Q1. Which of the following statements is NOT true about Phase I biotransformation reactions?
a) They introduce or expose functional groups on drugs.
b) They can increase the polarity of drugs.
c) They always make drugs more water-soluble.
d) They prepare drugs for further metabolism in Phase II.
e) Oxidation, reduction, and hydrolysis are the primary reactions.
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C
This is not always true.
Q2. The most common Phase I reaction, primarily catalyzed by CYP450 enzymes, involves:
a) Gain of electrons by the drug molecule.
b) Removal of amine groups from the drug molecule.
c) Addition of oxygen or removal of hydrogen atoms from the drug molecule.
d) Cleavage of bonds in the drug molecule by water.
e) All of the above.
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C
This is the function of oxidation
Q3. N-dealkylation, where an alkyl group is removed from nitrogen, is an example of which Phase I reaction?
a) Oxidation
b) Reduction
c) Hydrolysis
d) None of the above
e) Requires further information
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D
N-dealkylation is a specific type of oxidation
Q4. Which of the following drugs undergoes conversion to morphine during Phase I biotransformation?
a) Acetaminophen
b) Aspirin
c) Codeine
d) Lidocaine
e) Sulfadiazine
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C
Codeine is converted to morphine
Q5. In the hydrolysis reaction converting aspirin to salicylic acid, which enzyme is involved?
a) Cytochrome P450
b) Reductase
c) Esterase
d) Amidase
e) Dehydrogenase
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C
Esterase is responsible for ester hydrolysis
Q6. Which of the following statements about Phase II biotransformation reactions is NOT correct?
A) Phase II reactions involve the conjugation of drugs with an endogenous substance to form water-soluble metabolites.
B) The primary purpose of Phase II reactions is to increase the polarity of drugs and their metabolites to facilitate renal excretion.
C) Glucuronidation, sulfation, and acetylation are examples of Phase II biotransformation reactions.
D) Phase II reactions are typically catalyzed by cytochrome P450 enzymes.
E) Glutathione conjugation is an important Phase II reaction that helps in detoxifying reactive metabolites.
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D
Option D is incorrect because cytochrome P450 enzymes are primarily involved in Phase I reactions.
Q7. Which of the following is a primary enzyme involved in glucuronidation?
A) Cytochrome P450
B) UDP-glucuronosyltransferase
C) N-acetyltransferase
D) Glutathione S-transferase
E) Sulfotransferase
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B
Q8. Phase II biotransformation reactions primarily occur in which organ?
A) Kidney
B) Liver
C) Lungs
D) Heart
E) Brain
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B
Q9. Which of the following Phase II reactions involves the addition of a sulfate group to a drug?
A) Glucuronidation
B) Sulfation
C) Acetylation
D) Methylation
E) Glutathione conjugation
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B
Q10. Which of the following is NOT typically a result of Phase II biotransformation?
A) Increased drug polarity
B) Decreased drug toxicity
C) Enhanced renal excretion
D) Formation of reactive intermediates
E) Inactivation of active drugs
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D
Q11. The conjugation of drugs with glutathione primarily serves to:
A) Increase the lipid solubility of drugs
B) Decrease the renal excretion of drugs
C) Detoxify reactive intermediates
D) Increase the duration of drug action
E) Convert drugs into active metabolites
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C
Q12. Which Phase II enzyme is responsible for the conjugation of small endogenous molecules such as acetyl groups to drugs, making them more water-soluble?
A) UDP-glucuronosyltransferase (UGT)
B) N-acetyltransferase (NAT)
C) Glutathione S-transferase (GST)
D) Sulfotransferase (SULT)
E) Methyltransferase
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B
Q13. Which of the following statements about glucuronidation is true?
A) It only occurs in the liver.
B) It always leads to the formation of inactive metabolites.
C) It is an energy-dependent process requiring UDP-glucuronic acid.
D) It is less common than sulfation in drug metabolism.
E) It cannot occur for drugs that contain a hydroxyl group.
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C
Q14. The biotransformation of acetaminophen involves which of the following Phase II pathways as a key detoxification route?
A) Glucuronidation only
B) Sulfation only
C) Glutathione conjugation
D) Acetylation
E) Methylation
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C
Q15. In which condition is the rate of glucuronidation likely to be reduced, potentially leading to drug toxicity?
A) Chronic renal failure
B) Hypothyroidism
C) Hepatic cirrhosis
D) Asthma
E) Hyperlipidemia
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C
Q16. Which Phase II reaction is primarily involved in the metabolism of isoniazid, a drug used to treat tuberculosis?
A) Glucuronidation
B) Sulfation
C) Acetylation
D) Methylation
E) Glutathione conjugation
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C
Q17. Which cofactor is essential for the function of sulfotransferases in Phase II biotransformation?
A) UDP-glucuronic acid
B) Glutathione
C) Acetyl-CoA
D) S-adenosylmethionine (SAM)
E) 3'-Phosphoadenosine-5'-phosphosulfate (PAPS)
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E
Q18. Which of the following factors can lead to increased glucuronidation activity?
A) Advanced age
B) Liver disease
C) Genetic polymorphisms leading to slower enzyme activity
D) Induction by certain drugs or dietary components
E) Renal impairment
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D
Q19. Which of the following factors can lead to increased glucuronidation activity?
A) UDP-glucuronosyltransferase (UGT)
B) N-acetyltransferase (NAT)
C) Glutathione S-transferase (GST)
D) Sulfotransferase (SULT)
E) Methyltransferase
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C
Q20. Which Phase II reaction is commonly involved in the metabolism of bilirubin, a breakdown product of heme?
A) Glucuronidation
B) Sulfation
C) Acetylation
D) Methylation
E) Glutathione conjugation
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A
Q21. Which of the following statements about Phase II reactions is true?
A) They involve the addition of hydroxyl groups to drugs.
B) They primarily occur in the endoplasmic reticulum of cells.
C) They convert lipophilic drugs into more lipophilic metabolites.
D) They do not require cofactors for enzymatic activity.
E) They generally produce inactive metabolites.
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E
Q22. The metabolism of which of the following drugs primarily involves glucuronidation and sulfation pathways?
A) Acetaminophen
B) Morphine
C) Warfarin
D) Isoniazid
E) Amiodarone
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A
Q23. Which Phase II enzyme system is responsible for the methylation of catecholamines and other drugs?
A) UDP-glucuronosyltransferase (UGT)
B) N-acetyltransferase (NAT)
C) Glutathione S-transferase (GST)
D) Sulfotransferase (SULT)
E) Methyltransferase
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E
Q24. The Phase II biotransformation pathway involving glucuronidation is often saturable and can be influenced by:
A) pH of the environment
B) Concentration of endogenous substances
C) Presence of other drugs
D) Temperature of the body
E) Size of the organ
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C
Q25. Which Phase II enzyme system is primarily responsible for the conjugation of drugs with glucuronic acid, increasing their water solubility and facilitating their elimination?
A) UDP-glucuronosyltransferase (UGT)
B) N-acetyltransferase (NAT)
C) Glutathione S-transferase (GST)
D) Sulfotransferase (SULT)
E) Methyltransferase
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A
Q26. In Phase II biotransformation, the formation of mercapturic acid conjugates is associated with which enzyme system?and facilitating their elimination?
A) UDP-glucuronosyltransferase (UGT)
B) N-acetyltransferase (NAT)
C) Glutathione S-transferase (GST)
D) Sulfotransferase (SULT)
E) Methyltransferase
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C
Q27. A deficiency in which Phase II enzyme system can lead to reduced metabolism of estrogens and other endogenous compounds, potentially affecting hormone levels?
A) UDP-glucuronosyltransferase (UGT)
B) N-acetyltransferase (NAT)
C) Glutathione S-transferase (GST)
D) Sulfotransferase (SULT)
E) Methyltransferase
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A
Q28. The metabolism of which of the following drugs primarily involves both glucuronidation and sulfation pathways?
A) Diazepam
B) Lidocaine
C) Warfarin
D) Acetaminophen
E) Morphine
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D
Q29. Which of the following is a MAJOR pathway for the inactivation and detoxification of xenobiotics (foreign chemicals) in the body?
A. Oxidation by CYP450 enzymes
B. Hydrolysis by esterases
C. Reduction by reductases
D. Decarboxylation
E. All of the above
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A
Q30. A patient with liver cirrhosis is likely to have a:
A. Decreased metabolism of most drugs
B. Increased metabolism of most drugs
C. No change in drug metabolism
D. Increased metabolism of fat-soluble drugs
E. Increased metabolism of water-soluble drugs
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A
Q31. Which of the following factors can influence drug metabolism?
A. Age
B. Genetics
C. Liver disease
D. All of the above
E. Only A and B
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D
Q32. CYP3A4 is a major drug-metabolizing enzyme. Which of the following statements about CYP3A4 is FALSE?
A. It is located primarily in the liver
B. It can be inhibited by some medications
C. It can be induced by some medications and environmental factors
D. It metabolizes a wide variety of drugs
E. It is the only CYP450 enzyme involved in drug metabolism
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E
Q33. Drug-drug interactions can occur when two medications compete for the same metabolic pathway. This can lead to:
A. Increased blood levels of one or both drugs
B. Decreased blood levels of one or both drugs
C. Both A and B
D. No change in blood levels of either drug
E. Increased toxicity of a non-metabolized drug
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C
Q34. A drug containing an alcohol group is most likely to undergo:
A. Oxidation to an aldehyde or carboxylic acid
B. Reduction to a ketone
C. Hydrolysis
D. Conjugation
E. Decarboxylation
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A
Q35. A drug with a high protein binding percentage will have a:
A. Larger volume of distribution
B. Smaller volume of distribution
C. No change in volume of distribution
D. Faster elimination rate
E. Slower elimination rate
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A
Q36. The primary route of excretion for most water-soluble drug metabolites is through the:
A. Kidneys
B. Liver
C. Lungs
D. Skin
E. Feces
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A
Q37. What is the primary cause of acetaminophen toxicity at high doses?
A. Glucuronidation metabolism
B. Sulfate conjugation
C. Glutathione conjugation
D. Glycine conjugation
E. Hydroxylation
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C
Q38. Fluconazole is known for its interaction with which enzyme system?
A. CYP3A4 inhibitor
B. CYP3A4 substrate
C. CYP3A4 inducer
D. CYP2C9 substrate
E. CYP1A2 inhibitor
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A
Q39. Which factor does NOT affect drug metabolism in the liver?
A. tissue binding
B. changes with liver blood circulation
C. changes with intrinsic activity
D. chronic liver diseases
E. Oxidative metabolism catalyzed by cytochrome CYP450
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A
Q40. Which medication combination poses an increased risk of myopathy when used with simvastatin?
A. Azithromycin
B. Nifedipine
C. Fluconazole
D. Diltiazem
E. No effect. Can take safely.
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D
When taken together, diltiazem increases the levels of these statins in your body. This can increase the risk of statin-related side effects, like muscle pain or damage.
Q41. Smoking affects drug metabolism primarily by acting as a:
A. Enzyme inhibitor
B. Enzyme substrate
C. Cytochrome polymorphism inducer
D. Enzyme inducer
E. Enzyme inhibitor and substrate
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D
CYP1A2 inducer