Ethoxzolamide

log Kow = 2.01

0.4

CRYSTALS FROM ETHYL ACETATE + SKELLYSOLVE B

WHITE OR SLIGHTLY YELLOW CRYSTALLINE POWDER

SLIGHTLY SOL IN ALC, ACETONE, CHLOROFORM & ETHER; PRACTICALLY INSOL IN WATER

Water solubility = 40 mg/l @ 25 deg

6.88e-01 g/L

>38.7 [ug/mL] (The mean of the results at pH 7.4)

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

188-190.5

188-190.5 °C

189 °C

Warning

H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]

P261, P264, P264+P265, P271, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 39 reports by companies from 2 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

PATIENTS RECEIVING DIGITALIS GLYCOSIDES, HYPOKALEMIA MAY PREDISPOSE PATIENT TO DIGITALIS TOXICITY & POSSIBLY FATAL CARDIAC ARRHYTHMIAS MAY RESULT... DIURETICS, CORTICOSTEROIDS, CORTICOTROPIN & AMPHOTERICIN B /USED CONCOMITANTLY WITH CARBONIC ANHYDRASE INHIBITORS MAY CAUSE SEVERE HYPOKALEMIA/

CARBONIC ANHYDRASE INHIBITORS MAY AUGMENT EFFECTS OF OTHER DIURETICS SUCH AS THIAZIDES.../USEFUL/ IN ENHANCING & RESTORING RESPONSIVENESS TO MERCURIAL DIURETICS...RARELY, /DRUG/ MAY INTERFERE WITH HYPOGLYCEMIC RESPONSE TO INSULIN OR ORAL HYPOGLYCEMIC DRUGS, POSSIBLY BY CAUSING HYPOKALEMIA.

ALKALINIZATION OF URINE PRODUCED BY /DRUG INCREASES/ RATE OF EXCRETION OF WEAK ACIDS, INCLUDING PHENOBARBITAL & SALICYLATES...METHENAMINE, METHENAMINE HIPPURATE, & METHENAMINE MANDELATE...MAY BE INACTIVE IN ALKALINE URINE PRODUCED BY CARBONIC ANHYDRASE INHIBITORS.

Ethoxzolamide is an inhibitor of the carbonic anhydrase enzyme in proximal renal tubules that works by decreasing the reabsorption of water, sodium, potassium, bicarbonate. It also decreases the activity of carbonic anhydrase expressed in the CNS, which leads to increased seizure threshold. Inhibition of carbonic anhydrase in the eye contributes to its effect of reducing intraocular pressure and decreasing aqueous humor.

Ethoxzolamide binds to and inhibits carbonic anhydrase I, which plays an essential role in facilitating the transport of CO2 and H+ in the intracellular space, across biological membranes, and in the layers of the extracellular space. Through inhibition of the enzyme, the balance of applicable membrane equilibrium systems are affected.

MAJOR PHARMACOLOGICAL ACTION...IS INHIBITION OF...CARBONIC ANHYDRASE. STUDIES WITH PURIFIED ENZYME HAVE SHOWN THAT INHIBITION IS NONCOMPETITIVE. NONCATALYZED HYDRATION OR DEHYDRATION REACTION CAN TAKE PLACE, OF COURSE, IN ABSENCE OF ENZYME.

CARBONIC ANHYDRASE INHIBITORS...DECR CONCN OF HYDROGEN IONS AVAIL FOR EXCHANGE WITH SODIUM & POTASSIUM & TO COMBINE WITH BICARBONATE TO FORM CARBONIC ACID. /CARBONIC ANHYDRASE INHIBITORS/

...EFFECT /OF CARBONIC ANHYDRASE INHIBITORS/ ON INTRAOCULAR PRESSURE DOES NOT DEPEND UPON DIURESIS. THEY REDUCE AQUEOUS PRODN ... & THUS LOWER PRESSURE. /CARBONIC ANHYDRASE INHIBITORS/

A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES.

Agents that promote the excretion of urine through their effects on kidney function.

Rapidly absorbed with 65% bioavailability

ABSORBED FROM GI TRACT...DISTRIBUTED IN PLASMA, MUSCLES, BRAIN, KIDNEYS, LIVER, LUNGS, ERYTHROCYTES, AQUEOUS HUMOR, & CSF. APPROX 40%...EXCRETED UNCHANGED BY KIDNEYS /HUMAN, ORAL/