化合物信息

Drug Groups

approved

Description

A rapid-onset, short-acting cholinesterase inhibitor used in cardiac arrhythmias and in the diagnosis of myasthenia gravis. It has also been used as an antidote to curare principles. [PubChem]

Indication

For the differential diagnosis of myasthenia gravis and as an adjunct in the evaluation of treatment requirements in this disease. It may also be used for evaluating emergency treatment in myasthenic crises.

Pharmacology

Edrophonium is a short and rapid-acting anticholinesterase drug. Its effect is manifest within 30 to 60 seconds after injection and lasts an average of 10 minutes. Edrophonium's pharmacologic action is due primarily to the inhibition or inactivation of acetylcholinesterase at sites of cholinergic transmission. Nicotinic acetylcholine (nAChR)receptors are found throughout the body, especially on muscle. Stimulation of these receptors causes to muscle contraction. In myasthenia gravis the body's immune system destroys many of the nicotinic acetylcholine receptors, so that the muscle becomes less responsive to nervous stimulation. Edrophonium chloride increases the amount of acetylcholine at the nerve endings. Increased levels of acetylcholine allow the remaining receptors to function more efficiently.

Toxicity

With drugs of this type, muscarine-like symptoms (nausea, vomiting, diarrhea, sweating, increased bronchial and salivary secretions and bradycardia) often appear with overdosage (cholinergic crisis).

Affected Organisms

Absorption

Rapidly absorbed.

Half Life

Distribution half-life is 7 to 12 minutes. Elimination half-life is 33 to 110 minutes.

Elimination

Edrophonium is primarily renally excreted with 67% of the dose appearing in the urine.
Hepatic metabolism and biliary excretion have also been demonstrated in animals

Distribution

* 1.6±0.4 L/kg [Adults]
* 2.2±1.5 L/kg [Children (0.08-10 yrs)]
* 1.8±1.2 L/kg [Elderly (65-75 yrs)]

Clearance

* 6.8 +/- 2. mL/kg/min [Adults]
* 6.4 +/- 3.9 mL/kg/min [Children (0.08-10 yrs)]
* 2.9 +/- 1.9 mL/kg/min [Elderly (65-75 yrs)]

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