About: HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs     Goto   Sponge   NotDistinct   Permalink

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  • Oxime HI-6 DMS (dimethanesulfonate) is an asymmetric bispyridinium aldoxime and essential acetylcholinesterase (AChE) reactivator. The high effectiveness is due to its wide spectrum of therapeutic activity against different structures of nerve agents. Aim of this study was to compare plasma time profiles and tissue distribution (to delimitation of potential toxicity risks) after its intramuscular (i.m.) and intragastric (i.g.) administration to experimental pigs. The study entered female Landrace pigs (Sus scrofa f. domestica), 4-5 months old animals, 29+-3.2 kg of body weight. Before the HI-6 DMS administration (i.m. injection or i.g. using a gastric tube), vena auricularis was cannulated (under general anaesthesia) for collection of blood samples. The tissue distribution study was carried out at expected t-max. Concentrations of HI-6 DMS in blood plasma and other tissue samples were detected by means of HPLC method. Fast absorption after i.m. administration, relatively slow absorption and no even elimination after i.g. administration were found. Tissue distribution showed low accumulation in the liver, but a higher content in the kidneys and high concentrations in the brain and gastrointestinal wall.Plasma time profiles after i.g. administration has a prolonged pharmacokinetics. Tissue distribution study showed potential side effects to the stomach due to a higher accumulation of HI-6 in this tissue after i.g. administration but not after a standard i.m. administration. Higher content of HI-6 in the kidneys after i.m. administration suggests the main way of the oxime elimination.
  • Oxime HI-6 DMS (dimethanesulfonate) is an asymmetric bispyridinium aldoxime and essential acetylcholinesterase (AChE) reactivator. The high effectiveness is due to its wide spectrum of therapeutic activity against different structures of nerve agents. Aim of this study was to compare plasma time profiles and tissue distribution (to delimitation of potential toxicity risks) after its intramuscular (i.m.) and intragastric (i.g.) administration to experimental pigs. The study entered female Landrace pigs (Sus scrofa f. domestica), 4-5 months old animals, 29+-3.2 kg of body weight. Before the HI-6 DMS administration (i.m. injection or i.g. using a gastric tube), vena auricularis was cannulated (under general anaesthesia) for collection of blood samples. The tissue distribution study was carried out at expected t-max. Concentrations of HI-6 DMS in blood plasma and other tissue samples were detected by means of HPLC method. Fast absorption after i.m. administration, relatively slow absorption and no even elimination after i.g. administration were found. Tissue distribution showed low accumulation in the liver, but a higher content in the kidneys and high concentrations in the brain and gastrointestinal wall.Plasma time profiles after i.g. administration has a prolonged pharmacokinetics. Tissue distribution study showed potential side effects to the stomach due to a higher accumulation of HI-6 in this tissue after i.g. administration but not after a standard i.m. administration. Higher content of HI-6 in the kidneys after i.m. administration suggests the main way of the oxime elimination. (en)
Title
  • HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs
  • HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs (en)
skos:prefLabel
  • HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs
  • HI-6 oxime (an acetylcholinesterase reactivator): blood plasma pharmacokinetics and organ distribution in experimental pigs (en)
skos:notation
  • RIV/00216208:11150/14:10283810!RIV15-MSM-11150___
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • I, V
http://linked.open...iv/cisloPeriodika
  • Suppl. 2
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
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  • 19339
http://linked.open...ai/riv/idVysledku
  • RIV/00216208:11150/14:10283810
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • pigs; tissue distribution; pharmacokinetics; oxime; HI-6; acetylcholinesterase reactivator (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • SE - Švédské království
http://linked.open...ontrolniKodProRIV
  • [C0089DD6CC4B]
http://linked.open...i/riv/nazevZdroje
  • Neuroendocrinology Letters
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 35
http://linked.open...iv/tvurceVysledku
  • Bureš, Jan
  • Kuča, Kamil
  • Kuneš, Martin
  • Květina, Jaroslav
  • Musílek, Kamil
  • Pavlík, Michal
  • Tachecí, Ilja
  • Žďárová Karasová, Jana
http://linked.open...ain/vavai/riv/wos
  • 000351064900025
issn
  • 0172-780X
number of pages
http://localhost/t...ganizacniJednotka
  • 11150
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