====== Benzodiazepines ====== Benzodiazepines (BZDs) are a class of psychoactive drugs with anxiolytic, sedative, muscle relaxant, anticonvulsant, and hypnotic properties. They act by enhancing the effect of gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the central nervous system. ===== Classification ===== * **Drug class:** Central nervous system depressants * **ATC code:** N05BA (anxiolytics), N05CD (hypnotics), N03AE (antiepileptics) * **Schedule:** Controlled substances in most countries (e.g., Schedule IV in the U.S.) ===== Mechanism of Action ===== * Bind to the **benzodiazepine site** on the **GABA-A receptor** * Increase the **frequency** of chloride channel opening → **hyperpolarization** of the neuron → reduced excitability ===== Clinical Uses ===== * **Anxiety disorders** (e.g., generalized anxiety disorder, panic disorder) * **Insomnia** (short-term use) * **Seizure control** (e.g., status epilepticus) * **Muscle spasms** * **Alcohol withdrawal** * **Procedural sedation** * **Adjunctive treatment in tinnitus-related distress** (off-label) ===== Common Benzodiazepines ===== * **Short-acting:** Midazolam, Triazolam * **Intermediate-acting:** Lorazepam, Alprazolam, Oxazepam * **Long-acting:** Diazepam, Clonazepam, Chlordiazepoxide ===== Adverse Effects ===== * **Common:** Drowsiness, dizziness, confusion, impaired coordination * **Cognitive:** Anterograde amnesia, slowed psychomotor performance * **Dependence and withdrawal** with long-term use * **Risk of falls** and **delirium** in the elderly * **Respiratory depression** in overdose or when combined with other CNS depressants ===== Contraindications ===== * History of **substance use disorder** * Severe **hepatic impairment** * **Sleep apnea** * **Myasthenia gravis** * Use with **opioids** (risk of fatal respiratory depression) ===== Monitoring ===== * Monitor sedation level, respiratory status (especially if IV) * Reassess regularly for continued need * Taper gradually to avoid withdrawal ===== Special Considerations ===== * Risk of **tolerance** and **dependence** increases with duration * Should be **avoided in elderly** (Beers Criteria) unless clearly indicated * Use lowest effective dose for the **shortest duration possible** ===== Reversal Agent ===== * **Flumazenil** (competitive antagonist of the BZD receptor) — used in overdose or procedural reversal; risk of seizures ===== Synonyms ===== * **BZD**, **benzos** * Not to be confused with **barbiturates** (different receptor modulation) ===== Related Concepts ===== * [[antidepressants|Antidepressants]] * [[GABA_A receptor|GABA-A receptor]] * [[dependence|Dependence and withdrawal]]