E1: Antidepressants

Question 1

What is the MOA of TCAs?

Answer 1

• Inhibits re-uptake of NE and serotoninc

- blocks alpha-adrenergic, histamine, and muscarinic receptors

Question 2

What are the uses of TCAs?

Answer 2

• Depression
• Chronic pain (TMJ), fibromyalgia
• enuresis

Question 3

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

Answer 3

TCAs

Question 4

Which TCAs are tertiary amines?

Answer 4

Amitripyline and Imipramine

Question 5

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

Answer 5

Serotonin: Amitriptyline and Imipramine

NE: Nortriptyline and Desipramine

Question 6

What are the side effects of the tertiary amine TCAs?

Answer 6

• Produces more seizure than secondary amines

- more sedating than secondary amines

Question 7

How are TCAs metabolized?

Answer 7

• well absorbed orally, given once per day

- Metabolized by CYP2D6 and drug interactions are very common

Question 8

What are the side effects of TCAs?

Answer 8

• 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

Question 9

Why does analgesia happen with TCAs?

Answer 9

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

Question 10

What are the toxicites associated with TCAs?

Answer 10

• TORSADES DE POINTES
• Prolonged QT
• Cardiac arrhythmias
• severe hypotension
• seizure

Question 11

What is the treatment of TCA overdose?

Answer 11

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

Question 12

What can occur if TCAs and MAOIs are combined?

Answer 12

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

Question 13

What happens when TCA and SSRIs are combined?

Answer 13

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

Question 14

What can happen when TCAs and amphetamines are combined?

Answer 14

Hypertension

Question 15

What are the uses of SSRIs?

Answer 15

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

Question 16

What are the 5 SSRIs?

Answer 16

-Fluoxetine, Sertraline, Paroxetine, citalopram, and Escitalopram

Question 17

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

Answer 17

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

Question 18

What is currently the DOC for depression?

Answer 18

Citalopram or escitalopram

Question 19

What is the MOA of SSRIs?

Answer 19

• Selectively inhibits serotonin reuptake

- 2-3 weeks to be effective

Question 20

What are the common side effects of SSRIs?

Answer 20

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

Question 21

What happens when SSRIs are combined with Phenytoin or Carbamazepine?

Answer 21

Increases levels and toxicity

Question 22

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

Answer 22

-Codeine, Meriperidine, and tramadol

Question 23

What kind of drugs are Venlafaxine and Duloxentine?

Answer 23

SNRIs

Question 24

What are the uses of SNRIs?

Answer 24

Depression, neuropathic pain, and post menopausal hot flashes

Question 25

What is the main side effect of Venlafaxine?

Answer 25

May increase BP

Question 26

What are the side effects of Duloxetine?

Answer 26

- Hepatotoxicity | - May cause bilateral acute angle closure glaucoma

Question 27

What is the MOA of MAOIs?

Answer 27

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

Question 28

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

Answer 28

- 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

Question 29

What kind of drugs are Phenelzine and Selegiline?

Answer 29

MAOIs

Question 30

What is the MOA of Phenelzine?

Answer 30

- Inhibits both MAO-A and MAO-B - Increases NE, serotonin, and DA ** drug of last choice due to serious side effects

Question 31

What is the MOA of Selegiline?

Answer 31

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

Question 32

What is the use of MAOIs?

Answer 32

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

Question 33

What are the side effects of Phenelzine?

Answer 33

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

Question 34

What are the general side effects of MAOIs?

Answer 34

- Orthostatic hypotension - weight gain - Anticholinergics effects

Question 35

What is the MOA of Buproprion?

Answer 35

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

Question 36

What are the uses of Buproprion?

Answer 36

- ADHD, alcoholism | - Extended release for quitting smoking

Question 37

What are the side effects of Bupropion?

Answer 37

- Seizures - CNS: anxiety, insomnia - tachycardia - sexual dysfunction side effects are RARE

Question 38

What is the MOA of Mirtazapine?

Answer 38

- Blocks presynaptic alpha2 receptors which inhibit release of NE and serotonin - increases release of NE and serotonin

Question 39

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

Answer 39

Mirtazapine

Question 40

What is the MOA of Atomoxetine?

Answer 40

Selective inhibitor of NE reuptake | -first non stimulant for treatment of ADHD

Question 41

What is the MOA of trazosone?

Answer 41

5-HT2A receptor antagonists

Question 42

Why is atomoxetine a good drug for addicts?

Answer 42

It does not cause euphoria

Question 43

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

Answer 43

Serotonin syndrome