(a LOE se tron)
- Alosetron HCl
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Lotronex: 0.5 mg, 1 mg
Generic: 0.5 mg, 1 mg
Brand Names: U.S.
- Selective 5-HT3 Receptor Antagonist
Alosetron is a potent and selective antagonist of a subtype of the serotonin 5-HT3 receptor. 5-HT3 receptors are ligand-gated ion channels extensively distributed on enteric neurons in the human gastrointestinal tract, as well as other peripheral and central locations. Activation of these channels affect the regulation of visceral pain, colonic transit, and gastrointestinal secretions. In patients with irritable bowel syndrome, blockade of these channels may reduce pain, abdominal discomfort, urgency, and diarrhea.
Vd: 65 to 95 L
Extensive hepatic metabolism via CYP2C9, 3A4, and 1A2. Thirteen metabolites have been detected in the urine. Biological activity of these metabolites in unknown.
Urine (74%, 13% of total dose as unchanged drug); feces (11%, 1% of total dose as unchanged drug)
Time to Peak
Special Populations: Hepatic Function Impairment
Exposure to alosetron is increased.
Special Populations: Elderly
Plasma levels are elevated by about 40% in patients 65 years and older.
Special Populations: Gender
Plasma concentrations are 30% to 50% lower and less variable in men.
Use: Labeled Indications
Irritable bowel syndrome: Treatment of women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have chronic IBS symptoms (generally lasting 6 months or longer), have had anatomic or biochemical abnormalities of the GI tract excluded, and who have not responded adequately to conventional therapy.
Do not initiate in patients with constipation. History of chronic or severe constipation or sequelae from constipation; history of ischemic colitis, intestinal obstruction, stricture, toxic megacolon, GI perforation, adhesions, diverticulitis, Crohn disease, ulcerative colitis, history of severe hepatic impairment; history of impaired intestinal circulation, thrombophlebitis, or hypercoagulable state; coadministration with fluvoxamine.
Irritable bowel syndrome (IBS): Females: Oral: Initial: 0.5 mg twice daily for 4 week; if tolerated, but response is inadequate, may be increased after 4 weeks to 1 mg twice daily (maximum dose: 2 mg/day). If response is inadequate after 4 weeks of 1 mg twice-daily dosing, discontinue treatment.
Refer to adult dosing. Dosage adjustment is not required; however, postmarketing experience suggests that elderly patients may be at greater risk for complications of constipation.
Dosing: Renal Impairment
There are no dosage adjustments provided in the manufacturer’s labeling.
Dosing: Hepatic Impairment
Mild to moderate impairment (Child-Pugh class A or B): There are no dosage adjustments provided in the manufacturer’s labeling; use with caution due to extensive metabolism and increased drug exposure.
Severe impairment (Child-Pugh class C): Use is contraindicated.
Dosing: Adjustment for Toxicity
Constipation: Patients experiencing constipation with 0.5 mg twice daily should discontinue therapy until constipation resolves. Therapy may be reinitiated at 0.5 mg once daily. Discontinue immediately if constipation recurs at lower dose.
Ischemic colitis: Discontinue therapy immediately; do not restart
May be administered with or without food.
Store at 20°C to 25°C (68°F to 77°F). Protect from light and moisture.
Abiraterone Acetate: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy
Apomorphine: Antiemetics (5HT3 Antagonists) may enhance the hypotensive effect of Apomorphine. Avoid combination
CYP1A2 Inhibitors (Moderate): May increase the serum concentration of Alosetron. Avoid combination
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Alosetron. Monitor therapy
Eluxadoline: Alosetron may enhance the constipating effect of Eluxadoline. Avoid combination
FluvoxaMINE: May decrease the metabolism of Alosetron. Avoid combination
Obeticholic Acid: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy
Peginterferon Alfa-2b: May increase the serum concentration of CYP1A2 Substrates (High risk with Inhibitors). Monitor therapy
Serotonin Modulators: Antiemetics (5HT3 Antagonists) may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Exceptions: Nicergoline. Monitor therapy
Tapentadol: Antiemetics (5HT3 Antagonists) may diminish the analgesic effect of Tapentadol. Monitor therapy
TraMADol: Antiemetics (5HT3 Antagonists) may diminish the analgesic effect of TraMADol. Monitor therapy
>10%: Gastrointestinal: Constipation (9% to 29%; dose related)
1% to 10%:
Central nervous system: Fatigue (≥3%), headache (≥3%)
Gastrointestinal: Abdominal distress (≤1% to 7%), abdominal pain (≤1% to 7%), nausea (6%), gastrointestinal distress (≤5%), gastrointestinal pain (≤5%), gastroenteritis (≥3%), vomiting (≥3%), diarrhea (2% to 3%), flatulence (1% to 3%), hemorrhoids (1% to 3%), abdominal distention (2%), acid regurgitation (≤2%), gastroesophageal reflux disease (≤2%)
Genitourinary: Urinary tract infection (≥3%)
Neuromuscular & skeletal: Muscle spasm (≥3%)
Respiratory: Cough (≥3%), nasopharyngitis (≥3%), upper respiratory tract infection (≥3%)
<1%, postmarketing, and/or case reports: Abnormal bilirubin levels, abnormal erythrocytes, active gastrointestinal lesion, allergic skin reaction, alopecia, anxiety, cardiac arrhythmia, cholecystitis, cognitive dysfunction, colitis, confusion, cystitis, decreased gastrointestinal motility, depression, dermatitis, diaphoresis, disruption of body temperature regulation, disturbance in fluid balance, diverticulitis, drowsiness, dyspepsia, extrasystoles, fecal impaction, gastrointestinal obstruction, gastrointestinal perforation, gastrointestinal spasm, gastrointestinal ulcer, hematoma, hemoglobinopathy, hemorrhage, hepatitis, hyperacidity, hyperglycemia, hypertension, hypoesthesia, hypoglycemia, hypothalamic disease, intestinal obstruction, intussusception, ischemic colitis, memory impairment, mesenteric ischemia (small bowel), muscle cramps, muscle rigidity, myalgia, occult blood in stools, ostealgia, pain, pituitary insufficiency, proctitis, respiratory tract disease, sedation, sexual disorder, skeletal pain, skin rash, tachyarrhythmia, tremor, ulcerative colitis, urinary frequency, urticaria
Concerns related to adverse effects:
• Constipation: [US Boxed Warning]: Discontinue immediately in patients who develop constipation; infrequent but serious complications of constipation, have resulted in hospitalization, and rarely, blood transfusion, surgery, or death have been reported (obstruction, ileus, perforation [rare], impaction, toxic megacolon, secondary bowel ischemia). Constipation is a frequent, dose-related side effect; risk for complications from constipation may be increased in elderly, debilitated patients, or with concurrent use of other medications which decrease GI motility. Nonsevere constipation may be managed by temporarily interrupting therapy and decreasing the dose. Do not initiate in patients with constipation.
• Ischemic colitis: [US Boxed Warning]: Ischemic colitis has been reported during treatment without warning. Discontinue and evaluate immediately in patients who experience rectal bleeding, bloody diarrhea, or a sudden worsening of abdominal pain, and do not restart therapy if ischemic colitis is diagnosed.
• Hepatic impairment: Use caution in mild to moderate hepatic impairment (Child-Pugh class A or B) (extensively metabolized); contraindicated in severe impairment (Child-Pugh class C).
• Debilitated patients: Use with caution in debilitated patients due to increased risk of complications from constipation.
• Elderly: Use with caution in the elderly due to increased risk of complications from constipation.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
• Appropriate use: [US Boxed Warning]: Only indicated for women with severe diarrhea-predominant irritable bowel syndrome who have not responded adequately to conventional therapy who have chronic IBS symptoms (lasting ≥6 months) and are without anatomic or biochemical abnormalities of the GI tract. Severe diarrhea-predominant IBS includes at least one of the following: frequent and severe abdominal pain/discomfort, frequent bowel urgency or fecal incontinence, and disability or restriction of daily activities due to IBS.
Pregnancy Risk Factor
Adverse events have not been observed in animal reproduction studies. Alosetron should be used in pregnant women only if clearly needed.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience abdominal pain and nausea. Have patient report immediately to prescriber signs of gastrointestinal problems (constipation, new or severe abdominal pain, or blood in stools), bloating, mood changes, rectal bleeding, rectal pain, vomiting, or tachycardia (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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- Drug class: serotoninergic neuroenteric modulators
Other brands: Lotronex