Products
Clobazam is commercially available in tablet form (Urbanyl). It has been approved in many countries since 1979.
Structure and properties
Clobazam (C16H13ClN2O2, Mr = 300.7 g/mol) exists as a white crystalline powder that is sparingly soluble in water. It belongs structurally to the 1,5-benzodiazepines. The other active ingredients are 1,4-benzodiazepines.
Effects
Clobazam (ATC N05BA09) has antianxiety, sedative, sleep-inducing, anticonvulsant, and muscle relaxant properties. The effects are due to binding to GABA-A receptors and enhancing GABAergic inhibition. Clobazam has a long half-life of over 20 hours. The main metabolite -desmethylclobazam has an even longer half-life of about 50 hours.
Indications
For the treatment of anxiety disorders and as an adjunctive medication for the treatment of chronic forms of epilepsy.
Abuse
Like all benzodiazepines, clobazam can be abused as a depressant narcotic. Abuse is dangerous, especially in combination with other depressant and respiratory drugs and with alcohol.
Dosage
According to the prescribing information. The duration of treatment should be kept as short as possible and should not exceed three months.
Contraindications
- Hypersensitivity
- Myasthenia gravis
- Severe respiratory failure
- Alcohol or narcotic dependence
- Sleep apnea
- Severe hepatic insufficiency
- First trimester of pregnancy and during lactation.
Full precautions can be found in the drug label.
Interactions
Clobazam is biotransformed primarily by CYP3A4 and to a lesser extent by CYP2C19 and CYP2B6. Drug-drug interactions have been described with central depressant drugs, some antiepileptic drugs, CYP inhibitors, and muscle relaxants.
Adverse effects
Possible adverse effects include psychiatric disturbances, fatigue, drowsiness, visual disturbances, respiratory disturbances, digestive problems, muscle weakness, and ataxia. With rapid discontinuation, withdrawal symptoms may occur. Like all benzodiazepines, clobazam can be addictive.
