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Pharm 3 > E1: Antidepressants > Flashcards

E1: Antidepressants Flashcards

1
Q

What is the MOA of TCAs?

A
  • Inhibits re-uptake of NE and serotoninc

- blocks alpha-adrenergic, histamine, and muscarinic receptors

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2
Q

What are the uses of TCAs?

A
  • Depression
  • Chronic pain (TMJ), fibromyalgia
  • enuresis
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3
Q

What kind of drugs are amitriptyline, Imipramine, Nortriptyline, and desipramine?

A

TCAs

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4
Q

Which TCAs are tertiary amines?

A

Amitripyline and Imipramine

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5
Q

Which TCAs primarily inhibit serotonin re-uptake and which primarily block NE re-uptake?

A

Serotonin: Amitriptyline and Imipramine

NE: Nortriptyline and Desipramine

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6
Q

What are the side effects of the tertiary amine TCAs?

A
  • Produces more seizure than secondary amines

- more sedating than secondary amines

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7
Q

How are TCAs metabolized?

A
  • well absorbed orally, given once per day

- Metabolized by CYP2D6 and drug interactions are very common

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8
Q

What are the side effects of TCAs?

A
  • Weight gain
  • Histamine receptor blockade (drowsiness, fatigue, and sedation)
  • Cholinergic blockade (blurred vision, tachycardia, constipation, dry mouth)
  • Alpha1 receptor blockade (Cardiac depression and arrhythmias
  • Analgesia
  • SIADH
  • Sexual dysfunction
  • Decrease seizure threshold
  • tolerance
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9
Q

Why does analgesia happen with TCAs?

A

-Results from activation of descending noradrenerigc pathways in the spinal cord (NE acts on Alpha2 receptors to decreased glutamate input into the brain)

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10
Q

What are the toxicites associated with TCAs?

A
  • TORSADES DE POINTES
  • Prolonged QT
  • Cardiac arrhythmias
  • severe hypotension
  • seizure
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11
Q

What is the treatment of TCA overdose?

A
  • Magnesium, isoproterenol, and cardiac pacing for Torsades
  • Lidocaine, propanaolol, phenytoin for arrhythmias
  • sodium bicarb and potassium chloride to restore acid/base balance
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12
Q

What can occur if TCAs and MAOIs are combined?

A

-Serotonin syndrome: severe CNS toxicities manifested by hyperpyrexia, convulsions, and coma

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13
Q

What happens when TCA and SSRIs are combined?

A

TCAs complete for metabolism of SSRIs, so combo can lead to toxic levels of TCAs

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14
Q

What can happen when TCAs and amphetamines are combined?

A

Hypertension

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15
Q

What are the uses of SSRIs?

A
  • Depression
  • Panic disorder
  • OCD
  • Social anxiety
  • Bulimia
  • Alcoholism
  • Children and teenagers
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16
Q

What are the 5 SSRIs?

A

-Fluoxetine, Sertraline, Paroxetine, citalopram, and Escitalopram

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17
Q

What is unique about Fluoxetine when compared to the other SSRIs?

A

-Most likely to inhibit CYP450 enzymes and therefore has more drug interactions than other SSRIs

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18
Q

What is currently the DOC for depression?

A

Citalopram or escitalopram

19
Q

What is the MOA of SSRIs?

A
  • Selectively inhibits serotonin reuptake

- 2-3 weeks to be effective

20
Q

What are the common side effects of SSRIs?

A
  • Mostly mild
  • GI (nausea, loss of appetite)
  • Weight loss or gain
  • CNS stimulation
  • possible sedation
  • sexual disinterest
21
Q

What happens when SSRIs are combined with Phenytoin or Carbamazepine?

A

Increases levels and toxicity

22
Q

What are the 3 opioids that should be avoided with SSRIs?

A

-Codeine, Meriperidine, and tramadol

23
Q

What kind of drugs are Venlafaxine and Duloxentine?

A

SNRIs

24
Q

What are the uses of SNRIs?

A

Depression, neuropathic pain, and post menopausal hot flashes

25
Q

What is the main side effect of Venlafaxine?

A

May increase BP

26
Q

What are the side effects of Duloxetine?

A
  • Hepatotoxicity

- May cause bilateral acute angle closure glaucoma

27
Q

What is the MOA of MAOIs?

A

-Irreversibly inhibits MAOs which metabolize NE, NA, and serotonin

28
Q

What is the difference between MAO-A and MAO-B?

A
  • MAO-A metabolizes NE, DA, and serotoninc in both the CNS and the periphery
  • MAO-B selectively metabolizes DA in the CNS but not in the GI tract
29
Q

What kind of drugs are Phenelzine and Selegiline?

A

MAOIs

30
Q

What is the MOA of Phenelzine?

A
  • Inhibits both MAO-A and MAO-B
  • Increases NE, serotonin, and DA

** drug of last choice due to serious side effects

31
Q

What is the MOA of Selegiline?

A
  • selectively inhibits MAO-B
  • Increases DA
  • Fewer side effects
  • May be used in Parkinson’s
32
Q

What is the use of MAOIs?

A

-Used for depression which doesn’t response to other drugs

33
Q

What are the side effects of Phenelzine?

A

Hypertensive crisis: MAO-A is inhibited in the GI tract, tyramine causes release of amines, and with limited metabolism by MOA-A, can lead to severe HTN
-Avoid foods with tyramine

34
Q

What are the general side effects of MAOIs?

A
  • Orthostatic hypotension
  • weight gain
  • Anticholinergics effects
35
Q

What is the MOA of Buproprion?

A

-Inhibits DA and to a minimal extend, NE and 5HT re-uptake

36
Q

What are the uses of Buproprion?

A
  • ADHD, alcoholism

- Extended release for quitting smoking

37
Q

What are the side effects of Bupropion?

A
  • Seizures
  • CNS: anxiety, insomnia
  • tachycardia
  • sexual dysfunction side effects are RARE
38
Q

What is the MOA of Mirtazapine?

A
  • Blocks presynaptic alpha2 receptors which inhibit release of NE and serotonin
  • increases release of NE and serotonin
39
Q

If a patient has significant side effects with SSRIs, what could you consider switching them to that eliminates the side effects associated with SSRIs?

A

Mirtazapine

40
Q

What is the MOA of Atomoxetine?

A

Selective inhibitor of NE reuptake

-first non stimulant for treatment of ADHD

41
Q

What is the MOA of trazosone?

A

5-HT2A receptor antagonists

42
Q

Why is atomoxetine a good drug for addicts?

A

It does not cause euphoria

43
Q

What can happen when St Johns Wort is combined with other anti-depressants?

A

Serotonin syndrome

Pharm 3 (20 decks)

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