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Antimalarial Bioavailability and Disposition of Artesunate in Acute Falciparum Malaria

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Newton, P., Suputtamongkol, Y., Teja-Isavadharm, P., Pukrittayakamee, S., Navaratnam, V, Bates, Imelda ORCID: https://orcid.org/0000-0002-0862-8199 and White, N. (2000) 'Antimalarial Bioavailability and Disposition of Artesunate in Acute Falciparum Malaria'. Antimicrobial Agents and Chemotherapy, Vol 44, Issue 4, pp. 972-977.

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Abstract

The pharmacokinetic properties of oral and intravenous artesunate (2 mg/kg of body weight) were studied in 19 adult patients with acute uncomplicated Plasmodium falciparum malaria by using a randomized crossover design. A sensitive bioassay was used to measure the antimalarial activity in plasma which results from artesunate and its principal metabolite, dihydroartemisinin. The oral study was repeated with 15 patients during convalescence. The mean absolute oral bioavailability of the antimalarial agent in patients with acute malaria was 61% (95% confidence interval [CI], 52 to 70%). The absorption and elimination of oral artesunate were rapid, with a mean elimination half-life of antimalarial activity of 43 min (95% CI, 33 to 53 min). Following oral administration to patients with acute falciparum malaria, peak antimalarial activity in plasma and the area under the plasma concentration-time curve were approximately double those during convalescence and the apparent volume of distribution and clearance were approximately half those during convalescence(P < 0.005). Acute malaria is associated with a significant reduction in the clearance of artesunateassociated antimalarial activity.

Item Type: Article
Subjects: QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 750 Malaria
WC Communicable Diseases > Tropical and Parasitic Diseases > WC 765 Prevention and control
Faculty: Department: Pre 2002
Digital Object Identifer (DOI): https://doi.org/10.1128/AAC.44.4.972-977.2000
Depositing User: Tina Bowers
Date Deposited: 10 Apr 2014 11:20
Last Modified: 22 Oct 2019 08:22
URI: https://archive.lstmed.ac.uk/id/eprint/3636

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