Exam 2 - Anti-anginal & other vasodilators

Question 1

Nitroglycerin and Isosorbide dinitrate belong to what class of drugs?

Answer 1

Nitrates/Nitrites

Question 2

What is the MOA for Nitrates/Nitrates?

Answer 2

Stimulates NO production which will produce cGMP and ultimately lead to vasodilation

Question 3

What is the DOC for ACUTE anginal attacks?

Answer 3

Nitrates/Nitrites (Nitroglycerin, Isosorbide dinitrate)

Question 4

What is the predominant mechanism of Nitrates/Nitrites that allow them to provide anginal relief?

Answer 4

They decrease myocardial O2 requirement

Question 5

Why is the sublingual administration of Nitrates/Nitrites preferred?

Answer 5

• Avoid hepatic destruction
• Rapid absorption
• Immediate anginal relief within 1-3 minutes

Question 6

What are some adverse effects of Nitrates/Nitrites?

Answer 6

Pronounced vasodilation can lead to:

• Throbbing HA
• Orthostatic hypotension
• Reflex tachycardia

Frequent exposure can lead to tolerance or marked reduction of most effects (not suitable for long-term treatment)

Question 7

What are CCBs good for in regards to angina?

Answer 7

Good for CHRONIC angina treatment and not for immediate relief

Question 8

Why is slow release nifedipine (a CCB) only indicated in HTN and not angina?

Answer 8

May provoke angina pectoris due to possible reflex tachycardia

Question 9

B-blockers have CV effects at what 3 organs?

Answer 9

• Heart: Decrease CO
• Kidneys: Decrease renin
• CNS: Decrease SNS tone

Question 10

How to B-blockers provide anginal relief?

Answer 10

Decrease oxygen demand

Question 11

Why are B-blockers not used for variant angina?

Answer 11

B-blockers are ineffective in producing coronary vasodilation/will not dilate spastic vessels

Question 12

What are adverse effects of B-blockers?

Answer 12

• Bronchoconstriction (do not use in asthmatics)
• Increase plasma triglycerides
• Decrease insulin and hypoglycemic response (do not use in diabetics)
• CNS side-effects

Question 13

What is the MOA for Ranolazine?

Answer 13

• Partial fatty-acid oxidation inhibitor and decreases O2 consumption in ischemic tissue
• Inhibits late inward sodium current, decreasing contractility

Question 14

What are uses for Ranolazine?

Answer 14

• Angina
• Reduces left ventricular wall stiffness and increases coronary circulation

***Last choice drug and only used when other meds have not worked

Question 15

What is the preferred treatment for variant or angiospastic angina?

Answer 15

Nitrates or CCBs

Question 16

What is the most effective drug combination for treatment of angina pectoris?

Answer 16

B-blockers and a vasodilator (nitrate/CCB)

Question 17

What class of drug is Sildenafil (Viagra)?

Answer 17

PDE-5 Inhibitor

Question 18

What is the MOA for Sildenafil (Viagra)?

Answer 18

Inhibits PDE-5 from degrading cGMP into GMP, allowing accumulation of cGMP and vasodilation

Question 19

What is Sildenafil (Viagra) used for?

Answer 19

• ED

- Pulmonary HTN

Question 20

When is the max concentration of Sildenafil (Viagra) reached?

Answer 20

Within 30-120 minutes

Question 21

What is Sildenafil (Viagra) metabolized by?

Answer 21

Primarily by CYP3A4

Question 22

What are some adverse effects of Sildenafil (Viagra)?

Answer 22

• Headache, flushing, nasal congestion (due to vasodilation)

- Visual impairment (can also partially inhibit PDE6 in the retina)

Question 23

What are contraindications to using Sildenafil (Viagra)?

Answer 23

• Inhibitors of CYP3A4 and 2C9 (will reduce its clearance, leading to build up and increased adverse effects)
• Concurrent treatment with nitrates/nitrates (will have too much vasodilation)
• Concurrent use with alpha blockers (symptomatic hypotension)
• Use in pregnant or lactating women, infants, children

Question 24

It is contraindicated to use Sildenafil (Viagra) with inhibitors of CYP3A4 and 2C9 isoenzymes. What are some examples of these enzymes?

Answer 24

• Ritonavir
• “azoles”
• Cimetidine (OTC antiacid and grapefruit juice)
• Erythromycin
• Quinidine

Question 25

What makes Vardenafil (Levitra) and Tadalafil (Cialis) different from Sildenafil in regards to their MOA?

Answer 25

They are more selective for PDE5 than PDE6, causing less visual disturbances

Question 26

Which PDE5 Inhibitor has the fastest onset of action?

Answer 26

Vardenafil

Question 27

Which PDE5 Inhibitor has the longest duration of action?

Answer 27

Tadalafil

Up to 24-36 hours, so can be taken the day before and allows for spontaneity