XENICAL ® is an Orlistat-based drug
THERAPEUTIC GROUP: Peripheral anti-obesity drugs
Indications XENICAL ® Orlistat
XENICAL ® is indicated in the treatment of obesity (BMI equal to or greater than 30 Kg / m2) or overweight (BMI greater than or equal to 28 Kg / m2) complicated by associated risk factors, in conjunction with a moderately low-calorie diet.
Mechanism of action XENICAL ® Orlistat
XENICAL ® is a drug based on Orlistat, the only active anti-obesity ingredient still on the market in Italy after the withdrawal of sibutramine from the market.
Its therapeutic action is closely related to the particular chemical structure, which vaguely recalls that of the most common triglycerides, which allows this active principle to selectively interact with the lipases present in the gastro-intestinal tract, preventing their action.
The irreversible inhibition, which is achieved through the formation of covalent bonds between Orlistat and a Serine expressed in the active domain of lipase, prevents these enzymes from digesting dietary lipids into fatty acids and glycerol, drastically reducing intestinal absorption, with a significant drop in the caloric and lipid intake of the meal just made.
This action is also possible thanks to some pharmacokinetic characteristics of Orlistat, which reduce its systemic absorption to a minimum, making it practically inconsistent, thus allowing a concentrated activity at the gastrointestinal level.
At this point both the unabsorbed lipids and Orlistat and some of its inactive metabolites, produced by the intestinal mucosa itself, are excreted in the faeces.
Studies carried out and clinical efficacy
1. XENDOS STUDY AND THE EFFECTIVENESS OF THE ORLISTAT
Endocr Pract. 2006 Jan-Feb; 12
Analysis of the XENDOS study (Xenical in the Prevention of Diabetes in Obese Subjects).
Sjöström L.
Milestone in the functional evaluation of orlistat which shows that in about 60% of patients treated with this drug it was possible to detect a weight loss of 5% in 12 weeks of treatment, compared to 35% of patients receiving placebo. the same relationship was maintained in prolonged treatments for 1 and 4 years.
2. ORLISTAT, GLUCOSE AND CARDIAC FUNCTIONALITY IN DIABETIC PATIENTS
J Obes. 2011; 2011: 394658.
Impact of orlistat-induced weight loss on diastolic function and heart rate variability in severely obese subjects with diabetes.
Martin J, Paquette C, Marceau S, Hould FS, Lebel S, Simard S, Dumesnil JG, Poirier P.
The administration of Orlistat for a period of 12 weeks in patients with type II diabetes and obesity, has been shown to be useful in ensuring a further weight decrease compared to placebo and in improving glycemic levels as well as cardiac function.
3. ORLISTAT AND BEHAVIORAL ASPECTS
J Obes. 2011; 2011: 806896.
Taking Orlistat: Predicting Weight Loss over 6 Months.
Hollywood A, Ogden J.
Very interesting study that demonstrates how taking Orlistat can, in addition to guaranteeing a significant decrease in weight, contribute to an improvement in lifestyle. Patients' questionnaires before and after treatment with Orlistat have shown a growing attention to the care of their own nutrition and lifestyle improvement, highlighting the main role of healthy habits, not just eating habits, in weight loss and in maintaining the condition of well-being.
Method of use and dosage
XENICAL ® Orlistat 120mg hard capsules: it is recommended to take one capsule of XENICAL ® before, at the same time or after the ingestion of a meal containing lipids.
Given the mechanism of action of the active ingredient, concentrated on the digestion and absorption of lipids, it is obvious that the drug should not be taken at the same time as low-fat meals, and that at the same time the diet should ensure the correct intake of fiber, macro and micronutrients with a lipid percentage around 30% of the total caloric portion of the meal.
The excretion of fats with the faeces is observed already 24 - 48 hours after the first intake and persists up to 72 hours from the last.
In any case, the maximum effective dose is that of three capsules per day, above which, the therapeutic effects have remained unchanged in the face of an increase in adverse reactions.
XENICAL ® Orlistat warnings
Therapy with XENICAL ® should be associated with careful monitoring of some important laboratory parameters such as coagulation and blood glucose in patients respectively undergoing therapy with oral anticoagulants or antidiabetic agents.
At the same time, particular attention is also recommended in patients taking oral contraceptives, given the reduced bioavailability that could be observed in case of concomitant administration.
To avoid the appearance of unpleasant side effects, such as rectal bleeding and gastro-intestinal disorders, it is essential to follow a healthy diet at the same time that does not exceed 30% of the calories deriving from lipids per meal.
Further side effects could occur following the intake of XENICAL ® in patients with chronic renal insufficiency and hypothyroidism.
In case of failure to reduce body weight by at least 5% in 12 weeks of treatment, the intake of XENICAL ® should be discontinued. Although the Orlistat contained in XENICAL ® does not undergo significant systemic absorption, its persistence at the gastro level -intestinal could alter the normal pharmacokinetic properties of various active ingredients, mainly related to the absorption capacity and bioavailability.
PREGNANCY AND BREASTFEEDING
At the moment there are no studies that clarify the safety profile of Orlistat on the health of the fetus when taken in pregnancy, while different pharmacokinetic tests have shown the presence of this molecule in breast milk.
In the light of this evidence, it would be advisable to avoid taking XENICAL ® both during pregnancy and in the subsequent lactation phase.
Interactions
Although the Orlistat contained in XENICAL ® does not undergo an important systemic absorption, its persistence at the gastrointestinal level could alter the normal pharmacokinetic properties of various active ingredients, mainly related to the absorption capacity and bioavailability.
Indeed, pharmacokinetic studies show a significant reduction in the bioavailability of cyclosporine, oral anticoagulants, amiodarone and probably oral anticoagulants (in this case due to increased faecal excretion) when administered concomitantly with Orlistat.
For the same reason, supplementary therapy with fat-soluble vitamins may be recommended, preferably to be taken at least 2 hours after taking XENICAL ®.
Contraindications XENICAL ® Orlistat
XENICAL ® is contraindicated in patients suffering from cholestasis, chronic malabsorption syndrome and hypersensitivity to the active substance or one of its excipients.
The intake of Orlistat is also contraindicated during breastfeeding and not recommended during pregnancy.
Undesirable Effects - Side Effects
The most common side reactions described following the intake of XENICAL ® mainly affect the gastrointestinal system with impelling defecatory stimulus, greasy and oily stools, abdominal pain, increased stool frequency and rectal bleeding in the most severe cases and metabolic bleeding with hypoglycemia.
Cases of headache, transaminase changes, asthenia and fatigue, and dermatological hypersensitivity reactions were rarer.
Note
XENICAL ® is a prescription drug.
The information on XENICAL ® Orlistat published on this page may be out of date or incomplete. For a correct use of this information, see the Disclaimer and useful information page.
