Antianginals Flashcards
Blood Flow Equation
PA / (RL + RS)
P should actuall be PA-PV, but PV is so small it is ignored
RL = large vessel resistence
RS = small vessel resistence
Angina Pectoris
Syndrome of ischemic heart diesease. angina pain occurs when O2 delivery is inadequate for myocardial requirements
Angina of Effort
Caused most often by a fixed obstruction which caused narrowing of coronary arteries. When exercise causes an increased demand for myocardial O2, there is an episode of myocardial ischemia and angina results.
Aka stable angina
Beta blockers, Ca channel blockers, & nitrodilators all useful, if single drug is inadequate, can use multiple
Variant Angina
Coronary insufficiency caused by localized vasospasm of large coronary vessels.
Can occur at rest or with exercise
Do NOT use beta blocker, but nitrodilators & Ca channel blockers are useful
Unstable Angina
Complicated pathology
occurs at rest or when there is a change in the nature of the angina which had previously been stable or when patients without history of angina show frequent and severe angina
**usually caused by thrombosis or ruptured plaque**
Rationale for Drug Therapy
- Increase O2 delivery
- coronary vasodilators
- nitrates
- Ca2+ blockers
- anti-thrombrotic & thrombolytic agents
- asa
- heparin
- dipyridamole
- plasminogen activators
- coronary vasodilators
- Decrease O2 demand
- venodilators
- nitrodilators
- arterial dilators
- Ca2+ blockers
- nitrodilators
- venodilators
Calcium Channel Blockers
useful for variant & angina of effort
orally active
inhibit L-type calcium channels, reducing intracellular Ca2+
affects impulse generation in SA node or AV node or calcium dependent action potentials
cardia contractility reduced
reduces peripheral vascular resistence
relaxes/dilates coronary arteries
Dihydropyridines
- Other Names
- Nifedepine
- Amlodepine
- Nicardepine
- Uses: variant angina & angina of effort
- Mechanism: Ca channel blocker
- decreases afterload -> decreases myocardial o2 demand
- increase coronary blood flow by dilating coronary arteries
- Contraindications:CHF
- Adverse Effects:
- hypotension
- peripherial edema
- flushing
- reflex tachycardia
- Other:
- vascular selective
- less effects on cardiac contractility
Verapamil
- Other Names: none mentioned
- Uses: very advantageous in atrial fibrilllation, flutter & tachycardia, & angina of effort & variant angina
- Mechanism: Ca channel blocker
- reduces Ca2+ current at AV & SA nodes-> decreases cardiac contractility (reduces myocardial o2 demand)-> arteriolar vasodilator (reduces afterload)
- Contraindications: CHF
- Adverse Effects
- constipation
- peripheral edema
- hypotension
- bradycardia
- heart block
- heart failure
- Other: very little vascular selectivity
Diltiazem
- Other names: none mentioned
- Uses: variant & angina of effort
- Mechanism: Ca channel blocker
- vasodilates coronary vessels without as much negative ionotropic effects as Verapamil
- Contraindications: CHF
- Adverse Effects:
- bradycardia
- hypotension
- peripheral edema
- heart block
- heart failure
Nitrodilators
NO enters vasular smooth muscle tissue->increases cGMP production->decreases Ca2+ levels->vasodilation
increases coronary blood flow, reduces preload by dilating veins, reduces afterload by dilating arterioles
inhibits platelet aggregation, coronary spasm, & restenosis (narrowing of blood vessels)
increases myocardial O2 to demand ratio
- Names: Nitroglycerin, isosorbide dinitrate, amyl nitrite
- Uses: all forms of angina & decreases MI size & mortaily
- Mechanism: see above
- Contraindications: none mentioned
- Adverse Effects:
- TOLERANCE (minimize by low dose interval therapy)
- orthostatic hypotension
- tachycardia
- throbbing headache
- methemoglobinemia (can lead to tissue hypoxia)
- toxicity with sildenafil
- Other: used in combination with ACE inhibitors & antithrombotics post MI
Nitroglycerin
- Other names: none
- Uses: all forms of angina & decreases MI size & post MI mortality
- Mechanism: nitrodilation
- Contraindications: none
- Adverse Effects: see nitrodilation
- Other:
- usually given sublingually, but can be transdermal paste for longer duration
- do NOT want to be metabolized by liver
Isosorbide Dinitrate
nitrodilator, usually given sublingually
oral preparation for longer duration
Amyl Nitrite
Inhalant nitrodilator
Beta Blockers
- Mechanism:
- decrease hr, contractility & bp
- reduce myocardial O2 demand
- Uses:
- chronic stable (extertional) angina
- angina with recent MI
- Differ:
- receptor subtype selectivity beta 1 or 2
- intrinsic sympathomimetic activity
- pharmacokinetics
- Adverse Effects:
- bradycardia, fatigue
- may exacerbate diabetes, asthma, PVD
- may cause nightmares
- may increase triglycerides
- may decrease HDL cholesterol (good ones)
- Contraindications:
- diabetics
- asthma patients
- PVD patients
- variant angina