title: Transfer of beta-lactam preparations created in Japan to lung tissue and the drug selection for chemotherapy of respiratory tract infections.
abstract: Intraoperative transfer of eight beta-lactam preparations to lung tissues was investigated by one-gram one-hour intravenous drip infusion immediately prior to operation. The Japanese drugs used were piperacillin, cefotiam, ceftizoxime, cefuzonam, latamoxef, flomoxef, cefotetan and cefbuperazone. The serum peak level was highest with cefotetan, 104.1 micrograms/ml, followed by cefbuperazone, latamoxef, ceftizoxime, cefotiam, piperacillin, flomoxef and cefuzonam, in decreasing order. Except for cefuzonam, there was a correlation between the serum peak level and the human serum protein binding rate (r = 0.89). There was a correlation (r = 0.98) between the Cmax of normal lung tissue (alveoli) level and the serum peak level (Cmax), but no correlation between the former and the human serum protein binding rate. The tumour level was lower than that in normal lung tissue (alveoli), but the tissue level at the obstructive pneumonia area was higher. The Cmax of bronchiolar tissue level was highest with cefuzonam, followed by latamoxef. There was no correlation between the Cmax of bronchiolar tissue level and the serum peak level, human serum protein binding rate or the Cmax of lung tissue (alveoli) level. It is therefore presumed that the drug level in tissue of the acute pneumonia area can be determined from the serum peak level of the respective drug. An appropriate drug for chemotherapy may be selected from beta-lactam preparations which are effective against main causative organisms in acute respiratory tract infections. Cefuzonam and latamoxef are especially useful for chemotherapy in patients with acute bronchiolitis.
authors.affiliation: Department of Thoracic Surgery, Nagoya University School of Medicine, Japan.
authors.forename: M
authors.initials: M
authors.lastname: Imaizumi
authors.forename: T
authors.initials: T
authors.lastname: Ojika
authors.forename: M
authors.initials: M
authors.lastname: Sakakibara
authors.forename: D
authors.initials: D
authors.lastname: Kondo
authors.forename: H
authors.initials: H
authors.lastname: Watanabe
authors.forename: M
authors.initials: M
authors.lastname: Nishimura
authors.forename: T
authors.initials: T
authors.lastname: Abe
mesh_terms: D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000900:Anti-Bacterial Agents / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001798:Blood Proteins / Q000378:metabolism; D001980:Bronchi / Q000378:metabolism; D005260:Female; D006207:Half-Life; D006801:Humans; D007262:Infusions, Intravenous; D007564:Japan; D008168:Lung / Q000187:drug effects / Q000378:metabolism*; D008175:Lung Neoplasms / Q000150:complications; D008297:Male; D008875:Middle Aged; D011485:Protein Binding; D012141:Respiratory Tract Infections / Q000150:complications / Q000188:drug therapy* / Q000382:microbiology; D047090:beta-Lactams
chemical_list: D000900:Anti-Bacterial Agents; D001798:Blood Proteins; D047090:beta-Lactams