Tegaserod Maleate

Trade Names:
Zelnorm
- Tablets 2 mg
- Tablets 6 mg

Pharmacology

Feedback for Tegaserod Maleate As a treatment for... Avg User Ratings [?] Constipation -- Chronic 10 2 comments  Rate it! Irritable Bowel Syndrome 9.3 5 comments  Rate it! Compare with other drugs.

Binds with high affinity to human 5-HT ₄ receptors, acting as an agonist at neuronal 5-HT ₄ receptors to trigger the release of neurotransmitters. Activation of 5-HT ₄ receptors in the GI tract stimulates peristaltic reflex and intestinal secretion, and inhibits visceral sensitivity.

Pharmacokinetics

Absorption

Tegaserod T _max is 1 hr. Bioavailability is approximately 10% when given to fasting subjects. When given with food, tegaserod bioavailability is decreased 40% to 65%, and C _max is decreased approximately 20% to 40%.

Distribution

Tegaserod is approximately 98% protein bound (predominantly to alpha-1-acid glycoprotein) and exhibits pronounced distribution into tissues following IV dosing. Vd is approximately 368 L.

Metabolism

Tegaserod is metabolized 1) by presystemic acid catalyzed hydrolysis in stomach followed by oxidation and conjugation, and 2) by direct glucuronidation. The main metabolite is a 5-methoxyindole-3-carboxylic acid glucuronide and has negligible affinity.

Elimination

Plasma Cl of tegaserod is approximately 77 L/hr. Elimination t _½ is approximately 11 hr following IV dosing. About 67% of the orally administered dose is excreted unchanged in the feces; 33% is excreted in the urine primarily as the main metabolite.

Special Populations

Tegaserod is not recommended in severe renal impairment because AUC of main pharmacologically inactive metabolite is increased 10-fold.

Mean AUC is approximately 31% higher, but no dosage adjustment is required in mild hepatic impairment; however, caution is recommended. Tegaserod has not been adequately studied in patients with moderate to severe hepatic impairment, and its use is not recommended.

Indications and Usage

Short-term treatment of women with irritable bowel syndrome (IBS) whose primary symptom is constipation; treatment of patients younger than 65 yr of age with chronic idiopathic constipation.

Contraindications

Severe renal impairment; moderate to severe hepatic impairment; history of bowel obstruction; symptomatic gall bladder disease; suspected sphincter of Oddi dysfunction; abdominal adhesions; known hypersensitivity to the drug or any of its excipients.

Dosage and Administration

PO 6 mg bid before meals for 4 to 6 wk. If response noted, consider an additional 4 to 6 wk of therapy.

PO 6 mg bid before meals. Periodically assess need for continued therapy.

Storage/Stability

Store tablets at controlled room temperature (59° to 86°F). Protect from moisture.

Drug Interactions

Plasma concentrations of these drugs may be reduced; however, adjustments in therapy are unlikely to be necessary.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Fatigue (1%); angina pectoris; arrhythmia; bundle branch block; flushing; hypotension; syncope; supraventricular tachycardia.

CNS

Headache (15%); dizziness (4%); insomnia, migraine (2%); depression; increased appetite; restlessness; sleep disorder; vertigo.

Dermatologic

Pruritis, skin rash (1%).

EENT

Visual disturbance.

GI

Abdominal pain (12%); diarrhea (9%); nausea (8%); flatulence (6%); abdominal distension (4%); vomiting (2%); bile duct stone, dyspepsia, fecal incontinence, gangrenous bowel, gastritis, GI reflux, hemorrhoids, ischemic colitis, mesenteric ischemia, proctalgia, rectal bleeding, stomach discomfort, suspected sphincter of Oddi spasm (postmarketing).

Genitourinary

Dysmenorrhea (2%); UTI (1%); breast carcinoma; menorrhagia; miscarriage.

Hepatic

Cholelithiasis; cholecystectomy; cholecystitis with elevated transaminases (postmarketing).

Metabolic

Electrolyte disorders, hypovolemia; increased creatine phosphokinase; peripheral edema.

Musculoskeletal

Back pain (5%); arthropathy (2%); myalgia (1%).

Respiratory

Upper respiratory tract infection (4%); sinusitis (3%); pharyngitis, sinus congestion (1%); dyspnea, pharyngolaryngeal pain.

Miscellaneous

Accidental trauma (3%); fungal infection, leg pain (1%); chest pain; hypersensitivity; increased eosinophil count; low neutrophil count; pain.

Precautions

Pregnancy

Category B .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Abdominal pain

Discontinue immediately in patients with new or sudden worsening of abdominal pain.

Diarrhea

Discontinue immediately in patients who develop severe diarrhea. Do not initiate therapy in patients who are experiencing, or frequently experience, diarrhea.

Ischemic colitis

May occur. Discontinue immediately in patients who develop symptoms of ischemic colitis, such as rectal bleeding, bloody diarrhea, or new or worsening abdominal pain. Do not resume treatment in patients who develop findings of ischemic colitis or other forms of intestinal ischemia.

Overdosage

Symptoms

Diarrhea, headache, intermittent abdominal pain, flatulence, nausea, vomiting.

Patient Information

• Explain name, dose, action, potential side effects, and potential benefits of therapy.
• Advise patient to read Information for the Patient before starting therapy and with each refill.
• Instruct patient to take prescribed dose twice daily on an empty stomach shortly before a meal.
• Instruct patient that if a dose is missed to skip that dose and take the next dose at the regularly scheduled time. Warn patient not to double the dose to make up the missed dose.
• Warn patient not to start medication if they are currently experiencing diarrhea or frequently experience diarrhea.
• Advise patient that symptoms of their condition may return within 1 to 2 wk of stopping therapy.
• Advise patient with IBS that medication does not cure IBS, should be taken as prescribed, and not to stop taking or change the dose unless advised by health care provider.
• Advise patient with IBS that medication is usually taken for 4 to 6 wk and that if improvement is noted (eg, decreased bloating, constipation, and pain and discomfort in the abdominal area), their health care provider may recommend an additional 4 to 6 wk of therapy.
• Advise patient with chronic idiopathic constipation that if the medication works they should note a reduction in straining, bloating, and abdominal discomfort and an increase in number of bowel movements. Advise patient to talk with health care provider regularly about whether they need to stay on tegaserod.
• Instruct patient to discontinue use and immediately notify health care provider if any of the following occur: new or worsening abdominal pain; severe diarrhea or diarrhea accompanied by severe cramping, stomach pain, fainting, or dizziness; or rectal bleeding or bloody diarrhea.
• Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding.
• Warn patient not to take any prescription or OTC drugs, dietary supplements, or herbal preparations without consulting health care provider.
• Advise patient that follow-up visits may be necessary to monitor therapy and to keep appointments.

Link to this page

Printable Version

Email Page

Add to my drug list

Constipation -- Chronic, Irritable Bowel Syndrome

User Reviews:

7 comment(s) about Tegaserod Maleate