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Pronunciation
(nee oh STIG meen)
Generic Available (U.S.)
Yes: Injection
Index Terms
Brand Names: U.S.
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Reversal of the effects of nondepolarizing neuromuscular-blocking agents; treatment of myasthenia gravis; prevention and treatment of postoperative bladder distention and urinary retention
Pregnancy Risk Factor
C
Pregnancy Considerations
Animal reproduction studies have not been conducted; anticholinesterases have caused uterine irritability and induced premature labor with I.V. use in near-term pregnant women.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to neostigmine, bromides, or any component of the formulation; GI or GU obstruction
Warnings/Precautions
Concerns related to adverse effects:
• Anticholinesterase insensitivity: For brief or prolonged periods, anticholinesterase insensitivity can develop.
• Cholinergic effects: Discontinue if symptoms of excess cholinergic activity (eg, salivation, sweating, urinary incontinence); overdosage may result in cholinergic crisis, which must be distinguished from myasthenic crisis.
• Hypersensitivity reactions: Have atropine and epinephrine ready to treat hypersensitivity reactions.
Disease-related concerns:
• Asthma: Use with caution in patients with asthma.
• Cardiovascular disease: Use with caution in patients with bradycardia and cardiac arrhythmias.
• GI disease: Use with caution in patients with GI disease, including peptic ulcer disease.
• Hyperthyroidism: Use with caution in patients with hyperthyroidism.
• Myasthenia gravis: Adequate facilities should be available for cardiopulmonary resuscitation when testing and adjusting dose for myasthenia gravis.
• Seizure disorder: Use with caution in patients with a history of seizure disorder.
• Vagotonia: Not generally recommended for use in patients with vagotonia.
Concurrent drug therapy issues:
• Muscle relaxants: Does not antagonize and may prolong the Phase I block of depolarizing muscle relaxants (eg, succinylcholine).
Adverse Reactions
Frequency not defined.
Cardiovascular: Arrhythmias (especially bradycardia), AV block, cardiac arrest, flushing, hypotension, nodal rhythm, nonspecific ECG changes, syncope, tachycardia
Central nervous system: Convulsions, dizziness, drowsiness, dysarthria, dysphonia, headache, loss of consciousness
Dermatologic: Skin rash, thrombophlebitis (I.V.), urticaria
Gastrointestinal: Diarrhea, dysphagia, flatulence, hyperperistalsis, nausea, salivation, stomach cramps, vomiting
Genitourinary: Urinary urgency
Neuromuscular & skeletal: Arthralgias, fasciculations, muscle cramps, spasms, weakness
Ocular: Lacrimation, small pupils
Respiratory: Bronchiolar constriction, bronchospasm, dyspnea, increased bronchial secretions, laryngospasm, respiratory arrest, respiratory depression, respiratory muscle paralysis
Miscellaneous: Allergic reactions, anaphylaxis, diaphoresis increased
Metabolism/Transport Effects
None known.
Drug Interactions
Beta-Blockers: Acetylcholinesterase Inhibitors may enhance the bradycardic effect of Beta-Blockers. Exceptions: Levobunolol; Metipranolol. Risk C: Monitor therapy
Cholinergic Agonists: Acetylcholinesterase Inhibitors may enhance the adverse/toxic effect of Cholinergic Agonists. Risk C: Monitor therapy
Corticosteroids (Systemic): May enhance the adverse/toxic effect of Acetylcholinesterase Inhibitors. Increased muscular weakness may occur. Risk C: Monitor therapy
Dipyridamole: May diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy
Neuromuscular-Blocking Agents (Nondepolarizing): Acetylcholinesterase Inhibitors may diminish the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Risk C: Monitor therapy
Succinylcholine: Acetylcholinesterase Inhibitors may increase the serum concentration of Succinylcholine. Management: Consider alternatives to this combination due to a risk of prolonged neuromuscular blockade. Risk D: Consider therapy modification
Compatibility
Stable in D5LR, D51/4NS, D51/2NS, D5NS, D5W, D10W, LR, NS.
Y-site administration: Compatible: Heparin, hydrocortisone sodium succinate, palonosetron, potassium chloride, vitamin B complex with C.
Compatibility in syringe: Compatible: Glycopyrrolate, heparin, ondansetron, pentobarbital, thiopental.
Mechanism of Action
Inhibits destruction of acetylcholine by acetylcholinesterase which facilitates transmission of impulses across myoneural junction
Pharmacodynamics/Kinetics
Onset of action: I.M.: 20-30 minutes; I.V.: 1-20 minutes
Duration: I.M.: 2.5-4 hours; I.V.: 1-2 hours
Absorption: Oral: Poor, <2%
Metabolism: Hepatic
Half-life elimination: Normal renal function: 0.5-2.1 hours; End-stage renal disease: Prolonged
Excretion: Urine (50% as unchanged drug)
Dosage
Myasthenia gravis: Diagnosis: I.M.: Note: In the diagnosis of myasthenia gravis, all anticholinesterase medications should be discontinued for at least 8 hours before administering neostigmine.
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., SubQ: 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; interval between doses must be individualized to maximal response
I.M., I.V., SubQ: 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 (must administer atropine several minutes prior to neostigmine): 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., SubQ:
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:
Clcr 10-50 mL/minute: Administer 50% of normal dose
Clcr <10 mL/minute: Administer 25% of normal dose
Administration: I.M.
In the diagnosis of myasthenia gravis, all anticholinesterase medications should be discontinued for at least 8 hours before administering neostigmine.
Administration: I.V.
May be administered undiluted by slow I.V. injection over several minutes.
Administration: I.V. Detail
pH: 5.9 (adjusted)
Patient Education
You may experience visual difficulty (eg, blurring and dark adaptation) or urinary frequency. Promptly report any muscle weakness, respiratory difficulty, severe or unresolved diarrhea, persistent abdominal cramping or vomiting, sweating, or tearing.
Geriatric Considerations
Many elderly will have diseases which may influence the use of neostigmine. Also, many elderly will need doses reduced by 50% due to creatinine clearances in the 10-50 mL/minute range. Side effects or concomitant disease may warrant use of pyridostigmine.
Additional Information
In the diagnosis of myasthenia gravis, all anticholinesterase medications should be discontinued for at least 8 hours before administering neostigmine.
Anesthesia and Critical Care Concerns/Other Considerations
Clinical Pearls/Comments: Neostigmine has occasionally been used to improve gastrointestinal motility (Ponec, 1999; van der Spoel, 2001). Atropine may be needed to treat symptomatic bradycardia.
Evidence-based Information: Atropine or glycopyrrolate should be administered along with edrophonium when reversing the effects of nondepolarizing agents to antagonize the cholinergic effects at the muscarinic receptors.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May rarely cause drowsiness, restlessness, or agitation
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Used for MG diagnosis by prescribers. For bladder atony, assess bladder adequacy prior to treatment. Monitor for cholinergic crisis.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Injection, solution, as methylsulfate: 0.5 mg/mL (10 mL); 1 mg/mL (10 mL)
Prostigmin®: 0.5 mg/mL (1 mL [DSC], 10 mL [DSC]); 1 mg/mL (10 mL [DSC])
Tablet, oral, as bromide:
Prostigmin®: 15 mg [scored]
References
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.
Ponec RJ, Saunders MD, and Kimmey MB, "Neostigmine for the Treatment of Acute Colonic Pseudo-Obstruction," N Engl J Med, 1999, 341(3):137-41.
van der Spoel JI, Oudemans-van Straaten HM, Stoutenbeek CP, et al, "Neostigmine Resolves Critical Illness-Related Colonic Ileus in Intensive Care Patients With Multiple Organ Failure--A Prospective, Double-Blind, Placebo-Controlled Trial,"Intensive Care Med, 2001, 27(5):822-7.
International Brand Names
Lexi-Comp.com
Last full review/revision March 2012
Content last modified March 2012
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