[Intermediary effectiveness of procaine and procaine metabolites following oral administration].
The influence of orally administrated procaine hydrochloride and of its metabolites diethylaminoethanol, monoethylaminoethanol and ethanolamine on specific intermediary processes in rats was tested. While the animals got procaine hydrochloride in a single dose or via food the incorporation rate of amino acids in protein was measured in homogenisates of liver tissue by the incorporation of a mixture of 14C-amino acids. Procaine hydrochloride, the commercial product K. H. 3, as well as diethylaminoethanol, monoethylaminoethanol and ethanolamine increased the amino acid incorporation rate in a dose and time dependent mode, while p-aminobenzoic acid remained without any effect. The dose of procaine hydrochloride inducing a maximal reaction was in the range of 50 to 100 mg/kg b. w. (250 to 500 mg/kg food). The minimal active dose was nearly at 10 mg/kg b. w. Paying regard to a metabolic factor of 10 the effective dose-range is nearly the dose used in experience with human beings to influence geriatric complaints. In the study described here haematoporphyrine (a component of the commercial product K. H. 3, not absorbed) shows no specific intermediary effect. May be it promotes the intestinal absorption of procaine hydrochloride by protection against intestinal hydrolysis. The intermediary effect of procaine hydrochloride is to measure on cellular or subcellular level without compatibility to the activity as a local anaesthetic. With regard to other intermediary effects mentioned in the literature like growth promotion or inhibition of monoamine oxidase activity, it is discussed whether the increase of the hepatic amino acid incorporation rate is corresponding to geriatric experiences made with procaine hydrochloride.
Kaemmerer
K
K
Institut für Pharmakologie, Toxikologie und Pharmazie, Tierärztlichen Hochschule Hannover.
Kietzmann
M
M
D000818:Animals; D046508:Culture Techniques; D004305:Dose-Response Relationship, Drug; D019856:Ethanolamine; D004983:Ethanolamines / Q000494:pharmacology*; D006415:Hematoporphyrins / Q000494:pharmacology; D008658:Inactivation, Metabolic; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects; D011343:Procaine / Q000493:pharmacokinetics / Q000494:pharmacology*; D014176:Protein Biosynthesis; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D004983:Ethanolamines; D006415:Hematoporphyrins; D011343:Procaine; D019856:Ethanolamine; C007369:2-diethylaminoethanol
Untersuchungen zur intermediären Wirksamkeit von Procain und Procainmetaboliten nach oraler Verabreichung.