Psychopharmacology Flashcards

1
Q

What receptor does ondansetron target?

A

5HT-3 (antagonist)

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2
Q

What receptor does granisetron target?

A

5-HT3 (antagonist)

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3
Q

What functional class do ondansetron and granisetron belong to, and what is their common clinical application?

A

Anti-emetics

Management of chemotherapy-associated nausea

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4
Q

What is a common side effect of 5-HT3 receptor antagonists?

A

Constipation

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5
Q

Where is the common site of action of 5-HT3 antagonists?

A

Chemoreceptor trigger zone area of medulla oblongata

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6
Q

What is the active metabolite of diazepam?

A

Desmethyldiazepam

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7
Q

What is the active metabolite of dothiepin?

A

Dothiepinsulfoxide

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8
Q

What is the active metabolite of fluoxetine?

A

Norfluoxetine

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9
Q

What is the active metabolite of imipramine?

A

Desimipramine

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10
Q

What is the active metabolite of risperidone?

A

9-Hydroxyrisperidone

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11
Q

What is the active metabolite of amitriptyline?

A

Nortriptyline

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12
Q

What is the active metabolite of codeine?

A

Morphine

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13
Q

What name is given to a drug that when administered is inactive?

A

Prodrug

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14
Q

What name is given to the substance that a prodrug is metabolised into?

A

Active metabolite

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15
Q

What is the active metabolite of lisdexamfetamine?

A

Dexamfetamine

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16
Q

Is lisdexamfetamine a stimulant or non-stimulant?

A

Stimulant

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17
Q

Is dexamfetamine a stimulant or non-stimulant?

A

Stimulant

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18
Q

Is methylphenidate a stimulant or non-stimulant?

A

Stimulant

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19
Q

Is atomoxetine a stimulant or non-stimulant?

A

Non-stimulant

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20
Q

Is guanfacine a stimulant or non-stimulant?

A

Non-stimulant

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21
Q

Is clonidine a stimulant or non-stimulant?

A

Non-stimulant

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22
Q

What is the hypothesised mechanism of dexamfetamine and lisdexamfetamine in ADHD?

A

Increase synaptic levels of dopamine and noradrenaline

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23
Q

What is the hypothesised mechanism of methylphenidate in ADHD?

A

Increases synaptic levels of dopamine and noradrenaline

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24
Q

What is the hypothesised mechanism of atomoxetine in ADHD?

A

Increases synaptic levels of noradrenaline

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25
Q

What is the hypothesised mechanism of guanfacine in ADHD?

A

Selective agonist of alpha-2A adrenergic receptors. Binds to post-synaptic alpha-2A receptors mimicking noradrenaline.

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26
Q

What is the hypothesised mechanism of clonidine in ADHD?

A

Agonist of alpha-2A adrenergic receptors mimicking noradrenaline.

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27
Q

What is the overall hypothesised mechanism of action of drugs used to manage ADHD?

A

Mediated through action of noradrenaline (and dopamine, but mainly noradrenaline) in prefrontal cortex.

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28
Q

ADHD drug(s) contraindicated in significant cardiovascular disorders?

A

Lis/dexamfetamine
Methylphenidate
Atomoxetine
Clonidine - specifically bradyarrhythmias (sick sinus or AV block of 2nd or 3rd degree)

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29
Q

Which ADHD medication is specifically contraindicated in bradyarrhythmias (sick sinus or AV block of 2nd or 3rd degree)?

A

Clonidine

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30
Q

Which ADHD medication’s only contraindication is sensitivity to the drug itself?

A

Guanfacine

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31
Q

ADHD drug(s) contraindicated in cerebrovascular disorders?

A

Lis/dexamfetamine
Methylphenidate
Atomoxetine

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32
Q

ADHD drug(s) contraindicated in glaucoma?

A

Lis/dexamfetamine
Methylphenidate
Atomoxetine

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33
Q

ADHD drug(s) contraindicated in concurrent use of MAO-inhibitors?

A

Lis/dexamfetamine
Methylphenidate
Atomoxetine

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34
Q

ADHD drug(s) contraindicated in patients with history of drug abuse?

A

Lis/dexamfetamine
Methylphenidate

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35
Q

ADHD drug(s) contraindicated in patients with hypertension?

A

Lis/dexamfetamine
Methylphenidate

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36
Q

ADHD drug(s) contraindicated in patients with hyperthyroidism?

A

Lis/dexamfetamine
Methylphenidate

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37
Q

ADHD drug(s) contraindicated in patients with psychosis or poorly controlled bipolar I

A

Lis/dexamfetamine
Methylphenidate

38
Q

Common (1/10) side effects of lis/dexamfetamine

A

Decreased appetite
In children, reduced weight gain and weight loss
Nervousness
Insomnia

39
Q

Bupropion - stimulant or non-stimulant?

A

Non-stimulant

40
Q

Hypothesised mechanism of action of bupropion in ADHD?

A

Blocks presynaptic uptake of noradrenaline and dopamine

41
Q

Common (1/10) side effects of methylphenidate?

A

Decreased appetite
Insomnia
Nervousness
Headache
Nausea
Dry mouth

42
Q

Common (1/10) side effects of atomoxetine?

A

Decreased appetite
Headache
Somnolence
Abdo pain (epigastric discomfort)
Nausea
Vomiting
Increased BP
Increased HR

43
Q

Common (1/10) side effects of guanfacine?

A

Somnolence
Headache
Fatigue
Abdo pain

44
Q

In adverse drug reactions what is a Type A reaction?

A

Pharmacological reaction

45
Q

In adverse drug reactions what is a Type B reaction?

A

Idiosyncratic reaction

46
Q

What type of adverse drug reaction is described by ‘these drug reactions can be predicted based on the known pharmacology of the drug. They are typically dose-dependent and reversible upon discontinuing the medication’?

A

Type A - pharmacological reaction

47
Q

What type of adverse drug reaction is described by ‘these reactions cannot be predicted from the known pharmacology of the drug. They are often unrelated to the drug’s intended pharmacological action. Allergic reactions fall into this category’?

A

Type B - idiosyncratic reaction

48
Q

What percentage of adverse drug reactions do Type A reactions account for?

A

80%

49
Q

Are the Gell and Coombs allergic reactions examples of Type A or Type B adverse drug reactions?

A

Type B

50
Q

Which allergic reaction is IgE-mediated?

A

Type I

51
Q

Which allergic reaction is cytotoxic?

A

Type II

52
Q

Which allergic reaction is immune-complex?

A

Type III

53
Q

Which allergic reaction is cell-mediated?

A

Type IV

54
Q

Which allergic reaction is described by: ‘these are immediate hyper-sensitivity reactions mediated by the IgE antibody’?

A

Type I, IgE

55
Q

Which allergic reaction is described by ‘these involve the activation of complement proteins and destruction of cells by antibodies’?

A

Type II, cytotoxic

56
Q

Which allergic reaction is described by ‘antigen-antibody aggregates can form and deposit in tissues, leading to inflammation. This can manifest as conditions such as serum sickness or drug-induced lupus’?

A

Type III, immune complex

57
Q

Which allergic reaction is described by ‘these reactions are mediated by T cells and occur over a delayed period, often days to weeks after exposure to the drug. Contact dermatitis and some forms of drug-induced hepatitis are examples’?

A

Type IV, cell-mediated

58
Q

Which receptors does agomelatine target?

A

Agonist at melatonin M1 and M2 receptors.
Antagonist at 5HT2C receptors.

59
Q

What is agomelatine’s clinical application?

A

Depression

60
Q

What is the mechanism of action of agomelatine?

A

Melatonin effects promote sleep.
5HT2C antagonism leads to release of dopamine and noradrenaline in the prefrontal cortex.

61
Q

Does agomelatine affect serotonin levels?

A

No.

62
Q

Define a partial agonist

A

Produces the biological response but cannot produce 100% of the response, even at high doses.

62
Q

Define an agonist

A

A compound that binds to a receptor and produces the biological response

63
Q

Define antagonist

A

Antagonists block the effects of agonists. They have no effect on their own.

64
Q

Define competitive antagonist

A

Competitive antagonists bind to the receptor in a reversible way without affecting a biological response. They make the agonist look less potent.

65
Q

Define inverse agonist

A

Have opposite effects to full agonists.

NB. not the same as an antagonist which blocks the effects of agonists and inverse agonists.

66
Q

Define full agonists

A

Displays full efficacy (100% biological response) at the receptor

67
Q

What is an agonist-antagonist?

A

Binds to certain receptors and acts as an agonist and binds to other receptors where it acts as an antagonist

68
Q

What is the most common form of dementia in the UK?

A

Alzheimer’s

69
Q

What percentage of Alzheimer’s cases are inherited via an autosomal dominant pattern of inheritance?

A

5%

70
Q

Name three genes implicated in inherited Alzheimer’s

A

Amyloid precursor protein (chromosome 21)
Presenilin 1 (chromosome 14)
Presenilin 2 (chromosome 1)

71
Q

What does apolipoprotein E allele E4 encode?

A

Cholesterol transport protein

72
Q

What are the pathological macroscopic changes seen in Alzheimer’s?

A

Widespread cerebral atrophy, especially involving the cortex and hippocampus

73
Q

What are the pathological microscopic changes seen in Alzheimer’s?

A

Cortical plaques due to deposition of type-A beta-amyloid protein and intraneuronal neurofibrillary tangles caused by aggregation of the tau protein

74
Q

What are the pathological biochemical changes seen in Alzheimer’s?

A

Reduced acetylcholine due to damage to ascending forebrain projection

75
Q

What are neurofibrillary tangles?

A

Paired helical filaments partly made from a protein called tau.

76
Q

What characterises the neurofibrillary tangles in Alzheimer’s?

A

Excessively phosphorylated

77
Q

What is the NICE guidance for medication for mild-moderate Alzheimer’s disease?

A

Acetylcholinesterase inhibitor: donepezil, galantamine or rivastigmine.

78
Q

What drug can be used for moderate to severe Alzheimer’s disease?

A
79
Q

What type of amines are first generation tricyclic antidepressants and second generation tricyclic antidepressants?

A

First generation TCAs = tertiary amines
Second generation TCAs = secondary amines

80
Q

What neurotransmitter is affected by secondary amines?

A

Noradrenaline

81
Q

What neurotransmitter(s) is affected by tertiary amines?

A

Noradrenaline and serotonin

82
Q

What is the presumed benefit of second generation TCAs over first generation TCAs?

A

Lower side effect profile as second generation act on noradrenaline, whereas first generation also impact serotonin

83
Q

Name 4 secondary amines (second generation TCAs)

A

Desimipramine
Nortriptyline
Protriptyline
Amoxapine

84
Q

Name 8 tertiary amines (first generation TCAs)

A

Amitriptyline
Lofepramine
Imipramine
Clomipramine
Dosulepin (dothiopin)
Doxepin
Trimipramine
Butriptyline

85
Q

What are anabolic steroids?

A

Synthetic derivatives of testosterone

86
Q

What is meant by anabolic and androgenic properties of steroids?

A

Anabolic - tissue forming
Androgenic - masculinising

87
Q

What type of drug is nandrolone?

A

Anabolic steroid

88
Q

What type of drug is stanozolol?

A

Anabolic steroid

89
Q
A