Details of the Drug
General Information of Drug (ID: DMAL4G0)
Drug Name |
Flurazepam
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Synonyms |
Dalmadorm; Dalmane; Felison; Felmane; Flunox; Flurazepamum; Insumin; Noctosom; Paxane; Somnol; Stauroderm; Valdorm; Flurazepam HCL; Flurazepam hydrochloride; Dalmadorm (TN); Dalmane (TN); Dalmane-R; Flurazepamum [INN-Latin]; Insumin (TN); Flurazepam (JP15/INN); Flurazepam [INN:BAN:JAN]; Ro-5-6901/3; 2H-1,4-Benzodiazepin-2-one,7-chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-, dihydrochloride; 7-Chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one; 7-Chloro-1-(2-(diethylamino)ethyl)-5-(2-fluorophenyl)-1H-1,4-benzodiazepin-2(3H)-one; 7-Chloro-1-[2-(diethylamino)ethyl]-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one; 7-chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-3H-1,4-benzodiazepin-2-one
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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) | 387.9 | ||||||||||||||||||
Topological Polar Surface Area (xlogp) | 3 | |||||||||||||||||||
Rotatable Bond Count (rotbonds) | 6 | |||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 0 | |||||||||||||||||||
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 Flurazepam (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: 7188). | ||||
---|---|---|---|---|---|
2 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 070344. | ||||
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 | 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 | ||||
7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
8 | Is 1-aminobenzotriazole an appropriate in vitro tool as a nonspecific cytochrome P450 inactivator? Drug Metab Dispos. 2009 Jan;37(1):10-3. | ||||
9 | 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. | ||||
10 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
11 | 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. | ||||
12 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
13 | 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. | ||||
14 | 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. | ||||
15 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
16 | 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. | ||||
17 | 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. | ||||
18 | Roles of cytochromes P450 1A2, 2A6, and 2C8 in 5-fluorouracil formation from tegafur, an anticancer prodrug, in human liver microsomes. Drug Metab Dispos. 2000 Dec;28(12):1457-63. | ||||
19 | Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. | ||||
20 | Genotoxicity of tamoxifen, tamoxifen epoxide and toremifene in human lymphoblastoid cells containing human cytochrome P450s. Carcinogenesis. 1994 Jan;15(1):5-9. | ||||
21 | Psychotropic drug interactions with valproate. Clin Neuropharmacol. 2005 Mar-Apr;28(2):96-101. | ||||
22 | The role of human cytochrome P450 enzymes in the formation of 2-hydroxymetronidazole: CYP2A6 is the high affinity (low Km) catalyst. Drug Metab Dispos. 2013 Sep;41(9):1686-94. | ||||
23 | Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95. | ||||
24 | CYP2A6- and CYP2A13-catalyzed metabolism of the nicotine delta-5'(1')iminium ion. J Pharmacol Exp Ther. 2012 Nov;343(2):307-15. | ||||
25 | 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. | ||||
26 | Comparison of five benzodiazepine-receptor agonists on buprenorphine-induced mu-opioid receptor regulation. J Pharmacol Sci. 2009 May;110(1):36-46. | ||||
27 | 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. | ||||
28 | 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). | ||||
29 | 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. | ||||
30 | New hypnotics: perspectives from sleep physiology. Vertex. 2007 Jul-Aug;18(74):294-9. | ||||
31 | Chun AH, Carrigan PJ, Hoffman DJ, Kershner RP, Stuart JD "Effect of antacids on absorption of clorazepate." Clin Pharmacol Ther 22 (1977): 329-35. [PMID: 19188] | ||||
32 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
33 | 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.". | ||||
34 | Product Information. Synercid (dalfopristin-quinupristin) Rhone-Poulenc Rorer, Collegeville, PA. | ||||
35 | Amsden GW "Macrolides versus azalides: a drug interaction update." Ann Pharmacother 29 (1995): 906-17. [PMID: 8547740] | ||||
36 | Product Information. Tykerb (lapatinib). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
37 | Product Information. Tukysa (tucatinib). Seattle Genetics Inc, Bothell, WA. | ||||
38 | 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.". | ||||
39 | Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002] | ||||
40 | Gill SS, Wright EM, Reilly CS "Pharmacokinetic interaction of propofol and fentanyl: single bolus injection study." Br J Anaesth 65 (1990): 760-5. [PMID: 2265045] | ||||
41 | Divoll M, Greenblatt DJ, Lacasse Y, Shader RI "Benzodiazepine overdosage: plasma concentrations and clinical outcome." Psychopharmacology (Berl) 73 (1981): 381-3. [PMID: 6789361] | ||||
42 | Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ. | ||||
43 | 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] | ||||
44 | Cerner Multum, Inc. "Australian Product Information.". | ||||
45 | Product Information. Xcopri (cenobamate). SK Life Science, Inc., Paramus, NJ. | ||||
46 | EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.". | ||||
47 | Backman JT, Olkkola KT, Ojala M, Laaksovirta H, Neuvonen PJ "Concentrations and effects of oral midazolam are greatly reduced in patients treated with carbamazepine or phenytoin." Epilepsia 37 (1996): 253-7. [PMID: 8598183] | ||||
48 | Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA. | ||||
49 | Ochs HR, Greenblatt DJ, Knuchel M "Differential effect of isoniazid on triazolam oxidation and oxazepam conjugation." Br J Clin Pharmacol 16 (1983): 743-6. [PMID: 6140941] | ||||
50 | Ochs HR, Greenblatt DJ, Roberts GM, Dengler HJ "Diazepam interaction with antituberculosis drugs." Clin Pharmacol Ther 29 (1981): 671-8. [PMID: 7214796] | ||||
51 | Product Information. Agenerase (amprenavir). Glaxo Wellcome, Research Triangle Pk, NC. | ||||
52 | Product Information. Stribild (cobicistat/elvitegravir/emtricitabine/tenofov). Gilead Sciences, Foster City, CA. | ||||
53 | 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] | ||||
54 | Product Information. Orladeyo (berotralstat). BioCryst Pharmaceuticals Inc, Durham, NC. | ||||
55 | Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
56 | Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA. | ||||
57 | Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA. | ||||
58 | Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA. | ||||
59 | Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN. | ||||
60 | Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC. | ||||
61 | Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ. | ||||
62 | Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
63 | 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] | ||||
64 | Product Information. Gattex (teduglutide). NPS Pharmaceuticals, Bedminster, NJ. | ||||
65 | Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA. | ||||
66 | EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.". | ||||
67 | Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200] | ||||
68 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
69 | Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA. | ||||
70 | Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA. | ||||
71 | 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] | ||||
72 | Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL. | ||||
73 | Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA. | ||||
74 | DSouza DL, Levasseur LM, Nezamis J, Robbins DK, Simms L, Koch KM "Effect of alosetron on the pharmacokinetics of alprazolam." J Clin Pharmacol 41 (2001): 452-4. [PMID: 11304902] | ||||
75 | Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY. | ||||
76 | 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] | ||||