Term
| 3 CLASSES OF VASODILATORS |
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Definition
NITROVASODILATORS
CALCIUM CHANNEL ANTAGONISTS/BLOCKERS
POTASSIUM CHANNEL BLOCKER |
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Term
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Definition
| These replenish vascular smooth muscle cells with nitric oxide (NO) gas. NITRIC OXIDE allows MLCK to be phosphorylated and become inactive preventing contraction and causing vasodilation. |
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Term
| ENZYME THAT SYNTHESIZES NITRIC OXIDE |
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Definition
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Term
| SPECIFIC MOA OF ORGANIC NITRATES (I.E.) NITROGLYCERIN |
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Definition
| v Organic nitrates such as nitroglycerin react with –SH-containing compounds such as Cysteine and Glutathione to release NO. |
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Term
Reddish brown photosensitive direct acting vasodilator that must be activated first in order to release nitric oxide
Hint: Complex of iron, cyanide groups and a nitroso moiety |
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Definition
| Sodium Nitropusside (Nitropress) |
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Term
| MOA of potassium channel blockers |
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Definition
These open plasma membrane ATP-sensitive potassium channels.
v Potassium efflux causes hyperpolarization.
v This inhibitory influence results in less intracellular calcium and muscle relaxation. |
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Term
| De-sulfamoyl analogue of benzothiazine diuretics that has an increases anti-hypertensive properties |
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Definition
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Term
| This potassium channel agonist is activated by liver sulfotransferase and N-oxide is required for bioactivity |
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Definition
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Term
| D1 agonist that acts as a vasodilator? Give the active enantimoeric form |
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Definition
Fenoldopam (Corlopam)
R-isomer |
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Term
Acetylation at azo bond render this direct acting vasodilator inactive
Hint: Phthalazine substituted hydrazine |
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Definition
| Hydralazine HCl (Apresoline) |
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Term
| Prevents interaction of myosin with actin in heart muscle |
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Definition
| tropins I,C,T and tropomyosin |
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Term
| Type of calcium channels that are responsible for contraction of cardiac and smooth muscles |
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Definition
| voltage-dependent calcium channels |
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Term
| voltage-dependent calcium channels located on skeletal, cardiac and smooth muscles |
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Definition
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Term
Benzothiazepine calcium channel blocker
peak concentration in 3-4 hrs
Metabolism: Deacetylation, oxidative O- and N-demethylation and conjugation |
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Definition
| Diltiazem HCl (Cardiazem) |
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Term
| Active metabolite of diltiazem with 40-50% of its activity |
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Definition
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Term
Prototype drug for calcium channel blockers
Low bioavailability
Metabolism: N-dealkylation, O-demethylation and conjugation |
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Definition
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Term
Site of action for the following diuretic agents:
A. Carbonic Anhydrase Inhibitors
B. Loop diuretics
C. Thiazides
D. Potassium-sparing
E. Osmotic diuretic |
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Definition
A. Proximal convoluted tubule
B. thick ascending loop of henle
C. distal convoluted tubule
D. connecting tubule (late distal convoluted tubule) and collecting duct
E. PCT, descending loop of henle, collecting duct (late distal convoluted tubule) |
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Term
SAR: Carbonic Anhydrase inhibitors
Sulfamoyl group |
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Definition
| essential for in vitro carbonic anhydrase inhibitory activity and for diuresis in vivo. |
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Term
SAR: Carbonic Anhydrase inhibitors
sulfamoyl nitrogen |
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Definition
| must remain unsubstituted to retain both in vivo and in vitro activities. |
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Term
SAR: Carbonic Anhydrase inhibitors
moiety to which the sulfamoyl group is attached |
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Definition
| must possess aromatic character |
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Term
SAR: Carbonic Anhydrase inhibitors
derivatives with the highest lipid/water partition coefficients and the lowest pKa values |
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Definition
| have the greatest carbonic anhydrase inhibitory and diuretic activities |
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Term
| What position are the 2 sulfamoyl groups from each other in carbonic anhydrase inhibitors |
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Definition
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Term
| The ring of carbonic anhydrase inhibitor |
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Definition
| must be aromatic (not necessarily a benzene ring) |
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Term
| THE ACTIVATING GROUP ORTHO TO the sulfamoyl group on a carbonic anhydrase inhibitor can be |
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Definition
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Term
| Substitution on a carbonic anhydrase inhibitor with an amino (NH2) group |
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Definition
| Increase saluretic (excretion of salt or NaCl)activity, but decreases carbonic anhydrase inhibitory activity |
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Term
| One of the sulfamoyl groups of carbonic anhydrase inhibitors can be replaced with |
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Definition
| a similar electrophilic group that may increase diuretic potency but decrease carbonic anhydrase inhibitory activity |
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Term
| Prototype sulfonamide carbonic anhydrase that produces systemic acidosis after 2-4 days |
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Definition
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Term
| N-methyl substituted "acetazolamide" |
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Definition
| Methazolamide (Neptazane) |
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Term
| carbonic anhydrase that is the protype for site III (thiazide) diuretics |
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Definition
| Dichlorphenamide (Daranide) |
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Term
| SAR of site II (Loop) diuretics |
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Definition
The acidic group is essential for activity and must be para to the sulfamoyl group.
The sulfamoyl group (-SO2NH2) is essential for potency.
The activating group ortho to the sulfamoyl group can be a -Cl atom or –CF3 or a similar electron withdrawing group without decreasing activity or potency. |
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Term
5-sulfamoyl-2-aminobenzoic acid derivative
Loop diuretic |
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Definition
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Term
| 5-sulfamoyl-3-aminobenzoic acid derivative Loop diuretic (more potent b/c aminobenzoic acid is on 3 position instead of 2) |
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Definition
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Term
Loop diuretic that contain a sulfonylurea instead of a sulfonamide group
4-amino-3-pyridinesulfonylurea |
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Definition
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