Xenical, Orlistat
Xenical [Orlistat] marketed by Roche Labs is a drug designed to treat obesity.
Its primary is preventing the absorption of fats from the human diet, this leads to decrease in calorific intake.
In plain language it blocks some of the fat that we eat thereby keeping it from being absorbed by the body.
Xenical is used together with a reduced-calorie diet and weight maintenance to treat obesity in people with certain risk factors (such as diabetes mellitus, high blood pressure, and atherosclerosis, family history of stroke, heart attack, and high serum cholesterol and serum triglycerides.
But why do we need to keep obesity in check? Here’s the reason why.
Obesity is one of the leading causes of diabetes mellitus and hypertension in the world. The situation is so grim that, heart attack, which once used to be seen only in aged people [>50 years] is now commonly seen in people as young as 20-25years.
Obesity has not even spared our children who just can’t seem to get enough of the fast food culture.
Combine this with the stressful life and it becomes a deadly cocktail. Our sedentary lifestyle makes matters worse.
Observational epidemiologic studies have established a relationship between obesity and visceral fat and the risks for cardiovascular disease, type 2 diabetes, and certain forms of cancer, gallstones, certain respiratory disorders, and an increase in overall mortality. This suggests that weight loss, if maintained, may produce health benefits for obese patients who have or are at risk of developing weight-related co morbidities. The long-term effects of Xenical [Orlistat] on morbidity and mortality associated with obesity have not been established.
Obesity/Body Mass Index [BMI] can be calculated by the following formula: kg/m2
The normal range is 17.99 to 24.99. Above 30 is termed as obese and more than 40 is termed as morbid obesity.
The effects of Xenical [Orlistat] on weight loss and maintenance and related co-morbidities like type 2 diabetes mellitus, lipids and blood pressure were assessed in a study called the XENDOS, a 4 year study. The XENDOS study found a 37% reduction in the incidence of Type II Diabetes Mellitus, a significant difference
In one-year clinical trials carried out on humans, between 35.5% and 54.8% of subjects a 5% or greater decrease in body mass was achieved, although not all of this mass was necessarily fat. Between 16.4% and 24.8% achieved at least a 10% decrease in body mass. After discontinuation of Xenical [Orlistat], a majority of the subjects showed weight gain of up to 35% of the total weight they had lost
Xenical [Orlistat], chemically a tetrahydrolipstatin is a saturated derivative of lipostatin which is a potent inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini. But lipostatin is an unstable and complex compound, thus Xenical [Orlistat] which is a simple and stable compound was developed as an antiobesity drug.
Xenical [Orlistat] reversibly inhibits lipases, an enzyme that breaks down the triglycerides in the gastro-intestinal tract, especially in the lumen of the stomach and small intestine. It forms a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes thus cannot hydrolyze the dietary fat which is in the form of triglycerides. Meaning, the pancreatic and gastric lipases cannot hydrolyze the triglycerides from the fat in the diet into simpler monoglycerides and free fatty acids [FFAs].These unabsorbed triglycerides are then excreted in the stools in an undigested form. The resulting calorie deficit may lead to weight control.
Xenical [Orlistat] is metabolized mainly in the gastro-intestinal tract
Side effects and Contraindications:
The most common side effect of Xenical [Orlistat] is altered bowel movement habits. This is usually experienced during the initial weeks of treatment; though this may be seen throughout the regimen in rare cases. This is supported by the XENDOS study which found that of the 91% of subjects who suffered from gastrointestinal side effects in the first year only 36% had the gastrointestinal adverse effects during their fourth year of taking Xenical [Orlistat]. In case the side effects are severe then this should be immediately brought to the notice of the prescribing physician.
• Steatorrhea i.e. oily, loose stools seen as oily spotting on underwear or on clothing
• Feacal incontinence- urgent need to have a bowel movement along with flatus
• increased number of bowel movements
• difficulty controlling bowel movements
• gas with oily spotting
• loose stools
• oily or fatty stools
• pain or discomfort in the rectum/anus
• irregular menstrual periods
• headache
• anxiety
• hives
• rash
• itching
• difficulty breathing or swallowing
• severe or continuous abdominal pain
• Cold or flu-like syndrome.
Contraindications:
- Hypersensitivity to Xenical [Orlistat]
- Reduced gall bladder function
- Chronic Malabsorption syndrome
- Pregnancy [FDA Pregnancy category B drug] and lactation. Can be prescribed to the pediatric age group of elder than 10 years.
Precaution:
- Impaired liver profile
- Impaired pancreatic profile
- Obstructed bile duct
- History of hyperoxaluria, calcium oxalte nephrolithiasis
- Obesity due to any organic cause like hypothyroidism
- Any eating disorder like anorexia or bulimia
- If taking any other weight loss drug
Drug interactions:
- Amiodarone [antiarrhythimic]
- Cyclosporine
- Digoxin
- Warfarin
Special information:
Since Xenical [Orlistat] inhibits the body’s absorption of beta carotene and certain fat soluble vitamins, multivitamin supplements should be taken daily. This multivitamin can be taken 2 hours before or after having food. It can also be taken during midnight or in the morning.
Avoid fat rich food and prefer foodstuffs which are likely to contain less than 30% fat.
The recommended dose of XENICAL [Orlistat] is one 120-mg capsule three times a day with each main meal containing fat.during or up to 1 hour after the meal.
Samir is the author of Xenical , Orlistat information located at Genericsmed.com site
References:
Pharmacology and Pharmacotherapeutics Revised 17th Edition, R.S.Satoskar, S.D.Bhandarkar, and S.S.Ainapure
http://www.rxlist.com/cgi/generic/orlistat_cp.htm
http://www.nlm.nih.gov/medlineplus/d...r/a601244.html
http://en.wikipedia.org/wiki/Orlistat
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