AIM:To evaluate the effect of brinzolamide-timolol fixed combination on intraocular pressure(IOP)after cataract surgery.METHODS:The study included 92 eyes of 87 patients who underwent cataract surgery and intraocular ...AIM:To evaluate the effect of brinzolamide-timolol fixed combination on intraocular pressure(IOP)after cataract surgery.METHODS:The study included 92 eyes of 87 patients who underwent cataract surgery and intraocular lens implantation.Patients scheduled for phacoemulsification were assigned to 1 of 2 groups.The treatment group received 1 drop of brinzolamide-timolol fixed combination immediately after surgery,and the control group received no treatment.The IOP was measured preoperatively and at 2h and 24h postoperatively.RESULTS:The mean IOP change was lower in the treatment group than in the control group at 2h postoperatively.The difference between the mean IOP values of the two groups at 2h postoperatively was found to be statistically significant.Twenty-four hours after the surgery,the mean IOP change was still higher in the control group when compared to the treatment group.CONCLUSION:The fixed combination brinzolamidetimolol can effectively reduce IOP after cataract surgery.展开更多
AIM：To investigate if significant improvement of optic disc blood flow（ODBF） occurs after instillation of brinzolamide onto rabbit eyes.METHODS：Testing of bilateral intraocular pressure（IOP） and left ODBF in 10 ...AIM：To investigate if significant improvement of optic disc blood flow（ODBF） occurs after instillation of brinzolamide onto rabbit eyes.METHODS：Testing of bilateral intraocular pressure（IOP） and left ODBF in 10 male rabbits took place every 3 h over a 24 h period.Brinzolamide（1% ophthalmic solution,two drops at 9：00 and 21：00） was administered to the left eye.ODBF,assessed using laser speckle flowgraphy,was determined as the mean blur rate（MBR）.Furthermore,the effect of brinzolamide on isolated rabbit ciliary arteries using isometric tension recording system was performed.RESULTS：After brinzolamide instillation,IOP was significantly decreased in the left eye.MBR-vessel was greater at 18：00 and 21：00（P〈0.05） than in the controls.MBRtissue and MBR-average were greater at 18：00（P〈0.05） than in the controls.For isolated arteries pre-contracted with a high-K solution,brinzolamide induced concentration-dependent relaxation,reaching 46.1%±9%（n=21） at 1 mmol/L.In Ca^2＋-free solutions,incubation with brinzolamide suppressed 1 μmol/L histamine-induced contractions（P〈0.05）.CONCLUSION：Brinzolamide decreases IOP and increases ocular blood flow.The direct vasodilatory effect of brizolamide is mediated by suppression of Ca^2＋ release from intracellular calcium stores.展开更多
Purpose: This is a retrospective, comparative, head-to-head, not commissioned study about the efficacy of bimato-prost 0.03%, brimonidine 0.2%, brinzolamide 1%, dorzolamide 2%, and travoprost 0.004%/timolol 0.5%-fixed...Purpose: This is a retrospective, comparative, head-to-head, not commissioned study about the efficacy of bimato-prost 0.03%, brimonidine 0.2%, brinzolamide 1%, dorzolamide 2%, and travoprost 0.004%/timolol 0.5%-fixed combinations in patients affected by na?ve open-angle glaucoma and IOP > 25 mmHg. Patients and Methods: Files from 70 patients (35 M, 35 F, mean age 69.52 y, S.D. 11.56, range: 37-87y) in our Glaucoma Service were retrospectively analyzed as long as 12 months. Every subgroup, including 14 age- and sex-matched patients, was allocated to 1 of the 5 groups of the fixed combinations monotherapy. Data recorded after 3 months follow-up were statistically analyzed by descriptive and ANOVA statistics as percentage of IOP reduction from baseline. Results: All the fixed combinations were effective in lowering IOP. The mean percentage reduction was: brimonidine/timolol 43.57%, dorzolamide/timolol 37.67%, bimatoprost/timolol 35.60%, travoprost/timolol 33.25% and brinzolamide/timolol 23.0%. The brimonidine/timolol fixed combination showed to be statistically significant more effective only than brinzolamide/timolol fixed combination (p = 0.001). Setting the α error to 5%, the power of the study is 26%, phi: 0.842. Discussion: In all this cohort of patients the target IOP was successfully achieved. All the fixed combinations used in this study had a very good profile of efficacy. Brimonidine, dorzolamide, bimatoprost and travoprost/timolol fixed combinations statistically significantly reduced the percentage of IOP from baseline (p = 0.001) more than brinzolamide/timolol fixed combination.展开更多
目的:研究曲伏前列素与布林佐胺联合治疗原发性开角型青光眼(primary open angle glaucoma,POAG)、高眼压症(ocular hypertension,OHT)及抗青光眼术后高眼压的降眼压疗效及安全性。方法:将48例52眼POAG,OHT,抗青光眼术后高眼压的患者纳...目的:研究曲伏前列素与布林佐胺联合治疗原发性开角型青光眼(primary open angle glaucoma,POAG)、高眼压症(ocular hypertension,OHT)及抗青光眼术后高眼压的降眼压疗效及安全性。方法:将48例52眼POAG,OHT,抗青光眼术后高眼压的患者纳入为期2mo的前瞻性、单向性、开放性研究。经药物洗脱期测量眼压基线值。用药后2,4,8,12wk测量眼压、视力、视野,观察眼部症状、体征及全身副作用。计算12wk时眼压≤17mmHg患者百分比。结果:患者基线眼压28.08±2.50mmHg,4次随访眼压(17.12±1.42,16.71±1.55,16.13±1.52,16.12±1.49)mmHg,眼压下降均值10.35mmHg,最大下降率45%。用药后眼压与基线眼压比较差值有非常显著意义(P<0.01),用药12wk时,眼压≤17mmHg的患者占64%。常见的不良反应是结膜充血,偶见轻微烧灼感,轻度味觉异常等,对角膜、泪膜、视力、视野、血压、心率均未影响。结论:曲伏前列素与布林佐胺联合应用降眼压的效果明显,安全性好。联合用药,眼压≤17mmHg患者所占百分比显著。展开更多
In this paper,brinzolamide(S)-isomer was synthesized from 3-(2-bromoacetyl)-5-chloro-2-thiophenesulfonamide over five-step reactions of reduction cyclization,N-alkylation,sulfamation,amino protecting and amination fir...In this paper,brinzolamide(S)-isomer was synthesized from 3-(2-bromoacetyl)-5-chloro-2-thiophenesulfonamide over five-step reactions of reduction cyclization,N-alkylation,sulfamation,amino protecting and amination firstly,in total yield of 23%.The structures were characterized by 1H NMR、MS.The mixture of brinzolamide and its(S)-isomer was analyzed by HPLC indicating the resolution factor was 3.022 between brinzolamide and its(S)-isomer through column selection and factor modulation.The e.e.value of synthesized brinzolamide(S)-isomer was 96.9%.展开更多
文摘AIM:To evaluate the effect of brinzolamide-timolol fixed combination on intraocular pressure(IOP)after cataract surgery.METHODS:The study included 92 eyes of 87 patients who underwent cataract surgery and intraocular lens implantation.Patients scheduled for phacoemulsification were assigned to 1 of 2 groups.The treatment group received 1 drop of brinzolamide-timolol fixed combination immediately after surgery,and the control group received no treatment.The IOP was measured preoperatively and at 2h and 24h postoperatively.RESULTS:The mean IOP change was lower in the treatment group than in the control group at 2h postoperatively.The difference between the mean IOP values of the two groups at 2h postoperatively was found to be statistically significant.Twenty-four hours after the surgery,the mean IOP change was still higher in the control group when compared to the treatment group.CONCLUSION:The fixed combination brinzolamidetimolol can effectively reduce IOP after cataract surgery.
基金Supported by Japan Society for the Promotion of Science(JSPS) Grant-in-Aid for Scientific Research(C)(No.25462750)
文摘AIM：To investigate if significant improvement of optic disc blood flow（ODBF） occurs after instillation of brinzolamide onto rabbit eyes.METHODS：Testing of bilateral intraocular pressure（IOP） and left ODBF in 10 male rabbits took place every 3 h over a 24 h period.Brinzolamide（1% ophthalmic solution,two drops at 9：00 and 21：00） was administered to the left eye.ODBF,assessed using laser speckle flowgraphy,was determined as the mean blur rate（MBR）.Furthermore,the effect of brinzolamide on isolated rabbit ciliary arteries using isometric tension recording system was performed.RESULTS：After brinzolamide instillation,IOP was significantly decreased in the left eye.MBR-vessel was greater at 18：00 and 21：00（P〈0.05） than in the controls.MBRtissue and MBR-average were greater at 18：00（P〈0.05） than in the controls.For isolated arteries pre-contracted with a high-K solution,brinzolamide induced concentration-dependent relaxation,reaching 46.1%±9%（n=21） at 1 mmol/L.In Ca^2＋-free solutions,incubation with brinzolamide suppressed 1 μmol/L histamine-induced contractions（P〈0.05）.CONCLUSION：Brinzolamide decreases IOP and increases ocular blood flow.The direct vasodilatory effect of brizolamide is mediated by suppression of Ca^2＋ release from intracellular calcium stores.
文摘Purpose: This is a retrospective, comparative, head-to-head, not commissioned study about the efficacy of bimato-prost 0.03%, brimonidine 0.2%, brinzolamide 1%, dorzolamide 2%, and travoprost 0.004%/timolol 0.5%-fixed combinations in patients affected by na?ve open-angle glaucoma and IOP > 25 mmHg. Patients and Methods: Files from 70 patients (35 M, 35 F, mean age 69.52 y, S.D. 11.56, range: 37-87y) in our Glaucoma Service were retrospectively analyzed as long as 12 months. Every subgroup, including 14 age- and sex-matched patients, was allocated to 1 of the 5 groups of the fixed combinations monotherapy. Data recorded after 3 months follow-up were statistically analyzed by descriptive and ANOVA statistics as percentage of IOP reduction from baseline. Results: All the fixed combinations were effective in lowering IOP. The mean percentage reduction was: brimonidine/timolol 43.57%, dorzolamide/timolol 37.67%, bimatoprost/timolol 35.60%, travoprost/timolol 33.25% and brinzolamide/timolol 23.0%. The brimonidine/timolol fixed combination showed to be statistically significant more effective only than brinzolamide/timolol fixed combination (p = 0.001). Setting the α error to 5%, the power of the study is 26%, phi: 0.842. Discussion: In all this cohort of patients the target IOP was successfully achieved. All the fixed combinations used in this study had a very good profile of efficacy. Brimonidine, dorzolamide, bimatoprost and travoprost/timolol fixed combinations statistically significantly reduced the percentage of IOP from baseline (p = 0.001) more than brinzolamide/timolol fixed combination.
文摘目的:研究曲伏前列素与布林佐胺联合治疗原发性开角型青光眼(primary open angle glaucoma,POAG)、高眼压症(ocular hypertension,OHT)及抗青光眼术后高眼压的降眼压疗效及安全性。方法:将48例52眼POAG,OHT,抗青光眼术后高眼压的患者纳入为期2mo的前瞻性、单向性、开放性研究。经药物洗脱期测量眼压基线值。用药后2,4,8,12wk测量眼压、视力、视野,观察眼部症状、体征及全身副作用。计算12wk时眼压≤17mmHg患者百分比。结果:患者基线眼压28.08±2.50mmHg,4次随访眼压(17.12±1.42,16.71±1.55,16.13±1.52,16.12±1.49)mmHg,眼压下降均值10.35mmHg,最大下降率45%。用药后眼压与基线眼压比较差值有非常显著意义(P<0.01),用药12wk时,眼压≤17mmHg的患者占64%。常见的不良反应是结膜充血,偶见轻微烧灼感,轻度味觉异常等,对角膜、泪膜、视力、视野、血压、心率均未影响。结论:曲伏前列素与布林佐胺联合应用降眼压的效果明显,安全性好。联合用药,眼压≤17mmHg患者所占百分比显著。
文摘In this paper,brinzolamide(S)-isomer was synthesized from 3-(2-bromoacetyl)-5-chloro-2-thiophenesulfonamide over five-step reactions of reduction cyclization,N-alkylation,sulfamation,amino protecting and amination firstly,in total yield of 23%.The structures were characterized by 1H NMR、MS.The mixture of brinzolamide and its(S)-isomer was analyzed by HPLC indicating the resolution factor was 3.022 between brinzolamide and its(S)-isomer through column selection and factor modulation.The e.e.value of synthesized brinzolamide(S)-isomer was 96.9%.
