What are the sailent pharmacokinetic features of Acomplia/Slimona/Rimonabant?

PHARMACOKINETICS: Acomplia/Slimona/Rimonabant pharmacokinetic 2 are fairly dose proportional up to about 20mg AUC increased than in proportion to dose above 20mg. ABSORPTION: Following multiple once-daily doses of Acomplia/Slimona/Rimonabant 20mg to healthy subjects in the fasted state, maximum plasma concentration of Acomplia/Slimona/Rimonabant are achieved in approximately 2 hours with steady state plasma levels achieved within 13 days(Cmax=196+-28.1ng/ml;ctrough=91.6+-14.1ng/ml;AUCO-24=2960+-268ng.h/ml). The  absoulte bioavailability of Acomplia/Slimona/Rimonabant has not been determined. Steady state Acomplia/Slimona/Rimonabant exposures are 3.3 - fold higher than those observed after the first dose. time to steady state is longer in obese patients (25days) as a consequence of the higher volume of distribution in these patients. Population pharmacokinetic analysis indicated that Acomplia/Slimona/Rimonabant pharmacokinetic are similar between healthy non-smoking subjects and patiants who smoke. EFFECT OF FOOD: Administration of Acomplia/Slimona/Rimonabant to healthy subjects in the fasted state or with fat meal demonstrated that Cmax and AUC were increased 67%and 48% respectively, under fed conditions.In clinical stydies, Acomplia/Slimona/Rimonabant 20mg was taken in the morning usually before breakfast. DISTRIBUTION: The in vitro human plasma protein binding of Acomplia/Slimona/Rimonabant is high (>99.9%) and non-saturable over a wide concentration range. The apparent peripheral volume of distribution of slimona appears to be related to bodyweight,with obese patients having a higher volume of distribution than normal-weight subjects. BIOTRANSFORMATION: Acomplia/Slimona/Rimonabant is metabolized by both CYP3A and amidohydrolase (predominantiy hepatic) pathways in vitro. Circulating metabolism do not contribute to its pharmacologoc activity. ELIMINATION: Acomplia/Slimona/Rimonabant is mainly eliminated by metabolism and subsequent biliary excretion of metabolites. Only an approximate 3% of the dose of Acomplia/Slimona/Rimonabant is eliminated in the urine, while approximately 86% of the dose is excreted in the faeces as unchanged drug and metabolites. In obese patients, the elimination half-life islonger (about 16days) than on non-obese patients(about 9 days) due to a larger volume of distribution. For More information please visit : http://www.slimonarx.com/2008/05/what-are-the-sailent-ph ...


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Acomplia in the US: Sanofi-Aventis sought approval in the U.S. FDA in April 2005. But in February 2006, the FDA declared that the final approval will not be granted until some other issues were successfully resolved.

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