Summary
The tissue distribution of radioactivity after oral administration to rats of 14C-heteronium bromide is measured by liquid scintillation counting and the results expressed as specific activity and percentage of administered radioactivity. From the data obtained in blood, liver, kidney, stomach, duodenum, cecum, large intestine and stool some conclusions can be drawn. Heteronium bromide undergoes a rapid systemic absorption, the radioactivity being present as early as 15 min from the administration, in all the tested organs. The blood levels show two peaks: one at 120 min and a second at 360 min. This diphasic behaviour can be explained either by the presence of an active enterohepatic circulation, as indirectly indicated by the data from liver and duodenum, or by a transient shift of the molecule from blood to other tissues, rich in polysulfuronic acids. The principal route of excretion is represented by the kidney, where consistent levels are reached at 120 min, while the intestinal route becomes evident at 240 min and reaches its maximum at 720 min. The complete metabolic cycle of the compound is long lasting, since in all the tested tissues, marked radioactivity levels are still present after 720 min. The pharmacokinetic profile obtained, suggesting a long persistence of the drug and/or of its metabolites in the organism, is in agreement with previous pharmacodynamic data showing a long lasting action for heteronium bromide.
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Chernish, S. M., Resenak, B. D.: The effect of a new anticholinergic drug, heteronium bromide, on basal gastric secretion. Amer. J. dig. Dis. 10, 697–704 (1965)
Goodman, S., Smyrniotis, F. E., Funahashi, A.: Evaluation of the antisecretory effect of a new anticholinergic agent: heteronium bromide. Amer. J. dig. Dis. 14, 305–314 (1969)
Kasich, A. M.: A double-blind study of heteronium bromide and amobarbital in the management of gastrointestinal conditions associated with anxiety. Curr. ther. Res. 10, 508–513 (1968)
Petroff, C. P., Patt, H. H., Nair, P. P.: A rapid method for dissolving tissue for liquid scintillation counting. Int. J. appl. Radiat. Isot. 16, 599–601 (1965)
Vertua, R., furlani, A.: Distribution of radioactivity in the tissues of young and adult rats after administration of tritiated haloperidol. Europ. J. Pharmacol. 3, 347–350 (1968)
Vincenzi, L., Ubezio, G., Corsi, C.: Azione di un nuovo anticolinergico associato ad un ansiolitico sulla secrezione acida basale dello stomaco in ulcerosi duodenali. Atti Accad. Med. Lomb. 23, 1504–1506 (1968)
Waser, P. G.: Localization of 14C-pancuronium by histo- and wholebody-autoradiography in normal and pregnant mice. Naunyn-Schmiedeberg's Arch. Pharmacol. 279, 399–412 (1973)
Zaterka, S., Honda, S., Pfuhl Neves, D.: The effect of heteronium bromide on basal gastric secretion and on gastric secretion “maximally” stimulated by histalog and by insulin. Arquiv. Gastroenterol. 4, 39–43 (1967)
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Traversa, U., De Angelis, L. & Vertua, R. Tissue distribution of 14C-heteronium bromide: Radioactivity levels at different time intervals after oral administration in the rat. Naunyn-Schmiedeberg's Arch. Pharmacol. 294, 109–113 (1976). https://doi.org/10.1007/BF00507842
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DOI: https://doi.org/10.1007/BF00507842