Dianabol steroid is a specific inhibitor of gastrointestinal lipases having prolonged action. It has a therapeutic effect in the lumen of the stomach and small intestine, forming a covalent bond with the active serine site of gastric and intestinal lipases. Inactivated thus loses the ability to cleave an enzyme of dietary fats in the form of incoming trigliperidov on soaked free fatty acids and monoglycerides. Since uncleaved triglycerides are not absorbed into the body caloric intake is reduced, which leads to weight loss.
The therapeutic effect of the drug is carried out without absorption into the systemic circulation. Action orlistat results in an increase of fat in the feces within 24-48 hours after drug administration. After discontinuation of fat content in the stool usually returns to baseline within 48-72 hours.
The absorption of orlistat low. After 8 hours after the ingestion of therapeutic doses of unmodified orlistat plasma practically determined (concentration <5 ng / ml). Signs of cumulation are absent, confirming the minimum absorption of the drug
In vitro orlistat more than 99% bound to plasma proteins (mainly albumin and lipoproteins). The minimum amounts of orlistat can penetrate into erythrocytes.
Orlistat is metabolized primarily in the bowel wall to form pharmacologically inactive metabolites: Ml (hydrolyzed four-membered ring lactone) and M3 (M1 with N-cleaved formilleytsinovym residue).
The main route of elimination is the excretion through the intestine – about 97% of the dose of the drug, where 83% – Orlistat unchanged.
The cumulative excretion through the kidneys all substances structurally related to orlistat, is less than 2% of the dose of the drug. complete elimination time is 3 – 5 days. Orlistat and metabolites are excreted in bile.
Orsoten indicated for the long-term treatment of obese patients with a body mass index (BMI)> 30 kg / m, or overweight patients (BMI> 28 kg / m), including those associated with obesity risk factors, coupled with moderate low-calorie diet.
Orsoten can be administered in combination with hypoglycemic agents and / or moderately low-calorie diet in patients with type 2 diabetes are overweight or obese.
- chronic dianabol steroid malabsorption syndrome;
- sensitivity to orlistat or any other components of the formulation;
- Pregnancy and lactation:
- Children up to age 18 years (effectiveness and safety have been studied)
Pregnancy and lactation
Based on the results of pre-clinical studies: teratogenicity and embryotoxicity when taking orlistat were observed. Clinical data on the use of orlistat during pregnancy are not available, therefore should not be administered orlistat during pregnancy. Since the use during lactation are not available, orlistat should not be taken during lactation.
Dosage and administration
The recommended single dose of orlistat is one 120 mg capsule that is taken orally, with water just before each main meal, during meals or no later than one hour after eating. If you miss a meal, or if the food does not contain fat, you can skip receiving orlistat. Orlistat dose over 120 mg 3 times a day does not increase its therapeutic effect. The duration of therapy is not more than 2 years No dose adjustment is required for elderly patients or patients with impaired hepatic or renal function.
Safety and efficacy of orlistat in the treatment of children under the age of 18 years have not been established.
Adverse reactions to orlistat are mainly marked by the gastrointestinal tract and were due to an increased amount of fat in the feces. Typically, the observed side effects are mild and transient in nature. The appearance of these phenomena observed in the initial phase of treatment during the first three months (but not more than one occasion). Prolonged use of orlistat incidence of side effects is reduced.
There are: dianabol steroid bloating, accompanied by discharge from the rectum, urge to defecate, fatty / oily stools, oily discharge from the rectum, watery stools, soft stools, the inclusion of fat in the feces (steatorrhea), pain / discomfort in the abdomen, increased frequency of bowel movements, pain / discomfort in the rectum, compelling urge to defecate, fecal incontinence, loss of teeth and gums: hypoglycemia in patients with type 2 diabetes, headache, anxiety, flu, fatigue, infections of the upper respiratory tract, urinary tract infection, dysmenorrhea . Rare: allergic reactions (eg, pruritus, rash, urticaria, angioedema, bronchoconstriction, anaphylaxis). Very rare: diverticulitis, gallstones, hepatitis, possibly severe, bullous rash, increased liver transaminases and alkaline phosphatase.
Cases of overdose have not been described. Acceptance of a single dose of 800 mg of orlistat or multiple doses up to 400 mg three times a day for 15 days was not accompanied by significant side reactions. In addition, the dose of 240 mg three times a day, to patients with obesity assigned for 6 months did not cause a significant increase in side effects. It recommended to observe the patient within 24 hours in case of overdose orlistat.
The interaction with other drugs
in patients receiving warfarin or other anticoagulants and orlistat may be a decrease in the level of prothrombin, increasing international normalization ratio (INR), which leads to changes in haemostatic parameters. Interaction with amitriptyline, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, nifedipine GITS, nifedipine delayed release, sibutramine, furosemide, captopril, atenolol, glibenclamide or ethanol were observed. Increases the bioavailability of pravastatin and hypolipidemic effect, increasing its plasma concentration is 30%. Weight loss can improve the metabolism in diabetic patients, thus it is necessary to reduce the dose peroralngh hypoglycemic agents. Orlistat treatment could potentially disrupt the absorption of fat-soluble vitamins (A, D, E, K). If the recommended intake of multivitamins, they should be taken no earlier than 2 hours after taking orlistat or at bedtime.
At the same time taking orlistat and cyclosporine showed a decrease the level of concentration of cyclosporine in the blood plasma, it is recommended to increase the frequency of determining the level of concentration of cyclosporine in the blood plasma.
Patients receiving amiodarone, be more carefully monitored to conduct clinical and ECG monitoring, since the cases reduce the concentration of amiodarone in plasma are described.
Orlistat is effective for long-term control of body weight (weight loss, maintaining it at the appropriate level and preventing re weight gain). Treatment results in improvement of orlistat risk profile and diseases associated with obesity (including hypercholesterolemia, impaired glucose tolerance, hyperinsulinemia, hypertension, type 2 diabetes mellitus) and reduction in the amount of visceral fat.
Decrease in body weight during treatment with orlistat may be accompanied by an improvement of compensation of carbohydrate metabolism in patients with type 2 diabetes, which may allow to reduce the dose of hypoglycemic drugs.
To ensure adequate supply patients are advised to take multivitamin preparations.
Patients should follow the recommendations on diet. They should receive a balanced, moderately low-calorie diet containing no more than 30% of calories as fat. The daily intake of fat should be distributed into three main reception write.
The likelihood of adverse reactions from the gastrointestinal tract may increase when orlistat is taken against the background of a diet rich in fat. Patients should be aware that the more accurately they are dieting (especially with respect to the allowed amount of fat), the less the likelihood of side reactions. A dianabol steroid diet low in fat reduces the likelihood of adverse reactions from the gastrointestinal (GI) tract and help patients to monitor and regulate their fat intake.