Alosetron

DB00969

small molecule approved withdrawn

Deskripsi

Alosetron is a 5-HT3 antagonist used only for the management of severe diarrhoea-predominant irritable bowel syndrome (IBS) in women. Alosetron has an antagonist action on the 5-HT3 receptors and thus may modulate serotonin-sensitive gastrointestinal (GI) processes. Alosetron was voluntarily withdrawn from the US market in November 2000 by the manufacturer due to numerous reports of severe adverse effects including ischemic colitis, severely obstructed or ruptured bowel, and death. In June 2002, the FDA approved a supplemental new drug application allowing the remarketing of the drug under restricted conditions of use.

Struktur Molekul 2D

Berat 294.351
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1.5 hours
Volume Distribusi * 65 to 95 L
Klirens (Clearance) * 600 mL/min

Absorpsi

50-60 %

Metabolisme

Hepatic, via microsomal cytochrome P450 (CYP)

Rute Eliminasi

Renal elimination of unchanged alosetron accounts for only 6% of the dose. Alosetron is extensively metabolized in humans.

Interaksi Makanan

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

Interaksi Obat

1137 Data
Fluvoxamine The metabolism of Alosetron can be decreased when combined with Fluvoxamine.
Deferasirox The serum concentration of Alosetron can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Alosetron can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Alosetron can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Alosetron can be decreased when it is combined with Teriflunomide.
Buprenorphine Alosetron 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 Alosetron.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Alosetron.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Alosetron.
Hydrocodone Alosetron 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 Alosetron.
Magnesium sulfate The therapeutic efficacy of Alosetron can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Alosetron may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Alosetron may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Alosetron.
Mirtazapine Alosetron 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 Alosetron.
Orphenadrine Alosetron may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Alosetron 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 Alosetron.
Pramipexole Alosetron may increase the sedative activities of Pramipexole.
Rotigotine Alosetron may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Alosetron.
Sodium oxybate Alosetron may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Alosetron 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 Alosetron.
Thalidomide Alosetron may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Alosetron may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Alosetron.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Alosetron.
Phenindione The risk or severity of adverse effects can be increased when Alosetron is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Alosetron is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Alosetron is combined with Tioclomarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Alosetron is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Alosetron is combined with Ethyl biscoumacetate.
Clorindione The risk or severity of adverse effects can be increased when Alosetron is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Alosetron is combined with Diphenadione.
Agomelatine The serum concentration of Agomelatine can be increased when it is combined with Alosetron.
Pirfenidone The metabolism of Pirfenidone can be decreased when combined with Alosetron.
Tizanidine The serum concentration of Tizanidine can be increased when it is combined with Alosetron.
Abiraterone The serum concentration of Alosetron can be increased when it is combined with Abiraterone.
Eluxadoline Alosetron may increase the constipating activities of Eluxadoline.
Cyproterone acetate The metabolism of Alosetron can be increased when combined with Cyproterone acetate.
Ethanol Alosetron may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Alosetron 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 Alosetron.
Citalopram The risk or severity of adverse effects can be increased when Alosetron is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Alosetron is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Alosetron is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Alosetron is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Alosetron is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Alosetron is combined with Sibutramine.
Escitalopram The risk or severity of adverse effects can be increased when Alosetron is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Alosetron is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Alosetron is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Alosetron is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Alosetron is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Alosetron is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Alosetron is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Alosetron is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Alosetron is combined with Alaproclate.
Tolterodine The metabolism of Tolterodine can be decreased when combined with Alosetron.
Quetiapine The risk or severity of CNS depression can be increased when Alosetron is combined with Quetiapine.
Amitriptyline The metabolism of Amitriptyline can be decreased when combined with Alosetron.
Doxepin The metabolism of Doxepin can be decreased when combined with Alosetron.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Alosetron.
Desipramine The risk or severity of CNS depression can be increased when Alosetron is combined with Desipramine.
Zopiclone The risk or severity of adverse effects can be increased when Alosetron is combined with Zopiclone.
Albendazole The metabolism of Alosetron can be increased when combined with Albendazole.
Carbamazepine The metabolism of Alosetron can be increased when combined with Carbamazepine.
Primidone The metabolism of Alosetron can be increased when combined with Primidone.
Rifampin The metabolism of Alosetron can be increased when combined with Rifampicin.
Mefenamic acid The metabolism of Mefenamic acid can be decreased when combined with Alosetron.
Bortezomib The metabolism of Bortezomib can be decreased when combined with Alosetron.
Caffeine The metabolism of Alosetron can be decreased when combined with Caffeine.
Moxifloxacin The metabolism of Alosetron can be decreased when combined with Moxifloxacin.
Lidocaine The metabolism of Alosetron can be decreased when combined with Lidocaine.
Mexiletine The metabolism of Alosetron can be decreased when combined with Mexiletine.
Betaxolol The metabolism of Betaxolol can be decreased when combined with Alosetron.
Carmustine The metabolism of Carmustine can be decreased when combined with Alosetron.
Disopyramide The metabolism of Disopyramide can be decreased when combined with Alosetron.
Conjugated estrogens The metabolism of Conjugated estrogens can be decreased when combined with Alosetron.
Ropivacaine The metabolism of Ropivacaine can be decreased when combined with Alosetron.
Olanzapine The metabolism of Olanzapine can be decreased when combined with Alosetron.
Chlorzoxazone The metabolism of Chlorzoxazone can be decreased when combined with Alosetron.
Clozapine The metabolism of Alosetron can be decreased when combined with Clozapine.
Grepafloxacin The metabolism of Grepafloxacin can be decreased when combined with Alosetron.
Tacrine The metabolism of Tacrine can be decreased when combined with Alosetron.
Triamterene The metabolism of Triamterene can be decreased when combined with Alosetron.
Entecavir The metabolism of Entecavir can be decreased when combined with Alosetron.
Nabumetone The metabolism of Nabumetone can be decreased when combined with Alosetron.
Quinine The metabolism of Quinine can be decreased when combined with Alosetron.
Chlorpromazine The metabolism of Chlorpromazine can be decreased when combined with Alosetron.
Flutamide The metabolism of Flutamide can be decreased when combined with Alosetron.
Cinnarizine The metabolism of Cinnarizine can be decreased when combined with Alosetron.
Propranolol The metabolism of Propranolol can be decreased when combined with Alosetron.
Diclofenac The metabolism of Diclofenac can be decreased when combined with Alosetron.
Imatinib The metabolism of Imatinib can be decreased when combined with Alosetron.
Guanabenz The metabolism of Guanabenz can be decreased when combined with Alosetron.
Pemetrexed The metabolism of Pemetrexed can be decreased when combined with Alosetron.

Target Protein

5-hydroxytryptamine receptor 3A HTR3A

Referensi & Sumber

Synthesis reference: Buchi Reddy REGURI, Sampathkumar UPPARAPALLI, Nilam SAHU, Karunakara Rao JAVVAJI, Brahma Reddy GADE, "PROCESS FOR THE PREPARATION OF ALOSETRON." U.S. Patent US20120178937, issued July 12, 2012.
Artikel (PubMed)
  • PMID: 15061683
    Andresen V, Hollerbach S: Reassessing the benefits and risks of alosetron: what is its place in the treatment of irritable bowel syndrome? Drug Saf. 2004;27(5):283-92.
  • PMID: 11060667
    Camilleri M: Pharmacology and clinical experience with alosetron. Expert Opin Investig Drugs. 2000 Jan;9(1):147-59.
  • PMID: 14596662
    Mayer EA, Bradesi S: Alosetron and irritable bowel syndrome. Expert Opin Pharmacother. 2003 Nov;4(11):2089-98.
  • PMID: 18555935
    Rahimi R, Nikfar S, Abdollahi M: Efficacy and tolerability of alosetron for the treatment of irritable bowel syndrome in women and men: a meta-analysis of eight randomized, placebo-controlled, 12-week trials. Clin Ther. 2008 May;30(5):884-901. doi: 10.1016/j.clinthera.2008.05.002.
  • PMID: 20136586
    Lewis JH: Alosetron for severe diarrhea-predominant irritable bowel syndrome: safety and efficacy in perspective. Expert Rev Gastroenterol Hepatol. 2010 Feb;4(1):13-29. doi: 10.1586/egh.09.72.

Contoh Produk & Brand

Produk: 24 • International brands: 0
Produk
  • Alosetron
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Alosetron
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Alosetron
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
  • Alosetron
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Alosetron Hydrochloride
    Tablet, film coated • 0.5 mg/1 • Oral • US • Generic • Approved
  • Alosetron Hydrochloride
    Tablet, film coated • 1 mg/1 • Oral • US • Generic • Approved
  • Alosetron Hydrochloride
    Tablet • 0.5 mg/1 • Oral • US • Generic • Approved
  • Alosetron Hydrochloride
    Tablet • 1 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 24 produk.

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