Exam 3: Hallucinogens Flashcards by Angie Broga

3 broad categories of hallucinogens - what is in each (3)

serotonin like (LSD, Peyote, Psilocybin, DMT)
belladonna alkaloids (acetylholine like, atropine, scopolamine)
dissociative anesthetics (PCP, ketamine, salvia)

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substances that produce distortions of perception and of one’s sense of reality

hallucinogens

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properties of psychadelic (mind expanding) drugs

alter sensory perceptions in brain
perceptual disturbances
changes in thought processing (used in religious ceremonies)

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what schedule drug are hallucinogens?

schedule 1

- no accepted medical uses, high abuse liability

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most hallucinogens are ___

what are effects

alkaloids

antibacterial, anitmitotic, anti-inflammatory, analgesic, local anesthetic, hypnotic, psychotropic, antitumor activity

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LSD

schedule 1

synthetic drug derived from ergot

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ergot

LSD
toxic parasitic rye fungus
alkaloids in ergot contract smooth muscles of veins and arteries (restricts blood flow), uterus (early labor), changes in BP
poisoning led to gangrene (loss of blood flow to extremities, they die off) and death in the middle ages
accidental small dose ingestion led to hallucinogenic effects

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Project MKUltra

manipulated people’s mental status by giving LSD forcefully to force spys to reveal secrets

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pharmacology of LSD (ADME and route of admin)

route of admin: oral - so potent it is delivered by stamps/blotter paper

A: 30-60 min post-ingestion from GI tract

D: BBB and NO depot binding

M: SLOW in the liver into 2-oxo-3-hydroxy-LSD

E: half like ~5 hrs

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peyote

schedule 1
peyote cactus - peyote button cut off and dried cactus crown
active ingredient - mescaline (alkaloid)

psychoactive effects like LSD, BUT LSD is way more potent

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pharmacokinetics of peyote(mescaline)

route of admin: oral-peyote buttons - chewed raw or cooked and eaten

A: rapid from GI tract, onset within 30min highest effects ~2hrs post ingestion, effects last up to 8hrs

D: poor lipid solubility, not easily through BBB - so need higher dose to get effects

M: ~50% broken in liver - main metabolite= 3,4,5-trimethoxyphenylacetic acid

E: excreted in urine in 24-48 hrs - even though need high dose it is out quick, 50% unchanged in urine

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psilocybin

schedule 1
many species of magic mushrooms have alkaloids with hallucinogenic properties
cave paintings depicted as early as 3500 BC

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Timothy Leary

psilocybin project

- teach people to self administer drugs to free syches without reliance on doctors

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typical dose of psilocybin

1-2g o dried/powdered mushrooms

- way less than peyote (10-25 mg)

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psilocybin pharmacokinetics

route of admin: dried mushrooms eaten raw, boiled in water for tea, cooked with other foods to mask biter taste

A: broken down into psilocin - active component, only 50% absorbed, psilocin detected in blood plasma 30 min after ingestion

D: BBB, psychoactive effects 10-40min after ingestion, last 2-6hrs

M: psilocybin converted to psilocin which is broken down by MAO

E: excreted unchanged or as psilocin-glucuronide in urine (65%), 20% excreted in bile and feces

psilocin detected in urine up to 7 days - in system for long time

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glucuronide

psilocybin
substance produced by linking glucoronic acid to another substance via special chemical bond, makes water soluble

body does this when it comes across toxins

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DMT

schedule 1
naturally occuring compound in body - biological function unknwon
low levels in brain
inc in response to stress
packaged and stores in neurotransmitter vesicles - serotonin

Ayahuasca

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Ayahuasca

DMT
tea
vine of the soul 
mix of 2 plants (one has DMT, other B-carbolines )
B-carbolines - inhibit MAO activity

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what do you need to give DMT orally

MAO

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what is DMT structurally similar to?

serotonin - share biosynthesis pathway
AADC converts tryptophan to tryptamine
tryptamine convets DMT to INMT

VMAT2 packages DMT into vesicles

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pharmacokinetics of DMT

route of admin: smoked, snorted

A: DMT has no bioavailability taken orally - broken down by MAO, smoked or snorted produces short but very strong hallucinatory experiences

D: rapid to brain, active transport allows BBB, depot binding - small amount remains in brain for up to 7 days!!

M: metabolite= indole-3-acetic acid

E: rapid when taken WITHOUT MAO, excreted in urine in 24 hrs, 10% unchanged
if with MAO takes longer

ayahuasca pharmacokinetics

tea taken orally
B-carbolines block MAO and DMT breakdown in liver so DMT reaches brain
hallucnogenic effects start 30-60min post ingestion
peak 1-2hrs dissipate 4hrs - longer to kick in

effects of hallucinogens (8)

hallucinations
altered perceptions
profound effects on mood
altered thinking processes
altered physiological processes
altered state of consciousness
feeling of being separated from body 
psychosis

psychadelic effects time frame

begin 30-90min after ingestion
LSD trip can last 6-12 hrs
smoked DMT effects felt within seconds, peak over a few minutes, gone in an hour

flashbacks

re-experiencing hallucinations after chronic use, years later eventhough drug use stopped unc;ear why

what determines if you will have a good or bad trip

dose, personality, previous drug experiences, context

4 phases of LSD trip

onset: 30min-hr after LSD 1st feel behavioral effects plateau: 2 hrs in , time slows- perception it has been a long time peak: 3 hrs in , synesthesia , most hallucinations come-down: 5-6 hrs in

synesthesia

crossing of sensory modalities | ex: feeling sounds or hearing colors

smoking DMT effects over time

lungs burn, cough loud sound in ears until feel yourself blow up and enter universe break into another universe - heart beats faster you have left body visions fade out euphora lats 30min ater visual trip

physiological effects of hallucinogens

``` sympathetic nervous system - pupil dilation inc HR BP T restlessness dizziness, vomiting, nausea - peyote and ahowasa ```

LSD, DMT, and psilocin are chemically similar to...

serotonin

mescaline is structurally similar to..

NE and amphetamine (metabolite p-hydroxymethamphetamine had hallucinogenic effects)

LSD binds with high affinity to at least ____ different serotonergic receptor subtypes

LSD, mescaline, DMT, and psilocin bind to what type of receptors and are what agonists

serotonin receptors | 5-HT2A receptor agonists

hallucinogenic properties require the activation of what receptor subtype? and... this alters levels of what neurotransmitter in cerebral cortex?

5-HT2A receptors | glutamate levels altered

why is LSD so potent? | why do its effects last so long?

LSD binding to 5-HT2A forms lid that locks LSD in place temporarily trapping it lacks ability to unbind sustained activation

where are 5HT2A receptors found

raphe, PFC, locus coeruleus

activation of 5HT2A receptors increases the release of what into the cerebral cortex to turn on PFC

glutamate

what do EEG studies show about hallucinogens

they disrupt the normal rhythmic oscillations in the cerebral cortex - added extra stimuli for them to attend to that they would normally ignore

effect of hallucinogen on visual cortex

alters visual processes, including modal object completion | activation of occipital lobe

effect of hallucinogens on temporomedial cortex

inc activity - complex visual processing , integration area | some auditory hallucinations

effects of hallucinogens on cerebral cortex

inc sensory signals to PFC

effect of hallucinogens on locus coeruleus

dec spontaneous activity, sends normal suppressed sensory info to cerebral cortex sleep states, dream like states

effects of hallucinogens on PFC

inc activity of PFC | central sensory integration area of cerebral cortex

serotonin receptor binding causing hallucinations: thalamus

involved in sensory routing and sleep (reticular patwhay - arousal) - hallucinations like dreams activate your dreams while you are awake

sertonin receptor binding causing hallucinations in limbic pathway

emotional investment/context of meaning of hallucination vs dream when ppl scared bc of a bad trip - see something scary in their environment like monsters chasing them entorhinal cmpus and hippocampus for context

do hallucinogens produce depence and withdrawal symptoms

what hallucinogens produce rapid tolerance to repeated use through down regulation of 5HT2A receptors

most hallucinogens EXCEPT DMT

push to re-evaluate therapeutic uses for what 2 hallucinogens

psilocybin and LSD

why would hallucinogens improve mental health

when consume they have experience when they come off of it they get an afterglow period!!!

afterglow period

gives clarity, reduces negative affect (anxiety, fear, depression) in state of well being and calmness it persists for days - longer time used to treat long term chronic issues