Xenical: profile and news






MY HAIR LIP IS SO AWFUL I STAY IN  May 15, 2006
QI very overweight and my doctor suggested I try Xenical tablets. ... A XENICAL stops the body absorbing fat and decreases the amount of calories you consume. ... - Glasgow Sunday Mail,

Another Weightloss Pill Poses Health Risks  May 3, 2006
Consumer advocacy groups seek to block the over-the-counter release of weight loss drug, Xenical, because it has been linked to causing pre-cancerous tumors in ... - Emediawire (press release),

Glaxo feels weight of regulators who'll rule on obesity drug  Apr 25, 2006
NEW YORK When GlaxoSmithKline began talking to Roche three years ago about commercializing the prescription diet drug Xenical, the timing could not have been ... - International Herald Tribune,

Wednesday Newspaper Review - Irish Business News and International ...  Apr 26, 2006
New York Times reports that when GlaxoSmithKline began talking to Roche three years ago about commercializing the prescription diet drug Xenical, the timing ... - FinFacts Ireland,

Bariatric Surgery, answer to obesity  May 5, 2006
In the past years losing weight was very futile for some of us, from the daily intake of “Xenical� and “Reductril� to the some diet-modifying ... - News Today Online,

The "all you can stomach of their Bullshit Diet"  Apr 28, 2006
..."In his three years on Xenical, Mr. Burton said he has dropped to 210 pounds from 270, and kept it off.". Do you get what this REALLY says? ... - The Common Voice,

Glaxo Launches Weight-Loss Website Prior to FDA Action on Diet ...  Apr 26, 2006
Even though the FDA has not yet approved the diet drug Alli (low-dose Xenical) for over-the-counter sale, GlaxoSmithKline has launched a weight-loss website ... - Acomplia Report,

Diet drug launch by man who took a dose of his own medicine  Apr 26, 2006
The pill is currently only available on prescription, under the brand name Xenical. ... The group wants Xenical banned and Alli to be refused permission to launch. ... - Independent,

Just how safe are prescription drugs?  Apr 18, 2006
Depressed? Click on Prozac. Overweight? Order a course of Xenical. Can't get it up? Viagra's just a hyperlink away. It's easy - and ... - Belfast Telegraph,

Healthcare: At a Glance - Government Launches Weight-Control ...  May 12, 2006
Roche's Xenical (aka orlistat), Abbott's Reductil (sibutramine) and Sanofi-Aventis's Acomplia (rimonabant) are the three main anti- obesity pills. ... - International News Service,

Concern is growing at the use of prescription drugs as 'lifestyle ...  Apr 20, 2006
Young women with eating disorders can, at the click of a button, obtain access to weight-loss products such as Xenical that are only meant for the morbidly ... - Cape Times (subscription),

Allergan's Weight-Loss Bands Beat Diet, Exercise, Study Says  May 1, 2006
...non-surgical program was run by a physician and included behavioral modifications, a low-calorie diet and drug therapy with orlistat, sold as Xenical by Basel ... - Bloomberg

$33,000 fine for selling medicines over internet  May 8, 2006
...and August 2003. Included in their list of goods were Ventolin inhalers, Xenical and Argentinian-sourced Proscar. Many medicines ... - New Zealand Herald,

In Latest Drug Scandal, Ketek’s Safety and FDA Approval Are ...  May 2, 2006
Public Citizen has petitioned to have many dangerous drugs banned including the COX-2 inhibitors, Meridia, Crestor, Accutane, Xenical, and Tequin. ... - Newsinferno.com,

From the analyst's couch: Anti-obesity therapies  May 4, 2006
Orlistat (Xenical; Roche) reduces weight by limiting caloric intake through inhibition of the lipase-mediated breakdown of fat in the gastrointestinal tract. ... - Nature.com (subscription),

Pharmacist suspended for illegal distribution operation  Apr 27, 2006
She was part of an operation called Vanilla, which shipped medicines including Xenical, Viagra, Propecia and Proscar around the world through an agent in Fiji. ... - Stuff.co.nz,

Anti-obesity drug must go hand in hand with a healthy diet, says ...  Apr 27, 2006
...counter - in Europe. A higher-dose version of the drug, called Xenical, is already available on prescription in the US. But the ... - Telegraph.co.uk,

RealMoney Radio: Toothsome Weight Watchers  Apr 26, 2006
Nicorette. Glaxo is waiting for approval to sell the diet drug Xenical, and Cramer believes that it will happen later in the year. ... - TheStreet.com

Employees May Get Weight-Loss Help  Apr 26, 2006
...drug plan. But medication like Meridia and Xenical isn't effective without significant lifestyle changes, Zimmerman said. The program ... - The Ledger,

Cabinet shuffle may be just the remedy for Glaxo  Apr 26, 2006
...is now campaigning with the US drugs regulator, the Food and Drug Administration, to allow it to sell a lower-dose version of its obesity drug Xenical in the ... - Telegraph.co.uk,

AACE: Insulin Not Sodium May Be Hypertension's Bad Actor  Apr 28, 2006
...summer," he said. "We will be comparing the high fat, no-calorie-restriction diet, to a low fat diet plus Xenical (orlistat).". Asked to ... - MedPage Today,

Roche Showed Continued Strong Sales Growth in the First Quarter ...  Apr 26, 2006
Xenical performed well in the first quarter with sales growth of 16%. Sales were up both in the US (+24%) and in Europe/RoW (+14%). ... - PharmaLive.com (press release),


Other information


Indication
For the treatment of Obesity including management of weight loss and weight maintenance

Pharmacology
Orlistat is a lipase inhibitor used for obesity management that acts by inhibiting the absorption of dietary fats.

Mechanism Of Action
Orlistat is a reversible inhibitor of lipases. It exerts its therapeutic activity in the lumen of the stomach and small intestine by forming a covalent bond with the active serine residue site of gastric and pancreatic lipases. The inactivated enzymes are thus unavailable to hydrolyze dietary fat in the form of triglycerides into absorbable free fatty acids and monoglycerides. As undigested triglycerides are not absorbed, the resulting caloric deficit may have a positive effect on weight control.

Drug Category
Antiobesity Agents; Enzyme Inhibitors; ATC:A08AB01

Brand Names/Synonyms
Orlipastat; Orlipastatum [Inn-Latin]; Orlistat; Orlistat [Usan:Inn]; Tetrahydrolipstatin; Xenical

Dosage Forms
CAPSULE

Absorption
Not Available

Interactions
Interactions for Orlistat:

Alcohol: In a multiple-dose study in 30 normal weight subjects, coadministration of XENICAL and 40 grams of alcohol (e.g., approximately 3 glasses of wine) did not result in alteration of alcohol pharmacokinetics, orlistat pharmacodynamics (fecal fat excretion), or systemic exposure to orlistat.

Cyclosporine: Preliminary data from a XENICAL and cyclosporine drug interaction study indicate a reduction in cyclosporine plasma levels when XENICAL was coadministered with cyclosporine.

Digoxin: In 12 normal-weight subjects receiving XENICAL 120 mg three times a day for 6 days, XENICAL did not alter the pharmacokinetics of a single dose of digoxin.

Fat-soluble Vitamin Supplements and Analogues: A pharmacokinetic interaction study showed a 30% reduction in beta-carotene supplement absorption when concomitantly administered with XENICAL. XENICAL inhibited absorption of a vitamin E acetate supplement by approximately 60%. The effect of orlistat on the absorption of supplemental vitamin D, vitamin A, and nutritionally-derived vitamin K is not known at this time.

Glyburide: In 12 normal-weight subjects receiving orlistat 80 mg three times a day for 5 days, orlistat did not alter the pharmacokinetics or pharmacodynamics (blood glucose-lowering) of glyburide.

Nifedipine (extended-release tablets): In 17 normal-weight subjects receiving XENICAL 120 mg three times a day for 6 days, XENICAL did not alter the bioavailability of nifedipine (extended-release tablets).

Oral Contraceptives: In 20 normal-weight female subjects, the treatment of XENICAL 120 mg three times a day for 23 days resulted in no changes in the ovulation-suppressing action of oral contraceptives.

Phenytoin: In 12 normal-weight subjects receiving XENICAL 120 mg three times a day for 7 days, XENICAL did not alter the pharmacokinetics of a single 300-mg dose of phenytoin.

Pravastatin: In a 2-way crossover study of 24 normal-weight, mildly hypercholesterolemic patients receiving XENICAL 120 mg three times a day for 6 days, XENICAL did not affect the pharmacokinetics of pravastatin.

Warfarin: In 12 normal-weight subjects, administration of XENICAL 120 mg three times a day for 16 days did not result in any change in either warfarin pharmacokinetics (both R- and S-enantiomers) or pharmacodynamics (prothrombin time and serum Factor VII). Although undercarboxylated osteocalcin, a marker of vitamin K nutritional status, was unaltered with XENICAL administration, vitamin K levels tended to decline in subjects taking XENICAL. Therefore, as vitamin K absorption may be decreased with XENICAL, patients on chronic stable doses of warfarin who are prescribed XENICAL should be monitored closely for changes in coagulation parameters.



Chemical IUPAC Name
1-[(3-hexyl-4-oxo-oxetan-2-yl)methyl]dodecyl2-formylamino-4-methyl-pentanoate

Chemical Formula
C29H53NO5

Half Life
1-2 hours

Drug Type
Approved Drug

# Accession No
APRD00255

CAS Registry Number
96829-58-2

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