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低剂量酮咯酸在术后牙科疼痛中的药代动力学和疗效。

Pharmacokinetics and efficacy of low-dose ketoprofen in postoperative dental pain.

机构信息

Department of Restorative Dentistry, University of Newcastle upon Tyne, Newcastle upon Tyne, England.

出版信息

Clin Drug Investig. 1998;15(4):279-84. doi: 10.2165/00044011-199815040-00003.

DOI:10.2165/00044011-199815040-00003
PMID:18370482
Abstract

A double-blind, randomised trial was carried out to investigate the relationship between efficacy and various pharmacokinetic variables after single doses of racemic ketoprofen 12.5 and 25mg in patients with postoperative pain after third molar surgery over a 4-hour investigation period. Serial venous blood samples were obtained at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3 and 4 hours after administration for subsequent determination of R(-) and S(+) ketoprofen. The relationship between the R(-) and S(+) ketoprofen concentrations and pain experience was summarised for each patient by the slope of the regression line for that individual. There was no significant difference (p > 0.05) between the two doses of ketoprofen for any of the efficacy measures. Peak plasma concentrations of both R(-) and S(+) ketoprofen were observed between 60 and 90 minutes after dosage. A significant negative correlation (p < 0.002) was observed between the decrease in pain scores and plasma concentrations of both R(-) and S(+) ketoprofen after each dose. However, the amount of variability in each patient's response makes it difficult to identify a causal relationship between these parameters. Low doses of ketoprofen provide satisfactory pain relief in the early postoperative period after third molar surgery. Efficacy of this analgesic does not appear to be dose related or directly related to plasma concentrations of either R(-) or S(+) enantiomers.

摘要

一项双盲、随机试验研究了单剂量消旋酮洛芬 12.5 和 25mg 后与术后 3 小时内各种药代动力学变量与疗效之间的关系,患者为接受下颌第三磨牙拔除术后的疼痛。在 4 小时的研究期间,连续采集静脉血样,在给药后 0、0.25、0.5、0.75、1、1.5、2、3 和 4 小时进行测定,以测定 R(-)和 S(+)酮洛芬。通过个体的回归线斜率,总结每位患者 R(-)和 S(+)酮洛芬浓度与疼痛体验之间的关系。两种剂量的酮洛芬在任何疗效指标上均无显著差异(p > 0.05)。R(-)和 S(+)酮洛芬的血浆峰浓度均在剂量后 60-90 分钟观察到。在每次剂量后,疼痛评分的下降与 R(-)和 S(+)酮洛芬的血浆浓度呈显著负相关(p < 0.002)。然而,每位患者的反应存在大量差异,使得很难确定这些参数之间的因果关系。低剂量的酮洛芬在第三磨牙拔除术后的早期提供了令人满意的疼痛缓解。这种镇痛剂的疗效似乎与剂量无关,也与 R(-)或 S(+)对映体的血浆浓度无关。

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Sci Rep. 2017 Aug 21;7(1):8885. doi: 10.1038/s41598-017-09406-8.
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Diclofenac and ketoprofen liver toxicity in rat.双氯芬酸和酮洛芬对大鼠的肝脏毒性
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Pain-mediated altered absorption and metabolism of ibuprofen: an explanation for decreased serum enantiomer concentration after dental surgery.

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