Emergency Department, University Hospital of Patras, Patras, Greece.
Eur Rev Med Pharmacol Sci. 2020 Oct;24(20):10729-10735. doi: 10.26355/eurrev_202010_23433.
Antiretroviral drugs are the mainstay of treatment for human immunodeficiency virus (HIV) infection. Lifelong highly active antiretroviral therapy (HAART) is indicated to prevent disease progression to acquired immunodeficiency syndrome (AIDS). Efavirenz was a first-line component of HAART across the world for many years. The purpose of this article is to review the psychotropic properties of efavirenz, which are the most important adverse events associated with the drug and commonly result in treatment discontinuation.
A PubMed search was conducted using efavirenz as a search term, which returned 4655 results. Titles and abstracts of articles were screened for relevance, and all relevant articles published in English were included in the narrative review.
Acute exposure to efavirenz may cause profound perceptual disturbances (delusions and hallucinations) whereas chronic exposure may be associated with abnormal dreams and other sleep disturbances, anxiety, depressed mood and suicidality. It may also be abused as a hallucinogen, especially in individuals with a history of poly-substance abuse. Recent research indicates that efavirenz directly affects monoaminergic neurotransmission and may partially substitute for psychedelic drugs, such as lysergic acid diethylamide (LSD). Efavirenz acts as a serotonin 5-HT2A receptor antagonist, a serotonin-dopamine reuptake inhibitor, an inhibitor of monoamine oxidase (MAO) and a vesicular monoamine transporter 2 (VMAT2) inhibitor, which are mechanisms common with many psychotropic drugs. Efavirenz interacts with many of the same molecular targets as the empathogen methylendioxymethamphetamine (MDMA), but the effects of the 2 drugs may differ.
The exact mechanism of action of efavirenz as a psychotropic drug remains unclear and future studies should focus on evaluating whether prolonged exposure could lead to irreversible side effects.
抗逆转录病毒药物是治疗人类免疫缺陷病毒（HIV）感染的主要方法。终身高效抗逆转录病毒疗法（HAART）可预防疾病进展为获得性免疫缺陷综合征（AIDS）。依非韦伦多年来一直是全球 HAART 的一线药物。本文旨在回顾依非韦伦的精神活性特性，这是与该药物最相关的重要不良反应，通常导致治疗中断。
使用依非韦伦作为搜索词在 PubMed 上进行搜索，返回了 4655 个结果。筛选文章的标题和摘要以确定相关性，并将所有以英文发表的相关文章纳入叙述性综述。
依非韦伦的急性暴露可能导致深刻的感知障碍（妄想和幻觉），而慢性暴露可能与异常梦境和其他睡眠障碍、焦虑、抑郁情绪和自杀意念有关。它也可能被滥用于致幻剂，尤其是在有多种药物滥用史的个体中。最近的研究表明，依非韦伦直接影响单胺能神经递质传递，并可能部分替代迷幻药物，如麦角酸二乙酰胺（LSD）。依非韦伦作为 5-羟色胺 5-HT2A 受体拮抗剂、5-羟色胺-多巴胺再摄取抑制剂、单胺氧化酶（MAO）抑制剂和囊泡单胺转运体 2（VMAT2）抑制剂，其作用机制与许多精神药物相同。依非韦伦与致欣快剂亚甲二氧基甲基苯丙胺（MDMA）有许多相同的分子靶点相互作用，但这两种药物的作用可能不同。
依非韦伦作为精神药物的确切作用机制仍不清楚，未来的研究应重点评估长期暴露是否会导致不可逆转的副作用。
