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edrophonium (Tensilon)
Tradename: Tensilon.
Indications:
1) evaluation for myasthenia gravis
2) reversal of neuromuscular block
- reversal of effects of non-depolarizing neuromuscular blocking agents (atracurium, gallamine, pancuronium, tubocurarine)
- neostigmine & pyridostigmine are preferred agents
Dosage:
Diagnosis of myasthenia gravis:
1) discontinue all anticholinesterase medications at least 8 hours prior to administration of edrophonium
2) draw 10 mg of edrophonium into a syringe
3) 2 mg test IV over 15-30 seconds
a) if a cholinergic reaction occurs, stop infusion
b) administer 0.5 mg of atropine IV
4) 8 mg IV after 45 sec if no response to test dose
5) test may be repeated after 30 minutes
Reversal of neuromuscular block:
1) 10 mg IV slowly over 30-45 seconds
2) maximal dose 40 mg Phamacokinetics:
1) rapid onset & shorter duration following IV administration than neostigmine of pyridostigmine
2) effect on skeletal muscle begins within 30-60 seconds
3) duration: 5-10 minutes
Adverse effects:
1) common (> 10%)
- diarrhea, increased sweating, excessive salivation, nausea/vomiting, abdominal cramps
2) less common (1-10%)
- urinary urgency, increased bronchial secretions, miosis
3) uncommon (< 1%)
- thrombophlebitis, bradycardia, AV block, seizures, headache, dysphoria, drowsiness, muscle spasms, diplopia, laryngospasm, respiratory paralysis, hypersensitivity, weakness
4) other
- diarrhea
- increased peristalsis
- hypotension
Drug interactions:
1) edrophonium does not antagonize the effects of depolarizing agents
2) digoxin may increase the sensitivity of the heart to edrophonium, resulting in AV block
Mechanism of action:
1) reversible cholinesterase inhibitor
2) accumulation of acetylcholine at cholinergic synapses
3) quaternary ammonium salt, thus does not cross the blood- brain barrier with moderate dosing
Interactions
drug interactions
drug adverse effects of cholinesterase inhibitors
General
cholinesterase inhibitor
neurologic agent
Properties
MISC-INFO: elimination route PLASMA
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
Component-of
atropine/edrophonium