PSY 134 - hallucinogens

hallucinogen

higher order categorization; produce hallucinations (mostly only higher doses), profound subjective emotional effects, augmented sensations

psychedelics

magnify sensations and emotions; manifest or be in touch with the psyche, produce hallucinations at recreational doses

phantasticants

makes exp feel of great emotional or worldly significance

empathogens

magnify emotions, particularly empathy

psychotomimetics

produce sxs similar to psychosis; auditory/visual hallucinations, feelings of persecution/anxiety

club drugs

enhance the subjective experience of music and dancing

History of LSD (d-lysergic acid diethylamide)

Synthesized in 1938, popularized in the 60s, schedule I in 1967

Slang of LSD

acid, cid, L, blotter, tabs, LAD, doses, trips, microdots; experience = tripping, flying, frying

Dose of LSD

60s (200-400 micrograms), today (50-150 micrograms); LD50 (1200 microgram)

Chemistry of LSD

appear in ergot (fungal parasite of rye), structural similarity to 5-HT, agonist of 5HT2A and 5HT1C

pharmacology of 5HT2A receptors

located in dorsal and medial raphe nuclei (rostral system of 5-HT); rapidly desensitize then sensitize; reduce 5HT1A (inhibitory autoreceptor) function, so increase 5-HT release

Pharmacokinetics of LSD

1% availability PO, half life 2.5-5 hrs; liver metabolism

LSD tol

rapid tol development (2-3 days) via downreg of 5HT2A receptor; sens rebounds after 1 wk; cross tol w other psychedelics

LSD WD

Hallucinogen Persisting Perception Disorder; residual perceptual distortions, trailing phenomenon (“strobe lights”); no notable syndrome, may be due to lack of continuous use

positive fx of LSD

inc energy, inc assoc/creative thinking, mood lift, inc awareness/appreciation of music, inc awareness of senses

neutral psychological fx of LSD

change in consciousness, unusual thoughts/speech, time distortion, mood swings

neutral physiological fx of LSD

difficulty focusing, pupil dilation, inc salivation/mucus, inc body temp, inc HR

negative psychologicals fx of LSD

anxiety, confusion, paranoia, fear, panic, megalomania, overawareness/sensitization to music/noise, unwanted/overwhelming feelings, flashbacks

negative physiological fx of LSD

tension, diaphoresis, nausea, vertigo

threshold fx of P. cubensis

0.25-0.75g; psychological (nervousness, brightness, auras, sens to movement, emo sens); physiological (slight coldness, mild gas/nausea, slight pupil-dilation)

medium dose fx of P. cubensis

0.75-2.5g; psychological (intensification of threshold effects, open/closed eye visuals, time distortion, less focus, empathy, mental looping, insight/new perspectives); physiological (intensification of threshold effects)

high dose fx of P. cubensis

2.5-10g; psychological (more intense fx, more anxiety, mental discomfort, near death experiences, loss of self, manifestation of repressed memories, talking to external/autonomous entities); physiological (more intense fx, emesis)

DMT (N,N-dimethytryptamine)

metabolite of melatonin; full fx 10-60 sec from smoking, lasts 5-20 minutes, 1-2 hrs lingering, days of unsettling difficulty to integrate experiences; greatly variable experiences: changes in life view, dreamscapes, talking with aliens, frightening/overwhelming forces, abrupt return to baseline

mechanism of DMT

full agonist at 5HT2A receptor; also potentially agonist of TAAR1 (trace amine receptor)

2-CB-4-bromo-2,5-dimethoxyphenethylamine (2C-B, or Bees)

schedule I hallucinogen, marketed as a replacement to MDMA, found in raves/clubs; 5-25mg pills, 1/3 dose powder

Chemistry of Bees

phenethlyamine analogue of DOB; high affinity for 5HT2A (partial agonist)

Fx of Bees

positive (at onset: energy, altered sensations; at peak: new perspectives, insight, mood lifts/introspection, color shifts, moving vision); neutral (pupil dilation); negative (at onset: anticipation/anxiety; at peak: body load, powerful hallucinations, bad trip; physiological: GI distress, inc mucus, coughing)

Peyote cactus (mescal, buttons, big chief)

agonist of 5HT2A; recorded by by spanish conquistadors, used by native Mexicans

Hx MDMA

first synth 1890s, schedule II in 1985; euphoric empathogen

Duration and dosage of PO MDMA

dose: 30 mg (threshold), 75-125 mg (common); duration: 3-5 hours (onset 20-90 min, peak for a couple hours, comedown 1-2 hours), 2-24 hrs aftereffects; half life 8 hrs

Mechanism of action of MDMA

5-HT/NE releaser; SERT/NET/DAT reuptake inhibitor

positive fx of MDMA

extreme mood lift, communication, energy, love, comfort, belonging, empathy, forgiveness, awareness/appreciation for music, bright/intense sensations, urge to hug/kiss people

neutral fx of MDMA

loss of appetite, visual distortion, nystagmus, inc HR, HTN, change in body temp regulation, unexpected emotions

negative fx of MDMA

on drug (inappropriate/unintended emotional bonding, hyperthermia, dehydration, hyponatremia; can lead to death; increases with higher doses); during withdrawal (sadness on comedown, loss/nostalgia, psychological crisis; lasting days to weeks)

Salvia divinorum

salvinorin a; very potent KOR agonist; NO affinity for 5HT2A receptors; short duration of action (5-30 min) bc of rapid metabolism to salvinorin B after crossing BBB