A COMPARATIVE STUDY OF SOME CARBONIC ANHYDRASE INHIBITORS

A modification of a colorimetric method for the determination of carbonic anhydrase is described in which substrate is supplied in the form of gaseous carbon dioxide. Using this method, the inhibitory effects of seven carbonic anhydrase inhibitors used in the control of intraocular pressure were investigated. It was found that equilibrium between enzyme and inhibitor required from 2 minutes to 64 minutes to become established. A comparison of the inhibitory potencies of the various drugs is presented.

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Carbonic anhydrase inhibitors – part 70. Synthesis and ocular pharmacology of a new class of water-soluble, topically effective intraocular pressure lowering agents derived from nicotinic acid and aromatic/heterocyclic sulfonamides

European Journal of Medicinal Chemistry ◽

10.1016/s0223-5234(99)00212-3 ◽

1999 ◽

Vol 34 (10) ◽

pp. 799-808 ◽

Cited By ~ 9

Author(s):

C Supuran

Keyword(s):

Intraocular Pressure ◽

Carbonic Anhydrase ◽

Nicotinic Acid ◽

Water Soluble ◽

Carbonic Anhydrase Inhibitors ◽

New Class ◽

Pressure Lowering ◽

Aromatic Heterocyclic ◽

Ocular Pharmacology

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Carbonic Anhydrase Inhibitors Part 721 Synthesis and Antiglaucoma Properties of Metal Complexes of p-Fluorobenzolamide

Metal-Based Drugs ◽

10.1155/mbd.1999.67 ◽

1999 ◽

Vol 6 (2) ◽

pp. 67-73 ◽

Cited By ~ 8

Author(s):

Claudiu T. Supuran ◽

Andrea Scozzafava ◽

Luca Menabuoni ◽

Francesco Mincione ◽

Fabrizio Briganti ◽

...

Keyword(s):

Intraocular Pressure ◽

Carbonic Anhydrase ◽

Metal Ions ◽

Metal Complexes ◽

Carbonic Anhydrase Inhibitors ◽

Physico Chemical ◽

New Compounds

Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA) inhibitory properties, i.e., 5-(p-fluorobenzenesulfonylamido)-1,3,4-thiadiazole-2-sulfonamide (p-fluorobenzolamide) were prepared. The new complexes contained metal ions such as Zn(II), Cu(II), Co(II), Ni(II), Cd(II) and Mn(II). The new compounds were characterized by standard physico-chemical procedures, and assayed as inhibitors of three CA isozymes, CA I, II and IV. Very good inhibition has been evidenced both for the parent sulfonamides as well as for the prepared complexes, against all three investigated isozymes. Some of these new complexes as well as the parent sulfonamide, strongly lowered intraocular pressure (IOP) in normotensive rabbits when administered as a 2% solution into the eye.

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Again about carbonic anhydrase inhibitors: modern aspects of the use of ICA in ophthalmology

Archive of Ukrainian Ophthalmology ◽

10.22141/2309-8147.9.2.2021.241511 ◽

2021 ◽

Vol 9 (2) ◽

pp. 64-71

Author(s):

P.A. Bezdetko

Keyword(s):

Antioxidant Activity ◽

Intraocular Pressure ◽

Optic Nerve ◽

Carbonic Anhydrase ◽

Macular Edema ◽

Mechanism Of Action ◽

Corneal Endothelium ◽

Complex Treatment ◽

Efficacy And Safety ◽

Carbonic Anhydrase Inhibitors

For more than 70 years, the inhibitors of carbonic anhydrase (ICA) have been used in the treatment of glaucoma. Since 1995, topical forms of ICA have appeared among antiglaucoma drugs — dorzolamide, and since 1999 — brinzolamide. The hypotensive efficacy and safety of topical ICA gave rise to the widespread use of these drugs in the treatment of various forms of glaucoma. The peculiarities of the mechanism of action made it possible to create on their basis effective fixed combinations, which allow reducing the intraocular pressure by up to 40 % in patients with glaucoma. The attractiveness of the drug has expanded due to the effect of ICA on various tissues of the organ of vision. Thus, ICAs effectively improve the hemodynamics of the eye and optic nerve. The antioxidant activity of the drug makes it possible to expand the indications for its use in patients with vascular patho-logy of the retina and optic nerve. The biomechanical characte-ristics of the drug allowed its effective and safe use in the complex treatment of macular edema of various etiologies. The adjuvant use of topical ICAs expands the possibilities of anti-VEGF therapy in the treatment of macular edema of various etiologies. Features of the action of ICA on the endothelial pump function of the cornea made it possible to formulate the rules for the use of topical ICA in patients with an insufficient function of the corneal endothelium.

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