Carisoprodol is metabolized in the liver via cytochrome P450 enzyme, CYP2C19. This enzyme exhibits genetic polymorphism . For example, 15-20% of Asian populations may be expected to be poor metabolizers. For Caucasians and Blacks, the prevalence of poor metabolizers is 3-5%. Following a single 350 mg dose of carisoprodol, the corresponding normalized peak concentration of meprobamate, which is a metabolite of carisoprodol, was 2.08 ± 0.48 ug/mL. These levels are approximately ¼ of those seen following a single 400 mg dose of meprobamate.
Elimination
Carisoprodol is eliminated by both renal and non-renal routes with a terminal elimination half-life of 2.44 ± 0.93 hours. It is dialyzable by peritoneal and hemodialysis.
Special Populations
The pharmacokinetic profile of carisoprodol in patients with renal impairment or hepatic impairment has not been evaluated. Because carisoprodol is metabolized by the liver and excreted by the kidneys, possible increased exposure of carisoprodol is expected if hepatic and/or renal function is impaired. The drug should be used with caution in patients with impaired hepatic or renal function.
The pharmacokinetic profile of carisoprodol in elderly patients has not been evaluated.
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