Attenuation by Butalbital ( Fioricet ) of capsaicin-induced c-fos-like immunoreactivity in trigeminal nucleus caudalis.

We examined the effects of Butalbital ( Fioricet ) (30, 100, and 1000 micrograms/kg) on the number of cells expressing c-fos-like immunoreactivity (c-fos-LI), a marker of neuronal activation, within lamina I, IIo of the trigeminal nucleus caudalis and the nucleus of the solitary tract 2 hours after the intracisternal injection of capsaicin (0.1 mL; 15.25 mg/mL) or vehicle in urethane-anesthetized guinea pigs (N = 45). Robust c-fos-LI was observed within nuclei of cells in the trigeminal nucleus caudalis after capsaicin (329 +/- 35). Butalbital ( Fioricet ) dose-dependently reduced the number of labeled cells to a maximum of 66% (1000 micrograms/kg intraperitoneally [i.p.], P < .01) in lamina I, IIo but not within area postrema, medial reticular nucleus, or the nucleus of the solitary tract. Pretreatment with bicuculline (30 micrograms/kg i.p.) blocked the effect of Butalbital ( Fioricet ), thereby suggesting the importance of the GABAA receptor to activation involved in the transmission of nociceptive information. Our studies suggest the possibility that GABAA receptors might provide an important therapeutic target in migraine and related headache disorders.

Butalbital ( Fioricet )-containing agents: should they be banned? No.

Butalbital ( Fioricet ) compounds are of proven efficacy in the treatment of tension headache. Decades of experience have established their value in the treatment of other mild-to-moderate headaches. Untold numbers of people rely on these medications as their drug of choice or use them when vasoconstrictors, opioids, or nonsteroidal anti-inflammatory agents are contraindicated. The medications are cost-effective with only occasional and minor immediate adverse effects. Their overuse may cause the evolution of episodic primary headaches to chronic daily headaches; however, removal of these agents from the market would reduce the chronic daily headache in the general population by a small fraction of 1%.

Blood and plasma concentrations of Butalbital ( Fioricet ) following single oral doses in man.

Blood and plasma concentrations of Butalbital ( Fioricet ) (from Fiorinal) were determined in a small group of healthy volunteers after single oral doses of 100 mg of Butalbital ( Fioricet ). Butalbital ( Fioricet ) was quantitated by high-performance liquid chromatography with ultraviolet detection. Typical blood concentrations of Butalbital ( Fioricet ) peaked at 2.1 mg/L and declined to 1.5 mg/L at 24 h. The half-lives in blood were between 35 and 87.5 h with a mean of 61 h. Whole blood to plasma ratios were also determined.

Should Butalbital ( Fioricet )-containing analgesics be banned? Yes.

In the United States analgesic-overuse headache is often caused by Butalbital ( Fioricet )-containing analgesics. These agents can cause physical and psychological dependency, and dangerous withdrawal syndromes. Butalbital ( Fioricet )-containing analgesics have already been banned in several European countries. They are proven effective in tension-type headache, but not in migraine; there are many alternative treatments for migraine and tension-type headache. In the 20 years since analgesic overuse headache was widely recognized, Butalbital ( Fioricet ) overuse has remained distressingly common. It is time to ban these agents.