Peringatan Keamanan

Major adverse effects include drowsiness, sedation, muscle weakness and incoordination, fainting, headache, confusion, depression, slurred speech, visual disturbances and changes in libido and tremor L883. Flumazenil is a competitive antagonist of GABA-A receptors and can be also used to reverse the effect of etizolam overdosage. Etizolam demonstrates no effects on fertility, development and teratogenicity L884. LD50 values of etizolam when delivered orally, intraperitoneally, and subcutaneously are 3509mg/kg, 825mg/kg, and >5000mg/kg in rats, respectively, and 3070mg/kg, 783mg/kg and 5000mg/kg in mice, respectively MSDS.

Etizolam

DB09166

small molecule experimental

Deskripsi

Etizolam is a thienodiazepine which is chemically related to benzodiazepine (BDZ) drug class; it differs from BDZs in having a benzene ring replaced with a thiophene ring. It is an agonist at GABA-A receptors and possesses amnesic, anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant properties. Initially introduced in 1983 in Japan as treatment for neurological conditions such as anxiety and sleep disorders, etizolam is marketed in Japan, Italy and India. It is not approved for use by FDA in the US; however it remains unscheduled in several states and is legal for research purposes.

Struktur Molekul 2D

Berat 342.846
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average elimination half life of etizolam following a single oral dose of 0.5mg is 3.4 hours but may be increased up to 17 hours depending on the rate of metabolism [L884]. The main metabolite ?-hydroxyetizolam displays a longer elimination half life of 8.2 hours [A19776].
Volume Distribusi Apparent distribution volume was 0.9 ± 0.2 L/kg following a single oral doing of 0.5mg etizolam [L884].
Klirens (Clearance) -

Absorpsi

Etizolam is well absorbed from the intestines with a biological bioavailability of 93% following oral administration. After a single oral dosing of 0.5mg etizolam, it takes approximately 0.9 hours to reach the peak plasma concentration of 8.3 ng/mL L884.

Metabolisme

Biotransformation of etizolam is extensive and involves hydroxylation and conjugation L884. The main metabolite formed via 1'-hydroxylation is ?-hydroxyetizolam which retains pharmacological activity comparable to that of the parent drug, indicating that the action of metabolites may contribute to the clinical effects of etizolam A19776. CYP3A4 is predicted to be the main CYP enzyme responsible for mediating etizolam metabolism. CYP2C18 and CYP2C19 are also involved in the metabolic pathways L884, A19775.

Rute Eliminasi

In a rat study, the amounts of etizolam excreted was 30% in urine was 70% in feces, while the values in a mouse study were 40% in urine and 60% in feces L884.

Interaksi Obat

912 Data
Buprenorphine Etizolam 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 Etizolam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Etizolam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Etizolam.
Hydrocodone Etizolam 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 Etizolam.
Magnesium sulfate The therapeutic efficacy of Etizolam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Etizolam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Etizolam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Etizolam.
Mirtazapine Etizolam 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 Etizolam.
Orphenadrine Etizolam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Etizolam 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 Etizolam.
Pramipexole Etizolam may increase the sedative activities of Pramipexole.
Ropinirole Etizolam may increase the sedative activities of Ropinirole.
Rotigotine Etizolam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Etizolam.
Suvorexant Etizolam 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 Etizolam.
Thalidomide Etizolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Etizolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Etizolam is combined with Clozapine.
Methadone Etizolam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Sodium oxybate Etizolam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Etizolam can be increased when it is combined with Teduglutide.
Yohimbine The therapeutic efficacy of Etizolam can be increased when used in combination with Yohimbine.
Dabrafenib The serum concentration of Etizolam can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Etizolam can be increased when it is combined with Luliconazole.
Flumazenil Flumazenil may decrease the sedative activities of Etizolam.
Ethanol Etizolam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Etizolam 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 Etizolam.
Zimelidine The risk or severity of adverse effects can be increased when Etizolam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Etizolam is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Etizolam is combined with Seproxetine.
Citalopram The risk or severity of adverse effects can be increased when Etizolam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Etizolam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Etizolam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Etizolam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Etizolam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Etizolam is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Etizolam is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Etizolam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Etizolam is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Etizolam.
Indalpine The risk or severity of adverse effects can be increased when Etizolam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Etizolam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Etizolam is combined with Alaproclate.
Lumacaftor The serum concentration of Etizolam can be decreased when it is combined with Lumacaftor.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Etizolam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Etizolam.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Etizolam.
Zopiclone The risk or severity of adverse effects can be increased when Etizolam is combined with Zopiclone.
Caffeine The therapeutic efficacy of Etizolam can be decreased when used in combination with Caffeine.
Dyphylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Dyphylline.
Pentoxifylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Pentoxifylline.
Mercaptopurine The therapeutic efficacy of Etizolam can be decreased when used in combination with Mercaptopurine.
Oxtriphylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Oxtriphylline.
Theobromine The therapeutic efficacy of Etizolam can be decreased when used in combination with Theobromine.
Fenethylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Fenethylline.
8-azaguanine The therapeutic efficacy of Etizolam can be decreased when used in combination with 8-azaguanine.
7,9-Dimethylguanine The therapeutic efficacy of Etizolam can be decreased when used in combination with 7,9-Dimethylguanine.
Xanthine The therapeutic efficacy of Etizolam can be decreased when used in combination with Xanthine.
7-Deazaguanine The therapeutic efficacy of Etizolam can be decreased when used in combination with 7-Deazaguanine.
Guanine The therapeutic efficacy of Etizolam can be decreased when used in combination with Guanine.
9-Methylguanine The therapeutic efficacy of Etizolam can be decreased when used in combination with 9-Methylguanine.
Peldesine The therapeutic efficacy of Etizolam can be decreased when used in combination with Peldesine.
Hypoxanthine The therapeutic efficacy of Etizolam can be decreased when used in combination with Hypoxanthine.
9-Deazaguanine The therapeutic efficacy of Etizolam can be decreased when used in combination with 9-Deazaguanine.
Propentofylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Propentofylline.
Valomaciclovir The therapeutic efficacy of Etizolam can be decreased when used in combination with Valomaciclovir.
3-isobutyl-1-methyl-7H-xanthine The therapeutic efficacy of Etizolam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
Uric acid The therapeutic efficacy of Etizolam can be decreased when used in combination with Uric acid.
Doxofylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Doxofylline.
6-O-benzylguanine The therapeutic efficacy of Etizolam can be decreased when used in combination with 6-O-benzylguanine.
Lisofylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Lisofylline.
Lobucavir The therapeutic efficacy of Etizolam can be decreased when used in combination with Lobucavir.
Cafedrine The therapeutic efficacy of Etizolam can be decreased when used in combination with Cafedrine.
Theodrenaline The therapeutic efficacy of Etizolam can be decreased when used in combination with Theodrenaline.
Bamifylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Bamifylline.
Proxyphylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Proxyphylline.
Acefylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Acefylline.
Etamiphylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Etamiphylline.
Pentifylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Pentifylline.
Bufylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Bufylline.
Bromotheophylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Bromotheophylline.
Furafylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Furafylline.
8-chlorotheophylline The therapeutic efficacy of Etizolam can be decreased when used in combination with 8-chlorotheophylline.
PCS-499 The therapeutic efficacy of Etizolam can be decreased when used in combination with PCS-499.
Theophylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Theophylline.
Aminophylline The therapeutic efficacy of Etizolam can be decreased when used in combination with Aminophylline.
Ticlopidine The metabolism of Etizolam can be decreased when combined with Ticlopidine.
Chloramphenicol The metabolism of Etizolam can be decreased when combined with Chloramphenicol.
Lansoprazole The metabolism of Etizolam can be decreased when combined with Lansoprazole.
Zafirlukast The metabolism of Etizolam can be decreased when combined with Zafirlukast.
Isoniazid The metabolism of Etizolam can be decreased when combined with Isoniazid.
Miconazole The metabolism of Etizolam can be decreased when combined with Miconazole.
Gemfibrozil The metabolism of Etizolam can be decreased when combined with Gemfibrozil.

Target Protein

GABA(A) Receptor GABRA1
GABA(A) Receptor Benzodiazepine Binding Site GABRA1
Platelet-activating factor receptor PTAFR

Referensi & Sumber

Synthesis reference: Tahara T, Araki K, Shiroki M, Matsuo H, Munakata T. Syntheses and structure-activity relationships of 6-aryl-4H-s-triazolo3,4-cthieno2,3-e 1,4diazepines. Arzneimittelforschung. 1978;28(7):1153-8.
Artikel (PubMed)
  • PMID: 10083975
    Sanna E, Pau D, Tuveri F, Massa F, Maciocco E, Acquas C, Floris C, Fontana SN, Maira G, Biggio G: Molecular and neurochemical evaluation of the effects of etizolam on GABAA receptors under normal and stress conditions. Arzneimittelforschung. 1999 Feb;49(2):88-95.
  • PMID: 1981698
    Casacchia M, Bolino F, Ecari U: Etizolam in the treatment of generalized anxiety disorder: a double-blind study versus placebo. Curr Med Res Opin. 1990;12(4):215-23.
  • PMID: 2572494
    Bertolino A, Mastucci E, Porro V, Corfiati L, Palermo M, Ecari U, Ceccarelli G: Etizolam in the treatment of generalized anxiety disorder: a controlled clinical trial. J Int Med Res. 1989 Sep-Oct;17(5):455-60.
  • PMID: 2692969
    Pariante F, Caddeo S, Ecari U: Etizolam in the treatment of generalized anxiety disorder associated with depressive symptoms. Curr Med Res Opin. 1989;11(9):543-9.
  • PMID: 2890779
    Mikashima H, Takehara S, Muramoto Y, Khomaru T, Terasawa M, Tahara T, Maruyama Y: An antagonistic activity of etizolam on platelet-activating factor (PAF). In vitro effects on platelet aggregation and PAF receptor binding. Jpn J Pharmacol. 1987 Aug;44(4):387-91.
  • PMID: 2065698
    Fracasso C, Confalonieri S, Garattini S, Caccia S: Single and multiple dose pharmacokinetics of etizolam in healthy subjects. Eur J Clin Pharmacol. 1991;40(2):181-5.
Textbook
  • ISBN: 978-0-7020-3471-8
    43. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 533-538). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 0 • International brands: 12
International Brands
  • Arophalm — Nichi-Iko Pharmaceutical
  • Capsafe — Ohara Yakuhin
  • Dezolam — Taisho Yakuhin
  • E1 — Aarpik
  • Eticalm — Towa Yakuhin
  • Etisedan — Kyowa Yakuhin
  • Etizolan — Kobayashi Kako
  • Mozun — Tatsumi Kagaku
  • New Zomnia — Molekule
  • Nonnerv — Nisshin Pharmaceutical

Sekuens Gen/Protein (FASTA)

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