Drug/Small Molecule:

trandolapril

Trandolapril is an ACE inhibitor used to treat high blood pressure, it may also be used to treat other conditions. It is marketed by Abbott Laboratories with the brand name Mavik®.
Trandolapril is a prodrug that is deesterified to trandolaprilat. It is believed to exert its antihypertenive effect through the renin-angiotensin-aldosterone system. (source: Drug Bank)

For the treatment of hypertension. (source: Drug Bank)

The effect of trandolapril in hypertension appears to result primarily from the inhibition of circulating and tissue ACE activity thereby reducing angiotensin II formation, decreasing vasoconstriction, decreasing aldosterone secretion, and increasing plasma renin. Decreased aldosterone secretion leads to diuresis, natriuresis, and a small increase of serum potassium. (source: Drug Bank)

Trandolapril is the ethyl ester prodrug of a nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor, trandolaprilat. Trandolapril is deesterified to the diacid metabolite, trandolaprilat, which is approximately eight times more active as an inhibitor of ACE activity. ACE is a peptidyl dipeptidase that catalyzes the conversion of angiotensin I to the vasoconstrictor, angiotensin II. Angiotensin II is a potent peripheral vasoconstrictor that also stimulates secretion of aldosterone by the adrenal cortex and provides negative feedback for renin secretion. (source: Drug Bank)

Cleavage of the ester group of trandolapril, primarily in the liver, is responsible for conversion to trandolaprilat, the active metabolite. Seven other metabolites, resulting primarily from glucuronidation or de-esterification, have been identified. (source: Drug Bank)

Serum protein binding of trandolapril is about 80% (independent of concentration) while that of trandolaprilat is 65 to 94% (concentration-dependent). (source: Drug Bank)

Absolute bioavailability after oral administration of trandolapril is about 10% as trandolapril and 70% as trandolaprilat. Food slows absorption of trandolapril, but does not affect the area under the plasma concentration–time curve (AUC) or peak plasma concentration (C_max) of trandolaprilat or C_max of trandolapril. (source: Drug Bank)

No data are available with respect to overdosage in humans. The oral LD₅₀ of trandolapril in mice was 4875 mg/Kg in males and 3990 mg/Kg in females. In rats, an oral dose of 5000 mg/Kg caused low mortality (1 male out of 5; 0 females). In dogs, an oral dose of 1000 mg/Kg did not cause mortality and abnormal clinical signs were not observed. In humans the most likely clinical manifestation would be symptoms attributable to severe hypotension. (source: Drug Bank)

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