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Orlistat
Last reviewed: 10.08.2022
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Orlistat is a medication prescribed for obesity.
The therapeutic effect develops through the formation of covalent synthesis of the serine residue and pancreatic and gastric lipases inside the gastrointestinal tract. [1]
As a result of this action, the enzyme loses the ability to break down edible fats, in the form of triglycerides, to absorbable free fatty acids, as well as monoglycerides. This leads to a decrease in the number of calories that go into the body, which causes a decrease in the patient's weight. [2]
Indications Orlistat
It is used for overweight or obesity - in combination with a low-calorie dietary regimen.
Release form
The release of the drug substance is made in capsules - 10 pieces inside the cell plate, 2 plates inside the box.
Pharmacodynamics
After 24-40 hours, there is an increase in the indicators of fat inside the feces. After stopping the intake of Orlistat, the fat level returns to the initial level after 48-72 hours. [3]
Pharmacokinetics
After oral administration, the drug is almost not absorbed inside the gastrointestinal tract. The introduction of a single portion of 0.36 g does not reveal the intraplasmic parameters of the active element, from which it can be concluded that they are less than 5 ng / ml.
The distribution volume is also not determined due to the extremely weak overall absorption of the drug. Intraplasmic protein synthesis in vitro is 99%. The minimum volumes of orlistat pass inside the erythrocytes.
42% of the absorbed volume of orlistat undergoes metabolic processes. In this case, 2 metabolic components are formed, which have a low index inside the plasma (the average level is 25 ng / ml, as well as 108 ng / ml) and an extremely weak inhibitory effect relative to lipase. In this regard, it is believed that they have no therapeutic activity.
97% of the substance is excreted in feces (83% of them are in an unchanged state). A maximum of 2% of the drug is excreted in the urine. The half-life of a drug (with feces and urine) is 3-5 days. The metabolic components of Orlistat and its unchanged active element are capable of being excreted in the bile.
Dosing and administration
It is necessary to use 1 capsule (0.12 g) 3 times a day, together with eating or for a maximum of 60 minutes after that. When skipping food or taking low-fat food, it is allowed not to take Orlistat. The duration of therapy is selected by the attending physician, taking into account the personal sensitivity and severity of the drug effect provided.
An increase in dosage above the standard does not lead to potentiation of the drug effect.
- Application for children
There is no data regarding the safety of using Orlistat in pediatrics, which is why it is not prescribed for children.
Use Orlistat during pregnancy
The medication is not used during pregnancy, because there is no information regarding the safety of its use.
Studies of the possibility of excretion of drugs with breast milk have not been carried out, which is why it is not prescribed for breastfeeding.
Contraindications
Contraindicated in cases of chronic cholestasis or malabsorption.
Side effects Orlistat
Disorders associated with the function of the gastrointestinal tract: gas formation, discharge from the rectum (oily form), steatorrhea, urgency to defecate, fecal incontinence and increased frequency of emptying processes (usually such symptoms temporarily develop in the first 3 months of therapy). Occasionally, there is discomfort or pain in the rectum or abdomen, loose stools and bloating.
Signs of allergies: itching, anaphylactic symptoms, epidermal rash and Quincke's edema.
Overdose
There is no information on drug poisoning. During clinical tests, the use of 1-fold portion of 0.8 g or multiple administration of 0.4 g 3 times a day for a 15-day period did not cause the development of significant side symptoms.
In case of severe intoxication, the patient should be kept under medical supervision for 24 hours.
Interactions with other drugs
The introduction together with the medication leads to a weakening of the absorption of fat-soluble vitamins.
Storage conditions
Orlistat must be stored in a dark and dry place, closed from the penetration of children. Temperature values - no more than 250C.
Shelf life
Orlistat can be used for a 4-year term from the moment the therapeutic agent was marketed.
Analogs
The analogs of the drug are the substances Xenical, Orlip and Xenistat with Orlikel.
Attention!
To simplify the perception of information, this instruction for use of the drug "Orlistat" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.
Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.