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Purpose: to conduct a comparative analysis of the clinical efficacy of a fixed combination of antihypertensive drugs: brinzolamide 1 % = timolol 0.5 % and dorzolamide 2 % = timolol 0.5 % for the prevention of intraocular hypertension in patients with silicone oil tamponade of the vitreal cavity.Patients and methods. The study was conducted in the Orenburg branch of S. Fyodorov Eye Microsurgery Federal State Institution during 2022. A retrospective analysis of case histories of 60 patients with retinal detachment and severe proliferative syndrome was carried out. All patients underwent subtotal vitrectomy. To prevent intraocular hypertension after tamponade of the vitreal cavity with silicone oil, patients were prescribed antihypertensive drugs: group 1 (n = 30) — a combination of brinzolamide 1 % = timolol 0.5 %; group 2 (n = 30) — dorzolamide 2 % = timolol 0.5 %. The therapeutic result was evaluated after 2 weeks, 1, 2 and 3 months. The observation included an ophthalmological examination, as well as a questionnaire to assess drug tolerance.Results. IOP after silicone oil tamponade and before the application of drugs had no statistically significant differences between the studied groups and amounted to 27.15 ± 3.56 mm Hg — in group 1 and 28.53 ± 5.99 mm Hg — in group 2. Both studied combinations provided a decrease in IOP, however, a more pronounced effect after 2 weeks of therapy with subsequent maintenance of a normal IOP level for 3 months was recorded in group 2 when using the dorzolamide / timolol combination, despite the appearance of minor discomfort during instillation. A decrease in IOP from baseline was found to be 43.5 % (p ≤ 0.01) with the combination dorzolamide/timolol and 33.3 % (p ≤ 0.01) for brinzolamide/timolol.Conclusion. The results of the study showed that both fixed combinations of drugs provide a decrease in IOP in patients after silicone tamponade, but the dorzolamide/timolol combination had a more pronounced therapeutic effect.

The purpose was to report the outcome after usage of three topical eyedrops combination, consisting of one steroid, one carbonic anhydrase inhibitor (CAI), and one non-steroidal anti-inflammatory drug (NSAID) in the treatment of pseudophakic cystoid macula edema (PCME) or Irvine–Gass syndrome. Treatment response monitoring of two patients with PCME to the combination of three eyedrops in a fixed dose regimen done using Optical Coherence Tomography. In both cases, significant improvement was documented within 1 week of starting the treatment, with respect to both visual acuity as well as central macular thickness and intraretinal fluid or cystoid macula edema (CME) resolution. The combination of three topical drugs of difluprednate (steroid), dorzolamide (CAI), and nepafenac (NSAID) is highly effective in treating select cases of pseudophakic CME and negates the need for usage of intravitreal (IVT) or posterior sub-Tenon’s injection of drugs such as triamcinolone acetonide, i.e., IVT triamcinolone acetonide, or posterior subtenon thus avoiding its associated complications.

Background. Glaucoma as one of the most common eye diseases can be a comorbid condition of an epithelial corneal defect of various etiologies. Maintaining an optimal level of ophthalmotonus includes the prescription of antiglaucoma drugs, including benzalkonium chloride-preserved drugs.The aim of the study. To compare the effect of antiglaucoma drugs, as well as benzalkonium chloride (BC), on a primary culture of human corneal epithelium and A549 immortalized cell line.Methods. The effect of brimonidine, dorzolamide and timolol (1/100, 1/50, 1/20 and 1/10 dilutions; exposure 24 hours) on a monolayer of a human corneal epithelial primary culture and A549 immortalized cell line was assessed by structural changes in cells (phase-contrast microscopy) and MTT assay data. The cytotoxic effect of BC was studied in concentrations corresponding to its content in these dilutions of the antiglaucoma drug. Using a model of a linear defect in the monolayer of a corneal epithelial primary culture and A549 immortalized cell line, the effects of brimonidine, dorzolamide and timolol (1/100 and 1/20 dilutions; exposure 48 hours) were assessed by cell migration activity.Results. Among drugs (BC-free), dorzolamide (1/50, 1/20 and 1/10 dilutions) causes minor structural changes in human corneal epithelium and A549 immortalized cell line; timolol (1/100, 1/50, 1/20 and 1/10 dilutions) causes minor structural changes in A549 immortalized cell line. Structural changes in both types of cells, a decrease in their metabolic and migration activity occur under the influence of dorzolamide, brimonidine and timolol (BC-preserved) in 1/100, 1/50, 1/20 and 1/10 dilutions. BC at the studied concentrations exhibits a similar effect.Conclusion. The cytotoxic effect of antiglaucoma drugs is caused by the presence of BC in their composition. Despite similar morphofunctional changes in cells, A549 immortalized cell line is more resistant to the effects of drugs than the human corneal epithelial primary culture. When using it as a cellular model, it is advisable to change the experimental conditions (duration of exposure and concentration of the studied drug).

Background: This case report is applicable to the field of ophthalmology because there is a paucity of medical literature related to the clinical presentation, diagnosis, and management of uveal effusion syndrome. This is an urgent concern because there are severe complications associated with this disease, including non-rhegmatogenous retinal detachment, angle closure glaucoma, and possible blindness. This report will fill clinical knowledge gaps using a patient example. Case presentation: A 68-year-old white male with multiple cardiovascular risk factors initially presented to the Eye Institute Urgent Care Clinic with new onset visual symptoms, including eye pain, eye lid swelling, redness, and tearing of his left eye. He had experienced a foreign body sensation in the left eye and bilateral floaters weeks prior to his presentation. The patient was examined, and vision was 20/30 in both eyes, and intraocular pressure was 46 in the right eye and 36 in the left eye. After initial assessment, including compression gonioscopy, intermittent angle closure glaucoma was suspected. He received oral diamox 500 mg, one drop of alphagan in both eyes, one drop of latanoprost in both eyes, one drop of dorzolamide in both eyes, and one drop of 2% pilocarpine in both eyes. There was only slight response in intraocular pressure. Owing to the bilateral angle closure, he underwent laser peripheral iridotomy to decrease intraocular pressure and open the angle that was found closed on gonioscopy. The patient was discharged on oral and topical glaucoma drops and scheduled for the glaucoma clinic. When he presented for follow-up in the glaucoma clinic, he was evaluated and noted to have bilateral narrow angles and intraocular pressure in the mid-twenties. A brightness scan (B-scan) was performed and was noted to have bilateral choroidal effusions, confirmed by Optos fundus photos. He was started on prednisone at 60 mg once per day (QD) with taper, continuation of oral and topical glaucoma medications, and a retina evaluation. Evaluation with a retina specialist showed resolving choroidal effusion in the left eye. He continued the prednisone taper as well as glaucoma drops as prescribed. Follow-up in the glaucoma clinic revealed a grade 3 open angle. He continued the prednisone taper, cosopt twice per day in both eyes, and discontinued brimonidine. The magnetic resonance imaging (MRI) that was performed showed results that were remarkable. No hemorrhage or mass was present. Follow-up with the retina specialist found that the choroidal effusions had resolved completely. Conclusion: This case report emphasizes the value in early detection, keen diagnostic evaluation, and cross-collaboration between multiple ophthalmology specialists to optimize healthcare outcomes for patients with uveal effusion syndrome. [ABSTRACT FROM AUTHOR]

A sustainable reversed-phase chromatographic method has been developed and validated for the simultaneous determination of three active pharmaceutical ingredients, dorzolamide, brinzolamide, and timolol, used to treat glaucoma. The eco-friendly solvent isopropanol has been used as an organic mobile phase constituent. According to the Hansen space green solvent selection tool, isopropanol has a G score of 6.5, comparable to ethanol, which has a G score of 6.6. The mobile phase consists of isopropanol: aqueous sodium acetate buffer (0.1 M, pH 4.25) in the ratio of 10:90 (v/v). The flow rate was maintained at 1 mL/min. Dorzolamide and brinzolamide were detected at 254 nm, and timolol was detected at 295 nm. A high-purity silica with a polymeric C18 modification column (150 × 4.6 mm, 5 µm particle size) was used for this separation. The three compounds were eluted within 8 min. The method was validated according to ICH guidelines. The calibration curves were linear in the range of 20–70 µg/mL, 40–140 µg/mL, and 20–70 µg/mL for dorzolamide, brinzolamide, and timolol, respectively. The LODs were found to be 1.61 µg/mL, 1.60 µg/mL, and 3.16 µg/mL for dorzolamide, brinzolamide, and timolol, respectively. Good accuracy and precision were obtained for the three compounds. The greenness and whiteness of the method were indicated using the AGREE, ChlorTox, and RGB12 tools. [ABSTRACT FROM AUTHOR]

Sepsis is a life-threatening condition caused by the dysregulated host response to infection. Novel therapeutic options are urgently needed and aquaporin inhibitors could suffice as aquaporin 5 (Aqp5) knockdown provided enhanced sepsis survival in a murine sepsis model. Potential AQP5 inhibitors provide sulfonamides and their derivatives. In this study, we tested the hypothesis that sulfonamides reduce AQP5 expression in different conditions. The impact of sulfonamides on AQP5 expression and immune cell migration was examined in cell lines REH and RAW 264.7 by qPCR, Western blot and migration assay. Subsequently, whether furosemide and methazolamide are capable of reducing AQP5 expression after LPS incubation was investigated in whole blood samples of healthy volunteers. Incubation with methazolamide (10−5 M) and furosemide (10−6 M) reduced AQP5 mRNA and protein expression by about 30% in REH cells. Pre-incubation of the cells with methazolamide reduced cell migration towards SDF1-α compared to non-preincubated cells to control level. Pre-incubation with methazolamide in PBMCs led to a reduction in LPS-induced AQP5 expression compared to control levels, while furosemide failed to reduce it. Methazolamide appears to reduce AQP5 expression and migration of immune cells. However, after LPS administration, the reduction in AQP5 expression by methazolamide is no longer possible. Hence, our study indicates that methazolamide is capable of reducing AQP5 expression and has the potential to be used in sepsis prophylaxis. [ABSTRACT FROM AUTHOR]

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Background: The mainstay of treatment in diabetic macular edema (DME) is intravitreal administration of anti-vascular endothelial growth factors (anti-VEGFs). Aqueous depressants may enhance the effects of anti-VEGF agents by prolonging their clearance via aqueous outflow. Purpose: To compare the anatomical and functional outcomes of treatment with intravitreal bevacizumab (IVB) and topical timolol–dorzolamide versus IVB alone. Method: In this randomized placebo-controlled clinical trial, patients with center-involving DME (ci-DME) and best corrected visual acuity (BCVA) of 20/30 or less were enrolled and randomly allocated to two treatment arms. One group received three monthly IVB injections and timolol–dorzolamide eye drops twice a day (IVB + TD group); the other group received three monthly IVB injections and artificial tear drops as placebo (IVB group). Patients underwent ophthalmic evaluations and macular optical coherence tomography scans at baseline and 1 month after the third injection. Result: Forty-six eyes from 46 patients with ci-DME were recruited. There was no intergroup difference regarding age, gender distribution, diabetic retinopathy stage, glycemic indices, BCVA, central macular thickness (CMT), or intraocular pressure at baseline. BCVA was significantly improved in the IVB + TD group (0.46 ± 0.18 to 0.36 ± 0.18 logarithm of the minimum angle of resolution [logMAR], p = 0.002), in contrast to IVB group (0.40 ± 0.17 to 0.35 ± 0.22 logMAR, p = 0.113). Similarly, the IVB + TD group showed a significant reduction in CMT (p < 0.001), unlike the IVB group (p = 0.086); and the CMT change in the former was greater than in the latter (− 0.57 ± 57.67 vs. − 25.52 ± 68.02 μm, p = 0.033). Conclusion: Our findings support the short-term effectiveness of topical timolol–dorzolamide as adjunctive therapy to IVB injections in managing center-involving DME in terms of anatomical and visual outcomes. Trial registration: Clinicaltrials.gov NCT05083689 (October 19, 2021). [ABSTRACT FROM AUTHOR]

Purpose: to determine the efficacy and safety of fixed latanoprost/dorzolamide combination Dorzoprost in hypotensive treatment of primary open-angle glaucoma (POAG) patients previously treated with latanoprost.Material and methods. An observational study included 30 patients (37 eyes) with moderate and advanced POAG who had uncompensated elevated IOP receiving latanoprost monotherapy. During the screening visit, latanoprost was switched to Dorzoprost instilled once in the evening. The targets were IOP, visual acuity, MD and PSD perimetry indices, retinal nerve fiber layer thickness, minimum width of the neuroretinal rim, macula retinal nerve fiber layer thickness, and adverse events. The observation period lasted 12 weeks. IOP was measured at weeks 4 and 12.Results. After 4 weeks, a statistically significant decrease in IOP was noted, which remained stable at 12 weeks. The average additional IOP decrease of those treated with Dorzoprost was 17%. Statistically insignificant positive changes were registered in visual acuity, static perimetry and optical coherence tomography. By the end of the observation period, 6 cases revealed a decrease in the degree of conjunctival hyperemia, while all dry eye syndrome cases (5 patients) showed a decrease in the severity of the signs of the syndrome.Conclusion. Dorzoprost has a significant additive hypotensive effect and a favorable safety profile.

Abstract Three smart carbon paste electrodes were fabricated to quantify dorzolamide hydrochloride DRZ, including conventional carbon paste I, modified carbon paste embedding Silica II, and modified carbon paste embedding β-cyclodextrin III. This study is based on the insertion of DRZ with phosphomolybdic acid to create an electroactive moiety dorzolamide-phosphomolybdate ion exchanger using a solvent mediator dibutyl phthalate. The three constructed carbon paste electrodes displayed Nernstian responses and linear concentration ranges with lower detection limits. The vital performance of the created electrodes was verified in relation to various parameters. The electrodes enhance the selective determination of DRZ in the presence of inorganic ions, a co-formulated drug in the dosage form timolol maleate, and the excipient benzalkonium chloride. The modified carbon paste electrode including Silica was utilized to detect DRZ in ophthalmic eye drop form utilizing the direct calibration curve and potentiometric titration methods. Satisfactory findings were achieved by comparing them to other reported methods.

Introduction: This multicenter, randomized, comparative, and investigator-masked crossover clinical trial sought to compare the efficacy and tolerability of fixed combinations of 0.1% brimonidine/0.5% timolol (BTFC) versus 1% dorzolamide/0.5% timolol (DTFC) as adjunctive therapies to prostaglandin analogues. Methods: A total of 110 patients with open-angle glaucoma or ocular hypertension previously treated with prostaglandin analogue monotherapy were randomized to receive either BTFC or DTFC as adjunctive therapy for 8 weeks. These patients were then crossed over to the alternative treatment arm for another 8 weeks. The reduction in intraocular pressure (IOP) (primary outcome), occurrence of adverse events, ocular discomfort after instillation, and patient preference (secondary outcomes) were recorded through patient interviews. Results: BTFC instillation for 8 weeks reduced IOP by 3.55 mmHg, demonstrating non-inferiority to DTFC instillation (3.60 mmHg; P < 0.0001, mixed-effects model). Although adverse events were rare with both combinations, patients reported greater discomfort with DTFC than with BTFC (P < 0.0001). More patients preferred BTFC (P < 0.0001) over DTFC, as BTFC caused minimal or no eye irritation. Conclusion: As BTFC offered better tolerability than DTFC with comparable reduction in IOP, we recommend it as an alternative for patients who experience ocular discomfort with DTFC-prostaglandin analogue combination therapy. Trial Registration Number: jRCTs051190125. Plain Language Summary: Patients with glaucoma who require further reduction in intraocular pressure while undergoing monotherapy with prostaglandin analogue ophthalmic solution have been prescribed two enhanced treatment options: 0.1% brimonidine/0.5% timolol fixed combination ophthalmic solution (BTFC) and 1% dorzolamide/0.5% timolol fixed combination ophthalmic solution (DTFC). The Aibeta Crossover Study Group in Japan compared the efficacy and tolerability of fixed combinations of BTFC versus DTFC when an additional fixed combination ophthalmic solution was prescribed in patients with open-angle glaucoma or ocular hypertension who had been treated with prostaglandin analogue monotherapy. We recruited 110 patients previously treated with prostaglandin analogue monotherapy at 20 clinical centers in Japan, then randomly assigned them to two alternative treatment groups: the BTFC to DTFC group or the DTFC to BTFC group, as an adjunctive therapy to prostaglandin analogues for total of 16 weeks. We compared the reduction in intraocular pressure, occurrence of side effects, eye discomfort after instillation, and patient preference between BTFC versus DTFC instillations. The intraocular pressure reduction of BTFC instillation was comparable to that of DTFC instillation, showing non-inferiority to DTFC (3.55 mmHg vs. 3.60 mmHg; P < 0.0001, mixed-effects model). Both eye drops caused few side effects; however, patients felt greater eye discomfort with DTFC than with BTFC (P < 0.0001). Because of less eye irritation, more patients preferred BTFC (P < 0.0001) over DTFC. We can recommend using BTFC for patients who feel eye discomfort with DTFC–prostaglandin analogue combination therapy. [ABSTRACT FROM AUTHOR]

The number of ophthalmic antihypertensive drugs available in Russia is steadily increasing, which complicates the choice to be made by ophthalmologist practitioners. Purpose: to compare the efficacy and safety of the domestically produced drug Latanoprost-Optic with the original drug Xalatan used as monotherapy or combined with the domestic drug Dorzolamide-Optic in patients with primary open-angle glaucoma (POAG). Material and methods. 116 completed cases of patients aged 69.3 ± 5.7 with newly diagnosed POAG were retrospectively analyzed, whereby we assessed the efficacy, safety and tolerability of monotherapy with Latanoprost-Optic or Xalatan and their combinations with Dorzolamide-Optic. Results. Latanoprost-Optic efficacy is no worse than that of Xalatan as it reduces intraocular pressure (IOP) by 33.8%, and has a comparable safety and tolerability profile. More than 72% of patients rate the tolerability of treatment with LatanoprostOptic as very good or good. An additional hypotensive effect of Dorzolamide-Optic added to latanoprost is 2.6–2.8 mm Hg, or 13.2–14.4% and involves no significant effect on the safety profile and tolerability of therapy. Conclusion. Latanoprost-Optic can be considered as a more affordable alternative to the original drug. If the target IOP values cannot be achieved by latanoprost alone, its combination with DorzolamideOptic is recommended, especially for patients with chronic diseases of the respiratory system and the cardiovascular system.

PurposeCarbonic anhydrase inhibitors (CAIs) reduce macular schisis in patients with X-linked retinoschisis (XLRS). The purpose of this study was to determine if CAIs reduce the incidence of complications from XLRS, including macular atrophy, retinal tears, and retinal detachment (RD), the most common causes of vision loss in patients with XLRS.MethodsFor this retrospective interventional case series, a chart review of patients examined at Cincinnati Children’s Hospital Medical Center [CCHMC] and Cincinnati Eye Institute [CEI] between 1/1/2015 and 1/16/2023 was performed. Male patients were included based on genetically-confirmed RS1 or typical clinical presentation with known family history of XLRS with at least two follow-up visits.ResultsTwenty-eight patients (56 eyes) with XLRS were included. There were 10 RS1 variants among the 21 genotyped patients. Median age at clinical diagnosis was 10.4 years old (range: 0.4–55.7 years) with median follow-up time of 4.7 years (range: 0.2–38.3 years). Median presenting Snellen visual acuity was 20/60 (logMAR 0.48, range: 0.18–3). In 26 eyes of 15 patients treated with CAIs, median CST pre-treatment was 416 microns (range: 198–701 microns), and median percentage decrease in CST on treatment was 21.8% (range: 0–74.5%) from highest pre-treatment CST. Reduction in CST with CAI use was statistically significant (p = 0.02), but not logMAR VA (p = 0.64). There was no significant difference in CST between patients treated with topical vs. oral CAI (p = 0.95) or between patients with partial or complete CAI adherence (p = 0.60). Ten eyes of seven patients had an RD requiring surgical intervention. No treated eyes developed new macular atrophy, peripheral retinoschisis, retinal tears, or RD; two eyes on topical CAIs had spontaneous resolution of bullous peripheral retinoschisis.ConclusionDuring the follow-up period, patients taking CAIs reduced macular schisis and did not experience new complications of macular atrophy, retinal tears, or RD. This is a relatively large cohort with long-term follow-up periods for patients with XLRS. Reduced macular schisis may not require perfect adherence with CAIs. A large, prospective, randomized, controlled clinical trial is needed to determine the potential of CAIs to improve visual function, reduce retinoschisis, and prevent RD.

Purpose: To report a case of acute onset unilateral hemorrhagic and serous choroidal effusion associated with dorzolamide administration and antiplatelet use that recurred in a patient who experienced a dorzolamide-induced choroidal effusion ten years prior to presentation. Observations: A 78-year-old male with a history of POAG in both eyes presented with sudden onset decreased vision and flashes of light in the left eye two days after escalating from timolol maleate 0.5% twice daily in both eyes to fixed combination dorzolamide-timolol 22.3–6.8 mg/mL twice daily in both eyes. Systemic medication included daily aspirin 81 mg for primary prevention of cardiovascular disease. Dilated fundus examination and B-scan ultrasound of the left eye revealed a hemorrhagic choroidal effusion in the nasal retinal periphery and low lying serous choroidal effusion in the temporal periphery. Complete resolution of the choroidal detachment was achieved in four days following prompt cessation of dorzolamide, and treatment with topical prednisolone acetate 1% four times daily and atropine 1% two times daily. Conclusions and importance: Topical dorzolamide may induce an idiosyncratic reaction leading to serous and hemorrhagic choroidal effusion, which can be exacerbated by antiplatelet use. Prompt recognition and management of drug-induced choroidal effusion can lead to improved visual outcomes and prevent long-term sequelae.

Three smart carbon paste electrodes were fabricated to quantify dorzolamide hydrochloride DRZ, including conventional carbon paste I, modified carbon paste embedding Silica II, and modified carbon paste embedding β-cyclodextrin III. This study is based on the insertion of DRZ with phosphomolybdic acid to create an electroactive moiety dorzolamide-phosphomolybdate ion exchanger using a solvent mediator dibutyl phthalate. The three constructed carbon paste electrodes displayed Nernstian responses and linear concentration ranges with lower detection limits. The vital performance of the created electrodes was verified in relation to various parameters. The electrodes enhance the selective determination of DRZ in the presence of inorganic ions, a co-formulated drug in the dosage form timolol maleate, and the excipient benzalkonium chloride. The modified carbon paste electrode including Silica was utilized to detect DRZ in ophthalmic eye drop form utilizing the direct calibration curve and potentiometric titration methods. Satisfactory findings were achieved by comparing them to other reported methods. [ABSTRACT FROM AUTHOR]

Purpose: To evaluate the impact of prostaglandin analogues (PGAs) on idiopathic epiretinal membrane (iERM) formation in glaucoma patients. Materials and Methods: Fifty-five eyes of 46 patients that were diagnosed with iERM following at least 6 months of glaucoma treatment were retrospectively analyzed and included in the study group. Age and sex matched control group of 60 patients was formed from random consecutive patients who were followed up in the glaucoma unit and had no ERM. A multivariate generalized linear model for adjusted analysis including hypertension, diabetes, pseudophakia, and different kinds of glaucoma medication was used to test the differences between the groups. Logistic regression (LR) analysis was used in the multivariate evaluations of the effects on iERM. Results: The use of PGAs was significantly higher in iERM group (p = 0.009). The use of Dorzolamide in the iERM group was significantly lower than that in the non-ERM group (p = 0.044). The coexistence of PGA use and systemic hypertension (HT) was significantly higher in the iERM group (p=0.035). The effect of PGAs was found to be statistically significant, and the odds ratio of its effect on iERM was found to be 2.932 (95% confidence intervals: 1.295-6.639, p=0.01) times in the LR analysis. Conclusions: The use of dorzolamide was significantly higher in the non-ERM group. The use of PGAs was significantly higher in the iERM group. Also, there was a significant relationship between PGAs and iERM formation. [ABSTRACT FROM AUTHOR]

Objectives: This study constructed dorzolamide (DRZ)-loaded ophthalmic implants for extended drug delivery and increased drug retention. Materials and Methods: Carboxymethyl cellulose (CMC) and chitosan (CHI) were used to describe the ophthalmic implants. The implants were prepared by the solvent casting technique in presence of polyethylene glycol 6000 (PEG 6000) as plasticizer. Physicochemical characterization studies including mechanical characteristics [tensile strength (TS), elongation at break, and Young's modulus], bioadhesion studies, and in vitro and ex vivo drug release studies were conducted. Results: TS of drug-loaded ophthalmic implants was 10.70 and 11.68 MPa, respectively. Elongation at break of CMC and CHI implants was 62.00% and 59.05%, respectively. The in vitro release profiles fit into Higuchi type kinetic model. Ex vivo release study results for both implants were correlated with in vitro release investigations. Conclusion: CMC and CHI-based implants provide extended drug delivery. Implants prepared using CMC provided a significantly slower in vitro release rate, and drug retention on ocular surfaces increased. Thus, it has been concluded that DRZ-loaded CMC implants could provide effective treatment for glaucoma. [ABSTRACT FROM AUTHOR]

The aim of this report was to present a case of bilateral choroidal detachment following treatment with topical therapy dorzolamide/timolol without history of previous surgery. An 86-year-old woman, with intraocular pressures of 40.00/36.00 mm Hg, was treated with preservative-free double therapy with dorzolamide/timolol. One week later, she presented with bilateral vision loss and irritative symptoms in the face, scalp, and ears, with well controlled pressures. The anterior exam showed LOCS III N4C3 cataracts, and the fundus and ultrasound exams revealed a bilateral infero-temporal choroidal detachment in the absence of neoplasia or other systemic cause. One week in absence of hypotensive treatment and receiving topical prednisolone, she showed reattachment of the choroidal detachment. Six months after cataract surgery, the patient remains stable, without choroidal effusion regression. Hipotensive treatment following chronic angle closure can lead to choroidal effusion similar to cases of acute angle closure treated with oral carbonic-anhydrase inhibitors. The combined strategy of removing hipotensive treatment and topical corticosteroids could be useful for the initial management of choroidal effusion. Also, performing cataract surgery after choroidal reattachment can help with stabilization.

Introduction: Glaucoma is an irreversible chronic eye disease in which intraocular pressure (IOP) control is important. This study aimed to assess the IOP-lowering effects and adherence scores between fixed combination dorzolamide/timolol maleate (FCDT) and non-fixed combination dorzolamide and timolol XE (NFDT) in open-angle glaucoma (OAG) patients. Methods: A randomised controlled trial in a parallel, single-blinded study involving 60 OAG patients was conducted. The patients were randomised into FCDT or NFDT based on a block randomisation technique. A pre-study run-in with Gutt timolol was administered for two weeks. IOP was assessed at baseline, month 1 and month 3, with a bottle weight measurement at month 3. Results: Only 55 OAG patients were analysed, with 8.4% dropping out. A statistically significant mean IOP reduction was observed in each group from baseline to month 1 (FCDT: mean difference [MD] = 4.93, 95% confidence interval [CI] = 4.00, 5.86); NFDT: MD = 4.92, 95% CI = 4.024, 5.82) and from baseline to month 3 (FCDT: MD 5.17, 95% CI = 4.19, 6.15; NFDT: MD = 4.85, 95% CI = 3.874, 5.82). The overall FCDT mean IOP was significantly lower by 1.02 mmHg (95% CI = -2.01, -0.02) than NFDT (F(1, 53) = 4.19; P = 0.046). A significant interaction was observed between time and treatment at month 3, with the mean IOP for FCDT being lower by 1.22 mg than for NFDT (P = 0.037). The mean adherence score was significantly higher in the FCDT group than in the NFDT group (t stat (df) = 3.88 (53); P < 0.001). The reduction in IOP between the groups became non-significant after adherence was adjusted (F(1, 52) = 2.45; P = 0.124). Conclusion: Both drugs showed a decrease in IOP but more so in FCDT. However, no difference was found in terms of medication adherence. An emphasis on treatment compliance is needed. [ABSTRACT FROM AUTHOR]

Three cases of stellate nonhereditary idiopathic foveomacular retinoschisis are presented with novel findings including the progressive nature of foveal involvement and the lack of response to topical dorzolamide and intravitreal bevacizumab. Optical coherence tomography angiography findings were similar to the uninvolved fellow eye, pointing to preserved vasculature despite distortions in anatomy. Purpose: To present novel findings in stellate nonhereditary idiopathic foveomacular retinoschisis, including the largest series of optical coherence tomography angiography findings to date. Methods: A retrospective case series with multimodal imaging was obtained and reviewed. Results: All three patients were women, aged 59–63. Two cases were unilateral, and one was bilateral. Vision ranged from 20/20 to 20/60 in the affected eyes. Peripheral retinoschisis was observed in all three patients. All patients were followed for a minimum of 1 year. In one case, progressive macular retinoschisis leading to foveal involvement was observed over two years, with an associated vision decline from 20/25 to 20/60. Attempted interventions included topical dorzolamide in all cases and intravitreal bevacizumab in one patient; however, no treatment effect was observed. The foveal avascular zone size was within normal limits (mean 280 µ m). In all stellate nonhereditary idiopathic foveomacular retinoschisis eyes, the retinoschisis cavities were nonvascular. Conclusion: Novel findings regarding stellate nonhereditary idiopathic foveomacular retinoschisis include the progressive nature of foveal involvement and the lack of response to topical dorzolamide and intravitreal bevacizumab. Foveal avascular zone was normal in all eyes, consistent with the relatively preserved vision in these cases. Retinoschisis cavities were nonvascular in all eyes, a finding which may give insight into the mechanism of this disease. [ABSTRACT FROM AUTHOR]

Ocular hypotony is one of the common complication post-filtering surgery. Common causes include bleb leakage, over-filtration, choroidal detachment, cyclodialysis cleft, inflammation, and retinal detachment. Here, we are reporting a rare case of hypotony following anti-glaucoma medications.

Two Shih-Tzu dogs with atopic dermatitis presented with delayed periocular dermatitis (PD) following the instillation of dorzolamide and dorzolamide/timolol combination eyedrops; the development of dermatologic signs took 94 and 104 d in cases 1 and 2, respectively. Hypersensitivity to anti-glaucoma eyedrops was highly suspected, and treatment was discontinued. Delayed PD was significantly relieved in cases 1 and 2, at days 155 and 64 after discontinuation, respectively. In this study, the clinical characteristics and progression of delayed PD were described to inform clinicians who may encounter this rare side effect. [ABSTRACT FROM AUTHOR]

Purpose: Impaired ocular blood flow is an important risk factor in the pathogenesis of open-angle glaucoma (OAG). Studies have reported that dorzolamide 2% may be effective in improving ocular blood flow (OBF) in OAG patients. The objective of this study was to determine the efficacy of dorzolamide 2% (DORZOX, Cipla Ltd.) in improving retrobulbar blood flow in an Indian setting.Methods: The study was conducted as an interventional pilot project in 24 healthy subjects and 19 OAG patients. Baseline OBF measurements were done for all glaucoma patients with color Doppler imaging (CDI). Baseline ocular perfusion pressure (OPP) was calculated for all participants. Glaucoma patients were given dorzolamide 2% thrice daily for 12 weeks. The primary efficacy endpoints were mean changes in the CDI parameters of the retrobulbar vessels and OPP posttreatment. The secondary endpoint was mean change in the intraocular pressure (IOP) and adverse events, if any.Results: In comparison to healthy subjects, glaucoma patients displayed significantly reduced baseline OPP (P = 0.002). Treatment with dorzolamide 2% for 12 weeks led to a significant increase in OPP (P < 0.001) and a significant increase in end diastolic velocity (EDV) in all major ophthalmic arteries like ophthalmic artery (OA), central retinal artery (CRA), and short posterior ciliary artery (SPCA) (P < 0.001, P = 0.04, and P = 0.0075, respectively). A significant reduction in the intraocular pressure (IOP; P = 0.007) was observed posttreatment, with no adverse events reported.Conclusion: Dorzolamide 2% significantly improved parameters such as the EDV and OPP in major ophthalmic arteries. This pilot study shows promising results on using dorzolamide for treating Indian patients with OAG. [ABSTRACT FROM AUTHOR]

Purpose: Impaired ocular blood flow is an important risk factor in the pathogenesis of open-angle glaucoma (OAG). Studies have reported that dorzolamide 2% may be effective in improving ocular blood flow (OBF) in OAG patients. The objective of this study was to determine the efficacy of dorzolamide 2% (DORZOX, Cipla Ltd.) in improving retrobulbar blood flow in an Indian setting. Methods: The study was conducted as an interventional pilot project in 24 healthy subjects and 19 OAG patients. Baseline OBF measurements were done for all glaucoma patients with color Doppler imaging (CDI). Baseline ocular perfusion pressure (OPP) was calculated for all participants. Glaucoma patients were given dorzolamide 2% thrice daily for 12 weeks. The primary efficacy endpoints were mean changes in the CDI parameters of the retrobulbar vessels and OPP posttreatment. The secondary endpoint was mean change in the intraocular pressure (IOP) and adverse events, if any. Results: In comparison to healthy subjects, glaucoma patients displayed significantly reduced baseline OPP (P = 0.002). Treatment with dorzolamide 2% for 12 weeks led to a significant increase in OPP (P < 0.001) and a significant increase in end diastolic velocity (EDV) in all major ophthalmic arteries like ophthalmic artery (OA), central retinal artery (CRA), and short posterior ciliary artery (SPCA) (P < 0.001, P = 0.04, and P = 0.0075, respectively). A significant reduction in the intraocular pressure (IOP; P = 0.007) was observed posttreatment, with no adverse events reported. Conclusion: Dorzolamide 2% significantly improved parameters such as the EDV and OPP in major ophthalmic arteries. This pilot study shows promising results on using dorzolamide for treating Indian patients with OAG.

Aim and Objective: To compare the efficacy and safety of brinzolamide1% and timolol0.5% fixed combination eye drops versus dorzolamide2% and timolol0.5% fixed combination eye drops in the treatment of primary open-angle glaucoma. Design: Prospective, randomized, comparative, interventional study. Setting: Tertiary eye care centre. Material and Method: The present study was a comparative study carried out on patients visiting OPD of Ophthalmology Department and diagnosed with primary open-angle glaucoma. Group 1 (n-30 BT) received brinzolamide1% and timolol0.5% fixed combination eye drops, and Group 2 (N-30 DT) patients received dorzolamide2% and timolol0.5% fixed combination eye drops. A complete ophthalmic examination was performed, including Goldmann applanation tonometry. IOP was measured twice daily (9 AM and 4 PM). The patients were evaluated at 2, 4, 8, and 12 weeks. IOP was measured at follow-up. Side effects and tolerability of both drugs were assessed, and patient preference for drugs was noted. Results: Mean reduction in morning IOP was significantly more in Group 1 than in Group 2 at 8 weeks and 12 weeks (p < 0.05). Mean reduction in evening IOP was significantly more in Group 1 than in Group 2 at all follow-ups (p < 0.05). Conclusion: Brinzolamide1% + timolol0.5% fixed drug combination is more preferred and effective in lowering IOP than dorzolamide2% + timolol0.5% fixed drug combination in patients of primary open-angle glaucoma.

Simple Summary: Carbonic anhydrase inhibitors such as dorzolamide, brinzolamide, and acetazolamide are prescription drugs prohibited in sports. Detecting these substances and their biomarkers of consumption in urine and hair is crucial to documenting misuse in doping. We quantified dorzolamide, brinzolamide, acetazolamide, and their metabolites in the urine and hair of 88 patients under treatment, and samples of the patients' relatives were analyzed to assess potential for accidental exposure. We found that cutoff concentrations of urinary dorzolamide and brinzolamide are necessary to preclude false positives due to contamination or passive exposure. Additionally, we reported the first concentrations of brinzolamide in hair. Carbonic anhydrase inhibitors (CAIs) are prescription drugs also used in doping to dilute urine samples and tamper with urinalyses. Dorzolamide, brinzolamide, and acetazolamide are prohibited by the World Anti-Doping Agency. Detecting CAIs and their metabolites in biological samples is crucial to documenting misuse in doping. We quantified dorzolamide, brinzolamide, acetazolamide, and their metabolites in the urine and hair of 88 patients under treatment for ocular hypertension or glaucoma. Samples of the patients' relatives were analyzed to assess potential for accidental exposure. After washing, 25 mg hair was incubated with an acidic buffer at 100 °C for 1 h. After cooling and centrifugation, the supernatant was analyzed by ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). Urine (100 μL) was diluted and centrifuged before UHPLC-MS/MS analysis. Run time was 8 min through a reverse-phase column with a mobile phase gradient. MS/MS analysis was performed in a multiple-reaction monitoring mode after positive electrospray ionization. Median urinary concentration was 245 ng/mL (IQR: 116.2–501 ng/mL) for dorzolamide, 81.1 ng/mL (IQR: 35.9–125.3 ng/mL) for N-deethyl-dorzolamide, 0.77 ng/mL (IQR: 0.64 ng/mL–0.84 ng/mL) for N-acetyl-dorzolamide, 38.9 ng/mL (IQR: 20.4–79.2 ng/mL) for brinzolamide, and 72.8 ng/mL (IQR: 20.7–437.3 ng/mL) for acetazolamide. Median hair concentration was 0.48 ng/mg (IQR: 0.1–0.98 ng/mg) for dorzolamide, 0.07 ng/mg (IQR: 0.06–0.08 ng/mg) for N-deethyl-dorzolamide, 0.40 ng/mL (IQR: 0.13–1.95 ng/mL) for brinzolamide. Acetazolamide was detected in only one hair sample. Dorzolamide and brinzolamide were detected in the urine of three and one relatives, respectively. Cutoff concentrations of urinary dorzolamide and brinzolamide are necessary to preclude false positives due to contamination or passive exposure. We reported the first concentrations of brinzolamide in hair. [ABSTRACT FROM AUTHOR]

Early November 2020 an Olympic gold medal winner returned during an out‐competition control an adverse analytical finding for dorzolamide, a diuretic mostly used to treat glaucoma. Estimated urine concentrations were 2.2 and 1.6 ng/ml in the A and B specimens, respectively. As the athlete denied any use of dorzolamide, a complex forensic investigation was suggested. It revealed that the athlete was severely injured during a car crash 6 months before where he received 2× 500 ml of red blood cells transfusion. One of the blood donors declared using dorzolamide. A plasma aliquot, stored for legal purposes, was tested by LC‐MS/MS several months later and contained 4.3 ng/ml of dorzolamide. Given the very long half‐life of the drug, up to 150 days and its reported incorporation into erythrocyte, it was accepted by the French antidoping administration (AFLD) that the source of contamination was this blood transfusion and that the antidoping rule violation was unintended. [ABSTRACT FROM AUTHOR]

The aim of this report was to present a case of bilateral choroidal detachment following treatment with topical therapy dorzolamide/timolol without history of previous surgery. An 86-year-old woman, with intraocular pressures of 40.00/36.00 mm Hg, was treated with preservative-free double therapy with dorzolamide/timolol. One week later, she presented with bilateral vision loss and irritative symptoms in the face, scalp, and ears, with well controlled pressures. The anterior exam showed LOCS III N4C3 cataracts, and the fundus and ultrasound exams revealed a bilateral infero-temporal choroidal detachment in the absence of neoplasia or other systemic cause. One week in absence of hypotensive treatment and receiving topical prednisolone, she showed reattachment of the choroidal detachment. Six months after cataract surgery, the patient remains stable, without choroidal effusion regression. Hipotensive treatment following chronic angle closure can lead to choroidal effusion similar to cases of acute angle closure treated with oral carbonic-anhydrase inhibitors. The combined strategy of removing hipotensive treatment and topical corticosteroids could be useful for the initial management of choroidal effusion. Also, performing cataract surgery after choroidal reattachment can help with stabilization. [ABSTRACT FROM AUTHOR]

This study was aimed to evaluate the prophylactic anti-glaucoma effect of topical 5% betaxolol (BTX) and 2% dorzolamide (DRZ) on the second eye in dogs with unilateral primary angle closure glaucoma (PACG). Medical records of 60 dogs with unilateral PACG who received prophylactic anti-glaucoma eyedrops in the second eye, from 2016 to 2021, were reviewed. The prophylactic effects of BTX were maintained on 28/60 (46.7%) eyes until last visit and BTX failure was observed on median 510 (range, 53-1,927) days in 32/60 (53.3%) eyes. After DRZ instillation in BTX failure eyes, the prophylactic effects were extended at median 610 (range, 157-2,270) days in 21/32 (65.6%) eyes. DRZ failure eyes (17/21, 81.0%) eyes required chemical ablation or surgical intervention due to uncontrolled intraocular pressure. The duration of prophylactic effects was decreased with aging (R2 = 0.334, p = 0.006). The predominant breeds were Shih-Tzu (41.9%) and American Cocker Spaniel (30.6%) with no significant differences in survival curves (p = 0.210). The average prophylactic effects of BTX persisted more than 1.5 year and could be selected the first prophylactic eye drop in unilateral PACG. Also, early surgical intervention should be considered in prophylactic medications failure cases. [ABSTRACT FROM AUTHOR]

AIM: To study the effect of topical dorzolamide 2% on macular thickness reduction in diabetic cystoid macular edema (CME). METHODS: This was a prospective, non-randomized, open study including eyes with diabetic macular edema (DME). All eyes received topical dorzolamide 2% three times daily for one month. Changes in best-corrected visual acuity (BCVA), and central macular thickness (CMT) by optical coherence tomography) were evaluated at 1wk, 1, and 3mo post-treatment. RESULTS: Ninety-three eyes (84 patients) were included. Mean±SD (logMAR) BCVA improved significantly from 1.08±0.26 pretreatment to 0.66±0.24 at 1mo and 0.87±0.26 at 3mo post-treatment (P

Abstract Background Long-term use of topical, especially benzalkonium chloride (BAC)-preserved, antiglaucoma medications can cause a negative impact on the ocular surface. The aim of the study was to assess the effect of topical carbonic anhydrase inhibitors (CAIs) on selected oxidative stress biomarkers in the tear film. Methods The patients were divided into four sex-matched groups: group C (n = 25) – control group – subjects who did not use topical antiglaucoma medications, group DL (n = 14) – patients using preservative-free dorzolamide, group DL + BAC (n = 16) – patients using topical BAC-preserved dorzolamide, group BL + BAC (n = 17) – patients using BAC-preserved brinzolamide. Subjects in all the study groups have been using the eye drops two times daily for 6–12 months. The oxidative stress biomarkers in the tear film samples were measured: total protein (TP) concentration, advanced oxidation protein products (AOPP) content, total sulfhydryl (-SH) groups content, the activity of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), as well as Total Oxidant Status (TOS), Total Antioxidant Response (TAR), and Oxidative Stress Index (OSI). Results The advanced oxidation protein products content, Total Oxidant Status as well as superoxide dismutase and catalase activities in the group DL + BAC and BL + BAC were higher in comparison with the group C. The total sulfhydryl groups content was lower in the group DL + BAC and BL + BAC when compared to group C. Oxidative Stress Index was higher in the groups DL + BAC and BL + BAC in comparison with the groups DL and C. Conclusions Use of topical benzalkonium chloride-preserved carbonic anhydrase inhibitors increases oxidative stress in the tear film.

Glaucoma is the second leading cause of blindness in the world. Despite the fact that many treatments are currently available for eye diseases, the key issue that arises is the administration of drugs for long periods of time and the increased risk of inflammation, but also the high cost of eye surgery. Consequently, numerous daily administrations are required, which reduce patient compliance, and even in these conditions, the treatment of eye disease is too ineffective. Micellar polymers are core–shell nanoparticles formed by the self-assembly of block or graft copolymers in selective solvents. In the present study, polymeric micelles (PMs) were obtained by dialysis from smart biocompatible poly(ε-caprolactone)-poly(N-vinylcaprolactam-co-N-vinylpyrrolidone) [PCL-g-P(NVCL-co-NVP)] graft copolymers. Two copolymers with different molar masses were studied, and a good correlation was noted between the micellar sizes and the total degree of polymerisation (DPn) of the copolymers. The micelles formed by Cop A [PCL120-g-P(NVCL507-co-NVP128)], with the lowest total DPn, have a Z-average value of 39 nm, whereas the micellar sizes for Cop B [PCL120-g-P(NVCL1253-co-NVP139)] are around 47 nm. These PMs were further used for the encapsulation of two drugs with applications for the treatment of eye diseases. After the encapsulation of Dorzolamide, a slight increase in micellar sizes was noted, whereas the encapsulation of Indomethacin led to a decrease in these sizes. Using dynamic light scattering, it was proved that both free and drug-loaded PMs are stable for 30 days of storage at 4 °C. Moreover, in vitro biological tests demonstrated that the obtained PMs are both haemo- and cytocompatible and thus can be used for further in vivo tests. The designed micellar system proved its ability to release the encapsulated drugs in vitro, and the results obtained were validated by in vivo tests carried out on experimental animals, which proved its high effectiveness in reducing intraocular pressure. [ABSTRACT FROM AUTHOR]

Objectives. Nab-paclitaxel is a chemotherapeutic drug used to treat various solid malignant tumors. It was conceived with a solvent free formulation to overcome toxicity events and hypersensitivity reactions associated with paclitaxel. However, it still carries ocular adverse effects. The present review examines nab-paclitaxel related cystoid macular edema (CME) and the available therapeutic options. Materials and Methods. The literature was reviewed on nabpaclitaxel related CME on published articles through January 2021 using the keywords “nab-paclitaxel “and “cystoid macular edema”. Results. Bilateral CME is found in patients in treatment with nabpaclitaxel and causes considerable visual acuity decline. In ophthalmology multimodal imaging has an integral role in the diagnostic work up of patients and shows characteristic findings in nab-paclitaxel related CME. The case of a patient with treatment for bilateral CME is presented and analyzed. Conclusions. The preferred management strategy for nab-paclitaxel- related CME is drug cessation that leads to complete resolution of edema. When discontinuation of treatment is not possible due to the systemic conditions of patients, effective alternative therapeutic modalities are topical dorzolamide or steroidal treatment. Given the higher complication hazards of intravitreal therapy topical treatment should be preferred owing to comparable efficacy. [ABSTRACT FROM AUTHOR]

Abstract Background Cystoid macular edema is a rare, vision-threatening side effect of the taxane family of anticancer agents. There is no established treatment or standard treatment protocol for taxane-related cystoid macular edema. Here, we report two cases of taxane-related cystoid macular edema that were treated with topical dorzolamide. Case presentation In case 1, a 72-year-old Japanese woman with bilateral geographic choroiditis reported for a follow-up visit with a complaint of blurred vision in both eyes for 2 months after starting nanoparticle albumin-bound paclitaxel chemotherapy for multiple metastases of her breast cancer. Her best-corrected visual acuity had dropped from 1.2 to 0.9 in the right eye and from 1.0 to 0.4 in the left eye. Fundus examination showed no newly active geographic choroiditis lesion, but optical coherence tomography exhibited cystoid macular edema. We suspected taxane-related cystoid macular edema and terminated nanoparticle albumin-bound paclitaxel, and started topical dorzolamide treatment. Cystoid macular edema nearly resolved within 6 weeks in the right eye and within 10 weeks in the left eye after starting topical dorzolamide treatment. The resolution of cystoid macular edema without leaving a chorioretinal scar after discontinuation of paclitaxel confirmed our initial diagnosis of taxane-related cystoid macular edema. A few inconspicuous cystoid spaces persisted at the parafovea for a year after dorzolamide treatment ended, but regressed after restarting dorzolamide treatment without any side effects. Best-corrected visual acuity improved to 1.2 in the right eye and 1.0 in the left eye. In case 2, a 70-year-old Japanese man, who received nanoparticle albumin-bound paclitaxel for pancreatic cancer with multiple metastases, developed bilateral cystoid macular edema. Best-corrected visual acuity was 0.3 bilaterally. Cystoid macular edema resolved within 5 weeks after stopping nanoparticle albumin-bound paclitaxel and starting topical dorzolamide treatment confirming the diagnosis of taxane-related cystoid macular edema. Nine weeks later, best-corrected visual acuity improved to 0.8 in the right eye and 1.0 in the left eye. Conclusions Cystoid macular edema in each case resolved within a few months without any side effects using topical dorzolamide and terminating taxane-based chemotherapy. Topical dorzolamide appears to be a safe and effective treatment option for patients with taxane-related cystoid macular edema whose quality of life is threatened by visual disturbances.

Most of the medicines used for the treatment of glaucoma include a preservative in various concentrations. With long-term topical therapy, patients with glaucoma may develop dry eye syndrome (DES). The severity of symptoms depends on the number of drugs used and the presence of a preservative in them. Against the background of DES progression, compliance to glaucoma therapy may decrease, and, consequently, the effectiveness of the treatment may decrease. Currently, new non-preservative hypotensive drugs containing brimonidine, as well as a fixed combination (FC) of dorzolamide and timolol, are available on the market.Purpose: to compare assessment of the hypotensive effect and tolerability of preservative-free drugs FC Dorzolamid 20 mg/ml, Timolol 5 mg/ml (Dortmol Antiglau ECO) and Brimonidine 2 mg/ml (Brim Antiglau ECO) when switching from similar drugs containing a preservative in patients with compensated glaucoma.Patients and methods. In this prospective clinical study, 60 patients (60 eyes) with compensated primary open-angle glaucoma on combined topical therapy were examined. In group 1 (30 patients, 30 eyes), the combinations of dorzolamide / timolol or brinzolamide / timolol were switched with the non-preservative Dortmol Antiglau ECO. In group 2 (30 patients, 30 eyes), the brimonidine as part of the medication regimen were replaced with the non-preservative Brim Antiglau ECO. The level of corneal-compensated IOP was assessed before the switch in therapy and after 1 month. Subjective feelings and objective signs of the treatment’s use were monitored during examination and using a questionnaire, which was compiled to study the tolerance of therapy.Results. Switching to a preservative-free combination of dorzolamide and timolol resulted in a reduction in complaints of irritation, lacrimation, and foreign body sensation. The efficiency control did not reveal a significant change (p > 0.05) in the cornealcompensated intraocular pressure (IOPcc). When transferred to the Brim Antiglau ECO as part of the local hypotensive treatment, intraocular pressure decreased significantly (p < 0.05). The average total score characterizing drug intolerance, when evaluated by the patient, decreased by 2.4 times, by the attending physician-by 1.9 times. The degree of conjunctival hyperemia on the MacMonnies photographic scale decreased in both groups.Conclusion. Preservative-free drugs can be recommended for most patients with glaucoma as a starting treatment and as a replacement for current therapy.

Drug treatment optimization in primary open-angle glaucoma (POAG) is a topical issue of ophthalmology in recent decades. The review focuses on the choice of local hypotensive therapy and the effectiveness of a fixed combination (FC) of dorzolamide / timolol in glaucoma treatment. Since decreased perfusion eye pressure and disturbed regulation of local hemodynamics affect the development and progression of glaucomatous optical neuropathy, the use of anti-glaucomatous drugs or other hypotensive agents requires taking account of their effect on intraocular pressure (IOP), visual functions, and ocular blood flow. Most studies show that the hypotensive and hemodynamic effects of dorzolamide/timolol FC contribute to the preservation of visual fields in POAG patients by reducing significant risk factors for POAG progression, such as increased IOP and blood flow deficiency in the retinal and choroidal vessels. Improved hemodynamic parametersdue to local hypotensive treatment can be considered as basis for visual function stabilization, especially in long-term chronic courses of the disease.

In this work, we were going to generate first- and second-order electrochemical and spectroscopic data to investigate inhibition of the carbonic anhydrase II (CA II) by acetazolamide (AZ), dorzolamide (DZ) and methazolamide (MZ) which enabled us to have a deep insight to the mechanism of these inhibitions. MCR-ALS and PARAFAC were chosen for chemometric analyses of the data and after data resolution, spectral and voltammetric profiles and concentration profiles were obtained which helped us to obtain qualitative information about inhibition of the CA II which was completed by molecular docking and hard-modeling of the data. Our results showed that order of the inhibition of the CA II was occurred according to MZ > DZ > AZ. According to the results of inhibition of the CA II, the MZ was used to develop a novel amperometric method for determination of the CA II which was not electroactive. The sensor response was linearly correlated with concentration of the CA II in the range of 0–20 nM with a limit of detection (LOD) of 0.21 nM and a sensitivity of 0.57 μA nM−1. The developed method was stable, selective and sensitive for the determination of the CA II.

Aim and Objective: To compare the efficacy and safety of brinzolamide1% and timolol0.5% fixed combination eye drops versus dorzolamide2% and timolol0.5% fixed combination eye drops in the treatment of primary open-angle glaucoma. Design: Prospective, randomized, comparative, interventional study. Setting: Tertiary eye care centre. Material and Method: The present study was a comparative study carried out on patients visiting OPD of Ophthalmology Department and diagnosed with primary open-angle glaucoma. Group 1 (n-30 BT) received brinzolamide1% and timolol0.5% fixed combination eye drops, and Group 2 (N-30 DT) patients received dorzolamide2% and timolol0.5% fixed combination eye drops. A complete ophthalmic examination was performed, including Goldmann applanation tonometry. IOP was measured twice daily (9 AM and 4 PM). The patients were evaluated at 2, 4, 8, and 12 weeks. IOP was measured at follow-up. Side effects and tolerability of both drugs were assessed, and patient preference for drugs was noted. Results: Mean reduction in morning IOP was significantly more in Group 1 than in Group 2 at 8 weeks and 12 weeks (p < 0.05). Mean reduction in evening IOP was significantly more in Group 1 than in Group 2 at all follow-ups (p < 0.05). Conclusion: Brinzolamide1% + timolol0.5% fixed drug combination is more preferred and effective in lowering IOP than dorzolamide2% + timolol0.5% fixed drug combination in patients of primary open-angle glaucoma. [ABSTRACT FROM AUTHOR]

IntroductionTo investigate the efficacy of a treatment strategy with latanoprost and dorzolamide in primary pediatric glaucoma patients partially responsive to surgery.MethodsSingle arm, prospective, interventional multicenter study. Primary pediatric glaucoma patients younger than 13 years after a single surgical procedure with IOP between 22 and 26 mmHg were considered eligible. At baseline, patients were allocated to latanoprost monotherapy once daily. Depending on intraocular pressure (IOP) reduction at first visit, the patients were allocated to one of three groups: continuation of latanoprost monotherapy, addition of dorzolamide twice daily, or switch to dorzolamide three times daily. The same approach for allocation in medication groups was used in all subsequent visits. Patients in the dorzolamide monotherapy group with IOP reduction

Using topical application to deliver therapeutic concentrations of drugs to the posterior segment of the eye remains very challenging. As a result, posterior segment diseases are usually treated by intravitreal injection or implant. While topical treatments are commonly used for anterior segment conditions, they sometimes require frequent applications. Eye drop formulations based on γ‐cyclodextrin (γCD)‐based nanoparticle aggregates were developed, which in animal models and clinical studies deliver therapeutic concentrations of drugs (dorzolamide and dexamethasone) to both anterior and posterior segments of the eye. An early study in humans showed dorzolamide/γCD eye drops could achieve comparable intraocular pressure decreases to commercial dorzolamide eye drops, but with less frequent application. Pilot studies with dexamethasone/γCD eye drops suggested that they could be effective in a range of conditions, including diabetic macular oedema, cystoid macular oedema and vitritis secondary to uveitis, postcataract surgery inflammation and postoperative treatment in trabeculectomy. Phase II studies with similar dexamethasone/γCD nanoparticle eye drops in diabetic macular oedema and postcataract surgery inflammation have recently been completed. This technology has the potential to be used with other classes of drug molecules and to replace or complement invasive treatments, providing safer, non‐invasive therapies, particularly for posterior segment conditions, that can be self‐administered as eye drops by patients. [ABSTRACT FROM AUTHOR]

Purpose: To describe the successful closure of an idiopathic macular hole (MH) with topical therapy after surgery failed. Methods: A case report was evaluated and prospective literature review performed. Results: After surgery to correct an MH in a 57-year-old female patient failed, topical therapy was initiated. MH closure was successful using this modality. Conclusions: There are few reports in the literature describing successful closure of an idiopathic full-thickness MH with topical therapy after initial surgery fails. This reinforces the importance of the "hydration" hole in this disease. Characterization with optical coherence tomography may help determine which patients could benefit from topical treatment for MH closure and avoid costly and invasive surgical procedures., Competing Interests: The author(s) declared no potential conflicts of interest with respect to the research, authorship, and/or publication of the article., (© The Author(s) 2024.)

Background: Long-term use of topical, especially benzalkonium chloride (BAC)-preserved, antiglaucoma medications can cause a negative impact on the ocular surface. The aim of the study was to assess the effect of topical carbonic anhydrase inhibitors (CAIs) on selected oxidative stress biomarkers in the tear film.Methods: The patients were divided into four sex-matched groups: group C (n = 25) - control group - subjects who did not use topical antiglaucoma medications, group DL (n = 14) - patients using preservative-free dorzolamide, group DL + BAC (n = 16) - patients using topical BAC-preserved dorzolamide, group BL + BAC (n = 17) - patients using BAC-preserved brinzolamide. Subjects in all the study groups have been using the eye drops two times daily for 6-12 months. The oxidative stress biomarkers in the tear film samples were measured: total protein (TP) concentration, advanced oxidation protein products (AOPP) content, total sulfhydryl (-SH) groups content, the activity of superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx), as well as Total Oxidant Status (TOS), Total Antioxidant Response (TAR), and Oxidative Stress Index (OSI).Results: The advanced oxidation protein products content, Total Oxidant Status as well as superoxide dismutase and catalase activities in the group DL + BAC and BL + BAC were higher in comparison with the group C. The total sulfhydryl groups content was lower in the group DL + BAC and BL + BAC when compared to group C. Oxidative Stress Index was higher in the groups DL + BAC and BL + BAC in comparison with the groups DL and C.Conclusions: Use of topical benzalkonium chloride-preserved carbonic anhydrase inhibitors increases oxidative stress in the tear film. [ABSTRACT FROM AUTHOR]

Carbonic anhydrase inhibitors (CAIs) are prescription drugs also used in doping to dilute urine samples and tamper with urinalyses. Dorzolamide, brinzolamide, and acetazolamide are prohibited by the World Anti-Doping Agency. Detecting CAIs and their metabolites in biological samples is crucial to documenting misuse in doping. We quantified dorzolamide, brinzolamide, acetazolamide, and their metabolites in the urine and hair of 88 patients under treatment for ocular hypertension or glaucoma. Samples of the patients’ relatives were analyzed to assess potential for accidental exposure. After washing, 25 mg hair was incubated with an acidic buffer at 100 °C for 1 h. After cooling and centrifugation, the supernatant was analyzed by ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS). Urine (100 μL) was diluted and centrifuged before UHPLC-MS/MS analysis. Run time was 8 min through a reverse-phase column with a mobile phase gradient. MS/MS analysis was performed in a multiple-reaction monitoring mode after positive electrospray ionization. Median urinary concentration was 245 ng/mL (IQR: 116.2–501 ng/mL) for dorzolamide, 81.1 ng/mL (IQR: 35.9–125.3 ng/mL) for N-deethyl-dorzolamide, 0.77 ng/mL (IQR: 0.64 ng/mL–0.84 ng/mL) for N-acetyl-dorzolamide, 38.9 ng/mL (IQR: 20.4–79.2 ng/mL) for brinzolamide, and 72.8 ng/mL (IQR: 20.7–437.3 ng/mL) for acetazolamide. Median hair concentration was 0.48 ng/mg (IQR: 0.1–0.98 ng/mg) for dorzolamide, 0.07 ng/mg (IQR: 0.06–0.08 ng/mg) for N-deethyl-dorzolamide, 0.40 ng/mL (IQR: 0.13–1.95 ng/mL) for brinzolamide. Acetazolamide was detected in only one hair sample. Dorzolamide and brinzolamide were detected in the urine of three and one relatives, respectively. Cutoff concentrations of urinary dorzolamide and brinzolamide are necessary to preclude false positives due to contamination or passive exposure. We reported the first concentrations of brinzolamide in hair.

Background: Cystoid macular edema is a rare, vision-threatening side effect of the taxane family of anticancer agents. There is no established treatment or standard treatment protocol for taxane-related cystoid macular edema. Here, we report two cases of taxane-related cystoid macular edema that were treated with topical dorzolamide.Case Presentation: In case 1, a 72-year-old Japanese woman with bilateral geographic choroiditis reported for a follow-up visit with a complaint of blurred vision in both eyes for 2 months after starting nanoparticle albumin-bound paclitaxel chemotherapy for multiple metastases of her breast cancer. Her best-corrected visual acuity had dropped from 1.2 to 0.9 in the right eye and from 1.0 to 0.4 in the left eye. Fundus examination showed no newly active geographic choroiditis lesion, but optical coherence tomography exhibited cystoid macular edema. We suspected taxane-related cystoid macular edema and terminated nanoparticle albumin-bound paclitaxel, and started topical dorzolamide treatment. Cystoid macular edema nearly resolved within 6 weeks in the right eye and within 10 weeks in the left eye after starting topical dorzolamide treatment. The resolution of cystoid macular edema without leaving a chorioretinal scar after discontinuation of paclitaxel confirmed our initial diagnosis of taxane-related cystoid macular edema. A few inconspicuous cystoid spaces persisted at the parafovea for a year after dorzolamide treatment ended, but regressed after restarting dorzolamide treatment without any side effects. Best-corrected visual acuity improved to 1.2 in the right eye and 1.0 in the left eye. In case 2, a 70-year-old Japanese man, who received nanoparticle albumin-bound paclitaxel for pancreatic cancer with multiple metastases, developed bilateral cystoid macular edema. Best-corrected visual acuity was 0.3 bilaterally. Cystoid macular edema resolved within 5 weeks after stopping nanoparticle albumin-bound paclitaxel and starting topical dorzolamide treatment confirming the diagnosis of taxane-related cystoid macular edema. Nine weeks later, best-corrected visual acuity improved to 0.8 in the right eye and 1.0 in the left eye.Conclusions: Cystoid macular edema in each case resolved within a few months without any side effects using topical dorzolamide and terminating taxane-based chemotherapy. Topical dorzolamide appears to be a safe and effective treatment option for patients with taxane-related cystoid macular edema whose quality of life is threatened by visual disturbances. [ABSTRACT FROM AUTHOR]

A wild young adult western screech owl (Megascops kennicottii) of unknown sex was presented for evaluation of an abnormal left eye (OS). Ophthalmic examination OS revealed raised intraocular pressure (37 mm Hg; reference interval 7-16 mm Hg), mydriasis, conjunctival and episcleral hyperemia, shallow anterior chamber due to anterior displacement of the lens and iris, rubeosis iridis, and engorgement of the pecten. The intraocular pressure in the right eye (OD) was 11 mm Hg. Multifocal pale, variably translucent, curvilinear to vermiform opacities were observed in the medial and ventral peripheral regions of the retina OD, consistent with focal retinitis. Mannitol (0.46 g/kg IV) was administered over 10 minutes. Forty minutes later, the intraocular pressure was 27 mm Hg OS and 13 mm Hg OD. Dorzolamide (one drop OS q12h), diclofenac (one drop OU q8-12h), and meloxicam (0.5 mg/kg PO q24h) were administered for 3 days. The intraocular pressure OS was within normal limits 1 day (11 mm Hg), 7 days (13 mm Hg), and 4 weeks (14 mm Hg) after this treatment. Complications arising during hospitalization and rehabilitation included superficial corneal ulceration of both eyes presumed secondary to trauma on being caught and superficial damage to a talon. The owl was released after a period of rehabilitation. Characteristic presenting signs as well as response to therapy suggest aqueous misdirection was the cause of ocular hypertension in this owl. To our knowledge, this is the first report of suspected aqueous misdirection and its medical management in a raptor.

A 11-year-old boy presented with complaints of blurred vision and on evaluation was found to have X-linked retinoschisis (XLRS) with angle-closure glaucoma. Clinical and genetic evaluation of first-degree family members was done. His brother had a milder form of XLRS with shallow anterior chamber. Topical dorzolamide 2% and timolol 0.5% were used to control intraocular pressure. Genetic analysis revealed a novel three base pair deleterious mutation (c. 375_377 del AGA) in exon-5 of the RS1 gene in three members of the family.

Glaucoma is the second leading cause of blindness in the world. Despite the fact that many treatments are currently available for eye diseases, the key issue that arises is the administration of drugs for long periods of time and the increased risk of inflammation, but also the high cost of eye surgery. Consequently, numerous daily administrations are required, which reduce patient compliance, and even in these conditions, the treatment of eye disease is too ineffective. Micellar polymers are core–shell nanoparticles formed by the self-assembly of block or graft copolymers in selective solvents. In the present study, polymeric micelles (PMs) were obtained by dialysis from smart biocompatible poly(ε-caprolactone)-poly(N-vinylcaprolactam-co-N-vinylpyrrolidone) [PCL-g-P(NVCL-co-NVP)] graft copolymers. Two copolymers with different molar masses were studied, and a good correlation was noted between the micellar sizes and the total degree of polymerisation (DPn) of the copolymers. The micelles formed by Cop A [PCL120-g-P(NVCL507-co-NVP128)], with the lowest total DPn, have a Z-average value of 39 nm, whereas the micellar sizes for Cop B [PCL120-g-P(NVCL1253-co-NVP139)] are around 47 nm. These PMs were further used for the encapsulation of two drugs with applications for the treatment of eye diseases. After the encapsulation of Dorzolamide, a slight increase in micellar sizes was noted, whereas the encapsulation of Indomethacin led to a decrease in these sizes. Using dynamic light scattering, it was proved that both free and drug-loaded PMs are stable for 30 days of storage at 4 °C. Moreover, in vitro biological tests demonstrated that the obtained PMs are both haemo- and cytocompatible and thus can be used for further in vivo tests. The designed micellar system proved its ability to release the encapsulated drugs in vitro, and the results obtained were validated by in vivo tests carried out on experimental animals, which proved its high effectiveness in reducing intraocular pressure.