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QuickView for Estazolam (compound)
PubChem
| Name: | Estazolam |
|---|---|
| PubChem Compound ID: | 3261 |
| Description: | A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM. |
| Molecular formula: | C16H11ClN4 |
| Molecular weight: | 294.738 g/mol |
| Synonyms: |
Julodin; Abbott 47631; 8-Chloro-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine; Estazolam [USAN:INN:JAN]; U 33737; 8-Chloro-6-phenyl-4H-(1,2,4)triazolo-(4,3-a)(1,4)benzodiazepine; Esilgan; 8-Chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine (IUPAC); D00311; LS-7378.
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DrugBank
Identification
| Name: | Estazolam |
|---|---|
| Name (isomeric): | DB01215 |
| Drug Type: | small molecule |
| Description: | A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM. |
| Brand: | Eurodin, ProSom, Nuctalon, Nemurel, Julodin, Esilgan, Somnatrol, D 40TA, Cannoc |
| Category: | Anti-anxiety Agents, GABA Modulators, Anticonvulsants |
| CAS number: | 29975-16-4 |
Pharmacology
| Indication: | For the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings. |
|---|---|
| Pharmacology: | 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. |
| Mechanism of Action: |
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 (GABAA) receptors, this enhances the effects GABA by increasing GABA affinity for the GABA r...
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| Absorption: | 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. |
| Protein binding: | 93% protein bound, independant of concentration. |
| Biotransformation: | 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. |
| Toxicity: | Symptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech. |
| Affected organisms: | Humans and other mammals |
Interactions
| Food interaction: |
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Targets
Enzymes
