Quinaprilat: a review of its pharmacokinetics, pharmacodynamics, toxicological data and clinical application.
BACKGROUND
Quinaprilat is an ACE inhibitor for intravenous use especially in patients with arterial hypertension or chronic heart failure. In contrast to the oral prodrug quinapril, it has not been approved for clinical application.


OBJECTIVE
In this review, the pharmacokinetic and pharmacodynamic profile of quinaprilat as well as toxicological data and results of preclinical and clinical studies are summarized.


METHODS
In a PubMed search for the terms "quinaprilat" and "quinapril", literature relevant for this review was selected.


RESULTS
Quinaprilat is a potent nonsulfhydryl selective ACE inhibitor with a short elimination half-life of 2 - 3 h, but due to slow dissociation from tissue ACE, once daily dosing is sufficient for effective ACE inhibition. Quinaprilat is excreted mainly in urine. In long-term animal studies, quinaprilat was not teratogenic, mutagenic or carcinogenic. However, due to the risk of fetal and neonatal morbidity and death, it should not be administrated in pregnancy. Quinaprilat is characterized by an excellent safety profile; adverse events occur infrequently and are rarely serious.


CONCLUSIONS
Quinaprilat is an attractive ACE inhibitor, which potently inhibits tissue ACE.
Kieback
Arne Georg
AG
Universitätsklinikum Greifswald, Klinik für Innere Medizin B, Friedrich-Loeffler-Str. 23a, 17475 Greifswald, Germany. arne.kieback@uni-greifswald.de
Felix
Stephan B
SB
Reffelmann
Thorsten
T
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000818:Animals; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D005260:Female; D006207:Half-Life; D006333:Heart Failure / Q000188:drug therapy / Q000503:physiopathology; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D011247:Pregnancy; D044005:Tetrahydroisoquinolines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*
D000806:Angiotensin-Converting Enzyme Inhibitors; D044005:Tetrahydroisoquinolines; C054501:quinaprilat