Key highlights for cyclosporine

Non-modified cyclosporine (Sandimmune) is only approved to prevent organ rejection after an organ transplant.
Cyclosporine is available in the original or “non-modified” formulation (Sandimmune) and modified formulation (Neoral, Gengraf) — these formulations are not interchangeable, and you should take cyclosporine exactly as prescribed to ensure efficacy while minimizing side effects.
You should take cyclosporine at about the same time every day.
If you are using the cyclosporine oral solution, you should always use the dosing syringe provided with the original package. Remember never to use household spoons to avoid inaccurate dosing.

Cyclosporine is a generic medication. Brand name versions are available, called Neoral, Gengraf, and Sandimmune. Neoral and Gengraf (cyclosporine modified) aren’t to be used interchangeably with Sandimmune (cyclosporine non-modified).

In addition to cyclosporine oral capsules, doctors can prescribe cyclosporine oral solution (100 mg/mL) for children and adults who have trouble swallowing pills.

Cyclosporine capsules are available as 25 mg, 50 mg, and 100 mg. Besides oral capsule and oral solution, cyclosporine is available as eye drops and injectable solution. Talk to your healthcare provider to make sure you are taking the correct medication form and dosage.

What’s it used for?

Cyclosporine is used to treat autoimmune diseases such as rheumatoid arthritis (RA) and psoriasis. Doctors also use cyclosporine to prevent transplant rejection in patients post-organ transplant.

How cyclosporine works

Cyclosporine is classified as an immunosuppressant, meaning it works to suppress the immune system, limiting the body’s ability to fight off a potential threat.

Prevent organ rejection

Cyclosporine is used to prevent organ rejection of kidney, liver, and heart transplants. After receiving an organ transplant, your immune system recognizes the transplanted organ as a foreign object. Therefore, the immune system launches an attack to reject the new organ.

By suppressing the immune system, cyclosporine is used to help prevent rejection in transplant patients. More specifically, cyclosporine fights against T suppressor cells and T helper cells to stop their attack against the newly transplanted organ. These T-cells are a type of white blood cells that are part of the natural immune system to fight infections and get rid of foreign objects such as transplanted organs.

Treat autoimmune diseases

Cyclosporine is also used to treat rheumatoid arthritis (RA) and psoriasis caused by an overactive immune system. When someone has an autoimmune disease, it means their immune system mistakes healthy tissues and organs as invaders. So instead of performing its duty to fight infections from viruses and bacteria, the body’s immune system attacks itself.

The drug information contained herein of cyclosporine is for educational purposes only and may not include all possible indications, adverse effects, drug interaction, and potential warnings.

Instructions for taking cyclosporine

Your doctor will decide the cyclosporine dosing regimen for you depending on the condition being treated, the severity, other medical conditions, and your age.

The goal is to start you on a lower dose to see its effectiveness and how your body tolerates it, as well as to limit side effects. Take cyclosporine exactly as prescribed, and tell your doctor about any persistent or severe side effects. Do not skip a dose or try to adjust the dosage yourself without talking to your doctor. Not taking this medication as prescribed can cause the worsening of the treated condition or the rejection of the transplanted organ.

Typical dosage to prevent transplant rejection (heart, kidney, and liver transplants)

Adults dosage (18 years and older)

Cyclosporine (modified) such as Gengraf, Neoral, and generic equivalents:
- Dosage is based on the type of transplanted organ, your body weight, and your concurrent medications.
- Below are the usual starting dose for different types of organ transplant:
  - Heart transplant: The usual starting dose is typically 4 mg/kg to 10 mg/kg, divided into two equal doses taken by mouth twice daily.
  - Liver transplant: The usual starting dose is typically 4 mg/kg to 12 mg/kg, divided into two equal doses taken by mouth twice daily.
  - Kidney transplant: The usual starting dose is typically 6 mg/kg to 12 mg/kg, divided into two equal doses taken by mouth twice daily.
Cyclosporine (non-modified) such as Sandimmune and generic equivalents:
- The first dose is typically 15 mg/kg and should be taken 4 to 12 hours before transplant and is continued for 1 to 2 weeks after the transplant surgery. After that, the maintenance dose is typically 5 to 10 mg/kg per day.

Children dosage (between 1 and 17 years)

Dosage for children is the same as for adults. Similarly to adults, cyclosporine dosage for your child also depends on the body weight, the type of organ transplant, and concurrent medications.

Kidney disease patients: Cyclosporine can affect kidney function. Your doctor may reduce the dosage of cyclosporine to prevent further kidney damage if you already have impaired kidney function.
Liver disease patients: Cyclosporine can cause liver disease; your doctor may reduce the dosage of cyclosporine if you already have liver disease.

Useful tips on taking cyclosporine

Drinking grapefruit juice can. You should avoid grapefruit juice and other grapefruit products as they can increase the cyclosporine levels in the blood and lead to harmful side effects.

What if I miss a dose?

If you miss a dose of cyclosporine oral capsule, you should take the missed dose as soon as you remember. However, if it is almost time for your next dose, take only that dose and skip the missed dose. Do not take twice the amount to make up for the missed dose, as this can cause serious side effects.

With any maintenance medication (medication used for long-term treatment), not taking the medication exactly as prescribed can lead to severe complications.

For cyclosporine oral capsules, stopping this medication or not taking it exactly as prescribed can lead to the rejection of the transplanted organ or the worsening of rheumatoid arthritis or psoriasis.

Overdosage

For up to 10 g of cyclosporine (approximately 150 mg/kg) oral doses, the following symptoms have been reported -- headache, drowsiness, vomiting, and fast heart rate. Most people recover with temporary liver disease and kidney damage. There are some cases of more severe kidney damage. However, they are reversible.

If you think you’ve taken more than the usual dose, call your doctor or the American Association of Poison Control Center at 80-222-1222.

If your symptoms are severe, call 911 or get emergency medical attention at the nearest emergency department.

Pregnancy/Lactation

There are not enough studies on the effects of cyclosporine in pregnant women. Therefore, cyclosporine should only be prescribed to pregnant women when the potential benefit justifies the potential risk.

Talk to your doctor if you get pregnant while taking cyclosporine.

Cyclosporine passes into breast milk. Mothers who are taking cyclosporine should not breastfeed.

What are the side effects of cyclosporine?

Serious side effects

Call your doctor if you experience the following side effects:

Unusual bleeding, easy bruising
Mental status change
Vision change
Problems with walking or speaking
Symptoms of liver damage:
- Dark urine
- Nausea, loss of appetite
- Itching
- Lethargy
- Pale stools
- Jaundice (yellowing of the skin or the whites of the eyes)
- Stomach pain
Symptoms of kidney damage:
- Bloody or painful urination
- Nausea
- Vomiting
- Lethargy
- Unusual swelling of ankles and feet
- Muscle pain and cramps
Symptoms of heart problems:
- Unusual swelling of legs and ankles
Signs of infections:
- Fever, chills, flu-like symptoms
- Skin sores, lightheadedness, fast heart rate, shortness of breath
Symptoms of high potassium:
- Weakness
- Heart palpitations
- Muscle pain and weakness
- Shortness of breath
Symptoms of high blood pressure:
- Headache
- Racing heartbeat
- Chest discomfort
- Shortness of breath
- Vision change
- Confusion
Symptoms of brain damage:
- Vision changes (including blindness)
- Muscle or movement problems
- Loss of consciousness
- Seizures
- Mood disturbances

In rare cases, cyclosporine can cause a blood disorder resulting in low levels of platelets and red blood cells. Tell your doctor if you have a history of anemia or low platelet levels. This blood disorder can cause transplant failure if left untreated.

You should seek emergency medical attention if you experience any of the above symptoms.

Common side effects

Nausea, vomiting, diarrhea, stomach discomfort
Tremors
Headache
Acne
Increased hair growth on the face and other body parts
Unusual growth of gum tissue

These side effects should get better within a few weeks. Certain side effects can be improved with self-care, such as seeing a dentist regularly and practicing good personal hygiene.

Cyclosporine contraindications

Hypersensitivity

You should not take cyclosporine if you are allergic to cyclosporine or to any ingredients of the formulation. Ask your doctor or pharmacist for information on all of the ingredients of the medications you take.

Rheumatoid arthritis patients with certain comorbidities

You should not take Cyclosporine to treat rheumatoid arthritis if you have chronic kidney disease (CKD) or uncontrolled high blood pressure. Cyclosporine is also not safe if you have tumors.

Radiation therapy and other treatments for psoriasis

Psoriasis patients who take cyclosporine should not be treated with PUVA (Psoralen plus ultraviolet A), UVB therapy, radiation treatment, coal tar, methotrexate, or other medicines that suppress the immune system.

Taking cyclosporine may increase the risk of skin disease in those who have already received the above treatments for psoriasis.

You should always wear protective clothing and use a broad-spectrum sunscreen to decrease your risk of skin cancer.

Other warnings

Cyclosporine oral solution contains alcohol, which is unsafe for children, pregnant women, and breastfeeding mothers. In addition, the alcohol-containing oral solution should also be avoided if you have liver problems or seizures.
Talk to your healthcare providers before receiving a vaccination, as cyclosporine can reduce the effectiveness of vaccines.
Cyclosporine reduces the body’s ability to fight infections leading to an increased risk of infection and cancer. This risk could be significant in organ transplant patients who received more than immunosuppressant medications.
Only physicians who are experienced in management of immunosuppressive therapy prescribe cyclosporine. Patients receiving cyclosporine should be managed in facilities equipped with appropriate staff, laboratory, and medical resources.
Because of the difference in bioavailability between these formulations, these different formulations of cyclosporine are not interchangeable, and patients should not be switching from one formulation to another without a physician’s guidance and supervision.

Due to the high concentration of cyclosporine modified (Neoral, Gengraf), if your doctor switches you to Neoral or Gengraf from Sandimmune, you will have blood tests ordered by your doctor to monitor the blood levels of cyclosporine to prevent toxicity.

Drug Interactions

Just like any medicine, cyclosporine can interact with other medications and vice versa. Drug interactions can affect the blood tests that evaluate blood levels and can also lead to worsening side effects or cause other drugs to be less effective.

Tell your doctor or pharmacist about other drugs you are currently taking, including other prescription medications, over-the-counter products, and herbal and dietary supplements. The following drugs can have an interaction with cyclosporine:

Nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, sulindac, diclofenac, naproxen
Certain antibiotics such as azithromycin, erythromycin, vancomycin, gentamicin, tobramycin, rifampin
Antifungals such as amphotericin B, fluconazole, terbinafine
HIV medications such as ritonavir, indinavir, and nelfinavir
High blood pressure medications and calcium channel blockers such as verapamil, diltiazem, and nicardipine
Cancer therapy drugs such as doxorubicin, etoposide, melphalan
Steroid medications, such as Prednisone, methylprednisolone
Seizure medications, such as Phenytoin, carbamazepine, phenobarbital, oxcarbazepine
Cholesterol medications, such as Atorvastatin, simvastatin, fluvastatin, lovastatin, fenofibrate, gemfibrozil
Immunosuppressants, such as Tacrolimus
Herbal supplements, such as St. John’s wort
Birth control pills
GERD (gastroesophageal reflux disease) therapy, such as cimetidine

Cyclosporine can interact with many other drugs. Not all drug interactions are listed here. Ask your doctor or pharmacist about the potential drug interactions between your current medications and cyclosporine.

Reference:

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