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Pharmacology Test #3 > Targets for Antihypertensive Drugs > Flashcards

Targets for Antihypertensive Drugs Flashcards

(48 cards)

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1
Q

What does renin do?

A

cleaves angiotensinogen to angiotensin I

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2
Q

What does kallikrein do?

A

cleaves kininogen to bradykinin

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3
Q

What does angiotensin-converting enzyme do?

A

converts angiotensin I to angiotensin II and inactives bradykinin

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4
Q

What does bradykinin do in the body?

A

vasodilation, decreased peripheral vascular resistance, decreased blood pressure

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5
Q

What does angiotensin II do in the body?

A

vasoconstriction -> increased peripheral vascular resistance
aldosterone secretion -> increased sodium and water retension
INCREASES BLOOD PRESSURE

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6
Q

What does aminopeptidase do?

A

converts angiotensin II to angiotensin III

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7
Q

What does angiotensinases do?

A

breaks down angiotensin III

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8
Q

What does prorenin do besides act as a precursor for renin?

A

prorenin has a receptor itself and its activity regulates the renin-angiotensin system and plays a role in other stuff

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9
Q

Primary biologically active molecule in the renin-angiotensin system?

A

angiotensin II

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10
Q

Name the three pathways that control renin release.

A
  1. NaCl reabsorption at macula dense
  2. blood pressure in pre-glomerular vessels
  3. activation of beta1 adrenergic receptors on JGCs
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11
Q

Angiotensin II Type 1 (AT1) receptors

A

G-protein coupled; Gi and Gq

also couples to phospholipase A2

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12
Q

Where are AT1 receptors located?

A

blood vessels, brain, adrenals, kidney, and heart

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13
Q

Activation of AT1 receptors works to

A

increase BP through vasoconstriction and Na+/water reabsorption

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14
Q

Name three things that angiotensin II alters

A
  1. altered peripheral resistance
  2. altered renal function
  3. altered cardiovascular structure
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15
Q

How does angiotensin II alter peripheral resistance?

A
  1. direct vasoconstriction
  2. enhancement of peripheral noradrenergic neurotransmission (increased NE release, decreased NE reuptake, increased vascular response)
  3. increased sympathetic discharge
  4. release of catecholamines from adrenal medulla
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16
Q

Result of altered peripheral resistance from angiotensin II

A

rapid pressor reponse (increased bp)

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17
Q

How does angiotensin II alter renal function?

A
  1. direct effect to increase Na+ reabsorption in proximal tubule
  2. release of aldosterone from adrenal cortex
  3. altered renal hemodynamics (direct renal vasoconstrictoin, enhanced noradrenergic neurotransmission in kidney, increased renal sympathetic tone)
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18
Q

Result of altered renal function from angiotensin II?

A

slow pressor response (Na+ and water retention)

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19
Q

How does angiotensin II alter cardiovascular structure?

A

I. non-hemodynamically mediated effects (increased expression of proto-oncogenes, increased GFs, increased synthesis of extracellular matrix proteins)
II. Hemodynamically mediated effects (increased afterload, increased wall tension)

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20
Q

Result of altered cardiovascular structure from angiotensin II?

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A

vascular and cardiac hypertrophy and remodeling

21
Q

Three classes of drugs that inhibit the renin-angiotensin system

Study These Flashcards
A
  1. direct renin inhibitors
  2. ACE inhibitors
  3. Angiotensin receptor blockers
22
Q

Sulfhydryl-containing ACE inhibitor

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A

captopril (capoten)

23
Q

Dicarboxyl-containing ACE inhibitor

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A

enalopril (vasotec)

24
Q

Phosphorous-containing ACE inhibitor

Study These Flashcards
A

fosinopril sodium (monopril)

25
What class of drugs would interfere with bradykinin-mediated vasodilation?
NSAIDs
26
What is the effect of ACE inhibitors on bradykinin?
bradykinin is not inactivated, so more is available to promote vasodilation and decrease blood pressure
27
What is the effect of ACE inhibitors on angiotension II?
decreased angiotensin II, so blood pressure is decreased
28
Side effects of sulfhydryl-containing ACE inhibitors (captopril)
altered taste (metallic) and rash
29
What is significant about Moexipril?
only ACE inhibitor cleared through hepatic metabolism (dose doesn't have to be adjusted in patients with compromised renal function)
30
Dicarboxyl-containing ACE inhibitor (Enalopril) requires
requires hydrolysis of ethyl ester to form active diacid form, enalaprilat (soluble form); enalopril is a pro-drug
31
Parenteral dosage forms of ACE inhibitors end in which suffix?
-PRILAT
32
Lysine-derivative of enalaprilat
Lisinopril (dicarboxyl-containing ACE inhibitor)
33
Clinical uses of ACE inhibitors
hypertension, left ventricular systolic dysfunction, myocardial infarction, diabetic nephropathy (prevention)
34
Adverse effects of ACE inhibitors
hypotension, dry cough, hyperkalemia, acute renal failure, skin rash (captopril), angioedema (contraindication)
35
Drug-drug interactions of ACE inhibitors
antacids (reduce bioavailability), NSAIDs may reduce effectiveness, K+ supplements, may increase plasma levels of digoxin and lithium
36
Contraindications of ACE inhibitors
pregnancy, high doses in patients with renal insufficiency may lead to neutrpenia
37
Angiotensin II type 1 receptor antgaonists
"the sartans" | losartan potassium; valsartan; irbesartan; candesartan cilexetil; temisartan; eprosartan mesylate
38
Actions of angiotensin II type 1 receptor (AT1) antagonists
selective blocks effects of angiotensin II: pressor effects, stimulation of NE system, secretion of aldosterone, effects on renal vasculature, growth-promoting effects on cardiac and vascular tissue uricosuric effect
39
What system does AT1 antagonists NOT effect
no effect on bradykinin system
40
What do angiotensin II receptor antagonists provide more complete inhibition of the action of angiotensin II as compared to ACE inhibitors?
Angiotensin III also works on these receptors
41
Clinical uses of AT1 receptor antagonists
hypertension, CHF, diabetic nephropathy, stroke prophylaxis
42
Adverse effects of AT1 receptor antagonists
hypotension, hyperkalemia, teratogenic potential
43
Renin inhibitor
Aliskiren (Tekturna)
44
How does Aliskirin work?
direct renin inhibition; dipeptide like mimetic
45
Aliskiren used to treat
used alone or in combination to treat hypertension
46
What decreases the absorption of Aliskirin
high-fat meals
47
Side effects of Aliskirin
diarrhea
48
Contraindications for Aliskirin
contraindicated in pregnancy and nursing mothers

Pharmacology Test #3 (13 decks)

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