Systemic availability of itraconazole in lung transplantation was eval
uated by serially measuring the bioactivity of itraconazole in lung tr
ansplant patients who received itraconazole for prophylaxis (n = 12) o
r therapy (n = 5). These patients also received concomitant antacid an
d H-2 blocker therapy. In patients receiving itraconazole at 200 and 4
00 mg/day, the median concentrations in serum were 0.5 mu g/ml (range,
<0.5 to 2.7) and 3.5 mu g/ml (<0.5 to 14), respectively. The concentr
ation following administration of 400 mg/day was >2.5 mu g/ml in 56% o
f samples, while only 4% of samples from patients who were administere
d 200 mg/day had levels over 2.5 mu g/ml. This study documents that it
raconazole can be absorbed in patients receiving concomitant antacid a
nd H-2 blocker therapy. However, the reduced and variable absorption s
uggests the importance of confirming drug delivery by measurement of c
oncentrations in serum.