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Headache Treatments - Details

Beta-Blockers

  • The drugs belonging to the class of beta blockers are probably the most widely used in preventive treatment. Beta blockers combine a high level of effectiveness with a low level of side-effects. They are safe in long term use.
  • Most patients who take these drugs experience no side-effects. The people who do have side-effects usually say that they are minimal.
  • The beta blockers in general should be avoided in persons with asthma, diabetes and some heart and circulation conditions. They have to be used cautiously in conjunction with some medications, diet pills and eye drops. Many allergists do not like to do allergy testing or give allergy shots to patients while on this medication.
  • While these drugs are often used to treat high blood pressure, they do not significantly lower blood pressure if the blood pressure is normal before the start of treatment.
  • The commonly used beta blockers for headaches are Propranol [Inderal, Inderal[LA] Nadolol [Corgard] and Atenolol [Tenormin]. Nadolol and Atenolol, can be taken once per day and therefore are more convenient than some of the others.
  • Two of the drugs (Metoprolol [Lopressor] and Atenolol) are said to be "selective". This means they might be slightly safer in patients with asthma or some heart conditions.


Calcium Channel Blockers

  • Calcium channel blockers may be used in certain cases.  In general, we have found them to be somewhat less effective than the alternatives. 
  • These medications may have a special place in treating patients who cannot take beta blockers or have not responded to them.
  • Refer to the table for some of the common trade names.
  • Verapamil (Isoptin) has a particular tendency to cause constipation.  Patients with heart conditions, taking beta blockers or blood pressure lowering drugs might consider alternatives.  Paradoxically, some drugs in this class can occasionally induce headaches.


Feverfew

  • Feverfew comes from a plant with the scientific name of Tanacetum parthenium or Chyrsanthemum parthenium.
  • Studies suggest that feverfew can reduce the intensity, frequency of headaches and associated vomiting. 
  • There are few side effects. The occasional patient, especially someone taking whole leaves, has developed Canker sores. These are tiny painful spots inside the mouth, which heal by themselves and cannot be passed on.
  • Feverfew is probably less effective than some of the other available anti-headache treatments but it is so mild that it can be used as the first medication.
  • Feverfew comes in many different forms. The different brands can vary dramatically in terms of the amount of active ingredients that they contain. The best known brand is Tanacet-125.


MAOI (Monoamine Oxidase Inhibitors)

  • The monoamine oxidase inhibitors or MAOI's are used only occasionally for headache treatment. Some doctors find them useful for the most resistant headaches.
  • The possibility of serious side-effects limits their use. Taking one of the MAO inhibitors with the wrong sorts of food, drink or medication can cause a crisis in which the blood pressure rises to dangerous levels. Patients who take these drugs must be very careful to follow the diets given to them. Careful consultation with your doctor and pharmacist is crucial if you are given a MAOI. 


Riboflavin

  • Riboflavin is also known as vitamin B2. This is not the same as vitamin B12 or other members of the B-series.
  • High dose riboflavin is as effective as the previous standard preventive treatments (i.e. beta blockers or the calcium channel blockers) but appears to have few serious side-effects or interactions with other medications.
  • The full effect is slow to develop and may only be reached after three months of daily use.  As with most preventive medications, the benefits are not noticeable right away.Many patients make the mistake of stopping preventive medicines too early.
  • Riboflavin and the other drugs are preventives, not cures. Once patients stop taking the medicine, headaches may return to the same level had the medication never been used.
  • Riboflavin does turn the urine very yellow. This is not really a problem but the patients need to know that this will happen before they take the first dose.


Serotonin Agonists

  • Prescription drugs from the class of Serotonin receptor agonists such Sumatriptan (Imitrex) and its chemical relatives Naratriptan (Amerge), Zolmitriptan (Zomig) and Rizatriptan (Maxalt) and Dihydroergotamine (DHE) (Migranal) are specific for migraine-related headaches. They would not, for example, relieve pain from other conditions.
  • Ergotamine (Cafergot and others) is an older drug in this class. It can work well for some people.
  • Nausea and vomiting are common with ergotamine and limit its usefulness. Serious side effects are rare but can occur with excessive use. Regular use of ergotamine is felt to be associated with rebound headaches and even dependency. 
  • Ergotamine cannot be used in pregnancy or in persons with circulation problems.   
  • Combining ergotamine with sumatriptan naratriptan, zolmitriptan and rizatriptan:
      • Patients with circulation problems have to avoid sumatriptan and its relatives (know as “triptans”). These drugs (sumatriptan naratriptan, zolmitriptan, and rizatriptan) should not be combined with any ergotamine containing preparation. Speak to your doctor or pharmacist for details.   All of these drugs, while better than earlier medications, still leave something to be desired in terms of effectiveness.
      • Some dizziness, prickling, neck pain, and pressure in the chest are common. Nausea and vomiting are other potential side-effects. 
      • Migranal nasal spray has not been effective in our hands and is no longer used much. It should not be used during pregnancy or breast feeding. It should not come as a surprise that a nasal spray could cause irritation to the nose. Nausea and vomiting can also occur.
      • Unlike most nasal sprays, you should not tilt your head back or sniff the medicine but just spray it into the nose. After the vial is opened, you have eight hours to finish the medicine. Then you must throw any remainder away.


Serotonin Antagonists

  • Although classed together the serotonin antagonists are really quite different drugs. 
  • They are not used as much as they used to be. 


Tricyclics and Related Compounds

  • The tricyclic agents and their relatives work better for headaches, which are continuous or almost continuous. The Beta blockers, in contrast, are better for the headaches which are intermittent. That is, when there are definite headache-free periods between attacks.
  • Most of these drugs are marketed for the treatment of depression. They are therefore, sometimes, called anti-depressants. It has been shown by several studies that their use in headache is not necessarily related to an anti-depressant effect. They do not elevate mood in persons who are not depressed. Thus, they are not simple "uppers".
  • The tricyclics act on specific brain chemicals and alter the chemical balance of the brain. The same chemical imbalance in one area of the brain may cause depression whereas other brain areas involved in pain control may influence headache. The brain uses the same chemicals in different areas for different purposes. 
  • Furthermore the newer "antidepressants" agents belonging to the class of selective serotonin reuptake inhibitors (SSRI's) are not very effective for headaches. The best know of this class of drugs is fluoxetine, sold under the brand name Prozac. 
  • The most common side-effects of tricyclics are dry mouth and perhaps some constipation. A small dose of Milk of Magnesia, taken on a daily basis will alleviate the constipation. This dose can be minimal. Patients have to find their own ideal dose.
  • Occasionally there can be some dizziness on first standing up. With some of the drugs, such as amitriptyline (Elavil), sedation and drowsiness are more common than with some of the others, such as nortriptyline (Aventyl) or desipramine (Norpramin). Weight gain is a potential problem and must be guarded against.
  • Although it is quite rare, a tricyclic can impair the ability to pass urine. If this unusual side-effect develops, the medication must be stopped immediately.
  • It is important to begin these drugs with a low dose. With slow, gradual dose increases, the level of side-effects is less.
  • Interaction with other drugs is a possibility. Again, patients must provide their doctor and their pharmacist with a full medication list. Overdoses of tricyclics can be serious. These medications should be kept away from children and anyone who might take them by mistake.


Other Medications

  • Divalproex sodium is sold in Canada under the trade name Epival. It is mainly used to treat epilepsy. Side-effects can be troublesome with valproate to the point where a fraction of the patients have to quit. Birth defects may result in patients who take this drug during pregnancy. For this reason it must be totally avoided when pregnant or at least, used with birth control. Folate, a vitamin can be taken in conjunction with valproate in case an unexpected pregnancy occurs.

    Other "epilepsy" medications can help people with migraine. Neurontin in higher         doses that is typically recommended for epilepsy has been used with some                 success.

  • Vigabatrin (Sabril) and Topiramate (Topamax), both epilepsy drugs, might help people with headache. Side-effects are major concerns with these two drugs. Vigabatrin can impair vision in some patients and requires special monitoring. Over a quarter of the patients given Topiramate, find that it is too difficult for them to take, because of impaired thinking processes, memory problems, tiredness, and the like. On occasion, Topiramate can cause kidney stones. These drugs might be tried if other better alternatives have failed.
  • Certain drugs used in asthma known as leukotriene antagonists are being evaluated in headache patients.
  • Dotarizine, which has calcium channel blocking properties and effects certain brain chemicals, is being investigated for treating headache.
  • Low dose histamine injected under the skin is another possibly effective treatment.
  • Magnesium is a vital element that plays an important role in the occurrence of migraines. Migraine patients may have deficient magnesium levels.
  • Some clinical trials have shown improvement with oral magnesium but not all. Magnesium seems to work better if the blood levels of magnesium are less. Several weeks of continuous use are required before the medicine takes full effect. Magnesium may cause diarrhea. 


Other Treatments

Special types of strong muscle relaxants, derived from certain bacterial products and known under the trade names Botox and Myobloc, have been used to treat headaches. These medicines have to be injected into the head and neck muscles by a doctor. This treatment is still being evaluated but preliminary results are very promising.

Injection of local anesthetics into the scalp area, or into the neck ("nerve blocks"), alone or in combination with anti-inflammatory steroids are used by some doctors. We have not been impressed with the effectiveness of these treatments. Improvements do not appear to be long-lasting in most of our patients.