People suffering from obesity are often prescribed special medications that can control the amount of calories and fat they eat. One of these effective drugs is an inhibitor of special enzymes - steapsins (lipases). This drug is called Orlistat. Thanks to its use, it is possible to reduce excess weight.
Composition and release form
"Orlistat" for weight loss is available in the form of dense blue capsules. Inside the capsule there are white granules (pellets). The total weight of all granules is 240 mg. They contain 120 mg of the active substance - orlistat. Additional components have been added to it: povidone K30 (in an amount of 5.04 mg and cellulose (98.64 mg), as well as various sodium compounds: carboxymethyl starch (10.08 mg) and lauryl sulfate (6.24 mg). The capsules are made of gelatin and titanium dioxide, colored with blue dye.
The capsules are packed in dense cells and hidden in a cardboard box. Packages are available with a very different number of tablets: 5, 6 and 10. Sometimes the drug is placed in a glass jar with 20, 21, 30, 40, 42, 50, 80, 84, 100, 120 or 140 capsules each.
Effect of the drug
The drug suppresses the activity of intestinal, gastric and pancreatic lipases. It binds to fat droplets and inactivates lipases. Thanks to this effect, triglycerides do not penetrate into the blood. Thus, dietary fats are broken down less well and are less absorbed into the blood. Because of this, a lack of energy occurs in the body, and then fat is released from those reserves that the body “put aside for a rainy day.” Thanks to this, the volume of fat located in the viscero-abdominal region of the body is reduced.
Once in the intestines, Orlistat reduces the number of monoglycerides and free fatty acids. Due to this, cholesterol is less soluble in liquids and penetrates into the blood in smaller quantities. This allows you to cleanse the blood of excess “bad” cholesterol and improve the functioning of blood vessels.
Orlistat normalizes the fat composition of the blood and increases the sensitivity of body tissues to insulin. This allows you to get rid of excess insulin in the blood, which also leads to a decrease in fat mass in the abdominal area.
"Orlistat" is easily absorbed and quickly eliminated from the body without penetrating into the blood. It is broken down in the intestines and completely eliminated 5 days after the last dose.
According to research results, this medicine made it possible to lose 6.2% of excess body weight (from the original) in 52 weeks. Insulin levels decreased by 18% over the same time.
Mechanism of action and effectiveness
The substance orlistat was first synthesized in the mid-80s by Swiss biochemists. Its main property is inhibition of gastrointestinal lipase (an enzyme that breaks down fats). As a result, the breakdown of fats into fatty acids and monoglycerides becomes impossible.
Unlike most advertised dietary supplements, the drug actually works with lipid metabolism.
Since fats are no longer absorbed into the blood during Orlistat use, creating a calorie deficit, the body begins to use its own fat reserves as an energy source. According to numerous clinical studies, a therapeutic dose of the substance can block up to 30% of dietary fat.
Important! Orlistat is the only substance officially approved for use in the long-term treatment of obesity. It was once available in all countries only by prescription. This law still exists in Canada today. In Russia, patients also cannot make over-the-counter purchases. Some pharmacies are ready to sell the product over the counter, but only if the dosage of the active substance does not exceed 60 mg.
As a bonus, the drug reduces the level of “bad” cholesterol, provides control over blood pressure and prevents the development of type 2 diabetes. Doctors say that regular treatment of excess weight through drugs with orlistat forms a conditioned reflex in a person: as soon as overeating occurs, diarrhea is observed. However, this moment does not affect the general well-being. Since the substance does not penetrate into the blood, systemic effects on the body can be avoided. Metabolism of the drug is observed in the intestinal walls. It completely leaves the body after a few days.
Long-term therapy with Orlistat allows you to lose weight without going beyond dietary standards - up to approximately 8 kg in 3 months.
The World Organization of Gastroenterology considers orlistat medicinal products to be moderately effective in treating obesity. This is confirmed by test results:
- In 3 months, the volunteers managed to lose up to 5% of their original weight.
- Significant weight loss was observed in more than 70% of patients.
However, you can find quite a few reviews online about the drug containing orlistat that dispute its effectiveness. Some claim that in six months it is possible to get rid of a maximum of 10% of weight, and only in the case when a strict diet is followed at the same time and intense physical activity occurs. There is another opinion - after completing the course, the lost kilograms return. Doctors confirm the veracity of these words, recommending not to give up a healthy diet after completing medical weight loss.
Indications
This drug has a very limited list of indications. It is prescribed for certain conditions:
- overweight;
- obesity;
- metabolic syndrome.
Orlistat is also taken to consolidate the achieved result after losing a little weight. The medicine does not allow the extra pounds to return.
This drug can be taken by patients who are strictly following a moderate calorie diet. Due to excessively high-calorie foods in the diet, the medicine may not work.
Orlistat
20.05.18 11:26:24
Hello. By summer I decided to take care of myself. Go on a diet, start exercising. But how lazy it is, who would know. However, something needs to be done. I used to take a laxative drug, but it was not very beneficial for the body. The nutritionist, as usual, compiled a list of what you can’t eat (a whole list of almost all foods), and what you can eat—nothing. Funny. I went to the pharmacy to buy at least a set of “Turbo Slim”, but the pharmacist, such a pretty girl, said: “Try this product, Orlistat 60 mg, we are selling it.” I asked about its action, they explained to me that it removes fat from the body. I was overjoyed and daydreaming! I think I’ll buy it and try it, maybe it will help! I found out its price along the way, it seemed affordable - 625 rubles in total for the course. I bought it. Well, like a curious gopher, I sat down on the Internet to read, study reviews, and suddenly I bought it in vain? The reviews are different, some praise, some are dissatisfied, but since I bought it, I have to try it. With my weight of 78 kg at 160 cm, it certainly wouldn’t hurt to try it. So, I read the instructions, which said to take three times a day with meals, but no later than an hour after. I don't eat that much. I decided to save 42 tablets. Take two a day, just like I eat twice a day. I took it for three days, no side effects. I think, well, won’t it help me? I judge by side effects, but there are none. But in the evening it started. As prescribed - fatty stools, and other unpleasant fragments. I pulled myself together and limited myself to fatty foods, since the fat that was absorbed by me so deliciously, but not usefully, is removed. It seems like there are fewer problems, at least I’m no longer afraid to leave the house. Well, because fat stains laundry. Oh, worse than during the menstrual cycle! But, I’m stubborn, did I pay the money in vain? A week later I stepped on the scale - minus 600 grams! This has already made me happy. I started weighing myself every morning and discovered that on average I was losing 150 grams a day, no matter what I ate! And so, in 21 days I lost almost four kilograms and 74 kopecks simply amazed me! To celebrate, I bought shawarma with double cheese and away I went... My body rested for a month, I ate as usual, without these pills, especially trying to consume fatty vitamins, since Orlistat does not recognize the healthy or harmful fat we eat and removes absolutely all that was taken into the stomach. Therefore, it is still necessary to compensate for the lack of vitamins. When I weighed myself again, I realized that I had gained a little less than one and a half kg. Well, it's my own fault. You need to eat less. And yet, 75 and a half kg is better than 78 something. And I bought Orlistat again. In the same pharmacy, because for some reason it is more expensive in others. So, I’m thinking, where should I weigh myself? When they moved, the owners kept the scales. But I still feel that the fat is leaving my stomach and sides. As I understand it, having thrown out the absorbed fat from the body, the body begins to use the fat that was already deposited in the body for energy. That's the trick. At least I was able to fit into those breeches that for two years did not want to fit on my hips. This made me very happy and encouraged! Despite all the inconveniences associated with side effects, I bought another, already third, pack, although I have not drunk the second one yet. I will also drink in courses, take Orlistat for a month, rest for a month, although some in the reviews write that you can take it without a break for up to six months. Well, I don’t want to torture my body like that. Still, it needs healthy fat to function properly. My goal is to lose 56 kg to a normal weight. I hope I can do it this summer. In any case, I go for long walks once a week. And a contrast shower for skin tightening is said to help. This is my personal experience. There is an effect, I like it, despite the side effects.
Side effects
Orlistat causes many side symptoms from different organs and systems:
- frequent bowel movements;
- fat in stool;
- flatulence;
- oily discharge from the anus;
- urgency and fecal incontinence;
- seizures (in patients with epilepsy);
- symptoms of hypothyroidism;
- dizziness;
- insomnia or increased sleepiness;
- headache;
- anxiety;
- skin rash;
- abdominal pain;
- pancreatitis;
- renal failure;
- allergy.
Additional medications may be needed to manage side effects. During the course of taking the drug, it is advisable to wear absorbent pads or diapers for adults.
Contraindications
The drug is contraindicated in patients suffering from certain diseases:
- impaired absorption of certain substances - malabsorption syndrome;
- excessive sensitivity to components;
- calcium oxalate kidney stones (nephrolithiasis);
- excess oxalates in the urine (hyperoxaluria);
- stagnation of bile (cholestasis);
- periods of pregnancy and lactation;
- age less than 18 years.
It is prohibited to take Orlistat simultaneously with anticoagulants, including warfarin, as well as sitagliptin and cyclosporine.
This substance should be taken with great caution by patients with kidney, liver and gallbladder diseases.
In case of an overdose, you need to temporarily stop drinking this drug, then the body will quickly return to normal. The patient should be monitored during the first 24 hours after overdose symptoms, which manifest themselves in the form of gastrointestinal disturbances.
Orlistat
Diet and exercise are an integral part of a weight loss program. It is recommended to begin a dietary program and exercise before starting therapy with Orlistat.
While taking Orlistat, you must adhere to a fractional, balanced, moderately hypocaloric diet, with a fat content of no more than 30% of the daily calorie intake (for example, with a diet of 2000 kcal/day, fat intake should be no more than 66 g/day). You should adhere to the recommendations received regarding diet and physical activity, both during and after stopping the drug.
The use of the drug Orlistat leads to an increase in fat content in stool already 24-48 hours after the start of administration. After discontinuation of Orlistat, stool fat content usually returns to baseline levels within 48 to 72 hours.
Following a low-fat diet reduces the likelihood of adverse reactions from the gastrointestinal tract.
Taking orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E, K and beta-carotene). The vast majority of patients receiving orlistat during the four-year clinical studies had vitamin A, D, E, K and beta-carotene concentrations within normal limits. For preventive purposes, it is recommended to take multivitamins at night.
Since weight loss is usually accompanied by an improvement in carbohydrate metabolism, patients with type 2 diabetes mellitus should consult a doctor before starting therapy with Orlistat and, if necessary, adjust the dose of hypoglycemic drugs.
A decrease in body weight during treatment may be accompanied by a decrease in blood pressure and the concentration of TC in the blood plasma. Patients taking antihypertensive or lipid-lowering drugs should consult a doctor and, if necessary, adjust the dose of these drugs.
In clinical studies, no interaction was observed between oral contraceptives and orlistat. However, orlistat may indirectly reduce the bioavailability of oral contraceptives, which may lead to the development of unwanted pregnancy. It is recommended to use additional methods of contraception in case of acute diarrhea.
Patients with kidney disease should consult a doctor, as hyperoxaluria and nephropathy may develop.
Patients taking amiodarone, warfarin or other oral anticoagulants should also consult a physician before starting orlistat therapy as changes in the INR may occur.
Patients should stop taking Orlistat and consult a doctor if symptoms occur: icteric discoloration of the sclera or skin, itching, dark urine and loss of appetite.
Cases of rectal bleeding have been observed with the use of orlistat. If this phenomenon occurs, the patient should consult a doctor.
When orlistat and levothyroxine sodium are used together, hypothyroidism and/or decreased control of hypothyroidism may develop. Patients taking levothyroxine sodium should consult their doctor before starting treatment with orlistat, because It may be necessary to take orlistat and levothyroxine sodium at different times, and the dose of levothyroxine sodium may need to be adjusted.
Patients taking antiepileptic drugs should consult their doctor before starting treatment with orlistat, because they should be monitored for possible changes in the frequency and severity of seizures. In these cases, the possibility of taking orlistat and antiepileptic drugs at different times should be considered.
Patients should consult their physician before using orlistat concomitantly with antiretroviral drugs used to treat HIV infection. Orlistat may reduce the absorption of antiretroviral drugs and negatively affect their effectiveness.
Interaction with other drugs
This drug reduces the effectiveness of many other medications. The absorption of the following substances is reduced:
- vitamin K (by 30%);
- vitamin E (α-tocopherol);
- vitamin A (β-carotene);
- fat-soluble vitamin D;
- antiepileptic drugs;
- contraceptives;
- iodine;
- levothyroxine sodium.
As a last resort, you can take a multivitamin complex before bed or no earlier than 2 hours after Orlistat.
This medicine should not be taken together with cyclosporine, warfarin, or amiodarone. It suppresses the effect of antipsychotics, antidepressants and antiretroviral drugs against HIV infection.
ORLISTAT CAPS 120MG N42
Diet and exercise are an integral part of a weight loss program. It is recommended to begin a dietary program and exercise before starting therapy with Orlistat.
While taking Orlistat, you must adhere to a fractional, balanced, moderately hypocaloric diet, with a fat content of no more than 30% of the daily calorie intake (for example, with a diet of 2000 kcal/day, fat intake should be no more than 66 g/day). You should adhere to the recommendations received regarding diet and physical activity, both during and after stopping the drug.
The use of the drug Orlistat leads to an increase in fat content in stool already 24–48 hours after the start of administration. After discontinuation of Orlistat, stool fat content usually returns to baseline levels within 48 to 72 hours.
Following a low-fat diet reduces the likelihood of adverse reactions from the gastrointestinal tract.
Taking orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E, K and beta-carotene). The vast majority of patients receiving orlistat during the four-year clinical studies had vitamin A, D, E, K and beta-carotene concentrations within normal limits. For preventive purposes, it is recommended to take multivitamins at night.
Since weight loss is usually accompanied by an improvement in carbohydrate metabolism, patients with type 2 diabetes mellitus should consult a doctor before starting therapy with Orlistat and, if necessary, adjust the dose of hypoglycemic drugs.
A decrease in body weight during treatment may be accompanied by a decrease in blood pressure and the concentration of TC in the blood plasma. Patients taking antihypertensive or lipid-lowering drugs should consult a doctor and, if necessary, adjust the dose of these drugs.
In clinical studies, no interaction was observed between oral contraceptives and orlistat. However, orlistat may indirectly reduce the bioavailability of oral contraceptives, which may lead to the development of unwanted pregnancy. It is recommended to use additional methods of contraception in case of acute diarrhea.
Patients with kidney disease should consult a doctor, as hyperoxaluria and nephropathy may develop.
Patients taking amiodarone, warfarin or other oral anticoagulants should also consult a physician before starting orlistat therapy as changes in the INR may occur.
Patients should stop taking Orlistat and consult a doctor if symptoms occur: icteric discoloration of the sclera or skin, itching, dark urine and loss of appetite.
Cases of rectal bleeding have been observed with the use of orlistat. If this phenomenon occurs, the patient should consult a doctor.
When orlistat and levothyroxine sodium are used together, hypothyroidism and/or decreased control of hypothyroidism may develop. Patients taking levothyroxine sodium should consult their doctor before starting treatment with orlistat, because It may be necessary to take orlistat and levothyroxine sodium at different times, and the dose of levothyroxine sodium may need to be adjusted.
Patients taking antiepileptic drugs should consult their doctor before starting treatment with orlistat, because they should be monitored for possible changes in the frequency and severity of seizures. In these cases, the possibility of taking orlistat and antiepileptic drugs at different times should be considered.
Patients should consult their physician before using orlistat concomitantly with antiretroviral drugs used to treat HIV infection. Orlistat may reduce the absorption of antiretroviral drugs and negatively affect their effectiveness.
Impact on the ability to drive vehicles and machinery
The drug Orlistat does not affect the ability to drive vehicles and machines.
Can pregnant women take it?
These capsules should not be taken by pregnant or nursing mothers. Because of this drug, the amount of fat-soluble vitamins in the body decreases, and this can have an extremely negative impact on the health of the unborn child. It is during pregnancy that it is vital to take enough vitamins. This primarily concerns B vitamins, especially folic acid (B9). They are necessary for the formation of the child’s nervous system. You should also not take Orlistat while breastfeeding.
