Medication Summary
There are a variety of medications available to treat the pain of a headache, including pain relievers and combination medications. Patients should be advised to avoid repeated use of OTC pain relievers as these can cause medication overuse headaches. Opioids nor barbituates should be used in TTH when better options (e.g., simple analgesics and combintaion analgesics containing caffeine) are available. [17]
Barbiturates may be used when all other treatment options have failed.
Nonsteroidal anti-inflammatory drugs (NSAIDs)
Class Summary
These agents may alleviate headache pain by inhibiting prostaglandin synthesis, reducing serotonin release, and blocking platelet aggregation. Although the effects of NSAIDs in the treatment of headache pain tend to be patient specific, ibuprofen is usually the DOC for initial therapy. Other options include naproxen, ketoprofen, and ketorolac.
Ibuprofen (Ibuprin, Advil, Motrin)
Usually DOC for treatment of mild to moderately severe headache, if no contraindications.
Naproxen (Naprosyn, Naprelan)
For relief of mild to moderately severe pain. Inhibits inflammatory reactions and pain by decreasing enzyme cyclooxygenase activity, thus inhibiting prostaglandin synthesis.
Ketoprofen (Oruvail, Orudis, Actron)
Description For relief of mild to moderately severe pain and inflammation. Small dosages initially indicated in small and elderly patients and in those with renal or liver disease. Doses over 75 mg do not increase therapeutic effects. Administer high doses with caution and closely observe patient for response.
Ketorolac (Toradol)
Inhibits prostaglandin synthesis by decreasing activity of enzyme cyclooxygenase, which results in decreased formation of prostaglandin precursors. PO form offers no advantage over other less expensive PO NSAIDs.
Indomethacin (Indocin, Indochron E-R)
Absorbed rapidly; metabolism occurs in liver by demethylation, deacetylation, and glucuronide conjugation. Useful in diagnosis as it helps other headache syndromes (eg, chronic paroxysmal hemicrania).
Acetylsalicylic acids
Class Summary
These agents alleviate headache, possibly by inhibiting prostaglandin synthesis.
Aspirin (Anacin, Ascriptin, Bayer Aspirin, Bufferin)
Treats mild to moderately severe pain. Inhibits prostaglandin synthesis, which prevents formation of platelet-aggregating thromboxane A2.
Barbiturates
Class Summary
These agents are used in combination with aspirin and acetaminophen for pain relief and to induce sleep. Caffeine is used to increase its GI absorption. However, butalbital is associated with rebound headaches. Increasing use of these combination preparations may fail to provide pain relief and worsen headache symptoms.
Butalbital, aspirin, caffeine (Fiorinal)
Drug combination used to relieve tension headaches. Barbiturate component has generalized depressant effect on CNS.
Acetaminophen, butalbital, and caffeine (Fioricet)
Drug combination used to relieve tension headaches. Barbiturate component has generalized depressant effect on CNS.
Analgesics
Class Summary
Patients with infrequent headaches can be treated with simple analgesics initially.
Acetaminophen (Tylenol, Panadol, Aspirin Free Anacin)
DOC for pain in patients with documented hypersensitivity to aspirin or NSAIDs or upper GI disease or taking oral anticoagulants.
Acetaminophen with codeine (Tylenol #3)
Indicated for treatment of mild to moderately severe headache.
Acetaminophen and oxycodone (Percocet)
Indicated for relief of moderately severe to severe pain. DOC for aspirin-hypersensitive patients.
Analgesic/antiemetic or sedatives
Class Summary
These agents are useful in aborting headache and treating emesis that results from acute pain.
Promethazine (Phenergan)
Antidopaminergic agent effective in treating emesis. Blocks postsynaptic mesolimbic dopaminergic receptors in brain and reduces stimuli to brainstem reticular system.
Prochlorperazine (Compazine)
May relieve nausea and vomiting by blocking postsynaptic mesolimbic dopamine-receptors, through anticholinergic effects, and depressing reticular activating system. In addition to antiemetic effects, has advantage of augmenting hypoxic ventilatory response, acting as respiratory stimulant at high altitude.
Metoclopramide (Reglan) can be used as an alternative to prochlorperazine. Studies show prochlorperazine is better.
Metoclopramide (Reglan)
Dopamine antagonist that stimulates acetylcholine release in the myenteric plexus. Acts centrally on chemoreceptor triggers in the floor of the fourth ventricle, which provides important antiemetic activity.
Ergot alkaloids and derivatives
Class Summary
These are direct vasoconstrictors of smooth muscle in cranial blood vessels. Their activity depends on the CNS vascular tone at the time of administration.
Ergotamine tartrate (Cafergot, Cafatine, Cafetrate)
Alpha-adrenergic and serotonin antagonist. Causes constriction of peripheral and cranial blood vessels.
Dihydroergotamine (D.H.E. 45, Migranal Nasal Spray)
Alpha-adrenergic blocking agent with direct stimulating effect on smooth muscle of peripheral and cranial blood vessels; depresses central vasomotor centers. Mechanism of action is similar to ergotamine; nonselective 5HT1 agonist with wide spectrum of receptor affinities outside 5HT1 system; also binds to dopamine. Thus, has alpha-adrenergic antagonist and serotonin antagonist effect. Indicated to abort or prevent vascular headache when rapid control needed or when other routes of administration not feasible.
Available in IV or intranasal preparations, tends to cause less arterial vasoconstriction than ergotamine tartrate.
