Stereo-chemical Aspects of Drugs
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Questions and Answers

What is determined by steric factors in the drug-receptor complex?

  • The distribution of drug in the bloodstream
  • The formation and stability of the complex (correct)
  • The solubility of the drug in water
  • The metabolic rate of the drug

    • Which factor is NOT mentioned as important in drug-receptor interaction?

  • Pharmacokinetic properties of the drug (correct)
  • Conformations of drug and receptor
  • Electronic charge distribution
  • Specificity of the drug to the receptor

    • How can the formation and stability of a drug-receptor complex be altered?

  • By increasing the temperature of the environment
  • Through physical alterations such as molecular size substitution (correct)
  • By changing the pH of the solution
  • By limiting the exposure time of the drug

    • What does 'complementarity' in drug-receptor interactions refer to?

    <p>The rigid structure of receptors allowing for specific binding</p> Signup and view all the answers

    What primarily contributes to the activity of a drug in relation to its receptor?

    <p>The spatial arrangement of common moieties in the drug</p> Signup and view all the answers

    What is the maximum distance between two peptide bonds when a protein is extended?

    <p>3.61 Å</p> Signup and view all the answers

    What is the term for the distance between two consecutive turns in a protein structure?

    <p>Identity distance</p> Signup and view all the answers

    Which type of bonding is primarily responsible for the binding between a neurotransmitter and a receptor?

    <p>Ionic bonding</p> Signup and view all the answers

    Why must the bonding forces between a neurotransmitter and a receptor not be too strong?

    <p>To ensure the messenger can detach</p> Signup and view all the answers

    In the structural context of hormones, what is the configuration of Diethylstilbestrol?

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

    Which type of bonding is not typically associated with receptor and neurotransmitter interactions?

    <p>Covalent bonding</p> Signup and view all the answers

    What is the primary purpose of bonding forces in neurotransmitter-receptor interactions?

    <p>To change receptor shape and allow messenger release</p> Signup and view all the answers

    What is a characteristic distance for the identity distance in peptides?

    <p>3.61 Å</p> Signup and view all the answers

    What is the primary difference between structurally nonspecific drugs and structurally specific drugs?

    <p>Structurally specific drugs depend on their 3-D structure for biological action.</p> Signup and view all the answers

    Which phase in drug action pertains to the route of administration?

    <p>Pharmaceutical phase</p> Signup and view all the answers

    What do the pharmacokinetic phase and the pharmaceutical phase have in common?

    <p>Both phases describe what the body does to the drug.</p> Signup and view all the answers

    In what context is biopharmaceutics relevant?

    <p>It includes the development and use of delivery systems.</p> Signup and view all the answers

    Which drug delivery concept focuses on the adjustment of dosage based on individual patient needs?

    <p>Dose adjustment</p> Signup and view all the answers

    What is the primary focus of biostatistical analysis in the context of pharmaceuticals?

    <p>Assessing drug effects in clinical trials.</p> Signup and view all the answers

    Which aspect does pharmacokinetics not directly examine?

    <p>Chemical structure of the drug</p> Signup and view all the answers

    Designing agonists and antagonists primarily involves what concept in drug development?

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

    What is one requirement for a drug molecule to effectively interact with a receptor?

    <p>The drug must have the correct binding groups.</p> Signup and view all the answers

    Which of the following must be considered regarding the positioning of binding groups in drug design?

    <p>The binding groups must be correctly positioned.</p> Signup and view all the answers

    What size must the drug molecule be in relation to the binding site?

    <p>The drug must be the right size for the binding site.</p> Signup and view all the answers

    What can be expected from a drug structure that lacks one or more required binding groups?

    <p>The drug may have poor activity.</p> Signup and view all the answers

    Which of the following describes an antagonist in drug design?

    <p>An antagonist binds to a receptor but does not activate it.</p> Signup and view all the answers

    In designing a drug, what is the significance of the term ‘binding groups’?

    <p>Binding groups are responsible for drug-receptor interactions.</p> Signup and view all the answers

    Which factor does NOT impact the activity of a drug in relation to its receptor?

    <p>The aesthetic appeal of the drug.</p> Signup and view all the answers

    What is a likely outcome when a drug is not the right size for the binding site?

    <p>The drug will not properly fit and may fail to bind.</p> Signup and view all the answers

    Why is it important for binding groups to interact positively with target receptor binding sites?

    <p>It ensures the drug activates the receptor effectively.</p> Signup and view all the answers

    A drug molecule that is incorrectly designed may suffer from what consequence in terms of receptor interaction?

    <p>Reduced reactivity with the intended receptor.</p> Signup and view all the answers

    What is meant by competitive antagonism?

    <p>Antagonists that act at the binding site of the receptor</p> Signup and view all the answers

    Which statement accurately describes non-competitive antagonism?

    <p>It involves antagonists binding at a different site than the neurotransmitter.</p> Signup and view all the answers

    What is an allosteric antagonist?

    <p>An antagonist that modifies the receptor's activity without directly blocking the binding site</p> Signup and view all the answers

    What does the umbrella effect refer to in the context of antagonism?

    <p>The broad inhibition of receptor activity by binding at alternative sites</p> Signup and view all the answers

    How may some antagonists exert their effect despite lacking structural similarity to the neurotransmitter?

    <p>By altering the receptor conformation at a distant site</p> Signup and view all the answers

    Which of the following best describes the role of competitive antagonists?

    <p>They bind to the binding site but do not activate the receptor.</p> Signup and view all the answers

    Why might certain antagonists bind to entirely different parts of the receptor?

    <p>To prevent receptor activation through non-competitive mechanisms</p> Signup and view all the answers

    What is a key characteristic of antagonists that cannot fit the geometrical requirements of the binding site?

    <p>They inhibit receptor activity effectively.</p> Signup and view all the answers

    Study Notes

    Stereo-chemical Aspects of Drugs

    • The activity of a drug depends on a sequence of physicochemical events that begin when an active molecule penetrates a living organism.
    • Three characteristic phases govern the biological activity of a drug in a living organism:
      • The pharmaceutical phase: Route of administration (I.V. injection, oral, etc.)
      • The Pharmacokinetic phase: What the Body Does to a Drug?
      • Pharmacodynamic phase: What a Drug Does to the Body?
    • Receptor sites have a specific and relatively rigid structure.
    • Receptor binding is determined by steric factors, and medicinal action depends on the nature of the drug-receptor complex.
    • Complementarity between drug and receptor leads to specificity and activity.
    • Changes in the drug's spatial structure, such as substituting a large group with a small one, can strongly alter the formation and stability of the drug-receptor complex.
    • In drug-receptor interactions, two values are crucial:
      • Electronic charge distribution in the drug and receptor.
      • Conformations of the drug and receptor.
    • The distance between two peptide bonds, known as the identity distance, is approximately 3.61 Å.
    • Binding between a neurotransmitter or drug and a receptor can occur through:
      • Ionic bonding
      • Hydrogen bonding
      • Van der Waals interactions
    • The bonding forces should be strong enough to change the receptor's shape but not so strong that the neurotransmitter cannot leave.

    Design of Agonists

    • Agonist design involves considering the following requirements:
      • The drug must possess the correct binding groups.
      • The binding groups must be correctly positioned.
      • The drug must be the right size for the binding site.

    Design of Antagonists

    • Antagonists can act in two ways:
      • Competitive antagonism: Antagonists compete with the agonist for the same binding site.
      • Non-competitive antagonism: Antagonists act outside the binding site, often affecting the receptor's conformation or stability.
    • Allosteric antagonism: Antagonists bind to a site different from the agonist binding site, affecting the receptor's affinity for the agonist and altering its activity.
    • Antagonism by umbrella effect: The antagonist blocks the binding of the agonist by physically hindering access.
    • Many antagonists do not structurally resemble the native neurotransmitter.
    • Antagonists can bind to a different part of the receptor and disrupt its function.

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    Drug Design Lecture (2023/2024) - PC 710 - SINAI UNIVERSITY

    Description

    Explore the stereo-chemical characteristics that influence drug activity in living organisms. This quiz examines the three phases of drug action: pharmaceutical, pharmacokinetic, and pharmacodynamic phases. Additionally, it highlights the importance of receptor binding and the effects of molecular structure on drug efficacy.

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