Targets for antihypertensive drugs Flashcards
Renin cleaves what?
Angiotensinogen to angiotensin 1
Angiotensin converting enzyme is inhibited by what?
ACE inhibitors
Bradykinin causes what in the vascular system
Vasodilation
Which causes more vasoconstriction? Angiotensin 2 or 3?
Angiotensin 2
Angiotensin 2 affects which angiotensin receptors?
AT receptor 1 and 2
Angiotensin 3 affects which Angiotensin receptors?
Angiotensin receptor 1 and 2
Effect of NaCl reabsorption at Macula Densa?
Inhibits Renin release
Effect of Decrease in blood pressure in pre-glomerular vessels?
Inhibit of renin release
Activation of B1 Adrenergic receptors on JGCs causes what?
Causes renin release
Where are angiotensin 2 type 1 receptors located? (5)
Blood vessels, brain, adrenals, kidney, and heart
Activation of AT1 receptors does what?
Increase BP
Result of angiotensin 2 on altered cardiovascular structure?
Vascular and Cardiac Hypertrophy and remodeling
Inhibitors of renin angiotensin system?
Direct Renin inhibitors
ACE inhibitors
Angiotensin receptor blockers
Suffix that indicates an ACE inhibitor drug?
PRIL
Besides angiotensin what else do ACE inhibitors inhibit?
Bradykinin
What class of drugs would interfere with Bradykinin mediated vasodilation?
NSAIDS
Characteristics of Captopril? (4)
Active site inhibitor
Short half life
Absorption reduced by food
Altered taste, rash
Largest class of ACE inhibitors?
Dicarboxyl containing ACE inhibitors
Characteristics of Enalopril? (3)
It’s a pro-drug
Long half life
Parenteral administration
How are ACE inhibitors cleared from the body? Exception?
Renal
Moexipril cleared via hepatic
How do ACE inhibitors compete?
Competitively
Characteristics of Lisinopril? (3)
Not a prodrug
Lysine derivative of enalaprilat
Half life of 12 hours
Characteristics of Fosinopril (3)
Prodrug
Hepatic metabolism with excretion in urine and bile
Half life of 11.5 hours
Clinical uses of ACE inhibitors? (4)
Hypertension
Left Ventricular systolic dysfunction
Myocardial infarction
Diabetic Nephropathy
Main adverse effects of ACE inhibitors? (3)
Acute renal failure
Dry cough
Skin rash
When do you not want to use ACE inhibitors?
Pregnancy Renal insufficiency (causes neutropenia)
Antacids have what effect on ACE inhibitors?
Reduce bioavailability
NSAIDS have what effect on ACE inhibitors?
Reduce effectiveness
ACE inhibitors increase plasma levels of what?
Digoxin and lithium
ACE inhibitors can interact with what supplement?
K+ supplements
What are the Angiotensin 2 Type 1 receptor antagonists known as?
The “Sartans”
Do Angiotensin 2 Type 1 receptor antagonists affect Bradykinin system?
No
Clinical uses for Angiotensin 2 Type 1 Receptor Antagonists? (4)
Hypertension
Congestive Heart Failure
Diabetic Nephropathy
Stroke prophylaxis
Adverse effects of A2T1R?
Hypotension
Hyperkalemia
Teratogenic potential (2nd and 3rd trimester)
Side effect of Direct Renin inhibitor?
Diarrhea
Effect of high fat meals on direct renin inhibitor absorption?
Decrease in absorption
What are direct renin inhibitors used to treat?
Hypertension
Who do you not want to you renin inhibitors on?
Pregnant
Nursing mothers
