Generic
Neostigmine Methylsulphate
5 brands available in the market
At a glance
Neostigmine Methylsulphate is a reversible cholinesterase inhibitor used for myasthenia gravis, paralytic ileus, post-operative urinary retention and reversal of skeletal muscle relaxant effects after surgery.
Description
Neostigmine Methylsulfate Injection is an anticholinesterase agent for IM, IV or SC administration. Neostigmine is a parasympathomimetic, specifically a reversible cholinesterase inhibitor. It inhibits acetylcholinesterase to increase acetylcholine levels, stimulating nicotinic and muscarinic receptors involved in muscle contraction.
Indications
- Symptomatic control of myasthenia gravis (when oral therapy is impractical)
- Prevention and treatment of postoperative distention and urinary retention
- Reversal of nondepolarizing neuromuscular blocking agents
Therapeutic class
Anti-cholinesterases, Drugs used in Myasthenia Gravis
Pharmacological class
Reversible Cholinesterase Inhibitor
Pharmacology
Neostigmine inhibits acetylcholinesterase to increase acetylcholine levels in the synaptic cleft, stimulating nicotinic and muscarinic receptors to cause muscle contraction.
Mechanism of action
Improves muscle contraction and nerve transmission by increasing acetylcholine levels.
Dosage
Reversal of Neuromuscular Blockade:
- Adults: 2-3 mg + atropine 0.6-1.2 mg, slow IV over 1 min; max 5 mg
- Children: 0.05 mg/kg + atropine 0.02 mg/kg, slow IV; max 2.5 mg
Myasthenia Gravis (Adults): 1-2.5 mg IM/SC, up to 5-20 mg daily
Myasthenia Gravis (Neonates): 0.05-0.25 mg IM every 2-4 hours
Urinary Retention Prophylaxis: 0.25 mg SC/IM every 4-6 hours for 2-3 days
Urinary Retention Treatment: 0.5 mg SC/IM
Administration
- Administered by doctor or nurse IM/IV/SC
- IV: Administer slowly over at least 1 minute
- Use separate syringes for neostigmine and atropine
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Side Effects (Overdose):
- Cardiac arrhythmias (especially bradycardia)
- Hypotension, cardiac arrest, syncope
- Headache, dizziness, convulsions, coma
- Nausea, vomiting, diarrhea, abdominal cramps
- Muscle cramps, fasciculation, paralysis
- Respiratory depression, bronchospasm
- Allergic reactions (including anaphylaxis)
Precautions & warnings
- Caution in epilepsy, bronchial asthma, bradycardia, coronary occlusion, vagotonia, hyperthyroidism, cardiac arrhythmias or peptic ulcer
- Keep atropine and antishock medication readily available
- Overdose may cause cholinergic crisis
- Important to differentiate from myasthenic crisis
Contraindications
- Hypersensitivity
- Peritonitis
- Mechanical obstruction of intestinal or urinary tract
Drug interactions
- May reduce effects of anticholinergics
- May increase effects of cholinergic agonists
- Effects antagonized by aminoglycosides, clindamycin, colistin
Food interactions
Alcohol may cause excessive drowsiness.
Use in pregnancy
Use in Pregnancy: Neostigmine may be unsafe during pregnancy (Category C); use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Neostigmine is probably safe during breastfeeding; no significant risk to baby.
Pediatric use
Dose established for children and neonates (myasthenia gravis).
Geriatric use
Elderly may require dose adjustment.
Renal / hepatic impairment
Renal Impairment: Caution in kidney disease; dose adjustment may be needed.
Hepatic Impairment: Safe in liver disease.
Overdose effects
Overdose: Cholinergic crisis; diagnose with edrophonium; treat with atropine.
Storage conditions
Store at controlled room temperature protected from light; discard unused portion.
Chemical structure
Neostigmine Methylsulphate Injection