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Estazolam

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Collated from TripSit, Pharmacology, DrugCentral. Where sources differ (e.g. dosing), Compare shows them side by side.

Sections
BenzodiazepineHabit-formingDepressantTS

Also known as prosom, eurodin, elprazolamTS

A rarely prescribed medium-duration prescription benzodiazepine. Mainly used as a hypnotic, it can cause amnesia and lowered inhibitions in excess.TS

Oral

Route dataTripSit

Dose
WeakerStronger
ThresholdLightCommonStrongHeavy
—0.5–1 mg1–2 mg2–4 mg—+
04 mg
LightCommonStrongHeavy
Duration
ShorterLonger
Onset30–60 minutes
Total7–12 hours
After-effects2–24 hours
OnsetCome-upPeakOffset

🧬 Receptor activityDC

TargetActionAffinitySource
GABA-A receptor alpha-1/beta-2/gamma-2 (GABRA1)Positive allosteric modulator—DRUGCENTRAL
GABA-A receptor alpha-2/beta-3/gamma-2 (GABRG2)Positive allosteric modulator—DRUGCENTRAL
GABA-A receptor alpha-3/beta-3/gamma-2 (GABRG2)Positive allosteric modulator—DRUGCENTRAL
GABA-A receptor alpha-5/beta-3/gamma-2 (GABRG2)Positive allosteric modulator—DRUGCENTRAL
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Mechanism of actionPH

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABA<sub>A</sub>) receptors, this enhances the effects GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.

PharmacodynamicsPH

Estazolam, a triazolobenzodiazepine derivative, is an oral hypnotic agent with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.

Pharmacokinetics

Half-lifePH

The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.

AbsorptionPH

Tablets have been found to be equivalent in absorption to an orally administered solution of estazolam. In healthy subjects who received up to three times the recommended dose, peak estazolam plasma concentrations occurred within two hours after dosing (range 0.5 to 6.0 hours) and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested.
Estazolam is extensively metabolized. The elimination of the parent drug takes place via hepatic metabolism of estazolam to hydroxylated and other metabolites that are eliminated largely in the urine both free and conjugated. Less than 5% of a 2 mg dose of estazolam was excreted unchanged in the urine, with only 4% of the dose appearing in the feces. Radiolabel mass balance studies indicate that the main route of excretion is via the kidneys. After 5 days, 87% of the administered radioactivity was excreted in human urine. Less than 4% of the dose was excreted unchanged.

MetabolismPH

Extensively metabolized in the liver. In vitro studies with human liver microsomes indicate that the biotransformation of estazolam to the major circulating metabolite 4-hydroxy-estazolam is mediated by cytochrome P450 3A (CYP3A).
Estazolam has known human metabolites that include 4-hydroxyestazolam.
Extensively metabolized in the liver. In vitro studies with human liver microsomes indicate that the biotransformation of estazolam to the major circulating metabolite 4-hydroxy-estazolam is mediated by cytochrome P450 3A (CYP3A).
Route of Elimination: Estazolam is extensively metabolized. The elimination of the parent drug takes place via hepatic metabolism of estazolam to hydroxylated and other metabolites that are eliminated largely in the urine both free and conjugated. Less than 5% of a 2 mg dose of estazolam was excreted unchanged in the urine, with only 4% of the dose appearing in the feces. Radiolabel mass balance studies indicate that the main route of excretion is via the kidneys. After 5 days, 87% of the administered radioactivity was excreted in human urine. Less than 4% of the dose was excreted unchanged.
Half Life: The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.

Protein bindingPH

93% protein bound, independant of concentration.

Plan when to take Estazolam — see where onset, peak and comedown land on the clock

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.