PubMed · 13509612
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E JACOBSEN. 1958. Benactyzine.. https://pubmed.ncbi.nlm.nih.gov/13509612/
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Benactyzine and drofenine are widely used anticholinergic drugs. Benactyzine is used to treat organophosphate poisoning and drofenine acts on smooth muscle to stop muscle spasms. Both of these drugs are esters. After they enter the bloodstream, they will interact with butyrylcholinesterase (BChE; acylcholine acyl hydrolase: EC 3.1.1.8), which has an ability to hydrolyze a wide variety of esters. Therefore, the kinetic analysis of their inhibitory effects on human serum BChE was examined using butyrylthiocholine as substrate. Both drugs were competitive inhibitors of BChE and the Ki values of benactyzine and drofenine were calculated to be 0.010 +/- 0.001 and 0.003 +/- 0.000 mM, respectively, using the Systat (version 5.03, 1991) nonlinear regression analysis software package. According to these parameters, drofenine is a more potent competitive inhibitor of BChE than benactyzine.
The stability of benactyzine in a multicomponent injectable antidote formulation in deuterium oxide was studied in the presence of various concentrations of trimedoxime bromide. Benactyzine was found to be more stable in the absence of trimedoxime bromide and its degradation rate accelerated linearly with increasing concentrations of trimedoxime bromide. The main reasons for the accelerated decomposition rate of benactyzine were found to be the nucleophilic effect of the bromide ion and the oxime moiety. For each trimedoxime concentration studied, t90 for benactyzine at 25 degrees C was calculated and was found to be 5.3-1.5 years within the concentrations range of 0-120 mg/ml. Rate constants and activation energies for benactyzine degradation were determined for each of the concentrations studied.
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