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5-HT and migrane COPY Flashcards

1
Q

ondansetron, granisetron, dolasetron

A

5-HT3 receptor antagonist

  • Ondansetron, granisetron, dolasetron
    • 5-HT3 receptor antagonists
    • Treatment of nausea and vomiting in cancer chemo
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2
Q

frovatriptan

A

selective 5-HT1d and 5-HT1b receptor agonist

oral

  • 5-HT1b/1d agonists (sumatriptan)
    • Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
    • Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
    • Efficacy agasint migrane similar to other classes of drugs
    • Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
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3
Q

divalproex

A

anticonvulsant - used in preventive threapy for migrane

weight gain, tremor, hari loss, hemotological and liver problems, teratogenicity

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4
Q

dexfenfluramine

A

5-HT2c agonist

Appetite suppression

Withdrawn due to toxicity

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5
Q

ergonovine

A

non selective 5-HT agonist

ergot derivative

taking with caffene may help absorption

Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors

Disadvantages

Complex pharmacology/kinetics

Potent and sustained vasoconstrictor effects

Increased risk of vascular effects - contraindicated in patients with CAD

Ergonovine is the most selective for the uterus

If oxytocin fails, is utilized to limit post partum hemorrhage

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6
Q

propranolol

A

B blocker - used in preventive therapy for migranes

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7
Q

metoprolol

A

B blocker - used in preventive therapy for migranes

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8
Q

cabergoline

A

non selective 5-HT agonist

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9
Q

lysergic acid diethylamine

A

LSD - non selective 5-HT agonist

no clinical use

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10
Q

zolmitriptan

A

selective 5-HT1d and 5-HT1b receptor agonist

oral

  • 5-HT1b/1d agonists (sumatriptan)
    • Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
    • Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
    • Efficacy agasint migrane similar to other classes of drugs
    • Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
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11
Q

NSAIDs

A
  • used in migrane acute attacks

not selective for migranes - can have other probelms

  • Non specific pain therapy
    • Aspirin
    • Naproxen, ibuprofen (NSAIDs)
    • Acetaminophen
    • Geneally poorly effects - can also get sensitized to the pain
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12
Q

cisapride

A

5-HT4 agonist

Used for treatment of GERD and motility dissorders

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13
Q

bronmocriptine

A

non selective 5-HT agonist

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14
Q

meperidine

A

opiates

  • used in migrane acute attacks

not selective for migranes - can have other probelms

  • Meperidine, butophanol, oxycodone, hydromorphone
  • AE
    • Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
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15
Q

rizatriptan

A

selective 5-HT1d and 5-HT1b receptor agonist

oral

  • 5-HT1b/1d agonists (sumatriptan)
    • Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
    • Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
    • Efficacy agasint migrane similar to other classes of drugs
    • Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
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16
Q

methysergide

A

non selective 5-HT agonist

serotonin antaboinsts

AE: drowsiness, leg cramp, hair loss, retrorbital fibrosis

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17
Q

verapamil

A

CCB - used in preventive threapy for migrane

constipation, leg swelling, arterioventricular conduction disturbances

18
Q

metoclopramide

A

antiemetic - used in migrane acute attacks

Adjunctive therapy to combat nausea and vomiting due to migraine or ergot alkaloid treatment

Centrally acting dopamine receptor antagonists

19
Q

ergotamine

A

non selective 5-HT agonist

Ergotamine: potent vasoconstrictor

20
Q

eletriptan

A

selective 5-HT1d and 5-HT1b receptor agonist

oral

  • 5-HT1b/1d agonists (sumatriptan)
    • Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP)
    • Constrict cerebral and meningeal vessels in treatment of actue migrane headaches
    • Efficacy agasint migrane similar to other classes of drugs
    • Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
21
Q

buspirone

A

5-HT1 partial agonist

Non-benzodiazepine anxiolytic

22
Q

ergocryptine

A

non selective 5-HT agonist

23
Q

phenoxybenzamine

A

5-HT2 antagoinst

  • Long acting 5-HT2 antagonists (+ alpha adrenergic receptors)
    *
24
Q

dihydroergotamine

A

non selective 5-HT agonist

ergot derivative

taking with caffene may help absorption

Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors

Disadvantages

Complex pharmacology/kinetics

Potent and sustained vasoconstrictor effects

Increased risk of vascular effects - contraindicated in patients with CAD

25
naratriptan
selective 5-HT1d and 5-HT1b receptor agonist oral * 5-HT1b/1d agonists (sumatriptan) * Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP) * Constrict cerebral and meningeal vessels in treatment of actue migrane headaches * Efficacy agasint migrane similar to other classes of drugs * Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
26
fluoxetine
prozac - SSRI - used in preventive threapy for migrane anxiety, insomnia
27
flunarizine
CCB - used in preventive threapy for migrane tiredness, weight gain, depression ,parkinsonism
28
butorphanol
opiate - used in migrane acute attacks not selective for migranes - can have other probelms * Meperidine, butophanol, oxycodone, hydromorphone * AE * Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
29
topiramate
anticonvusant - used in preventive threapy for migrane weight gain, tremor, hari loss, hemotological and liver problems, teratogenicity
30
cyproheptadine
5-HT2 antagonist * Cyprohepatidine * 5-HT2 antagonist and H1 receptor antagonist * Useful for the SM effects of carcinoid tumors * Serotonin syndorme treatment
31
ergotamine mixtures, ergotamine tartrate
non selective 5-HT agonist * Taking with caffeine may help absorption * Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors * Disadvantages * Complex pharmacology/kinetics * Potent and sustained vasoconstrictor effects * Increased risk of vascular effects - contraindicated in patients with CAD
32
hydromorphone
opiate - used in migrane acute attacks not selective for migranes - can have other probelms * Meperidine, butophanol, oxycodone, hydromorphone * AE * Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
33
methysergide
serotonin antagonist - used in preventive threapy for migrane (withdrawn)
34
prochlorperazine
antiemetic - used in migrane acute attacks ## Footnote Adjunctive therapy to combat nausea and vomiting due to migraine or ergot alkaloid treatment Centrally acting dopamine receptor antagonists
35
methylergonovine
non selective 5-HT agonist * Taking with caffeine may help absorption * Mechanism - vasoconstriction due to stimulation of alpha and 5-HT receptors * Disadvantages * Complex pharmacology/kinetics * Potent and sustained vasoconstrictor effects * Increased risk of vascular effects - contraindicated in patients with CAD
36
chlorpromazine
antiemetic - used in migrane acute attacks ## Footnote Adjunctive therapy to combat nausea and vomiting due to migraine or ergot alkaloid treatment Centrally acting dopamine receptor antagonists
37
alosetron
5-HT3 receptor antagonist treatment of IBS drug
38
oxycodone
opiates - used in migrane acute attacks not selective for migranes - can have other probelms * Meperidine, butophanol, oxycodone, hydromorphone * AE * Rebound headaches, dizziness, nausea, vomiting, impaired cognitive function, constipation
39
sumatriptan
selective 5-HT1d and 5-HT1b receptor agonist oral * 5-HT1b/1d agonists (sumatriptan) * Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP) * Constrict cerebral and meningeal vessels in treatment of actue migrane headaches * Efficacy agasint migrane similar to other classes of drugs * Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)
40
amitriptyline
antidepressant - used in preventive threapy for migrane drowsyness
41
almotriptan
selective 5-HT1d and 5-HT1b receptor agonist oral * 5-HT1b/1d agonists (sumatriptan) * Inhbition of release of the vasodilating peptide calcitonin gene related peptide (CGRP) * Constrict cerebral and meningeal vessels in treatment of actue migrane headaches * Efficacy agasint migrane similar to other classes of drugs * Adverse effects including: tingling or warmth, sensations, dizziness, muscle weakness, neck pain, chest discomfort (vasospasm, angina - it can feel like this)

IC (32 decks)

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