93 Questions
Which enzyme system is mainly localized in the liver?
Phase I enzymes
Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?
CYP2
Which enzyme is responsible for the metabolism of 1/3 of all important drugs?
CYP3A4
Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?
Cytochrome P450
Which enzyme is responsible for the oxidation of methyl attached to oxygen?
CYP1A2
Which enzyme is involved in the N-oxidation of primary aromatic amines?
Glucuronyl transferase
Which category of drug metabolism involves the addition of endogenous compounds to a drug molecule?
Phase 2 metabolism
Which type of transformation is most prevalent in phase 1 metabolism?
Oxidation
Do all drugs require both phase 1 and phase 2 biotransformation?
No, some drugs do not require any metabolic transformations.
Which type of drugs require more metabolic transformations than hydrophilic drugs?
Highly lipid soluble drugs
In some cases, which type of transformation is all that is required for a drug molecule?
Phase 2 transformation
What can a hydroxyl group or carboxyl group in a drug molecule be conjugated with to form a readily excretable compound?
Glucuronic acid
Which of the following is the main pathway of biotransformation of primary aromatic amines?
b. Deamination
Which of the following is a phase I biotransformation?
A. Conversion of propranolol to 4-hydroxypropranolol
Which of the following is a phase II biotransformation?
H. Hydrolysis of aspirin
Which of the following drugs is metabolized by the dealkylation pathway?
A
What is the preferred route of metabolism for Drug B?
C. Acetylation
Which ester group in the structure of Cocaine is readily hydrolyzed by esterases and why?
B. Group B
True or False.
All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.
Which pathway is involved in the deactivation of reactive intermediates formed during biotransformation?
Glutathione conjugation
What type of reaction is N-dealkylation?
Oxidation
What is the result of N-dealkylation of tertiary amines?
A product with decreased activity and shorter duration of action
Which conjugation pathway is the most common phase 2 reaction?
Glucuronic acid conjugation
Do acetylation and methylation increase water solubility?
No
Which of the following is the most common conjugative pathway for xenobiotic substrates?
Glucuronidation
What is the main function of Phase I metabolism?
To prepare the compound for Phase II metabolism
Which enzyme is responsible for transferring glucuronic acid to the drug?
UDP-glucuronyl transferase
What is the most common phase I metabolic transformation?
Hydrolysis
Which of the following is a major pathway for cocaine metabolism?
Hydrolysis
Which conjugation pathway predominates at high substrate concentrations?
Glucuronidation
Which category of metabolic transformations involves the addition of endogenous compounds to a drug molecule?
Phase 2 metabolism
Which type of drugs require more metabolic transformations than hydrophilic drugs?
Lipid soluble drugs
Do all drugs require both phase 1 and phase 2 biotransformation?
No, some drugs do not require any biotransformation.
What is the main function of Phase I metabolism?
To increase water solubility of drugs
Which enzyme is responsible for the metabolism of a significant number of important drugs?
Cytochrome P450
What can a hydroxyl group or carboxyl group in a drug molecule be conjugated with to form a readily excretable compound?
Glucuronic acid
Which enzyme is responsible for the metabolism of approximately 50% of all clinically important drugs?
CYP2
What is the most common reaction catalyzed by cytochromes P450?
Oxidation
Which of the following is an example of phase I biotransformation?
Aromatic hydroxylation
Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?
Cytochrome P450
What is the result of N-demethylation of tertiary amines?
Oxidation of methyl attached to nitrogen
Which enzyme is responsible for transferring glucuronic acid to the drug?
Glucuronyl transferase
True or False: All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.
True
Which of the following is NOT a phase 1 biotransformation reaction?
Glucuronidation
True or False: The sulfhydryl group of glutathione is involved in the deactivation of reactive intermediates formed during biotransformation.
True
True or False: N-dealkylation is an oxidation reaction.
False
True or False: N-dealkylation of tertiary amines generally results in a product with the same activity and longer duration of action.
False
Which of the following is the main pathway of biotransformation of primary aromatic amines?
Acetylation
Which of the following is the main metabolic pathway for the drug mentioned in question 7?
Dealkylation
Which of the following is the main pathway of metabolism for drugs such as carbamazepine?
Hydroxylation
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.
True
Which of the following is the main pathway of biotransformation for primary aromatic amines?
N-acetylation
Which of the following is a phase I biotransformation?
Conversion of propranolol to 4-hydroxypropranolol
Which of the following is a phase II biotransformation?
Conversion of a drug to an acyl glucuronide
Which enzyme is responsible for the N-oxidation of primary aromatic amines?
Myeloperoxidase
Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?
CYP3A4
Which conjugation pathway is the most common phase 2 reaction?
Glucuronidation
Which enzyme is responsible for transferring glucuronic acid to the drug?
UDP-glucuronyl transferase (UGT)
Which ester group in the structure of Cocaine is readily hydrolyzed by esterases and why?
Methyl ester, because it is easily accessible
Which type of transformation is most prevalent in phase 1 metabolism?
Oxidation
Which organ has the highest metabolic capacity for drug biotransformation?
Liver
Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?
CYP2
Which enzyme is responsible for the metabolism of 1/3 of all important drugs?
CYP3A4
Which enzyme is involved in the oxidation of an alkyl group to a carboxylic acid?
CYP1A2
Which enzyme is responsible for the N-oxidation of primary aromatic amines?
CYP2D6
True or False: All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.
True
Which enzyme is responsible for the N-hydroxylation of procainamide?
Myeloperoxidase
Which of the following is a phase II biotransformation?
Glucuronidation
Which enzyme is responsible for transferring glucuronic acid to the drug?
UDP-glucuronyl transferase (UGT)
Which of the following is a common phase I metabolic transformation?
N-Dealkylation
Which enzyme is responsible for metabolizing approximately 50% of all clinically important drugs?
CYP2D6
Which of the following is the most common conjugative pathway for xenobiotic substrates?
Glucuronidation
Which phase of drug metabolism involves the addition of endogenous compounds to the drug molecule?
Phase 2 metabolism
What is the purpose of drug metabolism?
To remove drugs from the body
Which type of drugs require more metabolic transformations than hydrophilic drugs?
Highly lipid soluble drugs
Do all drugs require both phase 1 and phase 2 biotransformation?
No, some drugs require only phase 2 biotransformation
What is the main purpose of phase 1 transformations in drug metabolism?
To increase water solubility
Which of the following is NOT a phase 1 biotransformation reaction?
Conjugation
True or False: All drugs require both phase 1 and phase 2 biotransformation processes for their elimination from the body.
True
Which of the following is a phase I biotransformation?
Acetylation
Which enzyme is involved in the deactivation of reactive intermediates formed during biotransformation?
Glutathione S-transferase
What type of reaction is N-dealkylation?
Oxidation
Which enzyme is responsible for the metabolism of a significant number of important drugs?
Cytochrome P450
What can a hydroxyl group or carboxyl group in a drug molecule be conjugated with to form a readily excretable compound?
Glucuronic acid
Which of the following is the main pathway of biotransformation of primary aromatic amines?
Deamination
Which of the following is a phase I biotransformation?
Conversion of propranolol to 4-hydroxypropranolol
Which of the following is a phase II biotransformation?
Hydrolysis of aspirin
Which of the following is metabolized by dealkylation pathway?
C
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.
False
Which ester group in the structure of Cocaine is readily hydrolyzed by esterases and why?
A
RH + O2 + NADPH + H+ → ROH + H2O + NADP+ This is the most common reaction catalyzed by CYP450; a monooxygenase reaction.
True
One of the following phase 1 reactions do not present an inactive metabolite
-
Propranolol to 4-OH propranolol in Aromatic hydroxylation.
-
Diazepam Aromatic Hydroxylation
-
Codeine to Morphine
-
Biotransformation of Fenoprofen
3
Acetylation, Methylation do not hydrolyze in Phase II reaction, they are only there to terminate a reaction.
True
Quiz: Understanding Nitroso Intermediates and Adverse Effects Test your knowledge on nitroso intermediates and their implications in serious adverse effects such as agranulocytosis and Lupus. Learn about N-Acetyl Procainamide (NAPA) and its role in N-Acetylation and N-Acetyltransferase. Explore the impact of N-hydroxylation and Myeloperoxidase on procainamide. Discover why patients who are "slow
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