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Table 1 Summary of AS 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)

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

13685†a

3.01

0.16

2.19

876†

[9]

Binh et al, 2001

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

120 mg IV AS over 2 min

 

3.0; 2.2

0.19; 0.16

2.6; 3.3

846; 1269†

[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

16146;

16530†

2.8; 2.1

0.22

3.2

1038; 1230†

[11]

Li et al, 2009

30 healthy volunteers

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

4797; 6128; 19420; 36100; 83340

1.3; 18; 1.3; 1.4; 1.6†

Vss: 0.092; 0.187; 0.106; 0.109; 0.165†

7.2; 8.4; 14.4; 9.0; 12.6†

386; 593; 1595; 3038; 6994†

[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: 29677a

Group 2: 15369a

Group 1:

3.12†a

Group 2:

4.26†a

Group 1 Vss: 0.17†a

Group 2 Vss: 0.44†a

Group 1: 1.5a

Group 2:11.5a

Group 1:

1042†a

Group 2:

555†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)]

130+†a

64a

Vss:

15.2a

13.2+†a

49.2†a

[8]

Batty. Thu et al, 1998

26 adult uncomplicated falciparum malaria patients in Vietnam

120 mg IV AS over 2 min

 

2.33a

0.140a

2.73

1146†

[14]

Davis et al, 2001

30 parasitaemic adults with falciparum malaria

Group 1: 12 with complications (120 mg IV AS over 2 min)

Group 2: 8 without complications

(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:

1.63

Group 2:

2.49

Group 3: 3.07

Group 1:

0.08

Group 2:

0.24

Group 3:

0.23

Group 1:

2.3

Group 2:

4.3

Group 3:

3.2

 
  1. Values given as mean unless otherwise specified.
  2. †Units converted to uniform scale +The authors note that Cmax is likely underestimated and half-life overestimated due to the lack of usable data from six patients with extremely rapid AS elimination. a.Median