orlistat is a very popular weight loss medicine. It acts by preventing the action of enzymes from the digestive juices which break down fats in our diet. What it will do is to make around 30% of the fat consumed not been broke down and absorbed by the body. If you are obese or overweight you may use orlistat as this will help you lose weight. If you wish to try the 60-mg capsules, you can get them without a prescription. On the other hand, the 120-mg capsules option do require a prescription and it is oriented for obese people with a body mass index (BMI) of 28 kg/m or higher.
An online doctor consultation means filling out a medical questionnaire. A registered EU doctor assesses your medical questionnaire and analize whether Orlistat is suitable and safe for you to buy. After approval, a prescription is issued and send to the registered EU pharmacy. You will receive your discretely shipped Orlistat pills within 3 business days.
Orsoten is a drug that has a direct effect on metabolic processes within the body. With regular use, according to the rules that contain instructions for use, it leads to a significant reduction in weight. The drug Orsoten is available in the form of small capsules with yellow microgranules placed in a cell package. One blister may contain 84, 42 or 21 capsules. The active substance in the composition of Orsoten is a component called "orlistat".
One capsule contains 120 mg of the indicated ingredient. Also, the composition of the Orsoten capsule contains an auxiliary substance - microcrystalline cellulose. In essence, orlistat, contained in the preparation is an inhibitor of lipase, an enzyme that is directly involved in the breakdown of fat cells. Due to this property, when consuming Orsoten, the process of absorption of fats from the food that occurs in the intestine is suspended. As a result, triglycerides are excreted unchanged from the body, and the person taking the capsule notices a significant decrease in the initial weight.
The drug Orsoten is indicated for adult men and women who are suffering from obesity. Also, the instructions for use indicate that capsules can be used by people who are overweight, whose MI exceeds 28 units. Orsoten is used for a long course, during which a low-calorie diet is recommended. Treatment with Orsoten is contraindicated in the following cases: The instructions for use indicate that the recommended single dose of Orsoten is one capsule. It must be taken three times a day, preferably before meals.
The course of treatment with Orsoten should last no longer than 24 months. Most often, when using the drug Orsoten, negative reactions from the gastrointestinal tract develop. People complain of increased gas formation, accompanied by oily discharge from the anus. Such a reaction is not a reason for the withdrawal of the drug Orsoten. Typically, the symptoms described are present only in the first months of treatment and then disappear.
The instructions for use also indicate that in addition to the reaction from the gastrointestinal tract, Orsoten can cause other pathologies: Orlistat in Orsoten reduces the level of cyclosporin in the blood, therefore, the simultaneous use of these two substances is contraindicated. With the use of Orsoten and anticoagulants, a slight increase in INR is possible. Also, the drug can affect the level of prothrombin, which in general leads to a change in the hemostasiogram.
According to the instructions for use, no cases of overdose with Orsoten have been reported to date. If the recommended number of capsules is exceeded, it is recommended to seek medical help. The drug must be protected from children and kept in a dark place. A08AB01 Orlistat - microgranules or a mixture of powder and microgranules of white or almost white color. In such cases, symptomatic treatment is indicated. The presence of caked agglomerates is allowed, which easily crumble under pressure.
Pharmacological action - inhibiting gastrointestinal lipases. The drug Orsoten is a powerful, specific and reversible inhibitor of gastrointestinal lipases, which has a long-lasting effect. Its therapeutic effect is carried out in the lumen of the stomach and small intestine and consists in the formation of a covalent bond with the active serine region of the gastric and pancreatic lipases. In this case, an inactivated enzyme loses its ability to break down food fats in the form of triglycerides into absorbable free fatty acids and monoglycerides.
Since undigested triglycerides are not absorbed, the resulting decrease in calorie intake leads to a decrease in body weight. Thus, the therapeutic effect of the drug is carried out without absorption into the systemic circulation. Judging by the results of the fat content in feces, the effect of orlistat begins 24–48 hours after ingestion. After the cancellation of orlistat, the fat content in feces after 48–72 hours usually returns to the level that occurred before the start of therapy.
In clinical trials, patients taking orlistat showed greater weight loss compared with patients on diet therapy. Weight loss began already in the first 2 weeks after the start of treatment and lasted from 6 to 12 months, even in patients with a negative response to diet therapy. Over 2 years, a statistically significant improvement in the profile of metabolic risk factors associated with obesity was observed.
In addition, compared with placebo, there was a significant decrease in the amount of fat in the body. Orlistat is effective in preventing repeated weight gain. Repeated weight gain, not more than 25% of the lost, was observed in about half of the patients, and in half of these patients, repeated weight gain was not observed or even its further decrease was observed.
In clinical trials lasting from 6 months to 1 year, patients with overweight or obesity and type 2 diabetes mellitus taking orlistat showed greater body weight loss compared to patients treated with diet therapy alone. Loss of body weight occurred mainly due to a decrease in the amount of fat in the body. It should be noted that prior to the study, despite taking hypoglycemic agents, patients often had insufficient glycemic control. However, statistically and clinically significant improvement in glycemic control was observed with orlistat therapy.
Besides, during orlistat therapy, a decrease in the doses of hypoglycemic agents, plasma insulin concentration, and a decrease in insulin resistance were observed. In a 4-year clinical study, orlistat significantly reduced the risk of type 2 diabetes (by about 37% compared with placebo). The degree of risk reduction was even more significant in patients with an initial impaired glucose tolerance (approximately 45%).
In the orlistat therapy group, there was a more significant weight loss compared with the placebo group. Maintaining body weight at a new level was observed throughout the study period. Moreover, compared with placebo, patients receiving orlistat therapy showed a significant improvement in the profile of metabolic risk factors. In a 1-year clinical study in obese adolescents with orlistat, a decrease in BMI was observed compared with the placebo group, where there was even an increase in BMI.
In addition, in patients of the orlistat group, a decrease in fat mass, as well as in the waist and hips, was observed compared with the placebo group. Also, patients receiving orlistat therapy showed a significant decrease in d blood pressure compared with the placebo group. In volunteers with normal body weight and obesity, the systemic effect of the drug is minimal.
After a single oral administration of orlistat at a dose of 360 mg, unchanged orlistat in plasma could not be determined, which means that its concentrations are below the level of 5 ng/ml. In general, after taking therapeutic doses, it was possible to detect unchanged orlistat in the blood plasma only in rare cases, while its concentrations were extremely small (Judging by the data obtained in an animal experiment, the metabolism of orlistat is carried out mainly in the intestinal wall. The molecules M1 and M3 have an open β-lactone ring and extremely weakly inhibit lipase (1000 and 2500 times weaker, than orlistat, respectively. Given such a low inhibitory activity and low plasma concentrations (on average 26 and 108 ng / ml, respectively), after taking therapeutic doses, these metabolites are considered pharmacologically inactive.
Normally overweight and have shown that the main route of elimination is the excretion of orlistat nevsosavsheysya through the intestine through the intestinal excreted about 97% of the dose of the drug, and 83% -. orlistat as unchanged total renal excretion of substances. structurally related to orlistat, is less than 2% of the dose taken. The time to complete elimination of orlistat from the body (through the intestines and kidneys) is 3-5 days. The ratio of orlistat excretion routes in volunteers with normal and overweight was the same. Both orlistat and metabolites M1 and M3 may be excreted with bile. Plasma concentrations of orlistat and its metabolites (M1 and M3) in children do not differ from those in adults when comparing the same doses of orlistat. Daily excretion of fat with feces amounted to 27% of food intake during orlistat therapy and 7% when taking a placebo.
According to preclinical data, there were no additional risks for patients regarding the safety profile, toxicity, genotoxicity, carcinogenicity, and reproductive toxicity. In animal studies, a teratogenic effect was also not revealed. Due to the lack of teratogenic effect in animals, its detection in humans is unlikely. long-term therapy of patients with obesity (BMI ≥30 kg / m), with risk factors associated with obesity, in combination with a moderately hypocaloric diet; in combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and / or insulin) and / or a moderately hypocaloric diet in patients with type 2 diabetes mellitus who are overweight or obese. concomitant therapy with cyclosporine; concomitant therapy with warfarin or other anticoagulants for oral administration (see In studies of reproductive toxicity in animals, the teratogenic and embryotoxic effect of orlistat was not observed.
In the absence of a teratogenic effect in animals, a similar effect in humans should not be expected. However, due to the lack of clinical data, Orsoten should not be prescribed to pregnant women. It is not known whether orlistat passes into breast milk, so its use during breastfeeding is contraindicated. The classification of the frequency of development of side effects recommended by WHO: very often - ≥1 / 10; often - from ≥1 / 100 to Adverse reactions to orlistat occurred mainly from the gastrointestinal tract and were due to the pharmacological action of the drug, preventing the absorption of food fats.
The incidence of adverse events decreased with prolonged use of orlistat. The following adverse events occurred very often - pain or discomfort in the abdomen, oily discharge from the rectum, emission of gas with a certain amount of discharge, imperative urge to defecate, steatorrhea, flatulence, loose stools, increased frequency of bowel movements; often - pain or discomfort in the rectum, soft stools, fecal incontinence, tooth damage, gum disease, bloating *. In patients with type 2 diabetes mellitus, the nature and frequency of adverse events were comparable to those in individuals without diabetes with overweight and obesity.
The frequency of gastrointestinal disorders increases with increasing fat content in the diet. Patients should be informed about the possibility of adverse reactions from the gastrointestinal tract and taught how to eliminate them by better dieting, especially in relation to the amount of fat contained in it. The use of a low-fat diet reduces the likelihood of side effects from the gastrointestinal tract and thereby helps patients to control and regulate fat intake. As a rule, these adverse reactions were mild and transient. They occurred in the early stages of treatment (in the first 3 months), and most patients had no more than one episode of such reactions.
In a 4-year clinical study, the overall safety profile did not differ from that obtained in 1- and 2-year studies. At the same time, the total frequency of adverse events from the gastrointestinal tract decreased annually during the 4-year period of taking orlistat. with the simultaneous use of orlistat and antiepileptic drugs, there have been cases of seizures (see * The only new side effects in patients with obesity and type 2 diabetes were hypoglycemic conditions (very common) and bloating (often) that occurred with a frequency of 2% and an incidence of ≥1% compared with placebo.
An increase in the activity of hepatic transaminases and alkaline phosphatase, a decrease in the concentration of prothrombin in blood plasma, an increase in INR values and cases of unbalanced anticoagulant therapy, which led to a change in hemostatic parameters (see. With the simultaneous use of orlistat and cyclosporine, a decrease in the concentration of cyclosporine in blood plasma was noted, which can lead to decreased immunosuppressive efficacy of cyclosporine. Therefore, concomitant use of orlistat and cyclosporine is not recommended. However, if such concomitant use is necessary, it is recommended to conduct more frequent monitoring of cyclosporin concentration in blood plasma both with its simultaneous use with orlistat and after stopping the use of orlistat.
The concentration of cyclosporine in blood plasma should be controlled until it is stabilized. With simultaneous use with the drug Orsoten or at bedtime. When using amiodarone orally during orlistat therapy, a decrease in the systemic exposure of amiodarone and desethylamiodarone was noted (by 25–30%), however, due to the complex pharmacokinetics of amiodarone, the clinical significance of this phenomenon is unclear. Addition of Orsoten and acarbose due to lack of pharmacokinetic studies. With the simultaneous administration of orlistat and antiepileptic drugs, cases of the development of seizures were observed.
A causal relationship between the development of seizures and orlistat therapy has not been established. However, patients should be monitored for possible changes in the frequency and/or severity of the convulsive syndrome. According to clinical studies, there is no interaction of orlistat with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, fluoxetine, losartan, phenytoin, oral contraceptives, phentermine, pravastatin, nifedipine GITS (gastrointestinal therapeutic system).
However, with the simultaneous use of orlistat and warfarin or other anticoagulants, a decrease in the concentration of prothrombin and an increase in the INR index can be observed, which can lead to a change in hemostatic parameters. It is necessary to control the INR indicator with concomitant therapy with warfarin or other anticoagulants for oral administration. Rare cases of the development of hypothyroidism and/or violation of its control were noted.
The mechanism for the development of this phenomenon is unknown but may be due to a decrease in the absorption of iodized salt and/or sodium levothyroxine. There have been cases of decreased effectiveness of antiretroviral drugs for the treatment of HIV, antidepressants, and antipsychotics (including lithium preparations), which coincide with the beginning of the use of orlistat in previously compensated patients.
Orlistat therapy should be started only after a careful assessment of its possible effect on such patients. Orlistat is able to indirectly reduce the effectiveness of contraceptives for oral administration, which in some cases can lead to an unplanned pregnancy. It is recommended to use an additional method of contraception also in the case of severe diarrhea.
In adults and children over 12 years of age, the recommended dose of orlistat is 1 caps. 120 mg with each main meal (immediately before, during, or no later than 1 hour after a meal). In combination with hypoglycemic drugs (metformin, sulfonylurea derivatives and/or insulin) and/or a moderately low-calorie diet in patients with type 2 diabetes who are overweight or obese. In adults, the recommended dose of orlistat is 1 caps. 120 mg with each main meal (immediately before, during, or no later than 1 hour after a meal).
If a meal is skipped or the food does not contain fat, then the drug Orsoten should be taken in combination with a balanced, a moderately hypocaloric diet containing no more than 30% calorie in the form of fats. The daily intake of fats, carbohydrates, and proteins must be divided into 3 main doses. An increase in the dose of orlistat over the recommended (120 mg 3 times a day) does not lead to an increase in its therapeutic effect. The effectiveness and safety of orlistat in patients with impaired liver and/or kidney function, as well as in elderly and pediatric patients (under 12 years of age) have not been investigated.
In clinical trials in individuals with normal body weight and obese patients, single doses of 800 mg or multiple doses of orlistat 400 mg 3 times a day for 15 days were not accompanied by the appearance of significant adverse events. In addition, patients with obesity have experience using 240 mg of orlistat 3 times a day for 6 months, which was not accompanied by a significant increase in the frequency of adverse events.
According to studies in humans and animals, any systemic effects that could be associated with the lipase-inhibiting properties of orlistat should be quickly reversible. The use of the drug Orsoten should be discontinued if, after 12 weeks of therapy, body weight decreased by less than 5% compared to the initial body weight. Clinical studies have revealed a lower bodyweight reduction in patients with type 2 diabetes mellitus receiving orlistat compared with patients without diabetes mellitus receiving orlistat.
Orsoten leads to an improvement in the profile of risk factors and diseases associated with obesity, including hypercholesterolemia, type 2 diabetes mellitus, impaired glucose tolerance, hyperinsulinemia, arterial hypertension, and a decrease in visceral fat. When used in combination with hypoglycemic drugs such as metformin, sulfonylurea derivatives and/or insulin, in patients with type 2 diabetes mellitus with overweight (BMI ≥28 kg / m in combination with a moderately hypocaloric diet, it provides additional improvement in the compensation of carbohydrate metabolism. In clinical trials, in most patients, the concentrations of vitamins A, D, E, K, and beta-carotene during the 4 years of therapy with orlistat remained within the normal range to ensure adequate intake of all nutrients multivitamins should be prescribed.
The patient should receive a balanced, moderately hypocaloric diet containing no more than 30% calorie intake in the form of fats. The daily intake of fats, carbohydrates, and proteins should be divided into 3 main doses. When using orlistat, there have been cases of rectal bleeding. If severe and/or persistent symptoms of bleeding appear, an additional examination is necessary. The likelihood of adverse reactions from the gastrointestinal tract may increase if the drug Orsoten is taken against a diet rich in fats (for example, 2000 kcal/day, of which more than 30% is in the form of fats, which equals approximately 67 g of fat). Daily fat intake should be divided into 3 main doses.
If the drug Orsotens is accompanied by an improvement in the compensation of carbohydrate metabolism, which may allow or require a reduction in the dose of hypoglycemic drugs (for example, sulfonylurea derivatives). It is necessary to control coagulation parameters (for example, an INR indicator) during concomitant therapy with anticoagulants for oral administration. In the case of severe diarrhea with the use of orlistat for women using contraceptives for oral administration, it is necessary to use additional contraceptive measures.
When using orlistat, rare cases of the development of hypothyroidism and/or violation of its control have been noted. The mechanism for the development of this phenomenon is unknown but may be due to a decrease in the absorption of iodized salt and/or sodium levothyroxine. Orlistat has the potential to reduce the absorption of antiretroviral drugs for HIV treatment and the effectiveness of antiretroviral therapy.