Activity of benflumetol and its enantiomers in fresh isolates of Plasmodium falciparum from East Africa

Wernsdorfer, Walther H.; Landgraf, Barbara; Kilimali, V.A.E.B.; Wernsdorfer, Gunther

doi:10.1016/s0001-706x(97)00141-1

Cited by 31 publications

(14 citation statements)

References 1 publication

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“…With an EC90 level of 338.79 nM for lumefantrine the sensitivity of local P. falciparum is significantly below the baseline of 46.98 nM for northern Tanzania (Fig. 3) [17], obviously the result of heavy drug pressure. Similarly, EC90 and EC99 values for artemisinin of 311.50 nM and 2059.49 nM are far above the levels seen in Thailand although artemisinin derivatives are used there since almost 2 decades, albeit under conditions of very strict control [18] and also well above the baseline sensitivity observed in Tanzania (Fig.…”

Section: Resultsmentioning

confidence: 91%

Malariological baseline survey and in vitro antimalarial drug resistance in Gulu district, Northern Uganda

Prugger

Engl

Ogwang

et al. 2008

Wien Klin Wochenschr

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A comprehensive, representative malaria survey has been carried out in a population of internally displaced persons (IDP) in the district of Gulu, Northern Uganda. It included 74 households and 390 persons, and covered socio-economic and environmental information, individual physical data, malaria and the drug sensitivity of Plasmodium falciparum. The prevalence of infections with Plasmodium falciparum was 54.4% at a geometric mean asexual parasitaemia of 229/microl blood, typical for hyperendemic conditions. P. falciparum turned out to be highly resistant to chloroquine and amodiaquine. It showed also reduced sensitivity against lumefantrine and artemisinin, obviously the result of the liberal use of the lumefantrine-artemether combination without evidence-based indication.

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Section: Resultsmentioning

confidence: 91%

Malariological baseline survey and in vitro antimalarial drug resistance in Gulu district, Northern Uganda

Prugger

Engl

Ogwang

et al. 2008

Wien Klin Wochenschr

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“…Coartem ® is a well-tolerated, fast-acting and effective blood schizontocidal drug that serves primarily to treat uncomplicated falciparum malaria that is resistant to other antimalarials and has generally been adopted as a first-line treatment of uncomplicated falciparum malaria in most countries [2,[7][8][9][10]. It combines the fast onset of action of artemether (an artemisinin derivative) in terms of prompt parasite clearance with the long duration of action and high cure rate of lumefantrine (LF) [10][11][12].…”

Section: Introductionmentioning

confidence: 99%

A field-adapted sampling and HPLC quantification method for lumefantrine and its desbutyl metabolite in whole blood spotted on filter paper

Ntale¹,

Ogwal-Okeng²,

Mahindi³

et al. 2008

Journal of Chromatography B

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“…Although we did not measure this factor in Mbarara, African isolates have considerably lower IC50 values than those from western Thailand, where the high IC50 values are probably explained by the in-vitro cross-resistance between lumefantrine and mefloquine and halofantrine. 31,33,34 A day-7 lumefantrine concentration of less than 280 g/L as a pharmacokinetic predictor that treatment will not work might not be applicable to all regions, and further research should be done to assess the appropriate threshold as a function of parasite sensitivity.…”

mentioning

confidence: 99%

Supervised versus unsupervised intake of six-dose artemether-lumefantrine for treatment of acute, uncomplicated Plasmodium falciparum malaria in Mbarara, Uganda: a randomised trial

Piola¹,

Fogg²,

et al. 2005

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CitationSupervised versus unsupervised intake of six-dose artemether-lumefantrine for treatment of acute, uncomplicated Plasmodium falciparum malaria in Mbarara, Uganda: a randomised trial., 365 (9469 Articles IntroductionWith an estimated 500 million individuals affected every year, malaria is a leading cause of morbidity and mortality in sub-Saharan Africa along with HIV/AIDS. 1Of the 1 million deaths caused by malaria worldwide, about 90% occur in African children, a situation compounded by the emergence of drug resistance. 2In Uganda, which had a population of 24·7 million in 2003, an estimated 9·8 million individuals are infected with malaria every year (John Bosco Rwakimari, Ugandan Ministry of Health, Uganda, personal communication; http://www.health.go.ug). To tackle malaria-related mortality and morbidity, the Ugandan Ministry of Health (MoH) is concentrating on early diagnosis and effective treatment of the disease. In the 1970s and the 1980s, high malaria awareness in the population and easy access to cheap and effective antimalarials such as chloroquine and sulfadoxinepyrimethamine ensured the disease was reasonably well controlled. However, resistance to these drugs is now widespread in Uganda and in other parts of east Africa, with adverse consequences for malaria control. 3-7The MoH-recommended first-line antimalarial drug in Uganda is chloroquine combined with sulfadoxinepyrimethamine, 6 though introduction of artemisininbased combination treatments (ACTs) is planned for 2005.8 Day-28 cure rates of 52%, 9 65%, 7 and 77% 10 have been reported for this combination in different parts of Uganda. ACTs are judged effective in Africa, where they improve cure rates and reduce gametocyte carriage compared with presently used monotherapies.11,12 To combat drug-resistant malaria in Africa, WHO advocates the adoption of ACTs as first-line treatment.2 The use of the non-ACT combination of amodiaquine and sulfadoxine-pyrimethamine is considered by some as an interim measure while waiting for ACTs to become widely available. Day-28 efficacy rates of this combination were 84% and 90% in two studies in Uganda. 7,9 Artemether-lumefantrine (Coartem, Novartis Pharma, Basel, Switzerland) is the only fixed-dose formulation ACT on the WHO essential drug list. However, the combination is not registered for use in pregnant women, and was not registered for children under 10 kg in weight when we did our trial. Results of studies [13][14][15] from southeast Asia show that the six-dose regimen of artemether-lumefantrine has cure rates of more than 96%, is well tolerated, and has a good safety profile when Supervised versus unsupervised intake of six-dose artemether-lumefantrine for treatment of acute, uncomplicated Plasmodium falciparum malaria in Mbarara, Uganda: a randomised trial Patrice Piola, Carole Fogg, Francis Bajunirwe, Samuel Biraro, Francesco Grandesso, Eugene Ruzagira, Joseph Babigumira, Isaac Kigozi, James Kiguli, Juliet Kyomuhendo, Laurent Ferradini, Walter Taylor, Francesco Checchi, Jean-Paul Guthmann S...

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Activity of benflumetol and its enantiomers in fresh isolates of Plasmodium falciparum from East Africa

Cited by 31 publications

References 1 publication

Malariological baseline survey and in vitro antimalarial drug resistance in Gulu district, Northern Uganda

Malariological baseline survey and in vitro antimalarial drug resistance in Gulu district, Northern Uganda

A field-adapted sampling and HPLC quantification method for lumefantrine and its desbutyl metabolite in whole blood spotted on filter paper

Supervised versus unsupervised intake of six-dose artemether-lumefantrine for treatment of acute, uncomplicated Plasmodium falciparum malaria in Mbarara, Uganda: a randomised trial

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