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Mean plasma penicillin concentration time curves after 20 000 IU procaine penicillin G/kg was administered to five animals (4 horses, 1 pony) at five different sites (after Firth et al. 1986 5 ).
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Various types of information contribute to the selection of an antimicrobial agent. Initial requirements are diagnosis of the site and nature of the infection, assessment of the severity of the infectious process and medical condition of the diseased animal; these are embodied in clinical experience. Additional considerations include identification...
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... to horses but care must be taken to avoid inadvertent intravenous administration. The intramuscular injec- tion of procaine penicillin G in the neck region (M. serratus ventralis cervicis) produces a higher peak plasma concen- tration and higher systemic availability of penicillin G than injection of the long-acting product at other locations 5 (Fig. 1). The prime site for intramuscular injection in the neck of the horse appears to be at the level of the 5th cervical verte- bra, ventral to the funicular part of the ligamentum nuchae but dorsal to the brachiocephalic muscle 3 . The location of the intramuscular injection site does not affect the bioavailability (refers to rate and ...
Citations
... Furthermore, the AUC IM/IV ratio of MAA was over one, which indicates satisfactory absorption leading to systemic circulation of the drug after IM MET administration (assuming that MET had been totally converted to MAA after both IV and IM administrations). In a previous study, it was speculated that the IM injection site might affect the AUC value due to regional differences in blood flow and that the lateral neck would provide larger absorptive area with higher blood flow to tissues when compared to the buttock region (Baggot, 1998). However, although the goats received MET at the buttock area where the cats and dogs had been injected in previous studies, the present AUC IM/IV ratio value was evidently higher than that from the previously studied cats (0.63 ± 0.41) and dogs (0.75 ± 0.11). ...
Metamizole (dipyrone, MET) is a nonopioid analgesic drug commonly used in human and veterinary medicine. The aim of this study was to assess two major active metabolites of MET, 4‐methylaminoantipyrin (MAA) and 4‐aminoantipyrin (AA), in goat plasma after intravenous (IV) and intramuscular (IM) administration. In addition, metabolite concentration in milk was monitored after IM injection. Six healthy female goats received MET at a dose of 25 mg/kg by IV and IM routes in a crossover design study. The blood and milk samples were analyzed using HPLC coupled with ultraviolet detector and the plasma vs concentration curves analyzed by a noncompartmental model. In the goat, the MET rapidly converted into MAA and the mean maximum concentration was 183.97 μg/ml (at 0.08 hr) and 51.94 μg/ml (at 0.70 hr) after IV and IM administration, respectively. The area under the curve and mean residual time values were higher in the IM than the IV administered goats. The average concentration of AA was lower than MAA in both groups. Over 1 μg/ml of MAA was found in the milk (at 48 hr) after MET IM administration. In conclusion, IM is considered to be a better administration route in terms of its complete absorption with long persistence in the plasma. However, this therapeutic option should be considered in light of the likelihood of there being milk residue.
... ratio was found in a recent study in the dog (Giorgi et al., submitted), which used the same injection site, buttock muscle, as the present study, whereas, horses, sheep, and donkeys were injected in the neck muscle (Aupanun et al., 2016;Giorgi et al., 2015Giorgi et al., , 2017. In general, the extent of systemic T A B L E 2 Main pharmacokinetic profile (mean ± SD) of 4-aminoantipyrine (AA) in cats (n = 6) following intravenous (i.v.), intramuscular (i.m.), and per oral (p.o.) administration of metamizole (25 mg/kg) absorption of drugs injected intramuscularly is higher when the site of injection is the lateral neck compared to the buttock region, as this location provides a larger absorptive surface area with higher blood flow to tissues (Baggot, 1998). Moreover, although there are no reports on injection site-dependent differences in MET hydrolysis, a previous study implicated the influence of physicochemical factors, such as pH, temperature, and drug concentration on MET hydrolysis rate (Ergün, Frattarelli, & Aranda, 2004). ...
This study was performed to determine pharmacokinetic profiles of the two active metabolites of the analgesic drug metamizole (dipyrone, MET), 4-methylaminoantipyrine (MAA), and 4-aminoantipyrine (AA), after intravenous (i.v., intramuscular (i.m.), and oral (p.o.) administration in cats. Six healthy mixed-breed cats were administered MET (25 mg/kg) by i.v., i.m., or p.o. routes in a crossover design. Adverse clinical signs, namely salivation and vomiting, were detected in all groups (i.v. 67%, i.m. 34%, and p.o. 15%). The mean maximal plasma concentration of MAA for i.v., i.m., and p.o. administrations was 148.63 ± 106.64, 18.74 ± 4.97, and 20.59 ± 15.29 μg/ml, respectively, with about 7 hr of half-life in all routes. Among the administration routes, the area under the plasma concentration curve (AUC) value was the lowest after i.m. administration and the AUCEV/i.v. ratio was higher in p.o. than the i.m. administration without statistical significance. The plasma concentration of AA was detectable up to 24 hr, and the mean plasma concentrations were smaller than MAA. The present results suggest that MET is converted into the active metabolites in cats as in humans. Further pharmacodynamics and safety studies should be performed before any clinical use.
Cephalosporins (CEFs) are antibiotics frequently used to treat bone infections and septic arthritis. The effects of CEFs on chondrocytes have not been studied until now. Cefazolin (cef1) and ceftriaxone (cef3), first-and third-generation CEFs, were selected to investigate their direct effects on normal and osteoarthritic (OA) primary canine chondrocytes, which were either nonstimulated or stimulated with the pro-inflammatory cytokine IL-1β. In our results, treatment with CEFs increased the negative effects on both conditioned normal and OA chondrocytes, especially when applied to IL-1β-stimulated cells (inflammatory stimulus). CEFs significantly decreased cell viability and induced apoptotic cell death in both normal and OA chondrocytes; moreover, treatment with cef1 caused necrotic cell death in OA chondrocytes. Cef3 treatment could increase s-GAG synthesis in normal cells preincubated with IL-1β, while cef1 had no significant effect. The expression of TNF was clearly downregulated after cef3 treatments, whereas it was upregulated after cef1 treatments. However, cef3 induced stronger downregulation of TIMP1 and the extracellular matrix component genes COL2A1 and ACAN. In conclusion, these results suggest both the cytotoxic effects of CEFs and their adverse effects on chondrogenic marker genes at the transcriptional level, which provide additional insight into the clinical application of cef1 and cef3.
Increased interest in nanosilver during the last 10 years is mainly explained by the emergence and spread of pathogenic microorganisms with multiple drug resistance, including resistance to last-generation antibiotics. In this article, we for the first time, give a description of large-scale clinical trials of a new nanosilver based antibacterial drug [containing two active components: silver nanoparticles (AgNPs) (10–50 ppm) and benzyldimethyl[3-(miristoylamino)-propyl]ammonium chloride (100 ppm)] registered in Russia in 2015 as a veterinary drug under the brand name Argumistin™. This drug has been approved for application in a diluted dosage form – as eye drops, intranasal drops and orally; it has also been approved for application in a more concentrated dosage form (up to 50 ppm of nanosilver) as ear drops and as an antiseptic during demodicosis and gum disease treatment, open wound treatment, etc. We have registered the high therapeutic effectiveness of Argumistin™ during treatment of infectious conjunctivitis, gingivitis, parodontosis and enteritis of dogs. Application of this antibacterial drug gives considerable (up to 70% in case of periodontal diseases) reduction in the treatment period and prevention of complications. The results of clinical trials in the treatment of infectious diseases of dogs makes Argumistin™ a promising candidate for an effective antibacterial drug for human medicine.
