Please Wait
Applying Filters...
menu
    • menu
    DRL offers a portfolio of products & services, including APIs, CMO services, generics, biosimilars & differentiated formulations.

    Virtual Booth

    Contact Supplier

    Valsynthese, part of the SSE Group, is a CDMO focused on highly energetic and highly hazardous chemistry.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2024-10-07

    Virtual Booth

    Contact Supplier

    With Fermion, start the journey of your innovative API.

    Virtual Booth

    Contact Supplier

    Bloomage is a one-stop source for CEP Sodium Hyaluronate and Hyaluronic Acid// FDA-inspected & GMP-certified.

    Virtual Booth

    Contact Supplier

    xyz-pharma-m-2024-10-07

    Virtual Booth

    Contact Supplier

    Menu

    Acetazolamide

    ACTIVE PHARMA INGREDIENTS

    DEVELOPMENTS

    INTERMEDIATES

    FINISHED DOSAGE FORMULATIONS

    RELATED EXCIPIENT COMPANIES

    EXCIPIENTS BY APPLICATIONS

    DIGITAL CONTENT

    GLOBAL SALES INFORMATION

    MARKET PLACE

    REF. STANDARDS & IMPURITIES

    ANALYTICAL

    PharmaCompass
    $ API Ref.Price (USD/KG) : 57Xls

    Filters

    clear-filterReset all filters
    2D Structure
    Also known as: 59-66-5, Diamox, Acetamox, N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide, Glaupax, Acetazolamid
    Molecular Formula
    C4H6N4O3S2
    Molecular Weight
    222.3  g/mol
    InChI Key
    BZKPWHYZMXOIDC-UHFFFAOYSA-N
    FDA UNII
    O3FX965V0I
    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)
    Acetazolamide is a Carbonic Anhydrase Inhibitor. The mechanism of action of acetazolamide is as a Carbonic Anhydrase Inhibitor.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
    2.1.2 InChI
    InChI=1S/C4H6N4O3S2/c1-2(9)6-3-7-8-4(12-3)13(5,10)11/h1H3,(H2,5,10,11)(H,6,7,9)
    2.1.3 InChI Key
    BZKPWHYZMXOIDC-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CC(=O)NC1=NN=C(S1)S(=O)(=O)N
    2.2 Other Identifiers
    2.2.1 UNII
    O3FX965V0I
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Acetadiazol

    2. Acetazolam

    3. Acetazolamide Sodium, (sterile)

    4. Acetazolamide, Monosodium Salt

    5. Ak Zol

    6. Ak-zol

    7. Akzol

    8. Apo Acetazolamide

    9. Apo-acetazolamide

    10. Apoacetazolamide

    11. Dfiltran

    12. Diacarb

    13. Diamox

    14. Diuramide

    15. Edemox

    16. Glauconox

    17. Glaupax

    18. Huma Zolamide

    19. Huma-zolamide

    20. Humazolamide

    2.3.2 Depositor-Supplied Synonyms

    1. 59-66-5

    2. Diamox

    3. Acetamox

    4. N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide

    5. Glaupax

    6. Acetazolamid

    7. Defiltran

    8. Nephramide

    9. Edemox

    10. Phonurit

    11. Diacarb

    12. Donmox

    13. Didoc

    14. Cidamex

    15. Diluran

    16. Diuriwas

    17. Dehydratin

    18. Diuramid

    19. Diutazol

    20. Duiramid

    21. Eumicton

    22. Natrionex

    23. Nephramid

    24. Diakarb

    25. Fonurit

    26. Glupax

    27. Vetamox

    28. Sk-acetazolamide

    29. 5-acetamido-1,3,4-thiadiazole-2-sulfonamide

    30. Acetazolamidum

    31. Acetazoleamide

    32. Acetozalamide

    33. Diureticum-holzinger

    34. Acetamidothiadiazolesulfonamide

    35. Acetazolamida

    36. 4-diamox

    37. Acetamide, N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]-

    38. Carbonic Anhydrase Inhibitor No. 6063

    39. 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide

    40. N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]acetamide

    41. Atenezo

    42. 2-acetamido-5-sulfonamido-1,3,4-thiadiazole

    43. Carbonic Anhydrase Inhibitor 6063

    44. Nsc 145177

    45. 1,3,4-thiadiazole-2-sulfonamide, 5-acetamido-

    46. N-(5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl)acetamide

    47. 5-acetamide-1,3,4-thiadiazole-2-sulfonamide

    48. Chembl20

    49. Diamox (tn)

    50. Nsc-145177

    51. Mls000028435

    52. O3fx965v0i

    53. Acetamide, N-(5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl)-

    54. Chebi:27690

    55. Acetamide, N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-

    56. Cas-59-66-5

    57. Ncgc00015074-10

    58. Acetazolamine

    59. Atenezol

    60. Glaumox

    61. Smr000058394

    62. Diamox Sequels

    63. Dsstox_cid_2544

    64. 5-acetylamino-1,3,4-thiadiazole-2-sulfonamide

    65. Dsstox_rid_76621

    66. Dsstox_gsid_22544

    67. L 579486

    68. Acetazolamidum [inn-latin]

    69. Acetazolamida [inn-spanish]

    70. N-[5-(aminosulfonyl)-1,3,5-thiadiazol-2-yl]acetamide

    71. Ccris 5811

    72. Acetazolamide (aaz)

    73. Hsdb 3002

    74. Sr-01000000065

    75. Einecs 200-440-5

    76. Mfcd00003105

    77. Unii-o3fx965v0i

    78. Ai3-52458

    79. Prestwick_4

    80. 1azm

    81. 1yda

    82. 1ydb

    83. 1ydd

    84. 1zsb

    85. 2xtk

    86. 3czv

    87. 3ucj

    88. Acetazolamide, 5

    89. Acetazolamide [usp:inn:ban:jan]

    90. Acerazolamide, Aaz

    91. Acetazolamide, Aaz

    92. Acetazolamide, Aza

    93. Acetazolamide, Azm

    94. Spectrum_000018

    95. 1jd0

    96. 2h4n

    97. 2uy4

    98. 3dc3

    99. 3hs4

    100. 3ml5

    101. 4g0c

    102. Opera_id_288

    103. Aza2

    104. Prestwick0_000003

    105. Prestwick1_000003

    106. Prestwick2_000003

    107. Prestwick3_000003

    108. Spectrum2_000082

    109. Spectrum3_000284

    110. Spectrum4_000139

    111. Spectrum5_000738

    112. Lopac-a-6011

    113. Acetazolamide [mi]

    114. A 6011

    115. Acetazolamide [inn]

    116. Acetazolamide [jan]

    117. Acetazolamide [hsdb]

    118. Lopac0_000039

    119. Schembl23219

    120. Acetazolamide [vandf]

    121. Bspbio_000005

    122. Bspbio_001788

    123. Kbiogr_000558

    124. Kbioss_000358

    125. Mls001148438

    126. Acetazolamide [mart.]

    127. Bidd:gt0643

    128. Divk1c_000017

    129. Spectrum1500102

    130. N-(5-sulfamoyl-[1,3,4]thiadiazol-2-yl)-acetamide

    131. Spbio_000004

    132. Spbio_001926

    133. Acetazolamide [usp-rs]

    134. Acetazolamide [who-dd]

    135. Acetazolamide [who-ip]

    136. Bpbio1_000007

    137. Gtpl6792

    138. (non-d)acetazolamide-13c2-d3

    139. Acetazolamide, >=99%, Powder

    140. Dtxsid7022544

    141. Schembl11049053

    142. Bdbm10880

    143. Bzkpwhyzmxoidc-uhfffaoysa-

    144. Hms500a19

    145. Kbio1_000017

    146. Kbio2_000358

    147. Kbio2_002926

    148. Kbio2_005494

    149. Kbio3_001288

    150. Acetazolamide (jp17/usp/inn)

    151. Amy3289

    152. N-[5-(aminosulfonyl)-1,3,4-thiadiozol-2-yl]-acetamide

    153. Acetazolamide, Analytical Standard

    154. Ninds_000017

    155. Hms1568a07

    156. Hms1920a05

    157. Hms2091g05

    158. Hms2095a07

    159. Hms2232g23

    160. Hms3259i13

    161. Hms3260g19

    162. Hms3370p01

    163. Hms3712a07

    164. Hms3744a21

    165. Pharmakon1600-01500102

    166. Wln: T5nn Dsj Cszw Emv1

    167. Acetazolamide [ep Impurity]

    168. Acetazolamide [orange Book]

    169. Albb-023617

    170. Bcp29616

    171. Hy-b0782

    172. Zinc3813042

    173. Acetazolamide [ep Monograph]

    174. Tox21_110078

    175. Tox21_201559

    176. Tox21_302773

    177. Tox21_500039

    178. Acetazolamide [usp Monograph]

    179. Ccg-38900

    180. Nsc145177

    181. Nsc755854

    182. S4506

    183. Acetazolamidum [who-ip Latin]

    184. Akos000715163

    185. Tox21_110078_1

    186. Cs-3568

    187. Db00819

    188. Lp00039

    189. Nc00491

    190. Nsc-755854

    191. Sdccgsbi-0050028.p005

    192. Idi1_000017

    193. Ncgc00015074-01

    194. Ncgc00015074-02

    195. Ncgc00015074-03

    196. Ncgc00015074-04

    197. Ncgc00015074-05

    198. Ncgc00015074-06

    199. Ncgc00015074-07

    200. Ncgc00015074-08

    201. Ncgc00015074-09

    202. Ncgc00015074-11

    203. Ncgc00015074-12

    204. Ncgc00015074-14

    205. Ncgc00015074-15

    206. Ncgc00015074-17

    207. Ncgc00015074-22

    208. Ncgc00023455-03

    209. Ncgc00023455-04

    210. Ncgc00023455-05

    211. Ncgc00023455-06

    212. Ncgc00023455-07

    213. Ncgc00256374-01

    214. Ncgc00259108-01

    215. Ncgc00260724-01

    216. Ac-12779

    217. As-13169

    218. Sbi-0050028.p004

    219. 2-acetamido-5-sulfonamido-1,4-thiadiazole

    220. 5-acetamide-1,4-thiadiazole-2-sulfonamide

    221. Db-053437

    222. 5-acetamido-1,3,4-thiadiazol-2-sulfonamide

    223. Ab00051906

    224. Eu-0100039

    225. 1,4-thiadiazole-2-sulfonamide, 5-acetamido-

    226. C06805

    227. D00218

    228. D88526

    229. Ab00051906_15

    230. 003a105

    231. A832415

    232. N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)ethanamide

    233. Q413690

    234. Q-200579

    235. Q-200580

    236. Sr-01000000065-2

    237. Sr-01000000065-4

    238. Sr-01000000065-6

    239. Brd-k43457670-001-22-9

    240. Brd-k43457670-001-26-0

    241. Z277559108

    242. (1z)-n-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)ethanimidic Acid

    243. Acetazolamide, European Pharmacopoeia (ep) Reference Standard

    244. Acetazolamide, United States Pharmacopeia (usp) Reference Standard

    245. N - (5 - Sulfamoyl - 1,3, 4 - Thiadiazol - 2 - Yl) Acetamide

    246. Acetazolamide For System Suitability, European Pharmacopoeia (ep) Reference Standard

    247. Acetazolamide, Pharmaceutical Secondary Standard; Certified Reference Material

    248. 124442-28-0

    2.4 Create Date
    2005-03-25
    3 Chemical and Physical Properties
    Molecular Weight 222.3 g/mol
    Molecular Formula C4H6N4O3S2
    XLogP3-0.3
    Hydrogen Bond Donor Count2
    Hydrogen Bond Acceptor Count7
    Rotatable Bond Count2
    Exact Mass221.98813241 g/mol
    Monoisotopic Mass221.98813241 g/mol
    Topological Polar Surface Area152 Ų
    Heavy Atom Count13
    Formal Charge0
    Complexity297
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Information
    1 of 4  
    Drug NameAcetazolamide
    PubMed HealthAcetazolamide
    Drug ClassesAnticonvulsant, Antiglaucoma, Cardiovascular Agent, Musculoskeletal Agent, Renal-Urologic Agent, Urinary Stone Agent
    Drug LabelAcetazolamide, an inhibitor of the enzyme carbonic anhydrase is a white to faintly yellowish white crystalline, odorless powder, weakly acidic, very slightly soluble in water and slightly soluble in alcohol. The chemical name for acetazolamide is N-(...
    Active IngredientAcetazolamide
    Dosage FormTablet; Capsule, extended release
    RouteOral
    Strength250mg; 125mg; 500mg
    Market StatusPrescription
    CompanyMutual Pharm; Lannett; Taro; Zydus Pharms Usa; Heritage Pharms

    2 of 4  
    Drug NameDiamox
    PubMed HealthAcetazolamide (By mouth)
    Drug ClassesAnticonvulsant, Antiglaucoma, Cardiovascular Agent, Musculoskeletal Agent, Renal-Urologic Agent, Urinary Stone Agent
    Drug LabelDIAMOX SEQUELS (Acetazolamide Extended-Release Capsules) are an inhibitor of the enzyme carbonic anhydrase.DIAMOX is a white to faintly yellowish white crystalline, odorless powder, weakly acidic, very slightly soluble in water, and slightly soluble...
    Active IngredientAcetazolamide
    Dosage FormCapsule, extended release
    RouteOral
    Strength500mg
    Market StatusPrescription
    CompanyDuramed Pharms Barr

    3 of 4  
    Drug NameAcetazolamide
    PubMed HealthAcetazolamide
    Drug ClassesAnticonvulsant, Antiglaucoma, Cardiovascular Agent, Musculoskeletal Agent, Renal-Urologic Agent, Urinary Stone Agent
    Drug LabelAcetazolamide, an inhibitor of the enzyme carbonic anhydrase is a white to faintly yellowish white crystalline, odorless powder, weakly acidic, very slightly soluble in water and slightly soluble in alcohol. The chemical name for acetazolamide is N-(...
    Active IngredientAcetazolamide
    Dosage FormTablet; Capsule, extended release
    RouteOral
    Strength250mg; 125mg; 500mg
    Market StatusPrescription
    CompanyMutual Pharm; Lannett; Taro; Zydus Pharms Usa; Heritage Pharms

    4 of 4  
    Drug NameDiamox
    PubMed HealthAcetazolamide (By mouth)
    Drug ClassesAnticonvulsant, Antiglaucoma, Cardiovascular Agent, Musculoskeletal Agent, Renal-Urologic Agent, Urinary Stone Agent
    Drug LabelDIAMOX SEQUELS (Acetazolamide Extended-Release Capsules) are an inhibitor of the enzyme carbonic anhydrase.DIAMOX is a white to faintly yellowish white crystalline, odorless powder, weakly acidic, very slightly soluble in water, and slightly soluble...
    Active IngredientAcetazolamide
    Dosage FormCapsule, extended release
    RouteOral
    Strength500mg
    Market StatusPrescription
    CompanyDuramed Pharms Barr

    4.2 Therapeutic Uses

    Anticonvulsants; Carbonic Anhydrase Inhibitors; Diuretics

    National Library of Medicine's Medical Subject Headings online file (MeSH, 1999)

    MEDICATION (VET): IN LAMINITIS, UDDER EDEMA, ENTEROTOXEMIA, ASCITES, & GLAUCOMA IN VARIOUS SPECIES.

    Rossoff, I.S. Handbook of Veterinary Drugs. New York: Springer Publishing Company, 1974., p. 2

    Carbonic anhydrase inhibitors are indicated primarily as adjuncts to other agents in the treatment of open-angle (chronic simple) glaucoma and secondary glaucoma, and to lower intraocular pressure prior to surgery for some types of glaucoma. /Carbonic anhydrase inhibitors; Included in US product labeling/

    USP Convention. USPDI - Drug Information for the Health Care Professional. 16th ed. Volume I. Rockville, MD: U.S. Pharmaceutical Convention, Inc. 1996 (Plus updates)., p. 747

    Acetazolamide is used to lower intraocular pressure in the treatment of malignant (ciliary block) glaucoma, which may occur after inflammation surgery, trauma, or use of miotics. /NOT included in US product labeling/

    USP Convention. USPDI - Drug Information for the Health Care Professional. 16th ed. Volume I. Rockville, MD: U.S. Pharmaceutical Convention, Inc. 1996 (Plus updates)., p. 747

    For more Therapeutic Uses (Complete) data for ACETAZOLAMIDE (13 total), please visit the HSDB record page.

    4.3 Drug Warning

    VET: CONTRAINDICATED IN ADRENAL FAILURE OR LOW POTASSIUM AND SODIUM SYNDROMES.

    Rossoff, I.S. Handbook of Veterinary Drugs. New York: Springer Publishing Company, 1974., p. 2

    SAFE USE OF THESE AGENTS DURING PREGNANCY HAS NOT BEEN ESTABLISHED. THESE AGENTS ARE CONTRAINDICATED IN PT WITH IDIOPATHIC RENAL HYPERCHLOREMIC ACIDOSIS, RENAL FAILURE, KNOWN DEPLETION OF SODIUM & OF POTASSIUM, ADDISON'S DISEASE, & PT KNOWN TO BE SENSITIVE TO THIS CLASS OF DRUGS. /CARBONIC ANHYDRASE INHIBITORS/

    Osol, A. and J.E. Hoover, et al. (eds.). Remington's Pharmaceutical Sciences. 15th ed. Easton, Pennsylvania: Mack Publishing Co., 1975., p. 866

    DIURETICS, SUCH AS ACETAZOLAMIDE & THIAZIDES, CAN ALKALINIZE URINE & THUS THEORETICALLY WOULD LIMIT USEFULNESS OF METHENAMINE AS WELL AS ITS MANDELATE & HIPPURATE SALTS AS URINARY TRACT ANTI-INFECTIVE AGENTS.

    Evaluations of Drug Interactions. 2nd ed. and supplements. Washington, DC: American Pharmaceutical Assn., 1976, 1978., p. 391

    Maternal Medication usually Compatible with Breast-Feeding: Acetazolamide: Reported Sign or Symptom in Infant or Effect on Lactation: None. /from Table 6/

    Report of the American Academy of Pediatrics Committee on Drugs in Pediatrics 93 (1): 140 (1994)

    For more Drug Warnings (Complete) data for ACETAZOLAMIDE (13 total), please visit the HSDB record page.

    4.4 Drug Indication

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

    FDA Label

    5 Pharmacology and Biochemistry
    5.1 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.

    5.2 MeSH Pharmacological Classification

    Diuretics

    Agents that promote the excretion of urine through their effects on kidney function. (See all compounds classified as Diuretics.)

    Carbonic Anhydrase Inhibitors

    A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES. (See all compounds classified as Carbonic Anhydrase Inhibitors.)

    Anticonvulsants

    Drugs used to prevent SEIZURES or reduce their severity. (See all compounds classified as Anticonvulsants.)

    5.3 FDA Pharmacological Classification
    5.3.1 Active Moiety
    ACETAZOLAMIDE
    5.3.2 FDA UNII
    O3FX965V0I
    5.3.3 Pharmacological Classes
    Carbonic Anhydrase Inhibitors [MoA]; Sulfonamides [CS]; Carbonic Anhydrase Inhibitor [EPC]
    5.4 ATC Code

    S01EC01

    S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (in prep.). List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355

    S - Sensory organs

    S01 - Ophthalmologicals

    S01E - Antiglaucoma preparations and miotics

    S01EC - Carbonic anhydrase inhibitors

    S01EC01 - Acetazolamide

    5.5 Absorption, Distribution and Excretion

    Carbonic anhydrase inhibitors are avidly bound by carbonic anhydrase and, accordingly, tissues rich in this enzyme will have higher concentrations of carbonic anhydrase inhibitors following systemic administration. /Carbonic Anhydrase Inhibitors/

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 694

    Inhibitors of Carbonic Anhydrase. Drug: acetazolamide; Oral Absorption: nearly complete; Plasma Half-Life: 6-9 hours; and Route of Elimination: renal excretion of intact drug. /From table/

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 693

    ACETAZOLAMIDE RELATED TO RESPONSE IN RABBIT; KIDNEY RESPONSE, MEASURED BY MONITORING URINE FLOW & NA ELIMINATION, URINE FLOW & NA ELIMINATION OCCUR IMMEDIATELY AFTER INJECTION CORRELATED WITH LOG DOSE.

    PMID:423126 KUNKA RL, MATTOCKS AM; J PHARM SCI 68 (3): 347-349 (1979)

    IV BOLUS INJECTIONS OF (14)C-LABELED, ACETAZOLAMIDE WERE MADE IN RABBITS. PLASMA, URINE, & WASHED RED BLOOD CELL CONCN WERE MEASURED, THE LATTER INDICATING BOUND DRUG.

    PMID:423125 KUNKA RL, MATTOCKS AM; J PHARM SCI 68 (3): 342-346 (1979)

    For more Absorption, Distribution and Excretion (Complete) data for ACETAZOLAMIDE (6 total), please visit the HSDB record page.

    5.6 Metabolism/Metabolites

    ACETAZOLAMIDE DOSE NOT UNDERGO METABOLIC ALTERATION.

    Goodman, L.S., and A. Gilman. (eds.) The Pharmacological Basis of Therapeutics. 5th ed. New York: Macmillan Publishing Co., Inc., 1975., p. 828

    5.7 Biological Half-Life

    3 to 9 hours

    Plasma half-life: 6-9 hours /From table/

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 693

    5.8 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.

    Carbonic anhydrase inhibitors potently inhibit (IC50 for acetazolamide is 10 nM) both the membrane bound and cytoplasmic forms of carbonic anhydrase, resulting in nearly complete abolition of NaHCO3 reabsorption in the proximal tubule. /Carbonic Anhydrase Inhibitors/

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 693

    Although the proximal tubule is the major site of action of carbonic anhydrase inhibitors, carbonic anhydrase also is involved in secretion of titratable acid in the collecting duct system (a process which involves a proton pump), and therefore the collecting duct system is a secondary site of action for this class of drugs. /Carbonic Anhydrase Inhibitors/

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 693

    Acetazolamide frequently causes paresthesias and somnolence, suggesting an action of carbonic anhydrase inhibitors in the CNS. The efficacy of acetazolamide in epilepsy is in part due to the production of metabolic acidosis; however, direct actions of acetazolamide in the CNS also contribute to its anticonvulsant action.

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 694

    ... Inhibition of carbonic anhydrase decreases the rate of formation of aqueous humor and consequently reduce intraocular pressure. /Carbonic Anhydrase Inhibitors/

    Hardman, J.G., L.E. Limbird, P.B. Molinoff, R.W. Ruddon, A.G. Goodman (eds.). Goodman and Gilman's The Pharmacological Basis of Therapeutics. 9th ed. New York, NY: McGraw-Hill, 1996., p. 694

    For more Mechanism of Action (Complete) data for ACETAZOLAMIDE (6 total), please visit the HSDB record page.