Renal toxicity and hypertension are the most memorable side effects. It does not cause myelosuppression
- Oral calcineurin inhibitor with cyclical peptide composed of 11 aminoacids
and strongly hydrophobic.
- Derived from the fungus Tolypocladium inflatum Gams
Mode of action
- A Calcineurin inhibitor - Binds to and blocks calcineurin
- Reduces T cell proliferation and Reduced cytotoxic T cells
- Reduced IL-2 by blocking transcription prevents lymphocyte proliferation
- Little effect on acute inflammation and no bone marrow suppression
Indications
- Prevents organ rejection
- Prevent Graft versus Host Disease in Bone marrow transplant
- Autoimmune disorders e.g. myasthenia gravis
- Inflammatory bowel disease
- Low dose useful in Asthma or Psoriasis?
Contraindications
Side effects: BP, renal function, lipid profile should be monitored closely.
- Headaches, hirsutism, Nausea, Diarrhoea
- Nephrotoxicity, Hepatotoxicity, Hypertension
- Low calcium and magnesium
- Gum Hypertrophy/hyperplasia
- Malignancy e.g. lymphoproliferative disorder
- Opportunistic infection
- Haemolytic uraemic syndrome (rare)
Interactions
- Increased Nephrotoxicity with Gentamicin, Erythromycin and Trimethoprim, Diltiazem, Verapamil, NSAIDs and grapefruit juice
- Carbamazepine, Phenytoin, Rifampicin reduce Ciclosporin levels
Increase Ciclosporin levels
- Amiodarone, Fluconazole (> 200 mg/day)
- Anti-retroviral therapy
- Clarithromycin, Itraconazole
- Ketoconazole, Danazol, Diltiazem
- Nicardipine, Progestogens
- Erythromycin, Telaprevir/boceprevir
Reduce Ciclosporin levels
- Carbamazepine, Caspofungin
- Phenytoin, Primidone
- Griseofulvin, Rifampicin, Phenobarbitone
Cautions
- FBC, Uric acid, U&E, Lipids, Creatinine, Magnesium every 2 weeks for the first 3 months. Then monthly if stable. Monitor BP
- A low magnesium or cholesterol and IV Ciclosporin is associated with seizures
Dose
Indication | Dose | Freq | Route |
Autoimmune disease | 2-5 mg/kg per day | | PO |
References