静脉注射对乙酰氨基酚用于术后镇痛的最佳时机。
Optimal Timing of Intravenous Acetaminophen Administration for Postoperative Analgesia.
机构信息
Department of Perioperative Medicine, Division of Anesthesiology, Showa University School of Dentistry, Japan.
Department of Pharmacology, Toxicology and Therapeutics, Division of Pharmacokinetics and Pharmacodynamics, Showa University School of Pharmacy, Japan.
出版信息
Anesth Prog. 2022 Jun 1;69(2):3-10. doi: 10.2344/anpr-69-02-05.
OBJECTIVE
Acetaminophen (APAP) is widely used as an analgesic for postoperative pain relief. However, the pharmacokinetic-pharmacodynamic (PK-PD) properties of intravenous APAP administration remain unclear. We developed a PK-PD model in adult volunteers.
METHODS
APAP (1 g) was intravenously administered to 15 healthy volunteers. The pain equivalent current (PEC) was then measured using the pulse current, corresponding to the quantitative value of pain perception. The PK model was developed using a 2-compartment model, and the PD model was developed using a linear model and an effect compartment model.
RESULTS
APAP plasma concentration peaked just administration, whereas PEC significantly increased at 90 minutes and lasted through the experimental period (300 minutes). APAP plasma concentrations and PEC were processed for use in the PK-PD model. The developed PK-PD model delineates the analgesic effect profile, which peaked at 188 minutes and lasted until 327 minutes.
CONCLUSION
We developed the PK/PD model for APAP administered intravenously. The analgesic effect can be expected ∼90 minutes after administration and to last >5 hours. It is suggested that APAP be administered ∼90 minutes prior to the onset of anticipated postoperative pain.
目的
醋氨酚（APAP）被广泛用作术后镇痛的镇痛药。然而，静脉内给予 APAP 的药代动力学-药效学（PK-PD）特性尚不清楚。我们在成年志愿者中开发了 PK-PD 模型。
方法
将 15 名健康志愿者静脉内给予 1gAPAP。然后使用脉冲电流测量疼痛等效电流（PEC），与疼痛感知的定量值相对应。PK 模型采用 2 隔室模型开发，PD 模型采用线性模型和效应隔室模型开发。
结果
APAP 血浆浓度在给药时达到峰值，而 PEC 在 90 分钟时显著增加，并持续整个实验期（300 分钟）。APAP 血浆浓度和 PEC 用于 PK-PD 模型处理。开发的 PK-PD 模型描绘了镇痛作用谱，其在 188 分钟时达到峰值，并持续到 327 分钟。
结论
我们开发了静脉内给予 APAP 的 PK/PD 模型。预期在给药后约 90 分钟开始产生镇痛作用，持续时间超过 5 小时。建议在预期术后疼痛发作前约 90 分钟给予 APAP。
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