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Pharm Exam 3 > 8 - Antihypertensive Drugs > Flashcards

8 - Antihypertensive Drugs Flashcards

1
Q

Angiotensin affects what things

A

aldosterone and resistance arterioles

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2
Q

Renin inhibitor

A

Aliskiren

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3
Q

ARB’s =

effect?

A

Angiotensin receptor blockers

stop Vasoconstriction and Aldosterone secretion effecs of AT2

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4
Q

Spironolactone and eplerenone direct effects

A

inhibition of aldosterone recepors

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5
Q

Enzyme for AT2→AT3

A

Aminopeptidase

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6
Q

AT3

A

Also biologically active molecule

Promotes aldosterone release

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7
Q

Other routes to angiotensin

A

AP

ACE2

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8
Q

Prorenin

A

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

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9
Q

AT1 receptor function

A

receptor for AT2

???

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10
Q

ATr1 and ATr2 are receptors for

A

AT2 and AT3

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11
Q

Three ways we control renin release

A
  1. NaCl reabsorption at MD
  2. BP in Preglomerular vessels
  3. Activation of B1 adrenergic recepors on Juxtaglomerular cells
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12
Q

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

A

MD senses lower NaCl and increases Renin release

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13
Q

AT1 receptor aka

MOA

A

Angiotensin 2 type 1 receptor

  • GPCR: Gi and Gq
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14
Q

AT1r also couples to

A

phospholipase A2

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15
Q

AT1r is located where

A

BV

brain

adrenal

kidney

heart

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16
Q

Activation of AT1r works to

A

increase BP

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17
Q

Rapid pressor response of angiotensin 2 from

A

altered peripheral resistance

(direct vasoconstric, increased NE, increased sy discharge)

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18
Q

SLow pressor response of Angiotensin 2

A

from altered renal function

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

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19
Q

Vascular and cardiac effects of AT2

A

Vascular and Cardiac hypertrophy and remodeling

20
Q

Mechanisms that lead to CV hypertroph. and remodeling

A
  1. Nonhemodynnamic = increased proto-oncogene, GF’s, and ECF synthesis
  2. Hemodynamic = Increased afterload, wall tension
21
Q

Three classes that acct in RAAS inhibition

A

Direct renin inhibitors

Ace inhibitors

Ang. receptor blockers

22
Q

ACE inhibitor general classes

A

Sulfhydryl-containing

Dicarboxyl-containing

Phosphorous-containing

23
Q

All of the ACE inhibitors are

A

competitive inhibitors

24
Q

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

A

breakdown of bradykinin

builds up and promotes vasodilation

25
Q

____ will reduce the effectiveness of the ACE inhibitors

A

NSAIDs

Because it takes out the vasodilating arm (bradykinin)

26
Q

Captopril is a

A

active site inhibitor

Short half life

absorption reduced by food

27
Q

AE’s for captopril

A

ALtered taste and rash

28
Q

Hepatic-metabolized ACE inhibitor

A

Moexipril

(preferred for patients with renal failure)

29
Q

Enalopril is a ____

Half life

Admistration

A
  • Dicarboxyl-containing group Prodrug (needs hydrolysis of ethyl ester to form diacid form Enalaprilat)
  • 11 hours
  • Parenteral = enaliprilat
30
Q

Lisinopril is a _

A

Dicarboxyl-containing ACE inhibitor

(Lysine derivaive of enalaprilat)

Active molecule

31
Q

Fosinopril is what group/type of drug?

Metabolism

A

Phosphinate-containing ACEinh. , Prodrug of Fosinoprilat

Exttensive hepatic metabolism with excretion in urine and bile

32
Q

Clinical use of ACEi

A

HTN

LV systolic dysfunciton

Myocardial infarction

Diabetic nephropathy

33
Q

AE’s of ACEi’s

A

Hypotension

Dry cough

Hyperkalemia

ARF

Skin rash (captopril)

Angioedema

34
Q

AE that is also due to bradykinin effect of ACE inhibitors

A

Angioedema

35
Q

DDIs for ACEi

A

Antacids (reduce BA)

NSAIDs

K supps

Digoxin/lithium need to be monitored

36
Q

CI’s for ACEi

A

Pregnancy (teratogen)

Renal insufficiency may lead to neutropenia

37
Q

Angiotensin 2 Type 1 Receptor Antagonists

(AT1r)

A

(Sartans)

Losartan, Valsartan, etc.

38
Q

AT1r have no effect on

A

bradykinin system

39
Q

AT2T1 receptor antagonists selectively block

A

effects of Angiotensin 2

  • Pressor
  • NE stim
  • aldosterone secretion
  • Effects on renal vasculature
  • Growth promoting effects on cardiac and vascuar tissue
40
Q

AT2T1 receptor antagonists also have

A

Uricosuric effect

41
Q

AT2T1 receptor antagonists Clinical use

A

HTN

CHF

Diabetic nephropathy

Stroke prophylaxis

42
Q

AT2T1 receptor antag. AE’s

A

HoTN

Hyperkalemia

Teratogenic potential (2nd and 3rd trimester)

43
Q

Renin inhibitors drug name and MOA

A

Aliskiren

  • Direct inhibition of renin
  • Dipeptide-like mimetic
44
Q

Aliskiren used ____ or ____.

A

alone or in combo to treat HTN

45
Q

Contraindicated in pregnancy and nursing mothers

46
Q

Main AE of aliskiren

Pharm Exam 3 (11 decks)

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