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Pharmacology > ACE Inhibitors and AT1 receptor Antagonsit > Flashcards

ACE Inhibitors and AT1 receptor Antagonsit Flashcards

(58 cards)

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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?

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A

There is risk or severity of angioedema

25
How many functionally active domains are present in a somatic ACE enzyme?
two the N and C
26
The C domain of a somatic ACE enzyme is in charge of what?
blood pressure
27
The functionally active N domain of a somatic ACE plays a role in?
hematopoietic stem cell differentiation and proliferation
28
ACE inhibitors bind to?
Both the N and C domains of the angiotensin converting enzyme. But they have more affinity for the C domain
29
How does captopril work?
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
Captopril also has an inhibitory effect on?
type IV collagenase, matrix metalloproteinase-9, Leukotriene A-4 hydrolase
31
Captopril has an agonist effect on?
B1 bradykinin receptor
32
What are some important adverse effects of captopril?
Cough and angioedema
33
What is the mechanism of losartan?
It blocks the AT1 R so that angiotensin II cannot hind and exert its effects
34
Losartan and it’s active metabolite bind to the AT1 receptor with 1,000 times more affinity than they bind to the...
AT2 receptor
35
What are some adverse effects of losartan?
hypotension, tachycardia and bradycardia can also result fue to vagal nerve stimulation
36
What happens if warfarin is taken with losartan?
The metabolism of warfarin can be decreased
37
What happens if adenosine is taken with losartan?
The metabolism of Losartan can be decreased
38
What happens if losartan is taken with aliskiren?
There is a risk or severity for hyperkalemia
39
How does telmisartan work?
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
Telmisartan is a partial agonist of?
PPARy which is an established target for antidiabetic drugs
41
Telmisartan can improve what?
Carbohydrate and lipid metabolism as well as control insulin resistance
42
Are the cytochrome P450 enzymes involved in the metabolism of telmisartan?
No
43
What happens when telmisartan is used with acetylsalicylic acid?
There is risk or severity of renal failure, hyperkalemia, and hypertension
44
What happens when alteplase is taken with telmisartan?
There is risk or severity of angioedema
45
Aliskiren is used for?
Treating hypertension in children above 6 years of age and also adults
46
How does aliskiren work?
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
What are some common adverse effects of aliskiren?
Cough, skin rash, headaches, dizziness
48
What are some serious adverse effects of aliskiren?
Fetal toxicity, anaphylactic reactions, head and neck angioedema, hypotension
49
Do ACE inhibitors increase or decrease the production of bradykinin?
increase
50
What are some effects of bradykinin?
Increased nitric oxide, increased fibrinolysis, and decreased thrombocyte activity
51
Does the angiotensin receptor blockers decrease bradykinin levels?
Yes
52
Statistically, are angiotensin receptor blockers equally as effective as ace inhibitors?
Yes
53
What is the most common adverse effect of ace inhibitors?
Irritating cough
54
The prevalence of the cough caused by ACE inhibitors is more common is what ethnicity?
Asian Americans | 2.5 times higher than in caucasians
55
What is a less common adverse effect of ace inhibitors that occasionally can be fatal?
Angioedema
56
Angioedema caused by ace inhibitors is more prevalent in?
Black patients of African American origin
57
Life threatening angioedema typically affects the?
Larynx and upper respiratory tract
58
Telmisartan is the only angiotensin receptor blocker that can reach?
Blood brain barrier due to being liposoluble

Pharmacology (5 decks)

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