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1.
J Vet Pharmacol Ther ; 43(5): 435-439, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32743801

RESUMO

The objective of this study was to determine the pharmacokinetics of tolfenamic acid (TA) following intravenous (IV) administration at doses of 2 and 4 mg/kg in goats. In this study, six healthy goats were used. TA was administered intravenously to each goat at 2 and 4 mg/kg doses in a cross-over pharmacokinetic design with a 15-day washout period. Plasma concentrations of TA were analyzed using the high performance liquid chromatography with ultraviolet detector, and pharmacokinetic parameters were assigned by noncompartmental analysis. Following IV administration at dose of 2 mg/kg, area under the concentration-time curve (AUC0-∞ ), elimination half-life (t1/2ʎz ), total clearance (ClT ) and volume of distribution at steady state (Vdss ) were 6.64 ± 0.81 hr* µg/ml, 1.57 ± 0.14 hr, 0.30 ± 0.04 L h-1  kg-1 and 0.40 ± 0.05 L/kg, respectively. After the administration of TA at a dose of 4 mg/kg showed prolonged t1/2ʎz , increased dose-normalized AUC0-∞ , and decreased ClT . In goats, TA at 4 mg/kg dose can be administered wider dose intervals compared to the 2 mg/kg dose. However, further studies are needed to determine the effect of different doses on the clinical efficacy of TA in goats.

2.
J Vet Pharmacol Ther ; 43(5): 440-447, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32815194

RESUMO

The pharmacokinetics of cefquinome (2 mg/kg every 24 hr for 5 days) was determined following intramuscular administration alone and co-administration with ketoprofen (3 mg/kg every 24 hr for 5 days) in goats. Six goats were used for the study. In the study, the crossover pharmacokinetics design with 20-day washout period was performed in two periods. Plasma concentrations of cefquinome were assayed using high-performance liquid chromatography by ultraviolet detection. The mean terminal elimination half-life (t1/2ʎz ), area under the concentration-time curve (AUC0-24 ), peak concentration (Cmax ), apparent volume of distribution (Vdarea /F), and total body clearance (CL/F) of cefquinome after the administration alone were 4.85 hr, 11.06 hr*µg/ml, 2.37 µg/mL, 1.23 L/kg, and 0.17 L/h/kg after the first dose, and 5.88 hr, 17.01 hr*µg/mL, 3.04 µg/mL, 0.95 L/kg, and 0.11 L/h/kg after the last dose. Ketoprofen significantly prolonged t1/2ʎz of cefquinome, increased AUC0-24 and Cmax , and decreased Vdarea /F and CL/F. Cefquinome exhibited low accumulation after the administration alone and in combination with ketoprofen. These results indicated that ketoprofen prolonged the elimination of cefquinome in goats. The 24-hr dosing intervals at 2 mg/kg dose of cefquinome, which co-administered with ketoprofen, may maintain T> minimum inhibitory concentration (MIC) values above 40% in the treatment of infections caused by susceptible pathogens with the MIC value of ≤0.75 µg/ml in goats with an inflammatory condition.

3.
J Vet Pharmacol Ther ; 43(5): 429-434, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32420638

RESUMO

The aim of this study was to determine the changes in the pharmacokinetics of meloxicam in goat kids who were castrated following the administration of xylazine. Six goat kids were used for the study. The study was performed in two periods according to a longitudinal study, with a 15-day washout period between periods. In the first period (Control group), 1 mg/kg meloxicam was administered by i.v. route to kids. In the second period (Castration group), the kids were sedated with 0.3 mg/kg xylazine and castration was performed following meloxicam administration. Plasma meloxicam concentration was analyzed using HPLC-UV, and pharmacokinetic parameters were calculated by noncompartmental model. In the control group following the administration of meloxicam, mean elimination half-life (t1/2 ʎz ), area under the concentration-time curve (AUC0-∞ ), total body clearance (ClT ), and volume of distribution at steady-state (Vdss ) were 13.50 ± 0.62 hr, 41.10 ± 2.86 hr µg/ml, 24.43 ± 1.75 ml hr-1  kg-1 , and 0.45 ± 0.03 L/kg, respectively. In the castration group, the t1/2 ʎz of meloxicam prolonged, AUC0-∞ increased, and ClT and Vdss decreased. In conclusion, the excretion of meloxicam from the body slowed and the t1/2 ʎz was prolonged in the castrated goat kids following xylazine administration. However, there is a need to determine the pharmacodynamics of meloxicam in castrated goat kids.

4.
Andrologia ; 52(2): e13499, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31828839

RESUMO

Aluminium is a ubiquitous element that occurs naturally in the soil making human exposure to it is unavoidable. Tyrosol is present in olive oil and is known to have antioxidant effects. Therefore, the present study explores the toxic effects of aluminium chloride (AlCl3 ) and evaluates the possible protection by tyrosol in male rats. Testicular injury was induced by the administration of AlCl3 (34 mg kg-1  day-1 ). Rats were treated with either tyrosol (20 mg kg-1 day-1 ) or AlCl3 (34 mg kg-1 day-1 ). The experiment lasted for 10 weeks. Biochemical, histopathological and protein expression profiles were determined to decipher the role of tyrosol in protecting the cellular damage. Further, histomorphometric analyses of testes showed deranged architecture along with other noted abnormalities. AlCl3 group rats' testes showed decreased GSH levels, CAT activities, Nrf-2, HO-1, bcl-2 expressions and sperm motility whereas increased caspase-3 expressions, MDA levels, abnormal and dead/live sperm ratio. However, tyrosol treatment attenuated these changes. The present results demonstrate the beneficial role of tyrosol treatment in AlCl3 induced testicular toxicity alterations of rat.

5.
6.
Inflammation ; 42(5): 1680-1691, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31115770

RESUMO

In this study, the effects of tyrosol were investigated in DSS-induced experimental ulcerative colitis model. For this purpose, rats were divided into five groups of seven rats in each: control group, colitis group (DSS-4%), tyrosol group (tyrosol 20 mg/kg), sulfasalazine (sulfasalazine+DSS 100 mg/kg), and treatment group (tyrosol+DSS 20 mg/kg). In the study, the active substances were administered to all animals for a period of 21 days. At the end of the study, malondialdehyde (MDA) levels increased (p < 0.001); GSH level (p < 0.05) along with GSH.Px (p < 0.01) and CAT (p < 0.001) activities decreased in the DSS-induced colitis group. However, with the administration of tyrosol, MDA and GSH levels along with GSH.Px and CAT activities came to the same levels as the control group. In the colitis group, an increase occurred in IL-6, COX-2, and NF-κB parameters, which created a significant difference compared to the control group (p < 0.001). Similarly, TNF-α levels also significantly increased with the administration of DSS (p < 0.05) which created a significant difference compared to the control group, while there was no difference among the other groups. As for the Nrf-2 data, it decreased with the administration of DSS which created a significant difference compared to the control group (p < 0.05), while there was no difference in other groups. In the colitis-induced group, IL-6, COX-2, and NF-κB gene expression levels also similarly increased but returned to the normal levels with the administration of tyrosol. In the histopathological scoring, the negativity that increased with the administration of DSS returned to the normal levels with the administration of tyrosol+DSS. In conclusion, according to the data obtained, tyrosol fixed the destruction picture in the DSS-induced colitis model, giving rise to thought that it has a protective effect.


Assuntos
Antioxidantes/uso terapêutico , Colite Ulcerativa/tratamento farmacológico , Álcool Feniletílico/análogos & derivados , Substâncias Protetoras/uso terapêutico , Animais , Antioxidantes/farmacologia , Colite Ulcerativa/induzido quimicamente , Ciclo-Oxigenase 2/metabolismo , Sulfato de Dextrana , Glutationa/efeitos dos fármacos , Glutationa/metabolismo , Malondialdeído/metabolismo , NF-kappa B/metabolismo , Álcool Feniletílico/farmacologia , Álcool Feniletílico/uso terapêutico , Substâncias Protetoras/farmacologia , Ratos , Fator de Necrose Tumoral alfa/metabolismo
7.
Inflammopharmacology ; 2018 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-29736689

RESUMO

OBJECTIVE: To compare the potential protective effects of conventional and colon-targeted lycopene (TLC) and linalool (TLN) on acetic acid (AA)-induced ulcerative colitis (UC) in rats. METHODS: Conventional and colon-targeted LC (10 mg/kg) and LN (200 mg/kg) were administered in vivo orally for 7 days and sulfasalazine (100 mg/kg) was also used as reference drug. Then, 4% AA was administered intrarectally to induce UC. Subsequently, the colon tissues were taken as samples for biochemical and histopathological analysis. RESULTS: Malondialdehyde (MDA), interleukin 1ß (IL-1ß), IL-6, cyclooxygenase-2 (COX-2) and nuclear factor kappa B (NF-κB) levels were decreased (p < 0.05) in the targeted groups compared to the AA group, whereas nuclear factor-erythroid 2-related factor 2 (Nrf-2) level was increased (p < 0.05). Tumor necrosis factor α (TNF-α) level was also decreased (p < 0.05) and catalase activity (CAT) was increased (p < 0.05) in the TLC group compared to the AA group. IL-1ß and IL-6 levels were lower in the TLC group compared to the conventional LC and sulfasalazine groups (p < 0.05). COX-2 and NF-κB levels were lower, while the Nrf-2 level was higher in the targeted groups compared to the conventional groups (p < 0.05). Furthermore, COX-2 level was lower and Nrf-2 level was higher in the targeted groups compared to the sulfasalazine group (p < 0.05). CONCLUSION: As expected, sulfasalazine was effective on all parameters analyzed, but the colon-targeted pretreatments were more effective from sulfasalazine on some parameters. Therefore, colon-targeted plant-derived therapies might be alternative approaches to provide protection against UC, which deserves to be investigated further.

8.
Mar Pollut Bull ; 125(1-2): 487-491, 2017 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-28802660

RESUMO

The aim of the present study was to determine the concentrations of the most investigated environmentally relevant heavy metals in two highly endangered sea turtle species (Caretta caretta and Chelonia mydas) from the important nesting area on the Northeast Mediterranean Sea. The highest mean concentration was of Fe, while Hg and Pb were lowest. All tissue concentrations of Al, As, Fe and Mn were significantly different between the species. In particular, As, Cd, Cu, Mn, Ni, Se, Zn concentrations were lower in Caretta caretta and Cd, Hg, Mn, Zn concentrations were lower in Chelonia mydas than those reported in other parts of the world. Compared to studies conductud in other parts of the Mediterranean, Cd was lower.


Assuntos
Arsênico/análise , Metais Pesados/análise , Tartarugas/sangue , Poluentes Químicos da Água/análise , Animais , Arsênico/sangue , Monitoramento Ambiental , Feminino , Rim/química , Fígado/química , Masculino , Mar Mediterrâneo , Metais Pesados/sangue , Poluentes Químicos da Água/sangue
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