XENICAL
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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.
David Kelly is author of Generic Xenical.
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