What's the Best Medicine for My Headaches?

New headache drugs are coming onto the market every six months, with many more in the research and development pipeline. People with headache have never had so many options for controlling their attacks. But which option is right for you? Is newer better, or is older safer? How do you choose?

Each medicine has a different profile of benefits, side effects and other tradeoffs, but often it isn't possible to predict which will work best for a given individual with headache. All the same, it is possible to make an informed decision about which drug or which type of drug to try first.

Several considerations can help you and your doctor select the type of medication most likely to be helpful:

• Do you have symptoms other than pain with the attack, such as nausea or vomiting, that might interfere with your ability to use oral medication (pills or capsules)?
• Are these associated symptoms severe or annoying to the point that they need to be treated too?
• Do your headaches develop gradually or are they sudden and severe, requiring a fast-acting medication?
• Do your headaches tend to come back a few hours after the first dose of your current medication?
• Do you have other medical conditions that contraindicate the use of a particular drug?
• Do you have special preferences that need to be considered (for example, a non-sedating drug that may allow you to continue to work)?

Pill, Spray, Suppository or Needle?

Medications can be administered and absorbed by a number of different routes. Drugs taken in the form of pills and capsules are absorbed through the gastrointestinal tract. Sublingual tablets that dissolve in the mouth are usually absorbed faster than medication that is swallowed. The same is true of suppositories that are absorbed through the membrane of the rectum. Nasal sprays enter the bloodstream more quickly by being absorbed through the membrane lining the nose. Self-administered injections under the skin or into muscle are still quicker acting. Drugs injected directly into the bloodstream act very rapidly but are generally used only in the doctor's office or the emergency room. Medications for headache are available using all of these routes of administration. The choice involves balancing the need for quick pain relief with other treatment considerations as well as convenience and personal preference.

Pills and Capsules. Many people find oral medicines the most convenient to take, as well as the most portable. Because they take longer to act, however, they are not the best option for people whose severe headache pain peaks rapidly, within a few minutes or a half hour. Also, nausea and vomiting during a migraine attack can seriously interfere with the effectiveness of oral medications. Oral medications are a good choice for people who have tension-type headache, migraine without nausea and vomiting, or migraine attacks that come on slowly, allowing early treatment.

Sublingual tablets or lozenges that are held under the tongue to dissolve are another approach. They are absorbed through the membrane lining the mouth and may be a little quicker to act compared to conventional tablets that must pass through the stomach and small intestine before they enter the bloodstream.

Nasal Sprays and Suppositories. Nasal sprays may be quicker to act than oral drugs and they are easier to use than injection drugs, so they are good options for people who need quick relief or who have significant nausea and vomiting with their attacks. Depending on the product, they may require a little practice for effective use, since the position of the head during administration can affect the efficacy. DHE and sumatriptan are two highly effective headache medications that are available as nasal sprays. Lidocaine nasal drops are sometimes used as a treatment for severe migraine or cluster headache. Since the development of nasal spray medications for headache, suppositories are less often used, but also provide relatively quick pain relief and are good choices for people who have nausea and vomiting with their headaches.

Self-injection. Injected drugs generally provide the most rapid pain relief. The disadvantages are discomfort, "hassle," and any embarrassment over using an injection in public. When the headaches are rapid and severe, injection drugs may offer the most effective treatment or the only effective treatment. Side effects may be more intense with injections.

Understanding Your Medication Options

Route of administration is one important consideration in selecting the medication most likely to provide good headache control. There are different classes of headache drugs, which have different mechanisms of action in providing headache relief. Within each class of drugs, the available medications vary in their profile of benefits and side effects, so a person who had a poor result to one triptan or ergot drug, for example, might still do well with another.

Ads, package inserts and published drug profiles give information not only on safety, side effect profile, and overall efficacy, but may also give the rate of headache recurrence and the speed of action. This type of information is very useful in selecting the medicine most likely to suit your specific situation. However, bear in mind that everyone is different and may respond differently to medication. Also, one headache may be different from another. You may get results that are better or worse than those reported in studies.

Simple Analgesics

Simple analgesics include the familiar over-the-counter (OTC) pain relievers such as aspirin (Bufferin, Bayer) and acetaminophen (Tylenol), as well as ibuprofen (Advil, Motrin, Nuprin), ketoprofen (Orudis), and naproxen (Naprosyn, Aleve). These last three belong to a class of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs).

There are also several OTC combination drugs that contain caffeine, which can help relieve migraine when taken in small, well-timed doses. Extra Strength Excedrin and Excedrin for Migraine combine acetaminophen and aspirin with caffeine. Aspirin-Free Excedrin contains acetaminophen plus caffeine, and Anacin combines aspirin and caffeine. It's important to remember that too much caffeine can actually cause headache. Most people with frequent headache are advised to limit their daily intake of caffeine in coffee, tea and soft drinks.

Over-the-counter analgesics are a good choice for milder migraine headaches or for tension-type headaches. If the headache does not respond to these drugs, taking multiple doses won't help and can hurt. These medications can cause stomach irritation and are contraindicated for people with ulcers.

There are also stronger prescription NSAIDs that may be used for headache. Ketorolac (Toradol) is a prescription NSAID that is given by injection and is sometimes used as an emergency room treatment for severe headache.

The Ergot Drugs

The ergot drugs are a family of migraine medications that originally derived from a fungus that grows on rye. They have been available by prescription since the 1920s. Among other effects, they interact with receptors for the brain chemical serotonin, which regulates mood, pain awareness, and blood vessel tone. Ergot drugs reduce inflammation and have powerful effects on blood vessels, causing them to constrict. This vasoconstrictive property helps relieve the throbbing pain of migraine, but it also means these drugs are contraindicated for people with high blood pressure, heart disease, or peripheral vascular disease (for example, Raynaud's disease). Alert your doctor if you experience symptoms of blood vessel constriction after taking ergotamine, such as temporary numbness or tingling sensations, muscle cramps, or cold fingers or toes.

Ergotamine tartrate is available in several different brands and formulations. Combinations containing caffeine in addition to ergotamine are available in tablets (Wigraine) and suppository (Ercaf). Ergomar is a sublingual tablet that is allowed to dissolve under the tongue for somewhat quicker results than conventional tablets. Bellergal-S combines ergotamine with belladonna and phenobarbital. Ergotamine may produce nausea as a side effect. Patients who have good headache control with an ergotamine drug may find that taking an anti-nausea drug beforehand is effective in controlling any nausea.

Dihydroergotamine (DHE) is related to ergotamine but has a less powerful effect on blood vessel constriction, making it somewhat safer to use. It has a low rate of headache recurrence compared to the triptan family of headache medicines. Common side effects such as nausea seem to be milder with DHE compared to ergotamine. DHE is available as a self-injection drug (DHE-45) and as a nasal spray under the brand name Migranal. For best results, your doctor should instruct you in the proper head position for using Migranal. Because they enter the bloodstream more rapidly than pills or tablets, both DHE-45 and Migranal are good choices for people with relatively severe, rapid-onset headaches.

The Triptans

The triptans target specific groups of serotonin receptors that are known to play a role in migraine and in other types of headache. They have similar side effects to the ergot drugs, but the side effects tend to be less severe. As with the ergot drugs, the triptans are used with caution, or not at all, in patients with uncontrolled high blood pressure, heart disease or peripheral vascular disease. Any chest pain or discomfort should be reported to your physician for evaluation. Dosing strategies can sometimes help minimize any problems with headache recurrence, which sometimes happens to people who have prolonged migraine attacks, or a second medication can be prescribed for the recurrences. Four triptans are currently available in the U.S.: sumatriptan (Imitrex), naratriptan (Amerge), zolmitriptan (Zomig), and rizatriptan (Maxalt). Sumatriptan is available in three formulations, as a tablet, a subcutaneous ("under the skin") injection, and a nasal spray. Rizatriptan can be prescribed as either a conventional tablet or a specially formulated tablet (Maxalt-MLT) that dissolves in the mouth. The dissolving tablet can be taken without water but does not provide faster headache relief than the tablet. Zolmitriptan and naratriptan are available as tablets only. At least three more triptans may become available in the near future; they are eletriptan, frovatriptan, and almotriptan.

While these drugs all act on the nervous system in similar ways, there are some differences in typical side effects, speed of action, and headache recurrence rate. A person who has an unsatisfactory response with one triptan maystill do well with another drug in this class. The triptans are usually non-sedating and are often good choices for people who need to stay active and alert during a headache attack. Some people will experience fatigue, drowsiness or dizziness so the medication should be tried at home first.

Isometheptene (Midrin)

Isometheptene is available under the brand name Midrin as a capsule that also contains acetaminophen and dichloralphenazone, a mild sedative. It is a useful treatment for migraine that is often chosen for patients who cannot tolerate ergot drugs.

Combination Analgesics

Combination analgesics contain acetaminophen or aspirin combined with a barbiturate or opioid (narcotic) drug. These drugs are potentially habit-forming and are usually prescribed in limited quantities with strict controls on refills. Since many other migraine medications are contraindicated for people with heart disease or uncontrolled high blood pressure, combination analgesics may be an important option for these patients. They can also be appropriate choices for someone who has infrequent but severe migraine attacks.

Phrenilin combines acetaminophen with butalbital, a barbiturate. Fioricet contains acetaminophen, butalbital and caffeine, while Fiorinal is aspirin, butalbital and caffeine. Both Fioricet and Fiorinal are also available with codeine as an added analgesic. These drugs are all taken by mouth. The narcotic butorphanol is available as a nasal spray under the brand name Stadol. Like all drugs in this category, its use must be limited and closely monitored to avoid the potential for overuse and dependency.

Not Just the Headache: Treating Other Symptoms

For migraine sufferers, the associated symptoms such as sensitivity to light and sound and any nausea or vomiting can often be just as disruptive to normal functioning as the headache itself. An effective headache treatment should address the associated symptoms as well as the head pain.

There are several effective drugs for migraine-related nausea and vomiting. Metoclopramide (Reglan) is an anti-nausea or anti-emetic drug that is taken orally. Promethazine (Phenergan) and prochlorperazine (Compazine) are available as oral drugs or as suppository. Prochlorperazine is effective in relieving headache in addition to nausea. Both promethazine and prochlorperazine are sedating, which may be a benefit if the migraine sufferer is home and able to rest. Metoclopramide is generally preferable for daytime or workplace use. On rare occasions ondansetron (Zofran) may be necessary. It is most often used as an intravenous injection to treat the nausea and vomiting associated with cancer chemotherapy, but is available as a tablet.

Communicating with Your Doctor

Family practice physicians, internists, neurologists and gynecologists can all be skilled in treating headache. However, doctors who do not treat a large number of headache patients may not be aware of all the options for effective treatment, or how these options should be matched to the individual's preferences and needs. They may decide to start with the most familiar or best-studied drug, figuring they can always try something else if that doesn't work out. If your doctor does not ask you about symptoms and headache characteristics that might influence the choice of medication, you should volunteer that information.

For example, depending on your situation, you might say:

"I'm so nauseous during the headache that I don't think I could keep a pill down. Are there other choices besides oral drugs?"

"The headache comes on really fast. Can you give me something that will give quicker pain relief?"

"I operate machinery at work-will this drug make me drowsy or dizzy?"

"The medication you gave me last time works, but the headache always comes back. Is there something else we could try to prevent recurrence?"

"The medicine I'm on now sometimes works and sometimes doesn't. Is there a second medication I could use for the more severe headaches that don't respond to my usual treatment?"

What's Important to You?

Remember that you are unlikely to find a 100% effective, side-effect-free treatment for all your headaches. Before you see your doctor, you might want to take some time to think about your priorities and goals in seeking treatment, so you can be clear about what is most important to you in evaluating your medication options. You may have no bothersome side effects with one drug but find that recurrence of your severe headaches is a problem. If you have prolonged, moderate-intensity headaches, speed of action may not be essential, but a drug that leaves you feeling sleepy or light-headed may be unsatisfactory. You can use the following checklist to help you evaluate your preferences for effective treatment:

Rate the following treatment preferences from 0 (not important at all) to 5 (very important). An effective headache medication should:

____ Provide quick pain relief
____ Decrease pain
____ Decrease headache recurrence
____ Decrease nausea
____ Decrease light sensitivity
____ Not cause nausea
____ Not cause drowsiness
____ Be easy to administer
____ Allow me to return to normal functioning

Prevention for Frequent or Severe Headache

The medicines discussed here are all for occasional use and are known as acute or abortive treatments for headache, since they are used to stop a headache attack in progress. If you find you are using your medications more than three times a week on average, you should see your doctor to discuss trying a daily medication to prevent or reduce headache occurrence. Or, if you have three or more severe, hard-to-treat attacks per month, preventive medication should be considered. For people who have predictable patterns to their headache attacks-for example, with menstrual migraine or seasonal cluster headache-it's often possible to control the headaches by taking preventive medications just before and during the headache-prone times.

Preventive medications for headache include beta blockers such as propranolol (Inderal) and timolol (Blocadren); divalproex (Depakote); antidepressants such as amitriptyline (Elavil/Endep) and nortriptyline (Pamelor); calcium channel blockers such as verapamil (Calan/Isoptin SR); and methysergide (Sansert), among others. Methysergide requires special prescribing and monitoring precautions to avoid rare complications. Otherwise, these drugs have an excellent safety record and are preferable to overuse of the abortive medications described in this brochure.

Avoiding Overuse

A number of analgesic drugs that act to relieve headaches when taken as directed can actually make the headaches worse if overused. In this situation, overuse of headache medication (for example, more than three or four times per week) results in a type of chronic daily headache called drug rebound headache. The headache returns as each dose of medication wears off, prompting the individual to take another dose of medication. This results in a vicious cycle of headache-pain medicine-return of headache-more pain medicine-more headache. The only treatment for drug rebound headache is stopping the medication. Unfortunately, the headache becomes worse when the medication is withdrawn and does not improve significantly for weeks or even months. Most people will see a definite improvement in their headaches, such as a return to the frequency they had before the daily headaches developed.

Many different headache medications can result in a drug rebound headache if overused either singly or in combination with similar drugs. Excessive caffeine alone can produce drug rebound headache in susceptible individuals, even if pain medicine is not being overused. Limit your consumption of caffeine-containing coffee, teas and soft drinks if you are prone to frequent headaches.

Although there are other types of chronic daily headache, drug rebound headache appears to be the most common. While you should not hesitate to take an effective headache medicine as directed, be cautious about too frequent dosing, particularly if you find you are using your medication more than three or four times a week. If you do find you are taking medication several days a week, discuss your situation with your doctor. A combination of preventive and abortive medications may be safer and more effective. Non-drug approaches, such as biofeedback, relaxation therapy, and exercise, can also be helpful in reducing both headache frequency and need for medication.

Source: American Council for Headache Education, 2000