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Drug intelligence / Profile preview
butalbital + acetaminophen
- Development stage
- Approved
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Butalbital + acetaminophen is a combination drug used primarily for the symptomatic treatment of **tension-type headaches**. It combines butalbital, a barbiturate that produces central nervous system (CNS) depression and muscle relaxation, with acetaminophen, an analgesic and antipyretic agent. Butalbital works by acting as a CNS depressant that potentiates GABAergic inhibition via positive allosteric modulation at GABA-A receptors, and may provide muscle relaxation and anxiolytic effects. Acetaminophen is believed to exert its pain-relieving effect by inhibiting prostaglandin synthesis in the CNS and possibly modulating pain signaling pathways, although its precise mechanism is not fully understood. This combination is not first-line due to risks of dependence, misuse, and overuse headache, and is typically reserved when other medications fail or are not tolerated[1][2][3].
- Brand names
- BupapAllzitalButapap
- Other names
- butalbital/acetaminophen
02
Targets
GABA-B (Gamma-aminobutyric acid receptor type B)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)GABRA3 (Gamma-aminobutyric acid receptor subunit alpha-3)GABRA4 (GABA-A receptor subunit alpha-4)GABRA5 (Gamma-aminobutyric acid type A receptor subunit alpha-5)GABRA6 (Gamma-aminobutyric acid receptor subunit alpha-6)GRIA2 (AMPA receptor subunit GluA2)GRIK2 (Kainate receptor subunit GluK2)CHRNA4 (nAChR α4)CHRNA7 (α7 nicotinic receptor)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)
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