Fioricet contains a combination of the drugs butalbital, acetaminophen, and caffeine. It is indicated for treating tension headaches. Fioricet has a very particular mechanism of action which makes it very effective for headaches and safer than many alternatives.
Butalbital Mechanism of ActionThe primary ingredient in Fioricet is butalbital, a type of barbiturate drug. Barbiturates are a group of drugs which slow down the central nervous system and cause sedation as well as numerous other benefits, like anxiety relief and anesthesia. Barbiturates have now mostly been replaced by benzodiazepines, a group of drugs which has similar benefits but does not have such a risk of addiction. Yet, barbiturates are still the better choice for treating some conditions. This is true of the butalbital in Fioricet when it comes to treating headaches.
The main way that butalbital relieves headache pain is by acting on GABA receptors. GABA (gamma-aminobutyric acid) is the main neurotransmitter found in the body. Its receptors are found throughout the body and in more abundance than any other neurotransmitter receptor. The main job of GABA is to keep our bodies calm. Without adequate GABA, problems such as seizures can occur. Inadequate GABA can also cause muscular spasms which may lead to tension headaches. Since butalbital acts on GABA receptors, it is particularly effective in relieving headaches.
GABA receptors are found throughout the body and there is no way that butalbital can act just on the receptors in the head. Thus, taking Fioricet will cause calming effects throughout the body. This is why the Fioricet commonly causes side effects like drowsiness and delayed reaction time.
Drug Synergy of Fioricet
Even though butalbital is the primary pain-reliever in Fioricet, the medicine also contains acetaminophen and caffeine. Both of these drugs in Fioricet can help relieve headaches. Acetaminophen is a pain reliever and inflammation reduces. Caffeine causes blood vessels to contract. Since tension headaches are characterized by dilated blood vessels, caffeine can be effective in relieving these headaches.
While acetaminophen and caffeine do help relieve headaches, this is not the main reason they have been included with butalbital in Fioricet. Rather, it is because of the synergistic effect they have with butalbital. A drug synergy occurs when drugs enhance each other’s effects. Thus, by taking butalbital with acetaminophen and caffeine, the pain relieving benefits of the barbiturate are increased.
Since butalbital is a barbiturate, a synergistic effect is particularly helpful. Barbiturates notoriously can cause tolerance, dependence and addiction. This is why they should be used in the smallest dosage possible. By formulating Fioricet based on drug synergy properties, less butalbital is needed in the formula and the drug becomes much safer to use.
Patients should still be cautious when using Fioricet that they do not take it too often or in too high of dosages. If Fioricet is used regularly, patients could develop a tolerance to the butalbital component of it. If would then need to take more of the medicine to relieve the headache. But, if acetaminophen is taken in high dosages, it can lead to severe liver damage or death. Never take more than 2 tablets at once or more than 6 tablets of Fioricet daily.
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