Tegaserod

What is Tegaserod?

• Tegaserod (Zelnorm) is a serotonin-4 (5-HT4) receptor agonist used in women younger than 65 years of age to treat irritable bowel syndrome with constipation.

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Tegaserod chemical structure

Tegaserod structure

Tegaserod ball-and-stick model

What are the uses of this medicine?

• Tegaserod (Zelnorm) is a prescription medicine used for the treatment of adult women less than 65 years of age who have irritable bowel syndrome with constipation (IBS-C).

Limitations of use:

• It is not known if Zelnorm is safe and effective in men with IBS-C.
• It is not known if Zelnorm is safe and effective in children.

How does this medicine work?

• Tegaserod is an agonist of serotonin type-4 (5-HT4) receptors that stimulates the peristaltic reflex and intestinal secretion, inhibits visceral sensitivity, enhances basal motor activity, and normalizes impaired motility throughout the gastrointestinal tract.
• Tegaserod is an antagonist at 5-HT2B receptors in humans.
• It is expected to have minimal binding to 5-HT1 receptors.
• Tegaserod has no affinity for 5-HT3 or dopamine receptors.
• It enhances basal motor activity and normalized impaired motility throughout the gastrointestinal tract.
• In addition, studies demonstrated that tegaserod moderated visceral sensitivity during colorectal distension in animals.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have had a heart attack, stroke, transient ischemic attack or TIA, or angina.
• have had inflammation and injury of the intestines caused by reduced blood flow to the intestines (ischemic colitis).
• have severe kidney problems or end-stage kidney disease.
• have moderate or severe liver problems.
• have had an intestinal blockage (bowel obstruction), gallbladder problems that caused symptoms, or scar tissue that formed between the tissues of the abdomen and other organs in the abdomen.
• have or may have had a problem with the muscular valve that controls the flow of digestive juices (bile and pancreatic juice) to the first part of your intestine (sphincter of Oddi).
• are allergic to tegaserod.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Is this medicine FDA approved?

• It was approved for use in the United States in 2002 and was available in tablets of 2 or 6 mg under the brand name of Zelnorm.
• Tegaserod was withdrawn in 2007 because of adverse cardiovascular effects, postmarketing studies demonstrating an excess of severe adverse cardiovascular events in tegaserod treated patients (0.11%) compared to matched controls (0.01%).
• The association of tegaserod with adverse cardiovascular events has been contested but, currently, tegaserod is available only on an emergency basis and with prior authorization from the FDA.

How should this medicine be used?

Recommended dosage:

• The recommended dosage of Zelnorm in adult women less than 65 years of age is 6 mg taken twice daily orally at least 30 minutes before meals.
• Discontinue Zelnorm in patients who have not had adequate control of symptoms after 4 to 6 weeks of treatment.

Administration:

• Tegaserod comes as a tablet to take by mouth.
• Take Zelnorm exactly as your healthcare provider tells you to take it.
• The usual dose of Zelnorm is 1 tablet 2 times each day, taken by mouth.
• Take Zelnorm at least 30 minutes before a meal.
• If you take too much Zelnorm, call your healthcare provider or go to the nearest hospital emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 6 mg tegaserod.

This medicine is available in fallowing brand namesː

• Zelnorm

What side effects can this medication cause?

The most common side effects of this medicine may include:

• headache
• stomach-area (abdominal) pain
• nausea
• gas
• indigestion
• dizziness

Zelnorm can cause serious side effects, including:

• Major heart (cardiovascular) events
• ischemic colitis
• Loss of body fluids caused by diarrhea
• Suicidal thoughts and behavior

What special precautions should I follow?

• Stroke, MI, and cardiovascular death (major adverse cardiovascular events [MACE]) have been reported in adults taking Zelnorm. Advise patients to promptly seek medical attention if they develop symptoms of an MI, stroke, TIA, or angina. Also, advise patients to immediately inform their healthcare provider if they develop clinical or other evidence of cardiovascular ischemic heart disease (e.g., coronary artery disease) or other changes in their health status that could increase cardiovascular risk (e.g., smoking, hypertension, hyperlipidemia, diabetes mellitus, obesity) while taking Zelnorm.
• Ischemic colitis and other forms of intestinal ischemia have been reported postmarketing in patients receiving Zelnorm. Advise patients to stop taking Zelnorm and seek medical attention if they develop symptoms of ischemic colitis, such as rectal bleeding, bloody diarrhea or new or worsening abdominal pain.
• Diarrhea is one of the most common adverse reactions in Zelnorm-treated patients. Instruct patients to discontinue Zelnorm and contact their healthcare provider if they develop severe diarrhea, especially if they also experience symptoms of volume depletion (hypotension and/or syncope).
• Suicide, suicidal attempt and ideation, and self-injurious behavior have been reported in clinical trials of IBS-C and other gastrointestinal motility disorders. Counsel patients, their caregivers, and their families that Zelnorm may increase the risk of suicidal thoughts and behavior and advise them of the need to be alert for the emergence or worsening of symptoms of depression, any unusual changes in mood or behavior, or the emergence of suicidal thoughts, behavior, or thoughts of self-harm. Instruct patients, caregivers, and families that if any of these symptoms occur, they should immediately discontinue Zelnorm and report behaviors of concern to their healthcare provider.
• Advise a woman that breastfeeding is not recommended during treatment with Zelnorm.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• diarrhea and headache
• orthostatic hypotension
• abdominal pain
• flatulence
• nausea
• vomiting

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• Based on the large distribution volume and high protein binding of tegaserod, it is unlikely that tegaserod could be removed by dialysis.
• In cases of overdosage, treat symptomatically and institute supportive measures as appropriate.

Can this medicine be used in pregnancy?

• Available data from case reports with Zelnorm use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
• It is not known if Zelnorm will harm your unborn baby.

Can this medicine be used in children?

• Safety and effectiveness of Zelnorm in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: tegaserod
• Inactive Ingredients: colloidal silicon dioxide, crospovidone, glyceryl behenate, hypromellose, and lactose monohydrate

Who manufactures and distributes this medicine?

Distributed by:

• Alfasigma USA, Inc., Covington, LA USA

What should I know about storage and disposal of this medication?

• Store Zelnorm at room temperature between 68°F to 77°F (20°C to 25°C).
• Protect Zelnorm from moisture.

Antidiarrheal agents

Antidiarrheal agents include bulk forming agents, hydroscopic agents, bile acid resins, bismuth, inhibitors of intestinal motility, non-absorbed antibiotics and hormones. Bulk forming agents include methylcellulose; hydroscopic agents include pectin and kaolin; bile acid resins are cholestyramine, colestipol and colesevalam; inhibitors of intestinal motility include opioids such as diphenoxylate and loperamide. Antibiotics include rifamycin and rifaximin which are non-absorbed and are used for travelers' diarrhea. Hormones with antidiarrheal activity include octretide and somatostatin. Most antidiarrheal agents are active locally in the small intestine and colon and are largely not absorbed. Some, however, have been implicated in rare causes of liver injury (senna, cascara, cholestyramine). Telotristat is a relatively new agent that inhibits the synthesis of serotonin and is used specifically for the diarrhea of carcinoid syndrome.

• Cholestyramine
• Colesevelam
• Colestipol
• Crofelemer
• Difenoxin
• Diphenoxylate
• Kaolin
• Loperamide
• Methylcellulose
• Octreotide
• Pectin
• Rifamycin
• Rifaximin
• Somatostatin
• Telotristat

Antiemetics are a diverse group of medications that act at different points in the pathways that regulate nausea and vomiting. These include antihistamines, anticholinergic agents, phenothiazines, serotonin type 3 receptor blockers, centrally acting benzamides, cannabinoid receptor agonists, substance P antagonists and miscellaneous.

Anticholinergic Agents

• Hyoscyamine, Methscopolamine, Scopolamine

Antihistamines

• Cyclizine, Dimenhydrinate, Hydroxyzine, Meclizine, and Promethazine

Cannabinoid Receptor Agonists

• Dronabinol, Nabilone, Tetrahydrocannabinol
• Phenothiazines [See Antipsychotic Agents]
• Chlorpromazine, Prochlorperazine

Serotonin 5-HT3 Receptor Antagonists

• Alosetron, Dolasetron, Granisetron, Ondansetron, Palonosetron

Substance P/Neurokinin 1 Receptor Antagonists

• Aprepitant, Fosaprepitant, Rolapitant

Miscellaneous

• Dexamethasone, Metoclopramide, Trimethobenzamide

Acid peptic disease/antiulcer agents that include antacids, the histamine type 2 receptor blockers (H2 blockers), and the proton pump inhibitors (PPIs). These agents are some of the most commonly taken medications and are very well tolerated, most being available both by prescription and over-the-counter. While many of these drugs are approved for use in duodenal and gastric ulcer disease, their major use is for acid reflux and indigestion.

Histamine H2 Receptor Antagonists (H2 Blockers) Cimetidine, Famotidine, Nizatidine, Ranitidine

Proton Pump Inhibitors

• Dexlansoprazole, Esomeprazole, Lansoprazole, Omeprazole, Pantoprazole, Rabeprazole

Cathartics, laxatives or agents for constipation include bulk forming agents, osmotic agents, stool wetting agents, nonspecific stimulants, prokinetic agents and agents that increase fluid secretion. Many of these therapies are not systemically absorbed and none are considered particularly hepatotoxic. Naldemedine and naloxegol are opioid antagonists and are used to treat the constipation associated with opioid use.

• Bisacodyl
• Cascara Sagrada
• Castor Oil
• Docusate
• Fiber, Bran
• Lactulose
• Magnesium Sulfate
• Methylcellulose
• Naldemedine (Opioid Antagonist)
• Naloxegol (Opioid Antagonist)
• Plecanatide (for Chronic Idiopathic Constipation)
• Prucalopride (for Chronic Idiopathic Constipation)
• Senna

Inflammatory bowel disease encompasses several disorders, most commonly ulcerative colitis and Crohn colitis. Agents can be classified as 5-aminosalicyclic acid (5-ASA) based agents, immunosuppressive drugs, antitumor necrosis factor agents, corticosteroids, antibiotics and miscellaneous.

5-Aminosalicyclic Acid (5-ASA) Derivatives

• Balsalazide, Mesalamine, Olsalazine, Sulfasalazine

Immunosuppressive Agents

• Azathioprine, Mercaptopurine, Methotrexate

Tumor Necrosis Factor Antagonists

• Adalimumab, Certolizumab, Golimumab, Infliximab

Miscellaneous

• Metronidazole, Natalizumab, Vedolizumab

Irritable Bowel Syndrome Agents Antimuscarinics/Antispasmodics [See Anticholinergic agents

• Dicyclomine, Glycopyrrolate, Hyoscyamine, Methscopolamine

Prokinetic Agents - See Serotonin 5-ht4 receptor agonists Alosetron, Cisapride, Domperidone, Linaclotide, Lubiprostone, Metoclopramide, Plecanatide, Prucalopride, Tegaserod

Other

• Eluxadoline

• Dailymed label info on Tegaserod
• FDA Tegaserod

Tegaserod Resources
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