Fluoroquinolones are used for the treatment of deep and superficial skin infections, urinary tract infections in dogs, skin and soft tissue infections in cats, acute upper respiratory tract infections.
Used for respiratory tract, digestive tract, urinary tract and skin infection caused by sensitive bacteria in cattle, pigs, dogs and cats. There is also a whitlow effect on bovine and sheep mastitis and pig mastitis - hysteritis - agalactia syndrome.
Mbofloxacin is a novel fluoroquinolone antibiotic, which inhibits the growth of bacteria by inhibiting THE DNA transcriptase of bacteria, and has antibacterial effects on gram-negative bacteria, gram-positive bacteria and mycoplasma. Mbofloxacin can be well absorbed by oral and injection administration with low toxicity.
Pharmacodynamics: wide antibacterial spectrum and strong antibacterial activity. The MIC90 of most Enterobacter, Pasteurella multocide, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus intermediatus were 0.08-0.28, 0.04, 0.94, 0.2 and 0.23μg/mL, respectively, which were comparable to enrofloxacin and ciprofloxaci. The MIC90 of pasteurella multocide, Pasteurella hemolyticus, Haemophilus comatose and mycoplasma were 0.02, 0.17, 0.03 and 0.48μg/mL, respectively. This product is resistant to the following drugs such as erythromycin, lincomycin, chlomphenicol, doxycycline, sulfonamide drugs of the pathogen is still effective.
Table 1: Mean pharmacokinetic parameters following intravenous administration of marbofloxacin to 6 adult beagle dogs at a dosage of 2.5 mg/lb.
|
Parameter
|
Estimate ± SD* n=6
|
|
Total body clearance, (mL/h•kg)
|
94 ± 8
|
|
Volume of distribution at steady state, Vss, (L/kg)
|
1.19 ± 0.08
|
|
AUC0-inf (μg•h/mL)
|
59 ± 5
|
|
Terminal plasma elimination half-life, t1/2(h)
|
9.5 ± 0.7
|
* SD = standard deviation
Table 2: Mean pharmacokinetic parameters following oral administration of marbofloxacin tablets to adult beagle dogs at a nominal dosage of 1.25 mg/lb or
2.5 mg/lb and to cats at 2.5 mg/lb.†
|
Parameters
|
Dog Estimate ± SD* (1.25 mg/lb) n=6
|
Dog Estimate ± SD* (2.5 mg/lb) n=6
|
Cat Estimate ± SD* (2.5 mg/lb) n=7
|
|
Time of maximum concentration, Tmax(h)
|
1.5 ± 0.3
|
1.8 ± 0.3
|
1.2 ± 0.6
|
|
Maximum concentration, Cmax, (μg/mL)
|
2.0 ± 0.2
|
4.2 ± 0.5
|
4.8 ± 0.7
|
|
AUC0-inf (μg•h/mL)
|
31.2 ± 1.6
|
64 ± 8
|
70 ± 6
|
|
Terminal plasma elimination half-life, t1/2(h)
|
10.7 ± 1.6
|
10.9 ± 0.6
|
12.7 ± 1.1
|
† mean actual dosages administered to dogs were 1.22 mg/lb and 2.56 mg/lb, respectively, and the mean
actual dosage administered to cats was 2.82 mg/lb.
* SD = standard deviation
Figure 2: Mean plasma concentrations (µg/mL) following single oral administration of marbofloxacin to adult beagle dogs at dosages of 1.25 mg/lb or 2.5 mg/lb.
* See Table 4 in Microbiology section for MIC data.
Figure 3: Mean plasma concentrations (µg/mL) following single oral administration of marbofloxacin to adult cats at a dosage of 2.5 mg/lb.
* See Table 5 in Microbiology section for MIC data.
Table 3a: Tissue distribution following a single oral administration of marbofloxacin tablets to adult beagle dogs at a dosage of 1.25 mg/lb*.
|
Tissue
|
Marbofloxacin 2 hours (n=4)
|
Concentrations 18 hours (n=4)
|
(μg/g ± SD) 24 hours (n=4)
|
|
bladder
|
4.8 ± 1.1
|
2.6 ± 1.5
|
1.11 ± 0.19
|
|
bone marrow
|
3.1 ± 0.5
|
1.5 ± 1.5
|
0.7 ± 0.2
|
|
feces
|
15 ± 9
|
48 ± 40
|
26 ± 11
|
|
jejunum
|
3.6 ± 0.5
|
1.3 ± 1.0
|
0.7 ± 0.3
|
|
kidney
|
7.1 ±1.7
|
1.4 ± 0.5
|
0.9 ± 0.3
|
|
lung
|
3.0 ± 0.5
|
0.8 ± 0.2
|
0.57 ± 0.19
|
|
lymph node
|
5.5 ± 1.1
|
1.3 ± 0.3
|
1.0 ± 0.3
|
|
muscle
|
4.1 ± 0.3
|
1.0 ± 0.3
|
0.7 ± 0.2
|
|
prostate
|
5.6 ± 1.4
|
1.8 ± 0.6
|
1.1 ± 0.4
|
|
skin
|
1.9 ± 0.6
|
0.41 ± 0.13
|
0.32 ± 0.08
|
* SD = standard deviation
Table 3b: Tissue distribution following a single oral administration of marbofloxacin tablets to adult beagle dogs at a dosage of 2.5 mg/lb.
|
Tissue
|
Marbofloxacin 2 hours (n=4)
|
Concentrations 18 hours (n=4)
|
(μg/g ± SD*) 24 hours (n=4)
|
|
bladder
|
12 ± 4
|
6 ± 7
|
1.8 ± 0.4
|
|
bone marrow
|
4.6 ± 1.5
|
1.28 ± 0.13
|
0.9 ± 0.3
|
|
feces
|
18 ± 3
|
52 ± 17
|
47 ± 28
|
|
jejunum
|
7.8 ± 1.1
|
2.0 ± 0.3
|
1.1 ± 0.3
|
|
kidney
|
12.7 ±1.7
|
2.7 ± 0.3
|
1.6 ± 0.2
|
|
lung
|
5.48 ± 0.17
|
1.45 ± 0.19
|
1.0 ± 0.2
|
|
lymph node
|
8.3 ± 0.7
|
2.3 ± 0.5
|
2.03 ± 0.06
|
|
muscle
|
7.5 ± 0.5
|
1.8 ± 0.3
|
1.20 ± 0.12
|
|
prostate
|
11 ± 3
|
2.7 ± 1.0
|
2.0 ± 0.5
|
|
skin
|
3.20 ± 0.33
|
0.705 ± 0.013
|
0.46 ± 0.09
|
* SD = standard deviation
Microbiology
The primary action of fluoroquinolones is to inhibit the bacterial enzyme, DNA gyrase. In susceptible organisms, fluoroquinolones are rapidly bactericidal at relatively low concentrations. Marbofloxacin is bactericidal against a broad range of gram-negative and gram-positive organisms. The minimum inhibitory concentrations (MICs) of pathogens isolated in clinical field studies performed in the United States were determined using National Committee for Clinical Laboratory Standards (NCCLS) standards, and are shown in Tables 4 and 5.
Table 4. MIC Values* (μg/mL) of marbofloxacin against pathogens isolated from skin, soft tissue and urinary tract infections in dogs enrolled in clinical studies conducted during 1994–1996.
|
Organism
|
No. of Isolates
|
MIC50
|
MIC90
|
MIC Range
|
|
Staphylococcus intermedius
|
135
|
0.25
|
0.25
|
0.125-2
|
|
Escherichia coli
|
61
|
0.03
|
0.06
|
0.015-2
|
|
Proteus mirabilis
|
35
|
0.06
|
0.125
|
0.03-0.25
|
|
Beta-hemolytic Streptococcus,
(not Group A or Group B)
|
25
|
1
|
2
|
0.5-16
|
|
Streptococcus,
Group D enterococcus
|
16
|
1
|
4
|
0.008-4
|
|
Pasteurella multocida
|
13
|
0.015
|
0.06
|
≤0.008-0.5
|
|
Staphylococcus aureus
|
12
|
0.25
|
0.25
|
0.25-0.5
|
|
Enterococcus faecalis
|
11
|
2
|
2
|
1-4
|
|
Klebsiella pneumonia
|
11
|
0.06
|
0.06
|
0.01-0.06
|
|
Pseudomonas spp.
|
9
|
**
|
**
|
0.06-1
|
|
Pseudomonas aeruginosa
|
7
|
**
|
**
|
0.25-1
|
* The correlation between in vitro susceptibility data (MIC) and clinical response has not been
determined.
** MIC50 and MIC90 not calculated due to insufficient number of isolates.
Table 5: MIC Values* (μg/mL) of marbofloxacin against pathogens isolated from
skin and soft tissue infections in cats enrolled in clinical studies conducted in 1995
and 1998.
|
Organism
|
No. of Isolates
|
MIC50
|
MIC90
|
MIC Range
|
|
Pasteurella multocida
|
135
|
0.03
|
0.06
|
≤0.008-0.25
|
|
Beta-hemolytic Streptococcus
|
22
|
1
|
1
|
0.06-1
|
|
Staphylococcus aureus
|
21
|
0.25
|
0.5
|
0.125-1
|
|
Corynebacterium spp.
|
14
|
0.5
|
1
|
0.25-2
|
|
Staphylococcus intermedius
|
11
|
0.25
|
0.5
|
0.03-0.5
|
|
Enterococcus faecalis
|
10
|
2.0
|
2.0
|
1.0-2.0
|
|
Escherichia coli
|
10
|
0.03
|
0.03
|
0.015-0.03
|
|
Bacillus spp.
|
10
|
0.25
|
0.25
|
0.125-0.25
|
STORAGE CONDITIONS
Store below 30°C (86°F).
HOW SUPPLIED
Zeniquin tablets are available in the following strengths of marbofloxacin and bottle sizes:
25 mg scored tablets supplied in bottles that contain 100 or 250 tablets
50 mg scored tablets supplied in bottles that contain 100 or 250 tablets
100 mg scored tablets supplied in a 50 tablet bottle
200 mg scored tablets supplied in a 50 tablet bottle
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