[Sulfalene kinetics in the blood and cerebrospinal fluid in arachnoiditis]. / Kinetika sul'falena v krovi i spinnomozgovoi zhidkosti bol'nykh arakhnoiditom.

The kinetics of free sulfalene in the blood and cerebrospinal fluid was studied in patients suffering from chronic arachnoiditis without marked inflammation signs on the part of arachnoid after a single intake of 2 g of the drug. It was found that administration of the drug in this dose once a week is quite justified and that sulfalene penetrates well in the cerebrospinal fluid. Upon administering large doses of the drug its absorption from the gastrointestinal tract declines. Sulfalene is eliminated from the cerebrospinal fluid more slowly than from the blood. High enough drug concentration is maintained in the cerebrospinal fluid for 7 days.

[Mechanism of the effect of proteolytic enzymes on antibiotic pharmacokinetics]. / Mekhanizm vliianiia proteoliticheskikh fermentov na farmakokinetiku antibiotikov.

Possible relation between the changes in the penicillin pharmacokinetics and coagulograms under the effect of trypsin in rats and man was analysed. It was found that parenteral administration of the enzyme was accompanied by a simultaneous increase in the penicillin blood level, oliguria, a decrease in the antibiotic amount excreted with urine and drop of the fibrinogen level in plasma. The latter is consequent on intravascular coagulation which results in temporary impairment of the excretion function of the kidneys defining the changes in the penicillin pharmacokinetics under the effect of trypsin.

[Trypsin and lipase activity in the presence of antibiotics]. / Aktivnost' tripsina i lipazy v prisutstvii antibiotikov.

Effect of penicillin, kanamycin and streptomycin on the proteolytic activity of trypsin using hemoglobin and casein as substrates as well as effect of these antibiotics and oxacilin, methycillin and tetracycline on the lipase activity were studied in vitro. Penicillin, kanamycin and streptomycin (5 mg, 20 mg and 80 mg of the antibiotic per 1 mg of trypsin, respectively) did not inhibit the proteolytic activity of the enzyme. Kanamycin slightly activated the trypsin activity in reaction with hemoglobin and streptomycin -- in reaction with casein. Penicillin, oxacillin and methycillin inhibited the lipase activity, when 80-100 mg of the antibiotics were used per 1 mg of the enzyme.

[Antibiotic interaction with proteolytic enzymes]. / K voprosu o vzaimodeistvii antibiotikov s proteoliticheskimi fermentami

The effect of penicillin, tetracycline, aminoglucozide antibiotics and streptomycin on BAEE-esterase activity of trypsin was studied. It was found that benzylpenicillin in amounts of 50, 100 and 300 mg, ampicillin in an amount of 25 mg, methicillin in an amount of 12 mg and tetracycline in an amount of 2.5 mg as calculated per 1 mg of trypsin had no effect in vitro on the esterase activity of the enzyme. Neomycin, kanamycin and streptomycin in amounts of 5, 10, 100 or 300 mg per 1 mg of trypsin catalyzed splitting of BAEE by trypsin. When the antibiotics were added to the bile, its esterase activity increased. Preliminary intramuscular administration of trypsin and kanamycin to the rats had no effect on the ampicillin levels in the blood serum and brain and did not affect the permeability of the hemato-encephalic barrier as compared to the use of trypsin alone.