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Statements

Subject Item
n2:RIV%2F00216208%3A11150%2F13%3A10138882%21RIV14-MSM-11150___
rdf:type
skos:Concept n7:Vysledek
rdfs:seeAlso
http://dx.doi.org/10.1002/jat.1699
dcterms:description
K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-propane dibromide] is a promising new reactivator of organophosphate- or organophosphonate-inhibited acetylcholinesterase (AChE) with low acute toxicity and broad spectrum efficacy. The aim of the present study was to compare the pharmacokinetics of both compounds. Male Wistar rats (body weight = 320 +- 10 g) were administered a single intramuscular dose of K027 (22.07 mg kgMINUS SIGN 1) and an equimolar dose of trimedoxime. Blood was collected at various time intervals until 180 min. Plasma samples were analyzed by reversed-phase HPLC with ultraviolet (UV) detection. The recovery of both oximes from the plasma was approximately 90% and a linear relationship (R2 > 0.998) was observed between the peak areas and concentrations of calibrated standards in the range 1-100 µg mlMINUS SIGN 1. Near-identical plasma profiles were obtained for both compounds. No differences were found in the mean +- SD values of Cmax (18.6 +- 2.5 vs 20.0 +- 6.3 µg mlMINUS SIGN 1, P = 0.72) and AUC0-180min (2290 +- 304 vs 2269 +- 197 min µg mlMINUS SIGN 1, P = 0.84). However, the percentage coefficient of variation of the first-order rate constant of absorption (ka) was 3-fold higher (P < 0.01) providing evidence for more erratic absorption of intramuscular trimedoxime as compared with K027. In conclusion, oxime K027 might have superior pK properties that may be translated in its faster absorption and subsequent tissue distribution. K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-propane dibromide] is a promising new reactivator of organophosphate- or organophosphonate-inhibited acetylcholinesterase (AChE) with low acute toxicity and broad spectrum efficacy. The aim of the present study was to compare the pharmacokinetics of both compounds. Male Wistar rats (body weight = 320 +- 10 g) were administered a single intramuscular dose of K027 (22.07 mg kgMINUS SIGN 1) and an equimolar dose of trimedoxime. Blood was collected at various time intervals until 180 min. Plasma samples were analyzed by reversed-phase HPLC with ultraviolet (UV) detection. The recovery of both oximes from the plasma was approximately 90% and a linear relationship (R2 > 0.998) was observed between the peak areas and concentrations of calibrated standards in the range 1-100 µg mlMINUS SIGN 1. Near-identical plasma profiles were obtained for both compounds. No differences were found in the mean +- SD values of Cmax (18.6 +- 2.5 vs 20.0 +- 6.3 µg mlMINUS SIGN 1, P = 0.72) and AUC0-180min (2290 +- 304 vs 2269 +- 197 min µg mlMINUS SIGN 1, P = 0.84). However, the percentage coefficient of variation of the first-order rate constant of absorption (ka) was 3-fold higher (P < 0.01) providing evidence for more erratic absorption of intramuscular trimedoxime as compared with K027. In conclusion, oxime K027 might have superior pK properties that may be translated in its faster absorption and subsequent tissue distribution.
dcterms:title
Pharmacokinetic study of two acetylcholinesterase reactivators, trimedoxime and newly synthesized oxime K027, in rat plasma Pharmacokinetic study of two acetylcholinesterase reactivators, trimedoxime and newly synthesized oxime K027, in rat plasma
skos:prefLabel
Pharmacokinetic study of two acetylcholinesterase reactivators, trimedoxime and newly synthesized oxime K027, in rat plasma Pharmacokinetic study of two acetylcholinesterase reactivators, trimedoxime and newly synthesized oxime K027, in rat plasma
skos:notation
RIV/00216208:11150/13:10138882!RIV14-MSM-11150___
n7:predkladatel
n8:orjk%3A11150
n3:aktivita
n18:I
n3:aktivity
I
n3:cisloPeriodika
1
n3:dodaniDat
n10:2014
n3:domaciTvurceVysledku
n12:2975858 n12:1802054
n3:druhVysledku
n15:J
n3:duvernostUdaju
n13:S
n3:entitaPredkladatele
n17:predkladatel
n3:idSjednocenehoVysledku
95997
n3:idVysledku
RIV/00216208:11150/13:10138882
n3:jazykVysledku
n9:eng
n3:klicovaSlova
K027; trimedoxime; plasma; HPLC; pharmacokinetics; oxime; cholinesterase reactivator
n3:klicoveSlovo
n6:pharmacokinetics n6:trimedoxime n6:plasma n6:K027 n6:oxime n6:HPLC n6:cholinesterase%20reactivator
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[2E2DE05353AA]
n3:nazevZdroje
Journal of Applied Toxicology
n3:obor
n19:FR
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
6
n3:rokUplatneniVysledku
n10:2013
n3:svazekPeriodika
33
n3:tvurceVysledku
Hroch, Miloš Fusek, Josef Žďárová Karasová, Jana Kuča, Kamil Chládek, Jaroslav Hnídková, Daniela
n3:wos
000311692500003
s:issn
0260-437X
s:numberOfPages
6
n16:doi
10.1002/jat.1699
n20:organizacniJednotka
11150