Podcast
Questions and Answers
Which group shift prevents the action of COMT enzyme in the context of β2-agonist discovery?
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?
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?
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?
What prevents action by Ndealkylation in the metabolism of β2-agonists?
What makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site in the context of β2-agonist discovery?
What makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site in the context of β2-agonist discovery?
What role do direct-acting β-agonists play in binding to the receptor site?
What role do direct-acting β-agonists play in binding to the receptor site?
Which medication has a bitopic structure and is resistant to both MAO and COMT enzymes?
Which medication has a bitopic structure and is resistant to both MAO and COMT enzymes?
What is the main reason for the long duration of action of Formoterol?
What is the main reason for the long duration of action of Formoterol?
Which leukotriene antagonist is contraindicated in liver impairment?
Which leukotriene antagonist is contraindicated in liver impairment?
Which leukotriene antagonist has a FDA caution for the risk of neuropsychiatric events?
Which leukotriene antagonist has a FDA caution for the risk of neuropsychiatric events?
Which medication is an injectable prescription medicine used to treat moderate to severe allergic asthma?
Which medication is an injectable prescription medicine used to treat moderate to severe allergic asthma?
Which medication is highly lipophilic with optimal direct-acting β2-receptor selectivity and potency?
Which medication is highly lipophilic with optimal direct-acting β2-receptor selectivity and potency?
Which medication has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom?
Which medication has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom?
Which medication is associated with drug-drug interactions with other drugs metabolized by CYP3A4?
Which medication is associated with drug-drug interactions with other drugs metabolized by CYP3A4?
What makes Tiotropium bromide more cost-effective compared to Ipratropium in the treatment of COPD?
What makes Tiotropium bromide more cost-effective compared to Ipratropium in the treatment of COPD?
Which medication has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring?
Which medication has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring?
What is the fundamental pharmacophore for all β-adrenergic agonists?
What is the fundamental pharmacophore for all β-adrenergic agonists?
What is the main reason for the long duration of action of Formoterol?
What is the main reason for the long duration of action of Formoterol?
Which medication has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring?
Which medication has a lipophilic substituent in combination with a βOH group and a salicyl phenyl ring?
What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?
What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?
What makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site in the context of β2-agonist discovery?
What makes a compound unrecognizable by the metabolic enzyme while still binding to the receptor site in the context of β2-agonist discovery?
What prevents action by Ndealkylation in the metabolism of β2-agonists?
What prevents action by Ndealkylation in the metabolism of β2-agonists?
What is the primary reason behind the long duration of action of Tiotropium bromide?
What is the primary reason behind the long duration of action of Tiotropium bromide?
Which medication is hepatically metabolized by CYP2C9 and inhibits the action of CYP3A4, leading to drug-drug interactions with other drugs metabolized by CYP3A4?
Which medication is hepatically metabolized by CYP2C9 and inhibits the action of CYP3A4, leading to drug-drug interactions with other drugs metabolized by CYP3A4?
Which leukotriene antagonist is contraindicated in liver impairment?
Which leukotriene antagonist is contraindicated in liver impairment?
What is the role of LABAs such as Salmetrol in terms of receptor selectivity and potency?
What is the role of LABAs such as Salmetrol in terms of receptor selectivity and potency?
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?
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?
What makes XOLAIR® (omalizumab) unique in its use for treating allergic asthma?
What makes XOLAIR® (omalizumab) unique in its use for treating allergic asthma?
Which medication has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom?
Which medication has a lipophilic β-directing N-isopropyl p-methoxyphenyl group on the nitrogen atom?
What is the pharmacokinetic advantage of using Tiotropium bromide over Ipratropium in cases of COPD treatment?
What is the pharmacokinetic advantage of using Tiotropium bromide over Ipratropium in cases of COPD treatment?
What is the fundamental pharmacophore for all β-adrenergic agonists?
What is the fundamental pharmacophore for all β-adrenergic agonists?
What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?
What confers both β1- and β2-receptor selectivity in β-adrenergic agonists?
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.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
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.
