Comparative Pharmacology
Head-to-head clinical analysis: ARTESUNATE versus QUININE.
Head-to-head clinical analysis: ARTESUNATE versus QUININE.
ARTESUNATE vs Quinine
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Artesunate is a water-soluble artemisinin derivative that produces rapid parasite clearance. It is converted in vivo to dihydroartemisinin, which generates free radicals that alkylate and damage parasite proteins, particularly targeting the sarcoplasmic/endoplasmic reticulum calcium ATPase (SERCA) of Plasmodium species.
Quinine is a cinchona alkaloid that acts as a blood schizonticide against Plasmodium falciparum. It inhibits heme polymerase, leading to accumulation of toxic heme, and disrupts parasite membrane integrity. It also has mild analgesic and antipyretic properties.
2.4 mg/kg IV at 0, 12, 24, and 48 hours, then daily until oral therapy can be initiated.
Adults: 648 mg (2 capsules) orally every 8 hours for 7 days for uncomplicated chloroquine-resistant malaria, typically used in combination with other antimalarials.
None Documented
None Documented
Clinical Note
moderateQuinine + Gatifloxacin
"Quinine may increase the hypoglycemic activities of Gatifloxacin."
Clinical Note
moderateQuinine + Rosoxacin
"Quinine may increase the hypoglycemic activities of Rosoxacin."
Clinical Note
moderateQuinine + Levofloxacin
"Quinine may increase the hypoglycemic activities of Levofloxacin."
Clinical Note
moderateQuinine + Trovafloxacin
"Quinine may increase the hypoglycemic activities of Trovafloxacin."
Terminal elimination half-life of artesunate is approximately 1 hour. The active metabolite dihydroartemisinin has a half-life of 1-2 hours. This short half-life supports rapid parasite clearance in severe malaria.
Terminal elimination half-life: 18 hours (range 8–21 h) in healthy adults; prolonged to 26–44 h in severe malaria or hepatic impairment.
Primarily hepatic metabolism; renal excretion of metabolites accounts for <10% as unchanged drug. Biliary/fecal elimination is minimal. ~80% of the dose is recovered in urine as metabolites, mainly dihydroartemisinin.
Renal: ~20% unchanged; Hepatic metabolism (CYP3A4) to inactive metabolites, excreted in urine and feces. Total renal elimination of parent and metabolites ~80%.
Category C
Category C
Antimalarial
Antimalarial