Biopharmaceutical aspects of FK-506.

Transplantation proceedings ·Vol. 19 ·No. 5 Suppl 6 ·1987-10-00 ·Pages 30-5

Venkataramanan R, Warty VS, Zemaitis MA, Sanghvi AT, Burckart GJ, Seltman H, Todo S, Makowka L, Starzl TE

Abstract

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.

MeSH Terms

Administration, Oral Animals Chromatography, High Pressure Liquid Dogs Drug Evaluation, Preclinical Immunoenzyme Techniques Immunosuppressive Agents/administration & dosage,analysis,pharmacokinetics Inactivation, Metabolic/drug effects Injections, Intramuscular Male Microsomes, Liver/drug effects,enzymology Pyridines/administration & dosage,analysis,pharmacokinetics Rats Rats, Inbred Strains Tacrolimus

Chemicals

Immunosuppressive Agents Pyridines Tacrolimus

Authors & Affiliations

9 authors, click to expand affiliations / ORCID

Venkataramanan R

School of Pharmacy, University of Pittsburgh, PA.

Warty V S

Zemaitis M A

Sanghvi A T

Burckart G J

Seltman H

Todo S

Makowka L

Starzl T E

References (8)

8 references, click to expand

Determination of serum proteins by means of the biuret reaction.
J Biol Chem. 1949 Feb;177(2):751-66 PMID: 18110453
THE CARBON MONOXIDE-BINDING PIGMENT OF LIVER MICROSOMES. I. EVIDENCE FOR ITS HEMOPROTEIN NATURE.
J Biol Chem. 1964 Jul;239:2370-8 PMID: 14209971
Studies on the rate of reduction of hepatic microsomal cytochrome P-450 by reduced nicotinamide adenine dinucleotide phosphate: effect of drug substrates.
Mol Pharmacol. 1969 Mar;5(2):109-22 PMID: 4389181
Influence of prednisolone on antipyrine and chloramphenicol disposition in rabbits.
Pharmacology. 1984;29(2):117-20 PMID: 6473505
The effects of cyclosporin A (CsA) on hepatic microsomal drug metabolism in the rat.
Drug Metab Dispos. 1986 Jan-Feb;14(1):73-8 PMID: 2868869
Role of bile and bile salts on cyclosporine absorption in dogs.
Transplant Proc. 1987 Feb;19(1 Pt 2):1248-9 PMID: 3274312
Hepatic triphosphopyridine nucleotide-cytochrome c reductase: isolation, characterization, and kinetic studies.
J Biol Chem. 1962 Aug;237:2652-60 PMID: 14486217
The colorimetric estimation of formaldehyde by means of the Hantzsch reaction.
Biochem J. 1953 Oct;55(3):416-21 PMID: 13105648

Article Info

Journal

Transplantation proceedings

Abbr.

Transplant Proc

ISSN

0041-1345

Published

1987-10-00

Pages

30-5

Language

English

Region

United States

NLM ID

0243532

PMCID

PMC2953256

Subset

Grants

NIDDK NIH HHS · R01 DK029961-19 · United States

External Links

PubMed source PMC Full Text View journal details

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Biopharmaceutical aspects of FK-506.

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