The effect of cholestyramine on the pharmacokinetics of meloxicam, a new non-steroidal anti-inflammatory drug (NSAID), in man

U. Busch, G. Heinzel and H. Narjes

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Abstract

The influence of multiple oral doses of cholestyramine on the single dose pharmacokinetics of meloxicam has been studied in 12 healthy male volunteers. Each subject received on two occasions a single IV injection of meloxicam 30 mg. The cholestyramine group received the material suspended in water 3 times a day. Compared to controls, cholestyramine accelerated the elimination of meloxicam. The mean terminal phase elimination half-life was reduced from 19.5 h to 12.7 h due to an increase in clearance of the drug (0.426 vs 0.636 1·h–1). Also, as a consequence of increased clearance in the presence of cholestyramine, the mean residence time of the drug in the body was significantly decreased (39%) P<0.01. however,="" the="" volume="" of="" distribution="" for="" meloxicam="" was="" largely="" unaffected="" by="" cholestyramine="" which="" suggests="" that="" meloxicam="" undergoes="" gut="" recirculation.="" these="" changes="" are="" of="" the="" same="" magnitude="" as="" those="" previously="" reported="" for="" the="" structurally="" related="" piroxicam="" and="" are="" much="" smaller="" than="" those="" observed="" for="">

Key words  Meloxicam - Cholestyramine - NSAID pharmacokinetics - drug interaction - clearance - elimination - half-life - enteric recirculation processes

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