Fingolimod 0.5mg Capsules

Fingolimod is a sphingosine 1-phosphate (S1P) receptor modulator. It is phosphorylated by sphingosine kinase in vivo to fingolimod phosphate, which is an active metabolite. Fingolimod phosphate binds with high affinity to S1P receptors 1, 3, 4, and 5. By binding to S1P1 receptors on lymphocytes, fingolimod phosphate blocks the egress of lymphocytes from lymph nodes, leading to a dose-dependent reduction in peripheral blood lymphocyte counts. This reduces the migration of lymphocytes into the central nervous system (CNS), thereby reducing inflammation and nerve damage associated with multiple sclerosis.

Serious Side Effects: Seek Medical Help Immediately

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention right away:

Allergic reactions: Rash, hives, itching, red, swollen, blistered, or peeling skin with or without fever, wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Infections: Fever, chills, severe sore throat, ear or sinus pain, cough, increased or changed sputum production, painful urination, mouth sores, or unhealing wounds.
Herpes infections: Cold sores, shingles, genital sores, severe headache, confusion, changes in vision, eye redness, or eye pain.
Meningitis: Headache with fever, stiff neck, nausea, confusion, or sensitivity to light.
Liver problems: Dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes.
Skin cancer: New warts, lumps, or skin growths; bleeding or unhealing sores; shiny, white, pink, red, or skin-colored bumps that bleed or do not heal; or changes in mole color or size.
Blood pressure changes: Severe headache, dizziness, fainting, or changes in vision.
Cardiovascular issues: Chest pain or pressure, shortness of breath, or worsening breathing difficulties.
Abnormal heart rhythms: Slow heartbeat or irregular heartbeat, especially within 6 hours of the first dose or up to 24 hours after the first dose. If you experience dizziness, slow heartbeat, irregular heartbeat, or fatigue, contact your doctor immediately.

Additional Serious Side Effects

Macular edema: An eye problem that can lead to permanent vision loss, especially in people with diabetes or a history of uveitis. If you notice light sensitivity, abnormal colors, blurriness, shadows, or blind spots in your vision, contact your doctor right away.
Posterior reversible encephalopathy syndrome (PRES): A rare but potentially life-threatening brain disorder. Seek medical help immediately if you experience confusion, decreased alertness, changes in vision, loss of vision, seizures, or severe headache.
Progressive multifocal leukoencephalopathy (PML): A rare and potentially disabling or fatal brain condition. Contact your doctor if you notice confusion, memory problems, depression, changes in behavior, uneven strength, speech or thinking difficulties, balance problems, or vision changes.
Lymphoma: A type of cancer. If you experience significant weight loss, night sweats, or swollen glands, contact your doctor right away.

Common Side Effects

Not everyone experiences side effects, and many people have only minor issues. However, if you notice any of the following side effects or if they persist or bother you, contact your doctor:

Headache
Flu-like symptoms
Stomach pain or diarrhea
Back pain
Pain in arms or legs
* Sinus pain

This is not an exhaustive list of potential side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
A history of certain health conditions, such as:
+ Abnormal heart rhythms (heart block, sick sinus syndrome, slow heartbeat, or long QT interval on an electrocardiogram [ECG])
+ Chest pain (angina)
+ Heart attack
+ Heart failure
+ Brain blood vessel disease (including transient ischemic attack [TIA] or stroke)
+ High blood pressure
+ Sleep apnea
If you have received the varicella (chickenpox) vaccine within the past month
If you are undergoing light therapy, as this may interact with the medication
If you are taking another medication that contains the same active ingredient
If you are taking or have recently taken medications that can cause a slow heartbeat, prolong the QT interval, or suppress your immune system. There are many medications that can have these effects, so it is crucial to consult with your doctor or pharmacist if you are unsure.

This list is not exhaustive, and it is vital to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. This will help ensure your safety and proper care.

To avoid accidents, do not drive or perform tasks that require alertness until you understand how this medication affects you. Your doctor will also instruct you to undergo regular blood tests and heart function checks. Additionally, you will need to have eye and skin exams to monitor your health.

Be aware that this medication can cause high blood pressure. Your doctor will advise you on how often to have your blood pressure checked. In some cases, your doctor may order an MRI scan before starting this medication.

This medication can interfere with certain laboratory tests. Inform all your healthcare providers and laboratory personnel that you are taking this medication. If you have not had chickenpox or received the chickenpox vaccine, discuss this with your doctor. It is also crucial to be up-to-date with all recommended vaccinations before starting treatment with this medication.

Before receiving any vaccines while taking this medication or within 2 months after stopping it, consult your doctor. The use of this medication may increase the risk of infection or reduce the effectiveness of vaccines. This medication can remain in your body for up to 2 months after your last dose and may affect your immune system. If you plan to take another medication that suppresses your immune system within 2 months after stopping this medication, discuss this with your doctor.

While taking this medication and for 2 months after stopping it, you may be more susceptible to infections, some of which can be severe or life-threatening. To minimize this risk, practice good hygiene by washing your hands frequently, and avoid close contact with people who have infections, colds, or flu.

There is an increased risk of human papillomavirus (HPV) infections, including HPV-related growths and cancer, associated with this medication. Your doctor may recommend an HPV vaccine before starting treatment. It is also essential to follow your doctor's instructions for regular Pap smears.

If you stop taking this medication, your multiple sclerosis (MS) symptoms may return and could be worse than before or during treatment. In many cases, people do not regain their previous level of function after stopping this medication. This effect often occurs within the first 12 weeks after stopping the medication but can happen later. If you experience worsening MS symptoms after stopping this medication, contact your doctor immediately.

This type of medication has been linked to an increased risk of skin cancer. To reduce this risk, limit your exposure to sunlight, sunlamps, and tanning beds. Use sunscreen with a high sun protection factor (SPF) and wear protective clothing when outdoors.

In rare cases, this medication can cause liver problems, which can be severe and may require a liver transplant. Discuss any concerns with your doctor.

This medication can harm an unborn baby. A pregnancy test will be performed before starting treatment to confirm that you are not pregnant. If you may become pregnant, use effective birth control while taking this medication and for 2 months after your last dose. If you become pregnant, notify your doctor immediately.

If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.

• Class Ia antiarrhythmics (e.g., quinidine, procainamide, disopyramide)
• Class III antiarrhythmics (e.g., amiodarone, sotalol, ibutilide, dofetilide)
• Patients with a history of Mobitz Type II second-degree AV block, third-degree AV block, or sick sinus syndrome (unless patient has a functioning pacemaker)
• Patients with a QTc interval ≥500 msec
• Patients with a history of symptomatic bradycardia or recurrent syncope
• Patients with acute infection requiring hospitalization
• Patients with active chronic infections (e.g., hepatitis, tuberculosis)
• Patients with severe active infections (e.g., severe herpes zoster, cryptococcal meningitis)
• Live attenuated vaccines (during and for 2 months after treatment)

• Other immunosuppressants (e.g., natalizumab, alemtuzumab, ocrelizumab, mitoxantrone, cyclophosphamide, azathioprine, methotrexate, corticosteroids): Increased risk of infection and immunosuppression.
• QT-prolonging drugs (e.g., antipsychotics, tricyclic antidepressants, macrolide antibiotics, fluoroquinolones): Increased risk of bradycardia and AV block.
• Beta-blockers, calcium channel blockers (non-dihydropyridine), digoxin, ivabradine: Increased risk of bradycardia and AV block.
• CYP4F2 inhibitors (e.g., fluconazole, ketoconazole): May increase fingolimod exposure.
• CYP4F2 inducers (e.g., carbamazepine, rifampin, phenobarbital, phenytoin): May decrease fingolimod exposure.

• Vaccines (non-live): May have reduced efficacy.
• Antineoplastic agents: Increased risk of immunosuppression.

• Not available

• Signs and symptoms of infection (fever, chills, sore throat, fatigue, unusual weakness)
• Visual changes (blurred vision, central vision loss, blind spots)
• Cardiac symptoms (dizziness, lightheadedness, syncope, chest pain, palpitations)
• Respiratory symptoms (new or worsening cough, shortness of breath)
• Neurological symptoms (new or worsening weakness, cognitive changes, speech difficulties, vision changes, numbness, tingling - suggestive of PML or other CNS infections)
• Liver injury symptoms (unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, dark urine, jaundice)
• Skin lesions (new or changing moles, suspicious growths)

Fingolimod is classified as Pregnancy Category D. It can cause fetal harm when administered to a pregnant woman. It is contraindicated in pregnant women. Women of childbearing potential must use effective contraception during treatment and for at least 2 months after stopping fingolimod.

Fingolimod and its active metabolite are excreted in breast milk. Due to the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment with fingolimod and for 2 months after the last dose.

Approved for pediatric patients 10 years of age and older with relapsing forms of MS. Dosing is weight-based for those under 40 kg. Safety and efficacy in pediatric patients younger than 10 years have not been established.

Use with caution in patients 65 years of age and older due to limited clinical experience and potentially increased risk of adverse reactions, particularly cardiac effects and infections. First-dose observation should be carefully managed.

• First-dose observation (FDO) is critical: Patients must be monitored for at least 6 hours after the first dose for bradycardia and AV block. An ECG should be performed at 6 hours. Extended monitoring may be required.
• Risk of severe rebound MS activity: Discontinuation of fingolimod, especially abrupt discontinuation, can lead to a severe exacerbation of MS, including new or worsening symptoms and MRI lesions. Patients should be monitored closely for several months after stopping.
• Infection risk: Fingolimod significantly reduces lymphocyte counts, increasing the risk of serious and opportunistic infections, including PML, cryptococcal meningitis, and herpes viral infections. Patients should be educated on signs of infection.
• Macular edema: Regular ophthalmologic exams are crucial, especially at 3-4 months post-initiation, and if any visual changes occur.
• Vaccination: Live attenuated vaccines are contraindicated. Non-live vaccines may be less effective. Vaccination status (especially VZV) should be assessed prior to initiation.
• Skin cancer risk: Increased risk of basal cell carcinoma and other skin malignancies. Regular skin examinations are recommended, and patients should be advised to use sun protection.

• Interferon beta-1a (e.g., Avonex, Rebif)
• Interferon beta-1b (e.g., Betaseron, Extavia)
• Glatiramer acetate (e.g., Copaxone, Glatopa)
• Natalizumab (Tysabri)
• Alemtuzumab (Lemtrada)
• Ocrelizumab (Ocrevus)
• Dimethyl fumarate (Tecfidera)
• Teriflunomide (Aubagio)
• Cladribine (Mavenclad)
• Siponimod (Mayzent)
• Ozanimod (Zeposia)
• Ponesimod (Ponvory)

If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a valuable patient fact sheet. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, we encourage you to discuss them with your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the substance taken, the amount, and the time it occurred.