To prevent the rejection of transplanted kidney, heart, liver and bone marrow.

Inhibition of production and release of IL-2 and inhibits IL-2-induced activation of resting T-lymphocytes

Oral absorption is erratic and incomplete, about 30%, dependent on presence of food, bile acid, and GI motility. Distribution: widely in tissues and body fluids including the liver, pancreas, and lung; across placenta, enters breast milk. Protein binding: 90-98% to lipoproteins. Extensively metabolized in liver via CYP450 3A4 enzyme. Elimination half-life: 10.5-15 hr in adults, 7.5 hr in children, prolonged in the elderly and in patients with liver dysfunction. Excretion: primarily feces; urine (6%, 0.1% as unchanged drug and metabolites)

hypersensitivity to cyclosporine

C

Contraindicated

Nephrotoxicity (30%), hyperkalemia, hypertension, hirsutism, hyperuricemia and gout, tremor, cramps, headache, gum hypertrophy, lymphomas, GI disturbances, and transient hepatoxicity.

1. Aplastic anemia (off-label use):
Severe: Oral: 5 mg/kg/day in 2 divided doses (in combination with antithymocyte globulin [equine] and eltrombopag) for a minimum of 12 months.
Non-severe: Oral: 2.5 mg/kg every 12 hours (with antithymocyte globulin [equine]) for at least 6 months.
2. Focal segmental glomerulosclerosis (off-label use): Oral: Initial: 3 to 5 mg/kg/day in 2 divided doses.
3. Graft-versus-host disease, chronic, treatment (off-label use): Oral: 6 mg/kg twice daily every other day (in combination with prednisone) until week 40, followed by a gradual cyclosporine taper. 4. Immune thrombocytopenia, refractory (off-label use): Oral: 2.5 to 3 mg/kg/day as monotherapy or in combination with other agents (eg, prednisone).
5. Myasthenia gravis, chronic immunosuppressive therapy (alternative agent) (off-label use): Oral: Initial: 2.5 mg/kg/day in 2 divided doses given every 12 hours.
6. Nephrotic syndrome (Canadian labeling): Oral: Initial: 3.5 mg/kg/day in 2 divided doses (every 12 hours).
7. Psoriasis: Oral: Initial dose: 1 to 3 mg/kg/day in 2 divided doses.
8. Solid organ transplantation: Renal: 9 mg/kg/day in 2 divided doses; Liver: 8 mg/kg/day in 2 divided doses; Heart: 7 mg/kg/day in 2 divided doses.
9. T-cell large granular lymphocytic leukemia, symptomatic (off-label use): Oral: 5 to 10 mg/kg/day (in 2 divided doses).
10. Ulcerative colitis, severe, steroid-refractory (off-label use): Oral: Cyclosporine (modified): 2.3 to 3 mg/kg every 12 hours.
11. Uveitis (off-label use): Oral: 2.5 to 5 mg/kg/day in 2 divided doses.