Cyclosporine

Medically Reviewed by: Dr. Dipak Ladda, M.D.

Expertise: Consultant Pathologist

Last Updated: July 30, 2026

Medical Analysis

Comprehensive Medical Analysis of Cyclosporine Blood Test Insights and Clinical Guide

Introduction and Pharmacological Action of Cyclosporine

Cyclosporine is isolated from the fungus Beauveria nivea & Tolypocladium inflatum. Cyclosporine is an immunosuppressive agent used to treat organ rejection post-transplant [10]. It is equally useful in treating certain other autoimmune diseases, rheumatoid arthritis when the condition has not adequately responded to methotrexate, etc [4]. Cyclosporine is a calcineurin inhibitor. It has got immunomodulatory properties which prevent organ transplant rejection and also seems to be useful in certain inflammatory and autoimmune conditions [7].

How Cyclosporine Acts?

By binding with cyclophilin; cyclosporine forms a complex; which in turn inhibits calcineurin [6]. It causes reduced dephosphorylation of NFAT (Nuclear factor of activated T cells) and reduced synthesis of IL2 (Interleukin 2). It inhibits the production of cytokines involved in the regulation of T-cell activation.

Bioavailability

It is a lipophilic molecule, with its bioavailability dependent on food, bile and other interacting factors [1]. The bioavailability of cyclosporine is variable, ranging from less than 10% to 89% in various populations. As a result of its lipophilicity, cyclosporine is largely distributed outside of the blood volume once it is absorbed [1].

Contraindications, Indications, and Clinical History Assessment

Contraindications of Cyclosporine

Hypersensitivity to cyclosporine. Abnormal renal function [10]. Uncontrolled hypertension. Uncontrolled infections. Malignancy.

Indications

Patients put on Cyclosporine drugs itself is an indication. It is to monitor doses in sequence [12].

Clinical History with Sample Provided

Relevant clinical history. History of Transplant in detail. History of associated drugs [14]. Duration and dosage of cyclosporine.

Detection Methods, Sample Collection, and Laboratory Processing

Methods of detection

Enzyme Linked Immunosorbent Assay (ELISA) – Commonly used [11]. Chemiluminescent Microparticel Immunoassay. High Performance Liquid Chromatography (HPLC) – Tandem Mass spectrometry.

Blood Sample Collection Instructions

Collection Instructions: Very important and one should must remember to collect specimen immediately before a scheduled dose [12]. Send whole blood specimen as collected in toto in original tube to lab. Therapeutic range applies to trough specimens collected immediately prior to a.m. dose. (Trough: It refers to the lowest concentration of drugs in blood [12]. It is highly important as for drugs with a narrow therapeutic window, where to maintain a specific concentration is crucial for effectiveness and safety).

How to collect sample

Collect 3.0 ml blood in EDTA tube (Lavender capped) or Pink tube (K2EDTA) and send entire sample of whole blood to lab.

Storage and Transport of Samples

Storage Temperature: 2-8 degree C. Sample Containers: EDTA or K2 EDTA. Protection from light: Use opaque containers or wrap samples in aluminum foil to shield from light. Transport: During transport sample must be refrigerated using insulated packaging with ice packs. Don’t freeze the samples; otherwise there will be degradation. Timely Analysis: To avoid potential degradation immediate testing is always recommended.

Therapeutic Reference Range and Clinical Values

Therapeutic Reference Range (100-400 ng/ml) [5]

Post-Transplant Period – MonthsTherapeutic Range (Cyclosporine)
Kidney transplant (in combination with Everolimus)

1: 100-200 ng/mL


2-3: 75-150 ng/mL


4-5: 50-100 ng/mL


6-12: 25-50 ng/mL

Heart transplant

Up to 3: 350-525 ng/mL


4 or > 4: 145-350 ng/mL

Liver transplant–: 290-525 ng/mL
Toxic value> 700 ng/mL
Bone Marrow200-300 ng/ml

Adverse Effects and Therapeutic Applications of Cyclosporine

Adverse Effects of Cyclosporine

SystemAdverse Effects
RenalNephrotoxicity (most common) [10, 15]
CardiovascularHypertension
HepaticHepatotoxicity
NeurologicalTremor, paresthesia
DermatologicHirsutism, gingival hyperplasia
MetabolicHyperlipidemia, hyperuricemia
OthersInfection risk, malignancy risk

Therapeutic Applications

Therapeutic ApplicationDescription
Organ TransplantationPrevention/treatment of rejection in kidney, liver, heart, and bone marrow transplants [7]
Autoimmune DiseasesRheumatoid arthritis, psoriasis, atopic dermatitis, uveitis, Crohn’s disease [4]
Nephrotic SyndromeSteroid-resistant focal segmental glomerulosclerosis treatment [9]
Graft-versus-Host Disease (GVHD)Prevention and treatment
Ophthalmic ApplicationsKeratoconjunctivitis sicca, vernal keratoconjunctivitis
Other UsesAutoimmune hepatitis, Duchenne muscular dystrophy, pure red cell aplasia, Henoch-Schönlein purpura nephritis

Clinical Applications

Clinical ApplicationDescription
Organ TransplantationPrevents/treats rejection in kidney, liver, heart, bone marrow transplants [7]
Autoimmune DiseasesRheumatoid arthritis, psoriasis, atopic dermatitis, uveitis, Crohn’s disease [4]
Nephrotic SyndromeSteroid-resistant focal segmental glomerulosclerosis [9]
Graft-versus-Host DiseasePrevention and treatment
OphthalmicDry eyes (keratoconjunctivitis sicca), vernal keratoconjunctivitis
Off-label UsesAutoimmune hepatitis, muscular dystrophy, ulcerative colitis, others

Conclusion and Professional Acknowledgments

Thank You

Trusted Insights. Curated by Dr. Dipak Ladda.

For Non-Medicos

Understanding Your Cyclosporine Blood Test and Medication Guide

What is Cyclosporine and How Does It Work?

Cyclosporine is a specialized medication originally derived from a fungus that acts as an immune system suppressant [10]. It is primarily prescribed to prevent the body from rejecting transplanted organs such as kidneys, hearts, and livers [7]. Additionally, it helps manage severe autoimmune conditions like rheumatoid arthritis when standard treatments fall short [4]. It works by targeting specific immune cells to block the chemical signals that trigger inflammation and organ rejection [6]. Because every person’s body absorbs it differently, doctors closely monitor its presence in your blood to ensure it remains safe and effective [12].

Important Safety Rules and Blood Test Preparation

Before starting cyclosporine, doctors carefully check for conditions like high blood pressure, active infections, or kidney issues, as the drug can worsen these problems [10]. When your doctor orders a cyclosporine blood test, timing is everything. You must have your blood drawn immediately before taking your scheduled dose, which captures the lowest amount of the drug in your system [12]. A healthcare worker will collect a small blood sample in a special tube, keep it protected from light, and send it cold to the laboratory so the results stay accurate.

What Your Test Results and Potential Side Effects Mean

The laboratory analyzes your blood to make sure the drug levels fall within a safe therapeutic window—too little means your organ or condition is unprotected, while too much can cause toxicity [12]. Common side effects tracked during treatment include kidney strain, high blood pressure, hand tremors, and changes in hair growth or gum health [10, 15]. Regular testing helps your medical team adjust your dosage precisely, keeping you protected while minimizing unwanted health complications [12].

References:

  1. Ptachcinski, R. J., Venkataramanan, R., & Burckart, G. J. (1986). Clinical pharmacokinetics of cyclosporin. Clinical Pharmacokinetics, 11(2), 107–132. https://doi.org/10.2165/00003088-198611020-00002 Cited by: 563

  2. Yilmaz, D. E., Kirschner, K., Demirci, H., Himmerkus, N., Bachmann, S., & Mutig, K. (2022). Immunosuppressive calcineurin inhibitor cyclosporine A induces proapoptotic endoplasmic reticulum stress in renal tubular cells. Journal of Biological Chemistry, 298, 101589. https://doi.org/10.1016/j.jbc.2022.101589 Cited by: 51

  3. Barbarino, J. M., Staatz, C. E., Venkataramanan, R., Klein, T. E., & Altman, R. B. (2013). PharmGKB summary: cyclosporine and tacrolimus pathways. Pharmacogenetics and Genomics, 23(10), 563–585. https://doi.org/10.1097/fpc.0b013e328364db84 Cited by: 360

  4. Kahan, B. D. (1989). Cyclosporine. New England Journal of Medicine, 321(25), 1725–1738. https://doi.org/10.1056/NEJM198912213212507

  5. Staatz, C. E., & Tett, S. E. (2004). Clinical pharmacokinetics and pharmacodynamics of cyclosporin in organ transplantation. Clinical Pharmacokinetics, 43(10), 623–664. https://doi.org/10.2165/00003088-200443100-00003

  6. Liu, J., Farmer, J. D., Lane, W. S., Friedman, J., Weissman, I., & Schreiber, S. L. (1991). Calcineurin is a common target of cyclophilin-cyclosporin and FKBP-FK506 complexes. Cell, 66(4), 807–815. https://doi.org/10.1016/0092-8674(91)90124-H

  7. Florman, S., & Miller, J. (2000). Immunosuppression: historical perspective and current clinical status. The Mount Sinai Journal of Medicine, New York, 67(4), 294–305.

  8. Olyaei, A. J., & de Mattos, A. M. (2001). Cyclosporine versus tacrolimus: a medicinal comparison. Clinical Transplantation, 15(Suppl 6), 49–53. https://doi.org/10.1034/j.1399-0012.2001.00009.x

  9. National Kidney Foundation. (2000). K/DOQI clinical practice guidelines for chronic kidney disease: evaluation, classification, and stratification. American Journal of Kidney Diseases, 39(2 Suppl 1), S1–S266.

  10. Bennett, W. M., & Norman, D. J. (1986). Action and toxicity of cyclosporine. Annual Review of Medicine, 37(1), 215–224. https://doi.org/10.1146/annurev.me.37.020186.001243

  11. Shaw, L. M., Yatscoff, R. W., Bowers, L., & Emanuel, S. (1990). Cyclosporine measurement: analytical and clinical performance of current methods. Clinical Chemistry, 36(9), 1841–1846.

  12. Johnston, A., & Holt, D. W. (1999). Immunosuppressive drug monitoring: the role of therapeutic drug monitoring in transplant practice. Therapeutic Drug Monitoring, 21(3), 277–280. https://doi.org/10.1097/00007691-199906000-00001

  13. Sennesael, J. J., Verbeelen, D. L., & Jonckheer, M. H. (1990). Renal hemodynamic effects of cyclosporine in man. Transplantation, 49(3), 517–520. https://doi.org/10.1097/00007890-199003000-00010

  14. Yee, G. C., & McGuire, T. R. (1990). Pharmacokinetic drug interactions with cyclosporine. Clinical Pharmacokinetics, 19(5), 400–415. https://doi.org/10.2165/00003088-199019050-00004

  15. Andreani, M., Nesci, S., & Alfieri, R. (2005). Mechanisms of cyclosporine-induced nephrotoxicity. Journal of Nephrology, 18(5), 517–523.

FAQ’s:

  • What is cyclosporine?
    An immunosuppressive agent derived from fungi to treat organ rejection and autoimmune conditions.

  • How does cyclosporine act?
    It binds cyclophilin to inhibit calcineurin, reducing NFAT dephosphorylation and IL-2 synthesis.

  • What is its bioavailability?
    A lipophilic molecule with variable bioavailability ranging from under 10% to 89% across populations.

  • What are the contraindications?
    Hypersensitivity, abnormal renal function, uncontrolled hypertension, infections, and active malignancy.

  • Why monitor blood levels?
    To monitor sequential dosing and maintain concentrations within a narrow therapeutic window.

  • What sample is needed?
    3.0 ml of whole blood collected in an EDTA or K2EDTA tube.

  • How should samples be stored?
    Refrigerated at 2 to 8 degrees Celsius in opaque or foil-wrapped containers without freezing.

  • What is the toxic value?
    Blood concentrations exceeding 700 ng/mL are considered toxic.

  • What is the common side effect?
    Nephrotoxicity is the most frequently reported adverse effect.

What are its therapeutic uses?
Preventing transplant rejection, treating autoimmune diseases, nephrotic syndrome, and graft-versus-host disease.

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