Peringatan Keamanan

Benzodiazepine overdose is typically characterized by central nervous system depression ranging from mild drowsiness to coma.L44913 Mild-to-moderate cases may involve relatively minor symptoms like drowsiness, dysarthria, confusion, and ataxia, while severe cases may lead to respiratory depression and coma. In rare cases, paradoxical disinhibitory reactions (e.g. agitation, violent behaviour, impulsivity) may occur.

The management of benzodiazepine overdose should involve general supportive measures as clinically indicated. Flumazenil is a benzodiazepine receptor antagonist which is indicated for the complete or partial reversal of benzodiazepine-induced sedation, although its appropriateness is highly dependent on the clinical status and history of the patient.L44913 The use of flumazenil can lead to withdrawal and significant adverse reactions (e.g. seizures), especially in the context of mixed overdoses and in long-term benzodiazepine users with an established physical dependency, and its use is contraindicated in patients using benzodiazepines for potentially life-threatening conditions (e.g. status epilepticus).L44913 If the decision is made to use flumazenil, it should be used as specified in its prescribing information and as an adjunct alongside general supportive management.

Quazepam

DB01589

small molecule approved illicit

Deskripsi

Quazepam is a trifluoroethyl benzodiazepine derivative. It was first approved in the US in 1985 and is used as a hypnotic for the treatment of insomnia.L44913

It appears to be unique amongst other benzodiazepine derivatives in its relatively high affinity for sleep-promoting ?1 subunit-containing GABAA receptors and low affinity for other receptors.A256858

Struktur Molekul 2D

Berat 386.794
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-lives of both quazepam and 2-oxoquazepam is approximately 39 hours.[L44913] The mean elimination half-life of N-desalkyl-2-oxoquazepam is approximately 73 hours.[L44913]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

The half-life of absorption following oral administration is approximately 30 minutes.L44913 Peak plasma concentration (Cmax) is approximately 20 ng/mL and occurs around 2 hours following administration.L44913

Metabolisme

Quazepam undergoes extensive hepatic metabolism, primarily via CYP3A4 and to a lesser extent via CYP2C9, CYP2C19, and FMO1.A31235 Quazepam is first metabolized to 2-oxoquazepam, which is then further metabolized to both N-desalkyl-2-oxoquazepam (norflurazepam) and 3-hydroxy-2-oxoquazepam.A31235,A256823 Both 2-oxoquazepam and N-desalkyl-2-oxoquazepam exert CNS depressant activity.L44913

Rute Eliminasi

Over the course of five days following the administration of radiolabeled quazepam, approximately 31% of the administered dose appeared in the urine and 23% appeared in the feces.L44913 Unchanged drug appeared in only trace amounts in the urine.L44913

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Ingesting alcohol may increase the drowsiness and CNS depression caused by quazepam.

Interaksi Obat

798 Data
Buprenorphine Quazepam 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 Quazepam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Quazepam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Quazepam.
Hydrocodone Quazepam 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 Quazepam.
Magnesium sulfate The therapeutic efficacy of Quazepam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Quazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Quazepam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Quazepam.
Mirtazapine Quazepam 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 Quazepam.
Orphenadrine Quazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Quazepam 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 Quazepam.
Pramipexole Quazepam may increase the sedative activities of Pramipexole.
Ropinirole Quazepam may increase the sedative activities of Ropinirole.
Rotigotine Quazepam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Quazepam.
Suvorexant Quazepam 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 Quazepam.
Thalidomide Quazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Quazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Quazepam is combined with Clozapine.
Methadone Quazepam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Sodium oxybate Quazepam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Quazepam can be increased when it is combined with Teduglutide.
Flumazenil Flumazenil may decrease the sedative activities of Quazepam.
Ethanol Quazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Quazepam 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 Quazepam.
Fluvoxamine The risk or severity of adverse effects can be increased when Quazepam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Quazepam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Quazepam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Quazepam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Quazepam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Quazepam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Quazepam is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Quazepam is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Quazepam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Quazepam is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Quazepam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Quazepam is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Quazepam is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Quazepam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Quazepam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Quazepam is combined with Alaproclate.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Quazepam.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Quazepam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Quazepam.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Quazepam.
Pizotifen The risk or severity of CNS depression can be increased when Quazepam is combined with Pizotifen.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Quazepam.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Quazepam.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Quazepam.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Quazepam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Quazepam.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Quazepam.
Zopiclone The risk or severity of adverse effects can be increased when Quazepam is combined with Zopiclone.
Caffeine The therapeutic efficacy of Quazepam can be decreased when used in combination with Caffeine.
Dyphylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Dyphylline.
Pentoxifylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Pentoxifylline.
Mercaptopurine The therapeutic efficacy of Quazepam can be decreased when used in combination with Mercaptopurine.
Oxtriphylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Oxtriphylline.
Theobromine The therapeutic efficacy of Quazepam can be decreased when used in combination with Theobromine.
Fenethylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Fenethylline.
8-azaguanine The therapeutic efficacy of Quazepam can be decreased when used in combination with 8-azaguanine.
7,9-Dimethylguanine The therapeutic efficacy of Quazepam can be decreased when used in combination with 7,9-Dimethylguanine.
Xanthine The therapeutic efficacy of Quazepam can be decreased when used in combination with Xanthine.
7-Deazaguanine The therapeutic efficacy of Quazepam can be decreased when used in combination with 7-Deazaguanine.
Guanine The therapeutic efficacy of Quazepam can be decreased when used in combination with Guanine.
9-Methylguanine The therapeutic efficacy of Quazepam can be decreased when used in combination with 9-Methylguanine.
Peldesine The therapeutic efficacy of Quazepam can be decreased when used in combination with Peldesine.
Hypoxanthine The therapeutic efficacy of Quazepam can be decreased when used in combination with Hypoxanthine.
9-Deazaguanine The therapeutic efficacy of Quazepam can be decreased when used in combination with 9-Deazaguanine.
Propentofylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Propentofylline.
Valomaciclovir The therapeutic efficacy of Quazepam can be decreased when used in combination with Valomaciclovir.
3-isobutyl-1-methyl-7H-xanthine The therapeutic efficacy of Quazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
Uric acid The therapeutic efficacy of Quazepam can be decreased when used in combination with Uric acid.
Doxofylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Doxofylline.
6-O-benzylguanine The therapeutic efficacy of Quazepam can be decreased when used in combination with 6-O-benzylguanine.
Lisofylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Lisofylline.
Lobucavir The therapeutic efficacy of Quazepam can be decreased when used in combination with Lobucavir.
Cafedrine The therapeutic efficacy of Quazepam can be decreased when used in combination with Cafedrine.
Theodrenaline The therapeutic efficacy of Quazepam can be decreased when used in combination with Theodrenaline.
Bamifylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Bamifylline.
Proxyphylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Proxyphylline.
Acefylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Acefylline.
Etamiphylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Etamiphylline.
Pentifylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Pentifylline.
Bufylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Bufylline.
Bromotheophylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Bromotheophylline.
Furafylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Furafylline.
8-chlorotheophylline The therapeutic efficacy of Quazepam can be decreased when used in combination with 8-chlorotheophylline.
PCS-499 The therapeutic efficacy of Quazepam can be decreased when used in combination with PCS-499.
Theophylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Theophylline.
Aminophylline The therapeutic efficacy of Quazepam can be decreased when used in combination with Aminophylline.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Quazepam.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Quazepam.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Quazepam.

Target Protein

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15801544
    Miura M, Ohkubo T: In vitro metabolism of quazepam in human liver and intestine and assessment of drug interactions. Xenobiotica. 2004 Nov-Dec;34(11-12):1001-11.
  • PMID: 2858372
    Zampaglione N, Hilbert JM, Ning J, Chung M, Gural R, Symchowicz S: Disposition and metabolic fate of 14C-quazepam in man. Drug Metab Dispos. 1985 Jan-Feb;13(1):25-9.
  • PMID: 23789008
    Griffin CE 3rd, Kaye AM, Bueno FR, Kaye AD: Benzodiazepine pharmacology and central nervous system-mediated effects. Ochsner J. 2013 Summer;13(2):214-23.
  • 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.
  • PMID: 31274695
    Moniri NH: Reintroduction of quazepam: an update on comparative hypnotic and adverse effects. Int Clin Psychopharmacol. 2019 Nov;34(6):275-285. doi: 10.1097/YIC.0000000000000277.

Contoh Produk & Brand

Produk: 13 • International brands: 1
Produk
  • Doral
    Tablet • 15 mg/1 • Oral • US • Approved
  • Doral
    Tablet • 15 mg/1 • Oral • US • Approved
  • Doral
    Tablet • 15 mg/1 • Oral • US • Approved
  • Doral
    Tablet • 15 mg/1 • Oral • US • Approved
  • Quazepam
    Tablet • 15 mg/1 • Oral • US • Approved
  • Quazepam
    Tablet • 15 mg/1 • Oral • US • Approved
  • Quazepam
    Tablet • 15 mg/1 • Oral • US • Approved
  • Quazepam
    Tablet • 15 mg/1 • Oral • US • Approved
Menampilkan 8 dari 13 produk.
International Brands
  • Dormalin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul