• Archives of Pharmacal Research
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• v.17 no.1
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• pp.21-25
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• 1994

Physico-chemical characterization of human renal dipeptidase was carried out. It was a glycoprotein with a subunit MW of approximately 47,700 dalton. The pH optimum was at 8 and its stable conformation was retained between pH 5 and 12. The kinetic parameters determined with imipenem, a noval ${\beta}-lactam$ antibiotic, were Vmax, $5.21\;\mu{mol/min/mg}$; km, 4.35 mM ; and Ki with cilastatin, $0.25\;\mu{M}$ Cilastatin demonstrated reversible competitive inhibition.

• Clinical and Experimental Pediatrics
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• v.45 no.7
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• pp.836-846
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• 2002

Purpose : With the development of neonatal intensive care and the increased use of systemic antibiotics, candida sepsis has become one of the most important causes of neonatal morbidity and mortality. The purpose of this study was to investigate the prevalence rate and its associated risk factors. Methods : We retrospectively reviewed medical records of 28 cases with candida sepsis who were admitted in the neonatal intensive care unit(NICU) of Chonnam University Hospital from July 1995 to June 2001. Twenty-nine patients without candida sepsis were enrolled for the control group to verify the risk factors. Results : The overall incidence of candida sepsis was 0.61% for all NICU admissions and 3.68% for all very low birth weight infants with the gradual increase of the annual prevalance rate over time. The endotracheal intubation, percutaneous central vein catheter(PCVC), umbilical vein catheter, total parenteral nutrition, intralipid and dopamine were more applied than the control group (P<0.01 for all). The durations of mechanical ventilator care, central catheter appliance, nothing per os, and admission were also significantly longer than the control group(P<0.01 for all). Ampicillin/ sulbactam, ceftazidime, amikacin, netilmicin, teicoplanin and imipenem/cilastatin were significantly more used than the control group(P<0.05). The durations of ampicillin/sulbactam, ceftazidime, netilmicin and imipenem/cilastatin administration were also proved to be significant as the risk factors(P<0.01). Conclusion : The average annual prevalence rate of candida sepsis in NICU for six years was 0.61% with gradual increasing tendency over time. The elimination of the above risk factors is important in decreasing neonatal morbidity and mortality associated with candida sepsis.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.34-35
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• 1993

The Development of new asymmetric induction methods useful for syntheses of biologically active natural products and drugs, using C4-chiral 1,3-th-iazolidine-2-thiones, has been a recent focus of interest. 1-8) The present account describes the significance of particular heterocycles in the synthetic development of new 1${\beta}$-substituted carbapenems. A fungal metabolite, (＋)-thienamycin (1) has attracted one's attention as a hopeful candidate for new-generation antibiotic drugs because of its strong antimicrobial activities and wide antimicrobial spectra due to the extensive inhibition against various ${\beta}$-lactamases. However, it has been serious problems toward a practically useful drug that (＋)-thienamycin is fairly labile in the solution and can be metabolized by renal dehydropept- idase-I (DHP-I). Recently, a Merck Sharp ＆ Dohme research group exploited a non-natural ${\beta}$-lactam, imipenem (2) which has been appeared in the drug market as the first carbapenem-type antibiotic drug. 9) However 2 must be used with a DHP-I inhibitor, cilastatin sodium (3).9) Thus, a 1,${\beta}$-methyl- carbapenem derivative 4 has been disclosed by the same group. 10) It seems to be more hopeful candidate as a new-generation antibiotic because it can directly resist against metabolism by the renal DHP-1 without an enzyme inhibitor 3. 10)

• Tuberculosis and Respiratory Diseases
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• v.67 no.3
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• pp.239-243
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• 2009

Delftia acidovorans is a gram-negative motile rod found ubiquitously in soil and in water. Confirmed isolation from clinical infections is rare, and has been documented mostly in immunocompromised patients or those with indwelling catheters. A 53-year-old man was referred for the evaluation of a huge mass-like lesion found incidentally by chest X-ray. The lesion occupied more than half of the right lung and was diagnosed as a large loculated pleural effusion by CT scan. Bloody pus was drained through a percutaneous catheter, and D. acidovorans, identified by the Vitek GN card and confirmed by amplification of 16S ribosomal RNA and sequencing analysis, was isolated repeatedly from the drained pus. The patient was treated with imipenem/cilastatin to which the organism was sensitive. This is a rare report of chronic empyema associated with D. acidovorans in the respiratory system of an immunocompetent patient.

• Clinical and Experimental Pediatrics
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• v.48 no.10
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• pp.1107-1115
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• 2005

Purpose : An outbreak of ESBL-producing Shigella sonnei enteritis was unprecedented not only in Korea but throughout the world in the past. We intended to devise a management guideline for ESBL-producing shigellosis based on analysis of clinical manifestations and response to therapy. Methods : We analyzed 103 patients who were admitted to the hospital with acute GI symptoms and were shown positive result for S. sonnei on stool culture. We performed sensitivity test to the antibiotics and DNA sequencing of ESBL gene in the isolated S. sonnei colonies. In addition, we retrospectively analyzed their clinical characteristics, laboratory results, and clinical and microbiological responses to the antibiotics. Results : Among the clinical manifestations, fever was the most frequent(96.1%), followed by diarrhea(93.2%), abdominal pain(76.7%), headache(71.8%), vomiting(65.0%), and nausea(41.7%). The fever was sustained for average of 2.0 days and diarrhea for 3.9 days. Watery diarrhea was the most common(69%) followed by mucoid(26%), and bloody stool(5%). On peripheral blood smear, leukocytosis was noted in 53.4% of patients, and 78.6% of patients tested positive for serum CRP response. On stool direct smear, 11.7% of patients showed more than 50 WBCs/HPF, and 9.7% of patients between 5 to 20 WBCs/HPF. Stool occult blood was positive in 71% of patients. Production of CTX-M-14 type ESBL was reported for all S. sonnei strains isolated from this outbreak. Microbiological eradication rates to various antibiotics were as follows : 100%(9/9) to ciprofloxacin, 100% 5/5) to azithromycin, 6.9%(5/72) to cefdinir, 0%(0/8) to ceftriaxone, 12.5%(1/8) to ceftizoxime, 0%(0/ 8) to TMP/SMX, 42.9%(3/7) to ampicillin/sulbactam, 20%(1/5) to amoxicillin/clavulanic acid, and 68.8 %(11/16) to imipenem/cilastatin. Conclusion : It is presumed that azithromycin can be an attractive option for the treatment of ESBL-producing S. sonnei enteritis in pediatric population, given its cost-effectiveness and safety. Although ciprofloxacin is another cost-effective agent, its use in pediatric population may be a bit too premature.

• YAKHAK HOEJI
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• v.39 no.4
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• pp.360-366
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• 1995

1-$\beta$-Methyl carbapenem-2-substituted pyrroudine derivatives. CRB 529 and CRB 550, were synthesized as investigational carbapenem derivatives. It has been reported that the in vitro antibacterial activities of the compounds against G(+) and G(-) bacteria were almost the same or more effective than those of imipenem (IPM) and meropenem (MEPM), and also showed better in vivo efficacy than MEPM and inlipeneni/cilastatin (IPM/CS) against representative G(-) organisms, P. aeruginosa and MRSA organisms, S. aureus. The antibacterial activities, pharmacokinetics and protective efficacy of IPM/CS and CRB 529 and CRB 550 wereconducted after subcutaneous or intravenous administration to mice and rats. The pharmacokinetic parameters of CRB 529 and CRB 550 in mice were as follows: the observed maximal serum concentrations (C$_{max}$) following I.V. administration were 87.5 and 101 $\mu\textrm{g}$/ml for CRB 529 and CRB 550, respectively, and 63.6 $\mu\textrm{g}$/ml for IPM/CS. The half-lives (t$_{1/2}$) were 14.0 and 12.0 n-dn for CRB 529 and CRB 550, respectively, and 14.8 min for IPM/CS. In rats, $C_{max}$ after I.V. administration were 74.0 and 91.8 $\mu\textrm{g}$/ml for CRB 529 and CRB 550, respectively, and 41.2 $\mu\textrm{g}$/ml for IPM/CS. The tissue levels of CRB 529 and CRB 550 and IPM/CS after I.V. administration at a dose of 20 mg/kg decreased by the following order: lung, heart, kindney, liver and spleen for CRB 529, lddney, liver. lung, heart and spleen for CRB 550 and kidney, lung, liver, heart, spleen and brain for IPM/CS. In systemic infection, CRB 529 and CRB 550 showed excellent efficacies against P. aeruginosa and S. aureus (MRSA) at a dose of 5 mg/kg. The PD$_{50s}$ were 0.80, 0.36 mg/kg for CRB 529 and CRB 550, respectively, and 3.22 mg/kg for IPM/CS against P. aeruginosa. The corresponding values against S. aureus (MRSA) were 76.0, 55.3 mg/kg for CRB 529 and CRB 550, respectively, and 146 mg/kg for IPM/CS. In local infection, the antibacterial activities of CRB 529 and CRB 550 were more effective than those of IPM/CS against intrarenal infection with E. coli and P. aeruginosa and also showed as effective as IPM/CS against respiratory tract infection with E. coli and P. aeruginosa at a dose of 5 mg/kg.