Antidepressants Pharmacology Flashcards

1
Q

List a irreversible MAOI. What is its MOA?

A
  • Phenelzine
  • MOA: inhibit MAO -> increase biological availability of monoamines
  • Non-selective for MAO-A, selective for MAO-B
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

MAO-A breaks down ________, and both MAO-A and MAO-B breaks down ____________.

A

5-HT
Dopamine and NE

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the SEs of MAOIs?

A
  • Postural hypotension
  • Restlessness and insomnia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Explain the drug-food interaction of MAOIs (type of food, SEs, mechanism of interaction, management)

A
  • Tyramine-rich foods e.g. cheese, marmite
  • SE: acute HTN, severe headache, occasionally ICH
  • MAO breask down tyramine in intestines and liver
  • when MAOIs are used, tyramine is not broken down and gets taken up into adrenergic terminals -> competes with NA for vesicular compartment
  • Tyramine displaces NA -> increase in NA release in synapses -> sympathomimetic effect
  • Management: less likely with moclobemide (reversible, MAO-A selective)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

True or false?

The SE of postural hypotension in MAOIs, TCAs, SSRIs and SNRIs are all caused by the same mechanism

A

False
* MAOIs: ↑dopamine in cervical ganglia, where it acts as an inhibitory transmitter → sympathetic block → ↓response of blood vessels, ↓vasoconstriction → ↓blood supply to brain
* TCAs, SSRIs, SNRIs: due to α-adrenergic antagonism

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

List 3 TCAs. What are their MOA?

A
  • Non-selective for SERT: imipramine, amitriptyline, notriptyline, dothiepin
  • Selective for NET: desipramine, clomipramine
  • MOA: block reuptake of NE and serotonin

SERT: serotonin transport
NET: NE transport

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

List 3 SEs of TCAs

A
  • Anticholinergic: sedation, weight gain, orthostatic hypotension, arrhythmias, seizure
  • H1 antagonism: sedation, drowsiness (tolerance develop in 1-2w)
  • α-adrenergic antagonism: postural hypotension
  • GI and sexual dysfunction
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

List 3 SSRIs. What are their MOA?

A
  • Fluoxetine, fluvoxamine, paroxetine, sertaline, escitalopram, citalopram
  • Block reuptake of 5HT selectively
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

List 2 SNRIs. What are their MOA?

A
  • Venlafaxine, desvenlafaxine, duloxetine
  • Block reuptake of NE and 5HT
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

List 3 SEs of SSRIs and SNRIs

A
  • Nausea, insomnia (due to discontinuation/ rebound sx of withdrawal when plasma lvls of drug ↓btw doses)
  • Headache, transient nervousness during initiation
  • Hyponatremia (SIADH)
  • GI and sexual dysfunction, EPSE
  • Bleeding risk (↑risk in elderly on concomitant NSAIDs, warfarin, and steroids, consider adding PPI + discontinuing 2w before surgery if high bleeding risks (agomelatine safest))
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

True or false?

Paroxetine is the most favoured SSRI, as it has the least SEs

A

False!
Paroxetine is the most anticholinergic and sedating, ↑weight, short t1/2 (withdrawal) → least favoured!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

True or false?

Citalopram and escitalopram can cause QTc prolongation

A

True
When in high doses in elderly

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

True or false?

Duloxetine has an added SE of urinary hesitation

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

True or false?

Venlafaxine has an added SE of hypotension

A

False
It causes an increase in BP!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

True or false?

SNRIs are less favoured than SSRIs

A

True
SNRIs has more SEs (e.g. anticholinergic SEs, orthostatic hypotension, sedation) compared to SSRIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Briefly list out the signs and symptoms of serotonin syndrome

A

Fever, anxiety/ restlessness/ disorientation/ flushing/ muscle rigidity, ↑↑ BP/ HR/ body temp, tremors, jerking movements, loss of consciousness, cardiovascular collapse

17
Q

What is the drug class and MOA of mirtazapine?

A

Noadrenergic and specific serotonergic antidepressant (NaSSA)
α2- adrenoceptor and 5-HT2&3 antagonism -> ↑5-HT and NE

Also antagonises H1 histamine receptors, peripheral
α1-adrenergic receptors, & muscarinic receptors

18
Q

What antidepressant is the least sedating?

A

MOAIs (moclobemide less sedating than phenelzine)

19
Q

What are the advantages and disadvantages of mirtazapine according to its SEs?

A

SEs: somnolence, increased appetite, weight gain
Less GI and sexual SEs than SSRIs/ SNRIs

20
Q

What is the drug class and MOA of bupropion?

A

Norepinephrine-Dopamine Reuptake Inhibitor (NDRI)
Block reuptake of NA and dopamine

21
Q

What are the advantages and disadvantages of bupropion according to its SEs?

A

SEs: seizure-risk, insomnia, psychosis
Not suitable for eating disorders, and not to be taken at bedtime (stimulating in nature)
Less GI and sexual SEs than SSRIs/ SNRIs

22
Q

Bupropion is a potent CYP_____________

A

CYP2D6 inhibitor

23
Q

What is the drug class and MOA of aglomelatine?

A

Melatonin Receptor Agonist
MT1 and MT2 agonist, 5HT2C antagonist → ↑dopamine and NE

24
Q

What drugs have reduced GI and sexual SEs when compared to SSRIs/ SNRIs?

A

GI and sexual: mirtazapine, bupropion
Sexual only: aglomelatine

25
Q

What are the advantages and disadvantages of aglomelatine according to its SEs? What drugs are C/I with aglomelatine?

A

GI SEs, hepatic SEs
Less sexual dysfuntion and risk of bleeding
C/I: fluvoxamine, ciprofloxacin

Helps in sleep disorders

26
Q

What is the drug class and MOA of vortioxetine?

A

Serotonin Modulators and Stimulators (SMS)
Multimodal serotonergic antidepressant, blocks reuptake of 5HT

27
Q

What are the advantages and disadvantages of vortioxetine according to its SEs?

A

As for SSRI
May ↑risk of suicidal thoughts/ actions in children and teens
May be efficacious in pts resistant to other antidepressants

28
Q

What is the drug class and MOA of trazodone?

A

Serotonin antagonist and reuptake inhibitor (SARI)
Blocks reuptake of 5HT
Antagonises 5HT2A, H1 and α1 adrenoreceptor

29
Q

What are the advantages and disadvantages of trazodone according to its SEs?

A

As for SSRI + sedation, orthostatic hypotension
Rare: priapism

Used for insomnia rather than depression

30
Q

What is the drug class of ketamine and esketamine?

A

Glutamate NMDA receptor antagonist

31
Q

What are the advantages and disadvantages of ketamine and esketamine according to its SEs?

A

SEs: dissociation, dizziness, anxiety, nausea, sedation, increased BP
Ketamine: used as anesthestic
Esketamine: adjunct to SSRI/ SNRI for tx-resistant depression

32
Q

Which antidepressant is the most/ least sedating?

A

Most: TCAs, trazodone, mirtazapine
Least: SSRIs

33
Q

Which antidepressant produces the most/ least anticholinergic effects?

A

Most: TCAs
Least: SSRIs

34
Q

Which antidepressant has the highest/ lowest risk of orthostatic hypotension?

A

Highest: TCAs, trazodone
Lowest: SSRIs