Comparative efficacy of fixed dose combination of brinzolamide 1% and timolol 0.5% without versus with benzalkonium chloride following single ocular instillation in New Zealand white rabbits

Background: Benzalkonium chloride (BAK) is the most used preservative in topical ophthalmic formulations. BAK causes dry eye and trabecular meshwork degeneration. Hence, BAK-free formulations are desirable for chronic conditions like glaucoma. The objective of this study was to compare the efficacy of BAK-free versus BAK-containing ophthalmic suspension of fixed dose combination (FDC) of brinzolamide and timolol on their intraocular pressure (IOP) lowering effect following a single ocular instillation in New Zealand White (NZW) rabbits. Methods: Twelve normotensive NZW rabbits (male) between 9-12 months of age (3.4-4.4 kg) received a single ocular instillation (35 ml) in left eye of either ophthalmic suspension containing FDC of brinzolamide (1% w/v)/timolol (0.5% w/v) without BAK (n=6, test) or with BAK 0.01% w/v (n=6, reference). IOP was measured before ocular instillation (baseline) and at 2, 4, 6, 8 and 24 hours after instillation using a pneumatonometer. Change in IOP from baseline were calculated and analysed using repeated measures analysis of variance (ANOVA) followed by Bonferroni post-test for pairwise comparisons. Results: Significant IOP reduction (p<0.05) from baseline was seen in both test and reference groups, up to 6 hours after instillation. Maximum IOP reduction was 25.5% and 22.6% at 2 hours in the test and reference group respectively. No significant differences (p>0.05) were observed between the test and reference group for the change in IOP at all time points. Conclusions: BAK-free and BAK-containing ophthalmic suspension of FDC of brinzolamide 1% and timolol 0.5% after a single ocular instillation in normotensive NZW rabbits produces similar reductions in IOP.

Minimally invasive dissolving microneedles for ocular brinzolamide delivery / 药学学报

The permeation and pharmacodynamics of ocular drugs are influenced by the corneal barrier. Here, a hard-soluble drug, brinzolamide, was selected as the model drug and used for preparation of minimally invasive dissolving microneedles. Brinzolamide was dissolved in ethanol and polyvinylpyrrolidone (PVP) K90 was added and dissolved. The mixture solution was casted into the dissolving microneedles mold and dried and brinzolamide dissolving microneedles (BMN) were obtained after demolding. The stereoscopic and scanning electron microscopic images showed that BMN were conical needles with the height of 750 μm, the bottom diameter of 300 μm, and the inter-tip distance of 500 μm. The dissolving microneedles patch was composed of 10×10 arrays with the area of 1 cm2 and the high drug load of 7.3 mg·cm-2. BMN showed a rapid in vitro drug release with 93% accumulative release at 2 h and the high drug corneal permeation amount of 877 ± 105 μg. BMN exhibited the high mechanical strength of 0.32 N/needle, leading to easy rat corneal insertion with the depth of 200 μm. Moreover, BMN were rapidly dissolved in the cornea, and more importantly, the damaged cornea were quickly self-healed within 24 h. Animal experiments were approved by the Ethics Committee of Beijing Institute of Radiation Medicine, Academy of Military Medical and the experiments were conducted in accordance with relevant guidelines and regulations. Ocular minimally invasive dissolving microneedles have the advantages of corneal minimal wounds and rapid healing, high drug loading, and high permeability, favoring the treatment of ocular diseases.

Regression of macular edema with topical brinzolamide and nepafenac alone and identification of a novel gyrate atrophy mutation / Regressão de edema macular com o uso tópico de brinzolamida e nepafenac e identificação de uma nova mutação na atrofia girata

ABSTRACT Gyrate atrophy is a rare metabolic autosomal recessive disorder caused by ornithine aminotransferase enzyme deficiency that leads to characteristic progressive, degenerative chorioretinal findings. Patients complain mostly of low vision, night blindness, and peripheral vision loss. Posterior subcapsular cataract, myopia, choroid neovascularization, and intraretinal cysts may be accompanying factors related to vision loss. We encountered a patient with vision loss secondary to posterior subcapsular cataract and intraretinal cysts. After treatment with topical brinzolamide and nepafenac (and without any diet mo dification and/or supplementation), we observed 143- and 117-mm macular thickness resolutions with 2 and 1 Snellen lines of visual gain in his right and left eyes, respectively. Also, we detected a novel homozygous mutation in the ornithine aminotransferase gene: c.1253T>C (p.Leu418Pro). Carbonic anhydrase inhibitors and/or non-steroid anti-inflammatory drugs can control macular edema in patients with gyrate atrophy-associated intraretinal cysts. The genetic variants may also be a determinant in the responsiveness to the therapy type.

RESUMO A atrofia girata é um distúrbio autossômico recessivo metabólico raro causado pela deficiência da enzima ornitina ami notransferase, que leva a achados degenerativos coriorretinianos progressivos característicos. Os pacientes queixam-se principalmente de baixa visão, cegueira noturna e perda de vi são periférica. A catarata subcapsular posterior, a miopia, a neovascularização da coróide e os cistos intrarretinianos podem ser fatores associados à perda da visão. Encontramos um paciente com perda de visão secundária à catarata subcapsular posterior e cistos intrarretinianos. Após o tratamento com brinzolamida tópica e nepafenaco (e sem modificação e/ou suplementação da dieta), observamos resoluções de espessura macular de 143 e 117 mm e com 2 e 1 linhas de Snellen de ganho visual nos olhos direito e esquerdo, respectivamente. Além disso, detectamos uma nova mutação homozigótica no gene da ornitina aminotransfera se: c.1253T>C (p.Leu418Pro). Inibidores da anidrase carbônica e/ou drogas anti-inflamatórias não esteróides podem controlar o edema macular em pacientes com cistos intrarretinianos associados à atrofia girata. As variantes genéticas também podem ser determinantes na responsividade ao tipo de terapia.

Clinical Effectiveness of a Brinzolamide 1%-Brimonidine 0.2% Fixed Combination for Normal Tension Glaucoma in South Koreans

PURPOSE: This study evaluated the efficacy and safety of a brinzolamide 1%-brimonidine 0.2% fixed combination (BBFC) for normal tension glaucoma (NTG) in a South Korean population. METHODS: This study included 45 patients who were newly diagnosed with NTG and treated with BBFC as the first therapy from January 2016 through December 2016. The unilateral eye of NTG eyes of all patients were enrolled. If both eyes were eligible, the eye with the more severe glaucomatous change was selected. If the glaucomatous change was similar in both eyes, the right eye was selected. The patients received the BBFC twice a day. Diurnal intraocular pressure (IOP) was measured every 2 and 1/2 hours between 09:00 am and 04:30 pm. The IOP change with respect to body position (positional IOP) was measured at baseline and at 6 months after eyedrop instillation. Throughout the study, all side effects were recorded and monitored by the investigators. RESULTS: Ten patients were excluded due to an allergic reaction or follow-up loss. A total of 35 patients were enrolled in this study. The mean IOP was 15.32 ± 4.00 mmHg at baseline and 13.38 ± 3.30 mmHg at 6 months after BBFC instillation (p < 0.001). The IOP fluctuation decreased from 3.33 ± 3.10 to 2.35 ± 1.40 mmHg after BBFC instillation; however, the difference was not statistically significant (p = 0.150). The mean change in positional IOP showed a statistically significant reduction from 16.94 ± 3.18 to 14.80 ± 3.27 mmHg (p = 0.025). There was no serious adverse drug reaction except in three cases of allergic reaction. CONCLUSIONS: BBFC is effective for the reduction of mean IOP and positional IOP in NTG patients.

Clinical efficacy and safety of brinzolamide combined with travoprost in primary open-angle glaucoma / 中国生化药物杂志

Objective To investigate the clinical efficacy and safety of brinzolamide combined with travoprost in the treatment of primary open-angle glaucoma.Methods 112 cases(140 eyes)of open-angle glaucoma patients from March 2015 to March 2016 were selected and randomly divided into the group A and the group B 56 cases(70 eyes)in each group.The group A was treated with travoprost therapy,while the group B was given travoprost combined with brinzolamide treatment,the adverse reactions and clinical curative effects in the two groups were observed and compared during treatment.Results After two weeks,one months,three months and six months in the two groups intraocular pressure were significantly lower than those before treatment,the difference was statistically significant(P<0.05),but in two weeks,one months,three months and six months in the group B the intraocular pressure was significantly lower than that in the group A,the difference was statistically significant(P<0.05).After treatment,two groups of BUT and ST were decreased significantly lower than before treatment,the difference was statistically significant(P<0.05),but there was no significant difference between BUT and ST after treatment,two groups of corneal fluorescein staining and ocular; Bengal staining scores were all significantly higher than before treatment,the difference was statistically significant(P<0.05),however,there was no significant difference in corneal fluorescein staining and ocular surface of rose bengal staining between the two groups.There was no significant difference in the incidence of adverse reactions between the two groups.Conclusion Brinzolamide combined with travoprost can reduce the intraocular pressure of patients with primary open-angle glaucoma,but can reduce tear film stability,damage the cornea,conjunctiva,reduce tear secretion,there is some damage to the conjunctiva,cornea,similar with travoprost.

The clinical effect of the treatment of open-angle glaucoma and ocular hypertension in trevastatin and brinazolamine / 中国生化药物杂志

Objective To analyze the travoprost and brinzolamide for clinical effect of open-angle glaucoma and ocular hypertension in the treatment of persistent state.MethodsA total of 104 patients with open-angle glaucoma and ocular hypertension who were treated in our hospital from June 2014-2016 in June were randomly divided into control group and study group, each group had 52 cases.The control group were only treated by travoprost therapy, study group with travoprost combined with brinzolamide treatment, to study and analyze the efficacy of two groups.ResultsAfter treatment,the intraocular pressure improved,compared with before treatment,the difference was statistically significant(P<0.05).Visual acuity was significantly improved compared with before treatment,the difference was satistically significant(P<0.05).ConclusionFor open angle glaucoma and ocular hypertension patients combined with travoprost and brinzolamide treatment, patients can improve clinical curative effect, improve the visual acuity, it has practical value.

Effect of prophylactic intraocular pressure‑lowering medication (brinzolamide) on intraocular pressure after ranibizumab intravitreal injection: A case–control study.

Purpose: To observe the effect of prophylactic intraocular pressure (IOP)‑lowering medication (brinzolamide) on IOP after ranibizumab intravitreal injections (IVIs). Materials and Methods: This prospective case–control study included 352 eyes from 352 patients (1 eye per patient) who were treated with ranibizumab intravitreal injection and divided randomly into two groups. Two hundred and three patients in control group only received the ranibizumab IVI, but 149 patients in case group received one drop of prophylactic intraocular brinzolamide preinjection. The IOP was measured by noncontact tonometer before injection, at 10, 30, 120 min and 1 day after injection in a sitting position. Results: The mean IOP measured before injection, at 10, 30, 120 min and 1 day after injection individually were 15.79 ± 2.21 mmHg, 19.33 ± 4.86 mmHg, 16.64 ± 2.93 mmHg, 16.17 ± 3.13 mmHg, and 15.07 ± 2.55 mmHg in case group and were 15.82 ± 2.57 mmHg, 21.34 ± 5.88 mmHg, 18.17 ± 4.06 mmHg, 17.59 ± 4.42 mmHg, and15.48 ± 2.92 mmHg in control group. Comparing two groups, the mean increase on IOP was statistically significant at 10, 30, 120 min postinjection (P < 0.05). Conclusions: IVI of ranibizumab causes a considerable short‑term transient rise on IOP in most patients. The effect of prophylactic IOP‑lowering medication on IOP after IVIs can be statistically significant from 10 min to 2 h after IVIs.

Brinzolamide/timolol versus dorzolamide/timolol fixed combinations: A hospital‑based, prospective, randomized study.

Purpose: To compare the efficacy and tolerability of brinzolamide/timolol (BT) and dorzolamide/ timolol (DT) fixed combinations on intraocular pressure (IOP) reduction. Methods: Patients with primary open angle glaucoma or normal tension glaucoma were randomized to receive either BT or DT. IOPs were measured at baseline, 2 weeks, and 1, 2, and 3 months. The primary outcome measures were the mean change in IOP from baseline at each visit. Secondary outcome measures included the tolerability of each fixed combination. Results: Seventy‑three patients (73 eyes) were included; 37 eyes in BT group and 36 eyes in DT group. Baseline mean IOP were 24.14 ± 4.5 and 29.53 ± 6 mmHg for BT and DT, respectively (P < 0.001). Both BT and DT provided statistically significant mean IOP reductions from baseline values within each group at all study visits (P < 0.001). DT provided greater mean IOP reductions from baseline than BT at each visit which was statistically significant at 2 weeks (P = 0.037). Mean percentage of IOP reduction was 24.35% and 46.33% at 2 weeks (P < 0.001), and 24.65% and 47% at 3 months (P < 0.001) for BT and DT, respectively. Patients’ tolerability appeared to be better for DT than for BT with complete ocular comfort without any ocular adverse effects in 31 patients (81.1%) in DT group and 11 patients (29.7%) in BT group (P < 0.001). Conclusion: Both drops provide effective IOP reduction which was greater, and patients were more likely to achieve lower target pressures with DT than with BT.

The Efficacy of Brinzolamide 1%/Brimonidine 0.2% Fixed Combination in Normal Tension Glaucoma

PURPOSE: To evaluate the efficacy and safety of brinzolamide 1%/brimonidine 0.2% fixed combination (BBFC) in normal tension glaucoma (NTG) patients. METHODS: This prospective study included patients treated with brinzolamide 1% monotherapy, brimonidine 0.2% monotherapy or brinzolamide 1% and brimonidine 0.2% concomitant therapy, as well as newly diagnosed NTG patients. The enrolled patients who used brinzolamide 1% or brimonidine 0.2% switched to BBFC and newly diagnosed NTG patients were treated with BBFC. The patients receiving brinzolamide 1% or brimonidine 0.2% monotherapy or brinzolamide 1% and brimonidine 0.2% concomitant therapy switched antiglaucoma drugs to BBFC. Newly diagnosed NTG patients used BBFC as the first therapy. The study consisted of 1 screening/baseline visit and 3 follow-up visits conducted after 1, 4, 8, 12 and 24 weeks of treatment. Intraocular pressure (IOP), mean deviation value and adverse drug reactions were evaluated before treatment and after treatment with BBFC. RESULTS: The mean IOP in the brinzolamide 1% monotherapy group was 13.5 ± 1.6 mm Hg and the mean IOP after switched from brinzolamide 1% monotherapy to BBFC was 12.1 ± 1.5 mm Hg. The mean IOP in the brimonidine 0.2% monotherapy group was 14.2 ± 1.3 mm Hg and the mean IOP after switched from brimonidine 0.2% monotherapy to BBFC was 11.7 ± 1.5 mm Hg. The mean IOP was 11.9 ± 2.1 mm Hg in the brinzolamide 1% and brimonidine 0.2% concomitant therapy group and the mean IOP after switched from brinzolamide 1% and brimonidine 0.2% concomitant therapy to BBFC was 12.0 ± 1.1 mm Hg. The mean IOP and reduction rate were 10.7 ± 2.1 mm Hg and 35.5%, respectively,in the newly diagnosed NTG patients treated with BBFC. There was no serious adverse drug reaction causing ocular damage. CONCLUSIONS: BBFC provides a significant IOP reduction and is a safe antiglaucoma medication for NTG patients.

The Effects of Topical Carbonic Anhydrase Inhibitors on Nitric Oxide Production in Trabecular Meshwork Cells

PURPOSE: To investigate and compare the effects of topical carbonic anhydrase inhibitors on the production and expression of nitric oxide in cultured human trabecular meshwork cells (HTMC). METHODS: Primarily cultured HTMC were exposed to 0, 10, and 100 microM dorzolamide and brinzolamide using serum-deprived media for 3 days. Production of nitric oxide was assessed with Griess assay. Expressions of eNOS mRNA were assessed with RT-PCR. RESULTS: Both dorzolamide and brinzolamide increased the production of nitric oxide eNOS activity (p < 0.05). Dorzolamide had a more potent effect than brinzolamide on the production of nitric oxide and the expression of eNOS mRNA. CONCLUSIONS: Topical carbonic anhydrase inhibitors increased the production of nitric oxide, which was accompanied by increased eNOS activity. Dorzolamide had a more potent effect than brinzolamide on the production of nitric oxide and expression of eNOS mRNA in HTMC. The increased production of nitric oxide by topical carbonic anhydrase inhibitors involves mechanisms other than carbonic anhydrase inhibition.

Clinical efficacy of brinzolamideon mechanical contusion ocular trauma / 中国基层医药

Objective To observe clinical efficacy of brinzolamide on mechanical contusion ocular trauma . Methods 50 patients(57 eyes) of mechanical contusion ocular trauma were selected and divided into observation group and control group randomly and evenly ( 29 eyes in the observe group ,28 eyes in the control group ) .On the basis of mechanical contusion ocular trauma basic treatment for all the patients , the observing group was added brinzolamide ophthalmic suspension .Their vision , intraocular pressure and ERG were observed .Results The vision of patients in the observing group was obviously better than that in the control group (χ2 =4.49,P<0.05).Intraocular pressure in the observing group (14.88 ±0.83)mmHg was obviously lower than that in the control group (19.64 ± 2.30)mmHg(P<0.05).Sum of a-wave amplitude and sum of b-wave amplitude after treatment were better than those before treatment ,and those in the observing group were higher than theose in the control group ( observation group:ta =0.44,tb =0.24;the control group:[ ta =1.03,tb =0.32;between two grous:ta =3.35,tb =2.37,P<0.05 ) ] .Conclusion Using Brinzolamide ophthalmic suspension to treat mechanical contusion ocular trauma preven -tively can obviously improve patients′vision, control their intraocular pressure and promote the recovery of retinal function.It has positive clinical effect .

The Effect of Fixed Combination of Brinzolamide 1% and Timolol 0.5% in Normal-Tension Glaucoma

PURPOSE: We conducted a study to evaluate the effects of brinzolamide/timolol fixed combination (BTFC) in normal-tension glaucoma (NTG) patients. METHODS: We reviewed the records of 33 normal-tension glaucoma patients treated with BTFC in the unilateral eye. We measured intraocular pressure (IOP) every 2 and 1/2 hours between 09:00 am and 04:30 pm. After using BTFC at 8:00 am and 8:00 pm for 6 months, we measured the IOP at the same time period. We analyzed and compared the IOP of eyes treated with BTFC and contralateral eyes. RESULTS: The mean reduction in IOP was -2.85 +/- 1.43 mm Hg (-18.36 +/- 8.58%) in the eyes treated with BTFC and -2.21 +/- 1.73 mm Hg (-13.90 +/- 10.66%) in the contralateral eyes. The IOP lowering effect was greater in the eyes treated with BTFC than in the contralateral eyes. After 6 months of BTFC instillation, the changes in IOP measurements were the lowest at 11:30 am and increased at each time point afterwards. The greatest reduction in IOP was observed at 1 month; however, significant IOP reduction was observed at 3 and 6 months in both BTFC and contralateral eyes. There was no serious adverse event causing ocular damage. CONCLUSIONS: BTFC provided a significant IOP reduction in both BTFC and contralateral eyes in NTG patients.

Influence of topical carbonic anhydrase inhibitor on the expression of aquaporin-1 in rat cornea with neovascularization / 中华实验眼科杂志

Background Researches showed that aquaporin-1 (AQP1) is closely associated with corneal neovescularization(CNV).Carbonic anhydrase inhibitor has the inhibitory effect on the AQP1 and further suppresses the CNV.However,the systemic adverse effect of Carbonic anhydrase inhibitor limit its clinical application.Therefore,the influence of topical carbonic anhydrase inhibitor on CNV is concerned.Objective Present study was to investigate the effects of topical carbonic anhydrase inhibitors on the expression of AQP1 in rat cornea after alkali burn and explore its role in corneal neovascularization (CNV).Methods The alkali-burn animal models were established in 60 eyes of 30 clean Sprague Dawley rats by putting the filter paper soaked 1 mol/L NaOH solution at the central cornea for 40 seconds.1％ Brinzolamide was topically administered in the 30 eyes of 15 models (Brinzolamide group),and the normal saline solution was used at the same way in other 30 eyes of 15 rats (model group).The 10 eyes of 5 normal Sprague Dawley received the eye drops of normal saline solution as the normal control group.The corneal burning degree was graded on the Mahoney ' s criteria in the third day,and Ee ' s method was used to score the opacification of cornea and the CNV area was analyzed in 3,5,7,10 days under the slit lamp microscope.The cornea tissue was obtained in the tenth day after burning for the observation of the pathology under the light microscope and the ultrastructure under the transmission electron microscope.The expressions of AQP1 and vascular endothelial growth factor(VEGF) in cornea tissue were detected using immunohistochemistry.The use of animals complied with the Statement of ARVO.Results No significant difference was seen in the scores of rat corneal alkali burn between the model group and brinzolamide group( t=0.97,P＞0.05 ).The scores of corneal edema and opacification and neovascular area were lower in brinzolamide group compared with model group ( t =2.18,P＜0.05 ;t =6.58,P＜0.01 ).The pathological and ultrastructural examinations showed less CNV and inflammatory cells in rat corneal tissue of the brinzolamide group in comparison with model group.The grey values of VEGF were 84.92±9.49 and 78.18± 11.41,and those of AQP1 were 88.01 ± 11.03 and 58.10 ± 12.14 in the model group and brinzolamidegroup respectively,showing statistically significant differences ( VEGF:t =2.48,P =0.02 ; AQPI:t =9.99,P =0.00 ).Conclusions 1％ Brinzolamide suppresses alkali burn-induced CNV by downregulating the expressions of AQP1 and VEGF in cornea in rat.

Toxic Epidermal Necrolysis Induced by the Topical Carbonic Anhydrase Inhibitors Brinzolamide and Dorzolamide

Brinzolamide and dorzolamide are highly specific topical carbonic anhydrase inhibitors (CAIs). They lower intraocular pressure (IOP) by reducing the rate of aqueous humour formation without serious side effects. Although systemic CAIs are the most potent medications for lowering intraocular pressure for conditions with ocular hypertension, many cases with adverse systemic reactions have been reported, including Stevens-Johnson syndrome (SJS) and Toxic epidermal necrolysis (TEN). Here, we report 2 cases of TEN that were associated with topical CAIs rather than systemic CAIs.

The Efficacy of Topical 1%Brinzolamide (AzoptTM) as Combined Therapy of beta-blocker for Primary Open Angle Glaucoma and Ocular Hypertension

We investigated the effects of 1%brinzolamide on intraocular pressure (IOP)and peripapillary and optic nerve head (ONH)microcirculation with Heidelberg Retina Flowmeter (HRT)in primary open-angle glaucoma (POAG) and ocular hypertension. Primary open-angle glaucoma and ocular hypertension patients (60 eyes 60 person)were divided into 2 groups named A and B.In group A, patients had 1%brinzolamide and beta-blocker (30 eyes 30 person).In group B, patients had beta-blocker only (30 eyes 30 person).IOP and peripapillary and ONH microcirculation were measured before, 1 week, 2 weeks, 1 month, and 3 months after instillation and adverse effects were monitored. In group A, the rate of IOP decrease was 15.5%at 8:00 AM after 1 week of instillation, 17.6%at 4:00 PM after 1 week of instillation, 20.8%at 8:00 AM after 3 months of instillation, 20.8%at 4:00PM after 3 months of instillation, which were statistically significant.The adverse effects were rare including bitter tasting (3 eyes), transient visual disturbance (2 eyes), foreign body sensation (1 eye), etc.But there was no stastically significant change of microcirculation in both groups (P>0.05). We concluded that 1%brinzolamide had good effect for IOP decrease as an adjuvant medication to the beta-blocker.Moreover, long term and further evaluations are considered to be necessary.

Effects of pilocarpine and brinzolamide on rabbit ocular surface / 中国病理生理杂志

AIM:To evaluate the effects of pilocarpine, brinzolamide and the preservatives of them on corneal epithelial cells and the histopathology of rabbit conjunctiva. METHODS: Fifteen New Zealand white rabbits weighing 1.5 kg to 2.5 kg were randomly divided into three groups. One group with three rabbits served as untreated controls. Pilocarpine 1% and brinzolamide 1% each were administered to the right eyes in one treated group, and the preservatives (chlorobutanol 0.01% in pilocarpine, benzalkonium chloride 0.01% in brinzolamide) to the left eyes. Corneal epithelial damage was evaluated by scanning electron microscopy, and conjunctival specimens were examined under light microscopy. RESULTS: Compared with normal controls, brinzolamide and BAC caused corneal epithelium damage and increased number of inflammatory cells in the conjunctiva, while pilocarpine and the preservative chlorobutanol mainly influenced the corneal epithelium. Brinzolamide produced significantly more damage than pilocarpine (P

Efficacy of Intraocular Pressure Decrease and Safety after Topical 1%Brinzolamide (Azopt) Instillation on Normal Eyes

The aim of this study is to evaluate intraocular pressure (IOP)-lowering effects and side effects of 1%brinzolamide in its single use, and also in combined use with beta-blocker. Eighty normal eyes of 40 persons were randomized and divided into two groups: group A and B,20 persons each. In group A, patients had brinzolamide on unilateral eyes (subgroup A-1), and normal saline on the contralateral eyes (subgroup A-2). In group B, patients had 0.5% timolol and 1%brinzolamide on unilateral eyes and 0.5% timolol only on the contralateral eyes. IOP was measured before, 1/2,1,2,4 and 8 hours after instillation, respectively, and adverse effects were monitored. In both subgroups A-1 and B-1, the decrease of IOP was statistically significant compared with controls between 30minutes and 8 hours after instillation. Subgroup A-1 showed maximal decrease of IOP (22.2%) at 4 hours after instillation,while subgroup B-1 showed maximal decrease of IOP (48.3%) at 2 hours after instillation. Moreover,subgroup B-1 showed 12.1% of additional IOP-lowering effect on the average, compared with subgroup B-2. Out of the few adverse effects reported reported, bitter taste was the most common complaint. Brinzolamide might be used as a single agent or as an adjunct to betablocker for decreasing IOP in glaucoma patients. But further evaluation on more controls and patients of glaucoma or ocular hypertension through longer follow-up is required to support its clinical use.

The Effect of Short Term Use of Azopt in Normal Koreans

Azopt (brinzolamide ophthalmic suspension, 1%)is a carbonic anhydrase type II inhibitor,which reduces intraocular pressure by suppression of aque-ous humor production in ciliary process. It was developed as an agent which has little systemic side effect and was adjusted to physiologic ophthalmic environment. We observed the effect of intrao- cular pressure, pulsatile ocular blood flow and side effect to investigate the clinical effectiveness of Azopt in normal Azopt was instilled to 10 eyes of 10 volunteers and artificial tear was instilled to the other 10 eyes of 10 volunteers three times daily, respectively. We measured intraocular pressure by Goldman applanation tonometer at twohours, 8 hours, 1 day and 7 days after instillation. Pulsatile ocular blood flow, pupil diameter, blood pressure and pulse rate were also measured. Decrease of intraocular pressure after instillation of Azopt was statistically significant (p<0.05), compared with the pressure before instillation of Azopt and the decrease of pressure after instillation of artifical tear. No systemic side effect and ophthalmic discomfort was noted except for temporary visual blurring. Therefore we expect that Azopt will have a great effect on glaucoma patients in Korea who must be treated for long duration.