Details of the Drug
General Information of Drug (ID: DMC3JST)
Drug Name |
Clorazepate
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Synonyms |
Chlorazepate; Tranxene; Cchlorazepic acid; Chlorazepic acid; Clorazepate dipotassium; Clorazepic acid; Clorazepic acid [BAN]; Gen-xene; Novo-Clopate; Tranxene (Cherazepate dipotasium); Tranxene (TN); Novo-Clopate (TN); (Chloromethyl)(dimethyl)(tridecyloxy)silane; 7-Chloro-2,3-dihydro-2,2-dihydroxy-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid; 7-chloro-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepine-3-carboxylic acid; 7-chloro-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine-3-carboxylic acid
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Indication |
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Therapeutic Class |
Hypnotics and Sedatives
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Drug Type |
Small molecular drug
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Structure | ||||||||||||||||||||
3D MOL | 2D MOL | |||||||||||||||||||
#Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 314.72 | ||||||||||||||||||
Topological Polar Surface Area (xlogp) | 3.3 | |||||||||||||||||||
Rotatable Bond Count (rotbonds) | 2 | |||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 2 | |||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 4 | |||||||||||||||||||
ADMET Property |
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Chemical Identifiers |
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Cross-matching ID | ||||||||||||||||||||
Molecular Interaction Atlas of This Drug
Drug Therapeutic Target (DTT) |
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Drug-Metabolizing Enzyme (DME) |
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Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Disease Different from Clorazepate (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) 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: 7548). | ||||
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2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 071852. | ||||
3 | BDDCS applied to over 900 drugs | ||||
4 | Critical Evaluation of Human Oral Bioavailability for Pharmaceutical Drugs by Using Various Cheminformatics Approaches | ||||
5 | Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds | ||||
6 | FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41. | ||||
7 | 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 | ||||
8 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
9 | In vitro drug allergy detection system incorporating human liver microsomes in chlorazepate-induced skin rash: drug-specific proliferation associated with interleukin-5 secretion. Br J Dermatol. 2001 Feb;144(2):316-20. | ||||
10 | Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65. | ||||
11 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
12 | Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75. | ||||
13 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
14 | Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772. | ||||
15 | Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98. | ||||
16 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
17 | The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76. | ||||
18 | Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. | ||||
19 | Translocator protein (18 kDa) mediates the pro-growth effects of diazepam on Ehrlich tumor cells in vivo. Eur J Pharmacol. 2010 Jan 25;626(2-3):131-8. | ||||
20 | Comparison of five benzodiazepine-receptor agonists on buprenorphine-induced mu-opioid receptor regulation. J Pharmacol Sci. 2009 May;110(1):36-46. | ||||
21 | Effects of the combination of metyrapone and oxazepam on cocaine and food self-administration in rats. Pharmacol Biochem Behav. 2008 Nov;91(1):181-9. | ||||
22 | 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. (Target id: 2879). | ||||
23 | Effects of benzodiazepines and non-benzodiazepine compounds on the GABA-induced response in frog isolated sensory neurones. Br J Pharmacol. 1989 Nov;98(3):735-40. | ||||
24 | New hypnotics: perspectives from sleep physiology. Vertex. 2007 Jul-Aug;18(74):294-9. | ||||
25 | Greenblatt DJ, Allen MD, MacLaughlin DS, Harmatz JS, Shader RI "Diazepam absorption: effect of antacids and food." Clin Pharmacol Ther 24 (1978): 600-9. [PMID: 699484] | ||||
26 | US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.". | ||||
27 | Product Information. Synercid (dalfopristin-quinupristin) Rhone-Poulenc Rorer, Collegeville, PA. | ||||
28 | Mattila MJ, Idanpaanheikkila JJ, Tornwall M, Vanakoski J "Oral single doses of erythromycin and roxithromycin may increase the effects of midazolam on human performance." Pharmacol Toxicol 73 (1993): 180-5. [PMID: 8265524] | ||||
29 | Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ. | ||||
30 | Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002] | ||||
31 | McClune S, McKay AC, Wright PM, et al "Synergistic interaction between midazolam and propofol." Br J Anaesth 69 (1992): 240-5. [PMID: 1389840] | ||||
32 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
33 | Lilja JJ, Kivisto KT, Neuvonen PJ "Grapefruit juice-simvastatin interaction: Effect on serum concentrations of simvastatin, simvastatin acid, and HMG-CoA reductase inhibitors." Clin Pharmacol Ther 64 (1998): 477-83. [PMID: 9834039] | ||||
34 | Divoll M, Greenblatt DJ, Lacasse Y, Shader RI "Benzodiazepine overdosage: plasma concentrations and clinical outcome." Psychopharmacology (Berl) 73 (1981): 381-3. [PMID: 6789361] | ||||
35 | Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ. | ||||
36 | Dresser GK, Spence JD, Bailey DG "Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition." Clin Pharmacokinet 38 (2000): 41-57. [PMID: 10668858] | ||||
37 | Barbhaiya RH, Shukla UA, Kroboth PD, Greene DS "Coadministration of nefazodone and benzodiazepines: 2. a pharmacokinetic interaction study with triazolam." J Clin Psychopharmacol 15 (1995): 320-6. [PMID: 8830062] | ||||
38 | EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.". | ||||
39 | Murphy A, Wilbur K "Phenytoin-diazepam interaction." Ann Pharmacother 37 (2003): 659-63. [PMID: 12708941] | ||||
40 | Product Information. Victrelis (boceprevir). Schering-Plough Corporation, Kenilworth, NJ. | ||||
41 | Product Information. Incivek (telaprevir). Vertex Pharmaceuticals, Cambridge, MA. | ||||
42 | Ochs HR, Greenblatt DJ, Roberts GM, Dengler HJ "Diazepam interaction with antituberculosis drugs." Clin Pharmacol Ther 29 (1981): 671-8. [PMID: 7214796] | ||||
43 | Product Information. Priftin (rifapentine). Hoechst Marion-Roussel Inc, Kansas City, MO. | ||||
44 | Product Information. Agenerase (amprenavir). Glaxo Wellcome, Research Triangle Pk, NC. | ||||
45 | Bailey DG, Dresser GK "Natural products and adverse drug interactions." Can Med Assoc J 170 (2004): 1531-2. [PMID: 15136542] | ||||
46 | Cerner Multum, Inc. "Australian Product Information.". | ||||
47 | Product Information. Intelence (etravirine). Ortho Biotech Inc, Bridgewater, NJ. | ||||
48 | Product Information. Prezista (darunavir). Ortho Biotech Inc, Bridgewater, NJ. | ||||
49 | Gunston GD, Mehta U "Potentially serious drug interactions with grapefruit juice." S Afr Med J 90 (2000): 41. [PMID: 10721388] | ||||
50 | Abernethy DR, Greenblatt DJ, Ameer B, Shader RI "Probenecid impairment of acetaminophen and lorazepam clearance: direct inhibition of ether glucuronide formation." J Pharmacol Exp Ther 234 (1985): 345-9. [PMID: 4020675] | ||||
51 | Gilman AG, Rall TW, Nies AS, Taylor P, eds. "Goodman and Gilman's the Pharmacological Basis of Therapeutics. 8th ed." New York, NY: Pergamon Press Inc. (1990):. | ||||
52 | Product Information. Retevmo (selpercatinib). Lilly, Eli and Company, Indianapolis, IN. | ||||
53 | Bailey DG, Malcolm J, Arnold O, Spence JD "Grapefruit juice-drug interactions." Br J Clin Pharmacol 46 (1998): 101-10. [PMID: 9723817] | ||||
54 | Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA. | ||||
55 | Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN. | ||||
56 | Product Information. Exjade (deferasirox). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
57 | Bailey DG, Arnold JMO, Spence JD "Grapefruit juice and drugs - how significant is the interaction." Clin Pharmacokinet 26 (1994): 91-8. [PMID: 8162660] | ||||
58 | Doherty MM, Charman WN "The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism?" Clin Pharmacokinet 41 (2002): 235-53. [PMID: 11978143] | ||||
59 | Hukkinen SK, Varhe A, Olkkola KT, Neuvonen PJ "Plasma concentrations of triazolam are increased by concomitant ingestion of grapefruit juice." Clin Pharmacol Ther 58 (1995): 127-31. [PMID: 7648762] | ||||
60 | Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA. | ||||
61 | EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.". | ||||
62 | Hansen BS, Dam M, Brandt J, et al "Influence of dextropropoxyphene on steady state serum levels and protein binding of three anti-epileptic drugs in man." Acta Neurol Scand 61 (1980): 357-67. [PMID: 6998251] | ||||
63 | Schuman-Olivier Z, Hoeppner BB, Weiss RD, Borodovsky J, Shaffer HJ, Albanese MJ "Benzodiazepine use during buprenorphine treatment for opioid dependence: clinical and safety outcomes." Drug Alcohol Depend 132 (2013): 580-6. [PMID: 23688843] | ||||
64 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
65 | Benoist G, van Oort I, et al "Drug-drug interaction potential in men treated with enzalutamide: Mind the gap." Br J Clin Pharmacol 0 (2017): epub. [PMID: 28881501] | ||||
66 | Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL. | ||||
67 | Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA. | ||||
68 | Kerin NZ, Aragon E, Faitel K, Frumin H, Rubenfire M "Long-term efficacy and toxicity of high- and low-dose amiodarone regimens." J Clin Pharmacol 29 (1989): 418-23. [PMID: 2661600] | ||||