Pharmacology Chapter 1: Hypercholesterolaemia and Statins
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Questions and Answers

What is the primary function of 3-Hydroxy-methylglutaryl coenzyme A (3-HMG CoA) reductase in the regulation of cholesterol synthesis?

  • Inhibiting the synthesis of bile salts
  • Controlling the rate of cholesterol synthesis in the liver (correct)
  • Regulating the activity of enzymes involved in steroid hormone production
  • Activating the transport of cholesterol in lipoproteins

    • What is the primary mechanism by which the liver takes up LDL?

  • Active transport using ATP-dependent pumps
  • Facilitated diffusion through specific protein channels
  • Receptor-mediated endocytosis (correct)
  • Passive diffusion through the liver cell membrane

    • What is the role of cholesterol in animal membranes?

  • It provides structural integrity and fluidity to the membrane (correct)
  • It is involved in the regulation of gene expression
  • It is a key component of the electron transport chain
  • It acts as a precursor to steroid hormones

    • What is the fate of cholesterol and other lipids in excess of those needed by the liver?

    <p>They are exported as VLDL and converted to LDL</p> Signup and view all the answers

    What is the origin of the term 'cholesterol'?

    <p>It is a combination of the Greek words for 'bile' and 'alcohol'</p> Signup and view all the answers

    What is the primary mechanism by which nitrates lead to vasodilation in the treatment of angina?

    <p>Release of nitric oxide (NO) and subsequent binding to sGC</p> Signup and view all the answers

    What is the key difference between stable and unstable angina in terms of chest pain?

    <p>Stable angina occurs on exertion, while unstable angina occurs at rest</p> Signup and view all the answers

    What is the primary effect of β-blockers on the heart in the treatment of angina?

    <p>Negative inotropic effect, decreasing the force of heartbeat</p> Signup and view all the answers

    What is the primary mechanism of action of Ca2+ channel blockers in the treatment of angina?

    <p>Inhibition of Ca2+ influx into smooth muscle cells</p> Signup and view all the answers

    What is the primary effect of glyceryl trinitrate on coronary arteries in the treatment of angina?

    <p>Increase in blood flow and decrease in oxygen demand</p> Signup and view all the answers

    What is the key similarity between unstable angina and myocardial infarction (MI) in terms of pathology?

    <p>Platelet and fibrin thrombus with ruptured atheroma</p> Signup and view all the answers

    What is the primary risk factor for atherosclerosis?

    <p>High cholesterol</p> Signup and view all the answers

    Which enzyme is inhibited by statins?

    <p>HMG CoA reductase</p> Signup and view all the answers

    What is the name of the gene responsible for familial hypercholesterolemia?

    <p>LDL-R</p> Signup and view all the answers

    What is the normal range for total cholesterol?

    <p>≤ 5mMol/L</p> Signup and view all the answers

    What is the cause of angina in coronary heart disease?

    <p>Narrowing/blocking of coronary arteries</p> Signup and view all the answers

    What is the purpose of statins in the treatment of cardiovascular disease?

    <p>To reduce lipid levels</p> Signup and view all the answers

    What is the primary mechanism of action of dabigatran?

    <p>Synthetic serine protease inhibitor</p> Signup and view all the answers

    What is the primary reason for avoiding warfarin in the first few months of pregnancy?

    <p>Teratogenic effects</p> Signup and view all the answers

    What is the primary benefit of using bivalirudin in percutaneous coronary artery surgery?

    <p>Combined use with aspirin and clopidogrel</p> Signup and view all the answers

    What is the primary mechanism by which liver disease affects warfarin therapy?

    <p>Impaired synthesis of clotting factors</p> Signup and view all the answers

    What is the primary reason for monitoring prothrombin time (PT) in patients taking warfarin?

    <p>To adjust the dose of warfarin</p> Signup and view all the answers

    What is the primary effect of high metabolic rate on warfarin therapy?

    <p>Increased degradation of clotting factors</p> Signup and view all the answers

    What is the mechanism of action of aspirin in the context of antiplatelet therapy?

    <p>Irreversible inhibition of COX-1</p> Signup and view all the answers

    Which of the following antibiotics can decrease vitamin K availability?

    <p>Broad spectrum antibiotics and sulphonamides</p> Signup and view all the answers

    What is the effect of dipyridamole on platelet aggregation?

    <p>Inhibition of TXA2 synthesis</p> Signup and view all the answers

    Which of the following drugs can bind to warfarin in the gut and reduce its absorption?

    <p>Colestyramine</p> Signup and view all the answers

    What is the indication for using abciximab?

    <p>High risk patients undergoing coronary angioplasty</p> Signup and view all the answers

    Which of the following drugs can be used as a single agent in patients intolerant to aspirin?

    <p>Clopidogrel</p> Signup and view all the answers

    Cholesterol is synthesised from Acetyl-CoA in the mitochondria.

    <p>False</p> Signup and view all the answers

    LDL is formed from VLDL in the liver.

    <p>False</p> Signup and view all the answers

    HDL is responsible for transporting cholesterol from the liver to peripheral tissues.

    <p>False</p> Signup and view all the answers

    Chylomicrons are involved in transporting dietary fats from the intestine to the liver.

    <p>True</p> Signup and view all the answers

    Bile salts are synthesised from cholesterol in the liver.

    <p>True</p> Signup and view all the answers

    Inhibition of myosin light chain kinase leads to decreased vasodilatation

    <p>False</p> Signup and view all the answers

    Atherosclerosis is a sudden symptomatic manifestation.

    <p>False</p> Signup and view all the answers

    Platelet-activating factor is involved in the coagulation cascade

    <p>True</p> Signup and view all the answers

    Genetic risk factors include HMG CoA reductase polymorphism and LDL-R gene polymorphism.

    <p>True</p> Signup and view all the answers

    Nifedipine is a β-blocker

    <p>False</p> Signup and view all the answers

    Unstable angina is characterized by chest pain on exertion

    <p>False</p> Signup and view all the answers

    Statins are used to increase LDL receptors.

    <p>False</p> Signup and view all the answers

    A healthy total cholesterol level is ≤ 6 mmol/L.

    <p>False</p> Signup and view all the answers

    Atenolol is a Ca2+ channel blocker

    <p>False</p> Signup and view all the answers

    Angina is a symptom of atherosclerosis.

    <p>True</p> Signup and view all the answers

    Glyceryl trinitrate increases the work done by the heart

    <p>False</p> Signup and view all the answers

    Vasodilatation and pain are caused by the release of K+ and H+ ions.

    <p>False</p> Signup and view all the answers

    Warfarin is a direct inhibitor of Factor Xa

    <p>False</p> Signup and view all the answers

    Bivalirudin is an oral anticoagulant used in patients with type 2 HIT

    <p>False</p> Signup and view all the answers

    Lepirudin is used in patients with type 2 diabetes

    <p>False</p> Signup and view all the answers

    Dabigatran is a vitamin K antagonist

    <p>False</p> Signup and view all the answers

    Rivaroxaban is used in conjunction with aspirin and clopidogrel in percutaneous coronary artery surgery

    <p>False</p> Signup and view all the answers

    Thrombin is essential for the production of protein C and S.

    <p>False</p> Signup and view all the answers

    Warfarin can be used safely in the first few months of pregnancy

    <p>False</p> Signup and view all the answers

    Hirudins are indirect thrombin inhibitors, relying on ATIII activation.

    <p>False</p> Signup and view all the answers

    Fondaparinux is an example of a low-molecular-weight heparin (LMWH).

    <p>True</p> Signup and view all the answers

    Heparin is a single substance, not a family of glycosaminoglycans.

    <p>False</p> Signup and view all the answers

    Gut flora can synthesise vitamin K in humans.

    <p>True</p> Signup and view all the answers

    Enoxaparin is a type of novel anticoagulant.

    <p>False</p> Signup and view all the answers

    Study Notes

    Hypercholesterolaemia

    • Cholesterol is a steroid component of animal membranes and a precursor of steroid hormones, sex hormones, Vit D, and bile salt.
    • Cholesterol is synthesised from Acetyl-CoA in the ER, and its synthesis is regulated in the liver by changes in 3-Hydroxy-methylglutaryl coenzyme A (3-HMG CoA) reductase.
    • Cholesterol is transported in complex with proteins (lipoproteins) – HDL, IDL, LDL, VLDL, and chylomicrons.
    • The liver takes up LDL by receptor-mediated endocytosis.

    Angina/Coronary Artery Disease

    • Angina is a symptom of coronary heart disease, characterized by chest pain due to increased oxygen demand.
    • Stable angina is predictable, whereas unstable angina occurs with less and less exertion or at rest.
    • Unstable angina is caused by a platelet and fibrin thrombus with ruptured atheroma, but not complete occlusion.

    Treatment for Angina

    • Nitrates relax smooth muscle, releasing nitric oxide (NO), which binds to soluble guanylyl cyclase (sGC) and produces cGMP, activating protein kinase G (PKG).
    • PKG inhibits myosin light chain kinase (MLCK), leading to vasodilation.
    • Β-blockers have a negative inotropic effect, decreasing the force of the heartbeat and heart rate.
    • Ca2+ channel blockers inhibit Ca2+ influx, leading to vasodilation.

    Thrombosis

    • Thrombosis is a complex process involving the coagulation cascade and platelet activation.
    • Platelet-activating factor (PAF) and thromboxane A2 (TXA2) are key players in thrombosis.

    Statins

    • Statins are lipid-lowering drugs that inhibit HMG CoA reductase in the liver and intestine.
    • Statins increase the expression of LDL receptors, leading to increased clearance of LDL from the bloodstream.
    • Healthy lipid levels are: total cholesterol ≤ 5mMol/L, non-HDL ≤ 4mMol/L, LDL ≤ 3mMol/L, TC/HDL ratio ≤ 6.

    Antiplatelet Drugs

    • Aspirin inhibits platelet thromboxane synthesis, irreversibly inhibiting COX-1.
    • Aspirin is efficacious in thrombotic stroke evolution and acute myocardial infarction.
    • Dipyridamole inhibits platelet aggregation, and its effects are additive to aspirin's.
    • ADP receptor (purine P2YX1/12) antagonists, such as clopidogrel, prasugrel, and ticagrelor, can be used in combination with aspirin or as a single agent in patients intolerant to aspirin.
    • Glycoprotein IIB/IIIA receptor antagonists, such as abciximab, tirofiban, and eptifibatide, inhibit all platelet activation pathways.

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    Description

    Test your knowledge of hypercholesterolaemia, cholesterol, and statins in pharmacology. This quiz covers key facts about cholesterol, its synthesis, and its role in the body.

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