Classifications: cholinergic agent; cholinesterase inhibitor; Therapeutic: cholinesterase inhibitor
Pregnancy Category: C
1:1000, 1:2000, 1:4000 injection
Produces reversible cholinesterase inhibition or inactivation. Has direct stimulant action on voluntary muscle fibers and
possibly on autonomic ganglia and CNS neurons. Allows intensified and prolonged effect of acetylcholine at cholinergic synapses
(basis for use in myasthenia gravis).
Produces generalized cholinergic response including miosis, increased tonus of intestinal and skeletal muscles, constriction
of bronchi and ureters, slower pulse rate, and stimulation of salivary and sweat glands.
To prevent and treat postoperative abdominal distension and urinary retention; for symptomatic control of and sometimes
for differential diagnosis of myasthenia gravis; and to reverse the effects of nondepolarizing muscle relaxants (e.g., tubocurarine).
Hypersensitivity to neostigmine, cholinergics; cholinesterase inhibitor toxicity; GI obstruction; ileus; bradycardia, hypotension;
mechanical obstruction of intestinal or urinary tract; peritonitis; administration with other cholinergic drugs; pregnancy
(category C), lactation.
Recent ileorectal anastomoses; epilepsy; bronchial asthma; hepatic disease; bradycardia, recent coronary occlusion; vagotonia;
hyperthyroidism; cardiac arrhythmias; renal failure; renal impairment; renal disease; peptic ulcer; seizure disorder.
Route & Dosage
|Diagnosis of Myasthenia Gravis
Adult: IM 0.02 mg/kg
Child: IM 0.04 mg/kg
Treatment of Myasthenia Gravis
Adult: IM/SC 0.52.5 mg q13h (max 10 mg/d)
Child: IM/SC 0.010.04 mg/kg q24h
Reversal of Nondepolarizing Neuromuscular Blockade
Adult: IV 0.52.5 mg slowly (max dose 5 mg)
Child: IV 0.0250.08 mg/kg
Infant: IV 0.0250.1 mg/kg
Postoperative Distention and Urinary Retention
Adult: IM/SC 0.25 mg q46h for 23 d
Clcr 1050 mL/min: use 50% of dose; <10 mL/min: use 25% of dose
- Note: 1 mg = 1 mL of the 1:1000 solution; 0.5 mg = 1 mL of the 1:2000 solution; 0.25 mg = 1 mL of the 1:4000 solution.
- Give undiluted.
PREPARE: Direct: Give undiluted.
ADMINISTER: Direct: Give at a rate of 0.5 mg or a fraction thereof over 1 min.
Adverse Effects (≥1%)Body as a Whole:
Muscle cramps, fasciculations,
twitching, pallor, fatigability, generalized weakness, paralysis, agitation, fear, death. CV:
Tightness in chest, bradycardia, hypotension, elevated BP. GI: Nausea,
vomiting, eructation, epigastric discomfort, abdominal cramps, diarrhea, involuntary or difficult defecation. CNS: CNS
stimulation. Respiratory: Increased salivation
and bronchial secretions, sneezing, cough, dyspnea, diaphoresis, respiratory depression
. Special Senses:
Lacrimation, miosis, blurred vision. Urogenital:
InteractionsDrug: Succinylcholine decamethonium
may prolong phase I block or reverse phase II block; neostigmine antagonizes effects of tubocurarine; atracurium, vecuronium, pancuronium; procainamide, quinidine, atropine
antagonize effects of neostigmine.
1030 min IM or IV. Peak:
2030 min IM or IV. Distribution:
Not reported to cross placenta or appear in breast milk. Metabolism:
In liver. Elimination:
80% of drug and metabolites excreted in urine within 24 h. Half-Life:
Assessment & Drug Effects
- Check pulse before giving drug to bradycardic patients. If below 60/min or other established parameter, consult physician.
Atropine will be ordered to restore heart rate.
- Monitor respiration, maintain airway or assisted ventilation, and give oxygen as indicated when used as antidote for tubocurarine
or other nondepolarizing neuromuscular blocking agents (usually preceded by atropine). Respiratory assistance is continued
until recovery of respiration and neuromuscular transmission is assured.
- Monitor pulse, respiration, and BP during period of dosage adjustment in treatment of myasthenia gravis.
- Report promptly and record accurately the onset of myasthenic symptoms and drug adverse effects in relation to last dose
in order to assist physician in determining lowest effective dosage schedule.
- Note carefully time of muscular weakness onset. It may indicate whether patient is in cholinergic or myasthenic crisis:
Weakness that appears approximately 1 h after drug administration suggests cholinergic crisis (overdose) and is treated by
prompt withdrawal of neostigmine and immediate administration of atropine. Weakness that occurs 3 h or more after drug administration
is more likely due to myasthenic crisis (underdose or drug resistance) and is treated by more intensive anticholinesterase
- Record drug effect and duration of action. S&S of myasthenia gravis relieved by neostigmine include lid ptosis; diplopia;
drooping facies; difficulty in chewing, swallowing, breathing, or coughing; and weakness of neck, limbs, and trunk muscles.
- Manifestations of neostigmine overdosage often appear first in muscles of neck and those involved in chewing and swallowing,
with muscles of shoulder girdle and upper extremities affected next.
- Report to physician if patient does not urinate within 1 h after first dose when used to relieve urinary retention.
Patient & Family Education
- Be aware that regulation of dosage interval is extremely difficult; dosage must be adjusted for each patient to deal with
unpredictable exacerbations and remissions.
- Keep a diary of "peaks and valleys" of muscle strength.
- Keep an accurate record for physician of your response to drug. Learn how to recognize adverse effects, how to modify dosage
regimen according to your changing needs, or how to administer atropine if necessary.
- Be aware that certain factors may require an increase in size or frequency of dose (e.g., physical or emotional stress,
infection, menstruation, surgery), whereas remission requires a decrease in dosage.
- Some patients become refractory to neostigmine after prolonged use and require change in dosage or medication.