Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00397)
Name
Meperidine
Synonyms    Click to Show/Hide the Synonyms of This API
meperidine; Pethidine; Demerol; Isonipecaine; Pethidin; Meperidol; Pethanol; Pethidineter; Phetidine; Ethyl 1-methyl-4-phenylpiperidine-4-carboxylate; Pipersal; Nemerol; 57-42-1; Petydyna; Petidina; Pethidinum; 4-Piperidinecarboxylic acid, 1-methyl-4-phenyl-, ethyl ester; Ethyl 1-methyl-4-phenylisonipecotate; Methyl phenylpiperidine carbonic acid ethyl ester; N-Methyl-4-phenyl-4-carbethoxypiperidine; Isonipecotic acid, 1-methyl-4-phenyl-, ethyl ester; 1-Methyl-4-phenylisonipecotic acid, ethyl ester; 1-Methyl-4-phenylpiperidine-4-carboxylic acid ethyl ester; HSDB 3116; UNII-9E338QE28F; 1-Methyl-4-phenyl-4-piperidinecarboxylic acid ethyl ester; CHEMBL607; Mepergan; 1-Methyl-4-phenyl-piperidin-4-carbon-saeure-aethylester; CHEBI:6754; IDS-NP-001; 9E338QE28F; meperidina; Mepridine; Petydyna [Polish]; Demarol; Piperosal; Pethidinum [INN-Latin]; Petidina [INN-Spanish]; 1-Methyl-4-phenyl-piperidine-4-carboxylic acid ethyl ester; Pethidine (INN); Pethidine DBL (TN); Pethidine [INN:BAN]; EINECS 200-329-1; Renaudin; DEA No. 9230; 1-Methyl-4-phenyl-piperidin-4-carbon-saeure-aethylester [German]; Lidol (Salt/Mix); Lydol (Salt/Mix); Dolsin (Salt/Mix); Dolaren (Salt/Mix); Dolosal (Salt/Mix); Dispadol (Salt/Mix); Dolantin (Salt/Mix); Petantin (Salt/Mix); Operidine (Salt/Mix); Piridosal (Salt/Mix); 4-Carbethoxy-1-methyl-4-phenylpiperidine; Centralgin (Salt/Mix); Dolcontral (Salt/Mix); 1-methyl-4-phenylisonipecotic acid ethyl ester; Ethyl 1-methyl-4-phenyl-4-piperidinecarboxylate; SCHEMBL25431; DivK1c_000983; GTPL7221; ZINC1681; DTXSID9023253; KBio1_000983; NINDS_000983; YIsonipecotic acid, 1-methyl-4-phenyl-, ethyl ester (8CI); BDBM50026752; DB00454; IDI1_000983; DB-053051; C07128; D08343; Pethidine (Meperidine) 0.1 mg/ml in Methanol; Pethidine (Meperidine) 1.0 mg/ml in Methanol; Q55434; 4-Ethoxycarbonyl-1-methyl-4-phenyl-piperidinium; L000908; SR-01000944492; SR-01000944492-1; Meperidine solution, 1 mg/mL in methanol, drug standard; 1-Methyl-4-phenyl-piperidine-4-carboxylic acid ethyl ester(Meperidine); Meperidine solution, 1.0 mg/mL in methanol, ampule of 1 mL, certified reference material
Clinical Status
Approved
Disease Indication Anaesthesia ICD-11: 8E22 [1]
PubChem CID
4058
Formula
C15H21NO2
Canonical SMILES
CCOC(=O)C1(CCN(CC1)C)C2=CC=CC=C2
InChI
1S/C15H21NO2/c1-3-18-14(17)15(9-11-16(2)12-10-15)13-7-5-4-6-8-13/h4-8H,3,9-12H2,1-2H3
InChIKey
XADCESSVHJOZHK-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=4058"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 247.33 Topological Polar Surface Area 29.5
XlogP 2.5 Complexity 276
Heavy Atom Count 18 Rotatable Bond Count 4
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Meperidine 150 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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; D&c red no. 27; Fd&c yellow no. 6; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Mikart
                   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]
D&C red no. 27 DIG Info Solute carrier SLCO2B1 (Ki = 1 uM) [3]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Meperidine 100 mg tablet Click to Show/Hide the Full List of Formulation(s):          9 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; Talc; Povidone; Dibasic calcium phophate; Microcrystalline cellulose; Pregelatinized starch
                   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]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate 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
Stearic acid; Anhydrous dibasic calcium phosphate; Calcium sulfate; Talc; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   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]
Calcium hydrogenphosphate 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
Stearic acid; Anhydrous dibasic calcium phosphate; Calcium sulfate; Talc; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sanofi-Aventis
                   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]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Epic 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]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Mikart
                   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]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Stearic acid; Calcium sulfate; Talc; Calcium phosphate, dibasic, anhydrous; Starch, corn
                   Dosage Form Oral Tablet
                   Company Validus 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]
             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
Stearic acid; Cellulose, microcrystalline; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Qualitest 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]
             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
Lactose monohydrate; Magnesium stearate; Croscarmellose sodium; Povidone k30; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company 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) [4]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
             Drug Formulation 9 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; Croscarmellose sodium; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company Barr Laboratories; Caraco Pharmaceutical Laboratories; Teva 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) [4]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
          Meperidine 50 mg tablet Click to Show/Hide the Full List of Formulation(s):        11 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; Talc; Povidone; Dibasic calcium phophate; Microcrystalline cellulose; Pregelatinized starch
                   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]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [5]
Magnesium stearate 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
Stearic acid; Anhydrous dibasic calcium phosphate; Calcium sulfate; Talc; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care
                   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]
Calcium hydrogenphosphate 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
Stearic acid; Anhydrous dibasic calcium phosphate; Calcium sulfate; Talc; Starch, corn
                   Dosage Form Oral Tablet
                   Company Sanofi-Aventis
                   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]
Calcium hydrogenphosphate DIG Info Albendazole monooxygenase (Protein expression downregulation) [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; Silicon dioxide; Cellulose, microcrystalline; Starch, corn
                   Dosage Form Oral Tablet
                   Company Epic 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]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
             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
Stearic acid; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Mikart
                   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]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [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
Stearic acid; Calcium sulfate; Talc; Calcium phosphate, dibasic, anhydrous; Starch, corn
                   Dosage Form Oral Tablet
                   Company Validus 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]
             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
Stearic acid; Calcium sulfate; Talc; Calcium phosphate, dibasic, anhydrous; Starch, corn
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack
                   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]
             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
Stearic acid; Cellulose, microcrystalline; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Physicians Total Care; Qualitest 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]
             Drug Formulation 9 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; Microcrystalline cellulose; Sodium starch glycolate type a potato; Starch, corn
                   Dosage Form Oral Tablet
                   Company Bryant Ranch Prepack
                   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]
             Drug Formulation 10 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; Croscarmellose sodium; Povidone k30; Microcrystalline cellulose; Starch, corn
                   Dosage Form Oral Tablet
                   Company 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) [4]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
             Drug Formulation 11 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; Croscarmellose sodium; Cellulose, microcrystalline
                   Dosage Form Oral Tablet
                   Company Barr Laboratories; Caraco Pharmaceutical Laboratories; Teva 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) [4]
Carmellose sodium DIG Info Albendazole monooxygenase (Protein expression upregulation) [4]
          Meperidine 75 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 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. 6; Silicon dioxide; Cellulose, microcrystalline; Hypromellose 2910 (5 mpa.s); Sodium starch glycolate type a potato
                   Dosage Form Oral Tablet
                   Company Mikart
                   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]
Sunset yellow FCF DIG Info Solute carrier SLCO2B1 (Ki = 68.4 uM) [3]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved meperidine 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 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
5 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.

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