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QuickView for Alosetron (compound)

Name: alosetron
PubChem Compound ID: 10335284
Molecular formula: C17H18N4O
Molecular weight: 306.306 g/mol
Name: alosetron
Name (isomeric): DB00969
Drug Type: small molecule
Alosetron HCl
Brand: Lotronex
Category: Serotonin Antagonists, Gastrointestinal Agents
CAS number: 122852-42-0
Indication: Only for the treatment of symptoms of severe diarrhea-predominant irritable bowel syndrome (IBS) in women with chronic symptoms (generally lasting greater than 6 months) who does not present with anatomic or biochemical GI abnormalities and have not responded to conventional therapy.
Alosetron is a potent and selective antagonist of the serotonin 5-HT3 receptor type. Activation of these receptors and the resulting neuronal depolarization affects the regulation of visceral pain, colonic transit, and GI secretions processes that are related to IBS. By blocking these receptors, alosetron is able to effectively control I...
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Mechanism of Action:
Alosetron is a potent and selective 5-HT3 receptor antagonist. 5-HT3 receptors are nonselective cation channels that are extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels and the resulting neuronal depolarization affec...
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Absorption: 50-60 %
Protein binding: 82%
Biotransformation: Hepatic, via microsomal cytochrome P450 (CYP)
Route of elimination: Renal elimination of unchanged alosetron accounts for only 6% of the dose. Alosetron is extensively metabolized in humans.
Half Life: 1.5 hours
Clearance: 600 mL/min
Affected organisms: Humans and other mammals
Food interaction:
Absorption is decreased by about 25% when taken with meals.
Take without regard to meals.
Drug interaction:
ThiabendazoleThe strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Alosetron by decreasing Alosetron metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Alosetron if Thiabendazole is initiated, discontinued or dose changed.