Perindopril

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Perindopril.jpg

[edit] MECHANISM OF ACTION

Perindopril is an ACE inhibitor. (Angiotensin Converting Enzyme Inhibitor) ACE inhibitors acts by:

  • Inhibiting the formation of angiotensin II from the inactive angiotensin I. Angiotensin II is a potent vasoconstrictor that leads to increased blood pressure.
  • ACE catalyses the breakdown of bradykinin (a powerful vasodilator). Therefore, ACE inhibitors, by inhibiting bradykinin metabolism, increase bradykinin levels, which can contribute to the vasodilator activity
  • Angiotensin II promotes aldosterone release which normally acts to retain sodium and water, therefore ACE inhibitors promote renal excretion of sodium and water (natriuretic and diuretic effects) by blocking angiotensin II stimulation of aldosterone secretion.

Perindopril is a prodrug. Following oral administration, it is bioactivated to Perindoprilat, which is the active form. ì

[edit] INDICATIONS

  • Treatment of hypertension, alone or in combination with other antihypertensive agents, especially thiazide-like diuretics. (ACE inhibitors have an effect on blood pressure that is less in black patients than in non-blacks)
  • Treatment of patients with stable coronary artery disease to reduce the risk of cardiovascular mortality or nonfatal myocardial infarction.

[edit] DOSAGE

  • Hypertension: The recommended initial dose is 4 mg once a day. Dosage should be adjusted according to blood pressure response. The usual maintenance dosage is 4-8 mg administered as a single daily dose or in two divided doses.
  • Stable coronary artery disease: 4 mg once daily for 2 weeks, and then increased as tolerated, to a maintenance dose of 8 mg once daily. In elderly patients (greater than 70 years), Perindopril should be given as a 2 mg dose once daily in the first week, followed by 4 mg once daily in the second week and 8 mg once daily for maintenance dose if tolerated

Perindopril can be taken with or without food.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Perindopril
  • Patients with a history of angioedema related to previous treatment with an angiotensin converting enzyme inhibitor and in patients with hereditary or idiopathic angioedema.
  • Pregnancy and lactation

[edit] PRECAUTIONS

[edit] INTERACTIONS

  • Patients on diuretics may experience an excessive reduction of blood pressure.
  • Caution is advised if non steroidal antiinflammatory drugs NSAIDs are prescribed with ACE inhibitors. (Concomitant use of NSAIDS may result in decreased ACE inhibitor effectiveness). In some patients with compromised renal function who are being treated with NSAIDS, the co-administration of ACE inhibitors may result in further deterioration of renal function. Cases of acute renal failure, usually reversible, have also been reported.
  • Potassium-sparing diuretics may have an additive effect on potassium retention, resulting in hyperkalemia.
  • Lithium toxicity has been reported when used in combination with ACE inhibitors.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category D (US). ACE inhibitors can cause fetal and neonatal morbidity and mortality when administered to pregnant women (espacially in the second and third trimester of pregnancy). When pregnancy is detected, Perindopril should be discontinued as soon as possible.

[edit] SIDE EFFECTS

ACE inhibitors are usually well tolerated. Possible side effects include: Dry irritant cough attributable to accumulation of bradykinin, dizziness, hypotension, back pain, fatigue, headache and skin rashes(rare). GI disturbances include nausea and abdominal pain.

  • Risk of hyperkalaemia due to potassium retention (rarely and especially in patients with renal dysfunction)
  • Angioedema (rare but potentially fatal).

[edit] RELATED LINKS

ACE INHIBITORS: Mechanism of Action, Indications and Side Effects

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)