• Journal of Yeungnam Medical Science
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• 제16권2호
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• pp.219-227
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• 1999

만성 폐질환 환자의 하부 기도감염은 건강인의 지역사회감염 폐렴과 달리 원인균이 다양하며, 병원내 감염이나 특히 집중치료를 받고 있는 중환자실 환자의 폐렴은 보통 한 가지 이상의 병원균에 의하여 발생하는 경우가 많아 보다 넓은 항균범위를 가진 항균제의 필요성은 더욱 높아지고 있다. 본 연구에서는 호흡기 질환 중 폐렴으로 입원한 환자 30명을 대상으로 cefpirome의 임상적 유효성 과 안정성을 알아보기 위하여 cefpirome 1gm을 단독으로 하루 2회 환자들에게 투여하여 다음과 같은 결과를 얻었다. 1) 전체 30례 중 21례(70%)는 아주 유효하였고, 7례(23%)는 유효하여, cefpirome의 전체적인 임상적 유효율은 93%이었다. 2) 객담배양검사 결과 원인균이 동정된 14례 중 전예에서 cefpirome에 감수성이 있었으며, 추적 배양결과 11례(78.6%)에서 약제사용 후 균소설을 확인할 수 있었다. 3) 약제사용중 부작용은 transaminase가 경미하게 상승된 경우가 5례(16.7%)가 있었으나 문제없이 정상화되었으며, 프로트롬빈 시간은 2례(6.7%)에서 연장되었으나 임상적으로 투약을 중단할 정도의 중요한 부작용은 없었다. 이상의 결과로 cefpirome은 폐렴, 특히 만성 폐질환이 있는 환자에서 단일요법으로 선택하여 유용하고 안전하게 사용할 수 있는 약제로 생각된다.

• 약학회지
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• 제40권1호
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1993년도 제2회 신약개발 연구발표회 초록집
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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.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1992년도 제1회 신약개발 연구발표회 초록집
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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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• 제19권1호
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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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• 대한임상약리학회 1999년도 제8차 추계학술대회 및 정기총회
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• pp.62-62
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• 1999

• Archives of Pharmacal Research
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• 제14권3호
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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.

• 약학회지
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• 제44권4호
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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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• 제1권2호
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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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• 제24권2호
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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.