Peringatan Keamanan

The oral LD50 in rats and mice is >8000 mg/kg and 1540 mg/kg, respectively.L13904

Symptoms of oxazepam overdose are likely to be consistent with its adverse effect profile and range from mild to severe, sometimes fatal, CNS depression.L13895 Treatment should include gastric decontamination, via lavage or induced vomiting, followed by symptomatic and supportive measures. The benzodiazepine antagonist flumazenil may be used in hospitalized patients as an adjunct to non-pharmacological management, but may increase the risk of seizure in long-term benzodiazepine users and in cyclic antidepressant overdose.L13895

Oxazepam

DB00842

small molecule approved

Deskripsi

Oxazepam is an intermediate-acting, 3-hydroxybenzodiazepine used in the treatment of alcohol withdrawal and anxiety disorders. Oxazepam, like related 3-hydroxybenzodiazepine lorazepam, is considered less susceptible to pharmacokinetic variability based on patient-specific factors (e.g. age, liver disease) - this feature is advantageous as compared to other benzodiazepines, and is likely owing in part to oxazepam's relatively simple metabolism.A203516 It is an active metabolite of both diazepam and temazepamA39486 and undergoes very little biotransformation following absorption, making it unlikely to participate in pharmacokinetic interactions.L13895

Struktur Molekul 2D

Berat 286.713
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of oxazepam is 8.2 hours.[L13895]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Following oral administration, peak plasma levels (Cmax) averaged 450 mg/mL and occurred approximately 3 hours (Tmax) after dosing.L13895

Metabolisme

Oxazepam has a single major inactive metabolite, a glucuronide conjugate.L13895 The glucuronidation of the S-isomer is catalyzed by UGT2B15. The glucuronidation of the R-isomer is catalyzed by UGT2B7 and UGT1A9.A18016

Rute Eliminasi

Oxazepam is primarily eliminated in the urine as its glucuronide metabolite, with the feces containing approximately 21% of the unchanged drug.L13898 The majority of an orally ingested dose of oxazepam is excreted within 48 hours.L13898

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Co-administration with alcohol may potentiate the CNS effects of oxazepam.

Interaksi Obat

1341 Data
Buprenorphine Oxazepam 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 Oxazepam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Oxazepam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Oxazepam.
Hydrocodone Oxazepam 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 Oxazepam.
Magnesium sulfate The therapeutic efficacy of Oxazepam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Oxazepam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Oxazepam.
Mirtazapine Oxazepam 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 Oxazepam.
Orphenadrine Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Oxazepam 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 Oxazepam.
Pramipexole Oxazepam may increase the sedative activities of Pramipexole.
Ropinirole Oxazepam may increase the sedative activities of Ropinirole.
Rotigotine Oxazepam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Oxazepam.
Suvorexant Oxazepam 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 Oxazepam.
Thalidomide Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Oxazepam is combined with Clozapine.
Methadone Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Sodium oxybate Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Oxazepam can be increased when it is combined with Teduglutide.
Yohimbine The therapeutic efficacy of Oxazepam can be increased when used in combination with Yohimbine.
Flumazenil Flumazenil may decrease the sedative activities of Oxazepam.
Ethanol Oxazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Oxazepam 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 Oxazepam.
Zimelidine The risk or severity of adverse effects can be increased when Oxazepam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Oxazepam is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Oxazepam is combined with Seproxetine.
Fluvoxamine The risk or severity of adverse effects can be increased when Oxazepam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Oxazepam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Oxazepam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Oxazepam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Oxazepam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Oxazepam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Oxazepam is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Oxazepam is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Oxazepam is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Oxazepam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Oxazepam is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Oxazepam is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Oxazepam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Oxazepam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Oxazepam is combined with Alaproclate.
Benzatropine Benzatropine may decrease the excretion rate of Oxazepam which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Oxazepam which could result in a higher serum level.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Oxazepam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Oxazepam.
Propantheline Propantheline may decrease the excretion rate of Oxazepam which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Oxazepam which could result in a higher serum level.
Tolterodine Oxazepam may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Flavoxate Oxazepam may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Oxazepam may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Fesoterodine Oxazepam may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Oxazepam may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Oxazepam may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Oxazepam may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Oxazepam may decrease the excretion rate of Propiverine which could result in a higher serum level.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Oxazepam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Oxazepam.
Doxepin The risk or severity of CNS depression can be increased when Oxazepam is combined with Doxepin.
Desipramine The risk or severity of CNS depression can be increased when Oxazepam is combined with Desipramine.
Zopiclone The risk or severity of adverse effects can be increased when Oxazepam is combined with Zopiclone.
Caffeine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Caffeine.
Dyphylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Dyphylline.
Pentoxifylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Pentoxifylline.
Mercaptopurine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Mercaptopurine.
Oxtriphylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Oxtriphylline.
Theobromine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Theobromine.
Fenethylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Fenethylline.
8-azaguanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 8-azaguanine.
7,9-Dimethylguanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 7,9-Dimethylguanine.
Xanthine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Xanthine.
7-Deazaguanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 7-Deazaguanine.
Guanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Guanine.
9-Methylguanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 9-Methylguanine.
Peldesine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Peldesine.
Hypoxanthine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Hypoxanthine.
9-Deazaguanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 9-Deazaguanine.
Propentofylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Propentofylline.
Valomaciclovir The therapeutic efficacy of Oxazepam can be decreased when used in combination with Valomaciclovir.
3-isobutyl-1-methyl-7H-xanthine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
Uric acid The therapeutic efficacy of Oxazepam can be decreased when used in combination with Uric acid.
Doxofylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Doxofylline.
6-O-benzylguanine The therapeutic efficacy of Oxazepam can be decreased when used in combination with 6-O-benzylguanine.
Lisofylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Lisofylline.
Lobucavir The therapeutic efficacy of Oxazepam can be decreased when used in combination with Lobucavir.
Cafedrine The therapeutic efficacy of Oxazepam can be decreased when used in combination with Cafedrine.
Theodrenaline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Theodrenaline.
Bamifylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Bamifylline.
Proxyphylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Proxyphylline.
Acefylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Acefylline.
Etamiphylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Etamiphylline.
Pentifylline The therapeutic efficacy of Oxazepam can be decreased when used in combination with Pentifylline.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 8700792
    Peppers MP: Benzodiazepines for alcohol withdrawal in the elderly and in patients with liver disease. Pharmacotherapy. 1996 Jan-Feb;16(1):49-57.
  • PMID: 6135616
    Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8.
  • PMID: 2570451
    Oelschlager H: Chemical and pharmacologic aspects of benzodiazepines. Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72.
  • PMID: 1349754
    Christensen P, Lolk A, Gram LF, Kragh-Sorensen P: Benzodiazepine-induced sedation and cortisol suppression. A placebo-controlled comparison of oxazepam and nitrazepam in healthy male volunteers. Psychopharmacology (Berl). 1992;106(4):511-6.
  • PMID: 851373
    Olive G, Dreux C: Pharmacologic bases of use of benzodiazepines in pereinatal medicine. Arch Fr Pediatr. 1977 Jan;34(1):74-89.
  • PMID: 23330992
    Altamura AC, Moliterno D, Paletta S, Maffini M, Mauri MC, Bareggi S: Understanding the pharmacokinetics of anxiolytic drugs. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):423-40. doi: 10.1517/17425255.2013.759209. Epub 2013 Jan 21.
  • PMID: 21671987
    Chin PK, Jensen BP, Larsen HS, Begg EJ: Adult age and ex vivo protein binding of lorazepam, oxazepam and temazepam in healthy subjects. Br J Clin Pharmacol. 2011 Dec;72(6):985-9. doi: 10.1111/j.1365-2125.2011.04036.x.
  • PMID: 23038269
    Sigel E, Steinmann ME: Structure, function, and modulation of GABA(A) receptors. J Biol Chem. 2012 Nov 23;287(48):40224-31. doi: 10.1074/jbc.R112.386664. Epub 2012 Oct 4.
Menampilkan 8 dari 13 artikel.

Contoh Produk & Brand

Produk: 61 • International brands: 24
Produk
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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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