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Purpose: Glaucoma is the second leading cause of blindness worldwide, affecting more than 64 million people aged 40–80. The best way to manage primary open?angle glaucoma (POAG) is by lowering the intraocular pressure (IOP). Netarsudil is a Rho kinase inhibitor, the only class of antiglaucoma medications that reorganizes the extracellular matrix to improve the aqueous outflow through the trabecular pathway. Methods: An open?label, real?world, multicentric, observation?based 3?month study was performed for assessing the safety and ocular hypotensive efficacy of netarsudil ophthalmic solution (0.02% w/v) in patients with elevated IOP. Patients were given netarsudil ophthalmic solution (0.02% w/v) as a first?line therapy. Diurnal IOP measurements, best?corrected visual acuity, and adverse event assessments were recorded at each of the five visits (Day?1: screening day and first dosing day; subsequent observations were taken at 2 weeks, 4 weeks, 6 weeks, and 3 months). Results: Four hundred and sixty?nine patients from 39 centers throughout India completed the study. The mean IOP at baseline of the affected eyes was 24.84 ± 6.39 mmHg (mean ± standard deviation). After the first dose, the IOP was measured after 2, 4, and 6 weeks, with the final measurement taken at 3 months. The percentage reduction in IOP in glaucoma patients after 3 months of once?daily netarsudil 0.02% w/v solution use was 33.34%. The adverse effects experienced by patients were not severe in the majority of cases. Some adverse effects observed were redness, irritation, itching, and others, but only a small number of patients experienced severe reactions, as reported in a decreasing order: redness > irritation > watering > itching > stinging > blurring. Conclusion: We found that netarsudil 0.02% w/v solution monotherapy when used as the first?line treatment in primary open?angle glaucoma and ocular hypertension was both safe and effective.
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Purpose: To describe clinical course, characteristics, and outcome of reticular epithelial corneal edema (RECE) occurring as a not?so?infrequent adverse effect of a novel drug, Rho?kinase inhibitors (ROCK?I)? netarsudil (0.02%) and ripasudil (0.4%). Methods: This was a retrospective observational non?randomized study. In this study, 12 eyes of 11 patients presenting at a tertiary eye care center between April 2021 and September 2021 were included. All 12 eyes developed a distinctive honeycomb pattern of RECE after starting topical ROCK?I. All patients were subjected to detailed ophthalmic examinations. Results: Eight patients were started on netarsudil (0.02%) and three on ripasudil (0.4%). Five eyes had a prior history of corneal edema. The remaining seven had the presence of ocular comorbidities predisposing to corneal edema. The average time for RECE occurrence was 25 days for netarsudil and 82 days for ripasudil. Visual acuity decreased in two eyes, remained unaffected in four eyes, and could not be quantified in four eyes due to preexisting profound visual impairment. Five eyes had symptoms of ocular surface discomfort associated with bullae. Symptoms and bullae resolved in all eyes in whom ROCK?I was stopped. The average time to resolution of RECE was 10 days for netarsudil and 25 days for ripasudil. Conclusion: RECE after ROCK?I occurs with the use of both netarsudil and ripasudil, although the characteristics differ. The presence of corneal edema and endothelial decompensation seem to be a risk factor, and cautious use is warranted in these patients. Four clinical stages of RECE are described. ROCK?I act as a double?edged sword in patients with endothelial decompensation. Large?scale studies are required to know the exact incidence, pathophysiology, and long?term consequences of the aforementioned side?effect.
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@#AIM: To evaluate the efficacy and safety of ripasudil in the treatment of glaucoma in recent years by Meta-analysis.<p>METHODS:According to the Cochrane systematic review method, we searched three databases(Pubmed, Web of Knowledge and CNKI). The change of intraocular pressure was used to assess the effect of ripasudil, WMD with 95% confidence intervals(<i>CI</i>)were used to report the outcome. Subgroup analysis was performed according to different types of glaucoma.<p>RESULTS:A total of 9 trials all in English, totally 3446 patients, Meta-analysis showed that compared with before-treated groups, after-treated groups have significant lower IOP(Test of WMD= -2.96 95% <i>CI</i>: -3.48 to -2.45, <i>P</i><0.001), which indicates that ripasudil has great efficacy of curing glaucoma.<p>CONCLUSION:Ripasudil have significant efficacy in reducing IOP, which can be used as a treatment for glaucoma.
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Aim To evaluate the vasorelaxant effect of two new chemical entities, J35242 and J35243, on iso-lated rat thoracic aorta rings as Rho-kinase inhibitors, and further to explore the underlying mechanisms of these two compounds. Methods Isolated rat thoracic aorta rings pre-contracted by KCl or norepinephrine ( NE) were used to evaluate the vasodilatory effect of J35242 and J35243 . Through the interventions of sev-eral tool drugs, the mechanisms of compounds concern-ing endothelium, K+ channels and Ca2+ were studied. Results J35242 and J35243 showed potent relaxant effect on both KCl and NE pre-contracted vessels, and exhibited partial endothelium dependency. L-NAME and Methylene Blue( MB) could influence the relaxant effect of these compounds. Meanwhile, the compounds could inhibit intracellular Ca2+ release and extracellu-lar Ca2+ influx, which indicated that the compounds might block the calcium channels to relax the vessels. In addition, the two compounds probably did not dilate the aorta rings through opening potassium channels. Conclusions J35242 and J35243 have vasorelaxant effects on vessels in vitro and the potency of J35242 is stronger than that of J35243 . The underlying mecha-nisms might be endothelium-dependent. Also the com-pounds might block Ca2+ channels, lowering intracel-lular Ca2+ concentration to relax the vessels.
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Recent advances have seen a surge of new ideas and technologies to aid in the detection, treatment and further understanding of glaucoma. These technologies and advances are discussed to provide information on risk-factors, diagnosis and treatment. Glaucoma has never before seen such an advance in research and therapies coming forward in to the clinical workplace. It is an exciting time for physicians and researchers alike and over the next decade will certainly see advances in early detection, efficacious treatments and neuroprotection.