L1 Antidepressants Flashcards

1
Q

5-HT is broken down mainly by

A

MAO-A

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2
Q

Noradrenaline is broken down mainly by

A

MAO-A and MAO-B

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3
Q

Dopamine is broken down mainly by

A

MAO-A and MAO-b

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4
Q

What is the type of MAOi used in Parkinson’s disease?

A

MAO-B

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5
Q

Phenelzine is: (2)

A
  1. non-selective for MAO-A vs MAO-B

- and irreversible MAOi

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6
Q

ADR of MAOis

A
  1. postural hypotension - dopamine as inhibitory neurotransmitter, cervical block
  2. restlessness or insomnia - CNS stimulation
  3. should not be combined with other drugs with seretoninergic function eg. pethidine - myoclonus, hyperexcitability, loss of consciousness, increased muscular tone
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7
Q

Significant drug-food interaction related to the use of MAOIs (also its major limitation)

A

the ‘cheese’ reaction

- cheeses and concentrated yeast products eg. marmites

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8
Q

Tyramine has a high affinity for

A

NA transporters

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9
Q

TCAs were initially produced as

A

potential antipsychotic drugs in 1949, but found to be ineffective in schizophrenia

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10
Q

Examples of non-selective TCAs

A

imipramine, amitriptyline, nortriptyline

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11
Q

Example of NET-selective TCA

A

desipramine

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12
Q

Which one of the non-selective TCAs has the mildest side effect profile?

A

nortriptyline

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13
Q

ADR of TCAs (4)

A
  1. sedation - H1 antagonism, tolerance can be developed in 1-2weeks
  2. postural hypotension - a-adrenoceptor sympathetic block
  3. dry mouth, blurred vision, constipation - muscarinic receptor antagonism
  4. ddi - rely on hepatic metabolism
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14
Q

Which is the first drug class to be developed for the purpose of antidepressant treatment?

A

SSRIs

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15
Q

What is the mostly widely prescribed antidepressant currently?

A

Fluoxetine

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16
Q

3 key advantages of SSRIs

A
  1. low affinity for alpha-adrenoceptors
  2. low affinity for muscarinic cholinergic receptors
  3. lack of effect at histamine receptors
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17
Q

Which SSRIs still retain some level of sedation?

A

citalopram - still has some histamine receptor antagonism

18
Q

adr of SSRIs

A

nausea, insomnia, sexual dysfunction

19
Q

What drugs can be given to prevent SSRTI-induced sexual dysfunction?

A

cyproheptadine or other 5HT2 blockers

20
Q

What is the current first line therapy used for depression?

A

SSRIs, but it is not perfect:

  • only 2/3 achieve remission
  • adverse effects, esp at the start
  • discontinuation can be a problem in some
21
Q

Maprotiline

A

an earlier NARI, had TCA-like adverse effects due to alpha-adrenoceptor and histamine receptor effects and occasionally caused seizures

22
Q

Examples of SNRIs in clinical use

A

venlafaxine, desvenlafaxine (synthetic metabolite of venlafaxine), and duloxetine

23
Q

Withdrawal effects is more common and stronger for SSRIs/TCAs/SNRIs?

A

SNRIs

24
Q

Example of a NDRI

A

bupropion

25
Q

Example of an anesthetic, currently evaluated for rapid-onset antidepressant effect

A

Ketamine, a glutamate NMDA receptor antagonist

26
Q

Example of a NaSSA

A

mirtazapine, adrenergic a2 autoreceptor antagonist + 5HT2c receptor antagonist

27
Q

Aglomelatine

A

agonist of MT1 and MT2 receptors, also has antagonist at 5HT2c receptors

  • also helps in sleep disorders
  • less TCA/SSRI-associated adr
28
Q

Vortioxetine

A

multimodal serotonergic antidepressant + additional receptor affinities

29
Q

Vortioxetine is generally used in

A

patients resistant to other antidepressants, pro cognitive effects too, appear to work well with children and young adults

30
Q

Close monitoring required in initial stages of vortioxetine use due to

A

increased risk of suicidal thoughts or actions in childrens and teens

31
Q

Does fluoxetine or citalopram has a higher selectivity for 5-HT?

A

50-fold vs 1000-fold, citalopram

32
Q

Does TCA and SSRI bind to the same site?

A

Yes

- SSRI has greater 5-HT reuptake selectivity though, fewer adverse effects

33
Q

Adverse effects of TCAs lead to

A

prescription of subtherapeutic doses
- improved adverse side effect profile of SSRIs lead to better compliance and so prescription of more adequate doses, better efficacy

34
Q

Symptoms of serotonin syndrome

A

tremor, hyperthermia, cardiovascular collapse

35
Q

Why is SSRis safer in overdose?

A

low affinity for alpha-adrenoreceptors: lack of cardiovascular effects (postural hypotension, bradycardia)

36
Q

NARI

A

reboxetine, maprotiline

37
Q

ADR of SNRI

A
  • similar to SSRI: nausea, insomnia, sexual dysfunction
  • ‘serotonin syndrome’ when combined with other serotoninergic drugs and MAOis
  • withdrawal effects may be more common and stronger than for SSRIs and TCAs
38
Q

Which of the following has the fewest adr? TCAs/SSRIs/NARIs

A

NARI

39
Q

Does venlafaxine have the same structure as TCA?

A

NO, fewer adr than TCAs

40
Q

Adv of velnlafaxine

A
  • different structure to TCAs and fewer side effects

- claimed to work slightly faster, 2-4weeks, work better in treatment-resistant patients

41
Q

ADR of reboxetine

A
  • dry mouth, constipation
  • insomnia: noradrenergic activity on CNS
  • tachycardia: increased NA availability