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33 Cards in this Set

  • Front
  • Back
What factors affect the demand of the heart and how can you use these to help with angina?
Ventricular wall stress (preload and afterload): dilate to help
HR, dec to help
Contractility, dec to help
What are the 3 types of angina?
Stable: Predictive pain pattern
Unstable: Changes, MI!
Printzmetal's or Variant: Vasospastic <-- Use DHP-CCB's
What is the MOA of Calcium channel blockers?
Inhibit Ca through L-type channels in HEART and VASCULAR SM.
Cardiac: neg inotropy, neg AV conduction, SAN depression
Vascular: dilate vessels to decrease afterload
What kinds of CI do they have compared to beta-blockers?
NOT CI in asthma, chronic bronchitis, peripheral arterial dz, diabetes UNLIKE beta blockers
What are the actions of calcium channel blockers related to angina?
Coronary relaxation (good for coronary vasospasms)
Arteriolar dilation, decrease afterload
Negative inotropy (not as much for dihydropyridines-vascular) -- can be CI in HF!
What are the toxicites of calcium channel blockers?
HA, flushing (vasodilation)
Increased urination due to increased Ca in bladder muscle

(Inappropriate cardiac- cardiac arrest, heart block, CHF- and vascular effects- postural hypotension, edema)
What are the dihydropyridines? What is their MOA
(pines) Nifedipine (reflex tachycardia and gum hypertrophy), Amlodipine (best), Nicardipine
Also Felodipine, Isradipine

Vascular specific Calcium channel blockers
What are the effects of dihydropyridines?
Inc HR (reflex tachycardia)
Dec BP! vascular effects <-- cause the greatest decrease in BP versus other CCB's
Inc CO (no cardiac effects really)

Cause ankle swelling bc peripheral dilation
What is the name of the phenylalkamine? What is its MOA?
Verapamil -- CCB. Cardiac specific!
Causes neg inotrop, dec AV conduction, SAN depression

Dec HR-- cardiac
some dec BP (slightly vascular)
no change in CO (effects cancel)
What is the use of verapamil?
Arrhythmias! BC blocks AVN conduction!
What is the AE of verapamil?
CCB's AE and CONSTIPATION! (vera wang wears wedding dresses to hide her constipation?)
Where are verapamil and diltiazem CI? What kinds of drug interactions does verapamil have?
Heart failure! (neg inotropy)
Heart block and bradycardia (affects both nodes)
Beta blockers -- excessive negative inotropy
Digoxin/Digitalis -- increases concentration of digoxin

Note: they do not cause reflex tachycardia bc they depress the SAN and neg inotropy but may be CI in heart problems
Name the benzothiazepine. What is its MOA?
Diltiazem - CCB with vascular and cardiac intermediate effects

Dilation in coronaries and arterioles
Neg inotropy, dec AVN conduction, SAN depression
What is the "anti-platelet" used for angina? What is its MOA?
Aspirin! Irrev inhibition of COX-1 and COX-2.
Anti-platelet, anti-pyretic, analgesic = without pain, anti-inflammatory
Where should you use aspirin?
Improve risk of survival post-MI and reduce risk of MI in stable/unstable angina
Reduce stroke in cerebral TIA
Reduce thromboembolism in pts with atrial fib and after valve replacement
When is aspirin NOT used?
Prophylaxis because of AE of bleeding
What are the nitrates used in angina?
Nitroglycerin
Isosorbide Dinitrate and Isosorbide Mononitrate
Erythrityl tetranitrate, Pentaerythitol tetranitrate
How is nitroglycerin administered?
Sublingual tablets, aerosol
Transdermal (patch instead of ointment)
Oral (1st pass effect)
IV for periop HTN, CHF, severe angina, pulmonary edema assoc with acute MI
How should nitrates be stored?
In amber bottles, protect from light and moisture
What is the MOA of nitrates?
Release of NO.
Nitroglycerin is metabolized to glutathione S-transferase in SMCs t NO
Intermediate step requires sulfhydryl groups!
Why do you need a 10-12 hour nitrate free interval?
TOLERANCE!
depletes sulfhydryl groups required for activation
What 2 enzymes does NO stimulate and what are their effects?
Stimulates guanylyl cyclase to increase cGMP, sequesters free Ca in SM -- relaxation (endothelium-independent mechanism)
Stimulates guanylate cyclase to inhibit platelet function
What are the 3 hemodynamic effects of nitrates?
Vascular SM relaxation (more venous, IV/high dose for arterial)
Coronary blood flow improvement
Non-vascular SM relaxation
What is the use of nitrates in angina?
Acute symptomatic relief of stable and unstable -- sublingual (but does NOT help with mortality-- beta blockers do)
Acute prophylaxis - sublingual
Long-term prophylaxis (tolerance!) - slow release, transdermal
What are the toxicities of nitrates?
HA (common! bc meningeal artery vasodilation)
Hypotension - esp with PDE-5 inhibitors
Tachyphylaxis with tolerance! (stop dosing at night)
What drug should you avoid when taking nitrates?
PDE-5 inhibitors (for erectile dysfunction)
When should you use isosorbide dinitrate and mononitrate? Which has better bioavailability and a longer half life?
Mono > Di > Tri
Good for oral prophylactic use, esp long-term
What four beta blockers are used in angina? Which are selective and nonselective? Which has lipid solubility?
Atenolol, metroprol, propanolol, nadolol

Atenolol, metoprolol - selective
lipid solubility: propanolol

These do not have intrinsic sympathetic activity so can be used to dec HR and red BP
How is propanolol metabolized? Why is it not used for angina?
CYP2D6 metabolism - needs constant dosing
Nonselective, so worse AE
How are atenolol and metoprolol better for angina versus propanolol and how are they excreted/metabolized?
Selective, better with dosing

Atenolol- unchanged by kidneys
Metoprolol- inactivated by hepatic metab
What is the MOA of beta blockers?
Block G proteins linked with adenyl cyclase, decrease cAMP, decrease beta receptor actions

Decrease HR, decrease contractility
What are the uses of beta blockers in angina?
Angina prophylaxis
Reduce risk of sudden death or reinfarction after MI (with aspirin)

NOT vasospastic angina (bc unopposed alpha receptors)
NOT tx acute angina (unlike nitrates)
What are the toxicities/CI of beta blockers?
Obstructive airway dz worsened
Heart block
Peripheral vascular dz, Raynaud's
Diabetes (masks hypoglycemia)
Get REBOUND angina after abrupt stop
CNS if lipophilic (dizziness, fatigue, depression, lethargy, dreams)
IMPOTENCE, wheezing, dyspnea