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MO28 Introduction to Drug Metabolism

Mer Scott 10 questions

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  1. 1Metabolism is the [blank_start]modification[blank_end] of the chemical structure of compounds by [blank_start]enzymes[blank_end] present in the body. This is done by drug metabolising enzymes (DMEs)
    Roles of DMEs:
    1. [blank_start]Biosynthesis[blank_end] and subsequent breakdown of molecules required by the body
    – [blank_start]endogenous[blank_end] compounds like insulin, adrenalin, cholesterol
    2. [blank_start]Biotransformation[blank_end] of foreign (toxic) compounds known as xenobiotics to [blank_start]deactivate[blank_end] and facilitate [blank_start]secretion[blank_end]
    – Therapeutic drugs
    – Recreational drugs
    – Occupational hazards
    3. [blank_start]Prodrug[blank_end] activation
    1. Amodification
    2. Benzymes
    3. CBiosynthesis
    4. Dendogenous
    5. EBiotransformation
    6. Fdeactivate
    7. Gsecretion
    8. HProdrug
  2. 2Metabolism occurs mainly in which two sub-cellular organelles?
    1. Athe endoplasmic reticulum and cytosol
    2. Bthe endoplasmic reticulum and golgi complex
    3. Cthe golgi complex and nucleus
    4. Dthe golgi complex and cytosol
  3. 3Phase 1 enzymes & UGT are almost exclusively in the cytoplasm, while Phase 2 enzymes (except UGT) are almost exclusively on the ER.
    1. ATrue
    2. BFalse
  4. 4Metabolism in vitro is divided into:
    1. Microsomal metabolism:
    • Includes [blank_start]membrane-bound[blank_end] enzymes in the [blank_start]smooth[blank_end] ER of cells.
    • Microsomal enzymes bring about most [blank_start]oxidations, reductions,[blank_end]
    [blank_start]glucuronide[blank_end] conjugations, acetylations.
    2. Non-microsomal metabolism
    • Occurs in the [blank_start]mitochondria and cytosol[blank_end]
    • Includes:
    – [blank_start]alcohol and aldehyde[blank_end] oxidation,
    – [blank_start]aldehyde and nitro[blank_end] reduction,
    – Hydrolysis
    – phase 2 [blank_start]conjugations[blank_end] other than glucuronidation
    1. Amembrane-bound
    2. Bsmooth
    3. Crough
    4. Doxidations, reductions,
    5. Eglucuronide
    6. Fmitochondria and cytosol
    7. Galcohol and aldehyde
    8. Haldehyde and nitro
    9. Iconjugations
  5. 5Lipophilic compounds are metabolised to more hydrophobic compounds to facilitate their excretion.
    1. ATrue
    2. BFalse
  6. 6It is important to identify ALL drug metabolites before marketing a drug because:
    1. ADrug metabolites can lead to hepatotoxicity and acute liver failure
    2. BDrug metabolites can lead to acidification or alkalation of blood and kidney failure
    3. CDrug metabolites can lead to multidrug resistance and cancer
  7. 7Select all the Phase 2 reactions.
    1. AOxidation
    2. BReduction
    3. CHydrolysis
    4. DGlucurondiation
    5. ESulfation
    6. FAcetylation
    7. GMethylation
    8. HAmino acid conjugation
    9. IGlutathione conjugation
  8. 8Choose the incorrect statement about microsomal oxidation.
    1. AIt involves the oxidative enzymes on the ER, mainly cytochrome P450 monooxygenases
    2. BIt requires molecular oxygen and the coenzyme FADH2
    3. CIt incorporates one atom of oxygen into an organic substrate molecule (RH, the drug) and reduces the other to water
  9. 9Label the parts of CYP nomenclature.Image for question 9
    1. AFamily
    2. BSubfamily
    3. CIsoform
  10. 10Grapefruit juice can significantly decrease the bioavailability of CYP3A4 substrates by inhibiting the enzyme.
    1. ATrue
    2. BFalse

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Description
PHCY211 (Molecules) Quiz on MO28 Introduction to Drug Metabolism, created by Mer Scott on 15/04/2018.
Author
Mer Scott
Language
English
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