Anti-anginal drugs

Question 1

drug therapy options for exertional angina

Answer 1

Nitrates
 Calcium Channel Blockers
 Beta Blockers
 Ranolazine
 Ivabradine

Question 2

how do nitrates work in SMC

Answer 2

Activates Guanylyl Cyclase
Increases cGMP
Dephosphorylates Myosin Light Chains
Ultimately Produces Smooth Muscle Relaxation
Relaxation Is ENDOTHELIUM-INDEPENDENT

Question 3

NITRATE MECHANISM OF ACTION

Answer 3

• DECREASED VENOUS RETURN
Dilates Venous Capacitance Vessels
• REDUCED LV WALL TENSION
LaPlace’s Law
• REDUCED AFTERLOAD
• DIRECT CORONARY ARTERY VASODILATATION
Increased Subendocardial Perfusion

Question 4

CLINICAL USE OF ORGANIC NITRATES

Answer 4

Angina Pectoris
Exertional Angina
Unstable Angina
Prinzmetal’s Angina
Hypertensive Emergencies
Congestive Heart Failure

Question 5

MOST COMMONLY USED ORGANIC NITRATES FOR ANGINA

Answer 5

Nitroglycerine (sublingual, spray, patch or ointment)

Isosorbide mono/dinitrate (sublingual, chewable, oral)

Question 6

nitrate side effects

Answer 6

orthostatic hypotension
reflex tachycardia
headache

nitrate tolerance (cannot be given 24/7)

Question 7

what type of channel regulates smooth muscle contracton

Answer 7

voltage gated L-type Ca channels

Question 8

what type of channel regulates cardiac muscle contration

Answer 8

voltage gated L-type Ca channels - in cardiac cells the amount of Ca that enters is proportional to the strength of contraction

Question 9

what type of channel regulates cardiac pacemaker activity

Answer 9

L-type Ca channels

Question 10

CLINICAL USE OF CALCIUM CHANNEL BLOCKERS (6)

Answer 10

Angina Pectoris
Hypertension
Arrhythmias
Hypertrophic Cardiomyopathy
Migraine
Raynaud’s Phenomenon

Question 11

CALCIUM CHANNEL BLOCKERS FOR ANGINA exampes

Answer 11

DIHYDROPYRIDINES
Nifedipine
Nicardipine
Amlodipine

VERAPAMIL
DILTIAZEM
BEPRIDIL

Question 12

nifedipine has mainly what type of effect

Answer 12

vasodilatory (very little negative inotrophic and chronotropic effects)

Question 13

side effects of Verapamil and diltiazem (CCB)

Answer 13

bradycardia
CHF
heart block
hypotension

Question 14

side effects of nifedipine

Answer 14

reflex tachycardia
peripheral edema (a little usually means the drug is working and will go away)
hypotension

Question 15

where are B1 and B2 receptors found?

Answer 15

β1 Receptors:
Cardiac Muscle

β2 Receptors:
Cardiac Muscle
Bronchial Smooth Muscle
Vascular Smooth Muscle

Question 16

cAMP ACTIONS 
IN CARDIAC MUSCLE

Answer 16

• Increased Opening of L-type Ca channels
Inotropy
• Increased Reuptake of Ca into SR stores
Inotropy & Lusitropy
• Increased Pacemaker Current
Chronotropy
• Increased Rate of Conduction
Dromotropy

Question 17

B-blockers effects on the heart

Answer 17

block cAMP effects: 
• decrease HR
• decrease afterload
• increase heart size
• decrease contractility 
• decrease O2 wastage
* anti-arrhythmic
• increased diastolic perfusion
• decrease O2 demand

Question 18

CLINICAL USE OF BETA BLOCKING AGENTS (8)

Answer 18

Angina Pectoris
Hypertension
Arrhythmias
Dissecting Aortic Aneurysm
Mitral Valve Prolapse
Post-MI Prophylaxis
Hyperthyroidism
Migraine

Question 19

NONSELECTIVE (BETA-1+BETA-2) BBs

Answer 19

PROPRANOLOL

NADOLOL

Question 20

CARDIOSELECTIVE (BETA-1) BB

Answer 20

ATENOLOL

METOPROLOL

Question 21

NONSELECTIVE WITH ISA

Answer 21

LABETALOL

PINDOLOL

Question 22

CARDIOSELECTIVE WITH ISA

Answer 22

ACEBUTOLOL

Question 23

BB primarily eliminated by the liver

Answer 23

Propranolol, Caredilol, Metoprolol

Question 24

BB primarily eliminated by the kidney

Answer 24

Atenolol, Nadolol, Sotalol

Question 25

BETA BLOCKER SIDE-EFFECTS

Answer 25

BRONCHOSPASM* (do not give if pt has obstructive pulmonary disease)
PERIPHERAL VASOSPASM
EXAGGERATION OF CARDIAC THERAPEUTIC EFFECTS

CNS EFFECTS
INSOMNIA
DEPRESSION
FATIGUE

Question 26

CONTRAINDICATIONS TO ADMINISTRATION OF BETA BLOCKERS

Answer 26

Acute Congestive Heart Failure
Marked bradycardia (HR

Question 27

RANOLAZINE - suggested MOA

Answer 27

Ranolazine partially inhibits fatty acid oxidation, allowing the heart to use more glucose as a fuel by relieving the inhibition on pyruvate dehydrogenase.

The net result is reduced lactic acid accumulation, less intracellular acidosis, and a reduction in the severity of the myocardial ischemic response.

Question 28

IVABRADINE MOA

Answer 28

Ivabradine is an If Current Inhibitor (The “funny” current) responsible for Phase IV depolarization of the SA node.
Inhibits pacemaker activity and slows the heart rate at rest and during exercise

Question 29

who is Ivabradine recommended for?

Answer 29

Indicated for the symptomatic treatment of chronic stableangina pectoris in patients with normalsinus rhythmwho cannot take beta blockers.

Also indicated in combination with beta blockers in heart failure patients with LVEF lower than 35 percent inadequately controlled by beta blockers alone and whose heart rate exceeds 70 beats per minute.

Question 30

how effective is ivabradine

Answer 30

As effective as beta blockers and comparable withamlodopine in the management of chronic stable angina

Question 31

side effects of ivabradine

Answer 31

Luminous Phenomena; bradycardia, AV block

Question 32

NONPHARMACOLOGICAL Rx OF ANGINA PECTORIS

Answer 32

Exercise Training
Angioplasty
Atherectomy
Stents
Intra-Aortic Balloon Counterpulsation
Coronary Artery Bypass Grafting (CABG)
? Angiogenic Gene Therapy