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Details

Stereochemistry ACHIRAL
Molecular Formula C15H10ClN3O3
Molecular Weight 315.711
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CLONAZEPAM

SMILES

[O-][N+](=O)C1=CC2=C(NC(=O)CN=C2C3=C(Cl)C=CC=C3)C=C1

InChI

InChIKey=DGBIGWXXNGSACT-UHFFFAOYSA-N
InChI=1S/C15H10ClN3O3/c16-12-4-2-1-3-10(12)15-11-7-9(19(21)22)5-6-13(11)18-14(20)8-17-15/h1-7H,8H2,(H,18,20)

HIDE SMILES / InChI

Description

Clonazepam, a benzodiazepine, is used primarily as an anticonvulsant in the treatment of absence seizures, petit mal variant seizures (Lennox-Gastaut syndrome), akinetic and myoclonic seizures, and nocturnal myoclonus. Klonopin is the brand name for Clonazepam, an anxiolytic and anticonvulsant. The precise mechanism by which clonazepam exerts its antiseizure and antipanic effects is unknown, although it is believed to be related to its ability to enhance the activity of gamma aminobutyric acid (GABA), the major inhibitory neurotransmitter in the central nervous system. Allosteric interactions between central benzodiazepine receptors and gamma-aminobutyric acid (GABA) receptors potentiate the effects of GABA. As GABA is an inhibitory neurotransmitter, this results in increased inhibition of the ascending reticular activating system. Benzodiazepines, in this way, block the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
0.06 nM [EC50]
57.0 µM [EC50]
40.0 µM [EC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
KLONOPIN
Primary
KLONOPIN

Cmax

ValueDoseCo-administeredAnalytePopulation
2.3 ng/mL
0.5 mg single, oral
CLONAZEPAM plasma
Homo sapiens
3 ng/mL
0.5 mg 3 times / day steady-state, oral
CLONAZEPAM plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
102 ng × h/mL
0.5 mg single, oral
CLONAZEPAM plasma
Homo sapiens
339 ng × h/mL
0.5 mg 3 times / day steady-state, oral
CLONAZEPAM plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
40 h
0.5 mg 3 times / day steady-state, oral
CLONAZEPAM plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
15%
0.5 mg single, oral
CLONAZEPAM plasma
Homo sapiens

Doses

AEs

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer







Drug as perpetrator​

Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
Seizure Disorders: Adults: The initial dose for adults with seizure disorders should not exceed 1.5 mg/day divided into three doses. Dosage may be increased in increments of 0.5 to 1 mg every 3 days until seizures are adequately controlled or until side effects preclude any further increase. Maintenance dosage must be individualized for each patient depending upon response. Maximum recommended daily dose is 20 mg. Clonazepam is available as a tablet or an orally disintegrating tablet (wafer). The tablets should be administered with water by swallowing the tablet whole. The orally disintegrating tablet should be administered as follows: After opening the pouch, peel back the foil on the blister. Do not push tablet through foil. Immediately upon opening the blister, using dry hands, remove the tablet and place it in the mouth. Tablet disintegration occurs rapidly in saliva so it can be easily swallowed with or without water.
Route of Administration: Oral
In Vitro Use Guide
Clonazepam (100 nM) increased inhibitory postsynaptic current (IPSC) decay time constants in rat thalamic nuclei-the reticular nucleus (nRt) (from 44.3 to 77.9 ms, P < 0.01) but not in the ventrobasal (VB) complex..