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PubMed1989

Levobunolol. A four-year study of efficacy and safety in glaucoma treatment. The Levobunolol Study Group.

In a 4-year, double-masked, parallel, multicenter study comparing the efficacy and safety of levobunolol and timolol, 391 patients with open-angle glaucoma or ocular hypertension were randomly assigned to receive masked 0.5% or 1% levobunolol, or 0.5% timolol, twice daily. Mean decreases in intraocular pressure (IOP) over 4 years of therapy were 7.1, 7.2, and 7.0 mmHg for 0.5% levobunolol, 1% levobunolol, or 0.5% timolol, respectively. Little attenuation of ocular hypotensive efficacy occurred. The 4-year efficacy failure rate for the three groups, which did not differ from each other, was approximately 30%. Adverse experiences requiring cessation of therapy occurred in an additional 10% of patients. The vast majority of efficacy failures (79/95) and of adverse events (33/37) requiring removal from the study occurred during the first 2 years. Overall mean decreases in heart rate for the 4 years ranged from 3 to 6 beats per minute for all treatment groups; overall mean decreases in systolic and diastolic blood pressure ranged between 1 and 2 mmHg. The authors concluded that levobunolol is relatively effective and relatively safe for the long-term (4-year) treatment of elevated IOP.

Adolescent↗

PubMed1985

Levobunolol. A beta-adrenoceptor antagonist effective in the long-term treatment of glaucoma. The Levobunolol Study Group (Appended).

We compared the ocular-hypotensive efficacy and systemic and ocular safety of an ophthalmic solution of levobunolol (0.5% and 1%) twice daily, with timolol (0.5%) twice daily in a long-term double-masked study of 391 patients with open-angle glaucoma or ocular hypertension. Patients received the test medication in both eyes for up to two years. Over the two-year period, both concentrations of levobunolol reduced mean IOP by 27% (range, -6 to -8 mmHg). This ocular-hypotensive effect was sustained throughout the study and was similar to that produced by timolol. Slight decreases in mean heart rate and blood pressure were observed. No unexpected adverse ocular or systemic reactions were reported. The results of these studies indicate that levobunolol is an effective therapy for the long-term treatment of glaucoma.

Adrenergic beta-Antagonists↗

PubMed2002

A comparison of the efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution QD and 0.5% levobunolol hydrochloride BID in patients with ocular hypertension or open-angle glaucoma.

The purpose of this study was to compare the ocular hypotensive efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution (timolol gel) and 0.5% levobunolol hydrochloride (levobunolol). This was a randomized, double-masked, multi-center, active-controlled, 2-period, crossover study. After a 3-week, single-masked placebo run-in phase, patients with ocular hypertension or open-angle glaucoma and an intraocular pressure (IOP) > or = 22 mmHg were randomized to receive timolol gel QD or levobunolol BID for 6 weeks followed by a 3-week, placebo washout period. Patients were then crossed over to the alternate treatment for 6 weeks. IOP and heart rate (HR) were measured at 3 and 6 weeks after the start of therapy with either timolol gel or levobunolol. Of 133 patients randomized, 116 received both treatments. Timolol gel QD was comparable to levobunolol BID in reducing trough and peak IOP. At trough, HR was marginally increased with timolol gel and was decreased with levobunolol (p = < 0.001). At peak, HR was decreased with both treatments, but the decrease was significantly less with timolol gel than with levobunolol (p = 0.049). Significantly more patients experienced at least one adverse event (p = 0.024), adverse events related to special senses (p = 0.002), and burning and stinging (p < 0.001) with levobunolol compared to timolol gel. The study demonstrates that timolol gel QD has IOP-lowering effects comparable to those of levobunolol BID with fewer adverse experiences and less effect on HR.

Adrenergic beta-Antagonists↗

PubMed1986

Glaucoma treatment with once-daily levobunolol.

Although twice-daily instillation of topical beta-blockers is the standard regimen for treatment of increased intraocular pressure, once-daily therapy might improve patient compliance and provide greater safety. In a three-month, double-masked clinical trial, 92 patients with open-angle glaucoma or ocular hypertension received levobunolol 0.5% or 1% or timolol 0.5% once daily, in both eyes. Overall mean decreases in intraocular pressure were significantly greater in the groups treated with levobunolol than in the group treated with timolol. Intraocular pressure decreases averaged 7.0 mm Hg with levobunolol 0.5%, 6.5 mm Hg with levobunolol 1%, and 4.5 mm Hg with timolol. The intraocular pressures of 72% (18 of 25 patients) of those treated with levobunolol 0.5%, 79% (22 of 28 patients) of those treated with levobunolol 1%, and 64% (16 of 25 patients) of those treated with timolol were successfully controlled during the study. Heart rate and blood pressure decreases were minimal with both levobunolol and timolol. Study results indicated that once-daily treatment with levobunolol and, to a lesser extent, timolol is sufficient to control intraocular pressure successfully and safely.

Actuarial Analysis↗

PubMed1988

Prophylactic treatment of intraocular pressure elevations after neodymium: YAG laser posterior capsulotomies and extracapsular cataract extractions with levobunolol.

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. In study 1, 42 patients received either levobunolol or vehicle 1 hour before a unilateral Nd:YAG laser posterior capsulotomy. Elevated IOP (greater than or equal to 10 mmHg) occurred in up to 38% of those in the vehicle group and none in the levobunolol group. Mean IOP increased up to 6 mmHg in the vehicle group, whereas it decreased up to 3 mmHg in the levobunolol group. 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). The incidence of IOP elevations (greater than or equal to 10 mmHg) was up to 40% in the vehicle group and 19% in the levobunolol group. Mean IOP increased up to 9 mmHg in the vehicle group and up to 2 mmHg in the levobunolol group. Thus, marked elevations in IOP after posterior capsulotomies or ECCEs may be minimized by prophylactic treatment with levobunolol.

Cataract Extraction↗

PubMed1997

Effect of one week of levobunolol HCl 0.5% on the human retinal circulation.

PURPOSE: To determine the effect of one week of topical treatment with levobunolol HCl 0.5% on the retinal circulation of normal subjects. METHODS: Fifteen healthy volunteers with no history of ocular disease were included in this study. In a double-masked, randomized, cross-over design, one eye of each subject was treated, for one week, with one drop of either levobunolol or placebo, administered twice daily. Following a washout period of at least three weeks, the same eye received the alternate treatment for one week. Before the beginning of therapy and then two hours after the last drop, vessel diameter (D), maximum erythrocyte velocity (Vmax), and volumetric blood flow rate (Q) were determined in one major retinal vein of the treated eye, using bidirectional laser Doppler velocimetry and monochromatic fundus photography. Statistical analysis was performed using two-tailed, paired Student's t-test, linear regression, and correlation analysis. RESULTS: The average percentage change from baseline in intraocular pressure was statistically significant following levobunolol (-15% +/- 13% (+/-1 SD), P < .001), but not following placebo (-3% +/- 11%, P > .05). No significant changes in average D, Vmax, or Q were observed after levobunolol treatment (-1% +/- 4%, 5% +/- 11%, 4% +/- 15%, respectively) or placebo treatment (-1% +/- 4%, -2% +/- 9%, -5% +/- 10%, respectively). The average difference between the changes in Q from baseline after levobunolol and placebo treatments (9% +/- 17%) achieved a significance level of P = 0.06. Furthermore, following levobunolol treatment, Q was 7% +/- 14% higher than following placebo treatment (P = 0.05). CONCLUSIONS: A comparison of the effects of placebo and levobunolol treatments suggests that levobunolol has a variable effect on the retinal circulation with a tendency to show an overall slight increase in flow.

Adrenergic beta-Antagonists↗

PubMed1995

Comparison of concentration-time profiles of levobunolol and timolol in anterior and posterior ocular tissues of albino rabbits.

The potential effects of anti-glaucoma drugs, such as levobunolol and timolol, on blood flow in the posterior segment of the eye are of great interest in terms of changes in optic nerve head perfusion and prevention of visual field loss. These effects are related to the rate and extent of their absorption into the site of action. In this study, the concentrations of timolol and levobunolol in the aqueous humor, iris-ciliary body, vitreous humor, choroid-retina, and optic nerve were compared following instillation of a single drop of 0.5% ophthalmic solutions into albino rabbit eyes. Tissue drug and metabolite concentrations were measured by liquid chromatography-mass spectrometry. Dihydrobunolol (DHB) is an equipotent metabolite of levobunolol. In the anterior segment of the eye, levobunolol plus DHB concentrations were higher than timolol concentrations in aqueous humor and were comparable to those of timolol in iris-ciliary body. However, in the choroid-retina and optic nerve, timolol concentrations were greater than those of levobunolol plus DHB. Overall, the study demonstrates comparable concentrations of levobunolol and timolol in the anterior section of the eye. 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.

Absorption↗

PubMed1988

Ocular metabolism of levobunolol.

Dihydrobunolol is an ocular metabolite equipotent to levobunolol. In order to understand the formation and distribution of dihydrobunolol after an ophthalmic dose of levobunolol, studies in vitro and in vivo were initiated. The metabolism of levobunolol to dihydrobunolol was investigated using an organ-culture technique. The corneal formation of dihydrobunolol was pH-dependent and increased as the pH of the incubation fluid increased from 5.3 to 8.3. Its formation from levobunolol was saturable with Vmax and Km values (pH 7.4) of 13.2 nmol/min/gm of cornea and 1.48 mM, respectively. After a topical dose of 0.5% levobunolol hydrochloride to rabbit eyes, rapid absorption of levobunolol and facila formation of dihydrobunolol were noted. The drug concentration in the eye drop (approximately 17 mM) was much higher than Km and would saturate the epithelial reductase system in the cornea during drug absorption. The total concentrations of levobunolol and dihydrobunolol in ocular tissues were in the micromolar range throughout the experimental period. Dihydrobunolol, after distribution equilibrium, was the major drug-derived species in the cornea, aqueous humor, and iris-ciliary body. The study results indicated pH-dependent and capacity-limited formation of dihydrobunolol in the cornea. Buffering capacity and the drug concentration in the ophthalmic dose are important formulation strategies because they may affect the rate and the extent of dihydrobunolol formation in the epithelial cell layers of the cornea.

Animals↗

PubMedDate not supplied

Efficacy and tolerability of 0.5% timolol maleate ophthalmic gel-forming solution QD compared with 0.5% levobunolol hydrochloride BID in patients with open-angle glaucoma or ocular hypertension.

We compared the efficacy of timolol maleate ophthalmic gel-forming solution 0.5% QD with that of levobunolol hydrochloride 0.5% BID, as measured by change in intraocular pressure (IOP), effect on heart rate, and ocular tolerability. The study had a positive-controlled, double-masked, randomized, multicenter, 12-week, two-period (6 weeks each), crossover design. 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. IOP and heart rate were measured at morning trough and peak during weeks 3, 6, 9, and 12. Timolol maleate gel-forming solution QD was comparable to levobunolol BID in reducing IOP at peak and trough. 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). The incidence of ocular burning and stinging was comparable between the two treatments. Patients experienced significantly more blurred vision when using timolol maleate gel-forming solution than when using levobunolol (P = 0.013). Overall, more patients experienced at least one adverse event when using timolol maleate gel-forming solution. Timolol maleate gel-forming solution QD is as efficacious in reducing IOP as levobunolol BID.

Adrenergic beta-Antagonists↗

PubMed1988

Ocular hypotensive efficacy of 0.25% levobunolol instilled once daily.

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. All patients started the study using 0.25% levobunolol administered once daily for 3 months (phase I). If a patient's intraocular pressure (IOP) was not controlled with this concentration of levobunolol, the concentration was increased to 0.5% administered once daily for 3 months (phase II). During phase I, a significant reduction in IOP was observed in 21 of the 29 patients (72%), with an average IOP reduction of 24%. During phase II, in six patients whose IOP was reduced inadequately with 0.25% levobunolol, one had a significant reduction in IOP with 0.5% levobunolol. The authors concluded that levobunolol, instilled once daily at a concentration of 0.25%, was effective in significantly reducing IOP in the majority of the patients evaluated.

Adult↗

PubMed2003

Comparison of the effects of topical levobunolol and timolol solution on the human ocular surface.

PURPOSE: To compare the effects of levobunolol hydrochloride and timolol maleate on tear volume, precorneal tear film stability, and corneal epithelial barrier function in normal human eyes. SUBJECTS AND METHODS: The study population consisted of 14 healthy volunteers. To obtain pretreatment baseline values, we determined the radius of the tear meniscus (RTM) by meniscometry; the noninvasive breakup time (NIBUT) of the precorneal tear film with a tear specular microscope; and corneal fluorescein uptake with a fluorophotometer. Levobunolol hydrochloride (0.5%) or timolol maleate solution (0.5%) was instilled twice daily for 4 weeks into 1 eye; the contralateral eye was treated with the other topical drug twice daily for the same period. At the end of the study period, the same tests were performed, and the pre- and posttreatment results were compared. RESULTS: Timolol solution did, and levobunolol did not, significantly reduce NIBUT from the baseline values. RTM was significantly decreased by treatment with either timolol or levobunolol solution. Corneal fluorescein uptake was not significantly changed, although it was higher after treatment with both topical drugs. CONCLUSIONS: Four-week treatment with timolol solution resulted in significant instability of the precorneal tear film. Both timolol and levobunolol solution significantly decreased tear volume on the ocular surface. These results indicate that levobunolol solution applied twice daily has equal effects on the tear volume and corneal epithelial barrier function as does timolol solution applied twice daily and that it affects precorneal tear film stability less than timolol solution.

Adrenergic beta-Antagonists↗

PubMed1992

In-vitro assessment of a matrix system of levobunolol.

In order to study the feasibility of systemic delivery of levobunolol transdermally, a matrix-type delivery system was fabricated using a silicone elastomer. The relationship between loading dose and skin permeation rate was evaluated in-vitro using hairless mouse skin mounted on the stirred receptor compartment of the Keshary-Chien glass diffusion cell maintained at 37 degrees C. The concentration of levobunolol in the receptor compartment was determined by HPLC. A similar study without using the skin was carried out to determine the effect of loading dose on the release of levobunolol from discs. It was observed that the release of drug from disc followed a matrix-diffusion controlled (Q) vs square root of time relationship at different loading doses. In contrast, the results of skin permeation of levobunolol from transdermal discs containing different loading doses showed a linear Q vs time relationship indicating a constant zero order skin permeation rate at each loading dose. Skin permeation of levobunolol appeared to reach a plateau at a 5% (w/w) loading dose in the disc indicating the attainment of equilibrium concentration of levobunolol in the skin.

Administration, Cutaneous↗

PubMed1985

Long-term ocular hypotensive effect of levobunolol: results of a one-year study.

Data for the first 12 months are reported for an ongoing, multicentre, clinical study comparing the long-term, ocular hypotensive efficacy and safety of topical levobunolol (0.5% and 1%) and timolol (0.5%). This study was a double-masked trial testing 88 patients with chronic open angle glaucoma or ocular hypertension. During the 12-month period drops were instilled twice daily into both eyes after a washout of prestudy ocular hypotensive medication. The effect of the three treatments in reducing intraocular pressure (IOP) was similar. Mean IOP reductions over the 12 months averaged 7.2 mmHg for the 0.5% levobunolol group, 6.2 mmHg for the 1% levobunolol group, and 6.0 mmHg for the timolol group. Decreases in mean heart rate of up to 5 beats per minute were observed in the 0.5% levobunolol group, up to 8 beats per minute in the 1% levobunolol group, and up to 4 beats per minute in the timolol group. Several patients were removed from the study owing to side effects possibly related to levobunolol treatment.

Adult↗

PubMed1986

[Local subjective tolerance of levobunolol and metipranolol in a double-blind comparative study in patients with increased intraocular pressure].

We evaluated the ocular comfort of 0.5% levobunolol hydrochloride and 0.6% metipranolol hydrochloride ophthalmic solutions in a randomized, double-masked, paired-comparison clinical trial. The drugs were given twice daily for 7 days to 16 patients with open-angle glaucoma or ocular hypertension. Patients rated comfort in terms of the severity of burning and/or stinging. For both drugs, the severity rating of ocular discomfort was low, averaging between 1 and 2 on a scale of 0-10. At initial and follow-up visits, the mean severity rating of burning or stinging with metipranolol was 2, slightly greater than the mean score of 1 with levobunolol. At 55% (26 of 47) of the patient visits, the patients rated levobunolol as more comfortable than metipranolol. Metipranolol (Betamann; Mann) was rated as more comfortable than levobunolol at only 9% (4 of 47) of the patient visits. The duration of burning and stinging was also rated as longer lasting with metipranolol treatment than with levobunolol (Vistagan; Pharma-Allergan) treatment. Although little ocular discomfort was reported for either drug, the majority of the patients tested rated levobunolol the more comfortable of the two drugs.

Clinical Trials as Topic↗

PubMed1982

A clinical evaluation of the effects of topically applied levobunolol and timolol on increased intraocular pressure.

Data from two short-term double-masked studies using 24 and 16 subjects suggest that topically applied levobunolol safely and effectively treats open-angle glaucoma and ocular hypertension. The onset of effect of a single drop of 0.5% levobunolol occurred within the first hour, producing a maximal hypotensive effect of more than 8 mm Hg after two hours. An intraocular pressure deceased of greater than or equal to 2 mm Hg was still observed after 24 hours for both concentrations of levobunolol tested (0.5% and 1%). Intraocular pressure decreases of more than 9 mm Hg persisted during a one-month trial in which patients were treated twice daily, confirming the results obtained in the 24-hour study. Systemic effects of both timolol (0.5%) and levobunolol (0.5% and 1%) included a consensual intraocular pressure-decreasing effect in the untreated eye and clinically significant reductions in heart rate. Diastolic blood pressure was decreased at two and four hours after administration of 0.5% levobunolol.

Administration, Topical↗

PubMed1985

Levobunolol vs timolol for open-angle glaucoma and ocular hypertension.

A group of 162 patients with chronic open-angle glaucoma or ocular hypertension were treated twice daily for up to 15 months with one of the following topical ophthalmic solutions: 0.5% levobunolol, 1% levobunolol, or 0.5% timolol. Overall mean reductions in intraocular pressure were 8 mm Hg for patients receiving 0.5% levobunolol or timolol and 8.2 mm Hg for patients receiving 1% levobunolol. There were no significant differences between levobunolol and timolol in mean reductions in intraocular pressure, percent of patients with adequately controlled intraocular pressure, or life-table estimates of the probability of successful treatment.

Clinical Trials as Topic↗

PubMed1987

The effect of levobunolol on aqueous humor dynamics.

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. Aqueous flow was measured by fluorophotometry and total outflow facility by tonography. Aqueous flow decreased approximately 29% in the eyes treated with levobunolol. Total outflow facility and episcleral venous pressure measurements were similar in levobunolol-treated eyes and contralateral eyes treated with vehicle. A 36% decrease in intraocular pressure was observed in the levobunolol-treated eyes and a slight intraocular pressure reduction was seen in the vehicle-treated eyes. The results of this study indicate that, similar to timolol, levobunolol lowers intraocular pressure primarily by decreasing aqueous humour production.

Adrenergic beta-Antagonists↗

PubMed1994

A comparison of timolol maleate and levobunolol. Length of use per 5-ml bottle.

PURPOSE: The authors analyzed the actual length of use of commercially available 5-ml bottles of 0.5% timolol maleate (Timoptic) and 0.5% levobunolol (Betagan) among patients who routinely use topical beta-blockers (1 drop twice daily in both eyes) for glaucoma treatment. METHODS: Patients were randomized to receive two 5-ml bottles of either timolol or levobunolol in a double-blind fashion. The patients used the drops independently and the bottles in sequence. The dates were recorded when each of the two 5-ml bottles were used. Sixty patients were enrolled, 15 were excluded from the study, and the data from the remaining 45 were analyzed. RESULTS: There was a 21% greater length of use per 5-ml bottle among patients who were randomized to 0.5% timolol maleate (36.6 +/- 10.4 days) compared with 0.5% levobunolol (28.9 +/- 8.1 days) (P = 0.009). The length of use of the first bottle versus the second bottle was compared and was found not to be significantly different in either group. There was no statistical difference in intraocular pressure control among patients before and after the study. CONCLUSION: There is a markedly greater length of use of the 5-ml bottle of timolol compared with the 5-ml bottle of levobunolol. The difference is believed to be due to the configuration of the levobunolol's bottle tip and the vehicle used to deliver the drug. The data may be extrapolated to a substantial patient savings and should be considered in prescription recommendations.

Aged↗