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TUSM13 - Renal - Pharmacology of HTN
L19
11
Other
Graduate
09/09/2010

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Cards

Term
What are the major risks of untreated hypertension?
Definition
1) coronary thrombosis (MI)
2) heart failure
3) stroke
4) renal failure
Term
Describe Loop diuretics

site of action
mechanism
major actions
major side-effects
examples
Definition
1) thick ascending limb of the loop of henle
2) inhibition of Na/K/2Cl contransporter
3) increased distal tubular Na, dec. hypertonicity of interstitium, and less water reabsorption in collecting duct (i.e. diuresis and natriuresis). Induction of prostaglandins (i.e. dilation of afferent arteriole)
4) hypokalemia, hypocalcemia, hypomagnesia, metabolic alkalosis
5) furosemide, ethacrynic acid, bumetamide, torsemide
Term
Describe thiazides diuretics

site of action
mechanism
major actions
major side-effects
examples
Definition
1) distal tubule
2) inhibition of Na/Cl transporter; antihypertensive activity
3) diuresis; natriuresis (less powerful than loop-diuretics)
4) hypokalemia, metabolic alkalosis, hypercalcemia, hyponatremia
5) HCTZ; metolazone; chlorthalidone
Term
Describe potassium-sparing diuretics

site of action
mechanism
major actions
major side-effects
examples
Definition
1) distal segment of distal tubule
2) spironolactone: antagonizes aldosterone; triamterene, amiloride: inhibits sodium channels
3) decreased sodium reabsorption, and decreased potassium and acid loss
4) spironolactone, triamterene, amiloride
Term
Describe nitrates

site of action
mechanism
major actions
major side-effects
examples
Definition
1) vascular smooth muscle
2) stimulation of intracellular cyclic guanosine monophosphate production (venous > arterial)
3) reduce systolic, diastolic, and MAP
4) reflex tachycardia, flushing, headache *made up*, impractical due to short t1/2
5) nitroglycerin
Term
Describe Ca-CBs

site of action
mechanism
major actions
major side-effects
examples
Definition
1) vascular smooth muscle; cardiac myocytes, cardiac nodal tissue (SA, AV)
2) inhibition of L-type calcium channels, causing vasodilation (a>v), negative inotropy, negative chronotropy, negative dromotropy (esp @ AV node)
4)
5) dihydropyridines (smooth muscle selective): amlodipine, nifedipine; phenylalkylamine (myocardium): verapamil; benzothiazepine (intermediate): diltiazem
Term
Describe beta-blockers

site of action
mechanism
major actions
major side-effects
examples
Definition
1) cardiac nodal tissue, conducting system, contracting myocytes, vascular smooth muscle
2) beta-2 inhibition, causes decreased activation of adenylyl cyclase, and decreased activity of L-type Ca-Channels. This leads to negative chronotropy, inotropy, dromotropy, and lusitropy, and vasoconstriction
4) acute treatment is not very effective due to compensatory increase in systemic vascular resistance
5) propaanolol, metoprolol, atenolol
Term
Describe sympatholytics agents

site of action
mechanism
major actions
major side-effects
examples
Definition
1) peripheral at effector organ; ganglionic blockers at sympathetic gaanglia; centrally-acting sympatholytics drugs within the brain
2) centrally: activation of alpha-2 adrenoceptors; peripherally: competitive antagonists for alpha adrenoceptors (alpha1)
3) central: decrease HR and contractility and decrease SNA on vasculature; peripheral: dilate both arteries and veins (a>v)
4)
5) central: clinidine, methyldopa; peripheral: prazocin, doxazocin, terazocin
Term
Describe ACEi

site of action
mechanism
major actions
major side-effects
examples
Definition
1) vascular smooth muscle
2) inhibition of the formation of angiotensin II; inhibit bradykinin breakdown
3) decrease AII vasoconstriction; increase bradykinin levels; dilate arteries and veins; down regulate sympathetic adrenergic activity; promote urinary excretion of sodium and water (aldosterone release block); inhibit cardiac and vascular remodeling
4) dry cough
5) captopril; lisinopril; enalapril
Term
Describe angiotensin II receptor antagonist (ARBs)

site of action
mechanism
major actions
major side-effects
examples
Definition
1) vascular smooth muscle
2) block AII receptors
3) "vasodilation"; do not cause an increase in bradykinin
4) decreased cough, decreased angioedema
5) losartan; valsartan; irbesartan
Term
Describe Direct-Acting Vasodilators

site of action
mechanism
major actions
major side-effects
examples
Definition
1) arterial vessels
2) hyperpolarization w/ K channels; inhibit release of Ca; formation of NO
3) arterial vasodilation
4) reflex tachycardia
5) hydralazine
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