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Pronunciation
(teg a SER od)
Generic Available
No
Index Terms
Prescribing and Access Restrictions
Available in U.S. under an emergency investigational new drug (IND) process. Emergency situations are defined as immediately life-threatening or requiring hospitalization. Physicians with patients who may qualify can contact the FDA's Division of Drug Information via email (druginfo@fda.hhs.gov). The FDA may either deny the request or authorize shipment of Zelnorm® by Novartis. Additional information can be found at http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm103223.htm.
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Use: Labeled Indications
Emergency treatment of irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation (CIC) in women (<55 years of age) in which no alternative therapy exists
Pregnancy Risk Factor
B
Pregnancy Considerations
Safety and efficacy have not been established in pregnant women. Use during pregnancy only if clearly needed.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Per product labeling: Hypersensitivity to tegaserod or any component of the formulation; severe renal impairment; moderate or severe hepatic impairment; history of bowel obstruction, symptomatic gallbladder disease, suspected sphincter of Oddi dysfunction, or abdominal adhesions. Treatment should not be started in patients with diarrhea or in those who experience diarrhea frequently.
Exclusion criteria under the emergency-IND process: Unstable angina, history of MI or stroke, hypertension, hyperlipidemia, diabetes, age ≥55 years, smoking, obesity, depression, anxiety, or suicidal ideation.
Warnings/Precautions
Concerns related to adverse reactions:
• Cardiovascular effects: Serious cardiovascular events (eg, MI, stroke, unstable angina) may occur; patients should seek emergency care following any sign and symptom suggestive of a serious cardiac event.
• Diarrhea: May occur after the start of treatment, most cases reported as a single episode within the first week of therapy, and may resolve with continued dosing. However, serious consequences of diarrhea (hypovolemia, syncope) have been reported; patients should be warned to contact healthcare provider immediately if they develop severe diarrhea, or diarrhea with severe cramping, abdominal pain, or dizziness.
• Intestinal ischemic events: Use has been associated with rare intestinal ischemic events; discontinue immediately with new or sudden worsening abdominal pain or rectal bleeding.
Disease-related concerns:
• Cardiovascular disease: Use will not be permitted in patients with unstable angina, a history of MI or stroke, hyperlipidemia, cigarette smoking, hypertension, or obesity.
• Depression: Use will not be permitted in patients with depression or anxiety, or with any signs of suicidal ideation or behavior.
• Diabetes: Use will not be permitted in patients with diabetes.
• Hepatic impairment: Use with caution in patients with mild hepatic impairment; not recommended with moderate or severe impairment.
Special populations:
• Elderly women: Contraindicated in women ≥55 years of age.
• Males: Safety and efficacy have not been established in males.
Other warnings/precautions:
• Risk vs benefit: Potential benefits should be weighed against potential risks in qualifying patients eligible for emergency-IND use.
Adverse Reactions
>10%:
Central nervous system: Headache (15%)
Gastrointestinal: Abdominal pain (12%)
1% to 10%:
Central nervous system: Dizziness (4%), migraine (2%)
Gastrointestinal: Diarrhea (9%; severe <1%), nausea (8%), flatulence (6%)
Neuromuscular & skeletal: Back pain (5%), arthropathy (2%), leg pain (1%)
<1%: Albuminuria, ALT increased, angina pectoris, appendicitis, appetite increased, arrhythmia, asthma, AST increased, breast carcinoma, bundle branch block, cholecystitis, concentration impaired, CPK increased, cramps, depression, diaphoresis, emotional lability, eructation, facial edema, fecal incontinence, flushing, hypotension, irritable colon, menorrhagia, micturition, miscarriage, ovarian cyst, pain, polyuria, pruritus, renal pain, serum bilirubin increased, sleep disorder, subileus, suicide attempt, supraventricular tachycardia, syncope, tenesmus, vertigo
Postmarketing and/or case reports: Alopecia, bile duct stone, cholecystitis (with increased transaminases), gangrenous bowel, hepatitis, hypersensitivity reaction, hypokalemia (secondary to diarrhea), ischemic colitis, mesenteric ischemia, MI, rectal bleeding, sphincter of Oddi spasm (suspected), severe diarrhea (complicated by hypovolemia, hypotension, syncope), stroke, unstable angina
Drug Interactions
There are no known significant interactions.
Ethanol/Nutrition/Herb Interactions
Food: Bioavailability is decreased by 40% to 65% and Cmax is decreased by 20% to 40% when taken with food. Tmax is prolonged from 1 hour up to 2 hours when taken following a meal, but decreased to 0.7 hours when taken 30 minutes before a meal.
Storage
Store at controlled room temperature of 15°C to 30°C (59°F to 86°F). Protect from moisture.
Mechanism of Action
Tegaserod is a partial neuronal 5-HT4 receptor agonist. Its action at the receptor site leads to stimulation of the peristaltic reflex and intestinal secretion, and moderation of visceral sensitivity.
Pharmacodynamics/Kinetics
Distribution: Vd: 368 ± 223 L
Protein binding: 98% primarily to α1-acid glycoprotein
Metabolism: GI: Hydrolysis in the stomach; Hepatic: Oxidation, conjugation, and glucuronidation; metabolite (negligible activity); significant first-pass effect
Bioavailability: Fasting: 10%
Half-life elimination: I.V.: 11 ± 5 hours
Time to peak: 1 hour
Excretion: Feces (~66% as unchanged drug); urine (~33% as metabolites)
Dosage
Oral:
Adults (<55 years of age): Females:
IBS with constipation: 6 mg twice daily, before meals, for 4-6 weeks; may consider continuing treatment for an additional 4-6 weeks in patients who respond initially
Chronic idiopathic constipation: 6 mg twice daily, before meals; the need for continued therapy should be reassessed periodically
Elderly: Use in women ≥55 years of age is contraindicated.
Dosage adjustment in renal impairment: Cmax and AUC of the inactive metabolite are increased with renal impairment.
Mild-to-moderate impairment: No dosage adjustment recommended
Severe impairment: Use is contraindicated
Dosage adjustment in hepatic impairment: Cmax and AUC of tegaserod are increased with hepatic impairment.
Mild impairment: No dosage adjustment recommended; however, use caution
Moderate-to-severe impairment: Use is contraindicated
Administration: Oral
Administer 30 minutes before meals.
Dietary Considerations
Take on an empty stomach, 30 minutes before meals.
Patient Education
Take on an empty stomach, 30 minutes before meals. Effectiveness of treatment will need to be evaluated by prescriber; maintain contact/appointment schedule as directed. May cause headache, dizziness, nausea, flatulence, or diarrhea. Stop taking Zelnorm® and contact prescriber immediately with any new or sudden worsening abdominal pain or rectal bleeding, or severe or bloody diarrhea. Seek emergency medical care immediately if you experience severe chest pain, shortness of breath, dizziness, sudden onset of weakness, or difficulty walking or talking.
Geriatric Considerations
No dosing adjustment is required.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause dizziness and headache; may rarely cause depression, mood lability, and insomnia
Mental Health: Effects on Psychiatric Treatment
GI side effects are common; use caution with SSRIs
Nursing: Physical Assessment/Monitoring
For emergency use only under FDA emergency investigational new drug process. Monitor for cardiac event, clinically-significant diarrhea (hypovolemia, hypotension, syncope), and ischemic colitis (rectal bleeding, bloody diarrhea, abdominal pain) frequently when beginning therapy and at regular intervals during treatment.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral:
Zelnorm®: 2 mg, 6 mg
Pricing: U.S. (www.drugstore.com)
Tablets (Zelnorm)
2 mg (60): $198.24
6 mg (60): $198.24
International Brand Names
Lexi-Comp.com
Last full review/revision March 2011
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