Pharmaceutical And Pharmacological Issues

Many preparations have been developed in an attempt to circumvent the side effects of NSAIDs. A systematic review comparing routes of administration suggests that the oral route should be used when patients can swallow. The intramuscular and rectal routes are associated with a higher adverse effects rate including pain on injection, rectal irritation, and diarrhea.9[I]

A large in vitro analysis of COX-1 and COX-2 selectivity for NSAIDs has been performed for a wide range of agents.75 This demonstrates the relative specificities for COX-1 against COX-2, but also demonstrates the level of COX-1 inhibition when COX-2 is inhibited by 80 percent. The postulate is that this is the level of COX-2 inhibition required for a therapeutic benefit. It is suggested that the agents with greatest COX-1 selectivity correlate with those that have higher GI side effects.

The NSAIDs are often grouped by chemical structure. This does not really aid drug choice and lack of efficacy of one member of a class does not exclude other members of the same class from being effective.76

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