Medication for Headaches: What Works?

Medication for headaches can be an important part of a headache treatment plan. Medications for headaches include various nonprescription and prescription drugs. In general, medications for headaches fall into two types: drugs used to treat acute headache, and drugs used to prevent attacks in people with chronic headache syndromes. For people who experience chronic or severe headache, medications are an essential part of headache treatment.

Medications Used to Treat Acute Headache

When a person feels the pain of a headache, no matter how severe, the headache is considered acute. Most people can find headache relief in over the counter headache medications. However, during an acute headache, people with severe, chronic headache may need to turn to their “headache meds.” People with severe headaches should consult their doctors about using one of the many prescription drugs used for headache treatment.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

Nonsteroidal anti-inflammatory drugs (NSAIDs), which are available in both prescription and OTC forms, are the first line of defense against headache pain. Many patients will initially self-medicate with one of the following OTC formulations:

  • Aspirin (the most common)
  • Ibuprofen (Advil, Motrin)
  • Naproxen sodium (Aleve)

Prescription formulations such as the following should only be used under the supervision of a doctor:

  • Indomethacin (Indocin)
  • Piroxicam (Feldene)
  • Sulindac (Clinoril)
  • Tolmetin sodium (Tolectin)
  • Meclofenamate sodium (Meclomen)
  • Ketorolac (Acular, Toradol)
  • Naproxen (Naprosyn) in higher doses; Naproxen sodium (Naprelan, Anaprox)
  • Ibuprofen in higher doses
Need to Know

Although over-the counter medications can be purchased without a prescription, they are still potent drugs. They should be used according to the package directions, and patients need to be alert to side effects. In addition, prolonged or frequent use can lead to dependency (which can, in turn, lead to medication overuse headaches). People who take painkillers of any sort more often than two days per week should consult a doctor for further advice about preventing headaches.

NSAIDs, as a group, share certain common side effects. They may cause stomach upset, nausea, and vomiting. These effects may be avoided by taking the drugs with food or milk. Long-term and high-dose use can damage the kidneys or stomach lining and may contribute to the development of ulcers.

NSAIDs also have a “blood thinning” effect, so they should not be combined with other anticoagulants (such as warfarin [Coumadin] or other NSAIDs). If you have asthma or heart disease, consult your doctor or pharmacist before taking any NSAIDs, whether OTC or prescription. Individual formulations may have additional, specific side effects; read labels and follow directions carefully.

Acetaminophen (Tylenol, Anacin-3, Panadal, Tempra), a non-narcotic analgesic, is a reasonable alternative to the OTC drugs noted above when existing stomach distress, ulcers, or allergic reactions prohibit the use of NSAIDs. Pregnant women may be able to take acetaminophen, but they should consult their physicians first. Side effects are rare when the drug is used according to instructions, but overuse or prolonged use can lead to liver damage and other toxic effects.


Triptan drugs are prescription drugs used to treat moderate to severe migraine pain. Among migraine medications, triptans are preferred for moderate to severe pain. Injectable and inhaled forms of triptan drugs are also accepted medications for cluster headaches. Because these forms of the drug are absorbed quickly and begin to act almost immediately, they are sometimes used to treat cluster headaches.

Triptans act by increasing levels of the neurotransmitter serotonin in the brain. Serotonin lowers the pain threshold, making it easier for you to handle pain, and causes blood vessels to constrict, lessening the pain signals in the head.

Seven triptans are available for treatment of acute migraine. These are:

  • Sumatription (Imitrex, Imigran)
  • Zolmitriptan (Zomig, Zomig-ZMT)
  • Naratripton (Amerge, Naramig)
  • Rizatriptan (Maxalt, Maxalt-MLT)
  • Almotriptan (Axert)
  • Frovatriptan (Frova
  • Eletriptan (Relpax)

Ergot Derivatives

Ergot derivative drugs are sometimes used to help control migraine and cluster headache pain when triptans fail. They work by binding to serotonin receptors on nerve cells, thus lessening the transmission of pain signals along nerve fibers. They also act on some other receptors, most likely on those for dopamine and noradrenalin. Ergo derivatives include:

  • Ergotamine tartrate (Cafergot)
  • Dihydroergotamine (D.H.E. 45 Injection, Migranal Nasal Spray)
  • Acetaminophen-isometheptene-dichloralphenazone (Midrin)

Narcotic and Combination Analgesics (Pain Relievers)

Individuals with more severe headaches may need to use narcotic pain medications, which require a doctor’s prescription. Narcotic pain medications work by interfering with pain receptors on nerves, thus interrupting the pain signal.

To make them more effective, narcotic pain medications are often combined with other drugs. Many combination analgesic “cocktails” consist of an analgesic, caffeine, and a narcotic. Caffeine acts as an adjuvant, helping the pain-killing drugs to work more effectively, and it helps to constrict blood vessels. These combination analgesics help lessen any kind of pain.

Examples of these combination drugs include

  • Acetaminophen with codeine (Tylenol with Codeine)
  • Butalbital-acetaminophen-caffeine (Fioricet)
  • Butalbital-aspirin-caffeine (Fiorinal),

As with NSAIDs, overuse of narcotic analgesics for chronic headaches can lead to dependency and medication overuse (previously called “rebound”) headaches. Other side effects that may occur with narcotic analgesics include light-headedness, sedation, dizziness, shortness of breath, nausea, and vomiting. Abdominal pain, constipation, depression, and itchy skin are less common side effects.

Need To Know

Caffeine is a drug familiar to headache sufferers for two reasons: It can be a cause of pain, and it can help to relieve it. In small amounts, caffeine acts to constrict blood vessels. It is often added to analgesic drugs to make them more effective. A small amount of caffeine can actually reduce the dose of a pain medication needed to relieve pain. When caffeine is a regular component of the diet, however, such as for habitual coffee- or soda-drinkers, tolerance and dependence on this stimulant drug can lead to medication overuse and/or withdrawal headache.

What Medications are Used to Prevent Headaches?

Medications may be used to help prevent headaches in people with chronic headache syndromes such as migraine or cluster. Indeed, many of the medications used to prevent migraines are also used to prevent cluster headaches. Preventing migraines or cluster headaches requires a comprehensive approach, and medications can be an important part of managing chronic headaches of any type.

Medications commonly used to prevent migraines and cluster headache include oral steroids, antidepressants, Botox, anticonvulsants, beta blockers, calcium channel blockers, and lithium. Less commonly, Methysergide maleate (Sansert) may be prescribed.

Oral Steroids

Oral steroids (corticosteroids) are generally a form of prednisolone. These compounds can be effective in relieving pain caused by inflammation. Steroids should only be used under a doctor’s supervision; the appropriate dose is often highly individual.

Common side effects associated with oral steroids include diarrhea or constipation; headache; increased or decreased appetite; increased sweating; nervousness, restlessness, or difficulty sleeping; upset stomach; and unusual or increased growth of hair on the face or body.


Antidepressants effectively help prevent several types of severe headaches. Mild tranquilizers are also prescribed occasionally, but they tend to be highly addictive and should only be used on a short-term basis.

Side effects vary widely according to individual drugs, but some of the more common effects related to antidepressant medications include: changes in sleep patterns; dry mouth; changes in vision; constipation; anxiety; nausea; and worsening of existing heart disease. Patients should be alert to any and all changes that may result from a new or changed antidepressant treatment.


Botox (onabotulinumtoxinA), known widely for its use in cosmetic procedures, is sometimes used as a treatment for chronic migraine and other severe headache types. Botox is a formulation that contains botulinum toxin, a neuro-muscular poison that causes temporary paralysis. It has been tested and approved for a number of neuro-muscular conditions, and is considered to be safe in the small doses required for therapy.

Botox was approved by the FDA in October 2010 to help people with chronic migraine prevent future attacks. To effectively avoid or dull future attacks, Botox should be given approximately every 12 weeks as multiple injections around the head and neck. However, the drug has not been shown to work for the treatment of episodic migraine headaches that occur 14 days or fewer per month, or for other forms of headache.

The most common adverse reactions reported by patients being treated with Botox for chronic migraine were neck pain and headache. The most common side effect of Botox treatments in other contexts is muscle weakness in the treated area, but this is generally temporary. Rarely, flu-like symptoms have been reported.

Other preventive medications

Other medications may be prescribed to help prevent repeated attacks for specific types of headaches. These include:

  • Anticonvulsants. These drugs, originally developed to treat people with seizure disorders, may help to lessen pain and increase levels of certain neurotransmitters in the brain. Specific anticonvulsants used to prevent migraine and cluster headaches are valproic acid, gabapentin, phenobarbital, and topiramate.
  • Beta blockers. Generally used to treat high blood pressure and irregular heart rhythms, beta blockers are also helpful for some people in controlling migraines. Propanolol, in particular, is approved by the FDA for prevention of migraine. Migraine frequency usually decreases within four to six weeks of starting treatment. Doctors do not know exactly how these drugs help prevent migraines. Some experts speculate that beta blockers help to stabilize blood vessels and prevent them from widening too much. Beta blockers may also help prevent migraine by reducing anxiety and excitability of the nervous system, as well as balancing levels of the neurotransmitter serotonin , People with asthma or other respiratory diseases should not use beta blockers. Alert your doctor if you receive allergy shots. Slow heart rate and low blood pressure are common side effects. Beta blockers should not be stopped abruptly, as this can lead to a dangerous rise in heart rate.
  • Calcium channel blockers. These medications are used to treat heart and blood vessel problems such as high blood pressure. They help to control blood pressure by altering the movement of calcium ions into the muscle cells that control blood vessels. By controlling the narrowing and widening of blood vessels, these drugs can help to prevent migraine and cluster headaches. Calcium channel blockers have not been approved by the FDA for prevention of migraine. However, some research suggests that the calcium channel blocker Verapimil may help prevent both migraine and cluster headache. High doses of Verapimil may be needed to treat cluster headache cycles. People with asthma and other respiratory diseases can use calcium channel blockers. Side effects of these drugs include low blood pressure and constipation.
  • Lithium. Lithium is very helpful in prevention of chronic cluster headaches and sometimes episodic cluster. It is given in small doses, one to three 300 mg. tablets per day, for cluster headache. Although lithium is usually well tolerated in low doses, side effects may include drowsinesss, mood swings, nausea, tremor, and diarrhea may occur. People taking lithium need to have blood tests done regularly.
  • Methysergide maleate (Sansert) may be prescribed for people with severe migraine or cluster headache. The drug acts by counteracting blood vessel constriction. Methysergide maleate has several side effects, including nausea, leg cramps, dizziness, and a feeling of heat in the head; it can lead to fibrosis when used for extended periods. Pregnant women and people with stomach ulcers, heart and blood vessel disease, or kidney disease should not use methysergide maleate. However, used judiciously, the drug can be effective in preventing both migraine and episodic cluster headaches.

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