An overview of the clinical pharmacokinetics of nabumetone. 1992

M L Hyneck
SmithKline Beecham Pharmaceuticals, King of Prussia, PA 19406.

Nabumetone is a new, nonacidic, nonsteroidal antiinflammatory drug. At least 80% of nabumetone is absorbed, and food, milk, and aluminum antacids increase the rate, but not the extent, of absorption. It is rapidly metabolized in the liver to 6-methoxy-2-naphthylacetic acid (6MNA), the major circulating active metabolite. At steady state, the time to maximum plasma concentration for 6MNA is 1 to 4 h. 6MNA has a very low clearance rate and long half-life (about 24 h). In general, steady state plasma concentrations of 6MNA increase in proportion with increases in the dose of nabumetone administered. Steady state plasma concentrations of 6MNA in the elderly are slightly higher than in healthy volunteers; however, this does not appear to be clinically significant. Preliminary studies in patients with impaired renal function indicate that the pharmacokinetics are not altered in patients with mild to moderate disease.

UI MeSH Term Description Entries
D007674 Kidney Diseases Pathological processes of the KIDNEY or its component tissues. Disease, Kidney,Diseases, Kidney,Kidney Disease
D008107 Liver Diseases Pathological processes of the LIVER. Liver Dysfunction,Disease, Liver,Diseases, Liver,Dysfunction, Liver,Dysfunctions, Liver,Liver Disease,Liver Dysfunctions
D002074 Butanones Derivatives of butanone, also known as methyl ethyl ketone (with structural formula CH3COC2H5).
D004435 Eating The consumption of edible substances. Dietary Intake,Feed Intake,Food Intake,Macronutrient Intake,Micronutrient Intake,Nutrient Intake,Nutritional Intake,Ingestion,Dietary Intakes,Feed Intakes,Intake, Dietary,Intake, Feed,Intake, Food,Intake, Macronutrient,Intake, Micronutrient,Intake, Nutrient,Intake, Nutritional,Macronutrient Intakes,Micronutrient Intakes,Nutrient Intakes,Nutritional Intakes
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077430 Nabumetone A butanone non-steroidal anti-inflammatory drug and cyclooxygenase-2 (COX2) inhibitor that is used in the management of pain associated with OSTEOARTHRITIS and RHEUMATOID ARTHRITIS. 4-(6-Methoxy-2-naphthyl)-2-butanone,Apo-Nabumetone,Arthraxan,BRL 14777,Gen-Nabumetone,Listran,Mebutan,Nabucox,Nabumeton,Relafen,Relif,Relifex,Rhoxal-nabumetone,ApoNabumetone,Rhoxal nabumetone
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults
D000368 Aged A person 65 years of age or older. For a person older than 79 years, AGED, 80 AND OVER is available. Elderly
D000375 Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. Senescence,Aging, Biological,Biological Aging
D000863 Antacids Substances that counteract or neutralize acidity of the GASTROINTESTINAL TRACT. Alkalinizing Agent,Antacid,Alkalinizing Agents,Agent, Alkalinizing,Agents, Alkalinizing

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