Malaria Drugs

Question 1

Name the 4 categories or classes of malaria drugs.

Answer 1

Quinolone derivatives, artemisinin compounds, antifolates, and antibiotics

Question 2

Name the 5 quinolone derivatives.

Answer 2

Quinine/quinidine, chloroquine, hydroxychloroquine, mefloquine, primaquine

Question 3

Which 4 quinolone derivatives are believed to accumulate in food vacuoles, disrupt heme polymerization to hemozoin, and cause oxidative damage to Plasmodium parasites?

Answer 3

Quinine/quinidine, chloroquine, hydroxychloroquine, mefloquine

Question 4

Which quinolone derivative functions by forming quinolone-quinone intermediates that oxidize schizont membranes, and is therefore the only drug that inhibits exoerythrocytic schyzogony (reproduction outside the RBCs)?

Answer 4

Primaquine

Question 5

What are 4 therapeutic functions of all the quinolone derivatives?

Answer 5

Malaria prophylaxis, treatment of acute malaria attacks, rheumatoid arthritis therapy, and SLE therapy

Question 6

Which quinolone derivative can cause side effects of temporary deafness, hypotension, hypoglycemia, abortion, and arrhythmias?

Answer 6

Quinine/quinidine

Question 7

What term refers to the temporary deafness, tinnitus, headache, dizziness, and rash that can follow quinine use?

Answer 7

Cinchonism

Question 8

Which quinolone derivative can cause side effects of itching and retinitis?

Answer 8

Chloroquine

Question 9

Which quinolone derivative can cause side effects of nausea, fever, vomiting, methemoglobinemia, and hemolysis in patients with G6PD deficiency?

Answer 9

Primaquine (although all the quinolones can cause G6PD deficiency hemolytic anemia)

Question 10

What drug is used in combination with chloroquine to treat chloroquine-resistant malaria? How does its positive charge help make Plasmodium chloroquine-sensitive?

Answer 10

Amantadine; it binds to the parasite pores to prevent chloroquine efflux

Question 11

Name the 2 artemisinin compounds. Which one can cause side effects of neurotoxicity and prolonged QT interval?

Answer 11

Artesunate and artemether; artesunate

Question 12

Name the 2 antifolate malaria drugs. What enzyme do they inhibit in both humans and parasites?

Answer 12

Pyrimethamine and chloroguanide/proguanil; inhibit DHFR (dihydrofolate reductase)

Question 13

The artemisinin compounds, artesunate and artemether, specifically target what organelle of which Plasmodium species?

Answer 13

SERCA (sarco/endoplasmic reticulum Ca/ATPase) of P. falciparum

Question 14

Name the 3 “supplementary” malaria drugs that are only used in combination regimens. Which 3 drugs do they supplement?

Answer 14

Amantadine, lumefantrine, and atovaquone; used with chloroquine, artemether, and chloroguanide, respectively

Question 15

What aminoalcohol malaria drug, also called benflumetol or coartem, is only used in conjunction with artemether?

Answer 15

Lumefantrine

Question 16

What napthalene malaria drug is used in conjunction with proguanil for prophylaxis and treatment of P. falciparum, including for chloroquine-resistant strains?

Answer 16

Atovaquone

Question 17

The napthalene atovaquone specifically targets what organelle of which Plasmodium species?

Answer 17

Mitochondria of P. falciparum (mitochondrial depolarization inhibits electron transport)

Question 18

Name 3 antibiotics that can be used to treat severe or chloroquine-resistant uncomplicated malaria.

Answer 18

Clindamycin, tetracycline, and doxycycline

Question 19

How do doxycycline and tetracycline inhibit Plasmodium function? Which one can cause photosensitivity as a side effect?

Answer 19

Inhibit protein synthesis; doxycycline