Fingolimod

Also known as: FTY720

Drug #2249

The first oral treatment for the relapsing forms of multiple sclerosis. It may replace current treatment with interferon-beta 1a intramuscular injections. It binds with high affinity to sphingosine-1-phosphate receptors. Blocks the capacity of lymphocytes to leave the lymph nodes, reducing their number in peripheral blood. Its exact mechanism of action in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system. It is indicated for the treatment of patients with relapsing forms of multiple sclerosis to reduce frequency of relapses and to delay the accumulation of physical disability.

← Previous drug Next drug →

Primary Characteristics

Fingolimod is also known as FTY720, Fingolimod hydrochloride.

It belongs to Immunomudulator.

It belongs to Immune Modifiers pharmacological group on the basis of mechanism of action.

Molecular Weight: 307.5 · pK_a: 7.82 · Solubility in Water: High Solubility at low ph · Non-proprietary name: Fingolimod.

Pharmacokinetics

Absorption: Fingolimod has an oral bioavailability is 93%, pre-systemic (first-pass) metabolism accounts for 10% (±10%).

Distribution: Fingolimod has a volume of distribution is 1200 L. plasma protein binding is greater than 99.7%.

Elimination: it is metabolised via active metabolite fingolimod-phosphate., plasma half-life is 6-9 days, renal excretion is 81%.

Indications

Fingolimod is primarily indicated in conditions like Multiple sclerosis.

Contraindications

Fingolimod is contraindicated in conditions like Hepatitis, Tuberculosis, Immunocompromised patient, Malignancy, Severe liver impairment, Hypersensitivity to any component of product, Severe infections.

Dosage

Fingolimod's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0.5 mg	0.5 mg	Every 24h	PO	can be taken with or without food.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

None recorded.

Side Effects

Fingolimod in overdosage may give rise to further complications which include Hepatic impairment , Leukopenia.

Fingolimod produces potentially life-threatening effects which include Allergic reactions, Hives, Rash, Cancer, Severe liver toxicity, Macular edema, Life threatening infections, Varicella Zoster infection, Brian infection, Allergic reactions, Trouble breathing. Careful monitoring is needed with proper medical management.

The signs and symptoms that are produced after acute overdosage of Fingolimod are Bradycardia, Mild chest tightness or discomfort, Slow AV conduction.

Fingolimod is known to cause more or less tolerable side effects which are usually transient. These include Asthenia , Back pain, Blurred vision, Bradycardia , Bronchitis , Cough , Depression, Diarrhea, Dizziness, Eye Pain , Headache, Herpes viral infection, Hypertension , Increased SGPT, Influenza viral infection, Lymphopenia, Migraine , Pneumonia , Sinusitis .

Warnings / Precautions

It may decarease heart rate and AV conduction after the first dose. There is increased risk of infection. It may cause Macular edema, Hepatic dysfunction, decrease in pulmonary function tests, and Lympho and leukopenia. Fingolimod remains in blood for up to 2 months after dicontinuation. Other immunosuppressants should be avoided or used with caution during this time. Since fingolimod reduces blood lymphocyte counts via re-distribution in secondary lymphoid organs, peripheral blood lymphocyte counts cannot be utilised to evaluate the lymphocyte subset status of a patient treated with it. Laboratory tests involving the use of circulating mononuclear cells require larger blood volumes due to reduction in the number of circulating lymphocytes. QTc interval prolongation.

Interference in Pathology

Fingolimod may interfere in the diagnosis of Reduce blood lymphocytes count.

Available Brands

None recorded.

Storage Conditions

Fingolimod should be stored .

Drug Classification

1.8.1 — Immunomodulators