Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00701)
Name
Triazolam
Synonyms    Click to Show/Hide the Synonyms of This API
triazolam; Halcion; 28911-01-5; Songar; Clorazolam; Novidorm; Triazolamum [INN-Latin]; U-33,030; 8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; DEA No. 2887; U 33030; UNII-1HM943223R; CHEMBL646; U-33030; 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine; CHEBI:9674; 28911-01-5 (free); 4H-(1,2,4)Triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-(2-chlorophenyl)-1-methyl-; 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine, 8-chloro-6-(2-chlorophenyl)-1-methyl-; 8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-(1,2,4)triazolo(4,3-a)(1,4)benzodiazepine; 1HM943223R; NCGC00168258-01; Triazolamum; Novodorm; Trilam; 8-Chloro-6-(o-chlorophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine; 4H-s-Triazolo(4,3-a)(1,4)benzodiazepine, 8-chloro-6-(o-chlorophenyl)-1-methyl-; 8-Chloro-6-[2-chlorophenyl]-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine; Hypnostat; 8-chloro-6-(2-chlorophenyl)-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine; Halcion (TN); Halcion (triazolam); CCRIS 1932; HSDB 6759; EINECS 249-307-3; TGAR01H; BRN 1226643; Triazolam (JAN/USP/INN); Triazolam civ; N05CD05; Triazolam [USAN:USP:INN:BAN:JAN]; DSSTox_CID_26763; DSSTox_RID_81886; DSSTox_GSID_46763; SCHEMBL29228; MLS003899243; GTPL7313; ZINC2212; DTXSID6046763; Triazolam 0.1 mg/ml in Methanol; Triazolam 1.0 mg/ml in Methanol; HY-B0694; Tox21_112617; BDBM50001765; MFCD00079623; DB00897; SMR000058837; CAS-28911-01-5; D00387; U33030; 911T015; L000796; Q412143; SR-01000937604; SR-01000937604-2; Triazolam, European Pharmacopoeia (EP) Reference Standard; 8-chloro-1-methyl-6-(o-chlorophenyl)-4H-s-triazolo-[4,3-a][1,4] benzodiazepine; 8-chloro-1-methyl-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepine; 8-Chloro-6-(2-chlorophenyl)-1-methyl-4H-s-triazolo[4,3-a][1,4]-benzodiazepine; Triazolam solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material; (E)-8-chloro-6-(2-chlorophenyl)-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepine; 12-chloro-9-(2-chlorophenyl)-3-methyl-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
5556
Formula
C17H12Cl2N4
Canonical SMILES
CC1=NN=C2N1C3=C(C=C(C=C3)Cl)C(=NC2)C4=CC=CC=C4Cl
InChI
1S/C17H12Cl2N4/c1-10-21-22-16-9-20-17(12-4-2-3-5-14(12)19)13-8-11(18)6-7-15(13)23(10)16/h2-8H,9H2,1H3
InChIKey
JOFWLTCLBGQGBO-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=5556"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 343.2 Topological Polar Surface Area 43.1
XlogP 2.4 Complexity 472
Heavy Atom Count 23 Rotatable Bond Count 1
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Triazolam 0.25 mg tablet Click to Show/Hide the Full List of Formulation(s):          3 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, unspecified form; Sodium benzoate; Docusate sodium; Fd&c blue no. 2; Magnesium stearate; Silicon dioxide; Powdered cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Aphena Pharma Solutions-Tennessee; Greenstone; PD-Rx Pharmaceuticals; Pharmacia and Upjohn Company; Unit Dose Services
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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; Sodium benzoate; Docusate sodium; Fd&c blue no. 2; Magnesium stearate; Silicon dioxide; Powdered cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Stat Rx USA
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Anhydrous lactose; Docusate sodium; Fd&c blue no. 1; Magnesium stearate; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company A-S Medication Solutions; Aphena Pharma Solutions-Tennessee; Bryant Ranch Prepack; Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care; Preferred Pharamaceuticals; Rebel Distributors; Roxane Laboratories; Unit Dose Services
                   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) [5]
Docusate sodium DIG Info Solute carrier SLCO2B1 (Ki = 2.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Triazolam 0.125 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
Lactose, unspecified form; Sodium benzoate; Docusate sodium; Magnesium stearate; Silicon dioxide; Powdered cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Greenstone
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
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) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Anhydrous lactose; Docusate sodium; Magnesium stearate; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care; Rebel Distributors; Roxane Laboratories
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Docusate sodium DIG Info Solute carrier SLCO2B1 (Ki = 2.3 uM) [2]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved triazolam 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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 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.

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