Avaliação cardiovascular em eqüinos sedados com xilazina ou amitraz

Avaliaram-se efeitos cardiovasculares decorrentes da administração intravenosa (IV) de xilazina (1,0mg/kg) ou amitraz (0,1 ou 0,4mg/kg) em cavalos. Os índices ventriculares, a freqüência cardíaca (FC) e o débito cardíaco (DC) foram mensurados por ecocardiografia, e o bloqueio atrioventricular de segundo grau (BAV2), detectado por eletrocardiografia. A pressão arterial invasiva foi também avaliada. Todos os parâmetros foram mensurados imediatamente antes e durante 60 minutos após a administração dos fármacos. Os valores da FC, do DC e do BAV2 apresentaram alterações significativas nos grupos da xilazina e do amitraz na dose de 0,4mg/kg. A xilazina induziu hipertensão inicial 10 minutos após sua administração e a dose de 0,4mg/kg amitraz induziu hipotensão após 30 minutos. Exceto pela ocorrência de BAV2 aos cinco minutos, não houve alteração nas mensurações ecocardiográficas após a administração de amitraz-0.1mg/kg. Nas doses utilizadas, a xilazina (1,0mg/kg) e o amitraz-0,4mg/kg promoveram alterações semelhantes no sistema cardiovascular, porém os efeitos cardiovasculares provocados pelo amitraz foram mais prolongados.Cardiovascular effects due to intravenous (IV) xylazine (1.0mg/kg) or amitraz (0.1 or 0.4mg/kg) were evaluated in horses. Left ventricular function indexes, heart rate (HR), and cardiac output (CO) were measured by echocardiography. Second degree atrioventricular (AV) block was detected by electrocardiography. Invasive arterial blood pressure (AP) was also evaluated. All parameters were measured immediately before and during 60 minutes after drug injection. HR, CO, and second degree AV block were different between xylazine and amitraz-0.4mg/kg groups. Xylazine induced initial hypertension 10 minutes after injection, and hypotension was observed 30 minutes after amitraz-0.4mg/kg administration. Except for the second degree AV block which occurred only at five minutes, there was no change in the echocardiographic measurements after administration of amitraz-0.1mg/kg. Thus, amitraz-0.4mg/kg and xylazine (1.0mg/kg) induced similar cardiovascular side effects, but long-lasting action of amitraz-0.4mg/kg in the cardiovascular system was observed

Bioavailability and pharmacokinetics of oral and injectable formulations of methadone after intravenous, oral, and intragastric administration in horses

OBJECTIVE: To characterize the bioavailability and pharmacokinetics of oral and injectable formulations of methadone after IV, oral, and intragastric administration in horses. ANIMALS: 6 healthy adult horses. PROCEDURES: Horses received single doses (each 0.15 mg/kg) of an oral formulation of methadone hydrochloride orally or intragastrically or an injectable formulation of the drug orally, intragastrically, or IV (5 experimental treatments/horse; 2-week washout period between each experimental treatment). A blood sample was collected from each horse before and at predetermined time points over a 360-minute period after each administration of the drug to determine serum drug concentration by use of gas chromatography-mass spectrometry analysis and to estimate pharmacokinetic parameters by use of a noncompartmental model. Horses were monitored for adverse effects. RESULTS: In treated horses, serum methadone concentrations were equivalent to or higher than the effective concentration range reported for humans, without induction of adverse effects. Oral pharmacokinetics in horses included a short half-life (approx 1 hour), high total body clearance corrected for bioavailability (5 to 8 mL/min/kg), and small apparent volume of distribution corrected for bioavailability (0.6 to 0.9 L/kg). The bioavailability of methadone administered orally was approximately 3 times that associated with intragastric administration. CONCLUSIONS AND CLINICAL RELEVANCE: Absorption of methadone in the small intestine in horses appeared to be limited owing to the low bioavailability after intragastric administration. Better understanding of drug disposition, including absorption, could lead to a more appropriate choice of administration route that would enhance analgesia and minimize adverse effects in horses

Influência do treinamento aeróbio sobre o cortisol e glicose plasmáticos em equinos

Estudou-se a resposta do cortisol e da glicemia em 12 equinos da raça Puro Sangue Árabe destreinados (T0) por oito meses e submetidos a um período de 90 dias de treinamento aeróbio (T90). Para avaliação dos efeitos do treinamento, empregou-se teste ergométrico constituído de exercício progressivo em esteira rolante, acompanhado por colheitas de sangue 15 segundos antes do término de cada etapa de esforço. A velocidade (intensidade) do treino foi definida como sendo 80% da V4 (velocidade na qual a lactacidemia atinge 4mmol/L). Adicionalmente, no último mês de treinamento, foi instituído, uma vez por semana, exercício com velocidades variáveis, chamado fartlek. Após 90 dias de treinamento, a concentração plasmática de cortisol elevou-se e após o teste de esforço (20min), houve aumento da glicemia. Este resultado reflete a possibilidade de adaptação ao treinamento. Conclui-se que o cortisol plasmático pode ser utilizado como ferramenta na avaliação de um programa de treinamento em equinos.Cortisol and glucose responses were evaluated in 12 Arabian (PSA) horses submitted to a detraining period of eight months (T0) and to 90 days of aerobic training (T90). For the evaluation of the effect of training, a standardized incremental exercise test in a treadmill was used. Fifteen seconds before the ending of each effort step, blood samples were collected. The speed (intensity) of the training was defined as being 80% of the V4 (speed at which the blood lactate concentration reaches 4mmol/L). Additionally, in the last month of training, velocity play, a type of exercise with varying velocities called fartlek was instituted, once a week. Results showed that after 90 days of training, the plasmatic concentrations of cortisol and glucose increased when compared to the untrained horses. This result reflects the possibility of adaptation to the training. The blood cortisol levels may be used as a tool for the evaluation of a training program in horses

Injeção epidural preventiva de xilazina ou amitraz em eqüinos: efeitos clínicos e comportamentais

A xilazina é o fármaco agonista adrenérgico α2 mais utilizado pela via epidural de eqüinos e sabe-se que o amitraz tem ação sobre esses receptores. Assim, foram avaliados os efeitos clínicos e comportamentais causados pela injeção epidural de 0,17mg kg-1 de xilazina (GX) ou de 0,1mg kg-1 de amitraz diluído em emulsão lipídica (GA) durante 24 horas, em doze eqüinos. A freqüência cardíaca e a altura de cabeça mantiveram-se inalteradas; a freqüência respiratória aumentou de T105 a T360 no GX; a temperatura retal elevou-se de T120 a T720 em GA e de T360 a T720 em GX. Não houve diferença no tempo de latência para urinar ou defecar em ambos os grupos. em relação às alterações comportamentais, o amitraz provocou sedação (50%), ptose labial (33,4%) e palpebral (16,7%), enquanto que a xilazina promoveu ataxia (50%), sudorese perineal (33,4%), ptose palpebral (16,6%) e relaxamento do esfíncter anal (16,6%). Considera-se segura a injeção epidural de xilazina ou amitraz em eqüinos, pois as alterações clínicas e comportamentais promovidas são leves e não limitam seu uso.Xylazine is the α2-adrenergic agonist more employed by epidural route in horses and it is known that amitraz acts on these receptors. So, clinical and behavioral effects caused by epidural injection of 0.17mg kg-1 xylazine (GX) or 0.1mg.kg-1 amitraz diluted in lipidic emulsion (GA) were evaluated in 12 horses. Heart rate and height of the head didn't change; respiratory rate increased from T105 to T360 in GX; rectal temperature increased from T120 to T720 in GA and from T360 to T720 in GX. There is no difference in latency to urine or defecate in both groups. Concerning behavioral changes, amitraz promoted sedation (50%), lip (33.4%) and eye (16.6%) dropping, while xylazine caused ataxia (50%), perineal sweating (33.4%), eye dropping (16.6%) and anal sphincter relaxation (16.6%). So, epidural injection of xylazine or amitraz was considered safe because the clinical and behavioral changes observed are subtle and don't limit its application.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP