Chapter 12: Drugs Used in the Treatment of Angina Pectoris

Question 1

Industrial disease caused by chronic exposure to vasodilating concentrations of organic nitrates in the workplace; characterized by headache, dizziness, and tachycardia on return to work after 2 days absence

Answer 1

“Monday disease”

Question 2

Loss of effect of a nitrate vasodilator when exposure is prolonged beyond 10–12 h

Answer 2

Nitrate tolerance, tachyphylaxis

Question 3

What is the primary mechanism of the therapeutic benefit of nitrates in atherosclerotic angina?

Answer 3

Reduction of the oxygen requirement

Question 4

What is the secondary mechanism of the therapeutic benefit of nitrates in atherosclerotic angina?

Answer 4

Increase in coronary flow via collateral vessels in ischemic areas

Question 5

These drugs are used only for prophylactic therapy of angina; they are of no value in an acute attack.

Answer 5

Beta blockers

Question 6

Toxicity with these drugs includes constipation, pretibial edema, nausea, flushing, and dizziness. More serious adverse effects include heart failure, AV blockade, and sinus node depression

Answer 6

Calcium channel blockers

Question 7

Releases nitric oxide (NO), increases cGMP (cyclic guanosine monophos-phate), and relaxes vascular smooth muscle

Answer 7

Nitroglycerin

For:

1. Acute angina pectoris (short acting)
2. Prophylaxis of angina (long/intermediate acting)

Question 8

Blocks L-type Ca2+ channels in smooth muscle and heart (decreases intracellular Ca2)

Answer 8

Calcium channel blockers

1. Verapamil
2. Diltiazem (shorter half-life)

Toxicity:
Constipation, pretibial edema, flushing, dizziness
Higher doses: cardiac depression, hypotension
*Nifedipine (less constipation, less cardiac effect)

Question 9

Blocks sympathetic effects on heart and blood pressure (reduces renin release)

Answer 9

Beta blockers

Question 10

Blocks late Na current in myocardium, reduces cardiac work

Answer 10

Ranolazine

Toxicity:
QT prolongation on ECG • inhibits CYP3A and 2D6

Question 11

Blocks pacemaker Na current (If) in sinoatrial node, reduces heart rate

Answer 11

Ivabradine

Toxicity:
Excessive bradycardia

Question 12

Block phosphodiesterase 5 (PDE-5); increase cGMP

Answer 12

Drugs for erectile dysfunction:

Sildenafil, tadalafil, vardenafil

ADR:
Interaction with nitrates - priapism, fatal hypotension