CHEMOTHERAPY
Online ISSN : 1884-5894
Print ISSN : 0009-3165
ISSN-L : 0009-3165
眼科領域におけるPipemidic acidの基礎的, 臨床的検討
大石 正夫西塚 憲次本山 まり子小川 武
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1975 年 23 巻 9 号 p. 2969-2973

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Results of basic and clinical studies for ophthalmic use of pipemidic acid (PPA) are summarized as follows.
1) PPA has an antibacterial activity against gram-negative bacteria including Pseudomonas aeruginosa.
2) The sensitivity of 20 strains of Pseudomonas aeruginosa was distributed in the MIC range of 12. 5->100μg/ml, and 12 strains of them (60%) were inhibited by 25μg/ml or lower.
3) The blood concentrations of PPA in healthy adults by single oral administration of 1.0 g and 2.0 g reached the highest levels of 4.9μg/ml and 14. 25μg/ml respectively 2 hours after administration, and were high enough to be measured even at 6 hours.
4) When PPA was orally given to rabbits at a single dose of 500 mg, the aqueous humor levels were below 1.25μg/ml throughout 1-6 hours. However the aqueous humor levels were detected to be 3.8μg/ml after 2.5 hours and 4.3μg/ml after 4 hours, and the ocular tissue concentrations were recognized to be relatively high in both of outer and inner parts of the eye when 500 mg PPA was administered twice every 4 hours.
5) The oral administration of PPA at a dose of 1 g, 4 times a day, combined with the local application of 5% PPA ointment, showed satisfactory effects on 4 cases of corneal ulcer and 1 case of acute dacryocystitis caused by Pseudomonas aeruginosa.
6) No side effects were noted in any of the cases.

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