General Information of API (ID: D00406)
Name
Methadone
Synonyms    Click to Show/Hide the Synonyms of This API
methadone; dl-Methadone; Dolophine; Phenadone; Amidone; Methadon; Adanon; Diaminon; Dolophin; Ketalgin; Physeptone; 76-99-3; Algovetin; Heptadone; Heptanon; Sedo-Rapide; Racemic methadone; 6-(dimethylamino)-4,4-diphenylheptan-3-one; Amidon; (+-)-Methadone; (+/-)-Methadone; Methadonum; Heptanon (pharmaceutical); Methadose; 3-Heptanone, 6-(dimethylamino)-4,4-diphenyl-; Methadone HCL; 6-Dimethylamino-4,4-diphenyl-3-heptanone; Westadone; (RS)-methadones; Althose; l-Methadone; rac-Methadone; CHEBI:6807; 6-(Dimethylamino)-4,4-diphenyl-3-heptanone; Metadone; (+/-)-Methadone hydrochloride; Metadone [DCIT]; Metadona [Spanish]; Methadonum [Latin]; Methadona [Spanish]; Metadona; Metasedin; Methadona; Dolophine HCL; Methadone [INN:BAN]; Metadona [INN-Spanish]; Methadonum [INN-Latin]; UNII-UC6VBE7V1Z; Eptadone; Symoron; Methadone (BAN); HSDB 3119; 3-14-00-00279 (Beilstein Handbook Reference); EINECS 200-996-9; A 4624; Fenadone (*Hydrochloride*); Heptanon (*Hydrochloride*); BRN 3213669; Dolophine (*Hydrochloride*); Heptadone (*Hydrochloride*); Levomethadon; Phenadone (*Hydrochloride*); UC6VBE7V1Z; AN-148 (*Hydrochloride*); DEA No. 9250; (plusmn)-methadone; Hoescht 10820 (*Hydrochloride*); Mecodin (Salt/Mix); Methadone-HCL,(-); Polamidon (Salt/Mix); Polamidone (Salt/Mix); (.+/-.)-Methadone; CHEMBL651; SCHEMBL34140; DivK1c_000963; GTPL5458; IDS-NM-002; Adanon hydrochloride (Salt/Mix); DTXSID7023273; BDBM82507; KBio1_000963; CHEBI:167309; NINDS_000963; NSC_22266; STL455106; AKOS015962259; rac-Methadone 0.1 mg/ml in Methanol; rac-Methadone 1.0 mg/ml in Methanol; DB00333; IDI1_000963; NCGC00248116-01; NCGC00248116-02; AC-16055; 2-Dimethylamino-4,4-diphenyl-5-heptanone; CAS_5967-73-7; DB-053574; 6-(dimethylamino)-4,4-diphenyl-heptan-3-one; 6481-EP1441224A2; 6481-EP2275420A1; 6481-EP2277875A2; 6481-EP2280008A2; 6481-EP2298764A1; 6481-EP2298765A1; 6481-EP2298776A1; 6481-EP2305654A1; 6481-EP2308509A1; 6481-EP2308872A1; 6481-EP2316829A1; C07163; D08195; L000874; Q179996; 3-Heptanone, 6-(dimethylamino)-4,4-diphenyl-, (.+/-.)-
Clinical Status
Approved
Disease Indication Anaesthesia ICD-11: 8E22 [1]
PubChem CID
4095
Formula
C21H27NO
Canonical SMILES
CCC(=O)C(CC(C)N(C)C)(C1=CC=CC=C1)C2=CC=CC=C2
InChI
1S/C21H27NO/c1-5-20(23)21(16-17(2)22(3)4,18-12-8-6-9-13-18)19-14-10-7-11-15-19/h6-15,17H,5,16H2,1-4H3
InChIKey
USSIQXCVUWKGNF-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=4095"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 309.4 Topological Polar Surface Area 20.3
XlogP 3.9 Complexity 346
Heavy Atom Count 23 Rotatable Bond Count 7
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 2
Full List of Drug Formulations (DFMs) Containing This API
          Methadone 40 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; Fd&c yellow no. 5; Fd&c yellow no. 6; Magnesium stearate; Potassium phosphate, monobasic; Silicon dioxide; Aluminum oxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Tablet for Oral Suspension
                   Company Mallinckrodt
                   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]
Potassium phosphate monobasic DIG Info Intestinal alkaline phosphatase (IC50 = 2410 nM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
Hydrazine yellow DIG Info GABA(A) receptor alpha-1 (IC50 = 13 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
Stearic acid; Fd&c yellow no. 6; Magnesium stearate; Potassium phosphate, monobasic; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Tablet for Oral Suspension
                   Company West-Ward Pharmaceticals
                   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]
Potassium phosphate monobasic DIG Info Intestinal alkaline phosphatase (IC50 = 2410 nM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [4]
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
Stearic acid; Magnesium stearate; Dibasic calcium phosphate dihydrate; Silicon dioxide; Microcrystalline cellulose; Starch, corn
                   Dosage Form Tablet for Oral Suspension
                   Company American Health Packaging; Mallinckrodt
                   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]
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
Magnesium stearate; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Tablet for Oral Suspension
                   Company VistaPharm
                   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) [5]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [5]
          Methadone 5 mg tablet 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
Stearic acid; Magnesium stearate; Calcium phosphate, dibasic, dihydrate; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Mallinckrodt
                   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]
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; Magnesium stearate; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company American Health Packaging; Aurolife Pharma
                   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) [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; Magnesium stearate; Silicon dioxide; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company H. J. Harkins Company; Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care; Stat Rx USA
                   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) [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; Magnesium stearate; Silicon dioxide; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack; SpecGx
                   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) [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
Magnesium stearate; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company CorePharma; Lake Eire Medical & Surgical Supply DBA Quality Care Products; PD-Rx Pharmaceuticals; Stat Rx USA; West-Ward Pharmaceticals
                   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) [5]
          Methadone 10 mg tablet Click to Show/Hide the Full List of Formulation(s):          7 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; Magnesium stearate; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Aurolife Pharma
                   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) [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; Magnesium stearate; Silicon dioxide; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company H. J. Harkins Company; Lake Eire Medical & Surgical Supply DBA Quality Care Products; Physicians Total Care; Stat Rx USA
                   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) [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; Magnesium stearate; Silicon dioxide; Microcrystalline cellulose
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack; SpecGx
                   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) [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
Anhydrous lactose; Magnesium stearate; Sucrose; Talc; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company VistaPharm
                   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) [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
Anhydrous lactose; Magnesium stearate; Sucrose; Talc; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company VistaPharm
                   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) [5]
             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
Magnesium stearate; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company American Health Packaging; Ascend Laboratories; CorePharma; DirectRX; Lake Eire Medical & Surgical Supply DBA Quality Care Products; McKesson; PD-Rx Pharmaceuticals; West-Ward Pharmaceticals
                   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) [5]
             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
Magnesium stearate; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company Major 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) [5]
References
1 FDA label for approved methadone 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 Synthesis, crystal structure and biological evaluation of some novel 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines. Eur J Med Chem. 2014 May 6; 78:167-77.
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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