[The interactions of abiraterone and its pharmacologically active metabolite D4A with cytochrome P450 2C9 (CYP2C9)]. / Vzaimodeistvie abiraterona i ego farmakologicheski aktivnogo metabolita D4A s tsitokhromom R450 2S9 (CYP2C9).

Interactions of cytochrome P450 2C9 (CYP2C9) were studied with the antitumor drug abiraterone and its pharmacologically active metabolite D4A, promising as an agent for prostate cancer treatment. It was shown by absorption spectroscopy, that both investigated compounds induced spectral changes of CYP2C9, indicating interactions of the pyridine nitrogen atom with the heme iron ion of the active site of the enzyme, but interactions of the ligands with the enzyme could be mediated by a water molecule bound to the heme iron ion. Based on the spectral changes, the values of dissociation constants (KS) for complexes of abiraterone and D4A with CYP2C9 were calculated as 1.73±0.14 µM and 3.95±0.16 µM. Both compounds inhibited O-demethylase activity of CYP2C9 towards its substrate. At 100 µM concentration of naproxen the concentrations of abiraterone, D4A and sulfaphenazole inhibiting CYP2C9 activity by 50% (IC50) were determined as 13.9 µM, 40 µM and 41 µM, respectively. The obtained results can be used for prognosis of drug-drug interactions at CYP2C9 level during administration of abiraterone or D4A as an antitumor agent for prostate cancer treatment in complex pharmacotherapy.

[The first successful bilateral lung transplantation in Russia].

Lung transplantation is one of the most difficult fields of contemporary transplantology. The operation was performed on a 53-year-old female who had been suffering from terminal stage COPD. The period of cold ischemia for the right and left lung was 1 hour 30 minutes and 2 hours 25 minutes respectively. The total operation time was 4 hours and 40 minutes. There were no surgical complications. There were no signs of transplant rejection 6 weeks after the operation. The considerable decrease in dispnea and increase in quality of life were registered during the follow-up. FEV1 was increased by 80% and 6 minute walk test distance was increased by 200 meters.

[Erythrocyte and microcirculatory functions during artificial circulation]. / Sostoianie éritrotsitov i mikrotsirkuliatsii pri iskusstvennom krovoobrashchenii.

Erythrocyte morphology, their aggregation ability and microcirculatory pattern in the mesentery of the small intestine have been studied stepwise on 12 dogs under artificial blood circulation. It has been shown that erythrocyte lesions followed by pathological aggregation play an important role in the pathogenesis of microcirculatory failure. Prolonged artificial circulation provokes structural reorganization in erythrocytes, thus affecting both blood rheology and gas exchange.