Pyridostigmine

Indications
 Oral
Myasthenia gravis
Adult: 0.3-1.2 g daily in divided doses.
Child: <6 yr: Initially, 30 mg, 6-12 yr: Initially, 60 mg. Dose may be gradually increased by 15-30 mg on a daily basis until a satisfactory response is observed.
Renal impairment: Dose reduction may be required.
Oral
Neonatal myasthenia gravis
Child: 5-10 mg given every 4-6 hr.
Oral
Paralytic ileus and postoperative urinary retention
Adult: Doses of 60-240 mg.
Intramuscular
Neonatal myasthenia gravis
Child: 50-150 mcg/kg, given every 4-6 hr.
Intravenous
Reversal of neuromuscular blockade
Adult: 10-20 mg with or preceded by 0.6-1.2 mg atropine sulfate to counteract any muscarinic effects.
Contraindications
 GI or urinary obstruction.
Warnings / Precautions
 Renal impairment, pregnancy and lactation, epilepsy, bronchial asthma, bradycardia, cardiac arrhythmias, recent coronary occlusion, vagotonia, hyperthyroidism, peptic ulcer, recent bladder/intestinal surgery. Care should be taken in the use of atropine for counteracting side effects.
Adverse Reactions
 Muscarinic side effects e.g. nausea, vomiting, diarrhoea, abdominal cramps, increased peristalsis, increased salivation, increased bronchial secretions, miosis and diaphoresis. Nicotinic side effects include muscle cramps, fasciculation and weakness.
Overdose Reactions
 May cause a cholinergic crisis resulting in excessive sweating, lachrymation, increased peristalsis, involuntary defaecation and urination. Death may result from respiratory failure.
Drug Interactions
 Quaternary ammonium ions are poorly absorbed and their absorption may be completely inhibited by bulk laxatives eg, methylcellulose. Quinidine, procainamide, propranolol block acetylcholine receptor and may aggravate myasthenia gravis. Antagonistic effects with atropine. Increased risk of bradycardia and hypotension when used with β-blockers. Drugs with neuromuscular blocking activity e.g. aminoglycosides may reduce the efficacy of pyridostigmine.
Potentially Fatal: May inhibit the metabolism of suxamethonium, thus concurrent use is not recommended.
See Below for More pyridostigmine bromide Drug Interactions
Mechanism of Actions
 Pyridostigmine bromide is a potent reversible inhibitor of acetylcholinesterase, the enzyme responsible for destroying acetylcholine. Inhibiting the enzyme allows free transmission of nerve impulses across the neuromuscular junction. Pyridostigmine bromide has a carbonyl ester linkage that is hydrolysed by acetylcholinesterase but much more slowly than is acetylcholine itself.
Absorption: Poorly absorbed from the GI tract (oral).
Distribution: CNS (poor penetration); crosses the placenta and enters breast milk (small amounts).
Metabolism: Hepatic: Hydrolysed by cholinesterases.
Excretion: Excreted in the urine (as unchanged drug and metabolites).
Administration
 Should be taken with food.
Available As
  • Pyridostigmine 180 mg
  • Pyridostigmine 30 mg
  • Pyridostigmine 60 mg

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