Trandolapril
Trandolapril. ACE inhibitor prodrug — converted to trandolaprilat. Long half-life supports once-daily dosing. Used in hypertension + post-MI… Oral half-life 0.7 h.
ACE inhibitor prodrug — converted to trandolaprilat. Long half-life supports once-daily dosing. Used in hypertension + post-MI heart failure.
PK: A THIRTY-THREE-FOLD ERROR WITH THE CORRECT NUMBER SITTING IN THE RECORD OWN CITATION. The stored 24 h is the ACTIVE DIACID accumulation half-life, taken from a review, while the cited paper states plainly "Trandolapril is rapidly absorbed, with a single elimination half-life (t1/2) of 0.72 h, irrespective of dose" — for trandolapril itself, the molecule the stored mass of 430.54 names. Trandolaprilat is 402.49, an ester factor of 1.070. The same paper explains the class behaviour: exposure to the diacid "increased with increasing doses but in a nonlinear fashion, probably owing to saturable plasma ACE binding", becoming linear only at the highest doses where the enzyme sink saturates — so any long half-life read from low-dose data is a binding phase. Effect persists far beyond the curve: significant blood-pressure reduction lasts 48 h after the last dose and residual enzyme inhibition is near 60% at 24 h. ka 2.5 and V 18 L dropped as unsourced.
Pharmacokinetics
- Oral — t½ 43 min · F 11%
Sources: PMID:7527100, PMID:8480624