- Brinzolamide-brimonidine fixed combination to prevent intraocular pressure elevation after neodymium:YAG laser posterior capsulotomy. [Letter]
- JCJ Cataract Refract Surg 2018; 44(4):514-515
- Efficacy of additional topical betamethasone in persistent cystoid macular oedema after carbonic anhydrase inhibitor treatments in retinitis pigmentosa. [Journal Article]
- BOBMJ Open Ophthalmol 2018; 3(1):e000107
- CONCLUSIONS: Our data suggested that additional betamethasone might improve treatments for persistent CMO. Topical steroids could be an alternative option for managing persistent CMO in RP.
- Comparative cost evaluation of brand name and generic ophthalmology medications in Ontario. [Review]
- CJCan J Ophthalmol 2018; 53(2):173-187
- Medication cost for the same indication can vary considerably and can affect patient compliance. In this comparative cost analysis of commonly prescribed ophthalmology medications, the differences in...
Medication cost for the same indication can vary considerably and can affect patient compliance. In this comparative cost analysis of commonly prescribed ophthalmology medications, the differences in cost between generic and brand name medications as well as different medications within an individual drug class were evaluated. Eye preparations from the Ontario Drug Benefit Formulary were identified, and further agents commonly prescribed by ophthalmologists were included. The standardized prescription drug cost, which includes the cost of the medication, mark-up, and dispensing cost, was provided by Ontario Shoppers Drug Mart stores in July 2016 for 103 common medications using typical dosages and durations. Based on medication class, the highest and lowest cost medications were antiallergy agents (Zaditor [ketotifen], Vasocon [naphazoline]), antibiotic ophthalmic solutions (Vigamox [moxifloxacin], generic ciprofloxacin), oral antibiotics (Cipro [ciprofloxacin], generic cephalexin), antibiotic ophthalmic ointments (generic erythromycin, Tobrex [tobramycin]), antiviral treatment (Valtrex [oral valacyclovir], Viroptic [topical trifluridine]), blepharitis treatment (Zithromax [oral azithromycin], generic oral tetracycline), beta-adrenergic inhibitors (Timoptic [topical timolol], generic topical timolol), topical prostaglandin analogues (Xalatan [latanoprost], generic travoprost), oral carbonic anhydrase inhibitors (methazolamide, acetazolamide), topical carbonic anhydrase solutions (Trusopt preservative-free [dorzolamide], Azopt [brinzolamide]), topical alpha-adrenergic agonists (Alphagan [brimonidine], generic brimonidine), topical muscarinic agonists (Isopto carpine [pilocarpine], Diocarpine [pilocarpine]), topical combination glaucoma agents (Cosopt [dorzolamide-timolol], generic dorzolamide-timolol), topical lubricants (Lacri-lube, Isopto tears), topical nonsteroidal anti-inflammatory drugs (Acuvail [ketorolac], Ilevro [nepafenac]), and steroids (Durezol [difluprednate], Pred mild [prednisolone]). Substantial cost differences exist between ophthalmology medications of the same class. We encourage ophthalmologists to be aware of the associated costs of the medications they prescribe and to use this information in their decision making.
- Reversal of retinal pigment epithelial detachment after cessation of topical travoprost therapy. [Journal Article]
- IOInt Ophthalmol 2018 Mar 22
- CONCLUSIONS: Hence, clinicians should be aware of this rare incidence of RPED followed by travoprost therapy. First case of RPED following travoprost therapy and complete reattachment upon withdrawal is reported here in this case report.
- A novel ocular delivery of brinzolamide based on gellan gum: in vitro and in vivo evaluation. [Journal Article]
- DDDrug Des Devel Ther 2018; 12:383-389
- CONCLUSIONS: The results of pharmacodynamics implied that the novel preparation of BLZ in situ gel effectively prolonged the intraocular pressure-lowering effect after administration.
- Nanoliposome-Encapsulated Brinzolamide-hydropropyl-β-cyclodextrin Inclusion Complex: A Potential Therapeutic Ocular Drug-Delivery System. [Journal Article]
- FPFront Pharmacol 2018; 9:91
- Novel ocular drug delivery systems (NODDSs) remain to be explored to overcome the anatomical and physiological barriers of the eyes. This study was to encapsulate brinzolamide (BRZ)-hydropropyl-β-cyc...
Novel ocular drug delivery systems (NODDSs) remain to be explored to overcome the anatomical and physiological barriers of the eyes. This study was to encapsulate brinzolamide (BRZ)-hydropropyl-β-cyclodextrin (HP-β-CD) inclusion complex (HP-β-CD/BRZ) into nanoliposomes and investigate its potential as one of NODDS to improve BRZ local glaucomatous therapeutic effect. HP-β-CD/BRZ was firstly prepared to enhance the solubility of poorly water-soluble BRZ. The HP-β-CD/BRZ loaded nanoliposomes (BCL) were subsequently constructed by thin-film dispersion method. After the optimization of the ratio of BRZ to HP-β-CD, the optimal BCL showed an average size of 82.29 ± 6.20 nm, ζ potential of -3.57 ± 0.46 mV and entrapment efficiency (EE) of 92.50 ± 2.10% with nearly spherical in shape. The X-ray diffraction (XRD) confirmed the formation of HP-β-CD/BRZ and BCL. Thein vitrorelease study of BCL was evaluated using the dialysis technique, and BCL showed moderate sustained release. BCL (1 mg/mL BRZ) showed a 9.36-fold increase in the apparent permeability coefficient and had a sustained and enhanced intraocular pressure reduction efficacy when compared with the commercially available formulation (BRZ-Sus) (10 mg/mL BRZ). In conclusion, BCL might have a promising future as a NODDS for glaucoma treatment.
- "To Be or Not to Be" Protonated: Atomic Details of Human Carbonic Anhydrase-Clinical Drug Complexes by Neutron Crystallography and Simulation. [Journal Article]
- SStructure 2018 Mar 06; 26(3):383-390.e3
- Human carbonic anhydrases (hCAs) play various roles in cells, and have been drug targets for decades. Sequence similarities of hCA isoforms necessitate designing specific inhibitors, which requires d...
Human carbonic anhydrases (hCAs) play various roles in cells, and have been drug targets for decades. Sequence similarities of hCA isoforms necessitate designing specific inhibitors, which requires detailed structural information for hCA-inhibitor complexes. We present room temperature neutron structures of hCA II in complex with three clinical drugs that provide in-depth analysis of drug binding, including protonation states of the inhibitors, hydration water structure, and direct visualization of hydrogen-bonding networks in the enzyme's active site. All sulfonamide inhibitors studied bind to the Zn metal center in the deprotonated, anionic, form. Other chemical groups of the drugs can remain neutral or be protonated when bound to hCA II. MD simulations have shown that flexible functional groups of the inhibitors may alter their conformations at room temperature and occupy different sub-sites. This study offers insights into the design of specific drugs to target cancer-related hCA isoform IX.
- Sulfonamide inhibition studies of two β-carbonic anhydrases from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2. [Journal Article]
- JEJ Enzyme Inhib Med Chem 2018; 33(1):390-396
- The two β-carbonic anhydrases (CAs, EC 18.104.22.168) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 a...
The two β-carbonic anhydrases (CAs, EC 22.214.171.124) recently cloned and purified from the ascomycete fungus Sordaria macrospora, CAS1 and CAS2, were investigated for their inhibition with a panel of 39 aromatic, heterocyclic, and aliphatic sulfonamides and one sulfamate, many of which are clinically used agents. CAS1 was efficiently inhibited by tosylamide, 3-fluorosulfanilamide, and 3-chlorosulfanilamide (KIs in the range of 43.2-79.6 nM), whereas acetazolamide, methazolamide, topiramate, ethoxzolamide, dorzolamide, and brinzolamide were medium potency inhibitors (KIs in the range of 360-445 nM). CAS2 was less sensitive to sulfonamide inhibitors. The best CAS2 inhibitors were 5-amino-1,3,4-thiadiazole-2-sulfonamide (the deacetylated acetazolamide precursor) and 4-hydroxymethyl-benzenesulfonamide, with KIs in the range of 48.1-92.5 nM. Acetazolamide, dorzolamide, ethoxzolamide, topiramate, sulpiride, indisulam, celecoxib, and sulthiame were medium potency CAS2 inhibitors (KIs of 143-857 nM). Many other sulfonamides showed affinities in the high micromolar range or were ineffective as CAS1/2 inhibitors. Small changes in the structure of the inhibitor led to important differences of the activity. As these enzymes may show applications for the removal of anthropically generated polluting gases, finding modulators of their activity may be crucial for designing environmental-friendly CO2capture processes.
- Evolution of pH buffers and water homeostasis in eukaryotes: homology between humans and Acanthamoeba proteins. [Journal Article]
- FMFuture Microbiol 2018; 13:195-207
- This study intended to trace the evolution of acid-base buffers and water homeostasis in eukaryotes. Acanthamoeba castellanii was selected as a model unicellular eukaryote for this purpose. Homologi...
This study intended to trace the evolution of acid-base buffers and water homeostasis in eukaryotes. Acanthamoeba castellanii was selected as a model unicellular eukaryote for this purpose. Homologies of proteins involved in pH and water regulatory mechanisms at cellular levels were compared between humans and A. castellanii.
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- The Efficacy and Safety of the Fixed Combination of Brinzolamide 1% and Brimonidine 0.2% in Normal Tension Glaucoma: An 18-Month Retrospective Study. [Journal Article]
- JOJ Ocul Pharmacol Ther 2018; 34(3):274-279
- CONCLUSIONS: BBFC provides a significant IOP reduction and is a safe antiglaucoma medication for NTG patients.