Antianginal Drugs Overview

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Questions and Answers

What characterizes unstable angina compared to stable angina?

  • Relief with physical activity
  • Pain does not respond to rest (correct)
  • Chest pain occurs with less effort (correct)
  • Shorter duration of symptoms

Which condition is primarily associated with coronary artery spasm?

  • Acute coronary syndrome
  • Stable angina
  • Prinzmetal angina (correct)
  • Unstable angina

Which medication class is generally ineffective for treating vasospastic angina?

  • Calcium channel blockers
  • Sodium channel blockers
  • Organic nitrates
  • Beta-blockers (correct)

What is a potential outcome of acute coronary syndrome if not treated promptly?

<p>Myocardial infarction (C)</p> Signup and view all the answers

What role do antianginal drugs play in managing angina symptoms?

<p>They balance cardiac oxygen supply and demand (D)</p> Signup and view all the answers

What feature differentiates Prinzmetal angina from other types of angina?

<p>Attacks occur at rest (C)</p> Signup and view all the answers

Which of the following is a benefit of using beta-blockers for angina management?

<p>Decrease oxygen demand at exertion (C)</p> Signup and view all the answers

What is a key trigger that can initiate anginal symptoms?

<p>Emotional stress (C)</p> Signup and view all the answers

Why should nonselective β-blockers be avoided in patients with asthma?

<p>They can worsen bronchospasm. (C)</p> Signup and view all the answers

Which condition requires careful monitoring when using β-blockers?

<p>Peripheral vascular disease (A)</p> Signup and view all the answers

What is the primary therapeutic effect of calcium channel blockers (CCBs) in exercise-induced angina?

<p>Decrease myocardial oxygen consumption (D)</p> Signup and view all the answers

Which type of calcium channel blocker is specifically effective for variant angina?

<p>Nifedipine (A)</p> Signup and view all the answers

What is the effect of nondihydropyridine CCBs on heart rate?

<p>Decrease the heart rate (A)</p> Signup and view all the answers

What essential mechanism is involved in the action of organic nitrates for angina relief?

<p>Conversion to nitric oxide (D)</p> Signup and view all the answers

What characterizes stable angina?

<p>The pattern of chest pain does not vary over time. (C)</p> Signup and view all the answers

Which of the following is contraindicated when using nondihydropyridine CCBs?

<p>Preexisting depressed cardiac function (B)</p> Signup and view all the answers

Which type of angina is commonly associated with transient symptoms?

<p>Stable angina (D)</p> Signup and view all the answers

Why should short-acting dihydropyridine CCBs be avoided in patients with coronary artery disease (CAD)?

<p>They are linked to increased mortality after myocardial infarction. (A)</p> Signup and view all the answers

Which patient demographic is most likely to experience atypical symptoms of angina?

<p>Diabetic patients (D)</p> Signup and view all the answers

What is a common lifestyle modification recommended for managing angina?

<p>Smoking cessation (C)</p> Signup and view all the answers

What is a defining feature of unstable angina?

<p>It can occur at rest and may indicate a more serious condition. (B)</p> Signup and view all the answers

Which of the following is NOT a typical symptom of angina pectoris?

<p>Constant sharp pain that does not change (D)</p> Signup and view all the answers

What underlying condition primarily causes stable angina?

<p>Atherosclerosis leading to fixed obstruction (C)</p> Signup and view all the answers

What is typically indicated by the presence of dyspnea during angina episodes?

<p>It suggests that angina is becoming unstable. (D)</p> Signup and view all the answers

What is the primary role of cGMP in smooth muscle relaxation?

<p>Mediates dephosphorylation of myosin light chain (C)</p> Signup and view all the answers

What effect do organic nitrates have on the coronary vasculature?

<p>Increase oxygen supply to the myocardium (B)</p> Signup and view all the answers

How can tolerance to organic nitrates be effectively managed?

<p>By implementing daily 'nitrate-free intervals' (C)</p> Signup and view all the answers

Which drug is preferred for the prompt relief of effort-induced angina?

<p>Nitroglycerin (C)</p> Signup and view all the answers

What is a common adverse effect associated with organic nitrates?

<p>Postural hypotension (C)</p> Signup and view all the answers

What pharmacokinetic characteristic does Isosorbide mononitrate have compared to Nitroglycerin?

<p>Slower onset of action (C)</p> Signup and view all the answers

What physiological mechanism does Ranolazine act upon?

<p>Late sodium channel openings (D)</p> Signup and view all the answers

How does the interaction between phosphodiesterase type V inhibitors and nitrates present a clinical risk?

<p>It leads to severe hypotension (B)</p> Signup and view all the answers

Flashcards

Coronary Artery Disease (CAD)

A condition where the coronary arteries narrow, restricting blood flow to the heart and causing chest pain.

Stable Angina

A type of chest pain caused by reduced blood flow to the heart muscle, usually triggered by physical exertion.

Unstable Angina

Chest pain that is more severe and frequent, occurring at rest or with minimal exertion, and may be a sign of an impending heart attack.

Prinzmetal Angina

Chest pain that occurs at rest due to spasms in the coronary arteries, often triggered by cold temperatures or stress.

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Myocardial O2 Demand

The amount of blood that the heart needs to supply to the body during exertion.

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Myocardial O2 Supply

The amount of blood that the heart can actually deliver through the coronary arteries.

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Myocardial O2 Supply and Demand

The balance between the amount of blood the heart needs and the amount it can actually deliver.

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Pathogenesis of Stable Angina

Atherosclerosis causes a fixed obstruction in the coronary arteries, reducing blood flow, leading to ischemia and angina during exertion.

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Acute Coronary Syndrome (ACS)

A condition characterized by sudden, severe chest pain caused by a complete or partial blockage of a coronary artery, often due to a ruptured plaque.

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Antianginal Drugs

A group of drugs used to treat angina by balancing oxygen supply and demand.

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Beta-blockers

Drugs that block the effects of adrenaline, reducing heart rate and force of contraction, lowering oxygen demand.

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Beta-blockers for angina

Beta-blockers are generally recommended for all patients except those with vasospastic angina.

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Beta-blockers and vasospastic angina

Beta-blockers are not effective and can even worsen vasospastic angina.

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Beta-blockers with intrinsic sympathomimetic activity

Beta-blockers that also have a mild stimulating effect on the heart should be avoided.

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Beta-blockers and Bradycardia

Beta-blockers should not be used in individuals with a slow heart rate, as it could worsen their condition.

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Nonselective Beta-blockers and Asthma

Nonselective beta-blockers should be avoided in patients with asthma due to their potential to trigger bronchospasm.

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How do CCBs work?

Calcium channel blockers (CCBs) work by blocking the entry of calcium into cardiac and smooth muscle cells, leading to vasodilation of coronary and peripheral arteries.

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Dihydropyridine CCBs and Variant Angina

Dihydropyridine CCBs, like amlodipine and nifedipine, are effective for variant angina due to their potent vasodilation effect.

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Short-acting Dihydropyridines and CAD

Short-acting dihydropyridines should be avoided in patients with coronary artery disease (CAD) because they may increase the risk of heart attack.

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Verapamil: Effects on the Heart

Verapamil, a nondihydropyridine CCB, directly slows conduction in the heart, leading to decreased heart rate, contractility, and blood pressure.

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Diltiazem: Useful for Variant Angina

Diltiazem, a nondihydropyridine CCB, is useful for variant angina because it can relieve coronary artery spasms.

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Organic Nitrates: Mechanism of Action

Organic nitrates, like nitroglycerin, are converted into nitric oxide, which leads to vasodilation and reduced myocardial oxygen demand.

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How do organic nitrates affect blood vessels?

Organic nitrates cause dilation of systemic arteries and veins, decreasing afterload and preload, and reducing oxygen demand by the heart.

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How do organic nitrates affect coronary arteries?

Organic nitrates directly dilate coronary arteries, improving the supply of oxygen to the heart muscle.

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What is nitrate tolerance?

Tolerance to nitrates develops rapidly as blood vessels become desensitized to vasodilation.

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When are nitrate-free intervals usually recommended?

Nitrates are typically taken in the late afternoon/early evening to avoid tolerance.

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How do the onset times for nitroglycerin and isosorbide mononitrate differ?

Nitroglycerin acts quickly, within about 1 minute, while isosorbide mononitrate takes around 30 minutes to take effect.

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Which drug is best for rapid relief of angina and how is it usually administered?

Nitroglycerin is the drug of choice for rapid relief of angina because it has a fast onset of action. It's often taken sublingually or as a buccal spray.

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Why is nitroglycerin often administered sublingually or transdermally?

Nitroglycerin undergoes extensive first-pass metabolism, meaning a significant portion is broken down before reaching the bloodstream. Therefore, it's often given sublingually or transdermally to bypass the liver.

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What makes isosorbide mononitrate more effective than nitroglycerin?

Isosorbide mononitrate has improved bioavailability, meaning more of it reaches the bloodstream, due to less first-pass metabolism.

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Study Notes

Antianginal Drugs

  • Coronary artery disease (CAD) is a significant cause of mortality globally.
  • Atherosclerosis obstructs blood flow, creating an imbalance between myocardial oxygen supply and demand.
  • Angina pectoris involves chest pain that can radiate to other areas like the neck, jaw, back, and arms.
  • Symptoms can include indigestion, nausea, vomiting, and sweating.
  • Unstable angina involves worsening chest pain, increasing frequency, duration, and intensity, even at rest; it can progress quickly to a heart attack (MI).
  • Prinzmetal angina (variant angina) is a less common type that occurs at rest, linked to spasms in the coronary arteries.
  • Stable angina is the most common type, triggered by exertion; pain generally subsides with rest or nitroglycerin.
  • Antianginal drugs aim to balance myocardial oxygen supply and demand through various mechanisms.

Classes of Antianginal Drugs

  • β-blockers: Reduce myocardial oxygen demand, frequency, and severity of angina attacks, improving exercise tolerance and mortality; however, they may worsen vasospastic angina in some patients.
  • Calcium channel blockers (CCBs): Prevent calcium from entering cardiac and smooth muscle cells, leading to vasodilation; effective for both exercise-induced and vasospastic angina.
  • Organic nitrates: Convert to nitric oxide (NO), relaxing smooth muscles and causing vasodilation, which reduces myocardial oxygen demand and improves oxygen supply. However, tolerance is common and can be overcome through "nitrate-free intervals."
  • Sodium channel blockers (Ranolazine): Reduce sodium influx during the plateau phase, affecting intracellular calcium levels and potentially reducing oxygen demand.

Specific Drug Information

  • β-blockers: Should be used with caution in patients with diabetes, peripheral vascular disease, or chronic obstructive pulmonary disease (COPD).
  • Calcium channel blockers (CCBs): Dihydropyridines (e.g., nifedipine) are more effective for vasospastic angina, while non-dihydropyridines (e.g., verapamil, diltiazem) are beneficial in other types. Short-acting dihydropyridines are often avoided in CAD patients due to increased risk of heart attack (MI).
  • Organic nitrates: Nitroglycerin is often preferred for quick relief of angina. Tolerance can be a concern, so "nitrate-free intervals" are often recommended.
  • Sodium channel blockers (Ranolazine): This drug can also have an antiarrhythmic effect and cause a prolonged QT interval.

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