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    ch4 8

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    Wafa S
    This document discusses several key concepts relating to drug distribution and elimination in the body. It explains that distribution extent, rate, and volume impact how quickly a drug reaches its site of action and how long it remains in the body. Drug binding, tissue permeability, blood flow, and patient factors like age, obesity, or disease can influence these distribution properties. The document also covers drug elimination rates and clearance, noting how metabolism, plasma binding, and organ function affect the speed a drug is removed from the body and its resulting pharmacokinetics. Concepts like volume of distribution, half-life, and clearance are important for calculating dosages and understanding a drug's behavior over time.

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    ch4 8

    Uploaded by

    Wafa S
    19 views2 pages
    This document discusses several key concepts relating to drug distribution and elimination in the body. It explains that distribution extent, rate, and volume impact how quickly a drug reaches its site of action and how long it remains in the body. Drug binding, tissue permeability, blood flow, and patient factors like age, obesity, or disease can influence these distribution properties. The document also covers drug elimination rates and clearance, noting how metabolism, plasma binding, and organ function affect the speed a drug is removed from the body and its resulting pharmacokinetics. Concepts like volume of distribution, half-life, and clearance are important for calculating dosages and understanding a drug's behavior over time.

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    This document discusses several key concepts relating to drug distribution and elimination in the body. It explains that distribution extent, rate, and volume impact how quickly a drug reaches its site of action and how long it remains in the body. Drug binding, tissue permeability, blood flow, and patient factors like age, obesity, or disease can influence these distribution properties. The document also covers drug elimination rates and clearance, noting how metabolism, plasma binding, and organ function affect the speed a drug is removed from the body and its resulting pharmacokinetics. Concepts like volume of distribution, half-life, and clearance are important for calculating dosages and understanding a drug's behavior over time.

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    © All Rights Reserved
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    19 views2 pages

    ch4 8

    Uploaded by

    Wafa S
    This document discusses several key concepts relating to drug distribution and elimination in the body. It explains that distribution extent, rate, and volume impact how quickly a drug reaches its site of action and how long it remains in the body. Drug binding, tissue permeability, blood flow, and patient factors like age, obesity, or disease can influence these distribution properties. The document also covers drug elimination rates and clearance, noting how metabolism, plasma binding, and organ function affect the speed a drug is removed from the body and its resulting pharmacokinetics. Concepts like volume of distribution, half-life, and clearance are important for calculating dosages and understanding a drug's behavior over time.

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    • High distribution rate - drug reaches to the site of action quickly - fast drug effect (i.e.

    short
    onset time).

    • High distribution extent - drug reaches to a large portion of the body - long residence time
    in the body - prolonged therapeutic duration.

    • High Blood flow rate -- Increased rate of drug transfer --Decreased equilibration time

    • High permeability rate -- Increased rate of drug transfer -- Decreased equilibration time

    • Plasma protein binding is a reversible process.

    • Drugs that are highly bound to plasma protein have low distribution extent and distribution
    volume

    • Drugs that are highly bound to plasma protein have slow elimination rate, long half-life and
    residence time in the body

    • Drugs having high affinity to the tissues are characterized by large distribution extent and
    distribution volume

    • Distribution volume normalized by body weight of polar and water soluble drugs (e.g.
    digoxin, antipyrene, gentamicin) increases in newborns and decreases in obesity.

    • Distribution volume normalized by body weight of non-polar and lipid soluble drugs (e.g.
    barbiturates) decreases in newborns and increases in obesity.

    • Vd is not constant; it increases with time and plateaus when equilibrium is reached.

    • Vd (normalized by body weight) measures distribution extent − Large normalized Vd


    indicates large distribution extent.

    • elimination extent is always 100%

    • Increasing elimination rate decreases drug plasma concentration and thus reduces drug
    pharmacological effect.

    • Decreasing elimination rate increases drug plasma concentration and thus produces dose-
    dependent toxicity. And prolongs the life of the drug in the body and thus extends drug
    therapeutic duration.

    • k (Elimination rate constant) is directly proportional to elimination rate.

    • t0.5 is inversely proportional to elimination rate.


    • Large CL (𝐶𝑙𝑒𝑎𝑟𝑎𝑛𝑐𝑒) indicates fast elimination

    Applications 𝐶𝑙𝑒𝑎𝑟𝑎𝑛𝑐𝑒:
    • CL is used for calculation of the maintenance dose.
    • CL is used for calculation of the average steady state concentration

    Applications of Apparent volume of distribution:


    • Vd is used to identify the distribution pattern that characterizes a particular drugs.
    • calculation of the loading dose.

    • Rate of drug metabolism is described by Michaelis- Menten equation

    • Increasing hepatic clearance decreases drug plasma concentration and thus reduces drug
    pharmacological effect.

    • Increasing blood flow to the liver increases hepatic clearance.

    • In neonates, elderly, hepatic, kidney, and cardiac diseases, hepatic clearance is slower than
    in healthy adults.

    • highly bound to plasma protein have slow hepatic clearance

    • Increasing metabolic activity of the enzymes increases rate of metabolism of their


    substrates, thus increases hepatic clearance.

    • Drug metabolism is slower in neonates (due to immaturity of enzymes) and elderly humans
    (due to lower enzymatic activity).

    • Females metabolize alcohol more slowly than males

    • Rapid metabolizers are prone to reduced drug effect.


    • Slow metabolizers are prone to dose-dependent toxicity.

    • People who acetylate warfarin slowly (slow acetylators) are subject to excessive bleeding.
    • People who acetylate phenytoin slowly (slow acetylators) are subject to ataxia.

    • Biliary secretion promotes hepatic clearance, while intestinal reabsorption reverses it.

    • t0.5 and t0.9 are inversely proportional to reaction rate constants.

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