Peringatan Keamanan

A single intravenous dose of palonosetron at 30 mg/kg (947 and 474 times the human dose for rats and mice, respectively, based on body surface area) was lethal to rats and mice. The major signs of toxicity were convulsions, gasping, pallor, cyanosis and collapse.

Palonosetron

DB00377

small molecule approved investigational

Deskripsi

Palonosetron (INN, trade name Aloxi) is an antagonist of 5-HT3 receptors that is indicated for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is the most effective of the 5-HT3 antagonists in controlling delayed CINV nausea and vomiting that appear more than 24 hours after the first dose of a course of chemotherapy and is the only drug of its class approved for this use by the U.S. Food and Drug Administration. As of 2008, it is the most recent 5-HT3 antagonist to enter clinical use.

Struktur Molekul 2D

Berat 296.414
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Approximately 40 hours
Volume Distribusi * 8.3 ± 2.5 L/kg
Klirens (Clearance) * 160 +/- 35 mL/h/kg

Absorpsi

Low oral bioavailability.

Metabolisme

Hepatic (50%), primarily CYP2D6-mediated, although CYP3A4 and CYP1A2 are also involved.

Rute Eliminasi

After a single intravenous dose of 10 mcg/kg 14C-palonosetron, approximately 80% of the dose was recovered within 144 hours in the urine

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1543 Data
Buprenorphine Palonosetron 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 Palonosetron.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Palonosetron.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Palonosetron.
Hydrocodone Palonosetron 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 Palonosetron.
Magnesium sulfate The therapeutic efficacy of Palonosetron can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Palonosetron may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Palonosetron.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Palonosetron.
Orphenadrine Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Palonosetron 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 Palonosetron.
Pramipexole Palonosetron may increase the sedative activities of Pramipexole.
Ropinirole Palonosetron may increase the sedative activities of Ropinirole.
Rotigotine Palonosetron may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Palonosetron.
Sodium oxybate Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Palonosetron 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 Palonosetron.
Thalidomide Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Palonosetron 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 Palonosetron.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Palonosetron.
Dicoumarol The risk or severity of adverse effects can be increased when Palonosetron is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Palonosetron is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Palonosetron is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Palonosetron is combined with Tioclomarol.
Phenprocoumon The risk or severity of adverse effects can be increased when Palonosetron is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Palonosetron is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Palonosetron is combined with 4-hydroxycoumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Palonosetron is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Palonosetron is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Palonosetron is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Palonosetron is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Palonosetron is combined with Diphenadione.
(S)-Warfarin The risk or severity of adverse effects can be increased when Palonosetron is combined with (S)-Warfarin.
Mirabegron The serum concentration of Palonosetron can be increased when it is combined with Mirabegron.
Mirtazapine Palonosetron may increase the serotonergic activities of Mirtazapine.
Ethanol Palonosetron may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Palonosetron 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 Palonosetron.
Citalopram The risk or severity of adverse effects can be increased when Palonosetron is combined with Citalopram.
Sertraline The risk or severity of adverse effects can be increased when Palonosetron is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Palonosetron is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Palonosetron is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Palonosetron is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Palonosetron is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Palonosetron.
Seproxetine The risk or severity of adverse effects can be increased when Palonosetron is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Palonosetron is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Palonosetron is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Palonosetron is combined with Alaproclate.
Methylene blue Palonosetron may increase the serotonergic activities of Methylene blue.
Trospium The metabolism of Palonosetron can be decreased when combined with Trospium.
Solifenacin The metabolism of Solifenacin can be decreased when combined with Palonosetron.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Palonosetron.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Palonosetron.
Benzatropine Benzatropine may decrease the excretion rate of Palonosetron which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Palonosetron which could result in a higher serum level.
Lamotrigine The risk or severity of CNS depression can be increased when Palonosetron is combined with Lamotrigine.
Propantheline Palonosetron may decrease the excretion rate of Propantheline which could result in a higher serum level.
Dicyclomine Palonosetron may decrease the excretion rate of Dicyclomine which could result in a higher serum level.
Maprotiline The risk or severity of CNS depression can be increased when Palonosetron is combined with Maprotiline.
Tolterodine Palonosetron may decrease the excretion rate of Tolterodine which could result in a higher serum level.
Promethazine The risk or severity of CNS depression can be increased when Palonosetron is combined with Promethazine.
Doxacurium The risk or severity of CNS depression can be increased when Palonosetron is combined with Doxacurium.
Flavoxate Palonosetron may decrease the excretion rate of Flavoxate which could result in a higher serum level.
Tiotropium Palonosetron may decrease the excretion rate of Tiotropium which could result in a higher serum level.
Fesoterodine Palonosetron may decrease the excretion rate of Fesoterodine which could result in a higher serum level.
Aclidinium Palonosetron may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Palonosetron may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Palonosetron may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Palonosetron may decrease the excretion rate of Propiverine which could result in a higher serum level.
Quetiapine The risk or severity of CNS depression can be increased when Palonosetron is combined with Quetiapine.
Doxepin The risk or severity of CNS depression can be increased when Palonosetron is combined with Doxepin.
Zopiclone The risk or severity of adverse effects can be increased when Palonosetron is combined with Zopiclone.
Fluvoxamine The metabolism of Palonosetron can be decreased when combined with Fluvoxamine.
Duloxetine The metabolism of Palonosetron can be decreased when combined with Duloxetine.
Ritanserin The metabolism of Palonosetron can be decreased when combined with Ritanserin.
Venlafaxine The risk or severity of serotonin syndrome can be increased when Palonosetron is combined with Venlafaxine.
Tranylcypromine The metabolism of Palonosetron can be decreased when combined with Tranylcypromine.
Vilazodone The metabolism of Palonosetron can be decreased when combined with Vilazodone.
Tegaserod The metabolism of Palonosetron can be decreased when combined with Tegaserod.
Celecoxib The metabolism of Palonosetron can be decreased when combined with Celecoxib.
Metoprolol The metabolism of Palonosetron can be decreased when combined with Metoprolol.
Clobazam The serum concentration of Palonosetron can be increased when it is combined with Clobazam.
Clozapine The serum concentration of Palonosetron can be increased when it is combined with Clozapine.
Chlorpromazine The metabolism of Palonosetron can be decreased when combined with Chlorpromazine.
Cimetidine Palonosetron may decrease the excretion rate of Cimetidine which could result in a higher serum level.
Chloroquine The metabolism of Palonosetron can be decreased when combined with Chloroquine.
Nicardipine The metabolism of Palonosetron can be decreased when combined with Nicardipine.
Primaquine The metabolism of Palonosetron can be decreased when combined with Primaquine.
Fusidic acid The metabolism of Palonosetron can be decreased when combined with Fusidic acid.
Cholecalciferol The metabolism of Palonosetron can be decreased when combined with Cholecalciferol.
Perhexiline The metabolism of Palonosetron can be decreased when combined with Perhexiline.
Abiraterone The metabolism of Palonosetron can be decreased when combined with Abiraterone.
Panobinostat The metabolism of Palonosetron can be decreased when combined with Panobinostat.
Sulfaphenazole The metabolism of Palonosetron can be decreased when combined with Sulfaphenazole.

Target Protein

5-hydroxytryptamine receptor 3A HTR3A

Referensi & Sumber

Synthesis reference: Pierluigi Rossetto, Peter MacDonald, Ettore Bigatti, Gaia Banfi, Dario Tentorio, "Processes for preparing palonosetron salts." U.S. Patent US20080200681, issued August 21, 2008.
Artikel (PubMed)
  • PMID: 17106506
    De Leon A: Palonosetron (Aloxi): a second-generation 5-HT(3) receptor antagonist for chemotherapy-induced nausea and vomiting. Proc (Bayl Univ Med Cent). 2006 Oct;19(4):413-6.
  • PMID: 15102873
    Stoltz R, Cyong JC, Shah A, Parisi S: Pharmacokinetic and safety evaluation of palonosetron, a 5-hydroxytryptamine-3 receptor antagonist, in U.S. and Japanese healthy subjects. J Clin Pharmacol. 2004 May;44(5):520-31.
  • PMID: 16163194
    Rubenstein EB: Palonosetron: a unique 5-HT3 receptor antagonist indicated for the prevention of acute and delayed chemotherapy-induced nausea and vomiting. Clin Adv Hematol Oncol. 2004 May;2(5):284-9.
  • PMID: 19852528
    Yang LP, Scott LJ: Palonosetron: in the prevention of nausea and vomiting. Drugs. 2009 Nov 12;69(16):2257-78. doi: 10.2165/11200980-000000000-00000.
  • PMID: 15139789
    Siddiqui MA, Scott LJ: Palonosetron. Drugs. 2004;64(10):1125-32; discussion 1133-4.
  • PMID: 14760130
    Eisenberg P, MacKintosh FR, Ritch P, Cornett PA, Macciocchi A: Efficacy, safety and pharmacokinetics of palonosetron in patients receiving highly emetogenic cisplatin-based chemotherapy: a dose-ranging clinical study. Ann Oncol. 2004 Feb;15(2):330-7.
  • PMID: 15378559
    Stoltz R, Parisi S, Shah A, Macciocchi A: Pharmacokinetics, metabolism and excretion of intravenous l4C-palonosetron in healthy human volunteers. Biopharm Drug Dispos. 2004 Nov;25(8):329-37.

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