Plasma and urine pharmacokinetics of niacin and its metabolites from an extended-release niacin formulation

International Journal of Clinical Pharmacology and Therapeutics

Volumn 45, Issue 8, 2007, Pages 448-454

  Menon, R M ^a   Adams, M H ^b   Gonzales M A ^c   Tolbert, D S ^a   Leu, J H ^a   Cefali, E A ^a  

^a Kos Pharmaceuticals Inc   (United States)

^b MH Adams and Associates Inc   (United States)

^c P'Kinetics International   (United States)

Author keywords

Metabolism; Niacin; Pharmacokinetics

Indexed keywords

DRUG METABOLITE; N METHYL 2 PYRIDONE 5 CARBOXAMIDE; N METHYLNICOTINAMIDE; NICOTINAMIDE; NICOTINAMIDE N OXIDE; NICOTINIC ACID; NICOTINURIC ACID; UNCLASSIFIED DRUG;

ADULT; AREA UNDER THE CURVE; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIZZINESS; DRUG BLOOD LEVEL; DRUG EXCRETION; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; DRUG URINE LEVEL; HUMAN; HUMAN EXPERIMENT; LOW FAT DIET; MALE; NORMAL HUMAN; OPEN STUDY; PARESTHESIA; PLASMA HALF LIFE; PRURITUS; SIDE EFFECT; VASODILATATION; VOLUNTEER;

EID: 34547841472     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/cpp45448     Document Type: Article

References (22)

1. Carlson LA, Hanngren A. Initial distribution in mice of H3-labeled nicotinic acid studied with autoradiography Life Sci. 1964; 3: 867-871.
2. Carlson LA. Niaspan, the prolonged release preparation of nicotinic acid (niacin), the broad-spectrum lipid drug. Int J Clin Pract. 2004; 58: 706-713.
3. Carter EG. Quantitation of urinary niacin metabolites by reversed-phase liquid chromatography. Am J Clin Nutr. 1982; 36: 926-930.
4. Cefali EA, Bova DJ. Methods for reducing flushing in individuals being treated with nicotinic acid for hyperlipidemia. US Patent No. 6,676,967; 2004.
5. Ding RW, Kolbe K, Merz B, Vries JD, Weber E, Benet ZB. Pharmacokinetics of nicotinic acid-salicylic acid interaction. Clin Pharmacol Ther. 1989; 46: 642-647.
6. Felsted R, Chaykin S. N-Methylnicotinamide oxidation in a number of mammals. J Biol Chem. 1967; 242: 1274-1279.
7. Figge HL, Figge J, Souney PF, Mutnick AH, Sacks F. Nicotinic acid: a review of its clinical use in the treatment of lipid disorders. Pharmacotherapy 1988a; 8: 287-294.
8. Figge HL, Figge J, Souney PF, Sacks FM, Shargel L, Janosik JE. Comparison of excretion of nicotinic acid after ingestion of two controlled release nicotinic acid preparations in man. J Clin Pharmacol. 1988b; 28: 1136-1140.
9. Fumagalli R. Pharmaocokinetics of nicotine acid and some of its derivates. In: Carlson LA, Gey KF (eds). Metabolic effects of nicotinic acid and its derivatives. Bern - Stuttgart - Vienna: Hans Huber Publishers; 1971. pp. 33-49.
10. Harthon L, Svedmyr N. Plasma half-life of nicotinic acid in man. Int Res Commun Sys. 1973; 8-13-2.
11. Hengen N, Seiberth V, Hengen M. High-performance liquid-chromatographic determination of free nicotinic acid and its metabolite, nicotinuric acid, in plasma and urine. Clin Chem. 1978; 24: 1740-1743.
12. McCormack PL, Keating GM. Prolonged-release nicotinic acid: a review of its use in the treatment of dyslipidaemia. Drugs. 2005; 65: 2719-2740.
13. Morgan JM, Capuzzi DM, Guyton JR. A new extended-release niacin (Niaspan): efficacy, tolerability, and safety in hypercholesterolemic patients. Am J Cardiol. 1998; 82: 29U-41U.
14. Mrochek JE. Metabolic responses of humans to ingestion of nicotinic acid and nicotinamide. Clin Chem. 1976; 22: 1821-1827.
15. Neuvonen PJ, Roivas L, Laine K, Sundholm O. The bioavailability of sustained release nicotinic acid formulations. Br J Clin Pharmacol. 1991; 32: 473-476.
16. Niaspan (package insert). Cranbury, NJ, USA: Kos Pharmaceuticals Inc.; 2005.
17. Pieper JA. Understanding niacin formulations. Am J Manag Care. 2002; 8: 308-314.
18. Pieper JA. Overview of niacin formulations: differences in pharmacokinetics, efficacy, and safety. Am J Health Syst Pharm. 2003; 60: 9-14.
19. Piepho RW. The pharmacokinetics and pharmacodynamics of agents proven to raise high-density lipoprotein cholesterol. Am J Cardiol. 2000; 86: 35L-40L.
20. Shibata K. Simultaneous measurement of nicotinic acid and its major metabolite, nicotinuric acid, in blood and urine by reversed-phase high performance liquid chromatography. Agric Biol Chem. 1988; 52: 2973-2976.
21. Shibata K et al. Simultaneous micro-determination of nicotinamide and its major metabolites, N-methyl-2-pyridone-5-carboxamide and N-methyl-4-pyridone-3-carboxamide, by high-performance liquid chromatography. J Chromatogr. 1988; 425: 22-28.
22. Stern RH, Freeman D, Spence JD. Differences in metabolism of time-release and unmodified nicotinic acid: explanation of the differences in hypolipidemic action. Metabolism. 1992; 8: 879-881.