Chap 23 Antianginal Drugs Flashcards
Angina Pectoris
Result of myocardial ischemia caused by imbalance between myocardial blood supply and oxygen demand
Angina or chest pain is common
Ischemia
Ischemia*
Poor blood supply to an organ
Ischemic heart disease*
Poor blood supply to the heart muscle
Atherosclerosis
Coronary artery disease
Myocardial infarction (MI)*
Necrosis, or death, of cardiac tissue
Disabling or fatal
Types of Angina
Stable Angina*
“effort angina” triggered by physical or mental exertion
resolves with rest or nitrates
Unstable Angina*
new onset or worsening angina - unpredictable
rest/meds do not resolve
acute coronary syndrome; may lead to MI
Vasospastic Angina*
aka, variant/prinzmetal
occurs spontaneously, often at rest, common at night/early morning, especially exercise
more common in women and smokers
responds to nitrates: CCBs suppress(beta blockers do not)
Microvascular Angina*
Angina due to coronary microvascular dysfunction or vasospasm
accounts or chest pain up to 50% of pts w/out obstructive epicardial CAD
can occur with exertion or at rest
may respond less with exertion or at rest
be difficult to distinguish from epicardial angina, diagnose with PET or CMR
Drugs for Angina
Nitrates* or nitrites*
Beta blockers*
Calcium channel blockers (CCBs)
Goal: to increase blood flow to the ischemic myocardium, decrease myocardial oxygen demand, or both
Nitrates and Nitrites Forms& exs.
Available forms
Sublingual*
Chewable tablets
Oral capsules/tablets
Intravenous (IV) solutions*
Transdermal patches*
Ointments
Translingual sprays*
*Bypass the liver and the first-pass effect.
Nitroglycerin (both rapid and long acting)
Isosorbide dinitrate* (both rapid and long acting)*
Isosorbide mononitrate* (primarily long acting)
Nitrates and Nitrites: Mechanism of Action and Drug Effects
Cause vasodilation* because of relaxation of smooth muscles
Potent dilatingeffect on coronary arteries
Result:* oxygen to ischemic myocardial tissue
Used for prevention and treatment of angina
Nitrates and Nitrites: Indications
Treat stable, unstable, and vasospastic angina
Rapid-acting forms
Used to treat acute* anginal attacks*
Sublingual tablets; IV infusion
Long-acting forms*
Used to PREVENT anginal episodes
Nitrates: Contraindications
Known drug allergy
Severe anemia
Closed-angle glaucoma
Hypotension
Severe head injury*
Use of the erectile dysfunction drugs sildenafil (Viagra), tadalafil* (Cialis), and vardenafil *(Levitra)
Nitrates Adverse Effects
mostly due to vasodilatation
most common is throbbing headache 60% of pts
postural hypotension*
facial flushing
tachycardia
Tolerance develops rapidly on continued use
most practical way prevent nitrate tolerance, provide nitrate free intervals everyday
interval typically 10-12 hrs at night cause decreased demand on heart
Nitrate Tolerance
Occurs in patients taking nitrates around the clock or with long-acting forms
Prevented by allowing a regular nitrate-free period to allow enzyme pathways to replenish
Transdermal forms: remove patch at bedtime for 8 hours, then apply a new patch in the morning
Nitroglycerin
Prototypical nitrate
important drug used in symptomatic treatment of ischemic heart conditions such as angina
Routes—PO, SL, metered-dose aerosol that is sprayed under the tongue, IV, and topical
Large first-pass* effect with oral* forms
Beta Blockers
Mainstay in the treatment of several cardiovascular diseases
Angina*
MI*
Hypertension*
Dysrhythmias *
Cardioselective Beta Blockers mnemonic
HINT: M—E
Metoprolol
Atenolol
Nebivolol
Bisoprolol
Acebutolol
Betaxolol
Esmolol
B1 = 1 Heart
B2 = 2 Lungs
Beta Blockers: Mechanism of Action
Block beta1 receptors on the heart
Decrease heart rate, resulting in decreased* myocardial oxygen demand* and increased* oxygen delivery to the heart*
Decrease myocardial contractility, helping to conserve energy or decrease demand
Beta Blockers: Indications
Angina*
Antihypertensive*
Cardiac dysrhythmias*
Cardioprotective* effects, especially after MI*
Some used for migraine* headaches, essential tremors, and stage fright