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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/10/25 17:35:23」(JST)

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Perindopril is a long-acting ACE inhibitor. It is used to treat high blood pressure, heart failure or stable coronary artery disease^[1] in form of perindopril arginine (trade names include Coversyl, Coversum) or perindopril erbumine (trade name Aceon). According to the Australian government's Pharmaceutical Benefits Scheme website, based on data provided to the Australian Department of Health and Aging by the manufacturer, perindopril arginine and perindopril erbumine are therapeutically equivalent and may be interchanged without differences in clinical effect.^[2] However the dose prescribed to achieve the same effect will differ due to different molecular weights for the two forms.

Indications

Essential hypertension.
Stable coronary artery disease: reduction of risk of cardiac events in patients with a history of myocardial infarction and/or revascularization.
Treatment of symptomatic heart disease or failure.

Dosage and administration

For Perindopril as treatment for hypertension, the initiation dose is 5 mg perindopril arginine (or 4 mg perindopril erbumine) once daily, then the dose may be increased to 10 mg perindopril arginine (or 8 mg perindopril erbumine) after 1 month of treatment to improve blood pressure control or in case of concomitant stable coronary artery disease.

The Anglo-Scandinavian Cardiac Outcomes Trial showed the benefits of taking the two drugs Coversyl and Amlodipine together. The 9000 British patients aged 40 to 79 were involved in the five-year trial. Half were given the new drug combination, the rest were given traditional drugs. Coversyl and Amlodipine were found to be so effective that the trial was stopped early so that all patients could receive the combination.^[3]^[4]

For stable coronary artery disease

A starting dose of 4 mg for two weeks is recommended, then uptitration to 8 mg once daily, depending on acceptability.

Congestive heart disease

Coversyl (perindopril) should be started under close medical supervision at a starting dose of 2 mg. This may be increased to 4 mg once blood pressure acceptability has been demonstrated.

Elderly patients should start treatment at 2 mg daily (2.5 mg daily of perindopril arginine in Australia).

Contraindications

Children
Pregnancy
Lactation
Situations where a patient has a history of hypersensitivity to Coversyl (perindopril).
Renal failure

Precautions

Assess renal function before and during treatment where appropriate.
Renovascular hypertension.
Surgery/anesthesia.
Renal failure: the dose should be cautiously adjusted in accordance with the creatinine clearance (refer to complete data sheet).
Symptomatic hypotension is rarely seen, but is more likely in volume-depleted patients, those receiving diuretics, or with the first two doses. In diuretic-treated patients, stop the diuretic 3 days before starting Coversyl (perindopril). A diuretic may later be given in combination if necessary; potassium-sparing diuretics are not recommended. Combination with neuroleptics or imipramine-type drugs may increase the hypotensive effect. Serum lithium concentrations may rise during lithium therapy.

Side effects

Rare and mild, usually at the start of treatment.

Cough
fatigue
asthenia
headache
disturbances of mood and/or sleep

Less often

taste impairment
epigastric discomfort
nausea
abdominal pain
rash.

Reversible increases in blood urea and creatinine may be observed. Proteinuria has occurred in some patients. Rarely, angioneurotic edema and decreases in hemoglobin, red cells, and platelets have been reported.

Composition

Each tablet contains 2 mg, 4 mg or 8 mg of the tert-butylamine salt of perindopril. Perindopril is also available under the trade name Coversyl Plus, containing 4 mg of perindopril combined with 1.25 mg indapamide.

In Australia, each tablet contains 2.5 mg, 5 mg or 10 mg of arginine. Perindopril is also available under the trade name Coversyl Plus and Coversyl Plus LD, containing 5 mg of perindopril combined with 1.25 mg indapamide and 2.5 mg of perindopril combined with 0.625 mg indapamide respectively.

The efficacy and tolerability of a fixed-dose combination of Perindopril (ACE Inhibitor) and Amlodipine (a calcium channel antagonist) and is now the world's first flexible dose combination in the class of Perindopril 4mg and Amlodipine 5mg (COVERSYL-AM 4/5), Perindopril 4mg and Amlodipine 10mg (COVERSYL-AM 4/10), Perindopril 8mg and Amlodipine 5mg (COVERSYL-AM 8/5), Perindopril 8mg and Amlodipine 10mg (COVERSYL-AM 8/10), has recently been confirmed in a prospective, observational multicenter trial 1250 hypertensive patients.^[5] A preparation of the two drugs is available commercially as Coveram.

Presentation

Packs of 30 tablets of Coversyl (perindopril) 2 mg. Packs of 30 tablets of Coversyl (perindopril) 5 mg (scored). Packs of 30 tablets of Coversyl (perindopril) 10 mg.

Also available under the brand names:

Aceon
Acertil
Armix
Coverene
Coverex
Coversum
Prestarium
Prexanil
Prexum
Procaptan
Provinace
Covinace

References

Bounhoure JP, Bottineau G, Lechat P, et al.. "Value of perindopril in the treatment of chronic congestive heart failure: multicentre double-blind placebo-controlled study." Clin Exp Hypertens. 1989;A11(suppl 2):575-586.
Lechat P, Granham SP, Desche P, et al.. "Efficacy and acceptability of perindopril in mild-to-moderate chronic congestive heart failure." Am Heart J. 1993;126:798-806.
Morgan T and Anderson A; "Clinical efficacy of perindopril in hypertension." Clin Exp Pharmacol Physiol. 1992;19:61-65.
Myers MG; (on behalf of the perindopril multicentre dose-response study group) "A dose-response study of perindopril in hypertension: effects on blood pressure 6 and 24h after dosing." Can J Cardiol. 1996;12:1191-1196.
"The European trial On reduction of cardiac events with Perindopril in stable coronary Artery disease Investigators. Efficacy of perindopril in reduction of cardiovascular events among patients with stable coronary artery disease: randomized, double-blind, placebo controlled, multicentre trial (the EUROPA study)." The Lancet 2003;362:782-788.

Citations

^ Royal Australian College of General Practitioners. "Consumer Medicine Information, GenRx Perindopril". Clinical Resources, Medicine information for health professionals. http://www.racgp.org.au/cmi/gxcperin.pdf.
^ Australian Government Department of Health and Ageing (2008). "PBS For Health Professionals". Pharmaceutical Benefits Scheme. http://www.pbs.gov.au/html/healthpro/search/results?term=perindopril&scope=PBS+STATIC&form-type=simple. Retrieved 2008-09-04.
^ Charlotte Harding (2005). "What you need to know about the new wonder drug cocktail for high blood pressure...". JADN Repository. http://jadn.co.uk/w/CoversylAmlodipineForHighBloodPressure.htm. Retrieved 2007-07-01.
^ Linda Brookes (2003). "ASCOT: Anglo-Scandinavian Cardiac Outcomes Trial -- Results From The Lipid-Lowering Arm". Medscape Today. http://www.medscape.com/viewarticle/451914. Retrieved 2007-07-01.
^ Bahl VK, Jadhav UM, Thacker HP. Management of Hypertension with the Fixed Combination of Perindopril and Amlodipine in Daily Clinical Practice: Results from the STRONG Prospective, Observational, Multicenter Study. American Journal of Cardiovascular Drugs May 22, 2009; 9 (3): 135-42 Link text

External links

Official homepage

UpToDate Contents

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English Journal

Inadvertent dispensing of Coumadin instead of Coversyl.

Owen AM1, Hungerford SL2.
The Medical journal of Australia.Med J Aust.2014 Mar 3;200(4):204-5.
PMID 24580516

Inadvertent dispensing of Coumadin instead of Coversyl.

Carradice DP1, Maxwell EL2.
The Medical journal of Australia.Med J Aust.2013 Dec 16;199(11):750.
PMID 24329639

Angiotensin-converting enzyme inhibition by perindopril in the treatment of cardiovascular disease.

Brugts JJ1, Ferrari R, Simoons ML.Author information 1Department of Cardiology, Erasmus Medical Centers, Gravendijkwal 230, 3015CE Rotterdam, The Netherlands. j.brugts@erasmusmc.nlErratum inExpert Rev Cardiovasc Ther. 2009 Jun;7(6):722. AbstractThe angiotensin-converting enzyme (ACE) inhibitor perindopril (Coversyl) is a long-acting lipophilic drug with a high-tissue affinity for the ACE. ACE inhibition by perindopril has two main effects: it inhibits the angiotensin II formation and potentiates bradykinin. Perindopril is one of the ACE inhibitors that has been extensively studied in randomized clinical trials within various patient populations. The clinical efficacy has been demonstrated in patients with hypertension, diabetes mellitus, cerebrovascular disease, stable coronary artery disease (CAD) and heart failure. Perindopril has a positive safety and tolerability profile. Therefore, perindopril, as an ACE inhibitor, has an established place in the major clinical treatment guidelines. This article discusses several studies that have shown that an antihypertensive treatment with perindopril reduces and prevents cardiovascular events in a large range of patients with established vascular disease. The observed cardioprotective benefits of perindopril were independent of blood pressure. The outcome of these and other trials support the concept of specific cardioprotective properties of ACE inhibition by perindopril in addition to the blood pressure-lowering effects, such as anti-atherosclerotic, anti-inflammatory and antithrombotic properties. In addition, the observed consistency of the treatment benefit across subgroups indicates that the absolute benefits conferred by treatment are mainly established by each patient's future risk of vascular complications, rather than their initial blood pressure level or other risk factors. This article describes these issues according to the main studies with perindopril or perindopril-based regimens, concluding that the blood pressure-dependent and -independent cardioprotective effects extend to all patients with vascular disease. This concept supports the provision of ACE inhibitor-based treatment, not on the basis of arbitrary cut-off points for blood pressure but rather on assessment of vascular risk, which is raised in patients with stable CAD, diabetes and stroke.
Expert review of cardiovascular therapy.Expert Rev Cardiovasc Ther.2009 Apr;7(4):345-60. doi: 10.1586/erc.09.2.
The angiotensin-converting enzyme (ACE) inhibitor perindopril (Coversyl) is a long-acting lipophilic drug with a high-tissue affinity for the ACE. ACE inhibition by perindopril has two main effects: it inhibits the angiotensin II formation and potentiates bradykinin. Perindopril is one of the ACE in
PMID 19379059

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★リンクテーブル★

リンク元

「ペリンドプリル」

Perindopril
Systematic (IUPAC) name
	(2S,3aS,7aS)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxopentan-2-yl]amino}propanoyl]-octahydro-1H-indole-2-carboxylic acid
Clinical data
Trade names	Coversyl, Coversum, Preterax, Aceon
AHFS/Drugs.com	monograph
MedlinePlus	a602017
Pregnancy cat.	D (US)
Legal status	℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	24%
Protein binding	20%
Metabolism	Renal
Half-life	1–17 hours for perindoprilat (active metabolite)
Identifiers
CAS number	82834-16-0
ATC code	C09AA04; C09BA04 (with diuretics); C09BB04 (with amlodipine)
PubChem	CID 107807
DrugBank	DB00790
ChemSpider	96956
UNII	1964X464OJ
KEGG	D03753
ChEBI	CHEBI:8024
ChEMBL	CHEMBL1581
Chemical data
Formula	C19H32N2O5
Mol. mass	368.468 g/mol
	SMILES O=C(OCC)[C@@H](N[C@H](C(=O)N1[C@H](C(=O)O)C[C@@H]2CCCC[C@H]12)C)CCC;
	InChI InChI=1S/C19H32N2O5/c1-4-8-14(19(25)26-5-2)20-12(3)17(22)21-15-10-7-6-9-13(15)11-16(21)18(23)24/h12-16,20H,4-11H2,1-3H3,(H,23,24)/t12-,13-,14-,15-,16-/m0/s1 ; Key:IPVQLZZIHOAWMC-QXKUPLGCSA-N ;
(what is this?) (verify);

　　[★]

英: perindopril
化: ペリンドプリルエルブミン perindopril erbumine
商: コバシル Coversyl、コバスロー、ペリンシール、ペリンドプリル
関: 降圧薬、アンジオテンシン変換酵素阻害薬 ACE阻害薬

アンギオテンシン変換酵素阻害薬。
プロドラッグ
用量：2-4mg, 極量は8mg 1日1回内服￥

代謝

エステル型プロドラッグである本剤の主要代謝経路は、エチルエステル基が加水分解されて活性代謝物であるペリンドプリラートを生成する経路であった。第2の代謝経路は分子内脱水反応による環状ラクタム体を生成する経路であり、第3の経路はグルクロン酸抱合体であった。

排泄

健康成人にペリンドプリルエルブミン2mg、4mg、8mg、12mgを単回経口投与した場合、投与後24時間までに投与量の21～26％が未変化体、3～10%がペリンドプリラート、12～14%がペリンドプリラートのグルクロン酸抱合体として尿中に排泄された。

[0] Royal Australian College of General Practitioners. "Consumer Medicine Information, GenRx Perindopril". Clinical Resources, Medicine information for health professionals. http://www.racgp.org.au/cmi/gxcperin.pdf.

[1] Australian Government Department of Health and Ageing (2008). "PBS For Health Professionals". Pharmaceutical Benefits Scheme. http://www.pbs.gov.au/html/healthpro/search/results?term=perindopril&scope=PBS+STATIC&form-type=simple. Retrieved 2008-09-04.

[2] Charlotte Harding (2005). "What you need to know about the new wonder drug cocktail for high blood pressure...". JADN Repository. http://jadn.co.uk/w/CoversylAmlodipineForHighBloodPressure.htm. Retrieved 2007-07-01.

[3] Linda Brookes (2003). "ASCOT: Anglo-Scandinavian Cardiac Outcomes Trial -- Results From The Lipid-Lowering Arm". Medscape Today. http://www.medscape.com/viewarticle/451914. Retrieved 2007-07-01.

[test-4] Bahl VK, Jadhav UM, Thacker HP. Management of Hypertension with the Fixed Combination of Perindopril and Amlodipine in Daily Clinical Practice: Results from the STRONG Prospective, Observational, Multicenter Study. American Journal of Cardiovascular Drugs May 22, 2009; 9 (3): 135-42 Link text

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案内

案内

Coversyl