Browsing by Subject "Tildipirosin"

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    Disposition kinetics of tildipirosin in alpacas after parenteral administrations
    (Elsevier, 2023-11-10) Galecio, Juan Sebastian; Escudero, Elisa; Egas, David; Mena, Luis; Badillo Puerta, Elena; Marin, Pedro; Hernandis, Verónica; Farmacología
    Tildipirosin is a macrolide antibiotic marketed in veterinary medicine to treat respiratory infections in pigs and calves. There are no pharmacokinetics studies of tildipirosin after parenteral administration in alpacas which is an extremely decisive step for determining dosage regimen. Thus, the aim of the present study was to establish the disposition fate of tildipirosin following intravenous (IV), intramuscular (IM) and subcutaneous (SC) administrations in alpacas. A crossover study was used, and each alpaca received a single dose of tildipirosin by IV and IM or SC. All the routes of administration were adequately tolerated, and no adverse reactions was observed in any alpaca. Tildipirosin in alpacas reached peak concentrations (Cmax = 0.68 µg/mL vs. 0.79 µg/mL) at 0.22 and 0.50 h (tmax) after IM and SC administration, respectively, with an absolute bioavailability of >100 % for both routes of administration. Steady-state volume of distribution and clearance were 6.02 ± 1.34 L/kg and 2.76 ± 0.28 L/h/kg, respectively. Tildipirosin presents a particular pharmacokinetic behaviour in alpacas, distinctive from other ruminant species, confirming the need to perform studies in the target species in order to promote rational dose regimens of this antimicrobial to maximize its efficacy, minimize its toxicity and avoid the emergence of resistant bacteria.
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    Pharmacokinetics of tildipirosin in horses after intravenous and intramuscular administration and its potential muscle damage
    (Elsevier, 2022-07-23) Galecio Naranjo, Juan Sebastian; Escudero Pastor, Elisa; Badillo Puerta, Elena; Marín Carrillo, Pedro; Farmacología
    Tildipirosin is a novel semisynthetic macrolide antibiotic exclusively used in veterinary practice to treat respiratory infections. There are no pharmacokinetic or safety information available regarding the use of tildipirosin after intramuscular administration in horses. Thus, the objective of this work was to determine the disposition kinetics of tildipirosin after intravenous (IV) and intramuscular (IM) administration in horses and its potential muscle damage and cardiotoxicity. Six mature, Spanish-breed horses were used in a crossover study with a washout period of 30 days. Tildipirosin (18%) was administered at single doses by IV (2 mg/kg) and IM (4 mg/kg) routes. Tildipirosin plasma concentrations were determined by HPLC assay with ultraviolet detection. Muscle damage and inflammation were assessed by creatine kinase (CK) and haptoglobin (Hp), respectively. Creatine kinase myocardial band (CK-MB) and troponin (Tn) were used to evaluate cardiotoxicity. Tildipirosin in horses reached peak concentrations (Cmax = 1.13 μg/mL) at 0.60 h (tmax) after IM administration with an absolute bioavailability of 109.2%. Steady-state volume of distribution and clearance were 3.31 ± 0.57 L/kg and 0.22 ± 0.02 L/h/kg, respectively. Tildipirosin did not cause cardiotoxicity since CK-MB and Tn basal levels were not significantly different from those obtained after several days post-administration. Mild local reactions were observed after IM administration. This local inflammation was associated with mild myolysis (CK 239–837 UI/L), which was detectable for 48 h. In brief, tildipirosin could help to treat respiratory infections in horses because it showed extensive distribution, high bioavailability and did not provoke general adverse reactions.
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    Susceptibility of caprine mastitis pathogens to tildipirosin, gamithromycin, oxytetracycline, and danofloxacin: effect of serum on the in vitro potency of current macrolides
    (Springer, 2022-09-13) Galecio Naranjo, Juan Sebastian; Escudero Pastor, Elisa; Corrales, Juan Carlos; García-Romero, Edgar; Fe, Christian de la; Hernandis Belenguer, Verónica; Marín Carrillo, Pedro; Farmacología
    Mastitis is a significant disease in dairy ruminants, causing economic losses to the livestock industry and severe risks to public health. Antibiotic therapy is one of the most crucial practices to treat mastitis, although the susceptibility of caprine mastitis pathogens to current antibiotics has not been tested under standard or modified incubation conditions. This work evaluated the in vitro activity of tildipirosin, gamithromycin, oxytetracycline, and danofloxacin against caprine mastitis pathogens incubated following standard conditions of Clinical and Laboratory Standards Institute (CLSI) and deviation method by 25% supplementation with goat serum. Mycoplasma agalactiae, Escherichia coli, Staphylococcus aureus, Streptococcus spp., and coagulase-negative Staphylococci (CNS) were isolated from dairy goats with mastitis in Spain. Minimum inhibitory concentrations (MICs) were determined using the broth microdilution technique. The lowest MIC90 under standard conditions was obtained with danofloxacin for mastitis-causing pathogens. An exception was M. agalactiae, where danofloxacin and oxytetracycline obtained low values. However, after adding serum, gamithromycin showed the lowest MIC50 for S. aureus, Streptococcus spp., and CNS. The lowest MIC50 was obtained with all the antibiotics tested (< 0.125 µg/ml) against M. agalactiae. Supplementing with serum resulted in a significant variation in tildipirosin and gamithromycin MIC values for CNS, S. aureus, M. agalagtiae, and E. coli. In brief, the MIC for antibiotics used against mastitis should be determined under conditions closely resembling intramammary infections to obtain representative susceptibility patterns against mastitis pathogens. Caprine mastitis pathogens were broadly susceptible to danofloxacin under standard conditions. The potency of macrolides against caprine mastitis pathogens increases when serum is present in culture media.