Lecture 13: Cannabinoid Agonists/Antagonists Flashcards

1
Q

marijuana is a mild ___ agent

A

sedative-hypnotic

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2
Q

4 ways THC resembles ethyl alcohol effects

A
  1. disrupted attn
  2. short term memory
  3. altered sensory awareness
  4. altered control of motor movement and posture
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3
Q

main psychoactive ingredient in cannabis

A

delta9 tetrahydro-cannabinol

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4
Q

THC is sold commercially as ___

A

Marinol

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5
Q

3 other significant ingredients in cannabis

A
  1. cannabinol
  2. cannabidiol
  3. terpenes
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6
Q

hashish (%)?

A

dried resinous exudate of female flowers (10-20%)

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7
Q

sinsemilla (%)

A

dried tops of unfertilized female plants (5-8%, no seeds)

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8
Q

bhang

A

dried remainder of plant; THC content 2-5%

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9
Q

3 methods of marijuana consumption

A
  1. smoking

2. vaping

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10
Q

firecracker

A

nutella or peanut butter on a cracker with weed sprinkled on top

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11
Q

2 extraction methods for edibles

A
  1. butter

2. alcohol

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12
Q

when was cannabis considered a narcotic that caused violent behavior?

A

1920s

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13
Q

when did weed get its public image as a killer drug?

A

1930s-1940s

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14
Q

what 2 groups don’t support weed legalization?

A

seniors

republicans

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15
Q

how many americans use marijuana?

A

15 million

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16
Q

what percentage of teenagers had smoked marijuana in the past month?

A

25%

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17
Q

heavy use at early age is associated with ___

A

psychopathology later in life

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18
Q

sativex

A

THC + CBD 1:1

oramucosal mouth spray

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19
Q

6 args in favor of legalization

A
  1. legal consistency
  2. regulation
  3. crime
  4. destroys lives
  5. racism
  6. cost
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20
Q

2 endocannabinoids

A
  1. anandamide

2. 2-AG

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21
Q

THC mimics the action of __

A

anandamide

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22
Q

2 cannabinoid receptors THC binds to

A

CB1

CB2

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23
Q

where are CB1 receptors?

A

brain and spinal cords

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24
Q

where are CB2?

A

periphery

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25
CB receptors are ___
metabotropic; 7 membrane spanning reasons
26
when THC binds to CB receptors, what second messenger does it activate?
adenylate cyclase
27
what does adenylate cyclase ultimately do?
inhibits glu release
28
there are ___ more CB1 receptors than opioid receptors in the brain
10-20x
29
CB1 receptor function in frontal cortex (4)
1. psychoactive effects 2. distortions of time/sound/color/taste 3. inability to concentrate 4. dreamlike state
30
CB1 function in hippocampus (2)
1. memory | 2. coding of sensory input
31
CB1 function in bg & cerebellum
movement & postural control
32
CB1 function in spinal cord
on nociceptors in dorsal horn and dorsal root ganglion
33
what are nociceptors?
responsible for pain
34
are there CB1 receptors in brain stem?
no
35
why doesnt weed affect respiration?
no CB1 receptors in brain stem
36
4 areas with CB2 receptors
1. lymphatic system 2. heart 3. tissues involved in inflammation and pain response 4. some immune cells
37
anandamide blocks ___ responses
nerve growth factor protein-induced pain and inflammatory response
38
retrograde signaling
released from postsynaptic cell and act on presynaptic terminal
39
activation of presynaptic cannabinoid receptors temporarily ___
reduces amount of conventional NT release
40
endocannabinoid-mediated system permits ___
the postsynaptic cell to control its own incoming synaptic traffic
41
when the release of GABA is reduced, the net postsynaptic effect is ___
increase in postsynaptic excitation
42
typical marijuana ciagarette contains ___
75mg of THC; 25-50% available in smoke
43
how long does weed last?
2-3 hours
44
THC is metabolized by ___
CYP450
45
THC active metabolite
11-hydroxy-delta-9-THC
46
inactive THC metabolite
carboxy-THC
47
how long is carboxy-THC present in urine?
1-3 days in infrequent smokers 7-21 in regular smokers 30 days in chronic smokers
48
THC is stored in ___
body fat
49
THC can persist in body for ___. longer in who?
days to 2 weeks | chronic and obese smokers
50
reverse tolerance
delayed elimination prolongs and intensifies effects of subsequently smoked marijuana
51
5 ways CNS effects vary
1. dose 2. route 3. experience 4. vulnerability 5. setting
52
mice lacking CB receptors have ___ (4)
1. higher mortality rates 2. weight loss 3. less active 4. lower pain thresholds
53
4 THC and opioid effects
1. analgesia 2. sedation 3. hypothermia 4. hypotension
54
THC activates CB1 receptors in (2), which stimulates ___
1. hypothalamus 2. limbic structures appetite for sweet and fattening foods
55
possible MoA for memory problems
activation of CB1 receptors in hippocampus
56
how long can adverse cognitive effects last?
1 month
57
THC impaires (4)
1. coordination 2. perception 3. reaction time 4. attention
58
2 high dose effects of THC
1. acute depressive reactions | 2. acute panic reaction/mild paranoia
59
cannabis exposure can contribute to ___ in adolescents with ___. cannabis is likely a ___
schizophreniform psychosis family history component cause
60
cannabinoid hypothesis of schizophrenia
psychotic disorders involve disturbances in DA NT systems, with which the cannabinoid sys interacts
61
THC and anandamide active the ___
mesolimbic dopaminergic reward system
62
cannabis use during adolescence increases risk of non-affective psychosis in people who ___
experienced childhood sexual trauma
63
LD50
ratio of lethal to effective is ~1000
64
CB2 receptors in heart might protect against ___
ischemic attacks
65
marijuana smoking increases risk of lung cancer by ___
8% for each year of combined tobacco and marijuana use
66
2 effects of chronic use by males
1. reduced testosterone | 2. reduced sperm formation
67
2 effects of chronic use by females
1. reduced level of follicle-stimulating hormone and luteinizing hormone 2. impact on menstrual cycles and anovulatory cycles
68
4 effects on fetus
1. impaired visuospatial function 2. impulsivity/inattention 3. depressive symptoms 4. later substance abuse
69
fetal exposure is similar to effect of ___. why?
prenatal stress | impacts endocannabinoid system; exposure may interfere with stress coping ability
70
infants born to marijuana-smoking mothers may display (3)
1. tremulousness 2. abnormal responses to stimuli 3. neurobehavioral performance deficits
71
chronic marijuana use (2)
downregulates and desensitizes CB1 receptors (behavioral tolerance)
72
__ in 10 people who smoke cannabis become dependent
1
73
8 withdrawal symptoms
1. irritability 2. anxiety 3. craving 4. disrupted sleep 5. aggression 6. depression 7. decreased appetite 8. weight loss
74
dronabinol
synthetic formulation of THC; most effective pharmacotherapy for withdrawal
75
naltrexone effectiveness
moderate, but can be overcome with high doses of cannabis
76
3 investigated medicines
1. rimonabant (CB1 receptor reverse agonist) 2. bupropion 3. buspirone (serotonergic antidepressant)
77
6 effects of THC/things it can treat
1. pain relief 2. appetite stimulant 3. glaucoma treatment 4. sleep aid 5. anti-epileptic 6. muscle spasm relief
78
3 cannabinoids
1. THC 2. cannabidiol (CBD) 3. cannabinol (CBN)
79
6 effects of CBD
1. pain relief 2. anti inflammatory 3. anti epileptic 4. strengthens bones 5. anti nausea 6. reduces negative effects of THC
80
is CBN psychoactive?
mildly
81
how is CBN produced?
degradation of THC
82
CBN MoA
weak agonist at CB1 and CB2
83
which receptor does CBN have higher affinity to?
CB2
84
what effect is CBN responsible for?
couch lock
85
synthetic THC
dronabinol
86
terpenes; how many?
100+; aromatic compounds in cannabis
87
5 terpenes
1. A-pinene 2. linalool 3. beta caryophyllene 4. myrcene 5. limonene
88
ensemble effect
all compounds in weed work together to produce a greater effect
89
sativa may have a higher ___ ratio than indica
CBD:THC
90
indicas tend to be more psychoactive due to higher ___
THC:CBD ratio
91
indicas are used to relieve/treat (4)
1. relieve stress 2. aid with sleep 3. muscle spasms 4. nausea
92
drugs that stimulate cannabinoid receptor synthetically
cannabinomimetics
93
cannabinomimetics are ___ in blood and urine
undetectable
94
___ is more potent than THC
JWH-018