Clobazam
- Atc Codes:N05BA09
- CAS Codes:22316-47-8
- PHARMGKB ID:22316-47-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Frisium; Belgium: Frisium; Czech Republic: Frisium; Denmark: Frisium; Finland: Frisium; France: Urbanyl; Germany: Frisium; Greece: Frisium; Hungary: Frisium; Ireland: Frisium; Italy: Frisium; Luxembourg: Frisium; Malta: Frisium; Netherlands: Frisium; Poland: Frisium; Portugal: Castilium; Slovakia: Frisium; Spain: Noiafren; UK: Frisium.
North America
Canada: Clobazam, Frisium.
Latin America
Argentina: Clozam, Karidium; Brazil: Frisium, Urbanil; Mexico: Frisium.
Asia
Japan: Mystan.
Drug combinations
Chemistry
Clobazam: C~16~H~13~ClN~2~O~2~. Mw: 300.74. (1) 1H-1,5-Benzodiazepine-2,4(3H,5H)-dione, 7-chloro-1-methyl-5-phenyl-; (2) 7-Chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4-(3H,5H)-dione. CAS-22316-47-8 (1975).
Pharmacologic Category
Anxiolytics, Sedatives, and Hypnotics; Benzodiazepines. (ATC-Code: N05BA09).
Mechanism of action
Binds to stereospecific receptors on the postsynaptic GABA neuron at several sites within the CNS (limbic system, reticular formation). Enhances the inhibitory effect of GABA on neuronal excitability by increasing neuronal membrane permeability to chloride ions, which results in hyperpolarization (a less excitable state) and stabilization.
Therapeutic use
Adjunctive treatment of epilepsy.
Pregnancy and lactiation implications
Clobazam crosses the placenta. Contraindicated in 1^st^ trimester. Inguinal hernia, cardiac defects, spina bifida, dysmorphic facial features, skeletal defects, and multiple other malformations reported. Hypotonia and withdrawal symptoms reported following use during 3^rd^ trimester or near time of delivery. Contraindicated during lactation (infant sedation).
Unlabeled use
Monotherapy for epilepsy or intermittent seizures, antianxiety, anticonvulsant, and sedative agent.
Contraindications
Hypersensitivity to clobazam or any component of the formulation (cross-sensitivity with other benzodiazepines may exist). Myasthenia gravis. Narrow-angle glaucoma. Severe hepatic or respiratory disease. Sleep apnea. History of substance abuse. Pregnancy (particularly 1^st^ trimester). Breast-feeding.
Warnings and precautions
Benzodiazepines have been associated with anterograde amnesia. May cause CNS depression. Paradoxical reactions, including hyperactive or aggressive behavior, reported with benzodiazepines, particularly in adolescent/pediatric or psychiatric patients. Use caution in depression, particularly if suicidal risk may be present. Use with caution in history of drug abuse or acute alcoholism (risk of drug dependency). Tolerance, psychological and physical dependence may occur with prolonged use. Use with caution in the following cases: hepatic/renal impairment, impaired gag reflux, respiratory disease, and debilitated patients. Use with extreme caution in patients who are at risk of falls (caution in elderly patients). Tolerance and loss of seizure control reported with chronic administration. Rebound or withdrawal symptoms may occur following abrupt discontinuation or large decreases in dose.