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In general, both enantiomers of Raloxifene and M1 follow a parallel time course in the body following single and multiple doses although small differences (~10%) exist in the absolute amount of each enantiomer present.
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Raloxifene is extensively metabolized by a number of pathways, including CYP2D6 and CYP3A4, as well as by conjugation of parent and metabolites.
A single i.m. dose of Raloxifene is useful pre-treatment to minimize the risk of acid aspiration during operation,
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It is slightly soluble in water and freely soluble in alcohol,
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Raloxifene is well absorbed orally with an absolute bioavailability of 75%. Raloxifene has a volume of distribution of approximately 2.7 L/kg and is only 20% bound to plasma proteins.
Raloxifene is administered as a racemate and both [-] and [+] forms of both Raloxifene and M1 are detected in the circulation.
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