lifitegrast ophthalmic

Action and Spectrum

Actions and Spectrum: 

lifitegrast ophthalmic, sold under Xiidra, is a medication used to treat dry eye disease. It generally belongs to a class of drugs called lymphocyte function-associated antigen-1 (LFA-1) antagonists. Here’s some information about the action and spectrum of lifitegrast ophthalmic: 

Action: lifitegrast acts as a selective LFA-1 antagonist. LFA-1 is a cell surface protein generally found on leukocytes (white blood cells) and plays a role in the inflammatory response. By blocking the interaction between LFA-1 and its ligands, lifitegrast inhibits the activation and migration of inflammatory cells into the ocular surface tissues. This helps to reduce the inflammation associated with dry eye disease. 

Spectrum: lifitegrast ophthalmic is specifically indicated for treating signs, symptoms of dry eye disease in adult patients. Dry eye disease is characterized by insufficient moisture and lubrication on the eye’s surface, leading to discomfort, irritation, and visual disturbances. lifitegrast helps to alleviate these symptoms by reducing inflammation and promoting the natural production of tears. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Dysgeusia (5-25%) 

Instillation site irritation (5-25%) 

Reduced visual acuity (5-25%) 

1-10% 

Eye irritation (1-5%) 

Sinusitis (1-5%) 

Eye pruritus (1-5%) 

Blurred vision (1-5%) 

Conjunctival hyperemia (1-5%) 

Headache (1-5%) 

Eye discomfort (1-5%) 

Increased lacrimation (1-5%) 

Eye discharge (1-5%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

lifitegrast ophthalmic (Xiidra) has specific contraindications that should be considered before use. The contraindications of lifitegrast ophthalmic include: 

• Hypersensitivity: lifitegrast should not be used in individuals with known hypersensitivity or allergic reactions to lifitegrast or any of its components. Allergic reactions can range from mild skin reactions to more severe reactions, like difficulty breathing/anaphylaxis. 

It’s important to note that contraindications may vary depending on factors such as the individual’s medical history, current medications, and specific conditions. It’s always advisable to meet with a healthcare professional or refer to the prescribing information for the most accurate and up-to-date contraindications associated with lifitegrast ophthalmic. 

Caution 

When using lifitegrast ophthalmic (Xiidra), some cautions should be considered. These cautions include: 

• Ocular Effects: lifitegrast ophthalmic may cause temporary blurred vision upon instillation. Therefore, patients should exercise caution while driving or operating machinery until their vision clears. 
• Contact Lenses: It should be removed before administering lifitegrast ophthalmic. Patients can reinsert their contact lenses 15 minutes after using the eye drops. 
• Eye Infections: lifitegrast ophthalmic is not recommended in patients with active eye infections. Patients should discontinue lifitegrast and consult their healthcare provider for appropriate treatment if an eye infection develops during treatment. 
• Pregnancy and Lactation: Safety and efficacy of lifitegrast ophthalmic have not been established in pregnant or breastfeeding women. It’s advisable to consult a healthcare professional before using lifitegrast if you are pregnant, planning to become pregnant, or breastfeeding. 
• Pediatric Use: The safety and effectiveness of lifitegrast ophthalmic have not been established in pediatric patients. Its use in children below 17 years of age is not recommended. 

Pregnancy / Lactation

Pregnancy consideration:  

AU TGA pregnancy category: B1
US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk is Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

lifitegrast ophthalmic (Xiidra) has a specific pharmacological profile influencing its therapeutic effects in treating dry eye disease. Here’s an overview of the pharmacology of lifitegrast: 

lifitegrast is a lymphocyte function-associated antigen-1 antagonist. LFA-1 is a cell surface protein generally found on leukocytes (white blood cells) and plays a role in the inflammatory response.

By blocking the interaction between LFA-1 and its ligands, mainly intracellular adhesion molecule-1 (ICAM-1), lifitegrast inhibits the activation and also migration of inflammatory cells into the ocular surface tissues. This helps to reduce the inflammation associated with dry eye disease. 

Pharmacodynamics: 

Mechanism of action: lifitegrast ophthalmic (Xiidra) exerts its therapeutic effects through its mechanism of action, which involves the modulation of inflammatory pathways within the ocular surface tissues. Here’s a detailed explanation of the mechanism of action: 

lifitegrast is a small-molecule lymphocyte function-associated antigen-1 antagonist. LFA-1 is a cell surface protein generally found on leukocytes (white blood cells) and plays a crucial role in the immune response. It is involved in leukocyte adhesion, activation, and migration. 

In dry eye disease, the ocular surface tissues have chronic inflammation and immune activation. This inflammation can lead to ocular discomfort, dryness, redness, and other symptoms associated with the condition. lifitegrast targets this inflammation by inhibiting the interaction between LFA-1 and its ligand, intracellular adhesion molecule-1 (ICAM-1). 

By binding to ICAM-1, lifitegrast blocks the activation and migration of inflammatory cells, such as T cells, into the ocular surface tissues. This inhibition reduces the local immune response and inflammation, which is characteristic of dry eye disease. Lifitegrast’s anti-inflammatory effects help alleviate the signs and symptoms of dry eye disease, including discomfort, dryness, redness, and irritation. 

Furthermore, lifitegrast has been shown to promote the secretion of tear film components, such as mucin and water, by goblet cells, which further aids in improving ocular surface lubrication and relieving dry eye symptoms. 

Overall, the mechanism of action of lifitegrast involves inhibiting the LFA-1/ICAM-1 interaction, reducing the migration of inflammatory cells, and modulating the immune response within the ocular surface tissues. By targeting these inflammatory pathways, lifitegrast helps to alleviate the signs and symptoms associated with dry eye disease. 

Pharmacokinetics: 

Absorption 

lifitegrast is administered as an ophthalmic solution for topical use in the eye. After application, it is expected to be absorbed through the ocular surface. However, the systemic absorption of lifitegrast following ocular administration is low, resulting in minimal systemic exposure. 

Distribution 

lifitegrast is primarily intended to act locally on the ocular tissues. Limited information is available regarding its distribution in the body. Based on its action and intended use, the distribution of lifitegrast beyond the ocular tissues is expected to be minimal. 

Metabolism 

The metabolism of lifitegrast needs to be better characterized. Although, based on available information, it is likely that lifitegrast undergoes minimal to no significant metabolism. Extensive metabolic processes are not anticipated since it is primarily administered topically and has low systemic exposure. 

Elimination and Excretion 

Details regarding the excretion of lifitegrast are limited. Due to its low systemic exposure, lifitegrast is expected to be eliminated primarily through local clearance from the ocular tissues. It is unlikely to undergo significant renal or hepatic excretion. 

Adminstartion

Administration: 

Ophthalmic administration 

lifitegrast ophthalmic (Xiidra) is typically administered as eye drops. Here are the general guidelines for the administration of lifitegrast: 

• Before using lifitegrast, wash your hands thoroughly with soap and water. 
• Shake the lifitegrast eye drop bottle gently before each use to ensure proper medication mixing. 
• Tilt your head back gently and look up. 
• Gently pull down lower eyelid to create a small pocket. 
• Hold the dropper tip close to your eye without touching it, and carefully squeeze the bottle to instill one drop into the pocket formed by the lower eyelid. Avoid blinking or squeezing your eyelids tightly. 
• After instilling the drop, gently release the lower eyelid and close your eyes. Keep your eyes closed for a small time period to allow the medication to spread across the eye’s surface. 
• If you must administer another drop, wait at least 5 minutes before repeating the process. 
• If you are using other eye medications, wait at least five minutes between applying each medication to allow sufficient time for absorption. 
• Replace the cap tightly on the lifitegrast bottle immediately after use. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: lifitegrast ophthalmic 

Pronounced: [ LIF-e-TEG-rast-off-THAL-mik ] 

Why do we use lifitegrast ophthalmic? 

lifitegrast ophthalmic (Xiidra) is primarily used to treat dry eye disease, a condition characterized by insufficient moisture and lubrication on the eye’s surface. lifitegrast helps to alleviate the signs and symptoms of dry eye disease, which may include: 

• Eye discomfort: lifitegrast can help reduce the discomfort associated with dry eyes, such as a gritty or foreign body sensation. 
• Dryness: It helps to increase tear production and improve the lubrication of the eyes, relieving the sensation of dryness. 
• Redness: lifitegrast can help reduce the redness and inflammation of the eyes that may occur with dry eye disease. 
• Irritation: It can alleviate the irritation and itching sensations caused by dry eyes. 
• Blurred vision: lifitegrast may help to improve visual clarity by reducing the dryness-related blurring of vision. 

It’s important to note that lifitegrast ophthalmic is intended for use in adults. The specific dosage and duration of treatment may vary depending on the individual’s condition and their healthcare provider’s recommendation. lifitegrast ophthalmic is available by prescription only, and it’s key to follow the instructions provided by your healthcare professional for its proper use.