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RAAS drugs

Pharmacology Exam 2

DrugMOASOASE / ADRsEK
Aliskiren Selective Renin inhibitor REVERSIBLE antagonist Blood stream (Renin - 1st step in RAAS pathway) Lower TPR Lower aldosterone Decrease sodium and water reabsorption Angioedema, hypotension, cough, headache, diarrhea, skin rash Low drug bioavailability but high affinity for renin Renin is the rate limiting enzyme for the RAAS pathway
Captopril Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists Blood stream Lower TPR Lower aldosterone Decrease sodium and water reabsorption Dry cough, hyperkalemia, angioedema, first dose hypotension, fetopathic potential ACE inhibitors block Ang I→Ang II and bradykinin breakdown. Ang I can form Ang 1-7, activating AT2 to counter AT1. ↑Bradykinin → vasodilation & dry cough. Most are prodrugs (better ADMET). 1st-line for HTN.
Losartan (Cozaar) Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil ARB Angiotensin II receptor blocker REVERSIBLE antagonists Blood stream Lower TPR Lower aldosterone Decrease sodium and water reabsorption Hyperkalemia, angioedema Primary effect: Block AT1 Bonus effect 1: increase AT2 activation (oppose AT1) Losartan is an active drug that turns into an even more active metabolite – very effective Most are Pro-drugs  improve ADMET profile High affinity for AT1
Spironolactone Eplerenone Potassium-sparing diuretic Mineralocorticoid (MR) receptor antagonist Kidney > Collecting duct of nephron Hyperkalemia, diarrhea, drowsiness Males: gynecomastia & impotence Aldosterone normally ↑Na⁺ channels (lumen) and Na⁺/K⁺ pumps (basolateral). Antagonists block the receptor, preventing this effect → ↓Na⁺ reabsorption, ↓K⁺ excretion, causing natriuresis and K⁺ retention.
Metoprolol Selective β1 blocker Kidney Less renin production >no RAAS pathway
Created by: PharmacistJulian
 

 



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