Zofenopril

From Drugs Prescribing Information
(Redirected from Bifril)
Jump to: navigation, search

Zofenopril (Brand names: Zofenil, Bifril, Zopranol, among others) belongs to a group of blood pressure lowering medicines called angiotensin converting enzyme (ACE) inhibitors.

Zofenopril is used to treat the following conditions:

  • high blood pressure (hypertension).
  • heart attack (acute myocardial infarction) in people who may or may not show signs and symptoms of heart failure, and who have not received treatment that helps dissolve blood clots (thrombolytic therapy).

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Zofenopril.jpg

[edit] MECHANISM OF ACTION

Zofenopril 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.

Zofenopril is a prodrug. Following oral administration, it is bioactivated to Zofenoprilat, which is the active form. Zofenoprilat has a plasma half-life of about 5.5 hours

[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 initiated within the first 24 hours of patients with acute myocardial infarction with or without signs and symptoms of heart failure, who are haemodynamically stable and have not received thrombolytic therapy.

[edit] DOSAGE

  • Hypertension: The recommended initial dose in patients not on diuretics is 15 mg once daily. The dosage should be titrated upwards to achieve optimal blood pressure control. The usual effective dose is 30 mg once daily. The maximum dose is 60 mg per day administered in a single or two divided doses. In case of inadequate response, other antihypertensive agents such as diuretics may be added.
  • Acute myocardial infarction: Zofenopril must be started within 24 hours after the onset of symptoms of acute myocardial infarction and continued for six weeks.
    • 1st and 2nd day: 7.5 mg every 12 hours
    • 3rd and 4th day: 15 mg every 12 hours
    • from 5th day and onwards: 30 mg every 12 hours
      In the event of low systolic blood pressure (< 120mmHg) at the start of treatment or during the first three days following myocardial infarction, the daily dose should not be increased. In the event of hypotension (< 100mmHg), the treatment can be continued with the dose that was previously tolerated. In the event of severe hypotension (systolic blood pressure lower than 90mmHg in two consecutive measurement at least one hour apart),Zofenopril should be discontinued.
      After 6 weeks treatment patients must be re-evaluated and the treatment should be discontinued in patients without signs of left ventricular dysfunction or cardiac failure. If these signs are present, treatment might be continued long term.
      Patients should also receive, as appropriate, the standard treatment such as Nitrates, Aspirin or Beta blockers.

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Zofenopril or to any other ACE inhibitor
  • 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, triamterene, or amiloride) or potassium supplements may have an additive effect on potassium retention, resulting in hyperkalemia.
  • Lithium: Reversible increases in serum lithium concentrations and toxicity have been reported during concomitant administration of lithium carbonate with ACE inhibitors, therefore, Zofenopril is not recommended in association with lithium carbonate

[edit] PREGNANCY AND LACTATION

  • ACE inhibitors should not be initiated during pregnancy. When pregnancy is diagnosed, treatment with ACE inhibitors should be stopped immediately, and, if appropriate, alternative therapy should be started

[edit] SIDE EFFECTS

ACE inhibitors are usually well tolerated. Possible side effects include: Dry irritant cough attributable to accumulation of bradykinin, dizziness, fatigue and headache. GI disturbances include nausea, vomiting, diarrhea, constipation, and dry mouth.

  • First dose hypotension (Rare)
  • 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] BIBLIOGRAPHY

[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)