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UM2010 Pharmacology > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Depression types

A

Unipolar

Bipolar

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2
Q

Unipolar depression can be divided into

A 
Reactive depression (~75%)
Endogenous depression (~25%)
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3
Q

What are the factors of reactive depression ?

A

Associated with circumstance (e.g. stress)

Non-familial

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4
Q

What are the factors of endogenous depression?

A

Unrelated to external pressure

Familial

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5
Q

Biological symptoms of depression.

A

Cognitive deficits
Loss of sex drive
Sleep disturbance
Loss of appetite

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6
Q

Depression can be treatable through surge affecting which pathways?

A

Serotonergic and noradrenergic

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7
Q

Where is 5-HT released from?

A

Dorsal rapid

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8
Q

What are the main 5-HT receptors?

A

5-HT1A
5-HT2A
5-HT2c
5-HT3

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9
Q

Location and function of 5-HT1A receptor

A

Presynaltic Gi/o

Decrease 5-HT release

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10
Q

Other location of 5-HT1A and function receptors?

A

Postsynaptic Gi/o

Decrease depression & decrease anxiety

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11
Q

Location and function of 5-HTA2A receptor

A

Gq

Increase anxiety

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12
Q

Location and function of 5-HTA2c receptor

A

Gq

Increase depression, anxiety, stress & appetite

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13
Q

Location and function of 5-HTA3 receptor

A

Ligand-gated cation channel

Increase nausea

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14
Q

How long does it take for antidepressants to generate a therapeutic effect?

A

~ 2 weeks

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15
Q

Antidepressant classes

A

Selective serotonin reuptake inhibitors (SSRIs)

Tricyclic antidepressants (TCAs)

Serotonin / Noradrenaline reuptake inhibitors (SNRIs)

Monoamine receptor antagonists

Monoamine oxidase inhibitors

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16
Q

Function of SSRIs

A

Increase amount on serotonin in synaptic cleft

Increase activity through post synaptic receptors

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17
Q

All SSSRIs have a half life of?

A

Long- 18 hours

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18
Q

Administration of SSRIs

A

Oral tablets once daily

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19
Q

Side effects of SSRIs on CNS

A

Sleep disturbance, weight gain, sexual dysfunction, agitation / anxiety

20
Q

SSRIs side effects on GI

A

diarrhoea & nausea

21
Q

SSRIs side effect on CVS

A

Bleeding disorders

22
Q

What happens when SSRIs is taking in overdose

A

Serotonin syndrome

23
Q

Fluoxetine

A

Specific SSRI
“Prozac”
Long duration (t 1/2 up to 96h)

24
Q

Citalopram

A

Specific SSRI

Milder side effects (anti cholinergic)

25
Q

Escitalopram

A

Specific SSRI
Racemic form of citalopram
No anti cholinergic

26
Q

Paroxetine

A

Specific SSRI
“Seroxat”
Withdrawal symptoms
Anti cholinergic effect

27
Q

SSRIs with anti cholinergic effect

A

Citalopram

Paroxetine

28
Q

MOA of TCA & SNRIs

A

Serotonin cleared from synapse by 5-HT & Noradrenaline re-uptake transporters

Subsequent breakdown by intracellular monoamine oxidase A (5-HT & NA) and catechol-O-methyltransferase (NA only)

29
Q

Venlafaxine

A

SNRI inhibitor (Serotonin & Noradrenaline Reuptake Inhibitors )

Weak, non selective
Weak receptor blocking

30
Q

Side effects of SNRIs

A 
Similar to SSRIs +
Dry mouth 
Dizziness
Arrhythmia 
Seizure
Overdose risk of serotonin syndrome
31
Q

Most famous tricyclic antidepressant (TCA)

A

Amitryptline

32
Q

Use of TCA

A

neuropathic pain with lower dose

antagonists at α1, mACh, Histamine H1 (similar side effects to antipsychotics)

33
Q

Side effects of TCA

A

Anticholinergic effects
Sedation
Postural hypotension
Impotence

34
Q

Cautions with TCA

A

Significant overdose risk

Drug interactions with other CNS depressant and hepatic metabolism

CV disorders

35
Q

Most common noradrenaline selective reuptake inhibitor

A

Bupropion

36
Q

Bupropion

A

NA- selective reuptake inhibitor

antidepressant & anxiolytic. Also inhibits DA uptake, some 5-HT uptake. Mostly used for smoking cessation

37
Q

Side effects of bupropion (or any NA-selective reuptake inhibitor)

A

General sympathomimetic & CNS stimulant side effects (e.g. dry mouth, insomnia, dizziness, tachycardia, constipation)

38
Q

Most common monoamine receptor antagonist(MOA)

A

Mirtazepine

39
Q

Mirtazepine

A

MOA antagonist

Antagonist adrenergic a2

5-HT2A,C & 5-HT3

No serious drug interactions. Faster onset

40
Q

MOA inhibitors mechanism of action

A
  • Monoamines cleared from synapse by 5-HT & NA re-uptake transporters
  • Subsequent breakdown by intracellular monoamine oxidase A, and catechol-O-methyltransferase (NA only)
  • Some MAOIs nonselective; also inhibit MAO-B
41
Q

Side effects for MAO

A

Serious; SSRI side effects plus “cheese reaction” (tyramine), anticholinergic side effects, arrhythmias

42
Q

MAOIs must not be given concurrently with other antidepressants at least?

A

2 week gap between medication changed

43
Q

All antidepressant classes have similar effectiveness; usually side effects determine preference. In which order?

A

SSRIs > SNRIs > TCAs

44
Q

How do we treat bipolar disorder?

A

Generally stabilise mania, less so depression

Conventional antidepressants controversial for bipolar disorder; usually given with additional anti-mania drug

45
Q

What is used as anti-mania drug?

A

Lithium

46
Q

moa of lithium to as anti-mania

A

Enters cells selectively via certain Na+ channels (e.g. brain, kidneys)

Accumulation: not pumped out by Na+/K+ exchanger.

47
Q

Other bipolar disorder drugs are?

A

Anticonvulsants
Atypical antipsychotics
(May be prescribed in conjunction with antidepressants, usually SSRI (e.g. fluoxetine)

UM2010 Pharmacology (7 decks)

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