Pharmacokinetics of FK506 after intravenous and oral administration in patients awaiting renal transplantation

Journal of Clinical Pharmacology
S A GruberD M Canafax

Abstract

The authors examined the safety and pharmacokinetics of FK506, a new hepatically metabolized immunosuppressant, after single-dose intravenous (i.v.) infusion (20 micrograms.kg(-1) x 4 hours-1) and oral (80 micrograms/kg) administration in six nondialysis patients, aged 27 to 53 years, with chronic renal failure awaiting transplantation. A two-period, randomized, crossover study protocol was used with blood samples drawn for 72 hours after each dose and a washout period of 4 days. Whole-blood FK506 levels were determined using a standard, two-step, nonspecific enzyme immunoassay. There were no significant changes in vital signs, EKG, or complete laboratory test battery for any patient during the entire study period. No side effects were noted after i.v. or oral FK506 dosing. Mean +/- SD distribution half life was 0.9 +/- 0.2 hours, elimination half life (t1/2 beta) 33 +/- 8 hours, total body clearance (CL) 2.4 +/- 1.1 L/hour, and bioavailability 14 +/- 12%. There was no significant correlation between serum creatinine (Cr) and CL (r = 0.36) or between Cr and t1/2 beta (r = -0.30). It was found that FK506 is incompletely and erratically absorbed after oral administration and is rapidly distributed outside the blood compartment af...Continue Reading

References

Feb 23, 1991·Lancet·K F Sewing, U Christians
Oct 1, 1991·Current Opinion in Immunology·P J Morris
Feb 1, 1983·Computer Programs in Biomedicine·K K Chan, K Wnuck

❮ Previous
Next ❯

Citations

Aug 26, 2009·Rheumatology International·Soo-Kyung ChoSang-Cheol Bae
Feb 27, 2008·Modern Rheumatology·Yuko SugiokaTatsuya Koike
Jun 27, 2003·Transplantation Proceedings·N KaramperisK A Jørgensen
Jan 9, 1998·Transplantation·F S ShihabT F Andoh
Apr 12, 2007·British Journal of Clinical Pharmacology·Marie AntignacSaïk Urien
Dec 4, 2004·Clinical Chemistry and Laboratory Medicine : CCLM·Pierre E Wallemacq
Jan 1, 2010·International Journal of Nephrology and Renovascular Disease·P DalalLorenzo Gallon
Jul 26, 2005·Drugs & Aging·Christine E Staatz, Susan E Tett
May 23, 2001·Clinical Pharmacokinetics·P E Wallemacq, R K Verbeeck
Jul 13, 2004·Clinical Pharmacokinetics·Christine E Staatz, Susan E Tett
Jul 31, 2007·Journal of Clinical Pharmacology·Richard BorrowsDavid Taube
Jan 12, 2011·British Journal of Clinical Pharmacology·Katherine A BarracloughChristine E Staatz
Jul 1, 1997·Clinical Pharmacology and Therapeutics·L C FlorenM F Hebert
Jul 10, 2001·International Journal of Urology : Official Journal of the Japanese Urological Association·S SatohT Kato
May 17, 2008·CNS Neuroscience & Therapeutics·Germán Sierra-Paredes, Germán Sierra-Marcuño
Sep 22, 2005·Therapeutic Drug Monitoring·Eva M VasquezEnrico Benedetti
Dec 12, 2012·Expert Opinion on Pharmacotherapy·Thomas Rath

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.

Related Papers

Transplant International : Official Journal of the European Society for Organ Transplantation
M C MichelT Philipp
Liver Transplantation : Official Publication of the American Association for the Study of Liver Diseases and the International Liver Transplantation Society
C StaatzS Tett
© 2021 Meta ULC. All rights reserved