Slimia (Slimia)

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: & nbspcapsules
    Composition:TOWaiting for the capsule contains: active substance: sibutramine hydrochloride monohydrate 10 or 15 mg; Excipients: lactose monohydrate 95.5 / 95.50 mg, cellulose

    microcrystalline 95.50 / 95.50 mg, sodium carboxymethyl starch 5.00 / 5.00 mg, silicon dioxide colloid 2.00 / 2.00 mg, magnesium stearate 2.00 / 2.00 mg; composition of an empty hard gelatin capsule: water

    14.5 ± 1.5 / 14.5 ± 1.5%, methyl parahydroxybenzoate 0.8 / 0.8%, propyl parahydroxybenzoate 0.2 / 0.2%, gelatin q.s. up to 100 % / q.s. up to 100%, sodium lauryl sulfate 0.08 / 0.08%, yellow quinoline dye 0.2100 / 0.5433%, titanium dioxide 5.85 / 1.6244%, dye floxin B

    0.033 / 0.0525%, coloring sunset sunset yellow 0.0060 / -%

    Description:

    10 mg: Hard gelatin capsule with a light orange lid and casing, containing white or almost white powder.

    15 mg: Hard gelatin capsule with orange lid and body, containing powder of white or almost white color.

    Pharmacotherapeutic group:obesity treatment
    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 MAO; do not have an affinity for a large number of neurotransmitter receptors, including serotonin (5-HT1, 5-HT1A, 5-HT1AT, 5-NT2A, 5-HT2c), adrenergic (beta1 beta2, beta3, alpha1, alpha2), dopamine (D1, D2), muscarinic, histamine (H1), benzodiazepine and NMDA receptors.

    Pharmacokinetics:

    After oral administration, it is rapidly absorbed from the digestive tract by at least 77%. When the "first pass" through the liverundergoes biotransformation under the influence of the cytochrome P450 isoenzyme 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) monodesmegylsibutramine is 4 ng / ml (3.2-4.8 ng / ml), didles methyl sibutramine - 6.4 ng / ml (5.6-7.2 ng / ml). Cmax is achieved after 1.2 hours (sibutramine), 3-4 hours (active metabolites). Simultaneous food intake lowers Сmах 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-14 hours, didesmethylsibutramine-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 Turegta syndrome (generalized tics);

    • simultaneous administration of MAO inhibitors or their use within 2 weeks before the appointment of the drug Slymia; 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 the peripheral arteries, tachycardia, arrhythmia, cerebrovascular diseases (stroke, transient disorders of cerebral circulation);
    • uncontrolled arterial hypertension (blood pressure (BP) above 145/90 mmHg).See also "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:

                        the drug should be prescribed under 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 seizures (in including a history), 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,During the reception of the drug, Slymia should use contraceptives.

                        Do not take the drug Slymia during breastfeeding.

                        Dosing and Administration:

                        Sibutramine is given orally once a day. The dose is set individually, depending on the tolerability and clinical effectiveness. An initial dose of 10 mg is recommended. 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 there is no reduction in body weight by 5% or more, the dose increases to 15 mg / day.

                        Treatment with Slymia 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 with the drug Slimia 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 light and reversible. Side effects, depending on the effect on organs and organ systems, are presented in the following order (often> 10%, sometimes 1-10%, rarely <1%). From the side of the central nervous system, frequent side effects are dry mouth and insomnia, sometimes headache, dizziness, anxiety, paresthesia, and taste change. From the cardiovascular system, tachycardia, palpitations, increased blood pressure, and symptoms of vasodilatation are sometimes observed. On the part of the digestive system, loss of appetite and constipation, and sometimes nausea and exacerbation of hemorrhoids, are observed. From the side of the skin, sweating is sometimes noted.

                        In isolated cases in the treatment with sibutramine the following undesirable clinically significant phenomena are described: dysmenorrhea,swelling, 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 Genocha (hemorrhages in skin), seizures, 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 abstinence syndrome, withdrawal or mood disorder occurs.

                        Changes in the cardiovascular system

                        There is a moderate rise in blood pressure at rest by 1-3 mm. gt; Art. and a moderate increase in heart rate 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 of Slymia 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.

                        Medical measures for overdose: there is no special treatment or specific antidotes. It is necessary to perform general measures: to ensure free breathing, to observe the state of the cardiovascular system, and also, if necessary, to maintain symptomatic therapy. The timely use of activated carbon can reduce the intake of sibutramine in the body. Gastric lavage can also have a beneficial effect. Patients with elevated blood pressure and tachycardia can be assigned beta-blockers. The effectiveness of forced diuresis or hemodialysis is not established.


                        Interaction:

                        Interaction with other drugs

                        Inhibitors of microsomal oxidation, incl.inhibitors P450 ZA4 (ketoconazole, erythromycin, ciclosporin , etc.) increase the plasma concentrations of sibutramin metabolites with an increase in heart rate and 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 serotonin syndrome may develop in rare cases with the simultaneous use of the Slymia preparation with selective serotonin reuptake inhibitors (drugs for the treatment of depression), with certain medications for the treatment of migraine (sumatriptan, dihydroergotamine), with potent analgesics (pentazocine, pethidine, fentanyl), or antitussive drugs (dextromethorphan). Drugs that increase blood pressure and / or heart rate (ephedrine, phenylpropanolamine, pseudoephedrine, and also combined drugs for the treatment of "catarrhal" diseases containing these drugs),increase the risk of increased blood pressure and heart rate.

                        Sibutramine does not affect the effect of oral contraceptives.

                        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 recommended dietary measures when taking sibutramine.

                        Special instructions:

                        Sibutramine 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 with Slymia should be carried out within the framework of complex therapy for weight loss under the supervision of a doctor who has practical experience in the treatment of obesity. Complex therapy includes both a change in diet and lifestyle, as well as an increase in 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 need to change their lifestyle and habits in the way of Slymia therapy in such a way that after the treatment is completed, the achieved reduction in body weight should be maintained.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.

                        Sibutramine 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 with Slymia should be carried out within the framework of complex therapy for weight loss under the supervision of a doctor who has practical experience in the treatment of obesity. Complex therapy includes both a change in diet and lifestyle, as well as an increase in 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 need to change their lifestyle and habits in the way of Slymia therapy in such a way that after the treatment is completed, the achieved reduction in body weight should be maintained. Patients should clearly understand,that non-observance of these requirements will lead to a repeated increase in body weight and repeated calls to the attending physician.

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

                        Reception of the drug Slymia may limit the ability to drive vehicles and manage mechanisms

                        Form release / dosage:

                        Capsules 10 mg, 15 mg.

                        10 capsules in an aluminum foil blister. 2,

                        3, 6 or 9 blisters in a cardboard box together

                        with instructions for use.

                        Packaging:

                        10 capsules in an aluminum foil blister. 2,

                        3, 6 or 9 blisters in a cardboard box together

                        with instructions for use.

                        Storage conditions:

                        Store at a temperature not higher than 30 ° C. Keep out of the reach of children.

                        Shelf life:3 years. Do not use at the expiration date indicated on the package.
                        Terms of leave from pharmacies:On prescription
                        Registration number:LSR-000591/09
                        Date of registration:29.01.2009
                        The owner of the registration certificate:TORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India
                        Manufacturer: & nbsp
                        Representation: & nbspTORRENT PHARMACEUTICALS LTD. TORRENT PHARMACEUTICALS LTD. India
                        Information update date: & nbsp18.05.2012
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