Antidepressants B&B Flashcards

1
Q

what are the side effects of TCAs?

A
  1. anti-histamine: sedation, weight gain, confusion (elderly)
  2. anti-muscarinic: blurry vision, constipation, dry mouth, urinary retention
  3. alpha-1 block: orthostatic hypotension
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2
Q

contrast the 2 groups of TCAs

A
  1. tertiary amines (3 N groups): more sedating (anti-histamine); ex - amitriptyline, clomipramine, doxepin, imipramine, trimipramine
  2. secondary amines (2 N groups): more activity (NE effects); ex - desipramine, nortriptyline, protriptyline
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3
Q

which of the following TCAs would be most appropriate for a patient with depression who is experiencing excessive drowsiness? why?
a. amitriptyline
b. desipramine
c. doxepin
d. imipramine

A

b. desipramine - secondary amine, which have NE effects (activating)

tertiary amines (all other choices) are sedative due to anti-histamine effects (better for patients having trouble sleeping)

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4
Q

what serious effects (3) can occur if a patient overdoses on TCAs?

A
  1. seizures - antagonize GABA
  2. hyperthermia (due to loss of sweating) - anti-cholinergic
  3. hypotension/ prolonged QT interval (arrhythmias) - alpha1 blockage
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5
Q

how should patients with TCA overdose be monitored? what is the treatment for TCA overdose?

A

monitor ECG for increased QRS interval - TCAs block cardiac alpha1 receptors

tx with sodium bicarbonate - extra Na+ overcomes Na+ channel blockage + increased pH favors inactive drug form

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6
Q

for what non-depression uses are TCAs prescribed? 6

A
  1. OCD (clomipramine)
  2. diabetic peripheral neuropathy (amitriptyline, desipramine)
  3. chronic pain
  4. migraine prophylaxis (amitriptyline)
  5. bed wetting (enuresis) - 2nd line after desmopressin
  6. insomnia (doxepin)
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7
Q

which TCA is used to treat OCD?

A

clomipramine

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8
Q

which 2 TCAs are used to treat diabetic peripheral neuropathy?

A
  1. amitriptyline
  2. desipramine
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9
Q

which TCA is used for migraine prophylaxis?

A

amitriptyline

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10
Q

which TCA is used to treat insomnia?

A

doxepin

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11
Q

MAO-A vs MAO-b inhibitors

give examples of each

A

MAO-A inhibitors are non-selective - prevent breakdown of dopamine, serotonin, NE (tranylcypromine, phenelzine, isocarboxazid) - treats refractory depression/ anxiety

MAO-B inhibitors only prevent breakdown of dopamine (selegiline) - treats Parkinson’s

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12
Q

name an example of each of the following that can induce serotonin syndrome:
a. illicit substance
b. anti-nausea med
c. migraine treatment
d. antibiotic
e. cough suppressant
f. herbal supplement

A

a. illicit substance - MDMA (ecstasy)

b. anti-nausea med - ondanestron (5-HT3 antagonist)

c. migraine treatment - triptans (5-HT agonists)

d. antibiotic - linezolid (weak MAO inhibitor)

e. cough suppressant - dextromethorphan (weak SSRI)

f. herbal supplement - St. John’s wart (increases 5-HT activity)

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13
Q

name 7 conditions for which SSRIs are prescribed

A
  1. depression
  2. generalized anxiety
  3. panic disorder
  4. OCD
  5. bulimia
  6. social anxiety
  7. PTSD
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14
Q

what is the main side effect of SSRIs?

A

sexual dysfunction - decreased libido, anorgasmia, ED

due to increased serotonin in spinal cord

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15
Q

name an SNRI used to treat fibromyalgia

A

duloxetine

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16
Q

name an SNRI used to treat diabetic neuropathy

A

venlafaxine

17
Q

what is the MOA and clinical use of bupropion?

A

blocks reuptake of NE and dopamine (NET/DAT) + increases presynaptic release of catecholamines (NO serotonin effects)

tx depression + smoking cessation, may improve sexual dysfunction of SSRIs (used in combo to cancel out effects)

18
Q

drug used in smoking cessation which blocks reuptake of NE and dopamine

A

bupropion: blocks reuptake of NE and dopamine (NET/DAT) + increases presynaptic release of catecholamines (NO serotonin effects)

tx depression + smoking cessation, may improve sexual dysfunction of SSRIs (used in combo to cancel out effects)

19
Q

what is the MOA (2) and clinical use of mirtazapine?

A

antidepressant which:
1. blocks presynaptic alpha-2 receptors (decrease in neg. feedback for NE release)
2. blocks postsynaptic 5-HT2 + 5-HT3 receptors

—> increase in NE and serotonin release + increase in 5-HT1 receptor activity (bc the other 2 are blocked)

20
Q

what side effects are associated with mirtazapine?

A

antidepressant, blocks presynaptic alpha-2 receptors (decrease in neg. feedback of NE release) + blocks postsynaptic 5-HT2 + 5-HT3 receptors (increased 5-HT1 R activity)

also anti-histamine - causes sedation, dry mouth, increased appetite, weight gain

21
Q

Pt presents with complaint of fatigue, dry mouth, and recent weight gain, which are attributed to side effects of their antidepressant. Their antidepressant works by blocking presynaptic alpha-2 receptors and postsynaptic 5-HT2/3 receptors. What drug are they taking?

A

mirtazapine:

  1. blocks presynaptic alpha-2 receptors (decrease in neg. feedback for NE release)
  2. blocks postsynaptic 5-HT2 + 5-HT3 receptors (increases 5-HT1 receptor activity bc the other 2 are blocked)

also anti-histamine - causes sedation, dry mouth, increased appetite, weight gain

22
Q

name 3 serotonin modulators which have minimal effect on NE or dopamine

A
  1. trazadone - tx insomnia
  2. vilazodone
  3. vortioxetine
23
Q

what is the MOA and clinical use of trazadone?

A

weak serotonin reuptake inhibitor (5-HT2A and 5-HT2C)

5-HT antagonist at low doses, agonist at high doses

treats insomnia (sedating)

24
Q

serotonin modulator that treats insomnia

A

trazadone: weak serotonin reuptake inhibitor (5-HT2A and 5-HT2C)

antagonist at low doses; agonist at high doses

25
Q

what is the MOA of vilazodone?

A

serotonin modulator - blocks reuptake + partial agonist at 5-HT1A

side effects - diarrhea, sexual dysfunction, serotonin syndrome

26
Q

what kind of drug is vortioxetine?

A

serotonin modulator (minimal effect on NE/dopamine) - blocks reuptake through various mechanisms (depending on receptor type)

can be antagonist (5-HT3), partial agonist (5-HT1B), full agonist (5-HT1A)

27
Q

name 5 SSRIs

A
  1. citalopram
  2. escitalopram
  3. fluoxetine
  4. paroxetine
  5. sertraline

ESCape the PAROtt FLU in SERT [SSRI’s block SERT!] CITy

28
Q

which antidepressant is particularly useful for patients with major depression with insomnia or marked weight loss?

A

mirtazepine: blocks presynaptic alpha-2 receptors (decrease in neg. feedback of NE release) + blocks postsynaptic 5-HT2 + 5-HT3 receptors (increased 5-HT1 R activity)

also anti-histamine - causes sedation, dry mouth, increased appetite, weight gain

29
Q

name 5 TCAs

A
  1. imipramine
  2. amitriptyline
  3. clomipramine
  4. desipramine
  5. nortriptyline

basically, “-triptyline” and “-pramine” !!

30
Q

phenelzine vs tranylcypromine

A

both are MOA-A inhibitors

phenelzine = irreversible
tranylcypromine = reversible

31
Q

what are the adverse effects of phenelzine and tranylcypromine?

A

MAO-A (non-selective) inhibitors, treat atypical depression

AE: tyramine cheese effect (sympathomimetic, hyperthermia) + serotonin syndrome (w/ SSRIs/SNRIs)

32
Q

what is the MOA and clinical use of esketamine?

A

potent NMDA receptor antagonist

treats resistant depression, administered intranasally under supervision of healthcare professional (risk of sedation and dissociation requires monitoring)

33
Q

potent NMDA receptor antagonist that treats resistant depression and is administered intranasally under supervision

A

esketamine - only available through restricted distribution system (REMS) due to risk of sedation and dissociation (requires monitoring)