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B Pharmaco Ex2
PCOL RAAS Drug/Extra Key Info
Drug | Extra/ Key Info |
---|---|
Aliskiren | Low drug bioavailability but HIGH affinity for Renin Renin is the rate-limiting enzyme for the RAAS Pathway |
Captopril Enalapril (Vasotec) Lisinopril (Prinvil) Benazepril (Lotensin) Quinapril (Accupril) Ramipril (Altace) | Primary effect: Inhibit ACE (ACE converts Angiotensin I to Angiotensin II & breaks down Bradykinin) Bonus effect 1: Ang I goes down alternate pathway and is converted to Angiotensin 1-7 which binds to AT2-->oppose AT1. Bonus effect 2: Increase levels of Bradykinin (dilator)-->Dry cough. Most are Pro-drugs-->improve ADMET profile 1st line HTN |
Losartan (Cozaar) 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 High affinity for AT1 |
Spironolactone Eplerenone | These drugs are Aldosterone Antagonists Aldosterone enhances the production of Na+/K+ channels (lumen) and pumps (interstitial space inside cell) and these drugs binds to the same space therefore not allowing aldosterone to binds and thus decreasing the production of these channels/pumps-->Less Na+ reabsorption. |
Metoprolol | ----- |