Table 1.
Summary of AS pharmacokinetic results following IV AS 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 |
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Values given as mean unless otherwise specified.
†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