Cyclosporine (Gengraf™; Neoral®; Sandimmune®)

Drug Class

  Immunosuppressive drugs of this class prevent rejection of transplanted organs such as kidneys and suppress the immune system to treat systemic autoimmune diseases such as lupus nephritis and vasculitis. 

 

Mechanism of Action

Cyclosporine inhibits production and release of a cellular substance known as interleukin II.  This inhibition prevents interleukin II from activating T lymphocytes.  It is used to treat many kidney disorders such as systemic vasculitis, lupus nephritis, and membranous nephropathy.  Cyclosporine is also used to treat rheumatic diseases.


Dosage Regimens 

    Condition Information Oral Dosage Intravenous Dosage

    Rheumatoid arthritis

    patients who have inadequate responses to methotrexate

    Initial:  Neoral® 2.5 mg/kg daily; divided into 2 doses
    Dose may be increased by 0.5-0.75 mg/kg/day at 8 and 12 weeks; Maximum dose is 4 mg/kg/day

     

    Transplanted organ rejection

    For kidney, liver and heart transplants; prophylaxis treatment;use with adrenal corticosteroids

    Initial (preoperative): 15 mg/kg 4-12 hr before transplant, continue same dose for 1-2 wk; Neoral® total daily dose should be divided into 2 equal daily doses
    Maintenance: decrease by 5% per week to 5-10 mg/kg/day

    Initial (preoperative): 5-6 mg/kg/day 4-12 hr before transplant; continue same dose as daily dose until patient can tolerate oral formulation

    Systemic vasculitis, membranous nephropathy

     

    3-5 mg/kg daily in 2 divided doses

     
 


Contraindications  

 
  • This drug should NOT be taken if you are allergic to cyclosporine or polyoxyethylated castor oil (Cremophor).    
 

Common Side Effects

  • High blood pressure (hypertension)
  • Pancreatitis
  • Kidney function decline
  • Seizures
  • Infection 

Drug Interactions

Drug Name Interaction

Allopurinol (Zyloprim®); Clonidine (catapres®); Erythromycin; Ibuprofen (Motrin®); Naproxen (Naprosyn®, Alleve®); Verapamil (Calan®, Isoptin®, Verelan®)

Increased risk of cyclosporine toxicity causing kidney dysfunction, gall bladder disease and tingling sensations

Azathioprine (Imuran®)

Decreased cyclosporine concentrations in the blood

Colchicine

Increases risk of cyclosporine toxicity causing kidney dysfunction, gall bladder disease, and tingling sensations. Also causes gastrointestinal dysfunction and neuromyopathy.

Cyclophosphamide (Cytoxan®)

Decreased cyclosporine concentrations in the blood

Prednisone

Increased risk of cyclosporine toxicity (kidney dysfunction, gall bladder disease, tingling sensations)

  

Patient Instructions

  • Store at room temperature, away from heat and direct light.  Do not keep this medicine in the refrigerator or freezer.
  • If you forget to take your medicine or miss a dose, take it as soon as possible.  If it is close to the time for your next dose, skip the missed dose and take the medicine on schedule.  DO NOT take extra medicine to make up for missed doses.
  • You should not receive the injection form of this medication if you are allergic to cyclosporine, castor oil, or Cremophor® EL. 
  • Do not take this medication if you are breastfeeding.