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Estelle Royal College > MDD Pharmacology_EO > Flashcards

MDD Pharmacology_EO Flashcards

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1
Q

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

A

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

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2
Q

Trazodone targets which receptors?

A

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

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

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3
Q

What are the side effects of Trazodone?

A

Rare priapism, sedation, orthostatic hypotension, rare arrythmias.

Note: less sexual dysfonction and less weight gain

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4
Q

What metabolizes trazodone?

A

CYP4A4

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5
Q

Which receptors are targeted by mirtazapine?

A

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

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6
Q

What happens when alpha2 receptors are blocked?

A

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

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7
Q

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

A

Risperidone, paliperidone, mirtazapine, asenapine,quetiapine and clozapine

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8
Q

What happens when 5HT2C is blocked?

A

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

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9
Q

What happens when 5HT3 is blocked?

A

Increase in DA and ACh, anti-nausea effect

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10
Q

What are the side effects of mirtazapine?

A

Weight gain, sedation, rare blood dyscrasia and rare hepatotoxicity

Note: rere sexual side-effects

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11
Q

On which receptors does quetiapine work?

A

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

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12
Q

What metabolizes quetiapine?

A

CYP 3A4

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13
Q

Which receptors are targeted by wellbutrin?

A

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

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14
Q

What are the side effects of wellbutrin

A

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

Decreases seizure threshold

Note: minimal weight gain and sexual side effects.

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15
Q

What metabolizes wellbutrin

A

Substat of CYP 2B6

Inhibits 2D6

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16
Q

On which receptores does vortioxetine (trintellix) work?

A

Inhibits SERT, 5HT3 and 5HT7

5HT1A agonist

17
Q

Which receptor causes weight gain?

A

H1

As well as sedation

18
Q

Whats the side effect of receptors targeting alpha1?

A

HTO and sedation

19
Q

Most SERT inhibition among TCA?

A

Clomipramine

Good for OCD

20
Q

TCA metabolism?

A

Tertiary amines converted in secondary amines.

Amytriptiline in nortriptyline

Imipramine in desipramine

Most TCA are metabolizedby 2D6

21
Q

2D6 inhibitors?

A

Fluoxetine and paroxetine: 4x dose

Bupropion, duloxetin and high dose sertralinr: 2x dose

22
Q

Receptors targetted by TCA?

A 
SERT
NET
5-HT2
H1
Alpha1
MAch
Na-channeld
23
Q

TCA overdose sx?

A

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

24
Q

Side effects of moclobemide

A

Insomnia, GI, irritability

Rareweight gain, uncommon sexual side effectd, activating

25
Q

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

A

5x half life of ssri

26
Q

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

A

2weeks

27
Q

What is the mechanism under tyramine hypertensice crisis?

A

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

28
Q

Tyramine hypertensive crisis sx?

A

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

29
Q

Foods that contain tyramine to avoid when taking MAOI

A

Draft beer
Old cheese
Fermented veggies and old meat
Soy

30
Q

Mechanism of serotonin syndrome

A

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

Usually within 6-8 hours of starting or increasing drug

31
Q

Sx of serotonin toxicity

A

Clonus-tremor
Hyperreflexia

Autonomic instability:
Tachypnea
Tachycardia

Agitation
Hyperthermia
Diaphorese

32
Q

Tx of serotonin syndrome

A

Cyproheptadine 12mg, then 2mg q2hrs

If cannot take PO, chlorpromazine 50-100mg IM

33
Q

Rx to avoid with IMAO?

A

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

34
Q

What are the theoritical benefits of blocking NET?

A

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

35
Q

What are the theoritical benefits of blocking SERT

A

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

Estelle Royal College (23 decks)

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