Cadorex pharmacology
The pharmacokinetic disposition of Cadorex™ was evaluated in feeder calves following a single subcutaneous injection at a dose rate of 40 mg Cadorex/kg body weight. Administration of Cadorex™ resulted in Cadorex plasma concentrations of 2 µg (mcg)/mL within two hours of injection.
Cmax (µg/mL) | Tmax (hr) | AUClast (µg*hr/mL) | T½ (hr) | |
---|---|---|---|---|
Cmax: Maximum observed plasma concentration Tmax: Time at which Cmax was observed AUClast: Area under the plasma-concentration-time curve from time zero to the last quantifiable concentration that is equal to or greater than the limit of quantification of the validated analytical method T½: Terminal elimination half-life % CV: Percent coefficient of variance | ||||
| ||||
n | 24 | 24 | 24 | 23* |
Mean | 5.93 | 5† | 150 | 37.7 |
% CV | 38.3 | 2-12† | 20.9 | 27.3 |
Figure 1. Mean Cadorex Plasma Concentration versus Time Following a Single Subcutaneous Injection of Cadorex™ at a Dose Rate of 40 mg Florfenico/kg Body Weight in Feeder Calves (Mean ± Standard Error of the Mean) |
MICROBIOLOGY
Cadorex is a synthetic, broad-spectrum antibiotic active against many Gram-negative and Gram-positive bacteria isolated from domestic animals. It acts by binding to the 50S ribosomal subunit and inhibiting bacterial protein synthesis. Cadorex is generally considered a bacteriostatic drug, but it exhibits bactericidal activity against certain bacterial species. In vitro studies demonstrate that Cadorex is active against the BRD pathogens M. haemolytica, P. multocida, H. somni, and M. bovis and that Cadorex exhibits bactericidal activity against strains of M. haemolytica and H. somni.
The minimum inhibitory concentrations (MICs) of Cadorex were determined for BRD isolates obtained from calves enrolled in BRD field studies in the U.S. in 2006 using methods recommended by the Clinical and Laboratory Standards Institute (M31-A2). Isolates were obtained from pre-treatment nasal swabs from all calves enrolled at all four sites, post-treatment nasal swabs from treatment failures in the Cadorex Injectable Solution and saline control treatment groups at three sites, and lung tissue from one calf that died in the saline control treatment group. The results are shown below in Table 2.
Indicated pathogens | Year of isolation | No. of isolates | MIC50† (µg/mL) | MIC90† (µg/mL) | MIC range (µg/mL) |
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| |||||
Mannheimia haemolytica | 2006 | 158 | 1.0 | 1.0 | 0.5 to 32 |
Pasteurella multocida | 2006 | 103 | 0.5 | 0.5 | ≤ 0.125 to 16 |
Histophilus somni | 2006 | 85 | ≤ 0.125 | ≤ 0.125 | ≤ 0.125 to 0.25 |
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Information checked by Dr. Sachin Kumar, MD Pharmacology