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Cyclosporine

Medical and Pharmacy Editor:

Brand Name: Neoral, Sandimmune, Gengraf

Generic Name: Cyclosporine

Drug Class: Immunosuppressants; DMARDs, Immunomodulators; Calcineurin Inhibitors

What Is Cyclosporine and How Does It Work?

Cyclosporine is used to prevent organ rejection in people who have received a liver, kidney, or heart transplant. It is usually used along with other medications to allow your new organ to function normally. Cyclosporine belongs to a class of drugs known as immunosuppressants. It works by slowing down your body's defense system (immune system) to prevent your body from rejecting a transplanted organ.

Because of the risk of severe allergic reactions from intravenous cyclosporine, it should be used only in patients who are unable to take cyclosporine by mouth. Once you are able to take medications by mouth, you should be switched from this form of cyclosporine to either the capsules or oral solution.

Cyclosporine may also be used to prevent rejection in other types of organ transplants (e.g., cornea, pancreas) or bone marrow transplant. It may also be used to treat other conditions that may be helped by affecting the immune system (e.g., Crohn's disease, ulcerative colitis).

Cyclosporine is available under the following different brand names: Neoral, Sandimmune, and Gengraf.

Dosages of Cyclosporine:

Dosages of Cyclosporine:

Adult and Pediatric Dosage Forms and Strengths

Capsule

  • 25 mg (Gengraf, Neoral, Sandimmune)
  • 50 mg (Gengraf, Sandimmune)
  • 100 mg (Gengraf, Neoral, Sandimmune)

Oral solution

  • 100mg/mL (Gengraf, Neoral, Sandimmune)

Injectable solution

  • 50 mg/mL (Sandimmune)

Dosage Considerations – Should be Given as Follows:

Solid Organ Transplantation

  • Prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants; has been used in combination with azathioprine and corticosteroids
  • Adjust dosage according to trough levels, general dosage guidelines listed below
  • Oral
    • 4-12 hours pre-transplant: 15 mg/kg orally for 1 dose
    • 1-2 weeks post-transplant: 15 mg/kg/day orally divided twice daily
    • Reduce 5% per week until: 5-10 mg/kg/day orally divided twice daily
  • Intravenous (IV)
    • 4-12 hours pre-transplant IV: 5-6 mg/kg IV for 1 dose over 2-6 hours
    • Post-transplant, until can tolerate oral therapy: 5-6 mg/kg IV once/day

Solid Organ Transplantation, Pediatric (Off-Label)

  • Children as young as 6 months have received cyclosporine to prevent solid organ transplant rejection
  • Dosage is same as adults, although children may require higher mg/kg dose than adults
  • Adjust dosage according to trough levels, general dosage guidelines listed below
  • Oral
    • 4-12 hours pre-transplant: 15 mg/kg orally for 1 dose
    • 1-2 weeks post-transplant: 15 mg/kg/day orally divided twice daily
    • Reduce 5% per week until: 5-10 mg/kg/day orally divided twice daily
  • Intravenous (IV)
    • 4-12 hours pre-transplant IV: 5-6 mg/kg IV for 1 dose over 2-6 hours
    • Post-transplant, until can tolerate oral therapy: 5-6 mg/kg IV once/day

Rheumatoid Arthritis

  • Indicated for severe active, rheumatoid arthritis where the disease has not adequately responded to methotrexate; may be used in combination with methotrexate
  • Gengraf or Neoral: 1.25 mg/kg orally twice daily; may increase by 0.5-0.75 mg/kg/day after 8 weeks and again after 12 weeks if needed, not to exceed 4 mg/kg/day
  • Discontinue if no improvement observed by 16 weeks
  • Decrease dose by 25-50% at any time to control adverse effects (e.g., hypertension, elevations in serum creatine greater than 30% pretreatment level

Psoriasis

  • Indicated for treatment of adult, non-immunocompromised patients with severe, recalcitrant, plaque psoriasis who have failed to respond to at least 1 systemic therapy (e.g., PUVA, retinoids, or methotrexate) or in patients for whom other systemic therapies are contraindicated, or cannot be tolerated
  • Gengraf or Neoral: 1.25 mg/kg orally twice daily; may increase by 0.5 mg/kg/day after 4 weeks and every 2 weeks if needed, not to exceed 4 mg/kg/day
  • Discontinue if no improvement observed at 6 weeks on maximum daily dose of 4 mg/kg/day
  • Decrease dose by 25-50% at any time to control adverse effects (e.g., hypertension, elevations in serum creatine greater than 30% pretreatment level

What Are Side Effects Associated with Using Cyclosporine?

Common side effects of Cyclosporine include:

Less common side effects of cyclosporine include:

Other side effects of cyclosporine include:

Serious side effects of cyclosporine include:

Postmarketing side effects of cyclosporine reported include:

  • Pain in lower extremities

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

What Other Drugs Interact with Cyclosporine?

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider or pharmacist first.

Severe Interactions of cyclosporine include:

Cyclosporine has serious interactions with at least 158 different drugs.

Cyclosporine has moderate interactions with at least 376 different drugs.

Cyclosporine has mild interactions with at least 105 different drugs.

This information does not contain all possible interactions or adverse effects. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share this information with your doctor and pharmacist. Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns or for more information about this medicine.

What Are Warnings and Precautions for Cyclosporine?

Warnings

Should be prescribed only by physicians who have experience with immunosuppression in solid organ transplant recipients and can provide necessary follow-up and appropriate monitoring.

Coadministration with other immunosuppressants in kidney, liver, and heart transplant recipients, but risk of infection and neoplasia may be increased.

Increased risk for development of lymphomas and other malignancies, particularly those of the skin; avoid excess UV light exposure.

Increased risk appears related to the intensity and duration of immunosuppression rather than to the use of specific agents; over-suppression of the immune system may result in infection or malignancy; caution with regimens containing multiple immunosuppressants.

Sandimmune and Neoral are not bioequivalent and should not be interchanged without physician approval; Neoral (capsules and oral solution) has increased bioavailability compared with Sandimmune (capsules and oral solution).

For a given trough concentration, cyclosporine exposure will be greater with Neoral than with Sandimmune.

Sandimmune has decreased bioavailability compared with Neoral and erratic absorption; requires careful monitoring of blood levels and subsequent dosage adjustments.

Patients with psoriasis who have been treated with PUVA, methotrexate or immunosuppressants, UVB, coal tar, or radiation are at increased risk for skin malignancies, hypertension, and renal dysfunction.

This medication contains cyclosporine.

Do not take Neoral, Sandimmune, or Gengraf if you are allergic to cyclosporine or any ingredients contained in this drug.

Keep out of reach of children. In case of overdose, get medical help or contact a Poison Control Center immediately.

Contraindications

  • Hypersensitivity
  • Breastfeeding
  • Rheumatoid Arthritis (RA)/Psoriasis use: Abnormal renal function, uncontrolled hypertension, malignancies
  • Psoriasis use: Concomitant PUVA, UVB radiation, coal tar, methotrexate, other immunosuppressants

Effects of Drug Abuse

  • No information available

Short-Term Effects

  • See "What Are Side Effects Associated with Using Cyclosporine?"

Long-Term Effects

  • See "What Are Side Effects Associated with Using Cyclosporine?"

Cautions

  • Injection: monitor closely for at least 30 minutes
  • Risk of hepatotoxicity and nephrotoxicity
  • Myelosuppression may be severe and prolonged; monitor complete blood and platelet counts
  • Potential increase risk for optic disk edema and infusion-related anaphylactic reactions
  • Some malignancies caused by cyclosporine immunosuppression may be fatal (e.g., lymphoma)
  • Serious and fatal cerebral, gastrointestinal and pulmonary hemorrhage; monitor platelets and coagulation parameters and treat accordingly
  • Anticipate and monitor for signs and symptoms of tumor lysis syndrome occur; treat promptly
  • Monitor for and discontinue promptly if systemic inflammatory response or capillary leak syndrome suspected
  • Monitor for signs and symptoms of infection; severe and fatal sepsis as a result of bone marrow suppression; discontinue therapy promptly if infection occur
  • Monitor for and discontinue if venous occlusive disease of the liver suspected
  • Monitor liver enzymes and discontinue therapy at first signs of severe hepatotoxicity; fatal hepatotoxicity may occur
  • Monitor renal function and interrupt or discontinue if creatinine levels increase or acute renal failure occur
  • Increased risk for serious infection with fatal outcome because of immunosuppression, including activation of latent viruses, e.g., BK virus-induced nephropathy
  • Patients with psoriasis who received coal tar, PUVA, methotrexate, or other immunosuppressants have higher risk of skin cancer with Neoral
  • Discontinue therapy if exfoliative or bullous rash suspected or if Stevens-Johnson syndrome or toxic epidermal necrolysis suspected
  • Monitor for signs and symptoms of enterocolitis and treat promptly
  • Extensively metabolized by CYP3A isoenzymes, in particular CYP3A4, and is a substrate of the multidrug efflux transporter P-glycoprotein (P-gp); various agents are known to either increase or decrease plasma or whole blood of cyclosporine levels usually by inhibition or induction of CYP3A4 or P-gp or both
  • Occasionally, patients develop a syndrome of thrombocytopenia and thrombotic microangiopathic hemolytic anemia may result in graft failure
  • Significant hyperkalemia and hyperuricemia may occur
  • Neurotoxicity may occur, particularly with high dose methylprednisolone; caution with other drugs that may cause neurotoxicity
  • Mild or moderate hypertension and rarely severe hypertension may occur; incidence decreases over time; antihypertensive therapy may be required in recipients of kidney, liver, and heart allografts treated with cyclosporine; potassium-sparing diuretics should not be used to treat cyclosporine associated hypertension as cyclosporine may cause hyperkalemia; calcium antagonists can be effective but can interfere with cyclosporine metabolism
  • Gingival hyperplasia may occur; avoid concomitant nifedipine administration in patients who develop gingival hyperplasia (swollen gums)
  • Seizures may occur when used in combination with high-dose corticosteroids

Pregnancy and Lactation

  • Use cyclosporine with caution during pregnancy if benefits outweigh risks. Animal studies show risk and human studies are not available or neither animal nor human studies were done. Take into consideration alcohol content of various cyclosporine formulations.
  • Cyclosporine is excreted in breast milk. Do not nurse while using cyclosporine.
Reviewed on 9/6/2017

Medscape. Cyclosporine.
https://reference.medscape.com/drug/neoral-sandimmune-cyclosporine-343196
RxList. Sandimmune Monograph.
https://www.rxlist.com/sandimmune-side-effects-drug-center.htm

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