Drugs Used in ACS/Stable Angina Flashcards
What is stable angina?
When do symptoms occur?
1) Occlusion of coronary arteries resulting from the formation of atherosclerotic plaque
2) During exertion or stress
What is Vasospastic angina?
When do symptoms occur?
1) Episodes of vasoconstriction of coronary arteries
2) At rest
What are the two approaches to treat stable angina?
1) To increase (or restore) coronary blood flow
2) To reduce myocardial oxygen demand
What pharmacotherapy regimen is used to increase blood flow through the stenotic coronary artery in order to treat stable angina?
There is none
What are the nitrates used in treating stable angina?
1) Nitroglycerin
2) Isosorbide dinitrate
3) Isosorbide mononitrate
Why do nitrates have a significant first-pass metabolism?
High nitrate reductase activity in the liver
What is the MOA of nitrates in stable angina?
Nitrates release NO which causes cGMP to activate protein kinase G causing venous dilation and reduced preload which ultimately leads to decrease in O2 demand
The development of tolerance to nitrates leads to the increased generation of?
Superoxide radical
Short-acting formulations of nitrates are used to?
Long-acting preparations may be used to?
1) Relieve the angina attack
2) Prevent attacks
What drug interaction are seen with nitrates?
What does it cause molecularly?
What conditions have been reported due to the interaction?
1) Drugs used in ED such as sildenafil, vardenafil, and tadalafil
2) Massive increase in cGMP
3) Acute MI
What are the non-cardioactive (dihydropyridines) calcium channel blockers used in treating stable angina?
1) Amlodipine
2) Nifedipine
3) Nicardipine
What are the cardioactive calcium channel blockers used in treating stable angina?
1) Diltiazem
2) Verapamil
The non-cardioactive calcium channel blockers act on?
Vascular smooth muscle
The cardioactive calcium channel blockers act on?
1) Vascular smooth muscle
2) Cardiac muscle
3) Cardiac pacemakers cells
What is the end goal of calcium channel blockers in order to treat stable angina?
Decrease myocardial O2 demand
How do calcium channel blockers decrease myocardial O2 demand?
(Indicate if the MOA is done by dihydropyridines or by cardioactive CCB)
1) Dilation of peripheral arterioles (Both)
2) Decrease cardiac contractility (Cardioactive CCB)
3) Reduce heart rate (Cardioactive CCB)
What are the beta-blockers used in treatment of stable angina?
1) Propranolol
2) Nadolol
3) Metoprolol
4) Atenolol
What is the end goal of beta-blockers in order to treat stable angina?
How does it accomplish this?
1) Decrease myocardial O2 demand
2) Decrease HR, cardiac contractility, and BP
What is the MOA of ranolazine?
Inhibits late Na+ current in cardiomyocytes
Ranolazine may reduce?
1) Diastolic tension and compression of coronary vessels in diastole
2) Cardiac contractility and oxygen demand
What is the goal in treating vasospastic angina?
To relieve coronary spasm and increase blood flow into the affected area using vasodilators
What are the first choice drugs for treating vasospastic angina?
CCBs such as Diltiazem or amlodipine
If CCBs are contraindicated due to low BP, bradycardia, or AV block what are used instead to treat vasospastic angina?
Long-acting nitrates
Where do red thrombus form?
What are they composed of?
What pathologic condition is it associated with?
1) In low-pressure veins and in the heart
2) Fibrin-rich with trapped RBCs
3) Embolic stroke
Where do white thrombus form?
What are they composed of?
What pathologic condition is it associated with?
1) In high-pressure arteries
2) Platelet rich
3) Acute coronary syndrome
What drug class is used to prevent white thrombi from forming in the arteries?
Prevent red thrombi from forming in venous system?
Re-establish blood flow through vessels once clots have formed?
1) Antiplatelet drugs
2) Anticoagulants
3) Thrombolysis
What antiplatelet drug is an inhibitor of thromboxane A2 synthesis?
Aspirin
Clopidogrel, Prasugrel, and Ticagrelor make up what class of antiplatelet drugs?
P2Y12 (ADP) Receptor Blockers
Abciximab, Eptifibatide, and Tirofiban make up what class of antiplatelet drugs?
Platelet glycoprotein IIB/IIIA receptor blockers
What is the MOA of aspirin?
Irreversible inhibition of cyclooxygenase to block TxA2 production
What is the MOA of the P2Y12 (ADP) Receptor Blockers?
Blocks these receptors to increase adenylyl cyclase activity and cAMP levels which prevent platelet aggregation
What populations have the highest resistance to clopidogrel?
Why?
1) Chinese and African Americans
2) CYP2C19 allele present
What is the MOA of Abciximab, Eptifibatide, and Tirofiban?
Prevent binding of ligands to the GP IIb/IIIa receptor to inhibit platelet aggregation
What is an adverse effect of the glycoprotein IIB/IIIA receptor blockers that is more often seen with abciximab?
Thrombocytopenia
Alteplase, Reteplase, Tenecteplase are the thrombolytic drugs that fall under the category of?
What thrombolytic drug is in its own separate category?
1) Tissue-type Plasminogen Activator (tPA)
2) Streptokinase
What do thrombolytic drugs induce?
How does it do this?
1) Fibrinolysis
2) Converting plasminogen into plasmin
What clinical use do thrombolytic drugs have?
Used in STEMI within 12 hours