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Pharmacokinetics Overview
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Pharmacokinetics Overview

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Questions and Answers

What characterizes the distribution of a drug that has central and peripheral compartments?

  • Drugs can only move from the central to the peripheral compartment.
  • Equilibrium is established quickly between plasma and tissue.
  • Elimination occurs from the peripheral compartment.
  • Drugs can move to and from the peripheral compartment back to the central compartment. (correct)
  • Which statement accurately describes first order elimination kinetics?

  • The rate of decrease in drug concentration is constant regardless of the amount in the body.
  • A constant fraction of the drug is eliminated at any given time. (correct)
  • A constant amount of drug is eliminated independent of dose.
  • The elimination rate is dependent on the dose administered.
  • In a semi-log plot for first order kinetics, what does the graphical representation look like?

  • An upward sloping line.
  • A straight linear line. (correct)
  • A parabolic curve.
  • A horizontal line.
  • What is true regarding zero order elimination kinetics?

    <p>A constant amount of drug is eliminated independent of the dose.</p> Signup and view all the answers

    What does bioavailability refer to in pharmacokinetics?

    <p>The fraction of unchanged drug reaching systemic circulation.</p> Signup and view all the answers

    What is the bioavailability of drugs administered intravenously?

    <p>1</p> Signup and view all the answers

    In a first order elimination process, which equation best describes the relationship between drug concentration and time?

    <p>C = (dose/Vd) e-kt</p> Signup and view all the answers

    What does the term 'bioavailability' in pharmacokinetics refer to?

    <p>The rate and extent to which the active ingredient or active moiety is absorbed and becomes available at the site of action.</p> Signup and view all the answers

    In a one-compartment model, what happens to the plasma concentration of a drug when it follows first-order kinetics?

    <p>The plasma concentration decreases exponentially.</p> Signup and view all the answers

    How is the elimination rate constant related to the half-life of a drug?

    <p>The half-life is inversely proportional to the elimination rate constant.</p> Signup and view all the answers

    What is a key characteristic of a two-compartment model?

    <p>Drug distribution occurs rapidly followed by a slower elimination phase.</p> Signup and view all the answers

    What is the primary principle of pharmacokinetics regarding drug effects?

    <p>The effect of a drug is related to the blood concentration of the drug.</p> Signup and view all the answers

    What is the purpose of administering a drug by IV and another route for comparison?

    <p>To measure plasma concentrations over time</p> Signup and view all the answers

    How is bioavailability generally expressed mathematically?

    <p>AUC oral / AUC iv</p> Signup and view all the answers

    What is the percent of a drug remaining in the body after three half-lives?

    <p>12.5%</p> Signup and view all the answers

    What does bioavailability indicate when a drug is administered orally?

    <p>The extent of absorption and/or first pass effect</p> Signup and view all the answers

    What does the half-life of a drug represent?

    <p>The time for a 50% decrease in plasma drug concentration</p> Signup and view all the answers

    Which of the following describes the volume of distribution (Vd) of a drug?

    <p>It reflects the apparent volume a drug would occupy in body fluids at equilibrium.</p> Signup and view all the answers

    After four half-lives, what fraction of the drug remains in the body?

    <p>0.06</p> Signup and view all the answers

    What formula is used to calculate the half-life of a drug in a one compartment model?

    <p>t1/2 = 0.693 / ke</p> Signup and view all the answers

    Which statement is true regarding drugs with high volume of distribution?

    <p>They indicate a drug is highly lipophilic or has low protein binding.</p> Signup and view all the answers

    What is a characteristic of half-life when determined graphically?

    <p>It can be illustrated using a semi-log plot</p> Signup and view all the answers

    What is the formula used to calculate the fraction of a drug eliminated from the body?

    <p>Fraction eliminated = 1 - 1/(2n)</p> Signup and view all the answers

    In the equation Ct = C0 e(-kxt), what does Ct represent?

    <p>Plasma concentration at time t</p> Signup and view all the answers

    Why is bioavailability important in pharmacology?

    <p>It allows for comparisons of different products with the same active ingredients</p> Signup and view all the answers

    What does the area under the curve (AUC) indicate in pharmacokinetics?

    <p>The extent of the drug's absorption into the bloodstream</p> Signup and view all the answers

    What factor may influence the bioavailability of a drug when it is administered orally?

    <p>Influence of food or other drugs</p> Signup and view all the answers

    Study Notes

    Pharmacokinetics Overview

    • Pharmacokinetics quantifies relationships among absorption, distribution, and elimination of drugs over time.
    • Blood concentration of a drug is directly related to its therapeutic effect, influencing efficacy and safety.

    Key Pharmacokinetic Parameters

    • Bioavailability (F): Fraction of unchanged drug reaching systemic circulation post-administration; intravenous (IV) drugs have F = 1, others < 1.
    • Half-Life (t1/2): Time required for plasma drug concentration to decrease by 50%; determined using ke (elimination rate constant).
    • Clearance (CL): Volume of plasma cleared of drug per unit time; inversely related to steady-state concentration.
    • Volume of Distribution (Vd): Apparent volume in which drug distributes; large Vd indicates high lipophilicity or low protein binding.
    • Elimination Rate Constant (ke): Rate at which drug concentration decreases over time; key in predicting drug clearance.
    • Steady State Concentration (Css): Stable level of drug in the body during continuous administration; reached after 4-5 half-lives.

    Compartment Models

    • One-Compartment Model: Assumes rapid equilibrium between plasma and tissues; characterized by linear decline in plasma concentration in semi-log plots.
    • Two-Compartment Model: Drug distributes between a central and a peripheral compartment; displays a biphasic decline in plasma concentration.

    Kinetics

    • First Order Kinetics: Rate of drug elimination is proportional to its concentration; results in a linear semi-log plot.
    • Zero Order Kinetics: Constant amount of drug eliminated regardless of concentration; occurs when elimination pathways are saturated.

    Relationship Between Parameters

    • Clearance, half-life, volume of distribution, and plasma concentration are interrelated, affecting drug dosing and frequency.
    • Decreases in clearance will double Css if dosing rate remains constant.

    Calculating Pharmacokinetic Parameters

    • Formulas:
      • Half-Life: t1/2 = 0.693 / ke
      • Clearance: CL = Dose / Css
      • Bioavailability: F = AUC (oral) / AUC (IV)
    • Volume of Distribution calculation: Vd = Dose / (Css x ke).

    Practical Applications

    • Administer IV loading doses considering volume of distribution to achieve desired Css levels quickly.
    • Importance of bioavailability assessment for effective drug formulation comparison and understanding absorption variability.

    Additional Information

    • Four half-lives rule: After 4 half-lives, a drug is considered essentially eliminated, retaining only 6% in the body.
    • Knowledge of pharmacokinetics is crucial for appropriate drug therapy management, individualization of dose regimens, and optimization of therapeutic outcomes.

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    Related Documents

    HO pharmacokinetics 9-9-24.pdf

    Description

    This quiz covers the key concepts and parameters in pharmacokinetics, including bioavailability, half-life, clearance, and volume of distribution. Understanding these parameters is essential for evaluating drug efficacy and safety. Test your knowledge of how drugs are absorbed, distributed, and eliminated from the body.

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