Drug intelligence / Profile preview

acetaminophen + butalbital

Development stage
Approved
Modality
Small Molecules
Administration
Oral
01

Overview

**acetaminophen + butalbital** is an oral pharmaceutical combination of two small molecules: acetaminophen, an analgesic and antipyretic, and butalbital, a short-to-intermediate acting barbiturate. It is primarily indicated for the symptomatic treatment of **tension-type (muscle contraction) headaches** when other non-opioid analgesics and alternative treatments are inadequate[3][6][8]. Acetaminophen alters the way the body senses pain, likely through central inhibition of prostaglandin synthesis and modulation of serotonergic pathways, although its precise analgesic mechanism is not fully understood[3][7]. Butalbital is a central nervous system depressant that acts as a positive allosteric modulator at the GABA(A) receptor and can also antagonize certain neuronal acetylcholine and glutamate receptors, providing sedative and muscle-relaxing effects[1]. Butalbital is habit-forming, with risk of dependence, tolerance, and withdrawal. The use of this combination is limited due to potential for medication overuse headaches, CNS depression, abuse, and acetaminophen-related hepatotoxicity at high doses. The product is available as branded and generic oral tablets and capsules[6][7][8].

Brand names
BupapAllzitalAxocetBucetCephadynDolgicMartenORBIVAN CFPhrenilinPhrenilin FortePromacetRepan CFSedapapTencon
Other names
butalbital + acetaminophen
02

Targets

GABRA2 (Gamma-aminobutyric acid receptor subunit alpha 2)CHRNA7 (α7 nicotinic receptor)BZD site (GABA-A receptor benzodiazepine site)ADORA1 (Adenosine receptor A1 subtype)COXGRIA2 (AMPA receptor subunit GluA2)GABRA4 (GABA-A receptor subunit alpha-4)GABRA3 (Gamma-aminobutyric acid receptor subunit alpha-3)GABRA1 (Gamma-aminobutyric acid type A receptor alpha 1 subunit)GABRR (GABA-A receptor subunit rho)GABRA5 (Gamma-aminobutyric acid type A receptor subunit alpha-5)CHRNA4 (nAChR α4)GABRA6 (Gamma-aminobutyric acid receptor subunit alpha-6)GRIK2 (Kainate receptor subunit GluK2)

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