Cardiovascular Pharmacology PHAR-20030

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Questions and Answers

What was the main class of drugs developed in the 1960s for hypertension treatment?

PCSK9 inhibitors

β-blockers (correct)

ACE inhibitors

Statins

What significant discovery related to LDL metabolism occurred in 2003?

Discovery of the LDL metabolic pathway

Development of statins

Discovery of the PCSK9 gene (correct)

Development of PCSK9 inhibitors

Which of the following describes a key development in the 1980s related to cardiovascular disease?

Discovery of β adrenergic receptors

Development of statins (correct)

Introduction of β-blockers

Development of ACE inhibitors

What is the action of PCSK9 inhibitors in relation to LDL cholesterol?

Reduce LDL concentrations Signup and view all the answers

Which system is primarily targeted by β-blockers in cardiovascular treatment?

Sympathetic Nervous System (SNS) Signup and view all the answers

What is the primary function of the tunica media in arteries?

To regulate blood flow and pressure Signup and view all the answers

Which of the following statements is accurate regarding veins compared to arteries?

Veins contain valves for unidirectional blood flow Signup and view all the answers

What role do erythrocytes play in the cardiovascular system?

Transporting oxygen to lungs Signup and view all the answers

Which term best encompasses all diseases affecting the heart and blood vessels?

Cardiovascular Disease (CVD) Signup and view all the answers

What component of blood is primarily responsible for the defense against infections?

Leukocytes Signup and view all the answers

What is the primary function of the Renin-Angiotensin-Aldosterone-System (RAS) in the cardiovascular system?

To regulate blood volume and systemic vascular resistance Signup and view all the answers

Which of the following correctly describes the role of adrenergic receptors in the cardiovascular system?

They are involved in the fight-or-flight response affecting heart rate and blood pressure Signup and view all the answers

What class of medications do calcium blockers belong to in the context of hemodynamics?

Vasodilators Signup and view all the answers

Which neurotransmitter is primarily involved in the adrenergic nervous system's action on the cardiovascular system?

Norepinephrine Signup and view all the answers

What is the effect of Nitric Oxide (NO) in the cardiovascular system?

It serves as a vasodilator, improving blood flow Signup and view all the answers

Study Notes

Cardiovascular Pharmacology Teaching Block

The course is PHAR-20030 Pharmacology
The instructor is Ass. Prof. Monica de Gaetano, PhD
The course focuses on cardiovascular pharmacology

Background

Instructor's educational background includes a classical high school education (Latin & Greek), BSc in Pharmaceutical Chemistry, MSc in Environmental Toxicology, PhD in Biomolecular & Biomedical Science, and Postdoctoral work in Medicinal Chemistry
The instructor also has experience at various levels in Cell Biology & Genetics and Pharmacology.

Research Focus

Research focuses on the Resolution of Inflammation
Research also investigates Macrovascular Diabetes Complications
The professor's research includes Drug Discovery.

Teaching Topics

The course content includes Cardiovascular Pharmacology, Advanced Immunology (PHAR20030, PHAR20040), CV & Renal Pharmacology (PHAR30020, PHAR30110), PHAR40030, and BMOL40410.

Schedule

The schedule includes lectures on pharmacological principles (I-IV), autonomic nervous system (I-III), respiratory, cardiovascular (I-IV), renal, chemotherapeutics (I-IV), neuropharmacology (I-IV), endocrine (I-II), reproductive (I-II), reviews, and principles of pharmacology.

CV Pharmacology Syllabus

The syllabus covers Regulation of Cardiovascular function
Anti-hypertensive medications
Angina and Dyslipidemia treatments
Anti-platelet and Anti-coagulants
Renal System and Diuretics
Mid-term and End-term review sessions

CVD Pharmacology Milestones

Discovery of ß-adrenergic & ACE receptors as blood pressure checkpoints (1950s)
Development of anti-hypertensives (beta-blockers like propranolol - 1960s, ACE inhibitors like Captopril - 1970s)
Discovery of the LDL metabolic pathway (1970s)
Development of statins to tackle LDL metabolic pathway (1980s)
Discovery of PCSK9 gene as a mediator of LDL metabolism (2003)
Development of PCSK9 inhibitors to reduce LDL and MI/stroke rate (2017)

Cardiovascular Disease (CVD)

CVD is a global pandemic, not limited to Western countries
CVD is a major cause of death worldwide

CV Teaching Block Overview

Diseases covered include Hypertension, Atherosclerosis, and Heart disease (Angina)
Systems targeted by drugs include the sympathetic nervous system (SNS), renin-angiotensin-aldosterone system (RAAS), coagulation system (hemostasis), renal system, and hemodynamics of the heart
Students are recommended to follow a NAC (Nature, Action, Consequence) approach for studies for better knowledge retention.

How to perform well at the exam?

Focus on the nature of the drug (e.g., receptor agonist/antagonist, enzyme inhibitor/stimulator).
Understand the action of the drug (e.g., which receptor/enzyme/channel does it target?).
Identify the consequences of drug action (e.g., the drug's effect and potential side effects).

Cardiovascular System Lecture 1 (Structure, Function, Regulation)

The circulatory/cardiovascular (CV) system delivers oxygen and nutrients to the entire body through a complex network of vessels.
Key features include arteries, arterioles, capillaries, veins, and venules

Today's Learning Outcome

Understand cardiovascular anatomy, physiology, and pathophysiology
Define the role of the adrenergic nervous system (ANS) and its receptors in the CV system.
Identify examples of where adrenergic agonists and antagonists are utilized.
Understand the hemodynamics governing cardiac function.
Define the renin-angiotensin-aldosterone system (RAS) and its role in cardiovascular disease (CVD).
Understand the role of nitric oxide (NO) and other vital mediators within the CV system.

Lecture 1 Structure

Course sections include cardiovascular system definition, components, and functions; adrenergic system neurotransmitters, receptor distribution/function, agonists/antagonists and hemodynamics, renin-angiotensin system (RAS), RAS antagonists, and vasodilators (calcium blockers, and nitric oxide).

Cardiovascular System

The cardiovascular (CV) system is responsible for maintaining homeostasis, providing oxygen and nutrients to cells, and removing cellular waste.

Cardiovascular System Anatomy and Physiology

Components of the CV system include the heart, blood vessels (arteries, veins, capillaries), and blood.
The heart's functions include pumping blood and coordinating electrical impulses for contraction.
Blood vessels maintain blood flow and regulate blood pressure.
Blood cells (red blood cells, leukocytes, and platelets) perform various functions within the circulatory system.

Cardiovascular System Structure of Components

Arteries have a thick tunica media with smooth muscle to regulate blood flow and pressure.
Veins have thinner walls, less smooth muscle, and valves to facilitate unidirectional blood flow toward the heart.
Blood cells include erythrocytes (oxygen transport), leukocytes (defense cells), and platelets (blood clotting).

Cardiovascular Pathology: CVD

CVD encompasses various diseases affecting the heart and blood vessels (coronary artery disease (CAD), peripheral artery disease (PAD)).
Heart diseases (angina, heart failure, myocardial infarction).

Adrenergic Nervous System (ANS)

The ANS (or sympathetic nervous system) controls several functions, including exocrine excretion, metabolic processes, smooth muscle activity (contraction or relaxation), and heart rate/force.
Main neurotransmitters include adrenaline (epinephrine), noradrenaline (norepinephrine), and acetylcholine.

Adrenergic Receptors

Adrenergic receptors (α- and β- subtypes) mediate a variety of effects on blood vessels, heart muscle, and other tissues depending on the type of receptor.

Effects on Heart and Blood Vessels

Adrenaline and noradrenaline impact various tissues/effects, including smooth muscles, blood vessels, and the heart, leading to either constriction or dilation depending on the receptor type.

Adrenergic Agonists and the Heart

Adrenaline (epinephrine) activates all adrenergic receptor subtypes and affects cardiac muscle, vascular smooth muscle, and other muscles.

Use of Adrenaline in Anaphylaxis

Anaphylaxis causes peripheral vasodilation, smooth muscle contraction, and bronchoconstriction.
Adrenaline (epinephrine) is used to counteract the symptoms and causes increased peripheral resistance, improved blood pressure, and reduction in angioedema.

ANS and CV System - Main Effects

The autonomic nervous system (ANS) affects the heart via β1-receptors which increase heart rate, force of contraction, and cardiac efficiency.
Physiological effects can be positive, while pathological effects can include hypertension, cardiac failure, and myocardial infarction.

Adreno-blockers

Adreno-blockers (β-blockers, and other antagonists) are used to reduce cardiac work, lower blood pressure, and limit sympathetic nervous system (SNS) activity following myocardial infarction.

β-adrenergic Receptor Antagonists (β-blockers)

Cardioselective (β1) and Non-selective (β1 and β2) receptor antagonists are used to treat angina, high blood pressure, and post-MI conditions.
Understanding the side effects (e.g., nightmares, depression, insomnia, and bronchospasm)

Haemodynamics and the Heart

Arterial blood pressure results from cardiac output (CO) and peripheral vascular resistance (PVR).
Venous return (preload) determines ventricular volume.
Peripheral resistance (afterload) determines the resistance overcome to pump blood.

Renin-Angiotensin-System (RAS)

The renin-angiotensin-aldosterone system (RAAS) regulates blood pressure by influencing either vasoconstriction or peripheral vascular resistance.

Renin-Angiotensin-Aldosterone-System Inhibitors

Angiotensin-converting enzyme (ACE) inhibitors (ACEIs), angiotensin II receptor antagonists (ARBs), and aldosterone antagonists (K+ sparing diuretics), and renin inhibitors target the RAAS in preventing/treating hypertension and cardiac failure due to excessive RAAS activity.

Vascular Tone Regulation

Maintaining appropriate vascular tone regulates blood vessel diameter, affecting blood flow, and related issues like oxygen delivery and waste removal.
Vasodilation increases blood vessel diameter, increasing oxygen and nutrient transfer (reducing cellular waste transport).

Vasodilators (i): Calcium Channel Blockers

Calcium channel blockers impact vascular tone by influencing calcium ion influx in controlling vascular smooth muscle contraction, thereby decreasing vasoconstriction.
This is used to treat hypertension and angina.

Vasodilators: Nitric Oxide (NO)

Nitric oxide (NO) is produced by endothelial cells and relaxes vascular smooth muscle.
Nitrates are pro-drugs to increase NO production and cause vasodilation.

Summary & Conclusion

The cardiovascular system (heart, blood vessels, and blood) works in conjunction with the autonomic nervous system (ANS) to maintain homeostasis and supply oxygen and nutrients.
Drugs targeting adrenergic receptors (e.g., β-blockers), renin-angiotensin-aldosterone system (RAAS) components (e.g., ACE inhibitors, ARBs), and vasodilators (e.g., calcium channel blockers, nitrates) are utilized to treat CVDs associated with those systems.

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Description

This quiz covers key concepts in cardiovascular pharmacology as part of the PHAR-20030 course led by Ass. Prof. Monica de Gaetano. Students will be tested on their understanding of drug discovery, inflammation resolution, and related pharmacological topics vital for advancing medical science. Prepare to delve into cardiovascular drugs and their impacts on health.