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QuickView for Acetazolamide (compound)


PubChem
Name: Acetazolamide
PubChem Compound ID: 1986
Description: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)
Molecular formula: C4H6N4O3S2
Molecular weight: 222.248 g/mol
Synonyms:
Acetazolamide (JP15/USP); EU-0100039; Prestwick1_000003; C06805; 2-Acetylamino-1,3,4-thiadiazole-5-sulfonamide; SPBio_001926; CHEBI:27690; Acetazoleamide; KBio2_000358; Diluran.
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DrugBank
Identification
Name: Acetazolamide
Name (isomeric): DB00819
Drug Type: small molecule
Description: One of the CARBONIC ANHYDRASE INHIBITORS that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)
Synonyms:
Acetozalamide; Acetazolamine; Acetazolamid; Carbonic Anhydrase Inhibitor 6063; Acetazoleamide; Acetazolamide Sodium; Acetamidothiadiazolesulfonamide
Brand: Diutazol, Apo-Acetazolamide, Ak-Zol, Eumicton, Dazamide, Nephramid, Atenezol, Fonurit, Natrionex, Acetamox, Duiramid, Glaupax, Defiltran, Diakarb, Storzolamide, Dehydratin, Didoc, Donmox, Glupax, Diamox Sequels, Phonurit, Nephramide, Diacarb, Vetamox, Diamox, Acetazolam, Diuramid, Diuriwas, Diluran, Sk-Acetazolamide, Cidamex, Edemox, Diureticum-Holzinger
Category: Carbonic Anhydrase Inhibitors, Diuretics, Anticonvulsants
CAS number: 59-66-5
Pharmacology
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 ...
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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 a...
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Protein binding: 98%
Half Life: 3 to 9 hours
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Take with food; at least 6 hours before bedtime.
Drink plenty of liquids.
Drug interaction:
TopiramateAdditive renal carbonic anhydrase inhibition may occur increasing the risk of crystaluria and renal calculi. Increased risk of nephrolithiasis. Consider altnerate therapy.
CyclosporineAcetazolamide may increase the effect and toxicity of cyclosporine.
BrinzolamideAs both brinzolamide and acetazolamide are carbonic anhydrase inhibitors, there is an increased risk of adverse effects.The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Avoid concurrent use of different carbonic anhydrase inhibitors when possible.
TriprolidineThe CNS depressants, Triprolidine and Acetazolamide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
TobramycinIncreased risk of nephrotoxicity
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