LOTRONEX Dosage & Rx Info | Uses, Side Effects

Lotronex Generic Name & Formulations

Legal Class

General Description

Alosetron (as HCl) 0.5mg, 1mg; tabs.

Pharmacological Class

5-HT₃ receptor antagonist.

How Supplied

Tabs—30

Manufacturer

Prometheus Labs, Inc.

Generic Availability

YES

Mechanism of Action

Alosetron is a potent and selective 5-HT₃ receptor antagonist. 5-HT₃ receptors are ligand-gated 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 IBS. 5-HT₃ receptor antagonists such as alosetron inhibit activation of non-selective cation channels, which results in the modulation of the enteric nervous system.

Lotronex Indications

Indications

For women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have chronic IBS symptoms (generally lasting 6 months or longer) and have had anatomic or biochemical abnormalities of the GI tract excluded, and not responded adequately to conventional therapy. Restricted to patients for whom the benefit-to-risk balance is most favorable.

Lotronex Dosage and Administration

Adult

Initially 0.5mg twice daily. May increase to 1mg twice daily after 4 weeks if starting dose is tolerated but inadequate. Discontinue if inadequate control of symptoms after 4 weeks of treatment at 1mg twice daily. If constipation occurs, discontinue until constipation resolves, then restart at 0.5mg once daily. If constipation recurs, discontinue immediately.

Children

Not recommended.

Lotronex Contraindications

Contraindications

Constipation. Intestinal obstruction, stricture. Toxic megacolon. GI perforation, and/or adhesions. Ischemic colitis. Impaired intestinal circulation. Thrombophlebitis. Hypercoagulable state. Crohn's disease. Ulcerative colitis. Diverticulitis. Severe hepatic impairment. Concomitant fluvoxamine.

Lotronex Boxed Warnings

Boxed Warning

Serious gastrointestinal adverse reactions.

Lotronex Warnings/Precautions

Warnings/Precautions

Discontinue immediately if constipation or symptoms of ischemic colitis develop; may resume if constipation resolves but not if ischemic colitis occurs. Hepatic impairment. Elderly. Debilitated. Pregnancy. Nursing mothers: monitor infants.

Lotronex Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal. Half-life: ~1.5 hours.

Lotronex Interactions

Interactions

See Contraindications. Avoid concomitant moderate CYP1A2 inhibitors (eg, quinolones, cimetidine). May be potentiated by strong CYP3A4 inhibitors (eg, ketoconazole, clarithromycin, telithromycin, protease inhibitors, voriconazole, itraconazole). Caution with drugs that decrease GI motility.

Lotronex Adverse Reactions

Adverse Reactions

Constipation, abdominal discomfort/pain, nausea, GI discomfort/pain; ischemic colitis, complications of constipation (may be serious).

Lotronex Clinical Trials

See Literature

Lotronex Note

Not Applicable

Lotronex Patient Counseling