MI drugs Flashcards
what causes stable angine
due to coronary atherosclerotic occlusion
what causes Vasospastic/variant/Prinzmetal angina
due to reversible reduction in coronary blood flow
anginal pain is usually due to release of what?
release of bradykinin and adenosine onto nociceptive afferents
duration for acute MI
sudden onset, last >/=30 min
duration of rest or unstable angina
<20 min
duration of angina
2-10 min
organic nitrates for MI
Nitroglycerin (GTN), Isosorbide Dinitrate (ISDN), Isosorbide Mononitrate (ISMN)
MOA of organic nitrates
Organic nitrates are prodrugs that must undergo denitrification by mitochondrial aldehyde reductase to yield NO
NO activates soluble GC, increasing cGMP –> cGK-1 activation:
- increase mitochondrial Ca2+ uptake
- decrease Ca2+ influx
- Phosphorylates MLCK
–> vasorelaxation
explain nitrate tolerance
When given acutely, nitrates have potent hemodynamic and therapeutic effects. However, these effects were lost rapidly during sustained therapy, almost completely when significant plasma concentrations are present throughout the 24-hr period. Tolerance develops early, and cannot be overcome with higher doses
how can nitrate effects be maintained (avoiding tolerance)
Nitrate effects could be maintained using dosing regimens that allow for a nitrate-free or low-nitrate concentration for several hours each day.
what nitrate undergoes hepatic and intravascular metabolism
Nitroglycerin
- fast acting
Nitroglycerin is very effective when given via what route
sublingual or transdermal
what forms of isosorbide dinitrate are available
Available in phasic, sustained release form –> QD dosing –> avoid tolerance
which nitrate does not undergo first pass hepatic metabolism – completely available
isosorbide mononitrate
what forms of isosorbide mononitrate are available
Available in sustained, phasic release form –> QD dosing –> avoid tolerance