The Sound of Evolution
Butalbital
Mechanism of action:
Butalbital is a barbiturate central nervous system depressant. Butalbital binds to the barbiturate binding site on the GABA_A receptor complex, prolonging the opening time of the chloride ion channel and increasing Cl⁻ influx. This causes neuronal hyperpolarization, reduces neuronal excitability, and produces sedative and relaxation-related effects, while also influencing central nervous system regulation associated with tension-type headache.
Reference(s):
1. Silberstein SD et al. (2001). Butalbital in the treatment of headache: history, pharmacology, and efficacy. Headache.
2. Wenzel RG et al. (2002). Do butalbital-containing products have a role in the management of migraine? Pharmacotherapy.
3. Bryczkowski C et al. (2012). Combined butalbital/acetaminophen/caffeine overdose: case files of the Robert Wood Johnson Medical School Toxicology Service. J Med Toxicol.