Ciclosporin is an immunosuppressant drug that is used to treat inflammatory conditions.
What is ciclosporin?
It is used to treat skin diseases as well as conditions affecting other body organs. Ciclosporin is offered as a pill and an oral liquid. It’s also accessible without a prescription as eye drops and an injection.
Ciclosporin works by inhibiting calcineurin, a calcium-dependent serine-threonine protein phosphatase present in immune system T cells. T-cell activation and immune system function are reduced by calcineurin inhibitors.
Who uses ciclosporin?
In dermatology, ciclosporin can be used as a systemic agent for adults and children who have severe skin problems that aren’t responding to topical treatments alone.
Atopic eczema/dermatitis and psoriasis are two common skin disorders that ciclosporin is used to treat.
The following are some of the less prevalent skin disorders for which ciclosporin is sometimes used off-label:
- Pyoderma gangrenosum
- Dyshidrotic eczema
- Chronic urticaria
- Behçet disease
- Pityriasis rubra pilaris
- Pemphigus vulgaris
- Epidermolysis bullosa acquisita
- Lichen planus
- Hidradenitis suppurativa
- Prurigo nodularis
- Systemic sclerosis
Other systemic uses of ciclosporin include to:
- Prevent organ rejection after solid-organ transplantation (eg, kidney transplant, lung transplant, liver transplant, or heart transplant)
- To prevent or treat graft-versus-host disease (a possible complication of bone marrow transplantation)
- To treat nephrotic syndrome
- To treat severe rheumatoid arthritis
For keratoconjunctivitis and endogenous uveitis, topical ciclosporin eye drops can be administered. The amount of ciclosporin absorbed into the bloodstream when taken as an eye drop is usually unnoticeable.
Other off-label applications of ciclosporin exist, as well as occasions when ciclosporin has been shown to be beneficial for ailments for which it is not typically prescribed. Treatments for Stevens–Johnson syndrome and toxic epidermal necrolysis, as well as severe acute ulcerative colitis that hasn’t responded to conventional treatments, are examples.
What are the contraindications with ciclosporin
Ciclosporin should not be used by anyone with the following conditions:
- Current active cancer (except in some non-melanoma skin cancers)
- Uncontrolled hypertension
- Uncontrolled infection (eg, with chronic infections like hepatitis, tuberculosis, or human immunodeficiency virus [HIV]; or with acute infections like pneumonia or cellulitis)
- Had a previous allergic reaction to ciclosporin or ingredients in the ciclosporin preparations.
People who acquire these problems while using ciclosporin should have their ciclosporin withheld or stopped in most situations.
More about ciclosporin
Ciclosporin is a tiny lipophilic (fat-binding) protein that was originally produced from fungi and consists of a circular chain of 11 amino acids. Following oral administration, it is absorbed by the gut and metabolized by cytochrome P-450 3A enzymes in the liver. Ciclosporin is eliminated in the bile after that.
All systemic formulations of ciclosporin should be given twice a day (every 12 hours) at the same time every day at first. Adults and children have different metabolisms. Because ciclosporin is absorbed more slowly in children and eliminated more quickly, they may need to take it three times a day.
Cilosporin takes about 1–8 hours to reach peak blood concentrations when taken orally. It has a varied half-life when it comes to elimination.
Cyclosporin is now available in two forms: a modified version and the original, unaltered formulation.
- The unmodified formulation can be given orally or as an injection, but gut absorption is variable. The oral form requires bile to be absorbed.
- The modified version can only be given orally, but does not rely on bile for absorption and is better and more reliably absorbed from the gut. Its half-life is around 19 hours.
Ciclosporin does not have to be taken with food, however it should be taken around mealtime. To improve the taste, the liquid formulation can be blended with fruit juice (excluding grapefruit juice), however it should be administered immediately after mixing. Because ciprofloxacin solutions can stick to plastic, they should be administered in a non-plastic container.
The dosage of ciclosporin is usually 2–15 mg/kg per day in divided doses, depending on the patient’s body weight and the ailment being treated. Dose adjustments are performed based on the improvement of symptoms and the absence of side effects. Blood testing for ciclosporin concentrations in the blood can also be beneficial; these blood tests can be performed in two ways:
- 12 hours after the first dose, before the second dose (12-hour trough level)
- Two hours after the first dose (peak dose)
At the time of the next administration, the dose can be increased or lowered by 25–50 mg.
The dose of ciclosporin can be gradually reduced if disease remission has been reached, usually after 6–8 weeks of treatment. Ciclosporin can eventually be administered as maintenance therapy on an as-needed basis, such as twice weekly. This is frequently done over a longer period of time, up to a year.
What are the benefits of ciclosporin?
Ciclosporin is a versatile drug that can be used to treat a variety of ailments.
When taken under the supervision and supervision of a qualified health practitioner, cyclosporin is a safe medication. Cyclosporin is one of the only therapeutic options for some disorders, such as severe atopic dermatitis. Although novel drugs (biologic agents) for atopic eczema and psoriasis are constantly being developed, they have not yet been proved to be more effective than ciclosporin.
What are the disadvantages of ciclosporin?
Ciclosporin has the potential to interact with certain foods, such as grapefruit, as well as other drugs. Before starting any new drug, make sure to check for potential interactions. The following are some of the most prevalent drugs that interact with ciclosporin:
- Simvastatin and atorvastatin (suitable alternatives are fluvastatin, pravastatin and rosuvastatin)
- Non-steroidal anti-inflammatory drugs (NSAIDs), such as indomethacin and naproxen
- Antibiotics, such as sulfamethoxazole, trimethoprim, rifampicin, erythromycin, ciprofloxacin, tobramycin, and gentamicin
- Anticonvulsants, such as phenytoin and carbamazepine
- Antifungals, such as amphotericin B, ketoconazole, itraconazole, and fluconazole
- Anticoagulants, such as warfarin and dabigatran (interactions will increase the risk of bleeding)
- St John’s wort (Hypericum perforatum)
These medications should be avoided if at all possible, and if that isn’t possible, ciclosporin levels should be constantly watched. Regular general blood tests and doctor supervision are essential during ciclosporin medication due to the possibility of toxicity to the kidneys and other bodily organs.
Use in pregnant women
Ciclosporin is classified as a category B drug. There is little research on the use of ciclosporin during pregnancy and nursing, and the medication’s safety is unknown. Despite the fact that it has been used safely in the past and has been shown to be non-teratogenic (i.e., it does not cause birth defects), it should be avoided unless the benefits outweigh the risks. Concerns have been raised concerning the possibility of causing hypertension.
Use in older people
Only a few studies have been done on the use of ciclosporin for skin problems in the elderly. To avoid drug–drug interactions and the exacerbation of any comorbidities, such as impaired renal function, extreme caution is required.
Following the discontinuation of ciclosporin medication, there is a risk of recurrence or flare-up of diseases, such as a worsening of atopic eczema or psoriasis. This can be minimized by gradually lowering the dose.
What are the side effects and risks of ciclosporin?
Ciclosporin has a lot of potential side effects. With a longer treatment period, the chance of side effects increases. The following are examples of common side effects:
- Stomach or intestinal upset (eg, nausea, stomach pain, loss of appetite, vomiting, or diarrhoea)
- Headache and muscle aches
- Nephrotoxicity (damage to kidneys)
- Hepatotoxicity (damage to the liver)
- New or worsening hypertension
- Increased risk of infection (both acute and chronic)
- Paraesthesia (tingling), commonly affecting the hands, feet, or lips
Other important risks with ciclosporin include:
- A small increased risk of certain malignancies, especially cutaneous squamous cell carcinoma and lymphoproliferative disorders such as lymphoma
- A new onset of diabetes mellitus, or worsening of pre-existing diabetes
- New or worsening dyslipidaemia
- A flare of gout
- Electrolyte disturbances such as abnormally high potassium (hyperkalaemia) or a magnesium deficiency (hypomagnesaemia)
- Gingival hyperplasia
- Interactions with medications
Before starting ciclosporin medication, it’s critical to assess each person’s risk. Before commencing ciclosporin, a general physical checkup should be performed.
Kidney function, liver function, full blood count, fasting lipid profile, electrolytes, and chronic infection screening are all done with blood testing.
Routine vaccines, such as those for measles and varicella-zoster, may need to be examined and updated.
By changing their behaviors, patients can lower their risk of suffering side effects. Patients taking ciclosporin should do the following:
- Seek prior approval from their treating health professional before taking any new medications or over-the-counter supplements
- Avoid excessive sunlight exposure, sunbeds and phototherapy
- Avoid medications that can irritate the stomach
- Seek early treatment of any infection or fever
- Avoid excessive intake of alcohol
- Have regular dental check-ups.
For the first month of treatment, blood pressure should be tested once to twice weekly, then monthly for the next three months, and then less regularly after that.
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