Names and pronunciation
(fin-gol′i-mod) (fin-go′li-mod) Gilenya
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Drug reference
(fin-gol′i-mod) (fin-go′li-mod) Gilenya
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Func. class.: Immunosuppressant
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Chem. class.: Sphingosine 1-phos- phate receptor modulator
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ACTION: Binds with high affinity to sphingosine 1-phosphate receptors; blocks lymphocyte egress to lymph nodes, thereby reducing the number of periph- eral blood lymphocytes; may reduce lym- phocyte migration into the CNS
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USES: To reduce frequency of exacer- bation, to delay physical disability of relapsing forms of MS
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CONTRAINDICATIONS: Hyper- sensitivity Precautions: Pregnancy, breastfeeding, neonates/infants/children, AIDS, asthma, AV block, bradycardia, cardiac disease, COPD, diabetes mellitus, dysrhythmias, heart failure, hepatic disease, HIV, hyper- tension, immunosuppression, leukemia, lymphoma, QT prolongation, respiratory insufficiency, sick sinus syndrome, syn- cope, uveitis
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SIDE EFFECTS CNS: Asthenia, depression, fatigue, head- ache, dizziness, progressive multifocal leukoencephalopathy, migraine, pares- thesias, stroke CV: AV block, bradycardia, chest pain, hypertension, palpitations, QT prolongation EENT: Blurred vision, vision impairment, ocular pain, macular edema GI: Abdominal pain, anorexia, diarrhea, jaundice, vomiting, weight loss, hepatotoxicity HEMA: Leukopenia, lymphopenia, neutropenia INTEG: Alopecia, pruritus MS: Back pain RESP: Dyspnea, cough SYST: Infection, influenza, secondary malignancy
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INTERACTIONS Increase: risk of heart block, serious bradycardia—β-blockers, calcium chan- nel blockers, digoxin; avoid if possible Increase: immunosuppression— antineoplastics, immunosuppressants, immune-modulating therapies Increase: fingolimod effect—ketoconazole Increase: infection risk—live vaccines Decrease: effect of—inactive vaccines, toxoids Increase: risk of torsades de pointes— Class Ia/III antidysrhythmics
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DOSAGE AND ROUTES • Adult/child ≥10 and ≥40 kg: PO 0.5 mg/day Child ≥10 yr and ≤40 kg: 0.25 mg daily Hepatic dose • Adult: PO Child-Pugh C, total score >10: closely monitor, fingolimod exposure is doubled
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Available forms: Caps 0.5 mg
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Administer: PO route • Watch patient for 6 hr after initial dose or if product not given for >2 wk for development of bradycardia • Give without regard to food • Store at room temperature, protect from moisture
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Assess: • Multiple sclerosis: improving pares- thesia, muscle weakness, clonus, mus- cle spasms, difficulty with moving, dif- ficulty with coordination of balance, speech, swallowing, vision problems, fatigue; prevention of increasing dis- ability • Vision: opthalmologic exam baseline and periodically • Laboratory monitoring: baseline: CBC, LFTs, serum bilirubin, ophthalmo- logic exam, antibodies to VZV; if there is no history of chickenpox or no vaccina- tion, may give VZV vaccination to anti- body-negative patient before giving product, postpone for 1 mo after vacci- nation; obtain ECG for evidence of bra- dycardia, AV block; monitor pulmonary function tests periodically • Progressive multifocal leukoenceph- alopathy (PML): confusion, apathy, dizzi- ness, unstable gait; may be fatal, discon- tinue product, contact prescriber • Bradycardia: monitor for ≥6 hr after beginning dose, ECG before and after 1st dose, if heart rate <45 bpm or new heart block (2nd degree) occurs, do not use until F resolved • Infections: fever, chills, nausea, vomit- ing, fatigue, sore throat; monitor during and for up to 2 mo after last dose • Monitor for QT prolongation • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk, may cause fetal harm; contraception should be used during and for 2 mo after fi- nal dose; enroll in Gilenya Pregnancy Registry (1-877-598-7237) if pregnant; discontinue breastfeeding or product, excretion unknown
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Evaluate: • Therapeutic response: improved symp- toms of multiple sclerosis and prevention of increasing disability
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • About use of product and expected re- sults; provide med guide to patient • That continuing follow-up exams and laboratory tests will be required on a regular basis • Pregnancy/breastfeeding: To use con- traception during and for 2 mo after conclusion of treatment • Vaccines: not to receive any live atten- uated vaccines during and for ≥2 mo af- ter last dose • Malignancy: Use sunscreen, protective clothing; may cause melanoma basal cell carcinoma • Liver dysfunction: to report jaundice, nausea, vomiting, anorexia, abdominal pain, fatigue, dark urine • Cardiac changes: to report chest pain, palpitations
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PHARMACOKINETICS Protein binding (99.7%), distributed to RBCs (86%), steady-state 1-2 mo, metab- olized by CYP4F2 and CYP2D6 to a lesser extent, terminal half-life 6-9 days, excreted in urine (81% inactive metabo- lites), peak 12-16 hr
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• Adult/child ≥10 and ≥40 kg: PO 0.5 mg/day Child ≥10 yr and ≤40 kg: 0.25 mg daily Hepatic dose
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