Tegaserod

(te gas' a rod)

Molecule Info

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WARNING

Serious consequences of diarrhea, including hypovolemia, hypotension, and syncope have been reported in the clinical studies and during marketed use of Tegaserod maleate In some cases, these complications have required hospitalization for rehydration. Tegaserod maleate should be discontinued immediately in patients who develop severe diarrhea, hypotension or syncope. Tegaserod maleate should not be initiated in patients who are currently experiencing or frequently experience diarrhea.

Indication(s) & Dosage

Tegaserod maleate is indicated in-

IBS with Constipation

Tegaserod maleate (Zelnorm®)  is indicated for the short-term treatment of women with irritable bowel syndrome (IBS) whose primary bowel symptom is constipation. The safety and effectiveness of Tegaserod maleate (Zelnorm®) in men with IBS with constipation have not been established.

Chronic Idiopathic Constipation

Tegaserod maleate is indicated for the treatment of patients less than 65 years of age with chronic idiopathic constipation. The effectiveness of Tegaserod maleate in patients 65 years or older with chronic idiopathic constipation has not been established. The efficacy of Tegaserod maleate for the treatment of IBS with constipation or chronic idiopathic constipation has not been studied beyond 12 weeks.

Chronic idiopathic constipation, Constipation-predominant irritable bowel syndrome
Adult: 6 mg taken bid for 4-6 wk continued for another 4-6 wk in responsive patients. 
Severe Renal impairment: Not recommended.
Hepatic impairment: Moderate to severe impairment: Not recommended.

Administration

Should be taken before meals.

Contraindications

Tegaserod maleate is contraindicated in those patients with:

  • severe renal impairment.
  • moderate or severe hepatic impairment.
  • a history of bowel obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions.
  • a known hypersensitivity to the drug or any of its excipients.

Warning & Precautions

 

General precaution

Tegaserod maleate should be discontinued immediately in patients with new or sudden worsening of abdominal pain.

Ischemic colitis

Ischemic colitis and other forms of intestinal ischemia have been reported in patients receiving Tegaserod maleate during marketed use of the drug. In some cases, hospitalization was required. Tegaserod maleate should be discontinued immediately in patients who develop symptoms of ischemic colitis, such as rectal bleeding, bloody diarrhea or new or worsening abdominal pain. Patients experiencing these symptoms should be evaluated promptly and have appropriate diagnostic testing performed. Treatment with Tegaserod maleate should not be resumed in patients who develop findings consistent with ischemic colitis or other forms of intestinal ischemia.

Adverse Drug Reaction(s)

Diarrhoea, abdominal pain, nausea, flatulence, headache, dizziness, migraine, leg or back pain, arthropathy, insomnia, hypotension, arrhythmia, ischaemic colitis.
Potentially Fatal: MI, stroke.

Drug Interactions

Potentially Fatal: Reduction in peak plasma conc of digoxin.

Food Interaction

Food reduces bioavailability by 40-65% and Cmax 20-40%. Tmax is prolonged from approx 1-2 hrs.

Pregnancy Category (FDA)

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Storage

Oral: Store at 25°C.

Pharmacology

Tegaserod, is a prokinetic with partial agonistic activity at 5HT4. Activation of these receptors stimulate peristaltic reflex and intestinal secretion as well as inhibit visceral sensitivity.
Absorption: Bioavailability: 10%. Peak plasma concentrations after 1 hr.
Distribution: Protein-binding: 98% primarily to α-acid glycoprotein. Widely distributed into tissues.
Metabolism: Extensively hepatic by oxidation, conjugation and glucuronidation; hydrolysis in the stomach.
Excretion: Faeces (as unchanged drug), urine (as metabolites). Terminal half life: 11hr.

ATC Classification

A03AE02 - tegaserod; Belongs to the class of drugs acting on serotonin receptors. Used in the treatment of functional bowel disorders.

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Brand/Product Info


Total Products : 4    
Brand Name Manufacturer/Marketer Composition Dosage Form Pack Size & Price
DORESA Incepta Pharmaceuticals Limited Tegaserod maleate INN 6mg Tablet Tablet 10x5's:MRP 300 Tk
TEGARID Renata Limited Tegaserod maleate INN 6mg Tablet 30's: 180.00 MRP
TIBS Eskayef Bangladesh Ltd Tegaserod maleate INN 6mg Tablet 50's MRP: 300.00
ZILED Kemiko Pharmaceuticals Ltd Tegaserod maleate INN 6mg Tablet 30's: 180.00 MRP

Gen. MedInfo

IMPORTANT WARNING from FDA:

In 2007, tegaserod was removed from the U.S. market and was made available only through a restricted distribution program from the manufacturer. Beginning in April 2008, tegaserod will no longer be available through the restricted distribution program; therefore, the U.S. Food and Drug Administration (FDA) has decided to make tegaserod available to physicians for patients in emergency situations that are life-threatening or require hospitalization. If your doctor believes that you should receive tegaserod, he or she may contact the FDA for more information. If you are receiving tegaserod through the restricted distribution program, you should talk to your doctor about switching to another treatment.

Why is Tegaserod prescribed?

Tegaserod is used to relieve pain, bloating, and constipation caused by irritable bowel syndrome (IBS; a condition that causes stomach pain, bloating, constipation, and diarrhea) in women whose main symptom is constipation. Tegaserod is also used to increase the frequency of bowel movements and relieve bloating, straining, and stomach pain in women and men with chronic idiopathic constipation (constipation that is not due to other diseases or medications and that has been a problem for longer than 6 months). Tegaserod is in a class of medications called serotonin agonists. It works by improving muscle movement and increasing production of fluid in the bowels.

How should Tegaserod be used?

Tegaserod comes as a tablet to take by mouth. It is usually taken twice a day on an empty stomach shortly before a meal. Take tegaserod at around the same times every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take tegaserod exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

If you have IBS with constipation, your doctor will probably tell you to take tegaserod for 4-6 weeks. If your symptoms improve, your doctor may tell you to take tegaserod for another 4-6 weeks. If you have chronic idiopathic constipation, you should talk to your doctor regularly to see if you should continue to take tegaserod. Be sure to tell your doctor how you are feeling, and do not take tegaserod for longer than your doctor prescribes.

Tegaserod controls the symptoms of irritable bowel syndrome and chronic idiopathic constipation, but does not cure these conditions. Continue to take tegaserod even if you feel well. Do not stop taking tegaserod without talking to your doctor. If you stop taking tegaserod, your symptoms may return within 1-2 weeks.

What special precautions to follow?

Before taking tegaserod,

  • tell your Doctor if you are allergic to tegaserod or any other medications.
  • tell your Doctor what other prescription and nonprescription medications, vitamins, herbal products, or nutritional supplements you are taking. Your doctor may need to adjust the dose of your medications or monitor you more carefully for side effects.
  • tell your doctor if you have diarrhea now or if you often have diarrhea; if you have or have ever had gallbladder, kidney, or liver disease; a blockage in your intestines or unexplained stomach pain; abdominal surgery (surgery on the area between your chest and hips); jaundice (yellowing of the skin or eyes); sphincter of Oddi dysfunction (blockage of bile or digestive juices flowing into the intestine that causes pain and/or jaundice); or ischemic colitis (decreased blood flow to the intestines causing rectal bleeding, bloody diarrhea, or stomach pain).
  • tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking tegaserod, call your doctor. Do not breast-feed while you are taking tegaserod.
  • you may have some diarrhea, especially during your first week of taking tegaserod. However, if you have a lot of diarrhea, or if you also have severe cramping, dizziness, light-headedness, fainting, blurred vision, upset stomach or a fast heartbeat, you should stop taking tegaserod and call your doctor immediately.

What side effects can Tegaserod cause?

Tegaserod may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:

  • headache
  • diarrhea
  • nausea
  • vomiting
  • gas
  • leg or back pain
  • joint pain or problems
  • difficulty falling asleep or staying asleep
  • runny nose, congestion, or other cold symptoms
  • rash
  • hives
  • itching
  • swelling of the face, throat, tongue, lips, or eyes
  • difficulty breathing and swallowing
  • hoarseness

Some side effects can be serious. If you experience any of the following symptoms Consult your doctor immediately:

People with IBS may need to have abdominal surgery, especially gallbladder surgery, more often than people who do not have IBS. People with IBS who took tegaserod needed this type of surgery somewhat more often than people who did not take tegaserod. It is not known if taking tegaserod increases your chance of needing abdominal surgery. Talk to your doctor about the risk of taking Tegaserod.

You should know that tegaserod rarely may cause ischemic colitis. Tell your doctor and stop taking tegaserod right away if you have new or worsening stomach pain, bloody diarrhea, rectal bleeding, or blood in your stools.

Tegaserod may cause other side effects. Consult your doctor if you have any unusual problems while taking Tegaserod.

Ref: MedlinPlus, U.S. Natl. Library of Medicine.

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