Richards John R, Richards Irina N, Ozery Gal, Derlet Robert W
Department of Emergency Medicine, UC Davis Medical Center, Sacramento, California 95817, USA.
J Emerg Med. 2011 Oct;41(4):389-96. doi: 10.1016/j.jemermed.2010.07.005. Epub 2010 Sep 15.
Patients with acute and chronic pain syndromes such as migraine headache, fibromyalgia, and sickle cell disease represent a significant portion of emergency department (ED) visits. Certain patients may have tolerance to opioid analgesics and often require large doses and prolonged time in the ED to achieve satisfactory pain mitigation. Droperidol is a unique drug that has been successfully used not only as an analgesic adjuvant for the past 30 years, but also for treatment of nausea/vomiting, psychosis, agitation, sedation, and vertigo.
In this review, we examine the evidence supporting the use of droperidol for analgesia, adverse side effects, and controversial United States (US) Food and Drug Administration (FDA) black box warning.
Droperidol has myriad pharmacologic properties that may explain its efficacy as an analgesic, including: dopamine D2 antagonist, dose-dependent GABA agonist/antagonist, α2 adrenoreceptor agonist, serotonin antagonist, histamine antagonist, muscarinic and nicotinic cholinergic antagonist, anticholinesterase activity, sodium channel blockade similar to lidocaine, and μ opiate receptor potentiation.
Droperidol is an important adjuvant for patients who are tolerant to opioid analgesics. The FDA black box warning does not apply to doses below 2.5 mg.
患有急性和慢性疼痛综合征（如偏头痛、纤维肌痛和镰状细胞病）的患者占急诊就诊人数的很大一部分。某些患者可能对阿片类镇痛药产生耐受性，在急诊室通常需要大剂量且长时间用药才能实现满意的疼痛缓解。氟哌利多是一种独特的药物，在过去30年中不仅成功用作镇痛辅助药物，还用于治疗恶心/呕吐、精神病、躁动、镇静和眩晕。
在本综述中，我们研究支持使用氟哌利多进行镇痛、不良反应以及美国食品药品监督管理局（FDA）黑框警告存在争议的证据。
氟哌利多具有多种药理特性，这可能解释了其作为镇痛药的疗效，包括：多巴胺D2拮抗剂、剂量依赖性γ-氨基丁酸（GABA）激动剂/拮抗剂、α2肾上腺素能受体激动剂、5-羟色胺拮抗剂、组胺拮抗剂、毒蕈碱和烟碱胆碱能拮抗剂、抗胆碱酯酶活性、类似于利多卡因的钠通道阻滞以及μ阿片受体增强作用。
氟哌利多是对阿片类镇痛药产生耐受性患者的重要辅助药物。FDA的黑框警告不适用于低于2.5毫克的剂量。
