[The effect of applied cytotoxic drugs on biological behaviour of 99mTc-radiopharmaceuticals].

INTRODUCTION: This study was aimed at investigating the influence of certain cytotoxic drugs on the organ uptake of the following 9mTc-radiopharmaceuticals: 99mTc-2,3-dicarboxypropane-1, 1-diphosphonic acid, 99mTc-meso-2,3-dimercaptosuccinic acid, 9mTc-tin colloid and 99mTc-macraggregated albumin. Methotrexate sodium and cyclophosphamide were used as models to evaluate these effects. MATERIAL AND METHODS: Two groups of healthy male Wistar rats were treated separately by oral application of the drugs for 7 days. On the eighth day, each of the 99Tc-radiopharmaceuticals was applied in a separate group of treated animals. They were sacrificed at different time intervals and the radioactivity in the organs of interest was measured. The organ uptake of the 99mTc-radiopharmaceuticals in an additional control group of animals was also studied. RESULTS: The results obtained showed an alteration in the organ uptake of 99mTc-radiopharmaceuticals in animals treated with cytotoxic drugs. In the rats treated with methotrexate sodium, there was a higher uptake of 99mTc-meso-2,3-dimercaptosuccinic acid in the bones, stomach and intestine, a higher uptake of 99mTc-2,3-dicarboxypropane-1-,1-diphosphronic acid in the bones, intestine, blood and muscle, a lower uptake of 99mTc-tin colloid in the liver and a lower accumulation of 99mTc-macroaggregated albumin in the lungs. Cyclophosphamide-treated animals showed enhanced uptake of 99mTc-meso-2,3-dimercaptosuccinic acid in the kidneys, a twofold enhanced uptake of 99mTc-2,3-dicarboxypropane-1,1-diphosphronic acid in all organs except the stomach, a decreased uptake of 99mTc-tin colloid in the lungs, spleen and kidneys and a significantly decreased uptake of 99mTc-macroaggregated albumin in the lungs. CONCLUSION: These results confirm that both methotrexate sodium and cyclophosphamide may alter the organ uptake of 99mTc-radiopharmaceuticals in experimental animals.

[Technetium-99m radiopharmaceuticals for in vivo diagnostics].

INTRODUCTION: Technetium-99m is an ideal radionuclide with optimum decay characteristics. It can be obtained in sterile, pyrogen-free and carrier-free condition, as sodium pertechnetate (Na99mTcO4), from 99Mo/99mTc generator. Because of its six-hour physical half-life and monochromatic 140 keV photons free of -radiation, administration of small amounts of 99mTc solution is possible, without a significant radiation damage to the patient. Technetium eluted from the 99Mo/99mTc generator is in the highest oxidation form (+ 7). It can be used for diagnostic purposes alone, but it is often used for labeling different organic and inorganic compounds. As it is unreactive, reduction with a chemical reductant, (+1), (+3) and (+5) oxidation are necessary before use. Nowadays almost 80% of radiopharmaceuticals are based on 99mTc. RADIOPHARMACEUTICALS: Radiopharmaceuticals are radionuclides or radioactive compounds used in diagnosis and therapy of human diseases. A pharmaceutical is chosen based on its localization in the organ, or its participation in its physiological function. Radiation emitted from a radionuclide is detected by a radiation detector. The ability to incorporate available radionuclides into tracer molecules has been the main goal in developing radiopharmaceuticals. As radionuclides with nuclear characteristcs used as either diagnostic or therapeutic radiopharmaceuticals, are predominantly metals, they can be designed as metal essential, whereby biological distribution is determined by coordination compound, or metal tagged, in which case the properties of the carrier molecule (ligand system) determine the biological distribution. This paper reviews the development of 99mTc-radiopharmaceuticals.