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- Capsules 5 mg
- Capsules 10 mg
- Capsules 15 mg
Inhibits reuptake of norepinephrine, serotonin, and dopamine. May stimulate satiety center in brain, causing appetite suppression.
Sibutramine T max is 1.2 h; food delays T max by approximately 3 h. Approximately 77% of a single oral dose is absorbed. Steady state is reached within 4 days.
Sibutramine is extensively bound and is rapidly and extensively distributed into tissues. Highest concentrations are in liver and kidneys.
Sibutramine undergoes extensive first-pass metabolism and is metabolized primarily by the CYP-450 3A4 isoenzyme. The pharmacologically active metabolites are mono- and di-desmethyl M 1 and M 2 .
Sibutramine t ½ is 1.1 h. Oral clearance is 1,750 L/h, and approximately 85% is excreted in urine.
Special PopulationsRenal Function Impairment
Do not use in severe renal function impairment.Hepatic Function Impairment
Do not use in severe hepatic function impairment.Elderly
Dose selection should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Indications and Usage
As an adjunct to a reduced calorie diet for the management of obesity, including weight loss and maintenance of weight loss. Recommended for patients with an initial body mass index greater than 30 kg/m 2 or greater than 27 kg/m 2 in the presence of other risk factors (eg, hypertension, diabetes, dyslipidemia).
Concurrent use of, or within 2 wk of discontinuing, an MAOI; anorexia nervosa; concurrent use of other centrally acting appetite suppressants; allergy to sibutramine or any product component; uncontrolled or poorly controlled hypertension.
Dosage and AdministrationAdults and Children older than 16 yr of age
PO 10 mg once daily. May titrate to 15 mg/day after 4 wk if necessary.
Store at room temperature in a tightly closed container. Protect from heat and moisture.
Drug Interactions5-HT receptor agonists (eg, sumatriptan), bupropion, dextromethorphan, ergots (eg, dihydroergotamine), fentanyl, lithium, meperidine, pentazocine, SSRIs (eg, fluoxetine), tetracyclic antidepressants (eg, trazodone), tricyclic antidepressants (eg, amitriptyline), tryptophan
May precipitate “serotonin syndrome” if used concurrently with sibutramine. Avoid concurrent use.Centrally acting appetite suppressants (eg, prescription, OTC, and herbal products)
Concurrent use is contraindicated.Ephedrine, phenylpropanolamine, pseudoephedrine
Use with caution. Potential additive effects on BP and pulse.MAOIs
Do not use concomitantly with sibutramine. Separate therapy with either agent by at least 2 wk.
Laboratory Test Interactions
None well documented.
Tachycardia; vasodilation; hypertension; palpitations.
Headache; migraine; dizziness; nervousness; anxiety; depression; paresthesia; somnolence; CNS stimulation; emotional lability; agitation; hypertonia; abnormal thinking; insomnia.
Rash; sweating; herpes simplex; acne; pruritus.
Amblyopia; ear disorder; ear pain; rhinitis; sinusitis; laryngitis; pharyngitis.
Abdominal pain; anorexia; constipation; increased appetite; nausea; dyspepsia; gastritis; vomiting; rectal disorder; dry mouth; taste perversion; diarrhea; flatulence; gastroenteritis; tooth disorder; thirst.
Dysmenorrhea; urinary tract infection; vaginitis; metrorrhagia; menstrual disorder.
Cough; bronchitis; dyspnea.
Back, chest, or neck pain; flu syndrome; accidental injury; asthenia; allergic reactions; edema; arthralgia; myalgia; tenosynovitis; fever; leg cramps.
Category C .
Safety and efficacy in children younger than 16 yr of age not established.
Use with caution in patients older than 65 yr of age.
Do not use in patients with severe renal function impairment.
Do not use in patients with severe hepatic function impairment.
Sibutramine can cause tachycardia and hypertension. Use with caution in patients with a history of hypertension. Do not administer to patients with uncontrolled or poorly controlled hypertension.
Concomitant CV disease
Do not use in patients with a history of coronary artery disease, CHF, arrhythmias, or stroke.
Use with caution in patients with narrow angle glaucoma.
Use with caution in patients with a history of seizures. Discontinue use in any patient who develops seizures.
Weight loss can precipitate or exacerbate gallstone formation.
Carefully evaluate patients for a history of drug abuse. Follow such patients closely, observing for signs of misuse or abuse.
Primary pulmonary hypertension/Cardiac valve dysfunction
Although not reported with sibutramine, these have occurred in patients receiving certain other centrally-acting appetite suppressants.
- Advise patient to take drug daily as prescribed. Remind patient that it can be taken without regard to food.
- Instruct patient not to change the dose or discontinue therapy unless advised to do so by their health care provider.
- Encourage patient to follow medically supervised weight reduction program. Emphasize that this medication will only work in conjunction with a diet and exercise program.
- Advise patient to avoid alcohol and other CNS depressants.
- Emphasize importance of follow-up visits for monitoring BP and pulse as well as weight loss.
- Advise patient to contact their health care provider if they note any of the following: unexplained shortness of breath, swelling of ankles, decreased exercise tolerance, skin rash, hives, or other signs of an allergic reaction.
- Advise patient that drug may cause drowsiness or dizziness and to use caution while driving or performing other tasks requiring mental alertness.
- Advise women of childbearing potential to use an effective birth control method while on this drug.
- Instruct patient not to take any other medications (including OTC and herbal products) unless advised to do so by their health care provider. Many drugs can interact with sibutramine and cause potentially life-threatening reactions.
- Advise patient that safety of long term (longer than 1 yr) use has not been determined.
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