Makindo Medical Notes

⚠️ Overdose (accidental or intentional): – Manage ABCs, monitor O₂ sats, and give supplemental oxygen. – Ensure ability to manage respiratory depression and airway issues. – Respiratory and airway support as needed. – Flumazenil may be given with caution (risk of seizures, esp. in mixed overdoses).

💊 About: Always check the BNF link here

• 🔹 A long-acting benzodiazepine.
• ⏳ Active metabolites (e.g. desmethyldiazepam) have a half-life up to 100 hours → prolonged sedation.

⚙️ Mode of Action

• 📌 Binds to a specific site on the GABA(A) receptor–chloride ionophore complex (allosteric site, not the GABA site).
• 💡 Enhances the effect of GABA, the main inhibitory neurotransmitter in the CNS.
• ⚡ Increases the frequency of Cl⁻ channel opening → neuronal hyperpolarisation → CNS depression.

🎯 Indications

• 💤 Hypnotic for insomnia (short-term use only).
• 😟 Anxiolytic (anxiety disorders, premedication before procedures).
• 🧠 Anticonvulsant (status epilepticus, myoclonus).
• 💪 Muscle relaxant (spasms, tetanus).
• 🍺 Alcohol withdrawal (reduces agitation, tremors, seizures).
• 📝 Amnesia (for unpleasant procedures, e.g. endoscopy).

📊 Dose (BNF / specialist guidance)

• 😟 Anxiety / Sedation: 2–5 mg TDS PO (up to 30 mg/day in divided doses).
• ⚡ Status epilepticus: 5–10 mg slow IV (Diazemuls formulation less irritating). May repeat up to 20 mg total.

⛔ Contraindications

• 🚫 Driving or operating machinery (due to sedation).
• 😴 Sleep apnoea syndrome.
• 💨 Respiratory depression or significant respiratory muscle weakness.
• ⚠️ Myasthenia gravis (risk of worsening weakness).
• ❌ Concomitant use with alcohol or other strong sedatives.

⚠️ Cautions

• 🚗 Warn about impaired driving/operating machinery.
• 📉 Reduce dose in elderly, renal or hepatic impairment (risk of accumulation).
• ⚠️ Avoid long-term use → dependence risk after 4–6 weeks.

⚠️ Side Effects

• 💤 Sedation, drowsiness, ataxia, impaired psychomotor skills.
• 🧠 Anterograde amnesia, confusion.
• ⬇️ Respiratory depression (esp. IV or with other sedatives).
• 🔄 Rebound insomnia/anxiety on withdrawal.
• 📉 Dependence & withdrawal syndrome (convulsions, agitation, insomnia).
• ⏳ Long half-life → “hangover” effects (daytime sedation).

🔄 Interactions

• 💉 Effects reversed by flumazenil, but caution: risk of rebound seizures, especially in mixed overdoses.
• ⚠️ Potentiated by other CNS depressants (opioids, antipsychotics e.g. olanzapine, antihistamines).
• 🔬 Metabolised by hepatic enzymes – levels ↑ with CYP450 inhibitors (e.g. erythromycin, cimetidine).

📚 References

• Diazepam – BNF