Pharmacologic Management of Headaches Flashcards

1
Q

Abortive tx for migraine headaches

A
  • Aspirin, acetaminophen, NSAID, Combination thereof including caffeine
  • *Triptans: 5-HT 1b/1D agonists
    • (like alpha 2 for NE) (sumitriptan or Imitrex) (60-85% effective)
  • *Ergotamine derivative
    • not often used b/c cause nausea. Super effective (90% abort)
  • * Migraine specific analgesic
    • e.g. combo drug: ibuprofen/caffeine/aspirin
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2
Q

Prophylactic tx for migraine headaches

A
  • daily dosing, limit side effects (about 50% effective at limiting migraines in terms of frequency, duration, or severity)
  • ​Beta blockers
  • Calcium channel blockers
  • Tricyclic antidepressants
  • Anti-epileptics
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3
Q

Cluster headache tx

A
  • Oxygen, triptans, ergots, lidocaine locally
  • Transitional (use during cluster): corticosteroids to get over hump
  • Prophylaptic: Ca channel blocker, lithium (not effective in other HA types), anti-epileptics
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4
Q

Tension headache tx

A
  • Abortive - aspirin, NSAID, tylenol, muscle relaxants
  • Prophylactic: trycyclic antidepressant (amitriptyline), SSRI (e.g prozac)
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5
Q

Serotonin involvement in first phase of migraine headache

A
  • First phase is characterized by cerebral vasoconstriction and ischemia.
    • Serotonin release (5HT) from neurons and platelets (PERIPHERAL MECHANISMS) that acts on 5-HT2 receptors contributes to this phase.
    • Target: decrease release of seratonin with a _triptan _
      • triptans MOA ~ alpha-2 agonist effect on NE release
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6
Q

Serotonin involvement in second phase of migraine headache

A
  • Second phase is characterized by cerebral vasodilation and pain.
    • Neurons in the trigeminal complex release the vasoactive peptides substance P and calcitonin gene-related peptide [CGRP] ==> vasodilation and neuroinflammation of pial and dural vessels (SENSORY NERVE DISCHARGE).
    • This in turn stimulates nociceptive fibers of the trigeminal nerve that causes pain.
    • Target: decrease vasodialtion - triptans
      • MOA: agonist @ serotonin receptors ==> vasoconstriction
        • decreases sub P/CGRP release
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7
Q

Triptans examples & general use

A
  • sumatriptan
  • zolmitriptan
  • abortive tx for migraine headache
  • 1st line for severe headache (if no CV issues)
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8
Q

Triptans (sumatriptan, zolmitriptan) MOA

A
  • Vasoconstriction,
  • Inhibition of inflammatory mediators presynaptically
  • Inhibit activation of trigeminal neuron
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9
Q

Triptans (sumatriptan, zolmitriptan) Route of administratration

A
  • Oral
  • Nasal
  • subcutaneous possible for sumatriptan
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10
Q

Triptans (sumatriptan, zolmitriptan) Route of onset/duration

A
  • onset: ~30-60 min
  • duration: short
    • t1/2 = 2-4 hr
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11
Q

Triptans (sumatriptan, zolmitriptan) side effects

A
  • Paresthesias, flushing, dizziness, drowsiness, chest tightness
  • Rarely: coronary vasospasm, angina, MI, arrythimia, stroke, death
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12
Q

NSAIDs examples and general use

A
  • Ibuprofin
  • Naproxin
  • abortive therapy for tension or migraine headaches
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13
Q

NSAIDs MOA & route of administration

A
  • Inhibition of COX-2
  • Decrease inflammation
  • oral administration
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14
Q

NSAIDs onset/duration

A
  • 4-6 hours duration (ibuprofen)
  • 8-12 hours duration (Naproxen)
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15
Q

NSAIDs side effects

A
  • Increased risk of bleeding if taking anticoagulants/antiplatelets
  • take caution in pts w/peptic ulcer, acute gastritis, renal insufficiency, or bleeding disorder
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16
Q

Ergot Alkyloids examples and general use

A
  • dihydroergotamine
  • 2nd line in severe HA
17
Q

Ergot Alkyloids (duhyrdoergotamine) MOA

A
  • Seratonin (5HT) 1b/1d agonist = ~similar MOA to triptans
    • inhibits serotonin release (similar to alpha-2 receptor effect on NE)
  • ==> vasoconstriction
  • ==> inhibition of inflammatory mediators presynaptically
  • ==> inhibiton of activation of trigeminal neuron
18
Q

Ergot Alkyloids (duhyrdoergotamine) route of administration

A
  • dihydroergotamine: intranasal or paranasal
  • ergotamine: oral
19
Q

Ergot Alkyloids (duhyrdoergotamine) onset & duration

A
  • rapid onset
  • long duration
20
Q

Ergot Alkyloids (duhyrdoergotamine) side effects

A
  • Less effective + more toxic than triptans, 2nd line
  • Cause N/V, diarrhea, cramps, parathesis.
    • Give w/ anti-emetic.
  • SERIOUS: vascular occlusion and gangrene (strict dosage limits) → alpha 1 adrengergic vasoconstriciton
  • Severe peripheral ischemia with beta blockers due to vasoconstriction
21
Q

NSAIDs in migraine prophylaxis: efficacy vs. safety/side effects

A
  • used as short term prevention
  • SE: gastric problems, increased risk of bleeding if taken w/anticoag or antiplatelets
22
Q

Beta-Blockers (propanolol) in migraine prophylaxis: efficacy vs. safety/side effects

A
  • First line drug of choice:
    • reduces migraine frequency by 50% in 50% of patients.
    • dose must be titrated to each patient
  • SE: Fatigue, exercise intolerance, depression, orthostatic hypertension
23
Q

Calcium-channel blockers (verapamil) in migraine prophylaxis: efficacy vs. safety/side effects

A
  • less effective than BB
  • limited evidence of effectiveness
  • contraindicated with concurrent BB use b/c of heart block
24
Q

Tricyclic antidepressants (amitriptyline) in migraine prophylaxis: efficacy vs. safety/side effects

A
  • occassionaly efficacy in migraine prevention
  • SE:
    • sedation
    • dry mouth
    • constipation
    • tachycardia
    • urinary retention
    • weight gain
25
Q

Anticonvulsant agents (topiramate) in migraine prophylaxis: efficacy vs. safety/side effects

A
  • Reduces frequency of migraines by 50% in 50% of patients
  • SE:
    • sedation
    • nausea
    • weight gain
    • tremor
    • hair loss
    • contraindicated in pregnancy
26
Q
A