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Pharmacology Exam 4: HTN
pharm exam 4: HTN
193
Pharmacology
Graduate
03/24/2011
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Term
Goal bp for uncomplicated hypertension:
 Definition
<140/90
Term
Goal bp for HTN + Diabetes Mellitus:
 Definition
<130/80
Term
Goal bp for HTN + chronic renal disease:
 Definition
<130/80
Term
JNC7, ADA, NFK, and ISHIB all urge physicians to bring patients to new even lower blood pressure goals via ___ of agents and use of ___ drug therapy when appropriate.
 Definition
- titration
- combination
Term
FYI: JNC 7= Joint National Committee on Prevention, Detection, Evaluation and Treatment of High Blood Pressure Seventh Report
 Definition
Term
According to JNC 7, in people older than 50 years, ___ ___ ___ greater than ___ is a much more important cardiovascular disease risk factor than diastolic blood pressure.
 Definition
- systolic blood pressure over 140 mmHg
Term
According to JNC7, the risk of CVD beginning at 115/75 mmHg doubles with each increment of ___ mmHg.Individuals who are normotensive at age 55 have a ___ lifetime risk for developing hypertension.
 Definition
20/10
90%
Term
According to JNC7, individuals with a systolic blood pressure of ____ mmHg OR a diastolic blood pressure of ____mmHg should be considered as ___ and require health-promoting lifestyle modifications to prevent CVD.
 Definition
120-139
80-89
prehypertensive
Term
According to JNC7, ____ ____ should be used in drug treatment for most patients with uncomplicated hypertension, either alone or combined with drugs from other classes. Certain high-risk conditions are compelling indications for initial use of of antihypertensive drug classes (ACEI, angiotensin receptor blockers, beta blockers, and calcium blockers).
 Definition
- thiazide-like diuretics
Term
According to JNC7, most patients with HTN will require two or more antihypertensive medications to achieve a goal blood pressure of below ____ or ___ if pt also has DM or chronic kidney disease.
 Definition
140/90
130/80
Term
According to JNC7, the most effective therapy prescribed by the most careful physician will control HTN only if the patient is motivated. Motivation improves when patients have positive experiences with, and trust in the clinician. Empathy builds trust and is a potent motivator. In presenting the above guidelines JNC recognizes that the responsible physician's judgement remains paramount.
 Definition
Term
Non-drug treatment of HTN:
 Definition
Diet modifications:
- decrease weight, fat, and cholesterol
- decrease sodium
- decaffeinate the diet (mainly an acute effect)

Behavior modifications:
- aerobic exercise
- avoid tobacco
- decrease alcohol intake
Term
If advise lifestyle modifications to lower blood pressure, give it ____ to see effect before follow up.
 Definition
6-8 weeks
Term
According to JNC7, Stage 1 HTN is a systolic bp b/w ____ or a diastolic bp b/w ____. If there are no other compelling indications, treat with ____ ___ for most. May consider ACEI, ARB, BB, CCB, or combination as well.
 Definition
- 140-159
- 90-99
- thiazide like diuretic for most
Term
According to JNC7, Stage 2 HTN is a systolic greater than or equal to ___ and a diastolic greater than or equal to ___. If there are no other compelling indications treat with __ __ __ for most, usually a thiazide-like diuretic and ACEI, or ARB, or BB, or CCB.
 Definition
- 160
- 100
- 2-drug combination therapy
Term
If start patient on Thiazides, give them ___ months to work, then re-check, and add ACEI if necessary. But if patient is in stage 2 HTN can start both drugs initially.
 Definition
1-2 months
Term
ACE Inhibitors result in increased bradykinin in the lungs leading to __ __.
 Definition
dry cough
Term
As recommended by JNC 7, hypertension treatment should start with lifestyle modifications. If the patient is not at goal BP of <140/90 mm Hg (<130/80 mm Hg for those with diabetes or chronic kidney disease), pharmacologic therapy should be initiated. Initial drug choices for patients without compelling indications should be a thiazide diuretic for most patients with stage 1 hypertension. Typically, combination therapy with 2 drugs is required for stage 2 hypertension. When use of a single drug fails to achieve the BP goal, addition of a second drug from a different class should be initiated. A 2-drug combination usually consists of a thiazide-type diuretic plus an ACEI, an ARB, a -blocker, or a CCB.
Specific antihypertensives are designated for compelling indications (ie, HF, post-MI, high coronary artery disease [CAD] risk, diabetes, etc.).
 Definition
Term
General approach for sequence of drug administration for HTN based on JNC-7:
 Definition
Thiazides
ACE-I
ATII blockers (ARBS)
Beta blockers
Calcium channel blockers
Alpha blockers
Vasodilators
Term
___ __ and ___ patients respond well to thiazide treatment of blood pressure.
 Definition
African American and elderly
Term
mechanism of action of diuretics in HTN treatment:
 Definition
- acute effects: sodium and water loss> decreased blood volume> decreased CO> decreased bp

- chronic effects: sodium loss> decreased responsiveness of arterioles to NE> decreased arteriolar resistance
Term
Usually start with thiazide diuretic first like HCTZ for HTN tmt, less potential for harm.
 Definition
Term
Loop diuretics are used for hypertension with __ __ and used __ for ___ ___.
 Definition
- renal insufficiency
- i.v. for hypertensive emergency
Term
Potassium sparing diuretics are used in combination with thiazides or loops for treatment of HTN.
 Definition
Term
Advantages to Thiazide use for HTN tmt:
 Definition
- sometimes effective alone
- combat sodium retention- vasodilators, alpha-blockers
- potentiate effects of other anti-hypertensive drugs
- African Americans and elderly respond well
- minimal hypotension
- loop diuretics are effective in renal failure
Term
Thiazide diuretics:
 Definition
hydrochlorothiazides
chlorthalidone

12.5-25mg daily
Term
Thiazide side effects:
 Definition
common:
- hypokalemia
- hyponatremia

less common:
- high serum uric acid> gout
- hypertriglyceridemia
- DM exacerbation (make you retain glucose)
Term
ACE Inhibitors mechanism of action:
 Definition
- block conversion of angiotension I to II> decrease angII> decrease aldosterone release> decreased breakdown of bradykinin> decrease SNS (little reflex tachycardia)> decreased preload, decreased afterload> decreased blood pressure
Term
ACE inhibitors do NOT effect ____ ___. They decrease preload, which decreases __ __, and decrease afterload/resistance meaning they increase blood flow.
 Definition
- do NOT effect heart rate
- stroke volume
Term
BP= CO X TPR

CO= SV X HR
 Definition
Term
formula for blood pressure:
 Definition
BP = CO x TPR
Term
formula for blood pressure:
 Definition
BP = CO x TPR
Term
Renin is secreted by the ___ ___ in the ___ in response to decreased ___. Renin cleaves __ to make ___ _. Then ___ cleave __ _ to make ___ _, which feedbacks and inhibits renin release.
 Definition
- juxtaloglomerular apparatus
- kidney
- perfusion
- angiotensenogen
- angiotensin I
- ACE
- angiotensin I
- angiotensin II
Term
The "prils" are ___ ___.
 Definition
ACE inhibitors
Term
prototype ACE inhibitor:
 Definition
captopril= prototype

(also Enalapril, Lisonapril, and others)
Term
Uses of ACE inhibitors/"prils" in HTN tmt (4):
 Definition
1. Essential hypertension (efficacious and relatively minimal side effects)
2. Preferred for high plasma renin
3. Diabetes mellitus (preferred anti-hypertensive b/c reduces proteinuria)
4. CHF (preferred anti-hypertensive b/c reduces mortality)
Term
what is the preferred antihyptensive for high plasma renin ?
 Definition
ACE inhibitor
Term
what is the preferred anti-hypertensive for Diabetes Mellitus and why?
 Definition
- ACE inhibitors because the decrease proteinuria
Term
what is the preferred anti-hypertensive for CHF and why?
 Definition
- ACE inhibitors
- decrease mortality
- slow changes in cardiac shape (cardiac remodeling), which is big problem with CHF
Term
Advantages to ACE inhibitors:
 Definition
- predictable, mild, dose-related side effects
- blunt hypokalemia caused by other diuretics
- little orthostatic hypotension or SNS activation
- no effect on triglycerides or cholesterol
Term
ACE-I Disadvantages:
 Definition
- cough
- initial dose hypotension, especially if hypvolemic
- skin rash/neutropenia (captopril may be worse with this)
- acute renal failure in renal artery stenosis
- may cause hyperkalemia (in combinations with other drugs that promote this)
- ANGIOEDEMA (this is the serious life threatening side effect of ACE-I)
- African Americans and elderly may not respond well
- contraindicated in the 2nd and 3rd pregnancies> fetal malformations, hypotension, renal failure
Term
Contraindication for ACE-I:
 Definition
- renal failure or renal artery stenosis
- 2nd or 3rd trimester pregnancy
Term
ACE-I inhibitors cause a dry non-productive irritating cough in 3-15% of patients due to elevated ___ in the lungs. This is/is not seen with ARBs.
 Definition
- bradykinin
- is not

So if patient gets the cough with ACE-I, switch them to ARBs
Term
In renal artery stenosis, ___ levels are high. ACE-I will ___ the efferent arteriole, resulting in even ___ pressure in the glomerulus.
 Definition
- renin
- dilate
- lower
Term
A life threatening allergic response to ACE-I is :
 Definition
angioedema

If patient gets this, take them off ACE-I and send them to ER. They are never to be on ACE-I again.
Term
what does ARB stand for?
 Definition
Angiotensin II Receptor Blockers (or Antagonists)
Term
ARBs all end in:
 Definition
"-sartan"

Losartan, Valsartan, and several others
Term
ARBs block the ___ __ of the ___ __ receptors.
 Definition
- AT1 subtype of the ATII receptors
Term
The effects, uses, and side effects of ARBs are similar to those of ACE-I, but ARBs do not cause ___ and are less likely to cause ___. ARBs should be avoided during ___. Generally ACE-I are tried before going to ARBs.
 Definition
- do not cause cough
- less likely to cause angioedema
- pregnancy
Term
ACE-I are generic and cheaper than ARBs.
 Definition
Term
____ is a direct renin inhibitor, meaning it blocks the secretion of renin, so not a lot of ____ is made. It causes a __% decrease in plasma renin activity which ultimately leads to decreased blood pressure.
 Definition
- Aliskiren
- angiotensin
- 50-80%
Term
Aliskiren:
 Definition
- antihypertensive: direct renin inhbitor that blocks secretion of renin so not much angiotensin is made
Term
Aliskiren is slow on, slow off. It has an accumulation half life of ___ hours and takes ___ days to achieve a steady state.It has an elimination half life of ___ hours. __% is excreted by the kidneys. It is metabilized by ____. It does NOT induce or suppress CYP450 and has NO effect on the QT interval.
 Definition
- 24 hours
- 7-8 days
- 48 hours
- 25%
- CYP 450-3A4
Term
Aliskiren adverse effects:
 Definition
- discontinuation
- cough
- angioedema
- hyperkalemia
- diarrhea/GI side effects
- do NOT use in pregnancy
Term
Beta receptors and HTN:
Beta 1 adrenergic receptor stimulation causes:
 Definition
- increased heart rate
- increased contractility
- increased AV conduction
- increased electrical excitability of heart
- increased renin release
Term
Beta 2 adrenergic receptor stimulation causes:
 Definition
- bronchodilation
- arteriole dilation
- uterine relaxation
- insulin release
- increased glycogenolysis
Term
beta blockers end in :
 Definition
"-olol"
Term
Beta blockers decrease heart ___ ( a negative __ effect), which reduces ___ requirements of myocardial cells. Beta blockers also decrease __ ___ firing rate, a negative ___ effect.
 Definition
- decrease heart contractility
- ionotropic
- oxygen
- AV node
- chronotropic effect
Term
summary of beta blockers mechanism of action:
 Definition
- decrease contractility= ionotropic effect> decrease oxygen requirements of myocardial cells
- decreases AV node firing= chronotropic effect
Term
Therapeutic effects of beta blockers (5):
 Definition
- decreased heart rate
- decreased myocardial oxygen demand
- decreaed angina
- fewer rhythm disturbances
- decreased renin release
Term
beta blockers decrease the release of __.
 Definition
renin
Term
Beta blocker prototypes:
 Definition
- Propanolol
- Atenolol
- Metoprolol

PAM is on beta blockers.
Term
4 main effects of beta blockers:
 Definition
- decreased contractility
- decreased heart rate
- decreased cardiac output
- decreased total peripheral resistance
Term
Beta blockers inhibit the release of ___ by blocking ___ ___, this ___ total peripheral resistance.
 Definition
- renin
- beta 1 receptors
- decreases
Term
Propanolol is a ____ ___ ___ used to treat __. . What are some advantages of this drug
 Definition
- non-selective beta blocker
- HTN
- cheap, efficacious, extensive history
Term
Disadvantages of Propanolol:
 Definition
- CONTRAINDICTED IN ASTHMA, COPD, AND ACUTE CHF (note: indicated in stable CHF
- impotence
- inhibits glycogenolyis, impairs recovery from hypoglycemia
- blocks muscle tension and tachycardia typically seen with hypoglycemia (masks warnings to Diabetics of low blood sugar)
Term
Beta blockers as treatment for patients with essential hypertension w/o known CHF or CAD actually ___ risk of ___ ___ and ___. Patients with CAD and CHF and HTN do better on these.
 Definition
- increases
- cardiovascular events and death
Term
don't put pt with essential htn who does not have CAD or CHF on beta blockers.
 Definition
Term
Beta 1 selective blockers:
 Definition
- Metoprolol
- Atenolol
Term
Beta 1 selective blockers, like ___ or ___, are preferred for tmt of hypertension in patient with __ ___ __.
 Definition
- Metoprolol
- Atenolol
- peripheral vascular disease
Term
___ is a newer beta-1 selective agent that was recently approved. It is a cardiospecific agent which is also a ___ by the ___ ____ ___ _____.
 Definition
- Nebivolol
- vasodilator
- endothelial L-arginine/NO pathway
Term
Nebivolol has the highest ___ of any beta blocker, exhibiting a 321-fold higher selectivity for the beta 1 receptor over the beta 2 receptor.
 Definition
- cardioselectivity
Term
Nebivolol has fewer ___ ___ and less ___ than other beta blockers.
 Definition
- fewer respiratory effects
- less bradycardia
Term
Nebivolol is what type of drug:
 Definition
- cardioselective beta 1 blocker that is also a vasodilator via the endothelial L-arginine/NO pathway
Term
side effects of beta blockers:
 Definition
- AV block
- severe bradycardia
- BRONCHOSPASM AND RESPIRATORY DISTRESS
- EXACERBATION OF CHF AND PULMONARY EDEMA
- delay of recovery from hypolgycemia
- hypertriglyceridemia and decreased HDL cholesterol
Term
alpha blockers are NOT first, second, or third line treatments for HTN.
 Definition
Term
Prototype calcium channel blocker:
 Definition
nifedipine
Term
calcium channel blockers end in:
 Definition
"-ipine"
Term
calcium channel blockers decrease ___ influx resulting in __ ___ ___ which decreases __ ___ __. these drugs are relatively selective for ___ ___ ___ calcium channels
 Definition
- calcium
- smooth muscle relaxation
- decreases peripheral vascular resistance
- vascular smooth muscle
Term
Dihydropyridine agents/calcium channel blockers:
 Definition
- Nifedipine
- Nicardipine
- Felodipine
- Amlodipine

Never Never Feed Animals Calcium.

Note these are all the dihyropyridine calcium channel blockers that act in the peripheral vasculature and can be used for angina and HTN.

There are also non-dihydropyridine calcium channel blockers like Verapamil and Diltiazem that work in the heart muscle itself and are used for rate/rhythm control with arrhythmias.
Term
What dihyropyridine agent/calcium channel blocker is ok for CHF patient?
 Definition
Amlodipine
Term
Calcium channel blocker/dihydropyridine uses:
 Definition
- hypertension
- angina (Prinzmetal variant angina)
Term
Why are calcium channel blockers less preferred than ACE-I and ARBs?
 Definition
- calcium channel blockers have a higher profile of side effects related to vasodilation
Term
Advantages of calcium channel blockers:
 Definition
- efficacious
- less side effects than many older antihypertensives
Term
Disadvantages of calcium channel blockers:
 Definition
- headache
- flushing
- orthostatic problems
- peripheral edema/swelling
Term
Central adrenergic agonists, like ___, act on the ___ and are ___ __ ___.
 Definition
- Clonidine
- CNS (brain)
- alpha 2 agonists
Term
Adverse effects of Clonidine, a central adrenergic agonist:
 Definition
- drowsiness
- DRY MOUTH
- depression
- REBOUND HYPERTENSION IF TAKEN OFF TOO FAST> CAN LEAD TO HYPERTENSIVE CRISIS, SO STOP SLOWLY AND TITRATE DOWN (THIS IS OFTEN A BOARD QUESTION)
Term
Clonidine has to be taken at least __ times a day, or a __ can be worn.
 Definition
- 3
- patch
Term
Methyldopa is not a first line HTN treatment, except in ___ (BOARD QUESTION).
 Definition
pregnancy
Term
To treat HTN in pregnancy, what should you use?
 Definition
Methyldopa
Term
Methyldopa for tmt of HTN side effects:
 Definition
- CNS: dry mouth, sedation, fatigue, depression, night mares
- sexual dysfunction
- hemolytic anemia, hepatitis (rare)
Term
What antihypertensives seem to be advantageous to use for patients with Coronary heart disease?
 Definition
- beta blockers
- ACE inhibitors

TEST KNOW THIS
Term
What antihypertensives are advantageous for patients with CHF?
 Definition
- beta blockers
- ACE inhibitors
- ARBs
- spiranolactone
Term
What antihypertensives are advantageous for patients with Diabetes?
 Definition
- ACE-I
- ARBs
Term
What antihypertensives are advantageous for patients with renal insufficiency?
 Definition
- ACE-I
- ARBs
Term
In hypertensive crisis emergencies ___ __ is present or progressive and blood pressure control should be achieved within __ __.
 Definition
- end-organ damage
- one hour
Term
With hypertensive crisis urgencies there is __ ___ ____ ___ and blood pressure control should be achieved within ___ ___.
 Definition
- no obvious end-organ damage
- 24 hours
Term
When treating hypertensive crisis, the goal is to get ___ pressure to ___ and then move to normal over the next few days. Excessive and rapid decreases in BP should be avoided since this can lead to ___ or ___ ___.
 Definition
- diastolic
- 100-110
- cerebral or cardiac hypoperfusion
Term
For hypertensive crisis emergencies, use drugs ___.
 Definition
parenterally
Term
For hypertensive crisis urgencies, use drugs ___ and occasionally ___.
 Definition
parenterally
orally
Term
Vasodilators used in hypertensive crisis:
 Definition
- Nitroprusside
- Fenoldopam
- Labetalol

"NFL players may get hypertensive crisis"
Term
Nitroprusside uses ___ to cause ___. This is used in the treatment of __ ___.
 Definition
- NO
- vasodilation
- hypertensive crisis
Term
Labetalol is a ___ ___ which blocks __ __ receptors and some ___ __. This results in ___ and is used in treatment of __ ___.
 Definition
- beta blocker
- beta 1
- alpha receptors
- vasodilation
- hypertensive crisis
Term
Fenoldopam is a __ ___ that causes __ allowing the ___ to remain perfused. This is used in the treatment of ___ __.
 Definition
- dopamine agonist
- vasodilation
- kidneys
- hypertensive crisis
Term
Overly agressive therapy of hypertensive crisis is associated with severe hypotensive problems, including insufficient circulation to the __.
 Definition
CNS
Term
Insufficient therapy of hypertensive crisis is associated with end-organ damage including ___.
 Definition
stroke
Term
Since the NFL drugs used to treat hypertensive crisis (Nitroprusside, Fenoldopam, Labetalol) all ultimately result in vasodilation, what is a significant side effect for most patients?
 Definition
orthostatic hypotension
Term
Nitroprusside is used in ___ ___ and is given ___. It is also given for ___ to cause ___ ___.
 Definition
- hypertensive emergencies
- i.v.
- surgery
- controlled hypotension
Term
Adverse effects of Nitroprusside:
 Definition
- excessive hypotension
- cyanide/thiocyanate toxicity
Term
Nitroprusside causes what kind of toxicity:
 Definition
- cyanide/thiocyanate toxicity
Term
Fenoldopam is a __ __ ___. It is an __ for ___ __ receptors. It is indicated in the hospital for in-hospital, ___ __ (up to __ __) management of ___ __ when rapid, but quickly reversible, emergency reduction of blood pressure is clinically indicated, including ___ ___ with ___ ___ ___ ___.
 Definition
- rapid-acting vasodilator
- agonist for dopamine D1 receptors
- short term (up to 48 hours)
- severe hypertension
- malignant hypertension with deteriorating end-organ function
Term
Labetalol is a __ mixture of __ isomers with __ blocking activity, mixed ___ __ blocker activity and is a ___ ___ agonist.
 Definition
- racemic mixture of 4 isomers
- with alpha blocking
- mixed non-selective beta
- selective beta-2 agonist
Term
Labetalol is basically a ___ ___ with __ __. It is used in __ ___, __ __, and ___.
 Definition
- beta blocker
- intrinsic activity
- hypertensive crisis
- pre-eclampsia
- pheochromocytoma
Term
Atherosclerosis decreases __ of vessel.
 Definition
lumen

change in flow= (1/radius^4)
Term
Atherosclerosis timeline:
 Definition
- foam cells> fatty streak> intermediate lesion> atheroma> fibrous plaque> complicated lesion/rupture
Term
The foam cells, fatty streak, intermediate lesion, and atheroma growth stages are all characterized by __ ___. In the fibrous plaque stage ___ __ and __ build up. In the complicated lesion/rupture stage __ and __ occur.
 Definition
- lipid accumulation
- smooth muscle and collagen
- hematoma and thrombosis
Term
3 Pharmacological Treatment approaches to treatment of peripheral arterial disease:
 Definition
- prevent platelet plugs and clotting
- slow the build up of atherosclerotic plaques
- improve circulation
Term
Major risk factors that modify LDL goals:
 Definition
- cigarette smoking - Hypertension (>140/90, or on antihypertensive medication) - low HDL (less than 40mg/dL) - Family Hx of premature CHD: CHD in male first degree relative younger than 55 years, CHD in female first degree relative younger than 65 years - age (men 45 or older, women 55 or older)
Term
HDL cholesterol greater than or equal to __ mg/dL counts as a negative risk factor, its presence removes ___ __ __from the total count.
 Definition
- 60
- removes one risk factor
Term
A patient who has 0-1 risk factors for CHD is considered lower risk. What should this patients LDL goal be and at what LDL level should treatment be initiated and at what level should drug therapy be considered?
 Definition
- LDL goal of less than 160mg/dL
- treatment inititiated if LDL is greater than or equal to 160mg/dL
- drug therapy when LDL is at 190mg/dL

(kind of confusing chart explaining this on slide 78 of HTN/PVD lecture)
Term
A patient with 2 or more risk factors for CHD and a 10 year risk factor of less than 10% is considered at moderate risk for CHD. What should this patient's LDL goal be, when should treatment be initiate, and when should drug therapy be considered?
 Definition
- LDL goal of < 130mg/dL
- initiate treatment when LDL is greater than or equal to 130 mg/dL
- consider drug therapy when LDL reaches 160mg/dL
Term
Patients with 2 or more risk factors for CHD and who have a 10 year risk factor of 10-20% are considered to be at moderately high risk for CHD. What should their goal LDL be, when should treatment be initiated, and when should drug therapy be considered?
 Definition
- LDL goal of <130mg/dL
- initiate tmt at > or equal to 130mg/dL
- consider drug therapy at 130mg/dL
Term
Those with CHD or CHD risk equivalents are considered high risk for CHD and have a 10 year risk of greater than 20%. What should their LDL goal be, when should treatment be initiated, and when should drug therapy be considered?
 Definition
- LDL of less than 100mg/dL
- initiate tmt if LDL is greater than or equal to 100 mg/dL
- consider drug therapy when LDL is 100mg/dL
Term
Antilipemics are used to prevent or slow the progression of ___ to reduce the risk of ___ __ __ and ___ __.
 Definition
- atherosclerosis
- coronary artery disease
- prolong life
Term
Importance of cholesterol (3):
 Definition
- component of cell membranes and intracellular organelle membranes
- involved in the synthesis of certain hormones including estrogen, progesterone, testosterone, adrenal corticosteriods
- needed for synthesis of bile salts, which are needed for digestion and absorption of fat
Term
Cholesterole is synthesized in the ___. ___ __ is converted to ___ ___ and ultimately to cholesterol by ___ __ ___ __ ___ (___).
 Definition
- liver
- acetyl coA
- mevalonic acid
- hydroxymethyl glutaryl coenzyme A reductase (HMG-COA)
Term
VLDL stands for __ __ __ __ and contains __ and some ___ . It accounts for nearly all ___ in the blood and contains ___.
 Definition
- very low density lipoprotein
- triglycerides and some cholesterol
- nearly all triglycerides in blood
- B-100
Term
VLDL delivers TGs from the __ to ___ __ and ___. TGs are then __ and removed by __ ___ leaving __ __ __ for storage in adipose tissue or ___ in ___ __ or __ __.
 Definition
- from the liver to adipose tissue and muscle
- TGs are then hydrolyzed and removed by lipoprotein lipase
- free fatty acids
- oxidation in cardiac tissue or skeletal muscle
Term
liver> VLDL with triglycerides> adipose tissue and skeletal muscle> (lipoprotein lipase)> hydrolyzes triglycerides> free fatty acids get stored in adipose tissue or oxidized in cardiac or skeletal muscle
 Definition
Term
After VLDL is hydrolyzed, the remnants are called ___, which get transported to the liver to make ___.
 Definition
- IDL (intermediate density lipoprotein)
- LDL
Term
high levels of ___ increase risk for pancreatitis.
 Definition
IDL
Term
LDL is __ cholesterol and accounts for__ to __ % of cholesterol in the blood. It delivers __ to __ ___.
 Definition
- bad
- 60-70%
- cholesterol to peripheral tissues
Term
__ makes the greatest contribution to __ ___. __ __ forms atherosclerotic plaques. ___ gets removed from the plasma by __ ___ which converts it to bile acids to be excreted in the GI tract.
 Definition
- LDL
- coronary atheroslcerosis
- oxidized LDL
- LDL
- liver endocytosis
Term
HDL is __ cholesterol and accounts for __ to __% of blood cholesterol. Some contains __ and __. ___ is cardioprotective. HDL transports cholesterol from __ __ back to the __, thereby promoting __ __. HDL is considered ___.
 Definition
- good
- 20-30% of blood cholesterol
- ApoI and ApoII
- ApoI is cardioprotective
- from peripheral tissues back to the liver
- cholesterol removal
- HDL is antatherogenic
Term
Mechanism of action of atherosclerotic plaque formation:
 Definition
- LDL cholesterol moves into subendothelial space of an artery> LDL gets oxidized> oxidized LDL attracts monocytes from circulation inhibiting their motility> monocytes get converted to macrophages> macrophages take up the LDL cholesterol> macrophages become more and more full of LDL= foam cells
Term
foam cells:
 Definition
macrophages full of oxidized LDL
Term
when foam cells accumulate a __ __ forms.
 Definition
fatty streak
Term
Accumulation of foam cells can cause __ of the endothelium causing __ __ resulting in the formation of ___.
 Definition
- rupture of the endothelium
- causing platelet adhesion
- formation of microthrombi
Term
Repeated rupture and healing of endothelium due to foam cells ultimately leads to __ __ . As the __ grows, it impedes blood flow resulting in __ __ and ultimately an __.
 Definition
- plaque formation
- plaque
- anginal pain
- MI
Term
1st line treatment of hyperlipidemia:
 Definition
- non-pharmacological
- diet modifications
- increase exercise to increase HDL
- reduce risk factors as much as possible

Diet guidelines include:
- decrease total intake of fat, esecially saturated fat
- increase fiber intake
- increase omega 3 fatty acid (fish)
- decrease homocysteine
- increase fruits and vegetables
- decrease simple sugars
- moderate alcohol consumption b/c etoh can increase TGs
Term
Drug therapy options for hyperlipidemia (5):
 Definition
- Niacin
- HMG-CoA reductase inhibitors
- Fibric acid derivatives
- cholesterol uptake inhibitors
- omega 3 fatty acids
Term
HMG-CoA reductase inhibitors are good for the prevention of __ and __ ___.
 Definition
primary and secondary CHD
Term
First generation HMG-CoA reductase inhibitors:
All in this generation are derived from ___, while the other statins are synthetic.
 Definition
- Simvastatin
- Lovastatin
- Pravastatin

- fungi

In first grade you love SLP.
Term
Second generation HMG-CoA reductase inhibitors:
 Definition
- Fluvastatin
Term
Third generation HMG-CoA reductase inhibitors:
 Definition
- Atorvistatin
- Rosuvastatin

AR was so cool in the 3rd grade.
Term
All HGM-CoA reductase inhibitors end in ___.
 Definition
"-statin"
Term
statins work by inhibiting HMG-coa reductase. These drugs are __ __of the ___ ___. Statins lead to increased synthesis of __ __
 Definition
- structural analogues of the HMG-CoA intermediate
- LDL receptors
Term
Simvastatin and Lovastatin are extensively metabolized by ___ in the intestinal wall and liver. Thus inhibitors of ___can produce a marked ___ in their effect.
 Definition
- CYP3A4
- CYP3A4
- increase
Term
Atorvistatin is metabolized by ___, though not as extensively as Lovastatin and Simvastatin. But inhibitors of ___ would still __ its concentratio.
 Definition
- CYP3A4
- CYP3A4
- increase
Term
Cerivastatin is metabolized by ___ and __. There is not much information on cerivastatin drug interactions, except that it seems to have a high incidence of ___ __ when it is combined with ____.
 Definition
- CYP3A4 and CYP2C8
- muscle damage
- gemfibrozil
Term
Fluvastatin is metabolized by ___ and can have drug interaction involving that enzyme.
 Definition
CYP2C9
Term
___ is not metabolized by the CYP450 system, and of all the statins it is the least likely to have adverse side effects.
 Definition
Pravastatin
Term
So if start patient on a statin and they have lots of side effects, try switching them to ___.
 Definition
pravastatin
Term
Statin applications (3):
 Definition
- elevated cholesterol of all types, particularly effective at lowering LDL
- decreasing cholesterol> increasing LDL receptors in liver> decrease LDL cholesterol
- often see a small decrease in TGs and small increase in HDL
Term
Statins are used as ___ therapy in __ risk patients.
 Definition
- aggressive
- high
Term
Recent data on statins show a __% reduction in strokes (no reduction in brain hemorrhage) in at risk populations.
 Definition
25
Term
Statin toxicity has low incidence and is less likely to occur than with other lipid lowering drugs. Most frequently this results in __ __(1-2%). Elevated serum __ __ occur, and can cause ___. Thus when pt is on statin monitor __ __ every __ ___ and then every __ __. There are also increasing number of reports of __ __ with statin toxicity, though this is reversible with discontinuation of the drug.
 Definition
- hepatic damage
- hepatic enzymes
- hepatitis
- liver enzymes every 1-2 months and then every 6 months
- peripheral neuropathies
Term
Also with statin toxicity watch for ___ , __ (less than 1%), and ___. Monitor this especially when combining a statin with ___ or ___ drugs, which can cause the same toxicity.
 Definition
- myalgia
- myopathy
- rhabdomyalgia
- niacin or fibrate drugs
Term
____ is a potentially life threatening side effect of statins, especially when combined with __ or __ drugs. Avoid combining statins with ___ completely b/c this decreases metabolism of statins making myopathy and rhabdomyalgia more frequent.
 Definition
- Rhabdomyalgia
- niacin or fibrate drugs
- avoid combing statins with eryhtromycin
Term
Rhabdomyalgia is the muscle breakdown of proteins that will float around and block the ___. Monitor ___ and/or __ to watch out for this.
 Definition
- glomeruli
- creatine phosphokinase (CPK) and/or creatine kinase
Term
HMG-CoA inhibitors also inhibit Q10, and this mechanism is most likely cause of rhabdomyalgia.
 Definition
Term
Statin contraindications:
 Definition
- hepatic disease
- pregnancy b/c fetus needs cholesterol cell membrane formation
Term
Make sure not being too agressive with statin therapy, b/c abrupt drop in cholesterol may cause ability to maintain __ __ __.
 Definition
cell wall structure
Term
___ and ___ cross the blood brain barrier and may cause sleep disturbances.
 Definition
- Lovastatin and Simvastatin
Term
CYP3A4 enzymes are found in the __ and enteric mucosa of the __ ___. These enzymes metabolize many drugs in clinical practice and are responsible for the __ __ ___. Many drugs and grapefruit juice alter the activity of the CYP3A4 enzymes.
 Definition
- liver
- small intestine
- first pass effect
Term
Natural components in grapefruit juice called ___ bind to and ___ CYP3A4 enzymes leading to ___ drug metabolism and ___ concentration.
 Definition
- furanocoumarins
- deactivate CYP3A4 enzymes
- decreased drug metabolism
- increased concentration
Term
Statins should not be taken with ___ b/c this will __ the concentration of drug and may lead to myalgias or rhabdomyolysis.
 Definition
- grapefruit juice
- increase
Term
Grapefruit can increase drug exposure for atorvastatin, lovastatin, simvastatin, cerivastatin but not for ___.
 Definition
pravastatin
Term
Niacin (aka vit B3, nicotinic acid, niaspan, or slo-niacin) inhibits ___ secretion, which leads to ___ VLDL, ___ LDL, and ___ HDL. HDL ___ due to ___ rate of catabolism caused by niacin.
 Definition
- inhibits VLDL secretion
- decreased VLDL
- decreased LDL
- increased HDL
- HDL increases due to decreased rate of catabolism caused by niacin.
Term
Any lipoprotein disorder, particularly ___ hyperlipidemias with __ TGs niacin would be helpful.
 Definition
- mixed
- elevated
Term
for Niacin to work on hyperlipidemia, have to have ___ quantities, won't work in just vitamin form.
 Definition
gram
Term
DOC to decrease levels of triglycerides (VLDL) in patients at risk for pancreatitis.
 Definition
Niacin
Term
___ is approved for elevating HDL levels.
 Definition
Niaspan
Term
With Niacin, start with __ dose and gradually increase. Give at __ with __.
 Definition
- low
- night with food
Term
Niacin toxicity symptoms:
 Definition
- ITCHING, FLUSHING, UNPLEASANT SENSATION OF FEELING WARM: prostaglandin mediated, give aspirin to blunt, but not remove, this effect
- G.I. distress (may activate ulcers)
- hyperuricemia in 20% of pts b/c inhibits urate secretion
- hepatotoxicity
- hyperglycemia (impaired CHO tolerance, but still can be given to diabetics on insulin)
Term
Niacin hepatotoxicity:
 Definition
- rare
- reversible
- occurs with older sustained release formulas
- monitor liver fx frequently
- liver injury is less likely with Niaspan (given once daily) the new extended release formula
Term
Name the 2 fibrate derivatives:
 Definition
- Gemfibrozil
- Fenofibrate
Term
Fibrate derivatives, such as ___ and __, __ the activity of lipoprotein lipase, for __ lipolyis of TG and clearance. This leads to __ VLDL formtaion in the liver, leading to __ TGs. There tends to be a modest __ in LDL in some patients (though it may rise slightly in others). But it does cause a nice moderate __ in HDL.
 Definition
- Gemfibrozil and Fenofibrate
- increase the activity of lipoprotein lipase
- increased lipolysis and clearance
- decreased VLDL
- decreased TGs
- modest decrease in LDL
- increase in HDL
Term
Gemfibrozil uses:
 Definition
This is a fibrate derivative drug used for:
- reduction of TGs when VLDL is very high, or when IDL is elevated
Term
To know if Gemfibrozil should be used, follow ___. If __ is elevated, you should use Gemfibrozil. But if ___ is elevated and VLDL is not, you should not use this drug.
 Definition
- follow VLDL
- VLDL
- LDL
Term
Gemfribrozil toxicities (rare, but long list):
 Definition
- blood cell deficiencies
- skin rash and other hypersensitivity reactions
- GI problems
- liver enzyme abnormalities (usually transient)
- myositis- myopathy and rhabdomyolis reported when combined with HGM-coA reductase inhibitors
- lithiasis due to increased biliary cholesterol excretion (do NOT use in patients with gall bladder problems)
Term
Gemfibrozil contraindications:
 Definition
- patients with gall bladder problems

Also do not combine with HMG-CoA reductase inhibitors b/c may cause rhabdomyolysis
Term
Name 3 bile acid binders:
 Definition
- Cholestyramine
- Colestipol
- Colesevelam
Term
Mechanism of action of bile acid binders (Cholestyramine, Colestipol, Colesevelam):
 Definition
- enhance 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, thereby decreasing LDL
Term
Inhibitor of intestinal sterol absorption (1):
 Definition
- Ezetimibe
Term
Ezetimibe inhibits absorption of ___ and ___. It is primarily useful in __ LDL cholesterol. It decreases cholesterol absorption by about __, but does not modify __ absorption. It is often used in combination with a __.
 Definition
- phytosterols and cholesterol
- reducing LDL cholesterol
- decreases cholesterol absorption by 50%
- does NOT modify TG absorption
- used in combo with a statin
Term
Ezetimibe is excreted with __ and acts at the __ __ of the __ __ to inhibit uptake of dietary and biliary cholesterol into the enterocytes.
 Definition
- excreted with bile
- brush border of the small intestine
Term
Ezetimibe is a cholesterol/phyosterol absorption inhibitor, thus unlike bile acid binders it does not ___ absorption of other fatty substances. It is well tolerated.
 Definition
- does NOT decrease absorption of other fatty substances
Term
Ezetimibe does NOT inhibit cholesterol synthesis in the liver and does NOT increase bile acid secretion. It merely inhibits absorption of sterols in intestines.
 Definition
Term
Ezetimibe has relatively benign side effects, especially when compared to bile acid binders. But Ezetimibe may cause:
 Definition
- reversible change in liver fx
- if pushed too aggressively> myalgia/rhabdomyolysis (particular hazard when combined with statin)
Term
when you combine ezetimide with a statin, what do you need to be very cautious of?
 Definition
- that rhabdomyolysis does not occur
Term
“In conclusion, the reduction of LDL cholesterol by the addition of ezetimibe to simvastatin did not reduce intima–media thickness of the carotid-artery wall in patients with familial hypercholesterolemia in our study. The reason for the failure to observe an incremental effect on intima–media thickness despite a reduction in levels of LDL cholesterol remains unknown.”
 Definition
so even though simvastatin + ezetimide decreased LDL, the intima media thickness of the carotid artery did not change
Term
Omega-3 fatty acids are in fish oils. Data supports that they are __ __. They are antiatherogenic by reducing __ and ___ synthesis in the liver. This requires such large amounts of fish consumption, that other factors come into play (mercury?).
 Definition
- cardio-protective
- reducing VLDL and TG synthesis in liver
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