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

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

<p>CYP1A2 (D)</p> Signup and view all the answers

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

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

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

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

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

<p>Highly lipid soluble drugs (B)</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 (A)</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 (C)</p> Signup and view all the answers

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

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

Which of the following is a phase I biotransformation?

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

Which of the following is a phase II biotransformation?

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

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

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

What is the preferred route of metabolism for Drug B?

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

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

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

What type of reaction is N-dealkylation?

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

Which conjugation pathway is the most common phase 2 reaction?

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

Do acetylation and methylation increase water solubility?

<p>No (A)</p> Signup and view all the answers

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

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

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

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

What is the most common phase I metabolic transformation?

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

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

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

Which conjugation pathway predominates at high substrate concentrations?

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

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

<p>Lipid soluble drugs (A)</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. (B)</p> Signup and view all the answers

What is the main function of Phase I metabolism?

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

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

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

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

<p>CYP2 (C)</p> Signup and view all the answers

What is the most common reaction catalyzed by cytochromes P450?

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

<p>N-acetylation (C)</p> Signup and view all the answers

Which of the following is a phase I biotransformation?

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

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

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

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

<p>CYP3A4 (D)</p> Signup and view all the answers

Which conjugation pathway is the most common phase 2 reaction?

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

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

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

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

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

Which organ has the highest metabolic capacity for drug biotransformation?

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

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

<p>CYP2 (A)</p> Signup and view all the answers

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

<p>CYP3A4 (C)</p> Signup and view all the answers

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

<p>CYP1A2 (A)</p> Signup and view all the answers

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

<p>CYP2D6 (B)</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 (A)</p> Signup and view all the answers

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

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

Which of the following is a phase II biotransformation?

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

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

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

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

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

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

<p>CYP2D6 (A)</p> Signup and view all the answers

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

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

What is the purpose of drug metabolism?

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

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

<p>Highly lipid soluble drugs (D)</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 (B)</p> Signup and view all the answers

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

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

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

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

Which of the following is a phase I biotransformation?

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

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

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

What type of reaction is N-dealkylation?

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

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

<p>Cytochrome P450 (C)</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 (A)</p> Signup and view all the answers

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

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

Which of the following is a phase I biotransformation?

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

Which of the following is a phase II biotransformation?

<p>Hydrolysis of aspirin (D)</p> Signup and view all the answers

Which of the following is metabolized by dealkylation pathway?

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

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

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

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