Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00286)
Name
Flurazepam
Synonyms    Click to Show/Hide the Synonyms of This API
flurazepam; 17617-23-1; Dalmane; Flurazepamum; Noctosom; Flurazepam HCL; Insumin; UNII-IHP475989U; 7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-3H-1,4-benzodiazepin-2-one; 7-Chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one; 7-Chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1H-1,4-benzodiazepin-2(3H)-one; Stauroderm; 17617-23-1(free base); IHP475989U; Dalmane-R; 2H-1,4-Benzodiazepin-2-one, 7-chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1,3-dihydro-; 7-Chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one; DEA No. 2767; NCGC00164573-01; Felmane; DSSTox_CID_3071; DSSTox_RID_76863; DSSTox_GSID_23071; 2H-1,4-Benzodiazepin-2-one, 1,3-dihydro-7-chloro-1-(2-(diethylamino)ethyl)-5-(o-fluorophenyl)-; 2H-1,4-Benzodiazepin-2-one, 7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-; 2H-1,4-Benzodiazepin-2-one, 7-chloro-1-[2-(diethylamino)ethyl]-5-(o-fluorophenyl)-1,3-dihydro-; Flurazepamum [INN-Latin]; Flurazepam [INN:BAN:JAN]; 7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one; Insumin (TN); CAS-17617-23-1; Ro-5-6901/3; HSDB 3085; Ro 5-6901; EINECS 241-591-7; BRN 0767925; Flurazepam (JAN/INN); CHEMBL968; SCHEMBL29793; 5-24-04-00322 (Beilstein Handbook Reference); CHEBI:5128; GTPL7188; DTXSID1023071; ZINC537752; Flurazepam 0.1 mg/ml in Methanol; Flurazepam 1.0 mg/ml in Methanol; Tox21_112201; Ro-56901; AKOS015889971; Tox21_112201_1; DB00690; Ro-5-6901; NCGC00164573-02; Ro 56901/3; DB-044253; D00329; 191044-EP2275420A1; 191044-EP2280008A2; 617F231; A812156; Q418998; 7-chloranyl-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-3H-1,4-benzodiazepin-2-one; Flurazepam solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material; Flurazepam-D4 solution, 100 mug/mL in methanol, certified reference material; (E)-7-chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1H-benzo[e][1,4]diazepin-2(3H)-one; 7-Chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1H-benzo[e][1,4]diazepin-2(3H)-one; 7-Chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one #; 7-Chloro-1-[2-(diethylamino)ethyl]-5-(o-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one
Clinical Status
Approved
Disease Indication Insomnia ICD-11: 7A00 [1]
PubChem CID
3393
Formula
C21H23ClFN3O
Canonical SMILES
CCN(CC)CCN1C(=O)CN=C(C2=C1C=CC(=C2)Cl)C3=CC=CC=C3F
InChI
1S/C21H23ClFN3O/c1-3-25(4-2)11-12-26-19-10-9-15(22)13-17(19)21(24-14-20(26)27)16-7-5-6-8-18(16)23/h5-10,13H,3-4,11-12,14H2,1-2H3
InChIKey
SAADBVWGJQAEFS-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=3393"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 387.9 Topological Polar Surface Area 35.9
XlogP 3 Complexity 540
Heavy Atom Count 27 Rotatable Bond Count 6
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 4
Full List of Drug Formulations (DFMs) Containing This API
          Flurazepam 15 mg capsule 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
Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Cellulose, microcrystalline; Gelatin; Powdered cellulose; Shellac
                   Dosage Form Oral Capsule
                   Company Mylan Pharamceuticals; Physicians Total Care
                   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]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide 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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Silicon dioxide; Gelatin; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Capsule
                   Company Bryant Ranch Prepack
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide 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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Colloidal silicon dioxide; Gelatin; Sodium starch glycolate type a potato; Starch, pregelatinized corn
                   Dosage Form Oral Capsule
                   Company West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Colloidal silicon dioxide; Gelatin; Sodium starch glycolate type a potato; Starch, pregelatinized corn
                   Dosage Form Oral Capsule
                   Company A-S Medication Solutions
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Flurazepam 30 mg capsule Click to Show/Hide the Full List of Formulation(s):          5 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
Sodium lauryl sulfate; D&c yellow no. 10; Fd&c red no. 40; Fd&c blue no. 1; Fd&c blue no. 2; Magnesium stearate; Ferrosoferric oxide; Propylene glycol; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Cellulose, microcrystalline; Gelatin; Powdered cellulose; Shellac
                   Dosage Form Oral Capsule
                   Company Mylan Pharamceuticals; PD-Rx Pharmaceuticals; Physicians Total Care
                   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]
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Quinoline yellow WS DIG Info Estrogen receptor alpha (IC50 = 18 uM) [2]
Allura red AC dye DIG Info Solute carrier SLCO2B1 (Ki = 2.59 uM) [3]
Propylene glycol DIG Info Albendazole monooxygenase (Inhibition ratio < 20 %) [4]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide 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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Colloidal silicon dioxide; Gelatin; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Capsule
                   Company Rebel Distributors
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide 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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Gelatin, unspecified; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Capsule
                   Company Bryant Ranch Prepack; Preferred Pharamaceuticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Silicon dioxide; Colloidal silicon dioxide; Gelatin; Sodium starch glycolate type a potato; Starch, pregelatinized corn
                   Dosage Form Oral Capsule
                   Company H. J. Harkins Company; West-Ward Pharmaceticals
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Lactose monohydrate; Sodium lauryl sulfate; Fd&c blue no. 1; Magnesium stearate; Titanium dioxide; Fd&c red no. 3; Colloidal silicon dioxide; Gelatin; Sodium starch glycolate type a potato; Starch, pregelatinized corn
                   Dosage Form Oral Capsule
                   Company A-S Medication Solutions
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 1 DIG Info Solute carrier SLCO2B1 (Ki = 13 uM) [3]
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [3]
FD&C red no. 3 DIG Info Phosphodiesterase 3A (IC50 = 0.092 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
References
1 FDA label for approved flurazepam 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 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.
4 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.
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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