Ranibizumab

Pronunciation: (RA-ni-BIZ-oo-mab)
Class: Selective vascular endothelial growth factor antagonist

Trade Names

Lucentis
- Injection, intravitreal 10 mg/mL

Pharmacology

Binds to and inhibits the biologic activity of human vascular endothelial growth factor A (VEGF-A), reducing endothelial cell proliferation, vascular leakage, and new blood vessel formation.

Pharmacokinetics

Absorption

C _max is below the concentration thought necessary to inhibit biological activity of VEGF-A by 50% (0.3 to 2.36 ng/mL). T _max is 24 h.

Elimination

Vitreous elimination half-life was approximately 9 days.

Special Populations

Renal Function Impairment

No studies have been conducted.

Hepatic Function Impairment

No studies have been conducted.

Indications and Usage

Treatment of neovascular (wet) age-related macular degeneration and macular edema following retinal vein occlusion.

Contraindications

Ocular or periocular infection; hypersensitivity to any component of the product.

Dosage and Administration

Adults

Intravitreal 0.5 mg (0.05 mL) once per month (approximately 28 days).

General Advice

• For ophthalmic intravitreal injection only.
• Withdraw 0.2 mL through a 5-micron 19-gauge filter needle attached to a 1 mL tuberculin syringe.
• Replace filter needle with a 30-gauge × 1/ 2 -inch needle for intravitreal injection.
• Expel contents until the plunger tip is aligned with the 0.05 mL mark on the syringe.
• Prior to the injection, give adequate anesthesia and broad-spectrum microbicide.
• Perform the intravitreal injection procedure under aseptic conditions, including use of sterile gloves, sterile drape, and a sterile eyelid speculum.
• Use each vial for the treatment of a single eye.

Storage/Stability

Store at 36° to 46°F. Do not freeze. Protect from light. Store in original carton until use.

Drug Interactions

None well documented.

Adverse Reactions

Cardiovascular

Atrial fibrillation (5%); arterial thromboembolic events (3%).

CNS

Headache (12%); insomnia (5%); anxiety (4%).

EENT

Conjunctival hemorrhage (74%); eye pain (35%); vitreous floaters (27%); increased IOP (24%); vitreous detachment (21%); intraocular inflammation, visual disturbance or vision blurred (18%); cataract (17%); foreign body sensation in eye (16%); eye irritation (15%); increased lacrimation (14%); blepharitis, dry eye, eye pruritus (12%); maculopathy, ocular hyperemia (11%); retinal disorder (10%); retinal degeneration (8%); conjunctival hyperemia, ocular discomfort, posterior capsule opacification (7%); injection-site hemorrhage (5%).

GI

Nausea (9%); gastroenteritis viral (4%).

Musculoskeletal

Arthralgia (11%); pain in extremity (5%).

Respiratory

Nasopharyngitis (16%); bronchitis (11%); cough, upper respiratory tract infection (9%); sinusitis (8%); COPD (6%); dyspnea (4%).

Miscellaneous

UTI (9%); anemia (8%); influenza (7%); hypercholesterolemia (5%).

Precautions

Monitor Monitor IOP and for endophthalmitis. Monitoring may consist of a check for perfusion of the optic nerve head immediately after the injection and tonometry within 30 min following the injection. Monitor patients during the week following the injection to permit early treatment in case an infection occurs. Monitor IOP as well as the perfusion of the optic nerve head.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Hypersensitivity

May occur and manifest as ocular inflammation.

Endophthalmitis and retinal detachments

May occur.

Increased IOP

May occur within 60 min of intravitreal injection.

Thromboembolic events

Arterial thromboembolic events (eg, nonfatal MI, nonfatal stroke, vascular death) may occur.

Overdosage

Symptoms

Intraocular inflammation.

Patient Information

• Advise patient to seek immediate care from an ophthalmologist if the eye becomes red, sensitive to light, or painful, or if the patient develops a change in vision.

Copyright © 2009 Wolters Kluwer Health.