Pharmacology: Drug Metabolism and Elimination
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Questions and Answers

What is the primary location of liver cells in relation to capillaries for drug delivery?

  • Inside the capillaries extending from the central vein
  • Right adjacent to the capillaries extending from the central vein (correct)
  • Between the capillaries extending from the central vein and the peripheral vein
  • Far away from the capillaries extending from the central vein

    • What is the primary purpose of Phase-II metabolism in biotransformation?

  • To increase the overall polarity of a molecule (correct)
  • To break down a molecule into smaller components
  • To change the chemical structure of a molecule
  • To decrease the overall polarity of a molecule

    • Where are the Cytochrome P450 enzymes primarily found in hepatocytes?

  • Nucleus and cytoplasm
  • Mitochondria and smooth endoplasmic reticulum (correct)
  • Rough endoplasmic reticulum and Golgi apparatus
  • Lysosomes and peroxisomes

    • How many gene families are responsible for drug metabolism among the 63 Cytochrome P450 genes?

    <p>3 families</p> Signup and view all the answers

    What is the primary type of reaction in Phase-I metabolism?

    <p>Oxidation reaction</p> Signup and view all the answers

    What is the primary function of microsomes in liver metabolism?

    <p>To isolate and concentrate Cyp P450 enzymes</p> Signup and view all the answers

    Which of the following reactions is NOT an example of a Phase-I reaction?

    <p>Glucuronidation</p> Signup and view all the answers

    Where can extrahepatic metabolism occur?

    <p>In blood and other tissues</p> Signup and view all the answers

    What is the primary difference between microsomal and non-microsomal liver metabolism?

    <p>The presence or absence of Cyp P450 enzymes</p> Signup and view all the answers

    What type of enzyme is involved in peptide bond hydrolysis?

    <p>Peptidases</p> Signup and view all the answers

    What is the name of the enzyme involved in dehalogenation reactions?

    <p>None of the above</p> Signup and view all the answers

    What is the primary goal of drug metabolism?

    <p>To increase the polarity of the molecule</p> Signup and view all the answers

    Which organ is responsible for the majority of drug metabolism?

    <p>Liver</p> Signup and view all the answers

    What is the name of the functional unit in the liver where most metabolism takes place?

    <p>Liver lobule</p> Signup and view all the answers

    What is the percentage of cardiac output that goes to the liver?

    <p>25%</p> Signup and view all the answers

    What is the approximate blood flow rate to the liver?

    <p>1.5 L/min</p> Signup and view all the answers

    How many liver lobules are present in the human liver?

    <p>50,000 to 100,000</p> Signup and view all the answers

    Which type of reaction involves the conversion of the parent drug to a new molecule?

    <p>Phase-I Reaction</p> Signup and view all the answers

    What type of oxidation is mediated by Cytochrome P450 enzymes?

    <p>All of the above</p> Signup and view all the answers

    Which of the following is an example of a Phase-II reaction?

    <p>Glucuronidation</p> Signup and view all the answers

    What is the result of the acetylation process in Phase-II metabolism?

    <p>A more polar compound</p> Signup and view all the answers

    Which enzyme is involved in the hydrolysis of esters and amides?

    <p>Esterases</p> Signup and view all the answers

    What is the prosthetic group used by Monoamine Oxidase (MAO) for delivering oxygen?

    <p>Flavin adenine dinucleotide (FAD)</p> Signup and view all the answers

    Which enzyme family is involved in reducing ethanol and other endogenous/exogenous alcohols?

    <p>Alcohol Dehydrogenase</p> Signup and view all the answers

    What is the primary function of Xanthine Oxidase?

    <p>To oxidize purines</p> Signup and view all the answers

    Which co-factor is used by Monoamine Oxidase (MAO) for its catalytic activity?

    <p>Flavin adenine dinucleotide (FAD)</p> Signup and view all the answers

    What is the primary function of Monoamine Oxidase (MAO) in neurotransmitter regulation?

    <p>To degrade and regulate neurotransmitters</p> Signup and view all the answers

    What is the primary type of reaction involved in Phase-I metabolism?

    <p>Oxidation</p> Signup and view all the answers

    What is the name of the enzyme family primarily responsible for Phase-I metabolism?

    <p>Cytochrome p450</p> Signup and view all the answers

    What is the purpose of Phase-II metabolism in biotransformation?

    <p>To increase the polarity of a molecule</p> Signup and view all the answers

    Where are the Cytochrome p450 enzymes primarily found in hepatocytes?

    <p>Mitochondria and smooth endoplasmic reticulum</p> Signup and view all the answers

    What is the major metabolizing organ responsible for drug metabolism?

    <p>Liver</p> Signup and view all the answers

    What is the primary function of UDP-glucuronyl transferase in Phase-II metabolism?

    <p>To conjugate glucuronic acid with hydroxyl or carboxyl groups</p> Signup and view all the answers

    What is the role of CYP3A4 in Phase-I metabolism?

    <p>To oxidize substrates, such as buspirone</p> Signup and view all the answers

    What is the purpose of acetylation in Phase-II metabolism?

    <p>To conjugate acetyl-CoA with amines</p> Signup and view all the answers

    What is the result of glucuronidation in Phase-II metabolism?

    <p>The formation of a more hydrophilic compound</p> Signup and view all the answers

    What is the purpose of Phase-II metabolism?

    <p>To conjugate compounds with hydrophilic groups, increasing their water solubility</p> Signup and view all the answers

    What is the direction of movement of small lipid-soluble molecules during passive diffusion?

    <p>From an area of high to low concentration</p> Signup and view all the answers

    What is the primary function of human serum albumin (HSA) in the bloodstream?

    <p>To bind and transport drug molecules</p> Signup and view all the answers

    What is the characteristic of phospholipid molecules that allows them to form a membrane?

    <p>They are amphipathic and have a hydrophobic tail and a hydrophilic head</p> Signup and view all the answers

    What is the result of a drug molecule binding to a plasma protein?

    <p>The molecule is unavailable for binding to pharmacological targets</p> Signup and view all the answers

    What is the primary factor that determines the ability of a molecule to cross a phospholipid membrane?

    <p>The lipophilicity of the molecule</p> Signup and view all the answers

    What is the primary mechanism that allows lipophilic molecules to pass through the plasma membrane?

    <p>Passive diffusion</p> Signup and view all the answers

    Which type of molecules have a harder time passing through the fatty cell membranes?

    <p>Hydrophilic</p> Signup and view all the answers

    What is the characteristic of the plasma membrane that allows it to selectively permeable?

    <p>It is selectively permeable to lipophilic molecules</p> Signup and view all the answers

    What is the primary function of active transport in the context of drug delivery?

    <p>To facilitate the movement of molecules across the membrane</p> Signup and view all the answers

    What is a characteristic of lipophilic molecules in the context of drug delivery?

    <p>They are more permeable than ionized or polar molecules</p> Signup and view all the answers

    What is the direction of movement of molecules in active transport?

    <p>From low to high concentration</p> Signup and view all the answers

    What is a characteristic of a saturable active transport system?

    <p>It has a specific binding site on the carrier</p> Signup and view all the answers

    What is required for active transport to occur?

    <p>Energy, such as ATP</p> Signup and view all the answers

    Which of the following is an example of a drug that is well-absorbed despite being an acid?

    <p>Penicillin</p> Signup and view all the answers

    What type of molecules are more likely to be transported via active transport?

    <p>Ionized molecules</p> Signup and view all the answers

    What is the primary purpose of plasma protein binding in pharmacokinetics?

    <p>To retain the drug in the plasma compartment</p> Signup and view all the answers

    What is the primary determinant of passive diffusion across a phospholipid membrane?

    <p>Lipid solubility of the drug</p> Signup and view all the answers

    According to Fick's Law, what is the direction of diffusion?

    <p>From higher concentration to lower concentration</p> Signup and view all the answers

    What is the optimal range of LogP for a compound to have high oral bioavailability?

    <p>0 &lt; LogP &lt; 3</p> Signup and view all the answers

    What is the definition of lipophilicity?

    <p>The tendency of a compound to partition in a nonpolar lipid matrix</p> Signup and view all the answers

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