Tegaserod

INTRODUCTION

Indications

Short-term treatment of irritable bowel syndrome (IBS) in women whose primary symptom is constipation in patients younger than 55 yr. Chronic idiopathic constipation in patients younger than 55 yr for whom no other treatment has provided satisfactory relief and/or who had satisfactory improvement previously with tegaserod. Only available under an emergency investigational new drug (IND) process. To qualify, patients must have a condition characterized as immediately life threatening or requiring hospitalization. Physicians would need to make the request for emergency use through the FDA.

Action

Acts as a partial agonist of 5-hydroxytryptamine (5-HT, serotonin) at the 5-HT₄ receptor site. Agonist activity causes the release of other neurotransmitters and results in increased peristalsis, increased intestinal secretion, and decreased visceral sensitivity. Therapeutic Effects: Decreased constipation.

Adverse Reactions/Side Effects

CNS: headache. GI: diarrhea.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

• Monitor GI symptoms (constipation, abdominal pain, bloating, cramps) to help document whether drug therapy is successful in reducing these symptoms.

Patient/Client-Related Instruction

• Advise patient to avoid alcohol and foods that may increase GI irritation and constipation.

• Instruct patient to report other bothersome side effects such as severe or prolonged headache or diarrhea.

Pharmacokinetics

Absorption: 10% absorbed following oral administration.

Distribution: Extensively distributed to tissues.

Protein Binding: 98% bound to plasma proteins.

Metabolism and Excretion: 66% excreted unchanged in feces; remainder is metabolized in the GI tract and by the liver. Metabolites are renally excreted.

Half-life: 11 hr.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; Moderate-to-severe hepatic impairment; Severe renal impairment; History of bowel obstruction, gallbladder disease, sphincter of Oddi dysfunction, or intra-abdominal adhesions; Concurrent or frequent diarrhea; Exclusion criteria for emergency access include history, current diagnosis, or symptoms of CV disease, Presence of CV risk factors, Uncompensated depression or anxiety, Suicidal ideation or behavior.

Use Cautiously in: Mild hepatic impairment; Geri: Safety not established; OB: Pregnancy, lactation, or children <18 yr (safety not established).

Interactions

Drug-Drug: None known.

Route/Dosage

PO (Adults): 6 mg bid before meals.

Availability

Tablets: 2 mg, 6 mg.