Angiotensin-converting enzyme inhibitors fosinopril

As angiotensin-converting enzyme inhibitors influence protein excretion in renal disease, Gansevoort et al. (G2) and Keilani et al. (K10) investigated serum Lp(a) concentrations in patients treated with Lisinopril resp. fosinopril and detected a reduction. 

K10. Keilani, T., Schlueter, A., Levin, M. L., and Battle, D. C., Improvement of lipid abnormalities associated with proteinuria using fosinopril, an angiotensin-converting enzyme inhibitor. Ann. Intern. Med. 118, 246-254 (1994). 

Fosinopril sodium, an angiotensin-converting enzyme inhibitor, has been found to exist in two anhydrous polymorphic forms. No single crystal of sufficiently high crystallographic quality was obtained for the polymorphic phases and polymorphism was characterized by solid state and P NMR. The analysis of chemical shifts in C spectra suggested that polymorphism originates from conformational differences in the acetal side chains and/or cis-trans isomerization about the peptide C-N bond. The difference in chemical shift between P resonances in the two spectra is 2.2 ppm and demonstrates the existence of various envirorunents of phosphorus nuclei in each polymorph [43]. 

Enalaprilat and SQ27,519 are angiotensin-converting enzyme (ACE) inhibitors with poor oral absorption. Enalapril and fosinopril are dipeptide and amino acid derivatives of enalaprilat and SQ27,519, respectively [51] (Fig. 10). Both prodrugs are converted via deesterification to the active drug by hepatic biotransformation. In situ rat perfusion of enalapril indicated a nonpassive absorption mechanism via the small peptide carrier-mediated transport system. In contrast to the active parent, enalapril renders enalaprilat more peptide-like, with higher apparent affinity for the peptide carrier. The absorption of fosinopril was predominantly passive. Carrier-mediated transport was not demonstrated, but neither was its existence ruled out. 

DI Friedman, GL Amidon. Passive and carrier-mediated intestinal absorption components of two angiotensin converting enzyme (ACE) inhibitor prodrugs in rats Enalapril and fosinopril. Pharm Res 6(12) 1043-1047, 1989. 

Angiotensin converting ENZYME (ACE) inhibitors captopril cilazapril enalapril maleate fosinopril sodium lisinopril... 

Angiotensin-converting enzyme (ACE) inhibitors, such as benazepril (Lotensin), enalapril (Vasotec), fosinopril (Monopril), lisinopril (Prinivil, Zestril), quinapril (Accupril), and ramipril (Altace). 

Vcp couplings have been determined by Liu et for two conformers of fosinopril sodium, the only angiotensin-converting enzyme (ACE) inhibitor that depends on a phosphinyl group to inhibit ACE by a zinc ligand relationship. 

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