1996 Volume 37 Issue 4 Pages 239-243
Itraconazole (ITCZ), a triazole antifungal agent, was administered to 10 cases with proven or suspected pulmonary aspergillus infection, and its serum levels and tissue penetration were measured. In 9 cases with proven infection, the clinical efficacy was also evaluated.
Serum levels of ITCZ were well correlated with the daily dose, and a peak concentration of over 1, 300ng/ml was obtained in cases of 200-400mg daily 200-400mg for more than 8 days. In some cases the concentrations were lower than expected from the dosages, suggesting the difference in absorption and metabolism among individuals.
ITCZ showed good penetration into the lung tissue at about 2/3 of the serum level, however, level in the pleural effusion was relatively low. The penetration of ITCZ into sputum was also low at less than 10ng/g.
The clinical efficacy was evaluated considering all the other treatments and the efficacy rate was 77.8% (cure; 2, improved; 5, stable; 1 and died; 2). The results did not always reffect the serum levels of the drug. Even with long-term administration, no severe side effects were observed.
ITCZ is thus considered to be effective not only in the treatment of chronic infections and maintenance therapy for various types of pulmonary aspergillosis, but also in the treatment of some invasive-type infections with rapid achievement of high serum levels by relatively high loading dose at the start of the therapy.
