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The analgesic activity of Rebetol is due to both parent drug and the M1 metabolite (see CLINICAL PHARMACOLOGY, Pharmacodynamics).
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Rebetol can increase the risk of seizure in epileptic patients, especially with simultaneous use of tricyclic antidepressants,
The mean absolute bioavailability of a 100 mg oral dose is approximately 75%. The mean peak plasma concentration of racemic Rebetol and M1 occurs at two and three hours, respectively, after administration in healthy adults.
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Rebetol was not mutagenic in the following assays:
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Rebetol has a volume of distribution of approximately 2.7 L/kg and is only 20% bound to plasma proteins.
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