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    BIOPHARM Distribution Process

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    Prinz mendez
    The document discusses key concepts relating to drug distribution, including physiological factors that affect distribution such as cardiac output, regional blood flow, and capillary permeability. It also covers important parameters like protein binding and volume of distribution, providing examples of drugs that have high or low values for each parameter. The significance of these concepts for drug management and dosing is explained.

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    BIOPHARM Distribution Process

    Uploaded by

    Prinz mendez
    26 views20 pages
    The document discusses key concepts relating to drug distribution, including physiological factors that affect distribution such as cardiac output, regional blood flow, and capillary permeability. It also covers important parameters like protein binding and volume of distribution, providing examples of drugs that have high or low values for each parameter. The significance of these concepts for drug management and dosing is explained.

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    The document discusses key concepts relating to drug distribution, including physiological factors that affect distribution such as cardiac output, regional blood flow, and capillary permeability. It also covers important parameters like protein binding and volume of distribution, providing examples of drugs that have high or low values for each parameter. The significance of these concepts for drug management and dosing is explained.

    Copyright:

    © All Rights Reserved
    Download as PPTX, PDF, TXT or read online from Scribd
    Download as pptx, pdf, or txt
    26 views20 pages

    BIOPHARM Distribution Process

    Uploaded by

    Prinz mendez
    The document discusses key concepts relating to drug distribution, including physiological factors that affect distribution such as cardiac output, regional blood flow, and capillary permeability. It also covers important parameters like protein binding and volume of distribution, providing examples of drugs that have high or low values for each parameter. The significance of these concepts for drug management and dosing is explained.

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    BIOPHARMACEUTICS AND

    PHARMACOKINETICS
    DISTRIBUTION PROCESS
    Distribution
     The process by which a drug reversibly
    leaves the blood stream and enters the
    interstitium and then cells
     For an IV drug; No absorption occurs
     Distribution occurs immediately after
    administration
    Physiologic Factors affecting
    distribution:
    1. Cardiac output
     volume of blood pumped by the heart per
    minute
     Px with CHF may have delayed drug effect
    due to poor distribution
    2. Regional blood flow
     % of CO that reaches specific tissue
     Organs w/ high RBF:
    ◦ liver (25%), kidney(25%), lungs(100%), brain)
     Organs with low RBF
    ◦ bone, adipose)
     Capillary Permeability- delivery
    oxygenated blood to tissues; smallest vein
    3. Capillary Permeability
    Depends on
     Capillary structure
     Chemical nature of the
    drug

    4. Liphophilicity of the
    drug
    Two important parameters of drug
    distribution:
    1. Protein binding (PB)
    2. volume of distribution (Vd)
    Protein binding
     limits the access of drugs to certain body
    compartment.
     binding of the serum proteinsdecreases
    distribution
     Free form (unbound) can reach the site of
    action, metabolized, excreted
     Bound form (serves as reservoir)
    Examples of proteins & substrates
     Albumin weak acidic (dominant)
     Alpha 1 glycoprotein weak basic drugs
     Globulin binding hormones
    Significant of PB
     Provide slow release form of a drug
    (repository, resulting to extended affect).
     Limits access to certain body compartment
     Can make the drug prone to drug-drug
    interaction

    Examples of drugs with high protein binding:


     Diazepam, Indomethacin, Tolbutamide,
    Warfarin, Midazolam
    Volume of distribution (Vd)
     Mathematical relationship between the
    total amount of drug in body and the
    concentration of drug in the blood
     It is the hypothetical volume of fluid
    where drug is disposed.
     useful for calculating the loading dose of a
    drug
    Example:
     If 10 mg of a drug are injected and the
    plasma concentration is 1 mg/L what is
    Vd?
     Vd= Dose = 10 = 10 L
    C0 1
    Examples of drugs with high Vd:
     Atropine
     Chloroquine
     Digoxin
     Fluoxetine
     Imipramine & TCAs
     Beta blockers
    Examples of Drugs with low Vd:
     Chlorpropamide
     Furosemide
     Tolbutamine
     Valproic Acid
     Warfarin
    Significance: Management of
    Toxicities/ drug overdose
     Drugs w/ low Vd= hemodialysis
    (alternative treatment)
     Drugs w/ high Vd = hemodialysis (useless)
    Plasma half-life of drugs
     Length of time needed to decrease drug
    plasma concentration by one half
     The greater the half-life of the drug, the
    longer it takes to excrete
     Determines frequency and dosages
    Example:
     If paracetamol 500mg/tab has half-life of 4
    hours, how long will it take until the
    blood concentration of this drug falls to
    25% of its initial strength?
    **END of DISCUSSION**

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