Drug intelligence / Profile preview

aspirin + caffeine + butalbital + codeine

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

Overview

**Aspirin + caffeine + butalbital + codeine** is an oral fixed-dose **small-molecule combination** analgesic product marketed in capsule form for the management of **tension (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 pharmacology reflects the four active ingredients: aspirin inhibits cyclooxygenase enzymes and prostaglandin synthesis to provide analgesic and anti-inflammatory effects; butalbital is a barbiturate that depresses CNS activity via the GABA-A receptor complex; caffeine is a methylxanthine CNS stimulant and cerebral vasoconstrictor that can enhance analgesic efficacy; and codeine is an opioid agonist that acts primarily through mu-opioid receptors to inhibit ascending pain pathways. The product is available as branded and generic formulations and is reserved for selected patients because of the risks of addiction, abuse, misuse, medication-overuse headache, and other opioid- and barbiturate-related toxicities.

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

Targets

ADORA2A (Adenosine A₂A Receptor)ADORA3 (Adenosine A3 receptor)GABRR (GABA-A receptor subunit rho)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ADORA2B (Adenosine A2B receptor)ADORA1 (Adenosine receptor A1 subtype)MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)

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