Cardiovascular Pharmacology

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Questions and Answers

Which of the following drug classes is NOT typically used as a primary treatment for cardiovascular conditions?

  • Inotropic Drugs
  • HMG CoA Reductase Inhibitors
  • Anti-arrhythmics
  • Anticholinergics (correct)

What is the primary mechanism of action of HMG-CoA reductase inhibitors (statins)?

  • Promoting the synthesis of HMG-CoA reductase enzyme
  • Inhibiting the absorption of cholesterol from the intestine
  • Blocking the conversion of HMG-CoA to mevalonate (correct)
  • Increasing the conversion of squalene to cholesterol

A patient is prescribed a drug that blocks alpha1-adrenergic receptors. What is the MOST likely intended effect of this medication?

  • Increased heart rate
  • Bronchodilation
  • Vasodilation (correct)
  • Vasoconstriction

Which of the following drug classes primarily affects myocardial contractility?

<p>Inotropic Drugs (D)</p> Signup and view all the answers

A patient with a history of arrhythmia is prescribed amiodarone. Which Vaughn Williams class does Amiodarone belong to?

<p>Class III (D)</p> Signup and view all the answers

A researcher is investigating a novel compound that appears to inhibit cholesterol synthesis, but not through direct inhibition of HMG-CoA reductase. At which of the following steps in the cholesterol biosynthesis pathway could this compound potentially be acting?

<p>Conversion of squalene to cholesterol (D)</p> Signup and view all the answers

A clinical trial is evaluating a new drug that is hypothesized to both reduce platelet aggregation and directly inhibit the synthesis of cholesterol by a mechanism independent of HMG-CoA reductase inhibition. If the drug is effective, which combination of the following established drug classes would it MOST likely replace?

<p>An antiplatelet agent and a bile acid sequestrant (A)</p> Signup and view all the answers

What is the recommended action if a patient on Warfarin misses a dose?

<p>Skip the missed dose and continue with the regular schedule, but record the missed dose and inform the doctor. (D)</p> Signup and view all the answers

Why is Warfarin use problematic during pregnancy?

<p>It crosses the placental barrier and can cause bleeding and other complications in the fetus. (B)</p> Signup and view all the answers

What is the primary mechanism of action of Aspirin at lower doses?

<p>Inhibition of platelet aggregation by blocking thromboxane A2 production. (D)</p> Signup and view all the answers

Clopidogrel requires first-pass metabolism. What is the significance of this?

<p>It means Clopidogrel must be metabolized into an active form, potentially leading to variability in drug response. (B)</p> Signup and view all the answers

Which of the following statements best describes the dual action of aspirin related to cyclooxygenase (COX) inhibition and its implications?

<p>By inhibiting both COX-1 and COX-2, aspirin reduces thromboxane A2, preventing platelet aggregation, and diminishes prostaglandin production, alleviating inflammation but increasing the risk of GI bleeding. (C)</p> Signup and view all the answers

Which medication is classified as a thrombolytic?

<p>Alteplase (Activase, TPA) (B)</p> Signup and view all the answers

What is the primary mechanism of action of heparin?

<p>Accelerating the anticoagulant cascade via antithrombin III (D)</p> Signup and view all the answers

Which statement is correct regarding low-molecular-weight heparins (LMWHs)?

<p>They achieve anticoagulation with a lower risk of bleeding compared to heparin. (C)</p> Signup and view all the answers

What is the mechanism of action of warfarin?

<p>Inhibits vitamin K epoxide reductase (C)</p> Signup and view all the answers

A patient taking warfarin should be educated to maintain a consistent intake of which of the following?

<p>Vitamin K (D)</p> Signup and view all the answers

What laboratory value is most important to monitor in a patient receiving warfarin?

<p>International Normalized Ratio (INR) (D)</p> Signup and view all the answers

Why are patients instructed to take antiplatelet drugs with or after food?

<p>To reduce the risk of gastric bleeding (C)</p> Signup and view all the answers

Which of the following drugs is used to manage intermittent claudication?

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

A patient on warfarin with an INR of 6.0 is at a significantly increased risk for bleeding. Which of the following interventions is MOST crucial to include in the plan of care?

<p>Prepare to administer vitamin K and consider fresh frozen plasma per physician order. (C)</p> Signup and view all the answers

A patient with a history of heparin-induced thrombocytopenia (HIT) requires anticoagulation. Which of the following medications would be MOST appropriate and safe to administer?

<p>Fondaparinux, a synthetic pentasaccharide that selectively inhibits factor Xa (B)</p> Signup and view all the answers

Which of the following is a common indication for the use of statins?

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

Which laboratory test should be regularly monitored in patients taking statins?

<p>Liver function test (B)</p> Signup and view all the answers

How does grapefruit consumption affect statin metabolism?

<p>Grapefruit reduces the body's ability to break down statins, potentially increasing side effects. (C)</p> Signup and view all the answers

A patient on statins reports muscle pain and weakness. Which lab value is MOST important to assess?

<p>Creatine kinase (CK) (D)</p> Signup and view all the answers

What is the primary characteristic of hypercoagulability?

<p>An increased tendency for blood to clot. (B)</p> Signup and view all the answers

Why is grapefruit consumption typically discouraged for patients taking statins?

<p>Grapefruit juice can inhibit certain enzymes, increasing statin levels in the blood and the risk of side effects. (C)</p> Signup and view all the answers

Which of the following is NOT a commonly reported side effect of statin medications?

<p>Improved kidney function (C)</p> Signup and view all the answers

Which of the following is an example of a hypo-coagulable condition?

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

Heparin functions as an anticoagulant by which mechanism?

<p>Inhibiting clotting factors. (C)</p> Signup and view all the answers

A patient taking warfarin is prescribed a statin. Which consideration is MOST important regarding bleeding risk?

<p>Lovastatin, rosuvastatin, and simvastatin may increase bleeding risk when administered with warfarin. (D)</p> Signup and view all the answers

A researcher is investigating the effects of a novel drug on cholesterol metabolism and discovers that the drug increases the expression of HMG-CoA reductase. What predictable outcome might the researcher observe in cells treated with this drug?

<p>Increased cholesterol synthesis, potentially resulting in elevated intracellular cholesterol concentrations. (C)</p> Signup and view all the answers

Aspirin's antiplatelet action is primarily due to its...

<p>Inhibition of COX-1 and subsequent reduction in thromboxane A2 (TXA2). (D)</p> Signup and view all the answers

Which drug classification directly inhibits the action of thrombin?

<p>Direct Thrombin Inhibitors (D)</p> Signup and view all the answers

A clinical trial is evaluating a new statin analog, and preliminary results indicate a significant reduction in LDL cholesterol levels but also an unexpected increase in the expression of ryanodine receptors in skeletal muscle cells WITHOUT any reported muscle pain. Considering the known mechanism of action of statins and their effects on ryanodine receptors, what might be a plausible explanation for the absence of myalgia in this scenario?

<p>The statin analog selectively modulates ryanodine receptors, preventing abnormal calcium release and subsequent muscle damage, while still lowering cholesterol. (A)</p> Signup and view all the answers

What is the mechanism of action of Glycoprotein IIB/IIIA receptor antagonists?

<p>Blocking the final common pathway for platelet aggregation. (A)</p> Signup and view all the answers

How do low-molecular-weight heparins (LMWH) differ from unfractionated heparin in terms of mechanism?

<p>LMWH primarily inhibits Factor Xa, with less effect on thrombin, while unfractionated heparin inhibits both thrombin and Factor Xa equally. (A)</p> Signup and view all the answers

A patient with a known hypersensitivity to aspirin requires an antiplatelet agent. Which of the following would be the MOST appropriate alternative?

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

A researcher is investigating novel approaches to prevent thrombosis. If they aim to selectively target and inhibit the intrinsic pathway of coagulation, which factor would be the MOST specific and effective target, considering minimal impact on the extrinsic pathway?

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

Flashcards

Inotropic Drugs

Increase heart contraction force. Examples include adrenergic drugs.

Anti-adrenergic Drugs

Block the effects of adrenergic neurotransmitters, lowering blood pressure.

Vasodilator Drugs

Dilate blood vessels, reducing blood pressure.

Anti-arrhythmic Drugs

Regulate heart rhythm, preventing arrhythmias.

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Statins

Reduce cholesterol levels by blocking HMG-CoA reductase.

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HMG-CoA Reductase

Enzyme that converts HMG-CoA to mevalonate, a key step in cholesterol synthesis.

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Cholesterol Biosynthesis Pathway

Acetic acid is converted into squalene, which then becomes cholesterol.

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Statins: Mechanism of Action

HMG-CoA reductase inhibitors reduce cholesterol production by inhibiting the HMG-CoA reductase enzyme.

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Statin Indications

Statins are used to treat high cholesterol, reduce CAD risk, and prevent MI or stroke.

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Examples of Statins

Common statin drugs include Atorvastatin (Lipitor), Simvastatin (Zocor), and Rosuvastatin.

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Common Statin Side Effects

GI symptoms and increased liver enzymes (ALP, ALT, bilirubin) are common side effects.

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Severe Statin Side Effects

Severe side effects include muscle pain (myopathy) and rhabdomyolysis (muscle breakdown).

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Statins and Ryanodine Receptors

Statins may damage muscle cells' ryanodine receptors, which control calcium release.

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Monitoring Liver Function

Regularly monitor Liver Function Tests (LFTs) when a patient is taking statins.

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Monitoring Creatine Kinase (CK)

Regularly monitoring Creatine Kinase (CK) levels is important while on statins.

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Grapefruit and Statins

Patients taking statins must avoid grapefruit.

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Warfarin Missed Dose

Do not compensate for a missed dose by doubling the next one. Keep a record of missed doses and inform your doctor or pharmacist during your next consultation.

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Warfarin & Pregnancy

Warfarin can cross the placental barrier, leading to fetal plasma levels similar to the mother's. This can cause bleeding in the fetus and is linked to complications like spontaneous abortion and stillbirth.

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Aspirin's Mechanism

Aspirin blocks cyclooxygenase (COX) enzymes, reducing thromboxane A2, inhibiting platelet activation and aggregation, all of which reduces clot formation.

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Aspirin Dosage in ACS

Aspirin is used in Acute Coronary Syndrome with a loading dose of 160-300 mg orally, followed by a maintenance dose of 80mg daily alongside a P2Y12 inhibitor such as Plavix.

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Clopidogrel Activation

Clopidogrel (Plavix) is a prodrug that requires initial metabolism in the liver to become effective.

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Hypercoagulability

Increased tendency of blood to form clots.

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Hypocoagulability

Reduced ability of blood to clot, leading to increased bleeding risk.

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Anticoagulants

Drugs that prevent the formation of blood clots.

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Heparin

A natural substance from liver; prevents clot formation.

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LMWH

A type of anticoagulant with a lower molecular weight than standard heparin.

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Direct Thrombin Inhibitors

Directly inhibit thrombin to prevent clot formation.

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Factor Xa Inhibitors

Inhibit factor Xa to prevent clot formation.

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Antiplatelets

Prevent platelet aggregation to inhibit clot formation.

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Aspirin (as antiplatelet)

Inhibits COX-1 to reduce thromboxane A2 production, preventing platelet aggregation.

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ADP Receptor Blockers

Block ADP receptors on platelets, inhibiting their activation and aggregation.

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Abciximab (ReoPro)

Blocks platelet aggregation by binding to glycoprotein IIb/IIIa receptors on platelets.

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Drugs for Intermittent Claudication

Medications to alleviate intermittent claudication symptoms.

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Thrombolytics

Dissolve existing blood clots by activating plasminogen to form plasmin.

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Examples of Thrombolytics

Alteplase (Activase, TPA), Reteplase (Retavase), Streptokinase (Kabikinase), tenecteplase, urokinase.

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Heparin's Action

Combines with antithrombin III, accelerating the anticoagulant cascade of reactions that prevents thrombosis formation; inhibits thrombin and prevents fibrin clot formation.

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Low Molecular Weight Heparins (LMWH)

Same anticoagulation effect as heparin but with a lower risk of bleeding.

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Examples of LMWH

Enoxaparin (Clexane, Lovenox), Nadroparin (Fraxiparine), Dalteparin, Tinzaparin.

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Warfarin's Action

Inhibits vitamin K epoxide reductase, reducing production of vitamin K-dependent clotting factors.

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Warfarin Indications

Prevent/treat thromboembolism and arterial embolism in patients with atrial fibrillation or prosthetic heart valves.

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Warfarin - Nursing Considerations

Monitor INR to maintain therapeutic range, avoid Vitamin K-rich foods, prevent bleeding.

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Study Notes

  • Cardiac drugs are categorized into seven major classes.

Inotropic Drugs

  • Adrenergic drugs, also known as sympathomimetic amines, are one type of inotropic drug
  • Anticholinergics, including antimuscarinics and cholinergic blockers, constitute another type
  • Digitalis glycosides, such as Digoxin, are also included

Anti-adrenergic Drugs

  • Alpha1-adrenergic blockers act as antagonists.
  • Beta-adrenergic receptor antagonists are also part of this category.

Vasodilator Drugs

  • Angiotensin-Converting Enzyme Inhibitors
  • Angiotensin II type 1 Receptor Antagonists
  • Calcium Channel Blockers
  • Direct vasodilators and Organic Nitrates are also included in this category.

Anti-arrhythmic Drugs

  • Class I, Class II, Class III, and Class IV anti-arrhythmics
  • Other agents include amiodarone, digoxin, and adenosine

Diuretics

  • Refer to specific lectures on the pharmacological treatment of the urinary system for details.

Antiplatelets, Anticoagulants, and Thrombolytics

  • These drugs affect blood clotting mechanisms

Antilipemic Drugs

  • HMG COA Reductase Inhibitors (statins)

HMG-CoA Reductase Inhibitors

  • Statins inhibit cholesterol production and are classified as antilipemic drugs
  • The cholesterol biosynthesis pathway converts acetic acid into squalene, eventually forming cholesterol
  • Early steps involve reducing HMG-CoA to mevalonate via the HMG-CoA reductase enzyme, followed by steps until squalene and cholesterol are produced

Mechanism of Action

  • HMG-CoA reductase inhibitors (statins) block the HMG-CoA reductase enzyme, which converts HMG-CoA to mevalonate
  • Ultimately, this reduces cholesterol production.

Indications

  • Statins treat hypercholesterolemia, reducing the risk of CAD (coronary artery disease), prevents myocardial infarction or strokes
  • Examples include Atorvastatin (Lipitor), Simvastatin (Zocor), fluvastatin, lovastatin, pravastatin, and rosuvastatin

Side Effects

  • Gastrointestinal symptoms
  • Most cholesterol-lowering drugs may damage liver function, increasing alkaline phosphatase (ALP), alanine transaminase (ALT), and bilirubin levels
  • Other hepatic effects may include pancreatitis, drug-induced hepatitis, cirrhosis, and easy bleeding
  • Lovastatin, rosuvastatin, and simvastatin may elevate the risk of bleeding, especially when taken with warfarin
  • Severe but rare side effects include muscle pain, myopathy, and rhabdomyolysis (muscle tissue breakdown)
  • Statins can damage muscle cells' gatekeeper proteins, called ryanodine receptors, which regulate calcium release

Nursing Considerations

  • Monitor liver function regularly
  • Monitor creatine kinase (CK) levels regularly
  • Creatine kinase is an enzyme in skeletal muscle, heart muscle, and brain
  • When muscle is damaged, CK leaks into the bloodstream
  • Elevated CK levels may suggest muscle injury or disease
  • Avoid grapefruit, as it can reduce the statin, increasing the risk of side effects

Cholesterol-Lowering Medications

  • Different classes of medications have varying common side effects and precautions.
  • Statins may cause headache, stomach upset, and muscle pain also Simvastatin should be taken in the evening and antacids should not be taken at the same time as rosuvastatin
  • Fibrates may cause stomach pain, shin rash, or abdominal pain
  • Cholesterol absorption inhibitors may cause headache, tiredness, abdominal pain, and flatulence
  • Bile acid sequestrants often lead to constipation, gas, or bloating.
  • PCSK9 inhibitors may cause injection site reactions (redness, pain, bruising), flu-like symptoms, and muscle pain
  • RNA-based therapy may cause injection site reactions, bronchitis, and joint pain

Coagulation Disorders

  • Many common diseases affect hemostasis
  • Characterized by Hyper-coagulability or thrombophilia, where blood clots form more easily
  • Thromboembolic disorders include venous or arterial thrombosis and myocardial infarction
  • Hypo-coagulable conditions, also known as bleeding disorders, involve abnormal hemostasis and elevated bleeding risk.
  • Examples include thrombocytopenia and hemophilia, which are also considered bleeding disorders

Coagulation Modifiers

  • These are used to modify coagulation.
  • Anticoagulants inhibit clotting factors, including heparin, which naturally prevents clot formation, and warfarin.
  • Antiplatelets interfere with platelet action, such as aspirin and clopidogrel.
  • Thrombolytics attack and dissolve existing clots, including alteplase and streptokinase

Heparin

  • Heparin is a natural liver substance that prevents clot formation
  • It combines with antithrombin III, accelerating reactions that prevent thrombosis
  • Heparin inhibits thrombin action, blocking fibrinogen conversion to fibrin, and prevents fibrin clot formation
  • Low-molecular-weight heparins (LMWHS) achieve similar anticoagulation with a lower bleeding risk
  • Examples include Enoxaparin, Nadroparin, Dalteparin, Tinzaparin,

Warfarin

  • Warfarin is a drug that inhibits vitamin K epoxide reductase, impairing vitamin K-dependent clotting factors
  • It prevents/treats thromboembolism and arterial embolism, especially in patients with atrial fibrillation or prosthetic heart valves
  • A side effect includes bleeding

Warfarin Nursing Considerations

  • Monitor International Normalized Ratio (INR) to keep therapeutic range.

Warfarin Prevent Bleeding

  • Monitor for unusual bleeding and report bleeding
  • Bleeding refers to prolonged nosebleeds, blood in urine, dark urine, vomiting blood, and coughing up blood
  • Seek medical attention for excessive bleeding or head injuries
  • Notify healthcare providers if invasive medical/dental procedures are needed.

Warfarin Handle With Care

  • Patients should hold Warfarin 5 days prior procedures
  • Take antiplatelet drugs with food to lessen stomach irritation
  • Avoid injury and heavy sports activities
  • Avoid alcohol, as it increases bleeding risk. The daily alcohol unit limit is three for men and two for women.

Warfarin Missed Dose

  • Take missed dose on that same day
  • Skip the dose and take the following dose as scheduled
  • Do not double the dose and consult a doctor.
  • Warfarin crosses the placental barrier, hence should be avoiaded.
  • Warfarin causes fetal bleeding and abnormalities
  • Warfarain is not safe during pregnancy

Hemostatics for Promotion of Clot Formation

  • Aminocaproic Acid (Amicar) and Tranexamic Acid (Transamin) which helps to prevent and stop bleeding.
  • Vitamin K also a substance that promote clot formation and stops bleeding
  • Fresh frozen plasma (FFP) acts a an unconcentrated source of all clotting.
  • Platelet concentrate treat/prevents bleeding and dysfunction

Tranexamic Acid (Transamin)

  • It reduces plasmin and plasminogen inhibiting fiber destruction
  • It can also bind fibrin with hemostatic effect

Drugs for Anemia

  • Vitamin Supplements, such as Cyanocobalamin (Nascobal)
  • Iron Salts, such as Ferrous Sulfate.
  • Erythropoiesis occurs in the bone marrow, causing the red cells to be produced
  • The Erythropoietin Glycoprotein aids in red blood cell production
  • Epoetin alfa, also treats anemia

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