Goldlayn

General characteristics. Structure:

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

Excipients: lactose, cellulose microcrystallic, silicon dioxide colloid, magnesium stearate.

Structure of the case of the capsule: dye sunset yellow, dye quinoline yellow, titanium dioxide, sodium lauryl sulfate, gelatin.

Structure of a lid of the capsule: dye fuchsin acid (D&C33), dye diamond blue, titanium dioxide, sodium lauryl sulfate, gelatin.

Goldlayn – the drug of the central action used for treatment of alimentary obesity.

Pharmacological properties:

Pharmacodynamics. Sibutramin is pro-medicine and shows the action of in vivo at the expense of metabolites (primary and secondary amines) inhibiting the return capture of monoamines (preferential serotonin and noradrenaline).

Increase in contents in synapses of neurotransmitters increases activity of the central serotoninovy 5HT-receptors and adrenoceptors that promotes increase in feeling of saturation and decrease in food requirement, and also increase in thermoproducts. Indirectly activating β3-адренорецепторы, сибутрамин influences brown fatty tissue.

Decrease in body weight is followed by increase in concentration in LPVP blood serum and reduction in the amount of triglycerides, the general cholesterol, LPNP and uric acid.

Indications to use:

• alimentary obesity with the body weight index (BWI)> 30 kg/sq.m
• alimentary obesity with IMT more than 27 kg/sq.m in combination with a diabetes mellitus of type 2 or a dislipoproteinemiya.

Route of administration and doses:

Goldlayn is appointed in 1 times a day. The dose is established individually, depending on portability and clinical performance. The initial dose of 10 mg is recommended, at bad portability reception of 5 mg is possible. Capsules should be accepted in the morning, without chewing and washing down with enough liquid (a glass of water). Drug can be accepted as on an empty stomach, and to combine with meal. If within 4 weeks from an initiation of treatment decrease in body weight by 5% and more is not reached, then the dose increases to 15 mg/days.

Treatment by Goldlayn should not continue more than 3 months at patients who insufficiently well react to therapy i.e. which within 3 months of treatment do not manage to reach 5% of level of decrease in body weight of initial level. Treatment should not be continued if at further therapy, after the reached decrease in body weight, the patient adds in the body weight of 3 kg and more again. Duration of treatment should not exceed 2 years as concerning more long period of reception of a sibutramin data on efficiency and safety are absent.

Treatment by Goldlayn has to be performed in a complex with a diet and physical exercises under control of the doctor having practical experience of treatment of obesity.

Features of use:

Use during pregnancy and feeding by a breast. As so far there is no rather convincing number of researches concerning safety of impact of a sibutramin on a fruit, the yielded drug should not be used during pregnancy. The women who are in childbearing age during administration of drug Goldlayn have to use contraceptive means. It is not necessary to accept Goldlayn during feeding by a breast.

Goldlayn it is necessary to apply only when all non-drug actions for decrease in body weight are ineffective if decrease in body weight within 3 months made less than 5 kg.

Treatment by drug Goldlayn has to be performed within complex therapy on decrease in body weight under control of the doctor having practical experience of treatment of obesity. Complex therapy includes both change of a diet and a way of life, and increase in physical activity. An important component of therapy is creation of premises to permanent change of habits of food and a way of life which are necessary for preservation of the reached decrease in body weight and after cancellation of medicamentous therapy. It is necessary for patients within therapy by drug Goldlayn to change the way of life and habits so that after completion of treatment to provide preservation of the reached body degrowth. Patients have to have a clear view that non-compliance with these requirements will lead to repeated increase in body weight and repeated addresses to the attending physician.

At the patients accepting Goldlayn it is necessary to measure the ABP level and heart rate. In the first 2 months of treatment it is necessary to control these parameters each 2 weeks, and then monthly. At patients with arterial hypertension at whom against the background of hypotensive therapy the ABP level is higher than 145/90 mm of mercury., this control has to be carried out especially carefully and, if necessary, through shorter intervals. At patients at whom the ABP twice at repeated measurement exceeded the level of 145/90 mm of mercury., treatment by drug Goldlayn has to be suspended (See the section "Side effect. From cardiovascular system").

The special attention is required by co-administration of the drugs increasing QT interval. Blockers belong to these drugs H1-histamine receptors (астемизол, терфенадин); the antiarrhytmic drugs increasing QT interval (Amiodaronum, quinidine, флекаинид, мексилетин, пропафенон, соталол); stimulator of motility of digestive tract цизаприд; Pimozidum, сертиндол and tricyclic antidepressants. It concerns also states which are capable to lead to increase in an interval of QT, such as, a hypopotassemia and a hypomagnesiemia. (See also section "Interaction with Other Medicines").

Interval between reception of MAO inhibitors and drug Goldlayn has to make not less than 2 weeks. Though connection between administration of drug Goldlayn and development of primary pulmonary hypertensia is not established, however, considering well-known risk of drugs of this group, at regular medical control it is necessary to pay special attention to such symptoms as progressing dispny (breath disturbance), thorax pain and hypostases standing.

At the admission of a dose of drug Goldlayn, it is not necessary to accept a double dose of drug in the following reception, it is recommended to continue further administration of drug according to the ordered scheme.

Duration of reception of Goldlayn should not exceed 2 years.

Influence on ability to driving of motor transport, to control of mechanisms. Administration of drug Goldlayn can limit ability to driving of motor transport and control of mechanisms.

Side effects:

Most often side effects arise in an initiation of treatment (in the first 4 weeks). Their expressiveness and frequency weaken eventually. Side effects carry, in general, not difficult and reversible difficult character and, depending on impact on bodies and systems of bodies, are presented in the following order (often> 10%, sometimes 1-10%, are rare <1%).

From the central nervous system frequent side effects are dryness in a mouth and sleeplessness, the headache, dizziness, concern, paresthesias, and also taste change are sometimes noted.

From cardiovascular system tachycardia, heartbeat, increase in the ABP, symptoms of a vazodilatation including a dermahemia sometimes meet.

From system of digestive organs loss of appetite and a lock, sometimes nausea and an exacerbation of hemorrhoids are often observed.

From integuments perspiration is sometimes noted.

From immune system: allergic reactions of hypersensitivity from insignificant rash on skin and small tortoiseshells to a Quincke's disease and an anaphylaxis.

In isolated cases at treatment sibutraminy the following undesirable clinically significant phenomena are described: a dysmenorrhea, hypostases, a grippopodobny syndrome, a skin itch, a dorsodynia, an abdominal pain, paradoxical increase in appetite, thirst, rhinitis, a depression, drowsiness, emotional lability, uneasiness, irritability, nervousness, acute intersticial nephrite, bleedings, Shenleyn-Genokh's purpura (hemorrhages in skin), spasms, thrombocytopenia, tranzitorny increase in activity of "hepatic" enzymes in blood.

At one patient with schizoaffective disturbance which presumably existed prior to treatment after treatment acute psychosis developed.

Reactions to cancellation, such as headache or the increased appetite, are observed seldom. There are no data that after treatment the abstinence syndrome, a withdrawal or disturbances of mood is observed.

Changes of cardiovascular system. Moderate raising of the ABP at rest on 1-3 mm of mercury is observed. and moderate increase in pulse by 3-7 beats per minute. In some cases more expressed increases in the ABP and heart rate are not excluded. Clinically significant changes of the ABP level and pulse are registered preferential in an initiation of treatment (in the first 4-8 weeks).

Drug use Goldlayn at patients with the raised ABP: watch the section "Contraindications" and "Special Instructions".

Interaction with other medicines:

Inhibitors of a microsomal oxidation, including P450 3A4 inhibitors (кетоконазол, erythromycin, cyclosporine, etc.) raise in plasma of concentration of metabolites of a sibutramin with increase in heart rate and clinically insignificant increase in an interval of QT.

Rifampicin, antibiotics from group of macroleads, Phenytoinum, carbamazepine, phenobarbital and dexamethasone can accelerate metabolism of a sibutramin. Simultaneous use of several drugs increasing the content of serotonin in blood can lead to development of serious interaction.

The so-called serotoninovy syndrome can develop in rare instances at simultaneous use of drug Goldlayn with selective serotonin reuptake inhibitors (drugs for treatment of a depression), with some drugs for treatment of migraine (суматриптан, dihydroergotamine), with narcotic analgetics (pentazocine, pethidine, fentanyl), or antibechic drugs (dextromethorphan).

Sibutramin does not influence action of oral contraceptives.

The medicines increasing the ABP or heart rate (ephedrine, фенилпропаноламин, pseudoephedrine, and also combined medicines for treatment of "catarrhal" diseases containing these medicines), increase risk of increase in the ABP and heart rate.

At a concomitant use of a sibutramin and alcohol strengthening of negative effect of alcohol was not noted. However alcohol is not combined with the dietary actions recommended at reception of a sibutramin at all.

Contraindications:

• the established hypersensitivity to a sibutramin or to other components of drug;
• existence of the organic reasons of obesity (for example, hypothyroidism);
• serious violations of food – nervous anorexia or nervous bulimia;
• mental diseases;
• syndrome Gilles de la Turetta (generalized tics);
• a concomitant use of MAO inhibitors or their use within 2 weeks before purpose of drug Goldlayn; use of other drugs operating on the central nervous system (for example, antidepressants, neuroleptics); the drugs appointed at the sleep disorders containing tryptophane and also other drugs of the central action for decrease in body weight;
• coronary heart disease, dekompensirovanny chronic cordial insufficiency, inborn heart diseases, occlusal diseases of peripheral arteries, tachycardia, arrhythmia, cerebrovascular diseases (stroke, tranzitorny disturbances of cerebral circulation);
• uncontrollable arterial hypertension (the arterial pressure (AP) is higher than 145/90 mm of mercury.) (See also section "Special Instructions");
• thyrotoxicosis;
• heavy abnormal liver functions and/or kidneys;
• benign hyperplasia of a prostate;
• pheochromocytoma;
• closed-angle glaucoma;
• the established pharmacological, drug or alcohol addiction;
• pregnancy and period of feeding by a breast;
• the age up to 18 years is also more senior than 65 years.

With care: it is necessary to appoint drug at the following states: arrhythmia in the anamnesis, a chronic circulatory unefficiency, diseases of coronary arteries (including in the anamnesis), a cholelithiasis, arterial hypertension (controlled and in the anamnesis), neurologic disturbances, including a delay of intellectual development and a spasm (including in the anamnesis), an abnormal liver function and/or kidneys easy and moderate severity, motor and verbal tics in the anamnesis.

Overdose:

There are extremely limited data on an occasion of overdose of a sibutramin. Specific characters of overdose are unknown, nevertheless, it is necessary to consider a possibility of more expressed manifestation of side effects. It is necessary to inform the attending physician in case of alleged overdose.

The most often found adverse reactions connected with overdose of a sibutramin: tachycardia, increase in the ABP, headache, dizziness.

Treatment of any special treatment and specific antidotes does not exist. It is necessary to carry out the general actions: to provide free breath, to watch a condition of cardiovascular system, and also if necessary to perform the supporting symptomatic therapy. Timely use of absorbent carbon can reduce absorption of a sibutramin in intestines. The gastric lavage also reduces drug absorption. Patients with the raised ABP and tachycardia can appoint beta adrenoblockers. Efficiency of an artificial diuresis or hemodialysis is not established.

Storage conditions:

To store in the dry place at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to use after a period of validity.

Issue conditions:

According to the recipe

Packaging:

Mg capsules 10, 15. On 10 capsules in the blister from aluminum foil and PVC/PVdH of a film; 1 or 3 blisters together with the application instruction in a cardboard pack.