| In vitro: |
| Transactions of the Royal Society of Tropical Medicine & Hygiene, 1996,164(2):380-6. | | Antimalarial activity and interactions between quinine, dihydroquinine and 3-hydroxyquinine against Plasmodium falciparum in vitro.[Reference: WebLink] |
METHODS AND RESULTS:
The antimalarial activities of quinine, Dihydroquinine (a natural impurity found in commercial pharmaceutical formulations of quinine) and 3-hydroxyquinine (the principal metabolite of quinine in humans) were tested both individually and in pairs against 5 strains of Plasmodium falciparum isolated from patients in Thailand. The median inhibitory concentrations (IC50) were similar for quinine (168 nmol/L, range 68–366), and Dihydroquinine (129 nmol/L, range 54–324), and both were significantly lower than that of 3-hydroxyquinine (1160 nmol/L, range 378–3154) (P = 0·027). When these drugs were tested in combination, there was no evidence of synergy or antagonism, as determined by fractionary inhibitory indices and isobolograms.
CONCLUSIONS:
Quinine and its impurity, Dihydroquinine, have equivalent antimalarial activities which are approximately 10 times greater than that of the metabolite 3-hydroxyquinine. These 2 compounds, which are not usually measured in specific drug assays, contribute to antimalarial activity after quinine administration. |
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