Butalbital as a single agent is discontinued. It is used in combination with acetaminophen or acetylsalicylic acid (aspirin) to treat pain and vascular headaches.

Combos

With acetaminophen: Fioricet

With acetylsalicylic acid (aspirin): Fiorinal

 

Butalbital is well absorbed from the gastrointestinal tract and is expected to distribute to most tissues in the body. Barbiturates in general may appear in breast milk and readily cross the placental barrier. They are bound to plasma and tissue proteins to a varying degree and binding increases directly as a function of lipid solubility.

Elimination of butalbital is primarily via the kidney (59% to 88% of the dose) as unchanged drug or metabolites. The plasma half-life is about 35 hours. Urinary excretion products include parent drug (about 3.6% of the dose), 5-isobutyl-5-(2, 3-dihydroxypropyl) barbituric acid (about 24% of the dose), 5-allyl-5(3-hydroxy-2-methyl-1-propyl) barbituric acid (about 4.8% of the dose), products with the barbituric acid ring hydrolyzed with excretion of urea (about 14% of the dose), as well as unidentified materials. Of the material excreted in the urine, 32% is conjugated.

The in vitro plasma protein binding of butalbital is 45% over the concentration range of 0.5-20 mcg/mL. This falls within the range of plasma protein binding (20%-45%) reported with other barbiturates such as phenobarbital, pentobarbital, and secobarbital sodium. The plasma-to-blood concentration ratio was almost unity, indicating that there is no preferential distribution of butalbital into either plasma or blood cells.

Butalbital and Acetaminophen

Butalbital and acetaminophen combination is a pain reliever and relaxant. It is used to treat tension headaches. Butalbital belongs to the group of medicines called barbiturates. Barbiturates act in the central nervous system (CNS) to produce their effects.

When you take butalbital for a long time, your body may get used to it so that larger amounts are needed to produce the same effects. This is called tolerance to the medicine. Also, butalbital may become habit-forming (causing mental or physical dependence) when it is used for a long time or in large doses. Physical dependence may lead to withdrawal side effects when you stop taking the medicine. In patients who get headaches, the first symptom of withdrawal may be new (rebound) headaches.

Some butalbital and acetaminophen combinations also contain caffeine. Caffeine may help to relieve headaches. However, caffeine can also cause physical dependence when it is used for a long time. This may lead to withdrawal (rebound) headaches when you stop taking it.

Butalbital and acetaminophen combination may also be used for other kinds of headaches or other kinds of pain as determined by your doctor.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe Interactions of butalbital include:

• sodium oxybate

Butalbital has serious interactions with at least 51 different drugs.

Butalbital has moderate interactions with at least 301 different drugs.

Butalbital has mild interactions with at least 127 different drugs.

Butalbital has mild interactions with at least 39 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.