Ciclosporin

Renal toxicity and hypertension are the most memorable side effects. It does not cause myelosuppression

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• 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

• Tacrolimus usage

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 Ciclosprin 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

References

• Summary Product Characteristics