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Pharm > Anti-depressants > Flashcards

Anti-depressants Flashcards

1
Q

Anti-depressant uses

A 
Major depression
Persistent depressive disorder
Anxiety Disorders
Trauma and Stressor Related Disorders
Obsessive Compulsive Disorder
Eating Disorders
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2
Q

MAOIs (Monoamine Oxidase Inhibitors)

A

Tranylcypromine
Phenelzine
Isocarboxazid
Selegiline

“MAO Takes Pride in Shanghai”

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3
Q

TCAs (Tricyclic Antidepressants)

A 
Amitriptyline
Nortriptyline
Doxepin
Imipramine
Desipramine
Clomipramine
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4
Q

SSRIs (Selective Serotonin Reuptake Inhibitors)

A 
Fluoxetine
Sertraline
Paroxetine
Citalopram
Escitalopram
Fluvozamine
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5
Q

SNRIs (Serotonin Norepinephrine Reuptake Inhibitors)

A

Venlavaxine
Desvenlafaxine
Duloxetine

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6
Q

Atypical Antidepressants

A 
Mitazepine
Buproprion
Nefazodone
Vilazodone
Vortioxetine
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7
Q

Noradrenergic and serotoneric alpha 2 adrenergic antagonist

A

Mitazepine

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8
Q

NDRI: Norepinephrine and Dopamine reuptake inhibitor

A

Buproprion

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9
Q

Serotonin/NE reuptake inhibitor and serotonin 2A antagonist

A

Nefazodone

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10
Q

Serotonin reuptake blockade and serotonin 1A partial agonist

A

Vilazodone

Vortioxetine

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11
Q

MAOI MOA

A

Block the break down of serotonin, NE, and dopamine by MAO inside the presynaptic terminal

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12
Q

MAO-A MOA

A 
metabolizes catecholamine (NE, Epi), 5HT
metabolizes tyramine and DA
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13
Q

MAO-B MOA

A

metabolizes trace amines and 5HT (at high concentrations)

Metabolizes tyramine and DA

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14
Q

MAO irreversible inhibitors

A

Phenelzine
Tranylcypromine
Selegiline

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15
Q

MAOI irreversible inhibitor MOA

Phenelzine, Tranylcypromine

A

Block MAO-A and MAO B by covalently binding the enzyme, permanently disables the enzyme

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16
Q

MAOI irreversible inhibitor MOA

Selegiline

A

Preferentially inhibits MAO-B

At high doses can inhibit MAO-A

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17
Q

How long does it take an MAO enzyme to be replaced after irreversible inhibitors are stopped

A

10-14 days

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18
Q

How long does it take an MAO enzyme to be replaced after reversible inhibitors are stopped?

A

1 day

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19
Q

MAOI reversible inhibitors

RIMAs: reversible inhibitors of monoamine oxidase

A

Meclobemide

NOT FDA approved in the US

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20
Q

MAOI half-life

A

brief

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21
Q

MAOI side effects

A 
Due to excess serotonin and NE
GI (nausea, constipation, appetite change)
Sleep disturbances
Sexual dysfunction
Sedation
Weight gain
*Hypertensive Crisis
*Serotonin Syndrome
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22
Q

MOAI Hypertensive Crisis

A

Increased NE system

  • Food with high amounts of tyramine (aged cheeses, wines, cured meats); tyramine is metabolized by MAO, unmetabolized tyramine is a pressor
  • Sympathomimetics (cold medicine)
  • cocaine, ecstasy, opioids
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23
Q

How does Selegiline protect against a hypertensive crisis when given as a transdermal patch?

A

Drug goes 1st to brain (higher dose for anti-depressant effect), goes through 1st pass in liver, then goes to GI (lower dose)

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24
Q

MOAI Serotonin Syndrome

A

Increased Serotonin system
If give combo of MAOIs and SSRIs, SNRIs, or TCAs: prevent metabolism of serotonin and reuptake of serotonin > excess serotonin
-Increased reflexes, myoclonus, autonomic dysfunction (unstable BP, increased temp, disorientation)

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25
Q

Food restrictions with MAOIs (severe):

A 
Aged cheeses
Aged meats
All beers on tap
Sauerkraut
Fava or broad bean pods
Banana peels
Soy sauce
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26
Q

Food restrictions with MAOIs (Moderation):

A 
Red wine (4 oz)
White wine (4 oz)
Bottle or canned beer (12 oz)
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27
Q

Food restrictions with MAOIs (mild to none):

A 
Fresh/processed  cheeses
Fresh or processed meats
Bouillon
Chocolate
Avocados
Banana pulp
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28
Q

Which drugs put you at risk for Serotonin Syndrome when combined with a MAOI?

A

Analgesics/Opioids: Meperidine, Methadone, Pentazocine, Tramadol (weak serotonin reuptake inhibitors)
Antidepressants: Mirtazepine, SNRIs, TCAs, SSRIs
OTC cold remedy: Dextromethorphan (weak serotonin reuptake inhibitor)

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29
Q

Which drugs put you at risk for Hypertensive crisis when combined with a MAOI?

A

Analgesics/opioids: Tramadol
Antidepressants: Buproprion, Other MAOIs, Mirtazepine, SNRIs, TCAs
Sympathomimetics
OTC cold remedies

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30
Q

Indication for MAOIs

A

Treatment resistant depression
Treatment resistant anxiety disorders
Treatment resistant atypical depression
Not used much anymore due to SE

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31
Q

TCAs: Tricyclic Antidepressant MOA

A

NE and Serotonin reuptake inhibitors

Also block histamine, acetylcholine, alpha adrenergic receptors!

32
Q

What is the secondary TCA metabolite of Imipramine?

A

Desipramine

33
Q

What is the secondary TCA metabolite of Amitriptyline?

A

Nortriptyline

34
Q

Tertiary TCA metabolite MOA

A

NE= 5-HT reuptake inhibitor

35
Q

Secondary TCA metabolite MOA

A

NE > 5-HT reuptake inhibitor

36
Q

What is unique about Clomipramine and Doxepine TCAs?

A

Tertiary but act like secondary

37
Q

TCA Pharmacokinetics

A 
High lipid solubility
High protein binding
Large volume of distribution
Rapid absorption
Significant 1st pass metabolism
38
Q

TCA side effects

A 
Block H1 rec: sedation, weight gain
Block M1 rec: sedation, confusion, blurred vision, dry mouth, constipation
Block a1 rec: sedation
Increased serotonin: sexual dysfunction
Increased NE: increased BP, sweating
39
Q

TCA Contraindications

A

Elderly (65+) - risk of sedation and confusion, avoid polypharmacy
CNS depressants: alcohol, barbituates, opiates, benzodiazepines
Overdose- hypotension, respiratory depression, confusion, delirium, altered, severe arrhythmias

40
Q

Serotonin Selective Reuptake Inhibitors (SSRIs) MOA

A

Selectively bind the serotonin reuptake pump (much less risk of side effects)

41
Q

Which drug has the longest half life of the SSRIs?

A

Fluoxetine has the longest half life (7-15 days)- could take 5 weeks before completely gone!

42
Q

Which SSRIs inhibit CYP450 2D6 enzymes?

A

Fluoxetine and paroxetine are strong inhibitors

43
Q

Which SSRI has significantly less protein binding than the others?

A

Escitalopram (56%)

44
Q

Which SSRIs have the shortest half lives?

A

Paroxetine and Fluvoxamine

45
Q

Which SSRIs have the high risk for discontinuation syndrome?

A

Paroxetine and Fluvoxamine

46
Q

Describe the relationship between Citalopram and escitalopram?

A

Escitalopram is purified S isomer of citalopram

47
Q

Characteristics of SSRI side effects

A

Occur prior to onset of anti-depressant effect
Are dose dependent
May happen once, intermittently, or chronically
May have different levels of severity

48
Q

Common SSRI side effects

A 
*Due to excessive serotonin*
GI
Anxiety
CNS
Sexual Dysfunction
49
Q

Symptoms of SSRI discontinuation syndrome

A

Dizziness, nausea, fatigue, headache, insomnia, restlessness, unstable gait, brain zaps

50
Q

Serotonin Norepinephrine Reuptake Inhibitors (SNRIs)

A

Blocks serotonin and NE reuptake pumps

At high dose can block dopamine reuptake pump

51
Q

What is the most commonly used SNRI?

A

Venlafaxine

52
Q

Which SSRI has the highest affinity for the 5-HT transporter?

A

Paroxetine

53
Q

Which SSRI is the least 5-HT selective?

A

Fluoxetine

54
Q

Which SSRI is most likely to have drug-drug interactions due to inhibition of CYP enzymes?

A

Fluvoxamine

55
Q

Which SNRI has the shortest half life?

A

Venlafaxine

56
Q

Which SNRI has the greatest risk of causing discontinuation syndrome if stopped abruptly?

A

Venlafaxine

also Desvenlafaxine

57
Q

What is the metabolite of Venlafaxine?

A

Desvenlafaxine

58
Q

Mirtazapine MOA

A

Block a-2 presynaptic autoreceptors on NE and 5HT neurons, leads to increased NE and 5HT

Also blocks Histamine, 5HT2A, 5HT2C, 5HT3

59
Q

Mirtazapine Side effects (or lack thereof…)

A

Block histamine: weight gain, dry mouth, sedation

Block 5HT2A, 5HT2C, 5HT3: NO nausea, NO sexual dysfunction, NO insomnia, NO anxiety!

60
Q

Buproprion MOA

A

NE and DA reuptake inhibitor

No effects on 5HT, histamine

61
Q

Burproprion side effects (or lack thereof…)

A

No 5HT related (sexual)
No H1 related (sedation/weight gain)
Increased seizure risk at high doses

62
Q

Can Buproprion and Mirtazapine be used in combination with SSRIs and SNRIs?

A

Yes! Especially if you are only getting partial improvement in depression symptoms

63
Q

Nefazodone MOA

A

Blocks 5-HT reuptake (SSRI effects)

5-HT2A receptor antagonist: no sexual side effects

64
Q

Nefazodone Side effects (or lack thereof…)

A

Mild sedation

No sexual side effects

65
Q

Vilazodone MOA

A

Blocks 5HT reuptake (SSRI)

Partial agonist of 5-HT1A receptors (additional help for depression/anxiety)

66
Q

Vilazodone side effects (or lack thereof…)

A

No weight gain
No sexual side effects
GI, nausea, vomiting, diarrhea
Insomnia

67
Q

Vortioxetine MOA

A

Blocks 5-HT reuptake (SSRI)
Agonist at 5-HT1A
Partial agonist at 5-HT1B
Antagonist at 5-HT3 (less GI) and 5-HT7

68
Q

Vortioxetine side effects (or lack thereof)

A

No weight gain
No sexual side effects (except at high dose)
GI (nausea > vomiting/diarrhea)

69
Q

After stopping an MAOI, how long to wait until starting new antidepressant?
What are you waiting for?
What if MAOI is reversible?

A

10-14 days
Neurons to regenerate MAO
Only need to wait 1 day

70
Q

After stopping other anti-depressants, how long wait until starting MAOI?
What are you waiting for?
Are there any anti-depressants that would require a longer wait before starting MAOI?

A

Need to wait ~1 week (5 half life for drug to clear)
Drugs to clear
Fluoxetine (~5 weeks)

71
Q

What is the risk of overlapping an anti-depressant with an MAOI?

A

Risk of serotonin syndrome (increased serotonin)

Risk of hypertensive crisis (increased NE)

72
Q

Which drug inhibits CYP 1A2?

A

Fluvoxamine

73
Q

Which drugs inhibit CYP2C9 and CYP2C19?

A

Fluvoxamine

Fluoxetine

74
Q

Which drugs inhibit CYP2D6?

A

Paroxetine
Fluoxetine
Buproprion

75
Q

Which drugs inhibit CUP3A4?

A

Nefazadone

Fluxoxamine

76
Q

Which 2 drugs are the MOST likely to produce interactions with other drugs?

A

Fluvoxamine

Fluoxetine

Pharm (20 decks)

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