Fosinopril

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Fosinopril.jpg

[edit] MECHANISM OF ACTION

Fosinopril 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.

Fosinopril is a prodrug. Following oral administration, it is bioactivated to Fosinoprilat, which is the active form. Fosinoprilat half-life is approximately 12 hours.

[edit] INDICATIONS

  • Treatment of hypertension, alone or in combination with thiazide diuretics
  • Management of heart failure

[edit] DOSAGE

  • Hypertension: The recommended initial dose is 10 mg once a day. Dosage should be adjusted according to blood pressure response. The usual dosage range is 10-40 mg/day administered in a single dose or two divided doses. in some patients treated once daily, the antihypertensive effect may diminish toward the end of the dosing interval. In such patients, an increase in dosage or twice daily administration should be considered.
  • Heart failure: The recommended initial dose is 10 mg once a day. Maintenance dose is 20-40 mg once a day. Dosage should be increased, over a several week period, to a dose that is maximal and tolerated but not exceeding 40 mg once a day.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Fosinopril
  • 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 (spironolactone, amiloride, triamterene) 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

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, Fosinopril 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, fatigue, hypotension, headache, blurred vision and weakness. GI disturbances include nausea, vomiting and abnormal taste.

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

[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)