ranibizumab intravitreal implant

Action and Spectrum

Actions and Spectrum: 

Action: 

ranibizumab functions as an anti-vascular endothelial growth factor (anti-VEGF) agent, specifically targeting the VEGF-A isoform. By binding to VEGF-A, ranibizumab inhibits the activation of VEGF receptors, thereby preventing the growth and leakage of abnormal blood vessels within the retina.  

Spectrum: 

ranibizumab intravitreal implant exhibits a broad spectrum of activity due to its ability to neutralize VEGF-A. By targeting the primary mediator of abnormal angiogenesis and vascular permeability, drug exerts its therapeutic effect on multiple retinal diseases. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10% 

Iritis (23%) 

Conjunctival hemorrhage (72%) 

Conjunctival hyperemia (26%) 

1-10% 

Corneal edema (4%) 

Vitreous detachment (6%) 

Corneal abrasion (4%) 

Conjunctival edema (5%) 

Headache (7%) 

Vitreous floaters (9%) 

Corneal disorder (4%) 

Foreign body sensation in eyes (7%) 

Eye pain (10%) 

Vitreous hemorrhage (5%) 

Conjunctival bleb/ filtering bleb leak (9%) 

Hypotony of eye (6%) 

Black Box Warning

Black Box Warning:  

Endophthalmitis 

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: ranibizumab is contraindicated in individuals who have a known hypersensitivity or allergy to ranibizumab or any of its components. 

Ocular Infections: The use of drug is contraindicated in individuals with active ocular or periocular infections, such as bacterial, viral, or fungal infections. Treating the underlying infection should take priority before initiating ranibizumab therapy. 

Uncontrolled Glaucoma: Individuals with uncontrolled glaucoma (high intraocular pressure) may be at an increased risk of adverse events when receiving ranibizumab. It is advisable to stabilize glaucoma before considering treatment with ranibizumab. 

Pediatric Use: The safety and efficacy of ranibizumab have not been established in pediatric patients, and its use in this population is limited. 

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:  

ranibizumab intravitreal implant is a novel pharmacological agent designed for the treatment of various retinal diseases. 

Pharmacodynamics:  

ranibizumab intravitreal implant exerts its therapeutic effects through the inhibition of vascular endothelial growth factor (VEGF). VEGF is a crucial protein involved in angiogenesis and vascular permeability, which are pathological processes contributing to retinal diseases such as neovascular age-related macular degeneration (nAMD).

The implant releases a sustained and controlled amount of ranibizumab, a monoclonal antibody fragment that binds specifically to VEGF-A isoforms, preventing their interaction with VEGF receptors. By neutralizing VEGF-A, ranibizumab inhibits abnormal blood vessel growth and leakage, thereby preserving and improving visual function.   

Pharmacokinetics: 

Absorption 

Upon administration of the ranibizumab intravitreal implant, ranibizumab is released into the vitreous humor, from which it is absorbed by the surrounding retinal tissue.  

Distribution 

Following absorption, ranibizumab is distributed within the retinal layers, where it acts on specific molecular targets involved in retinal diseases. The high molecular weight and hydrophilic nature of ranibizumab limit its systemic distribution, minimizing the potential for off-target effects. 

Metabolism 

ranibizumab is a monoclonal antibody fragment that undergoes proteolytic degradation within the retinal tissue. The precise metabolic pathways involved in the degradation of ranibizumab intravitreal implant are not fully elucidated, but it is likely mediated by retinal enzymes. 

Excretion and Elimination 

As ranibizumab is primarily localized within the retinal tissue, its elimination occurs through gradual clearance from the vitreous humor. The exact mechanisms and kinetics of ranibizumab excretion are yet to be determined. 

Adminstartion

Administration:  

ranibizumab is typically administered as an intravitreal injection, where a small amount of the medication is directly injected into the vitreous cavity of the eye. The injection is usually performed by a healthcare professional, such as an ophthalmologist, in a clinical setting. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: ranibizumab intravitreal implant 

Why do we use ranibizumab intravitreal implant?  

Diabetic Macular Edema (DME): ranibizumab intravitreal implant exhibits robust anti-VEGF effects, promoting the resolution of macular edema and enhancing visual acuity. The implant’s sustained-release mechanism offers the advantage of reducing treatment frequency and the associated burden of intravitreal injections.  

Macular Edema Secondary to Retinal Vein Occlusion (RVO): ranibizumab intravitreal implant has demonstrated favorable outcomes in treating macular edema secondary to RVO. By inhibiting VEGF activity, the implant effectively reduces retinal thickness and improves visual acuity. This treatment modality has proven to be particularly beneficial in cases resistant to conventional therapy, providing an alternative option for patients with persistent macular edema. 

Choroidal Neovascularization (CNV) Associated with Pathologic Myopia: Pathologic myopia is frequently associated with CNV, leading to severe visual impairment. ranibizumab intravitreal implant has exhibited significant therapeutic efficacy in managing CNV associated with pathologic myopia, improving visual outcomes and preventing disease progression. The sustained-release implant offers a promising approach for long-term treatment in these cases.