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Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. Their clinical use has been established as anti- glaucoma agents, diuretics , antiepileptics , in the management of mountain sickness , gastric and duodenal ulcers , idiopathic intracranial hypertension , neurological disorders , or ...
For example, carbonic anhydrase produces acid in the stomach lining. In the kidney, the control of bicarbonate ions influences the water content of the cell. The control of bicarbonate ions also influences the water content in the eyes. Inhibitors of carbonic anhydrase are used to treat glaucoma, the excessive build-up of water in the eyes.
Sultiame (or sulthiame) is a sulfonamide and inhibitor of the enzyme carbonic anhydrase. It is used as an anticonvulsant and in recent studies showed promise in reducing sleep disordered breathing and other symptoms of obstructive sleep apnea (OSA).
Acetazolamide is a carbonic anhydrase inhibitor, hence causing the accumulation of carbonic acid. [12] Carbonic anhydrase is an enzyme found in red blood cells and many other tissues that catalyses the following reaction: [26] H 2 CO 3 ⇌ H 2 O + CO 2. hence lowering blood pH, by means of the following reaction that carbonic acid undergoes: [27]
While definitive sites of metabolism have not been firmly established, there are several metabolites worthy of note. N-Desethylbrinzolamide is an active metabolite of the parent compound, and thus exhibits carbonic anhydrase inhibitory activity (largely carbonic anhydrase-I, when in the presence of Brinzolamide) and also accumulates in the erythrocytes.
Methazolamide (trade name Neptazane) is a potent carbonic anhydrase inhibitor. It is indicated in the treatment of increased intraocular pressure (IOP) in chronic open-angle glaucoma and secondary glaucoma. Also it is used preoperatively in acute angle-closure (narrow-angle) glaucoma where lowering the IOP is desired before surgery.
Diclofenamide (or dichlorphenamide) is a sulfonamide and a carbonic anhydrase inhibitor of the meta-disulfamoylbenzene class.Dichlorphenamide as a carbonic anhydrase inhibitor is used for the treatment of acute angle closure glaucoma.
The reaction catalyzed by CA1 is the same as other carbonic anhydrase family proteins: + (in tissues - high CO 2 concentration) [9]. The CA1-catalyzed reaction has a relatively low reaction affinity (Km) of 4.0 mM for CO 2, [7] [10] turnover number (Kcat) of 2 × 10 5 s −1, and catalytic efficiency (Kcat/Km) of 5 × 10 7 M −1 s −1 comparing to other isozymes of the α-CA family of ...