2022-09-07T17:26:15+03:00[Europe/Moscow] en true <p>Metabolism</p>, <p>more polar</p>, <p>Liver, intestine, kidney, lung, other tissues</p>, <p>Metabolitess</p>, <p>Detoxification</p>, <p>Bioactivation</p>, <p>Phase I</p>, <p>Phase II</p>, <p>Oxidation, dealkylation, deamination, reduction, hydrolysis</p>, <p>glucuronidation, sulfation, acetylation, methylation</p>, <p>First pass metabolism</p>, <p>CYP450</p>, <p>True</p>, <p>Electron withdrawing</p>, <p>Electron donating</p>, <p>Oxidation</p>, <p>NADPH</p>, <p>Prodrugs</p>, <p>esterases</p>, <p>Phase 2 reactions</p>, <p>elimination in urine or bile</p>, <p>Glucuronidation</p>, <p>Sulfation &amp; Glucuronidation</p>, <p>CYP3A4</p>, <p>-OH, -COOH, -NH2, -SH</p>, <p>endoplasmic reticulum </p>, <p>CYP 1, 2, 3</p>, <p>NADPH &amp; O2</p>, <p>intestinal mucosa</p> flashcards
Drug Metabolism

Drug Metabolism

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  • Metabolism

    conversion of one substance into another substance in the body

  • more polar

    The goal of metabolism is to rid the body of foreign compounds (xenobiotic) by making ____ products

  • Liver, intestine, kidney, lung, other tissues

    Drugs undergo chemical changes in the body by enzymes produced by what organs?

  • Metabolitess

    Products of metabolism

  • Detoxification

    -metabolites are inactive

    -metabolites are less toxic

  • Bioactivation

    -metabolites are more active

    -metabolites are more toxic

  • Phase I

    -introduces new functional groups

    -modifies existing functional groups

    -creates substrates for phase II

    -Enhances polarity and solubility

  • Phase II

    -conjugation and elimination

    -conjugation of drug or metabolite

    -conjugation adds an additional group

  • Oxidation, dealkylation, deamination, reduction, hydrolysis

    Phase I metabolism will include what type of chemical reactions?

  • glucuronidation, sulfation, acetylation, methylation

    Phase II metabolism will include what type of chemical reactions?

  • First pass metabolism

    drugs metabolized by liver or extra hepatic tissue before reaching systemic circulation

  • CYP450

    most common and important type of biotransformation

  • True

    Most drugs are metabolized by CYP3A4. T/f?

  • Electron withdrawing

    reduce aromatic oxidation

  • Electron donating

    enhances para- and ortho-oxidation

  • Oxidation

    -makes highly polar products for elimination

  • NADPH

    Reduction reactions require what chemical?

  • Prodrugs

    -carboxylic acid containing drugs that have a difficult time crossing membranes at some pHs

    - these are ester derivatives that are inactive

  • esterases

    carboxylic acid is released by ____

  • Phase 2 reactions

    -conjugate functional groups that were created during Phase I are already present on parent drug

    -inactivate the drug in most cases

  • elimination in urine or bile

    Phase II reactions all lead to what?

  • Glucuronidation

    -most common reaction to form water soluble metabolites

    -primarily excreted by kidneys, sometimes GI tract with bile

  • Sulfation & Glucuronidation

    What are the primary metabolic reactions in first pass metabolism?

  • CYP3A4

    found in intestinal mucosa and affects oral bioavailability of many drugs

  • -OH, -COOH, -NH2, -SH

    Which functional groups symbolize oxidation, reduction, or hydrolysis?

  • endoplasmic reticulum

    Where is CYP450 located?

  • CYP 1, 2, 3

    Which enzymes in the CYP family are involved in drug metabolism?

  • NADPH & O2

    CYP450 enzyme requires what molecules?

  • intestinal mucosa

    Where is CYP3A4 located?