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Pharmacology Exam 2

RAAS

QuestionAnswer
Aliskiren MOA Selective Renin inhibitor REVERSIBLE antagonist
Aliskiren SOA Blood stream (Renin - 1st step in RAAS pathway)
Aliskiren SE Lower TPR Lower aldosterone Decrease sodium and water reabsorption Angioedema, hypotension, cough, headache, diarrhea, skin rash
Aliskiren EI Low drug bioavailability but high affinity for renin Renin is the rate limiting enzyme for the RAAS pathway
Captopril MOA Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) ACE inhibitor Angiotensin converting enzyme inhibitor REVERSIBLE antagonists
Captopril SOA Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) Blood stream
Captopril SE Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) Lower TPR Lower aldosterone Decrease sodium and water reabsorption Dry cough, hyperkalemia, angioedema, first dose hypotension, fetopathic potential
Captopril EI Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) Part 1 Primary effect: inhibit ACE (ACE converts Ang I to Ang II & breaks down bradykinin) Bonus effect 1: Ang 1 goes down alternate pathway and is converted to Angiotensin 1-7 which bind to AT2  oppose AT1
Captopril EI Enalapril (Vasotec) Lisinopril (Prinivil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) Part 2 Bonus effect 2: Increase levels of bradkykinin (dilator)  dry cough Most are Pro-drugs -> improve ADMET profile 1st line for HTN
Losartan (Cozaar) MOA Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil ARB Angiotensin II receptor blocker REVERSIBLE antagonists
Losartan (Cozaar) SOA Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil Blood stream
Losartan (Cozaar) SE Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil Lower TPR Lower aldosterone Decrease sodium and water reabsorption Hyperkalemia, angioedema
Losartan (Cozaar) EI Valsartan (Diovan) Olmesartan (Benicar) Telmisartan (Micardis) Irbesartan (Avapro) Medoxomil 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 MOA Eplerenone Potassium-sparing diuretic Mineralocorticoid (MR) receptor antagonist
Spironolactone SOA Eplerenone Kidney -> Collecting duct of nephron
Spironolactone SE Eplerenone Hyperkalemia, diarrhea, drowsiness Males: gynecomastia & impotence
Spironolactone EI Eplerenone Aldosterone antagonists Aldosterone enhances the production of Na+/K+ channels (lumen) and pumps (interstitial space side of cell), and these drugs bind to the same space therefore not allowing aldosterone to bind -> less Na+ reabsorption
Metoprolol MOA Selective β1 blocker
Metoprolol SOA Kidney
Metoprolol SE Less renin production  no RAAS pathway
Created by: jflaman
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