Peringatan Keamanan

Symptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech.

Estazolam

DB01215

small molecule approved illicit

Deskripsi

A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.

Struktur Molekul 2D

Berat 294.738
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

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.

Metabolisme

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).

Rute Eliminasi

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.

Interaksi Makanan

2 Data
  • 1. Avoid alcohol.
  • 2. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1526 Data
Buprenorphine Estazolam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Hydrocodone Estazolam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Magnesium sulfate The therapeutic efficacy of Estazolam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Estazolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Estazolam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Mirtazapine Estazolam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Orphenadrine Estazolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Estazolam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Pramipexole Estazolam may increase the sedative activities of Pramipexole.
Ropinirole Estazolam may increase the sedative activities of Ropinirole.
Rotigotine Estazolam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Estazolam.
Suvorexant Estazolam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Thalidomide Estazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Estazolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Estazolam is combined with Clozapine.
Methadone Estazolam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Sodium oxybate Estazolam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Estazolam can be increased when it is combined with Teduglutide.
Yohimbine The therapeutic efficacy of Estazolam can be increased when used in combination with Yohimbine.
Erythromycin The serum concentration of Estazolam can be increased when it is combined with Erythromycin.
Sirolimus The serum concentration of Estazolam can be increased when it is combined with Sirolimus.
Dirithromycin The serum concentration of Estazolam can be increased when it is combined with Dirithromycin.
Telithromycin The serum concentration of Estazolam can be increased when it is combined with Telithromycin.
Candicidin The serum concentration of Estazolam can be increased when it is combined with Candicidin.
Clarithromycin The serum concentration of Estazolam can be increased when it is combined with Clarithromycin.
Josamycin The serum concentration of Estazolam can be increased when it is combined with Josamycin.
Everolimus The serum concentration of Estazolam can be increased when it is combined with Everolimus.
Epothilone D The serum concentration of Estazolam can be increased when it is combined with Epothilone D.
Patupilone The serum concentration of Estazolam can be increased when it is combined with Patupilone.
6-Deoxyerythronolide B The serum concentration of Estazolam can be increased when it is combined with 6-Deoxyerythronolide B.
Ixabepilone The serum concentration of Estazolam can be increased when it is combined with Ixabepilone.
KOS-1584 The serum concentration of Estazolam can be increased when it is combined with KOS-1584.
Ridaforolimus The serum concentration of Estazolam can be increased when it is combined with Ridaforolimus.
Temsirolimus The serum concentration of Estazolam can be increased when it is combined with Temsirolimus.
AVE9633 The serum concentration of Estazolam can be increased when it is combined with AVE9633.
Coltuximab ravtansine The serum concentration of Estazolam can be increased when it is combined with Coltuximab ravtansine.
Cethromycin The serum concentration of Estazolam can be increased when it is combined with Cethromycin.
Mitemcinal The serum concentration of Estazolam can be increased when it is combined with Mitemcinal.
Brefeldin A The serum concentration of Estazolam can be increased when it is combined with Brefeldin A.
Solithromycin The serum concentration of Estazolam can be increased when it is combined with Solithromycin.
Kitasamycin The serum concentration of Estazolam can be increased when it is combined with Kitasamycin.
Carbomycin The serum concentration of Estazolam can be increased when it is combined with Carbomycin.
Doramectin The serum concentration of Estazolam can be increased when it is combined with Doramectin.
Eprinomectin The serum concentration of Estazolam can be increased when it is combined with Eprinomectin.
Oleandomycin The serum concentration of Estazolam can be increased when it is combined with Oleandomycin.
Selamectin The serum concentration of Estazolam can be increased when it is combined with Selamectin.
Tildipirosin The serum concentration of Estazolam can be increased when it is combined with Tildipirosin.
Tilmicosin The serum concentration of Estazolam can be increased when it is combined with Tilmicosin.
Tylosin The serum concentration of Estazolam can be increased when it is combined with Tylosin.
Tylvalosin The serum concentration of Estazolam can be increased when it is combined with Tylvalosin.
Bryostatin 1 The serum concentration of Estazolam can be increased when it is combined with Bryostatin 1.
Lorvotuzumab mertansine The serum concentration of Estazolam can be increased when it is combined with Lorvotuzumab mertansine.
Epofolate The serum concentration of Estazolam can be increased when it is combined with Epofolate.
Sagopilone The serum concentration of Estazolam can be increased when it is combined with Sagopilone.
Troleandomycin The serum concentration of Estazolam can be increased when it is combined with Troleandomycin.
Miocamycin The serum concentration of Estazolam can be increased when it is combined with Miocamycin.
Flurithromycin The serum concentration of Estazolam can be increased when it is combined with Flurithromycin.
Rokitamycin The serum concentration of Estazolam can be increased when it is combined with Rokitamycin.
Midecamycin The serum concentration of Estazolam can be increased when it is combined with Midecamycin.
Clindamycin The serum concentration of Estazolam can be increased when it is combined with Clindamycin.
Mepartricin The serum concentration of Estazolam can be increased when it is combined with Mepartricin.
Mefloquine The therapeutic efficacy of Estazolam can be decreased when used in combination with Mefloquine.
Mianserin The therapeutic efficacy of Estazolam can be decreased when used in combination with Mianserin.
Orlistat Orlistat can cause a decrease in the absorption of Estazolam resulting in a reduced serum concentration and potentially a decrease in efficacy.
Topotecan Estazolam may increase the excretion rate of Topotecan which could result in a lower serum level and potentially a reduction in efficacy.
Flumazenil Flumazenil may decrease the sedative activities of Estazolam.
Tetracosactide The risk or severity of liver damage can be increased when Tetracosactide is combined with Estazolam.
Ethanol Estazolam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Estazolam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Estazolam.
Zimelidine The risk or severity of adverse effects can be increased when Estazolam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Estazolam is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Estazolam is combined with Seproxetine.
Fluvoxamine The risk or severity of adverse effects can be increased when Estazolam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Estazolam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Estazolam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Estazolam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Estazolam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Estazolam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Estazolam is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Estazolam is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Estazolam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Estazolam is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Estazolam is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Estazolam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Estazolam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Estazolam is combined with Alaproclate.
Benzatropine Benzatropine may decrease the excretion rate of Estazolam which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Estazolam which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Estazolam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Estazolam.

Target Protein

GABA(A) Receptor GABRA1
Translocator protein TSPO
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Synthesis reference: Hester, J.B. Jr.; U.S. Patent 3,701,782; October 31, 1972; assigned to The Upjohn Co.
Artikel (PubMed)

Contoh Produk & Brand

Produk: 23 • International brands: 3
Produk
  • Estazolam
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 2 mg/1 • Oral • US • Generic • Approved
  • Estazolam
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 23 produk.
International Brands
  • Esilgan — Takeda
  • Eurodin — Takeda
  • Nuctalon — Takeda

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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