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Prophylactic transdermal treatment with physostigmine and scopolamine against soman intoxication in guinea‐pigs
Author(s) -
Meshulam Yacov,
Davidovici Rachel,
Wengier Ada,
Levy Aharon
Publication year - 1995
Publication title -
journal of applied toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.784
H-Index - 87
eISSN - 1099-1263
pISSN - 0260-437X
DOI - 10.1002/jat.2550150406
Subject(s) - soman , physostigmine , scopolamine , transdermal , medicine , guinea pig , pharmacology , anesthesia , parasympatholytic , nerve agent , atropine , chemistry , acetylcholinesterase , acetylcholine , muscarinic acetylcholine receptor , biochemistry , enzyme , receptor
This study was designed to evaluate the prophylactic efficacy of transdermally administered physostigmine (PHY) against soman exposure using guinea‐pigs. Transdermal PHY pad (3 cm 2 kg −1 ; 60 μg cm −2 ), containing a vehicle based on propionic acid, was applied onto the dorsal back of the animals, 24 h before exposure to the organophosphate. At the time of exposure, PHY concentrations in brain and plasma were ca. 3.6 ng g −1 and 4.1 ng ml −1 , respectively. Brain and whole blood cholinesterase (ChE) activity was inhibited to 70% and 47% of the original activity, respectively. Transdermal PHY by itself protected up to 70% of the animals exposed to 1.5 LD 50 of soman (100% mortality was recorded in the control group). Combining transdermal PHY with Scopoderm provided full protection against 1.5 LD 50 of soman (protection of 70% against 3 LD 50 ). When the prophylactic treatment was combined with post‐exposure therapy (atropine, 10 mg kg −1 ; toxogonin, 10 mg kg −1 ) 1 min after 5 LD 50 of soman, protection of 90% of the animals was achieved.