Author: Hon A/Prof Amanda Oakley, Dermatologist, Hamilton, New Zealand, 1998. Updated by Anna Yu Luo, Medical Registrar, Department of General Medicine, Rotorua Hospital, Rotorua, NZ. DermNet NZ Editor in Chief: Adjunct A/Prof Amanda Oakley, Dermatologist, Hamilton, New Zealand. Copy edited by Gus Mitchell. November 2018.
Ciclosporin is an immunosuppressant medication that is used to treat a number of inflammatory illnesses. It is used for conditions that affect the skin and for conditions that affect other body organs. In New Zealand, ciclosporin is available and fully funded as a tablet and as an oral liquid. It is also available unfunded as eye drops and as an injection .
Ciclosporin works by selectively blocking calcineurin, a chemical found in the T-cells of the immune system. Calcineurin inhibits T-cell activation and reduces the activity of the immune system .
In dermatology, ciclosporin can be used as a systemic agent for adults and children with severe skin conditions that are not adequately treated with topical therapies alone.
Less common skin conditions for which ciclosporin is sometimes used off-licence include:
Other systemic uses of ciclosporin include:
Topical ciclosporin eye drops can be used for keratoconjunctivitis and endogenous uveitis . When used as an eye drop, there are usually undetectable levels absorbed into the bloodstream .
There are other off-label uses of ciclosporin, and cases where ciclosporin has been effective, even though it is not usually used for those conditions. Examples include the treatment of Steven-Johnson / toxic epidermal necrolysis, and treatment of severe acute ulcerative colitis that has not responded to other treatments [1,5].
People who should not use ciclosporin include those who have:
In most cases, people who develop these conditions while on ciclosporin should have the ciclosporin withheld or discontinued .
Ciclosporin is a small lipophilic (fat-binding) protein, made up of a circular chain of 11 amino acids. It is originally derived from fungi. It is absorbed by the intestine after oral administration, and is metabolised by cytochrome P-450 CYP3A enzymes in the liver. Ciclosporin is then excreted in the bile [2,6].
All systemic forms of ciclosporin should initially be administered twice a day (every 12 hours), at the same time each day. Its metabolism differs between adults and children. In children, ciclosporin is likely absorbed slower and cleared quicker, so children may need to take ciclosporin three times a day.
When given orally, ciclosporin takes approximately one to eight hours to reach peak blood concentrations. Its elimination half-life is variable.
There are now two forms of ciclosporin; a modified version and the original, unmodified formulation .
Ciclosporin does not have to be given with food, but should be given at the same time in relation to meals. The liquid formulation can be mixed with fruit juice (except grapefruit juice) to improve the taste, but should be given straight after mixing. Ciclosporin solutions can adhere to plastic, so should be given in a non-plastic container .
The administered dose of ciclosporin is based on body weight and the condition being treated, usually 2–15 mg/kg per day in divided doses. Adjustments to the dose are made based on improvement of symptoms and adverse effects. Blood tests for ciclosporin concentrations in the blood can also be helpful, and is done in one of two ways:
The dose can then be increased or decreased by 25–50 mg at the time of next administration [2,6].
After disease remission is achieved, usually after 6–8 weeks of treatment, the dose of ciclosporin can be slowly reduced. Ciclosporin can eventually be given intermittently, such as twice weekly, as maintenance therapy. This is often continued for a longer period of time, such as up to a year [7,8].
Ciclosporin is an effective medication that can be used for a wide range of conditions.
Ciclosporin is a safe medication when used under the guidance and monitoring of an experienced health professional. For some conditions, such as severe atopic dermatitis, ciclosporin is one of the few treatment options available. Although there are new medications (biologics) currently under development for atopic eczema and psoriasis, these have not yet been shown to be superior in effect to ciclosporin [7–10].
Ciclosporin can interact with some food, such as grapefruit, and other medications. It is important to check for interactions prior to starting any new medication. Some common medications that interact with ciclosporin include:
These medications should be avoided, or if not possible, ciclosporin levels should be monitored closely [1,2,6].
Ciclosporin is a category B medication. There are limited studies regarding the use of ciclosporin use in pregnancy and breastfeeding, and the safety of this medication is not well-established. Although it has previously been used safely and has demonstrated non-teratogenicity (ie, it does not cause birth defects), it should be avoided unless the benefits outweigh potential harm [1,2,8,9]. There are specific concerns about the risk of inducing hypertension.
There are limited studies on the use of ciclosporin for skin conditions in older people. Caution is needed to avoid drug-drug interactions and aggravation of any co-morbidities such as poor renal function [8,9].
There is a risk of recurrence or flare of disease, such as worsening of atopic eczema or psoriasis after ciclosporin treatment is discontinued. This is mitigated by reducing the dose slowly and gradually .
Ciclosporin has important potential risks. The risk of side effects increases with longer duration of treatment. Common side effects include:
Other important risks with ciclosporin include:
It is important to evaluate each person’s risk prior to beginning treatment with ciclosporin. A general physical examination should be done prior to starting ciclosporin.
Blood tests are undertaken for kidney function, liver function, full blood count, fasting lipid profile, electrolytes and screening for chronic infections.
Patients can reduce the risk of developing side effects by modifying their lifestyle.
It is recommended that blood pressure should be measured once to twice-weekly for the first month, then monthly thereafter .
Repeat blood tests can be done once monthly for the first 3 months, then less frequently thereafter.
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