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[Diethylnicotinamid (cordiamine) stabilization of the liver hydroxylating function in rabbits with CCl4 poisoning].

Three and ten days after the administration of CCl4 (subcutaneously, once, 4 ml/kg of 50% oil solution) there were found a decrease of the rate of antipyrine elimination (intravenously, 50 mg/kg) from the blood plasma, an increase of the total bilirubin content, ALT activity and stimulation of lipid peroxidation processes. Cordiamine administration (subcutaneously, twice a day, 3 and 10 days) exerts the normalizing effect.

Alanine Transaminase↗

[Effect of various analeptics on the outcome of acute microwave lesion in mice].

The survival of albino mice irradiated by microwaves till the terminal state (wave length of 12.5 cm, intensity-62 +/- 5 microvat, for 14-16 minutes), given directly after irradiation diethylamide of nicotinic acid (cordiamine) in a dose of 50 mg/kg intraperitoneally and strychnine nitrate in a dose of 1 mg/kg, subcutaneously, i. e. nearly 1.5 times as much as received by controls, was studied. The application of caffeine sodium benzoate, camphor, metrasol, lobeline hydrochloride and cytisine, employed in different doses, proved to be little effective.

Acute Disease↗

[The effect of diethylnicotinamide (cordiamine) on the activity of the hydroxylating and glucuronyl-conjugating systems in humans].

Administration of diethylnicotinamide (250 mg orally three times for 8 days) to healthy subjects increased antipyrine (AP) elimination from the saliva by 23% and decreased its half-life by 26%. The excretion in the urine of the products of AP hydroxylation 3-carboxymethylantipyrine and nor-antipyrine as well as glucuronides 3-hydroxymethylantipyrine increased. A positive correlation between the dynamics of the excretion of antipyrine metabolites and glucuronic acid was observed. The elimination from blood of bilirubin glucuronides increased. Diethylnicotinamide in therapeutic doses is supposed to stimulate the processes of hydroxylation and glucuronyl conjugation in humans.

Adult↗

[A comparative study of the effects of nicotinamide and diethylnicotinamid on hepatic monooxygenase, glucuronyl and glutathione conjugating systems].

The nicotinamide administration to rats (50 mg/kg, subcutaneously, over 5 days) increased the concentration of liver cytochrome b5, the activities of cytosol and microsomal glutathione S-transferase, UDP-glucuronosyltransferase and urinary excretion of bound glucuronic acid by 26.7, 33.1, 33.3, 53.0 and 31.0%, respectively. The chloral hydrate-induced sleep time in mice was reduced by 65%. Under similar experimental conditions the administration of equimolar amounts of diethylamide of nicotinic acid (75 mg/kg) exerted a more pronounced enzyme-stimulating effect. The cytochrome P-450 concentration, the activities of cytosol and microsomal glutathione S-transferase, UDP-glucuronosyltransferase as well as the sulphobromophthalein elimination from blood plasma and urinary excretion of bound glucuronic acid were increased by 37.0, 33.1, 54.6, 80.5, 24.5 and 49.0%, whereas the chloral hydrate-induced sleep time decreased by 75%. The nicotinamide and diethylamide of nicotinic acid stimulating effects on xenobiotic biotransformation in rat liver are assumed to be due to enhanced NADPH, glutathione and UDP-glucuronic acid biosynthesis as well as their antioxidant properties.

Animals↗

[Effect of the diethylamide of nicotinic acid (cordiamine) on the hydroxylating function of the liver].

Diethylamide of nicotinic acid (subcutaneously, 40 and 120 mg/kg, once a day for 4 days) was shown to exert no influence on p-hydroxylation of aniline and to increase the rate of N-demethylation of amidopyrine and ethylmorphine in the rat liver microsomal fraction by 21 and 47% as compared with the control. At the same dose of 40 mg/kg and the same schedule of administration the drug was found to increase urine excretion of antipyrine metabolites: nor-antipyrine, 4-hydroxy-antipyrine and the sum of metabolites by 229, 89 and 80%, respectively, during the first 90 min of the experiment. Excretion of antipyrine, 3-hydroxymethyl-antipyrine and 3-carboxymethyl-antipyrine underwent no significant changes. The duration of hexobarbital-induced sleep of the rats was shown to be decreased by 26%.

Aminopyrine↗

[Antisoporific and cardiotropic properties of new amino acid derivatives of nicotinic acid].

On the models of urethane, nembutal and ethyl alcohol sleep it was shown that nicotinoylcapronate, nicotinoylserine and nicotinoylvaline possess antihypnotic properties being superior to those of cordiamine and on some models phenamine. Nicotinoylvaline and nicotinoylalanine normalized the myocardial contraction in animals with experimental ischemia.

Alanine↗

[Interaction in vitro of nicotinamide and diethylnicotinamid (cordiamine) with enzymes of the liver microsomal hydoxylating system in the rat].

Addition of nicotinamide and diethylnicotinamide (cordiamine) to rat liver microsomes leads to the formation of an enzyme-substrate Type II complex with cytochrome P-450. Diethylnicotinamide exceeded nicotinamide approximately 2-fold as regards the degree of the affinity to the enzyme. The ability of nicotinamide and diethylnicotinamide to interact with cytochrome P-450 underlies their antagonism with respect to in-vitro metabolism of the substrates of both Type I (amidopyrine) and Type II (aniline) as well as with respect to the competition with CO for the common center of binding on the enzyme.

Aminopyrine↗