OVERVIEW
- AMITIZA is the ONLY locally acting ClC-2 chloride channel activator1
- AMITIZA promotes fluid secretion into the intestinal lumen1
- In clinical studies, no clinically significant changes were seen in serum electrolyte levels1
SUGGESTED MECHANISM OF ACTION
THE ROLE OF CHLORIDE CHANNELS IN THE INTESTINAL TRACT
- Chloride channels are key regulators in the intestinal tract, actively transporting chloride ions into the lumen. Sodium ions and fluids passively follow2,3,4
- By regulating fluid absorption and secretion, chloride channels help regulate fluid balance5
- In clinical studies, no clinically significant changes were seen in serum electrolyte levels1
WHAT MAKES AMITIZA DIFFERENT?
- AMITIZA directly targets CIC-2 chloride channels via its mechanism of action (MOA),1 distinguishing it from osmotic laxatives
- AMITIZA promotes fluid secretion into the intestinal lumen1
The MOA of AMITIZA in IBS-C is not fully understood. However, ex vivo animal studies suggest that AMITIZA stimulates recovery of mucosal barrier function by restoring intestinal tight junction protein complexes.6 The role of tight junctions is also unclear.
PATIENTS TAKING AMITIZA MAY EXPERIENCE NAUSEA
If this occurs, concomitant administration of food with AMITIZA may reduce symptoms of nausea. Patients who experience severe nausea should inform their healthcare provider.
WATCH THE SUGGESTED MECHANISM OF ACTION
VIDEO FOR IBS-C
IN DEPTH
The mechanism of action of AMITIZA in IBS-C is not fully understood.
Tight junctions between cells act as gatekeepers for solutes and macromolecules passing between the apical and basolateral regions of the gut.6
Damaged or compromised tight junctions are associated with leaking of luminal contents through the mucosal barrier.6 The role of tight junctions in IBS-C is also unclear.
In ex vivo studies of ischemic porcine intestine, activation of ClC-2 chloride channels by AMITIZA has been shown to stimulate tight junction restoration and help recover intestinal barrier function.1
REFERENCES
- AMITIZA [package insert]. Bethesda, MD: Sucampo Pharmaceuticals, Inc.; 2011.
- Jentsch TJ, Stein V, Weinreich F, et al. Physiol Rev. 2002;82:503-568.
- Guyton AC, Hall JE. Textbook of Medical Physiology. 9th ed. Philadelphia, Pa: WB Saunders; 1996.
- Lipecka J, Bali M, Thomas A, et al. Am J Cell Physiol. 2002;282:C805-C816.
- Barrett KE, Keely SJ. Chloride secretion by the intestinal epithelium: molecular basis and regulatory aspects. Annu Rev Physiol. 2000;62:535-572.
- Moeser AJ, Nighot PK, Engelke JK, Ueno R, Bliksglager AT. Recovery of mucosal barrier function in ischemic porcine ileum and colon is stimulated by a novel agonist of the ClC-2 chloride channel, lubiprostone. Am J Physiol Gastrointest Liver Physiol. 2006;292:G647-G656.
Indication
AMITIZA (lubiprostone) is indicated for the treatment of Chronic Idiopathic Constipation (24 mcg twice daily) in adults and for Irritable Bowel Syndrome with Constipation (8 mcg twice daily) in women ≥ 18 years old.
Important Safety Information
- AMITIZA is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction. Patients with symptoms suggestive of mechanical gastrointestinal obstruction should be thoroughly evaluated by the treating healthcare provider to confirm the absence of such an obstruction prior to initiating AMITIZA treatment.
- The safety of AMITIZA in pregnancy has not been evaluated in humans. AMITIZA should be used during pregnancy only if the benefit justifies the potential risk to the fetus. Women who could become pregnant should have a negative pregnancy test prior to beginning therapy with AMITIZA and should be capable of complying with effective contraceptive measures.
- Patients taking AMITIZA may experience nausea. If this occurs, concomitant administration of food with AMITIZA may reduce symptoms of nausea. Patients who experience severe nausea should inform their healthcare provider.
- AMITIZA should not be prescribed to patients that have severe diarrhea. Patients should be aware of the possible occurrence of diarrhea during treatment and inform their healthcare provider if the diarrhea becomes severe.
- Patients taking AMITIZA may experience dyspnea within an hour of first dose. This symptom generally resolves within three hours, but may recur with repeat dosing. Patients who experience dyspnea should inform their healthcare provider. Some patients have discontinued therapy because of dyspnea.
- In clinical trials of AMITIZA (24 mcg twice daily vs placebo; N=1113 vs N=316) in patients with Chronic Idiopathic Constipation (CIC), the most common adverse reactions (incidence > 4%) were nausea (29% vs 3%), diarrhea (12% vs < 1%), headache (11% vs 5%), abdominal pain (8% vs 3%), abdominal distension (6% vs 2%), and flatulence (6% vs 2%).
- In clinical trials of AMITIZA (8 mcg twice daily vs placebo; N=1011 vs N=435) in patients with Irritable Bowel Syndrome with Constipation (IBS-C), the most common adverse reactions (incidence > 4%) were nausea (8% vs 4%), diarrhea (7% vs 4%), and abdominal pain (5% vs 5%).
- Reduce the dosage in CIC patients with moderate and severe hepatic impairment. Reduce the dosage in IBS-C patients with severe hepatic impairment.
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AMITIZA is a trademark of Sucampo Pharmaceuticals, Inc. registered with the U.S. Patent and Trademark Office and used under license by Takeda Pharmaceuticals America, Inc.
©2011 Takeda Pharmaceuticals North America, Inc.
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