Antidepressant Drugs (Segars) Flashcards by Billy Harrah

ALL Antidepressants either are known to, or can, be associated with a withdrawal syndrome that is characterized by what symptoms?

FINISH:

1) Flu-like symptoms
2) Insomnia
3) Nausea
4) Imbalance
5) Sensory disturbances
6) Hyperarousal

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The following list makes up what class of drugs?

1) Citalopram
2) Escitalopram
3) Fluoxetine
4) Paroxetine
5) Sertraline
6) Vilazodone
7) Vortioxetine

SSRI’s

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What is the MOA of SSRI’s?

Selectively inhibit the pre-synaptic reuptake of serotonin via SERT

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Which SSRI is also a partial agonist on 5-HT(1A)?

Which SSRI is also a partial agonist on 5-HT(1B), a full agonist on 5-HT(1A), and a full antagonist on 5-HT(1D,3,7)?

1) Vilazodone

2) Vortioxetine

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What is the most common adverse effect of SSRI’s?

Sexual dysfunction

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Serious effects of SSRI’s include?

1) Serotonin syndrome

2) Suicidality

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Serotonin syndrome which causes sweating, hyperreflexia, akathisia/myoclonus, and shivering/tremors has an increased risk when?

When multiple serotonin affecting agents are given together

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Which SSRI’s has the most CYP450 interactions (broad and strong inhibitor)?

Fluoxetine

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Which SSRI’s have the least CYP450 interactions?

1) Vortioxetine

2) Escitalopram

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What are the SSRI’s?

1) Citalopram
2) Escitalopram
3) Fluoxetine
4) Paroxetine
5) Sertraline
6) Vilazodone
7) Vortioxetine

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The following list makes up what class of drugs?

1) All TCA’s
2) Desvenlafaxine
3) Duloxetine
4) Venlafaxine
5) Levomilnacipran
6) Amoxapine

SNRI’s (incl. TCA’s)

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What is the MOA of SNRI’s?

Selectively Inhibit the pre-synaptic Reuptake of Serotonin (via SERT) and Norepinephrine (via NET)

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Which TCA’s inhibit both NE/5-HT relatively-equally?

Which inhibit NE more than 5-HT?

1) 3°-amine TCA’s

2) 2°-amine TCA’s

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TCA’s have a lot of side effects because they also block other receptors such as?

1) Histamine (H1)
2) Muscarinic (cholinergic)
3) α1 (adrenergic)

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TCA’s affecting alpha1 receptors causes what side effects?

TCA’s affecting muscarinic receptors causes what side effects?

TCA’s affecting histamine receptors causes what side effects?

1) Cardiovascular (tachycardia, orthostatic hypotension)
2) Anticholinergic (dry mouth, urinary retention/constipation)
3) CNS (Sedation, seizures)

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What are the three main toxicities noted with over-dose of TCAs?

1) Coma
2) Cardiotoxicity (conduction abnormalities)
3) Convulsions

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What are the SNRI’s?

1) All TCA’s
2) Desvenlafaxine
3) Duloxetine
4) Venlafaxine
5) Levomilnacipran
6) Amoxapine (SNRI + DA)

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The following list makes up what class of drugs?

1) Mirtazapine
2) Nefazodone
3) Trazadone

SARA’s

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What is the MOA of the SARA drugs Trazodone and Nefazodone?

Act like SSRI’s and also selectively block post-synaptic α1 receptors on noradrenergic (NE) neurons and post-synaptic 5-HT2 receptors

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What is the MOA of the SARA drug Mirtazapine?

Blocks pre-synaptic α2 receptors on noradrenergic (NE) and Serotonergic (5HT) neurons and also blocks post-synaptic 5-HT2/3 receptors

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Which SARA has no SERT/NET activity?

Mirtazapine

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Because the SARA drugs also block H1, what can they cause?

Sedation

What side effect is seen mostly with Trazodone / Mirtazapine?

With just Trazodone?

With just Mirtazapine?

1) Sedation
2) Orthostatic hypotension
3) Weight gain

What are the SARA drugs?

1) Mirtazapine
2) Nefazodone
3) Trazadone

Bupropion makes up what drug class?

NDRI's

What is the MOA of bupropion?

Selectively inhibits pre-synaptic Reuptake of Norepinephrine (via NET) and Dopamine (via DAT)

With Bupropion, evidence also suggests enhanced pre-synaptic release of NE and DA via?

VMAT2

What side effects are seen with Bupropion?

1) Seizures | 2) Agitation/Insomnia (Stimulating)

What drug makes up the NDRI?

Bupropion

The following list makes up what class of drugs? 1) Isocarboxazid 2) Phenelzine 3) Selegiline 4) Tranylcypromine

MAOI's

What is the MOA of MAOI's?

Inhibition of MAO increases levels of monoamines in neuronal vesicles and increases amount of NE, 5-HT, and DA released

All oral MAOI agents are considered?

Irreversible (averages 14 days for recovery)

All MAOI agents are non-selective (MAO A/B), except? It is selective for?

1) Selegiline | 2) MAO B

The anti-depressant form of selegiline is given in what form?

Patch

MAOI's have drug interactions with?

5-HT/NE affecting drugs

What should be done to avoid MAOI drug interactions? What is the exception?

1) 2 week wash-out period | 2) Fluoxetine takes 5 weeks

What risk is the major concern of MAOI's?

Hypertensive crisis (Severe headache, Sweating, Nosebleeds, Tachycardia, Confusion, Chest pain)

What does MAOI's increase the levels of which leads to the hypertensive crisis?

Tyramine (MAO-A induces its metabolism)

Which MAOI has the least amount of risk for hypertensive crisis occuring?

Selegiline (because it minimally blocks MAO-A)

What are the MAOI's?

1) Isocarboxazid 2) Phenelzine 3) Selegiline 4) Tranylcypromine

Esketamine, which is indicated for treatment-resistant depression in conjunction with ongoing antidepressant therapy is what type of antidepressant?

NMDA-receptor (glutamate) antagonist

Brexanolone, which is indicated for post-partum depression, is what type of antidepressant?

GABA(A) receptor positive allosteric modulator

What is the MOA of lithium in neurotransmitter modulation?

1) Inhibits dopamine neurotransmission 2) Downregulates NMDA receptor 3) Promotes GABAergic neurotransmission

Lithium which is a monovalent ion, competes with what ion for kidney reabsorption?

Na+

Accumulation of Li+ in principal cells of collecting duct can lead to? This results in?

1) ADH resistance | 2) Polyuria/polydipsia

Lithium therapy is the most common cause of?

Nephrogenic diabetes insipidus

Lithium has drug interactions with other agents impacting Na+/K+ such as?

1) Diuretics 2) ACEIs 3) NSAIDs

What was one of the biggest reasons why lithium therapy use decreased?

It has a narrow therapeutic window (Therapeutic concentrations = 0.6-1.2 mEq/L)

Lithium is indicated for acute and maintenance treatment of?

Mania/bipolar I disorder

Can lithium be used for unipolar depressive patients?

Yes, as an adjunctive therapy if there was inadequate response to other antidepressant therapies

What off label use does lithium have?

Reduce risk of suicide in patients with mood disorders

Valproic acid/Divalproex is a mood stabilizer (anti-seizure) agent that is indicated for acute treatment of?

Bipolar I disorder

Lamotrigine is a mood stabilizer (anti-seizure) agent that is indicated for maintenance of?

Bipolar I and II disorder

Carbamazepine is a mood stabilizer (anti-seizure) agent that is indicated acute and maintenance treatment of? What affect does carbamazepine have on CYP450?

1) Mania and mixed episodes (Bipolar I) | 2) CYP450 Inducer