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Home > Medical Reference > Encyclopedia (English)



 

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Pronunciation:

(ed roe FOE nee um)

U.S. Brand Names:

Enlon®; Reversol®

Synonyms:

Edrophonium Chloride

Generic Available:

No

Canadian Brand Names:

Enlon®

Use:

Diagnosis of myasthenia gravis; differentiation of cholinergic crises from myasthenia crises; reversal of nondepolarizing neuromuscular blockers; adjunct treatment of respiratory depression caused by curare overdose

Pregnancy Risk Factor:

C

Lactation:

Excretion in breast milk unknown

Contraindications:

Hypersensitivity to edrophonium, sulfites, or any component of the formulation; GI or GU obstruction

Warnings/Precautions:

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.

Adverse Reactions:

Frequency not defined.

Cardiovascular: Arrhythmias (especially bradycardia), hypotension, decreased carbon monoxide, tachycardia, AV block, nodal rhythm, nonspecific ECG changes, cardiac arrest, syncope, flushing

Central nervous system: Convulsions, dysarthria, dysphonia, dizziness, loss of consciousness, drowsiness, headache

Dermatologic: Skin rash, thrombophlebitis (I.V.), urticaria

Gastrointestinal: Hyperperistalsis, nausea, vomiting, salivation, diarrhea, stomach cramps, dysphagia, flatulence

Genitourinary: Urinary urgency

Neuromuscular & skeletal: Weakness, fasciculations, muscle cramps, spasms, arthralgia

Ocular: Small pupils, lacrimation

Respiratory: Increased bronchial secretions, laryngospasm, bronchiolar constriction, respiratory muscle paralysis, dyspnea, respiratory depression, respiratory arrest, bronchospasm

Miscellaneous: Diaphoresis (increased), anaphylaxis, allergic reactions

Overdosage/Toxicology:

Symptoms of overdose include muscle weakness, nausea, vomiting, miosis, bronchospasm, and respiratory paralysis. Maintain an adequate airway. For muscarinic symptoms, the antidote is atropine 0.4-0.5 mg I.V. repeated every 3-10 minutes (initial doses as high as 1.2 mg have been administered). Skeletal muscle effects of edrophonium are not alleviated by atropine.

Drug Interactions:

Decreased effect: Atropine, nondepolarizing muscle relaxants, procainamide, quinidine

Increased effect: Succinylcholine, digoxin, I.V. acetazolamide, neostigmine, physostigmine

Compatibility:

Y-site administration: Compatible: Heparin, hydrocortisone sodium succinate, potassium chloride, vitamin B complex with C

Mechanism of Action:

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.

Pharmacodynamics/Kinetics:

Onset of action: I.M.: 2-10 minutes; I.V.: 30-60 seconds

Duration: I.M.: 5-30 minutes: I.V.: 10 minutes

Distribution: Vd: 1.1 L/kg

Half-life elimination: 1.8 hours

Dosage:

Usually administered I.V., however, if not possible, I.M. or SubQ may be used:

Infants:

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 or

Alternative dosing (manufacturer's recommendation):

34 kg: 1 mg; if no response after 45 seconds, repeat dosage in 1 mg increments every 30-45 seconds, up to a total of 5 mg

>34 kg: 2 mg; if no response after 45 seconds, repeat dosage in 1 mg increments every 30-45 seconds, up to a total of 10 mg

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

Administration:

Edrophonium is administered by direct I.V. injection; see Dosage

Monitoring Parameters:

Pre- and postinjection strength (cranial musculature is most useful); heart rate, respiratory rate, blood pressure

Test Interactions:

Increased aminotransferase [ALT (SGPT)/AST (SGOT)] (S), amylase (S)

Patient Education:

Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Additional Information:

Atropine should be administered along with edrophonium when reversing the effects of nondepolarizing agents to antagonize the cholinergic effects at the muscarinic receptors, especially bradycardia. It is important to recognize the difference in dose for diagnosis of myasthenia gravis versus reversal of muscle relaxant, a much larger dose is needed for desired effect of reversal of muscle paralysis.

Anesthesia and Critical Care Concerns/Other Considerations:

Atropine should be administered along with edrophonium when reversing the effects of nondepolarizing agents to antagonize the cholinergic effects at the muscarinic receptors, especially bradycardia; important to recognize the difference in dose for diagnosis of myasthenia gravis versus reversal of muscle relaxant, a much larger dose is needed for desired effect of reversal of muscle paralysis

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Mental Health: Effects on Mental Status:

May cause drowsiness

Mental Health: Effects on Psychiatric Treatment:

None reported

Dosage Forms:

Injection, solution, as chloride:

Enlon®: 10 mg/mL (15 mL) [contains sodium sulfite]

Reversol®: 10 mg/mL (10 mL) [contains sodium sulfite]

International Brand Names:

Anticude® (ES); Edrophonium® (GB); Enlon® (CA); Tensilon® (ZA)

References

Azar I, Pham AN, Karamkekar, et al, "The Heart Rate Following Edrophonium-Atropine and Edrophonium Glycopyrrolate Mixtures,"Anesthesiology, 1983, 59(2):139-41.

Cronnely R and Morris RB, "Antagonism of Neuromuscular Blockade,"Br J Anaesth, 1982, 54(2):183-93.

Fisher DM, et al, "Clinical Pharmacology of Edrophonium in Infants and Children,"Anesthesiology, 1984, 61(4):428-33.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings,"Chest, 2003, 123(3):897-922.

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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