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neostigmine (Prostigmin)
Tradename: Prostigmin. Neostigmine bromide.
Indications:
1) myasthenia gravis
a) diagnostic aid
b) treatment
2) neuromuscular block
- antidote for non-depolarizing neuromuscular blocking agents, (tubocurarine, pancuronium)
3) prevention & treatment of post-operative bladder distension & urinary retention
Dosage:
1) myasthenia gravis
a) diagnosis:
1] adults: 0.02 mg//kg IM as single dose
2] children: 0.04 mg//kg IM as single dose
b) treatment
1] 0.5-2.4 mg IM/IV/SC every 1-3 hours
2] 15-375 mg/day PO in divided every 3-4 hours
3] 15 mg PO every 3-4 hours
4] children:
a] 0.01-0.04 mg/kg IM/IV/SC every 2-4 hours
b] 2 mg/kg/day divided every 3-4 hours
3) surgery:
a) dosage titrated using a peripheral nerve stimulator
b) 0.5-2.5 mg IV should antagonize most non-depolarizing neuromuscular blocks in most adults
4) bladder atony: adults
a) prevention: 0.25 mg IM/SC every 4-6 hours for 2-3 days
b) treatment:
-> 0.5-1 mg every 3 hours for 5 doses after emptying bladder
5) 0.6-1.2 mg of atropine or 0.2-0.6 mg of glycopyrrolate should be given a few minutes before neostigmine to counteract muscarinic effects
Tabs: 15 mg.
Injection: (methylsulfate)
- 0.5 mg/mL (1:2000) (1 mL), 1 mg/mL (1:1000) (10 mL)
Pharmacokinetics:
1) poorly absorbed orally (1-2%)
2) peak plasma effects occur in 1-2 hours with variable duration of action
3) effects on peristaltic activity occur 10-30 minutes after parenteral administration
4) effects on skeletal muscle effects occur within 20-30 minutes after parenteral administration
5) effects last 2.5-4 hours
6) 1/2life 52-90 minutes
7) metabolized in the liver, excreted in the urine
Adverse effects:
1) common (> 10%)
- diarrhea, increased sweating, excessive salivation, nausea, epigastric cramps
2) less common (1-10%)
- urge to urinate, increased bronchial secretions, miosis, lacrimation
3) uncommon (< 1%)
- thrombophlebitis, bradycardia, AV-block, seizures, headache, dysphoria, drowsiness, muscle spasms, diplopia, laryngospasm, respiratory paralysis, hypersensitivity, hyper-reactive cholinergic responses, weakness
4) other [2]
- muscle cramps
- fasciculations
- hypotension
Toxicity: atropine sulfate should be available as an antagonist for effects of neostigmine
Mechanism of action:
1) competitively binds to & inhibits acetylcholinesterase
2) produces generalized cholinergic response
a) miosis
b) increased tone of skeletal & intestinal musculature
c) constriction of bronchi & ureters
d) bradycardia
e) stimulation of secretion by salivary & sweat glands
3) quaternary ammonium salt, does not cross blood-brain barrier
Interactions
drug interactions
drug adverse effects of cholinesterase inhibitors
General
cholinesterase inhibitor
neurologic agent
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Deprecated Reference