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.Pharmacology > Chapter 17: Drugs of Abuse > Flashcards

Chapter 17: Drugs of Abuse Flashcards

1
Q

what causes tolerance/decreased response to drug?

A

neuronal changes and changes in receptors/metabolism

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2
Q

physiological dependence is characterized by ___or ___ effect when the drug is removed

A

withdrawal symptoms; rebound

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3
Q

why cant beta blockers be abruptly stopped?

A

the body has become used to their BP lowering effects , causing rebound hypertension

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4
Q

what is psychologic dependence?

A

drug-seeking behaviour

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5
Q

prescription drugs that have either ___ or ___ effects are often misused

A

sedative or stimulant

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6
Q

does LSD have a therapeutic use?

A

no

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7
Q

can LSD be addictive?

A

no evidence to say it is addictive

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8
Q

t/f not all drugs that are misused are addictive

A

true

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9
Q

t/f all recreational drugs are addictive

A

no

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10
Q

there is a link between the activation of ___ pathways in the brain and the development of addiction

A

dopamine

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11
Q

activation of the mesolimbic dopamine pathways promotes ___ and ___ leading to addiction

A

reinforcement and reward

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12
Q

t/f different brain regions communicate to determine how we respond to a situation

A

true

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13
Q

the dopaminergic neurons that are linked to addiction are found in the mesolimbic pathways that runs from the ___ to the nucleus accumbens

A

ventral tegmental area (VTA)

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14
Q

drugs that cause addictive typically release ___ from the VTA neurons in the nucleus accumbens

A

dopamine

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15
Q

what happens in terms of addiction and aversion when dopamine is blocked from entering the nucleus accumbens?

A

has an avoidance effect in animal studies

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16
Q

t/f just blocking the release of dopamine from the VTA will 100% cure addiction

A

false, not that simple

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17
Q

the dopamine hypothesis of addiction states that all addictive drugs cause an increase in the release of dopamine from the ___ into the ___

A

VTA into nucleus accumbens

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18
Q

opioids, THC and GHB affect the dopamine release from the VTA by targeting ____ receptors

A

GPCR

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19
Q

benzodiazepines, nicotine, and ethanol affect the dopamine release from the VTA by targeting ___ receptors

A

ion channel

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20
Q

cocaine, amphetamine, ecstasy affect dopamine release from the VTA by targeting ___

A

transporters

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21
Q

drugs may act upstream of the VTA on ___ neurons to cause disinhibition of the dopaminergic neurons

A

GABAergic

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22
Q

opioids act on ___ receptors of the GABA neuron to reduce the amount of GABA onto VTA

A

mu opiod

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23
Q

cannabinoids act on ____ receptors of the GABA neuron to reduce GABA release on VTA

A

CB1

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24
Q

dopaminergic VTA neurons are influenced by inhibitory ___ neurons

A

inhibitory GABA

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25
Q

where are mu opioid receptors found on GABA and dopaminergic neurons?

A 
GABA= dendrites of cell body 
dopa= presynaptic terminals
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26
Q

where are CB1 receptors found on GABA neurons?

A

presynaptic terminals

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27
Q

the mu opioid and CB1 receptors are coupled to a ___ G protein

A

GI/GO

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28
Q

the GI/GO pathway in GABA neurons stimulated by opioids and cannabinoids is mediated by ____ subunits

A

G beta-gamma

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29
Q

in cell body dendrites, when the mu opioid receptors are stimulated, the Gbeta-gamma subunit increases ___ efflux leading to ____that reduces the excitability of the neuron

A

K+; hyperpolaization

30
Q

in the presynaptic terminals, when Gbeta-gamma subunits are activated they have an inhibitory impact on ___channels preventing the release of ____ which results in disinhibition of VTA dopaminergic neuron

A

Ca; NT

31
Q

t/f drugs can act directly on VTA dopaminergic neuron

A

t

32
Q

nicotine acts on nicotinic Ach receptors on the VTA dopaminergic neuron, causing influx of ___ ions leading to membrane ____.

A

Na; depolarization

33
Q

nicotine on the VTA dopaminergic neuron has what effect?

A

increases excitability; releasing more DA into the nuclei accumbens

34
Q

nicotine stimulates ___ nicotinic Ach receptors

A

NN

35
Q

nicotine is ___ agonist of the NN receptor and varenicline is a ___agonist of the NN receptor

A

full; partial

36
Q

which has a higher binding affinity for nicotine receptor? varenicline or nicotine?

A

varenicline

37
Q

cocaine increases DA signalling by preventing ___

A

DA re-uptake

38
Q

amphetamines increase DA signalling by increasing ___

A

DA release into synapse

39
Q

amphetamines and cocaine influence the storage and re-uptake of ___ in presynaptic neurons

A

NE

40
Q

how do amphetamines make NE be released from neurons?

A

bind to catecholamine transporters to be brought into NE vesicles until there is no room for NE and it gets pushed out into the cytoplasm, reaches such high levels that the NET lets it out into the synapse w/o energy required

41
Q

how does cocaine increase NE levels?

A

blocks the NET so NE cant be taken back up into the presynaptic neuron, so it has a longer duration of action

42
Q

t/f what amphetamines and cocaine do to NE, they also do to DA

A

treu

43
Q

cociane acts on ___ tp prevent DA re-uptake by presynaptic neuron

A

DAT

44
Q

t/f derivatives of amphetamines can be used to treat ADHD

A

t

45
Q

ADHD is thought to involve reduced levels of __ and ___

A

DA and NE

46
Q

t/f effects of amphetamines are opposite in patients with ADHD

A

t

47
Q

cocaine is used as an anesthetic in some parts of the world bc of its ability to block ___channels

A

Na

48
Q

if cociane is more pure, it will make the gums ___

A

tingle and possibly go numb

49
Q

the intoxicating effects of drugs are based on what 2 factors?

A

how much and how fast the drug gets into the CNS

50
Q

compare snorted and smoked (crack) cocaine in terms of peak blood concentration and onset time

A

crack has faster onset with lower peak concentration compared to nasal

51
Q

the white fluffy powder form of coccaineis the ___ form

A

hydrochloride salt

52
Q

what type of cocaine can be injected? how?

A

the white fluffy hydrochloride salt form which is ionized and can be dissolved in water to be injected

53
Q

what is the “downside” of snorting the ionized form of cocaine?

A

ionized form has less optimal absorption across membrane

54
Q

the free base form of cocaine is more known as ___

A

crack

55
Q

which is better absorbed across membranes, crack or fluffy cocaine?

A

crack b/c its more neutral and not ionized

56
Q

heroin has a much higher ability to accumulate in the CNS compared to morphine due to a small change in the ___

A

chemical structure

57
Q

heroin is a ___opiod also known as diacetylmorphine

A

semi-synthetic

58
Q

what is the structural change between heroin and morphine that makes heroine better absorbed across the BBB?

A

heroin has acetyl groups added to the hydroxyl groups, making it less polar so it dissolves across the lipphillic BBB better

59
Q

once in the CNS, heroin is ___ to exert its effect

A

deacetylated

60
Q

t/f heroin can be metabolized to morphine in the periphery which reduces its crossing of BBB when given orally

A

t

61
Q

Fentanyl is a ____ opioid with a very different structure from heroin and morphine

A

fully synthetic

62
Q

Fentanyl has a much higher LogP values, therefore its crossing of the BBB is much ___ (higher/lower) than heroin and morphine

A

higher

63
Q

fentanyl has a much higher affinity for the ___receptor, making it much more likely to experience an overdose

A

mu opioid

64
Q

t/f fentanyl is very cheap to produce and many people have overdose bc their drugs have been laced with fentanyl

A

true

65
Q

Naltrexone MOA

A

opioid antagonist that quickly reverse life threatening respiratory suppression during an acute opioid overdose

66
Q

why cant opioid antagonists like Naltrexone be used to help patients with chronic opioid use?

A

worsen withdrawal effects that will go away as soon as an opioid is used, so could make patients want to use opioid more that if they quit cold turkey

67
Q

what are the withdrawal symptoms for opioids?

A

chills, muscle aches, vomiting, diarrhea, anxiety, hostility

68
Q

what is a good treatment for helping patients stop opioid use?

A

a long acting opioid agonists with a slow onset so there is less addictive rush

69
Q

Methadoen MOA

A

long-acting opioid agonist commonly used in treatment of opioid use disorder

70
Q

Buprenorphine MOA

A

partial agonist of Mu opioid receptor that has slow action and also competes out full opioid agonists

.Pharmacology (55 decks)

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