Pharmacology: Receptor Agonists and Antagonists
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Questions and Answers

What physiological response is associated with α1 receptor agonists?

  • Glycogenolysis
  • Increased insulin secretion
  • Contraction (correct)
  • Relaxation
  • Which medication is an inhibitor of fibrinolysis and is useful in trauma situations?

  • Albuterol
  • Levalbuterol
  • Aminocaproic Acid (correct)
  • Propranolol
  • What effect does Propranolol have on β2 receptors?

  • Glycogenolysis and gluconeogenesis
  • Relaxation of smooth muscles
  • Increased renin secretion
  • Inhibition of glycogenolysis (correct)
  • Which class of drugs is primarily used for rescue treatment in asthma management?

    <p>Short-acting beta-2 agonists</p> Signup and view all the answers

    What side effect might be experienced from the overuse of short-acting beta-2 agonists?

    <p>Reduction in beta-receptor efficacy</p> Signup and view all the answers

    What is the primary mechanism of action of β1 receptor agonists like Dobutamine?

    <p>Increased contractile force</p> Signup and view all the answers

    Which agonist is known to cause relaxation of airway smooth muscle?

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

    What physiological outcomes are associated with β2 receptor agonists?

    <p>Glycogenolysis and uptake of K+</p> Signup and view all the answers

    Which medication helps in preventing exacerbations in mild asthma?

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

    What is the primary adverse effect associated with oral corticosteroids like prednisone?

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

    Which class of medication targets the G551D mutation in cystic fibrosis?

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

    What is a notable side effect of monoclonal antibodies like Omalizumab?

    <p>Injection site reactions</p> Signup and view all the answers

    Which of the following is a clinical pearl regarding the use of inhaled corticosteroids?

    <p>They reduce asthma mortality when initiated early.</p> Signup and view all the answers

    Which medication requires rinsing the mouth to reduce oral thrush risk?

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

    What is a significant risk associated with Omalizumab treatment?

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

    Which of the following IL-5 inhibitors is known for reducing eosinophil recruitment?

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

    What is a significant risk associated with the use of long-acting beta-2 agonists (LABA) as monotherapy in asthma?

    <p>Increased risk of asthma-related death</p> Signup and view all the answers

    Which of the following is true about short-acting anticholinergics (SAMA)?

    <p>They can prevent hospitalization with LABA therapy.</p> Signup and view all the answers

    What is the primary mechanism of action for leukotriene receptor antagonists (LTRA)?

    <p>Blocking leukotriene receptor or synthesis</p> Signup and view all the answers

    What characterizes methylxanthines as a last-resort treatment for asthma?

    <p>They have a high risk of adverse effects.</p> Signup and view all the answers

    Which of the following side effects is most commonly associated with methylxanthines?

    <p>Nausea/vomiting</p> Signup and view all the answers

    What treatment option can be used as a first-line therapy in children for asthma?

    <p>5-Lipoxygenase inhibitors</p> Signup and view all the answers

    What is the main indication for using short-acting beta-2 agonists (SABA)?

    <p>Relief of acute asthma exacerbations</p> Signup and view all the answers

    What is a notable side effect associated with long-acting beta-2 agonists?

    <p>Increased risk of asthma-related death</p> Signup and view all the answers

    Study Notes

    Case 1: Shock and Receptor Agonists/Antagonists

    • Receptor α1: Agonists include Epinephrine, Norepinephrine, and Phenylephrine. Antagonist is Prazosin. Physiological outcome is contraction.
    • Receptor α2: Agonists include Epinephrine, Norepinephrine, and Clonidine. Antagonist is Yohimbine. Physiological outcome is contraction.
    • Receptor β1: Agonists include Dobutamine, Epinephrine, and Isoproterenol. Antagonists include Metoprolol. Physiological outcome is increased renin secretion and increased force, rate of contraction.
    • Receptor β2: Agonists include Terbutaline, Epinephrine, and Isopertrenol. Antagonists include Propranolol. Physiological outcome is relaxation and glycogenolysis.

    Medication Mechanisms and Clinical Usage

    • Aminocaproic Acid: Inhibits the conversion of plasminogen to plasmin, inhibiting fibrinolysis. Clinical use is to preserve integrity of clot formation in surgery and trauma.
    • Tranexamic Acid: Inhibitor of fibrinolysis. Useful in surgery, trauma, including knife, gunshot.

    Case 2: Pharmacotherapy of Asthma Management

    • Short-Acting Beta-2 Agonists (SABA): Stimulate adenylyl cyclase to increase cAMP, leading to airway and smooth muscle relaxation. Used as rescue treatment ("as needed"). Examples include Albuterol and Levalbuterol.
    • Long-Acting Beta-2 Agonists (LABA): Also stimulate adenylyl cyclase to increase cAMP, but have a longer duration of action than SABAs. Must be used in combination with inhaled corticosteroids. Examples include Salmeterol and Formoterol.
    • Anti-cholinergics (SAMA/LAMA): Antagonize acetylcholine's effects on muscarinic receptors, resulting in airway relaxation. Can be short or long acting.
    • Leukotriene Modifiers (LTRA-M): Block leukotriene receptor or block leukotriene synthesis. Reduce granulocyte migration and increase bronchodilation. Examples include Montelukast and Zafirlukast.
    • 5-Lipoxygenase Inhibitors: Similar to leukotriene modifiers, they inhibit 5-lipoxygenase synthesis and reduce granulocyte migration. Examples include Zafirlukast and Montelukast.

    Case 3: Treatment of Asthma Management

    • Methylxanthines (Theophylline, Caffeine): Phosphodiesterase 4 inhibitors, increase cAMP, and thus reducing airway inflammation. Often last-resort due to high risk of adverse events.
    • Inhaled Corticosteroids (ICS): Inhibit transcription of pro-inflammatory genes and reduce airway inflammation. Examples include Beclomethasone, Budesonide, Fluticasone, and Mometasone.
    • Oral Corticosteroids: Anti-inflammatory agents. Can cause adverse effects like adrenal suppression, hyperglycemia, and hypertension.
    • Monoclonal Antibodies: Targets IgE (Omalizumab), IL-5 targets eosinophil recruitment (Mepolizumab, Reslizumab, Benralizumab).

    Case 3: Treatment of Cystic Fibrosis

    • Ivacaftor: Targets the G551D mutation, opening the chloride channel.
    • Trikafta: Combination of elexacaftor, tezacaftor, and ivacaftor. Assists in moving CFTR protein within cells (improving processing of proteins with deltaF508 mutation), in combination with ivacaftor.

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    Description

    This quiz covers the mechanisms and physiological outcomes of various receptor agonists and antagonists, focusing on adrenergic receptors. It includes specific medications like Epinephrine, Prazosin, and others used in clinical settings. Test your understanding of their actions and applications in medicine.

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