U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C16H13ClN2O2
Molecular Weight 300.74
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLOBAZAM

SMILES

CN1C2=C(C=C(Cl)C=C2)N(C3=CC=CC=C3)C(=O)CC1=O

InChI

InChIKey=CXOXHMZGEKVPMT-UHFFFAOYSA-N
InChI=1S/C16H13ClN2O2/c1-18-13-8-7-11(17)9-14(13)19(16(21)10-15(18)20)12-5-3-2-4-6-12/h2-9H,10H2,1H3

HIDE SMILES / InChI
Molecular Formula C16H13ClN2O2
Molecular Weight 300.74
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/cdi/clobazam.html; http://www.epilepsy.com/medications/clobazam https://www.ncbi.nlm.nih.gov/pubmed/?term=23318278

Clobazam belongs to the 1,5-benzodiazepine class of drugs with antiepileptic properties. It has been used to treat anxiety and epilepsy since 1970s. In the US clobazam was approved for marketing in October of 2011 for the adjunctive treatment of seizures associated with Lennox-Gastaut syndrome. It is also approved for adjunctive therapy for epilepsy in patients who have not responded to first-line drugs and in children who are refractory to first-line drugs. The mechanism of action for clobazam is not fully understood but is thought to involve what is known as potentiation of GABAergic neurotransmission resulting from binding at a benzodiazepine site at the GABA(A) receptor. Possible side effects: constipation, fever, drowsiness, sedation, ataxia, aggressive behavior, lethargy, drooling, and irritability. Other side effects include: urinary tract infection, pneumonia, cough, dysphagia, dysarthria, bronchitis, insomnia, fatigue, decreased appetite, and increased appetite.

CNS Activity

CNS Active
3828
Curator's Comment: Has a central nervous system (CNS) depressant effect

Originator

Maestretti Research Laboratories
1
Curator's Comment: Discovery of Clobazam at the Maestretti Research Laboratories was first published in 1969. Maestretti Research Laboratories became part of Sanofi.

Approval Year

2011
562
Targets

Targets

Primary TargetPharmacologyConditionPotency
Activator
1410
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Approved
8360
ONFI

Approved Use

Indicated for the adjunctive treatment of seizures associated with Lennox-Gastaut syndrome (LGS) in patients 2 years of age or older.

Launch Date

1.31915514E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
641 μg/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/6529527/
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CLOBAZAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
13741 μg × h/L
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/6529527/
30 mg single, oral
dose: 30 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CLOBAZAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
36 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf
30 mg 1 times / day unknown, oral
dose: 30 mg
route of administration: Oral
experiment type: UNKNOWN
co-administered:
CLOBAZAM plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
10%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/202067s005,203993s007lbl.pdf
30 mg 1 times / day unknown, oral
dose: 30 mg
route of administration: Oral
experiment type: UNKNOWN
co-administered:
CLOBAZAM plasma
Homo sapiens
population: UNKNOWN
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Disc. AE: Somnolence, Depressed mood...
Other AEs: Delirium...
AEs leading to
discontinuation/dose reduction:
Somnolence (1 patient)
Depressed mood (1 patient)
Libido decreased (1 patient)
Erectile dysfunction (1 patient)
Insomnia (1 patient)
Dysarthria (1 patient)
Unsteady gait (1 patient)
Dizziness (1 patient)
Other AEs:
Delirium (2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Disc. AE: Transaminases increased...
AEs leading to
discontinuation/dose reduction:
Transaminases increased (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Disc. AE: Transaminases increased...
AEs leading to
discontinuation/dose reduction:
Transaminases increased (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 70
Disc. AE: Transaminases increased...
AEs leading to
discontinuation/dose reduction:
Transaminases increased (2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 70
60 mg 2 times / day steady, oral
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Disc. AE: Somnolence...
AEs leading to
discontinuation/dose reduction:
Somnolence (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
70 mg 2 times / day steady, oral
Dose: 70 mg, 2 times / day
Route: oral
Route: steady
Dose: 70 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Disc. AE: Dizziness, Somnolence...
AEs leading to
discontinuation/dose reduction:
Dizziness (1 patient)
Somnolence (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
AEs

AEs

AESignificanceDosePopulation
Depressed mood 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Dizziness 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Dysarthria 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Erectile dysfunction 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Insomnia 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Libido decreased 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Somnolence 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Unsteady gait 1 patient
Disc. AE
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Delirium 2 patients
80 mg 2 times / day steady, oral
Highest studied dose
Dose: 80 mg, 2 times / day
Route: oral
Route: steady
Dose: 80 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69-70
Transaminases increased 1 patient
Disc. AE
10 mg 2 times / day steady, oral
Dose: 10 mg, 2 times / day
Route: oral
Route: steady
Dose: 10 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Transaminases increased 1 patient
Disc. AE
15 mg 2 times / day steady, oral
Dose: 15 mg, 2 times / day
Route: oral
Route: steady
Dose: 15 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Transaminases increased 2 patients
Disc. AE
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 70
healthy
n = 70
Health Status: healthy
Population Size: 70
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 70
Somnolence 1 patient
Disc. AE
60 mg 2 times / day steady, oral
Dose: 60 mg, 2 times / day
Route: oral
Route: steady
Dose: 60 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Dizziness 1 patient
Disc. AE
70 mg 2 times / day steady, oral
Dose: 70 mg, 2 times / day
Route: oral
Route: steady
Dose: 70 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Somnolence 1 patient
Disc. AE
70 mg 2 times / day steady, oral
Dose: 70 mg, 2 times / day
Route: oral
Route: steady
Dose: 70 mg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
healthy
n = 24
Health Status: healthy
Population Size: 24
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/202067Orig1s000MedR.pdf
Page: p. 69
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
768

substrate
1709

inhibitor
1579
inhibitor
1752
inhibitor
1837
inhibitor
1599

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1509

CYP2C8
901

CYP2C19
1463

UGT1A1
204

UGT1A4
77

UGT1A6
108

UGT2B4
19

P-gp
1437
CYP2C19
985

CYP2B6
660

P-gp
1527

OAT
1
UGT1A1
69
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1673
 no
CYP2C19
1537
 no
CYP2C8
955
 no
CYP2C9
1803
 no
CYP3A4
1909
 no
P-gp
1626
 no
UGT1A1
254
 no
UGT1A4
80
 no
UGT1A6
141
 no
UGT2B4
19
 no
CYP2D6
1875
 no
yes (co-administration study)
Comment: clobazam increased dextromethorphan cmax 90%, auc 59%
Page: 16.0
UGT1A1
254
 weak
CYP3A4
1909
 weak
yes (co-administration study)
Comment: clobazam decreased midazolam auc 27%, cmax 24%
Page: 9.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1709
 major
yes (co-administration study)
Comment: ketoconazole increased clobazam auc 54%, no effect on cmax
Page: 15.0
CYP2B6
660
 minor
CYP2C19
985
 minor
yes (co-administration study)
Comment: omeprazole increased clobazam auc 30-36%, no effect on cmax
Page: 15.0
OAT
1
 no
P-gp
1527
 yes
yes (co-administration study)
Comment: verapamil reduced clobazam transport >96%
Page: 17.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1632
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:31413
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:31413
ZINC
ZINC000000001175
http://zinc15.docking.org/substances/ZINC000000001175
eMolecules
536528
https://www.emolecules.com/cgi-bin/more?vid=536528
PubMed

PubMed

TitleDatePubMed
[Efficacy and withdrawal of clobazam, lorazepam and buspirone in the treatment of anxiety disorders].
1996 Nov-Dec
Efficacy of clobazam as add-on therapy in patients with refractory partial epilepsy.
2001 Apr
[Clinical features and treatment of refractory epilepsy in children].
2001 Dec
Evaluation of native GABA(A) receptors containing an alpha 5 subunit.
2001 Feb 9
A stability-indicating LC method for the simultaneous determination of ramipril and hydrochlorothiazide in dosage forms.
2001 Jan
Induction of hypersensitivity to a previously tolerated antiepileptic drug by a second antiepileptic drug.
2001 Mar
Atypical evolution in childhood epilepsy with occipital paroxysms (Panayiotopoulos type).
2001 Sep
On the use of tranquillisers in epilepsy.
2002
Successful treatment of severe infantile hyperekplexia with low-dose clobazam.
2002 Feb
Pharmacological and endocrinological characterisation of stress-induced hyperthermia in singly housed mice using classical and candidate anxiolytics (LY314582, MPEP and NKP608).
2002 Jan 25
Clobazam shows a different antiepileptic action profile from clonazepam and zonisamide in Ihara epileptic rats.
2002 May
[A case of intractable epilepsy showing frequent gelastic seizures by administration of clobazam].
2003 Sep
Clobazam as a new antiepileptic drug and clorazepate dipotassium as an alternative antiepileptic drug in Japan.
2004
Hypersensitivity to topiramate sprinkle capsules does not preclude the use of topiramate tablets.
2004
Screening, library-assisted identification and validated quantification of 23 benzodiazepines, flumazenil, zaleplone, zolpidem and zopiclone in plasma by liquid chromatography/mass spectrometry with atmospheric pressure chemical ionization.
2004 Aug
Unusual side-effects due to clobazam: a case report with genetic study of CYP2C19.
2004 Jan
[Idiopathic epilepsies: some therapeutic aspects].
2004 Jan 16-31
Sporadic major hyperekplexia in neonates and infants: clinical manifestations and outcome.
2004 Jul
Pharmacodynamic interaction studies with topiramate in the pentylenetetrazol and maximal electroshock seizure models.
2004 Jul
Forensic intoxication with clobazam: HPLC/DAD/MSD analysis.
2004 Jul 16
Affinity of various benzodiazepine site ligands in mice with a point mutation in the GABA(A) receptor gamma2 subunit.
2004 Oct 15
Substrate depletion approach for determining in vitro metabolic clearance: time dependencies in hepatocyte and microsomal incubations.
2004 Sep
The difficulty in diagnosing non-convulsive status epilepticus during routine medical practice.
2004 Sep
Management of Landau-Kleffner syndrome.
2005
Levetiracetam in the treatment of infantile spasms.
2005
Stiripentol: new preparation. Severe myoclonic epilepsy of infancy: promising.
2005 Apr
Molecular regulation of glutamate and GABA transporter proteins by clobazam during epileptogenesis in Fe(+++)-induced epileptic rats.
2005 Dec 14
Clobazam as add-on therapy for temporal lobe epilepsy and hippocampal sclerosis.
2005 Feb
Effect of antiepileptic drug polytherapy on crystalluria.
2005 Feb
Treatment of electrical status epilepticus during slow-wave sleep with high-dose corticosteroid.
2005 Jan
[Antiepileptic drugs in the treatment of autistic regression syndromes].
2005 Jan 15
A common variable immunodeficient patient who developed acute disseminated encephalomyelitis followed by the Lennox-Gastaut syndrome.
2005 Jun
Motor impairment on awakening in a patient with an EEG pattern of "unilateral, continuous spikes and waves during slow sleep".
2005 Jun
Screening and confirmatory method for benzodiazepines and hypnotics in oral fluid by LC-MS/MS.
2005 Jun 10
Evaluation of health status in epilepsy using the EQ-5D questionnaire: a prospective, observational, 6-month study of adjunctive therapy with anti-epileptic drugs.
2005 May
Levetiracetam in idiopathic generalised epilepsy and porphyria cutanea tarda.
2006
Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels.
2006 Apr
In vitro and in vivo inhibitory effect of stiripentol on clobazam metabolism.
2006 Apr
Landau-Kleffner syndrome is not an eponymic badge of ignorance.
2006 Aug
Effects of some antiepileptics on septal-kindled seizures in rats.
2006 Dec
Anticonvulsant hypersensitivity syndrome to lamotrigine confirmed by lymphocyte stimulation in vitro.
2006 Feb
Pharmacological properties of GABAA receptors containing gamma1 subunits.
2006 Feb
Benign angiopathy of the central nervous system associated with phenytoin intoxication.
2006 Jun
Abusive prescription of psychostimulants: a study of two cases.
2006 Mar
Quantification of benzodiazepines in whole blood and serum.
2006 Nov
Treatment in the pediatric emergency department is evidence based: a retrospective analysis.
2006 Oct 6
Clobazam.
2007 Jan
Stiripentol.
2007 Jan
Patents

Patents

JP2008516961A
21
US2010317715
1
US2010331312
5
US6699849
1

Sample Use Guides

In Vivo Use Guide
Patients ≤30 kg body weight: Initiate at 5 mg daily and titrate as tolerated up to 20 mg daily. Patients > 30 kg body weight: Initiate at 10 mg daily and titrate as tolerated up to 40 mg daily. For doses above 5 mg/day administer in two divided doses. Dosage adjustment needed in following groups: Geriatric patients. Known CYP2C19 poor metabolizers. Mild or moderate hepatic impairment; no information for severe hepatic impairment.
Route of Administration: Oral
In Vitro Use Guide
Recurrent ictal-like seizures (ILEs, four per hour) were generated in intact corticohippocampal formations (CHFs) of P7-8 rats, and extracellular recordings were performed in the hippocampus and neocortex. Clobazam was applied at clinically relevant concentrations (at least two), during 30 min after the third ILE. Clobazam prevented the occurrence of seizures in recurrent ictal-like seizures.
Substance Class Chemical
Created
by admin
on Wed Jul 05 22:43:19 UTC 2023
Edited
by admin
on Wed Jul 05 22:43:19 UTC 2023
Record UNII
2MRO291B4U
Record Status Validated (UNII)
Record Version
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Name Type Language
CLOBAZAM
DASH   EP   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CLOBAZAM [MI]
Common Name English
CLOBAZAM [JAN]
Common Name English
URBADAN
Brand Name English
1H-1,5-BENZODIAZEPINE-2,4(3H,5H)-DIONE, 7-CHLORO-1-METHYL-5-PHENYL-
Systematic Name English
CLOBAZAM [ORANGE BOOK]
Common Name English
CLOBAZAM [VANDF]
Common Name English
FRISIUM
Brand Name English
URBANYL
Brand Name English
ONFI
Brand Name English
LM 2717
Code English
LM-2717
Code English
COLBAZAM [VANDF]
Common Name English
NSC-336279
Code English
HR-376
Code English
MYSTAN
Brand Name English
H 4723
Code English
HR 376
Code English
CLOBAZAM [EP MONOGRAPH]
Common Name English
CLOBAZAM [MART.]
Common Name English
7-Chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione
Common Name English
SYMPAZAN
Brand Name English
H-4723
Code English
clobazam [INN]
Common Name English
CLOBAZAM [USAN]
Common Name English
Clobazam [WHO-DD]
Common Name English
Classification Tree Code System Code
DEA NO. 2751
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
FDA ORPHAN DRUG 248307
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
LIVERTOX NBK548865
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
WHO-ATC N05BA09
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
NCI_THESAURUS C28197
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
WHO-VATC QN05BA09
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
NDF-RT N0000175694
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
Code System Code Type Description
CAS
22316-47-8
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
CHEBI
31413
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
WIKIPEDIA
CLOBAZAM
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
MESH
C012255
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
EPA CompTox
DTXSID2046759
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
PUBCHEM
2789
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
NSC
336279
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
INN
3055
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
DAILYMED
2MRO291B4U
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
DRUG BANK
DB00349
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
EVMPD
SUB06673MIG
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
SMS_ID
100000084299
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
ChEMBL
CHEMBL70418
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
HSDB
8343
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
FDA UNII
2MRO291B4U
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
NCI_THESAURUS
C81615
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
ECHA (EC/EINECS)
244-908-7
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
LACTMED
Clobazam
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
RXCUI
21241
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY RxNorm
MERCK INDEX
M3626
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY Merck Index
NDF-RT
N0000182137
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY Cytochrome P450 2D6 Inhibitors [MoA]
IUPHAR
7149
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
DRUG CENTRAL
682
Created by admin on Wed Jul 05 22:43:19 UTC 2023 , Edited by admin on Wed Jul 05 22:43:19 UTC 2023
PRIMARY
Related Record Type Details
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INDUCER
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of CLOBAZAM
EXCRETED UNCHANGED
FECAL
Structure of CLOBAZAM
EXCRETED UNCHANGED
Clobazam is cleared mainly by metabolism with subsequent renal elimination of metabolites. In a mass balance study, 82% of the dose administered was recovered in the urine and 11% in the feces. Clobazam represents ~2 % of the dose recovered in urine.
URINE
CYTOCHROME P450 2C19
METABOLIC ENZYME -> SUBSTRATE
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
CYTOCHROME P450 2B6
METABOLIC ENZYME -> SUBSTRATE
MINOR
Related Record Type Details
Structure of 9-HYDROXY-N-DESMETHYLCLOBAZAM
METABOLITE -> PARENT
Structure of N-DEMETHYLCLOBAZAM-3',4'-DIHYDRODIOL
METABOLITE -> PARENT
Structure of N-Desmethylclobazam
METABOLITE ACTIVE -> PARENT
Structure of 4'-HYDROXY-N-DESMETHYLCLOBAZAM
METABOLITE -> PARENT
Structure of 4'-HYDROXYCLOBAZAM
METABOLITE -> PARENT
Structure of 7-CHLORO-5-((3S,4S)-3,4-DIHYDROXYCYCLOHEXA-1,5-DIEN-1-YL)-1-METHYL-1,5-BENZODIAZEPINE-2,4-DIONE
METABOLITE -> PARENT
Related Record Type Details
Structure of 7-chloro-1,3,3-trimethyl-5-phenyl-1,5-dihydro-3H-1,5-benzodiazepine-2,4-dione
IMPURITY -> PARENT
Structure of N-[4-Chloro-2-(phenylamino)phenyl]-N-methylacetamide
IMPURITY -> PARENT
Structure of N-Desmethylclobazam
IMPURITY -> PARENT
Structure of 3-METHYLCLOBAZAM
IMPURITY -> PARENT
Structure of Methyl 3-((4-chloro-2-(phenylamino)phenyl)(methyl)amino)-3-oxopropanoate
IMPURITY -> PARENT
Structure of Deschloroclobazam
IMPURITY -> PARENT
Structure of 5-Chloro-1,2-dimethyl-3-phenyl-1H-benzimidazolium
IMPURITY -> PARENT
Related Record Type Details
Structure of CLOBAZAM
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC SINGLE- OR MULTIPLE-DOSE ADMINISTRATIONS

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