II. Indications
- See Ophthalmic Cyclosporine
- FDA Approved (adults)
- Solid Organ Transplant (Kidney, heart, liver, and Bone Marrow)
- Immunosuppression (maintenance prevention of rejection)
- Cyclosporine is typically combined with Corticosteroids when used for organ transplant
- Refractory Rheumatoid Arthritis
- May be used in combination with Methotrexate
- Refractory Plaque Psoriasis
- Solid Organ Transplant (Kidney, heart, liver, and Bone Marrow)
- Other Non-FDA approved Indications
- Graft versus host disesase
- Autoimmune Conditions (Behcet's Disease, Vasculitis, Myopathy)
- Psoriatuc Arthritis
- Thrombocytopenia (chronic, idiopathic, refractory)
- Solid Organ Transplant in children
III. Mechanism
- See Calcineurin Inhibitor
- Cyclosporine is a cyclic polypeptide isolated from the fungus Beauveria nivea
- Cyclosporine is a Calcineurin Inhibitor via binding cytophilin
IV. Medications
- Cyclosporine is available in both microemulsion (Neoral, Gengraf) and original formulation (Sandimmune)
- Original formulation has variable absorption due to dependence on GI bile acid concentrations
- Microemulsion has more consistent Bioavailability as it is not dependent on bile acids
- Monitor levels closely if switching between formulations
- Cyclosporine capsules: 25 mg, 100 mg
- Cyclosporine: 100 mg/ml
V. Dosing
- See other references for specific dosing regimens per indication
- Prescribers are typically specialists knowledgeable about the risks and monitoring of Cyclosporine
- Decrease dose in renal dysfunction, and adjust doses based on serum levels
VI. Adverse Effects
- See Calcineurin Inhibitor
- Nephrotoxicity
- Venous Thromboembolism
- Hepatotoxicity
- Hypertension
- Hyperlipidemia
- Gingival Hyperplasia
- Hirsutism
- Serious infections (Bacterial, viral, fungal)
- Gastrointestinal (less prominent than with Tacrolimus)
- Neurotoxicity
- Secondary Malignancy
- Squamous cell cancer
- Lymphoproliferative disorders
VII. Pharmacokinetics
- Hepatic metabolism (CYP3A4)
- No renal dose adjustments needed
VIII. Safety
- Pregnancy Category C
- Associated wirh preterm delivery and low birth weight
- Preeclampsia risk
- Avoid in Lactation per drug label
- However thought to be safe in Lactation based on registry data
- https://pubmed.ncbi.nlm.nih.gov/30000743/
- Monitoring
- Cyclosporine blood concentrations (frequent)
- Monitoring of renal and hepatic function
IX. Drug Interactions
- See Calcineurin Inhibitor
- Numerous Drug Interactions (see other references)
- Cyclosporine is CYP3A4 metabolized
-
Nephrotoxic Drugs (e.g. Aminoglycosides, Amphotericin B)
- Avoid in combination with Cyclosporine (combination increases nephrotoxicity)
X. Resources
Images: Related links to external sites (from Bing)
Related Studies
| 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 |