Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new azopt research articles will be listed here shortly after becoming available to us.
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Medical research on azopt
Ophthalmology. 2008 Jun 4;
Kaback M, Scoper SV, Arzeno G, James JE, Hua SY, Salem C, Dickerson JE, Landry TA, Bergamini MV,
PURPOSE: To compare the safety and intraocular pressure (IOP)-lowering efficacy of brinzolamide 1%/timolol 0.5% fixed combination with brinzolamide 1% or timolol 0.5% alone in patients with open-angle glaucoma (OAG) or ocular hypertension (OHT). DESIGN: Randomized, double-masked, parallel group, multicenter study. PARTICIPANTS: Five hundred twenty-three patients were randomized to the study treatments. METHODS: Patients with OAG or OHT were recruited to the study. Qualifying eyes had IOPs of 24 to 36 mmHg at 8 am and 21 to 36 mmHg at 10 am on 2 eligibility visits after an appropriate washout period from previous treatment. Patients were assigned randomly to either brinzolamide 1%/timolol 0.5%, brinzolamide 1% (Azopt; Alcon Laboratories, Fort Worth, TX), or timolol 0.5%, dosed twice daily and were followed up while receiving therapy for 6 months. At selected sites, additional IOP measurements were performed at 12 pm, 4 pm, and 8 pm during the 2 eligibility visits, at month 3, and at month 6. MAIN OUTCOME MEASURE: Mean IOP. RESULTS: Brinzolamide 1%/timolol 0.5% produced statistically significant and clinically relevant reductions from baseline ranging from 8.0 to 8.7 mmHg, which were statistically and clinically superior to that of either brinzolamide 1% (5.1-5.6 mmHg) or timolol 0.5% (5.7-6.9 mmHg). No safety concerns were identified based on an assessment of ocular and cardiovascular parameters and a review of adverse events. CONCLUSIONS: Brinzolamide 1%/timolol 05% is superior in IOP-lowering efficacy to either brinzolamide 1% or timolol 0.5%.
Equine Vet J. 2008 May 12;
Germann SE, Matheis FL, Rampazzo A, Burger D, Roos M, Speiss BM
Reasons for performing study: Only few drugs with limited efficacy are available for topical treatment of equine glaucoma. Objective: To evaluate the effect of topical administration of 1% brinzolamide on intraocular pressure (IOP) in clinically normal horses. Methods: Healthy mature horses (n = 20) with normal ocular findings, were studied. The IOP was measured 5 times daily (7000, 1100, 1500, 1900 and 2300 h) over 10 days, On Days 1 and 2, baseline values were established. On Days 3-5 one eye of each horse was treated with one drop of 1% brinzolamide every 24 h immediately following the 0700 h measurement. On Days 6-8 the same eye was treated with 1% brinzolamide every 12 h (0700 and 1900 h). Measurements on Days 9 and 10 documented the return of IOP to baseline values. Statistical analysis of the data was performed. Results: In the treated eye a significant decrease in IOP compared to baseline values was noted during both the 24 and 12 h dosing periods (P
Curr Med Res Opin. 2008 Jun; 24(6): 1755-61
Holló G, Kóthy P
OBJECTIVE: To investigate if combined intraocular pressure (IOP)-lowering medication with travoprost/timolol fixed combination and a carbonic anhydrase inhibitor, brinzolamide, is superior to both travoprost monotherapy and travoprost/timolol fixed-combination therapy in primary open-angle glaucoma and ocular hypertension. METHODS: Following a 4-week wash-out period and using 4-week long treatment periods, 20 primary open-angle glaucoma or ocular hypertension patients were treated with evening travoprost 0.004%, then switched to evening travoprost 0.004%/timolol 0.5% fixed combination, and finally the treatment was combined with adjunctive twice-daily brinzolamide 1% ophthalmic suspension. Both eyes were treated, but only one eye per patient (the eye with the higher mean diurnal IOP at baseline), was evaluated. IOP was measured at 8 a.m., 12 noon and 4 p.m. at baseline and at the end of each treatment period. RESULTS: Mean diurnal IOP (mean (SD)) at baseline was 28.5 (7.3) mmHg which decreased to 22.3 (6.3) mmHg on travoprost, 19.2 (3.4) mmHg on travoprost/timolol fixed combination and 17.3 (3.4) mmHg when the brinzolamide was added to the travoprost/timolol combination (ANOVA, contrast test, p
Short-term effect of topical brinzolamide on human central corneal thickness.
Eur J Ophthalmol. 2008 May-Jun; 18(3): 338-40
Ornek K, Gullu R, Ogurel T, Ergin A
PURPOSE. To investigate the effect of short-term brinzolamide application on human central corneal thickness (CCT). METHODS. Seventeen eyes of 16 patients who underwent neodymium:YAG laser posterior capsulotomy were included in the study group. Twenty-two subjects served as controls. Brinzolamide twice daily and fluorometholone four times daily were initiated after the procedure. Corneal thickness was evaluated with an ultrasound pachymetry from the central region. CCT measurements were performed before the procedure, at first day, and at the end of first week. RESULTS. The mean baseline CCT value was 535.1+/-37.8 micronm. In comparison to the control group (546.4+/-22.2 micronm), there was no statistically significant difference (p=0.248). After brinzolamide instillation, the mean CCT values at first day and at first week was measured as 545.1+/-40.1 micronm and 538.8+/-39.4 micronm, respectively. The difference at first day was statistically significant when compared to the baseline values (p=0.00017). When compared to the control group, no statistically significant difference was observed for the mean CCT values of the first day and first week (p=0.906 and p=0.484, respectively). In the fellow eyes, mean CCT values increased following the dorzolamide instillation (529.3+/-42.6 micronm, 534+/-41.7 micronm, and 533+/-41.9 micronm, respectively). No statistically significant difference was observed between the control group and fellow eye group when compared (p=0.162, p=0.247, p=0.270, respectively). CONCLUSIONS. Brinzolamide may cause a short-term increase in the human CCT, particularly on the first day.
Comparison of ocular hypotensive effect and safety of brinzolamide and timolol added to latanoprost.
J Glaucoma. 2008 Apr-May; 17(3): 233-7
Miura K, Ito K, Okawa C, Sugimoto K, Matsunaga K, Uji Y
PURPOSE: To compare the ocular hypotensive effect and safety of brinzolamide and timolol added to latanoprost monotherapy. METHODS: In prospective randomized fashion, we evaluated the ocular hypotensive effect and safety of brinzolamide or timolol in 1 eye of 32 patients with primary open-angle glaucoma, normal-tension glaucoma, or ocular hypertension who had been treated with latanoprost for more than 1 month. Intraocular pressure (IOP), blood pressure, and pulse were measured before and at 4, 8, and 12 weeks. Corneal endothelial cell density was measured at baseline and at 12 weeks. RESULTS: The IOP was 17.8+/-1.7 mm Hg (mean+/-SD) before the addition of brinzolamide (n=15) and 15.7+/-2.1 mm Hg at 12 weeks (P
Curr Med Res Opin. 2008 May; 24(5): 1435-42
Day DG, Hollander DA
OBJECTIVE: To evaluate the efficacy and tolerability of brimonidine purite 0.1% in comparison to brinzolamide 1% when used as adjunctive therapy to latanoprost 0.005% in patients with glaucoma or ocular hypertension. METHODS: Randomized, single-center, investigator-masked, parallel-group clinical study. Patients with IOP >or= 18 mmHg while on once-daily latanoprost were randomized to adjunctive treatment with brimonidine purite TID (n = 20) or brinzolamide TID (n = 20) for 3 months. Intraocular pressure (IOP) was measured at 8 a.m., 10 a.m., and 4 p.m. at latanoprost-treated baseline and after 1 and 3 months of latanoprost and adjunctive therapy. A patient questionnaire was administered to evaluate the tolerability of eye drop instillation. RESULTS: Baseline mean diurnal IOP (+/- standard deviation, mmHg) on latanoprost was comparable between groups (brimonidine purite: 19.6 +/- 2.94; brinzolamide: 19.8 +/- 3.25; p = 0.846). Mean diurnal IOP at Month 3 was 16.3 +/- 2.63 mmHg with brimonidine purite and 17.8 +/- 2.19 mmHg with brinzolamide (p = 0.028). Adjunctive use of brimonidine purite provided greater IOP lowering than brinzolamide at 10 a.m. (p < 0.001) and 4 p.m. (p = 0.050) and equivalent IOP lowering to brinzolamide at 8 a.m. (p = 0.716). Blurred vision at Month 1 and bitter taste at Months 1 and 3 were more common upon instillation of brinzolamide eye drops. CONCLUSION: Brimonidine purite 0.1% provided significantly lower IOP compared with brinzolamide 1% when used as adjunctive therapy to latanoprost. Both adjunctive therapies were well tolerated. Limitations of this study include the use of a single site and the sample size. Additional studies are needed to further evaluate these drugs as adjunctive therapy to prostaglandin analogs.
Bestrophin-2 is involved in the generation of intraocular pressure.
Invest Ophthalmol Vis Sci. 2008 Apr; 49(4): 1563-70
Bakall B, McLaughlin P, Stanton JB, Zhang Y, Hartzell HC, Marmorstein LY, Marmorstein AD
PURPOSE: The bestrophin family of proteins has been demonstrated to generate or regulate Ca2+-activated Cl(-) conductances. Mutations in bestrophin-1 (Best1) cause several blinding eye diseases, but little is known about other bestrophin family members. This study involved disruption of the Best2 gene in mice. METHODS: The mouse Best2 gene was disrupted by replacing exons 1, 2, and part of exon 3 with a Lac Z. The expression profile of Bestrophin-2 (Best2) was examined using RT-PCR, X-gal staining, and immunohistochemistry. Intraocular pressure (IOP) was measured by anterior chamber cannulation. RESULTS: RT-PCR of mouse tissues revealed Best2 mRNA in eye, colon, nasal epithelia, trachea, brain, lung, and kidney. X-gal staining, confirmed expression in colon epithelia and in the eye, in the nonpigmented epithelia (NPE). Best2 was not expressed in RPE cells. Best2 protein was observed only in NPE and colon epithelia. The absence of Best2 had no obvious deleterious effect on the mice. However, the Best2-/- mice were found to have significantly (P < 0.02) diminished IOP with respect to the Best2+/+ and Best2+/- littermates. The Best2-/- and Best2+/- mice responded better to the carbonic anhydrase inhibitor brinzolamide than did their Best2+/+ littermates, although the beta-blocker timolol brought IOP to the same level, regardless of genotype. CONCLUSIONS: Best2 plays a role in the generation of IOP by regulating formation of aqueous humor, and inhibition of Best2 function represents an attractive new avenue for regulating IOP in individuals with glaucoma.
Br J Ophthalmol. 2008 Apr; 92(4): 500-4
Siesky B, Harris A, Cantor LB, Kagemann L, Weitzman Y, McCranor L, Marques C, Werne A, Stefansson E
AIMS: To assess the effects of brinzolamide and dorzolamide on ocular haemodynamics and retinal oxygen saturation in patients with primary open-angle glaucoma (OAG). METHODS: Fifteen patients with OAG were evaluated in a randomised, cross-over, double-blind study. They were treated with either brinzolamide or dorzolamide for 3 months and then crossed-over after a 4-week washout period. They were given timolol during a 4-week run-in period and during washout. The following were performed after run-in, after washout and after each treatment period: adverse events check, measurement of visual acuity, contrast sensitivity, blood pressure, heart rate, and intraocular pressure, and fundus examination. Ocular blood flow was assessed using confocal scanning laser Doppler flowmetry (HRF) and colour Doppler imaging (CDI). Retinal oxygenation levels were determined using a non-invasive measurement of haemoglobin oxygen saturation by digital photographic fundus oximetry. RESULTS: Both brinzolamide and dorzolamide reduced the number of zero-flow pixels in the retina as measured by HRF, suggesting an increase in retinal blood flow (-6.86 and -0.452 respectively) with brinzolamide treatment resulting in fewer zero-flow pixels than dorzolamide (-6.41) (p = 0.024). Both brinzolamide and dorzolamide increased oxygen saturation in the retina as measured by photographic retinal oximetry in the superior (0.82 (p = 0.002) and 0.87 (p = 0.005)) and inferior (0.88 (p = 0.035) and 0.82 (p = 0.002)) retinal veins. No significant changes were found in CDI measurements of the retrobulbar blood supply during either treatment. CONCLUSION: This pilot study suggests that brinzolamide and dorzolamide may increase retinal oxygen saturation in patients with OAG.
Bioorg Med Chem Lett. 2008 Apr 15; 18(8): 2669-74
Di Fiore A, Pedone C, Antel J, Waldeck H, Witte A, Wurl M, Scozzafava A, Supuran CT, De Simone G
Ethoxzolamide, an almost forgotten inhibitor of the metalloenzyme carbonic anhydrase (CA, EC 4.2.1.1), is the only classical inhibitor whose structure in adduct with any isoform was not reported yet. We report here the inhibition data of this molecule with the 12 catalytically active mammalian isozymes (CA I-CA XIV) and the X-ray crystal structure with the cytosolic, ubiquitous isoform CA II. These data are presumably useful for the design of novel CA inhibitors, targeting various CA isozymes, considering that ethoxzolamide was already the lead molecule to obtain the second generation inhibitors, dorzolamide and brinzolamide, clinically used antiglaucoma agents with topical action, as well as various other investigational agents.
J Med Case Reports. 2008; 2: 81
Cannon PS, Spencer AF, Lavin M
ABSTRACT: INTRODUCTION: Bleb needling is a recognised procedure in the management of patients with failing trabeculectomies. Suprachoroidal haemorrhage can occur as an unusual complication. We report a pseudophakic man who had early surgical intervention for this complication. This intervention may have contributed to the good recovery of his visual acuity and the minimum changes to his visual fields. CASE PRESENTATION: A 79-year-old pseudophakic man with chronic open angle glaucoma presented with further deterioration of his right visual field despite maximum medical therapy and a previous trabeculectomy. The right visual acuity was 6/9 with an intraocular pressure (IOP) of 16 mmHg. Bleb needling with 5-fluouracil was performed in a standard manner. His postoperative IOP was 6 mmHg. Thirty-six hours later the visual acuity was reduced to hand movements and two large choroidal detachments where observed clinically, which progressed to suprachoroidal haemorrhages. Five days after the initial needling, the patient had complex surgery involving anterior chamber reformation, a bleb compression suture and drainage of the haemorrhagic suprachoroidal detachments. Subsequently, the patient had a right vitrectomy with endolaser following a vitreous haemorrhage. The final visual acuity was 6/9 with an intraocular pressure of 8 mmHg on travoprost and brinzolamide. The final visual field showed little change when compared with the pre-suprachoroidal haemorrhage visual field. CONCLUSION: It is important to consider the possibility of delayed suprachoroidal haemorrhage as a complication in bleb needling, and early surgical intervention may be beneficial.