PHARM - Drugs of Abuse - Week 9 Flashcards

1
Q

Why does dependence to drugs occur?

A

Progressive pharmacological adaptation to the drug, resulting in tolerance

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2
Q

What happens to homeostasis in response to repeated drug exposure? What is a consequence of this?

A

It is reset. An individual in this state needs continuous drug administration to maintain normal function.

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3
Q

If there is a dependence on drugs, what happens if the drug is abruptly stopped?

A

Withdrawal symptoms occur

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4
Q

Define abstinence.

A

Practice of not doing something or having something that is wanted or enjoyable

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5
Q

Define psychological dependence, including the physiological basis for it, and what normally happens in individuals with no dependence.

A

Also called addiction - administration of substances or certain behaviours activate brain reward circuits.
These motivate normal behaviour which most people enjoy without being compelled to repeat them.

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6
Q

What occurs with reflexice acivation of reward circuits?

A

It becomes involuntary, drawing a person into compulsive repetition and putting focus on the immediate pleasure despite negative consequences.

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7
Q

Where is the primary action of drugs of abuse?

A

In the CNS - the brain reward circuits

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8
Q

What system specifically do addictive drugs activate? What consequence does this result in?

A

The mesolimbic dopamine system, producing a rewarding-reinforcing action.

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9
Q

What effect does alcohol have on the CNS?

A

Depressant

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10
Q

What neurotransmitter does alcohol bind to and increases transmission of what neurotransmitter?

A

Binds to GABA and increases GABA-ergic transmission

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11
Q

What two neurotransmitter receptors are altered by alcohol?

A

NMDA and 5-HT3 (serotonin)

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12
Q

Is alcohol rapidly or slowly absorbed and distributed?

A

Rapid

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13
Q

Describe how alcohol is processed by the body in terms of percentages (5).

A

90% is oxidised in the liver

The rest is eliminated via saliva, sweat, breath, and urine

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14
Q

Can an overdose of alcohol be fatal? Explain why.

A

Yes, due to the effects of being a depressant and acetaldehyde (a metabolite)

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15
Q

After what time period following cessation of heavy drinking does the dependence on alcohol become apparent?

A

6-12 hours

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16
Q

Name 5 withdrawal symptoms of alcohol after 6-12 hours.

A
Hand tremors
Nausea
Excessive sweating
Agitation
Anxiety
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17
Q

Name a withdrawal symptom of alcohol after 12-24 hours (1).

A

In some individuals, visual/tactile/auditory hallucinations may occur

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18
Q

Name a withdrawal symptom of alcohol after 24-48 hours (1).

A

In some individuals, siezures may occur

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19
Q

Name a withdrawal symptom of alcohol after 48-72 hours. What percentage of mortality is it associated with?

A

Delirium - 5-15% mortality

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20
Q

What is the standard first-line treatment for acute alcohol withdrawal symptoms?

A

Benzodiazepines

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21
Q

What is naltrexone and what does it prevent? How long is its action?

A

An opioid receptor antagonist
Prevents euphoria
Long action - 24-72h

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22
Q

How does naltrexone work (2)?

A

Blocks action of the endogenous opioids released by alcohol

Blocks activation of dopamine reward pathways

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23
Q

What overall effect will naltrexone have (2)?

A

Decreases pleasurable effects linked to alcohol consumption

Reduces cravings

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24
Q

Name 4 common adverse effects and one serious but rare adverse effect of naltrexone.

A
Insomnia
Headache
Fatigue
Dizziness
Hepatotoxicity
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25
Q

What must be monitored during naltrexone therapy?

A

Liver function

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26
Q

What does disulphiram promote?

A

Abstinence in motivated alcoholics after initial detoxification

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27
Q

What is disulphiram?

A

Aldehyde dehydrogenase inhibitor

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28
Q

How does disulphiram work (2)?

A

Blocks degradation of acetaldehyde to acetate

Acetaldehyde accumulates in the body and casues unpleasant symptoms

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29
Q

Name 7 symptoms of disulphiram and a reason why if applicable.

A
Intense flushing
Headache (throbbing)
Sweating
The above are caused due to acetaldehyde being a potent vasodilator
Nausea
Vomiting
BP changes
Hyperventilation
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30
Q

When is acamprosate used?

A

Maintenance of abstinence in alcohol dependence

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31
Q

What effect does acamprosate have on the CNS (2)?

A

Restores normal activity in glutamate and GABA systems.

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32
Q

How long does acamprosate therapy last?

A

Up to a year

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33
Q

What should be checked before acamprosate therapy?

A

Creatinine levels

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34
Q

Name 3 side effects of acamprosate.

A

Rash
Diarrhoea
Changes in libido

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35
Q

What addiction exceeds all others?

A

Nicotine addiction

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36
Q

What does nicotine cause the release of? Give 3 consequences of this. What do these 3 increase the risk of?

A

Catecholamine release
Increases heart rate, vascular resistance, and hypertension
Increases risk for coronary artery disease

37
Q

What do catecholamines stimulate the mobilisation of?

A

Free fatty acids

38
Q

How does nicotine affect LDLs and HDLs?

A

Increases LDLs and decreases LDLs

39
Q

Mechanistically, how does nicotine act?

A

Acts as a nAChR agonist, increasing dopamine neuron activity

40
Q

How do nicotine patches work?

A

Patch impregnated with nicotine, which provides slow absorption into the circulation.
Heps reduce cravings.

41
Q

How does bupropion aid nicotine addiction?

A

Inhibits noradrenaline and dopamine re-uptake

42
Q

Name 6 side effects of bupropion.

A
Insomnia
Agitation
Anxiety
Visual disturbances
Impaired concentration
Rash
43
Q

What are opioids used for typically?

A

Treatment of pain

44
Q

What do opioids do in addition to reducing the perception of pain?

A

Produce a state of well-being or euphoria

45
Q

What is the most frequently abused opioid?

A

Heroid (diacetylmorphine)

46
Q

What kind of drug is heroin (aside from being an opioid)?

A

Prodrug

47
Q

What is heroin metabolised to?

A

Morphine

48
Q

Why is heroin more effective than morphine (2)?

A

Greater lipid solubility - crosses the blood brain barrier more rapidly

49
Q

Why does heroin cause respiratory depression?

A

It inhibits brainstem respiratory mechanisms

50
Q

Name 6 adverse effects of heroin.

A
Antitussive effect
Miosis
Bradycardia
Nausea
Vomiting
Constipation
51
Q

What are opioids agonists of?

A

G-protein coupled opioid receptors

52
Q

Which receptor do heroin, morphine, codeine, and oxycodone act on?

A

μ receptor

53
Q

Do all opioids induce tolerance and dependence upon cessation?

A

Yesd

54
Q

What kind of drug is used for opioid overdose?

A

Opioid antagonists

55
Q

Give an example of an opioid antagonist, what kind of overdose it is used to treat, and how quickly it acts.

A

Naloxone, short acting so used for acute opioid overdose

56
Q

What is the main active constituent in cannabinoids?

A

THC

57
Q

Name 4 beneficial therapeutic effects of THC (5).

A

Anti-emetic
Muscle relaxing effects
Improves seizure control in patients with epilepsy
Useful for anorexia linked to weight loss in cancer patients and patients infected with HIV (cachexia)

58
Q

What is the main CNS action of THC? Name 2 effects this can have.

A

CB1 receptor

Can cause loss of coordination and painful muscle spasms

59
Q

What kind of a drug is cocaine?

A

Psychostimulant and hallucinogen

60
Q

Name three kinds of psychostimulants.

A

Cocaine

Ice Speed

61
Q

What three effects do psychostimulants have?

A

Procudes excitement
Euphoria
Decreases fatigue

62
Q

Name 4 hallucinogens.

A

LSD
PCP
Ecstasy
GHB (liquid ecstasy)

63
Q

Are hallucinogens addictive?

A

No, theyre non-addictive drugs of abuse

64
Q

Where do hallucinogens typically target?

A

Cortical and thalaic circuits rather than mesolimbic dopamine ones.

65
Q

What do psychostimulants and hallucinogens interfere with?

A

Multiple neurotransmitter and receptor systems

66
Q

In what three ways can cocaine be administered?

A

Injected
Snorted
Smoked

67
Q

Is cocaine rapidly or slowly absorbed?

A

Rapid

68
Q

Does cocaine cause CNS or PNS effects?

A

Both

69
Q

What does cocaine block the uptake of (3)?

A

Neuronal uptake of dopamine, noradrenaline, and serotonin

70
Q

What happens following a dose of cocaine (3)?

A

Intense euphoria
Dysphoria/irritability
Craving for more drug

71
Q

Name 5 symptoms of cocaine overdose.

A
Acute fear
Psychotic symptoms
Hypertension
Tachycardia
Coronary vasospasm
72
Q

Describe the mechanisms of amphetamines (2).

A

Acts as a competitive inhibitor reducing uptake of noradrenaline and dopamine

73
Q

How do amphetamines enter neurons?

A

By uptake or diffusion

74
Q

What do amphetamines do once inside the cell (3)?

A

Interact with VMAT and inhibit uptake of dopamine and noradrenaline into vesicles

75
Q

What is LSD an agonist of and what does it increase transmission of?

A

Agonist of serotonin, increases glutaminergic transmission

76
Q

What does LSD inhibit and where?

A

Inhibits 5-HT neurons from firing in raphe nuclei

77
Q

What is PCP? Give its common name.

A

Phencyclidine - angel dust

78
Q

What is PCP and antagonist to?

A

Glutamate NMDA-receptor

79
Q

What four effects does PCP have on neurotransmitters?

A

Inhibits uptake of dopamine, noradrenaline, and serotonin

Stimulates dopamine release

80
Q

What four behavioural effects does PCP have?

A

Euphoria
Excitation
Dysphoria
Aggression

81
Q

What can chronic use of PCP lead to? Is it reversible or irreversible?

A

Irreversible schizophrenia-like psychosis

82
Q

What is the common name for MDMA?

A

Ecstasy

83
Q

What two neurotransmitters does MDMA stimulate the release of?

A

Dopamine and serotonin

84
Q

What four things does MDMA affect?

A

Mood, sleep, memory, and apetite

85
Q

What does acute toxicity of MDMA cause?

A

Hyperthermia

86
Q

What is meant by serotonin syndrome, what drug is it caused by, and is it fatal?

A

Hyperserotoninergic state caused by MDMA

May be fatal

87
Q

Name 12 symptoms of serotonin syndrome.

A
Abnormal muscle movements
Muscle rigidity
Sweating
Disruption in thermoregulation
Confusion
Agitation
Restlessness
Hallucinations
Tachycardia
Hypertension
Loss of control
Death
88
Q

What is a common date rape drug and why?

A

GHB - it is an odourless liquid that readily mixes with alcohol
Causes euphoria, enhanced safety perceptions, social closeness, amnesia, then sedation/coma