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Nonsteroidal Anti-inflammatory Drugs

Nonsteroidal Anti-inflammatory Drugs Abstract Over the past decade, many new nonsalicylate, nonsteroidal anti-inflammatory drugs (NSAIDs) have been introduced in the United States. These include fenoprofen, ibuprofen, meclofenamate, naproxen, piroxicam, sulindac, and tolmetin in addition to indomethacin and phenylbutazone, which were previously available. These drugs have added to our therapeutic armamentarium for management of degenerative joint disease (DJD) and rheumatoid arthritis (RA) as well as other rheumatic and nonrheumatic disorders. CLASSIFICATION AND CLINICAL PHARMACOLOGY Figure 1 provides a chemical classification of currently available NSAIDs. Although these groupings do not hold notable clinical relevance, differences among the classes may be unveiled as we gain more understanding of their pharmacologic activity.All NSAIDs are rapidly absorbed and highly protein bound with peak serum levels occurring within four hours after ingestion. Half-life varies from two to 50 hours with excretion via urine, bile, and feces as inactive metabolites, with less than 10% excreted unchanged. At pharmacologic doses, NSAIDs References 1. Vane JR: Inhibition of prostaglandin synthesis as a mechanism of action of aspirin-like drugs. Nature New Biol 1971;231:233-235.Crossref 2. Wasner C, Britton MC, Kraines G, et al: Nonsteroidal agents in rheumatoid arthritis and ankylosing spondylitis. JAMA 1981;246:2168-2172.Crossref 3. Coles LS, Fries JF, Kraines RG, et al: From experiment to experience: Side effects of non-steroidal anti-inflammatory drugs. Am J Med 1983;74: 820-828.Crossref 4. Rainsford KD: An analysis of the gastro-intestinal side-effects of nonsteroidal anti-inflammatory drugs, with particular reference to comparative studies in man and laboratory species. Rheumatol Int 1982;2:1-10.Crossref 5. Caruso I, Porro GB: Gastroscopic evaluation of anti-inflammatory agents. Br Med J 1980;280:75-78.Crossref 6. Dunn MJ, Hood VL: Prostaglandins and the kidney. Am J Physiol 1977;233:169-184. 7. Donker AJM, Arisz L, Brentjens JRH, et al: The effect of indomethacin on kidney function and plasma renin activity in man. Nephron 1976;17:288-296.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Internal Medicine American Medical Association

Nonsteroidal Anti-inflammatory Drugs

Archives of Internal Medicine , Volume 144 (8) – Aug 1, 1984

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Publisher
American Medical Association
Copyright
Copyright © 1984 American Medical Association. All Rights Reserved.
ISSN
0003-9926
eISSN
1538-3679
DOI
10.1001/archinte.1984.00350200170024
Publisher site
See Article on Publisher Site

Abstract

Abstract Over the past decade, many new nonsalicylate, nonsteroidal anti-inflammatory drugs (NSAIDs) have been introduced in the United States. These include fenoprofen, ibuprofen, meclofenamate, naproxen, piroxicam, sulindac, and tolmetin in addition to indomethacin and phenylbutazone, which were previously available. These drugs have added to our therapeutic armamentarium for management of degenerative joint disease (DJD) and rheumatoid arthritis (RA) as well as other rheumatic and nonrheumatic disorders. CLASSIFICATION AND CLINICAL PHARMACOLOGY Figure 1 provides a chemical classification of currently available NSAIDs. Although these groupings do not hold notable clinical relevance, differences among the classes may be unveiled as we gain more understanding of their pharmacologic activity.All NSAIDs are rapidly absorbed and highly protein bound with peak serum levels occurring within four hours after ingestion. Half-life varies from two to 50 hours with excretion via urine, bile, and feces as inactive metabolites, with less than 10% excreted unchanged. At pharmacologic doses, NSAIDs References 1. Vane JR: Inhibition of prostaglandin synthesis as a mechanism of action of aspirin-like drugs. Nature New Biol 1971;231:233-235.Crossref 2. Wasner C, Britton MC, Kraines G, et al: Nonsteroidal agents in rheumatoid arthritis and ankylosing spondylitis. JAMA 1981;246:2168-2172.Crossref 3. Coles LS, Fries JF, Kraines RG, et al: From experiment to experience: Side effects of non-steroidal anti-inflammatory drugs. Am J Med 1983;74: 820-828.Crossref 4. Rainsford KD: An analysis of the gastro-intestinal side-effects of nonsteroidal anti-inflammatory drugs, with particular reference to comparative studies in man and laboratory species. Rheumatol Int 1982;2:1-10.Crossref 5. Caruso I, Porro GB: Gastroscopic evaluation of anti-inflammatory agents. Br Med J 1980;280:75-78.Crossref 6. Dunn MJ, Hood VL: Prostaglandins and the kidney. Am J Physiol 1977;233:169-184. 7. Donker AJM, Arisz L, Brentjens JRH, et al: The effect of indomethacin on kidney function and plasma renin activity in man. Nephron 1976;17:288-296.Crossref

Journal

Archives of Internal MedicineAmerican Medical Association

Published: Aug 1, 1984

References