Vasodilators for Angina Pectoris DRUGS

Question 1

what are the 3 drugs that reduce cardiac size, rate, force and reduce cardiac o2 demand are?

Answer 1

vasodilators
B-blockers
CCB

Question 2

what is the MOA for Nitric Oxide

Answer 2

activates and increases cGMP

Question 3

What 2 drug classes decrease intracellular Ca2+

Answer 3

Beta blockers
CCB

Question 4

What drug class prevents the depolarization of vascular smooth muscle?

Answer 4

Potassium channel openers
ex. Minoxidil (K+ opener)

Question 5

what is the MOA of Nitrates

Answer 5

releases and increases NO into the SM cells leading to vasodilation

Question 6

what is rapid and short acting nitrates primarily used for?

Answer 6

Acute angina pectoris
Hypertensive urgency

Question 7

What are the 3 main side effects of Nitrate

Answer 7

1. headache
2. GERD
3. Hypotension with syncope

Question 8

Is there a difference in MOA between organic nitrate vs nitrous acid esters of polyalcohols

Answer 8

Not a big difference in MOA

Question 9

What is the required activation for organic nitrates?

Answer 9

by mitochondrial aldehyde reductase (so the action is not immediate)

Question 10

what are 3 examples of organic nitrates?

Answer 10

1. nitroglycerin
2. isosorbide dinitrate
3. isosorbide mononitrate

Question 11

What is the onset of action of sodium nitroprusside?

Answer 11

immediate b/c it is activated non-enzymatically

Question 12

What is the most favorable route of nitrates

Answer 12

sublingual b/c it avoids the first pass effect

Question 13

What is the bioavailability level of nitrates/nitrites?

Why?

Answer 13

Low bioavailability due to the liver containing an organic nitrate reductase that in activates nitrates/nitrites

Question 14

What is the best route to administer nitroglycerin and isosorbide dinitrate? How long does it take to reach therapeutic levels?

Answer 14

sublingual route
within a few minutes

Question 15

what is the total duration of effect for nitroglycerin and isosorbide dinitrate?

Answer 15

15-30 minutes (brief)

Question 16

what are the other routes for nitroglycerin

Answer 16

transdermal
buccal absorption (slow release)

Question 17

what is the effect of Nitroglycerin in the body?

Answer 17

relaxes all types of smooth muscle regardlesss of preexisting muscle tone

Question 18

What muscle does nitroglycerin not have a direct effect on?

Answer 18

cardiac or skeletal muscle

Question 19

what is the primary direct result of an effective dose nitroglycerin?

4

Answer 19

1. marked relaxation in the veins
2. increase venous capacity and decreased ventricular period
3. pulmonary vascular pressure decreased
4. heart size is decrereased
5. if absense of heart failure= output is reduced

Question 20

what pulsations are associated with the headache from nitrates/ nitrites

Answer 20

temporal artery pulsations
meningeal artery pulsations

Question 21

Why are nitrates/nitrites beneficial for heart failure

Answer 21

vasodilators reduce preload and have a benefit for cardiac output

Question 22

what are indirect effects of nitroglycerin

Answer 22

1. decreased arterial pressure
2. ^ results in tachycardia and increased cardiac contractility
3. retention of salt and water

Question 23

what is the result of nitRITE ion and hemoglobin?

Answer 23

produces methemoglobin (by oxidation of ferrous to ferric iron)

“methemoglobinemia”- needs a lot to cause significant rx

Question 24

what inotropic effect on the heart does nitroglycerin have?

Answer 24

weak negative inotropic effect

Question 26

what ways can nitrate already be present in the human body in high levels?

Answer 26

processed meats well water

Question 27

how can nitrites be used to treat cyanide poisoning?

Answer 27

methemoglobin iron administration of sodium nitrite after cyanide exposure regenerates cytochrome

Question 28

what do you follow sodium nitrite with for treatment of cyanide exposure

Answer 28

IV sodium thiocyanate methylen blue

Question 29

What is the new treatment for cyanide exposure

Answer 29

hydrooxocobalamin

Question 30

the major acute toxicities of organic nitrates are ___

Answer 30

direct extensions of therapeutic vasodilation

Question 31

what is a major contraindication of nitrates

Answer 31

if intracranial pressure is elevated

Question 32

what nitrate does not experience tolerance

Answer 32

nitroprusside because it retains activity over long periods

Question 33

what is the onset of action of nitrates

Answer 33

1-3 minutes

Question 34

Why are nitrates not suitable for maintenance therapy

Answer 34

becuase duration of action is short (20-30 minutes)

Question 35

what is IV nitroglycerin used for?

Answer 35

ONLY used for recurrent rest angina

Question 36

What are the CCB drugs

Answer 36

verapamil Nifedipine Diltiazem

Question 37

What calcium channel blockers are administered via IV

Answer 37

Verapamil and diltiazem

Question 38

what are the characteristics of the pharmacokinetics of CCB

Answer 38

High first pass effect high plasma protein binding extensive metabolism

Question 39

what is the MOA of CCB

Answer 39

reduces the frequency of opening in response to depolarization -decreased transmembrane calcium current -reduces contractility -decreases sinus node pacemaker rate and AV node conduction

Question 40

How can CCB be partially reversed?

Answer 40

Elevating the concentration of Calcium or increase the transmembrane flux of calcium (sympathomimetics)

Question 41

do slide 20

Question 47

Clinical effects of CCB | list 5

Answer 47

1. decrease myocardial contractile force (reduces myocardial o2 req.) 2. decreals arterial and intraventricular pressure 3. relieve and prevent focal coronary artery spasm (contraction inhibited) 4. SA and AV nodes are slowed

Question 48

Verapamil _____ affects slow response cells in SA and AV nodes

Answer 48

markedly

Question 49

Diltiazem _____ affects slow response cells in SA and AV nodes

Answer 49

moderately

Question 50

Dihydropyridines _____ affects slow response cells in SA and AV nodes

Answer 50

doesn't (as much)

Question 51

What are calcium channel blockers used for prophylatically

Answer 51

angina pectoris

Question 52

Verapamil main effect? When is this possibly unwanted?

Answer 52

slows conduction through AV node -unwanted in TX of HTN

Question 53

what is the effect of verapamil and b-blockers

Answer 53

AV block

Question 54

What are the peripheral *vasodilator* effects of verapamil?

Answer 54

reduce afterload and BP

Question 55

Toxic effects of verapamil | list 3 + 2 peripheral effects

Answer 55

1. mild cardiodepression 2. heart failure 3. edema 1. headache 2. reflex tachycardia

Question 56

Nifedipine brand name

Answer 56

Procardia

Question 57

what class is Nifedipine

Answer 57

dihydropyridine CCB

Question 58

what is the predominant effect of nifedipine

Answer 58

-IN peripheral vasculature -decreases afterload

Question 59

what vasodilator is recommended for pts already on a vasodilator? why

Answer 59

Nifedipine they have less effect on the heart

Question 60

what drug class is diltiazem?

Answer 60

a benzodiazepine CCB

Question 61

what is the benefit of diltiazem

Answer 61

it has intermediate proprerties between verapamil and dihydropyridines

Question 62

what is diltiazem used to treat?

Answer 62

variant angina (prinzmetals) stable angina

Question 63

what is the 1st line prophylactic treatment of chronic angina

Answer 63

beta-blockers

Question 64

what are the benefits of beta-blockers for angina pectoris

Answer 64

decreases HR, BP and contractility this decreases myocardial O2 requirments at rest and during exertion

Question 65

# For beta-blockers what is a decreased heart rate also associated with (perfusion related)

Answer 65

increase diastolic perfusion time increase coronary perfusion

Question 66

For maintenance therapy of chronic stable angina, what therapy regimes are options for your patient?

Answer 66

1. Beta blockers 2. CCB 3. long acting nitrates

Question 67

for hypertensive pts, what therapy regimes may be used for angina pectoris?

Answer 67

1. monotherapy with slow-release 2. long acting CCB 3. Beta blockers

Question 68

For normotensive patients, what vasodilator regime may be suitable?

Answer 68

long-acting nitrates

Question 69

what are the two combinations of drug classes that are more effective for angina together?

Answer 69

1. B-blocker and CCB 2. two different CCB

Question 70

In patients with unstable angina, NSTEMI, what is the recommended therapy regime? | 4

Answer 70

1. coronary stenting 2. antilipid drugs 3. heparin 4. antiplatelet agents