Caffeine is a naturally occurring compound that stimulates the human central nervous system and increases the body's metabolic rate. The U.S. Food and Drug Administration categorizes caffeine as both a drug and a food additive. Caffeine has been used to treat a wide variety of medical problems: headaches, obesity, asthma, gallbladder disease, attention deficit-hyperactivity disorder (ADHD), shortness of breath in newborns, fatigue and low blood pressure.
How Caffeine Helps Relieve Headache Pain
Caffeine is an ingredient in many prescription and non-prescription pain medications. These products often contain codeine, acetaminophen, aspirin or ibuprofen as the main pain killer. Anecdotal and scientific evidence suggests that caffeine, in combination with a known analgesic, provides enhanced pain relief.
Caffeine is believed to relieve headache by restricting blood flow in the brain. Both migraines and tension headaches are triggered by an increase in cerebral blood flow. Caffeine acts by blocking the blood vessel dilating and blood flow increasing effects of the neurotransmitter, adenosine. The caffeine molecule resembles adenosine closely enough to fool the adenosine receptors that control the diameter of cerebral blood vessels.
Research Supports Caffeine's Effectiveness
Caffeine appears to work in synergy with analgesics such as acetaminophen or aspirin to relieve headache pain. In a sense, the cause and the symptoms of the headache are relieved at the same time. This synergy has been confirmed by several double-blinded scientific studies. The Diamond Headache Clinic, Chicago, Illinois, sponsored a study of the effectiveness of a combination of caffeine and ibuprofen. The study examined four sets of subjects who had been diagnosed with tension headache. The subjects were randomly treated with the combination of ibuprofen and caffeine, ibuprofen alone, caffeine alone or placebo. The results showed that ibuprofen combined with caffeine was significantly more effective than placebo, ibuprofen alone or caffeine alone.
The Diamond study also showed that caffeine alone did relieve headaches in 58 percent of the subjects tested. The dose of caffeine given in the study was 200 mg -- roughly the amount of caffeine in two cups of coffee. While effective, the caffeine-only pain relief subsided within 90 minutes.
A study conducted at the Albert Einstein College of Medicine and reported in "Archives of Neurology" in February 1998 examined a common over-the-counter headache preparation containing aspirin, acetaminophen and caffeine. Patients diagnosed with migraine headaches were randomly given the combination or a placebo. The researchers found the caffeine combination to highly effective, safe and well tolerated.
Available Pain Relievers Containing Caffeine
Several prescription-only pain medicines contain caffeine. One formula, which targets migraine sufferers, contains caffeine and the vasoconstrictor ergotamine. Another formula for tension headache combines caffeine, aspirin and the barbiturate, butalbital. Yet another formulation used to treat muscle injury pain mixes aspirin, caffeine and the muscle relaxant orphenadrine.
Precautions to Take with Headache Medicines Containing Caffeine
Consider the total amount of caffeine you consume each day in the form of coffee, tea, energy drinks, chocolate, etc. When caffeine intake is reduced abruptly, symptoms of withdrawal occur. Headaches are common during caffeine withdrawal. If you are taking a pain reliever and you reduce your total intake of caffeine rapidly, you may experience caffeine withdrawal symptoms and a rebound headache. It is best to limit your caffeine intake while you are treating your headache.
References
- PubMed Abstract: Ibuprofen plus caffeine in the treatment of tension-type headache
- Albert Einstein College of Medicine, Montefiore Headache Unit: Efficacy and safety of acetaminophen, aspirin, and caffeine in alleviating migraine headache pain: three double-blind, randomized, placebo-controlled trials
- British Medical Journal: Changes in cerebral blood flow during a migraine attack
- Wellness.MA: What is a Migraine?



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