Unraveling Nitroso Intermediates
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Questions and Answers

Which enzyme system is mainly localized in the liver?

  • Phase I enzymes (correct)
  • Cytosolic enzymes
  • Phase II enzymes
  • Microsomal enzymes

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

  • CYP3
  • CYP1
  • CYP2 (correct)
  • CYP4

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

  • CYP3A4 (correct)
  • CYP1A2
  • CYP2D6
  • CYP4A11

    • Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?

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

    Which enzyme is responsible for the oxidation of methyl attached to oxygen?

    <p>CYP1A2</p> Signup and view all the answers

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

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

    Which category of drug metabolism involves the addition of endogenous compounds to a 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

    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

    Which type of drugs require more metabolic transformations than hydrophilic drugs?

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

    In some cases, which type of transformation is all that is required for a drug molecule?

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

    What can a hydroxyl group or carboxyl group in a drug molecule be conjugated with to form a readily excretable compound?

    <p>Glucuronic acid</p> Signup and view all the answers

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

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

    Which of the following is a phase I biotransformation?

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

    Which of the following is a phase II biotransformation?

    <p>H. Hydrolysis of aspirin</p> Signup and view all the answers

    Which of the following drugs is metabolized by the dealkylation pathway?

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

    What is the preferred route of metabolism for Drug B?

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

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

    <p>B. Group B</p> Signup and view all the answers

    True or False.

    <p>All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.</p> Signup and view all the answers

    Which pathway is involved in the deactivation of reactive intermediates formed during biotransformation?

    <p>Glutathione conjugation</p> Signup and view all the answers

    What type of reaction is N-dealkylation?

    <p>Oxidation</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 conjugation pathway is the most common phase 2 reaction?

    <p>Glucuronic acid conjugation</p> Signup and view all the answers

    Do acetylation and methylation increase water solubility?

    <p>No</p> Signup and view all the answers

    Which of the following is the most common conjugative pathway for xenobiotic substrates?

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

    What is the main function of Phase I metabolism?

    <p>To prepare the compound for Phase II metabolism</p> Signup and view all the answers

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

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

    What is the most common phase I metabolic transformation?

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

    Which of the following is a major pathway for cocaine metabolism?

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

    Which conjugation pathway predominates at high substrate concentrations?

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

    Which category of metabolic transformations involves the addition of endogenous compounds to a drug molecule?

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

    Which type of 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 biotransformation.</p> Signup and view all the answers

    What is the main function of Phase I metabolism?

    <p>To increase water solubility of drugs</p> Signup and view all the answers

    Which enzyme is responsible for the metabolism of a significant number of important drugs?

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

    What can a hydroxyl group or carboxyl group in a drug molecule be conjugated with to form a readily excretable compound?

    <p>Glucuronic acid</p> Signup and view all the answers

    Which enzyme is responsible for the metabolism of approximately 50% of all clinically important drugs?

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

    What is the most common reaction catalyzed by cytochromes P450?

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

    Which of the following is an example of phase I biotransformation?

    <p>Aromatic hydroxylation</p> Signup and view all the answers

    Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?

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

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

    <p>Oxidation of methyl attached to nitrogen</p> Signup and view all the answers

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

    <p>Glucuronyl transferase</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 of the following is NOT a phase 1 biotransformation reaction?

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

    True or False: The sulfhydryl group of glutathione is involved in the deactivation of reactive intermediates formed during biotransformation.

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

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

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

    True or False: N-dealkylation of tertiary amines generally results in a product with the same activity and longer duration of action.

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

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

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

    Which of the following is the main metabolic pathway for the drug mentioned in question 7?

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

    Which of the following is the main pathway of metabolism for drugs such as carbamazepine?

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

    True or False: 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

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

    <p>N-acetylation</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 enzyme is responsible for the N-oxidation of primary aromatic amines?

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

    Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?

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

    Which conjugation pathway is the most common phase 2 reaction?

    <p>Glucuronidation</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

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

    <p>Methyl ester, because it is easily accessible</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 organ has the highest metabolic capacity for drug biotransformation?

    <p>Liver</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 an alkyl group to a carboxylic acid?

    <p>CYP1A2</p> Signup and view all the answers

    Which enzyme is responsible for the N-oxidation of primary aromatic amines?

    <p>CYP2D6</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 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?

    <p>Glucuronidation</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

    Which of the following is a common phase I metabolic transformation?

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

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

    <p>CYP2D6</p> Signup and view all the answers

    Which of the following is the most common conjugative pathway for xenobiotic substrates?

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

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

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

    What is the purpose of drug metabolism?

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

    Which type of drugs require more metabolic transformations than hydrophilic drugs?

    <p>Highly 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 require only phase 2 biotransformation</p> Signup and view all the answers

    What is the main purpose of phase 1 transformations in drug metabolism?

    <p>To increase water solubility</p> Signup and view all the answers

    Which of the following is NOT a phase 1 biotransformation reaction?

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

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

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

    Which of the following is a phase I biotransformation?

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

    Which enzyme is involved in the deactivation of reactive intermediates formed during biotransformation?

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

    What type of reaction is N-dealkylation?

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

    Which enzyme is responsible for the metabolism of a significant number of important drugs?

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

    What can a hydroxyl group or carboxyl group in a drug molecule be conjugated with to form a readily excretable compound?

    <p>Glucuronic acid</p> Signup and view all the answers

    Which of the following is the main pathway of biotransformation of 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>Hydrolysis of aspirin</p> Signup and view all the answers

    Which of the following is metabolized by dealkylation pathway?

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

    True or False: 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>False</p> Signup and view all the answers

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

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

    RH + O2 + NADPH + H+ → ROH + H2O + NADP+ This is the most common reaction catalyzed by CYP450; a monooxygenase reaction.

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

    One of the following phase 1 reactions do not present an inactive metabolite

    1. Propranolol to 4-OH propranolol in Aromatic hydroxylation.

    2. Diazepam Aromatic Hydroxylation

    3. Codeine to Morphine

    4. Biotransformation of Fenoprofen

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

    Acetylation, Methylation do not hydrolyze in Phase II reaction, they are only there to terminate a reaction.

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

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