sulindac and fenbufen

Fenbufen (Cinopal) is an orally active nonsteroidal anti-inflammatory drug with analgesic and antipyretic activity. Like clinically used nonsteroidal anti-inflammatory drugs, it shows activity in a wide spectrum of laboratory tests in mice, rats, guinea pigs, and dogs. Fenbufen has a long duration of anti-inflammatory and analgesic activity. Mechanistic studies indicate that fenbufen has no intrinsic effect on cyclooxygenase activity, whereas its major metabolite, biphenylacetic acid, is a potent inhibitor of prostaglandin synthesis. These observations indicate that fenbufen is a pro-drug and account for its low ulcerogenic potential. Anti-inflammatory pro-drugs that are readily metabolized to the biologically active molecule are expected to retain a favorable anti-inflammatory to ulcerogenic ratio because the gastrointestinal tract is not exposed to a large concentration of the active molecule. Comparative studies in the type II collagen arthritis model indicate that the anti-inflammatory properties of fenbufen are more potent than those of a second nonsteroidal anti-inflammatory drug, sulindac.

Topics: Animals; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Biotransformation; Dogs; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Guinea Pigs; Inflammation; Phenylacetates; Phenylbutyrates; Propionates; Rats; Sulindac; Synovitis

Topics: Anti-Inflammatory Agents; Arthritis; Aspirin; Diclofenac; Humans; Ibuprofen; Indomethacin; Naproxen; Phenylbutazone; Phenylbutyrates; Piroxicam; Propionates; Sulindac; Thiazines

Topics: Anti-Inflammatory Agents; Arthritis, Rheumatoid; Clinical Trials as Topic; Double-Blind Method; Gastrointestinal Diseases; Humans; Indomethacin; Phenylbutazone; Phenylbutyrates; Propionates; Sulindac

Topics: Aged; Anemia, Aplastic; Anti-Inflammatory Agents, Non-Steroidal; Female; Humans; Phenylbutyrates; Recurrence; Sulindac

The effect of fenbufen and sulindac, two novel antiinflammatory agents, on the developing and established lesion of type II collagen arthritis was investigated. Using paw diameter and radiology as parameters, these studies suggest that fenbufen is more efficacious than sulindac in this model.

Topics: Animals; Anti-Inflammatory Agents; Arthritis; Collagen; Indenes; Male; Phenylbutyrates; Propionates; Rats; Rats, Inbred Strains; Sulindac

Topics: Analgesics; Animals; Anti-Inflammatory Agents; Arthritis; Erythema; Guinea Pigs; Phenylacetates; Phenylbutyrates; Propionates; Rats; Sulindac; Ultraviolet Rays