Ocular Metipranolol

Abstract

Metipranolol is a non-selective beta-adrenoceptor blocking agent used for the topical treatment of elevated intraocular pressure in patients with chronic open angle glaucoma or ocular hypertension. In double-blind comparative studies of up to 4 months duration, metipranolol 0.1 to 0.6% produced comparable reductions in intraocular pressure to timolol 0.25 to 0.5% and levobunolol 0.5%, lowering pressure by about 20 to 29% from baseline. Metipranolol has been well tolerated by most patients, producing only minor changes in objective measurements of ophthalmic status and systemic parameters. Similarly, subjective ophthalmic complaints have been minimal although reports of initial stinging or burning upon instillation have occurred. Further published reports, in which larger numbers of patients are treated over extended periods, are needed to confirm the drug's apparent long term comparative efficacy. Studies of ocular metipranolol to date are encouraging, and the drug demonstrates a lasting intraocular pressure reducing effect with good tolerability. Thus, ocular metipranolol provides a viable alternative to ocular timolol and levobunolol in the topical treatment of chronic open angle glaucoma or ocular hypertension.

Chemical Insights into Topical Agents in Intraocular Pressure Management: From Glaucoma Etiopathology to Therapeutic Approaches

“…In this study, mean IOP decreases ranging from 31 to 38% from baseline were observed with the reductive effects of the dose persisting for up to 24 h and longer [ 209 ]. Metipranolol 0.1–0.6% demonstrated IOP reduction effects ranging from 20 to 29% decreases from baseline, determined to be comparable to the therapeutic activity of timolol 0.25–0.5% and levobunolol 0.5% [ 210 , 211 ]. In vivo studies regarding the unintended ocular effects of metipranolol have reported consequential corneal alterations: reduced number of microvilli covering the outer plasma membrane and widened intracellular spaces on the surface cell layers.…”

“…In vivo studies regarding the unintended ocular effects of metipranolol have reported consequential corneal alterations: reduced number of microvilli covering the outer plasma membrane and widened intracellular spaces on the surface cell layers. These observations, however, were deemed to be insignificant considering the overall well-being of the eye [ 211 ]. At the clinical level, research endeavors monitored the hemodynamic effects of the ocular instillation of the drug, demonstrating that systolic or diastolic blood pressure and heart rate are not significantly altered following ocularly instilled metipranolol 0.1 to 0.6% [ 212 ].…”

“…At the clinical level, research endeavors monitored the hemodynamic effects of the ocular instillation of the drug, demonstrating that systolic or diastolic blood pressure and heart rate are not significantly altered following ocularly instilled metipranolol 0.1 to 0.6% [ 212 ]. Battershill et al have provided an organized review of the clinical trials comparatively assessing the therapeutic efficacy of metipranolol with other beta blockers and antiglaucoma substances [ 211 ]. Metipranolol reportedly induces common ocular adverse effects that are observed with other beta blockers: stinging and burning in 12–56% of patients, hyperemia, reduction in tear production, and blurred vision [ 213 ].…”

Recent Patents on Emerging Therapeutics for the Treatment of Glaucoma, Age Related Macular Degeneration and Uveitis

“…Levobunolol undergoes enzymatic hydrolysis to generate dihydrolevobunolol, a potent β-adrenoceptor blocker in the cornea, aqueous humor and iris-ciliary body. Both these molecules exhibit comparable activity in reducing IOP [18, 19]. Carteolol, a hydrophilic non-selective partial β-adrenoceptor antagonist reduces IOP and is more preferable in patients with bradycardia, heart failure and pulmonary complications.…”