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Information about Edrophonium

Edrophonium is a readily reversible acetylcholinesterase inhibitor. It prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction. It is sold under the trade names Tensilon, Enlon and Reversol.

Clinical uses

Because its duration of action is only about 10 minutes, edrophonium (by the so-called Tensilon test) is used to differentiate myasthenic crisis from cholinergic crisis. In myasthenic crisis, where a person is not able to produce enough neuromuscular stimulation, edrophonium will reduce the muscle weakness by effectively supplying more acetylcholine. In a cholinergic crisis, where a person has too much neuromuscular stimulation, edrophonium will make the muscle weakness worse by inducing a depolarizing block.

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


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Anticholinesterases''' (N06DA, N07AA)
CarbamatesAmbenonium - Demecarium - Stigmine (Neostigmine, Physostigmine, Pyridostigmine, Rivastigmine)
OtherGalantamine - Metrifonate - Donepezil - Tacrine - Edrophonium
Identifiers
Symbol BCHE
Alt. Symbols CHE1

Entrez 590
HUGO 983
OMIM 177400

RefSeq NM_000055
UniProt P06276
Other data
EC number 3.1.1.8
Locus Chr. 3 q26.1-26.
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Neurotransmitters are chemicals that are used to relay, amplify and modulate signals between a neuron and another cell. According to the prevailing beliefs of the 1960s, a chemical can be classified as a neurotransmitter if it meets the following conditions:

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The chemical compound acetylcholine, often abbreviated as ACh, was the first neurotransmitter to be identified. It is a chemical transmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.
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Identifiers
Symbol BCHE
Alt. Symbols CHE1

Entrez 590
HUGO 983
OMIM 177400

RefSeq NM_000055
UniProt P06276
Other data
EC number 3.1.1.8
Locus Chr. 3 q26.1-26.
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neuromuscular junction (NMJ) is the synapse or junction of the axon terminal of a motoneuron with the motor end plate, the highly-excitable region of muscle fiber plasma membrane responsible for initiation of action potentials across the muscle's surface, ultimately
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Edrophonium is a readily reversible acetylcholinesterase inhibitor. It prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
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Myasthenia gravis
Classification & external resources

Global view of a neuromuscular junction:
1. Axon
2. Motor end-plate
3. Muscle fiber
4. Myofibril
ICD-10 G 70.0
ICD-9 358.
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A cholinergic crisis is an over-stimulation at a neuromuscular junction due to an excess of acetylcholine (ACh), as of a result of the inactivity (perhaps even inhibition) of the AChE enzyme, which normally breaks down acetylcholine. This is a consequence of some types of nerve gas.
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Nicotinic acetylcholine receptors, or nAChRs, are ionotropic receptors that form ligand gated ion channels in cells' plasma membranes. Like the other type of acetylcholine receptors, muscarinic acetylcholine receptors (mAChRs), their opening is triggered by the
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The chemical compound acetylcholine, often abbreviated as ACh, was the first neurotransmitter to be identified. It is a chemical transmitter in both the peripheral nervous system (PNS) and central nervous system (CNS) in many organisms including humans.
..... Click the link for more information.
Nicotinic acetylcholine receptors, or nAChRs, are ionotropic receptors that form ligand gated ion channels in cells' plasma membranes. Like the other type of acetylcholine receptors, muscarinic acetylcholine receptors (mAChRs), their opening is triggered by the
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acetylcholinesterase inhibitor or anti-cholinesterase is a chemical that inhibits the cholinesterase enzyme from breaking down acetylcholine, so increasing both the level and duration of action of the neurotransmitter acetylcholine.
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Carbamates or urethanes are a group of organic compounds sharing a common functional group with the general structure -NH(CO)O-. Carbamates are esters of carbamic acid, NH2COOH, an unstable compound.
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Ambenonium (as ambenonium dichloride, trade name Mytelase) is a cholinesterase inhibitor used in the management of myasthenia gravis.


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Stigmine refers to a class of acetylcholinesterase inhibitor.

Examples include:
  • Distigmine
  • Neostigmine
  • Physostigmine
  • Pyridostigmine
  • Rivastigmine


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Neostigmine is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor. By interfering with the breakdown of acetylcholine, neostigmine indirectly stimulates both nicotinic and muscarinic receptors. It does cross the blood-brain barrier albeit poorly.
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Physostigmine (also known as eserine) is a parasympathomimetic, specifically, a reversible cholinesterase inhibitor obtained from the Calabar bean. By interfering with the metabolism of acetylcholine, physostigmine indirectly stimulates both nicotinic and muscarinic
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Pyridostigmine is a parasympathomimetic and a reversible cholinesterase inhibitor. Since it is a quaternary amine, it is poorly absorbed in the gut and doesn't cross the blood-brain barrier, except in stressful conditions[2].
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Rivastigmine (sold under the trade name Exelon) is a parasympathomimetic or cholinergic agent that was developed by Novartis for the treatment of mild to moderate dementia of the Alzheimer’s type.
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Galantamine (trade names Razadyne, Razadyne ER, Reminyl, Nivalin) is a drug developed by Janssen Pharmaceutica, and used for the treatment of mild to moderate Alzheimer’s disease.
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Trichlorfon is an organophosphate acetylcholinesterase inhibitor.


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Donepezil, marketed under the trade name Aricept (Eisai), is a centrally acting reversible acetyl cholinesterase inhibitor. Its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.
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Tacrine is a parasympathomimetic and a centrally acting cholinesterase inhibitor (anticholinesterase). It was the first centrally-acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex.
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