Aryl and Heteroarylakanoic Acid Type Drugs

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The prototypes of this large class of NSAIDs are in-domethacin and ibuprofen. These drugs are indicated for the relief of acute and chronic rheumatoid arthritis and osteoarthritis. In addition, a number of drugs of this class are also useful in ankylosing spondylitis, acute gouty arthritis, bursitis, and tendinitis.

Adverse reactions are common with the use of these drugs but usually do not result in serious morbidity. GI and CNS effects and prolonged bleeding may occur. Fluid retention, skin rashes, and ocular toxicity also occur, but with much lower frequency than with the sali-cylates. The selectivity for COX-1 and COX-2 varies from drug to drug and accounts for some of the differences in toxicity. None of the agents seems to be clearly more efficacious than the others; however, they generally cause less GI blood loss and fewer other adverse reactions than does aspirin, and the overall incidence of adverse reactions may be lower with these drugs.


Indomethacin (Indocin) is used in the treatment of acute gouty arthritis, rheumatoid arthritis, ankylosing spondylitis, and osteoarthritis. It is not recommended for use as a simple analgesic or antipyretic because of its potential for toxicity. While indomethacin inhibits both COX-1 and COX-2, it is moderately selective for COX-1. It produces more CNS side effects than most of the other NSAIDs. Severe headache occurs in 25 to 50% of patients; vertigo, confusion, and psychological disturbances occur with some regularity. GI symptoms also are more frequent and severe than with most other

NSAIDs. Hematopoietic side effects (e.g., leukopenia, hemolytic anemia, aplastic anemia, purpura, thrombocytopenia, and agranulocytosis) also may occur. Ocular effects (blurred vision, corneal deposits) have been observed in patients receiving indomethacin, and regular ophthalmological examinations are necessary when the drug is used for long periods. Hepatitis, jaundice, pancreatitis, and hypersensitivity reactions also have been noted.

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