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Headache Medications

Headache Drugs, Headache Medicines


About headache medications

Headache medications are drugs used to soothe discomfort that a patient may experience in the head. They may work by blocking pain, reducing inflammation or opening restricted blood vessels. However, exactly how most of these medications exert their analgesic effects still remains unclear.

Headache medications may provide the following types of relief:

Abortive therapy

Abortive therapy, where the medications provide symptomatic relief. Relieves common headache symptoms after they already have appeared. This may include pain that occurs in the head and other symptoms associated with certain types of headaches, such as nausea and vomiting that may occur with migraines. Examples of such drugs include triptans, aspirin, acetaminophen, ibuprofen and narcotic analgesics (opioids). Some are available over the counter, but others require a prescription.

Preventive therapy

Used to treat migraines, tension headaches and cluster headaches that may occur frequently. These drugs are taken regularly in hopes of preventing headache symptoms before they appear if the headaches occur on a frequent and predictable schedule. Most of these medications require a prescription.

Many medications are used to treat headaches. Some of the most common are available over the counter (without a prescription). The drugs most often used to treat common headaches include:


Another name for acetylsalicylic acid. Salicylate is a naturally occurring substance found in the bark of willow trees that was used for hundreds of years as a way to relieve pain. Aspirin was introduced to the U.S. market in 1899. It belongs to a class of medications known as nonsteroidal anti-inflammatory drugs (NSAIDs). This drug reduces the pain, inflammation, fever, redness, swelling and discomfort associated with medical disorders such as headaches, infections and arthritis. Aspirin also helps prevent blood from clotting, and has been shown to reduce the risk of heart attacks and certain forms of strokes.

Scientists are unsure exactly how aspirin works, but it may act on the hypothalamus (part of the brain that regulates body temperature and other autonomic activities) and block the generation of pain impulses. It also reduces inflammation by inhibiting prostaglandin production, and this may also provide pain relief. Prostaglandins are hormone-like substances in the body that mediate a wide range of physiological functions.


Medication used to relieve mild to moderate pain. It can also be used as a fever reducer, but it does not significantly reduce the stiffness, redness and inflammation associated with diseases such as arthritis. Acetaminophen first appeared as an over-the-counter drug in 1954. It belongs to the drug family called analgesics, and is often used as a painkiller by patients who cannot tolerate NSAIDs, such as aspirin or ibuprofen. Scientists are unsure exactly how acetaminophen works to relieve pain.


An NSAID used to relieve many types of pain, including discomfort associated with headaches, muscle aches, arthritis, menstruation and many other conditions. It is usually taken in an over-the-counter formulation but is also available by prescription.

It is unknown exactly how ibuprofen works. However, it is believed that it works by inhibiting prostaglandin production.

Other drugs also may be taken to treat symptoms of specific types of headaches. For example, certain medications are known to be effective in treating symptoms related to migraines. These include:

  • Triptans
  • Dihydroergotamine mesylate
  • Ergotamine tartrate and caffeine
  • Isometheptene, dichloralphenazone and acetaminophen
  • Butalbital compounds
  • Metoclopramide

Finally, some classes of drugs used to treat other conditions are also known to be effective in preventing headaches before they start. These include:

  • Anticonvulsants
  • Antihistamines
  • Blood pressure drugs (antihypertensives) including beta blockers and calcium channel blockers
  • Corticosteroids
  • Lithium (a preventive agent for cluster headaches)
  • Tricyclic antidepressants

In some cases, certain headache medications (e.g., aspirin, acetaminophen) may be combined with caffeine or a sedative into a single drug for headache relief. Patients are advised to always follow their physician’s instructions regarding combining medications.

Though these medications often help relieve headache symptoms, they also can worsen symptoms if taken too frequently. The most effective method of treating headaches is to use these medications in conjunction with other preventive measures, such as eating a well-balanced diet, engaging in regular exercise, participating in relaxation therapy and making other health lifestyle changes.


Conditions treated with headache medications

The International Headache Society has composed a comprehensive list of more than 150 types of headache, all of which may be treated using headache medications. According to the society’s classification of headache disorders, headaches may be categorized as primary, secondary or cranial neuralgias. Migraine, tension-type or cluster headaches are usually classed as primary headaches. According to the American Council for Headache Education, more than 90 percent of headaches are primary headaches. Primary headaches are not due to an underlying condition and are typically not life-threatening. Secondary headaches can be caused by numerous underlying conditions or injuries, such as head or neck trauma or disorders, blood vessel (vascular) disorders within the head and neck, infection, tumor and certain substances (e.g., medication, illegal drugs). Cranial neuralgias (nerve pain in the head) include central and primary facial pain and other headaches. Different types of headaches may respond to various treatment approaches. For example, tension-type headaches often respond to over-the-counter medications such as aspirin or ibuprofen, but some may need to be treated with prescription medications.

Conditions of concern with headache meds

Certain conditions may raise concerns for patients taking headache medications. Patients who have ulcers or who experience gastrointestinal upset when taking aspirin, ibuprofen or other nonsteroidal anti-inflammatory drugs (NSAIDs) for headaches should cease taking these drugs. Patients should inform their physician if they are pregnant or have been diagnosed with any of the following conditions:

  • Allergies to headache medications
  • Anemia
  • Asthma
  • Diabetes or other endocrine disorders
  • Gout
  • Heart disease
  • Hemophilia or other bleeding problems
  • High blood pressure
  • History of gastrointestinal problems
  • History of nasal polyps
  • Hodgkin’s disease
  • Kidney or liver disease

Patients who are planning to have surgery should inform their physician if they are taking headache medications regularly. Depending on the medications being used, patients may be asked to stop taking these for one week before surgery to lower the risk of excessive bleeding.

Side effects

Potential side effects of headache medications

Aspirin, ibuprofen and other nonsteroidal anti-inflammatory drugs (NSAIDs) may cause an upset stomach in some people. This effect tends to be more pronounced in people who take aspirin but may occur with any of these medications. Acetaminophen is less likely to cause upset stomach and may be a good alternative for some people.

Taking aspirin or ibuprofen with a full glass of water or milk may also help reduce stomach upset. In addition, certain medications (e.g., buffered aspirin) may be coated with an antacid designed to reduce stomach upset. However, if patients suffer from gastrointestinal ulcers all these medications with the exception of acetaminophen should generally be avoided.

Other side effects associated with certain headache medications include:

  • Allergic reaction or increased risk of asthma attack
  • Bloody or black stools
  • Constipation, diarrhea or gas
  • Dizziness
  • Drowsiness
  • Headache
  • Increased risk of bleeding and other blood problems
  • Mental confusion
  • Ringing in the ears (tinnitus) or hearing loss
  • Skin rash
  • Stomach pain, cramps and vomiting
  • Wheezing or other breathing difficulties

In 2005, the U.S. Food and Drug Administration (FDA) announced that it was asking manufacturers of NSAIDs to include new warnings on their labeling about certain potential health dangers associated with these medications, such as an increased risk of cardiovascular events. Patients concerned about these risks should consult their physician about the risks and benefits of taking NSAIDs.

People who take too much of a medication may find that doing so worsens the severity or frequency of headaches. These are known as rebound headaches. For this reason, it is critical that patients take these medications exactly as prescribed by a physician.


Drug or other interactions with headache meds

Patients should consult their physicians before taking any additional prescriptions, over-the-counter medications, nutritional supplements or herbal medications.

The U.S. Food and Drug Administration (FDA) in 2006 warned that a life-threatening condition called serotonin syndrome may result when triptans are used with certain antidepressants. The condition involves excessive amounts of the brain chemical serotonin. However, research indicates that this very rarely occurs.

Other drugs that may interact poorly with headache medications include:

  • Antacids
  • Anticoagulants
  • Anticonvulsants
  • Blood pressure medications (antihypertensives), including beta blockers and diuretics
  • Corticosteroids
  • Medications for gout or other forms of arthritis
  • Medications for diabetes
  • Acetazolamide
  • Cyclosporine
  • Digoxin
  • Lithium
  • Methotrexate (an antimetabolite)
  • Nizatidine
  • Phenothiazine
  • Probenecid

Patients should not combine the use of various headache medications. Consumption of alcohol – even in moderate amounts – while using certain headache medications can substantially increase the risk of liver damage, bleeding from gastrointestinal ulcers and damage to the brain. Alcohol use activates a process that turns acetaminophen into chemicals that cause liver damage. Use of caffeine may increase the effect of some headache medications.


Symptoms of headache drug overdose

Symptoms of overdose can be similar to the medication’s side effects, but are usually more severe. Overdose of headache medications can lead to toxicity and even death. Patients exhibiting any of these symptoms should contact their physicians immediately:

  • Severe headache
  • Seizures
  • Nausea
  • High fever
  • Gastrointestinal discomfort (e.g., stomach pain, diarrhea, vomiting)
  • Delirium
  • Incoherence and confusion
  • Drowsiness
  • Blurred vision
  • Decreased urine output
  • Swelling of the feet, ankles and legs
  • Irregular heartbeat
  • Jaundice (yellow discoloration of the eyes and skin)
  • Rapid breathing
  • Ringing in the ears (tinnitus)
  • Skin eruptions
  • Sweating
  • Bluish discoloration of the skin (cyanosis)
  • Unsteadiness throughout the body
How to use

Pregnancy issues with headache medications

Women who are pregnant or nursing are advised to be cautious in their use of headache medications. For example, studies have indicated that aspirin may cause birth defects in humans. As a result, it is recommended that pregnant women not use aspirin. Aspirin also passes into breast milk and should not be taken by women who are breastfeeding unless recommended by a physician.

Studies on whether or not ibuprofen and acetaminophen cause birth defects in humans have not been performed. However, it is possible that ibuprofen may cause undesirable effects on the heart or blood flow of the fetus when taken by the mother during the last few months of pregnancy. To date, there are no indications linking the use of acetaminophen during pregnancy with birth defects. Nonetheless, pregnant women should take ibuprofen or acetaminophen only in close consultation with a physician.

It is not known whether ibuprofen passes into breast milk. Acetaminophen does pass into breast milk, but only in low levels that do not appear to hurt infants of mothers who breastfeed. Breastfeeding mothers are urged to consult a physician before using these headache medications.

In addition, other medications that may be used to treat headaches may be unsuitable for women who are pregnant or nursing. For example, tricyclic antidepressants have been linked with muscle spasms and heart, breathing and urinary problems in newborns whose mothers took the drugs immediately prior to the child’s birth. Also, the overuse of some medications while pregnant, especially opioids, may lead to dependency in newborns.

In general, women who are pregnant or breastfeeding should consult their physician before taking any over-the-counter or prescription headache medication.

Child use issues

Parents are urged not to give headache medications to their children without first consulting a physician. Dosage levels generally are lower for children than adults, with the proper dosage level typically based on a child’s weight rather than age.

Infants and children should not take aspirin. Use of aspirin in children has been associated with Reye’s syndrome, a rare but extremely serious condition that affects all organs of the body and can be fatal. The risk of Reye’s syndrome is increased in children who take aspirin when they have a viral infection, such as the flu or chickenpox. Symptoms include:

  • Vomiting
  • Lethargy
  • Behavioral changes, including belligerence

As a result of this risk, experts usually suggest that aspirin not be used by anyone under the age of 18, especially if they have a viral illness.

Ibuprofen should be given only to children who are older than 6 months of age, and should not be given to children under age 12 without close supervision of a physician. It should not be given to children who are dehydrated or who are vomiting continuously. Parents are urged to consult with their child’s physician before giving ibuprofen to children diagnosed with kidney disease, asthma, ulcers or other chronic illnesses.

Acetaminophen can be safely used to treat pain and fever in children. However, special attention must be paid to making sure children get the appropriate dosage of the drug. Acetaminophen overdose is among the most common causes of drug-related deaths in children and adolescents.

Other headache medications may also involve special considerations for children. For example, corticosteroids may make children more susceptible to viral infections and can delay growth if taken over a long period of time.

Elderly use issues

Patients older than age 60 may be more susceptible to the toxic effects of headache medications. For example, aspirin, ibuprofen and the other nonsteroidal anti-inflammatory drugs (NSAIDs) can affect renal prostaglandins (hormone-like substances in the body that mediate a wide range of physiological functions), causing fluid retention and edema (excessive watery fluid in cells, tissues or serous cavities). This can be a significant medical problem for older people.

Older people who mix NSAIDs with alcohol consumption also are at high risk for episodes of gastric bleeding. As a result of these risks, older patients should use NSAIDs carefully and in close consultation with a physician.

Elderly patients are more likely to have increased sensitivity to the effects of acetaminophen. In addition, use of acetaminophen may be contraindicated in patients of any age who have liver disease or are taking drugs that are metabolized through the liver. Older patients should consult closely with a physician before taking acetaminophen.

Questions for your doctor

Patients may wish to ask their doctor the following questions about headache medications:
  1. Which headache medications are safe for me to use?
  2. What type of headache medication is likely to be effective in treating my headache?
  3. Will I need a prescription dosage to treat more substantial pain?
  4. What should I do if I miss a dose or take too much?
  5. What side effects might I experience from taking my headache medication?
  6. At what point should I inform you of side effects?
  7. Do I have any conditions that rule out use of certain headache medications?
  8. Can any of my other medications interact with my headache medication?
  9. What are my other options if my headache medication does not relieve my condition?
  10. Are there other steps I can take (e.g., dietary or lifestyle changes) to reduce my risk of experiencing headaches?

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