Eagle

Orlip has a peripheral principle of influence; is a medicine used for obesity. The orlistat component is a specific substance that has a powerful inhibitory effect on lipases in the gastrointestinal tract (has a long-lasting effect).

The drug effect of drugs is realized inside the small intestine and gastric lumen - covalent ligaments are formed with active serine regions of pancreatic and gastric lipases. The inactivated enzyme in this case loses the ability to break down dietary fats, which come in the form of triglycerides, and in addition, the effect on absorbed free fatty acids and monoglycerides. [1]

Indications Eagle

It is used in combination with a dietary regimen (moderate hypocaloricity) in obese people (BMI is ≥30 kg / m2) or overweight people (BMI is ≥28 kg / m2), including those who has risk factors associated with obesity.

The introduction of orlistat must be canceled after 3 months, if a weight loss of at least 5% is not registered in comparison with the initial level.

Release form

The drug is produced in the form of capsules, in the amount of 10 pieces inside the cell plate. The box contains 3 such records.

Pharmacokinetics

Absorption.

Testing in normal weight and obese volunteers has shown that the effect of weight on absorption rates is extremely low. After 8 hours after oral administration of drugs, the unchanged substance inside the blood plasma was not recorded, from which we can conclude that its indicator is less than 5 ng / mol. [2]

In general, with the introduction of therapeutic portions of Orlip, it was possible to determine unchanged orlistat inside the blood plasma only sporadically; at the same time, its indicators were very low (<10 ng / ml or 0.02 μmol). At the same time, no signs of accumulation were observed, which confirms the weak absorption of the drug. [3]

Distribution processes.

The distribution volume cannot be detected, because the drug is poorly absorbed. In vitro, more than 99% of the drug is synthesized with blood intraplasmic protein (most of it with albumin and lipoproteins). The minimum volumes of orlistat pass inside the erythrocytes.

Exchange processes.

The information obtained during testing with animals showed that the metabolic processes of orlistat are mainly realized through the walls of the gastrointestinal tract. About 42% of the minimum values of drugs undergoing total absorption in obese individuals are 2 of Orlip's main metabolic products - M1 with MZ.

Molecules of the M1 and M3 types have an open β-lactone ring and rather weakly slow down the activity of lipase (1000 and also 2500 times less than orlistat). Given such a weak retarding effect and low plasma values (the average level is, respectively, 26 and 108 ng / ml), after the administration of therapeutic portions, these metabolic products are considered to have no drug activity.

Excretion.

The unabsorbed drug is mainly eliminated with feces (approximately 97% of the dosage, and 83% unchanged).

Cumulative renal excretion of all substances that are structurally synthesized with orlistat is less than 2% of the serving. The term until complete excretion of drugs (together with urine and feces) is 3-5 days. The proportions of the pathways of excretion of the drug in volunteers with overweight and normal weight are completely similar. Both the metabolic elements M1 with MZ and orlistat are capable of being excreted in the bile.

Dosing and administration

Adults are prescribed the use of the 1st capsule of 0.12 g (with plain water) immediately before eating, together with it, or for the next hour after. If you skip eating or eating low-fat food, the use of Orlip is allowed to be skipped.

Patients should eat a balanced diet, a low-calorie diet in moderate form, containing about 30% of calories (in the form of fats). It is required to eat a lot of vegetables along with fruits. The daily amount of proteins with fats, as well as carbohydrates, should be divided into 3 daily meals.

Exceeding the standard dosage of drugs (0.12 g 3 times a day) does not cause potentiation of the drug effect.

The use of orlistat leads to an increase in the secretion of fat along with feces after 24-48 hours from the moment of taking the drug. At the end of therapy, the secretion of fat in the feces returns to its original volume after 48-72 hours.

• Application for children

There is no information regarding the use of Orlip in pediatrics.

Use Eagle during pregnancy

There is no clinical information regarding the use of orlistat during pregnancy.

Animal testing did not determine whether there was an indirect or direct adverse effect on pregnancy, fetal / embryonic development, labor, or postnatal development. But orlistat is still prohibited to use during the specified period.

There is no information on whether orlistat is excreted in breast milk, which is why it is not prescribed for breastfeeding.

Contraindications

It is contraindicated to prescribe with a chronic malabsorption syndrome or with intolerance to the active element or other components of the drug.

Side effects Eagle

Among the side symptoms:

• impairment of NS function: headaches usually develop;
• disorders associated with the respiratory tract, sternum and mediastinum: often there are lesions of the lower and upper regions of the respiratory system;
• problems with the gastrointestinal tract: fatty discharge from the rectum, pain or discomfort in the abdominal area, bloating accompanied by the discharge of a small amount of bowel movements, steatorrhea, loose stools, oily discharge, imperative bowel movements and an increase in bowel movements are often observed. Often, there may be soft stools, damage to the gums or teeth, discomfort or pain in the rectal area, and fecal incontinence;
• violations of the renal and urinary activity: often there is an infection of the urethra;
• metabolic problems: hypoglycemia usually develops;
• invasions and other infections: flu often appears;
• systemic signs: weakness is often observed;
• disorders associated with the mammary glands and reproductive function: dysmenorrhea often appears;
• mental problems: anxiety is often noted.

Overdose

Clinical tests in people with normal weight and obesity who took 1-fold servings of 0.8 g of orlistat or reusable dosages of 0.4 g 3 times a day for 15 days did not show the development of noticeable negative symptoms. In addition, obese individuals have experience of using drugs 3 times a day at a dosage of 0.24 g for six months.

Usually, with an overdose of a drug during post-marketing tests, negative signs were absent or were similar to those observed with the introduction of therapeutic portions of drugs.

In case of severe poisoning, it is required to monitor the patient's condition for 24 hours. Evidence from animal and volunteer testing suggests that the overall effect that can be associated with the lipase-inhibiting effect of orlistat usually disappears quickly.

Interactions with other drugs

Cyclosporine.

The combination of the drug with cyclosporine leads to a decrease in the plasma parameters of the latter. As a result, the immunosuppressive activity of cyclosporin may be weakened. Because of this, such a combination is prohibited. But with a strict need to use these substances at the same time, you need to regularly monitor the plasma values of cyclosporine. Plasma cyclosporine levels should be monitored until they stabilize.

Acarbose.

Because the pharmacokinetic interaction of the drug with acarbose has not been studied, they cannot be combined.

Anticoagulants taken orally.

The combination of drugs with warfarin and other anticoagulants requires regular monitoring of INR values.

Fat-soluble vitamins.

Administration with orlistat causes a weakening of the absorption of retinol, calciferol, tocopherol and vitamin K. At the same time, in the majority of patients who used the drug for up to 4 full years, normal values of these vitamins, as well as β-carotene, were observed in clinical tests.

In order to ensure adequate nutrition for dieters, you need to include more vegetables and fruits in your diet and take a multivitamin supplement to control your weight.

If you need multivitamins, they should be consumed at least 2 hours after the introduction of orlistat, or in the evening, before bedtime.

Amiodarone.

The combination of the drug with amiodarone led to a slight decrease in the parameters of the latter within the plasma in a small number of volunteers. In individuals who use amiodarone, it was not possible to clarify the clinical significance of this symptom, but sometimes it can be important. In people who combine Orlip with amiodarone, clinical observation and ECG monitoring should be strengthened.

Other combinations.

Administration of the medication together with anticonvulsants (lamotrigine or valproate) sometimes leads to the development of seizures. It was not possible to determine the connection between these phenomena, but patients should be monitored for the possible appearance of changes in the intensity or frequency of seizures.

Occasionally, hypothyroidism develops or its control is weakened. It was not possible to prove the mechanism of this violation, but there may be a weakening of the absorption of levothyroxine or iodine salts.

There is information about a decrease in the therapeutic activity of antiretroviral drugs in people with HIV, antipsychotics (among them lithium) and antidepressants, coinciding with the start of drug treatment in people with an adequately controlled course of pathologies. Because of this, before starting therapy, it is required to carefully evaluate any possible complications for such patients.

Orlistat is able to indirectly weaken the activity of oral contraception, which can sometimes lead to unplanned conception. For severe diarrhea, additional contraception should be used.

Storage conditions

The eagle should be kept out of the reach of children, in a dark and dry place, with temperatures in the range of 10-20˚С.

Shelf life

Orlip is allowed to be used within a 36-month period from the date of sale of the therapeutic product.

Analogs

The analogs of the drug are the substances Xenical, Orlikel and Xenistat with Olistat.

Reviews

Orlip receives mixed reviews from patients. As a means that allows you to remove excess weight, it is considered effective, but at the same time, a large number and high intensity of the development of side effects during its use are noted.