Pharmacokinetics of Fluvoxamine Maleate in Patients with Liver Cirrhosis after Single-Dose Oral Administration

Summary

The pharmacokinetics of fluvoxamine maleate were investigated in 13 patients with biopsy-proven liver cirrhosis. They received a single oral 100mg dose as an enteric-coated tablet, and plasma samples were collected up to 168h after administration. Geometric mean values for peak plasma concentrations and area under the plasma concentration-time curves (AUC) were 39 µg/L and 1338 µg · h/L, respectively. Mean (± SD) elimination half-life (t_½) was 25 ± 11h, and increased with higher plasma bilirubin levels, although no relationship between bilirubin and AUC was observed.

AUC was about 50% higher in patients than in healthy volunteers from another similar study. This was mainly because of a longer t_½. Although there is a great overlap between AUC values of fluvoxamine in patients and healthy volunteers, it is nevertheless concluded that in patients with signs of active liver disease, e.g. raised bilirubin, it is wise to lower the initial daily dose and to carefully monitor the patient during subsequent upward dose adjustments.