scholarly journals Comparison of Oral Artesunate and Dihydroartemisinin Antimalarial Bioavailabilities in Acute Falciparum Malaria

2002 ◽  
Vol 46 (4) ◽  
pp. 1125-1127 ◽  
Author(s):  
Paul N. Newton ◽  
Michele van Vugt ◽  
Paktiya Teja-Isavadharm ◽  
Duangsuda Siriyanonda ◽  
Maneerat Rasameesoroj ◽  
...  

ABSTRACT Plasma antimalarial activity following oral artesunate or dihydroartemisinin (DHA) treatment was measured by a bioassay in 18 patients with uncomplicated falciparum malaria. The mean antimalarial activity in terms of the bioavailability of DHA relative to that of artesunate did not differ significantly from 1, suggesting that DHA can be formulated to be an acceptable oral alternative to artesunate.

2003 ◽  
Vol 47 (11) ◽  
pp. 3458-3463 ◽  
Author(s):  
S. Pukrittayakamee ◽  
S. Wanwimolruk ◽  
K. Stepniewska ◽  
A. Jantra ◽  
S. Huyakorn ◽  
...  

ABSTRACT The relationships between the pharmacokinetic properties of quinine during a 7-day treatment course and the therapeutic response were studied in 30 adult patients with uncomplicated falciparum malaria monitored for ≥28 days. All patients received a 7-day oral quinine regimen either alone (n = 22) or in combination with rifampin (n = 8). The median fever clearance time was 58.5 h, and the mean ± standard deviation parasite clearance time was 73 ± 24 h. After recovery, six patients had recrudescences of Plasmodium falciparum malaria and seven had delayed appearances of P. vivax infection between days 16 and 23. Between the patients with and without recrudescences, there were no significant differences either in fever clearance time or parasite clearance time or in the overall pharmacokinetics of quinine and 3-hydroxyquinine. Patients for whom the area under the concentration-time curve from 3 to 7 days for quinine in plasma was <20 μg · day/ml had a relative risk of 5.3 (95% confidence interval = 1.6 to 17.7) of having a subsequent recrudescence of infection (P = 0.016). Modeling of these data suggested an average minimum parasiticidal concentration of quinine in plasma of 3.4 μg/ml and an MIC of 0.7 μg/ml for uncomplicated falciparum malaria in Thailand. To ensure a cure, the minimum parasiticidal concentration must be exceeded during four asexual cycles (>6 days).


2000 ◽  
Vol 44 (4) ◽  
pp. 972-977 ◽  
Author(s):  
Paul Newton ◽  
Yupin Suputtamongkol ◽  
Paktiya Teja-Isavadharm ◽  
Sasithon Pukrittayakamee ◽  
V Navaratnam ◽  
...  

ABSTRACT The pharmacokinetic properties of oral and intravenous artesunate (2 mg/kg of body weight) were studied in 19 adult patients with acute uncomplicated Plasmodium falciparum malaria by using a randomized crossover design. A sensitive bioassay was used to measure the antimalarial activity in plasma which results from artesunate and its principal metabolite, dihydroartemisinin. The oral study was repeated with 15 patients during convalescence. The mean absolute oral bioavailability of the antimalarial agent in patients with acute malaria was 61% (95% confidence interval [CI], 52 to 70%). The absorption and elimination of oral artesunate were rapid, with a mean elimination half-life of antimalarial activity of 43 min (95% CI, 33 to 53 min). Following oral administration to patients with acute falciparum malaria, peak antimalarial activity in plasma and the area under the plasma concentration-time curve were approximately double those during convalescence and the apparent volume of distribution and clearance were approximately half those during convalescence (P ≤ 0.005). Acute malaria is associated with a significant reduction in the clearance of artesunate-associated antimalarial activity.


Author(s):  
Khalid Abdelsamea Mohamedahmed ◽  
Zeinab Abdalmalik Ahmed ◽  
Bakri Yousif Mohammed Nour ◽  
Adam Dawoud Abakar ◽  
Asaad Ma. Babker

Background: Falciparum malaria remains one of the most global infection among children particularly in communities with poor resources. Falciparum malaria associated with several hematological changes that affect the major blood cell lines such as platelets lead to platelets parameters (platelets count and indices) abnormalities. Objectives: The aim of this study was to evaluate the effects of falciparum malaria on platelets parameters (platelets count and indices) among Sudanese children. In addition to study relationships and correlation between platelets parameters and malaria parasitemia and parasite count. Materials and Methods: A case control study was conducted in Wad Medani Pediatric Hospital in collaboration with Faculty of Medical laboratory Sciences, University of Gezira, Sudan among 100 children with severe falciparum malaria (mean age 8.63 ± 3.40 years; 61% males), 100 children with uncomplicated falciparum malaria (mean age 8.83 ± 4.20 years; 45% males) and 100 children with normal healthy children controls (mean age 10.08 ± 3.58 years; 50% males). Parasitemia and parasite count (%) was determined directly from thick and thin blood films respectively. The platelets parameters (platelets count and indices) measured by using Sysmex XP 300 N automated analyzer, and platelets count was confirmed and assessed using stained thin blood film. SPSS software (V 20.0) and Stat disk software (V 13.0) were used for data analysis. Results: 72 % of severe falciparum malaria (SM) have hyperparasitemia, while 18 % among uncomplicated falciparum malaria (UM). The thrombocytopenia account for 43 % (SM: 30.5 %; UM: 12.5 %), low PCT account for 35.5 % (SM: 27 %; UM: 8.5 %) and high PDW account for 46.5 % (SM: 23.5 %; UM: 23 %) in falciparum malaria cases. The mean PLTs count and PDW were statistically significantly differences between falciparum malaria cases and normal healthy control (P value 0.000 and 0.008 respectively). The mean PLTs count and PCT in severe falciparum malaria cases were lower than uncomplicated falciparum malaria cases (P value 0.005 and 0.000 respectively). The PLTs count and PCT had significant negative correlation within malaria parasitemia (P value 0.000; r -0.286; P value 0.004; r -0.205 respectively) and malaria parasite count (P value 0.000; r -0.450; P value 0.000; r -0.270 respectively). Conclusion: The study concluded that thrombocytopenia, low PCT and high PDW were observed as most platelets parameters changes in falciparum malaria. PLTs count along with PCT to be recommended as hematological diagnostic markers and prognostic tool to assess the disease severity and to improve the management of falciparum malaria among patients.


2000 ◽  
Vol 20 (4) ◽  
pp. 229-235
Author(s):  
A. Sowunmi ◽  
C.O. Falade ◽  
A.A. Adedeji ◽  
T.C. Happi ◽  
C.O. Sowunmi ◽  
...  

PLoS ONE ◽  
2007 ◽  
Vol 2 (10) ◽  
pp. e1101 ◽  
Author(s):  
Tanilu Grande ◽  
Andrea Bernasconi ◽  
Annette Erhart ◽  
Dioni Gamboa ◽  
Martin Casapia ◽  
...  

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