Expiration date: 04/2026

Active substance (per 1 capsule):

• sibutramine hydrochloride monohydrate is 10 mg or 15
  
• microcrystalline cellulose 158.5 or 153.5 mg
  

Other ingredients: calcium stearate.

Description pharmaceutical form:

10 mg capsules: cyan.

15 mg capsules: blue.

The contents of capsules - powder white or white with a slightly yellowish tint.

Pharmacokinetics:

After intake of rapidly absorbed from the gastrointestinal tract is not less than 77%. The first passage through the liver biotransformation under the influence of isoenzyme of cytochrome P4503A4 with the formation of two active metabolites (mono and didesmetilsibutramin). After administration of a single dose of 15 mg monodesmetilsibutramina blood Cmax is 4 ng / mL (3.2-4.8 ng / ml) didesmetilsibutramina - 6.4 ng / ml (5,6-7,2 ng / ml). Cmax is reached after 1.2 hours (for sibutramine), 3-4 hours (for the active metabolites). Simultaneous eating reduces Cmax of metabolites by 30% and increases the time to achieve 3 hours, without changing the AUC. Quickly spread to tissues. Protein binding is 97% (for sibutramine) and 94% (for mono and didesmetilsibutramina). CSS active metabolites in blood is achieved within 4 days after the initiation of treatment, and about 2 times higher than the plasma levels after administration of a single dose.

T1 / 2 of sibutramine - 1.1 hours, monodesmetilsibutramina - 14 hours didesmetilsibutramina -. 16 h active metabolites are hydroxylation and conjugation to inactive metabolites that are excreted primarily by the kidneys.

Description of the pharmacological actions:

Reduxine - combined drug whose action is due to its constituent components.

Sibutramine is a prodrug and exerts its effects in vivo due to metabolites (primary and secondary amines) which inhibit the reuptake of monoamines (norepinephrine, serotonin and preferably).

The increase of neurotransmitters in the synapses increases the activity of central serotonin (5HT), and adrenergic receptor, which helps to increase satiety and reduce the need for food, as well as an increase in termoproduktsii. Indirectly activating &, beta3-adrenergic receptors, sibutramine affects the brown adipose tissue. Weight loss accompanied by an increase in serum HDL concentration and decreasing amounts of triglycerides, total cholesterol, LDL cholesterol, and uric acid. Sibutramine and its metabolites have no effect on the release of monoamines, do not inhibit MAO not have an affinity for a large number of neurotransmitter receptors, including serotonergic (5-HT1, 5-HT1A, 5-NT1V, 5-HT2A, 5-HT2C), adrenergic (beta1- , beta2, beta3, alpha1, alpha2), dopamine (D, D2), muscarinic, histamine (H1), and NMDA-benzodiazepine receptors.

Microcrystalline cellulose is enterosorbent has sorption properties and non-specific detoxification effect. Associates and displays the body of a variety of microorganisms, their metabolic products, toxins exogenous and endogenous nature, allergens, xenobiotics, as well as an excess of certain metabolic products and metabolites responsible for the development of endogenous toxicosis.

Testimony:

Reduxine shown to reduce body weight under the following conditions:

• alimentary obesity with a body mass index (BMI) of 30 kg / m2 or more
  
• alimentary obesity with a BMI of 27 kg / m2 or more, if there are other risk factors are overweight, such as type 2 diabetes or dislipoproteinemia (violation of lipid metabolism).
  

Contraindications:

• established hypersensitivity to sibutramine or to other components of the drug
  
• the presence of organic causes of obesity (eg hypothyroidism)
  
• serious eating disorders (anorexia nervosa or bulimia nervosa)
  
• mental illness
  
• Gilles de la Tourette syndrome (generalized tics)
  
• simultaneous reception of MAO inhibitors (for example, phentermine, fenfluramine, dexfenfluramine, ethylamphetamine, ephedrine) or using them for 2 weeks prior to the appointment of the drug Reduxine
  
• the use of other drugs acting on the CNS (such as antidepressants, neuroleptics) drugs prescribed sleep disorders, containing tryptophan and other centrally acting drugs for weight loss
  
• Coronary artery disease, decompensated chronic heart failure, congenital heart disease, peripheral arterial occlusive disease, tachycardia, arrhythmia, cerebrovascular disease (stroke, transient ischemic attacks)
  
• uncontrolled hypertension (blood pressure above 145/90 mm Hg -... see also "Special Instructions" section)
  
• thyrotoxicosis
  
• severe liver and / or kidney disease
  
• benign prostatic hyperplasia
  
• pheochromocytoma
  
• angle-closure glaucoma
  
• established pharmaceutical, drug or alcohol dependence
  
• pregnancy
  
• lactation
  
• age 18 years and older than 65 years.
  

Precautions should be prescribed the drug under the following conditions:

• arrhythmia history
  
• chronic circulatory insufficiency
  
• coronary artery disease (including history)
  
• cholelithiasis
  
• hypertension (controlled and history)
  
• neurological disorders, including mental retardation and seizures (including history)
  
• liver and / or kidney disease and mild to moderate severity
  
• motor and verbal tics history.
  

Application of pregnancy and breastfeeding:

Because so far there is not enough convincing number of studies on the safety of sibutramine impact on the fetus, this drug should not be used during pregnancy.

Women who are of childbearing age during treatment Reduxine should use contraceptives.

Do not take Reduxine during breastfeeding.

Side effect:

Most often side effects occur at the beginning of treatment (first 4 weeks). Their severity and frequency over time weakens. Side effects are generally not heavy and reversible. Side effects, depending on the effects on organs and organ systems in the following order (often -> 10%, sometimes - 1.10%, rare - <1%). p = "">,

CNS: often - dry mouth, insomnia, sometimes - headache, dizziness, anxiety, paresthesia, and changes in taste.

Since the cardiovascular system: sometimes - tachycardia, palpitations, increased blood pressure, vasodilatation.

On the part of the digestive system: common - loss of appetite, constipation, sometimes - nausea, exacerbation of hemorrhoids. When a tendency to constipation in the early days should be monitored for the evacuation of bowel function. If you have constipation reception stop and take a laxative.

For the skin: sometimes - sweating.

In rare cases, the treatment with sibutramine describes the following undesirable clinically significant phenomenon: dysmenorrhea, edema, flu syndrome, skin itching, back pain, abdominal pain, paradoxically increased appetite, thirst, rhinitis, depression, lethargy, emotional lability, anxiety, irritability, anxiety, acute interstitial nephritis, bleeding-Henoch purpura (bleeding into the skin), seizures, thrombocytopenia, transient 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 the cancellation, such as headache or increased appetite, are rare. There is no evidence that observed after treatment withdrawal, withdrawal, or mood disorder.

Changes in the cardiovascular system

There has been a moderate rise in blood pressure at rest for 1-3 mm Hg and moderate increase in heart rate at 3-7 bpm. In some cases, it is not excluded more marked increase in blood pressure and heart rate. Clinically significant changes in blood pressure and heart rate are recorded primarily in the treatment of early (within the first 4-8 weeks). Application Reduxine the drug in patients with elevated blood pressure - see section "Contraindications" and "Cautions"..

Drug Interactions:

Microsomal oxidation inhibitors, including inhibitors P4503A4 (ketoconazole, erythromycin, cyclosporine, etc..), increases in plasma concentrations of metabolites of sibutramine with an increase in heart rate and clinically insignificant increase in the QT interval.

Rifampicin, antibiotics, macrolide, phenytoin, carbamazepine, phenobarbital, and dexamethasone may accelerate sibutramine metabolism. Simultaneous use of several drugs that increase serotonin in the blood, can lead to serious interactions. In rare cases, the concomitant use of Reduxine medication with selective serotonin reuptake inhibitors (drugs for the treatment of depression), certain drugs for the treatment of migraine (sumatriptan, dihydroergotamine), potent analgesics (pentazocine, pethidine, fentanyl), or antitussive drug (dextromethorphan) can develop the so-called serotonin syndrome.

Sibutramine has no effect on the effect of oral contraceptives.

At the same time taking sibutramine and alcohol was not observed amplification of negative effects of alcohol. However, alcohol is absolutely not compatible with the recommended dietary measures taking sibutramine.

Dosage and administration:

Inside, 1 time a day, in the morning, without chewing and drinking plenty of fluids (a glass of water). The drug can be taken on an empty stomach or with a meal mix.

The dosage is determined individually depending on the tolerability and clinical efficacy. The recommended initial dose - 10 mg, with poor tolerance can receive 5 mg. If within 4 weeks of starting treatment is not achieved weight loss of 5% or more, the dose increases to 15 mg / day.

Treatment with Reduxine should not last longer than three months in patients who are not adequately respond to therapy, i.e. that within 3 months of treatment fails to reach the level of 5% reduction in body weight from baseline. Treatment should not be continued, if further therapy after weight loss achieved, the patient's body weight increased by 3 kg or more.

The duration of treatment should not exceed 2 years, as regards longer period sibutramine receiving data on efficacy and safety are absent.

Treatment with Reduxine should be administered in combination with diet and exercise under the supervision of a doctor having experience of treatment of obesity.

Overdose:

Symptoms: There are very limited data about sibutramine overdose. Specific signs overdose unknown, however the possibility should be considered a more pronounced manifestation of side effects. Patients should notify their physician in case of suspected overdose. In case of overdose may increase the severity of side effects.

Treatment: any special treatment, and there is no specific antidotes. It is necessary to carry out the general measures: to provide free breathing, observe the state of the cardiovascular system, as well as to supporting the symptomatic therapy if necessary. Appointment of activated charcoal, gastric lavage, with increased blood pressure and tachycardia - appointment &, beta-blockers. The effectiveness of forced diuresis or hemodialysis has not been established.

Special instructions:

Reduxine should be used only in cases where all the non-pharmacological interventions to reduce weight are ineffective - if the body weight reduction for 3 months was less than 5 kg.

Treatment with Reduxine should be carried out within the framework of a comprehensive therapy for reducing under medical supervision body weight, having practical experience in the treatment of obesity.

Complex therapy includes both changes in diet and lifestyle, and increasing physical activity.

An important component of therapy is to create prerequisites to permanent changes in eating habits and lifestyle, which are necessary to preserve the achieved weight loss after discontinuation of drug therapy. Patients must be drug therapy within Reduxine change their way of life and habits so that after treatment to ensure the preservation of body weight reduction achieved.

Patients should clearly understand that failure to comply with these demands will lead to re-weight gain and repeated appeals to the doctor.

Patients taking Reduxine, 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 - on a monthly basis. Patients with hypertension whose antihypertensive therapy on a background of blood pressure above 145/90 mm Hg. Art., this control must be carried out very carefully and, if necessary, at shorter intervals. Patients whose blood pressure measured twice during the second level higher than 145/90 mm Hg. Art., Treatment with Reduxine should be suspended (see "Side Effects." - "Changes in the cardiovascular system").

Special attention should be given co-administration of drugs that increase the QT interval. These medications include blockers of histamine H1 receptors (astemizole, terfenadine) antiarrhythmic drugs, increase the interval QT (amiodoron, quinidine, flecainide, mexiletine, propafenone, sotalol) GI motility stimulant cisapride pimozide, sertindole, and tricyclic antidepressants. This also applies to conditions that could lead to an increase in the QT interval (hypokalemia and hypomagnesemia - see "Interactions" section.).

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

Although no association between the intake of the drug Reduxine and development of 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 such as progressive dyspnoea (breathlessness), chest pain and swelling in the legs .

Omitting Reduxine dose of the drug should not be taken in the following method a double dose of the drug, it is recommended to continue the further reception scheme prescribed drug.

Duration of Reduxine drug should not exceed 2 years.

Effects on ability to drive vehicles, management mechanisms. Admission Reduxine drug may limit the ability to drive vehicles and management mechanisms.