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
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.