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PHAR 557 > Major Depressive Disorder - Pharmacotx > Flashcards

Major Depressive Disorder - Pharmacotx Flashcards

1
Q

T or F: Antidepressant trials have shown that antidepressants have a huge impact upon MDD sx’s

A

F

There are large placebo effects in these trials > indicates unspecific factors are strongly involved in MDD tx

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2
Q

What kind of MDD has been studied the most in antidepressant trials?

A

mod-sev MDD

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3
Q

CANMAT 1st line SSRIs:

A 
sertraline
escitalopram
citalopram
fluoxetine
paroxetine
vortioxetine
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4
Q

What’s special about vortioxetine?

A

It’s an SSRI that also has 5-HT actions (i.e. it’s a serotonin MODULATOR)

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5
Q

What SSRI is NOT recommended by CANMAT as a first-line agent for MDD?

A

fluvoxamine (Luvox) > due to DIs and reduced tolerability

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6
Q

SSRI MOA?

A

Inhibit reuptake of 5-HT by inhibiting 5-HT transporters in CNS neurons

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7
Q

SSRI onset of action?

A

1st few days for decreased agitation and anxiety, improved sleep, and improved appetite.

1-3 wks: increased activity, increased sex drive, improved self care, conc, memory, thinking, movements

2-4 weeks on average for relief of depressed mood/anhedonia/hopeless feelings/suicidal thoughts

(can take up to 8 weeks for full effects)

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8
Q

SSRI AEs?

A

HANDS

h/a, anxiety (esp. when starting SSRI tx), nausea, diarrhea (and other GI upset), Sexual and sleep dysfn (insomnia, sedation, sexual dysfn [men and women])

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9
Q

SSRI’s most commonly assoc w/ sedation?

A

Sertraline, citalopram, and paroxetine

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10
Q

SSRIs assoc w/ wt gain?

A

Paroxetine

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11
Q

T or F: SSRIs are commonly assoc w/ wt gain.

A

F

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12
Q

What’s so special about fluoxetine?

A

It is the most stimulating SSRI and has a long half life (4-6 days)

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13
Q

Which SSRIs have the highest rates of N/D?

A

Fluvoxamine and sertraline

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14
Q

Which SSRI is assoc w/ the least amt of sexual dysfn?

A

Escitalopram

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15
Q

Which SSRI is the least tolerable overall?

A

Fluvoxamine

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16
Q

What life-threatening adverse effect are SSRIs assoc w/?

A

SIADH (syndrome of inappropriate ADH)

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17
Q

What is SIADH?

A

A condition where a lot of ADH is produced > causes lots of fluid retention > electrolyte dilution > hyponatremia/concentrated urine

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18
Q

Sx’s/signs of SIADH?

A

Lethargy, change in mental status, Na<130 mEq/L, hyperosmolar urine (>300 mOsm/kg)

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19
Q

Fluvoxamine’s inhibition of CYP1A2 is s.times strategically used to increase the levels of this drug.

A

clozapine (clozapine is metabolized by 1A2)

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20
Q

DIs of SSRI?

A
  1. NSAIDs, antiplatelets, anticoags
    - SSRIs reduce platelet aggregation > increased bleeding risk
  2. Serotonergic agents
    - increased risk of serotonin syndrome
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21
Q

How does food affect SSRI absorption?

A

It doesn’t

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22
Q

There is ONE SSRI that is affected by food.

A

It’s sertraline; its F increases w/ food

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23
Q

How are SSRIs metabolized?

A

By CYP enzymes

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24
Q

These three SSRIs are metabolized into active metabolites by the liver.

A
  1. fluoxetine
  2. citalopram
  3. sertraline
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25
Q

How often are SSRIs taken per day?

A

OD

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26
Q

Are SSRIs safe in pregnancy?

A

Yes, as far as the evidence is concerned (no teratogenicity)

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27
Q

Which SSRI should be avoided during pregnancy?

A

Paroxetine

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28
Q

Why should paroxetine be avoided in pregnancy?

A

It’s assoc w/ most reports of pulmonary HTN and SSRI withdrawal (jitteriness, restlessness, irritability, tremors) [although, these are in fact seen w/ other SSRIs too]

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29
Q

Which SSRIs are safe in breastfeeding?

A

Sertraline and paroxetine (most research + low to undetectable levels)

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30
Q

Which SSRIs should be avoided in breastfeeding?

A

Fluoxetine (high levels in breast milk + prolonged half-life)

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31
Q

SSRI warnings:

A
  1. increased risk of suicide in children, adolescents, and young adults <24yrs
  2. reduced BMD and increased fracture risk
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32
Q

Which SSRI is assoc w/ QTc prolongation?

A

Citalopram

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33
Q

What is the max dose for citalopram in order to reduce the risk of QTc prolongation?

A

40mg

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34
Q

This SSRI is assoc w/ the most diarrhea and male sexual dysfn:

A

Sertraline

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35
Q

Which SSRI is most assoc w/ sedation?

A

paroxetine

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36
Q

T or F: SSRIs do not need to be tapered when being d/c’ed.

A

F (They SHOULD be tapered to avoid withdrawal sx’s)

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37
Q

What is vortioxetine (i.e. class of medication)?

A

It’s a serotonin modulator

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38
Q

1st line SNRIs (CANMAT)?

A

Duloxetine, Venlafaxine

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39
Q

2nd line SNRIs (CANMAT)?

A

Levomilnacipran

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40
Q

SNRI MOA?

A

Inhibits presynaptic 5-HT and NE reuptake in CNS neurons.

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41
Q

T or F: Venlafaxine can also work as an SSRI.

A

T

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42
Q

Minimum dose of venlafaxine for it to work as an SNRI.

A

150mg/day

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43
Q

Venlafaxine dosed at doses <150mg/day works as a what?

A

SSRI

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44
Q

Duloxetine vs. venlafaxine: which one inhibits NE transporter better?

A

Duloxetine

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45
Q

SNRI onset of action

A

SAME AS SSRIs!

1st few days for decreased agitation and anxiety, improved sleep, and improved appetite.

1-3 wks: increased activity, increased sex drive, improved self care, conc, memory, thinking, movements

2-4 weeks on average for relief of depressed mood/anhedonia/hopeless feelings/suicidal thoughts

(can take up to 8 weeks for full effects)

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46
Q

SNRI AEs

A

HANDS (like SSRIs)

h/a, anxiety (esp. when starting SSRI tx), nausea, diarrhea (and other GI upset), Sexual and sleep dysfn (insomnia, sedation, sexual dysfn [men and women])

Antichol effects (dose-related) [can’t pee/see/spit/shit, sedation]

Increased BP/HR (dose-related)

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47
Q

T or F: SSRIs must be tapered when d/c’ing, but SNRIs do not.

A

F (SNRIs must be tapered before d/c too)

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48
Q

SNRI vs SSRI: withdrawal sx’s are worse with which one?

A

SNRI

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49
Q

How does food affect SNRI absorption?

A

It doesn’t

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50
Q

Does kidney fn affect dosing of SNRIs?

A

Yes, dosing must be adjusted

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51
Q

T or F: Venlafaxine and duloxetine are excreted unchanged by the kidneys.

A

F (They’re metabolized hepatically first)

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52
Q

Duloxetine and venlafaxine are inhibitors and substrates for which CYP enzyme?

A

2D6

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53
Q

Besides CYP450 interactions, name 2 other DIs involving SNRIs

A
  1. NSAIDs/antiplatelets/anticoagulants (increased bleeding risk)
  2. Serotonergic agents (increased risk of serotonin syndrome)
54
Q

SNRI warnings/precautions:

A
  1. narrow angle glaucoma
  2. HTN pts
  3. increased risk of suicide if <24yrs
  4. avoid abrupt withdrawal
55
Q

1st line NDRI (CANMAT):

A

Bupropion (Wellbutrin)

56
Q

Bupropion MOA

A

inhibits NE and DA transporters increasing concs in the synapses

57
Q

T or F: Bupropion has some 5-HT effects at higher doses.

A

F

58
Q

Bupropion (NDRI) onset

A

Similar to SSRIs/SNRIs

1st few days for decreased agitation and anxiety, improved sleep, and improved appetite.

1-3 wks: increased activity, increased sex drive, improved self care, conc, memory, thinking, movements

2-4 weeks on average for relief of depressed mood/anhedonia/hopeless feelings/suicidal thoughts

(can take up to 8 weeks for full effects)

59
Q

What enzyme metabolizes bupropion?

A

CYP2B6

60
Q

T or F: The metabolite of bupropion is nonactive

A

F (It’s also active - hydroxybupropion)

61
Q

Bupropion route of elimination

A

Kidneys mainly (87%)

62
Q

Brand name of bupropion used for MDD?

A

Wellbutrin

63
Q

Brand name of bupropion used for smoking cessation?

A

Zyban

64
Q

T or F: You cannot use Zyban for MDD - the brand must be changed to Wellbutrin.

A

F

They’re the exact same drug. If using Zyban for smoking cessation, it can also concurrently be used for MDD tx

65
Q

If a patient is on Zyban for smoking cessation, and he is dx’ed with MDD, he can be put on Wellbutrin to tx it.

A

F

They are the SAME drug!

66
Q

Bupropion inhibits this enzyme strongly

A

2D6

67
Q

Common bupropion AEs

A
  • Activating (ANXIETY, agitation, insomnia, tremor - due to NE)
  • Sweating (due to NE)
  • Reduced appetite/wt loss
  • GI upset
  • Psychosis (due to DA)
  • Seizures
  • Sexual dysfn (less so than SSRIs/SNRIs)
68
Q

T or F: There’re no dosing adjustments needed for bupropion for renal/hepatic impairment.

A

F (dosing adjustments needed for impairment in either of those organs)

69
Q

Bupropion contraindications?

A
  1. MAOI tx > causes hypertensive crisis
  2. seizures disorder
  3. eating disorder
  4. abrupt d/c of alcohol or sedatives (another risk factor for seizures)
70
Q

What’s mirtazapine’s MOA?

A

central alpha-2-blocker > increased NE and 5HT release

5HT2 receptor blocker > lower anxiety

5HT3 receptor blocker > GI AEs

H1 histamine receptor blocker > sedation, wt gain

71
Q

Where does mirtazapine fit in CANMAT’s MDD guidelines?

A

It’s another 1st line agent for MDD

72
Q

Mirtazapine AEs

A
  1. sedation (lasts long)
  2. increased appetite > wt gain
  3. sig sexual dysfn (more than other antidepressants)
73
Q

Mirtazapine onset?

A

Like SSRIs/SNRIs

1st few days for decreased agitation and anxiety, improved sleep, and improved appetite.

1-3 wks: increased activity, increased sex drive, improved self care, conc, memory, thinking, movements

2-4 weeks on average for relief of depressed mood/anhedonia/hopeless feelings/suicidal thoughts

(can take up to 8 weeks for full effects)

74
Q

How is mirtazapine excreted?

A

75% renally excreted

75
Q

T or F: Mirtazapine has no risk of serotonin syndrome, just like bupropion.

A

F (it causes more serotonin release from central neurons)

76
Q

When should mirtazapine be taken?

A

At night due to its sedating effects

77
Q

When should mirtazapine be taken?

A

At night due to its sedating effects

78
Q

When does the sedative effect of mirtazapine begin to disappear?

A

30 mg

79
Q

When is mirtazapine usually used?

A

When pts have insomnia and if wt gain is desired

80
Q

T or F: Mirtazapine is dangerous in overdose

A

F

It’s pretty safe in overdose

81
Q

Black box warning assoc w/ SSRIs, SNRIs, bupropion, AND mirtazapine?

A

Increased suicide risk for inds <24yrs

82
Q

Agranulocytosis is assoc w/ which antidepressant?

A

Mirtazapine

83
Q

Name the 2nd line agents recommended by CANMAT for tx of MDD

A 
1. TCAs:
Amitriptyline
Clomipramine
Nortriptyline
(others)
SNRI
2. Levomilnacipran
Reversible MAOI
3. Moclobemide
Serotonin reuptake inhibitor/5HT2 antagonist
4. trazodone
Atypical antipsychotic
5. quetiapine
Serotonin reuptake inhibitor/5HT1A partial agonist
6. Vilazodone
84
Q

MOA of TCAs

A

Inhibit presynaptic 5HT and NE reuptake

85
Q

MOA of TCAs is similar to this class of medication.

A

SNRI (reuptake of NE and 5HT is delayed)

86
Q

What kind of TCAs have more 5HT reuptake inhibition (and hence more 5HT activity)?

A

Those w/ 3º amines

87
Q

What kind of TCAs have more NE reuptake inhibition (and hence more NE activity)?

A

Those w/ 2º amines

88
Q

Name a TCA with 3º amine.

A

amitriptyline

89
Q

Name a TCA w/ 2º amine.

A

nortriptyline

90
Q

What kind of TCA is better tolerated?

A

2º amine TCAs since they have more NE activity relative to 5HT activity

91
Q

amitriptyline vs nortriptyline - which is better tolerated? Why?

A

Nortriptyline since it contains a 2ºamine, and hence has more NE activity.

92
Q

What comorbidity should be considered before Rx’ing nortriptyline?

A

HTN (increased BP w/ increased NE activity)

93
Q

What did the Cipriani paper tell us about amitriptyline?

A

It may be more effective than the other antidepressants.

94
Q

Common AEs w/ TCAs

A

sedation, anticholinergic effects (reduced sweating, dry mouth, reduced urination, mydriasis, flushing, delirium and confusion, constipation), CV AEs, wt gain, sexual dysfn, urine discolouration (blue-green with amitriptyline)

95
Q

What happens in TCA overdose?

A

It has potentially lethal cardiotoxic effects such as heart block or ventricular tachycardia

96
Q

Trazodone MOA

A

Weak inhibition of 5HT and NE uptake

5HT2A antagonist

Alpha-1 and histamine-1 receptor antagonists (sedating)

97
Q

How is trazodone mainly excreted?

A

Kidneys (75%)

98
Q

How does food affect trazodone?

A

It enhances yet delays peak conc

99
Q

CYP enzyme involved in trazodone metabolism

A

CYP3A4

100
Q

Trazodone DIs

A

CYP3A4 inducers/inhibitors

Antihypertensives (due to alpha-1 blocking activity > hypotn)

Serotonergic meds

QT prolonging meds

101
Q

Trazodone AEs

A

Dizziness, sedation, h/a, orthostatic hypotn, QT prolongation, N, constipation, dry mouth

102
Q

Should trazodone be taken with a meal? Why or why not?

A

Yes > it delays peak conc > reduces AEs

103
Q

What is trazodone usually used for?

A

sedation (NOT MDD usually due to AEs)

104
Q

Quetiapine MOA

A

Antagonist at 5HT1, 5HT2, D1 and D2, H1 (sedation), alpha-1 and alpha-2 receptors

105
Q

What kind of drug is quetiapine?

A

Atypical antipsychotic

106
Q

Quetiapine has a usual dose range (150-300mg/day) and a max daily dose range (300-600mg/day). What’re ea. used for?

A

Usual daily dose range: MDD

Max daily dose range: psychotic depression (quetiapine is an atypical antipsychotic)

107
Q

Which MAOI is often used in MDD pts (in Canada)?

A

Moclobemine

108
Q

How does moclobemine differ from the other MAOIs?

A

It’s reversible (the other MAOIs are irreversible)

109
Q

MAO-A preferentially metabolizes ______

A

5HT and NE (DA, but less than MAO-B)

110
Q

MAO-B preferentially metabolizes ______

A

trace amines (like DA)

111
Q

MAO-A and MAO-B both metabolize ______

A

DA and tyramine

112
Q

Which MAO subtype has a larger effect on DA metabolism?

A

MAO-B

113
Q

MOA of moclobemide?

A

Short-acting reversible inhibitor of MAO-A > reduces metabolism of 5HT, NE, and DA

114
Q

At what dose of moclobemide do we begin to see tyramine rxns?

A

> 600mg/day

115
Q

Why do we begin to see tyramine rxns after exceeding the daily max dose of moclobemide?

A

The drug loses its specificity to MAO-A

116
Q

DI’s of moclobemide:

A

Serotonergic drugs, anesthesia

117
Q

If taking a serotonergic drug, what should you do if you want to start an MAOI?

A

Stop the serotonergic drug 2 weeks before starting the MAOI

118
Q

Why do we stop the serotonergic drug if starting an MAOI?

A

Avoid hypertensive rxn or serotonin syndrome

119
Q

D/c THIS SSRI 5 weeks before starting MAOI. Why?

A

Fluoxetine > it has a longer t1/2

other SSRIs are stopped 2 weeks prior to MAOI initiation

120
Q

Moclobemide main AEs

A

Nervousness/anxiety (due to NE and DA)

Antichol effects

121
Q

Levomilnacipran - MOA?

A

SNRI

122
Q

AEs of levomilnacipran

A

HANDS (like SSRIs)

h/a, anxiety (esp. when starting SSRI tx), nausea, diarrhea (and other GI upset), Sexual and sleep dysfn (insomnia, sedation, sexual dysfn [men and women])

Antichol effects (dose-related) [can’t pee/see/spit/shit, sedation]

Increased BP/HR (dose-related)

123
Q

Vilazodone - MOA

A

Serotonin reuptake inhibitor/5HT1A partial agonist

124
Q

3rd line tx’s for MDD

A

Irreversible MAOIs

125
Q

Irreversible MAOIs - name the two drugs:

A

Phenelzine

Tranylcypromine

126
Q

What do irreversible MAOIs do (MOA)?

A

Inhibit MAO-A and MAO-B > increase 5HT, NE, and DA concs in synapses

127
Q

CANMAT 1st line SSRIs:

A 
sertraline
escitalopram
citalopram
fluoxetine
paroxetine
vortioxetine
128
Q

1st line SNRIs (CANMAT)?

A

Duloxetine, Venlafaxine

129
Q

1st line NDRI (CANMAT):

A

Bupropion (Wellbutrin)

130
Q

Where does mirtazapine fit in CANMAT’s MDD guidelines?

A

It’s another 1st line agent for MDD

131
Q

MOA of ketamine?

A

helps to rebalance glutamate levels in the CNS > reduces chronic excitatory stress on neurons

132
Q

Major ketamine AE

A

Dissociation (50%!!)

PHAR 557 (36 decks)

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