General Information of Drug (ID: DMGE0CW)

Drug Name
Glutethimide
Synonyms
Alfimid; Doriden; Dorimide; Elrodorm; Gimid; Glimid; Glutathimid; Glutethimid; Glutethimidum; Glutetimid; Glutetimida; Glutetimide; Glutetimidu; Gluthetimide; Noxiron; Noxyron; Ondasil; Rigenox; Sarodormin; Glutetimide [DCIT]; Glutetimidu [Polish]; CC 11511; LT00114358; Doriden (TN); Doriden-sed; Glutethimide [INN:BAN]; Glutethimidum [INN-Latin]; Glutetimida [INN-Spanish]; Glutethimide (JAN/INN); Phenyl-aethyl-glutarsaeureimid; Phenyl-aethyl-glutarsaeureimid [German]; Alpha-Ethyl-alpha-phenylglutarimide; Alpha-Phenyl-alpha-ethylglutaric acid imide; Alpha-Phenyl-alpha-ethylglutarimide; 2-Ethyl-2-phenylglutarimide; 2-Phenyl-2-ethylglutaric acid imide; 3-Ethyl-3-phenyl-2,6-diketopiperidine; 3-Ethyl-3-phenyl-2,6-dioxopiperidine; 3-Ethyl-3-phenyl-2,6-piperidinedione; 3-Phenyl-3-ethyl-2,6-diketopiperidine; 3-Phenyl-3-ethyl-2,6-dioxopiperidine; 3-ethyl-3-phenylpiperidine-2,6-dione
Indication
Disease Entry ICD 11 Status REF
Insomnia 7A00-7A0Z Approved [1]
Therapeutic Class
Hypnotics and Sedatives
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 217.26
Logarithm of the Partition Coefficient (xlogp) 1.9
Rotatable Bond Count (rotbonds) 2
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 2
ADMET Property
Half-life
The concentration or amount of drug in body reduced by one-half in 10 - 12 hours [2]
Metabolism
The drug is metabolized via the hepatic []
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 38.33939 micromolar/kg/day [3]
Chemical Identifiers
Formula
C13H15NO2
IUPAC Name
3-ethyl-3-phenylpiperidine-2,6-dione
Canonical SMILES
CCC1(CCC(=O)NC1=O)C2=CC=CC=C2
InChI
InChI=1S/C13H15NO2/c1-2-13(10-6-4-3-5-7-10)9-8-11(15)14-12(13)16/h3-7H,2,8-9H2,1H3,(H,14,15,16)
InChIKey
JMBQKKAJIKAWKF-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
3487
ChEBI ID
CHEBI:5439
CAS Number
77-21-4
DrugBank ID
DB01437
TTD ID
D0Z9NZ
INTEDE ID
DR1769
ACDINA ID
D01130

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Debrisoquine 4-hydroxylase (CYP2D6) TTVG215 CP2D6_HUMAN Inducer [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Myeloperoxidase (MPO)
Main DME
DEA3U9Y PERM_HUMAN Substrate [5]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
Stearic acid E00079 5281 Emulsifying agent; Solubilizing agent; Viscosity-controlling agent; lubricant
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Glutethimide 250mg tablet 250mg Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7192).
2 Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
3 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
4 A study of the effects of large doses of glutethimide that were used for self-poisoning during pregnancy on human fetuses. Toxicol Ind Health. 2008 Feb-Mar;24(1-2):69-78.
5 Proteomic profile of aminoglutethimide-induced apoptosis in HL-60 cells: role of myeloperoxidase and arylamine free radicals. Chem Biol Interact. 2015 Sep 5;239:129-38.