Disease relevance of THR-221

• Ceftazidime, ceftizoxime, cefotaxime and HR 221 in experimental chronic Escherichia coli pyelonephritis in rats [1].
• The pharmacokinetics of cefodizime (HR 221) were studied in 6 healthy male individuals and 12 male patients with various degrees of chronic renal failure following intravenous bolus injection of 1 g of the drug [2].
• HR 221 was highly active against Gram-negative bacteria [3].
• HR 221 exerted potent bactericidal activity against Streptococcus pneumoniae Sp-1 inoculated into the mouse lung; the duration of action was prolonged [4].
• The protective effects of HR 221 on experimental infections in mice caused by Staphylococcus aureus Smith, Escherichia coli C-11, Proteus vulgaris GN-76 and Serratia marcescens No. 2 were directly related to its in vitro activity against these strains [4].

High impact information on THR-221

• Clinical, microbiological and pharmacokinetic studies were carried out after 1 or 2 g intramuscular injections bd of cefodizime (HR 221), a new aminothiazolyl cephalosporin, in 41 patients hospitalized for acute purulent exacerbations of chronic respiratory disease [5].
• Clinical, microbiological and pharmacokinetic studies were carried out after 1 or 2 g intramuscular injections bd of cefodizime (HR 221), a new aminothiazolyl cephalosporin, in 41 patients hospitalized for acute purulent exacerbations of chronic respirators disease [5].
• Cefodizime (HR 221) potentiation of human neutrophil oxygen-independent bactericidal activity [6].
• Ceftazidime was significantly more active than HR 221 in both experimental models, although the serum levels of HR 221 were higher and were maintained for a longer period of time than those of ceftazidime [1].
• The concentrations of cefodizime (HR 221, CAS 69739-16-8) in bronchial secretions were measured after administration of a single intravenous bolus of 2 g in 19 patients requiring fibreoptic bronchoscopy for diagnostic purposes or as therapeutic follow-up [7].

Chemical compound and disease context of THR-221

• When tested against the E. coli Ec-89 infection induced in the rat uterus, the activity of HR 221 given to rats once daily was equal to that of CTX or CMZ given at the same dose twice daily [4].

Biological context of THR-221

• THR-221 caused no increases in the number of chromosomal aberrants at dose levels of 0.75, 1.5, 3.0 and 6.0 mg/ml in the absence and presence of the metabolic activation [8].

References