DRUGS & SUPPLEMENTS
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Lesfat is an drug for the treatment of central action obesity. The mechanism of action is due to selective inhibition of serotonin reuptake of norepinephrine and, to a lesser extent, of dopamine. This medication accelerates the onset and prolong satiety, which leads to a decrease in food consumption. It increases energy expenditure by stimulating thermogenesis mediated by activation of beta3-adrenergic receptors. Acts on both sides of the balance of energy and helps Lesfat body weight.
Sibutramine and its metabolites did not release monoamines, and they are not MAO inhibitors, have no affinity for serotonergic, adrenergic, dopaminergic, muscarinic, histamine, benzodiazepine and NMDA receptors.
After oral administration Lesfat is rapidly absorbed from the gastrointestinal tract. Almost completely metabolized in the liver, with the participation of cytochrome isozymes CYP3A4, as well as by hydroxylation and conjugation to form inactive metabolites. Cmax of sibutramine is achieved in 1.2 h. This medicine is quickly and widely distributed in tissues. The plasma protein binding is 97%. T1/2 is 1.1 h. Lesfat derived primarily by the kidneys as inactive metabolites.
As part of the supporting complex treatment of patients with overweight in alimentary obesity with a body mass index of 30 kg / m2 or more, with alimentary obesity with a body mass index of 27 kg / m2 or more in the presence of other risk factors due to overweight, including diabetes mellitus type 2, or hyperlipidemia.
The initial dose is 10 mg / day. With lack of effectiveness when used in this dose (weight loss less than 2 kg for 4 weeks) and if tolerated the dose can be increased to 15 mg / day.
If no effect when Lesfat used in doses of 15 mg / day (weight loss less than 2 kg per 4 weeks), this drug should be discontinued.
In patients not adequately responding to treatment, that is who within 3 months can not reach the level of 5% weight loss from baseline, the duration of use this medication should not exceed 3 months.
The course of treatment is not more than 1 year since no data on efficacy and safety of longer use.
Do not use sibutramine, if after made weight loss achieved in the course of further therapy, the patient again adds to the weight of 3 kg or more.
Digestive system: frequently - anorexia, constipation, dry mouth, nausea, transient increases in liver enzymes.
CNS and peripheral nervous system: insomnia, headaches, dizziness, anxiety, paresthesia, increased sweating, change in taste, seizures; one patient with schizoaffective disorder, which presumably existed prior to initiating therapy with sibutramine after treatment developed acute psychosis.
Cardiovascular system: tachycardia, palpitations, increased blood pressure, vasodilation (flushing with a sensation of heat), exacerbation of hemorrhoids; in some cases - a more pronounced increase in blood pressure and heart rate acceleration.
Urinary system: in rare cases - acute interstitial nephritis, mesangiocapillary glomerulonephritis.
Blood coagulation system: thrombocytopenia, Henoch-Schonlein purpura.
Most often side effects occur early in therapy (the first 4 weeks), their severity and frequency of occurrence over time are weaken.
Organic cause of obesity, well-known and established severe eating disorders (anorexia nervosa or bulimia nervosa), mental illness, Tourette syndrome, IBS, chronic heart failure in the stage of decompensation, congenital heart disease, occlusive peripheral artery disease, tachycardia, arrhythmias, cerebrovascular accident (including transient), uncontrolled hypertension (BP is more than 145/90 mm Hg), hyperthyroidism, severe renal dysfunction, severe hepatic dysfunction, benign prostatic hyperplasia with the formation of residual urine, pheochromocytoma, glaucoma, established pharmaceutical drug and alcohol abuse, pregnancy, lactation (breastfeeding), simultaneous taking or up to 2 weeks after discontinuation of MAO inhibitors or other drugs that have a dampening effect on the central nervous system (antidepressants, antipsychotics, tryptophan), or other medicines for weight loss, increased sensitivity to sibutramine.
Lesfat is contraindicated during pregnancy and lactation.
Women of childbearing age in the period of treatment should apply adequate methods of contraception.
Category of the fetus by FDA - C.
Use Lesfat only in cases where all activities are ineffective weight loss (when weight loss is less than 5 kg within 3 months).
Treatment should only be undertaken within the framework of the treatment of weight loss under medical supervision, which has practical experience in the treatment of obesity. Combined therapy includes both changes in diet and lifestyle and increased physical activity.
With caution use Lesfat in combination with drugs that increase the range of QT, in patients with hypokalemia and hypomagnesemia, epilepsy, impaired liver function with mild to moderate severity, with impaired renal function and mild to moderate severity, in patients with motor tics or family history of vocalism, simultaneously with drugs that increase blood pressure and heart rate (including medications used for coughs, colds and allergies).
Do not use in persons over 65 years due to lack of sufficient clinical experience with sibutramine in geriatrics.
Reactions to the cancellation of sibutramine (headache, increased appetite) are rare.
During the period of treatment you should not drink alcohol because of the need to diet.
Should not be used in children and adolescents under the age of 18 years due to lack of sufficient clinical experience with this category of patients.
There is currently no established effect on the ability of Lesfat to employment in potentially hazardous activities.
When this drug applied simultaneously with:
- drugs inhibiting isoenzyme CYP3A4 increased plasma concentrations of metabolites of sibutramine, slightly increased the interval of QT.
- rifampin, phenytoin, carbamazepine, phenobarbital, dexamethasone, macrolide antibiotics may accelerate the metabolism of this medication.
- selective serotonin reuptake inhibitors (citalopram, fluoxetine, paroxetine, sertraline), agonist 5-HT1-receptors, derivatives of ergot alkaloids, opioids, centrally acting antitussives increases the risk of serotonin syndrome.
Symptoms: increased severity of side effects, most often - tachycardia, increased blood pressure, headache and dizziness.
Treatment: taking activated charcoal, symptomatic therapy, monitoring of vital functions, if an increase in blood pressure and tachycardia - a prescription of beta-blockers.
Depending on the reaction of the Lesfat after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Lesfat not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.Is Lesfat addictive or habit forming?
Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.
Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.
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The information was verified by Dr. Rachana Salvi, MD Pharmacology