Oral Medications for Migraine Treatment
For mild to moderate migraines, start with NSAIDs (ibuprofen, naproxen sodium, or aspirin) as first-line therapy; for moderate to severe migraines or those unresponsive to NSAIDs, use oral triptans, specifically sumatriptan 100 mg, rizatriptan, or zolmitriptan. 1, 2
First-Line Treatment Algorithm
Mild to Moderate Migraine
- NSAIDs are the initial treatment of choice with proven efficacy including aspirin, ibuprofen, naproxen sodium, or the combination of acetaminophen plus aspirin plus caffeine 1, 2
- Acetaminophen alone is ineffective and should not be used 2
- Administer early in the attack while pain is still mild for maximum effectiveness 1, 3
Moderate to Severe Migraine or NSAID Failure
- Oral triptans are recommended as first-line therapy for moderate to severe attacks or when NSAIDs provide inadequate relief 4, 1
- Sumatriptan 100 mg is the most studied oral triptan with an NNT of 4.7 for pain-free response at 2 hours and 3.5 for headache relief at 2 hours 3
- Alternative oral triptans with good evidence include rizatriptan (Maxalt), naratriptan (Amerge), and zolmitriptan 4, 1
- Rizatriptan reaches peak concentration faster (60-90 minutes) compared to most other triptans (2-3 hours), making it advantageous when rapid onset is needed 4
Dosing Specifics for Oral Sumatriptan
- Start with 50 mg or 100 mg sumatriptan at the onset of migraine symptoms 4, 5
- The 100 mg dose is significantly more effective than 50 mg for pain-free and headache relief at 2 hours 3
- The 25 mg dose has similar efficacy to 50 mg but is less preferred by patients 6
- Maximum dose is 200 mg per 24 hours 5
- In patients with mild to moderate hepatic impairment, do not exceed 50 mg as a single dose 5
Critical Contraindications to Triptans
Do not use triptans in patients with: 4, 2
- Ischemic vascular conditions or vasospastic coronary disease
- Uncontrolled hypertension
- Significant cardiovascular disease
- Basilar or hemiplegic migraine
- Concurrent use with ergotamine derivatives or within 24 hours of ergot use
Important Management Principles
Trial Multiple Triptans if Needed
- If one triptan fails, try a different triptan before abandoning this class as failure of one does not predict failure of others 4, 1
- Patients should trial a medication for 2-3 headache episodes before determining ineffectiveness 4
Prevent Medication Overuse Headache
- Limit acute treatment to no more than twice weekly to prevent medication-overuse headache 1, 2, 7
- Frequent use (more than 2 days per week) leads to increasing headache frequency and potentially daily headaches 1
- If patients require acute treatment more frequently, transition to preventive therapy 1
Optimize Timing and Combination Therapy
- Treat early during the mild pain phase for significantly better outcomes than treating established moderate or severe pain 3
- Consider combining triptans with fast-acting NSAIDs to prevent headache recurrence, which occurs in approximately 40% of patients within 24 hours 1, 3
Alternative Routes When Oral Route Inadequate
- When significant nausea or vomiting is present, use non-oral routes: subcutaneous sumatriptan (6 mg), intranasal sumatriptan, or rizatriptan orally disintegrating tablet (Maxalt MLT) 4, 2
- Subcutaneous sumatriptan reaches peak concentration in 15 minutes and is effective in 70-82% of patients 4
Common Pitfalls to Avoid
- Do not use sumatriptan during the migraine aura phase—wait until headache begins 8
- Do not combine triptans with ergotamine derivatives as this is contraindicated 4
- Avoid opioids as they have questionable efficacy, risk of dependency, and contribute to medication-overuse headache 1, 2, 7
- Do not dismiss treatment failure after a single use—efficacy should be assessed over 2-3 attacks 4