TY - JOUR
T1 - In vitro antimicrobial activity of biapenem and its therapeutic efficacy in the treatment of respiratory infections
AU - Honda, Yoshihiro
AU - Saito, Junichi
AU - Nakai, Yushi
AU - Watanabe, Akira
AU - Shoji, Satoshi
AU - Takahashi, Hiroshi
AU - Kikuchi, Hiroaki
AU - Nukiwa, Toshihiro
AU - Motomiya, Masakichi
AU - Sayama, Tsuneo
AU - Konno, Kiyoshi
AU - Masuda, Masahumi
AU - Takeuchi, Kenichi
AU - Honma, Mitsunobu
AU - Nagai, Kousaku
AU - Niizuma, Kazunao
AU - Anzai, Yoshiyuki
PY - 1994/1/1
Y1 - 1994/1/1
N2 - Biapenem (BIPM), a newly developed carbapenem antibiotic agent, was evaluated by in vitro tests and by in vivo trials. The minimum inhibitory concentrations (MICs) of BIPM, imipenem (IPM) and ceftazidime (CAZ) against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillinresistant Staphylococcus aureus (MRSA), Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Pseudomonas aeruginosa and Branhamella (Moraxella) catarrhalis were determined by the microbroth dilution method. BIPM showed the strongest antimicrobial activity against P. aeruginosa, B. catarrhalis and E. cloacae. The MIC values of BIPM against MRSA, MSSA and gram-negative bacteria were equal to those of IPM. Penetration of BIPM into the lung tissue was studied in nine patients who had undergone chest surgery. The lung tissue levels of BIPM after intravenous administration of 0.3g ranged from 0.08 to 3.32μg/g and the lung/plasma concentration ratio ranged from 0.92 to 40.2%(mean 18.0%). BIPM concentration in plasma and sputum was studied in six patients with respiratory infections. The peak plasma concentration which ranged from 11.3 to 25.4μg/ml was observed immediately after infusion. The peak sputum concentration ranged from 0.43 to 2.72μg/ml at 1 to 4 hours after infusion. The sputum/plasma concentration ratio of 1.89∼∼12.48%(mean 6.3%) suggested that BIPM penetrated rapidly into the lung. Adaily dose of 0.3∼12g of BIPM was given intravenously for 15∼15 days to a total of 38 patients: 30 with pneumonia, 4 with pulmonary abscess, 2 with bronchiectasis, 1 with chronic bronchitis, 1 with infection supervening on pulmonary emphysema. Clinical effects were excellent in 12, good in 21, fair in 2 cases. No side effect was observed. From the above results, we conclude that BIPM is one of the most useful carbapenem agents for parenteral use as a first choice in the treatment of respiratory tract infections.
AB - Biapenem (BIPM), a newly developed carbapenem antibiotic agent, was evaluated by in vitro tests and by in vivo trials. The minimum inhibitory concentrations (MICs) of BIPM, imipenem (IPM) and ceftazidime (CAZ) against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillinresistant Staphylococcus aureus (MRSA), Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens, Pseudomonas aeruginosa and Branhamella (Moraxella) catarrhalis were determined by the microbroth dilution method. BIPM showed the strongest antimicrobial activity against P. aeruginosa, B. catarrhalis and E. cloacae. The MIC values of BIPM against MRSA, MSSA and gram-negative bacteria were equal to those of IPM. Penetration of BIPM into the lung tissue was studied in nine patients who had undergone chest surgery. The lung tissue levels of BIPM after intravenous administration of 0.3g ranged from 0.08 to 3.32μg/g and the lung/plasma concentration ratio ranged from 0.92 to 40.2%(mean 18.0%). BIPM concentration in plasma and sputum was studied in six patients with respiratory infections. The peak plasma concentration which ranged from 11.3 to 25.4μg/ml was observed immediately after infusion. The peak sputum concentration ranged from 0.43 to 2.72μg/ml at 1 to 4 hours after infusion. The sputum/plasma concentration ratio of 1.89∼∼12.48%(mean 6.3%) suggested that BIPM penetrated rapidly into the lung. Adaily dose of 0.3∼12g of BIPM was given intravenously for 15∼15 days to a total of 38 patients: 30 with pneumonia, 4 with pulmonary abscess, 2 with bronchiectasis, 1 with chronic bronchitis, 1 with infection supervening on pulmonary emphysema. Clinical effects were excellent in 12, good in 21, fair in 2 cases. No side effect was observed. From the above results, we conclude that BIPM is one of the most useful carbapenem agents for parenteral use as a first choice in the treatment of respiratory tract infections.
KW - Biapenem
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U2 - 10.11250/chemotherapy1953.42.Supplement4_301
DO - 10.11250/chemotherapy1953.42.Supplement4_301
M3 - Article
AN - SCOPUS:0028605805
VL - 42
SP - 301
EP - 313
JO - CHEMOTHERAPY
JF - CHEMOTHERAPY
SN - 0009-3165
ER -