3.4.2. Anataginal Drugs Flashcards
What is the goal of therapy with antianginal drugs?
Restore the balance between oxygen supply and demand in the ischemic region of the myocardium
What is the most important determinant of myocardial O2 demand?
HEART RATE - mediate high HRs w/antianginals to reduce symptoms and risk of sudden cardiac death
aldehyde reductase enzymes are necessary to do what to anti-anginals?
these enzymes liberate NO and allow vasodilation to occur
what drug does NOT need an aldehyde reductase? (ie, it spontaneously releases NO)
sodium nitroprusside
anti-anginals initially act on what membrane protein, and cause an increase in concentration of what intracellular compound?
they activate guanylyl cyclase, which increases intracellular [cGMP]
after cGMP-dependent kinases are activated by cGMP, what happens to myosin?
the contractile units are phosphorylated, inducing relaxation
which experience greater degrees of vasodilation from these drugs: veins, or arteries?
VEINS»_space; arteries. recall that venodilation induces a DECREASE IN PRELOAD that is desired in Pts w/angina because it decreases myocardial O2 demand
list three of the clinical uses of anti-anginals
angina, acute coronary syndrome, pulmonary edema
list four of the reported side effects of nitrates
reflex tachycardia (treat with beta-blockers), hypotension, flushing, headache
these drugs act on which arteries to specifically prevent coronary steal?
they dilate the large epicardial coronary vessels (vasodilators in general affect the entire body, as opposed to the heart specifically)
what is another useful way to decrease myocardial O2 demand?
Modest declines in systolic blood pressure (afterload) are useful for this
Fill in the blanks:
Nitrates have a ____ bioavailability due to metabolism by the liver, and have a very ____ half life with a fairly quick tolerance buildup
… they have a LOW bioavailability … and have a very SHORT half life …
(use these drugs PRN, like advil)
what is an absolute CONTRAINDICATION of nitrates?
NEVER USE NITRATES WITH SILDENAFIL - together they can cause hypotension, coronary steal, and MI
what are FOUR physiological actions of Ca-channel blockers?
1) Arteriolar dilator: reduce afterload
2) Reduce cardiac contractility
3) Decrease the heart rate
4) Decrease coronary resistance to increase coronary blood flow
what are three uses of Ca-channel blockers?
- Angina (these are very good for variant/Prinzmetal angina)
- Acute MI
- Hypertension
- ** Ca-channel blockers are the drugs of choice for treating STABLE and VARIANT angina ***