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IC > 5-HT/Migraine > Flashcards

5-HT/Migraine Flashcards

1
Q
  • rapidly metabolized by MAO and stored, 90% found in enterochromaffin cells of GI treact
  • stored in platelets and serotonergic nerve endings
  • concentration in vesicles blocked by reserpine
A

serotonin (5-hydroxytryptamine)

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2
Q

-5-HT3 receptors in GI tract and medulla produce the ______ reflex

A

vomiting

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3
Q

5-HT2 stimulates platelet _______

A

activation

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4
Q
  • serotonin receptor on GI tract that stimulates smooth muscle
  • increased tone, facilitation of peristalsis
A

5-HT2

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5
Q
  • serotonin receptor on GI tract that increases acetylcholine from nervous system
  • prokinetic effect
A

5-HT4

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6
Q

carcinoid syndrome in GI tract produces ______

A

diarrhea

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7
Q
  • 5HT1a partial agonist

- non benzodiazepine anxiolytic

A

buspirone

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8
Q
  • 5-HT2c agonist
  • appetite suppression
  • withdrawn due to toxicity
A

dexfenfluramine

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9
Q
  • inhibit release of vasodilating peptide CGRP
  • constrict cerebral and meningeal vessels in treatment of acute migraine headaches
  • adverse: tingling, warm sensations, muscle weakness, neck pain, chest discomfort
A

-triptans (5-HT1b/1d agonist)

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10
Q

-5HT4 agonist used for treatment of GERD and motility disorders

A

cisapride

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11
Q

-partial 5HT4 agonist, utilized for IBS with constipation

A

tegaserod

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12
Q
  • long acting 5-HT2 antagonist

- also alpha adrenergic antagonist

A

phenoxybenzamine

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13
Q
  • 5HT2 antagonist and H1 receptor antagonist
  • useful for smooth muscle effects of carcinoid tumors
  • serotonin syndrome treatment
A

cyprohepatidine

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14
Q
  • 5HT3 receptor antagonists

- treatment of nausea and vomiting in cancer chemo

A

-setrons

ondansetron, granisetron, dolasetron

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15
Q
  • HTN, hyperreflexia, tremor, clonus, hyperthermia, hyperactive bowel sounds, diarrhea, mydriasis, agitation, coma
  • precipitating drugs: SSRIs, 2nd gen antidepressants, MAOIs, linezolid, tramadol, meperidine, fentanyl, ondansetron, sumatriptan, MDMA, LSD, St Johns Wort, ginseng
A

Serotonin syndrome

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16
Q
  • catecholamine and serotonin like

- admin with caffeine increases absorptin

A

ergot alkaloids

17
Q
  • selectivity for dopamine receptors

- ergot alkaloids that suppress prolactin secretion, treat pituitary tumor

A

bromocriptine, cabergoline

18
Q

ergot alkaloid that’s a potent vasoconstrictor in vascular smooth muscle

A

ergotamine

19
Q

limited 5-HT effects, but preferred for treatment of migraine, an ergot alkaloid

A

dihydroergotamine

20
Q
  • most selective ergot alkaloid for the uterus, stimulate smooth muscle
  • if oxytocin fails, is utilized to limit postpartum hemorrhage
A

ergonovine

21
Q
  • side effects: GI disturbances n/v/d due to increased GI motility resulting from activation of 5-HT receptors in CNS and GI
  • prolonged vasospasm in arms and legs, may cause gangrene
  • drowsiness and hallucinations occur infrequently
A

toxicity of ergot alkaloids

22
Q
  • episodic attacks of headache lasting 4-72 hours
  • two of following: unilateral pain, pain moderate to severe, throbbing, aggravation on movement
  • one or more: nausea, vomiting, photophobia, phonophobia
A

migraine

23
Q

ergotamine, dihydroergotamine, triptans are _______ migraine drugs

A

specific

24
Q
  • which beta blockers used in preventive therapy of migraine?
  • adverse: tiredness, postural, contra in asthma
A

propanolol (b1, b2)

metoprolol (b1)

25
Q

antidepressant used in preventive migraine therapy? adverse - drowsiness

A

amitriptyline

26
Q
  • anticonvulsants used in preventive therapy of migraine

- adverse: drowsiness, weight gain, tremor, hair loss, liver abnormality

A

valproate, topiramate

27
Q

calcium channel blockers used in preventive therapy of migraine?
-adverse: tiredness, weight gain, depression, parkinsonism

A

flunarizine, verapamil

28
Q
  • serotonin antagonist used in preventive therapy of migraine?
  • drowsiness, leg cramps, hair loss, retroorbital fibrosis
A

methysergide

29
Q

SSRI used in preventive therapy of migraine?

-adverse: anxiety, insomnia

A

fluoxetine

30
Q

NSAIDS are non specific therapy for treatment of ______ migraine attacks

A

acute

31
Q

analgesic overuse can _______ migraine, limit drug treatment to 2-3 days

A

transform

32
Q
  • meperidine, butophanol, oxycodone, hydromorphone
  • relief for severe migraine, risk of dependence and tolerance
  • rebound headaches, dizziniess, n/v, cognitive function
  • risk of transforming migraine
A

opiate analgesics

33
Q
  • metoclopramide
  • chlorpormazine
  • prochlorperazine
A

antiemetics, treat acute migraines

34
Q
  • adjunctive therapy to combat n/v due to migraine and alkloid treatment
  • centrally acting dopaming receptor antagonists
A

antiemetics - metoclopramide, chlorpromazine, prochlorperazine

35
Q
  • weak 5-HT3 receptor antagonist

- anti-emetic

A

metoclopramine

36
Q
  • migraine specific therapy
  • vascoconstriction due to stimulation of alpha-adrenergic and 5-HT3 receptors
  • cerebral vasoconstriction has been attributed to partial agonist effects on neuronal 5-HT1d receptors
A

ergotamine, dihydroergotamine

37
Q
  • effective, low cost
  • adverse: complex, variable absorption, potent and sustained vasoconstrictive effect –> increased risk of vascular effects
A

ergot derivatives

38
Q
  • selective 5-HT1d and 1b receptor agonists
  • distinctive advantages: selective pharm, established efficacy
  • higher cost and restrictions in presence of CV disease
  • inhibit activation of trigeminal afferent nociceptors, cranial vasoconstriction
A

-triptans

39
Q
  • mimic angina
  • contraindications - ischemic heart disease, HTN, cerebrovascular disease
  • tingling, sensation of warmth, dizzy, flushing, neck pain, stiffness
A

triptans

IC (29 decks)

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