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Review ArticleContinuing Education

Pharmacology, Part 2: Introduction to Pharmacokinetics

Geoffrey M. Currie
Journal of Nuclear Medicine Technology September 2018, 46 (3) 221-230; DOI: https://doi.org/10.2967/jnmt.117.199638
Geoffrey M. Currie
Faculty of Science, Charles Sturt University, Wagga Wagga, New South Wales, Australia, and Regis University, Boston, Massachusetts
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  • FIGURE 1.
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    FIGURE 1.

    Schematic of relationship between pharmacokinetics and pharmacodynamics (1).

  • FIGURE 2.
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    FIGURE 2.

    Schematic of pharmacokinetics and absorption, distribution, metabolism, and excretion concept (A), and same schematic highlighting interplay between free and bound drug, and pathway from site of administration to site of action (B).

  • FIGURE 3.
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    FIGURE 3.

    Schematics of equilibrium between drug concentration and plasma, well-perfused tissue, and poorly perfused tissue. Set of 3 schematics at top does not incorporate effects of metabolism or elimination but illustrate early equilibrium in well-perfused tissue (A) followed by period of concentration in poorly perfused tissues (A to B) before reaching equilibrium in all tissues and plasma (B). Set of 3 schematics at bottom provides phases as discrete intervals (straight line) and illustrates impact of elimination. (Adapted from (3).)

  • FIGURE 4.
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    FIGURE 4.

    Schematic of 1-compartment model, 2-compartment model, and multicompartment model. Elimination rate constant reflects movement from one compartment or volume of distribution to another and can be calculated numerically. Schematically, rate constant may be represented in several ways. In multiple-compartment model, k5 and k6 have arrows of different sizes, indicating greater movement of drug to tissue compartment than from it. Likewise, for k7 and k8, double-head arrow with different sizes of arrowhead is used to represent relative k values. When drug transport between compartments is not reversible, single-head arrow is used (k9). Note that multiple methods would not be used on a single schematic as is done here.

  • FIGURE 5.
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    FIGURE 5.

    Phase I and II metabolism of acetaminophen. Phase I hydroxylation results in toxic metabolite, with 3 forms of phase II metabolism converting metabolite to a form for urine excretion. Toxic interaction can occur, leading to liver necrosis and potential renal failure, especially with deleted hepatic glutathione. (Adapted from (13).)

  • FIGURE 6.
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    FIGURE 6.

    Schematic of first-order and zero-order elimination. First-order elimination follows exponential trend and can be displayed with logarithmic y-axis to generate straight line (inset). Zero-order elimination removes constant amount of drug per unit time.

  • FIGURE 7.
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    FIGURE 7.

    (A) Logarithmic/linear plot confirming single-compartment monoexponential curve (scenario 1). (B) Linear/linear and logarithmic/linear plots demonstrating interplay between absorption and elimination for scenario 2 (scenario 2). (C) Logarithmic/linear plots for raw data (dashed line) and for R (scenario 2). (D) Linear/linear and logarithmic/linear plots demonstrating interplay between absorption and elimination for scenario 3 (scenario 3). (E) Logarithmic/linear plots for raw data (dashed) and for elimination curve minus plasma curve (R) (solid line) (scenario 3).

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    TABLE 1

    Characteristics of Various Routes of Administration of Drugs (2–6)

    RouteAdvantageDisadvantage
    Intranasal (e.g., antihistamine)Rapid delivery and immediate effect. High bioavailability. No first-pass metabolism. Avoids gastric environment.Local irritation. Limited to small doses and small range of drugs.
    Sublingual (e.g., nitroglycerin)Easy and convenient delivery. Rapid delivery and immediate effect. High bioavailability. No first-pass metabolism. Avoids gastric environment. Self-administration.Changes in absorption if swallowed, chewed, or taken after emesis.
    Oral/enteral (e.g., captopril)Easy, reliable, economic, convenient, painless, no infection risk. Self-administration.First-pass metabolism/elimination decreases bioavailability. Slow delivery and onset of action. Dose form needs to accommodate gastric environment (e.g., transit stomach intact for small-bowel absorption). Bioavailability can be influenced by changes in gut status (e.g., emesis, diarrhea, or constipation).
    Rectal (e.g., laxatives)Rapid delivery and immediate effect. High bioavailability. No first-pass metabolism. Avoids gastric environment. Suitable for patients with emesis or otherwise inappropriate oral route.Unpleasant form of administration, with bacteremia risk for immunocompromised patient. Altered absorption in diarrhea and constipation.
    Inhalation (e.g., albuterol)Rapid delivery and immediate effect. High bioavailability. No first-pass metabolism. Avoids gastric environment. Direct delivery to affected tissues. Self-administration.Local irritation. Limited to small doses and small range of drugs. May require special equipment and decreased efficacy with incorrect use.
    Intramuscular (e.g., morphine)Intermediate onset of action. Suitable for oil-based drugs. Easier (less skill) administration than intravenous.Local edema, irritation, or pain. Slower onset of action. Infection risk.
    Intravenous (e.g., furosemide)Rapid delivery and immediate effect. Is 100% bioavailable. No first-pass metabolism. Avoids gastric environment. Controlled drug delivery.Irritation or pain. Risk of infection. Solution must be dissolved well. Risk of embolism. Action not easily reversed. Rapid onset of toxicity.
    Subcutaneous (e.g., insulin)Slower absorption and onset of action. Suitable for oil-based drugs.Local edema, irritation, or pain. Small volumes. Slow onset of action. Infection risk.
    Transdermal (e.g., fentanyl)Easy, reliable, economic, convenient, painless. Enables slow and prolonged drug delivery. No first-pass metabolism. Avoids gastric environment. Self-administration.Slow onset of action. Local skin reactions can occur. Needs highly lipophilic drugs.
    Percutaneous (e.g., diclofenac/diclofenac sodium gel)Easy, reliable, economic, convenient, painless. Suitable for local effect.Slow onset of action. Local skin reactions can occur.
    • View popup
    TABLE 2

    Summary of Useful Formulae and Definitions

    UseEquationDefinition
    Drug concentrationC = C0 e−ktC = drug concentration at time t after C0
    C0 = drug concentration at reference time
    k = elimination rate constant
    t = time between C and C0
    Elimination rate constantk = ln2/T0.5k = elimination rate constant
    ln2 = 0.693
    T0.5 = half clearance time
    Volume of distributionV = amount in body (μg)/actual C0V = volume of distribution
    Actual C0 = concentration at time of administration
    Area under curveAUC0–∞ = FD/VkAUC0–∞ = area under curve (total drug dose) from time 0 to infinity
    F = fraction of drug absorbed
    D = dose
    V = volume of distribution
    k = elimination rate constant
    ClearanceCL = k × VCL = clearance
    k = elimination rate constant
    V = volume of distribution
    Time to maximum concentrationTmax = (1/[ka − k]) ln (ka/k)Tmax = time to maximum concentration
    ka = absorption rate constant
    k = elimination rate constant
    • View popup
    TABLE 3

    Data for First Scenario

    Time (h)Plasma concentration (μg/L)
    2139.0
    465.6
    631.1
    814.6
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    TABLE 4

    Data for Second Scenario

    Time (min)Plasma concentration (U/L)
    00
    131.3
    249.3
    358.6
    462.5
    562.8
    758.1
    1050.6
    1636.1
    2425.3
    • View popup
    TABLE 5

    Use of Data for 7- to 24-Hour Stable Elimination Period to Calculate Elimination Rate Constant and Backproject Elimination Curve by Calculating Earlier Values (Bold) for Elimination Confounded by Absorption

    Time (h)Plasma concentration (U/L)Elimination curve concentrationR (elimination – plasma)
    0081.881.8
    131.377.946.6
    249.374.024.7
    358.670.712.1
    462.567.14.6
    562.864.11.3
    758.158.1
    1050.650.6
    1636.136.1
    2425.325.3
    • View popup
    TABLE 6

    Data for Third Scenario

    Time (h)Plasma concentration (μg/mL)
    00
    0.516.0
    122.0
    1.522.0
    219.0
    411.0
    65.6
    83.2
    • View popup
    TABLE 7

    Use of Data for 2- to 8-Hour Stable Elimination Period to Calculate Elimination Rate Constant and Backproject Elimination Curve by Calculating Earlier Values (Bold) for Elimination Confounded by Absorption

    Time (h)Plasma concentration (μg/mL)Elimination curve concentrationR (elimination – plasma)
    0037.837.8
    0.51632.416.4
    12227.85.8
    1.522
    21919
    41111
    65.65.6
    83.23.2
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Journal of Nuclear Medicine Technology: 46 (3)
Journal of Nuclear Medicine Technology
Vol. 46, Issue 3
September 1, 2018
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Pharmacology, Part 2: Introduction to Pharmacokinetics
Geoffrey M. Currie
Journal of Nuclear Medicine Technology Sep 2018, 46 (3) 221-230; DOI: 10.2967/jnmt.117.199638

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Pharmacology, Part 2: Introduction to Pharmacokinetics
Geoffrey M. Currie
Journal of Nuclear Medicine Technology Sep 2018, 46 (3) 221-230; DOI: 10.2967/jnmt.117.199638
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    • Abstract
    • ABSORPTION
    • DISTRIBUTION
    • METABOLISM
    • ELIMINATION
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