Carisoprodol Therapy and CYP2C19 Genotype

Review
In: Medical Genetics Summaries [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2012.
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Excerpt

Carisoprodol is a centrally acting muscle relaxant used to relieve acute back pain. Due to the risk of dependence and abuse, carisoprodol should only be used for treatment periods of up to two or three weeks. Carisoprodolol is a Schedule IV controlled substance and carisoprodol overdose can lead to CNS respiratory depression, seizures, and death.

Carisoprodol is metabolized by CYP2C19 to meprobamate, a sedative used to treat anxiety disorders. In individuals who have little or no CYP2C19 activity (“CYP2C19 poor metabolizers”), standard doses of carisoprodol can lead to a 4-fold increase in exposure to carisoprodol and a concomitant 50% reduced exposure to meprobamate compared to normal metabolizers. Approximately 3‑5% of Caucasians and Africans, and 15‑20% of Asians, are CYP2C19 poor metabolizers (1).

The FDA-approved drug label for carisoprodol states that caution should be used when administering carisoprodol to patients with reduced CYP2C19 activity and when co-administering drugs that inhibit or induce CYP2C19 (1). There are no data on the use of carisoprodol in pregnancy, and the efficacy, safety, and pharmacokinetics of carisoprodol have not been established in pediatric patients (less than 16 years of age).

Publication types

  • Review