Psychopharmacology Flashcards
1
Q
What receptor does ondansetron target?
A
5HT-3 (antagonist)
2
Q
What receptor does granisetron target?
A
5-HT3 (antagonist)
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
4
Q
What is a common side effect of 5-HT3 receptor antagonists?
A
Constipation
5
Q
Where is the common site of action of 5-HT3 antagonists?
A
Chemoreceptor trigger zone area of medulla oblongata
6
Q
What is the active metabolite of diazepam?
A
Desmethyldiazepam
7
Q
What is the active metabolite of dothiepin?
A
Dothiepinsulfoxide
8
Q
What is the active metabolite of fluoxetine?
A
Norfluoxetine
9
Q
What is the active metabolite of imipramine?
A
Desimipramine
10
Q
What is the active metabolite of risperidone?
A
9-Hydroxyrisperidone
11
Q
What is the active metabolite of amitriptyline?
A
Nortriptyline
12
Q
What is the active metabolite of codeine?
A
Morphine
13
Q
What name is given to a drug that when administered is inactive?
A
Prodrug
14
Q
What name is given to the substance that a prodrug is metabolised into?
A
Active metabolite
15
Q
What is the active metabolite of lisdexamfetamine?
A
Dexamfetamine
16
Q
Is lisdexamfetamine a stimulant or non-stimulant?
A
Stimulant
17
Q
Is dexamfetamine a stimulant or non-stimulant?
A
Stimulant
18
Q
Is methylphenidate a stimulant or non-stimulant?
A
Stimulant
19
Q
Is atomoxetine a stimulant or non-stimulant?
A
Non-stimulant
20
Q
Is guanfacine a stimulant or non-stimulant?
A
Non-stimulant
21
Q
Is clonidine a stimulant or non-stimulant?
A
Non-stimulant
22
Q
What is the hypothesised mechanism of dexamfetamine and lisdexamfetamine in ADHD?
A
Increase synaptic levels of dopamine and noradrenaline
23
Q
What is the hypothesised mechanism of methylphenidate in ADHD?
A
Increases synaptic levels of dopamine and noradrenaline
24
Q
What is the hypothesised mechanism of atomoxetine in ADHD?
A
Increases synaptic levels of noradrenaline
25
What is the hypothesised mechanism of guanfacine in ADHD?
Selective agonist of alpha-2A adrenergic receptors. Binds to post-synaptic alpha-2A receptors mimicking noradrenaline.
26
What is the hypothesised mechanism of clonidine in ADHD?
Agonist of alpha-2A adrenergic receptors mimicking noradrenaline.
27
What is the overall hypothesised mechanism of action of drugs used to manage ADHD?
Mediated through action of noradrenaline (and dopamine, but mainly noradrenaline) in prefrontal cortex.
28
ADHD drug(s) contraindicated in significant cardiovascular disorders?
Lis/dexamfetamine
Methylphenidate
Atomoxetine
Clonidine - specifically bradyarrhythmias (sick sinus or AV block of 2nd or 3rd degree)
29
Which ADHD medication is specifically contraindicated in bradyarrhythmias (sick sinus or AV block of 2nd or 3rd degree)?
Clonidine
30
Which ADHD medication's only contraindication is sensitivity to the drug itself?
Guanfacine
31
ADHD drug(s) contraindicated in cerebrovascular disorders?
Lis/dexamfetamine
Methylphenidate
Atomoxetine
32
ADHD drug(s) contraindicated in glaucoma?
Lis/dexamfetamine
Methylphenidate
Atomoxetine
33
ADHD drug(s) contraindicated in concurrent use of MAO-inhibitors?
Lis/dexamfetamine
Methylphenidate
Atomoxetine
34
ADHD drug(s) contraindicated in patients with history of drug abuse?
Lis/dexamfetamine
Methylphenidate
35
ADHD drug(s) contraindicated in patients with hypertension?
Lis/dexamfetamine
Methylphenidate
36
ADHD drug(s) contraindicated in patients with hyperthyroidism?
Lis/dexamfetamine
Methylphenidate
37
ADHD drug(s) contraindicated in patients with psychosis or poorly controlled bipolar I
Lis/dexamfetamine
Methylphenidate
38
Common (1/10) side effects of lis/dexamfetamine
Decreased appetite
In children, reduced weight gain and weight loss
Nervousness
Insomnia
39
Bupropion - stimulant or non-stimulant?
Non-stimulant
40
Hypothesised mechanism of action of bupropion in ADHD?
Blocks presynaptic uptake of noradrenaline and dopamine
41
Common (1/10) side effects of methylphenidate?
Decreased appetite
Insomnia
Nervousness
Headache
Nausea
Dry mouth
42
Common (1/10) side effects of atomoxetine?
Decreased appetite
Headache
Somnolence
Abdo pain (epigastric discomfort)
Nausea
Vomiting
Increased BP
Increased HR
43
Common (1/10) side effects of guanfacine?
Somnolence
Headache
Fatigue
Abdo pain
44
In adverse drug reactions what is a Type A reaction?
Pharmacological reaction
45
In adverse drug reactions what is a Type B reaction?
Idiosyncratic reaction
46
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'?
Type A - pharmacological reaction
47
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'?
Type B - idiosyncratic reaction
48
What percentage of adverse drug reactions do Type A reactions account for?
80%
49
Are the Gell and Coombs allergic reactions examples of Type A or Type B adverse drug reactions?
Type B
50
Which allergic reaction is IgE-mediated?
Type I
51
Which allergic reaction is cytotoxic?
Type II
52
Which allergic reaction is immune-complex?
Type III
53
Which allergic reaction is cell-mediated?
Type IV
54
Which allergic reaction is described by: 'these are immediate hyper-sensitivity reactions mediated by the IgE antibody'?
Type I, IgE
55
Which allergic reaction is described by 'these involve the activation of complement proteins and destruction of cells by antibodies'?
Type II, cytotoxic
56
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'?
Type III, immune complex
57
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'?
Type IV, cell-mediated
58
Which receptors does agomelatine target?
Agonist at melatonin M1 and M2 receptors.
Antagonist at 5HT2C receptors.
59
What is agomelatine's clinical application?
Depression
60
What is the mechanism of action of agomelatine?
Melatonin effects promote sleep.
5HT2C antagonism leads to release of dopamine and noradrenaline in the prefrontal cortex.
61
Does agomelatine affect serotonin levels?
No.
62
Define a partial agonist
Produces the biological response but cannot produce 100% of the response, even at high doses.
62
Define an agonist
A compound that binds to a receptor and produces the biological response
63
Define antagonist
Antagonists block the effects of agonists. They have no effect on their own.
64
Define competitive antagonist
Competitive antagonists bind to the receptor in a reversible way without affecting a biological response. They make the agonist look less potent.
65
Define inverse agonist
Have opposite effects to full agonists.
NB. not the same as an antagonist which blocks the effects of agonists and inverse agonists.
66
Define full agonists
Displays full efficacy (100% biological response) at the receptor
67
What is an agonist-antagonist?
Binds to certain receptors and acts as an agonist and binds to other receptors where it acts as an antagonist
68
What is the most common form of dementia in the UK?
Alzheimer's
69
What percentage of Alzheimer's cases are inherited via an autosomal dominant pattern of inheritance?
5%
70
Name three genes implicated in inherited Alzheimer's
Amyloid precursor protein (chromosome 21)
Presenilin 1 (chromosome 14)
Presenilin 2 (chromosome 1)
71
What does apolipoprotein E allele E4 encode?
Cholesterol transport protein
72
What are the pathological macroscopic changes seen in Alzheimer's?
Widespread cerebral atrophy, especially involving the cortex and hippocampus
73
What are the pathological microscopic changes seen in Alzheimer's?
Cortical plaques due to deposition of type-A beta-amyloid protein and intraneuronal neurofibrillary tangles caused by aggregation of the tau protein
74
What are the pathological biochemical changes seen in Alzheimer's?
Reduced acetylcholine due to damage to ascending forebrain projection
75
What are neurofibrillary tangles?
Paired helical filaments partly made from a protein called tau.
76
What characterises the neurofibrillary tangles in Alzheimer's?
Excessively phosphorylated
77
What is the NICE guidance for medication for mild-moderate Alzheimer's disease?
Acetylcholinesterase inhibitor: donepezil, galantamine or rivastigmine.
78
What drug can be used for moderate to severe Alzheimer's disease?
79
What type of amines are first generation tricyclic antidepressants and second generation tricyclic antidepressants?
First generation TCAs = tertiary amines
Second generation TCAs = secondary amines
80
What neurotransmitter is affected by secondary amines?
Noradrenaline
81
What neurotransmitter(s) is affected by tertiary amines?
Noradrenaline and serotonin
82
What is the presumed benefit of second generation TCAs over first generation TCAs?
Lower side effect profile as second generation act on noradrenaline, whereas first generation also impact serotonin
83
Name 4 secondary amines (second generation TCAs)
Desimipramine
Nortriptyline
Protriptyline
Amoxapine
84
Name 8 tertiary amines (first generation TCAs)
Amitriptyline
Lofepramine
Imipramine
Clomipramine
Dosulepin (dothiopin)
Doxepin
Trimipramine
Butriptyline
85
What are anabolic steroids?
Synthetic derivatives of testosterone
86
What is meant by anabolic and androgenic properties of steroids?
Anabolic - tissue forming
Androgenic - masculinising
87
What type of drug is nandrolone?
Anabolic steroid
88
What type of drug is stanozolol?
Anabolic steroid
89
