Acecor: Full Drug Profile

Acecor - General Information

A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat.

Pharmacology of Acecor

Acecor is an angiotensin-converting enzyme (ACE) inhibitor. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II. By blocking ACE, Acecor decreases angiotensin II which is a vasoconstrictor. Acecor is used to treat hypertension and heart failure, to reduce proteinuria and renal disease in patients with nephropathies, and to prevent stroke, myocardial infarction, and cardiac death in high-risk patients. Angiotensin II also stimulates aldosterone secretion by the adrenal cortex.

Acecor for patients

Acecor Interactions

Diuretics: Patients on diuretics, especially those with intravascular volume depletion, may occasionally experience an excessive reduction of blood pressure after initiation of therapy with fosinopril sodium. The possibility of hypotensive effects can be minimized by either discontinuing the diuretic or increasing salt intake prior to initiation of treatment with fosinopril sodium. If this is not possible, the starting dose should be reduced and the patient should be observed closely for several hours following an initial dose and until blood pressure has stabilized (see DOSAGE AND ADMINISTRATION.)

Potassium Supplements and Potassium-Sparing Diuretics: Fosinopril sodium can attenuate potassium loss caused by thiazide diuretics. Potassium-sparing diuretics (spironolactone, amiloride,triamterene, and others) or potassium supplements can increase the risk of hyperkalemia. Therefore, if concomitant use of such agents is indicated, they should be given with caution, and the patient's serum potassium should be monitored frequently.

Lithium: Increased serum lithium levels and symptoms of lithium toxicity have been reported in patients receiving ACE inhibitors during therapy with lithium. These drugs should be coadministered with caution, and frequent monitoring of serum lithium levels is recommended. If a diuretic is also used, the risk of lithium toxicity may be increased.

Antacids: In a clinical pharmacology study, coadministration of an antacid (aluminum hydroxide, magnesium hydroxide, and simethicone) with fosinopril reduced serum levels and urinary excretion of fosinoprilat as compared with fosinopril administered alone, suggesting that antacids may impair absorption of fosinopril. Therefore, if concomitant administration of these agents is indicated, dosing should be separated by 2 hours.

Other: Neither fosinopril sodium nor its metabolites have been found to interact with food. In separate single or multiple dose pharmacokinetic interaction studies with chlorthalidone, nifedipine, propanolol, hydrochlorothiazide, cimetidine, metoclopramide, propantheline, digoxin, and warfarin, the bioavailability of fosinoprilat was not altered by coadministration of fosinopril with any one of these drugs. In a study with concomitant administration of aspirin and fosinopril sodium, the bioavailability of unbound fosinoprilat was not altered.

In a pharmacokinetic interaction study with warfarin, bioavailability parameters, the degree of protein binding, and the anticoagulant effect (measured by prothrombin time) of warfarin were not significantly changed.

Drug/Laboratory Test Interaction

Fosinopril may cause a false low measurement of serum digoxin levels with the Digi- Tab® RIA Kit for Digoxin. Other kits, such as the Coat-A-Count® RIA Kit, may be used.

Acecor Contraindications

Fosinopril sodium is contraindicated in patients who are hypersensitive to this product or to any other angiotensin converting enzyme inhibitor (e.g., a patient who has experienced angioedema with any other ACE inhibitor therapy).

Additional information about Acecor

Acecor Indication

For the treatment of hypertension. It may be used alone or in combination with thiazide diuretics. It is also indicated in the management of heart failure.

Mechanism Of Action

Acecorat, the active metabolite of fosinopril, competes with angiotensin I for binding at the angiotensin-converting enzyme, blocking the conversion of angiotensin I to angiotensin II. Inhibition of ACE results in decreased plasma angiotensin II. As angiotensin II is a vasoconstrictor and a negative-feedback mediator for renin activity, lower concentrations result in a decrease in blood pressure and stimulation of baroreceptor reflex mechanisms, which leads to decreased vasopressor activity and to decreased aldosterone secretion. Acecorat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin.

Drug Interactions

Amiloride Increased risk of hyperkaliemia

Food Interactions

Avoid alcohol.

Generic Name

Fosinopril

Synonyms

Fosinopril Sodium

Drug Category

Antihypertensive Agents; Angiotensin-converting Enzyme Inhibitors

Drug Type

Small Molecule; Approved

Other Brand Names containing Fosinopril

Acecor; Monopril; Secorvas; Staril;

Absorption

Bioavailability is approximately 36% following oral administration.

Toxicity (Overdose)

Human overdoses of fosinopril have not been reported, but the most common manifestation of human fosinopril overdosage is likely to be hypotension. Oral doses of fosinopril at 2600 mg/kg in rats were associated with significant lethality.

Protein Binding

87%

Biotransformation

Since fosinoprilat is not biotransformed after intravenous administration, fosinopril, not fosinoprilat, appears to be the precursor for the glucuronide and p-hydroxy metabolites.

Half Life

12 hours

Dosage Forms of Acecor

Tablet Oral

Chemical IUPAC Name

(2S,4S)-4-cyclohexyl-1-[2-[(2-methyl-1-propanoyloxypropoxy)-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid

Chemical Formula

C30H46NO7P

Fosinopril on Wikipedia

https://en.wikipedia.org/wiki/Fosinopril

Organisms Affected

Humans and other mammals