diazepam

Diazepam is a long-acting benzodiazepine used to treat anxiety, muscle spasm, seizures, and alcohol withdrawal. It enhances the effect of gamma-aminobutyric acid (GABA) at the GABA-A receptor, producing calming, anticonvulsant, and muscle-relaxant effects. It is available orally and by injection, and is rapidly absorbed when taken by mouth.

Common indications include generalized anxiety disorder and short-term anxiety relief, relief of muscle spasm, preoperative sedation, and management of alcohol withdrawal. It may be used as an adjunct in certain seizure disorders.

Pharmacokinetics: Diazepam is metabolized in the liver to active metabolites such as nordazepam and temazepam. Its elimination half-life ranges from about 20 to 50 hours in adults and is longer in the elderly, leading to potential accumulation with long-term use. Effects may persist for more than a day, especially in older patients.

Adverse effects include drowsiness, dizziness, impaired coordination, and confusion. It can cause anterograde amnesia and cognitive impairment; paradoxical reactions occur in some individuals. Dependence and withdrawal can occur with prolonged use; abrupt cessation may trigger rebound anxiety or seizures. Contraindications include hypersensitivity to benzodiazepines, acute narrow-angle glaucoma, severe respiratory impairment, and sleep apnea. Use with caution in pregnancy and breastfeeding; avoid with concurrent CNS depressants such as alcohol. Diazepam has been widely used since the 1960s, with emphasis on the lowest effective dose and shortest duration.