Butalbital

Category: pharmacological

Aliases: Component of Fioricet

Pharmacological Mechanism

Short-acting barbiturate — GABA-A receptor positive allosteric modulator. Combined with acetaminophen + caffeine (Fioricet) for tension-type headache + migraine in legacy use. Schedule III; medication-overuse headache + dependence concerns limit current guidelines' enthusiasm. PK (Fioricet label, butalbital component): Well-absorbed from GI tract (F ~0.95 — textbook for short/intermediate-acting barbiturates), t½ 35 h (intermediate-acting), elimination 59–88% renal as parent or metabolites. Vd ~0.8 L/kg (~56 L, textbook barbiturate). The 35-h t½ underlies the rebound-headache risk on chronic Fioricet use — multi-day accumulation at qid dosing. Tmax not in the label; co-formulated APAP (t½ 1–3 h) + caffeine (t½ 3 h) clear long before butalbital.

Half-Life (t½)

PO: 35h

Dosing Guidelines

Target Organ Systems