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Pharmacology 200 > 2-cannabis and cannabinoids > Flashcards

2-cannabis and cannabinoids Flashcards

1
Q

what is cannabis

A

genus of flowering plant, contains many bioactive compounds (THC and CBD)

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2
Q

what is the primary psychoactive compound in cannabis

A

THC

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3
Q

what are cannabinoids

A

class of chemical compunds that act at the cannabinoid receptors

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4
Q

are all cannabinoids cannabis

A

no

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5
Q

are cannabis all cannabinoids

A

yes i think

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6
Q

are THC and CBD cannabis or cannabinoids

A

cannabinoids that came from cannabis

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7
Q

what are phytocannabinoids

A

things that cannabis contain hundreds of

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8
Q

what are terpenoids

A

in cannabis, a non-cannadiboid constituent which gives the characteristic smell
maybe also anti-inflammatory, bacterial and anxiety

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9
Q

why is it difficult to harness clinical utility

A

because there are so many compounds with synergistic effects and many different strains

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10
Q

what is bioavailalability

A

absorption, fraction of an administered drug that reaches effectors (receptors, plasma, CNS)

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11
Q

what is bioavailalability

A

absorption, fraction of an administered drug that reaches effectors (receptors, plasma, CNS)

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12
Q

what is bioavailability and time to reach peak plasma concentration time for smoking weed

A

25%

6-10mins

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13
Q

what is bioavailability and time to reach peak plasma concentration time for eating weed

A

6%

2-6 hours

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14
Q

what kind of molecule is THC (philic/phobic to what)

A

highly lipophilic

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15
Q

where is THC rapidly taken up by

A

tissues with high blood flow

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16
Q

where does THC accumulate slowly

A

tissues with less blood flow and release it over a longer period of time

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17
Q

how is THC metabolized and into what

A

in the enzyme by CYP 2C9 into 11-OH_THC and THC-COOH

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18
Q

how is most of the THC excreted

A

as metabolites, 65% in feces and 25% in urine

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19
Q

how many days for 80-90% of THC to be excreted

A

5

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20
Q

how many days can you detect THC in the urine for low dose THC

A

2-5 days

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21
Q

how many days can you detect THC in the urine for chronic daily THC users

A

for weeks because it stores in the adipose tissues

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22
Q

which G protein is cannabinoid receptors

A

Gi

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23
Q

what are the types of cannabinoid receptors

A

CB1 and CB2

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24
Q

how do CB receptors work (pathway after G protein)

A

decrease cAMP accumulation which decreases Ca++ in firing neuron, increases K+, inhibits neurotransmitter release and synaptic transmissions

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25
Q

what ions are affected by cannabinoid receptor activation

A

inhibits influx of Ca and promotes outflux of K

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26
Q

what does THC do to the receptors and which receptors

A

THC is a partial agonist at CB1

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27
Q

what does CBD do to what receptor

A

not totally understood

but maybe negative allosteric modulator of CB1

28
Q

what does CBD do to the effects of THC

A

it can blunt the effects of THC

29
Q

where are CB1 receptors found

A

some of the most abundant GPCR

brain, peripheral organs (heart, liver, fat, stomach, testes) and peripheral nerves

30
Q

where are CB2 receptors found

A

mostly on immune cells

31
Q

what are the psychoactive effects of CB2 receptors

A

none

32
Q

where are there high CB1 receptors in the brain

A

areas of thought, reward, memory, motor

cerebral cortex, hippocampus, cerebellum, etc

33
Q

where are there low CB1 receptors in the brain

A

in the brain stem (autonomic reflexes)

34
Q

what are the general effects of THC

A

euphoria, relaxation, disinhibition, changes in perceptrion, vasodilation, increase pulse rate

35
Q

what are the potential theuraputic effects of THC

A

nausea, appetite increase, decreased ocular pressure, pain releafe

36
Q

what are the unwanted effects of THC

A

memory impairment, dysphoric state, hallucination, depersonalization, psychosis

37
Q

what can be a therapeutic potential for CBD

A

inflammation, anxiety, emesis, nausea, inflammatory pain, epilepsy

38
Q

what are the acute effects of weed

A

panic attacks, anxiety, psychosis, paranoia, convulsions, hyperemesis, RARE

39
Q

what are the prenatal effects of weed

A

maybe neuroanatomical and behavioural changes

40
Q

why is weed not deadly

A

CB1 receptors are very sparse in the brain stem region (controls respiratory and cardiovascular)

41
Q

is there a correlation with schizophrenia and cannabis

A

there is a lot a correlative data for schizophrenics to use more cannabis, and early cannabis use predicts later onset schizophrenia (dose dependent)

but not causation

42
Q

when is cannabis use a risk for schizophrenia

A

when it may be a trigger for people that are genetically at risk

43
Q

what is tolerance

A

decreased response to the effects of the drug, necessitating ever larger doses to achieve the same effect

44
Q

how does tolerance work for CB1 receptors

A

chronic activation of CB1 receptor uncouples from intracellular downstream signal transduction events or receptor downregulation (internalization or degradation of receptor)

45
Q

what is psychological dependence

A

compulsive drug-seeking behaviour in which the individual uses the drug receptively for personal satisfaction, often in the face of known risks to health

46
Q

what is physiological depende

A

revealed when withdrawal of the drug produces symptoms and signs that are frequently opposite of those sought by the user

47
Q

what is cannabis withdrawal like

A

mild, short lives

restlessness, irritability, mild agitation, insomnia, nausea, cramping

48
Q

what are synthetic cannabinoids

A

a manufactured compounds whose properties imitate those of the active constituents of cannabis

49
Q

why do synthetic cannabinoids

A

increased specificity
decreased off target effects
easier dosing
better controlled studies

50
Q

what are the most well confirmed clinical effects

A

help with nausea, appetite loss

51
Q

what is nabilone

A

synthetic analog of THC

52
Q

whast is Dronabinol

A

a trans isomer of THC (enantiomer), approved nausea for chemo patients and weight loss for AIDs

53
Q

how are nabilone and dronabinol taken?

A

orally

54
Q

why does nabilone and dronabinol have less psychotropic effects than cannabis

A

b/c they are taken orally and also because the strictures are different. also because this is pure, not with the other stuff in it

55
Q

what is nabiximol (sativex)

A 
botanical drug, cannabis extract
1:1 mixture of THC and cannabinol
sublingual spray
pain relief for MS or cancer
less psychotropic effects than smoked
56
Q

what is rimonbant

how does it work

A

inverse agonist at the CB1 receptor

thought it would be good for obesity. it was but then people got depressed

57
Q

what are the 2 types of endocannabinoids

A

anadamide (AEA) and 2-arachinoyl glycerol (2-AG)

58
Q

what are endocannabinoids

what do they do

A

endogenous cannabinoids that mediate mood, feeding and motor function

59
Q

how are AEA and 2-AG made

A

from the phospholipid bilayer of the cell membrane

60
Q

what kind of neurotransmitters are AEA and 2-AG

A

retrograde neurotransmitters

61
Q

whats a retrograde neurotransmitters

A

they are not stored in vesicles, but are synthesized in demand when needed

released by a postsynaptic dendrite or cell body, and travels “backwards” across a chemical synapse to bind to the axon terminal of a presynaptic neuron

62
Q

how do endocannabinoids affect neuronal release

A

like THC, it decreases neuronal release of other transmitters

63
Q

how is synthesis of 2AG or AEA stimulated

A

by an increase in intracellular Ca (when synaptic neuron becomes depolarized by the action of a neurotransmitter)

this is how it is only produced in activated brian regions

64
Q

how are AEA and 2AG rapidly cleared from the synapse and inactivated

A

rapidly by FAAH

fatty-acid amide hydrolase) and MAGL (monoacylclycerol lipase

65
Q

what does suppression of FAAH and MAGL cause

A

a prolongation of the activity of endocannabinoids (enhance CB1 activation) where AEA and 2AG levels are the highest

66
Q

how were FAAH and MAGL thought to work

A

maybe for chronic pain

but some show severe side effects

67
Q

does FAAH and MAGL produce the typical psychoactive effects of THC

A

no

but it does do analgesia

Pharmacology 200 (29 decks)

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