Drugs Acting on the Renin-Angiotensin-Aldosterone System

Functions of RAAS

1.Regulation of blood pressure, blood volume, and fluid and electrolyte balance
2.Mediates pathophysiologic changes associated with hypertension, heart failure, and myocardial infarction

Formation of Angiotensin II by Renin and Angiotensin-Converting Enzyme (ACE) (Fig 44-1)

1.Renin�Catalyzes formation of angiotensin I from angiotensinogen, which is rate-limiting step of angiotensin II formation
2.Regulation of renin release�Increase due to decrease in BP, blood volume, plasma sodium content, or renal perfusion pressure; decr

Action of Angiotensin II

1. Vasoconstriction�Extremely potent vasoconstrictor; acts directly on vascular smooth muscle especially in arterioles and less in veins, by action in the CNS to increase sympathetic outflow, by increasing release of NE from neurons and by acting on adren

Classes of medication inhibit RAAS function

1. ACE inhibitors
2. Angiotensin receptor blockers
3. Aldosterone antagonists
4. Direct renin inhibitors
5. Beta-blockers

Enalapril (Vasotec) Medication Class

Angiotensin Converting Enzyme Inhibitor; ACE inhibitor

Enalapril (Vasotec) Mechanism of Action

-Inhibit the action of the enzyme ACE resulting in decreased production of angiotensin II (and therefore decreased release of aldosterone). The same enzyme also causes the breakdown of the vasodilator bradykinin. So ACE inhibitors also cause an increase i

Enalapril (Vasotec) Therapeutic Uses

-Enalapril itself is approved for hypertension, heart failure, and asymptomatic left ventricular dysfunction
1.Hypertension
a.Decreases angiotensin II which results in vasodilation
b.Increases bradykinin which results in vasodilation
c.Decreases aldostero

Enalapril (Vasotec) Adverse Effects

1.First-dose hypotension - from vasodilation
2.Cough - Persistent, dry, nonproductive, irritating cough; related to increase in bradykinin
3.Hyperkalemia - Decreased aldosterone action causes potassium retention by kidney
4.Fetal injury - Contraindicated

Enalapril (Vasotec) Precautions, Warnings, and Contraindications

1.Contraindicated during pregnancy.
2.Contraindicated in patients with bilateral renal artery stenosis or stenosis to a single remaining kidney.
3.Contraindicated if patient has had a previous reaction (angioedema) to an ACE inhibitor.
-Use caution in pat

Enalapril (Vasotec) Drug Interactions

Diuretics, antihypertensive agents, drugs that raise potassium levels, lithium, NSAIDs

Enalapril (Vasotec) Pharmacokinetics

Prodrug. Undergoes renal excretion.

Enalapril (Vasotec) Nursing Implications

1.Preadministration Assessment: BP, renal function, volume status, pregnancy status, potassium. Identify patients in which ACE inhibitors would be contraindicated including history of angioedema from ACE inhibitor or bilateral renal artery stenosis. Check

Other drugs that are similar to prototype Enalapril (Vasotec)

1.Benazepril (Lotensin)
2.Captopril (Capoten) - Take at least one hour before meals. Can also cause adverse effects of dysgeusia, rash, and neutropenia.
3.Fosinopril (Monopril)
4.Lisinopril (Prinivil, Zestril)
5.Moexipril (Univasc) - Take at least one hou

Losartan (Cozaar) Medication Class

Angiotensin II Receptor Blocker (ARB)

Losartan (Cozaar) MOA

Blocks action of angiotensin II at receptors in blood vessels, adrenals and all other tissues; does not inhibit kinase II so no increase in bradykinin

Losartan (Cozaar) Uses

-List is for class of ARBs. Losartan itself is approved for use in hypertension, stroke prevention, and diabetic nephropathy.
1. Hypertension - through block of angiotensin II actions; note that there is no increase in vasodilatory bradykinin here though

Losartan (Cozaar) Adverse Effects

1. ARBs do not cause cough because there is no increase in bradykinin.
2. Hyperkalemia
3. Angioedema
4. Fetal harm
5. Renal failure

Losartan (Cozaar) Precautions, Warnings, and Contraindications

1. Contraindicated during pregnancy.
2. Contraindicated in patients with bilateral renal artery stenosis or stenosis to a single remaining kidney.
3. Contraindicated if patients has had a previous reaction (angioedema) to an ARB.
-Use caution in patients

Losartan (Cozaar) Drug Interactions

Diuretics, antihypertensive agents, drugs that raise potassium levels, lithium, NSAIDs

Losartan (Cozaar) Pharmacokinetics

metabolized to active metabolite.

Losartan (Cozaar) Nursing Implications

1.Preadministration Assessment: BP, renal function, potassium, volume status, pregnancy status. Watch for patients in which an ARB would be contraindicated. Check for drug interactions.
2.Administration: Oral
3.Monitoring: BP, renal function, potassium

Other drugs that are similar to prototype Losartan (Cozaar)

1. Candesartan (Atacand)
2. Eprosartan (Teveten)
3. Irbesartan (Avapro)
4. Olmesartan (Benicar)
5. Telmisartan (Micardis)
6. Valsartan (Diovan)
7. Azilsartan (Edarbi)

Eplerenone (Inspra) Medication Class

Aldosterone antagonist

Eplerenone (Inspra) Mechanism of Action

Blocks action of aldosterone in kidney as well as nonrenal sites

Eplerenone (Inspra) Therapeutic Uses

Hypertension and heart failure

Eplerenone (Inspra) Adverse Effects

Hyperkalemia

Eplerenone (Inspra) Precautions, Warnings, and Contraindications

Contraindicated in patients with hyperkalemia, impaired renal function, type 2 diabetes with microalbuminuria.

Eplerenone (Inspra) Drug Interactions

Inhibitors of CYP3A4, drugs that raise potassium levels, potassium supplements, salt substitutes, lithium

Eplerenone (Inspra) Pharmacokinetics

Metabolized by CYP3A4

Eplerenone (Inspra) Nursing Implications

1.Preadministration Assessment: Potassium, renal function. Watch for contraindications and drug interactions.
2.Administration: Oral
3.Monitoring: Potassium, renal function

Other drugs that are similar to prototype Eplerenone (Inspra)

1. Spironolactone (Aldactone) - Also potassium sparing diuretic (Chapter 41)

Aliskiren (Tekturna) Medication Class

Direct renin inhibitor

Aliskiren (Tekturna) Mechanism of Action

Inhibits the conversion of angiotensinogen to angiotensin I by renin

Aliskiren (Tekturna) Therapeutic Uses

Hypertension

Aliskiren (Tekturna)

Angioedemia, hyperkalemia, fetal injury, GI effects

Aliskiren (Tekturna) Precautions, Warnings, and Contraindications

Do not use during pregnancy. Watch renal function and potassium. Do not use in combination with ACE inhibitors or ARBs in diabetic patients.

Aliskiren (Tekturna) Drug Interactions

Drugs that raise potassium levels, antihypertensive agents

Aliskiren (Tekturna) Pharmacokinetics

Eliminated by hepatic metabolism and urinary excretion.

Aliskiren (Tekturna) Nursing Implications

1.Preadministration Assessment: BP, potassium, renal function
2.Administration: Oral
3.Monitoring: BP, potassium renal function