Peringatan Keamanan

LD50>2000 mg/kg (rat, oral)

Granisetron

DB00889

small molecule approved investigational

Deskripsi

A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic and antinauseant for cancer chemotherapy patients.

Struktur Molekul 2D

Berat 312.417
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 4-6 hours in healthy patients, 9-12 hours in cancer patients
Volume Distribusi -
Klirens (Clearance) * 0.52 L/h/kg [Cancer Patients with 1 mg bid for 7 days] * 0.41 L/h/kg [Healthy subject with a single 1 mg dose]

Absorpsi

Absorption of is rapid and complete, though oral bioavailability is reduced to about 60% as a result of first pass metabolism.

Metabolisme

Primarily hepatic; undergoes N -demethylation and aromatic ring oxidation followed by conjugation. Animal studies suggest that some of the metabolites may have 5-HT 3 receptor antagonist activity.

Rute Eliminasi

The remainder of the dose is excreted as metabolites, 48% in the urine and 38% in the feces.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1026 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Granisetron.
Buprenorphine Granisetron 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 Granisetron.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Granisetron.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Granisetron.
Hydrocodone Granisetron may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Granisetron can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Granisetron may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Granisetron may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Granisetron.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Granisetron.
Orphenadrine Granisetron may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Granisetron 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 Granisetron.
Pramipexole Granisetron may increase the sedative activities of Pramipexole.
Ropinirole Granisetron may increase the sedative activities of Ropinirole.
Rotigotine Granisetron may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Granisetron.
Sodium oxybate Granisetron may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Granisetron 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 Granisetron.
Thalidomide Granisetron may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Granisetron 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 Granisetron.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Granisetron.
Dicoumarol The risk or severity of adverse effects can be increased when Granisetron is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Granisetron is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Granisetron is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Granisetron is combined with Tioclomarol.
Warfarin The risk or severity of adverse effects can be increased when Granisetron is combined with Warfarin.
Phenprocoumon The risk or severity of adverse effects can be increased when Granisetron is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Granisetron is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Granisetron is combined with 4-hydroxycoumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Granisetron is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Granisetron is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Granisetron is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Granisetron is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Granisetron is combined with Diphenadione.
(S)-Warfarin The risk or severity of adverse effects can be increased when Granisetron is combined with (S)-Warfarin.
Mirtazapine Granisetron may increase the serotonergic activities of Mirtazapine.
Ethanol Granisetron may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Granisetron 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 Granisetron.
Fluvoxamine The risk or severity of adverse effects can be increased when Granisetron is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Granisetron is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Granisetron is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Granisetron is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Granisetron is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Granisetron is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Granisetron is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Granisetron is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Granisetron.
Seproxetine The risk or severity of adverse effects can be increased when Granisetron is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Granisetron is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Granisetron is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Granisetron is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Granisetron is combined with Alaproclate.
Methylene blue Granisetron may increase the serotonergic activities of Methylene blue.
Zopiclone The risk or severity of adverse effects can be increased when Granisetron is combined with Zopiclone.
Citalopram The risk or severity of QTc prolongation can be increased when Granisetron is combined with Citalopram.
Anagrelide The risk or severity of QTc prolongation can be increased when Granisetron is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Granisetron is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Granisetron is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Granisetron is combined with Valproic acid.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Granisetron is combined with Grepafloxacin.
Quinine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Quinine.
Sotalol The risk or severity of QTc prolongation can be increased when Granisetron is combined with Sotalol.
Erlotinib The risk or severity of QTc prolongation can be increased when Granisetron is combined with Erlotinib.
Toremifene The risk or severity of QTc prolongation can be increased when Granisetron is combined with Toremifene.
Imatinib The risk or severity of QTc prolongation can be increased when Granisetron is combined with Imatinib.
Thioridazine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Granisetron is combined with Trovafloxacin.
Mifepristone The risk or severity of QTc prolongation can be increased when Granisetron is combined with Mifepristone.
Cocaine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Cocaine.
Procainamide The risk or severity of QTc prolongation can be increased when Granisetron is combined with Procainamide.
Arsenic trioxide The risk or severity of QTc prolongation can be increased when Granisetron is combined with Arsenic trioxide.
Domperidone The risk or severity of QTc prolongation can be increased when Granisetron is combined with Domperidone.
Sparfloxacin The risk or severity of QTc prolongation can be increased when Granisetron is combined with Sparfloxacin.
Halofantrine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Halofantrine.
Bepridil The risk or severity of QTc prolongation can be increased when Granisetron is combined with Bepridil.
Paliperidone The risk or severity of QTc prolongation can be increased when Granisetron is combined with Paliperidone.
Lithium cation The risk or severity of QTc prolongation can be increased when Granisetron is combined with Lithium cation.
Temafloxacin The risk or severity of QTc prolongation can be increased when Granisetron is combined with Temafloxacin.
Zuclopenthixol The risk or severity of QTc prolongation can be increased when Granisetron is combined with Zuclopenthixol.
Tetrabenazine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Tetrabenazine.
Iloperidone The risk or severity of QTc prolongation can be increased when Granisetron is combined with Iloperidone.
Vandetanib The risk or severity of QTc prolongation can be increased when Granisetron is combined with Vandetanib.
Romidepsin The risk or severity of QTc prolongation can be increased when Granisetron is combined with Romidepsin.
Asenapine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Asenapine.
Artemether The risk or severity of QTc prolongation can be increased when Granisetron is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Lumefantrine.
Vemurafenib The risk or severity of QTc prolongation can be increased when Granisetron is combined with Vemurafenib.
Glasdegib The risk or severity of QTc prolongation can be increased when Granisetron is combined with Glasdegib.
Deutetrabenazine The risk or severity of QTc prolongation can be increased when Granisetron is combined with Deutetrabenazine.
Macimorelin The risk or severity of QTc prolongation can be increased when Granisetron is combined with Macimorelin.
Terodiline The risk or severity of QTc prolongation can be increased when Granisetron is combined with Terodiline.
Dofetilide The risk or severity of QTc prolongation can be increased when Granisetron is combined with Dofetilide.
Cisapride The risk or severity of QTc prolongation can be increased when Granisetron is combined with Cisapride.
Astemizole The risk or severity of QTc prolongation can be increased when Granisetron is combined with Astemizole.

Target Protein

5-hydroxytryptamine receptor 3A HTR3A

Referensi & Sumber

Synthesis reference: Neal Ward, David Alan Jones, Victor Witold Jacewicz, "Process for the preparation of granisetron." U.S. Patent US6268498, issued April, 1986.
Artikel (PubMed)
  • PMID: 15740177
    Gan TJ: Selective serotonin 5-HT3 receptor antagonists for postoperative nausea and vomiting: are they all the same? CNS Drugs. 2005;19(3):225-38.
  • PMID: 12943486
    Tan M: Granisetron: new insights into its use for the treatment of chemotherapy-induced nausea and vomiting. Expert Opin Pharmacother. 2003 Sep;4(9):1563-71.
  • PMID: 16044252
    Feyer P, Seegenschmiedt MH, Steingraeber M: Granisetron in the control of radiotherapy-induced nausea and vomiting: a comparison with other antiemetic therapies. Support Care Cancer. 2005 Sep;13(9):671-8. Epub 2005 Jul 26.

Contoh Produk & Brand

Produk: 74 • International brands: 3
Produk
  • Apo-granisetron
    Tablet • 1 mg • Oral • Canada • Generic • Approved
  • Granisetron
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Granisetron
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Granisetron
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Granisetron
    Injection, solution • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Granisetron
    Injection, solution • 0.1 mg/1mL • Intravenous • US • Generic • Approved
  • Granisetron Hydrochloride
    Injection • 1 mg/1mL • Intravenous • US • Generic • Approved
  • Granisetron Hydrochloride
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 74 produk.
International Brands
  • Kevatril
  • Sancuso
  • Sustol

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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