Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00245)
Name
Estazolam
Synonyms    Click to Show/Hide the Synonyms of This API
estazolam; 29975-16-4; Eurodin; ProSom; Nuctalon; Julodin; Esilgan; D 40TA; 8-Chloro-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; Estazolamum; D-40TA; Abbott-47631; 8-Chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine; UNII-36S3EQV54C; NSC 290818; U 33737; 36S3EQV54C; CHEBI:4858; NSC-290818; NCGC00168250-01; 8-Chloro-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine; Nemurel; Somnatrol; Cannoc; 4H-s-Triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-phenyl-; 4H-(1,2,4)Triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-phenyl-; 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-phenyl-; Abbott 47631; Estazolamum [INN-Latin]; 53180-72-6; Estazolam [USAN:INN:JAN]; Prosom (TN); CCRIS 1955; EINECS 249-982-4; BRN 1220868; Estazolam civ; 8-Chloro-6-phenyl-4H-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine; DEA No. 2756; 8-Chloro-6-phenyl-4H-(1,2,4)triazolo-(4,3-a)(1,4)benzodiazepine; Eurodin; ProSom; 8-Chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine (IUPAC); DSSTox_CID_572; DSSTox_RID_75665; DSSTox_GSID_20572; SCHEMBL28766; MLS003899222; BIDD:GT0481; Estazolam (JP17/USP/INN); CHEMBL285674; GTPL7550; ZINC1370; DTXSID5020572; CDCHDCWJMGXXRH-UHFFFAOYSA-; Estazolam 0.1 mg/ml in Methanol; Estazolam 1.0 mg/ml in Methanol; 8-Chloro-6-phenyl-4H-2,3,5,10b-tetraaza-benzo[e]azulene; BCP13317; Tox21_112609; MFCD00867537; NSC290818; AKOS005064373; AB07556; DB01215; SMR000238168; CAS-29975-16-4; WLN: T B576 BN DNN HN GHJ IR& LG; C06981; D00311; A820132; Q-201071; Q3045264; 8-Chloro-6-phenyl-4H-s-triazolo[4,4]benzodiazepine; 4H-s-Triazolo[4,4]benzodiazepine, 8-chloro-6-phenyl-; Estazolam solution, drug standard, 100 mug/L in methanol; 8-chloro-6-phenyl-4H-s-triazolo [4,3-a][1,4] benzodiazepine; 8-chloro-6-phenyl-4H-s-triazolo-[4,3-a][1,4]benzodiazepine; Estazolam, United States Pharmacopeia (USP) Reference Standard; 4H-[1,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-phenyl-; 8-Chloro-6-phenyl-4H-[1,4]triazolo[4,3-a][1,4]benzodiazepine; 8-chloranyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; Estazolam solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material; 12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,8,11,13-hexaene
Clinical Status
Approved
Disease Indication Insomnia ICD-11: 7A00 [1]
PubChem CID
3261
Formula
C16H11ClN4
Canonical SMILES
C1C2=NN=CN2C3=C(C=C(C=C3)Cl)C(=N1)C4=CC=CC=C4
InChI
1S/C16H11ClN4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10H,9H2
InChIKey
CDCHDCWJMGXXRH-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=3261"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 294.74 Topological Polar Surface Area 43.1
XlogP 1.7 Complexity 407
Heavy Atom Count 21 Rotatable Bond Count 1
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Estazolam 2 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
Stearic acid; Lactose monohydrate; Sodium benzoate; Docusate sodium; Fd&c red no. 40; Magnesium stearate; Aluminum oxide; Cellulose, microcrystalline; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Rebel Distributors
                   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) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Sodium benzoate DIG Info Carbonic anhydrase II (Ki = 30000 nM) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
Docusate sodium DIG Info Solute carrier SLCO2B1 (Ki = 2.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Stearic acid; Lactose monohydrate; Sodium benzoate; Docusate sodium; Fd&c red no. 40; Magnesium stearate; Microcrystalline cellulose; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Actavis Pharma
                   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) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Sodium benzoate DIG Info Carbonic anhydrase II (Ki = 30000 nM) [3]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
Docusate sodium DIG Info Solute carrier SLCO2B1 (Ki = 2.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Stearic acid; Lactose monohydrate; Fd&c red no. 40; Fd&c yellow no. 6; Starch, corn
                   Dosage Form Oral Tablet
                   Company Teva Pharmaceuticals
                   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) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
             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
Stearic acid; Lactose monohydrate; Fd&c red no. 40; Fd&c yellow no. 6; Starch, corn
                   Dosage Form Oral Tablet
                   Company Mayne Pharma
                   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) [2]
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [4]
          Estazolam 1 mg tablet Click to Show/Hide the Full List of Formulation(s):          2 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
Stearic acid; Lactose monohydrate; Sodium benzoate; Docusate sodium; Magnesium stearate; Microcrystalline cellulose; Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Actavis Pharma
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
Sodium benzoate DIG Info Carbonic anhydrase II (Ki = 30000 nM) [3]
Docusate sodium DIG Info Solute carrier SLCO2B1 (Ki = 2.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
             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
Stearic acid; Lactose monohydrate; Starch, corn
                   Dosage Form Oral Tablet
                   Company Mayne Pharma; Teva Pharmaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Stearic acid DIG Info Phosphodiesterase 3A (IC50 = 3.1 uM) [2]
References
1 FDA label for approved estazolam from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
3 Carbonic anhydrase inhibitors. Interaction of isozymes I, II, IV, V, and IX with carboxylates. Bioorg Med Chem Lett. 2005 Feb 1; 15(3):573-8.
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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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