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Table 2 Summary of DHA pharmacokinetic results following IV AS administration.

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

Ref.

Subjects & Regimen

Cmax (ng/mL)

Tmax (min)

Clearance (L/kg/hr)

Volume (L/kg)

Half-life (min)

AUC (ng*hr/mL)

[7]

Batty, Le et al, 1998

12 Vietnamese adults with vivax malaria

120 mg IV AS over 2 min

2192†a

8a

1.10

0.92

36.7

1845†

[9]

Binh et al, 2001

17 healthy Vietnamese volunteers; subjects randomized into two groups, both receiving:

120 mg IV AS over 2 min

1507; 1678†

9; 16

  

53; 47

 

[10]

Ilett et al, 2002

23 Vietnamese adults with uncomplicated falciparum malaria; subjects randomized into two groups, both receiving:

120 mg IV AS over 2 min

2758; 2730†a

7; 9a

0.64; 0.48

0.8; 0.55

59; 50

2872; 3298†

[11]

Li et al, 2009

30 healthy volunteers

0.5, 1, 2, 4, or 8 mg/kg IV AS over 2 min

428; 802; 1286; 3148; 4744

9.6; 15; 9.6; 7.2; 24†

1.3; 0.98; 1.1; 0.86; 0.82†

Vss: 1.734; 2.201; 1.860; 1.701; 2.403†

57.6; 92.4; 69.0; 82.2; 128.4†

385; 1082; 1850; 4886; 10410

[12]

Nealon et al, 2002

28 paediatric Gabonese patients with severe malaria randomized into two groups

Group 1: 2.4 mg/kg IV AS

Group 2: 1.2 mg/kg IV AS

Group 1:

3011†a

Group 2:

1584†a

Group 1:

0.5a

Group 2:

1.4a

Group 1:

2.16†a

Group 2:

1.08†a

Group 1

Vss: 0.75a

Group 2

Vss: 0.77a

Group 1:

20.7a

Group 2:

32.0a

Group 1:

923†a

Group 2:

737†a

[13]

Newton et al, 2006

17 adults with severe falciparum malaria in Thailand

2.4 mg/kg IV AS over 2 min

[2.1 (1.4 - 2.8 mg/kg)]

605†a

Tmax reached by 15 min

5.6a

Vss: 1.9a

20.4†a

418†a

[8]

Batty. Thu et al, 1998

26 adult uncomplicated falciparum malaria patients in Vietnam

120 mg IV AS over 2 min

2648†a

9.0a

0.75a

0.76

40.2

2377†

[14]

Davis et al, 2001

30 parasitaemic adults with falciparum malaria

Group 1: 12 with complications

Group 2: 8 without complications

Group 1 & 2:

120 mg IV AS over 2 min

Group 3: 10 with moderately severe complications

(240 mg IV AS infused over 4 hours; samples taken after infusion discontinued)

Group 1:

2417†

Group 2:

2531†

Group 3:

910 †

Group 1:

10.4

Group 2:

9.9

Group 3:

240 (end of infusion)

Group 1:

1.09

Group 2:

0.73

Group 3:

0.73

Group 1:

0.77

Group 2:

1.01

Group 3:

0.78

Group 1: 40.0

Group 2: 64.1

Group 3: 46.2

Group 1:

2078†

Group 2:

2559†

Group 3:

5573†

Krishna et al, 2001

[15]

34 Ghanaian children (8 months - 7 years) with moderate falciparum malaria

Group 1 & 2: AS rectal suppository, IV AS 2.4 mg/kg 12 hr later

Group 3: 2.4 mg/kg IV AS, AS rectal suppository 12 hr later

Groups 1 & 2:

1280†a

Group 3:

1592 †a

Groups 1 & 2:

12†a

Group 3:

12†

Groups 1 & 2:

1.5a

Group 3: 1.0a

Groups 1 & 2:

0.6a

Group 3:

0.9a

Groups 1 & 2:

18†a

Group 3:

31.8†a

Groups 1 & 2:

1166†a

Group 3:

1706†a

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