Perindopril

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Drug Info:

Perindopril

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Brand names: Aceon®

Chemical formula:



Perindopril tablets

What are perindopril tablets?

PERINDOPRIL (Aceon®) is a medication which lowers blood pressure by relaxing blood vessels; it is not a cure. High blood pressure levels can damage your kidneys, and may lead to a stroke or heart failure. Generic perindopril tablets are not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• autoimmune disease (such as lupus), or suppressed immune function
• previous swelling of the tongue, face, or lips with difficulty breathing, difficulty swallowing, hoarseness, or tightening of the throat (angioedema)
• bone marrow disease
• diabetes
• heart or blood vessel disease
• low blood pressure
• kidney disease
• if you are on a special diet, such as a low-salt diet
• an unusual or allergic reaction to perindopril, other ACE inhibitors, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I take this medicine?

Take perindopril tablets by mouth one hour before meals. Follow the directions on the prescription label. Swallow the tablets with a drink of water. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking perindopril except on your prescriber's advice.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What if I miss a dose?

If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. If you take only one dose a day and forget to take it that day, do not take a double dose the next day.

What drug(s) may interact with perindopril?

• antiinflammatory drugs (NSAIDs, such as ibuprofen)
• gold compounds, often used for arthritis
• hawthorn
heparin
lithium
• medicines for diabetes
• medicines for high blood pressure
• monoamine oxidase inhibitors (Azilect®, Eldepryl®, Emsam®, Marplan®, Nardil®, Parnate®, Zelapar™)
• potassium salts
• water pills

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking perindopril?

Visit your prescriber or health care professional for regular checks on your progress. Check your blood pressure regularly while you are taking perindopril. Ask your prescriber or health care professional what your blood pressure should be and when you should contact him or her. Stop taking perindopril and call your prescriber or health care professional if you have difficulty breathing, or notice any swelling of the lips, tongue or face.

Check with your prescriber or health care professional if you get an attack of severe diarrhea, nausea and vomiting, or if you sweat a lot. The loss of body fluid can make it dangerous to take perindopril.

You may get dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how perindopril affects you. To avoid dizzy or fainting spells, do not stand or sit up quickly, especially if you are an older person. Alcohol can make you more dizzy. Avoid alcoholic drinks.

If you are going to have surgery, tell your prescriber or health care professional that you are taking perindopril.

Avoid salt substitutes or other foods or substances high in potassium salts.

Do not treat yourself for cough, sore throat, colds, or pain while you are using perindopril without asking your prescriber or health care professional for advice.

Women should inform their doctor if they wish to become pregnant or think they might be pregnant. There is a potential for serious side effects to an unborn child. Talk to your health care professional or pharmacist for more information.

What side effects may I notice from taking perindopril?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• decreased amount of urine passed
• difficulty breathing, or difficulty swallowing
• dizziness, lightheadedness or fainting spells
• fast or uneven heart beat, palpitations, or chest pain
• fever or chills
• numbness or tingling in your fingers or toes
• skin rash, itching
• swelling of your face, lips, or tongue
• sore throat

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• cough
• headache
• tiredness

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Protect from moisture. Keep container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.


An angiotensin-converting enzyme inhibitor used as an adjunct to diuretics for the treatment of heart failure and to prevent further heart damage after a heart attack; it is also licensed for use in the treatment of hypertension. It is available as tablets in two forms, perindopril erbumine and perindopril arginine, on prescription only.

Side effects, precautions, and interactions with other drugs:
see angiotensin-converting enzyme inhibitors.

Proprietary preparations:
Coversyl Arginine; Coversyl Arginine Plus (combined with indapamide).

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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 Aceon
AHFS/Drugs.com monograph
MedlinePlus a602017
Pregnancy cat. D
Legal status  ?
Routes oral
Pharmacokinetic data
Bioavailability 24%
Protein binding 20%
Metabolism Renal
Half-life 1 hour - 17 hours for perindoprilat (active metabolite)
Identifiers
CAS number 82834-16-0 N
ATC code C09AA04
C09BA04 (with diuretics)
C09BB04 (with amlodipine)
PubChem CID 107807
DrugBank DB00790
ChemSpider 96956 YesY
UNII 1964X464OJ N
KEGG D03753 YesY
ChEBI CHEBI:8024 YesY
ChEMBL CHEMBL1581 YesY
Chemical data
Formula C19H32N2O5 
Mol. mass 368.468 g/mol
SMILES eMolecules & PubChem
 N (what is this?)  (verify)

Perindopril, or perindopril arginine, (trade names include Coversyl and Aceon) is a long-acting ACE inhibitor. Perindopril is used to treat high blood pressure, heart failure or stable coronary artery disease.[1] It is also available in a generic form, perindopril erbumine. 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.

Contents

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 2 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 (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 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

  1. ^ 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. 
  2. ^ 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. 
  3. ^ 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. 
  4. ^ 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. 
  5. ^ 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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