[The clinical study of fluconazole against pulmonary mycosis. Effects of fluconazole on pulmonary cryptococcosis and aspergillosis, and its pharmacokinetics in patients].
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.
Nakashima
M
M
Department of Respiratory Disease, Kyoto City Hospital.
D000328:Adult; D000368:Aged; D000935:Antifungal Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001228:Aspergillosis / Q000097:blood / Q000188:drug therapy*; D003453:Cryptococcosis / Q000097:blood / Q000188:drug therapy*; D004341:Drug Evaluation; D015725:Fluconazole; D006207:Half-Life; D006801:Humans; D008172:Lung Diseases, Fungal / Q000097:blood / Q000188:drug therapy*; D008297:Male; D008875:Middle Aged; D014230:Triazoles / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*
D000935:Antifungal Agents; D014230:Triazoles; D015725:Fluconazole