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

A
20
Q

What is a disadvantage of enalaprilat

A
21
Q

Explain what is enalapril (renitec)

A
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

A
24
Q

What is aliskiren

A
25
Q

What is the advantage of renin inhibitors

A
26
Q

What is losartan

A
27
Q

Explain vasodilators

A
28
Q

Arterial dilator drugs are used for what

A
29
Q

Venous dilator drugs are used for what

A
30
Q

List the examples of vasodilators

A

Nitrates (nitric oxide releasing agents)
K+ channel activation
K+ channel openers
Phosphodiesterase inhibitors
Calcium channel blockers

31
Q

List the example of nitrate drugs

A

Nitroglycerin
Sodium nitroprosside

32
Q

Give example of K+ channel activator

A

Hydralazine

33
Q

Give example of K+ channel opener

A

Minoxidil (rogaine)

34
Q

Give example of phosphodiesterase inhibitors

A

Sildehafil (viagra)

35
Q

Give example of calcium channel blockers

A

Hydropyridines ( nifedipine)

36
Q

Explain nitroglycerine

A
37
Q

Explain the nitric oxide mediated vasodilation

A
38
Q

Explain hydralazine and sodium nitroprusside

A
39
Q

What is the indication of nitroprusside

A

Hypertensive emergency

40
Q

What is the mechanism of hydralazine and sodium nitroprusside

A
41
Q

What is the toxicity of hydralazine and sodium nitroprusside

A
42
Q

Explain minoxidil

A
43
Q

Why is the side effect of minoxidil

A
44
Q

Explain calcium channel blockers

A
45
Q

Explain dihydropyridines

A
46
Q

What is the prototype of dihydropyridines

A

Nifedipine

47
Q

Explain verapamil and its use

A