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Pronunciation:

(si BYOO tra meen)

U.S. Brand Names:

Meridia®

Synonyms:

Sibutramine Hydrochloride Monohydrate

Generic Available:

Canadian Brand Names:

Meridia®

Use:

Management of obesity, including weight loss and maintenance of weight loss; should be used in conjunction with a reduced-calorie diet

Restrictions:

C-IV; recommended only for obese patients with a body mass index 30 kg/m² or 27 kg/m² in the presence of other risk factors such as hypertension, diabetes, and/or dyslipidemia

Pregnancy Risk Factor:

Lactation:

Excretion in breast milk unknown/not recommended

Contraindications:

Hypersensitivity to sibutramine or any component of the formulation; during or within 2 weeks of MAO inhibitors (eg, phenelzine, selegiline) or concomitant centrally-acting appetite suppressants; anorexia nervosa; bulimia nervosa; uncontrolled or poorly-controlled hypertension; congestive heart failure; coronary heart disease; conduction disorders (arrhythmias); stroke; concurrent use of serotonergic agents (eg, SSRIs sumatriptan, dihydroergotamine, dextromethorphan, meperidine, pentazocine, fentanyl, lithium)

Warnings/Precautions:

Use with caution in renal impairment or hepatic dysfunction, seizure disorder, hypertension, gallstones, narrow-angle glaucoma, nursing mothers, and elderly patients. Primary pulmonary hypertension (PPH), a rare and frequently fatal pulmonary disease, has been reported to occur in patients receiving other agents with serotonergic activity which have been used as anorexiants. Although not reported in clinical trials, it is possible that sibutramine may share this potential, and patients should be monitored closely. Rare cases of bleeding have been reported; use caution in patients with bleeding disorders. Stimulants may unmask tics in individuals with coexisting Tourette's syndrome. Sibutramine may have the potential to potentiate or impair judgment or motor skills.

Serious, potentially life-threatening toxicities may occur when thyroid hormones (at dosages above usual daily hormonal requirements) are used in combination with sympathomimetic amines to induce weight loss.

Safety and efficacy have not been established with severe renal or hepatic dysfunction or in children <16 years of age.

Adverse Reactions:

Frequency not defined.

Central nervous system: Thinking abnormal, agitation, fever

Dermatologic: Pruritus

Endocrine & metabolic: Menstrual disorders/irregularities

Gastrointestinal: Diarrhea, flatulence, gastroenteritis, tooth disorder

Neuromuscular & Skeletal: Arthritis, hypertonia, leg cramps

Ocular: Amblyopia

Respiratory: Bronchitis, dyspnea

>10%

Central nervous system: Headache, insomnia

Gastrointestinal: Anorexia, xerostomia, constipation

Respiratory: Rhinitis

1% to 10%

Cardiovascular: Tachycardia, vasodilation, hypertension, palpitation, chest pain, edema

Central nervous system: Migraine, dizziness, nervousness, anxiety, depression, somnolence, CNS stimulation, emotional liability

Dermatologic: Acne, herpes simplex, rash

Endocrine & metabolic: Dysmenorrhea

Gastrointestinal: Appetite increased, nausea, dyspepsia, gastritis, vomiting, taste perversion, abdominal pain, rectal disorder

Genitourinary: Urinary tract infection, vaginal Monilia

Hepatic: Abnormal LFTs

Neuromuscular & skeletal: Weakness, arthralgia, back pain, neck pain, myalgia

Otic: Ear disorder, ear pain

Respiratory: Pharyngitis, sinusitis, cough, laryngitis

Miscellaneous: Diaphoresis, flu-like syndrome, allergic reactions, thirst

<1%: Bruising, ecchymosis, interstitial nephritis, seizure

Postmarketing and/or case reports (frequency not defined; limited to important or life-threatening): Alopecia, anaphylactic shock, anaphylactoid reaction, anemia, angina, angioedema, arrhythmia, arthrosis, atrial fibrillation, cardiac arrest, CHF, cholecystitis, cholelithiasis, GI hemorrhage, goiter, hematuria, hyper-/hypoglycemia, hyper-/hypothyroidism, impotence, increased intraocular pressure, intestinal obstruction, lymphadenopathy, mania, nightmares, petechiae, photosensitivity, stroke, syncope, torsade de pointes, urinary frequency increased, urinary retention, urticaria, transient ischemic attack, vascular headache, ventricular dysrhythmias

Overdosage/Toxicology:

Symptoms of overdose include hypertension, tachycardia, headache, and palpitations. Treatment is supportive.

Drug Interactions:

Substrate of CYP3A4 (major)

Buspirone: Concurrent use may result in serotonin syndrome; these combinations are best avoided.

CNS stimulants: May increase potential for sibutramine-associated cardiovascular complications or serotonergic effects; includes decongestants, centrally-acting weight loss products, amphetamines, and amphetamine-like compounds.

CYP3A4 inhibitors: May increase the levels/effects of sibutramine. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

Dihydroergotamine: Concurrent use may result in serotonin syndrome; these combinations are best avoided.

Dextromethorphan: Concurrent use may result in serotonin syndrome; these combinations are best avoided.

Lithium: Concurrent use may result in serotonin syndrome; these combinations are best avoided.

MAO inhibitors: Sibutramine should not be used with nonselective MAO inhibitors (isocarboxazid, phenelzine) due to a theoretical risk of serotonin syndrome.

Meperidine: Concurrent use may result in serotonin syndrome; these combinations are best avoided.

Nefazodone: Concurrent use may result in serotonin syndrome; these combinations are best avoided.

Serotonergic agents: Concurrent use may result in serotonin syndrome; includes selective serotonin reuptake inhibitors (eg, sumatriptan, lithium, tryptophan), some opioid/analgesics (eg, meperidine, tramadol), and venlafaxine.

SSRIs: Combined use with other drugs which inhibit the reuptake (sibutramine) may cause serotonin syndrome; avoid these combinations.

Serotonin agonists: Theoretically may increase the risk of serotonin syndrome; includes sumatriptan, naratriptan, rizatriptan, and zolmitriptan.

Tramadol: Sibutramine combined with tramadol (serotonergic effects) may cause serotonin syndrome; monitor.

Trazodone: Sibutramine may inhibit the metabolism of trazodone resulting in increased toxicity; monitor.

Tricyclic antidepressants: Sibutramine may inhibit the metabolism of tricyclic antidepressants (amitriptyline, desipramine, imipramine, nortriptyline) resulting is elevated serum levels; if combination is warranted, a low dose of TCA (10-25 mg/day) should be utilized.

Tryptophan: Sibutramine may inhibit the reuptake of serotonin; combination with tryptophan, a serotonin precursor, may cause agitation and restlessness; this combination is best avoided.

Venlafaxine: Combined use with sibutramine may increase the risk of serotonin syndrome.

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid excess ethanol ingestion.

Herb/Nutraceutical: St John's wort may decrease sibutramine levels.

Stability:

Store at room temperature of 15°C to 30°C (59°F to 86°F).

Mechanism of Action:

Sibutramine blocks the neuronal uptake of norepinephrine, serotonin, and (to a lesser extent) dopamine

Pharmacodynamics/Kinetics:

Absorption: Rapid

Protein binding, plasma: 94% to 97%

Metabolism: Hepatic; undergoes first-pass metabolism via CYP3A4; forms metabolites (active)

Time to peak: Within 3-4 hours

Excretion: Primarily urine (77%); feces

Dosage:

Adults 16 years: Initial: 10 mg once daily; after 4 weeks may titrate up to 15 mg once daily as needed and tolerated (may be used for up to 2 years, per manufacturer labeling)

Monitoring Parameters:

Do initial blood pressure and heart rate evaluation and then monitor regularly during therapy. If patient has sustained increases in either blood pressure or pulse rate, consider discontinuing or reducing the dose of the drug.

Dietary Considerations:

Sibutramine, as an appetite suppressant, is the most effective when combined with a low calorie diet and behavior modification counseling.

Patient Education:

Take exactly as directed; do not increase dose or frequency without consulting prescriber. May be taken with meals (do not take at bedtime). Avoid alcohol, caffeine, or OTC medications that act as stimulants. You may experience restlessness, dizziness, sleepiness (use caution when driving or engaging in tasks requiring alertness until response to drug is known); insomnia (taking medication early in morning may help, warm milk, and quiet environment at bedtime may help); increased appetite, nausea or vomiting (small, frequent meals, frequent mouth care may help); constipation (increased exercise, fluids, fruit, or fiber may help); diarrhea (buttermilk, boiled milk, or yogurt may help); or altered menstrual periods (reversible when drug is discontinued). Report chest pain, palpitations, or irregular heartbeat; excessive nervousness, excitation, or sleepiness; back pain, muscle weakness, or tremors; CNS changes (acute headache, aggressiveness, restlessness, excitation, sleep disturbances); menstrual pattern changes; rash; blurred vision; runny nose, sinusitis, cough, or respiratory difficulty. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.

Additional Information:

Physicians should carefully evaluate patients for history of drug abuse and follow such patients closely, observing them for signs of misuse or abuse (eg, development of tolerance, excessive increases of doses, drug seeking behavior).

Unlike dexfenfluramine and fenfluramine, the medication does not cause the release of serotonin from neurons. Tests done on humans show no evidence of valvular heart disease and experiments done on animals show no evidence of the neurotoxicity which was found in similar testing using animals treated with fenfluramine and dexfenfluramine; has minimal potential for abuse.

Cardiovascular Considerations:

Sibutramine may induce a significant blood pressure increase and should be avoided in patients with cardiovascular disease. The hypertensive effect of sibutramine may theoretically potentiate the nocturnal hypertension in patients with sleep apnea. Because this drug is used in the management of obesity, it is likely that many of the patients receiving it will have coexisting obstructive sleep apnea.

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

Dental Comment:

The mechanism of action is thought to be different from the "fen" drugs. Sibutramine works to suppress the appetite by inhibiting the reuptake of norepinephrine and serotonin. Unlike dexfenfluramine and fenfluramine, it is not a serotonin releaser. Sibutramine is closer chemically to the widely used antidepressants such as fluoxetine (Prozac®). The FDA approved sibutramine over the objections of its own advisory panel, who called the drug too risky. FDA reported that the drug causes blood pressure to increase, generally by a small amount, though in some patients the increases were higher. It is now recommended that patients taking sibutramine have their blood pressure evaluated regularly.

Dosage Forms:

Capsule, as hydrochloride: 5 mg, 10 mg, 15 mg

International Brand Names:

Asisten® (CO); Ectiva® (IT); Ipomex® (AR); Meridia® (CA, CZ, PL); Plenty® (BR, CO); Raductil® (AR, CR, DO, GT, HN, MX, PA, SV); Reductil® (AT, BE, BR, CH, CL, CO, DE, DK, EG, ES, FI, GB, HR, HU, IE, IL, IT, JO, KW, LB, MX, NO, NZ, PT, RO, SE, SG, SI, SY, TH, TR, ZA); Sacietyl® (AR); Saton® (EC); Sibu-Estirol® (AR); Sibumin® (DO); Sibutral® (FR); Sibutramina MK® (CO)

References

Colchamiro R, "FDA Clears Obesity Drug,"Am Druggist, 1998, 12.

King DJ and Devaney N, "Clinical Pharmacology of Sibutramine Hydrochloride (BTS 54524), A New Antidepressant, in Healthy Volunteers,"Br J Clin Pharmacol, 1988, 26(5):607-11.

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