is a potent, specific and long acting inhibitor of gastrointestinal
lipases. It exerts its therapeutic activity in the lumen of the
stomach and small intestine by forming a covalent bond with the
active serine site of the gastric and pancreatic lipases. The
inactivated enzyme is thus unable to hydrolyse dietary fat, in
the form of triglycerides, into absorbable free fatty acids and
monoglycerides. As undigested triglycerides are not absorbed,
the resulting caloric deficit has a positive effect on weight
control. Systemic absorption is therefore not needed for activity.
and repeated dose toxicity studies in rodents and dogs have demonstrated
a similar pattern of dose related effects across species, none
of which is considered relevant to the recommended use in man.
orlistat associated mutagenicity or genotoxicity has been observed
in a standard battery of five different short-term assays.
studies in rats and mice have not shown a carcinogenic potential
for orlistat at doses up to 1000mg/kg/day and 1500mg/kg/day respectively.
These doses are 182 and 125 times the daily human dose calculated
on a body surface area (mg/m 2) basis. There was a decreased incidence
of mammary fibroadenoma in female rats in the high dose group.
No orlistat associated adverse effects were observed in Segment
l, ll and Ill reproductive toxicity studies at doses ranging 62-241
times the recommended clinical dose.
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