- Pyrazole/pyrazoline as an excellent pharmacophore in the design of carbonic anhydrase inhibitors (2018-2022). [Review]Arch Pharm (Weinheim). 2023 Jan 04 [Online ahead of print]AP
- Carbonic anhydrase (CA) is a metalloenzyme that catalyzes the interconversion between carbon dioxide and water and dissociated ions of carbonic acid. In addition, CA performs various other functions in animals and plants, depending on the part of the living being. CAs have been found in almost all organisms. Besides, CAs are associated with several diseases, such as glaucoma, obesity, epilepsy, c…
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- Frequent self-monitoring of intraocular pressure can determine effectiveness of medications in eyes with normal tension glaucoma: A case report. [Case Reports]
- CONCLUSIONS: We conclude that frequent self-measurements of the IOP can determine that small changes of the IOPs are significant.
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- [Efficacy and safety of a fixed combination drug Brinzolol Duo in the treatment of patients with primary open-angle glaucoma]. [Journal Article]Vestn Oftalmol. 2022; 138(6):99-106.VO
- CONCLUSIONS: The new drug Brinzolol Duo (brinzolamide + timolol) significantly reduces IOP in POAG patients with efficacy comparable to Azarga.
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- The Efficacy, Safety, and Satisfaction Associated with Switching from Brinzolamide or Brimonidine to Brinzolamide/Brimonidine in Open-Angle Glaucoma Patients. [Journal Article]
- We evaluated switching from brinzolamide 1% or brimonidine 0.1% to a fixed-combination of brinzolamide 1% and brimonidine 0.1%, and then determined the efficacy, safety, and satisfaction associated with these changes in glaucoma patients. This prospective, nonrandomized study evaluated a total of 31 enrolled glaucoma patients who underwent treatment with at least brinzolamide 1% or brimonidine 0.…
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- A Novel Ocular Delivery of Brinzolamide Based on Gellan Gum: In vitro and in vivo Evaluation [Retraction]. [Retraction of Publication]Drug Des Devel Ther. 2022; 16:4109-4110.DD
- [This retracts the article DOI: 10.2147/DDDT.S153405.].
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- AAV2/4-RS1 gene therapy in the retinoschisin knockout mouse model of X-linked retinoschisis. [Journal Article]
- CONCLUSIONS: AAV2/4-RS1 shows promise for improving retinal phenotype in the Rs1-KO mouse model. Subretinal delivery was superior to intravitreal. Topical brinzolamide did not improve efficacy. AAV2/4-RS1 may be considered as a potential treatment for XLRS patients.
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- Design, Synthesis and Evaluation of Novel Molecular Hybrids between Antiglaucoma Drugs and H2S Donors. [Journal Article]
- Glaucoma is a group of eye diseases consisting of optic nerve damage with corresponding loss of field vision and blindness. Hydrogen sulfide (H2S) is a gaseous neurotransmitter implicated in various pathophysiological processes. It is involved in the pathological mechanism of glaucomatous neuropathy and exerts promising effects in the treatment of this disease. In this work, we designed and synth…
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- Design, Synthesis, Kinetic Analysis and Pharmacophore-Directed Discovery of 3-Ethylaniline Hybrid Imino-Thiazolidinone as Potential Inhibitor of Carbonic Anhydrase II: An Emerging Biological Target for Treatment of Cancer. [Journal Article]
- Carbonic anhydrases (CA), having Zn2+ metal atoms, are responsible for the catalysis of CO2 and water to bicarbonate and protons. Any abnormality in the functioning of these enzymes may lead to morbidities such as glaucoma and different types of cancers including brain, renal and pancreatic carcinomas. To cope with the lack of presence of a promising therapeutic agent against these cancers, searc…
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- Proteome-Based Investigation Identified Potential Drug Repurposable Small Molecules Against Monkeypox Disease. [Journal Article]
- Monkeypox Virus (MPXV), the causative agent of Monkeypox (MPX) disease, is an emerging zoonotic pathogen spreading in different endemic and non-endemic nations and creating outbreaks. MPX treatment mainly includes Cidofovir and Tecovirimat but they have several side effects and solely depending on these drugs may promote the emergence of drug-resistant variants. Hence, new drugs are required to c…
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- Quantification of Carbonic Anhydrase Inhibitors and Metabolites in Urine and Hair of Patients and Their Relatives. [Journal Article]
- 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 metab…
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- Mucoadhesive brinzolamide-loaded nanofibers for alternative glaucoma treatment. [Journal Article]Eur J Pharm Biopharm. 2022 Nov; 180:48-62.EJ
- Despite the advances in the field of pharmaceutical materials and technology, topical administration remains a method of choice for the treatment of eye diseases such as glaucoma, with eye drops being a leading dosage form. Their main disadvantage is a very short drug residence time and thus poor drug bioavailability, leading to the necessity of continuous repeated dosing. Mucoadhesive electrospu…
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- Bilateral Cystoid Macular Edema after COVID-19: 1 Year Follow Up. [Journal Article]Ocul Immunol Inflamm. 2022 Sep 08 [Online ahead of print]OI
- CONCLUSIONS: This is an unusual case of CME in previous COVID-19 infection. This presentation may be a parainfectious or a post-viral manifestation of COVID-19.
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- A novel loss-of-function mutation of the voltage-gated potassium channel Kv10.2 involved in epilepsy and autism. [Journal Article]
- CONCLUSIONS: By in vitro studying primary cells from the patient and the activation capacity of the mutated protein, we could first, find a readout for the cellular defects and second, test pharmaceutical treatments that proved to be beneficial. The results show the involvement of a novel LOF mutation of a Potassium channel in autism syndrome with epilepsy and the great potential of in vitro cultures of primary cells in personalised medicine of rare diseases.
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- Evaluation of the Use of Brinzolamide-Brimonidine Fixed Combination in Maximum Medical Therapy. [Journal Article]
- CONCLUSIONS: Maximum medical therapy with BBFC provides significant IOP reduction and antiglaucoma therapy simplification with a favorable safety profile in patients with glaucoma.
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- Intraocular pressure-lowering effects and safety of brimonidine/brinzolamide fixed combination after switching from other medications. [Journal Article]
- CONCLUSIONS: BBFC had satisfactory IOP-lowering effects without serious adverse reactions in patients who switched medications.
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- Longitudinal Photoreceptor Phenotype Observation and Therapeutic Evaluation of a Carbonic Anhydrase Inhibitor in a X-Linked Retinoschisis Mouse Model. [Journal Article]
- CONCLUSIONS: In addition to post receptoral impairments, photoreceptor cells underwent progressive dysfunction since early age in Rs1 -/Y mice. Long-term CAI treatment improved the shrinkage of the splitting retinal cavity, while no functional improvement was observed.
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- Comparative study to assess efficacy and safety of brinzolamide1% and timolol0.5% fixed combination eye drops versus dorzolamide2% and timolol0.5% fixed combination eye drops in management of open-angle glaucoma. [Journal Article]
- CONCLUSIONS: 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.
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- Brinzolamide- and latanoprost-loaded nano lipid carrier prevents synergistic retinal damage in glaucoma. [Journal Article]Acta Biochim Pol. 2022 May 26; 69(2):423-428.AB
- Glaucoma is a common eye disease and a major cause of blindness. We designed brinzolamide (Brla)- and latanoprost (Ltp)-loaded nano-lipoidal carriers (NLCs) for glaucoma treatment. Brla and Ltp-loaded NLCs were designed and characterized by assessing the zeta potential, polydispersity index, X-ray diffraction and scanning electron microscopy images, and particle size. Drug release was assessed by…
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- Brinzolamide-loaded soft contact lens for ophthalmic delivery. [Journal Article]Ther Deliv. 2022 04; 13(4):233-247.TD
- Aim: In this study, brinzolamide (BRZ) was loaded in balafilcon A silicone hydrogel soft contact lens to enhance delivery in glaucoma therapy. Materials & methods: BRZ-loaded soft contact lens was prepared by the soaking method with optimization of pH, temperature and concentration of drug loading solution. Results: At pH 7.4, loading temperature and concentration of 32°C and 3 mg/ml, respectivel…
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- Intraluminal deposits: A rare cause of glaucoma drainage implant total obstruction. [Journal Article]Eur J Ophthalmol. 2023 Jan; 33(1):307-311.EJ
- CONCLUSIONS: Our study describes a new cause of total obstruction GDI tubes. The long-term use of timolol maleate and brinzolamide and their presence in the intraluminal solid sample collected from the blocked GDI tube suggest that the glaucoma medication may have a role in the pathogenesis. However, the exact mechanism is unknown and requires further studies.
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- Peripheral anterior synechiae after selective laser trabeculoplasty among Chinese patients. [Journal Article]
- CONCLUSIONS: PAS development after SLT appears to be more common in Chinese patients, with a presumed 4-year incidence of 13.6%, based on retrospective review of eyes with subsequent documented gonioscopy findings.
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- Retinal evaluation by fundus angiography before and after vitrectomy and foreign body removal in a patient with ocular siderosis: a case report. [Case Reports]
- CONCLUSIONS: The influence of iron ion on retinal vein and the distribution of iron ion along retinal artery can be seen macroscopically by FA before and after foreign body removal.
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- Assessment of the readability and quality of online patient education materials for the medical treatment of open-angle glaucoma. [Journal Article]
- CONCLUSIONS: The majority of online patient education materials for the medical treatment of glaucoma are written at a level too difficult for the general population and fail to meet accountability standards.
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- Effects of Topical Antiglaucomatous Medications on Conjunctival Thickness: A Prospective Anterior Segment Optical Coherence Tomography Study. [Journal Article]J Ocul Pharmacol Ther. 2022 05; 38(4):287-293.JO
- Purpose: Our aim was to evaluate the effects of topical antiglaucomatous medications on conjunctival thickness using anterior segment optical coherence tomography (AS-OCT). Methods: Thirty eyes of 30 patients with primary open angle glaucoma, who had never used any antiglaucomatous medications, enrolled in this prospective study. Followed by a full ophthalmologic examination, the conjunctival thi…
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- Comparative Assessment of Retinal Blood Flow Velocity Changes Following Brimonidine and Brinzolamide Administration Using Retinal Function Imaging. [Randomized Controlled Trial]
- CONCLUSIONS: Neither brimonidine nor brinzolamide appear to alter retinal blood flow velocity in a clinically relevant manner. The slight velocity changes detected in our study are likely physiologic fluctuations. Our findings do not support the rationale of a detrimental effect of topical brimonidine on ocular blood flow and hence brimonidine may be further administered for lowering intraocular pressure with the appropriate caution. However, our study is strongly limited by the small sample size and, thus, further research with larger cohorts of healthy volunteers and patients with glaucoma is needed to confirm the results.
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- Efficacy of brinzolamide in the initial management of acute primary angle closure: A randomized controlled trial. [Randomized Controlled Trial]J Clin Pharm Ther. 2022 Jun; 47(6):792-797.JC
- WHAT IS KNOWN AND OBJECTIVE?: Since comprehensive medication has an important role in the initial management of patients presenting with acute primary angle closure, it is necessary to analyse the effect of each drug on alleviating the disease. This study aimed to evaluate the intraocular pressure-lowering effect of brinzolamide in the sequential treatment of acute primary angle closure. METHODS:…
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- Inhibition of Carbonic Anhydrase 2 Overcomes Temozolomide Resistance in Glioblastoma Cells. [Journal Article]
- About 95% of Glioblastoma (GBM) patients experience tumor relapse as a consequence of resistance to the first-line standard chemotherapy using temozolomide (TMZ). Recent studies reported consistently elevated expression levels of carbonic anhydrase CA2 in recurrent glioblastoma and temozolomide-resistant glioblastoma stem-like cells (GSCs). Here we show that CA2 is preferentially expressed in GSC…
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- Effects of Topical Carbonic Anhydrase Inhibitors on the Olfactory Sense. [Journal Article]
- CONCLUSIONS: No negative effect on the sense of smell was determined after 7 days of topical application of a carbonic anhydrase enzyme inhibitor to the eye in patients with no previous anosmia.
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- Intravitreal Ranibizumab Had Limited Effect on Cystoid Macular Edema Due to Albumin-Bound Paclitaxel: A Case Report and Literature Review. [Case Reports]
- Angiographically silent cystoid macular edema (CME) is a rare complication from nab-paclitaxel. Here we report a 45-year-old woman with breast cancer who developed CME after several months of treatment with albumin-bound paclitaxel (nab-paclitaxel). Her visual acuity did not improve significantly with the cessation of nab-paclitaxel and intravitreal ranibizumab treatment. Then, brinzolamide eye d…
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- The Efficacy, Safety and Satisfaction Associated with Switching from Brinzolamide 1% and Brimonidine 0.1% to a Fixed Combination of Brinzolamide 1% and Brimonidine 0.1% in Glaucoma Patients. [Journal Article]
- We evaluated glaucoma patients for the efficacy, safety and satisfaction associated with switching from brinzolamide 1% and brimonidine 0.1% to a fixed combination of brinzolamide 1% and brimonidine 0.1%. A total of 22 glaucoma patients were enrolled and completed this prospective, nonrandomized study that evaluated patients who underwent treatment with at least brinzolamide 1% and brimonidine 0.…
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