Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
Piperaquine is being developed as a long-acting component in artemisinin combination therapies. It was highly active in vitro and drug interaction studies showed that dihydroartemisinin combinations with piperaquine, chloroquine, and amodiaquine were indifferent tending toward antagonism. Competitive uptake of radiolabeled chloroquine and dihydroartemisinin in combination with other antimalarials was observed.
Fivelman
Quinton L
QL
Third Floor ITD, London School of Hygiene and Tropical Medicine, Keppel Street, London WC1E 7HT, United Kingdom. quinton.fivelman@lshtm.ac.uk
Adagu
Ipemida S
IS
Warhurst
David C
DC
D000655:Amodiaquine / Q000494:pharmacology; D000818:Animals; D000962:Antimalarials / Q000378:metabolism / Q000494:pharmacology*; D037621:Artemisinins / Q000378:metabolism / Q000494:pharmacology; D002738:Chloroquine / Q000378:metabolism; D004336:Drug Antagonism; D004338:Drug Combinations; D004347:Drug Interactions; D004351:Drug Resistance; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000494:pharmacology; D012717:Sesquiterpenes / Q000378:metabolism / Q000494:pharmacology; D014316:Tritium / Q000378:metabolism; D010879:Piperazines
D000655:Amodiaquine; D000962:Antimalarials; D037621:Artemisinins; D002738:Chloroquine; D004338:Drug Combinations; D011804:Quinolines; D012717:Sesquiterpenes; D014316:Tritium; C039060:artenimol; C034759:piperaquine; D010879:Piperazines