Antidepressant Drugs Flashcards

1
Q

What is the paradox of antidepressants?

A

SEs can start immediately but the therapeutic effects can take weeks

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2
Q

What is the action of MAO inhibitors?

A

Leads to increased serotonin, dopamine and norepinephrine due to decreased breakdown from the inhibition of MAO.

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3
Q

MAO-A

A

Metabolizes catecholamines (NE, Epi), 5HT

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4
Q

MAO-B

A

Metabolizes trace amines and 5HT

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5
Q

Hypertensive Crisis

A

Tyramine is not degraded while a pt is on an MAO and so it builds up and acts as a pressor and increases BP.

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6
Q

Serotonin Syndrome

A

Due to a combination of MAO-I and SSRIs that leads to a build up of serotonin that increases its activity leading to increased activity and reflexes.

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7
Q

What are the tertiary tricyclic antidepressants (TCAs) more selective for?

A

Serotonin and NE are equally selected for

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8
Q

What are the secondary TCAs more selective for?

A

Norepinephrine

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9
Q

Who should TCAs be avoided in?

A
  • Elderly

- Con-current with CNS Depressants

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10
Q

Where do TCAs act?

A

All TCAs block the re‐uptake pumps of both 5‐HT and NE thus preventing their re‐uptake.

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11
Q

What are the general SEs of SSRIs?

A
  • GI effects
  • Sexual dysfunction
  • CNS effects
  • SSRI discontinuation syndrome
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12
Q

SSRI Discontinuation Syndrome

A

Dizziness and nausea that is due to withdrawal and is more likely with short actin SSRIs like paroxetine and fluvoxamine.

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13
Q

Why are there no nausea sexual dysfunction or insomnia as SE from mirtazapine?

A

It also blocks the other serotonin receptors like 5HT2A/2C/3 which prevents these SEs.

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14
Q

What is the major SE of bupropion?

A

Can increase risk of seizures at high doses

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15
Q

After stopping an MAOI to switch to another drug, why is there a wait period?

A

Waiting for the regeneration of the MAO enzyme in the case of irreversible inhibitors. With reversible inhibitors, less time is needed to wait.

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16
Q

When switching from another antidepressant to a MAOI, what is the wait period for?

A

Wait around a week to wait out the half lives of the drug in the system to flush out. Fluoxetine requires a bit longer of a wait period due to its long half life.

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17
Q

What antidepressant drugs are most likely to cause interactions with other drugs from inhibition of CYP450 systems?

A
  • Fluoxetine

- Fluvoxamine

18
Q

What are the irreversible MAOIs?

A
  • Phenelzine
  • Selegiline
  • Tranylcypromine
  • Isocarboxazid
19
Q

What is the half life of MAOI like?

A

Short - 2-4 hours

20
Q

What drug combination with MAOI can lead to hypertensive crisis?

A
  • Alpha1 agonists

- NE reuptake blockers

21
Q

What is a reversible MAO-I?

A

Moclobemide - not available in the US

22
Q

Tricyclic Antidepressant MOA

A

All TCAs block the re‐uptake pumps of both 5‐HT and NE thus preventing their re‐uptake.

23
Q

What are the tertiary TCAs and what do they act on?

A

Imipramine and Amitriptyline ‐ produces a comparable blockade of both 5‐HT and NE reuptake.

24
Q

What are the secondary TCAs and what do they act on?

A

Desipramine and Nortriptyline - preferentially blocks NE over 5-HT

25
Q

What are tertiary TCAs metabolized to?

A

Secondary TCAs

26
Q

TCA SE

A

1) H‐1 histamine receptors: excessive sedation, fatigue, weight gain
2) M‐1 muscarinic receptors: confusion & memory dysfunction, excessive sedation, fatigue
3) NE alpha‐1 receptors: postural (orthostatic) hypotension, excessive sedation

27
Q

TCA Contraindications

A
  • Elderly pts

- Alcoholics

28
Q

SSRI MOA

A

Selectively block 5-HT reuptake channels

29
Q

Which SSRI has the longest half life?

A

Fluoxetine

30
Q

Which of the SSRIs has the shortest half lives?

A
  • Paroxetine

- Fluvoxamine

31
Q

SSRI SE

A

a) GI‐ decreased appetite, nausea, diarrhea, constipation, dry mouth
b) Anxiety during 1st week of use; (paroxetine in particular)
c) CNS‐insomnia, sedation, headache, dizziness
d) Sexual dysfunction‐loss of libido, impotence, anorgasmia

32
Q

What is an example of a SNRI?

A

Venlafaxine

33
Q

SNRI SE

A
  • Diaphoresis

- Increase in BP that is dependent upon dose

34
Q

Mirtazapine MOA

A

Blockade of both noradrenergic and serotonergic nerve terminal’s presynaptic alpha2 receptors which causes increased NE and 5‐HT neurotransmission.

35
Q

Buproprion MOA

A

NE and DOPA reuptake inhibitor

36
Q

Buproprion SE

A
  • can cause dry mouth, nausea, insomnia

- increased seizure risk

37
Q

Nefazodone MOA

A

5‐HT2A serotonin receptor antagonist and 5‐HT reuptake inhibitor

38
Q

What is a SE that nefazodone does not have that makes if favorable?

A

NO sexual function SE

39
Q

Nefazodone SE

A
  • Nausea
  • Dry Mouth
  • Increased Appetite
40
Q

Vilazodone and Vortioxetine MOA

A

Serotonin re‐ uptake blockade and serotonin 1A receptor partial agonist

41
Q

Vilazodone SE

A
  • GI
  • Insomnia
  • NO weight gain or sexual dysfunction
42
Q

Vortioxetine SE

A
  • GI
  • Some sexual dysfunction at high doses
  • NO weight gain