NEOSTIGMINE

Cholinesterase inhibitor. Enhances neuromuscular transmission by prolonging action of acetylcholine through inhibition of acetylcholinesterase

Dosage Forms

Tablet

15 mg

Injection

2.5 mg/ml

Uses

  • Myasthenia gravis
  • Reversal of non-depolarising muscle relaxants effects
  • Post-operative non-obstructive urinary retention

Dose and Duration

Myasthenia gravis

Adult and child > 12 years: by mouth, initially 15–30 mg at suitable intervals throughout the day; gradually increase until desired response is obtained.
Usual total daily dose, 75–300 mg. Most patients tolerate max 180 mg

By SC or IM injection: 1–2.5 mg as required up to a total daily dose of 5–20 mg

Child 6–12 years: by mouth, initially 15 mg, gradually increased to a usual total daily dose of 15–90 mg given in divided doses at appropriate intervals

By IM or SC injection: 0.2–0.5 mg as required

Child 1 month–6 years: by mouth, initially 7.5 mg.
By IM or SC injection, 0.2–0.5 mg as required

Neonate: 1–2 mg by mouth or 0.05–0.25 mg.
By SC or IM injection every 4 hours, 30 minutes before feeds

Reversal of non-depolarizing block

Adult: by IV injection over 1 minute, 2.5 mg followed by 0.5 mg supplements if required to maximum total dose of 5 mg

Child: 0.04 mg/kg (titrate using peripheral nerve stimulator). Max 2.5 mg

Postoperative urinary retention

Adult: by SC or IM injection, 0.5 mg

Contraindications

  • Recent intestinal or bladder surgery
  • Intestinal or urinary tract obstruction
  • After suxamethonium
  • Pneumonia
  • Peritonitis

Side Effects

  • Increased salivation
  • Nausea and vomiting, abdominal cramps, diarrhoea
  • Overdose: increased bronchial secretions, sweating and tear production, bronchoconstriction, miosis, nystagmus, involuntary defecation and micturition, bradycardia, heart block, arrhythmias, hypotension, agitation, excessive dreaming and weakness

Interactions

  • Amikacin, gentamicin, streptomycin, polymixins (effect of neostigmine antagonised)

Pregnancy

  • Can be used

Breast-feeding

  • Can be used

⚠️ Caution

  • Large doses in 3ʳᵈ trimester of pregnancy may lead to neonatal myasthenia
  • Reduce dose in moderate and severe renal impairment
  • Use with extreme caution in asthma and in patients with bradycardia, recent coronary occlusion, hypotension, peptic ulcer, epilepsy or parkinsonism