LABORATORY AND CLINICAL STUDIES OF CEFADROXIL IN OPHTHALMOLOGIC FIELD

Cefadroxil, a new cephalosporin antibiotic, has an antibacterial activity similar to that of cephalexin (CEX). Sensitivity of 15 strains of Staph. aureus isolated clinically was distributed between 1.56-6.25μg/ml, and the peak of 3.13μg/ml was noticed in 8 strains (53.3%). Three healthy volunteers w...

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Published inCHEMOTHERAPY Vol. 28; no. Supplement2; pp. 499 - 505
Main Authors OISHI, MASAO, NISHIZUKA, KENJI, MOTOYAMA, MARIKO, OGAWA, TAKESHI, NAGAI, SHIGEO
Format Journal Article
LanguageJapanese
Published Japanese Society of Chemotherapy 1980
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Abstract Cefadroxil, a new cephalosporin antibiotic, has an antibacterial activity similar to that of cephalexin (CEX). Sensitivity of 15 strains of Staph. aureus isolated clinically was distributed between 1.56-6.25μg/ml, and the peak of 3.13μg/ml was noticed in 8 strains (53.3%). Three healthy volunteers were administered orally 500mg of the agent at fasting early in the morning, and the average peak value of 12.93μg/ml was obtained after 2 hours, then decreasing gradually, the average level was 2.16μg/ml after 6 hours. Intraocular penetration was determined in white mature rabbit. A dose of 50mg/kg was administered orally, and the peak value in aqueous humor was 1.73μg/ml after 2 hours, aqueous humor/serum ratio being 20.11%. The ocular tissue levels were transferred well too in outer and inner parts of the eyes after 2 hours. A dose of 250mg or 500mg of the agent was administered clinically per os 3 times per day in 20 cases of various bacterial infections of eye, and the result obtained was excellent in 3 cases, good in 11 cases, fair in 4 cases, poor in 1 case, and unknown in 1 case. As to the side effect of the agent, 1 case complained of diarrheic symptoms, and the administration was interrupted. No other effects as allergic reaction were observed.
AbstractList Cefadroxil, a new cephalosporin antibiotic, has an antibacterial activity similar to that of cephalexin (CEX). Sensitivity of 15 strains of Staph. aureus isolated clinically was distributed between 1.56-6.25μg/ml, and the peak of 3.13μg/ml was noticed in 8 strains (53.3%). Three healthy volunteers were administered orally 500mg of the agent at fasting early in the morning, and the average peak value of 12.93μg/ml was obtained after 2 hours, then decreasing gradually, the average level was 2.16μg/ml after 6 hours. Intraocular penetration was determined in white mature rabbit. A dose of 50mg/kg was administered orally, and the peak value in aqueous humor was 1.73μg/ml after 2 hours, aqueous humor/serum ratio being 20.11%. The ocular tissue levels were transferred well too in outer and inner parts of the eyes after 2 hours. A dose of 250mg or 500mg of the agent was administered clinically per os 3 times per day in 20 cases of various bacterial infections of eye, and the result obtained was excellent in 3 cases, good in 11 cases, fair in 4 cases, poor in 1 case, and unknown in 1 case. As to the side effect of the agent, 1 case complained of diarrheic symptoms, and the administration was interrupted. No other effects as allergic reaction were observed.
Author OISHI, MASAO
NAGAI, SHIGEO
NISHIZUKA, KENJI
OGAWA, TAKESHI
MOTOYAMA, MARIKO
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  fullname: NAGAI, SHIGEO
  organization: Department of Ophthalmology, Niigata University School of Medicine
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References 3) 三国政吉, 大石正夫, 林日出人, 周田茂雄, 今井正雄: 合成Cephalosporin Cについて, 眼科領域における応用. J.Antibiotics, Ser. B18: 298-301. 1965
2) 三国政吉, 大石正夫, 周田茂雄, 今井正雄, 高橋重子: Cephalexinの眼科的応用. Chemotherapy 18: 985-990, 1970
5) 大石正夫, 西塚憲次, 本山まり子, 小川武: Cephradineの眼科的応用のための基礎的ならびに臨床的検討. Chemotherapy23; 480-487, 1975
4) PFEFFER, M.; A. JACKSON, J. XIMENES & J. P. DE MENEZES: Comparative human oral clinical pharmacology of cefadroxil, cephalexin and cephradine. Antimicr. Agents & Chemoth. 11: 331-338. 1977
1) BUCK, R. E. & K. E. PRICE: Cefadroxil, a new broad-spectrum cephalosporin. Antimicr. Agents & Chemoth. 11: 324-330, 1977
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