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Pharmacology > ACE Inhibitors and AT1 receptor Antagonsit > Flashcards

ACE Inhibitors and AT1 receptor Antagonsit Flashcards

1
Q

Where is the gene that codes for renin located?

A

1q32

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2
Q

Renin is produced as an aspartyl protease enzyme that does what?

A

Catalyzes the restrictive excision of the angiotensinogen to angiotensin 1

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3
Q

How are baroreceptors activated?

A

by sensing changes in diameter of arterioles locally

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4
Q

The activation of glomerular chemoreceptors is going to be mediated by..

A

Sensing changes in the concentration of sodium and chloride

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5
Q

The activation of the beta-adrenergic receptors as well as the catecholamines can induce the activation of the…

A

Mácula densa

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6
Q

The mesangial cells are located in the…

A

mácula densa

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7
Q

The mesangial cells are responsible for secreting what substance?

A

renin

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8
Q

Angiotensinogen is what type of protein?

A

Glycoprotein and serine protease inhibitor

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9
Q

Glycosylation and polymerization increase the affinity of what substance?

A

Renin

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10
Q

Angiotensinogen is principally produced in the…

A

Liver but can be expressed in other tissues such as the neurons, renal, endothelial, heart, etc

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11
Q

After the angiotensinogen undergoes glycosylation and polymerization, it is…

A

Oxidized

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12
Q

Angiotensin I interacts with 3 other enzymes which are?

A
  1. Angiotensin converting enzyme
  2. angiotensin converting enzyme 2
  3. aspartyl amino peptidase
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13
Q

When angiotensin I interacts with its enzyme what 3 metabolites can be found?

A
  1. Ang 2
  2. Ang 1-9
  3. Ang 2-10

They can all lock into the AT1R and AT2R receptors but they all have different actions on it

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14
Q

The Ang 2-10 and And 1-9 interacts with…

A

ACE and produce ANG III and ANG 1-7

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15
Q

The Ang II interacts with…

A

ASAP ( aminopeptidase A) and APA to produce ANG III but can also interact with ACE-2 to produce ANG 1-7

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16
Q

ANG III is an

A

agonist of AT1R and AT2R

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17
Q

ANG 1-7 is an agonist of the

A

AT2R and AT7R as well as the Más receptor

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18
Q

ANG III interacts with APN and APB to produce what?

A

ANG IV which can lock into AT4R

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19
Q

The angiotensin receptors belong to the…

A

seven transmembrane family and can be coupled with membrane enzymes

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20
Q

What is the active metabolite of enalapril?

A

enalaprilat

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21
Q

What happens if enalapril is taken with acetylsalicylic acid?

A

It decreases the enalapril efficacy

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22
Q

What could go wrong if enalapril is taken with aliskiren?

A

there is risk or severity of hypotension, hyperkalemia, and nephrotoxicity

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23
Q

What could go wrong if enalapril is taken with amiodarone?

A

there is risk or severity of myopathy, rhabdomiolysis, myoglobinuria

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24
Q

What happens if enalapril and sacubitril are taken together?

A

There is risk or severity of angioedema

25
Q

How many functionally active domains are present in a somatic ACE enzyme?

A

two the N and C

26
Q

The C domain of a somatic ACE enzyme is in charge of what?

A

blood pressure

27
Q

The functionally active N domain of a somatic ACE plays a role in?

A

hematopoietic stem cell differentiation and proliferation

28
Q

ACE inhibitors bind to?

A

Both the N and C domains of the angiotensin converting enzyme. But they have more affinity for the C domain

29
Q

How does captopril work?

A

It works by competing with angiotensin I for binding to ACE and inhibits an enzymatic proteolysis of angiotensin I to angiotensin II decreasing the angiotensin II levels and increasing the renin levels

30
Q

Captopril also has an inhibitory effect on?

A

type IV collagenase, matrix metalloproteinase-9, Leukotriene A-4 hydrolase

31
Q

Captopril has an agonist effect on?

A

B1 bradykinin receptor

32
Q

What are some important adverse effects of captopril?

A

Cough and angioedema

33
Q

What is the mechanism of losartan?

A

It blocks the AT1 R so that angiotensin II cannot hind and exert its effects

34
Q

Losartan and it’s active metabolite bind to the AT1 receptor with 1,000 times more affinity than they bind to the…

A

AT2 receptor

35
Q

What are some adverse effects of losartan?

A

hypotension, tachycardia and bradycardia can also result fue to vagal nerve stimulation

36
Q

What happens if warfarin is taken with losartan?

A

The metabolism of warfarin can be decreased

37
Q

What happens if adenosine is taken with losartan?

A

The metabolism of Losartan can be decreased

38
Q

What happens if losartan is taken with aliskiren?

A

There is a risk or severity for hyperkalemia

39
Q

How does telmisartan work?

A

By interfering with the binding of angiotensin II by binding reversibly to the AT1 receptors that are located in the vascular smooth muscle and the adrenal gland

40
Q

Telmisartan is a partial agonist of?

A

PPARy which is an established target for antidiabetic drugs

41
Q

Telmisartan can improve what?

A

Carbohydrate and lipid metabolism as well as control insulin resistance

42
Q

Are the cytochrome P450 enzymes involved in the metabolism of telmisartan?

A

No

43
Q

What happens when telmisartan is used with acetylsalicylic acid?

A

There is risk or severity of renal failure, hyperkalemia, and hypertension

44
Q

What happens when alteplase is taken with telmisartan?

A

There is risk or severity of angioedema

45
Q

Aliskiren is used for?

A

Treating hypertension in children above 6 years of age and also adults

46
Q

How does aliskiren work?

A

prevents the RAAS process by binding to renin at it’s active site stopping the cleavage of angiotensin in turn inhibiting the formation of angiotensin I

47
Q

What are some common adverse effects of aliskiren?

A

Cough, skin rash, headaches, dizziness

48
Q

What are some serious adverse effects of aliskiren?

A

Fetal toxicity, anaphylactic reactions, head and neck angioedema, hypotension

49
Q

Do ACE inhibitors increase or decrease the production of bradykinin?

A

increase

50
Q

What are some effects of bradykinin?

A

Increased nitric oxide, increased fibrinolysis, and decreased thrombocyte activity

51
Q

Does the angiotensin receptor blockers decrease bradykinin levels?

A

Yes

52
Q

Statistically, are angiotensin receptor blockers equally as effective as ace inhibitors?

A

Yes

53
Q

What is the most common adverse effect of ace inhibitors?

A

Irritating cough

54
Q

The prevalence of the cough caused by ACE inhibitors is more common is what ethnicity?

A

Asian Americans

2.5 times higher than in caucasians

55
Q

What is a less common adverse effect of ace inhibitors that occasionally can be fatal?

A

Angioedema

56
Q

Angioedema caused by ace inhibitors is more prevalent in?

A

Black patients of African American origin

57
Q

Life threatening angioedema typically affects the?

A

Larynx and upper respiratory tract

58
Q

Telmisartan is the only angiotensin receptor blocker that can reach?

A

Blood brain barrier due to being liposoluble

Pharmacology (5 decks)

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