Objective

To investigate the pharmacokinetics, efficacy and convulsive dose of articaine hydrochloride in goat kids.

Study design

Experimental prospective study.

Animals

A total of 18 (n = 6 animals per experiment) male Saanen goat kids (2–4 weeks old).

Methods

The study consisted of three experiments. The first determined the pharmacokinetics of articaine following intravenous administration of articaine hydrochloride (8 mg kg^–1). The second experiment investigated the anaesthetic efficacy and pharmacokinetics following cornual nerve block using 1.5% articaine hydrochloride. Anaesthesia of horn buds was evaluated using the response to pinprick test. Non-compartmental analysis was used. The final experiment determined the convulsive dose of articaine and its corresponding plasma concentration following intravenous infusion of articaine hydrochloride (4 mg kg^–1 minute^–1). Data are shown as mean ± standard deviation.

Results

The mean terminal half-life (t_1/2λz), mean volume of distribution at steady state (Vd_ss) and mean plasma clearance (CL) of articaine following intravenous administration were 0.66 hour, 3.81 L kg^–1 and 5.33 L hour^–1 kg^–1, respectively. After cornual nerve block, the mean maximum plasma concentration of articaine was 587 ng mL^–1 at 0.22 hour and its mean t_1/2λz was 1.26 hours. Anaesthesia of horn buds was observed within 4 minutes following cornual nerve block. The mean dose required to produce convulsions was 16.24 mg kg^–1 and mean convulsive plasma concentrations of articaine and articainic acid were 9905 and 1517 ng mL^–1, respectively.

Conclusions

Intravenous administration of 8 mg kg^–1 of articaine hydrochloride did not cause any adverse effects. Pharmacokinetic data suggest that articaine was rapidly eliminated and cleared. Cornual nerve block using 1.5% articaine hydrochloride alleviated the response to the acute nociceptive stimulus during disbudding.

Clinical relevance

Articaine hydrochloride appears to be a safe and effective local anaesthetic for disbudding in goat kids.

中文翻译：

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盐酸阿替卡因在山羊仔中的药代动力学、疗效及惊厥剂量

客观的

研究盐酸阿替卡因在山羊幼仔体内的药代动力学、疗效及惊厥剂量。

学习规划

实验性前瞻性研究。

动物

总共 18 个（ 每个实验n = 6 只动物）雄性 Saanen 山羊孩子（2-4 周大）。

方法

该研究包括三个实验。第一个确定了静脉注射盐酸阿替卡因 (8 mg kg ^–1 )后阿替卡因的药代动力学。第二个实验研究了使用 1.5% 盐酸阿替卡因进行角神经阻滞后的麻醉效果和药代动力学。使用对针刺试验的反应评价角芽的麻醉。使用非房室分析。最后的实验确定了静脉输注盐酸阿替卡因（4 mg kg ^–1分钟^–1）后阿替卡因的惊厥剂量及其相应的血浆浓度。数据显示为平均值±标准偏差。

结果

静脉给药后阿替卡因的平均终末半衰期 ( t _1/2λz )、稳态平均分布容积 (Vd _ss ) 和平均血浆清除率 (CL) 分别为 0.66 小时、3.81 L kg ^–1和 5.33 L/h ^–分别为¹ kg ^–1。角神经阻滞后，阿替卡因的平均最大血浆浓度在 0.22 小时为 587 ng mL ^–1，其平均t _1/2λz为 1.26 小时。在角神经阻滞后 4 分钟内观察到角芽的麻醉。产生惊厥所需的平均剂量为 16.24 mg kg ^–1阿替卡因和阿替卡因酸的平均惊厥血浆浓度分别为 9905 和 1517 ng mL ^–1。

结论

静脉注射 8 mg kg ^–1盐酸阿替卡因未引起任何不良反应。药代动力学数据表明阿替卡因被迅速消除和清除。使用 1.5% 盐酸阿替卡因的角神经阻滞减轻了脱芽期间对急性伤害性刺激的反应。

临床相关性

盐酸阿替卡因似乎是一种安全有效的局部麻醉剂，可用于山羊孩子的脱芽。