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  • Topic 6 Pharmacokinetics and Drug Metabolism: Chapter 8 Patrick

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    This document discusses key aspects of drug pharmacokinetics and metabolism. It covers the ADME process - absorption, distribution, metabolism and excretion of drugs in the body. It describes various drug administration routes and formulations. Factors like a drug's acid-base properties, size and hydrophobicity can impact its absorption and distribution in the body. The document also discusses phase I and phase II metabolism pathways in the liver, as well as drug distribution through serum albumin and examples of metabolic conjugation reactions. Maintaining the therapeutic window of a drug is important through proper dosing and consideration of its pharmacokinetics.

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    This document discusses key aspects of drug pharmacokinetics and metabolism. It covers the ADME process - absorption, distribution, metabolism and excretion of drugs in the body. It describes various drug administration routes and formulations. Factors like a drug's acid-base properties, size and hydrophobicity can impact its absorption and distribution in the body. The document also discusses phase I and phase II metabolism pathways in the liver, as well as drug distribution through serum albumin and examples of metabolic conjugation reactions. Maintaining the therapeutic window of a drug is important through proper dosing and consideration of its pharmacokinetics.

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    © All Rights Reserved
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    8 views32 pages

    Topic 6 Pharmacokinetics and Drug Metabolism: Chapter 8 Patrick

    Uploaded by

    grcp
    This document discusses key aspects of drug pharmacokinetics and metabolism. It covers the ADME process - absorption, distribution, metabolism and excretion of drugs in the body. It describes various drug administration routes and formulations. Factors like a drug's acid-base properties, size and hydrophobicity can impact its absorption and distribution in the body. The document also discusses phase I and phase II metabolism pathways in the liver, as well as drug distribution through serum albumin and examples of metabolic conjugation reactions. Maintaining the therapeutic window of a drug is important through proper dosing and consideration of its pharmacokinetics.

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    Topic 6 Pharmacokinetics and

    Drug Metabolism
    Chapter 8 Patrick

    Drug candidate pharmaceutics are critical:


    ADME

    Absorption
    Distribution
    Metabolism
    Excretion

    Drug candidate pharmaceutics are critical:


    Drug Administration route1. Oral
    2. Mucous membranes
    1. Rectal
    2. Oral (buccal)
    3. Topical-transdermal
    4. Inhaled
    5. Injected
    1. Intravenous
    2. Intramuscular
    3. Subcutaneous
    4. Intrathecal-spinal
    5. Intraperotoneal

    Drug candidate pharmaceutics are critical:


    Formulations
    1.
    2.
    3.
    4.

    Pills, capsules
    Liquid
    Patch
    Liposome/micelle

    Pharmaceutics

    Therapeutic
    Window must
    be maintained
    by dosing

    Pharmaceutics

    Therapeutic
    Window must
    be maintained
    by dosing

    Absorption
    Drug Absorption, Metabolism and Excretion
    http://www.cc.nih.gov/training/training/principles/schedule.html

    Drug molecule factors affecting absorption and


    distribution
    1. Acid-base properties

    2. Hydrophobicity/Functional groups

    3. Size

    Absorption

    A good drug
    A lousy drug: insulin

    Lipinskis rules for lousy drug absorption:


    1. MW>500
    2. H-bond donors>5
    3. H-bond acceptors>10
    4. log Partition coefficient > 5
    i.e. octanol /water > 100,000:1

    Distribution:Serum Albumin, The


    distributor of non polar drugs

    Seeing distribution: e.g.


    fluconazole

    PET scan of 18F fluconazole

    Metabolism/excretion

    Phase I Metabolism
    Oxidation

    Metabolism/excretion
    1. Phase 1 metabolism- Liver microsomal system

    Metabolism/excretion
    1. Phase 1 metabolism- Liver microsomal system

    Metabolism/excretion

    Metabolism/excretion

    Metabolism/excretion
    1. Phase 1 metabolism- Liver microsomal system

    Metabolism/excretion
    1. Phase 1 metabolism

    Metabolism/excretion
    1. Phase 1 metabolism

    Metabolism/excretion

    EXAMPLE: a Ca 2+ channel blocker for hypertension

    EXAMPLE: a Ca 2+ channel blocker for hypertension

    Phase II Metabolism

    Metabolism/excretion
    Conjugation examples

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