Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00010)
Name
Acetazolamide
Synonyms    Click to Show/Hide the Synonyms of This API
acetazolamide; 59-66-5; Diamox; N-(5-Sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide; Acetazolamid; Acetamox; Diacarb; Glaupax; Defiltran; Nephramide; Cidamex; Diluran; Edemox; Dehydratin; Diuramid; Diutazol; Duiramid; Eumicton; Natrionex; Nephramid; Phonurit; Diakarb; Donmox; Fonurit; Glupax; Vetamox; SK-acetazolamide; 5-Acetamido-1,3,4-thiadiazole-2-sulfonamide; Diuriwas; Acetazoleamide; Acetozalamide; Diureticum-holzinger; Acetamidothiadiazolesulfonamide; Acetazolamida; Acetazolamidum; 4-Diamox; Acetamide, N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]-; Carbonic Anhydrase Inhibitor No. 6063; 2-Acetylamino-1,3,4-thiadiazole-5-sulfonamide; N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]acetamide; C4H6N4O3S2; 2-Acetamido-5-sulfonamido-1,3,4-thiadiazole; Carbonic anhydrase inhibitor 6063; UNII-O3FX965V0I; MFCD00003105; NSC 145177; 1,3,4-Thiadiazole-2-sulfonamide, 5-acetamido-; 5-Acetamide-1,3,4-thiadiazole-2-sulfonamide; CHEMBL20; Diamox (TN); N-(5-(Aminosulfonyl)-1,3,4-thiadiazol-2-yl)acetamide; MLS000028435; O3FX965V0I; CHEBI:27690; Acetamide, N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-; NSC-145177; CAS-59-66-5; N-[5-(Aminosulfonyl)-1,3,4-thiadiozol-2-yl]-Acetamide; NCGC00015074-10; Acetazolamine; Acetamide, N-(5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl)-; Atenezol; Glaumox; SMR000058394; Diamox Sequels; DSSTox_CID_2544; 5-acetylamino-1,3,4-thiadiazole-2-sulfonamide; DSSTox_RID_76621; DSSTox_GSID_22544; Acetazolamidum [INN-Latin]; Acetazolamida [INN-Spanish]; N-(5-[Aminosulfonyl]-1,3,4-thiadiazol-2-yl)acetamide; N-[5-(aminosulfonyl)-1,3,5-thiadiazol-2-yl]acetamide; CCRIS 5811; Acetazolamide (AAZ); HSDB 3002; SR-01000000065; EINECS 200-440-5; AI3-52458; Prestwick_4; Acetazolamide, 5; Acetazolamide [USP:INN:BAN:JAN]; Acerazolamide, AAZ; Acetazolamide, AAZ; Acetazolamide, AZA; Acetazolamide, AZM; ACMC-20gwkd; PubChem12858; Spectrum_000018; Opera_ID_288; Prestwick0_000003; Prestwick1_000003; Prestwick2_000003; Prestwick3_000003; Spectrum2_000082; Spectrum3_000284; Spectrum4_000139; Spectrum5_000738; Lopac-A-6011; A 6011; Lopac0_000039; SCHEMBL23219; BSPBio_000005; BSPBio_001788; KBioGR_000558; KBioSS_000358; MLS001148438; BIDD:GT0643; DivK1c_000017; SPECTRUM1500102; N-(5-Sulfamoyl-[1,3,4]thiadiazol-2-yl)-acetamide; SPBio_000004; SPBio_001926; BPBio1_000007; GTPL6792; (non-d)Acetazolamide-13C2-d3; Acetazolamide, >=99%, powder; DTXSID7022544; SCHEMBL11049053; BDBM10880; BZKPWHYZMXOIDC-UHFFFAOYSA-; HMS500A19; KBio1_000017; KBio2_000358; KBio2_002926; KBio2_005494; KBio3_001288; Acetazolamide (JP17/USP/INN); Acetazolamide, analytical standard; NINDS_000017; HMS1568A07; HMS1920A05; HMS2091G05; HMS2095A07; HMS2232G23; HMS3259I13; HMS3260G19; HMS3370P01; HMS3712A07; HMS3744A21; Pharmakon1600-01500102; WLN: T5NN DSJ CSZW EMV1; ALBB-023617; BCP29616; EBD55026; HY-B0782; ZINC3813042; Tox21_110078; Tox21_201559; Tox21_302773; Tox21_500039; CCG-38900; NSC145177; NSC755854; SBB056640; AKOS000715163; Tox21_110078_1; CS-3568; DB00819; LP00039; MCULE-4029778803; NC00491; NSC-755854; SDCCGSBI-0050028.P005; Acetazolamide Related Compound (5-acetamido-1,3,4-thiadiazole-2-sulfonic acid); IDI1_000017; NCGC00015074-01; NCGC00015074-02; NCGC00015074-03; NCGC00015074-04; NCGC00015074-05; NCGC00015074-06; NCGC00015074-07; NCGC00015074-08; NCGC00015074-09; NCGC00015074-11; NCGC00015074-12; NCGC00015074-14; NCGC00015074-15; NCGC00015074-22; NCGC00023455-03; NCGC00023455-04; NCGC00023455-05; NCGC00023455-06; NCGC00023455-07; NCGC00256374-01; NCGC00259108-01; NCGC00260724-01; AC-12779; AK324920; AS-13169; SBI-0050028.P004; 2-Acetamido-5-sulfonamido-1,4-thiadiazole; 5-Acetamide-1,4-thiadiazole-2-sulfonamide; DB-053437; 5-Acetamido-1,3,4-thiadiazol-2-sulfonamide; AB00051906; EU-0100039; ST45022057; 1,4-Thiadiazole-2-sulfonamide, 5-acetamido-; C06805; D00218; J10059; 20506-EP2269989A1; 20506-EP2275420A1; 20506-EP2280008A2; 20506-EP2295406A1; 20506-EP2298772A1; 20506-EP2308562A2; 20506-EP2308839A1; 20506-EP2314585A1; AB00051906_15; 003A105; A832415; N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)ethanamide; Q413690; L 579486; Q-200579; Q-200580; SR-01000000065-2; SR-01000000065-4; SR-01000000065-6; BRD-K43457670-001-22-9; BRD-K43457670-001-26-0; Z277559108; Acetazolamide, European Pharmacopoeia (EP) Reference Standard; Acetazolamide, United States Pharmacopeia (USP) Reference Standard; N - (5 - Sulfamoyl - 1,3, 4 - thiadiazol - 2 - yl) acetamide; Acetazolamide, Pharmaceutical Secondary Standard; Certified Reference Material; 124442-28-0
Clinical Status
Approved
Disease Indication Glaucoma ICD-11: 9C61 [1]
PubChem CID
1986
Formula
C4H6N4O3S2
Canonical SMILES
CC(=O)NC1=NN=C(S1)S(=O)(=O)N
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)
InChIKey
BZKPWHYZMXOIDC-UHFFFAOYSA-N
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=1986"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 222.3 Topological Polar Surface Area 152
XlogP -0.3 Complexity 297
Heavy Atom Count 13 Rotatable Bond Count 2
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 7
Full List of Drug Formulations (DFMs) Containing This API
          Acetazolamide 500 mg capsule Click to Show/Hide the Full List of Formulation(s):          8 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Oleic acid; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Ammonia; Ferric oxide yellow; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Medium-chain triglycerides; Silicon dioxide; Cellulose, microcrystalline; Ethylcelluloses; Gelatin; Hypromellose 2910 (5 mpa.s); Shellac
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Nostrum Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Oleic acid DIG Info Liver lipid-binding protein (Ki = 180 nM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [3]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [4]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
Medium-chain triglyceride DIG Info Colon cancer Caco-2 cells (Inhibition ratio > 36 %) [6]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
D&c red no. 28; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Propylene glycol 1,2-distearate; Ferrosoferric oxide; Talc; Titanium dioxide; Gelatin hydrolysate (porcine skin, mw 3000); Cellulose, microcrystalline
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [3]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [4]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 28 DIG Info Organic anion transporter 1 (Ki = 0.064 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
Gelatin DIG Info Mephenytoin 4-hydroxylase (EC50 = 20.5 uM) [8]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
D&c red no. 28; Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Ferrosoferric oxide; Propylene glycol; Talc; Titanium dioxide; Aluminum oxide; Cellulose, microcrystalline; Gelatin; Shellac
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Barr Laboratories; Teva Women's Health
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 4.7 uM) [3]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [4]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [3]
D&C red no. 28 DIG Info Organic anion transporter 1 (Ki = 0.064 uM) [3]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Sodium lauryl sulfate; Ferric oxide yellow; Ferrosoferric oxide; Potassium hydroxide; Propylene glycol; Talc; Titanium dioxide; Cellulose, microcrystalline; Fd&c green no. 3; Gelatin; Hydroxypropyl cellulose; Shellac
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Heritage Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [5]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Sodium lauryl sulfate; Fd&c yellow no. 6; Talc; Titanium dioxide; Ammonio methacrylate copolymer type a; Ammonio methacrylate copolymer type b; Cellulose, microcrystalline; Gelatin
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Zydus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Sodium lauryl sulfate; Fd&c yellow no. 6; Talc; Titanium dioxide; Cellulose, microcrystalline; Gelatin; Methacrylic acid - methyl methacrylate copolymer (1:1)
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company American Health Packaging
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
             Drug Formulation 7 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Sodium lauryl sulfate; Fd&c yellow no. 6; Talc; Titanium dioxide; Cellulose, microcrystalline; Gelatin; Methacrylic acid - methyl methacrylate copolymer (1:1); Methacrylic acid - methyl methacrylate copolymer (1:2)
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Kaiser Foundation Hospitals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
             Drug Formulation 8 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Sodium lauryl sulfate; Ferrosoferric oxide; Potassium hydroxide; Talc; Titanium dioxide; Cellulose, microcrystalline; Gelatin; Hydroxypropyl cellulose; Shellac; Starch, pregelatinized corn
                   Dosage Form 12 HR Extended Release Oral Capsule
                   Company Ingenus Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
          Acetazolamide 125 mg tablet Click to Show/Hide the Full List of Formulation(s):          4 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Sodium lauryl sulfate; Magnesium stearate; Povidone; Cellulose, microcrystalline; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company AvKARE; Heritage Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [8]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Strides Shasun
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company PD-Rx Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin; Sodium starch glycolate type b potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
          Acetazolamide 250 mg tablet Click to Show/Hide the Full List of Formulation(s):          6 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Sodium lauryl sulfate; Magnesium stearate; Povidone; Cellulose, microcrystalline; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company AvKARE; Heritage Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [4]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [8]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 2 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Strides Shasun
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 3 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company NCS HealthCare of KY, Inc dba Vangard Labs; RemedyRepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 4 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin; Sodium starch glycolate type b potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Golden State Medical Supply
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 5 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Magnesium stearate; Glycerin; Talc; Water; Gelatin, unspecified; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company PD-Rx Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [7]
             Drug Formulation 6 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Calcium stearate; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company American Health Packaging; AvKARE; Lannett Company; Marlex Pharmaceuticals; Physicians Total Care; RedPharm; RemedyRepack
References
1 FDA label for approved acetazolamide from the official website of the U.S. Food and Drug Administration.
2 Characterization of the drug binding specificity of rat liver fatty acid binding protein. J Med Chem. 2008 Jul 10; 51(13):3755-64.
3 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
4 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
5 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
6 Interactions between human multidrug resistance related protein (MRP2; ABCC2) and excipients commonly used in self-emulsifying drug delivery systems (SEDDS). Int J Pharm. 2013 Apr 15;447(1-2):192-8.
7 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
8 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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