Serotonin Flashcards

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1
Q

5-HT1(A-E)

A
  • inhibition of adenylate cyclase (GPCR)

- 5HT1A also opens K channgel

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2
Q

5-HT2(A-C)

A

-PI hydrolysis (GPCR)

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3
Q

5-HT3

A
  • ligand-gated cation channel

- NOT GPCR

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4
Q

5-HT4-7

A

-activation of adenylate cyclase or unknown

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5
Q

CV effects of serotonin

A
  • potent vasoconstriction of large arteries and veins, including cranial blood vessels, via 5-HT1D
  • vasodilation of coronary, skeletal muscle, and cutaneous blood vessels
  • Bezold-Jarisch reflex: coronary chemoreceptors (causes bradycardia, hypotension, hypoventilation)
  • platelet aggregation-active uptake of serotonin from circulation
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6
Q

CNS effects of serotonin

A
  • sensory perception/LSD and drug abuse
  • sleep–slow wave deep sleep
  • temperature regulation
  • neuroendocrine regulation: release of ACTH, GH, prolactin, TSH, FSH, LH (anterior pituitary hormones)
  • learning and memory, particularly short-term
  • pain perception
  • emesis–5-HT3 receptors
  • mental illness–affective disorders, schizophrenia, OCD, anxiety, aggressive behavior
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7
Q

Lysergic acid diethylamide

A

-relatively non-specific; 5HT2 receptor. potent hallucinogen.

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8
Q

Buspirone

A
  • 5-HT1A receptor partial agonist

- Antianxiety med

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9
Q

Sumatriptan

A
  • and other triptans
  • 5-HT1B/D receptors on cerebral blood vessels
  • inhibit release of vasoactive peptides (CGRP), promote vasoconstriction, block brainstem pain pathways, inhibit trigeminal nucleus caudalis.
  • treatment of migraine headaches; stops existing ones (abortive)
  • triptans are major class of drugs used to stop existing migraines (frovatriptan is long-acting; can be used prophylactically)
  • side effects: peripheral vasoconstriction, nausea/vomiting, angina, dizziness, flushing
  • contraindications: stroke, MI, uncontrolled HTN, ischemic heart disease
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10
Q

Other abortive migraine treatment

A
  • ergots: DHE, many routes; ergotamine, oral
  • NSAIDS with caffeine
  • steroids
  • butalbital/caffeine/acetaminophen–base choice because it has potential for abuse and headaches get worse when you stop taking it.
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11
Q

Amitryptyline, Nortriptyline

A
  • TCAs used for migraine prophylaxis

- sedating, anticholinergic, effective for many pain sources

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12
Q

Antiseizure meds used for migraine prophylaxis

A
  • Divalproex sodium/Valproic acid
  • Topiramate
  • Gabapentin, Pregabalin, Lamotrigine
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13
Q

Vasoactive agents used for migraine prophylaxis

A
  • Beta blockers: propranolol, atenolol

- CCBs: verapamil, diltiazem

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