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KMID : 0360419760120020051
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Korean Journal of Pharmacology
1976 Volume.12 No. 2 p.51 ~ p.59
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The Effect of Deoxycholic acid on the Excretion of Methylene bis (3,4,6-Trichlorophenoxy acetic acid)
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Abstract
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Methylene bis (3,4,6-trichlorophenoxy acetic acid) "MTPA" has been developed for the purpose of treatment of clonorchiasis.
It has been rpeorted that, in patients treated with MTPA, the flukes in the liver were killed, elevated serum bilirubin returned to normal and the patients´ general condition was improved. However it took 1~4 weeks to obtain sufficient therapeutic effects. In rabbits, excretion of bilirubin in the bile was increased by the MTPA, and this action was enhanced by a combination of deoxycholic acid with MTPA.
This study was designed as a part of a series to increase the therapeutic effect of MTPA, by observing the relation of the blood level of MTPA with the excretion of MTPA in the bile, and the excretion of MTPA with bilirubin excretion in the bile caused by the injection of MTPA alone or in combination with deoxycholic acid.
^(14)C-labeled MTPA alone or with deoxycholic acid were injected into the ear veins of rabbits. The amout of bile, MTPA and bilirubin in the bile and the blood level of MTPA were measured.
The results obtained were as follows:
1. The amount of excreted bile was decreased gradually as the time elapsed in both groups, that is groups injected with MTPA alone and with deoxycholic acid, without any significant difference between either group.
2. The largest amount of MTPA excretion in the early stage of the MTPA excretion in both groups, but deoxycholic acid caused an increase in blood level of MTPA whereas biliary excretion of MTPA decreased, especially in the early stage after drug injection.
3. The significant increment of bilirubin excretion began within an hour and it reached peak level in 2~2½ hours after drug injection in both groups, but the amount of excreted bilirubin was larger in the combined group.
The above results suggest that deoxycholic acid interferes with the biliary excretion of MTPA, and that there is no close relation between the increased excretion of MTPA and bilirubin excretion. But there is a close relation between blood level or tissue concentration of MTPA and bilirubin excretion. Concerning the influence of deoxycholic acid on the therapeutic effect of MTPA, deoxycholic acid would enhance the effect of MTPA, if the parasites take the drug from the blood, but diminish its effectiveness if they take the drug from the bile.
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