Sacubitril/valsartan represents the first agent in a new class of drugs developed for heart failure (HF) treatment and termed angiotensin receptor neprilysin (NEP) inhibitors (ARNIs). It is a fixed-dose combination compound containing molecular moieties of valsartan, an angiotensin-type I receptor (AT1)-inhibitor, and the NEP inhibitor sacubitril in a 1:1 molar ratio [1]. Sacubitril is a prodrug that, following oral administration, is rapidly metabolized to the biologically active molecule sacubitrilat. This inhibits the NEP, which is a ubiquitous endopeptidase that is responsible for the breakdown of many vasoactive peptides, including the biologically active natriuretic peptides (NPs), adrenomedullin, substance P, bradykinin, vasoactive intestinal polypeptide, calcitonin gene-related peptide, and enkephalins. Inhibition of NEP increases the levels of these substances, countering the neurohormonal overactivation that contributes to vasoconstriction, sodium retention, and maladaptive...
Mulè, G., Sorce, A., Nardi, E., Geraci, G., Cottone, S. (2019). The nephroprotective effect of sacubitril/valsartan in heart failure: insights from the real-life clinical setting. INTERNAL AND EMERGENCY MEDICINE, 14(8), 1205-1208 [10.1007/s11739-019-02149-6].
The nephroprotective effect of sacubitril/valsartan in heart failure: insights from the real-life clinical setting
Mulè, Giuseppe
Writing – Review & Editing
;Nardi, EmilioVisualization
;Geraci, GiulioVisualization
;Cottone, SantinaSupervision
2019-01-01
Abstract
Sacubitril/valsartan represents the first agent in a new class of drugs developed for heart failure (HF) treatment and termed angiotensin receptor neprilysin (NEP) inhibitors (ARNIs). It is a fixed-dose combination compound containing molecular moieties of valsartan, an angiotensin-type I receptor (AT1)-inhibitor, and the NEP inhibitor sacubitril in a 1:1 molar ratio [1]. Sacubitril is a prodrug that, following oral administration, is rapidly metabolized to the biologically active molecule sacubitrilat. This inhibits the NEP, which is a ubiquitous endopeptidase that is responsible for the breakdown of many vasoactive peptides, including the biologically active natriuretic peptides (NPs), adrenomedullin, substance P, bradykinin, vasoactive intestinal polypeptide, calcitonin gene-related peptide, and enkephalins. Inhibition of NEP increases the levels of these substances, countering the neurohormonal overactivation that contributes to vasoconstriction, sodium retention, and maladaptive...File | Dimensione | Formato | |
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