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Tegaserod Maleate

Class: GI Drugs, Miscellaneous
VA Class: GA900
Chemical Name: 2-[(5-methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide
Molecular Formula: C16H23N5O
CAS Number: 145158-71-0
Brands: Zelnorm


Special Alerts:

Data became available in early 2007 indicating that tegaserod may be associated with an increased risk of ischemic cardiovascular events (e.g., unstable angina, MI, stroke).17 19 20 (See Cardiovascular Effects under Cautions.) Based on these data, FDA concluded that the benefits of the drug no longer outweighed the risks, and the manufacturer agreed voluntarily to withdraw the drug from the US market in March 2007.17 19 20 Subsequently (in July 2007), the manufacturer and FDA established an investigational, limited-access program (treatment IND protocol) to make the drug available for use, if deemed medically necessary, in select women with constipation-predominant irritable bowel syndrome (IBS) or chronic idiopathic constipation.21 22

In 2008, FDA announced that the manufacturer of tegaserod had decided to discontinue making the drug available under the treatment IND protocol. The manufacturer agreed to continue to supply tegaserod in emergency situations (e.g., life-threatening, serious enough to qualify for hospitalization). Requests for the drug for such situations would have to be made to the FDA, which could authorize shipment of the drug by the manufacturer. However, the drug now is listed as discontinued on FDA websites.


Partial type 4 serotonergic (5-HT4) receptor agonist; modulates serotonin-sensitive GI processes.1 2 3 4 5 6 7 8 9

Uses for Tegaserod Maleate

Constipation-predominant Irritable Bowel Syndrome in Women

Management of irritable bowel syndrome (IBS) in women whose predominant intestinal symptom is constipation.1 2 3 4 5 9 However, only select patients with this disorder were eligible to receive the drug through the restricted-access program in the US.21 22 (See Notice.)

Slideshow: Bowled Over By Your Bowel: IBS Causes, Risk Factors and Treatments

Chronic Idiopathic Constipation

Initially received approval from FDA for the management of chronic idiopathic constipation in adults younger than 65 years of age.1 However, only select patients with this disorder were eligible to receive the drug through the restricted-access program in the US.21 22 (See Notice.)

Tegaserod Maleate Dosage and Administration


Oral Administration

Administer orally before a meal.1 12


Available as tegaserod maleate; dosage expressed in terms of tegaserod.1


Constipation-predominant IBS in Women

6 mg twice daily for 4–6 weeks.1 2 4

Consider additional 4- to 6-week course of therapy in patients who respond.1

Chronic Idiopathic Constipation

Adults <65 years of age: 6 mg twice daily.1

Periodically assess need for continued therapy.1

Prescribing Limits


Constipation-predominant IBS in Women

Efficacy beyond 12 weeks of therapy not studied.1

Chronic Idiopathic Constipation

Efficacy beyond 12 weeks of therapy not studied.1

Special Populations

Hepatic Impairment

Mild hepatic impairment: Dosage adjustment not necessary.1 5 (See Contraindications and also Hepatic Impairment under Cautions.)

Renal Impairment

Mild to moderate renal impairment: Dosage adjustment not necessary.1 (See Contraindications under Cautions.)

Geriatric Patients

Dosage adjustment not necessary in patients ≥65 years of age with constipation-predominant IBS.1

Cautions for Tegaserod Maleate


  • Severe renal impairment.1 9

  • Moderate or severe hepatic impairment.1 9

  • History of intestinal obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions.1 9

  • Known hypersensitivity to tegaserod or any ingredient in the formulation.1



Cardiovascular Effects

Possible increased risk of ischemic cardiovascular events.17 19 20 A pooled analysis of 29 short-term (1–3 months) controlled trials involving approximately 18,600 patients (88% women, average age of 43 years) with various GI disorders indicated an increased risk of ischemic cardiovascular events (e.g., unstable angina, MI, stroke) in patients receiving tegaserod (0.1%) compared with those receiving placebo (0.01%).17 19 20 All patients who experienced ischemic cardiovascular events during these studies had preexisting cardiovascular disease or risk factors for cardiovascular disease.19 No discernible pattern with regard to the timing of the event.19 Events did not appear to be dose related.19

Men, women ≥55 years of age, and patients with a history or current diagnosis of ischemic cardiovascular disease, symptoms suggestive of such disease, or any cardiovascular risk factors are not eligible for enrollment in the limited-access (treatment IND) program.21 22 (See Notice.)


Diarrhea resulting in serious consequences (e.g., hypovolemia, hypotension, syncope) reported; hospitalization for rehydration required in some cases.1 13 14 16

Immediately discontinue if hypotension or syncope occurs.1 13 14 16

Do not initiate tegaserod in patients with diarrhea or in those who frequently experience diarrhea.1 13 14 16

General Precautions

Abdominal Pain

Immediately discontinue if new (or suddenly worsening) abdominal pain occurs.1 13 (See Ischemic Colitis under Cautions.)

Ischemic Colitis

Ischemic colitis and other intestinal ischemia reported during postmarketing use; causal relationship not established.1 13 14 16

Immediately discontinue if symptoms of ischemic colitis (e.g., rectal bleeding, bloody diarrhea, new or worsening abdominal pain) occur.1 13 14 16 Promptly evaluate patients with these symptoms, perform appropriate diagnostic tests; do not resume treatment if findings are consistent with ischemic colitis.1 13 16

Specific Populations


Category B.1


Not known whether tegaserod is distributed into human milk.1 Discontinue nursing or the drug.1

Pediatric Use

Safety and efficacy not established in pediatric patients.1

Geriatric Use

In geriatric patients with constipation-predominant IBS, no substantial differences in safety or pharmacokinetics relative to younger adults.1

Efficacy not established in geriatric patients with chronic idiopathic constipation; tegaserod was no more effective than placebo in patients ≥65 years of age with this condition.1 Higher incidence of tegaserod-related diarrhea and diarrhea-related discontinuance of the drug in these patients than in younger adults.1

Hepatic Impairment

Not recommended in patients with moderate or severe hepatic impairment; not adequately studied.1 Caution in patients with mild impairment.1

Renal Impairment

Not recommended in patients with severe renal impairment.1


Safety and efficacy not established in men with constipation-predominant IBS.1 9

Common Adverse Effects

IBS patients: headache, migraine, dizziness, abdominal pain, diarrhea, nausea, flatulence, back pain, leg pain, accidental trauma, arthropathy.1 5 6 8 9

Patients with chronic idiopathic constipation: diarrhea, abdominal pain, nausea, abdominal distension, upper abdominal pain, vomiting, dizziness, insomnia, aggravated headache, fatigue, upper respiratory tract infection, sinusitis, fungal infection, back pain, myalgia, dysmenorrhea, pharyngitis, sinus congestion, urinary tract infection, rash, pruritus.1

Interactions for Tegaserod Maleate

Does not inhibit CYP2C8, CYP2C9, CYP2C19, CYP2E1, or CYP3A4 in vitro.1

Drugs Affecting Hepatic Microsomal Enzymes

CYP2D6 and CYP1A2 substrates: Pharmacokinetic interaction unlikely.1

Specific Drugs





Pharmacokinetic interaction unlikely1


Pharmacokinetic interaction unlikely1


Decreased digoxin peak plasma concentrations and exposure1

Not considered clinically important1


Pharmacokinetic interaction unlikely1

Hormonal contraceptives

Levonorgestrel: Decreased peak plasma concentrations and exposure (8%) 1

Ethinyl estradiol: Pharmacokinetic interaction unlikely1

Unlikely to be clinically important (risk of ovulation not expected to be altered) or require oral contraceptive dosage adjustment1


Pharmacokinetic interaction unlikely1


Pharmacokinetic interaction unlikely1


Interaction unlikely1

Warfarin dosage adjustment not necessary1

Tegaserod Maleate Pharmacokinetics



Peak plasma concentrations attained within 1 hour.1

Bioavailability is about 10% in fasting individuals.1


Food reduces bioavailability by 40–65% and delays time to peak plasma concentrations.1

Administration of tegaserod ≤30 minutes before, with, or 2.5 hours after a meal reduces peak plasma concentrations by 20–40%.1

Special Populations

Severe renal impairment requiring dialysis (Clcr ≤15 mL/minute): No change in pharmacokinetics of tegaserod; peak plasma concentration and AUC of main (inactive) metabolite increased.1

Mild hepatic impairment: Peak plasma concentration increased 16%, AUC increased 31%.1

Moderate to severe hepatic impairment: Not adequately studied.1

Geriatric women (65–85 years of age): Peak plasma concentration and exposure increased relative to younger women; values in geriatric women were within variability reported in healthy individuals.1



Widely distributed.1

Not known whether tegaserod crosses the placenta.1 Distributed into milk in rats; not known whether distributed into human milk.1

Plasma Protein Binding




Presystemic gastric acid hydrolysis, then undergoes oxidation and glucuronidation to main inactive metabolite; also undergoes direct glucuronidation.1

Elimination Route

Excreted mainly (about 67%) in feces as unchanged drug and in urine (about 33%) principally as main metabolite.1


About 11 hours (range: 6–16 hours).1





25°C (may be exposed to 15–30°C).1 Protect from moisture.1


  • Binds with high affinity to 5-HT4 receptors on neurons in the GI tract.1 2 3 4 5 6 8 9 Activates these receptors, stimulating the peristaltic reflex and intestinal secretion, and inhibits visceral sensitivity.1 2 3 4 5 6 8 9

  • Also may enhance basal motor activity and normalize impaired motility throughout the GI tract.1 2 4 5 6 7 8

Advice to Patients

  • Importance of understanding the potential risks and benefits of tegaserod therapy prior to initiating therapy with the drug.21 22

  • Potential risk of ischemic cardiovascular events (e.g., unstable angina, MI, stroke).17 19 20 Importance of seeking immediate emergency medical care if symptoms suggestive of MI or stroke (e.g., severe chest pain, shortness of breath, dizziness, sudden onset of weakness or difficulty in walking or talking) occur.17 20

  • Importance of immediately discontinuing tegaserod and informing clinician if new or worsening abdominal pain, rectal bleeding, or bloody diarrhea occurs.1 13 14 15 16

  • Importance of not starting tegaserod if currently experiencing diarrhea or if diarrhea occurs frequently.1

  • Diarrhea may occur during therapy, but usually will resolve with continued use; importance of informing clinician if diarrhea is severe or is accompanied by severe cramping, abdominal pain, dizziness, feeling lightheaded or faint.1 13 14 15 16

  • Importance of taking before a meal.1

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1

  • Importance of informing patients of other important precautionary information.1 (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Was available in the US on a restricted basis only.21 22 (See Notice.)

Tegaserod Maleate


Dosage Forms


Brand Names




2 mg (of tegaserod)



6 mg (of tegaserod)



AHFS DI Essentials. © Copyright, 2004-2015, Selected Revisions October 1, 2015. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.


1. Novartis. Zelnorm (tegaserod maleate) tablets prescribing information. East Hanover, NJ; 2006 Jul.

2. Camilleri M. Management of irritable bowel syndrome. Gastroenterol. 2001; 120:652-68.

3. Talley NJ. Serotoninergic neuroenteric modulators. Lancet. 2001; 358:2061-8. [PubMed 11755632]

4. Camilleri M. Novel medications for the irritable bowel syndrome: motility and sensation. J Pediatr Gastroenterol Nutr. 2001; 32:S35-7. [PubMed 11321419]

5. Beglinger C. Tegaserod: a novel, selective 5-HT4 receptor partial agonist for irritable bowel syndrome. Int J Clin Pract. 2002; 56:47-51. [PubMed 11831835]

6. Zhou H, Khalilieh S, Lau H et al. Effect of meal timing not critical for the pharmacokinetics of tegaserod (HTF 919). J Clin Pharmacol. 1999; 39:911-19. [PubMed 10471981]

7. Prather CM, Camilleri M, Zinsmeister AR et al. Tegaserod accelerates orocecal transit in patents with constipation-predominant irritable bowel syndrome. Gastrenterol. 2000; 118:463-8.

8. Scott LJ, Perry CM. Tegaserod. Drugs. 1999; 58:491-6. [PubMed 10493276]

9. Anon. Tegaserod maleate for IBS with constipation. Med Lett Drugs Ther. 2002; 44:79-80. [PubMed 12237618]

10. GlaxoWellcome Inc. Lotronex (alosetron hydrochloride) tablets prescribing information. Research Triangle Park, NC; 2000 Feb.

11. Anon. FDA approves irritable bowel syndrome treatment for women. FDA Talk Paper. Rockville, MD: Food and Drug Administration; 2000 Feb. 9.

12. Novartis, East Hanover, NJ: Personal communication.

13. Bess AL, Cunningham SR. Dear health care professional letter regarding diarrhea and ischemic colitis. East Hanover, NJ: Novartis; 2004 Apr 26.

14. Food and Drug Administration. Questions and answers in Zelnorm (tegaserod maleate). Rockville, MD; 2004 Aug 10. From FDA website (

15. Novartis. Zelnorm (tegaserod maleate) tablets information for the patient. East Hanover, NJ; 2004 Aug.

16. FDA updates Zelnorm labeling with new risk information. FDA Talk Paper. Rockville, MD: Food and Drug Administration; 2004 Apr 28. From FDA website (

17. FDA public health advisory: tegaserod maleate (marketed as Zelnorm). Rockville, MD; 2007 Mar 30. From FDA website (

18. Novartis. Reimbursement policy for Zelnorm patients and frequently asked questions about reimbursement. From Zelnorm website (). Accessed 2007 May 23.

19. Bess AL, Cunningham SR. Dear health care professional letter: Urgent: marketing and sales suspension notice for Zelnorm tablets, 2-mg and 6-mg, all lots within expiry. East Hanover, NJ: Novartis Pharmaceuticals Corporation: 2007 Mar 30.

20. Questions and answers on Zelnorm (tegaserod maleate). Rockville, MD: Food and Drug Administration; 2007 Mar 30. From FDA website ().

21. Novartis. The Zelnorm reimbursement program ends September 30, 2007. 2007 Oct. From Zelnorm website (). Accessed 2007 Oct 29.

22. US Food and Drug Administration. FDA permits restricted use of Zelnorm for qualifying patients. Rockville, MD; 2007 Jul 27. From FDA website ().