Fatlos is indicated in conjunction with a mildly hypocaloric diet for the treatment of obese patients with a body mass index (BMI) greater or equal to 30 kg/m², or overweight patients (BMI ≥ 28 kg/m²) with associated risk factors. Treatment with Fatlos should be discontinued after 12 weeks if patients have been unable to lose at least 5 % of the body weight as measured at the start of therapy.

Composition

Each hard capsule of Fatlos contains:

• Active ingredient: Orlistat 120 mg.

Pharmaceutical Form: Hard gelatin capsule.

Dosage

• Fatlos Adults dosage: The recommended dose of Orlistat is one 120 mg capsule (one capsule of Fatlos) taken with water immediately before, during or up to one hour after each main meal. If a meal is missed or contains no fat, the dose of Fatlos should be omitted.
• The patient should be on a nutritionally balanced, mildly hypocaloric diet that contains approximately 30% of calories from fat. It is recommended that the diet should be rich in fruit and vegetables. The daily intake of fat, carbohydrate and protein should be distributed over three main meals.
• Doses of Orlistat above 120 mg three times daily have not been shown to provide additional benefit.
• The effect of Orlistat results in an increase in faecal fat as early as 24 to 48 hours after dosing. Upon discontinuation of therapy, faecal fat content usually returns to pre-treatment levels, within 48 to 72 hours.
• Special Populations: The effect of Orlistat in patients with hepatic and/or renal impairment, children and elderly patients has not been studied. There is no relevant indication for use of Fatlos in children.

Photo album: Fatlos similar products – Orlistat Products

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Is Orlistat The Best Option For Weight Loss?

Orlistat prevents the intestines from absorbing fats from food, causing them to flow through the colon and pass into the stool. This sounds great! But orlistat preparations do not actually cause significant weight loss, in contrast to the unpleasant side effects of orlistat preparations such as flatulence, foul-smelling gas, and the flow of oily droplets through the anus with stool or sometimes without defecation.

Orlistat can help you to lose around 5 pounds (about 2.5 kilograms) more weight per year than those who don’t take medication, diet, and exercise. I think 365 days of medication for 5 lbs (2.5 kg) of weight loss doesn’t seem to be worth it.

The reason why Orlistat does not work well is that it treats excessive fat consumption, meaning it prevents weight gain caused by increased consumption of fatty or fried foods, but Orlistat has no role in reducing the effects of carbohydrates, starches or sugars, and the fact that most of the contents of the unhealthy diet is processed foods with a high content of sugars, starches and carbohydrates, and excessive consumption of simple carbohydrates is a major factor in weight gain. Orlistat’s lack of effect on carbohydrates or simple sugars does not make it an effective weight loss drug. However, it will work for you if you consume large amounts of fats such as fried foods or fast food.

Orlistat is a drug that prevents the absorption of fats by inhibiting an enzyme called “lipase”, an enzyme that breaks down fats in the intestines, so that the fats in food pass without being absorbed by the body, and this reduces the calories absorbed by the body. However, simply taking orlistat will not help you lose weight. It can help you shed some pounds, if only you follow a reasonable and balanced diet, along with exercise.

Conclusion:

• Orlistat does not affect carbohydrates, which are the main cause of weight gain.
• Orlistat does not cause significant weight loss compared to those who follow a healthy diet.
• Orlistat only prevents the absorption of fat, and this reduces the calories absorbed through fat metabloism.
• Orlistat should be taken in conjunction with a healthy diet and moderate exercise.

Contraindications

• Hypersensitivity to the active substance or to any of the excipients.
• Chronic malabsorption syndrome.
• Cholestasis.
• Breast-feeding.

Special Warnings

• In clinical trials, the decrease in bodyweight with Orlistat treatment was less in type II diabetic patients than in non-diabetic patients. Antidiabetic medicinal product treatment may have to be closely monitored when taking Orlistat.
• Co-administration of Orlistat with ciclosporin is not recommended.
• Patients should be advised to adhere to the dietary recommendations they are given.
• The possibility of experiencing gastrointestinal adverse reactions may increase when Orlistat is taken with a diet high in fat (e.g. in a 2000 kcal/day diet, > 30 % of calories from fat equates to> 67 g of fat). The daily intake of fat should be distributed over three main meals. If Orlistat is taken with a meal very high in fat, the possibility of gastrointestinal adverse reactions may increase.
• Cases of rectal bleeding have been reported with Orlistat.
• Prescribers should investigate further in case of severe and/or persistent symptoms.
• The use of an additional contraceptive method is recommended to prevent possible failure of oral contraception that could occur in case of severe diarrhoea.
• Coagulation parameters should be monitored in patients treated with concomitant oral anticoagulants.
• The use of Orlistat may be associated with hyperoxaluria and oxalate nephropathy in patients with underlying chronic kidney disease and/or volume depletion.
• Rare occurrence of hypothyroidism and/or reduced control of hypothyroidism may occur. The mechanism, although not proven, may involve a decreased absorption of iodine salts and/or levothyroxine.
• Antiepileptics patient: Orlistat may unbalance anti_convulsant treatment by decreasing the absorption of antiepileptic drugs, leading to convulsions.
• Cases of severe liver injury have been reported rarely with the use of Orlistat. Patients should stop use of Orlistat and contact their healthcare professional if they develop the signs and symptoms of liver injury, including itching, yellow eyes or skin, dark urine, light-colored stools, or loss of appetite.

Interaction With Other Medicinal Products And Other Forms Of Interaction

• Ciclosporin: A decrease in ciclosporin plasma levels has been observed in a drug-drug-interaction study and also reported in several cases, when Orlistat was administered concomitantly. This can lead to a decrease of immunosuppressive efficacy. Therefore the combination is not recommended. However, if such concomitant use is unavoidable, more frequent monitoring of ciclosporin blood levels should be performed both after addition of Orlistat and upon discontinuation of Orlistat in ciclosporin treated patients. Ciclosporin blood levels should be monitored until stabilised.
• Acarbose: In the absence of pharmacokinetic interaction studies, the concomitant administration of Orlistat with acarbose should be avoided.
• Oral anticoagulants: When warfarin or other anticoagulants are given in combination with Orlistat, international normalised ratio (INR) values should be monitored.
• Fat soluble vitamins: Treatment with Orlistat may potentially impair the absorption of fat-soluble vitamins (A, D, E and K). The vast majority of patients receiving up to four full years of treatment with Orlistat in clinical studies had vitamin A, D, E and K and beta-carotene levels that stayed within normal range. In order to ensure adequate nutrition, patients on a weight control diet should be advised to have a diet rich in fruit and vegetables and use of a multivitamin supplement could be considered. If a multivitamin supplement is recommended, it should be taken at least two hours after the administration of Orlistat or at bedtime.
• Amiodarone: A slight decrease in plasma levels of amiodarone, when given as a single dose, has been observed in a limited number of healthy volunteers who received Orlistat concomitantly. In patients receiving amiodarone treatment, the clinical relevance of this effect remains unknown but may become clinically relevant in some cases. In patients receiving concomitant amiodarone treatment, reinforcement of clinical and ECG monitoring is warranted.
• Convulsions have been reported in patients treated concomitantly with Orlistat and antiepileptic drugs e.g. valproate, lamotrigine, for which a causal relationship to an interaction cannot be excluded. Therefore, these patients should be monitored for possible changes in the frequency and/or severity of convulsions.
• Rare occurrence of hypothyroidism and/or reduced control of hypothyroidism may occur. The mechanism, although not proven, may involve a decreased absorption of Iodine salts and/or levothyroxine.
• Lack of interactions: No interactions with amitriptyline, atorvastatin, biguanides, digoxin, fibrates, uoxetine, losartan, phenytoin, phentermine, pravastatin, nifedipine Gastrointestinal Therapeutic System (GITS), nifedipine slow release, sibutramine or alcohol have been observed. The absence of these interactions has been demonstrated in specific drug-drug-interaction studies.
• The absence of an interaction between oral contraceptives and Orlistat has been demonstrated in specific drug-drug interaction studies. However, Orlistat may indirectly reduce the availability of oral contraceptives and lead to unexpected pregnancies in some individual cases. An additional contraceptive method is recommended in case of severe diarrhea.

Pregnancy and lactation

For Orlistat, no clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Caution should be exercised when prescribing to pregnant women. As it is not known whether Orlistat is secreted into human milk, Orlistat is contra-indicated during breast-feeding.

Effects On Ability To Drive And Use Machines

Orlistat has no influence on the ability to drive and use machines.

Undesirable Effects

Adverse reactions to Orlistat are largely gastrointestinal in nature. The incidence of adverse events decreased with prolonged use of Orlistat.  Adverse events are listed below by system organ class and frequency. Frequencies are defined as:

• very common (≥1/10).
• common (≥1/100 to <1/10).
• uncommon (≥1/1,000 to <1/100).
• rare (≥1/10,000 to <1/1,000).
• and very rare (<1/10,000) including isolated reports.

Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness. The following undesirable effects (first year of treatment) is based on adverse events that occurred at a frequency of > 2 % and with an incidence ≥1 % above placebo in clinical trials of 1 and 2 years duration:

• Nervous system disorders: Very common: Headache.
• Respiratory, thoracic and mediastinal disorders: Very common: Upper respiratory infection. Common: Lower respiratory infection.
• Gastrointestinal disorders: Very common: abdominal pain/discomfort, oily spotting from the rectum, atus with discharge, faecal urgency, fatty/oily stool, atulence, liquid stools, oily evacuation, increased defecation. Common: rectal pain/discomfort, soft stools, faecal incontinence, abdominal distension, tooth disorder, gingival disorder.
• Renal and urinary disorders: Common: urinary tract infection.
• Metabolism and nutrition disorders: Very common: hypoglycaemia.
• Infections and infestations: Very common: influenza.
• General disorders and administration site conditions: Common: fatigue.
• Reproductive system and breast disorders: Common: menstrual irregularity.
• Psychiatric disorders: Common: anxiety.

The following undesirable effects are based on post-marketing spontaneous reports, and therefore the frequency remains unknown:

• Increase in liver transaminases and in alkaline phosphatase.
• Decreased prothrombin, increased INR and unbalanced anticoagulant treatment resulting in variations of haemostatic parameters have been reported in patients treated with anticoagulants in association with Orlistat.
• Gastrointestinal disorders: Rectal bleeding, diverticulitis, pancreatitis.
• Skin and subcutaneous tissue disorders: Bullous eruptions.
• Immune system disorders: Hypersensitivity (e.g. pruritus, rash, urticaria, angioedema, bronchospasm and anaphylaxis).
• Hepatobiliary disorders: Cholelithiasis, hepatitis that may be serious.
• Renal and urinary disorders: Oxalate nephropathy.

Overdose

Single doses of 800 mg Orlistat and multiple doses of up to 400 mg three times daily for 15 days have been studied in normal weight and obese subjects without significant adverse findings. In addition, doses of 240 mg tid (three times per day) have been administered to obese patients for 6 months. The majority of Orlistat overdose cases received during post-marketing reported either no adverse events or adverse events that are similar to those reported with recommended dose. Should a significant overdose of Orlistat occur, it is recommended that the patient be observed for 24 hours. Based on human and animal studies, any systemic effects attributable to the lipase-inhibiting properties of Orlistat should be rapidly reversible.

Pharmacological Properties

Pharmacodynamic properties

Pharmaco-therapeutic group: Peripherally acting anti-obesity agent. Orlistat is a potent, specific and long-acting inhibitor of gastrointestinal lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine site of the gastric and pancreatic lipases. The inactivated enzyme is thus unavailable to hydrolyse dietary fat, in the form of triglycerides, into absorbable free fatty acids and monoglycerides.

Pharmacokinetic Properties

Absorption: Studies in normal weight and obese volunteers have shown that the extent of absorption of Orlistat was minimal. Plasma concentrations of intact Orlistat were non-measurable (< 5 ng/ml) eight hours following oral administration of Orlistat. In general, at therapeutic doses, detection of intact Orlistat in plasma was sporadic and concentrations were extremely low (< 10 ng/ml or 0.02 µmol), with no evidence of accumulation, which is consistent with minimal absorption.

Distribution: The volume of distribution cannot be determined because the drug is minimally absorbed and has no defined systemic pharmacokinetics. In vitro Orlistat is> 99 % bound to plasma proteins (lipoproteins and albumin were the major binding proteins). Orlistat minimally partitions into erythrocytes.

Metabolism: Based on animal data, it is likely that the metabolism of Orlistat occurs mainly within the gastrointestinal wall. Based on a study in obese patients, of the minimal fraction of the dose that was absorbed systemically, two major metabolites, M1 (4-member lactone ring hydrolysed) and M3 (M1 with N-formyl leucine moiety cleaved), accounted for approximately 42 % of the total plasma concentration. M1 and M3 have an open beta-lactone ring and extremely weak lipase inhibitory activity (1000 and 2500 fold less than Orlistat respectively). In view of this low inhibitory activity and the low plasma levels at therapeutic doses (average of 26 ng/ml and 108 ng/ml respectively), these metabolites are considered to be pharmacologically inconsequential.

Elimination: Studies in normal weight and obese subjects have shown that faecal excretion of the unabsorbed drug was the major route of elimination. Approximately 97 % of the administered dose was excreted in faeces and 83 % of that as unchanged Orlistat. The cumulative renal excretion of total Orlistat-related materials was < 2 % of the given dose. The time to reach complete excretion (faecal plus urinary) was 3 to 5 days. The disposition of Orlistat appeared to be similar between normal weight and obese volunteers. Orlistat, M1 and M3 are all subject to biliary excretion.

Preclinical Safety Data

Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and toxicity to reproduction.

In animal reproductive studies, no teratogenic effect was observed. In the absence of a teratogenic effect in animals, no malformative effect is expected in man. To date, active substances responsible for malformations in man have been found teratogenic in animals when well-conducted studies were performed in two species.

كيف يُخفض أورليستات الوزن

Resources And References

• إَليزا كبسولات – نشرة معلومات المريض.
• أُورلِيستات- نشرة معلومات المريض.
• Xenical – Patient Information Leaflet.
• Fatlos – Patient Information Leaflet.
• UNI-CAL- Patient Information Leaflet.
• Onlefit- Patient Information Leaflet.

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