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butalbital + aspirin + caffeine + codeine
- Development stage
- Approved
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This is a fixed-dose combination oral medication containing **butalbital** (a barbiturate CNS depressant), **aspirin** (a non-steroidal anti-inflammatory drug), **caffeine** (a CNS stimulant and adenosine receptor antagonist), and **codeine** (an opioid analgesic). It is primarily indicated for the treatment of tension-type (muscle contraction) headaches and may also be used for other pain conditions. Each component acts via a distinct mechanism: butalbital depresses the central nervous system (producing sedation), aspirin inhibits cyclooxygenase (reducing prostaglandin-mediated pain and inflammation), caffeine enhances analgesic efficacy (through vasoconstriction and CNS stimulation), and codeine binds to mu-opioid receptors (modulating pain perception). The combination is available as capsules and is associated with risks of dependence and withdrawal due to the butalbital and codeine components.
- Brand names
- Fiorinal with CodeineAscomp with CodeineFiorinal-C 1/2Fiorinal-C 1/4Teva-Tecnal C1/2Teva-Tecnal C1/4Trianal C1/2Trianal C1/4
- Other names
- butalbital-aspirin-caffeine-codeineaspirin/butalbital/caffeine/codeine combination
02
Targets
ADORA2A (Adenosine A₂A Receptor)GABRR (GABA-A receptor subunit rho)ADORA1 (Adenosine receptor A1 subtype)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)MOR (Mu opioid receptor)
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