Slimiya

General characteristics. Structure:

Active ingredient: 10 mg or 15 mg of a sibutramin of a hydrochloride monohydrate.

Pharmacological properties:

Pharmacodynamics. Means for treatment of obesity of the central action. The mechanism of action is caused by the selection inhibition of the return serotonin reuptake and noradrenaline, to a lesser extent - a dopamine. Accelerates approach and prolongs feeling of saturation that leads to reduction of consumption of food. Increases power consumption due to stimulation of thermogenesis by the mediated activation β3-адренорецепторов. Affects both parties of balance of energy and promotes decrease in body weight.

Sibutramin and his metabolites do not release monoamines and are not MAO inhibitors, also NMDA to receptors have no affinity to serotonergic, adrenergic, dopaminergic, muskarinovy, histamine, benzodiazepine.

Pharmacokinetics. After intake сибутрамин it is quickly absorbed from a GIT. It is almost completely metabolized in a liver with the participation of isoenzymes of system of CYP3A4 cytochrome with education mono - (дисметилсибутрамин) and di-dismetil (di-dismetilsibutramin) of forms of active metabolites (M1 and Sq.m), and also by a hydroxylation and a konjyugirovaniye with formation of inactive metabolites. Cmax of a sibutramin is reached in 1.2 h, M1 and Sq.m – in 3-4 h Cmax of M1 and Sq.m after a single dose inside in a dose of 15 mg – 4 ng/ml (3.2-4.8 ng/ml) and 6.4 ng/ml (5.6-7.2 ng/ml) respectively. Reception with food increases time of achievement of Cmax and reduces the size Cmax dismetit metabolites on 3 h and 30% respectively; does not influence the size AUC dismetit metabolites. It is quickly and well distributed in fabrics. Linkng with proteins of plasma: сибутрамин – 97%, M1 and Sq.m – 94%. T1/2 of a sibutramin is 1.1 h, M1 – 14 h, Sq.m – 16 h. It is removed, generally by kidneys in the form of inactive metabolites.

At a renal failure the key pharmacokinetic parameters (Cmax, T1/2, AUC) a sibutramin and its active metabolites significantly do not change.

Indications to use:

As a part of the supporting complex therapy of patients with excess body weight at alimentary obesity with a body weight index from 30 kg/sq.m and more, at alimentary obesity with a body weight index from 27 kg/sq.m and more with other risk factors caused by excess body weight including a diabetes mellitus of type 2 (non-insulin-dependent) or lipidemias.

Route of administration and doses:

The initial dose makes 10 mg. At insufficient efficiency at use in this dose (decrease in body weight less than on 2 kg in 4 weeks) and at good tolerance a dose can be increased to 15 mg.

In the absence of effect at use in a dose of 15 mg. (decrease in body weight less than 2 kg in 4 weeks) сибутрамин should be cancelled.

At the patients who insufficiently are adequately reacting to the carried-out therapy i.e. at which within 3 months it is not possible to reach 5% of level of decrease in body weight of initial level duration of use has to make no more than 3 months.

The course of treatment makes no more than 1 year since there are no data on efficiency and safety of more long use.

It is not necessary to continue use if after the reached decrease in body weight during further therapy the patient adds in weight of 3 kg and more again.

Features of use:

Use during pregnancy. At pregnancy it is not recommended (adequate and strictly controlled researches at women are not conducted).

Category of action on a fruit on FDA — C. It is unknown whether gets сибутрамин and its metabolites into breast milk. During breastfeeding use is not recommended.

It is necessary to control the ABP level and pulse rate each 2 weeks in the first 2 months of treatment and then — once a month. At patients with arterial hypertension at the ABP level> 145/90 mm hg control has to be exercised more carefully and more often, and in case of twice registered raising of the ABP> 145/90 mm hg treatment should be stopped. Emergence during therapy of pain in a thorax, progressing диспноэ (breath disturbance) and hypostases of the lower extremities can indicate development of pulmonary hypertensia (in this case it is necessary to see surely a doctor).

The concomitant use of the drugs increasing QT interval (астемизол, терфенадин, antiarrhytmic and other means), the means containing ephedrine, фенилпропаноламин, pseudoephedrine, etc. (danger of increase in the ABP and increase in ChSS), and also other anorexigenic means with the central mechanism of action is not recommended. With care it is necessary to appoint against the background of gipokaliye-and hypomagnesiemia, at an abnormal liver function and kidneys easy and moderate severity.

Women of childbearing age during treatment have to use adequate measures of contraception.

It must be kept in mind what сибутрамин can reduce salivation and promote development of caries, periodontal diseases, candidiasis and discomfort in an oral cavity. During treatment it is recommended to limit alcohol intake.

It is not necessary to apply in operating time to drivers of vehicles and people whose profession is connected with the increased concentration of attention.

Special instructions at reception. Use is possible only when all other actions directed to decrease in body weight are ineffective. Treatment has to be performed under control of the doctor having experience of correction of obesity within complex therapy (a diet, change of habits of food and a way of life, increase in physical activity). The reception period in a dose of 15 mg has to be limited in time.

Side effects:

In placebo - controlled researches of 9% of the patients receiving сибутрамин (n=2068) and 7% of the patients receiving placebos (n=884) stopped treatment because of emergence of side effects.

In placebo - controlled researches dryness in a mouth, anorexia, an insomniya, a lock, a headache were the most frequent side effects.

Further side effects which were noted at the patients accepting сибутрамин with a frequency of 1% are specified and it is more frequent, than in group of placebo. Near the name the frequency of occurrence of this side effect in group accepting сибутрамин, in brackets — similar data in group of placebo is specified.

Organism in general: a headache — 30,3% (18,6%), a dorsodynia — 8,2% (5,5%), a grippopodobny syndrome — 8,2% (5,8%), an accidental injury — 5,9% (4,1%), an adynamy — 5,9% (5,3%), abdominal pain — 4,5% (3,6%), a stethalgia — 1,8% (1,2%), neck pain — 1,6% (1,1%), allergic reactions — 1,5% (0,8%).

From cardiovascular system and blood (a hemopoiesis, a hemostasis): tachycardia — 2,6% (0,6%), a vazodilatation (a dermahemia with a caumesthesia) — 2,4% (0,9%), migraine — 2,4% (2,0%), hypertensia/increase in the ABP — 2,1% (0,9%), heartbeat — 2,0% (0,8%).

From bodies of a GIT: anorexia — 13,0% (3,5%), a lock — 11,5% (6,0%), increase in 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%), an exacerbation of hemorrhoids — 1,2% (0,5%).

From a musculoskeletal system: the arthralgia — 5,9% (5,0%), a mialgiya — 1,9% (1,1%), tendosinovit — 1,2% (0,5%), diseases of joints — 1,1% (0,6%).

From a nervous system and sense bodys: dryness in a mouth — 17,2% (4,2%), an insomniya — 10,7% (4,5%), dizziness — 7,0% (3,4%), nervousness — 5,2% (2,9%), alarm — 4,5% (3,4%), a depression — 4,3% (2,5%), paresthesia — 2,0% (0,5%), drowsiness — 1,7% (0,9%), excitement — 1,5% (0,5%), emotional lability — 1,3% (0,6%), taste change — 2,2% (0,8%), ear diseases — 1,7% (0,9%), ear pain — 1,1% (0,7%).

From respiratory system: rhinitis — 10,2% (7,1%), pharyngitis — 10,0% (8,4%), sinusitis — 5,0% (2,6%), strengthening of cough — 3,8% (3,3%), laryngitis — 1,3% (0,9%).

From integuments: rash — 3,8% (2,5%), perspiration — 2,5% (0,9%), Herpes simplex — 1,3% (1,0%), an acne — 1,0% (0,8%).

From urinogenital system: a dysmenorrhea — 3,5% (1,4%), infections of urinary tract — 2,3% (2,0%), vaginal candidiasis — 1,2% (0,5%), a metrorrhagia — 1,0% (0,8%).

Others: generalized hypostasis — 1,2% (0,8%).

Interaction with other medicines:

At simultaneous use with the means inhibiting activity of an isoenzyme of CYP3A4 (кетоконазол, erythromycin, тролеандомицин, cyclosporine) concentration in plasma of metabolites of a sibutramin increase, QT interval slightly increases.

At simultaneous use with rifampicin, Phenytoinum, carbamazepine, phenobarbital, dexamethasone, antibiotics of group of macroleads acceleration of metabolism of a sibutramin is possible.

At simultaneous use with selective serotonin reuptake inhibitors (with tsitalopramy, fluoxetine, paroksetiny, sertraline), agonists of 5-HT1-receptors, derivatives of alkaloids of an ergot, opioid analgetics, antibechics of the central action the risk of development of a serotoninovy syndrome increases.

Contraindications:

Hypersensitivity, existence of the organic reasons of obesity, nervous anorexia or nervous bulimia, mental diseases, Giles de la Tourett's syndrome, coronary heart disease, dekompensirovanny heart failure, inborn heart diseases, occlusal diseases of peripheral arteries, tachycardia, arrhythmia, cerebrovascular diseases (stroke, tranzitorny disturbances of cerebral circulation), arterial hypertension (the ABP> of 145/90 mm hg), a hyperthyroidism, heavy abnormal liver functions or kidneys, the benign hyperplasia of a prostate which is followed by existence of a residual urine, a pheochromocytoma, glaucoma, the established pharmacological, drug and alcohol addiction, a concomitant use or the period less than 2 weeks after cancellation of the MAO inhibitors or other drugs operating on TsNS (including antidepressants, neuroleptics, tryptophane), and also other drugs for a body degrowth.

Storage conditions:

To store at a temperature not above 30 °C in places, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

- capsules of 10 mg; blister 10 pack cardboard 2; - capsules of 10 mg; blister 10 pack cardboard 3; - capsules of 15 mg; blister 10 pack cardboard 2; - capsules of 15 mg; blister 10 pack cardboard 3