Peringatan Keamanan

LD50: 265 mg/kg (Rat, oral).

Tropisetron

DB11699

small molecule approved investigational

Deskripsi

Tropisetron is an indole derivative with antiemetic activity. As a selective serotonin receptor antagonist, tropisetron competitively blocks the action of serotonin at 5HT3 receptors, resulting in suppression of chemotherapy- and radiotherapy-induced nausea and vomiting.

Tropisetron appears to be well tolerated with the most frequently reported adverse effect being headache. Extrapyramidal side effects are rare upon using tropisetron.

Struktur Molekul 2D

Berat 284.3529
Wujud -

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 5.7 h.
Volume Distribusi 400-600 L.
Klirens (Clearance) 1800 ml/min.

Absorpsi

The absorption of tropisetron from the gastrointestinal tract is rapid (mean half-life of about 20 minutes) and nearly complete (more than 95%). Due to first-pass metabolism in the liver, the absolute bioavailability of a 5 mg oral dose is 60%. The peak plasma concentration is attained within three hours.

Metabolisme

The metabolism of tropisetron occurs by hydroxylation at the 5, 6 or 7 positions of its indole ring, followed by a conjugation reaction to the glucuronide or sulphate with excretion in the urine or bile (urine to faeces ratio 5:1). The metabolites have a greatly reduced potency for the 5-HT3 receptor and do not contribute to the pharmacological action of the drug.

Rute Eliminasi

About 8% of tropisetron is excreted in the urine as unchanged drug, 70% as metabolites; 15% is excreted in the feces.

Interaksi Makanan

1 Data
  • 1. Avoid alcohol.

Interaksi Obat

1413 Data
Buprenorphine Tropisetron 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 Tropisetron.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Tropisetron.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Tropisetron.
Hydrocodone Tropisetron 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 Tropisetron.
Magnesium sulfate The therapeutic efficacy of Tropisetron can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Tropisetron may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Tropisetron may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Tropisetron.
Mirtazapine Tropisetron 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 Tropisetron.
Orphenadrine Tropisetron may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Tropisetron 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 Tropisetron.
Pramipexole Tropisetron may increase the sedative activities of Pramipexole.
Ropinirole Tropisetron may increase the sedative activities of Ropinirole.
Rotigotine Tropisetron may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Tropisetron.
Sodium oxybate Tropisetron may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Tropisetron 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 Tropisetron.
Thalidomide Tropisetron may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Tropisetron 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 Tropisetron.
Dicoumarol The risk or severity of adverse effects can be increased when Tropisetron is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Tropisetron is combined with Phenindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Tropisetron is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Tropisetron is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Tropisetron is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Tropisetron is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Tropisetron is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Tropisetron is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Tropisetron is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Tropisetron is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Tropisetron is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Tropisetron is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Tropisetron is combined with (S)-Warfarin.
Ethanol Tropisetron may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Tropisetron 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 Tropisetron.
Fluvoxamine The risk or severity of adverse effects can be increased when Tropisetron is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Tropisetron is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Tropisetron is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Tropisetron is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Tropisetron is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Tropisetron is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Tropisetron is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Tropisetron is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Tropisetron is combined with Escitalopram.
Zimelidine The risk or severity of adverse effects can be increased when Tropisetron is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Tropisetron is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Tropisetron is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Tropisetron is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Tropisetron is combined with Seproxetine.
Levomilnacipran Levomilnacipran may decrease the excretion rate of Tropisetron which could result in a higher serum level.
Indalpine The risk or severity of adverse effects can be increased when Tropisetron is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Tropisetron is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Tropisetron is combined with Alaproclate.
Esmolol Esmolol may increase the arrhythmogenic activities of Tropisetron.
Betaxolol Betaxolol may increase the arrhythmogenic activities of Tropisetron.
Dofetilide Dofetilide may increase the arrhythmogenic activities of Tropisetron.
Lidocaine Lidocaine may increase the arrhythmogenic activities of Tropisetron.
Atenolol Atenolol may increase the arrhythmogenic activities of Tropisetron.
Diltiazem Diltiazem may increase the arrhythmogenic activities of Tropisetron.
Mexiletine Mexiletine may increase the arrhythmogenic activities of Tropisetron.
Amlodipine Amlodipine may increase the arrhythmogenic activities of Tropisetron.
Nimodipine Nimodipine may increase the arrhythmogenic activities of Tropisetron.
Sotalol Sotalol may increase the arrhythmogenic activities of Tropisetron.
Acetyldigitoxin Acetyldigitoxin may increase the arrhythmogenic activities of Tropisetron.
Lercanidipine Lercanidipine may increase the arrhythmogenic activities of Tropisetron.
Cinnarizine Cinnarizine may increase the arrhythmogenic activities of Tropisetron.
Adenosine Adenosine may increase the arrhythmogenic activities of Tropisetron.
Losartan Losartan may increase the arrhythmogenic activities of Tropisetron.
Levomenthol Levomenthol may increase the arrhythmogenic activities of Tropisetron.
Loperamide Loperamide may increase the arrhythmogenic activities of Tropisetron.
Levosimendan Levosimendan may increase the arrhythmogenic activities of Tropisetron.
Felodipine Felodipine may increase the arrhythmogenic activities of Tropisetron.
Nitrendipine Nitrendipine may increase the arrhythmogenic activities of Tropisetron.
Tocainide Tocainide may increase the arrhythmogenic activities of Tropisetron.
Perhexiline Perhexiline may increase the arrhythmogenic activities of Tropisetron.
Deslanoside Deslanoside may increase the arrhythmogenic activities of Tropisetron.
Carvedilol Carvedilol may increase the arrhythmogenic activities of Tropisetron.
Bretylium Bretylium may increase the arrhythmogenic activities of Tropisetron.
Propafenone Propafenone may increase the arrhythmogenic activities of Tropisetron.
Acebutolol Acebutolol may increase the arrhythmogenic activities of Tropisetron.
Flecainide Flecainide may increase the arrhythmogenic activities of Tropisetron.
Encainide Encainide may increase the arrhythmogenic activities of Tropisetron.
Bepridil Bepridil may increase the arrhythmogenic activities of Tropisetron.
Practolol Practolol may increase the arrhythmogenic activities of Tropisetron.
Mibefradil Mibefradil may increase the arrhythmogenic activities of Tropisetron.
Digitoxin Digitoxin may increase the arrhythmogenic activities of Tropisetron.
Ajmaline Ajmaline may increase the arrhythmogenic activities of Tropisetron.
Aprindine Aprindine may increase the arrhythmogenic activities of Tropisetron.
Dexpropranolol Dexpropranolol may increase the arrhythmogenic activities of Tropisetron.
Prenylamine Prenylamine may increase the arrhythmogenic activities of Tropisetron.
Cyclandelate Cyclandelate may increase the arrhythmogenic activities of Tropisetron.
Celiprolol Celiprolol may increase the arrhythmogenic activities of Tropisetron.
Dronedarone Dronedarone may increase the arrhythmogenic activities of Tropisetron.
Nebivolol Nebivolol may increase the arrhythmogenic activities of Tropisetron.

Target Protein

5-hydroxytryptamine receptor 3A HTR3A

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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