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Toxicity and Pharmacokinetic Studies of Lidocaine and Its Active Metabolite, Monoethylglycinexylidide, in Goat Kids

机译:利多卡因及其活性代谢产物一乙基甘氨糖苷对山羊儿童的毒性和药代动力学研究

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This study determined the convulsant plasma concentrations and pharmacokinetic parameters following cornual nerve block and compared the results to recommend a safe dose of lidocaine hydrochloride for goat kids. The plasma concentrations of lidocaine and monoethylglycinexylidide (MGX) were quantified using liquid chromatography-mass spectrometry. A total dose of 7 mg/kg body weight (BW) was tolerated and should therefore be safe for local and regional anesthesia in goat kids. The mean plasma concentration and mean total dose that produced convulsions in goat kids were 13.59 ± 2.34 μg/mL and 12.31 ± 1.42 mg/kg BW (mean ± S.D.), respectively. The absorption of lidocaine following subcutaneous administration was rapid with C max and T max of 2.12 ± 0.81 μg/mL and 0.33 ± 0.11 h, respectively. The elimination half-lives (t ?λz ) of lidocaine hydrochloride and MGX were 1.71 ± 0.51 h and 3.19 ± 1.21 h, respectively. Injection of 1% lidocaine hydrochloride (0.5 mL/site) was safe and effective in blocking the nerves supplying horn buds in goat kids.
机译:这项研究确定了角膜神经阻滞后惊厥的血浆浓度和药代动力学参数,并比较了结果,为山羊儿童推荐了安全剂量的盐酸利多卡因。使用液相色谱-质谱法定量测定利多卡因和单乙基甘氨糖苷(MGX)的血浆浓度。耐受的总剂量为7 mg / kg体重(BW),因此对于山羊孩子的局部和区域麻醉应该是安全的。在山羊儿童中引起惊厥的平均血浆浓度和平均总剂量分别为13.59±2.34μg/ mL和12.31±1.42 mg / kg BW(平均值±标准差)。皮下给药后利多卡因的吸收迅速,C max和T max分别为2.12±0.81μg/ mL和0.33±0.11 h。盐酸利多卡因和MGX的消除半衰期(tΔλz)分别为1.71±0.51 h和3.19±1.21 h。注射1%盐酸利多卡因(0.5毫升/部位)可安全有效地阻断山羊儿童提供角芽的神经。

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