Abstract

The cardioselective beta-blocker, betaxolol, is an effective ocular antihypertensive agent. Its mode of action in lowering intraocular pressure is similar to that of the nonselective blockers, by suppressing the flow of aqueous humor. The most frequent adverse reaction to betaxolol is stinging upon administration, which is minimised by an ocular suspension with a similarly effective twofold reduced concentration (Betoptic S, 0.25%). The extent of beta 1-adrenoceptor occupancy of topically applied betaxolol in the systemic circulation is less than that of the nonselective blockers and beta 2-receptor occupancy is negligible, providing a better safety profile in patients with cardiopulmonary disease. Experimental studies have revealed that the drug reaches the retina after topical administration and displays a voltage-dependent L-type calcium channel blocking activity, which probably allows betaxolol to improve retinal perfusion and to serve as a neuroprotective agent recommendable in various forms of glaucoma.