Deja review Cardio/Renal agents - Antianginal agents Flashcards
Define angina pectoris
Chest pain resulting from a myocardial oxygen demand that is not met by adequate oxygen supply, seen in patient with myocardial ischemia
What type of angina is caused by spontaneous coronary vasospasm?
Prinzmetal (variant) angina
What type of angina is caused by atherosclerosis of coronary vessels and is precipitated by exertion?
Classic angina
What type of angina can be acute in onset and is caused by platelet aggregation?
Unstable angina
What 2 mechanistic strategies are used in treatment of angina?
1) INC oxygen supply to the myocardium
2) DEC myocardial oxygen demand
What types of drugs can INC oxygen supply?
Nitrates, calcium channel blockers (CCBs)
What types of drugs can DEC oxygen demand?
Nitrates, CCBs, ß-blockers
What is the drug of choice for immediate relief of anginal symptoms?
Sublingual nitroglycerin (NTG)
What is MOA of nitrates?
Nitrates form nitrites, nitrites form nitric oxide (NO), NO activates guanylyl cyclase to INC cGMP, INC cGMP leads to INC relaxation of smooth muscle
How does cGMP lead to relaxation of vascular smooth muscle?
Causes dephosphorylation of myosin light chains
How do nitrates INC oxygen supply?
Dilation of coronary vessels which leads to INC blood supply
How do nitrates DEC oxygen demand?
Dilation of large veins which leads to preload reduction, DEC preload reduces the amount of work done by the heart, DEC amount of work results in DEC myocardial oxygen requirement
What are the adverse effects of nitrates?
Headache, hypotension, reflex tachycardia, facial flushing, metnemoglobinemia
Why must patients have at least a 10-12 hour “nitrate free” interval every day?
Tolerance (tachyphylaxis) develops to nitrates if given on a continous (around the clock) basis
Nitrates are contraindicated in patients taking any of what 3 medications?
1) Sildenafil
2) Vardenafil
3) Tadalafil
Methemoglobin formation, specifically by amyl nitrite, can be used to treat what type of poisoning?
Cyanide
What are the common formulations of nitrates?
NTG, isosorbide mononitrate, isosorbide dinitrate
What is the time to peak effect of sublingual NTG?
2 minutes
What is the dosing frequency of sublingual NTG during an anginal episode?
Every 5 minutes for a max of 3 doses
How do ß-blockers work in the treatment of angina?
Inhibition of α2 adrenoceptors which leads to DEC CO, HR, and force of contraction, thus reducing the workload of the heart
Do α-blockers INC oxygen supply?
NO
For each of the following CCBs, state whether their primary effects are on the myocardium or peripheral vasculature:
- Verapamil
- Dihydropyridine (DHP, nifedipine, amlodipine, felodipine, isradipine, nicardipine)
- Diltiazem
- Verapamil: Myocardium (greater negative inotropic effects)
- Dihydropyridine (DHP, nifedipine, amlodipine, felodipine, isradipine, nicardipine): Peripheral vasculature (more potent vasodilators)
- Diltiazem: Myocardium
How do CCBs work in the treatment of angina?
Block vascular L-type calcium channels which leads to DEC heart contractility and INC vasodilation