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Edrophonium
 
 
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Edrophonium is a readily reversible acetylcholinesterase inhibitor
Acetylcholinesterase inhibitor

An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical compound that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine....
. It prevents breakdown of the neurotransmitter
Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
 acetylcholine
Acetylcholine

The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including homo sapiens....
 and acts by competitively inhibiting the enzyme acetylcholinesterase
Acetylcholinesterase

Acetylcholinesterase, also known as AChE, is an enzyme that degrades the neurotransmitter acetylcholine, producing choline and an acetate group....
, mainly at the neuromuscular junction
Neuromuscular junction

A neuromuscular junction is the synapse or junction of the axon terminal of a motoneuron with the motor end plate, the highly-excitable region of muscle plasma membrane responsible for initiation of action potentials across the muscle's surface, ultimately causing the muscle to contract....
. It is sold under the trade names Tensilon, Enlon and Reversol.

use its duration of action is only about 20 minutes, edrophonium (by the so-called Tensilon test) is used to differentiate myasthenic crisis from cholinergic crisis
Cholinergic crisis

A cholinergic crisis is an over-stimulation at a neuromuscular junction due to an excess of acetylcholine , as of a result of the inactivity of the AChE enzyme, which normally breaks down acetylcholine....
.






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Edrophonium is a readily reversible acetylcholinesterase inhibitor
Acetylcholinesterase inhibitor

An acetylcholinesterase inhibitor or anti-cholinesterase is a chemical compound that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine....
. It prevents breakdown of the neurotransmitter
Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
 acetylcholine
Acetylcholine

The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including homo sapiens....
 and acts by competitively inhibiting the enzyme acetylcholinesterase
Acetylcholinesterase

Acetylcholinesterase, also known as AChE, is an enzyme that degrades the neurotransmitter acetylcholine, producing choline and an acetate group....
, mainly at the neuromuscular junction
Neuromuscular junction

A neuromuscular junction is the synapse or junction of the axon terminal of a motoneuron with the motor end plate, the highly-excitable region of muscle plasma membrane responsible for initiation of action potentials across the muscle's surface, ultimately causing the muscle to contract....
. It is sold under the trade names Tensilon, Enlon and Reversol.

Clinical uses

Because its duration of action is only about 20 minutes, edrophonium (by the so-called Tensilon test) is used to differentiate myasthenic crisis from cholinergic crisis
Cholinergic crisis

A cholinergic crisis is an over-stimulation at a neuromuscular junction due to an excess of acetylcholine , as of a result of the inactivity of the AChE enzyme, which normally breaks down acetylcholine....
. In myasthenic crisis, where a person is not able to produce enough neuromuscular
Nicotinic acetylcholine receptor

Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons....
 stimulation, edrophonium will reduce the muscle weakness by effectively supplying more acetylcholine
Acetylcholine

The chemical compound acetylcholine is a neurotransmitter in both the peripheral nervous system and central nervous system in many organisms including homo sapiens....
. In a cholinergic crisis, where a person has too much neuromuscular
Nicotinic acetylcholine receptor

Nicotinic acetylcholine receptors, or nAChRs, are cholinergic receptors that form ligand-gated ion channels in the plasma membranes of certain neurons....
 stimulation, edrophonium will make the muscle weakness worse by inducing a depolarizing block
Neuromuscular-blocking drugs

Neuromuscular-blocking drugs block neuromuscular transmission at the neuromuscular junction, causing paralysis of the affected skeletal muscles....
.

Sources

  1. Brenner, G. M. (2000). Pharmacology. Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6
  2. Canadian Pharmacists Association (2000). Compendium of Pharmaceuticals and Specialties (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4