Pharm: Angina Therapy

Question 1

What are the differences between chronic stable, unstable, and Prinzmetal (variant) angina?

Answer 1

Stable: due to atherosclerosis, plaque is stable, only occurs during exertion

Unstable: due to unstable atherosclerotic plaque, occurs even during rest

Variant: occurs because of coronary artery vasospasm

Question 2

Function of Nitric Oxide in smooth muscle.

Answer 2

Released from endothelial cells in response to shear stress on vessel walls.

Diffuses into smooth muscle cells and activates adenylyl cyclase which forms cGMP from GTP.

cGMP activates myosin light chain phosphatase (MLCP) which dephosphorylates the myosin light chain preventing muscle contraction.

Leads to vasodilation

Question 3

Sodium Nitroprusside

Answer 3

MOA: spontaneously converts to NO and leads to vascular vasodilation (mostly in veins). This decreases venous pressure and venous return decreasing the heart’s workload

Indications: angina, hypertension, hemodynamic control during emergency

Adverse Effects: hypotension, CN toxicity, not tissue selective, headache, flushing, RENAL IMPAIRMENT due to thiocyanate accumulation.

Contraindications: PDE5 inhibitors, hypotension, increased intra-cranial pressure

Question 4

Nitroglycerine (NTG)

Answer 4

Short 5 min half life, given IV or sublingual to avoid first pass.

MOA: enzymatically converted to NO in vascular endothelium to cause venodilation. Decreases heart’s workload.

Indications: angina, hypertension

Adverse Effects: hypotension, headache, flushing, RENAL IMPAIRMENT due to thiocyanate accumulation.

Contraindications: PDE5 inhibitors, hypotension, increased intra-cranial pressure

Question 5

Isosorbide Mononitrate

Answer 5

2 hr. half-life, given IV or sublingual to avoid first pass.

MOA: enzymatically converted to NO in vascular endothelium to cause venodilation. Decreases heart’s workload.

Indications: angina, hypertension

Adverse Effects: hypotension, headache, flushing, RENAL IMPAIRMENT due to thiocyanate accumulation.

Contraindications: PDE5 inhibitors, hypotension, increased intra-cranial pressure

Question 6

Isosorbide Dinitrate

Answer 6

5 hr. half-life, given IV or sublingual to avoid first pass.

MOA: enzymatically converted to NO in vascular endothelium to cause venodilation. Decreases heart’s workload.

Indications: angina, hypertension

Adverse Effects: hypotension, headache, flushing, RENAL IMPAIRMENT due to thiocyanate accumulation.

Contraindications: PDE5 inhibitors, hypotension, increased intra-cranial pressure

Question 7

Propranolol

Answer 7

MOA: non-selective Beta blocker to decrease isotropy and chronotropy in the heart.

Indications: angina, tachycardia

Adverse Effects: hypotension, bradycardia, fatigue, malaise, sleep disturbance, sexual dysfunction and depression

Contraindications: COPD, asthma, bradycardia

Question 8

Nadolol

Answer 8

MOA: non-selective Beta blocker to decrease isotropy and chronotropy in the heart.

Indications: angina, tachycardia

Adverse Effects: hypotension, bradycardia, fatigue, malaise, sleep disturbance, sexual dysfunction and depression

Contraindications: COPD, asthma, bradycardia

Question 9

Metoprolol

Answer 9

MOA: selective B-1

Indications: angina, tachycardia

Adverse Effects: hypotension, bradycardia, fatigue, malaise, sleep disturbance, sexual dysfunction and depression

Question 10

Atenolol

Answer 10

MOA: selective B-1

Indications: angina, tachycardia

Adverse Effects: hypotension, bradycardia, fatigue, malaise, sleep disturbance, sexual dysfunction and depression

Question 11

Beta blockers with intrinsic sympathomimetic activity that should be avoided in angina.

Answer 11

Pindolol, acebutolol

Question 12

Verapamil

Answer 12

MOA: cardio-selective L-type calcium channel blocker. Moderate peripheral dilation decreasing afterload, Potent coronary vasodilators to improve perfusion of heart. Decrease HR and contractility.
Excretion by kidneys

Indications: angina

Adverse Effects: bradycardia, hypotension

Question 13

Diltiazem

Answer 13

MOA: cardio-selective L-type calcium channel blocker. Moderate peripheral dilation decreasing afterload, Potent coronary vasodilators to improve perfusion of heart. Decrease HR and contractility.
Excretion by liver

Indications: angina

Adverse Effects: bradycardia, hypotension

Question 14

Nifedipine

Answer 14

MOA: L-type calcium channel blocker in peripheral arteriole smooth muscle. Rapid acting, excreted by kidneys.

Indications: angina

Adverse Effects: reflex tachycardia, hypotension

Question 15

Amlodipine

Answer 15

MOA: L-type calcium channel blocker in peripheral arteriole smooth muscle. Slow hepatic metabolism and slow acting.

Indications: angina

Adverse Effects: hypotension

Question 16

Ranolazine

Answer 16

MOA: blockade of late phase cardiac sodium current thereby reducing calcium entry indirectly. This decreases ventricular wall stress and oxygen demand.

Indications: angina

Adverse Effects: prolonged QT, dizziness, headache, nausea,

Contraindications: previous Torsaides, hepatic impairment.