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Abstract
1. The pharmacokinetics of feprazone have been studied in 10 patients with rheumatoid arthritis (RA), and in a further six patients with renal impairment (RI) who were not suffering from rheumatoid disease.
2. For RA patients, the mean elimination half-life (t1/2) of feprazone after a single oral dose was 21 ± 5h (SD), the mean apparent clearance (Cl) was 0.012±0.0091/h per kg, and the mean apparent volume of distribution (Vd) was 0.33±0.71/kg. Corresponding values for RI patients were 25±13h, 0.016±0.0111/h per kg, and 0.46±0.241/kg, respectively.
3. These results show no impairment of the elimination of feprazone in RA or RI patients; Vd and Cl are greater than in healthy young volunteers or elderly subjects, the AUC values are lower, but t1/2 values are similar in all groups.
4. It is suggested that the greater Cl and Vd, and lower AUC, in RA and RI patients may be due to renal insufficiency and decreased plasma protein binding of feprazone and its metabolite, or to induction of glucuronyl transferase activity by the prior medication, thus enhancing the formation of the major metabolite, the C(4)-glucuronide, and increasing drug elimination.