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brain > IC4 Migraine meds pharmacology > Flashcards

IC4 Migraine meds pharmacology Flashcards

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1
Q

What causes a headache/migraine? (pathophysiology)

A

vasodilation of intracranial extracerebral (ie. meningeal) bood vessels –> activation of perivascular trigeminal nerves –> releases vasoactive neuropeptides –> promotes neurogenic inflammation

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2
Q

What are the common OTC meds that can be used for headache/mild migraine?

A

paracetamol
NSAIDs

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3
Q

What are the medications available for moderate to severe migraines refractive to NSAIDs and paracetamol?

A
  1. cafergot
  2. sumatriptan
  3. erenumab
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4
Q

What are the components of cafergot?

A

caffeine + ergotamine

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5
Q

Describe the MOA of cafergot

A

Ergotamine: 5-HT1B/1D receptor agonist + alpha adrenergic receptor partial agonist

Caffeine: cranial vasoconstrictor + enhances GI absorption of ergotamine

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6
Q

When can cafergot be used?

A

Acute treatment of migraine

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7
Q

What quirk does cafergot have?

A

Inhibits 3A4

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8
Q

What is the impact of its quirk?

A

Avoid use with other 3A4 inhibitors eg. macrolide abx as it increases risk of ergot toxicity

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9
Q

What are the common side effects of cafergot?

A

N/V

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10
Q

What are the rare side effects of cafergot?

A
  • Hypersensitivity
  • MI
  • Ergot poisoning
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11
Q

What drugs cannot be used together with cafergot?

A

other vasoconstricting agents eg. ergot alkaloids, sumatriptan, other 5HT1 agonists

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12
Q

Describe the MOA of sumatriptan

A

Selective agonist for 5-HT1B and 5-HT1D receptors on trigeminal nerves and intracranial extracerebral (ie. meningeal) blood vessels

*does not affect cerebral blood flow

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13
Q

When can sumatriptan be used?

A

Acute treatment of migrane w or w/o aura and those a/w menstrual period in women

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14
Q

What are the common side effects of sumatriptan?

A
  • Dysgeusia (unpleasant taste)
  • N/V
  • Dizziness
  • Flushing, tingling sensation
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15
Q

What are the rare and serious side effects of sumatriptan?

A
  • Serotonin syndrome (feeling agitated & restless, other mental changes eg. hallucination, heavy sweating/shivering, fast HR/irregular heartbeat, rigit/twitching muscles, N/V or diarrhoea)
  • MI
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16
Q

What are the contraindications of sumatriptan?

A
  • hypersensitivity to triptans
  • concurrent MAOi
  • MI
  • uncontrolled HTN, IHD, PVD, CVA, TIA, severe hepatic impairment
17
Q

How is sumatriptan cleared?

A

mainly via hepatic metabolism via MAO-A

18
Q

Can sumatriptan be used in pediatrics?

A

no

19
Q

Can sumatriptan be used in elderly >65?

A

use with caution

20
Q

Can sumatriptan be used in pregnancy?

A

use w caution

21
Q

Can sumatriptan be used in breastfeeding

A

excreted into breastmilk; withhold breastfeeding for 8-12h after dose

22
Q

Can sumatriptan be used in renal impairment?

A

yes; no dosage adj req

23
Q

Can sumatriptan be used in hepatic impairment?

A

mild-moderate: dose reduction (due to increased F)
severe: C/I

24
Q

What are the key DDIs to look out for sumatriptan?

A
  1. ergotamines (avoid sumatriptan within 24h of ergot meds; avoid ergot meds within 6h after taking sumatriptan)
  2. MAOi (cannot use triptan within 2wk of discontinuation of MAOi)
  3. triptans (cannot take another triptan within 24h after taking sumatriptan)
25
Q

What is a key counseling point for sumatriptan?

A

limit use to 9-10 days per month as may result in medication overuse headache (MOH)

26
Q

Describe the MOA of erenumab

A

Blocks CGRP receptor

27
Q

When can erenumab be used?

A

Prophylaxis of migraine in adults who have at least 4 migraine days per month

28
Q

What is the route of administration of erenumab?

A

monthly SQ injection

29
Q

What are the side effects of erenumab?

A
  • hypersensitivity
  • injection site reaction
  • constipation
  • pruritis

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