XENICAL ® Orlistat

XENICAL ® is a drug based on Orlistat

THERAPEUTIC GROUP: Anti-obesity drugs with peripheral action

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Directions 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 hypocaloric diet.

Action mechanism XENICAL ® Orlistat

XENICAL ® is a drug based on Orlistat, the only active anti-obesity principle that is 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 resembles that of the most common triglycerides, which allows this active principle to interact selectively with the lipases present in the gastro-intestinal tract, preventing its 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 food lipids in fatty acids and glycerol, drastically reducing intestinal absorption, with a significant drop in caloric and lipid intake of the meal just taken.

This action is also possible thanks to some pharmacokinetic characteristics of Orlistat, which reduce systemic absorption to a minimum, making it practically inconsistent, thus allowing an activity concentrated at the gastro-intestinal level.

At this point both the unabsorbed lipids and the Orlistat and some of its inactive metabolites, produced by the same intestinal mucosa, are excreted through the faeces.

Studies carried out and clinical efficacy

1. STUDIO XENDOS AND EFFECTIVENESS OF THE ORLISTAT

A milestone in the functional evaluation of the orlistat that 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 treated with placebo. The same ratio was maintained in prolonged treatments for 1 and 4 years.

2. ORLISTAT, GLYCEMIA AND CARDIAC FUNCTIONALITY IN DIABETIC PATIENTS

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 further weight reduction compared to placebo and in improving glycemic levels as well as heart function.

3. ORLISTAT AND BEHAVIORAL ASPECTS

A very interesting study that shows how taking Orlistat can guarantee a significant decrease in weight and contribute to improving lifestyle. Questionnaires submitted to patients before and after treatment with Orlistat, have shown a growing attention to the care of their diet and to the improvement of lifestyle, highlighting the main role of healthy habits not only in food, in weight loss and in maintaining the condition of well-being.

Method of use and dosage

XENICAL ® 120mg hard capsules of Orlistat: we recommend taking one of XENICAL ® capsules before, contextually or after ingesting 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 feces is already observed 24 - 48 hours after the first intake to persist up to 72 hours after the last.

In any case, the maximum effective dose is that of three capsules a day, above which, the therapeutic effects remained unchanged in the face of an increase in adverse reactions.

Warnings XENICAL ® Orlistat

Therapy with XENICAL ® should be associated with careful monitoring of some important laboratory parameters such as coagulation and glycaemia in patients treated with oral anticoagulants or antidiabetic therapy, respectively.

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 that does not exceed 30% of the calories deriving from lipids per meal.

Additional side effects may occur following the intake of XENICAL ® in patients with chronic renal failure and hypothyroidism.

In case of a failure to reduce body weight by at least 5% in 12 weeks of treatment, the intake of XENICAL ® should be stopped. Although the Orlistat contained in XENICAL ® does not undergo an important systemic absorption, its persistence at the gastro-intestinal level could alter the normal pharmacokinetic properties of different active ingredients, mainly related to absorption capacity and bioavailability.

PREGNANCY AND BREASTFEEDING

At the moment there are no studies available to clarify the safety profile of Orlistat on fetal health when taken during pregnancy, while different pharmacokinetic tests have shown the presence of this molecule in breast milk.

In light of this evidence, it would be good to avoid taking XENICAL ® both during the pregnancy and in the subsequent breastfeeding phase.

Interactions

Although the Orlistat contained in XENICAL ® does not undergo an important systemic absorption, its persistence at the gastro-intestinal level could alter the normal pharmacokinetic properties of different active ingredients, mainly related to absorption capacity and bioavailability.

Indeed, pharmacokinetic studies show a significant reduction in the bioavailability of ciclosporin, oral anticoagulants, amiodarone and probably oral anticoagulants (in this case due to increased fecal excretion) when administered concomitantly with Orlistat.

For the same reason, an integrative therapy with fat-soluble vitamins could be recommended, preferably taken at least 2 hours after taking XENICAL ® .

Contraindications XENICAL ® Orlistat

XENICAL ® is contraindicated in patients with cholestasis, chronic malabsorption syndrome and hypersensitivity to the active ingredient or one of its excipients.

Orlistat intake is also contraindicated during breastfeeding and not recommended during pregnancy.

Undesirable effects - Side effects

The most common side reactions described following the use of XENICAL ® mainly concern the gastrointestinal tract with impulsive defecatory stimulus, fatty and oily stools, abdominal pains, increased evacuation frequency and rectal bleeding in more severe cases and metabolic with hypoglycemia.

Cases of headache, transaminase abnormalities, fatigue and fatigue and hypersensitivity dermatological reactions have been more rare.