Drugs acting on Renin-Angiotensin-Aldosterone system Lecture PDF Flashcards
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ARB is short for…
Angiotensin II receptor blockers
Some angiotensin II is produced without requiring ____, therefore drugs that block this enzyme do not completely stop angiotensin II production
ACE
ACE inhibitors mech of action and ADR’s (5)
Prevents conversion from angiotensin I to II, major response is vasodilation, reduced aldosterone promoting renal retention of K+ and excretion of Na+ and H2O
- hypotension
- cough due to increased bradykinin levels
- hyperkalemia
- fetal injury use during 2nd or 3rd trimester
- neutropenia
ACE is also known as…
….Kinase II when it functions on bradykinin metabolism
ACE inhibitors therapuetic uses (4) and administration
- hypertension and reduce risk of cardiovascular mortality caused by HTN
- heart failure
- ASAP therapy after MI
- slow progression of established nephropathy (diabetic and nondiabetic)
Oral administration
ACEI advantages to other antihypertensive agents (4)
- no cardiovascular reflexes
- used safely with bronchial asthma
- does not promote hypokalemia or hyperglycemia like seen with thiazide diuretics
- does not induce lethargy, weakness, or sexual dysnfunciton
Angiotensin II action in the vasculature and at the kidney
-constricts afferent arterioles and constricts efferent glomerular arteriole raising glomerular pressure and stasis in high enough conc.
ACEI drug interactions (3)
- Diuretics should be withdrawn 2-3 days earlier and can be started later if needed
- hypotensive agents are additive effects
- hyperkalemia if administered with K+ supplements or K+ sparing diuretics
ARB’s therapeutic uses (4) and mech of action
- hypertension
- diabetic neuropathy
- MI
- prevention of MI, stroke, and death in patients with high CV risk
-block binding of angiotensin II to type 1 angiotensin II receptors in blood vessels and other tissues causing dilation of arterioles and veins, block all angiotensin II regardless of where it is produced, decrease release of aldosterone from adrenals, does not impact bradykinin
ARB vs ACEI
ARBs have lower risk of cough/hyperkalemia than ACEI
ARB’s therapuetic uses
- hypertension
- heart failure
- diabetic neurpathy
- MI
- stroke prevention
- prevention of MI, stroke, and death of patients with high CV risk
ARB’s ADR’s (4)
- low incidence of dizziness
- rare angioedema (discontinue if occurs)
- hyperkalemia may occur
- fetal harm in 2nd 3rd trimesters
Aliskiren (tekturna) drug class and mech of action
- Direct renin inhibitor
- binds renin blocking cleavage of angiotensinogen to angiotensin I leading to decreased levels of II and aldosterone
Aliskiren (tekturna) effectiveness
Seen to reduce BP to same extent as ACEI, ARB, or ca2+ blockers, not DOC until long term benefits are found out
Aliskiren (tekturna) ADRs (4)
- does not increase bradykinin levels
- diarrhea
- hyperkalemia
- fetal harm same as ARBS and ACEI’s, contraindicated in 2nd and 3rd trimesters