局部麻醉药的安全性及其新剂型研究进展  

Safety of local anesthetics and the research progress of their new dosage forms

作　　者：朱愿超[1] 张亚同[1] 梁良[1] Zhu Yuanchao;Zhang Yatong;Liang Liang(Department of Pharmacy,Beijing Hospital,National Center of Gerontology,Institute of Geriatric Medicine,Chinese Academy of Medical Sciences,Beijing Key Laboratory of Assessment of Clinical Drugs Risk and Individual Application(Beijing Hospital),Beijing 100730,China)

机构地区：[1]北京医院药学部/国家老年医学中心/中国医学科学院老年医学研究院/北京市药物临床风险与个体化应用评价重点实验室(北京医院),北京100730

出　　处：《药物不良反应杂志》2024年第2期111-117,共7页Adverse Drug Reactions Journal

基　　金：中央高水平医院临床科研业务费(BJ-2022-173);科技部国家重点研发计划(2020YFC2009001)。

摘　　要：局部麻醉(局麻)药是一类能在用药局部可逆性地阻断感觉神经冲动发生与传导的药品,临床上广泛用于皮肤黏膜麻醉、周围神经阻滞麻醉、脊髓神经麻醉和治疗慢性疼痛等。局麻药的不良反应主要包括过敏反应、心脏毒性和神经毒性。局麻药的新剂型包括经皮给药剂型和缓控释剂型。经皮给药剂型的优点是实现表面局麻,避免肝脏首过效应,减少注射麻醉对患者局部的损伤和刺激,提高患者的耐受性;缓控释剂型可维持较长效的麻醉效果,避免因局麻药吸收过快产生血药浓度过高,从而减轻药物不良反应。Local anesthetics are a class of medications that can reversibly block the occurrence and transmission of sensory nerve impulses in the local administration area,which are widely used in clinic for skin and mucous membrane anesthesia,peripheral nerve block anesthesia,spinal nerve anesthesia,and the treatment of chronic pain.The adverse reactions of local anesthetics mainly include allergic reactions,cardio⁃toxicity,and neurotoxicity.The new dosage forms of local anesthetics include cutaneous administration and sustained⁃release formulations.The advantage of cutaneous administration is to achieve surface local anesthesia,avoid liver first pass effect,reduce local damage and stimulation caused by injection anesthesia,and improve patient tolerance.The sustained⁃release dosage form can help maintain a longer lasting anes⁃thetic effect,avoid excessive blood drug concentration caused by rapid absorption of local anesthetic drugs,and thus reduce adverse drug reactions.

关 键 词：麻醉药 局部 经皮给药 剂型 安全性 药物相关副作用和不良反应 

分 类 号：R971.2[医药卫生—药品]