The renin-angiotensin system has been established as an attractive target for pharmacological intervention
since the discovery of first angiotensin-converting enzyme inhibitors (ACE-Is). In fact, these drugs are primarily
used in the management of cardiovascular system-related diseases and renal insufficiency. Their mechanism of
action involves the adjustment of balance between vasoconstrictive, hypertrophic and salt/water-retentive angiotensin
II and vasodilatory and natriuretic bradykinin by the inhibition of angiotensin II biosynthesis and bradykinin
degradation. Currently there are thirteen family members approved for use in humans. They differ in structure,
chemistry and pharmacokinetic and pharmacodynamic properties yet they display a similar pharmacologic and
toxicologic profile. All of them are effective in the treatment of hypertension as well as in cardiac insufficiency or diabetic nephropathy.
Although they are generally well-tolerated several serious side-effects including life-threatening angioedema, renal failure and persistent
dry cough could occur during the administration of ACE-Is, which may require the cessation of therapy. Furthermore, to provide maximum
safety and efficiency of ACE-Is-based therapy, the knowledge of the related drug interactions and chronokinetics seems to be an
absolute requirement. Here we discuss the above-mentioned issues regarding the pharmaceutical and chemical properties of the commercially-
Keywords: Hypertension, pharmacotherapy, interactions, the renin-angiotensin system.
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