Cyclosporine

Editor: Abdelwahab Ward, PharmD.

This topic was published in Oct 02, 2021.

Pharmacology

Cyclosporine inhibits production and release of lymphokines, thereby suppressing cell-mediated immune response.

For adult: 2 mg/kg, to be given over 24 hours, dose adjusted according to blood-ciclosporin concentration and response.

For adult: Initially 1.5 mg/kg orally twice daily, increased if necessary up to 2.5 mg/kg twice daily after 6 weeks, dose increases should be made gradually, for maintenance treatment, titrate dose individually to the lowest effective dose according to tolerability, treatment may be required for up to 12 weeks.

Severe active rheumatoid arthritis [in combination with low-dose methotrexate, when methotrexate monotherapy has been ineffective] (administered on expert advice)

For Adult: Initially 1.25 mg/kg orally twice daily, increased if necessary up to 2.5 mg/kg twice daily after 6 weeks, dose increases should be made gradually, for maintenance treatment, titrate dose individually to the lowest effective dose according to tolerability, treatment may be required for up to 12 weeks.

Short-term treatment of severe atopic dermatitis where conventional therapy ineffective or inappropriate (administered on expert advice)

For adult: Initially 1.25 mg/kg orally twice daily (max. per dose 2.5 mg/kg twice daily) usual maximum duration of 8 weeks but may be used for longer under specialist supervision, if good initial response not achieved within 2 weeks, increase dose rapidly up to maximum.

Short-term treatment of very severe atopic dermatitis where conventional therapy ineffective or inappropriate (administered on expert advice)

For Adult: 2.5 mg/kg orally twice daily usual maximum duration of 8 weeks but may be used for longer under specialist supervision.

Severe psoriasis where conventional therapy ineffective or inappropriate (administered on expert advice)

For Adult: Initially 1.25 mg/kg orally twice daily (max. per dose 2.5 mg/kg twice daily), increased gradually to maximum if no improvement within 1 month, initial dose of 2.5 mg/kg twice daily justified if condition requires rapid improvement; discontinue if inadequate response after 3 months at the optimum dose; max. duration of treatment usually 1 year unless other treatments cannot be used.

Organ transplantation (used alone)
For adult: 10–15 mg/kg orally, to be administered 4–12 hours before transplantation, followed by 10–15 mg/kg daily for 1–2 weeks postoperatively, then maintenance 2–6 mg/kg daily, reduce dose gradually to maintenance. Dose should be adjusted according to blood-ciclosporin concentration and renal function; dose is lower if given concomitantly with other immunosuppressant therapy (e.g. corticosteroids); if necessary one-third corresponding oral dose can be given by intravenous infusion over 2–6 hours.
Bone-marrow transplantation

For adult: 3–5 mg/kg daily, to be administered over 2–6 hours from day before transplantation to 2 weeks postoperatively, alternatively (by mouth) initially 12.5–15 mg/kg daily, then (by mouth) 12.5 mg/kg daily for 3-6 months and then tailed off (may take up to a year after transplantation).

Nephrotic syndrome
For adult: 5 mg/kg daily in 2 divided doses, for maintenance reduce to lowest effective dose according to proteinuria and serum creatinine measurements; discontinue after 3 months if no improvement in glomerulonephritis or glomerulosclerosis (after 6 months in membranous glomerulonephritis).

Unlicensed use

With systemic use for use in severe acute ulcerative colitis refractory to corticosteroid treatment.

When used by eye: Active or suspected ocular or peri-ocular infection; Ocular or peri-ocular malignancies or premalignant conditions
With systemic use: Malignancy (in non-transplant indications); uncontrolled hypertension (in non-transplant indications); uncontrolled infections (in non-transplant indications)

Cautions

When used by eye: Glaucoma—limited information available; history of ocular herpes—no information available
With systemic use: Elderly—monitor renal function; hyperuricemia; in atopic dermatitis, active herpes simplex infections—allow infection to clear before starting (if they occur during treatment withdraw if severe); in atopic dermatitis, Staphylococcus aureus skin infections—not absolute contra-indication providing controlled (but avoid erythromycin unless no other alternative); in psoriasis treat, patients with malignant or pre-malignant conditions of skin only after appropriate treatment (and if no other option); in uveitis, Behcet's syndrome (monitor neurological status); lymphoproliferative disorders (discontinue treatment); malignancy

When used by eye (topical) ー Eye discomfort; eye disorders; vision blurred
With oral/parenteral use ー Appetite decreased, diarrhea, electrolyte imbalance, fatigue, gastrointestinal discomfort, hepatic disorders, hyperglycaemia, hyperlipidaemia, hypertension, hyperuricaemia, leucopenia, muscle complaints