Chemotherapy: Antiprotozoal

Question 1

Melarsen

Uses?

Answer 1

Arsenic compound
Selectively accumulated in Trypanosoma species, inhibits energy metabolism.
Used for treatment of human sleeping sickness etc

Question 2

Suramin

Uses?

Answer 2

Introduced in 1920s, remains drug of choice for human trypanosomiasis
Does not contain toxic metal-> much higher therapeutic index than melarsen
Molecular mechanism unknown, might act on glycolytic enzymes

Question 3

Amphotericin B

Answer 3

Polyene antifungal and antiprotozoal drug

Forms pores in membrane by ergosterol-dependent mechanism

Question 4

Miconazole

Answer 4

Imidazole antifungal and antiprotozoal drug

Inhibits ergosterol biosynthesis

Question 5

Chloroquine

Answer 5

Antimalarial 4-aminoquinoline drug

Inhibits heme polymerisation in food vacuole of Plasmodium

Question 6

Mefloquine

Answer 6

Antimalarial 4-aminoquinoline drug

Inhibits heme polymerisation in food vacuole of Plasmodium

Question 7

Artemisinin

Mode of action?

Answer 7

Produg- metabolised to dihydroartemisinin.
Active during stage when parasite is located inside RBCs
Mode of action may be based on production of oxygen radicals

Question 8

Sulfadoxin

Analogue of?

Answer 8

Sulfa drug
Inhibits DHPS in Plasmodium
Analogue of antibiotic sulfamethoxazole

Question 9

Pyrimethamine

Analogue of?

Answer 9

Inhibits DHFR in Plasmodium

Analogue of antibiotic trimethoprim

Question 10

Fansidar

Analogous to?
Uses?

Answer 10

Combination of sulfadoxin & pyrimethamine (analogous to antibacterial co-trimoxazole)
Used in treatment of patients with P.falciparum malaria where chloroquine resistance is suspected.
Oral treatment

Question 11

Tetracycline

Answer 11

-

Question 12

Lincomycin

Answer 12

-