Drug/Small Molecule:

fosinopril

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. PubChem (source: Drug Bank)

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. (source: Drug Bank)

Fosinoprilat, 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. Fosinoprilat may also act on kininase II, an enzyme identical to ACE that degrades the vasodilator bradykinin. (source: Drug Bank)

Fosinopril 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, Fosinopril decreases angiotensin II which is a vasoconstrictor. Fosinopril 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. (source: Drug Bank)

Avoid alcohol.
Avoid natural licorice.
Avoid salt substitutes containing potassium.
Do not take calcium, aluminum, magnesium or Iron supplements within 2 hours of taking this medication.
Take without regard to meals. (source: Drug Bank)

Since fosinoprilat is not biotransformed after intravenous administration, fosinopril, not fosinoprilat, appears to be the precursor for the glucuronide and p-hydroxy metabolites. (source: Drug Bank)

87% (source: Drug Bank)

Bioavailability is approximately 36% following oral administration. (source: Drug Bank)

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. (source: Drug Bank)

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