Anti-Depressant Drugs Flashcards

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1
Q

Describe RESPONSE.

A

> 50% reduction in Sx

Majority take up to 3-4 weeks (can be 3-8+ weeks)

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2
Q

Describe PARTIAL RESPONSE.

A

> 25% reduction but <50% reduction in Sx

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3
Q

Describe REMISSION.

A

Sx-free
Healthy state

Minority reach remission on single agent

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4
Q

Describe RECOVERY.

A

2-6 months of ongoing remission

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5
Q

Describe RELAPSE.

A

Return of Sx AFTER remission but BEFORE recovery

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6
Q

Describe RECURRENCE.

A

Return of Sx AFTER recovery

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7
Q

What is the goal of using Anti-depressants?

A

REMISSION/Recovery

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8
Q

When do you use mono-therapy with anti-depressants?

A

Only for unipolar depression, not depressive phase of bipolar disorder

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9
Q

What Syndrome are all antidepressants associated with? How can you manage it?

A

Withdrawal Syndrome

Management = Slow titration downward

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10
Q

What Sx are associated with Withdrawal syndrome?

A

FINISH

Flu-like Sx
Insomnia 
Nausea 
Imbalance 
Sensory disturbances 
Hyperarousal (lower risk with long acting agents)
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11
Q

What antidepressant is associated with nicotine withdrawal?

A

Bupropion

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12
Q

What antidepressant is associated with enuresis?

A

Imipramine

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13
Q

What conditions does the antidepressant, DULOXETINE, treat?

A

Diabetic peripheral neuropathy
Fibromyalgia
Chronic musculoskeletal pain
Stress incontinence

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14
Q

What are SSRIs? What is the MOA?

A

Selective Serotonin Reuptake Inhibitors

Prevents presynaptic uptake of 5HT via inhibition of SERT
-results in prolonged 5HT neurotrasmission

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15
Q

What are the drugs in the SSRI category?

A

-PRAMs = Citalopram and Escitalopram

Fluoxetine 
Paroxitine 
Sertraline 
Vilazodone 
Vortioxetine
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16
Q

What are the side effects for SSRIs?

A

CNS = sedation or insomnia/agitation/nervousness

Sexual dysfunction

Weight gain in adults, weight loss in adolescents/mild

Rare = (dose-dependent)
QT prolongation
Hyponatremia (SIADH like)

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17
Q

What are the most serious side effects seen with SSRIs?

A

Serotonin syndrome

Suicidality with highest risk in children/YA

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18
Q

What Sx are seen with serotonin syndrome?

A

Sweating
Hyperreflexia (classic)
Akathisia/myclonus
Shivering/Tremors

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19
Q

What characteristics are specific to Vilazodone and Vortioxetine?

A

Vila = partial agonist on 5HT1A

Vortio = partial agonist on 5HT1B and full agonist on 5HT1A(1D,3,7)

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20
Q

Which class has fewer side effects - TCAs or SSRIs?

A

SSRIs

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21
Q

Which SSRI has the most drug-drug interactions?

A

Fluoxetine (broad and strong inhibitor)

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22
Q

Which SSRI has the Least drug-drug interactions?

A

Vortioxetine and escitalopram

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23
Q

What are SNRIs? What class do they include?

A

Serotonin and Norepinephrine Reuptake Inhibition

Include TCAs

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24
Q

Name all the SNRIs.

A

Desvenlafaxine
Duloxetine
Venlafaxine
Levomilnacipran

TCAs!

Amoxipine (SNRI+DA)

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25
Q

Describe how much effect tertiary and secondary TCAs have on NE and 5HT inhibition?

A

Tertiary amines = inhibit NE and 5-HT equally

Secondary amines = NE > 5-HT

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26
Q

Name all the tertiary amines TCAs.

A

Amitriptyline
Clomipramine

Doxepin
Imipramine

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27
Q

Name all the secondary amines TCAs.

A

Amoxapine
Desipramine
Nortriptyline

28
Q

Which tertiary amines have a different effect on 5HT and NE?

A

Clomipramine
Amitriptyline

Affect 5-HT > NE

29
Q

Only TCA-based SNRIs block other receptors. What are they?

A

Histamine (H1)
Muscarinic (cholinergic)
a1 (adrenergic)

*on the postsynaptic neuron

30
Q

Because TCAs block the receptors that they do, what side effects are seen?

A

adrenergic (if blocked) = tachycardia, orthostatic HTN, dysrhythmias

anticholinergic (b/c muscarinic blocked) = dry mouth, urinary retention/ constipation, blurred vision

antihistamine (CNS probs) = sedation/ fatigue, dizziness/sz

31
Q

What does toxic ingestion of TCA’s cause?

A

Coma

Convulsions

Cardiotoxicity (conduction abnormalities = quinidine-like = class 1 antiarrhythmic)

32
Q

What do class 1 antiarrhythmics do?

A

In ventricular cells:
slows phase 0 depolarization & conduction velocity
Alters QRS

33
Q

Compare the risk of SNRI (non-TCA) SEs to SSRI SEs

A

SEs are similar but non-TCA SNRIs have less risk of sexual dysfunction

34
Q

Name all the SARAs.

A

Trazadone
Nefazodone

Mirtazapine

35
Q

What is the MAO of Trazadone and Nefazodone?

A

Act like SSRIs (block pre-synaptic SERT)

Block POST synaptic 5HT receptors)

Block POST synaptic a1 receptors on NE neurons and

36
Q

What is the MAO of Mirtazapine?

A

Blocks PRE-synaptic A2 receptors on NE and 5HT neurons

Block POST-synaptic 5-HT receptors

37
Q

What are the SEs of Trazadone vs. Mirtazapine?

A

Both = sedation

Trazadone = orthostatic HTN

Mirtazapine = weight gain

38
Q

What are NDRIs?

A

NE and Dopamine Reuptake Inhibitors

39
Q

What are the only 2 drugs that affect dopamine?

A

Amoxapine

Bupropion (only NDRI)

40
Q

What are the SEs of NDRIs?

A

Agitation/insomnia
-at higher doses = HTN, tachy, tremors

Weight loss

SEIZURES

41
Q

What is the mechanism of MAOIs?

A

MAO inhibitors

Increases levels of NE, 5HT, and DA released

42
Q

What are the MAOIs?

A

Isocarboxazid
Phenelzine
Selegiline
Tranylcypromine

*orally = irreversible

43
Q

All MAOIs are nonselective except which?

A

Selegiline (b-selective)

*Becomes non selective at high doses

44
Q

What are the SEs for MAOIs?

A

Orthostatic HTN
Sexual dysfunction
Weight gain
Insomnia/agitation

45
Q

What drugs do MAOIs interact with? What risks can be seen?

A

5HT/NE affecting drugs

Antihypertensive, amphetamines, SSRIs, TCAs, SNRIs

46
Q

Before given an MAOI, how long must you wait after discontinuing interacting drugs?

A

2 week wash-out period

*5 if discontinuing Fluoxetine

47
Q

What are some major risks with MAOIs? Why do they occur?

A

Serotonin syndrome
Hypertensive crisis

SS - cause messing with serotonin

HC - b/c will inhibit MAO-A necessary in GI for tyramine metabolism, which increases tyramine levels leading to increased catecholamines

48
Q

Why would Selegiline help with preventing hypertensive crisis?

A

Will minimally block MAO-a at low doses

49
Q

What is Esketamine? MOA?

A
Drug with no class 
NMDA receptor (glutamate) antagonist
50
Q

When do you used Esketamine? Why does a patient need to be observed for 2 hours post-dose?

A

Treatment-resistant depression augmentation

Issues with:
Blood pressure
Dissociation/cognitive impairment/sedation

51
Q

What is Brexanolone? MOA?

A
No class drug
GABAa receptor + allosteric modulator
52
Q

When do you use Brexanolone? How is it given? Why does a pt need to be observed q2h during infusion?

A

Post-partum depression
60 hour IV by authorized physician

Issues with:
excessive somnolence and LOC

53
Q

Name the mood stabilizer meds.

A

Anti-Sz =
Carbamazepine
Lamotrigine
Divalproex/Valproic acid

Lithium (non Anti-sz)

54
Q

What are the multiple actions of Lithium?

A

Neuroprotective
Neurotransmitter modulation
Intracellular changes

55
Q

What is the MOA behind Lithium’s neurotransmitter modulation?

A

Inhibits dopamine transmission

  • thought is increased DA NT means decreased neurotransmission assoc with depression
  • Li interferes with Gs and Gi proteins keeping them inactive

Downregulates NMDA receptor

Promotes GABAergic neurotransmission
-increases GABA in CSF

56
Q

What are the intracellular changes associated with Li?

A

Inhibits IPPase and IMPase
-these make myoinositol (which will be depleted)

Inhibits PKC, MARCKS, GSK-3

Facilitates production on neuroprotective factors

  • CREB (+, tf)
  • CREB makes BDNF and Bcl-2
57
Q

What is lithium and how is it handled?

A

Monovalent ion

Handled by the kidneys, similar to Na/K, Li competes with Na for kidney reabsorption

58
Q

Since Li competes with Na for reabsorption, what effects can be see in the kidneys?

A

Accumulation of Li leads to:

  • Resistance to ADH
  • Polyuria/polydipsia - clinical picture of Nephrogenic DI
59
Q

What drug interactions can occur with Lithium impacting Na/K?

A

Diuretics
ACEIs
NSAIDs

60
Q

What range of Lithium should be given?

A

O.6-1.2 mEq/L

Lower for elderly (0.4-0.8) 
Refractory cases (1.5)
61
Q

What are some other SEs from Lithium?

A
Tremor 
Confusion/dizziness/sedation 
Thyroid goiter (inhibits iodination)
Leukocytosis (stim M-CSF) 
Sz and serotonin syndrome
62
Q

When should Li be used?

A

Acute and maintenance tx of mania/bipolar I disorder

Augmentation in unipolar depressive pts with inadequate response to antidepressant Tx

63
Q

When should Valproic acid/Divalproex be used? How much?

A

Acute Bipolar I (with or without psychosis)

50-125 mcg/mL

64
Q

When should Lamotrigine be used?

A

Maintenance of Bipolar disorder (I & II)

65
Q

When should Carbamazepine be used? What is it a major inducer of?

A

Acute and maintenance Tx of acute mania and mixed episodes (Bipolar I)

Major inducer of CYP450