Antidepressants-Craviso Flashcards

1
Q

What do the current antidepressants do?

A

target monoamine levels

take several weeks to work as they increase BDNF levels

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2
Q

What percentage of patients are refractory to multiple antidepressants?

A

20%

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3
Q

What are the 4 major classes of antidepressants?

A
  1. SSRIs. First line.
  2. SNRIs
  3. Newer Antidepressant: inhibit reuptake of dopamine
  4. Monoamine Oxidase INhibitors-inhibit metabolism of NE & serotonin
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4
Q

Which category do tricyclic antidepressants fall into?

A

SNRI
work on a variety of receptors
NE & serotonin affected
side effects!!!

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5
Q

Give examples of common SSRIs.

A
FLUOXETINE (Prozac; Prozac Weekly)
SERTRALINE (Zoloft)
PAROXETINE (Paxil)
CITALOPRAM (Celexa) 
ESCITALOPRAM (Lexapro)
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6
Q

What is an important effect that SSRis have on the liver?

A

some of them can be potent inhibitors of cytochrome P450 enzymes. Esp CYP2D6. If another drug metabolized by this is taken…can build up to toxic levels.
they are themselves metabolized in the liver

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7
Q

Which SSRis have a high & low potential for inhibiting Cyt p450 enzymes?

A

high potential: fluoxetine, paroxetine

low potential: citalopram, escitalopram

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8
Q

What are important adverse side effects of SSRIs?

A
sexual dysfunction
GI issues
insomnia, restlessness
anorexia, weight loss or weight gain
QT prolongation w/ citalopram
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9
Q

Which SSRI if taken during pregnancy can cause cardiovascular malformations of the fetus?

A

paroxetine

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10
Q

What can happen if you have taken an SSRI long term & stop suddenlY?

A

nausea, dizziness, anxiety, tremor, palpitations

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11
Q

Once again, which SSRI can cause QT prolongation?

A

citalopram

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12
Q

Which SSRIs can cause serotonin syndrome?

A

MAO inhibitors

or other drugs that enhance serotonin neurotransmission

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13
Q

What are the symptoms of serotonin syndrome?

A

Cognitive: headache, confusion
Autonomic: shivering, sweating
Somatic: tremor, hyperreflexia

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14
Q

What is the issue with prescribing SSRis to adolescents?

A

linked to increased risk of suicide

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15
Q

What are the 2 antidepressants approved for used in children & adolescents?

A

fluoxetine (SSRI)

escitalopram

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16
Q

What are additional uses of SSRIs, aside from alleviating depression?

A
anxiety disorders
seasonal affective disorder
bulimia nervosa
migraine prophylactic
PMS, hot flashes
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17
Q

Which drugs is used for seasonal affective disorder?

A

paroxetine

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18
Q

Which drug is used for bulimia nervosa?

A

fluoxetine

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19
Q

Which drug is used for migraine prophylactic?

A

fluoxetine

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20
Q

Which drug is used for PMS & hot flashes?

A

paroxetine

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21
Q

What are important SNRIs to keep in mind?

A

Venlafaxine: Effexor
Duloxetine: Cymbalta
TCAs

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22
Q

What are some tricyclic antidepressants?

A

nortriptyline, imipramine, amitryptyline

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23
Q

What are some important new antidepressants?

A

Bupropion-Wellbutrin (dopamine reuptake inihbitor)
Mirtazapine-Remeron
Trazodone-Desyrel
Vilazodone-Virbyl

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24
Q

What are 2 important MAOIs?

A

Selegiline-Eldepryl

Phenelzine-Nardil

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25
Q

What are some important classes of bipolar disorder medications?

A
Lithium
Valproic Acid
Carbamazepine
Atypical antipsychotics
Benzodiazepines
Lamotrigine-only bipolar depression
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26
Q

Which drugs belong in the category of atypical antipsychotics used to treat bipolar disorder?

A
QUETIAPINE (Seroquel)
OLANZAPINE (Zyprexa)
RISPERIDONE (Risperdal)
ARIPIPRAZOLE (Abilify)
LURASIDONE (Latuda) – bipolar depression only 
ASENAPINE (Saphris)
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27
Q

What are 2 important benzodiazepines used to treat bipolar disorder?

A

lorazepam (ativan)

clonazepam (klonopin)

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28
Q

What does venlafaxine/effexor do?

A

SNRI
blocks reuptake of NE & 5-HT
weakly inhibits DM reuptake

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29
Q

What are the adverse side effects of venlafaxine/effexor?

A

same as SSRIs: sexual dysfunction, insomnia, GI)

could increase BP

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30
Q

What are additional uses of venlafaxine/effexor? What is the name of its metabolite?

A

anxiety disorders
neuropathic pain
**desvenlafaxine (pristiq)

31
Q

What does duloxetine/cymbalta do? What are its adverse side effects?

A

SNRI

contraindicated if you have liver problems

32
Q

What are additional uses for duloxetine/cymbalta?

A

fibromyalgia
diabetic peripheral neuropathy
generalized anxiety disorder

33
Q

What do tricyclic antidepressants do?

A

block reuptake of NE & 5-HT

type of SNRIs

34
Q

Which TCAs block 5-HT more than NE?

A

imipramine/tofranil & amitriptyline/elavil

35
Q

Which TCAs block NE more than 5-HT?

A

nortriptyline/aventyl

36
Q

Why aren’t TCAs used anymore?

A
can be fatal w/ overdose
can commit suicide w/ this drug
lower seizure threshold
block 3 types of receptors to varying degrees: mACH, alpha1, H1
cardiotoxicity
**also: sexual dysfunction & weight gain
37
Q

What is an additional use of amitriptyline?

A

migraine prophylactic

38
Q

Which TCA has the greatest ability to block additional receptors?

A

amitryptiline

39
Q

What are the effects of blocking mACH?

A

sedation, cognitive impairment, confusion, delirium, blurred vision, dry mouth, tachycardia, urinary retention

40
Q

What are the effects of blocking alpha 1 receptors w/ TCAs?

A

orthostatic hypotension, sedation

41
Q

What is the effect of blocking H1 receptor w/ a TCA?

A

sedation

42
Q

What should TCAs not be taken with?

A

MAO inhibitors–risk of HTN & serotonin syndrome
anticholinergics & antihistamines-they already block these receptors enough!
CNS depressants-they already cause sedation people!!

43
Q

What does bupropion or Wellbutrin do?

A

blocks reuptake of dopamine, also possibly some NE & 5-HT

44
Q

What are the adverse side effects of buproprion aka Wellbutrin?

A

restlessness, insomnia, anxiety
risk of seizure activity (dose-related)
contraindicated for those with a history of seizures, and eating disorders (electrolyte imbalances)
may precipitate psychotic episodes in susceptible individuals
b/c schizophrenia etc are due to excessive dopamine levels.

Note: few sexual side effects compared to other antidepressants

45
Q

WHat is zyban?

A

sustained release form of Wellbutrin used as an aid for smoking cessation

46
Q

What does mirtazapine/remeron do?

A

new antidepressant
antagonist @ presynaptic alpha 2 adrenergic autoreceptors (no neg. feedback for NE & 5-HT release).
blocks 5-HT2 & 5-HT3 receptors
no sexual side effects

47
Q

What are the adverse side effects of mirtazapine? How does this relate to its old use?

A

sedation, somnolence
dizziness
stimulates appetite, weight gain
**used to be used to treat insomnia

48
Q

What does trazodone/desyrel do?

A

blocks 5-HT reuptake

antagonist @ 5-HT2 receptors & 5-HT1a

49
Q

What are the adverse side effects of trazodone?

A
significant drowsiness and dizziness
GI upset (nausea and vomiting)
orthostatic hypotension 
can cause protracted erection (priapism)
50
Q

WHat does vilazodone/vibryd do?

A

SSRI

partial agonist of 5-HT1a receptors

51
Q

What are the adverse side effects of vilazodone?

A

insomnia
GI disturbances
no sexual side effects, no weight gain

52
Q

HOw do MAOIs work?

A

block MAO, the enzyme in the nerve terminal that converts NTs into inactive products

53
Q

When should MAOIs be prescribed?

A

for those who can’t tolerance normal antidepressants
last choice, tho b/c could get HTN crisis w/ certain foods
also used in Parkinson’s disease.

54
Q

Why can MAOIs cause a massive HTN crisis w/ ingestion of certain foods?

A

MAO also found in the liver where it breaks down tyrimine.

somehow displaces NE in nerve terminals when it is blocked in the liver. Massive release of NE causes HTN crisis.

55
Q

Which foods are high in tyrimine?

A

salami
certain cheeses
red wine

56
Q

What is selegiline/eldepryl?

A

MAOI
reversible inhibitor of MAO
can be transdermal as ensam
bypasses the gut so central MAO enzymes are intact, less risk of hypertensive crisis

57
Q

WHat is phenelzine/nardil? What are some of its negative side effects?

A
irreversible inhibitor of MAO
sexual impotence
insomnia
weight gain
orthostatic hypotension
58
Q

How do you get drug interactions w/ MAOIs?

A

don’t take w/ tyramine-containing food or w/ sympathomimetics b/c of risk for HTN crisis.
don’t take w/ SSRIs & 5-HT receptor agonists for risk of serotonin syndrome.

59
Q

What are the features of a manic bipolar episode?

A

exaggerated optimism and self-confidence
decreased sleep without experiencing fatigue
grandiose delusions, inflated sense of self-importance
excessive irritability; aggressive behavior
racing speech, flight of ideas
impulsiveness, poor judgment
easily distracted
reckless behavior

60
Q

What is considered rapid cycling bipolar disorder?

A

more than 4 full cycles per year

61
Q

What is the first line drug for bipolar disorder?

A

Lithium-works thru long term neuroplastic changes

  • *ineffective for rapid cyclers
  • *good for mania or depression of bipolar patients
62
Q

What are the immediate effects of lithium?

A

inhibition of inositol substrates

altering G proteins associated w/ beta adrenergic & M1 Ach receptors.

63
Q

When are there peak plasma levels of lithium? How is it eliminated? WHat is its half life?

A

peak plasma: 1-2 hours
eliminated by kidney
t1/2: 20-24 hours
*renal clearance proportional to plasma concentration

64
Q

Which physiologic states are associated w/ a decrease in renal clearance?

A
dehydration
CHF
renal disease
old age
**if these happen--can have increased lithium levels
65
Q

LIthium interferes somehow with sodium reabsorption. Thus…if you have good lithium retention you could have what happen to sodium?

A

sodium depletion!

66
Q

Which drugs decrease the clearance of lithium–increase lithium levels?

A

loop & thiazide diuretics
NSAIDs
ACE inhibitors

67
Q

Which drugs increase clearance of lithium-less lithium retention?

A

osmotic diuretics
acetazolamide
caffeine
theophylline

68
Q

At therapeutic levels…what are the side effects of lithium?

A
drowsiness, forgetfullness
GI
polyuria, thirst
weight gain
mild tremor
69
Q

With long term use what are the adverse side effects of lithium?

A

degeneration of kidney & thyroid

70
Q

When should lithium not be used?

A

during first trimester of pregnancy & during breast feeding

71
Q

At the level of 2.5 mEq/L what does lithium produce?

A

ataxia
gross tremor
cardiac arrhythmias
coma and convulsions (can cause death)

72
Q

What is valproic acid/depakote used for?

A

anti epileptic drug can be used for mania & mixed states

73
Q

What is carbamazepine used for?

A

anti epileptic drug for mania & mixed states

74
Q

What are benzodiazepines used for?

A

sometimes used to help treat acute mania & agitation