Orlistat: profile and news






Low-dose Orlistat helps in fat war -- but heed warning  16 May 2006
Recently one of them, Orlistat, moved a step closer to becoming available without a prescription. use. This is a lower dose than the prescription form. ... - Miami Herald,

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),

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,

Another Weightloss Pill Poses Health Risks  May 3, 2006
The group said a December 2005 study confirmed earlier company data showing Xenical, known generically as orlistat, can cause abnormal cell growth in the ... - Emediawire (press release),

Allergan's Weight-Loss Bands Beat Diet, Exercise, Study Says  May 1, 2006
The 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 ... - Bloomberg

The Heavy Burden of Stereotyping  May 8, 2006
Sally Squires discusses the weight-loss drug Orlistat in a February 2006 interview, on the nationally syndicated radio program, 'The Satellite Sisters' on ABC ... - Washington Post,

Stomach surgery may have a role in moderate obesity  May 2, 2006
...weight. Forty patients were randomized to diet, exercise, and treatment with the weight loss drug, orlistat, over a 6-month period. ... - Reuters.uk,

Australian LAP-BAND Study Passes Over Low-Carb Comparison  May 3, 2006
...between 30-35 and split them into two groups: 1) physician-directed, very low-calorie diet in combination with the weight loss pill orlistat, lifestyle change ... - The Common Voice,

Gastric Banding May Help In Moderate Obesity  May 2, 2006
Half of patients were randomized to diet, exercise, and treatment with the weight loss drug, orlistat, over a 6-month period under regular observance. ... - All Headline News

LAP-BAND Patients Lose Significantly Greater Amounts of Initial ...  May 1, 2006
...non-surgical program was physician directed and consisted of behavioral modifications, a very low calorie diet and pharmacotherapy with orlistat plus education ... - PR Newswire (press release),

Gastric Banding Effective for Mild to Moderate Obesity  May 1, 2006
Forty patients were randomized to the nonsurgical group, which included a very-low-calorie diet, advice for exercise, and treatment with orlistat over a 6 ... - Medscape (subscription)

Glaxo Launches Weight-Loss Website Prior to FDA Action on Diet ...  Apr 26, 2006
...in order to post comments or questions and take part in surveys -- is collecting thousands of email addresses for use in its orlistat marketing campaign. ... - Acomplia Report,

Cutting weight without the knife  Apr 23, 2006
FDA drugs that will be administered to the subjects are one of two medications: Sibutramine, which acts as an appetite suppressant, and Orlistat, which blocks ... - University at Buffalo The Spectrum,

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,


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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