Xenalten
Xsenalten: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Xenalten
ATX code: A08AB01
Active ingredient: orlistat (orlistat)
Producer: Obolensk pharmaceutical company, CJSC (Russia)
Description and photo updated: 2018-23-11
Prices in pharmacies: from 676 rubles.
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Xsenalten - a drug for the treatment of obesity, is an inhibitor of lipases in the digestive tract.
Release form and composition
Ksenalten is produced in the form of capsules: size No. 1, blue body and lid; content - almost white or white granules (7 or 21 pcs. in blister strip packs, in a carton box 1, 2, 3, 4, 6 or 12 packs).
1 capsule (with an average weight of the filler - 240 mg) contains:
- active substance: orlistat - 120 mg;
- auxiliary components: microcrystalline cellulose (MCC) - 59.6 mg; sodium carboxymethyl starch (sodium starch glycolate) - 38 mg; sodium lauryl sulfate - 10 mg; talc - 2.4 mg; povidone - 10 mg;
- capsule cap and body: gelatin, titanium dioxide, patented blue dye.
Pharmacological properties
Pharmacodynamics
The active component of Xsenalten, orlistat, is a specific inhibitor of gastrointestinal lipases. It creates a covalent bond with the active serine site of gastric and pancreatic lipases in the lumen of the stomach and small intestine, as a result of which inactivated enzymes lose their ability to break down dietary fats in the form of triglycerides. Triglycerides that have not been cleaved are not absorbed, resulting in a decrease in caloric intake in the body, which leads to weight loss. 24-48 hours after taking orlistat increases the content of fat in the feces. It provides a reduction in body fat, allowing you to effectively control body weight.
There is no need for systemic absorption of orlistat for its activity. Acceptance of the recommended therapeutic dose (120 mg 3 times a day) inhibits the absorption of lipids from food by about 30%.
Pharmacokinetics
Orlistat is extremely low in absorption. 8 hours after taking Xonalten inside, the concentration of unchanged orlistat is less than 5 ng / ml, so its determination in plasma is not possible.
Orlistat systemic exposure rates are also minimal. After oral administration of 360 mg of isotope 14 C-orlistat, the plasma peak of its radioactivity is reached after 8 hours, and the concentration of unchanged orlistat approaches the detection limit (<5ng / ml). In the course of therapeutic studies, which included the evaluation of patient plasma samples, unchanged orlistat was detected sporadically in it, and its level was low (<10 ng / ml), without signs of deposition, which confirms the minimal absorption of the drug.
During in vitro laboratory studies, it was determined that orlistat binds to plasma proteins by more than 99% (mainly with albumin and lipoproteins). The substance penetrates into erythrocytes minimally. Its metabolism occurs mainly in the walls of the gastrointestinal tract (gastrointestinal tract), resulting in the formation of pharmacologically inactive metabolites M1 (hydrolyzed four-membered lactone ring) and M3 (M1 with a cleaved N-formylleucine residue).
In a study of obese patients who took 14 C-orlistat orally, the total plasma radioactivity was provided by 42% of its two metabolites - M1 and MZ, which have an open β-lactone ring and exhibit extremely weak inhibitory activity against lipases (weaker, respectively, in 1000 and 2500 times in comparison with orlistat). The level of metabolites in plasma 2–4 hours after oral administration of therapeutic doses of orlistat is about 26 ng / ml and 108 ng / ml, respectively. Given the low activity and low plasma concentration of these metabolites, they are considered to be pharmacologically insignificant.
The half-life (T 1/2) of the main metabolite (M1) is about 3 hours, the second metabolite (M3) is excreted more slowly, its T 1/2 is 13.5 hours. In obese patients, C ss (equilibrium concentration) M1 (but not MZ) increases according to the increase in the dose of orlistat. As a result of a single dose of 360 mg 14C-orlistat inside with normal body weight and obesity, unabsorbed orlistat was mainly excreted through the intestines with feces - about 97%, of which 83% - unchanged. Partially, orlistat and its metabolites are also excreted in the bile; less than 2% of the substance is excreted through the kidneys. The time for complete elimination of orlistat with urine and feces is from 3 to 5 days. Orlistat excretion was similar in patients with normal weight and obesity. According to limited data, the absorbed orlistat T 1/2 ranges from 1 to 2 hours.
Indications for use
According to the instructions, Xsenalten is recommended to be used in combination with a hypocaloric diet for the treatment of obesity, including reduction and maintenance of body weight, as well as to reduce the risk of re-gaining weight after its initial loss.
Ksenalten prescribed to patients with a BMI of obesity (BMI) ≥ 30 kg / m 2 or BMI ≥ 28 kg / m 2 with the presence of concomitant risk factors (hypertension, diabetes, dyslipidemia).
The BMI is calculated according to the formula: BMI = M / P 2 (M - body weight in kg, P - height in m).
Contraindications
Absolute:
- cholestasis;
- malabsorption syndrome;
- simultaneous reception with cyclosporine;
- pregnancy and breastfeeding;
- age under 18;
- increased individual sensitivity to orlistat or any other components of Xsenalten.
The drug is used with caution in the presence of nephrolithiasis (calcium oxalate stones) and a history of hyperoxaluria.
Xsenalten instructions for use: method and dosage
Xsenalten capsules are taken orally during each meal or no later than one hour after a meal.
The recommended dosage of Xsenalten for adult patients: 120 mg (1 capsule) 3 times a day.
You can skip the capsule if you eat a fat-free meal.
The maximum duration of therapy is 2 years.
Side effects
The frequency of side effects was determined in accordance with the following gradation: very often - more than 0.1%; often - more than 0.01%, but less than 0.1%; sometimes - more than 0.001%, but less than 0.01%; rarely - more than 0.0001%, but less than 0.001%; extremely rare - less than 0.0001%, including individual messages.
Adverse reactions from systems and organs:
- digestive tract: very often - steatorrhea, imperative urge to defecate, discharge of gas and some discharge, discharge of oily substance from the rectum, pain / discomfort in the abdomen, loose stools, increased frequency of bowel movements, flatulence [as a rule, these adverse reactions are mild and transient (occurring in the early stages of therapy, usually in the first 3 months); with an increase in the dietary fat content, the frequency of such adverse reactions increases, in connection with which patients should be informed about the possibility of their occurrence and explained that their elimination is carried out by better adherence to the diet, in particular by reducing the amount of fat contained in the food]; often - pain / discomfort in the rectum, soft stools, fecal incontinence, bloating, damage to the gums / teeth;
- respiratory system, mediastinal and chest organs: very often - infection of the upper respiratory tract; often - infection of the lower respiratory tract;
- immune system: rarely - urticaria, itching, rash, bronchospasm, angioedema, anaphylaxis;
- nervous system: very often - headache;
- hepatobiliary system: extremely rarely - an increase in the activity of hepatic transaminases and alkaline phosphatase, hepatitis;
- genitourinary system: often - urinary tract infections;
- other reactions: very often - flu; often - anxiety, dysmenorrhea, weakness.
In case of aggravation of any of the indicated side effects or the occurrence of other reactions not specified in the instructions, you should inform your doctor.
Overdose
Overdose cases of orlistat have not been described.
In obese patients and people with normal weight, no clinically significant adverse reactions were observed due to a single oral administration of orlistat at a dose of 800 mg or its repeated administration 3 times a day at doses up to 400 mg (for 15 days).
If a significant overdose of orlistat is detected during the day, monitoring the patient's condition is required. Data from animal and human studies have shown a rapid reversibility of systemic effects associated with orlistat's ability to inhibit lipase.
special instructions
During therapy, a balanced hypocaloric diet is required, containing no more than 30% fat, enriched with vegetables and fruits. The content of vitamin D and β-carotene in obesity may be lower than in normal body weight. If it is necessary to compensate for the decrease in the absorption of fat-soluble vitamins, an additional course of multivitamin preparations is possible, which should be taken with Xsenalten, observing a 2-hour interval between their doses, for example, before bedtime.
Before prescribing Xsenalten, it is important to exclude organic and hormonal causes of excess weight, for example, hypothyroidism.
It is necessary to distribute the daily intake of fats, proteins and carbohydrates between the three main meals. But it is important to take into account that when food contains more than 30% of the daily calorie content in the form of fats, the likelihood of side effects from the gastrointestinal tract increases.
Taking Xsenalten in doses of more than 120 mg 3 times a day does not provide an additional effect.
When it is impossible to avoid the simultaneous administration of orlistat and cyclosporine, it is necessary to constantly monitor the plasma level of the latter.
According to the results of observations, patients who did not receive vitamin supplements for the prevention of vitamin deficiency demonstrated a reduced level of vitamins in plasma [with consecutive visits to the doctor (two or more) during two years of orlistat therapy].
In some cases, with the use of Xonalten, an increase in the level of oxalates in the urine may be observed.
As with other weight-loss drugs, patients with anorexia nervosa or bulimia nervosa may be prone to abuse Xenalten.
Orlistat can reduce the absorption of vitamin K, therefore, patients taking Xsenalten against the background of long-term constant treatment with warfarin need to monitor blood coagulation parameters.
In connection with the induction of a decrease in body weight by orlistat, it is possible to improve the metabolic control of diabetes mellitus, which may require adjusting the doses of oral hypoglycemic agents (metformin, sulfonylurea derivatives, etc.) or insulin in the direction of their reduction.
The question of the need to continue therapy with Xsenalten, provided that after 3 months of taking the drug, the decrease in body weight is less than 5%, is decided after consulting a specialist.
Influence on the ability to drive vehicles and complex mechanisms
Xsenalten does not affect the ability of patients to drive vehicles and perform other types of work that require the mobilization of motor and mental reactions.
Application during pregnancy and lactation
- pregnancy: it is contraindicated to use Xsenalten due to the lack of reliable data confirming its safety for the mother and fetus;
- lactation: not recommended during breastfeeding, since it has not been reliably established whether the drug passes into breast milk.
Pediatric use
Xsenalten is not used in pediatric practice.
Drug interactions
- digoxin, amitriptyline, phenytoin, fluoxetine, sibutramine, atorvastatin, pravastatin, nifedipine, losartan, glibenclamide, furosemide, captopril, atenolol and ethanol: no clinically significant interactions were observed;
- cyclosporine: its plasma level decreases (simultaneous administration is not recommended; to reduce the likelihood of drug interaction, cyclosporine should be taken 2 hours before or 2 hours after orlistat);
- warfarin, other indirect anticoagulants: a decrease in the level of prothrombin and a change in the MHO indicator (international normalized ratio) is possible, which requires regular monitoring of its indicator;
- β-carotene contained in food additives: orlistat reduces its absorption by 30%;
- vitamin E (in the form of α-tocopherol acetate): orlistat inhibits its absorption by about 60%;
- pravastatin: its bioavailability and hypolipidemic effect increase, its concentration in plasma increases by 30%;
- vitamins A, D, E and K: orlistat reduces their absorption (multivitamins should be taken 2 hours before or 2 hours after taking Xsenalten, for example, before bedtime);
- acarbose: simultaneous use is not recommended due to the lack of information about the pharmacokinetic interaction with orlistat;
- amiodarone: a decrease in its plasma level was noted after a single use, the combination is possible only on the recommendation of a specialist;
- oral contraceptives: orlistat is able to indirectly reduce their bioavailability, reducing the contraceptive effect, which may result in the development of unwanted pregnancy; with the development of acute diarrhea, it is recommended to use additional methods of protection.
Analogs
Analogs of Xsenalten are: Garcinia-Forte, Listata, Orsoten, Orsoten Slim, Xenical, Listata Mini, LiDa Premium, Meridia, Momordica Harantskaya, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dry, dark place. Keep out of the reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Xenalten
In most positive reviews, Xsenalten is called an effective and safe weight loss product with a fairly quick result. It is noted that at the same time the vessels are cleaned from toxins and cholesterol, in addition, Xsenalten is less expensive compared to similar means for getting rid of excess weight.
As a disadvantage, most patients note fatty oily stools, especially after overeating fatty foods. But it must be borne in mind that the manufacturer warns about this side effect in the instructions and makes recommendations to reduce the likelihood of its manifestation.
Price for Xsenalten in pharmacies
Estimated price of Xsenalten: 21 pcs. in the package - 720 rubles; 42 pcs. - 1135 rubles; 84 pcs. - 2070 rubles.
Xsenalten: prices in online pharmacies
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Drug name Price Pharmacy |
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Xsenalten caps. 120mg n21 RUB 676 Buy |
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Xsenalten 120 mg capsules 21 pcs. RUB 676 Buy |
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Xsenalten caps. 120mg n42 820 RUB Buy |
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Xenalten 120 mg capsules 42 pcs. 820 RUB Buy |
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Xsenalten 120 mg capsules 84 pcs. 1494 RUB Buy |
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Xsenalten caps. 120mg n84 1591 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
