• Journal of Yeungnam Medical Science
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• v.16 no.2
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• pp.219-227
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• 1999

Background: In contrast to a healthy person, patients who have acute lower respiratory tract infection with underlying pulmonary diseases have various pathogens, a rapidly progressive downhill course, and a poor response to prior antimicrobial therapy. Broad spectrum antibacterial therapy is needed for full evaluation. Materials and Methods: To evaluate the efficacy and safety of cefpirome, we administered 1gm cefpirome, twice a day to 30 patients, who had signs and symptoms of acute lower respiratory infection regardless of their underlying disease, except to those who had an allergic history to antibiotics or severe systemic diseases. Results: The results were as follows: 1) Among 30 cases, 21 cases(70.0%) showed excellent improvement, and 7 cases(23.3%) showed good improvement in their symptoms and signs of acute lower respiratory infection. 2) In 14 cases with isolated pathogens, we observed bacteriologic eradication in 11 cases(78. 6%). 3) Significant side effects were not found. Conclusion: Above results suggest that cefpirome was effective as a monotherapy in patients with acute lower respiratory infection, especially on those with an underlying chronic obstructive pulmonary disease(COPD).

• YAKHAK HOEJI
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• v.40 no.1
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• pp.95-101
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• 1996

The in vitro antibacterial activities of LB10522, a new catechol-substituted cephalosporin, were compared with those of cefpirome, ceftazidime, ceftriaxone, and cefoperaz one against clinical isolates and laboratory standard anaerobes. LB10522 had broad spectrum antibacterial activities against both gram-positive and gram-negative microorganisms. It was most active against gram-positve bacteria among the reference cephalosporins tested. Against gram-negative strains such as the family Enterobacteriaceae, LB10522 showed an activity comparable to that of cefpirome. But LB10522 was more potent than ceftazidime, ceftriaxone and cefoperazone. In particular, Pseudomonas aeruginosa was highly susceptible to LB10522, which was 32-fold and 64-fold more active than ceftazidime and cefpirome, respectively. Against anaerobic strains, the activity of LB10522 was similar to those of reference compounds. LB10522 exhibited potent therapeutic activities against experimental local infections in mice. The therapeutic effect of LB10522 against urinary tract infection (UTI) caused by P. aeruginosa 1912E in mice was superior to that of cefpirome. Against experimental respiratory tract infection (RTI) caused by K. pneumoniae DT-S in mice, LB10522 was as effective as cefpirome. The in vivo efficacy of LB10522 was correlated well with its in vitro activity.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.106-106
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• 1993

DWC-751은 그람양성 및 음성균주에 대하여 광범위한 항균스펙트럼을 가지는 것으로 나타났다. 그람양성균 S. aureus에 대하여는 cefpirome과 동등하며, cefotaxime 보다 4배, ceftazidime보다 16배 우수하였고 그람음성균에 대하여 DWC-751의 항균력은 cefpirome, cefotaxime보다 2배, ceftazidime보다 4-8배 우수하였다. Ps. aeruginosa에 대한 DWC-751의 항균력은 ceftazidime과 거의 동등한 항균력을 나타내었고, cefpirome보다 2배, cefotaxime보다 4-8배 우수한 항균력을 나타내었다. 임상분리균주 및 ofloxacin 내성균주에 대한 DWC-751의 항균력은 표준균주에 대한 결과와 같이 대조약물보다 우수하였다. 전신감염치료효과에 있어서 Streptococcus pyogenes, Serratia marcescens, Acinetobacter calcoaceticus, Morganella morganii, Proteus mirabilis에 대한 동물실험 결과, ED$_{50}$치에 의한 효능은 cefotaxime 보다 우수하였으며,Enterobacter cloacae, Pseudomonas aeruginosa에 대하여는 ceftazidime과 거의 동등하였다.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1992.05a
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• pp.15-15
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• 1992

4세대 cephalosporin계 약물로 개발되고 있는 cefpirome, cefepime, SCE-2787과 같은 화합물은 항균 spectrum 및 항균력에서 3세대 약물인 cefotaxime, ceftazidime보다 우수하며 구조적으로 C-3 quarternized기률 함유한 특징을 가지고 있다. 본 연구소에서는 기존에 보고된 화합물보다 개선된 약물을 찾으려는 시도로서 benzimidazole, imidazolopyridine등 기타 유사구조를 가진 C-3 quarternized 화합물 합성을 하여 왔으며, 본 연구에서는 최근에 합성된 9종의 신규 화합물에 대한 합성 및 항균활성을 보고한다. 이중 9 종의 화합물은 시험한 균주에서 일반적으로 cefpirome 보다 우수한 항균 profile을 나타내었으나 실제 신약으로의 개발 가능성 평가를 위하여 자세한 연구가 필요한 것이었다 이 화합물에 대한 확립된 실험실적 합성 공정과 물성자료를 함께 보고한다.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.46-51
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• 1996

The in vitro activity of LB 10517, a new catechol-substituted cephalosporin, was compared with those of E-1077, cefpirome and ceftazidime 1034 clinical isolates collected in Japan. LB10517 showed a broad-spectrum antibacterial activity against a wide range of grampositive and gram-negative bacteria including non-glucose fermenting rods, Pseudomonas aeruginosa. Against the methicillin-susceptible strains of Staphylococcus aureus (MSSA) and Strptoccus pyogenes, the $MIC_{90}$ values of LB10517 which required to inhibit 90% of the strains wre $3.13\mug/ml\; and\; 0.1\mug/ml$, respectively. It was as active as E-1077 but more active than cefpirome and ceftazidime. Methicillin-resistant strains of S.aureus (MRSA) and Enterococcus spp. were highly resistant to all the test compunds. LB10517 was highly active against most members of the family Enterobacteriaceae, 90% of which were inhibited at a concentration of less than $0.78\mug/ml$, except for Enterobacter cloacae ($1.56\mug/ml$) and Serratia marcescens ($3.13\mug/ml$)Its activity was comparable to those of E-1077 and cefpirome but it was greater than that of ceftazidime. Against Pseudomonas aeruginosa, LB10517 showed the most potent antibacterial activity among the compounds tested. Ninety percent of P. aeruginosa isolates were susceptible at the concentration of $0.39\mug/ml$. Its activity was 32-to 128 fold higher than those of E-1077, cefpirome and ceftazidime. Against imipenem- or ofloxacin-resistant P. aeruginosa, LB10517 with $MIC_{90}\; of\; 6.25 \\mug/ml\; and\; 3.13\mug/ml$, respectively, showed 16-fold more potent activity than the other test compounds. LB10517 showed a relatively high plasma level and long plasma elimination half-life in rats $(t_{1/2}(\beta,\; 52 min)\; and\; dogs\; (t_{1/2}(\beta),\; 103 min)$.

• 대한임상약리학회:학술대회논문집
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• 1999.12a
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• pp.62-62
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• 1999

• Archives of Pharmacal Research
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• v.14 no.3
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• pp.279-281
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• 1991

In the field of cephalosporins, introduction of quaternary heterocyclic methyl goups at the C-3 position has led to a new class of cephalosporins such as cefepime and cefpirome, the so-called 4th generation cephalosporins which are characterized by their potent activity. Since than many efforts were attempted to synthesize more effective analogs.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.315-317
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• 2000

The in vitro activities of DA-074, a new cephalosporin against 34 various standard strains and its in vivo efficacies against 6 important strains were obtained. DA-074 showed two fold enhanced in vitro antibacterial activity against some Pseudomonas aeruginosa compared to Ceftazidime and more than 2 fold in vivo efficacy against Staphylococcus aureus Smith, Klebsiella pneumoniae 1 and Escherichia coli KC-14, compared to Cefpirome. DA-074 might be a good candidate for further evaluations.

• Biomolecules & Therapeutics
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• v.1 no.2
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• pp.196-203
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• 1993

We compared in vitro antibacterial activity of DWC-751, a new parenteral cephalosporin antibiotic, with those of cefpirome (CPR), cefotaxime (CTX) and ceftazidime (CAZ). DWC-751 showed a broad antimicrobial spectrum against Gram-positive and negative bacteria. The antibacterial activity of DWC-751 against Stapylococcus aureus was equal to that of CPR and superior to those of CTX and CAZ. The activity of it against Excherichia coli was more potent than those of CPR, CTX and CAZ. Against Pseudomonas aeruginosa, DWC-751 was slightly inferior to that of CAZ and superior to those of CPR and CTX. The antibacterial activity of DWC-751 was superior to those of CPR, CTX and CAZ against clinical isolates and ofloxacin resistant strains. DWC-751 showed bactericidal action against Escherichia coli at concentrations close to the MIC and induced the formation of filament and burge and lysis of Escherichia coli in a microscopic examination.

• Archives of Pharmacal Research
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• v.24 no.2
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• pp.89-94
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• 2001

Several quaternary pyridinium cephalosporin analogues were prepared analogues were Prepared and evaluated in vitro for antibacterial activity against selected Gram-positive and Cram-negative organisms. Most of the synthesized analogues were either as effective or less effective against the tested bacterial organ isms than the reference com pounds, Cefpirome and Ceftazidime.