100 Migraine drugs, A to Z: butalbital

Butalbital, a short-acting barbiturate, is one of the three ingredients in headache drugs such as Fioricet, Fiorinal, Esgic and their generic equivalents. Fiorinal and Fioricet derive their name from the Montefiore Headache Clinic, where they were developed over 60 years ago. In those days extensive clinical trials were not required by the FDA and they were approved without much testing. The approval was and still is only for the treatment of tension-type headaches. They have never been shown to be effective for migraines, although this is what they are mostly used for. Fioricet and Esgic contain butalbital, caffeine, and acetaminophen, while in Fiorinal acetaminophen is replaced with aspirin.

Neurologists have a strong dislike of this drug, although general practitioners tend to like it because they are very familiar with it. The dislike comes from the fact that butalbital is addictive and caffeine can make headaches worse. I’ve seen patients who openly admitted that they often take Fiorinal to relieve anxiety and many become physically dependent and addicted to it. My most memorable patient was one who took 20 to 30 tablets every day. I had to hospitalize her for detoxification. In patients who take more than 5-6 tablets a day sudden discontinuation can lead to an epileptic seizure. We usual switch patients to a long-acting barbiturate, phenobarbital, which is easier to stop. Withdrawal from caffeine worsens headaches, for which sumatriptan tablets or injections can help. Botox injections and other preventive migraine drugs can also make the withdrawal process less painful.

I should mention that I do have a very small number of patients for whom I prescribe these drugs for occasional use, but these exceptions confirm the rule – Fioricet and Fiorinal are ineffective for the vast majority of migraine sufferers and can lead to worsening of migraines and addiction.