Levels of metrifonate and dichlorvos in plasma and erythrocytes during treatment of schistosomiasis with Bilarcil.
A method for the simultaneous quantitation of metrifonate (0,0-dimethyl-(1-hydroxy-2,2,2-trichloroethyl)-phosphonate) and dichlorvos (2,2-dichlorovinyl dimethyl phosphate, DDVP) in human blood has been worked out. It is based upon multiple labelling of the compounds with deuterium and gas phase analysis using the mass spectrometer as a selective detector. The amount of DDVP in plasma is about 1% of the amount of metrifonate. In erythrocytes the corresponding amount of DDVP is 0.5% or less of metrifonate. Both compounds reach peak levels in blood within two hours after oral dosing and are detectable for at least eight hours. Cholinesterase activity in plasma reaches zero levels within 15 min. and remains inhibited for more than eight hours. Red blood cell cholinesterase is inhibited only 60-80%. According to kinetic calculations, clearance of metrifonate occurs primarily via dichlorvos. If dichlorvos is the only active component, which in all likelihood it is, it's slow release may be important in the schistosomicidal effect. Clinical data in seven metrifonate treated patients revealed that mild vertigo subsiding in a few hours was the most common side effect.
D000293:Adolescent; D002648:Child; D002802:Cholinesterases / Q000097:blood; D004006:Dichlorvos / Q000097:blood*; D004912:Erythrocytes / Q000201:enzymology / Q000378:metabolism*; D005260:Female; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D008297:Male; D012548:Schistosoma haematobium; D012552:Schistosomiasis / Q000188:drug therapy*; D012556:Schistosomicides / Q000378:metabolism* / Q000627:therapeutic use; D014236:Trichlorfon / Q000097:blood* / Q000378:metabolism* / Q000627:therapeutic use
D012556:Schistosomicides; D004006:Dichlorvos; D014236:Trichlorfon; D002802:Cholinesterases