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Complication management and prevention
Published in Jani van Loghem, Calcium Hydroxylapatite Soft Tissue Fillers, 2020
Pieter Siebenga, Jani van Loghem
Administration of a beta-adrenergic antagonist in the form of eye drops (e.g., Timolol 0.5%), brinzolamide or azetazolamide will also help to reduce intraocular pressure; azetazolamide may be of greater benefit if administered intravenously. Aspirin (500 mg) should be prescribed to reduce the risk of blood clotting and intravenous dexamethasone should be used to decrease inflammation.
Therapeutic Use of Carbonic Anhydrase Inhibitors and Their Multiple Drug Interactions
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Andrea Angeli, Claudiu T. Supuran
The systemic carbonic anhydrase inhibitor, acetazolamide (1), was initially discovered as a diuretic agent (Supuran, 2008; Neri and Supuran, 2011) and introduced in 1954 into ophthalmology as a treatment for glaucoma and, since then, has been widely used for this purpose. At first, its clinical use as diuretic drug is limited to development of metabolic acidosis (Kassamali and Sica, 2011). However, this feature can afford some potential clinical benefit for disease states such as metabolic alkalosis (Faisy et al., 2010; Mazur et al., 1999) nephrolithiasis (Sterrett et al., 2008), rhabdomyolysis (Subbaramaiah et al., 2010; Davidov et al., 2006), contrast-induced nephropathy (CIN) (Pakfetrat et al., 2009), sleep apnea (Nakayama et al., 2002; Angeli and Supuran, 2018), and high-altitude erythropoiesis (Leaf and Goldfarb, 2007; Richalet et al., 2008). In subsequent years the systemic side effects of acetazolamide led to the development of new CAIs such as brinzolamide 3 and dorzolamide 4 (Fig. 3.2) with their high water solubility are administered via the topical route directly into the eye, making them less prone to drug-drug interactions and systemic side effects (Carta et al., 2012; Masini et al., 2013).
Medical Therapy for Glaucoma
Published in Neil T. Choplin, Carlo E. Traverso, Atlas of Glaucoma, 2014
Jennifer E. Williamson, Janet B. Serle
Subsequently, in 1998, brinzolamide 1% (Azopt), a second topical CAI, was approved for clinical use. Brinzolamide is similar in efficacy to dorzolamide. These agents are commonly prescribed twice daily due to the poor compliance with t.i.d. dosing. IOP should be evaluated in the afternoon to determine whether t.i.d. dosing would be beneficial in an individual patient. The most common ocular side effects of these two agents differ, however. Because brinzolamide is a suspension, it may cause blurring upon instillation, and the most common ocular side effect with use of dorzolamide is stinging upon instillation due to its acidic pH.
Ocular microemulsion of brinzolamide: Formulation, physicochemical characterization, and in vitro irritation studies based on EpiOcular™ eye irritation assay
Published in Pharmaceutical Development and Technology, 2021
Panoraia I. Siafaka, Emre Şefik Çağlar, Hande Sipahi, Mohammad Charehsaz, Ahmet Aydın, Neslihan Üstündağ Okur
In this study, blank and brinzolamide loaded microemulsions with various drug concentrations (0.2, 0.5 and 1% w/w) were prepared, characterized, and evaluated for their physicochemical properties, in vitro drug release and in vitro ocular irritation. The construction of pseudo ternary phase diagrams was applied to optimize the formulation of microemulsions. According to the results, Brinzolamide-loaded microemulsions were successfully developed with low and desirable narrow globule size. Apparently, the developed optimized microemulsions can be used as ocular carriers for glaucoma management; nonetheless, the most optimal of all was M1 comprised from Isopropyl Myristate as oil phase and Tween 80/Ethanol as surfactant. In fact, M1 provides prolonged release and optimal physicochemical values, which are significant advantages. According to the EpiOcular Irritation study, M1 has not presented any irritation since more than 60% of cells were viable. Accordingly, the present study can suggest that the developed ocular MEs loaded with Brinzolamide can possibly enhance the therapeutic efficiency of the drug and maximize glaucoma therapy due to enhanced solubility, prolonged-release and non-irritancy.
Efficacy of topical brinzolamide in children with retinal dystrophies
Published in Ophthalmic Genetics, 2019
Brittni A. Scruggs, Constance V. Chen, Wanda Pfeifer, Jill S. Wiley, Kai Wang, Arlene V. Drack
Unique challenges are present in the pediatric patient population, including compliance and reliance on a caregiver to administer therapy. To date, few studies have been conducted on the use of CAIs in children for the treatment of macular cysts. The newer generation of CAIs is better tolerated by children since they do not cause stinging upon application (9). Brinzolamide (1%), a high-affinity and high-specificity carbonic anhydrase II inhibitor, is one such drug and is FDA-approved for topical use in patients with primary open-angle glaucoma (10). It is also used off-label for the treatment of macular cysts, and there are case reports demonstrating favorable outcomes in the reduction of macular cysts in XLRS patients (11).
Direct and crossover effects of brinzolamide, betaxolol, and latanoprost on choroidal thickness
Published in Cutaneous and Ocular Toxicology, 2019
Murat Okutucu, Hüseyin Fındık, Mehmet Gökhan Aslan
Latanoprost, brinzolamide, and betaxolol are eye pressure reducing agents commonly used in glaucoma treatment. Latanoprost is a prostaglandin F2α analog and a selective prostanoid FP receptor antagonist, which reduces intraocular pressure by increasing the outflow of aqueous humor1. Brinzolamide is a potent inhibitor of carbonic anhydrase II (CA ll), which is the dominant carbonic anhydrase isoenzyme in human eyes2. Betaxolol is a selective beta-1 receptor blocker, which lowers the pressure inside the eye by decreasing aqueous humor production in the ciliary body3.