REMS
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:
Sandimmune cannot be used interchangeably with Gengraf or Neoral because they are not bioequivalent.
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)
Therapeutic Classification: Immunosuppressant agents, antirheumatics (DMARD)
Pharmacologic Classification: polypeptides (cyclic)
Absorption: Erratically absorbed (range 1060%) after oral administration, with significant first-pass metabolism by the liver.
Microemulsion (Gengraf or Neoral) has better bioavailability than Sandimmune.
IV administration results in complete bioavailability.Distribution: Widely distributed, mainly into extracellular fluid and blood cells.
Protein Binding: 9098%.
Half-Life: Children: 7 hr; Adults: 19 hr.
(plasma concentrations)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | unknown‡ | 26 hr | unknown |
IV | unknown | end of infusion | unknown |
‡Onset of action in rheumatoid arthritis is 48 wk and may last 4 wk after discontinuation; for psoriasis, onset is 26 wk and lasts 6 wk following discontinuation.
NDC Code