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Table 8 DHA half-life values obtained following artesunate administration.

From: Review of the clinical pharmacokinetics of artesunate and its active metabolite dihydroartemisinin following intravenous, intramuscular, oral or rectal administration

Ref.

Subjects

Artesunate regimen

DHA half-life (hours)

[29]

10 healthy male Vietnamese adults

200 mg once daily × 5 days

0.87 (from pooled data)

[30]

12 healthy male Malaysian adults

200 mg single dose

0.49

[40]

20 male and female healthy Thai adults

4 mg/kg once

0.74a

[27]

13 healthy adults in Africa

Mean dose: 4.26 mg/kg with (ACT) or without (AS only) amodiaquine single dose

AS only:1.46

ACT: 3.08

[28]

8 healthy male Thai adults

300 mg AS (Guilin or Arenco formulation)

Guilin: 1.77

Arenco:1.73

[41]

10 healthy Vietnamese males

100 mg AS once

Half-life: 0.55b

[25]

6 healthy adults in Geneva

200 mg AS once

0.65

[26]

23 healthy Malaysian adults

200 mg once with amodiaquine as fixed or non-fixed product

Fixed:1.68

Non-fixed:1.42

[24]

20 healthy adult males in Australia

200 mg/day × 3 days alone (Period 1); repeated with mefloquine after washout (Period 2)

Period 1/Day 1: 1.14

Period 1/Day 3: 1.14

Period 2/Day 1: 1.02

Period 2/Day 3: 1.09

[23]

15 healthy Cambodian male adults

4 mg/kg once with mefloquine

1.30b

[42]

12 healthy adults

200 mg once

0.68

[34]

86 acute uncomplicated falciparum malaria patients from Malawi and Gambia

1, 2, or 4 mg/kg AS with chlorproguanil and dapsone once daily × 3 days

1 mg/kg: 0.779b

2 mg/kg: 0.917b

4 mg/kg: 1.09b

[7]

12 Vietnamese adult male vivax malaria patients

100 mg single dose

0.67 (n = 11)

[8]

26 Vietnamese adult patients with uncomplicated falciparum malaria

100 mg single dose

0.66 (n = 16)

[39]

21 children (5 - 13 years) with uncomplicated malaria in Uganda

4 mg/kg once daily with amodiaquine × 3 days

1.3a

[38]

24 children with uncomplicated falciparum malaria in Gabon

4 mg/kg once daily for 3 days in one of two formulations (blister pack and fixed dose) of AS/mefloquine

Fixed dose: 0.9(n = 9)a

Blister pack: 1.0 (n = 11)a

[32]

43 adults with uncomplicated falciparum malaria in Thailand

200 mg/day for fixed dose AS-mefloquine tablet or 4 mg/kg/day as nonfixed AS-mefloquine

Fixed: 1.1 (n = 14)

Nonfixed: 0.8 (n = 18)

[31]

11 male Thai adults with uncomplicated falciparum malaria

200 mg AS once, followed by 100 mg 12 hours later, then 100 mg once daily × 4 days

Acute: 0.64a

Convalescence: 0.66a

[43]

24 pregnant Karen women in the 2nd and 3rd trimesters with uncomplicated falciparum malaria

4 mg/kg once daily × 3 days with atovaquone plus proguanil

Half-life: 1.0 (n = 13)a

PopPK half-life estimate: 1.81 hr

[35]

6 male Thai adults with uncomplicated falciparum malaria and 6 healthy male adults

100 mg AS once

Healthy: 0.85

Patients: 1.06

[9]

8 Vietnamese adults with uncomplicated falciparum malaria and 10 healthy Vietnamese adults

150 mg once

Healthy: 0.77

Patients: 0.88

[53]

26 2nd and 3rd trimester pregnant women with asymptomatic falciparum parasitaemia, the same women postpartum, and 25 non-pregnant asymptomatic, parasitaemic controls

200 mg once

Pregnant: 1.28a

Postpartum:1.63a

Controls: 1.41a

[36]

57 children (2-14 years) with uncomplicated falciparum malaria in Gabon

AS dose (mg/kg)

Group A:2.1(1.4-2.4)

Group B:3.3(2.4 - 3.9)

Group C:4.8(3.0 - 6.1)

Group D: 3.8(3.0-4.3)

Administered with pyronaridine

Group A:1.0

Group B: 0.9

Group C: 1.2

Group D:1.2

[37]

40 children and adults with uncomplicated falciparum malaria in Pailin, Cambodia and 40 adults with uncomplicated falciparum malaria in Wang Pha, Thailand

At each site:

Group 1: AS monotherapy: 2 mg/kg/day × 7 days

Group 2: AS 4 mg/kg/day × 3 days + mefloquine

Thailand:

Group 1: 0.71a

Group 2: 0.85a

Cambodia:

Group 1: 0.84a

Group 2: 0.77a

  1. Estimates from PopPK studies are described in the text. Values given as mean unless otherwise specified.
  2. a. Median b. Geometric mean