Drugs for migraine

Question 1

DRUGS FOR MILD TO MODERATE ATTACKS

Answer 1

• Acetaminophen & NSAIDs: For mild to moderate attacks not associated with vomiting or severe nausea, acetaminophen and NSAIDs are first choice.
• TRIPTANS
• ERGOT ALKALOIDS

Question 2

TRIPTANS

Answer 2

• Triptans are the DOC for moderate-to-severe migraine.
• Triptans are selective agonists at 5-HT1D and 5-HT1B receptors
• Combination of sumatriptan and naproxen provides better pain relief than either drug alone.
• SC sumatriptan is the fastest-acting and most effective triptan formulation.

Adverse

• Tingling, flushing, dizziness, fatigue.
• Chest tightness.
• Rare: Angina, MI, arrhythmia, stroke, and death.
• Contraindicated in coronary, cerebrovascular or other arterial disease, or uncontrolled hypertension.

Question 3

Ergotamine & Dihydroergotamine

Answer 3

• ERGOT ALKALOIDS
• Ergotamine acts as an agonist at α-adrenoceptors, 5-HT and D2 receptors
• The agonist actions of ergot alkaloids at 5-HT1B/1D receptors likely mediate their anti-migraine effects.

Adverse

• Nausea and vomiting. Can be prevented with an antiemetic such as metoclopramide.
• Serious adverse effects: vascular occlusion and gangrene. Rare. Usually associated with overdosage.
• Dihydroergotamine is a weaker vasoconstrictor than ergotamine and causes fewer AE.
• Ergots are contraindicated in arterial disease or uncontrolled hypertension.

Question 4

Drugs for prevention of migraine

Answer 4

FIRST LINE AGENTS

• Beta Blockers
• Valproate
• Topiramate

SECOND OR THIRD LINE AGENTS

• Tricyclic Antidepressants
• SNRIs
• Calcium Channel Blockers
• Gabapentin
• ACEIs or ARBs
• Botulinum Toxin: Pericranial injections
• NSAIDs

Question 5

VALPROATE

Answer 5

• Indicated for bipolar disorder, epilepsy, and migraine prophylaxis; also effective for neuropathic pain.
• Valproate inhibits voltage gated Na+ channels and T-type Ca2+ channels.
• Adverse effects: GI side effects. Thrombocytopenia. Rarely hepatotoxicity. Teratogenic.

Question 6

TOPIRAMATE

Answer 6

• Indicated for epilepsy and migraine prophylaxis.
• Inhibits voltage-gated Na+ channels.GABAA receptor agonist and glutamate receptor antagonist.

Adverse

• Somnolence, fatigue, cognitive slowing, nervousness, confusion.
• Acute myopia, glaucoma.
• Hyperthermia,
• renal stones.
• Teratogenic.

Question 7

Amitriptyline
Nortriptyline
Imipramine

Answer 7

• TCAs inhibit norepinephrine and serotonin reuptake.
• Adverse effects: Sedation, dry mouth, weight gain.

Question 8

Venlafaxine

Answer 8

• SNRIs
• Adverse effects: nausea, constipation, insomnia, headaches, sexual dysfunction.

Question 9

Verapamil

Answer 9

• CCBs are used for prevention of migraine, but evidence for their effectiveness is weak.
• Verapamil is the CCB with most evidence of efficacy.

Question 10

GABAPENTIN

Answer 10

• decreases glutamate release by blocking presynaptic voltage-gated Ca2+ channels.
• Adverse effects: sleepiness, dizziness, fatigue.