renin angiotensin system inhibitors Flashcards
what are the 3 types of renin system inhibitors?
1- Angiotensin converting enzyme inhibitors (ACE inhibitors )—> PRILS
2- Angiotensin receptor blocker (ARBS )—> Atran
3- Renin inhibitors ——-> skirin
what are the effects of angiotensin 2?
1- potent vasoconstrictor via gq, AT1 receptors (ADH, Alpha agonists , endothelin also work on this receptors )
2-increase aldestrone release (Increase water retention )
3- Increase apoptosis—> thats why ACE inhibitors is bad for pregnancy cuz apoptosis is important for newborn development
4- Increase ADH/Vasopressin release (Increase water retention and vasoconstriction
ace inhibitors MOA
1- vasodilation ( directly) ( EVEN IF RENIN IS NOT THE PROBLEM)
2- Decrease aldosterone release and ADH ( INDIRECT VASODILATION cuz it blocks vasopressin which is adh )
3- inhibit apoptosis BAX. BAD1( Bad for pregnancy )
4- Increase bradykinin /prostaglandins which induce VASODILATION (indirect vasodilation mechanism)
5- reset baroreceptors like bb no reflex tachy cardia and activate parasympathetic activity
What are examples of ace inhibitors
Captopril —> الكابتن –> prototype
Enalapril
lisinopril
Fosinopril
Benzapril
Ramipril
enalaprilat IV formula
which ace inhibitor has sulfate group
captopril
zofenopril
what does the sulfate group does?
cause immune problems and angioedema ( With bradykenin) , Rash, leukopenia
which ace inhibitor is iv and given in emergencies
enalaprilat
which of the ace inhibitors is not a prodrug and that doesnt require activation
lisinopril and can be used in hepatic failure cuz it doesn’t require activation
which of the ace drug is not primarily eliminated by kidneys
Fosinopril
whats the relation between nsaids and ace inhibitors/antihypertensive agents?
nsaids inhibit the actions of all antihypertensive drugs
what are the uses of ace inhibitors
1- NUMBER 1 drug used for hypertension
2- congestive heart failure cuz it leads to vasodilation of vessels and reduce the pressure and decrease afterload
3- after MI cuz they inhibit apoptosis and stop the heart from remodeling
4- diabetes + hypertension = whenever you see diabetes + hypertension give ACE CUZ DIABETES CAUSE DIABETES NEPHROPATHY
What are the adverse effects of ACE inhibitors
C = cough caused by bradykinin SWITCH TO ARB
A= angioedema caused by bradykinin/sulfate SWITCH TO ARB
P= proteinurea = caused by kidney failure = stop medication cuz kidney needs RAAS
T= taste loss = temporarily
O= orthstatic hyptension = temporarily
P= pregnancy ( fetal abnormalities ) = never give
R = rash due to sulfate = switch to something without sulfate
I= increased potassium / hyperkalemia = need to stop medication cuz it leads to paralysis
L = leukopenia = due to sulfate = switch to something without sulfate
Renal failure
Also lead to increased renin secretion cuz of negative feedback
what are the contraindicated scenarios where you cant give aces
1- pregnancy
2- hyperkalemia
3-proteinurea
4-leukopenia
5- BILATERAL RENAL STENOSIS AND RENAL FAILURE
when do you give ACE and whats the relation between creatinine
creatinine levels indicate kidney function
0.8 - 1.2 = normal kidney
1.2 - 3 = minor kidney damage
3+ = sever kidney ischemia = never give AC
what are angiotensin receptor blockers ( ARBS)
Atrans : block AT1 receptor leading to the same effects as ace inhibitors
give examples of ARBS
loseratran, valsartran , telmeatran, comedyatran
what are the advantages of ARBS over ACE inhibitors
1- no braddykinine accumulation side effects : no angioedema/no dry cough
2- Spares AT2 receptors which is a good receptor that causes vasodilation cuz ARB only blocks AT1
3- avoids the problem with none angiotensin converting enzyme ( there are other enzymes that convert angiotensin 1 into ang 2 that are not ACE so sometimes when you give ACE inhibitors it will only block ace but not the others and the other enzymes that are non ace will convert ang 1 into ang 2 so you are not actually blocking ang 2) ARB avoids this
what are renin release inhibitors :
ALISIRKIN which block the renin release directly
what are the side effects of aliskirin
1- Diarrhea
2- cough
3-angioedema
which liver enzyme metabolizes aliskirin
CYP3A4
when is alirskirin contraindicated
pregnancy
