Serotonin Agonists Flashcards

1
Q

5-HT receptors:

1B does what?

A

mediate vasoconstriction

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2
Q

5-HT receptors:

1D does what?

A

inhibit neurotransmitter release

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3
Q

5-HT receptors:

1F does what?

A

inhibit release of nociceptive signaling molecules

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4
Q

what is the structural difference between Ergotamine and Dihydroerotamine?

A

DHE does not have a double bond in a ring

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5
Q

Ergots are selective for which subsets of serotonin receptors

A

2A; 1B; 1D; 1F

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6
Q

Poor or Great Absorption of Ergots?

A

Poor

aka available as IM, nasal spray, SL tablet

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7
Q

Ergots are partial ________ receptor agonists

A

alpha1

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8
Q

which ergot is less prone to cause severe peripheral vasoconstriction with frequent dosing

A

DHE

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9
Q

Do Ergots have short or long half lives

A

long

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10
Q

why do Ergots have a long half life

A

because they have active metabolites and and tight binding to tissues

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11
Q

what are the side effects of Ergots

A

GI (diarrhea, N/V)
causes uterine stimulants (aka contraindicated in pregnancy)
Gangrene

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12
Q

Triptans are selective for which subsets of serotonin receptors

A

1B, 1D, 1F

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13
Q

which triptan has the shortest half life

A

Sumtriptan and Rizatriptan (with 2 hr)

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14
Q

which triptan has the longest half life

A

Frovatriptan

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15
Q

what is the notable structural difference in Frovatriptan

A

it is TRICYCLIC

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16
Q

what drug is under study for selective 5-HT1F agonist

A

Lasmiditan

17
Q

why is selective 5-HT1F agonists beneficial

A

1F agonism can prevent Substance P, Neurokinin A, CGRP release (aka prevent inflammation)

18
Q

CGRP is a vaso_______

A

dilator

19
Q

CGRP potentiates ______

A

pain

20
Q

(Agonism or Antagonism) of CGRp receptor is effective for aborting migraine

A

Antagonism

21
Q

Rank the Drug Classes for Migraines with Most Risk for Vasospasm to Least Likely

A

MOST LIKELY: Ergot –> Triptans –> 5-HT1F