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    Drugs Acting On The Renin-Angiotensin-Aldosterone System

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    Kate Evangelista
    The document discusses drugs that act on the renin-angiotensin-aldosterone system. It describes ACE inhibitors which inhibit the enzyme that converts angiotensin I to angiotensin II, thereby decreasing vasoconstriction and increasing vasodilation. It also discusses angiotensin receptor blockers which block the effects of angiotensin II without affecting bradykinin. Both classes of drugs are useful for treating heart failure, chronic kidney disease, and other conditions by modulating the renin-angiotensin system, though ACE inhibitors can cause cough and angioedema as side effects.

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    Drugs Acting On The Renin-Angiotensin-Aldosterone System

    Uploaded by

    Kate Evangelista
    27 views2 pages
    The document discusses drugs that act on the renin-angiotensin-aldosterone system. It describes ACE inhibitors which inhibit the enzyme that converts angiotensin I to angiotensin II, thereby decreasing vasoconstriction and increasing vasodilation. It also discusses angiotensin receptor blockers which block the effects of angiotensin II without affecting bradykinin. Both classes of drugs are useful for treating heart failure, chronic kidney disease, and other conditions by modulating the renin-angiotensin system, though ACE inhibitors can cause cough and angioedema as side effects.

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    Drugs-acting-on-the-Renin

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    The document discusses drugs that act on the renin-angiotensin-aldosterone system. It describes ACE inhibitors which inhibit the enzyme that converts angiotensin I to angiotensin II, thereby decreasing vasoconstriction and increasing vasodilation. It also discusses angiotensin receptor blockers which block the effects of angiotensin II without affecting bradykinin. Both classes of drugs are useful for treating heart failure, chronic kidney disease, and other conditions by modulating the renin-angiotensin system, though ACE inhibitors can cause cough and angioedema as side effects.

    Copyright:

    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    27 views2 pages

    Drugs Acting On The Renin-Angiotensin-Aldosterone System

    Uploaded by

    Kate Evangelista
    The document discusses drugs that act on the renin-angiotensin-aldosterone system. It describes ACE inhibitors which inhibit the enzyme that converts angiotensin I to angiotensin II, thereby decreasing vasoconstriction and increasing vasodilation. It also discusses angiotensin receptor blockers which block the effects of angiotensin II without affecting bradykinin. Both classes of drugs are useful for treating heart failure, chronic kidney disease, and other conditions by modulating the renin-angiotensin system, though ACE inhibitors can cause cough and angioedema as side effects.

    Copyright:

    © All Rights Reserved
    Download as DOCX, PDF, TXT or read online from Scribd
    Download as docx, pdf, or txt
    of 2

    Drugs acting on the Renin-Angiotensin-

    Aldosterone System
    Renin converts angiotensinogen to angiotensin I. Block by aliskiren blocks the sequence at the
    start. ACE is responsible for activating angiotensionogen I to Angiotensinogen II and for inactivating
    bradykinin, a vasodilator normally present in very low concentrations. Block of the enzyme thus decreases
    the concentration of a vasoconstrictor and increases the concentration of a vasodilator. The AT receptor
    antagonists lack the effect on bradykinin levels, which may explain the lower incidence of cough observed
    with these agents.

    I. ACE Inhibitors

    - inhibit the converting enzyme peptidyl dipeptidase that hydrolyzes angiotensin I to angiotensin II
    and (under the name plasma kininase) inactivates bradykinin, a potent vasodilator, which works at
    least in part by stimulating release of nitric oxide and prostacyclin
    - the hypotensive activity of the ACEIs results both from an inhibitory action on the renin-
    angiotensin system and a stimulating action on the kallikrein-kinin system.

     Enalapril is an oral prodrug that is converted by hydrolysis to a converting enzyme inhibitor,


    enalaprilat, with effects similar to those of captopril. Enalaprilat itself is available only for IV use,
    primarily for hypertensive emergencies.
     Lisinopril is a lysine derivative of enalaprilat
     Benazepril, fosinopril, moexipril, perindopril, quinapril, ramipril, and trandolapril are other long-
    acting members of the class. All are prodrugs like enalapril, and are converted to the active agents
    by hydrolysis, primarily in the liver
     Unlike direct vasodilators, these agents do not result in reflex sympathetic activation and can be
    used safely in persons with ischemic heart disease. The absence of reflex tachycardia may be due
    to downward resetting of the baroreceptors or to enhanced parasympathetic activity

    - ACEIs have a particularly useful role in treating px with chronic kidney disease because they
    diminish proteinuria and stabilize renal function (even in the absence of lowering of BP)
    - This effect is particularly valuable in DM, and these drugs are now recommended in diabetes even
    in the absence of HTN. These benefits probably result from improved intrarenal hemodynamics
    with decreased glomerular capillary pressure
    - ACEIs have also proved to be extremely useful in the Tx of heart failure and after MI, and there is
    recent evidence that ACEIs reduce the incidence of DM in px with high CV risk
    - Cough and angioedema due to bradykinin and substance P
    - Minor toxic effects seen more typically include altered sense of taste, allergic skin rashes, drug
    fever, which may occur in up to 10% of patients

    II. Angiotensin II receptor antagonists

    - Losartan and valsartan were the first marketed blockers of the angiotensin II type (AT1) receptor.
    Candesartan, eprosartan, irbesartan, telmisartan, and olmesartan are also available
    - They have no effect on bradykinin metabolism and are therefore more selective blockers of
    angiotensin effects than ACE inhibitors
    - They also have the potential for more complete inhibition of angiotensin action compared with
    ACEIs because there are enzymes other than ACE that are capable of generating angiotensin II
    - Angiotensin receptor blockers provide benefits similar to those of ACE inhibitors in px with heart
    failure and CKD
    - Cough and angioedema can occur but are uncommon
    - Angiotensin receptor-blocking drugs are most commonly used in px who have had adverse
    reactions to ACEIs
    - Combinations of ACEIs and ARBs or aliskiren, which had once been considered useful for more
    complete inhibition of the renin-angiotensin system, are not recommended due to toxicity
    demonstrated in recent clinical trials
    - Aliskiren causes headache and diarrhea

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