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Pronunciation ⬇

SYE-kloe-spor-een

Classifications ⬆ ⬇

Therapeutic Classification: Immunosuppressant agents, antirheumatics (DMARD)

Pharmacologic Classification: polypeptides (cyclic)

Indications ⬆ ⬇

REMS


Unlabeled Use:
  • Management of recalcitrant ulcerative colitis.
  • Treatment of steroid-resistant nephrotic syndrome.
  • Treatment of severe steroid-resistant autoimmune disease.
  • Prevention and treatment of graft vs. host disease in bone marrow transplant patients.

Action ⬆ ⬇

  • Inhibits normal immune responses (cellular and humoral) by inhibiting interleukin-2, a factor necessary for initiation of T-cell activity.
Therapeutic effects:
  • Prevention of rejection reactions.
  • Slowed progression of rheumatoid arthritis or psoriasis.

Pharmacokinetics ⬆ ⬇

Absorption: Erratically absorbed (range 10–60%) after oral administration, with significant first-pass metabolism by the liver. Microemulsion (Neoral) has better bioavailability. IV administration results in complete bioavailability.

Distribution: Widely distributed, mainly into extracellular fluid and blood cells.

Protein Binding: 90–98%.

Metabolism/Excretion: Extensively metabolized by the liver by the CYP3A4 isoenzyme (first pass); excreted in bile, small amounts excreted unchanged in urine.

Half-Life: Children: 7 hr; Adults: 19 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTEONSETPEAKDURATION
POunknown‡2–6 hrunknown
IVunknownend of infusionunknown

‡Onset of action in rheumatoid arthritis is 4–8 wk and may last 4 wk after discontinuation; for psoriasis, onset is 2–6 wk and lasts 6 wk following discontinuation.

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Drug-drug:

Drug-Natural Products:

Drug-Food:

Route/Dosage ⬆ ⬇

Prevention of Transplant Rejection (Sandimmune)

Prevention of Transplant Rejection (Neoral)

Rheumatoid Arthritis (Neoral only)

Severe Psoriasis (Neoral only)

Autoimmune Diseases (Neoral only)

Availability ⬆ ⬇

(Generic available)

Assessment ⬆ ⬇

Lab Test Considerations:

Toxicity and Overdose:

Implementation ⬆ ⬇

IV Administration:

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

Gengraf, Neoral, SandIMMUNE

Code ⬆

NDC Code