No reaction
No reactionWARNINGMIXING OR WITHDRAWAL CAN BE DANGEROUS
Ordinary doses in combination with other depressants can fatally stop breathing. After prolonged dependency, stopping suddenly can also cause seizures or delirium; seek medical help.
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Estazolam
Estazolam is a triazolobenzodiazepine benzodiazepine1 indicated for the short-term management of insomnia.1 It is a benzodiazepine with anticonvulsant, hypnotic, and muscle-relaxant properties2, distinguished by a benzodiazepine structure fused with a triazole ring.3 It was patented in 1968 and entered medical use in 1975. Estazolam may be habit-forming.4
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Threshold~0.5 mg
Light0.5-1 mg
Moderate1-2 mg
Strong2-4 mg
Heavy4+ mg
Duration
Onset30-60 minutes
After Effects2-24 hours
Total7-12 hours
Subjective Effects
Subjective Effects not written up yet
Pharmacology
Pharmacodynamics
Estazolam is a positive allosteric modulator of GABA-A receptors at the benzodiazepine binding site, enhancing GABA-mediated chloride-channel opening and neuronal inhibition. This mechanism supports its anticonvulsant, hypnotic, muscle-relaxant, and anxiolytic effects. DrugBank also lists agonism at the translocator protein.
Pharmacokinetics
Estazolam is administered orally and is absorbed with tablets equivalently to an oral solution1. In healthy subjects receiving up to three times the recommended dose, peak plasma concentrations occurred 0.5 to 6 hours after dosing and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested1. It is extensively metabolized in the liver, with CYP3A mediating formation of the major circulating metabolite 4-hydroxy-estazolam1. Hydroxylated and other metabolites are eliminated mainly by the kidneys in urine, both free and conjugated; less than 5% of a dose is excreted unchanged in urine and about 4% appears in feces1. The reported mean elimination half-life ranges from 10 to 24 hours1.
Interactions
Interactions not written up yet
An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Tolerance to estazolam's hypnotic effects may develop within a few days in elderly patients, reducing the short-term sleep benefits. Long-term benzodiazepine use is associated with drug tolerance.5
Harm Potential
Addiction & Dependence
Psychological
HighEstazolam has demonstrated abuse potential in primate studies. As a benzodiazepine, it carries significant risk of psychological dependence, with recreational misuse occurring to achieve intoxication or continued use against medical advice being documented patterns of misuse.
Physical
HighPhysical dependence is a primary safety concern with estazolam. Long-term use is associated with drug dependence and a benzodiazepine withdrawal syndrome upon discontinuation. Tolerance to hypnotic effects develops within days, particularly in elderly users.
Toxicity
Acute CNS depression occurs during use, with symptoms including somnolence, dizziness, hypokinesia, abnormal coordination, and next-day hangover effects impairing mental and physical performance; overdose can progress to confusion, depressed breathing, and coma.
History & Culture
Development and medical introduction
Estazolam was patented in 1968 and entered medical use in 1975. It was developed as a triazolobenzodiazepine and later marketed for short-term treatment of insomnia.
Legality
By Country
Illegal1
United StatesIllegalEstazolam is listed by exact name in federal Schedule IV under the Controlled Substances Act, implemented at 21 C.F.R. § 1308.14(c)(21). The schedule covers any quantity of estazolam, including its salts, isomers, and salts of isomers where chemically possible, unless specifically excepted or listed in another schedule. Federal law controls possession, manufacture, distribution, dispensing, import, export, and possession with intent to manufacture, distribute, or dispense; simple possession pursuant to a valid prescription or order, and other authorized possession, is excepted. The classification took effect on November 5, 1984.
Controlled / restricted1
CanadaRestrictedEstazolam is expressly listed under benzodiazepines in Schedule IV, item 18(11), of the Controlled Drugs and Substances Act. Ordinary possession is not prohibited by subsection 4(1), which applies only to substances in Schedules I, II, and III. Schedule IV substances remain subject to prohibitions on trafficking, possession for trafficking, unauthorized import or export, possession for export, unauthorized production, and obtaining a substance from a practitioner without the disclosure required by subsection 4(2). The Act came into force on May 14, 1997.
References
Citations
Article Status
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