Respiratory System Issues: β2-Agonist Discovery
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Respiratory System Issues: β2-Agonist Discovery

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Questions and Answers

Which group shift prevents the action of COMT enzyme in the context of β2-agonist discovery?

  • Shifting the OH group from para position to meta position (correct)
  • Moving the OH group out by one carbon unit
  • Adding a methyl group to the benzene ring
  • Removing the OH group from the benzene ring

    • What is the fundamental pharmacophore for all β-adrenergic agonists?

  • Substituted α-phenylethanolamine
  • Unsubstituted β-phenylethanolamine
  • Substituted β-phenylethanolamine (correct)
  • Unsubstituted α-phenylethanolamine

    • What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?

  • The bulk of the N-substituent (R1) (correct)
  • The presence of an m-OH group (R2)
  • The absence of any substituents
  • The size of the R2 group

    • What prevents action by Ndealkylation in the metabolism of β2-agonists?

    <p>Addition of a tertiary butyl group</p> Signup and view all the answers

    What makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site in the context of β2-agonist discovery?

    <p>Presence of an m-OH group (R2)</p> Signup and view all the answers

    What role do direct-acting β-agonists play in binding to the receptor site?

    <p>They bind to the receptor similar to EPI</p> Signup and view all the answers

    Which medication has a bitopic structure and is resistant to both MAO and COMT enzymes?

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

    What is the main reason for the long duration of action of Formoterol?

    <p>Association with lipid bilayer</p> Signup and view all the answers

    Which leukotriene antagonist is contraindicated in liver impairment?

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

    Which leukotriene antagonist has a FDA caution for the risk of neuropsychiatric events?

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

    Which medication is an injectable prescription medicine used to treat moderate to severe allergic asthma?

    <p>XOLAIR® (omalizumab)</p> Signup and view all the answers

    Which medication is highly lipophilic with optimal direct-acting β2-receptor selectivity and potency?

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

    Which medication has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom?

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

    Which medication is associated with drug-drug interactions with other drugs metabolized by CYP3A4?

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

    What makes Tiotropium bromide more cost-effective compared to Ipratropium in the treatment of COPD?

    <p>Given once compared to three to four times daily</p> Signup and view all the answers

    Which medication has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring?

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

    What is the fundamental pharmacophore for all β-adrenergic agonists?

    <p>Substituted β-phenylethanolamine</p> Signup and view all the answers

    What is the main reason for the long duration of action of Formoterol?

    <p>Resistance to MAO and COMT enzymes</p> Signup and view all the answers

    Which medication has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring?

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

    What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?

    <p>Bulk of the N-substituent (R1)</p> Signup and view all the answers

    What makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site in the context of β2-agonist discovery?

    <p>Shift of the OH group to the meta position</p> Signup and view all the answers

    What prevents action by Ndealkylation in the metabolism of β2-agonists?

    <p>Tertiary butyl groups</p> Signup and view all the answers

    What is the primary reason behind the long duration of action of Tiotropium bromide?

    <p>Association with lipid bilayer</p> Signup and view all the answers

    Which medication is hepatically metabolized by CYP2C9 and inhibits the action of CYP3A4, leading to drug-drug interactions with other drugs metabolized by CYP3A4?

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

    Which leukotriene antagonist is contraindicated in liver impairment?

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

    What is the role of LABAs such as Salmetrol in terms of receptor selectivity and potency?

    <p>Highly lipophilic with optimal selectivity and potency</p> Signup and view all the answers

    Which medication is an orally administered leukotriene receptor antagonist used for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older?

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

    What makes XOLAIR® (omalizumab) unique in its use for treating allergic asthma?

    <p>Injectable monoclonal antibody/IgE binding inhibitor</p> Signup and view all the answers

    Which medication has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom?

    <p>Formotero l</p> Signup and view all the answers

    What is the pharmacokinetic advantage of using Tiotropium bromide over Ipratropium in cases of COPD treatment?

    <p>Cost-effectiveness due to less frequent administration</p> Signup and view all the answers

    What is the fundamental pharmacophore for all β-adrenergic agonists?

    <p>Salicyl phenyl ring for optimal direct-acting β2-receptor selectivity and potency</p> Signup and view all the answers

    What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?

    <p>Presence of 3’-formylamino (β-directing) group</p> Signup and view all the answers

    Study Notes

    β2-Agonist Discovery

    • The para-hydroxyl group shift prevents the action of COMT enzyme in the context of β2-agonist discovery.
    • The fundamental pharmacophore for all β-adrenergic agonists is a β-phenethylamine structure.
    • A lipophilic substituent on the nitrogen atom confers both β1- and β2-receptor selectivity in β-adrenergic agonists.
    • A βOH group prevents action by Ndealkylation in the metabolism of β2-agonists.
    • A lipophilic substituent on the nitrogen atom makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site.

    Medications

    • Salmeterol has a bitopic structure and is resistant to both MAO and COMT enzymes.
    • The main reason for the long duration of action of Formoterol is its high lipophilicity.
    • Zafirlukast is contraindicated in liver impairment.
    • Montelukast has a FDA caution for the risk of neuropsychiatric events.
    • Omalizumab is an injectable prescription medicine used to treat moderate to severe allergic asthma.
    • Formoterol is highly lipophilic with optimal direct-acting β2-receptor selectivity and potency.
    • Salmeterol has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom.
    • Montelukast is associated with drug-drug interactions with other drugs metabolized by CYP3A4.

    COPD Treatment

    • Tiotropium bromide is more cost-effective compared to Ipratropium in the treatment of COPD due to its longer duration of action.
    • Tiotropium bromide has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring.
    • The primary reason behind the long duration of action of Tiotropium bromide is its high lipophilicity.
    • The pharmacokinetic advantage of using Tiotropium bromide over Ipratropium in cases of COPD treatment is its longer duration of action.

    Leukotriene Antagonists

    • Zafirlukast is an orally administered leukotriene receptor antagonist used for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older.
    • XOLAIR (omalizumab) is unique in its use for treating allergic asthma as it is an injectable prescription medicine.

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    Description

    Test your knowledge of the discovery and mechanism of β2-agonists in the context of respiratory system issues. This quiz covers the storyline of β2-agonist discovery and its application in medicinal PD511, Fall Semester 2023/2024.

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