Etizolam

Etizolam

File:Etizolam.svg
File:Etizolam3d.png
Systematic (IUPAC) name
7-(2-chlorophenyl)- 4-ethyl- 13-methyl- 3-thia- 1,8,11,12- tetraazatricyclo [8.3.0.02,6}] trideca- 2(6),4,7,10,12- pentaene
Clinical data
Pregnancy category	?
Routes of administration	Oral
Legal status
Legal status	US: Unscheduled
Pharmacokinetic data
Bioavailability	93%
Metabolism	Hepatic
Biological half-life	about 6 hours
Excretion	Renal
Identifiers
CAS Number	40054-69-1
ATC code	N05BA19 (WHO)
PubChem	CID 3307
DrugBank	?
Chemical data
Formula	C17H15ClN4S
Molar mass	342.8[[]]

Etizolam (marketed under the brand name Etilaam, Sedekopan, Pasaden or Depas) is a thienodiazepine drug which is a benzodiazepine analog. The etizolam molecule differs from most other benzodiazepines in that the benzene ring has been replaced by a thiophene ring. It possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties.

Indications

• Short-term treatment of insomnia
• Short-term treatment of anxiety or panic attacks, if a benzodiazepine is required

Dosage

• For anxiety: 0,25-0,50 mg two or three times per day (maximum 2 mg per day)
• For insomnia: 1 or 2 mg before bedtime

Side effects

• Blepharospasms with long term use

Very Rare

• Erythema annulare centrifugum skin lesions

Tolerance, dependence and withdrawal

Abrupt or over rapid withdrawal from etizolam as with other benzodiazepines may result in the appearance of the benzodiazepine withdrawal syndrome, including rebound insomnia. A neuroleptic malignant syndrome, a rare event in benzodiazepine withdrawal has been documented in a case of abrupt withdrawal from etizolam.

Contraindications and special caution

Benzodiazepines require special precaution if used in the elderly, during pregnancy, in children, alcohol or drug-dependent individuals and individuals with comorbid psychiatric disorders.

Pharmacology

Etizolam a thienodiazepine benzodiazepine derivative, is absorbed fairly rapidly with peak plasma levels achieved between 30 minutes and 2 hours and has a mean elimination half life of about 3 and a half hours. However, its pharmacologically active metabolite alpha-hydroxyetizolam which has the same potency as etizolam is eliminated more slowly with a mean half life of just over 8 hours. So it can be classified as a short-medium action benzodiazepine. Etizolam possesses potent hypnotic properties. Etizolam acts as a full agonist at the benzodiazepine receptor to produce its range of therapeutic as well as adverse effects. Similar to other benzodiazepines etizolam binds unselectively to benzodiazepine receptor subtypes.

In addition etizolam unlike most other benzodiazepines has prolactogenic effects leading to an increase in prolactin blood levels.

According to the Italian P.I. sheet etizolam belongs to a new class of diazepines, thienotriazolodiazepines. This new class is easily oxidized, rapidly metabolized, and has a lower risk of accumulation, even after prolonged treatment. Etizolam has an anxiolytic action about 6 times greater than that of diazepam. Etizolam produces, especially at higher dosages, a reduction in time taken to fall asleep, an increase in total sleep time and a reduction in the number of awakenings. During tests there were not substantial changes in deep sleep. There is a reduction of REM sleep. In EEG tests of healthy volunteers Etizolam showed some characteristics of tricyclic antidepressants.

Interactions

Itraconazole and fluvoxamine slow down the rate of elimination of etizolam leading to accumulation of etizolam and thus increased pharmacological effects. Carbamazepine speeds up the metabolism of etizolam resulting in reduced pharmacological effects of etizolam.

Overdose

See also: Benzodiazepine overdose

Etizolam has been used in cases of suicidal benzodiazepine overdose. An overdose of etizolam can prove fatal.

Abuse

See also: Benzodiazepine drug misuse

Etizolam is a drug of potential abuse. Etizolam has been shown to be able to substitute for the behavioural effects of barbiturates in primate studies.

See also

• Brotizolam
• Clotiazepam
• Benzodiazepine
• Benzodiazepine dependence
• Benzodiazepine withdrawal syndrome
• Long term effects of benzodiazepines

External links

• Inchem.org - Etizolam

ja:エチゾラム