Effect of the rate of niacin administration on the plasma and urine pharmacokinetics of niacin and its metabolites

Journal of Clinical Pharmacology

Volumn 47, Issue 6, 2007, Pages 681-688

  Menon, Rajeev M ^a   González, Mario A ^b   Adams, Marijke H ^c   Tolbert, Dwain S ^a   Leu, Jocelyn H ^a   Cefali, Eugenio A ^a  

^a Kos Pharmaceuticals Inc   (United States)

^b P'Kinetics   (United States)

^c MH Adams and Associates Inc   (United States)

Author keywords

N methylnicotinamide; Niacin; Nicotinamide; Nicotinamide N oxide; Nicotinuric acid

Indexed keywords

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

ADULT; ARTICLE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG URINE LEVEL; FLUSHING; HUMAN; MALE; NORMAL HUMAN; PRURITUS; SIDE EFFECT; URINALYSIS; URINE;

ADULT; AREA UNDER CURVE; DRUG ADMINISTRATION SCHEDULE; HUMANS; MALE; MIDDLE AGED; NIACIN; NIACINAMIDE; NICOTINIC ACIDS; VITAMIN B COMPLEX;

EID: 34249034223     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270007300264     Document Type: Article

References (19)

1. Niaspan [prescribing information]. Cranbury, NJ: Kos Pharmaceuticals, Inc ; 2005.
2. Pieper JA Overview of niacin formulations: differences in pharmacokinetics, efficacy, and safety. Am J Health Syst Pharm. 2003 ; 60: S9 - S14.
3. Pieper JA Understanding niacin formulations. Am J Manag Care. 2002 ; 8: S308 - S314.
4. Piepho RW The pharmacokinetics and pharmacodynamics of agents proven to raise high-density lipoprotein cholesterol. Am J Cardiol. 2000 ; 86: 35L - 40L.
5. 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.
6. 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.
7. Carlson LA Niaspan, the prolonged release preparation of nicotinic acid (niacin), the broad-spectrum lipid drug. Int J Clin Pract. 2004 ; 58: 706-713.
8. McCormack PL, Keating GM Prolonged-release nicotinic acid: a review of its use in the treatment of dyslipidaemia. Drugs. 2005 ; 65: 2719-2740.
9. Fumagalli R. Pharmacokinetics of nicotinic acid and some of its derivatives. In: Gey KF, Carlson LA, eds. Metabolic Effects of Nicotinic Acid and Its Derivatives. Bern, Switzerland: Hans Huber Publishers ; 1971: 33-49.
10. Carlson LA, Hanngren A. Initial distribution in mice of H3-labeled nicotinic acid studied with autoradiography. Life Sci. 1964 ; 3: 867-871.
11. Mrochek JE Metabolic responses of humans to ingestion of nicotinic acid and nicotinamide. Clin Chem. 1976 ; 22: 1821-1827.
12. 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.
13. Felsted R., Chaykin S. N-Methylnicotinamide oxidation in a number of mammals. J Biol Chem. 1967 ; 242: 1274-1279.
14. 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.
15. 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.
16. Carter EG Quantitation of urinary niacin metabolites by reversed-phase liquid chromatography. Am J Clin Nutr. 1982 ; 36: 926-930.
17. Shibata K. 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 ; 424: 23-28.
18. Neuvonen PJ, Roivas L., Laine K., Sundholm O. The bioavailability of sustained release nicotinic acid formulations. Br J Clin Pharmacol. 1991 ; 32: 473-476.
19. Figge HL, Figge J., Souney PF, Sacks FM, Shargel L., Janosik JE Comparison of excretion of nicotinuric acid after ingestion of two controlled release nicotinic acid preparations in man. J Clin Pharmacol. 1988 ; 28: 1136-1140.