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Orlistat
Last reviewed: 04.07.2025
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Orlistat is a medication prescribed for obesity.
The therapeutic effect develops through the formation of covalent synthesis of serine residue and pancreatic and gastric lipases within the gastrointestinal tract. [ 1 ]
As a result of this action, the enzyme loses the ability to break down dietary fats, which are in the form of triglycerides, into absorbable free fatty acids and monoglycerides. This leads to a decrease in the number of calories that enter the body, which causes the patient to lose weight. [ 2 ]
Indications Orlistat
It is used in cases of excess weight or obesity – in combination with a low-calorie diet.
Release form
The medicinal substance is released in capsules - 10 pieces inside a cell plate, 2 plates inside a box.
Pharmacodynamics
After 24-40 hours, there is an increase in the fat levels in the feces. After stopping taking Orlistat, the fat level returns to the initial level after 48-72 hours. [ 3 ]
Pharmacokinetics
After oral administration, the drug is almost not absorbed in the gastrointestinal tract. The introduction of a 1-fold portion of 0.36 g does not allow to detect intraplasmic indicators 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%. Minimal volumes of orlistat pass into erythrocytes.
42% of the absorbed volume of orlistat undergoes metabolic processes. In this case, 2 metabolic components are formed, which have a low value 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, they are considered to have no therapeutic activity.
97% of the substance is excreted in feces (83% of which are unchanged). A maximum of 2% of the drug is excreted in urine. The half-life of the drug (with feces and urine) is 3-5 days. Metabolic components of Orlistat and its unchanged active ingredient can be excreted in bile.
Dosing and administration
It is necessary to use 1 capsule (0.12 g) 3 times a day, together with food or for a maximum of 60 minutes after that. If you skip a meal or eat low-fat food, you can skip Orlistat. The duration of therapy is selected by the attending physician, taking into account personal sensitivity and the severity of the medicinal effect.
Increasing the dosage above the standard does not lead to a potentiation of the drug's effect.
- Application for children
There is no data regarding the safety of Orlistat use in pediatrics, which is why it is not prescribed to children.
Use Orlistat during pregnancy
The medication is not used during pregnancy because there is no information regarding the safety of its use.
No studies have been conducted on the possibility of excretion of the drug with breast milk, which is why it is not prescribed during breastfeeding.
Contraindications
Contraindicated in case of cholestasis or malabsorption of a chronic nature.
Side effects Orlistat
Disorders associated with the gastrointestinal tract: gas formation, discharge from the rectum (oily form), steatorrhea, imperative urge to defecate, fecal incontinence and increased frequency of bowel movements (usually such symptoms temporarily develop in the first 3 months of therapy). Occasionally, discomfort or pain in the rectum or abdomen, loose stools and bloating may occur.
Signs of allergy: itching, anaphylactic symptoms, epidermal rash and Quincke's edema.
Overdose
There is no information on poisoning with the drug. During clinical tests, the use of a single dose of 0.8 g or multiple administration of 0.4 g 3 times a day over a 15-day period did not cause the development of significant side effects.
In case of severe intoxication, the patient should be kept under medical supervision for 24 hours.
Interactions with other drugs
Administration together with medication leads to a weakening of the absorption of fat-soluble vitamins.
Storage conditions
Orlistat should be stored in a dark and dry place, out of the reach of children. Temperature values are no more than 250C.
Shelf life
Orlistat can be used for a period of 4 years from the date of sale of the therapeutic agent.
Analogues
The analogs of the drug are 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.