Chloroquine blood plasma ratio

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  1. uspex User

    Chloroquine blood plasma ratio

    Chloroquine has been extensively used in mass drug administrations, which may have contributed to the emergence and spread of resistance. It is recommended to check if chloroquine is still effective in the region prior to using it.

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    Chloroquine is deposited in the tissues in considerable amounts. In animals, from 200 to 700 times the plasma concentration may be found in the liver,spleen, kidney, and lung; leukocytes also concentrate the drug. The brain and spinal cord, in contrast, contain only 10 to 30 times the amount present in plasma. A significant correlation r=0.97, p0.05 was observed between saliva and plasma levels of chloroquine. The saliva plasma concentrations ratio was found to be 0.53. From the saliva plasma relationship, the extent of chloroquine binding to plasma proteins was estimated to be 47%. Blood from the volunteers was incubated with varying concentrations of chloroquine CQ, desethylchloroquine DCQ and bisdesethyl-chloroquine BDCQ for 15 min and the RBC/plasma concentration ratio determined. Desethylchloroquine and BDCQ were concentrated in the red cells of uninfected blood to the same extent as chloroquine.

    The Centers for Disease Control and Prevention recommend against treatment of malaria with chloroquine alone due to more effective combinations. In areas where resistance is present, other antimalarials, such as mefloquine or atovaquone, may be used instead.

    Chloroquine blood plasma ratio

    Chloroquine - FDA prescribing information, side effects and uses, Pharmacokinetics of chloroquine Saliva and plasma levels.

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  4. The drug is extensively distributed, with a volume of distribution of 200 to 800 L/kg when calculated from plasma concentrations and 200 L/kg when estimated from whole blood data concentrations being 5 to 10 times higher. Chloroquine is 60% bound to plasma proteins and equally cleared by the kidney and liver.

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    Reference plasma and whole blood are spiked with tested compound to 5 μM with a final DMSO concentration less than 0.1%. Both the spiked whole blood and plasma control are incubated at 37°C for up to 60 min. During the time course, aliquots of plasma and whole blood from both incubation mixtures are sampled at 10 and 60 min. Stability of chloroquine and desethylchloroquine in whole blood, plasma and DBS was investigated by exposing the samples to five freeze and thaw cycles. The samples were frozen at -80°C for 24 h for the first freeze cycle and 12–24 h for the following freezing cycles and thawed at room temperature for 2–3 h. Chloroquine enters the red blood cell by simple diffusion, inhibiting the parasite cell and digestive vacuole. Chloroquine then becomes protonated to CQ2+, as the digestive vacuole is known to be acidic pH 4.7; chloroquine then cannot leave by diffusion.

  5. AndreVla Moderator

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