Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Where is MAOa located and what does it metabolize?

A

brain, liver, GI

NE, 5-HT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Where is MAOb located and what does it metabolize?

A

brain, platelets

DA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are the MAOIs?

A

1) phenlzine
2) tranylcypromine
3) selegiline

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What are the ADRs of MAOIs?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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]

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the interactions for MAOIs?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What are the additional indications of MAOIs?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

PK data for phenelzine:

A

t1/2 = 12 hours

liver metabolized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

PK data for tranylcypromine:

A

t1/2 = 2.5 hours

CYP2A6, C19, 2D6, MAOa, MAOb

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

PK data for selegiline:

A

t1/2 = 10 hours

liver metabolized

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is the MoA for selegiline?

A

MAOI

– selective for MAOb

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the MoA of TCAs?

A

SERT, NET, a1 antagonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are the TCA agents?

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What are the TCA effects in normal people?

A
    • no mood-elevating effect

- - sleepiness, lightheadedness (used for insomnia)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What does H1 antagonism by TCAs cause?

A

1) weight gain
2) drowsiness
3) sedation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What does M1 antagonism by TCAs cause?

A

anti-sludge

    • drowsiness
    • glaucoma
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the sexual dysfunction sxs caused by TCAs?

A

1) ED

2) anorgasmia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
What TCAs have alternate indications? What are they?
1) amitriptyline - - anxiety, psychosis, ADHD, bipolar 2) clomipramine - - anxiety, OCD, pain 3) desipramine - - ADHD 4) maprotiline - - panic disorder
26
PK data for amitriptyline:
t1/2 = 22-24 h | CYP2D6
27
PK data for amoxapine:
t1/2 = 8-10 h (active met 30h)
28
PK data for clomipramine:
t1/2 = 32 hours (active met = 70 hours) | CYP2D6
29
PK data for desipramine:
t1/2 = 24-36 hrs
30
PK data for imipramine:
t1/2 = 20 hours | CYP1A2, 2C19, 2D6
31
PK data for maprotiline:
t1/2 = 27-48 h
32
PK data for nortriptyline:
t1/2 = 16-90 h
33
Which TCAs are secondary vs. tertiary amines?
all secondary except: - - imipramine - - clomipramine - - amitriptyline
34
ADRs of amitriptyline:
severe QT prolongation
35
ADRs of amoxapine:
- - tachycardia, seizures - - hypomania - - agranulocytosis - - NMS - - tardive dyskinesia
36
ADRs of imipramine
agranulocytosis
37
What are the SSRI agents?
1) citalopram 2) fluoxetine 3) fluvoaxime 4) paroxetine 5) sertraline
38
All SSRIs are approved for:
depressive disorder panic disorder -- exception: fluvoxamine doesn't have panic disorder
39
What are the other indications of the SSRIs?
``` all except citalopram -- + OCD fluvoxamine: -- + anxiety fluoxetine: -- + PMDD, bulimia nervosa paroxetine: -- + anxiety, PMDD, hot flashes, PTSD ```
40
MoA of SSRIs:
inhibit SERT
41
What are the ADRs of serotonergic syndrome
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
What are the ADRs of SSRIs?
1) nausea, diarrhea 2) weight gain 3) stimulation - - anxiety, nervousness, insomnia 4) sex dysfunction - - delayed ejaculation, anorgasmia 5) black box
43
What is the use-limiting ADR for SSRIs?
stimulation | -- 1/3 to 1/2 of patients are limited
44
Which SSRI is FDA-approved for OCD?
fluvoxamine
45
PK data for citalopram:
t1/2 = 24-36 h | CYP2C19, 3A4, 2D6
46
PK data for fluoxetine:
t1/2 = 24-96 hours
47
PK data for fluvoxamine:
t1/2 = 6-26 hours | CYP1A2, 2C19
48
PK data for paroxetine:
t1/2 = 18-24 hours
49
PK data for sertraline:
t1/2 = 24-36 hours | CYP2D6, 2B6
50
ADRs of celexa:
QT prolongation | -- FDA recommends less than 40 mg/day
51
What are the ADRs of fluoxetine?
-- urticaria, rash, itchiness
52
What are the ADRs of paroxetine?
mania | caution withdrawal reaction
53
What are the ADRs of sertraline?
stimulation | agitation
54
What are the DDIs for sertraline?
pimozide (increased AUC, QT prolongation) | disulfiram (sertraline concentrate has EtOH)
55
What are the SNRI agents?
venlafaxine | duloxetine
56
What is the MoA of SNRIs?
inhibit SERT and NET
57
What are ADRs of SNRIs?
same as SSRIs | -- add constipation
58
PK data for venlafaxine:
t1/2 = 5 hours (active met = 11 hours) | CYP2C19, 3A4, 2D6
59
PK data for duloxetine:
t1/2 = 12 hours | CYP2D6, 1A2
60
What are the indications for SNRIs?
depressive disorders and anxiety disorders for duloxetine -- + neuropathic pain
61
What are the C/Is of duloxetine?
hepatic insufficiency | renal disease
62
What are the NRIs?
bupropion
63
What is bupropion indicated for?
depressive disorder | smoking cessation
64
PK data for bupropion:
t1/2 = 14-21 hr (active mets = 37h) | CYP1A2, 2A6, 2C9, 3A4, 2E1, 2C19
65
What are ADRs of bupropion?
stimulation - - agitation - - anorexia - - insomnia
66
What are the monoamine receptor antagonists?
1) mirtazipine | 2) trazodone
67
MoA of mirtazipine:
``` a2 antagonist 5-HT 2c antagonist 5-HT 3 antagonist -- increases 5-HT release -- increases NE release ```
68
MoA of trazodone:
5-HT 2A antagonist 5-HT 2C antagonist H1 antagonist weak SERT-inhibitor
69
PK data for mirtazipine:
t1/2 = 20-40 hours | CYP1A2, 2D6, 3A4
70
PK data for trazodone:
t1/2 = 6-12 hours
71
ADRs of mirtazipine:
sedation! dry mouth weight gain
72
ADRs of trazodone:
cardiac arrhythmia | hepatotoxicity
73
What are the indications of the monoamine receptor antagonists?
depressive disorders + trazodone: anxiety
74
What are the phases of pharmacotherapy of depression? How long does each last?
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
What are the GoTs of the continuation vs. maintenance phases?
continuation: - - eliminate residual symptoms, prevent relapse maintenance: - - prevent recurrence of sxs
76
How long until peak antidepressant effect?
2-4 weeks
77
What drugs besides lithium are used for bipolar disorder?
1) ASDs - - carbamazepine, valproate, lamotrigine 2) antipsychotics - - olanzapine, risperidone, quetiapine 3) other drugs - - BZDs, memantine, amantadine, ketamine 4) antidepressants
78
What is the MoA of lithium carbonate?
inhibits inositol monophosphatase | -- disrupts a-adrenergic signaling
79
PK data for lithium:
t1/2 = 24 hours - - good GI absorption - - steady state CNS in 6-10 days - - 95% renal excretion - - 70-80% reabsorbed (Na+ transporter)
80
What is the therapeutic blood concentration for lithium?
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
Lithium toxicity occurs at what blood range?
acute: 1.3-1.4 mmol/L chronic: any range
82
Relapse/recurrence of bipolar sxs while on lithium treatment is associated with what blood concentration?
less than 0.6 mmol/L
83
What are the indications for lithium?
bipolar
84
What are the ADRs of lithium?
1) fatigue, sedation 2) dry mouth - - excessive thirst and urination 3) weight gain, acne 4) slurred speech, ataxia, fine hand tremor, muscle weakness
85
To what ADRs of lithium does tolerance develop?
after 4 weeks, all sxs except: - - tremor - - urination/thirst
86
How are the ADRs of lithium managed?
beta-blocker for tremor | H2O intake regulated for urination/thirst
87
What are the sxs of acute toxicity of lithium?
mainly CNS -- coma - - muscle rigidity, hyperreflexia, tremor, muscle twitching - - kidney failure
88
How is lithium toxicity treated?
symptomatic treatment | dialysis if severe poisoning
89
What are the interactions of lithium?
``` Na deficiency -- thiazides (Na-depleting) NSAIDs, TCNs -- decrease Li clearance excess sweating -- contributes to Li toxicity ```
90
When is lithium conraindicated?
pregnancy | -- increases risk for congenital malformation
91
What are the categories of bipolar sxs and when do they usually appear?
late adolescence/early adulthood (depression first) - - manic mood - - depressive mood - - psychotic symptoms - - cognitive symptoms
92
What are the manic sxs of bipolar disorder?
1) amplified mood, energy 2) rapid speech, thoughts 3) hypersexuality 4) recklessness 5) decreased need for sleep
93
What are the depressive sxs of bipolar disorder?
1) depression 2) anxiety, irritability 3) hostility, violence 4) suicide
94
What are the psychotic symptoms of bipolar disorder?
delusions hallucinations formal thought disorder
95
What are the cognitive symptoms of bipolar disorder?
1) racing thoughts 2) distractibility 3) disorganization 4) inattentiveness
96
What is thought to be the cause of bipolar disorder?
imbalance of monoamines and other NTs
97
When is bipolar disease diagnosed?
only in manic phase! | -- need neuropsychiatric history
98
What is the prevalence of bipolar disease (and suicide in patients)?
4% of adults, 1% of kids | -- 20-25% attempt suicide
99
How was lithium historically used?
gout salt sub in CVD 7-up -- tried for mania in humans after sedation was noticed in guinea pigs
100
How is lithium supplied for bipolar disorder treatment?
lithium carbonate (lithobid)
101
What black box is on all antidepressants?
may increase risk of suicide in patients under the age of 25

PHS 931 (29 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions