Butalbital

Products

In many countries, drugs containing butalbital are no longer approved (e.g., Cafergot-PB). Combination products are still on the market in some countries, including the United States, where numerous products are available.

Structure and properties

Butalbital (C11H16N2O3, Mr = 224.3 g/mol) or 5-allyl-5-isobutylbarbituric acid exists as a slightly bitter, white, odorless, crystalline powder that is soluble in boiling water.

Effects

Butalbital (ATC N05CA) has depressant, sedative, and sleep-inducing properties. The effects are due to interaction with GABA receptors, resulting in increased chloride transport and hyperpolarization of the cell membrane. Butalbital has a long half-life of 35 to 88 hours.

Indications

Butalbital is administered in combination with other agents (eg, acetylsalicylic acid, caffeine, acetaminophen, codeine) for the treatment of headache and migraine.

Abuse

Butalbital can be abused as a sedative narcotic.