Vasodilators for Angina Pectoris DRUGS Flashcards
what are the 3 drugs that reduce cardiac size, rate, force and reduce cardiac o2 demand are?
vasodilators
B-blockers
CCB
what is the MOA for Nitric Oxide
activates and increases cGMP
What 2 drug classes decrease intracellular Ca2+
Beta blockers
CCB
What drug class prevents the depolarization of vascular smooth muscle?
Potassium channel openers
ex. Minoxidil (K+ opener)
what is the MOA of Nitrates
releases and increases NO into the SM cells leading to vasodilation
what is rapid and short acting nitrates primarily used for?
Acute angina pectoris
Hypertensive urgency
What are the 3 main side effects of Nitrate
- headache
- GERD
- Hypotension with syncope
Is there a difference in MOA between organic nitrate vs nitrous acid esters of polyalcohols
Not a big difference in MOA
What is the required activation for organic nitrates?
by mitochondrial aldehyde reductase (so the action is not immediate)
what are 3 examples of organic nitrates?
- nitroglycerin
- isosorbide dinitrate
- isosorbide mononitrate
What is the onset of action of sodium nitroprusside?
immediate b/c it is activated non-enzymatically
What is the most favorable route of nitrates
sublingual b/c it avoids the first pass effect
What is the bioavailability level of nitrates/nitrites?
Why?
Low bioavailability due to the liver containing an organic nitrate reductase that in activates nitrates/nitrites
What is the best route to administer nitroglycerin and isosorbide dinitrate? How long does it take to reach therapeutic levels?
sublingual route
within a few minutes
what is the total duration of effect for nitroglycerin and isosorbide dinitrate?
15-30 minutes (brief)
what are the other routes for nitroglycerin
transdermal
buccal absorption (slow release)
what is the effect of Nitroglycerin in the body?
relaxes all types of smooth muscle regardlesss of preexisting muscle tone
What muscle does nitroglycerin not have a direct effect on?
cardiac or skeletal muscle
what is the primary direct result of an effective dose nitroglycerin?
4
- marked relaxation in the veins
- increase venous capacity and decreased ventricular period
- pulmonary vascular pressure decreased
- heart size is decrereased
- if absense of heart failure= output is reduced
what pulsations are associated with the headache from nitrates/ nitrites
temporal artery pulsations
meningeal artery pulsations
Why are nitrates/nitrites beneficial for heart failure
vasodilators reduce preload and have a benefit for cardiac output
what are indirect effects of nitroglycerin
- decreased arterial pressure
- ^ results in tachycardia and increased cardiac contractility
- retention of salt and water
what is the result of nitRITE ion and hemoglobin?
produces methemoglobin (by oxidation of ferrous to ferric iron)
“methemoglobinemia”- needs a lot to cause significant rx
what inotropic effect on the heart does nitroglycerin have?
weak negative inotropic effect
what ways can nitrate already be present in the human body in high levels?
processed meats
well water
how can nitrites be used to treat cyanide poisoning?
methemoglobin iron
administration of sodium nitrite after cyanide exposure regenerates cytochrome
what do you follow sodium nitrite with for treatment of cyanide exposure
IV sodium thiocyanate
methylen blue