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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/01/09 16:55:47」(JST)

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Bucolome (Paramidine) is a barbiturate derivative. Unlike most barbiturates it does not have any significant sedative or hypnotic effects, but instead acts as an analgesic and antiinflammatory. It also acts as a CYP2C9 inhibitor and reduces the metabolism of several commonly used drugs, which makes it useful for potentiating or extending the duration of action of those drugs, or reducing the production of unwanted metabolites.^[1]^[2]^[3]

References

^ Takamura N, Maruyama T, Chosa E, Kawai K, Tsutsumi Y, Uryu Y, Yamasaki K, Deguchi T, Otagiri M. Bucolome, a potent binding inhibitor for furosemide, alters the pharmacokinetics and diuretic effect of furosemide: potential for use of bucolome to restore diuretic response in nephrotic syndrome. Drug Metabolism and Disposition. 2005 Apr;33(4):596-602. PMID 15640375
^ Osawa M, Hada N, Matsumoto K, Hasegawa T, Kobayashi D, Morimoto Y, Yamaguchi M, Kanamoto I, Nakagawa T, Sugibayashi K. Usefulness of coadministration of bucolome in warfarin therapy: pharmacokinetic and pharmacodynamic analysis using outpatient prescriptions. International Journal of Pharmaceutics. 2005 Apr 11;293(1-2):43-9. PMID 15778043
^ Kobayashi M, Takagi M, Fukumoto K, Kato R, Tanaka K, Ueno K. The effect of bucolome, a CYP2C9 inhibitor, on the pharmacokinetics of losartan. Drug Metabolism and Pharmacokinetics. 2008;23(2):115-9. PMID 18445991

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English Journal

Pharmacokinetic alteration of (99m)Tc-MAG3 using serum protein binding displacement method.

Nishi K, Kobayashi M, Nishii R, Shikano N, Takamura N, Kuga N, Yamasaki K, Nagamachi S, Tamura S, Otagiri M, Kawai K.SourceSchool of Health Sciences, College of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Kanazawa, Ishikawa 920-0942, Japan.
Nuclear medicine and biology.Nucl Med Biol.2013 Apr;40(3):366-70. doi: 10.1016/j.nucmedbio.2012.12.002. Epub 2013 Jan 9.
INTRODUCTION: When a radiopharmaceutical is simultaneously administered with a medicine that has high affinity for the same plasma protein, the radiopharmaceutical is released at higher concentrations in blood, leading to enhanced transfer into target tissues. This is known as the serum protein bind
PMID 23312701

Effects of combination therapy with warfarin and bucolome for anticoagulation in patients with atrial fibrillation.

Obata H, Watanabe H, Ito M, Hirono S, Hanawa H, Kodama M, Aizawa Y.SourceDivision of Cardiology, Niigata University School of Medical and Dental Sciences, Niigata, Japan. h-oba@qc4.so-net.ne.jp
Circulation journal : official journal of the Japanese Circulation Society.Circ J.2011;75(1):201-3. Epub 2010 Dec 2.
BACKGROUND: Bucolome, a nonsteroidal antiinflammatory drug, enhances the effects of warfarin. In the present study, the effects of combination therapy (bucolome+warfarin) vs. warfarin alone on atrial fibrillation were investigated.METHODS AND RESULTS: Combined therapy resulted in a decrease in the w
PMID 21139249

Identification of the UDP-glucuronosyltransferase responsible for bucolome N-glucuronide formation in rats.

Kanoh H, Okada K, Mohri K.SourceClinical Pharmaceutics Laboratory, Department of Pharmacy and Health Sciences, Faculty of Pharmacy and Pharmaceutical Sciences, Meiji Pharmaceutical University, Tokyo, Japan.
Die Pharmazie.Pharmazie.2010 Nov;65(11):840-4.
Bucolome N-glucuronide (BCP-NG), a major metabolite of bucolome (BCP), is the first unique N-glucuronide of barbituric acid derivatives to be reported. The purpose of the present study was to identify the UGT isoform(s) responsible for BCP-NG formation in rats. A pharmacokinetic study of BCP and the
PMID 21155392

Japanese Journal

Effects of Combination Therapy With Warfarin and Bucolome for Anticoagulation in Patients With Atrial Fibrillation

OBATA Hiroaki,WATANABE Hiroshi,ITO Masahiro,HIRONO Satoru,HANAWA Haruo,KODAMA Makoto,AIZAWA Yoshifusa
Circulation journal : official journal of the Japanese Circulation Society 75(1), 201-203, 2010-12-25
… Background: Bucolome, a nonsteroidal antiinflammatory drug, enhances the effects of warfarin. … In the present study, the effects of combination therapy (bucolome+warfarin) vs. warfarin alone on atrial fibrillation were investigated. … Interestingly, uric acid was lower in the bucolome group. …
NAID 10027425977

Risks and Benefits of Combined Use of Bucolome and Warfarin in Anticoagulation Therapy

Hatakeyama Yuko,Niwano Shinichi,Niwano Hiroe,Kosukegawa Tomoko,Izumi Tohru
International Heart Journal 51(6), 399-403, 2010
… Although bucolome has been used empirically to enhance and stabilize warfarin action in some institutes, the clinical risks and benefits of this combination are unclear. … In the present study, warfarin monotherapy (WM) and bucolome combination (BC) therapy were compared in anticoagulation therapy.One hundred and ninety-five patients indicated for anticoagulation therapy were randomly assigned to WM (n = 98) or BC (bucolome 300 mg/day, n = 97). …
NAID 130000410624

Related Pictures

★リンクテーブル★

リンク元

「ブコローム」

Bucolome
Clinical data
AHFS/Drugs.com	International Drug Names
ATC code	none
Identifiers
	IUPAC name 5-butyl-1-cyclohexyl-1,3-diazinane-2,4,6-trione;
Synonyms	Bucolome, Paramidine
CAS Number	841-73-6
PubChem (CID)	2461
ChemSpider	2367
UNII	9T08RAL174
ChEBI	CHEBI:31314
ChEMBL	CHEMBL2106136
ECHA InfoCard	100.011.515
Chemical and physical data
Formula	C14H22N2O3
Molar mass	224.256 g/mol
3D model (Jmol)	Interactive image
	SMILES CCCCC1C(=O)NC(=O)N(C1=O)C2CCCCC2 ;
	InChI InChI=1S/C14H22N2O3/c1-2-3-9-11-12(17)15-14(19)16(13(11)18)10-7-5-4-6-8-10/h10-11H,2-9H2,1H3,(H,15,17,19) ; Key:DVEQCIBLXRSYPH-UHFFFAOYSA-N ;
(verify)

　　[★]

英: bucolome
商: パラミヂン

[1] Takamura N, Maruyama T, Chosa E, Kawai K, Tsutsumi Y, Uryu Y, Yamasaki K, Deguchi T, Otagiri M. Bucolome, a potent binding inhibitor for furosemide, alters the pharmacokinetics and diuretic effect of furosemide: potential for use of bucolome to restore diuretic response in nephrotic syndrome. Drug Metabolism and Disposition. 2005 Apr;33(4):596-602. PMID 15640375

[2] Osawa M, Hada N, Matsumoto K, Hasegawa T, Kobayashi D, Morimoto Y, Yamaguchi M, Kanamoto I, Nakagawa T, Sugibayashi K. Usefulness of coadministration of bucolome in warfarin therapy: pharmacokinetic and pharmacodynamic analysis using outpatient prescriptions. International Journal of Pharmaceutics. 2005 Apr 11;293(1-2):43-9. PMID 15778043

[3] Kobayashi M, Takagi M, Fukumoto K, Kato R, Tanaka K, Ueno K. The effect of bucolome, a CYP2C9 inhibitor, on the pharmacokinetics of losartan. Drug Metabolism and Pharmacokinetics. 2008;23(2):115-9. PMID 18445991

v t e Non-steroidal anti-inflammatory drugs (NSAIDs) (primarily M01A and M02A, also N02BA)

Pyrazolones / Pyrazolidines	Aminophenazone Ampyrone Azapropazone Clofezone Difenamizole Famprofazone Feprazone Kebuzone Metamizole Mofebutazone Morazone Nifenazone Oxyphenbutazone Phenazone Phenylbutazone Propyphenazone Sulfinpyrazone Suxibuzone^‡

Salicylates	Aspirin (acetylsalicylic acid)^# Aloxiprin Benorylate Carbasalate calcium Diflunisal Dipyrocetyl Ethenzamide Guacetisal Magnesium salicylate Methyl salicylate Salsalate Salicin Salicylamide Salicylic acid (salicylate) Sodium salicylate

Acetic acid derivatives and related substances	Aceclofenac Acemetacin Alclofenac Amfenac Bendazac Bromfenac Bumadizone Bufexamac Diclofenac Difenpiramide Etodolac Felbinac Fenclozic acid Fentiazac Indomethacin Indomethacin farnesil Isoxepac Ketorolac Lonazolac Oxametacin Prodolic acid Proglumetacin Sulindac Tiopinac Tolmetin Zomepirac^†

Oxicams	Ampiroxicam Droxicam Isoxicam Lornoxicam Meloxicam Piroxicam Tenoxicam

Propionic acid derivatives (profens)	Alminoprofen Benoxaprofen^† Carprofen^‡ Dexibuprofen Dexketoprofen Fenbufen Fenoprofen Flunoxaprofen Flurbiprofen Ibuprofen^# Ibuproxam Indoprofen^† Ketoprofen Loxoprofen Miroprofen Naproxen Oxaprozin Pirprofen Suprofen Tarenflurbil Tepoxalin^‡ Tiaprofenic acid Vedaprofen^‡ COX-inhibiting nitric oxide donator: Naproxcinod

N-Arylanthranilic acids (fenamates)	Azapropazone Clonixin Etofenamate Flufenamic acid Flunixin Meclofenamic acid Mefenamic acid Morniflumate Niflumic acid Tolfenamic acid Flutiazin

Coxibs	Apricoxib Celecoxib Cimicoxib^‡ Deracoxib^‡ Etoricoxib Firocoxib^‡ Lumiracoxib^† Mavacoxib^‡ Parecoxib Robenacoxib^‡ Rofecoxib^† Valdecoxib^†

Other	Aminopropionitrile Benzydamine Chondroitin sulfate Diacerein Fluproquazone Glucosamine Glycosaminoglycan Hyperforin Nabumetone Nimesulide Oxaceprol Proquazone Superoxide dismutase/Orgotein Tenidap

Items listed in bold indicate initially developed compounds of specific groups. ^#WHO-EM ^†Withdrawn drugs. ^‡Veterinary use medications.

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bucolome