|Summary sheet: Efavirenz|
|Common names||Efavirenz, Sustiva|
|Routes of Administration|
|Selective serotonin re-uptake inhibitors|
|Serotonin-norepinephrine reuptake inhibitors|
Efavirenz (sold by the brand name Sustiva) is an antiretroviral medication used in the treatment and prevention of HIV/AIDS. It is notable for being able to produce psychedelic and hallucinogenic effects despite possessing an extremely novel pharmacological profile and chemical structure not shared with any other psychedelic substance.
Efavirenz was approved for medical use in the United States in 1998. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.
- 1 Chemistry
- 2 Pharmacology
- 3 Subjective effects
- 4 Toxicity and harm potential
- 5 Legal status
- 6 See also
- 7 External links
- 8 References
Unlike most psychedelics, efavirenz is not a tryptamine, phenethylamine or lysergamide. Efavirenz is classified as a benzoxazine and has several different moieties which give it a unique pharmacological profile. On the two position of the benzoxazine ring, efavirenz has a ketone attached. Efavirenz also has a trifluoromethyl group as well as a cyclopropane ring.
Efavirenz is a white to slightly pink crystalline powder with a molecular mass of 315.68 g/mol. It is practically insoluble in water (<10 µg/mL).
Pharmacologically, efavirenz is primarily classified as a non-nucleotide reverse transcriptase inhibitor, or NNRTI. Reverse transcriptase is an enzyme found in several viral species that is a type of DNA polymerase and nuclease that allows viruses like hepatitis and human immunodeficiency virus to transcribe viral RNA into DNA. Efavirenz is considered a non-nucleotide reverse transcriptase inhibitor because it does not have a structure based off of a nucleotide.
Unlike most non-nucleotide reverse transcriptase inhibitors, efavirenz is also a 5-HT2A partial agonist, similar to LSD. Additionally, efavirenz is a serotonin and dopamine reuptake inhibitor and a vesicular monoamine transporter 2 inhibitor. Efavirenz also acts as a GABAA positive allosteric modulator, similar to benzodiazepines and barbiturates. Efavirenz has a bioavailability of about 40-45% when it is taken on an empty stomach.
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. These effects should be taken with a grain of salt and will rarely (if ever) occur all at once, but heavier doses will increase the chances of inducing a full range of effects. Likewise, adverse effects become much more likely on higher doses and may include serious injury or death.
- Drifting (melting, breathing, morphing and flowing)
- After images
- Colour replacement
- Colour shifting
- Scenery slicing
- Symmetrical texture repetition
- Tracers - This is considered the most common visual effect of efavirenz.
The geometry found within efavirenz is generally extremely mild, and for many users, it may not happen at all.
Toxicity and harm potential
Efavirenz has a low toxicity relative to dose. Like many HIV medications, efavirenz may cause liver toxicity at high doses or after chronic use.
It is strongly recommended that one use harm reduction practices when using this drug.
Tolerance and addiction potential
Efavirenz is not known to be habit-forming. While developing a tolerance to efavirenz is extremely rare, abusing efavirenz may cause HIV to become resistant to the drug and increase the viral load in patients with HIV.
As efavirenz may cause hepatoxicity at high doses or after chronic use, it is not recommended to take this substance concurrently with other substances that may cause hepatoxicity. Efavirenz is an inducer of the CYP2B6 and CYP3A4 enzymes of the cytochrome P450 system, and as a result may change the metabolism of drugs metabolized by them. Consuming garlic may decrease serum levels of efavirenz.
Serotonin syndrome risk
Efavirenz is a weak serotonin reuptake inhibitor, so it is possible that combining heavy doses of efavirenz and the substances listed below may result in serotonin syndrome. Combinations with the following substances can cause dangerously high serotonin levels. Serotonin syndrome requires immediate medical attention and can be fatal if left untreated.
- MAOIs such as syrian rue, banisteriopsis caapi, 2C-T-7, αMT, phenelzine, selegiline, and moclobemide
- Serotonin releasers such as MDMA, 4-FA, methamphetamine, methylone and αMT
- Selective serotonin re-uptake inhibitors (SSRIs)
- Serotonin-norepinephrine reuptake inhibitors (SNRIs) such as tramadol and DXM
This legality section is a stub.
As such, it may contain incomplete or wrong information. You can help by expanding it.
Efavirenz is not known to be illegal in any jurisdictions, and is considered a prescription only medication.
- Efavirenz (Wikipedia)
- Efavirenz (Isomer Design)
- Getting High On HIV Medication (Hammilton Morris / YouTube)
- Efavirenz and the CNS: what we already know and questions that need to be answered. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/26203180
- Vrouenraets, S. M., Wit, F. W., Tongeren, J. V., & Lange, J. M. (2007). Efavirenz: a review. Expert Opinion on Pharmacotherapy, 8(6), 851-871. https://doi.org/10.1517/146565188.8.131.521
- "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
- Getting high on HIV drugs in S Africa. BBC News, 8 December 2008. Template:Webarchive
- 'No Turning Back': Teens Abuse HIV Drugs. ABC News, April 6, 2009. Template:Webarchive
- Getting High On HIV Medication Template:Webarchive Vice 7.04.2014.
- Neuropsychopharmacology | http://www.nature.com/npp/journal/v38/n12/full/npp2013135a.html
- Gillman, P. K. (2005). Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicity. British Journal of Anaesthesia, 95(4), 434-441. https://doi.org/10.1093/bja/aei210