It exerts anorectic action by inhibiting the reuptake of both nor adrenaline and serotonin. It also stimulates thermogenesis by indirectly activating ß3 system in adipose tissue.
Pharmacokinetics
Absorption : About 77% of a dose is rapidly absorbed orally
Distribution: Widely distributed in the body (especially in to liver and kidney) in a protein bound form,
Metabolism : Metabolized in to active metabolites in the liver, Excretion: Excreted mainly through urine.
Adverse Effects
1. Dry mouth
2. Anxiety
3. Insomnia
4. Mood swings
5. Constipation
6. Chest pain
7. Mild increase in BP and heart rate
8. Altered liver function tests
9. Allergic reactions
ContraIndications
1. Hypersensitivity to the drug
2. In patient`s receiving MAO inhibitors
3. Patients receiving other centrally acting appetite suppressants
4. Anorexia nervosa
5. In patients with coronary artery diseases, heart failure, arrhythmias and stroke
6. Severe renal impairment
7. Severe hepatic impairment
8. History of Seizures
Special Precautions
1. Narrow angle glaucoma
2. Regularly monitors BP during therapy
3. Exclude organic causes of obesity like hypothyroidism
4. Avoid driving or using hazardous machinery which requires mental alertness
5. Hepatic impairment
6. Renal impairment
Pregnancy
Contraindicated
Breast Feeding
Contraindicated
Elderly
Use with caution
Children
Contraindicated
Interactions
CNS Active Drugs : Use with caution with other CNS active drugs. It should not be used with MAOIs. Atleast 2-weeks should elapse between discontinuation of a MAOI and initiation of treatment with sibutramine.
Drugs that may raise blood pressure and/or heart rate: Caution should be used when prescribing sibutramine to patients who use these medications.
Drugs that inhibit cytochrome P450 (3A4) metabolism (Erythromycin, ketoconazole): Concomitant administration of these drugs with sibutramine is not recommended since there is a potential for interaction.
Cimetidine: Efficacy of cimetidine enhanced.
Alcohol : Concomitant use with alcohol is not recommended.
Oral Contraceptives: Sibutramine does not inhibit suppression of ovulation by oral contraceptives.
Indications
Management of obesity, including weight loss and maintenance of weight loss; should be used in conjunction with a reduced calorie diet.
Dosage
Oral : 10mg once daily with or without food. Dose may increase to 15mg daily after 4 weeks if weight loss is inadequate. Patients who don`t tolerate the 10mg dose may receive 5mg daily. Should not use doses above 15mg daily.
Others
Schedule
NULL
Storage
Store at controlled room temperature at a range of 15 to 30 degree C. Protect from moisture, light, and excess heat. Keep out of reach of Children.
Missed Dose
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Over Dose
Provide supportive measures and symptomatic treatment. Establish air way, monitor cardiac and vital signs. Beta blockers may be use with caution to control elevated BP and tachycardia. |