Antihypertensives - diuretics and vasodilators (exam 3) Flashcards
thiazide diuretics
chlorthalidone
HCTZ (esidrix)
metolazone (zaroxolyn)
loop diuretics
bumetanide
furosemide (lasix)
torsemide (demadex)
K sparing diuretics
amiloride (midamor)
triamterene (dyrenium)
eplerenone (Inspra)
spironolactone (aldactone)
loop diuretic MOA
act on thick ascending limb
inhibits NA/K/2CL carrier in the luminal membrane
thiazide diuretics MOA
bind to the Cl site of the Na/Cl co transport system in the distal convoluted tubule
loss of Na and Cl in urine
K sparing diuretics MOA (amiloride and triamterene)
excretion of sodium and water while preventing the loss of potassium in the urine
direct vasodilators examples
hydralazine (apresoline)
minoxidil (loniten)
nitroprusside (nitropress)
direct vasodilators MOA
reduce peripheral resistance directly by relaxing smooth muscle cell layer in arterial vessels
dihydropyridines have more effect on __________ and less effect on _____________
vasodilation
heart function
non-dihydropyridines have more effect on ____________ and less effect on ________________
heart function
vasodilation
ADRs of thiazide diuretics
hyponatremia
hypercalcemia
hypokalemia
metabolic alkalosis (inc pH)
hyperglycemia
hyperuricemia
hyperlipidemia
____________ in 1.5-2x more potent at lowering blood pressure compared to ____________ and may be preferred
chlorthalidone
HCTZ
K sparing diuretics MOA (eplerenone and spironolactone)
antagonist at aldosterone receptor which reduces Na/K exchange in distal convoluted tubule
leads to increased Na excretion and K reabsorption
Hydralazine MOA
directly relaxes arteriolar smooth muscle by reduction in intracellular calcium
direct vasodilators ADRs
strong reflex tachycardia
increased fluid retention
peripheral edema
Minoxidil MOA
opens K channels causing hyper polarization and arterial relaxation
Minoxidil increases
blood flow to skin, skeletal muscle, GI tract and the heart
Minoxidil is used to promote
hair growth by increasing nutrient flow to hair follicles
Nitroprusside MOA
prodrug that reacts with sulfhydrl groups on RBCs to produce nitric oxide –> vasodilation
Nitroprusside is given as an IV infusion when
rapid BP reduction is required (hypertensive crisis, acute decompensated HF)
Nitroprusside includes a risk of
cyanide toxicity
antidotes for cyanide toxicity from nitroprusside
hydroxocobalamin, sodium nitrate or sodium thiosulfate
symptoms of cyanide toxicity
metabolic acidosis
dyspnea
bradycardia
confusion
flushing
reflex tachycardia occurs due to
baroreceptors
baroreceptors
specialized neurons found in the heart and arteries
detects changes in BP
activate when BP is high
vasodilators decreased blood pressure, leading to
less activation of baroreceptors
less suppression of the SNS
increased release of NE/E at the heart leading to tachycardia
drugs that cause vasodilation can cause ____________
why?
peripheral edema (swelling of lower legs and feet due to fluid accumulation)
drugs that vasodilator the arterial system and NOT the venous system do this
vasodilation of the arterial system without concurrent venous vasodilation leads to _______________ which leads to ___________________
increased capillary pressure
fluid extravasation and edema
drugs that cause peripheral edema include
CCBs and direct vasodilators
how can peripheral edema be lessened?
add on a ACEI or ARB since they cause venous vasodilation
CCB DHPs
block L-type calcium channels on arterial smooth muscle
causes vasodilation
CCB non-DHPs
verapamil - Ca channels on cardiac tissue (dec HR and contractility)
diltiazem - arterial smooth muscle and cardiac tissue
ADRs of DHPs
reflex tachycardia
peripheral edema
dizziness
flushing
rare ADR of DHPs and non-DHPs
gingival hyperplasia
ADRs of verapamil
bradycardia
atrioventricular block
constipation
ADRs of diltiazem
similar to DHPs and verapamil but milder
are calcium channel blockers first line agents for HTN?
only DHPs
not non-DHPs due to side effects
Non-DHPs should be avoided in combination with
beta blockers due to additive bradycardia
CCBs absorption/distribution
hepatic first pass metabolism by CYP3A4
3A4 inhibitory potential of CCBs
verapamil and diltiazem (moderate inhibitors) > amlodipine > other DHPs
amlodipine has a _________ half life and diltiazem and verapamil have a ___________ half life
long
shorter
about 20% of patients will require
more than 3 medications
majority of patients will require ________________ to reach BP goals
more than 1 medication