SYE-kloe-spor-een
Therapeutic Classification: Immunosuppressant agents, antirheumatics (DMARD)
Pharmacologic Classification: polypeptides (cyclic)
REMS
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%.
Half-Life: Children: 7 hr; Adults: 19 hr.
(plasma concentrations)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO | unknown‡ | 2–6 hr | unknown |
| IV | unknown | end of infusion | unknown |
‡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.
Contraindicated in:
Use Cautiously in:
CV: hypertension
Derm: hirsutism, acne, psoriasis
F and E: hyperkalemia, hypomagnesemia
GI: diarrhea, nausea, vomiting, abdominal discomfort, anorexia, HEPATOTOXICITY, PANCREATITIS
GU: nephrotoxicity
Hemat: anemia, leukopenia, thrombocytopenia
MS: lower extremity pain
Neuro: tremor, confusion, flushing, headache, hyperesthesia, paresthesia, POSTERIOR REVERSIBLE ENCEPHALOPATHY SYNDROME (PRES), PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY (PML), psychiatric problems, SEIZURES
Misc: gingival hyperplasia, hypersensitivity reactions, infection (including activation of latent viral infections such as BK virus-associated nephropathy), MALIGNANCY
Drug-drug:
Drug-Natural Products:
Drug-Food:
Prevention of Transplant Rejection (Sandimmune)
Prevention of Transplant Rejection (Gengraf or Neoral)
Rheumatoid Arthritis (Gengraf or Neoral)
Severe Psoriasis (Gengraf or Neoral)
Autoimmune Diseases (Neoral only)
Lab Test Considerations:
Toxicity and Overdose:
IV Administration:
NDC Code