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DEN 2026 - Pharmacology > Antidepressants, Anxiolytics and Parkinson's Disease > Flashcards

Antidepressants, Anxiolytics and Parkinson's Disease Flashcards

1
Q

What is depression?

A

A pathological mood state with persistent and pervasive symptoms present for at least 2 weeks

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2
Q

Describe the possible role for serotonin (5-HT) in depression

A
  • Serotonin is neurotransmitter
  • Pathways widespread in brain
  • Primary involved in expression and emotion regulation
  • Abnormal levels in depression
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3
Q

Describe a simple version of the monoamine hypothesis

A

Depression is caused by a functional deficiency of monoamines

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4
Q

Give 2 examples of monoamines

A
  1. Serotonin

2. Noradrenaline

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5
Q

Name 5 categories of antidepressants

A
  1. SSRIs (selective serotonin reuptake inhibitors)
  2. SNRIs (serotonin and noradrenaline reuptake inhibitors)
  3. NaSSAs (noradrenergic and specific serotinergic antidepressants)
  4. Tricyclic Antidepressants
    MAOIs (monoamine reuptake inhibitors)
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6
Q

Name 4 examples of SSRI drugs

A
  1. Sertraline
  2. Fluoxetine
  3. Citalopram
  4. Escitalopram
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7
Q

Describe SSRIs mode of action

A
  • Prevent reuptake of serotonin back into presynaptic bulb
  • Increases volume of serotonin in cleft
  • Increase post synaptic firing
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8
Q

Give an overview of the adverse effects of SSRIs

A
  • Generally well tolerated
  • Relatively safe in overdose
  • First line treatment (NICE)
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9
Q

Name 5 side effects of SSRIs

A
  1. Nausea / vomiting
  2. Headache
  3. Agitation / anxiety
  4. Hyponatraemia
  5. Insomnia
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10
Q

Name 3 types of drugs SSRIs interact with

A
  1. St John’s Wort
  2. Other antidepressants
  3. CYP enzyme inhibitors
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11
Q

What is a possible effect of a drug interaction of citalopram / escitalopram?

A

QT prolongation

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12
Q

Name 2 examples of SNRI drugs

A
  1. Venlafaxine

2. Duloxetine

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13
Q

Describe SNRIs mode of action

A
  • Prevent reuptake of serotonin and noradrenaline back into presynaptic bulb
  • Increases volume of serotonin and noreadrenaline in cleft
  • Increase post synaptic firing
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14
Q

Name 5 side effects of SSRIs

A
  1. Nausea / vomiting
  2. Headache
  3. Agitation / anxiety
  4. Hyponatraemia
  5. Insomnia
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15
Q

Name 3 types of drugs SSRIs interact with

A
  1. St John’s Wort
  2. Other antidepressants
  3. CYP enzyme inhibitors
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16
Q

Name an example of an NaSSA drug

A

Mirtazapine

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17
Q

What is the function of homeostatic autoreceptors?

A

Regulate release of neurotransmitter into synaptic cleft

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18
Q

Describe 2 mechanisms of action for NaSSAs

A
  1. NaSSAs block α-2 auto receptors blocking negative feedback mechanism which increases noradrenaline release
  2. Antagonises 5-HT2 and 5-HT3 receptors which increases agonism at 5-HT1 receptors
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19
Q

Name 4 common side effects of mirtazapine

A
  1. Drowsiness
  2. Increased appetite / weight gain
  3. Dizziness
  4. Potential for blood dyscrasia
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20
Q

Name 4 tricyclic antidepressants

A
  1. Amitriptyline
  2. Clomipramine
  3. Lofepramine
  4. Dosulepin
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21
Q

Describe the mode of action of tricyclic antidepressants

A
  • Prevent reuptake of serotonin and noradrenaline back into presynaptic bulb by blocking reuptake transporters
  • Increases volume of serotonin and noradrenaline in cleft
  • Increase post synaptic firing
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22
Q

Give a general overview of tricyclic safety profile

A
  • Less well tolerated than other antidepressants
  • Potentially fatal in overdose
  • Not recommended first line
  • Dangerous in combination with other antidepressants or St John’s Wort
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23
Q

Name 3 general side effects of tricyclics

A
  1. Nausea
  2. Vomiting
  3. Headache
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24
Q

Name 2 side effects of tricyclics caused by action at histamine receptor

A
  1. Sedation

2. Hangover

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25
Q

Name 3 side effects of tricyclics caused by α-1 receptor antagonism

A
  1. Postural hypotension
  2. Tachycardia
  3. Arrhythmia
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26
Q

Name 4 side effects of tricyclics caused by action as an anticholinergic

A
  1. Dry mouth
  2. Blurred vision
  3. Constipation
  4. Urinary retention
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27
Q

Name a reversible MAOI

A

Moclobemide

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28
Q

Name 2 irreversible MAOIs

A
  1. Phenylzine

2. Tranylcypromine

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29
Q

Describe the mode of action of MAOIs

A
  • Inhibition of MAO enzymes which break down noradrenaline and serotonin in synaptic cleft
  • Increases volume of serotonin and noradrenaline in cleft
  • Increase post synaptic firing
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30
Q

Name a dietary interaction of MAOIs

A

Tyramine containing foods

31
Q

Name 2 pharmacological interactions of MAOIs

A
  1. Other antidepressants

2. St John’s Wort

32
Q

Why do MAOIs interact with tyramine containing foods?

A
  • Tyramine is normally inactivated by MAO enzymes in GIT
  • Tyramine cannot be metabolised
  • Causes release of catecholamines
  • Leads to tachycardia, hypertension, arrhythmias and strokes
33
Q

Name 5 side effects of MAOIs

A
  1. Postural hypotension
  2. Drowsiness
  3. Anticholinergic effects
  4. Weight gain
  5. Parathesia
34
Q

Name 4 antidepressants which may cause QT prolongation

A
  1. Escitalopram (SSRI)
  2. Citalopram (SSRI)
  3. Venlafaxine (SNRI)
  4. Mirtazapine (Tricyclic)
35
Q

Describe NICE guidelines for prescribing antidepressants

A
  1. SSRI 1st line
  2. Switch to alternative SSRI or another class of antidepressant
  3. Augment (lithium, antipsychotic, mirtazapine)
36
Q

Name 5 common anxiety disorders

A
  1. Generalized anxiety disorder
  2. Panic disorder
  3. Social phobia
  4. OCD
  5. PTSD
37
Q

Name a common self medicated anxiolytic

38
Q

Name 5 treatments used in anxiety

A
  1. SSRIs (usually first line)
  2. Benzodiazepines / Z drugs
  3. Pregabalin
  4. Buspirone
  5. Antipsychotics
39
Q

What receptor is important for benzodiazepines and Z-drugs?

A

GABA-A receptor

40
Q

Describe the GABA-A receptor

A
  • Ionotropic (chloride channel)

- 5 subunits cause of 16 isoforms

41
Q

How do benzodiazepines and Z-drugs affect GABA-A receptor?

A

Increase affinity for GABA and therefore enhance inhibitory effect

42
Q

Name 5 uses of benzodiazepines

A
  1. Anxiolytic
  2. Hypnotic
  3. Muscle relaxant
  4. Anti convulsant
  5. Amnestic
43
Q

Name 5 side effects of benzodiazepines

A
  1. Headaches
  2. Confusion
  3. Ataxia
  4. Dysarthria
  5. Disinhibition
44
Q

Name 4 uses of diazepam

A
  1. Anxiety
  2. Muscle spasms
  3. Seizures
  4. Alcohol withdrawal
45
Q

Name 4 routes of administration of diazepam

A
  1. Orally
  2. IV
  3. Rectally
46
Q

How is diazepam excreted?

A

Glucuronide conjugates excreted in the urine

47
Q

Describe the main differences between lorazepam and diazepam

A
  • Faster acting
  • Shorter half life (no active metabolites)
  • More potent
48
Q

Describe Z drugs

A
  • Different chemical structure to benzodiazepines
  • Acts on benzodiazepine site at GABA-A receptor
  • Short onset of action
  • Side effects similar to benzodiazepines
49
Q

Name an example of a barbiturate drug

A

Phenobarbital

50
Q

Why can barbiturates act synergistically with benzodiazepines?

A

Bind to different sites on GABA-A receptors

51
Q

Why can barbiturates be toxic at high doses?

A

Act as agonist in the absence of GABA

52
Q

What is flumazenil used for?

A

Treat overdose of benzodiazepines

53
Q

How does flumazenil work?

A

Competitive antagonist on benzodiazepine binding site

54
Q

Name 3 clinical indications of pregabalin

A
  1. Anticonvulsant
  2. Anxiolytic
  3. Neuropathic pain
55
Q

Describe the mechanism of action of pregabalin

A
  • Inhibitory action at α-2 delta subunit of presynaptic voltage gated calcium channels
  • Modulates release of excitatory neurotransmitters
56
Q

Describe the mechanism of action of buspirone

A
  • Agonist at presynaptic 5HT-1A receptor
  • Partial agonist of postsynaptic 5HT-1A receptors
  • Supresses serotinergic tranmission
  • Enhances dopaminergic and noradrenergic transmission
57
Q

Describe the mechanism of action of alcohol

A
  • Acts like benzodiazepine at GABA-A receptor

- Antagonist at glutamate receptor

58
Q

Describe 2 components of the dependence of alcohol

A
  • Upregulation of NMDA

- Downregulation of GABA receptors

59
Q

What causes Parkinson’s disease?

A
  • Imbalance of dopamine and acetylcholine neuronal function in extrapyramidal system
  • Loss of dampening of movement causing both muscle groups to contract
  • Leads to rigidity and stiffness
60
Q

Name 4 types of dopamine enhancing drugs

A
  1. Levodopa + carbidopa
  2. Dopamine agonists
  3. COMT inhibitors
  4. MAO-B inhibitors
61
Q

How do COMT inhibitors increase dopamine transmission?

A

Allow more levodopa to cross blood brain barrier

62
Q

How do MAO-B inhibitors increase dopamine transmission?

A

Less dopamine is broken down in synaptic cleft so more is available for post synaptic firing

63
Q

What is levodopa?

A

Precursor of dopamine given instead of dopamine as it crosses the blood brain barrier

64
Q

Why is levodopa given with carbidopa?

A

Carbidopa is a dopa decarboxylase inhibitor which allows more levodopa to cross into the brain

65
Q

Name 3 psychiatric adverse effects of levodopa

A
  1. Confusion
  2. Anxiety
  3. Impulse control disorders
66
Q

Name 4 peripheral adverse effects of levodopa

A
  1. Nausea / vomiting
  2. Hypotension
  3. Arrhythmias
  4. Sweating
67
Q

What is dementia?

A

Symptoms associated with decline in memory and thinking of a degree sufficient to impair functioning in daily living

68
Q

Describe 4 presentations of dementia

A
  1. Early changes in mood and memory
  2. Gradual decline in short term memory
  3. Loss of ability to conduct complex tasks
  4. Impaired concentration
69
Q

What is the main type of dementia?

A

Alzheimer’s disease

70
Q

Describe 4 components of the pathology of dementia

A
  1. Gliosis / loss of neurones
  2. Reduction of cerebral cortex subcortical white matter
  3. Depletion of cholinergic neurones
  4. Excessive gluatmatergic transmission
71
Q

Name 2 types of drugs used to treat dementia

A
  1. Acetylcholinesterase inhibitors

2. NMDA receptor antagonist

72
Q

Name 3 acetylcholinesterase inhibitors

A
  1. Donepezil
  2. Rivastigmine
  3. Galantamine
73
Q

Name an NMDA receptor antagonist

74
Q

Name 4 side effects of acetylcholinesterase inhibitors

A
  1. Nausea / vomiting
  2. Bradycardia
  3. Heart block
  4. Muscle cramps

DEN 2026 - Pharmacology (22 decks)

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