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 (B)</p> Signup and view all the answers

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

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

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

<p>Glucuronidation (C)</p> Signup and view all the answers

Where can extrahepatic metabolism occur?

<p>In blood and other tissues (A)</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 (B)</p> Signup and view all the answers

What type of enzyme is involved in peptide bond hydrolysis?

<p>Peptidases (D)</p> Signup and view all the answers

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

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

What is the primary goal of drug metabolism?

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

Which organ is responsible for the majority of drug metabolism?

<p>Liver (D)</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 (D)</p> Signup and view all the answers

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

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

What is the approximate blood flow rate to the liver?

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

How many liver lobules are present in the human liver?

<p>50,000 to 100,000 (B)</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 (C)</p> Signup and view all the answers

What type of oxidation is mediated by Cytochrome P450 enzymes?

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

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

<p>Glucuronidation (D)</p> Signup and view all the answers

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

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

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

<p>Esterases (B)</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) (B)</p> Signup and view all the answers

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

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

What is the primary function of Xanthine Oxidase?

<p>To oxidize purines (C)</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) (A)</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 (D)</p> Signup and view all the answers

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

<p>Oxidation (B)</p> Signup and view all the answers

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

<p>Cytochrome p450 (D)</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 (B)</p> Signup and view all the answers

Where are the Cytochrome p450 enzymes primarily found in hepatocytes?

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

What is the major metabolizing organ responsible for drug metabolism?

<p>Liver (D)</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 (A)</p> Signup and view all the answers

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

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

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

<p>To conjugate acetyl-CoA with amines (C)</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 (C)</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 (B)</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 (C)</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 (B)</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 (C)</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 (A)</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 (C)</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 (C)</p> Signup and view all the answers

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

<p>Hydrophilic (D)</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 (D)</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 (B)</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 (A)</p> Signup and view all the answers

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

<p>From low to high concentration (B)</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 (A)</p> Signup and view all the answers

What is required for active transport to occur?

<p>Energy, such as ATP (A)</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 (B)</p> Signup and view all the answers

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

<p>Ionized molecules (B)</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 (A)</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 (D)</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 (A)</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 (B)</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 (B)</p> Signup and view all the answers

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