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口服和复合静脉给予甘丙肽在山羊中的药代动力学特征和生理效应。

Pharmacokinetic profile and physiological effects of oral and compounded intravenous gabapentin in goats.

机构信息

Department of Specialty Medicine, Midwestern University Companion Animal Hospital, Glendale, AZ, USA.

Department of Specialty Medicine, Midwestern University Companion Animal Hospital, Glendale, AZ, USA.

出版信息

Vet Anaesth Analg. 2024 Sep-Oct;51(5):539-547. doi: 10.1016/j.vaa.2024.06.006. Epub 2024 Jun 18.

Abstract

OBJECTIVE

To determine the pharmacokinetics and physiological effects following oral and intravenous (IV) administration of gabapentin in goats.

STUDY DESIGN

Prospective, crossover study with a 3 week washout period between treatments.

ANIMALS

A total of eight healthy, client-owned, female goats.

METHODS

Gabapentin (10 mg kg) was administered to goats either orally or IV. Gabapentin concentrations were measured in serum samples collected 0-96 hours post-administration using liquid chromatography-quadrupole time-of-flight mass spectrometry. Heart rate, respiratory rate, blood pressure and temperature were recorded before and throughout the study. Correlations of the mean serum concentrations of gabapentin to those of each physiological parameter were determined using the Pearson method.

RESULTS

The mean and standard deviation of oral bioavailability for gabapentin was 60.9 ± 11.2%. Maximum serum concentration of gabapentin was lower following oral (1.19 ± 0.29 μg mL) than after IV administration (59.76 ± 14.38 μg mL, p < 0.0001). Half-lives were longer following PO (8.18 ± 0.57 hours) than after IV administration (1.79 ± 0.06 hours, p < 0.0001). Time to maximum concentration was 6.86 ± 2.27 hours following oral administration. Heart rate was inversely correlated with serum gabapentin concentrations. Slight ataxia was observed in three animals, and one became recumbent following IV gabapentin.

CONCLUSIONS AND CLINICAL RELEVANCE

Gabapentin is well-absorbed following oral administration to goats but yielded significantly lower serum concentrations than the IV route. The longer half-life of gabapentin following oral than after IV administration may result from prolonged absorption throughout the caprine gastrointestinal tract. IV gabapentin may cause slight ataxia in some goats.

摘要

目的

确定给山羊口服和静脉(IV)给予加巴喷丁后的药代动力学和生理效应。

研究设计

在治疗之间有 3 周洗脱期的前瞻性、交叉研究。

动物

总共 8 只健康的、客户拥有的、雌性山羊。

方法

给山羊口服或 IV 给予加巴喷丁(10 mg/kg)。给药后 0-96 小时采集血清样本,使用液相色谱-四极杆飞行时间质谱法测定血清中加巴喷丁的浓度。在研究开始前和整个研究过程中记录心率、呼吸频率、血压和体温。使用 Pearson 方法确定加巴喷丁的平均血清浓度与每个生理参数的相关性。

结果

口服生物利用度的平均值和标准差为 60.9 ± 11.2%。口服(1.19 ± 0.29 μg/ml)后加巴喷丁的最大血清浓度低于 IV 给药(59.76 ± 14.38 μg/ml,p<0.0001)。PO 后的半衰期较长(8.18 ± 0.57 小时)比 IV 给药后(1.79 ± 0.06 小时,p<0.0001)。口服后达到最大浓度的时间为 6.86 ± 2.27 小时。心率与血清加巴喷丁浓度呈负相关。3 只动物出现轻微的共济失调,1 只在 IV 给予加巴喷丁后变得卧倒。

结论和临床相关性

加巴喷丁口服给予山羊后吸收良好,但血清浓度明显低于 IV 途径。口服后加巴喷丁的半衰期长于 IV 给药,可能是由于整个山羊胃肠道的吸收时间延长。IV 给予加巴喷丁可能会导致一些山羊出现轻微的共济失调。

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