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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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