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Pharmacological particulars
ATCvet code: QJ51RV01
Pharmacotherapeutic group
Antibacterials for intramammary use, combinations of antibacterials and corticosteroids.
Pharmacodynamic properties
Cefapirin is a first generation cephalosporin which acts by inhibition of cell wall synthesis. It is bactericidal with a time dependant mechanism of action and is characterised by its broad therapeutic spectrum of activity.
In vitro activity has been demonstrated against common Gram positive and Gram negative bacteria including Escherichia coli, Staphylococcus aureus, coagulase negative staphylococci, Streptococcus dysgalactiae, Streptococcus agalactiae, and Streptococcus uberis.
An overview of the MIC50 and MIC90 values of common bacterial mastitis pathogens collected for a resistance monitoring programme (VetPath programme from the European Animal Health Study Centre (CEESA)) is presented in the table below (except for data regarding Streptococcus agalactiae, which were gathered during clinical trials conducted between 1984 and 2005):
Bacterial species isolated
N
MIC50 (μg/ml)
MIC50 (μg/ml)
Staphylococcus aureus
192
0.12
0.25
Coagulase negative staphylococci
165
0.12
0.25
Streptococcus uberis
188
0.25
0.5
Streptococcus dysgalactiae
95
0.06
0.06
Streptococcus agalactiae
58
0.25
0.25
Escherichia coli
207
16
> 32
During the last 10 years only an increase in the MIC90 values of E.coli was observed.
Prednisolone exerts anti-inflammatory properties through the inhibition of the early and the late phases of inflammation. After intramammary application, prednisolone induces a reduction in the swelling and subsequent size of the infected quarter and promotes a return to normal temperature in infected animals
Pharmacokinetic properties
After intramammary administration of the veterinary medicinal product, cefapirin and prednisolone are mainly excreted via milk during milking. The absorption of both cefapirin and prednisolone into the blood stream is fast and limited. The absorbed fractions of both cefapirin and prednisolone are mainly excreted in urine.
An overview of the concentrations of cefapirin and prednisolone in milk during treatment is presented in the table below:
Active substance
Mean milk concentrations of active substances at milking relative to first treatment
0
1st milking
2nd milking
3rd milking
4th milking
Cefapirin (µg/ml)
0
27.0 ± 6.2
30.2 ± 7.9
40.0 ± 8.8
34.6 ± 6.5
Prednisolone (ng/ml)
0
182.0 ± 61.7
100.8 ± 51.0
283.7 ± 129.8
101.5 ± 38.8