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Usual Adult Dose for:
Additional dosage information:
Usual Adult Dose for Multiple Sclerosis
Initial dose: 0.5 mg orally once daily.
Renal Dose Adjustments
No adjustment recommended
Liver Dose Adjustments
Mild to moderate liver dysfunction: No adjustment recommended.
Severe liver dysfunction: Caution and close monitoring are recommended.
Although no specific dose adjustment guidelines have been suggested, caution is recommended in elderly patients (65 years of age or older).
Because of a risk for bradyarrhythmia and atrioventricular (AV) blocks, patients should be carefully monitored during fingolimod treatment initiation. Initiation of fingolimod treatment results in a decrease in heart rate. This typically occurs within an hour of the first dose with the nadir seen within 6 hours. In some instances, the nadir can be observed up to 24 hours after the first dose. Following the second dose, a further decrease in heart rate may occur, but this change is typically of a smaller magnitude than that observed following the first dose. With continued dosing, the heart rate typically returns to baseline within one month.
The first dose of fingolimod should be given in a setting with appropriate resources to manage symptomatic bradycardia. All patients should be observed for at least 6 hours for signs and symptoms of bradycardia (including hypotension, dizziness, fatigue, palpitations, and chest pain) with hourly pulse and blood pressure measurement. An electrocardiogram (ECG) is recommended in all patients prior to dosing, and at the end of the observation period.
If the heart rate 6 hours postdose is less than 45 bpm, or is at its lowest value, or if the ECG 6 hours postdose shows new onset second degree or higher AV block, additional observation should be instituted until these findings have resolved.
Should postdose symptomatic bradycardia occur, initiate appropriate management, begin continuous ECG monitoring, and continue observation until the symptoms have resolved. Should the symptomatic bradycardia require pharmacologic intervention, continuous overnight ECG monitoring in a medical facility is recommended. In this scenario, the first dose monitoring strategy should be repeated after the second dose.
Patients with certain preexisting conditions (e.g., 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, sinoatrial heart block) may poorly tolerate the fingolimod- induced bradycardia, or experience serious rhythm disturbances after the first dose of fingolimod. Prior to treatment with fingolimod, these patients should have a cardiac evaluation and if treated with fingolimod, should be monitored overnight with continuous ECG in a medical facility after the first dose.
Since initiation of fingolimod treatment results in decreased heart rate and may prolong the QT interval, patients with a prolonged QT interval (greater than 450 ms in males, greater than 470 ms in females) before dosing or during 6 hour observation, or patients at additional risk for QT prolongation (e.g., hypokalemia, hypomagnesemia, congenital long QT syndrome, concurrent therapy with QT prolonging drugs) should be monitored overnight with continuous ECG in a medical facility. Fingolimod is contraindicated in patients with a baseline QTc of 500 ms or greater.
If, after the first month of treatment, fingolimod therapy is discontinued for more than 14 days, the effects on heart rate and
AV conduction may recur on reintroduction of fingolimod treatment and the same first dose monitoring precautions as for initial dosing should apply. Within the first 2 weeks of treatment, first dose procedures are recommended after interruption of one day or more. During weeks 3 and 4 of treatment, first dose procedures are recommended after treatment interruption of more than 7 days.
Use of fingolimod has been associated with an increase in blood pressure which typically develops approximately 2 months after initiating treatment and persists with continued treatment. Blood pressure should be monitored throughout treatment.
Caution and close monitoring are recommended in patients with severe liver dysfunction. An increase in liver enzymes has been reported in patients treated with fingolimod. In most cases, liver transaminase elevations occurred within the first 6 to 9 months of treatment and returned to normal within 2 months following discontinuation of fingolimod. Liver enzymes and bilirubin levels should be obtained prior to initiation of therapy and in patients who develop symptoms of liver dysfunction (e.g., nausea, vomiting, anorexia, abdominal pain, fatigue, jaundice, dark urine). Patients with preexisting liver dysfunction may be at an increased risk of developing fingolimod induced elevated liver enzymes. Fingolimod should be discontinued in patients who develop significant liver dysfunction.
Dose-dependent reductions in FEV1 and diffusion lung capacity for carbon monoxide (DLCO) have been reported within 1 month after initiation of fingolimod. If clinically warranted, spirometric assessment of respiratory function and evaluation of DLCO is recommended during treatment.
A complete blood count (CBC) is recommended prior to initiating treatment with fingolimod. In patients with active acute or chronic infection, treatment with fingolimod should be delayed until the infection is resolved. Patients should be monitored for signs of infection during treatment and for 2 months following discontinuation. Patients should be advised to report signs of infection to their healthcare provider. Interruption of therapy should be considered in patients who develop a serious infection during treatment with fingolimod.
Safety and effectiveness have not been established in pediatric patients (less than 18 years of age).
Data not available
The US FDA requires a Risk Evaluation and Mitigation Strategy (REMS) for fingolimod. It includes a communication plan. Additional information is available at www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm111350.htm.
Fingolimod may be administered with or without food.
Doses greater than 0.5 mg daily have been associated with a higher incidence of adverse effects and no additional benefit.
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