Phenylephrine prodrug. Report of clinical trials.
The authors evaluated the mydriatic effect of phenylephrine oxazolidine prodrug, a lipophilic sympathomimetic that undergoes hydrolysis to phenylephrine as it passes through the cornea and aqueous humor. Double-masked clinical trials were performed randomizing 66 healthy subjects to receive either the silicone vehicle as a placebo, 10% viscous phenylephrine hydrochloride (HCl), or prodrug in 0.25%, 0.50%, or 1.0% concentrations. A mean horizontal pupillary diameter of 8.8 mm was achieved in 30 minutes in those receiving 1% prodrug versus 6.5 mm obtained at 30 minutes with 10% viscous phenylephrine HCl. Statistically, this difference was highly significant at P less than or equal to 0.0001. There were minimal systemic or ocular adverse effects from any preparation.
Miller-Meeks
M J
MJ
Department of Ophthalmology, University of Iowa, Iowa City.
Farrell
T A
TA
Munden
P M
PM
Folk
J C
JC
Rao
C
C
Schoenwald
R D
RD
D000287:Administration, Topical; D000328:Adult; D000869:Anterior Eye Segment / Q000187:drug effects; D001794:Blood Pressure / Q000187:drug effects; D004311:Double-Blind Method; D005260:Female; D005654:Fundus Oculi; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D009184:Mydriatics / Q000494:pharmacology*; D010656:Phenylephrine / Q000031:analogs & derivatives* / Q000494:pharmacology; D011355:Prodrugs / Q000494:pharmacology*; D011680:Pupil / Q000187:drug effects*; D013008:Somatotypes
D009184:Mydriatics; D011355:Prodrugs; D010656:Phenylephrine; C050817:berefrine