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Absorption
Absorbed rapidly after oral administration. Bioavailability is 2%.
Distribution
Vd is 2348 L/kg. Protein binding is 95%. Binds albumin and alpha-1-acid glycoprotein.
Metabolism
Extensive first pass metabolism to glucuronide conjugates.
Elimination
Primarily excreted in feces. Less than 0.2% is excreted unchanged in urine. Cl (oral) is 44.1 L/kg/h and t ½ is 27.7 to 32.5 h. Chronic dosing Cl is 40 to 60 L/kg/h.
Special Populations
Cirrhosis
Plasma concentrations increase 2.5 times. Safety and efficacy have not been evaluated any further.
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Cholestyramine
Major reduction in absorption and enterohepatic cycling of raloxifene; avoid concurrent use.
Highly protein-bound drugs (eg, clofibrate, indomethacin, naproxen, ibuprofen, diazepam, diazoxide)
May displace raloxifene from protein-binding sites, increasing the effects of raloxifene.
Warfarin
Raloxifene may decrease anticoagulant effect.
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