Disease relevance of LEVOBUNOLOL

• Levobunolol is a potent non-selective beta-adrenoceptor blocking agent used for the topical treatment of increased intraocular pressure in patients with chronic open angle glaucoma or ocular hypertension [1].
• In comparative studies of up to 2 years' duration levobunolol 0.5 to 1% reduced intraocular pressures by about 30% and adequately controlled intraocular hypertension in 50 to 85% of those treated [1].
• Contact dermatitis to levobunolol eyedrops superimposed on IgE-mediated rhinoconjunctivitis [2].
• Syncope, bradycardia, and atrioventricular block associated with topical ophthalmic levobunolol [3].
• Allergic contact dermatitis from levobunolol eyedrops [4].

High impact information on LEVOBUNOLOL

• Levobunolol, known to inhibit aqueous humor inflow in humans, slowed decay [5].
• Selective beta 1-adrenoceptor blockade (betaxolol) and nonselective beta-adrenoceptor blockade (levobunolol) were superimposed on graded exercise [6].
• Timolol (100 nM, 10 microM) and levobunolol (10 microM) produced cAMP-independent inhibition of the regulatory volume increase (RVI) in PE cells and increased intracellular Ca(2+) and pH [7].
• Location of penetration and metabolic barriers to levobunolol in the corneal epithelium of the pigmented rabbit [8].
• EDTA, which loosened the tight junctions between the superficial corneal epithelial cells, reduced both the transcorneal flux and metabolism of levobunolol [8].

Chemical compound and disease context of LEVOBUNOLOL

• Thus, ocular levobunolol is a well-tolerated and effective therapy for the management of raised intraocular pressure, and is a suitable alternative to ocular timolol in patients with chronic open angle glaucoma or ocular hypertension [1].
• One hundred fifty-two patients with open-angle glaucoma or ocular hypertension were randomized to receive either timolol maleate gel-forming solution QD or levobunolol BID for 6 weeks, followed by a crossover to the alternate treatment [9].
• Allergic contact dermatitis due to levobunolol with cross-sensitivity to befunolol [10].
• Betaxolol and levobunolol are two beta-adrenergic blocking agents being marketed as ophthalmic solutions for treatment of primary open-angle glaucoma (POAG) and ocular hypertension (OHT) [11].

Biological context of LEVOBUNOLOL

• Although the effects on peak heart rate were similar between the two medications, the effect on trough heart rate of timolol maleate gel-forming solution QD was significantly less than that of levobunolol BID (P = 0.001) [9].
• Total outflow facility and episcleral venous pressure measurements were similar in levobunolol-treated eyes and contralateral eyes treated with vehicle [12].
• Application of this method indicated that an azone-containing ophthalmic formulation of levobunolol did not produce better ocular bioavailability than a formulation containing no penetration enhancer [13].
• Diastolic blood pressure was decreased at two and four hours after administration of 0.5% levobunolol [14].

Anatomical context of LEVOBUNOLOL

• The low availability of levobunolol in the posterior segment as compared to timolol may be a key advantage for levobunolol in producing less adverse effect on blood flow in the choroid-retina and optic nerve [15].
• Topically applied levobunolol does not cause changes in the corneal endothelium [16].
• The number of endothelial cells, determined with a McIntyre eyepiece and an Eisner's contact lens, was not affected by levobunolol therapy [16].
• In scanning electron micrographs of the levobunolol treated animals, the corneal surface resembled the corneas of normal rabbits treated with artificial tears [17].
• The effects of levobunolol hydrochlorid (Bun) on the type L calcium channel currents (ICA) and delayed rectifier potassium channel currents (IK) in isolated ventricular myocytes of guinea pig were studied by using patch clamp whole cell recording techniques [18].

Associations of LEVOBUNOLOL with other chemical compounds

• Determination of levobunolol and dihydrolevobunolol in blood and urine by high-performance liquid chromatography using fluorescence detection [19].
• DATA SYNTHESIS: Timolol maleate, levobunolol, metipranolol, and carteolol have similar effectiveness in lowering intraocular pressure; however, levobunolol and timolol gel forming solution may have an advantage of once-daily dosing [20].
• These results indicate that high concentrations of unoprostone and beta-adrenergic blocking agents including betaxolol, timolol, levobunolol, and carteolol may inhibit ET-1-induced increase of [Ca2+]i. The mechanism may be mediated by inhibition of extracellular calcium influx via blocking of L-type voltage-dependent Ca2+ channel in A7r5 cells [21].
• 2. The ocular absorption of levobunolol in the presence of pilocarpine at acidic pH was enhanced by the use of sulfosuccinates, specifically Schercopol CMS [22].
• In logistic regression analysis previous allergy to a topically given antiglaucoma medication (t = -5.13) and concurrent use of levobunolol (t = 3.46) were retained as the most probable predictor variables of allergy to brimonidine [23].

Analytical, diagnostic and therapeutic context of LEVOBUNOLOL

• Once-daily versus twice-daily levobunolol (0.5%) therapy. A crossover study [24].
• The authors evaluated the efficacy of once-daily treatment with levobunolol in patients with primary open-angle glaucoma or ocular hypertension in an open-labeled, two-phase titration clinical trial [25].
• In study 2, 41 patients received either levobunolol or vehicle immediately after a unilateral ECCE involving the use of a viscoelastic preparation and the implantation of a posterior chamber intraocular lens (PC IOL) [26].
• The prophylactic effect of topical 0.5% levobunolol on intraocular pressure (IOP) elevations after neodymium:YAG (Nd:YAG) laser posterior capsulotomies and extracapsular cataract extractions (ECCEs) was investigated in two separate, double-masked, placebo-controlled studies [26].
• We evaluated the acute effects of installation of 0.5% levobunolol on aqueous humor dynamics in a double-masked study in 18 patients with ocular hypertension [12].

References