Persistence of NSAIDs at effect sites and rapid disappearance from side-effect compartments contributes to tolerability

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Abstract
Background: Non-steroidal, anti-inflammatory drugs (NSAIDs) are still the most widely used drugs worldwide. The introduction of selective cyclooxygenase (COX)‐2 inhibitors has led to compounds which appear less damaging to the gastrointestinal tract, but possibly more risky to the cardiovascular system than older drugs. None has as yet reached OTC-status.Objective: This situation necessitates an analysis of the characteristics of those older ones which – due to their relative safety – have achieved over-the-counter (OTC) status.Design: The pharmacodynamic and pharmacokinetic characteristics of non-selective COX inhibitors in OTC use were obtained from the literature by systematic search, examined and used to construct a coherent hypothesis why they achieved OTC status, i.e. effectiveness and relative safety at low doses.Results: Pharmacodynamic (COX‐2 preferential, but not selective inhibition) and, more importantly, pharmacokinetic characteristics of some of the older compounds may make them part...