Pharmacokinetics of quinine chloroquine and amodiaquine

Discussion in 'Canadian Pharmacy' started by Lou, 17-Mar-2020.

  1. sovsemdrugoy XenForo Moderator

    Pharmacokinetics of quinine chloroquine and amodiaquine


    It is bioactivated hepatically to its primary metabolite, N-desethylamodiaquine, by the cytochrome p450 enzyme CYP2C8. Among amodiaquine users, several rare but serious side effects have been reported and linked to variants in the CYP2C8 alleles.

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    Quinine is active against the Plasmodium falciparum strain and may be used where other medicines – such as chloroquine or artesunate – are either ineffective or unavailable. Quinine is most effective at treating uncomplicated malaria. It becomes progressively less effective at treating more complicated, severe forms of malaria. The pharmacokinetics of artesunate and amodiaquine and their main active metabolites dihydroartemisinin and desethylamodiaquine were compared following monotherapy and combination therapy using analysis of variance. Chloroquine, noncurative, and amodiaquine, partially curative, have nearly the same initial dose-independent killing with a lag phase of minimal parasite reduction at all doses between 6 and 24.

    People who are poor metabolizers of amodiaquine display lower treatment efficacy against malaria, as well as increased toxicity. CYP2C8*1 is characterized as the wild-type allele, which shows an acceptable safety profile, while CYP2C8*2, *3 and *4 all show a range of "poor metabolizer" phenotypes.

    Pharmacokinetics of quinine chloroquine and amodiaquine

    Clinical Pharmacokinetics and Metabolism of Chloroquine., Pharmacokinetics and tolerability of artesunate and.

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  5. Concomitant administration of Mefloquine and quinine or chloroquine may increase the risk of convulsions. Ocular Effects Eye disorders, including but not limited to optic neuropathy and retinal disorders, have been reported during treatment with Mefloquine.

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    Clinical Pharmacokinetics of Zidovudine. Pharmacokinetics of Quinine, Chloroquine and Amodiaquine. Dr Sanjeev Krishna, Nicholas J. White Pages 263-299. Pharmacokinetics of chloroquine in Thais plasma and red-cell concentrations following an intravenous infusion to healthy subjects and patients with Plasmodium vivax malaria. Br. J. Quinine is well absorbed by mouth or following intramuscular injection even in severe cases of malaria estimated bioavailability more than 85%. Quinine and chloroquine may cause potentially lethal hypotension if given by intravenous injection.

     
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