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

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

<p>Phase 2 (B)</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

Where are the phase I oxidative enzymes predominantly localized?

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

Which enzyme is involved in the oxidation of aromatic rings?

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

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

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

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

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

Which 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 metabolic transformations (D)</p> Signup and view all the answers

What is the purpose of drug metabolism?

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

Which phase of drug metabolism increases water solubility?

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

Which of the following is a phase I biotransformation?

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

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

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

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

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

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

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

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

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

What is the most common phase 1 metabolic transformation?

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

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

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

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

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

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

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

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

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

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

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

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

<p>Phase I (A)</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 type of biotransformation involves the addition of endogenous compounds to the drug molecule?

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Which of the following is a phase II biotransformation pathway?

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

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

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

Which enzyme is responsible for transferring glucuronic acid to drugs?

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

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

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

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

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

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

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

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

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

Which amino acid is commonly used for conjugation with xenobiotics?

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

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

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

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

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

Which of the following is a phase I biotransformation?

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

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

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

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

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

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

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

Which of the following is a phase II biotransformation pathway?

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

Which enzyme is responsible for transferring glucuronic acid to drugs?

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

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

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

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

<p>CYP3A4 (A)</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 phase of biotransformation is involved in the deactivation of reactive intermediates formed during drug metabolism?

<p>Phase 2 (B)</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 (D)</p> Signup and view all the answers

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

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

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

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

Which phase of drug metabolism increases water solubility?

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

Which of the following is a phase 2 biotransformation?

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

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

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

Which enzyme is responsible for transferring glucuronic acid to drugs?

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

Which organ has the highest metabolic capacity for drug biotransformation?

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

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

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

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

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

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

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

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

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

Which cytochrome P450 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 one-third of all important drugs?

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

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

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

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

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

Which of the following is metabolized by dealkylation pathway?

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

The following biotransformation takes place in Phase I

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

Ketoprofen has no aromatic hydroxylation.

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

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