Drug intelligence / Profile preview

caffeine + codeine phosphate + butalbital + aspirin

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

Overview

caffeine + codeine phosphate + butalbital + aspirin is an oral fixed-dose **small molecule** combination analgesic approved for the management of the symptom complex of tension or muscle contraction headache when non-opioid and non-barbiturate alternatives are inadequate. The capsule commonly contains aspirin 325 mg, butalbital 50 mg, caffeine 40 mg, and codeine phosphate 30 mg. Its therapeutic effect is produced through complementary mechanisms: codeine acts as an opioid agonist in the central nervous system to reduce ascending pain signaling, butalbital is a barbiturate central nervous system depressant that promotes relaxation and sedation, aspirin inhibits cyclooxygenase-mediated prostaglandin synthesis to provide analgesic and anti-inflammatory activity, and caffeine is a methylxanthine that acts as a central stimulant and cranial vasoconstrictor that can enhance analgesia. It is marketed under brand names including Fiorinal with Codeine and Ascomp with Codeine and is a Schedule III controlled substance because of abuse, dependence, overdose, and respiratory depression risks associated with the codeine and butalbital components.

Brand names
Fiorinal with CodeineAscomp with Codeine
Other names
butalbital + aspirin + caffeine + codeine phosphatebutalbital aspirin caffeine and codeine phosphate capsulesbutalbital aspirin caffeine and codeine phosphate capsules usp
02

Targets

GABRR (GABA-A receptor subunit rho)COXMOR (Mu opioid receptor)ADORA1 (Adenosine receptor A1 subtype)PDE (Phosphodiesterase family)ADORA2A (Adenosine A₂A Receptor)

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