Pharmacokinetics: First-Order and Zero-Order Elimination
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Questions and Answers

What is a characteristic of drugs that demonstrate first-order kinetics?

  • The concentration of the drug in the blood will decrease in a linear fashion over time.
  • The half-life of elimination is constant regardless of the amount of drug in the body. (correct)
  • The elimination mechanisms are saturated at concentrations of clinical interest.
  • The rate of elimination is constant regardless of concentration.
  • What is the term for the rate of elimination that is constant regardless of concentration?

  • Zero-order elimination (correct)
  • Non-linear elimination
  • First-order elimination
  • Linear elimination
  • What is the typical pattern of concentration decrease for drugs that demonstrate zero-order elimination?

  • The concentration decreases in a linear fashion over time. (correct)
  • The concentration decreases by 50% for every half-life.
  • The concentration remains constant over time.
  • The concentration decreases in a logarithmic fashion over time.
  • What is the purpose of a two-compartment model in pharmacokinetics?

    <p>To simulate the behavior of a drug that undergoes an early distribution phase followed by a slower elimination phase.</p> Signup and view all the answers

    What is a characteristic of the elimination phase of a first-order drug when plotted on a logarithmic axis?

    <p>It is a straight line.</p> Signup and view all the answers

    What is the term for the time it takes for the concentration of a drug to decrease by 50%?

    <p>Half-life</p> Signup and view all the answers

    What is the characteristic of drugs with first-order kinetics?

    <p>The rate of elimination is proportional to concentration.</p> Signup and view all the answers

    What is the characteristic of zero-order elimination?

    <p>The rate of elimination is constant and independent of concentration</p> Signup and view all the answers

    What is the initial curvilinear portion of the serum concentration-time curve representing?

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

    What is the primary function of the Food and Drug Administration (FDA) in the United States?

    <p>To regulate the sale and use of drugs.</p> Signup and view all the answers

    How is the elimination half-life typically measured?

    <p>By measuring the time between any two plasma concentration points on the elimination phase that differ by twofold</p> Signup and view all the answers

    What type of elimination is characterized by a constant rate of elimination, regardless of concentration?

    <p>Zero-order elimination</p> Signup and view all the answers

    What is the goal of rational molecular design or screening?

    <p>To find a molecule that selectively alters the function of the target</p> Signup and view all the answers

    What is a prerequisite for a new drug to be approved for regular therapeutic use in humans?

    <p>A series of animal and experimental human studies.</p> Signup and view all the answers

    What is the characteristic of 'me-too' drugs?

    <p>They are the result of simple chemical alteration of the pharmacokinetic properties of the original prototype agent</p> Signup and view all the answers

    What is the purpose of constructing accurate mathematical models in pharmacokinetics?

    <p>To predict the behavior of drugs in the body.</p> Signup and view all the answers

    What is the significance of a drug being distributed to only one compartment?

    <p>It behaves as if it were restricted to the vascular compartment.</p> Signup and view all the answers

    What is the significance of the linear portion of the serum concentration-time curve?

    <p>It represents the elimination phase of the drug</p> Signup and view all the answers

    Study Notes

    Drug Elimination

    • Drugs with first-order elimination have a constant half-life of elimination, regardless of the amount of drug in the body.
    • The concentration of a first-order elimination drug in the blood decreases by 50% for every half-life.
    • Most drugs in clinical use demonstrate first-order kinetics.
    • Zero-order elimination involves a constant rate of elimination, regardless of concentration.
    • Zero-order elimination drugs do not have a constant half-life, and their concentrations in plasma decrease in a linear fashion over time.

    Pharmacokinetic Models

    • A two-compartment model is used to simulate the distribution and elimination phases of a drug.
    • The two compartments consist of the blood and the extravascular tissues.
    • Each phase has a characteristic half-life: 1/2a for the first phase, and 1/2β for the second phase.
    • When concentration is plotted on a logarithmic axis, the elimination phase for a first-order drug is a straight line.

    Distribution Models

    • Some drugs behave as if they were distributed to only 1 compartment (e.g., if they are restricted to the vascular compartment).
    • Others have more complex distributions that require more than 2 compartments for accurate mathematical models.

    Drug Development and Regulation

    • The sale and use of drugs are regulated in almost all countries by governmental agencies, such as the FDA in the United States.
    • New drugs are developed in industrial or academic laboratories, and must undergo a series of animal and experimental human studies (clinical trials) before being approved for therapeutic use.
    • New drugs can emerge from a variety of sources, including the identification of a new target for a disease.

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    Description

    Understand the concepts of first-order and zero-order elimination in pharmacokinetics, including their characteristics and effects on drug concentration in the body.

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