Pharmacology of β2 Adrenergic Agonists

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Questions and Answers

What is the primary outcome of bronchodilation achieved by β2 adrenergic receptor agonists?

  • Decrease in Forced Expiratory Volume (FEV1)
  • Relaxation of respiratory smooth muscle (SM) (correct)
  • Decrease in Peak Expiratory Flow (PEF)
  • Increase in membrane hyperpolarization

Which is a common adverse effect associated with β2 adrenergic receptor agonists?

  • Acute myocardial infarction (MI)
  • Hyperglycemia
  • Tachyarrhythmias
  • Nervousness (correct)

What serious cardiovascular condition can result from the use of β2 adrenergic receptor agonists?

  • Dehydration
  • Atrial fibrillation (A.Fib) (correct)
  • Acute bronchospasm
  • Respiratory failure

Which of the following describes an important contraindication for the use of LABA inhalation powders?

<p>To use without other long-term asthma control medications (A)</p> Signup and view all the answers

What common precaution should be discussed with patients regarding the use of β2 adrenergic receptor agonists?

<p>Paradoxical bronchospasm may occur (A)</p> Signup and view all the answers

What is one of the primary warnings associated with terbutaline sulfate use?

<p>Serious adverse reactions including death have been reported (D)</p> Signup and view all the answers

How does the potency of t-butyl compare to metaproterenol?

<p>t-butyl has 3-fold greater potency than metaproterenol (D)</p> Signup and view all the answers

What is the duration of action (DOA) for metaproterenol?

<p>2-6 hours (D)</p> Signup and view all the answers

Which statement about salmeterol is true?

<p>It is a long-acting β2-selective agonist indicated for asthma and COPD. (D)</p> Signup and view all the answers

What is the half-life of terbutaline sulfate when taken orally?

<p>3 hours (C)</p> Signup and view all the answers

Which short-acting beta-adrenergic receptor agonist is commonly used as a bronchodilator?

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

What is a common characteristic of long-acting muscarinic antagonists (LAMA)?

<p>They are used for chronic management of COPD. (C)</p> Signup and view all the answers

Which of the following agents is indicated as a combination treatment for asthma?

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

Which systemic corticosteroid is commonly used for severe asthma exacerbations?

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

Which β-blocker is considered safer for patients with asthma or COPD?

<p>Atenolol (B), Metoprolol (D)</p> Signup and view all the answers

What role do leukotriene antagonists play in asthma management?

<p>They reduce inflammation. (C)</p> Signup and view all the answers

Which medication is classified as a methylxanthine used in asthma management?

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

Which of the following is a long-acting beta-adrenergic receptor agonist (LABA) used in asthma treatment?

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

Which of the following medications is an IgE antibody?

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

Which medication is a long-acting beta-agonist (LABA) indicated for asthma and COPD?

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

Which of the following medications should be avoided in patients with bronchospasm conditions like asthma?

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

Which combination agent contains both a long-acting beta-agonist and an inhaled corticosteroid?

<p>Trelegy Ellipta (A), Breo Ellipta (C)</p> Signup and view all the answers

Which medication is a SAMA used for its bronchodilator effects?

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

Which agent is known for its long duration of action and is typically dosed twice daily?

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

Which of the following agents is a non-catecholamine?

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

What is a unique aspect of the medication Dupixent (dupilumab)?

<p>It is an interleukin antagonist (A)</p> Signup and view all the answers

What distinguishes Vilanterol in terms of dosing frequency?

<p>Given once daily (A)</p> Signup and view all the answers

Which of the following medications is not a combination of LABA and ICS?

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

What is the immediate response in asthma pathogenesis characterized by?

<p>Release of histamine and bronchoconstriction (C)</p> Signup and view all the answers

Which of the following is a consequence of untreated asthma?

<p>Narrowed and hyper-responsive airways (D)</p> Signup and view all the answers

What happens during the late phase reaction in asthma?

<p>Eosinophils infiltrate the airway (B)</p> Signup and view all the answers

Which pharmacological management option is classified as a maintenance treatment?

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

What does GINA recommend regarding the treatment of asthma for adults and adolescents?

<p>Low dose ICS-containing controller treatment (D)</p> Signup and view all the answers

Which mediator is NOT involved in the immediate phase response of asthma?

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

What structural change is associated with the remodeling of lung tissue in asthma?

<p>Sub-epithelial fibrosis (B)</p> Signup and view all the answers

What type of treatment is an inhaled short-acting β2-adrenergic agonist primarily used for?

<p>Rescue or reversal (D)</p> Signup and view all the answers

Which of the following is a common symptom of asthma due to airway inflammation?

<p>Shortness of breath (D)</p> Signup and view all the answers

What is bronchial hyper-responsiveness indicative of in asthma patients?

<p>Overreaction to environmental triggers (D)</p> Signup and view all the answers

What is the key approach to take when noticing a decline in performance despite using previous study methods?

<p>Reassess your study approach and identify the root cause. (C)</p> Signup and view all the answers

Why is time management emphasized in the context of studying for iMCP3?

<p>Improper time allocation can negatively impact overall academic performance. (A)</p> Signup and view all the answers

How should study guides be treated throughout the pharmacy curriculum?

<p>Keep and enhance them to build on previous knowledge. (B)</p> Signup and view all the answers

What is a crucial reason for avoiding complacency in a pharmacy program?

<p>Each course introduces new challenges requiring adaptability. (B)</p> Signup and view all the answers

Which of the following strategies is discouraged when facing difficulties in coursework?

<p>Procrastinating until deadlines are near. (D)</p> Signup and view all the answers

What can enhance the learning process in pharmacotherapy courses?

<p>Brushing up on notes from previous courses for context. (B)</p> Signup and view all the answers

What should a student do if they realize their study techniques are no longer effective?

<p>Meet with faculty to address the issue and seek advice. (B)</p> Signup and view all the answers

In terms of continuous improvement, what should a pharmacy student prioritize?

<p>Identifying and adjusting study approaches based on performance. (C)</p> Signup and view all the answers

Flashcards

Which Beta Blockers are suitable for patients with asthma/COPD/emphysema?

Beta blockers that selectively block beta-1 receptors, typically used for heart conditions, are suitable for patients with asthma/COPD/emphysema because they don't significantly affect the beta-2 receptors in the lungs, minimizing bronchospasm risks.

What is Asthma?

A long-term condition characterized by inflamed and narrowed airways, leading to symptoms like wheezing, shortness of breath, and chest tightness.

What are Bronchodilators?

These medications help to open up the narrowed airways in patients with asthma and COPD, making breathing easier.

What are β2-adrenergic receptor agonists?

These medications work by directly stimulating beta-2 receptors in the lungs, causing relaxation and widening of the airways. They can be short-acting for quick relief or long-acting for ongoing control over asthma symptoms.

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What are Muscarinic Antagonists?

These medications block the action of acetylcholine, a neurotransmitter that causes airway narrowing. This results in airway relaxation and easier breathing. They can be short-acting for immediate relief or long-acting for sustained control.

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What are Anti-inflammatory agents?

These medications work by reducing inflammation in the airways, thereby reducing symptoms like wheezing and breathlessness in patients with asthma and COPD.

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What are Inhaled Corticosteroids (ICS)?

These corticosteroids are inhaled directly into the lungs, providing targeted relief and reducing systemic side effects. They help to control inflammation in the airways, reducing asthma symptoms.

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What are Leukotriene antagonists?

These medications block the action of leukotrienes, a type of chemical that causes inflammation and airway narrowing in asthma. They can be helpful in reducing symptoms like wheezing, cough, and shortness of breath.

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Long-Acting Beta-2 Agonists (LABAs)

A type of medication used to treat asthma by relaxing the muscles in the airways, making it easier to breathe.

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Tachyphylaxis

A reduction in the effectiveness of a medication over time, requiring higher doses to achieve the same effect.

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Paradoxical Bronchospasm

A serious side effect of LABAs, where the airways become narrower and breathing worsens instead of improving.

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LABA Monotherapy

The use of LABAs alone, without a long-acting asthma control medication like inhaled corticosteroids, can increase the risk of asthma-related deaths.

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Inhaled Corticosteroids

A type of asthma control medication that reduces inflammation in the airways.

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IgE Antibody Therapy: Omalizumab (Xolair)

Omalizumab (Xolair) targets and inhibits the action of IgE antibodies, reducing the severity of allergic reactions. It's used for moderate to severe asthma that is not adequately controlled with other therapies.

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Interleukin Antagonists: Reslizumab (Cinqair), Mepolizumab (Nucala), Benralizumab (Fasenra), Dupixent (Dupilumab)

Reslizumab (Cinqair), Mepolizumab (Nucala), and Benralizumab (Fasenra) are monoclonal antibodies that target and inhibit the action of interleukin-5, a key cytokine involved in the inflammatory cascade leading to airway inflammation in asthma. They are used to treat severe, eosinophilic asthma. Dupilumab (Dupixent) targets interleukin 4 and 13, which are involved in many types of inflammation

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Cromolyns: Cromolyn sodium, nedocromil sodium

Cromolyn sodium and nedocromil sodium are mast cell stabilizers, meaning they prevent the release of inflammatory mediators from mast cells, which can lead to airway inflammation.

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Beta-blockers (BBs)

Beta-blockers are used to manage blood pressure and heart rate. They are often used to treat high blood pressure, heart failure, and some types of heart rhythm abnormalities. They also are used to prevent migraines and some types of tremors.

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Beta-blockers (BBs) in Asthma, COPD, Emphysema

Beta-blockers can worsen bronchospasm, or narrowing of the airways, in patients with asthma, COPD, or emphysema. This is because they block the beta-2 receptors that are responsible for airway dilation. However, there are some beta-blockers that are relatively safe for patients with these conditions, and there is no contraindication with the use of beta blockers for hypertension in these patients.

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Beta-blockers (BBs) in Heart Failure with Reduced Ejection Fraction (HFrEF)

Beta-blockers are used to treat heart failure with reduced ejection fraction (HFrEF). They help to reduce the workload on the heart and improve heart function. By slowing the heart rate and reducing the force of contraction, beta-blockers help to reduce the strain on the heart and improve outcomes in patients with HFrEF. However, special considerations are needed for patients with asthma, COPD, or emphysema.

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Epinephrine

Epinephrine is a catecholamine. It stimulates both α and β-adrenergic receptors. It is the most potent β-agonist.

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Albuterol

Albuterol is a β2-selective short-acting bronchodilator. It is commonly used for the relief of acute asthma symptoms.

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Salmeterol

Salmeterol is a long-acting β2-selective bronchodilator. It is used twice daily for the prevention of asthma symptoms.

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Vilanterol

Vilanterol is a long-acting β2-selective bronchodilator. It has the longest duration of action (24 hours) among the available β2-agonists. It is used once daily for the prevention of asthma symptoms.

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Terbutaline: Metabolism

Terbutaline is a short-acting beta-2 agonist (SABA) that is resistant to breakdown by COMT and MAO enzymes. This means it stays active in the body longer.

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Terbutaline: Onset and Duration

Terbutaline has a rapid onset of action (5-30 minutes) but a relatively short duration of action (3-4 hours). This makes it suitable for treating acute asthma symptoms but not for long-term control.

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Terbutaline: Potency

Terbutaline is a powerful bronchodilator that is three times more potent than metaproterenol.

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Metaproterenol: Characteristics

Metaproterenol is a short-acting beta-2 agonist (SABA) that is resistant to breakdown by COMT enzymes. It is available as a syrup, making it easy to administer.

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Salmeterol: Applications

Salmeterol is a long-acting beta-2 agonist (LABA) commonly prescribed for asthma, COPD, exercise-induced bronchospasm, and nocturnal asthma. It is often combined with inhaled corticosteroids, such as fluticasone propionate, for optimal treatment effectiveness.

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Asthma

A condition where airways become hypersensitive to stimuli causing reversible bronchospasms, resulting in airway obstruction and inflammation.

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Early Phase Asthma Response

The initial, rapid response to asthma triggers, involving immediate release of inflammatory mediators by mast cells and basophils.

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Late Phase Asthma Response

A late-onset reaction to asthma triggers, occurring hours after the initial response, characterized by inflammation caused by eosinophils and other immune cells.

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Chronic Inflammation in Asthma

Inflammation that persists in the airways causing them to become thickened and narrowed due to tissue remodeling.

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Airway Hyper-responsiveness in Asthma

The tendency of the airways to overreact to stimuli, leading to severe bronchoconstriction in asthma.

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Bronchodilators

Drugs that open up constricted airways, providing immediate relief from asthma symptoms.

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Rescue Bronchodilators

Bronchodilator medications used to treat sudden, acute asthma symptoms, like shortness of breath.

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Maintenance Bronchodilators

Bronchodilator medications used regularly to prevent asthma symptoms or attacks.

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Anti-inflammatory Medications for Asthma

Drugs that reduce inflammation in the airways, helping to manage asthma.

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GINA 2019 Asthma Management Guideline Change

The 2019 Global Initiative for Asthma (GINA) guidelines recommend that all adults and adolescents with asthma should receive ICS-containing controller treatment, regardless of severity, to reduce the risk of serious exacerbations.

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Adaptability in Learning

The ability to adjust your study approach and learning strategies based on your progress and changing demands of the program. It involves recognizing when your current methods are ineffective, identifying the root cause, and adapting them accordingly.

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Constantly Re-evaluate Your Learning

Regularly assess your understanding and identify areas where improvement is needed. This can be done through self-reflection, review sessions, meeting with faculty, or analyzing your performance on quizzes and exams.

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Effective Time Management

The art of managing your time efficiently to balance the demands of iMCP3 with other courses and responsibilities. It involves prioritizing tasks, setting realistic goals, and avoiding procrastination.

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Proactive Problem-Solving

Don't wait until it's too late to address challenges. If you notice difficulties understanding concepts or struggling with assignments, seek help promptly. Engage with faculty, discuss your concerns, and explore solutions together.

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Preserve Your Study Guides

Keeping your study materials organized and readily accessible. This includes electronic copies of notes, tables, and summaries for easy reference. These materials can be valuable resources as the curriculum builds upon previous knowledge.

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Leverage Previous Learning

The iMCP3 curriculum is designed to build upon previous learning experiences. Use your study guides from earlier modules to refresh your understanding of fundamental concepts, reducing the burden of relearning and allowing you to focus on new material.

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Active Learning Techniques

The key to successful learning is active engagement. Utilize different techniques like flashcards, practice quizzes, and group study to learn effectively.

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Strive for Deep Understanding

Focus on consistently achieving a high level of understanding. This means going beyond just memorizing facts and aiming to grasp the underlying principles and concepts.

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Study Notes

In-Class Patient Cases Assignment

  • On-ground class: Thursday, January 16th, 8:30 AM
  • Hybrid class: Friday, January 17th, 8:30 AM
  • Cases will be released by Wednesday.
  • Students must participate for the entire duration of the session.
  • Accurate response rate of >90% for >90% of questions is required for full credit.
  • MA 2025

Pharmacology of Asthma and COPD Management (Part 1)

  • Course taught by Maha Abdalla, PharmD, PhD, RPh
  • Associate Professor of Pharmaceutical Sciences
  • Email: [email protected]
  • Office Room: 276
  • Phone: (865)288-5837
  • Office Hours: Tuesdays and Thursdays, 9:00 AM - 12:00 PM, or by appointment.
  • MA 2025

Asthma Pathogenesis

  • Definition: a hyper-responsive state of airways to stimuli, resulting in reversible bronchospasm and airway inflammation
  • Biphasic asthma response: two stages
    • Early acute phase reaction: mast cells and basophils release mediators like histamine, prostaglandins, and leukotrienes, leading to smooth muscle contraction and bronchoconstriction
    • Late phase reaction: involves infiltration of the airways by eosinophils and other cytokine-secreting leukocytes, causing chronic inflammation and structural changes in the airways.
  • Outcome: Chronic inflammation and airway remodeling including: mucus hypersecretion, remodeling of lung tissue, sub-epithelial fibrosis, epithelial shedding, airway smooth muscle hypertrophy and hyperplasia, angiogenesis
  • Triggers: allergens (mold, pollen, dust mites, pet dander), upper respiratory tract viral infections, exercise and hyperventilation, cold air or sudden temperature changes, drugs (beta-blockers, aspirin, NSAIDs) and some irritants (cigarette smoke, air pollution, chemicals)
  • Risk factors: endogenous factors (genetic predisposition, atopy, airway hyper-responsiveness, gender, ethnicity) and environmental factors (outdoor allergens, indoor allergens, occupational sensitizers, passive smoking, respiratory infections, obesity, early viral infections)

Inhaler Therapy for Asthma

  • SABAs (short-acting beta agonists): albuterol (various brand names), levalbuterol, epinephrine
  • SAMAs (short-acting muscarinic antagonists): ipratropium
  • LABAs (long-acting beta agonists): salmeterol, formoterol, vilanterol
  • LAMAS (long-acting muscarinic antagonists): tiotropium
  • Corticosteroids (inhaled and oral): fluticasone, beclomethasone, budesonide
  • Leukotriene antagonists: montelukast
  • IgE antibody: Omalizumab (Xolair)
  • Interleukin antagonist: Reslizumab, Mepolizumab, Benralizumab, Dupilumab
  • Cromolyns: Cromolyn sodium

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