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Antihypertensives & Antilipidemics
N/A
108
Pharmacology
Professional
04/03/2011

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Cards

Term
goal BP for uncomplicated HTN
Definition
<140/90
Term
goal BP for HTN + DM
Definition
<130/80
Term
goal BP for HTN + chronic renal disease
Definition
<130/80
Term
stage 1 HTN: initial drug choices for pts without compelling indications
Definition
thiazide-type diuretics for most

may consider ACE inhibitor, ARB, BB, CCB, or combo
Term
stage 1 HTN
Definition
systolic 140-159
diastolic 90-99
Term
stage 2 HTN
Definition
systolic 160 or higher
diastolic 100 or higher
Term
stage 2 HTN: initial drug choices for pts without compelling indications
Definition
2-drug combo for most (usually thiazide-type diuretic and ACE inhibitor, ARB, BB, or CCB)
Term
initial drug choices for HTN pts with compelling indications (past MI, etc.)
Definition
other antiHTN drugs as needed
Term
general approach based on JNC-7
Definition
1. thiazides
2. ACE inhibitor
3. ARB
4. beta blocker
5. calcium channel blocker
6. alpha blocker
7. vasodilator
Term
mechanism of action of diuretics in HTN
Definition
acute effects: Na+ and H20 loss-->decreased blood volume-->decreased CO-->decreased BP

chronic effects: Na+ loss causes decreased responsiveness of arterioles to NE-->decreased arteriolar resistance
Term
When do you not choose a thiazide first for HTN?
Definition
renal disease
Term
Use _________ diuretics for HTN in renal insufficiency pts.
Definition
loop
Term
Thiazides are very effective in what populations?
Definition
elderly and African Americans
Term
common side effects of thiazides
Definition
hypokalemia
hyponatremia
Term
less common side effects of thiazides
Definition
high serum uric acid
hypertriglyceridemia
DM exacerbation
Term
ACE inhibitors mechanism of action
Definition
block conversion of angiotensin I to angiotensin II
Term
effects of ACE inhibitors
Definition
decrease preload (venous dilation)
decrease afterload (arteriole dilation)
decrease BP
Term
ACE inhibitors do/do not have effect on heart rate.
Definition
do not
Term
Renin comes from...
Definition
JG cells
Term
Angiotensin I comes from...
Definition
liver
Term
ACE inhibitors are preferred for...
Definition
high plasma renin
diabetes mellitus (reduces proteinuria)
CHF (decreases mortality)
Term
In addition to being antihypertensive, these drugs slow changes in cardiac shape that is a key problem in CHF.
Definition
ACE inhibitors ("prils")
Term
advantages of ACE inhibitors
Definition
-predictable, typically mild, dose-related side effects
-blunt hypokalemia caused by diuretics
-little orthostatic hypotension or SNS activation
-no effect on TGs or cholesterol
Term
ACE inhibitors side effects
Definition
cough, initial dose hypotension, skin rashes, neutropenia, acute renal failure in renal artery stenosis, angioedema, AAs and elderly may not respond well, hyperkalemia possible
Term
Why do ACE inhibitors cause cough?
Definition
elevated bradykinin in the lungs
Term
ACE inhibitors contradindications
Definition
pregnancy (2nd and 3rd trimester)
Term
ARB mechanism of action
Definition
block AT1 subtype of the angiotensin II receptors
Term
ARBs have a greater/lesser chance of causing angioedema.
Definition
lesser
Term
ARB contraindications
Definition
pregnancy
Term
aliskiren
Definition
direct renin inhibitor
Term
beta 1 stimulation causes
Definition
increased HR
increased contractility
increased AV conduction
increased electrical excitability
increased renin release
Term
beta 2 stimulation causes
Definition
bronchodilation
arteriole dilation
relaxation of the uterus
insulin release
increased glycogenolysis
Term
beta blockers mechanism of action
Definition
-decreases heart contractility (negative inotrope) reducing O2 requirements of myocardial cells
-decreases SA node firing rate (negative chronotrope)
Term
beta blockers therapeutic effects
Definition
-decreased HR
-decreased myocardial oxygen demand
-decreased angina
-fewer rhythm disturbances
-decreased renin release
Term
How do beta blockers decreased total peripheral resistance?
Definition
block of renin release through block of beta 1 receptors
Term
propranolol
Definition
non-selective beta blocker

cheap, efficacious, extensive history
Term
propranolol contraindication
Definition
asthma, acute CHF, AV conduction problems
Term
propranolol side effects
Definition
impotence
impairs recovery from hypoglycemia
masks symptoms of hypoglycemia
Term
Beta blockers used to treat hypertension have been suggested to _________________________ in pateints with essential hypertension wihtout known CAD and CHF.
Definition
increase the risk of cardiovascular events and death
Term
beta 1 selective blockers (metoprolol, atenolol) are preferred in individuals who also have...
Definition
peripheral vascular disease
Term
nebivolol
Definition
beta 1 selective blocker that is also a vasodilator by the endothelial L-arginine/NO pathway
Term
drug that has the highest cardioselectivity of any currently available beta blocker
Definition
nebivolol
Term
Which drug has fewer respiratory effects and less bradycardia than other beta blockers?
Definition
nebivolol
Term
beta blocker side effects
Definition
AV block, severe bradycardia, bronchospasm, respiratory distress, exacerbation of CHF and pulmonary edema, delay of recovery from hypoglycemia, hypertriglyceridemia, decreased HDL
Term
alpha blocker side effect
Definition
orthostatic hypotension
Term
nifedipine
Definition
calcium channel blocker
Term
calcium channel blocker mechanism of action
Definition
decreased calcium influx results in smooth muscle relaxation which causes vasodilation
Term
Calcium channel blockers are relatively selective for...
Definition
vascular smooth muscle Ca channels
Term
dihydropyridine agents
Definition
nifedipine
felodipine
amlodipine
nicardipine
Term
What is the only calcium channel blocker that is okay to use in CHF pts?
Definition
amlodipine
Term
Why are calcium channel blockers less preferred than ACE inhibitors or ARBs?
Definition
higher profile of side effects related to vasodilation
Term
What is a specific use for calcium channel blockers?
Definition
Prinzmetals angina
Term
calcium channel blocker side effects
Definition
headache, flushing, orthostatic problems, peripheral edema
Term
clonidine
Definition
central adrenergic agonist
alpha 2 agonist
Term
clonidine side effects
Definition
drowsiness, dry mouth, depression, rebound hypertension (can elicit HTN crisis)
Term
first line HTN drug during pregnancy
Definition
methyldopa
Term
methyldopa side effects
Definition
dry mouth, sedation, fatigue, depression, nightmares, sexual dysfunction, hemolytic anemia, hepatitis (rare)
Term
antiHTN for coronary heart disease
Definition
beta blockers
ACE inhibitors
Term
antiHTN for CHF
Definition
ACE inhibitors
beta blockers
ARBs
spiranolactone
Term
antiHTN for diabetics
Definition
ACE inhibitors
ARBs
Term
antiHTN for renal insufficiency
Definition
ACE inhibitors
ARBs
Term
hypertensive emergency
Definition
end-organ damage is present or progressive

BP control should be achieved within 1 hr
Term
hypertensive urgency
Definition
no obvious end-organ damage

BP control should be achieved within 24 hrs
Term
treatment of hypertensive crisis
Definition
-get diastolic down to 100-110, then move to normal over the next few days
-avoid excessive and rapid decrease in BP
Term
vasodilators
Definition
nitroprusside
labetalol
fenoldopam
Term
precautions with vasodilator therapy
Definition
-overly aggressive therapy is associate with severe hypotensive problems, including insufficient circulation to the CNS
-insufficient therapy is associated with end-organ damage, including stroke
Term
vasodilator mechanism of action
Definition
decrease BP by decreasing systemic vascular resistance
Term
nitroprusside uses
Definition
hypertensive emergencies
surgery (controlled hypotension)
Term
nitroprusside side effects
Definition
excessive hypotension
cyanide/thiocyanate toxicity
Term
Which vasodilator is a D1 agonist?
Definition
fenoldopam
Term
fenoldopam indications
Definition
in-hospital, short-term (up to 48 hrs) management of severe hypertension when rapid, but quickly reversible, emergency reduction of BP is clinically indicated

ex: malignant HTN with deteriorating end-organ function
Term
What vasodilator is a beta blocker with intrinsic activity?
Definition
labetalol
Term
labetalol indications
Definition
hypertensive crises
pre-eclampsia
pheochromocytoma
Term
major risk factors that modify LDL goals
Definition
cigarette smoking
HTN
low HDL
family history of premature CHD
age
Term
high risk
Definition
CHD or CHD risk equivalents
Term
moderately high risk
Definition
2+ risk factors
10 year risk 10-20%
Term
moderate risk
Definition
2+ risk factors
10 year risk <10%
Term
lower risk
Definition
0-1 risk factor
Term
goal LDL for high risk
Definition
<100
Term
goal LDL for moderately high risk and moderate risk
Definition
<130
Term
goal LDL for lower risk
Definition
<160
Term
VLDL contains...
Definition
triglycerides
Term
High levels of VLDL increase risk of...
Definition
pancreatitis
Term
Which cholesterol makes the greatest contribution to coronary atherosclerosis?
Definition
oxidized LDL
Term
Which cholesterol promotes cholesterol removal?
Definition
HDL
Term
statins derived from fungi
Definition
lovastatin
pravastatin
simvastatin
Term
statin mechanism of action
Definition
inhibition of HMG-CoA reductase
Term
statin indications
Definition
elevated cholesterol of all types (particularly effective in lowering LDL)
Term
Statins increase/decrease LDL receptors in the liver.
Definition
increase
Term
What do you often see with statins in addition to lowered LDL?
Definition
small decrease in TGs and small increase in HDL
Term
"optional" goal for LDL in pts with 2 risks
Definition
<70
Term
statin side effects
Definition
hepatic damage, peripheral neuropathies
Term
What do you have to watch for with statins?
Definition
myalgia, myopathy, and rhabdomyolysis (esp. when combining with niacin, fibrate drugs, or erythromycin)
Term
statin contraindications
Definition
pregnancy
Term
Which statins cross the BBB and therefore may cause sleep disturbances?
Definition
lovastatin
simvastatin
Term
Why can't you drink grapefruit juice when taking a statin?
Definition
furanocoumarins bind to and deactivet the CYP3A4 enzyme causing possible increased drug effects due to decreased metabolism
Term
Which statin does the grapefruit juice stipulation not apply to?
Definition
pravastatin
Term
niacin mechanism of action
Definition
inhibits VLDL secretion which leads to decreased VLDL, decreased LDL, and increased HDL
Term
niacin indications
Definition
any lipoprotein disorder, particularly mixed hyperlipidemia with elevated TGs

DOC for decreasing TG levels in pts at risk for pancreatitis
Term
niacin side effects
Definition
itching, flushing, unpleasant sensation of being warm, GI distress, hyperuricemia, hepatotoxicity, carb intolerance
Term
fibrate derivatives
Definition
gemfibrozil
fenofibrate
Term
fibrate derivatives mechanism of action
Definition
increased activity of lipoprotein lipase
Term
fibrate derivatives therapeutic effects
Definition
decrease VLDL formation in the liver leading to decreased TGs

modest reduction in LDL, more impressive rise ind HDL
Term
fibrate derivative indications
Definition
reduction of TGs when VLDL is very high or when IDL is elevated

do NOT use if VLDL is not elevated!
Term
gemfibrozil contraindication
Definition
pt with gall bladder problems (causes lithiasis)
Term
bile acid binders mechanism of action
Definition
enhanced excretion of bile acids, leading to increased conversion of cholesterol to bile acids in the liver

loss of cholesterol triggers up regulation of LDL receptors in the liver; therefore, decreased LDL
Term
ezetimibe mechanism of action
Definition
inhibits absorption of phytosterols and cholesterol
Term
omega-3-fatty acids mechanism of action
Definition
reduce TG and VLDL synthesis in the liver
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