Alosetron Hcl (alosetron HCl)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Alosetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptors, and thus may modulate serotonin-sensitive GI processes.
Alosetron is a selective inhibitor of type 3 serotonergic (5-HT3) receptors that is structurally related to other 5-HT3 receptor inhibitors (e.g., granisetron, ondansetron). The 5-HT3 receptors are nonselective cation channels that are widely distributed on enteric neurons within the GI tract and other peripheral and central sites. Activation of these receptors and the resulting neuronal depolarization affect regulation of visceral pain, colonic transit, and GI secretion processes related to the pathophysiology of irritable bowel syndrome (IBS).
Alosetron inhibits the activation of 5-HT3 receptors, and thus may modulate serotonin-sensitive GI motor and sensory processes. Alosetron has not been evaluated as an antiemetic in humans; limited data from a single animal study indicate that the drug may have antiemetic activity.
Alosetron is extensively metabolized via the cytochrome P-450 (CYP) system, principally by CYP isoenzyme 1A2, and to a lesser extent by CYP 2C9 and 3A4. Several circulating metabolites of alosetron have been identified in humans; these metabolites are present in low concentrations (no more than 15% of the concentration of unchanged alosetron) and are unlikely to contribute to the pharmacologic activity of the drug. Approximately 13 and 1% of an oral dose of alosetron is excreted in urine and feces, respectively, as unchanged drug.
USES: Alosetron is used to treat women with severe irritable bowel syndrome (IBS) who have diarrhea as the main problem. It is not a cure, but it may help to decrease abdominal pain, sudden urges to have a bowel movement, and diarrhea. This medication is not recommended for use by children because of the serious side effects that have been seen in adults.
Generic name: alosetron HCl
Pronunciation: (al-OH-se-tron)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Alosetron Hcl
Indications
The following indications are listed for Alosetron Hcl:
- Diarrhea Predominant Irritable Bowel Syndrome
Also known as: Diarrhea Predominant Ibs, Diarrhea Predominant Spastic Colon.
Dosing
Dosage of alosetron hydrochloride is expressed in terms of alosetron.
For the treatment of severe diarrhea-predominant irritable bowel syndrome (IBS) in women, the recommended initial dosage of alosetron is 0.5 mg twice daily. Data from a dose-ranging study indicate that risk of constipation is reduced with this dosage compared with a dosage of 1 mg twice daily; however, efficacy of the 0.5-mg twice-daily dosage in women with severe diarrhea-predominant IBS has not been adequately evaluated in clinical studies. If constipation occurs at a dosage of 0.5 mg twice daily, therapy should be withheld until constipation resolves; upon resolution, alosetron may be reinitiated at a reduced dosage of 0.5 mg once daily. If constipation recurs at a dosage of 0.5 mg once daily, treatment with alosetron should be immediately discontinued.
Patients may continue receiving an alosetron dosage of 0.5 mg once or twice daily as maintenance therapy if the dosage is well tolerated and symptoms of IBS are adequately controlled. If the patient tolerates but does not respond adequately to the dosage after 4 weeks, dosage may be increased up to 1 mg twice daily. If adequate control of symptoms is not achieved after 4 weeks of treatment on a dosage of 1 mg twice daily, alosetron therapy should be discontinued.
Alosetron should be discontinued immediately and permanently in patients who develop ischemic colitis. (See Ischemic Colitis under Warnings/Precautions: Warnings, in Cautions.)
If a dose of alosetron is missed, the dose should be skipped and the next dose should be taken at the regularly scheduled time. A double dose should not be taken to make up for the missed dose.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Current constipation, history of chronic or severe constipation, or history of complications related to constipation. History of intestinal obstruction, stricture, toxic megacolon, GI perforation, and/or adhesions. History of ischemic colitis, impaired intestinal circulation, thrombophlebitis, or hypercoagulable state. History of Crohn's disease, ulcerative colitis, or diverticulitis.
History of severe hepatic impairment.
Concomitant use of fluvoxamine. (See Drug Interactions: Fluvoxamine.)
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects occurring in 2% or more of patients with IBS receiving alosetron in clinical studies include constipation, abdominal discomfort or pain, nausea, GI discomfort or pain, abdominal distention, regurgitation and reflux, and hemorrhoids. In women with severe diarrhea-predominant IBS, diarrhea, hemorrhoidal hemorrhage, and flatulence also were reported in addition to the adverse effects observed in the general IBS population.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of alosetron have not been established in pediatric patients younger than 18 years of age. The drug is not recommended for use in the pediatric population because of the risk of serious GI complications.
Category B. (See Users Guide.) There are no adequate and well-controlled studies of alosetron in pregnant women; animal reproduction studies using alosetron doses up to 160-240 times the recommended human dose have not demonstrated any evidence of fetal harm. Alosetron should be used during pregnancy only if clearly needed.
Alosetron and/or its metabolites are distributed into milk in rats; it is not known whether alosetron is distributed into milk in humans. Caution is advised if the drug is administered in nursing women.
In some studies in healthy individuals, plasma concentrations of alosetron were increased by approximately 40% in those 65 years of age or older compared with younger adults.
Because of evidence suggesting that geriatric patients may be at greater risk for complications of constipation, alosetron should be used with caution and appropriate follow-up in such patients.
ICD codes
No ICD codes are available for this drug.
Formulary status
Search health-plan coverage for this drug by ZIP code.
Choose the first character of a health plan name.
Last reviewed · Source: First Databank (FDB) drug data
On this page
Actions
Sign in to save favorites
Saving this drug requires a free Physicians Office Resource account.