Brands, Medical Use, Clinical Data
- Carbonic Anhydrase Inhibitors
Brands / Synonyms
Acetamidothiadiazolesulfonamide; Acetamox; Acetazolam; Acetazolamid; Acetazolamide; Acetazolamide Sodium; Acetazolamine; Acetazoleamide; Acetozalamide; Ak-Zol; Apo-Acetazolamide; Atenezol; Carbonic Anhydrase Inhibitor; Carbonic Anhydrase Inhibitor 6063; Cidamex; Dazamide; Defiltran; Dehydratin; Diacarb; Diakarb; Diamox; Diamox Sequels; Didoc; Diluran; Diuramid; Diureticum-Holzinger; Diuriwas; Diutazol; Donmox; Duiramid; Edemox; Eumicton; Fonurit; Glaupax; Glupax; Natrionex; Nephramid; Nephramide; Phonurit; Sk-Acetazolamide; Storzolamide; Vetamox
For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma
Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion, in the treatment of certain convulsive disorders and in the promotion of diuresis in instances of abnormal fluid retention. Acetazolamide is not a mercurial diuretic. Rather, it is a nonbacteriostatic sulfonamide possessing a chemical structure and pharmacological activity distinctly different from the bacteriostatic sulfonamides.
Mechanism of Action
The anticonvulsant activity of Acetazolamide may depend on a direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. This leads to alkaline urine and an increase in the excretion of bicarbonate, sodium, potassium, and water.
Biotrnasformation / Drug Metabolism
Hypersensitivity to acetazolamide or any excipients in the formulation. Since acetazolamide is a sulfonamide
derivative, cross sensitivity between acetazolamide, sulfonamides and other sulfonamide derivatives is possible.
DIAMOX therapy is contraindicated in situations in which sodium and/or potassium blood serum levels are depressed,
in cases of marked kidney and liver disease or dysfunction, in suprarenal gland failure, and in hyperchloremic
acidosis. It is contraindicated in patients with cirrhosis because of the risk of development of hepatic
Long-term administration of DIAMOX is contraindicated in patients with chronic noncongestive angle-closure
glaucoma since it may permit organic closure of the angle to occur while the worsening glaucoma is masked by lowered
DIAMOX®. modifies phenytoin metabolism with increased serum levels of phenytoin. This may increase or enhance
the occurrence of osteomalacia in some patients receiving chronic phenytoin therapy. Caution is advised in patients
receiving chronic concomitant therapy.
By decreasing the gastrointestinal absorption of primidone, DIAMOX may decrease serum concentrations of primidone
and its metabolites, with a consequent possible decrease in anticonvulsant effect. Caution is advised when beginning,
discontinuing, or changing the dose of DIAMOX in patients receiving primidone.
Because of possible additive effects with other carbonic anhydrase inhibitors, concomitant use is not
Acetazolamide may increase the effects of other folic acid antagonists.
Acetazolamide may increase or decrease blood glucose levels. Consideration should be taken in patients being
treated with antidiabetic agents.
Acetazolamide decreases urinary excretion of amphetamine and may enhance the magnitude and duration of their
Acetazolamide reduces urinary excretion of quinidine and may enhance its effect.
Acetazolamide may prevent the urinary antiseptic effect of methenamine.
Acetazolamide increases lithium excretion and the lithium may be decreased.
Acetazolamide and sodium bicarbonate used concurrently increases the risk of renal calculus formation.
Acetazolamide may elevate cyclosporine levels.