Trandolapril
Brand names,
Trandolapril
Analogs
Trandolapril
Brand Names Mixture
Trandolapril
Chemical_Formula
C24H34N2O5
Trandolapril
RX_link
http://www.rxlist.com/cgi/generic3/mavik.htm
Trandolapril
fda sheet
Trandolapril
msds (material safety sheet)
Trandolapril
Synthesis Reference
No information avaliable
Trandolapril
Molecular Weight
430.537 g/mol
Trandolapril
Melting Point
119-123oC
Trandolapril
H2O Solubility
No information avaliable
Trandolapril
State
Solid
Trandolapril
LogP
3.599
Trandolapril
Dosage Forms
Capsule; Tablets (1 mg, 2 mg, or 4 mg of trandolapril for oral administration)
Trandolapril
Indication
For the treatment of hypertension.
Trandolapril
Pharmacology
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.
Trandolapril
Absorption
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 (Cmax) of trandolaprilat or Cmax of trandolapril.
Trandolapril
side effects and Toxicity
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.
Trandolapril
Patient Information
Trandolapril
Organisms Affected
Humans and other mammals