1. Indications and Usage
\nRelapsing Multiple Sclerosis:
\nIndicated for the treatment of patients with relapsing forms of multiple sclerosis (RMS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults and pediatric patients 10 years of age and older.
\n2. Dosage and Administration
\nRoute of Administration:
\nFor Oral Use ONLY. Swallow capsules whole; do not open or crush. Can be taken with or without food.
\nRecommended Dosage:
\nAdults and Pediatric Patients (>40 kg): 0.5 mg once daily.
\nPediatric Patients (10 to <40 kg body weight): 0.25 mg once daily.
\nNote: Doses higher than 0.5 mg provide no additional benefit and are associated with an increased rate of adverse reactions.
\nFirst-Dose Monitoring:
\nBecause fingolimod initiation results in a decrease in heart rate, all patients must undergo first-dose monitoring in a healthcare facility equipped to treat symptomatic bradycardia. This includes obtaining an ECG before dosing and monitoring hourly pulse and blood pressure for 6 hours post-dose. Extended overnight monitoring may be required if heart rate drops significantly or conduction abnormalities occur.
\nMissed Doses \/ Treatment Interruption:
\nIf a dose is missed during the first two weeks of treatment, medical supervision and first-dose monitoring are required for the next dose. If treatment is interrupted for more than 14 days after the first month of therapy, first-dose monitoring procedures must be repeated upon reinitiation.
\n3. Mechanism of Action
\nS1P Receptor Modulation:
\nFingolimod is phosphorylated in vivo to form fingolimod-phosphate, which acts as a functional antagonist at sphingosine 1-phosphate (S1P) receptors 1, 3, 4, and 5.
\nLymphocyte Sequestration:
\nBy binding to S1P receptors on lymphocytes, fingolimod prevents their egress from lymph nodes. This sequestration reduces the number of circulating autoreactive lymphocytes capable of infiltrating the central nervous system (CNS), thereby reducing CNS inflammation and demyelination characteristic of multiple sclerosis.
\n4. Safety and Warnings
\nCardiovascular Effects (Bradycardia & AV Block):
\nInitiation causes transient bradycardia and atrioventricular (AV) conduction delays. It is contraindicated in patients with recent myocardial infarction, unstable angina, stroke, NYHA Class III\/IV heart failure, or high-degree AV block without a pacemaker.
\nInfections & Immunosuppression:
\nIncreases the risk of infections, including opportunistic infections like Progressive Multifocal Leukoencephalopathy (PML). Test for varicella-zoster virus (VZV) antibodies prior to initiation; vaccinate VZV-negative patients one month before starting therapy. Avoid live-attenuated vaccines during treatment and for 2 months after discontinuation.
\nMacular Edema:
\nRisk of fingolimod-associated macular edema. Baseline ophthalmologic evaluation is recommended, with follow-up exams at 3\u20134 months and periodically thereafter. Risk is higher in patients with diabetes or a history of uveitis.
\nHepatotoxicity:
\nElevations in liver enzymes can occur. Assess liver function tests within 6 months prior to initiation and monitor periodically. Discontinue if significant hepatic injury is suspected.
\nPost-Treatment Disease Rebound:
\nSevere worsening of MS, including tumor-like lesions, has been reported within 12 weeks (up to 24 weeks) after stopping fingolimod. Close clinical and MRI monitoring is required upon discontinuation.
\nEmbryo-Fetal Toxicity:
\nMay cause fetal harm. Females of reproductive potential must use effective contraception during treatment and for 2 months after stopping.
\n5. Adverse Reactions
\nMost Common (Incidence \u226510%):
\nHeadache, elevated liver enzymes (ALT), diarrhea, cough, influenza, sinusitis, back pain, and abdominal pain.
\nOther Significant Reactions:
\nLymphopenia, decreased pulmonary function (FEV1 and DLCO reductions), hypertension, and peripheral skin cancers (basal cell carcinoma, melanoma).
\n6. Drug Interactions
\nHeart Rate-Lowering Drugs:
\nConcomitant use with beta-blockers, non-dihydropyridine calcium channel blockers (e.g., verapamil, diltiazem), or antiarrhythmics (Class Ia or III) may cause severe bradycardia or heart block. Avoid concomitant use or conduct intensive cardiac monitoring.
\nStrong CYP Inhibitors:
\nCo-administration with strong CYP inhibitors (e.g., ketoconazole) increases fingolimod exposure. Monitor these patients closely.
\nImmunosuppressants\/Antineoplastics:
\nConcurrent or recent use of immunosuppressive or antineoplastic therapies may lead to unintended additive immunosuppression. Exercise caution when transitioning between therapies.
\nVaccines:
\nVaccinations may be less effective during treatment and for up to 2 months post-treatment. Live vaccines should be avoided due to infection risk.
\n7. Pharmaceutical Information
\nChemical Composition:
\nActive Ingredient: Fingolimod Hydrochloride.
\nAvailable Strength: 0.5 mg hard gelatin capsules.
\nAppearance: White to off-white powder inside a hard capsule.
\nPharmacokinetics:
\nPeak plasma concentrations are reached within 12\u201316 hours. The half-life is approximately 6 to 9 days. It is extensively metabolized (primarily via CYP4F2) and excreted mainly in urine as inactive metabolites.
\nStorage:
\nStore at 20\u00b0C to 25\u00b0C (68\u00b0F to 77\u00b0F); excursions permitted to 15\u00b0C\u201330\u00b0C (59\u00b0F\u201386\u00b0F). Keep in original package to protect from moisture.<\/p>\n","protected":false},"excerpt":{"rendered":"
Brand Name:\u6377\u7075\u4e9a \u00ae(Gilenya\u00ae)
\nGeneric Name: Fingolimod Hydrochloride
\nStrength: 0.5 mg per capsule, 14 capsules\/blister, 2 blisters\/box (total 28 capsules per box)
\nManufacturer: Novartis Pharma Stein AG
\nMarketing Authorization Holder: Novartis Pharma Stein AG. Domestic filing entities are Beijing Novartis Pharma Co., Ltd. and Novartis (China) Limited.
\nApproval Date in China: July 12, 2019
\nRegistration Number: \u56fd\u836f\u51c6\u5b57 HJ20190024
\nStorage: Store at 20\u00b0C\u201325\u00b0C (68\u00b0F\u201377\u00b0F) in the original package, protected from light and moisture. Brief exposure to 15\u00b0C\u201330\u00b0C (59\u00b0F\u201386\u00b0F) is permitted. Keep out of the sight and reach of children.<\/p>\n
Price&Cost:Contact Us now for the best price of Fingolimod Hydrochloride(Gilenya)<\/p>\n","protected":false},"featured_media":3951,"comment_status":"open","ping_status":"closed","template":"","meta":[],"product_brand":[80],"product_cat":[26],"product_tag":[],"class_list":["post-3950","product","type-product","status-publish","has-post-thumbnail","product_brand-novartis","product_cat-capsules","first","instock","shipping-taxable","product-type-simple"],"yoast_head":"\n