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Questions and Answers

True or False: All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.

  • True
  • False (correct)
  • Which phase of biotransformation is involved in the deactivation of reactive intermediates formed during drug metabolism?

  • Phase 1
  • Phase 2 (correct)
  • Which pathway is involved in the metabolism of aspirin?

  • Phase 2 conjugation
  • Phase 1 hydrolysis (correct)
  • True or False: N-dealkylation is an oxidation reaction.

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

    What is the result of N-dealkylation of tertiary amines?

    <p>A product with decreased activity and shorter duration of action</p> Signup and view all the answers

    Which phase of biotransformation involves the conjugation of drugs with glucuronic acid?

    <p>Phase 2</p> Signup and view all the answers

    Which organ has the highest metabolic capacity for drug biotransformation?

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

    Where are the phase I oxidative enzymes predominantly localized?

    <p>Endoplasmic reticulum</p> Signup and view all the answers

    Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?

    <p>CYP2</p> Signup and view all the answers

    Which enzyme is responsible for the metabolism of 1/3 of all important drugs?

    <p>CYP3A4</p> Signup and view all the answers

    Which enzyme is involved in the oxidation of aromatic rings?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which enzyme is involved in the N-oxidation of primary aromatic amines?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which category of drug metabolism involves the addition of endogenous compounds to the drug molecule?

    <p>Phase 2 metabolism</p> Signup and view all the answers

    Which type of transformation is most prevalent in phase 1 metabolism?

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

    Which drugs require more metabolic transformations than hydrophilic drugs?

    <p>Lipid soluble drugs</p> Signup and view all the answers

    Do all drugs require both phase 1 and phase 2 biotransformation?

    <p>No, some drugs do not require any metabolic transformations</p> Signup and view all the answers

    What is the purpose of drug metabolism?

    <p>To remove/eliminate drugs from the body</p> Signup and view all the answers

    Which phase of drug metabolism increases water solubility?

    <p>Phase 1 metabolism</p> Signup and view all the answers

    Which of the following is a phase I biotransformation?

    <p>Conversion of propranolol to 4-hydroxypropranolol</p> Signup and view all the answers

    Which of the following is a phase II biotransformation?

    <p>Conversion of a drug to an acyl glucuronide</p> Signup and view all the answers

    Which of the following is the main metabolic pathway for the drug?

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

    Which of the following is a common biotransformation pathway for secondary and tertiary amines?

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

    Which ester group in the structure of Cocaine is readily hydrolyzed by esterases?

    <p>The ester group on the methyl ester moiety</p> Signup and view all the answers

    Which phase of metabolism introduces a new functional group or modifies an existing group?

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

    Which conjugative pathway is the most common and greatly increases water solubility of the conjugated product?

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

    What is the major conjugation pathway for phenols, alcohols, and amines?

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

    Which enzyme is responsible for transferring glucuronic acid to the drug?

    <p>UDP-glucuronyl transferase (UGT)</p> Signup and view all the answers

    What is the most common phase 1 metabolic transformation?

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

    Which phase of metabolism prepares the compound for phase II metabolism?

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

    Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?

    <p>CYP2</p> Signup and view all the answers

    Which phase of biotransformation involves the conjugation of drugs with glucuronic acid?

    <p>Phase II</p> Signup and view all the answers

    Which enzyme is responsible for the metabolism of 1/3 of all important drugs?

    <p>CYP3A4</p> Signup and view all the answers

    Which enzyme is involved in the N-oxidation of primary aromatic amines?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which phase of metabolism prepares the compound for phase II metabolism?

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

    Which organ has the highest metabolic capacity for drug biotransformation?

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

    Which type of biotransformation involves the addition of endogenous compounds to the drug molecule?

    <p>Phase 2 metabolism</p> Signup and view all the answers

    Which phase of drug metabolism prepares the compound for phase II metabolism?

    <p>Phase 1 metabolism</p> Signup and view all the answers

    Which phase of biotransformation involves the conjugation of drugs with glucuronic acid?

    <p>Phase 2 metabolism</p> Signup and view all the answers

    Which enzyme is responsible for transferring glucuronic acid to the drug?

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

    Which phase of metabolism increases the water solubility of drug molecules?

    <p>Phase 1 metabolism</p> Signup and view all the answers

    Do all drugs require both phase 1 and phase 2 biotransformation?

    <p>Depends on the drug</p> Signup and view all the answers

    Which of the following is a phase I biotransformation pathway that involves hydrolysis?

    <p>O-dealkylation</p> Signup and view all the answers

    Which enzyme is responsible for the N-hydroxylation of procainamide?

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

    Which of the following is a phase II biotransformation pathway?

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

    Which of the following is a common metabolic pathway for secondary and tertiary amines?

    <p>N-dealkylation</p> Signup and view all the answers

    Which enzyme is responsible for transferring glucuronic acid to drugs?

    <p>UDP-glucuronyl transferase</p> Signup and view all the answers

    Which of the following is a major conjugation pathway for phenols, alcohols, and amines?

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

    True or False: Glutathione conjugation is a phase II biotransformation process.

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

    Which enzyme is involved in N-acetylation of primary amino groups?

    <p>N-acetyltransferase</p> Signup and view all the answers

    What is the main metabolic product of p-aminosalicylic acid?

    <p>N-acetylated PAS</p> Signup and view all the answers

    Which amino acid is commonly used for conjugation with xenobiotics?

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

    True or False: Acetylation increases the water solubility of drugs.

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

    Which enzyme is responsible for the formation of amide or peptide bonds during amino acid conjugation?

    <p>Glutamine synthetase</p> Signup and view all the answers

    Which of the following is the main pathway of biotransformation for primary aromatic amines?

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

    Which of the following is a phase I biotransformation?

    <p>Conversion of propranolol to 4-hydroxypropranolol</p> Signup and view all the answers

    Which of the following is a phase II biotransformation?

    <p>Conversion of a drug to an acyl glucuronide</p> Signup and view all the answers

    Which of the following is the main metabolic pathway for the drug?

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

    Which of the following is a common biotransformation pathway for secondary and tertiary amines?

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

    Which ester group in the structure of Cocaine is readily hydrolyzed by esterases and why?

    <p>The ester group on the methyl benzoate moiety</p> Signup and view all the answers

    Which of the following is a phase I biotransformation pathway that involves hydrolysis?

    <p>N-Dealkylation</p> Signup and view all the answers

    Which of the following is a phase II biotransformation pathway?

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

    Which enzyme is responsible for transferring glucuronic acid to drugs?

    <p>UDP-glucuronyl transferase</p> Signup and view all the answers

    Which of the following is a common metabolic pathway for secondary and tertiary amines?

    <p>N-Dealkylation</p> Signup and view all the answers

    Which phase of drug metabolism introduces a new functional group or modifies an existing group?

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

    Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?

    <p>CYP3A4</p> Signup and view all the answers

    True or False: All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.

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

    Which phase of biotransformation is involved in the deactivation of reactive intermediates formed during drug metabolism?

    <p>Phase 2</p> Signup and view all the answers

    Which enzyme is responsible for the formation of amide or peptide bonds during amino acid conjugation?

    <p>Glutathione S-transferase</p> Signup and view all the answers

    True or False: N-dealkylation is an oxidation reaction.

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

    Which enzyme is responsible for the metabolism of 1/3 of all important drugs?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which phase of drug metabolism increases water solubility?

    <p>Phase 2</p> Signup and view all the answers

    Which of the following is a phase 2 biotransformation?

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

    True or False: Acetylation increases the water solubility of drugs.

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

    Which enzyme is responsible for transferring glucuronic acid to drugs?

    <p>Glucuronyl transferase</p> Signup and view all the answers

    Which organ has the highest metabolic capacity for drug biotransformation?

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

    Which phase of drug metabolism prepares the compound for phase II metabolism?

    <p>Phase 1 metabolism</p> Signup and view all the answers

    Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which of the following organs have significant metabolic capacity for drug biotransformation?

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

    Which site is predominantly responsible for the localization of phase I oxidative enzymes?

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

    Which cytochrome P450 family is responsible for metabolizing approximately 50% of all clinically important drugs?

    <p>CYP2</p> Signup and view all the answers

    Which enzyme is responsible for the metabolism of one-third of all important drugs?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which functional groups can be introduced into a wide variety of compounds by cytochromes P450?

    <p>Aromatic rings and aliphatic chains</p> Signup and view all the answers

    Which enzyme is involved in the oxidation of alkenes to epoxides?

    <p>Cytochrome P450</p> Signup and view all the answers

    Which of the following is the main pathway of biotransformation for primary aromatic amines?

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

    Which of the following is a phase I biotransformation?

    <p>Conversion of propranolol to 4-hydroxypropranolol</p> Signup and view all the answers

    Which of the following is a phase II biotransformation?

    <p>Conversion of a drug to an acyl glucuronide</p> Signup and view all the answers

    Which of the following is metabolized by dealkylation pathway?

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

    The structure of Cocaine contains two ester groups. Which of these groups is readily hydrolyzed by esterases and why?

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

    N-dealkylation of secondary and tertiary amines is a common biotransformation pathway. The product formed has a longer half-life and contributes to biological activity.

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

    The following biotransformation takes place in Phase I

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

    Phase II reaction involving glucuronic acid takes place in

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

    Phase I reaction involving CYP450 takes place in, a monooxygenase reaction

    <p>Endoplasmic Reticulum</p> Signup and view all the answers

    One of the following medications is converted to an active metabolite after Phase I Reaction

    <p>A and B</p> Signup and view all the answers

    Conversion of propranolol by Phase I reaction produces an active metabolite called

    <p>4-OH propranolol</p> Signup and view all the answers

    Codeine converts to an active (morphine metabolite) in Phase 1 reaction by N-demethylation

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

    Which one of the following uses Cytochrome P 450 family called CYP3A4 in Phase I

    <p>Dealkylation of secondary and tertiary amines, Tegretol, Diazepam, Imipramine</p> Signup and view all the answers

    VS.-Para location is the most preferred location for Aromatic hydroxylation in molecules with steric hindrance groups and electron donating groups

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

    Ketoprofen has no aromatic hydroxylation.

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

    Most Aromatic Oxidations first produces ______________ which is highly (reactive, toxic and carcinogenic) metabolites; this later reacts with________________ making the product non toxic by deactivation.

    Signup and view all the answers

    _____________________it undergoes ____________to a metabolite in aplastic anemia and undergoes __________, therefore repeated doses will bring about decreased half life.

    Signup and view all the answers

    One of the following actions are used to terminate actions.

    <p>Acetylation and Methylation in Phase II</p> Signup and view all the answers

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