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PHS 931 > Block 4 Lecture 7 -- Antidepressants > Flashcards

Block 4 Lecture 7 -- Antidepressants Flashcards

1
Q

What is the MoA of MAOIs?

A

irreversibly blocks MAOa and MAOb

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2
Q

Where is MAOa located and what does it metabolize?

A

brain, liver, GI

NE, 5-HT

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3
Q

Where is MAOb located and what does it metabolize?

A

brain, platelets

DA

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4
Q

What are the MAOIs?

A

1) phenlzine
2) tranylcypromine
3) selegiline

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5
Q

What are the ADRs of MAOIs?

A

1) hepatotoxic
2) stimulation, insomnia, agitation
3) HTN
4) toxicity/od

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6
Q

What are symptoms of toxicity/od? How is it treated?

A

1) anxiety
2) HA
3) sweating, fever
4) seizures
5) sleepiness

treat sxs
– hospitalize x 1 week to rebuild normal [MAO]

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7
Q

What are the interactions for MAOIs?

A

1) sympathomimetic amines
- - inhaled b-agonists
- - stimulants (adderall)
2) PD drugs
3) tyramine

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8
Q

Where is tyramine found?

A

– found in fermented foods (beer, red wine, cheese, aged things)

ok in small amounts:
– yogurt, chocoalte, caffeine, ripe fruits ok in small amounts

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9
Q

What are the additional indications of MAOIs?

A

1) phenelzine
- - anxiety disorders, PTSD
2) tranylcypromine
- - anxiety disorders
3) selegiline
- - PD

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10
Q

PK data for phenelzine:

A

t1/2 = 12 hours

liver metabolized

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11
Q

PK data for tranylcypromine:

A

t1/2 = 2.5 hours

CYP2A6, C19, 2D6, MAOa, MAOb

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12
Q

PK data for selegiline:

A

t1/2 = 10 hours

liver metabolized

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13
Q

What is the MoA for selegiline?

A

MAOI

– selective for MAOb

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14
Q

What is the MoA of TCAs?

A

SERT, NET, a1 antagonists

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15
Q

What are the TCA agents?

A

1) amitriptyline
2) amoxapine
3) clomipramine
4) desipramine
5) imipramine
6) maprotiline

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16
Q

What are the TCA effects in normal people?

A
    • no mood-elevating effect

- - sleepiness, lightheadedness (used for insomnia)

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17
Q

What are the on-target effects of TCAs in depressed patients?

A

– elevation in mood after 2-3 weeks

not used on PRN basis

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18
Q

What are the causes/categories of ADRs of TCAs?

A

1) H1 antagonism
2) mAChR (M1) antagonism
3) a1 antagonism
4) Na-channel antagonism
5) sexual dysfunction
6) CNS ADRs

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19
Q

What does H1 antagonism by TCAs cause?

A

1) weight gain
2) drowsiness
3) sedation

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20
Q

What does M1 antagonism by TCAs cause?

A

anti-sludge

    • drowsiness
    • glaucoma
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21
Q

What does Na-channel antagonism by TCAs cause?

A

1) QT prolongation
2) palpitations
3) arrhythmias (hi-dose)
4) cardiac arrest
5) seizures (lowered threshold)

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22
Q

What are the sexual dysfunction sxs caused by TCAs?

A

1) ED

2) anorgasmia

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23
Q

What are the CNS side effects of TCAs?

A 
confusion
memory impairment
hallucinations
disorientation
restlessness
agitation
insomnia
nightmares
-- black box: suicide younger than 25 yo
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24
Q

What are drug-drug interactions of TCAs?

A

1) central depressants
2) dirty drugs
3) drugs that increase presynaptic NTs
- - St. Johns wort
4) 5-HT precursors
- - 5-HTP
- - Trp

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25
Q

What TCAs have alternate indications? What are they?

A

1) amitriptyline
- - anxiety, psychosis, ADHD, bipolar
2) clomipramine
- - anxiety, OCD, pain
3) desipramine
- - ADHD
4) maprotiline
- - panic disorder

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26
Q

PK data for amitriptyline:

A

t1/2 = 22-24 h

CYP2D6

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27
Q

PK data for amoxapine:

A

t1/2 = 8-10 h (active met 30h)

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28
Q

PK data for clomipramine:

A

t1/2 = 32 hours (active met = 70 hours)

CYP2D6

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29
Q

PK data for desipramine:

A

t1/2 = 24-36 hrs

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30
Q

PK data for imipramine:

A

t1/2 = 20 hours

CYP1A2, 2C19, 2D6

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31
Q

PK data for maprotiline:

A

t1/2 = 27-48 h

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32
Q

PK data for nortriptyline:

A

t1/2 = 16-90 h

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33
Q

Which TCAs are secondary vs. tertiary amines?

A

all secondary except:

    • imipramine
    • clomipramine
    • amitriptyline
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34
Q

ADRs of amitriptyline:

A

severe QT prolongation

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35
Q

ADRs of amoxapine:

A
    • tachycardia, seizures
    • hypomania
    • agranulocytosis
    • NMS
    • tardive dyskinesia
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36
Q

ADRs of imipramine

A

agranulocytosis

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37
Q

What are the SSRI agents?

A

1) citalopram
2) fluoxetine
3) fluvoaxime
4) paroxetine
5) sertraline

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38
Q

All SSRIs are approved for:

A

depressive disorder
panic disorder
– exception: fluvoxamine doesn’t have panic disorder

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39
Q

What are the other indications of the SSRIs?

A 
all except citalopram
-- + OCD
fluvoxamine:
-- + anxiety
fluoxetine:
-- + PMDD, bulimia nervosa
paroxetine:
-- + anxiety, PMDD, hot flashes, PTSD
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40
Q

MoA of SSRIs:

A

inhibit SERT

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41
Q

What are the ADRs of serotonergic syndrome

A

central and peripheral

1) diarrhea
2) euphoria, dizziness, loss of consciousness
3) REM, mydriasis, hyperreflexia
4) shivering, high body temp, seizures
5) irregular heart beat, death

42
Q

What are the ADRs of SSRIs?

A

1) nausea, diarrhea
2) weight gain
3) stimulation
- - anxiety, nervousness, insomnia
4) sex dysfunction
- - delayed ejaculation, anorgasmia
5) black box

43
Q

What is the use-limiting ADR for SSRIs?

A

stimulation

– 1/3 to 1/2 of patients are limited

44
Q

Which SSRI is FDA-approved for OCD?

A

fluvoxamine

45
Q

PK data for citalopram:

A

t1/2 = 24-36 h

CYP2C19, 3A4, 2D6

46
Q

PK data for fluoxetine:

A

t1/2 = 24-96 hours

47
Q

PK data for fluvoxamine:

A

t1/2 = 6-26 hours

CYP1A2, 2C19

48
Q

PK data for paroxetine:

A

t1/2 = 18-24 hours

49
Q

PK data for sertraline:

A

t1/2 = 24-36 hours

CYP2D6, 2B6

50
Q

ADRs of celexa:

A

QT prolongation

– FDA recommends less than 40 mg/day

51
Q

What are the ADRs of fluoxetine?

A

– urticaria, rash, itchiness

52
Q

What are the ADRs of paroxetine?

A

mania

caution withdrawal reaction

53
Q

What are the ADRs of sertraline?

A

stimulation

agitation

54
Q

What are the DDIs for sertraline?

A

pimozide (increased AUC, QT prolongation)

disulfiram (sertraline concentrate has EtOH)

55
Q

What are the SNRI agents?

A

venlafaxine

duloxetine

56
Q

What is the MoA of SNRIs?

A

inhibit SERT and NET

57
Q

What are ADRs of SNRIs?

A

same as SSRIs

– add constipation

58
Q

PK data for venlafaxine:

A

t1/2 = 5 hours (active met = 11 hours)

CYP2C19, 3A4, 2D6

59
Q

PK data for duloxetine:

A

t1/2 = 12 hours

CYP2D6, 1A2

60
Q

What are the indications for SNRIs?

A

depressive disorders and anxiety disorders

for duloxetine
– + neuropathic pain

61
Q

What are the C/Is of duloxetine?

A

hepatic insufficiency

renal disease

62
Q

What are the NRIs?

A

bupropion

63
Q

What is bupropion indicated for?

A

depressive disorder

smoking cessation

64
Q

PK data for bupropion:

A

t1/2 = 14-21 hr (active mets = 37h)

CYP1A2, 2A6, 2C9, 3A4, 2E1, 2C19

65
Q

What are ADRs of bupropion?

A

stimulation

    • agitation
    • anorexia
    • insomnia
66
Q

What are the monoamine receptor antagonists?

A

1) mirtazipine

2) trazodone

67
Q

MoA of mirtazipine:

A 
a2 antagonist
5-HT 2c antagonist
5-HT 3 antagonist
-- increases 5-HT release
-- increases NE release
68
Q

MoA of trazodone:

A

5-HT 2A antagonist
5-HT 2C antagonist
H1 antagonist
weak SERT-inhibitor

69
Q

PK data for mirtazipine:

A

t1/2 = 20-40 hours

CYP1A2, 2D6, 3A4

70
Q

PK data for trazodone:

A

t1/2 = 6-12 hours

71
Q

ADRs of mirtazipine:

A

sedation!
dry mouth
weight gain

72
Q

ADRs of trazodone:

A

cardiac arrhythmia

hepatotoxicity

73
Q

What are the indications of the monoamine receptor antagonists?

A

depressive disorders

+ trazodone: anxiety

74
Q

What are the phases of pharmacotherapy of depression? How long does each last?

A

1) acute phase (6-16 weeks)
2) continuation phase (4-9 mos after initial sxs reside)
3) maintenance phase (9-24 mos)
4) discontinuation phase

75
Q

What are the GoTs of the continuation vs. maintenance phases?

A

continuation:
- - eliminate residual symptoms, prevent relapse
maintenance:
- - prevent recurrence of sxs

76
Q

How long until peak antidepressant effect?

A

2-4 weeks

77
Q

What drugs besides lithium are used for bipolar disorder?

A

1) ASDs
- - carbamazepine, valproate, lamotrigine
2) antipsychotics
- - olanzapine, risperidone, quetiapine
3) other drugs
- - BZDs, memantine, amantadine, ketamine
4) antidepressants

78
Q

What is the MoA of lithium carbonate?

A

inhibits inositol monophosphatase

– disrupts a-adrenergic signaling

79
Q

PK data for lithium:

A

t1/2 = 24 hours

    • good GI absorption
    • steady state CNS in 6-10 days
    • 95% renal excretion
    • 70-80% reabsorbed (Na+ transporter)
80
Q

What is the therapeutic blood concentration for lithium?

A

0.6-1.2 mmol/L

    • mania: 0.6-1.0 mmol/L
    • maintenance: 0.6-0.8 mmol/L
    • depression: 0.4-0.8 mmol/L
81
Q

Lithium toxicity occurs at what blood range?

A

acute: 1.3-1.4 mmol/L
chronic: any range

82
Q

Relapse/recurrence of bipolar sxs while on lithium treatment is associated with what blood concentration?

A

less than 0.6 mmol/L

83
Q

What are the indications for lithium?

A

bipolar

84
Q

What are the ADRs of lithium?

A

1) fatigue, sedation
2) dry mouth
- - excessive thirst and urination
3) weight gain, acne
4) slurred speech, ataxia, fine hand tremor, muscle weakness

85
Q

To what ADRs of lithium does tolerance develop?

A

after 4 weeks, all sxs except:

    • tremor
    • urination/thirst
86
Q

How are the ADRs of lithium managed?

A

beta-blocker for tremor

H2O intake regulated for urination/thirst

87
Q

What are the sxs of acute toxicity of lithium?

A

mainly CNS – coma

    • muscle rigidity, hyperreflexia, tremor, muscle twitching
    • kidney failure
88
Q

How is lithium toxicity treated?

A

symptomatic treatment

dialysis if severe poisoning

89
Q

What are the interactions of lithium?

A 
Na deficiency
-- thiazides (Na-depleting)
NSAIDs, TCNs
-- decrease Li clearance
excess sweating
-- contributes to Li toxicity
90
Q

When is lithium conraindicated?

A

pregnancy

– increases risk for congenital malformation

91
Q

What are the categories of bipolar sxs and when do they usually appear?

A

late adolescence/early adulthood (depression first)

    • manic mood
    • depressive mood
    • psychotic symptoms
    • cognitive symptoms
92
Q

What are the manic sxs of bipolar disorder?

A

1) amplified mood, energy
2) rapid speech, thoughts
3) hypersexuality
4) recklessness
5) decreased need for sleep

93
Q

What are the depressive sxs of bipolar disorder?

A

1) depression
2) anxiety, irritability
3) hostility, violence
4) suicide

94
Q

What are the psychotic symptoms of bipolar disorder?

A

delusions
hallucinations
formal thought disorder

95
Q

What are the cognitive symptoms of bipolar disorder?

A

1) racing thoughts
2) distractibility
3) disorganization
4) inattentiveness

96
Q

What is thought to be the cause of bipolar disorder?

A

imbalance of monoamines and other NTs

97
Q

When is bipolar disease diagnosed?

A

only in manic phase!

– need neuropsychiatric history

98
Q

What is the prevalence of bipolar disease (and suicide in patients)?

A

4% of adults, 1% of kids

– 20-25% attempt suicide

99
Q

How was lithium historically used?

A

gout
salt sub in CVD
7-up
– tried for mania in humans after sedation was noticed in guinea pigs

100
Q

How is lithium supplied for bipolar disorder treatment?

A

lithium carbonate (lithobid)

101
Q

What black box is on all antidepressants?

A

may increase risk of suicide in patients under the age of 25

PHS 931 (29 decks)

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