Trade Names:Prostigmin- Tablets 15 mg- Injection 1:1,000- Injection 1:2,000- Injection 1:4,000
Facilitates myoneural junction impulse transmission by inhibiting acetylcholine destruction by cholinesterase.
Rapid absorption of neostigmine methylsulfate; neostigmine bromide is poorly absorbed from the GI tract. T max is 30 min (IV) and 1 to 2 h (oral).
Neostigmine protein binding is 15% to 25% (serum albumin).
Neostigmine is metabolized in the liver by microsomal enzymes and undergoes hydrolysis by cholinesterase.
Neostigmine is eliminated in urine (50% as unchanged). Half-life is 51 to 90 min and plasma half-life is 47 to 60 min (IV); half-life ranges from 42 to 60 min, with a mean half-life of 52 min (oral).
Onset of IM neostigmine is 20 to 30 min.
Duration of IM neostigmine is 2.5 to 4 h.
Symptomatic control of myasthenia gravis; antidote for nondepolarizing neuromuscular blocking agents after surgery; prevention and treatment of postoperative distention and urinary retention (IV only).
Hypersensitivity to anticholinesterases and bromides; mechanical intestinal or urinary obstruction; peritonitis.
IV 0.5 to 2 mg by slow infusion repeated as needed, preceded by 0.6 to 1.2 mg of atropine sulfate. May be repeated as needed up to total dose of 5 mg.Myasthenia GravisAdults
PO 15 to 375 mg/day; Subcutaneous/IM 1 mL of 1:2,000 solution (0.5 mg); individualize subsequent doses.Prevention of Postoperative Urinary Distention and RetentionAdults
Subcutaneous / IM 1 mL of 1:4,000 solution (0.25 mg) after surgery; repeat every 4 to 6 h for 2 or 3 days.Treatment of Postoperative DistentionAdults
Subcutaneous / IM 1 mL of 1:2,000 solution (0.5 mg), as required.Treatment of Urinary RetentionAdults
Subcutaneous / IM 1 mL of 1:2,000 solution (0.5 mg) after bladder is emptied; continue 0.5 mg injection every 3 h for at least 5 injections.
Store at 59° to 86°F. Keep injection in carton until ready to use and protect from light.
Intestinal motility may be slowed, increasing neostigmine absorption. Use with caution. Adjust the neostigmine dose as needed.Beta-blockers (eg, propranolol)
Severe or prolonged bradycardia may occur because of additive pharmacologic effects. Use with caution. Larger dosages of atropine and sympathomimetic pressor agents may be needed to reverse bradycardia and hypotension.Corticosteroids (eg, corticotropin, hydrocortisone)
The effects of neostigmine may be decreased. In addition, the effects of neostigmine may be increased after corticosteroids are discontinued. Provide mechanical respiratory support if needed.Drugs that interfere with neuromuscular transmission
May interfere with neuromuscular transmission. Use with caution in myasthenic patients. Monitor the patient and increase the neostigmine dose as needed.Kanamycin, streptomycin
Neuromuscular blockade may be enhanced. Use these antibiotics in myasthenic patients only when clearly indicated. Closely monitor the patient. Adjust the neostigmine dose as needed.Local/General anesthetics, antiarrhythmic agents (eg, procainamide)
Use with caution in myasthenic patients; may interfere with neuromuscular transmission. Increase the neostigmine dose as needed.Quinine
Quinine may antagonize the effects of neostigmine. Avoid using quinine in patients receiving neostigmine for myasthenia gravis.Succinylcholine
Neuromuscular blockade produced by succinylcholine may be prolonged. Avoid this combination in the presence of a depolarizing (phase 1) type of neuromuscular blockade. Use with caution if a nondepolarizing (phase 2) type of blockade is present. Provide mechanical respiratory support as needed.
None well documented.
Arrhythmia (AV block, bradycardia, nodal rhythm, tachycardia); cardiac arrest; hypotension; nonspecific ECG changes; syncope.
Convulsions; dizziness; drowsiness; dysarthria; dysphonia; headache; loss of consciousness.
Diaphoresis; flushing; rash; urticaria.
Miosis; vision changes.
Bowel cramps; diarrhea; emesis; flatulence; increased peristalsis; nausea; salivation; vomiting.
Dyspnea; increased oral, pharyngeal, and bronchial secretions; respiratory arrest, respiratory depression, and bronchospasm (IV).
Arthralgia; muscle cramps and spasms.
Allergy and anaphylaxis; fasciculations; weakness.
Frequently assess muscle strength and function in patient with myasthenia gravis or patient recovering from nondepolarizing neuromuscular blocking agent.
Category C .
Safety and efficacy not established.
Anaphylaxis may occur. Have atropine and antishock medications available.
Use with caution in patients with bradycardia, bronchial asthma, cardiac arrhythmias, epilepsy, hyperthyroidism, peptic ulcer, recent coronary occlusion, or vagotonia.
Abdominal cramps, anxiety, diarrhea, excessive salivation, miosis, panic attacks, progressive muscle weakness leading to paralysis and death, sweating, urinary urgency.
Copyright © 2009 Wolters Kluwer Health.