Edrophonium chloride


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : IV Diagnosis of myasthenia gravis Initial: 2 mg over 15-30 seconds. If no reaction after 45 seconds, administer 8 mg. If reaction occurs, discontinue treatment. Anticholinesterase therapy evaluation 1-2 mg given 1 hr after oral anticholinesterase dose. Cholinergic and myasthenic crisis differentiation 1 mg, may repeat after 1 min. Reversal of nondepolarising neuromuscular blockade 10 mg over 30-45 seconds, may repeat as necessary. Max: 40 mg. Alternative: 0.5-1 mg/kg. IM Diagnosis of myasthenia gravis Initial: 10 mg. If reaction occurs, administer 2 mg after 30 min.
Dosage Details
Intramuscular
Diagnosis of myasthenia gravis
Adult: Initially, 10 mg. If cholinergic reaction occurs, administer 2 mg after 30 min to rule out false-negative reactions.
Child: ≤34 kg: 2 mg; >34 kg: 5 mg.

Intravenous
Diagnosis of myasthenia gravis
Adult: Initially, 2 mg test dose over 15-30 seconds. If no cholinergic reaction after 45 seconds, administer 8 mg. If reaction occurs, discontinue testing and then administer IV atropine. Test may be repeated after 30 min, if necessary.
Child: ≤34 kg: 1 mg test dose; >34 kg: 2 mg test dose. If no reaction after 45 seconds, 1 mg may be given every 30-45 seconds up to max cumulative dose of 5 mg (≤34 kg) or 10 mg (>34 kg). Infants: 0.5 mg.

Intravenous
Anticholinesterase therapy evaluation
Adult: 1-2 mg given 1 hr after oral anticholinesterase dose. Controlled patients show adequate response; undertreated patients show myasthenic response; and overtreated patients show cholinergic response.

Intravenous
Cholinergic and myasthenic crisis differentiation
Adult: 1 mg, may repeat after 1 min.

Intravenous
Reversal of neuromuscular blockade
Adult: Given to reverse blockade from nondepolarising agents: 10 mg given slowly over 30-45 seconds, may repeat every 5-10 min as necessary. Max total: 40 mg. Alternatively, 0.5-1 mg/kg.
Contraindications
Mechanical obstruction of GI or genitourinary tract.
Special Precautions
Patient w/ bronchial asthma, cardiac arrhythmia (e.g. bradyarrhythmia). Not indicated to reverse non-depolarising neuromuscular blockade in patients w/ myasthenia gravis. Childn. Pregnancy and lactation.
Adverse Reactions
Significant: Transient bradycardia, cardiac and resp arrest, anticholinesterase insensitivity.
Nervous: Weakness, seizure, dysarthria, dizziness, drowsiness, headache, loss of consciousness.
CV: Arrhythmia, hypotension, AV block, nonspecific ECG changes, flushing, syncope, tachycardia, thrombophlebitis.
GI: Nausea, vomiting, diarrhoea, abdominal cramps, increased peristalsis, increased gastric and intestinal secretions, dysphagia, dysphonia, flatulence.
Resp: Laryngospasm, increased bronchial secretions, bronchospasm, resp paralysis.
Genitourinary: Urinary frequency, urgency, and incontinence.
Musculoskeletal: Muscle cramps, fasciculation.
Ophthalmologic: Increased lacrimation, miosis, accommodation spasm, diplopia, conjunctival hyperaemia.
Dermatologic: Diaphoresis, rash, urticaria.
Potentially Fatal: Cholinergic crisis, asthma.
IM/IV/Parenteral: C
MonitoringParameters
Monitor pre- and post-injection strength, heart and resp rate, and BP.
Overdosage
Symptoms: Cholinergic crisis manifesting as nausea, vomiting, diarrhoea, excessive sweating, increased bronchial and salivary secretions, bradycardia or tachycardia, cardiospasm, hypotension, blurred vision, weakness, incoordination, muscle cramps, fasciculation, paralysis, bronchospasm, airway obstruction, resp paralysis, pulmonary oedema, cardiac arrest. Management: Administer 0.4-0.5 mg IV atropine, repeated every 3-10 min to control cholinergic symptoms. Maintain adequate respiration by assuring an open airway (through tracheostomy, bronchial aspiration, and postural drainage) and providing assisted respiration w/ oxygen. Monitor cardiac function until complete stabilisation. In case of airway obstruction due to bronchial secretions, administer up to 1.2 mg IV atropine, repeated every 20 min until secretions are controlled.
Drug Interactions
Antagonised muscarinic effects w/ atropine. May cause an increased sensitivity of the heart to edrophonium when given w/ digitalis. May prolong the phase 1 blockade of depolarising muscle relaxants (e.g. suxamethonium, decamethonium). May antagonise the effects of nondepolarising muscle relaxants (e.g. atracurium, pancuronium, vecuronium, tubocurarine, metocurine).
Action
Description: Edrophonium chloride is a synthetic quaternary ammonium cholinergic agent. It reversibly inhibits the hydrolysis of acetylcholine by binding to the anionic site of acetylcholinesterase, thereby causing accumulation of acetylcholine. This results in increased cholinergic responses including increased tonus of skeletal and intestinal muscles, bronchial and ureteral constriction, miosis, bradycardia, and increased sweat and salivary secretions.
Onset: 30-60 seconds (IV); 2-10 min (IM).
Duration: 5-10 min (IV); 5-30 min (IM).
Pharmacokinetics:
Distribution: Volume of distribution: 0.9 ± 0.13 L/kg.
Excretion: Mainly via urine (67%). Elimination half-life: 126 ± 59 min.
Chemical Structure

Chemical Structure Image
Edrophonium chloride

Source: National Center for Biotechnology Information. PubChem Database. Edrophonium chloride, CID=8307, https://pubchem.ncbi.nlm.nih.gov/compound/Edrophonium-chloride (accessed on Jan. 21, 2020)

Storage
Store between 20-25°C.
References
Anon. Edrophonium. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/05/2017.

Buckingham R (ed). Edrophonium Chloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/05/2017.

Enlon Injection, Solution (Mylan Institutional LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/05/2017.

McEvoy GK, Snow EK, Miller J et al (eds). Edrophonium Chloride. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 04/05/2017.

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