Classes
DEA Class; Rx
Common Brand Names; Mestinon, Regonol
- Acetylcholinesterase Inhibitors, Peripheral
Description
Oral and parenteral cholinesterase inhibitor
Used for myasthenia gravis and reversal of neuromuscular blocking effects of nondepolarizing muscle relaxants as well as for military medical use as pretreatment for exposure to Soman nerve agent
Longer duration of action and associated with fewer muscarinic effects compared to neostigmine
Indications
For the treatment of myasthenia gravis.
For neuromuscular blockade reversal of non-depolarizing muscle relaxants.
For adjunctive use in Soman nerve gas exposure prophylaxis.
Contraindications
Hypersensitivity
Mechanical intestinal or urinary obstruction
Adverse Effects
Fewer GI effects than neostigmine
Cholinergic effects (N/V, increases peristalsis, increases salivation, urinary frequency
Weakness
Hypotension
ECG changes
Loss of consciousness
Convulsions
Drowsiness
Thrombophlebitis
Urticaria
Arrhythmia
Laryngospasm
Bradycardia
Cardiac standstill (rare)
Cholinergic crisis (rare)
Transient rash in bromide-sensitive patients
Warnings
Caution in epilepsy, asthma, COPD, recent MI, hypertension, vagotonia, hyperthyroidism, dysrhythmia
Keep atropine and epinephrine immediately available to treat hypersensitivity reactions resulting from therapy
Injection unstable in alkaline solutions
If symptoms of excess cholinergic activity occur discontinue therapy
Anticholinesterase sensitivity may develop for brief or prolonged periods
Pregnancy and Lactation
Pregnancy Category: B
Lactation: Compatible
Maximum Dosage
1,500 mg/day PO regular-release tablets or syrup or 1,080 mg/day PO extended-release tablets for myasthenia gravis; 180 mg/day PO regular-release tablets for Soman nerve gas exposure prophylaxis; 0.25 mg/kg/dose IV for neuromuscular blockade reversal.
1,500 mg/day PO regular-release tablets or syrup or 1,080 mg/day PO extended-release tablets for myasthenia gravis; 180 mg/day PO regular-release tablets for Soman nerve gas exposure prophylaxis; 0.25 mg/kg/dose IV for neuromuscular blockade reversal.
1 mg/kg/dose PO (Max: 60 mg/dose PO) and 7 mg/kg/day PO (Max: 300 mg/day PO) for myasthenia gravis.
1 mg/kg/dose PO (Max: 60 mg/dose PO) and 7 mg/kg/day PO (Max: 300 mg/day PO) for myasthenia gravis.
1 mg/kg/dose PO and 7 mg/kg/day PO for myasthenia gravis.
1 mg/kg/dose PO and 7 mg/kg/day PO for myasthenia gravis.