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Indications

REMS


Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

CV: asystole, bradycardia, heart block, QT interval prolongation, hypertension, syncope

Derm: BASAL/SQUAMOUS CELL CARCINOMA, MELANOMA

EENT: blurred vision, eye pain, macular edema

GI: liver enzymes, diarrhea, HEPATOTOXICITY

Hemat: leukopenia, lymphopenia

MS: back pain

Neuro: headache, posterior reversible encephalopathy syndrome (pres), progressive multifocal leukoencephalopathy (pml), tumefactive MS

Resp: cough, pulmonary function

Misc: hypersensitivity reactions (including angioedema), IMMUNE RECONSTITUTION INFLAMMATORY SYNDROME (IRIS), INFECTION (INCLUDING BACTERIAL, VIRAL AND FUNGAL), LYMPHOMA

Interactions

Drug-drug:

Availability

(Generic available)

Route/Dosage

US Brand Names

Gilenya, Tascenso ODT

Action

  • Converted by sphingosine kinase to the active metabolite fingolimod-phosphate, which binds to sphingosine 1-phosphate receptors, resulting in migration of lymphocytes into peripheral blood. This may lymphocyte migration into the CNS.
Therapeutic effects:
  • frequency of relapses/delayed accumulation of disability.

Classifications

Therapeutic Classification: anti-multiple sclerosis agents

Pharmacologic Classification: receptor modulators

Pharmacokinetics

Absorption: 93% absorbed following oral administration.

Distribution: Extensively distributed to body tissues; 86% of parent drug distributes into red blood cells; active metabolite uptake 17%.

Protein Binding: >99.7%.

Metabolism/Excretion: Converted to its active metabolite, then metabolized mostly by the CYP4F2 isoenzyme, with further degradation by other enzyme systems. Most inactive metabolites excreted in urine (81%); <2.5% excreted as fingolimod and fingolimod-phosphate in feces.

Half-Life: 6–9 days.

Time/Action Profile

ROUTEONSETPEAKDURATION
POunknown1–2 mo*2 mo

*Time to steady state plasma concentrations, peak plasma concentrations after a single dose at 12–16 hr.

Time for complete elimination.

Patient/Family Teaching

Pronunciation

fin-GO-li-mod

Code

NDC Code