Aerosol of Fluticasone Propionate (FP), a new topical adrenocorticosteroid developed for treatment of nasal allergy, was examined for its tolerance and pharmacokinetic profile, in healthy male volunteers, with single dosing (100μg, 200μg, 400μg or placebo; n=6) and multiple dosing (either 400μg or placebo ; n=5; 14 days), and the following results were obtained.
1. The following tests were performed: subjective symptoms, anterior rhinoscopy, physical examinations, adrenal function tests, clinical laboratory tests, biochemical urinalysis, nasal and pharyngeal fungal tests, and nasal mucociliary transport test. No abnormality attributable to this drug was observed except for one case receiving single dose of 100μg, who felt transient intranasal irritancy immediately after dosing. Based on these results, it was confirmed that this drug was well tolerated as far as it was administered for not longer than 14 consecutive days in the dose of 400μg daily.
2, Concentrations of FP (as the unmetabolised drug) present in plasma following the single doses of 200μg and 400μg, and multiple dosing of 400μg/day, were all below the detectable limit (50pg/ml).

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In patients with perennial nasal allergy, clinical efficacy and safety of FP were evaluated and its optimal dosage was also confirmed, through intergroup comparison among 50,100,200 and 400mcg/day, all with 2 weeks' treatment.
1. In the analysis of final overall improvement, there were significant differences among the four groups (H test, p≤0.05). Cases assessed as markedly improved accounted for 5% in the 50mcg/day group, 19% in the 100mcg/day group, 40% in the 200mcg/day group, and 33% in the 400mcg/day group ; the rates being higher in the high dose groups than in the low dose groups. The rates of markedly improved plus moderately improved cases were as high as above 70%, in the three groups except the 50mcg/day group.
2. Although adverse events were observed in 6 cases out of the total 198 cases assessed, the major symptoms were intranasal irritancy feeling and intranasal pain at the time of dosing, none of which were severe.
Based on the above results, clinical efficacy and safety of FP were established and the 200mcg/day (25mcg×2 shots per nostril, twice daily) was judged as the optimal dose.

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To patients with vasomotor rhinitis, Fluticasone Propionate (FP) Aerosol was administered in the dose of 200mcg/day for at least 2 weeks in principle, and for 16 weeks at most, to evaluate its clinical efficacy and safety, and the following results were obtained.
1. The total number of the cases receiving the drug was 72.
2. In the assessment of final overall improvement, cases assessed as “markedly improved” plus “moderately improved” accounted for 73.1%, and cumulative rate with “slightly improved” cases added was 88.5%, both rating high.
3. No adverse event was observed in any case. Although there were abnormal values in clinical laboratory tests in 4 cases, they were all of slight nature.
Based on the above results, FP Aerosol was confirmed to be an effective and safe drug also for treatment of vasomotor rhinitis.

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To patients with perennial nasal allergy, Fluticasone Propionate (FP) Aerosol was administered in the dose of either 200 mcg/day or 400 mcg/day for a long term of at least 4 in principle and at most 24 weeks, to evaluate its clinical efficacy and safety, and the following results were obtained.
1. Total number of cases receiving the drug was 68, consisted of 57 receiving 200 mcg/day, and 11 receiving 400 mcg/day.
2. In the assessment of final overall improvement, cases assessed as “markedly improved” plus “moderately improved” accounted for about 80%, and cumulative rate with “slightly improved” cases added was about 90%, both rating high. Even 1 week after completion of treatment, efficacy was observed to be sustained in about 80% of the cases.
3. Adverse events occurred in 4 cases and abnormality in clinical laboratory test values was observed in 1 case. However, they were all of slight nature, and no such tendency was observed that the incidence rate increased related to the duration of the treatment period.
Based on the above results, FP Aerosol was confirmed to be a drug with superior clinical efficacy, and with safety even when used for a long term treatment.

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In paediatric patients with perennial nasal allergy, clinical efficacy and safety of Fluticasone Propionate Aerosol (FP) were evaluated and its optimal dosage was also confirmed, through intergroup comparison between 100, ug/day (25μg×1 shot/nostril) and 200μg/day (25μg×2 shots/nostril), both b. i. d. 1. Final overall improvement rates were: cases assessed as ‘markedly improved’ accounted for 37.0% of all the cases assessed in the 100μg/day group, and 44.0% in the 200μg/day group, and ‘markedly improved’ plus ‘moderately improved’ cases accounted for 89.1% in the 100μg/day group and 74.0% in the 200μg/day group. No significant difference was observed between the two groups.
2. As to clinical adverse events, transient headache immediately after dosing was noted only in 1 case in the 100μg/day group out of the total 108 cases assessed. Although some changes were observed in several clinical laboratory test items between pre-and post-treatment with FP, but all the values were within the normal range.
Based on the above results, clinical efficacy and safety of FP were established and 100μg/day (25μg×1shot/nostril×twice daily) was judged as the optimal standard dose for children.

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In order to make an objective assessment of clinical efficacy, safety and usefulness of FP in treatment of perennial nasal allergy, a double blind comparative study was carried out at 200 mcg/day in two divided doses, against BP 400 mcg/day in four divided doses. In the analysis of final overall improvement, cases assessed as markedly improved accounted for FP 33.3% and BP 37.5%, rates of markedly plus moderately improved cases were FP 73.1% and BP 83.0%, and total of those assessed as either markedly, moderately or slightly improved exceeded 96% in both groups ; good improvement being demonstrated without significant intergroup difference. In the analysis of overall safety, both treatments showed high safety. In the analysis of clinical usefulness, cases assessed as very useful accounted for FP 34.6% and BP 36.4%, rates of very useful plus useful were FP 80.8% and BP 85.2%, and total of those assessed as either very useful, useful or slightly useful exceeded 97% in both groups; high usefulness being demonstrated without significant intergroup difference. Based on the above results, it was suggested that FP, even dosed twice daily, was sufficiently useful, with high efficacy and safety like BP four times daily.

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FP was examined for its inhibitory effect on Japanese cedar pollinosis, and its clinical safety, by dosing it before start of the season of Japanese cedar pollen scattering in the air. Double blind comparative manner was adopted using placebo (P) as the control. During the pollen scattering season, therapeutic effect of FP was also examined. The inhibitory effect of FP in the early season was significantly better than that of P. In the mid through to the late season when treatment in the P group was switched to FP, inhibitory effect was high in both of the groups, without significant intergroup difference. In the analysis of therapeutic effect, cases assessed as markedly improved accounted for 33% in the mid season and 62% in the late season, markedly improved plus moderately improved cases accounted for 64 and 88% respectively, and adding up of those assessed as slightly improved resulted in 91 and 94%, demonstrating an excellent therapeutic effect of FP. Adverse events occurred in 2 cases in the FP group and in 1 case in the P group in the preseason and early season, and in 3 cases in the mid to late season, and abnormal change in the laboratory test values was observed in 1 case in the late season, none of which being severe. Based on the above results, FP was confirmed to be a useful treatment of Japanese cedar pollinosis, with remarkable suppression of symptoms in the use before start of pollen scattering season, and rapid relief of symptoms when used after development of symptoms.

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Aqueous Nasal Spray of Fluticasone Propionate (FP), a new topical adrenocorticosteroid developed for treatment of nasal allergy, was examined for its tolerance and pharmacokinetic profile, in healthy male volunteers, with single dosing (100μg, 200μg or 400μg; n=6) and multiple dosing (either 400μg or placebo; n=5; 14 days), and the following results were obtained.
1. No abnormality attributable to this drug was observed in any of the following tests: subjective symptoms, anterior rhinoscopy, physical examinations, adrenal function tests, clinical laboratory tests, biochemical urinalysis, nasal and pharyngeal fungal tests, and nasal mucociliary transport test. Based on these results, it was confirmed that this drug was well tolerated as far as it was administered for not longer than 14 consecutive days in the dose of 400μg daily.
2. Concentrations of FP (as the unmetabolised drug) present in plasma following the single doses of 200μg and 400μg, and multiple dosing of 400μg/day, were all below the detectable limit (50pg/ml).

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In patients with perennial nasal allergy, clinical efficacy and safety, and optimal dose level and dosing frequency, of FP were confirmed, through intergroup comparisons among 100,200 and 400mcg/day, each in twice daily administration, and 200mcg/day in once daily, all with 2 weeks' treatment. The three dose levels of twice daily administration were compared in the double blind manner, and comparison between the two dosing frequencies of 200mcg/day was made in the open labelled manner.
1. In the analysis of final overall improvement, comparison among the three dose levels resulted that cases assessed as markedly improved accounted for 32% with 100mcg/day, 44% with 200mcg/day, and 41% with 400mcg/day; the rates were higher with high dose (200mcg and 400mcg) than with low dose (100mcg). in comparison of dosing frequency, improvement rate was significantly higher in twice daily than in once daily administration.
2. Although adverse events occurred in 2 cases among the 215 cases assessed, none of them were severe. Based on the above results, clinical efficacy and safety of FP were established and 200mcg/day (50mcg×1 shot per nostril×twice daily) was judged as the optimal dose level and frequency.

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