Jane S. Ricciuti, RPh, MS


September 20, 2002

In This Article

Gastrointestinal Agents

(tegaserod maleate) Tablets

Manufacturer: Novartis

Drug Approval Classification: Original New Drug Application (Approval Date: 7/24/02)

Indication: Zelnorm (tegaserod maleate) is indicated for the short-term treatment of women with irritable bowel syndrome (IBS) whose primary bowel symptom is constipation.

The safety and effectiveness of Zelnorm in men have not been established.

Dosing: The recommended dosage of Zelnorm is 6 mg taken twice daily orally before meals for 4-6 weeks. For those patients who respond to therapy at 4-6 weeks, an additional 4- to 6-week course can be considered.

Clinical Summary: Tegaserod is a 5-HT4 receptor partial agonist that binds with high affinity at human 5-HT4 receptors. The activation of 5-HT4 receptors in the gastrointestinal tract stimulates the peristaltic reflex and intestinal secretion, and also inhibits visceral sensitivity.

Tegaserod 6 mg twice daily was studied in three 3-month, multicenter, double-blind, placebo-controlled studies, involving 2470 women (mean age 43 years) with at least a 3-month history of IBS symptoms (including abdominal pain, bloating, and constipation) prior to the study baseline period. Patients received either Zelnorm (tegaserod maleate) 6 mg twice daily or placebo.

Response rates after the first month of therapy in patients treated with Zelnorm were 14% higher than those for placebo. Response rates at the end of the third month were 5% to 11% higher than those seen with placebo. Response was defined as the patient's self-report that she was considerably or completely relieved for at least 2 of the 4 weeks, or if she was at least somewhat relieved for each of the 4 weeks.

Zelnorm is contraindicated in patients who have a history of bowel obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions.

Adverse Effects: Zelnorm-induced diarrhea occurred in 8.8% of patients compared with 3.8% of patients in the placebo groups during phase 3 clinical trials. Diarrhea occurred during the first week of therapy and resolved with continued therapy. In addition to diarrhea, other adverse events included abdominal pain (12%), nausea (8%), flatulence (6%), headache (15%), and back pain (5%).

Pharmacokinetics: Peak plasma concentrations are reached approximately 1 hour after oral dosing. When the drug is administered with food, the bioavailability of tegaserod is reduced by 40% to 65% and Cmax by approximately 20% to 40%. Tmax of tegaserod is prolonged from approximately 1 hour to 2 hours when taken following a meal, but decreased to 0.7 hours when taken 30 minutes prior to a meal.

Dose adjustments are recommended for patients with mild-to-moderate renal impairment. In reduced hepatic function, the mean area under the curve (AUC) was 31% higher; caution is advised in patients with mild hepatic impairment. Use of tegaserod is not recommended in patients with moderate or severe hepatic impairment.

Several drug-drug interaction studies were conducted with tegaserod; results showed no clinically meaningful interactions.

Zelnorm (tegaserod) Labeling

(lansoprazole) Capsules

Manufacturer: TAP Pharmaceutical Products, Inc.

Drug Approval Classification: Supplemental New Drug Application (Approval Date: 8/6/02)

New Indication: This supplemental indication is approved for use in children 1-11 years of age for the short-term treatment of symptomatic gastroesophageal reflux disease and the short-term treatment of erosive esophagitis.

Dosing: For pediatric patients weighing < 30 kg, the recommended dosage is 15 mg once daily for up to 12 weeks. For pediatric patients weighing ≥ 30 kg, the recommended dosage is 30 mg once daily for up to 12 weeks.

Clinical Summary: An open-label efficacy study evaluated lansoprazole in 66 pediatric patients (1-11 years of age). After 8-12 weeks of Prevacid treatment, the intent-to-treat analysis demonstrated an approximate 50% reduction in frequency and severity of gastroesophageal reflux disease symptoms. Twenty-one of 27 erosive esophagitis patients were healed at 8 weeks, and 100% of patients were healed at 12 weeks by endoscopy.

Adverse Effects: Prevacid-associated adverse events in pediatric patients were similar to adult adverse events. The most frequently reported events included constipation (5%) and headache (3%).

Prevacid (lansoprazole) Labeling


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