
(peer id oh stig’ meen)
Mestinon, Regonol
PREGNANCY CATEGORY C
Drug Classes
Antidote
Antimyasthenic
Cholinesterase inhibitor
Therapeutic Actions
Increases the concentration of acetylcholine at the sites of cholinergic transmission and prolongs and exaggerates the effects of acetylcholine by reversibly inhibiting the enzyme acetylcholinesterase, thus facilitating transmission at the skeletal neuromuscular junction.
Indications
Treatment of myasthenia gravis
Parenteral: Antidote for nondepolarizing neuromuscular junction blockers (eg, tubocurarine) after surgery
To increase survival after exposure to sarin “nerve gas” poisoning in conjunction with protective measures
Unlabeled use: Postpoliomyelitis syndrome
Contraindications and Cautions
Contraindicated with hypersensitivity to anticholinesterases; adverse reactions to bromides; intestinal or urogenital tract obstruction, peritonitis, lactation.
Use cautiously with asthma, peptic ulcer, bradycardia, cardiac arrhythmias, recent coronary occlusion, vagotonia, hyperthyroidism, epilepsy, pregnancy (given IV near- term, drug may stimulate uterus and induce premature labor).
Available Forms
Tablets—60 mg ER tabletsDNC—180 mg; syrup—60 mg/5 mL; injection—5 mg/mL
Dosages
Adults
Oral
Symptomatic control of myasthenia gravis: Average dose is 600 mg PO given over 24 hr; range, 60–1,500 mg, spaced to provide maximum relief. ER tablets, average dose is 180–540 mg PO daily or bid. Individualize dosage, allowing at least 6 hr between doses. Optimum control may require supplementation with the more rapidly acting syrup or regular tablets.
Military personnel who face the threat of sarin nerve gas: 30 mg PO every 8 hr starting several hr before exposure; stop drug if exposure occurs.
Parenteral
To supplement oral dosage preoperatively and postoperatively, during labor, during myasthenic crisis, etc: Give 1/30 the oral dose IM or very slowly IV. May be given 1 hr before second stage of labor is complete (enables patient to have adequate strength and protects neonate in immediate postnatal period).
Antidote for nondepolarizing neuromuscular blockers: Give atropine sulfate 0.6–1.2 mg IV immediately before slow IV injection of pyridostigmine 0.1–0.25 mg/kg. 10–20 mg pyridostigmine usually suffices. Full recovery usually occurs within 15 min but may take 30 min.
Pediatric patients

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