Pharm: Antianginal drugs Flashcards
What are the drug therapies for exertional angina?
Nitrates CCBs Beta blockers Ranolazine Ivabradine
Describe the mechanism of action of nitrates
Nitrates cause endothelium independent smooth muscle relaxation by activating GC to increase cGMP, dephosphorylates myosin light chains
Decreased venous return, decreased LV wall tension, reduced afterload and direct coronary artery vasodilation
Where in the body are nitrates most effective?
Systemic circulation
Clinical use of nitrates
Angina pectoris
Hypertensive emergencies
CHF
What are the most commonly used nitrates for angina?
Nitroglycerin
Isosorbide mono/dinitrate
Are nitrates used prophylactically?
Yes. They can be used as treatment or prophylaxis for exertional angina.
What are the side effects of nitrates?
Exaggeration of therapeutic effects: -orthostatic hypotension -reflex tachycardia -headache Tolerance can also develop
How do calcium channel blockers affect the action potential?
Slower AP upstroke, slowed conduction velocity
Inhibition of Ca influx during AP and also during diastole
What are the clinical uses of calcium channel blockers?
Angina Pectoris Hypertension Arrhythmias Hypertrophic cardiopyopathy Migraine Raynaud's phenomenon
What are the calcium channel blockers used for angina?
Dihydropyridines: nifedipine, nicardipine, amlodipine
Verapamil
Diltiazem
Bepridil
Which CCB has the strongest negative inotropic and chronotropic effects?
Verapamil has the strongest inotropic and chronotropic effects
Which CCB has the strongest vasodilatory effect?
Nifedipine
What are the side effects of verapamil and diltiazem?
Bradycardia
CHF
Heart block
Hypotension
What are the side effects of nifedipine?
Reflex tachycardia: major adverse effect
Peripheral edema
Hypotension
What are the effects of cAMP in cardiac muscle?
Inotropy, lusitropy, chronotropy, dromotropy
What are the most used beta blockers for exertional angina?
Cardioselective: atenolol and metoprolol
Describe the elimination of beta blockers
Liver: Propranolol, carvedilol, metoprolol
Kidney: atenolol, nadolol, sotalol
What are the side effects of beta blockers?
Bronchospasm
Peripheral vasospasm
Exaggerated cardiac effects: bradycardia, heart block
CNS effects: insomnia, depression, fatigue
What are the contraindications for beta blockers?
Acute CHF Bradycardia, heart block Peripheral vascular disease Insulin-dependent diabetes mellitus Sexual impotence Bronchospasm
What is ranolazine?
New class of antianginal drugs with a unknown mechanism Inhibits pFOX, decreasing beta oxidation
What is ivabradine?
Funny current inhibitor
Newest anti-anginal drug
What are the side effects of ivabradine?
Luminous phenomena, bradycardia, AV block
Describe the effect of metoprolol on exercise performance
Decreases variation in heart rate and reduces ischemic changes in response to exercise
What are the nonpharmacological treatments of angina pectoris?
Exercise training Angioplasty Atherectomy Stents Intra-aortic balloon counterpulsation CABG
