Alosetron
Alosetron Uses, Dosage, Side Effects, Food Interaction and all others data.
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 Alosetron was voluntarily withdrawn from the US market in November 2000 by the manufacturer due to numerous reports of severe adverse effects including ischemic colitis, severely obstructed or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.
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 IBS.
Trade Name | Alosetron |
Availability | Prescription only |
Generic | Alosetron |
Alosetron Other Names | Alosetron |
Related Drugs | dicyclomine, Bentyl, hyoscyamine, Amitiza, Metamucil, Lotronex |
Weight | 0.5mg, 1mg |
Type | Oral tablet |
Formula | C17H18N4O |
Weight | Average: 294.351 Monoisotopic: 294.148061218 |
Protein binding | 82% |
Groups | Approved, Withdrawn |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alosetron is a 5-HT3 antagonist used to treat diarrhea-predominant IBS.
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 also used to associated treatment for these conditions: Severe Diarrhea predominant irritable bowel syndrome
How Alosetron works
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 affect the regulation of visceral pain, colonic transit and gastrointestinal secretions, processes that relate to the pathophysiology of irritable bowel syndrome (IBS). 5-HT3 receptor antagonists such as alosetron inhibit activation of non-selective cation channels which results in the modulation of serotonin-sensitive GI motor and sensory processes.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Alosetron Drug Interaction
Unknown: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, meperidine, meperidine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, atropine / diphenoxylate, atropine / diphenoxylate, valacyclovir, valacyclovir, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol, ondansetron, ondansetron, cetirizine, cetirizine
Alosetron Disease Interaction
Major: gastrointestinal complications, hepatic impairment, thrombotic disordersModerate: renal impairment
Volume of Distribution
- 65 to 95 L
Elimination Route
50-60 %
Half Life
1.5 hours
Clearance
- 600 mL/min
Elimination Route
Renal elimination of unchanged alosetron accounts for only 6% of the dose. Alosetron is extensively metabolized in humans.
Innovators Monograph
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