3. Segars Antidepressants and Mood Stabilizers Flashcards

1
Q

What drug is indicated for nicotine withdrawl?

A

Buproprion (zyban)

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2
Q

What drug is indicated for enuresis (involuntary urination)?

A

Imipramine - Tertiary amine TCA

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3
Q

What drug is indicated for:

  • diabetic peripheral neuropathy
  • fibromyalgia
  • stress incontinence
  • chronic MSK pain?
A

Duloxetine -SNRI

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4
Q

What are the 5 R’s of Antidepressant Efficacy?

A
  1. Response–> more than 50% reduction in sx (not well, just better)
  2. Remission –> sx free (well functioning state) less than 6 months
  3. Recovery –>not cured, 6-12 months of remisssion
  4. Relapse –> return of sx after remission but before recovery
  5. Recurrence –> return of sx after recovery
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5
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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6
Q

What are signs of an antidepressant withdrawal syndrome?

A

FINISH

  • Flu like sx
  • Insomnia
  • Nausea
  • Imbalance
  • Sensory Disturbances
  • Hyperarousal
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7
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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8
Q

Citalopram is what?

A

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

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9
Q

Escitalopram is what?

A

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

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10
Q

Fluoxetine is what?

A

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

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11
Q

Paroxetine is what?

A

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

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12
Q

Setraline is what?

A

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

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13
Q

Vilazodone is what?

A
  1. SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT
  2. partial agonist on 5-HT 1A
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14
Q

Vortioxetine is what?

A
  1. SSRI -selectivly inhibit the pre-synaptic reuptake of Serotonin via presynaptic transporter SERT
  2. Partial agonist off 5-HT1B and full agonist on 5-HT-1D
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15
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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16
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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17
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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18
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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19
Q

What SSRI has the most interactions with CYP450?

A

Fluoxetine - strong and broad CYP450 inhibitor

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20
Q

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

A

Vortioxetine and Escitalopram

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21
Q

What SSRIs are mild CYP 450 inhibitors? (3)

A
  • Citalopram
  • sertraline
  • vilazodone
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22
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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23
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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24
Q

How do secondary amine TCAs work?

Amoxapine, Desipramine, Nortriptyline

A

Inhibit NE>5HT

25
Q

Do SNRIs generally affect 5HT or NE reuptake more?

A

5HT>NE

26
Q

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

A

Amitriptyline

27
Q

What tertiary amine TCA is metabolized to Despiramine?

A

Imipramine

28
Q

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

A
  1. Histamine (H1)
  2. Muscarinic (cholinergic)
  3. alpha 1 (adrenergic)
29
Q

What are TCA side effects?

A
  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
30
Q

What can result from toxic ingestion of TCAs?

A

3 C’s:

  1. Coma
  2. Cardiotoxicity (conduction abnormalities)
  3. Convulsions
31
Q

What type of drugs are Nefazodone, and Trazodone?

A

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
32
Q

What type of drug is Mirtazapine?

A

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
33
Q

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

A
  • CNS: sedation (most with Trazodone/Mirtazapine)
  • Orthostatic HTN (most with Trazodone)
  • weight gain (most with mirtazapine)
34
Q

What are NDRIs?

A

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
35
Q

What type of drug is buproprion?

A

NDRI

36
Q
  • Agitation/Insomnia (stimulating)–> HTN/Tachycardia/tremors
  • Weightloss
  • Seizures (dose-dependent or those at risk)

are side effects of what drugs?

A

NDRI’s

37
Q

What do MAO inhibitors do?

A
  1. Increase levels of monoamines in neuronal vesicles

2. increase the amount of NE, 5-HT and DA released

38
Q

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

A

MAOI’s

39
Q

What type of MAOI’s are irreversible?

A

Oral agents

40
Q

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

A

Selegiline is B selective–> nonselective at high doses

41
Q

What MAOI is a patch?

A

Selegiline

42
Q
  • Isocarboxazid
  • Phenelzine
  • Selegiline (patch)
  • Tranylcypromine

are what types of drugs?

A

MAOIs

43
Q

MAOI’s can interact with what drugs?

A

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

44
Q

A major concern of MAOI’s is what?

A

Hypertensive Crisis

Signs:

  • severe headache
  • sweating/severe anxiety
  • nosebleeds
  • tachycardia
  • chest pain
45
Q

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

A

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
46
Q

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

A

Brexanolone

sounds like pregnenolone

47
Q

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

A

efficacy lasts up to 30 days post does

48
Q

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

A

Mood stabalizers

49
Q

What are the targets of lithium as a mood stabilizer?

A
  1. Brain Structure
  2. Neurotransmitter modulation
  3. Intracellular changes
50
Q

What neurotransmitter transmission is inhibited by lithium?

A

dopamine

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

51
Q

What receptor is down regulated by lithium?

A

NMDA receptor in chronic use

52
Q

Lithium increase the neuronstransmission of what?

A

GABA

53
Q

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

A

Lithium

-

54
Q

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

A
  • resistance to ADH
  • Polyuria/Polydipsia

**Nephrogenic Diabetes insidious is a big side effect

55
Q

What drugs interact with lithium?

A
  1. Diuretics
  2. ACEIs
  3. NSAIDs
56
Q

What are the indications of Lithium?

A
  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
57
Q

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

A

acute bipolar I (with or without psychotic features)

58
Q

What is the use of Lamotrigine as an mood stabilizer?

A

lamotrigine is used for maintenance of Bipolar I and II

59
Q

What is the use of carbamazepine as a mood stabilizer?

A

acute maintenance treatment of acute mania and mixed episodes of bipolar I

  • carbamazepine is a major CYP450 inducer