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Pharmacologic class: Anticholinesterase
Therapeutic class: Muscle stimulant
Pregnancy risk category C
Inhibits enzyme acetylcholinesterase, leading to increased acetylcholine concentration at synapse and prolonged acetylcholine effects. Exerts direct cholinomimetic effect on skeletal muscle.
Injection (methylsulfate): 2 mg/ml, 1 mg/ml, 0.5 mg/ml, 0.25 mg/ml
Tablets (bromide): 15 mg
Indications and dosages
➣ Myasthenia gravis
Adults: 15 mg/day P.O.; may increase p.r.n. up to 375 mg/day; average dosage is 150 mg/day. Or 1 ml of 1:2,000 solution (0.5 mg) subcutaneously or I.M. based on response and tolerance.
➣ Postoperative abdominal distention and bladder atony
Adults: 0.5 to 1 mg I.M. or subcutaneously. If given for urinary retention and no response occurs within 1 hour, catheterize patient as ordered and repeat dose q 3 hours for five doses.
➣ Antidote for nondepolarizing neuromuscular blockers
Adults: 0.5 to 2.5 mg I.V.; repeat p.r.n. up to 5 mg. Precede initial dose with 0.6 to 1.2 mg atropine sulfate I.V., as ordered.
• Hypersensitivity to cholinergics or bromide
• Mechanical obstruction of GI or urinary tract
Use cautiously in:
• asthma, peptic ulcer, bradycardia, arrhythmias, recent coronary occlusion, vagotonia, hyperthyroidism, seizure disorder
• pregnant or breastfeeding patients.
Before giving, ensure that atropine sulfate is available to treat cholinergic crisis.
• Know that atropine may be combined with usual neostigmine dose to decrease risk of adverse reactions.
• Give oral form 1 hour before or 2 hours after a meal.
• Administer I.V. dose undiluted directly into vein or I.V. line. Give 0.5-mg dose slowly over 1 minute.
Keep resuscitation equipment nearby.
CNS: dizziness, headache, drowsiness, asthenia, loss of consciousness
CV: hypotension, tachycardia, bradycardia, atrioventricular (AV) block, cardiac arrest
EENT: vision changes, lacrimation, miosis
GI: nausea, vomiting, diarrhea, abdominal cramping, flatulence, increased peristalsis
GU: urinary frequency
Musculoskeletal: muscle cramps, spasms, and fasciculations; joint pain
Respiratory: dyspnea, bronchospasm, respiratory depression, respiratory arrest, laryngospasm
Skin: rash, urticaria, flushing
Drug-drug. Aminoglycosides, anticholinergics, atropine, corticosteroids, local and general anesthetics: reversal of anticholinergic effects
Cholinergics: additive toxicity
Kanamycin, neomycin, streptomycin: increased neuromuscular blockade
Succinylcholine: potentiation of neuromuscular blockade, prolonged respiratory depression
Monitor vital signs. Assess patient for hypotension, bradycardia or tachycardia, AV block, and evidence of impending cardiac arrest.
• Evaluate respiratory and neurologic status.
• Instruct patient to take tablets 1 hour before or 2 hours after meals.
Tell patient drug may alter his respiratory and cardiac status. Teach him to recognize and immediately report warning signs.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, muscle function, and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.