Gj. Lawson et al., METHYLPREDNISOLONE-HEMISUCCINATE AND ITS METABOLITES IN SERUM, URINE AND BILE FROM 2 PATIENTS WITH ACUTE GRAFT-REJECTION, British journal of clinical pharmacology, 39(2), 1995, pp. 176-178
Methylprednisolone-hemisuccinate (MPHS), methylprednisolone (MP), 20-a
lpha-hydroxy- (20 alpha HMP) and 20-beta-hydroxymethyl-prednisolone (2
0 beta HMP) concentrations were measured in serum, urine and bile from
two liver transplant recipients who had received 1 g MPHS by a 1 h in
travenous infusion for treatment of an acute rejection episode. These
patients excreted similar total amounts of the dose in urine as patien
ts with rheumatoid arthritis (historical controls) who had normal live
r function. The transplant patients showed a ratio in urine of 'total
metabolites'/MPHS that was one third that of patients with rheumatoid
arthritis. Less than 0.2% of the administered MPHS appeared in bile as
MPHS, MP, 20 alpha HMP and 20 beta HMP during the 24 h following infu
sion. Liver transplantation did not affect the overall elimination of
drug in urine. However, the impaired liver function following transpla
ntation resulted in reduced conversion of MPHS to its active form (MP)
.