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Medical Pharmacology Exam 3 > Serotonin > Flashcards

Serotonin Flashcards

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USMLE® Step 1 flashcards
1
Q

What are 3 areas where serotonin is stored?

A

Platelets
Neurons
Enterochromaffin cells (GI)

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2
Q

What are 4 stimuli that can cause release of serotonin from enterochromaffin cells?

A

Mechanical stim
NOR
Hypertonicity
Vagal stimulation

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3
Q

What are 2 events that cause serotonin release from platelets?

A

Aggregation

Degranulation

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4
Q

How does a carcinoid tumor affect serotonin release?

A

It enhances 5HT release

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5
Q

All but one of the 5HT receptors (1-7) are GPCRs. What is the exception? What is the function of this exception?

A

5HT3

Activation - Neuronal activation / NT release

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6
Q

What is the direct effect of serotonin on vascular smooth muscle? Which 2 receptor subtypes mediate this action?

A

Vasoconstiction

5HT2 and 5HT1D

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7
Q

How can serotonin indirectly cause vasodilation? What receptor subtype mediates this action?

A
  • presynaptic receptor inhibits the release of NOR

- 5HT1

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8
Q

What serotonin receptor mediates platelet aggregation?

A

5HT2

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9
Q

What are the 2 major roles of serotonin following vascular injury? What receptor subtype mediates these actions?

A

Platelet aggregation / thrombus formation
Vasoconstriction
5HT2A

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10
Q

What is the bezold Jarisch reflex? What serotonin receptor subtype mediates this effect?

A

reflex bradycardia due to stimulation of sensory nerve endings - decreased sympathetic stim, increased vagus activity to heart
5HT3

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11
Q

What is the effect of serotonin on the GI and bronchiolar smooth muscle? What is carcinoid syndrome?

A
  • Contraction of those muscles

- Diarrhea because of too much 5HT release

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12
Q

What are the receptor targets of cyproheptadine? What are its actions at these receptors? What is this drug used for? What is a non-specific receptor target of this drug? What are 2 side effects?

A
  • 5hT 1 and 5ht2
  • Antagonist
  • Carcinoid tumors
  • H1 histamine receptor
  • Drowsiness, GI disturbance
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13
Q

What is the receptor subtype targeted by ketanserin? What is it used for? What is the mechanism? What is a non selective drug target of this drug?

A

5HT2 antagonist
Hypertension
Blocks vascular 5HT2
Alpha 1 adrenergics on smooth muscle

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14
Q

What is the action of LSD on serotonin receptors? What is its physiological effect?

A

5HT2 antagonist

Vascular smooth muscle constrictor

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15
Q

What is the action of ergonivine on serotonin receptors? What is it used to test diagnostically? What is it used to treat? (2)

A
  • 5ht2 partial agonist, weak antagonist
  • diagnostic for vasospastic angina
  • Post partum and post abortal hemorrhage
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16
Q

What is the action of methysergide on serotonin receptors ? What is it used to treat?

A

5HT2 antagonist, 5HT1 partial agonist

Carcinoid tumors

17
Q

What is the action of ergotamine on serotonin receptors? What is its physiological action? What is it used to treat? (2)

A

Partial 5HT1/2 agonist
VSM constrictor
Migraines, post partum bleeding

18
Q

Both ergotamine and ergonovine are effective for the treatment of post partum bleeding. Which is preferred and why?

A

Ergonovine

Less toxic, more active

19
Q

What are 2 general side effects associated with 5HT2 agonists? What is specific for methysergide?

A

GI disturbances, prolonged vasospasm

Methy - CNS disturbances (hallucination)

20
Q

What are the receptor targets of the triptans? What are their actions at these receptors? What are they used to treat (2)?

A

5HT1B/D/F agonists

Migraines, cluster headaches

21
Q

What are the 3 triptans provided as examples? What is their mechanism? What is a secondary effect on these drugs on vasculature?

A

Suma/Zolmi/Riza-triptan
Activate presynaptic 5HTR, block trigem system, block release of inflammatory peptides
Vasoconstriction

22
Q

How does zolmitriptan compare to sumatriptan (tablet form for both)? (2)

A

More lipophillic

Longer half life

23
Q

What are 2 side effects of triptans? What patient population is contraindicated?

A

Recurrent migraine, coronary spasm (in CV disease)

Hepatic failure patients

24
Q

While none are on the market yet, what is the expected effect of inverse agonists of the 5HT2A receptor? (3) What would they be used for (2)?

A

Reduced platelet aggregation
Reduced arterial constriction
Reduced vessel wall thickening
Prevent MI and stroke

Medical Pharmacology Exam 3 (13 decks)

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