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Pronunciation |
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(ed
roe FOE nee
um) |
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U.S. Brand
Names |
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Enlon® Injection; Reversol®
Injection; Tensilon®
Injection |
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Generic
Available |
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No |
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Synonyms |
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Edrophonium Chloride |
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Pharmacological Index |
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Antidote; Cholinergic Agonist; Diagnostic Agent, Myasthenia
Gravis |
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Use |
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Diagnosis of myasthenia gravis; differentiation of cholinergic crises from
myasthenia crises; reversal of nondepolarizing neuromuscular blockers; treatment
of paroxysmal atrial tachycardia |
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Pregnancy Risk
Factor |
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C |
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Contraindications |
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Hypersensitivity to edrophonium or any component, GI or GU obstruction,
hypersensitivity to sulfite agents |
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Warnings/Precautions |
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Use with caution in patients with bronchial asthma and those receiving a
cardiac glycoside; atropine sulfate should always be readily available as an
antagonist. Overdosage can cause cholinergic crisis which may be fatal. I.V.
atropine should be readily available for treatment of cholinergic
reactions. |
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Adverse
Reactions |
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>10%:
Gastrointestinal: Nausea, vomiting, diarrhea, excessive salivation, stomach
cramps
Miscellaneous: Diaphoresis (increased)
1% to 10%:
Genitourinary: Polyuria
Ocular: Small pupils, lacrimation
Respiratory: Increased bronchial secretions
<1%: Bradycardia, A-V block, seizures, headache, drowsiness, dysphoria,
weakness, muscle cramps, muscle spasms, thrombophlebitis, diplopia, miosis,
laryngospasm, bronchospasm, respiratory paralysis, hypersensitivity,
hyper-reactive cholinergic responses |
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Overdosage/Toxicology |
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Symptoms of overdose include muscle weakness, nausea, vomiting, miosis,
bronchospasm, respiratory paralysis
Maintain adequate airway; antidote is atropine for muscarinic symptoms;
pralidoxime (2-PAM) may also be needed to reverse severe muscle weakness or
paralysis; skeletal muscle effects of edrophonium not alleviated by atropine.
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Drug
Interactions |
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Decreased effect: Atropine, nondepolarizing muscle relaxants, procainamide,
quinidine
Increased effect: Succinylcholine, digoxin, I.V. acetazolamide, neostigmine,
physostigmine |
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Mechanism of
Action |
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Inhibits destruction of acetylcholine by acetylcholinesterase. This
facilitates transmission of impulses across myoneural junction and results in
increased cholinergic responses such as miosis, increased tonus of intestinal
and skeletal muscles, bronchial and ureteral constriction, bradycardia, and
increased salivary and sweat gland secretions. |
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Pharmacodynamics/Kinetics |
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I.M.:
Onset of effect: Within 2-10 minutes
Duration: 5-30 minutes
I.V.:
Onset of effect: Within 30-60 seconds
Duration: 10 minutes
Distribution: Vd: 1.1 L/kg
Half-life: 1.8 hours |
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Usual Dosage |
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Usually administered I.V., however, if not possible, I.M. or S.C. may be
used:
I.M.: 0.5-1 mg
I.V.: Initial: 0.1 mg, followed by 0.4 mg if no response; total dose = 0.5 mg
Children:
Diagnosis: Initial: 0.04 mg/kg over 1 minute followed by 0.16 mg/kg if no
response, to a maximum total dose of 5 mg for children <34 kg, or 10 mg for
children >34 kg
I.M.:
<34 kg: 1 mg
>34 kg: 5 mg
Titration of oral anticholinesterase therapy: 0.04 mg/kg once given 1 hour
after oral intake of the drug being used in treatment; if strength improves, an
increase in neostigmine or pyridostigmine dose is indicated
Adults:
Diagnosis:
I.V.: 2 mg test dose administered over 15-30 seconds; 8 mg given 45 seconds
later if no response is seen; test dose may be repeated after 30 minutes
I.M.: Initial: 10 mg; if no cholinergic reaction occurs, administer 2 mg 30
minutes later to rule out false-negative reaction
Titration of oral anticholinesterase therapy: 1-2 mg given 1 hour after oral
dose of anticholinesterase; if strength improves, an increase in neostigmine or
pyridostigmine dose is indicated
Reversal of nondepolarizing neuromuscular blocking agents (neostigmine with
atropine usually preferred): I.V.: 10 mg over 30-45 seconds; may repeat every
5-10 minutes up to 40 mg
Termination of paroxysmal atrial tachycardia: I.V. rapid injection: 5-10 mg
Differentiation of cholinergic from myasthenic crisis: I.V.: 1 mg; may repeat
after 1 minute. Note: Intubation and controlled ventilation may be
required if patient has cholinergic crisis
Dosing adjustment in renal impairment: Dose may need to be reduced in
patients with chronic renal failure |
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Administration |
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Edrophonium is administered by direct I.V. injection; see Usual
Dosage |
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Test
Interactions |
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aminotransferase [ALT
(SGPT)/AST (SGOT)] (S),
amylase (S) |
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Mental Health: Effects
on Mental Status |
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May cause drowsiness |
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Mental Health:
Effects on Psychiatric
Treatment |
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None reported |
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Patient
Information |
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Pregnancy/breast-feeding precautions: Inform prescriber if you are or
intend to be pregnant. Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Parenteral: Edrophonium is administered by direct I.V. injection
Monitor pre- and postinjection strength (cranial musculature is most useful);
heart rate, respiratory rate, blood pressure |
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Dosage Forms |
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Injection, as chloride: 10 mg/mL (1 mL, 10 mL, 15 mL) |
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References |
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Fisher DM, et al,
"Clinical Pharmacology of Edrophonium in Infants and Children,"
Anesthesiology, 1984, 61(4):428-33.
Rossen RN, Krikorian J, and Hancock EW,
"Ventricular Asystole After Edrophonium Chloride Administration," JAMA,
1976, 235(10):1041-2.
Youngberg JA,
"Cardiac Arrest Following Treatment of Paroxysmal Atrial Tachycardia With Edrophonium,"
Anesthesiology, 1979, 50(3):234-5.
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