Sibutramine - instructions for use, analogs, reviews and release forms (powder hydrochloride monohydrate for the manufacture of drugs based on it) drugs for the treatment of obesity and weight loss in adults, children and pregnancy. Prohibited or authorized
In this article, you can read the instructions for using the drug Sibutramine. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Sibutramine in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Sibutramine in the presence of existing structural analogs.Use for the treatment of alimentary obesity and weight loss in adults, children, as well as during pregnancy and lactation. The drug is prohibited or permitted on the territory of Russia and in Europe.
Sibutramine - a tool for the treatment of obesity central action. The mechanism of action is due to selective inhibition of reuptake of serotonin and norepinephrine, to a lesser extent - dopamine. Accelerates the attack and prolongs the sense of saturation, which leads to a reduction in food intake. Increases energy consumption by stimulating thermogenesis through the mediated activation of beta3-adrenergic receptors. It acts on both sides of the energy balance and helps to reduce body weight.
Sibutramine and its metabolites do not release monoamines and are not MAO inhibitors, do not have an affinity for serotonergic, adrenergic, dopaminergic, muscarinic, histamine, benzodiazepine, and NMDA receptors.
Composition
Sibutramine hydrochloride monohydrate.
Pharmacokinetics
After ingestion sibutramine is rapidly absorbed from the digestive tract. Almost completely metabolized in the liver with the participation of isoenzymes of the cytochrome CYP3A4 system with the formation of mono- (dismethylsibutramine) and di-dimethyl (di-dimethylsibutramine) forms of active metabolites (M1 and M2),and also by hydroxylation and conjugation to form inactive metabolites. Quickly and well distributed in tissues. It is excreted mostly by kidneys in the form of inactive metabolites.
Indications
- in the supportive complex therapy of patients with excessive body weight with alimentary obesity with a body mass index of 30 kg / m 2 and more, with alimentary obesity with a body mass index of 27 kg / m 2 and more in the presence of other risk factors due to excessive body weight, in t.ch. Type 2 diabetes mellitus (non-insulin-dependent) or hyperlipidemia.
Forms of release
Substance powder (used to make preparations based on Sibutramine).
Instructions for use and reception scheme
The initial dose is 10 mg per day. With insufficient effectiveness when used in this dose (a decrease in body weight of less than 2 kg in 4 weeks) and with good tolerability, the dose can be increased to 15 mg per day.
In the absence of effect when administered at a dose of 15 mg per day (weight loss of less than 2 kg for 4 weeks) sibutramine should be discontinued.
In patients who do not adequately respond to ongoing therapy, i.e.who for 3 months can not reach 5% of the level of weight loss from the baseline, the duration of use should be no more than 3 months.
The course of treatment is no more than 1 year. There is no data on the efficacy and safety of longer-term use.
Do not continue to use, if after the achieved weight loss in the course of further therapy, the patient again adds a mass of 3 kg or more.
Side effect
- loss of appetite;
- constipation;
- dry mouth;
- nausea;
- insomnia;
- headache;
- dizziness;
- anxiety;
- paresthesia;
- increased sweating;
- change in taste;
- convulsive seizures;
- acute psychosis;
- tachycardia;
- a feeling of palpitations;
- increased blood pressure;
- vasodilation (redness of the skin with a sense of heat);
- exacerbation of hemorrhoids;
- acute interstitial nephritis;
- mesangiocapillary glomerulonephritis;
- thrombocytopenia;
- purple Shenlaine-Genocha.
Contraindications
- organic cause of obesity;
- known and established severe eating disorders (anorexia nervosa or bulimia nervosa);
- mental illness;
- Tourette's syndrome;
- IHD;
- chronic heart failure in the stage of decompensation;
- congenital heart defects;
- occlusive diseases of peripheral arteries;
- tachycardia;
- arrhythmias;
- disorders of cerebral circulation (including transient);
- uncontrolled arterial hypertension (blood pressure more than 145/90 mm Hg);
- hyperthyroidism;
- severe renal dysfunction;
- severe violations of liver function;
- benign prostatic hyperplasia with the formation of residual urine;
- pheochromocytoma;
- glaucoma;
- established pharmacological narcotic and alcohol dependence;
- pregnancy;
- lactation (breastfeeding);
- simultaneous administration or a period of up to 2 weeks after the abolition of MAO inhibitors or other drugs that have an inhibitory effect on the CNS (antidepressants, antipsychotics, tryptophan) or other medications to reduce body weight;
- hypersensitivity to sibutramine.
Application in pregnancy and lactation
Sibutramine is contraindicated in pregnancy and lactation (breast-feeding).
Women of childbearing age in the period of treatment should apply adequate methods of contraception.
special instructions
Apply only in cases where all measures to reduce body weight are ineffective (i.e.weight loss is less than 5 kg for 3 months).
Treatment should be conducted only 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 changing diet and lifestyle, and increasing physical activity. Thus, the prerequisites for a permanent change in eating habits and lifestyle are formed, which are necessary to maintain the achieved weight loss after the abolition of drug therapy.
With caution apply simultaneously with drugs that increase the QT interval in patients with hypokalemia and hypomagnesemia, epilepsy, with violations of the liver function of mild and moderate severity (because there may be an asymptomatic increase in the concentration of sibutramine in the blood plasma), with impaired renal function mild to moderate severity (because inactive metabolites are partially excreted by the kidneys), in patients with motor tics or vocalisms in a family history, concomitantly with drugs that increase blood pressure and heart rate (including medication by means of cough, allergy and colds).
On the territory of the Russian Federation, the drug based on Sibutramine (Reduxin) is included in the list of potent drugs that can be sold only for a special prescription of the doctor.
Do not use in people older than 65 years due to the lack of sufficient clinical experience with the use of sibutramine in geriatric patients.
During the treatment period it is necessary to control blood pressure and heart rate: in the first 2 months of therapy - every 2 weeks, then monthly. In patients with arterial hypertension (blood pressure more than 145/90 mm Hg), monitoring of these parameters should be carried out particularly carefully and, if necessary, more often. If blood pressure during repeated measurement twice exceeded 145/90 mm Hg, then sibutramine should be discontinued.
Regular medical supervision during treatment should pay attention to progressive dyspnea, chest pain and swelling, although the relationship between sibutramine intake and the development of primary pulmonary hypertension is not established.
Reactions to the abolition of sibutramine (headache, increased appetite) are rare.
During the treatment period, you should not drink alcohol because of the need to follow a diet.
Do not use in children and adolescents under the age of 18 due to lack of sufficient clinical experience in this category of patients.
Influence on the ability to drive vehicles and control mechanisms
At present, the influence of sibutramine on the ability to engage in potentially hazardous activities has not been established. However, it is impossible to exclude the possibility of such an impact. Use with caution in patients whose activities require increased attention and speed of psychomotor reactions.
Use of the drug in the US and European countries
In the United States, the drug is approved for use under the Meridia brand name, but only as directed by the doctor and with a large number of sales restrictions. The US Food and Drug Administration has conducted a study of 10,000 volunteers with varying degrees of obesity and, as a result of a significant number of deaths reported from Sibutramine, recommended the use of this drug only in absolutely healthy patients, without presence of problems with health, especially from the side of the cardiovascular system.
The implementation of sibutramine, used to treat obesity, is stopped in all EU countries.
The implementation of preparations based on sibutramine was discontinued in the Old World, as the European Committee on Medical Preparations discovered the negative effect of sibutramine on the cardiovascular system. To obtain such data, special studies were conducted with the participation of patients exposed to cardiovascular diseases.
Drug Interactions
When applied simultaneously with the means of inhibiting the activity of the isoenzyme CYP3A4 (ketoconazole, erythromycin, troleandomycin, cyclosporin) increased plasma concentration of metabolites of sibutramine, QT interval increases slightly.
With simultaneous use with rifampicin, phenytoin, carbamazepine, phenobarbital, dexamethasone, antibiotics of the macrolide group, it is possible to accelerate the metabolism of sibutramine.
While the use of selective serotonin reuptake inhibitors (with citalopram, fluoxetine, paroxetine, sertraline), agonists of 5-HT1-receptorsderivatives of alkaloids of ergot, opioid analgesics, antitussive agents of central action, the risk of developing serotonin syndrome increases.
Analogues of the drug Sibutramine
Structural analogs for the active ingredient and preparations containing Sibutramine:
- Goldline;
- Lindax;
- Meridia;
- Reduxine;
- Sibutramine hydrochloride monohydrate;
- Slimia.
Similar medicines:
Other medicines:
- Nifedipine - instructions for use, analogs, reviews and release forms (tablets and pills 10 mg, retard or prolonged 20 mg, capsules 5 mg and 10 mg) of the drug for the treatment of angina and depression in adults, children and pregnancy
- Gramdin - instructions for use, reviews, analogs and release forms (tablets for resorption with an anesthetic Neo and antibiotic) of a drug for the treatment of inflammatory diseases of the throat in adults, children and during pregnancy. Composition
- Coldrex - instructions for use, reviews, analogues and form of release (powder for the preparation HotRem, syrup Knight and Broncho, MaxGrip, Junior Hotdrink, tablets) medications for colds in adults, children and pregnancy. Composition