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Questions and Answers
What does the C50 represent in pharmacology?
What does the C50 represent in pharmacology?
- The concentration of the drug (correct)
- The therapeutic index of the drug
- The efficacy of a drug
- The maximal effect of a drug
On which axis of a dose-response curve is potency represented?
On which axis of a dose-response curve is potency represented?
- Y-axis
- It is not represented on the graph
- X-axis (correct)
- Z-axis
How are drug potency and receptor affinity related?
How are drug potency and receptor affinity related?
- They have a direct relationship (correct)
- They are unrelated
- They have an indirect relationship
- Potency depends on affinity but not vice versa
What is represented by the plateau part of a dose-response curve?
What is represented by the plateau part of a dose-response curve?
What indicates a highly potent drug on a dose-response curve?
What indicates a highly potent drug on a dose-response curve?
What does the slope of a dose response curve represent?
What does the slope of a dose response curve represent?
What is the therapeutic index calculated from?
What is the therapeutic index calculated from?
Which option best defines efficacy in pharmacological terms?
Which option best defines efficacy in pharmacological terms?
What is the primary reason for using an infusion of opioids instead of single or repeated doses?
What is the primary reason for using an infusion of opioids instead of single or repeated doses?
What is a characteristic of antagonists in relation to receptors?
What is a characteristic of antagonists in relation to receptors?
Which of the following describes inverse agonists?
Which of the following describes inverse agonists?
Which statement correctly describes the effect of continuous blockade by an antagonist?
Which statement correctly describes the effect of continuous blockade by an antagonist?
What is the effect of inverse agonists on cyclic AMP?
What is the effect of inverse agonists on cyclic AMP?
Naloxone displays which type of pharmacological activity?
Naloxone displays which type of pharmacological activity?
Which of the following best defines allosteric modulators?
Which of the following best defines allosteric modulators?
Which statement is true concerning competitive antagonism?
Which statement is true concerning competitive antagonism?
What is the primary effect of administering ephedrine to a patient taking metoprolol?
What is the primary effect of administering ephedrine to a patient taking metoprolol?
What role does neostigmine play at the neuromuscular junction?
What role does neostigmine play at the neuromuscular junction?
In the context of beta-blocker interaction, what may happen even if norepinephrine displaces metoprolol?
In the context of beta-blocker interaction, what may happen even if norepinephrine displaces metoprolol?
What is a key challenge in sedating patients who are on extended release metoprolol?
What is a key challenge in sedating patients who are on extended release metoprolol?
What is the primary function of an allosteric modulator?
What is the primary function of an allosteric modulator?
What is the mechanism by which Narcan acts on opioid receptors?
What is the mechanism by which Narcan acts on opioid receptors?
How does midazolam function as an allosteric modulator of the GABA receptor?
How does midazolam function as an allosteric modulator of the GABA receptor?
What characterizes non-competitive antagonists in clinical use?
What characterizes non-competitive antagonists in clinical use?
What type of allosteric modulator increases the effect of GABA?
What type of allosteric modulator increases the effect of GABA?
Why is there often a need for larger doses of catecholamines in patients on beta blockers?
Why is there often a need for larger doses of catecholamines in patients on beta blockers?
What is the result of a synergistic effect in drug interactions?
What is the result of a synergistic effect in drug interactions?
What commonality exists between neostigmine and Narcan?
What commonality exists between neostigmine and Narcan?
Which of these scenarios describes an antagonistic drug interaction?
Which of these scenarios describes an antagonistic drug interaction?
When combining nitrous oxide with sevoflurane in anesthesia, which type of drug interaction is demonstrated?
When combining nitrous oxide with sevoflurane in anesthesia, which type of drug interaction is demonstrated?
Which outcome occurs when a positive allosteric modulator is present without the primary ligand?
Which outcome occurs when a positive allosteric modulator is present without the primary ligand?
What effect does the binding of propofol and fentanyl together have on a patient during sedation?
What effect does the binding of propofol and fentanyl together have on a patient during sedation?
What does it mean if a drug does not travel into certain tissues?
What does it mean if a drug does not travel into certain tissues?
Where will students access the exam and when?
Where will students access the exam and when?
What feedback do students receive immediately after the exam?
What feedback do students receive immediately after the exam?
What is the relationship between pKa and the ionization of a weak acid at physiological pH?
What is the relationship between pKa and the ionization of a weak acid at physiological pH?
Flashcards
Competitive Antagonism
Competitive Antagonism
When two drugs compete for the same receptor, the drug with higher affinity will bind more strongly and produce a greater effect.
Antagonist
Antagonist
A drug that binds to a receptor and prevents its activation by an agonist, but doesn't produce any effect itself.
Agonist
Agonist
A drug that binds to a receptor and triggers a response.
Non-Competitive Antagonism
Non-Competitive Antagonism
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Drug Affinity
Drug Affinity
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Drug Efficacy
Drug Efficacy
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Beta Blocker
Beta Blocker
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Sympathomimetic
Sympathomimetic
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Inverse Agonist
Inverse Agonist
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Dual Function Antagonist
Dual Function Antagonist
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Allosteric Modulator
Allosteric Modulator
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Positive Allosteric Modulator (PAM)
Positive Allosteric Modulator (PAM)
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Negative Allosteric Modulator (NAM)
Negative Allosteric Modulator (NAM)
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Additive Effect
Additive Effect
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Synergistic Effect
Synergistic Effect
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Antagonistic Effect
Antagonistic Effect
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Volume of Distribution
Volume of Distribution
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Limited Distribution
Limited Distribution
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Exam Scope
Exam Scope
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Exam Password
Exam Password
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Exam Results
Exam Results
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Exam Platform
Exam Platform
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Exam Availability
Exam Availability
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Grade Release Time
Grade Release Time
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What is C50?
What is C50?
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What is efficacy? And what part of the curve represents it?
What is efficacy? And what part of the curve represents it?
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How is drug potency related to receptor affinity?
How is drug potency related to receptor affinity?
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What is LD50/ED50?
What is LD50/ED50?
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What is drug potency?
What is drug potency?
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What does the slope of a dose-response curve represent?
What does the slope of a dose-response curve represent?
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What is a racemic mixture?
What is a racemic mixture?
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What is an agonist?
What is an agonist?
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What is pKa?
What is pKa?
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What is the significance of the pKa of a weak acid?
What is the significance of the pKa of a weak acid?
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What is passive diffusion?
What is passive diffusion?
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What is the blood-brain barrier?
What is the blood-brain barrier?
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What is ionization?
What is ionization?
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How does the pKa of a weak acid affect its entry into the brain?
How does the pKa of a weak acid affect its entry into the brain?
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How is the ionization state of a weak acid related to its pH?
How is the ionization state of a weak acid related to its pH?
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Why would a weak acid with a pKa of 9 have a greater fraction of its ionized form in the plasma compared to a neuron?
Why would a weak acid with a pKa of 9 have a greater fraction of its ionized form in the plasma compared to a neuron?
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Study Notes
Agonist and Antagonist Interaction
- Agonists are substances that bind to receptors and trigger a response.
- Antagonists bind to receptors but do not trigger a response. They prevent agonists from binding and thus block the response.
- Full agonists produce a maximal response.
- Partial agonists produce a response that is less than maximal, even at maximal receptor occupancy.
- Competitive antagonists bind to the same receptor as the agonist, competing for binding sites.
- Non-competitive antagonists bind to a different site from the agonist, altering the receptor's shape and blocking agonist binding.
- Irreversible competitive antagonists bind to the receptor and do not dissociate, permanently blocking the agonist's effect.
Receptor Occupancy and Efficacy
- Efficacy is the ability of a drug to produce a desired effect.
- Potency is the amount of drug needed to produce a certain effect.
- Competitive antagonism decreases potency, but not necessarily efficacy.
- Non-competitive antagonism decreases both potency and efficacy.
Real World Examples
- Beta-blockers are competitive antagonists that obstruct norepinephrine from receptors, requiring increased norepinephrine for an effect.
- Examples of using drugs in an operating room are given when dealing with beta-blockers, such as metoprolol and ephedrine.
- Anesthetics and opioids, such as Narcan, can be antagonists that compete with the agonist leading to a lesser effect from the agonist.
Inverse Agonists
- Inverse agonists bind to the receptor and produce the opposite effect of the agonist.
- Inverse agonists decrease constitutive activity of the receptor.
Allosteric Modulators
- Allosteric modulators bind at a different site on the receptor, altering the receptor's conformation and influencing agonist binding and effects.
- They can either increase or decrease the agonist's effect.
Synergistic and Antagonistic Effects
- Synergistic effects occur when two drugs together produce a greater effect than the sum of their individual effects.
- Antagonistic effects occur when two drugs together produce a weaker effect than the sum of their individual effects.
Hormonal Differences
- Females may have a higher sensitivity to muscle relaxants and may emerge from anesthesia more quickly than males.
- Hormonal changes can influence drug responses.
Tachyphylaxis
- Tachyphylaxis is a rapid decrease in the response to a drug upon repeated administration.
- This is caused by reduced receptor availability or changes in receptor function due to repeated agonist exposure.
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Description
Test your knowledge on pharmacological concepts related to dose-response relationships, including drug potency, efficacy, and receptor interactions. This quiz covers essential terms and definitions necessary for understanding pharmacodynamics and drug actions.