indication

Used for short-term hypnotic therapy in the management of insomnia for periods of up to one week in duration; however, this medication generally has been replaced by other sedative-hypnotic agents.

pharmacology

Ethchlorvynol is a sedative drug and schedule IV (USA) controlled substance. It produces cerebral depression, however the exact mechanism of action is not known.

mechanism of action

Although the exact mechanism of action is unknown, ethchlorvynol appears to depress the central nervous system in a manner similar to that of barbiturates. Barbiturates bind at a distinct binding sites associated with a Cl^- ionopore at the GABA_A receptor, increasing the duration of time for which the Cl^- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.

toxicity

Symptoms of overdose include thrombocytopenia.

biotransformation

About 90% of a dose is metabolized in the liver. Some ethchlorvynol may also be metabolized in the kidneys. Ethchlorvynol and metabolites undergo extensive enterohepatic recirculation.

absorption

Rapidly absorbed from gastrointestinal tract.

half life

Plasma half-life is approximately 10 to 20 hours, terminal half-life is 21-100 hours.

drug interactions

Acenocoumarol: Ethchlorvynol may decrease the anticoagulant effect of acenocoumarol.

Anisindione: Ethchlorvynol may decrease the anticoagulant effect of anisindione.

Dicumarol: Ethchlorvynol may decrease the anticoagulant effect of dicumarol.

Warfarin: Ethchlorvynol may decrease the anticoagulant effect of warfarin.