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Table 7 Artesunate and DHA AUC and Cmax values following oral artesunate administration.

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

Ref.

Subjects

Oral AS regimen

AUC (ng*hr/mL)

Cmax (ng/mL)

[29]

10 healthy male Vietnamese adults

200 mg once daily × 5 days

ASa

Day 1: 67

Day 5: 60

ASa

Day 1:67

Day 5: 58

   

DHAa

Day 1:1158

Day 5:1300

DHA

Pooled:654

[30]

12 healthy male Malaysian adults

200 mg AS once

AS

119

AS

256.3

   

DHA

AUC0-t:1331

DHA

873.7

[27]

13 healthy adults in Africa

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

AS

AS only: 206.4

ACT: 183.3

AS

AS only: 231.8

ACT: 141.6

   

DHA

AS only: 2044.4

ACT: 1410.5

DHA

AS only: 844.5

ACT: 446.2

[28]

8 healthy male Thai adults

300 mg AS

(Guilin and Arenco formulations)

AS

Guilin: 406

Arenco: 190.8

AS

Guilin: 397

Arenco: 194

   

DHA

Guilin: 1630

Arenco: 2600

DHA

Guilin: 500

Arenco:928

[6]

8 healthy adults in Australia

150 mg once

AS

AUC0-6 hr:154 (n = 6)

ASa

111 (n = 6)

   

DHA

AUC0-6 hr: 824

DHAa

546

[26]

23 healthy Malaysian adults

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

AS†

Fixed: 391.1

Non-fixed: 213.2

AS†

Fixed: 333

Non-fixed: 444

   

DHA†

Fixed: 1468.9

Non-fixed: 1656.0

DHA†

Fixed: 609.8

Non-fixed:874.5

[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

ASb

1 mg/kg: 64.6 (n = 16)

2 mg/kg:151(n = 19)

4 mg/kg: 400(n = 23)

ASb

1 mg/kg: 48.9

2 mg/kg: 106

4 mg/kg: 224

   

DHAb

1 mg/kg: 538 (n = 24)

2 mg/kg: 1445(n = 29)

4 mg/kg: 383(n = 23)

DHAb

1 mg/kg: 228

2 mg/kg: 581

4 mg/kg: 1414

[39]

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

4 mg/kg once daily with amodiaquine × 3 days

AS

113 (data pooled from all subjects)

AS 51 (data pooled from all subjects)

   

DHAa

1404

DHAa

473

[32]

43 adults with uncomplicated falciparum malaria in Thailand

200 mg/day for fixed dose AS-mefloquine tablet (n = 20) or 4 mg/kg/day as nonfixed (n = 23) AS-mefloquine

AS

AUC0-t:

Fixed:310 (n = 19)

Nonfixed: 419 (n = 21)

AS

Fixed:255 (n = 19)

Nonfixed:451 (n = 23)

   

DHA

AUC0-t:

Fixed:3027

Nonfixed: 3633

DHA

Fixed:1234

Nonfixed:2043

[35]

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

100 mg AS once

AS

AUC0-12 hr

Healthy: 97

Patients: not determined

AS

Healthy: 114

Patients: not determined

   

DHA

AUC0-12 hr

Healthy: 501

Patients: 1144

DHA

Healthy: 339

Patients: 554

[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)

AS

Group A: 104 (n = 12)

Group B: 154 (n = 12)

Group C:232 (n = 10)

Group D: 179 (n = 13)

AS

Group A: 93

Group B:154

Group C: 287

Group D: 171

  

Administered with pyronaridine

DHA

Group A: 1055

Group B: 1989

Group C: 2961

Group D: 2245

DHA

Group A:479

Group B: 940

Group C:1186

Group D:792

[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

AS†a

AUC0-24 hr

Thailand:

Group 1: 128

Group 2: 237

Cambodia:

Group 1: 173

Group 2: 338

AS†a

Thailand:

Group 1: 171

Group 2: 200

Cambodia:

Group 1: 270

Group 2: 316

   

DHA†a

AUC0-24 hr

Thailand:

Group 1: 1308

Group 2: 2957

Cambodia:

Group 1: 1382

Group 2: 4123

DHA†a

Thailand:

Group 1: 859

Group 2: 1191

Cambodia:

Group 1: 802

Group 2: 1590

  1. Values given as mean unless otherwise specified.
  2. †Units converted to uniform scale a. Median b. Geometric mean