Pharmacologic properties of 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.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D001168:Arthritis / Q000188:drug therapy; D001711:Biotransformation; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006168:Guinea Pigs; D007249:Inflammation / Q000188:drug therapy; D010648:Phenylacetates / Q000378:metabolism; D010654:Phenylbutyrates; D011422:Propionates / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D013467:Sulindac / Q000627:therapeutic use; D013585:Synovitis / Q000188:drug therapy
D000893:Anti-Inflammatory Agents; D000894:Anti-Inflammatory Agents, Non-Steroidal; D010648:Phenylacetates; D010654:Phenylbutyrates; D011422:Propionates; D013467:Sulindac; C012776:biphenylylacetic acid; C010725:fenbufen