Orlistat: instructions for the use of drugs for weight loss, composition, dosage, analogues

You can deal with the problem of excess weight on your own, changing the way you eat and increasing physical activity. At the same time, you can turn to specialists for the selection of auxiliary means, for example, such as Orlistat. This drug is used in combination with a low-calorie diet. It interferes with the absorption of fats and thereby contributes to weight loss. However, inaccuracies in the diet, in particular, insufficient receipt of certain groups of compounds, can affect well-being, since therapy carries some risks, it must be carefully worked out by a dietitian.

Description of the release form and composition

Slimming medicine is available in the form of elongated gelatin capsules of blue color, the main active ingredient of which is the substance of the same name - orlistat. Inside the capsule, you can see a white friable powder, consisting of chemically modified fillers of starch and cellulose, an anti-caking agent of silicon oxide, a foaming agent of sodium lauryl sulfate and the active compound in an amount of 120 mg.
The basis of the pill shells is gelatin. Indigo carmine and titanium oxide give the capsule a blue color.

The drug is dispensed from pharmacies in a cardboard box. Inside the pack are several plastic, transparent, foil-coated blisters with capsules. You can store the medicine for no longer than three years from the date of release.

Pharmacological action, pharmacodynamics and pharmacokinetics

Orlistat is a drug that does not have a systemic effect on the body. It is practically not absorbed and acts exclusively at the level of the small intestine. The substance forms a strong complex with fat-breaking enzymes of the stomach and intestines - lipases, inhibiting their activity.

Due to the process, large fat molecules remain intact. They leave the body unchanged. A person loses part of the calories.
Energy deficit is covered by burning fats deposited in the abdominal region and around internal organs. Thus, Orlistat tablets work for weight loss.

A decrease in the amount of fat from food leads to normalization of the lipid composition of the blood and a decrease in the total cholesterol level, as a result of which the sensitivity of cells to insulin is restored. The process of glucose uptake is normalized, which again leads to a decrease in the formation of fatty deposits.

Inactivation of gastrointestinal lipases begins a day or two after administration of the drug. Two to three days after the drug is discontinued, the lipase concentration returns to its previous level. Five days after discontinuation of therapy, orlistat is no longer detected in the body.

It is extremely poorly absorbed in the digestive tract. Of the entire dose taken, no more than 3% enters the bloodstream. Communication with blood proteins cannot be established. The distribution mechanism also remains unclear due to the extremely low level of assimilation. It is known that part of orlistat can bind to red blood cells. Up to a fifth of the active substance is converted into metabolites inside the intestinal wall.

The compound that enters the bloodstream is removed from the body by the kidneys. That amount of the drug that remains in the intestine is excreted along with the feces unchanged.
The efficacy of the compound has been studied for four years. Tests have shown that weight loss occurs in the third week after the start of therapy. The rate of loss of kilograms lasts for 6-12 months. Weight loss is observed even in those who were not helped by a separate diet therapy. After a long intake of the drug while maintaining proper nutrition, no more than a quarter of the lost weight is returned.

When is Orlistat prescribed

Orlistat is used in the fight against obesity. It is shown with a body mass index above 28-30 kg / m2. The drug is recommended to be combined with a low-calorie diet. The tool is prescribed when diet therapy without medical support does not bring results, and excess weight threatens the development of concomitant diseases.
Orlistat helps remove kilograms for type 2 diabetes. For these purposes, it is prescribed in conjunction with hypoglycemic drugs and a low-fat diet.

After achieving certain results, the medication for obesity continues to be taken to prevent weight gain. If, after a year from the start of therapy, the weight has decreased by less than 5%, the medication is stopped and people start looking for alternative treatments.

Instructions for use and dosage of drugs for weight loss

Medication for weight loss is prescribed from twelve years. It is taken for a long time, on average 6-12, but less than three months and no more than two years.
Along with taking the drug, losing weight is required to follow a low-calorie diet. Such an indicator of all fats in the diet should not exceed a third of the daily energy value of food consumed. The total calorie content should be evenly distributed between breakfast, lunch and dinner. It is recommended to fill the menu with vegetables and fruits.

No more than three capsules are taken per day - one is intended for simultaneous food intake. Exceeding these standards is impractical, since this does not lead to an increase in the effect.

Orlistat medicine should be drunk, starting a meal, directly with meals or for an hour after eating.If on a certain part of the day the consumed dishes are practically free of fat, then you can skip the use of the substance.

For patients with diabetes, the same standards are taken into account. A single dose of the substance remains at 120 mg. It may be necessary to adjust the composition of hypoglycemic drugs, because orlistat improves blood lipid levels and reduces the need for insulin.

During pregnancy and lactation

Clinically, safety for pregnant and lactating women has not been established. No similar human studies have been conducted. If we apply the analogy with the results of experiments on animals, it can be argued that orlistat has no toxic and teratogenic effects.

However, since it interferes with the absorption of fats, prolonged use of this drug can provoke a deficiency of B vitamins in a pregnant woman. A decrease in cholesterol levels threatens with a lack of hormones that support pregnancy. Since it is not known whether the substance is able to penetrate into the mother’s milk, the drug does not need to be taken during lactation.

Drug interaction

Orlistat is chemically active, it is present for a long time in the stomach and intestines, therefore, it can affect the effectiveness of many medications taken. The following are medicines that can not be combined with the drug, as well as the consequences of such a combination:

• antiarrhythmic drug amiodarone - a decrease in the concentration of heart medication;
• epilepsy medications - a violation of the absorption of these drugs, and, as a result, an increased risk of developing an attack;
• immunosuppressant cyclosporine - increased likelihood of tissue rejection after transplantation;
• anticoagulants - a decrease in the number of components of the blood coagulation system;
• fat-soluble vitamins - problems with the absorption and absorption of these elements;
• acarbose - the consequences of the combination have not been studied, therefore, such a combination should be avoided;
• sodium salt of L-thyroxine - a deficiency of thyroid hormones due to incomplete absorption of the drug;
• hormonal contraceptives - weakening of the contraceptive effect;
• antipsychotics, antidepressants, benzodiazepines, HIV medications - reduced effectiveness from therapy.

If losing weight it is necessary to accept any of the listed means, the therapy should be rebuilt. Incompatible drugs should be separated by time. You may need a dose adjustment or withdrawal of certain medications. No interaction was observed with other medications.

Contraindications, side effects and overdose

The drug is prescribed in the absence of the following contraindications:

• lack of access to bile in the digestive system due to inhibition of its formation or excretion due to pathological processes;
• established deficiency of any group of nutrients;
• high sensitivity to the components of the drug;
• children's age (less than twelve years).

Due to the lack of safety data, pregnancy and the period of breastfeeding are also included.

Most side effects come from the digestive system. Problems are associated with a deficiency in the absorption of fat and its excretion with feces.

 

A patient undergoing treatment may experience abdominal pain, bloating, fecal incontinence.

Due to the high fat content in excrement, diarrhea, oily stools, frequent urge to defecate and pain in the rectum appear. These symptoms can be reduced by reducing the fat fraction in the diet.

Lipid deficiency can manifest itself in the form of nervous and hormonal disorders. Among the side effects were irritability, headaches and menstrual irregularities. Some people have suffered gums and teeth.
Taking the drug reduces the overall resistance of the body, as a result of which there are infectious lesions of the respiratory and urinary tract, digestive tract organs. Flu and respiratory infections are often a threat.

Most often, a lack of lipids and fat-soluble vitamins is manifested by weakness. One of the adverse reactions is the accumulation of crystals in the urinary ducts.

Instructions for use do not describe cases of overdose. When these indicators are exceeded, no amplification of side effects is observed.

Analogs of Orlistat

 

Orlistat-based lipase inhibitors are:
• Xenalten;
• "Xenical";
• “Lista”;
• Orsoten.
These drugs are available in the form of tablets and capsules in dosages of 60 and 120 mg.
Any means for weight correction should be taken strictly according to the indications and according to the scheme prescribed by the doctor.