[The action of Essentiale and its combination with cordiamine and vitamin E on the processes of xenobiotic biotransformation and lipid peroxidation and on liver structure in rats with cholestasis]. / Deistvie essentsiale, ego kombinatsii s kordiaminom i vitaminom E na protsessy biotransformatsii ksenobiotikov, perekisnogo okisleniia lipidov i struktury pecheni krys s kholestazom.

Intensive regeneration of cholangia and cholangioles, fibrosis, microglobular cirrhosis, vacuolar and granular dystrophy, and necrosis of hepatocytes were found in the liver of rats 36 days after ligation of the common bile duct. Lipid peroxidation was activated, the activity of the mono-oxidase system was inhibited in maintained function of glucuro- and glutathione transferase. Essentiale (per os in starch mucilage, 1 ml/kg. for 35 days) increased the activity of cytosol glutathione-S-transferase and normalized the decreased blood plasma antioxidant activity. Combination of essentiale with cordiamin (nikethamide) and viatmin E (50 mg/kg for 35 days) considerably activated the mono-oxigenase, glucoro- and glutathione transferase systems of the liver: the free-radical processes became less intense. The structure of the liver improves insignificantly in both methods of treatment.

[Effects of oxygen and nikethamide on central drive, ventilation and blood gases of patients with obstructive lung disease in acute exacerbation of respiratory failure].

Twelve subjects with COPD in acute exacerbation of respiratory failure were studied. The experiment of each subject was divided into three steps: room air breathing, 35% O2 inhalation for one hour, and then intravenous drip of nikethamide (1.875g) for two hours with 35% oxygen inhalation at the same time. At the end of each step, mouth occlusion pressure (P0.1), VT, VE, VA, VCO2, VD and PaO2, PaCO2 were measured respectively. The results showed that, when breathing air, all the patients presented significant higher P0.1 than normal subjects, indicated higher central drive. After oxygen inhalation, P0.1 decreased markedly, but still higher than normal. No correlation was found between delta P0.1 and delta PaO2. VE declined with the drop of P0.1, but this was due to a decrease of respiratory frequency, while VA remained unchanged (P > 0.05). The increase of PaCO2 was unremarkable. Neither correlation was found between delta VA and delta P0.1, nor between delta VA and delta PaCO2. However, a close correlation existed between delta VCO2/VCO2 and delta VE/VE. The result of our study is not consistent with the postulation, the removal of the hypoxic stimulate after oxygen administration results in a decrease of ventilation and CO2 retention. After nikethamide administration, P0.1 increased as well as VE while VA and PaCO2 remained unchanged. The increase of VE was caused by the increase of respiratory rate. Furthermore, PaO2 decreased in some patients. All of the changes demonstrated that nothing is worthwhile with the treatment of nikethamide, but a side effect from increasing work of breathing and consumption of oxygen.(ABSTRACT TRUNCATED AT 250 WORDS)

[Correction of disorders in the monooxygenase system function with diethylnicotinamide (cordiamine) in tetrachloromethane- induced and viral hepatitis]. / Korrektsiia diétilnikotinamidom (kordiaminom) narusheniia funktsii monooksigenaznoi sistemy pri tetrakhlormetanovom i virusnom gepatitakh.

Content of cytochromes P-450 and b5 and the rate of oxidative dealkylation in liver microsomes as well as the antipyrine pharmacokinetics were normalized in rats with acute CCl4-induced hepatitis after treatment with cordiamine (diethyl nicotinamide) at a dose of 40 mg, subcutaneously, 2 times daily within 4 days. Cordiamine (30 drops 3 times daily within 8 days) contributed to normalization of the hydroxylating reaction in liver tissue of patients with viral hepatitis A, estimated by the "antipyrine" test. The drug exhibited stabilizing effect on hydrophobic interactions in microsomal membranes; diethyl nicotinamide possessed antiradical and vitamin properties.

[Diethylnicotinamid (cordiamine) stabilization of the liver hydroxylating function in rabbits with CCl4 poisoning]. / Stabilizatsiia diétilnikotinamidom (kordiaminom) gidroksiliruiushchei funktsii pecheni krolikov pri otravlenii CCl4.

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.

Animal studies on the treatment of poisoning by amitraz (a formamidine pesticide) and xylene.

In Charles River CD rats the pesticide MITAC 20 EC (containing amitraz and 75% xylene) given orally at an LD80 dose caused toxicity featuring hypothermia, reduced spontaneous activity, episodes of increased activity and minor signs of general debilitation. Recovery in survivors was complete within about 8 days. Therapies including absorption retardants, diuretics, reduction of urine pH, thermal support and treatment with phentolamine or nikethamide were given to groups showing these signs of poisoning. None of the therapies gave consistent evidence of benefit during acute poisoning in terms of reduced intensity or duration of symptoms or reduced mortality. Comparison with animals given amitraz alone suggested that the hypothermia and the later phase of reduced spontaneous activity were attributable to the pharmacological effects of amitraz. While the product was apparently more acutely toxic by the oral route than xylene alone, the evidence was that xylene caused the early signs of poisoning. This work indicates that any case of poisoning by ingestion of MITAC 20 EC should initially be treated for the xylene exposure. There is no specific therapy or antidote for the subsequent possible pharmacological effects of amitraz. Many other pesticides also contain high proportions of aromatic solvents and the importance of the solvent in cases of ingestion is seen to be applicable to a variety of pesticides as well as MITAC 20 EC.

Hepatic enzymes, their induction and usefulness in predicting maximal serum bilirubin levels in premature newborn infants.

Sixty-seven babies were utilized to (a) document the serum bilirubin lowering effect and safety of a phenobarbitone and nikethamide combination in neonatal hyperbilirubinaemia of non-hemolytic origin; (b) determine whether birthweight and/or SGOT, SGPT or SGGT activity on day one of life correlated with the maximum serum bilirubin level achieved; and (c) investigate the pattern of hepatic enzyme levels in serum under normal conditions anf following drug induction. Results indicate a significantly lower serum bilirubin level in the treated group of babies. Birthweight and day one SGGT levels, and SGGT/birthweight ratio correlated well with the maximum serum bilirubin reached, the latter ratio being particularly useful in predicting the degree of hyperbilirubinaemia.

[Effect of various analeptics on the outcome of acute microwave lesion in mice]. / Vliianie nekotorykh analeptikov na iskhod ostrogo mikrovolnovogo porazheniia myshei.

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.