CV drugs (8) Flashcards
What drugs are used to treat Angina?
Calcium channel blockers, Nitrates, Beta blockers
Nitrates MOA
relaxation of smooth muscle whin blood vessels, resulting in the desired vasodilatory effect
decrease preload and afterload reduce workload of heart reduce O2 demand
How do you store Nitrates?
Limit light expossure by keeping in brown glass bottle
Short shelf life (6 months, 3 months)
How do you know if Nitrates is working?
Tingling sensation as drug dissolves
What is the dosage for Nitrates?
After 1st dose relief should occur within 1-2 minutes
2nd dose if symptoms still present after 5 minutes ( up to 3 doses in 15 min)
No relief possible MI
Nitrates AE
reflex tachycardia, dizziness, OH (orthostasis), weakness, severed headache
What do you do when suspecting cardiac event?
chew 325 mg non-enteric coated aspirin.
Up to 3 doses of NG can be administered over 15 minutes
IV nitroglycerin may be started in ED
Antithrombotic Classes
Antiplatelets, Anticoagulants, Fibrinolytics
What is the difference between Antiplanets and Anticoagulants?
Antiplatelets- preventing the thrombus
Anticoagulants-use when some one developed a clot and prevent it from worsening
What drugs class are Antiplatelets?
Aspirin, ADP receptor inhibitors
ADP Receptor drugs?
Clopidogrel (Plavix)
MOA ADP Receptor Inhibitors (Irreversible)
block ADP binding to receptor thus decrease platelet aggregation
How long does Clopidogrel (Plavix) last?
platelet aggregation (for lifespan of platelet, 7-10 days)
What is the biggest concern for clopidogrel (Plavix)?
Bleed is biggest concern- monitor symptoms and labs (Hgb/Hct)
How is ADP Receptor Inhibitors metabolized?
CPY
What are some uses for ADP Receptor Inhibitors?
Used after ACS (acute coronary syndrome) with PCI (stent placement), stroke (Plavix only)
Heparin MOA
inactivates thrombin and FIXa, FXa, FXIa, FXIIa = prevents conversion of fibrinogen to fibrin
How long does it take for Warfarin to have an effect
Does not have immediate effect- usually 3-5 days for full effect and longer to stabilize dose
When do you use nitrates?
Sublingual nitrates drug of choice for acute attacks to provide immediate symptom relief
also be administered before activity to prevent symptoms
What are the Nitrate drugs?
Nitroglycerin
Isosorbide mononitrate
What is the role of Thrombin?
Converts fibrinogen to fibrin
What are the box warnings for ADP Receptor Inhibitors (Irreversible)?
↓ efficacy in some genetic variants that make them CYP2C19 poor metabolizers (present in 50% of Asians, 30% African-Americans, 25% Caucasians)
What are the Parenteral and PO Anticoagulant class?
Parenteral- Heparin, LMWH
PO: Vitamin K antagonist, Direct thrombin inhibitor, Factor SX inhibitors
Reversal Agent for Heparin
protamine sulfate
What is HIT?
How do you treat HIT?
When antibodies which bind to heparin thus is activates platelets and increase clotting
Treat with direct thrombin inhibitors or Factor Xa inhibitors
What is a LMWH drug?
enoxaparin (Lovenox)
How is LMWH different than Heparin?
LMWH has greater effect on inhibiting FXa than thrombin
Why is LMWH preferred over Heparin?
simple dosing, no monitoring requires, decrease HIT
What is the new reversal agent for LMWH?
andexanet alfa (Andexxa)
What is drug is Vitamin K Antagonist?
warfarin (Coumadin)
Vitamin K Antagonist MOA?
depletes Vitamin K thus synthesis of factors VII, IX, X and II, and protein C and S
If INR is low, what is the patient at risk for?
more risk of clotting
If INR is high, what is the patient at risk for?
More risk for a bleed
What are INR levels for Atrial fibulation or venous thrombus embolism
AF: 2-3
VTE: 2.5-3.5
What CV drugs have genetic variants for CYP?
Warfarin and Clopidogrel (Plavix)
What happens to INR when there is an increase consumption of vitamin K foods/
Decrease INR
Direct Thrombin Inhibitor MOA
binds directly and reversibly to thrombin with high selectivity inhibits conversion of fibrinogen to fibrin
What to lookout for when taking Direct Thrombin Inhibitor?
Less intracranial bleeding than warfarin but more GI bleeding
What are Factor XA Inhibitor drugs?
rivaroxaban (Xarelto), apixaban (Eliquis)
Factor XA Inhibitor MOA
selectively and reversibly binds FXa thus stops further coagulation cascade
What is the difference between Rivaroxaban and Warfarin?
less intracranial bleed than warfarin; rivaroxaban has more GI bleed (also on Beers List)
Less drug interactions than warfarin
What to look for when taking Rivarozaban?
It must be taken with a high fat meal
Which Factor XA inhibitor drug is has the lowest risk for a bleed?
Apixaban
What is preferred anticoagulant drug when patient is noncompliant
Take Warfarin b/c DOAC’s have a shorter duration of action
How do you monitor with Antiplatelets and Antithrombotics?
Bleeding, Brusing, Block, tarry stools,
Seek med help if nosebleed or a cut wont stop bleeding
Seek med help if hit head during a fall b/c risk of intercranial bleeding
Clotting-Red, swollen, warm extremity, usually unilateral and in calf
Fibrinolytics MOA and uses
MOA: plasmin breaks fibrin links in the thrombus
Use: start immediately after stroke, MI, PE
What drugs to use for VTE Prophylaxis
LMWH or heparin used for prevention
Then bridge to PO
What is 1st line long term VTE treatment?
DOAC
Therapeutic Concerns for Antithrombotic Drugs
Falls could cause internal bleeding
Contraindicated PT treatments
What drug classes are use to treat Atherosclerosis?
HMG-COA reductase inhibitors (Statins) and Ezetimibe (Cholesterol absorption Inhibitor)
Statins MOA
block cholesterol synthesis
Statins AE
myalgia (symmetrical, large proximal muscle groups), myopathy and rhabdomyolysis is rare, tendinopathy and tendon rupture
Which population is likely to get myalgia from statins?
elderly female, low BMI Asian descent, excess alcohol, high levels physical activity
Which statins are less likely to get myalgia?
pravastatin, rosuvastatin
Ezetimibe MOA
inhibits absorption of cholesterol in small intestine
What is the 1st and 2nd line Cholesterol drugs
1st line = statin
2nd line = ezetimibe added on if remain uncontrolled or can’t tolerate statin
Therapeutic Concerns about Statins
Myositis and Myalgia
Muscle pain, fatigue, weakness
Creatinine kinase (CK) >10 times upper normal limits
Rhabdomyolysis
Severe muscle damage, marked CK elevation, renal
dysfunction
Grapefruit juice (perhaps pomegranate): inhibits CYP3A4
HFpEF treatment
diuretics (loop), aldosterone antagonist (K+ sparing antagonist)
Goals in HFrEF
decrease edema and congestion, increase contractility, ↓ preload and afterload = vasodilators (hydralazine, isosorbide dinitrate, sacubitril), ACEi, or ARB
Baseline HFrEF
ACEi or ARB + beta-blocker + diuretic prn(loop
Entresto MOA and AE
ACE and ARB MOA and AE
Digoxin MOA
inhibits Na+/K+ ATPase pump in myocardial cells = ↑ intracellular sodium = ↑ Ca2+ from Na+/Ca2+ exchange pump = ↑ contractility
Drug classes to treat Arrythmia?
B-blockers, Amiodarone
Amiodarone MOA and uses
Used for ventricular arrhythmias
Basic MOA: Prolong the duration of the action potential by blocking K+, Na+, and Ca2+ channels; also some beta-blocker activity
Amiodarone AE
Liver toxicity, thyroid dysfunction, pulmonary fibrosis, neuropathy, bluish discoloration on exposed areas of the skin
How long does Amiodarone last?
Long 1/2 life. 50 days can prolone AE even after withdrawal
What are some therapeutic concerns with Antidysrhythmic Agents?
Drugs may cause arrhythmias
Hypokalemia increases risk of arrhythmia
Be aware of dehydration (Diuretics!)
Effect on exercise tolerance: adequate warm up time
Negative inotropic effects = heart will not respond normally to demands of exercise
Exercise may cause rhythm disturbance from increased catecholamines, making drugs ineffective during exercise
Lack of “cool down” period will also contribute to rhythm disturbance
Therapeutic Concerns about Digoxin
NTI
GI symptoms: nausea, vomiting, diarrhea, abdominal pain, anorexia
CNS: blurred vision, confusion, lethargy
Cardiac: arrhythmia (due to increased intracellular calcium increased cardiac contractility)
What happens when an individual taking Digoxin has impaired renal clearance?
Digoxin toxicity b/c its cleared mainly by the kidney