Applications of cholinesterase inhibitors.
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Biomedical subjects
Publications and source records attributed to H Reinbold.
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Psychopharmacological agents may cause changes in receptor sensitivity. Long-term treatment with high doses of neuroleptics has been shown to lead to supersensitivity of postsynaptic dopamine and noradrenaline receptors. Receptor supersensitivity is seen more frequently with neuroleptics known to have a high receptor affinity. The mechanism by which psychoses of the supersensitivity type work is presented and is illustrated by two case reports. Possible pathophysiological mechanisms for the emergence of these psychoses and implications for the treatment of patients suffering from them are discussed.
The authors report on two years of experience collected during jointly performed medico-pharmaceutical visits in a psychiatric hospital. From the viewpoint of quality assurance and quality control such a procedure has now gained topical importance. Attention is drawn to problematic drug regimens and interactions between drugs.
The chemotherapeutic activity of 12 newly synthesized nitrosoureas was compared in tests using Yoshida sarcoma ascites cells implanted into the wall of the descending colon in Sprague-Dawley rats. Cyclophosphamide and the nitrosoureas BCNU, MeCCNU, and chlorozotocin served as positive controls. Among the nitrosoureas tested, 1-(2-hydroxyethyl)-3-(2-chloroethyl)-3-nitrosourea (hydroxyethyl-CNU), chlorozotocin, 1-(2-chloroethyl)-1-nitroso-3-(4-morpholino) urea, 1-(2-chloroethyl)-1-nitroso-3-(1-piperidino) urea, 4-[1-(2-chloroethyl)-1-nitroso-3-[4-(2,6-dimethylmorpholino)] urea, and 1-(2-chloroethyl)-1-nitroso-3-(3,4-methylenedioxybenzyl) urea were found to be the most active compounds in this tumor model. Based on the present results, morpholino-CNU is considered the most promising compound among these newly synthesized BCNU analogues.
Three thousand Yoshida sarcoma cells were inoculated into the wall of the descending colon of each of 120 male Sprague-Dawley rats. On day 8 after the tumor implantation, the animals were at random divided into four groups of 30 rats each. The effect of cyclophosphamide (70 mg/kg), BCNU (25 mg/kg), and methyl-CCNU (45 mg/kg) after single i.p. application was investigated. The Yoshida sarcoma transplanted into the colon is sensitive to all three chemotherapeutic drugs. At the doses given cyclophosphamide showed the best results. The two nitrosoureas had a comparable antitumor activity but methyl-CCNU showed a more distinct toxic effect. The introduction of this model for testing new cytostatics in animal experiments is discussed.