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临床药理学以及阿替卡因在局部和区域麻醉中的应用。

Clinical pharmacology and the use of articaine for local and regional anaesthesia.

作者信息

Vree Tom B, Gielen Mathieu J M

机构信息

Institute for Anaesthesia, University Medical Centre St Radboud, PO Box 9101, 6500HB Nijmegen, The Netherlands.

出版信息

Best Pract Res Clin Anaesthesiol. 2005 Jun;19(2):293-308. doi: 10.1016/j.bpa.2004.12.006.

Abstract

Quicker onset and shorter elimination time favours (+/-) articaine as a short-acting local anaesthetic for regional anaesthesia in day-case settings, e.g. arthroscopy (shoulder, knee), hand and foot surgery, and dentistry, because patients treated with articaine will be 'drug free' more quickly than those who receive other local anaesthetics. Articaine diffuses better through soft tissue and bone than other local anaesthetics. The concentration of articaine in the alveolus of a tooth in the upper jaw after extraction was about 100 times higher than that in systemic circulation. Articaine is metabolised via hydrolysis into articainic acid, 75% of which in turn is excreted as such and 25% in the glucuronidated form by the kidneys. The half-lives of elimination (t1/2alpha and t1/2beta) of articaine are 0.6 and 2.5 hours, whereas the apparent half-life of the metabolite articainic acid is 2.5 hours. Intrinsic half-lives of articainic acid are: t1/2alpha 12 minutes, and t1/2beta 64 minutes (1 hour). In dentistry, articaine is the drug of choice in the vast majority of literature. In other regional anaesthesia techniques (intravenous regional anaesthesia, epidural, spinal and plexus blocks) there are not enough data to prove that (+/-) articaine is safer and more effective than the short-acting local anaesthetics lidocaine, (+/-) prilocaine or (+/-) mepivacaine.

摘要

起效更快和消除时间更短使(±)阿替卡因成为日间手术环境中区域麻醉的短效局部麻醉剂的首选,例如关节镜检查(肩部、膝盖)、手足外科手术和牙科手术,因为使用阿替卡因治疗的患者比接受其他局部麻醉剂的患者更快“无药”。阿替卡因比其他局部麻醉剂在软组织和骨骼中扩散得更好。拔牙后上颌牙齿牙槽中的阿替卡因浓度比体循环中的浓度高约100倍。阿替卡因通过水解代谢为阿替卡因酸,其中75% 原样排泄,25% 以葡萄糖醛酸结合形式经肾脏排泄。阿替卡因的消除半衰期(t1/2α和t1/2β)分别为0.6小时和2.5小时,而代谢产物阿替卡因酸的表观半衰期为2.5小时。阿替卡因酸的固有半衰期为:t1/2α 12分钟,t1/2β 64分钟(1小时)。在牙科领域,在绝大多数文献中阿替卡因是首选药物。在其他区域麻醉技术(静脉区域麻醉、硬膜外麻醉、脊髓麻醉和神经丛阻滞)中,没有足够的数据证明(±)阿替卡因比短效局部麻醉剂利多卡因、(±)丙胺卡因或(±)甲哌卡因更安全、更有效。

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