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a complex consisting of an organic base in association with hydrogen chloride

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/28 15:24:26」(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 nonsulfhydryl ACE inhibitor.

Medical uses

Kidney disease

Patients with advanced renal insufficiency taking benazepril show "substantial" kidney benefits.^[1] 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.^[2] 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.^[2]" 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.

Side effects

The most common side effects patients experience are a headache or a chronic cough. The chronic cough develops in about 20% of patients treated,^[3] and those patients that experience it find it develops after a few months of use. Anaphylaxis, angioedema, and elevation of potassium levels are more serious side effects that can also occur.

Contraindications

Benazepril should be discontinued during pregnancy, as it can harm the fetus.

Dosage forms

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

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

^ 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.
^ Dykewicz, Mark S. (April 2004). "Cough and Angioedema From Angiotensin-Converting Enzyme Inhibitors: New Insights Into Mechanisms and Management". Medscape. Retrieved 2 April 2014.
^ 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. 原発性（本態性）高血圧における治療選択：推奨 choice of therapy in primary essential hypertension recommendations
2. 成人の非糖尿病性慢性腎臓病患者に対する降圧療法と病状の進展 antihypertensive therapy and progression of nondiabetic chronic kidney disease in adults
3. 原発性（本態性）高血圧における治療選択：臨床試験 choice of therapy in primary essential hypertension clinical trials
4. 糖尿病患者における高血圧治療 treatment of hypertension in patients with diabetes mellitus
5. 高齢者における高血圧、特に収縮期高血圧の治療 treatment of hypertension in the elderly patient particularly isolated systolic hypertension

English Journal

Comparison of Benazepril Plus Amlodipine or Hydrochlorothiazide in High-Risk Patients With Hypertension and Coronary Artery Disease.

Bakris G, Briasoulis A, Dahlof B, Jamerson K, Weber MA, Kelly RY, Hester A, Hua T, Zappe D, Pitt B; ACCOMPLISH Investigators.SourceUniversity of Chicago Pritzker School of Medicine, Chicago, Illinois. Electronic address: gbakris@gmail.com.
The American journal of cardiology.Am J Cardiol.2013 Apr 11. pii: S0002-9149(13)00822-9. doi: 10.1016/j.amjcard.2013.03.026. [Epub ahead of print]
Combination therapy with benazepril 40 mg and amlodipine 10 mg (B+A) has been shown to be more effective than benazepril 40 mg and hydrochlorothiazide (HCTZ) 25 mg (B+H) in reducing cardiovascular (CV) events in high-risk patients with stage 2 hypertension with similar blood pressure reductions. In
PMID 23582626

Regulation of podocalyxin expression in the kidney of streptozotocin-induced diabetic rats with Chinese herbs (Yishen capsule).

Fang J, Wei H, Sun Y, Zhang X, Liu W, Chang Q, Wang R, Gong Y.AbstractBACKGROUND: Diabetic nephropathy is an emergent issue in China with increase in patients with type II diabetes. There are several successful Chinese herbal products for the treatment of patients with diabetic nephropathy in China. However, the mechanisms mediating the biological activity of these products are still unclear. Podocalyxin is a sialoprotein critical to maintaining integrity of filtration function of glomerulus.
BMC complementary and alternative medicine.BMC Complement Altern Med.2013 Apr 5;13(1):76. [Epub ahead of print]
BACKGROUND: Diabetic nephropathy is an emergent issue in China with increase in patients with type II diabetes. There are several successful Chinese herbal products for the treatment of patients with diabetic nephropathy in China. However, the mechanisms mediating the biological activity of these pr
PMID 23560927

Capturing the dynamics of systemic Renin-Angiotensin-Aldosterone System (RAAS) peptides heightens the understanding of the effect of benazepril in dogs.

Mochel JP, Peyrou M, Fink M, Strehlau G, Mohamed R, Giraudel JM, Ploeger B, Danhof M.SourceDepartment of Drug Metabolism and Pharmacokinetics, Novartis Campus St. Johann, Basel, Switzerland. jonathan.mochel@novartis.com
Journal of veterinary pharmacology and therapeutics.J Vet Pharmacol Ther.2013 Apr;36(2):174-80. doi: 10.1111/j.1365-2885.2012.01406.x. Epub 2012 May 8.
In dogs, activation of the Renin-Angiotensin-Aldosterone System (RAAS) is an important feature of congestive heart failure (CHF). Long-term increases in angiotensin II (AII) and aldosterone (ALD) lead to the progression of heart failure to its end stage. Angiotensin-converting enzyme inhibitors (ACE
PMID 22568394

Japanese Journal

Simultaneous Determination of Amlodipine Besylate and Benazepril Hydrochloride in Pharmaceutical Dosage Form by LC

Analytical sciences : the international journal of the Japan Society for Analytical Chemistry 25(12), 1495-1498, 2009-12-10
NAID 10026780780

The QUEST Study: 自然発症した粘液腫様変性性僧帽弁閉鎖不全症によるうっ血性心不全の犬におけるピモベンダンまたは塩酸ベナゼプリルの生存期間に及ぼす効果

J-vet 22(1), 36-49, 2009-01
NAID 40016445720

イヌの実験的慢性腎不全モデルにおける高血圧の発現とBenazepril Hydrochlorideの効果(内科学)

The journal of veterinary medical science 70(5), 455-460, 2008-05-25
NAID 110006688949

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★リンクテーブル★

リンク元	「ベナゼプリル」
関連記事	「hydrochloride」

「ベナゼプリル」

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; category	D;
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Pharmacokinetic data
Protein binding	96.7%
Metabolism	Hepatic glucuronidation
Biological half-life	10-11 hours
Excretion	Renal and biliary
Identifiers
CAS Registry Number	86541-75-5
ATC code	C09AA07
PubChem	CID: 5362124
IUPHAR/BPS	6374
DrugBank	DB00542
ChemSpider	4514935
UNII	UDM7Q7QWP8
ChEBI	CHEBI:3011
ChEMBL	CHEMBL838
Chemical data
Formula	C24H28N2O5
Molecular 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: benazepril
化: 塩酸ベナゼプリル、benazepril hydrochloride
商: ベナゼップ、タツジピン、チバセン

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[Hou-1] 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-2] Hitti, Miranda; Chang, Louise (January 11, 2006). "Drug May Treat Advanced Kidney Disease". WebMD. Retrieved 2006-09-07.

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

[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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案内

benazepril hydrochloride