Tegaserod (Oral)

As a 5-HT4 agonist, Tegaserod is a useful medicine in the management of IBS, constipation and associated complications.

Overview

Tegaserod is used as an effective short-term treatment of irritable bowel syndrome (IBS) most notably in women. It is also effective in treating constipation in certain men and women who suffer from chronic lack of bowel movements. It can also be used "off label"to treat other ailments at the discretion of the patient's doctor.

As a selective serotonin receptor agonist, this medication works on the nerves within the bowel to help improve and normalize bowel function, resulting in healthier, easily-passed stools and more regular bowel movements.

Although approved by the FDA in 2002, Tegaserod was removed from the market in 2007 on account of concerns regarding potentially adverse cardiovascular effects. Prior to this, it was the only medication that had been approved by the US Food and Drug Administration to help relieve bloating, abdominal discomfort and constipation experienced by sufferers of irritable bowel syndrome and/or chronic idiopathic constipation.

Tegaserod functions as a motility stimulant, and it achieves this by activating 5-HT4 receptors of the nervous system in the gastro-intestinal tract. At the same time, it stimulates the peristaltic reflex which allegedly reduces abdominal cramps and pains. In addition to functioning as a 5-HT4 agonist, Tegaserod also works on the 5-HT2B receptors.

Conditions treated

  • Irritable bowel syndrome
  • Chronic idiopathic constipation

Type of medicine

  • Motility stimulant

Side effects

As well as the desired effects, Tegaserod may also cause some unwanted side effects. These can range from those which cause mild discomfort to others which may require medical attention or even warrant discontinuing treatment with the medicine. The most common side effects recorded by patients taking Tegaserod include: dizziness, migraine, joint pain, back pain, abdominal pain, stomach cramps, vomiting, bloating, nausea, leg pain, dry mouth and fatigue.

As the patient continues to take Tegaserod as described, the majority of these side effects should subside to a tolerable level or dissipate completely. In the instance of minor side effects, such as dry mouth, a healthcare practitioner may be able to offer practical advice on alleviating the discomfort, such as drinking a glass of water or chewing sugar-free gum in this instance. If certain side effects remain persistent over a long period of time or get worse as treatment continues, the patient is strongly advised to inform their doctor or healthcare provider.

The majority of patients will only experience minimal side effects when undergoing a course of treatment with Tegaserod, if any whatsoever. The drug actually functions to alleviate a number of the described side effects and is generally prescribed because the benefits of using it outweigh the risks or unpleasantness of minor side effects.

The following side effects may occur rarely (albeit often enough to warrant mentioning): a feeling of general warmth, itchy skin, redness in the face/neck/arms/chest, black or tarry stools, diarrhea, indigestion, and/or rectal bleeding. Like the more common side effects, these should subside in patients who experience them over time, as the patient's body will adjust to the way the drug works.

Because Tegaserod has the potential to cause confusion and affect the psychology of the patient, doctors advise that anybody undergoing treatment with this medicine should refrain from driving or operating heavy machinery until is has been observed that they do not pose a risk to themselves or other road users.

Patients who experience any of the following side effects are advised to discontinue use of this medication and seek medical assistance, as they may be allergic to one or more ingredients: excessive air and gas in the intestines or stomach, cold sweats, a bloated or full feeling, lightheadedness or faintness when standing up from a prone position, and/or acute headaches.

Dosage

As with all medicines, it is incredibly important for patients to only take Tegaserod as prescribed by a physician. This means that patients should not take more of this medication than advised by their doctor, either in terms of size or frequency of doses. On top of this, patients should understand that they should cease taking Tegaserod if a doctor advises them to do so, even if they still have a supply of the medication remaining.

Tegaserod comes in tablet form, and can be taken with or without food. Healthcare professionals recommend that this medication is washed down with a glass of water to help it reach the stomach faster. Tablets should be swallowed whole as opposed to crushed, chewed or diluted in liquid. Dosages for the treatment of constipation and/or IBS may vary from patient to patient, dependent on a number of factors including severity of the condition and physiology of the patient. The recipient of this medication should pay close attention to their doctor at the moment they prescribe Tegaserod in order to understand precisely when, how and in what size dose they should take the medicine.

The manufacturers of Tegaserod provide general dosage instructions on the literature supplied with the medication, although patients should understand that these are only guidelines and should instead take the drug as directed by their healthcare provider.

Most doctors agree that the standard dose for the treatment of irritable bowel syndrome with Tegaserod is 6mg, taken orally, twice daily, for a period of 4-6 weeks. Patients who respond to therapy at 4-6 weeks can be considered for an additional course of the same length.

For the treatment of chronic idiopathic constipation, doctors are likely to prescribe a dose of 6mg of Tegaserod taken twice daily, orally, before meals. Both doctor and patient should periodically assess the need for continuous therapy with this medication. Patients undergoing treatment with this medication may also wish to consider the health benefits of switching to a fiber-rich diet in helping to naturally alleviate the symptoms of constipation without the use of medication.

There are no recommended pediatric doses of Tegaserod. In the event that a minor requires treatment with this medicine, the dose size and frequency should be decided at the discretion of the doctor overseeing treatment.

If a dose is missed, patients are advised to simply wait until the time for the next dose is due, and to continue dosage as normal. Patients should refrain from taking double or extra doses in an attempt to make up for missed doses, as this increases the potential of overdose. In the event of an overdose, the patient or their caregiver should contact the local disease control center or emergency department immediately.

Interactions

All drugs have the potential to interact with other medications or chemicals within the body. These interactions can cause one or more medications to become ineffective, and in some instances interactions can cause potentially harmful effects. For these reasons, it is imperative that patients keep a fully detailed list of all medicines they are currently undergoing treatment with. This extends to vitamins, herbal supplements and over the counter remedies as well as prescription medications. Some patients fail to understand this and run the risk of experiencing harmful side effects as a result of simply not disclosing their entire non-prescription drug regimen.

Below is a partial list of medicines known to negatively interact with Tegaserod. Patients who are currently being treated with one or more of these drugs should notify their doctor or healthcare provider before beginning a course of Tegaserod:

  • albuterol
  • baclofen
  • Cymbalta (duloxetine)
  • diazepam
  • Mucinex (guaifenesin)
  • Nexium (esomeprazole)
  • pantoprazole
  • Skelaxin (metaxalone)
  • sumatriptan
  • Synthroid (levothyroxine)
  • Topamax (topiramate)
  • tramadol
  • Vitamin C (ascorbic acid)
  • Zyrtec (cetirizine)
  • diphenhydramine
  • Elavil (amitriptyline)
  • gabapentin
  • hydroxyzine
  • ibuprofen
  • morphine

Food can cause levels of Tegaserod in the body to decrease. Although Tegaserod can be taken with food, it is advisable that patients attempt to take it on an empty stomach at least 30 minutes prior to eating, or at least two hours after. This will make it easier for the body to absorb the medicine.

Warnings

Tegaserod was taken off the market by the FDA in 2007 at the request of its manufacturer due it its propensity to induce heart problems in a not insignificant number of patients in a control study group. It is therefore not advisable for patients who currently suffer from any congenital heart defects or diseases, or those with a history of heart attack, stroke, angina or any heart complication whatsoever to consider using Tegaserod. Those suffering from any of these conditions who wish to seek treatment for chronic IBS or constipation are urged to consult their doctor or healthcare provider who will be able to offer an alternative course of therapy.

Patients with a history of intestinal obstruction are advised against the use of Tegaserod, as the stimulation of gastro-intestinal motility could cause harm in these instances. Examples of intestinal obstructions include symptomatic gallbladder disease, sphincter dysfunction and/or abdominal adhesions.

The use of Tegaserod in patients with moderate to severe liver disease is not recommended, as this can result in weak plasma concentration in comparison to patients with normal hepatic function. Patients suffering from moderate to severe liver issues are advised to take an adjusted dose of Tegaserod, and to only take the medicine if the benefits outweigh the risks. Patients with liver impairment should discuss these dosage adjustments with their healthcare provider, who may suggest an alternate course of treatment.

Animal studies have revealed no evidence of fetal harm, therefore Tegaserod has been classified as a pregnancy category B drug by the FDA. However, this medication is recommended for use by pregnant women only if the benefits of doing so outweigh the risks.

Tegaserod has been observed to excrete into breast milk with a high milk-to-plasma ratio. Because of the potential for tumorigenicity observed in animal studies, the manufacturer of Tegaserod recommends that breastfeeding mothers should either discontinue nursing their infant(s) with breastmilk, or discontinue the use of Tegaserod, dependent on the importance of treatment with the drug.

Storage

Tegaserod should be stored in a cool, dark and dry place, such as a dedicated medicine storage cupboard, out of the reach of children. It is not suitable for freezing or refrigeration, and should be kept away from moisture - it is therefore unsuitable for storage in the bathroom cabinet.

Patients who need to dispose of unwanted or unused Tegaserod tablets should do so with great care and attention, ensuring that the medicine is not flushed down a drain or toilet. Many pharmacies offer a takeback scheme, where they will dispose of unwanted medicines in a safe and hygenic manner, for free. Patients with unwanted medications are advised to take advantage of such schemes.

Summary

Although Tegaserod is an effective and popular treatment for IBS and chronic constipation, studies have suggested that it poses a risk of inducing cardiovascular events such as stroke, heart attack or severe chest pain, at a rate of approximately 13 cases out of every 11,600. Because of this risk, the manufacturer of the medication (Novartis) requested that the medication be withdrawn from everyday medical use by the FDA.

Despite its withdrawal from mainstream medical treatment, the drug is still prescribed by a number of physicians worldwide, particularly if the patient undergoing treatment is relatively healthy and does not have a history or family history of congenital heart problems. In some instances, Tegaserod is used off-label for the treatment of other nervous system conditions not associated with constipation or irritable bowel syndrome.

In order to get the greatest benefit from this medicine, patient and doctor are urged to work together in order to come to a conclusion as to what the most beneficial dosage is, and how long the course of treatment should last.

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Last Reviewed:
December 23, 2017
Last Updated:
April 05, 2018
Content Source: