Anticholinergic Bronchodilators Overview
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Questions and Answers

Which of the following drugs is a combination therapy for COPD?

  • Tiotropium bromide (Spiriva)
  • Umeclidinium bromide (Incruse Ellipta)
  • Aclidinium bromide (Tudorza Pressair)
  • Combivent HFA (correct)

    • What is the mechanism of action of anticholinergic bronchodilators?

  • Increasing the production of cAMP
  • Blocking the action of acetylcholine (correct)
  • Stimulating the release of acetylcholine
  • Decreasing the production of cAMP

    • How do anticholinergics compare to β-adrenergics as bronchodilators in emphysema/bronchitis?

  • Anticholinergics are less potent.
  • There is no difference in potency.
  • Anticholinergics are more potent. (correct)
  • Anticholinergics are just as potent.

    • Which of the following side effects is most likely to occur with inhaled ipratropium?

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

    What is the FDA-approved use for anticholinergics?

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

    What is NOT a condition where anticholinergics could be useful in treating asthma?

    <p>Asthma caused by a viral infection. (C)</p> Signup and view all the answers

    Which of the following drugs is a long-acting anticholinergic bronchodilator used once daily?

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

    What is the difference between tertiary and quaternary ammonium compounds in terms of their effects on the central nervous system?

    <p>Tertiary ammonium compounds have no effect on the central nervous system, while quaternary ammonium compounds can have a significant effect. (C)</p> Signup and view all the answers

    What is the main reason to use β-adrenergic and anticholinergic agents together in COPD?

    <p>They have different sites of action on bronchi and their mechanisms enhance each other. (C)</p> Signup and view all the answers

    Which of the following drugs is approved for the maintenance treatment of COPD?

    <p>Aclidinium bromide (Tudorza Pressair) (D)</p> Signup and view all the answers

    What is the approximate mean peak increase in lung function for combining β-agonists and anticholinergics?

    <p>30-35%. (C)</p> Signup and view all the answers

    Why might the β-agonist be given first when administering both β-agonists and anticholinergics?

    <p>The β-agonist has a more rapid onset of action and is distributed in both large and small airways. (A)</p> Signup and view all the answers

    Which of the following drugs has a very low and transient systemic exposure?

    <p>Aclidinium bromide (Tudorza Pressair) (D)</p> Signup and view all the answers

    When assessing the effectiveness of anticholinergic bronchodilator therapy, what should NOT be monitored?

    <p>Blood pressure. (B)</p> Signup and view all the answers

    What is the primary effect of parasympathetic innervation on the airways?

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

    Which of the following is NOT a potential benefit of anticholinergics in asthma?

    <p>Relief of asthma caused by allergies. (A)</p> Signup and view all the answers

    Which of the following is NOT a specific stimulus that can trigger a vagally mediated bronchoconstriction reflex?

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

    Which muscarinic receptor subtype is primarily responsible for smooth airway muscle contraction?

    <p>M3 (D)</p> Signup and view all the answers

    What is the primary mechanism by which anticholinergic agents act as bronchodilators?

    <p>Competitively inhibiting acetylcholine from binding to its receptors (C)</p> Signup and view all the answers

    Which of the following is a common side effect of anticholinergic medications?

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

    What is the role of substance P in vagally mediated reflex bronchoconstriction?

    <p>It is released by sensory C-fibers and plays a role in transmitting the signal to the central nervous system. (D)</p> Signup and view all the answers

    Which of the following anticholinergics is selective for M1 and M3 receptors, potentially reducing the risk of adverse effects on the heart rate?

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

    What is the primary impact of anticholinergics on the ventilation-perfusion ratio?

    <p>They have no significant effect on ventilation-perfusion abnormalities. (A)</p> Signup and view all the answers

    What is the main reason why anticholinergics are not typically associated with a risk of tolerance or loss of protective reflexes?

    <p>They do not directly affect the receptors involved in these reflexes. (C)</p> Signup and view all the answers

    What is the primary use of anticholinergic bronchodilators?

    <p>To manage COPD maintenance. (C)</p> Signup and view all the answers

    Which of these is NOT a specific anticholinergic agent listed in the content?

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

    What is the specific type of receptor that anticholinergics target?

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

    In what form is ipratropium bromide available?

    <p>In various forms including MDIs, solutions, and nasal sprays (C)</p> Signup and view all the answers

    What is the primary advantage of inhaled anticholinergics?

    <p>They have a long duration of action. (A)</p> Signup and view all the answers

    What is the main reason why ipratropium bromide may be used in some individuals with asthma?

    <p>It may be used when β-agonists are ineffective. (D)</p> Signup and view all the answers

    What type of drug is ipratropium bromide classified as chemically?

    <p>A quaternary ammonium derivative (D)</p> Signup and view all the answers

    Flashcards

    Ipratropium and Albuterol

    Combination medication used for COPD management.

    Combivent HFA

    A combination inhaler with ipratropium (18 μg) and albuterol (90 μg).

    Tiotropium bromide

    Once-daily bronchodilator specific to M1 and M3 receptors.

    Umeclidinium bromide

    Once-daily bronchodilator administered by DPI (62.5 μg).

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    Aclidinium bromide

    Antagonist effective in COPD maintenance, available as DPI (400 μg).

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    Anticholinergic Agents

    Medications that block acetylcholine effects, primarily in the lungs.

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    Parasympathetic Innervation

    Nervous system activity that increases bronchomotor tone.

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    Bronchodilation Mechanism

    Process by which parasympatholytic agents relax airway muscles.

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    Anticholinergic bronchodilators

    Medications that block acetylcholine at muscarinic receptors in bronchial smooth muscle.

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    Parasympatholytic response

    A response that inhibits the actions of the parasympathetic nervous system.

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    Ipratropium bromide

    An anticholinergic bronchodilator used for COPD maintenance.

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    Clinical indications for anticholinergics

    Used for COPD maintenance, asthma, and rhinitis.

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    Combination therapies

    Use of anticholinergic and β-agonist bronchodilators together.

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    Administration forms of Ipratropium

    Available as MDI, SVN solution, and nasal spray.

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    COPD Treatment

    Use of potent bronchodilators like tiotropium in COPD.

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    Tiotropium vs. Ipratropium

    Tiotropium maintains higher PFT levels than ipratropium.

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    Asthma Indications

    Antimuscarinics not approved for asthma in the US but may help with certain types.

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    Combination Therapy

    Using β-adrenergic and anticholinergic agents together in COPD leads to an additive effect.

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    Drug Administration Sequence

    No preference for which drug to administer first, but β-agonist acts faster.

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    Assessing Effectiveness

    Monitor flow rates and perform respiratory assessments post-treatment.

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    Nocturnal Asthma

    Anticholinergics may be useful for asthma at night.

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    Acute Asthma Episodes

    Anticholinergics can be alternatives when β-agonists fail during acute asthma episodes.

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    Vagally Mediated Reflex

    Reflex broncoconstriction triggered by irritants that send impulses to the CNS.

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    M1 Receptors

    Muscarinic receptors in the parasympathetic ganglia, facilitating neurotransmission.

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    M2 Receptors

    Muscarinic receptors that inhibit acetylcholine, potentially increasing acetylcholine release.

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    M3 Receptors

    Muscarinic receptors in smooth airway muscles causing bronchoconstriction.

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    Adverse Effects of Anticholinergics

    Common side effects include dry mouth, cough, and mydriasis.

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    Mechanism of Action

    Blocking acetylcholine prevents bronchoconstriction via anticholinergic drugs.

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    Role of Acetylcholine

    Neurotransmitter that triggers bronchoconstriction and mucus secretion.

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    Study Notes

    Anticholinergic Bronchodilators

    • Anticholinergic bronchodilators are specifically parasympatholytic agents.
    • They block the effects of acetylcholine at cholinergic (muscarinic) receptors on bronchial smooth muscle.
    • They are used for COPD maintenance.
    • Ipratropium bromide may be used for some individuals with asthma.
    • Combined anticholinergic and β-agonist bronchodilators are also used in cases of COPD with airflow obstruction or severe asthma not responsive to β-agonist therapy.

    Clinical Indications

    • Anticholinergic nasal spray is used for allergic and nonallergic perennial rhinitis and the common cold.

    Inhaled Anticholinergic Bronchodilator Agents

    • Ipratropium bromide (Atrovent)
    • Ipratropium bromide and albuterol (Combivent, Duoneb, Combivent Respimat)
    • Aclidinium bromide (Tudorza Pressair)
    • Tiotropium bromide (Spiriva)
    • Umeclidinium bromide (Incruse Ellipta)
    • Umeclidinium bromide and vilanterol (Anoro Ellipta)

    Ipratropium Bromide (Atrovent HFA)

    • Available as Metered-Dose Inhaler (MDI), 17 µg/puff, 2 puffs every four hours.
    • Available as a solution for nebulizer (SVN), 0.2% solution, 0.5 mg every four hours.
    • Approved for maintenance treatment of airflow obstruction in COPD.
    • Quaternary ammonium derivative of atropine.
    • Distribution limited to the lungs when inhaled.

    Ipratropium and Albuterol (Combivent HFA, Duoneb, Combivent Respimat)

    • Combivent: 18 µg ipratropium and 90 µg albuterol/puff, 2 puffs every four hours.
    • Duoneb: 0.5 mg ipratropium and 2.5 mg albuterol
    • Combivent Respimat: 20 µg ipratropium and 100 µg albuterol/puff, every four hours.
    • Combination therapy is more effective in stable COPD than either agent alone.

    Once-Daily Anticholinergic Bronchodilators

    • Tiotropium bromide (Spiriva): M1 and M3 selectivity, DPI 18 µg/inhalation, once daily.
    • Umeclidinium bromide (Incruse Ellipta): DPI 62.5 µg/inhalation, once daily.
    • Umeclidinium bromide and vilanterol (Anoro Ellipta): DPI 62.5 µg umeclidinium and 25 µg vilanterol/puff, once daily.

    Aclidinium Bromide (Tudorza Pressair)

    • Approved for the maintenance treatment in COPD.
    • DPI: 400 µg/inhalation, 1 inhalation twice daily.
    • Potent antagonist for all muscarinic receptors.
    • Very low and transient systemic exposure.
    • Reduced potential for side effects.

    Pharmacological Effects

    • Anticholinergic (antimuscarinic) agents have tertiary ammonium compound effects on the respiratory tract, central nervous system, eyes, cardiac, gastrointestinal, and genitourinary systems.
    • Quaternary ammonium compound effects when inhaled: Respiratory tract – bronchodilation, Central nervous system – no effect, Eyes – pupillary dilation and lens paralysis, Cardiac – no effect, Gastrointestinal – dry mouth, Genitourinary – usually no effect.
    • Side effects are localized to the site of drug exposure.

    Mode of Action

    • Parasympathetic innervation increases basal level bronchomotor tone.
    • Parasympatholytic bronchodilators block this tone.
    • Degree of bronchodilation depends on the amount of parasympathetic tone present.

    Receptor Subtypes

    • Muscarinic receptors: M1, M2, M3
    • M1: parasympathetic ganglia, neurotransmission and bronchoconstriction, secretion/rhinitis (GUT)
    • M2: inhibit acetylcholine, blockade may enhance release, counteracting bronchodilation (tiotropium is selective for M1 and M3)
    • M3: smooth airway muscle and submucosal glands, bronchoconstriction, secretion/rhinitis

    Adverse Effects

    • Changes in BP, EKG, or HR are not usually seen.
    • No worsening of ventilation-perfusion abnormalities.
    • No tolerance/loss of protection.
    • Side effects: dry mouth (most common), cough, mydriasis (eyes should be protected), SVN: pharyngitis, dyspnea, flulike symptoms, bronchitis, upper respiratory infection.

    Clinical Application

    • In COPD: more potent bronchodilators than β-adrenergics in emphysema/bronchitis. FDA approved specifically for COPD; Tiotropium maintains higher PFT levels than ipratropium.
    • In Asthma: No label indication in the US. Antimuscarinics may be equal or slightly inferior to β-agonists. May be useful in nocturnal asthma, psychogenic asthma, asthma patients on β-blockers, acute/severe episodes not responding to β-agonists, alternative to theophylline.

    Combination Therapy

    • β-Adrenergic and anticholinergic agents in COPD have complementary sites of action.
    • Additive effect on peak increases (31-33% for combined drugs, 24-25% for ipratropium alone, 24-27% for albuterol alone).

    Administration

    • Sequence: No data to support one drug being administered before the other.
    • β agonists have more rapid onset due to dispersion in large and small airways.

    Respiratory Care Assessment

    • Assess effectiveness using indication for use, monitor flow rates, perform respiratory assessment (breath sounds, auscultation, respiratory rate), assess pulse, and subjective reaction. - Arterial blood gases/SpO2, long-term PFTs.
    • Instruct/verify correct device use, monitor lung function over time, look for concomitant β-agonist use and nocturnal/exacerbated symptoms, check for hospitalizations and absences from work/school.

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    Description

    This quiz covers the role of anticholinergic bronchodilators in the management of COPD and asthma. It includes information on specific agents, their clinical indications, and combinations with β-agonists. Test your knowledge on key medications and their uses in respiratory therapy.

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