Pharm 1 - Antianginal (Nierenberg)

Front 1

How to prevent HTN crisis when removing a pheo (it's like a sponge)...

Back 1

Phentolamine (alpha1 receptor blocker) and tie off veins/arteries.

Front 2

Factors for O2 supply

Back 2

Coronary flow
Aortic diastolic BP
O2 sat
Hgb
Flow to endocardium, epicardium, through collaterals
Diameter of large arteries

Front 3

Factors for O2 demand

Back 3

Wall tension
Ventricle radius
Wall thickness
Systolic BP (more afterload)
Preload
Heart rate
contractility

Front 4

Nitroglycerin

Back 4

Antianginal, vaso/venodilator
Reacts with nitrate receptor on SM cells, is reduced to NO2 and then NO. NO crosses into SM cells and activates guanylate cyclase leading to prod of cGMP from GTP.

cGMP relaxes SM cells by dephos of myosin light chains and this produces vaso and venodilation.

Very good for variant angina because of the spasms.

Front 5

Nitroglycerin
Pharmacokinetics

Back 5

High first pass effect orally. So it is given sublingual, through skin or IV

liver metabolizes it

Front 6

Nitroglycerin
Special considerations

Back 6

Excessive hypotension if pt is volume depleted
throbbing headhache, flushing

Not in conjunction with sildenafil

Remove patch before defilbrillation

Give 8 hour holiday per day to avoid tolerance.

Front 7

Beta-blockers in angina

Back 7

Less demand, more time for diastole.

Remember to never abruptly stop a beta blocker.

Not good for prinzmetals angina because beta receptors on vessels promote dilatation--you don't wanna block those or you will get more vasospasms..

Front 8

CEBs for angina

Back 8

e.g. verapimil or diltiazem.
Nifedipine can increase MI risk.
Very good for prinzmetals angina.

Front 9

Aspirin should be rx in people with...

Back 9

angina, MI, CV risk factors.
don't want the ruptured plaque to be able to recruit platelets.

Front 10

COX2 inhibitors contraind in...

Back 10

Pts with potential CV events.

This is because you stop the synth of PGI2 (prostacyclin) which dilates vessels and inhibits platelet aggregation.

So basically, thromboxane A2 (vasoconstriction and aggregation) is still being made and it is unopposed.

In general, you don't want these pts on any sort of NSAID.

Front 11

Key tx to vasospastic angina

Back 11

Intracoronary nitroglycerine immediately.

Then CEBs (BUT NOT BETA BLOCKERS!!!)

Front 12

Unstable angina/acute coronary syndrome

Back 12

Usually a chronically narrow coronary artery with the acute development of a ruptured plaque.

Imperative that the tx include suppression of platelet adhesion and aggregation.

Front 13

Aspirin

Back 13

Analgesic, anti-inflamm, antiplatelet, antipyretic.

Low doses - irrev inhibits COX1 in platelets (less thromboxane A2 so less vasoconstriction and platelet agg) and transiently inhibits COX2 in endothelium so there is less prostacyclin (less vasodilation and more platelet agg--but this is only transient)

MI in ER? First think you do is give aspirin.

Front 14

Aspirin
Pharmacokinetics

Back 14

F=60%
90% excreted as metabolites in urine

Front 15

Aspirin
Special considerations

Back 15

High doses can cause ulcerations of GI tract, bleeding disorders and tinnitus.

Inhibits tubular secretion of methotrexate and potentiates warfarin bleeding.

Avoid in pts with polyps, asthma

Front 16

Clopidogrel

Back 16

Platelet agg inhibitor
Blocks ADP receptors which prevents aggregation.

Good for primary or secondary prev of TIA, stroke, angina, MI, angioplasty, stent placement, acute coronary syndrome...

Aspirin and plavix often used together - must be careful of bleeding (especially in the brain).

Front 17

Clopidogrel
Pharmacokinetics

Back 17

Well absorbed.
Hepatic metabolism

Front 18

Clopidogrel
Special considerations

Back 18

Hemorrhage at almost any site.
May inhibit CYP3A4.

Front 19

Abciximab

Back 19

Adjunct to PCI to prevent ischemic complications. Also in tx of MI

Noncomp inhib of GPIIb/IIIa receptor. So less binding of fibrinogen, vWF and other ligands so less aggregation.

Must block 80% of these receptors.

Front 20

Abciximab
Pharmacokinetics

Back 20

IV bolus followed by IV infusion.

Front 21

Abciximab
Special considerations

Back 21

Contraind in presence of aneurysm, AV malformation, bleeding, coagulopathy, GI bleed, intracranial mass, retinal bleeding, stroke, surg, thrombocytopenia, trauma, fasculitis.

Front 22

Role of NO

Back 22

Causes vasodilation, inhib of platelet agg, phagocytosis, excitatory neurotransmission in the CNS.

Front 23

Give sildafenil with nitrates?

Back 23

NO!
Sildafenil inhibits PDE5 and that is what breaks down cGMP (which is increased with nitrates).