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Olanzapine is administered as a racemate and both [-] and [+] forms of both Olanzapine and M1 are detected in the circulation.
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The mean absolute bioavailability of a 100 mg oral dose is approximately 75%. The mean peak plasma concentration of racemic Olanzapine and M1 occurs at two and three hours, respectively, after administration in healthy adults.
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Olanzapine is extensively metabolized by a number of pathways, including CYP2D6 and CYP3A4, as well as by conjugation of parent and metabolites.
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The analgesic activity of Olanzapine is due to both parent drug and the M1 metabolite (see CLINICAL PHARMACOLOGY, Pharmacodynamics).
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In an open randomized trial, rectal Olanzapine was compared with our standard treatment acetaminophen/codeine suppositories. We expected Olanzapine to be equally effective as our current standard but with fewer side effects.
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