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Buspirone is authorised in the world under the following brand names: Ansial, Ansiced, Anxiron, Axoren, Bespar, Buspar, Buspimen, Buspinol, Buspisal, Censpar, Lucelan, Narol, Travin, Wellbutrin XL.

CYP3A4 Isoenzyme Metabolism

The CYP3A enzyme family is composed of four isozymes involved with metabolism: CYP3A, CYP3A4, CYP3A5, and CYP3A7. Of these, the CYP3A4 isozyme is the most common; however, these enzymes are so closely related, they are often referred to collectively by their subfamily name, CYP3A. The CYP3A enzyme family is responsible for hepatic metabolism of approximately 60% of currently available pharmaceutical agents.A significant quantity of CYP3A4 isozyme is present in the intestinal mucosa, especially in the duodenum, jejunum and, to a lesser extent, in the ileum. This isozyme is responsible for a majority of the first-pass metabolism of compounds. Common substrates for CYP3A4 include steroids, some tricyclic antidepressants, antifungals, benzodiazepines, calcium-channel blockers, hormones, macrolides, selective serotonin reuptake inhibitors (SSRIs), R-warfarin, etc. Inhibitors of CYP3A4 include some antifungals (e.g., azoles), antivirals (e.g., protease inhibitors), anticonvulsants, HMG-CoA reductase inhibitors (e.g., statins), macrolides, and verapamil. Inducers of CYP3A4 include glucocorticoids, rifampins, and some anticonvulsants. A comprehensive listing of drugs involved with CYP3A4 are listed in Table 1. To date, no data have been reported that suggest 3A4 isoenzymes exhibit genetic polymorphism.

Some drug metabolism by the CYP3A4 isozyme in the intestinal tract can be inhibited by ingesting grapefruit juice, which contains bioflavonoids (e.g., quercetin, kaempferol, and naringenin). Some calcium-channel modulators (e.g., nitrendipine, nifedipine, and felodipine) and other drugs metabolized by CYP3A4 may be affected. In one study the AUC for felodipine was increased two-to-three fold following oral administration along with grapefruit juice. The metabolism of buspirone, cyclosporine, terfenadine, midazolam, warfarin and caffeine can also be inhibited by grapefruit juice.