Page last updated: 2024-11-04

carbamazepine

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Description

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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

carbamazepine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine carrying a carbamoyl substituent at the azepine nitrogen, used as an anticonvulsant. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID2554
CHEMBL ID108
CHEBI ID3387
SCHEMBL ID21639
SCHEMBL ID19838283
MeSH IDM0003328

Synonyms (276)

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

Research Excerpts

Overview

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.

ExcerptReferenceRelevance
"Carbamazepine (CBZ) is a medication used commonly in epilepsy. "( Carbamazepine drug effect simulating biochemical central hypothyroidism in a patient with Bardet-Biedl syndrome.
Kishlyansky, D; Kline, G, 2021
)
3.51
"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, particularly in a massive overdose where serum protein binding is saturated. "( Combined Hemoperfusion and Continuous Veno-Venous Hemofiltration for Carbamazepine Intoxication.
Baldwin, I; Baylis, S; Bellomo, R; Costa-Pinto, R; Hodgson, S, 2022
)
2.4
"Carbamazepine is a medication used to treat a variety of neurological and psychiatric conditions including seizure disorders, neuropathic pain syndromes, and bipolar disorder. "( Neurologic toxicity of carbamazepine in treatment of trigeminal neuralgia.
Birdsong, S; Bridwell, RE; Brown, S; Clerkin, S; Long, B, 2022
)
2.47
"Carbamazepine is an antiepileptic drug used in the treatment of epilepsy, trigeminal neuralgia, and bipolar disorder. "( Acute lymphocytic leukemia in a patient with long-term carbamazepine exposure: Acute lymphoblastic leukemia that develops in a patient who has been using carbamazepine for a long time.
Bagci, M; Sayin, S, 2023
)
2.6
"Carbamazepine is an iminostilbene derivative. "( Acute lymphocytic leukemia in a patient with long-term carbamazepine exposure: Acute lymphoblastic leukemia that develops in a patient who has been using carbamazepine for a long time.
Bagci, M; Sayin, S, 2023
)
2.6
"Carbamazepine (CBZ) is a common antiepileptic drug that may cause overdoses with seizures as a common neurological manifestation. "( Stimulus-induced focal motor seizure in a pediatric patient with carbamazepine overdose.
Fujimoto, A; Kanai, S; Maegaki, Y; Nakamura, Y; Ohta, K; Okanishi, T, 2022
)
2.4
"Carbamazepine (CBZ) is an anticonvulsant with multiple neuropsychiatric indications."( Carbamazepine Therapy After Bariatric Surgery: Eight Sleeve Gastrectomy Cases and Review of the Literature.
Dahan, A; Lavon, O; Margolin, N; Porat, D, 2022
)
2.89
"Carbamazepine (CBZ) is an FDA-approved anticonvulsant that is widely used to treat epilepsy, bipolar disorder, trigeminal neuralgia and chronic pain. "( Development of label-free electrochemical impedance spectroscopy for the detection of HLA-B*15:02 and HLA-B*15:21 for the prevention of carbamazepine-induced Stevens-Johnson syndrome.
Attapong, J; Chomean, S; Kaset, C; Nakkam, N; Tassaneeyakul, W, 2022
)
2.37
"Carbamazepine (CBZ) is an anticonvulsant characterized by poor water solubility, nanonization can improve its bioavailability."( Nanonized carbamazepine for nose-to-brain delivery: pharmaceutical formulation development.
Bonaccorso, A; Di Martino, P; Gigliobianco, MR; Lombardo, R; Mancuso, A; Musumeci, T; Pellitteri, R, 2023
)
2.03
"Carbamazepine (CBZ) is an aromatic anticonvulsant known to cause drug hypersensitivity reactions, which range in severity from relatively mild maculopapular exanthema to potentially fatal Stevens-Johnson syndrome and toxic epidermal necrolysis (SJS-TEN). "( Characterization of Drug-Specific CD4
Alfirevic, A; Hammond, S; Jaruthamsophon, K; Naisbitt, DJ; Pirmohamed, M; Sukasem, C; Thomson, PJ; Zhang, E, 2023
)
2.35
"Carbamazepine (CBZ) is a FDA-approved antiepileptic drug and a histone deacetylase inhibitor."( Carbamazepine, a Histone Deacetylase Inhibitor Induces Apoptosis in Human Colon Adenocarcinoma Cell Line HT-29.
, 2020
)
2.72
"Carbamazepine (CBZ) is a widely used antiepileptic drug that has a potential impact on the environment due to its Physico-chemical properties, which are rarely eliminated in conventional water treatment."( Chronic Toxicological Effects of Carbamazepine on Daphnia magna Straus: Effects on Reproduction Traits, Body Length, and Intrinsic Growth.
Ahmad, Z; Tian, Y; Wang, J; Xia, X; Zhang, F; Zhu, L, 2019
)
1.52
"Carbamazepine (CBZ) is a typical pharmaceutical residue commonly found in aqueous environments, but its removal through activated carbon or advanced oxidation processes is often disrupted by co-existing organic matter. "( Removal of the environmental pollutant carbamazepine using molecular imprinted adsorbents: Molecular simulation, adsorption properties, and mechanisms.
Chen, LX; Chen, SL; He, Q; Liang, JJ; Liu, HX; Zhang, HJ; Zheng, HL, 2020
)
2.27
"Carbamazepine is a drug that is widely used in the treatment of epilepsy and bipolar disorder. "( Carbamazepine Enhances Adipogenesis by Inhibiting Wnt/β-catenin Expression.
Chau, GC; Im, DU; Kim, SC; Um, SH, 2019
)
3.4
"Carbamazepine is a commonly used iminostilbene antiepileptic medication and it is estimated that 46.9% of the total antiepileptic drug overdose in the United Kingdom is because of this drug. "( Carbamazepine-induced hyperglycemia: A rare case report.
Devasree, S; Harika, V; Parveen, S; Varma, KVS; Venkatasubbaiah, M,
)
3.02
"Carbamazepine (CBZ) is an anticonvulsant medication with highly persistent properties in the aquatic environment, where it has the potential to affect nontarget biota. "( Carbamazepine Ozonation Byproducts: Toxicity in Zebrafish (
Carlsson, G; Eriksson, J; Glynn, A; Golovko, O; Örn, S; Pohl, J; Weiss, J, 2020
)
3.44
"Carbamazepine (CBZ) is an anticonvulsant pharmaceutical compound of environmental concern due to its persistence, bioactive toxicity, and teratogenic effects. "( Phytotransformation and Metabolic Pathways of
Cheng, Y; Ding, T; Li, J; Li, M; Wang, H; Wang, W; Ye, Q, 2020
)
2
"Carbamazepine (CBZ) is a recalcitrant pharmaceutical often detected in wastewater and in the environment. "( Ozonation of carbamazepine and its main transformation products: product determination and reaction mechanisms.
Eklund, P; Kråkström, M; Kronberg, L; Kumar, N; Saeid, S; Salmi, T; Tolvanen, P, 2020
)
2.37
"Carbamazepine is an effective drug for treating seizures and trigeminal neuralgia. "( Development and Validation of a Free Carbamazepine Assay on an Automated Chemistry Analyzer.
Bowers, K; Boyert, N; McShane, AJ; Mitro, M; Tang, X; Zhang, X, 2020
)
2.27
"Carbamazepine (CBZ) is a widely employed anti-seizure medication that crosses the blood-brain barrier (BBB) to exert its anti-convulsant action. "( Carbamazepine induces a bioenergetics disruption to microvascular endothelial cells from the blood-brain barrier.
Al-Ghafari, A; Alelwani, W; Alnajeebi, AM; Babteen, NA; Carter, WG; Elmorsy, E; Kattan, SW, 2020
)
3.44
"Carbamazepine (CBZ) is a poorly water soluble drug owing to the Biopharmaceutic Classification System (BCS) class II. "( 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
)
2.22
"Carbamazepine is an antiepileptic drug that is not easily degraded in the environment. "( Adsorption and removal of a selected emerging contaminant,
Alaghmand, M; Alizadeh-Saei, J; Barakat, S, 2020
)
2
"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
"Carbamazepine is an effective and promising drug for initial monotherapy of FE. "( [The efficacy and tolerability of extended release carbamazepine in adult patients with new-onset epilepsy using epileptiform activity index].
Karlov, VA; Kozhokaru, AB; Orlova, AS; Vlasov, PN, 2021
)
2.32
"Carbamazepine (CBZ) is a widely used anti-epileptic drug that has been detected in wastewaters from sewage treating plants and thus appears in rivers, streams and other water bodies. "( Antioxidative response of lettuce (Lactuca sativa) to carbamazepine-induced stress.
Carvalho, L; Leitão, I; Marques, MM; Martins, LL; Mourato, MP; Oliveira, MC, 2021
)
2.31
"Carbamazepine (CBZ) is an anticonvulsant drug that usually is used for the treatment of seizures. "( Exercise Improved the Anti-Epileptic Effect of Carbamazepine through GABA Enhancement in Epileptic Rats.
Barzroodi Pour, M; Bayat, M; Karimzadeh, F; Navazesh, A; Soleimani, M, 2021
)
2.32
"Carbamazepine (CBZ) is a wildly used anti-epileptic drug (AED). "( Association of EPHX1 polymorphisms with plasma concentration of carbamazepine in epileptic patients: Systematic review and meta-analysis.
Hu, T; Liu, J; Tian, T; Zeng, X, 2021
)
2.3
"Carbamazepine (CBZ) is a commonly used anti-epileptic in rural hospitals in India. "( Determination of serum carbamazepine concentration using dried blood spot specimens for resource-limited settings.
Alexander, M; Das, S; Fleming, DH; Mathew, BS; Prabhakar, AT; Winston A, B, 2017
)
2.21
"Carbamazepine (CBZ) is an active pharmaceutical ingredient used in the treatment of epilepsy that can form at least 5 polymorphic forms. "( Spray Drying as a Reliable Route to Produce Metastable Carbamazepine Form IV.
Bhardwaj, RM; Briggs, NEB; Brown, CJ; Dunn, J; Florence, AJ; Halliwell, RA; Nordon, A; Robertson, J, 2017
)
2.15
"Carbamazepine (CBZ) is an antiepileptic drug which is persistent in wastewater treatment plants and the environment. "( Extensive Transformation of the Pharmaceutical Carbamazepine Following Uptake into Intact Tomato Plants.
Moeder, M; Reemtsma, T; Riemenschneider, C; Schwarz, D; Seiwert, B, 2017
)
2.15
"Carbamazepine (CBZ) is an effective antiepileptic drug that has been associated with hypersensitivity reactions. "( Mass Spectrometric Characterization of Circulating Covalent Protein Adducts Derived from Epoxide Metabolites of Carbamazepine in Patients.
Jenkins, RE; Maggs, JL; Marlot, PT; Marson, AG; Meng, X; Park, BK; Pirmohamed, M; Yip, VLM, 2017
)
2.11
"Carbamazepine (CBZ) is a pharmaceutical frequently categorized as a recalcitrant pollutant in the aquatic environment. "( Metabolism of carbamazepine in plant roots and endophytic rhizobacteria isolated from Phragmites australis.
Harpaintner, R; May, R; Poschenrieder, C; Sauvêtre, A; Schröder, P, 2018
)
2.28
"IV carbamazepine is a reasonable option for adults with generalized tonic-clonic or focal seizures, previously stabilized on oral carbamazepine, who are unable to tolerate oral medications for up to 7 days. "( Intravenous Carbamazepine for Adults With Seizures.
DeFalco, AP; Tillery, EE; Vickery, PB, 2018
)
1.48
"Carbamazepine (CBZ) is a common cause of life-threatening cutaneous adverse drug reactions such as Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). "( Association of the HLA-B alleles with carbamazepine-induced Stevens-Johnson syndrome/toxic epidermal necrolysis in the Javanese and Sundanese population of Indonesia: the important role of the HLA-B75 serotype.
Cavallari, LH; Kristin, E; Mahasirimongkol, S; Menaldi, SL; Prayuni, K; Sachrowardi, Q; Suyatna, FD; Wichukchinda, N; Yuliwulandari, R, 2017
)
2.17
"Carbamazepine (CBZ) is a commonly prescribed antiepileptic drug, and is mainly metabolized to 10,11-CBZ epoxide in humans. "( Carbamazepine 10,11-epoxidation in human liver microsomes: influence of the
Hanioka, N; Isobe, T; Miyata-Nozaka, Y; Shigeyama, M; Taguchi, M; Zain, SM, 2017
)
3.34
"Carbamazepine (CBZ) is an antiepileptic drug, which also could be used in the treatment of neurodegenerative diseases, such as the Alzheimer's disease. "( PAMAM dendrimers as a carbamazepine delivery system for neurodegenerative diseases: A biophysical and nanotoxicological characterization.
Alonso, SDV; Igartúa, DE; Martinez, CS; Prieto, MJ; Temprana, CF, 2018
)
2.24
"Carbamazepine (CBZ) is a widely used antiepileptic drug with large interindividual variability in serum concentrations. "( Effects of CYP3A5 and UGT2B7 variants on steady-state carbamazepine concentrations in Chinese epileptic patients.
Huang, YT; Lu, Q; Qu, J; Qu, Q; Shu, Y; Xiang, DX; Xu, P, 2018
)
2.17
"Carbamazepine is a valuable pharmacological agent prescribed in treatment of epilepsy and trigeminal neuralgia. "( Multifunctional carbamazepine loaded nanostructured lipid carrier (NLC) formulation.
Abdel-Bakky, MS; Ali, HM; Badran, MM; Elmowafy, M; Ibrahim, HM; Shalaby, K, 2018
)
2.27
"Carbamazepine is a current first-line treatment for focal onset seizures, and is used in the USA and Europe."( Carbamazepine versus phenobarbitone monotherapy for epilepsy: an individual participant data review.
Marson, AG; Nevitt, SJ; Tudur Smith, C, 2018
)
2.64
"Carbamazepine treatment is a protective factor against uncontrolled seizures for EAF. "( Factors predicting uncontrolled seizures in epilepsy with auditory features.
Chen, L; Zhang, L; Zhu, X; Zou, X, 2019
)
1.96
"Carbamazepine (CBZ) is a worldwide anti-epileptic drug, whose fate and migration can be greatly influenced by contact with dissolved organic matter (DOM). "( Insight into the binding properties of carbamazepine onto dissolved organic matter using spectroscopic techniques during grassy swale treatment.
An, Y; Guo, X; He, L; Wang, H; Yuan, D, 2019
)
2.23
"Carbamazepine (CAB) is a commonly detected pharmaceutical in the surface waters. "( Toxic effects and metabolic fate of carbamazepine in diatom Navicula sp. as influenced by humic acid and nitrogen species.
Ding, T; Li, J; Lin, K; Yang, B; Yang, M, 2019
)
2.23
"Carbamazepine (CBZ) is a widespread antiepileptic drug and due to its physical-chemical characteristics minimal removal is achieved in conventional water treatments, and thus has been suggested as a molecular marker of wastewater contamination in surface water and groundwater."( Carbamazepine is degraded by the bacterial strain Labrys portucalensis F11.
Bessa, VS; Castro, PML; Mascolo, G; Moreira, IS; Murgolo, S, 2019
)
2.68
"Carbamazepine is a current first-line treatment for focal onset seizures in the USA and Europe."( Carbamazepine versus phenytoin monotherapy for epilepsy: an individual participant data review.
Marson, AG; Nevitt, SJ; Tudur Smith, C, 2019
)
2.68
"Carbamazepine (CBZ) is an anti-epileptic drug that acts on Leydig cells, affecting steroidogenesis and causes fetal malformation. "( 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
)
3.29
"Carbamazepine (CBZ) is a first-line widely used anticonvulsant. "( Pharmacogenetic potential biomarkers for carbamazepine adverse drug reactions and clinical response.
Cook, HJ; Galindo, IF; Jaramillo, NM; LLerena, A; López, ML; Vázquez, AO, 2014
)
2.11
"Carbamazepine overdose is a common, toxic ingestion, manifesting as central nervous system (CNS) and respiratory depression. "( Successful treatment of severe carbamazepine toxicity with 5% albumin-enhanced continuous venovenous hemodialysis.
Cole, M; Narayan, R; Rizzo, M, 2014
)
2.13
"Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. "( 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
)
2.06
"Carbamazepine (CBZ) is a recalcitrant xenobiotic pharmaceutical pollutant highly stable in soil and wastewater during treatment. "( Potential of newly isolated wild Streptomyces strains as agents for the biodegradation of a recalcitrant pharmaceutical, carbamazepine.
Amrane, A; Bahrim, G; Dinica, R; Djelal, H; Favier, L; Popa, C; Semrany, S,
)
1.78
"Carbamazepine (CBZ) is a first-line drug for the treatment of different forms of epilepsy and the first choice drug for trigeminal neuralgia. "( Therapeutic drug monitoring of carbamazepine and its metabolite in children from dried blood spots using liquid chromatography and tandem mass spectrometry.
Della Bona, M; Forni, G; Funghini, S; Guerrini, R; la Marca, G; Malvagia, S; Ombrone, D; Rosati, A; Shokry, E; Villanelli, F, 2015
)
2.15
"Carbamazepine (CBZ) is an antiepileptic drug used as a mood stabilizer in child psychiatry."( [Carbamazepine and psychotropic treatment interaction: Two case studies of carbamazepine overdosage].
Askenazy, F; Dor, E; Fernandez, A; Menard, ML; Thümmler, S, 2015
)
2.05
"Carbamazepine is a potent inducer of cytochrome P450 3A and P-glycoprotein. "( Multiple inductive effects of carbamazepine on combined therapy with paliperidone and amlodipine.
Akamine, Y; Miura, M; Uehara, H; Uno, T; Yasui-Furukori, N, 2015
)
2.15
"Carbamazepine is a current first-line treatment for partial onset seizures in the USA and Europe."( Carbamazepine versus phenobarbitone monotherapy for epilepsy: an individual participant data review.
Marson, AG; Nolan, SJ; Tudur Smith, C; Weston, J, 2015
)
2.58
"Carbamazepine is a current first line treatment for partial onset seizures in the USA and Europe."( Carbamazepine versus phenytoin monotherapy for epilepsy: an individual participant data review.
Marson, AG; Nolan, SJ; Tudur Smith, C; Weston, J, 2015
)
2.58
"Carbamazepine (CBZ) is a worldwide used antiepileptic drug, which is metabolized to a large extent in the human body to several metabolites, including 10,11-dihydroxy-10,11-dihydrocarbamazepine (DiOHCBZ), 2-hydroxycarbamazepine (2OHCBZ), and 3-hydroxycarbamazepine (3OHCBZ). "( Why Small Differences Matter: Elucidation of the Mechanisms Underlying the Transformation of 2OH- and 3OH-Carbamazepine in Contact with Sand Filter Material.
Brezina, E; Prasse, C; Ternes, TA; Wagner, M, 2015
)
2.07
"Carbamazepine is an antiepileptic drug widely used for the treatment of epilepsy. "( Comparison of a high-performance liquid chromatography method for quantification of carbamazepine with chemiluminescent microparticle immunoassay.
Castro, N; Escalante-Membrillo, C; Fernández, Á; González-Esquivel, DF; Guerrero Garduño, Ó; Jung Cook, H; Rojas-Tomé, IS, 2016
)
2.1
"Carbamazepine (CBZ) is a potent inducer of these enzymes; thus, the effect of oral extended-release CBZ on DTG pharmacokinetics (PK) was evaluated to provide dose recommendation when co-administered."( 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
)
1.56
"Carbamazepine (CBZ) is an anticonvulsant drug, prescribed worldwide for the treatment of epilepsy, bipolar disorder and trigeminal neuralgia, which has been frequently detected in aquatic environments. "( Effects of carbamazepine on cortisol levels and behavioral responses to stress in the fish Jenynsia multidentata.
Bistoni, Mde L; Calcagno, E; Durando, P; Franchioni, L; Valdés, ME, 2016
)
2.27
"Carbamazepine is a frequently used drug that can produce adverse reactions like vertigo, somnolence and severe skin reactions like Drug Rash with Eosinophilia and Systemic Symptoms Syndrome (DRESS Syndrome). "( [Skin reaction to carbamazepine or DRESS syndrome: a case presentation].
Cabrera Fundora, EJ; Cabrera Osorio, C; Cabrera Osorio, Y, 2016
)
2.21
"Carbamazepine is a classical anticonvulsant that requires therapeutic drug monitoring. "( 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
)
2.28
"Carbamazepine (CBZ) is a drug used for treating epilepsy, neuropathic pain, schizophrenia and bipolar disorder. "( Mechanochemical removal of carbamazepine.
Mingelgrin, U; Nasser, A; Samara, M, 2016
)
2.17
"Carbamazepine (CBZ) is a BCS Class II drug with poor solubility profile. "( Factors influencing the fabrication of albumin-bound drug nanoparticles (ABDns): Part II. Albumin-bound carbamazepine nanoparticles (ABCns).
Chatterjee, P; Erukula, SV; Srivari, Y, 2016
)
2.09
"Carbamazepine is an emerging contaminant and resistant to biodegradation, which cannot be effectively removed by the conventional biological wastewater treatment processes. "( Carbamazepine degradation by gamma irradiation coupled to biological treatment.
Wang, J; Wang, S, 2017
)
3.34
"Carbamazepine (CBZ) is a commonly used drug for epilepsy that is associated with troublesome adverse events including dizziness, double vision, drowsiness, poor co-ordination and unsteadiness. "( Immediate-release versus controlled-release carbamazepine in the treatment of epilepsy.
Marson, AG; Powell, G; Rigby, A; Saunders, M, 2016
)
2.14
"Carbamazepine is a current first-line treatment for partial onset seizures, and is used in the USA and Europe."( Carbamazepine versus phenobarbitone monotherapy for epilepsy: an individual participant data review.
Marson, AG; Nolan, SJ; Tudur Smith, C; Weston, J, 2016
)
2.6
"Carbamazepine (CBZ) is an antiepileptic drug commonly detected in aquatic systems, with toxic effects to inhabiting organisms. "( Toxicity associated to uptake and depuration of carbamazepine in the clam Scrobicularia plana under a chronic exposure.
Almeida, Â; Calisto, V; Esteves, VI; Figueira, E; Freitas, R; Schneider, RJ; Soares, AMVM, 2017
)
2.15
"Carbamazepine which is an anti-neuralgic as well as an anti-convulsant medication is the first line drug for treatment of trigeminal neuralgia."( An observational study of trigeminal neuralgia patients taking carbamazepine during the fasting month of Ramadan.
Ajura, AJ; Lau, SH; Nur Suffia, S, 2016
)
1.4
"Carbamazepine is an antiepileptic drug that can be used as a marker for the cleaning efficiency of wastewater treatment plants. "( Application of fluorescence polarization immunoassay for determination of carbamazepine in wastewater.
Dahmen-Levison, U; Garbe, LA; Oberleitner, L; Schneider, RJ, 2017
)
2.13
"Carbamazepine is a current first-line treatment for partial onset seizures in the USA and Europe."( Carbamazepine versus phenytoin monotherapy for epilepsy: an individual participant data review.
Marson, AG; Nevitt, SJ; Tudur Smith, C; Weston, J, 2017
)
2.62
"Carbamazepine (CBZ) is a widely used antiepileptic agent that frequently interacts with other drugs. "( Kainic acid does not modify the oral pharmacokinetics of carbamazepine in rats.
Alfaro-Rodríguez, A; Ayala-Guerrero, F; Carrasco-Portugal, Mdel C; Flores-Murrieta, FJ; Labra-Ruiz, N; Pérez-Guillé, B; Soriano-Rosales, R, 2007
)
2.03
"Carbamazepine (CBZ) is a first-line antiepileptic drug (AED), although it is also utilized for treatment of psychiatric disorders and neuropathic pain. "( Carbamazepine damage to rat spermatogenesis in different sexual developmental phases.
de Oliva, SU; Miraglia, SM, 2009
)
3.24
"Carbamazepine (CBZ) is an anticonvulsant drug used to treat epilepsy and mood disorders. "( Carbamazepine protects against neuronal hyperplasia and abnormal gene expression in the megencephaly mouse.
Almgren, M; Lavebratt, C; Nyengaard, JR; Persson, B, 2008
)
3.23
"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,
)
2.3
"Carbamazepine is a therapeutic anticonvulsant, used to manage pain. "( An atypical case of fulminant interstitial pneumonitis induced by carbamazepine.
Isshiki, A; Matsumoto, S; Narita, H; Nishiyama, T; Ozawa, T; Watanabe, S, 2009
)
2.03
"Carbamazepine is a first-choice antiepileptic drug for the treatment of simple and complex partial seizures. "( 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
)
2.03
"Carbamazepine (CBZ) is a first-line antiepileptic agent with mood-stabilizing effects in bipolar disorder. "( High resolution micro-SPECT scanning in rats using 125I beta-CIT: effects of chronic treatment with carbamazepine.
Cain, SM; Dewar, D; Duncan, R; Patterson, J; Pimlott, S; Ruest, T; Sills, GJ, 2009
)
2.01
"Carbamazepine is a medication routinely used to treat tinnitus."( Treatment of subjective tinnitus: a comparative clinical study of intratympanic steroid injection vs. oral carbamazepine.
Chen, F; Cui, X; Dai, Y; Ding, X; Du, X; She, W, 2009
)
1.29
"Carbamazepine is a potent inducer of drug metabolizing enzymes, which results in a number of clinically significant drug-drug interactions. "( Characterization of the time course of carbamazepine deinduction by an enzyme turnover model.
Birnbaum, AK; Cloyd, JC; Leppik, IE; Marino, SE; Pennell, PB; Punyawudho, B; Ramsay, RE; White, JR, 2009
)
2.06
"Carbamazepine is an active pharmaceutical ingredient (API) used worldwide as a medicine for treating epileptic seizures and trigeminal neuralgia."( Human health risk assessment of carbamazepine in surface waters of North America and Europe.
Bechter, R; Cunningham, VL; D'Aco, VJ; Hartmann, A; Perino, C, 2010
)
1.37
"Carbamazepine is an antiepileptic drug used widely for the treatment of epileptic seizures and neuropathic pain. "( Teratogenic effects of carbamazepine on embryonic eye development in pregnant mice.
Afshar, M; Houshang Mohammadpour, A; Jafar Golalipour, M; Majid Jalalian, S; Moallem, SA; Shiravi, A, 2010
)
2.11
"Carbamazepine (CBZ) is a commonly used antiepileptic agent. "( Management of a severe carbamazepine overdose with continuous venovenous hemodiafiltration.
Goktas, U; Kati, I; Yuce, HH, 2010
)
2.11
"Carbamazepine (Carba) is an anticonvulsant and psychotropic drug used widely for the treatment of intellectual disability and severe pains, but the incidence of hyponatremia is a common related occurrence. "( Carbamazepine can induce kidney water absorption by increasing aquaporin 2 expression.
de Bragança, AC; Magaldi, AJ; Moyses, ZP, 2010
)
3.25
"Carbamazepine is an anticonvulsant requiring routine therapeutic drug monitoring. "( Analytical performance evaluation of ADVIA Chemistry Carbamazepine_2 assay: minimal cross-reactivity with carbamazepine 10, 11-epoxide and none with hydroxyzine or cetirizine.
Dasgupta, A; Davis, BG; Johnson, M; Marlow, AM; Reyes, MA, 2010
)
2.05
"Carbamazepine is a prescription anticonvulsant and mood stabilizing pharmaceutical administered to humans. "( Sorption and desorption of carbamazepine from water by smectite clays.
Boyd, SA; Ding, Y; Li, H; Teppen, BJ; Zhang, W, 2010
)
2.1
"Carbamazepine (CBZ) is a useful anticonvulsive drug associated with rare severe adverse drug reactions. "( Presence and ex vivo formation of acridone in blood of patients routinely treated with carbamazepine: exploration of the 9-acridinecarboxaldehyde pathway.
Dereure, O; Hillaire-Buys, D; Mathieu, O, 2011
)
2.03
"Carbamazepine is a (CYP1A2 and CYP3A4 enzyme inducer) medicine which is used by epileptic patients for a long time. "( Therapeutic effects of ciprofloxacin on the pharmacokinetics of carbamazepine in healthy adult male volunteers.
Ashraf, MY; Asi, MR; Aslam, B; Javed, I; Muhammad, F; Shahzadi, A, 2011
)
2.05
"Carbamazepine is a widely used anticonvulsive agent. "( Effects of carbamazepine and metabolites on IL-2, IL-5, IL-6, IL-10 and IFN-γ secretion in epileptic patients: the influence of co-medication.
Breton, H; Demoly, P; Gelisse, P; Hillaire-Buys, D; Mathieu, O; Picot, MC, 2011
)
2.2
"Carbamazepine is a psychiatric pharmaceutical widely detected in aquatic environments. "( Application of an ELISA to the quantification of carbamazepine in ground, surface and wastewaters and validation with LC-MS/MS.
Bahlmann, A; Calisto, V; Esteves, VI; Schneider, RJ, 2011
)
2.07
"Carbamazepine (CBZ) is an environmentally recalcitrant compound highly stable in soil and during wastewater treatment. "( Transformation of the recalcitrant pharmaceutical compound carbamazepine by Pleurotus ostreatus: role of cytochrome P450 monooxygenase and manganese peroxidase.
Ben-Ari, J; Chefetz, B; Geva, J; Golan-Rozen, N; Hadar, Y, 2011
)
2.06
"Carbamazepine (CBZ) is a commonly prescribed antiepileptic drug. "( Histone deacetylase 1 is required for Carbamazepine-induced CYP3A4 expression.
Liu, Y; Luo, X; Shi, X; Wang, J; Wen, A; Wu, Y; Zhang, X, 2012
)
2.09
"Carbamazepine (CBZ) is an antiepileptic orally administered drug, but due to its low solubility in water, its gastrointestinal absorption is slow and irregular, leading to delayed brain uptake with consequent peripheral side actions. "( Carbamazepine mucoadhesive nanoemulgel (MNEG) as brain targeting delivery system via the olfactory mucosa.
Hanan, R; Kamal, el T; Samia, O, 2012
)
3.26
"Carbamazepine is a widely prescribed antiepileptic drug. "( 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
)
2.19
"Carbamazepine is a commonly used antiepileptic drug in elderly patients. "( Population pharmacokinetics of carbamazepine in elderly patients.
Birnbaum, AK; Brundage, RC; Collins, JF; Macias, FM; Punyawudho, B; Ramsay, ER, 2012
)
2.11
"Carbamazepine (CBZ) is a first-line antiepileptic drug (AED), although it is also used for the treatments of psychiatric disorders and neuropathic pain. "( Harmful effects of carbamazepine on the postnatal development of the rat ventral prostate.
Miraglia, SM; Okada, FK; Oliva, SU; Scarano, WR, 2012
)
2.15
"Carbamazepine is an iminostilbene derivative structurally related to cyclic antidepressants which implies its potential cardiotxic properties, especially in acute poisoning. "( Relationship of cardiovascular complications with level of consciousness in patients with acute carbamazepine intoxication.
Gheshlaghi, F; Ghoreishi, A; Soh, EH; Yaraghi, A, 2012
)
2.04
"Carbamazepine (CBZ) is a commonly used antiepileptic that is metabolized by CYP3A isoforms."( Opposing regulation of cytochrome P450 expression by CAR and PXR in hypothyroid mice.
Jang, HC; Lee, EK; Lee, YK; Moore, DD; Park, DJ; Park, YJ, 2012
)
1.1
"Carbamazepine is a murine radiation protector and mitigator."( Ionizing irradiation protection and mitigation of murine cells by carbamazepine is p53 and autophagy independent.
Bernard, ME; Cobanoglu, MC; Dixon, T; Epperly, M; Farkas, A; Franicola, D; Goff, J; Greenberger, JS; Houghton, F; Kalash, R; Kim, H; Shields, D; Wang, H; Zhang, X,
)
1.81
"Carbamazepine is an antiepileptic pharmaceutical which is commonly found in environmental matrices. "( Adsorption of the antiepileptic carbamazepine onto agricultural soils.
Calisto, V; Esteves, VI, 2012
)
2.11
"Carbamazepine (CBZ) is a drug widely used in the therapy of epilepsy and mood disorders. "( Carbamazepine affects water and electrolyte homoeostasis in rat--similarities and differences to vasopressin antagonism.
Bleich, M; Himmerkus, N; Sievers, B, 2012
)
3.26
"Carbamazepine (CBZ) is a widely used antiepileptic agent."( Metabolic activation and inflammation reactions involved in carbamazepine-induced liver injury.
Fukami, T; Higuchi, S; Nakajima, M; Takai, S; Tsuneyama, K; Yano, A; Yokoi, T, 2012
)
1.34
"Carbamazepine (CBZ) is an iminostilbene derivative commonly used for treatment of neuralgic pain and bipolar affective disorders. "( Antiepileptic carbamazepine drug treatment induces alteration of membrane in red blood cells: possible positive effects on metabolism and oxidative stress.
Barreca, D; Bellocco, E; Carelli-Alinovi, C; Ficarra, S; Galtieri, A; Giardina, B; Laganà, G; Leuzzi, U; Misiti, F; Russo, A; Tellone, E; Toscano, G, 2013
)
2.19
"Carbamazepine (amizepine) is a widely used psychotropic agent. "( Carbamazepine poisoning: elimination kinetics and quantitative relationship with carbamazepine 10,11-epoxide.
Szymańska, B; Szymczak, WM; Topaciński, B; Winnicka, RI, 2002
)
3.2
"Carbamazepine is a well-established, effective treatment of complex partial seizures and is well tolerated in most patients. "( Transient neurologic deficits associated with carbamazepine-induced hypertension.
Choi, JY; Labutta, RJ; Marini, AM,
)
1.83
"Carbamazepine is a mood stabilizer used as monotherapy or as an adjunct to lithium in the treatment of acute mania or the prophylaxis of bipolar disorder. "( Chronic carbamazepine selectively downregulates cytosolic phospholipase A2 expression and cyclooxygenase activity in rat brain.
Bell, JM; Bosetti, F; Ghelardoni, S; Rapoport, SI; Tomita, YA, 2004
)
2.2
"Carbamazepine (CBZ) is a common antiepileptic drug (AED) that acts through multiple mechanisms including blockade and potentiation of cation channels and modulation of neurotransmitter levels. "( Carbamazepine is an inhibitor of histone deacetylases.
Beutler, AS; Li, S; Nicol, R; Walsh, MJ, 2005
)
3.21
"Carbamazepine is a widely used drug. "( Carbamazepine-induced acute liver failure as part of the DRESS syndrome.
Holt, AP; Mutimer, DJ; Naisbitt, DJ; Pirmohamed, M; Syn, WK, 2005
)
3.21
"Carbamazepine is an antiepileptic drug widely used by neurological and psychiatric patients. "( Comparison of fluorescence polarization immunoassay and high performance liquid chromatography for determination of carbamazepine concentration in blood of poisoned patients.
Gomółlka, E; Jenner, B; Pasich, A; Szpak, D; Wilimowska, J, 2005
)
1.98
"Carbamazepine (CBZ) is a drug of choice for the treatment of simple or complex partial seizures and secondary generalized seizures in adults and children. "( A comparative study of vigabatrin vs. carbamazepine in monotherapy of newly diagnosed partial seizures in children.
Boćkowski, L; Kułak, W; Smigielska-Kuzia, J; Sobaniec, W; Strzelecka, J,
)
1.85
"Carbamazepine is a commonly used anticonvulsant agent; however, it has been linked with various blood cell abnormalities. "( Folic acid supplementation reduces the development of some blood cell abnormalities in children receiving carbamazepine.
Asadi-Pooya, AA; Ghetmiri, E, 2006
)
1.99
"Carbamazepine (CBZ) is an oral anticonvulsant drug, structurally similar to tricyclic antidepressants. "( [Fixed pigmented erythema related to the oral administration of carbamazepine: report of one case].
Alvarez, VJ; Goncalves, ET; Luna, JR; Morales, AR; Picón, JE, 2006
)
2.02
"Carbamazepine is a medication rarely implicated in drug-induced cutaneous lupus, moreover there are very few reports of such long periods between the start of therapy and the presentation of the clinical symptoms."( Drug-induced cutaneous lupus erythematosus after 5 years of treatment with carbamazepine.
Amerio, P; Angelucci, D; Feliciani, C; Gambi, D; Innocente, C; Tulli, A,
)
1.08
"Carbamazepine (CBZ) is a pharmacological agent used to control epileptic syndromes. "( [Evaluation of the drug interaction between carbamazepine and lamotrigine in the treatment of refractory epilepsy patients].
Ceiki-Sakamoto, A; de Carvalho, D; Pereira, LR; Velasco, TR,
)
1.84
"Carbamazepine (CBZ) is an inducer of cytochrome P450 enzymes, which have been implicated in many drug interactions. "( Induction of P-glycoprotein in lymphocytes by carbamazepine and rifampicin: the role of nuclear hormone response elements.
Goldring, C; Morgan, P; Owen, A; Park, BK; Pirmohamed, M, 2006
)
2.03
"Carbamazepine (CBZ) is a commonly used antiepileptic drug known to block voltage-gated sodium channels. "( Carbamazepine protects against megencephaly and abnormal expression of BDNF and Nogo signaling components in the mceph/mceph mouse.
Josephsson, A; Klason, T; Lavebratt, C; Ohman, I; Olson, L; Persson, AS; Schalling, M; Spenger, C; Trifunovski, A; Wang, FH, 2006
)
3.22
"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
"Carbamazepine is a widely used antiepileptic agent. "( Carbamazepine poisoning managed with haemodialysis and haemoperfusion in three adolescents.
Aydin, OF; Bek, K; Koçak, S; Ozkaya, O; Taşdöven, CS; Yilmaz, Y, 2007
)
3.23
"Carbamazepine is a UGT1A4 inducer."( Two case reports of oral ulcers with lamotrigine several weeks after oxcarbazepine withdrawal.
de Leon, J; O'Neill, A, 2007
)
1.06
"Carbamazepine (CBZ) is an antiepileptic drug with tricyclic structure which implies its potential cardinotxic properties, especially in acute poisoning."( The influence of carbamazepine plasma level on blood pressure and some ECG parameters in patients with acute intoxication.
Ciszowski, K; Jenner, B; Szpak, D, 2007
)
2.12
"Carbamazepine is a popular drug that has been detected in natural environments, but little is known about its biogeochemical cycling, influencing factors, and eco-environmental effects in aquatic ecosystems. "( Interaction between carbamazepine and humic substances: a fluorescence spectroscopy study.
Bai, Y; Fu, P; Guo, J; Li, W; Liu, C; Wu, F; Xing, B, 2008
)
2.11
"Carbamazepine (CBZ) is a widely prescribed anticonvulsant whose use is often associated with idiosyncratic hypersensitivity. "( CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile.
Correia, MA; Kang, P; Leeder, JS; Liao, M; Pearce, RE; Wester, MR, 2008
)
2.13
"Carbamazepine is an anticonvulsant agent that has been found clinically useful in the treatment of refractory seizure disorders. "( Carbamazepine-induced thrombocytopenia, rash, and hepatic dysfunction.
Ponte, CD, 1983
)
3.15
"Carbamazepine is an anticonvulsant drug in widespread use for the treatment of tonic-clonic and temporal lobe seizure disorders. "( Acute carbamazepine intoxication: clinical spectrum and management.
May, DC, 1984
)
2.19
"Carbamazepine is a commonly used anticonvulsant agent, particularly in the management of partial seizures. "( Leucopenia as an adverse reaction to carbamazepine therapy.
Beran, RG; Rush, JA, 1984
)
1.98
"Carbamazepine is a valuable drug in the treatment of trigeminal neuralgia and temporal lobe epilepsy. "( Agranulocytosis associated with carbamazepine, and a positive reaction with anti-lymphoid leukaemia antiserum during recovery.
Davies, J; Nunn, PP; Owens, CW; Parker, NE, 1980
)
1.99
"Carbamazepine is an anticonvulsant drug useful in the management of epilepsy. "( Homogeneous substrate-labeled fluorescent immunoassay for carbamazepine.
Burd, JF; Li, TM; Miller, JE; Ward, FE, 1982
)
1.95
"Carbamazepine may prove to be a useful additional treatment for affective illness."( Carbamazepine in manic-depressive illness: a new treatment.
Ballenger, JC; Post, RM, 1980
)
2.43
"Carbamazepine is a most effective drug."( VIIIth nerve vascular compression syndrome: vestibular paroxysmia.
Brandt, T; Dieterich, M, 1994
)
1.01
"Carbamazepine (CBZ) is a first-line drug in the treatment of epileptic seizures and neuralgia. "( [Effects of carbamazepine on heart conduction in young patients: a serial study using ambulatory ECG].
Borgia, MC; Curione, M; Fanari, F; Matteoli, S; Puletti, M; Trappolini, M, 1994
)
2.11
"Carbamazepine is a widely used drug associated with numerous side effects including skin eruptions that appear in about 4% of patients. "( Epicutaneous test in carbamazepine cutaneous reactions.
Dorado, JM; Fernández-Herrera, J; García-Díez, A; Jones, M; Ruiz, M; Sols, M, 1994
)
2.05
"Carbamazepine is an anticonvulsant which is associated with a significant incidence of hypersensitivity reactions including agranulocytosis. "( Carbamazepine metabolism to a reactive intermediate by the myeloperoxidase system of activated neutrophils.
Furst, SM; Uetrecht, JP, 1993
)
3.17
"Carbamazepine (CBZ) is a sodium-channel blocker used mainly for the treatment of epileptic seizures and neuralgias. "( Electrophysiological evaluation of the sodium-channel blocker carbamazepine in healthy human subjects.
Bergfeldt, L; Kennebäck, G; Tomson, T, 1995
)
1.97
"Carbamazepine is a drug commonly used in the treatment of neuropathic pain. "( Carbamazepine-induced hepatitis in a patient with cervical myelopathy.
Kong, KH, 1996
)
3.18
"Carbamazepine is a good substitute for lithium when severe renal problems exclude the use of lithium."( Lithium therapy in the treatment of manic-depressive illness. Present status and future perspectives. A critical review.
Charles, G; Emilien, G; Maloteaux, JM; Seghers, A,
)
0.85
"Carbamazepine is a potent inducer of CYP3A4 and other oxidative enzyme system in the liver, and it may also increase glucuronyltransferase activity."( Clinically significant pharmacokinetic drug interactions with carbamazepine. An update.
Perucca, E; Pisani, F; Spina, E, 1996
)
1.26
"Carbamazepine is a known enzyme inducer. "( Induction of CYP1A2 activity by carbamazepine in children using the caffeine breath test.
Choonara, I; Parker, AC; Preston, T; Pritchard, P, 1998
)
2.03
"Carbamazepine is an anticonvulsant associated with a high risk for severe cutaneous reactions. "( Covalent binding of carbamazepine reactive metabolites to P450 isoforms present in the skin.
Bagot, M; Beaune, P; Charue, D; Garcia-Martin, N; Lecoeur, S; Tan, C; Wechsler, J; Wolkenstein, P, 1998
)
2.07
"Carbamazepine is a drug commonly prescribed by medical and dental practitioners for the treatment of trigeminal neuralgia. "( A severe reaction to carbamazepine: consequences for patient monitoring.
Edmondson, HD; Hamburger, J; Neale, SJ, 1998
)
2.06
"Carbamazepine (CBZ) is a drug frequently used to treat variety of neurological diseases or symptoms. "( Reversible pitch perception deficit due to carbamazepine.
Imai, K; Kashihara, K; Shiro, Y; Shohmori, T, 1998
)
2.01
"Carbamazepine is an anticonvulsant, but also has an anti-manic effect, and recently it has been increasingly used in combination with neuroleptics. "( Addition of carbamazepine to long-term treatment with neuroleptics may induce neuroleptic malignant syndrome.
Ishiguro, T; Kusakabe, Y; Nisijima, K; Ohtuka, K, 1998
)
2.12
"Carbamazepine (CBZ) is an effective anticonvulsant agent. "( Exacerbation of epileptic seizures by carbamazepine: report of 10 cases.
Fraticelli, E; Parmeggiani, A; Rossi, PG, 1998
)
2.01
"Carbamazepine (CBZ) is a drug which can induce the syndrome of inappropriate antidiuretic hormone (SIADH). "( [Carbamazepine induced hyponatremia].
Fukui, M; Hisada, K; Inamura, T; Kuba, H; Morioka, T; Muraishi, M; Muratani, H, 1999
)
2.66
"Carbamazepine is a major antiepileptic drug which is primarily used to treat epileptic patients suffering from partial seizures with or without secondary generalization, but which also has applications in those suffering from primary generalized tonic-clonic seizures. "( Carbamazepine in the treatment of epilepsy in people with intellectual disability.
Alvarez, N; Waisburg, H, 1998
)
3.19
"Carbamazepine is a potent anticonvulsant agent with proven efficacy in the treatment of partial and tonic-clonic seizures. "( Suspected carbamazepine-induced hepatotoxicity.
Morales-Diaz, M; Pinilla-Roa, E; Ruiz, I, 1999
)
2.15
"Carbamazepine is a commonly prescribed anticonvulsant medication that affects various levels of the nervous system. "( Carbamazepine-induced sensorineural hearing loss.
Bance, M; de la Cruz, M, 1999
)
3.19
"Carbamazepine (CBZ) is a well-established drug in the therapy of temporal lobe epilepsy (TLE). "( Carbamazepine effects on Na+ currents in human dentate granule cells from epileptogenic tissue.
Beck, H; Elger, CE; Reckziegel, G; Schramm, J; Urban, BW, 1999
)
3.19
"Carbamazepine is a potent enzyme inducer, predominantly of the CYP3A enzyme system, while HIV-protease inhibitors such as indinavir are substrates for and inhibitors of CYP3A."( Carbamazepine--indinavir interaction causes antiretroviral therapy failure.
Brinkman, K; Burger, DM; Hekster, YA; Hugen, PW; Koopmans, PP; Schuurman, R; ter Hofstede, HJ, 2000
)
2.47
"Carbamazepine (CBZ) is an antiepileptic drug frequently used to treat a variety of neurologic diseases or symptoms. "( Reversible pitch perception deficit caused by carbamazepine.
Horiguchi, J; Itoga, M; Miyaoka, T; Seno, H,
)
1.83
"Carbamazepine is an anticonvulsant and psychotropic medication commonly used in the treatment of people with intellectual disability (ID). "( Hyponatremia during carbamazepine therapy in patients with intellectual disability.
Hillery, J; Kelly, BD, 2001
)
2.08
"Carbamazepine is a standard anticonvulsant in children and adults. "( Carbamazepine in phenobarbital-nonresponders: experience with ten preterm infants.
Bartmann, P; Elger, CE; Hoppen, T, 2001
)
3.2
"Carbamazepine seems to be an effective treatment, both in the acute phase, and as maintenance in a subgroup of retarded catatonic patients."( Catatonia: an open prospective series with carbamazepine.
Jordaan, GP; Kritzinger, PR, 2001
)
1.29
"Carbamazepine is a second-line alternative."( Disodium valproate: new preparation. An alternative for acute mania after lithium failure or intolerance.
, 2001
)
1.03
"Carbamazepine (CBZ) is an antiepileptic drug that was developed and marketed mainly for the treatment of epileptic seizures."( The teratogenic effect of carbamazepine: a meta-analysis of 1255 exposures.
Goldzweig, G; Matalon, S; Ornoy, A; Schechtman, S,
)
1.15
"Carbamazepine is an anticonvulsant most effective in treating complex partial and generalized tonic-clonic seizures. "( Dystonia associated with carbamazepine administration: experience in brain-damaged children.
Crosley, CJ; Swender, PT, 1979
)
2.01
"Carbamazepine is a suitable substitute for phenobarbital, primidone, and phenytoin, alone or in combination, when used in the treatment of generalized tonic-clonic or partial epilepsy. "( Carbamazepine as a substitute treatment of single and compound seizures.
McFarland, HR, 1978
)
3.14
"Carbamazepine was found to be an effective anticonvulsant in the treatment of grand mal epilepsy."( Plasma level and effect of carbamazepine in grand mal and psychomotor epilepsy.
Christiansen, J; Dam, M; Jensen, A, 1975
)
1.27
"Carbamazepine is an interesting new drug, with both anticonvulsant and psychotropic properties, for which both the behavioral effects and pharmacological actions have been defined."( Carbamazepine in the dyscontrol syndrome associated with limbic system dysfunction.
Dermer, SW; Tunks, ER, 1977
)
2.42
"As carbamazepine is a potent drug and is often prescribed for long periods together with other anticonvulsants, it seems important to prove that the allergic reaction is caused by carbamazepine."( Lymphocyte-stimulation tests and patch tests to carbamazepine hypersensitivity.
De Gast, GC; Esselink, MT; Houwerzijl, J; Nater, JP; Nieweg, HO, 1977
)
1.03
"Carbamazepine (CBZ) is a widely used therapeutic agent in seizure, pain, and mood disorders. "( Effects of carbamazepine on pituitary-adrenal function in healthy volunteers.
Chrousos, GP; Devinsky, O; Gallucci, WT; Gold, PW; Hauser, P; Kling, MA; Perini, GI; Theodore, WH, 1992
)
2.12
"Carbamazepine is a first line drug in the treatment of epilepsy and trigeminal neuralgia, but may exert negative chronotropic and dromotropic effects on the cardiac conduction system. "( Carbamazepine induced bradycardia--a problem in general or only in susceptible patients? A 24-h long-term electrocardiogram study.
Bergfeldt, L; Edhag, O; Kennebäck, G; Spina, E; Tomson, T, 1992
)
3.17
"Carbamazepine appears to be a useful treatment, combined with neuroleptics, for acute schizophrenic episodes."( [Carbamazepine: an efficient adjuvant treatment in schizophrenia].
Guajardo-Fajardo Ibarra, I; Martín Muñoz, JC; Mateo Martín, I; Moriñigo Domínguez, AV; Noval Lamos, D,
)
1.76
"Carbamazepine is an anticonvulsant that is being used more frequently in the treatment of various psychiatric disorders. "( Carbamazepine hypersensitivity reaction.
Rivey, MP; Stone, JD,
)
3.02
"Carbamazepine is an effective antiepileptic drug for the treatment of partial and convulsive generalised epilepsy in adults and children. "( Risk-benefit assessment of carbamazepine in children.
Pellock, JM; Seetharam, MN,
)
1.87
"Carbamazepine is an important drug used in the management of seizures, trigeminal neuralgia, and chronic pain syndromes. "( Carbamazepine-induced eruption histologically mimicking mycosis fungoides.
Gradini, R; Massa, M; Nakao, J; Welykyj, S, 1990
)
3.16
"Carbamazepine (CBZ) is a widely used antiepileptic drug (AED). "( The efficacy and tolerability of chewable carbamazepine compared to conventional carbamazepine in patients with epilepsy.
Finnerty, G; Patsalos, PN; Russell-Jones, D; Sander, JW; Shorvon, SD, 1990
)
1.99
"Carbamazepine appears to be a useful treatment, combined with neuroleptics, for acute schizophrenic episodes."( [Carbamazepine: an effective adjuvant treatment in the schizophrenias].
Guajardo-Fajardo Ibarra, I; Martín Muñoz, JC; Mateo Martín, I; Moriñigo Domínguez, AV; Noval Lamos, D,
)
1.76
"Carbamazepine is a tricyclic compound structurally related to imipramine that has been used since the 1960's for the treatment of trigeminal neuralgias and then approved as an anticonvulsant in the U.S. "( Carbamazepine in psychiatry: a review.
Beaudry, P; Israel, M, 1988
)
3.16
"Carbamazepine is a drug of choice for partial epilepsies, certain affective disorders and neuralgic pain syndromes. "( A fatal overdose of carbamazepine: case report and review of literature.
Cysyk, B; Fisher, RS, 1988
)
2.04
"Carbamazepine is a broad-spectrum enzyme inducer."( Clinical pharmacokinetics of carbamazepine.
Kerr, BM; Levy, RH, 1988
)
1.29
"Carbamazepine is a safe drug, but physicians and patients should be aware of the exceedingly rare but potentially fatal side effects, better prevented by clinical than by laboratory monitoring."( Fatal aplastic anemia in a patient treated with carbamazepine.
Borri, A; Canal, N; Ciboddo, G; Franceschi, M; Truci, G,
)
1.11
"Carbamazepine is a first-line drug in the treatment of most forms of epilepsy and also the drug of first choice in trigeminal neuralgia. "( Clinical pharmacokinetics and pharmacological effects of carbamazepine and carbamazepine-10,11-epoxide. An update.
Bertilsson, L; Tomson, T,
)
1.82

Effects

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.

ExcerptReferenceRelevance
"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

Actions

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.

ExcerptReferenceRelevance
"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

Treatment

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.

ExcerptReferenceRelevance
"The carbamazepine treatment was discontinued and standard chemotherapy was started for acute lymphoblastic leukemia (CALGB protocol)."( Acute lymphocytic leukemia in a patient with long-term carbamazepine exposure: Acute lymphoblastic leukemia that develops in a patient who has been using carbamazepine for a long time.
Bagci, M; Sayin, S, 2023
)
1.64
"Carbamazepine treatment could delay the disease onset and extend life span of SOD1-G93A mice by about 14.5% and 13.9%, respectively. "( Repurposing carbamazepine for the treatment of amyotrophic lateral sclerosis in SOD1-G93A mouse model.
Chen, S; Le, WD; Zhang, JJ; Zhou, QM, 2018
)
2.3
"Carbamazepine treatment is a protective factor against uncontrolled seizures for EAF. "( Factors predicting uncontrolled seizures in epilepsy with auditory features.
Chen, L; Zhang, L; Zhu, X; Zou, X, 2019
)
1.96
"Carbamazepine-treated patients showed mean serum thyroid hormone levels significantly lower than baseline evaluation and the control group."( Evaluation of thyroid hormones in children receiving carbamazepine or valproate: a prospective study.
Arapoglu, M; Dalgıç, N; Kafadar, İ; Kılıç, BA; Yalçın, K, 2015
)
1.39
"Carbamazepine-XR treatment was associated with normalization of activation in right Brodmann area 10 (BA)."( The effects of carbamazepine on prefrontal activation in manic youth with bipolar disorder.
Adler, CM; Bitter, SM; DelBello, MP; Elliott, KB; Klein, CC; Schneider, MR; Strakowski, SM; Weber, W, 2014
)
1.48
"Carbamazepine pretreatment significantly altered fexofenadine pharmacokinetics, decreasing the mean (+/- standard deviation) peak plasma concentration from 176.6 (+/- 82.1) ng/mL to 103.2 (+/- 33.6) ng/mL (P < 0.01) and the area under the plasma concentration-time curve from 1058.4 (+/- 528.7) ng/h/mL to 604.8 (+/- 255.9) ng/h/mL (P < 0.01) without changing the elimination half-life."( Effects of the P-glycoprotein inducer carbamazepine on fexofenadine pharmacokinetics.
Akamine, Y; Kaneko, S; Uno, T; Yamada, S; Yasui-Furukori, N, 2009
)
1.35
"Carbamazepine treatment was only partially and transiently effective."( Serial monitoring of basal metabolic rate for therapeutic evaluation in an Isaacs' syndrome patient with chronic fluctuating symptoms.
Hayashi, Y; Hozumi, I; Inuzuka, T; Kimura, A; Sakurai, T; Tanaka, Y; Watanabe, N; Yamada, M, 2010
)
1.08
"Carbamazepine treatment was started at 200 mg every 12 hours and increased at discharge to 300 mg every 8 hours."( Effects of carbamazepine/oxycodone coadministration in the treatment of trigeminal neuralgia.
Avenoso, T; De Sarro, G; Gallelli, L; Siniscalchi, A; Squillace, A, 2011
)
1.48
"Carbamazepine treatment showed excellent results."( [A case of symptomatic paroxysmal kinesigenic dsykinesia with primary central nervous system lymphoma].
Ganser, A; Rollnik, JD; Winkler, T, 2003
)
1.04
"carbamazepine (CBZ)] in the treatment of inpatients with alcohol withdrawal syndrome were compared."( Treatment of alcohol withdrawal: chlormethiazole vs. carbamazepine and the effect on memory performance--a pilot study.
Emrich, HM; Jahn, K; Metzner, C; Ohlmeier, M; Peters, E; Schneider, U; Seifert, J; te Wildt, B, 2004
)
1.29
"Carbamazepine treatment alters the serum lipid profile of children in such a way that it could potentially facilitate the development of atherosclerosis."( Serum lipid levels during carbamazepine therapy in epileptic children.
Iranpour, R; Mahmoudian, T; Messri, N, 2005
)
1.35
"Carbamazepine treatment significantly decreased the peak plasma concentration (17.5+/-4.1 ng/ml versus 13.9+/-4.1 ng/ml; P<0.05), total area under the plasma concentration-time curve (194.8+/-88.9 ng h/ml versus 105.9+/-33.0 ng h/ml; P<0.001), and elimination half-life (11.1+/-4.6 h versus 6.8+/-2.8 h; P<0.01) of etizolam. "( Induction of the metabolism of etizolam by carbamazepine in humans.
Aoshima, T; Fukasawa, T; Inoue, Y; Kondo, S; Otani, K; Suzuki, A; Tateishi, T; Yasui-Furukori, N, 2005
)
2.03
"Carbamazepine-treated rats (n = 5) had a significantly greater total duration of SWD than vehicle-treated rats (17.9% versus 8.8%, P = 0.04)."( Aggravation of absence seizures by carbamazepine in a genetic rat model does not induce neuronal c-Fos activation.
Jupp, B; Li, S; Morris, MJ; O'Brien, TJ; Wallengren, C,
)
1.13
"Carbamazepine treatment caused worsening of the depressive episodes and facial tics."( Nonconvulsive status epilepticus precipitated by carbamazepine presenting as dissociative and affective disorders in adolescents.
D'Arcangelo, G; Guerrini, R; Marini, C; Masi, G; Parmeggiani, L, 2005
)
1.3
"Carbamazepine treatment could inhibit the proliferation of MCF-7 and T47D cells stimulated by estradiol (P<0.01). "( [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
"The carbamazepine treatment was stopped and laboratory parameters improved."( [Carbamazepine hepatoxicity--a case report].
Gawlikowski, T; Hydzik, P, 2007
)
1.73
"Carbamazepine treatment was subsequently discontinued, and the patient was treated with red blood cell transfusions, haptoglobin, and methylprednisolone."( Carbamazepine-induced hemolytic and aplastic crises associated with reduced glutathione peroxidase activity of erythrocytes.
Fujii, H; Hatakeyama, N; Kanno, H; Kubo, N; Suzuki, N; Tachi, N; Tsutsumi, H; Yamamoto, M, 2007
)
2.5
"Carbamazepine treatment increased mean plasma 4beta-hydroxycholesterol significantly already after 1 week of treatment (from 43 to 80 ng ml(-1), P < 0.001)."( Time course of the increase in 4beta-hydroxycholesterol concentration during carbamazepine treatment of paediatric patients with epilepsy.
Bertilsson, L; Diczfalusy, U; Larsson, H; Wide, K, 2008
)
1.3
"Carbamazepine treatment of paediatric patients with epilepsy resulted in an induction of CYP3A4/5 and a concomitant increase in plasma 4beta-hydroxycholesterol. "( Time course of the increase in 4beta-hydroxycholesterol concentration during carbamazepine treatment of paediatric patients with epilepsy.
Bertilsson, L; Diczfalusy, U; Larsson, H; Wide, K, 2008
)
2.02
"Carbamazepine treatment caused at least a 4-fold increase in the N-demethylation clearance of clobazam."( Analysis of parent drug-metabolite relationship in the presence of an inducer. Application to the carbamazepine-clobazam interaction in normal man.
Brachet-Liermain, A; Cenraud, B; Guyot, M; Lane, EA; Levy, RH; Loiseau, P,
)
1.07
"With carbamazepine treatment marked improvement occurred both clinically and electromyographically."( Motor neuron rigidity. An electrophysiological, pharmacological and pathological study.
Bulcke, J; De Meirsman, J; Dom, R; Van den Bergh, P, 1983
)
0.72
"Carbamazepine treated rats had a lowered epididymal sperm content which did not affect their fertility."( The effect of anticonvulsant drugs on the development of male rats and their fertility.
Cohn, DF; Homonnai, ZT; Paz, GF, 1982
)
0.99
"Carbamazepine treatment was effective in all patients."( Hypnogenic paroxysmal dystonia: epileptic seizure or a new syndrome?
Cirignotta, F; Lugaresi, E, 1981
)
0.98
"Carbamazepine treatment resulted in prolongation of peak latencies of waves I-III-V and interpeak intervals I-III and I-V."( Effects of carbamazepine and valproate on brainstem auditory evoked potentials in epileptic children.
Cenani, A; Dirican, A; Keskin, G; Senocak, D; Sozuer, D; Yalcin, E; Yuksel, A, 1995
)
1.4
"Carbamazepine treatment not only completely eliminated the recurring attacks of his choreo-athetosis but also, contrary to expectations, the visual disturbances and even the symptoms of his obsessive-compulsive disorder."( Familial paroxysmal kinesigenic choreo-athetosis in a child with visual hallucinations and obsessive-compulsive behaviour.
Freeman, RD; Good, WV; Jan, JE, 1995
)
1.01
"Carbamazepine treatment rendered the patient free of seizures."( [Focal epilepsy with seizures from the supplementary sensorimotor area. False interpretation as a spinal disease].
Noachtar, S, 1995
)
1.01
"Carbamazepine treatment seemingly brought about a slight decrease in the frequency of attacks."( SUNCT syndrome in the female.
Pareja, JA; Sjaastad, O, 1994
)
1.01
"Carbamazepine treatment was consistently and significantly associated with increased cerebrospinal fluid thyrotropin-releasing hormone levels (P < .0001)."( Carbamazepine increases cerebrospinal fluid thyrotropin-releasing hormone levels in affectively ill patients.
Bissette, G; George, MS; Huggins, T; Marangell, LB; Pazzaglia, P; Post, RM, 1994
)
3.17
"Carbamazepine treatment of a patient with 48-hour rapid cycling led to a dampening of mood cycling, and prolonged rapid eye movement (REM) sleep latency. "( The effect of carbamazepine on endocrine and sleep EEG variables in a patient with 48-hour rapid cycling, and healthy controls.
Bahro, M; Berger, M; Gann, H; Hohagen, F; Müller, WE; Riemann, D, 1993
)
2.09
"Carbamazepine is the first treatment for the disorders of mood that has been demonstrated to enhance a physiological response to clonidine."( Treatment with carbamazepine may enhance alpha 2-noradrenergic autoreceptor sensitivity.
Dilsaver, SC; Peck, JA; Swan, AC; Traumata, D, 1993
)
1.36
"Carbamazepine treatment normalized REM sleep variables, damped the amplitude of mood cycling of the patient, increased TSH and decreased FT4."( 48-hour rapid cycling: results of psychopathometric, polysomnographic, PET imaging and neuro-endocrine longitudinal investigations in a single case.
Berger, M; Dressing, H; Gann, H; Hohagen, F; Müller, WE; Riemann, D; Strauss, LG, 1993
)
1.01
"Carbamazepine treatment increased EEG fast alpha power and self-rated fatigue, and decreased self-rated concentration and vigor."( Carbamazepine and cocaine-cue reactivity.
Bauer, LO; Hersh, D; Kranzler, HR, 1995
)
2.46
"Carbamazepine pretreatment enhanced chloride uptake after diazepam withdrawal but did not modify chloride flux in stressed or unstressed vehicle-treated rats."( Carbamazepine normalizes the altered behavioral and neurochemical response to stress in benzodiazepine-withdrawn rats.
Lacerra, C; Martijena, ID; Molina, VA, 1997
)
2.46
"Carbamazepine treatment alters the serum lipid profile of the children in such a way that it facilitates the development of atherosclerosis."( Carbamazepine and valproic acid: effects on the serum lipids and liver functions in children.
Demircioğlu, S; Dirik, E; Soylu, A, 2000
)
2.47
"Carbamazepine and depakine treatment during at least 6 months does not predispose to ovary polycystosis syndrome."( [The pharmacological and hormonal effects of carbamazepine and valproic acid in the treatment of reproductive age women with epilepsy].
Karlov, VA; Kushlinskiĭ, NE; Vlasov, PN, 2001
)
1.29
"The carbamazepine-treated group demonstrated a lower incidence of withdrawal symptoms rated according to the Physician Withdrawal Check List (p < 0.01), better results with the Hopkins Symptom Check List (Covi cluster, p < 0.01) and a more markedly reduced score with the Hamilton Rating Scale for Anxiety (p < 0.05)."( [The prophylaxis of benzodiazepine withdrawal syndrome in the elderly: the effectiveness of carbamazepine. Double-blind study vs. placebo].
Di Costanzo, E; Rovea, A,
)
0.83
"Carbamazepine treatment was used with 54 patients suffering from endogenous depression and organic depression. "( [Carbamazepine in the treatment of depressive syndromes].
Matkowski, K; Rybakowski, J,
)
2.48
"Carbamazepine treatment also produced an increase in the growth hormone response to subcutaneous administration of the dopamine agonist apomorphine hydrochloride (5 micrograms/kg)."( Effects of carbamazepine on dopamine- and serotonin-mediated neuroendocrine responses.
Cowen, PJ; Elphick, M; Yang, JD, 1990
)
1.39
"Carbamazepine treatment lowers the serum 25-OH-D concentration, and inactivity which leads to a lower degree of time spent out-of-doors and thus a low exposure to sunlight still decreases the concentration."( Vitamin D status of ambulatory and nonambulatory mentally retarded children with and without carbamazepine treatment.
Grönlund, T; Lamberg-Allardt, C; Saraste, KL; Wilska, M, 1990
)
1.22
"Carbamazepine treatment completely resolved his symptoms, with full normalization of EEG activity."( Nocturnal complex partial seizures precipitated by REM sleep. A case report.
De Domenico, P; Di Perri, R; Longo, M; Marabello, L; Mento, G; Musolino, R; Silvestri, R, 1989
)
1
"Carbamazepine-treated animals displayed higher levels of adenosine receptors in virtually all brain areas tested, most of which reached significance in the 11-day treatment group."( Chronic carbamazepine treatment increases brain adenosine receptors.
Cappabianca, AM; Marangos, PJ; Montgomery, P; Narang, PK; Patel, J; Post, RM; Weiss, SR,
)
1.29
"Carbamazepine treatment was associated with limited reductions in white blood cell indices."( Hematological effects of lithium potentiation of carbamazepine in patients with affective illness.
Joffe, RT, 1988
)
1.25
"Carbamazepine treatment improved sleep stability."( [Organization of sleep in recent temporal lobe epilepsy before and after treatment with carbamazepine].
Baldy-Moulinier, M; Besset, A; Billiard, M; Cadilhac, J; Touchon, J; Valmier, J, 1987
)
1.22
"Carbamazepine pretreatment was associated with significant increases in apparent Vmax,m and Km,m of epoxide formation."( Inhibition of epoxidation of carbamazepine by valproic acid in the isolated perfused rat liver.
Chang, SL; Levy, RH, 1985
)
1.28
"Carbamazepine effectively treated the depression and mania was avoided."( Carbamazepine in bipolar-depressed disorder complicated by tricyclic antidepressant switching: case report.
Finkel, JA; Nurnberg, HG, 1985
)
2.43
"Treatment with carbamazepine was initiated."( A woman in her sixties with epilepsy and syncope.
Engelsen, BA; Gradek, G; Midelfart-Hoff, J; Wendelbo, Ø, 2022
)
1.06
"Treatment with carbamazepine remains first-line therapy, although other membrane stabilizing agents and surgical interventions can be effective."( Ocular neuromyotonia: a review of diagnosis and treatment.
Lee, MS; Lee, SK, 2022
)
1.06
"Treatment with carbamazepine failed in two children due to drowsiness and auditory disturbance."( Lacosamide for children with paroxysmal kinesigenic dyskinesia.
Furukawa, G; Ishihara, N; Negishi, Y; Okumura, A; Takeuchi, T, 2020
)
0.9
"Treatment with carbamazepine was also a protective factor against uncontrolled seizures for families with LGI1 mutations (OR = 0.248, 95% CI: 0.085-0.724, p = 0.011)."( Factors predicting uncontrolled seizures in epilepsy with auditory features.
Chen, L; Zhang, L; Zhu, X; Zou, X, 2019
)
0.85
"Treatment with carbamazepine resulted in the complete reversal of the paroxysmal ataxia and dysarthria."( Paroxysmal ataxia and dysarthria in multiple sclerosis.
Batocchi, AP; Capone, F; Iorio, R; Plantone, D, 2014
)
0.74
"Oral treatment of carbamazepine was started but her seizures were not controlled."( Serial EEG study in a girl with Landau-Kleffner syndrome associated with continuous spikes and waves during slow sleep.
Arisaka, O; Imataka, G, 2014
)
0.73
"Treatment with carbamazepine was effective."( Midbrain lesions and paroxysmal dysarthria in multiple sclerosis.
Blanco, Y; Compta, Y; Graus, F; Saiz, A, 2008
)
0.69
"Treatment with carbamazepine not only controlled hyperkinetic motor seizures but also helped interictal inattentiveness and behavioral impulsivity."( A case with hyperkinetic frontal lobe epilepsy presenting as a psychiatric disturbance.
Elmi, H; Kilinçaslan, A; Oztürk, M; Yapici, Z,
)
0.47
"Treatment with carbamazepine provided significant analgesic relief in terms of both the frequency and intensity of pain."( A new variant nummular headache: large diameter accompanied with bitrigeminal hyperalgesia and successful treatment with carbamazepine.
Li, LS; Man, YH; Mao, XJ; Wu, J; Yao, G; Yu, TM, 2012
)
0.93
"A treatment with carbamazepine was started and proved to be successful."( Complex visual hallucinations in a Parkinson patient: don't blame James if it's Charles's fault.
Segers, K, 2013
)
0.72
"Treatment with carbamazepine could not prevent these painful sensations, but a selective amygdalohippocampectomy completely controlled the episodic pain and the seizures associated with loss or alteration of consciousness."( Epilepsy with severe abdominal pain.
Eschle, D; Siegel, AM; Wieser, HG, 2002
)
0.65
"Treatment with carbamazepine (CBZ) is known to affect apolipoprotein B-containing lipoprotein concentrations in serum. "( Lipoprotein(a) concentration increases during treatment with carbamazepine.
Berthold, HK; Brämswig, S; Luers, C; Sudhop, T; von Bergmann, K, 2003
)
0.91
"Treatment with carbamazepine was effective, and the disorder evolved to total resolution in 4 to 8 weeks."( Neuropathic pain and dysesthesia of the feet after Himalayan expeditions.
Botella de Maglia, J; Misiego, M; Onaga Pueyo, H; Real Soriano, R; Ricart de Mesones, A; Turón Sans, J, 2002
)
0.65
"Treatment with carbamazepine (CBZ) in combination with parenteral diazepam induced both a dramatic increase of focal reflex proprioceptive seizures and choreoathetoid dyskinesias in the affected hand."( Carbamazepine, clonazepam and focal reflex proprioceptive seizures.
Contu, S; Corda, D; Deiana, GA; Rosati, G; Sechi, G,
)
1.91
"Treatment with carbamazepine normalized the abnormalities in transcallosal inhibition, but had no effect on other parameters."( Abnormal cortical and spinal inhibition in paroxysmal kinesigenic dyskinesia.
Berardelli, A; Bhatia, KP; Edwards, MJ; Gilio, F; Huang, YZ; Mir, P; Rothwell, JC, 2005
)
0.67
"If treatment with carbamazepine cannot be avoided, patients taking warfarin should be frequently monitored, especially when initiating or stopping carbamazepine therapy."( The influence of co-treatment with carbamazepine, amiodarone and statins on warfarin metabolism and maintenance dose.
Breskvar, K; Dolzan, V; Grabnar, I; Herman, D; Lainscak, M; Locatelli, I; Mrhar, A; Peternel, P; Stegnar, M, 2006
)
0.93
"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
"Treatment with carbamazepine resulted in substantial improvement of the symptoms within 7 days."( Acquired neuromyotonia (Isaacs' syndrome): a case report with autonomic physiologic studies.
Mitrabhakdi, E; Phanthumchinda, K; Sukajintanakarn, D, 2006
)
0.67
"Treatment with carbamazepine is associated with decreases in the serum levels of thyroxine, free thyroxine and triiodothyronine without alteration in the thyrotropin. "( Carbamazepine does not interact with thyroid hormone receptors in human fibroblasts.
Eil, C; Joffe, RT; Post, RM, 1984
)
2.06
"Treatment with carbamazepine or phenytoin was effective, but haloperidol increased the severity of the choreoathetoid attacks."( Therapeutic aspects of kinesiogenic paroxysmal choreoathetosis and familial paroxysmal choreoathetosis of the Mount and Reback type.
Monninger, P; Przuntek, H, 1983
)
0.61
"Treatment of carbamazepine overdose consists of aggressive orogastric lavage followed by activated charcoal administration with catharsis."( Acute carbamazepine intoxication: clinical spectrum and management.
May, DC, 1984
)
1.1
"Treatment with carbamazepine was of short-term benefit in most patients but failed to affect the long-term course of the disease."( Superior oblique myokymia.
Glaser, JS; Rosenberg, ML, 1983
)
0.61
"Treatment with carbamazepine, verapamil, and fluoxetine greatly improved the patient's symptoms."( Neurobehavioural dysfunction following mild traumatic brain injury in childhood: a case report with positive findings on positron emission tomography (PET).
Bushnell, DL; Hines, ME; Manshadi, FF; Roberts, MA, 1995
)
0.63
"Treatment with carbamazepine slow-release tablets in children with epilepsy can be replaced by carbamazepine suppositories in 25% higher dosage, with good clinical effect and appropriate pharmacokinetic values, when it is unsuitable to use the common oral route of administration."( Replacing carbamazepine slow-release tablets with carbamazepine suppositories: a pharmacokinetic and clinical study in children with epilepsy.
Arvidsson, J; Flesch, G; Nilsson, HL; Sandstedt, P; Steinwall, G; Tonnby, B, 1995
)
1.03
"Pretreatment with carbamazepine or valproate for 4 or 8 days combined with an injection immediately before noxious stimulation further significantly decreased the number of c-Fos neurons in the deep dorsal horn only in animals treated with valproate."( Anticonvulsants suppress c-Fos protein expression in spinal cord neurons following noxious thermal stimulation.
Castro-Lopes, JM; Evan, G; Schadrack, J; Tölle, TR; Zieglgänsberger, W, 1995
)
0.61
"On treatment with carbamazepine (n = 27) and phenytoin (n = 8), the excretion of alpha 1-microglobulin was significantly increased, as compared with the healthy controls."( Renal tubular dysfunction following treatment with anti-epileptic drugs.
Korinthenberg, R; Wehrle, L; Zimmerhackl, LB, 1994
)
0.61
"Treatment with carbamazepine was evaluated in an open study design in 29 gerontopsychiatric inpatients."( [Therapeutic use of carbamazepine for treatment of agitation and affective disorders in geriatric psychiatry patients].
Lemke, MR; Stuhlmann, W, 1994
)
0.95
"Treatment with carbamazepine was successful in both patients."( [Rapid cycling in bipolar disorders].
Hoogduin, CA; Knoppert-van der Klein, EA; Nolen, WA, 1994
)
0.63
"Treatment with carbamazepine raised serum total cholesterol levels, C-HDL, phospholipid and A-I apoprotein in all groups, low density lipoproteins in females and B apoprotein males."( [The effects of phenobarbital, valproic acid and carbamazepine on the serum lipids and lipoproteins in a pediatric population].
Braga Hernández, S; Crespo Hernández, M; de Juan Frigola, J, 1996
)
0.89
"Treatment with carbamazepine, initiated at age 7 months (corrected age of 5 months) has produced marked and continued resolution of myotonia, lessened malformation of her bell-shaped chest, and developmental progress."( Neonatal diagnosis of Schwartz-Jampel syndrome with dramatic response to carbamazepine.
Prangley, J; Squires, LA, 1996
)
0.87
"Treatment with carbamazepine in one patient and external beam radiation therapy in the second patient."( Ocular neuromyotonia in Graves dysthyroid orbitopathy.
Chung, SM; Cruz, OA; Holds, JB; Lee, AG; Roper-Hall, G, 1997
)
0.65
"Treatment with carbamazepine decreased plasma OE1S levels from a mean value of 810.8 to 411.6 pmol/l (mean suppression to 50.7% of pretreatment levels, P < 0.001)."( Differential effect of carbamazepine and valproate monotherapy on plasma levels of oestrone sulphate and dehydroepiandrosterone sulphate in male epileptic patients.
Berntsen, H; Engelsen, BA; Geisler, J; Geisler, S; Lønning, PE, 1997
)
0.95
"Treatment with carbamazepine was then started, reaching a dose of 1,200 mg/day and maintaining plasma levels of 8.8 mcg/ml."( [Organic personality disorder: response to carbamazepine].
González Torres, MA; Muñoz, P,
)
0.73
"Treatment with carbamazepine, an antiepileptic drug, suppressed the attacks including the associated urinary incontinence."( Paroxysmal urinary incontinence associated with multiple sclerosis.
Nagahama, Y; Ueda, T; Yoshida, O; Yoshimura, N, 1997
)
0.64
"Treatment with carbamazepine was successful in only one patient; in the other two subjects, their hiccups were controlled with haloperidol or baclofen."( Intractable hiccups during stroke rehabilitation.
Dromerick, AW; Kumar, A, 1998
)
0.64
"Pretreatment with carbamazepine provoked anti-immobility effects when tested in combination with RU 24969 (P<0.01) and 8-OH-DPAT (P<0.01), whereas prior administration of sodium valproate enhanced the antidepressant-like effects of (+/-) pindolol (P<0.01), 8-OH-DPAT (P<0.01) and RU 24969 (P<0.01)."( Evidence of the activity of lithium on 5-HT1B receptors in the mouse forced swimming test: comparison with carbamazepine and sodium valproate.
Bourin, M; Redrobe, JP, 1999
)
0.84
"Treatment with carbamazepine (CBZ) affects cholesterol concentrations, but little is known about the precise nature and underlying mechanisms of changes in lipoprotein metabolism. "( Carbamazepine increases atherogenic lipoproteins: mechanism of action in male adults.
Berthold, HK; Brämswig, S; Kerksiek, A; Luers, C; Sudhop, T; Von Bergmann, K, 2002
)
2.11
"Treatment with carbamazepine led to clinical improvement in behaviour, reduction in the paroxysms and appearance of sleep spindles, but little effect on the degree of aphasia."( [Landau kleffner syndrome].
Bernal, M; Carvajal, P; Pablo, MJ; Peralta, P; Sáenz de Cabezón, A; Valdizán, JR,
)
0.47
"Pre-treatment with carbamazepine increases the rate of formation of carbamazepine epoxide in rat liver microsomal preparations."( Activity of liver microsomal mono-oxygenases on some epoxide-forming cyclic tricyclic drugs. I. Kinetics in vitro.
Belvedere, G; Cantoni, L; Frigerio, A; Mussini, E; Pachecka, J; Pantarotto, C; Salmona, M, 1976
)
0.57
"Treatment with carbamazepine 200-400 mg three times daily led to disappearance or great improvement of flutter and clinical symptoms in all three patients."( High-frequency diaphragmatic flutter: symptoms and treatment by carbamazepine.
Decramer, M; Harlet, R; Vantrappen, G, 1992
)
0.86
"Treatment with carbamazepine resulted in a statistically, but not clinically, significant decrease in serum sodium levels in patients receiving anticonvulsant polytherapy."( Carbamazepine-induced hyponatremia in patients with mental retardation.
Friedman, DL; Kastner, T; Pond, WS, 1992
)
2.07
"Treatment with carbamazepine attenuated (P less than 0.10) this increase."( Chronic benzodiazepine administration. IX. Attenuation of alprazolam discontinuation effects by carbamazepine.
Browne, TR; Galpern, WR; Greenblatt, DJ; Miller, LG; Shader, RI; Szabo, GK, 1991
)
0.84
"Treatment with carbamazepine reduced CSF somatostatin (p less than .01) in contrast to the absence of effect of imipramine, desmethylimipramine, and lithium carbonate and the significant increase in CSF somatostatin seen in a small group of patients treated with zimelidine."( CSF somatostatin in affective illness and normal volunteers.
Ballenger, JC; Gold, PW; Post, RM; Rubinow, DR, 1985
)
0.61
"Treatment with carbamazepine was successful in reducing the attacks as might be expected in partial seizures."( Paroxysmal appearing palsy of epileptic origin.
Dierckx, R; Ebinger, G; Formisano, R; Van der Niepen, P; Volckaert, A,
)
0.47
"Treatment with carbamazepine produced considerable symptomatic improvement."( Continuous motor unit activity confined to the upper extremities.
Fries, TJ; Tandan, R, 1988
)
0.61
"Treatment with carbamazepine was started again, and there was remission of the trigeminal neuralgia after several weeks."( Cluster-tic syndrome.
Klimek, A, 1987
)
0.61
"The treatment with carbamazepine has showed a very good response."( [Hemifacial spasm: report of a case].
Fortes-Rêgo, J, 1985
)
0.59

Toxicity

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.

ExcerptReferenceRelevance
" The neurotoxicity induced by carbamazepine may be involved in the teratogenic and adverse effects of overdose associated with the treatment of manic-depressive illness and seizures."( Carbamazepine-induced neurotoxicity and its prevention by NMDA in cultured cerebellar granule cells.
Chuang, DM; Gao, XM, 1992
)
2.01
"Rare, serious adverse effects of antiepileptic drugs (AEDs) include hepatotoxicity and bone marrow suppression."( Routine laboratory monitoring for serious adverse effects of antiepileptic medications: the controversy.
Wyllie, E; Wyllie, R, 1991
)
0.28
" Experts note that adverse drug reactions (ADRs) have become the 'greatest imitator' of disease in clinical medicine."( Distinguishing drug toxicity syndromes from medical diseases: a QMR computer-based approach.
Mabry, ME; Miller, RA, 1991
)
0.28
" 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
" In this series chronic exposure to carbamazepine did not appear to increase the risk of coma or respiratory depression for a given toxic serum level and may add some protective effect."( Carbamazepine overdose: a prospective study of serum levels and toxicity.
Cookson, E; Krenzelok, EP; Spiller, HA, 1990
)
2
" Other features of this adverse drug reaction were unremitting fever, leukocytosis with eosinophilia and atypical lymphocytosis, and proteinuria."( Phenobarbital hepatotoxicity in an 8-month-old infant.
Goldbach, M; Phillips, MJ; Roberts, EA; Spielberg, SP, 1990
)
0.28
" The introduction of oral erythromycin produces a two- to fourfold increase in the carbamazepine serum concentration and the resultant toxic manifestations."( Carbamazepine toxicity precipitated by intravenous erythromycin.
Mitsch, RA, 1989
)
1.94
" It is usually preferred to phenobarbitone or phenytoin because of its powerful antiepileptic activity combined with a relative lack of adverse effects."( Carbamazepine toxicity and poisoning. Incidence, clinical features and management.
Cavallo, R; Durelli, L; Massazza, U,
)
1.57
" Oral administration of CBZ as an aqueous suspension every 8 h at a dose of 250 mg/kg was continuously protective against HFDE-induced seizures and was minimally toxic as measured by weight gain over 8 weeks of treatment."( Chronic carbamazepine treatment in the rat: efficacy, toxicity, and effect on plasma and tissue folate concentrations.
Carl, GF; Smith, ML,
)
0.57
" The findings of this study are comparable with those of other series assessing carbamazepine-associated adverse reactions in children and adults."( Carbamazepine side effects in children and adults.
Pellock, JM, 1987
)
1.94
" These results show that barbiturates should not be first-choice drugs in patients who have a chronic disease such as epilepsy, and indicate a schedule for barbiturate withdrawal which is safe and independent of hospitalization or monitoring of antiepileptic drug serum concentrations."( Barbiturate-refractory epilepsy: safe schedule for therapeutic substitution.
Bittencourt, PR; Gorz, AM; Silvado, CE, 1986
)
0.27
" Indeed, although some form of side effect occurred in 50% of patients, treatment had to be changed in only 18% and the drug had to be stopped in only 7%."( Clinical side effects of phenobarbital, primidone, phenytoin, carbamazepine, and valproate during monotherapy in children.
Armijo, JA; Arteaga, R; Herranz, JL,
)
0.37
" However, carbamazepine consistently produced fewer adverse effects on tests of attention/concentration and motor performance than did the other three antiepileptic drugs."( Results of a nationwide Veterans Administration Cooperative Study comparing the efficacy and toxicity of carbamazepine, phenobarbital, phenytoin, and primidone.
Collins, JF; Craft, B; Cramer, JA; Mattson, RH; Novelly, RA; Smith, DB, 1987
)
0.89
" Two female patients in middle age with epilepsy had been treated with carbamazepine for more than 7 years when they experienced sudden visual disturbances and reduction of visual acuity without known concomitant systemic toxic effects."( Possible retinotoxic effect of carbamazepine.
Nielsen, NV; Syversen, K, 1986
)
0.79
" Concentrations of phenytoin considered therapeutic (10 and 20 micrograms/ml) and a dose considered acutely toxic (40 micrograms/ml) were used while carbamazepine levels of 8 micrograms/ml (therapeutic) and 10 and 16 micrograms/ml (acutely toxic) were tested."( Effects of phenytoin and carbamazepine on human natural killer cell activity and genotoxicity in vitro.
Coulombe, RA; Hincks, JR; Margaretten, NC; Warren, RP, 1987
)
0.78
" These side effects were dose related: ventricular tachycardia appeared at a toxic serum phenytoin level in one patient and disappeared as the concentration fell within the therapeutic range, and atrioventricular block grade 1 developed in two patients at low serum carbamazepine levels, its severity increasing with the drug level."( Cardiac side effects of phenytoin and carbamazepine. A dose-related phenomenon?
Durelli, L; Glorioso, N; Gusmaroli, G; Monaco, F; Mutani, R; Sechi, GP, 1985
)
0.72
" However, whereas toxic reactions following phenytoin and carbamazepine are characterised by a rather short duration of exposure before symptoms occur with accompanying clinical features of hypersensitivity, valproate-induced hepatic toxicity exhibits no signs of hypersensitivity and often occurs following prolonged exposure, speaking in favor of a metabolic aberration as the underlying cause."( Hepatic toxicity of antiepileptic drugs: a review.
Bentsen, KD; Gram, L, 1983
)
0.51
" At levels between 34 and 38 mumol/L adverse effects were inconsistently observed."( 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
)
0.5
" Serum carbamazepine levels were measured before, during, and, in most cases, after the toxic episodes."( Carbamazepine--erythromycin interaction leading to carbamazepine toxicity in four epileptic children.
Cate, JC; Hedrick, R; Lamb, WA; Morin, R; Williams, F, 1983
)
2.16
"All 10 patients tolerated the addition of an MAOI well, and mean self-rated side effect scores did not change significantly."( Addition of monoamine oxidase inhibitors to carbamazepine: preliminary evidence of safety and antidepressant efficacy in treatment-resistant depression.
Ketter, TA; Parekh, PI; Post, RM; Worthington, K, 1995
)
0.55
"Clinically significant cardiovascular toxicity occurs rarely in patients with toxic carbamazepine concentrations."( Cardiovascular effects of carbamazepine toxicity.
Apfelbaum, JD; Bossart, PJ; Caravati, EM; Kerns, WP; Larsen, G, 1995
)
0.82
"We evaluated the efficacy, development of adverse effects, and possible correlation between the plasma concentration of carbamazepine (CBZ) and its major metabolite, carbamazepine-10,11-epoxide (CBZ-E), in a group of epileptic patients in whom selective increases in CBZ doses were made."( Carbamazepine and its epoxide: an open study of efficacy and side effects after carbamazepine dose increment in refractory partial epilepsy.
Baulac, M; Gimenez, F; Laplane, D; Longer, E; Semah, F; Thuillier, A, 1994
)
1.94
"The pharmacokinetics, tolerability, and efficacy of carbamazepine (CBZ) and the pharmacokinetics of carbamazepine-10, 11-epoxide (CBZE) were studied after chronic administration of a conventional tablet formation or of the controlled-release (CR) formulation of CBZ 400 mg (Tegretol 400) to 20 patients with epilepsy treated with carbamazepine and complaining of intermittent adverse effects."( 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
)
0.77
"In order to assess whether doses or serum levels are predictive for the efficacy and adverse effects of antiepileptic drugs (AEDs), measures for exposure to drug combinations have to be used."( Neither dosage nor serum levels of antiepileptic drugs are predictive for efficacy and adverse effects.
Hekster, YA; Keyser, A; Lammers, MW; Meinardi, H; Renier, WO; van Lier, H, 1995
)
0.29
" Adverse effects of antiepileptic treatment may affect the patient's quality of life to an even greater extent than the occurrence of seizures."( Adverse effects of established and new antiepileptic drugs: an attempted comparison.
Gram, L; Rogvi-Hansen, B, 1995
)
0.29
" Since gaze-evoked nystagmus, dizziness, and ataxia are some of the typical adverse effects (AEs) of the dose-dependent toxicity of carbamazepine, preexisting CA could possible explain in part the interindividual variation in the tolerance of high serum concentrations of carbamazepine."( Cerebellar atrophy decreases the threshold of carbamazepine toxicity in patients with chronic focal epilepsy.
May, TW; Rohde, M; Schmidt, RC; Schütz, M; Specht, U; Wagner, V; Wolf, P, 1997
)
0.76
" Patients were slowly titrated to doses at which the first toxic AEs of carbamazepine occurred."( Cerebellar atrophy decreases the threshold of carbamazepine toxicity in patients with chronic focal epilepsy.
May, TW; Rohde, M; Schmidt, RC; Schütz, M; Specht, U; Wagner, V; Wolf, P, 1997
)
0.79
"Attention for adverse effects (AEs) is important for optimizing epilepsy treatment."( Adverse effects in epilepsy therapy. Wait and see or go for it?
Deckers, CL; Hekster, YA; Keyser, A; Lammers, MW; Meinardi, H; Renier, WO, 1997
)
0.3
" AWD 140-190 thus presents an orally active and safe anticonvulsant agent, which is structurally unrelated to anticonvulsants currently used."( AWD 140-190: a new anticonvulsant with a very good margin of safety.
Bartsch, R; Engel, J; Rostock, A; Rundfeldt, C; Tober, C; Unverferth, K; White, HS; Wolf, HH, 1997
)
0.3
" During clarithromycin coadministration, four out of the seven patients developed moderate-to-severe toxic symptoms of carbamazepine, such as drowsiness, dizziness, and ataxia, which resolved within 5 days after clarithromycin discontinuation."( Carbamazepine toxicity induced by clarithromycin coadministration in psychiatric patients.
Kaneko, S; Ohkubo, T; Otani, K; Shimoyama, R; Sugawara, K; Yasui, N, 1997
)
1.95
"05) change in the serum concentrations of either CBZ or its epoxide metabolite when LTG was added either to the group as a whole or to the nine patients who experienced adverse CNS effects."( Carbamazepine toxicity with lamotrigine: pharmacokinetic or pharmacodynamic interaction?
Berry, DJ; Besag, FM; Newbery, JE; Pool, F; Subel, B, 1998
)
1.74
" PB was also the most toxic drug, followed by CBZ and by PHT."( Anticonvulsant and neurotoxic effects of intracerebroventricular injection of phenytoin, phenobarbital and carbamazepine in an amygdala-kindling model of epilepsy in the rat.
Alós, M; Barcia, JA; Belda, V; Rubio, P; Serralta, A, 1999
)
0.52
" Two analyses of adverse events are presented: tolerability and safety."( Safety and tolerability of gabapentin as adjunctive therapy in a large, multicenter study.
Bernstein, P; Faught, RE; Holmes, GL; Magnus-Miller, L; McLean, MJ; Morrell, MJ; Privitera, MD; Rose-Legatt, A; Willmore, LJ, 1999
)
0.3
" Within these 281 patients, two mutually exclusive groups were compared (a) those reporting adverse events at only < or =1,800 mg/day (low dose); and (b) those reporting adverse events at only >1,800 mg/day (high dose)."( Safety and tolerability of gabapentin as adjunctive therapy in a large, multicenter study.
Bernstein, P; Faught, RE; Holmes, GL; Magnus-Miller, L; McLean, MJ; Morrell, MJ; Privitera, MD; Rose-Legatt, A; Willmore, LJ, 1999
)
0.3
"Gabapentin doses >1,800 mg/day were as well tolerated as doses < or =1,800 mg/day and were not associated with more adverse events."( Safety and tolerability of gabapentin as adjunctive therapy in a large, multicenter study.
Bernstein, P; Faught, RE; Holmes, GL; Magnus-Miller, L; McLean, MJ; Morrell, MJ; Privitera, MD; Rose-Legatt, A; Willmore, LJ, 1999
)
0.3
" We investigated whether this drug was comparable to standard first-line monotherapy in efficacy and incidence of adverse events."( Safety and efficacy of vigabatrin and carbamazepine in newly diagnosed epilepsy: a multicentre randomised double-blind study. Vigabatrin European Monotherapy Study Group.
Chadwick, D, 1999
)
0.57
" After initial maintenance doses were reached, doses were adjusted downwards (in the case of adverse events) or upwards (in the case of seizures) by the clinician."( Safety and efficacy of vigabatrin and carbamazepine in newly diagnosed epilepsy: a multicentre randomised double-blind study. Vigabatrin European Monotherapy Study Group.
Chadwick, D, 1999
)
0.57
"Time to withdrawal for lack of efficacy or adverse events did not differ between groups (p=0."( Safety and efficacy of vigabatrin and carbamazepine in newly diagnosed epilepsy: a multicentre randomised double-blind study. Vigabatrin European Monotherapy Study Group.
Chadwick, D, 1999
)
0.57
" Carbamazepine was restarted and the patient experienced no further adverse events."( Potential fluconazole-induced carbamazepine toxicity.
Morris, HH; Nair, DR,
)
1.33
" In this study, we examined the anticonvulsant and adverse effects of the three clinically established AEDs carbamazepine (CBZ), phenobarbital (PB), and valproate (VPA) once per month in the same two groups of amygdala-kindled rats over a period of 9 (group 1) or 6 (group 2) consecutive months."( Repeated acute testing of anticonvulsant drugs in amygdala kindled rats: increase in anticonvulsant but decrease in adverse effect potential.
Fiedler, M; Löscher, W, 2000
)
0.52
"These data demonstrate that repeated use of the same kindled rats for acute drug testing significantly alters the sensitivity of the animals to the anticonvulsant and adverse effects of drugs."( Repeated acute testing of anticonvulsant drugs in amygdala kindled rats: increase in anticonvulsant but decrease in adverse effect potential.
Fiedler, M; Löscher, W, 2000
)
0.31
" Further increment in dose was carried out at weekly intervals, guided by clinical improvement, serum levels and treatment emergent adverse events."( Carbamazepine and valproate monotherapy: feasibility, relative safety and efficacy, and therapeutic drug monitoring in manic disorder.
Goswami, U; Kohli, K; Vasudev, K, 2000
)
1.75
" Significantly more patients in the CBZ group reported adverse events, including nausea, vomiting and dizziness, than VPA."( Carbamazepine and valproate monotherapy: feasibility, relative safety and efficacy, and therapeutic drug monitoring in manic disorder.
Goswami, U; Kohli, K; Vasudev, K, 2000
)
1.75
" Treatment was discontinued in 7% because of adverse events."( Open study evaluating lamotrigine efficacy and safety in add-on treatment and consecutive monotherapy in patients with carbamazepine- or valproate-resistant epilepsy.
Jozwiak, S; Terczynski, A, 2000
)
0.52
" However, on rare occasions, they can progress to more severe cutaneous disorders, including Stevens-Johnson syndrome and toxic epidermal necrolysis."( Therapeutic safety monitoring: what to look for and when to look for it.
Harden, CL, 2000
)
0.31
" 23 patients (30%) had at least one adverse event (AE), but only 1/4 of all AEs might be reasonably regarded as an effect of the medication."( [Open study evaluating lamotrigine efficacy and safety in add-on treatment and consecutive monotherapy in adult patients with epilepsy resistant carbamazepine and valproate].
Jóźwiak, S; Mańko, E; Niedzielska, K; Terczyński, A,
)
0.33
" Lamotrigine is a safe and well-tolerated drug."( [Open study evaluating lamotrigine efficacy and safety in add-on treatment and consecutive monotherapy in adult patients with epilepsy resistant carbamazepine and valproate].
Jóźwiak, S; Mańko, E; Niedzielska, K; Terczyński, A,
)
0.33
" The most common adverse effect was paresthesia (n= 2)."( [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
" It's toxic influence on action potential in Purkinje fibres and 4 depolarization phase expresses clinically as the His bundle and atrioventricular blocks especially in patients with cardiologic disturbances."( [Cardiac toxicity of carbamazepine].
Klimaszyk, D; Łukasik-GŁebocka, M, 2002
)
0.63
" There was no significant difference between the two groups with respect to premature discontinuation due to adverse events."( Safety and tolerability of oxcarbazepine in elderly patients with epilepsy.
Beydoun, A; D'Souza, J; Kutluay, E; McCague, K, 2003
)
0.32
" OXC was well tolerated, with 13% of patients exiting because of adverse events."( 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 incidence of adverse events, which were mild in severity, was similar between all treatment groups, including the placebo group."( Safety, tolerability and pharmacokinetic profile of BIA 2-093, a novel putative antiepileptic agent, during first administration to humans.
Almeida, L; Soares-da-Silva, P, 2003
)
0.32
" All adverse events were mild in severity, except for 1 case of somnolence of moderate severity, which occurred in a subject receiving 1200 mg BIA 2-093."( 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
"Newly designed antiepileptic drugs (AEDs) are being evaluated for their efficacy in preventing seizures and for their toxic profiles."( Neurotoxicity induced by antiepileptic drugs in cultured hippocampal neurons: a comparative study between carbamazepine, oxcarbazepine, and two new putative antiepileptic drugs, BIA 2-024 and BIA 2-093.
Ambrósio, AF; Araújo, IM; Carvalho, AP; Carvalho, CM; Leal, EC; Malva, JO; Soares-da-Silva, P; Verdasca, MJ, 2004
)
0.54
"In all parameters assayed, OXC was more toxic than the other AEDs used."( Neurotoxicity induced by antiepileptic drugs in cultured hippocampal neurons: a comparative study between carbamazepine, oxcarbazepine, and two new putative antiepileptic drugs, BIA 2-024 and BIA 2-093.
Ambrósio, AF; Araújo, IM; Carvalho, AP; Carvalho, CM; Leal, EC; Malva, JO; Soares-da-Silva, P; Verdasca, MJ, 2004
)
0.54
" In recent years, several rating scales have been developed that focus on both common adverse effects and various aspects of HRQOL that are more relevant to this patient population."( Assessment of adverse events and quality of life in epilepsy: design of a new community-based trial.
Ficker, DM; Privitera, M, 2004
)
0.32
" The aim of the study was to evaluate the frequency of AED utilisation and reported adverse events, in a cohort of MS patients."( Antiepileptic medications in multiple sclerosis: adverse effects in a three-year follow-up study.
Battaglia, MA; Brichetto, G; Mancardi, GL; Messmer Uccelli, M; Solaro, C, 2005
)
0.33
"To explore the time course of treatment-emergent adverse events (AEs) during topiramate (TPM) adjunctive therapy."( Time course of adverse events in patients with localization-related epilepsy receiving topiramate added to carbamazepine.
Majkowski, J; Neto, W; Van Oene, J; Wapenaar, R, 2005
)
0.54
" Patient demographics, medications, type of surgery, seizure history, adverse events, CBZ doses and concentrations were evaluated."( Risk factors for carbamazepine elevation and toxicity following epilepsy surgery.
Bingaman, W; Hiremath, GK; Hovinga, C; Kotagal, P; Morris, H; Nelson, D; Wyllie, E, 2005
)
0.67
"The effect of levetiracetam (LEV) on the acute neurotoxic profiles of various antiepileptic drugs (carbamazepine [CBZ], phenytoin [PHT], phenobarbital [PB], valproate [VPA], lamotrigine [LTG], topiramate [TPM], oxcarbazepine [OXC], and felbamate [FBM]) was evaluated in the rotarod test, allowing the determination of median toxic doses (TD50 values) with respect to impairment of motor coordination in mice."( Levetiracetam selectively potentiates the acute neurotoxic effects of topiramate and carbamazepine in the rotarod test in mice.
Andres, MM; Cioczek-Czuczwar, A; Czuczwar, P; Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N; Wojcik-Cwikla, J, 2005
)
0.77
"Many adverse drug reactions are caused by the cytochrome P450 (CYP) dependent activation of drugs into reactive metabolites."( An in vitro approach to detect metabolite toxicity due to CYP3A4-dependent bioactivation of xenobiotics.
Grossi, P; Kanter, Rd; Monaci, S; Monshouwer, M; Turlizzi, E; Vignati, L, 2005
)
0.33
" The most common adverse events (10%) in the CDP were headache (32."( Long-term safety and tolerability of oxcarbazepine in children: a review of clinical experience.
Bourgeois, BF; D'Souza, J, 2005
)
0.33
" OXC was well tolerated, with the most common adverse events consisting of vertigo, tremor, somnolence, hypotension and nausea."( Oxcarbazepine is effective and safe in the treatment of neuropathic pain: pooled analysis of seven clinical studies.
Arghetti, S; Bianconi, C; Cavallotti, G; Di Palma, F; Galimberti, V; Jann, S; Magenta, P; Osio, M; Siciliano, G; Sterlicchio, M; Sterzi, R, 2005
)
0.33
" The rate of patients discontinuing treatment due to adverse events or a lack of efficacy was 19% with CBZ compared to 9% with LTG (not statistically different)."( The LAM-SAFE Study: lamotrigine versus carbamazepine or valproic acid in newly diagnosed focal and generalised epilepsies in adolescents and adults.
Bergmann, L; Kurlemann, G; Schmitz, B; Siemes, H; Steinhoff, BJ; Ueberall, MA, 2005
)
0.6
" No serious medical complications or adverse events were observed except for one case of delirium tremens."( Efficacy and safety of outpatient alcohol detoxification with a combination of tiapride/carbamazepine: additional evidence.
Schmidt, F; Schmidt, P; Soyka, M, 2006
)
0.56
"Results from this study give further evidence for a combination of tiapride and the anticonvulsant carbamazepine as an effective and safe treatment for outpatient alcohol detoxification in patients with moderate severity of withdrawal syndrome."( Efficacy and safety of outpatient alcohol detoxification with a combination of tiapride/carbamazepine: additional evidence.
Schmidt, F; Schmidt, P; Soyka, M, 2006
)
0.77
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
"To investigate the relationship between the serum concentration of the mono-hydroxy-derivative (MHD) of oxcarbazepine (OXC) and adverse effects (AEs) in epileptic patients on high-dose OXC therapy."( Relationship between serum mono-hydroxy-carbazepine concentrations and adverse effects in patients with epilepsy on high-dose oxcarbazepine therapy.
Bilo, L; Di Nocera, P; Fasiello, C; Italiano, D; Pisani, F; Ruosi, P; Striano, P; Striano, S, 2006
)
0.33
" Therefore, the authors summarise adverse events of greatest prevalence and/or greatest severity based on data derived predominately from studies of geriatric patients with epilepsy and/or other non-psychiatric indications."( Safety and tolerability of mood-stabilising anticonvulsants in the elderly.
Alldredge, B; Fenn, HH; Ketter, TA; Sommer, BR, 2006
)
0.33
" The authors present the cases of two children who developed relatively uncommon adverse effects to new anticonvulsant medications, including metabolic acidosis with topiramate and hyponatremia with oxcarbazepine."( New anticonvulsants--new adverse effects.
Tebb, Z; Tobias, JD, 2006
)
0.33
" In SH-SY5Y cells amitriptyline was severely toxic, while selegiline and paracetamol failed to show any toxic effect, and carbamazepine was only slightly toxic at the highest concentration."( The combined use of human neural and liver cell lines and mouse hepatocytes improves the predictability of the neurotoxicity of selected drugs.
Mannerström, M; Tähti, H; Toimela, T; Ylikomi, T, 2006
)
0.54
" Subsequently, the patient developed a possible adverse skin reaction to his antiretrovirals and was hospitalized."( Carbamazepine toxicity induced by lopinavir/ritonavir and nelfinavir.
Bates, DE; Herman, RJ, 2006
)
1.78
" Most common adverse events were somnolence, dizziness, and nausea."( Carbamazepine extended-release capsules use in bipolar disorder: efficacy and safety in adult patients.
Ginsberg, LD, 2006
)
1.78
"Carbamazepine extended-release capsules appear safe and efficacious for the treatment of bipolar disorder."( Carbamazepine extended-release capsules use in bipolar disorder: efficacy and safety in adult patients.
Ginsberg, LD, 2006
)
3.22
" The safety of CBZ-ERC was determined by comparing the adverse event profiles of patients on monotherapy versus those of patients on polytherapy."( Safety of carbamazepine extended-release capsules in bipolar disorder polypharmacy.
Ginsberg, LD, 2006
)
0.74
"We found that patients taking CBZ-ERC together with other agents (antipsychotics, antiepileptics, selective serotonin reuptake inhibitors and other antidepressants, anxiolytics, lithium, and attention-deficit/hyperactivity disorder medications) were no more likely to report gastrointestinal, nervous system, or cutaneous adverse events than patients on CBZ-ERC monotherapy."( Safety of carbamazepine extended-release capsules in bipolar disorder polypharmacy.
Ginsberg, LD, 2006
)
0.74
"These real-world data suggest that the occurrence of adverse events may not differ significantly between patients on CBZ-ERC monotherapy and those on polytherapy with multiple other agents."( Safety of carbamazepine extended-release capsules in bipolar disorder polypharmacy.
Ginsberg, LD, 2006
)
0.74
" The most frequent (>10%) adverse events were dizziness, nausea, headache, somnolence, and fatigue."( Efficacy, safety, and tolerability of oxcarbazepine monotherapy.
Barkley, GL; Blakeslee, M; D'Souza, J; Ingenito, A; Martinez, W; McCague, K, 2006
)
0.33
" Their detection in the environment and their bioactivity have resulted in concern for potential adverse effects on non-target species."( Aquatic toxicity of acetaminophen, carbamazepine, cimetidine, diltiazem and six major sulfonamides, and their potential ecological risks in Korea.
Choi, K; Jung, J; Kim, PG; Kim, Y; Park, J; Park, S, 2007
)
0.62
" Safety was assessed by monitoring adverse events (AEs), serious AEs (SAEs), hematology, blood chemistry, urinalysis values, and vital signs."( Long-term safety and tolerability of oxcarbazepine in painful diabetic neuropathy.
Alarcón, F; Beydoun, S; Mangat, S; Wan, Y, 2007
)
0.34
" A secondary goal was to demonstrate quantitatively the relationship between the risk of neurological adverse effects to orally ingested CBZ and the rate of absorption."( Exposure-response analysis reveals that clinically important toxicity difference can exist between bioequivalent carbamazepine tablets.
Endrenyi, L; Speidl, S; Tothfalusi, L, 2008
)
0.56
" Following an exploratory data analysis step, a mixed-effect pharmacokinetic-pharmacodynamic (PK-PD) model was built to describe the dependence of adverse events on the CBZ concentration."( Exposure-response analysis reveals that clinically important toxicity difference can exist between bioequivalent carbamazepine tablets.
Endrenyi, L; Speidl, S; Tothfalusi, L, 2008
)
0.56
"Rapid development of tolerance was demonstrated for most neurological adverse effects, with a characteristic half-life of 02."( Exposure-response analysis reveals that clinically important toxicity difference can exist between bioequivalent carbamazepine tablets.
Endrenyi, L; Speidl, S; Tothfalusi, L, 2008
)
0.56
"In clinical and regulatory considerations, the development of acute tolerance for adverse effects of CBZ must be taken into account."( Exposure-response analysis reveals that clinically important toxicity difference can exist between bioequivalent carbamazepine tablets.
Endrenyi, L; Speidl, S; Tothfalusi, L, 2008
)
0.56
"Idiosyncratic hepatotoxicity is a well-known complication associated with aromatic antiepileptic drugs (AAED), and it has been suggested to occur due to the accumulation of toxic arene oxide metabolites."( Aromatic antiepileptic drugs and mitochondrial toxicity: effects on mitochondria isolated from rat liver.
Curti, C; Martins, NM; Medina, WS; Mingatto, FE; Santos, AC; Santos, NA, 2008
)
0.35
"The aim of this study was to investigate the relationships between oxcarbazepine (OXC) dosage, metabolite mono-hydroxy-derivative (MHD) serum concentrations, number of concomitant antiepileptic drugs, age and incidence of adverse events (AEs) in epileptic patients."( Oxcarbazepine and adverse events: impact of age, dosage, metabolite serum concentrations and concomitant antiepileptic therapy.
Foschi, N; Ortenzi, A; Paggi, A; Pistoli, E; Sabbatini, D,
)
0.13
" Adverse effects were rated before treatment onset, at day 3, then every week and at discharge or at discontinuation."( Efficiency and safety of oxcarbazepine in mood disorders: a naturalistic study exploring the interest of plasma dosages.
Droulout, T; Grolleau, A; Misdrahi, D; Molimard, M; Titier, K; Tournier, M; Verdoux, H, 2008
)
0.35
" However, the clinical use of these drugs is limited by several adverse effects, mainly idiosyncratic hepatotoxicity."( Involvement of oxidative stress in the hepatotoxicity induced by aromatic antiepileptic drugs.
Curti, C; Martins, NM; Medina, WS; Rodrigues, MA; Santos, AC; Santos, NA, 2008
)
0.35
" Adverse events were systematically recorded throughout the study."( 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
" A significantly greater number of patients in divalproex group experienced one or more adverse drug events as compared to patients in the oxcarbazepine group (66."( 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
" Also the overall adverse event profile was found to be superior for oxcarbazepine."( 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
"To evaluate and to compare the possible toxic effects of oxcarbazepine (OXC) and valproic acid (VPA) on retinal ganglion cells (RGCs) in rat."( Retinal ganglion cell toxicity due to oxcarbazepine and valproic acid treatment in rat.
Aktaş, Z; Cansu, A; Erdoğan, D; Goktas, G; Ozdek, S; Serdaroglu, A; Take, G, 2009
)
0.35
"OXC seems to be toxic to RGCs at 100mg/kg dose when it is been given as a monotherapy or combined with VPA."( Retinal ganglion cell toxicity due to oxcarbazepine and valproic acid treatment in rat.
Aktaş, Z; Cansu, A; Erdoğan, D; Goktas, G; Ozdek, S; Serdaroglu, A; Take, G, 2009
)
0.35
"In epilepsy, slow-release formulations of carbamazepine (CBZ) have fewer adverse events (AEs) compared with immediate-release (IR) formulations."( Adverse event load in bipolar participants receiving either carbamazepine immediate-release or extended-release capsules: a blinded, randomized study.
Chopra, AS; El-Mallakh, RS; Mickus, GJ; Penagaluri, P; Salem, MR, 2009
)
0.86
"Antiepileptic drugs (AEDs) have been widely used in patients with epilepsy but the adverse effects in adult Chinese patients have not been investigated."( Adverse effects of carbamazepine, phenytoin, valproate and lamotrigine monotherapy in epileptic adult Chinese patients.
Wang, X; Xi, Z; Yan, Y; Zeng, K, 2010
)
0.69
" An adverse effect profile, as well as efficacy of monotherapy, was obtained through a face-to-face interview with the patient at each visit."( Adverse effects of carbamazepine, phenytoin, valproate and lamotrigine monotherapy in epileptic adult Chinese patients.
Wang, X; Xi, Z; Yan, Y; Zeng, K, 2010
)
0.69
" Overall, 18% of patients experienced adverse effects: for CBZ (25/168; 14."( Adverse effects of carbamazepine, phenytoin, valproate and lamotrigine monotherapy in epileptic adult Chinese patients.
Wang, X; Xi, Z; Yan, Y; Zeng, K, 2010
)
0.69
" No fatal adverse events occurred."( Adverse effects of carbamazepine, phenytoin, valproate and lamotrigine monotherapy in epileptic adult Chinese patients.
Wang, X; Xi, Z; Yan, Y; Zeng, K, 2010
)
0.69
"There were no serious adverse drug reactions reported during this study."( Safety profile of oxcarbazepine: results from a prescription-event monitoring study.
Buggy, Y; Fogg, C; Layton, D; Shakir, SA, 2010
)
0.36
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" Adverse effects were observed in 11."( [Efficacy and safety of the monotherapy with trileptal (oxcarbazepine) in children and adolescents].
, 2010
)
0.36
" The low frequency and intensity of adverse effects during the treatment with trileptal was observed: there were 93 adverse effects in 60 patients included in the trial; 3 (3."( [Efficacy and safety of the mono- and combined therapy with oxcarbazepine in adult patients].
Badalian, OL; Burd, SG; Glukhova, LIu, 2010
)
0.36
" In this study, the toxic effects of carbamazepine (CBZ), an anticonvulsant drug commonly present in surface and groundwater, was studied in juvenile rainbow trout, Oncorhynchus mykiss, by acute semi-static bioassay."( Acute toxicity of carbamazepine to juvenile rainbow trout (Oncorhynchus mykiss): effects on antioxidant responses, hematological parameters and hepatic EROD.
Grabic, R; Kolarova, J; Li, P; Li, ZH; Machova, J; Randak, T; Velisek, J; Zlabek, V, 2011
)
0.98
"Co-administration of phenytoin and oxcarbazepine resulted in toxic levels of phenytoin."( Phenytoin toxicity secondary to an oxcarbazepine-phenytoin 2C19 interaction.
Kane, AJ; Soskin, DP; Stern, TA,
)
0.13
" Genetic analysis of DHS patients has revealed a striking association between carbamazepine (CBZ)-induced severe bullous reactions, such as Steven-Johnson Syndrome, and toxic epidermal necrolysis in individuals from Southeast Asia who carry a specific HLA allele (HLA-B*1502)."( Severe bullous hypersensitivity reactions after exposure to carbamazepine in a Han-Chinese child with a positive HLA-B*1502 and negative in vitro toxicity assays: evidence for different pathophysiological mechanisms.
Bend, JR; Elzagallaai, AA; Finkelstein, Y; Garcia-Bournissen, F; Koren, G; Rieder, MJ, 2011
)
0.84
" Adverse effects were observed in 11."( [Efficacy and safety of the monotherapy with trileptal (oxcarbazepine) in children and adolescents].
Belousova, ED; Ermolenko, NA; Guzeva, VI; Mironov, MB; Mukhin, KIu; Petrukhin, AS; Tysiachina, MD, 2010
)
0.36
" Overall, DCF was the most cytotoxic drug for zebra mussel cells, followed by GEM, CBZ, while ATL has not a noteworthy toxic potential."( Cytotoxicity assessment of four pharmaceutical compounds on the zebra mussel (Dreissena polymorpha) haemocytes, gill and digestive gland primary cell cultures.
Binelli, A; Parolini, M; Provini, A; Quinn, B, 2011
)
0.37
" Our work showed that adverse effects in epileptics under high doses of AVP was related to the association of the AVP with other antiepileptic in particular carbamazépine, phenobarbital and benzodiazepines rather than supra-therapeutic plasmatic concentrations of AVP."( [Relationship between plasma concentrations of valproic acid and hepatotoxicity in patients receiving high doses].
Atheymen, R; Ben Mahmoud, L; Ghozzi, H; Hakim, A; Hammami, S; Sahnoun, Z; Zeghal, K,
)
0.13
"LTG is generally an effective and safe treatment for management of TN, compared to CBZ."( Lamotrigine for trigeminal neuralgia: efficacy and safety in comparison with carbamazepine.
Abd Rahman, RB; Shaikh, S; Yaacob, HB, 2011
)
0.6
"In recent years, phenobarbital, as an antiepileptic drug, has become less popular based on adverse events, especially cognitive and behavioural side effects."( Side effects of phenobarbital in epilepsy: a systematic review.
Li, YP; Zeng, LN; Zhang, LL, 2011
)
0.37
" The determination of adverse effects of combined antiepileptic drugs (AEDs) from different studies was complicated by numerous factors including study design, different descriptions of adverse events and a lack of standardised data collection."( Side effects of phenobarbital in epilepsy: a systematic review.
Li, YP; Zeng, LN; Zhang, LL, 2011
)
0.37
"Phenobarbital was associated with a higher rate of drug withdrawal although there was no evidence to suggest that phenobarbital caused more adverse events compared to carbamazepine, valproic acid or phenytoin."( Side effects of phenobarbital in epilepsy: a systematic review.
Li, YP; Zeng, LN; Zhang, LL, 2011
)
0.56
" 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
" Safety was assessed by treatment-emergent adverse events (TEAEs), vital signs, weight, and extrapyramidal symptoms (EPSs)."( Safety and efficacy of olanzapine monotherapy and olanzapine with a mood stabilizer in 18-week treatment of manic/mixed episodes for Japanese patients with bipolar I disorder.
Higuchi, T; Kanba, S; Katagiri, H; Takahashi, M; Takita, Y; Tohen, M, 2012
)
0.38
"There were no deaths or serious adverse events considered potentially related to olanzapine in the monotherapy group (N = 100) or the combination-therapy group (N = 39)."( Safety and efficacy of olanzapine monotherapy and olanzapine with a mood stabilizer in 18-week treatment of manic/mixed episodes for Japanese patients with bipolar I disorder.
Higuchi, T; Kanba, S; Katagiri, H; Takahashi, M; Takita, Y; Tohen, M, 2012
)
0.38
" 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
" Tizanidine-induced adverse effects were examined in 100 patients treated with coadministration of tizanidine and 8 CYP1A2 inhibitors."( [Clinical survey of tizanidine-induced adverse effects--impact of concomitant drugs providing cytochrome P450 1A2 modification--].
Homma, M; Kohda, Y; Matsumoto, S; Momo, K; Sasaki, T, 2013
)
0.39
"Analysis of overall tolerability and neurological adverse effects (AEs) of eslicarbazepine acetate (ESL), lacosamide (LCM) and oxcarbazepine (OXC) from double-blind, placebo-controlled trials."( Neurological adverse events of new generation sodium blocker antiepileptic drugs. Meta-analysis of randomized, double-blinded studies with eslicarbazepine acetate, lacosamide and oxcarbazepine.
Fadda, V; Giovannelli, F; Maratea, D; Verrotti, A; Zaccara, G, 2013
)
0.39
" Adverse event types reflected the drug's established profile."( 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
" Adverse event occurrence and discontinuations due to adverse events suggest improved tolerability vs previously published data with immediate-release OXC."( 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
"Carbamazepine overdose is a common, toxic ingestion, manifesting as central nervous system (CNS) and respiratory depression."( Successful treatment of severe carbamazepine toxicity with 5% albumin-enhanced continuous venovenous hemodialysis.
Cole, M; Narayan, R; Rizzo, M, 2014
)
2.13
" Of particular concern is the occurrence of pharmaceutical mixtures, which may lead to increased adverse effects compared to individual compounds."( Individual and mixture toxicity of pharmaceuticals naproxen, carbamazepine, and sulfamethoxazole to Australian striped marsh frog tadpoles (Limnodynastes peronii).
Cameron, MC; Lanctôt, CM; Melvin, SD, 2014
)
0.64
" Our data suggest that valproate has adverse effects on renal tubular functions."( Does nephrotoxicity exist in pediatric epileptic patients on valproate or carbamazepine therapy?
Buyan, N; Demir, E; Gücüyener, K; Gülbahar, Ö; Gürkaş, E; Havali, C; Serdaroğlu, A; Yılmaz, Ü, 2015
)
0.65
" Safety assessments included treatment-emergent adverse events (TEAEs) and clinical laboratory parameters."( 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
)
0.65
" There were no reports of Stevens-Johnson syndrome or toxic epidermal necrolysis in either group."( 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
)
0.65
" Taking all together, this demo-case study showed that inclusion of multiple-endpoints in ZET may increase the sensitivity of the assay, contribute to the elucidation of the mode of toxic action and to a better definition of the applicability domain of ZET."( Zebrafish embryotoxicity test for developmental (neuro)toxicity: Demo case of an integrated screening approach system using anti-epileptic drugs.
Beker van Woudenberg, A; Bouma, M; de Groot, D; Hermsen, S; Menke, A; Piersma, A; Rijkmans, E; Snel, C; Wolterbeek, A, 2014
)
0.4
" These toxic effects can be negated by using antioxidant agent."( Carbamazepine toxic effects in chick cardiomyocyte micromass culture and embryonic stem cell derived cardiomyocyte systems--possible protective role of antioxidants.
Garle, MJ; Latif, ML; Memon, S; Parker, TL; Pratten, MK; Qureshi, WM, 2014
)
1.85
" It is being used more and more widely in clinical practice, but its adverse effects should not be ignored."( [Adverse effects of oxcarbazepine].
Fang, S; Gong, ZC, 2015
)
0.42
"00μg/L seemed to be a "threshold" concentration, beyond which the concentration levels of CBZ began to exert a toxic effect, compromising the activity of biotransformation and antioxidant enzymes, with notorious effects at the highest CBZ concentration (9."( Chronic toxicity of the antiepileptic carbamazepine on the clam Ruditapes philippinarum.
Almeida, Â; Calisto, V; Esteves, VI; Figueira, E; Freitas, R; Schneider, RJ; Soares, AM,
)
0.4
" This systematic review aimed to assess the prevalence of their adverse effects (AEs) and to provide recommendations on their clinical management."( Management of adverse effects of mood stabilizers.
Hidalgo, D; León-Caballero, J; Murru, A; Pacchiarotti, I; Popovic, D; Vieta, E, 2015
)
0.42
" Adverse effects include somnolence and weight decrease, but data suggest that long-term treatment with ZNS is safe with only rare newly occurring adverse effects, and good long-term tolerability also regarding mood, behavior, cognition and bone maturation."( The safety and long-term efficacy of zonisamide as adjunctive therapy for focal epilepsy.
Schulze-Bonhage, A, 2015
)
0.42
" Treatment-emergent adverse events occurred in 82% (CBZ/OXC), 76% (LTG), 73% (LEV), and 67% (VPA) of patients; most were of mild-to-moderate intensity."( 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
" The aim of this study was to examine the frequency of the adverse events of antiepileptic drugs (AEDs), in particular carbamazepine (CBZ) and oxcarbazepine (OXC) in patients with neuralgiform pain using the psychometrically tested Liverpool Adverse Events Profile (AEP) and provide clinicians with guidance as to when to change management."( Comparison of tolerability and adverse symptoms in oxcarbazepine and carbamazepine in the treatment of trigeminal neuralgia and neuralgiform headaches using the Liverpool Adverse Events Profile (AEP).
Besi, E; Boniface, DR; Cregg, R; Zakrzewska, JM, 2015
)
0.86
" At each consultation they completed the AEP questionnaire which provides scores of 19-76 with toxic levels being considered as scores >45."( Comparison of tolerability and adverse symptoms in oxcarbazepine and carbamazepine in the treatment of trigeminal neuralgia and neuralgiform headaches using the Liverpool Adverse Events Profile (AEP).
Besi, E; Boniface, DR; Cregg, R; Zakrzewska, JM, 2015
)
0.65
" Potential toxic dose for females is approximately 1200 mg of OXC and 800 mg of CBZ and1800mg of OXC and 1200 mg of CBZ for males."( Comparison of tolerability and adverse symptoms in oxcarbazepine and carbamazepine in the treatment of trigeminal neuralgia and neuralgiform headaches using the Liverpool Adverse Events Profile (AEP).
Besi, E; Boniface, DR; Cregg, R; Zakrzewska, JM, 2015
)
0.65
" Potentially, females need to be prescribed lower dosages in view of their tendency to reach toxic levels at lower dosages."( Comparison of tolerability and adverse symptoms in oxcarbazepine and carbamazepine in the treatment of trigeminal neuralgia and neuralgiform headaches using the Liverpool Adverse Events Profile (AEP).
Besi, E; Boniface, DR; Cregg, R; Zakrzewska, JM, 2015
)
0.65
"To evaluate the relationship between serum concentrations of mono-hydroxy-carbazepine (MHD), the main metabolite of oxcarbazepine (OXC), and the occurrence of adverse effects (AE) in a large group of patients on OXC monotherapy."( Relationship between mono-hydroxy-carbazepine serum concentrations and adverse effects in patients on oxcarbazepine monotherapy.
May, TW; Sattler, A; Schaefer, M, 2015
)
0.42
"In patients taking antiepileptic drugs (AEDs) for epilepsy, adverse effects (AEs) often lead to unfavorable quality of life, impaired adherence, and, eventually, discontinuation of pharmacological treatment."( Specific adverse effects of antiepileptic drugs--A true-to-life monotherapy study.
Fidzinski, P; Gaus, V; Holtkamp, M; Kowski, AB; Losch, F; Weissinger, F, 2016
)
0.43
"All patients ≥16years of age with epilepsy for ≥12months were routinely asked to complete the Liverpool Adverse Event Profile (LAEP) just before their appointment."( Specific adverse effects of antiepileptic drugs--A true-to-life monotherapy study.
Fidzinski, P; Gaus, V; Holtkamp, M; Kowski, AB; Losch, F; Weissinger, F, 2016
)
0.43
" In this research, we have explored the feasibility of retrospectively mapping population-level adverse events from the FDA Adverse Event Reporting System (FAERS) to chemical and biological databases to identify drug safety signals and the underlying molecular mechanisms."( Improving drug safety with a systems pharmacology approach.
Bojunga, N; Lesko, LJ; Schotland, P; Trame, MN; Zien, A, 2016
)
0.43
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
0.43
"This study provides evidence that CBZ is safe and rapidly effective in neonates with BFNE, even in status epilepticus."( Rapid and safe response to low-dose carbamazepine in neonatal epilepsy.
Bakken, EH; Balestri, M; Bellini, G; Cilio, MR; Danhaive, O; Holmes, GL; Mulkey, SB; Oldham, MS; Sands, TT; Taglialatela, M; Vigevano, F, 2016
)
0.71
" Treatment-emergent adverse events were reported in 328 (74%) patients receiving lacosamide and 332 (75%) receiving carbamazepine-CR."( Efficacy, safety, and tolerability of lacosamide monotherapy versus controlled-release carbamazepine in patients with newly diagnosed epilepsy: a phase 3, randomised, double-blind, non-inferiority trial.
Baulac, M; Brock, M; De Backer, M; Li, T; Rosenow, F; Terada, K; Toledo, M; Werhahn, KJ, 2017
)
0.89
"Antiepileptic drugs do cause adverse effects, affecting patients' quality of life, adherence and seizures."( Adverse effects of carbamazepine monotherapy among patients in Nigeria: a pilot study and implications.
Danesi, M; Fadare, J; Godman, B; Ogunleye, O; Olusanya, A, 2017
)
0.78
"Descriptive cross-sectional study assessing the extent of adverse effects with carbamazepine monotherapy and potential factors."( Adverse effects of carbamazepine monotherapy among patients in Nigeria: a pilot study and implications.
Danesi, M; Fadare, J; Godman, B; Ogunleye, O; Olusanya, A, 2017
)
1.01
"3%) reported no adverse effects, while 30 did."( Adverse effects of carbamazepine monotherapy among patients in Nigeria: a pilot study and implications.
Danesi, M; Fadare, J; Godman, B; Ogunleye, O; Olusanya, A, 2017
)
0.78
"Perception of adverse effects was common in patients on carbamazepine monotherapy, more common in women than men."( Adverse effects of carbamazepine monotherapy among patients in Nigeria: a pilot study and implications.
Danesi, M; Fadare, J; Godman, B; Ogunleye, O; Olusanya, A, 2017
)
1.03
"Carbamazepine (CBZ) is an antiepileptic drug commonly detected in aquatic systems, with toxic effects to inhabiting organisms."( Toxicity associated to uptake and depuration of carbamazepine in the clam Scrobicularia plana under a chronic exposure.
Almeida, Â; Calisto, V; Esteves, VI; Figueira, E; Freitas, R; Schneider, RJ; Soares, AMVM, 2017
)
2.15
" We verified the feasibility of using synchrotron-based Fourier Transform Infrared (SR-FTIR) spectromicroscopy to explore in vivo toxic effects on single living Chlorococcum sp."( 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
)
0.73
" Side effects like genotoxic effects of AEDs are of prime importance resulting from toxic metabolites, free radicals and reactive oxygen species (ROS)."( The genotoxic effect of oxcarbazepine on mice blood lymphocytes.
Akbar, H; Begum, I; Khan, A; Khisroon, M; Mohammadzai, I, 2018
)
0.48
" This study compared adverse event (AE) reporting rates for brand vs."( Comparison of brand versus generic antiepileptic drug adverse event reporting rates in the U.S. Food and Drug Administration Adverse Event Reporting System (FAERS).
Alatawi, Y; Berg, RL; Cheng, N; Hansen, RA; Page, D; Peissig, PL; Plotkina, AV; Qian, J; Rahman, MM, 2017
)
0.46
" Food and Drug Administration Adverse Event Reporting System between January 2004 to March 2015 with lamotrigine, carbamazepine, and oxcarbazepine listed as primary or secondary suspect were classified as brand, generic, or AG based on the manufacturer."( Comparison of brand versus generic antiepileptic drug adverse event reporting rates in the U.S. Food and Drug Administration Adverse Event Reporting System (FAERS).
Alatawi, Y; Berg, RL; Cheng, N; Hansen, RA; Page, D; Peissig, PL; Plotkina, AV; Qian, J; Rahman, MM, 2017
)
0.67
"Valproate alone or combined with another AED is associated with the greatest odds of adverse neurodevelopmental outcomes compared with control."( Comparative safety of antiepileptic drugs for neurological development in children exposed during pregnancy and breast feeding: a systematic review and network meta-analysis.
Cogo, E; D'Souza, J; Finkelstein, Y; Hemmelgarn, BR; Hutton, B; Kealey, R; MacDonald, H; Reynen, E; Rios, P; Soobiah, C; Straus, SE; Thavorn, K; Tricco, AC; Veroniki, AA; Yazdi, F, 2017
)
0.46
" This study highlighted the potential adverse effects generated in ozonation process and the oxidation of N-heterocyclic containing pollutants."( Chlorination, chloramination and ozonation of carbamazepine enhance cytotoxicity and genotoxicity: Multi-endpoint evaluation and identification of its genotoxic transformation products.
Han, Y; Hou, R; Huang, C; Li, N; Ma, M; Oda, Y; Wang, Z, 2018
)
0.74
" Rates of treatment-emergent adverse events were similar between groups for patients in the safety set."( Efficacy and safety of eslicarbazepine acetate versus controlled-release carbamazepine monotherapy in newly diagnosed epilepsy: A phase III double-blind, randomized, parallel-group, multicenter study.
Ben-Menachem, E; Elger, C; Keller, B; Kowacs, PA; Löffler, K; Rocha, JF; Soares-da-Silva, P; Trinka, E, 2018
)
0.71
" The aim of this observational cross-sectional study was to compare the A-B Neuropsychological Assessment Schedule (ABNAS), which measures cognitive side effects to the Adverse Events Profile (AEP), which looks at a broader range of side effects, and to investigate drug/dosage relationships with questionnaire scores to help determine a point at which a drug change would be indicated."( Adverse effects of anti-epileptics in trigeminal neuralgiform pain.
Cregg, R; Lee, G; O'Keeffe, AG; Reading, J; Tentolouris-Piperas, V; Zakrzewska, JM, 2018
)
0.48
" Toxic range on the ABNAS was estimated to occur when scores were >43/72 (95% CI: 37."( Adverse effects of anti-epileptics in trigeminal neuralgiform pain.
Cregg, R; Lee, G; O'Keeffe, AG; Reading, J; Tentolouris-Piperas, V; Zakrzewska, JM, 2018
)
0.48
"This study aims to describe the incidence of adverse drug reactions (ADRs) in children receiving antiepileptic drugs (AEDs) and compare ADRs to the individual drugs when given as monotherapy."( Safety of antiepileptic drugs in children and young people: A prospective cohort study.
Choonara, I; Egunsola, O; Sammons, HM; Whitehouse, WP, 2018
)
0.48
" Adverse reactions to antiepileptic drugs (AEDs) were elicited at the time of enrolment and after 3 months using the Paediatric Epilepsy Side Effects Questionnaire."( Safety of antiepileptic drugs in children and young people: A prospective cohort study.
Choonara, I; Egunsola, O; Sammons, HM; Whitehouse, WP, 2018
)
0.48
"Usually, no adverse effects are observed in breastfed infants whose mothers are treated with the anti-epileptic carbamazepine."( Maternal Carbamazepine Therapy and Unusual Adverse Effects in a Breastfed Infant.
Antonucci, R; Cherchi, C; Cuzzolin, L; Locci, C; Manconi, A; Oggiano, AM, 2018
)
1.11
"The use of carbamazepine is considered compatible with breastfeeding, even if the potential risk of adverse reactions in breastfed infants exists."( Maternal Carbamazepine Therapy and Unusual Adverse Effects in a Breastfed Infant.
Antonucci, R; Cherchi, C; Cuzzolin, L; Locci, C; Manconi, A; Oggiano, AM, 2018
)
1.29
" There were no notable differences in overall tolerability between subgroups, but the incidence of some adverse events (eg, dizziness, somnolence, nausea) differed between subgroups and/or between treatment periods."( Efficacy and safety of eslicarbazepine acetate monotherapy in patients converting from carbamazepine.
Blum, D; Cheng, H; Grinnell, T; Harvey, JH; Pazdera, L; Sam, MC; Sperling, MR; Strom, LA, 2018
)
0.7
"Despite morbidities and fatalities, nationwide epidemiologic data for severe cutaneous adverse reactions (SCARs), including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and drug reaction with eosinophilia and systemic symptoms (DRESS), are not widely available."( Analysis of Individual Case Safety Reports of Severe Cutaneous Adverse Reactions in Korea.
Kang, DY; Kang, HR; Kang, MG; Lee, JY; Park, HK; Sohn, KH; Yang, MS, 2019
)
0.51
"We analyzed individual case safety reports (ICSRs) of SCARs in the Korea Adverse Event Reporting System from 1988 to 2013."( Analysis of Individual Case Safety Reports of Severe Cutaneous Adverse Reactions in Korea.
Kang, DY; Kang, HR; Kang, MG; Lee, JY; Park, HK; Sohn, KH; Yang, MS, 2019
)
0.51
" The number of SCAR ICSRs has been increasing with increasing ICSRs for overall adverse drug events."( Analysis of Individual Case Safety Reports of Severe Cutaneous Adverse Reactions in Korea.
Kang, DY; Kang, HR; Kang, MG; Lee, JY; Park, HK; Sohn, KH; Yang, MS, 2019
)
0.51
" Even though ozonation has proven to be very efficient in reducing pharmaceutical parent compound concentrations in wastewater effluents, much remains unclear regarding potentially toxic ozonation by-product (OBP) formation."( Embryotoxicity of ozonated diclofenac, carbamazepine, and oxazepam in zebrafish (Danio rerio).
Ahrens, L; Carlsson, G; Golovko, O; Norrgren, L; Örn, S; Pohl, J; Weiss, J, 2019
)
0.78
" The co-exposure to TBY enhanced the adverse effects of CBZ on snails (reduced production of embryos)."( Laboratory-to-field extrapolation: Increase in carbamazepine toxicity in a higher tier, multiple-stress experiment.
Graumnitz, S; Heye, K; Jungmann, D; Oehlmann, J; Oetken, M; Rybicki, M; Schür, C; Völker, J; Wick, A, 2019
)
0.77
" Primary outcomes of the extension were treatment-emergent adverse events (TEAEs), serious TEAEs, and discontinuations due to TEAEs."( Long-term safety and efficacy of lacosamide and controlled-release carbamazepine monotherapy in patients with newly diagnosed epilepsy.
Ben-Menachem, E; Biton, V; Brock, M; De Backer, M; Gasalla, T; Grebe, HP; Jensen, L; Li, T; Steiniger-Brach, B; Terada, K, 2019
)
0.75
" Safety and tolerability were assessed throughout follow-up by evaluating adverse events (AEs) and ESL discontinuation due to AEs, respectively."( Safety, tolerability and effectiveness of transition to eslicarbazepine acetate from carbamazepine or oxcarbazepine in clinical practice.
Assenza, G; McMurray, R; Peltola, J; Rocamora, R; Villanueva, V, 2020
)
0.78
" In this work, we propose to infuse a competitor drug into the extracorporeal circuit that increases the free fraction of a toxic drug and thereby increases its dialytic removal."( A model-based analysis of phenytoin and carbamazepine toxicity treatment using binding-competition during hemodialysis.
Fuertinger, DH; Hoffman, RS; Kotanko, P; Maheshwari, V; Tao, X; Thijssen, S, 2020
)
0.83
"Phenobarbitone is at least as efficacious and safe as other drugs like phenytoin and levetiracetam."( Efficacy and Safety of Phenobarbitone as First-Line Treatment for Neonatal Seizure: A Systematic Review and Meta-Analysis.
Kumar, J; Meena, J; Saini, L; Yadav, J, 2021
)
0.62
"This study aimed to develop a pharmacokinetic (PK) model of oxcarbazepine (OXC) and analyse the relationship between monohydroxylated derivative (MHD), an active metabolite of OXC, and the adverse events of OXC."( Population pharmacokinetic model development and its relationship with adverse events of oxcarbazepine in adult patients with epilepsy.
Chu, K; Jang, IJ; Jang, Y; Kim, TJ; Lee, S; Lee, SK; Yoon, S; Yu, KS, 2021
)
0.62
"Stevens-Johnson syndrome and toxic epidermal necrolysis are viewed as the most severe drug-induced types of cutaneous adverse reactions, with high rates of morbidity and mortality."( Assessing carbamazepine and oxcarbazepine-associated Stevens-Johnson syndrome/toxic epidermal necrolysis: Data mining the public version of the FDA adverse event reporting system.
Fang, W; Pan, L; Sun, Q; Xu, C; Zhang, J; Zhang, Y, 2021
)
1.02
" Pharmacovigilance tools were employed for the quantitative detection of signals, where a signal represents a drug-associated adverse event, including the reporting odds ratio, proportional reporting ratio, an information component given by a Bayesian confidence propagation neural network, and the empirical Bayes geometric mean."( Assessing carbamazepine and oxcarbazepine-associated Stevens-Johnson syndrome/toxic epidermal necrolysis: Data mining the public version of the FDA adverse event reporting system.
Fang, W; Pan, L; Sun, Q; Xu, C; Zhang, J; Zhang, Y, 2021
)
1.02
"The total number of reports identified as Stevens-Johnson syndrome or toxic epidermal necrolysis associated with carbamazepine or oxcarbazepine included in this study was 1231."( Assessing carbamazepine and oxcarbazepine-associated Stevens-Johnson syndrome/toxic epidermal necrolysis: Data mining the public version of the FDA adverse event reporting system.
Fang, W; Pan, L; Sun, Q; Xu, C; Zhang, J; Zhang, Y, 2021
)
1.23
"The results of our study are consistent with clinical observations, suggesting the necessity for further clinical research on Stevens-Johnson syndrome and toxic epidermal necrolysis associated with carbamazepine or oxcarbazepine."( Assessing carbamazepine and oxcarbazepine-associated Stevens-Johnson syndrome/toxic epidermal necrolysis: Data mining the public version of the FDA adverse event reporting system.
Fang, W; Pan, L; Sun, Q; Xu, C; Zhang, J; Zhang, Y, 2021
)
1.21
" However, the formation of potentially toxic ozonation byproducts (OBPs) is a matter of concern."( Gene co-expression network analysis reveals mechanisms underlying ozone-induced carbamazepine toxicity in zebrafish (Danio rerio) embryos.
Ahi, EP; Carlsson, G; Golovko, O; Örn, S; Pohl, J; Schmitz, M, 2021
)
0.85
" Unfortunately, its pharmacokinetics and side effect profile may lead to significant toxicities due to its sodium channel blockade."( Neurologic toxicity of carbamazepine in treatment of trigeminal neuralgia.
Birdsong, S; Bridwell, RE; Brown, S; Clerkin, S; Long, B, 2022
)
1.03
" Outcomes included incident seizures, delirium tremens, AW severity scores, adverse events, dropouts, dropouts from adverse events, length of hospital stay, use of additional medications, total benzodiazepine requirements, and death."( Comparative efficacy and safety of pharmacotherapies for alcohol withdrawal: a systematic review and network meta-analysis.
Bach, P; Bahji, A; Crockford, D; Danilewitz, M; Devoe, DJ; El-Guebaly, N; Saitz, R, 2022
)
0.72
" Promazine and carbamazepine were the only agents significantly associated with greater dropouts because of adverse events."( Comparative efficacy and safety of pharmacotherapies for alcohol withdrawal: a systematic review and network meta-analysis.
Bach, P; Bahji, A; Crockford, D; Danilewitz, M; Devoe, DJ; El-Guebaly, N; Saitz, R, 2022
)
1.07
"Although some pharmacotherapeutic modalities, particularly benzodiazepines, appear to be safe and efficacious for reducing some measures of alcohol withdrawal, methodological issues and a high risk of bias prevent a consistent estimate of their comparative performance."( Comparative efficacy and safety of pharmacotherapies for alcohol withdrawal: a systematic review and network meta-analysis.
Bach, P; Bahji, A; Crockford, D; Danilewitz, M; Devoe, DJ; El-Guebaly, N; Saitz, R, 2022
)
0.72
"Acetic acid is an organic acid that can be used in the food industry, which normally has an insignificant rate of adverse reactions when used rationally."( Lethal toxicity induced by combined ingestion of dietary acetic acid and carbamazepine.
Chitescu, C; Dragostin, OM; Fulga, A; Fulga, I; Irimia, I; Pîrăianu, A; Stamate, E, 2023
)
1.14
"We review the main adverse drug reactions (ADRs) associated with CMZ, drug-drug interactions, and genetic predictors of the development of ADR."( Possible Clinical and Pharmacogenetic Predictors of the Efficacy and Safety of Carbamazepine in Post-COVID-19 Depression.
Cumming, P; Davydkin, I; Fedyashov, I; Gayduk, A; Nasyrova, R; Shnayder, N; Smirnova, D; Strelnik, A; Vaiman, E, 2022
)
0.95
"All nine drugs can relieve the pain of CPSP patients to different degrees; among them pregabalin and gabapentin have the most significant effect, and gabapentin and pregabalin also have the most adverse reactions."( Efficacy and safety of different antidepressants and anticonvulsants in central poststroke pain: A network meta-analysis and systematic review.
Chen, KY; Li, RY, 2022
)
0.72

Pharmacokinetics

The influence of progabide, a new antiepileptic drug, on the pharmacokinetic profiles of phenobarbital, phenytoin, carbamazepine, and valproic acid was evaluated.

ExcerptReferenceRelevance
" After single oral doses of carbamazepine, the absorption is fairly complete and the elimination half-life is about 35 hours (range 18 to 65 hours)."( Clinical pharmacokinetics of carbamazepine.
Bertilsson, L,
)
0.72
" Pharmacokinetic of carbamazepine were made in 7 new-borns and in 5 children."( 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
)
0.91
" The half-life of carbamazepine in the plasma was not significantly different from the half-life in the saliva."( The pharmacokinetics of carbamazepine in plasma and saliva of man.
Pynnönen, S, 1977
)
0.9
" Saliva level variation was too large for pharmacokinetic studies but acceptable for clinical purposes if sampling was long enough after the last dose."( Pharmacokinetic comparison of tablet and suspension dosage forms of carbamazepine.
Friel, P; Leal, K; Pearmain, J; Remick, R; Troupin, AS; Wada, JA, 1978
)
0.49
"Anticonvulsant therapy was among the first areas to benefit from clinical pharmacokinetic studies."( Clinical pharmacokinetics of anticonvulsants.
Dam, M; Hvidberg, EF, 1976
)
0.26
" In all cases, data on plasma levels were subjected to pharmacokinetic analyses."( Carbamazepine pharmacokinetics in young, adult and pregnant rats. Relation to pharmacological effects.
Assael, BM; Bossi, L; Garattini, S; Gerna, M; Gomeni, R; Morselli, PL, 1976
)
1.7
" Urinary excretion measurements confirmed the short elimination half-life and showed that less than 1% of the dose was excreted unchanged."( Pharmacokinetics of carbamazepine in monkeys following intravenous and oral administration.
Friel, P; Green, JR; Levy, RH; Lockard, JS; Martis, L, 1975
)
0.58
" 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
"Over the past 10 years, knowledge gained about the pharmacokinetic profiles of valproate and carbamazepine has increased the clinical effectiveness of their use."( Pharmacokinetics of valproate and carbamazepine.
Wilder, BJ, 1992
)
0.78
" A pharmacodynamic interaction may exist, inhibiting effective use of dihydropyridines as adjunctive therapy in epileptic patients."( Dihydropyridine calcium antagonists in mice: blood and brain pharmacokinetics and efficacy against pentylenetetrazol seizures.
Brodie, MJ; Drennan, JE; Forrest, G; Larkin, JG; Scobie, G; Thompson, GG,
)
0.13
"The paper is concerned with the data of economic evaluation of pharmacokinetic prediction of the individual efficacy of preventive carbamazepin therapy of patients suffering from affective and schizoaffective psychoses."( [An economic evaluation in the pharmacokinetic prediction of preventive carbamazepine therapy].
Kostiukova, EG; Kudriakova, TB; Ushakov, IuV, 1991
)
0.51
" A pharmacokinetic profile after a single oral 400-mg dose of ADD 94057 was used to calculate ADD 94057 dosages."( 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
"Since calcium channel antagonists are a diverse class of drugs frequently administered in combination with other agents, the potential for clinically significant pharmacokinetic drug interactions exists."( Pharmacokinetic interactions with calcium channel antagonists (Part II).
Bottorff, MB; Myre, SA; Schlanz, KD, 1991
)
0.28
"The objective of this study was to describe the postinduction clearance of carbamazepine (CBZ) in adult psychiatric patients by population pharmacokinetic analysis using the NONMEM program."( Postinduction carbamazepine clearance in an adult psychiatric population.
Crismon, ML; Godley, PJ; Martin, ES, 1991
)
0.87
" The two formulations, therefore, have a similar pharmacokinetic profile and could be used interchangeably in the management of patients with epilepsy."( A comparative pharmacokinetic study of conventional and chewable carbamazepine in epileptic patients.
Patsalos, PN, 1990
)
0.52
" Noncompartmental methods were used to estimate pharmacokinetic data."( 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
" The pharmacokinetic study was repeated under steady-state conditions after 3 months of drug intake in 6 of these subjects."( First dose and steady-state pharmacokinetics of oxcarbazepine and its 10-hydroxy metabolite.
Dickinson, RG; Dunstan, PR; Eadie, MJ; Hooper, WD, 1989
)
0.28
" The half-life and apparent clearance were the same for each day, indicating that hemodialysis/hemoperfusion had little effect on the overall removal of carbamazepine from the body."( Carbamazepine clearance in hemodialysis and hemoperfusion.
Gal, P; Kandrotas, RJ; Love, JM; Oles, KS, 1989
)
1.92
"6 microgram/ml; LTG has a favorable pharmacokinetic profile and appears to exhibit first-order linear kinetics during long-term chronic dosing; LTG shows preliminary evidence of efficacy during long-term administration; and to date, our patients represent the longest reported experience of continuous and closely monitored LTG therapy in the literature."( Long-term tolerability, pharmacokinetic and preliminary efficacy study of lamotrigine in patients with resistant partial seizures.
Ashworth, M; Keally, M; Kupferberg, H; Mikati, MA; Osborne-Shafer, P; Schachter, SC; Schomer, DL; Seaman, CA; Sheridan, PH; Valakas, A, 1989
)
0.28
"Drugs labeled with stable isotopes have been successfully used in pharmacokinetic drug interaction studies."( Pharmacokinetic drug interactions.
Eichelbaum, M,
)
0.13
"The influence of progabide, a new antiepileptic drug, on the pharmacokinetic profiles of phenobarbital, phenytoin, carbamazepine, and valproic acid was evaluated in four separate studies, each including six young healthy volunteers."( Pharmacokinetic interactions of progabide with other antiepileptic drugs.
Bianchetti, G; Morselli, PL; Padovani, P; Thénot, JP; Thiercelin, JF,
)
0.34
" Standard pharmacological equations can be used to provide this information from pharmacokinetic data which are readily available in most hospital settings."( Application of pharmacokinetics in the diagnosis of chemical abuse in Münchausen syndrome by proxy.
Kearns, GL; Mahesh, VK; Stern, HP; Stroh, SE, 1988
)
0.27
"Major pharmacokinetic parameters of the Soviet anticonvulsive drug benzobarbital used with different regimens of administration (single and prolonged) are described."( [Pharmacokinetic aspects of anticonvulsant therapy with benzonal].
Antadze, ZI; Chanvetadze, BG; Chkhenkeli, SI; Okudzhava, VM; Rukhadze, MD, 1988
)
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
" The pharmacokinetic parameters have been found to be important for specifying the causes of dissociation between the level of blood anticonvulsant and the therapeutic effect when the attacks cannot be controlled or there were signs of intoxication."( [Role of the pharmacokinetic parameters of carbamazepine in optimizing epilepsy treatment].
Antadze, ZI; Chankvetadze, BG; Okudzhava, VM; Vetrogon, FG, 1987
)
0.54
" Therefore, the present study was undertaken in order to develop a pharmacokinetic model to predict the behavior of EPO in the body after administration of CBZ."( Pharmacokinetic study of carbamazepine and its epoxide metabolite in humans.
Kaneniwa, N; Sumi, M; Umezawa, O; Watari, N, 1987
)
0.58
"The determination of possible modifications of pharmacokinetic parameters of carbamazepine by josamycin in an experimental study after chronic administration of the drugs in the rat was undertaken to assay, or not, the enzymatic inhibition hypothesis which is supported in human clinical studies."( [Pharmacokinetic, biochemical and histological study of the carbamazepine-josamycin interaction in the rat following chronic administration].
Bouyard, P; Bussière, H; Jadot, G; Payan, MJ; Tamalet, C; Valli, M, 1986
)
0.74
" The half-life of this CBZ-D4 dose in the two patients (20 and 26 hr, respectively) was similar to the post-steady-state half-life of CBZ (23 hr in both patients) measured later."( Pharmacokinetics: time-dependent changes--autoinduction of carbamazepine epoxidation.
Bertilsson, L; Tomson, T; Tybring, G,
)
0.37
"In our recent study, oral cimetidine increased carbamazepine plasma levels after a single oral dose by 26 percent and prolonged the elimination half-life by 18 percent."( Ranitidine does not alter single-dose carbamazepine pharmacokinetics in healthy adults.
Dalton, MJ; Messenheimer, JA; Powell, JR, 1985
)
0.8
" Pharmacokinetic interactions between antiepileptic drugs may lead to considerable fluctuation in plasma drug concentration, and monotherapy is often preferable."( Pharmacokinetics of antiepileptic drugs.
Neuvonen, PJ; Tokola, RA, 1983
)
0.27
" Some other pharmacokinetic aspects which could be useful in extrapolating to the amount and time of ingestion of the overdose are discussed."( Pharmacokinetic aspects of carbamazepine and its two major metabolites in plasma during overdosage.
Aucamp, AK; Hundt, HK; Müller, FO, 1983
)
0.56
" The time-concentration curves showed a median Tmax of 8 h followed by a plateau until 24 h indicating saturable kinetic processes."( Pharmacokinetics of 10-OH-carbazepine, the main metabolite of the antiepileptic oxcarbazepine, from serum and saliva concentrations.
Jönsson, B; Klitgaard, NA; Kristensen, O; Sindrup, S, 1983
)
0.27
" This review contains relevant pharmacokinetic data on anticonvulsant drugs widely used during pregnancy and the neonatal period."( Anticonvulsants during pregnancy and lactation. Transplacental, maternal and neonatal pharmacokinetics.
Egger, HJ; Helge, H; Kuhnz, W; Nau, H; Rating, D,
)
0.13
"), as evidenced by a shift of tmax from 2 h in controls to 6 h in (+)-catechin-treated animals."( [Effect of (+)-catechin on the pharmacokinetics of carbamazepine in rabbits].
Pentz, R; Siegers, CP; Younes, M, 1982
)
0.52
" 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
"Therapeutic drug monitoring (TDM) of chronic treatments is justified for several reasons, including relative over- or underdosage due to variable individual elimination, pharmacokinetic interactions in drug combinations, and noncompliance."( Validation of a quick modeling program generating clearance estimates at steady state for routine therapeutic drug monitoring.
Alric, R; Beglia, S; el Battah, A, 1995
)
0.29
" On the basis of pharmacokinetic parameters, mean optimal dosages sufficient for maintenance of effective and safe carbamazepine concentrations were calculated."( [Therapeutic drug monitoring and the pharmacokinetics of carbamazepine in children with a convulsive syndrome].
Dubrovina, LIu; Ivanova, ES; Kholodov, LE; Kopanev, IuA; Postnikov, SS; Prityko, AG; Sokolov, AV; Tatarinov, PA; Tishchenkova, IF; Veselov, NK, 1995
)
0.75
" Pharmacokinetic parameters of monohydroxyoxcarbazepine and dihydroxyoxcarbazepine were determined from plasma and urine samples obtained on the tenth day of each treatment period."( Effects of felbamate on the pharmacokinetics of the monohydroxy and dihydroxy metabolites of oxcarbazepine.
Banfield, CR; Colucci, RD; Hulsman, JA; Lin, CC; Meehan, JW; Mojaverian, P; Nezamis, J; Radwanski, E; Reidenberg, P; Rentmeester, TW, 1995
)
0.29
" Pharmacokinetic studies indicated that glycofurol inhibited CBZ metabolism by decreasing formation of the major CBZ metabolite CBZ-10,11-epoxide (CBZ-E)."( New injectable aqueous carbamazepine solution through complexing with 2-hydroxypropyl-beta-cyclodextrin: tolerability and pharmacokinetics after intravenous injection in comparison to a glycofurol-based formulation.
Brewster, ME; Düsing, R; Hönack, D; Löscher, W; Richter, A; Schulz, HU; Schürer, M, 1995
)
0.6
" Neither the serum concentrations nor the pharmacokinetic parameters of sodium valproate (SV) were altered by the coadministration of aminophylline (AMP)."( 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
" When issuing a license to any drug, FDA stipulates at most a difference of 20% from the reference drug only in peak concentration and AUC (area under the curve)."( Pharmacokinetics of carbamazepine. Part I: A new bioequivalency parameter based on a relative bioavailability trial.
Ertaş, M; Kayali, A; Tuğlular, I,
)
0.45
" The pharmacokinetic part of the study comprised 22 children, and an additional nine children were included in the clinical part of the study."( Replacing carbamazepine slow-release tablets with carbamazepine suppositories: a pharmacokinetic and clinical study in children with epilepsy.
Arvidsson, J; Flesch, G; Nilsson, HL; Sandstedt, P; Steinwall, G; Tonnby, B, 1995
)
0.69
" The apparent elimination half-life of the monohydroxy-metabolite [19 (SD 3) h] in these patients was about twice that in healthy subjects."( 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
" A review of published studies involving small numbers of elderly subjects or patients given phenytoin sodium, valproic acid, or carbamazepine demonstrates decreased protein binding and intrinsic clearance and increased half-life with advancing age."( Antiepileptics in the elderly. Pharmacoepidemiology and pharmacokinetics.
Cloyd, JC; Lackner, TE; Leppik, IE, 1994
)
0.49
" 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
"Population-based pharmacokinetic prediction algorithms have been developed for several medications."( A pharmacodynamic approach to the estimate of carbamazepine autoinduction.
Cramer, JA; Mattson, RH; Scheyer, RD, 1994
)
0.55
" Differential effects on the pharmacodynamic parameters were seen."( Characterization of the pharmacodynamics of several antiepileptic drugs in a direct cortical stimulation model of anticonvulsant effect in the rat.
Danhof, M; Hoogerkamp, A; Vis, PW; Voskuyl, RA, 1994
)
0.29
" The 266 serum concentration data at steady-state after repetitive oral administration were analyzed using the nonlinear mixed effects model (NONMEM) program designed for estimation of population pharmacokinetic parameters."( 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
" These results suggest that ZNS has little effect on the pharmacokinetic behaviors of other antiepileptic drugs."( 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
" Steady-state pharmacokinetic parameters of FEL and its pyridine metabolite were not influenced by the single dose of OXC."( 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
"The purpose of the present study was to compare the pharmacokinetic parameters of two carbamazepine (CBZ) tablet formulations (conventional (CBZ-CO) and controlled-release (CBZ-CR)) in patients with epilepsy receiving the drug as monotherapy or polytherapy."( 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
)
0.74
" Three of the new drugs, gabapentin, topiramate and vigabatrin, are more promising on the basis of their pharmacokinetic features."( Comparative pharmacokinetics of the newer antiepileptic drugs.
Bialer, M, 1993
)
0.29
"To compare carbamazepine pharmacokinetic parameters between obese and lean subjects following the administration of a single 200-mg tablet."( Carbamazepine pharmacokinetics in obese and lean subjects.
Berry, EM; Caraco, Y; Levy, M; Zylber-Katz, E, 1995
)
2.12
"Carbamazepine elimination half-life (t1/2), apparent volume of distribution (Varea/F), and its oral clearance (Clpo/F) were derived from the drug concentration-time curves."( Carbamazepine pharmacokinetics in obese and lean subjects.
Berry, EM; Caraco, Y; Levy, M; Zylber-Katz, E, 1995
)
3.18
" The terminal elimination half-life (t1/2z) is relatively long in neonates; it then decreases during the first postnatal month to lower values than in adults, and then progressively increases with age due to an age-dependent decrease in the metabolic rate."( Clinical pharmacokinetics of antiepileptic drugs in paediatric patients. Part II. Phenytoin, carbamazepine, sulthiame, lamotrigine, vigabatrin, oxcarbazepine and felbamate.
Avanzini, G; Battino, D; Estienne, M, 1995
)
0.51
" The current study investigates the pharmacokinetic or pharmacodynamic mechanisms responsible for this observation."( Pharmacokinetic origin of carbamazepine-induced resistance to vecuronium neuromuscular blockade in anesthetized patients.
Alloul, K; Ebrahim, Z; Shutway, F; Varin, F; Whalley, DG, 1996
)
0.59
" Plasma vecuronium concentrations were fitted to a two-compartment pharmacokinetic model, and the effect compartment equilibration rate constant was derived with a nonparametric link model."( Pharmacokinetic origin of carbamazepine-induced resistance to vecuronium neuromuscular blockade in anesthetized patients.
Alloul, K; Ebrahim, Z; Shutway, F; Varin, F; Whalley, DG, 1996
)
0.59
"The twofold increase in clearance provides evidence of a pharmacokinetic origin to the carbamazepine-vecuronium interaction; however, the possibility of a concurrent pharmacodynamic alteration cannot be assessed."( Pharmacokinetic origin of carbamazepine-induced resistance to vecuronium neuromuscular blockade in anesthetized patients.
Alloul, K; Ebrahim, Z; Shutway, F; Varin, F; Whalley, DG, 1996
)
0.82
" Samples for pharmacokinetic analyses were obtained on Days 15 and 32; trough plasma concentrations of carbamazepine and its principal metabolite, carbamazepine-10, 11-epoxide (CBZ-E), were determined daily beginning on Day 13."( 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
)
0.73
"There were no significant differences between the sertraline and placebo groups in any of the pharmacokinetic parameters for carbamazepine or CBZ-E."( 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
)
0.72
"Antiepileptic drugs (AEDs) in broad use today have a number of pharmacokinetic liabilities, including a propensity for clinically meaningful drug interactions."( Pharmacokinetic profile of topiramate in comparison with other new antiepileptic drugs.
Perucca, E, 1996
)
0.29
" The median elimination half-life (t1/2) in patients receiving concomitant valproate (VPA) was 43."( Pharmacokinetic interactions between lamotrigine and other antiepileptic drugs in children with intractable epilepsy.
Boreus, L; Eriksson, AS; Hoppu, K; Nergårdh, A, 1996
)
0.29
"We studied the steady-state pharmacokinetic profile of topiramate (TPM) as a function of dose and the effects of comedication with carbamazepine (CBZ)."( Steady-state pharmacokinetics of topiramate and carbamazepine in patients with epilepsy during monotherapy and concomitant therapy.
Doose, DR; Kramer, LD; Nayak, RK; Sachdeo, RC; Sachdeo, SK; Walker, SA, 1996
)
0.75
" Adjusting the CBZ dose for pharmacokinetic reasons when TPM is administered as adjunctive treatment does not appear to be necessary."( Steady-state pharmacokinetics of topiramate and carbamazepine in patients with epilepsy during monotherapy and concomitant therapy.
Doose, DR; Kramer, LD; Nayak, RK; Sachdeo, RC; Sachdeo, SK; Walker, SA, 1996
)
0.55
" 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
" Estimation of the pharmacokinetic parameters in each drug was performed by Higuchi's Bayesian program, PEDA Pearson's correlation coefficient (r) between clearance and body weight was calculated for each drug."( 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
" Routine clinical pharmacokinetic data (N = 1,010) collected from 466 patients receiving carbamazepine were analyzed according to a simple steady-state pharmacokinetic model with the use of NONMEM, a computer program designed for population pharmacokinetic analysis that allows pooling of data."( Detection of carbamazepine drug interaction by multiple peak approach screening using routine clinical pharmacokinetic data.
Aoyama, T; Yukawa, E, 1996
)
0.88
" This study compares the pharmacokinetics of CBZ-CO against CBZ-CR in patients with epilepsies chronically treated with CBZ in monotherapy or CBZ-PB in bitherapy, the effect of PB on CBZ-CO and CBZ-CR pharmacokinetic parameters, and the effect of the two formulations of CBZ on PB pharmacokinetic parameters."( 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
"This article surveys the pharmacokinetic parameters for the new antiepileptic drugs (AEDs): felbamate, gabapentin, lamotrigine, oxcarbazepine, tiagabine, topiramate, and vigabatrin."( Pharmacokinetics of new antiepileptic drugs.
Gram, L, 1996
)
0.29
" The terminal phase half-life was 22."( Pharmacokinetics of carbamazepine derived from a new tablet formulation.
Jakovljevic, V; Mikov, M; Popović, J,
)
0.45
" The equations describing the models for AUC using two time points (3 and 24h) and Cmax for the training data set of 30 subjects were AUCpredicted = 11."( A limited sampling method for the estimation of flunarizine area under the curve (AUC) and maximum plasma concentration (Cmax).
Mahmood, I; Sahlroot, JT, 1997
)
0.3
" No clinically relevant pharmacokinetic interactions were noted between felbamate and lamotrigine, clonazepam, vigabatrin, nor the active monohydroxy metabolite of oxcarbazepine."( Pharmacokinetic interactions with felbamate. In vitro-in vivo correlation.
Banfield, CR; Glue, P; Levy, RH; Mather, GG; Perhach, JL; Racha, JK, 1997
)
0.3
" Routine clinical pharmacokinetic data (n = 479) were collected from 207 epilepsy patients on combination therapy."( Detection of carbamazepine-induced changes in valproic acid relative clearance in man by simple pharmacokinetic screening.
Aoyama, T; Higuchi, S; Honda, T; Ohdo, S; Yukawa, E, 1997
)
0.67
" Following multiple dosing, the LSM was developed from a training data set of 10 subjects using the steady state Cmin (plasma concentration obtained 5 min before the last CBZ-SR dose)."( A limited sampling method for the estimation of AUC and Cmax of carbamazepine and carbamazepine epoxide following a single and multiple dose of a sustained-release product.
Chamberlin, N; Mahmood, I, 1998
)
0.54
"The model provided good estimates of AUC and Cmax for CBZ and CBZE."( A limited sampling method for the estimation of AUC and Cmax of carbamazepine and carbamazepine epoxide following a single and multiple dose of a sustained-release product.
Chamberlin, N; Mahmood, I, 1998
)
0.54
"The method described here may be used to estimate AUC and Cmax for CBZ and CBZE without detailed pharmacokinetic studies following single or multiple dose of CBZ."( A limited sampling method for the estimation of AUC and Cmax of carbamazepine and carbamazepine epoxide following a single and multiple dose of a sustained-release product.
Chamberlin, N; Mahmood, I, 1998
)
0.54
"54 ml/min/kg) and shortened the elimination half-life (17."( Effect of carbamazepine on the single oral dose pharmacokinetics of alprazolam.
Furukori, H; Kaneko, S; Kondo, T; Nagasaki, T; Ohkubo, T; Otani, K; Shimoyama, R; Sugawara, K; Yasui, N, 1998
)
0.7
"The present study evaluates effect of pharmacokinetic interaction between caffeine (300 mg) in three divided doses with sodium valproate (400 mg) and carbamazepine (200 mg) given as single doses, in normal human volunteers, using a open cross over design."( Influence of caffeine on pharmacokinetic profile of sodium valproate and carbamazepine in normal human volunteers.
David, J; Joseph, T; Kulkarni, C; Vaz, J, 1998
)
0.73
"To conduct a population pharmacokinetic analysis of carbamazepine (CBZ)."( Population pharmacokinetics of carbamazepine in adults with epilepsy.
Ahman, P; Brundage, RC; Cascino, G; Graves, NM; Krause, S; Leppik, IE; Rarick, J; So, E; Wen, Y,
)
0.67
"To determine whether the toxicity that occurs in some patients when lamotrigine (LTG) is added to carbamazepine (CBZ) is the result of either a pharmacokinetic or a pharmacodynamic interaction."( Carbamazepine toxicity with lamotrigine: pharmacokinetic or pharmacodynamic interaction?
Berry, DJ; Besag, FM; Newbery, JE; Pool, F; Subel, B, 1998
)
1.96
" This appears to be the result of a pharmacodynamic interaction."( Carbamazepine toxicity with lamotrigine: pharmacokinetic or pharmacodynamic interaction?
Berry, DJ; Besag, FM; Newbery, JE; Pool, F; Subel, B, 1998
)
1.74
" Pharmacokinetic data and occurrence of AE were compared between the two groups at the time of the single-dose kinetic study, at the completion of the switchover to CBZ, and 4 weeks after discontinuation of the previous AED."( Rapid switchover to carbamazepine using pharmacokinetic parameters.
Bourgeois, BF; Hasegawa, H; Hutson, P; Kanner, AM, 1998
)
0.62
"25 for each of the pharmacokinetic parameters for CBZ and for the summation of CBZ and CBZ-epoxide (CBZ-E)."( 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
)
0.54
"Our results demonstrate that extended-release CBZ twice daily was bioequivalent to immediate-release CBZ four times daily, with regard to CBZ levels and summation of CBZ and CBZ-E levels, based on the pharmacokinetic parameters evaluated."( 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
)
0.54
" A linear pharmacokinetic model which describes clearances of parent and metabolite is developed."( A partial area difference analysis for estimating elimination rate constants and distribution volumes of metabolites.
Riad, LE; Sawchuk, RJ, 1998
)
0.3
"hr/L, and terminal elimination half-life from 14."( Feasibility and pharmacokinetics of carbamazepine oral loading doses.
Cohen, H; Devinsky, O; Goldfrank, LR; Hoffman, RS; Howland, MA; Kutt, H; Leung, LK; Luciano, DJ; Rubin, RN, 1998
)
0.58
"In this study our aim was to assess pharmacokinetic effects and adverse cognitive effects of switches between generic and branded formulations of carbamazepine (CBZ)."( Pharmacokinetics and cognitive effects of carbamazepine formulations with different dissolution rates.
Aldenkamp, AP; Diepman, L; Doelman, J; Franken, M; Hulsman, J; Majoie, M; Olling, M; Rentmeester, T; Schellekens, A, 1998
)
0.76
"Area under the curve and a number of pharmacokinetic properties (serum concentration day curves, change in serum concentration (delta scores), peak/trough concentrations and peak time) did not differ among the three CBZ formulations."( Pharmacokinetics and cognitive effects of carbamazepine formulations with different dissolution rates.
Aldenkamp, AP; Diepman, L; Doelman, J; Franken, M; Hulsman, J; Majoie, M; Olling, M; Rentmeester, T; Schellekens, A, 1998
)
0.56
" The purpose of the present study was to assess the potential for a pharmacokinetic interaction between olanzapine and carbamazepine, since these agents are likely to be used concomitantly in the treatment of manic psychotic disorder."( A pharmacokinetic interaction between carbamazepine and olanzapine: observations on possible mechanism.
Bergstrom, RF; Gilfillan, DJ; Lucas, RA, 1998
)
0.78
" Olanzapine pharmacokinetic values for Cmax and AUC were significantly lower after the second dose, the elimination half-life was significantly shorter, and the clearance and volume of distribution were significantly increased."( A pharmacokinetic interaction between carbamazepine and olanzapine: observations on possible mechanism.
Bergstrom, RF; Gilfillan, DJ; Lucas, RA, 1998
)
0.57
" No significant changes were observed in the mean values of OXC pharmacokinetic parameters (Cmax, Tmax, t1/2 and AUC0-infinity) between the control and the pre-treated groups."( Effect of valproic acid on the pharmacokinetic profile of oxcarbazepine in the rat.
al-Hassan, MI; Bawazir, SA; Matar, KM; Nicholls, PJ; Tekle, A, 1999
)
0.3
" The pharmacokinetic assessment was repeated on day 18."( 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
)
0.54
" For CBTL and TXR, the key CBZ pharmacokinetic measures of area under the curve of concentration versus time (AUC(0-tau)), maximum concentration (Cmax), and minimum concentration (Cmin) were bioequivalent."( 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
" In this study, we retrospectively evaluated the predictive performance in an adult outpatient population of six different methods, representing six sets of CBZ pharmacokinetic parameters selected according to the literature using a Bayesian computer program (PKS System; Abbott Laboratories, Abbott Park, IL, USA)."( Predictive capacity of carbamazepine pharmacokinetic parameters in a Portuguese outpatient population.
Caramona, MM; de Almeida, AM; Falcão, AC; Leitão, F; Sales, F; Santos, J, 1999
)
0.61
" The present study was designed to ascribe dose-response differences among the three rat strains to pharmacokinetic or pharmacodynamic factors."( 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
" The simultaneous administration of TJ-19 significantly lengthened the time to reach the peak plasma concentration (Tmax), but did not influence the peak plasma concentration, area under the plasma concentration-time curve or terminal elimination half-life (t1/2)."( Studies on interactions between traditional herbal and Western medicines. I. Effects of Sho-seiryu-to on the pharmacokinetics of carbamazepine in rats.
Kuroda, K; Nagasawa, K; Nakasako, S; Ohnishi, N; Yokoyama, T; Yonekawa, Y; Yoshioka, M, 1999
)
0.51
" 'Level C' IVIVC according to the USP were optimised by plotting percentages dissolved on selected time points (D values) or their reciprocals (1/D values), against several pharmacokinetic parameters primarily related to the absorption phase and against AUC(0-infinity)."( 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
" Because 10-hydroxycarbazepine is a chiral molecule, the objective of the study was to perform a stereoselective pharmacokinetic analysis of 10-hydroxycarbazepine in humans."( Enantioselective pharmacokinetics of 10-hydroxycarbazepine after oral administration of oxcarbazepine to healthy Chinese subjects.
Bialer, M; Perucca, E; Sintov, A; Volosov, A; Xiaodong, S; Yagen, B, 1999
)
0.3
"004), the elimination half-life was 35% shorter (12."( Cytochrome P450-inducing antiepileptics increase the clearance of vincristine in patients with brain tumors.
Joensuu, H; Kivistö, KT; Mäenpää, H; Neuvonen, PJ; Villikka, K, 1999
)
0.3
" Pharmacokinetic data were obtained on days 3 and 28."( The effect of carbamazepine on the steady-state pharmacokinetics of ziprasidone in healthy volunteers.
Anziano, RJ; Hansen, RA; Laurent, A; Miceli, JJ; Robarge, L, 2000
)
0.67
" Carbamazepine administration to group 1 was associated with modest reductions in ziprasidone exposure, with mean decreases in ziprasidone AUC(0,12 h) and Cmax values of 36% and 27%, respectively, on day 28 compared with day 3 (P<0."( The effect of carbamazepine on the steady-state pharmacokinetics of ziprasidone in healthy volunteers.
Anziano, RJ; Hansen, RA; Laurent, A; Miceli, JJ; Robarge, L, 2000
)
1.58
" Steady state Cmax and AUC0-24 of carbamazepine were also reduced significantly in comparison to those of control rabbits after 7 days co-administration of Septilin."( Effect of Septilin--a herbal preparation on pharmacokinetics of carbamazepine in rabbits.
Garg, SK; Islam, AS; Kumar, N, 1998
)
0.82
" Pharmacokinetic interactions between antiepileptic drugs represent a major complication of epilepsy treatment with polytherapy."( Investigation of phenobarbital-carbamazepine-valproic acid interactions using population pharmacokinetic analysis for optimisation of antiepileptic drug therapy: an overview.
Yukawa, E, 2000
)
0.59
" The difference in the pharmacokinetic parameters found after administration of individual MHD enantiomers compared with the administration of MHD in a racemic form suggests the possibility of interaction between the two enantiomers."( Comparative stereoselective pharmacokinetic analysis of 10-hydroxycarbazepine after oral administration of its individual enantiomers and the racemic mixture to dogs.
Bialer, M; Volosov, A; Yagen, B, 2000
)
0.31
" The mean (+/- SEM) elimination half-life of CBZ was 33."( Effects of short-term lamotrigine treatment on pharmacokinetics of carbamazepine.
Keränen, T; Kerttula, T; Malminiemi, K; Moilanen, E; Ylitalo, P, 2000
)
0.54
" We compared carbamazepine and carbamazepine-10,11-epoxide noncompartmental pharmacokinetic parameter values before and after St John's Wort with a paired Student t test."( Lack of effect of St John's Wort on carbamazepine pharmacokinetics in healthy volunteers.
Alfaro, RM; Burstein, AH; Dunn, T; Horton, RL; Piscitelli, SC; Theodore, W, 2000
)
0.95
"We found no significant differences before or after the administration of St John's Wort in carbamazepine peak concentration (7."( Lack of effect of St John's Wort on carbamazepine pharmacokinetics in healthy volunteers.
Alfaro, RM; Burstein, AH; Dunn, T; Horton, RL; Piscitelli, SC; Theodore, W, 2000
)
0.8
" Based on two case reports in which increased carbamazepine (CBZ) plasma concentrations were observed in patients receiving clarithromycin, a crossover multiple dose study was designed to find out the pharmacokinetic interaction between CBZ and clarithromycin in rhesus monkeys."( Effect of clarithromycin on the pharmacokinetics of carbamazepine in rhesus monkeys.
Badyal, DK; Garg, SK, 2000
)
0.82
" While the therapeutic plasma concentration range of CBZ is only vaguely defined, pharmacokinetic differences in the disposition of CBZ among subjects could be responsible for the inadequate control of seizures in some."( Association of drug levels & pharmacokinetics of carbamazepine with seizure control.
Puri, V; Tripathi, KD; Vasudev, A, 2000
)
0.56
" Serum CBZ levels were measured by HPLC and the pharmacokinetic parameters were calculated."( Association of drug levels & pharmacokinetics of carbamazepine with seizure control.
Puri, V; Tripathi, KD; Vasudev, A, 2000
)
0.56
" Thus, non-attainment or non-maintenance of therapeutic CBZ level or other pharmacokinetic difference was not responsible for occurrence of seizures in the uncontrolled patients."( Association of drug levels & pharmacokinetics of carbamazepine with seizure control.
Puri, V; Tripathi, KD; Vasudev, A, 2000
)
0.56
"It appears that pharmacodynamic resistance of the seizure to CBZ rather than pharmacokinetic factors is responsible for lack of efficacy of CBZ in nonresponding epileptic patients."( Association of drug levels & pharmacokinetics of carbamazepine with seizure control.
Puri, V; Tripathi, KD; Vasudev, A, 2000
)
0.56
"Study was conducted to compare the pharmacokinetic profile of conventional and slow-release carbamazepine formulations in Indian epileptic patients."( A comparative evaluation of pharmacokinetics of conventional and slow-release carbamazepine formulation in newly treated patients of epilepsy: a random evaluation.
Agarwal, A; Garg, RK; Nag, D, 1998
)
0.75
" To avoid complex pharmacokinetic interactions among multiple antiepileptic drugs, the data on serum concentrations in the current study were collected from patients who were co-administered only one additional antiepileptic drug (phenobarbital-carbamazepine, phenobarbital-valproic acid, or carbamazepine-valproic acid) or who received monotherapy."( Pharmacokinetic interactions among phenobarbital, carbamazepine, and valproic acid in pediatric Japanese patients: clinical considerations on steady-state serum concentration-dose ratios.
Aoyama, T; Higuchi, S; Hokazono, T; Ohdo, S; Satou, M; Yukawa, E, 2000
)
0.74
" The pharmacokinetic parameters of CBZ were calculated using the model-independent method."( 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
"In the present study, Mentat, a herbomineral psychotropic preparation, was studied for its pharmacokinetic interaction with the commonly used anti-epileptic drugs, carbamazepine and phenytoin."( Pharmacokinetic interactions of Mentat with carbamazepine and phenytoin.
Gopumadhavan, S; Mitra, SK; Rafiq, M; Sundaram, R; Tripathi, M; Venkataranganna, MV,
)
0.59
" We used a linear one-compartmental model with oral absorption and found the pharmacokinetic parameter values of CBZ behaviour to be in good agreement with those reported earlier."( Population pharmacokinetic modelling of carbamazepine by using the iterative Bayesian (IT2B) and the nonparametric EM (NPEM) algorithms: implications for dosage.
Bondareva, IB; Jelliffe, RW; Sokolov, AV; Tischenkova, IF, 2001
)
0.58
" Because of the diversity within the population, use of the mean population model without knowledge of an individual patient's pharmacokinetic characteristics gives poor prediction."( Population pharmacokinetic modelling of carbamazepine by using the iterative Bayesian (IT2B) and the nonparametric EM (NPEM) algorithms: implications for dosage.
Bondareva, IB; Jelliffe, RW; Sokolov, AV; Tischenkova, IF, 2001
)
0.58
" The half-life of MHD was 10."( [Pharmacokinetic variability of oxcarbazepine in epileptic patients].
Bercellini, MA; Rubio, MC; Saidón, P; Viola, MS, 2000
)
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
"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
"The possibility of pharmacokinetic interactions between Saiko-ka-ryukotsu-borei-to extract powder (TJ-12), a widely used traditional Chinese herbal (Kampo) medicine, and carbamazepine (CBZ), an important anti-epileptic drug, was examined in rats."( Studies on interactions between traditional herbal and Western medicines. IV: lack of pharmacokinetic interactions between Saiko-ka-ryukotsu-borei-to and carbamazepine in rats.
Kuroda, K; Nagasawa, K; Nakasako, S; Ohnishi, N; Okada, K; Takara, K; Umehara, S; Yokoyama, T; Yoshioka, M,
)
0.52
" Pharmacokinetic variables were derived from plasma samples collected before and after administration of vecuronium."( Pharmacokinetics and pharmacodynamics of vecuronium in children receiving phenytoin or carbamazepine for chronic anticonvulsant therapy.
Greenblatt, DJ; Martyn, JA; Soriano, SG; Sullivan, LJ; Venkatakrishnan, K, 2001
)
0.53
" Concurrent administration of LTG with CBZ did not have any significant effect on the pharmacokinetic parameters of CBZ."( Effect of lamotrigine on the pharmacokinetics of carbamazepine and its active metabolite in dogs.
Al-Hassan, MI; Al-Khamis, KI; Bawazir, SA; Matar, KM; Nicholls, PJ,
)
0.39
"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-date levetiracetam is not known to be associated with any clinically significant pharmacokinetic interaction."( Carbamazepine toxicity during combination therapy with levetiracetam: a pharmacodynamic interaction.
Patsalos, PN; Sander, JW; Sisodiya, SM, 2002
)
1.76
" The AUC0-infinity and Cmax of carbamazepine were significantly enhanced after Coca-Cola while tmax was achieved earlier with Coca-Cola."( Effect of an acidic beverage (Coca-Cola) on the pharmacokinetics of carbamazepine in healthy volunteers.
Dixit, RK; Garg, SK; Malhotra, S,
)
0.65
" The significant decrease in Tmax indicated that simultaneous oral administration of PR contributed to more rapid absorption of CBZ."( Pharmacokinetic interactions between carbamazepine and the traditional Chinese medicine Paeoniae Radix.
Chen, LC; Chen, YF; Chou, MH; Lin, MF; Yang, LL; Yen, KY, 2002
)
0.59
" The pharmacokinetic parameters were analyzed by analysis of variance followed by the Tukey-Kramer test."( Pharmacokinetic interaction between albendazole sulfoxide enantiomers and antiepileptic drugs in patients with neurocysticercosis.
Dreossi, SA; Garcia, FS; Lanchote, VL; Takayanagui, OM, 2002
)
0.31
" The fitted pharmacokinetic parameters of CBZ and CBZ-E were generally consistent with published values from previous studies."( Reanalysis of carbamazepine and carbamazepine-epoxide pharmacokinetics after multiple dosing of extended release formulation.
Dechasathian, S; Konsil, J; Mason, DH; Stevens, RE,
)
0.49
"The aim of this study was to obtain a pharmacokinetic calculation for valproic acid (VPA) and its free fraction in 50 children and adolescents (4-18 years) treated for epilepsy in VPA monotherapy and bitherapy with carbamazepine (CBZ)."( Studies on the pharmacokinetics of total and free valproate in mono- and bitherapy with carbamazepine in epileptic children and adolescents.
Galas-Zgorzalewicz, B; Steinborn, B, 2002
)
0.72
"The possibility of pharmacokinetic interactions between Sho-saiko-to extract powder (TJ-9), the most widely used traditional Chinese herbal (Kampo) medicine in Japan, and carbamazepine (CBZ), an important anti-epileptic drug, was examined in rats."( Studies on interactions between traditional herbal and western medicines. V. effects of Sho-saiko-to (Xiao-Cai-hu-Tang) on the pharmacokinetics of carbamazepine in rats.
Kuroda, K; Nagasawa, K; Ohnishi, N; Okada, K; Takara, K; Yokoyama, T; Yoshioka, M, 2002
)
0.71
"To study the pharmacokinetics of a combination oral contraceptive (OC) containing norethindrone and ethinyl estradiol during OC monotherapy, concomitant OC and topiramate (TPM) therapy, and concomitant OC and carbamazepine (CBZ) therapy in order to comparatively evaluate the pharmacokinetic interaction, which may cause contraceptive failure."( Effect of topiramate or carbamazepine on the pharmacokinetics of an oral contraceptive containing norethindrone and ethinyl estradiol in healthy obese and nonobese female subjects.
Bialer, M; Doose, DR; Jacobs, D; Padmanabhan, M; Schwabe, S; Wang, SS, 2003
)
0.81
"To investigate the pharmacokinetic profile of carbamazepine (CBZ) in Chinese epilepsy patients."( Population pharmacokinetics of carbamazepine in Chinese epilepsy patients.
Hu, M; Jiao, Z; Shi, XJ; Zhang, JH; Zhong, MK, 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
" d(-1) given twice daily had 1 to 4 blood samples collected per patient for population pharmacokinetic analysis of oxcarbazepine's major bioactive 10-monohydroxy metabolite."( Pharmacokinetic drug interactions in children taking oxcarbazepine.
D'souza, J; Hossain, M; Milosavljev, S; Sallas, WM, 2003
)
0.32
"The population pharmacokinetic data for 10-monohydroxy metabolite consisted of a total of 376 observations from 109 patients, aged 3 to 17 years."( Pharmacokinetic drug interactions in children taking oxcarbazepine.
D'souza, J; Hossain, M; Milosavljev, S; Sallas, WM, 2003
)
0.32
"The pharmacokinetic properties of a drug are the primary deter-minant of the extent and duration of drug action, and influence susceptibility to clinically important drug interactions."( The ideal pharmacokinetic properties of an antiepileptic drug: how close does levetiracetam come?
Johannessen, SI; Perucca, E, 2003
)
0.32
"75-4h and 6h postdose, after which they declined with an approximate mean apparent terminal half-life of 8-17h and 7-12h, respectively."( Safety, tolerability and pharmacokinetic profile of BIA 2-093, a novel putative antiepileptic agent, during first administration to humans.
Almeida, L; Soares-da-Silva, P, 2003
)
0.32
"This paper describes a developed pharmacokinetic model for the estimation of valproic acid (VPA) clearance (CL) calculated from routine clinical data taken from Egyptian epileptic patients."( Pharmacokinetic modelling of valproic acid from routine clinical data in Egyptian epileptic patients.
Cosson, V; EL Desoky, ES; EL Din Amry, S; Fuseau, E, 2004
)
0.32
"The population pharmacokinetic model for VPA could be used for a priori recommendation and dose optimisation of that drug in the Egyptian population of epileptic patients."( Pharmacokinetic modelling of valproic acid from routine clinical data in Egyptian epileptic patients.
Cosson, V; EL Desoky, ES; EL Din Amry, S; Fuseau, E, 2004
)
0.32
" A pharmacokinetic interaction may be involved in such potentiation."( Effect of nimodipine, a dihydropyridine calcium channel antagonist on the pharmacokinetics of carbamazepine in rhesus monkeys.
Bhargava, VK; Das, BP; Garg, SK; Gupta, MC, 2003
)
0.54
" The aim of the present work was to study the pharmacokinetic behavior of this group of women during steady state."( Pharmacokinetic study of carbamazepine and its carbamazepine 10,11-epoxide metabolite in a group of female epileptic patients under chronic treatment.
Amancio, O; Belmont, A; Campos, MG; Heinze, G; Jaimes, O; López, G; Moreno, J; Pérez, P; Santos, JA,
)
0.43
" Pharmacokinetic parameters were calculated by statistical moment method after obtaining serum concentrations."( Pharmacokinetic study of carbamazepine and its carbamazepine 10,11-epoxide metabolite in a group of female epileptic patients under chronic treatment.
Amancio, O; Belmont, A; Campos, MG; Heinze, G; Jaimes, O; López, G; Moreno, J; Pérez, P; Santos, JA,
)
0.43
"The schedule we suggest for therapeutic monitoring of serum concentrations of CBZ in chronic treatments is 3 h for maximum peak concentration of C(max) after dose administration and for minimum peak concentration, C(min) prior to subsequent administration of the dose."( Pharmacokinetic study of carbamazepine and its carbamazepine 10,11-epoxide metabolite in a group of female epileptic patients under chronic treatment.
Amancio, O; Belmont, A; Campos, MG; Heinze, G; Jaimes, O; López, G; Moreno, J; Pérez, P; Santos, JA,
)
0.43
"To develop a population pharmacokinetic model to evaluate the effects of variety of covariates on clearance of carbamazepine (CBZ) and its main metabolite carbamazepine-10,11-epoxide (CBZE) in Chinese population."( Population pharmacokinetic modeling of steady state clearance of carbamazepine and its epoxide metabolite from sparse routine clinical data.
Jiao, Z; Shi, XJ; Zhao, ZG; Zhong, MK, 2004
)
0.77
" Median maximum plasma concentrations of the major metabolite (licarbazepine, (+/-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide) were attained (t(max)) at 2 to 3 h postdose; thereafter, plasma concentrations declined with a mean apparent terminal half-life of 9 to 13 h following repeated dosing."( 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
" Part I was a pharmacokinetic study in children stratified by age (2-5 years and 6-12 years) and randomized to receive a single oxcarbazepine dose of 5 mg/kg or 15 mg/kg."( Oxcarbazepine pharmacokinetics and tolerability in children with inadequately controlled epilepsy.
Bulteau, C; D'Souza, J; Dulac, O; Markabi, S; Motte, J; Pons, G; Rey, E; Sturm, Y; Tran, A, 2004
)
0.32
" Ten CYP2D6 genotyped and depressive (F32x and F33x, ICD-10) patients participated in an open study on the pharmacokinetic and pharmacodynamic consequences of a carbamazepine augmentation in VEN non-responders."( Combination therapy with venlafaxine and carbamazepine in depressive patients not responding to venlafaxine: pharmacokinetic and clinical aspects.
Baumann, P; Brawand-Amey, M; Brocard, M; Ciusani, E; Eap, CB; Zullino, DF, 2004
)
0.79
" Plasma was separated and stored at -20 degrees C until assayed for phenytoin and carbamazepine by HPLC and different pharmacokinetic parameters were calculated."( Influence of high fat diet (butter) on pharmacokinetics of phenytoin and carbamazepine.
Garg, SK; Malhotra, S; Sidhu, S, 2004
)
0.78
" Two hundred and thirty-four patients, and 1254 and 1251 plasma concentrations for delavirdine and N-delavirdine, respectively, were available for population pharmacokinetic analysis."( 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
" Mean (%CV) population pharmacokinetic parameter estimates for delavirdine were: volume of distribution at steady state 67."( 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
"Delavirdine disposition exhibits nonlinear pharmacokinetics and large interpatient variability, and is significantly altered by time of day (impacting potential therapeutic drug monitoring and future pharmacokinetic study designs)."( 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
" On the other hand, the elimination half-life of carbamazepine and the AUC ratio of carbamazepine 10,11-epoxide to carbamazepine were not altered by the injection of pomegranate juice."( Effects of pomegranate juice on human cytochrome p450 3A (CYP3A) and carbamazepine pharmacokinetics in rats.
Arimori, K; Fujita, K; Hidaka, M; Iwakiri, T; Ogikubo, T; Okumura, M; Setoguchi, N; Yamasaki, K, 2005
)
0.82
" However, these combinations were associated with significant pharmacokinetic interactions, in that LCZ increased brain TPM (94%), OXC (21%), FBM (46%), and LTG (8%) concentrations."( Pharmacodynamic and pharmacokinetic interaction studies of loreclezole with felbamate, lamotrigine, topiramate, and oxcarbazepine in the mouse maximal electroshock seizure model.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2005
)
0.33
" However, these conclusions are confounded by the fact that LCZ is associated with significant pharmacokinetic interactions."( Pharmacodynamic and pharmacokinetic interaction studies of loreclezole with felbamate, lamotrigine, topiramate, and oxcarbazepine in the mouse maximal electroshock seizure model.
Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2005
)
0.33
" Age was identified as a statistically significant predictor of CL/F at multiple regression analysis, but it accounted for only a modest component of the interindividual pharmacokinetic variation."( Phenobarbital pharmacokinetics in old age: a case-matched evaluation based on therapeutic drug monitoring data.
Battino, D; Croci, D; Mamoli, D; Messina, S; Perucca, E; Ratti, S, 2005
)
0.33
" Simultaneously, the effects on hippocampal monoamines were studied as pharmacodynamic markers for the anticonvulsant activity."( Quantitative in vivo microdialysis study on the influence of multidrug transporters on the blood-brain barrier passage of oxcarbazepine: concomitant use of hippocampal monoamines as pharmacodynamic markers for the anticonvulsant activity.
Clinckers, R; Ebinger, G; Meurs, A; Michotte, Y; Smolders, I, 2005
)
0.33
"Population models can be important extensions of therapeutic drug monitoring (TDM), as they allow estimation of individual pharmacokinetic parameters based on a small number of measured drug concentrations."( 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
"This study used a Bayesian approach to explore the utility of routinely collected and sparse TDM data (1 sample per patient) for carbamazepine (CBZ) monotherapy in developing a population pharmacokinetic (PPK) model for CBZ in pediatric patients that would allow prediction of CBZ concentrations for both immediate- and controlled-release formulations."( 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
)
0.78
" 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
" VPA was not found to have any clinically significant influence on TPM pharmacokinetic and metabolic profiles."( A comparative study of the effect of carbamazepine and valproic acid on the pharmacokinetics and metabolic profile of topiramate at steady state in patients with epilepsy.
Bialer, M; Britzi, M; Doose, DR; Gatti, G; La Neve, A; Levy, RH; Maryanoff, BE; Mimrod, D; Perucca, E; Soback, S; Specchio, LM; Specchio, N, 2005
)
0.6
" Pharmacokinetic parameters were determined by noncompartmental methods."( Lack of pharmacokinetic interaction between oxcarbazepine and lamotrigine.
Ascher, J; Bullman, J; Job, S; Palmer, J; Sidhu, J; Theis, JG, 2005
)
0.33
"The aim of the study was to obtain pharmacokinetic data for carbamazepine (CBZ) and its fractions not bound with proteins in bitherapy with lamotrigine (LTG), topiramate (TPM), vigabatrin (VGB) or valproic acid (VPA) in children and adolescents treated for epilepsy."( Pharmacokinetic interactions of carbamazepine with some antiepileptic drugs during epilepsy treatment in children and adolescents.
Steinborn, B, 2005
)
0.85
" For pharmacokinetic calculations of total and free CBZ, one-compartment model was used according to standardized procedure."( Pharmacokinetic interactions of carbamazepine with some antiepileptic drugs during epilepsy treatment in children and adolescents.
Steinborn, B, 2005
)
0.61
"No significant differences in pharmacokinetic parameters of unbound CBZ in four groups of patients on bitherapy with CBZ and LTG, TPM, VGB or VPA were found."( Pharmacokinetic interactions of carbamazepine with some antiepileptic drugs during epilepsy treatment in children and adolescents.
Steinborn, B, 2005
)
0.61
" The effects on dopamine and serotonin levels are therefore proposed as pharmacodynamic markers for the anticonvulsant activity of these compounds."( Hippocampal dopamine and serotonin elevations as pharmacodynamic markers for the anticonvulsant efficacy of oxcarbazepine and 10,11-dihydro-10-hydroxycarbamazepine.
Clinckers, R; Ebinger, G; Meurs, A; Michotte, Y; Smolders, I, 2005
)
0.53
" Likewise, PGB steady-state pharmacokinetic parameter values were similar among patients receiving CBZ, PHT, LTG, or VPA and, in general, were similar to those observed historically in healthy subjects receiving PGB alone."( 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
" In population pharmacokinetic analyses of such TDM data, CL has frequently been modeled as a function of dose."( Inherent correlation between dose and clearance in therapeutic drug monitoring settings: possible misinterpretation in population pharmacokinetic analyses.
Ahn, JE; Birnbaum, AK; Brundage, RC, 2005
)
0.33
" Plasma carbamazepine levels were assayed by high-performance liquid chromatography and pharmacokinetic parameters calculated."( Effects of artemisinin, artemether, arteether on the pharmacokinetics of carbamazepine.
Medhi, B; Pandhi, P; Sukhija, M, 2006
)
1
" Brain AED concentrations were determined to ascertain any pharmacokinetic contribution to the observed antiseizure effect."( Pharmacodynamic and pharmacokinetic characterization of interactions between levetiracetam and numerous antiepileptic drugs in the mouse maximal electroshock seizure model: an isobolographic analysis.
Andres, MM; Cioczek-Czuczwar, A; Czuczwar, P; Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.33
"These preclinical data would suggest that LEV in combination with TPM is associated with beneficial anticonvulsant pharmacodynamic interactions."( Pharmacodynamic and pharmacokinetic characterization of interactions between levetiracetam and numerous antiepileptic drugs in the mouse maximal electroshock seizure model: an isobolographic analysis.
Andres, MM; Cioczek-Czuczwar, A; Czuczwar, P; Czuczwar, SJ; Luszczki, JJ; Patsalos, PN; Ratnaraj, N, 2006
)
0.33
" Concurrently, we have noted a significant constant reduction of the half-life of CBZ from serum in the first group: 12."( Influence of activated charcoal on the pharmacokinetics and the clinical features of carbamazepine poisoning.
Amamou, M; Brahmi, N; Kouraichi, N; Thabet, H, 2006
)
0.56
" In that control group, TDM was performed in the same pharmacokinetic (PK) laboratory, using the same sampling strategy as in the present study, and the same PK population modelling software was used for data analysis."( 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
"Previous studies have demonstrated that pharmacokinetic behavior of several drugs such as paracetamol, theophylline, and aminoglycosides are significantly altered in patients with spinal cord injury."( The influence of experimental spinal cord injury on carbamazepine pharmacokinetics.
Ansari, M; Karamousian, S; Reihani-Kermani, H, 2006
)
0.58
" Pharmacokinetic parameters including maximum concentration, time to reach maximum concentration, half-life, and area under the curve(0 - 24) were directly determined from the concentration-time curve."( The influence of experimental spinal cord injury on carbamazepine pharmacokinetics.
Ansari, M; Karamousian, S; Reihani-Kermani, H, 2006
)
0.58
" In spinal cord-injured group, area under the curve and half-life were increased from 29."( The influence of experimental spinal cord injury on carbamazepine pharmacokinetics.
Ansari, M; Karamousian, S; Reihani-Kermani, H, 2006
)
0.58
"We concluded that pharmacokinetic behavior of carbamazepine was not significantly changed by spinal cord injury, although its subtle pharmacokinetic changes could be resulted from alteration in gastrointestinal tract motility, blood perfusion, or metabolism."( The influence of experimental spinal cord injury on carbamazepine pharmacokinetics.
Ansari, M; Karamousian, S; Reihani-Kermani, H, 2006
)
0.84
"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
"Prediction of the exposure of neonates, infants and children to xenobiotics is likely to be more successful using physiologically based pharmacokinetic models than simplistic allometric scaling, particularly in younger children."( 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
" In vitro enzyme pharmacokinetic parameters (maximum rate of metabolism [Vmax] and Michaelis-Menten constant [Km]) and in vivo clearance data were obtained from the literature."( 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
"The in silico prediction of pharmacokinetic behaviour in paediatric patients is not intended to replace clinical studies."( 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 drugs that are eliminated renally completely unchanged (gabapentin, pregabalin and vigabatrin) or mainly unchanged (levetiracetam and topiramate), the pharmacokinetic variability is less pronounced and more predictable."( Pharmacokinetic variability of newer antiepileptic drugs: when is monitoring needed?
Johannessen, SI; Tomson, T, 2006
)
0.33
"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
"9 L/h and consequently its mean half-life was shortened from 10."( 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
" CBZ induced RWJ-333369 clearance, resulting in shortened half-life and decreased exposure (AUCss) and C(max)."( 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
" Quinidine Cmax decreased by means of 29% (CI: 16-40, p=0."( A comparative pharmacokinetic study in healthy volunteers of the effect of carbamazepine and oxcarbazepine on cyp3a4.
Andreasen, AH; Brøsen, K; Damkier, P, 2007
)
0.57
" The elimination half-life for the entire patient population was approximately twofold longer than the value reported in the product labeling (40-50 h vs 22 h)."( Factors affecting antiepileptic drug pharmacokinetics in community-dwelling elderly.
Birnbaum, AK; Cloyd, JC; Marino, S, 2007
)
0.34
" The data were evaluated using a mechanistic pharmacokinetic approach in NONMEM."( 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
)
0.67
"The aim of the present study was to develop a population pharmacokinetic model of carbamazepine from routine therapeutic drug monitoring data."( 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
)
0.84
"The aim of this study was to define a population pharmacokinetic model that could estimate the clearance of valproate (VPA) in a Serbian epileptic population."( Pharmacokinetic modeling of valproate from clinical data in Serbian epileptic patients.
Jankovic, SM; Milovanovic, JR, 2007
)
0.34
" Because it was known from the literature that the half-life of midazolam can increase at high dosage, the kinetics of midazolam (MDZ), 1'-hydroxymidazolam, and 4-hydroxymidazolam were assessed at steady state (dosage 1 mg/min) and after stopping treatment."( Pharmacokinetics of midazolam and metabolites in a patient with refractory status epilepticus treated with extraordinary doses of midazolam.
Bodmer, M; Grignaschi, N; Haschke, M; Krähenbühl, S; Kummer, O; Link, B; Ruegg, S, 2008
)
0.35
" In summary, a 2-way pharmacokinetic interaction between efavirenz and carbamazepine was demonstrated in this study."( Pharmacokinetic interaction between efavirenz and carbamazepine after multiple-dose administration in healthy subjects.
Damle, B; Grasela, DM; Ji, P; Kaul, S; Unger, SE; Xie, J, 2008
)
0.83
"Four different approaches to population pharmacokinetic analysis were applied to routine clinical data on carbamazepine intoxications in epileptic and alcoholic patients."( A comparison of computational approaches to the population pharmacokinetics. An example of toxicological data.
Jawień, W; Krypel, Ł; Piekoszewski, W,
)
0.34
"The purpose of the present study was to evaluate the effect of kainic acid (KA)-induced acute seizures on the pharmacokinetic profiles of antiepileptic drug, carbamazepine (CBZ) in mice."( Evaluation of carbamazepine pharmacokinetic profiles in mice with kainic acid-induced acute seizures.
Honda, N; Nishimura, A; Shibata, N; Sugioka, N; Takada, K, 2008
)
0.9
" There have been no previous studies designed to investigate a potential pharmacokinetic (PK) interaction between MCB and VPA or CBZ; however, these agents are likely to be used concomitantly for the treatment of depressive disorders."( Moclobemide monotherapy vs. combined therapy with valproic acid or carbamazepine in depressive patients: a pharmacokinetic interaction study.
Miljkovic, B; Pokrajac, M; Rakic Ignjatovic, A; Timotijevic, I; Todorovic, D, 2009
)
0.59
"The purpose of this study was to perform population pharmacokinetic (PPK) analysis on carbamazepine and to determine the population model of clearance of this drug in terms of individual patient characteristics."( Pharmacokinetic modeling of carbamazepine based on clinical data from Serbian epileptic patients.
Jankovic, SM; Jovanovic, D; Milovanovic, JR, 2008
)
0.86
" The pharmacokinetic parameters were compared by Students t-test."( Pharmacokinetic interaction of single dose of piperine with steady-state carbamazepine in epilepsy patients.
Hota, D; Kharbanda, P; Pandhi, P; Pattanaik, S; Prabhakar, S, 2009
)
0.58
" Both formulations showed similar pharmacokinetic profiles and could represent valuable formulations in case of emergencies, when a rapid action in the central nervous system is desirable."( Pharmacokinetic study of a carbamazepine nanoemulsion in beagle dogs.
de Araújo, BV; Kelmann, RG; Koester, LS; Kratz, JM; Kuminek, G; Ribeiro, R; Simões, CM; Teixeira, HF, 2009
)
0.65
" The half-life of omeprazole was also increased after both acute and chronic administration of soybean."( Effect of soybean administration on the pharmacokinetics of carbamazepine and omeprazole in rats.
Asad, M; Singh, D, 2010
)
0.6
"Pharmacokinetic and pharmacodynamic interactions between carbamazepine and aripiprazole were studied in 18 inpatients with schizophrenia being treated with aripiprazole."( Pharmacokinetic and pharmacodynamic interactions between carbamazepine and aripiprazole in patients with schizophrenia.
Kondo, T; Mihara, K; Nagai, G; Nakamura, A; Suzuki, T, 2009
)
0.84
" Two open-label, multiple-dose clinical trials were conducted to evaluate the potential for pharmacokinetic interaction between lacosamide and carbamazepine."( No pharmacokinetic interaction between lacosamide and carbamazepine in healthy volunteers.
Cawello, W; Eggert-Formella, A; Nickel, B, 2010
)
0.81
" The developed assay was applied to a pharmacokinetic study in humans."( Development and validation of a highly sensitive LC-MS/MS method for simultaneous quantitation of nortriptyline and 10-hydroxynortriptyline in human plasma: application to a human pharmacokinetic study.
Bharathi, DV; Hotha, KK; Jagadeesh, B; Kumar, KK; Mullangi, R; Rao, DV; Ravindranath, LK; Reddy, YR; Veera, KN, 2010
)
0.36
"The aim of the present study was to build population pharmacokinetic models for the clearance of valproate (VPA) in 2 separate populations of Serbian patients with epilepsy, children and adults."( Factors influencing valproate pharmacokinetics in children and adults.
Jankovic, S; Jankovic, SM; Milovanovic, JR, 2010
)
0.36
" The pharmacokinetic models obtained were validated in groups of 15 epileptic patients, each showing good predictive performance of the model."( Factors influencing valproate pharmacokinetics in children and adults.
Jankovic, S; Jankovic, SM; Milovanovic, JR, 2010
)
0.36
" Information on the kinetics of these drug interactions with HSA would be valuable in understanding the pharmacokinetic behavior of these drugs and could provide data that might lead to the creation of improved assays for these analytes in biological samples."( Kinetic studies of drug-protein interactions by using peak profiling and high-performance affinity chromatography: examination of multi-site interactions of drugs with human serum albumin columns.
Hage, DS; Ohnmacht, CM; Papastavros, E; Schiel, JE; Smith, QR; Tong, Z, 2011
)
0.37
"The objective of this study was to evaluate the pharmacokinetic interaction between zolpidem and carbamazepine in healthy volunteers."( Pharmacokinetic interaction between zolpidem and carbamazepine in healthy volunteers.
Bâldea, I; Leucuţa, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.84
" Change in pharmacokinetic parameters was due to slow metabolism or elimination of CBZ when given concurrently with ciprofloxacin to the adult volunteers."( Therapeutic effects of ciprofloxacin on the pharmacokinetics of carbamazepine in healthy adult male volunteers.
Ashraf, MY; Asi, MR; Aslam, B; Javed, I; Muhammad, F; Shahzadi, A, 2011
)
0.61
" We sought to assess the pharmacodynamic effects of CBZ on breakthrough bleeding and ovulation during oral contraceptive (OC) use."( Carbamazepine coadministration with an oral contraceptive: effects on steroid pharmacokinetics, ovulation, and bleeding.
Davis, AR; Stanczyk, FZ; Westhoff, CL, 2011
)
1.81
" Our objective was to evaluate a possible pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.84
" Pharmacokinetic parameters of ivabradine administered in each treatment period were calculated using non-compartmental and compartmental analysis to determine if there were statistically significant differences."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.62
" These differences were statistically significant for C(max) and AUC(0-∞) when ivabradine was administered with carbamazepine, whereas they were not for t(max), half-life and mean residence time."( Pharmacokinetic interaction between ivabradine and carbamazepine in healthy volunteers.
Bâldea, I; Leucuta, SE; Muntean, D; Neag, M; Popa, A; Vlase, L, 2011
)
0.83
"Most of bayesian pharmacokinetic studies and the influence of clinical variables have been carried out in adults."( Effect of treatment and additional disease on pharmacokinetic of valproic acid in children with epilepsy.
Flores Pérez, J; Flores-Murrieta, F; Juárez-Olguín, H; Lares Asseff, I; Lugo-Goytia, G; Ruiz-García, M,
)
0.13
"The aim was to estimate population-based pharmacokinetic of valproic acid (VPA) and to determine the effect of treatment and additional disease on its performance in children with epilepsy."( Effect of treatment and additional disease on pharmacokinetic of valproic acid in children with epilepsy.
Flores Pérez, J; Flores-Murrieta, F; Juárez-Olguín, H; Lares Asseff, I; Lugo-Goytia, G; Ruiz-García, M,
)
0.13
"Based on a population model of children with epilepsy, the pharmacokinetic of VPA could be altered by weight, age and the administration of CBZ and additional GER to epilepsy."( Effect of treatment and additional disease on pharmacokinetic of valproic acid in children with epilepsy.
Flores Pérez, J; Flores-Murrieta, F; Juárez-Olguín, H; Lares Asseff, I; Lugo-Goytia, G; Ruiz-García, M,
)
0.13
"Blood samples for the pharmacokinetic assessment were taken at pre-dose, and 1, 2, 3, 4, 6, 8, 12 and 24h post-dose at steady-state in 51 patients stabilised on chronic (beyond 1 year) treatment with ESL 400mg (n=7), 800mg (n=26) or 1200mg (n=18) once-daily."( 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 major compound in plasma was the active metabolite eslicarbazepine, which reached maximum concentrations (C(max)) 2h post-dose; thereafter, its plasma concentrations declined with a mean apparent half-life of 13, 14, and 20h in patients receiving ESL doses of 400, 800, and 1200mg once daily, respectively."( 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 aim of the present study was to build population pharmacokinetic models for the clearance of carbamazepine (CBZ) in two separate populations of Serbian patients with epilepsy, children and adults."( Factors influencing carbamazepine pharmacokinetics in children and adults: population pharmacokinetic analysis.
Jankovic, SM; Milovanovic, JR, 2011
)
0.91
" The pharmacokinetic models obtained were validated in groups of 18 children and 13 adults with epilepsy."( Factors influencing carbamazepine pharmacokinetics in children and adults: population pharmacokinetic analysis.
Jankovic, SM; Milovanovic, JR, 2011
)
0.69
"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
" The P-gp inducer showed a greater effect on the pharmacokinetic parameters of (S)-fexofenadine."( Carbamazepine differentially affects the pharmacokinetics of fexofenadine enantiomers.
Akamine, Y; Kojima, M; Miura, M; Uno, T; Yasui-Furukori, N, 2012
)
1.82
" Similar pharmacokinetic changes were observed in HL rats after oral administration of CBZ."( Effects of poloxamer 407-induced hyperlipidemia on the pharmacokinetics of carbamazepine and its 10,11-epoxide metabolite in rats: Impact of decreased expression of both CYP3A1/2 and microsomal epoxide hydrolase.
Kang, HE; Kim, SG; Kim, YW; Lee, I; Lee, MG; Lee, YS, 2012
)
0.61
" A population pharmacokinetic model was developed using NONMEM."( 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
" In population pharmacokinetic modeling, the apparent clearance of OHC was higher by 31."( 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
" Population pharmacokinetic analysis showed that the apparent clearance of OHC increased with comedication with EIAEDs."( 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
" Owing to the lack of an intravenous formulation, its absolute bioavailability, absolute clearance, and half-life in patients at steady state have not been determined."( 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
" The aims of this study were to determine the pharmacokinetic parameters and their variability of carbamazepine in elderly patients and to quantify the effect of covariates on these parameters."( Population pharmacokinetics of carbamazepine in elderly patients.
Birnbaum, AK; Brundage, RC; Collins, JF; Macias, FM; Punyawudho, B; Ramsay, ER, 2012
)
0.88
"Prospectively collected carbamazepine concentrations from 121 patients aged 60 years or older were used to develop a population pharmacokinetic model."( Population pharmacokinetics of carbamazepine in elderly patients.
Birnbaum, AK; Brundage, RC; Collins, JF; Macias, FM; Punyawudho, B; Ramsay, ER, 2012
)
0.97
" UGT polymorphisms had no influence on the pharmacokinetic interactions between carbamazepine and VPA."( Influence of UDP-glucuronosyltransferase polymorphisms on valproic acid pharmacokinetics in Chinese epilepsy patients.
Chu, XM; Hao, HP; Wang, GJ; Zhang, LF; Zhang, SN; Zhou, JH, 2012
)
0.61
" There is still insufficient documentation regarding pharmacokinetic variability of these AEDs in different patient groups."( Pharmacokinetic variability of four newer antiepileptic drugs, lamotrigine, levetiracetam, oxcarbazepine, and topiramate: a comparison of the impact of age and comedication.
Baftiu, A; Johannessen Landmark, C; Johannessen, SI; Larsson, PG; Rytter, E; Tysse, I; Valsø, B, 2012
)
0.38
"The purpose of this study was to compare age and comedication as factors contributing to pharmacokinetic variability between 4 newer AEDs (lamotrigine, levetiracetam, oxcarbazepine, and topiramate) among patients with refractory epilepsy."( Pharmacokinetic variability of four newer antiepileptic drugs, lamotrigine, levetiracetam, oxcarbazepine, and topiramate: a comparison of the impact of age and comedication.
Baftiu, A; Johannessen Landmark, C; Johannessen, SI; Larsson, PG; Rytter, E; Tysse, I; Valsø, B, 2012
)
0.38
" The interindividual pharmacokinetic variability was extensive, as illustrated by a 10-fold variability in serum concentration compared with dose."( Pharmacokinetic variability of four newer antiepileptic drugs, lamotrigine, levetiracetam, oxcarbazepine, and topiramate: a comparison of the impact of age and comedication.
Baftiu, A; Johannessen Landmark, C; Johannessen, SI; Larsson, PG; Rytter, E; Tysse, I; Valsø, B, 2012
)
0.38
"Age and comedication are important contributors to pharmacokinetic variability."( Pharmacokinetic variability of four newer antiepileptic drugs, lamotrigine, levetiracetam, oxcarbazepine, and topiramate: a comparison of the impact of age and comedication.
Baftiu, A; Johannessen Landmark, C; Johannessen, SI; Larsson, PG; Rytter, E; Tysse, I; Valsø, B, 2012
)
0.38
"CBZ and CBZE time-concentration profiles in various scenarios were generated based on a population pharmacokinetic study in Chinese epilepsy patients using Monte Carlo simulation."( 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
" Consequences of these pharmacokinetic (PK) properties may include adverse events (AEs) and breakthrough seizures, potentially leading to poor adherence."( Extended-release antiepileptic drugs: a comparison of pharmacokinetic parameters relative to original immediate-release formulations.
Hovinga, CA; Leppik, IE, 2013
)
0.39
" The proposed method was found to be applicable to pharmacokinetic studies."( A rapid and sensitive liquid chromatography-tandem mass spectrometric assay for cycloserine in 50μL of human plasma: Its pharmacokinetic application.
Gajula, R; Gandu, V; Maddela, R; Pilli, NR; Polagani, SR, 2013
)
0.39
"To establish using dried blood spot (DBS) as a surrogate to plasma for therapeutic drug monitoring (TDM) of carbamazepine (CBZ), we compared the population pharmacokinetic (PPK) estimates from concurrent DBS and plasma levels."( Estimation and comparison of carbamazepine population pharmacokinetics using dried blood spot and plasma concentrations from people with epilepsy: the clinical implication.
Chan, E; Ho, PC; Kong, ST; Lim, SH, 2014
)
0.91
" Pharmacokinetic parameters were calculated by using PK Solver."( Pharmacokinetic interaction studies of fenugreek with CYP3A substrates cyclosporine and carbamazepine.
Ahad, A; Al-Jenoobi, FI; Al-Mohizea, AM; Al-Suwayeh, SA; Alam, MA; Alkharfy, KM; Iqbal, M; Korashy, HM; Raish, M, 2014
)
0.62
" The present investigation was mainly carried out in order to generate in vivo pharmacokinetic data that can be utilized for development and validation of in silico models."( 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
"To determine the effects of CYP3A5 polymorphisms on carbamazepine (CBZ) pharmacokinetic parameters when CBZ is used either as monotherapy or co-administered with phenytoin (PHT), phenobarbital (PB) or valproic acid (VPA)."( 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
)
0.89
" Pharmacokinetic parameters of CBZ; clearance and dose-adjusted CBZ levels in patients with different genotypes were calculated and compared."( 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
" Finally, we successfully applied this analytical method to a pre-clinical oral pharmacokinetic study, revealing the plasma profiles of both carbamazepine and carbamazepine-10,11-epoxide following oral administration of carbamazepine to rats."( Quantification of carbamazepine and its 10,11-epoxide metabolite in rat plasma by UPLC-UV and application to pharmacokinetic study.
Beig, A; Dahan, A, 2014
)
0.94
" 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
" A sensitive and selective liquid chromatography mass spectrometry method for determination of acetylcorynoline in rat plasma was developed over the range of 5-1000 ng/mL to characterize the pharmacokinetic properties."( 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
"Pharmacotherapy for mood disorders during pregnancy is often complicated by pregnancy-related pharmacokinetic changes and the need for dose adjustments."( Pharmacotherapy for mood disorders in pregnancy: a review of pharmacokinetic changes and clinical recommendations for therapeutic drug monitoring.
Byatt, N; Deligiannidis, KM; Freeman, MP, 2014
)
0.4
"The English-language literature indexed on MEDLINE/PubMed was searched for original observational studies (controlled and uncontrolled, prospective and retrospective), case reports, and case series that evaluated or described pharmacokinetic changes or TDM during pregnancy or the postpartum period."( Pharmacotherapy for mood disorders in pregnancy: a review of pharmacokinetic changes and clinical recommendations for therapeutic drug monitoring.
Byatt, N; Deligiannidis, KM; Freeman, MP, 2014
)
0.4
"Substantial pharmacokinetic changes can occur during pregnancy in a number of commonly used antidepressants and mood stabilizers."( Pharmacotherapy for mood disorders in pregnancy: a review of pharmacokinetic changes and clinical recommendations for therapeutic drug monitoring.
Byatt, N; Deligiannidis, KM; Freeman, MP, 2014
)
0.4
" Perampanel is metabolized primarily via CYP3A4, yet it has a relatively long half-life of 105h; it is, therefore, recommended that perampanel be given once daily (preferably at bedtime)."( 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
"Pharmacokinetic simulations were performed using validated perampanel pharmacokinetic parameters, derived from 19 phase I studies in 606 subjects, to investigate the effect on perampanel plasma concentration of (1) missing a dose of perampanel followed by delayed replacement of the missed dose, (2) missing a dose followed by resumption of scheduled therapy, and (3) missing a dose in the presence/absence of carbamazepine."( 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
)
0.57
"Our results corroborate that given the pharmacokinetic characteristics of perampanel, a missed dose is unlikely to cause as much fluctuation in plasma concentration as would be expected for a drug with a short half-life."( 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
"These pharmacokinetic simulations suggest that the long half-life of perampanel may be advantageous in conferring a relatively smooth concentration-time profile with a once-daily or twice-daily dosing, even in the presence of concomitant EIAEDs."( 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 purpose of the current study was to use physiologically based pharmacokinetic modeling (PBPK) quantitatively to predict the PK of the XR formulation in children and adolescents."( 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
"This study was to establish the population pharmacokinetic (PPK) model of pharmacologically active metabolite of oxcarbazepine (OXC) and to estimate PPK parameters for the optimal individuation administration 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
" Pharmacokinetic parameters were estimated according to a one-compartment model with first-order absorption and elimination."( 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 purpose of this study is to investigate the effects of multiple-trough sampling design and nonlinear mixed effect modeling (NONMEM) algorithm on the estimation of population and individual pharmacokinetic parameters."( [Effects of multiple-trough sampling design and algorithm on the estimation of population and individual pharmacokinetic parameters].
Ding, JJ; Jiao, Z; Ling, J; Qian, LX, 2014
)
0.4
"The population values of pharmacokinetic parameters estimated in the final model were as follows: Ka=0."( Population pharmacokinetics modeling of oxcarbazepine to characterize drug interactions in Chinese children with epilepsy.
Chen, YJ; Gao, P; Liu, MC; Niu, CH; Peng, J; Wang, Y; Xu, H; Zhang, HN, 2014
)
0.4
" Part 1 was an open-label pharmacokinetic assessment of a single 5-mg vilazodone dose with or without ketoconazole."( 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 upper limit of the 90% CIs for the vilazodone AUC and Cmax geometric mean ratios exceeded 125%."( 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
"Valproic acid (VPA) follows a non-linear pharmacokinetic profile in terms of protein-binding saturation."( 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
" The population pharmacokinetic model was developed using NONMEM(®) software."( 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
" 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
" 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
" Pharmacokinetic parameters for carbamazepine, armodafinil, and their major circulating metabolites were determined when dosed alone and after pretreatment with the other drug."( 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
)
0.92
"Eighty-one subjects enrolled in the study (group 1 = 40; group 2 = 41), of whom 79 (group 1 = 40; group 2 = 39) were evaluable for pharmacokinetic analysis and 80 (group 1 = 40; group 2 = 40) were evaluable for safety analysis."( 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
)
0.64
" Furthermore, RSV pretreatment significantly decreased metabolite to parent (CBZE/CBZ) ratios of Cmax and AUC and significantly increased CBZE/CBZ ratios of CL/F and Vd/F, indicating the reduced formation of CBZE to CBZ."( Effect of resveratrol on the pharmacokinetics of carbamazepine in healthy human volunteers.
Bedada, SK; Nearati, P, 2015
)
0.67
"The aim of the study was to develop a population pharmacokinetic (PPK) model of oxcarbazepine and optimize the treatment of oxcarbazepine in Chinese patients with epilepsy."( 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
" As a third-generation medication, ESL is believed to have favorable efficacy/safety profile and pharmacokinetic properties in comparison with related drugs (carbamazepine and oxcarbazepine)."( Pharmacokinetic/pharmacodynamic evaluation of eslicarbazepine for the treatment of epilepsy.
Banach, M; Borowicz, KK; Czuczwar, SJ, 2015
)
0.61
"The aim of the paper was to evaluate pharmacodynamic and pharmacokinetic properties of ESL with aspect to epilepsy treatment."( Pharmacokinetic/pharmacodynamic evaluation of eslicarbazepine for the treatment of epilepsy.
Banach, M; Borowicz, KK; Czuczwar, SJ, 2015
)
0.42
"The population pharmacokinetic model reported here was developed using data from 2 phase 2 trials of irinotecan for treatment of malignant glioma to quantify the impact of concomitant therapy with enzyme-inducing antiepileptic drugs (EIAEDs) on irinotecan pharmacokinetics."( Quantification of the impact of enzyme-inducing antiepileptic drugs on irinotecan pharmacokinetics and SN-38 exposure.
Ames, MM; Berg, AK; Buckner, JC; Galanis, E; Jaeckle, KA; Reid, JM, 2015
)
0.42
" The pharmacokinetic (PK) profiles of MHD were evaluated in pediatric epileptic patients and a possible ethnic difference in PK of MHD between Japanese and non-Japanese pediatric patients was assessed."( 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
" The method was successfully applied to a pharmacokinetic study involving oral administration of caudatin to rats."( Determination of Caudatin in Rat Plasma by UPLC-MS/MS: Application to a Preclinical Pharmacokinetic Study.
Ge, RS; Hu, Y; Mao, B; Shan, Y; Wang, Y; Wu, X; Zhu, Q, 2015
)
0.42
" The parenteral nanoemulsion of CBZ showed significantly higher AUC0→5, AUC0→∞, AUMC0→5, AUMC0→∞, Cmax and lower clearance than that of CBZ solution in plasma."( Nanoemulsion-based Parenteral Drug Delivery System of Carbamazepine: Preparation, Characterization, Stability Evaluation and Blood-Brain Pharmacokinetics.
Abedi Karjiban, RA; Basri, HB; Basri, M; Kirby, BP; Sani, D; Stanslas, J; Tan, SL, 2015
)
0.67
"We recently published analyses regarding the predictive performance of physiologically based pharmacokinetic (PBPK) models, submitted to the US Food and Drug Administration (FDA), for the effect of cytochrome P450 (CYP) inhibitors on the pharmacokinetics of substrate drugs."( Predicting the Effect of CYP3A Inducers on the Pharmacokinetics of Substrate Drugs Using Physiologically Based Pharmacokinetic (PBPK) Modeling: An Analysis of PBPK Submissions to the US FDA.
Hsu, V; Pan, Y; Sinha, V; Wagner, C; Zhao, P, 2016
)
0.43
" This method is suitable for pharmacokinetic study in small animals."( Evaluation of the Effects of Ketoconazole and Voriconazole on the Pharmacokinetics of Oxcarbazepine and Its Main Metabolite MHD in Rats by UPLC-MS-MS.
Cai, JP; Chen, M; Chen, X; Gu, E; Hu, G; Wang, L; Wang, S; Zheng, X; Zhou, H, 2016
)
0.43
" Noncompartmental pharmacokinetic analysis was performed using the WinNonlin program."( Influence of verapamil on the pharmacokinetics of oxcarbazepine and of the enantiomers of its 10-hydroxy metabolite in healthy volunteers.
Alexandre Junior, V; Antunes, Nde J; Coelho, EB; Della Pasqua, O; Lanchote, VL; Marques, MP; Takayanagui, OM; Tozatto, E; Wichert-Ana, L, 2016
)
0.43
" For pharmacokinetic analysis, NONMEM software with implementation of ADVAN 1 subroutine was used."( CYP1A2 genotype affects carbamazepine pharmacokinetics in children with epilepsy.
Djordjevic, N; Jakovljevic, M; Jankovic, S; Milovanovic, D; Milovanovic, DD; Milovanovic, JR; Obradovic, S; Radosavljevic, I; Radovanovic, M, 2016
)
0.74
" Our methodology allowed for a precise pharmacokinetic assessment of clearance based on total quantity of parent drug and active metabolite removed."( Carbamazepine and carbamazepine-10,11-epoxide clearance measurements during continuous venovenous hemofiltration in a massive overdose.
Kearney, T; Petrie, MS; Smollin, CG, 2016
)
1.88
"29); Cmax : 62."( Effect of carbamazepine on the pharmacokinetics of paliperidone extended-release tablets at steady-state.
Berwaerts, J; Cleton, A; Kerbusch-Herben, V; Remmerie, B; Vandebosch, A, 2014
)
0.8
"Based on ibrutinib pharmacokinetics and potential sensitivity towards CYP3A4-mediated drug-drug interactions (DDIs), a physiologically based pharmacokinetic approach was developed to mechanistically describe DDI with various CYP3A4 perpetrators in healthy men under fasting conditions."( Ibrutinib Dosing Strategies Based on Interaction Potential of CYP3A4 Perpetrators Using Physiologically Based Pharmacokinetic Modeling.
De Jong, J; de Zwart, L; Mannaert, E; Monshouwer, M; Snoeys, J; Sukbuntherng, J, 2016
)
0.43
" The purpose of the study was to investigate 2-way pharmacokinetic interactions between ESL and other AEDs as compared to OXC and CBZ."( The Impact of Pharmacokinetic Interactions With Eslicarbazepine Acetate Versus Oxcarbazepine and Carbamazepine in Clinical Practice.
Baftiu, A; Brodtkorb, E; Burns, ML; Dinarevic, J; Johannessen Landmark, C; Johannessen, SI; Kufaas, RF; Reimers, A; Svendsen, T, 2016
)
0.65
"Possible pharmacokinetic interactions have been studied for ESL as compared to OXC and CBZ."( The Impact of Pharmacokinetic Interactions With Eslicarbazepine Acetate Versus Oxcarbazepine and Carbamazepine in Clinical Practice.
Baftiu, A; Brodtkorb, E; Burns, ML; Dinarevic, J; Johannessen Landmark, C; Johannessen, SI; Kufaas, RF; Reimers, A; Svendsen, T, 2016
)
0.65
" The objective of the study was to identify pharmacokinetic interactions of different mood stabilizers on the metabolism of risperidone (RIS) under natural conditions."( 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
"The data give evidence for pharmacokinetic interactions between RIS and different anticonvulsant mood stabilizers."( 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
" 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
"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
" Pharmacokinetic analysis was performed using non-linear mixed effects modelling, and a stepwise covariate search was used to determine factors influencing brivaracetam clearance."( Brivaracetam population pharmacokinetics in children with epilepsy aged 1 month to 16 years.
Schoemaker, R; Stockis, A; Wade, JR, 2017
)
0.46
"This population pharmacokinetic model of oxcarbazepine supports current dose recommendations, except for 10-kg children with concomitant EIAEDs and 50-kg children without EIAEDs."( Population pharmacokinetics of oxcarbazepine and its monohydroxy derivative in epileptic children.
Chiron, C; Comets, E; Dulac, O; Jullien, V; Pons, G; Rey, E; Rodrigues, C, 2017
)
0.46
" The effects of these fibers on the pharmacokinetic profile of CBZ following its oral administration were also examined in rats."( In vitro and in vivo effects of selected fibers on the pharmacokinetics of orally administered carbamazepine: Possible interaction between therapeutic drugs and semisolid enteral nutrients.
Hatsuda, Y; Mukai, J; Myotoku, M; Nagai, K; Omotani, S; Otani, M; Sasatani, M; Takashima, T, 2018
)
0.7
" The pharmacokinetic examination of orally administered CBZ revealed that the area under the curve was significantly lower in the guar gum and xanthan gum groups than in the control group."( In vitro and in vivo effects of selected fibers on the pharmacokinetics of orally administered carbamazepine: Possible interaction between therapeutic drugs and semisolid enteral nutrients.
Hatsuda, Y; Mukai, J; Myotoku, M; Nagai, K; Omotani, S; Otani, M; Sasatani, M; Takashima, T, 2018
)
0.7
"CBZ was adsorbed by fibers used for the semisolidification of enteral nutrients, which may be partially responsible for the alterations observed in the pharmacokinetic profile of CBZ."( In vitro and in vivo effects of selected fibers on the pharmacokinetics of orally administered carbamazepine: Possible interaction between therapeutic drugs and semisolid enteral nutrients.
Hatsuda, Y; Mukai, J; Myotoku, M; Nagai, K; Omotani, S; Otani, M; Sasatani, M; Takashima, T, 2018
)
0.7
"This open-label, single-sequence study in healthy subjects investigated the effects of steady-state carbamazepine on the pharmacokinetic (PK) profile of a single 2-mg dose of fingolimod."( Pharmacokinetic Interaction Between Fingolimod and Carbamazepine in Healthy Subjects.
Behrje, R; David, OJ; Hara, H; Lates, CD; Pal, P; Schmouder, R, 2018
)
0.95
" 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 pharmacological efficacies of CBZ might be reduced by SA through the pharmacokinetic interactions, and that the careful attention should be paid to the timing of administration of CBZ and semi-solid enteral nutrients."( 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
)
0.76
" There are no MHD population pharmacokinetic (PPK) models that describe the influence of genetic factors on MHD pharmacokinetics (PK)."( 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
" Pharmacokinetic variables were derived from plasma concentration-time curves best fitted to a two-compartment model."( Prolonged therapy with the anticonvulsant carbamazepine leads to increased plasma clearance of fentanyl.
Akeju, O; Eskandar, E; Greenblatt, DJ; Hossain, MA; Ma, Z; Martyn, JAJ; Mirzakhani, H; Nozari, A; Wang, Q, 2019
)
0.78
" In the present study, in vitro kinetic solubility in water and dissolution in biorelevant medium integrated with in silico physiologically based pharmacokinetic (PBPK) modeling was used to predict biopharmaceutical performance of SDDS of poorly water-soluble compound, carbamazepine (CBZ)."( Assessment of Biopharmaceutical Performance of Supersaturating Formulations of Carbamazepine in Rats Using Physiologically Based Pharmacokinetic Modeling.
Bansal, AK; Gangwal, R; Narang, AS; Sangamwar, AT; Shete, G; Thakore, SD; Thakur, PS, 2019
)
0.92
"Background Valproic acid is one of several antiepileptic medications requiring therapeutic drug monitoring due to its complex and wide pharmacokinetic interindividual variability."( Estimation of apparent clearance of valproic acid in adult Saudi patients.
Alandas, N; Alqahtani, S; Alsultan, A, 2019
)
0.51
"The clinical value of therapeutic drug monitoring can be increased most significantly by integrating assay results into clinical pharmacokinetic models for optimal dosing."( Development of a methodology to make individual estimates of the precision of liquid chromatography-tandem mass spectrometry drug assay results for use in population pharmacokinetic modeling and the optimization of dosage regimens.
Jelliffe, RW; Karvaly, GB; Kovács, K; Neely, MN; Vásárhelyi, B; Vincze, I, 2020
)
0.56
" This permits optimal dosages by providing the correct weighting factor of assay results in the development of population and individual pharmacokinetic models."( Development of a methodology to make individual estimates of the precision of liquid chromatography-tandem mass spectrometry drug assay results for use in population pharmacokinetic modeling and the optimization of dosage regimens.
Jelliffe, RW; Karvaly, GB; Kovács, K; Neely, MN; Vásárhelyi, B; Vincze, I, 2020
)
0.56
" Plasma samples had been collected and analyzed for CBZ and CBZE, then their noncompartmental pharmacokinetic parameters before and after CBD administration were determined."( The effect of cannabidiol on the pharmacokinetics of carbamazepine in rats.
Darweesh, RS; El-Elimat, T; Khamis, TN, 2020
)
0.81
" This study was to investigate the herb-drug interactions of GR and CBZ, an AED, through pharmacokinetic approach in rats."( 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
)
0.82
" Pharmacokinetic interactions were noted in concomitant use of GR with CBZ by comparing two single-dose treatments (CBZ versus CBZ/GR)."( 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
)
0.82
" Because of its large between-subject variability, several population pharmacokinetic studies have been performed to identify its pharmacokinetic covariates, and thus facilitate individualised therapy."( Population Pharmacokinetics of Levetiracetam: A Systematic Review.
Jiao, Z; Li, ZR; Wang, CY; Zhu, X, 2021
)
0.62
"The aim of this review was to provide a synopsis for population pharmacokinetic studies of levetiracetam and explore the identified influencing covariates."( Population Pharmacokinetics of Levetiracetam: A Systematic Review.
Jiao, Z; Li, ZR; Wang, CY; Zhu, X, 2021
)
0.62
" Moreover, the pharmacokinetic profiles were compared among neonates, children, and adults."( Population Pharmacokinetics of Levetiracetam: A Systematic Review.
Jiao, Z; Li, ZR; Wang, CY; Zhu, X, 2021
)
0.62
"This study aimed to develop a pharmacokinetic (PK) model of oxcarbazepine (OXC) and analyse the relationship between monohydroxylated derivative (MHD), an active metabolite of OXC, and the adverse events of OXC."( Population pharmacokinetic model development and its relationship with adverse events of oxcarbazepine in adult patients with epilepsy.
Chu, K; Jang, IJ; Jang, Y; Kim, TJ; Lee, S; Lee, SK; Yoon, S; Yu, KS, 2021
)
0.62
" 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 most important pharmacokinetic parameters of the chosen 29 AEDs, mechanism of action and clinical application, as well as their biotransformation, are presented."( 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
"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
" The pharmacokinetic behavior of CBZ was considerably altered when administered concurrently with PG."( 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
)
0.93
" In this context, pharmacokinetic interactions between these drugs may occur."( Pharmacokinetic Interactions Between Antiseizure and Psychiatric Medications.
Franco, V; Zaccara, G, 2023
)
0.91
" Using this fact we aimed to develop an MHD population pharmacokinetic (PPK) model in Chinese adult epileptic patients to facilitate the clinical implementation of model-guided individualised drug therapy."( Population pharmacokinetics of oxcarbazepine 10-monohydroxy derivative in Chinese adult epileptic patients.
Dai, H; Hu, Y; Li, X; Yang, Q; Zhang, X, 2023
)
0.91
" VPA showed a relatively short half-life in both mice and rats, which correlated with a sharp decline in efficacy."( Evaluating the efficacy of prototype antiseizure drugs using a preclinical pharmacokinetic approach.
Johnson, K; Mensah, JA; Metcalf, CS; Reilly, CA; Rower, JE; Wilcox, KS, 2022
)
0.72
" There is currently evidence on its extensive pharmacokinetic variability in real clinical practice."( Extensive pharmacokinetic variability of Levetiracetam. ¿Are doctors aware?
de la Fuente, E; de Toledo, M; de Toledo, MP; Ferreiros-Martinez, R; Lagares, A; Muro, I; Ovejero-Benito, MC; Ramos, C; Sobrado, M; Vieira Campos, A, 2022
)
0.72
"To describe levetiracetam pharmacokinetic variability in patients with epilepsy in real clinical practice."( Extensive pharmacokinetic variability of Levetiracetam. ¿Are doctors aware?
de la Fuente, E; de Toledo, M; de Toledo, MP; Ferreiros-Martinez, R; Lagares, A; Muro, I; Ovejero-Benito, MC; Ramos, C; Sobrado, M; Vieira Campos, A, 2022
)
0.72
"The pharmacokinetic variability of levetiracetam is wider than originally thought."( Extensive pharmacokinetic variability of Levetiracetam. ¿Are doctors aware?
de la Fuente, E; de Toledo, M; de Toledo, MP; Ferreiros-Martinez, R; Lagares, A; Muro, I; Ovejero-Benito, MC; Ramos, C; Sobrado, M; Vieira Campos, A, 2022
)
0.72
" This study aimed to develop a population pharmacokinetic (PPK) model considering the dynamics of enzyme induction and evaluate the effect of CBZ on PER pharmacokinetics."( Population Pharmacokinetic Analysis of Drug-Drug Interactions Between Perampanel and Carbamazepine Using Enzyme Induction Model in Epileptic Patients.
Fujita, Y; Hirota, T; Ieiri, I; Matsunaga, N; Murai, M; Muraki, S; Suetsugu, K; Tsuchiya, Y, 2023
)
1.13
" To support the use of cenobamate monotherapy, this pharmacokinetic (PK)-based simulation analysis evaluated the predicted PK exposure of cenobamate when used as monotherapy versus adjunctive therapy."( Pharmacokinetics of cenobamate as monotherapy compared with adjunctive therapy.
Ferrari, L; Kamin, M; Rosenfeld, WE; Vashi, V, 2023
)
0.91
"A population pharmacokinetic (PopPK) model of cenobamate was developed using pooled human data from eight phase 1 studies in healthy subjects or special populations, and three phase 2 and 3 studies in patients with focal seizures (N = 960)."( Pharmacokinetics of cenobamate as monotherapy compared with adjunctive therapy.
Ferrari, L; Kamin, M; Rosenfeld, WE; Vashi, V, 2023
)
0.91

Compound-Compound Interactions

The study investigated the neuronal protective effect of SXC combined with carbamazepine (CBZ) on epilepsy and cognitive impairment in kainic acid-kindled SD rats.

ExcerptReferenceRelevance
" 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

Bioavailability

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.

ExcerptReferenceRelevance
", 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

Dosage Studied

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.

ExcerptRelevanceReference
" 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 ( 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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (11)

RoleDescription
anticonvulsantA drug used to prevent seizures or reduce their severity.
EC 3.5.1.98 (histone deacetylase) inhibitorAn 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).
mitogenA chemical substance that encourages a cell to commence cell division, triggering mitosis.
glutamate transporter activatorA neurotransmitter transporter modulator that activates glutamate transporters.
antimanic drugAntimanic drugs are agents used to treat bipolar disorders or mania associated with other affective disorders.
analgesicAn 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 analgesicA drug that has principally analgesic, antipyretic and anti-inflammatory actions. Non-narcotic analgesics do not bind to opioid receptors.
environmental contaminantAny minor or unwanted substance introduced into the environment that can have undesired effects.
xenobioticA 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 allergenAny drug which causes the onset of an allergic reaction.
sodium channel blockerAn 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]

Drug Classes (2)

ClassDescription
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]

Pathways (1)

PathwayProteinsCompounds
Carbamazepine Metabolism Pathway718

Protein Targets (41)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Beta-lactamaseEscherichia coli K-12Potency6.30960.044717.8581100.0000AID485341
acetylcholinesteraseHomo sapiens (human)Potency35.40020.002541.796015,848.9004AID1347395
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.23710.006038.004119,952.5996AID1159521
USP1 protein, partialHomo sapiens (human)Potency31.62280.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency29.09290.000811.382244.6684AID686979
AR proteinHomo sapiens (human)Potency5.47280.000221.22318,912.5098AID588515; AID743036; AID743040; AID743042; AID743053; AID743054
thyroid stimulating hormone receptorHomo sapiens (human)Potency6.30960.001318.074339.8107AID926; AID938
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency12.00530.000214.376460.0339AID588532; AID720691; AID720692; AID720719
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency30.48210.003041.611522,387.1992AID1159552
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency51.45180.001530.607315,848.9004AID1224841; AID1224848; AID1224849
pregnane X nuclear receptorHomo sapiens (human)Potency44.84350.005428.02631,258.9301AID1346982; AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency4.36390.000229.305416,493.5996AID743075; AID743080
IDH1Homo sapiens (human)Potency1.03230.005210.865235.4813AID686970
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency0.02240.035520.977089.1251AID504332
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency3.75780.001723.839378.1014AID743083
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency0.44670.010039.53711,122.0200AID588547
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency32.64270.00419.984825.9290AID504444
mitogen-activated protein kinase 1Homo sapiens (human)Potency0.10000.039816.784239.8107AID995
gemininHomo sapiens (human)Potency1.44880.004611.374133.4983AID624296; AID624297
VprHuman immunodeficiency virus 1Potency0.89131.584919.626463.0957AID651644
lamin isoform A-delta10Homo sapiens (human)Potency0.00400.891312.067628.1838AID1487
Cellular tumor antigen p53Homo sapiens (human)Potency0.35480.002319.595674.0614AID651743
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)1,000.00000.40002.75008.6000AID1209456
Bile salt export pumpHomo sapiens (human)IC50 (µMol)711.00000.11007.190310.0000AID1209455; AID1449628; AID1473738
Sodium channel protein type 1 subunit alphaRattus norvegicus (Norway rat)IC50 (µMol)167.00000.01001.14052.9390AID205273
Sodium channel protein type 2 subunit alphaRattus norvegicus (Norway rat)IC50 (µMol)167.00000.00401.14854.7300AID205273
Sodium channel protein type 3 subunit alphaRattus norvegicus (Norway rat)IC50 (µMol)167.00000.00600.86052.9390AID205273
Cytochrome P450 2C9 Homo sapiens (human)IC50 (µMol)50.00000.00002.800510.0000AID1210069
Sodium channel protein type 4 subunit alphaHomo sapiens (human)Ki52.00000.18000.18000.1800AID205290
Cytochrome P450 2J2Homo sapiens (human)IC50 (µMol)50.00000.01202.53129.4700AID1210069
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)104.71300.00091.901410.0000AID576612
Sodium channel protein type 9 subunit alphaHomo sapiens (human)IC50 (µMol)22.00000.00602.77499.0000AID314412
Sodium channel protein type 9 subunit alphaHomo sapiens (human)Ki32.70000.36000.43000.5000AID1227820
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
P2X purinoceptor 4Homo sapiens (human)IC50 (µMol)100.00000.15602.93526.1000AID1064727
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
AlbuminRattus norvegicus (Norway rat)Kd103.00001.47006.53179.3100AID1215123
Major prion proteinHomo sapiens (human)EC50 (µMol)10.00000.30004.900010.0000AID161627
Cytochrome P450 2B6Homo sapiens (human)EC50 (µMol)145.00001.30001.30001.3000AID1210066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (282)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cellular response to copper ionMajor prion proteinHomo sapiens (human)
negative regulation of protein phosphorylationMajor prion proteinHomo sapiens (human)
intracellular copper ion homeostasisMajor prion proteinHomo sapiens (human)
response to oxidative stressMajor prion proteinHomo sapiens (human)
learning or memoryMajor prion proteinHomo sapiens (human)
long-term memoryMajor prion proteinHomo sapiens (human)
negative regulation of protein processingMajor prion proteinHomo sapiens (human)
protein destabilizationMajor prion proteinHomo sapiens (human)
negative regulation of type II interferon productionMajor prion proteinHomo sapiens (human)
negative regulation of interleukin-17 productionMajor prion proteinHomo sapiens (human)
negative regulation of interleukin-2 productionMajor prion proteinHomo sapiens (human)
negative regulation of apoptotic processMajor prion proteinHomo sapiens (human)
negative regulation of DNA-binding transcription factor activityMajor prion proteinHomo sapiens (human)
positive regulation of neuron apoptotic processMajor prion proteinHomo sapiens (human)
negative regulation of activated T cell proliferationMajor prion proteinHomo sapiens (human)
response to cadmium ionMajor prion proteinHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationMajor prion proteinHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationMajor prion proteinHomo sapiens (human)
positive regulation of calcium-mediated signalingMajor prion proteinHomo sapiens (human)
negative regulation of T cell receptor signaling pathwayMajor prion proteinHomo sapiens (human)
protein homooligomerizationMajor prion proteinHomo sapiens (human)
regulation of cell cycleMajor prion proteinHomo sapiens (human)
negative regulation of calcineurin-NFAT signaling cascadeMajor prion proteinHomo sapiens (human)
cellular response to xenobiotic stimulusMajor prion proteinHomo sapiens (human)
positive regulation of protein targeting to membraneMajor prion proteinHomo sapiens (human)
dendritic spine maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of long-term synaptic potentiationMajor prion proteinHomo sapiens (human)
regulation of glutamate receptor signaling pathwayMajor prion proteinHomo sapiens (human)
positive regulation of glutamate receptor signaling pathwayMajor prion proteinHomo sapiens (human)
regulation of potassium ion transmembrane transportMajor prion proteinHomo sapiens (human)
negative regulation of amyloid-beta formationMajor prion proteinHomo sapiens (human)
negative regulation of dendritic spine maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of amyloid precursor protein catabolic processMajor prion proteinHomo sapiens (human)
positive regulation of protein localization to plasma membraneMajor prion proteinHomo sapiens (human)
response to amyloid-betaMajor prion proteinHomo sapiens (human)
cellular response to amyloid-betaMajor prion proteinHomo sapiens (human)
regulation of calcium ion import across plasma membraneMajor prion proteinHomo sapiens (human)
neuron projection maintenanceMajor prion proteinHomo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2C9 Homo sapiens (human)
steroid metabolic processCytochrome P450 2C9 Homo sapiens (human)
cholesterol metabolic processCytochrome P450 2C9 Homo sapiens (human)
estrogen metabolic processCytochrome P450 2C9 Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 2C9 Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
urea metabolic processCytochrome P450 2C9 Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 2C9 Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2C9 Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
amide metabolic processCytochrome P450 2C9 Homo sapiens (human)
icosanoid biosynthetic processCytochrome P450 2C9 Homo sapiens (human)
oxidative demethylationCytochrome P450 2C9 Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 2C9 Homo sapiens (human)
lipid metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
androgen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
estrogen metabolic processUDP-glucuronosyltransferase 2B7Homo sapiens (human)
cellular glucuronidationUDP-glucuronosyltransferase 2B7Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2B6Homo sapiens (human)
steroid metabolic processCytochrome P450 2B6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2B6Homo sapiens (human)
cellular ketone metabolic processCytochrome P450 2B6Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2B6Homo sapiens (human)
sodium ion transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
muscle contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
regulation of skeletal muscle contraction by action potentialSodium channel protein type 4 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
fatty acid metabolic processCytochrome P450 2J2Homo sapiens (human)
icosanoid metabolic processCytochrome P450 2J2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart contractionCytochrome P450 2J2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2J2Homo sapiens (human)
linoleic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
organic acid metabolic processCytochrome P450 2J2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
sodium ion transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
inflammatory responseSodium channel protein type 9 subunit alphaHomo sapiens (human)
circadian rhythmSodium channel protein type 9 subunit alphaHomo sapiens (human)
response to toxic substanceSodium channel protein type 9 subunit alphaHomo sapiens (human)
post-embryonic developmentSodium channel protein type 9 subunit alphaHomo sapiens (human)
sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 9 subunit alphaHomo sapiens (human)
behavioral response to painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of painSodium channel protein type 9 subunit alphaHomo sapiens (human)
detection of mechanical stimulus involved in sensory perceptionSodium channel protein type 9 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 9 subunit alphaHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
regulation of ruffle assemblyP2X purinoceptor 4Homo sapiens (human)
tissue homeostasisP2X purinoceptor 4Homo sapiens (human)
regulation of sodium ion transportP2X purinoceptor 4Homo sapiens (human)
response to ischemiaP2X purinoceptor 4Homo sapiens (human)
signal transductionP2X purinoceptor 4Homo sapiens (human)
regulation of blood pressureP2X purinoceptor 4Homo sapiens (human)
positive regulation of calcium ion transport into cytosolP2X purinoceptor 4Homo sapiens (human)
negative regulation of cardiac muscle hypertrophyP2X purinoceptor 4Homo sapiens (human)
neuronal action potentialP2X purinoceptor 4Homo sapiens (human)
sensory perception of painP2X purinoceptor 4Homo sapiens (human)
calcium-mediated signalingP2X purinoceptor 4Homo sapiens (human)
positive regulation of prostaglandin secretionP2X purinoceptor 4Homo sapiens (human)
response to ATPP2X purinoceptor 4Homo sapiens (human)
monoatomic ion transmembrane transportP2X purinoceptor 4Homo sapiens (human)
response to fluid shear stressP2X purinoceptor 4Homo sapiens (human)
purinergic nucleotide receptor signaling pathwayP2X purinoceptor 4Homo sapiens (human)
endothelial cell activationP2X purinoceptor 4Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationP2X purinoceptor 4Homo sapiens (human)
positive regulation of nitric oxide biosynthetic processP2X purinoceptor 4Homo sapiens (human)
behavioral response to painP2X purinoceptor 4Homo sapiens (human)
response to axon injuryP2X purinoceptor 4Homo sapiens (human)
positive regulation of calcium-mediated signalingP2X purinoceptor 4Homo sapiens (human)
regulation of chemotaxisP2X purinoceptor 4Homo sapiens (human)
sensory perception of touchP2X purinoceptor 4Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionP2X purinoceptor 4Homo sapiens (human)
membrane depolarizationP2X purinoceptor 4Homo sapiens (human)
positive regulation of calcium ion transportP2X purinoceptor 4Homo sapiens (human)
regulation of cardiac muscle contractionP2X purinoceptor 4Homo sapiens (human)
relaxation of cardiac muscleP2X purinoceptor 4Homo sapiens (human)
excitatory postsynaptic potentialP2X purinoceptor 4Homo sapiens (human)
calcium ion transmembrane transportP2X purinoceptor 4Homo sapiens (human)
cellular response to zinc ionP2X purinoceptor 4Homo sapiens (human)
cellular response to ATPP2X purinoceptor 4Homo sapiens (human)
apoptotic signaling pathwayP2X purinoceptor 4Homo sapiens (human)
positive regulation of microglial cell migrationP2X purinoceptor 4Homo sapiens (human)
positive regulation of endothelial cell chemotaxisP2X purinoceptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (113)

Processvia Protein(s)Taxonomy
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
type 8 metabotropic glutamate receptor bindingMajor prion proteinHomo sapiens (human)
amyloid-beta bindingMajor prion proteinHomo sapiens (human)
protease bindingMajor prion proteinHomo sapiens (human)
copper ion bindingMajor prion proteinHomo sapiens (human)
protein bindingMajor prion proteinHomo sapiens (human)
lamin bindingMajor prion proteinHomo sapiens (human)
glycosaminoglycan bindingMajor prion proteinHomo sapiens (human)
microtubule bindingMajor prion proteinHomo sapiens (human)
tubulin bindingMajor prion proteinHomo sapiens (human)
aspartic-type endopeptidase inhibitor activityMajor prion proteinHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingMajor prion proteinHomo sapiens (human)
signaling receptor activityMajor prion proteinHomo sapiens (human)
identical protein bindingMajor prion proteinHomo sapiens (human)
ATP-dependent protein bindingMajor prion proteinHomo sapiens (human)
transmembrane transporter bindingMajor prion proteinHomo sapiens (human)
protein-containing complex bindingMajor prion proteinHomo sapiens (human)
protein-folding chaperone bindingMajor prion proteinHomo sapiens (human)
molecular adaptor activityMajor prion proteinHomo sapiens (human)
molecular function activator activityMajor prion proteinHomo sapiens (human)
molecular condensate scaffold activityMajor prion proteinHomo sapiens (human)
cupric ion bindingMajor prion proteinHomo sapiens (human)
cuprous ion bindingMajor prion proteinHomo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
iron ion bindingCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
(S)-limonene 7-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
caffeine oxidase activityCytochrome P450 2C9 Homo sapiens (human)
(R)-limonene 6-monooxygenase activityCytochrome P450 2C9 Homo sapiens (human)
aromatase activityCytochrome P450 2C9 Homo sapiens (human)
heme bindingCytochrome P450 2C9 Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2C9 Homo sapiens (human)
retinoic acid bindingUDP-glucuronosyltransferase 2B7Homo sapiens (human)
glucuronosyltransferase activityUDP-glucuronosyltransferase 2B7Homo sapiens (human)
monooxygenase activityCytochrome P450 2B6Homo sapiens (human)
iron ion bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-alpha-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
heme bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-beta-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2B6Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2B6Homo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 4 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 4 subunit alphaHomo sapiens (human)
monooxygenase activityCytochrome P450 2J2Homo sapiens (human)
iron ion bindingCytochrome P450 2J2Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 14,15-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 11,12-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
isomerase activityCytochrome P450 2J2Homo sapiens (human)
linoleic acid epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
hydroperoxy icosatetraenoate isomerase activityCytochrome P450 2J2Homo sapiens (human)
arachidonic acid 5,6-epoxygenase activityCytochrome P450 2J2Homo sapiens (human)
heme bindingCytochrome P450 2J2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2J2Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 9 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 9 subunit alphaHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
purinergic nucleotide receptor activityP2X purinoceptor 4Homo sapiens (human)
extracellularly ATP-gated monoatomic cation channel activityP2X purinoceptor 4Homo sapiens (human)
signaling receptor bindingP2X purinoceptor 4Homo sapiens (human)
copper ion bindingP2X purinoceptor 4Homo sapiens (human)
protein bindingP2X purinoceptor 4Homo sapiens (human)
ATP bindingP2X purinoceptor 4Homo sapiens (human)
zinc ion bindingP2X purinoceptor 4Homo sapiens (human)
identical protein bindingP2X purinoceptor 4Homo sapiens (human)
cadherin bindingP2X purinoceptor 4Homo sapiens (human)
ligand-gated calcium channel activityP2X purinoceptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (57)

Processvia Protein(s)Taxonomy
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
dendriteMajor prion proteinHomo sapiens (human)
cytoplasmMajor prion proteinHomo sapiens (human)
endoplasmic reticulumMajor prion proteinHomo sapiens (human)
Golgi apparatusMajor prion proteinHomo sapiens (human)
cytosolMajor prion proteinHomo sapiens (human)
plasma membraneMajor prion proteinHomo sapiens (human)
external side of plasma membraneMajor prion proteinHomo sapiens (human)
cell surfaceMajor prion proteinHomo sapiens (human)
postsynaptic densityMajor prion proteinHomo sapiens (human)
inclusion bodyMajor prion proteinHomo sapiens (human)
extrinsic component of membraneMajor prion proteinHomo sapiens (human)
nuclear membraneMajor prion proteinHomo sapiens (human)
terminal boutonMajor prion proteinHomo sapiens (human)
intracellular membrane-bounded organelleMajor prion proteinHomo sapiens (human)
membrane raftMajor prion proteinHomo sapiens (human)
extracellular exosomeMajor prion proteinHomo sapiens (human)
postsynapseMajor prion proteinHomo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2C9 Homo sapiens (human)
plasma membraneCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
cytoplasmCytochrome P450 2C9 Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2C9 Homo sapiens (human)
endoplasmic reticulum membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
membraneUDP-glucuronosyltransferase 2B7Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2B6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2B6Homo sapiens (human)
cytoplasmCytochrome P450 2B6Homo sapiens (human)
plasma membraneSodium channel protein type 4 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 4 subunit alphaHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2J2Homo sapiens (human)
extracellular exosomeCytochrome P450 2J2Homo sapiens (human)
cytoplasmCytochrome P450 2J2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2J2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membraneSodium channel protein type 9 subunit alphaHomo sapiens (human)
axonSodium channel protein type 9 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 9 subunit alphaHomo sapiens (human)
extracellular regionFrizzled-8Mus musculus (house mouse)
plasma membraneFrizzled-8Mus musculus (house mouse)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
lysosomal membraneP2X purinoceptor 4Homo sapiens (human)
plasma membraneP2X purinoceptor 4Homo sapiens (human)
membraneP2X purinoceptor 4Homo sapiens (human)
cell junctionP2X purinoceptor 4Homo sapiens (human)
neuronal cell bodyP2X purinoceptor 4Homo sapiens (human)
terminal boutonP2X purinoceptor 4Homo sapiens (human)
dendritic spineP2X purinoceptor 4Homo sapiens (human)
cell bodyP2X purinoceptor 4Homo sapiens (human)
perinuclear region of cytoplasmP2X purinoceptor 4Homo sapiens (human)
extracellular exosomeP2X purinoceptor 4Homo sapiens (human)
plasma membraneP2X purinoceptor 4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (1053)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS 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.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The 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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588461High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588459High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, Validation compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588460High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, Validation Compound Set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS 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.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The 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.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1392271Inhibition 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 assay2018Bioorganic & medicinal chemistry, 05-15, Volume: 26, Issue:9
4-Substituted carbamazepine derivatives: Conformational analysis and sodium channel-blocking properties.
AID1335453Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 100 mg/kg, ip after 4 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID113855Effective dose against convulsions induced by clonic pentylenetetrazole after intraperitoneal administration in experiment 21989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID344482Neurotoxicity in CF1 albino mouse after 0.5 hrs by rotarod test2008European 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.
AID1185528Toxicity 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 test2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID603570Antiallodynic 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, ip2011European 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.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1265485Neurotoxicity in po dosed Sprague-Dawley rat after 0.5 hrs by rotarod test2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID481710Anticonvulsant 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 hrs2010European 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.
AID489789Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs2010European 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.
AID477356Neurotoxicity in ip dosed Swiss albino mouse2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current 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.
AID351281Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against maximal electroshock-induced seizures administered before 30 mins of MES induction2009European 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.
AID178169Compound was tested for anticonvulsant activity after Oral Administration into rat by using MES screen test after 2 hr1996Journal 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.
AID433901Toxicity in Kunming mouse assessed as thiosemicarbazide-induced lethality at 50 mg/kg, ip after 2.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID47016Anticonvulsant activity administered intraperitoneally in CF1 mice is the ability to protect the mice from MES(maximal electroshock seizure).1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID590663Neurotoxicity against Swiss mouse after 4 hrs by rotarod ataxia test2011European 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.
AID114383Tested for NMDLA induced seizures and protection against full generalized tonic seizures was recorded; Percentage of protection at 150 mg/kg per os.1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug 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.
AID286866Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1160939Effective permeability of the compound at pH 4 by PAMPA2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID286893Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 2 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID1185532Anticonvulsant activity in Kunming mouse assessed as protection against sc-PTZ-induced tonic seizures 50 mg/kg, sc administered 30 mins before PTZ injection2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID682350Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 300 mg/kg, ip after 0.5 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID351285Anticonvulsant 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 hr2009European 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.
AID226701Protective index was measured as TD50/ED50 in rat on oral administration1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID112536yohimbine 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.1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID1220556Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1755097Solubility in PBS buffer at pH 7.42021Bioorganic & medicinal chemistry letters, 09-01, Volume: 47Antimalarial activity of 2,6-dibenzylidenecyclohexanone derivatives.
AID1229794Inhibition 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 assay2015Journal 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.
AID1676757Solubility in pH 7.4 PBS buffer at 50 to 150 uM incubated for 18 hrs by UV-vis spectrophotometry2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4-
AID1193495Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID1217729Intrinsic 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 formation2011Drug 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.
AID384086Anticonvulsant activity in CF1 albino mouse assessed as prevention of maximal electroshock-induced seizures at 300 mg/kg, ip after 4 hrs2008European 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.
AID481439Absolute bioavailability in human2010Journal 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?
AID496020Plasma protein binding in human after 30 min by ultrafiltration2010Antimicrobial 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.
AID1720877Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for anticonvulsant activity in mouse assessed as protection against 50 mA current-induced seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID352392Anticonvulsant 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 test2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles.
AID679942TP_TRANSPORTER: inhibition of Rhodamine 123 efflux (R123: 1.5 ug/mL, Carbamazepine: 100 uM) in human lymphocytes2001British journal of clinical pharmacology, Apr, Volume: 51, Issue:4
Carbamazepine is not a substrate for P-glycoprotein.
AID256139Number 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 activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID1079936Choleostatic 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]
AID112456Anticonvulsant potency using the maximal electroshock test in mice1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.
AID226543Protective index value is the ratio between TD50 and ED50 values.1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID1720862Anticonvulsant 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 test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID481715Protective index, ratio of TD50 for po dosed mouse to ED50 for maximum electric stimulus-induced seizure in po dosed mouse2010European 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.
AID1215125Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM using four compound cocktail after 5 hrs by TRANSIL assay2011Drug 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.
AID351287Neurotoxicity in C57B/6 mouse assessed as inability to maintain equilibrium on 1-in diameter rod for 1 min after 30 mins by rotarod test2009European 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.
AID114014Effective dose for anticonvulsant activity determined in mice using MES test procedure. (Phase II)1995Journal 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.
AID112460Compound was tested for anticonvulsant potency using the STRY (strychnine) test in mice upon peroral administration1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.
AID684370Anticonvulsant activity in ip dosed Sprague-Dawley albino rat assessed as protection against pilocarpine-induced status epilepticus after 0.5 hrs2012Journal of medicinal chemistry, Mar-22, Volume: 55, Issue:6
Syntheses and evaluation of anticonvulsant activity of novel branched alkyl carbamates.
AID678713Inhibition 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 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID603472Antiallodynic 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, ip2011European 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.
AID178049Inhibition of hind limb tonus was tested by maximal electroshock test (MES) in rat after 4 hr of peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID351011Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against pentylenetetrazole-induced clonic seizure administered 30 mins before pentylenetetrazole challenge measured after 30 mins2009European 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.
AID1809053Oral bioavailability in human2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Discovery of Cyclic Peptidomimetic Ligands Targeting the Extracellular Domain of EGFR.
AID420787Antagonist activity at human 5HT3A receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced inward Na+ current at >= 10 uM2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Molecular properties of psychopharmacological drugs determining non-competitive inhibition of 5-HT3A receptors.
AID231431Protective index, ratio of ED50 ataxia and ED50 MES1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID113857Effective dose against convulsions induced by maximal electroshock (MES) after intraperitoneal administration in experiment 21989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID433896Toxicity in Kunming mouse assessed as isoniazid-induced lethality at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID121852Compound was tested for toxicity after intraperitoneal injection into mice by using neurotoxicity screen test after 0.25 hr1996Journal 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.
AID351282Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against pentylenetetrazole-induced seizures administered before 30 mins of pentylenetetrazole induction2009European 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.
AID1336191Anticonvulsant activity in ip dosed maximal electroshock induced seizure mouse model2017Bioorganic & 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
AID709894Drug metabolism in human liver microsomes assessed as compound turnover at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID418136Toxicity in po dosed rat assessed as minimal muscular or neurological impairment by rotarod paradigm test2009Journal 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.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID24183Distribution coefficient in octanol/water at pH 5.51998Journal 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.
AID624608Specific activity of expressed human recombinant UGT1A42000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID113856Effective dose against convulsions induced by maximal electroshock (MES) after intraperitoneal administration in experiment 11989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID1210069Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS method2013Drug 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.
AID1215122Percentage unbound in solid supported porcine brain membrane vesicles at 5 uM by TRANSIL assay2011Drug 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.
AID1899543Permeability of compound by PAMPA-BBB assay2022European journal of medicinal chemistry, Jan-15, Volume: 228Imidazolylacetophenone oxime-based multifunctional neuroprotective agents: Discovery and structure-activity relationships.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current 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.
AID489288Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs2010Bioorganic & 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.
AID449305Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of subcutaneous pentylenetetrazole-induced seizure after 0.5 hrs2009European 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.
AID693327Protective index, ratio of TD50 for mouse to ED50 for anticonvulsant activity in mouse by subcutaneous pentylenetetrazol-induced seizure test2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID1246319Apparent permeability from basolateral to apical side in human Caco2 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID351010Protective index, ratio of TD50 for neurotoxicity in C57B/6 mouse to ED50 for anticonvulsant activity in C57B/6 mouse2009European 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.
AID286876Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr, ip2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID481698Neurotoxicity against ip dosed mouse by rotarod ataxia test2010European 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.
AID490621Anticonvulsant 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 hrs2010European 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.
AID109721Anticonvulsant activity after intraperitoneal injection into mice by using scPTZ screen test after 4 hr1996Journal 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.
AID1217707Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system2011Drug 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.
AID351015Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against isoniazid-induced tonic seizure administered 30 mins before isoniazide challenge measured after 1 hrs2009European 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.
AID363534Toxicity in pentylenetetrazole-induced seizure C57B/6 mouse model assessed as lethality at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID682318Neurotoxicity in mouse assessed as motor impairment at 30 mg/kg, ip after 4 hrs by rotarod test2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID1160937Aqueous solubility of the compound at pH 42014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID226700Protective index was measured as TD50/ED501992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID114623Evaluated for Bicuculline-induced seizures (anticonvulsant activity) when administered orally in mice.1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1191599Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in clonic seizures after 4 hrs by subcutaneous pentylenetetrazole seizure test2015Bioorganic & 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.
AID286863Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID588220Literature-mined public compounds from Kruhlak et al phospholipidosis modelling dataset2008Toxicology mechanisms and methods, , Volume: 18, Issue:2-3
Development of a phospholipidosis database and predictive quantitative structure-activity relationship (QSAR) models.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID727992Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against maximal-electric shock-induced seizures after 4 hrs2013Bioorganic & 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.
AID256408Minimum dose required for anticonvulsant activity when given i.p., at 0.5 hr in mice upon subcutaneous pentylenetetrazole seizure2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID1517334Inhibition of human LDH5 assessed as remaining activity at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID178294Anticonvulsant activity was measured by maximal electroshock seizure test in rat by po administration1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID1265492Anticonvulsant activity in ip dosed albino Carworth Farms No.1 mouse assessed as protection against maximal electroshock-induced seizures after 0.25 hrs2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID170484Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 0.25 hr; Compound was not screened1996Journal 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.
AID255720Anticonvulsant activity of compound expressed in terms of median effective dose (ED50) produced after ScMet test in mouse by i.p. administration2005Bioorganic & 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.
AID1220555Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1264986Anticonvulsant activity in ip dosed Swiss albino mouse assessed as reduction of maximal electroshock-induced seizure2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents.
AID1360444Binding affinity to human serum albumin assessed as fraction unbound after 4 hrs by LC-MS method2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID1470584Anticonvulsant activity in ip dosed maximal electroshock induced seizure mouse model assessed as suppression of hind limb tonic extension measured at 4 hrs post dose2017European journal of medicinal chemistry, May-26, Volume: 132Recent synthetic and medicinal perspectives of dihydropyrimidinones: A review.
AID1660934Permeability of the compound assessed as drug level in donor plate at 200 uM measured after 5 hrs at pH 7.4 by PAMPA2020Journal 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.
AID1772563Apparent permeability of the compound across apical side to basolateral side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID286862Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID727852Antiepileptic activity in Wistar rat assessed as protection against scSTY-induced seizures at 300 mg/kg, ip measured after 4 hrs2013Bioorganic & 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.
AID1336220Protection index, ratio of TD50 for neurotoxicity in po dosed Sprague-Dawley rat model to ED50 for po dosed pentylenetetrazole induced seizure Sprague-Dawley rat model2017Bioorganic & 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
AID1304304Displacement 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 method2016Bioorganic & 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.
AID123952Locomotor activity in maximal electroshock seizure+ indicates increase at 100 mg/kg1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID231425Protective index was calculated (TD50/ED50) in MES assay in rat after oral administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID231263Protective index was calculated (TD50/ED50) in MES assay in mice after intraperitoneal administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID205274In vitro inhibition of [3H]-BTX-B binding to sodium channels in rat brain synapto-neurosomes1988Journal 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.
AID286883Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 2 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1705558Drug metabolism in rat liver microsomes at 10 uM preincubated with microsomes followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction.
AID1154495Passive transcellular permeability of the compound at pH 7.4 by PAMPA2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Antileishmanial activity of a series of N²,N⁴-disubstituted quinazoline-2,4-diamines.
AID682356Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 100 mg/kg, ip after 4 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID608519Anticonvulsant activity against maximal electric shock-induced seizures in ip dosed Kunming mouse assessed as median effective dose2011European 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.
AID361980Membrane permeability assessed as passive transport after 4 hrs by PAMPA2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries.
AID176420Minimal motor impairment activity by Rotarod test in rat following p.o. administration.1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID467613Volume of distribution at steady state in human2009European 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.
AID588215FDA HLAED, alkaline phosphatase increase2004Current 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.
AID131776Tested for inhibition of 3-mercaptopropanoic acid induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID286878Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs, ip2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID364295Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test2008European 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.
AID489793Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs2010European 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.
AID679256TP_TRANSPORTER: transepithelial transport (basal to apical) in Caco-2 cells2001British journal of clinical pharmacology, Apr, Volume: 51, Issue:4
Carbamazepine is not a substrate for P-glycoprotein.
AID433895Anticonvulsant activity against isoniazid-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID453203Lipophilicity, log D of the compound2010Bioorganic & 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.
AID178048Inhibition of hind limb tonus was tested by maximal electroshock test (MES) in rat after 1 hr of peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID1065323Anticonvulsant activity in po dosed albino rat assessed as protection against maximal electroshock-induced seizures after 1 hr2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID481703Anticonvulsant 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 hrs2010European 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.
AID119692Protective index, ratio of ED50 ataxia and ED50 MES1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID136273Tested for the neurotoxicity in mouse rotarod test was reported 1 hr after po dosing1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines.
AID176423Muscle-relaxant action in vertical screen method.1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants.
AID29811Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1571367Anticonvulsant activity in po dosed Sprague-Dawley rat model of maximal electroshock-induced seizure assessed as suppression of tonic hind limb extension
AID1336211Anticonvulsant activity in po dosed pentylenetetrazole induced seizure Sprague-Dawley rat model assessed as no observable episode of clonic convulsion of at least 5 secs2017Bioorganic & 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
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID481699Protective index, ratio of TD50 for ip dosed mouse to ED50 for maximum electric stimulus-induced seizure in ip dosed mouse2010European 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.
AID545529Toxicity against ip dosed mouse2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives.
AID624612Specific activity of expressed human recombinant UGT1A92000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID709891Stability in human liver microsomes assessed as dioxygenated metabolite formation at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current 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.
AID361979Membrane permeability by PAMPA2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries.
AID1220560Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1335444Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 0.5 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID27575HPLC capacity factor (k)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID363542Anticonvulsant activity in C57B/6 mouse assessed as inhibition of strychnine-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID139326Time of peak effect activity against maximal electroshock induced seizures1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID167920Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 4 hr; Compound was not screened1996Journal 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.
AID135325Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID1720880Neurotoxicity in ip and po injected mouse2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID232413Relative affinity for inactivated and resting human SkM1 expressed in HEK293 cells2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers.
AID693318Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizures2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID540235Phospholipidosis-negative literature compound
AID1473738Inhibition 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 assay2013Toxicological 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.
AID226542Protective index value is the ratio between ED50 and TD501998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID255708Neurotoxicity expressed as median toxic dose (TD50) produced after Rotarod ataxia test in mouse by i.p. administration (range 45.9-135)2005Bioorganic & 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.
AID286884Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 2.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID7812In vitro rate of absorption observed as Caco-2 permeability in humans2002Journal 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.
AID1264982Neurotoxicity in ip dosed Swiss albino mouse assessed as inability of animal to maintain equilibrium on rod after 0.5 hrs by rotarod test2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents.
AID112461Anticonvulsant potency using the intravenous-BIC (bicuculline) test in mice1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.
AID681167TP_TRANSPORTER: Northern blot from LS174T cell2001The Journal of biological chemistry, May-04, Volume: 276, Issue:18
Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin.
AID109725Compound was tested for toxicity after intraperitoneal injection into mice by using toxicity screen test after 4 hr1996Journal 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.
AID394946Neurotoxicity 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 test2009European 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.
AID382366Anticonvulsant activity in ip dosed mouse assessed as inhibition of maximal electroshock-induced seizures after 0.5 hrs2008European 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.
AID682345Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 4 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID1720883Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for anticonvulsant activity in mouse assessed as protection against current-induced seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID1720885Neurotoxicity in KunMing mouse after 30 mins by rotarod test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID491236Permeability in buffer of pH 7.4 by PAMPA2010Bioorganic & medicinal chemistry, Jul-01, Volume: 18, Issue:13
Amide conjugates of ketoprofen and indole as inhibitors of Gli1-mediated transcription in the Hedgehog pathway.
AID129975Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse maximal electroshock seizures (MES) at time of peak effect after ip administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID727991Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against scPTZ-induced seizures after 0.5 hrs2013Bioorganic & 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.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID114017Effective dose for anticonvulsant activity determined in mice using subcutaneous Met test procedure. (Phase II); Potentiates1995Journal 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.
AID15711Calculated partition coefficient (clogP)1998Journal 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.
AID212211Toxicity using neurological impairment measured by rotarod test in mice1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.
AID608533Anticonvulsant activity in Kunming mouse assessed as inhibition of bicuculline-induced death at 30 mg/kg, ip after 0.5 hrs2011European 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.
AID1720889Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for anticonvulsant activity in mouse assessed as protection against pentylenetetrazole-induced seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID1064727Antagonist 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 assay2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Carbamazepine derivatives with P2X4 receptor-blocking activity.
AID462612Permeability across artificial membrane assessed as compound transport at 200 uM after 4 hrs by PAMPA using HPLC/MS method2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID1895157Permeability in PBS buffer measured after 18 hrs by PAMPA based LC-MS analysis2021Journal 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.
AID477728Protective index, ratio of TD50 for neurotoxicity in Swiss albino mouse to ED50 for inhibition of PTZ-induced motor impairment Swiss albino mouse2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.
AID666675Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against maximal electroshock-induced seizures2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives.
AID1209393AUC(0 to 7 hrs) in Sprague-Dawley rat cerebrospinal fluid at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID134732Median lethal dose was measured after 24 hr1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID1517278Neurotoxicity against ip dosed Kunming mouse assessed as time remained in rod measured at 0.5 hrs by rotarod test2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID286868Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1742412Neurotoxicity in ip dosed Kunming mouse measured after 30 mins by rotarod test
AID286895Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID590662Anticonvulsant activity in ip dosed Swiss mouse assessed as protection against maximal electroshock-induced seizures after 30 mins2011European 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.
AID1517274Anticonvulsant activity in ip dosed Kunming mouse assessed as MES-induced hind limb extension administered 0.5 hrs before MES stimulation2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1335459Neurotoxicity in Swiss albino mouse at 100 mg/kg, ip after 4 hrs by rotarod test2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID1193496Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID608433Anticonvulsant activity in Kunming mouse assessed as inhibition of isoniazid-induced clonic seizures at 50 mg/kg, ip after 1 hrs2011European 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.
AID27580Partition coefficient (logP)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID608531Anticonvulsant activity in Kunming mouse assessed as inhibition of bicuculline-induced clonic seizures at 30 mg/kg, ip after 0.5 hrs2011European 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.
AID490626Anticonvulsant activity in mouse assessed as bicuculline-induced tonic seizures at 30 mg/kg, ip administered 30 mins before bicuculline challenge measured after 0.5 hrs2010European 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.
AID608431Anticonvulsant activity in Kunming mouse assessed as inhibition of isoniazid-induced death at 50 mg/kg, ip after 1 hrs2011European 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.
AID1335445Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 0.5 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID394935Anticonvulsant 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 test2009European 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.
AID217796In vitro inhibition of Voltage-gated sodium channel by the displacement of [3H]batrachotoxin A 20-alpha-benzoate in rat brain cerebral cortex synaptoneurosomes1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.
AID489277Anticonvulsant activity against subcutaneous strychnine-induced seizures in Wistar rat at 300 mg/kg, ip after 4 hrs2010Bioorganic & 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.
AID217926Inhibition of [3H]BTX binding to cardiac voltage-gated sodium channel2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID130890Inhibition of hind limb tonus was tested by maximal electroshock test (MES) in mouse after 1 hr of peroral administration of compound1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID693326Protective index, ratio of TD50 for mouse to ED50 for anticonvulsant activity in mouse by maximal electroshock-seizure test2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID1636357Drug 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 NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1544808Anticonvulsant 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 inducti2019Bioorganic & 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.
AID212543The compound was tested for the toxic dose on oral administration1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID608532Anticonvulsant activity in Kunming mouse assessed as inhibition of bicuculline-induced tonic seizures at 30 mg/kg, ip after 0.5 hrs2011European 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.
AID608436Anticonvulsant activity in Kunming mouse assessed as inhibition of subcutaneous pentylenetetrazol-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs2011European 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.
AID481441Aqueous diffusivity at 37C2010Journal 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?
AID1215124Binding affinity to Wistar rat brain lipid assessed as percentage unbound by TRANSIL assay2011Drug 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.
AID474786Membrane permeability at 10 uM at pH 7.4 by PAMPA method2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones.
AID1210066Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method2013Drug 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.
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The 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.
AID608518Neurotoxicity in ip dosed Kunming mouse by rotarod test2011European 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.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID1473741Inhibition 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 assay2013Toxicological 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.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID344483Neurotoxicity in CF1 albino mouse after 4 hrs by rotarod test2008European 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.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current 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.
AID1193492Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID481701Ratio of HD50 for hypnotic activity to EC50 for inhibition of maximum electric stimulus-induced seizure in mouse2010European 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.
AID1720863Neurotoxicity in ip injected albino mouse2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID1753899Passive 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 analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.
AID433890Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID608427Anticonvulsant activity in Kunming mouse assessed as inhibition of thiosemicarbazide-induced clonic seizures at 30 mg/kg, ip after 2.5 hrs2011European 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.
AID481704Anticonvulsant 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 hrs2010European 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.
AID1194717Solubility in pH 7.4 buffer after 18 hrs by UV spectroscopy based microSol assay2015Bioorganic & medicinal chemistry letters, May-01, Volume: 25, Issue:9
Improving both aqueous solubility and anti-cancer activity by assessing progressive lead optimization libraries.
AID109717Anticonvulsant activity after intraperitoneal injection into mice by using MES screen test after 0.25 hr1996Journal 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.
AID693313Anticonvulsant activity in ip dosed mouse assessed as compound concentration causing protection against subcutaneous pentylenetetrazol-induced seizures in half or more test animals after 4 hrs2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID195317Compound was tested for anticonvulsant activity against MES-induced seizures in rat1999Journal 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.
AID433892Toxicity in Kunming mouse assessed as subcutaneous pentylenetetrazole-induced lethality at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID678715Inhibition 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 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1217728Intrinsic clearance for reactive metabolites formation per mg of protein based on cytochrome P450 (unknown origin) inactivation rate by TDI assay2011Drug 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.
AID1251236Anticonvulsant activity in ip-dosed mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizure2015Bioorganic & 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.
AID223434Effective dose was measured in mouse by maximal electroshock method by ip administration1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and CLOGP correlation of imidooxy anticonvulsants.
AID128992Anticonvulsant activity in mice(induced by maximal electroshock )after 0.25 hr of administration, for Phase-II screening1988Journal 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.
AID194784Percent inhibition of 22Na+ uptake by voltage sensitive sodium channel of rat cortical synaptosomes at 300 uM1999Journal 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.
AID682342Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 0.5 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID177085Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in rat maximal metrazole seizures (MMS) after peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID1265488Neurotoxicity in ip dosed albino Carworth Farms No.1 mouse after 0.25 hrs by rotarod test2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID178031Effective dose for anticonvulsant activity determined in rats using subcutaneous Met test procedure. (Phase VIA); No protection1995Journal 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.
AID1605379Binding 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 assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID590661Anticonvulsant activity in ip dosed Swiss mouse assessed as protection against maximal electroshock-induced seizures administered 30 mins before electroshock challenge measured after 30 mins2011European 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.
AID481716Neurotoxicity against po dosed mouse by rotarod ataxia test2010European 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.
AID490617Anticonvulsant activity in mouse assessed as isoniazid-induced tonic seizures at 30 mg/kg, ip administered 30 mins before isoniazid challenge measured after 1 hr2010European 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.
AID709904Drug 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 method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID314412Blockade of human Nav1.7 channel expressed in HEK293 cells by FRET assay2008Bioorganic & medicinal chemistry letters, Mar-01, Volume: 18, Issue:5
Imidazopyridines: a novel class of hNav1.7 channel blockers.
AID1185525Toxicity 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 test2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1571343Neurotoxicity in ip dosed CF-1 mouse by rotarod test
AID489795Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause impair in motor coordination after 0.5 hrs by rotarod test2010European 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.
AID590664Protective index, ratio of TD50 for Swiss mouse to ED50 for Swiss mouse by maximal electroshock-induced seizures test2011European 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.
AID628633Neurotoxicity in ip dosed CF1 albino mouse assessed as minimum dose required to cause motor impairment after 4 hrs by rotarod test2011European 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.
AID1636440Drug 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 NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1449628Inhibition 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 method2012Drug 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.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal 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.
AID7974Metabolic stability observed at 30 min after administration in human liver microsomes2002Journal 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.
AID1065338Neurotoxicity in ip dosed albino mouse after 0.5 hrs by rotorod test2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID608426Anticonvulsant activity in Kunming mouse assessed as inhibition of thiosemicarbazide-induced tonic seizures at 30 mg/kg, ip after 2.5 hrs2011European 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.
AID545526Protective index, ratio of TD50 for mouse to ED50 for inhibition of subcutaneous pentylenetetrazole-induced seizure in mouse2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives.
AID28924Effective permeability (Pe) across a hexadecane membrane (pH 6.8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID132473The compound was tested for anticonvulsant activity against (subcutaneous administered) bicuculline induced seizures after intraperitoneal administration; Protected at 100 mg/ kg1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal 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?
AID128999Anticonvulsant activity in mice, (induced by subcutaneous administration of Metrazol.) after 0.25 hr of administration, for Phase-II screening; Inactive1988Journal 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.
AID1742400Anticonvulsant activity in Kunming mouse assessed as reduction in MES-induced seizure at 30 mg/kg, ip measured after 30 mins
AID637074Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizure2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones.
AID1336218Protection 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 model2017Bioorganic & 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
AID128129Ability to block seizures induced by bicuculline after intraperitoneal administration; NA indicates not active1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents.
AID1195112Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse assessed as time to peak effect after 2 hrs by subcutaneous pentylenetetrazole test2015Bioorganic & 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.
AID1173470Anticonvulsant activity against ip dosed CF1 albino mouse seizure model after 4 hrs by 6 Hz psychomotor seizure test2014Bioorganic & 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.
AID727850Neurotoxicity against ip dosed Swiss albino mouse after 0.5 hrs by rotarod test2013Bioorganic & 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.
AID286897Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 1.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1304303Displacement 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 method2016Bioorganic & 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.
AID496828Antimicrobial activity against Leishmania donovani2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1335457Neurotoxicity in Swiss albino mouse at 300 mg/kg, ip after 0.5 hrs by rotarod test2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID433888Neurotoxicity in ip dosed Kunming mouse by rotarod test2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID1195111Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse assessed as time to peak effect by maximal electroshock test2015Bioorganic & 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.
AID286880Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID196513t max for anticonvulsant activity was tested in rats intraperitoneally1999Journal 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.
AID114622Evaluated for Bicuculline-induced lethality (anticonvulsant activity) when administered orally in mice.1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug 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.
AID255434Minimum dose required for anticonvulsant activity when given i.p., at 0.5 hr in mice upon neurotoxicity seizure using rotarod test2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID128174Anticonvulsant activity in mouse maximal electroshock seizure test following i.p. administration.1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents.
AID53026Compound was evaluated for effective dose by maximal electroshock test after intraperitoneal administration of the compound.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis and anticonvulsant activity of imidooxy derivatives.
AID1519638Neurotoxicity in ip dosed CF-1 mouse assessed as reduction in equilibrium measured after 30 mins by rotarod test
AID1742405Neurotoxicity in Kunming mouse at 30 mg/kg, ip measured after 30 mins by rotarod test
AID1605380Binding 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 assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID1229792Inhibition 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 assay2015Journal 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.
AID1519637Anticonvulsant activity in ip dosed CF-1 mouse assessed as reduction in ScPTZ-induced seizure administered before 30 mins of ScPTZ stimulation
AID496817Antimicrobial activity against Trypanosoma cruzi2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID576612Inhibition of human ERG2011European 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.
AID361982Membrane permeability assessed as passive transport after 4 hrs by PAMPA in presence of 20% 1-propanol2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries.
AID363527Anticonvulsant activity in ip dosed C57B/6 mouse assessed as inhibition of maximal electroshock-induced seizures2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID221081Therapeutic dosage was measured by ip administration in mice1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and CLOGP correlation of imidooxy anticonvulsants.
AID496825Antimicrobial activity against Leishmania mexicana2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1336192Anticonvulsant activity in ip dosed pentylenetetrazole induced seizure mouse model2017Bioorganic & 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
AID699540Inhibition 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 counting2012Journal 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.
AID177579Ability to suppress PTZ (pentylenetetrazole) induced clonic convulsions seizures in male Wistar rats1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants.
AID490622Anticonvulsant activity in mouse assessed as thiosemicarbazide-induced clonic seizures at 30 mg/kg, ip administered 30 mins before thiosemicarbazide challenge measured after 2.5 hrs2010European 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.
AID136272Rotarod toxicity test for the compound in Phase-II screening was determined1988Journal 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.
AID679895TP_TRANSPORTER: inhibition of cyclosporin A transcellular transport by carbamazapine 224 uM in MDR1-expressing LLC-PK1 cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID1220558Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID286885Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID632994Neurotoxicity in po dosed rat assessed as neurological deficit by rotarod test2011Bioorganic & 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.
AID1065213Permeability coefficient, log Pe of the compound at pH 7.4 by PAMPA2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Development of novel Vitamin D Receptor-Coactivator Inhibitors.
AID351284Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against thiosemicarbazide-induced seizures administered before 30 mins of thiosemicarbazide induction measured after 1 hr2009European 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.
AID131218Maximal metrazole seizures was determined for the inhibition of hind limb tonus in mouse 1 hr after po dosing1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines.
AID1215121Fraction unbound in Wistar rat brain homogenate at 5 uM after 5 hrs by equilibrium dialysis method2011Drug 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.
AID679123TP_TRANSPORTER: transcellular transport in mdr1a-expressing LLC-PK1 cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID43581Inhibition of beta-lactamase at 100 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1709683Anticonvulsant activity in mouse by measuring free brain concentration2021ACS medicinal chemistry letters, Apr-08, Volume: 12, Issue:4
Discovery of the First Orally Available, Selective K
AID1335451Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 300 mg/kg, ip after 0.5 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID382370Neurotoxicity in ip dosed mouse after 0.5 hrs by rotarod test2008European 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.
AID1519674Chromatographic hydrophobicity index of compound at 250 uM at pH 7.4 by HPLC analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.
AID19463Partition coefficient (logP)1999Journal of medicinal chemistry, May-06, Volume: 42, Issue:9
Comparative molecular field analysis of hydantoin binding to the neuronal voltage-dependent sodium channel.
AID1065320Protective index, ratio of TD50 for neurotoxicity to ED50 for protection against maximal electroshock-induced seizure in albino rat after 1 hr2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID286881Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 1 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1720860Anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure measured after 30 mins2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID490612Protective index, ratio of TD50 for mouse by rotarod test to ED50 for mouse by MES test2010European 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.
AID1193500Thermodynamic equilibrium solubility, log S of the compound2015Bioorganic & 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.
AID256412Minimum dose required for anticonvulsant activity when given i.p., at 2 hr in mice upon subcutaneous strychnine seizure; Absence of activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID1544804Neurotoxicity in ip dosed albino mouse assessed as motor impairment measured at 4 hrs by rotarod test2019Bioorganic & 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.
AID677694Permeability of the compound at pH 7.4 by PAMPA2012Journal 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.
AID624606Specific activity of expressed human recombinant UGT1A12000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1336209Anticonvulsant activity in po dosed maximal electroshock induced seizure Sprague-Dawley rat model assessed as suppression in hindlimb tonic extension2017Bioorganic & 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
AID666678Protective index, ratio of TD50 for neurotoxicity in Kunming mouse to ED50 for protection against MES-induced seizures in Kunming mouse2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives.
AID210595Ratio of TD50/ED50; TI indicates Therapeutic index1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents.
AID545525Protective index, ratio of TD50 for mouse to ED50 for inhibition of maximal electroshock-induced seizure in mouse2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives.
AID286898Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 2 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1336195Protection index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for ip dosed pentylenetetrazole induced seizure mouse model2017Bioorganic & 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
AID363546Toxicity in strychnine-induced seizure C57B/6 mouse model assessed as lethality at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID1217711Metabolic activation in human liver microsomes assessed as [3H]GSH adduct formation rate measured per mg of protein at 100 uM by [3H]GSH trapping assay2011Drug 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.
AID490615Anticonvulsant activity in mouse assessed as pentylenetetrazole-induced death at 30 mg/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 0.5 hrs2010European 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.
AID352566Anticonvulsant 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 test2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles.
AID305067Anticonvulsant activity against pentylenetetrazole-induced seizures in Albino mouse at 300 mg/kg, ip after 4 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain.
AID314682Anticonvulsant activity in C57BL6J mouse assessed as prevention of shock-induced tonic-clonic seizures at 3 mg/kg, po after 30 mins2008Bioorganic & medicinal chemistry letters, Mar-15, Volume: 18, Issue:6
3-Amino-1,5-benzodiazepinones: potent, state-dependent sodium channel blockers with anti-epileptic activity.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID727853Antiepileptic activity in Wistar rat assessed as protection against scSTY-induced seizures at 300 mg/kg, ip measured after 0.5 hrs2013Bioorganic & 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.
AID1160933Aqueous solubility of the compound at pH 7.42014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID481711Anticonvulsant 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 hrs2010European 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.
AID106806Inhibition of malate dehydrogenase (MDH) at 400 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID344488Hepatotoxicity in Sprague-Dawley rat assessed as presence of normal hepatic parenchyma with portal triad and central vein by histopathological study2008European 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.
AID496832Antimicrobial activity against Trypanosoma brucei rhodesiense2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1227822Kinetic solubility of the compound at pH 1.22015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Dibenzazepines and dibenzoxazepines as sodium channel blockers.
AID1623669Apparent permeability of compound form apical to basolateral side in human Caco2 cells2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID637073Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against maximal electroshock-induced seizure2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones.
AID212546Toxic dose determined in rats using MES test procedure. (Phase VIA)1995Journal 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.
AID361981Membrane permeability by PAMPA in presence of 20% 1-propanol2008Journal of medicinal chemistry, Aug-28, Volume: 51, Issue:16
Toward an optimal blood-brain barrier shuttle by synthesis and evaluation of peptide libraries.
AID1079938Chronic 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]
AID418134Anticonvulsant activity in po dosed rat assessed as protection against maximal electroshock-induced seizure2009Journal 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.
AID253080Inhibition of native TTX-R sodium currents in acutely dissociated rat dorsal root ganglion (DRG)2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors.
AID496831Antimicrobial activity against Cryptosporidium parvum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID190113In vivo toxic dose in rotarod assay2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID253081Inhibition of native TTX-S sodium currents in acutely dissociated rat dorsal root ganglion (DRG)2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors.
AID205291Affinity for resting human SkM1 sodium channel expressed in HEK293 cells2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers.
AID363544Anticonvulsant activity in C57B/6 mouse assessed as inhibition of strychnine-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID226526Protective index is the ratio between TD50 and ED50 values1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID1220554Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1209401AUC(0 to infinity) in Sprague-Dawley rat cerebrospinal fluid at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID489791Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs2010European 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.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal 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).
AID490614Anticonvulsant activity in mouse assessed as pentylenetetrazole-induced tonic seizures at 30 mg/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 0.5 hrs2010European 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.
AID47029Time of peak neurotoxic effect in CF1 mice1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID1246318Apparent permeability from apical to basolateral side in human Caco2 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID131995Median hypnotic dose by loss of righting reflex1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID28234% absorbed in human GI-tract2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID255468Minimum dose required for anticonvulsant activity when given i.p., at 0.5 hr in mice upon maximal electroshock seizure2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID490618Anticonvulsant activity in mouse assessed as isoniazid-induced death at 30 mg/kg, ip administered 30 mins before isoniazid challenge measured after 1 hr2010European 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.
AID114817Sedative properties by the rotarod test1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1217712Time dependent inhibition of CYP2C8 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID637076Protective index, ratio of TD50 for ip dosed Kunming mouse to ED50 for ip dosed Kunming mouse by subcutaneous pentylenetetrazole induced seizure test2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones.
AID1742413Protection index, ratio of TD50 for neurotoxicity in ip dosed Kunming mouse to ED50 for anticonvulsant activity in ip dosed MES-induced Kunming mouse
AID481702Anticonvulsant 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 hrs2010European 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.
AID131932Tested for inhibition of strychnine-induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID29421Partition coefficient (logP) (HPLC)2000Journal of medicinal chemistry, Jul-27, Volume: 43, Issue:15
ElogPoct: a tool for lipophilicity determination in drug discovery.
AID608430Anticonvulsant activity in Kunming mouse assessed as inhibition of 3-mercaptopropionic acid-induced clonic seizures at 30 mg/kg, ip after 0.5 hrs2011European 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.
AID1810294Aqueous solubility of compound at pH 2.42021Journal 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
AID364290Anticonvulsant activity in ip dosed mouse after 0.5 hrs by scPTZ test2008European 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.
AID727993Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against maximal-electric shock-induced seizures after 0.5 hrs2013Bioorganic & 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.
AID344480Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 0.5 hrs by scPTZ test2008European 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.
AID305066Anticonvulsant activity against pentylenetetrazole-induced seizures in Albino mouse at 100 mg/kg, ip after 0.5 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain.
AID179593In vitro inhibition of [3H]GABA uptake in rat Hippocampal slices.1992Journal 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.
AID1753897Passive 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 analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.
AID352568Neurotoxicity 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 test2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles.
AID1215127Ratio 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 method2011Drug 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.
AID1264988Protective 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 seizure2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents.
AID1473740Inhibition 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 assay2013Toxicological 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.
AID682320Neurotoxicity in mouse assessed as motor impairment at 300 mg/kg, ip after 4 hrs by rotarod test2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID432063Apparent permeability at pH 7.4 after 24 hrs by PAMPA method2009European 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.
AID1261691Protein binding to human serum albumin at 0.5 to 1.5 mg/ml by HPLC method2015Journal 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.
AID590665Protective index, ratio of TD50 for Swiss mouse to ED50 for Swiss mouse by subcutaneous pentylenetetrazol-induced seizure test2011European 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.
AID114575Tested for the abolition of the hand leg tonic extensor component of the seizure induced by a 0.96 mg/kg sc injection of strychnine1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID624640Drug glucuronidation reaction catalyzed by human recombinant UGT2B72005Pharmacology & therapeutics, Apr, Volume: 106, Issue:1
UDP-glucuronosyltransferases and clinical drug-drug interactions.
AID490624Anticonvulsant activity in mouse assessed as thiosemicarbazide-induced death at 30 mg/kg, ip administered 30 mins before thiosemicarbazide challenge measured after 2.5 hrs2010European 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.
AID1193498Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID1065322Neurotoxicity in po dosed albino rat after 1 hr2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID1211297Drug recovery in plasma (unknown origin)2011Drug 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.
AID490613Anticonvulsant activity in mouse assessed as pentylenetetrazole-induced clonic seizures at 30 mg/kg, ip administered 30 mins before pentylenetetrazole challenge measured after 0.5 hrs2010European 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.
AID1229793Inhibition 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 assay2015Journal 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.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID226508Protection index = TD50/ED501996Journal 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.
AID1195116Protective index, ratio of neurotoxic TD50 in Albino Swiss CD1 mouse by rotarod test to anticonvulsant ED50 in Albino Swiss CD1 mouse by maximal electroshock test2015Bioorganic & 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.
AID727851Neurotoxicity against ip dosed Swiss albino mouse after 4 hrs by rotarod test2013Bioorganic & 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.
AID112455Compound was tested for anticonvulsant potency using the 3-MPA (3-mercaptopropionic acid) test in mice upon peroral administration1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.
AID682316Neurotoxicity in mouse assessed as motor impairment at 100 mg/kg, ip after 0.5 hrs by rotarod test2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID445819CNS 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)2010European 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.
AID129974Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse against maximal electroshock seizures (MES) after peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID1065321Anticonvulsant activity in po dosed albino rat assessed as protection against pentylenetetrazole-induced seizure after 1 hr2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID28925Highest effective permeability across hexadecane membrane (pH 4-8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID1742410Anticonvulsant activity in ip dosed Kunming mouse assessed as reduction in MES-induced seizure measured after 30 mins
AID190132The cytotoxicity after intraperitoneal administration in rat1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID1335454Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 300 mg/kg, ip after 4 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID693319Anticonvulsant 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 hrs2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID433900Anticonvulsant activity against thiosemicarbazide-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 2.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID132652The effective dose of compound was tested against subcutaneous administered Metrazol induced seizures after intraperitoneal administration; Not effective1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID22951Time of peak effect (TPE) for toxicity1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis and anticonvulsant activity of imidooxy derivatives.
AID286888Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 2 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1517275Anticonvulsant activity in ip dosed Kunming mouse assessed as reduction in ScPTZ-induced seizure administered 0.5 hrs before ScPTZ stimulation2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1217727Intrinsic 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 assay2011Drug 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.
AID588214FDA HLAED, liver enzyme composite activity2004Current 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.
AID539464Solubility of the compound in 0.1 M phosphate buffer at 600 uM at pH 7.4 after 24 hrs by LC/MS/MS analysis2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID489797Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause impair in motor coordination after 4 hrs by rotarod test2010European 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.
AID226523Protective index (rat) was from the ratio of plasma concentration at which side effects occur by plasma concentration at which anticonvulsant activity occur.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID481446Effective permeability across human jejunum2010Journal 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?
AID190459Anticonvulsant activity in corneal kindled rats was determined when 10 mg/kg was administered orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID344481Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 4 hrs by scPTZ test2008European 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.
AID1220557Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1660933Permeability of the compound assessed as drug level in acceptor plate at 200 uM measured after 5 hrs at pH 7.4 by PAMPA2020Journal 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.
AID28679Partition coefficient (logD6.8)2001Journal of medicinal chemistry, Mar-15, Volume: 44, Issue:6
High-throughput permeability pH profile and high-throughput alkane/water log P with artificial membranes.
AID47026Time of peak anticonvulsant effect in CF1 mice1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID129293Antimaximal electroshock seizure activity was determined in mice when administered perorally1988Journal 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.
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID40039Antagonist activity to generalized seizures Photically induced seizures in senegalese Papio papio baboons1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID121850Compound was tested for rotarod test in mice and TD50 value at which 50% of trained animals fall off rotarod1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID394939Anticonvulsant 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 test2009European 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.
AID462615Apparent permeability in BBMEC assessed as compound transport after 2 hrs2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID161627Half maximal inhibition of Prion protein PrPsc formation was assayed in ScN2a cells2003Journal of medicinal chemistry, Aug-14, Volume: 46, Issue:17
Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein.
AID418132Anticonvulsant activity in ip dosed mouse assessed as protection against subcutaneous metrazole-induced seizure2009Journal 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.
AID194783Percent inhibition of 22Na+ uptake by voltage sensitive sodium channel of rat cortical synaptosomes at 30 uM1999Journal 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.
AID1335452Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 30 mg/kg, ip after 4 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID449310Antidepressant activity against Wistar rat assessed as increase in immobility time at 30 mg/kg, ip after 60 mins by forced swim pool method2009European 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.
AID490616Anticonvulsant activity in mouse assessed as isoniazid-induced clonic seizures at 30 mg/kg, ip administered 30 mins before isoniazid challenge measured after 1 hr2010European 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.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID384082Anticonvulsant activity in ip dosed CF1 albino mouse assessed as prevention of maximal electroshock-induced seizures after 0.5 hrs2008European 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.
AID628728Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against subcutaneous pentylenetetrazole-induced after 4 hrs2011European 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.
AID351286Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against strychnine-induced seizures administered before 30 mins of strychnine induction measured for 30 mins2009European 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.
AID1217710Covalent binding in human liver microsomes measured per mg of protein using radiolabelled compound at 10 uM after 1 hr incubation by liquid scintillation counting2011Drug 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.
AID170633Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 2 hr; Compound was not screened1996Journal 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.
AID1079931Moderate 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]
AID394934Anticonvulsant 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 test2009European 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.
AID1720892Neurotoxicity in KunMing mouse by rotarod test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID633209Blockade 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 control2011Bioorganic & 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.
AID190107Compound was tested for toxicity after oral administration in rat by using neurotoxicity screen test after 0.5 hr1996Journal 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.
AID693322Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID196514t max was for the anticonvulsant effect was tested in rats administered by gastric tube; t max1999Journal 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.
AID1193499Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID286890Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID433891Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID1544805Neurotoxicity in ip dosed albino mouse assessed as motor impairment measured at 0.5 hrs by rotarod test2019Bioorganic & 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.
AID489787Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs2010European 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.
AID197266In vivo anticonvulsant activity to prevent seizures from maximum electroshock (MES) in rat hippocampal slices2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID496824Antimicrobial activity against Toxoplasma gondii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID305070Neurotoxicity in Albino mouse at 300 mg/kg, ip after 4 hrs by rotarod test2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain.
AID366586Protective index, ratio of TD50 for mouse by rotarod test to ED50 for mouse by MES test2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Anticonvulsant activity of some xanthone derivatives.
AID1519639Protective index, ratio of TD50 for neurotoxicity in ip dosed CF-1 mouse to ED50 for anticonvulsant activity in ip dosed Kunming mouse
AID132653The effective dose of compound was tested against subcutaneous administered Metrazol induced seizures in mice1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID132645The effective dose of compound was tested against maximal electroshock induced seizures after intraperitoneal administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID481709Anticonvulsant 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 hrs2010European 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.
AID24184Distribution coefficient in octanol/water at pH 6.51998Journal 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.
AID1304302Displacement 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 method2016Bioorganic & 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.
AID1772565Efflux ratio of apparent permeability in human Caco-2 cells2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID19689Partition coefficient (logP)1996Journal 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.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID286892Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 1.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1517280Protective 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 seiz2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID481700Sedative-hypnotic activity in mouse assessed as reduction in righting reflex2010European 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.
AID490619Anticonvulsant 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 hrs2010European 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.
AID1720886Protective 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 seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID1079933Acute 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
AID1185526Protective index, ratio of intraperitoneal neurotoxic TD50 against Kunming mouse by rotarod test to intraperitoneal anticonvulsant ED50 in Kunming mouse by MES test2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID180530The compound was tested for the effective oral dose to inhibit 50% of the anticonvulsant in rats.1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID131925Tested for inhibition of pentylenetetrazole induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID433897Anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in Kunming mouse assessed as tonic seizures of at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID222384Protective index (TD50/ED50) value in MES test in mice1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and CLOGP correlation of imidooxy anticonvulsants.
AID363529Protective index, ratio of TD50 for C57B/6 mouse by rotarod test to ED50 for C57BL/6 mouse by MES test2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID666676Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against subcutaneous pentylenetetrazol-induced clonic seizures2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives.
AID496823Antimicrobial activity against Trichomonas vaginalis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID249395Ratio between Kr to Ki2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors.
AID682343Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 0.5 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1217713Time dependent inhibition of CYP3A4 (unknown origin) at 10 uM by LC/MS system2011Drug 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.
AID1195115Neurological toxicity in intraperitoneally dosed Albino Swiss CD1 mouse by rotarod test2015Bioorganic & 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.
AID1269481Displacement of [3H]Batrachotoxinin from sodium channel site 2 in rat cerebral cortex at 100 uM after 60 mins by scintillation counting method2016Bioorganic & 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.
AID603563Antiallodynic 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, ip2011European 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.
AID131914Tested for inhibition of maximal electroshock -induced seizures in mice; Value ranges from 13-251990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID114873Effective dose required to inhibit ataxia after intraperitoneal administration in experiment 11989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID1220559Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID682315Neurotoxicity in mouse assessed as motor impairment at 30 mg/kg, ip after 0.5 hrs by rotarod test2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID1058304Anticonvulsant activity in ip dosed Sprague-Dawley rat hippocampal kindling model assessed as suppression of seizure activity treated 15 for mins post suprathreshold-stimulation2013Journal 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).
AID608429Anticonvulsant activity in Kunming mouse assessed as inhibition of 3-mercaptopropionic acid-induced tonic seizures at 30 mg/kg, ip after 0.5 hrs2011European 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.
AID1623668Permeability of compound at pH 7.4 by PAMPA2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID490627Anticonvulsant activity in mouse assessed as bicuculline-induced death at 30 mg/kg, ip administered 30 mins before bicuculline challenge measured after 0.5 hrs2010European 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.
AID433899Anticonvulsant activity against thiosemicarbazide-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 2.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID366585Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed mouse2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Anticonvulsant activity of some xanthone derivatives.
AID1584806Permeability of the compound at pH 7.4 by PAMPA2018Journal 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.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID113457Anticonvulsant activity against bicuculline induced seizures in mice; Percentage of protection at 100 mg/kg per os.1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID52790Inhibition of chymotrypsin at 250 uM2003Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21
Identification and prediction of promiscuous aggregating inhibitors among known drugs.
AID1064724Antagonist 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 assay2014Bioorganic & medicinal chemistry, Feb-01, Volume: 22, Issue:3
Carbamazepine derivatives with P2X4 receptor-blocking activity.
AID194782Percent inhibition of 22Na+ uptake by voltage sensitive sodium channel of rat cortical synaptosomes at 100 uM1999Journal 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.
AID231427Protective index was calculated (TD50/ED50) in scMET assay in mice after oral administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID114802Anticonvulsant activity in tonic seizures when administered orally in mice1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1720864Protective 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 seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID496829Antimicrobial activity against Leishmania infantum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID132475The compound was tested for anticonvulsant activity against (subcutaneous administered) strychnine induced seizures after intraperitoneal administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID433889Protective index, ratio of TD50 for neurotoxicity to ED50 for anticonvulsant activity in ip dosed Kunming mouse2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID382367Anticonvulsant activity in ip dosed mouse assessed as inhibition of maximal electroshock-induced seizures after 4 hrs2008European 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.
AID699541Inhibition 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 counting2012Journal 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.
AID255438Protective index (TD50/ED50) produced by compound in mouse after MES test2005Bioorganic & 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.
AID1336193Neurotoxicity in ip dosed mouse2017Bioorganic & 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
AID136280The cytotoxicity after intraperitoneal administration in mice1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID305061Anticonvulsant activity against maximal electroshock-induced seizure in Albino mouse at 30 mg/kg, ip after 0.5 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain.
AID1335460Neurotoxicity in Swiss albino mouse at 300 mg/kg, ip after 4 hrs by rotarod test2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID1519676Retention time of compound at pH 7.4 by LC-UV analysis2020European journal of medicinal chemistry, Jan-01, Volume: 185Design of novel monoamine oxidase-B inhibitors based on piperine scaffold: Structure-activity-toxicity, drug-likeness and efflux transport studies.
AID418133Toxicity in ip dosed mouse assessed as minimal muscular or neurological impairment by rotarod paradigm test2009Journal 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.
AID1772564Apparent permeability of the compound across basolateral side to apical side in human Caco-2 cells incubated for 150 mins by LC-MS/MS analysis2021European journal of medicinal chemistry, Nov-05, Volume: 223Non-carboxylic acid inhibitors of aldose reductase based on N-substituted thiazolidinedione derivatives.
AID217795Displacement of [3H]BTX from voltage-gated sodium channel of rat cortical synaptosomes1999Journal 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.
AID178027Effective dose for anticonvulsant activity determined in rats using MES test procedure. (Phase VIA)1995Journal 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.
AID132471The compound was tested for anticonvulsant activity against (subcutaneous administered) Metrazol induced seizures after intraperitoneal administration; No protection up to 100 mg/kg1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID170612Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 0.5 hr; Compound was not screened1996Journal 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.
AID286889Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 2.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID679137TP_TRANSPORTER: transcellular transport in mdr1b-expressing LLC-PK1 cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1215128Ratio, 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 cocktai2011Drug 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.
AID156202Binding to POPC (palmitoyl-oleolyl-phosphatidyl-choline) liposomes using biosensor system2000Journal 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.
AID490611Neurotoxicity in ip dosed mouse assessed as time spent on rotarod by rotarod test2010European 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.
AID489274Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause toxicity after 4 hrs2010Bioorganic & 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.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug 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.
AID244602Dissociation constant for binding to inactivated state of rat brain NaIIa (rNav1.2) -B2 cell line stably expressed in HEK293 Cells2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors.
AID1335446Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 4 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID286870Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1605378Binding 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 assay2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID212345Toxic dose determined in mice using MES test procedure. (Phase II)1995Journal 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.
AID112459Anticonvulsant potency using the PTX (picrotoxin) test in mice by peroral administration1998Journal of medicinal chemistry, Feb-12, Volume: 41, Issue:4
Synthesis and anticonvulsant activity of a new class of 2-[(arylalky)amino]alkanamide derivatives.
AID1265486Anticonvulsant activity in po dosed Sprague-Dawley rat assessed as protection against subcutaneous dosed pentetrazol-induced seizures after 0.5 hrs2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID190586Anticonvulsant activity in corneal kindled rats was determined when 80 mg/kg was administered orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID632997Protective index, ratio of TD50 for neurotoxicity in mouse to ED50 for inhibition of maximal electroshock-induced seizures in mouse2011Bioorganic & 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.
AID481712Anticonvulsant 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 hrs2010European 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.
AID1720878Anticonvulsant activity in mouse assessed as protection against 50 mA current-induced seizure after 0.5 hrs by maximal electroshock seizure test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID628632Neurotoxicity in ip dosed CF1 albino mouse assessed as minimum dose required to cause motor impairment after 0.5 hrs by rotarod test2011European 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.
AID682355Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 300 mg/kg, ip after 4 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID490623Anticonvulsant activity in mouse assessed as thiosemicarbazide-induced tonic seizures at 30 mg/kg, ip administered 30 mins before thiosemicarbazide challenge measured after 2.5 hrs2010European 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.
AID243422log (1/Km) value for human liver microsome cytochrome P450 3A42005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Modeling K(m) values using electrotopological state: substrates for cytochrome P450 3A4-mediated metabolism.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1265487Anticonvulsant activity in po dosed Sprague-Dawley rat assessed as protection against maximal electroshock-induced seizures after 0.5 hrs2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID1246320Efflux ratio of permeability from basolateral to apical side over apical to basolateral side in human Caco2 cells2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1720879Anticonvulsant activity in mouse assessed as protection against current-induced seizure by maximal electroshock seizure test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID545527Anticonvulsant activity in ip dosed mouse assessed as inhibition of maximum electric shock-induced hind limb tonic extension2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives.
AID1209341Ratio of drug level in cerebrospinal fluid to unbound plasma concentration in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID185053Neuroprotective activity was determined in the rat middle cerebral artery occlusion (MCAO) model of focal stroke2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID1209357Ratio of unbound drug level in brain to plasma in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID1138688Permeability of the compound at pH 4 by PAMPA2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines.
AID678714Inhibition 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 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID180909The effective dose of compound was tested against subcutaneous administered Metrazol induced seizures in rat; Not effective1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID121847Central nervous system toxicity was performed by determining the median toxic dose in the rotarod test1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID255467Minimum dose required for anticonvulsant activity when given i.p., at 4 hr in mice upon maximal electroshock seizure2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID433887Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against maximal electroshock-induced seizures2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID1227824Metabolic stability in human liver microsomes assessed as compound remaining at 1 uM after 30 mins2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Dibenzazepines and dibenzoxazepines as sodium channel blockers.
AID112135Effective dose required to inhibit ataxia after intraperitoneal administration in experiment 21989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID1473739Inhibition 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 assay2013Toxicological 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.
AID286867Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID131217Maximal electroshock seizures was determined for the inhibition of hind limb tonus in mouse by 1 hr after po dose1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines.
AID384090Neurotoxicity in ip dosed CF1 albino mouse after 4 hrs by rotarod test2008European 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.
AID693325Neurotoxicity in ip dosed mouse after 30 mins by rotarod test2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID490620Anticonvulsant 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 hrs2010European 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.
AID678734TP_TRANSPORTER: inhibition of cyclosporin A transcellular transport by carbamazepine at a concentration of 224uM in mdr1a-expressing LLC-PK1 cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID156204Binding to POPC/GMI liposomes using biosensor system2000Journal 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.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID286865Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID608428Anticonvulsant activity in Kunming mouse assessed as inhibition of 3-mercaptopropionic acid-induced death at 30 mg/kg, ip after 0.5 hrs2011European 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.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1211294Unbound fraction in plasma (unknown origin) at pH 7.4 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug 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.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID217794Inhibition of [3H]BTX-B binding to neurotoxin site 2 of sodium channel of rat cerebral cortex synaptoneurosomes1995Journal 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.
AID178176Compound was tested for anticonvulsant activity by maximal electroshock seizure(MES) test in rat upon intraperitoneal administration1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents.
AID114634Anticonvulsant activity in Maximal electroshock (MES) when administered orally in mice1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1304301Displacement 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 method2016Bioorganic & 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.
AID471592Anticonvulsant 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 stimu2009Journal 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.
AID1138687Permeability of the compound at pH 7.4 by PAMPA2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines.
AID628727Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against subcutaneous pentylenetetrazole-induced after 0.5 hrs2011European 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.
AID1660935Permeability of the compound at 200 uM measured after 5 hrs at pH 7.4 by PAMPA2020Journal 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.
AID474787Solubility of compound in PBS buffer at pH 7.42010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Synthesis and structure-activity relationships of antimalarial 4-oxo-3-carboxyl quinolones.
AID363538Anticonvulsant activity in C57B/6 mouse assessed as inhibition of isoniazid-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID384089Neurotoxicity in ip dosed CF1 albino mouse after 0.5 hrs by rotarod test2008European 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.
AID632996Anticonvulsant activity in po dosed rat assessed as protection against maximal electric shock-induced seizures2011Bioorganic & 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.
AID136253Minimal motor impairment was measured in mouse by rotating rod test upon intraperitoneal administration1997Journal of medicinal chemistry, May-23, Volume: 40, Issue:11
Aroyl(aminoacyl)pyrroles, a new class of anticonvulsant agents.
AID226707Protective index which is the ratio of TD50 to ED50 of in maximal electroshock test. 1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis and anticonvulsant activity of imidooxy derivatives.
AID177577Ability to suppress MES (maximal electroshock) induced seizures in male Wistar rats1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants.
AID176347Compound was tested intraperitoneally for anticonvulsant activity against MES-induced seizures in rat by MES test1999Journal 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.
AID1264987Anticonvulsant activity in ip dosed Swiss albino mouse assessed as reduction of subcutaneous pentylenetetrazole-induced seizure2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID449306Neurotoxicity in ip dosed albino mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test2009European 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.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID678718Metabolic 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 analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID693317Anticonvulsant activity in ip dosed mouse assessed as compound concentration causing protection against maximal electroshock-induced seizures in half or more test animals after 4 hrs2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID1211293Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.22 after 6 hrs by equilibrium dialysis method2011Drug 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.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID190465Antagonist activity to generalized seizures kindled amygdaloid seizures in rats1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug 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.
AID1269482Displacement of [3H]Batrachotoxinin from sodium channel site 2 in rat cerebral cortex at 500 uM after 60 mins by scintillation counting method2016Bioorganic & 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.
AID682344Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 0.5 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID709901Stability in Wistar rat hepatocytes assessed as metabolite formation at >200 uM incubated for 6 hrs by HPLC and LC-MS/Ms method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID364286Anticonvulsant activity in ip dosed mouse after 0.5 hrs by MES test2008European 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.
AID632995Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electric shock-induced seizures2011Bioorganic & 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.
AID1544806Anticonvulsant 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 secs2019Bioorganic & 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.
AID608434Anticonvulsant activity in Kunming mouse assessed as inhibition of subcutaneous pentylenetetrazol-induced death at 50 mg/kg, ip after 0.5 hrs2011European 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.
AID1185524Anticonvulsant activity in ip dosed Kunming mouse assessed as protection against MES-induced seizures after 0.5 hrs by MES test2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID1210065Induction of CYP2B6 mRNA expression in human donor hepatocytes after 48 hrs by real-time PCR method relative to untreated control2013Drug 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.
AID130891Inhibition of hind limb tonus was tested by maximal metrazole seizure (MMS) test in mouse after 1 hr of peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID29363Dissociation constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID382368Anticonvulsant activity in ip dosed mouse assessed as inhibition of pentylenetetrazole-induced seizure after 0.5 hrs2008European 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.
AID1517279Protective 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 extension2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID1623670Apparent permeability of compound form basolateral to apical side in human Caco2 cells2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1753898Passive membrane permeability of the compound in phosphate buffered saline at 200 uM incubated for 5 hrs by PAMPA assay based HPLC analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.
AID190461Anticonvulsant activity in corneal kindled rats was determined when 20 mg/kg was administered orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID363536Anticonvulsant activity in C57B/6 mouse assessed as inhibition of isoniazid-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID1605381Inhibition 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 u2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID1335450Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 100 mg/kg, ip after 0.5 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID1217706Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID136098Effect of compound on mouse motor performance was studied by performing a rotarod test in mouse dosing intraperitoneally at time of peak effect.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID255734Anticonvulsant 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)2005Bioorganic & 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.
AID682317Neurotoxicity in mouse assessed as motor impairment at 300 mg/kg, ip after 0.5 hrs by rotarod test2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID24185Distribution coefficient in octanol/water at pH 7.41998Journal 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.
AID1193493Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID1265481Protection 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 seizures2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID131927Tested for inhibition of quinoline-induced seizures in mice.1990Journal of medicinal chemistry, Oct, Volume: 33, Issue:10
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
AID136096Effect of compound on mouse motor performance was studied by performing a rotarod test in mouse 1 hr after peroral dosing1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug 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.
AID305069Neurotoxicity in Albino mouse at 100 mg/kg, ip after 0.5 hrs by rotarod test2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain.
AID1193497Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method2015Bioorganic & 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.
AID384088Anticonvulsant activity in CF1 albino mouse assessed as prevention of subcutaneous pentylenetetrazole-induced seizure at 300 mg/kg, ip after 4 hrs2008European 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.
AID1211296Unbound fraction in plasma (unknown origin) under normal atmospheric condition at pH 7.72 after 6 hrs by equilibrium dialysis method2011Drug 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.
AID366629Protective index, ratio of TD50 for mouse by rotarod test to ED50 for mouse by scMET test2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Anticonvulsant activity of some xanthone derivatives.
AID1544807Anticonvulsant 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 secs2019Bioorganic & 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.
AID481713Anticonvulsant 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 hrs2010European 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.
AID178051Inhibition of hind limb tonus was tested by maximal metrazole seizure test after 1 hr of peroral administration of compound1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID1720881Protective 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 seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID1215120Binding affinity to Wistar rat brain lipid by TRANSIL assay2011Drug 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.
AID176271Maximal electroshock seizures determined for the inhibition of hind limb tonus in rat 1 hr after po dosing1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines.
AID132639Inhibition of s.c. pentylenetetrazole induced seizure in mice following i.p. administration.1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID344479Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 4 hrs by MES screen test2008European 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.
AID496826Antimicrobial activity against Entamoeba histolytica2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1360429Binding affinity to human serum albumin after 4 hrs by LC-MS method2018European journal of medicinal chemistry, Jul-15, Volume: 155Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.
AID29845Estimation of fraction absorbed (Fa) in the human intestine using biosensor technology.2000Journal 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.
AID489282Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs2010Bioorganic & 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.
AID1210067Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method relative to untreated control2013Drug 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.
AID21264Effective permeability measured in human.1998Journal 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.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1571357Anticonvulsant 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
AID1246317Permeability of the compound at pH 7.4 by PAMPA assay2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID496821Antimicrobial activity against Leishmania2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID351288Protective index, ratio of TD50 for neurotoxicity in C57B/6 mouse to ED50 for anticonvulsant activity in C57B/6 mouse2009European 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.
AID1304298Displacement 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 method2016Bioorganic & 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.
AID1154496Passive transcellular permeability of the compound at pH 4 by PAMPA2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Antileishmanial activity of a series of N²,N⁴-disubstituted quinazoline-2,4-diamines.
AID382369Anticonvulsant activity in ip dosed mouse assessed as inhibition of pentylenetetrazole-induced seizure after 4 hrs2008European 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.
AID681118TP_TRANSPORTER: transepithelial transport in Caco-2 cells2003International journal of pharmaceutics, Sep-16, Volume: 263, Issue:1-2
Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.
AID496818Antimicrobial activity against Trypanosoma brucei brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID462613Permeability across artificial membrane assessed as membrane retention at 200 uM by PAMPA using HPLC/MS method2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID643480Anticonvulsant activity in ip dosed Swiss albino mouse assessed as protection against maximal electroshock-induced seizures after 2 hrs2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents.
AID1217705Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID352393Anticonvulsant 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 test2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles.
AID394938Anticonvulsant 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 test2009European 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.
AID608435Anticonvulsant activity in Kunming mouse assessed as inhibition of subcutaneous pentylenetetrazol-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs2011European 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.
AID26047logBB, log(C brain / C blood)1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Computation of brain-blood partitioning of organic solutes via free energy calculations.
AID22950Time of peak effect (TPE) for activity1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis and anticonvulsant activity of imidooxy derivatives.
AID693337CNS depressant activity in mouse assessed as immobility time at 100 mg/kg, ip measured 60 mins post dose by porsolt's swimming pool test2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID286873Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID112295Compound was tested for anticonvulsant activity after intraperitoneal injection into mice by using scPTZ screen test after 0.25 hr1996Journal 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.
AID1191600Neurological toxicity in intraperitoneally dosed Swiss albino mouse assessed as motor impairment after 0.5 hrs by rotarod test2015Bioorganic & 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.
AID682346Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 4 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID382382Antidepressant activity in Wistar rat assessed as increase in immobility time at 30 mg/kg, ip after 30 mins by forced-swimming test2008European 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.
AID490625Anticonvulsant activity in mouse assessed as bicuculline-induced clonic seizures at 30 mg/kg, ip administered 30 mins before bicuculline challenge measured after 0.5 hrs2010European 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.
AID449311Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of subcutaneous pentylenetetrazole-induced seizure after 4 hrs2009European 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.
AID364288Anticonvulsant activity in ip dosed mouse after 4 hrs by MES test2008European 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.
AID255439Protective index (TD50/ED50) produced by compound in mouse after ScMet test2005Bioorganic & 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.
AID1636356Drug 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 NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1079935Cytolytic 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]
AID1210064Induction of CYP2B6 mRNA expression in human donor hepatocytes after 48 hrs by real-time PCR method2013Drug 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.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1191596Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in electrical stimulus-induced seizures after 0.5 hrs by maximal electroshock seizure test2015Bioorganic & 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.
AID205290Affinity for inactive human SkM1 sodium channel expressed in HEK293 cells2004Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
3-(4-phenoxyphenyl)pyrazoles: a novel class of sodium channel blockers.
AID122469Ratio of the dose showing muscle relaxant action in rats and the dose suppressing MES induced seizures in rats1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Substituted (omega-aminoalkoxy) stilbene derivatives as a new class of anticonvulsants.
AID1720890Anticonvulsant activity in KunMing mouse assessed as protection against current-induced seizure by maximal electroshock seizure test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID727990Antiepileptic activity in ip dosed Swiss albino mouse assessed as protection against scPTZ-induced seizures after 4 hrs2013Bioorganic & 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.
AID129448Antipentylene tetrazole activity was determined in mice when administered perorally1988Journal 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.
AID637069Neurotoxicity in ip dosed Kunming mouse assessed as minimal motor impairment after 0.5 hrs by rotarod test2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones.
AID52381Oral dose protecting 50% of the mice from electroshock induced seizures.1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID1336194Protection index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for ip dosed maximal electroshock induced seizure mouse model2017Bioorganic & 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
AID226509Protection index = TD50/ED50 (MES)1996Journal 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.
AID221089Time of peak effect of toxicity of compound was measured by both MES and sc Met test in mice1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and CLOGP correlation of imidooxy anticonvulsants.
AID628629Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against maximal electroshock after 4 hrs2011European 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.
AID190105Compound was tested for anticonvulsant activity administered by gastric tube in rat by rotarod test1999Journal 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.
AID217928Inhibition of veratridine-induced guanidine flux in cardiac voltage-gated sodium channel (veratridine block vs. Na release)2001Journal of medicinal chemistry, Jan-18, Volume: 44, Issue:2
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1209333Ratio of drug level in brain to plasma in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID1335449Anticonvulsant activity in Swiss albino mouse assessed as protection against subcutaneously injected metrazol induced seizures at 30 mg/kg, ip after 0.5 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID433898Toxicity in Kunming mouse assessed as 3-mercaptopropionic acid-induced lethality at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID1185529Protective index, ratio of oral neurotoxic TD50 against Kunming mouse by rotarod test to oral anticonvulsant ED50 in Kunming mouse by MES test2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID353056Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against maximal electroshock-induced seizure after 30 mins2009European 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.
AID433893Anticonvulsant activity against isoniazid-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID477359Protective index, ratio of TD50 for neurotoxicity in Swiss albino mouse to ED50 for inhibition of maximal electroshock-induced seizures Swiss albino mouse2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.
AID1605382Inhibition 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 mea2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID709905Drug 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 method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID709902Drug 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 method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID286861Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID286886Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 1 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID678927TP_TRANSPORTER: no change in brain concentration in mdr1a/1b(-/-) mouse2001British journal of clinical pharmacology, Apr, Volume: 51, Issue:4
Carbamazepine is not a substrate for P-glycoprotein.
AID47017Dose producing neurotoxic effects in 50% of the CF1 mice after intraperitoneal administration.1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID136279The cytotoxicity after intraperitoneal administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID1227820Inhibition of Nav1.7 (unknown origin) by electrophysiological assay2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Dibenzazepines and dibenzoxazepines as sodium channel blockers.
AID109718Anticonvulsant activity after intraperitoneal injection into mice by using MES screen test after 0.5 hr1996Journal 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.
AID109720Anticonvulsant activity after intraperitoneal injection into mice by using scPTZ screen after 0.5 hr1996Journal 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.
AID286894Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 2.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID114126Anticonvulsant activity in mice using the maximal electroshock seizure test.1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID1701383Intrinsic clearance in mouse liver microsomes at 1 uM measured up to 30 mins in presence of NADPH by UPLC-MS/MS analysis
AID189164Protective index value of the compound, given by intraperitoneally (TD50/ED50)1999Journal 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.
AID256147Number 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 activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID1544809Anticonvulsant 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 induc2019Bioorganic & 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.
AID205273Concentration required to inhibit [3H]BTX binding to Sodium channel of rat brain2004Bioorganic & medicinal chemistry letters, Jul-05, Volume: 14, Issue:13
2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators.
AID396643Anticonvulsant activity in OF1 mouse assessed as protection against maximal electroshock-induced seizures at 50 mg/kg, ip after 2 hrs2008European journal of medicinal chemistry, Dec, Volume: 43, Issue:12
Indanesulfonamides as carbonic anhydrase inhibitors and anticonvulsant agents: structure-activity relationship and pharmacological evaluation.
AID489279Anticonvulsant activity against subcutaneous strychnine-induced seizures in Wistar rat at 300 mg/kg, ip after 0.5 hrs2010Bioorganic & 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.
AID256138Number 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 activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID462611Effective permeability across artificial membrane at 200 uM by PAMPA using HPLC/MS method2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID1227823Kinetic solubility of the compound at pH 6.82015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Dibenzazepines and dibenzoxazepines as sodium channel blockers.
AID496827Antimicrobial activity against Leishmania amazonensis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID129976Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in mouse maximal metrazole seizures (MMS) after peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID709900Drug 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 method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID1264989Protective 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 seizure2015European journal of medicinal chemistry, Dec-01, Volume: 106Synthesis of 2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxide derivatives as potent anticonvulsant agents.
AID363540Toxicity in isoniazid-induced seizure C57B/6 mouse model assessed as lethality at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID353057Neurotoxicity in ip dosed C57B/6 mouse after 30 mins by rotarod test2009European 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.
AID1335447Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 100 mg/kg, ip after 4 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID1304297Displacement 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 method2016Bioorganic & 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.
AID1251235Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizure2015Bioorganic & 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.
AID132648The effective dose of compound was tested against maximal electroshock induced seizures after oral administration in mice1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID1195113Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse by maximal electroshock test2015Bioorganic & 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.
AID1223490Apparent permeability across human differentiated Caco2 cells2012Drug 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.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID363532Anticonvulsant activity in C57B/6 mouse assessed as inhibition of pentylenetetrazole-induced tonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID682319Neurotoxicity in mouse assessed as motor impairment at 100 mg/kg, ip after 4 hrs by rotarod test2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID1229816Inhibition 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 assay2015Journal 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.
AID481707Anticonvulsant 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 hrs2010European 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.
AID170623Compound was tested for anticonvulsant activity after Oral Administration into Rats by using MES screen test after 1 hr; Compound was not screened1996Journal 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.
AID1720894Protective index, ratio of TD50 for neurotoxicity in KunMing mouse to ED50 for anticonvulsant activity in KunMing mouse assessed as protection against current-induced seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID24420Partition coefficient (logP)1998Journal 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.
AID545528Anticonvulsant activity in ip dosed mouse assessed as inhibition of PTZ-induced clonic seizure2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
Synthesis and anticonvulsant activity of N-3-arylamide substituted 5,5-cyclopropanespirohydantoin derivatives.
AID481705Anticonvulsant 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 hrs2010European 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.
AID256413Minimum dose required for anticonvulsant activity when given i.p., at 0.5 h in mice upon subcutaneous strychnine seizure; Absence of activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID225157Dose reducing the seizure severity in rat cornea 1 hr after peroral administration.1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID227701Anticonvulsant activity; NC denotes that compound is not classified2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
AID643474Neurotoxicity in ip dosed Swiss albino mouse assessed as impair in motor coordination from 0.5 to 4 hrs post administration by rotarod test2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents.
AID1336188Anticonvulsant activity in ip dosed 6-Hz induced seizure mouse model assessed as restoration of normal activity within 10 secs from stimulation at 32 mA2017Bioorganic & 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
AID136110Inhibition of hind limb tonus was tested by maximal metrazole seizure (MMS) test administered intraperitoneally in mouse1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID177915Inhibition of hind limb tonus was tested at time of peak effect by maximal electroshock test (MES) on intraperitoneal administration of compound in rats1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID286872Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1211295Unbound fraction in plasma (unknown origin) at pH 7.63 after 6 hrs by equilibrium dialysis method in presence of 5% CO22011Drug 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.
AID256144Number 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 activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID418135Anticonvulsant activity in po dosed rat assessed as protection against subcutaneous metrazole-induced seizure2009Journal 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.
AID130888Inhibition of hind limb tonus was tested at time of peak effect by maximal electroshock test (MES) in mouse on intraperitoneal administration of compound1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID286871Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID462614Apparent permeability in BBMEC2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID1160934Effective permeability of the compound at pH 7.4 by PAMPA2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID624609Specific activity of expressed human recombinant UGT1A62000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID1185527Anticonvulsant activity in orally dosed Kunming mouse assessed as protection against MES-induced seizures after 0.5 hrs by MES test2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID1720887Anticonvulsant activity in KunMing mouse assessed as protection against 50 mA current-induced seizure after 0.5 to 4 hrs by maximal electroshock seizure test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID418138Therapeutic index, ratio of TD50 for po dosed rat to ED50 for protection against subcutaneous metrazole-induced seizure in po dosed rat2009Journal 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.
AID1191601Neurological toxicity in intraperitoneally dosed Swiss albino mouse assessed as motor impairment after 4 hrs by rotarod test2015Bioorganic & 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.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID110223Ability to prevent the tonic extensor component induced by 106.25 mg/kg sc of pentylenetetrazole1994Journal of medicinal chemistry, Jul-08, Volume: 37, Issue:14
Synthesis and anticonvulsant properties of new benzylpyridazine derivatives.
AID1623671Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Caco2 cells2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID221087Time of peak effect of activity of compound was measured by both MES and sc Met test in mice1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and CLOGP correlation of imidooxy anticonvulsants.
AID1304299Displacement 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 method2016Bioorganic & 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.
AID489286Anticonvulsant activity against maximal electroshock-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 4 hrs2010Bioorganic & 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.
AID1209379AUC(0 to 7 hrs) in Sprague-Dawley rat plasma at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID709893Drug metabolism in human liver microsomes assessed as 10,11 epoxidation level at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID1571282Neurotoxicity in Sprague-Dawley rat at 100 mg/kg, ip measured after 2 hrs by rotarod test
AID1336196Protection index, ratio of TD50 for neurotoxicity in ip dosed mouse to ED50 for ip dosed 6-Hz induced seizure mouse model at 32 mA2017Bioorganic & 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
AID363530Anticonvulsant activity in C57B/6 mouse assessed as inhibition of pentylenetetrazole-induced clonic seizures at 50 mg/kg, ip after 0.5 hrs relative to control2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID51429Compound was evaluated for toxic dose at peak neurologic deficit after intraperitoneal administration of the compound.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis and anticonvulsant activity of imidooxy derivatives.
AID114861Effective dose required for the inhibition of spontaneous locomotion after intraperitoneal administration in experiment 11989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID608530Anticonvulsant activity in Kunming mouse assessed as inhibition of thiosemicarbazide-induced death at 30 mg/kg, ip after 2.5 hrs2011European 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.
AID489284Anticonvulsant activity against subcutaneous pentylenetetrazole-induced seizures in ip dosed Swiss albino mouse assessed as minimum effective dose after 0.5 hrs2010Bioorganic & 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.
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID286879Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs, ip2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1335456Neurotoxicity in Swiss albino mouse at 100 mg/kg, ip after 0.5 hrs by rotarod test2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID364292Anticonvulsant activity in ip dosed mouse after 4 hrs by scPTZ test2008European 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.
AID132637The compound was tested to inhibit 50% of induced maximal electroshock seizure in mice on ip administration.1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID178166Compound was tested for anticonvulsant activity administered by gastric tube in rat by MES test1999Journal 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.
AID366628Anticonvulsant activity against scMet-induced seizures in ip dosed mouse2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Anticonvulsant activity of some xanthone derivatives.
AID643475Protection index, ratio of TD50 for Swiss albino mouse by rotarod test to ED50 for Swiss albino mouse by maximal electroshock test2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Design and synthesis of 3,5-diarylpiperidin-2,6-diones as anticonvulsant agents.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID132474Anticonvulsant activity against subcutaneous picrotoxin induced seizures after intraperitoneal administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID1065339Anticonvulsant activity in albino rat assessed as protection against pentylenetetrazole-induced seizure at 300 mg/kg, ip measured after 4 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID295296Anticonvulsant activity in OF1 mouse at 30 mg/kg, ip after 2 hrs by MES test2007Bioorganic & 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.
AID1404017Permeability of the compound at 500 uM after 8 hrs by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID7779Oral bioavailability in human2002Journal 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.
AID1246354Permeability of the compound at pH 7.4 assessed as drug retention by PAMPA assay2015European journal of medicinal chemistry, Sep-18, Volume: 102(+)-Dehydroabietylamine derivatives target triple-negative breast cancer.
AID1065341Anticonvulsant activity in albino rat assessed as protection against pentylenetetrazole-induced seizure at 300 mg/kg, ip measured after 0.5 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID212343The compound was determined for the dose (mg/kg) by rotarod test at the time of peak neurotoxic effect in mice on ip administration.1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Synthesis and anticonvulsant activity of 2(3H)-benzoxazolone and 2(3H)-benzothiazolone derivatives.
AID632993Neurotoxicity in ip dosed mouse assessed as inability to maintain equilibrium on rotarod by rotarod test2011Bioorganic & 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.
AID1335458Neurotoxicity in Swiss albino mouse at 30 mg/kg, ip after 4 hrs by rotarod test2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID637075Protective index, ratio of TD50 for ip dosed Kunming mouse to ED50 for ip dosed Kunming mouse by maximal electroshock seizure test2012European journal of medicinal chemistry, Feb, Volume: 48Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones.
AID709899Drug metabolism in Wistar rat hepatocytes assessed as GSH adduct formation at 50 uM incubated for 6 hrs by HPLC and LC-MS/Ms method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID1193494Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method2015Bioorganic & 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.
AID709903Drug 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 method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID113854Effective dose against convulsions induced by clonic pentylenetetrazole after intraperitoneal administration in experiment 11989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
AID1265489Protection 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 seizures2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID1705559Drug metabolism in rat liver microsomes at 50 uM preincubated with compound followed by NADPH addition and measured after 60 mins by LC-MS/MS analysis2020European journal of medicinal chemistry, Dec-15, Volume: 208Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction.
AID1720882Neurotoxicity in mouse by rotarod test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID1215123Binding affinity to Wistar rat serum albumin2011Drug 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.
AID382371Neurotoxicity in ip dosed mouse after 4 hrs by rotarod test2008European 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.
AID440595Anticonvulsant activity in Webster mouse assessed as protection against yohimbine-HCl-induced clonic seizure at 5 mg/kg, ip administered 30 mins before yohimbine-HCl challenge2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
Analgesic, anticonvulsant and anti-inflammatory activities of some synthesized benzodiazipine, triazolopyrimidine and bis-imide derivatives.
AID1404016Permeability of the compound by PAMPA2018European journal of medicinal chemistry, Feb-10, Volume: 145Chameleon-like behavior of indolylpiperidines in complex with cholinesterases targets: Potent butyrylcholinesterase inhibitors.
AID189163Protective index value of the compound, given by gastric tube (TD50/ED50)1999Journal 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.
AID1304300Displacement 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 method2016Bioorganic & 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.
AID624607Specific activity of expressed human recombinant UGT1A32000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID418131Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizure2009Journal 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.
AID366627Neurotoxicity in ip dosed mouse by rotarod test2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Anticonvulsant activity of some xanthone derivatives.
AID286882Anti-dynamic allodynic effect in Sprague-Dawley rat CCI model assessed as latency to paw withdrawal after 1.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID384084Anticonvulsant activity in ip dosed CF1 albino mouse assessed as prevention of subcutaneous pentylenetetrazole-induced seizure after 0.5 hrs2008European 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.
AID286896Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 1 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID481714Anticonvulsant in po dosed mouse assessed as protection against maximum electric stimulus-induced seizures2010European 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.
AID682348Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 30 mg/kg, ip after 0.5 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID608432Anticonvulsant activity in Kunming mouse assessed as inhibition of isoniazid-induced tonic seizures at 50 mg/kg, ip after 1 hrs2011European 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.
AID693315Anticonvulsant 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 hrs2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID449307Neurotoxicity in ip dosed albino mouse assessed as minimal motor impairment after 4 hrs by rotarod test2009European 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.
AID286899Anti-cold allodynia effect in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal 100 mg/kg, ip after 2.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID462616Apparent permeability in BBMEC assessed as membrane retention2010Journal of medicinal chemistry, Mar-25, Volume: 53, Issue:6
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
AID178052Inhibition of hind limb tonus was tested by maximal metrazole seizure test after 4 hr of peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
AID1383763Effective permeability of the compound at pH 7.4 at 200 uM after 4 hrs by PAMPA-BBB assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Metallomics for Alzheimer's disease treatment: Use of new generation of chelators combining metal-cation binding and transport properties.
AID1336213Neurotoxicity in po dosed Sprague-Dawley rat assessed as behavioral change2017Bioorganic & 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
AID1660936Permeability of the compound assessed as mass retention at 200 uM measured after 5 hrs at pH 7.4 by PAMPA2020Journal 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.
AID1720884Anticonvulsant activity in KunMing mouse assessed as protection against 50 mA current-induced seizure after 30 mins interval by maximal electroshock seizure test2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID394945Neurotoxicity 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 test2009European 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.
AID678717Inhibition 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 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID244690Dissociation constant for binding to resting state of rat brain NaIIa (rNav1.2) -B2 cell line stably expressed in HEK293 Cells2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Phenoxyphenyl pyridines as novel state-dependent, high-potency sodium channel inhibitors.
AID1209409AUC(0 to 7 hrs) in Sprague-Dawley rat brain at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID449304Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of maximal electric shock-induced seizures after 4 hrs2009European 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.
AID481697Anticonvulsant in ip dosed mouse assessed as protection against maximum electric stimulus-induced seizures2010European 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.
AID190581Anticonvulsant activity in corneal kindled rats was determined when 40 mg/kg was administered orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID666677Neurotoxicity in ip dosed Kunming mouse measured 30 mins post compound administration by rotorod test2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives.
AID477358Anticonvulsant activity in ip dosed Swiss albino mouse assessed as inhibition of PTZ-induced motor impairment2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.
AID1517333Inhibition of human LDH1 assessed as remaining activity at 0.5 mM using sodium pyruvate as substrate by UV-VIS spectrophotometry method relative to control2019European journal of medicinal chemistry, Dec-01, Volume: 183Polygala tenuifolia-Acori tatarinowii herbal pair as an inspiration for substituted cinnamic α-asaronol esters: Design, synthesis, anticonvulsant activity, and inhibition of lactate dehydrogenase study.
AID114036Minimal motor impairment activity by Rotarod test in mice following i.p. administration.1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID205268Inhibition 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 uM1985Journal 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.
AID1720867Anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID449303Anticonvulsant activity in ip dosed albino mouse assessed as inhibition of maximal electric shock-induced seizures after 0.5 hrs2009European 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.
AID509497Reduction of immobility time in albino Swiss mouse at 100 mg/kg, ip pretreated for 1 hrs by forced swimming test2010European 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.
AID1058306Anticonvulsant 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-stimulation2013Journal 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).
AID256140Number 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 activity2005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID682349Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 100 mg/kg, ip after 0.5 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID1191598Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in clonic seizures after 0.5 hrs by subcutaneous pentylenetetrazole seizure test2015Bioorganic & 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.
AID693324Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 4 hrs by rotarod test2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID1265491Anticonvulsant activity in ip dosed albino Carworth Farms No.1 mouse assessed as protection against subcutaneous dosed pentetrazol-induced seizures after 0.25 hrs2016European journal of medicinal chemistry, Jan-01, Volume: 107Anticonvulsant activity, crystal structures, and preliminary safety evaluation of N-trans-cinnamoyl derivatives of selected (un)modified aminoalkanols.
AID177084Compound was evaluated for inhibition of hind limb tonus (anticonvulsant activity) in rat maximal electroshock seizures (MES) after peroral administration1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
AID352567Neurotoxicity 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 test2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles.
AID190110Compound was tested intraperitoneally for anticonvulsant activity by rotarod test1999Journal 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.
AID351012Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against thiosemicarbazide-induced tonic seizure administered 30 mins before thiosemicarbazide challenge measured after 1 hrs2009European 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.
AID286875Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr, ip2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1160938Aqueous solubility of the compound at pH 22014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Orally bioavailable 6-chloro-7-methoxy-4(1H)-quinolones efficacious against multiple stages of Plasmodium.
AID709897Stability 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 method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID1227825Metabolic stability in rat liver microsomes assessed as compound remaining at 1 uM after 30 mins2015Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1
Dibenzazepines and dibenzoxazepines as sodium channel blockers.
AID217788Displacement of [3H]batrachotoxin A 20alpha-benzoate (BTX-B) from rat cerebral cortex voltage-gated sodium channel1989Journal 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.
AID1783665Effective permeability of the compound in PBS/EtOH buffer (9:1) at 200 mM after 10 hrs by HPLC-UV based PAMPA-BBB assay2021European journal of medicinal chemistry, Nov-15, Volume: 2241,10-Seco-Eudesmane sesquiterpenoids as a new type of anti-neuroinflammatory agents by suppressing TLR4/NF-κB/MAPK pathways.
AID453204Permeability in human skin after 48 hrs by Franz cell permeability assay2010Bioorganic & 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.
AID1571287Anticonvulsant activity in ip dosed CF-1 mouse model of maximal electroshock-induced seizure assessed as suppression of tonic hind limb extension
AID286891Anti-dynamic allodynia effect in Sprague-Dawley rat SNL model assessed as latency to paw withdrawal 100 mg/kg, ip after 1 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID679773TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Carbamazepine: 100 uM) in MDR1-expressing MDCKII cells2002The 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.
AID139327Time of peak effect toxicity against maximal electroshock induced seizures1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID1701382Intrinsic clearance in human liver microsomes at 1 uM measured up to 30 mins in presence of NADPH by UPLC-MS/MS analysis
AID286874Effect on spontaneous pain in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID231424Protective index was calculated (TD50/ED50) in MES assay in mice after oral administration1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID223442Effective dose was measured in mouse by subcutaneous pentylenetetrazole method by ip administration; Not determined1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and CLOGP correlation of imidooxy anticonvulsants.
AID1065335Neurotoxicity in ip dosed albino mouse after 4 hrs by rotorod test2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID1335455Neurotoxicity in Swiss albino mouse at 30 mg/kg, ip after 0.5 hrs by rotarod test2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID1753896Passive 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 analysis2021Journal of medicinal chemistry, 04-22, Volume: 64, Issue:8
Beyond Basicity: Discovery of Nonbasic DENV-2 Protease Inhibitors with Potent Activity in Cell Culture.
AID351283Anticonvulsant activity in ip dosed C57B/6 mouse assessed as protection against isoniazid-induced seizures administered before 30 mins of isoniazid induction measured for 1 hr2009European 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.
AID679128TP_TRANSPORTER: transcellular transport in MDR1-expressing LLC-PK1 cells2007Neuropharmacology, Feb, Volume: 52, Issue:2
Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein.
AID366631Displacement of [3H]nitrendipine from voltage-dependent calcium channel in rat brain cortex by scintillation counting2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Anticonvulsant activity of some xanthone derivatives.
AID286887Anti-cold allodynia effect in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal 100 mg/kg, ip after 1.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID608517Protective index, ratio of TD50 for neurotoxicity in Kunming mouse to ED50 for inhibition of MES-induced seizures in Kunming mouse2011European 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.
AID1720865Protective index, ratio of TD50 for neurotoxicity in ip injected albino mouse to ED50 for anticonvulsant activity in albino mouse assessed as pentylenetetrazole-induced seizure2020Bioorganic & medicinal chemistry, 08-01, Volume: 28, Issue:15
Synthetic and therapeutic perspectives of nitrogen containing heterocycles as anti-convulsants.
AID50621Compound was evaluated for effective dose by subcutaneous pentylenetetrazole test after intraperitoneal administration of the compound; Not Effective1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Synthesis and anticonvulsant activity of imidooxy derivatives.
AID467612Fraction unbound in human plasma2009European 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.
AID305062Anticonvulsant activity against maximal electroshock-induced seizure in Albino mouse at 300 mg/kg, ip after 4 hrs2007Bioorganic & medicinal chemistry letters, Jan-01, Volume: 17, Issue:1
Synthesis and anticonvulsant activity of sulfonamide derivatives-hydrophobic domain.
AID1304305Displacement 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 method2016Bioorganic & 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.
AID693321Anticonvulsant activity in ip mouse assessed as protection against subcutaneous pentylenetetrazol-induced seizures2012European journal of medicinal chemistry, Dec, Volume: 58Design, synthesis and evaluation of N-(substituted benzothiazol-2-yl)amides as anticonvulsant and neuroprotective.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID256185Post 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) 1312005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
Discovery of N-(2,6-dimethylphenyl)-substituted semicarbazones as anticonvulsants: hybrid pharmacophore-based design.
AID481708Anticonvulsant 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 hrs2010European 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.
AID1173473Protective index, ratio of TD50 for CF1 albino mouse neurotoxicity to ED50 for protection against 6 Hz electroshock-induced seizure in CF1 albino mouse2014Bioorganic & 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.
AID497005Antimicrobial activity against Pneumocystis carinii2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID114801Anticonvulsant activity in Clonic seizures when administered orally in mice1986Journal of medicinal chemistry, Mar, Volume: 29, Issue:3
Synthesis and activity of 6-aryl-3-(hydroxypolymethyleneamino)pyridazines in animal models of epilepsy.
AID1217704Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID1335443Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 30 mg/kg, ip after 0.5 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID1605383Binding 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 formati2020Journal of medicinal chemistry, 03-26, Volume: 63, Issue:6
Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
AID496820Antimicrobial activity against Trypanosoma brucei2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1209457Unbound Cmax in human plasma2012Drug 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.
AID1065344Anticonvulsant activity in ip dosed albino mouse assessed as protection against maximal electroshock-induced seizures after 4 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID1185533Anticonvulsant activity in Kunming mouse assessed as protection against sc-PTZ-induced mortality 50 mg/kg, sc administered 30 mins before PTZ injection2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID481706Anticonvulsant 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 hrs2010European 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.
AID180905The effective dose of compound was tested against maximal electroshock induced seizures after oral administration in rat1990Journal of medicinal chemistry, Mar, Volume: 33, Issue:3
Synthesis and anticonvulsant activity of 2-benzylglutarimides.
AID344478Anticonvulsant activity in ip dosed CF1 albino mouse assessed as minimum effective dose after 0.5 hrs by MES screen test2008European 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.
AID363528Neurotoxicity in ip dosed C57B/6 mouse after 30 mins by rotarod test2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis of novel 7-benzylamino-2H-1,4-benzoxazin-3(4H)-ones as anticonvulsant agents.
AID1573965Anticonvulsant 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
AID1623690Permeability of compound at pH 7.4 assessed as drug retention by PAMPA2019European journal of medicinal chemistry, Feb-15, Volume: 164Identification of substituted 5-membered heterocyclic compounds as potential anti-leukemic agents.
AID1217708Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system2011Drug 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.
AID1209385AUC(0 to infinity) in Sprague-Dawley rat plasma at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID481444Octanol-water partition coefficient, log P of the compound2010Journal 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?
AID286860Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 0.5 hr2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID433894Anticonvulsant activity against 3-mercaptopropionic acid-induced seizures in Kunming mouse assessed as clonic seizures of at 50 mg/kg, ip after 0.5 hrs2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Synthesis and anticonvulsant activity of N-(2-hydroxyethyl) cinnamamide derivatives.
AID1185531Anticonvulsant activity in Kunming mouse assessed as protection against sc-PTZ-induced clonic seizures 50 mg/kg, sc administered 30 mins before PTZ injection2014European journal of medicinal chemistry, Sep-12, Volume: 84Synthesis and anticonvulsant activity of novel purine derivatives.
AID1810293Aqueous solubility of compound at pH 7.42021Journal 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
AID1335448Anticonvulsant activity in Swiss albino mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 4 hrs2016European journal of medicinal chemistry, Nov-29, Volume: 124New (arylalkyl)azole derivatives showing anticonvulsant effects could have VGSC and/or GABA
AID632998Protective index, ratio of TD50 for neurotoxicity in rat to ED50 for inhibition of maximal electroshock-induced seizures in rat2011Bioorganic & 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.
AID286864Effect on spontaneous pain in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID1209349Ratio of unbound brain concentration to drug level in cerebrospinal fluid in Sprague-Dawley rat at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID539470Solubility of the compound in water2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
Experimental solubility profiling of marketed CNS drugs, exploring solubility limit of CNS discovery candidate.
AID286877Antihyperalgesic effects in Sprague-Dawley rat SNL model assessed as duration of paw withdrawal at 100 mg/kg, ip after 1.5 hrs, ip2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID496830Antimicrobial activity against Leishmania major2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID1209417AUC(0 to infinity) in Sprague-Dawley rat brain at 3 mg/kg, sc by LC-MS/MS analysis2012Drug 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.
AID20163The ratio of brain-blood partitioning, (C brain / C blood).1996Journal of medicinal chemistry, Nov-22, Volume: 39, Issue:24
Computation of brain-blood partitioning of organic solutes via free energy calculations.
AID477357Anticonvulsant activity in ip dosed Swiss albino mouse assessed as inhibition of maximum electric shock-induced motor impairment2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.
AID351013Anticonvulsant 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 hrs2009European 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.
AID109723Toxicity after intraperitoneal injection into mice by using toxicity screen test after 0.5 hr1996Journal 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.
AID1065346Anticonvulsant activity in ip dosed albino mouse assessed as protection against maximal electroshock-induced seizures after 0.5 hrs2013European journal of medicinal chemistry, Sep, Volume: 67Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
AID352389Anticonvulsant 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 test2009European journal of medicinal chemistry, Mar, Volume: 44, Issue:3
Synthesis and anticonvulsant activity of some substituted 1,2,4-thiadiazoles.
AID1191597Anticonvulsant activity in intraperitoneally dosed Swiss albino mouse assessed as reduction in electrical stimulus-induced seizures after 4 hrs by maximal electroshock seizure test2015Bioorganic & 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.
AID666679Protective index, ratio of TD50 for neurotoxicity in Kunming mouse to ED50 for protection against subcutaneous pentylenetetrazol-induced clonic seizures in Kunming mouse2012European journal of medicinal chemistry, Aug, Volume: 54Synthesis and anticonvulsant activity of ethyl 1-(2-arylhydrazinecarboxamido)-2,2-dimethylcyclopropanecarboxylate derivatives.
AID223725Oral dose producing neurotoxic effects in 50% of rats1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Synthesis and anticonvulsant activity of enaminones.
AID351014Anticonvulsant 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 mins2009European 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.
AID113965Anticonvulsant activity was measured by maximal electroshock seizure test in mice by ip administration1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles.
AID682347Anticonvulsant activity in mouse assessed as protection against maximal electroshock-induced seizures at 300 mg/kg, ip after 4 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID286869Antihyperalgesic effects in Sprague-Dawley rat CCI model assessed as duration of paw withdrawal at 100 mg/kg, ip after 2.5 hrs2007Journal of medicinal chemistry, May-17, Volume: 50, Issue:10
Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.
AID418137Therapeutic index, ratio of TD50 for ip dosed mouse to ED50 for protection against subcutaneous metrazole-induced seizure in ip dosed mouse2009Journal 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.
AID682353Anticonvulsant activity in mouse assessed as protection against subcutaneous pentylenetetrazole-induced seizures at 30 mg/kg, ip after 4 hrs2012European journal of medicinal chemistry, Nov, Volume: 57Synthesis of some novel 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone oxime ester derivatives and evaluation of their anticonvulsant activity.
AID364303Central nervous system depressant activity in Wistar rat assessed as immobility time at 30 mg/kg, ip after 1 hr by forced swim pool test2008European 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.
AID490610Anticonvulsant activity in ip dosed mouse assessed as protection against maximal electroshock-induced seizures2010European 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.
AID709892Stability in human liver microsomes assessed as diol formation at 50 uM incubated for 60 mins by HPLC and LC-MS/Ms method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
Haloarene derivatives of carbamazepine with reduced bioactivation liabilities: 2-monohalo and 2,8-dihalo derivatives.
AID364296Neurotoxicity in ip dosed mouse assessed as minimal motor impairment after 4 hrs by rotarod test2008European 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.
AID1195114Anticonvulsant activity in intraperitoneally dosed Albino Swiss CD1 mouse by subcutaneous pentylenetetrazole test2015Bioorganic & 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.
AID489276Neurotoxicity in ip dosed Swiss albino mouse assessed as minimum dose required to cause toxicity after 0.5 hrs2010Bioorganic & 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.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID109719Anticonvulsant activity after intraperitoneal injection into mice measured in a maximal electroshock scree (MES) screen1996Journal 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.
AID628628Anticonvulsant activity in ip dosed CF1 albino mouse assessed as protection against maximal electroshock after 0.5 hrs2011European 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.
AID298031Lipophilicity, log D at pH7.42007Journal 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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal 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.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & 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.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1224864HCS microscopy assay (F508del-CFTR)2016PloS 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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-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]

Research

Studies (11,004)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902756 (25.05)18.7374
1990's2297 (20.87)18.2507
2000's2556 (23.23)29.6817
2010's2642 (24.01)24.3611
2020's753 (6.84)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 110.08

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

MetricThis Compound (vs All)
Research Demand Index110.08 (24.57)
Research Supply Index9.48 (2.92)
Research Growth Index4.56 (4.65)
Search Engine Demand Index209.16 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (110.08)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1,128 (9.41%)5.53%
Reviews1,217 (10.15%)6.00%
Case Studies2,747 (22.91%)4.05%
Observational45 (0.38%)0.25%
Other6,855 (57.16%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (105)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Phase IV Open Non Comparative Trial to Evaluate Efficacy and Safety of Tegretol® in Diabetes Neuropathy Pain. [NCT01089855]Phase 4123 participants (Actual)Interventional2009-12-31Completed
A Randomized Controlled Trial of Generic Substitution of Antiepileptic Drugs [NCT02429596]Phase 4200 participants (Anticipated)Interventional2012-05-31Recruiting
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 4374 participants (Anticipated)Interventional2020-01-07Not 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 116 participants (Actual)Interventional2011-04-30Completed
[NCT01382017]18 participants (Actual)Interventional2011-06-30Completed
PHASE II STUDY TO EVALUATE EFFICACY AND SAFETY OF CARBAMAZEPINE FOR THE PREVENTION OF CHEMOTHERAPY-INDUCED NAUSEA AND VOMITING. [NCT01581918]Phase 243 participants (Anticipated)Interventional2011-12-31Recruiting
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 112 participants (Actual)Interventional2023-08-18Active, 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 133 participants (Actual)Interventional2023-08-08Completed
Role of Clinical Pharmacists in Epilepsy Management at a General Hospital in Vietnam: A Before-and-after Study [NCT04967326]Phase 4141 participants (Actual)Interventional2016-01-01Completed
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 132 participants (Actual)Interventional2022-07-27Completed
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 128 participants (Actual)Interventional2005-11-30Completed
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 147 participants (Actual)Interventional2023-07-12Completed
CSP #428 - Treatment of Seizures in the Elderly Population [NCT00007670]Phase 3720 participants Interventional1998-01-31Completed
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 127 participants (Actual)Interventional2022-01-05Terminated(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 4200 participants (Actual)Interventional2006-05-31Completed
Assessment of the Inter-patient Variability in Clinical Response and Correlated Genetic Variations in Substance Use Disorders [NCT05833399]200 participants (Anticipated)Observational2022-11-28Recruiting
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 136 participants (Actual)Interventional2022-10-06Completed
Lamotrigine in Trigeminal Neuralgia: Efficacy and Safety in Comparison With Carbamazepine [NCT00913107]Phase 2/Phase 321 participants (Actual)Interventional2007-09-30Completed
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)Interventional2008-02-29Completed
A Randomised Controlled Trial of the Ketogenic Diet in the Treatment of Epilepsy in Children Under the Age of Two Years [NCT02205931]Phase 4160 participants (Anticipated)Interventional2015-01-31Recruiting
Effect of Anti-epileptic Drugs on Etonogestrel-releasing Implant Pharmacokinetics in Women With Epilepsy [NCT03307863]Phase 469 participants (Anticipated)Interventional2017-11-01Recruiting
Open-label, Fixed Sequence Crossover Study to Investigate the Effects of Carbamazepine on the Pharmacokinetics of Elinzanetant (BAY 3427080) in Healthy Participants. [NCT05028608]Phase 116 participants (Actual)Interventional2021-09-06Completed
Characterization of Epilepsy Patients At-risk for Adverse Outcomes Related to Switching Antiepileptic Drug Products: BEEP 2b Study [NCT02707965]Phase 121 participants (Actual)Interventional2017-06-08Completed
A Phase 1 Study to Evaluate the Potential Drug Interactions Between ALXN2080 and Itraconazole, Fluconazole, and Carbamazepine in Healthy Adult Participants [NCT06173596]Phase 160 participants (Anticipated)Interventional2023-12-21Not yet recruiting
Fed Bioequivalence Study of Carbamazepine Controlled Release Formulations in Healthy Male Uruguayan Subjects [NCT02132897]Phase 120 participants (Actual)Interventional2014-05-31Completed
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 4100 participants (Anticipated)Interventional2023-03-01Recruiting
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 440 participants (Actual)Interventional2009-01-31Completed
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 113 participants (Actual)Interventional2023-04-17Completed
Efficacy and Safety of Olanzapine in the Extended Treatment for Manic or Mixed Episode of Bipolar I Disorder [NCT00266630]Phase 3139 participants (Actual)Interventional2005-11-30Completed
Treatment for Bipolar Depression: Acute & Prophylactic Efficacy With Citalopram [NCT00562861]Phase 2/Phase 3119 participants (Actual)Interventional2007-11-30Completed
Effect of Carbamazepine and Oxcarbazepine on Serum Neuron-specific Enolase and S100B in Focal Seizures [NCT02705768]Phase 490 participants (Actual)Interventional2016-04-30Completed
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 417 participants (Actual)Interventional2016-10-24Terminated(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 4121 participants (Actual)Interventional2006-05-31Completed
A Sequential, Open-Label Study of the Pharmacokinetics and Safety of Intravenous Carbamazepine Relative to Oral Carbamazepine in Adult Patients With Epilepsy [NCT01079351]Phase 198 participants (Actual)Interventional2007-04-30Completed
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 3295 participants (Actual)Interventional2008-10-31Completed
Assessment of Marketed AEDs in the Human Photosensitivity Proof of Concept Trial [NCT00894010]Phase 26 participants (Actual)Interventional2009-05-31Completed
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 3108 participants (Actual)Interventional2010-06-30Completed
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)Interventional2009-05-31Recruiting
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 182 participants (Actual)Interventional2021-04-26Completed
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 350 participants Interventional2005-02-28Completed
Randomised, Placebo Controlled, Double Blind, Parallel Group 3-Months Study of Carbamazepine Efficacy in Moderate Persistent and Severe Asthma Therapy [NCT00153296]Phase 468 participants Interventional2004-08-31Completed
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)Observational2007-02-28Completed
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 160 participants (Anticipated)Interventional2023-10-09Recruiting
Randomized, Placebo Controlled, Double Blind Study of Carbamazepine in Treatment of Bronchial Asthma [NCT00207428]Phase 465 participants Interventional1999-08-31Completed
Second-Line Treatment Choice for Epilepsy [NCT00208520]60 participants Interventional2003-07-31Active, 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 45 participants (Actual)Interventional2019-08-02Terminated(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)Observational2016-09-30Completed
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 164 participants (Actual)Interventional2006-09-30Completed
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 118 participants (Actual)Interventional2021-12-15Completed
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 1144 participants (Anticipated)Interventional2023-07-04Recruiting
Double-Blind, Randomized, Two Period Crossover Comparison of the Cognitive and Behavioral Effects of Eslicarbazepine Acetate and Carbamazepine in Healthy Adults [NCT02912364]Phase 446 participants (Actual)Interventional2016-07-31Completed
[NCT00004758]Phase 230 participants Interventional1993-11-30Completed
Multicenter, Comparative, Randomized, Open Trial to Evaluate Efficacy and Safety of Levetiracetam Versus Carbamazepine in Post Stroke Late Onset Crisis [NCT00542802]Phase 3630 participants (Anticipated)Interventional2007-09-30Recruiting
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 2144 participants (Actual)Interventional2006-02-28Completed
Carbamazepine and Lorazepam in Outpatient Detoxification [NCT00000441]Phase 40 participants InterventionalCompleted
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 130 participants (Anticipated)Interventional2023-05-08Recruiting
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 4161 participants (Actual)Interventional2006-07-31Completed
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 3888 participants (Actual)Interventional2011-04-30Completed
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 116 participants (Actual)Interventional2022-10-19Completed
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 3583 participants (Actual)Interventional2007-05-31Completed
Olanzapine Plus Carbamazepine Versus Carbamazepine Alone in the Treatment of Manic or Mixed Episodes Associated With Bipolar I Disorder [NCT00190892]Phase 4120 participants Interventional2004-09-30Completed
Carbamazepine Extended-Release for the Treatment of Bipolar Depression [NCT00203567]Phase 425 participants (Actual)Interventional2005-08-31Completed
Pharmacotherapy and Intensive Treatment [NCT00000218]Phase 4353 participants InterventionalCompleted
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 160 participants (Actual)Interventional2012-05-31Completed
Pilot Study on the Response of Inherited Erythromelalgia Patients With NaV1.7 Mutations to Carbamazepine: Clinical Imaging Study [NCT02214615]Phase 42 participants (Actual)Interventional2014-04-30Completed
Carbamazepine Treatment for Cocaine Dependence [NCT00000191]Phase 20 participants Interventional1991-01-31Completed
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 3102 participants Interventional2005-01-31Completed
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 31,701 participants (Actual)Interventional2005-02-28Completed
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 433 participants (Actual)Interventional2005-07-31Completed
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 4361 participants (Actual)Interventional2007-01-31Completed
Effect of Sleeve Gastroctomy on Pharmacokinetics of Paracetamol and Antiepileptic Drugs [NCT03161509]Phase 42 participants (Actual)Interventional2017-07-01Terminated(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)Observational2008-04-30Completed
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 4207 participants (Actual)Interventional2008-03-31Completed
Pharmacokinetic Interaction Study Between Eslicarbazepine Acetate and Carbamazepine in Healthy Subject [NCT02284854]Phase 143 participants (Actual)Interventional2009-07-31Completed
Induction of Drug Metabolism: A Comparative, Pharmacokinetic in Vivo Study of the Effect of Carbamazepine and Oxcarbazepine on CYP3A4. [NCT00260247]Phase 410 participants (Actual)Interventional2005-04-30Completed
TOPAMAX (Topiramate) Monotherapy Comparison Trial to Standard Monotherapy in the Treatment of Newly Diagnosed Epilepsy (RWJ-17021-000); Phase IIIB [NCT00236717]Phase 3865 participants (Actual)Interventional1997-09-30Completed
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 116 participants (Actual)Interventional2012-06-30Completed
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 124 participants (Actual)Interventional2012-05-31Completed
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 132 participants (Actual)Interventional2012-09-01Completed
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 116 participants (Actual)Interventional2023-09-11Completed
Assessment of Cost- Effectiveness Interventions and the Quality of Life in Patients With Mood Disorders Through Resources Available in Brazilian Public Health [NCT02870283]Phase 4107 participants (Actual)Interventional2010-05-31Completed
A Preliminary Study of the Efficacy and Safety of Carbamazepine in Severe Liver Disease Due to Alpha-1 Antitrypsin Deficiency [NCT01379469]Phase 220 participants (Actual)Interventional2012-01-31Terminated
[NCT00381537]92 participants InterventionalCompleted
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 140 participants (Actual)Interventional2022-01-25Completed
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 112 participants (Actual)Interventional2021-07-15Completed
Symptomatic Trigeminal Neuralgia Attributed to Multiple Sclerosis - Clinical Characteristics, Neuroanatomical Abnormalities and Treatment Efficacy [NCT04371575]60 participants (Actual)Observational2012-09-01Completed
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 120 participants (Actual)Interventional2021-03-01Completed
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 172 participants (Actual)Interventional2020-11-05Completed
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 114 participants (Actual)Interventional2022-01-13Completed
The Role of Drug Metabolizing Enzymes in the Pathogenesis Adverse Drug Reactions in Children [NCT00224952]274 participants (Actual)Observational2002-07-31Completed
Open Label Prophylaxis Study of Lithium Plus Extended- Release Carbamazepine (Equetro®) Combination for Rapid Cycling Bipolar Disorder [NCT00325286]Phase 420 participants (Anticipated)Interventional2006-05-31Active, not recruiting
Carbamazepine Treatment of Cocaine Dependence [NCT00000242]Phase 20 participants Interventional1992-10-01Completed
Pharmacotherapy and Intensive Treatment of Drug Abuse [NCT00000217]Phase 20 participants Interventional1990-09-30Completed
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 128 participants (Actual)Interventional2022-10-18Completed
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 115 participants (Actual)Interventional2020-03-31Completed
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 3551 participants (Actual)Interventional2012-05-31Completed
Comparative Efficacy of Carbamazepine Versus Oxcarbazepine in Treatment of Trigeminal Neuralgia- a Randomized Controlled Clinical Study [NCT04996199]Phase 4132 participants (Anticipated)Interventional2021-09-18Recruiting
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
Population Pharmacokinetics of Antiepileptic in Pediatrics [NCT03196466]1,000 participants (Anticipated)Observational2017-06-19Recruiting
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 3436 participants (Actual)Interventional2013-09-30Completed
Electroacupuncture Therapy for Change of Pain in Classical Trigeminal Neuralgia [NCT03580317]120 participants (Actual)Interventional2018-07-12Completed
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 160 participants (Anticipated)Interventional2023-08-15Recruiting
Pharmacological Mechanisms of Low-intensity Focused Ultrasound for Motor Cortex Neuroplasticity [NCT04923659]Early Phase 120 participants (Anticipated)Interventional2021-05-25Recruiting
Electroclinical Effect of Steroid in Patients With Benign Childhood Epilepsy With Centrotemporal Spikes [NCT03490487]Phase 4100 participants (Anticipated)Interventional2018-06-20Recruiting
The Efficacy and Safety of Lamotrigine Versus Carbamazepine in Focal Epilepsy: A Randomized, Open Label Clinical Trial in Dhaka Medical College Hospital [NCT05748236]Phase 470 participants (Anticipated)Interventional2022-11-01Enrolling by invitation
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00224952 (4) [back to overview]Age-related Changes in Bioactivation
NCT00224952 (4) [back to overview]Age-related Changes in Bioactivation
NCT00224952 (4) [back to overview]Drug (Valproic Acid or Carbamazepine) Metabolite Profiles in Urine
NCT00224952 (4) [back to overview]Drug (Valproic Acid or Carbamazepine) Metabolite Profiles in Urine
NCT00266630 (20) [back to overview]Change From Baseline to Endpoint in Young Mania Rating Scale (YMRS) Total Scores - Olanzapine Monotherapy Arm Only
NCT00266630 (20) [back to overview]Number of Participants With Response of Manic Symptoms - Olanzapine Monotherapy Arm Only
NCT00266630 (20) [back to overview]Number of Participants With Treatment-Emergent Akathisia Based on DIEPSS Scores
NCT00266630 (20) [back to overview]Number of Participants With Treatment-Emergent Dyskenisia Based on DIEPSS Scores
NCT00266630 (20) [back to overview]Number of Participants With Treatment-Emergent Dystonia Based on DIEPSS Scores
NCT00266630 (20) [back to overview]Number of Participants With Treatment-Emergent Parkinsonism Based on DIEPSS Scores
NCT00266630 (20) [back to overview]Clinical Global Impressions - Bipolar Version, Severity of Illness (CGI-BP) Overall, Visit Data
NCT00266630 (20) [back to overview]Number of Participants With Potentially Clinically Significant Changes in Laboratory Analytes
NCT00266630 (20) [back to overview]Number of Participants With Potentially Clinically Significant Changes in Vital Signs and Weight
NCT00266630 (20) [back to overview]Number of Participants With Treatment-emergent Abnormal, High, or Low Laboratory Values
NCT00266630 (20) [back to overview]Positive and Negative Syndrome Scale Positive Scores - Visit Data
NCT00266630 (20) [back to overview]Maximum Change From Baseline to Endpoint on the Drug Induced Extra-Pyramidal Symptoms Scale (DIEPSS) - Total Score
NCT00266630 (20) [back to overview]Change From Baseline to Endpoint on the YMRS Total Score - Olanzapine + Mood Stabilizer Only
NCT00266630 (20) [back to overview]Number of Participants Who Experienced Remission of Bipolar Disorder
NCT00266630 (20) [back to overview]Number of Participants Who Experienced Switch to Symptomatic Depression as Measured by the Hamilton Depression Scale - 17 Item Version (HAMD-17)
NCT00266630 (20) [back to overview]Number of Participants Who Switched to Syndromic Depression
NCT00266630 (20) [back to overview]Number of Participants With Potentially Clinically Significant Changes in Electrocardiograms - High Fridericia Corrected QT Interval (QTcF)
NCT00266630 (20) [back to overview]Number of Participants With Relapse of Depressive Symptoms
NCT00266630 (20) [back to overview]Number of Participants With Relapse of Manic Symptoms - Olanzapine Monotherapy Arm Only
NCT00266630 (20) [back to overview]Number of Participants With Remission of Mania - Olanzapine Monotherapy Arm Only
NCT00438451 (12) [back to overview]58-week Retention Rate Measured by the Number of Drop Outs Due to Adverse Events or Seizures From Day 1 of Treatment
NCT00438451 (12) [back to overview]Results of Cognitive Testing (EpiTrack© by UCB) - Changes to Baseline (V0) at Week 58 (V6)
NCT00438451 (12) [back to overview]Results of Cognitive Testing (EpiTrack© by UCB) - Categories at V6
NCT00438451 (12) [back to overview]Portland Neurotoxicity Scale (PNS) at V6
NCT00438451 (12) [back to overview]Time to Drop Out
NCT00438451 (12) [back to overview]QOLIE-31 (Quality Of Life In Epilepsy) Results at V6
NCT00438451 (12) [back to overview]The Time (in Days) to First Break-through Seizure (From Day 1 of Treatment)
NCT00438451 (12) [back to overview]The Absolute Seizure Frequency During the Maintenance Phase (Weeks 7 - 58)
NCT00438451 (12) [back to overview]Results of Cognitive Testing (EpiTrack© by UCB) - Score at V6
NCT00438451 (12) [back to overview]Proportion of Seizure-free Days During the Maintenance Phase for Subjects Who Enter the Maintenance Phase
NCT00438451 (12) [back to overview]Percentage of Patients Remaining Seizure-free at Week 30 (Visit 4)
NCT00438451 (12) [back to overview]Percentage of Patients Remaining Seizure Free at Week 58 (Visit 6)
NCT00477295 (11) [back to overview]Percentage of Participants Who Experienced Seizure Freedom for 26-weeks During the Maintenance Phase
NCT00477295 (11) [back to overview]Time to 12-months Seizure Freedom
NCT00477295 (11) [back to overview]Time to 6-months Seizure Freedom
NCT00477295 (11) [back to overview]Change From Baseline in Bond and Lader VAS Mood Sub-Scores at Maintenance Period Visit 1
NCT00477295 (11) [back to overview]Change From Baseline in SF-36 Aggregate Mental and Physical Component Score at Maintenance Period Visit 1
NCT00477295 (11) [back to overview]Percentage of Participants With EQ-5D Scores at Maintenance Period Visit 1
NCT00477295 (11) [back to overview]Analysis of Time to Drop Out Due to an Adverse Event (AE)
NCT00477295 (11) [back to overview]Analysis of Time to Drop Out Due to Lack of Efficacy
NCT00477295 (11) [back to overview]Change From Baseline in QOLIE-31-P Overall Score at Maintenance Period Visit 1
NCT00477295 (11) [back to overview]Change From Baseline in Total ABNAS Score at Maintenance Period Visit 1
NCT00477295 (11) [back to overview]Percentage of Participants Who Experienced Seizure Freedom for 12-months During the FDP and Maintenance Period
NCT00562861 (1) [back to overview]MADRS Rating Scale Change
NCT00621751 (7) [back to overview]Neuropsychiatric Inventory Irritability-Aggression Domains Composite Measure Completed by Participant [Time Frame: 42 Days]
NCT00621751 (7) [back to overview]Clinicians Global Impression of Change
NCT00621751 (7) [back to overview]Global Impression of Change -- Observer
NCT00621751 (7) [back to overview]Global Impression of Change -- Participant
NCT00621751 (7) [back to overview]Neuropsychiatric Inventory Irritability-Aggression Domains Composite Measure -- Observer
NCT00621751 (7) [back to overview]Proportion of Participants With Minimal Clinically Important Difference -- Observer Rating
NCT00621751 (7) [back to overview]Proportion of Participants With Minimal Clinically Important Difference (MCID) -- Participant
NCT00807989 (3) [back to overview]Retention Rate After 52 Weeks Maintenance Period
NCT00807989 (3) [back to overview]Seizure Free Rate for 52 Weeks at Initial Target Dose
NCT00807989 (3) [back to overview]Seizure Free Rate for 24 Weeks at Initial Target Dose
NCT00848549 (5) [back to overview]Percentage of Participants That Are Seizure Free for at Least 24 Month Consecutive Period in the Base Study and Extension Phase
NCT00848549 (5) [back to overview]Time to Drop-out Due to Lack of Efficacy
NCT00848549 (5) [back to overview]Time to Drop-out Due to Adverse Event (AE)
NCT00848549 (5) [back to overview]Change From Baseline in Quality of Life Assessed by Quality of Life in Epilepsy-Problems Questionnaire (QOLIE-31-P) Overall Score at Each Visit
NCT00848549 (5) [back to overview]Percentage of Participants Remaining in the Study at Each Visit
NCT01127256 (3) [back to overview]Quality of Life in Epilepsy (QoL-QOLIE31)
NCT01127256 (3) [back to overview]The Percentage of Participants With Seizure Free Rate
NCT01127256 (3) [back to overview]The Percentage of Participants With Retention Rate
NCT01128959 (1) [back to overview]Adverse Events
NCT01243177 (6) [back to overview]Number of Subjects Who Withdraw From the Study Due to a Treatment-emergent Adverse Event (AE) During the Treatment Phase (up to 113 Weeks)
NCT01243177 (6) [back to overview]Proportion of Subjects Remaining Seizure Free for 12 Consecutive Months (52 Consecutive Weeks) Following Stabilization at the Last Evaluated Dose for Each Subject
NCT01243177 (6) [back to overview]Number of Subjects With at Least One Treatment-emergent Adverse Event (AE) During the Treatment Phase (up to 113 Weeks)
NCT01243177 (6) [back to overview]Number of Subjects With at Least One Treatment-emergent Serious Adverse Event (SAE) During the Treatment Phase (up to 113 Weeks)
NCT01243177 (6) [back to overview]Proportion of Subjects in the Full Analysis Set (FAS) Remaining Seizure Free for 6 Consecutive Months (26 Consecutive Weeks) of Treatment Following Stabilization at the Last Evaluated Dose for Each Subject
NCT01243177 (6) [back to overview]Proportion of Subjects in the Per Protocol Set (PPS) Remaining Seizure Free for 6 Consecutive Months (26 Consecutive Weeks) of Treatment Following Stabilization at the Last Evaluated Dose for Each Subject
NCT01465997 (3) [back to overview]Number of Subjects Who Withdrew From the Study Due to a Treatment-emergent Adverse Event (AE) During the Treatment Phase (Maximum 3.5 Years)
NCT01465997 (3) [back to overview]Number of Subjects With at Least One Treatment-emergent Adverse Event (AE) During the Treatment Phase (Maximum of 3.5 Years)
NCT01465997 (3) [back to overview]Number of Subjects With at Least One Treatment-emergent Serious Adverse Event (SAE) During the Treatment Phase (Maximum of 3.5 Years)
NCT01954121 (5) [back to overview]Time to First Seizure or Discontinuation Due to an Adverse Event (AE) / Lack of Efficacy (LOE) During the Evaluation Period
NCT01954121 (5) [back to overview]Proportion of Subjects Remaining Seizure Free During the 6-months Evaluation Period
NCT01954121 (5) [back to overview]Proportion of Subjects Retained in the Study for the Duration of the Period Covering the Up Titration Period, Stabilization Period, and Evaluation Period
NCT01954121 (5) [back to overview]Time to First Seizure During the Evaluation Period
NCT01954121 (5) [back to overview]Time to First Seizure During the Period Covering the Up Titration Period, Stabilization Period, and Evaluation Period From the First Dose of Study Drug
NCT02214615 (2) [back to overview]Carbamazepine Affects Pain in Patients With S241T NaV1.7 IEM Mutation
NCT02214615 (2) [back to overview]Carbamazepine Affects Mean Duration of Pain Episode
NCT02284854 (6) [back to overview]AUC0-t (CBZE) - Area Under the Curve to Last Measurable Concentration for CBZE
NCT02284854 (6) [back to overview]AUC0-t (BIA 2-093) - Area Under the Curve to Last Measurable Concentration for BIA 2-093
NCT02284854 (6) [back to overview]AUC0-t (CBZ) - Area Under the Curve to Last Measurable Concentration for CBZ
NCT02284854 (6) [back to overview]Cmax (BIA 2-093) - the Maximum Plasma Concentration
NCT02284854 (6) [back to overview]Cmax (CBZ) - the Maximum Plasma Concentration
NCT02284854 (6) [back to overview]Cmax (CBZE) - the Maximum Plasma Concentration
NCT02707965 (5) [back to overview]Mean AUC0-last_ss (Test vs. Reference)
NCT02707965 (5) [back to overview]Mean Cmax_ss (Test vs. Reference)
NCT02707965 (5) [back to overview]Mean Cmin_ss (Test vs. Reference)
NCT02707965 (5) [back to overview]Number of Seizures Reported
NCT02707965 (5) [back to overview]Number of Adverse Events
NCT02870283 (3) [back to overview]"Number of Participants With Response to Treatment"
NCT02870283 (3) [back to overview]Number of Participants With Remission to Treatment
NCT02870283 (3) [back to overview]Quality of Life - WHOQOL Bref Intrument
NCT02912364 (5) [back to overview]Dual Task Percent of Time in Box.
NCT02912364 (5) [back to overview]Overall Composite Z Score of Neuropsychological Battery as a Measure of Direct Comparison of the 2 Antiepileptic Drugs.
NCT02912364 (5) [back to overview]MCG Paragraph Recall Scores.
NCT02912364 (5) [back to overview]Overall Z-score for Executive Function.
NCT02912364 (5) [back to overview]Profile of Mood States (POMS) Score.
NCT04962230 (18) [back to overview]Tmax of Ritonavir
NCT04962230 (18) [back to overview]Vz/F of Ritonavir
NCT04962230 (18) [back to overview]Apparent Volume of Distribution (Vz/F) of PF-07321332
NCT04962230 (18) [back to overview]Number of Participants With Clinically Significant Change in Electrocardiogram (ECG) Findings
NCT04962230 (18) [back to overview]Number of Participants With Laboratory Abnormalities
NCT04962230 (18) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT04962230 (18) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of PF-07321332
NCT04962230 (18) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-07321332
NCT04962230 (18) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-07321332
NCT04962230 (18) [back to overview]AUCinf of Ritonavir
NCT04962230 (18) [back to overview]AUClast of Ritonavir
NCT04962230 (18) [back to overview]CL/F of Ritonavir
NCT04962230 (18) [back to overview]Cmax of Ritonavir
NCT04962230 (18) [back to overview]Maximum Observed Plasma Concentration (Cmax) of PF-07321332
NCT04962230 (18) [back to overview]t1/2 of Ritonavir
NCT04962230 (18) [back to overview]Terminal Half-Life ( t1/2) of PF-07321332
NCT04962230 (18) [back to overview]Apparent Oral Clearance (CL/F) of PF-07321332
NCT04962230 (18) [back to overview]Number of Participants With Clinically Significant Change From Baseline in Vital Signs
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Drug (Valproic Acid or Carbamazepine) Metabolite Profiles in Urine

1. To examine the individual metabolic profiles of pediatric patients receiving carbamazepine or valproate therapy, in an attempt to determine the identities of the reactive metabolites or, alternatively, the identities of those metabolites that serve as potential precursors to reactive species (e.g., through conjugation with detoxifying compounds such as glutathione). (NCT00224952)
Timeframe: urine samples (overnight collections) collected longitudinally through study completion for time frame ranging from 2-5 years

Interventionnmol per mg creatinine (Mean)
5-N-acetylcysteine-3-ene VPA isomers5-N-acetylcysteine-2-ene VPATotal N-acetylcysteine conjugates
Valproic Acid Phase 21.152.135.88

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Drug (Valproic Acid or Carbamazepine) Metabolite Profiles in Urine

1. To examine the individual metabolic profiles of pediatric patients receiving carbamazepine or valproate therapy, in an attempt to determine the identities of the reactive metabolites or, alternatively, the identities of those metabolites that serve as potential precursors to reactive species (e.g., through conjugation with detoxifying compounds such as glutathione). (NCT00224952)
Timeframe: urine samples (overnight collections) collected longitudinally through study completion for time frame ranging from 2-5 years

,
Interventionnmol per mg creatinine (Mean)
4-Methylthio-2-hydroxyiminostilbene
Carbamazepine Phase 115.2
Carbamazepine Phase 213.1

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Change From Baseline to Endpoint in Young Mania Rating Scale (YMRS) Total Scores - Olanzapine Monotherapy Arm Only

The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. The primary objective was only interested in the effects in the olanzapine monotherapy arm. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionunits on a scale (Mean)
Olanzapine Monotherapy-3.0

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Number of Participants With Response of Manic Symptoms - Olanzapine Monotherapy Arm Only

Defined by a 50% or more reduction in YMRS total score from baseline in Study BMAC to endpoint. The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. The primary objective was only interested in the effects in the olanzapine monotherapy arm. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy97

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Number of Participants With Treatment-Emergent Akathisia Based on DIEPSS Scores

DIEPSS assesses the extrapyramidal symptoms attributable to antipsychotics. Consists of 9 items (8 to assess individual symptoms and 1 to assess global severity). Each item is assessed from 0 (none, normal) to 4 (severe). The total points of 8 items are defined as DIEPSS total (0 to 32 points). The items are classified into 4 categories of parkinsonism, akathisia, dystonia and dyskinesia. Treatment-emergent akathisia was defined as a score of equal or more than 2 or an increase of equal or more than 2 points from baseline on the akathisia item (total score possible 0 to 4 points). (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy3
Olanzapine + Mood Stabilizer2

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Number of Participants With Treatment-Emergent Dyskenisia Based on DIEPSS Scores

DIEPSS assesses the extrapyramidal symptoms attributable to antipsychotics. Consists of 9 items (8 to assess individual symptoms and 1 to assess global severity). Each item is assessed from 0 (none, normal) to 4 (severe). The total points of 8 items are defined as DIEPSS total (0 to 32 points). The items are classified into 4 categories of parkinsonism, akathisia, dystonia and dyskinesia. Treatment-emergent dyskenisia was defined as a score of equal or more than 2 or an increase of equal to or more than 2 points from baseline on the dyskenisia item (total score possible 0 to 4 points). (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy0
Olanzapine + Mood Stabilizer0

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Number of Participants With Treatment-Emergent Dystonia Based on DIEPSS Scores

DIEPSS assesses the extrapyramidal symptoms attributable to antipsychotics. Consists of 9 items (8 to assess individual symptoms and 1 to assess global severity). Each item is assessed from 0 (none, normal) to 4 (severe). The total points of 8 items are defined as DIEPSS total (0 to 32 points). The items are classified into 4 categories of parkinsonism, akathisia, dystonia and dyskinesia. Treatment-emergent dystonia was defined as a score equal or more than 2 or an increase of equal or more than 2 points from baseline on the dystonia item (total score possible 0 to 4 points). (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy0
Olanzapine + Mood Stabilizer1

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Number of Participants With Treatment-Emergent Parkinsonism Based on DIEPSS Scores

DIEPSS assesses the extrapyramidal symptoms attributable to antipsychotics. Consists of 9 items (8 to assess individual symptoms and 1 to assess global severity). Each item is assessed from 0 (none, normal) to 4 (severe). The total points of 8 items are defined as DIEPSS total (0 to 32 points). Parkinsonism is assessed by the total points of items 1 to 5 (total score of 0 to 20). Treatment-emergent parkinsonism was defined as a score of equal or greater than 3 on 1 item, equal or greater than 2 on 2 items, or an increase of equal or greater than 3 from baseline on the parkinsonism total. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy1
Olanzapine + Mood Stabilizer3

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Clinical Global Impressions - Bipolar Version, Severity of Illness (CGI-BP) Overall, Visit Data

Measures severity of the patient's overall severity of bipolar symptoms (1=normal, not at all ill; 7=among the most extremely ill patients). (NCT00266630)
Timeframe: baseline, Weeks 1, 2, 4, 6, 10, 14, 18

,
Interventionunits on a scale (Mean)
baseline1 week2 weeks4 weeks6 weeks10 weeks14 weeks18 weeks endpoint
Olanzapine + Mood Stabilizer4.74.13.73.53.43.03.02.9
Olanzapine Monotherapy1.91.81.81.71.71.71.81.7

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Number of Participants With Potentially Clinically Significant Changes in Laboratory Analytes

Triglycerides: high limit equal to or more than 500 milligram/deciliter (mg/dL); Glucose (non-fasting): low limit 2.4975 mmol/liter (L); high limit 13.875 mmol/L; Glucose (fasting): low limit 2.4975 mmol/L; high limit 6.993 mmol/L. (NCT00266630)
Timeframe: baseline through 18 weeks

,
Interventionparticipants (Number)
High triglycerides; n=100, n=38Low glucose (non-fasting); n=64, n=28High glucose (non-fasting); n=64, n=28Low glucose (fasting); n=40, n=6High glucose (fasting); n=40, n=6
Olanzapine + Mood Stabilizer20000
Olanzapine Monotherapy50003

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Number of Participants With Potentially Clinically Significant Changes in Vital Signs and Weight

Low systolic blood pressure (SBP): <=90 millimeter mercury (mmHg) and decrease of >=20 mmHg; High SBP: >=180 mmHg and increase of >=20 mmHg; Low diastolic blood pressure (DBP): <=50 mmHg and decrease of >=15 mmHg; High DBP: >=105 mmHg and increase of >=15 mmHg; Low pulse: <50 beats per minute (bpm) and decrease of >=15 bpm; High pulse: >120 bpm and an increase of >=15 bpm; Low weight: decrease of >=7%; High weight: increase of >=7%; (NCT00266630)
Timeframe: baseline through 18 weeks

,
Interventionparticipants (Number)
Low systolic blood pressureHigh systolic blood pressureLow diastolic blood pressureHigh diastolic blood pressureLow weightHigh weightLow pulseHigh pulse
Olanzapine + Mood Stabilizer201011000
Olanzapine Monotherapy604131700

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Number of Participants With Treatment-emergent Abnormal, High, or Low Laboratory Values

High density lipoprotein: males low 40 milligram/deciliter (mg/dL), high 80 mg/dL; females low 40 mg/dL, high 90 mg/dL. Low density lipoprotein (LDL): males and females low 70 mg/dL, high 139 mg/dL. Hemoglobin A1C (HBA1C): males and females low 4.3%, high 5.8%. (NCT00266630)
Timeframe: baseline through 18 weeks

,
Interventionparticipants (Number)
Low high density lipoprotein (HDL); n=93, n=36High high density lipoprotein (HDL); n=95, n=37Low low density lipoprotein (LDL); n=97; n=37High low density lipoprotein (LDL); n=71, n=31Low hemoglobin A1C (HBA1C); n=100, n=39High hemoglobin A1C (HBA1C); n=97, n=38
Olanzapine + Mood Stabilizer3111110
Olanzapine Monotherapy10512412

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Positive and Negative Syndrome Scale Positive Scores - Visit Data

Assesses positive symptoms associated with schizophrenia. 7 items make up the Positive scale. Each item is rated on a scale from 1 (symptom not present) to 7 (symptoms extremely severe). Total Positive Subscale scores range from 7 to 49. For the analysis, the score was converted to 0 to 6 for each item range; hence, the total score ranges from 0 to 42. (NCT00266630)
Timeframe: baseline, Weeks 1, 2, 4, 6, 10, 14, 18

,
Interventionunits on a scale (Mean)
baseline1 week2 weeks4 weeks6 weeks10 weeks14 weeks18 week endpoint
Olanzapine + Mood Stabilizer12.510.510.110.110.19.99.99.9
Olanzapine Monotherapy7.77.57.57.47.37.47.47.4

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Maximum Change From Baseline to Endpoint on the Drug Induced Extra-Pyramidal Symptoms Scale (DIEPSS) - Total Score

A scale used to assess the extrapyramidal symptoms attributable to antipsychotics. Consists of 9 items (8 to assess individual symptoms and 1 to assess global severity). Each item is assessed from 0 (none, normal) to 4 (severe). The total points of 8 items are defined as DIEPSS total (0 to 32 points). The items for the assessment of individual symptoms are classified into 4 categories of parkinsonism, akathisia, dystonia and dyskinesia. Parkinsonism is assessed by the total points of items 1 to 5; akathisia, dystonia and dyskinesia are assessed by the points given to the corresponding items. (NCT00266630)
Timeframe: baseline through 18 weeks

,
Interventionunits on a scale (Mean)
BaselineMaximum Change from baseline to endpoint
Olanzapine + Mood Stabilizer0.180.64
Olanzapine Monotherapy0.350.05

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Change From Baseline to Endpoint on the YMRS Total Score - Olanzapine + Mood Stabilizer Only

The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionunits on a scale (Mean)
Olanzapine + Mood Stabilizer-19.8

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Number of Participants Who Experienced Remission of Bipolar Disorder

Participants who had equal to or less than 12 points in YMRS total score and equal to or less than 7 points in HAMD-17 total score at 18 weeks. YMRS: 11-item scale, measures the severity of manic episodes. 4 items are rated from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total: 0 to 60. The 17-item HAMD measures depression severity. Each item was evaluated and scored using a 3-point scale or a 5-point scale. HAMD-17 total score: 0 (normal) to 52 (severe). (NCT00266630)
Timeframe: Week 18

Interventionparticipants (Number)
Olanzapine Monotherapy54
Olanzapine + Mood Stabilizer12

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Number of Participants Who Experienced Switch to Symptomatic Depression as Measured by the Hamilton Depression Scale - 17 Item Version (HAMD-17)

Incidence of depressive symptoms was defined as a score of equal to or more than 13 points on the HAMD-17. The 17-item HAMD measures depression severity. Each item was evaluated and scored a 3-point scale (e.g. absent, mild, marked) or a 5-point scale (e.g. absent, mild, moderate, severe, very severe). The total score of HAMD-17 may range from 0 (normal) to 52 (severe). (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy4
Olanzapine + Mood Stabilizer1

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Number of Participants Who Switched to Syndromic Depression

As defined as a shift from a Manic Episode at baseline to a Major Depressive Episode, at any post baseline visit, based on Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition Text Revision. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy8
Olanzapine + Mood Stabilizer4

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Number of Participants With Potentially Clinically Significant Changes in Electrocardiograms - High Fridericia Corrected QT Interval (QTcF)

High QTcF: more than or equal to 450 milliseconds (msec) for males; more than or equal to 470 milliseconds (msec) for females (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy0
Olanzapine + Mood Stabilizer0

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Number of Participants With Relapse of Depressive Symptoms

Assessed were participants meeting remission criteria for bipolar disorder in Study BMAC and have a HAMD-17 total score greater than or equal to 13 at any time. The 17-item HAMD measures depression severity. Each item was evaluated and scored using a 3-point scale (e.g. absent, mild, marked) or a 5-point scale (e.g. absent, mild, moderate, severe, very severe). The total score of HAMD-17 may range from 0 (normal) to 52 (severe). (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy4

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Number of Participants With Relapse of Manic Symptoms - Olanzapine Monotherapy Arm Only

Patients achieved remission in Study BMAC (defined as YMRS total score <=12 and HAMD-17 total score <=7) and obtained YMRS total score of >=15 at any time during Study BMEX. The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. The primary objective was only interested in the effects in the olanzapine monotherapy arm. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy3

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Number of Participants With Remission of Mania - Olanzapine Monotherapy Arm Only

Remission of Mania was defined as a YMRS total score of less than or equal to 12 at endpoint. The YMRS is an 11-item scale that measures the severity of manic episodes. Four items are rated on a scale from 0 (symptom not present) to 8 (symptom extremely severe). The remaining items are rated on a scale from 0 (symptom not present) to 4 (symptom extremely severe). The YMRS total score ranges from 0 to 60. The primary objective was only interested in the effects in the olanzapine monotherapy arm. (NCT00266630)
Timeframe: baseline through 18 weeks

Interventionparticipants (Number)
Olanzapine Monotherapy93

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58-week Retention Rate Measured by the Number of Drop Outs Due to Adverse Events or Seizures From Day 1 of Treatment

(NCT00438451)
Timeframe: 58 weeks

Interventionproportion of participants (Mean)
Levetiracetam0.61
Carbamazepine0.46
Lamotrigine0.56

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Results of Cognitive Testing (EpiTrack© by UCB) - Changes to Baseline (V0) at Week 58 (V6)

"Evaluation of Changes~Changes in the EpiTrack® Score were categorized as follows:~≥5 score points: Improved;~-3 to 4 score points: Unchanged;~≤-4 score points: Worsened" (NCT00438451)
Timeframe: week 58

,,
Interventionparticipants (Number)
ImprovedUnchangedWorsened
Carbamazepine16568
Lamotrigine155313
Levetiracetam15616

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Results of Cognitive Testing (EpiTrack© by UCB) - Categories at V6

"Evaluation of current testing at V6:~≥29 score points: Inconspicuous; 26 to 28 score points: Borderline;~≤25 score points: Impaired" (NCT00438451)
Timeframe: 58 weeks

,,
Interventionparticipants (Number)
Without pathological findingsBorderlineImpaired
Carbamazepine341733
Lamotrigine311539
Levetiracetam381036

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Portland Neurotoxicity Scale (PNS) at V6

"The PNS is a 15-item scale. Each item can be scored from 1 to 9. There are a total score (includes all items, range:15 to 135) and two subscores: The cognitive toxicity subscore (10 items: Energy Level, Memory, Interest, Concentration, Forgetfulness, Sleepliness, Moodiness, Alertness, Attention Span, Motivation, range:10 to 90) and the somatomoto subscore (5 items: Vision, Walking, Coordination, Tremor, Speech, range:5-45). The score is calculated by taking the mean of all non-missing values times the number of items.~Lower values indicate better quality of life." (NCT00438451)
Timeframe: at week 58

,,
Interventionunits on a scale (Mean)
Cognitive toxicity subscoreSomatomotor subscoreTotal Score
Carbamazepine27.311.438.7
Lamotrigine23.710.834.5
Levetiracetam22.210.532.7

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Time to Drop Out

number of days between randomization and premature discontinuation of the study (NCT00438451)
Timeframe: 58 weeks

Interventiondays (Median)
LevetiracetamNA
Carbamazepine265
LamotrigineNA

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QOLIE-31 (Quality Of Life In Epilepsy) Results at V6

The QOLIE-31 is a 31 item score that measures the quality of life in epilepsy (each item with a range of 0 to 100). There are 7 sub-scores seizure worry (items 11,21,22,23,25), overall quality of life (items 1,14), emotional well-being (items 3,4,5,7,9), energy/fatigue (items 2,6,8,10), cognitive functioning (items 12,15,16,17,18,26), medication effects (items 24,29,30) and social functioning (13,19,20,27,28). These scores were combined to a total score by Total score = seizure worry*0.08 + overall quality of life*0.14 + emotional well-being*0.15 + energy/fatigue*0.12 + cognitive functioning*0.27 + medication effects*0.03 + social functioning*0.21 For all scores, higher values indicate better quality of life. Each score has a possible range from 0 to 100. (NCT00438451)
Timeframe: 58 weeks, final visit

,,
Interventionunits on a scale (Mean)
Seizure worryOverall quality of lifeEmotional well-beingEnergy/fatigueCognitive functioningMedication effectsSocial functioningTotal ScoreHealth Scale
Carbamazepine75.465.069.854.568.970.676.368.965.7
Lamotrigine75.067.167.459.868.072.676.769.167.5
Levetiracetam85.167.272.060.875.177.681.173.969.5

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The Time (in Days) to First Break-through Seizure (From Day 1 of Treatment)

(NCT00438451)
Timeframe: over the whole duration of 58 weeks

Interventiondays (Median)
LevetiracetamNA
CarbamazepineNA
LamotrigineNA

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The Absolute Seizure Frequency During the Maintenance Phase (Weeks 7 - 58)

"Seizure frequency was assessed by investigators in the CRF at the Visits V3, V4, V5 and V6.~The absolute seizure frequency during the maintenance phase was defined as the sum of those entries." (NCT00438451)
Timeframe: over 52 weeks

Interventionnumber of seizures (Number)
Levetiracetam168
Carbamazepine131
Lamotrigine130

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Results of Cognitive Testing (EpiTrack© by UCB) - Score at V6

EPITrack-Score shows the performance of attention and executive functions. Higher values indicate a better performance. The results of EPITrack Score ranges between 7 and 45. (NCT00438451)
Timeframe: week 58

Interventionunits on a scale (Mean)
Levetiracetam26.0
Carbamazepine26.0
Lamotrigine25.4

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Proportion of Seizure-free Days During the Maintenance Phase for Subjects Who Enter the Maintenance Phase

(NCT00438451)
Timeframe: 52 weeks

Interventionproportion of seizure-free days (Number)
Levetiracetam0.99
Carbamazepine0.99
Lamotrigine0.99

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Percentage of Patients Remaining Seizure-free at Week 30 (Visit 4)

Percentage of patients experiencing no seizures until week 30 (Visit 4) and did not discontinue the study until week 30. (NCT00438451)
Timeframe: Week 30

Interventionpercentage of participants (Number)
Levetiracetam48
Carbamazepine39
Lamotrigine49

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Percentage of Patients Remaining Seizure Free at Week 58 (Visit 6)

Percentage of patients experiencing no seizures until week 58 (Visit 6) and did not discontinue the study until week 58. (NCT00438451)
Timeframe: week 58

Interventionpercentage of participants (Number)
Levetiracetam43
Carbamazepine33
Lamotrigine38

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Percentage of Participants Who Experienced Seizure Freedom for 26-weeks During the Maintenance Phase

A subject achieved a 26-week seizure-free period if they were free of all seizures, regardless of seizure type, for 26 weeks while receiving the same dose. The occurrence of seizures was documented in the seizure diary, which was maintained by the subject and reviewed at each following visit. (NCT00477295)
Timeframe: Week 31 through Week 109

InterventionPercentage of Participants (Number)
Zonisamide79.4
Carbamazepine83.7

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Time to 12-months Seizure Freedom

A subject achieved a 12-month seizure-free period if they were free of all seizures, regardless of seizure type, for 12-months while receiving the same dose. The occurrence of seizures was documented in the seizure diary, which was maintained by the subject and reviewed at each following visit. (NCT00477295)
Timeframe: Week 5 through Week 83

InterventionDays (Mean)
Zonisamide399.3
Carbamazepine395.6

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Time to 6-months Seizure Freedom

A subject achieved a 6-months seizure-free period if they were free of all seizures, regardless of seizure type, for 6-months while receiving the same dose. The occurrence of seizures was documented in the seizure diary, which was maintained by the subject and reviewed at each following visit. (NCT00477295)
Timeframe: Week 5 through Week 83

InterventionDays (Mean)
Zonisamide222.7
Carbamazepine220.4

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Change From Baseline in Bond and Lader VAS Mood Sub-Scores at Maintenance Period Visit 1

"The Bond-Lader Visual Analogue Scale (VAS) is made up of 16 pairs of alternative descriptors of mood and attention at either end of a 10 cm line.~Subjects were asked to rate their feelings at the time of assessment by indicating the point on the line which best represent their mood. Each item was scored by measuring the position relative to the left hand end of the line and levels of anxiety, sedation, and dysphoria were then calculated from the combined scores of selected items. The scores ranged from 0 to 100, with a high score reflecting a high level of anxiety, sedation or dysphoria." (NCT00477295)
Timeframe: Baseline and Maintenance Period Visit 1 (Week 31 to Week 83)

,
InterventionScores on a Scale (Mean)
AnxietySedationDysphoria
Carbamazepine-1.993-1.362-3.833
Zonisamide-2.036-0.475-1.930

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Change From Baseline in SF-36 Aggregate Mental and Physical Component Score at Maintenance Period Visit 1

The Short Form 36 Health and Well-Being Questionnaire (SF-36) is a 36-item generic health related QOL instrument covering the following domains: physical functioning, role-physical,bodily pain, general health, social functioning,role-emotional, mental health, and vitality. It yields a profile of eight scores, one for each domain, and physical and mental health summary measures. Each domain is described by a score ranging from 0 to 100, for a range of total possible scoes of 0-400 for physical and 0-400 for mental. An increase represents an improvement, whereas a decrease reflects a worsening. (NCT00477295)
Timeframe: Baseline and Maintenance Period Visit 1 (Week 31 to Week 83)

,
InterventionScores on a Scale (Mean)
Aggregate Mental Component ScoreAggregate Physical Component Score
Carbamazepine2.4952.041
Zonisamide1.0271.895

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Percentage of Participants With EQ-5D Scores at Maintenance Period Visit 1

The European Quality of Life Group 5-Dimension Self-Report Questionnaire (EQ-5D) is a preference based generic health related quality of life (HRQoL) instrument which classifies health states across five domains: mobility, self-care, usual activities, pain/discomfort, and anxiety/depression. Each domain has three levels, they are (1) no problems, (2) some problems, (3) extreme problems. The percentages shown are calculated from the number of subjects at that visit with non-missing data for that score. (NCT00477295)
Timeframe: Week 31 through Week 83

,
InterventionPercentage of Participants (Number)
Mobility: No problemsMobility: Some problemsMobility: Confined to BedSelf-Care:No problemsSelf-Care: Some problemsSelf-Care: Unable to wash or dressUsual Activities: No problemsUsual Activities: Some problemsUsual Activities: Unable to performPain/Discomfort: NonePain/Discomfort: ModeratePain/Discomfort: ExtremeAnxiety/Depression: NoneAnxiety/Depression: ModerateAnxiety/Depression: Extreme
Carbamazepine86.712.90.597.62.40.084.815.20.073.225.41.462.934.82.4
Zonisamide90.88.70.596.72.70.589.19.81.175.522.32.264.331.34.4

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Analysis of Time to Drop Out Due to an Adverse Event (AE)

An AE is defined as any untoward medical occurrence in a subject and does not necessarily have a causal relationship with the medicinal product. Adverse events were identified by: any unfavorable or unintended sign, symptom or disease temporarily associated with the use of a medicinal product; any new disease or exacerbation of an existing disease; any deterioration in nonprotocol-required measurements of laboratory values or other clinical test; and recurrence of an intermittent medical condition not present at Baseline. (NCT00477295)
Timeframe: Week 1 through Week 109

InterventionMedian Days (Median)
ZonisamideNA
CarbamazepineNA

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Analysis of Time to Drop Out Due to Lack of Efficacy

Lack of efficacy was evaluated by the subject and on the basis of whether zonisamide and carbamazepine gave the subject at least a 26-week seizure free rate. The subject could withdraw at any time due to lack of efficacy. (NCT00477295)
Timeframe: Week 1 through Week 109

InterventionMedian Days (Median)
Zonisamide722
CarbamazepineNA

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Change From Baseline in QOLIE-31-P Overall Score at Maintenance Period Visit 1

"The Quality of Life in Epilepsy - Problems(QOLIE-31-P) was completed by the patient and contained 30 items covering seven subscales(seizure worry, overall~Quality of Life (QOL),emotional well-being,energy-fatigue, cognition,medication effects and social function) and one item covering health status. It also included seven items addressing overall distress related to each subscale, an item addressing the relative importance of each subscale topic, and an item addressing perception of overall change in QOL at the end of the study. A high score reflects a good QOL. The following scale range is a sample of 1 of the 7 of the subscales:~10 (Best possible quality of life) - 0 (Worst possible quality of life);~Rand Corporation QOLIE-31 Scoring Manual was used. The QOLIE-31 overall score is calculated by summing the product of each scale score times its weight and summing overall all scales." (NCT00477295)
Timeframe: Baseline and Maintenance Period Visit 1 (Week 31 to Week 83)

InterventionScores on a Scale (Mean)
Zonisamide4.474
Carbamazepine6.090

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Change From Baseline in Total ABNAS Score at Maintenance Period Visit 1

The Aldenkamp-Baker Neuropsychological Assessment Scale(ABNAS) is a subject based questionnaire to measure subjective perceived drug-related cognitive impairments. The ABNAS measured seven critical domains of cognition(tiredness/fatigue,hyperexcitability, slowing(mental and motor),memory impairment,attention disorders,impairment of motor coordination, and language disorders). The total score ranged from 0 to 72, with a higher score reflecting a high level of problems. (NCT00477295)
Timeframe: Baseline and Maintenance Period Visit 1 (Week 31 to Week 83)

InterventionScores on a Scale (Mean)
Zonisamide1.6
Carbamazepine-0.1

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Percentage of Participants Who Experienced Seizure Freedom for 12-months During the FDP and Maintenance Period

A subject achieved a 12-month seizure-free period if they were free of all seizures, regardless of seizure type, for 12 months while receiving the same dose. The occurrence of seizures was documented in the seizure diary, which was maintained by the subject and reviewed at each following visit. (NCT00477295)
Timeframe: Week 5 through Week 109

InterventionPercentage of participants (Number)
Zonisamide67.6
Carbamazepine74.7

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MADRS Rating Scale Change

Montgomery Asberg Depression Rating scale assessed in mixed effects regression model. The total range for the scale is 0 to 60. Lower values involve less depression, while higher values involve worse depression. The change in the MADRS scale is interpreted as higher values meaning better outcomes, because more depressive symptoms are improved. (NCT00562861)
Timeframe: 6 weeks

Interventionunits on a scale (Mean)
Citalopram13.1
Placebo15.2

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Neuropsychiatric Inventory Irritability-Aggression Domains Composite Measure Completed by Participant [Time Frame: 42 Days]

Neuropsychiatry Inventory-Irritability (NPI-I) & Aggression domains (NPI-A): NPI is a 40-item assessment of 12 behavioral domains (NPI-I & NPI-A domains used in this study). The most problematic aspect of each domain is graded for severity (1=mild, to 3=severe) and frequency (1-4 with 4 representing highest frequency); the domain scores (0-12) are the product of severity and frequency. To best reflect treatment target intent and meet parametric statistical method criteria, a composite measure of participant-rated NPI-I & -A domains transformed to a Rasch logit scale running from 0 (best) to 100 (worse) units (i.e., participant-rated NPI-I/A Rasch construct scores). Mean day-42 participant-rated NPI-I/A Rasch construct scores were compared between placebo vs. CBZ using ANCOVA with baseline score as covariate. (NCT00621751)
Timeframe: Day 42

Interventionscore on a scale (Least Squares Mean)
Carbamazepine37.5
Placebo36.4

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Clinicians Global Impression of Change

Study physician's impression of change since study onset. Clinicians Global Impressions of Change (CGI) is a sensitive, standardized tool to assess psychopharmacologic treatment response completed by the study physician. The Global Improvement (GI) CGI subscale documented the clinician's impression of change. The GI uses a 7-point scale to assess beneficial and negative effects. Low GI values (1 -3) indicate improvement; higher values (4-7) represent worsening. (NCT00621751)
Timeframe: 42 days

Interventionunits on a scale (Mean)
Carbamazepine3.1
Placebo2.9

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Global Impression of Change -- Observer

Global Impression of Change (GIC) is a 5-item Likert Scale rated participants and observer impression of change in the person with TBI. Responses range 1 = much improved to 5 = much worse. (NCT00621751)
Timeframe: 42 days

Interventionunits on a scale (Mean)
Carbamazepine3.3
Placebo3.1

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Global Impression of Change -- Participant

Global Impression of Change (GIC) is a 5-item Likert Scale rated participants and observer impression of change in the person with TBI. Responses range 1 = much improved to 5 = much worse. (NCT00621751)
Timeframe: Day-42

Interventionscore on a scale (Mean)
Carbamazepine3.1
Placebo3.1

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Neuropsychiatric Inventory Irritability-Aggression Domains Composite Measure -- Observer

Neuropsychiatry Inventory-Irritability (NPI-I) & Aggression domains (NPI-A): NPI is a 40-item assessment of 12 behavioral domains (NPI-I & NPI-A domains used in this study). The most problematic aspect of each domain is graded for severity (1=mild, to 3=severe) and frequency (1-4 with 4 representing highest frequency); the domain scores (0-12) are the product of severity and frequency. To best reflect treatment target intent and meet parametric statistical method criteria, the primary outcome was a composite measure of observer-rated NPI-I & -A domains transformed to a Rasch logit scale running from 0 (best) to 100 (worse) units (i.e., observer-rated NPI-I/A Rasch construct scores). Mean day-42 observer-rated NPI-I/A Rasch construct scores were compared between placebo vs. carbamazepine using ANCOVA with baseline score as covariate. (NCT00621751)
Timeframe: 42 days

Interventionscore on a scale (Least Squares Mean)
Carbamazepine37.7
Placebo36.7

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Proportion of Participants With Minimal Clinically Important Difference -- Observer Rating

Proportion of participants with Minimal Clinically Important Difference (MCID) on Neuropsychiatric Inventory Irritability-Aggression Composite Measure completed by Observer. Specifically, the proportion of participants that experienced a decrease of > 1 (MCID) in the NPI-I/A Rasch construct score (i.e., participants that are considered to have meaningful reduction in irritability/aggression) from baseline to day-42 between the groups using a chi-square test. MCID was defined as 0.5 times the standard deviation of baseline scores. (NCT00621751)
Timeframe: 42-day

InterventionParticipants (Count of Participants)
Carbamazepine20
Placebo26

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Proportion of Participants With Minimal Clinically Important Difference (MCID) -- Participant

Proportion of participants with Minimal Clinically Important Difference (MCID) on Neuropsychiatric Inventory Irritability-Aggression Composite Measure completed by Participant. Specifically, the proportion of participants that experienced a decrease of > 1 (MCID) in the NPI-I/A Rasch construct score (i.e., participants that are considered to have meaningful reduction in irritability/aggression) from baseline to day-42 between the groups using a chi-square test. MCID was defined as 0.5 times the standard deviation of baseline scores. (NCT00621751)
Timeframe: Day-42

InterventionParticipants (Count of Participants)
Carbamazepine21
Placebo16

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Retention Rate After 52 Weeks Maintenance Period

* Retention rate means completion rate (CR), the proportion of patients who have completed the 60-week study as planned. (NCT00807989)
Timeframe: 52 weeks

Interventionparticipants (Number)
Carbamazepine104
Lamotrigine/Valproate98

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Seizure Free Rate for 52 Weeks at Initial Target Dose

(NCT00807989)
Timeframe: 52 weeks

Interventionparticipants (Number)
Carbamazepine43
Lamotrigine/Valproate50

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Seizure Free Rate for 24 Weeks at Initial Target Dose

(NCT00807989)
Timeframe: 24 weeks

Interventionparticipants (Number)
Carbamazepine51
Lamotrigine/Valproate59

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Percentage of Participants That Are Seizure Free for at Least 24 Month Consecutive Period in the Base Study and Extension Phase

The number of participants that have remained seizure free for at least a 24 month consecutive period from the start of the Flexible Dosing Period (FDP: the period following the Titration Period and leading into the Maintenance Period) in the base study through the treatment period of this study. Seizure freedom was defined as the absence of all seizure regardless of seizure type. (NCT00848549)
Timeframe: Week 5 to Week 109 (in base study) and Month 1 to Month 27 (in extension phase)

InterventionPercentage of Participants (Number)
Zonisamide32.3
Carbamazepine35.2

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Time to Drop-out Due to Lack of Efficacy

Lack of efficacy was if the subject had poor seizure control (defined as experiencing a seizure despite being on the maximum dose for = 2 weeks). The subject could withdraw at any time due to lack of efficacy. (NCT00848549)
Timeframe: Week 1 to Week 109 (in core study) and Month 1 to Month 27 (in extension study)

InterventionDays (Mean)
Zonisamide297.9
Carbamazepine289.0

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Time to Drop-out Due to Adverse Event (AE)

"Adverse events in study subjects included any change in the subject's condition.~This includes symptoms, physical findings, or clinical syndromes. All AEs that occurred after signing of informed consent through the last visit and for 15 days following study drug discontinuation were captured on the AE Case Report Form (CRF)." (NCT00848549)
Timeframe: Week 1 to Week 109 (in base study) and Month 1 to Month 27 (in extension study)

InterventionDays (Mean)
Zonisamide131.9
Carbamazepine97.2

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Change From Baseline in Quality of Life Assessed by Quality of Life in Epilepsy-Problems Questionnaire (QOLIE-31-P) Overall Score at Each Visit

The QOLIE-31-P is a 31-item questionnaire evaluating a participant's QOL perception in 7 domains: seizure worry,emotional well being,energy/fatigue, cognitive functioning, medication effects, social functioning,overall QOL. The overall score is derived by weighing and then summing the 7 domain scores. Precoded numeric values for some domains are such that a higher number reflects a more favorable health state; others are such that a higher number reflects a less favorable state. Precoded values are converted to 0-100 point scores; higher converted scores always reflect better QOL. (NCT00848549)
Timeframe: Weeks 0, 26, 52, 78 and 117

,
InterventionScore on a scale (Mean)
Week 0Week 26Week 52Week 78Week 117
Carbamazepine7.10110.95611.6871.90215.849
Zonisamide4.6976.1018.6024.287-0.292

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Percentage of Participants Remaining in the Study at Each Visit

The retention rate is defined as the percentage of subjects remaining on the study at each visit, starting from the first dose of study drug in the extension phase. (NCT00848549)
Timeframe: At 3, 6, 9, 12, 15, 18, 21, 24, and 27 months

,
InterventionPercentage of Participants (Number)
3 months6 months9 months12 months15 months18 months21 months24 months27 months
Carbamazepine93.784.275.361.443.727.812.72.50.6
Zonisamide95.687.676.658.438.727.713.15.81.5

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Quality of Life in Epilepsy (QoL-QOLIE31)

Quality of life assessment tool. Overall scores is calculated by summing subsections, and it ranges from 0 to 100. Higher score presents higher quality of life. (NCT01127256)
Timeframe: 24 weeks

,
InterventionUnits On a Scale (Mean)
Pre-QOLIE 31Post-QOLIE 31
Carbamazepine61.9669.51
Zonisamide60.7267.27

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The Percentage of Participants With Seizure Free Rate

The percentage of participants who had no seizure during the trial. (NCT01127256)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
Zonisamide73.7
Carbamazepine83.1

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The Percentage of Participants With Retention Rate

The percentage of participants who completed the trial. (NCT01127256)
Timeframe: 24 weeks

Interventionpercentage of participants (Number)
Zonisamide59.4
Carbamazepine62.5

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Adverse Events

(NCT01128959)
Timeframe: Baseline to after last iv dose on day 4

InterventionNumber of adverse events (Number)
Intravenous Carbamazepine (IV CBZ) 15 Minutes Infusion126
Intravenous Carbamazepine (IV CBZ) 5 Minutes Infusion26

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Number of Subjects Who Withdraw From the Study Due to a Treatment-emergent Adverse Event (AE) During the Treatment Phase (up to 113 Weeks)

An Adverse Event is any untoward medical occurrence in a patient or clinical investigation subject administered a pharmaceutical product which does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product. Treatment-emergent AEs were defined as AEs that started on or after the date of first dose of study medication and within 30 days following the date of final study medication administration, or AEs whose intensity worsened on or after the date of first dose of study medication and within 30 days following the date of last dose. (NCT01243177)
Timeframe: Duration of the Treatment Phase (up to 113 weeks)

InterventionParticipants (Number)
Lacosamide47
Carbamazepine-Controlled Release (CBZ-CR)69

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Proportion of Subjects Remaining Seizure Free for 12 Consecutive Months (52 Consecutive Weeks) Following Stabilization at the Last Evaluated Dose for Each Subject

The proportion of subjects remaining seizure free for 12 months (52 weeks) was estimated using Kaplan-Meier methods. (NCT01243177)
Timeframe: 12 consecutive months of treatment following stabilization at the last evaluated dose for each subject

Interventionpercentage of subjects (Number)
Lacosamide77.8
Carbamazepine-Controlled Release (CBZ-CR)82.7

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Number of Subjects With at Least One Treatment-emergent Adverse Event (AE) During the Treatment Phase (up to 113 Weeks)

An Adverse Event is any untoward medical occurrence in a patient or clinical investigation subject administered a pharmaceutical product which does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product. Treatment-emergent AEs were defined as AEs that started on or after the date of first dose of study medication and within 30 days following the date of final study medication administration, or AEs whose intensity worsened on or after the date of first dose of study medication and within 30 days following the date of last dose. (NCT01243177)
Timeframe: Duration of the Treatment Phase (up to 113 weeks)

InterventionParticipants (Number)
Lacosamide328
Carbamazepine-Controlled Release (CBZ-CR)332

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Number of Subjects With at Least One Treatment-emergent Serious Adverse Event (SAE) During the Treatment Phase (up to 113 Weeks)

"An Adverse Event is any untoward medical occurrence in a patient or clinical investigation subject administered a pharmaceutical product which does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product.~A Serious Adverse Event must meet 1 or more predefined criteria like death, life-threatening, etc. Treatment-emergent AEs were defined as AEs that started on or after the date of first dose of study medication and within 30 days following the date of final study medication administration, or AEs whose intensity worsened on or after the date of first dose of study medication and within 30 days following the date of last dose." (NCT01243177)
Timeframe: Duration of the Treatment Phase (up to 113 weeks)

InterventionParticipants (Number)
Lacosamide32
Carbamazepine-Controlled Release (CBZ-CR)43

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Proportion of Subjects in the Full Analysis Set (FAS) Remaining Seizure Free for 6 Consecutive Months (26 Consecutive Weeks) of Treatment Following Stabilization at the Last Evaluated Dose for Each Subject

The proportion of subjects remaining seizure free for 6 months (26 weeks) was estimated using Kaplan-Meier methods. (NCT01243177)
Timeframe: 6 consecutive months (26 consecutive weeks) of treatment following stabilization at the last evaluated dose for each subject

Interventionpercentage of subjects (Number)
Lacosamide89.8
Carbamazepine-Controlled Release (CBZ-CR)91.1

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Proportion of Subjects in the Per Protocol Set (PPS) Remaining Seizure Free for 6 Consecutive Months (26 Consecutive Weeks) of Treatment Following Stabilization at the Last Evaluated Dose for Each Subject

The proportion of subjects remaining seizure free for 6 months (26 weeks) was estimated using Kaplan-Meier methods. (NCT01243177)
Timeframe: 6 consecutive months (26 consecutive weeks) of treatment

Interventionpercentage of subjects (Number)
Lacosamide91.4
Carbamazepine-Controlled Release (CBZ-CR)92.8

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Number of Subjects Who Withdrew From the Study Due to a Treatment-emergent Adverse Event (AE) During the Treatment Phase (Maximum 3.5 Years)

Treatment-emergent AEs were defined as those events which started on or after the date of first dose of SP0994 study medication, or events in which severity worsened on or after the date of first dose of SP0994 study medication. AEs which occurred within 30 days after last dose of study medication were considered treatment emergent. (NCT01465997)
Timeframe: Up to 3.5 Years (Duration of the Treatment Phase)

InterventionParticipants (Count of Participants)
Lacosamide12
Carbamazepine-Controlled Release (CBZ-CR)21

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Number of Subjects With at Least One Treatment-emergent Adverse Event (AE) During the Treatment Phase (Maximum of 3.5 Years)

Treatment-emergent AEs were defined as those events which started on or after the date of first dose of SP0994 study medication, or events in which severity worsened on or after the date of first dose of SP0994 study medication. AEs which occurred within 30 days after last dose of study medication were considered treatment emergent. (NCT01465997)
Timeframe: Up to 3.5 Years (Duration of the Treatment Phase)

InterventionParticipants (Count of Participants)
Lacosamide (SS)181
Carbamazepine-Controlled Release (CBZ-CR) (SS)182

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Number of Subjects With at Least One Treatment-emergent Serious Adverse Event (SAE) During the Treatment Phase (Maximum of 3.5 Years)

A Serious Adverse Event is any untoward medical occurrence that at any dose results in death, is life threatening, requires in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity is a congenital anomaly/birth defect. (NCT01465997)
Timeframe: Up to 3.5 Years (Duration of the Treatment Phase)

InterventionParticipants (Count of Participants)
Lacosamide32
Carbamazepine-Controlled Release (CBZ-CR)22

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Time to First Seizure or Discontinuation Due to an Adverse Event (AE) / Lack of Efficacy (LOE) During the Evaluation Period

Number of qualifying events is reported because it is the only descriptive measure available from the proportional hazards model, that was applied. (NCT01954121)
Timeframe: From first day in the Evaluation Period (Week 4) up to end of the Evaluation Period (Week 30)

Interventionevents (Number)
Levetiracetam (Per Protocol Set)88
Carbamazepine-IR (Per Protocol Set)45

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Proportion of Subjects Remaining Seizure Free During the 6-months Evaluation Period

(NCT01954121)
Timeframe: 6-months Evaluation Period (From Week 4 to Week 30)

Interventionpercentage of subjects (Number)
Levetiracetam (Per Protocol Set)47.3
Carbamazepine-IR (Per Protocol Set)68.4

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Proportion of Subjects Retained in the Study for the Duration of the Period Covering the Up Titration Period, Stabilization Period, and Evaluation Period

(NCT01954121)
Timeframe: From Week 1 to Week 30

Interventionpercentage of subjects (Number)
Levetiracetam (Per Protocol Set)48.4
Carbamazepine-IR (Per Protocol Set)70.2

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Time to First Seizure During the Evaluation Period

Number of qualifying events is reported because it is the only descriptive measure available from the proportional hazards model, that was applied. (NCT01954121)
Timeframe: From first day in the Evaluation Period (Week 4) up to end of the Evaluation Period (Week 30)

Interventionevents (Number)
Levetiracetam (Per Protocol Set)87
Carbamazepine-IR (Per Protocol Set)39

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Time to First Seizure During the Period Covering the Up Titration Period, Stabilization Period, and Evaluation Period From the First Dose of Study Drug

Number of qualifying events is reported because it is the only descriptive measure available from the proportional hazards model, that was applied. (NCT01954121)
Timeframe: From Randomization (Week 1) up to Evaluation Visit (Week 30)

Interventionevents (Number)
Levetiracetam (Per Protocol Set)97
Carbamazepine-IR (Per Protocol Set)57

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Carbamazepine Affects Mean Duration of Pain Episode

(NCT02214615)
Timeframe: 15 days

,
Interventionminutes (Number)
Mean episode duration with CarbamazepineMean episode duration with placebo
Carbamazepine Then Placebo274.1615
Placebo Then Carbamazepine45.391.5

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AUC0-t (CBZE) - Area Under the Curve to Last Measurable Concentration for CBZE

"Reference - Day 28 following twice-daily oral administration of CBZ 400 mg Test - Day 35 following twice-daily oral administration of CBZ 400 mg~CBZE - carbamazepine-epoxide is the active metabolite of CBZ" (NCT02284854)
Timeframe: Day 28 to 35

Interventionng*h/mL (Mean)
AUC0-t CBZE (D28 CBZ 400 mg twice-daily)AUC0-t CBZE (D35 CBZ 400 mg twice-daily)
Group B1532214953

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AUC0-t (BIA 2-093) - Area Under the Curve to Last Measurable Concentration for BIA 2-093

Reference - Day 7 following once-daily oral administration of ESL 800 mg Test - Day 35 following once-daily oral administration of ESL 800 mg (NCT02284854)
Timeframe: Day 7 to 35

Interventionng*h/mL (Mean)
AUC0-t ESL (D7 ESL 800mg)AUC0-t ESL (D35 ESL 800mg)
Group A276836188648

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AUC0-t (CBZ) - Area Under the Curve to Last Measurable Concentration for CBZ

Reference - Day 28 following twice-daily oral administration of CBZ 400 mg Test - Day 35 following twice-daily oral administration of CBZ 400 mg (NCT02284854)
Timeframe: Day 28 to 35

Interventionng*h/mL (Mean)
AUC0-t CBZ (D28 CBZ 400 mg twice-daily)AUC0-t CBZ (D35 CBZ 400 mg twice-daily)
Group B10449494394

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Cmax (BIA 2-093) - the Maximum Plasma Concentration

Reference - Day 7 following once-daily oral administration of ESL 800 mg Test - Day 35 following once-daily oral administration of ESL 800 mg (NCT02284854)
Timeframe: Day 7 to 35

Interventionng/mL (Mean)
Cmax ESL (D7 ESL 800mg)Cmax ESL (D35 ESL 800mg)
Group A1860114591

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Cmax (CBZ) - the Maximum Plasma Concentration

Reference - Day 28 following twice-daily oral administration of CBZ 400 mg Test - Day 35 following twice-daily oral administration of CBZ 400 mg (NCT02284854)
Timeframe: Day 28 to 35

Interventionng/mL (Mean)
Cmax CBZ (D28 CBZ 400 mg twice-daily)Cmax CBZ (D35 CBZ 400 mg twice-daily)
Group B104149719

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Cmax (CBZE) - the Maximum Plasma Concentration

"Reference - Day 28 following twice-daily oral administration of CBZ 400 mg twice-daily Test - Day 35 following twice-daily oral administration of CBZ 400 mg twice-daily~CBZE - carbamazepine-epoxide is the active metabolite of CBZ" (NCT02284854)
Timeframe: Day 28 to 35

Interventionng/mL (Mean)
Cmax CBZE (D28 CBZ 400 mg twice-daily)Cmax CBZE (D35 CBZ 400 mg twice-daily)
Group B15621560

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Mean AUC0-last_ss (Test vs. Reference)

Average AUC (area under the drug plasma curve. (NCT02707965)
Timeframe: For all study drugs, time points are: predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, and 6 hr postdose. For twice-a-day regimen, additional points are:8, 10, and 12 hr postdose. For once-a-day drugs, additional times are:8, 10, 12, 16, and 24 hr postdose.

,,,,,,
Interventionmicro/mL/hr (Mean)
Test ProductReference Product
Carbamazepine ER Capsule114.96106.45
Carbamazepine ER Tablet104.6115.16
Lamotrigine ER Tablet62.7666666767.19333333
Levetiracetam ER Tablet260.3262.305
Levetiracetam IR Tablet419.97445.2
Topiramate Tablet92.88494.456
Zonisamide Capsule233.16226.14

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Mean Cmax_ss (Test vs. Reference)

Average maximum drug plasma concentration; (NCT02707965)
Timeframe: For all study drugs, time points are: predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, and 6 hr postdose. For twice-a-day regimen, additional points are:8, 10, and 12 hr postdose. For once-a-day drugs, additional times are:8, 10, 12, 16, and 24 hr postdose.

,,,,,,
Interventionmicrog/mL (Mean)
Test ProductReference Product
Carbamazepine ER Capsule10.959.91
Carbamazepine ER Tablet10.0010.6
Lamotrigine ER Tablet6.246.903333333
Levetiracetam ER Tablet31.0528.04
Levetiracetam IR Tablet71.0233333369.29333333
Topiramate Tablet9.8749.646
Zonisamide Capsule12.2911.68

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Mean Cmin_ss (Test vs. Reference)

Average minimum drug plasma concentration (Cmin); (NCT02707965)
Timeframe: For all study drugs, time points are: predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, and 6 hr postdose. For twice-a-day regimen, additional points are:8, 10, and 12 hr postdose. For once-a-day drugs, additional times are:8, 10, 12, 16, and 24 hr postdose.

,,,,,,
Interventionmicrog/mL (Mean)
Test ProductReference Product
Carbamazepine ER Capsule8.567.66
Carbamazepine ER Tablet7.377.97
Lamotrigine ER Tablet4.0533333334.21
Levetiracetam ER Tablet12.60514.395
Levetiracetam IR Tablet15.4533333317.45666667
Topiramate Tablet6.3266.53
Zonisamide Capsule8.468.34

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Number of Seizures Reported

Number of seizures reported in all groups (NCT02707965)
Timeframe: Through the approximately 2 week period when the treatment is given.

,,,,,,,,
InterventionNumber of Seizures (Number)
Reference ProductTest (Generic)
Carbamazepine ER Capsule31
Carbamazepine ER Tablet00
Lamotrigine ER Tablet Group4425
Lamotrigine IR Tablet Group00
Levetiracetam ER Tablet Group4272
Levetiracetam IR Tablet Group165
Topiramate Tablet Group95
Valproic Acid ER Tablet Group120
Zonisamide Capsule Group00

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Number of Adverse Events

summed for each anti-epileptic drug from when taking brand and generic. (NCT02707965)
Timeframe: Through the approximately 2 week period when the treatment is given.

Interventionevents (Number)
Topiramate29
Lamotrigine ER9
Levetiracetam IR17
Levetiracetam ER4
Carbamazepine ER Capsule15
Zonisamide6
Carbamazepine ER Tablet10
Valproic Acid10

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"Number of Participants With Response to Treatment"

"Response to treatment was defined as a 50% reduction from baseline scores in Hamilton Rating Scale for Depression (HRSD)and Young Mania Rating Scale (YMRS) scales HRSD was developed to evaluate and quantify depression.Its abbreviated version,. Scoring is based on the 17-item scale and scores of 0-7 are considered as being normal. The cutoff points are: 8-17 for mild depression,18-24 for moderate depression, and 25 or more for severe depression. The maximum score being 52 on the 17-point scale.~YMRS is is the most widely used assessment tool for manic symptoms. The scale consists of 11 items .The YMRS follows the style of the Hamilton Rating Scale for Depression (HAM-D) with each item given a severity rating. There are four items that are graded on a 0 to 8 scale (irritability, speech, thought content, and disruptive/agressive behavior), while the remaining seven items are graded on a 0 to 4 scale. Scores of YMRS > 20 generates indicate mania" (NCT02870283)
Timeframe: 8 weeks

InterventionParticipants (Count of Participants)
Lithium31
Acid Valproic28
Carbamazepine27

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Number of Participants With Remission to Treatment

The remission outcome was established as obtaining three consecutive visits with scores of values considered asymptomatic Hamilton Rating Scale for Depression(HRSD <7 points) and Young Mania Rating Scale (YMRS <6 points) during the trial. The subjects that were asymptomatic for at least 6-8 month were considered to be in partial remission and complete if at least 12 months without symptoms, according to Diagnostic and Statistical Manual of Mental Disorders (DSM-IV). (NCT02870283)
Timeframe: 8 months

InterventionParticipants (Count of Participants)
Lithium10
Acid Valproic9
Carbamazepine9

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Quality of Life - WHOQOL Bref Intrument

Quality of Life - WHOQOL -BREF instrument scores scores 0-20 . higher scores mean a better outcome. The quality of life was assessed for entire algorithm. There were no comparisons between each arms of the study. (NCT02870283)
Timeframe: 12 weeks

Interventionscore on a scale (Mean)
Lithium10.91
Acid Valproic10.91
Carbamazepine10.91

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Dual Task Percent of Time in Box.

"Participants were asked to use their computer mouse to keep the cursor inside a moving box on the computer screen while simultaneously responding with a button press when a number on the screen exceeded a certain value.~Assessments were performed prior to treatment (non-drug condition average) and at the end of each treatment period." (NCT02912364)
Timeframe: Prior to treatment (non-drug condition average) and at the end of each six-week treatment period.

Interventionpercentage of time in box (Mean)
Non-drug Condition Average62
Eslicarbazepine62
Carbamazepine60

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Overall Composite Z Score of Neuropsychological Battery as a Measure of Direct Comparison of the 2 Antiepileptic Drugs.

Z score of cognitive tests at end of each 6-week drug treatment period for each intervention (i.e., Eslicarbazepine and Carbamazepine). The Z-score indicates the number of standard deviations away from a reference population. A Z-score of 0 is equal to the mean. Negative numbers indicate poor cognitive performance compared to the mean and positive numbers represent higher cognitive performance compared to the mean. (NCT02912364)
Timeframe: At the end of each 6-week drug treatment period.

InterventionZ-score (Mean)
Eslicarbazepine.001
Carbamazepine-.23

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MCG Paragraph Recall Scores.

"Participants were read a paragraph and were asked to recall content immediately following and twenty minutes after hearing the reading. MCG = Medical College of Georgia.~Assessments were performed prior to treatment (non-drug condition average) and at the end of each treatment period. Score range: 0 - 60, higher scores indicate better memory function." (NCT02912364)
Timeframe: Prior to treatment (non-drug condition average) and at the end of each six-week treatment period.

,,
Interventionunits on a scale (Mean)
Immediate RecallDelayed Recall
Carbamazepine3130
Eslicarbazepine3331
Non-drug Condition Average3433

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Overall Z-score for Executive Function.

Executive function consists of a composite of measures from the computerized cognitive tests. The Z-score indicates the number of standard deviations away from a reference population. A Z-score of 0 is equal to the mean. Negative numbers indicate poor cognitive performance compared to the mean and positive numbers represent higher cognitive performance compared to the mean. (NCT02912364)
Timeframe: At the end of each 6-week drug treatment period.

InterventionZ-score (Mean)
Eslicarbazepine.22
Carbamazepine-.32

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Profile of Mood States (POMS) Score.

"Participants were asked to rate the extent to which they feel a variety of emotions/feelings. The overall score is presented.~Assessments were performed prior to treatment (non-drug condition average) and at the end of each treatment period. Score range: -32 to 200. Lower scores correspond to better mood state." (NCT02912364)
Timeframe: Prior to treatment (non-drug condition average) and at the end of each six-week treatment period.

Interventionunits on a scale (Mean)
Non-drug Condition Average8
Eslicarbazepine11
Carbamazepine15

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Tmax of Ritonavir

Tmax was defined as time to reach maximum observed plasma concentration and can be observed directly from data as time of first occurrence. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionhour (hr) (Median)
Period1: PF-07321332 300 mg/Ritonavir 100 mg3.98
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg1.98

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Vz/F of Ritonavir

Vz/F was defined as apparent volume of distribution. Vz/F is calculated as Dose/(AUCinf * kel), where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

InterventionL (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg234.0
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg697.5

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Apparent Volume of Distribution (Vz/F) of PF-07321332

Vz/F was defined as apparent volume of distribution. Vz/F is calculated as Dose/(AUCinf * kel), where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

InterventionLiter (L) (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg109.4
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg157.2

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Number of Participants With Clinically Significant Change in Electrocardiogram (ECG) Findings

All ECG assessments (triplicate) were made after at least a 10 minute rest in a supine position and prior to any blood draws or vital sign measurements. (NCT04962230)
Timeframe: Screening and Day 1 pre-dose, and at 1.5, 8, and 24 hours post dose in Period 1; Days 2, 3, 4, Day 14 pre-dose, and at 1.5, 8, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

,
InterventionParticipants (Count of Participants)
PR interval, aggregate value ≥300 milliseconds (msec)PR interval, aggregate percent change ≥25/50%QRS duration, aggregate value ≥140 msecQRS duration, aggregate percent change ≥50%QTCF interval, aggregate value >450 msec and ≤480 msecQTCF interval, aggregate value >480 msec and ≤500 msecQTCF interval, aggregate value >500 msecQTCF interval, aggregate change ≥30 msec and ≤60 msecQTCF interval, aggregate change >60 msec
Period1: PF-07321332 300 mg/Ritonavir 100 mg000000000
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg000000000

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Number of Participants With Laboratory Abnormalities

Safety laboratory assessments included hematology, urinalysis, and clinical chemistry. All the safety laboratory samples were collected following at least a 4 hour fast. (NCT04962230)
Timeframe: Screening, Day -1 prior to dosing, and Day 2 in Period 1; Days 3, 6, 9, 12, 16 or early termination/discontinuation in Period 2

,
InterventionParticipants (Count of Participants)
Hemoglobin (g/dL) <0.8x lower limit of normal (LLN)Hematocrit (%) <0.8x LLNErythrocytes (10^6/mm^3) <0.8x LLNLymphocytes (10^3/mm^3) <0.8x LLNNeutrophils (10^3/mm^3) <0.8x LLNEosinophils/Leukocytes (%) >1.2x upper limit of normal (ULN)Monocytes/Leukocytes (%) >1.2x ULNAlanine Aminotransferase (U/L) >3.0x ULNSodium (milliequivalent per liter (mEq/L)) <0.95x LLNUrobilinogen (EU/dL) ≥1Fibrinogen (mg/dL) >1.25x BaselineURINE Hemoglobin ≥1
Period1: PF-07321332 300 mg/Ritonavir 100 mg000001100000
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg111214541113

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An Adverse event (AE) was any untoward medical occurrence in a participant. A serious AE was any untoward medical occurrence at any dose that resulted in death; was life-threatening; required hospitalization or prolongation of existing hospitalization; resulted in persistent or significant disability/incapacity, congenital anomaly/birth. An AE was considered treatment-emergent AE (TEAE) if the event occurred during the on-treatment period. A treatment-related AE was any untoward medical occurrence attributed to the study drug in a participant who received study drug. A treatment-related SAE was a treatment-related AE and was defined as any untoward medical occurrence at any dose that: was fatal or life-threatening; resulted in persistent or significant disability/incapacity; constituted a congenital anomaly/birth defect; was medically significant; required inpatient hospitalization or prolongation of existing hospitalization. Relatedness to study drug was assessed by the investigator. (NCT04962230)
Timeframe: Screening up to Day 3 in Period 1; Day 1 up to 35 days from administration of the final dose of study intervention or early termination/discontinuation in Period 2 (maximum of approximately 12 weeks)

,
InterventionParticipants (Count of Participants)
Participants with all-causality adverse eventsParticipants with all-causality serious adverse eventsParticipants with treatment related adverse eventsParticipants with treatment related serious adverse events
Period1: PF-07321332 300 mg/Ritonavir 100 mg4010
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg9060

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Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of PF-07321332

AUCinf was defined as area under the concentration-time curve from time 0 to infinity and was calculated as AUClast + (Clast*/kel), where Clast* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg23010
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg10280

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of PF-07321332

AUClast was defined as area under the plasma concentration-time profile from time 0 to the time of last observed quantifiable plasma concentration (Clast) and was determined by Linear/Log trapezoidal method. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionng*hr/mL (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg22450
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg10050

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Time to Reach Maximum Observed Plasma Concentration (Tmax) of PF-07321332

Tmax was defined as time to reach maximum observed plasma concentration and can be observed directly from data as time of first occurrence. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionhour (hr) (Median)
Period1: PF-07321332 300 mg/Ritonavir 100 mg3.00
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg1.50

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AUCinf of Ritonavir

AUCinf was defined as area under the concentration-time curve from time 0 to infinity and was calculated as AUClast + (Clast*/kel), where Clast* is the predicted plasma concentration at the last quantifiable time point estimated from the log-linear regression analysis. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionng*hr/mL (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg3599
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg677.6

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AUClast of Ritonavir

AUClast was defined as area under the plasma concentration-time profile from time 0 to the time of Clast and was determined by Linear/Log trapezoidal method. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionng*hr/mL (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg3414
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg466.2

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CL/F of Ritonavir

CL/F was defined as apparent clearance. Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is a quantitative measure of the rate at which a drug substance is removed from the blood. CL/F is calculated as dose/AUCinf. AUCinf = area under the plasma concentration versus time curve from time zero extrapolated to infinite time. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

InterventionL/hr (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg27.78
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg147.6

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Cmax of Ritonavir

Cmax was defined as maximum observed plasma concentration and can be observed directly from data. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionng/mL (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg359.3
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg96.07

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Maximum Observed Plasma Concentration (Cmax) of PF-07321332

Cmax was defined as maximum observed plasma concentration and can be observed directly from data. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg2210
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg1300

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t1/2 of Ritonavir

t1/2 was defined as the time measured for the plasma concentration of drug to decrease by one half. t1/2 is calculated as Loge(2)/kel, where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. Only those data points judged to describe the terminal log-linear decline was used in the regression. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionhr (Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg6.149
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg3.345

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Terminal Half-Life ( t1/2) of PF-07321332

t1/2 was defined as the time measured for the plasma concentration of drug to decrease by one half. t1/2 is calculated as Loge(2)/kel, where kel is the terminal phase rate constant calculated by a linear regression of the log-linear concentration-time curve. Only those data points judged to describe the terminal log-linear decline was used in the regression. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

Interventionhours (hr) (Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg6.053
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg3.845

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Apparent Oral Clearance (CL/F) of PF-07321332

CL/F was defined as apparent clearance. Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is a quantitative measure of the rate at which a drug substance is removed from the blood. CL/F is calculated as dose/AUCinf. AUCinf = area under the plasma concentration versus time curve from time zero extrapolated to infinite time. (NCT04962230)
Timeframe: Day 1 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post dose in Period 1; Day 14 pre-dose, and at 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

InterventionLiter per hour (L/hr) (Geometric Mean)
Period1: PF-07321332 300 mg/Ritonavir 100 mg13.06
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg29.17

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Number of Participants With Clinically Significant Change From Baseline in Vital Signs

Vital signs including single supine blood pressure and pulse rate were performed following at least a 5 minute rest in a supine position. Blood pressure (BP) and pulse rate (PR) assessments were performed after collection of electrocardiograms (ECGs) and prior to collection of blood draws if planned together. Respiratory rate (RR) was also evaluated. (NCT04962230)
Timeframe: Screening and Day 1 pre-dose, and at 1.5, 8, and 24 hours post dose in Period 1; Days 2, 3, 4, 6, 8, 10, 12, Day 14 pre-dose, and at 1.5, 8, 24, and 48 hours post-dose or early termination/discontinuation in Period 2

,
InterventionParticipants (Count of Participants)
Supine diastolic blood pressure value <50 mmHgSupine diastolic blood pressure change ≥20mmHg increaseSupine diastolic blood pressure change ≥20mmHg decreaseSupine pulse rate value <40 beats per minute(bpm)Supine pulse rate value >120 bpmSupine systolic blood pressure value <90mmHgSupine systolic blood pressure change ≥30mmHg decreaseSupine systolic blood pressure change ≥30mmHg increase
Period1: PF-07321332 300 mg/Ritonavir 100 mg00000100
Period2: Carbamazepine + PF-07321332 300 mg/Ritonavir 100 mg01000000

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