ABSTRACT

Nonsteroidal anti-inflammatory drugs (NSAIDs), such as aspirin and ibuprofen, inhibit the cyclooxygenase activity of prostaglandin H synthase (PHS), the enzyme catalyzing the initial step in prostaglandin synthesis (formation of PGG2 and PGH2 from arachidonic acid) (Figure 20.1). Since prostaglandins are involved in inflammation, interrupting the synthesis of prostaglandins relieves the inflammation that accompanies many diseases, including rheumatoid arthritis, osteoarthritis, and systemic lupus erythematosus. Additionally, prostaglandins may be involved in body temperature elevation and pain production, accounting for the use of NSAIDs for fever reduction and analgesia. Overall, NSAID therapy is safe and effective, and the most significant adverse effects involve gastrointestinal irritation and ulceration.