Tegaserod is a serotonin type-4 (5HT4) receptor partial agonist. Tegaserod binds with high affinity at human 5HT4 receptors, present on caudate membranes, whereas it has no appreciable affinity for human recombinant 5HT3 receptors or human recombinant dopamine D2 receptors. In vitro and animal study has revealed that Tegaserod can trigger the peristaltic reflex via 5HT4 receptor activation and thereby enhance basal motor activity and normalize impaired GI motility.

Tegaserod is indicated for the symptomatic treatment of irritable bowel syndrome with constipation (IBS-C) in patients whose main symptoms are constipation and abdominal pain or discomfort. The maximum duration of treatment is 12 weeks and treatment should be discontinued if there has been no response after 4 weeks.

General recommended dosage for adult: Tegaserod 6 mg twice daily taken orally with a glass of water 30 minutes before meal. The maximum duration of treatment is 12 weeks and treatment should be discontinued after 4 weeks if no response has occurred.

Use in elderly: Dose adjustment is not necessary when administering Tegaserod to patients over 65 years old.

Use in children: There is no clinical trial in document to safety and efficacy of tegaserod in children. Therefore, it is not recommended for use in children.

Administration

Patient should be advised to take Tegaserod (6 mg twice daily) 30 minutes before meal.

Patient should also be made aware of the possible occurrence of diarrhea during therapy. In most cases, the diarrhea occurred early, is transient, is most often observed as a single episode during the 12 week treatment period, and resolved with continued therapy.

Patients should be instructed to consult their physician if they experience new or worsening abdominal pain not typical of their IBS symptoms.

Tegaserod is not recommended in patients with severe renal or hepatic impairment. It is also contraindicated in patients with hypersensitivity to tegaserod or any excipient of this formulation.

Abdominal pain, diarrhea, nausea, flatulence, headache, fatigue, back pain etc.

Overdose Effects

Signs and symptoms of overdosage may include diarrhoea, headache, abdominal pain and orthostatic hypotension. As in any case of over dose, general supportive measures should be utilized.

Diarrhea was reported in some of the patients receiving Tegaserod in the Phase III clinical studies. Caution is required in patients in whom increased diarrhea could have negative effects. Patients who are currently experiencing or frequently experience diarrhea should not initiate therapy with Tegaserod.

Use in Special Populations

Renal impairment: No dosage adjustment is required in patients with mild to moderate renal impairment. Tegaserod is not recommended in patients with severe renal impairment.

Hepatic impairment: No dosage adjustment is required in patients with mild to moderate hepatic impairment, however, caution is recommended when using Tegaserod in this patient population. It has not been studied in patients with severe hepatic impairment, and therefore, it is not recommended in this group.

Pregnancy & Lactation

Pregnancy: In view of limited experience in human, use of Tegaserod during pregnancy is not recommended.

Nursing mothers: Tegaserod should not be prescribed to nursing mothers.