Goldline Plus, 10 mg+158, 5 mg capsules 30 pcs

Goldline® PLUS is a combination drug, the action of which is due to its constituent components. Sibutramine is a prodrug and exerts its effect in vivo due to metabolites (primary and secondary amines) that inhibit monoamine reuptake (serotonin, norepinephrine, dopamine).

The increase of neurotransmitters in synapses increases the activity of central 5NT-serotonin and adrenergic receptors, which contributes to an increased feeling of satiety and decreased need for food, as well as increased heat production. By activating betaz-adrenoreceptors indirectly, sibutramine affects brown adipose tissue. Reduction of body weight is accompanied by an increase in plasma concentrations of high density lipoproteins (HDL) and a decrease in triglycerides, total cholesterol, low density lipoproteins (LDL) and uric acid.

Sibutramine and its metabolites do not affect the release of monoamines, do not inhibit monoamine oxidase (MAO); have low affinity for a large number of neurotransmitter receptors, including serotonin (5-HTi, 5-HTia, 5-HTm, b-NTgs), adrenergic (beta, betaz, alpha], alphag), dopamine (Di, D2), muscarinic, histamine (Hi), benzodiazepine and glutamate (NMDA) receptors.

Microcrystalline cellulose is an enterosorbent, has sorption properties and non-specific detoxifying action. It binds and removes from the body various microorganisms, products of their vital functions, toxins of exogenous and endogenous nature, allergens, xenobiotics and excess of certain metabolic products and metabolites responsible for the development of endogenous toxicosis.

Indications

Goldline® PLUS is indicated for weight loss in the following conditions:
nutritional obesity with a body mass index (BMI) of 30 kg/m2 or more;
nutritional obesity with a body mass index of 27 km/m2 or more in combination with type 2 diabetes mellitus and dyslipidemia.

Pharmacological effect

Goldline® PLUS is a combination drug, the effect of which is determined by the components included in its composition. Sibutramine is a prodrug and exhibits its effect in vivo due to metabolites (primary and secondary amines) that inhibit the reuptake of monoamines (serotonin, norepinephrine, dopamine).

An increase in the content of neurotransmitters in synapses increases the activity of central 5HT-serotonin and adrenergic receptors, which increases the feeling of satiety and reduces the need for food, as well as an increase in thermal production. By indirectly activating beta-adrenergic receptors, sibutramine acts on brown adipose tissue. A decrease in body weight is accompanied by an increase in plasma concentrations of high-density lipoproteins (HDL) and a decrease in the amount of triglycerides, total cholesterol, low-density lipoproteins (LDL) and uric acid.

Sibutramine and its metabolites do not affect the release of monoamines and do not inhibit monoamine oxidase (MAO); have low affinity for a large number of neurotransmitter receptors, including serotonin (5-HTi, 5-HTia, 5-HTm, b-HTgs), adrenergic (beta-betag, betaz, alpha], alphag), dopamine (Di, D2), muscarinic, histamine (Hi), benzodiazepine and glutamate (NMDA) receptors.

Microcrystalline cellulose is an enterosorbent, has sorption properties and a nonspecific detoxification effect. Binds and removes from the body various microorganisms, their metabolic products, toxins of exogenous and endogenous nature, allergens, xenobiotics, as well as an excess of certain metabolic products and metabolites responsible for the development of endogenous toxicosis.

Special instructions

Goldline® PLUS should be used only in cases where all non-drug measures for weight loss are ineffective – if the weight loss over 3 months is less than 5 kg.

Treatment with Goldline® PLUS should be carried out as part of complex weight loss therapy under the supervision of a physician with practical experience in the treatment of obesity. Complex therapy includes both changing diet and lifestyle, as well as increasing physical activity. An important component of therapy is to create the prerequisites for persistent changes in eating behavior and lifestyle, which are necessary to maintain the achieved weight loss even after drug therapy is discontinued. As part of treatment with Goldline® PLUS, patients need to change their lifestyle and habits in such a way as to ensure that the achieved weight loss is maintained after completion of treatment.

Patients should be clear that failure to comply with these requirements will lead to repeated weight gain and repeated visits to their doctor. Patients taking Goldline® PLUS should have their blood pressure and heart rate measured regularly. During the first 3 months of treatment, these parameters should be monitored every 2 weeks and then monthly. If during two consecutive visits an increase in resting heart rate >00910 beats per minute or systolic/diastolic pressure > 10 mm Hg is detected. Art., it is necessary to stop treatment. In patients with arterial hypertension whose blood pressure is above 145/90 mm Hg during antihypertensive therapy. Art., this control should be carried out especially carefully and, if necessary, at shorter intervals.

In patients whose blood pressure exceeded 145/90 mmHg twice during repeated measurements. Art., treatment with Goldline® PLUS should be discontinued (see section “Side effects”).

Blood pressure should be monitored especially carefully in patients with sleep apnea.

The simultaneous administration of drugs that increase the QT interval requires special attention. These drugs include Hi-histamine blockers (astemizole, terfenadine); antiarrhythmic drugs that increase the QT interval (amiodarone, quinidine, flecainide, mexiletine, propafenone, sotalol); gastrointestinal motility stimulator cisapride; pimozide, sertindole and tricyclic antidepressants. This also applies to conditions that can lead to an increase in the QT interval, such as hypokalemia and hypomagnesemia (see also section “Interaction with other drugs”).

The interval between taking MAO inhibitors (including furazolidone, procarbazine, selegiline) and Goldline® PLUS should be at least 2 weeks.

Although no connection has been established between taking sibutramine and the development of primary pulmonary hypertension, however, given the well-known risk of drugs in this group, with regular medical monitoring it is necessary to pay special attention to symptoms such as progressive dyspnea (breathing difficulty), chest pain and swelling in the legs.

If you miss a dose of Goldline® PLUS, you should not take a double dose of the drug at the next dose; it is recommended to continue taking the drug according to the prescribed regimen.

The duration of taking Goldline® PLUS should not exceed 1 year.

When taking sibutramine and other serotonin reuptake inhibitors together, there is an increased risk of bleeding. In patients predisposed to bleeding or taking drugs that affect hemostasis or platelet function, sibutramine should be used with caution.

Although there is no clinical evidence of addiction to sibutramine, the patient’s history of drug dependence should be assessed and attention should be paid to possible signs of drug abuse.

Effect on the ability to drive vehicles and machinery Taking Goldline® PLUS may limit the ability to drive vehicles and machinery. During the period of use of the drug Goldline® PLUS, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Sibutramine, microcrystalline cellulose

Composition

Active substances:

sibutramine hydrochloride monohydrate,

microcrystalline cellulose.

Excipients:

calcium stearate – 1.5 mg.

Composition of the capsule shell:

cap:

Azorubine dye (E122) – 0.0570%;

indigo carmine (E132) – 0.3079%;

sodium lauryl sulfate – 0.0800%;

titanium dioxide – 1.0000%;

gelatin – up to 100%.

Housing:

sodium lauryl sulfate – 0.0800%;

titanium dioxide – 2.0000%;

gelatin – up to 100%.

Contraindications

Known hypersensitivity to sibutramine or other components of the drug;
The presence of organic causes of obesity (for example, hypothyroidism);
Serious eating disorders – anorexia nervosa or bulimia nervosa;
Mental illnesses;
Gilles de la Tourette syndrome (generalized tics);
Concomitant use of MAO inhibitors (for example, phentermine, fenfluramine, dexfenfluramine, ethylamphetamine, ephedrine) or use within 2 weeks before taking the drug Goldline® PLUS and 2 weeks after the end of its use of other drugs acting on the central nervous system, inhibiting the reuptake of serotonin (for example, antidepressants, antipsychotics); sleeping pills containing tryptophan, as well as other centrally acting drugs for weight loss or for the treatment of mental disorders;

Cardiovascular diseases (history or current): coronary heart disease (myocardial infarction (MI), angina); chronic heart failure in the stage of decompensation, occlusive diseases of peripheral arteries, tachycardia, arrhythmia, cerebrovascular diseases (stroke, transient cerebrovascular accidents);
Uncontrolled arterial hypertension (blood pressure (BP) above 145/90 mm Hg) (see also section “Special instructions”);
Angle-closure glaucoma;
Thyrotoxicosis;
Severe liver and/or kidney dysfunction;
Benign prostatic hyperplasia;
Pheochromocytoma;
Established pharmacological, drug or alcohol dependence;
Pregnancy and breastfeeding period;
Age under 18 and over 65 years.

The drug should be prescribed with caution in the following conditions: a history of arrhythmias, chronic circulatory failure, coronary artery diseases (including a history), except for coronary heart disease (MI, angina); glaucoma, except for angle-closure glaucoma, cholelithiasis, arterial hypertension (controlled and in history), neurological disorders, including mental retardation and seizures (including in history), epilepsy, mild to moderate liver and/or kidney dysfunction, history of motor and verbal tics, tendency to bleeding, bleeding disorders, taking medications, affecting hemostasis or platelet function.

Side Effects

Most side effects when taking Goldline Plus are observed during the first month of use; they are not severe, do not require pharmacological correction and go away on their own after a month.

The main side effects observed are: dry mouth, insomnia, headache, dizziness, anxiety, increased heart rate, increased blood pressure, loss of appetite, constipation, nausea, increased sweating.

Interaction

Inhibitors of microsomal oxidation, incl. inhibitors of the CYP3A4 isoenzyme (ketoconazole, erythromycin, cyclosporine, etc.) increase plasma concentrations of sibutramine metabolites with an increase in heart rate and a clinically insignificant increase in the QT interval. Rifampicin, macrolide antibiotics, phenytoin, carbamazepine, phenobarbital and dexamethasone can accelerate the metabolism of sibutramine.

The simultaneous use of several drugs that increase the level of serotonin in the blood plasma can lead to the development of serious interactions. The so-called serotonin syndrome can develop in rare cases when sibutramine is used simultaneously with selective serotonin reuptake inhibitors (drugs for the treatment of depression), with certain drugs for the treatment of migraines (sumatriptan, dihydroergotamine), with potent analgesics (pentazocine, pethidine, fentanyl) or antitussive drugs (dextromethorphan). Sibutramine does not affect the effect of oral contraceptives.

When sibutramine and alcohol were taken simultaneously, there was no increase in the negative effects of alcohol. However, alcohol is absolutely not compatible with the dietary measures recommended when taking sibutramine.

When used simultaneously with sibutramine, other drugs that affect hemostasis or platelet function increase the risk of bleeding. Drug interactions with the simultaneous use of sibutramine with drugs that increase blood pressure and heart rate have not been fully studied at present.

This group of drugs includes decongestants, cough suppressants, cold and allergy medications that contain ephedrine or pseudoephedrine. Therefore, in cases of simultaneous use of these drugs with sibutramine, caution should be exercised. The combined use of sibutramine with drugs for weight loss that act on the central nervous system or drugs for the treatment of mental disorders is contraindicated.

Manufacturer

Izvarino Pharma, Russia