Pharmacokinetics and Drug Design (PC 710)
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Questions and Answers

What does the 'A' in the ADME acronym stand for?

  • Adjuvant
  • Allocation
  • Absorption (correct)
  • Attenuation

    • Which of the following processes occurs after absorption in the ADME sequence?

  • Excretion
  • Metabolism (correct)
  • Synthesis
  • Activation

    • In the context of drug disposition, what does the term 'distribution' refer to?

  • The initial uptake of drugs
  • The conversion of drugs into metabolites
  • The movement of drugs throughout the body (correct)
  • The elimination of drugs from the body

    • Which step in the ADME process primarily involves the liver's processing of substances?

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

    Which component of ADME is most directly concerned with how drugs leave the body?

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

    What is the primary focus of the lecture on Drug Design (PC 710)?

    <p>Effects of physicochemical properties on pharmacokinetics</p> Signup and view all the answers

    Which factors are likely to affect the pharmacokinetic profile of a drug?

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

    Which aspect is most directly impacted by the physicochemical properties of a drug?

    <p>Absorption, distribution, metabolism, and excretion</p> Signup and view all the answers

    Which of the following is NOT a classical physicochemical property considered in drug design?

    <p>Brand loyalty</p> Signup and view all the answers

    How do physicochemical properties influence drug solubility?

    <p>They determine the lipid-water partitioning of the drug.</p> Signup and view all the answers

    What is the maximum molecular mass for a compound to meet the specified criteria?

    <p>500</p> Signup and view all the answers

    What is the highest allowable value for log P in the criteria given?

    <p>5</p> Signup and view all the answers

    How many hydrogen bond donors can a compound have at maximum according to the criteria?

    <p>5</p> Signup and view all the answers

    Which of the following statements about the criteria is correct?

    <p>No more than 5 hydrogen bond donors are permitted.</p> Signup and view all the answers

    Which characteristic does NOT adhere to the given criteria for a compound?

    <p>Hydrogen bond donors totaling 6</p> Signup and view all the answers

    What is essential for a drug to effectively bind to its receptor?

    <p>Specific physiochemical properties</p> Signup and view all the answers

    Which physiochemical property is least likely to affect a drug's biological activity?

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

    How does the solubility of a drug influence its action?

    <p>It affects its distribution in the body</p> Signup and view all the answers

    If a drug exhibits high ionization at physiological pH, what is the likely consequence?

    <p>Decreased ability to bind to receptors</p> Signup and view all the answers

    What role does molecular weight play in drug design?

    <p>It helps determine the route of administration</p> Signup and view all the answers

    What is the primary mechanism of passive diffusion?

    <p>Movement along the concentration gradient</p> Signup and view all the answers

    Which statement best describes active transport?

    <p>It requires energy to move substances against the concentration gradient.</p> Signup and view all the answers

    In passive diffusion, how does the concentration gradient affect drug movement?

    <p>Drugs move from high to low concentration.</p> Signup and view all the answers

    What is necessary for active transport to occur?

    <p>Energy input from ATP or another source.</p> Signup and view all the answers

    Which of the following is NOT true regarding passive diffusion?

    <p>It requires energy to occur.</p> Signup and view all the answers

    What does absorption involve in the context of drug administration?

    <p>Transportation of molecules across cell membranes</p> Signup and view all the answers

    Which type of injection involves depositing a drug directly into the skin layers?

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

    Which of the following best describes an intraperitoneal injection?

    <p>Injection into the peritoneal cavity</p> Signup and view all the answers

    What is a common purpose of drug absorption in the body?

    <p>To facilitate the therapeutic effects of a drug</p> Signup and view all the answers

    Which statement accurately describes the absorption process?

    <p>It requires the drug to be in a solution form.</p> Signup and view all the answers

    Study Notes

    Drug Design (PC 710) Lecture

    • The lecture covered the effect of physicochemical properties on the pharmacokinetic profile of drugs.
    • Physicochemical properties are crucial for a drug to bind to its receptor and exert its biological activity.
    • These properties influence how a drug reaches its site of action, its affinity to the target, and overall activity.
    • Factors affecting drug structure and physicochemical properties include pKa, solubility, polarity, and steric factors (bulkiness).
    • Lipinski's rule of five determines the likelihood of a drug being orally bioavailable. This includes:
      • Molecular mass less than 500
      • Log P not greater than 5
      • No more than 5 hydrogen bond donors
      • No more than 10 hydrogen bond acceptors
      • 10 or fewer rotatable bonds
      • Polar surface area (PSA) not greater than 140 Å2
    • In-silico prediction tools (SwissADME.com and Molinspiron.com) are available to predict oral bioavailability and pharmacokinetic parameters.
    • Physicochemical properties affect the drug's absorption, distribution, metabolism, and excretion (ADME).
    • Absorption is the transportation of molecules across cell membranes (Passive, active, convective).
      • Examples of absorption factors include the dissolution/solubility rate, dissociation constant (pKa), and partition coefficient (Log P).
      • Particle size and pH of the medium affect the solubility of drugs.
        • Smaller particle size leads to increased surface area and faster solubility.
        • pH affects the ionization of acids or bases impacting their absorption.
    • Distribution involves the drug traveling to the target organ.
      • Plasma protein binding can act as a storage site, preventing drug activity.
      • Neutral fats and adipose tissue can also store drugs.
      • Factors influencing deposition in adipose tissue include partition coefficient (Log P).
    • Metabolism: The lecture emphasized referring to a separate metabolism lecture for further details on phases I and II.
    • Excretion: The process of removing metabolic waste products from the body, occurs in the lungs, liver, kidneys, and skin.

    Drug Absorption Factors

    • Dissolution/Solubility Rate: crucial step; the rate at which the drug dissolves in the gastrointestinal (GI) fluids.
    • Dissociation Constant (pKa): affects the ionization state of a drug (acids/bases) and its absorption based on the pH of the GI tract.
    • Partition Coefficient (Log P): measures a drug's lipophilicity (lipid-water solubility). A higher log P value indicates better absorption.
      • Higher Log P values indicate increased lipid solubility, promoting absorption
    • Example: Spironolactone and Griseofulvin are formulated as micronized capsules to improve their bioavailability, thereby impacting these properties

    Absorption: pKa

    • For weak acids: pKa = pH + log [unionized acid / ionized acid].
    • For weak bases: pKa = pH + log [unionized base / ionized base].
    • Drugs are more easily absorbed in their unionized state. This state depends on the pH of the absorption site.
      • Drugs are better absorbed in their unionized forms in areas where their pKa is higher than the pH.
      • Drugs are better absorbed in their ionized forms in areas where their pKa is lower than the pH.

    Absorption: Log P

    • log P = log ([organic phase concentration] / [aqueous phase concentration])
    • A higher log P value indicates better lipid solubility and better absorption.

    Modifying Drug Properties to Improve Absorption

    • Changing a drug's lipophilicity or introducing hydrophobic groups can improve its absorption.
    • Hydrophobicity constants (π) are available in tables for modifying drugs.

    Distribution to Target Organ

    • Discusses factors impacting a drug's distribution to the target organ, including plasma protein binding, neutral fat deposition in adipose tissue.

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    Drug Design (PC 710) Lecture Notes PDF

    Description

    Test your knowledge on pharmacokinetics and key concepts in drug design with this quiz. Topics include the ADME process, factors affecting pharmacokinetics, and physicochemical properties of drugs. Ideal for students studying pharmacology or related fields.

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