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Table 10 Summary of DHA pharmacokinetic results following rectal 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 (hours)

Clearance (L/kg/hr)

Volume (L/kg)

Half-life (hours)

AUC (ng*hr/mL)

[49]

Sirivichay et al, 2007

16 paediatric patients with uncomplicated falciparum malaria

10 mg/kg (n = 7) or 20 mg/kg (n = 9) AS as rectal suppositories

898; 1535†a

1.5; 2.0a

  

1.3; 1.8a

2403; 5633†a

[50]

Halpaap et al, 1998

12 paediatric patients with uncomplicated falciparum malaria

50 mg AS as rectal suppository

[0.86 - 2.55 mg/kg AS]

180†

1.13

    

[42]

Awad et al, 2004

12 healthy Sudanese adults

200 mg AS as rectal suppository

219.1†

1.95

  

1.21

1185.17

[30]

Navaratnam et al, 1998

12 healthy Malaysian adults

200 mg AS as rectal suppository

385.6†

1.80

   

AUC0-t

965

Krishna et al, 2001

[15]

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

Group 1: AS 10 mg/kg as rectal suppository, IV AS 2.4 mg/kg 12 hr later

Group 2: AS 20 mg/kg AS as rectal suppository, IV AS 2.4 mg/kg 12 hr later

Group 3: 2.4 mg/kg IV AS, 20 mg/kg AS as rectal suppository 12 hr later

Group 1:

682†a

Group 2 & 3:

881†a

Group 1:

1.7a

Tlag: 0.63a

Group 2 & 3:

1.8a

Tlag: 0.37a

Group 1:

2.6

Group 2 & 3:

3.9

Group 1:

4.4a

Group 2 & 3:

5.9a

Group 1:

0.79a

Group 2 & 3:

0.85a

Group 1:

2787 †a

Group 2 & 3:

3753†a

  1. Estimates from PopPK studies are described in the text. Values given as mean unless otherwise specified
  2. †Units converted to uniform scale a. Median