Chloroquine blood plasma ratio

Discussion in 'Canadian Pharmaceuticals Online' started by Kukan, 25-Feb-2020.

  1. kingz New Member

    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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    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. For example, the clearance of CQ from whole blood and plasma is approximately 0.1 to 0.25 liter/h/kg of body weight and 0.5 to 0.9 liter/h/kg, respectively, in healthy volunteers, and the t 1/2 of CQ is 150 to 290 h 17–19, 32, 35, 47, 59. Verapamil, chloroquine Figure 1 and 2 Detection method LC-MS/MS with internal standard Results blood to plasma ratio Figure 1. Blood to plasma ratio obtained for two reference compounds in 3 different species Figure 2. Comparison of in-house human blood to plasma ratio with literature values 1,2 1 Obach 1999, Drug Metab Dispos 27, 1350

    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

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    Our upper and lower plasma concentrations, 2 μM and 0.3 μM, respectively, were based on the assumption that a 10- to 30-fold greater brain concentration exists when compared to plasma concentrations for CQ.49, 50 We used the average of this range, a 20-fold lower plasma concentration compared with the reported range of inhibitory concentration of 6-40 μM.17, 48 While not being able to directly verify human fetal brain concentrations, our range of predicted peak plasma concentrations 0.1. The distribution of chloroquine was studied in the tissues and blood of rat. 2. 2. The time to peak concentration and the maximum concentration varied in various tissues and were higher than for plasma and red blood cells. Therefore, determining the blood-to-plasma ratio is important for deciding whether plasma or whole blood would provide more physiologically relevant pharmacokinetic parameters. For these studies, chloroquine is used as a positive control. Caco-2 Permeability Studies

     
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