ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2013
The HIV antiretroviral drug efavirenz has LSD-like properties.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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Who cites it
39 citing papers in PubMed, 85 citations in OpenAlex.
- Prevalence, patterns, and associated factors of psychoactive substance use among people living with HIV in Lomé, Togo : a cross-sectional study.BMC public health · 2026Article
- Distinct biochemical phenotypes of HIV exposed infants driven by antiviral medication.medRxiv : the preprint server for health sciences · 2026Article
- Mind the gap! Addressing unresolved aspects of abuse potential evaluation and scheduling of classic and novel psychedelic drugs.Journal of psychopharmacology (Oxford, England) · 2026Review
- Allosteric modulation of the solute carrier transporter SLC39A8 potentiates manganese and cadmium uptake.The Journal of clinical investigation · 2025Article
- Involvement of virus infections and antiviral agents in schizophrenia.Psychological medicine · 2025Review
- Oral Administration of Efavirenz Dysregulates thePharmaceuticals (Basel, Switzerland) · 2024Article
- The Impact of Drugs and Substance Abuse on Viral Pathogenesis-A South African Perspective.Viruses · 2024Review
- Efavirenz: History, Development and Future.Biomolecules · 2022Review
- Molecular targets of psychedelic-induced plasticity.Journal of neurochemistry · 2022Review
- Prolonged efavirenz exposure reduces peripheral oxytocin and vasopressin comparable to known drugs of addiction in male Sprague Dawley rats.IBRO neuroscience reports · 2021Article
- HIV-Associated Apathy/Depression and Neurocognitive Impairments Reflect Persistent Dopamine Deficits.Cells · 2021Review
- Psychedelic-like Properties of Quipazine and Its Structural Analogues in Mice.ACS chemical neuroscience · 2021Article
- Evaluating Neurodevelopmental Consequences of Perinatal Exposure to Antiretroviral Drugs: Current Challenges and New Approaches.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2021Review
- Uptake of antiretroviral treatment and viral suppression among men who have sex with men and transgender women in sub-Saharan Africa in an observational cohort study: HPTN 075.International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases · 2021Observational
- Inflammatory Mechanisms and Cascades Contributing to Neurocognitive Impairment in HIV/AIDS.Current topics in behavioral neurosciences · 2021Article
- Bidirectional Associations among Nicotine and Tobacco Smoke, NeuroHIV, and Antiretroviral Therapy.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2020Review
- HIV Neuropathogenesis in the Presence of a Disrupted Dopamine System.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2020Review
- Therapeutic activities of naringenin on efavirenz-induced sleep-like disorder in the midbrain of white albino mice.Iranian journal of basic medical sciences · 2020Article
- Neuropsychiatric Effects of Antiviral Drugs.Cureus · 2020Review
- Risk and protective factors forAddictive behaviors reports · 2020Article
Corrections and comments
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Authors and funding
11 authors at 5 institutions in 1 country.
Funding
Abstract
Anecdotal reports have surfaced concerning misuse of the HIV antiretroviral medication efavirenz ((4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one) by HIV patients and non-infected teens who crush the pills and smoke the powder for its psychoactive effects. Molecular profiling of the receptor pharmacology of efavirenz pinpointed interactions with multiple established sites of action for other known drugs of abuse including catecholamine and indolamine transporters, and GABAA and 5-HT(2A) receptors. In rodents, interaction with the 5-HT(2A) receptor, a primary site of action of lysergic acid diethylamine (LSD), appears to dominate efavirenz's behavioral profile. Both LSD and efavirenz reduce ambulation in a novel open-field environment. Efavirenz occasions drug-lever responding in rats discriminating LSD from saline, and this effect is abolished by selective blockade of the 5-HT(2A) receptor. Similar to LSD, efavirenz induces head-twitch responses in wild-type, but not in 5-HT(2A)-knockout, mice. Despite having GABAA-potentiating effects (like benzodiazepines and barbiturates), and interactions with dopamine transporter, serotonin transporter, and vesicular monoamine transporter 2 (like cocaine and methamphetamine), efavirenz fails to maintain responding in rats that self-administer cocaine, and it fails to produce a conditioned place preference. Although its molecular pharmacology is multifarious, efavirenz's prevailing behavioral effect in rodents is consistent with LSD-like activity mediated via the 5-HT(2A) receptor. This finding correlates, in part, with the subjective experiences in humans who abuse efavirenz and with specific dose-dependent adverse neuropsychiatric events, such as hallucinations and night terrors, reported by HIV patients taking it as a medication.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.