Anticoagulants: Warfarin, Heparin, Enoxaparin
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Questions and Answers

What mechanism does warfarin use to exert its anticoagulant effect?

  • Direct activation of thrombin
  • Binding to antithrombin III
  • Inhibition of vitamin K epoxide reductase (VKOR1) (correct)
  • Inhibition of factor 10 alone

Which of the following agents is used as a reversal agent for heparin?

  • Idarucizumab
  • Aspirin
  • Andexanet alfa
  • Protamine sulfate (correct)

What is the primary action of enoxaparin?

  • Binding to vitamin K
  • Inactivation of factor 10 (correct)
  • Directly inhibiting thrombin
  • Inhibition of factor 2

Which anticoagulant can cause skin necrosis?

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

Which of the following statements about rivaroxaban is incorrect?

<p>It can be reversed with protamine sulfate. (A)</p> Signup and view all the answers

What is the primary role of cilostazol?

<p>Intermittent claudication treatment (C)</p> Signup and view all the answers

What distinguishes dabigatran from other anticoagulants?

<p>It is a direct thrombin inhibitor and a prodrug. (A)</p> Signup and view all the answers

Which antiplatelet drug irreversibly binds to the P2Y12 ADP receptor?

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

What is the primary adverse effect associated with thrombolytics like alteplase?

<p>Severe bleeding complications (A)</p> Signup and view all the answers

What is the main action of statins?

<p>Inhibiting de novo cholesterol synthesis (A)</p> Signup and view all the answers

Which of the following uses increase LDL clearance primarily via the LDL receptor?

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

What is the primary effect of niacin in lipid management?

<p>Reduce LDL and increase HDL (B)</p> Signup and view all the answers

Which combination of medications is indicated for elevated triglycerides?

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

Which class of drugs primarily prevents the conversion of angiotensinogen to angiotensin I?

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

Which beta-blocker is non-selective and affects both beta1 and beta2 receptors?

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

Which class of medications is most effective for lowering serum triglycerides and increasing HDL levels?

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

What adverse effect is commonly associated with ACE inhibitors?

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

Which medication is a selective blocker of beta1 receptors and often prescribed for hypertension?

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

What mechanism do bile acid sequestrants primarily use to lower LDL cholesterol?

<p>Bile acids excretion leading to increased cholesterol conversion (B)</p> Signup and view all the answers

Which drug class decreases blood pressure by limiting intracellular calcium levels?

<p>Calcium channel blockers (B)</p> Signup and view all the answers

Flashcards

Statin Pharmacokinetics

Statins' absorption after oral intake varies.

Statin Cholesterol Reduction

Statins lower LDL by reducing liver's VLDL production and increasing LDL receptor clearance.

Niacin's Effect on Lipids

Niacin reduces VLDL and LDL, and significantly raises HDL by inhibiting fat release.

Bile Acid Sequestrants

Resins bind bile acids, forcing the liver to use cholesterol to make more bile.

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Ezetimibe's Action

Ezetimibe blocks cholesterol in the gut, lowering LDL.

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Statins and Resins Combination

Combining statins and resins can effectively lower LDL cholesterol.

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Diuretics' Blood Pressure Effect

Diuretics decrease blood volume and thus blood pressure.

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Beta-Blockers' Mechanism

Beta-blockers lower blood pressure by blocking adrenaline receptors and reducing heart rate.

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ACE Inhibitors' Action

ACE inhibitors block the conversion of angiotensin I to angiotensin II.

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Calcium Channel Blockers' Function

Calcium channel blockers limit calcium entry into heart and blood vessels, lowering blood pressure.

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Warfarin's Mechanism

Warfarin is a vitamin K antagonist that inhibits factors 2, 7, 9, and 10, reducing clotting factors.

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Heparin's Action

Heparin binds to antithrombin III to inactivate factors 2 and 10, preventing blood clotting.

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Enoxaparin's Function

Enoxaparin (LMWH) binds to antithrombin III and inactivates factor 10, preventing blood clots.

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Protamine Sulfate's Role

Protamine sulfate is an antidote that reverses the effects of heparin and enoxaparin. It's highly basic and a stable salt.

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Fonaparinux's Action

Fonaparinux inhibits factor 10 via antithrombin III, preventing blood clots.

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Direct Factor Xa Inhibitors

Rivaroxaban and apixaban directly inhibit factor 10 preventing blood clots orally.

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Aspirin's Mechanism

Aspirin inhibits COX reducing thromboxane A2 (TXA2) production, an important role in blood clotting.

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Clopidogrel's Action

Clopidogrel is an irreversible inhibitor of platelet activation via P2Y12 receptor.

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Alteplase Function

Alteplase is a thrombolytic drug that breaks up blood clots used for acute ischemic stroke.

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Statins' Action

Statins inhibit HMG-CoA reductase, reducing cholesterol production and stabilizing plaques.

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Study Notes

Warfarin

  • Vitamin K antagonist
  • Inhibits factors 2, 7, 9, and 10
  • Inhibits VKOR1
  • Reduces clotting factors due to lack of gamma-carboxylglutamyl side chains
  • Used for prosthetic heart valves
  • Requires bridging drugs (heparin or enoxaparin) initially due to hypercoagulability
  • Reversal: Vitamin K + 4F-PCC or FFP (non-life threatening)
  • Contraindicated in pregnancy
  • INR target range 2-3
  • Oral administration

Heparin

  • Highly acidic
  • Binds to antithrombin III via pentasaccharide complex
  • Inactivates factors 2 and 10
  • Subcutaneous or IV administration (prophylaxis)
  • Adverse effects: bleeding, Heparin-induced thrombocytopenia (HIT)

Enoxaparin

  • Low-molecular-weight heparin (LMWH)
  • Binds to antithrombin III via pentasaccharide complex
  • Inactivates factor 10
  • Subcutaneous injections
  • Adverse effects: bleeding, HIT (greater risk than heparin)
  • Protamine sulfate is used for reversal (partially effective for enoxaparin)

Fondaparinux

  • Pentasaccharide
  • Inhibits factor 10 via antithrombin III
  • Injectable
  • Contraindicated in renal disease
  • No reversal agent

Rivaroxaban and Apixaban

  • Direct factor 10 inhibitors
  • Oral tablets
  • Contraindicated in renal disease
  • Reversal agents exist (andexant alfa for rivaroxaban)

Dabigatran

  • Direct thrombin inhibitor
  • Oral prodrug
  • Contraindicated in renal disease
  • Reversal agent (idarucizumab)

Other Drugs

  • Bivalirudin and argatroban: direct thrombin inhibitors
  • Alteplase: thrombolytic (for acute ischemic stroke)
  • Aspirin: COX inhibitor (acetylation of a serine residue on COX, reduces TxA2, GI bleeding and ulcer risk)
  • Clopidogrel andticagrelor: P2Y12 ADP receptor inhibitors
  • Abciximab and eptifibatide: GPIIb/IIIa inhibitors
  • Cilostazol: PDE3 inhibitor (inhibition of PDE3 resulting in decreased catabolism of cAMP)
  • Statins: HMG-CoA reductase inhibitors

Cholesterol-Lowering Drugs

  • Competitive inhibitors (inhibiting de novo synthesis, deplete intracellular supply of cholesterol, plaque stabilization, improvement of coronary endothelial function)
  • Statins: reduce LDL cholesterol principally by increasing LDL clearance via the LDL receptor
  • Nicotinic acid (niacin): strongly inhibits lipolysis, reduce VLDL and LDL, increase HDL
  • Fibric acid derivatives (fibrates): increase HDL levels, reduce triglycerides
  • Bile acid sequestrants: bind bile acids and bile salts in the small intestine, increase LDL receptors
  • Ezetimibe: selectively inhibits cholesterol absorption in the small intestine

Other Information

  • Adverse effects are mentioned for many of the drugs, including bleeding and other complications.
  • Contraindications are discussed for certain conditions (e.g., renal disease)
  • Reversal agents/alternatives are mentioned where applicable.

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Description

Test your knowledge on anticoagulants including Warfarin, Heparin, and Enoxaparin. This quiz covers their mechanisms, uses, contraindications, and reversal strategies. Perfect for students in pharmacology or medicine.

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