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Roche Orlistat (Xenical) Diet Pills
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Basic information
- Generic name: Orlistat
- Brand/Trade names: Xenical
- Dosages:
Capsules 120 mg; 60 mg.
- Pharmacologic category: Lipase Inhibitor
- FDA approved: April 23, 1999
- Habit forming? No
- Pregnancy risk factor: B
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Medical uses
Xenical (Orlistat) is used together with a reduced-calorie diet
and weight maintenance to treat obesity in people with certain
risk factors (such as diabetes, high blood pressure, and high
cholesterol or triglycerides).
Orlistat promotes loss of weight by preventing the digestion
and absorption of fat in food.
Side effects of Xenical are largely gastrointestinal in nature
and related to the pharmacologic effect of orlistat on preventing
the absorption of ingested fat. Most common side effects include:
bowel movement urgency; gas with discharge; inability to control
bowel movements; increased number of bowel movements; oily discharge;
oily or fatty stools; oily spotting.
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Pharmacological characteristics
- Elimination half-life: half-life for M1 metabolite
is approximately 3 h; half-life M3 metabolite is approximately
13.5 h; half-life of absorbed orlistat is 1 to 2 h.
- Metabolism: Occurs mainly in the gastrointestinal wall.
Two metabolites are M1 (4-member lactone ring hydrolyzed) and
M3 (M1 with N-formyl leucine moiety cleaved); considered pharmacologically
inconsequential.
- Excretion: Eliminated by fecal excretion (major route);
biliary excretion for metabolites. 97% eliminated through feces,
83% as unchanged drug, and less than 2% through urine.
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Benefits
- Provides effective weight loss. About 81% of users
are satisfied or very satisfied with Xenical (Orlistat). Xenical
is effective in weight loss, weight maintenance and prevention
of weight regain. Provides rapid and continuous weight loss
in the first 12 weeks of treatment.
- Additional health benefits. Treatment with Xenical
results in an improvement of risk factors and comorbidities
in overweight persons, including high blood pressure, high cholesterol
and high blood sugar.
- Anti-diabetic properties. Xenical is the first weight
loss medication to show a reduction in the risk of developing
type 2 diabetes1.
It also helps to improve glycemic control in individuals with
type 2 diabetes.
- Acts only in the digestive system. Does not affect
other body systems. The systemic exposure to orlistat is minimal.
Unlike appetite suppressants Xenical does not act on the brain.
- Well tolerated.
- Low potential for misuse. Not centrally acting. No
dose dependent effect.
- Low potential for drug interactions.
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Concerns
- Can lead to vitamin deficiency. By blocking fat absorption,
the drug also make it harder for your body to absorb fat-soluble
vitamins A, D, E and K, as well as beta-carotene.
- Increased risk of kidney stone formation. Fat malabsorption
induced by the orlistat (Xenical) elevate the risk of developing
kidney stones, especially with a high intake of oxalate-containing
foods.
- High rate of gastrointestinal side effects such as
oily spotting or discharge, gas with discharge, fatty or oily
stools, increased bowel movements, an urgent need to have them
and an inability to control them. These bowel difficulties are
caused by the excretion of undigested fat and typically occur
after high-fat meals.
- Possible drug interactions. Cyclosporine and Warfarin
drug interaction.
- High cost.
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Unlabeled uses
- Polycystic ovarian syndrome (PCOS)2
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Mechanism of action
Orlistat belongs to a group of medicines called lipase inhibitors.
This medicine works by preventing the absorption of dietary fat
in your body.
Enzymes in your digestive system, called lipases, help digest
(or break down) fat. When taken with meals, Xenical (Orlistat)
attaches to the lipases and blocks them from breaking down some
of the fat you have eaten. The undigested fat cannot be absorbed
and is eliminated in your bowel movements. By working this way,
Orlistat helps block about one-third of the fat in the foods you
eat from being absorbed by your body.
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Xenical Discussions Boards, Forums, & Reviews
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References
- 1. XENical in the prevention of diabetes
in obese subjects (XENDOS) study: a randomized study of orlistat
as an adjunct to lifestyle changes for the prevention of type
2 diabetes in obese patients. Torgerson JS, Hauptman J, Boldrin
MN, Sjo"stro"m L. Diabetes Care. 2004 Jan;27(1):155-61.
- 2. Diamanti-Kandarakis E, Katsikis I, Piperi
C, Alexandraki K, Panidis D. Effect of long-term orlistat treatment
on serum levels of advanced glycation end-products in women
with polycystic ovary syndrome. Clin Endocrinol (Oxf). 2007
Jan;66(1):103-9.
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Interesting Orlistat facts
- Unlike appetite suppressants, orlistat (Xenical) works as a weight
loss aid by acting upon the function of the gastrointestinal tract.
- The U.S. FDA approved orlistat capsules, branded as Alli, as an
over-the-counter (OTC) treatment for overweight adults in February,
2007.
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