The use of the antimalarial agent amodiaquine has been curtailed due to drug-induced idiosyncratic reactions. These have been attributed to the formation of a protein-reactive quinoneimine species via oxidation of the 4-aminophenol group. Therefore, the effects of chemical modifications on the disposition of amodiaquine in relation to its metabolism, distribution, and pharmacological activity h...

OBJECTIVES To compare the efficacy and safety of artemisinin combination therapies for the treatment of uncomplicated falciparum malaria in Uganda. DESIGN Randomized single-blind controlled trial. SETTING Tororo, Uganda, an area of high-level malaria transmission. PARTICIPANTS Children aged one to ten years with confirmed uncomplicated P. falciparum malaria. INTERVENTIONS Amodiaquine + ...

Artesun-Plus is a fixed-dose combination antimalarial agent containing artesunate and amodiaquine. The current study was conducted to compare the pharmacokinetic and safety profiles of Artesun-Plus and the WHO-designated comparator product Artesunate Amodiaquine Winthrop. To overcome the high intrasubject variability of artesunate, the study applied a two-sequence and four-period crossover (2 b...

The spread of chloroquine-resistant Plasmodium falciparum in most counmes in sub-saharan Africa has raised an urgent need to determine what alternative antimalarial drug should replace chloroquine for the first-line oral treatment of acute uncomplicated falciparum malaria. The drug must satisfy the following requirements to be a viable option in Africa: high and rapid clinical efficacy, short t...

antimalarial drugs with the 4-aminoquinoline scaffold such as the important drugs, chloroquine (cq) and amodiaquine (aq), have been used to prevent and treat malaria for many years. the importance of these drugs is related to their simple usage, high efficacy, affordability, and cost-effectiveness of their synthesis. in recent years, with the spread of parasite resistance to cq and cross-resist...

Muley et al. (8) and Jadhav et al. (2) have recently shown histamine to be responsible for the cataleptic effect of morphine and clonidine in mice. Since amodiaquine is reported to inhibit histarnine-Nvrnethvl transferase, an enzyme concerned with major, catabolism of brain histamine by methylation (4), we have investigated the effect of pretreatment with amodiaquine on morphine-and clonidine-i...

K1 strain of Plasmdoium falciparum is resistant in vitro to chloroquine, pyrimethamine and sulfadoxine. Response of this strain to combinations of antimalarial drugs in the in vitro hypoxanthine incorporation test was coupled with that of a line of strain NF54 relatively sensitive to chloroquine and fully sensitive to other antimalarials. Pyrimethamine and sulfadoxine showed potentiative synerg...

OBJECTIVE To test a novel methodology to define age-based dosing regimens for the treatment of malaria with a new, user-friendly, blister-packaged fixed-dose combination of artesunate and amodiaquine. METHODS A weight-for-age reference database of 88 054 individuals from sub-Saharan Africa was compiled using data from Demographic Health Surveys, observational and intervention studies, and sta...

Key parasite polymorphisms were assessed in subjects treated for malaria with artesunate-amodiaquine in Tororo, Uganda. For pfcrt, all of the isolates tested had the CVIET haplotype. For pfmdr1, 86Y and 1246Y were common at baseline and their prevalences were significantly higher in new isolates after therapy, indicating that treatment selected for mutations associated with a decreased response...