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Anti-Migraine Agents
Dr. Barman's Lecture Rx's
15
Medical
Graduate
11/09/2011

Additional Medical Flashcards

 


 

Cards

Term
Pharmacological effects of Ergot Alkaloids
Definition

- Compounds based on Lysergic Acid

- Amine or amino side chain

- Non-selective pharmacological agents that interact with:

    • α-adrenergic receptors
    • serotonergic receptors (5-HT1 and 5-HT2)
    • dopaminergic receptors

- Anti-migraine effects likely mediated via 5HT1B/1D receptors.

 

Term
Side effects of Ergot Alkaloids
Definition

- Excessive use: Rebound Headaches, coronary vasospasm, ergotism (toxic effects of chronic ergot use - convulsions, hallucinations, dry gangrene etc...)

 

Common Side Effects:

  • N&V
  • Tingling in extremities
  • Abdominal Pain
  • Muscle aches/tremors
Contraindicated:
  • pregnancy
  • uncontrolled hypertension
  • coronary artery or peripheral vascular disease
  • sepsis
  • peptic ulcer, liver or kidney disease
Term
Pharmacological Effects of Serotonin Agonists
Definition

- Agonists are highly selective for 5-HT1B/1D receptors

- Inhibit cGRP release

- Inhibit vasodilation

Term
Side Effects of Serotonin Agonists
Definition
  • Drowsiness
  • Dizziness
  • Fatigue
  • N&V
Contraindicated:
  • Ischemic HD
  • Angina pectoris
  • Hypertension
Term
Sumatriptan
Definition

- 5-HT1B/1D agonist

- Inhibitor of proinflammatory NTs

- Closes carotid anastamoses

- Single dose effective in decreasing migraine severity (80%)

- Subcutaneous: Rapidly absorbed, high bioavailability, max concentration in 10 min., faster onset than ergots

- Oral: Only 15% bioavailable, max concentration in 1.5 hours, can titrate, more effective that ergotamine/caffeine combo.

- Intranasal: do not give 2 doses w/in 2 hours of each other, relief in 15-60 minutes post-dose, minimal side effects

Term
Naratriptan
Definition

- Similar to sumatriptan

- Less HA recurrence

- Better bioavailability

- Prolonged duration of action

- Take tablet at onset of HA

Term
Zolmitriptan
Definition

- More rapidly absorbed than sumatriptan

- Tablet form

- Better oral availability than sumatriptan

- Use with caution in pts. with liver disease (clearance reduced which can lead to hypertension**)

Term
Treximet
Definition

- Sumatriptan/Naproxen (Takes care of the neuronal and vascular)

- 5-HT1B/1D agonist + NSAID

- Constricts basilar artery and vasculature of dura mater

- Inhibits synthesis of inflammatory mediators (prostaglandins)

- No significant effect on adrenergic, dopaminergic, muscarinic or benzodiazepine receptors

 

Contraindicated w/ any form of vascular disease or hepatic impariment, don't use with ergots

Term
When to use prophylaxis
Definition

- 3 or more attacks/month

- Do not respond to symptomatic Rx

- Migraines that are predicatable in occurence

- Start at low doses and titrate up

- Treat for 3-6 months and then titrate off treatment

Term

Ergotamine

Dihydroergotamine

-class

-mechanism

Definition
  • partial α-adrenergic receptor agonist
  • partial 5-HT1 receptor antagonist
  • ergot alkaloid - amino acid
Term

Bromocriptine

-class

-mechanism

 

 

Definition
  • dopamine receptor agonist
  • Ergot alkaloid - amino acid
Term

Methysergide

-class

-mechanism

Definition
  • 5-HT2 receptor antagonist
  • Ergot alkaloid - amine
Term
Migrane prophylactic agents
Definition

Beta blockers

Calcium channel blockers

Tricyclic antidepressants

Anticonvulsants

Methysergide

Supplements (riboflavin, magnesium)

Term
Acute migraine agents
Definition

Ergot derivatives

Serotonin agonists

NSAID's, aspirin, acetominophen

Combination drugs (ex: excedrin migraine)

Opiates

COX inhibitors/blockers

Angiotensin II receptor blockers

Term
Migraine Combo Therapy
Definition

Treximet = sumptriptan + Naproxen

(triptan + NSAID)

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