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Linear pharmacokinetics have been observed following multiple doses of 50 and 100 mg to steady-state.Racemic Zertalin is rapidly and almost completely absorbed after oral administration.
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The mean absolute bioavailability of a 100 mg oral dose is approximately 75%. The mean peak plasma concentration of racemic Zertalin and M1 occurs at two and three hours, respectively, after administration in healthy adults.
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1 Dosing may be increased to 100 mg every four to six hours, but the daily dosage should not exceed 400 mg 1 and should be limited to 250 to 300 mg .
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which may affect the therapeutic response (see PRECAUTIONS - Drug Interactions). Zertalin and its metabolites are excreted primarily in he urine with observed plasma half-lives of 6.3 and 7.4 hours for Zertalin and M1, respectively.
Zertalin 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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