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Cyclosporine

NEORAL

Pronunciation: SYE-kloe-spor-een

Cyclosporine ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Cyclosporine ballicule
Cyclosporine SANDIMMUNE mascot mnemonic cartoon
Visual mnemonic: Cyclosporine mascot
“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 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.

Cyclosporine molecular structure (skeletal formula)
Molecular structure: Cyclosporine

FDA-approved for

FDA label

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 dosingPopulationStartTargetMax
Organ transplant (kidney/liver/heart) — prophylaxis of rejectionAdultskidney 9, liver 8, heart 7 mg/kg/day BID dividedtitrate to target blood trough concentration
Rheumatoid arthritisAdults2.5 mg/kg/day BID divided4 mg/kg/day
PsoriasisAdults2.5 mg/kg/day BID divided4 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

Available strengths

Contraindications

Cautions

Adverse reactions

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

Lactation Undefined

Cost

Cyclosporine (NEORAL)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $CostPlus
25 mgcap60 BID$19.11/mooffered
50 mgcap60 BID$45.88/mooffered
100 mgcap60 BID$74.40/mooffered
0.09 %solper unitnot offered
0.1 %solper unitnot offered
100 mg/mLsolper unit$2.04/mLoffered

Other forms: Cyclosporine ophthalmic (RESTASIS)

Generic entry1999

⚠ BOXED WARNINGS

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.

Open Cyclosporine in the interactive console ↗

Memory aids: interaction avatars

Cyclosporine BCRP inhibitor avatar mnemonic
BCRP inhibitor
Cyclosporine CYP3A4 inhibitor avatar mnemonic
CYP3A4 inhibitor (moderate)
Cyclosporine CYP3A4 substrate avatar mnemonic
CYP3A4 substrate
Cyclosporine OATP inhibitor avatar mnemonic
OATP inhibitor
Cyclosporine P-gp inhibitor avatar mnemonic
P-gp inhibitor (strong)
Cyclosporine P-gp substrate avatar mnemonic
P-gp substrate (sensitive)

Open Cyclosporine in the interactive console ↗