Bd. Kuppermann et al., INTRAVITREAL GANCICLOVIR CONCENTRATION AFTER INTRAVENOUS ADMINISTRATION IN AIDS PATIENTS WITH CYTOMEGALOVIRUS RETINITIS - IMPLICATIONS FOR THERAPY, The Journal of infectious diseases, 168(6), 1993, pp. 1506-1509
To determine whether therapeutic intravitreal concentrations of gancic
lovir are achieved after intravenous administration, vitreous samples
were obtained intraoperatively from 23 eyes of 22 AIDS patients with r
etinal detachments associated with cytomegalovirus (CMV) retinitis. Th
e mean intravitreal ganciclovir concentration of all samples was 0.93
+/- 0.39 mug/mL (3.6 +/- 1.5 muM). This level is near the published tr
ough serum concentrations obtained with every-12-h intravenous dosing
and well below the peak. It is significantly below the concentration o
f ganciclovir required to achieve 50% of viral plaque formation for ma
ny human CMV strains. Only a small decrease in vitreous drug levels wa
s observed as a function of time after last dose. Intravenous administ
ration of ganciclovir results in near-steady-state subtherapeutic intr
avitreal ganciclovir concentrations for many CMV isolates. This may ex
plain the difficulty of long-term complete suppression of CMV retiniti
s.