General Information of Drug (ID: DMXOELT)

Drug Name
Midazolam Drug Info
Synonyms
Dazolam; Dormicum; Midanium; Midazolamum; Midosed; Versed; Midazolam Base; Dormicum (TN); Hypnovel (TN); Midacum (TN); Midazolamum [INN-Latin]; Ro 21-3981; Versed (TN); Midazolam (JAN/INN); Midazolam [INN:BAN:JAN]; 4H-Imidazo[1,5-a][1,4]benzodiazepine, 8-chloro-6-(2-fluoro-phenyl)-1-methyl-, (Z)-2-butenedioate; 8-Chlor-6-(2-fluorphenyl)-1-methyl-4H-imidazo(1,5-a)(1,4)benzodiazepin; 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine; 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5a][1,4]benzodiazepine hydrochloride; 8-Chloro-6-(O-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]-benzodiazepine; 8-Chloro-6-(o-fluorophenyl)-1-methyl-4H-imidazo(1,5-a)(1,4)benzodiazepine
Indication
Disease Entry ICD 11 Status REF
Agitation 6A70.3 Approved [1]
Anxiety Approved [1]
Irritability MB24 Approved [2]
Pain MG30-MG3Z Approved [1]
Traumatic brain injury NA07.Z Approved [1]
Epilepsy 8A60-8A68 Phase 3 [3]
Therapeutic Class
Hypnotics and Sedatives
Cross-matching ID
PubChem CID
4192
ChEBI ID
CHEBI:6931
CAS Number
CAS 59467-70-8
TTD Drug ID
DMXOELT
VARIDT Drug ID
DR00684
INTEDE Drug ID
DR1086

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Translocator protein (TSPO) DTT TSPO 7.51 8.89 7.64 8.008
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Cytochrome P450 4B1 (CYP4B1) DME CYP4B1 2.202 6.302 4.178 2.036
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

References

1 Midazolam FDA Label
2 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: 3342).
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5 A novel screening strategy to identify ABCB1 substrates and inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):11-26.
6 Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. Drug Metab Dispos. 2010 Jun;38(6):981-7.
7 In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug Metab Dispos. 2003 Jul;31(7):938-44.
8 Further characterization of the expression in liver and catalytic activity of CYP2B6. J Pharmacol Exp Ther. 1998 Sep;286(3):1253-9.
9 Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.