PMID- 33155233
OWN - NLM
STAT- MEDLINE
DCOM- 20210629
LR  - 20210629
IS  - 2284-0729 (Electronic)
IS  - 1128-3602 (Linking)
VI  - 24
IP  - 20
DP  - 2020 Oct
TI  - Efavirenz as a psychotropic drug.
PG  - 10729-10735
LID - 23433 [pii]
LID - 10.26355/eurrev_202010_23433 [doi]
AB  - OBJECTIVE: 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. 
      MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.
FAU - Zareifopoulos, N
AU  - Zareifopoulos N
AD  - Emergency Department, University Hospital of Patras, Patras, Greece. 
      nizareifopoulos@gmail.com.
FAU - Lagadinou, M
AU  - Lagadinou M
FAU - Karela, A
AU  - Karela A
FAU - Pouliasi, F
AU  - Pouliasi F
FAU - Economou, I
AU  - Economou I
FAU - Tsigkou, A
AU  - Tsigkou A
FAU - Velissaris, D
AU  - Velissaris D
LA  - eng
PT  - Journal Article
PT  - Review
PL  - Italy
TA  - Eur Rev Med Pharmacol Sci
JT  - European review for medical and pharmacological sciences
JID - 9717360
RN  - 0 (Alkynes)
RN  - 0 (Benzoxazines)
RN  - 0 (Cyclopropanes)
RN  - 0 (Psychotropic Drugs)
RN  - JE6H2O27P8 (efavirenz)
SB  - IM
MH  - Alkynes/*therapeutic use
MH  - Benzoxazines/*therapeutic use
MH  - Cyclopropanes/*therapeutic use
MH  - Humans
MH  - Psychotic Disorders/*drug therapy
MH  - Psychotropic Drugs/*therapeutic use
EDAT- 2020/11/07 06:00
MHDA- 2021/06/30 06:00
CRDT- 2020/11/06 06:02
PHST- 2020/11/06 06:02 [entrez]
PHST- 2020/11/07 06:00 [pubmed]
PHST- 2021/06/30 06:00 [medline]
AID - 23433 [pii]
AID - 10.26355/eurrev_202010_23433 [doi]
PST - ppublish
SO  - Eur Rev Med Pharmacol Sci. 2020 Oct;24(20):10729-10735. doi: 
      10.26355/eurrev_202010_23433.