Нейропротекторные свойства бримонидина

Abstract

Purpose. To summarize relevant data from publications appearing in the peer-reviewed scientific literature since1991 about mechanisms of neurodegeneration in glaucoma and the possibilities of neuroprotection; in particular, analysis of the results of laboratory and clinical studies on the neuroprotective properties of Brimonidine. Neurodegenerative processes in glaucoma occur due to ischemia and ocular blood flow disturbance, excitotoxicity, oxidative stress, neuroinflammation, as well as decrease in the level of neurotrophic factors, mitochondrial dysfunction, activation of apoptosis signaling pathways, protein dysfunction and genetic causes. In patients with glaucoma, these processes continue despite the optimization of intraocular pressure. In animal studies, Brimonidine has been shown to increase the ability of retinal ganglion cells (RGC) to survive in stress conditions. The mechanism of neuroprotective action of Brimonidine is multifaceted. The effects of brimonidine are mediated by its interaction with alpha-2 adrenergic receptors that are present in the retina. Clinical dosing of the topical formulation of brimonidine results in brimonidine concentrations in the posterior segment that are sufficient for both pharmacological activity at alpha-2 adrenergic receptors and neuroprotection. Brimonidine inhibits almost all known causes of cell apoptosis and neurodegeneration in glaucoma.Brimonidine reduces the severity of retinal ischemia, reduces the effect of excitotoxic amino acids on RGC, blocks the effects of oxidative stress, increases the production of neurotrophic factors, and regulates the function of glial cells and mitochondria. Its neuroprotective efficacy has been proven in animal studies and in human clinical studies. Brimonidine is the only antiglaucoma drug whose direct neuroprotective effect has been proven in large randomized clinical trials. Brimonidine can be used in glaucoma and diabetic retinopathy to prevent visual impairment associated with RGC death. Brimonidine helps to preserve, and in some cases to improve the visual field, contrast sensitivity and visual functions in general.