Makindo Medical Notes

💡 Zopiclone and Zolpidem are not benzodiazepines but are “Z-drugs.” They act on the same GABA_A receptor complex and produce similar hypnotic and anxiolytic effects.

📖 About

• 💊 Widely used for anxiety, insomnia, periprocedural amnesia, and sedation.
• 🦴 Also relax skeletal muscles (used in movement disorders, spasticity).
• 😴 Induce sleep — hence their key role in hypnotic therapy.

🧠 Mode of Action

• Bind to the benzodiazepine receptor site on the GABA_A receptor–Cl⁻ channel complex.
• Enhance the effect of GABA (they do not mimic GABA itself).
• Increase the frequency (not duration) of Cl⁻ channel opening → hyperpolarisation → CNS inhibition.
• Contrast: Barbiturates increase duration of Cl⁻ channel opening.

💊 Indications

• 🧩 Anxiolytic (e.g., lorazepam for acute anxiety).
• 😴 Hypnotic (temazepam, Z-drugs for insomnia).
• 🧪 Premedication before procedures (sedation + amnesia).
• ⚡ Anticonvulsant (clonazepam, diazepam in status epilepticus).
• 💪 Muscle relaxant (spasticity, myoclonus).
• 🍷 Alcohol withdrawal (e.g., chlordiazepoxide, diazepam).

⚠️ Contraindications / Cautions

• 🚗 Driving or operating machinery — causes sedation, impaired reflexes.
• 💊 Concurrent use with opioids/other CNS depressants → ↑ risk of respiratory depression.
• ⚠️ Caution in depression (may worsen suicidal risk).
• 📉 Avoid prolonged use (>4–6 weeks) → high risk of tolerance and dependence.

🧪 Common Benzodiazepines

• Short-acting: Temazepam, Lorazepam
• Long-acting: Diazepam, Chlordiazepoxide
• Special uses: Clonazepam (anticonvulsant)

❗ Side Effects

• 😴 Sedation, drowsiness, poor concentration.
• 🌀 Ataxia, impaired psychomotor performance, falls (elderly).
• 🫁 Respiratory depression (esp. with opioids/alcohol).
• 🧠 Amnesia, tolerance, withdrawal symptoms (agitation, seizures).
• 🔄 Rebound insomnia when stopped abruptly.
• ⚡ Dependence can develop after 4–6 weeks of regular use.
• ⏳ Long-acting BZDs (e.g., diazepam) → “hangover” effect.

🔀 Interactions

• 💊 Potentiated by alcohol, opioids, antihistamines, antipsychotics.
• Diazepam and chlordiazepoxide: few major drug–drug interactions, but cumulative sedation with other CNS depressants.
• ⛑️ Flumazenil = competitive antagonist at benzodiazepine receptor, reverses sedation but short-acting (risk of seizures in chronic BZD users).