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Pharmacology 200 > 2 - hallucinogens > Flashcards

2 - hallucinogens Flashcards

(69 cards)

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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
how does LSD interact with the 5-HT2a receptors
LSD has a high affinity and is a partial agonist at the 5-HT2a receptors
26
are all 5-HT2a agonists hallucinogenic why or why not
no because of biased agonism (LSD activates phospholipase A2, serotonin activates phospholipase C)
27
how do we know 5-HT2a mediates the hallucinations
tests in mice, they have head bobs
28
what does biased agonist of the 5-HT2a cause
different expression of transcription factors (Thats why some are hallucinogenic and others arent)
29
can you build a tolerance to LSD
yes | lasts several days
30
how does LSD tolerance happen
downregulation of 5-HT2 receptors (not other 5-HT tho)
31
what is cross tolerance
tolerance of multiple drugs that act at serotonin receptors (LSD, DMT, psilocybin)
32
what is the structure of indolamines
benzene + 5 membered pyrrole + amine
33
what structure are indolamines similar to
serotonin
34
what are the side effects of psilocybin
euphoria, hallucinations, change in perception of time
35
what are the adverse reactions of psilocybin
nausea, panic attacks
36
can you overdose from psilocybin
no
37
how is psilocybin handled in the body
psilocybin (prodrug) is dephosphorylated into psilocin
38
what kind of effects of psulocin have at which receptors
partial agonist at 5HT receptors. high affinity for 5HT-2c and 5-HT2b receptors, low affinity for 5-HT2a receptors
39
how does psilocybin have hallucinations
5-HT2a
40
what is DMT structurally similar to
tryptamine
41
what is the only hallucinogen that is naturally produced in the mammalian brain
DMT
42
how does DMT affect receptors
partial agonist at 5-HT receptors
43
how does DMT cause hallucinations
5-HT2a
44
what are the roles of phenethylamines in the body
modulate the monoamine system
45
what are types of ways phenethylamines affect the body
CNS stimulates (amphetamine, MDMA) Hallucinogenics (MDMA) antidepressants overall -->wide variety!!
46
what does mescaline come from
peyote cactus | naturally occurring!
47
what is mescaline synthesized from
tyrosine
48
which receptors do mescnaline bind to and what affinity
5-HT2A receptors with high affinity
49
is mescaline addictive
not really
50
what are the side effects (good)of MDMA
increased energy, empathy, pleasure, hallucinations
51
what are the bad side effects of MDMA
memory impairment, paranoia, difficulty sleepy, teeth grinding, blurred vision, sweating, tachycardia, addiction
52
what causes MDMA related deaths
increased body temperature and dehydration
53
what is MDMA similar in structure to
the monoamines
54
what is mescaline similar in structure to
the monoamines
55
how does MDMA cause the hallucinogenic effects
5HT-2A partial agonist
56
what is efflux
reversing the direction of transport, allows amines to flow backwards through plasma membrane transporters (exits the cell)
57
what does efflux cause to neurotransmitters
increased synaptic concentration of neurotransmitters
58
how does MDMA affect efflux
it acts as a substrate for monoaminergic transporters, where it induces efflux affects TRANSPORTERS not receptors
59
what does MDMA bind to
SERT (10x selectivity for SERT than NET or DAT)
60
what does amphetamines do to CNS
stimulates
61
how do amphetamines cause hallucinations
they dont lol
62
what are the effects of amphetamines
euphoria, fatigue resistance, improved cognitive control, addiction, psychosis
63
what receptors does amphetamines affect | and how
DAT and NET more than SERT | inhibits monoamine transporter through efflux (like MDMA)
64
why are amphetamines less hallucinogenic than MDMA
MDMA affects SERT (which affects the 5HT-2A receptors) while amphetamines are more selective for NET and DAT
65
what is methylphenidate
ritalin, used to treat ADHD
66
what are the effects of methylphenidate
improved alertness and concentration, no hallucination, safe and widely prescribed
67
which receptors does methylphenidate affect
NE and DAT efflux
68
why does amphetamine have a higher risk of addiction than methylphenidate
methylphenidate gets into the system slower, slow rate of onset, slow rate of offset, not a "rush" associated with the drug
69
what does small Ki
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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