Cyclosporine

DEA Class; Rx

Common Brand Names; Neoral, Sandimmune, Gengraf

• DMARDs, Immunomodulators; 
• Immunosuppressants; 
• Calcineurin Inhibitors
•  

Prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants; has been used in combination with azathioprine and corticosteroids

Indicated for severe active, rheumatoid arthritis where the disease has not adequately responded to methotrexate; may be used in combination with methotrexate

Indicated for treatment of adult, nonimmunocompromised patients with severe, recalcitrant, plaque psoriasis who have failed to respond to at least 1 systemic therapy (eg, PUVA, retinoids, or methotrexate) or in patients for whom other systemic therapies are contraindicated, or cannot be tolerated

Orphan Designations

ALS

• Treatment of amyotropohic lateral sclerosis and its variants

Traumatic Brain Injury

• Treatment of moderate-to-severe traumatic brain injury

Lung Transplant

• Prophylaxis of organ rejection in patients receiving allogeneic lung transplant
• Treatment of acute rejection in recipients of allogeneic lung transplants

GVHD

• Prophylaxis and treatment of graft versus host disease

Lung Allograft Rejection

• Liposomal: For aerosolized administration in the prevention and treatment of lung allograft rejection

Pulmonary Rejection With BMT

• Liposomal: For aerosolized administration in the prevention and treatment of pulmonary rejection events associated with bone marrow transplant (BMT)

Bronchioitis Obliterans (Orphan)

• Liposomal cyclosporine for inhalation

Hypersensitivity

Breastfeeding

(RA/Psoriasis use): Abnormal renal function, uncontrolled HTN, malignancies

(Psoriasis use) Concomitant PUVA, UVB radiation, coal tar, methotrexate, other immunosuppressants

• Tremor (12-55%)
• Nephrotoxicity (32%)
• Hypertension (26%)
• Infection (3-25%)
• Headache (2-25%)
• Nausea (23%)
• Hirsutism (21%)
• Hypertrichosis (5-19%)
• Female reproductive disorder (5-19%)
• Gum hyperplasia (2-16%)
• Triglycerides increased (15%)
• Abdominal discomfort (1-15%)
• URI (1-14%)
• Diarrhea (3-13%)
• Dyspepsia (2-12%)
• Leg cramps (2-12%)
• Parathesia (1-11%)
• Acne
• Convulsions
• Pruitus
• Hyperkalemia, hypomagnesemia
• Pancreatitis
• Hepatotoxicity
• Flu-like syndrome

Injection: monitor closely for at least 30 min

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 (eg, 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, eg, 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

Pregnancy Category: C; take into consideration alcohol content of various cyclosporine formulations

Lactation: excreted in breast milk, do not nurse

Cyclosporine 

capsule

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

oral solution

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

injectable solution

• 50mg/mL (Sandimmune)