ABSTRACT
From readily available starting materials, the preparation and characterization of a variety of pyrimidine 2', 3'-dideoxyribo-, 2'-deoxyribo-, 3'-deoxyribo- and ribo- N-protected 4'-aza nucleosides is reported. None was found to possess any significant antiviral activity.
Subject(s)
Aza Compounds/chemical synthesis , Deoxyribonucleosides/chemical synthesis , Ribonucleosides/chemical synthesis , Aza Compounds/chemistry , Deoxyribonucleosides/chemistry , Molecular Structure , Pyrrolidonecarboxylic Acid/chemistry , Ribonucleosides/chemistryABSTRACT
A patient with severe type V hyperlipoproteinemia and chronic end-stage renal disease received a renal transplant and therapy with cyclosporine. Concentrations of the drug in plasma as determined by liquid chromatography appeared extraordinarily high for the dose ingested. When we measured the drug in the plasma, plasma cleared by ultracentrifugation, leukocytes, erythrocytes, and whole blood, we found that the high concentrations of cyclosporine were associated with the chylomicrons that always were present in this patient's blood. Cyclosporine added directly to this patient's plasma was less associated with the plasma lipids. Isolated lymphocytes and kidney slices incubated with plasma from this patient bound no more drug than when incubated with nonhyperlipemic plasma containing cyclosporine at a normal therapeutic concentration. We conclude that the cyclosporine associated with the chylomicrons in this patient was not biologically available to either lymphocytes or kidney tissue. We strongly recommend the use of chylomicron-cleared plasma for therapeutic drug monitoring of cyclosporine in type V hyperlipoproteinemic patients.
Subject(s)
Cyclosporins/blood , Hyperlipoproteinemias/blood , Kidney Transplantation , Adult , Biological Transport , Cyclosporins/metabolism , Erythrocytes/metabolism , Female , Humans , Kidney/metabolism , Leukocytes/metabolism , Lipoproteins/blood , Lymphocytes/metabolismSubject(s)
Nuclear Medicine/methods , Xenon Radioisotopes , Drug Packaging , Quality Control , SolutionsABSTRACT
PIP: A table of 76 selected species of plants which Indian medicine regards as having antifertility effects is presented. All the plants used for fertility control contain alkaloids, resins, tannins and bitter principles. The vulnerable points in the process of reproduction at which these plants act is not known.^ieng
