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 (B)</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' (C)</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 (C)</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 (A)</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 (C)</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 (D)</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 (A)</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 (A)</p> Signup and view all the answers

What is the primary risk factor for atherosclerosis?

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

Which enzyme is inhibited by statins?

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

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

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

What is the normal range for total cholesterol?

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

What is the cause of angina in coronary heart disease?

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

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

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

What is the primary mechanism of action of dabigatran?

<p>Synthetic serine protease inhibitor (C)</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 (B)</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 (D)</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 (C)</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 (C)</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 (C)</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 (B)</p> Signup and view all the answers

Which of the following antibiotics can decrease vitamin K availability?

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

What is the effect of dipyridamole on platelet aggregation?

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

What is the indication for using abciximab?

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

Cholesterol is synthesised from Acetyl-CoA in the mitochondria.

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

LDL is formed from VLDL in the liver.

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

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

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

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

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

Bile salts are synthesised from cholesterol in the liver.

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

Inhibition of myosin light chain kinase leads to decreased vasodilatation

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

Atherosclerosis is a sudden symptomatic manifestation.

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

Platelet-activating factor is involved in the coagulation cascade

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

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

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

Nifedipine is a β-blocker

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

Unstable angina is characterized by chest pain on exertion

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

Statins are used to increase LDL receptors.

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

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

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

Atenolol is a Ca2+ channel blocker

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

Angina is a symptom of atherosclerosis.

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

Glyceryl trinitrate increases the work done by the heart

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

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

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

Warfarin is a direct inhibitor of Factor Xa

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

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

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

Lepirudin is used in patients with type 2 diabetes

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

Dabigatran is a vitamin K antagonist

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

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

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

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

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

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

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

Hirudins are indirect thrombin inhibitors, relying on ATIII activation.

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

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

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

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

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

Gut flora can synthesise vitamin K in humans.

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

Enoxaparin is a type of novel anticoagulant.

<p>False (B)</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.
  • Î’-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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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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