Antihypertensive Agents - Renin-angiotensin System Targeting Drugs Flashcards

1
Q

How does the renin angiotensin aldosterone system work

A
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2
Q

What is the effect of angiotensin II

A

Increase sympathetic activity
Tubular Na+ Cl- reabsorption and K+ excretion. H2O retention
Stimulate adrenal gland cortex
Arteriolar vasoconstriction
Stimulate pituitary gland - antidiuretic secretion

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3
Q

What is angiotensinogen

A
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4
Q

What is angiotensin I

A

Decapeptide

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5
Q

What is angiotensin II

A

Octapeptide

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6
Q

What is angiotensin III

A

Heptapeptide

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7
Q

What are the drugs for the renin-angiotensin system

A
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8
Q

What else can ACE inhibitors inhibit apart from conversion of angiotensin I to II

A

Bradykinin metabolism to the inactive form - causing an increase of bradykinin

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9
Q

What is the effect of bradykinin increase

A
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10
Q

Explain mode of binding of angiotensin I to ACE

A
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11
Q

What is the role of zinc in ACE

A

Weaken the bind to hydrolysis the peptide link - removing 2 amino acids

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12
Q

What is the important amino acid for ACE inhibitor

A

Proline

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13
Q

Why did they want to prepare peptide similar to those of the snake venom

A
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14
Q

What is teprotide

A
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15
Q

What was the first ACE inhibitor antihypertensive agent

A

Captopril (capoten)

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16
Q

Explain ACE inhibitors

A
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17
Q

What are the 3 groups of ACEIs

A
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18
Q

Why were dicarboxylate containing inhibitors developed

A
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19
Q

Why is enalaprilate more potent than captropil

20
Q

What is a disadvantage of enalaprilat

21
Q

Explain what is enalapril (renitec)

22
Q

What is the benefit of enalapril being a prodrug

A

Make ester to mask the polarity by removing one carboxylic bond and enhance absorption → then hydrolyzed into active form

23
Q

Explain the phosphate containing ACE inhibitors

24
Q

What is aliskiren

25
What is the advantage of renin inhibitors
26
What is losartan
27
Explain vasodilators
28
Arterial dilator drugs are used for what
29
Venous dilator drugs are used for what
30
List the examples of vasodilators
Nitrates (nitric oxide releasing agents) K+ channel activation K+ channel openers Phosphodiesterase inhibitors Calcium channel blockers
31
List the example of nitrate drugs
Nitroglycerin Sodium nitroprosside
32
Give example of K+ channel activator
Hydralazine
33
Give example of K+ channel opener
Minoxidil (rogaine)
34
Give example of phosphodiesterase inhibitors
Sildehafil (viagra)
35
Give example of calcium channel blockers
Hydropyridines ( nifedipine)
36
Explain nitroglycerine
37
Explain the nitric oxide mediated vasodilation
38
Explain hydralazine and sodium nitroprusside
39
What is the indication of nitroprusside
Hypertensive emergency
40
What is the mechanism of hydralazine and sodium nitroprusside
41
What is the toxicity of hydralazine and sodium nitroprusside
42
Explain minoxidil
43
Why is the side effect of minoxidil
44
Explain calcium channel blockers
45
Explain dihydropyridines
46
What is the prototype of dihydropyridines
Nifedipine
47
Explain verapamil and its use