Acetazolamide: profile and news

Other information

Indication
For adjunctive treatment of: edema due to congestive heart failure; drug-induced edema; centrencephalic epilepsies; chronic simple (open-angle) glaucoma

Pharmacology
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.

Drug Category
Diuretics; Anticonvulsants; Carbonic Anhydrase Inhibitors; ATC:S01EC01

Brand Names/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

Dosage Forms
TABLET

Absorption
Not Available

Interactions
Interactions for Acetazolamide:

(see WARNlNGS).

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 advisable.

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 effect.

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.

Chemical IUPAC Name
N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)ethanamide

Chemical Formula
C4H6N4O3S2

Half Life
Not Available

Drug Type
Approved Drug

# Accession No
APRD00119

CAS Registry Number
59-66-5