Drug intelligence / Profile preview

caffeine + butalbital + aspirin + codeine

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

Overview

caffeine + butalbital + aspirin + codeine is an oral fixed-dose combination small-molecule analgesic product indicated for the management of the symptom complex of tension or muscle contraction headache when non-opioid analgesics and alternative treatments are inadequate. The combination typically contains aspirin 325 mg, butalbital 50 mg, caffeine 40 mg, and codeine phosphate 30 mg per capsule. Its therapeutic effect is multimodal: aspirin inhibits cyclooxygenase-mediated prostaglandin synthesis, butalbital provides central sedative effects consistent with barbiturate activity and enhancement of GABAergic neurotransmission, caffeine acts as a central stimulant and adenosine receptor antagonist, and codeine is an opioid agonist whose analgesic activity is mediated largely through mu-opioid receptor signaling after metabolic conversion in part to morphine. It is an approved Schedule III controlled pharmaceutical product marketed as brands including Ascomp with Codeine, Fiorinal with Codeine, and Fiortal with Codeine, with use limited by risks of addiction, abuse, dependence, medication-overuse headache, and other opioid and barbiturate toxicities.

Brand names
Ascomp with CodeineFiorinal with CodeineFiortal with Codeine
Other names
butalbital + aspirin + caffeine + codeine phosphatebutalbital aspirin caffeine and codeine phosphate capsulesbutalbital aspirin caffeine and codeine phosphate capsules usp
02

Targets

ADORA2A (Adenosine A₂A Receptor)GABRR (GABA-A receptor subunit rho)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ADORA1 (Adenosine receptor A1 subtype)MOR (Mu opioid receptor)AMPAR (AMPA receptor)PDE (Phosphodiesterase family)PGHS-1 (Prostaglandin G/H Synthase 1)

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