Peringatan Keamanan

Overdosage may lead to cardiorespiratory depression, formic acid toxicity (methanol toxicity-like effects), and/or phosphate-induced hypocalemia. Most common adverse reactions (> 20%) are paresthesia and pruritus.

Fospropofol

DB06716

small molecule approved illicit investigational

Deskripsi

Fospropofol is a water soluble prodrug and is converted to propofol in the liver. Fospropofol is a short acting hypnotic/sedative/anesthetic agent. Unlike propofol, does not cause injection-site pain as it is unable to activate TRPA1. FDA approved in December 2008.
Fospropofol is a Schedule IV controlled substance in the United States under the Controlled Substances Act.

Struktur Molekul 2D

Berat 288.2766
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) When given to a patient, the half-lives are as follows: Fospropofol = 0.81 hours; Propofol metabolite = 1.13 hours
Volume Distribusi Fospropofol = 0.33±0.069 L/kg; Propofol metabolite = 5.8 L/kg.
Klirens (Clearance) Total body clearance (CLp), Fospropofol, healthy subject = 0.28 L/h/kg; CLp, fospropofol, patients = 0.31 L/h/kg; CLp/F, propofol, healthy subjects or patients = 2.74 L/h/kg.

Absorpsi

Adequate sedation achieved after 7 minutes with a IV bolus dose of 10mg/kg. It takes 21-45 minutes for patients to recover for fospropopol-induced sedation. Following an intravenous bolus administration of 6 mg/kg in a healthy subject, the pharmacokinetic parameters of fospropofol are as follows: Cmax = 78.7 ?g/mL; Tmax = 4 minutes; AUC(0-?) = 19.0 ?g ? h/mL;

Metabolisme

Fospropofol is metabolized into propofol, formaldehyde, and phosphate by endothelial alkaline phosphatase. The metabolite, formaldehyde, is quickly oxidized into formic acid by glutathione dependent and independent dehydrogenases and erythrocytes. Excess formic acid is eliminated via oxidation to carbon dioxide through the tetrahydrofolate pathway. Propofol is further metabolized into propofol glucuronide, quinol-4-sulfate, quinol-1-fluronide, and quinol-4-glucuronide. The cytochrome P450 enzyme system is not involved with the metabolism of fospropofol.

Rute Eliminasi

Chiefly eliminated by hepatic conjugation to inactive metabolites which are excreted by the kidney. There is negligible renal elimination of unchanged fospropofol (<0.02%).

Interaksi Obat

675 Data
Buprenorphine Fospropofol 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 Fospropofol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.
Hydrocodone Fospropofol 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 Fospropofol.
Magnesium sulfate The therapeutic efficacy of Fospropofol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Fospropofol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Fospropofol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.
Mirtazapine Fospropofol 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 Fospropofol.
Orphenadrine Fospropofol may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Fospropofol 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 Fospropofol.
Pramipexole Fospropofol may increase the sedative activities of Pramipexole.
Ropinirole Fospropofol may increase the sedative activities of Ropinirole.
Rotigotine Fospropofol may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Fospropofol.
Suvorexant Fospropofol 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 Fospropofol.
Thalidomide Fospropofol may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Fospropofol may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Fospropofol.
Sodium oxybate Fospropofol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Ethanol Fospropofol may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Fospropofol 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 Fospropofol.
Fluvoxamine The risk or severity of adverse effects can be increased when Fospropofol is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Fospropofol is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Fospropofol is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Fospropofol is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Fospropofol is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Fospropofol is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Fospropofol is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Fospropofol is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Fospropofol is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Fospropofol is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Fospropofol is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Fospropofol is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Fospropofol is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Fospropofol is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Fospropofol is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Fospropofol is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Fospropofol is combined with Alaproclate.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Fospropofol.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Fospropofol.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Fospropofol.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Fospropofol.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Fospropofol.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Fospropofol.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Fospropofol.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Fospropofol.
Desipramine The risk or severity of CNS depression can be increased when Desipramine is combined with Fospropofol.
Pizotifen The risk or severity of CNS depression can be increased when Pizotifen is combined with Fospropofol.
Dosulepin The risk or severity of CNS depression can be increased when Fospropofol is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Fospropofol is combined with Zopiclone.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Fospropofol.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Fospropofol.
Tryptophan The risk or severity of CNS depression can be increased when Tryptophan is combined with Fospropofol.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Fospropofol.
Lorazepam The risk or severity of CNS depression can be increased when Lorazepam is combined with Fospropofol.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Fospropofol.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Fospropofol.
Reserpine The risk or severity of CNS depression can be increased when Reserpine is combined with Fospropofol.
Eletriptan The risk or severity of CNS depression can be increased when Eletriptan is combined with Fospropofol.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Fospropofol.
Temazepam The risk or severity of CNS depression can be increased when Temazepam is combined with Fospropofol.
Reboxetine The risk or severity of CNS depression can be increased when Reboxetine is combined with Fospropofol.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Fospropofol.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Fospropofol.
Methysergide The risk or severity of CNS depression can be increased when Methysergide is combined with Fospropofol.
Cabergoline The risk or severity of CNS depression can be increased when Cabergoline is combined with Fospropofol.
Phenytoin The risk or severity of CNS depression can be increased when Phenytoin is combined with Fospropofol.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Fospropofol.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Fospropofol.
Venlafaxine The risk or severity of CNS depression can be increased when Venlafaxine is combined with Fospropofol.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Fospropofol.
Morphine The risk or severity of CNS depression can be increased when Morphine is combined with Fospropofol.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Fospropofol.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Fospropofol.
Valproic acid The risk or severity of CNS depression can be increased when Valproic acid is combined with Fospropofol.
Zolmitriptan The risk or severity of CNS depression can be increased when Zolmitriptan is combined with Fospropofol.
Codeine The risk or severity of CNS depression can be increased when Codeine is combined with Fospropofol.
Dihydroergotamine The risk or severity of CNS depression can be increased when Dihydroergotamine is combined with Fospropofol.
Tolcapone The risk or severity of CNS depression can be increased when Tolcapone is combined with Fospropofol.
Hydromorphone The risk or severity of CNS depression can be increased when Hydromorphone is combined with Fospropofol.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Fospropofol.
Cetirizine The risk or severity of CNS depression can be increased when Cetirizine is combined with Fospropofol.
Protriptyline The risk or severity of CNS depression can be increased when Protriptyline is combined with Fospropofol.
Trimethadione The risk or severity of CNS depression can be increased when Trimethadione is combined with Fospropofol.
Clobazam The risk or severity of sedation, somnolence, and CNS depression can be increased when Clobazam is combined with Fospropofol.
Chlorzoxazone The risk or severity of CNS depression can be increased when Chlorzoxazone is combined with Fospropofol.
Clozapine The risk or severity of CNS depression can be increased when Clozapine is combined with Fospropofol.
Meprobamate The risk or severity of CNS depression can be increased when Meprobamate is combined with Fospropofol.
Thiethylperazine The risk or severity of CNS depression can be increased when Thiethylperazine is combined with Fospropofol.
Palonosetron The risk or severity of CNS depression can be increased when Palonosetron is combined with Fospropofol.
Sulpiride The risk or severity of CNS depression can be increased when Sulpiride is combined with Fospropofol.
Alprazolam The risk or severity of CNS depression can be increased when Alprazolam is combined with Fospropofol.
Dexbrompheniramine The risk or severity of CNS depression can be increased when Dexbrompheniramine is combined with Fospropofol.

Target Protein

Gamma-aminobutyric acid receptor subunit beta-2 GABRB2
Gamma-aminobutyric acid receptor subunit beta-3 GABRB3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20205488
    Garnock-Jones KP, Scott LJ: Fospropofol. Drugs. 2010 Mar 5;70(4):469-77. doi: 10.2165/11204450-000000000-00000.
  • PMID: 12650488
    Schywalsky M, Ihmsen H, Tzabazis A, Fechner J, Burak E, Vornov J, Schwilden H: Pharmacokinetics and pharmacodynamics of the new propofol prodrug GPI 15715 in rats. Eur J Anaesthesiol. 2003 Mar;20(3):182-90.
  • PMID: 21804712
    Bengalorkar GM, Bhuvana K, Sarala N, Kumar T: Fospropofol: clinical pharmacology. J Anaesthesiol Clin Pharmacol. 2011 Jan;27(1):79-83.
  • PMID: 22584560
    Patwardhan A, Edelmayer R, Annabi E, Price T, Malan P, Dussor G: Receptor specificity defines algogenic properties of propofol and fospropofol. Anesth Analg. 2012 Oct;115(4):837-40. Epub 2012 May 14.

Contoh Produk & Brand

Produk: 1 • International brands: 1
Produk
  • Lusedra
    Injection • 35 mg/1mL • Intravenous • US • Approved
International Brands
  • Aquavan

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