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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/05/01 14:42:25」(JST)

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Irbesartan (INN) /ɜrbəˈsɑrtən/ is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Irbesartan was developed by Sanofi Research (now part of sanofi-aventis). It is jointly marketed by sanofi-aventis and Bristol-Myers Squibb under the trade names Aprovel, Karvea, and Avapro.

Clinical use

Main article: Angiotensin II receptor antagonist

Indications

As with all angiotensin II receptor antagonists, irbesartan is indicated for the treatment of hypertension. Irbesartan may also delay progression of diabetic nephropathy and is also indicated for the reduction of renal disease progression in patients with type 2 diabetes,^[1] hypertension and microalbuminuria (>30 mg/24 hours) or proteinuria (>900 mg/24 hours).^[2]

Combination with diuretic

Irbesartan is also available in a combination formulation with a low dose thiazide diuretic, invariably hydrochlorothiazide, to achieve an additive antihypertensive effect. Irbesartan/hydrochlorothiazide combination preparations are marketed under similar trade names to irbesartan preparations, including Irda, CoIrda, CoAprovel, Karvezide, Avalide and Avapro HCT.

Heart failure

A large randomized trial following 4100+ men and women with heart failure and normal ejection fraction (>=45%) over 4+ years found no improvement in study outcomes or survival with irbesartan as compared to placebo.^[3]

Market

BMS annual sales approx $1.3bn. Sanofi-aventis annual sales approx $2.1bn. In the United States, a generic version is available. Patent expired March 2012.

References

^ Lewis EJ, Hunsicker LG, Clarke WR, Berl T, Pohl MA, Lewis JB, Ritz E, Atkins RC, Rohde R, Raz I; Collaborative Study Group. (2001). "Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes". N Engl J Med 345 (12): 851–60. doi:10.1056/NEJMoa011303. PMID 11565517.
^ Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3
^ Massie BM, Carson PE, McMurray JJ, Komajda M, McKelvie R, Zile MR, Anderson S, Donovan M, Iverson E, Staiger C, Ptaszynska A (December 2008). "Irbesartan in patients with heart failure and preserved ejection fraction". N. Engl. J. Med. 359 (23): 2456–67. doi:10.1056/NEJMoa0805450. PMID 19001508.

UpToDate Contents

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1. ACE阻害剤、アンギオテンシン受容体遮断剤、および心房細動 ace inhibitors angiotensin receptor blockers and atrial fibrillation
2. 糖尿病性腎症の治療 treatment of diabetic nephropathy
3. 高血圧治療におけるレニン・アンギオテンシン系阻害 renin angiotensin system inhibition in the treatment of hypertension
4. 糖尿病患者における高血圧治療 treatment of hypertension in patients with diabetes mellitus
5. 2型糖尿病における、中等度に増加したアルブミン尿（微量アルブミン尿） moderately increased albuminuria microalbuminuria in type 2 diabetes mellitus

English Journal

Urinary renin and angiotensinogen in type 2 diabetes: added value beyond urinary albumin?

Persson F, Lu X, Rossing P, Garrelds IM, Danser AH, Parving HH.SourceaSteno Diabetes Center, Gentofte, Denmark bDivision of Pharmacology and Vascular Medicine, Department of Internal Medicine, Erasmus MC, Rotterdam, The Netherlands cFaculty of Health Science, University of Aarhus dNNF Center for Basic Metabolic Research eDepartment of Medical Endocrinology, University of Copenhagen, Denmark *Both authors contributed equally.
Journal of hypertension.J Hypertens.2013 Aug;31(8):1646-52. doi: 10.1097/HJH.0b013e328362217c.
OBJECTIVE: Urinary levels of renin-angiotensin-aldosterone system (RAAS) components may reflect renal RAAS activity and/or the renal efficacy of RAAS inhibition. Our aim was to determine whether urinary angiotensinogen and renin are circulating RAAS-independent markers during RAAS blockade.METHODS:
PMID 23743807

Ionic-liquid based dispersive liquid-liquid microextraction followed by high performance liquid chromatographic determination of anti-hypertensives in rat serum.

Rao RN, Raju SS, Vali RM.SourceAnalytical Chemistry Division, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 007, India. Electronic address: rnrao@iict.res.in.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.J Chromatogr B Analyt Technol Biomed Life Sci.2013 Jul 15;931:174-80. doi: 10.1016/j.jchromb.2013.05.027. Epub 2013 Jun 4.
A novel, simple and eco-friendly ionic liquid based dispersive liquid-liquid microextraction followed by HPLC determination of anti-hypertensive drugs viz., eprosartan, valasartan, irbesartan, losartan and telmisartan in rat serum has been developed and validated. Experimental parameters influencing
PMID 23797113

Comparative effectiveness of angiotensin-receptor blockers for preventing macrovascular disease in patients with diabetes: a population-based cohort study.

Antoniou T, Camacho X, Yao Z, Gomes T, Juurlink DN, Mamdani MM.AbstractBACKGROUND:Telmisartan, unlike other angiotensin-receptor blockers, is a partial agonist of peroxisome proliferator-activated receptor-γ, a property that has been associated with improvements in surrogate markers of cardiovascular health in small trials involving patients with diabetes. However, whether this property translates into a reduced risk of cardiovascular events and death in these patients is unknown. We sought to explore the risk of myocardial infarction, stroke and heart failure in patients with diabetes who were taking telmisartan relative to the risk of these events occurring in patients taking other angiotensinreceptor METHODS:We conducted a populationbased, retrospective cohort study of Ontario residents with diabetes aged 66 years and older who started treatment with candesartan, irbesartan, losartan, telmisartan or valsartan between Apr. 1, 2001, and Mar. 31, 2011. Our primary outcome was a composite of admission to hospital for acute myocardial infarction, stroke or heart failure. We examined each outcome individually in secondary analyses, in addition to all-cause mortality. RESULTS:We identified 54 186 patients with diabetes who started taking an angiotensinreceptor blocker during the study period. After multivariable adjustment, patients who took either telmisartan (adjusted hazard ratio [HR] 0.85, 95% confidence interval [CI] 0.74-0.97) or valsartan (adjusted HR 0.86, 95% CI 0.77-0.95) had a lower risk of the composite outcome compared with patients who took irbesartan. In contrast, no significant difference in risk was seen between other angiotensin-receptor blockers and irbesartan. In secondary analyses, we found a reduced risk of admission to hospital for heart failure with telmisartan compared with irbesartan (adjusted HR 0.79, 95% CI 0.66- 0.96), but no significant differences in risk were seen between angiotensin-receptor blockers in our other secondary analyses. INTERPRETATION:Compared with other angiotensin-receptor blockers, telmisartan and valsartan were both associated with a lower risk of admission to hospital for acute myocardial infarction, stroke or heart failure among older adults with diabetes and hypertension. Telmisartan and val sartan may therefore be the preferred angiotensin-receptor blockers for use in these patients.
CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne.CMAJ.2013 Jul 8. [Epub ahead of print]
BACKGROUND:Telmisartan, unlike other angiotensin-receptor blockers, is a partial agonist of peroxisome proliferator-activated receptor-γ, a property that has been associated with improvements in surrogate markers of cardiovascular health in small trials involving patients with diabetes. However, wh
PMID 23836857

Japanese Journal

Irbesartan Prevents Metabolic Syndrome in Rats via Activation of Peroxisome Proliferator-Activated Receptor γ

Takai Shinji,Jin Denan,Miyazaki Mizuo
Journal of Pharmacological Sciences 116(3), 309-315, 2011
… Irbesartan, an angiotensin-receptor blocker, is a known agonist of peroxisome proliferator-activated receptor (PPAR) γ. … In this study, thirteen-week-old spontaneously hypertensive (SHR)/NDmcr-cp rats, representing a genetic model of metabolic syndrome, were treated daily with placebo, irbesartan (30 mg/kg), valsartan (10 mg/kg), or pioglitazone (10 mg/kg) for 4 weeks. …
NAID 130001014461

Solubility, Dissolution Rate and Bioavailability Enhancement of Irbesartan by Solid Dispersion Technique

Boghra Rikisha Jaysukhbhai,Kothawade Pranita Chandrakant,Belgamwar Veena Shailendra,Nerkar Pankaj Padmakar,Tekade Avinash Ramrao,Surana Sanjay Javerilal
CHEMICAL & PHARMACEUTICAL BULLETIN 59(4), 438-441, 2011
… The objective of present work was to enhance the solubility and bioavailability of poorly aqueous soluble drug Irbesartan (IBS). … In conclusion, the prepared solid dispersions showed remarkable increase in solubility, dissolution rate and hence bioavailabilty of poorly water soluble drug Irbesartan. …
NAID 130000648960

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リンク元

「イルベサルタン」

Irbesartan
Systematic (IUPAC) name
	2-butyl-3-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1,3-diazaspiro[4.4]non-1-en-4-one
Clinical data
Trade names	Avapro
AHFS/Drugs.com	monograph
MedlinePlus	a698009
Licence data	EMA:Link, US FDA:link
Pregnancy cat.	D (Au)
Legal status	S4 (Au), POM (UK), ℞-only (U.S.)
Routes	Oral
Pharmacokinetic data
Bioavailability	60–80%
Protein binding	~90%
Metabolism	Hepatic (CYP2C9)
Half-life	11–15 hours
Excretion	Renal 20%, faecal 65%
Identifiers
CAS number	138402-11-6
ATC code	C09CA04
PubChem	CID 3749
IUPHAR ligand	589
DrugBank	DB01029
ChemSpider	3618
UNII	J0E2756Z7N
KEGG	D00523
ChEBI	CHEBI:5959
ChEMBL	CHEMBL1513
Chemical data
Formula	C25H28N6O
Mol. mass	428.53
	SMILES O=C1N(\C(=N/C12CCCC2)CCCC)Cc5ccc(c3ccccc3c4nnnn4)cc5;
	InChI InChI=1S/C25H28N6O/c1-2-3-10-22-26-25(15-6-7-16-25)24(32)31(22)17-18-11-13-19(14-12-18)20-8-4-5-9-21(20)23-27-29-30-28-23/h4-5,8-9,11-14H,2-3,6-7,10,15-17H2,1H3,(H,27,28,29,30) ; Key:YOSHYTLCDANDAN-UHFFFAOYSA-N ;
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　　[★]

英: irbesartan
商: アバプロ(大日本住友製薬)、イルベタン(塩野義)、アイミクス配合
関: アンジオテンシンII受容体拮抗薬、降圧薬

長時間作用型ARBとされる。

[Lewis-2001-1] Lewis EJ, Hunsicker LG, Clarke WR, Berl T, Pohl MA, Lewis JB, Ritz E, Atkins RC, Rohde R, Raz I; Collaborative Study Group. (2001). "Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes". N Engl J Med 345 (12): 851–60. doi:10.1056/NEJMoa011303. PMID 11565517.

[Rossi2006-2] Rossi S, editor. Australian Medicines Handbook 2006. Adelaide: Australian Medicines Handbook; 2006. ISBN 0-9757919-2-3

[pmid19001508-3] Massie BM, Carson PE, McMurray JJ, Komajda M, McKelvie R, Zile MR, Anderson S, Donovan M, Iverson E, Staiger C, Ptaszynska A (December 2008). "Irbesartan in patients with heart failure and preserved ejection fraction". N. Engl. J. Med. 359 (23): 2456–67. doi:10.1056/NEJMoa0805450. PMID 19001508.

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irbesartan