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CVS 🫀 > W3, 6 Pharma RAAS > Flashcards

W3, 6 Pharma RAAS Flashcards

1
Q

Components of the Renin-Angiotensin System

A
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2
Q

RAS is also expressed locally. In what organs & systems?

A
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3
Q

RAAS system

A
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4
Q

What’s the advantage of ARBs over ACEI ?

A
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5
Q

What are Alternate pathways of angiotensin II production? (Not involving ACE)

A
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6
Q

Angiotensin acts through what receptors?

A
  • AT 1-receptors
  • AT2-receptors
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7
Q

what are Pharmacological actions of Angiotensin II ?

A
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8
Q

Ang II type 1 (AT1R) receptor
A. What type of receptor?
B. Where is it expressed?
C. Action?

A
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9
Q

Pharma cological ations of AngII mediated by AT1- receptors

A
  1. Constriction of resistance vessels to increase systemic vascular resistance and blood pressure
  2. Stimulation of vascular, cardiac and renal hypertrophy
  3. Stimulation of sodium transport (Na/H+ exchanger) at several regions of the tubule leading to sodium and water retention
  4. Stimulation of antidiuretic hormone (vasopressin) release - water retention
  5. Enhancement of sympathetic nerve activity
  6. Contraction of intestinal smooth muscles
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10
Q

What are Selective antagonists of AT1R?

A

losartan, valsatan, telmisartan (drugs ending “tan” are selective AT1R blockers)

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11
Q

Ang II type 2 (AT2R) receptor
A. Type
B. Location
C. Action

A
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12
Q

Ang II type 2 (AT2R) receptor selective agonist & antagonist

A

• Selective antagonists –PD 123319
• Selective agonist -CGP42112

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13
Q

Pharmacological actions mediated by AT2-receptor activation

A
  1. Vasodilation – by increasing production of bradykinin, Nitric oxide and cGMP.
    AT2-receptor activation reduces BP when AT1-receptor is blocked.
  2. Inhibition of growth and cardiac remodeling
  3. Possible mediation of some beneficial effects of AT1-receptor blockade
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14
Q

Renin Inhibitors drug is

A

e.g. Aliskiren

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15
Q

Aliskiren
A. Used to trat …
B. What Type of inhibitor

A
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16
Q

Aliskiren
A. Orally active or not?
B. Peak Plasma concentration is reached within … hours?
C. Metabolized by ..?
D. Elimination?

A

A. Aliskirenis orally active with a very low bioavailability (~2.5%).
B. reached within 1–6 hours after oral administration
C. metabolized by cytochrome P450 enzyme 3A4.
D. More than 90% is eliminated unchanged in the feces, <2% is
eliminated as oxidized metabolites, and <1% is eliminated in the urine.

17
Q

Common adverse events of aliskiren include:

A

• Headache
• Dizziness
• Fatigue.
• Dose-related gastrointestinal events.
• A slight increase in cough (much less than ACE inhibitors).
• Hyperkalemia which is worsened when used in combination with an ACE inhibitor.

18
Q

What drug is useful in hypertensive diabetic patients?

A

ACE inhibitors

19
Q

Actions of ACE inhibitors

A

• Prevent the conversion of AngI into AngII –reduce systemic vascular resistance, reduce intravascular volume

20
Q

What’s the main Side effect of ACEI?

A

•Decrease bradykinin degradation –high levels of bradykinin - cough

21
Q

Uses of ACE inhibitors

A

•Mild to severe hypertension
•Congestive heart failure
•Diabetic nephropathy.

22
Q

Side effects of ACEI ?

A
  1. Hypotension
  2. Cough
  3. Hyperkalemia
  4. Renal failure
  5. Fetal anomalies
  6. Angioedema
  7. Neutropenia
23
Q

Angio tensin receptor blockers

A

e.g. losartan,valsartan

24
Q

ARBs administration and action

A

These are orally effective competitive antagonists of AT1 receptors – reduce blood pressure. They also reduce arteriolar and ventricular remodeling

25
Q

ARBs can be used to treat:

A

•Hypertension
•Heart failure
•Kidney failure in diabetes
•Chronic kidney diseases

26
Q

Side effects of ARBs

A

•Dizziness
•Elevated blood potassium level (hyperkalemia)
•Localized swelling of tissues (angioedema)
•Orthostatic hypotension (early in the treatment)

27
Q

Newer pathways of Angiotensin I metabolism

A
28
Q

What drugs are Useful in patients who cannot tolerate ACE inhibitors

A

ARBs

29
Q

What drug Can be detected in the kidneys for up to 3 weeks after
discontinuation of treatment (whereas its plasma levels become
undetectable at an earlier time)

A

Aliskiren

30
Q

What drug is Thought to be more effective in reducing blood pressure and ventricular hypertrophy

A

Aliskiren

31
Q

Administration of ACE inhibitors is accompanied by:

A
32
Q

سلايدة عبيطة مافهمت منها شي

A

CVS 🫀 (31 decks)

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