Effects on pulmonary
cryptococcosis and
aspergillosis and the pharmacokinetics of the new antimycotic agent,
fluconazole, were examined. 1. Cases Pulmonary
cryptococcosis: Two cases, 30 and 29 year-old men who were suspected of
pulmonary tuberculosis by routine health examinations.
Pulmonary aspergillosis: A 65 year-old man with
collagen disease and a 62 year-old man with bacilli free cavities of
tuberculosis. 2. Method
Fluconazole was administered at a dose level of 400 mg/day per os for 2 to 4 weeks. One exception was the 65 year-old
aspergillosis patient who was administered with
fluconazole 50 mg/day for 4 weeks, 100 mg/day for 6 weeks then 400 mg/day for 4 weeks. Sera of the cases 1, 2 and 4 were harvested before, and 1/2, 1, 2, 4, 8 and 24 hours after administration of
fluconazole on the 1st and the 7th day, and in every morning until the 9th day before administration and stored in a freezer. Serum
fluconazole concentrations were determined at Pfizer Taito Laboratory. As pharmacodynamic parameters, T1/2, Tmax and Cmax were calculated. 3. Result Effects of
fluconazole on 2 of the 2 cases with
cryptococcosis were excellent. On the other hand, the effects on the
aspergillosis were poor. The average Tmax was 2-4 hours. The average C maxs were 10.3 micrograms/ml on the 1st day and 30.6 micrograms/ml on the 7th day. Serum concentrations reached the plateau on the 5th-7th day, and the average C min (concentration before administration) was 21-23 micrograms/ml. Average T1/2s were 34.4 hours on the 1st day and 37.2 hours on the last (32th) day. 4. Conclusion
Fluconazole may be regarded as the promising remedy for pulmonary
cryptococcosis but not for
pulmonary aspergillosis.