Exam 1: Lecture 11, Angina Flashcards
3 Types of angina
Stable
Unstable
Variant
3 classes of drugs for angina
Organic nitrates
Calcium channel blockers
Beta blockers
Nitrates: Prototype
Nitroglycerin
Nitrates: MOA
Increase cGMP which decreases Ca that mediates contraction and dephosphorylates MLC’s leading to relaxation
Nitrates: Applications
Angina, acute coronary syndrome
Nitrates: notables
Undergoes large first pass effect, given sublingually to avoid
Tachyphylaxis - tolerance; decrease effect of same drug dose given repeatedly, so have to give it time
Interaction with sildenafil, don’t take together…space by 6 hours
Which types of Angina can nitrates be used for?
Stable
Variant/Vasospastic/Prinzmetal’s
Unstable
Beta-blockers: Prototype
Propranolol
Beta-blockers: MOA
Competitive inhibitors of Ne and EPi at B1 (cardiac) and B2 (smooth muscle/lung) receptors, inhibit renin release
Beta-blockers: Applications
Angina, hypertension, arrhythmias, migraine, performance anxiety
How many generations of Beta-blcokers?
3
1st = non-selective 2nd = B1 selective 3rd = Vasodilatory
Which types of Angina can Beta-blockers be used for?
Stable (mainly used here)
Unstable
Beta-blockers notables
By using drugs that block B2 receptors, it leaves the vasoconstricting alpha receptors unopposed and potentially making angina worse
Have to be weened off, ~ 3 weeks
Beta-blockers contraindicated in….
Asthma
Variant Angina
bronchospasm
AV/SA node dysfunction
Ca Channel blockers: prototype
Verapamil (nondihydropyridine)
Nifedipine (dihydropyridine)
Ca Channel blockers: MOA
Inhibition of L-type calcium channels,
Blocks calcium channels in the SR
Ca Channel blockers: Applications
Angina, hypertension, supraventricular tachyarrhythmias
Ca Channel blockers: notables
High 1st past effect,
High Albumin binding = cause for Drug-Drug interactions
Extensive metabolism, due to CYP450
Which types of Angina can Ca Channel-blockers be used for?
Stable
Variant/Vasospastic/Prinzmetals
unstable if pt refractory for other 2
MONA
Morphine, Oxygen, Nitroglycerin, Aspirin = treatment of Angina in ER
Monday disease and Nitrate tolerance
Those working in chemical plants or who get exposed to nitrates develop a tolerance during the week, then lose some of it over the weekend. When they return to work on Monday the exposure to nitrates can make them feel bad, but they regain tolerance and are better following days
Drugs to treat stable Angina
Nitrates, Ca Channel blockers, Beta-blockers
Drugs to treat Variant Angina
Nitrates, Calcium channel blockers
Drugs to treat Unstable Angina
Acute coronary syndrome must be treated with (anti platelets, aspirin, clopidogrel, heparin) plus nitrates and Beta-blockers
For refractory disease, calcium channel blockers used.
Most effective calcium channel blocker?
Verapamil in all aspects…ie Vasodilation, decreasing cardiac contractility, etc
Reperfusion
is when you have reoxygenation, when you reoxyenate it can trigger cell death by activating mPTP
Importance of Foam Cells
Macrophages that turn into these foam cells from collecting ApoB proteins. will then cause a build of of ApoB-Lp, instead of digesting them.
foam cells = responsible for formation of plaques
What happens when foam cells die?
Apoptosis, then all the stuff in the cell will build up and a necrotic core will form. This fibrous cap is weakened, then thrombus comes and binds to ruptured region and will lead to blocked vasculature
This is due to efferocytosis not being able to occur (clean up)
raynauds syndrome
cold sensitivity and poor circulation to extremities due to limited coruscation
usually in women
Vasospastic/Prinzmetals Angina
increase vasoconstriction and decrease vasodilation
drugs increasing oxygen delivery?
Nitrates and Calcium channel blockers
Drugs decreasing oxygen demand?
Nitrates/beta blockers/calcium channel blockers
Beta blockers will..
decrease heart rate, blood pressure and contractility
which decrease oxygen requirements at rest and exercise (effecting oxygen demand)
Main focus of beta blockeres
B1 receptor in cardiac cell…
Beta-blockers will reduce ca moving into the cell/ and from SR
B2 mediate vasodilation
Why beta-blockers not used in spastic angina/asthma?
By blocking beta receptors in vasculature, you’ll have more alpha receptors open which cause vasoconstriction
Ranolazine
Not common in angina, but used in patients who don’t respond to other options
MOA: blocks Late sodium channel, preventing Na/ca exchange and decreases contraction
Aspirin
Rational = anti platelet activity
COX1 inhibitor, it prevents cascade involved in platelet aggregation
given to patients with unstable angina
