8 - Antihypertensive Drugs

Question 1

Angiotensin affects what things

Answer 1

aldosterone and resistance arterioles

Question 2

Renin inhibitor

Answer 2

Aliskiren

Question 3

ARB’s =

effect?

Answer 3

Angiotensin receptor blockers

stop Vasoconstriction and Aldosterone secretion effecs of AT2

Question 4

Spironolactone and eplerenone direct effects

Answer 4

inhibition of aldosterone recepors

Question 5

Enzyme for AT2→AT3

Answer 5

Aminopeptidase

Question 6

AT3

Answer 6

Also biologically active molecule

Promotes aldosterone release

Question 7

Other routes to angiotensin

Answer 7

AP

ACE2

Question 8

Prorenin

Answer 8

Has a recepor of its own

Bound to its receptor = helps regulate the whole angiotensin system, as well as playing a role in cardio disease, brain development

Question 9

AT1 receptor function

Answer 9

receptor for AT2

???

Question 10

ATr1 and ATr2 are receptors for

Answer 10

AT2 and AT3

Question 11

Three ways we control renin release

Answer 11

1. NaCl reabsorption at MD
2. BP in Preglomerular vessels
3. Activation of B1 adrenergic recepors on Juxtaglomerular cells

Question 12

If blood pressure drops, less sodium sent to tubule, what happens

Answer 12

MD senses lower NaCl and increases Renin release

Question 13

AT1 receptor aka

MOA

Answer 13

Angiotensin 2 type 1 receptor

• GPCR: Gi and Gq

Question 14

AT1r also couples to

Answer 14

phospholipase A2

Question 15

AT1r is located where

Answer 15

BV

brain

adrenal

kidney

heart

Question 16

Activation of AT1r works to

Answer 16

increase BP

Question 17

Rapid pressor response of angiotensin 2 from

Answer 17

altered peripheral resistance

(direct vasoconstric, increased NE, increased sy discharge)

Question 18

SLow pressor response of Angiotensin 2

Answer 18

from altered renal function

(sodium and water retention, direct renal vasoconstriction, increased NE in kidney)

Question 19

Vascular and cardiac effects of AT2

Answer 19

Vascular and Cardiac hypertrophy and remodeling

Question 20

Mechanisms that lead to CV hypertroph. and remodeling

Answer 20

1. Nonhemodynnamic = increased proto-oncogene, GF’s, and ECF synthesis
2. Hemodynamic = Increased afterload, wall tension

Question 21

Three classes that acct in RAAS inhibition

Answer 21

Direct renin inhibitors

Ace inhibitors

Ang. receptor blockers

Question 22

ACE inhibitor general classes

Answer 22

Sulfhydryl-containing

Dicarboxyl-containing

Phosphorous-containing

Question 23

All of the ACE inhibitors are

Answer 23

competitive inhibitors

Question 24

ACEi prevents _____ in the other “arm” of the pathway

Answer 24

breakdown of bradykinin

builds up and promotes vasodilation

Question 25

\_\_\_\_ will reduce the effectiveness of the ACE inhibitors

Answer 25

NSAIDs Because it takes out the vasodilating arm (bradykinin)

Question 26

Captopril is a

Answer 26

active site inhibitor Short half life absorption reduced by food

Question 27

AE's for captopril

Answer 27

ALtered taste and rash

Question 28

Hepatic-metabolized ACE inhibitor

Answer 28

Moexipril (preferred for patients with renal failure)

Question 29

Enalopril is a \_\_\_\_ Half life Admistration

Answer 29

* Dicarboxyl-containing group **_Prodrug_** (needs hydrolysis of ethyl ester to form diacid form Enalaprilat) * 11 hours * Parenteral = enaliprilat

Question 30

Lisinopril is a \_

Answer 30

Dicarboxyl-containing ACE inhibitor *(Lysine derivaive of enalaprilat)* Active molecule

Question 31

Fosinopril is what group/type of drug? Metabolism

Answer 31

Phosphinate-containing ACEinh. , Prodrug of Fosinoprilat Exttensive hepatic metabolism with excretion in urine and bile

Question 32

Clinical use of ACEi

Answer 32

HTN LV systolic dysfunciton Myocardial infarction Diabetic nephropathy

Question 33

AE's of ACEi's

Answer 33

Hypotension **_Dry cough_** Hyperkalemia ARF Skin rash (captopril) Angioedema

Question 34

AE that is also due to bradykinin effect of ACE inhibitors

Answer 34

Angioedema

Question 35

DDIs for ACEi

Answer 35

Antacids (reduce BA) NSAIDs K supps Digoxin/lithium need to be monitored

Question 36

CI's for ACEi

Answer 36

Pregnancy (teratogen) Renal insufficiency may lead to neutropenia

Question 37

Angiotensin 2 Type 1 Receptor Antagonists (AT1r)

Answer 37

(Sartans) Losartan, Valsartan, etc.

Question 38

AT1r have no effect on

Answer 38

bradykinin system

Question 39

AT2T1 receptor antagonists selectively block

Answer 39

effects of Angiotensin 2 * Pressor * NE stim * aldosterone secretion * Effects on renal vasculature * Growth promoting effects on cardiac and vascuar tissue

Question 40

AT2T1 receptor antagonists also have

Answer 40

Uricosuric effect

Question 41

AT2T1 receptor antagonists Clinical use

Answer 41

HTN CHF Diabetic nephropathy Stroke prophylaxis

Question 42

AT2T1 receptor antag. AE's

Answer 42

HoTN Hyperkalemia Teratogenic potential (2nd and 3rd trimester)

Question 43

Renin inhibitors drug name and MOA

Answer 43

Aliskiren * Direct inhibition of renin * Dipeptide-like mimetic

Question 44

Aliskiren used ____ or \_\_\_\_.

Answer 44

alone or in combo to treat HTN

Question 45

Contraindicated in pregnancy and nursing mothers

Answer 45

aliskiren

Question 46

Main AE of aliskiren

Answer 46

Diarrhea