Goldline® (Goldliine)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceSibutramineSibutramine
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  • Goldline®
    capsules inwards 
    IZVARINO PHARMA, LLC     Russia
  • Slimia
    capsules inwards 
    TORRENT PHARMACEUTICALS LTD.     India
    • Dosage form: & nbsp
    capsules
    Composition:

    1 capsule contains:

    Capsules 10 mg:

    Active Ingredient: sibutramine hydrochloride monohydrate 10.00 mg.

    Inactive ingredients: lactose 232.00 mg, microcrystalline cellulose 30.00 mg, silicon dioxide colloid 1.00 mg, magnesium stearate 2.00 mg.

    Capsule shell:

    Cap: dye azorubin (E122), dye indigotine (E132), sodium lauryl sulfate, titanium dioxide, gelatin.

    Housing: dye sunset yellow (E110), dye quinoline yellow (E104), sodium lauryl sulfate, titanium dioxide, gelatin.

    Capsules 15 mg:

    Active Ingredient: sibutramine hydrochloride monohydrate 15 mg

    Inactive ingredients: lactose 227.00 mg, microcrystalline cellulose 30.00 mg, silicon dioxide colloid 1.00 mg, magnesium stearate 2.00 mg.

    Capsule shell:

    Cap: dye azorubin (E122), dye indigotine (E132), sodium lauryl sulfate, titanium dioxide, gelatin.

    Housing: sodium lauryl sulfate, titanium dioxide, gelatin.

    Description:

    Capsules 10 mg: hard gelatin capsules with a size of 2 with a blue lid and a yellow body, containing powder from white to almost white.

    Capsules 15 mg: hard gelatin capsules with a size of 2 with a blue lid and a white body, containing powder from white to almost white

    Pharmacotherapeutic group:Means for treating obesity
    ATX: & nbsp

    A.08.A.A   Preparations for the treatment of centralized obesity

    A.08.A.A.10   Sibutramine

    Pharmacodynamics:

    Sibutramine is a prodrug and shows its action in vivo due to metabolites (primary and secondary amines) inhibiting the reuptake of monoamines (mainly serotonin and norepinephrine). An increase in the content of neurotransmitters in the synapses increases the activity of central 5HT-serotonin and adrenergic receptors, which contributes to an increase in satiety and a decrease in the need for food, as well as an increase in thermal production. By indirectly activating beta3-adrenergic receptors, sibutramine affects the brown adipose tissue.

    The decrease in body weight is accompanied by an increase in the concentration in the blood serum of HDL and lowering the amount of triglycerides, total cholesterol, LDL and uric acid.

    Sibutramine and its metabolites do not affect the release of monoamines, do not inhibit monoamine oxidase (MAO); do not have an affinity for a large number of neurotransmitter receptors, including serotonin (5-HT1, 5-HT1A, 5-HT1AT, 5-HT2A, 5-HT2c), adrenergic (beta1, beta2, beta3, alpha1, alpha2), dopamine (D1, D2), muscarinic, histamine (H1), benzodiazepine and NMDAnd the receptors.

    Pharmacokinetics:

    After oral administration, it is rapidly absorbed from the gastrointestinal tract by at least 77%. At the "first passage" through the liver undergoes biotransformation under the influence of the isoenzyme cytochrome P450 ZA4 with the formation of two active metabolites (mono- and didesmethylsibutramine). After taking a single dose of 15 mg, the maximum concentration in the blood (Cmax) monodesmethylsibutramine is 4 ng / ml (3.2-4.8 ng / ml), didles methyl sibutramine - 6.4 ng / ml (5.6-7.2 ng / ml). FROMmax achieved after 1.2 hours (sibutramine), 3-4 h (active metabolites): Simultaneous food intake lowers FROMmax metabolites by 30% and increases the time of its achievement by 3 h without changing AUC. Quickly distributed to tissues. The connection with proteins is 97% (sibutramine) and 94% (mono- and didesmethylsibutramine). The equilibrium concentration of active metabolites in the blood is reached within 4 days after the start of treatment and approximately 2 times higher than the plasma level after taking a single dose. The half-life of sibutramine is 1.1 hours, monodesmethylsibutramine is 14 hours, and dides methyl sibutramine is 16 hours.Active metabolites undergo hydroxylation and conjugation with the formation of inactive metabolites, which are excreted mainly by the kidneys.

    Indications:
    • alimentary obesity with body mass index (BMI) of 30 kg / m2 and more;
    • Alimentary obesity with a BMI of 27 kg / m2 and more in combination with type 2 diabetes mellitus or dyslipoproteinemia.
    Contraindications:
    • established hypersensitivity to sibutramine or to other components of the drug;
    • the presence of organic causes of obesity (eg, Hypothyroidism);
    • severe eating disorders - anorexia nervosa or bulimia nervosa;
    • mental illness;
    • Gilles de la Tourette syndrome (generalized tics);
    • simultaneous administration of MAO inhibitors or their use within 2 weeks prior to the appointment of Goldline; the use of other drugs acting on the central nervous system (eg, antidepressants, neuroleptics); drugs prescribed for sleep disorders containing tryptophan, as well as other drugs of central action to reduce body weight;
    • ischemic heart disease, decompensated chronic heart failure, congenital heart disease,occlusive diseases of peripheral arteries, tachycardia, arrhythmia, cerebrovascular diseases (stroke, transient disorders of cerebral circulation);
    • uncontrolled arterial hypertension (blood pressure (BP) above 145/90 mm Hg) (See also section "Special instructions");
    • thyrotoxicosis;
    • severe dysfunction of the liver and / or kidney;
    • benign prostatic hyperplasia;
    • pheochromocytoma;
    • angle-closure glaucoma;
    • established pharmacological, narcotic or alcohol dependence;
    • pregnancy and the period of breastfeeding;
    • age 18 years and over 65 years
    Carefully:

    Caution should be given to the drug in the following conditions: history of an arrhythmia, chronic circulatory failure, coronary artery disease (including history), cholelithiasis, hypertension (controlled and in history), neurological disorders, including mental retardation and convulsions (including in the anamnesis), a violation of the liver and / or kidneys of mild and moderate severity, motor and verbal tics in the anamnesis.

    Pregnancy and lactation:

    Since there is not yet a sufficiently convincing amount of research on the safety of sibutramine exposure to fetuses, this drug should not be used during pregnancy.

    Women who are of childbearing age should use contraceptives while taking Goldline.

    Do not take Goldline while breastfeeding.

    Dosing and Administration:

    Goldline is prescribed inside once a day. The dose is set individually, depending on the tolerability and clinical effectiveness. An initial dose of 10 mg is recommended, with a poor tolerance of 5 mg. Capsules should be taken in the morning without chewing and drinking with a sufficient amount of liquid (a glass of water). The drug can be taken as an empty stomach or combined with a meal. If within 4 weeks from the beginning of treatment a decrease in body weight by 5% or more is not achieved, the dose increases to 15 mg / day.

    Treatment by Goldline should not last more than 3 months in patients who do not respond well enough to therapy, i.e. who during the 3 months of treatment can not achieve 5% of the level of weight loss from the baseline.Treatment should not be continued if, in further therapy, after the body weight reduction is achieved, the patient again adds 3 kg or more in the body mass. The duration of treatment should not exceed 2 years, since there is no data on efficacy and safety for a longer period of sibutramine intake.

    Treatment Goldlaynom should be carried out in conjunction with diet and exercise under the supervision of a doctor who has practical experience in the treatment of obesity.

    Side effects:

    Most often, side effects occur at the beginning of treatment (in the first 4 weeks). Their severity and frequency diminish over time. Side effects are generally of a non-severe and reversible nature and, depending on the effect on organs and organ systems, are presented in the following order (often> 10%, sometimes 1-10%, rarely < 1%).

    From the central nervous system frequent side effects are dry mouth and insomnia, sometimes headache, dizziness, anxiety, paresthesia, as well as a change in taste.

    From the side of the cardiovascular system Sometimes there are tachycardia, palpitations, increased blood pressure, symptoms of vasodilation including. hyperemia of the skin.

    On the part of the digestive system often there is loss of appetite and constipation, sometimes nausea and exacerbation of hemorrhoids.

    From the skin Sometimes sweating is noted.

    From the immune system: allergic hypersensitivity reactions from a minor rash on the skin and urticaria to angioedema and anaphylaxis.

    In single cases, the following undesirable clinically significant events are described in the treatment of sibutramine: dysmenorrhea, edema, flu-like syndrome, skin itching, back pain, abdominal pain, paradoxical appetite increase, thirst, rhinitis, depression, drowsiness, emotional lability, anxiety, irritability, nervousness, acute interstitial nephritis, bleeding, purpura Shenlen-Henoch (hemorrhages in the skin), convulsions, thrombocytopenia, transient increase in the activity of "hepatic" enzymes in the blood.

    In one patient with a schizo-affective disorder, which presumably existed before the start of treatment, acute psychosis developed after treatment.

    Reactions to cancellation, such as headache or increased appetite, are rare. There is no evidence that after treatment, there is an abstinence syndrome,withdrawal or mood disorder.

    Changes in the cardiovascular system

    There is a moderate rise in blood pressure at rest by 1-3 mm Hg. and a moderate increase in the pulse-at 3-7 beats per minute.

    In some cases, more pronounced increases in blood pressure and heart rate are not excluded. Clinically significant changes in blood pressure and pulse level are registered mainly at the beginning of treatment (in the first 4-8 weeks).

    Use Goldline in patients with elevated blood pressure: see the section "Contraindications" and "Special instructions."

    Overdose:

    There are extremely limited data on the overdose of sibutramine. Specific signs of an overdose are unknown, however, the possibility of a more pronounced manifestation of side effects should be taken into account. You should notify your doctor if there is an alleged overdose.

    The most common adverse reactions associated with overdose of sibutramine: tachycardia, increased blood pressure, headache, dizziness.

    Treatment there is no specific treatment or specific antidotes. It is necessary to carry out general measures: to ensure free dirsanie,monitor the state of the cardiovascular system, and also, if necessary, maintain symptomatic therapy. The timely use of activated charcoal can reduce sibutramine absorption in the intestine. Gastric lavage also reduces the absorption of the drug. Patients with elevated blood pressure and tachycardia can be prescribed beta-blockers. The effectiveness of forced diuresis or hemodialysis is not established.

    Interaction:

    Inhibitors of microsomal oxidation, incl. inhibitors P450 ZA4 (ketoconazole, erythromycin, ciclosporin and others) increase the concentration of metabolites in plasma sibutramine with an increase in heart rate and a clinically insignificant increase in the interval QT. Rifampicin, antibiotics from the macrolide group, phenytoin, carbamazepine, phenobarbital and dexamethasone can accelerate the metabolism of sibutramine. The simultaneous use of several drugs that increase serotonin levels in the blood can lead to the development of serious interaction. The so-called serotoninovys syndrome can develop in rare cases with simultaneous application of Goldline preparation with selective inhibitors of the inverseseizure of serotonin (drugs for the treatment of depression), with some drugs for the treatment of migraine (sumatriptan, dihydroergotamine), with narcotic analgesics (pentazocine, pethidine, fentanyl), or antitussive drugs (dextromethorphan).

    Sibutramine does not affect the effect of oral contraceptives.

    Drugs that increase blood pressure or heart rate (ephedrine, phenylpropanolamine, pseudoephedrine, as well as combined medicines for the treatment of "cold" diseases containing these drugs), increase the risk of increased blood pressure and heart rate.

    With the simultaneous administration of sibutramine and alcohol, there was no increase in the negative effect of alcohol. However, alcohol is absolutely not compatible with the recommended dietary measures when taking sibutramine.

    Special instructions:

    Goldline should be used only in those cases when all non-medicamentous measures to reduce body weight are ineffective if the weight loss within 3 months was less than 5 kg.

    Treatment Goldline should be carried out as part of a comprehensive therapy to reduce body weight under the supervision of a doctor who has practical experience in the treatment of obesity.Complex therapy includes how to change diet and lifestyle, and increase physical activity. An important component of therapy is the creation of prerequisites for a permanent change in eating habits and lifestyle that are necessary to maintain the achieved weight loss and after the abolition of drug therapy. Patients should, within the Goldline therapy, change their lifestyle and habits in such a way as to ensure that the achieved weight reduction is maintained after the treatment is completed. Patients should clearly realize that failure to comply with these requirements will lead to a second increase in body weight and repeated calls to the treating physician.

    In patients taking Goldline, it is necessary to measure blood pressure and heart rate. In the first 2 months of treatment, these parameters should be monitored every 2 weeks, and then monthly. In patients with hypertension who have a blood pressure level above 145/90 mm Hg on the background of antihypertensive therapy, this control should be carried out especially carefully and, if necessary, at shorter intervals.In patients whose blood pressure twice exceeded the level of 145/90 mm Hg twice, the treatment with Goldline should be suspended (see section "Side effect: from the cardiovascular system").

    Special attention should be paid to the simultaneous administration of drugs that increase the interval QT. These drugs are Hi-gistaminovyh receptors blockers (astemizole, Terfenadine); antiarrhythmic drugs that increase the interval QT (amiodorone, quinidine, flecainide, mexiletine, propafenone, sotalol); stimulator of gastrointestinal motility of cisapride; pimozide, sertindole and tricyclic antidepressants. This also applies to states that are capable of increasing the interval QT, such as hypokalemia and hypomagnesemia. (See also section "Interaction with Other Drugs").

    The interval between taking MAO inhibitors and Goldline preparation should be at least 2 weeks.

    Although there is no relationship between the administration of Goldline and the development of primary pulmonary hypertension, however, given the generally known risk of drugs in this group,with regular medical supervision, special attention should be paid to symptoms such as progressive dyspnea (breathing disorder), chest pain and swelling on the legs.

    If you miss a dose of Goldline, do not take the next dose of a double dose of the drug, it is recommended to continue taking the drug on a prescribed schedule.

    Duration of admission Oldline should not exceed 2 years.

    Effect on the ability to drive transp. cf. and fur:

    Taking Goldline can limit the ability to drive vehicles and manage mechanisms.

    Form release / dosage:

    Capsules 10, 15 mg.

    Packaging:10 capsules in a blister of aluminum foil and PVC / PVC film; 1,3, 6, 9 or 12 blisters together with instructions for use in a cardboard box.
    Storage conditions:

    In a dry place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-005820/09
    Date of registration:17.07.2009 / 20.03.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:IZVARINO PHARMA, LLC IZVARINO PHARMA, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspIZVARIN PHARMA LLC IZVARIN PHARMA LLC Russia
    Information update date: & nbsp23.04.2017
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