Biopharmaceutical aspects of FK-506

FK is a potent immunosuppressive agent. FK can be analyzed in biologic fluids by EIA. The oral absorption of FK is rapid but variable in dogs. After intramuscular administration, FK is slowly and continuously absorbed. FK is primarily eliminated by metabolism. Less than 1% of the administered dose i...

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Published inTransplantation proceedings Vol. 19; no. 5 Suppl 6; p. 30
Main Authors Venkataramanan, R, Warty, V S, Zemaitis, M A, Sanghvi, A T, Burckart, G J, Seltman, H, Todo, S, Makowka, L, Starzl, T E
Format Journal Article
LanguageEnglish
Published United States 01.10.1987
Subjects
Administration, Oral
Animals
Chromatography, High Pressure Liquid
Dogs
Drug Evaluation, Preclinical
Immunoenzyme Techniques
Immunosuppressive Agents - administration & dosage
Immunosuppressive Agents - analysis
Immunosuppressive Agents - pharmacokinetics
Inactivation, Metabolic - drug effects
Injections, Intramuscular
Male
Microsomes, Liver - drug effects
Microsomes, Liver - enzymology
Pyridines - administration & dosage
Pyridines - analysis
Pyridines - pharmacokinetics
Rats
Rats, Inbred Strains
Tacrolimus
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Summary:FK is a potent immunosuppressive agent. FK can be analyzed in biologic fluids by EIA. The oral absorption of FK is rapid but variable in dogs. After intramuscular administration, FK is slowly and continuously absorbed. FK is primarily eliminated by metabolism. Less than 1% of the administered dose is excreted in the bile or the urine. After chronic intramuscular administration FK inhibits drug metabolism. Monitoring of FK levels in plasma is essential for the proper interpretation of efficacy and toxicity studies.
ISSN:0041-1345
1873-2623