Neostigmine(nee oh stig’ meen)
Neostigmine Bromide Neostigmine Methylsulfate
Prostigmin
PREGNANCY CATEGORY C
Drug Classes
Antidote
Antimyasthenic
Cholinesterase inhibitor
Parasympathomimetic
Urinary tract drug
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, causing parasympathomimetic effects and facilitating transmission at the skeletal neuromuscular junction; also has direct cholinomimetic activity on skeletal muscle; may have direct cholinomimetic activity on neurons in autonomic ganglia and the CNS.
Indications
Prevention and treatment of postoperative distention and urinary retention
Symptomatic control of myasthenia gravis
Antidote for nondepolarizing neuromuscular junction blockers (tubocurarine or pancuronium) after surgery
Contraindications and Cautions
Contraindicated with hypersensitivity to anticholinesterases; adverse reactions to bromides (neostigmine bromide); intestinal or urogenital tract obstruction, peritonitis; pregnancy (may stimulate uterus and induce premature labor); lactation.
Use cautiously with asthma, peptic ulcer, bradycardia, cardiac arrhythmias, recent coronary occlusion, vagotonia, hyperthyroidism, epilepsy.
Available Forms
Injection—1:1,000 (1 mg/mL), 1:2,000 (0.5 mg/mL); tablets—15 mg
Dosages
Adults
Prevention of postoperative distention and urinary retention: 0.25 mg neostigmine methylsulfate subcutaneously or IM as soon as possible after operation. Repeat every 4–6 hr for 2–3 days.
Treatment of postoperative distention: 1 mL of the 1:2,000 solution (0.5 mg) neostigmine methylsulfate subcutaneously or IM, as required.
Treatment of urinary retention: 1 mL of the 1:2,000 solution (0.5 mg) neostigmine methylsulfate subcutaneously or IM. If urination does not occur within 1 hr, catheterize the patient. After the bladder is emptied, continue 0.5-mg injections every 3 hr for at least five injections.
Symptomatic control of myasthenia gravis: 1 mL of the 1:2,000 solution (0.5 mg) subcutaneously or IM. Individualize subsequent doses. Should be used with atropine to counteract adverse muscarinic effects. Tablets—15–375 mg/day PO; average daily dose is 150 mg.
Antidote for nondepolarizing neuromuscular blockers: Give atropine sulfate 0.6–1.2 mg IV several min before slow IV injection of neostigmine 0.5–2 mg. Repeat as required. Total dose should usually not exceed 5 mg.
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