Pharmacodynamics

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Questions and Answers

What does potency measure in pharmacology?

  • Amount of drug necessary to produce an effect (correct)
  • Receptor sensitivity to the drug
  • Maximum effect of the drug
  • Rate of absorption of the drug

How is potency often determined in pharmacology?

  • By assessing the maximum pharmacologic effect
  • By analyzing drug concentration at the receptor site
  • By calculating the EC50 value (correct)
  • Using the rate of metabolism of the drug

In pharmacology, what does the EC50 value represent?

  • Rate of absorption of the drug
  • Drug concentration at which all receptors are occupied
  • Amount of drug needed to achieve 50% of the maximum effect (correct)
  • Maximum effect of the drug

What information do graded dose-response curves provide in pharmacology?

<p>Potency and efficacy of the drug (C)</p> Signup and view all the answers

What is the main consequence of autophosphorylation of the receptor when insulin binds to its subunits?

<p>Activation of other important cellular signals (D)</p> Signup and view all the answers

How does the mechanism of Enzyme-linked Receptors differ from G protein–coupled receptors?

<p>They involve autophosphorylation of the receptor (C)</p> Signup and view all the answers

What is a key requirement for ligands to interact with Intracellular Receptors?

<p>Sufficient lipid solubility (B)</p> Signup and view all the answers

What happens after the activated ligand–receptor complex dimerizes in Intracellular Receptors?

<p>It binds to transcription factors in the cell nucleus (A)</p> Signup and view all the answers

What is pharmacodynamics?

<p>The study of drug actions on the body and how drug concentrations affect responses (C)</p> Signup and view all the answers

What happens when a drug binds to a receptor and activates it?

<p>It initiates a series of reactions that lead to a specific response (D)</p> Signup and view all the answers

What role do receptors play in signal transduction?

<p>They act as signal detectors (C)</p> Signup and view all the answers

How do cells respond to different types of agonists based on receptors?

<p>By producing a unique response specific to each type of agonist (B)</p> Signup and view all the answers

What is the fundamental difference between competitive and noncompetitive antagonists?

<p>Competitive antagonists reduce agonist potency, while noncompetitive antagonists reduce agonist efficacy. (D)</p> Signup and view all the answers

What effect does an allosteric antagonist have on the Emax and EC50 values of an agonist?

<p>It causes a downward shift in Emax with no change in EC50. (B)</p> Signup and view all the answers

What is an example of an allosteric antagonist mentioned in the text?

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

In what way does epinephrine counteract histamine-induced bronchoconstriction?

<p>By acting as an agonist at B2-adrenoceptors and causing bronchial smooth muscle relaxation. (B)</p> Signup and view all the answers

Which characteristic is considered more clinically useful than potency in pharmacology?

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

What determines a drug's ability to fully or partially activate receptors?

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

Which term refers to drugs that produce a maximal biologic response similar to the endogenous ligand?

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

What is the intrinsic activity value of full agonists?

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

What does potency refer to in pharmacology?

<p>The amount of drug needed to produce an effect (C)</p> Signup and view all the answers

How can potency be determined in pharmacology?

<p>By calculating the concentration of drug producing 50% of the maximum effect (D)</p> Signup and view all the answers

What characteristic can be determined by plotting graded dose-response curves?

<p>Potency and efficacy of the drug (C)</p> Signup and view all the answers

In pharmacology, what does EC50 represent?

<p>The concentration of drug producing 50% of the maximum effect (B)</p> Signup and view all the answers

What is a distinguishing feature of allosteric antagonists compared to competitive antagonists?

<p>They reduce agonist efficacy (A)</p> Signup and view all the answers

How does an allosteric antagonist impact the Emax and EC50 values of an agonist?

<p>Decreases Emax, no change in EC50 (D)</p> Signup and view all the answers

Which receptor does epinephrine act on to counteract histamine-induced bronchoconstriction?

<p>B2-adrenoceptors (B)</p> Signup and view all the answers

How does a noncompetitive antagonist differ from an allosteric antagonist in receptor binding?

<p>Noncompetitive antagonists have higher affinity for the agonist-binding site (B)</p> Signup and view all the answers

What is the main effect of a decrease in the diameter of an arteriole on blood flow and pressure?

<p>Increase in resistance and increase in blood pressure (B)</p> Signup and view all the answers

How do the dose–response curves of full agonists compare for receptor binding and biological responses?

<p>They are parallel (C)</p> Signup and view all the answers

What happens to the Emax of a receptor saturated with an agonist in the presence of increasing concentrations of a partial agonist?

<p>Emax decreases until it reaches the Emax of the partial agonist (A)</p> Signup and view all the answers

What role can a partial agonist play when exposed to a full agonist at the same receptor?

<p>It acts as an antagonist to the full agonist (C)</p> Signup and view all the answers

An agonist binds to a site on a receptor protein and deactivates it, resulting in a specific intracellular response.

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

Cells contain muscarinic receptors that bind and respond to epinephrine or norepinephrine.

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

Second messenger molecules are not involved in translating agonist binding into a cellular response.

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

Pharmacodynamics describes the actions of a drug on the body but not the influence of drug concentrations on the magnitude of the response.

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

Ligand-gated ion channels can be regulated by voltage-gated ion channels.

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

Stimulation of the nicotinic receptor by acetylcholine leads to potassium influx and sodium outflux.

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

Partial agonists can have a greater effect than full agonists when exposed to the same receptor.

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

G protein–coupled receptors do not recognize chemical signals that affect adenylyl cyclase activity.

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

Receptors may be internalized within the cell, making them unavailable for further _____ interaction.

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

During the recovery phase, unresponsive receptors are referred to as 'responsive'.

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

Repeated exposure of a receptor to an antagonist results in down-regulation of receptors.

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

Agonist drugs mimic the action of the endogenous ligand for the receptor.

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

A drug with a lower EC50 value is considered more potent than a drug with a higher EC60 value.

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

Efficacy of a drug is solely dependent on the number of drug receptor complexes formed.

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

Partial agonists can reach the same maximal response as full agonists even when occupying 100% of the receptors.

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

Maximal efficacy (Emax) occurs when the drug occupies all receptors, leading to no increase in response with higher drug concentrations.

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

What is the main consequence of autophosphorylation of the receptor when insulin binds to its subunits?

<p>Phosphorylation of other peptides or proteins (B)</p> Signup and view all the answers

What is the primary target of ligand-receptor complexes in Intracellular Receptors?

<p>Transcription factors in the cell nucleus (C)</p> Signup and view all the answers

What does the activated ligand-receptor complex typically do after translocating to the nucleus in Intracellular Receptors?

<p>Dimerizes before binding to transcription factors (A)</p> Signup and view all the answers

How does the mechanism of Enzyme-linked Receptors differ from G protein-coupled receptors?

<p>Enzyme-linked receptors phosphorylate other peptides or proteins upon activation, while G protein-coupled receptors directly activate transcription factors (C)</p> Signup and view all the answers

What determines the magnitude of a drug effect according to the text?

<p>Receptor sensitivity and drug concentration at the receptor site (D)</p> Signup and view all the answers

How is potency defined in pharmacology based on the text?

<p>Amount of drug required to produce an effect (A)</p> Signup and view all the answers

What does the EC50 for Drugs A and B indicate according to the text?

<p>Drug A is more potent than Drug B (A)</p> Signup and view all the answers

Which characteristic can be determined by plotting graded dose-response curves as mentioned in the text?

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

What distinguishes allosteric antagonists from competitive antagonists?

<p>Allosteric antagonists bind to a site other than the agonist-binding site, causing a downward shift in Emax. (A)</p> Signup and view all the answers

How does functional antagonism typically work?

<p>Functional antagonists bind to a separate receptor and initiate effects opposite those of the agonist. (C)</p> Signup and view all the answers

What is the specific effect of epinephrine on bronchial smooth muscle in response to histamine-induced bronchoconstriction?

<p>Epinephrine counteracts histamine-induced bronchoconstriction by causing relaxation of the muscles. (C)</p> Signup and view all the answers

Which drug mentioned in the text illustrates allosteric antagonism at GABA-controlled chloride channels?

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

Which of the following best describes drugs with low therapeutic indices?

<p>They have a small range of effective doses and a non-overlapping range of toxic doses. (B)</p> Signup and view all the answers

In the context of quantal dose-response curves, what is the significance of a two- to threefold increase in the international normalized ratio (INR) for warfarin?

<p>It indicates a desirable response to the drug. (B)</p> Signup and view all the answers

Why are some drugs with low therapeutic indices still used to treat serious diseases?

<p>The risk of adverse effects outweighs the risk of leaving the disease untreated. (D)</p> Signup and view all the answers

What effect does bioavailability have on drugs with low therapeutic indices?

<p>It is not critical for these drugs' therapeutic effects. (B)</p> Signup and view all the answers

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