Medicinal Chemistry & Pharmacology 2 - exam 1
Quiz yourself by thinking what should be in
each of the black spaces below before clicking
on it to display the answer.
Help!
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| show | -increase in HR
-increase in BP
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| BP equation | show 🗑
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| Renin-Angiotensin-Aldosterone System (RAAS) pathway and how it increases BP | show 🗑
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| show | -ACE inhibitors are structurally similar to AT1 and compete for the enzyme ACE
-ARBs are structurally similar to AT2 and compete for AT2 receptors
-leads to dec. BP by dec. Na+ & water retention
-SE is inc. in K+
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| effects of ACEIs & ARBs on: 1) Na+ 2) K+ 3) BP 4) Cl- | show 🗑
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| therapeutic uses of ACEIs | show 🗑
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| show | -sulfhydryl-containing inhibitors
-phosphonate-containing inhibitors
-dicarboxylate-containing inhibitors
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| show | captopril
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| phosphonate-containing ACEIs | show 🗑
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| show | benazepril, enalapril, lisinopril, perindopril, quinapril, ramipril, trandolapril, moexipril
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| main structural feature of all ACEIs | show 🗑
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| binding interactions of ACEIs | show 🗑
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| captopril (not including SE) | show 🗑
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| SE of captopril | show 🗑
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| show | captopril does not require activation by liver enzymes
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| enalaprilat | show 🗑
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| show | -ester prodrug of enalaprilat (2 carboxylate groups & secondary amine are responsible for low lipophilicity/oral bioavailability)
-once abosorbed, bioactivation by hepatic esterases leads to enalaprilat formation
-drawback in pts. w/hepatic problems
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| lisinopril (not including bioavailability) | show 🗑
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| lisinopril bioavailability | show 🗑
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| locations of ACE | show 🗑
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| show | -benazepril & ramipril
-higher potency than lisinopril
*these two have rings that are bio-isosteric replacements of proline
-advantage: better bioavailability
-disadvantage: requires hepatic activation = bad in hepatic disease
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| show | -apparently, according to his superior intellect, "similar" means = number of mg's while "equivalent" means doses that produce similar therapeutic effect
-ex: at similar doses, ramipril has inc. potency compared to lisinopril
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| fosinopril | show 🗑
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| advantage of fosinopril | show 🗑
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| N-ring of ACEIs | show 🗑
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| duration of action of ACEIs | show 🗑
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| metabolism of ACEIs | show 🗑
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| show | AT2 receptor type 1
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| ARBs | show 🗑
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| show | -imidazole ring forms H-bonds
-aromatic group/n-butyl chain forms hydrophobic interactioins
-ionizable (R1) group binds with receptor via dipole interactions
-R2 group is acidic group (absorbs well in stomach)
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| structural similarities between ARBs & AT2 | show 🗑
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| main structural difference of valsartan | show 🗑
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| show | -candesartan cilexitil
-olmesartan medoxomil
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| show | -azilsartan
-candesartan/olmesartan
-irbesartan/eprosartan
-telmisartan/valsartan
-losartan
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| show | -candesartan
-olmesartan
-irbesartan
-azilsartan
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| show | highly protein bound (>90%) to albumin
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| metabolism of losartan | show 🗑
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| metabolism of other ARBs (besides losartan) | show 🗑
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