Tegaserod

Indications

Tegaserod is used for: Irritable bowel syndrome and constipation

Adult Dose

Oral 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. Hepatic impairment: Moderate to severe impairment: Not recommended.

Child Dose

Renal Dose

Renal impairment: Severe impairment: Not recommended.

Administration

Should be taken on an empty stomach. Take before meals.

Contra Indications

Severe renal or moderate to severe hepatic impairment; history of bowel obstruction or symptomatic gallbladder disease; suspected sphincter of Oddi dysfunction or abdominal adhesions; known hypersensitivity. Patients currently experiencing or who frequently experience diarrhoea. Lactation.

Precautions

Discontinue immediately if rectal bleeding, bloody diarrhoea, new or sudden worsening of abdominal pain occurs. Mild hepatic impairment; child <18 yr; pregnancy.

Pregnancy-Lactation

Pregnancy Available data from case reports with use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes Animal studies Decreased survival of rat pups observed with maternal dietary administration of tegaserod at 71 times the recommended dose during organogenesis and through lactation Decreased body weight and delays in developmental landmarks in rat pups were observed with maternal dietary administration of 45 times the recommended dose Lactation There are no data regarding the presence in human milk, effects on breastfed infants, or on milk production Tegaserod and its metabolites are present in rat milk; the milk-to-plasma concentration ratio for tegaserod is very high When a drug is present in animal milk, it is likely that the drug will be present in human milk Because of the potential for serious reactions in the breastfed infant, including tumorigenicity, advise lactating women not to breastfeed during tegaserod treatment

Interactions

Adverse Effects

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

Mechanism of Action

Tegaserod is a 5-HT4 receptor partial agonist that binds with high affinity at human 5-HT4 receptors, whereas it has no appreciable affinity for 5-HT3 or dopamine receptors. It has moderate affinity for 5-HT1 receptors. Tegaserod, by acting as an agonist at neuronal 5-HT4 receptors, triggers the release of further neurotransmitters such as calcitonin gene-related peptide from sensory neurons. The activation of 5-HT4 receptors in the gastrointestinal tract stimulates the peristaltic reflex and intestinal secretion, as well as inhibits visceral sensitivity.