ACE Inhibitors and ARBs DSA I

Question 1

ANP

Answer 1

vasodilator - inhibits RAAS

Question 2

renin

Answer 2

released with sympathetic activation of beta-1 receptors on JG cells

Question 3

angiotensinogen

Answer 3

synthesized in liver
> ANG I (renin)

-can be increased in inflammation, corticosteroids, insulin, estrogen, thyroid, ANG II

Question 4

ANG I

Answer 4

> ANG II (ACE)

Question 5

ANG II

Answer 5

activates GPCRs
-rate of synthesis - depends on renin

EFFECTS

• vasoconstriction vas. smooth m
• adrenal - aldosterone
• renin inhibition from kidney (- feedback)
• heart - hypertrophy/remodeling
• brain - baroreceptor to higher set point

Question 6

ACE

Answer 6

activates ANG I > ANG II

inactivates bradykinin > inactive metabolite

Question 7

ANG II receptor

Answer 7

GPCRs - AT1 and AT2

AT1 - major in adults
-PLC > IP3 and DAG > smooth m. contraction

AT2 - bradykinin and NO production (vasodilation)

Question 8

aldosterone

Answer 8

increased reabsorption of Na - DCT and collecting tubules

increased ENaC and Na/K ATPase
-increased Na reabsorption and K secretion

Question 9

ACE inhibitors

Answer 9

inhibit ANG II formation and bradykinin inhibition

-decrease TPR ** (good in physically active patients)

Question 10

BP agents for athletes

Answer 10

ACE inhibitors

Question 11

ACE inhibitor clinical use

Answer 11

HTN, nephropathy, heart failure, left V dysfunction, AMI, prophylaxis of CVD events

Question 12

ACE inhibitor toxicity

Answer 12

hypotension
ARF (renal a stenosis )
hyperkalemia
cough**
angioedema

Question 13

ACE inhibitor contraindication

Answer 13

pregnancy

-fetal hypotension, anuria, renal failure, fetal malformation, tetarogen during first trimester

Question 14

ACE inhibitor drug drug interactions

Answer 14

potassium supps and K sparing diuretics
-hyperkalemia

NSAIDs - block hypertensive effects (bradykinin prostaglandin mediated)

Question 15

ARBs

Answer 15

selective blockade of AT1 receptors

-decreased smooth m contraction

Question 16

AT1 receptors

Answer 16

GPCR > PLC > IP3 and DAG > smooth muscle contraction

Question 17

ARB clinical use

Answer 17

HTN, diabetic nephropathy, HF, left ventricular dysfunction, AMI, prophylaxis for CV events

Question 18

effects of ARBs

Answer 18

(-) of ANG II

• block smooth m contraction
• decreases pressor response
• decreased aldosterone
• changed renal function
• decreased cellular hypertrophy and hyperplasia

Question 19

ACE (-) vs. ARB

Answer 19

ARB - only at AT1 receptors

Question 20

ARB toxicity

Answer 20

• lower cough and angioedema

- not recommended during pregnancy

Question 21

losartan

Answer 21

metabolized by CYP450 to more potent metabolite

Question 22

clonidine

Answer 22

alpha-2 agonist in brainstem - blocks renin secretion

Question 23

propanolol

Answer 23

non-selective beta agonist

• block JG cell beta-1 release of renin
• decrease blood pressure

Question 24

aliskiren

Answer 24

direct renin inhibitor
-decreased ANG I, ANG II, and aldosterone

fetal and neonatal morbidity in pregnancy

use with caution in patients with kidney insufficiency