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Pharmacological particulars
ATCvet code: QJ01CR02
Pharmacodynamics
Amoxicillin is an aminobenzylpenicillin from the β-lactam penicillin family which prevents the bacterial cell wall formation by interfering with the final step of peptidoglycan synthesis.
Clavulanic acid is an irreversible inhibitor of intracellular and extracellular β-lactamases which protects amoxicillin from inactivation by many β-lactamases.
Amoxicillin/clavulanate has a wide range of activity which includes β-lactamase producing strains of both Gram-positive and Gram-negative aerobes, facultative anaerobes and obligate anaerobes. The antimicrobial spectrum relevant for dog’s and cat’s indications is summarized in the two tables below.
Summary of susceptibility for dog target bacteria:
Target bacteria in each indication
n
Range of MIC (µg/mL)
MIC50 (µg/mL)
MIC90 (µg/mL)
Clinical breakpoints (I/R)
Skin and soft tissues
Staphylococcus spp
431*
0.03-32
0.12
1
0.25/1
S. aureus
38*
0.12-16
0.5
2
0.25/1
S. intermedius group
343*
0.03-8
0.12
0.5
0.25/1
Coagulase-negative
49*
0.03-32
0.12
2
0.25/1
Staphylococcus spp
Streptococcus spp
142*
0.015-0.06
≤0.015
≤0.015
Streptococcus canis
127*
0.015-0.06
≤0.015
≤0.015
Streptococcus
dysgalactiae
12*
0.015
≤0.015
≤0.015
Pasteurella spp
22*
0.03-0.25
0.12
0.25
Respiratory
Staphylococcus spp
112*
0.06-8
0.12
0.5
S. intermedius group
90*
0.06-8
0.12
0.25
S. aureus
22*
0.12-8
0.25
1
Dental
Streptococcus spp
16**
0.008 - 1
0.014
0.4
Pasteurella spp
68**
0.03 - 64
0.124
0.4
Urinary
Escherichia coli
236*
1-32
4
16
8/-
Klebsiella spp
33*
0.5-32
2
32
8/-
Proteus spp
66*
0.5-16
1
8
8/-
Digestive
Escherichia coli
- *
1-32
4
8
Clavaseptin: Dog
Table
Breakpoints are from CLSI VET01-S7.
* MIC values determined from bacteria collected in Europe in 2021-2022 (ComPath-IV survey). Susceptibility of digestive isolates is assumed similar to that of the same bacteria in other types of infection.
** MIC values determined from bacteria collected from dog dental infections in Europe in 2002.
- Missing information.
Summary of susceptibility for cat target bacteria:
Target bacteria in each indication
n
Range of MIC (μg/mL)
MIC50 (μg/mL)
MIC90 (μg/mL)
Clinical breakpoints (I/R)
Skin and soft tissues
Staphylococcus spp
150*
0.03-32
0.12
1
0.25/1
S. aureus
50*
0.03-32
0.25
1
0.25/1
S. intermedius group
32*
0.03-32
0.12
8
0.25/1
Coagulase-negative
66*
0.03-8
0.06
0.25
0.25/1
Staphylococcus spp
S. felis
50*
0.03-0.12
0.06
0.12
0.25/1
Streptococcus spp
30*
0.015-0.06
≤0.015
≤0.015
0.25/1
Streptococcus canis
27*
0.015-0.03
≤0.015
≤0.015
0.25/1
Pasteurella spp
58*
0.015-2
0.25
0.25
0.25/1
Respiratory
Staphylococcus spp
89*
0.03-8
0.12
1
Coagulase-negative
77*
0.03-8
0.12
1
Staphylococcus spp
S. intermedius group
12*
0.03-2
0.12
1
S. aureus
30*
0.12-8
0.5
4
S. felis
40*
0.03-0.12
0.06
0.12
Dental
Streptococcus spp
Pasteurella spp
Urinary
Escherichia coli
132*
1-32
4
8
8/-
Pasteurella multocida
0.25/1
Klebsiella spp
19*
1-32
2
32
8/-
Proteus spp
17*
0.5-32
1
4
8/-
Digestive
Escherichia coli
- *
1-32
4
8
Clavaseptin: Cat
Table
Breakpoints are from CLSI VET01-S7.
* MIC values determined from bacteria collected in Europe in 2021-2022 (ComPath-IV survey). Susceptibility of digestive isolates is assumed similar to that of the same bacteria in other types of infection.
- Missing information.
The two main mechanisms of resistance to amoxicillin/clavulanic acid are inactivation by β- lactamases that are not inhibited by clavulanic acid, and alteration of penicillin binding proteins, which lead to co-resistance to other β-lactam antibiotics. Impermeability of bacteria or efflux pump mechanisms may also contribute to bacterial resistance, including co- and cross-resistance. Susceptibility and resistance patterns can vary with geographical area and bacterial strain, and may change over time.
Pseudomonas spp are naturally resistant to the amoxicillin – clavulanic acid combination. Methicillin resistant S. aureus (MRSA) and methicillin resistant S. pseudintermedius (MRSP) isolates have been identified in cats and dogs and should be considered resistant to all β-lactam including amoxicillin/clavulanic acid combination.
High resistances (up to 100%) have been reported in E. coli isolates from skin and soft tissue infections in dogs.
Pharmacokinetic particulars
After oral administration at the recommended dose in dogs and cats, the absorption of amoxicillin and clavulanic acid is fast. In dogs, the maximum plasma concentration of amoxicillin of 8.5 µg/ml is reached in 1.4 hours and the maximum plasma concentration of clavulanic acid of 0.9 µg/ml is reached in 0.9 hours. Half-life is 1 hour in dogs for both substances.
In cats, the maximum plasma concentration of amoxicillin of 6.6 µg/ml is reached in 1.8 hours and the maximum plasma concentration of clavulanic acid of 3.7 µg/ml is reached in 0.75 hours. Half-life is 1 to 2 hours in cats for both substances.
Elimination is also fast. 12 % of the amoxicillin and 17 % of clavulanic acid is excreted in the urine. The remainder is excreted as inactive metabolites. After repeated oral administration of the recommended dose in dogs and cats, there is no accumulation of amoxicillin or clavulanic acid and the steady state is reached rapidly after first administration.