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Acetazolamide, usually sold under the trade name Diamox in some countries, is a health system.[3]
It is used in the treatment of glaucoma, drug-induced edema, heart failure-induced edema, centrencephalic epilepsy and in reducing intraocular pressure after surgery.[4][5] It has also been used in the treatment of mountain sickness,[6] Ménière's disease, increased intracranial pressure and neuromuscular disorders.[2]
In epilepsy, the main use of acetazolamide is in menstrual-related epilepsy and as an adjunct in refractory epilepsy.[4][7] It has been demonstrated in drug trials to relieve symptoms associated with [10][11] Acetazolamide is not an immediate cure for acute mountain sickness; rather, it speeds up part of the acclimatization process which in turn helps to relieve symptoms.[12]
It has also been used to prevent methotrexate-induced kidney damage by alkalinalizing one's urine, hence speeding up methotrexate excretion by increasing its solubility in urine.[2][13]
Acetazolamide is pregnancy category B3 in Australia, which means that studies in rats, mice and rabbits in which acetazolamide was given intravenously or orally caused an increased risk of fetal malformations, including defects of the limbs.[5] Despite this there is insufficient evidence from studies in humans to either support or discount this evidence.[5] It is also excreted in breast milk and hence breastfeeding is advised against in mothers taking this drug.[5]
Common adverse effects of acetazolamide include the following: paraesthesia, fatigue, drowsiness, depression, decreased libido, bitter or metallic taste, nausea, vomiting, abdominal cramps, diarrhea, black feces, polyuria, kidney stones, metabolic acidosis and electrolyte changes (hypokalemia, hyponatremia).[4] Whereas less common adverse effects include: Stevens-Johnson syndrome, anaphylaxis and blood dyscrasias.[4]
Contraindications include:[5]
It is possible that it might interact with:[5]
Acetazolamide is a carbonic anhydrase inhibitor, hence causing the accumulation of carbonic acid[2] Carbonic anhydrase is an enzyme found in red blood cells that catalyses the following reaction:[14]
\textrm{H}_2 \textrm{CO}_3 \rightleftharpoons \textrm{H}_2 \textrm{O} + \textrm{CO}_2
hence lowering blood pH, by means of the following reaction that carbonic acid undergoes:[15]
\textrm{H}_2 \textrm{CO}_3 \rightleftharpoons \textrm{HCO}_3^- + \textrm{H}^+
which has a pKa of 6.3.[15]
In the eye this results in a reduction in aqueous humour.[5]
The mechanism of diuresis involves the proximal tubule of the kidney. The enzyme carbonic anhydrase is found here, allowing the reabsorption of bicarbonate, sodium, and chloride. By inhibiting this enzyme, these ions are excreted, along with excess water, lowering blood pressure, intracranial pressure, and intraocular pressure. By excreting bicarbonate, the blood becomes acidic, causing compensatory hyperventilation, increasing levels of oxygen and decreasing levels of carbon dioxide in the blood.[16]
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