Efavirenz

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Efavirenz (also known by the brand name Sustiva) is a non-nucleotide reverse transcriptase inhibitor used in the treatment and prevention of human immunodeficiency virus infections type 1 (HIV-1). Efavirenz is notable for having a strange array of effects, many resembling psychedelics, as well as an extremely unique pharmacological profile and structure.

Efavirenz
Chemical Nomenclature
Common names	Efavirenz, Sustiva
Systematic name	(4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one
Class Membership
Psychoactive class	Psychedelic
Chemical class	Benzoxazine
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Smoked Dosage Bioavailability 50% Common 600 - 1800 mg Duration Onset 1 - 5 minutes Peak 1 - 2 hours After effects 6 - 12 hours DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Interactions
MAOIs
Serotonin releasers
SSRIs
5-HTP

Summary sheet: Efavirenz

Chemistry

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. The empirical formula of efavirenz is C₁₄H₉ClF₃NO₂ and has a molar mass of 315.675 grams per mole.

Pharmacology

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.

Unlike most non-nucleotide reverse transcriptase inhibitors, efavirenz is also a 5-HT_2A 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 GABA_A positive allosteric modulator, similar to benzodiazepines and barbiturates. Efavirenz has a bioavailability of about 40-45% when it is taken on an empty stomach.

Efavirenz is known to cause a false-positive for cannabis on some urine tests.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

• Physical euphoria - This effect is generally quite mild.
• Difficulty urinating
• Nausea
• Dizziness
• Headaches
• Spontaneous tactile sensations
• Stimulation
• Appetite suppression

Cognitive effects

• Anxiety
• Psychosis - At very high doses, efavirenz may cause a psychotic state.
• Unity and interconnectedness
• Confusion
• Introspection
• Dream potentiation - At non-recreational doses, efavirenz often induces strange dreams.

Visual effects

Enhancements

• Colour enhancement
• Pattern recognition enhancement
• Visual acuity enhancement

Distortions

• Drifting (melting, breathing, morphing and flowing)
• After images
• Colour replacement
• Colour shifting
• Recursion
• Scenery slicing
• Symmetrical texture repetition
• Tracers

Hallucinatory states

• Transformations
• Internal hallucinations (autonomous entities; settings, sceneries, and landscapes; alterations in perspective and scenarios and plots)
• External hallucinations (autonomous entities; settings, sceneries, and landscapes; alterations in perspective and scenarios and plots)

Auditory effects

• Enhancements
• Distortions
• Hallucinations

Toxicity and harm potential

Methadone has a moderate 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.

Dangerous interactions

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 banisteriopsis caapi, syrian rue, phenelzine, selegiline, and moclobemide.
• Serotonin releasers - Such as MDMA, 4-FA, methamphetamine, methylone and αMT.
• SSRIs - Such as citalopram and sertraline
• [[Wikipedia:SNRIs|DangerousInteraction::SNRIs]] - Such as tramadol and venlafaxine
• 5-HTP

Legal issues

Efavirenz is not known to be illegal in any jurisdictions, and is considered a prescription only medication.

See also

• Responsible use
• Hallucinogen
• Psychedelics

External links

• Efavirenz (Wikipedia)
• Getting High On HIV Medication (Hammilton Morris / YouTube)