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Lee, Joo H.,Lee, Myung G. WILEY PUBLISHERS 2007 BIOPHARMACEUTICS AND DRUG DISPOSITION Vol.28 No.4
<P>It was reported that the expression of CYP3A1 increased in rats with acute renal failure induced by uranyl nitrate (rat model of U-ARF) compared with controls. It was shown that telithromycin was mainly metabolized via CYP3A1/2 in rats in this study. Hence, the pharmacokinetic parameters of telithromycin were compared after both intravenous and oral administration at a dose of 50 mg/kg to control rats and a rat model of U-ARF. After intravenous administration of telithromycin to rats with U-ARF, the AUC and renal clearance (Cl<SUB>r</SUB>) were significantly greater (35.0% increase) and slower (99.1% decrease), respectively, than the controls. Unexpectedly, the nonrenal clearance (Cl<SUB>nr</SUB>) of telithromycin was comparable between the two groups of rats, suggesting that CYP3A isozyme responsible for the metabolism of telithromycin seemed not to be expressed considerably in the rat model of U-ARF. After oral administration of telithromycin to rats with U-ARF, the AUC was also significantly greater (127% increase) than the controls and the value, 127%, was considerably greater than 35.0% after intravenous administration of telithromycin. This may be due mainly to the decrease in the intestinal first-pass effect of telithromycin compared with controls in addition to significantly slower Cl<SUB>r</SUB> than controls. Copyright © 2007 John Wiley & Sons, Ltd.</P>
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민유홍,최응칠,윤은정,권애란,심미자 대한약학회 2011 Archives of Pharmacal Research Vol.34 No.12
We determined rates of resistance to the ketolide telithromycin in 56 Enterococcus faecalis isolates and 44 Enterococcus faecium isolates collected from hospitals in Korea between 2005 and 2006. Twenty nine (51.8%) isolates of E. faecalis and 35 (79.5%) isolates of E. faecium were resistant to telithromycin (minimum inhibitory concentrations, ≥ 4 μg/mL). All of the telithromycin-resistant E. faecalis carried the erm(B) gene only. Of the telithromycin-resistant E. faecium, 29 resistant strains carried erm(B) only, the other six carried erm(A) and erm(B) together. The nucleotide sequence of the erm(B) regulatory regions from 29 E. faecalis and 29 E. faecium isolates with erm(B) only was analyzed. Five types of alterations were detected. The first and second types had point mutations that destabilize the secondary structure of erm(B) mRNA sequestering the translation initiation region of the structural gene. The third type was identical to erm(Bv1), a previously reported variant of erm(B) with different induction specificity. The fourth and fifth types had point mutations within the critical sequence for induction and a point mutation destabilizing the stem-loop of erm(B) mRNA sequestering the translation initiation region of the structural gene.
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권애란,Eun-Jeong Yoon,Jong-Min Yoon,Hyunjee Kim,심미자,최응칠 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.7
The antibacterial activities of clindamycin, synercid, telithromycin, linezolid and mupirocin were evaluated against erythromycin-resistant Gram-positive coccal clinical isolates collected in Korean hospitals. In Staphylococcus aureus, synercid, linezolid and mupirocin were the most active agents. Against coagulase-negative staphylococci (CNS), synercid, linezolid and mupirocin were also active. Telithromycin and synercid resistance was common against enterococci, only linezolid and mupirocin were active. The reason of low activity of telithromycin against staphylococci and enterococci is because most of the isolates were constitutively resistant to erythromycin. Synercid, telithromycin, linezolid and mupirocin were active against streptococci.
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Kwon, Ae-Ran,Yoon, Eun-Jeong,Yoon, Jong-Min,Kim, Hyun-Jee,Shim, Mi-Ja,Choi, Eung-Chil 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.7
The antibacterial activities of clindamycin, synercid, telithromycin, linezolid and mupirocin were evaluated against erythromycin-resistant Gram-positive coccal clinical isolates collected in Korean hospitals. In Staphylococcus aureus, synercid, linezolid and mupirocin were the most active agents. Against coagulase-negative staphylococci (CNS), synercid, linezolid and mupirocin were also active. Telithromycin and synercid resistance was common against enterococci, only linezolid and mupirocin were active. The reason of low activity of telithromycin against staphylococci and enterococci is because most of the isolates were constitutively resistant to erythromycin. Synercid, telithromycin, linezolid and mupirocin were active against streptococci.
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