MPP lecture 2
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MPP lecture 2

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Questions and Answers

What type of antagonist affects a drug's efficacy by reducing it?

  • Inverse agonist
  • Noncompetitive antagonist (correct)
  • Partial agonist
  • Competitive antagonist
  • Which pharmacokinetic property describes the process of removing a drug from the body?

  • Metabolism
  • Elimination (correct)
  • Distribution
  • Absorption
  • What must happen to drug concentration for drugs to maintain the same effect in the presence of an antagonist?

  • Vary unpredictably
  • Increase (correct)
  • Stay the same
  • Decrease
  • Which term describes what the drug does to the body?

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

    Agonists interact with receptors to:

    <p>Bind and cause conformational change</p> Signup and view all the answers

    What is the significance of 'affinity' regarding drug-receptor interactions?

    <p>It describes the likelihood of the drug binding to its receptor.</p> Signup and view all the answers

    Which type of drug binds and inactivates active targets?

    <p>Inverse agonist</p> Signup and view all the answers

    What types of changes do drug-receptor interactions typically cause?

    <p>Biochemical and physiological changes</p> Signup and view all the answers

    What type of chemical interactions allow for drug-receptor binding?

    <p>Van der Waals forces and covalent bonding</p> Signup and view all the answers

    Which describes drugs in the context of pharmacology?

    <p>Molecules that interact with specific components of an organism</p> Signup and view all the answers

    What is the primary function of P-glycoprotein in the context of drug transport?

    <p>It actively pumps drugs out of the cell into the bloodstream.</p> Signup and view all the answers

    What is the primary purpose of the lock and key theory in drug-receptor binding?

    <p>It explains the specific interaction between a drug and its receptor.</p> Signup and view all the answers

    Which of the following is NOT a factor influencing the distribution of a drug from plasma to the interstitum?

    <p>Tissue metabolism</p> Signup and view all the answers

    Which pharmacokinetic property is specifically responsible for the entry of a drug into circulation?

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

    Enteric-coated drugs primarily serve what purpose?

    <p>To protect the drug from degradation by stomach acid.</p> Signup and view all the answers

    What does bioavailability measure regarding a drug?

    <p>The degree and rate at which a drug reaches systemic circulation.</p> Signup and view all the answers

    Which route of drug administration has the highest bioavailability?

    <p>Intravenous injection</p> Signup and view all the answers

    First-pass metabolism primarily occurs in which organ?

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

    In which category of drug absorption is sublingual administration classified?

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

    Which of the following mechanisms of absorption involves the active transport of substances into cells?

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

    What distinguishes extended-release oral preparations from other forms?

    <p>They allow for slower absorption and longer duration of action.</p> Signup and view all the answers

    In the context of drug absorption, what is the role of blood flow?

    <p>It affects the rate at which a drug enters systemic circulation.</p> Signup and view all the answers

    Which of the following routes provides rapid absorption while avoiding first-pass metabolism?

    <p>Nasal inhalation</p> Signup and view all the answers

    Drugs with high first-pass metabolism require which of the following regarding dosing?

    <p>Higher doses to increase bioavailability.</p> Signup and view all the answers

    Which area of high P-glycoprotein expression would limit drug absorption?

    <p>Epithelial tissues of the intestine</p> Signup and view all the answers

    What two barriers are primarily presented by the human body for drug absorption?

    <p>Integument and mucous membranes</p> Signup and view all the answers

    Which drug administration route is characterized by its ability to provide rapid onset and maximum control?

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

    What role do cardiac output and local blood flow play in drug distribution?

    <p>They affect drug absorption into tissues.</p> Signup and view all the answers

    Which factor does NOT influence drug absorption?

    <p>Molecular weight of the drug</p> Signup and view all the answers

    Which of the following statements about drug distribution is true?

    <p>It involves reversible dispersion between the vascular and extravascular spaces.</p> Signup and view all the answers

    Study Notes

    Pharmacology Basics

    • Pharmacology studies drug-receptor interactions and the body's effects on drug movement, known as pharmacokinetics.
    • Drugs interact with macromolecular receptors, leading to biochemical and physiological changes.
    • Pharmacodynamics explores what drugs do to the body, while pharmacokinetics examines what the body does to drugs.

    Drug-Receptor Interactions

    • Antagonists: Inhibit target activation or inactivation.
    • Competitive Antagonists: Bind to the same site as the agonist, reducing drug potency.
    • Noncompetitive Antagonists: Bind to alternative sites, affecting drug efficacy.
    • Inverse Agonists: Bind and deactivate active targets.
    • Partial Agonists: Activate targets partially without full activation.
    • Full Agonists: Fully activate their targets.
    • Effects of drug binding lead to receptor conformational changes that enhance binding and modify activity.

    Pharmacokinetics

    • Absorption, Distribution, Metabolism, and Elimination (ADME) are the four key properties of pharmacokinetics affecting onset, intensity, and duration of drug action.
    • Increased drug concentration may be necessary to achieve the same effects in the presence of antagonists.
    • Bioavailability reflects the rate and extent to which a drug reaches systemic circulation, critical for dosages in non-intravenous administration.
    • First-Pass Metabolism: Drug metabolism by the liver or GI tract before entering systemic circulation, influencing bioavailability.
    • Drug absorption mechanisms include passive diffusion, facilitated diffusion, active transport, and endocytosis.

    Factors Influencing Drug Absorption

    • Obstacles: Integument and mucous membranes hinder drug absorption.
    • Influencing factors: Blood flow, surface area, contact time, and P-glycoprotein expression impact absorption.
    • P-glycoprotein, a transmembrane transporter, pumps drugs out of cells, limiting absorption in high-expressing areas.

    Distribution

    • After leaving the bloodstream, drugs enter interstitial spaces and tissues.
    • Drug distribution is affected by cardiac output, local blood flow, capillary permeability, tissue volume, and the degree of drug binding to plasma and tissue proteins.

    Routes of Drug Administration

    • Enteral:
      • Oral: Complex, affected by gastric pH; examples include enteric-coated (protect from stomach acid) and extended-release (slower absorption).
      • Sublingual: Directly enters bloodstream, bypassing stomach acid.
    • Parenteral: Direct systemic circulation; highest bioavailability, especially via intravenous administration.
      • IV: Rapid effect and maximum control.
      • IM: Variable absorption; e.g., epipens.
      • SC: Slow absorption via diffusion; e.g., insulin.
    • Other:
      • Inhalation: Rapid absorption, avoids first-pass metabolism.
      • Intrathecal/Intraventricular: Bypasses the blood-brain barrier directly into CSF.
      • Transdermal: Varying absorption rates; e.g., nicotine patches.
      • Rectal: Useful for patients who cannot take oral medications (vomiting).

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    Description

    Explore the essential concepts of pharmacology related to drug-receptor interactions, including the definitions and roles of antagonists, competitive antagonists, and noncompetitive antagonists. This quiz will test your understanding of how these interactions influence drug potency and efficacy.

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