Antimalarial drugs – classification and mechanism MCQs With Answer
Antimalarial drugs encompass diverse classes—quinolines, artemisinins, antifolates, 8‑aminoquinolines, atovaquone combinations and antibiotics—each with distinct mechanisms such as inhibition of heme polymerization, generation of free radicals, DHFR/DHPS blockade and cytochrome bc1 inhibition. Understanding blood schizonticides, tissue schizonticides, gametocytocidal and hypnozoitocidal actions, pharmacokinetics, resistance mechanisms (pfcrt, cytochrome b, DHFR mutations) and safety issues (G6PD deficiency, pregnancy, neurocardiac effects) is essential for B.Pharm students. This concise, keyword‑rich primer prepares you for clinical application and exam questions. Now let’s test your knowledge with 30 MCQs on this topic.
Q1. Which of the following is a 4‑aminoquinoline antimalarial?
- Chloroquine
- Mefloquine
- Primaquine
- Artemisinin
Correct Answer: Chloroquine
Q2. The primary mechanism of action of chloroquine is:
- Inhibition of dihydrofolate reductase
- Generation of free radicals via endoperoxide cleavage
- Inhibition of heme polymerization (hemozoin formation)
- Blockade of mitochondrial cytochrome bc1 complex
Correct Answer: Inhibition of heme polymerization (hemozoin formation)
Q3. Artemisinin derivatives exert antimalarial activity mainly by:
- Reversible inhibition of protein synthesis
- Cleavage of an endoperoxide bridge producing free radicals
- Competitive antagonism at dihydropteroate synthase
- Direct inhibition of plasmodial DNA gyrase
Correct Answer: Cleavage of an endoperoxide bridge producing free radicals
Q4. Which drug primarily inhibits plasmodial dihydrofolate reductase (DHFR)?
- Pyrimethamine
- Sulfadoxine
- Atovaquone
- Quinine
Correct Answer: Pyrimethamine
Q5. Atovaquone’s antimalarial mechanism targets:
- Heme polymerization
- Mitochondrial cytochrome bc1 complex (electron transport)
- Folate synthesis at DHPS
- 30S ribosomal subunit
Correct Answer: Mitochondrial cytochrome bc1 complex (electron transport)
Q6. Which antimalarial is effective against hypnozoites of Plasmodium vivax and P. ovale?
- Chloroquine
- Primaquine
- Mefloquine
- Doxycycline
Correct Answer: Primaquine
Q7. A major adverse effect of primaquine is hemolysis in patients with:
- Porphyria
- G6PD deficiency
- Renal failure
- Hyperthyroidism
Correct Answer: G6PD deficiency
Q8. Which combination is commonly recommended for treatment and prophylaxis of chloroquine‑resistant P. falciparum?
- Chloroquine plus primaquine
- Atovaquone‑proguanil
- Sulfadoxine alone
- Dapsone monotherapy
Correct Answer: Atovaquone‑proguanil
Q9. Which antimalarial is primarily gametocytocidal against mature P. falciparum and used to reduce transmission?
- Artemether
- Primaquine
- Chloroquine
- Doxycycline
Correct Answer: Primaquine
Q10. Chloroquine resistance in P. falciparum is most commonly associated with mutations in:
- pfcrt gene (chloroquine resistance transporter)
- dhfr gene
- cytochrome b gene
- 16S rRNA
Correct Answer: pfcrt gene (chloroquine resistance transporter)
Q11. Doxycycline’s antimalarial action is mainly due to inhibition of:
- Plasmodial DHFR
- 30S ribosomal subunit protein synthesis
- Heme polymerization
- Plasmodial fatty acid synthase
Correct Answer: 30S ribosomal subunit protein synthesis
Q12. Which antimalarial is well known for neuropsychiatric adverse effects?
- Mefloquine
- Chloroquine
- Artesunate
- Sulfadoxine
Correct Answer: Mefloquine
Q13. For malaria prophylaxis in pregnancy in areas with chloroquine‑sensitive malaria, the preferred drug is:
- Primaquine
- Chloroquine
- Doxycycline
- Atovaquone‑proguanil
Correct Answer: Chloroquine
Q14. Which drug is classified as a tissue schizonticide (acts on hepatic stages)?
- Primaquine
- Quinine
- Lumefantrine
- Chloroquine
Correct Answer: Primaquine
Q15. In the combination sulfadoxine‑pyrimethamine, sulfadoxine inhibits:
- Dihydrofolate reductase (DHFR)
- Dihydropteroate synthase (DHPS)
- Cytochrome bc1
- Heme polymerization
Correct Answer: Dihydropteroate synthase (DHPS)
Q16. The partner drug lumefantrine primarily works by:
- Inhibiting heme polymerization similar to quinolines
- Inhibiting mitochondrial DNA replication
- Blocking folate uptake
- Stimulating host immune clearance
Correct Answer: Inhibiting heme polymerization similar to quinolines
Q17. Cinchonism (tinnitus, headache, visual disturbance) is classically associated with overdose of:
- Quinine
- Primaquine
- Atovaquone
- Doxycycline
Correct Answer: Quinine
Q18. Which drug is contraindicated in pregnancy because of risk to the fetus due to hemolysis if the fetus is G6PD deficient?
- Primaquine
- Chloroquine
- Mefloquine
- Artesunate
Correct Answer: Primaquine
Q19. Long‑term use of pyrimethamine can cause hematological toxicity due to:
- Folate antagonism leading to megaloblastic anemia
- Direct bone marrow toxicity unrelated to folate
- Excess iron chelation
- Severe hemolysis in all patients
Correct Answer: Folate antagonism leading to megaloblastic anemia
Q20. The drug of choice for severe falciparum malaria requiring IV therapy is:
- IV artesunate
- Oral chloroquine
- IM mefloquine
- Oral doxycycline
Correct Answer: IV artesunate
Q21. Tafenoquine belongs to which antimalarial class?
- 4‑aminoquinolines
- 8‑aminoquinolines
- Artemisinins
- Antifolates
Correct Answer: 8‑aminoquinolines
Q22. Resistance to atovaquone most commonly arises from mutations in:
- pfcrt gene
- Plasmodial cytochrome b gene
- DHFR gene
- rRNA gene
Correct Answer: Plasmodial cytochrome b gene
Q23. Which of the following is an artemisinin derivative used in ACTs?
- Artesunate
- Sulfadoxine
- Halofantrine
- Primaquine
Correct Answer: Artesunate
Q24. Which antimalarial is well known to cause prolongation of the QT interval and is cardiotoxic at high doses?
- Halofantrine
- Chloroquine
- Doxycycline
- Pyrimethamine
Correct Answer: Halofantrine
Q25. A commonly used fixed‑dose artemisinin‑based combination therapy (ACT) is:
- Artemether‑lumefantrine
- Chloroquine‑primaquine
- Pyrimethamine‑atovaquone
- Sulfadoxine‑mefloquine
Correct Answer: Artemether‑lumefantrine
Q26. Which antimalarial also has a clinically important use as an antiarrhythmic agent (historical/related compound)?
- Quinidine
- Primaquine
- Atovaquone
- Mefloquine
Correct Answer: Quinidine
Q27. Which drug combination interferes with folate synthesis and is used as intermittent preventive therapy in pregnancy in some settings?
- Sulfadoxine‑pyrimethamine
- Atovaquone‑proguanil
- Chloroquine‑primaquine
- Artemether‑lumefantrine
Correct Answer: Sulfadoxine‑pyrimethamine
Q28. Which laboratory method or marker is most specific for detecting chloroquine resistance mutations in P. falciparum?
- pfcrt gene PCR mutation analysis
- Peripheral eosinophil count
- Serum bilirubin measurement
- Urine heme test
Correct Answer: pfcrt gene PCR mutation analysis
Q29. Which antimalarial class includes drugs that are primarily blood schizonticides (active against erythrocytic stages)?
- 8‑aminoquinolines only
- Quinolines and artemisinins
- Antifolates only
- All antibiotics
Correct Answer: Quinolines and artemisinins
Q30. Which antimalarial should be avoided in children under 8 years due to effects on teeth and bone growth?
- Doxycycline
- Chloroquine
- Primaquine
- Artesunate
Correct Answer: Doxycycline

I am a Registered Pharmacist under the Pharmacy Act, 1948, and the founder of PharmacyFreak.com. I hold a Bachelor of Pharmacy degree from Rungta College of Pharmaceutical Science and Research. With a strong academic foundation and practical knowledge, I am committed to providing accurate, easy-to-understand content to support pharmacy students and professionals. My aim is to make complex pharmaceutical concepts accessible and useful for real-world application.
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