Carbonic Anhydrase Inhibitors in the Treatment of Glaucoma. Review. Part I

Курышева, Н. И.

doi:10.18008/1816-5095-2020-3s-542-549

Cited by 7 publications

(4 citation statements)

References 73 publications

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“…The human carboanhydrase II isoform (HCA II) is known to be a classic target for the treatment of glaucoma [2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Development of the chromatographic separation methodology and impurity profiling of 5-(5-trifluoromethyl-isoxazol-3-yl)furan-2-sulfonamide, a drug candidate for the glaucoma treatment

Ivanovskiy,

Yaichkov,

Shetnev

et al. 2023

From Chemistry Towards Technology Step-by-Step

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Glaucoma is the leading cause of irreversible blindness. Early diagnosis and effective treatment can reduce the progression of the disease and prevent irreversible decay of visual functions. Indeed, human carboanhydrase isoform II is a classical target for glaucoma treatment. We proposed a compound molecule 5 (5 trifluoromethyl-isoxazol-3-yl)furan-2-sulfonamide under the project name B016, which showed high activity as a human carboanhydrase II inhibitor by in vitro tests. Our team is currently conducting development and preclinical studies of a medicinal product in the eye drops form based on this compound. One of the stages of pharmaceutical research is the development of quality control methods for both the pharmaceutical substance and the finished dosage form. We have developed a chromatographic separation procedure, which can be used for quality control of active pharmaceutical substance by quantification indicators. We also determined the impurity profile, i.e. the structure of the impurities found in the reaction product of compound B016.

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“…The human carboanhydrase II isoform (HCA II) is known to be a classic target for the treatment of glaucoma [2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Development of the chromatographic separation methodology and impurity profiling of 5-(5-trifluoromethyl-isoxazol-3-yl)furan-2-sulfonamide, a drug candidate for the glaucoma treatment

Ivanovskiy,

Yaichkov,

Shetnev

et al. 2023

From Chemistry Towards Technology Step-by-Step

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“…This is a fairly common ophthalmic disease, which is the leading cause of irreversible blindness. According to the World Health Organization, the number of glaucoma patients in the world ranges from 60.5 to 105 million people, while the number of cases is predicted to increase by another 10 million over the next 10 years (Tham et al 2014;Kurysheva 2020).…”

Section: Introductionmentioning

confidence: 99%

“…The emergence, development and progression of glaucoma is a sequence of risk factors that are summed up in their action, resulting in the triggering of a mechanism that leads to the onset of the disease. Thus, the pathogenesis of glaucoma is complex and not fully understood, which ultimately determines the development of eye dysfunctions despite the treatment (Kurysheva 2020).…”

Section: Introductionmentioning

confidence: 99%

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Modeling experimental glaucoma for screening studies of antiglaucomatous activity

Fedorov,

Korsakov,

Vdovichenko

et al. 2023

RRP

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Introduction: In vivo screening studies, in which the efficacy of dozens of drugs is tested to select several applicants for further study of their safety in humans, are the main stage in the study of the pharmacodynamics of promising antiglaucoma drugs. This imposes a number of specific requirements both on experimental models of glaucoma and on laboratory animals used in the experiment. Materials and Methods: 32 male rabbits of the Soviet Сhinchilla breed, 6 male albino rabbits weighing 3-3.5 kg, and 20 outbred white rats weighing 220-250 g were used in total in experiments to reproduce the glaucoma process. All manipulations on the rabbit eye were performed by an ophthalmologist under general anesthesia with telazol. Triamcinolone (vitreous injection) was used to simulate glaucoma in rabbits, lauromacrogol 400 or fine kaolin (anterior chamber injection) was used to simulate glaucoma in rabbits; adrenaline hydrochloride (intraperitoneal administration) was used to simulate glaucoma in rats. Results and Discussion: Double intravitreal administration of a suspension of triamcinolone at a dose of 4 mg was the most attractive model in terms of the technique of reproducing the pathology and the results obtained in modeling glaucoma in rabbits. However, this model did not produce a stable increase in intraocular pressure (IOP). Doubling the dose of triamcinolone and replacing chinchilla rabbits with albinos did not lead to a positive result. The introduction of the venous sclerosing drug lauromacrogol 400 into the anterior chamber of the eye proved to be ineffective either. The introduction of finely dispersed kaolin into the anterior chamber of the eye of rabbits led to a persistent increase in IOP. The intraperitoneal administration of epinephrine hydrochloride to rats according to the described method gave no stable results. The increase in IOP became stable only after a significant increase in the dose of adrenaline. Conclusion: The conducted studies of four models of glaucoma and their three modifications in animals made it possible to select two of them, which contributed to a stable and fairly long-term increase in IOP in rabbits (introduction of finely dispersed kaolin into the anterior chamber of the eye) and rats (adrenaline-induced model).

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Pharmacological Properties of Sulfonamide Derivatives, New Inhibitors of Carbonic Anhydrase

et al. 2023

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Carbonic Anhydrase Inhibitors in the Treatment of Glaucoma. Review. Part I

Cited by 7 publications

References 73 publications

Development of the chromatographic separation methodology and impurity profiling of 5-(5-trifluoromethyl-isoxazol-3-yl)furan-2-sulfonamide, a drug candidate for the glaucoma treatment

Development of the chromatographic separation methodology and impurity profiling of 5-(5-trifluoromethyl-isoxazol-3-yl)furan-2-sulfonamide, a drug candidate for the glaucoma treatment

Modeling experimental glaucoma for screening studies of antiglaucomatous activity

Pharmacological Properties of Sulfonamide Derivatives, New Inhibitors of Carbonic Anhydrase

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