What is cyclosporine?

Cyclosporine is a prescription immunosuppressant that is used in combination with other medications indicated to treat several medical conditions.

The first indication of cyclosporine is to prevent your body from rejecting a transplanted organ (specifically kidney, liver, and heart transplants). The second indication is to fight rheumatoid arthritis in combination with methotrexate when methotrexate did not work alone. The third indication is to treat psoriasis (a skin disease in which scaly, red patches form on different areas of your skin) in patients who could not be treated by other (PUVA, retinoids, methotrexate) therapies.

Pediatric patients as young as 6 months have received cyclosporine to prevent solid organ transplant rejection. The dosage in children is the same as in adults, but they may need a higher mg/kg dose than adults.

How does cyclosporine work?

Cyclosporine is an immunosuppressant, which means it suppresses the immune system to stop the white blood cells from attacking the body. Specifically, cyclosporine works as a calcineurin inhibitor, that inhibits the CYP3A4 and P-glycoprotein enzymes. Cyclosporine reduces the number of autoimmune responses in your body by suppressing these enzymes.

What doses of cyclosporine are available?

Depending on which brand of drug you’re using, there are a few different dosage forms and strengths available to you.

A capsule is the most common form of cyclosporine. This comes in the following strengths:

25mg (Offered by: Gengraf, Neoral, Sandimmune)
50mg (Offered by: Gengraf, Sandimmune)
100mg (Offered by: Gengraf, Neoral, Sandimmune)

An oral solution is also common. This comes in the following strengths:

100mg/mL (Offered by: Gengraf, Neoral, Sandimmune)

An injectable solution only comes as:

50mg/mL (Offered by: Sandimmune)

Note: Gengraf, Neoral, Sandimmune, and other brands are not biosimilar and should not be used interchangeably.

How do you use cyclosporine?

Follow all directions given by your doctor and read all prescribing information and FDA-approved product labeling, and Medication Guide before using cyclosporine. Directions for use will change depending on which form of the medicine you are taking, your weight, lab tests, response to treatment, and the condition you are treating. Ensure that you continue to take cyclosporine even if you begin to feel better. This is especially true if you are using cyclosporine to treat the symptoms of psoriasis or rheumatoid arthritis.

You will typically take the oral solution or capsule by mouth once or twice daily, depending on the condition. You can take cyclosporine with or without food, but make sure to keep your regimen as consistent as possible. If you miss a dose of cyclosporine, take the missed dose as soon as you can. However, if it is close to the next dose, skip the missed dose and then begin your normal schedule again.

If you are taking the oral solution, choose a glass (not plastic) cup and fill it with a drink of choice, such as apple or orange juice, to take with your medicine. Fill the syringe by placing it into the medical solution and extract exactly how much your doctor prescribes. Dispense the liquid into your glass by pressing the plunger down. Stir the mixture well and drink all of your liquid in the glass right away. Ensure you get any remains of medicine by pouring a little more of the drink you have chosen into your glass, swirling it around the glass, and drinking the rest. Clean the syringe with a towel, do not rinse with water, and replace the protective covering for the next time you need it.

If you are taking cyclosporine as an injection, your healthcare professional will inject it four to 12 hours before your organ transplant, one to two weeks after your transplant, and as-prescribed the following weeks as your healthcare provider decides to avoid organ rejection.

Laboratory tests should be routine while you are taking cyclosporine. These would include renal and liver function tests measuring BUN, serum creatinine, serum bilirubin, and liver enzymes. Potassium, magnesium, serum lipids, and periodic cyclosporine blood level tests will most likely also be routine.

What are the side effects of cyclosporine?

The most common side effects of cyclosporine in clinical trials compared to placebo include:

Tremors or shaking
Acne
Increased or strange hair growth
Increased blood pressure
Nausea or upset stomach
Vomiting
Painful or swollen gums
- It is recommended to visit your dentist often to manage gum health.
Hypertension
Headache
Hot flush
Neurotoxicity

Rarely, cyclosporine may cause some serious side effects, including:

Kidney toxicity. Symptoms of worsening kidney function could include:
- Change in the amount of urine.
Liver toxicity. Symptoms of worsening liver function could include:
- Yellowing eyes or skin.
- Stomach or abdominal pain.
Mental/mood changes such as difficulty concentrating and confusion.
An increased risk of developing skin and malignancies in psoriasis patients treated with cyclosporine.
- Specifically, malignant lymphomas.
- An increase in the level of inflammatory cytokines and risk of infection is also possible.
Serious allergic reaction.
- Seek medical help immediately.

Contact your healthcare professional for medical advice about any possible adverse effects you experience while taking cyclosporine. You can report your adverse effects to the FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Cyclosporine drug interactions

When cyclosporine is taken with other prescription drugs, over-the-counter medications, vitamins, and supplements, it may change how they work or increase the frequency or severity of side effects. Some drug interactions with cyclosporine include:

Ambrisentan
Amphotericin B deoxycholate
Bosentan
Rifabutin
St. John’s wort
Antifungal
- Example: fluconazole
Antibiotics
- Example: erythromycin
Cholesterol-lowering medication
Steroid medication
Tacrolimus
Methylprednisolone (high doses of)
Calcium channel blockers
- Example: diltiazem‌

Note: grapefruit juice should also be avoided as it increases the concentration of cyclosporine in your blood.

Boxed warnings

Only physicians experienced in immunosuppressive management and therapy should prescribe cyclosporine. Maintenance therapy should be run by a physician with complete information about best follow-up practices.

Cyclosporine is an immunosuppressant, so it is intentionally lowering the activity of your immune system. This, therefore, increases your risk of developing malignancies (lymphomas) and infections. Make sure you tell your doctor if you are taking other immunosuppressants, as too much in your blood could lead to adverse effects. Some exceptions include:

Sandimmune (cyclosporine) can be administered with adrenal corticosteroids but not with other immunosuppressive agents.
Neoral and Gengraf can be administered with other immunosuppressive agents in kidney, liver, and heart transplant patients. This still increases your chance of infection and possible development of lymphoma.

Inform your doctor if you are taking any medications for psoriasis, either currently or in the past. Your risk for developing skin cancer is higher if taking cyclosporine with psoriasis treatment.

Cyclosporine can cause systemic hypertension and nephrotoxicity. Kidney function should be monitored throughout treatment, as renal dysfunction, including structural kidney damage, can occur.

Sandimmune, Neoral, and Gengraf are not biosimilar and cannot be used interchangeably.

Cyclosporine precautions

You should be sure that your healthcare provider is aware of all your medical conditions, including if you have:

An active infection. Tell your doctor if you show any signs of flu-like symptoms or an infection, including:
- Fever
- Chills
- Sore throat
- Coughing
- Trouble breathing
- Pain or tiredness that does not go away
Impaired renal function
History of kidney disease, kidney damage, or general kidney problems. These could get worse while taking cyclosporine. Ensure that you inform your doctor that you are taking any of the following medications:
- Amphotericin B (Amphotec, Fungizone)
- Cimetidine (Tagamet)
- Ciprofloxacin (Cipro)
- Ketoconazole (Nizoral)
- Nonsteroidal anti-inflammatory drugs, such as:
  - Diclofenac (Cataflam, Voltaren)
  - Naproxen (Aleve, Naprosyn)
  - Sulindac (Clinoril)
Asthma
History of blood dyscrasias
Recently or plan to have a vaccine
- Do not have a vaccine while taking cyclosporine or be near someone who has recently had a live vaccination.
Uncontrolled hypertension (high blood pressure)
In the case of psoriasis:
- Ongoing Concomitant PUVA therapy (treatment for psoriasis that combines a topical or oral medication with ultraviolet A light)
- Coal tar therapy
- Ultraviolet B (UVB) radiation
- Are currently taking methotrexate
- Are currently taking other immunosuppressant medications, including:
  - Imuran (azathioprine)
  - Cancer chemotherapy
  - Rheumatrex (methotrexate)
  - Rapamune (sirolimus)
  - Prograf (tacrolimus)
A pregnancy, plan to become pregnant or are breastfeeding.
- Cyclosporine has been found to pass into breast milk. Use caution and talk to your healthcare provider about what is best for you.

Is there a generic available for cyclosporine?

Yes, generics are available. Common brand-name drugs include Gengraf, Neoral, Restasis, and Sandimmune.

How do you store cyclosporine?

Store cyclosporine capsules at room temperature (77 °F [25 °C]). You can keep cyclosporine tightly closed in the container it came in. Keep it out of reach of children.

If taking the oral solution, make sure to store it in a clean, dry place. Keep it at room temperature. If the solution becomes gelled, allow it to warm to room temperature again to turn the solution back to a liquid.