Lifitegrast
Lifitegrast Uses, Dosage, Side Effects, Food Interaction and all others data.
Lifitegrast binds to the integrin LFA-1, a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1). ICAM-1 may be overexpressed in corneal and conjunctival tissues in DED. LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell activation and migration to target tissues. In vitro studies demonstrated that lifitegrast may inhibit Tcell adhesion to ICAM-1 in a human T-cell line and may inhibit secretion of inflammatory cytokines in human peripheral blood mononuclear cells. The exact mechanism of action of lifitegrast in DED is not known.
Lifitegrast addresses both the symptoms and the resulting ocular surface damage by interfering with ocular inflammatory cycle . Lifitegrast is a lymphocyte function–associated antigen-1 antagonist through direct competitive antagonism and sequentially inhibits the T-cell recruitment, activation, and proinflammatory cytokine release associated with dry eye syndrome .
| Trade Name | Lifitegrast |
| Generic | Lifitegrast |
| Lifitegrast Other Names | Lifitegrast |
| Weight | 5% |
| Type | Ophthalmic solution |
| Formula | C29H24Cl2N2O7S |
| Weight | Average: 615.48 Monoisotopic: 614.0681277 |
| Protein binding | Human plasma protein binding of lifitegrast was approximately 99%, independent of concentration (50 to 1000ng/mL). Binding to isolated human serum albumin was 95% to 98%, and 31.6% to 51.1% to human α1-acid glycoprotein . |
| Groups | Approved |
| Therapeutic Class | Other ophthalmic preparations |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lifitegrast 5% ophthalmic solution is used for the treatment of the signs and symptoms of dry eye disease (DED).
Pediatric Use: Safety and efficacy in pediatric patients below the age of 17 years have not been established.
Geriatric Use: No overall differences in safety or effectiveness have been observed between elderly and younger adult patients.
Lifitegrast is also used to associated treatment for these conditions: Dry Eye Syndrome (DES)
How Lifitegrast works
Lifitegrast binds to the integrin lymphocyte function-associated antigen-1 (LFA-1), a cell surface protein found on leukocytes and blocks the interaction of LFA-1 with its cognate ligand intercellular adhesion molecule-1 (ICAM-1). ICAM-1 may be overexpressed in corneal and conjunctival tissues in dry eye disease. LFA-1/ICAM-1 interaction can contribute to the formation of an immunological synapse resulting in T-cell proliferation/activation and migration to target tissues. In vitro studies demonstrated that lifitegrast may inhibit T-cell adhesion to ICAM-1 in a human T-cell line and may inhibit secretion of inflammatory cytokines, inflammatory mediators, chemokines, TNF-α, and IL-1 in human peripheral blood mononuclear cells.
Dosage
Lifitegrast dosage
Instill one drop of Lifitegrast twice daily (approximately 12 hours apart) into each eye. Contact lenses should be removed prior to the administration of Lifitegrast and may be reinserted 15 minutes following administration.
Side Effects
The common adverse effects are instillation site irritation, dysgeusia and reduced visual acuity. Less common are blurred vision, conjunctival hyperemia, headache, increased lacrimation, eye discharge, eye discomfort, eye pruritus and sinusitis.
Toxicity
Some adverse effects in 5-25% of the patients include instillation site irritation, dysgeusia and reduced visual acuity. There is no evidence or reports of potential carcinogenic, mutagenic or fertility-altering effects of this drug.
Precaution
Do not touch the dropper tip to surfaces since this may contaminate the solution. After one month of the opening do not use the medicine of dropper.
Food Interaction
No interactions found.Elimination Route
The mean peak plasma concentration (Cmax) of 1.70ng/mL was reached within 15 minutes of application. Quantifiable trough plasma concentrations ranged from 0.55 ng/mL to 3.74 ng/mL . Observations show limited systemic exposure that produces significant clinical outcomes.
Half Life
Not possible to calculate plasma elimination half-life based on plasma concentrations of lifitegrast, but reported to be relatively short in rat I.V. pharmacokinetics study .
Clearance
Not possible to calculate clearance rate based on plasma concentrations of lifitegrast, but reported to be relatively fast in rat I.V. pharmacokinetics study . It is predicted that lifitegrast is cleared via nasal and subsequently gastrointestinal tract .
Elimination Route
Not possible to perform mass balance study to determine the main route of elimination .
Pregnancy & Breastfeeding use
There are no available data on Lifitegrast use in pregnant women to inform any drug associated risks. There are no data on the presence of Lifitegrast in human milk, the effects on the breastfed infant or the effects on milk production.
Contraindication
Patients who are hypersensitive to this drug or to any ingredient in the formulation or component of the container.
Acute Overdose
There is no information regarding overdose in patients taking Lifitegrast. For management of a suspected drug overdose, contact your ophthalmologist.
Storage Condition
Store in a cool (below 30°C) and dry place, away from light. Keep out of the reach of children.
Innovators Monograph
You find simplified version here Lifitegrast
Lifitegrast contains Lifitegrast see full prescribing information from innovator Lifitegrast Monograph, Lifitegrast MSDS, Lifitegrast FDA label
