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Perindopril is a long-acting ACE inhibitor 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 (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 differs due to different molecular weights for the two forms.

Medical uses

Perindopril shares the indications of ACE inhibitors as a class, including essential hypertension, stable coronary artery disease (reduction of risk of cardiac events in patients with a history of myocardial infarction and/or revascularization) and treatment of symptomatic heart disease or failure. In addition, the Perindopril pROtection aGainst REcurrent Stroke Study (PROGRESS) found that perindopril reduces the risk of stroke in both hypertensive and nonhypertensive individuals with a history of stroke or transient ischemic attack.^[3]

Dosage and administration

For perindopril as treatment for hypertension, the initial 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 one 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 perindopril and amlodipine together. About 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. Perindopril and amlodipine were found to be so effective, the trial was stopped early so all patients could receive the combination.^[4]^[5]

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.

For 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).

For secondary prevention of stroke

The PROGRESS study recommends a dose of 4 mg daily, optionally supplemented by 2.5 mg-daily indapamide. The reduction of stroke risk seems to be stronger with a combination of the two drugs.^[3]

Contraindications

Children
Pregnancy
Lactation
Situations where a patient has a history of hypersensitivity
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 three days before starting 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

Side effects are mild, usually at the start of treatment; they include:

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, 4, 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, 5, or 10 mg of perindopril arginine. Perindopril is also available under the trade name Coversyl Plus, containing 5 mg of perindopril arginine combined with 1.25 mg indapamide and Coversyl Plus LD, containing 2.5 mg of perindopril arginine combined with 0.625 mg indapamide.

The efficacy and tolerability of a fixed-dose combination of 4 mg perindopril and 5 mg amlodipine, a calcium channel antagonist, has been confirmed in a prospective, observational multicenter trial of 1,250 hypertensive patients.^[6] A preparation of the two drugs is available commercially as Coveram.

Also, it is available under the brand names:

Aceon
Acertil
Actiprex
Armix
Coverene
Coverex
Coversum
Perineva
Prenessa
Prestarium
Prexanil
Prexum
Procaptan
Provinace
Covinace
Pericard
Percarnil

References

^ Royal Australian College of General Practitioners. "Consumer Medicine Information, GenRx Perindopril" (PDF). Clinical Resources, Medicine information for health professionals.
^ Australian Government Department of Health and Ageing (2008). "PBS For Health Professionals". Pharmaceutical Benefits Scheme. Retrieved 2008-09-04.
^ ^a ^b PROGRESS Collaborative Group. "Randomised trial of a perindopril-based blood-pressure-lowering regimen among 6,105 individuals with previous stroke or transient ischaemic attack". The Lancet. 2001 Sep 29; 358 (9287): 1033–1041. doi:10.1016/s0140-6736(01)06178-5. PMID 11589932.
^ Charlotte Harding (2005). "What you need to know about the new wonder drug cocktail for high blood pressure...". JADN Repository. Retrieved 2007-07-01.
^ Linda Brookes (2003). "ASCOT: Anglo-Scandinavian Cardiac Outcomes Trial -- Results From The Lipid-Lowering Arm". Medscape Today. 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 website

UpToDate Contents

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1. 糖尿病患者における高血圧治療 treatment of hypertension in patients with diabetes mellitus
2. 再発性脳卒中または一過性脳虚血発作の予防のための降圧療法 antihypertensive therapy to prevent recurrent stroke or transient ischemic attack
3. Goal blood pressure in patients with cardiovascular disease or at high risk
4. 心房細動患者における脳卒中 stroke in patients with atrial fibrillation
5. 脈圧の上昇 increased pulse pressure

English Journal

Novel ratio difference at coabsorptive point spectrophotometric method for determination of components with wide variation in their absorptivities.

Saad AS1, Abo-Talib NF2, El-Ghobashy MR3.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy.Spectrochim Acta A Mol Biomol Spectrosc.2016 Jan 5;152:480-4. doi: 10.1016/j.saa.2015.07.099. Epub 2015 Jul 29.
Different methods have been introduced to enhance selectivity of UV-spectrophotometry thus enabling accurate determination of co-formulated components, however mixtures whose components exhibit wide variation in absorptivities has been an obstacle against application of UV-spectrophotometry. The dev
PMID 26253440

Drug updates and approvals: 2015 in review.

Klibanov OM1, Phan D, Ferguson K.
The Nurse practitioner.Nurse Pract.2015 Dec 12;40(12):34-43. doi: 10.1097/01.NPR.0000473071.26873.3c.
This article highlights important prescribing information for some drugs that received FDA approval within the past year. These include: atazanavir and cobicistat (Evotaz®), ceftazidime and avibactam (Avycaz®), edoxaban (Savaysa®), ivabradine (Corlanor®), liraglutide (rDNA origin) injection (Sax
PMID 26545091

CAC score as a possible criterion for administration of angiotensin converting enzyme inhibitors and/or angiotensin receptor blockers: the MultiEthnic Study of Atherosclerosis.

Darabian S1, Luo Y, Homat A, Khosraviani K, Wong N, Zeb I, Nasir K, Budoff MJ.
Coronary artery disease.Coron Artery Dis.2015 Dec;26(8):678-85. doi: 10.1097/MCA.0000000000000303.
INTRODUCTION: Several trials have demonstrated that angiotensin converting enzyme inhibitors (ACEIs) decrease cardiovascular (CV) mortality rates in patients with heart failure; however, the Prevention of Events with Angiotensin-Converting Enzyme Inhibition (PEACE) and European Trial on Reduction of
PMID 26398149

Japanese Journal

Combination of an ACE Inhibitor and Indapamide Improves Blood Pressure Control, but Attenuates the Beneficial Effects of ACE Inhibition on Plasma Adiponectin in Patients With Essential Hypertension

HUANG Shao-Sung,WU Tao-Cheng,LIN Shing-Jong,CHEN Jaw-Wen
Circulation journal : official journal of the Japanese Circulation Society 73(12), 2282-2287, 2009-11-20
… After a 2-week placebo run-in phase, 30 patients with essential hypertension were randomized to receive preterax (2 mg perindopril/0.625 mg indapamide) or cilazapril (2.5 mg) once daily for 12 weeks. …
NAID 10025938377

Effects of ARB or ACE-Inhibitor Administration on Plasma Levels of Aldosterone and Adiponectin in Hypertension

Nakamura Tetsuya,Kawachi Kenji,Saito Yuichiro,Saito Tomoko,Morishita Koujurou,Hoshino Jin,Hosoi Tsutomu,Iwasaki Tsutomu,Ohyama Yoshio,Kurabayashi Masahiko
International Heart Journal 50(4), 501-512, 2009
… Thus, we investigated the effect of the ACE-I perindopril erbumin (perindopril) and the ARB telmisartan on plasma levels of aldosterone and adiponectin.Patients with essential hypertension were randomly assigned to receive 48 weeks of perindopril (2-8 mg/d) or telmisartan (20-80 mg/d). … Data on 51 subjects (25 in the perindopril group and 26 in the telmisartan group; …
NAID 130000120833

主要薬剤の大規模臨床試験 PROGRESS (大規模臨床試験--循環・代謝系を中心に) -- (脳血管障害)

尾前照雄
日本臨床 66(-) (945), 500-504, 2008-10-00
NAID 40016297645

Related Pictures

★リンクテーブル★

リンク元	「アンジオテンシン変換酵素阻害薬」「ペリンドプリル」
拡張検索	「perindopril erbumine」

「アンジオテンシン変換酵素阻害薬」

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	US: D Evidence of risk; ;
Administration	Oral
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	24%
Protein binding	20%
Metabolism	Renal
Biological half-life	1–17 hours for perindoprilat (active metabolite)
Identifiers
CASRN	82834-16-0
ATC code	C09AA04 (WHO); C09BA04 (WHO) (with diuretics); C09BB04 (WHO) (with amlodipine)
PubChem	CID 107807
IUPHAR/BPS	6367
DrugBank	DB00790
ChemSpider	96956
UNII	1964X464OJ
KEGG	D03753
ChEBI	CHEBI:8024
ChEMBL	CHEMBL1581
Chemical data
Formula	C19H32N2O5
Molar 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 ;
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英: angiotensin-converting enzyme inhibitor angiotensin converting enzyme inhibitor , ACE inhibitor, ACEI
同: アンジオテンシン変換酵素阻害剤アンギオテンシン変換酵素阻害薬アンギオテンシン変換酵素阻害剤アンジオテンシン転換酵素阻害薬、ACE阻害薬 ACE阻害剤 ACE inhibitor、アンギオテンシン変換酵素拮抗薬, アンギオテンシン変換酵素拮抗薬, angiotensin-converting enzyme antagonist
関: アンジオテンシン, アンジオテンシン転換酵素 ACE, 1型アンジオテンシンII受容体拮抗薬アンジオテンシンII受容体拮抗薬 ARB