Estazolam

(USAN, rINN)
Estazolam Chemical formula
Synonyms: Abbott-47631; D-40TA; Estatsolaami; Estazolamum. 8-Chloro6-phenyl-4H-1,2,4-triazolo[4,3a]-1,4-benzodiazepine.
Cyrillic synonym: Эстазолам.

💊 Chemical information

Chemical formula: C16H11ClN4 = 294.7.
CAS — 29975-16-4.
ATC — N05CD04.
ATC Vet — QN05CD04.

Pharmacopoeias.

In Chin. and Jpn.

💊 Dependence and Withdrawal

As for Diazepam.

💊 Adverse Effects, Treatment, and Precautions

As for Diazepam.

💊 Interactions

As for Diazepam.

💊 Pharmacokinetics

Peak plasma concentrations of estazolam are reached on average within 2 hours of oral doses. Estazolam is about 93% protein bound. Reported mean elimination half-lives have generally been in the range of 10 to 24 hours. Estazolam is extensively metabolised, mainly to 4-hydroxyestazolam and 1-oxoestazolam, which are considered inactive. These metabolites are excreted, either free or conjugated, in the urine with small amounts detected in the faeces. Only a small proportion of a dose is excreted as unchanged drug.

💊 Uses and Administration

Estazolam is a short-acting benzodiazepine with general properties similar to those of diazepam. It is given as a hypnotic in the short-term management of insomnia in usual oral doses of 1 to 2 mg at night. Small or debilitated elderly patients may be given an initial dose of 0.5 mg.

💊 Preparations

Proprietary Preparations

Arg.: Somnatrol†; Braz.: Noctal; Denm.: Domnamid†; Fr.: Nuctalon; Indon.: Esilgan; Ital.: Esilgan; Jpn: Eurodin; Mex.: Tasedan; Philipp.: Esilgan; Port.: Kainever; USA: Prosom†.
Published December 26, 2018.