Peringatan Keamanan

Symptoms of remimazolam overdoses, as with other benzodiazepines, are likely to be consistent with its adverse effect profile and may therefore involve significant CNS depression, respiratory depression, ataxia, and hypotension.L14647 The benzodiazepine receptor antagonist flumazenil may be used for reversal of the sedative effects associated with benzodiazepine overdose, though it is not a substitute for proper supportive care.L14647

Remimazolam

DB12404

small molecule approved investigational

Deskripsi

Remimazolam is an ultra short-acting benzodiazepine used in the induction and maintenance of sedation during short (<30 minute) procedures.L14647 Recent trends in anesthesia-related drug development have touted the benefits of so-called "soft drugs" - these agents, such as remifentanil, are designed to be metabolically fragile and thus susceptible to rapid biotransformation and elimination as inactive metabolites.A214857 These "soft drugs" are useful in the context of surgical procedures, wherein a rapid onset/offset is desirable, enabling anesthesiologists to manipulate drug concentrations as needed.A214852,A214857 Remimazolam was the first "soft" benzodiazepine analog to be developedA214862 and was approved for use by the FDA in July 2020 under the brand name Byfavo.L14722

Struktur Molekul 2D

Berat 439.313
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following intravenous administration, the distribution half-life is of remimazolam is 0.5 - 2 minutes and the terminal elimination half-life is 37 - 53 minutes.[L14647] Half-life is increased in patients with hepatic impairment necessitating careful dose titration in this population.[L14647] The half-life of remimazolam's major inactive metabolite, CNS7054, is 2.4 - 3.8 hours.[L14647]
Volume Distribusi The volume of distribution is approximately 0.76 - 0.98 L/kg.[L14647]
Klirens (Clearance) The clearance of remimazolam is approximately 24 - 75 L/h and is independent of body weight.[L14647]

Absorpsi

The Cmax and AUC0-inf following intravenous administration of 0.01 to 0.5 mg/kg were 189 to 6,960 ng/mL and 12.1 to 452 ng?h/mL, respectively,L14647 and appear to be relatively dose proportional. The Tmax of the inactive CNS7054 metabolite is approximately 20-30 minutes and its AUC0-inf ranges from 231 to 7,090 ng?h/mL.L14647

Metabolisme

Remimazolam does not appear to undergo biotransformation via hepatic cytochrome P450 enzymes, nor does it induce or inhibit these enzymes.L14647 Its primary route of metabolism is hydrolysis via hepatic carboxylesterase-1 (CES1) to yield the inactive CNS7054 metabolite, which then undergoes glucuronidation and hydroxylation prior to elimination.L14647,A214842 CNS7054 possesses a 300-fold lesser affinity for GABA(A) receptors as compared to the parent drug.

Rute Eliminasi

In patients undergoing colonoscopy, approximately 0.003% of the administered dose is excreted in the urine as unchanged parent drug and 50-60% is excreted in the urine as CNS7054.L14647 In healthy subjects, >80% of the administered dose is excreted in the urine as CNS7054.L14647

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. The sedative effects of benzodiazepines may be exacerbated by the co-administration of alcohol.

Interaksi Obat

717 Data
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Remimazolam.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Remimazolam.
Hydrocodone Remimazolam 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 Remimazolam.
Metyrosine Remimazolam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Remimazolam.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Remimazolam.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Remimazolam.
Pramipexole Remimazolam may increase the sedative activities of Pramipexole.
Ropinirole Remimazolam may increase the sedative activities of Ropinirole.
Rotigotine Remimazolam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Remimazolam.
Suvorexant Remimazolam 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 Remimazolam.
Thalidomide Remimazolam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Remimazolam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Clozapine The risk or severity of adverse effects can be increased when Remimazolam is combined with Clozapine.
Sodium oxybate Remimazolam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Teduglutide The serum concentration of Remimazolam can be increased when it is combined with Teduglutide.
Methadone Remimazolam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
Flumazenil Flumazenil may decrease the sedative activities of Remimazolam.
Ethanol Remimazolam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Remimazolam 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 Remimazolam.
Fluvoxamine The risk or severity of adverse effects can be increased when Remimazolam is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Remimazolam is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Remimazolam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Remimazolam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Remimazolam is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Remimazolam is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Remimazolam is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Remimazolam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Remimazolam is combined with Desvenlafaxine.
Dapoxetine The risk or severity of adverse effects can be increased when Remimazolam is combined with Dapoxetine.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Remimazolam.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Remimazolam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Remimazolam.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Remimazolam.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Remimazolam.
Lamotrigine The risk or severity of CNS depression can be increased when Lamotrigine is combined with Remimazolam.
Clidinium The risk or severity of CNS depression can be increased when Clidinium is combined with Remimazolam.
Brompheniramine The risk or severity of CNS depression can be increased when Brompheniramine is combined with Remimazolam.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Remimazolam.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Remimazolam.
Quetiapine The risk or severity of CNS depression can be increased when Quetiapine is combined with Remimazolam.
Aripiprazole The risk or severity of sedation and orthostatic hypotension can be increased when Aripiprazole is combined with Remimazolam.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Remimazolam.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Remimazolam.
Chlorprothixene The risk or severity of CNS depression can be increased when Chlorprothixene is combined with Remimazolam.
Dosulepin The risk or severity of CNS depression can be increased when Dosulepin is combined with Remimazolam.
Zopiclone The risk or severity of adverse effects can be increased when Remimazolam is combined with Zopiclone.
Caffeine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Caffeine.
Theophylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Theophylline.
Dyphylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Dyphylline.
Pentoxifylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Pentoxifylline.
Mercaptopurine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Mercaptopurine.
Aminophylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Aminophylline.
Oxtriphylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Oxtriphylline.
Theobromine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Theobromine.
Fenethylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Fenethylline.
8-azaguanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 8-azaguanine.
7,9-Dimethylguanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 7,9-Dimethylguanine.
Xanthine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Xanthine.
7-Deazaguanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 7-Deazaguanine.
Guanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Guanine.
9-Methylguanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 9-Methylguanine.
Peldesine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Peldesine.
Hypoxanthine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Hypoxanthine.
9-Deazaguanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 9-Deazaguanine.
Propentofylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Propentofylline.
Valomaciclovir The therapeutic efficacy of Remimazolam can be decreased when used in combination with Valomaciclovir.
3-isobutyl-1-methyl-7H-xanthine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
Uric acid The therapeutic efficacy of Remimazolam can be decreased when used in combination with Uric acid.
Doxofylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Doxofylline.
6-O-benzylguanine The therapeutic efficacy of Remimazolam can be decreased when used in combination with 6-O-benzylguanine.
Lisofylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Lisofylline.
Lobucavir The therapeutic efficacy of Remimazolam can be decreased when used in combination with Lobucavir.
Cafedrine The therapeutic efficacy of Remimazolam can be decreased when used in combination with Cafedrine.
Theodrenaline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Theodrenaline.
Bamifylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Bamifylline.
Proxyphylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Proxyphylline.
Acefylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Acefylline.
Etamiphylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Etamiphylline.
Pentifylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Pentifylline.
Bufylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Bufylline.
Bromotheophylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Bromotheophylline.
Furafylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with Furafylline.
8-chlorotheophylline The therapeutic efficacy of Remimazolam can be decreased when used in combination with 8-chlorotheophylline.
PCS-499 The therapeutic efficacy of Remimazolam can be decreased when used in combination with PCS-499.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Remimazolam.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Remimazolam.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Remimazolam.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Remimazolam.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Remimazolam.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Remimazolam.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Remimazolam.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Remimazolam.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Remimazolam.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Remimazolam.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Remimazolam.

Target Protein

Gamma-aminobutyric acid receptor subunit gamma-3 GABRG3
GABA(A) Receptor GABRA1
GABA(A) Receptor Benzodiazepine Binding Site GABRA1

Referensi & Sumber

Synthesis reference: Dolitzky Ben-Zion, Mendelovici Marioara, Bodkhe Arjun Rajaram, Mane Ganesh Shivaji, Samala Rajamouli Srihari, Joshi Ashutosh Vijay, Parven Kumar Luthra, Amit Singh, Anantha Rajmohan Muthusamy "Process for the preparation of remimazolam and solid state forms of remimazolam salts." U.S. Patent US20190359619A1, filed Feb, 2018.
Artikel (PubMed)
  • PMID: 31037028
    Freyer N, Knospel F, Damm G, Greuel S, Schneider C, Seehofer D, Stohr T, Petersen KU, Zeilinger K: Metabolism of remimazolam in primary human hepatocytes during continuous long-term infusion in a 3-D bioreactor system. Drug Des Devel Ther. 2019 Apr 2;13:1033-1047. doi: 10.2147/DDDT.S186759. eCollection 2019.
  • 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: 32530892
    Birgenheier NM, Stuart AR, Egan TD: Soft drugs in anesthesia: remifentanil as prototype to modern anesthetic drug development. Curr Opin Anaesthesiol. 2020 Jun 8. doi: 10.1097/ACO.0000000000000879.
  • PMID: 19625797
    Egan TD: Is anesthesiology going soft?: trends in fragile pharmacology. Anesthesiology. 2009 Aug;111(2):229-30. doi: 10.1097/ALN.0b013e3181ae8460.
  • PMID: 25191193
    Goudra BG, Singh PM: Remimazolam: The future of its sedative potential. Saudi J Anaesth. 2014 Jul;8(3):388-91. doi: 10.4103/1658-354X.136627.

Contoh Produk & Brand

Produk: 3 • International brands: 1
Produk
  • Byfavo
    - • 50 mg • Intravenous • EU • Approved
  • Byfavo
    Injection, powder, for solution • 20 mg • Intravenous • EU • Approved
  • Byfavo
    Injection, powder, lyophilized, for solution • 2.5 mg/1mL • Intravenous • US • Approved
International Brands
  • Byfavo

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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