No

Acetylcholinesterase Inhibitor

Diagnosis and treatment of myasthenia gravis and prevent and treat postoperative bladder distention and urinary retention; reversal of the effects of nondepolarizing neuromuscular blocking agents after surgery

C

Hypersensitivity to neostigmine, bromides or any component; GI or GU obstruction

Does not antagonize and may prolong the phase I block of depolarizing muscle relaxants (eg, succinylcholine); use with caution in patients with epilepsy, asthma, bradycardia, hyperthyroidism, cardiac arrhythmias, or peptic ulcer; adequate facilities should be available for cardiopulmonary resuscitation when testing and adjusting dose for myasthenia gravis; have atropine and epinephrine ready to treat hypersensitivity reactions; overdosage may result in cholinergic crisis, this must be distinguished from myasthenic crisis; anticholinesterase insensitivity can develop for brief or prolonged periods

>10%:

Gastrointestinal: Hyperperistalsis, nausea, vomiting, salivation, diarrhea, stomach cramps

Miscellaneous: Diaphoresis (increased)

1% to 10%:

Genitourinary: Urge to urinate

Ocular: Small pupils, lacrimation

Respiratory: Increased bronchial secretions

<1%: A-V block, bradycardia, hypotension, bradyarrhythmias, asystole, dysphoria, restlessness, agitation, seizures, headache, drowsiness, thrombophlebitis, muscle spasms, tremor, weakness, fasciculations, diplopia, miosis, laryngospasm, respiratory paralysis, hypersensitivity, hyper-reactive cholinergic responses, bronchoconstriction

Symptoms of overdose include muscle weakness, blurred vision, excessive sweating, tearing and salivation, nausea, vomiting, diarrhea, hypertension, bradycardia, muscle weakness, paralysis

Atropine sulfate injection should be readily available as an antagonist for the effects of neostigmine

Decreased effect: Antagonizes effects of nondepolarizing muscle relaxants (eg, pancuronium, tubocurarine); atropine antagonizes the muscarinic effects of neostigmine

Increased effect: Neuromuscular blocking agents effects are increased

Inhibits destruction of acetylcholine by acetylcholinesterase which facilitates transmission of impulses across myoneural junction

Onset of effect: I.M.: Within 20-30 minutes; I.V.: Within 1-20 minutes

Duration: I.M.: 2.5-4 hours; I.V.: 1-2 hours

Absorption: Oral: Poor, <2%

Metabolism: In the liver

Half-life: Normal renal function: 0.5-2.1 hours; End-stage renal disease: Prolonged

Elimination: 50% excreted renally as unchanged drug

Myasthenia gravis: Diagnosis: I.M.:

Children: 0.04 mg/kg as a single dose

Adults: 0.02 mg/kg as a single dose

Myasthenia gravis: Treatment:

Children:

Oral: 2 mg/kg/day divided every 3-4 hours

I.M., I.V., S.C.: 0.01-0.04 mg/kg every 2-4 hours

Adults:

Oral: 15 mg/dose every 3-4 hours up to 375 mg/day maximum

I.M., I.V., S.C.: 0.5-2.5 mg every 1-3 hours up to 10 mg/24 hours maximum

Reversal of nondepolarizing neuromuscular blockade after surgery in conjunction with atropine: I.V.:

Infants: 0.025-0.1 mg/kg/dose

Children: 0.025-0.08 mg/kg/dose

Adults: 0.5-2.5 mg; total dose not to exceed 5 mg

Bladder atony: Adults: I.M., S.C.:

Prevention: 0.25 mg every 4-6 hours for 2-3 days

Treatment: 0.5-1 mg every 3 hours for 5 doses after bladder has emptied

Dosing adjustment in renal impairment:

Cl_cr 10-50 mL/minute: Administer 50% of normal dose

Cl_cr <10 mL/minute: Administer 25% of normal dose

May be given undiluted by slow I.V. injection over several minutes

aminotransferase [ALT (SGPT)/AST (SGOT)] (S), amylase (S)

May rarely cause drowsiness, restlessness, or agitation

None reported

Take this drug exactly as prescribed. You may experience visual difficulty (eg, blurring and dark adaptation - use caution at night) or urinary frequency. Promptly report any muscle weakness, respiratory difficulty, severe or unresolved diarrhea, persistent abdominal cramping or vomiting, sweating, or tearing. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Breast-feeding is not recommended.

In the diagnosis of myasthenia gravis, all anticholinesterase medications should be discontinued for at least 8 hours before administering neostigmine

Injection, as methylsulfate: 0.25 mg/mL (1 mL); 0.5 mg/mL (1 mL, 10 mL); 1 mg/mL (10 mL)

Tablet, as bromide: 15 mg

Fisher DM, Cronnelly R, Miller RD, et al, "The Neuromuscular Pharmacology of Neostigmine in Infants and Children," Anesthesiology, 1983, 59(3):220-5.

Payne JP, Hughes R, and Al Azawi S, "Neuromuscular Blockade by Neostigmine in Anaesthetized Man," Br J Anaesth, 1980, 52(1):69-76.