![]() To minimize the potential risk for an adverse CV event in patients treated with an NSAID, the lowest effective dose should be used for the shortest duration possible. Patients with known CV disease or risk factors for CV disease may be at greater risk. All NSAIDs, both COX-2 selective and nonselective, may have a similar risk. In contrast to aspirin, salsalate causes no greater fecal gastrointestinal blood loss than placeboĬlinical trials of several COX-2 selective and nonselective NSAIDs of up to three years duration have shown an increased risk of serious cardiovascular (CV) thrombotic events, myocardial infarction, and stroke, which can be fatal. In vivo product of salsalate, in the treatment of arthritic disorders has been establishedĥ,6. The usefulness of salicylic acid, the active Unlike aspirin, salsalate does not inhibit platelet aggregationĤ. In vivo 1, providing anti-inflammatory activity equivalent to aspirinģ. In vitro, salsalate appears to selectively inhibit prostaglandin synthesis Although salicylic acid (the primary metabolite of salsalate) is a weak inhibitor of prostaglandin synthesis The mode of anti-inflammatory action of salsalate and other nonsteroidal anti-inflammatory drugs is not fully defined. Food slows the absorption of all salicylates including salsalate. The parent compound does not show capacity-limited biotransformation, nor does it accumulate in the plasma on multiple dosing. Therapeutic blood levels continue for up to 16 hours after the last dose. Thus, dosing with salsalate twice a day will satisfactorily maintain blood levels within the desired therapeutic range (10 to 30 mg/100 ml) throughout the 12-hour intervals. Such capacity-limited biotransformation results in an increase in the half-life of salicylic acid from 3.5 to 16 or more hours. Salicylic acid biotransformation is saturated at anti-inflammatory doses of salsalate. Thus, the amount of salicylic acid available from salsalate is about 15% less than from aspirin, when the two drugs are administered on a salicylic acid molar equivalent basis (3.6 g salsalate/5 g aspirin). About 13% is excreted through the kidneys as a glucuronide conjugate of the parent compound, the remainder as salicylic acid and its metabolites. A significant portion of the parent compound is absorbed unchanged and undergoes rapid esterase hydrolysis in the body: its half-life is about one hour. Salsalate is insoluble in acid gastric fluids (<0.1 mg/ml at pH 1.0), but readily soluble in the small intestine where it is partially hydrolyzed to two molecules of salicylic acid.
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