One of the categories of drugs most frequently used by the elderly, and probably the most commonly self-prescribed is Non-steroidal anti-inflammatory drugs (NSAID). However, NSAIDs are one of the primary causes of adverse drug reactions and are notorious for their gastric toxicity. They also inhibit renal function and reduce the efficacy of diuretics and ACE-inhibitors, commonly used by elderly patients. Recent studies have shown that COX-2 is also important in renal physiology, so even though coxibs are undoubtedly safer than NSAIDs for gastric toxicity they are not devoid of renal toxicity, beyond their now cleared adverse effect on coronary heart disease risk. Both gastric and renal toxicity induced by traditional NSAIDs and coxibs seem to be related to their inhibition of prostaglandin (PG) but not (leukotriene) LT synthesis. The correct balance between PGs and LTs is essential for maintaining good health, but both classes of mediators also play an important role in the pathogenesis of several diseases. Recently, a new class of anti-inflammatory drugs, LOX/COX inhibitors, has been developed in order to simultaneously inhibit the synthesis of prostaglandins, thromboxanes and leukotrienes. Inhibition of leukotriene synthesis increases anti-inflammatory efficacy, particularly in rheumatic diseases, while reducing the risk of gastric damage. The LOX/COX inhibitor, licofelone, currently in Phase III, is the representative of this new class in the most advanced stage of development. Preliminary data seem promising, but further well-designed clinical trials in the elderly will be necessary before give a final evaluation.

Activity and role of Licofelone in osteoarthritis.

CICERO, ARRIGO FRANCESCO GIUSEPPE
Primo
Writing – Original Draft Preparation
;
2007

Abstract

One of the categories of drugs most frequently used by the elderly, and probably the most commonly self-prescribed is Non-steroidal anti-inflammatory drugs (NSAID). However, NSAIDs are one of the primary causes of adverse drug reactions and are notorious for their gastric toxicity. They also inhibit renal function and reduce the efficacy of diuretics and ACE-inhibitors, commonly used by elderly patients. Recent studies have shown that COX-2 is also important in renal physiology, so even though coxibs are undoubtedly safer than NSAIDs for gastric toxicity they are not devoid of renal toxicity, beyond their now cleared adverse effect on coronary heart disease risk. Both gastric and renal toxicity induced by traditional NSAIDs and coxibs seem to be related to their inhibition of prostaglandin (PG) but not (leukotriene) LT synthesis. The correct balance between PGs and LTs is essential for maintaining good health, but both classes of mediators also play an important role in the pathogenesis of several diseases. Recently, a new class of anti-inflammatory drugs, LOX/COX inhibitors, has been developed in order to simultaneously inhibit the synthesis of prostaglandins, thromboxanes and leukotrienes. Inhibition of leukotriene synthesis increases anti-inflammatory efficacy, particularly in rheumatic diseases, while reducing the risk of gastric damage. The LOX/COX inhibitor, licofelone, currently in Phase III, is the representative of this new class in the most advanced stage of development. Preliminary data seem promising, but further well-designed clinical trials in the elderly will be necessary before give a final evaluation.
2007
Cicero A.; Laghi L.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/106107
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