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Artemether bioavailability after oral or intramuscular administration in uncomplicated falciparum malaria

Kamolrat Silamut1, Paul N Newton, Paktiya Teja-Isavadharm

  • 1Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.

Antimicrobial Agents and Chemotherapy
|November 26, 2003
PubMed

Insights

Oral artemether shows higher plasma concentrations and better antimalarial activity than intramuscular doses in acute malaria patients. This suggests oral administration is more effective for treating Plasmodium falciparum malaria.

Area of Science:

  • Pharmacology
  • Infectious Diseases
  • Clinical Medicine

Background:

  • Artemether is a crucial antimalarial drug.
  • Understanding its pharmacokinetics is vital for effective malaria treatment.
  • Plasmodium falciparum malaria remains a significant global health concern.

Purpose of the Study:

  • To compare the antimalarial activity of artemether after oral versus intramuscular administration.
  • To evaluate artemether's plasma concentrations and pharmacokinetic parameters in acute malaria.

Main Methods:

  • Bioassay of artemether in plasma from 15 adults with acute uncomplicated Plasmodium falciparum malaria.
  • Measurement of peak plasma concentrations (Cmax), area under the curve (AUC(0-24)), and clearance (CL/F).
  • Comparison of parameters between acute and convalescent phases, and between oral and intramuscular routes.

Main Results:

  • Oral artemether resulted in significantly higher peak plasma concentrations (median 16x) and AUC(0-24) (median 3.3x) compared to intramuscular administration.
  • Plasma concentrations were higher and clearance was lower in the acute phase versus the convalescent phase after oral dosing.
  • Time to peak concentration was significantly shorter with oral (median 1 hr) than intramuscular (median 8 hr) artemether.

Conclusions:

  • Oral artemether demonstrates superior antimalarial activity and pharmacokinetic profile compared to intramuscular administration in acute malaria.
  • Intramuscular artemether absorption is notably slow in patients with acute malaria.
  • These findings support the efficacy of oral artemether for treating Plasmodium falciparum malaria.

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