Antihypertensive Agents - Renin-angiotensin System Targeting Drugs Flashcards
How does the renin angiotensin aldosterone system work
What is the effect of angiotensin II
Increase sympathetic activity
Tubular Na+ Cl- reabsorption and K+ excretion. H2O retention
Stimulate adrenal gland cortex
Arteriolar vasoconstriction
Stimulate pituitary gland - antidiuretic secretion
What is angiotensinogen
What is angiotensin I
Decapeptide
What is angiotensin II
Octapeptide
What is angiotensin III
Heptapeptide
What are the drugs for the renin-angiotensin system
What else can ACE inhibitors inhibit apart from conversion of angiotensin I to II
Bradykinin metabolism to the inactive form - causing an increase of bradykinin
What is the effect of bradykinin increase
Explain mode of binding of angiotensin I to ACE
What is the role of zinc in ACE
Weaken the bind to hydrolysis the peptide link - removing 2 amino acids
What is the important amino acid for ACE inhibitor
Proline
Why did they want to prepare peptide similar to those of the snake venom
What is teprotide
What was the first ACE inhibitor antihypertensive agent
Captopril (capoten)
Explain ACE inhibitors
What are the 3 groups of ACEIs
Why were dicarboxylate containing inhibitors developed
Why is enalaprilate more potent than captropil
What is a disadvantage of enalaprilat
Explain what is enalapril (renitec)
What is the benefit of enalapril being a prodrug
Make ester to mask the polarity by removing one carboxylic bond and enhance absorption → then hydrolyzed into active form
Explain the phosphate containing ACE inhibitors
What is aliskiren
What is the advantage of renin inhibitors
What is losartan
Explain vasodilators
Arterial dilator drugs are used for what
Venous dilator drugs are used for what
List the examples of vasodilators
Nitrates (nitric oxide releasing agents)
K+ channel activation
K+ channel openers
Phosphodiesterase inhibitors
Calcium channel blockers
List the example of nitrate drugs
Nitroglycerin
Sodium nitroprosside
Give example of K+ channel activator
Hydralazine
Give example of K+ channel opener
Minoxidil (rogaine)
Give example of phosphodiesterase inhibitors
Sildehafil (viagra)
Give example of calcium channel blockers
Hydropyridines ( nifedipine)
Explain nitroglycerine
Explain the nitric oxide mediated vasodilation
Explain hydralazine and sodium nitroprusside
What is the indication of nitroprusside
Hypertensive emergency
What is the mechanism of hydralazine and sodium nitroprusside
What is the toxicity of hydralazine and sodium nitroprusside
Explain minoxidil
Why is the side effect of minoxidil
Explain calcium channel blockers
Explain dihydropyridines
What is the prototype of dihydropyridines
Nifedipine
Explain verapamil and its use
