Clobazam is a 1,5 benzodiazepine which binds to stereospecific benzodiazepine receptors on the postsynaptic GABA neuron at several sites within the central nervous system, including the limbic system, reticular formation.
藥動學
"Onset: 5 to 9 days (max); Absorption: Rapid and extensive; not affected by food or crushing tablet;Distribution: 100 L;Protein binding: 80% to 90%; Metabolism: Hepatic via CYP3A4 and to a lesser extent via CYP2C19 and 2B6; Bioavailability: 87%; Half-life elimination: Children: 16 hours; Adults: 36 to 42 hours;Time to peak: 0.5 to 4 hours; Excretion: Urine (~82%; unchanged drug: 2%); feces (~11%; 1% unchanged drug) "
禁忌症
"Myasthenia gravis; narrow-angle glaucoma; severe hepatic or respiratory disease; sleep apnea; history of substance abuse; use in the first trimester of pregnancy; breast-feeding"
"Lennox-Gastaut (adjunctive): ?30 kg: Initial: 5 mg QDfor ?1 week, then increase to 5 mg BID for ?1 week, then increase to 10 mg BID thereafter>30 kg: Initial: 5 mg BID for ?1 week, then increase to 10 mg BID for ?1 week, then increase to 20 mg BID thereafter(CYP2C19 poor metabolism: initial 5mg QD ?1 week)Epilepsy (adjunctive):Oral Initial: 5 to 15 mg/day; dosage may be gradually adjusted to a maximum of 80 mg/day.Catamenial epilepsy (off-label use):Oral: 20 to 30 mg daily for 10 days during the perimenstrual period."
小兒調整劑量
not found
腎功能調整劑量
No dosage adjustment is necessary
肝功能調整劑量
CYP2C19 poor metabolism: initial 5mg QD ?1 week)
安定性
Store at a controlled room temperature between 20 and 25 degrees C