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酮洛芬在儿科患者中的药代动力学、疗效和耐受性。

Ketoprofen pharmacokinetics, efficacy, and tolerability in pediatric patients.

机构信息

Department of Anesthesiology and Intensive Care, Kuopio University Hospital, University of Eastern Finland, Kuopio, Finland.

出版信息

Paediatr Drugs. 2010 Oct 1;12(5):313-29. doi: 10.2165/11534910-000000000-00000.

DOI:10.2165/11534910-000000000-00000
PMID:20799760
Abstract

The NSAID ketoprofen is used widely in the management of inflammatory and musculoskeletal conditions, pain, and fever in children and adults. Pharmacokinetic studies show that drug exposure after a single intravenous dose is similar in children and adults (after dose normalization), and thus similar mg/kg bodyweight dosing may be used in children and adults. Ketoprofen crosses the blood-brain barrier and therefore has the potential to cause central analgesic effects. Ketoprofen has been investigated in children for the treatment of pain and fever, peri- and postoperative pain, and inflammatory pain conditions. The results of four clinical trials in febrile conditions with the oral syrup formulation indicate that ketoprofen is as effective as acetaminophen (paracetamol) and ibuprofen, allowing children to rapidly return to daily activities with improvements in sleep quality and appetite. Studies of ketoprofen in the management of postoperative pain indicate that ketoprofen is a highly effective analgesic when administered perioperatively for a variety of surgical types, by a variety of routes, and whether given preoperatively or postoperatively. For adenoidectomy, intravenous ketoprofen provided superior postoperative analgesic efficacy compared with placebo. Analgesic efficacy was similar with intravenous, intramuscular, or rectal routes of administration, but oral administration just before surgery was inferior to intravenous administration in this setting. In patients undergoing a tonsillectomy, intravenous ketoprofen was superior to intravenous tramadol in terms of the need for postoperative rescue analgesia, but did not remove the need for rescue opioid therapy in these patients. Intravenous ketoprofen had superior postoperative analgesic efficacy to placebo when given as an adjuvant to epidural sufentanil analgesia after major surgery. Oral ketoprofen has shown efficacy in the treatment of juvenile rheumatoid arthritis. Ketoprofen is generally well tolerated in pediatric patients. Most of the adverse events reported are mild and transient, and are similar to those observed with other NSAIDs. Long-term tolerability has not yet been fully established in children, but data from three studies in >900 children indicate that oral ketoprofen is well tolerated when administered for up to 3 weeks after surgery. In conclusion, ketoprofen is effective and well tolerated in children for the control of post-surgical pain and for the control of pain and fever in inflammatory conditions.

摘要

非甾体抗炎药酮洛芬广泛用于治疗儿童和成人的炎症和肌肉骨骼疾病、疼痛和发热。药代动力学研究表明,单次静脉给药后,儿童和成人的药物暴露相似(在剂量归一化后),因此儿童和成人可能使用相似的毫克/公斤体重剂量。酮洛芬能穿过血脑屏障,因此具有潜在的中枢镇痛作用。酮洛芬已在儿童中用于治疗疼痛和发热、围手术期疼痛和炎症性疼痛疾病。口服糖浆制剂治疗发热疾病的四项临床试验结果表明,酮洛芬与对乙酰氨基酚(扑热息痛)和布洛芬一样有效,使儿童能够迅速恢复日常活动,改善睡眠质量和食欲。酮洛芬治疗术后疼痛的研究表明,酮洛芬在围手术期用于多种手术类型时是一种非常有效的镇痛剂,通过多种途径,无论是术前还是术后给予,都具有很好的镇痛效果。对于腺样体切除术,静脉注射酮洛芬与安慰剂相比提供了更好的术后镇痛效果。静脉、肌肉或直肠给药途径的镇痛效果相似,但在这种情况下,手术前口服给药不如静脉给药有效。在接受扁桃体切除术的患者中,静脉注射酮洛芬在需要术后解救性镇痛方面优于静脉注射曲马多,但不能消除这些患者对解救性阿片类药物治疗的需求。静脉注射酮洛芬作为硬膜外舒芬太尼镇痛后辅助药物用于大手术后,具有较好的术后镇痛效果。口服酮洛芬在治疗青少年类风湿性关节炎方面显示出疗效。酮洛芬在儿科患者中通常具有良好的耐受性。大多数报告的不良反应是轻微和短暂的,与其他 NSAIDs 观察到的相似。在儿童中尚未充分确定长期耐受性,但三项研究中超过 900 名儿童的数据表明,手术后口服酮洛芬长达 3 周时耐受性良好。总之,酮洛芬在儿童中有效且耐受良好,可用于控制术后疼痛和控制炎症性疾病中的疼痛和发热。

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本文引用的文献

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Ketoprofen versus paracetamol (acetaminophen) or ibuprofen in the management of fever: results of two randomized, double-blind, double-dummy, parallel-group, repeated-dose, multicentre, phase III studies in children.酮洛芬对比扑热息痛(对乙酰氨基酚)或布洛芬用于儿童发热的管理:两项随机、双盲、双模拟、平行分组、重复剂量、多中心、III 期研究的结果。
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Dose-finding studies of ketoprofen in the management of fever in children: report on two randomized, single-blind, comparator-controlled, single-dose, multicentre, phase II studies.两随机、单盲、对照药物比较、单次剂量、多中心、Ⅱ期临床试验中酮洛芬治疗儿童发热的剂量探索研究。
Clin Drug Investig. 2010;30(4):251-8. doi: 10.2165/11534520-000000000-00000.
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Can J Anaesth. 2024 Aug;71(8):1103-1116. doi: 10.1007/s12630-024-02760-y. Epub 2024 Apr 15.
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Efficacy and Safety of NSAIDs in Infants: A Comprehensive Review of the Literature of the Past 20 Years.非甾体抗炎药(NSAIDs)在婴儿中的疗效和安全性:对过去 20 年文献的综合回顾。
Paediatr Drugs. 2022 Nov;24(6):603-655. doi: 10.1007/s40272-022-00514-1. Epub 2022 Sep 2.
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