Pharmacology Dose-Response Quiz
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Questions and Answers

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?

  • Y-axis
  • It is not represented on the graph
  • X-axis (correct)
  • Z-axis

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?

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

What indicates a highly potent drug on a dose-response curve?

<p>Steep slope of the curve (A)</p> Signup and view all the answers

What does the slope of a dose response curve represent?

<p>Number of receptors occupied (C)</p> Signup and view all the answers

What is the therapeutic index calculated from?

<p>LD50 over ED50 (B)</p> Signup and view all the answers

Which option best defines efficacy in pharmacological terms?

<p>The ability of a drug to produce a desired effect (D)</p> Signup and view all the answers

What is the primary reason for using an infusion of opioids instead of single or repeated doses?

<p>The duration of action of opioids is often longer than that of antagonists like flumazenil. (D)</p> Signup and view all the answers

What is a characteristic of antagonists in relation to receptors?

<p>They do not activate receptors and lack efficacy. (A)</p> Signup and view all the answers

Which of the following describes inverse agonists?

<p>They decrease the intrinsic activity of receptors. (A)</p> Signup and view all the answers

Which statement correctly describes the effect of continuous blockade by an antagonist?

<p>It results in the downregulation of the target receptor. (A)</p> Signup and view all the answers

What is the effect of inverse agonists on cyclic AMP?

<p>They decrease cyclic AMP levels. (D)</p> Signup and view all the answers

Naloxone displays which type of pharmacological activity?

<p>Both inverse agonist and antagonist effects. (D)</p> Signup and view all the answers

Which of the following best defines allosteric modulators?

<p>They enhance or diminish the effect of an agonist. (A)</p> Signup and view all the answers

Which statement is true concerning competitive antagonism?

<p>It can be overcome by increasing the concentration of agonists. (C)</p> Signup and view all the answers

What is the primary effect of administering ephedrine to a patient taking metoprolol?

<p>Increases catecholamine levels while facing receptor competition (B)</p> Signup and view all the answers

What role does neostigmine play at the neuromuscular junction?

<p>It prevents the breakdown of acetylcholine to increase receptor activation (D)</p> Signup and view all the answers

In the context of beta-blocker interaction, what may happen even if norepinephrine displaces metoprolol?

<p>Metoprolol can reoccupy the receptor after being displaced (A)</p> Signup and view all the answers

What is a key challenge in sedating patients who are on extended release metoprolol?

<p>It complicates the administration of adrenergic agents (B)</p> Signup and view all the answers

What is the primary function of an allosteric modulator?

<p>To bind to a different site on the receptor (D)</p> Signup and view all the answers

What is the mechanism by which Narcan acts on opioid receptors?

<p>It competes with opioids at their receptors (D)</p> Signup and view all the answers

How does midazolam function as an allosteric modulator of the GABA receptor?

<p>It enhances GABA's effect without binding to the GABA site (D)</p> Signup and view all the answers

What characterizes non-competitive antagonists in clinical use?

<p>They permanently occupy receptors and cannot be displaced (D)</p> Signup and view all the answers

What type of allosteric modulator increases the effect of GABA?

<p>Positive allosteric modulator (A)</p> Signup and view all the answers

Why is there often a need for larger doses of catecholamines in patients on beta blockers?

<p>Catecholamines are less effective against fully occupied receptors (C)</p> Signup and view all the answers

What is the result of a synergistic effect in drug interactions?

<p>The combined effect exceeds the sum of individual effects (A)</p> Signup and view all the answers

What commonality exists between neostigmine and Narcan?

<p>Both act by competing for receptor sites (B)</p> Signup and view all the answers

Which of these scenarios describes an antagonistic drug interaction?

<p>Administering one drug that blocks the effect of another (A)</p> Signup and view all the answers

When combining nitrous oxide with sevoflurane in anesthesia, which type of drug interaction is demonstrated?

<p>Synergistic effect (B)</p> Signup and view all the answers

Which outcome occurs when a positive allosteric modulator is present without the primary ligand?

<p>The receptor remains inactive (D)</p> Signup and view all the answers

What effect does the binding of propofol and fentanyl together have on a patient during sedation?

<p>They may enhance the respiratory suppression effect (B)</p> Signup and view all the answers

What does it mean if a drug does not travel into certain tissues?

<p>The drug will have no effect on those tissues. (A)</p> Signup and view all the answers

Where will students access the exam and when?

<p>On Canvas, after 9 a.m. the day of the exam. (B)</p> Signup and view all the answers

What feedback do students receive immediately after the exam?

<p>No feedback or preliminary results. (C)</p> Signup and view all the answers

What is the relationship between pKa and the ionization of a weak acid at physiological pH?

<p>At pH lower than pKa, the acid remains unionized (B)</p> Signup and view all the answers

Flashcards

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

A drug that binds to a receptor and prevents its activation by an agonist, but doesn't produce any effect itself.

Agonist

A drug that binds to a receptor and triggers a response.

Non-Competitive Antagonism

A type of antagonist that binds to a receptor at a site different from the agonist binding site, preventing agonist binding and action.

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Drug Affinity

The strength of a drug's attraction to a receptor.

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Drug Efficacy

The ability of a drug to produce a physiological effect when it binds to a receptor.

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Beta Blocker

A drug that blocks the effects of beta-adrenergic receptors, which are found in the heart and blood vessels.

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Sympathomimetic

A drug that increases the levels of catecholamines, such as epinephrine and norepinephrine, in the body.

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Inverse Agonist

A type of drug that can bind to a receptor and reduce its activity below its normal baseline level.

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Dual Function Antagonist

Drugs like naloxone that have both antagonist and inverse agonist effects.

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Allosteric Modulator

A type of modulator drug that binds to a receptor at a different site than the agonist, changing the receptor's response to the agonist. This can occur by either enhancing or inhibiting the receptor's activity.

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Positive Allosteric Modulator (PAM)

An allosteric modulator that enhances the effect of the agonist.

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Negative Allosteric Modulator (NAM)

An allosteric modulator that reduces the effect of the agonist.

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Additive Effect

The combined effect of two drugs is equal to the sum of their individual effects.

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Synergistic Effect

The effect of two drugs together is greater than the sum of their individual effects.

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Antagonistic Effect

One drug cancels or reduces the effect of another drug.

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Volume of Distribution

The extent to which a drug is distributed to different tissues in the body.

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Limited Distribution

When a drug is not distributed to tissues where it won't have an effect, it's said to have limited distribution.

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Exam Scope

The exam will focus on the content covered in the PowerPoints and lectures. Materials not discussed in these resources may not be on the exam.

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Exam Password

The exam password will be provided on Canvas a short time before the test begins.

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Exam Results

The results of the exam will be uploaded to Canvas after the exam is graded.

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Exam Platform

The exam will be taken on ExamSoft, a digital platform.

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Exam Availability

The exam will be available until the weekend, and the time limit will be announced.

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Grade Release Time

The time it takes to release exam grades after the completion of grading. It is usually done quickly, within a reasonable time frame.

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What is C50?

The concentration of a drug, usually represented on the x-axis of a dose-response curve. It indicates the amount of drug needed to elicit a certain response.

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What is efficacy? And what part of the curve represents it?

The ability of a drug to produce a maximal effect, regardless of the dose. It is represented by the plateau on the dose-response curve.

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How is drug potency related to receptor affinity?

The strength of a drug's attraction to a receptor. A higher affinity means the drug binds more readily to the receptor.

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What is LD50/ED50?

The ratio of the lethal dose (LD50) to the effective dose (ED50). This indicates the safety margin of a drug.

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What is drug potency?

The measure of how much drug is needed to produce a certain level of effect. A highly potent drug produces a strong effect at low concentrations.

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What does the slope of a dose-response curve represent?

The slope of the dose-response curve represents the number of receptors occupied by the drug at different concentrations.

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What is a racemic mixture?

A mixture of two enantiomers, which are mirror images of each other. These mirror images often have different pharmacological effects.

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What is an agonist?

A drug that binds to a receptor and activates it, producing a biological response.

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What is pKa?

A measure of the tendency of a weak acid to donate a proton (H+). Lower pKa values indicate stronger acids.

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What is the significance of the pKa of a weak acid?

The pH at which a weak acid is 50% ionized and 50% non-ionized.

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What is passive diffusion?

The movement of a substance across a membrane from an area of high concentration to an area of low concentration.

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What is the blood-brain barrier?

The barrier that separates the blood from the brain, protecting the brain from harmful substances.

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What is ionization?

The tendency of a substance to exist in its ionized form. Higher pH favors the ionized form of an acid.

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How does the pKa of a weak acid affect its entry into the brain?

The ability of a weak acid to cross the blood-brain barrier depends on its ionization state. Non-ionized forms of weak acids cross more easily than ionized forms.

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How is the ionization state of a weak acid related to its pH?

At a pH higher than the pKa, a weak acid will be more ionized. At a pH lower than the pKa, a weak acid will be more non-ionized.

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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?

Due to a slightly higher pH in plasma compared to the neuron, a weak acid with a pKa of 9 would have a greater fraction of its ionized form in the plasma than in the 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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Related Documents

Lecture 2 -2 PDF

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.

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