MDD Pharmacology_EO

Question 1

Side effects of 5-HT (2&3) activation?

Answer 1

especially initial activation for insomnia (5HT2A) and anorexia (5HT2C). Sexual dysfunction and anxiety 5HT2.

5HT3: nausea & Diarrhea

EPS - stiffness if 5HT2 decreases dopaminergic firing in the nigrostriatal pathway

Question 2

Trazodone targets which receptors?

Answer 2

At low-dose (25-150mg): alpha1 and 5HT2A-antagonism

At higher dose: SERT antagonism, 5-HT2C- antagonism, alpha1 and 5HT2A-antagonism

Question 3

What are the side effects of Trazodone?

Answer 3

Rare priapism, sedation, orthostatic hypotension, rare arrythmias.

Note: less sexual dysfonction and less weight gain

Question 4

What metabolizes trazodone?

Answer 4

CYP4A4

Question 5

Which receptors are targeted by mirtazapine?

Answer 5

alpha2 antagonist, H1 antagonist
5-HT3 antagonist
5-HT2A antagonist
5-HT2C antagonist

Question 6

What happens when alpha2 receptors are blocked?

Answer 6

It increases the release of serotonine and NE.

By blocking presynaptic alpha2 receptors, the feedback inhibition exerted on the release of NE is removed. Thus, the net effect is to increase NE secretion

Question 7

Which psychotropics have the property of bloking alpha2? (6)

Answer 7

Risperidone, paliperidone, mirtazapine, asenapine,quetiapine and clozapine

Question 8

What happens when 5HT2C is blocked?

Answer 8

Increased NE and DA in PFC which may improve motivation and concentration

Question 9

What happens when 5HT3 is blocked?

Answer 9

Increase in DA and ACh, anti-nausea effect

Question 10

What are the side effects of mirtazapine?

Answer 10

Weight gain, sedation, rare blood dyscrasia and rare hepatotoxicity

Note: rere sexual side-effects

Question 11

On which receptors does quetiapine work?

Answer 11

Low dose: H1, alpha1
Depression dose: H1, alspha1, alpha2, norepinephrine-reuptake-inhibitor, 5HT2A, 5HT2C
More than 300mg: D2, 5HT1A agonist, M1, H1, alpha1, alpha2, norepinephrine-reuptake-inhibitor, 5HT2A, 5HT2C

Question 12

What metabolizes quetiapine?

Answer 12

CYP 3A4

Question 13

Which receptors are targeted by wellbutrin?

Answer 13

Mechanism of action not well understood. Increases DA, NE and increases firing of 5HT neurons.
Antagonist of nicotinic cholinergic receptor

Question 14

What are the side effects of wellbutrin

Answer 14

Dry mouth, nausea, headache, insomnia, constipation, irritability

Decreases seizure threshold

Note: minimal weight gain and sexual side effects.

Question 15

What metabolizes wellbutrin

Answer 15

Substat of CYP 2B6

Inhibits 2D6

Question 16

On which receptores does vortioxetine (trintellix) work?

Answer 16

Inhibits SERT, 5HT3 and 5HT7

5HT1A agonist

Question 17

Which receptor causes weight gain?

Answer 17

H1

As well as sedation

Question 18

Whats the side effect of receptors targeting alpha1?

Answer 18

HTO and sedation

Question 19

Most SERT inhibition among TCA?

Answer 19

Clomipramine

Good for OCD

Question 20

TCA metabolism?

Answer 20

Tertiary amines converted in secondary amines.

Amytriptiline in nortriptyline

Imipramine in desipramine

Most TCA are metabolizedby 2D6

Question 21

2D6 inhibitors?

Answer 21

Fluoxetine and paroxetine: 4x dose

Bupropion, duloxetin and high dose sertralinr: 2x dose

Question 22

Receptors targetted by TCA?

Answer 22

SERT
NET
5-HT2
H1
Alpha1
MAch
Na-channeld

Question 23

TCA overdose sx?

Answer 23

Cardiotoxic (ventricular arrhythmias, wideQRS, QTc prolongation, 1 degree AV block) and seizure from blockage of Na channels

Question 24

Side effects of moclobemide

Answer 24

Insomnia, GI, irritability

Rareweight gain, uncommon sexual side effectd, activating

Question 25

Switching from SSRI to MAOI, how long the pause in between?

Answer 25

5x half life of ssri

Question 26

Switching MAOI to SSRI, hoe long the pause in between?

Answer 26

2weeks

Question 27

What is the mechanism under tyramine hypertensice crisis?

Answer 27

Tyramine increases NE. Irréversible MAOI strops destruction of NE. Increase in NE leads to elevation of BP

Question 28

Tyramine hypertensive crisis sx?

Answer 28

Diastolic superior 120; occipital headache, palpitations, neck stiffness, No, Vo, mydriase, sweat

Do not treat (nifedipine) without evidence of tyramine ingestion or end organ damage

Question 29

Foods that contain tyramine to avoid when taking MAOI

Answer 29

Draft beer
Old cheese
Fermented veggies and old meat
Soy

Question 30

Mechanism of serotonin syndrome

Answer 30

5-HT post synaptic receptors over stimulated by SERT blocked and MAO stopped

Usually within 6-8 hours of starting or increasing drug

Question 31

Sx of serotonin toxicity

Answer 31

Clonus-tremor
Hyperreflexia

Autonomic instability:
Tachypnea
Tachycardia

Agitation
Hyperthermia
Diaphorese

Question 32

Tx of serotonin syndrome

Answer 32

Cyproheptadine 12mg, then 2mg q2hrs

If cannot take PO, chlorpromazine 50-100mg IM

Question 33

Rx to avoid with IMAO?

Answer 33

Ssri, snri, vilazodone, clomipramine, tramadol, methadone, fentanyl, ziprasidonr, dextromethorphan, Rx that can cause HTN

Question 34

What are the theoritical benefits of blocking NET?

Answer 34

Beneficial for symptoms of loss of interest, loss of energy and psychomotor retardation

Question 35

What are the theoritical benefits of blocking SERT

Answer 35

Most beneficial for negative affect sx such as guilt, irritability, dysphoria, SI and obsessions