Cyclosporine
NEORAL
Pronunciation: SYE-kloe-spor-een
“Cycling spore is Sand-immune”
Multi-enzyme inhibitor
Pea nose → OAT-P inHibitor
What it isCalcineurin inhibitor blocking T-cell activation; transplant rejection, psoriasis, and uveitis.
Why this oneFast, potent immunosuppression without myelosuppression; in severe psoriasis at least as effective as methotrexate.
What limits itNephrotoxicity and hypertension require creatinine and blood-pressure monitoring. A narrow index plus CYP3A4 and P-gp interactions makes levels essential.
Pearls
- Psoriasis or atopic dermatitis: avoid continuous use beyond 1 year.
- Ophthalmic emulsion for dry eye; full effect may take 3 months.
- Hirsutism and hypertriglyceridemia are common nuisances.
- Pregnancy: low birth weight, prematurity; enters breast milk.
FDA-approved for
- transplant immunosuppression (1983)
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
FDA label
Read the full label on DailyMed ↗
| 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
Available strengths
- cap 25, 50, 100 mg
- sol 0.09, 0.1 %
- sol 100 mg/mL
- drops 0.0009 g/mL
- drops 1 mg/mL
- emulsion 0.05, 0.1 %
- inj 50 mg/mL
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
Cost
| Strength | #/mo | generic $ | CostPlus | |
|---|---|---|---|---|
| 25 mg | cap | 60 BID | $19.11/mo | offered |
| 50 mg | cap | 60 BID | $45.88/mo | offered |
| 100 mg | cap | 60 BID | $74.40/mo | offered |
| 0.09 % | sol | per unit | not offered | |
| 0.1 % | sol | per unit | not offered | |
| 100 mg/mL | sol | per unit | $2.04/mL | offered |
Other forms: Cyclosporine ophthalmic (RESTASIS)
Generic entry1999
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Memory aids: interaction avatars
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Self-check
- Which two measures monitor cyclosporine’s major organ/BP toxicities?
Creatinine and blood pressure. - Why are cyclosporine levels essential?
Narrow index plus CYP3A4/P-gp interactions.