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Table 2 Population pharmacokinetic parameter values (BSV%) for each drug

From: Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development

  Drug
PKa parameter ARS/DHAb ART LF MQ PQc
ka (/h) 19.7d 0.37 0.17 7d 0.717
(26.5%) (63%) (52%) (26%) (168%)
CL/F (L/h) 24.2e 180 7.04 0.8e 66
(22.4%) (50%) (16%) (33%) (42%)
V/F (L) 0.83f 217 - 10.2f -
(50%) (30–50%) (51%)
Vc/F (L) - - 103 - 8660
(30–50%) (101%)
Q/F (L/h) - - 4.08 - 131
(30–50%) (85%)
Vp/F (L) - - 272 - 24000
    (30–50%)   (50%)
  1. ARS – artesunate, ART – artemether, DHA – dihydroartemisinin, LF – lumefantrine, MQ – mefloquine, PQ – piperaquine.
  2. Parameter values were taken from the literature: dihydroartemisinin[16], artemether[17], lumefantrine[17], mefloquine[18], piperaquine[19]. Between-subject variability (BSV%) presented as standard deviation multiplied by 100 (lognormal error model).
  3. aka – absorption rate constant; CL/F – clearance; V/F – volume of distribution; Vc – volume of central compartment; Q – inter-compartmental clearance; and Vp –volume of peripheral compartment.
  4. bDihydroartemisinin profiles were simulated for artesunate, since dihydroartemisinin is the primary active metabolite of artesunate and artesunate is considered the pro-drug.
  5. cPK parameters are for a 48kg individual.
  6. d/day.
  7. eL/kg/day.
  8. fL/kg.