Antianginal Drugs

Front 1

What is the main vascular level changes we try to make to treat angina?

Back 1

Vasodilation

Front 2

Two methods by which we can encourage vasodilation?

Back 2

UP cGMP, Down Ca

Front 3

What 3 major classes of drugs are used to treat angina?

Back 3

Beta Blockers, Ca Channel Blockers, Nitrates

Front 4

What are the two main mechanisms by which our antianginal drugs do their job?

Back 4

Decrease O2 requirement (vasodilation, Nitrates, Ca channel blockers), Decrease CO (beta blockers, Ca channel blockers)

Front 5

Drugs that we use for variant angina usually do what?

Back 5

reverse coronary spasms

Front 6

What types of drugs are best for variant angina?

Back 6

Ca channel blockers

Front 7

When should you and should you not use beta blockers?

Back 7

should - post MI; Shouldn't - Variant angina;

Front 8

What are the absolute contraindications for beta blocker use?

Back 8

Severe bradycardia, Heart Block, Severe bronchospasm, Severe Unstable LV failure

Front 9

What are the relative contraindications for beta blocker use?

Back 9

Asthma, diabetes

Front 10

Adverse effects of beta blockers from an angina standpoint and how do you counter?

Back 10

increased EDV and ejection increase O2 consumption a bit; Give nitrates with them to counter

Front 11

SE's of beta blockers?

Back 11

hypotension, Fatigue, bradycardia, ED, Hair Loss, Claudication

Front 12

Example of first gen non selective B blocker?

Back 12

propranolol

Front 13

Examples of second gen beta blockers?

Back 13

Metoprolol, Bisprolol

Front 14

How do second gen B blockers compare to first gen?

Back 14

selective for Beta 1, but will block Beta 2 at high levels;

Front 15

Diff between third gen beta blockers and the other gens?

Back 15

will also block alpha receptors

Front 16

Half life of bisprolol and why improtant?

Back 16

8-12 hours; allows for once daily dosing

Front 17

Which beta blocker is 30% bound to serum protein?

Back 17

Bisprolol

Front 18

Which B blocker is metabolied by CYP2D6 and why is this important?

Back 18

Metoprolol; half life can vary from 2.5 to 7.5 hours depending on genotype

Front 19

What is isosorbide dinitrate metabolized to and how biologically available are they?

Back 19

5 mononitrate dinitrate, very potent 100% available

Front 20

How are oral nitrate preparations dosed?

Back 20

high amounts for sustained systemic blood levels

Front 21

What is the metabolism pathway of nitroglycerine in body?

Back 21

glutathione S transferase releases NO from it

Front 22

Mechanism of NO?

Back 22

stimulates Guanyly cyclase, increases cGMP

Front 23

Why does tolerance to nitrates sometimes develop?

Back 23

due to decreased tissue SH groups

Front 24

How can you overcome nitrate tolerance?

Back 24

give SH regenerating agents (acetylcysteine)

Front 25

Anginal pain relief with nitrates probably due to what mechanism?

Back 25

peripheral vasodilation (decreases overall need for O2); NOT coronary artery vasodilation;

Front 26

SE's of Nitrates?

Back 26

Headache, Tachycardia, orthostatic Hypotension, Syncope

Front 27

How can you combat the reflex tachycardia from nitrates?

Back 27

give beta bockers or calcium channel blockers

Front 28

Possible dangerous drug interaction with nitrates?

Back 28

viagra, prevents the breakdown of cGMP, so you get extreme vasodilation, severe hypotension

Front 29

What do you need to tell patients about viagra if they're on nitrates?

Back 29

wait 6 hours after taking nitrates to use it

Front 30

You might use an intracoronary injection of Nitrates for what, but not for what?

Back 30

variant angina (relaxes vasospasm); Stable acute angina

Front 31

What type of calcium channels do we want to block with our drugs?

Back 31

L type (muscle, neurons)

Front 32

Which drug is the prototype of the DHP class of Ca channel blockers?

Back 32

nifedipine

Front 33

Mech of calcium channel blockers in angina therapy?

Back 33

relax smooth muscle, slow down heart

Front 34

What type of smooth muscle is most sensitive to the effects of ca channel blockers?

Back 34

Vascular

Front 35

What type of vascular tissue is most sensitive to Ca channel blockers?

Back 35

arterioles

Front 36

Main SE of Ca channel blockers?

Back 36

Orthostatic HTN

Front 37

Diff between DHP class Ca channel blockers and Diltiazaem/verapamil?

Back 37

DHP class more selective for vasc smooth muscle; D and V are more selective for Heart

Front 38

What Ca channel blocker is selective for cerebral blood vessels?

Back 38

Nimodipine

Front 39

Which is a more potent negative inotrope, V or D?

Back 39

V

Front 40

Which Ca channel blocker would be good to give someone post subarrachnoid hemorrhage?

Back 40

Nimodipine

Front 41

Main SE's of Ca channel blockers?

Back 41

Bradycardia, dizziness, constipation, peripheral edema

Front 42

What type of drug sometimes causes MI's and why?

Back 42

Quick release nifedipine; rapid decrease in BP causes reflex symp stim;

Front 43

Half life of amlodipine?

Back 43

30 - 50 hours

Front 44

Why should you always think about giving Nitrates in comb with either, beta or Ca channel blockers?

Back 44

their bad side effects cancel each other out

Front 45

What is the general progression of drug therapy for chronic stable angina?

Back 45

start with beta blocker; If it doesn't work add either nitrates or Ca blockers; If still not working, add the other