M. Fanciullacci et al., BUSPIRONE, BUT NOT SUMATRIPTAN, INDUCES MIOSIS IN HUMANS - RELEVANCE FOR A SEROTONINERGIC PUPIL CONTROL, Clinical pharmacology and therapeutics, 57(3), 1995, pp. 349-355
Background and objective: Drugs that act on the serotoninergic system
have been shown to influence the pupil size, However, the 5-hydroxytry
ptamine (5-HT) receptor type or subtype that affects pupil diameter ha
s not been defined in humans, With a placebo-conet olled, double-blind
randomized design, we investigated in healthy volunteers the effect o
n pupil size of buspirone and sumatriptan, which mainly act on 5-HT1A-
and the 5-HT1-like receptors, respectively. Methods: The pupil area w
as measured by means of a videopupillometer before and after a single
oral administration of placebo or of three different doses of active d
rugs. Heart rate and arterial blood pressure were recorded after pupil
area measurement. Results: Buspirone (5, 10, and 20 mg) caused a dose
-dependent miosis. Sumatriptan (50, 100, and 200 mg) did not affect th
e pupil size. Twenty milligrams of buspirone reduced the mydriasis ind
uced by pretreatment with homatropine eyedrops. A 20 mg dose of buspir
one reduced blood pressure without change in heart rate, whereas buspi
rone, at doses lower than 20 mg, and sumatriptan did not affect heart
rate and blood pressure. Conclusions: This study suggests that buspiro
ne, but not sumatriptan, the selective agonist of 5-HT1-like receptors
, causes miosis in humans by activation of 5-HT1A receptors, possibly
located in the central nervous system where they inhibit iris sympathe
tic pathways. Measurement of pupil size seems to provide a valuable an
d sensitive index of 5-HT1A receptor function in humans.