Amodiaquine – chemistry and use MCQs With Answer

Amodiaquine – chemistry and use MCQs With Answer

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Amodiaquine – chemistry and use MCQs With Answer

Amodiaquine is a 4‑aminoquinoline antimalarial used mainly in combination therapy for uncomplicated Plasmodium falciparum malaria. This introduction covers amodiaquine’s chemical class, structural relation to chloroquine, biotransformation to the active metabolite desethylamodiaquine, CYP2C8‑mediated metabolism, mechanism of action (inhibition of hemozoin formation), pharmacokinetics, adverse effects such as hepatotoxicity and agranulocytosis, and its clinical use in fixed‑dose combinations with artesunate. Keywords: Amodiaquine, chemistry, desethylamodiaquine, 4‑aminoquinoline, pharmacokinetics, CYP2C8, mechanism, adverse effects, artesunate, combination therapy. Now let’s test your knowledge with 30 MCQs on this topic.

Q1. What chemical class does amodiaquine belong to?

  • Macrolide
  • Sulfonamide
  • 4‑aminoquinoline
  • Tetracycline

Correct Answer: 4‑aminoquinoline

Q2. Which metabolite is primarily responsible for amodiaquine’s antimalarial activity?

  • Desethylamodiaquine
  • Amodiaquine glucuronide
  • Chloroquine
  • Primaquine

Correct Answer: Desethylamodiaquine

Q3. Which hepatic enzyme mainly catalyzes the N‑deethylation of amodiaquine?

  • CYP3A4
  • CYP2C8
  • CYP1A2
  • CYP2D6

Correct Answer: CYP2C8

Q4. What is the principal mechanism of action of amodiaquine against Plasmodium?

  • Inhibition of folate synthesis
  • Blockade of mitochondrial electron transport
  • Inhibition of hemozoin formation and heme detoxification
  • Inhibition of protein synthesis at the ribosome

Correct Answer: Inhibition of hemozoin formation and heme detoxification

Q5. Amodiaquine is most commonly used in combination with which antimalarial to form a WHO‑recommended ACT?

  • Sulfadoxine‑pyrimethamine
  • Artesunate
  • Mefloquine
  • Primaquine

Correct Answer: Artesunate

Q6. Which serious adverse effects are classically associated with amodiaquine therapy?

  • Nephrolithiasis and pancreatitis
  • Hepatotoxicity and agranulocytosis
  • Cardiac arrhythmias and ototoxicity
  • Hypoglycemia and alopecia

Correct Answer: Hepatotoxicity and agranulocytosis

Q7. Cross‑resistance between amodiaquine and which antimalarial is most commonly discussed?

  • Artemisinin
  • Chloroquine
  • Primaquine
  • Atovaquone

Correct Answer: Chloroquine

Q8. In pharmacokinetic terms, the active metabolite desethylamodiaquine is characterized by:

  • Extremely rapid clearance and negligible exposure
  • Short half‑life similar to artesunate
  • Longer terminal half‑life than the parent drug, providing prolonged activity
  • Complete renal excretion unchanged

Correct Answer: Longer terminal half‑life than the parent drug, providing prolonged activity

Q9. Which molecular target mutation in Plasmodium is most implicated in 4‑aminoquinoline resistance?

  • pfcrt K76T mutation
  • dhfr S108N mutation
  • cytochrome b Y268S mutation
  • kelch13 C580Y mutation

Correct Answer: pfcrt K76T mutation

Q10. Which of the following clinical monitoring parameters is most important during amodiaquine therapy?

  • Serum creatinine weekly
  • Complete blood count for neutropenia
  • Serial ECGs for QT prolongation
  • Blood glucose monitoring

Correct Answer: Complete blood count for neutropenia

Q11. Which formulation is commonly used for therapeutic administration of amodiaquine in combination therapy?

  • Intravenous solution
  • Topical cream
  • Oral fixed‑dose combination tablet with artesunate
  • Inhalation powder

Correct Answer: Oral fixed‑dose combination tablet with artesunate

Q12. A key chemical relationship between amodiaquine and chloroquine is that both:

  • Are sulfonamide derivatives
  • Belong to the 4‑aminoquinoline family
  • Are artemisinin derivatives
  • Are antifolate agents

Correct Answer: Belong to the 4‑aminoquinoline family

Q13. Which patient population requires extra caution or avoidance of amodiaquine due to increased risk of adverse effects?

  • Patients with severe renal impairment only
  • Pregnant women in the first trimester only
  • Patients with a history of liver disease or neutropenia
  • Children under 5 years always contraindicated

Correct Answer: Patients with a history of liver disease or neutropenia

Q14. Which drug interaction is most likely with amodiaquine due to CYP2C8 metabolism?

  • Induction by rifampicin increasing amodiaquine levels
  • Inhibition by gemfibrozil increasing desethylamodiaquine exposure
  • No interactions are known
  • Inhibition by proton pump inhibitors reducing activation

Correct Answer: Inhibition by gemfibrozil increasing desethylamodiaquine exposure

Q15. The primary route of elimination for the active metabolite desethylamodiaquine is most consistent with:

  • Renal excretion as unchanged drug
  • Hepatic metabolism followed by biliary excretion
  • Exhalation via the lungs
  • Rapid metabolism in plasma by esterases

Correct Answer: Hepatic metabolism followed by biliary excretion

Q16. Which laboratory finding would be most indicative of amodiaquine‑induced toxicity?

  • Elevated alkaline phosphatase only
  • Marked transaminase elevation with neutropenia
  • Isolated hyperbilirubinemia with normal blood counts
  • Thrombocytosis without liver enzyme changes

Correct Answer: Marked transaminase elevation with neutropenia

Q17. Which statement about the stability and storage of amodiaquine oral tablets is correct?

  • They require refrigerated storage at 2–8°C
  • They are highly photosensitive and must be stored in amber ampoules
  • They are stored at controlled room temperature, protected from moisture
  • They must be kept frozen to maintain potency

Correct Answer: They are stored at controlled room temperature, protected from moisture

Q18. In terms of stereochemistry and molecular action, amodiaquine’s antimalarial effect is primarily dependent on:

  • Specific chiral center configuration causing enzyme inhibition
  • Intercalation into parasite DNA exclusively
  • Accumulation in parasite digestive vacuole and interaction with heme
  • Blocking parasite cell wall synthesis

Correct Answer: Accumulation in parasite digestive vacuole and interaction with heme

Q19. For uncomplicated falciparum malaria, WHO‑recommended dosing of amodiaquine in fixed‑dose artesunate‑amodiaquine is typically:

  • A single dose of 30 mg/kg on day 1 only
  • 10 mg/kg once daily for 3 days (as amodiaquine base in combination)
  • 0.25 mg/kg daily for 14 days
  • 100 mg once weekly for 4 weeks

Correct Answer: 10 mg/kg once daily for 3 days (as amodiaquine base in combination)

Q20. Which resistance mechanism may reduce susceptibility specifically to amodiaquine and related drugs?

  • Overexpression of parasite dihydrofolate reductase
  • Mutations in pfmdr1 and pfcrt altering drug accumulation
  • Increased parasite aminotransferase activity
  • Altered host CYP2C8 activity

Correct Answer: Mutations in pfmdr1 and pfcrt altering drug accumulation

Q21. Which adverse effect would prompt immediate discontinuation of amodiaquine therapy?

  • Mild nausea for one day
  • Development of severe hepatic enzyme elevation and neutropenia
  • Transient headache after the first dose
  • Minor pruritus resolving without treatment

Correct Answer: Development of severe hepatic enzyme elevation and neutropenia

Q22. In medicinal chemistry, the 4‑aminoquinoline core of amodiaquine primarily contributes to:

  • High aqueous solubility for intravenous use
  • Interaction with heme in the parasite digestive vacuole
  • Inhibition of bacterial cell wall synthesis
  • Direct alkylation of parasite DNA

Correct Answer: Interaction with heme in the parasite digestive vacuole

Q23. Which statement best describes amodiaquine’s role in seasonal malaria chemoprevention (SMC) in some regions?

  • It is never used due to safety concerns
  • Used as monotherapy monthly for adults only
  • Used in combination regimens for children in high‑transmission seasons
  • Only administered intravenously for SMC

Correct Answer: Used in combination regimens for children in high‑transmission seasons

Q24. Which lab enzyme polymorphism in the host could alter amodiaquine metabolism and safety?

  • CYP2C8 polymorphisms affecting N‑deethylation
  • CYP2E1 polymorphisms causing rapid clearance
  • UGT1A1 polymorphisms causing increased glucuronidation
  • CYP4A11 polymorphisms altering renal excretion

Correct Answer: CYP2C8 polymorphisms affecting N‑deethylation

Q25. Which of the following is a pharmacodynamic property relevant to amodiaquine’s efficacy?

  • It requires coadministration with iron to be active
  • It acts as a prodrug that is activated extracorporeally
  • Its concentration in the parasite digestive vacuole determines activity
  • It works by chelating magnesium in the host plasma

Correct Answer: Its concentration in the parasite digestive vacuole determines activity

Q26. Which safety precaution is recommended before repeating amodiaquine therapy in the same patient?

  • No precautions are needed; repeat freely
  • Assess prior history of hepatotoxicity or neutropenia
  • Perform an exercise stress test
  • Administer a test dose intravenously

Correct Answer: Assess prior history of hepatotoxicity or neutropenia

Q27. In formulation development, improving amodiaquine oral bioavailability typically focuses on:

  • Reducing lipophilicity to prevent absorption
  • Optimizing salt form and dissolution characteristics
  • Converting to a topical ointment
  • Adding heavy metals to stabilize the molecule

Correct Answer: Optimizing salt form and dissolution characteristics

Q28. Which is a correct statement regarding use of amodiaquine in pregnancy?

  • It is absolutely contraindicated in all trimesters
  • Use is guided by risk–benefit assessment; some ACTs including amodiaquine combinations have been used in pregnancy
  • It enhances fetal growth and is recommended
  • It is only given via intramuscular injection in pregnancy

Correct Answer: Use is guided by risk–benefit assessment; some ACTs including amodiaquine combinations have been used in pregnancy

Q29. Which research area is important for improving amodiaquine’s clinical profile?

  • Design of injectable formulations for chronic use
  • Development of analogs with reduced hepatotoxicity and resistance susceptibility
  • Removal of the 4‑aminoquinoline core to improve potency
  • Ensuring it is coadministered with chloroquine always

Correct Answer: Development of analogs with reduced hepatotoxicity and resistance susceptibility

Q30. For B.Pharm students studying amodiaquine, which topics are critical to integrate for rational therapeutic use?

  • Only synthesis pathways without clinical context
  • Chemical structure, metabolism (CYP2C8), mechanism (hemozoin inhibition), safety (hepatotoxicity, neutropenia), and combination therapy principles
  • Pharmacy marketing strategies exclusively
  • Nutrition guidelines unrelated to drug action

Correct Answer: Chemical structure, metabolism (CYP2C8), mechanism (hemozoin inhibition), safety (hepatotoxicity, neutropenia), and combination therapy principles

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