brolucizumab intravitreal

Action and Spectrum

Actions and Spectrum: 

Action:  

brolucizumab belongs to a class of medications known as anti-vascular endothelial growth factor (anti-VEGF) drugs. It specifically targets and inhibits vascular endothelial growth factor A (VEGF-A), a protein that plays a critical role in the growth of abnormal blood vessels in the retina. By inhibiting VEGF-A, brolucizumab helps prevent the growth of these abnormal blood vessels, reducing the leakage and bleeding that contribute to the progression of wet AMD. 

Spectrum: 

brolucizumab has a high binding affinity for VEGF-A, allowing it to neutralize this protein effectively. Its mechanism of action makes it highly potent in suppressing the growth and leakage of abnormal blood vessels in the eye. It has been developed to have a longer duration of action compared to some other anti-VEGF drugs, which means it may require less frequent injections for maintenance therapy.

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Hypersensitivity (2%) 

Intraocular inflammation (4%) 

Vitreous detachment (4%) 

Corneal abrasion (2%) 

Eye pain (5%) 

Conjunctivitis (3%) 

Cataract (7%) 

Retinal pigment epithelial tear (3%) 

Vitreous floaters (5%) 

Retinal hemorrhage (4%) 

Conjunctival hemorrhage (6%) 

Blurred vision (10%) 

Intraocular pressure increased (4%) 

Black Box Warning

Black Box Warning: 

None

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: brolucizumab should not be used in individuals who have known hypersensitivity or allergic reactions to the drug or any of its components. Allergic reactions may manifest as itching, rash, swelling, or difficulty breathing. 

Active Ocular Infection: brolucizumab should not be administered in the presence of an active ocular infection. The injection can introduce the infection deeper into the eye, potentially leading to further complications. 

Intraocular Inflammation: If an individual has active intraocular inflammation (e.g., uveitis) in the eye where brolucizumab is to be injected, it may be contraindicated. The medication could exacerbate the inflammation or interfere with its treatment. 

Ocular or Periocular Infection History: Individuals with a history of ocular or periocular infections may require caution when considering brolucizumab treatment. The healthcare provider will assess the risks versus benefits on a case-by-case basis. 

Uncontrolled Glaucoma: brolucizumab has not been studied in patients with uncontrolled glaucoma, so caution is advised in these cases. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: AU TGA pregnancy category D 

US FDA pregnancy category Not Assigned 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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:  

brolucizumab is a pharmaceutical agent employed in the field of ophthalmology for neovascular (wet) age-related macular degeneration (AMD). 

Pharmacodynamics:  

brolucizumab, a monoclonal antibody, exhibits targeted inhibition against vascular endothelial growth factor (VEGF)-A. The vital involvement of VEGF-A in the formation of abnormal blood vessels in the retina, linked to wet AMD, is effectively addressed by this medication. By binding to VEGF-A, brolucizumab prevents it from binding to its receptors on the surface of endothelial cells, thus inhibiting the formation of new blood vessels and reducing vascular permeability.   

Pharmacokinetics: 

Absorption 

drug is administered directly into the vitreous humor of the eye, which allows for rapid absorption into the ocular tissues. Once injected, it starts to distribute within the eye. 

Distribution 

drug distributes within the posterior segment of the eye, particularly in the retina and choroid.  

Metabolism 

The metabolism of drug is not extensive because it is a monoclonal antibody, which means it is a large protein molecule that is typically not broken down by metabolic processes like small molecules. However, some proteolytic degradation may occur over time. 

Excretion and Elimination 

Drug is eliminated from the eye primarily through slow clearance mechanisms. It has a prolonged half-life, allowing for sustained therapeutic effects. 

Adminstartion

Administration:  

Injection procedure: After the eye is properly numbed, the healthcare professional will use a small needle to inject brolucizumab into the vitreous cavity, which is the gel-filled space inside the eye. The injection is usually given through the pars plana, which is the area just outside the colored part of the eye (iris). 

Patient Information Leaflet

Patient information leaflet 

Generic Name: brolucizumab intravitreal 

Why do we use brolucizumab intravitreal?  

Neovascular Age-Related Macular Degeneration (AMD): brolucizumab is primarily used for the treatment of neovascular AMD, a condition characterized by abnormal growth of blood vessels in the macula, the central part of the retina. It is administered by injection into the eye to inhibit the growth of these abnormal blood vessels and prevent further vision loss. 

Visual Acuity Improvement: The drug has demonstrated effectiveness in improving and preserving visual acuity in patients with neovascular AMD. By reducing the growth of abnormal blood vessels and controlling the associated inflammation, it helps prevent damage to the macula, which is responsible for central vision. 

Extended Treatment Intervals: Compared to some other anti-vascular endothelial growth factor (anti-VEGF) treatments for neovascular AMD, brolucizumab offers the advantage of extended treatment intervals. This means that patients may require fewer injections over time, potentially reducing the burden of treatment.