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TN Psychiatry > 22.2 Pharmacotherapy: Antidepressants > Flashcards

22.2 Pharmacotherapy: Antidepressants Flashcards

1
Q

Describe the onset of effects of antidepressants (2)

A
  • relief of neuro-vegetative/physical symptoms: 1-3 wk
  • relief of emotional/cognitive symptoms: 2-6 wk
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2
Q

Describe tapering of antidepressants (2)

A
  • tapering of most antidepressants is usually required to avoid withdrawal reactions;
  • speed of taper is based on the medication’s half-life and the patient’s individual sensitivity
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3
Q

Name an antidepressant that does not require a taper

A

fluoxetine does not require a taper due to its long half-life

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4
Q

Name antidepressants that require a slower taper than sertraline or citalopram

A

paroxetine and venlafaxine require a slower taper than sertraline or citalopram

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5
Q

Describe the treatment of bipolar depression with antidepressants (2)

A
  • patients with bipolar disorder should only be treated with an antidepressant if combined with a mood stabilizer or antipsychotic
  • monotherapy with antidepressants is not advisable as the depression can switch to mania
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6
Q

Name examples of SSRIs (6)

A
  • fluoxetine (Prozac®)
  • fluvoxamine (Luvox®)
  • paroxetine (Paxil®)
  • sertraline (Zoloft®)
  • citalopram (Celexa®)
  • escitalopram (Cipralex®)
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7
Q

Explain use of fluoxetine (Prozac®) (5)

A

Useful for

  • typical and atypical depression
  • seasonal depression
  • anxiety disorders
  • OCD
  • eating disorders
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8
Q

Compare effectiveness of SSRIs (1)

A

All SSRIs have similar effectiveness but consider side effect profiles and half-lives

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9
Q

Name the SSRIs that have the fewest drug-interactions and are sleep-wake neutral (2)

A

Citalopram, and escitalopram

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10
Q

Name the safest SSRI in pregnancy and breastfeeding

A

Sertraline is the safest

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11
Q

Name the most activating SSRI (recommend taking in the AM)

A

Fluoxetine (Prozac®)

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12
Q

Name the most used SSRI in children

A

Fluoxetine is the most used in children as it has most evidence

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13
Q

Fluoxetine does not require a taper why?

A

due to long half-life

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14
Q

Describe: Fluvoxamine (Luvox®) (2)

A
  • Fluvoxamine is sedating (should be taken in PM)
  • can be involved in many drug-drug interactions
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15
Q

Name examples of SNRIs (3)

A
  • venlafaxine (Effexor®)
  • Desvenlafaxine (Pristiq®)
  • duloxetine (Cymbalta®)
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16
Q

SNRIs are useful for what? (3)

A

Useful for depression, anxiety disorders, neuropathic pain

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17
Q

Name example norepinephrine and dopamine reuptake inhibitors NDRI (1)

A

bupropion (Wellbutrin®)

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18
Q

Bupropion (Wellbutrin®) is useful for what? And not recommended for what? (2)

A
  • Useful for depression, seasonal depression
  • not recommended for anxiety disorder treatment because of stimulating effects
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19
Q

Name pros and cons of Wellbutrin (2)

A
  • Causes less sexual dysfunction (may reverse effects of SSRIs/SNRIs), weight gain, and sedation
  • Increased risk of seizures at higher doses
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20
Q

Name contraindications of wellbutrin (5)

A

Contraindicated with

  • history of seizure
  • stroke
  • brain tumour
  • brain injury
  • closed head injury
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21
Q

Name examples tricyclic antidepressants (3º Amines) (2)

A
  • amitriptyline (Elavil®)
  • imipramine (Tofranil®)
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22
Q

Name TCA (3º Amines) useful for OCD (1)

A

Clomipramine (Anafranil)

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23
Q

Describe: TCA (3º Amines) (5)

A
  • Useful for OCD (clomipramine)
  • melancholic depression
  • requires ECG monitoring
  • check blood levels if using higher dosage
  • highly lethal in overdose
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24
Q

Name examples TCA (2º Amines) (2)

A
  • nortriptyline (Aventyl®)
  • desipramine (Norpramin®)
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25
Q

Describe TCA (2º Amines) (4)

A
  • Preferred to tertiary amines because of lower propensity for anticholinergic adverse effects
  • requires ECG monitoring
  • check blood levels if using higher dosage
  • highly lethal in overdose
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26
Q

Name examples of monoamine oxidase inhibitors MAOI (2)

A
  • phenelzine (Nardil®)
  • tranylcypromine (Parnate®)
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27
Q

Describe monoamine oxidase inhibitors MAOI (2)

A
  • Useful for moderate/severe depression that does not respond to other antidepressants, atypical depression;
  • requires strict adherence to MAOI diet
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28
Q

Name example reversible inhibition of MAO-A (RIMA) (1)

A

moclobemide (Manerix®)

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29
Q

Describe use: Reversible inhibition of MAO-A (RIMA) (1)

A

Useful for depression that does not respond to other antidepressants

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30
Q

Describe example: Noradrenergic and specific serotonin antagonists (NASSA) (3)

A

Useful in depression with prominent features

  • insomnia
  • agitation
  • cachexia
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31
Q

Describe treatment Approach for Depression (5)

A
  • optimization: increase dosage to maximum tolerated or highest therapeutic dosage
  • augmentation: the addition of a medication that is not considered an antidepressant to an antidepressant regimen (i.e. thyroid hormone, lithium, atypical antipsychotics [aripiprazole, quetiapine, olanzapine, risperidone])
  • combination: the addition of another antidepressant to an existing treatment regimen (i.e. the addition of bupropion or mirtazapine to an SSRI or SNRI)
  • switch: change of the primary antidepressant (within or outside a class)
  • note: it is important to fully treat depression symptoms (i.e. to remission) to decrease relapse rates
32
Q

Name antidepressants that are worst in terms of 5HT2C/5HT2A in brain activation (insomnia, anxiety)

A
  • Fluoxetine
  • Paroxetine
33
Q

Describe effect/side effect: Post-Synaptic Serotonin Receptor Stimulated

  • 5HT1A centrally
  • 5HT2A in spinal cord
  • 5HT2C/5HT2A in brain
  • 5HT3A in gut
34
Q

Describe mode of action: SSRI (1)

A

Block serotonin reuptake only

35
Q

Describe side effects: SSRI (14)

A
  • Fewer than TCA, therefore increased compliance
  • CNS:
    • restlessness
    • tremor
    • insomnia
    • headache
    • drowsiness
  • GI:
    • N/V
    • diarrhea
    • abdominal cramps
    • Weight gain
  • Sexual dysfunction:
    • erectile dysfunction
    • anorgasmia
  • CVS:
    • increased HR
    • Serotonin syndrome SIADH
    • EPS
36
Q

Describe Risk in overdose: SSRI (1)

A

Relatively safe in OD

37
Q

Describe drug interactions: SSRI (3)

A
  • MAOI
  • SNRI
  • Some SSRIs (fluoxetine, fluvoxamine, paroxetine) strongly inhibit cytochrome P450 enzymes, therefore will affect levels of drugs metabolized by P450 system
38
Q

Describe mode of action: SNRI (1)

A

Block norepinephrine and serotonin reuptake

39
Q

Describe side effects: SNRI (7)

A
  • Low dose side effects similar to SSRIs (serotonergic)
  • Higher dose side effects:
    • tremors, tachycardia
    • sweating
    • insomnia
    • orthostatic hypotension
    • increase in BP (noradrenergic)
    • SIADH
40
Q

Describe risk of overdose: SNRI (2)

A

Tachycardia and N/V seen in acute overdose

41
Q

Describe drug interactions: SNRI (3)

A
  • MAOI
  • SSRI
  • Low inhibition of cytochrome P450 compounds
42
Q

Describe mode of action: TCA (1)

A

Block norepinephrine reuptake (clomipramine also blocks serotonin reuptake)

43
Q

Describe side effects: TCA (11)

A
  • Anticholinergic effects:
    • Dry mouth
    • urinary retention
    • constipation
    • blurred vision
    • confusional states
  • Noradrenergic effects:
    • tremors
    • tachycardia
    • sweating
  • α-1 adrenergic effects:
    • orthostatic hypotension
    • falls
  • QRS prolongation
44
Q

Describe risk of overdose: TCA (4)

A
  • Toxic in OD
  • 3 times therapeutic dose may be lethal
  • Presentation: anticholinergic effects, CNS stimulation, then depression and seizures
  • ECG: prolonged QRS and QTc (reflect severity)
45
Q

Describe tx of overdose: TCA (6)

A
  • activated charcoal
  • cathartics
  • supportive treatment
  • IV diazepam for seizure
  • physostigmine salicylate for coma
  • Do not give ipecac, as can cause rapid neurologic deterioration and seizures
46
Q

Describe drug interactions: TCA (3)

A
  • MAOI
  • SSRI
  • EtOH
48
Q

Name example: MAOI (1)

A

Phenelzine

49
Q

Describe mode of action: MAOI (1)

A

Irreversible inhibition of monoamine oxidase A and B increases duration that NE and 5HT are in the synaptic cleft by preventing their degradation

50
Q

Name side effets: MAOI (10)

A
  • Antihistamine effects: sedation, weight gain
  • CVS:
    • orthostatic hypotension
    • hypertensive crises with tyramine rich foods (i.e. wine, cheese):
  • headache
  • flushes
  • reflex tachycardia
  • postural hypotension
  • sedation
  • insomnia
  • weight gain
  • Minimal anticholinergic and antihistamine effects
51
Q

Describe risk in overdose: MAOI (2)

A
  • Toxic in OD
  • but wider margin of safety than TCA
52
Q

Describe drug interactions: MAOI (2)

A
  • Hypertensive crises with noradrenergic medications (i.e. TCA, decongestants, amphetamines)
  • Serotonin syndrome with serotonergic drugs (i.e. SSRI, SNRI, tryptophan, dextromethorphan)
53
Q

Name example: NDRI (1)

A

Buproprion

54
Q

Describe mode of action: NDRI (1)

A

Block norepinephrine and dopamine reuptake

55
Q

Name side effects: NDRI (12)

A
  • CNS:
    • dizziness
    • headache
    • tremor
    • insomnia
  • CVS:
    • dysrhythmia
    • HTN
  • GI:
    • dry mouth
    • N/V
    • constipation
    • decreased appetite
  • Other:
    • agitation
    • anxiety
56
Q

Describe risk in overdose: NDRI (2)

A

Tremors and seizures seen in overdose

57
Q

Describe drug interaction: NDRI (2)

A
  • MAOI
  • Drugs that reduce seizure threshold: antipsychotics, systemic steroids, quinolone antibiotics, antimalarial drugs
58
Q

Name example: RIMA (1)

A

Moclobemide

59
Q

Describe mode of action: RIMA (2)

A
  • Reversible inhibitor of monoamine oxidase
  • A leads to increased duration NE and 5HT are in the synaptic cleft by preventing their degradation
60
Q

Name side effects: RIMA (13)

A
  • CNS:
    • dizziness
    • headache
    • tremor
    • insomnia
  • CVS:
    • dysrhythmia
    • hypotension
  • GI:
    • dry mouth
    • N/V
    • diarrhea
    • abdominal pain
    • dyspepsia
  • GU:
    • delayed ejaculation
  • Other: diaphoresis
61
Q

Describe risk in overdose: RIMA (1)

A

Risk of fatal overdose when combined with SSRIs, SNRIs or clomipramine

62
Q

Describe drug interaction: RIMA (3)

A
  • MAOI
  • paroxetine
  • Opioids
63
Q

Name example: NASSA (1)

A

Mirtazapine

64
Q

Describe mode of action: NASSA (1)

A

Enhance central noradrenergic and serotonergic activity by inhibiting presynaptic a-2 adrenergic receptors

65
Q

Name side effects: NASSA (7)

A
  • CNS:
    • sedation
    • dizziness
  • Endocrine:
    • increase in cholesterol
    • triglycerides
    • weight gain
  • GI:
    • constipation
    • ALT
66
Q

Describe risk in overdose: NASSA (1)

A

Relatively safe in OD

67
Q

Describe drug interactions: NASSA (2)

A

MAOI, RIMA

68
Q

Describe: Serotonin Syndrome (4)

A
  • thought to be due to over-stimulation of the serotonergic system
  • can result from medication combinations such as SSRI+SNRI, SSRI or SNRI +MAOI, SSRI+tryptophan, MAOI+meperidine, MAOI+tryptophan
  • rare but potentially life-threatening adverse reaction to SSRIs and SNRIs
  • important to distinguish from NMS
69
Q

Describe symptoms: Serotonin Syndrome (9)

A
  • nausea
  • diarrhea
  • palpitations
  • chills
  • diaphoresis
  • restlessness
  • confusion
  • and lethargy
  • but can progress to myoclonus, hyperthermia, rigor, and hypertonicity
70
Q

Describe tx: Serotonin Syndrome (2)

A
  • discontinue medication
  • and administer emergency medical care as needed
71
Q

Name sx: Discontinuation Syndrome (6)

A

FINISH

  • Flu-like symptoms
  • Insomnia
  • Nausea
  • Imbalance
  • Sensory disturbances
  • Hyperarousal (anxiety/agitation)
72
Q

Describe: Discontinuation Syndrome (3)

A
  • caused by the abrupt cessation of some antidepressants
  • symptoms usually begin within 1-3 d
  • consider avoiding drugs with a short half-life
73
Q

Name most common drugs that cause Discontinuation Syndrome (3)

A
  • paroxetine, fluvoxamine, and venlafaxine (drugs with shortest half-lives)
74
Q

Describe tx: Discontinuation Syndrome (2)

A
  • symptoms may last between 1-3 wk
  • but can be relieved within 24 h by restarting antidepressant at the same dosage the patient was taking and initiating a slower taper over several weeks
75
Q

Name: Symptoms of Antidepressant Discontinuation (6)

A

FINISH

  • Flu-like symptoms
  • Insomnia
  • Nausea
  • Imbalance
  • Sensory disturbances
  • Hyperarousal (anxiety/agitation)

TN Psychiatry (26 decks)

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