edrophonium (Tensilon)
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Introduction
Tradename: Tensilon.
Indications
- evaluation for myasthenia gravis
- reversal of neuromuscular block
- reversal of effects of non-depolarizing neuromuscular blocking agents (atracurium, gallamine, pancuronium, tubocurarine)
- neostigmine & pyridostigmine are preferred agents
- reversal of effects of non-depolarizing neuromuscular blocking agents (atracurium, gallamine, pancuronium, tubocurarine)
Dosage
Diagnosis of myasthenia gravis:
- discontinue all anticholinesterase medications at least 8 hours prior to administration of edrophonium
- draw 10 mg of edrophonium into a syringe
- 2 mg test IV over 15-30 seconds
- if a cholinergic reaction occurs, stop infusion
- administer 0.5 mg of atropine IV
- 8 mg IV after 45 sec if no response to test dose
- test may be repeated after 30 minutes
Reversal of neuromuscular block:
- 10 mg IV slowly over 30-45 seconds
- maximal dose 40 mg Phamacokinetics:
- rapid onset & shorter duration following IV administration than neostigmine of pyridostigmine
- effect on skeletal muscle begins within 30-60 seconds
- duration: 5-10 minutes
Adverse effects
- common (> 10%)
- less common (1-10%)
- urinary urgency, increased bronchial secretions, miosis
- uncommon (< 1%)
- other
- diarrhea
- increased peristalsis
- hypotension
Drug interactions
- edrophonium does not antagonize the effects of depolarizing agents
- digoxin may increase the sensitivity of the heart to edrophonium, resulting in AV block
- drug interaction(s) of cholinesterase inhibitors with NSAIDs
- drug interaction(s) of parasympatholytic with parasympathomimetic
Mechanism of action
- reversible cholinesterase inhibitor
- accumulation of acetylcholine at cholinergic synapses
- quaternary ammonium salt, thus does not cross the blood- brain barrier with moderate dosing
More general terms
Component of
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