Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1987-7-24
pubmed:abstractText
To determine the influence of in vitro activity, pharmacokinetic properties, and therapeutic regimen on the antibacterial effect in vivo, we compared three cephalosporins, cefotiam, cefmenoxime, and ceftriaxone, in a rabbit model of experimental Escherichia coli endocarditis after 4 days of treatment. The MBCs of cefotiam, cefmenoxime, and ceftriaxone for the E. coli strain were 0.5, 0.125, and 0.06 microgram/ml, respectively. Killing curves at 10 times the MBC were similar for the three cephalosporins. In serum, the elimination half-life of ceftriaxone was twice as much as the elimination half-life of cefotiam or cefmenoxime (2.8 +/- 0.45 versus 1.4 +/- 0.25 or 1.3 +/- 0.4 h, respectively). Ceftriaxone was much more effective than cefotiam. The bacterial titer in the vegetations (log10 CFU per gram of vegetation) was 7.56 +/- 1 with cefotiam and 2.41 +/- 2.6 with ceftriaxone, as their concentrations were 18 and 466 times higher, respectively, than their MBCs. Although ceftriaxone and cefmenoxime exhibited a similar rate of killing and percentage of protein binding, ceftriaxone was more effective than cefmenoxime at the same regimen of 15 mg/kg twice a day (3.08 +/- 1.1 versus 4.82 +/- 3.2 log10 CFU/g of vegetation). When antibiotic was given as a single daily injection of 30 mg/kg, the antibacterial effect persisted for ceftriaxone, but not for cefmenoxime. The longer elimination half-life and the higher local concentration/MBC ratio of ceftriaxone explained these results. The bacterial titer measured 24 h after the fourth injection of 30 mg of ceftriaxone per kg confirmed that this regimen prevented regrowth of bacteria. These results suggest that the local antibiotic level/MBC ratio roughly correlated with the antibacterial effect and could represent an adequate basis to explain the differences observed between the drugs in vivo. They also demonstrate that, provided that the dose is sufficient, a long-acting broad-spectrum cephalosporin may be effective in severe gram-negative infections, even when given at relatively long dosing intervals, in contrast with a rapidly cleared drug with the same intrinsic activity.
pubmed:commentsCorrections
http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-1086635, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-1117194, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-3510263, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-3516963, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-3710965, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-3878128, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-4091526, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-4492776, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-6260870, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-6275779, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-6282203, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-6297387, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-6316841, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-6826714, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-7013003, http://linkedlifedata.com/resource/pubmed/commentcorrection/3300530-7033400
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0066-4804
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
518-22
pubmed:dateRevised
2009-11-18
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Comparative efficacy of cefotiam, cefmenoxime, and ceftriaxone in experimental endocarditis and correlation with pharmacokinetics and in vitro efficacy.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't