Week 9 + 10: Cardiovascular Flashcards
Cardiovascular Prototype Drugs
- atorvastatin (Lipitor)
- methyldopa (Aldomet)
- prazosin (Minipress)
- atenolol (Tenormin)
- hydralazine (Apresoline)
- verapamil (Calan, Isoptin)
- lisinopril (Prinivil)
- losartan (Cozaar)
- nitroglycerin
- hydrochlorothiazide (Hydrodiuril)
- furosemide (Lasix)
- spironolactone
- mannitol
- digoxin (Lanoxin)
- Potassium
- Quinidine
- lidocaine (Xylocaine)
Respiratory drugs focused mainly on what receptors
Beta 2
Statin
Cardiovascular Drug Class
“Anti-Lipid” / Lower Cholesterol / Antilipemic Drugs
All Cholesterol/Anti Lipid Drugs end in…
-statin
How do statins affect lipid levels
Increases HDL (modestly - a little)
Decreases LDL, Total Cholesterol, VLDL, and Triglycerides (Main impact)
Atherosclorosis
Buildup of fatty plaque on the arterial walls
Narrows vessels but also makes the vessel more stiff - then the vessel cannot expand and constrict which is bad
The first thing to be done to lower elevated lipid levels is…
modify diet and exercise
Ex: Less meat, cheese, saturated fats, trans fats
What can be done after dietary/lifestyle changes for lipid levels
Drug therapy
A major cause of atherosclerosis is…
excess plasma levels of lipoproteins
What are the 2 ways we can modify/decrease lipoprotein
- Modify Diet and Exercise
2. Drug therapy if dietary changes do not work
VLDL
lipoprotein
produced in the liver, delivers triglycerides to adipose tissue and muscle
LDL
cholesterol
a by product of VLDL metabolism
delivers cholesterol to the liver and tissues
HDL
cholesterol
removes cholesterol from tissues
has a “good” protective effect
Nonpharmacologic Ways to Alter Plasma Lipoproteins
Diet modification (decrease LDL and triglyceride)
Weight loss - can be just a little
Exercise - even if you are not losing weight or change diet (Doesnt need to be strenuous just some movement)
Smoking (increases LDL and decreases HDL)
DM, Hypothyroidism, excessive ETOH ingestion increases risk
Alcohol ingestion can be toxic to ___ muscle as well
Heart
Most cases of high cholesterol/lipids will need to undergo
drug therapy for it - hard to change their ways
We want to lower ___ cholesterol without decreasing ___ cholesterol
LDL; HDL
Ideal LDL and HDL levels
LDL - Below 100
HDL - 40-60
What is important to know about how antilipemics work
They only ACT PROPHYLACTICALLY - they do not remove existing plaque, just prevents more from occurring
Once plaque is there it will stay there
What are the 2 basic mechanisms of Antilipemics
- Suppress lipoprotein formation
2. Accelerate removal (of lipoproteins)
Prototype Drug for Antilipemics
atorvastatin (Lipitor)
Statin means…
antilipemic
What is the classification of atorvastatin
Anti-lipid (HMG-CoA reductase inhibitor)
Action of atorvastatin (Lipitor)
Decreases the enzyme (HMG-CoA) which usually helps us make Cholesterol (which decreases the amount of cholesterol made)
Inhibits the enzyme thus decreasing cholesterol synthesis
Main 3 ADRs to Know for atorvastatin
- Muscle Issues
- Liver Function Issues (Serum Transaminase Levels)
- Peripheral Neuropathy
ADRs of Atorvastatin
Serum Transaminase levels (watch liver function)
Peripheral Neuropathy (tinglinh, numbing, fumbling in hands and feet)
Muscle: Pain, myalgia severe, myostitis, muscle weakness, rhabdomyolysis (muscle death or breakdown)
Other: Mild and transient GI disturbances, rash, HA, sleep issues, lupus like syndrome
When is atorvastatin given?
It can be given orally one time a day either with food or not
Older statins needed to be taken at night because as we sleep is when most cholesterol is made but the newer drugs do not need to worry about this
What 2 things should never be drunk with atorvastatin
- Alcohol - It can already cause liver disease/damage so taking alcohol will further increase this
- Grapefruit Juice - it inhibits statin metabolism causing toxic level buildup
What should be done at the beginning of atorvastating therapy and periodically throughout
liver function tests
When is atorvastatin contraindicated and why
Pregnancy
This is because cholesterol is important to the neurological system when the fetus is forming its neurological system from scratch so we do not want to prevent that
Atorvastatin may enhance the clinical effects of what other medicine
oral anticoagulants (bleeding risk)
What can you not eat while taking a statin drug
grapefruit juice
it inihibits statin metabolism meaning toxic level buildup can occur leading to toxic ADRs - even if its just once in a while
The important formula to know for Antihypertensive drugs is…
BP = CO x TPR (Total peripheral resistance0
TPR
Total Peripheral Resistance
It is how open or shut your arteries/arterioles are
If the vessels are tight and constricted BP will increase - also CO increases will increase BP
What prototype drugs are anti-hypertensives
- methyldopa (Aldomet)
- prazosin (Minipress)
- atenolol (Tenormin)
- hydralazine (Apresoline)
- verapamil (Calan, Isoptin)
- lisinopril (Prinivil)
- losartan (Cozaar)
What things do anti-HTN drugs influence to lower BP
CO
TPR
Vessels
The Heart
Variety of places
What things determine CO
HR
Contractility
Blood Volume
Venous Return (less return means decreased BP out of the heart)
What thing determines TPR
arteriolar constriction
What are some Non-Pharmacological Approaches for BP
Exercise
Weight Reduction (even just a small %)
Lower sodium intake (most comes from restuarants/fast food)
Lower Alcohol intake (Not good for the heart)
Reduce Stress
Sleep (7-8 hours a night)
What kind of exercise is best for BP
aerobic exercise (even just a walk)
What is the general approach to using anti-hypertensives / lowering BP
Mixing non-pharm and drug methods, but the goal is to have the drugs being used working in different ways so they do not duplicate each other
The overall goal (levels) for BP treatment are what
To reduce BP to <120/80!!! for most people WITH THE FEWEST SE (some people get dizzy and fall when that low)
What level is now considered HTN
above 130/80
What are the groups of drugs/actions that are used for HTN
Promotion of salt excretion (Diuretics)
Decrease Sympathetic NS Activity
Vasodilators
Calcium Channel Blockers
Angiotensin II Inhibitors and Related Drugs
What action/type of anti-hypertensive is most effective at decreasing BP
The ones that inhibit SNS function
*Ganglionic blockers work well too but they also affect the PNS so they can cause widespread effects - more used for antihypertensive crisis
What is the most common side effect with all Anti-Hypertensives
HYPOTENSION (usually postural/orthostatic)
Since Interference with SNS activity either centrally or peripherally make for the most effective BP drugs, what situations are they most used for
Mild to Moderate HTN
Those with impaired renal fxn too
SNS interfering BP Drugs are often used with…
a thiazide diuretic
methyldopa (Aldomet)
Anti-HTN Medicine
The one drug working on Alpha 2 Receptors
Classification of methyldopa
Sympatholytic Anti_HTN, Alpha 2 Adrenergic AGONIST
What does it mean to be an alpha 2 agonist
It connects to alpha 2 receptors in the brain, and when these are instigated they tell the brain to DECREASE/LOWER SNS Effects
Is methyldopa (Aldomet) a first line anti hypertensive medication?
No it is a second line therapy
Basically, methyldopa will …
inhibit SNS response (to decrease HTN)
What is another use for methyldopa (Aldomet) in regard to lower BP
it can be used to drop HTN related to withdrawal from substance abuse
Action of Methyldopa
Central Mechanism (Brain/Medulla) - Reduces sympathetic outflow
Reduces amount of Norepinephrine formed which results in decreased peripheral resistance and dropped SNS signalling
With Methyldopa there is little to no…
cardiac output effect
Absorption and Route of methyldopa
oral - good
ADRs of Methyldopa
- POSTURAL/ORTHOSTATIC HYPOTENSION
- SEDATION (some CNS effects go away)
- Na/H2O RETENTION IF NOT RECEIVING A DIURETIC
Other: Depression, Dry Mouth, Nasal Congestion, HA, Fever, Decreased WBC + Platelet, Hepatic Dysfunction, Sexual Dysfunction
Why do Anti-HTN meds often need a diuretic given with it (like methyldopa)
If BP is riding lower than the usual set point then the body recognized that and will try to hold onto Na and H2O to try and raise BP as a compensation mechanism
So, we need a diuretic to fight this issue
When is methyldopa contraindicated
liver disease hx
Major Depression hx
When is a special case of HTN where methyldopa can be utilized
PIH - pregnancy induced HTN 6-7 mo into the pregnancy
Alpha 1 Blocker activation causes ____
vasoconstriction
Prototype drug that is an antihypertensive, alpha 1 adrenergic antagonist (blocker)
prazosin (Minipress)
Action of prazosin (Minipress)
Blocks Alpha 1 Stimulation (blocks vasoconstriction) which means vasodilation occurs (arterioles and veins open up) so BP will lower
Net Result: Antagonizes Alpha 1 to prevent constriction by alpha stimulation causing vasodilation and decreased TPR
ADRs of prazosin (Minipress)
- ORTHOSTATIC HYPOTENSION
- REFLEX HR Response - palpitations, tachycardia
- First Dose Phenomenon
Other: HA, Dizziness, Syncope, Diarrhea, Dry Mouth, peripheral Edema, urinary urgency, IMPOTENCE
What is the Reflex Response that occurs from prazosin (Minipress)
When the baroreceptors in the brain detect a BP decrease, and it is unable to control the vessels (antibypertensive) or evn Na and H2O levels (diuretic) then it will increase HR
So whenever you dilate blood vessels there is a natural tendency of the heart to try and up BP using this reflex
First Dose Phenomenon
prazosin (Minipress)
One dose causes a massive drop in BP
Make sure the patient is sitting down or lying down so they do not fall over
What 2 situations can prazosin (Minipress) (or Alpha 1 Stimulation) be useful in
- HTN
2. BPH - relaxes smooth muscles and allows easier urination/pressure
Beta blocker drugs usually end in what
-olol / -lol
Selective Beta Adrenergic Inhibitor
Beta Blocker (Selective)
Only blocks Beta 1 Receptors
Non-Selective Beta Adrenergic Inhibitor
Beta Blocker (Non-selective)
Blocks both Beta 1 and Beta 2 –> More SE than seletive Beta Blocker
What type of drug may also be given a selective beta adrenergic inhibitor
an Alpha 1/Antihypertensive because beta 1 blockers can prevent the reflex tachycardia seen with vasodilators
Why might you never give a Beta 2 Blocker to someone with something like COPD
it may cause bronchoconstriction
What is the main reason beta blockers are used
to decrease cardiac workload (decrease heart rate, cardiac output, etc)
Someone post-MI cannot leave the hospital without….
beta blockers - the heart has been injured and we need to decrease the workload on it
Prototype Drug that is a Selective Beta 1 Adrenergic Inhibitor
atenolol (Tenormin)
Action of atenolol (Tenormin)
Blocks Beta 1 Adrenergic Receptors to cause AntiHTN, AntiAnginal, AntiArrhythmic
3 Important Effects of atenolol (Beta 1 Blocker)
- Anti HTN
- Anti Anginal (reduce myocardial O2 consumption)
- Anti Arrhythmic (Blocks B-adrenergic effect in SA node and Purkinje Fibers)
How might the Anti HTN effect of a beta 1 blocker occur
- decreased HR adn force of contraction (slow heart and decrease power of contraction)
- depress RAA system (decrease holding onto fluid) or
- (maybe some) Central Action
atenolol is given orally and has…
extensive first pass - 50% absorbed
ADRs of atenolol
- CV: Bradycardia, CHF, Intensify AV Block, Hypotension
- Fatigue (Dampening SNS Beta 1 Activity)
- Respiratory -Bronchospasm (in COPD and asthma(
Other: NVD, cramps, allergies
It is always important to do what before giving atenolol
check apical and radial pulse, and BP before giving
What causes the CV ADRs of atenolol
if you decrease things too much with the beta 1 blocker and the heart is not beating enough
atenolol as an anti-hypertensive is generally used in combination with…
a thiazide DIURETIC and a VASODILATOR
When is atenolol primarily used as an anti-arrhythmic
for supraventricular arrhythmias
Black Box Warning of Atenolol
DO NOT STOP ABRUPTLY - slowly taper before discontinuing
Quitting cold turkey can lead to HR and BP rising fast and if they have a weaker heart they could end up with an MI - Make sure they wont run out of Beta Blockers
Caution using Atenolol with what patients
Patients with CHF, asthma, COPD, or diabetes
What is another use for Beta Blockers besides as an anti-hypertensive
Migraine prophylaxis, MI Prophylaxis, Panic Attacks, Benign Essential tremor, and PTSD
Prevents some peoples issues in these areas when taken in low doses (often by decreasing/slowing down SNS response)
