HTN: ACE/ARB

Question 1

What are the two main ACEI?

Answer 1

1. Lisinopril
   - only TRUE QD ACEI (half life = 12hr)**
2. Enalapril
   - only ACEI that can come IV (prodrug = Enalaprilat)**

Question 2

What is the MOA of ACEI?

Answer 2

Inhibit ACE from converted Ang I –> Ang II

result:
VD efferent arteriole (drains glomerular capillary bed) –> dilating efferent arteriole DEC glomerular pressure

Question 3

List the 4 most common uses for ACEI

Answer 3

1. HTN (esp w/LVH)
2. HFrEF (slows cardiac dysfcn)
3. CKD (DM, non-DM) - slows rate of kidney loss
4. Post AMI which resulted in DEC systolic fcn

Question 4

What are 3 pearls of ACEI?

Answer 4

1. Black pt less sensitive to ACEI monotherapy**
2. Synergistic** w/diuretics
3. Renal protectors**
   - no absolute GFR when ACEI cannot be used

Question 5

What are some drug interactions to be aware of with ACEI?

Answer 5

• Lisinopril / enalapril = no CYP interactions
• Anti-HTN & Vasodilators
• Careful w/other meds leading to Hyperkalemia

Question 6

What are the two precautions / C.I. with ACEI?

Answer 6

1. Pt w/hereditary or idiopathic angioedema

2. Bilateral RAS or stenotic lesion to solitary kidney

Question 7

What are the five ADRs involved with ACEI?

Answer 7

1. Teratogen** (C.I. in pregnancy)
2. Cough
   - usually recurs with rechallenge w/same or different ACEI
3. Renal function decline
   - check SCr w/in few wks of starting [up to 30% INC from baseline is acceptable**]
4. Hyperkalemia
5. Angioedema
   - more common in blacks
   - d/t inhibiting breakdown of bradykinin

Question 8

Can you use ARBs in pt w/ACEI-induced angioedema?

Answer 8

• ARB is reasonable if angioedema sxs were MILD (swelling of face or tongue)
• consider another tx if sxs were SEVERE (resp sxs or airway obstruction)

Wait > 4wk after stopping ACEI to start an ARB to make sure angioedema has resolved

Question 9

What are the 3 commonly used ARBs?

Answer 9

Losartan**
Valsartan*
Candesartan

Question 10

What is the ARB MOA?

Answer 10

Interferes w/RAAS by impairing binding of Ang II to AT1 receptors
- blocks vasoconstricting and aldosterone-secreting effects of Ang II

Does not block AT2 receptor which is beneficial –> can lead to additional vasodilation by generation of NO

Question 11

What is the clinical use of ARBs?

Answer 11

Generally the same as ACEI

Most data with losartan > valsartan&raquo_space; others

Question 12

What is the unique clinical use of losartan?

Answer 12

Uricosuric activity and is used for Gout Prevention**

Question 13

What are drug interactions to be aware of with ARBs?

Answer 13

Mostly minimally metabolized
- Losartan is a 2C9 and 3A4 substrate

Other interactions are same as ACEI

Question 14

What are the ARB ADRs?

Answer 14

Same as ACEI without cough and less angioedema risk

Question 15

Olmesartan is an ARB you should not use but he gave a specific ADR, which is…?

Answer 15

Sprue-like enteropathy

• severe chronic diarrhea
• significant wt. loss
• intestinal changes

Question 16

What is the one renin inhibitor? What is its MOA?

Answer 16

Aliskiren

MOA: binds to renin –> inhibits formation of Ang I/II
- inhibits Activation of entire RAAS system

Question 17

What is the clinical use of Aliskiren?

Answer 17

FDA approved for HTN

Almost never a reason to use it**

Question 18

What are two drug interactions to be aware of with Aliskiren?

Answer 18

Pgp inhibitors may INC [aliskiren]

Anti-HTN & Vasodilators

Question 19

Should you combine ACEI, ARB, or Aliskiren in a patient?

Answer 19

No