Drug intelligence / Profile preview

acetaminophen + butalbital + caffeine

Development stage
Approved
Lead developer
Sandoz
Modality
Small Molecules
Administration
Oral
01

Overview

Acetaminophen + butalbital + caffeine is a combination pharmaceutical product used primarily for the treatment of tension headaches (muscle contraction headaches). It combines three active ingredients with synergistic effects: acetaminophen, a non-opioid analgesic and antipyretic; butalbital, a short-to-intermediate acting barbiturate; and caffeine, a methylxanthine central nervous system stimulant. Acetaminophen provides pain relief by increasing the pain threshold, potentially through the inhibition of prostaglandin synthesis in the CNS. Butalbital acts as a sedative by modulating GABA-A receptors, helping to relieve the muscle tension and anxiety often associated with headaches. Caffeine serves as a vasoconstrictor, reducing blood flow in the brain and enhancing the analgesic efficacy of the other components. Originally developed and marketed under the brand name Fioricet, the combination is now widely available in generic forms and various strengths, typically 325 mg or 500 mg of acetaminophen, 50 mg of butalbital, and 40 mg of caffeine.

Brand names
FioricetEsgicEsgic-PlusZebutalButexOrbivanRepanDolgicAlagesicArcetPharbecMargesicMedigesicTriadVanatolCapacetCephadynIde-cetBupapVtol
Other names
Butalbital, Acetaminophen, and CaffeineAcetaminophen/Butalbital/Caffeine
02

Targets

ADORA2A (Adenosine A₂A Receptor)PGHS-1 (Prostaglandin G/H Synthase 1)ADORA1 (Adenosine receptor A1 subtype)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)GABRR (GABA-A receptor subunit rho)

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