Pharmacokinetics studies and clinical aspect of antimony drugs

After administration of an SbV compound (e.g. stibogluconate or meglumine antimonate), the peak concentration of antimony reaches to 9-12 mgml-1 in blood 2h after initial dose, followed by a rapid drop within 24 h.60,69 About 80-95% of the drug appears in the urine within 6h, indicating that the drug is not biotransformed appreciably.61 About 12% of the drug accumulates in an extravascular compartment, primarily in liver, spleen or kidney, which becomes saturated after 5 days of therapy and from which antimony is slowly released.62 64 The kinetics of SbV agents is best described by a two-compartment, three-term pharmacokinetics model. The initial absorption phase has a mean half-life of 0.85 h, followed by a rapid elimination phase with a half-life of 2.02h and a slow elimination phase with a half-life of 76 h.60

The period of Leishmania treatment (30 days) by SbV is related to the slow accumulation of antimony in the human body. The minimum antimony concentration in blood increased from 0.04-0.08 mgml-1 at the beginning of the treatment to 0.19-0.33 mgml-1 at day 30 of the treatment.60 The slow accumulation phase was believed to be due to the reduction of SbV to Sb111 in vivo.

On the other hand, modifications of the stibogluconate formulation improve the pharmacokinetic parameters of antimony agents for a better treatment of L. donovani.65,66 The encapsulated stibogluconate favors the organ distribution and increases the tissue resistance time, both of which enhance the efficiency of the treatment.

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