndrome. Abouainain, Y; Al-Chalabi, M; Eid, J; Hegde, P; Keener, M; Moore, SR; Parvez, H; Saleem, S; Sheikh, A, 2023) | 1.16 |
"8), adsorbent dosage (1." | ( Sustainable development and analysis of a novel bio-derived (biochar) nanocomposite for the remediation of carbamazepine from aqueous solution. G, S; M, R; P, A; S, V, 2024) | 1.66 |
Role | Description |
---|---|
anticonvulsant | A drug used to prevent seizures or reduce their severity. |
EC 3.5.1.98 (histone deacetylase) inhibitor | An EC 3.5.1.* (non-peptide linear amide C-N hydrolase) inhibitor that interferes with the function of histone deacetylase (EC 3.5.1.98). |
mitogen | A chemical substance that encourages a cell to commence cell division, triggering mitosis. |
glutamate transporter activator | A neurotransmitter transporter modulator that activates glutamate transporters. |
antimanic drug | Antimanic drugs are agents used to treat bipolar disorders or mania associated with other affective disorders. |
analgesic | An agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms. |
non-narcotic analgesic | A drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors. |
environmental contaminant | Any minor or unwanted substance introduced into the environment that can have undesired effects. |
xenobiotic | A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means. |
drug allergen | Any drug which causes the onset of an allergic reaction. |
sodium channel blocker | An agent that inhibits sodium influx through cell membranes. |
[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] |
Class | Description |
---|---|
dibenzoazepine | |
ureas | |
[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] |
Pathway | Proteins | Compounds |
---|---|---|
Carbamazepine Metabolism Pathway | 7 | 18 |
Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 6.3096 | 0.0447 | 17.8581 | 100.0000 | AID485341 |
acetylcholinesterase | Homo sapiens (human) | Potency | 35.4002 | 0.0025 | 41.7960 | 15,848.9004 | AID1347395 |
RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 0.2371 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
USP1 protein, partial | Homo sapiens (human) | Potency | 31.6228 | 0.0316 | 37.5844 | 354.8130 | AID743255 |
TDP1 protein | Homo sapiens (human) | Potency | 29.0929 | 0.0008 | 11.3822 | 44.6684 | AID686979 |
AR protein | Homo sapiens (human) | Potency | 5.4728 | 0.0002 | 21.2231 | 8,912.5098 | AID588515; AID743036; AID743040; AID743042; AID743053; AID743054 |
thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 6.3096 | 0.0013 | 18.0743 | 39.8107 | AID926; AID938 |
glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 12.0053 | 0.0002 | 14.3764 | 60.0339 | AID588532; AID720691; AID720692; AID720719 |
retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 30.4821 | 0.0030 | 41.6115 | 22,387.1992 | AID1159552 |
estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 51.4518 | 0.0015 | 30.6073 | 15,848.9004 | AID1224841; AID1224848; AID1224849 |
pregnane X nuclear receptor | Homo sapiens (human) | Potency | 44.8435 | 0.0054 | 28.0263 | 1,258.9301 | AID1346982; AID720659 |
estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 4.3639 | 0.0002 | 29.3054 | 16,493.5996 | AID743075; AID743080 |
IDH1 | Homo sapiens (human) | Potency | 1.0323 | 0.0052 | 10.8652 | 35.4813 | AID686970 |
euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 0.0224 | 0.0355 | 20.9770 | 89.1251 | AID504332 |
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 3.7578 | 0.0017 | 23.8393 | 78.1014 | AID743083 |
thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 0.4467 | 0.0100 | 39.5371 | 1,122.0200 | AID588547 |
nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 32.6427 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 0.1000 | 0.0398 | 16.7842 | 39.8107 | AID995 |
geminin | Homo sapiens (human) | Potency | 1.4488 | 0.0046 | 11.3741 | 33.4983 | AID624296; AID624297 |
Vpr | Human immunodeficiency virus 1 | Potency | 0.8913 | 1.5849 | 19.6264 | 63.0957 | AID651644 |
lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0040 | 0.8913 | 12.0676 | 28.1838 | AID1487 |
Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 0.3548 | 0.0023 | 19.5956 | 74.0614 | AID651743 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.6315 | 4.4531 | 9.3000 | AID1473740 |
Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 0.2000 | 5.6774 | 10.0000 | AID1473741 |
Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 (µMol) | 1,000.0000 | 0.4000 | 2.7500 | 8.6000 | AID1209456 |
Bile salt export pump | Homo sapiens (human) | IC50 (µMol) | 711.0000 | 0.1100 | 7.1903 | 10.0000 | AID1209455; AID1449628; AID1473738 |
Sodium channel protein type 1 subunit alpha | Rattus norvegicus (Norway rat) | IC50 (µMol) | 167.0000 | 0.0100 | 1.1405 | 2.9390 | AID205273 |
Sodium channel protein type 2 subunit alpha | Rattus norvegicus (Norway rat) | IC50 (µMol) | 167.0000 | 0.0040 | 1.1485 | 4.7300 | AID205273 |
Sodium channel protein type 3 subunit alpha | Rattus norvegicus (Norway rat) | IC50 (µMol) | 167.0000 | 0.0060 | 0.8605 | 2.9390 | AID205273 |
Cytochrome P450 2C9 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0000 | 2.8005 | 10.0000 | AID1210069 |
Sodium channel protein type 4 subunit alpha | Homo sapiens (human) | Ki | 52.0000 | 0.1800 | 0.1800 | 0.1800 | AID205290 |
Cytochrome P450 2J2 | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0120 | 2.5312 | 9.4700 | AID1210069 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 104.7130 | 0.0009 | 1.9014 | 10.0000 | AID576612 |
Sodium channel protein type 9 subunit alpha | Homo sapiens (human) | IC50 (µMol) | 22.0000 | 0.0060 | 2.7749 | 9.0000 | AID314412 |
Sodium channel protein type 9 subunit alpha | Homo sapiens (human) | Ki | 32.7000 | 0.3600 | 0.4300 | 0.5000 | AID1227820 |
Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 (µMol) | 133.0000 | 2.4100 | 6.3433 | 10.0000 | AID1473739 |
P2X purinoceptor 4 | Homo sapiens (human) | IC50 (µMol) | 100.0000 | 0.1560 | 2.9352 | 6.1000 | AID1064727 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Albumin | Rattus norvegicus (Norway rat) | Kd | 103.0000 | 1.4700 | 6.5317 | 9.3100 | AID1215123 |
Major prion protein | Homo sapiens (human) | EC50 (µMol) | 10.0000 | 0.3000 | 4.9000 | 10.0000 | AID161627 |
Cytochrome P450 2B6 | Homo sapiens (human) | EC50 (µMol) | 145.0000 | 1.3000 | 1.3000 | 1.3000 | AID1210066 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588501 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588499 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2006 | Cytometry. 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. |
AID588497 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The Journal of biological chemistry, 11-15, Volume: 294, Issue:46 | Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens. |
AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2006 | Cytometry. 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. |
AID588461 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2006 | Cytometry. 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. |
AID588459 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Current protocols in cytometry, Oct, Volume: Chapter 13 | Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2006 | Cytometry. 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. |
AID588460 | High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set | 2010 | Assay and drug development technologies, Feb, Volume: 8, Issue:1 | High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors. |
AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
AID1347050 | Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347045 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
AID1347049 | Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen | 2019 | Science translational medicine, 07-10, Volume: 11, Issue:500 | Inhibition of natriuretic peptide receptor 1 reduces itch in mice. |
AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID504836 | Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation | 2002 | The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16 | Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells. |
AID588378 | qHTS for Inhibitors of ATXN expression: Validation | |||
AID588349 | qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay | |||
AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
AID1392271 | Inhibition of human Nav1.2 expressed in CHOK1 cells assessed as reduction in peak inward current at 30th pulse using holding potential of -50 mV by patch clamp assay | 2018 | Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9 | 4-Substituted carbamazepine derivatives: Conformational analysis and sodium channel-blocking properties. |
AID1335453 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 100 mg/kg, ip after 4 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID113855 | Effective dose against convulsions induced by clonic pentylenetetrazole after intraperitoneal administration in experiment 2 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID344482 | Neurotoxicity in CF1 albino mouse after 0.5 hrs by rotarod test | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID1185528 | Toxicity in orally dosed Kunming mouse assessed as inability of animal to maintain equilibrium on rod for at least 1 min in each trial by rotarod test | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID603570 | Antiallodynic activity in Wistar albino rat chronic constriction injury-induced neuropathic pain model assessed as attenuation of cold allodynia after 0.5 to 1 hr at 100 mg/kg, ip | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Discovery of molecules for the treatment of neuropathic pain: synthesis, antiallodynic and antihyperalgesic activities of 5-(4-nitrophenyl)furoic-2-acid hydrazones. |
AID1079942 | Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source] | |||
AID1265485 | Neurotoxicity in po dosed Sprague-Dawley rat after 0.5 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID481710 | Anticonvulsant activity in mouse assessed as reduction of 3-mercaptopropionic acid-induced lethality at 50 mg/kg, ip administered 30 mins prior to 3-mercaptopropionic acid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID489789 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Combating oxidative stress in epilepsy: design, synthesis, quantum chemical studies and anticonvulsant evaluation of 1-(substituted benzylidene/ethylidene)-4-(naphthalen-1-yl)semicarbazides. |
AID477356 | Neurotoxicity in ip dosed Swiss albino mouse | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. |
AID588219 | FDA HLAED, gamma-glutamyl transferase (GGT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID351281 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against maximal electroshock-induced seizures administered before 30 mins of MES induction | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID178169 | Compound was tested for anticonvulsant activity after Oral Administration into rat by using MES screen test after 2 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID433901 | Toxicity in Kunming mouse assessed as thiosemicarbazide-induced lethality at 50 mg/kg, ip after 2.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID47016 | Anticonvulsant activity administered intraperitoneally in CF1 mice is the ability to protect the mice from MES(maximal electroshock seizure). | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID590663 | Neurotoxicity against Swiss mouse after 4 hrs by rotarod ataxia test | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-one derivatives. |
AID114383 | Tested for NMDLA induced seizures and protection against full generalized tonic seizures was recorded; Percentage of protection at 150 mg/kg per os. | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID588210 | Human drug-induced liver injury (DILI) modelling dataset from Ekins et al | 2010 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12 | A predictive ligand-based Bayesian model for human drug-induced liver injury. |
AID286866 | Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1160939 | Effective permeability of the compound at pH 4 by PAMPA | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
AID286893 | Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 2 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID592681 | Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | QSAR-based permeability model for drug-like compounds. |
AID1185532 | Anticonvulsant activity in Kunming mouse assessed as protection against sc-PTZ-induced tonic seizures 50 mg/kg, sc administered 30 mins before PTZ injection | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID682350 | Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 300 mg/kg, ip after 0.5 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID351285 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against 3 mercaptopropionic acid-induced seizures administered before 30 mins of 3 mercaptopropionic acid induction measured after 1 hr | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID226701 | Protective index was measured as TD50/ED50 in rat on oral administration | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID112536 | yohimbine induced seizures by administrating sc and the compound which do not exhibit at least one clonic seizure within 60 min was recorded; Percentage of protection at 100 mg/kg per os. | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID1220556 | Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1755097 | Solubility in PBS buffer at pH 7.4 | 2021 | Bioorganic & medicinal chemistry letters, 09-01, Volume: 47 | Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives. |
AID1229794 | Inhibition of [3H]BTX binding to sodium channel site 2 in rat cerebral cortex synaptosomes at 1 uM incubated for 60 mins by scintillation counting based radioligand displacement assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides. |
AID1676757 | Solubility in pH 7.4 PBS buffer at 50 to 150 uM incubated for 18 hrs by UV-vis spectrophotometry | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4- |
AID1193495 | Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1217729 | Intrinsic clearance for reactive metabolites formation assessed as summation of [3H]GSH adduct formation rate-based reactive metabolites formation and cytochrome P450 (unknown origin) inactivation rate-based reactive metabolites formation | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID384086 | Anticonvulsant activity in CF1 albino mouse assessed as prevention of maximal electroshock-induced seizures at 300 mg/kg, ip after 4 hrs | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline. |
AID481439 | Absolute bioavailability in human | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID496020 | Plasma protein binding in human after 30 min by ultrafiltration | 2010 | Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2 | SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro. |
AID1720877 | Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for anticonvulsant activity in mouse assessed as protection against 50 mA current-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID352392 | Anticonvulsant activity in albino CF1 mouse assessed as minimum inhibition of maximal electroshock-induced seizure in half or more of mouse at 300 mg/kg, ip after 4 hrs by MES test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles. |
AID679942 | TP_TRANSPORTER: inhibition of Rhodamine 123 efflux (R123: 1.5 ug/mL, Carbamazepine: 100 uM) in human lymphocytes | 2001 | British journal of clinical pharmacology, Apr, Volume: 51, Issue:4 | Carbamazepine is not a substrate for P-glycoprotein. |
AID256139 | Number of rats protected at a dose of 30 mg/Kg when given oral at 2 hr upon maximal electroshock seizure; Total number of rats = 4; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID1079936 | Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source] | |||
AID112456 | Anticonvulsant potency using the maximal electroshock test in mice | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
AID226543 | Protective index value is the ratio between TD50 and ED50 values. | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID1720862 | Anticonvulsant activity in ip injected albino mouse assessed as protection against 50 mA current-induced seizure after 0.5 to 4 hrs interval by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID481715 | Protective index, ratio of TD50 for po dosed mouse to ED50 for maximum electric stimulus-induced seizure in po dosed mouse | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID1215125 | Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktail after 5 hrs by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID351287 | Neurotoxicity in C57B/6 mouse assessed as inability to maintain equilibrium on 1-in diameter rod for 1 min after 30 mins by rotarod test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID114014 | Effective dose for anticonvulsant activity determined in mice using MES test procedure. (Phase II) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID112460 | Compound was tested for anticonvulsant potency using the STRY (strychnine) test in mice upon peroral administration | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
AID684370 | Anticonvulsant activity in ip dosed Sprague-Dawley albino rat assessed as protection against pilocarpine-induced status epilepticus after 0.5 hrs | 2012 | Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6 | Syntheses and evaluation of anticonvulsant activity of novel branched alkyl carbamates. |
AID678713 | Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID603472 | Antiallodynic activity in Wistar albino rat chronic constriction injury-induced neuropathic pain model assessed as attenuation of mechanical allodynia measured as paw withdrawal latency at 100 mg/kg, ip | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Discovery of molecules for the treatment of neuropathic pain: synthesis, antiallodynic and antihyperalgesic activities of 5-(4-nitrophenyl)furoic-2-acid hydrazones. |
AID178049 | Inhibition of hind limb tonus was tested by maximal electroshock test (MES) in rat after 4 hr of peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID351011 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against pentylenetetrazole-induced clonic seizure administered 30 mins before pentylenetetrazole challenge measured after 30 mins | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID1809053 | Oral bioavailability in human | 2021 | Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15 | Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR. |
AID420787 | Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM | 2009 | European journal of medicinal chemistry, Jun, Volume: 44, Issue:6 | Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors. |
AID231431 | Protective index, ratio of ED50 ataxia and ED50 MES | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID113857 | Effective dose against convulsions induced by maximal electroshock (MES) after intraperitoneal administration in experiment 2 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID433896 | Toxicity in Kunming mouse assessed as isoniazid-induced lethality at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID121852 | Compound was tested for toxicity after intraperitoneal injection into mice by using neurotoxicity screen test after 0.25 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID351282 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against pentylenetetrazole-induced seizures administered before 30 mins of pentylenetetrazole induction | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID1336191 | Anticonvulsant activity in ip dosed maximal electroshock induced seizure mouse model | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID709894 | Drug metabolism in human liver microsomes assessed as compound turnover at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID418136 | Toxicity in po dosed rat assessed as minimal muscular or neurological impairment by rotarod paradigm test | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID1079934 | Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source] | |||
AID24183 | Distribution coefficient in octanol/water at pH 5.5 | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. |
AID624608 | Specific activity of expressed human recombinant UGT1A4 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID113856 | Effective dose against convulsions induced by maximal electroshock (MES) after intraperitoneal administration in experiment 1 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID1210069 | Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1 | Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors. |
AID1215122 | Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID1899543 | Permeability of compound by PAMPA-BBB assay | 2022 | European journal of medicinal chemistry, Jan-15, Volume: 228 | Imidazolylacetophenone oxime-based multifunctional neuroprotective agents: Discovery and structure-activity relationships. |
AID588217 | FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID489288 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID449305 | Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of subcutaneous pentylenetetrazole-induced seizure after 0.5 hrs | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID693327 | Protective index, ratio of TD50 for mouse to ED50 for anticonvulsant activity in mouse by subcutaneous pentylenetetrazol-induced seizure test | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID1246319 | Apparent permeability from basolateral to apical side in human Caco2 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID351010 | Protective index, ratio of TD50 for neurotoxicity in C57B/6 mouse to ED50 for anticonvulsant activity in C57B/6 mouse | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID286876 | Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr, ip | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID481698 | Neurotoxicity against ip dosed mouse by rotarod ataxia test | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID490621 | Anticonvulsant activity in mouse assessed as 3-mercaptopropionic acid-induced death at 30 mg/kg, ip administered 30 mins before 3-mercaptopropionic acid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID109721 | Anticonvulsant activity after intraperitoneal injection into mice by using scPTZ screen test after 4 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1217707 | Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID351015 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against isoniazid-induced tonic seizure administered 30 mins before isoniazide challenge measured after 1 hrs | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID363534 | Toxicity in pentylenetetrazole-induced seizure C57B/6 mouse model assessed as lethality at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID682318 | Neurotoxicity in mouse assessed as motor impairment at 30 mg/kg, ip after 4 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID1160937 | Aqueous solubility of the compound at pH 4 | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
AID625290 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID226700 | Protective index was measured as TD50/ED50 | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID114623 | Evaluated for Bicuculline-induced seizures (anticonvulsant activity) when administered orally in mice. | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1191599 | Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in clonic seizures after 4 hrs by subcutaneous pentylenetetrazole seizure test | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents. |
AID286863 | Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID588220 | Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset | 2008 | Toxicology mechanisms and methods, , Volume: 18, Issue:2-3 | Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models. |
AID625292 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID727992 | Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against maximal-electric shock-induced seizures after 4 hrs | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID256408 | Minimum dose required for anticonvulsant activity when given i.p., at 0.5 hr in mice upon subcutaneous pentylenetetrazole seizure | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID1517334 | Inhibition of human LDH5 assessed as remaining activity at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID178294 | Anticonvulsant activity was measured by maximal electroshock seizure test in rat by po administration | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID1265492 | Anticonvulsant activity in ip dosed albino Carworth Farms No.1 mouse assessed as protection against maximal electroshock-induced seizures after 0.25 hrs | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID170484 | Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 0.25 hr; Compound was not screened | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID255720 | Anticonvulsant activity of compound expressed in terms of median effective dose (ED50) produced after ScMet test in mouse by i.p. administration | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines. |
AID1220555 | Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1264986 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as reduction of maximal electroshock-induced seizure | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents. |
AID1360444 | Binding affinity to human serum albumin assessed as fraction unbound after 4 hrs by LC-MS method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study. |
AID1470584 | Anticonvulsant activity in ip dosed maximal electroshock induced seizure mouse model assessed as suppression of hind limb tonic extension measured at 4 hrs post dose | 2017 | European journal of medicinal chemistry, May-26, Volume: 132 | Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review. |
AID1660934 | Permeability of the compound assessed as drug level in donor plate at 200 uM measured after 5 hrs at pH 7.4 by PAMPA | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays. |
AID1772563 | Apparent permeability of the compound across apical side to basolateral side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives. |
AID286862 | Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID727852 | Antiepileptic activity in Wistar rat assessed as protection against scSTY-induced seizures at 300 mg/kg, ip measured after 4 hrs | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID1336220 | Protection index, ratio of TD50 for neurotoxicity in po dosed Sprague-Dawley rat model to ED50 for po dosed pentylenetetrazole induced seizure Sprague-Dawley rat model | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID1304304 | Displacement of [3H]D888 from L-type calcium channel verapamil binding site in rat cerebral cortex synaptoneurosomes at 100 uM measured after 120 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID123952 | Locomotor activity in maximal electroshock seizure+ indicates increase at 100 mg/kg | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID231425 | Protective index was calculated (TD50/ED50) in MES assay in rat after oral administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID588213 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID231263 | Protective index was calculated (TD50/ED50) in MES assay in mice after intraperitoneal administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID205274 | In vitro inhibition of [3H]-BTX-B binding to sodium channels in rat brain synapto-neurosomes | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel. |
AID286883 | Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 2 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1705558 | Drug metabolism in rat liver microsomes at 10 uM preincubated with microsomes followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction. |
AID1154495 | Passive transcellular permeability of the compound at pH 7.4 by PAMPA | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Antileishmanial activity of a series of N²,N⁴-disubstituted quinazoline-2,4-diamines. |
AID682356 | Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 100 mg/kg, ip after 4 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID608519 | Anticonvulsant activity against maximal electric shock-induced seizures in ip dosed Kunming mouse assessed as median effective dose | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID361980 | Membrane permeability assessed as passive transport after 4 hrs by PAMPA | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID176420 | Minimal motor impairment activity by Rotarod test in rat following p.o. administration. | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID467613 | Volume of distribution at steady state in human | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID588215 | FDA HLAED, alkaline phosphatase increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID131776 | Tested for inhibition of 3-mercaptopropanoic acid induced seizures in mice. | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. |
AID286878 | Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs, ip | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID364295 | Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID489793 | Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Combating oxidative stress in epilepsy: design, synthesis, quantum chemical studies and anticonvulsant evaluation of 1-(substituted benzylidene/ethylidene)-4-(naphthalen-1-yl)semicarbazides. |
AID679256 | TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells | 2001 | British journal of clinical pharmacology, Apr, Volume: 51, Issue:4 | Carbamazepine is not a substrate for P-glycoprotein. |
AID433895 | Anticonvulsant activity against isoniazid-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID453203 | Lipophilicity, log D of the compound | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay. |
AID178048 | Inhibition of hind limb tonus was tested by maximal electroshock test (MES) in rat after 1 hr of peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID1065323 | Anticonvulsant activity in po dosed albino rat assessed as protection against maximal electroshock-induced seizures after 1 hr | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID481703 | Anticonvulsant activity in mouse assessed as inhibition of PTZ-induced tonic seizure at 50 mg/kg, ip administered 30 mins prior to PTZ challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID119692 | Protective index, ratio of ED50 ataxia and ED50 MES | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID136273 | Tested for the neurotoxicity in mouse rotarod test was reported 1 hr after po dosing | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines. |
AID176423 | Muscle-relaxant action in vertical screen method. | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants. |
AID29811 | Oral bioavailability in human | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1571367 | Anticonvulsant activity in po dosed Sprague-Dawley rat model of maximal electroshock-induced seizure assessed as suppression of tonic hind limb extension | |||
AID1336211 | Anticonvulsant activity in po dosed pentylenetetrazole induced seizure Sprague-Dawley rat model assessed as no observable episode of clonic convulsion of at least 5 secs | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID1079937 | Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source] | |||
AID481699 | Protective index, ratio of TD50 for ip dosed mouse to ED50 for maximum electric stimulus-induced seizure in ip dosed mouse | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID545529 | Toxicity against ip dosed mouse | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives. |
AID624612 | Specific activity of expressed human recombinant UGT1A9 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID709891 | Stability in human liver microsomes assessed as dioxygenated metabolite formation at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID588218 | FDA HLAED, lactate dehydrogenase (LDH) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID361979 | Membrane permeability by PAMPA | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID1220560 | Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1335444 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 0.5 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID27575 | HPLC capacity factor (k) | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | ElogPoct: a tool for lipophilicity determination in drug discovery. |
AID678722 | Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID363542 | Anticonvulsant activity in C57B/6 mouse assessed as inhibition of strychnine-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID139326 | Time of peak effect activity against maximal electroshock induced seizures | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID167920 | Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 4 hr; Compound was not screened | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID135325 | Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID1720880 | Neurotoxicity in ip and po injected mouse | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID232413 | Relative affinity for inactivated and resting human SkM1 expressed in HEK293 cells | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | 3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers. |
AID693318 | Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizures | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID540235 | Phospholipidosis-negative literature compound | |||
AID1473738 | Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID226542 | Protective index value is the ratio between ED50 and TD50 | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID255708 | Neurotoxicity expressed as median toxic dose (TD50) produced after Rotarod ataxia test in mouse by i.p. administration (range 45.9-135) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines. |
AID286884 | Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 2.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID7812 | In vitro rate of absorption observed as Caco-2 permeability in humans | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1264982 | Neurotoxicity in ip dosed Swiss albino mouse assessed as inability of animal to maintain equilibrium on rod after 0.5 hrs by rotarod test | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents. |
AID112461 | Anticonvulsant potency using the intravenous-BIC (bicuculline) test in mice | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
AID681167 | TP_TRANSPORTER: Northern blot from LS174T cell | 2001 | The Journal of biological chemistry, May-04, Volume: 276, Issue:18 | Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. |
AID109725 | Compound was tested for toxicity after intraperitoneal injection into mice by using toxicity screen test after 4 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID394946 | Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum drug concentration required for falling off the rotarod by half or more of mouse after 4 hrs by rotarod test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants. |
AID382366 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of maximal electroshock-induced seizures after 0.5 hrs | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID682345 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 4 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID1720883 | Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for anticonvulsant activity in mouse assessed as protection against current-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID1720885 | Neurotoxicity in KunMing mouse after 30 mins by rotarod test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID491236 | Permeability in buffer of pH 7.4 by PAMPA | 2010 | Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13 | Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway. |
AID129975 | Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse maximal electroshock seizures (MES) at time of peak effect after ip administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID727991 | Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against scPTZ-induced seizures after 0.5 hrs | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID1079945 | Animal toxicity known. [column 'TOXIC' in source] | |||
AID114017 | Effective dose for anticonvulsant activity determined in mice using subcutaneous Met test procedure. (Phase II); Potentiates | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID15711 | Calculated partition coefficient (clogP) | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. |
AID212211 | Toxicity using neurological impairment measured by rotarod test in mice | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
AID608533 | Anticonvulsant activity in Kunming mouse assessed as inhibition of bicuculline-induced death at 30 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1720889 | Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for anticonvulsant activity in mouse assessed as protection against pentylenetetrazole-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID1064727 | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Carbamazepine derivatives with P2X4 receptor-blocking activity. |
AID462612 | Permeability across artificial membrane assessed as compound transport at 200 uM after 4 hrs by PAMPA using HPLC/MS method | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID1895157 | Permeability in PBS buffer measured after 18 hrs by PAMPA based LC-MS analysis | 2021 | Journal of medicinal chemistry, 06-24, Volume: 64, Issue:12 | Interplay among Conformation, Intramolecular Hydrogen Bonds, and Chameleonicity in the Membrane Permeability and Cyclophilin A Binding of Macrocyclic Peptide Cyclosporin O Derivatives. |
AID477728 | Protective index, ratio of TD50 for neurotoxicity in Swiss albino mouse to ED50 for inhibition of PTZ-induced motor impairment Swiss albino mouse | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. |
AID666675 | Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against maximal electroshock-induced seizures | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives. |
AID1209393 | AUC(0 to 7 hrs) in Sprague-Dawley rat cerebrospinal fluid at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID134732 | Median lethal dose was measured after 24 hr | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID1517278 | Neurotoxicity against ip dosed Kunming mouse assessed as time remained in rod measured at 0.5 hrs by rotarod test | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID286868 | Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1742412 | Neurotoxicity in ip dosed Kunming mouse measured after 30 mins by rotarod test | |||
AID286895 | Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID590662 | Anticonvulsant activity in ip dosed Swiss mouse assessed as protection against maximal electroshock-induced seizures after 30 mins | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-one derivatives. |
AID1517274 | Anticonvulsant activity in ip dosed Kunming mouse assessed as MES-induced hind limb extension administered 0.5 hrs before MES stimulation | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1335459 | Neurotoxicity in Swiss albino mouse at 100 mg/kg, ip after 4 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID1193496 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID608433 | Anticonvulsant activity in Kunming mouse assessed as inhibition of isoniazid-induced clonic seizures at 50 mg/kg, ip after 1 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID27580 | Partition coefficient (logP) | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | ElogPoct: a tool for lipophilicity determination in drug discovery. |
AID608531 | Anticonvulsant activity in Kunming mouse assessed as inhibition of bicuculline-induced clonic seizures at 30 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID490626 | Anticonvulsant activity in mouse assessed as bicuculline-induced tonic seizures at 30 mg/kg, ip administered 30 mins before bicuculline challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID608431 | Anticonvulsant activity in Kunming mouse assessed as inhibition of isoniazid-induced death at 50 mg/kg, ip after 1 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1335445 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 0.5 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID394935 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as minimum drug concentration required for inhibition of maximal electroshock-induced seizure in half or more of mouse after 4 hrs by MES test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants. |
AID217796 | In vitro inhibition of Voltage-gated sodium channel by the displacement of [3H]batrachotoxin A 20-alpha-benzoate in rat brain cerebral cortex synaptoneurosomes | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. |
AID489277 | Anticonvulsant activity against subcutaneous strychnine-induced seizures in Wistar rat at 300 mg/kg, ip after 4 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID217926 | Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2 | Medicinal chemistry of neuronal voltage-gated sodium channel blockers. |
AID130890 | Inhibition of hind limb tonus was tested by maximal electroshock test (MES) in mouse after 1 hr of peroral administration of compound | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID693326 | Protective index, ratio of TD50 for mouse to ED50 for anticonvulsant activity in mouse by maximal electroshock-seizure test | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID1636357 | Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1544808 | Anticonvulsant activity in ip dosed albino mouse model of subcutaneous pentylenetetrazole-induced seizure assessed as failure to observe even a single episode of clonic spasms for at least 5 secs pretreated for 4 hrs followed by pentylenetetrazole inducti | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation. |
AID212543 | The compound was tested for the toxic dose on oral administration | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID608532 | Anticonvulsant activity in Kunming mouse assessed as inhibition of bicuculline-induced tonic seizures at 30 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID608436 | Anticonvulsant activity in Kunming mouse assessed as inhibition of subcutaneous pentylenetetrazol-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID481441 | Aqueous diffusivity at 37C | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID1215124 | Binding affinity to Wistar rat brain lipid assessed as percentage unbound by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID474786 | Membrane permeability at 10 uM at pH 7.4 by PAMPA method | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones. |
AID1210066 | Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2 | Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy. |
AID681116 | TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells | 2002 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3 | Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. |
AID608518 | Neurotoxicity in ip dosed Kunming mouse by rotarod test | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1129361 | Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | A high-throughput cell-based method to predict the unbound drug fraction in the brain. |
AID1473741 | Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID625286 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID344483 | Neurotoxicity in CF1 albino mouse after 4 hrs by rotarod test | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID588216 | FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID1193492 | Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID481701 | Ratio of HD50 for hypnotic activity to EC50 for inhibition of maximum electric stimulus-induced seizure in mouse | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID1720863 | Neurotoxicity in ip injected albino mouse | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID1753899 | Passive membrane permeability of the compound in phosphate buffered saline assessed as mass retention of the compound at 200 uM incubated for 5 hrs by PAMPA assay based HPLC analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture. |
AID433890 | Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID608427 | Anticonvulsant activity in Kunming mouse assessed as inhibition of thiosemicarbazide-induced clonic seizures at 30 mg/kg, ip after 2.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID481704 | Anticonvulsant activity in mouse assessed as reduction of PTZ-induced lethality at 50 mg/kg, ip administered 30 mins prior to PTZ challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID1194717 | Solubility in pH 7.4 buffer after 18 hrs by UV spectroscopy based microSol assay | 2015 | Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9 | Improving both aqueous solubility and anti-cancer activity by assessing progressive lead optimization libraries. |
AID109717 | Anticonvulsant activity after intraperitoneal injection into mice by using MES screen test after 0.25 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID693313 | Anticonvulsant activity in ip dosed mouse assessed as compound concentration causing protection against subcutaneous pentylenetetrazol-induced seizures in half or more test animals after 4 hrs | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID195317 | Compound was tested for anticonvulsant activity against MES-induced seizures in rat | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID433892 | Toxicity in Kunming mouse assessed as subcutaneous pentylenetetrazole-induced lethality at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID678715 | Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1217728 | Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1251236 | Anticonvulsant activity in ip-dosed mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizure | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | Discovery of benzothiazine derivatives as novel, orally-active anti-epileptic drug candidates with broad anticonvulsant effect. |
AID223434 | Effective dose was measured in mouse by maximal electroshock method by ip administration | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Synthesis and CLOGP correlation of imidooxy anticonvulsants. |
AID128992 | Anticonvulsant activity in mice(induced by maximal electroshock )after 0.25 hr of administration, for Phase-II screening | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel. |
AID194784 | Percent inhibition of 22Na+ uptake by voltage sensitive sodium channel of rat cortical synaptosomes at 300 uM | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID682342 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 0.5 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID177085 | Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in rat maximal metrazole seizures (MMS) after peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID1265488 | Neurotoxicity in ip dosed albino Carworth Farms No.1 mouse after 0.25 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID178031 | Effective dose for anticonvulsant activity determined in rats using subcutaneous Met test procedure. (Phase VIA); No protection | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID1605379 | Binding affinity to immobilized human Frizzled-7 CRD (Q33 to G173 resideus) transfected with pDisplay_BirA-ER plasmid in HEK293T cells for biotinylation by surface plasmon resonance assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8. |
AID590661 | Anticonvulsant activity in ip dosed Swiss mouse assessed as protection against maximal electroshock-induced seizures administered 30 mins before electroshock challenge measured after 30 mins | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-one derivatives. |
AID481716 | Neurotoxicity against po dosed mouse by rotarod ataxia test | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID490617 | Anticonvulsant activity in mouse assessed as isoniazid-induced tonic seizures at 30 mg/kg, ip administered 30 mins before isoniazid challenge measured after 1 hr | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID709904 | Drug metabolism in Wistar rat hepatocytes assessed as ratio of N-glucuronide metabolite level to parent compound level at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID314412 | Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assay | 2008 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5 | Imidazopyridines: a novel class of hNav1.7 channel blockers. |
AID1185525 | Toxicity in ip dosed Kunming mouse assessed as inability of animal to maintain equilibrium on rod for at least 1 min in each trial by rotarod test | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID1079939 | Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source] | |||
AID625287 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1571343 | Neurotoxicity in ip dosed CF-1 mouse by rotarod test | |||
AID489795 | Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause impair in motor coordination after 0.5 hrs by rotarod test | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Combating oxidative stress in epilepsy: design, synthesis, quantum chemical studies and anticonvulsant evaluation of 1-(substituted benzylidene/ethylidene)-4-(naphthalen-1-yl)semicarbazides. |
AID590664 | Protective index, ratio of TD50 for Swiss mouse to ED50 for Swiss mouse by maximal electroshock-induced seizures test | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-one derivatives. |
AID628633 | Neurotoxicity in ip dosed CF1 albino mouse assessed as minimum dose required to cause motor impairment after 4 hrs by rotarod test | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs. |
AID1636440 | Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1449628 | Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12 | Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification. |
AID699539 | Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID7974 | Metabolic stability observed at 30 min after administration in human liver microsomes | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1065338 | Neurotoxicity in ip dosed albino mouse after 0.5 hrs by rotorod test | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID608426 | Anticonvulsant activity in Kunming mouse assessed as inhibition of thiosemicarbazide-induced tonic seizures at 30 mg/kg, ip after 2.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID545526 | Protective index, ratio of TD50 for mouse to ED50 for inhibition of subcutaneous pentylenetetrazole-induced seizure in mouse | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives. |
AID28924 | Effective permeability (Pe) across a hexadecane membrane (pH 6.8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID132473 | The compound was tested for anticonvulsant activity against (subcutaneous administered) bicuculline induced seizures after intraperitoneal administration; Protected at 100 mg/ kg | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID481442 | Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID128999 | Anticonvulsant activity in mice, (induced by subcutaneous administration of Metrazol.) after 0.25 hr of administration, for Phase-II screening; Inactive | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel. |
AID1742400 | Anticonvulsant activity in Kunming mouse assessed as reduction in MES-induced seizure at 30 mg/kg, ip measured after 30 mins | |||
AID637074 | Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizure | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones. |
AID1336218 | Protection index, ratio of TD50 for neurotoxicity in po dosed Sprague-Dawley rat model to ED50 for po dosed maximal electroshock induced seizure Sprague-Dawley rat model | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID128129 | Ability to block seizures induced by bicuculline after intraperitoneal administration; NA indicates not active | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents. |
AID1195112 | Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse assessed as time to peak effect after 2 hrs by subcutaneous pentylenetetrazole test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
AID1173470 | Anticonvulsant activity against ip dosed CF1 albino mouse seizure model after 4 hrs by 6 Hz psychomotor seizure test | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23 | Seizure prevention by the naturally occurring phenols, carvacrol and thymol in a partial seizure-psychomotor model. |
AID727850 | Neurotoxicity against ip dosed Swiss albino mouse after 0.5 hrs by rotarod test | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID286897 | Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 1.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1304303 | Displacement of [3H]nitrendipine from L-type calcium channel dihydropyridine site in rat cerebral cortex synaptoneurosomes at 200 uM measured after 90 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID496828 | Antimicrobial activity against Leishmania donovani | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1335457 | Neurotoxicity in Swiss albino mouse at 300 mg/kg, ip after 0.5 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID433888 | Neurotoxicity in ip dosed Kunming mouse by rotarod test | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID1195111 | Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse assessed as time to peak effect by maximal electroshock test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
AID286880 | Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID196513 | t max for anticonvulsant activity was tested in rats intraperitoneally | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID114622 | Evaluated for Bicuculline-induced lethality (anticonvulsant activity) when administered orally in mice. | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1474167 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID255434 | Minimum dose required for anticonvulsant activity when given i.p., at 0.5 hr in mice upon neurotoxicity seizure using rotarod test | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID128174 | Anticonvulsant activity in mouse maximal electroshock seizure test following i.p. administration. | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents. |
AID53026 | Compound was evaluated for effective dose by maximal electroshock test after intraperitoneal administration of the compound. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and anticonvulsant activity of imidooxy derivatives. |
AID1519638 | Neurotoxicity in ip dosed CF-1 mouse assessed as reduction in equilibrium measured after 30 mins by rotarod test | |||
AID1742405 | Neurotoxicity in Kunming mouse at 30 mg/kg, ip measured after 30 mins by rotarod test | |||
AID1605380 | Binding affinity to immobilized mouse C-terminal Rhinovirus 3C cleavage site-fused 6xHis-tagged Frizzled-8 CRD (Q33 to G173 resideus) transfected with pDisplay_BirA-ER plasmid in HEK293T cells for biotinylation by surface plasmon resonance assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8. |
AID1229792 | Inhibition of [3H]BTX binding to sodium channel site 2 in rat cerebral cortex synaptosomes at 100 uM incubated for 60 mins by scintillation counting based radioligand displacement assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides. |
AID1519637 | Anticonvulsant activity in ip dosed CF-1 mouse assessed as reduction in ScPTZ-induced seizure administered before 30 mins of ScPTZ stimulation | |||
AID496817 | Antimicrobial activity against Trypanosoma cruzi | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID576612 | Inhibition of human ERG | 2011 | European journal of medicinal chemistry, Feb, Volume: 46, Issue:2 | Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model. |
AID361982 | Membrane permeability assessed as passive transport after 4 hrs by PAMPA in presence of 20% 1-propanol | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID363527 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as inhibition of maximal electroshock-induced seizures | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID221081 | Therapeutic dosage was measured by ip administration in mice | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Synthesis and CLOGP correlation of imidooxy anticonvulsants. |
AID496825 | Antimicrobial activity against Leishmania mexicana | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1336192 | Anticonvulsant activity in ip dosed pentylenetetrazole induced seizure mouse model | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID699540 | Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID177579 | Ability to suppress PTZ (pentylenetetrazole) induced clonic convulsions seizures in male Wistar rats | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants. |
AID490622 | Anticonvulsant activity in mouse assessed as thiosemicarbazide-induced clonic seizures at 30 mg/kg, ip administered 30 mins before thiosemicarbazide challenge measured after 2.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID136272 | Rotarod toxicity test for the compound in Phase-II screening was determined | 1988 | Journal of medicinal chemistry, Nov, Volume: 31, Issue:11 | Anticonvulsant activities of phenyl-substituted bicyclic 2,4-oxazolidinediones and monocyclic models. Comparison with binding to the neuronal voltage-dependent sodium channel. |
AID679895 | TP_TRANSPORTER: inhibition of cyclosporin A transcellular transport by carbamazapine 224 uM in MDR1-expressing LLC-PK1 cells | 2007 | Neuropharmacology, Feb, Volume: 52, Issue:2 | Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. |
AID1220558 | Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1079948 | Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source] | |||
AID286885 | Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID632994 | Neurotoxicity in po dosed rat assessed as neurological deficit by rotarod test | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID1065213 | Permeability coefficient, log Pe of the compound at pH 7.4 by PAMPA | 2014 | ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2 | Development of novel Vitamin D Receptor-Coactivator Inhibitors. |
AID351284 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against thiosemicarbazide-induced seizures administered before 30 mins of thiosemicarbazide induction measured after 1 hr | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID131218 | Maximal metrazole seizures was determined for the inhibition of hind limb tonus in mouse 1 hr after po dosing | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines. |
AID1215121 | Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID679123 | TP_TRANSPORTER: transcellular transport in mdr1a-expressing LLC-PK1 cells | 2007 | Neuropharmacology, Feb, Volume: 52, Issue:2 | Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. |
AID43581 | Inhibition of beta-lactamase at 100 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
AID1709683 | Anticonvulsant activity in mouse by measuring free brain concentration | 2021 | ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4 | Discovery of the First Orally Available, Selective K |
AID1335451 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 300 mg/kg, ip after 0.5 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID382370 | Neurotoxicity in ip dosed mouse after 0.5 hrs by rotarod test | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID1519674 | Chromatographic hydrophobicity index of compound at 250 uM at pH 7.4 by HPLC analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies. |
AID19463 | Partition coefficient (logP) | 1999 | Journal of medicinal chemistry, May-06, Volume: 42, Issue:9 | Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel. |
AID1065320 | Protective index, ratio of TD50 for neurotoxicity to ED50 for protection against maximal electroshock-induced seizure in albino rat after 1 hr | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID286881 | Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 1 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1720860 | Anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure measured after 30 mins | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID588209 | Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset | 2010 | Chemical research in toxicology, Jul-19, Volume: 23, Issue:7 | Developing structure-activity relationships for the prediction of hepatotoxicity. |
AID490612 | Protective index, ratio of TD50 for mouse by rotarod test to ED50 for mouse by MES test | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID1193500 | Thermodynamic equilibrium solubility, log S of the compound | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID256412 | Minimum dose required for anticonvulsant activity when given i.p., at 2 hr in mice upon subcutaneous strychnine seizure; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID1544804 | Neurotoxicity in ip dosed albino mouse assessed as motor impairment measured at 4 hrs by rotarod test | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation. |
AID677694 | Permeability of the compound at pH 7.4 by PAMPA | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators. |
AID624606 | Specific activity of expressed human recombinant UGT1A1 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID395324 | Lipophilicity, log D at pH 7.4 by liquid chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID1336209 | Anticonvulsant activity in po dosed maximal electroshock induced seizure Sprague-Dawley rat model assessed as suppression in hindlimb tonic extension | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID666678 | Protective index, ratio of TD50 for neurotoxicity in Kunming mouse to ED50 for protection against MES-induced seizures in Kunming mouse | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives. |
AID210595 | Ratio of TD50/ED50; TI indicates Therapeutic index | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents. |
AID545525 | Protective index, ratio of TD50 for mouse to ED50 for inhibition of maximal electroshock-induced seizure in mouse | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives. |
AID286898 | Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 2 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1336195 | Protection index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for ip dosed pentylenetetrazole induced seizure mouse model | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID363546 | Toxicity in strychnine-induced seizure C57B/6 mouse model assessed as lethality at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID1217711 | Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID490615 | Anticonvulsant activity in mouse assessed as pentylenetetrazole-induced death at 30 mg/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID352566 | Anticonvulsant activity in albino CF1 mouse assessed as inhibition of pentylenetetrazole-induced seizures in half or more of mouse at 300 mg/kg, ip after 4 hrs by scPTZ test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles. |
AID305067 | Anticonvulsant activity against pentylenetetrazole-induced seizures in Albino mouse at 300 mg/kg, ip after 4 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain. |
AID314682 | Anticonvulsant activity in C57BL6J mouse assessed as prevention of shock-induced tonic-clonic seizures at 3 mg/kg, po after 30 mins | 2008 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6 | 3-Amino-1,5-benzodiazepinones: potent, state-dependent sodium channel blockers with anti-epileptic activity. |
AID625281 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID727853 | Antiepileptic activity in Wistar rat assessed as protection against scSTY-induced seizures at 300 mg/kg, ip measured after 0.5 hrs | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID1160933 | Aqueous solubility of the compound at pH 7.4 | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
AID481711 | Anticonvulsant activity in mouse assessed as inhibition of thiosemicarbazide-induced clonic seizure at 50 mg/kg, ip administered 30 mins prior to thiosemicarbazide challenge measured after 2.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID106806 | Inhibition of malate dehydrogenase (MDH) at 400 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
AID344488 | Hepatotoxicity in Sprague-Dawley rat assessed as presence of normal hepatic parenchyma with portal triad and central vein by histopathological study | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID496832 | Antimicrobial activity against Trypanosoma brucei rhodesiense | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1227822 | Kinetic solubility of the compound at pH 1.2 | 2015 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1 | Dibenzazepines and dibenzoxazepines as sodium channel blockers. |
AID1623669 | Apparent permeability of compound form apical to basolateral side in human Caco2 cells | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID637073 | Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against maximal electroshock-induced seizure | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones. |
AID212546 | Toxic dose determined in rats using MES test procedure. (Phase VIA) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID361981 | Membrane permeability by PAMPA in presence of 20% 1-propanol | 2008 | Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16 | Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries. |
AID1079938 | Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source] | |||
AID418134 | Anticonvulsant activity in po dosed rat assessed as protection against maximal electroshock-induced seizure | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID253080 | Inhibition of native TTX-R sodium currents in acutely dissociated rat dorsal root ganglion (DRG) | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors. |
AID496831 | Antimicrobial activity against Cryptosporidium parvum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID190113 | In vivo toxic dose in rotarod assay | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2 | Medicinal chemistry of neuronal voltage-gated sodium channel blockers. |
AID253081 | Inhibition of native TTX-S sodium currents in acutely dissociated rat dorsal root ganglion (DRG) | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors. |
AID205291 | Affinity for resting human SkM1 sodium channel expressed in HEK293 cells | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | 3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers. |
AID363544 | Anticonvulsant activity in C57B/6 mouse assessed as inhibition of strychnine-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID226526 | Protective index is the ratio between TD50 and ED50 values | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID1220554 | Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1209401 | AUC(0 to infinity) in Sprague-Dawley rat cerebrospinal fluid at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID489791 | Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Combating oxidative stress in epilepsy: design, synthesis, quantum chemical studies and anticonvulsant evaluation of 1-(substituted benzylidene/ethylidene)-4-(naphthalen-1-yl)semicarbazides. |
AID404304 | Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control | 2008 | Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11 | Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2). |
AID490614 | Anticonvulsant activity in mouse assessed as pentylenetetrazole-induced tonic seizures at 30 mg/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID47029 | Time of peak neurotoxic effect in CF1 mice | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID1246318 | Apparent permeability from apical to basolateral side in human Caco2 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID131995 | Median hypnotic dose by loss of righting reflex | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID28234 | % absorbed in human GI-tract | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID255468 | Minimum dose required for anticonvulsant activity when given i.p., at 0.5 hr in mice upon maximal electroshock seizure | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID490618 | Anticonvulsant activity in mouse assessed as isoniazid-induced death at 30 mg/kg, ip administered 30 mins before isoniazid challenge measured after 1 hr | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID114817 | Sedative properties by the rotarod test | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1217712 | Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID625285 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID637076 | Protective index, ratio of TD50 for ip dosed Kunming mouse to ED50 for ip dosed Kunming mouse by subcutaneous pentylenetetrazole induced seizure test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones. |
AID1742413 | Protection index, ratio of TD50 for neurotoxicity in ip dosed Kunming mouse to ED50 for anticonvulsant activity in ip dosed MES-induced Kunming mouse | |||
AID481702 | Anticonvulsant activity in mouse assessed as inhibition of PTZ-induced clonic seizure at 50 mg/kg, ip administered 30 mins prior to PTZ challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID131932 | Tested for inhibition of strychnine-induced seizures in mice. | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. |
AID29421 | Partition coefficient (logP) (HPLC) | 2000 | Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15 | ElogPoct: a tool for lipophilicity determination in drug discovery. |
AID608430 | Anticonvulsant activity in Kunming mouse assessed as inhibition of 3-mercaptopropionic acid-induced clonic seizures at 30 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1810294 | Aqueous solubility of compound at pH 2.4 | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1 |
AID364290 | Anticonvulsant activity in ip dosed mouse after 0.5 hrs by scPTZ test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID727993 | Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against maximal-electric shock-induced seizures after 0.5 hrs | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID344480 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 0.5 hrs by scPTZ test | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID305066 | Anticonvulsant activity against pentylenetetrazole-induced seizures in Albino mouse at 100 mg/kg, ip after 0.5 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain. |
AID179593 | In vitro inhibition of [3H]GABA uptake in rat Hippocampal slices. | 1992 | Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22 | Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake. |
AID1753897 | Passive membrane permeability of the compound in phosphate buffered saline assessed as concentration of the compound in donor plate at 200 uM incubated for 5 hrs by PAMPA assay based HPLC analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture. |
AID352568 | Neurotoxicity in ip dosed albino CF1 mouse assessed as minimum drug concentration required for motor impairment in half or more of mouse after 4 hrs by rotarod test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles. |
AID1215127 | Ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay to fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID1264988 | Protective index, ratio of TD50 for ip dosed Swiss albino mouse assessed as inability of animal to maintain equilibrium on rod after 0.5 hrs by rotarod test to ED50 for Swiss albino mouse assessed as reduction of maximal electroshock-induced seizure | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents. |
AID1473740 | Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID682320 | Neurotoxicity in mouse assessed as motor impairment at 300 mg/kg, ip after 4 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID432063 | Apparent permeability at pH 7.4 after 24 hrs by PAMPA method | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Determination of permeability and lipophilicity of pyrazolo-pyrimidine tyrosine kinase inhibitors and correlation with biological data. |
AID1261691 | Protein binding to human serum albumin at 0.5 to 1.5 mg/ml by HPLC method | 2015 | Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21 | Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo. |
AID590665 | Protective index, ratio of TD50 for Swiss mouse to ED50 for Swiss mouse by subcutaneous pentylenetetrazol-induced seizure test | 2011 | European journal of medicinal chemistry, Apr, Volume: 46, Issue:4 | Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-[1,2,4]triazolo[4,3-a][1]benzazepin-1-one derivatives. |
AID114575 | Tested for the abolition of the hand leg tonic extensor component of the seizure induced by a 0.96 mg/kg sc injection of strychnine | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID624640 | Drug glucuronidation reaction catalyzed by human recombinant UGT2B7 | 2005 | Pharmacology & therapeutics, Apr, Volume: 106, Issue:1 | UDP-glucuronosyltransferases and clinical drug-drug interactions. |
AID490624 | Anticonvulsant activity in mouse assessed as thiosemicarbazide-induced death at 30 mg/kg, ip administered 30 mins before thiosemicarbazide challenge measured after 2.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID1193498 | Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1065322 | Neurotoxicity in po dosed albino rat after 1 hr | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID1211297 | Drug recovery in plasma (unknown origin) | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID490613 | Anticonvulsant activity in mouse assessed as pentylenetetrazole-induced clonic seizures at 30 mg/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID1229793 | Inhibition of [3H]BTX binding to sodium channel site 2 in rat cerebral cortex synaptosomes at 10 uM incubated for 60 mins by scintillation counting based radioligand displacement assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides. |
AID395325 | Lipophilicity, log P by microemulsion electrokinetic chromatography | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID625284 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID226508 | Protection index = TD50/ED50 | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1195116 | Protective index, ratio of neurotoxic TD50 in Albino Swiss CD1 mouse by rotarod test to anticonvulsant ED50 in Albino Swiss CD1 mouse by maximal electroshock test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
AID727851 | Neurotoxicity against ip dosed Swiss albino mouse after 4 hrs by rotarod test | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID112455 | Compound was tested for anticonvulsant potency using the 3-MPA (3-mercaptopropionic acid) test in mice upon peroral administration | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
AID682316 | Neurotoxicity in mouse assessed as motor impairment at 100 mg/kg, ip after 0.5 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID445819 | CNS toxicity in albino mouse assessed as duration of immobility at 100 umol/kg, ip after 0.5 hrs by Porsolt's swimpool test (Rvb= 78 +/- 0.9) | 2010 | European journal of medicinal chemistry, Jan, Volume: 45, Issue:1 | Synthesis, anticonvulsant activity and 3D-QSAR study of some prop-2-eneamido and 1-acetyl-pyrazolin derivatives of aminobenzothiazole. |
AID129974 | Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse against maximal electroshock seizures (MES) after peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID1065321 | Anticonvulsant activity in po dosed albino rat assessed as protection against pentylenetetrazole-induced seizure after 1 hr | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID28925 | Highest effective permeability across hexadecane membrane (pH 4-8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID1742410 | Anticonvulsant activity in ip dosed Kunming mouse assessed as reduction in MES-induced seizure measured after 30 mins | |||
AID190132 | The cytotoxicity after intraperitoneal administration in rat | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID1335454 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 300 mg/kg, ip after 4 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID693319 | Anticonvulsant activity in ip dosed mouse assessed as compound concentration causing protection against subcutaneous pentylenetetrazol-induced seizures in half or more test animals after 0.5 hrs | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID433900 | Anticonvulsant activity against thiosemicarbazide-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 2.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID132652 | The effective dose of compound was tested against subcutaneous administered Metrazol induced seizures after intraperitoneal administration; Not effective | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID22951 | Time of peak effect (TPE) for toxicity | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and anticonvulsant activity of imidooxy derivatives. |
AID286888 | Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 2 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1517275 | Anticonvulsant activity in ip dosed Kunming mouse assessed as reduction in ScPTZ-induced seizure administered 0.5 hrs before ScPTZ stimulation | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1217727 | Intrinsic clearance for reactive metabolites formation per mg of protein in human liver microsomes based on [3H]GSH adduct formation rate at 100 uM by [3H]GSH trapping assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID588214 | FDA HLAED, liver enzyme composite activity | 2004 | Current drug discovery technologies, Dec, Volume: 1, Issue:4 | Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. |
AID539464 | Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. |
AID1079941 | Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source] | |||
AID489797 | Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause impair in motor coordination after 4 hrs by rotarod test | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Combating oxidative stress in epilepsy: design, synthesis, quantum chemical studies and anticonvulsant evaluation of 1-(substituted benzylidene/ethylidene)-4-(naphthalen-1-yl)semicarbazides. |
AID226523 | Protective index (rat) was from the ratio of plasma concentration at which side effects occur by plasma concentration at which anticonvulsant activity occur. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID481446 | Effective permeability across human jejunum | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID190459 | Anticonvulsant activity in corneal kindled rats was determined when 10 mg/kg was administered orally | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID344481 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 4 hrs by scPTZ test | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID1220557 | Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID1660933 | Permeability of the compound assessed as drug level in acceptor plate at 200 uM measured after 5 hrs at pH 7.4 by PAMPA | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays. |
AID28679 | Partition coefficient (logD6.8) | 2001 | Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6 | High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes. |
AID47026 | Time of peak anticonvulsant effect in CF1 mice | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID129293 | Antimaximal electroshock seizure activity was determined in mice when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
AID311935 | Partition coefficient, log P of the compound | 2008 | Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2 | Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model. |
AID40039 | Antagonist activity to generalized seizures Photically induced seizures in senegalese Papio papio baboons | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID121850 | Compound was tested for rotarod test in mice and TD50 value at which 50% of trained animals fall off rotarod | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID394939 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as minimum drug concentration required for inhibition of pentylenetetrazole-induced seizures in half or more of mouse after 4 hrs by scPTZ test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants. |
AID462615 | Apparent permeability in BBMEC assessed as compound transport after 2 hrs | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID161627 | Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells | 2003 | Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17 | Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein. |
AID418132 | Anticonvulsant activity in ip dosed mouse assessed as protection against subcutaneous metrazole-induced seizure | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID194783 | Percent inhibition of 22Na+ uptake by voltage sensitive sodium channel of rat cortical synaptosomes at 30 uM | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1335452 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 30 mg/kg, ip after 4 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID449310 | Antidepressant activity against Wistar rat assessed as increase in immobility time at 30 mg/kg, ip after 60 mins by forced swim pool method | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID490616 | Anticonvulsant activity in mouse assessed as isoniazid-induced clonic seizures at 30 mg/kg, ip administered 30 mins before isoniazid challenge measured after 1 hr | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID625288 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID384082 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as prevention of maximal electroshock-induced seizures after 0.5 hrs | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline. |
AID628728 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against subcutaneous pentylenetetrazole-induced after 4 hrs | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs. |
AID351286 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against strychnine-induced seizures administered before 30 mins of strychnine induction measured for 30 mins | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID1217710 | Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID170633 | Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 2 hr; Compound was not screened | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1079931 | Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source] | |||
AID394934 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as minimum drug concentration required for inhibition of maximal electroshock-induced seizure in half or more of mouse after 0.5 hrs by MES test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants. |
AID1720892 | Neurotoxicity in KunMing mouse by rotarod test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID633209 | Blockade of voltage-gated sodium channel in mouse N1E-115 cells assessed as stimulation at 100 umol at -90 mV holding potential by whole-cell patch clamp electrophysiological assay relative to control | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID190107 | Compound was tested for toxicity after oral administration in rat by using neurotoxicity screen test after 0.5 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID693322 | Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID196514 | t max was for the anticonvulsant effect was tested in rats administered by gastric tube; t max | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1193499 | Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID286890 | Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID433891 | Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID1544805 | Neurotoxicity in ip dosed albino mouse assessed as motor impairment measured at 0.5 hrs by rotarod test | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation. |
AID489787 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Combating oxidative stress in epilepsy: design, synthesis, quantum chemical studies and anticonvulsant evaluation of 1-(substituted benzylidene/ethylidene)-4-(naphthalen-1-yl)semicarbazides. |
AID197266 | In vivo anticonvulsant activity to prevent seizures from maximum electroshock (MES) in rat hippocampal slices | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2 | Medicinal chemistry of neuronal voltage-gated sodium channel blockers. |
AID496824 | Antimicrobial activity against Toxoplasma gondii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID625279 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID305070 | Neurotoxicity in Albino mouse at 300 mg/kg, ip after 4 hrs by rotarod test | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain. |
AID366586 | Protective index, ratio of TD50 for mouse by rotarod test to ED50 for mouse by MES test | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID1519639 | Protective index, ratio of TD50 for neurotoxicity in ip dosed CF-1 mouse to ED50 for anticonvulsant activity in ip dosed Kunming mouse | |||
AID132653 | The effective dose of compound was tested against subcutaneous administered Metrazol induced seizures in mice | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID19424 | Partition coefficient (logD7.4) | 2001 | Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15 | ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds. |
AID132645 | The effective dose of compound was tested against maximal electroshock induced seizures after intraperitoneal administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID481709 | Anticonvulsant activity in mouse assessed as inhibition of 3-mercaptopropionic acid-induced tonic seizure at 50 mg/kg, ip administered 30 mins prior to 3-mercaptopropionic acid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID24184 | Distribution coefficient in octanol/water at pH 6.5 | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. |
AID1304302 | Displacement of [3H]nitrendipine from L-type calcium channel dihydropyridine site in rat cerebral cortex synaptoneurosomes at 100 uM measured after 90 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID1772565 | Efflux ratio of apparent permeability in human Caco-2 cells | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives. |
AID19689 | Partition coefficient (logP) | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1079932 | Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source] | |||
AID286892 | Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 1.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1517280 | Protective index, ratio of TD50 for neurotoxicity against ip dosed Kunming mouse assessed as time remained in rod measured at 0.5 hrs by rotarod test to ED50 for anticonvulsant activity in ip dosed Kunming mouse assessed as reduction in ScPTZ-induced seiz | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID481700 | Sedative-hypnotic activity in mouse assessed as reduction in righting reflex | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID490619 | Anticonvulsant activity in mouse assessed as 3-mercaptopropionic acid-induced clonic seizures at 30 mg/kg, ip administered 30 mins before 3-mercaptopropionic acid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID1720886 | Protective index, ratio of TD50 for neurotoxicity in KunMing mouse to ED50 for anticonvulsant activity in KunMing mouse assessed as protection against 50 mA current-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID1079933 | Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is | |||
AID1185526 | Protective index, ratio of intraperitoneal neurotoxic TD50 against Kunming mouse by rotarod test to intraperitoneal anticonvulsant ED50 in Kunming mouse by MES test | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID180530 | The compound was tested for the effective oral dose to inhibit 50% of the anticonvulsant in rats. | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID1079944 | Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source] | |||
AID131925 | Tested for inhibition of pentylenetetrazole induced seizures in mice. | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. |
AID433897 | Anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID222384 | Protective index (TD50/ED50) value in MES test in mice | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Synthesis and CLOGP correlation of imidooxy anticonvulsants. |
AID363529 | Protective index, ratio of TD50 for C57B/6 mouse by rotarod test to ED50 for C57BL/6 mouse by MES test | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID666676 | Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against subcutaneous pentylenetetrazol-induced clonic seizures | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives. |
AID496823 | Antimicrobial activity against Trichomonas vaginalis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID249395 | Ratio between Kr to Ki | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors. |
AID682343 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 0.5 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID1079949 | Proposed mechanism(s) of liver damage. [column 'MEC' in source] | |||
AID1217713 | Time dependent inhibition of CYP3A4 (unknown origin) at 10 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1195115 | Neurological toxicity in intraperitoneally dosed Albino Swiss CD1 mouse by rotarod test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
AID1269481 | Displacement of [3H]Batrachotoxinin from sodium channel site 2 in rat cerebral cortex at 100 uM after 60 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones. |
AID603563 | Antiallodynic activity in Wistar albino rat chronic constriction injury-induced neuropathic pain model assessed as reversal of spontaneous pain response up to 1 hr at 100 mg/kg, ip | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Discovery of molecules for the treatment of neuropathic pain: synthesis, antiallodynic and antihyperalgesic activities of 5-(4-nitrophenyl)furoic-2-acid hydrazones. |
AID131914 | Tested for inhibition of maximal electroshock -induced seizures in mice; Value ranges from 13-25 | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. |
AID114873 | Effective dose required to inhibit ataxia after intraperitoneal administration in experiment 1 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID1220559 | Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Species independence in brain tissue binding using brain homogenates. |
AID682315 | Neurotoxicity in mouse assessed as motor impairment at 30 mg/kg, ip after 0.5 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID1058304 | Anticonvulsant activity in ip dosed Sprague-Dawley rat hippocampal kindling model assessed as suppression of seizure activity treated 15 for mins post suprathreshold-stimulation | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112). |
AID608429 | Anticonvulsant activity in Kunming mouse assessed as inhibition of 3-mercaptopropionic acid-induced tonic seizures at 30 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1623668 | Permeability of compound at pH 7.4 by PAMPA | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID490627 | Anticonvulsant activity in mouse assessed as bicuculline-induced death at 30 mg/kg, ip administered 30 mins before bicuculline challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID433899 | Anticonvulsant activity against thiosemicarbazide-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 2.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID366585 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed mouse | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID1584806 | Permeability of the compound at pH 7.4 by PAMPA | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents. |
AID1079947 | Comments (NB not yet translated). [column 'COMMENTAIRES' in source] | |||
AID113457 | Anticonvulsant activity against bicuculline induced seizures in mice; Percentage of protection at 100 mg/kg per os. | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID52790 | Inhibition of chymotrypsin at 250 uM | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Identification and prediction of promiscuous aggregating inhibitors among known drugs. |
AID1064724 | Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx at 100 uM preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay | 2014 | Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3 | Carbamazepine derivatives with P2X4 receptor-blocking activity. |
AID194782 | Percent inhibition of 22Na+ uptake by voltage sensitive sodium channel of rat cortical synaptosomes at 100 uM | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID231427 | Protective index was calculated (TD50/ED50) in scMET assay in mice after oral administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID114802 | Anticonvulsant activity in tonic seizures when administered orally in mice | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1720864 | Protective index, ratio of TD50 for neurotoxicity in ip injected albino mouse to ED50 for anticonvulsant activity in ip injected albino mouse assessed as protection against 50 mA current-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID496829 | Antimicrobial activity against Leishmania infantum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID132475 | The compound was tested for anticonvulsant activity against (subcutaneous administered) strychnine induced seizures after intraperitoneal administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID588208 | Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset | 2010 | Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5 | Predicting phospholipidosis using machine learning. |
AID433889 | Protective index, ratio of TD50 for neurotoxicity to ED50 for anticonvulsant activity in ip dosed Kunming mouse | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID382367 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of maximal electroshock-induced seizures after 4 hrs | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID699541 | Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting | 2012 | Journal of medicinal chemistry, May-24, Volume: 55, Issue:10 | Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. |
AID255438 | Protective index (TD50/ED50) produced by compound in mouse after MES test | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines. |
AID1336193 | Neurotoxicity in ip dosed mouse | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID136280 | The cytotoxicity after intraperitoneal administration in mice | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID305061 | Anticonvulsant activity against maximal electroshock-induced seizure in Albino mouse at 30 mg/kg, ip after 0.5 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain. |
AID1335460 | Neurotoxicity in Swiss albino mouse at 300 mg/kg, ip after 4 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID1519676 | Retention time of compound at pH 7.4 by LC-UV analysis | 2020 | European journal of medicinal chemistry, Jan-01, Volume: 185 | Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies. |
AID418133 | Toxicity in ip dosed mouse assessed as minimal muscular or neurological impairment by rotarod paradigm test | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID1772564 | Apparent permeability of the compound across basolateral side to apical side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis | 2021 | European journal of medicinal chemistry, Nov-05, Volume: 223 | Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives. |
AID217795 | Displacement of [3H]BTX from voltage-gated sodium channel of rat cortical synaptosomes | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID178027 | Effective dose for anticonvulsant activity determined in rats using MES test procedure. (Phase VIA) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID132471 | The compound was tested for anticonvulsant activity against (subcutaneous administered) Metrazol induced seizures after intraperitoneal administration; No protection up to 100 mg/kg | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID170612 | Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 0.5 hr; Compound was not screened | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID286889 | Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 2.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID679137 | TP_TRANSPORTER: transcellular transport in mdr1b-expressing LLC-PK1 cells | 2007 | Neuropharmacology, Feb, Volume: 52, Issue:2 | Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. |
AID625289 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1215128 | Ratio, ratio of fraction unbound in solid supported porcine brain membrane vesicles at 5 uM dosed as discrete compounds after 5 hrs by TRANSIL assay to fraction unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktai | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID156202 | Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans. |
AID490611 | Neurotoxicity in ip dosed mouse assessed as time spent on rotarod by rotarod test | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID489274 | Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause toxicity after 4 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID1209455 | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID244602 | Dissociation constant for binding to inactivated state of rat brain NaIIa (rNav1.2) -B2 cell line stably expressed in HEK293 Cells | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors. |
AID1335446 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 4 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID286870 | Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID678716 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID1605378 | Binding affinity to immobilized human Frizzled-5 CRD (P31 to Y150 resideus) transfected with pDisplay_BirA-ER plasmid in HEK293T cells for biotinylation by surface plasmon resonance assay | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8. |
AID212345 | Toxic dose determined in mice using MES test procedure. (Phase II) | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID112459 | Anticonvulsant potency using the PTX (picrotoxin) test in mice by peroral administration | 1998 | Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4 | Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives. |
AID1265486 | Anticonvulsant activity in po dosed Sprague-Dawley rat assessed as protection against subcutaneous dosed pentetrazol-induced seizures after 0.5 hrs | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID190586 | Anticonvulsant activity in corneal kindled rats was determined when 80 mg/kg was administered orally | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID632997 | Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for inhibition of maximal electroshock-induced seizures in mouse | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID481712 | Anticonvulsant activity in mouse assessed as inhibition of thiosemicarbazide-induced tonic seizure at 50 mg/kg, ip administered 30 mins prior to thiosemicarbazide challenge measured after 2.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID1720878 | Anticonvulsant activity in mouse assessed as protection against 50 mA current-induced seizure after 0.5 hrs by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID311524 | Oral bioavailability in human | 2007 | Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24 | Hologram QSAR model for the prediction of human oral bioavailability. |
AID628632 | Neurotoxicity in ip dosed CF1 albino mouse assessed as minimum dose required to cause motor impairment after 0.5 hrs by rotarod test | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs. |
AID682355 | Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 300 mg/kg, ip after 4 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID490623 | Anticonvulsant activity in mouse assessed as thiosemicarbazide-induced tonic seizures at 30 mg/kg, ip administered 30 mins before thiosemicarbazide challenge measured after 2.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID243422 | log (1/Km) value for human liver microsome cytochrome P450 3A4 | 2005 | Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18 | Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism. |
AID1079943 | Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source] | |||
AID1265487 | Anticonvulsant activity in po dosed Sprague-Dawley rat assessed as protection against maximal electroshock-induced seizures after 0.5 hrs | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID1246320 | Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID1720879 | Anticonvulsant activity in mouse assessed as protection against current-induced seizure by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID545527 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of maximum electric shock-induced hind limb tonic extension | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives. |
AID1209341 | Ratio of drug level in cerebrospinal fluid to unbound plasma concentration in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID185053 | Neuroprotective activity was determined in the rat middle cerebral artery occlusion (MCAO) model of focal stroke | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2 | Medicinal chemistry of neuronal voltage-gated sodium channel blockers. |
AID1209357 | Ratio of unbound drug level in brain to plasma in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID1138688 | Permeability of the compound at pH 4 by PAMPA | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines. |
AID678714 | Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID180909 | The effective dose of compound was tested against subcutaneous administered Metrazol induced seizures in rat; Not effective | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID121847 | Central nervous system toxicity was performed by determining the median toxic dose in the rotarod test | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID255467 | Minimum dose required for anticonvulsant activity when given i.p., at 4 hr in mice upon maximal electroshock seizure | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID28681 | Partition coefficient (logD6.5) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID433887 | Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against maximal electroshock-induced seizures | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID1227824 | Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 30 mins | 2015 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1 | Dibenzazepines and dibenzoxazepines as sodium channel blockers. |
AID112135 | Effective dose required to inhibit ataxia after intraperitoneal administration in experiment 2 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID1473739 | Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay | 2013 | Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1 | A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. |
AID286867 | Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID131217 | Maximal electroshock seizures was determined for the inhibition of hind limb tonus in mouse by 1 hr after po dose | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines. |
AID384090 | Neurotoxicity in ip dosed CF1 albino mouse after 4 hrs by rotarod test | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline. |
AID693325 | Neurotoxicity in ip dosed mouse after 30 mins by rotarod test | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID490620 | Anticonvulsant activity in mouse assessed as 3-mercaptopropionic acid-induced tonic seizures at 30 mg/kg, ip administered 30 mins before 3-mercaptopropionic acid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID678734 | TP_TRANSPORTER: inhibition of cyclosporin A transcellular transport by carbamazepine at a concentration of 224uM in mdr1a-expressing LLC-PK1 cells | 2007 | Neuropharmacology, Feb, Volume: 52, Issue:2 | Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. |
AID156204 | Binding to POPC/GMI liposomes using biosensor system | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans. |
AID977599 | Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
AID286865 | Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID608428 | Anticonvulsant activity in Kunming mouse assessed as inhibition of 3-mercaptopropionic acid-induced death at 30 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID588212 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID1211294 | Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID1079940 | Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source] | |||
AID217794 | Inhibition of [3H]BTX-B binding to neurotoxin site 2 of sodium channel of rat cerebral cortex synaptoneurosomes | 1995 | Journal of medicinal chemistry, Sep-29, Volume: 38, Issue:20 | Synthesis and anticonvulsant activity of enaminones. 3. Investigations on 4'-, 3'-, and 2'-substituted and polysubstituted anilino compounds, sodium channel binding studies, and toxicity evaluations. |
AID178176 | Compound was tested for anticonvulsant activity by maximal electroshock seizure(MES) test in rat upon intraperitoneal administration | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents. |
AID114634 | Anticonvulsant activity in Maximal electroshock (MES) when administered orally in mice | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1304301 | Displacement of [3H]diltiazem from L-type calcium channel diltiazem binding site in rat cerebral cortex synaptoneurosomes at 200 uM measured after 120 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID471592 | Anticonvulsant activity against electric stimulation-induced pharmacoresistant limbic epilepsy in Sprague-Dawley rat kindling model assessed as reduction of seizure severity and excitability at > 26 mg/kg, ip administered 15 mins after last electric stimu | 2009 | Journal of medicinal chemistry, Dec-10, Volume: 52, Issue:23 | Novel, broad-spectrum anticonvulsants containing a sulfamide group: advancement of N-((benzo[b]thien-3-yl)methyl)sulfamide (JNJ-26990990) into human clinical studies. |
AID1138687 | Permeability of the compound at pH 7.4 by PAMPA | 2014 | Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7 | Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines. |
AID628727 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against subcutaneous pentylenetetrazole-induced after 0.5 hrs | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs. |
AID1660935 | Permeability of the compound at 200 uM measured after 5 hrs at pH 7.4 by PAMPA | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays. |
AID474787 | Solubility of compound in PBS buffer at pH 7.4 | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones. |
AID363538 | Anticonvulsant activity in C57B/6 mouse assessed as inhibition of isoniazid-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID384089 | Neurotoxicity in ip dosed CF1 albino mouse after 0.5 hrs by rotarod test | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline. |
AID632996 | Anticonvulsant activity in po dosed rat assessed as protection against maximal electric shock-induced seizures | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID136253 | Minimal motor impairment was measured in mouse by rotating rod test upon intraperitoneal administration | 1997 | Journal of medicinal chemistry, May-23, Volume: 40, Issue:11 | Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents. |
AID226707 | Protective index which is the ratio of TD50 to ED50 of in maximal electroshock test. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and anticonvulsant activity of imidooxy derivatives. |
AID177577 | Ability to suppress MES (maximal electroshock) induced seizures in male Wistar rats | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants. |
AID176347 | Compound was tested intraperitoneally for anticonvulsant activity against MES-induced seizures in rat by MES test | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1264987 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as reduction of subcutaneous pentylenetetrazole-induced seizure | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents. |
AID625283 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID449306 | Neurotoxicity in ip dosed albino mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID91481 | Binding constant against human serum albumin (HSA) | 2001 | Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25 | Cheminformatic models to predict binding affinities to human serum albumin. |
AID678718 | Metabolic stability in human liver microsomes assessed as high signal/noise ratio (S/N of >100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID693317 | Anticonvulsant activity in ip dosed mouse assessed as compound concentration causing protection against maximal electroshock-induced seizures in half or more test animals after 4 hrs | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID1211293 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID1079946 | Presence of at least one case with successful reintroduction. [column 'REINT' in source] | |||
AID190465 | Antagonist activity to generalized seizures kindled amygdaloid seizures in rats | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1209456 | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID1269482 | Displacement of [3H]Batrachotoxinin from sodium channel site 2 in rat cerebral cortex at 500 uM after 60 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4 | New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones. |
AID682344 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 0.5 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID709901 | Stability in Wistar rat hepatocytes assessed as metabolite formation at >200 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID364286 | Anticonvulsant activity in ip dosed mouse after 0.5 hrs by MES test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID632995 | Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electric shock-induced seizures | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID1544806 | Anticonvulsant activity in ip dosed albino mouse model of maximal electroshock-induced seizures assessed as prevention of tonic hind limb extension pretreated for 0.5 hrs followed by 50 mA current-induction for 0.25 secs | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation. |
AID608434 | Anticonvulsant activity in Kunming mouse assessed as inhibition of subcutaneous pentylenetetrazol-induced death at 50 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1185524 | Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against MES-induced seizures after 0.5 hrs by MES test | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID1210065 | Induction of CYP2B6 mRNA expression in human donor hepatocytes after 48 hrs by real-time PCR method relative to untreated control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2 | Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy. |
AID130891 | Inhibition of hind limb tonus was tested by maximal metrazole seizure (MMS) test in mouse after 1 hr of peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID386623 | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy | 2008 | Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19 | Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1. |
AID29363 | Dissociation constant (pKa) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID382368 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of pentylenetetrazole-induced seizure after 0.5 hrs | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID1517279 | Protective index, ratio of TD50 for neurotoxicity against ip dosed Kunming mouse assessed as time remained in rod measured at 0.5 hrs by rotarod test to ED50 for anticonvulsant activity in ip dosed Kunming mouse assessed as MES-induced hind limb extension | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID1623670 | Apparent permeability of compound form basolateral to apical side in human Caco2 cells | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID1753898 | Passive membrane permeability of the compound in phosphate buffered saline at 200 uM incubated for 5 hrs by PAMPA assay based HPLC analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture. |
AID190461 | Anticonvulsant activity in corneal kindled rats was determined when 20 mg/kg was administered orally | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID363536 | Anticonvulsant activity in C57B/6 mouse assessed as inhibition of isoniazid-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID1605381 | Inhibition of full length mouse Frizzled-8 transfected in Frizzled-1/2/7 knockout HEK293T cells using lentiviral expression system cotransfected with Renilla luciferase assessed as reduction in Wnt3a signaling by measuring luciferase activity at 8 to 64 u | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8. |
AID1335450 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 100 mg/kg, ip after 0.5 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID1217706 | Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID136098 | Effect of compound on mouse motor performance was studied by performing a rotarod test in mouse dosing intraperitoneally at time of peak effect. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID255734 | Anticonvulsant activity of compound expressed in terms of median effective dose (ED50) produced after MES test in mouse by i.p. administration (range 5.5-14.1) | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines. |
AID682317 | Neurotoxicity in mouse assessed as motor impairment at 300 mg/kg, ip after 0.5 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID24185 | Distribution coefficient in octanol/water at pH 7.4 | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. |
AID1193493 | Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID1265481 | Protection index, ratio of TD50 for neurotoxicity in po dosed Sprague-Dawley rat to ED50 for anticonvulsant activity in po dosed Sprague-Dawley rat assessed as maximal electroshock-induced seizures | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID131927 | Tested for inhibition of quinoline-induced seizures in mice. | 1990 | Journal of medicinal chemistry, Oct, Volume: 33, Issue:10 | 2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents. |
AID136096 | Effect of compound on mouse motor performance was studied by performing a rotarod test in mouse 1 hr after peroral dosing | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID1474166 | Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index | 2016 | Drug discovery today, Apr, Volume: 21, Issue:4 | DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans. |
AID305069 | Neurotoxicity in Albino mouse at 100 mg/kg, ip after 0.5 hrs by rotarod test | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain. |
AID1193497 | Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID384088 | Anticonvulsant activity in CF1 albino mouse assessed as prevention of subcutaneous pentylenetetrazole-induced seizure at 300 mg/kg, ip after 4 hrs | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline. |
AID1211296 | Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID366629 | Protective index, ratio of TD50 for mouse by rotarod test to ED50 for mouse by scMET test | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID1544807 | Anticonvulsant activity in ip dosed albino mouse model of maximal electroshock-induced seizures assessed as prevention of tonic hind limb extension pretreated for 4 hrs followed by 50 mA current-induction for 0.25 secs | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation. |
AID481713 | Anticonvulsant activity in mouse assessed as reduction of thiosemicarbazide-induced lethality at 50 mg/kg, ip administered 30 mins prior to thiosemicarbazide challenge measured after 2.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID178051 | Inhibition of hind limb tonus was tested by maximal metrazole seizure test after 1 hr of peroral administration of compound | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID1720881 | Protective index, ratio of TD50 for neurotoxicity in ip and po injected mouse to ED50 for anticonvulsant activity in mouse assessed as protection against 50 mA current-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID1215120 | Binding affinity to Wistar rat brain lipid by TRANSIL assay | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID176271 | Maximal electroshock seizures determined for the inhibition of hind limb tonus in rat 1 hr after po dosing | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines. |
AID132639 | Inhibition of s.c. pentylenetetrazole induced seizure in mice following i.p. administration. | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID344479 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 4 hrs by MES screen test | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID496826 | Antimicrobial activity against Entamoeba histolytica | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1360429 | Binding affinity to human serum albumin after 4 hrs by LC-MS method | 2018 | European journal of medicinal chemistry, Jul-15, Volume: 155 | Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study. |
AID29845 | Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology. | 2000 | Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11 | SPR biosensor studies of the direct interaction between 27 drugs and a liposome surface: correlation with fraction absorbed in humans. |
AID489282 | Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID1210067 | Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method relative to untreated control | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2 | Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy. |
AID21264 | Effective permeability measured in human. | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. |
AID625280 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1571357 | Anticonvulsant activity in CF-1 mouse assessed as protection against 44 mA current-induced seizure at 40 to 80 mg/kg, ip after 0.5 hrs by 6 Hz psychomotor test | |||
AID1246317 | Permeability of the compound at pH 7.4 by PAMPA assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID496821 | Antimicrobial activity against Leishmania | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID351288 | Protective index, ratio of TD50 for neurotoxicity in C57B/6 mouse to ED50 for anticonvulsant activity in C57B/6 mouse | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID1304298 | Displacement of [125I]omega-Conotoxin GVIA from N-type calcium channel in rat cerebral cortex synaptoneurosomes at 100 uM measured after 30 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID1154496 | Passive transcellular permeability of the compound at pH 4 by PAMPA | 2014 | Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12 | Antileishmanial activity of a series of N²,N⁴-disubstituted quinazoline-2,4-diamines. |
AID382369 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of pentylenetetrazole-induced seizure after 4 hrs | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID681118 | TP_TRANSPORTER: transepithelial transport in Caco-2 cells | 2003 | International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2 | Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. |
AID496818 | Antimicrobial activity against Trypanosoma brucei brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID462613 | Permeability across artificial membrane assessed as membrane retention at 200 uM by PAMPA using HPLC/MS method | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID643480 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as protection against maximal electroshock-induced seizures after 2 hrs | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents. |
AID1217705 | Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID352393 | Anticonvulsant activity in ip dosed albino CF1 mouse assessed as minimum drug concentration required for inhibition of pentylenetetrazole-induced seizures in half or more of mouse after 0.5 hrs by scPTZ test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles. |
AID394938 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as minimum drug concentration required for inhibition of pentylenetetrazole-induced seizures in half or more of mouse after 0.5 hrs by scPTZ test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants. |
AID608435 | Anticonvulsant activity in Kunming mouse assessed as inhibition of subcutaneous pentylenetetrazol-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID26047 | logBB, log(C brain / C blood) | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Computation of brain-blood partitioning of organic solutes via free energy calculations. |
AID22950 | Time of peak effect (TPE) for activity | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and anticonvulsant activity of imidooxy derivatives. |
AID693337 | CNS depressant activity in mouse assessed as immobility time at 100 mg/kg, ip measured 60 mins post dose by porsolt's swimming pool test | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID286873 | Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID112295 | Compound was tested for anticonvulsant activity after intraperitoneal injection into mice by using scPTZ screen test after 0.25 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1191600 | Neurological toxicity in intraperitoneally dosed Swiss albino mouse assessed as motor impairment after 0.5 hrs by rotarod test | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents. |
AID682346 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 4 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID382382 | Antidepressant activity in Wistar rat assessed as increase in immobility time at 30 mg/kg, ip after 30 mins by forced-swimming test | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID490625 | Anticonvulsant activity in mouse assessed as bicuculline-induced clonic seizures at 30 mg/kg, ip administered 30 mins before bicuculline challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID449311 | Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of subcutaneous pentylenetetrazole-induced seizure after 4 hrs | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID364288 | Anticonvulsant activity in ip dosed mouse after 4 hrs by MES test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID255439 | Protective index (TD50/ED50) produced by compound in mouse after ScMet test | 2005 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 15, Issue:21 | Synthesis and anticonvulsant activity of 7-alkoxyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolines. |
AID1636356 | Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA | 2016 | Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16 | Development of a cell viability assay to assess drug metabolite structure-toxicity relationships. |
AID1079935 | Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source] | |||
AID1210064 | Induction of CYP2B6 mRNA expression in human donor hepatocytes after 48 hrs by real-time PCR method | 2013 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2 | Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy. |
AID27167 | Delta logD (logD6.5 - logD7.4) | 2000 | Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13 | QSAR model for drug human oral bioavailability. |
AID1191596 | Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in electrical stimulus-induced seizures after 0.5 hrs by maximal electroshock seizure test | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents. |
AID205290 | Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6 | 3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers. |
AID122469 | Ratio of the dose showing muscle relaxant action in rats and the dose suppressing MES induced seizures in rats | 1984 | Journal of medicinal chemistry, May, Volume: 27, Issue:5 | Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants. |
AID1720890 | Anticonvulsant activity in KunMing mouse assessed as protection against current-induced seizure by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID727990 | Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against scPTZ-induced seizures after 4 hrs | 2013 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 23, Issue:3 | Novel limonene and citral based 2,5-disubstituted-1,3,4-oxadiazoles: a natural product coupled approach to semicarbazones for antiepileptic activity. |
AID129448 | Antipentylene tetrazole activity was determined in mice when administered perorally | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | A novel class of potential central nervous system agents. 3-Phenyl-2-(1-piperazinyl)-5H-1-benzazepines. |
AID637069 | Neurotoxicity in ip dosed Kunming mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones. |
AID52381 | Oral dose protecting 50% of the mice from electroshock induced seizures. | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID1336194 | Protection index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for ip dosed maximal electroshock induced seizure mouse model | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID226509 | Protection index = TD50/ED50 (MES) | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID221089 | Time of peak effect of toxicity of compound was measured by both MES and sc Met test in mice | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Synthesis and CLOGP correlation of imidooxy anticonvulsants. |
AID628629 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against maximal electroshock after 4 hrs | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs. |
AID190105 | Compound was tested for anticonvulsant activity administered by gastric tube in rat by rotarod test | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID217928 | Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release) | 2001 | Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2 | Medicinal chemistry of neuronal voltage-gated sodium channel blockers. |
AID625282 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID1209333 | Ratio of drug level in brain to plasma in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID1335449 | Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 30 mg/kg, ip after 0.5 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID433898 | Toxicity in Kunming mouse assessed as 3-mercaptopropionic acid-induced lethality at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID1185529 | Protective index, ratio of oral neurotoxic TD50 against Kunming mouse by rotarod test to oral anticonvulsant ED50 in Kunming mouse by MES test | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID353056 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against maximal electroshock-induced seizure after 30 mins | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID433893 | Anticonvulsant activity against isoniazid-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID477359 | Protective index, ratio of TD50 for neurotoxicity in Swiss albino mouse to ED50 for inhibition of maximal electroshock-induced seizures Swiss albino mouse | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. |
AID1605382 | Inhibition of full length mouse Frizzled-8 transfected in Frizzled-1/2/7 knockout HEK293T cells using lentiviral expression system cotransfected with Renilla luciferase assessed as reduction in Wnt3a signaling by measuring luciferase activity at 64 uM mea | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8. |
AID709905 | Drug metabolism in Wistar rat hepatocytes assessed as ratio of 10,11-epoxide metabolite level to parent compound level at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID709902 | Drug metabolism in Wistar rat hepatocytes assessed as ratio of O-sulfonate I metabolite level to parent compound level at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID286861 | Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID286886 | Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 1 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID678927 | TP_TRANSPORTER: no change in brain concentration in mdr1a/1b(-/-) mouse | 2001 | British journal of clinical pharmacology, Apr, Volume: 51, Issue:4 | Carbamazepine is not a substrate for P-glycoprotein. |
AID47017 | Dose producing neurotoxic effects in 50% of the CF1 mice after intraperitoneal administration. | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID136279 | The cytotoxicity after intraperitoneal administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID1227820 | Inhibition of Nav1.7 (unknown origin) by electrophysiological assay | 2015 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1 | Dibenzazepines and dibenzoxazepines as sodium channel blockers. |
AID109718 | Anticonvulsant activity after intraperitoneal injection into mice by using MES screen test after 0.5 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID109720 | Anticonvulsant activity after intraperitoneal injection into mice by using scPTZ screen after 0.5 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID286894 | Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 2.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID114126 | Anticonvulsant activity in mice using the maximal electroshock seizure test. | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID1701383 | Intrinsic clearance in mouse liver microsomes at 1 uM measured up to 30 mins in presence of NADPH by UPLC-MS/MS analysis | |||
AID189164 | Protective index value of the compound, given by intraperitoneally (TD50/ED50) | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID256147 | Number of rats protected at a dose of 30 mg/Kg when given oral at 0.25 hr upon maximal electroshock seizure; Total number of rats = 4; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID1544809 | Anticonvulsant activity in ip dosed albino mouse model of subcutaneous pentylenetetrazole-induced seizure assessed as failure to observe even a single episode of clonic spasms for at least 5 secs pretreated for 0.5 hrs followed by pentylenetetrazole induc | 2019 | Bioorganic & medicinal chemistry letters, 07-15, Volume: 29, Issue:14 | Novel benzothiazole hydrazine carboxamide hybrid scaffolds as potential in vitro GABA AT enzyme inhibitors: Synthesis, molecular docking and antiepileptic evaluation. |
AID205273 | Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain | 2004 | Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13 | 2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators. |
AID396643 | Anticonvulsant activity in OF1 mouse assessed as protection against maximal electroshock-induced seizures at 50 mg/kg, ip after 2 hrs | 2008 | European journal of medicinal chemistry, Dec, Volume: 43, Issue:12 | Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation. |
AID489279 | Anticonvulsant activity against subcutaneous strychnine-induced seizures in Wistar rat at 300 mg/kg, ip after 0.5 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID256138 | Number of rats protected at a dose of 30 mg/Kg when given oral at 1 hr upon maximal electroshock seizure; Total number of rats = 4; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID395328 | Lipophilicity, log P of the compound | 2009 | Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6 | Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs. |
AID462611 | Effective permeability across artificial membrane at 200 uM by PAMPA using HPLC/MS method | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID1227823 | Kinetic solubility of the compound at pH 6.8 | 2015 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1 | Dibenzazepines and dibenzoxazepines as sodium channel blockers. |
AID496827 | Antimicrobial activity against Leishmania amazonensis | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID129976 | Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse maximal metrazole seizures (MMS) after peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID709900 | Drug metabolism in Wistar rat hepatocytes assessed as ratio of O-sulfonate II metabolite level to parent compound level at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID1264989 | Protective index, ratio of TD50 for ip dosed Swiss albino mouse assessed as inability of animal to maintain equilibrium on rod after 0.5 hrs by rotarod test to ED50 for Swiss albino mouse assessed as subcutaneous pentylenetetrazole-induced seizure | 2015 | European journal of medicinal chemistry, Dec-01, Volume: 106 | Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents. |
AID363540 | Toxicity in isoniazid-induced seizure C57B/6 mouse model assessed as lethality at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID353057 | Neurotoxicity in ip dosed C57B/6 mouse after 30 mins by rotarod test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID1335447 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 4 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID1304297 | Displacement of [3H]Batrachotoxinin from voltage-sensitive sodium channel site 2 in rat cerebral cortex synaptoneurosomes at 500 uM measured after 60 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID1251235 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizure | 2015 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 25, Issue:20 | Discovery of benzothiazine derivatives as novel, orally-active anti-epileptic drug candidates with broad anticonvulsant effect. |
AID132648 | The effective dose of compound was tested against maximal electroshock induced seizures after oral administration in mice | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID1195113 | Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse by maximal electroshock test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
AID1223490 | Apparent permeability across human differentiated Caco2 cells | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 40, Issue:2 | Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study. |
AID521220 | Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay | 2007 | Nature chemical biology, May, Volume: 3, Issue:5 | Chemical genetics reveals a complex functional ground state of neural stem cells. |
AID363532 | Anticonvulsant activity in C57B/6 mouse assessed as inhibition of pentylenetetrazole-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID682319 | Neurotoxicity in mouse assessed as motor impairment at 100 mg/kg, ip after 4 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID1229816 | Inhibition of [3H]BTX binding to sodium channel site 2 in rat cerebral cortex synaptosomes at 500 uM incubated for 60 mins by scintillation counting based radioligand displacement assay | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13 | Design, synthesis, and anticonvulsant activity of new hybrid compounds derived from 2-(2,5-dioxopyrrolidin-1-yl)propanamides and 2-(2,5-dioxopyrrolidin-1-yl)butanamides. |
AID481707 | Anticonvulsant activity in mouse assessed as reduction of isoniazid-induced lethality at 50 mg/kg, ip administered 30 mins prior to isoniazid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID170623 | Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 1 hr; Compound was not screened | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1720894 | Protective index, ratio of TD50 for neurotoxicity in KunMing mouse to ED50 for anticonvulsant activity in KunMing mouse assessed as protection against current-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID24420 | Partition coefficient (logP) | 1998 | Journal of medicinal chemistry, Dec-03, Volume: 41, Issue:25 | Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. |
AID545528 | Anticonvulsant activity in ip dosed mouse assessed as inhibition of PTZ-induced clonic seizure | 2010 | European journal of medicinal chemistry, Dec, Volume: 45, Issue:12 | Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives. |
AID481705 | Anticonvulsant activity in mouse assessed as inhibition of isoniazid-induced clonic seizure at 50 mg/kg, ip administered 30 mins prior to isoniazid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID256413 | Minimum dose required for anticonvulsant activity when given i.p., at 0.5 h in mice upon subcutaneous strychnine seizure; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID225157 | Dose reducing the seizure severity in rat cornea 1 hr after peroral administration. | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID227701 | Anticonvulsant activity; NC denotes that compound is not classified | 2003 | Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16 | Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity. |
AID643474 | Neurotoxicity in ip dosed Swiss albino mouse assessed as impair in motor coordination from 0.5 to 4 hrs post administration by rotarod test | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents. |
AID1336188 | Anticonvulsant activity in ip dosed 6-Hz induced seizure mouse model assessed as restoration of normal activity within 10 secs from stimulation at 32 mA | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID136110 | Inhibition of hind limb tonus was tested by maximal metrazole seizure (MMS) test administered intraperitoneally in mouse | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID177915 | Inhibition of hind limb tonus was tested at time of peak effect by maximal electroshock test (MES) on intraperitoneal administration of compound in rats | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID286872 | Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1211295 | Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO2 | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3 | Control and measurement of plasma pH in equilibrium dialysis: influence on drug plasma protein binding. |
AID256144 | Number of rats protected at a dose of 30 mg/Kg when given oral at 0.5 hr upon maximal electroshock seizure; Total number of rats = 4; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID418135 | Anticonvulsant activity in po dosed rat assessed as protection against subcutaneous metrazole-induced seizure | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID130888 | Inhibition of hind limb tonus was tested at time of peak effect by maximal electroshock test (MES) in mouse on intraperitoneal administration of compound | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID286871 | Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID462614 | Apparent permeability in BBMEC | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID1160934 | Effective permeability of the compound at pH 7.4 by PAMPA | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
AID624609 | Specific activity of expressed human recombinant UGT1A6 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID1185527 | Anticonvulsant activity in orally dosed Kunming mouse assessed as protection against MES-induced seizures after 0.5 hrs by MES test | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID1720887 | Anticonvulsant activity in KunMing mouse assessed as protection against 50 mA current-induced seizure after 0.5 to 4 hrs by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID418138 | Therapeutic index, ratio of TD50 for po dosed rat to ED50 for protection against subcutaneous metrazole-induced seizure in po dosed rat | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID1191601 | Neurological toxicity in intraperitoneally dosed Swiss albino mouse assessed as motor impairment after 4 hrs by rotarod test | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents. |
AID625276 | FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI | 2011 | Drug discovery today, Aug, Volume: 16, Issue:15-16 | FDA-approved drug labeling for the study of drug-induced liver injury. |
AID110223 | Ability to prevent the tonic extensor component induced by 106.25 mg/kg sc of pentylenetetrazole | 1994 | Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14 | Synthesis and anticonvulsant properties of new benzylpyridazine derivatives. |
AID1623671 | Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco2 cells | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID221087 | Time of peak effect of activity of compound was measured by both MES and sc Met test in mice | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Synthesis and CLOGP correlation of imidooxy anticonvulsants. |
AID1304299 | Displacement of [125I]omega-Conotoxin GVIA from N-type calcium channel in rat cerebral cortex synaptoneurosomes at 200 uM measured after 30 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID489286 | Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID1209379 | AUC(0 to 7 hrs) in Sprague-Dawley rat plasma at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID709893 | Drug metabolism in human liver microsomes assessed as 10,11 epoxidation level at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID1571282 | Neurotoxicity in Sprague-Dawley rat at 100 mg/kg, ip measured after 2 hrs by rotarod test | |||
AID1336196 | Protection index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for ip dosed 6-Hz induced seizure mouse model at 32 mA | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID363530 | Anticonvulsant activity in C57B/6 mouse assessed as inhibition of pentylenetetrazole-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID51429 | Compound was evaluated for toxic dose at peak neurologic deficit after intraperitoneal administration of the compound. | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and anticonvulsant activity of imidooxy derivatives. |
AID114861 | Effective dose required for the inhibition of spontaneous locomotion after intraperitoneal administration in experiment 1 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID608530 | Anticonvulsant activity in Kunming mouse assessed as inhibition of thiosemicarbazide-induced death at 30 mg/kg, ip after 2.5 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID489284 | Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID496819 | Antimicrobial activity against Plasmodium falciparum | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID286879 | Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs, ip | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1335456 | Neurotoxicity in Swiss albino mouse at 100 mg/kg, ip after 0.5 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID364292 | Anticonvulsant activity in ip dosed mouse after 4 hrs by scPTZ test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID132637 | The compound was tested to inhibit 50% of induced maximal electroshock seizure in mice on ip administration. | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID178166 | Compound was tested for anticonvulsant activity administered by gastric tube in rat by MES test | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID366628 | Anticonvulsant activity against scMet-induced seizures in ip dosed mouse | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID643475 | Protection index, ratio of TD50 for Swiss albino mouse by rotarod test to ED50 for Swiss albino mouse by maximal electroshock test | 2012 | Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2 | Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents. |
AID678712 | Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID977602 | Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM | 2013 | Molecular pharmacology, Jun, Volume: 83, Issue:6 | Structure-based identification of OATP1B1/3 inhibitors. |
AID132474 | Anticonvulsant activity against subcutaneous picrotoxin induced seizures after intraperitoneal administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID1065339 | Anticonvulsant activity in albino rat assessed as protection against pentylenetetrazole-induced seizure at 300 mg/kg, ip measured after 4 hrs | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID295296 | Anticonvulsant activity in OF1 mouse at 30 mg/kg, ip after 2 hrs by MES test | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Carbonic anhydrase inhibitors. Inhibition of isoforms I, II, IV, VA, VII, IX, and XIV with sulfonamides incorporating fructopyranose-thioureido tails. |
AID1404017 | Permeability of the compound at 500 uM after 8 hrs by PAMPA | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors. |
AID7779 | Oral bioavailability in human | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2 | Graphical model for estimating oral bioavailability of drugs in humans and other species from their Caco-2 permeability and in vitro liver enzyme metabolic stability rates. |
AID1246354 | Permeability of the compound at pH 7.4 assessed as drug retention by PAMPA assay | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | (+)-Dehydroabietylamine derivatives target triple-negative breast cancer. |
AID1065341 | Anticonvulsant activity in albino rat assessed as protection against pentylenetetrazole-induced seizure at 300 mg/kg, ip measured after 0.5 hrs | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID212343 | The compound was determined for the dose (mg/kg) by rotarod test at the time of peak neurotoxic effect in mice on ip administration. | 1998 | Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7 | Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives. |
AID632993 | Neurotoxicity in ip dosed mouse assessed as inability to maintain equilibrium on rotarod by rotarod test | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID1335458 | Neurotoxicity in Swiss albino mouse at 30 mg/kg, ip after 4 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID637075 | Protective index, ratio of TD50 for ip dosed Kunming mouse to ED50 for ip dosed Kunming mouse by maximal electroshock seizure test | 2012 | European journal of medicinal chemistry, Feb, Volume: 48 | Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones. |
AID709899 | Drug metabolism in Wistar rat hepatocytes assessed as GSH adduct formation at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID1193494 | Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery. |
AID709903 | Drug metabolism in Wistar rat hepatocytes assessed as ratio of epoxide N-glucuronide metabolite level to parent compound level at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID113854 | Effective dose against convulsions induced by clonic pentylenetetrazole after intraperitoneal administration in experiment 1 | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | 6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents. |
AID1265489 | Protection index, ratio of TD50 for neurotoxicity in ip dosed albino Carworth Farms No.1 mouse to ED50 for anticonvulsant activity in ip dosed albino Carworth Farms No.1 mouse assessed as protection against maximal electroshock-induced seizures | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID1705559 | Drug metabolism in rat liver microsomes at 50 uM preincubated with compound followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis | 2020 | European journal of medicinal chemistry, Dec-15, Volume: 208 | Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction. |
AID1720882 | Neurotoxicity in mouse by rotarod test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID1215123 | Binding affinity to Wistar rat serum albumin | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2 | Brain tissue binding of drugs: evaluation and validation of solid supported porcine brain membrane vesicles (TRANSIL) as a novel high-throughput method. |
AID382371 | Neurotoxicity in ip dosed mouse after 4 hrs by rotarod test | 2008 | European journal of medicinal chemistry, Jan, Volume: 43, Issue:1 | Synthesis and CNS depressant activity of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID440595 | Anticonvulsant activity in Webster mouse assessed as protection against yohimbine-HCl-induced clonic seizure at 5 mg/kg, ip administered 30 mins before yohimbine-HCl challenge | 2009 | European journal of medicinal chemistry, Dec, Volume: 44, Issue:12 | Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives. |
AID1404016 | Permeability of the compound by PAMPA | 2018 | European journal of medicinal chemistry, Feb-10, Volume: 145 | Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors. |
AID189163 | Protective index value of the compound, given by gastric tube (TD50/ED50) | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1304300 | Displacement of [3H]diltiazem from L-type calcium channel diltiazem binding site in rat cerebral cortex synaptoneurosomes at 100 uM measured after 120 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID624607 | Specific activity of expressed human recombinant UGT1A3 | 2000 | Annual review of pharmacology and toxicology, , Volume: 40 | Human UDP-glucuronosyltransferases: metabolism, expression, and disease. |
AID418131 | Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizure | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID366627 | Neurotoxicity in ip dosed mouse by rotarod test | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID286882 | Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 1.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID384084 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as prevention of subcutaneous pentylenetetrazole-induced seizure after 0.5 hrs | 2008 | European journal of medicinal chemistry, Apr, Volume: 43, Issue:4 | Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline. |
AID286896 | Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 1 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID481714 | Anticonvulsant in po dosed mouse assessed as protection against maximum electric stimulus-induced seizures | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID682348 | Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 30 mg/kg, ip after 0.5 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID608432 | Anticonvulsant activity in Kunming mouse assessed as inhibition of isoniazid-induced tonic seizures at 50 mg/kg, ip after 1 hrs | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID693315 | Anticonvulsant activity in ip dosed mouse assessed as compound concentration causing protection against maximal electroshock-induced seizures in half or more test animals after 0.5 hrs | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID449307 | Neurotoxicity in ip dosed albino mouse assessed as minimal motor impairment after 4 hrs by rotarod test | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID286899 | Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 2.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID462616 | Apparent permeability in BBMEC assessed as membrane retention | 2010 | Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6 | N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles. |
AID178052 | Inhibition of hind limb tonus was tested by maximal metrazole seizure test after 4 hr of peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines. |
AID1383763 | Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-BBB assay | 2018 | European journal of medicinal chemistry, Apr-25, Volume: 150 | Metallomics for Alzheimer's disease treatment: Use of new generation of chelators combining metal-cation binding and transport properties. |
AID1336213 | Neurotoxicity in po dosed Sprague-Dawley rat assessed as behavioral change | 2017 | Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2 | Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
AID1660936 | Permeability of the compound assessed as mass retention at 200 uM measured after 5 hrs at pH 7.4 by PAMPA | 2020 | Journal of medicinal chemistry, 08-13, Volume: 63, Issue:15 | A New Class of Dengue and West Nile Virus Protease Inhibitors with Submicromolar Activity in Reporter Gene DENV-2 Protease and Viral Replication Assays. |
AID1720884 | Anticonvulsant activity in KunMing mouse assessed as protection against 50 mA current-induced seizure after 30 mins interval by maximal electroshock seizure test | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID394945 | Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum drug concentration required for falling off the rotarod by half or more of mouse after 0.5 hrs by rotarod test | 2009 | European journal of medicinal chemistry, Jan, Volume: 44, Issue:1 | Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants. |
AID678717 | Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins | 2012 | Chemical research in toxicology, Oct-15, Volume: 25, Issue:10 | Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds. |
AID244690 | Dissociation constant for binding to resting state of rat brain NaIIa (rNav1.2) -B2 cell line stably expressed in HEK293 Cells | 2004 | Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17 | Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors. |
AID1209409 | AUC(0 to 7 hrs) in Sprague-Dawley rat brain at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID449304 | Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of maximal electric shock-induced seizures after 4 hrs | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID481697 | Anticonvulsant in ip dosed mouse assessed as protection against maximum electric stimulus-induced seizures | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID190581 | Anticonvulsant activity in corneal kindled rats was determined when 40 mg/kg was administered orally | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID666677 | Neurotoxicity in ip dosed Kunming mouse measured 30 mins post compound administration by rotorod test | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives. |
AID477358 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as inhibition of PTZ-induced motor impairment | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. |
AID1517333 | Inhibition of human LDH1 assessed as remaining activity at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control | 2019 | European journal of medicinal chemistry, Dec-01, Volume: 183 | Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study. |
AID114036 | Minimal motor impairment activity by Rotarod test in mice following i.p. administration. | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID227718 | Binding energy by using the equation deltaG obsd = -RT ln KD | 1984 | Journal of medicinal chemistry, Dec, Volume: 27, Issue:12 | Functional group contributions to drug-receptor interactions. |
AID205268 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM | 1985 | Journal of medicinal chemistry, Mar, Volume: 28, Issue:3 | [3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs. |
AID1720867 | Anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID449303 | Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of maximal electric shock-induced seizures after 0.5 hrs | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Synthesis, anticonvulsant and CNS depressant activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-phenyl/ethyl-4H-quinazolin-3-yl)-urea. |
AID509497 | Reduction of immobility time in albino Swiss mouse at 100 mg/kg, ip pretreated for 1 hrs by forced swimming test | 2010 | European journal of medicinal chemistry, Sep, Volume: 45, Issue:9 | Design & synthesis of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one as potential anticonvulsant agents. |
AID1058306 | Anticonvulsant activity in Sprague-Dawley rat hippocampal kindling model assessed as reduction in global seizures at >26 mg/kg, ip treated 15 for mins post suprathreshold-stimulation | 2013 | Journal of medicinal chemistry, Nov-27, Volume: 56, Issue:22 | Novel, broad-spectrum anticonvulsants containing a sulfamide group: pharmacological properties of (S)-N-[(6-chloro-2,3-dihydrobenzo[1,4]dioxin-2-yl)methyl]sulfamide (JNJ-26489112). |
AID256140 | Number of rats protected at a dose of 30 mg/Kg when given oral at 4 hr upon maximal electroshock seizure; Total number of rats = 4; Absence of activity | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID682349 | Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 100 mg/kg, ip after 0.5 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID1191598 | Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in clonic seizures after 0.5 hrs by subcutaneous pentylenetetrazole seizure test | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents. |
AID693324 | Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 4 hrs by rotarod test | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID1265491 | Anticonvulsant activity in ip dosed albino Carworth Farms No.1 mouse assessed as protection against subcutaneous dosed pentetrazol-induced seizures after 0.25 hrs | 2016 | European journal of medicinal chemistry, Jan-01, Volume: 107 | Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols. |
AID177084 | Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in rat maximal electroshock seizures (MES) after peroral administration | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives. |
AID352567 | Neurotoxicity in ip dosed albino CF1 mouse assessed as minimum drug concentration required for motor impairment in half or more of mouse after 0.5 hrs by rotarod test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles. |
AID190110 | Compound was tested intraperitoneally for anticonvulsant activity by rotarod test | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID351012 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against thiosemicarbazide-induced tonic seizure administered 30 mins before thiosemicarbazide challenge measured after 1 hrs | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID286875 | Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr, ip | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1160938 | Aqueous solubility of the compound at pH 2 | 2014 | Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21 | Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium. |
AID709897 | Stability in Wistar rat hepatocytes assessed as 10,11-epoxide N-glucuronide metabolite formation at 1 mM incubated for 6 hrs by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID1227825 | Metabolic stability in rat liver microsomes assessed as compound remaining at 1 uM after 30 mins | 2015 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1 | Dibenzazepines and dibenzoxazepines as sodium channel blockers. |
AID217788 | Displacement of [3H]batrachotoxin A 20alpha-benzoate (BTX-B) from rat cerebral cortex voltage-gated sodium channel | 1989 | Journal of medicinal chemistry, Jul, Volume: 32, Issue:7 | Sodium channel binding and anticonvulsant activities for the enantiomers of a bicyclic 2,4-oxazolidinedione and monocyclic models. |
AID1783665 | Effective permeability of the compound in PBS/EtOH buffer (9:1) at 200 mM after 10 hrs by HPLC-UV based PAMPA-BBB assay | 2021 | European journal of medicinal chemistry, Nov-15, Volume: 224 | 1,10-Seco-Eudesmane sesquiterpenoids as a new type of anti-neuroinflammatory agents by suppressing TLR4/NF-κB/MAPK pathways. |
AID453204 | Permeability in human skin after 48 hrs by Franz cell permeability assay | 2010 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1 | Development of an in silico model for human skin permeation based on a Franz cell skin permeability assay. |
AID1571287 | Anticonvulsant activity in ip dosed CF-1 mouse model of maximal electroshock-induced seizure assessed as suppression of tonic hind limb extension | |||
AID286891 | Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 1 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID679773 | TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Carbamazepine: 100 uM) in MDR1-expressing MDCKII cells | 2002 | The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3 | Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. |
AID139327 | Time of peak effect toxicity against maximal electroshock induced seizures | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID1701382 | Intrinsic clearance in human liver microsomes at 1 uM measured up to 30 mins in presence of NADPH by UPLC-MS/MS analysis | |||
AID286874 | Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID231424 | Protective index was calculated (TD50/ED50) in MES assay in mice after oral administration | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID223442 | Effective dose was measured in mouse by subcutaneous pentylenetetrazole method by ip administration; Not determined | 1993 | Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23 | Synthesis and CLOGP correlation of imidooxy anticonvulsants. |
AID1065335 | Neurotoxicity in ip dosed albino mouse after 4 hrs by rotorod test | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID1335455 | Neurotoxicity in Swiss albino mouse at 30 mg/kg, ip after 0.5 hrs by rotarod test | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID1753896 | Passive membrane permeability of the compound in phosphate buffered saline assessed as concentration of the compound in acceptor plate at 200 uM incubated for 5 hrs by PAMPA assay based HPLC analysis | 2021 | Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8 | Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture. |
AID351283 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against isoniazid-induced seizures administered before 30 mins of isoniazid induction measured for 1 hr | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design, synthesis of 8-alkoxy-5,6-dihydro-[1,2,4]triazino[4,3-a]quinolin-1-ones with anticonvulsant activity. |
AID679128 | TP_TRANSPORTER: transcellular transport in MDR1-expressing LLC-PK1 cells | 2007 | Neuropharmacology, Feb, Volume: 52, Issue:2 | Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. |
AID366631 | Displacement of [3H]nitrendipine from voltage-dependent calcium channel in rat brain cortex by scintillation counting | 2008 | Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15 | Anticonvulsant activity of some xanthone derivatives. |
AID286887 | Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 1.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID608517 | Protective index, ratio of TD50 for neurotoxicity in Kunming mouse to ED50 for inhibition of MES-induced seizures in Kunming mouse | 2011 | European journal of medicinal chemistry, Jul, Volume: 46, Issue:7 | Synthesis and anticonvulsant activity of 7-phenyl-6,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-ones and their derivatives. |
AID1720865 | Protective index, ratio of TD50 for neurotoxicity in ip injected albino mouse to ED50 for anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure | 2020 | Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15 | Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants. |
AID50621 | Compound was evaluated for effective dose by subcutaneous pentylenetetrazole test after intraperitoneal administration of the compound; Not Effective | 1991 | Journal of medicinal chemistry, Jan, Volume: 34, Issue:1 | Synthesis and anticonvulsant activity of imidooxy derivatives. |
AID467612 | Fraction unbound in human plasma | 2009 | European journal of medicinal chemistry, Nov, Volume: 44, Issue:11 | Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data. |
AID305062 | Anticonvulsant activity against maximal electroshock-induced seizure in Albino mouse at 300 mg/kg, ip after 4 hrs | 2007 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1 | Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain. |
AID1304305 | Displacement of [3H]D888 from L-type calcium channel verapamil binding site in rat cerebral cortex synaptoneurosomes at 200 uM measured after 120 mins by scintillation counting method | 2016 | Bioorganic & medicinal chemistry, 07-01, Volume: 24, Issue:13 | Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides. |
AID693321 | Anticonvulsant activity in ip mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures | 2012 | European journal of medicinal chemistry, Dec, Volume: 58 | Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective. |
AID588211 | Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans | 2010 | Chemical research in toxicology, Jan, Volume: 23, Issue:1 | Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species. |
AID256185 | Post treatment immobility time for CNS study using Porsolt's swimpool test at a dose of 100 mg/Kg after 1 hr when given i.p., in mice (No. of animals 6); Control (24h before) 131 | 2005 | Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20 | Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design. |
AID481708 | Anticonvulsant activity in mouse assessed as inhibition of 3-mercaptopropionic acid-induced clonic seizure at 50 mg/kg, ip administered 30 mins prior to 3-mercaptopropionic acid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID1173473 | Protective index, ratio of TD50 for CF1 albino mouse neurotoxicity to ED50 for protection against 6 Hz electroshock-induced seizure in CF1 albino mouse | 2014 | Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23 | Seizure prevention by the naturally occurring phenols, carvacrol and thymol in a partial seizure-psychomotor model. |
AID497005 | Antimicrobial activity against Pneumocystis carinii | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID114801 | Anticonvulsant activity in Clonic seizures when administered orally in mice | 1986 | Journal of medicinal chemistry, Mar, Volume: 29, Issue:3 | Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy. |
AID1217704 | Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1335443 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 0.5 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID1605383 | Binding affinity to immobilized mouse C-terminal Rhinovirus 3C cleavage site-fused 6xHis-tagged Frizzled-8 CRD (Q33 to G173 resideus) transfected with pDisplay_BirA-ER plasmid in HEK293T cells for biotinylation assessed as protein-compound complex formati | 2020 | Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6 | Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8. |
AID496820 | Antimicrobial activity against Trypanosoma brucei | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1209457 | Unbound Cmax in human plasma | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1 | In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans. |
AID1065344 | Anticonvulsant activity in ip dosed albino mouse assessed as protection against maximal electroshock-induced seizures after 4 hrs | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID1185533 | Anticonvulsant activity in Kunming mouse assessed as protection against sc-PTZ-induced mortality 50 mg/kg, sc administered 30 mins before PTZ injection | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID481706 | Anticonvulsant activity in mouse assessed as inhibition of isoniazid-induced tonic seizure at 50 mg/kg, ip administered 30 mins prior to isoniazid challenge measured after 0.5 hrs | 2010 | European journal of medicinal chemistry, May, Volume: 45, Issue:5 | Synthesis and anticonvulsant activity of a new 6-alkoxy-[1,2,4]triazolo[4,3-b]pyridazine. |
AID180905 | The effective dose of compound was tested against maximal electroshock induced seizures after oral administration in rat | 1990 | Journal of medicinal chemistry, Mar, Volume: 33, Issue:3 | Synthesis and anticonvulsant activity of 2-benzylglutarimides. |
AID344478 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 0.5 hrs by MES screen test | 2008 | European journal of medicinal chemistry, May, Volume: 43, Issue:5 | N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation. |
AID363528 | Neurotoxicity in ip dosed C57B/6 mouse after 30 mins by rotarod test | 2008 | European journal of medicinal chemistry, Jun, Volume: 43, Issue:6 | Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents. |
AID1573965 | Anticonvulsant activity in ip dosed F-1 albino mouse assessed as protection against 32 mA current-induced seizure pretreated at 0.5 to 2 hrs by maximal electroshock seizure test | |||
AID1623690 | Permeability of compound at pH 7.4 assessed as drug retention by PAMPA | 2019 | European journal of medicinal chemistry, Feb-15, Volume: 164 | Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents. |
AID1217708 | Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7 | Combination of GSH trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites. |
AID1209385 | AUC(0 to infinity) in Sprague-Dawley rat plasma at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID481444 | Octanol-water partition coefficient, log P of the compound | 2010 | Journal of medicinal chemistry, May-13, Volume: 53, Issue:9 | How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability? |
AID286860 | Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID433894 | Anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 0.5 hrs | 2009 | European journal of medicinal chemistry, Sep, Volume: 44, Issue:9 | Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives. |
AID1185531 | Anticonvulsant activity in Kunming mouse assessed as protection against sc-PTZ-induced clonic seizures 50 mg/kg, sc administered 30 mins before PTZ injection | 2014 | European journal of medicinal chemistry, Sep-12, Volume: 84 | Synthesis and anticonvulsant activity of novel purine derivatives. |
AID1810293 | Aqueous solubility of compound at pH 7.4 | 2021 | Journal of medicinal chemistry, 05-27, Volume: 64, Issue:10 | Aminoalkoxycarbonyloxymethyl Ether Prodrugs with a pH-Triggered Release Mechanism: A Case Study Improving the Solubility, Bioavailability, and Efficacy of Antimalarial 4(1 |
AID1335448 | Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 4 hrs | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA |
AID632998 | Protective index, ratio of TD50 for neurotoxicity in rat to ED50 for inhibition of maximal electroshock-induced seizures in rat | 2011 | Bioorganic & medicinal chemistry, Nov-15, Volume: 19, Issue:22 | Synthesis and anticonvulsant activity of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs. |
AID286864 | Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID1209349 | Ratio of unbound brain concentration to drug level in cerebrospinal fluid in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID539470 | Solubility of the compound in water | 2010 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24 | Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate. |
AID286877 | Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs, ip | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID496830 | Antimicrobial activity against Leishmania major | 2010 | Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6 | Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species. |
AID1209417 | AUC(0 to infinity) in Sprague-Dawley rat brain at 3 mg/kg, sc by LC-MS/MS analysis | 2012 | Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 40, Issue:11 | An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. |
AID20163 | The ratio of brain-blood partitioning, (C brain / C blood). | 1996 | Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24 | Computation of brain-blood partitioning of organic solutes via free energy calculations. |
AID477357 | Anticonvulsant activity in ip dosed Swiss albino mouse assessed as inhibition of maximum electric shock-induced motor impairment | 2010 | European journal of medicinal chemistry, Apr, Volume: 45, Issue:4 | Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening. |
AID351013 | Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against 3-mercaptopropionic acid-induced tonic seizure administered 30 mins before 3-mercaptopropionic acid challenge measured after 1 hrs | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID109723 | Toxicity after intraperitoneal injection into mice by using toxicity screen test after 0.5 hr | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID1065346 | Anticonvulsant activity in ip dosed albino mouse assessed as protection against maximal electroshock-induced seizures after 0.5 hrs | 2013 | European journal of medicinal chemistry, Sep, Volume: 67 | Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach. |
AID352389 | Anticonvulsant activity in ip dosed albino CF1 mouse assessed as minimum drug concentration required for inhibition of maximal electroshock-induced seizure in half or more of mouse after 0.5 hrs by MES test | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles. |
AID1191597 | Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in electrical stimulus-induced seizures after 4 hrs by maximal electroshock seizure test | 2015 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5 | Design, synthesis and pharmacological evaluation of N-[4-(4-(alkyl/aryl/heteroaryl)-piperazin-1-yl)-phenyl]-carbamic acid ethyl ester derivatives as novel anticonvulsant agents. |
AID666679 | Protective index, ratio of TD50 for neurotoxicity in Kunming mouse to ED50 for protection against subcutaneous pentylenetetrazol-induced clonic seizures in Kunming mouse | 2012 | European journal of medicinal chemistry, Aug, Volume: 54 | Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives. |
AID223725 | Oral dose producing neurotoxic effects in 50% of rats | 1992 | Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15 | Synthesis and anticonvulsant activity of enaminones. |
AID351014 | Anticonvulsant activity in C57B/6 mouse assessed as protection against strychnine-induced tonic seizure at 300 mg/kg, ip administered 30 mins before strychnine challenge measured after 30 mins | 2009 | European journal of medicinal chemistry, Mar, Volume: 44, Issue:3 | Design and synthesis of 5-alkoxy-[1,2,4]triazolo[4,3-a]quinoline derivatives with anticonvulsant activity. |
AID113965 | Anticonvulsant activity was measured by maximal electroshock seizure test in mice by ip administration | 1998 | Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1 | Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. |
AID682347 | Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 4 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID286869 | Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs | 2007 | Journal of medicinal chemistry, May-17, Volume: 50, Issue:10 | Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach. |
AID418137 | Therapeutic index, ratio of TD50 for ip dosed mouse to ED50 for protection against subcutaneous metrazole-induced seizure in ip dosed mouse | 2009 | Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7 | Antiseizure activity of novel gamma-aminobutyric acid (A) receptor subtype-selective benzodiazepine analogues in mice and rat models. |
AID682353 | Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 30 mg/kg, ip after 4 hrs | 2012 | European journal of medicinal chemistry, Nov, Volume: 57 | Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity. |
AID364303 | Central nervous system depressant activity in Wistar rat assessed as immobility time at 30 mg/kg, ip after 1 hr by forced swim pool test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID490610 | Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizures | 2010 | European journal of medicinal chemistry, Jul, Volume: 45, Issue:7 | Design and synthesis of 10-alkoxy-5, 6-dihydro-triazolo[4,3-d]benzo[f][1,4]oxazepine derivatives with anticonvulsant activity. |
AID709892 | Stability in human liver microsomes assessed as diol formation at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22 | Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives. |
AID364296 | Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 4 hrs by rotarod test | 2008 | European journal of medicinal chemistry, Sep, Volume: 43, Issue:9 | CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones. |
AID1195114 | Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse by subcutaneous pentylenetetrazole test | 2015 | Bioorganic & medicinal chemistry, May-15, Volume: 23, Issue:10 | Design, synthesis and biological evaluation of new hybrid anticonvulsants derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives. |
AID489276 | Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause toxicity after 0.5 hrs | 2010 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 20, Issue:14 | Novel semicarbazones based 2,5-disubstituted-1,3,4-oxadiazoles: one more step towards establishing four binding site pharmacophoric model hypothesis for anticonvulsant activity. |
AID625291 | Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal | 2011 | PLoS computational biology, Dec, Volume: 7, Issue:12 | Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps). |
AID109719 | Anticonvulsant activity after intraperitoneal injection into mice measured in a maximal electroshock scree (MES) screen | 1996 | Journal of medicinal chemistry, Sep-27, Volume: 39, Issue:20 | (Aryloxy)aryl semicarbazones and related compounds: a novel class of anticonvulsant agents possessing high activity in the maximal electroshock screen. |
AID628628 | Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against maximal electroshock after 0.5 hrs | 2011 | European journal of medicinal chemistry, Sep, Volume: 46, Issue:9 | Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs. |
AID298031 | Lipophilicity, log D at pH7.4 | 2007 | Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19 | High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery. |
AID1159607 | Screen for inhibitors of RMI FANCM (MM2) intereaction | 2016 | Journal of biomolecular screening, Jul, Volume: 21, Issue:6 | A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway. |
AID540299 | A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis | 2010 | Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21 | Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis. |
AID588519 | A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities | 2011 | Antiviral research, Sep, Volume: 91, Issue:3 | High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors. |
AID1159550 | Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening | 2015 | Nature cell biology, Nov, Volume: 17, Issue:11 | 6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling. |
AID1224864 | HCS microscopy assay (F508del-CFTR) | 2016 | PloS one, , Volume: 11, Issue:10 | Increasing the Endoplasmic Reticulum Pool of the F508del Allele of the Cystic Fibrosis Transmembrane Conductance Regulator Leads to Greater Folding Correction by Small Molecule Therapeutics. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 2756 (25.05) | 18.7374 |
1990's | 2297 (20.87) | 18.2507 |
2000's | 2556 (23.23) | 29.6817 |
2010's | 2642 (24.01) | 24.3611 |
2020's | 753 (6.84) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (110.08) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1,128 (9.41%) | 5.53% |
Reviews | 1,217 (10.15%) | 6.00% |
Case Studies | 2,747 (22.91%) | 4.05% |
Observational | 45 (0.38%) | 0.25% |
Other | 6,855 (57.16%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
Phase IV Open Non Comparative Trial to Evaluate Efficacy and Safety of Tegretol® in Diabetes Neuropathy Pain. [NCT01089855] | Phase 4 | 123 participants (Actual) | Interventional | 2009-12-31 | Completed | ||
A Randomized Controlled Trial of Generic Substitution of Antiepileptic Drugs [NCT02429596] | Phase 4 | 200 participants (Anticipated) | Interventional | 2012-05-31 | Recruiting | ||
Efficacy and Tolerability of Low vs. Standard Daily Doses of Antiepileptic Drugs in Newly Diagnosed, Previously Untreated Epilepsy (STANDLOW). A Multicenter, Randomized, Single-blind, Parallel-group Trial [NCT03689114] | Phase 4 | 374 participants (Anticipated) | Interventional | 2020-01-07 | Not yet recruiting | ||
A SINGLE CENTER, OPEN LABEL, FIXED SEQUENCE, TWO-PERIOD STUDY TO INVESTIGATE THE EFFECT OF MULTIPLE DOSE CARBAMAZEPINE ON SINGLE DOSE PHARMACOKINETICS OF RO4917838 IN HEALTHY MALE VOLUNTEERS [NCT01365403] | Phase 1 | 16 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
[NCT01382017] | 18 participants (Actual) | Interventional | 2011-06-30 | Completed | |||
PHASE II STUDY TO EVALUATE EFFICACY AND SAFETY OF CARBAMAZEPINE FOR THE PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING. [NCT01581918] | Phase 2 | 43 participants (Anticipated) | Interventional | 2011-12-31 | Recruiting | ||
An Interventional, Phase 1, Open-Label, Fixed Sequence, 2-Period Study to Estimate the Effect of Multiple Doses of Carbamazepine on the Pharmacokinetics of Single Dose Vepdegestrant (ARV-471, PF-07850327) 200 mg Under the Fed Condition in Healthy Adult Ma [NCT06005688] | Phase 1 | 12 participants (Actual) | Interventional | 2023-08-18 | Active, not recruiting | ||
A Phase 1, Single-Center, Open-Label, 2-Cohort, Fixed-Sequence, Drug-Drug Interaction Study to Assess the Pharmacokinetics of DC-806 When Orally Administered Alone, When Coadministered With Itraconazole, and When Coadministered With Carbamazepine in Healt [NCT05994807] | Phase 1 | 33 participants (Actual) | Interventional | 2023-08-08 | Completed | ||
Role of Clinical Pharmacists in Epilepsy Management at a General Hospital in Vietnam: A Before-and-after Study [NCT04967326] | Phase 4 | 141 participants (Actual) | Interventional | 2016-01-01 | Completed | ||
A Phase 1, Single-Center, Nonrandomized, Open-Label, 2-Part, Fixed-Sequence, Drug-Drug Interaction Study to Assess the Pharmacokinetics and Safety of AZD4205 When Orally Administered Alone, When Coadministered With Itraconazole, and When Coadministered Wi [NCT05486949] | Phase 1 | 32 participants (Actual) | Interventional | 2022-07-27 | Completed | ||
A Single Centre, Open-label Study With Healthy Adult Volunteers to Determine the Effects of Single-dose and Steady-state TPV/r 500/200 mg on the Steady-state Pharmacokinetics of Carbamazepine (200 mg Twice Daily) [NCT02253849] | Phase 1 | 28 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
A Phase 1, 3-arm, Open-label, Sequential Design Study to Investigate the Effect of Multiple Doses of Itraconazole, Gemfibrozil, or Carbamazepine on Single-dose Pharmacokinetics of BMS-986278 in Healthy Participants [NCT05932303] | Phase 1 | 47 participants (Actual) | Interventional | 2023-07-12 | Completed | ||
CSP #428 - Treatment of Seizures in the Elderly Population [NCT00007670] | Phase 3 | 720 participants | Interventional | 1998-01-31 | Completed | ||
A Phase 1, Two-part, Open-label, Fixed-sequence Study to Evaluate the Effects of Multiple Doses of Itraconazole and Carbamazepine on the Single-dose Pharmacokinetics of LY3410738 in Healthy Adult Subjects [NCT05205447] | Phase 1 | 27 participants (Actual) | Interventional | 2022-01-05 | Terminated(stopped due to Data from part 2 no longer deemed necessary for this program.) | ||
Comparative Study of Zonisamide and Carbamazepine as an Initial Monotherapy: Efficacy and Safety Evaluation [NCT01127256] | Phase 4 | 200 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
Assessment of the Inter-patient Variability in Clinical Response and Correlated Genetic Variations in Substance Use Disorders [NCT05833399] | 200 participants (Anticipated) | Observational | 2022-11-28 | Recruiting | |||
A NON-RANDOMIZED, OPEN-LABEL, THREE-PART, DRUG-DRUG INTERACTION STUDY TO EVALUATE THE EFFECTS OF ITRACONAZOLE, CARBAMAZEPINE, AND QUINIDINE ON THE PHARMACOKINETICS AND SAFETY OF EDP-235 IN HEALTHY PARTICIPANTS [NCT05594602] | Phase 1 | 36 participants (Actual) | Interventional | 2022-10-06 | Completed | ||
Lamotrigine in Trigeminal Neuralgia: Efficacy and Safety in Comparison With Carbamazepine [NCT00913107] | Phase 2/Phase 3 | 21 participants (Actual) | Interventional | 2007-09-30 | Completed | ||
Carbamazepine for the Treatment of Chronic Post-Traumatic Brain Injury Irritability and Aggression: A 42-Day, Single-Site, Forced-Titration, Parallel Group, Randomized, Double-Blind, Placebo Controlled Trial [NCT00621751] | 70 participants (Actual) | Interventional | 2008-02-29 | Completed | |||
A Randomised Controlled Trial of the Ketogenic Diet in the Treatment of Epilepsy in Children Under the Age of Two Years [NCT02205931] | Phase 4 | 160 participants (Anticipated) | Interventional | 2015-01-31 | Recruiting | ||
Effect of Anti-epileptic Drugs on Etonogestrel-releasing Implant Pharmacokinetics in Women With Epilepsy [NCT03307863] | Phase 4 | 69 participants (Anticipated) | Interventional | 2017-11-01 | Recruiting | ||
Open-label, Fixed Sequence Crossover Study to Investigate the Effects of Carbamazepine on the Pharmacokinetics of Elinzanetant (BAY 3427080) in Healthy Participants. [NCT05028608] | Phase 1 | 16 participants (Actual) | Interventional | 2021-09-06 | Completed | ||
Characterization of Epilepsy Patients At-risk for Adverse Outcomes Related to Switching Antiepileptic Drug Products: BEEP 2b Study [NCT02707965] | Phase 1 | 21 participants (Actual) | Interventional | 2017-06-08 | Completed | ||
A Phase 1 Study to Evaluate the Potential Drug Interactions Between ALXN2080 and Itraconazole, Fluconazole, and Carbamazepine in Healthy Adult Participants [NCT06173596] | Phase 1 | 60 participants (Anticipated) | Interventional | 2023-12-21 | Not yet recruiting | ||
Fed Bioequivalence Study of Carbamazepine Controlled Release Formulations in Healthy Male Uruguayan Subjects [NCT02132897] | Phase 1 | 20 participants (Actual) | Interventional | 2014-05-31 | Completed | ||
The Efficacy and Safety of First-Line Anti-Epileptic Drugs (AEDs) as Substitution Therapy in Children Who Are Resistant to Second-Line AEDs [NCT05697614] | Phase 4 | 100 participants (Anticipated) | Interventional | 2023-03-01 | Recruiting | ||
Efficacy and Tolerability of the Combination of LIthium and CArbamazepine Compared to Lithium and VALproic Acid in the Treatment of Young Bipolar Patients [NCT00976794] | Phase 4 | 40 participants (Actual) | Interventional | 2009-01-31 | Completed | ||
A Phase 1, Open-label, Fixed-Sequence Trial to Evaluate the Effect of Carbamazepine on the Single-Dose Pharmacokinetics of Darigabat in Healthy Adult Participants [NCT05824143] | Phase 1 | 13 participants (Actual) | Interventional | 2023-04-17 | Completed | ||
Efficacy and Safety of Olanzapine in the Extended Treatment for Manic or Mixed Episode of Bipolar I Disorder [NCT00266630] | Phase 3 | 139 participants (Actual) | Interventional | 2005-11-30 | Completed | ||
Treatment for Bipolar Depression: Acute & Prophylactic Efficacy With Citalopram [NCT00562861] | Phase 2/Phase 3 | 119 participants (Actual) | Interventional | 2007-11-30 | Completed | ||
Effect of Carbamazepine and Oxcarbazepine on Serum Neuron-specific Enolase and S100B in Focal Seizures [NCT02705768] | Phase 4 | 90 participants (Actual) | Interventional | 2016-04-30 | Completed | ||
A Double Blind Study To Evaluate the Dose Tolerance and Safety of Equetro (Carbamazepine) Versus Placebo Followed by a Long-Term Maintenance in Children and Adolescents Aged 10-17 Years With Acute Manic or Mixed Bipolar I Disorder [NCT02623504] | Phase 4 | 17 participants (Actual) | Interventional | 2016-10-24 | Terminated(stopped due to No apparent therapeutic effects that was superior to placebo) | ||
An Open, Randomized, Multicenter Comparative Clinical Trial of Lamotrigine or Carbamazepine for Cognitive Function as Initial Monotherapy in Adult Untreated Epilepsies [NCT00896987] | Phase 4 | 121 participants (Actual) | Interventional | 2006-05-31 | Completed | ||
A Sequential, Open-Label Study of the Pharmacokinetics and Safety of Intravenous Carbamazepine Relative to Oral Carbamazepine in Adult Patients With Epilepsy [NCT01079351] | Phase 1 | 98 participants (Actual) | Interventional | 2007-04-30 | Completed | ||
A Randomized, Double-Blind Extension Study To Assess The Long-Term Safety And To Explore The Long-Term Efficacy Of Zonisamide As Monotherapy In Newly Diagnosed Partial Seizures [NCT00848549] | Phase 3 | 295 participants (Actual) | Interventional | 2008-10-31 | Completed | ||
Assessment of Marketed AEDs in the Human Photosensitivity Proof of Concept Trial [NCT00894010] | Phase 2 | 6 participants (Actual) | Interventional | 2009-05-31 | Completed | ||
Open-Label Study to Assess the Safety and Tolerability of Intravenous Carbamazepine as Short-Term Replacement of Oral Carbamazepine in Adult Patients With Epilepsy [NCT01128959] | Phase 3 | 108 participants (Actual) | Interventional | 2010-06-30 | Completed | ||
A Single-center, Prospective, Randomized, Positive Controlled, Parallel Design Trial to Compare the Efficacy of Acupuncture Therapy and Carbamazepine Oral Dosage in Patients With Carpal Tunnel Syndrome by Multiple Excitability Test [NCT00952432] | 80 participants (Anticipated) | Interventional | 2009-05-31 | Recruiting | |||
Evaluation of the Effect of Food, Omeprazole, Itraconazole, and Carbamazepine on the Pharmacokinetics of LY3484356 in Healthy Females of Non-Child-Bearing Potential [NCT04840888] | Phase 1 | 82 participants (Actual) | Interventional | 2021-04-26 | Completed | ||
A Phase IIIb, Open Label Observational Study of SPD417 Used in Combination With Other Psychotropic Medications for the Treatment of Bipolar I Disorder [NCT00150605] | Phase 3 | 50 participants | Interventional | 2005-02-28 | Completed | ||
Randomised, Placebo Controlled, Double Blind, Parallel Group 3-Months Study of Carbamazepine Efficacy in Moderate Persistent and Severe Asthma Therapy [NCT00153296] | Phase 4 | 68 participants | Interventional | 2004-08-31 | Completed | ||
A Cross-sectional, Comparative, Multi-center Study to Investigate the Effect of Topiramate Monotherapy on Markers of Bone Mineral Metabolism and Bone Mineral Density in Premenopausal Women With Epilepsy [NCT01030094] | 140 participants (Actual) | Observational | 2007-02-28 | Completed | |||
A Three-Part Phase 1 Study to Evaluate the Potential Drug-Drug Interactions Between Vemircopan and Rosuvastatin, Metformin, Levonorgestrel-Ethinyl Estradiol-Containing Oral Contraceptives, and Carbamazepine in Healthy Adult Participants [NCT06071442] | Phase 1 | 60 participants (Anticipated) | Interventional | 2023-10-09 | Recruiting | ||
Randomized, Placebo Controlled, Double Blind Study of Carbamazepine in Treatment of Bronchial Asthma [NCT00207428] | Phase 4 | 65 participants | Interventional | 1999-08-31 | Completed | ||
Second-Line Treatment Choice for Epilepsy [NCT00208520] | 60 participants | Interventional | 2003-07-31 | Active, not recruiting | |||
Randomised Factorial Design Controlled Trial Comparing Carbamazepine, Levetiracetam or Active Monitoring Combined With or Without Sleep Behaviour Intervention in Treatment Naive Children With Rolandic Epilepsy [NCT04610879] | Phase 4 | 5 participants (Actual) | Interventional | 2019-08-02 | Terminated(stopped due to Following the internal pilot, the study did not meet prespecified stop/go criteria for continuation.) | ||
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371] | 1,037,352 participants (Actual) | Observational | 2016-09-30 | Completed | |||
Evaluation of the Effect of Carbamazepine on the Steady-state Pharmacokinetics of Paliperidone Extended Release in Clinically Stable Subjects With Schizophrenia or Bipolar I Disorder [NCT00892125] | Phase 1 | 64 participants (Actual) | Interventional | 2006-09-30 | Completed | ||
Phase I, Open-Label, Single-sequence, Cross-Over Study of the Effect of Multiple Doses of Carbamazepine on Single-Dose Tepotinib Pharmacokinetics in Healthy Participants [NCT05213481] | Phase 1 | 18 participants (Actual) | Interventional | 2021-12-15 | Completed | ||
A First-in-Human Multi-Part Phase 1 Study in Healthy Volunteers to Evaluate the Safety, Tolerability, Pharmacokinetics, and Drug-Drug Interaction Potential of Single and Multiple Doses of ALG-097558 [NCT05840952] | Phase 1 | 144 participants (Anticipated) | Interventional | 2023-07-04 | Recruiting | ||
Double-Blind, Randomized, Two Period Crossover Comparison of the Cognitive and Behavioral Effects of Eslicarbazepine Acetate and Carbamazepine in Healthy Adults [NCT02912364] | Phase 4 | 46 participants (Actual) | Interventional | 2016-07-31 | Completed | ||
[NCT00004758] | Phase 2 | 30 participants | Interventional | 1993-11-30 | Completed | ||
Multicenter, Comparative, Randomized, Open Trial to Evaluate Efficacy and Safety of Levetiracetam Versus Carbamazepine in Post Stroke Late Onset Crisis [NCT00542802] | Phase 3 | 630 participants (Anticipated) | Interventional | 2007-09-30 | Recruiting | ||
The Effect of Single Dose Carbamazepine on the Pharmacokinetics of Single Dose Nevirapine (Viramune, NVP) and Development of NVP Resistance, PMTCT Program of Moshi, Tanzania (VITA1) [NCT00294892] | Phase 2 | 144 participants (Actual) | Interventional | 2006-02-28 | Completed | ||
Carbamazepine and Lorazepam in Outpatient Detoxification [NCT00000441] | Phase 4 | 0 participants | Interventional | Completed | |||
A Phase 1 Study to Evaluate the Effects of Multiple Doses of Itraconazole or Carbamazepine on the Single-Dose Pharmacokinetics of LY3537982 in Healthy Adult Subjects [NCT05860933] | Phase 1 | 30 participants (Anticipated) | Interventional | 2023-05-08 | Recruiting | ||
A Phase IV, Multi-Center, Open-Label, Safety and Effectiveness Study of Extended-Release Carbamazepine in the Treatment of Mania in Children and Adolescents Aged 10-17 Years With Acute Manic or Mixed Bipolar I Disorder. [NCT00350857] | Phase 4 | 161 participants (Actual) | Interventional | 2006-07-31 | Completed | ||
A Multicenter, Double-blind, Double-dummy, Randomized, Positive- Controlled Study Comparing the Efficacy and Safety of Lacosamide (200 to 600 mg/Day) to Controlled Release Carbamazepine (400 to 1200 mg/Day), Used as Monotherapy in Subjects (≥ 16 Years) Ne [NCT01243177] | Phase 3 | 888 participants (Actual) | Interventional | 2011-04-30 | Completed | ||
A Phase 1, Open-label, Fixed-sequence, Crossover Trial to Evaluate the Effects of Cytochrome P450 (CYP) 3A4 Induction by Carbamazepine on the Steady-state Pharmacokinetics of Tavapadon in Healthy Adult Participants [NCT05581823] | Phase 1 | 16 participants (Actual) | Interventional | 2022-10-19 | Completed | ||
A Randomized, Multi-centre, Double-blind Study, to Compare the Efficacy and Safety of Zonisamide and Carbamazepine as Monotherapy, in Newly Diagnosed Partial Epilepsy [NCT00477295] | Phase 3 | 583 participants (Actual) | Interventional | 2007-05-31 | Completed | ||
Olanzapine Plus Carbamazepine Versus Carbamazepine Alone in the Treatment of Manic or Mixed Episodes Associated With Bipolar I Disorder [NCT00190892] | Phase 4 | 120 participants | Interventional | 2004-09-30 | Completed | ||
Carbamazepine Extended-Release for the Treatment of Bipolar Depression [NCT00203567] | Phase 4 | 25 participants (Actual) | Interventional | 2005-08-31 | Completed | ||
Pharmacotherapy and Intensive Treatment [NCT00000218] | Phase 4 | 353 participants | Interventional | Completed | |||
A Multicenter, Randomized, Double-blind, Double-dummy, 2-period Crossover Study of Neuropsychological Effects of Lacosamide and Carbamazepine Immediate Release in Healthy Subjects [NCT01530022] | Phase 1 | 60 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Pilot Study on the Response of Inherited Erythromelalgia Patients With NaV1.7 Mutations to Carbamazepine: Clinical Imaging Study [NCT02214615] | Phase 4 | 2 participants (Actual) | Interventional | 2014-04-30 | Completed | ||
Carbamazepine Treatment for Cocaine Dependence [NCT00000191] | Phase 2 | 0 participants | Interventional | 1991-01-31 | Completed | ||
A Phase IIIb, Randomized, Double-Blind, Parallel Group Study in Bipolar I Patients to Assess the Efficacy and Safety of SPD417 Administered Once Daily vs Twice Daily in the Treatment of Manic Symptoms [NCT00150553] | Phase 3 | 102 participants | Interventional | 2005-01-31 | Completed | ||
A Therapeutic Confirmatory, Open-label, Multi-center, Randomized 2 Parallel Groups, Community-based Trial Studying the Efficacy and Safety of Levetiracetam (1000 to 3000 mg/Day Oral Tablets 250-500 mg b.i.d.) Compared to Sodium Valproate (1000 to 2000 mg/ [NCT00175903] | Phase 3 | 1,701 participants (Actual) | Interventional | 2005-02-28 | Completed | ||
Open-Label Study of Equetro for the Treatment of Mania in Children Ages 6-12 With Bipolar I, Bipolar II, and Bipolar Spectrum Disorder [NCT00181870] | Phase 4 | 33 participants (Actual) | Interventional | 2005-07-31 | Completed | ||
A Multicentre, Double-blind, Randomized, Phase IV Clinical Trial Comparing the Safety, Tolerability and Efficacy of Levetiracetam Versus Lamotrigine and Carbamazepine in the Oral Antiepileptic Therapy of Newly Diagnosed Elderly Patients With Focal Epileps [NCT00438451] | Phase 4 | 361 participants (Actual) | Interventional | 2007-01-31 | Completed | ||
Effect of Sleeve Gastroctomy on Pharmacokinetics of Paracetamol and Antiepileptic Drugs [NCT03161509] | Phase 4 | 2 participants (Actual) | Interventional | 2017-07-01 | Terminated(stopped due to publication of better study) | ||
Comparison of Different Antiepileptic Drug Monotherapies for the Occurrence of Premenstrual Dysphoric Disorder Among Women With Epilepsy [NCT00612235] | 80 participants (Actual) | Observational | 2008-04-30 | Completed | |||
An Open Label, Randomized, Multicenter Clinical Trial to Compare the Efficacy and Safety of Lamotrigine / Valproate Coadministration and Carbamazepine as Initial Pharmacotherapy in Epilepsies (Phase Ⅳ) [NCT00807989] | Phase 4 | 207 participants (Actual) | Interventional | 2008-03-31 | Completed | ||
Pharmacokinetic Interaction Study Between Eslicarbazepine Acetate and Carbamazepine in Healthy Subject [NCT02284854] | Phase 1 | 43 participants (Actual) | Interventional | 2009-07-31 | Completed | ||
Induction of Drug Metabolism: A Comparative, Pharmacokinetic in Vivo Study of the Effect of Carbamazepine and Oxcarbazepine on CYP3A4. [NCT00260247] | Phase 4 | 10 participants (Actual) | Interventional | 2005-04-30 | Completed | ||
TOPAMAX (Topiramate) Monotherapy Comparison Trial to Standard Monotherapy in the Treatment of Newly Diagnosed Epilepsy (RWJ-17021-000); Phase IIIB [NCT00236717] | Phase 3 | 865 participants (Actual) | Interventional | 1997-09-30 | Completed | ||
A Single-Center, Open-Label, One-Sequence, Crossover Study to Investigate the Effects of Multiple Doses of Carbamazepine on the Pharmacokinetics of a Single Dose RO4917523 in Healthy Subjects [NCT01629368] | Phase 1 | 16 participants (Actual) | Interventional | 2012-06-30 | Completed | ||
A Phase I, Open-label, Randomized, 2-panel, Sequential Treatment Study in Healthy Subjects to Investigate the Potential Pharmacokinetic Interactions Between Multiple Doses of Phenytoin or Carbamazepine and Telaprevir at Steady-state [NCT01635829] | Phase 1 | 24 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
A Phase 1 Open-Label Study to Evaluate the Effect of CYP450 and P-gp Inhibition and Induction on the Pharmacokinetics of Pomalidomide (CC-4047) in Healthy Male Subjects [NCT01707407] | Phase 1 | 32 participants (Actual) | Interventional | 2012-09-01 | Completed | ||
The Effect of Multiple Doses of Carbamazepine on the Pharmacokinetics of a Single Oral Dose of BI 1810631 in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Trial) [NCT06028464] | Phase 1 | 16 participants (Actual) | Interventional | 2023-09-11 | Completed | ||
Assessment of Cost- Effectiveness Interventions and the Quality of Life in Patients With Mood Disorders Through Resources Available in Brazilian Public Health [NCT02870283] | Phase 4 | 107 participants (Actual) | Interventional | 2010-05-31 | Completed | ||
A Preliminary Study of the Efficacy and Safety of Carbamazepine in Severe Liver Disease Due to Alpha-1 Antitrypsin Deficiency [NCT01379469] | Phase 2 | 20 participants (Actual) | Interventional | 2012-01-31 | Terminated | ||
[NCT00381537] | 92 participants | Interventional | Completed | ||||
A Phase 1, Single-Center, Nonrandomized, Open-Label, 2-Part, Fixed-Sequence, Drug-Drug Interaction Study to Assess the Pharmacokinetics of DZD9008 When Orally Administered Alone, When Coadministered With Itraconazole, and When Coadministered With Carbamaz [NCT05418582] | Phase 1 | 40 participants (Actual) | Interventional | 2022-01-25 | Completed | ||
A PHASE 1, OPEN-LABEL, FIXED SEQUENCE, 2-PERIOD CROSSOVER STUDY TO ESTIMATE THE EFFECT OF CARBAMAZEPINE ON THE PHARMACOKINETICS OF PF-07321332 BOOSTED WITH RITONAVIR IN HEALTHY PARTICIPANTS [NCT04962230] | Phase 1 | 12 participants (Actual) | Interventional | 2021-07-15 | Completed | ||
Symptomatic Trigeminal Neuralgia Attributed to Multiple Sclerosis - Clinical Characteristics, Neuroanatomical Abnormalities and Treatment Efficacy [NCT04371575] | 60 participants (Actual) | Observational | 2012-09-01 | Completed | |||
A Phase 1 Study Assessing the Effect of Carbamazepine, a P-Glycoprotein Inducer, on the Pharmacokinetics of AT-527 in Healthy Adult Subjects [NCT04784000] | Phase 1 | 20 participants (Actual) | Interventional | 2021-03-01 | Completed | ||
A Non-Randomized, Open-Label, Three-Part, Drug-Drug Interaction Study to Evaluate the Effects of Itraconazole, Carbamazepine, and Quinidine on the Pharmacokinetics and Safety of EDP-514 in Healthy Subjects [NCT04783753] | Phase 1 | 72 participants (Actual) | Interventional | 2020-11-05 | Completed | ||
Phase I, Open-Label, Single-Sequence Study of the Effect of Multiple Doses of Carbamazepine on Single-Dose Evobrutinib Pharmacokinetics in Healthy Participants [NCT05248945] | Phase 1 | 14 participants (Actual) | Interventional | 2022-01-13 | Completed | ||
The Role of Drug Metabolizing Enzymes in the Pathogenesis Adverse Drug Reactions in Children [NCT00224952] | 274 participants (Actual) | Observational | 2002-07-31 | Completed | |||
Open Label Prophylaxis Study of Lithium Plus Extended- Release Carbamazepine (Equetro®) Combination for Rapid Cycling Bipolar Disorder [NCT00325286] | Phase 4 | 20 participants (Anticipated) | Interventional | 2006-05-31 | Active, not recruiting | ||
Carbamazepine Treatment of Cocaine Dependence [NCT00000242] | Phase 2 | 0 participants | Interventional | 1992-10-01 | Completed | ||
Pharmacotherapy and Intensive Treatment of Drug Abuse [NCT00000217] | Phase 2 | 0 participants | Interventional | 1990-09-30 | Completed | ||
A Phase 1, Open-label, Parallel-group Study to Assess the Effect of Steady-state Carbamazepine on the Pharmacokinetics of Ponesimod in Healthy Adult Participants [NCT05552196] | Phase 1 | 28 participants (Actual) | Interventional | 2022-10-18 | Completed | ||
An Open-label, Single-sequence, Drug-drug Interaction Study to Evaluate the Effect of Steady-state Carbamazepine on the Single-dose Pharmacokinetics of Erdafitinib Tablets in Healthy Adult Subjects [NCT04330248] | Phase 1 | 15 participants (Actual) | Interventional | 2020-03-31 | Completed | ||
A Multicenter, Double-blind, Double-dummy, Follow up Study Evaluating the Long-term Safety of Lacosamide in Comparison With Controlled-release Carbamazepine Used as Monotherapy in Subjects With Partial-onset or Generalized Tonic-clonic Seizures ≥16 Years [NCT01465997] | Phase 3 | 551 participants (Actual) | Interventional | 2012-05-31 | Completed | ||
Comparative Efficacy of Carbamazepine Versus Oxcarbazepine in Treatment of Trigeminal Neuralgia- a Randomized Controlled Clinical Study [NCT04996199] | Phase 4 | 132 participants (Anticipated) | Interventional | 2021-09-18 | Recruiting | ||
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567] | Phase 3 | 407 participants (Actual) | Interventional | 2015-01-31 | Terminated | ||
Population Pharmacokinetics of Antiepileptic in Pediatrics [NCT03196466] | 1,000 participants (Anticipated) | Observational | 2017-06-19 | Recruiting | |||
An Open-label, Randomized, Parallel-group, Active-controlled Study Comparing the Efficacy and Safety of Levetiracetam to Carbamazepine Used as Monotherapy in Subjects Newly or Recently Diagnosed as Epilepsy and Partial-onset Seizures [NCT01954121] | Phase 3 | 436 participants (Actual) | Interventional | 2013-09-30 | Completed | ||
Electroacupuncture Therapy for Change of Pain in Classical Trigeminal Neuralgia [NCT03580317] | 120 participants (Actual) | Interventional | 2018-07-12 | Completed | |||
A Phase 1, Open-label, Three-Part, Fixed-Sequence Trial in Healthy Adult Participants to Evaluate the Effects of Itraconazole and Carbamazepine on the Single-Dose Pharmacokinetics of Emraclidine, and the Effect of Emraclidine on the Single-Dose Pharmacoki [NCT05965219] | Phase 1 | 60 participants (Anticipated) | Interventional | 2023-08-15 | Recruiting | ||
Pharmacological Mechanisms of Low-intensity Focused Ultrasound for Motor Cortex Neuroplasticity [NCT04923659] | Early Phase 1 | 20 participants (Anticipated) | Interventional | 2021-05-25 | Recruiting | ||
Electroclinical Effect of Steroid in Patients With Benign Childhood Epilepsy With Centrotemporal Spikes [NCT03490487] | Phase 4 | 100 participants (Anticipated) | Interventional | 2018-06-20 | Recruiting | ||
The Efficacy and Safety of Lamotrigine Versus Carbamazepine in Focal Epilepsy: A Randomized, Open Label Clinical Trial in Dhaka Medical College Hospital [NCT05748236] | Phase 4 | 70 participants (Anticipated) | Interventional | 2022-11-01 | Enrolling by invitation | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |