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Related Experiment Videos

[Circulating forms of cyclosporin A].

J Barre1

  • 1Laboratoire Hospitalo-Universitaire de Pharmacologie, Centre Hospitalier Intercommunal, Créteil.

Therapie
|July 1, 1992
PubMed
Summary

Cyclosporin primarily binds to red blood cells, but this saturates at higher concentrations due to cyclophilin binding. This distribution impacts its pharmacological and toxicological effects.

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Toxicology

Context:

  • Cyclosporin is a widely used immunosuppressant drug.
  • Understanding cyclosporin's distribution in blood is crucial for optimizing its therapeutic use and managing side effects.

Purpose:

  • To elucidate the distribution of cyclosporin within various blood components.
  • To investigate the saturation phenomenon of cyclosporin binding to intracellular proteins.

Summary:

  • The majority of circulating cyclosporin, up to 58%, is found in red blood cells at lower concentrations (<1,000 ng/ml).
  • At higher concentrations, cyclosporin's red blood cell localization decreases due to saturation of binding to intracellular cyclophilin.
  • Other fractions distribute to lipoproteins (27.5%), albumin (5%), polymorphonuclears (4%), lymphocytes (5%), with only 0.5% free in plasma.

Impact:

  • Reveals key insights into cyclosporin pharmacokinetics and pharmacodynamics.
  • Highlights the significance of red blood cell and cyclophilin interactions in cyclosporin's behavior.
  • Provides a basis for understanding cyclosporin's varied pharmacological, pharmacokinetic, and toxicological outcomes.

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