Medicinal Chemistry & Pharmacology 2 - exam 1
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| general effect of sympathetic drugs on HR & BP | show 🗑
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| show | BP = CO * R
*CO = Cardiac Output
*R = arterial Resistance
*CO is determined by stroke volume & HR
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| Renin-Angiotensin-Aldosterone System (RAAS) pathway and how it increases BP | show 🗑
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| ACE inhibitors and ARBs | show 🗑
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| effects of ACEIs & ARBs on: 1) Na+ 2) K+ 3) BP 4) Cl- | show 🗑
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| show | -treatment of HTN, HF, left ventricular dysfunction (LVD)
-reduction of the risk of MI, stroke, and death from cardiovascular causes
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| show | -sulfhydryl-containing inhibitors
-phosphonate-containing inhibitors
-dicarboxylate-containing inhibitors
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| sulfhydryl-containing ACEIs | show 🗑
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| show | fosinopril
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| show | benazepril, enalapril, lisinopril, perindopril, quinapril, ramipril, trandolapril, moexipril
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| show | Zn-binding pocket
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| show | -ionic bond with Zn on ACE
-double bonded O of amide group can form H-bonds with ACE
-side chains contribute to overall binding affinity (hydrophobic/Van der Waals interactions)
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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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| show | - -SH group of captopril replaced with -COOH
-proline is still the AA for good activity
- ~10x more potent than captopril
-excellent IV activity but very poor oral bioavailability
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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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| show | -most hydrophilic ACEI
-presence of NH2 & COOH groups make it a double zwitterion -> neutralization -> absorbs readily in gut
-active transport across intestinal epithelium
-good oral bioavailability, long t_1/2
-QD
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| locations of ACE | show 🗑
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| other ACEIs that are ester prodrugs & associated advantages and disadvantages | show 🗑
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| Gupta's tricky use of the words "equivalent" and "similar" | show 🗑
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| show | -prodrug
-phosphate + proline derivative
-phosphinic acid interacts with Zn
-ionic, H, & hydrophobic bonds similar to enalapril
-most lipophilic ACEI
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| advantage of fosinopril | show 🗑
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| show | -must have carboxylic acid group
-large hydrophobic rings increases potency (ex. benazepril & ramipril) and alters PK parameters
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| duration of action of ACEIs | show 🗑
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| show | -captopril: forms disulfide dimer or a captopril-cysteine disulfide
-lisinopril & enalaprilat: no metabolism
-rest are all prodrugs
-further metabolic transformation: glucuronidation
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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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| show | isosteric replacement of imidazole ring
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| show | -candesartan cilexitil
-olmesartan medoxomil
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| ARB affinity for AT2 type I receptor (greatest to least) | show 🗑
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| ARBs whose clearance is not affected by hepatic insufficiency | show 🗑
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| show | highly protein bound (>90%) to albumin
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| show | -oxidized by CYP2C9 & 3A4 to produce EXP-3174
-EXP-3174 is 10 - 40x more potent than losartan
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| show | irbe-, telmi-, & epro- sartan are all metabolized to inactive glucuronide conjugates
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