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Ciclosporin

Ciclosporin is a calcineurin-inhibitor immunosuppressant; the SmPC describes it as a cyclic polypeptide consisting of 11 amino acids, also known as ciclosporin A. As Neoral, it is indicated for the prophylaxis of organ rejection in kidney, liver and heart allogeneic transplants. It is also indicated for severe active rheumatoid arthritis that has not adequately responded to methotrexate, and for adults with severe, recalcitrant plaque psoriasis who have failed at least one systemic therapy or cannot tolerate other systemic options.

Neoral

Rheumatoid Arthritis, Severe Plaque Psoriasis

25mg · 100mg

Utilised to manage severe autoimmune skin lesions to alleviate scaling and support normal epidermal development.

From$4.16/ capsuleView

Opticare Ointment

Keratoconjunctivitis Sicca, Dry Eye Disease

2mg

Indicated to address tear production deficits to manage dry eye disease and alleviate local corneal discomfort.

From$15.60/ tubeView

Ciclosporin Capsules

Rheumatoid Arthritis, Psoriasis

50mg · 100mg

Intended to relieve autoimmune cell proliferation to support chronic organ viability and target inflammatory responses.

From$4.10/ capsuleView

Key points

  • Ciclosporin blood levels fall in two phases, with a terminal half-life of about 8.4 hours (range 5 to 18 hours).
  • Ciclosporin is broken down mainly by the cytochrome P-450 3A system, particularly CYP3A4, and is also a substrate of the P-glycoprotein efflux transporter.
  • Regular monitoring of serum creatinine is required during treatment.

How it works

The SmPC describes ciclosporin as a potent immunosuppressive agent that, in animals, prolongs survival of allogeneic transplants of skin, heart, kidney, pancreas, bone marrow, small intestine or lung. Studies suggest it inhibits the development of cell-mediated immune reactions, including allograft immunity, delayed cutaneous hypersensitivity and graft-versus-host disease (GVHD), as well as T-cell dependent antibody production. At the cellular level it inhibits production and release of lymphokines including interleukin 2 (T-cell growth factor, TCGF). Ciclosporin appears to block resting lymphocytes in the G0 or G1 phase of the cell cycle and inhibits the antigen-triggered release of lymphokines by activated T-cells.

Safety specific to Ciclosporin

Ciclosporin carries a boxed warning. Psoriasis patients previously treated with PUVA, and to a lesser extent methotrexate or other immunosuppressive agents, UVB, coal tar, or radiation therapy, are at an increased risk of developing skin malignancies when taking Neoral. Ciclosporin, in recommended dosages, can cause systemic hypertension and nephrotoxicity; the risk increases with increasing dose and duration of therapy. Renal dysfunction, including structural kidney damage, is a potential consequence, and renal function must therefore be monitored during treatment.

Ciclosporin, the active ingredient of Neoral, can also cause hepatotoxicity. Like other immunosuppressants, ciclosporin increases susceptibility to a variety of bacterial, fungal, parasitic and viral infections, often involving opportunistic pathogens. In view of the potential risk of skin malignancy, patients on Neoral, particularly those treated for psoriasis or atopic dermatitis, should avoid excess unprotected sun exposure and should not receive concomitant ultraviolet B therapy.

When to seek urgent care

Seek urgent medical attention for signs of liver injury. Cases of hepatotoxicity and liver injury, including cholestasis, jaundice, hepatitis and liver failure, have been reported, with serious and/or fatal outcomes. A rarer effect is optic disc oedema, including papilloedema, with possible visual impairment, secondary to benign intracranial hypertension; new visual disturbance during treatment also warrants prompt review.

Further reading

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