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Topical Ophthalmic β‐Adrenergic Blockade for the Treatment of Glaucoma and Ocular Hypertension
Author(s) -
Frishman William H.,
Fuksbrumer Moshe S.,
Tannenbaum Mark
Publication year - 1994
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/j.1552-4604.1994.tb02042.x
Subject(s) - betaxolol , timolol , medicine , ocular hypertension , glaucoma , intraocular pressure , pharmacology , agonist , adrenergic beta antagonists , anesthesia , ophthalmology , propranolol , receptor
Since the late 1970s, topical β‐adrenergic blockers have been the drugs of choice in treating ocular hypertension and associated glaucoma. The currently available drugs are timolol, betaxolol, levobunolol, metipranolol, and carteolol. All reduce intraocular pressure by decreasing the production of aqueous humor. Although these drugs are applied locally in the eye, they may enter the general circulation and reach concentrations high enough to cause systemic effects, including alterations in heart rate and rhythm, bronchoconstriction, dyslipidemia, and central nervous system abnormalities. Interactions with other drugs may also occur. Ocular β‐ blockers differ in β 1 ‐selectivity (betaxolol is β 1 ‐selective, whereas the other drugs are nonselective) and in intrinsic sympathomimetic activity (ISA) or partial agonist properties (only carteolol possesses ISA). These differences give betaxolol and carteolol potential advantages in minimizing certain side effects. The advantage of betaxolol vis‐à‐vis systemic side effects is more clearly established than that of carteolol. Further systematic study is needed to determine what advantages, if any, are conferred by the presence of ISA.