5-HT and migrane Flashcards

1
Q

buspirone

A

5-HT1 partial agonist

Non-benzodiazepine anxiolytic

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2
Q

dexfenfluramine

A

5-HT2c agonist

Appetite suppression

Withdrawn due to toxicity

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3
Q

cisapride

A

5-HT4 agonist

Used for treatment of GERD and motility dissorders

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4
Q

almotriptan

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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5
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)
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6
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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7
Q

naratriptan

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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8
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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9
Q

sumatriptan

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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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

phenoxybenzamine

A

5-HT2 antagoinst

  • Long acting 5-HT2 antagonists (+ alpha adrenergic receptors)
    *
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12
Q

cyproheptadine

A

5-HT2 antagonist

  • Cyprohepatidine
    • 5-HT2 antagonist and H1 receptor antagonist
    • Useful for the SM effects of carcinoid tumors
    • Serotonin syndorme treatment
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13
Q

alosetron

A

5-HT3 receptor antagonist

treatment of IBS drug

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14
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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15
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

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16
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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17
Q

ergotamine mixtures, ergotamine tartrate

A

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
18
Q

methylergonovine

A

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
19
Q

methysergide

A

non selective 5-HT agonist

serotonin antaboinsts

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

20
Q

lysergic acid diethylamine

A

LSD - non selective 5-HT agonist

no clinical use

21
Q

ergotamine

A

non selective 5-HT agonist

Ergotamine: potent vasoconstrictor

22
Q

ergocryptine

A

non selective 5-HT agonist

23
Q

bronmocriptine

A

non selective 5-HT agonist

24
Q

cabergoline

A

non selective 5-HT agonist

25
Q

propranolol

A

B blocker - used in preventive therapy for migranes

26
Q

metoprolol

A

B blocker - used in preventive therapy for migranes

27
Q

amitriptyline

A

antidepressant - used in preventive threapy for migrane

drowsyness

28
Q

divalproex

A

anticonvulsant - used in preventive threapy for migrane

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

29
Q

topiramate

A

anticonvusant - used in preventive threapy for migrane

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

30
Q

flunarizine

A

CCB - used in preventive threapy for migrane

tiredness, weight gain, depression ,parkinsonism

31
Q

verapamil

A

CCB - used in preventive threapy for migrane

constipation, leg swelling, arterioventricular conduction disturbances

32
Q

methysergide

A

serotonin antagonist - used in preventive threapy for migrane (withdrawn)

33
Q

fluoxetine

A

prozac - SSRI - used in preventive threapy for migrane

anxiety, insomnia

34
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

35
Q

chlorpromazine

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

36
Q

prochlorperazine

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

37
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
38
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
39
Q

butorphanol

A

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
40
Q

oxycodone

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
41
Q

hydromorphone

A

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