Cyclosporine

NEORAL

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What it isCalcineurin inhibitor blocking T-cell activation; transplant rejection, psoriasis, and uveitis.

Why this oneIt provides rapid, potent immunosuppression without myelosuppression and works quickly in severe psoriasis.

What limits itNephrotoxicity and hypertension require creatinine and blood-pressure monitoring. A narrow index plus CYP3A4 and P-gp interactions makes levels essential.

FDA-approved for

transplant immunosuppression (1983)

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Only clinicians experienced in immunosuppression/organ-transplant management should prescribe; increases susceptibility to infection and to lymphoma/other neoplasia. Neoral and Sandimmune are not bioequivalent and are not interchangeable without physician supervision; monitor blood concentrations.

FDA dosing	Population	Start	Target	Max
Organ transplant (kidney/liver/heart) — prophylaxis of rejection	Adults	kidney 9, liver 8, heart 7 mg/kg/day BID divided	titrate to target blood trough concentration
Rheumatoid arthritis	Adults	2.5 mg/kg/day BID divided		4 mg/kg/day
Psoriasis	Adults	2.5 mg/kg/day BID divided		4 mg/kg/day

Titration RA: increase 0.5–0.75 mg/kg/day after 8 wk, again after 12 wk; psoriasis: increase ~0.5 mg/kg/day at 2-wk intervals after initial 4 wk

Renal Transplant: monitor renal function, reduce dose if indicated (nephrotoxic). RA/psoriasis: contraindicated in patients with impaired/abnormal renal function

Hepatic Reduce dose in severe liver impairment (clearance may be significantly reduced)

Instructions

Always give in two divided doses (BID) on a consistent schedule relative to meals
Avoid grapefruit and grapefruit juice
Oral solution: dilute with room-temperature orange or apple juice in a glass container and drink at once; do not let stand

Contraindications

Rheumatoid arthritis or psoriasis patients with abnormal renal function, uncontrolled hypertension, or malignancy
Psoriasis: concomitant PUVA/UVB, methotrexate or other immunosuppressives, coal tar, or radiation therapy

Cautions

Nephrotoxicity — monitor renal function
Hypertension
Increased risk of infection and of lymphoma/malignancy
Not bioequivalent to Sandimmune

Adverse reactions

Renal dysfunction
Hypertension
Hirsutism/hypertrichosis
Tremor
Gum hyperplasia
Headache
GI disturbances (nausea, diarrhea)

Pregnancy No identified drug-associated risk of major birth defects/miscarriage; increased hypertension, preeclampsia, preterm birth, and low birth weight

Lactation Undefined

⚠ BOXED WARNINGS