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| Trade names | Tensilon, Enlon |
| AHFS/Drugs.com | FDA Professional Drug Information |
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| Duration of action | 10–30 minutes |
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| Chemical and physical data | |
| Formula | C10H16NO+ |
| Molar mass | 166.244 g·mol−1 |
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Edrophonium, formerly sold under the brand nameTensilon among others, is a readily reversibleacetylcholinesterase inhibitor. It prevents breakdown of theneurotransmitteracetylcholine and acts by competitively inhibiting the enzymeacetylcholinesterase, mainly at theneuromuscular junction.
Edrophonium (by the so-calledTensilon test) is used to differentiatemyasthenia gravis fromcholinergic crisis andLambert-Eaton myasthenic syndrome. In myasthenia gravis, the body producesautoantibodies which block, inhibit or destroynicotinic acetylcholine receptors in the neuromuscular junction. Edrophonium—an effectiveacetylcholinesterase inhibitor— reduces the muscle weakness by blocking the enzymatic effect ofacetylcholinesterase enzymes, prolonging the presence ofacetylcholine in the synaptic cleft. It binds to a Serine-103 allosteric site, while pyridostigmine and neostigmine bind to the acetylcholinesterase active site for their inhibitory effects. In acholinergic crisis, where a person has too muchneuromuscular stimulation, edrophonium will make the muscle weakness worse by inducing adepolarizing block. However, the edrophonium and ice pack tests are no longer recommended as first-line tests due to false positive results. In practice, the edrophonium test has been replaced by testing for autoantibodies, including acetylcholine receptor autoantibodies and muscle specific tyrosine kinase autoantibodies.[1][2]
The Tensilon test may also be used to predict if neurotoxic paralysis caused by snake envenomation is presynaptic or postsynaptic. If it is postsynaptic, then paralysis will be temporally reversed, indicating that can be reversed by adequate antivenom therapy. If the neurotoxicity is presynaptic, then the Tensilon test will show no response and antivenom will not reverse such paralysis. In this instance reversal of paralysis will not occur until the damaged terminal axons at the neuromuscular junction have recovered, this may take days or weeks.[3]
The drug may also be used for reversal ofneuromuscular blockade at the end of a surgical procedure.[4]
Edrophonium, ethyl-(3-hydroxyphenyl)dimethylammonium chloride, is made by reacting 3-dimethylaminophenol withethyl bromide, which forms ethyl(3-hydroxyphenyl)dimethylammonium bromide, the bromine atom of which is replaced with a chlorine atom by reacting it withsilver chloride, giving edrophonium.[5]
The drug has a brief duration of action, about 10–30 mins.[4]
