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Title |
Cyclosporine | |
| Authors | Alkis Kostakis and George Vaiopoulos
General Laiko Hospital, Athens, Greece |
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| Citation | Kostakis, A. and Vaiopoulos, G.: Cyclosporine, Epitheorese Klin. Farmakol. Farmakokinet. 1(2): 105-112 (1987) | |
| Publication Date | 1987-10 | |
| Full Text Language | English | |
| Order – Buy | Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €)
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| Keywords | Cyclosporine, radioimmunoassay, RIA, high-performance liquid chromatography, HPLC, immunosuppressive agents. | |
| Other Terms | review article | |
| Summary | The discovery of cyclosporine, one of the most important immunosuppressive agents of the last decade, reduced dramatically graft loss caused by rejection in organ transplants. Cyclosporine was discovered in 1972 and is a lipid-soluble peptide composed of 11 amino acids with a molecular weight of 1200 d. Following per os administration, cyclosporine is absorbed from the GI tract and distributed mainly in the lipid tissue. Its distribution between plasma and red blood cells depends on temperature. It is metabolized in the liver and its major route of elimination is biliary excretion. A number of drugs have been reported to interact with cyclosporine, these interactions resulting in either an increase or decrease in blood cyclosporine concentrations. This must be taken into consideration when cyclosporine is administered to transplanted patients who are also on other medication. Drug level monitoring is recommended and carried out by two methods, by radioimmunoassay (RIA) which is most often used, and by high-performance liquid chromatography (HPLC). The recommended therapeutic range of cyclosporine concentration measured by RiA in whole blood is 300 to 800 ng/mi. The drug’s main action is a specific reduction of T helper lymphocytes activity with little effect on B lymphocytes activity. Much experimental research was been carried out in vitro and in vivo in several animal species to determine the drug’s exact mechanism and its effect on graft survival. Their results were that cyclosporine increased graft survival of heart, kidney, pancreas and liver transplantation in laboratory animals, in human cyclosporine is the most widely administered immunosuppressive drug in organ transplantation today and was greatly increased graft and patient survival rate. Its administration however, must be closely observed, because it also has some adverse reactions and toxic effects. | |
| References | 1. Borel, J.: Comparative study of in vitro and in vivo drug effects on cell-mediated cytotoxicity. Immunology 31: 631 (1976)
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Online ISSN 1011-6575
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