Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. Their anti-depressant and weight loss use has been established as anti- glaucoma agents, diureticsantiepilepticsin the management of mountain sicknessgastric and duodenal ulcersidiopathic intracranial hypertensionneurological disordersor osteoporosis.
Carbonic anhydrase inhibitors are primarily used for the treatment of glaucoma. They may also be used to treat seizure disorder and acute mountain sickness. Because they encourage solubilization and excretion of uric acid, they can be used in the treatment of gout, carbonic anhydrase inhibitors and diabetes. Acetazolamide is an inhibitor of carbonic anhydrase. It carbonic anhydrase inhibitors and diabetes used for glaucoma, epilepsy rarelyidiopathic intracranial hypertensionand altitude sickness.
For the reduction of intraocular pressure IOPacetazolamide inactivates carbonic anhydrase and interferes with the sodium pump, which decreases aqueous humor formation and thus lowers IOP.
Arterial Blood gases may show a mild hyperchloremic metabolic acidosis. Methazolamide is also a carbonic anhydrase inhibitor. It has a longer elimination half-life than acetazolamide and is less associated with adverse effects to the kidney. Carbonic anhydrase inhibitors and diabetes is a sulfonamide and topical carbonic anhydrase II inhibitor. It is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension and who are insufficiently responsive to beta-blockers.
Inhibition of carbonic anhydrase II in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. Brinzolamide trade names Azopt, Alcon Laboratories, Inc, Befardin Fardi Medicals is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. The combination of brinzolamide with timolol is marketed under the trade name Azarga.
Some diuretics  inhibit the activity of carbonic anhydrase in proximal convoluted tubules and prevent reabsorption of bicarbonates from renal tubules, resulting in osmotic diuresis. Acetazolamide is a carbonic anhydrase inhibitor. Acetazolamide is effective in the treatment of most types of seizures, including generalized tonic-clonic and focal seizures and especially absence seizures, although it has limited utility because tolerance develops with chronic use.
The drug is occasionally used on an intermittent basis to prevent seizures in catamenial epilepsy. The sulfur-containing antiseizure and antimigraine drug topiramate is a weak inhibitor of carbonic anhydrase, particularly subtypes II and IV, carbonic anhydrase inhibitors and diabetes.
In rare cases, the inhibition of carbonic anhydrase may be strong enough to cause metabolic acidosis of clinical importance.
Zonisamide is another sulfur containing antiseizure drug that weakly inhibits carbonic anhydrase. At high altitude, the partial pressure of oxygen is lower and people have to breathe more rapidly to get adequate oxygen. When this happens, the partial pressure of CO2 in the lungs pCO2 decreases is "blown off"causing a respiratory alkalosis.
This would normally be compensated by the kidney excreting bicarbonate and causing compensatory metabolic acidosisbut this mechanism takes several days. A more immediate treatment is carbonic anhydrase inhibitors, which prevent bicarbonate uptake in the kidney and help correct the alkalosis.
Loss of bicarbonate may result in metabolic acidosis. Ellagitannins extracted from the pericarps of Punica granatumthe pomegranate, such as punicalinpunicalagincarbonic anhydrase inhibitors and diabetes, granatin Bgallagyldilactonecasuarininpedunculagin and tellimagrandin Iare carbonic anhydrase inhibitors.
From Wikipedia, the free encyclopedia. Carbonic anhydrase inhibitor Drug class Acetazolamide. Expert Opinion on Therapeutic Patents. Neptazane Rmethazolamide. The Extra Pharmacopoeia electronic version. Cold Spring Harb Perspect Med. In Frost, Susan C. Experimental Biology and Medicine. New England Journal of Medicine. Competitive inhibition Uncompetitive inhibition Non-competitive inhibition Suicide inhibition Mixed inhibition.
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