A-Z Drug Facts > Neostigmine

Neostigmine

Pronouncation: (nee-oh-STIGG-meen)
Class: Anticholinesterase muscle stimulant

Trade Names:
Prostigmin
- Tablets 15 mg
- Injection 1:1,000
- Injection 1:2,000
- Injection 1:4,000

Pharmacology

Facilitates myoneural junction impulse transmission by inhibiting acetylcholine destruction by cholinesterase.

Pharmacokinetics

Absorption

Rapid absorption of neostigmine methylsulfate. T _max is 30 min.

Distribution

Neostigmine protein binding is 15% to 25% serum albumin.

Metabolism

Neostigmine is metabolized in the liver by microsomal enzymes.

Elimination

Neostigmine is eliminated in urine (50% as unchanged), t _½ is 51 to 90 min, and plasma t _½ is 47 to 60 min.

Onset

Onset of IM neostigmine is 20 to 30 min.

Duration

Duration of IM neostigmine is 2.5 to 4 h.

Indications and Usage

Neostigmine bromide (oral) and methylsulfate (injection)

Symptomatic control of myasthenia gravis; antidote for nondepolarizing neuromuscular blocking agents after surgery.

Neostigmine methylsulfate

Prevention and treatment of postoperative distention and urinary retention.

Contraindications

Hypersensitivity to anticholinesterases and bromides; mechanical intestinal or urinary obstruction; peritonitis.

Dosage and Administration

Antidote
Adults

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.

Control of Myasthenia Gravis
Adults

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 Retention
Adults

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 Distention
Adults

Subcutaneous / IM 1 mL of 1:2,000 solution (0.5 mg), as required.

Treatment of Urinary Retention
Adults

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.

General Advice

• Injection
• For IV, subcutaneous, or IM administration. Not for intradermal or intra-arterial administration.
• Do not administer if particulate matter or discoloration noted.

• Tablets
• Administer as prescribed. Size of dose (eg, number of tablets) and frequency of administration will be adjusted to provide max relief of myasthenia gravis symptoms.
• Administer without regard to meals. Administer with food if GI upset occurs.

Ensure that parenteral atropine is available for emergency treatment of cholinergic crisis.

Storage/Stability

Store tablets and injection at controlled room temperature (59° to 86°F). Keep injection in carton until ready to use and protect from light.

Drug Interactions

Corticosteroids

May antagonize anticholinesterases in myasthenia gravis, producing profound muscular depression.

Local/general anesthetics, antiarrhythmic agents

Use with caution, may interfere with neuromuscular transmission.

Streptomycin, kanamycin

May accentuate neuromuscular block.

Succinylcholine

Neuromuscular blockade produced by succinylcholine may be prolonged.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Arrhythmia (bradycardia, tachycardia, AV block, nodal rhythm); nonspecific ECG changes; cardiac arrest; hypotension; syncope.

CNS

Convulsions; dysarthria; dysphonia; dizziness; loss of consciousness; drowsiness; headache.

Dermatologic

Rash; urticaria; flushing.

EENT

Miosis.

GI

Vomiting; increased peristalsis; flatulence.

Genitourinary

Urinary frequency.

Respiratory

Increased oral, pharyngeal, and bronchial secretions, dyspnea; respiratory depression, respiratory arrest, and bronchospasm (injectable form).

Miscellaneous

Allergy and anaphylaxis; weakness; fasciculations; muscle cramps and spasms; arthralgia; diaphoresis.

Precautions

Monitor Frequently assess muscle strength and function in patient with myasthenia gravis or patient recovering from nondepolarizing neuromuscular blocking agent.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

Anaphylaxis may occur. Have atropine and antishock medications available.

Special Risk Patients

Use with caution in patients with epilepsy, bronchial asthma, bradycardia, recent coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias, or peptic ulcer.

Anticholinesterase insensitivity

May develop.

Overdosage

Symptoms

Abdominal cramps, miosis, diarrhea, sweating, excessive salivation, panic attacks, progressive muscle weakness leading to paralysis and death, urinary urgency, anxiety.

Patient Information

• Advise patient or caregiver that injection will be prepared and administered by a health care provider in a medical setting.
• Advise patient that dose and frequency of administration may be adjusted to achieve max benefit.
• Advise patient to take exactly as prescribed and not to change the dose or stop taking unless advised by health care provider.
• Advise patient to take prescribed dose without regard to meals but to take with food if stomach upset occurs.
• Advise patient with myasthenia gravis to keep a diary of medication administration times and times when muscle weakness or other symptoms occur. This log will help the health care provider adjust the dose and dosing interval to establish the most effective dose and times of administration.
• Instruct patient to contact health care provider immediately if any of the following occur: worsening muscle weakness, difficulty breathing, slow or irregular heart rate, dizziness, fainting, vomiting, severe abdominal pain.
• Advise patient that diarrhea, increased salivation, sweating, and nausea are common adverse reactions and to notify health care provider if any occur and are bothersome.

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