Monitoring the Level of 14C-Labelled Selegiline Following Oral Administration.

BACKGROUND: Selegiline [(-)-deprenyl] is widely used for the treatment of Parkinson's disease in humans. OBJECTIVE: Time-dependence of tissue distribution of selegiline following per os administration to rats. METHOD: Oral administration of radiolabeled selegiline to rats resulted in a pattern of tissue distribution similar to that following intraperitoneal injection. Analyses were done using both reversed-phase HPLC and also by counting radioactivity in various body compartments of rats. RESULTS: As a consequence of oral administration of 30 mg/kg of selegiline, its level in the stomach was extremely high (179.57 µg/g tissue through 54.67 µg/g at 15 min to 120 min), that is one magnitude higher than that in the serum level. High selegiline concentrations were also detected in the lacrimal glands (7.45 µg/g), kidneys (6.87 µg/g), livers (6.01 µg/g) and lungs (3.47 µg/g) after 30 minutes of application, which were higher than after intraperitoneal injections. CONCLUSION: The relatively high tissue levels remained for 120 min monitoring. Selegiline levels in the brain (1.69 µg/g) and in the testes (1.88 µg/g) were also considerably higher than following intraperitoneal administration during the entire period of observation (15 to 120 min).

Distribution of N-methyl-(14)C-labeled selegiline in the rat.

Tissue distribution of selegiline including N-methyl-(14)C-selegiline was studied with three different techniques. Whole body autoradiography of labeled selegiline in rats completed the former results obtained in mice. Counting radioactivity by liquid scintillation method in various body compartments gave an in-depth numerical estimation of distribution, while RP-HPLC determination of selegiline determined the fate of intact, non-metabolized parent compound. Whole body autoradiography following 15 and 60 min of intraperitoneal application of N-methyl-(14)C-selegiline verified definite and time-dependent blood-brain penetration of selegiline. Quantitative determination of tissue concentrations by liquid scintillation and RP-HPLC methods following 5, 15, 60 and 180 min of intraperitoneal administration of selegiline unanimously verified both blood-brain and blood-testis penetration of the compound through the barrier.

[Association of congenital chromosome abnormalities and malignant diseases]. / A veleszületett kromoszóma-rendellenességek és a malignus megbetegedések társulása.

Chromosome studies were carried out on 112 children with acute leukemia and 10 children with solid tumor. Acquired chromosome abnormalities were identified shown in 52% of patients with hematologic disorders (ALL 40%, ANLL 64%) and in four of 10 patients with non-hematologic disorders. Six patients had a constitutional chromosome aberration: three of them with ANLL and one child with ALL had trisomy 21, an other one with ALL had balanced translocation [t(2;7)] of maternal origin, and one child with Wilms' tumor-anirida syndrome had del(11)(p13). Two Down syndrome children with ANLL had additional acquired karyotypic changes. One of the Down's syndrome patients with ANLL M2 had t(8;21), the karyotype of the leukemic cells was: 47, XY, t(8;21) +21c. The other case with 21;21 centric fusion had hyperdiploidy, extra chromosomes were: +8, +14, +19, +20. It is very important to distinguish acquired and constitutional abnormalities in tumor cells.