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Pharmacology 200 > 2 - hallucinogens > Flashcards

2 - hallucinogens Flashcards

1
Q

what are three monoamine transmitters

A

serotonin, norepinephrine, dopamine

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2
Q

what is the role of the mooamines

A

regulate mood, appetite, sleep, cognition, perception, arousal

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3
Q

how do drugs affect the monoamines

A

increasing release, blocking reuptake, inhibit metabolism, or activate receptor

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4
Q

how many types of serotonin receptors

A

7 subtypes

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5
Q

what kind of receptors for norepinephrine

A

alpha and beta adrenergic receptors

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6
Q

what kind of receptors for dopamine

A

D1 and D2

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7
Q

what kind of receptors are 5HT, NE, domaine?

A

they are all GPCRs

except for 5HT-3

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8
Q

what kind of receptor is 5HT-3

A

a ligand gated ion channel

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9
Q

how many type of G protein receptors are there,

what are they called

A

Gi (inhibitory)
Gs (excitatory)
Gq (modulatory)

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10
Q

how are the monoamines metabolized

A

by monoamine oxidases (MAO)

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11
Q

how do the MAO work

A

catalyze the oxidation of the monoamines

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12
Q

how do MAOI work

A

they block the action of MAO (block monoamine oxidation)

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13
Q

what are the 3 monoamine transporters

A

NET
DAT
SERT

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14
Q

what do the NE DAT and SERT do

A

clear synaptic neurotransmitters by actively transporting the them into the cytosol

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15
Q

what is VMAT stand for

A

vesicular monoaminergic transporter

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16
Q

what does VMAT do

A

pump cytosolic neurotransmitters into vesicles to be released back into the synapse after AP

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17
Q

where are DAT, SERT and NET found

A

on the plasma membrane

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18
Q

where are VMATs found

A

on the membrane of vesicles

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19
Q

where does LSD originate from

A

ergot, fungus from rye

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20
Q

what are the effects of LSD

A

dilated pupils, increased heart rate, increased BP, hallucinations, some enlightenment

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21
Q

what are the adverse psychiatric effects of LSD

A

anxiety, paranoia and delusions are possible

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22
Q

what is hallucinogen persisting perception disorder

A

when distressing visual hallucinations that appear following drug use

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23
Q

how many receptor targets of LSD

what is the most common

A

over 50, with several 5-HT receptors

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24
Q

what receptor mediates hallucinogenic effects

A

5-HT2a

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25
Q

how does LSD interact with the 5-HT2a receptors

A

LSD has a high affinity and is a partial agonist at the 5-HT2a receptors

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26
Q

are all 5-HT2a agonists hallucinogenic

why or why not

A

no

because of biased agonism (LSD activates phospholipase A2, serotonin activates phospholipase C)

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27
Q

how do we know 5-HT2a mediates the hallucinations

A

tests in mice, they have head bobs

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28
Q

what does biased agonist of the 5-HT2a cause

A

different expression of transcription factors (Thats why some are hallucinogenic and others arent)

29
Q

can you build a tolerance to LSD

A

yes

lasts several days

30
Q

how does LSD tolerance happen

A

downregulation of 5-HT2 receptors (not other 5-HT tho)

31
Q

what is cross tolerance

A

tolerance of multiple drugs that act at serotonin receptors (LSD, DMT, psilocybin)

32
Q

what is the structure of indolamines

A

benzene + 5 membered pyrrole + amine

33
Q

what structure are indolamines similar to

A

serotonin

34
Q

what are the side effects of psilocybin

A

euphoria, hallucinations, change in perception of time

35
Q

what are the adverse reactions of psilocybin

A

nausea, panic attacks

36
Q

can you overdose from psilocybin

A

no

37
Q

how is psilocybin handled in the body

A

psilocybin (prodrug) is dephosphorylated into psilocin

38
Q

what kind of effects of psulocin have at which receptors

A

partial agonist at 5HT receptors. high affinity for 5HT-2c and 5-HT2b receptors, low affinity for 5-HT2a receptors

39
Q

how does psilocybin have hallucinations

A

5-HT2a

40
Q

what is DMT structurally similar to

A

tryptamine

41
Q

what is the only hallucinogen that is naturally produced in the mammalian brain

A

DMT

42
Q

how does DMT affect receptors

A

partial agonist at 5-HT receptors

43
Q

how does DMT cause hallucinations

A

5-HT2a

44
Q

what are the roles of phenethylamines in the body

A

modulate the monoamine system

45
Q

what are types of ways phenethylamines affect the body

A

CNS stimulates (amphetamine, MDMA)
Hallucinogenics (MDMA)
antidepressants
overall –>wide variety!!

46
Q

what does mescaline come from

A

peyote cactus

naturally occurring!

47
Q

what is mescaline synthesized from

A

tyrosine

48
Q

which receptors do mescnaline bind to and what affinity

A

5-HT2A receptors with high affinity

49
Q

is mescaline addictive

A

not really

50
Q

what are the side effects (good)of MDMA

A

increased energy, empathy, pleasure, hallucinations

51
Q

what are the bad side effects of MDMA

A

memory impairment, paranoia, difficulty sleepy, teeth grinding, blurred vision, sweating, tachycardia, addiction

52
Q

what causes MDMA related deaths

A

increased body temperature and dehydration

53
Q

what is MDMA similar in structure to

A

the monoamines

54
Q

what is mescaline similar in structure to

A

the monoamines

55
Q

how does MDMA cause the hallucinogenic effects

A

5HT-2A partial agonist

56
Q

what is efflux

A

reversing the direction of transport, allows amines to flow backwards through plasma membrane transporters (exits the cell)

57
Q

what does efflux cause to neurotransmitters

A

increased synaptic concentration of neurotransmitters

58
Q

how does MDMA affect efflux

A

it acts as a substrate for monoaminergic transporters, where it induces efflux
affects TRANSPORTERS not receptors

59
Q

what does MDMA bind to

A

SERT (10x selectivity for SERT than NET or DAT)

60
Q

what does amphetamines do to CNS

A

stimulates

61
Q

how do amphetamines cause hallucinations

A

they dont lol

62
Q

what are the effects of amphetamines

A

euphoria, fatigue resistance, improved cognitive control, addiction, psychosis

63
Q

what receptors does amphetamines affect

and how

A

DAT and NET more than SERT

inhibits monoamine transporter through efflux (like MDMA)

64
Q

why are amphetamines less hallucinogenic than MDMA

A

MDMA affects SERT (which affects the 5HT-2A receptors) while amphetamines are more selective for NET and DAT

65
Q

what is methylphenidate

A

ritalin, used to treat ADHD

66
Q

what are the effects of methylphenidate

A

improved alertness and concentration, no hallucination, safe and widely prescribed

67
Q

which receptors does methylphenidate affect

A

NE and DAT efflux

68
Q

why does amphetamine have a higher risk of addiction than methylphenidate

A

methylphenidate gets into the system slower, slow rate of onset, slow rate of offset, not a “rush” associated with the drug

69
Q

what does small Ki

A

The smaller the Ki, the greater the binding affinity and the smaller amount of medication needed in order to inhibit the activity of that enzyme.

Pharmacology 200 (29 decks)

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