Anti-Anginal Drugs

Front 1

Classic angina

Back 1

Due to coronary occlusion secondary to atherosclerosis
Angina appears with exercise/stress
Benefits by decreasing O2 demand

Front 2

Variant angina

Back 2

Transient, localized spasm
Usually occurs at rest
Major benefits by increasing 02 supply

Front 3

Unstable angina

Back 3

Acute Coronary Syndrome
Less responsive to nitroglycerin
Unpredictable
New onset or worsened

Front 4

Nitroglycerin

Back 4

Onset in 1-2 min.
Duration 15-30 min.

Front 5

Nitroglycerin MOA

Back 5

No travels across the membrane of smooth muscle and stimulates Guanylate Cyclase that coverts GTP to cGMP. cGMP stimulates cGMP-dependent protein kinase which phosphorylates Ca channels and myosin light chain phosphorylase. Prevents Ca from entering and crossbridges from forming.

Front 6

Nitroglycerin SEs and Adverse Effects

Back 6

SEs: Throbbing HA, orthostatic HTN
Adverse effects: Works by denitration: free nitrite is converted to NO
Adverse effects: Baroreceptor reflex, tolerance (give only every 8-12hr), Methemoglobin binding and subsequent hypoxia
CI: Patients on PDE-5 Inhibs

Front 7

Isosorbide dinitrate and mononitrate

Back 7

Less 1st pass metabolism than nitroglycerin and extended action oral preparation (12hr)
Isosorbide-5- mononitrate is a metabolite of dinitrate- no 1st pass met. and longer T1/2 (although others are usually sufficient)

Front 8

Spectrum of Ca Channel Blockers

Back 8

Dihydropyridines (Nifedipine and Amlodipine) cause peripheral vasodilation and no cardiosuppression.
Verapamil causes no dilation but extensive cardiosuppression.
Diltiazem causes some dilation and some suppression

Front 9

Nifedipine (Dihydropyridine)

Back 9

Ca Channel Blocker
Liver metabolism
Extensive plasma protein binding
Main effect is arteriole vasodilation
No cardiodepressant effects
Adverse effects: hypotn, reflex tach, flushing, edema (fixed by using extended release)

Front 10

Amlodipine (Dihydropyridine)

Back 10

Ca Channel Blocker
Slower absorption/ prolonged action
Coronary and peripheral vasodilation
Fewer adverse effects than Nifedipine

Front 11

Verapamil

Back 11

Ca Channel Blocker
Kidney elimination
Slows cardiac conduction
Good for variant angina bc it inhibits vasospasm
Adverse effects: Myocardial over-depression, development/worsening of HF

Front 12

Diltiazem

Back 12

Ca Channel Blocker
Liver metabolism
Midrange vasodilator and cardiac suppressor
Dilates epicardial/subendocardial arteries and inhibits vasospasm
Adverse effects: nausea, swelling, edema, arrhythmia
CI: ventricular dysfunction, conduction disturbance, systolic bp<90

Front 13

Beta Blockers MOA

Back 13

Competitive antagonist of catecholamines bind to the same receptor and prevent the Gprot-coupled receptor from activating the cAMP- PKA pathway. This results is decreases contractility, HR, and O2 consumption.
Decreases BP because the force of the pump is decreased.
**Use in combo with nitrate for prophylactic anti-anginal therapy

Front 14

Metoprolol

Back 14

Beta Blocker
B1 adrenergic receptor antagonist
Liver metabolism: CYP2D6 effect
Decrease HR, Contractility, prolongs diastole, anti-hypertensive (chronically)

Front 15

Beta Blockers adverse effects

Back 15

Cardiac depression
CNS: sedation, depression, insomnia
Beta2 Adrenergic blockade (Propranolol) *Asthma patients
Can exacerbate coronary spasm
Emergencies- reverse with glucagon or isoproterenol
Overdepression when given with CCB
Abrupt discontinuation leads to SNS overactivity

Front 16

Ranolazine

Back 16

Inhibits late Na current
For refractory angina and always adjunctive therapy
Inhibiting Na causes less intracellular Ca
CI: patients with long QT, patients taking Quinidine, Dofetilide, Sotalol, or CYP450 3A inhibitors, and those with liver/renal disease

Front 17

Paclitaxel

Back 17

Drug in a stent
Forms stable, nonfx microtubules that don't allow smooth muscle replication or proliferation

Front 18

Sirolimus

Back 18

Drug in stent
Inhibits microtubules or cell cycle kinase
Prevents smooth muscle replication/proliferation to prevent re-stenosis
Better distribution throughout vessel