Effect of proteolytic enzymes on antibiotic distribution when the preparations are administered by different routes]

The effect of proteolytic enzymes, such as terrilitine and chymotripsin on pharmacokinetics of morphocycline and streptomycin in rats after their administration by various routes was studied comparatively. The oral use of the enzymes or their introduction directly into the duodenum simultaneously or 30 minutes before the antibiotic administration did not increase the morphocycline and streptomycin levels in the biosubstrates tested. A tendency to a decrease in the serum and organ levels of the antibiotics in animals when used orally in combination with the enzymes was noted. When the drugs were administered intramuscularly, the morphocycline serum and organ levels in the rats increased insignificantly, while the streptomycin levels increased significantly. Administration of formalin as a stressor had an analogous effect which provided a supposition of a possibility of non-specific effect of the enzymes of distribution of the antibiotics on intramuscular injection of the enzymes in large doses having a local irritating effect.     

The blood anticoagulant system in rats perorally administered a heparin-acetylsalicylic acid complex]

Heparin/acetylsalicylate complexes (1:9 and 10:1) were obtained in vitro. Single or chronic (7-8 days) per os administration to white rats of 0.1% solution of the heparin/acetylsalicylate complex (0.3 ml/200 g body weight) enhanced anticoagulative properties of blood plasma, increased the fibrinolytic activity in respect of stabilized fibrin, and diminished the thrombin-induced platelet aggregation.     

Effect of flurbiprofen and acetylsalicylic acid on the ultrastructure of blood platelets

Flurbiprofene or acetylsalicylic acid did not change the structure of inactivated platelets. With flurbiprofene 50% aggregation inhibition was obtained at 10(-6) to 10(-5) M concentrations. To obtain the same result with acetylsalicylic acid, 10(-4) to 10(-3) M concentrations were necessary. With both agents, shape change was inhibited. The platelets in the small aggregates did not have the normal stretched dumb-bell shape but remained globulous and emitted a broad pseudopode containing normally-repolymerized microtubules.     

Prevention of reinfarction with acetylsalicylic acid]

A report is presented on the prospective trial for prophylaxis of myocardial reinfarction by means of acetylsalicyclic acid. For the first time it was organized on the basis of population. 1,340 patients were treated with acetylsalicylic acid or placebo respectively for 22 months on an average. There were 24 cases of reinfarction in the group of treatment and 51 in the placebo group. The difference is significant.     

Fibrinolytic complexes of low-molecular heparin and acetylsalicylic acid]

Complexes of low-molecular heparin with acetylsalicilic acid was formed in vitro when the weight ratio of components was 1:1, 1:5 and 5:1, respectively. All the complexes possessed fibrinolytic and anticoagulating activities. The complex possessed the highest activity when the ratio of heparin to acetylsalicilic acid was 5:1. This complex at a dose 1 mg/200 g of rat weight had the largest thrombolytic effect on the experimental fresh thrombus.     

Estimation of absorbed cadmium in tissues of male and female albino rats through different routes of administration

The resultant effects of cadmium exposure are seen in almost all the systems of the body, however, this study is designed to quantify its accumulation in tissues of animals exposed to cadmium. The rats were divided into two distinct groups of males and females, which were then divided into three groups, each for the monitoring of exposure. Group 1 served as control male and female and received normal rat chow and tap water. Group 2 males and females were treated with 5 mg/kg body weight of cadmium chloride (Cd) intraperitoneally for eight days while Group 3 males and females rats received 100 ppm of Cd in drinking water for 18 days. The concentrations of cadmium were analyzed in tissues (lung, stomach, kidney, heart, spleen, blood) by AAS. There were significant (P.     

Clinical-experimental studies on the inhibition of thrombocyte function with acetylsalicylic acid and with indobufen]

The mode of action of two inhibitors of platelet function is reported. At low doses both substances inhibit platelet aggregation, at higher doses they inhibit the availability of platelet factor 3 and liberation of platelet factor 4. Acetylsalicylic acid, however, possesses a long-lasting effect produced by irreversible acetylation of platelet membrane. This was demonstrated in a series of clinico-experimental studies in which 14C-labelled ASA was used. Indobufen was found to cause transitory changes of platelet function. It is easily washed out from platelets and binds loosely to cytosol proteins of platelets, as shown in studies with 14-C-labelled indobufen. In contrast to ASA, it exerts an effect on platelets lasting for a few hours only.     

Effect of different estro-progesterone sequences on nidation of dormant blastocysts administered in diapause in ovariectomized rats]

The hormonal condition permitting delayed nidation in rats ovarectomized on day 4 or 5 of pregnancy was studied by administering progesterone and estradiol in differents sequences between days 9 and 14. The best result was obtained when progesterone was given 3 days before an estrogen-progesterone association. The same treatment induced delayed nidation in rats receiving Reserpine and ovariectomized day 5, but not when progesterone and estradiol were present day 4.     

Ampicillin concentration in the blood when administered by jet injection and needle-syringe methods]

The studies were carried out on 50 persons. Ampicillin was administered with the help of a jet injector B1-2 and needle syringe in doses of 250 or 500 and 500 mg respectively. When the drug was administered by infusion, its maximum blood levels were achieved earlier than after needle-syringe administration of the drug and were higher (22.83+/-4.10 and 6.3+/-0.09 gamma/ml respectively). Even when ampicillin was administered with the help of the injector in a dose of 250 mg its blood levels were much higher than those after needle-syringe administration in a dose of 500 mg. After jet infusion the prolongation of the drug retention time in the blood at therapeutical levels was observed as compared to the needle-syringe administration.     

Lysozyme activity in the leukocytes and blood serum of white rats administered massive doses of penicillin preparations]

Activity of lysozyme in the blood serum and leucocytes was determined. The experiments were carried out on albino unbred rats weighing 170 to 200 gm. Benzylpenicillin and oxacillin were administered intramuscularly in doses of 500000 Units/kg or 20000 gamma/kg once every 24 hours for 2, 4 and 6 days. The activity of lysozyme was determined by the turbidimetric and agar-diffusion methods. It was found that the activity of lysozyme in the leucocytes increased by the 5th day accompanied by a simultaneous decrease in its level in the serum followed by reaching the initial values. The data are indicative of the fact that the use of antibiotics in mega-doses is not contraindicated from the point of view of their effect on lysozyme activity.     

The effect of suloctidil and acetylsalicylic acid on eicosanoid synthesis in human platelets]

The study aimed at comparing an effect of suloctidil and acetylsalicylic acid on malonyldialdehyde levels resulting from the arachidonic acid metabolism in blood platelets. It was shown that inhibitory effect of suloctidil is more potent than that of acetylsalicylic acid. Therefore the first is more inhibitor of an enzymatic metabolism of arachidonate in blood platelets than the latter.