GOLDLAIN

Active material: Siʙutramin
When ATH: A08AA10
CCF: Anti-obesity medication centrally acting
ICD-10 codes (testimony): E66
When CSF: 16.02.01
Manufacturer: RANBAXY LABORATORIES Ltd. (India)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

Capsules hard gelatin, size №2, with a yellow body and a blue Cap; contents of capsules – powder from white to almost white.

Excipients: lactose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate.

The composition of the shell capsules: colorant sunset yellow, dye quinoline yellow, Titanium dioxide, sodium lauryl, gelatin.
The composition of the capsule caps: acidic fuchsin dye (D&C33), dye brilliant blue, Titanium dioxide, sodium lauryl, gelatin.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Capsules hard gelatin, size №2, with a white body and a blue cap; contents of capsules – powder from white to almost white.

Excipients: lactose, microcrystalline cellulose, colloidal silicon dioxide, magnesium stearate.

The composition of the shell capsules: Titanium dioxide, sodium lauryl, gelatin.
The composition of the capsule caps: acidic fuchsin dye (D&C33), dye brilliant blue, Titanium dioxide, sodium lauryl, gelatin.

10 PC. – blisters (1) – packs cardboard.
10 PC. – blisters (3) – packs cardboard.

Pharmacological action

Anti-obesity medication centrally acting. Sibutramine is a prodrug and exerts its effect in vivo due to metabolites (primary and secondary amines), inhibiting the reuptake of monoamines (primarily serotonin and norepinephrine). Increase in neurotransmission neurotransmitters increases the activity of Central serotonin receptor and adrenoceptor 5NT, which increases satiety and reduce the need for food, as well as an increase in termoproduktsii. Опосредованно активируя b₃-adrenoreceptory, Sibutramine acts on brown adipose tissue.

Decrease in body weight is accompanied by an increase in serum concentrations of HDL CHOLESTEROL and lowering the amount of triglycerides, total cholesterol, Engineers and uric acid.

Sibutramine and its metabolites do not affect the release of monoamines, not inhibit MAO, It has no affinity to a large number of neurotransmitter receptors, including serotonin (5NT₁-, 5HT_1A-, 5HT_1IN-, 5NT_2A-, 5NT_2C-), adrenergic (b₁-, b₂-, b₃-, a₁-, a₂-) , dopamine (D₁-, D₂-), muscarinic, histamine (H₁-), benzodiazepine and NMDA-receptors.

Pharmacokinetics

Absorption

After intake of rapidly absorbed from the digestive tract to not less than 77%. At “first pass” through the liver is biotransformation influenced izofermenta zitohroma r450 3A4 into two active metabolites (mono- and дидесметилсибутрамин). After administration of a single dose of 15 mg C_max monodesmetilsibutramina is 4 ng / ml (3.2-4.8 ng / ml), C_max didesmetilsibutramina – 6.4 ng / ml (5.6-7.2 ng / ml). T_max siʙutramina – 1.2 no, T_max active metabolite – 3-4 no. Simultaneous eating lowers (C)_max metabolites 30% and increases the time to achieve it 3 no, without changing the AUC.

Distribution

Rapidly distributed to the tissues. Protein binding is 97% (sibutramine) and 94% (mono- and дидесметилсибутрамин). C_ss active metabolites in blood reached within 4 days after treatment initiation, and approximately 2 times the plasma levels after administration of a single dose of.

Metabolism and excretion

T_1/2 siʙutramina – 1.1 no, monodesmetilsibutramina – 14 no, didesmetilsibutramina -16 no. Active metabolites are hydroxylation and conjugation with formation of inactive metabolites, which are derived mainly kidneys.

Testimony

- Alimentary obesity with a body mass index (BMI) ≥30 kg / m²;

— nutritional obesity with a BMI ≥ 27 kg / m² combined with diabetes mellitus type 2 or dislipoproteinemiej.

Dosage regimen

Goldline's appointed Interior 1 time / day. Dose set individually, depending on tolerability and clinical efficacy. Recommended initial dose 10 mg, bad Portability can receive 5 mg. The capsules should be taken in the morning, not chewing and drinking plenty of fluids (glass of water). The drug can be taken on an empty stomach, and combine with a meal. If within 4 weeks from the beginning of treatment not been reducing body mass on 5% and more, the dose is increased to 15 mg / day.

Goldlajnom treatment should not last for more than 3 months in patients, are not well respond to therapy, ie. that during the 3 months of treatment cannot reach 5% body weight reduction from baseline. Treatment should not continue, if further treatment, after achieved weight loss, the patient is re-gaining body weight 3 kg or more. The duration of treatment should not exceed 2 year, as for a more prolonged period of sibutramine data on efficacy and safety absent.

Goldlajnom treatment should be carried out in conjunction with diet and exercise under the supervision of a physician, have practical experience in the treatment of obesity.

Side effect

The most common side effects occur early in treatment (first 4 of the week). Their severity and frequency over time weaken.

Side effects are, generally, not heavy and reversible and, depending on the effects on organs and organ systems, are presented in the following order: often (>10%), sometimes (1-10%), rarely (< 1%).

CNS: often – insomnia; sometimes – headache, dizziness, anxiety, paresthesia.

Cardio-vascular system: sometimes – tachycardia, heartbeat, increased blood pressure, symptoms of vasodilation (incl. dermahemia), aggravation of hemorrhoids. There has been a moderate rise in blood pressure at rest on 1-3 mm Hg. Article. and a moderate increase in pulse on 3-7 u. / min. In some cases, are not excluded more severe increase in blood pressure and heart rate. Clinically significant changes in blood pressure and heart rate are recorded mainly in the beginning of treatment (first 4-8 weeks).

From the digestive system: often – dry mouth, loss of appetite and constipation; sometimes – nausea, change in taste.

Dermatological reactions: sometimes – increased perspiration.

In a few cases in the treatment of sibutraminom describes the following unwanted clinically important phenomenon: dysmenorrhoea, swelling, flu-like symptoms, itchy skin, backache, abdominal pain, paradoxical increased appetite, thirst, rhinitis, depression, drowsiness, emotional lability, anxiety, irritability, nervousness, acute interstitial nephritis, bleeding, purpura Shenleyn-Genoa (bleeding into the skin), convulsions, thrombocytopenia, tranzithornoe increase in liver enzymes in the blood.

One patient with schizoaffective disorder, which presumably existed prior to treatment, after treatment developed acute psychosis.

Reactions to cancel, such as headache or increased appetite, are rare.

There is no evidence, observed that after treatment withdrawal syndrome, withdrawal or mood disorders.

Contraindications

- Availability of organic causes of obesity (eg, gipotireoz);

-serious eating disorders (anorexia nervosa or bulimia nervosa);

- Mental illness;

- Syndrome of Gilles de la Tourette (generalized tics);

— the simultaneous admission of MAO inhibitors or using them for 2 weeks before the appointment of Goldline's drug;

- The use of other drugs, acting on the central nervous system (eg, Antidepressants, neuroleptics);

- The use of drugs, prescribed for sleep disorders, containing tryptophan, and other central acting drugs for weight loss;

- CHD, decompensated chronic heart failure, congenital heart disease, occlusive peripheral arterial disease, tachycardia, arrhythmia, cerebrovascular diseases (stroke, transient ischemic attacks);

- Uncontrolled hypertension (BP above 145/90 mm Hg. Art.);

- Thyrotoxicosis;

- Severe liver and / or kidney;

- Benign prostatic hyperplasia;

- Pheochromocytoma;

- Zakrыtougolynaya glaucoma;

-established pharmacological, drug or alcohol dependence;

- Pregnancy;

- Lactation (breast-feeding);

- Up to 18 and older 65 years;

- Established hypersensitivity to sibutramine or to other components of the drug.

FROM caution should be prescribed in the following states: arrhythmia in history, chronic circulatory insufficiency, coronary artery disease (incl. history), cholelithiasis, arterial hypertension (controlled and history), neurological disorders, including mental retardation and seizures (incl. history), violation of the liver and/or kidney mild, motor and verbal tics history.

Pregnancy and lactation

Because so far, there is no convincing enough amount of research about the safety effects of sibutramine on the fetus, This drug should not be used during pregnancy.

Goldline's should not be taken while breastfeeding.

Women of childbearing age During dose Goldline's should use must use contraceptives.

Cautions

Goldline's should only be applied in cases, when all non-pharmacological interventions to reduce body weight are ineffective, If the decrease in body weight during 3 months amounted to less 5 kg.

Goldline's treatment should be carried out within the framework of a comprehensive therapy for reducing body weight under the supervision of a physician, have practical experience in the treatment of obesity. Integrated therapy includes both changing diet and lifestyle, and increased physical activity. An important component of therapy is to create the prerequisites to permanent change in eating habits and lifestyle, needed to maintain the achieved weight loss after discontinuation of drug therapy. Patients must be under therapy with Goldline's change their lifestyles and habits so, After completion of treatment to ensure that made reducing body weight. Patients need to be clear about, that non-compliance will lead to re-weight gain and repeated appeals to the doctor.

Patients, Goldline's host, It is necessary to measure the levels of HELL and HR. First 2 months of treatment, these parameters should be monitored every 2 of the week, and then monthly. In patients with hypertension, which on the background of antihypertensive therapy blood pressure above 145/90 mm Hg. Art., This monitoring should be carried out carefully and, if necessary, at shorter intervals. Patients, whose blood pressure twice with repeated measurements exceed the level 145/90 mm Hg. Art., Goldline's treatment should be suspended.

Special attention should be given co-administration of drugs, prolonging the QT interval. These drugs include gistaminovykh blockers (H)₁-receptors (astemizol, terfenadine), antiarrhythmic drugs, prolonging the QT interval (amiodoron, quinidine, flekainid, mexiletine, propafenone, sotalol), cisapride, pimozid, sertindole and tricyclic antidepressants. This also applies to the States, that can increase the QT interval, such as, hypokalemia and hypomagnesemia.

The interval between receiving MAO inhibitors and drug Goldline's should not be less than 2 weeks.

Although not a link between taking the drug and development of Goldline's primary pulmonary hypertension, However, given the well-known risk of drugs of this group, with regular medical monitoring is necessary to pay special attention to symptoms, as a progressive dyspnea, chest pain and swelling in the legs.

In case of skipping the dose of Goldline's, should not be taken at the following reception of a double dose of this medication, recommended to accept further drug prescribed schema.

Goldline's reception duration should not exceed 2 years.

Effects on ability to drive vehicles and management mechanisms

Goldline's drug may limit the ability to drive vehicles and management mechanisms.

Overdose

There are very limited data on overdose of sibutramine. Specific signs of an overdose are not known, Nonetheless, should take into account the possibility of a more pronounced manifestations of side effects. You should notify your doctor in case of alleged overdose.

The most common following symptoms: tachycardia, increased blood pressure, headache, dizziness.

Treatment: special treatment and there are no specific antidotes. You must provide free breathing, monitor the state of the cardiovascular system, as well as the need to implement supportive symptomatic therapy. Timely application of activated charcoal may decrease the absorption of sibutramine in the gut. Gastric lavage also reduces the absorption of the drug. Patients with high arterial pressure and tachycardia can assign beta-adrenoblokatora. The effectiveness of forced diuresis or hemodialysis is not installed.

Drug Interactions

Inhibitors of microsomal oxidation, incl. inhibitors izofermenta CYP3A4 (ketoconazole, Erythromycin, cyclosporine), increase in plasma concentrations of metabolites of sibutramine with an increase in heart rate and clinically insignificant increase in the QT interval.

Rifampicin, macrolide antibiotics, phenytoin, Carbamazepine, phenobarbital and dexamethasone may accelerate the metabolism of sibutramine.

The simultaneous use of several drugs, increasing the concentration of serotonin in the blood, It can lead to serious interactions.

Serotonin syndrome can occur in rare cases while applying the product Goldline's with selective serotonin reuptake inhibitors (drugs for the treatment of depression), some drugs for treating migraine (sumatriptan, digidroergotamin), opioid analgesics (pentazocin, pethidine, Fentanyl) or antitussive drugs (dextromethorphan).

Sibutramine has no effect on the effect of oral contraceptives.

Drugs, raising hell or HR (ephedrine, phenylpropanolamine, Pseudoephedrine, as well as combined medicines for the treatment of colds, containing these drugs), increase the risk of ad and HR.

While receiving sibutramine and alcohol was no amplification negative action of ethanol. However, alcohol is absolutely not combined with recommended when taking sibutramina dietary interventions.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored in a dry, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 2 year.