Details of the Drug
General Information of Drug (ID: DMW1OQ0)
Drug Name |
Clobazam - Lundbeck
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Synonyms |
Clobazam; Chlorepin; Urbanyl; Frisium; Clorepin; Urbadan; 22316-47-8; Clobazamum; Onfi; LM-2717; HR 376; RU-4723; Clobazamum [INN-Latin]; LM 2717; H-4723; H 4723; 7-Chloro-1-methyl-5-phenyl-1H-1,5-benzodiazepine-2,4(3H,5H)-dione; UNII-2MRO291B4U; 1H-1,5-Benzodiazepine-2,4(3H,5H)-dione, 7-chloro-1-methyl-5-phenyl-; NSC 336279; 1-Phenyl-5-methyl-8-chloro-1,2,4,5-tetrahydro-2,4-dioxo-3H-1,5-benzodiazepine; CCRIS 7506; 7-chloro-1-methyl-5-phenyl-1,5-benzodiazepine-2,4-dione; EINECS 244-908-7; BRN 0758410; Onfi
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Indication |
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Therapeutic Class |
Neurology Agents
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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) | 300.74 | ||||||||||||||||||||||
Topological Polar Surface Area (xlogp) | 2.1 | |||||||||||||||||||||||
Rotatable Bond Count (rotbonds) | 1 | |||||||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 0 | |||||||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 2 | |||||||||||||||||||||||
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 Transporter (DTP) |
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Drug-Metabolizing Enzyme (DME) |
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Molecular Interaction Atlas (MIA) | ||||||||||||||||||||||||||||||||||||||||||
Molecular Expression Atlas of This Drug
The Studied Disease | Anxiety disorder | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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ICD Disease Classification | 6B00-6B0Z | |||||||||||||||||||||||||||||||||||||||||||||||||||||
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Molecular Expression Atlas (MEA) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Disease Different from Clobazam - Lundbeck (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: 7149). | ||||
---|---|---|---|---|---|
2 | Drug information of Clobazam, 2008. eduDrugs. | ||||
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 | An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9. | ||||
8 | DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. | ||||
9 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
10 | Tarascon Pocket Pharmacopoeia 2018 Classic Shirt-Pocket Edition. | ||||
11 | In vitro characterization of clobazam metabolism by recombinant cytochrome P450 enzymes: importance of CYP2C19. Drug Metab Dispos. 2004 Nov;32(11):1279-86. | ||||
12 | A major influence of CYP2C19 genotype on the steady-state concentration of N-desmethylclobazam. Brain Dev. 2004 Dec;26(8):530-4. | ||||
13 | 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. | ||||
14 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
15 | 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. | ||||
16 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
17 | 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. | ||||
18 | 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. | ||||
19 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
20 | 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. | ||||
21 | 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. | ||||
22 | Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. | ||||
23 | Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70. | ||||
24 | Possible involvement of multiple human cytochrome P450 isoforms in the liver metabolism of propofol. Br J Anaesth. 1998 Jun;80(6):788-95. | ||||
25 | Identification of human cytochrome P450s involved in the formation of all-trans-retinoic acid principal metabolites. Mol Pharmacol. 2000 Dec;58(6):1341-8. | ||||
26 | Targeted antipeptide antibodies to cytochrome P450 2C18 based on epitope mapping of an inhibitory monoclonal antibody to P450 2C51. Arch Biochem Biophys. 1997 Feb 15;338(2):157-64. | ||||
27 | Involvement of cytochrome P450 3A4 enzyme in the N-demethylation of methadone in human liver microsomes. Chem Res Toxicol. 1996 Mar;9(2):365-73. | ||||
28 | CYP2C8/9 mediate dapsone N-hydroxylation at clinical concentrations of dapsone. Drug Metab Dispos. 2000 Aug;28(8):865-8. | ||||
29 | Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metab Dispos. 2001 Mar;29(3):242-51. | ||||
30 | Effect of tamoxifen on the enzymatic activity of human cytochrome CYP2B6. J Pharmacol Exp Ther. 2002 Jun;301(3):945-52. | ||||
31 | Hepatic metabolism of diclofenac: role of human CYP in the minor oxidative pathways. Biochem Pharmacol. 1999 Sep 1;58(5):787-96. | ||||
32 | Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. | ||||
33 | Insights into CYP2B6-mediated drug-drug interactions. Acta Pharm Sin B. 2016 Sep;6(5):413-425. | ||||
34 | Drugs that may have potential CYP2B6 interactions. | ||||
35 | Involvement of human cytochrome P450 2B6 in the omega- and 4-hydroxylation of the anesthetic agent propofol. Xenobiotica. 2007 Jul;37(7):717-24. | ||||
36 | Nicotine and 4-(methylnitrosamino)-1-(3-pyridyl)-butanone metabolism by cytochrome P450 2B6. Drug Metab Dispos. 2005 Dec;33(12):1760-4. | ||||
37 | PharmGKB summary: phenytoin pathway. Pharmacogenet Genomics. 2012 Jun;22(6):466-70. | ||||
38 | Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther. 2001 Apr;297(1):326-37. | ||||
39 | High-dose rabeprazole/amoxicillin therapy as the second-line regimen after failure to eradicate H. pylori by triple therapy with the usual doses of a proton pump inhibitor, clarithromycin and amoxicillin. Hepatogastroenterology. 2003 Nov-Dec;50(54):2274-8. | ||||
40 | Progesterone and testosterone hydroxylation by cytochromes P450 2C19, 2C9, and 3A4 in human liver microsomes. Arch Biochem Biophys. 1997 Oct 1;346(1):161-9. | ||||
41 | Cytochrome P450 pharmacogenetics and cancer. Oncogene. 2006 Mar 13;25(11):1679-91. | ||||
42 | CYP2C19*17 is associated with decreased breast cancer risk. Breast Cancer Res Treat. 2009 May;115(2):391-6. | ||||
43 | Cytochromes of the P450 2C subfamily are the major enzymes involved in the O-demethylation of verapamil in humans. Naunyn Schmiedebergs Arch Pharmacol. 1995 Dec;353(1):116-21. | ||||
44 | A mechanistic approach to antiepileptic drug interactions. Ann Pharmacother. 1998 May;32(5):554-63. | ||||
45 | Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. | ||||
46 | Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007. | ||||
47 | MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. | ||||
48 | Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64. | ||||
49 | Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31. | ||||
50 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. | ||||
51 | Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. | ||||
52 | Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50. | ||||
53 | 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: 415). | ||||
54 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
55 | Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16. | ||||
56 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020 | ||||
57 | Prodynorphin gene deletion increased anxiety-like behaviours, impaired the anxiolytic effect of bromazepam and altered GABAA receptor subunits gene expression in the amygdala. J Psychopharmacol. 2011Jan;25(1):87-96. | ||||
58 | Zolpidem, a selective GABA(A) receptor alpha1 subunit agonist, induces comparable Fos expression in oxytocinergic neurons of the hypothalamic paraventricular and accessory but not supraoptic nuclei in the rat.Brain Res Bull.2006 Dec 11;71(1-3):200-7. | ||||
59 | Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (... J Med Chem. 2005 Apr 21;48(8):3051-9. | ||||
60 | 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7. | ||||
61 | 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] | ||||
62 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
63 | 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.". | ||||
64 | Product Information. Onfi (clobazam). Lundbeck Inc, Deerfield, IL. | ||||
65 | Product Information. Aricept (donepezil). Pfizer US Pharmaceuticals, New York, NY. | ||||
66 | Product Information. Synercid (dalfopristin-quinupristin) Rhone-Poulenc Rorer, Collegeville, PA. | ||||
67 | Amsden GW "Macrolides versus azalides: a drug interaction update." Ann Pharmacother 29 (1995): 906-17. [PMID: 8547740] | ||||
68 | Product Information. Tykerb (lapatinib). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
69 | Product Information. Raxar (grepafloxacin). Glaxo Wellcome, Research Triangle Park, NC. | ||||
70 | 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.". | ||||
71 | Warrington SJ, Ankier SI, Turner P "Evaluation of possible interactions between ethanol and trazodone or amitriptyline." Neuropsychobiology 15 (1986): 31-7. [PMID: 3725002] | ||||
72 | Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.". | ||||
73 | Faculty of Sexual & Reproductive Healthcare "FSRH Clinical Guidance: Drug Interactions with Hormonal Contraception.". | ||||
74 | 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] | ||||
75 | Cerner Multum, Inc. "Canadian Product Information.". | ||||
76 | Divoll M, Greenblatt DJ, Lacasse Y, Shader RI "Benzodiazepine overdosage: plasma concentrations and clinical outcome." Psychopharmacology (Berl) 73 (1981): 381-3. [PMID: 6789361] | ||||
77 | Product Information. Prevymis (letermovir). Merck & Company Inc, Whitehouse Station, NJ. | ||||
78 | 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] | ||||
79 | 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] | ||||
80 | Product Information. Cymbalta (duloxetine). Lilly, Eli and Company, Indianapolis, IN. | ||||
81 | Product Information. Rexulti (brexpiprazole). Otsuka American Pharmaceuticals Inc, Rockville, MD. | ||||
82 | Cerner Multum, Inc. "Australian Product Information.". | ||||
83 | 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] | ||||
84 | EMEA. European Medicines Agency "EPARs. European Union Public Assessment Reports.". | ||||
85 | Product Information. Epidiolex (cannabidiol). Greenwich Biosciences Inc, Carlsbad, CA. | ||||
86 | Edeki TI, He HB, Wood AJJ "Pharmacogenetic explanation for excessive beta-blockade following timolol eye drops: potential for oral-ophthalmic drug interaction." JAMA 274 (1995): 1611-3. [PMID: 7474246] | ||||
87 | Brynne N, Svanstrom C, AbergWistedt A, Hallen B, Bertilsson L "Fluoxetine inhibits the metabolism of tolterodin-pharmacokinetic implications and proposed clinical relevance." Br J Clin Pharmacol 48 (1999): 553-63. [PMID: 10583026] | ||||
88 | Product Information. Enablex (darifenacin). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
89 | Grigoleit HG, Hajdu P, Hundt HK, et al. "Pharmacokinetic aspects of the interaction between clobazam and cimetidine." Eur J Clin Pharmacol 25 (1983): 139-42. [PMID: 6617718] | ||||
90 | Product Information. Alphagan (brimonidine ophthalmic). Allergan Inc, Irvine, CA. | ||||
91 | Castillo-Ferrando JR, Garcia M, Carmona J "Digoxin levels and diazepam." Lancet 2 (1980): 368. [PMID: 6105500] | ||||
92 | 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] | ||||
93 | Ochs HR, Greenblatt DJ, Roberts GM, Dengler HJ "Diazepam interaction with antituberculosis drugs." Clin Pharmacol Ther 29 (1981): 671-8. [PMID: 7214796] | ||||
94 | Barry M, Mulcahy F, Merry C, Gibbons S, Back D "Pharmacokinetics and potential interactions amongst antiretroviral agents used to treat patients with HIV infection." Clin Pharmacokinet 36 (1999): 289-304. [PMID: 10320951] | ||||
95 | Product Information. Agenerase (amprenavir). Glaxo Wellcome, Research Triangle Pk, NC. | ||||
96 | Greenblatt DJ, vonMoltke LL, Harmatz JS, Durol ALB, Daily JP, Graf JA, Mertzanis P, Hoffman JL, Shader RI "Alprazolam-ritonavir interaction: Implications for product labeling." Clin Pharmacol Ther 67 (2000): 335-41. [PMID: 10801241] | ||||
97 | 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] | ||||
98 | Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA. | ||||
99 | Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN. | ||||
100 | Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC. | ||||
101 | Product Information. Thalomid (thalidomide). Celgene Corporation, Warren, NJ. | ||||
102 | Product Information. Tasigna (nilotinib). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
103 | Product Information. Gleevec (imatinib mesylate). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
104 | Canadian Pharmacists Association. | ||||
105 | Product Information. Gattex (teduglutide). NPS Pharmaceuticals, Bedminster, NJ. | ||||
106 | 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] | ||||
107 | Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ. | ||||
108 | Sekar M, Mimpriss TJ "Buprenorphine, benzodiazepines and prolonged respiratory depression." Anaesthesia 42 (1987): 567-8. [PMID: 3592200] | ||||
109 | Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ. | ||||
110 | 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] | ||||
111 | Franco-Salinas G, de la Rosette JJ, Michel MC "Pharmacokinetics and pharmacodynamics of tamsulosin in its modified-release and oral controlled absorption system formulations." Clin Pharmacokinet 49 (2010): 177-88. [PMID: 20170206] | ||||
112 | Product Information. Prograf (tacrolimus). Fujisawa, Deerfield, IL. | ||||
113 | Abernethy DR, Greenblatt DJ, Steel K, Shader RI "Impairment of hepatic drug oxidation by propoxyphene." Ann Intern Med 97 (1982): 223-4. [PMID: 7103282] | ||||
114 | Product Information. Abilify (aripiprazole). Bristol-Myers Squibb, Princeton, NJ. | ||||
115 | Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA. | ||||
116 | Product Information. Zanaflex (tizanidine). Acorda Therapeutics, Hawthorne, NY. | ||||