People who suffer from tension headaches that do not respond to over-the-counter (OTC) medications may find relief with combination drugs that include butalbital.

Butalbital is not available as a single agent, but it is included with other ingredients in the prescription medications Fioricet and Fiorinal. It is a barbiturate sedative. In 2022, the Drug Enforcement Agency—responsible for the rules that govern access to these drugs—said it plans to put all forms into the more tightly controlled Class III category.1

This article explains butalbital use and why the drug offers benefits but also risks. It talks about why you should only use butalbital products prescribed by your healthcare provider.

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Uses

Butalbital combination drugs are strong pain relievers used in the treatment of tension headaches, but typically not for migraines. Its use in people with these headaches is not uncommon but it also comes with some cautions.

Among the drugs used to treat headaches severe enough to send people to the emergency department, one study found butalbital was used 2% of the time for care in the hospital and prescribed 5.3% of the time for continued treatment after discharge.2

However, the same study finds that butalbital use should be limited in favor of alternatives. That’s because it has a higher risk of medication overuse headaches, sometimes called rebound headaches. These headaches are caused by relying too heavily on medication to relieve symptoms.

Butalbital combination drugs also may lead to intoxication, drug dependency, and withdrawal syndrome.

Tension Headaches

A tension headache is the most common type of headache disorder. It occurs when neck and scalp muscles become tense. This causes pain, often described as a rubber-band-around-the-head feeling or pressure on both sides of the head.

Tension headaches can be triggered by a number of factors including stress, hunger, lack of sleep, anxiety, and temperature changes. They may occur at any age but are most common in adults and older teens. Some people are more prone to developing tension headaches than others, although the reason behind this is not very clear.

Most tension headaches are mild. They can be easily managed by:

• Getting rest
• Drinking more fluids to limit dehydration
• Avoiding any known triggers
• Taking an OTC medication like Motrin (ibuprofen) or Tylenol (acetaminophen)
• Trying physical therapy or cognitive behavioral therapy3

When recurring tension headaches do not respond to other treatments, your healthcare provider may prescribe Fiorinal or Fioricet. They are two different kinds of butalbital combination drugs.

Fioricet includes butalbital with acetaminophen and caffeine. Fiorinal is made with butalbital, aspirin, and caffeine. There are forms of each that also contain codeine. Codeine is an opiate drug, and it increases the risks of addiction and potential overdose.4

Butalbital relaxes the muscle tension believed to be associated with tension headaches. It also slows down your central nervous system by acting on a specific neurotransmitter, or chemical messenger, responsible for activating pain impulses.

Dosage

Always take these medications as prescribed by your healthcare provider. Be aware that extended and repeated use of butalbital can lead to physical dependence.

Fiorinal tablets were discontinued by the manufacturer, so it is now available only in capsule form. The capsules contain 50 milligrams (mg) butalbital, 325 mg aspirin, and 40 mg caffeine.5

One or two capsules of Fiorinal may be taken every four hours as needed. The total daily dosage is limited to six capsules. It should not be taken more than twice a week.

Fioricet is available in tablet or capsule form. It contains 50 mg butalbital, 300 mg acetaminophen, and 40 mg caffeine.

One or two tablets or capsules of Fioricet may be taken every four hours as needed. The total daily dosage is limited to six capsules, and its use should be limited to twice a week.6

Side Effects

Fioricet and Fiorinal should be taken with food or milk to prevent stomach irritation. The following side effects have been reported in people taking medications containing butalbital:7

• Confusion
• Depression
• Drowsiness
• Lightheadedness
• Stomach pain
• Nausea
• Vomiting

More serious side effects may occur and could be signs of an allergy or serious complications. See your healthcare provider immediately if you experience any of the following:8

• Difficulty breathing
• Itching
• Rash

Risks

Butalbital-containing medications can be habit-forming and may lead to addiction and other problems. It’s important that you understand the risks of taking Fioricet and Fiorinal.

It’s important that your healthcare provider know what medications you already take before you start a butalbital combination drug. Let them know if you:

• Are allergic to any ingredients in the medication, such as acetaminophen or aspirin
• Are currently taking blood thinners, antidepressants, antihistamines, or other sedatives such as sleeping pills or tranquilizers
• Have or previously had depression, liver disease, or porphyria, a rare metabolic condition
• Are pregnant, plan to become pregnant, or are currently breastfeeding

Intoxication

Because butalbital slows the central nervous system, you should not drive or operate heavy machinery while taking it. Watch for symptoms that include:

• Lack of coordination
• Problems with thinking and memory
• Slowness of speech
• Loss of inhibitions, meaning you may engage in risky behaviors
• Emotional disturbances

Medication Overuse Headache

A medication-overuse headache (MOH), once known as a drug-induced headache or medication-misuse headache, is a chronic headache that develops as a result of prolonged and frequent use of certain medications for acute headaches.

These headaches are a common side effect of butalbital, as well as a number of classes of medications used to treat headaches.

An MOH is diagnosed when a person has a headache 15 or more times a month and, in the case of combination pain relievers like Fioricet and Fiorinal, has been taking the drug for 10 days a month for more than three months.

Often, people with an MOH do not get pain relief from preventive headache medications. This lack of response is often a clue to healthcare providers that an MOH has developed.

Research suggests that butalbital combination drugs may lead to MOH headaches in just one year if they are taken only five times or more per month.

Withdrawal

When taking butalbital, you may experience withdrawal symptoms within eight to 36 hours after the last dose. Withdrawal symptoms may include:

• Anxiety
• Muscle twitching or tremors
• Confusion
• Dizziness
• Nausea and vomiting
• Insomnia
• Weight loss
• Seizures

Butalbital is one of the barbiturate drugs that may cause the most severe withdrawal symptoms, including seizures, delirium, and the collapse of your cardiovascular (heart and circulatory) system. These may be life-threatening symptoms and require monitoring by a healthcare provider.

Tolerance and Addiction

Tolerance and addiction may also occur with butalbital. Tolerance means that a person needs more of the medication to achieve headache relief. Addiction to butalbital is characterized by persistent behaviors, like compulsions, to take a butalbital-containing medication.

Acetaminophen Overdose

Do not take Fioricet along with other medications that contain acetaminophen as the combined dose can be toxic to the liver.

Precautions

Both Fiorinal and Fioricet can cause complications specific to their ingredients.

Acetaminophen

People who are sensitive to acetaminophen may experience an allergic reaction, and in rare cases a life-threatening form called anaphylaxis.

Butalbital

People with chronic renal (kidney) problems may have difficulty with butalbital in either of the two drugs. This is because butalbital is primarily cleared from the body through the kidneys. The acetaminophen also stresses the kidneys and may lead to early renal failure.

People with respiratory illnesses including sleep apnea, asthma, and chronic obstructive pulmonary disease (COPD) are at higher risk when taking butalbital because it depresses breathing function through its impacts on the nervous system.

In the Fiorinal form, the aspirin may add to breathing problems.

Codeine

When codeine is added to butalbital combination drugs, it may present risks to older people. It also may cause symptoms, some serious, in people with underlying medical conditions including:

• Heart problems, including arrhythmias (irregular heartbeats)
• High blood pressure or low blood pressure
• Diabetes
• Prostate conditions
• Respiratory diseases
• Inflammatory bowel disease and other digestive conditions

Your healthcare provider can help you to understand if butalbital combination drugs are safe for you, based on your overall health status, and prescribe the right product for your tension headaches.