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Automation, Direct-Sample Analysis, and Microcolumn Liquid Chromatography
Published in Steven H. Y. Wong, Iraving Sunshine, Handbook of Analytical Therapeutic Drug Monitoring and Toxicology, 2017
Kearns et al.63 characterized a cephalosporin, cefpirome disposition in lactating females by extracting a small amount of breast milk, serum, or urine (50 μl) with isopropanol, followed by microbore LC analysis. Analysis was performed with a C-18 column, 100 × 2-mm i.d., with MeOH/triethylamine (TEA) (1:9) as the mobile phase. Flow rate was 0.5 ml/min. Retention time was 2.7 min, with a total analysis time of 6 min per sample. Calibration was established for 0.6 to 500 mg/1. The protocol may be readily used for pharmacokinetic studies.
Cefepime, Cefpirome, and Cefepime–Tazobactam
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Andrea Endimiani, Parham Sendi
Like other cephalosporins, cefpirome is a time-dependent antibiotic. Standard dose recommendations of cefpirome, such as other beta-lactams, in ICU patients without renal dysfunction, can result in very low levels of antibiotic at the end of the dosing intervals (Lipman et al., 2001). In fact, CrCl may be more than the assumed normal range in critically ill patients as a result of high GFR. Septic patients often present with hypotension from the inflammatory response associated with infection. Standard initial management involves administration of i.v. fluids and inotropic agents that raise the renal preload, explaining the increased creatinine and drug clearances. Therefore, it is important to be aware that the dosing of cefpirome in ICU patients must take into account not only impaired renal function but also increased renal clearance (Lipman et al., 2003; Roos et al., 2007).
The war against bacteria, from the past to present and beyond
Published in Expert Review of Anti-infective Therapy, 2022
Lucrezia Bottalico, Ioannis Alexandros Charitos, Maria Assunta Potenza, Monica Montagnani, Luigi Santacroce
Bacterial sensitivity and representative drugs – Based on their resistance to the β-lactamases (in this case termed cephalosporinases) and their effectiveness to treat infections by Gram-positive or Gram-negative bacteria, they are divided into five groups or generations: (a) first generation includes cephalosporins such cephalexin, cefadroxil, all sensitive to cephalosporinases, and mostly effective against Gram-positive bacteria; (b) second-generation cephalosporins, such as cefuroxime, which are more resistant to cephalosporinases, may be effective toward Gram-negative bacteria but less active in Gram-positive-dependent infections; (c) third-generation cephalosporins, also resistant to β-lactamases, such as ceftiofur, cefquinom, and cefoperazone, are more effective against Gram-negative bacteria compared to both the first and second generations (d) fourth-generation cephalosporins, such as cefepime and cefpirome, resistant to β-lactamases and used for more severe bacterial infections; (e) ceftaroline is one fifth-generation cephalosporin used to treat infections, including MRSA infections, that are resistant to other antibiotics [91,98].
Clinical pharmacokinetics of drugs in cardiopulmonary associated cachexia without hepatorenal pathology: a systematic review
Published in Drug Metabolism Reviews, 2019
Regarding cefipirome intravenous route, approximately 80% of the dose is unchanged, when it is eliminated in the urine. Elimination appears to be primarily due to glomerular filtration as the total clearance of cefpirome is approximately equal to creatinine clearance (Strenkoski and Nix 1993). It means that the excretion of cefipirome totally depends on the creatinine clearance of the patient (Lipman et al. 2003). Builleta et al. concluded in their study that both renal clearance of cefipirome and creatinine clearance were higher in cystic fibrosis cachetic patients when compared with healthy volunteers, that is, 5.59 l/hr vs 5.51 l/hr and 131 ml/min vs 116 ml/min. Therefore, creatinine clearance could be a major factor in the high renal clearance of cefipirome in cachetic patients (Bulitta et al. 2011).
Synthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Yuanyuan Zhang, Chuan Xie, Yang Liu, Feng Shang, Rushiya Shao, Jing Yu, Chunxia Wu, Xinghui Yao, Dongfang Liu, Zhouyu Wang
Natural products such as Penicillin, Erythromycin, Cephalosporin C and Kanamycin are often used as main compounds in drug discoveries due to their potent bioactivity. Corresponding semi-synthesised derivatives Amoxicillin, Azithromycin, Cefpirome and Amikacin all exhibit higher potency than natural products5–7. Pleuromutilin (Figure 1, 1), a diterpenoid natural product from the basidiomycete species, shows moderate activities against Gram-positive strains and mycoplasmas8,9. Four semi-synthesised marketed drugs based on its structure have already been developed. Tiamulin and valnemulin (Figure 1, 2 and 3) can effectively prevent and control swine dysentery, mycoplasmal diseases such as enzootic pneumonia and chronic respiratory disease in poultry10,11. Retapamulin (Figure 1, 4) is used for the treatment of skin impetigo12,13. Lefamulin (Figure 1, 5) is approved for treatment of community-acquired bacterial pneumonia (CABP)14. These derivatives can inhibit bacterial protein synthesis via specific interaction with 23S rRNA of the 50S bacterial ribosome unit15, which are unaffected by resistance to major antibiotic classes, such as beta-lactam antibiotics, tetracyclines, macrolides, fluoroquinolones, and others. Thus, pleuromutilin is a promising candidate for treating drug-resistant bacteria infections16, and many compounds derived from four marketed drugs using the thioether as the linkage at the C14 side chain were developed in recent years17–20. To increase side chain diversity and improve modification success rate, the bioactive moiety piperazinyl urea, displaying multiple biological activities such as antifungal21, analgesic22, antibacterial23 and antitumour24 effects was introduced. In this study, a series of pleuromutilin derivatives 6a∼z with piperazinyl urea (Scheme 1) were efficiently synthesised. Their activities were evaluated against MRSA and Gram-negative strains, and interactions were examined by molecular docking.