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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/06/29 23:28:02」(JST)

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Benazepril, brand name Lotensin (Novartis), is a drug of the angiotensin-converting enzyme (ACE) inhibitor class used primarily in treatment of hypertension, congestive heart failure, and heart attacks, and also in preventing renal and retinal complications of diabetes. Its indications, contraindications and side effects are as those for all ACE inhibitors. The drug is a precursor of the active agent, which is metabolized by the liver into its active form. Upon cleavage of its ester group benazepril is converted into benazeprilat, its active form, which is a non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor.

Dosage forms

Benazepril is available as oral tablets, in 5-, 10-, 20-, and 40-mg doses.

Benazepril is also available in combination with hydrochlorothiazide, under the trade name Lotensin HCT, and with amlodipine (trade name Lotrel).

Side effects

The most common side effects patients experience are headaches or a chronic cough. The chronic cough develops in about 20 percent of patients treated,^[1] and those patients that experience it find it develops after a couple of months of use. Anaphylaxis, angioedema and hyperkalemia, the elevation of potassium levels, are more serious side effects that can also occur.

Benazepril may cause harm to the fetus during pregnancy.

Contraindications

Benazepril should be discontinued during pregnancy.

Kidney disease

According to a 2006 article in the New England Journal of Medicine, patients with advanced renal insufficiency taking benazepril showed "substantial" kidney benefits.^[2]

A long-term study of patients' kidney disease revealed patients who took benazepril had better kidney function and slower progressions of kidney disease than their peers who took a placebo drug.^[3] This is notable because this category of pharmaceuticals has long been thought to cause further kidney damage or increase the rate of progression for kidney disease.

According to coverage of the study on WebMD:

“

ACE inhibitors can pose a potential threat to kidneys as well. The key question was whether damaged kidneys would worsen if patients took ACE inhibitors. In a nutshell, concerns centered on blood levels of potassium and creatinine, waste products that are excreted by the kidneys. Testing creatinine levels in the blood is used as a way to monitor kidney function (...) kidney problems worsened more slowly in those taking Lotensin. Overall, there were no major differences in side effects between patients taking Lotensin or the placebo.^[3]

”

This study marks the first indication that benazepril, and perhaps other ACE inhibitors, may actually be beneficial in the treatment of hypertension in patients with kidney disease.

Veterinary use

Under the brand names Fortekor (Novartis) and VetACE (Jurox Animal Health),^{[citation needed]} benazepril hydrochloride is used to treat congestive heart failure in dogs^[4]^[5] and chronic renal failure in dogs and cats.^{[citation needed]}

References

^ Dykewicz, Mark S. (April 2004). "Cough and Angioedema From Angiotensin-Converting Enzyme Inhibitors: New Insights Into Mechanisms and Management". Medscape. Retrieved 2 April 2014.
^ Hou F, Zhang X, Zhang G, Xie D, Chen P, Zhang W, Jiang J, Liang M, Wang G, Liu Z, Geng R (2006). "Efficacy and safety of benazepril for advanced chronic renal insufficiency". N Engl J Med 354 (2): 131–40. doi:10.1056/NEJMoa053107. PMID 16407508.
^ ^a ^b Hitti, Miranda; Chang, Louise (January 11, 2006). "Drug May Treat Advanced Kidney Disease". WebMD. Retrieved 2006-09-07.
^ King JN, Mauron C, Kaiser G (December 1995). "Pharmacokinetics of the active metabolite of benazepril, benazeprilat, and inhibition of plasma angiotensin-converting enzyme activity after single and repeated administrations to dogs". Am. J. Vet. Res. 56 (12): 1620–8. PMID 8599524.
^ O'Grady MR, O'Sullivan ML, Minors SL, Horne R (2009). "Efficacy of benazepril hydrochloride to delay the progression of occult dilated cardiomyopathy in Doberman Pinschers". J. Vet. Intern. Med. 23 (5): 977–83. doi:10.1111/j.1939-1676.2009.0346.x. PMID 19572914.

External links

Prescribing Information for Lotensin

UpToDate Contents

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1. 心不全におけるアンギオテンシン変換酵素阻害剤およびアンギオテンシン受容体拮抗剤：作用機序 angiotensin converting enzyme inhibitors and receptor blockers in heart failure mechanisms of action

English Journal

Chronobiology and Pharmacologic Modulation of the Renin-Angiotensin-Aldosterone System in Dogs: What Have We Learned?

Mochel JP1,2, Danhof M3.
Reviews of physiology, biochemistry and pharmacology.Rev Physiol Biochem Pharmacol.2015 Oct 2. [Epub ahead of print]
Congestive heart failure (CHF) is a primary cause of morbidity and mortality with an increasing prevalence in human and canine populations. Recognition of the role of renin-angiotensin-aldosterone system (RAAS) overactivation in the pathophysiology of CHF has led to significant medical advances. By
PMID 26428686

Development of a new benazepril hydrochloride chewable tablet and evaluation of its bioequivalence for treatment of heart failure in dogs.

Qian M1, Chen T1, Zhou D1, Zhang Z1, Zhang Q1, Tang S1, Xiao X1.
Journal of veterinary pharmacology and therapeutics.J Vet Pharmacol Ther.2015 Jul 30. doi: 10.1111/jvp.12252. [Epub ahead of print]
The aim of the study was to develop a new chewable benazepril hydrochloride(BH) tablet, investigate its physical properties, and evaluate its bioequivalence with the branded formulation (Fortekor® ). A corrective agent was included in the formula to improve its palatability and convenience for admi
PMID 26228576

Pharmacokinetic/Pharmacodynamic Modeling of Renin-Angiotensin Aldosterone Biomarkers Following Angiotensin-Converting Enzyme (ACE) Inhibition Therapy with Benazepril in Dogs.

Mochel JP1, Fink M, Peyrou M, Soubret A, Giraudel JM, Danhof M.
Pharmaceutical research.Pharm Res.2015 Jun;32(6):1931-46. doi: 10.1007/s11095-014-1587-9. Epub 2014 Dec 2.
PURPOSE: The objective of this research was to provide a comprehensive description of the effect of benazepril on the dynamics of the renin-angiotensin aldosterone system (RAAS) in dogs.METHODS: Blood specimens for renin activity (RA), angiotensin II (AII), and aldosterone (ALD) quantitation in plas
PMID 25446774

Japanese Journal

Simultaneous determination of benazepril hydrochloride and benazeprilat in plasma by high-performance liquid chromatography/electrospray-mass spectrometry

XIAO Weitao,CHEN Bo,YAO Shouzhuo,CHENG Zeneng
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 814(2), 303-308, 2005-01-25
NAID 10018272963

アンジオテンシン変換酵素阻害剤ベナゼプリルは腹水を伴う犬糸状虫症犬の肝臓において活性型ベナゼプリラートに変換される(内科学)

北川均,大場恵典,桑原康人 [他],大根理恵子,近藤昌弘,中野正和,佐々木栄英,鬼頭克也
The journal of veterinary medical science 65(6), 701-706, 2003-06-25
アンジオテンシン変換酵素(ACE)阻害剤ベナゼプリルが,腹水を伴う犬糸状虫症犬の重度に傷害された肝臓によって活性型であるベナゼプリラートに変換されるかどうかを検討する目的で,塩酸ベナゼプリルを0.29mg/kgから0.625mg/kgの投与量で7日間経口投与し,ベナゼプリラートの血中濃度を測定した.腹水を伴う犬糸状虫症犬7例では,血漿ベナゼプリラート濃度は投与第1日と第7日とも対照犬よりも高い傾向 …
NAID 110003886241

Quantitative determination of benazepril and benazeprilat in human plasma by gas chromatography-mass spectrometry using automated 96-well disk plate solid-phase extraction for sample preparation

POMMIER F.,BOSCHET F.,GOSSET G.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 783(1), 199-205, 2003-01-05
NAID 10012028143

Related Pictures

★リンクテーブル★

リンク元	「ベナゼプリラート」

「ベナゼプリラート」

Benazepril
Systematic (IUPAC) name
	2-[(3S)-3-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino}-
Clinical data
Trade names	Lotensin
AHFS/Drugs.com	monograph
MedlinePlus	a692011
Pregnancy cat.	D
Legal status	℞ Prescription only
Routes	Oral
Pharmacokinetic data
Protein binding	96.7%
Metabolism	Hepatic glucuronidation
Half-life	10-11 hours
Excretion	Renal and biliary
Identifiers
CAS number	86541-75-5
ATC code	C09AA07
PubChem	CID 5362124
DrugBank	DB00542
ChemSpider	4514935
UNII	UDM7Q7QWP8
ChEBI	CHEBI:3011
ChEMBL	CHEMBL838
Chemical data
Formula	C24H28N2O5
Mol. mass	424.49 g/mol
	SMILES O=C(OCC)[C@@H](N[C@@H]2C(=O)N(c1ccccc1CC2)CC(=O)O)CCc3ccccc3;
	InChI InChI=1S/C24H28N2O5/c1-2-31-24(30)20(14-12-17-8-4-3-5-9-17)25-19-15-13-18-10-6-7-11-21(18)26(23(19)29)16-22(27)28/h3-11,19-20,25H,2,12-16H2,1H3,(H,27,28)/t19-,20-/m0/s1 ; Key:XPCFTKFZXHTYIP-PMACEKPBSA-N ;
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英: benazeprilat
同: ベナゼプリラト
関: ベナゼプリル

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ベナゼプリラト : 45 件
ベナゼプリラート : 約 593 件

アンジオテンシン変換酵素阻害薬ベナゼプリルの活性代謝物

[1] Dykewicz, Mark S. (April 2004). "Cough and Angioedema From Angiotensin-Converting Enzyme Inhibitors: New Insights Into Mechanisms and Management". Medscape. Retrieved 2 April 2014.

[Hou-2] Hou F, Zhang X, Zhang G, Xie D, Chen P, Zhang W, Jiang J, Liang M, Wang G, Liu Z, Geng R (2006). "Efficacy and safety of benazepril for advanced chronic renal insufficiency". N Engl J Med 354 (2): 131–40. doi:10.1056/NEJMoa053107. PMID 16407508.

[Hitti-3] Hitti, Miranda; Chang, Louise (January 11, 2006). "Drug May Treat Advanced Kidney Disease". WebMD. Retrieved 2006-09-07.

[4] King JN, Mauron C, Kaiser G (December 1995). "Pharmacokinetics of the active metabolite of benazepril, benazeprilat, and inhibition of plasma angiotensin-converting enzyme activity after single and repeated administrations to dogs". Am. J. Vet. Res. 56 (12): 1620–8. PMID 8599524.

[5] O'Grady MR, O'Sullivan ML, Minors SL, Horne R (2009). "Efficacy of benazepril hydrochloride to delay the progression of occult dilated cardiomyopathy in Doberman Pinschers". J. Vet. Intern. Med. 23 (5): 977–83. doi:10.1111/j.1939-1676.2009.0346.x. PMID 19572914.

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benazeprilat