3. Segars Antidepressants and Mood Stabilizers Flashcards by Sarah Mahonski

Q

What drug is indicated for nicotine withdrawl?

A

Buproprion (zyban)

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Q

What drug is indicated for enuresis (involuntary urination)?

A

Imipramine - Tertiary amine TCA

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Q

What drug is indicated for:

diabetic peripheral neuropathy
fibromyalgia
stress incontinence
chronic MSK pain?

A

Duloxetine -SNRI

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Q

What are the 5 R’s of Antidepressant Efficacy?

A

Response–> more than 50% reduction in sx (not well, just better)
Remission –> sx free (well functioning state) less than 6 months
Recovery –>not cured, 6-12 months of remisssion
Relapse –> return of sx after remission but before recovery
Recurrence –> return of sx after recovery

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Q

What do you do if a patient doesn’t respond fro an antidepressant after ~ 8 week trial?

A

Switch to another antidepressant with a different MOA

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Q

What are signs of an antidepressant withdrawal syndrome?

A

FINISH

Flu like sx
Insomnia
Nausea
Imbalance
Sensory Disturbances
Hyperarousal

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Q

Citalopram
Escitalopram
Fluoxetine
Paroxeitine 
Sertraline
Vilazodone
Vortioxetine

are what type of drugs?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT

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Q

Citalopram is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT

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Q

Escitalopram is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT

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Q

Fluoxetine is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT

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Q

Paroxetine is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT

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Q

Setraline is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT

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Q

Vilazodone is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT
partial agonist on 5-HT 1A

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Q

Vortioxetine is what?

A

SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT
Partial agonist off 5-HT1B and full agonist on 5-HT-1D

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Q

Do SSRIs or TCAs have more side effects?

A

TCA- SSRIs have less impact on histamine, muscarinic, and adrenergic receptors

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Q

CNS (sedation or insomnia/agitation/nervousness)
Sexual dysfunction (change in libido/impotence)
Weight gain (adults) / Weight loss (mild; adolescents)
Acute withdrawal reactions (concern w/ all categories)

Are primary side effects of what drug class?

A

SSRI

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Q

What is serotonin syndrome? What can cause it?

A

Sx: sweating, hyperreflexia, Akathisia/myoclonus, shivering/tremors
Serious dose dependent side effect of SSRI

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Q

What are rare dose dependent toxicities of SSRI?

A

QT prolongation
Hyponatremia (SIADH)
Serotonin syndrome
suicidality ( high risk in children, adolescents, and young adults

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Q

What SSRI has the most interactions with CYP450?

A

Fluoxetine - strong and broad CYP450 inhibitor

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Q

Which SSRI has the least amount of Reactions with CYP450? (2)

A

Vortioxetine and Escitalopram

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Q

What SSRIs are mild CYP 450 inhibitors? (3)

A

Citalopram
sertraline
vilazodone

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Q

What are SNRIs (including TCA)?

A

Selectivly inhibit the pre-synaptic reuptake of serotonin via SERT and Norepinephrine via NET

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Q

How do tertiary amines TCAs clomipramine, amitriptyline, Doxepin, and Imipramine TCAs work?

A

inhibit both NE/5-HT relatively equally

(Clomiprmaine/ Amitriptyline impact 5HT more)

more anticholinergic effects than secondary TCAs

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Q

How do secondary amine TCAs work?

Amoxapine, Desipramine, Nortriptyline

Study These Flashcards

A

Inhibit NE>5HT

Do SNRIs generally affect 5HT or NE reuptake more?

5HT>NE

What is tertiary TCA Amine is metabolized to secondary amine TCA Nortriptyline?

Amitriptyline

What tertiary amine TCA is metabolized to Despiramine?

Imipramine

What receptors do TCAs impact in addition to NET and SERT?

1. Histamine (H1) 2. Muscarinic (cholinergic) 3. alpha 1 (adrenergic)

What are TCA side effects?

1. Cardiovascular (a1)--> tachycardia, orthostatic hypotension, dysrhytmias 2. Anticholinergic (muscarinic)--> Dry mouth, Urinary retention/Constipation, Blurred vision/ increased intraoccular pressure 3. CNS (histamine) -- >Sedation/fatigue, dizziness/seizures

What can result from toxic ingestion of TCAs?

3 C's: 1. Coma 2. Cardiotoxicity (conduction abnormalities) 3. Convulsions

What type of drugs are Nefazodone, and Trazodone?

SARA - two agents that that act like SSRIs - selectively block at post synaptic a1 receptors on norAdrenergic neurons - block post synaptic 5-HT2 receptors - Also bloc H1 and cause sedation

What type of drug is Mirtazapine?

SARA - blocks presynaptic a2 receptors on norAdrenergic and Serotonergic 5HT neurons - blocks post synaptic 5-HT(2/3) receptors - Blocks H1 - No SERT/NET activity

What are the SARA side effects (H1/a1)?

- CNS: sedation (most with Trazodone/Mirtazapine) - Orthostatic HTN (most with Trazodone) - weight gain (most with mirtazapine)

What are NDRIs?

antidepressants that selectively inhibit presynaptic Reuptake of NE (via NET) and Dopamine (via DAT) - enhanced, prolonged NE and DA neurotransmission to post-synaptic receptors - enhances presynaptic release of NE and DA via VMAT2

What type of drug is buproprion?

NDRI

- Agitation/Insomnia (stimulating)--> HTN/Tachycardia/tremors - Weightloss - Seizures (dose-dependent or those at risk) are side effects of what drugs?

NDRI's

What do MAO inhibitors do?

1. Increase levels of monoamines in neuronal vesicles | 2. increase the amount of NE, 5-HT and DA released

Isocarboazid, Phenelzine, Selegiline, and Tranylcypromine are what type of drugs?

MAOI's

What type of MAOI's are irreversible?

Oral agents

All MAOIs are nonselective against MAO A/B except what?

Selegiline is B selective--> nonselective at high doses

What MAOI is a patch?

Selegiline

- Isocarboxazid - Phenelzine - Selegiline (patch) - Tranylcypromine are what types of drugs?

MAOIs

MAOI's can interact with what drugs?

5-HT/NE affecting drugs -there is a 2 week wash out period for fluoxetine, can take 5 weeks for it to leave the system making interactions possible

A major concern of MAOI's is what?

Hypertensive Crisis Signs: - severe headache - sweating/severe anxiety - nosebleeds - tachycardia - chest pain

What miscellaneous antidepressant is an NMDA receptor (glutamate) antagonist) that is indicated for treatment-resistant depression in conjunction with ongoing antidepressant therapy?

Esketamine- S isomer of ketamine - nasal administration by an REMs authorized physician and must be monitored 2 hrs post dose for blood person, and cognitive impairtment

What miscellaneous antidepressant is a GABA (A) receptor positive allosteric modulator that is identical to endogenous alloprenanolone and used to treat post partum depression?

Brexanolone | sounds like pregnenolone

How long does GABA(A) receptor positive allosteric modulatorBrexanolone last?

efficacy lasts up to 30 days post does

Anti-seizure agents carbamazepine, Lamotrigine, and valproic acid; and lithium are used to treat what aspect of mood disorders?

Mood stabalizers

What are the targets of lithium as a mood stabilizer?

1. Brain Structure 2. Neurotransmitter modulation 3. Intracellular changes

What neurotransmitter transmission is inhibited by lithium?

dopamine | -Li+ interferes with Gs anGi activity keeping them in the inactive state

What receptor is down regulated by lithium?

NMDA receptor in chronic use

Lithium increase the neuronstransmission of what?

GABA

What drug is a monovalent ion that compete with Na+ for kidney reabsorption?

Lithium -

Accumulation of Lithium in the principle cells of the collecting duct can lead to what?

- resistance to ADH - Polyuria/Polydipsia **Nephrogenic Diabetes insidious is a big side effect

What drugs interact with lithium?

1. Diuretics 2. ACEIs 3. NSAIDs

What are the indications of Lithium?

1. acute maintenance and treatment of mania/ bipolar I disorder 2. Augmentation for patients in unipolar depressive patients with inadequate response to antidepressant therapy 3. Off label reduces risk of suicide and mortality in patients with mood disorders

What is the use of Valproic acid/Divalproex as a mood stabilizer?

acute bipolar I (with or without psychotic features)

What is the use of Lamotrigine as an mood stabilizer?

lamotrigine is used for maintenance of Bipolar I and II

What is the use of carbamazepine as a mood stabilizer?

acute maintenance treatment of acute mania and mixed episodes of bipolar I - carbamazepine is a major CYP450 inducer