Adult Dosing

Diarrhea-predominant irritable bowel syndrome

• Initial dose: 0.5 mg PO twice daily for 4 wks; hold if constipation occurs then resume again with 0.5 mg PO daily when constipation resolves [Max: 2 mg/day]
• For adequate control of IBS symptoms after 4 wks of treatment: 1 mg PO bid

Restricted Use in the United States

• Restricted Distribution; call 1-888-423-5227 or www.lotronex.com for more info
• REMS program

Pediatric Dosing

• Safety and effectiveness in pediatric patients have not been established

[Outline]

• Adult Dosing
• Pediatric Dosing

• Treatment of severe diarrhea-predominant irritable bowel syndrome (IBS) in women who have failed conventional therapy

• Hypersensitivity to alosetron or any of the ingredients of the product
• Constipation
• History of severe hepatic impairment
• History of chronic or severe constipation or sequelae from constipation
• History of intestinal obstruction and stricture
• History of toxic megacolon
• History of gastrointestinal perforation and adhesions
• History of ischemic colitis
• History of impaired intestinal circulation
• History of thrombophlebitis or hypercoagulable state
• History of Crohn’s disease or ulcerative colitis
• History of diverticulitis
• Patients unable to comply with patient-physician agreement
• Concomitant use of strong inhibitor of CYP1A2

• Use of alosetron have reported infrequent but serious gastrointestinal adverse reactions including ischemic colitis and serious complications of constipation have resulted in hospitalization, blood transfusion, surgery, and death
• Therapy is only for women with severe diarrhea-predominant irritable bowel syndrome (IBS) who have not responded adequately to conventional therapy Patient must read and sign the patient acknowledgement form for alosetron before receiving the initial prescription of alosetron
• Immediately discontinue the treatment if constipation or symptoms of ischemic colitis develop. Patients should immediately report constipation or symptoms of ischemic colitis to their physician even after discontinuation of treatment. The treatment should be resume when constipation resolves only on the advice of their treating physician
• Prescribing program for alosetron was implemented to help reduce the risks of serious gastrointestinal adverse reactions. Only physicians who have enrolled in the prometheus prescribing program for alosetron, based on their understanding of the benefits and risks, should prescribe alosetron

Renal Dose Adjustment

• Renal impairment: No dose adjustments defined

Hepatic Dose Adjustment

• Mild to moderate hepatic impairment: Caution advised
• Several hepatic impairment: Contraindicated

See Supplemental Patient Information

• Use of alosetron have reported infrequent but serious gastrointestinal adverse reactions including ischemic colitis and serious complications of constipation have resulted in hospitalization, blood transfusion, surgery, and death [US Black Box Warning]
• Prescribing program for alosetron was implemented to help reduce the risks of serious gastrointestinal adverse reactions. Only physicians who have enrolled in the Prometheus Prescribing Program for alosetron should prescribe alosetron [US Black Box Warning]
• Patients have experienced serious complications from constipation including obstruction, ileus, impaction, toxic megacolon, and secondary bowel ischemia, some patients have reported constipation and ischemic colitis with use of 1 mg twice daily and with lower doses
• Serious complications of constipation risk is increased in patients who are elderly, debilitated, or taking medications that decrease bowel motility
• Discontinue the treatment immediately in patients with signs of ischemic colitis such as rectal bleeding, bloody diarrhea, worsening of abdominal pain. Ischemic colitis can be life-threatening, patients with signs or symptoms of ischemic colitis should be evaluated for diagnostic test

Cautions: Use cautiously in

• Mild-moderate hepatic impairment
• Elderly and debilitated patients
• Concomitant use of medications that reduce GI motility

Supplemental Patient Information

• Physician should counsel and educate patients for risks and benefits of alosetron
• Physician should give patient a copy of medication guide and instruct them to read it carefully and review the patient acknowledgement form and give a copy of the signed patient acknowledgement form to the patient
• Advise patient not to initiate therapy or stop therapy if they are constipated

Pregnancy Category:B

Breastfeeding: Safety unknown; use with caution.

• GI: Constipation, ischemic colitis, toxic megacolon, ileus, gastrointestinal obstruction, diverticulitis, ulcerative colitis, abdominal pain, nausea, vomiting, abdominal distension, regurgitation and reflux, hemorrhoids, flatulence
• GU: Urinary tract infection
• MUSC: Abdominal discomfort pain, muscle pain

• 5-HT3 receptor antagonist; inhibit activation of non-selective cation channels, resulting modulation of enteric nervous system
• Extensively metabolized by liver; CYP450: 1A2 (10%), 2C9 (30%), 3A4 (18%) substrate
• Renally excreted: 74%, feces 24% (1% unchanged)
• Half-life: 1.5 hrs

US Trade Name(s)

• Lotronex

US Availability

Lotronex

• TABS: 0.5, 1 mg

Canadian Trade Name(s)

• N/A

Canadian Availability

• N/A

UK Trade Name(s)

• N/A

UK Availability

• N/A

Australian Trade Name(s)

• N/A

Australian Availability

• N/A

[Outline]

Gastrointestinal

Functional Bowel Disorder Agents

Serotoninergic Neuroenteric Modulators

Pricing data from www.DrugStore.com in U.S.A.

• Lotronex 1 MG TABS [Bottle] (PROMETHEUS)
  30 mg = $700.89
  90 mg = $2040.67
• Lotronex 0.5 MG TABS [Bottle] (PROMETHEUS)
  30 mg = $472.03
  90 mg = $1374.18

Warning: This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.

• Lotronex 0.5 MG Oral Tablet (Prometheus Laboratories Inc.)
• Lotronex 0.5 MG Oral Tablet (Prometheus)
• Lotronex 1 MG Oral Tablet (Prometheus Laboratories Inc.)
• Lotronex 1 MG Oral Tablet (Prometheus)