Examples of using Ceftaroline in English and their translations into German
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Ceftaroline is primarily eliminated by the kidneys.
The active moiety after Zinforo administration is ceftaroline.
It is unknown whether ceftaroline fosamil or ceftaroline is excreted in human milk.
MIC has been shown tobe the parameter that best correlates with the efficacy of ceftaroline.
Ceftaroline is neither a substrate, nor an inhibitor of renal uptake transporters(OCT2, OAT1, and OAT3) in vitro.
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In vitro data indicate that the following species are not susceptible to ceftaroline.
Ceftaroline can be removed by haemodialysis; 21.6% of the dose was removed over a 4 hour dialysis period.
Seizures have occurred in toxicology studies at 7-25 times human ceftaroline Cmax levels see section 5.3.
The Cmax and AUC of ceftaroline increase approximately in proportion to dose within the single dose range of 50 to 1000 mg.
Clinical efficacy has not been established against the following pathogens although in vitrostudies suggest that they would be susceptible to ceftaroline in the absence of acquired mechanisms of resistance.
The plasma protein binding of ceftaroline is low(approximately 20%) and ceftaroline is not distributed into erythrocytes.
As with other beta-lactam antimicrobial agents, the percent time above the minimum inhibitory concentration(MIC) of the infecting organism over the dosing interval(%T> MIC)has been shown to be the parameter that best correlates with the efficacy of ceftaroline.
Hydrolysis of the beta-lactam ring of ceftaroline occurs to form the microbiologically inactive, open-ring metabolite, ceftaroline M-1.
As ceftaroline does not appear to undergo significant hepatic metabolism, the systemic clearance of ceftaroline is not expected to be significantly affected by hepatic impairment.
In pooled human liver microsomes, metabolic turnover was low for ceftaroline, indicating that ceftaroline is not metabolised by hepatic CYP450 enzymes.
However, when ceftaroline was administered throughout pregnancy and lactation, there was no effect on pup weight or growth.
As a result, minimum inhibitory concentrations(MICs) of ceftaroline against a proportion of these organisms tested fall into the susceptible range see Resistance section below.
Ceftaroline fosamil and ceftaroline were clastogenic in an in vitro chromosomal aberration assay, however there was no evidence of mutagenic activity in an Ames, mouse lymphoma and unscheduled DNA synthesis assay.
Organisms that express these enzymes and which are therefore resistant to ceftaroline occur at very variable rates between countries and between healthcare facilities within countries.
The mean plasma ceftaroline M-1 to ceftaroline AUC ratio following a single 600 mg intravenous infusion of ceftaroline fosamil in healthy subjects is approximately 20-30.
Following administration of a single 600 mg intravenous dose of ceftaroline fosamil, the pharmacokinetics of ceftaroline were similar between healthy elderly subjects(≥ 65 years of age), and healthy young adult subjects 18-45 years of age.
If ceftaroline is commenced before susceptibility test results are available then local information on the risk of encountering organisms that express these enzymes should be taken into consideration.
The median steady-state volume of distribution of ceftaroline in healthy adult males following a single 600 mg intravenous dose of radiolabeled ceftaroline fosamil was 20.3 l, similar to the volume of extracellular fluid.
When ceftaroline was administered during organogenesis, minor changes in foetal weight and delayed ossification of the interparietal bone were observed in the rat at exposures below that observed clinically.
The interaction potential of ceftaroline or ceftaroline fosamil on medicinal products metabolised by CYP450 enzymes is expected to be low since they are not inhibitors nor inducers of CYP450 enzymes in vitro.
Ceftaroline administration to pregnant rabbits resulted in an increased foetal incidence of angulated hyoid alae, a common skeletal variation in rabbit fetuses, at exposures similar to those observed clinically.