101 Questions
True or False: All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.
False
Which phase of biotransformation is involved in the deactivation of reactive intermediates formed during drug metabolism?
Phase 2
Which pathway is involved in the metabolism of aspirin?
Phase 1 hydrolysis
True or False: N-dealkylation is an oxidation reaction.
True
What is the result of N-dealkylation of tertiary amines?
A product with decreased activity and shorter duration of action
Which phase of biotransformation involves the conjugation of drugs with glucuronic acid?
Phase 2
Which organ has the highest metabolic capacity for drug biotransformation?
Liver
Where are the phase I oxidative enzymes predominantly localized?
Endoplasmic reticulum
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 aromatic rings?
Cytochrome P450
Which enzyme is involved in the N-oxidation of primary aromatic amines?
Cytochrome P450
Which category of drug metabolism involves the addition of endogenous compounds to the drug molecule?
Phase 2 metabolism
Which type of transformation is most prevalent in phase 1 metabolism?
Oxidation
Which 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 metabolic transformations
What is the purpose of drug metabolism?
To remove/eliminate drugs from the body
Which phase of drug metabolism increases water solubility?
Phase 1 metabolism
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 of the following is the main metabolic pathway for the drug?
Acetylation
Which of the following is a common biotransformation pathway for secondary and tertiary amines?
Deamination
Which ester group in the structure of Cocaine is readily hydrolyzed by esterases?
The ester group on the methyl ester moiety
Which phase of metabolism introduces a new functional group or modifies an existing group?
Phase I metabolism
Which conjugative pathway is the most common and greatly increases water solubility of the conjugated product?
Glucuronidation
What is the major conjugation pathway for phenols, alcohols, and amines?
Sulfation
Which enzyme is responsible for transferring glucuronic acid to the drug?
UDP-glucuronyl transferase (UGT)
What is the most common phase 1 metabolic transformation?
Hydrolysis
Which phase of metabolism prepares the compound for phase II metabolism?
Phase I metabolism
Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?
CYP2
Which phase of biotransformation involves the conjugation of drugs with glucuronic acid?
Phase II
Which enzyme is responsible for the metabolism of 1/3 of all important drugs?
CYP3A4
Which enzyme is involved in the N-oxidation of primary aromatic amines?
Cytochrome P450
Which phase of metabolism prepares the compound for phase II metabolism?
Phase I
Which organ has the highest metabolic capacity for drug biotransformation?
Liver
Which type of biotransformation involves the addition of endogenous compounds to the drug molecule?
Phase 2 metabolism
Which phase of drug metabolism prepares the compound for phase II metabolism?
Phase 1 metabolism
Which phase of biotransformation involves the conjugation of drugs with glucuronic acid?
Phase 2 metabolism
Which enzyme is responsible for transferring glucuronic acid to the drug?
Glucuronosyltransferase
Which phase of metabolism increases the water solubility of drug molecules?
Phase 1 metabolism
Do all drugs require both phase 1 and phase 2 biotransformation?
Depends on the drug
Which of the following is a phase I biotransformation pathway that involves hydrolysis?
O-dealkylation
Which enzyme is responsible for the N-hydroxylation of procainamide?
Myeloperoxidase
Which of the following is a phase II biotransformation pathway?
Glucuronidation
Which of the following is a common metabolic pathway for secondary and tertiary amines?
N-dealkylation
Which enzyme is responsible for transferring glucuronic acid to drugs?
UDP-glucuronyl transferase
Which of the following is a major conjugation pathway for phenols, alcohols, and amines?
Sulfation
True or False: Glutathione conjugation is a phase II biotransformation process.
True
Which enzyme is involved in N-acetylation of primary amino groups?
N-acetyltransferase
What is the main metabolic product of p-aminosalicylic acid?
N-acetylated PAS
Which amino acid is commonly used for conjugation with xenobiotics?
Glycine
True or False: Acetylation increases the water solubility of drugs.
False
Which enzyme is responsible for the formation of amide or peptide bonds during amino acid conjugation?
Glutamine synthetase
Which of the following is the main pathway of biotransformation for 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?
Conversion of a drug to an acyl glucuronide
Which of the following is the main metabolic pathway for the drug?
Dealkylation
Which of the following is a common biotransformation pathway for secondary and tertiary amines?
Hydroxylation
Which ester group in the structure of Cocaine is readily hydrolyzed by esterases and why?
The ester group on the methyl benzoate moiety
Which of the following is a phase I biotransformation pathway that involves hydrolysis?
N-Dealkylation
Which of the following is a phase II biotransformation pathway?
Glucuronidation
Which enzyme is responsible for transferring glucuronic acid to drugs?
UDP-glucuronyl transferase
Which of the following is a common metabolic pathway for secondary and tertiary amines?
N-Dealkylation
Which phase of drug metabolism introduces a new functional group or modifies an existing group?
Phase I metabolism
Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?
CYP3A4
True or False: All drugs require phase 1 and phase 2 biotransformation processes for their elimination from the body.
True
Which phase of biotransformation is involved in the deactivation of reactive intermediates formed during drug metabolism?
Phase 2
Which enzyme is responsible for the formation of amide or peptide bonds during amino acid conjugation?
Glutathione S-transferase
True or False: N-dealkylation is an oxidation reaction.
True
Which enzyme is responsible for the metabolism of 1/3 of all important drugs?
Cytochrome P450
Which phase of drug metabolism increases water solubility?
Phase 2
Which of the following is a phase 2 biotransformation?
Conjugation
True or False: Acetylation increases the water solubility of drugs.
False
Which enzyme is responsible for transferring glucuronic acid to drugs?
Glucuronyl transferase
Which organ has the highest metabolic capacity for drug biotransformation?
Liver
Which phase of drug metabolism prepares the compound for phase II metabolism?
Phase 1 metabolism
Which enzyme family is responsible for metabolizing approximately 50% of all clinically important drugs?
Cytochrome P450
Which of the following organs have significant metabolic capacity for drug biotransformation?
Liver and gastrointestinal tract
Which site is predominantly responsible for the localization of phase I oxidative enzymes?
The endoplasmic reticulum
Which cytochrome P450 family is responsible for metabolizing approximately 50% of all clinically important drugs?
CYP2
Which enzyme is responsible for the metabolism of one-third of all important drugs?
Cytochrome P450
Which functional groups can be introduced into a wide variety of compounds by cytochromes P450?
Aromatic rings and aliphatic chains
Which enzyme is involved in the oxidation of alkenes to epoxides?
Cytochrome P450
Which of the following is the main pathway of biotransformation for primary aromatic amines?
Oxidation
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 of the following is metabolized by dealkylation pathway?
A
The structure of Cocaine contains two ester groups. Which of these groups is readily hydrolyzed by esterases and why?
A
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
The following biotransformation takes place in Phase I
reduction
Phase II reaction involving glucuronic acid takes place in
the cytosol
Phase I reaction involving CYP450 takes place in, a monooxygenase reaction
Endoplasmic Reticulum
One of the following medications is converted to an active metabolite after Phase I Reaction
A and B
Conversion of propranolol by Phase I reaction produces an active metabolite called
4-OH propranolol
Codeine converts to an active (morphine metabolite) in Phase 1 reaction by N-demethylation
True
Which one of the following uses Cytochrome P 450 family called CYP3A4 in Phase I
Dealkylation of secondary and tertiary amines, Tegretol, Diazepam, Imipramine
VS.-Para location is the most preferred location for Aromatic hydroxylation in molecules with steric hindrance groups and electron donating groups
True
Ketoprofen has no aromatic hydroxylation.
True
Most Aromatic Oxidations first produces ______________ which is highly (reactive, toxic and carcinogenic) metabolites; this later reacts with________________ making the product non toxic by deactivation.
_____________________it undergoes ____________to a metabolite in aplastic anemia and undergoes __________, therefore repeated doses will bring about decreased half life.
One of the following actions are used to terminate actions.
Acetylation and Methylation in Phase II
Quiz: Understanding the Role of Nitroso Intermediates in Adverse Effects Test your knowledge on the connection between nitroso intermediates and serious adverse effects such as agranulocytosis and Lupus. Learn about the role of N-Acetyl Procainamide (NAPA), N-Acetylation, N-Acetyltransferase, and N-hydroxylation in the development of these side effects. Discover how the acetylation rate affects the generation of nit
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