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Anti-Depressant Drugs Flashcards

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
Describe how much effect tertiary and secondary TCAs have on NE and 5HT inhibition?
Tertiary amines = inhibit NE and 5-HT equally Secondary amines = NE > 5-HT
26
Name all the tertiary amines TCAs.
Amitriptyline Clomipramine Doxepin Imipramine
27
Name all the secondary amines TCAs.
Amoxapine Desipramine Nortriptyline
28
Which tertiary amines have a different effect on 5HT and NE?
Clomipramine Amitriptyline Affect 5-HT > NE
29
Only TCA-based SNRIs block other receptors. What are they?
Histamine (H1) Muscarinic (cholinergic) a1 (adrenergic) *on the postsynaptic neuron
30
Because TCAs block the receptors that they do, what side effects are seen?
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
What does toxic ingestion of TCA's cause?
Coma Convulsions Cardiotoxicity (conduction abnormalities = quinidine-like = class 1 antiarrhythmic)
32
What do class 1 antiarrhythmics do?
In ventricular cells: slows phase 0 depolarization & conduction velocity Alters QRS
33
Compare the risk of SNRI (non-TCA) SEs to SSRI SEs
SEs are similar but non-TCA SNRIs have less risk of sexual dysfunction
34
Name all the SARAs.
Trazadone Nefazodone Mirtazapine
35
What is the MAO of Trazadone and Nefazodone?
Act like SSRIs (block pre-synaptic SERT) Block POST synaptic 5HT receptors) Block POST synaptic a1 receptors on NE neurons and
36
What is the MAO of Mirtazapine?
Blocks PRE-synaptic A2 receptors on NE and 5HT neurons Block POST-synaptic 5-HT receptors
37
What are the SEs of Trazadone vs. Mirtazapine?
Both = sedation Trazadone = orthostatic HTN Mirtazapine = weight gain
38
What are NDRIs?
NE and Dopamine Reuptake Inhibitors
39
What are the only 2 drugs that affect dopamine?
Amoxapine | Bupropion (only NDRI)
40
What are the SEs of NDRIs?
Agitation/insomnia -at higher doses = HTN, tachy, tremors Weight loss SEIZURES
41
What is the mechanism of MAOIs?
MAO inhibitors | Increases levels of NE, 5HT, and DA released
42
What are the MAOIs?
Isocarboxazid Phenelzine Selegiline Tranylcypromine *orally = irreversible
43
All MAOIs are nonselective except which?
Selegiline (b-selective) *Becomes non selective at high doses
44
What are the SEs for MAOIs?
Orthostatic HTN Sexual dysfunction Weight gain Insomnia/agitation
45
What drugs do MAOIs interact with? What risks can be seen?
5HT/NE affecting drugs | Antihypertensive, amphetamines, SSRIs, TCAs, SNRIs
46
Before given an MAOI, how long must you wait after discontinuing interacting drugs?
2 week wash-out period *5 if discontinuing Fluoxetine
47
What are some major risks with MAOIs? Why do they occur?
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
Why would Selegiline help with preventing hypertensive crisis?
Will minimally block MAO-a at low doses
49
What is Esketamine? MOA?
``` Drug with no class NMDA receptor (glutamate) antagonist ```
50
When do you used Esketamine? Why does a patient need to be observed for 2 hours post-dose?
Treatment-resistant depression augmentation Issues with: Blood pressure Dissociation/cognitive impairment/sedation
51
What is Brexanolone? MOA?
``` No class drug GABAa receptor + allosteric modulator ```
52
When do you use Brexanolone? How is it given? Why does a pt need to be observed q2h during infusion?
Post-partum depression 60 hour IV by authorized physician Issues with: excessive somnolence and LOC
53
Name the mood stabilizer meds.
Anti-Sz = Carbamazepine Lamotrigine Divalproex/Valproic acid Lithium (non Anti-sz)
54
What are the multiple actions of Lithium?
Neuroprotective Neurotransmitter modulation Intracellular changes
55
What is the MOA behind Lithium's neurotransmitter modulation?
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
What are the intracellular changes associated with Li?
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
What is lithium and how is it handled?
Monovalent ion | Handled by the kidneys, similar to Na/K, Li competes with Na for kidney reabsorption
58
Since Li competes with Na for reabsorption, what effects can be see in the kidneys?
Accumulation of Li leads to: - Resistance to ADH - Polyuria/polydipsia - clinical picture of Nephrogenic DI
59
What drug interactions can occur with Lithium impacting Na/K?
Diuretics ACEIs NSAIDs
60
What range of Lithium should be given?
O.6-1.2 mEq/L ``` Lower for elderly (0.4-0.8) Refractory cases (1.5) ```
61
What are some other SEs from Lithium?
``` Tremor Confusion/dizziness/sedation Thyroid goiter (inhibits iodination) Leukocytosis (stim M-CSF) Sz and serotonin syndrome ```
62
When should Li be used?
Acute and maintenance tx of mania/bipolar I disorder Augmentation in unipolar depressive pts with inadequate response to antidepressant Tx
63
When should Valproic acid/Divalproex be used? How much?
Acute Bipolar I (with or without psychosis) 50-125 mcg/mL
64
When should Lamotrigine be used?
Maintenance of Bipolar disorder (I & II)
65
When should Carbamazepine be used? What is it a major inducer of?
Acute and maintenance Tx of acute mania and mixed episodes (Bipolar I) Major inducer of CYP450

Neuro/MSK/Psych (3 decks)

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