6-amino-2-benzothiazole-sulfonamide. The effect of a topical carbonic anhydrase inhibitor on aqueous humor formation in the normal human eye.
The carbonic anhydrase inhibitor, 6-amino-2-benzothiazolesulfonamide, formulated as a 3% suspension in a gel vehicle was instilled in one eye of 21 human subjects in a single dose study to determine its effect on aqueous dynamics. A small but statistically significant effect on aqueous humor flow was observed 2 to 7 hours after application. By 8 hours, the effect had disappeared, and intraocular pressure (IOP) measured 8 hours after application of a single dose was unchanged in these normal volunteers. The drug and its vehicle caused local side effects including irritation, hyperemia, and blurred vision. The authors wondered if multiple doses would produce a greater effect. Four subjects received up to four doses of the drug over 2 days and were restudied. Marked bulbar injection and follicular conjunctivitis, attributable to either the drug or the vehicle, developed in two of the subjects, both contact lens wearers. A milder form of bulbar injection and follicular conjunctivitis developed in a third subject, who received three doses of the drug and was not a contact lens wearer. These side effects precluded additional multiple-dose testing of this formulation of the drug, and no conclusions about the effect of the drug on aqueous flow can be drawn from this portion of the study.
Kalina
P H
PH
Department of Ophthalmology, Mayo Clinic, Rochester, MN 55905.
Shetlar
D J
DJ
Lewis
R A
RA
Kullerstrand
L J
LJ
Brubaker
R F
RF
D000328:Adult; D001082:Aqueous Humor / Q000187:drug effects* / Q000378:metabolism; D052160:Benzothiazoles; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D002940:Circadian Rhythm; D003231:Conjunctivitis / Q000139:chemically induced / Q000473:pathology; D004728:Endothelium, Corneal / Q000187:drug effects / Q000378:metabolism; D005016:Ethoxzolamide / Q000009:adverse effects / Q000031:analogs & derivatives / Q000493:pharmacokinetics / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D010539:Permeability; D012016:Reference Values; D013844:Thiazoles / Q000494:pharmacology*
D052160:Benzothiazoles; D002257:Carbonic Anhydrase Inhibitors; D013844:Thiazoles; C049027:aminozolamide; D005016:Ethoxzolamide