Aw. Hemming et al., A MICROEMULSION OF CYCLOSPORINE WITHOUT INTRAVENOUS CYCLOSPORINE IN LIVER-TRANSPLANTATION, Transplantation, 62(12), 1996, pp. 1798-1802
A microemulsion formulation of cyclosporine (CsA) has improved absorpt
ion compared with the original form, The purpose of this case control
study was to assess the safety and efficacy of the microemulsion witho
ut intravenous CsA for induction immunosuppression in adult liver tran
splantation, Twenty-one consecutive patients receiving induction immun
osuppression with the microemulsion 15 mg/kg/day were compared with 20
patients receiving intravenous CsA and the original oral form, Both g
roups received the same dose of methylprednisilone, Twenty of 21 patie
nts receiving the microemulsion required no intravenous CsA to achieve
target CsA levels, All patients receiving the original form received
initial intravenous CsA. There was no difference in trough CsA levels
between the two groups at 24 and 48 hours, The microemulsion group had
24 hr and 48 hr trough CsA levels of 227+/-15 and 520+/-300 ng/ml by
monoclonal RIA while the intravenous CsA group had 24 and 48 hr trough
levels of 293+/-18 and 405+/-91 ng/ml. CsA levels analyzed by HPLC we
re 20% lower than by RIA. The frequency of adverse events resulting in
reduction of drug dosage was similar for the microemulsion and the or
iginal form: neurotoxicity (23 vs, 40%, P=.30); nephrotoxicity (25 vs,
45%, P=.32), and no patients required dialysis. There was no differen
ce in septic complications, One patient required discontinuation of th
e microemulsion in an attempt to reverse severe neurotoxicity, A total
of 75% of microemulsion patients were rejection free at 3 months whil
e only 35% of CsA patients remained rejection free (P=0.02). These dat
a suggest that the use of the microemulsion without intravenous CsA in
liver transplantation is safe and efficacious, and may result in decr
eased episodes of acute rejection.