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Edrophonium !

A very short-acting cholinesterase inhibitor once used as a bedside test for myasthenia gravis. Antibody tests have largely replaced it.

Updated 2026-11-01

The figure shows edrophonium in the active site of Torpedo (electric ray) acetylcholinesterase, an enzyme with the same gorge and catalytic serine as the human one.

Target in 3D: Acetylcholinesterase. PDB structure 1AX9 (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Edrophonium binds the choline site of acetylcholinesterase reversibly, without forming a covalent bond, and blocks acetylcholine from entering. Its effect lasts only minutes because it is quickly removed by the kidney. In myasthenia gravis, an injection briefly improves strength, which was the basis of the old «edrophonium test».

  1. Binds the choline site of acetylcholinesterase reversibly
  2. Acetylcholine is broken down more slowly
  3. Strength improves briefly in myasthenia gravis
  4. The kidney clears it quickly

Pharmacokinetics

Distribution
Quaternary: acts only in the peripheral nervous system
Elimination
Rapid renal elimination, hence its short action
Onset and duration
Rapid after intravenous injection; lasts only minutes

Indications

  • Diagnostic test for myasthenia gravis (historical; antibody tests are now preferred) Myasthenia gravis →
  • Reversal of non-depolarizing neuromuscular block, like neostigmine

Adverse effects

Common

  • Salivation, sweating and tearing
  • Nausea and abdominal cramps
  • Fasciculations

Contraindications

  • Mechanical obstruction of the bowel or urinary tract (class)
  • Caution in asthma and heart rhythm disorders (class)

Key interactions

Atropine
Kept ready to treat bradycardia during the test
Succinylcholine
Prolonged block (class effect)

What is monitored

  • Heart rate and ECG during the test
  • Strength of a defined muscle (for example eyelid drooping) before and after

Administration and safety

  • Given intravenously in a monitored setting with atropine and airway equipment at hand

Nursing care

  • Attach a cardiac monitor before the injection
  • Watch for slow heart rate and wheeze
  • Record the muscle response the team is testing

Test yourself

Think of the answer, then tap the question to see it.

Why does edrophonium act for only a few minutes?

It binds acetylcholinesterase reversibly without a covalent bond and is quickly eliminated by the kidney.

What was a positive edrophonium test in myasthenia gravis?

A brief, clear improvement in muscle strength after the injection.

What has largely replaced the edrophonium test?

Blood tests for antibodies against the acetylcholine receptor, plus electrodiagnostic studies.

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← Back to the class: Cholinesterase inhibitors

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 12 (McGraw Hill, 2023); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); RCSB PDB - 1AX9: ACETYLCHOLINESTERASE COMPLEXED WITH EDROPHONIUM, LAUE DATA (RCSB Protein Data Bank, 2026).

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Representative model, for educational purposes only.