BASIC AND CLINICAL STUDIES ON CEFDINIR
We studied the antibacterial activity, absorption, excretion and clinical efficacy on cefdinir (CFDN), a new oral cephalosporin, and obtained the following results. 1. Antibacterial activity: the antibacterial activity of CFDN against 25 clinical isolates each of 5 organisms was investigated. CFDN h...
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| Published in | CHEMOTHERAPY Vol. 37; no. Supplement2; pp. 426 - 435 |
|---|---|
| Main Authors | , , , , , , , |
| Format | Journal Article |
| Language | English Japanese |
| Published |
Japanese Society of Chemotherapy
1989
公益社団法人 日本化学療法学会 |
| Subjects | |
| Online Access | Get full text |
| ISSN | 0009-3165 1884-5894 |
| DOI | 10.11250/chemotherapy1953.37.Supplement2_426 |
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| Abstract | We studied the antibacterial activity, absorption, excretion and clinical efficacy on cefdinir (CFDN), a new oral cephalosporin, and obtained the following results. 1. Antibacterial activity: the antibacterial activity of CFDN against 25 clinical isolates each of 5 organisms was investigated. CFDN had a broad- spectrum activity against Gram-positive and-negative organisms, and the MIC90s against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and methicillin-resistant S. aureus were 6.25, 1.56, 1.56, 1.56 and 50μg/ml, respectively. 2. Absorption and excretion: in adult and elderly subjects, the peak plasma concentrations of CFDN were 1.51 and 1.15μg/ml, respectively, 3-4 hours after a single oral administration of 200mg; the plasma half-lives were 1.76 and 1.90h, and the plasma concentrations at 12 h after dosing were 0.11 and 0.08μg/ml. In elderly subjects administered 100mg of CFDN the plasma concentration was 0.85μg/ml 3h. after administration with a plasma half-life of 1.76 h. The plasma concentration at 12 h after dosing was 0.035μg/ml. The 12-h urinary recovery rate was 16-26%. The peak sputum concentrations ranged from 0.057-0.088μg/ml in 2 patients with bronchial asthma after a single dose of 200mg. 3. Clinical evaluation: CFDN was administered orally at 100 and 200mg 2 or 3 times a day to 24 patients with respiratory tract infections. The clinical response was good in 22 cases and fair and poor in 1 each. A side effect, light headedness, was observed in one case, but no abnormal value was noted. |
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| AbstractList | We studied the antibacterial activity, absorption, excretion and clinical efficacy on cefdinir (CFDN), a new oral cephalosporin, and obtained the following results.1. Antibacterial activity: the antibacterial activity of CFDN against 25 clinical isolates each of 5 organisms was investigated. CFDN had a broad- spectrum activity against Gram-positive and-negative organisms, and the MIC90s against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and methicillin-resistant S. aureus were 6.25, 1.56, 1.56, 1.56 and 50μg/ml, respectively.2. Absorption and excretion: in adult and elderly subjects, the peak plasma concentrations of CFDN were 1.51 and 1.15μg/ml, respectively, 3-4 hours after a single oral administration of 200mg; the plasma half-lives were 1.76 and 1.90h, and the plasma concentrations at 12 h after dosing were 0.11 and 0.08μg/ml. In elderly subjects administered 100mg of CFDN the plasma concentration was 0.85μg/ml 3h. after administration with a plasma half-life of 1.76 h. The plasma concentration at 12 h after dosing was 0.035μg/ml. The 12-h urinary recovery rate was 16-26%. The peak sputum concentrations ranged from 0.057-0.088μg/ml in 2 patients with bronchial asthma after a single dose of 200mg.3. Clinical evaluation: CFDN was administered orally at 100 and 200mg 2 or 3 times a day to 24 patients with respiratory tract infections. The clinical response was good in 22 cases and fair and poor in 1 each. A side effect, light headedness, was observed in one case, but no abnormal value was noted.
新経口セファロスポリン剤cefdinirについて抗菌力, 吸収・排泄, 臨床効果を検討したところ, 以下のごとき成績を得た。1) 抗菌力: 臨床分離Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilisおよびmethicillin-resistant S. aureus (MRSA) に対する本剤の抗菌力を測定したところS. aureusは6.25μg/ml, E. coli, K. pneumonne, P. mirabilisは1.56μg/ml, MRSAは50μg/mlのMIC90値であった。2) 吸収・排泄: 成人4例 (健常成人と感染を伴った気管支喘息患者各2例) および高齢者5例に本剤100～200mgを空腹時1回経口使用した時の血漿中濃度, 尿中濃度, 喀痰中濃度を測定した。本剤200mg使用例の最高血漿中濃度 (Cmax) は成人では平均1.51μg/ml, 高齢者では平均1.15μg/mlで, それぞれの平均血漿中半減期 (T1/2) は1.76, 1.90時間であり, 12時間後でも平均0.11, 0, 08μg/mlの値が得られた。一方, 高齢者に1回100mg経口使用例のCmaxは平均0.85μg/mlであり, T1/2は平均1.76時間で12時間後でも平均0.035μg/mlの値が得られた。本剤使用12時間後までの尿中回収率は16～26%であり, 最高喀痰中濃度は0.057～0.088μg/mlであった。3) 臨床成績: 本剤を急性扁桃炎6例, 急性咽頭炎2例, 急性気管支炎10例, 慢性気管支炎3例, 細菌性肺炎3例計24例に1回100～200mg 1日2～3回使用したところ, 急性扁桃炎, 急性咽頭炎, 細菌性肺炎では全例, 急性気管支炎では10例中9例, 慢性気管支炎では3例中2例で有効の結果を得た。副作用は軽度ふらつきが1例に認められたのみで, その他自他覚所見および臨床検査値異常は認められなかった。 We studied the antibacterial activity, absorption, excretion and clinical efficacy on cefdinir (CFDN), a new oral cephalosporin, and obtained the following results. 1. Antibacterial activity: the antibacterial activity of CFDN against 25 clinical isolates each of 5 organisms was investigated. CFDN had a broad- spectrum activity against Gram-positive and-negative organisms, and the MIC90s against Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and methicillin-resistant S. aureus were 6.25, 1.56, 1.56, 1.56 and 50μg/ml, respectively. 2. Absorption and excretion: in adult and elderly subjects, the peak plasma concentrations of CFDN were 1.51 and 1.15μg/ml, respectively, 3-4 hours after a single oral administration of 200mg; the plasma half-lives were 1.76 and 1.90h, and the plasma concentrations at 12 h after dosing were 0.11 and 0.08μg/ml. In elderly subjects administered 100mg of CFDN the plasma concentration was 0.85μg/ml 3h. after administration with a plasma half-life of 1.76 h. The plasma concentration at 12 h after dosing was 0.035μg/ml. The 12-h urinary recovery rate was 16-26%. The peak sputum concentrations ranged from 0.057-0.088μg/ml in 2 patients with bronchial asthma after a single dose of 200mg. 3. Clinical evaluation: CFDN was administered orally at 100 and 200mg 2 or 3 times a day to 24 patients with respiratory tract infections. The clinical response was good in 22 cases and fair and poor in 1 each. A side effect, light headedness, was observed in one case, but no abnormal value was noted. |
| Author | SAKURAI, IWAO HOJO, TOSHIO MORITA, MASAYUKI TAKAHASHI, TAKAYUKI MATSUMOTO, FUMIO TAURA, YUJI IMAI, TAKEO KOKUBU, KATSUYA |
| Author_FL | 松本 文夫 今井 健郎 高橋 孝行 田浦 勇二 国分 勝弥 森田 雅之 北條 敏夫 桜井 磐 |
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| References | 1) MINE Y, KAMIMURA T, WATANABE Y, TAWARA S, MATSUMOTO Y, SHIBAYAMA F, KIKUCHI H, TAKAYA T, KUWAHARA S: In vitro antibacterial activity of FK482, a new orally active cephalosporin. J. Antibiot. 41: 1873-1887, 1988 2) MINE Y, YOKOTA Y, WAKAI Y, KAMIMURA T, TAWARA S, SHIBAYAMA F, KIKUCHI H, KUWAHARA S: In vivo antibacterial activity of FK482, a new orally active cephalosporin. J. Antibiot. 41: 1888-1895, 1988 3) 第36回日本化学療法学会西日本支部総会, 新薬シンポジウム. FK482, 高知, 1988 4) 日本化学療法学会: 最小発育阻止濃度 (MIC) 測定法再改訂について. Chemotherapy 29: 76-79, 1981 |
| References_xml | – reference: 1) MINE Y, KAMIMURA T, WATANABE Y, TAWARA S, MATSUMOTO Y, SHIBAYAMA F, KIKUCHI H, TAKAYA T, KUWAHARA S: In vitro antibacterial activity of FK482, a new orally active cephalosporin. J. Antibiot. 41: 1873-1887, 1988 – reference: 2) MINE Y, YOKOTA Y, WAKAI Y, KAMIMURA T, TAWARA S, SHIBAYAMA F, KIKUCHI H, KUWAHARA S: In vivo antibacterial activity of FK482, a new orally active cephalosporin. J. Antibiot. 41: 1888-1895, 1988 – reference: 4) 日本化学療法学会: 最小発育阻止濃度 (MIC) 測定法再改訂について. Chemotherapy 29: 76-79, 1981 – reference: 3) 第36回日本化学療法学会西日本支部総会, 新薬シンポジウム. FK482, 高知, 1988 |
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| Title | BASIC AND CLINICAL STUDIES ON CEFDINIR |
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