Noncardioselective beta-adrenoceptor antagonists are used for treatment of increased intraocular pressure. Because these agents may be absorbed systemically, their use is of concern in patients with restricted pulmonary function. We compared the efficacy of betaxolol, a cardioselective beta-adrenoceptor antagonist, and dipivefrin, an alpha/beta-adrenergic agonist. Seventy-six patients with open-angle glaucoma or ocular hypertension were randomly assigned to receive either betaxolol 0.5% or dipivefrin 0.1%. Patients were examined at two weeks, one month, two months, and three months. Intraocular pressure reductions were similar, with a mean decrease of 4.1 mm Hg in the betaxolol group and 3.5 mm Hg in the dipivefrin group. Both treatments caused similar minor increases in heart rate, typical with alpha-adrenergic agonists but atypical with beta-blockers. Stinging or burning in the betaxolol group was significantly (P = .008) greater than in the dipivefrin group. Our findings suggest that betaxolol and dipivefrin therapy are effective, equivalent ocular hypotensive agents.