II. Indications

  1. See Ophthalmic Cyclosporine
  2. FDA Approved (adults)
    1. Solid Organ Transplant (Kidney, heart, liver, and Bone Marrow)
      1. Immunosuppression (maintenance prevention of rejection)
      2. Cyclosporine is typically combined with Corticosteroids when used for organ transplant
    2. Refractory Rheumatoid Arthritis
      1. May be used in combination with Methotrexate
    3. Refractory Plaque Psoriasis
  3. Other Non-FDA approved Indications
    1. Graft versus host disesase
    2. Autoimmune Conditions (Behcet's Disease, Vasculitis, Myopathy)
    3. Psoriatuc Arthritis
    4. Thrombocytopenia (chronic, idiopathic, refractory)
    5. Solid Organ Transplant in children

III. Mechanism

  1. See Calcineurin Inhibitor
  2. Cyclosporine is a cyclic polypeptide isolated from the fungus Beauveria nivea
  3. Cyclosporine is a Calcineurin Inhibitor via binding cytophilin

IV. Medications

  1. Cyclosporine is available in both microemulsion (Neoral, Gengraf) and original formulation (Sandimmune)
    1. Original formulation has variable absorption due to dependence on GI bile acid concentrations
    2. Microemulsion has more consistent Bioavailability as it is not dependent on bile acids
    3. Monitor levels closely if switching between formulations
  2. Cyclosporine capsules: 25 mg, 100 mg
  3. Cyclosporine: 100 mg/ml

V. Dosing

  1. See other references for specific dosing regimens per indication
  2. Prescribers are typically specialists knowledgeable about the risks and monitoring of Cyclosporine
  3. Decrease dose in renal dysfunction, and adjust doses based on serum levels

VI. Adverse Effects

  1. See Calcineurin Inhibitor
  2. Nephrotoxicity
  3. Venous Thromboembolism
  4. Hepatotoxicity
  5. Hypertension
  6. Hyperlipidemia
  7. Gingival Hyperplasia
  8. Hirsutism
  9. Serious infections (Bacterial, viral, fungal)
  10. Gastrointestinal (less prominent than with Tacrolimus)
    1. Nausea or Vomiting
    2. Diarrhea
    3. Abdominal Pain
    4. Anorexia
  11. Neurotoxicity
    1. Seizures
    2. Headaches
    3. Encephalopathy (rare)
  12. Secondary Malignancy
    1. Squamous cell cancer
    2. Lymphoproliferative disorders

VII. Pharmacokinetics

  1. Hepatic metabolism (CYP3A4)
  2. No renal dose adjustments needed

VIII. Safety

  1. Pregnancy Category C
    1. Associated wirh preterm delivery and low birth weight
    2. Preeclampsia risk
  2. Avoid in Lactation per drug label
    1. However thought to be safe in Lactation based on registry data
    2. https://pubmed.ncbi.nlm.nih.gov/30000743/
  3. Monitoring
    1. Cyclosporine blood concentrations (frequent)
    2. Monitoring of renal and hepatic function

IX. Drug Interactions

  1. See Calcineurin Inhibitor
  2. Numerous Drug Interactions (see other references)
    1. Cyclosporine is CYP3A4 metabolized
  3. Nephrotoxic Drugs (e.g. Aminoglycosides, Amphotericin B)
    1. Avoid in combination with Cyclosporine (combination increases nephrotoxicity)

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Related Studies

Cost: Medications

cyclosporine (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
CYCLOSPORINE 0.05% EYE EMULSION Generic $3.93 each
CYCLOSPORINE 100 MG CAPSULE Generic $6.70 each
CYCLOSPORINE 25 MG CAPSULE Generic $2.30 each
CYCLOSPORINE MODIFIED 100 MG Generic $1.44 each
CYCLOSPORINE MODIFIED 25 MG Generic $0.43 each
CYCLOSPORINE MODIFIED 50 MG Generic $1.16 each
neoral (on 7/27/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
NEORAL 25 MG GELATIN CAPSULE Generic $0.43 each

Ontology: Cyclosporine (C0010592)

Definition (CHV) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body
Definition (CHV) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body
Definition (CHV) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body
Definition (CHV) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body
Definition (CHV) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body
Definition (CHV) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body
Definition (NCI) A natural cyclic polypeptide immunosuppressant isolated from the fungus Beauveria nivea. The exact mechanism of action of cyclosporine is not known but may involve binding to the cellular protein cytophilin, resulting in inhibition of the enzyme calcineurin. This agent appears to specifically and reversibly inhibit immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited with T-helper cells as the primary target. Cyclosporine also inhibits lymphokine production and release. (NCI04)
Definition (NCI_NCI-GLOSS) A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body. It is also used in clinical trials to make cancer cells more sensitive to anticancer drugs.
Definition (MSH) A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).
Definition (CSP) 11-residue cyclic peptide produced by certain fungi which has antifungal and T cell specific immunosuppressive properties.
Definition (PDQ) A natural cyclic polypeptide immunosuppressant isolated from the fungus Beauveria nivea. The exact mechanism of action of cyclosporine is not known but may involve binding to the cellular protein cytophilin, resulting in inhibition of the enzyme calcineurin. This agent appears to specifically and reversibly inhibit immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited with T-helper cells as the primary target. Cyclosporine also inhibits lymphokine production and release. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39201&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39201&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C406" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D016572
SnomedCT 387467008, 255649004, 80906007
LNC LP16098-3, MTHU005140, LA16776-9
English Cyclosporin, Cyclosporin A, Cyclosporine, Cyclosporine A, Ciclosporin, cyclosporine, cyclosporine (medication), cyclosporin-A (medication), cyclosporin-A, Cyclosporin - chemical, CYCLOSPORINE, Cyclosporine [Chemical/Ingredient], cyclosporin a, cyclosporine a, ciclosporins, cycloSPORINE, ciclosporin, Cyclosporin - chemical (substance), Ciclosporin - chemical, CYA - Cyclosporin, Cyclosporin product, CSA - Cyclosporin A, CYA - Cyclosporin A, Cyclosporine (product), Cyclosporine (substance), cyclosporin, cyclosporin A, CYSP, Ciclosporin product, CsA, CycloSPORINE A, CycloSPORINE
Swedish Ciklosporin
Czech cyklosporin, Consupren, cyklosporin A
Finnish Siklosporiini
French Ciclosporine, Cyclosporine, Ciclosporine A, Cyclosporine A
Russian TSIKLOSPORIN A, TSIKLOSPORIN, ЦИКЛОСПОРИН A, ЦИКЛОСПОРИН
Japanese サイクロスポリン, シクロスポリンA, サイクロスポリンA, シクロスポリン, サンディミュン, ネオーラル, ネオメルク, アマドラ, シクポラール, パピロック
Croatian CIKLOSPORIN
Polish Cyklosporyna A
Spanish ciclosporina - sustancia química, ciclosporina - sustancia química (sustancia), ciclosporina (producto), ciclosporina (sustancia), ciclosporina A, ciclosporina, Ciclosporina, Ciclosporina A
German Cyclosporin A, Cyclosporin
Italian Ciclosporina
Portuguese Ciclosporina A, Ciclosporina