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Pharmacology -- Test #3 > Targets of Antihypertensive Drugs > Flashcards

Targets of Antihypertensive Drugs Flashcards

1
Q

Significance of the penultimate position proline in angiotensin III

A

Puts a stop to aminopeptidase activity

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2
Q

Full words for AT1 receptor

A

Angiotensin II type I receptor

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3
Q

Three ways that renin release is regulated?

A
  1. NaCl reabs. in macula densa
  2. Blood pressre in preglomerular vessels
  3. Activation of beta-adrenergic receptors on JGCs
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4
Q

What type of receptors are AT1s

A

G protein couples, Gi and Gq (also coupled to phospholipase A2

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5
Q

Where are AT1s located?

A

BV, Brain, Adrenal, Kidney, Heart

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6
Q

Net job of AT1 receptors

A

Increase BP

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7
Q

Three types of reactions of angiotensin II that lower BP?

A

Altered Peripheral Resistance
Altered Renal Function
Altered Cardiovascular Structure.

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8
Q

How does angiotensin II modify peripheral resistance?

A

RAPID PRESSOR RESPONSE
Directed vasoconstriction
Enhancement of NE transmission –> inc sympathetics
Catecholamines from the adrenals

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9
Q

How does angiotensin II modify renal function?

A

SLOW PRESSOR RESPONSE
Increased Na reabsorption
Aldosterone release
Altered hemodynamics (constriction, increased renal symp tone)

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10
Q

How does angiotensin II modify cardiovascular structure?

A

Vascular and Cardiac hypertrophy and remodeling
Increased protooncogenes, growth factors
Increased afterload, increased wall tension

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11
Q

Three types of inhibitors of RAA system

A

Renin Inhibitors
ACE Inhibitors
Ang Receptor Blockers

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12
Q

Three types of ACE inhibitors

A
  1. Sulfhydryl-containing
  2. Dicarboxyl-containing
  3. Phosphorous-containing
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13
Q

Which type of ACE inhibitor is Catopril? What does it do?

A

Sulfhydryl-containing

It binds in the active site of ACE, blocking Ang I

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14
Q

ACE inhibitors will cause an increase in the levels of…

A

BRADYKININ

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15
Q

Captopril. Half life? Side effects?

A

Short – Under 3 hours

SE – Altered metallic taste from thiol, rash

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16
Q

Name two dicarboxyl-containing ACE inhibitors

A

Enalopril, Lisinopril

17
Q

Enalopril important features…

A

Prodrug, long half life

18
Q

What is unique about Moexipril

A

This is the one ACE inhibitor that is cleared hepatically. THe others are kidney cleared.

19
Q

Important details about Lisinopril?

A

Active molecule, not a prodrug
Lysine derivative of enalaprilat
Half life of 12 hours

20
Q

Important example of a phosphinate containing ACE inhibitor?

A

Fosinopril (Monopril)

21
Q

Important details abotu fosinopril?

A

Requires clevage by hepatic esterases
Extensive hepatic metabolism, excreted in urine/bile
Half life 11.5 hrs

22
Q

Clinical uses of ACE inhibitors

A

HTN
LV Systolic Dysfunction
MI
Diabetic Nephropathy

23
Q

Adverse effects of ACE inhibitors?

A

Hypotension, Dry Cough, Hyperkalemia, Acute Renal Failure, Angioedema

24
Q

ACE inhibitor drug-drug interactions?

A

Antacids drop bioavailability
NSAIDS reduce efficacy
K+ supplements can cause hyperkalemia
Can increase plasma levels of digoxin and lithium

25
Q

Contraindications for ACE inhibitors

A

Pregnancy

High doses in paitents with renal insufficiency

26
Q

Whats in the same of all of the Ang Type II receptor antagonists

A

Sartan

27
Q

Actions of AT1 receptor antagonists

A

No effects on bradykinin levels
blocks all ang II activity (pressor effects, etc.)
Uricosuric effect

28
Q

Clinical uses for AT1 receptor antagonists

A

HTN
CHF
Diabetic Nephropathy
Stroke Prophylaxis

29
Q

Adverse effects of AT1 receptor antagonists?

A

Hypotension
Hyperkalemia
Teratogenic Potential

30
Q

Name the renin inhibitor we discussed

A

Aliskiren (Tekturna)

31
Q

Aliskiren SE and Contraindications.

A

SE – Diarrhea

Contra – Pregnancy and Nursing Mothers

Pharmacology -- Test #3 (13 decks)

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