5. Antimalarial drugs
Gametocytic form Primaquine
Exoerythrocytic form Primaquine
Erythrocytic form Artemisinin, Chloroquine, Quinine,
Mefloquine, Pyrimethamine
Primaquine is a tissue schizonticide
Chloroquine is a blood schizonticide
6. Primaquine
MOA ā oxidant responsible for
schizonticidal action, hemolysis
and methemoglobenemia
PK ā PO administration, eliminated
by kidney
AE - drug induced anemia in G6PD
granulocytopenia, agranulocytosis
CI - pregnancy
Quinine, Quinidine
MOA ā interfere with heme polymerization
leading to death of erythrocytic form of
plasmoidal parasite
PK ā PO. Can reach fetus (fetotoxic). Alk
of urine decreases secretion
AE ā Cinchonism NVTnVr
CI - +ve Coombās test for haemolytic anem
DI ā antiacids, digoxin
7. Chloroquine side effects
āŖ Seizures
āŖ Hear reactions: deafness or tinnitus
āŖ Gastrointestinal reactions: nausea, vomiting, diarrhea, abdominal
cramps, and anorexia
āŖ Brain reactions: mild and transient headache
āŖ Skin reactions: itchiness, skin color changes, hair loss, and skin
rashes
āŖ Unpleasant metallic taste
āŖ chloroquine retinopathy
8. ā¢Antacids- may reduce absorption of chloroquine; take 4
hours apart
ā¢Kaolin- may reduce absorption of chloroquine; take 4
hours apart
ā¢Cimetidine- may inhibit metabolism of chloroquine;
increasing levels of chloroquine in the body
ā¢Ampicillin- levels may be reduced by chloroquine; take 2
hours apart
ā¢Cyclosporine- levels may be increased by chloroquine
ā¢Mefloquine- may increase risk of convulsions
Drug interactions with Chloroquine