Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 0.5mg
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Multiple Sclerosis

Indicated for relapsing forms of multiple sclerosis to reduce clinical exacerbation frequency and delay accumulation of physical disability

0.5 mg PO qDay

>0.5 mg PO qDay increases adverse effects with no clinical benefits

Hepatic Impairment

Mild to moderate impairment: Dose adjustment not necessary

Severe impairment: Monitor therapy; exposure the drug may double in severe hepatic impairment

Dosing Considerations

May take with or without food

First dose monitoring

  • Due to decreased heart rate after the first dose, administer in setting with ability to manage symptomatic bradycardia; observe heart rate (HR) and blood pressure hourly for at least 6 hours post dose; obtain ECG prior to first dose and at the end of observation period
  • Continue observing beyond 6 hours if post-dose heart rate is <45 bpm or at the lowest post-dose value (suggesting maximal effect on heart rate may not yet have occurred), or if new onset second-degree or higher AV block occurs
  • In cases where pharmacologic intervention for symptomatic bradycardia is necessary, continuous overnight ECG monitoring required, because of this, repeat first-dose monitory for the second dose
  • Cardiac evaluation and overnight monitoring required for some pre-existing conditions and for concomitant use of certain medications (see Cautions for more specifics)
  • Heart rate generally returns to baseline 2-4 weeks after therapy initiation; physicians should continue to be alert to patient reports of cardiac symptoms

Reinitiation of therapy following discontinuation

  • If discontinued for >14 days, after the first month of treatment, the same first dose monitoring should be applied upon reinitiation
  • Within the first 2 weeks of treatment, first dose procedures are recommended after an interruption of 1 day or more
  • During weeks 3 and 4 of treatment, first dose procedures are recommended after an interruption >7 days

Demyelinating Polyneuropathy (Orphan)

Treatment of chronic inflammatory demyelinating polyneuropathy

Orphan indication sponsor

  • Novartis Pharmaceutical Corporation; One Health Plaza; East Hanover, NJ 07936

Safety and efficacy not established

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Interactions

Interaction Checker

and fingolimod

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Headache (25%)

            ALT/AST increased (14%)

            Influenza viral infection (13%)

            Diarrhea (12%)

            Back pain (12%)

            Cough (10%)

            1-10%

            Herpes viral infections (9%)

            Depression (8%)

            Bronchitis (8%)

            Dyspnea (8%)

            Sinusitis (7%)

            Dizziness (7%)

            Hypertension (6%)

            Gastroenteritis (5%)

            GGT increased (5%)

            Weight decreased (5%)

            Paresthesia (5%)

            Migraine (5%)

            Tinea infections (4%)

            Bradycardia (4%)

            Alopecia (4%)

            Blurred vision (4%)

            Lymphopenia (4%)

            Leukopenia (3%)

            Eye pain (3%)

            Eczema (3%)

            Pruritus (3%)

            Asthenia (3%)

            Blood triglycerides decreased (3%)

            <1%

            Macular edema (0.4%)

            Postmarketing Reports

            Third degree AV block and AV block with junctional escape

            Delayed onset transient asystole and unexplained death

            Syncope

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            Warnings

            Contraindications

            Hypersensitivity

            History within past 6 months of MI, unstable angina, stroke, TIA, decompensated heart failure requiring hospitalization or Class III/IV heart failure History or presence of Mobitz Type II second-degree or third-degree atrioventricular (AV) block or sick sinus syndrome, unless patient has a functioning pacemaker

            Baseline QTc interval ≥500 ms

            Treatment with Class Ia or Class III anti-arrhythmic drugs

            Cautions

            Use caution in patients with certain pre-existing cardiac conditions (eg, ischemic heart disease, history of myocardial infarction, congestive heart failure, history of cardiac arrest, cerebrovascular disease, history of symptomatic bradycardia, history of recurrent syncope, severe untreated sleep apnea, AV block, sino-atrial heart block, prolonged QTc interval, hypokalemia, hypomagnesemia, congenital long-QT syndrome) or those taking certain concomitant medications (eg, citalopram, chlorpromazine, haloperidol, methadone, erythromycin, beta-blockers, diltiazem, verapamil, digoxin) requre overnight monitoring following administration of first dose of medication

            Transient decrease in heart rate occurs within 1 hour after the first dose, with maximal decline generally occurring after 6 hr and heart rate recovering, although not to baseline, by 8-10 hr; a second period of heart rate decline may occur at 24 hr post-dose due to physiological diurnal variation; heart rate generally returns to baseline after 1 month of treatment

            Transient AV conduction delays have been observed after treatment initiation; most abnormalities are asymptomatic and usually resolve within 24 hours

            Caution with other drugs that cause bradycardia (eg, beta-blockers, diltiazem); also see Contraindications for Class 1a and Class III antiarrhythmics

            Increased risk of infection, do not initiate with active acute or chronic infections until resolved; prior to initiation, a recent CBC (ie, within 6 months or after discontinuation of prior therapy) should be available

            Concomitant use with antineoplastic agents, immunosuppressives, or immune modulating therapies may increase risk of immunosuppression

            Progressive multifocal leukoencephalopathy (PML) reported; symptoms are diverse and included sudden onset of severe headache, altered mental status, progressive unilateral weakness, clumsiness, visual disturbances, and seizure; symptoms usually reversible but may evolve into ischemic stroke or cerebral hemorrhage and delay in diagnosis and treatment may lead to permanent neurological sequelae; an MRI scan may find brain lesions before symptoms develop

            Vaccination may be less effective during and for up to 2 months after discontinuing fingolimod; avoid live attenuated vaccines during and for 2 months after fingolimod because of increased risk for infection

            May cause macular edema (with or without visual symptoms), evaluate before initiating treatment and 3-4 months after starting treatment or any time after a patient reports visual disturbances while in therapy; history of diabetes mellitus or uveitis have increased risk of macular edema

            Decreases pulmonary function tests (FEV 1, diffusion lung capacity for carbon monoxide)

            May increase liver transaminases; recent (ie, within last 6 months) transaminase and bilirubin levels should be available before initiating fingolimod

            Discontinue therapy if posterior reversible encephalopathy syndrome (PRES) suspected

            Women of childbearing potential should use effective contraception during and for 2 months after stopping

            Monitor BP during treatment

            Cryptococcal infections, including cases of cryptococcal meningitis, reported; patients with symptoms and signs consistent with cryptococcal meningitis should undergo prompt diagnostic evaluation and treatment

            Patients without confirmed history of chickenpox or without documentation of full course of vaccination against varicella zoster virus (VZV) should be tested for antibodies to VZV before initiating therapy; vaccination of antibody-negative patients is recommended prior to commencing therapy; postpone therapy 1 month to allow full effect of vaccination to occur

            Serious infections with opportunistic pathogens including viruses John Cunningham virus (JCV), herpes simplex viruses 1 and 2, varicella-zoster virus), fungi (e.g., cryptococci), and bacteria (e.g., atypical mycobacteria) reported; patients with symptoms and signs consistent with any of these infections should undergo prompt diagnostic evaluation and treatment

            Cases of Kaposi’s sarcoma reported; patients with symptoms or signs consistent with Kaposi’s sarcoma should receive prompt diagnostic evaluation and management

            Liver injury with hepatocellular and/or cholestatic hepatitis reported

            Basal cell carcinoma associated with therapy; monitor for suspicious skin lesions; if a suspicious skin lesion observed, promptly evaluate

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            Pregnancy & Lactation

            Pregnancy Category: C; based on animal studies, may cause fetal harm; effective contraception needed for women of childbearing age during treatment and for 2 months after discontinuation

            Gilenya pregnancy registry established 1-877-598-7237

            Lactation: Unknown whether distributed in breast milk, a decision should be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the drug to the mother

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Sphingosine 1-phosphate receptor modulator; metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate.  

            Binds with high affinity to sphingosine 1-phosphate receptors 1, 3, 4, and 5; blocks lymphocyte capacity to egress from lymph nodes, and thereby reduces the lymphocyte count in peripheral blood

            The mechanism by which fingolimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system

            Absorption

            Bioavailability: 93%

            Plasma Time: 12-16 hr

            Steady-State: Time to steady state is 1-2 months following daily dosing; steady-state levels approximately 10-fold greater than initial dose

            Distribution

            86% distributed in RBCs

            Protein Bound: >99%

            Vd: 1200 L

            Metabolism

            Primarily by CYP4F2, minor substrate of CYP2D6, 2E1, 3A4, and 4F12

            Elimination

            Half-life: 6-9 days

            Clearance: 6.3 L/hr

            Excretion: Feces (<2.5%), urine (81% as inactive metabolites)

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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