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[Radionuclide visualization of the superior rectal and inferior mesenteric lymph nodes in rectal cancer].

Scintigraphic image of the superior rectal and inferior mesenteric lymph nodes 7-8 cm up from the anus was obtained by presacral administration of finely divided 99mTc-colloid (close to the posterior rectal wall). The results of radiometry of the lymph nodes dissected at radical operation for rectal cancer have shown that due to the above method the radioactive indicator is accumulated in these groups of lymph nodes. Several variants of a scintigraphic picture were defined on the basis of analysis of scintigrams of 23 patients with extrarectal tumors and nontumorous diseases and 40 rectal cancer patients. Evaluation of the lymphoscintigraphy results compared with the morphological findings of the lymph nodes dissected at operation in 32 rectal cancer patients, has shown that the overall accuracy of the above method is 0.81, specificity--0.63, sensitivity--1.0.

Adult↗

[Age-related changes in glycosaminoglycans in the cell nuclei of the rat liver--biochemical and histochemical pilot studies].

Cell nuclei of the livers of 12 male Wistar rats aged 24 months, and 16 male Wistar rats aged 4 months were isolated. 0.4 microCi [3H]-glucosamine/kg body weight were administered intraperitoneally. The livers of four animals were used for each biochemical analysis. The tissue was degraded by proteolysis, the glycosaminoglycans (GAGs) were isolated and the GAG types were determined by enzyme digestion, nitrite degradation and radiometry. The amount of GAGs was photometrically determined in single samples of pooled material of each of the two age groups. In paraffin sections (from other male Wistar rats of a different age), the influence of enzymes on specific GAG staining was observed. Most of the radioactivity was found in heparan sulfate (HS) and a lower content in chondroitin sulfates (CSs). In HS the incorporation increased with increasing age. The amount of HS showed no age-related differences. The results indicate an age-related activation of the HS metabolism. The GAG pattern and the age-related changes of the GAG types in total tissue (earlier results) are different from those in the nuclei. By histochemical methods, we observed a small but distinct effect of heparitinase in the cell nuclei.

Aging↗

The metabolic disposition of norgestrel in female rhesus monkeys.

Following single intragastric doses of d- and dl-[24C]norgestrel (Ng), rhesus monkeys excreted 29.5 +/- 2.0 (SE) and 52.6 +/- 5.4% of the administered radioactivity in urine. Fecal excretion accounted for 57.1 +/- 4.0 and 37.2 +/- 4.4%, respectively. Urinary radioactivity was separated into neutral, acidic, and conjugated fractions. The neutral and conjugated fractions contained Ng; 2 alpha, 16 alpha- and 16 beta-hydroxy-Ng; 3 alpha,5 beta-tetrahydro-Ng and 16 beta-hydroxy-3 alpha,5 beta-tetrahydro-Ng and their glucuronides. However, the bulk of the radioactivity in these fractions was associated with more polar metabolites. The acidic fraction contained unstable metabolies which lose 14CO2 at pH values below 5. The most abundant of these metabolites was isolated as its stable methyl ester. The structure of a 13-ethyl-D-homogon-4-ene-3,17 alpha-dione-17 carboxylic acid is proposed for the metabolite which decomposes to 13-ethyl-D-homogon-4-ene-3,17 alpha-dione [D-homo-G]. The probable mechanism of the metabolite's formation is postulated. Quantitative differences in urinary metabolite patterns were observed following the administration of d- and dl-Ng. Ng is the major identified drug-related entity in plasma. The d-Ng concentrations in plasma measured by radioimmunoassay were in good agreement with those determined by fractionation and radiometry. The latter method indicated the presence of D-homo-G and a glucuronide of 3 alpha,5 beta-tetrahydro-Ng following the administration of d- and dl-Ng.

Animals↗

Disposition and metabolism of [14C]-haloperidol in rats.

Absorption, distribution, excretion and metabolism of [14C]-haloperidol in rats were studied after administration of 5 mg/kg. After oral and intramuscular administration, plasma levels of [14C]-haloperidol radioactivity reached the maximum at 1 h and decreased biphasically. The biphasic elimination was also observed after intravenous administration. The area under plasma level-time curve (AUC) from 0 to 24 h after intramuscular and oral administration was 110 and 87% of AUC after intravenous route, respectively. After intramuscular administration, levels of radioactivity in all tissues examined were higher than plasma and blood levels at 1 h. The lung, Harderian gland, pancreas, kidney, liver, spleen and adrenal had higher levels than other tissues. Most of tissue levels decreased virtually with similar half lives to plasma level and lowered to less than 1 microgram eq/g at 48 h, when negligible recoveries were found in most tissues. Findings concerning distribution obtained by whole-body autoradiography essentially agreed with those by above radiometry. Levels in the placenta and fetus in the pregnant rat were similar to each other and obviously higher than maternal blood level at 1 h after intramuscular administration but no radioactivity was seen in fetus at 48 h. In the lactating rat, milk levels were several times as high as plasma levels and decreased virtually in parallel with plasma levels after intramuscular administration of [14C]-haloperidol. Within 96 h after intramuscular administration, about 99% of administered radioactivity was excreted in urine (about 46%) and feces (about 53%), respectively. About 54% of radioactivity was excreted in the rat bile within 48 h after intramuscular administration. Administration of the bile obtained and thus containing [14C]-haloperidol radioactivity into the duodenum revealed that partial enterohepatic circulation occurred. After intramuscular administration, plasma contained p-fluorobenzoylpropionic acid and p-fluorophenylaceturic acid with comparable concentrations to unchanged haloperidol. Haloperidol alone could be detected in the brain. The liver, kidney, lung and submaxillary gland were also analyzed for their metabolites. Their metabolite compositions differed from each other. Unchanged haloperidol concentration was much higher in all tissues examined than that in plasma. The major urinary and biliary metabolite was p-fluorophenylaceturic acid and conjugates (glucuronide and sulfate) of haloperidol, respectively.

Animals↗

Effect of ketanserin on Raynaud's phenomenon in progressive systemic sclerosis: a double-blind trial.

Ketanserin was used in a randomized double-blind trial in 15 patients with Raynaud's phenomenon in progressive systemic sclerosis (PSS). Its effect on Raynaud's phenomenon was evaluated by IR-radiometry, Doppler ultrasound, nailfold capillaroscopy, frequency of finger ulcerations and patient complaints before and after a 3-month course of treatment with oral ketanserin in the dosage of 60 mg daily in the first month and 120 mg in the second and third months. Of the 8 patients treated with ketanserin, 5 showed improvement. In the other 2 patients with progression of skin sclerosis and multiorgan involvement, the peripheral vascular disorder was unchanged. Ketanserin treatment was discontinued in one patient owing to dizziness and anxiety. In one patient ketanserin was reduced to 60 mg daily because of fluid retention. There were no other adverse effects. In 7 control patients on placebo there was no significant improvement in Raynaud's phenomenon. Ketanserin, a selective, specific and pure antagonist of 5-hydroxytryptamine (serotonin) appears to be an effective agent in the treatment of Raynaud's phenomenon and digital ischaemic ulcers in PSS. Moreover, ketanserin could contribute to the understanding of the role of 5-hydroxytryptamine in PSS pathogenesis.

Adult↗

[Results of the clinical use of 75Se-methionine in gastroenterology with different modes of administration].

Gamma-topography of the abdominal region and radiometry of duodenal aspirates were used for examination of 707 patients with different gastroenterological pathology using various modes of the administration of 75Se-methionine (intravenously, per os, into the duodenal and cecal lumens, intra-arterially in the celiac trunk and superior mesenteric artery). The RP administered intravenously was accumulated in health in the liver and pancreas. The drug fixation by the proximal part of the jejunum was also typical of chronic pancreatitis, the degree of fixation being well correlated with a period of disease. A jejunum image on gamma-topograms proved to be determined not by radioactivity of the jejunum in passage of labeled pancreatic juice but by extraction of the radionuclide from the blood by its wall. In transduodenal administration of the radionuclide its major part was rapidly absorbed and accumulated in the liver. At the same time a considerable part of the drug remained at the site of administration and retained there for several days. There was almost no absorption of the drug in the cecum and ascending colon. Like in the duodenum, the drug retained at the site of administration for a long time. Intestinal extravasal trophicity was assumed.

Administration, Oral↗

[Morphofunctional characteristics of the recovery processes in the resected thyroid of rats].

Histological, electron microscopy and radiometry methods were used to study the time-course of the recovery of the morphological and functional parameters of the rat thyroid after resecting 2/3 of the organ. The signs of thyrocyte regeneration, namely hypertrophy of the cells and ultrastructures, proliferation and formation of new follicles were most pronounced on the 5th day. The increase in the number of C cells, their hypertrophy and proliferation permit attaining the high calcitonin level in the blood serum, reaching a maximum on the 15th experimental day.

Animals↗

[Is cryosurgery as alternative treatment procedure for recurrent hyperplasia of the endometrium in perimenopause to be considered?].

Complex investigations were performed for the evaluation of the local biological effect of the total cryodestruction of endometrium in 7 perimenopausal women with relapsing hyperplasia of the endometrium before and after (in 3-4.5 months) surgery. The following methods were used: radiometry of uterus, cytomorphologic and cytomorphometric investigations, RIA of E2 in peripheral blood plasma, in cytosol and in a nuclear fraction, and an assay of the state of E2-receptor endometrial system. The results of the investigations showed the importance of these methods as the objective criteria for the treatment efficiency. It was established that the cryosurgery is an alternative method for the treatment of this pathology in perimenopausal women.

Adult↗

Pharmacokinetics of 3H-pipethiaden after single oral and intravenous administration in rats.

Tritium labelled anti-migraine drug 4-(1-methyl-4-piperidyliden)-4,9-dihydrothieno[2,3-c]-2-b enzothiepine (pipethiaden) was prepared. After oral and intravenous administration to rats not only the courses of total radioactivity in plasma and various organs were determined, but by means of TLC-radiometry also the levels of pipethiaden itself. After the oral dose 1.35 mg/kg the plasma levels of pipethiaden did not exceed 3.5 ng/ml. Some pharmacokinetic parameters (e.g. t1/2 el-4 h) were calculated by compartmental analysis of plasma levels.

Administration, Oral↗

[Evaluation of Panergon therapy in Raynaud syndrome within the scope of progressive scleroderma].

In 15 patients with progressive systemic sclerosis with Raynaud's phenomenon Papaverin hydrochloride retard (Panergon) therapy was used. The average age of 14 females and 1 male was 42 years (26-55). Panergon therapy lasted for 4 weeks, the daily dose being 450 mg. For the evaluation of the treatment, 3 instrumental methods were used: IR radiometry for measuring thermal changes in the hands, capillaroscopy of nailfold, and Doppler-ultrasonic examination for measuring the circulation in finger arteries. An increased temperature, particularly in the fingertips, was found by radiometric examination in 6 patients. We also observed the acceleration of capillary flow speed in 7 patients. The pulse wave in finger arteries was markedly increased in 5 patients. From the subjective point of view the Panergon therapy was judged to be successful in 12 patients. It was not necessary to interrupt the treatment because of unfavourable effects in any case. Panergon therapy seems to be an important step in the treatment of Raynaud's phenomenon in progressive systemic sclerosis.

Adult↗

[Extracellular fluid and total potassium content in obesity patients].

The content of extracellular fluid and total potassium was studied by total-body radiometry with 82Br and according to 40K in 162 females aged 41 to 55 years suffering from obesity. It was established that in patients with obesity the volume of extracellular tissue, in per cent, and the amount of total potassium, in gramms and millieequivalent per unit of actual body mass, were reduced. An increase in the content of extracellular fluid and a decrease in the level of total potassium in obese patients with circulatory insufficiency may be revealed only when the real content of extracellular fluid and the total potassium are stimated in relation to the unit of body surface. In obese patients with no signs of circulatory insufficiency these relative values hardly differ from the control values.

Adult↗

Measurement of cell-mediated inflammation in experimental murine autoimmune encephalomyelitis by radioisotopic labeling.

A radioisotopic index test was used to detect that time of onset and intensity of cell-mediated immune inflammation of experimental autoimmune encephalomyelitis (EAE) in mice. Mice were tested at various time intervals after an encephalitogenic immunization with mouse spinal cord to homogenate for delayed-type hypersensitivity (DTH) to myelin basic protein (MBP) by intradermal challenge with antigen in the ear pinna. After 25 hr, the intensity of DTH was measured by 125I-radiometry which depends upon the migration of 125I-UdR radiolabeled mononuclear cells into the antigen depot. Cells reactive to MBP were detected by the ear assay as early as 7 days after the initial encephalitogenic sensitization. The degree of cell-mediated immune inflammation in the brain and spinal cord during the evolution of EAE was also measured by a radioisotopic technique; increased 125I-UdR uptake could be detected in the brain 3 to 4 days before the onset of signs of EAE at days 11 to 12, whereas 125I-UdR in the spinal cord was detected only 1 day before, or concomitant with, the onset of signs of EAE. Both, or concomitant with, the onset of signs of EAE. Both the "ear" and "organ" radiometric index tests are useful in measuring the degree of cell-mediated inflammation in EAE, and supplement routine histopathological and observational assessments.

Animals↗

[A method for determination of alkaline sucrose gradient sedimentation patterns of DNA for nondividing and slowly dividing cells].

A radiometric method for developing the alkaline sucrose gradient sedimentation patterns of DNA from non-labeled cells is described. The method is based on labeling of DNA in the gradient fractions by means of a labeled amino acid binding to DNA in the presence of formaldehyde. The procedure involves incubation of the fractions with a mixture of the labeled amino acid and formaldehyde, filtration of the incubation mixtures through nitrocellulose filters and radiometry of the filters. Relationship between the radioactivity on the filter and DNA concentration in the sample is linear. DNA detection sensitivity and specificity are satisfactory for the use under gradient ultracentrifugation condition. The non-labeled cells DNA sedimentation patterns developed by the method described and those of DNA from the same cells labeled with 3H-thimidine in vivo are found to be similar.

Amino Acids↗

[Absorption, distribution, excretion and metabolism of SC-11800EE, a combined steroid preparation of SC-11800 (ethynodiol diacetate) and ethinyl estradiol in rats and mice (author's transl)].

Absorption, distribution, excretion and metabolism of SC-11800EE, a combined steroid preparation consisting of SC-11800(ethynodiol diacetate)as gestagen and ethinyl estradiol (EE)as estrogen in 20:1 (w:w), were studied with the use of 14C-SC-11800 and 3H-EE by radiometry in female rats and by the whole body autoradiography in female normal and pregnant mice. The gestagen orally given with EE was rapidly absorbed from digestive tracts and distributed in tissues in various levels. Gestagen levels in liver and kidney exceeded that in plasma. About 75% of dosed radioactivity was excreted in feces largely via bile and more than 20% in urine within 72 hr after administration. The gestagen was metabolized extensively to more polar products and their conjugates. The pharmacokinetic behavior of the gestagen given with EE did not alter after repeated administrations for 7 days, but was slightly different from that without EE, possibly due to the estrogen effect. The pharmacokinetic behavior of the estrogen was independent from the gestagen given simultaneously. The distribution of the gestagen given with EE revealed by the whole body autoradiography in normal mice were essentially consistent with the radiometric results in rats and that in the pregnant mice showed that the gestagen in fetus was virtually nil under the present conditions.

Animals↗

[Radionuclide studies of reparative osteogenesis during modeling the shape of the leg].

The time course of metabolic processes in the osseous tissue and the capillary blood circulation in the forming osseous regenerate and the bone as a whole were studied in 16 patients using pyrophosphate and DTPA. The results of radiometry made it possible to give a quantitative evaluation of regeneration intensity: during intensive osteogenesis the accumulation of labeled pyrophosphate increased up to 720%, and the capillary blood circulation speeded up to 380%. Before the completion of osteogenesis the drug accumulation decreased considerably up to 250%.

Adult↗

[57Co-bleomycetin pharmacokinetics in the body of mice with LIO-1 lymphosarcoma].

Pharmacokinetics of 57Co-bleomycetin was studied on mice with lymphosarcoma LIO-1. It was found that at early periods of intravenous administration of the labeled antibiotic, i.e. within the period from 5 minutes to 1 hour its higher levels are detected in the liver, kidneys, blood serum, lungs, intestine and tumor. At later periods the drug levels in the organs and tissues gradually decrease and by the 72nd hour the concentration of 57Co-bleomycetin in the blood serum appears to be 30 times lower as that after 5 minutes. In the muscles and tumor its concentrations by that period are 15 and 2 times lower respectively. Radiometry of the animals showed that within the first 24 hours more than 85 per cent of 57Co-bleomycetin was excreted from the mice.

Animals↗

[Hypophyseal-adrenocortical system reaction to the prolonged action of low doses of selenomethionine-75Se that form during internal contamination].

A method of radiometry in vivo was applied to study the regularities attending distribution of the absorbed dose and its formation in the course of one year after the administration of 0.033 muCu/g of selenomethionine-75Se to rats, as well as the functional condition of the adaptive hypophysis-adrenal glands system by the determination of plasma corticosterone. A high tropicity of this preparation to the endocrine system organs was demonstrated. Intensification of the functional activity of the adaptive system was indicated by an increase of the blood plasma corticosterone concentration following the administration of a, radioactive preparation and its statistically significant increase (in comparison with control) 3, 6, and 10 months from the beginning of the experiment. The action of acute stress (histamine and formalin) 10 months after the administration of selenomethionine-75Se caused no sharp elevation of the plasma corticosterone concentration characteristic of control rats, this indicating an extreme strain of the hypophysis-adrenal gland system and its incapacity to respond to additional loads. It is supposed that analysis of functional condition of the adaptive system could serve as the key in the assessment of the biological effect of low radiation doses.

Acute Disease↗

[Laparoscopy in the diagnosis of ovarian tumors].

The potentialities of laparoscopy, associated with instrumental palpation, intraperitoneal radiometry, aimed puncture biopsy, were assessed in females with genital tumors. Moreover, peritoneal smears obtained by a special sound-brush were assayed histologically. This enabled not only establishing the correct diagnosis (in 96.3% of cases) and the recognition of the tumor microdissemination but also a selection of the optimum therapeutic policy. In 14 patients with the ascites syndrome a laparoscopically guided drainage and infusion therapy with hyperoxygenation were performed. The preliminary results indicate the necessity to further study and elaborate the technic concerned.

Aged↗