Brotizolam

DB09017

small molecule investigational withdrawn

Deskripsi

Brotizolam is a sedative-hypnotic thienodiazepine drug which is a benzodiazepine analog. It demonstrates anxiolytic, anticonvulsant, hypnotic, sedative and skeletal muscle relaxant effects. Brotizolam has similar effects to short-acting benzodiazepines such as triazolam. Brotizolam is indicated for 2-4 weeks of treatment for severe or debilitating insomnia. Brotizolam is an extremely potent drug and it is rapidly eliminated with an average half-life of 4.4 hours (range 3.6 - 7.9 hours).

Brotizolam is not approved for sale in the UK, United States or Canada but is sold in the Netherlands, Germany, Spain, Belgium, Austria, Portugal, Israel, Italy and Japan.

Struktur Molekul 2D

Berat 393.689
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 4.4 hours.
Volume Distribusi 0.63 l/kg.
Klirens (Clearance) Total clearance: 109 ml/min.

Absorpsi

The plasma concentration profile of brotizolam can be described as a one compartmental open model with first-order absorption.

Metabolisme

There are two primary metabolites: 1-methyl-hydroxy- and the 4-hydroxy-derivatives (Eberts et al., 1981; Boehringer Ingelheim, product information). The 4-hydroxymetabolites have a pharmacological activity which is far less than that of the parent drugs, but the 1-methyl-hydroxymetabolites probably have comparable activity (Gall et al., 1978; Jochemsen et al., 1982; Sethy & Harris, 1982; Jochemsen et al., unpublished results). These active compounds are, however, not present in plasma in measurable amounts following a single dose of brotizolam to young healthy subjects (Jochemsen et al., 1982; Jochemsen et al., unpublished results).

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

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

Target Protein

GABA(A) Receptor GABRA1
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Synthesis reference: Brotizolam synthesis: Weber, K. H.; Bauer, A.; Danneberg, P.; Kuhn, F. J.; 1978, U.S. Patent 4,094,984.
Artikel (PubMed)
  • PMID: 6140948
    Jochemsen R, Wesselman JG, van Boxtel CJ, Hermans J, Breimer DD: Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects. Br J Clin Pharmacol. 1983;16 Suppl 2:291S-297S.

Contoh Produk & Brand

Produk: 0 • International brands: 17
International Brands
  • Amnezon — Nisshin Seiyaku
  • Bondormin — Rafa
  • Brometon — Mylan Seiyaku
  • Brotizolam M — Sannova
  • Dormex — Recalcine
  • Eurimolan — Choseido Pharmaceutical
  • Goodmin — Tanabe Mitsubishi Pharma
  • Lendorm — Boehringer Ingelheim
  • Lendormin — Boehringer Ingelheim
  • Lindormin — Boehringer Ingelheim

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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