Siʙutramin

When ATH:
A08AA10

Characteristic.

Sibutramine hydrochloride monohydrate - crystalline powder from white to cream color. Solubility in water: 2,9 mg / mL at pH 5,2. Distribution factor (octanol / water): 30,9 (pH 5,0). Molecular weight 334,33.

Pharmacological action.
Anoreksigennoe.

Application.

Comprehensive maintenance treatment of patients with overweight in the alimentary obesity with a body mass index of 30 kg / m² or more and with a body mass index of 27 kg / m² and more, but in the presence of other risk factors, due to overweight (diabetes mellitus type 2, dyslipoproteinemia).

Contraindications.

Hypersensitivity, the presence of organic causes of obesity, anorexia nervosa or bulimia nervosa, mental illness, syndrome Gilles de la Turetta, coronary artery disease, decompensated heart failure, congenital heart disease, occlusive peripheral arterial disease, tachycardia, arrhythmia, cerebrovascular diseases (stroke, transient ischemic attacks), arterial hypertension (FROM >145/90 mmHg.), hyperthyroidism, severe liver or kidney disease, benign prostatic hyperplasia, accompanied by the presence of residual urine, pheochromocytoma, glaucoma, established pharmacological, drug and alcohol dependence, simultaneous reception or for less than 2 weeks after discontinuation of MAO inhibitors or other drugs, acting on the central nervous system (incl. Antidepressants, neuroleptics, tryptophan), and other drugs for reducing body weight.

Restrictions apply.

Epilepsy, motor-flick verbalьnый (involuntary muscle contractions, violation artikulyatsii), children and old age (safety and efficacy in children under 18 years old and people over 65 years to be determined).

Pregnancy and breast-feeding.

When pregnancy is not recommended (adequate and well-controlled studies in women are not held).

Category actions result in FDA - C. (The study of reproduction in animals has revealed adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not held, However, the potential benefits, associated with drugs in pregnant, may justify its use, in spite of the possible risk.)

Unknown, It penetrates whether sibutramine and its metabolites in breast milk. During the period of breast-feeding is not recommended.

Side effects.

In placebo-controlled studies 9% patients, receiving sibutramine (n=2068) and 7% patients, placebo (n=884), stopped treatment because of side effects.

In placebo-controlled studies, the most common side effects were dry mouth, anorexia, insomnia, constipation, headache.

The following are the side effects, which were observed in patients, taking sibutramine, a frequency ≥1% and more often, than placebo. Next to the name contains the frequency of occurrence of side effects in the group treated with sibutramine, in brackets - the same data in the placebo group.

Body as a Whole: headache - 30,3% (18,6%), backache - 8,2% (5,5%), flu-like symptoms - 8,2% (5,8%), accidental injury - 5,9% (4,1%), asthenia - 5,9% (5,3%), abdominalьnaя fitting - 4,5% (3,6%), chest pain - 1,8% (1,2%), pain in the neck - 1,6% (1,1%), allergic reactions - 1,5% (0,8%).

Cardio-vascular system and blood (hematopoiesis, hemostasis): tachycardia - 2,6% (0,6%), vasodilation (flushing of the skin with a sensation of heat) - 2,4% (0,9%), Migraine - 2,4% (2,0%), hypertension / increased blood pressure - 2,1% (0,9%), palpitations - 2,0% (0,8%).

From the digestive tract: anorexia - 13,0% (3,5%), constipation - 11,5% (6,0%), increased appetite - 8,7% (2,7%), nausea - 5,9% (2,8%), dyspepsia - 5,0% (2,6%), gastritis - 1,7% (1,2%), thirst - 1,7% (0,9%), vomiting - 1,5% (1,4%), aggravation of hemorrhoids - 1,2% (0,5%).

On the part of the musculoskeletal system: arthralgia - 5,9% (5,0%), myalgia - 1,9% (1,1%), tenosynovitis - 1,2% (0,5%), diseases of the joints - 1,1% (0,6%).

From the nervous system and sensory organs: dry mouth - 17,2% (4,2%), Insomnia - 10,7% (4,5%), dizziness - 7,0% (3,4%), nervousness - 5,2% (2,9%), alarm - 4,5% (3,4%), Depression - 4,3% (2,5%), paraesthesia - 2,0% (0,5%), drowsiness - 1,7% (0,9%), excitement - 1,5% (0,5%), emotional lability - 1,3% (0,6%), change in taste - 2,2% (0,8%), diseases of the ear - 1,7% (0,9%), earache - 1,1% (0,7%).

From the respiratory system: Rhinitis - 10,2% (7,1%), pharyngitis - 10,0% (8,4%), sinusitis - 5,0% (2,6%), cough increased - 3,8% (3,3%), laryngitis - 1,3% (0,9%).

For the skin: rash - 3,8% (2,5%), sweating - 2,5% (0,9%), Herpes simplex - 1,3% (1,0%), Acne - 1,0% (0,8%).

With the genitourinary system: dysmenorrhea - 3,5% (1,4%), Urinary Tract Infection - 2,3% (2,0%), vaginal candidiasis - 1,2% (0,5%), metrorragija - 1,0% (0,8%).

Other: generalized edema - 1,2% (0,8%).

Cooperation.

Inhibitors of microsomal oxidation, incl. inhibitors of CYP3A4 cytochrome P450 (ketoconazole, Erythromycin, cyclosporin and others.) sibutramine reduced clearance. Funds, having serotonergic activity, increase the risk of serotonin syndrome (ažitaciâ, Sweating, diarrhea, fever, arrhythmia, convulsions, etc..).

Overdose.

Symptoms: increased severity of side effects, most often - tachycardia, increased blood pressure, headache and dizziness.

Treatment: administration of activated charcoal, simptomaticheskaya therapy, monitoring vital functions, with an increase in blood pressure and tachycardia - appointment of beta-blockers.

Dosing and Administration.

Inside, 1 once a day (morning), the initial dose - 10 mg (bad Portability can receive 5 mg); in the case of lack of effectiveness through 4 week increase the dose to 15 mg / day. Duration of treatment - 1 year.

Precautions.

It is necessary to control the level of blood pressure and heart rate every 2 in the first week 2 months of treatment, and then - 1 once a month. In patients with hypertension when blood pressure >145/90 mmHg. monitoring should be carried out carefully and more, in the case of double-registered rise in blood pressure >145/90 mmHg. treatment should be discontinued. The emergence during therapy of chest pain, progressive dyspnea (respiratory failure) and edema of the lower extremities may indicate the development of pulmonary hypertension (In this case, you must always consult a doctor).

It avoids simultaneous administration of drugs, prolonging the QT interval (astemizol, terfenadine, antiarrhythmic and other means), means, containing ephedrine, phenylpropanolamine, Pseudoephedrine etc.. (increase the risk of blood pressure and heart rate increase), and the other with a central anorectics mechanism of action. Precautions should be prescribed in the background gipokalie- and hypomagnesemia, in violation of liver and kidney function, and mild to moderate severity.

Women of childbearing age during treatment should use appropriate contraceptive measures.

It will be appreciated, that sibutramine may reduce saliva and contribute to the development of caries, periodontal disease, candidiasis and discomfort in the mouth. During treatment, it is recommended to limit the consumption of alcohol.

Should not be used during the drivers of vehicles and people, skills relate to the high concentration of attention.

Cautions.

Application is possible only in cases, when all other measures, aimed at the reduction of body weight, ineffective. Treatment should be under medical supervision, with experience correction obesity as part of combination therapy (diet, changes in eating habits and lifestyle, increasing physical activity). Reception period at a dose 15 mg should be limited in time.

Cooperation