Headache Pain Medication
For acute headache treatment, start with NSAIDs (ibuprofen 400-800 mg, naproxen 500-825 mg, or aspirin 1000 mg) or acetaminophen 1000 mg as first-line therapy, and add a triptan if NSAIDs fail or for moderate-to-severe attacks. 1, 2
First-Line Treatment Algorithm
Mild to Moderate Headache
- Begin with ibuprofen 400 mg every 4-6 hours (maximum 3200 mg/day), as this dose provides optimal efficacy for most patients 3
- Alternative first-line options include naproxen 500-825 mg or aspirin 1000 mg, all with strong evidence for efficacy 1, 2
- Acetaminophen 1000 mg is appropriate when NSAIDs are contraindicated, though it shows efficacy primarily at this higher dose rather than 500-650 mg 1, 4
Moderate to Severe Headache
- Combine a triptan with an NSAID immediately, as this combination is superior to either agent alone, with 130 more patients per 1000 achieving sustained pain relief at 48 hours 1, 2
- Specific triptan options include sumatriptan 50-100 mg, rizatriptan 10 mg (fastest oral triptan), or eletriptan 40 mg 1
- Add metoclopramide 10 mg if nausea is present, as it provides synergistic analgesia beyond antiemetic effects 1
Second-Line Options When Triptans Fail or Are Contraindicated
For Cardiovascular Disease or Triptan Contraindications
- Use CGRP antagonists (gepants) such as ubrogepant 50-100 mg or rimegepant, as these have no vasoconstrictor activity and are safe for patients with cardiovascular disease, uncontrolled hypertension, or cerebrovascular disease 1, 2
- Lasmiditan 50-200 mg is an alternative 5-HT1F agonist without vasoconstrictive properties, though patients cannot drive for 8 hours after use due to CNS effects 1, 5
If One Triptan Fails
- Try a different triptan for 2-3 headache episodes, as failure of one does not predict failure of others 1
- Consider subcutaneous sumatriptan 6 mg for rapid onset (15 minutes) with highest efficacy (59% pain-free at 2 hours) 1
Critical Medication Frequency Limits
- Strictly limit all acute headache medications to no more than 2 days per week (10 days per month) to prevent medication-overuse headache, which paradoxically increases headache frequency and can lead to daily headaches 1, 2
- The threshold for medication-overuse headache varies: ≥15 days/month for NSAIDs and ≥10 days/month for triptans 2
When to Initiate Preventive Therapy
- Start preventive therapy immediately if headaches occur ≥2 times per month with disability lasting ≥3 days, or if acute medications are needed more than twice weekly 1, 6, 2
- First-line preventive options include propranolol 80-240 mg/day, topiramate 100 mg/day, or candesartan 6, 2
- Allow 2-3 months to assess efficacy of oral preventive agents 6
Medications to Absolutely Avoid
- Never use opioids (including hydromorphone) or butalbital-containing compounds for acute headache treatment, as they have questionable efficacy, lead to dependency, cause rebound headaches, and result in loss of efficacy over time 1, 2
- Reserve opioids only for cases where all other medications cannot be used, sedation is not a concern, and abuse risk has been addressed 1
IV Treatment for Severe Headache in Urgent Care
- Administer metoclopramide 10 mg IV plus ketorolac 30 mg IV as first-line combination therapy for severe attacks requiring intravenous treatment 1
- Prochlorperazine 10 mg IV is equally effective as metoclopramide and can be substituted 1
- Avoid prednisone, as corticosteroids have limited evidence for acute headache treatment and are more appropriate for status migrainosus 1
Important Contraindications and Precautions
- Triptans are contraindicated in ischemic vascular disease, vasospastic coronary disease, uncontrolled hypertension, or significant cardiovascular disease 1
- Ketorolac should be used cautiously in renal impairment (creatinine clearance <30 mL/min), history of GI bleeding, or heart disease 1
- Valproate is strictly contraindicated in women of childbearing potential due to teratogenic effects 6, 2