Drug Guide
Fingolimod Hydrochloride
Classification
Therapeutic: Multiple Sclerosis Disease-Modifying Agent
Pharmacological: Sphingosine 1-phosphate receptor modulator
FDA Approved Indications
- Relapsing forms of multiple sclerosis (MS)
Mechanism of Action
Fingolimod is phosphorylated in vivo to form fingolimod-phosphate, which binds to sphingosine 1-phosphate receptors, sequestering lymphocytes in lymph nodes and preventing their migration into the central nervous system, thereby reducing MS flare-ups.
Dosage and Administration
Adult: 0.5 mg orally once daily
Pediatric: Not approved for pediatric use
Geriatric: Use with caution; adjust dose if necessary
Renal Impairment: Use with caution in patients with severe renal impairment
Hepatic Impairment: Use with caution in hepatic impairment; monitor liver function
Pharmacokinetics
Absorption: Well absorbed after oral administration, peak plasma levels in 12-16 hours
Distribution: Widely distributed; approximately 99.7% bound to plasma proteins
Metabolism: Primarily via CYP4F2 enzyme to inactive metabolites
Excretion: Metabolites excreted mainly in urine and feces
Half Life: 6-9 days, allowing once-daily dosing
Contraindications
- Acute or chronic autoimmune hepatitis
- History of myocardial infarction or unstable angina within 6 months
- Recent stroke or transient ischemic attack
- Baseline QTc interval >440 ms
- Heart failure
- Congenital long QT syndrome
- Recent arterial disease
- Infection with herpes zoster or other serious infections
Precautions
- Monitor for signs of infection, bradycardia, and macular edema; contraindicated in pregnancy; monitor LFTs periodically
Adverse Reactions - Common
- Bradycardia (Frequent)
- Headache (Common)
- Elevated liver enzymes (Common)
- Infections (e.g., herpes zoster) (Common)
Adverse Reactions - Serious
- Progressive multifocal leukoencephalopathy (PML) - rare but serious Ongoing risk from JC virus infection (Rare)
- Macular edema (Uncommon)
- Cardiac events (arrhythmia, conduction delays) (Uncommon)
- Liver injury leading to hepatitis, elevated liver enzymes (Rare)
Drug-Drug Interactions
- Avoid with Class Ia and III antiarrhythmics (e.g., quinidine, amiodarone) due to QT prolongation risk
- Caution with immunosuppressants and other immunomodulators
Drug-Food Interactions
- No specific interactions identified
Drug-Herb Interactions
- Limited data; caution advised
Nursing Implications
Assessment: Evaluate baseline cardiac status, LFTs, ophthalmologic and neurological assessments before initiation
Diagnoses:
- Risk for infection, bradycardia, hepatic impairment
Implementation: Monitor heart rate for at least 6 hours after first dose, and periodically thereafter; perform eye exams and liver function tests regularly; educate patient on signs of infection and vision changes
Evaluation: Assess for adverse reactions, infection, and efficacy in reducing MS relapses
Patient/Family Teaching
- Take medication exactly as prescribed, daily, without missing doses
- Report symptoms of infection, vision changes, or palpitations immediately
- Avoid pregnancy during and for 2 months after treatment—use effective contraception
- Attend scheduled eye and liver function exams
Special Considerations
Black Box Warnings:
- Increased risk of infections, including PML; fetal toxicity—must avoid pregnancy during treatment
Genetic Factors: None specific, but consider JC virus testing for PML risk assessment
Lab Test Interference: May alter lymphocyte count; monitor CBC regularly
Overdose Management
Signs/Symptoms: Bradycardia, hypotension, fever, chills, dizziness, or other signs of infection or cardiac distress
Treatment: Supportive care, continuous monitoring of cardiac function, and symptomatic treatment as needed; no specific antidote
Storage and Handling
Storage: Store at room temperature 15-30°C (59-86°F), protected from light and moisture
Stability: Stable under recommended storage conditions for the duration of the labeled shelf life