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PHARMACOKINETICS

Effect of the Rate of Niacin Administration on the Plasma and Urine Pharmacokinetics of Niacin and Its Metabolites

Rajeev M. Menon, PhD, Mario A. González, PhD, Marijke H. Adams, PharmD, PhD, Dwain S. Tolbert, PhD, Jocelyn H. Leu, PharmD, PhD and Eugenio A. Cefali, PharmD, PhD

From Kos Pharmaceuticals, Inc, Weston, Florida (Dr Menon, Dr Tolbert, Dr Leu, Dr Cefali); P'Kinetics, International, Inc, Pembroke Pines, Florida (Dr González); and MH Adams & Associates, Inc, Davie, Florida (Dr Adams).

The metabolic profile of niacin is influenced by the rate of niacin administration. This study characterizes the effect of administration rate on the pharmacokinetics of niacin and its metabolites. Twelve healthy males were enrolled in an open-label, dose-rate escalation study and received 2000 mg niacin at 3 different dosing rates. Plasma was analyzed for niacin, nicotinuric acid, nicotinamide, and nicotinamide-N-oxide. Urine was analyzed for niacin and the metabolites nicotinuric acid, nicotinamide, nicotinamide-N-oxide, N-methylnicotinamide, and N-methyl-2-pyridone-5-carboxamide. Cmax and AUC0-t for niacin and nicotinuric acid increased with an increase in dosing rate. The changes observed in plasma nicotinamide and nicotinamide-N-oxide parameters, however, did not correlate to dosing rate. The total amount of niacin and metabolites excreted in urine was comparable for all 3 treatments. However, with the increase in dosing rate, urine recovery of niacin and nicotinuric acid showed a significant increase, whereas N-methyl-2-pyridone-5-carboxamide and N-methylnicotinamide showed a significant decrease.

Key Words: Niacin • nicotinuric acid • nicotinamide • nicotinamide-N-oxide • N-methylnicotinamide

Address for reprints: Rajeev M. Menon, PhD, Kos Pharmaceuticals, Inc, 2100 N Commerce Parkway, Weston, FL 33326; e-mail: menonrm2000{at}gmail.com.






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