The effect of cholestyramine on the pharmacokinetics of meloxicam, a new non-steroidal anti-inflammatory drug (NSAID), in man.
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 l.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 tenoxicam.
Busch
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U
Department of Pharmacokinetics, Karl Thomae GmbH, Biberach, Germany.
Heinzel
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G
Narjes
H
H
D000284:Administration, Oral; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D002792:Cholestyramine Resin / Q000494:pharmacology*; D004347:Drug Interactions; D006801:Humans; D008297:Male; D000077239:Meloxicam; D008875:Middle Aged; D010599:Pharmacokinetics; D013843:Thiazines / Q000493:pharmacokinetics*; D013844:Thiazoles / Q000493:pharmacokinetics*; D013997:Time Factors; D014838:Volunteers
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013843:Thiazines; D013844:Thiazoles; D002792:Cholestyramine Resin; D000077239:Meloxicam