Pyridostigmine bromide


Generic Medicine Info
Indications and Dosage
Intravenous
Reversal of neuromuscular blockade
Adult: 0.1-0.25 mg/kg (approx 10-20 mg), w/ or preceded by atropine sulfate.

Oral
Myasthenia gravis
Adult: 30-120 mg in divided doses, up to a total daily dose of 0.3-1.2 g.
Child: <6 yr Initially, 30 mg; 6-12 yr Initially, 60 mg. Doses are repeated throughout the day up to a usual total daily dose of 30-360 mg, w/ increments of 15-30 mg daily until a satisfactory response is obtained.

Oral
Paralytic ileus and postoperative urinary retention
Adult: 60-240 mg daily.
Child: 15-60 mg daily.
Renal Impairment
Lower initial dose may be needed, titrate to desired effect.
Administration
Should be taken with food.
Contraindications
Mechanical GI or urinary obstruction.
Special Precautions
Patient w/ bronchial asthma, COPD, bradycardia, cardiac arrhythmias, vagotonia, peptic ulcer, epilepsy or parkinsonism, hyperthyroidism. Renal impairment. Childn. Pregnancy and lactation.
Adverse Reactions
Nausea, vomiting, diarrhoea, increased peristalsis and bronchial secretions, miosis, excessive salivation and sweating, abdominal cramps, bradycardia, bronchospasm, skin rash, muscle spasm, fasciculation, muscle weakness.
Potentially Fatal: Resp paralysis, cardiac arrest, pulmonary oedema.
IM/IV/Parenteral/PO: C
Monitoring Parameters
Monitor cholinergic reaction particularly in IV admin.
Overdosage
Symptoms: Cholinergic crisis characterised by severe muscarinic (e.g. nausea and vomiting, diarrhoea) and nicotinic symptoms (e.g. muscle weakness); electrolyte abnormalities. CNS symptoms (e.g. agitation, restlessness, confusion) may occur in extremely high doses. Death may result from CV and resp failure. Management: Maintain adequate respiration. Artificial respiration should be instituted in severe resp depression. Administer 1-4 mg of atropine sulfate IV, w/ additional doses given every 5-30 min as needed.
Drug Interactions
May exacerbate night vision problems w/ anti-glaucoma drugs. Antagonises the effect of non-depolarising muscle relaxants (e.g. pancuronium, vecuronium). Prolongs the effect of depolarising muscle relaxants (e.g. suxamethonium).
Action
Description: Pyridostigmine bromide facilitates impulse transmission across the myoneural junction by inhibiting the destruction of acetylcholine by acetylcholinesterase. It also has direct cholinomimetic effect on skeletal muscles.
Onset: 30-45 min (oral); w/in approx 15 min (IM); 2-5 min (IV).
Duration: 3-6 hr (oral); 2-3 hr (IV).
Pharmacokinetics:
Absorption: Poorly absorbed from the GI tract. Bioavailability: 10-20% (oral). Time to peak plasma concentration: Approx 1-3 hr (oral).
Distribution: Crosses the placenta and enters breast milk; poor penetration into CNS. Volume of distribution: Approx 19 L.
Metabolism: Undergoes hepatic metabolism and hydrolysis by cholinesterases.
Excretion: Via urine as unchanged drug and metabolites. Elimination half-life: 3 hr (oral); approx 1.5 hr (IV).
Chemical Structure

Chemical Structure Image
Pyridostigmine bromide

Source: National Center for Biotechnology Information. PubChem Database. Pyridostigmine bromide, CID=7550, https://pubchem.ncbi.nlm.nih.gov/compound/Pyridostigmine-bromide (accessed on Jan. 22, 2020)

Storage
Store at 25°C. Protect from light.
MIMS Class
Neuromuscular Disorder Drugs
ATC Classification
N07AA02 - pyridostigmine ; Belongs to the class of anticholinesterase. Used as parasympathomimetics.
References
Anon. Pyridostigmine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 31/07/2015.

Buckingham R (ed). Pyridostigmine Bromide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 31/07/2015.

McEvoy GK, Snow EK, Miller J et al (eds). Pyridostigmine Bromide. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 31/07/2015.

Regonol Injection, Solution (Sandoz Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 31/07/2015.

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