Raniʙizumaʙ
When ATH:
S01LA04
Pharmacological action
The drug for the treatment of exudative-hemorrhagic form of age-related macular degeneration (SHC). Ranibizumab is a human monoclonal fragment antibodies to endothelial growth factor A (VEGF-A) and is expressed by a recombinant Escherichia coli strain.
Ranibizumab binds selectively to isoforms of vascular endothelial growth factor, VEGF-А (VEGF110, VEGF121, VEGF165), and prevents the interaction of VEGF-A to its receptors on the surface of endothelial cells (Victory1and VEGR2), which leads to a suppression of neovascularization and vascular proliferation. Inhibiting the growth of new vessels in the retina, choroid, ranibizumab stops the progression of exudative-hemorrhagic form of age-related macular degeneration (SHC).
Pharmacokinetics
When administered intravitreally ranibizumab (1 times / month) patients with neovascular AMD Cmax ranibizumab in plasma was low and insufficient to inhibit the biological activity of VEGF-A in 50% (11 -27 ng / ml according to studies of cell proliferation in vitro). With the drug into the vitreous in the dose range of 0.05 to 1.0 mg Cmax ranibizumab in plasma was proportional to the dosage.
According to the results of pharmacokinetic analysis and in view of the elimination of ranibizumab average plasma T1/2 (at an application rate 0.5 mg) vitreous averaged about 9 days.
When administered intravitreally (1 once a month) FROMmax ranibizumab plasma levels achieved during the days after injection, and is in the range 0.79-2.90 ng / ml. FROMmin ranibizumab plasma ranges 0.07-0.49 ng / ml. Concentration in serum ranibizumab approximately 90 000 times lower than that of the vitreous body.
Testimony
Neovascular (wet) form of age-related macular degeneration in adults.
Dosage regimen
Ranibizumab applied only by injection into the vitreous body.
The recommended dose of ranibizumab 0.5 mg (0.05 ml) 1 times / month as intravitreal injection.
The first three injections of ranibizumab operate with frequency 1 X / mo consecutively for 3 months, then drug treatment is stopped (the stabilization phase) regularly (no less 1 times / month) check visual acuity. By reducing the visual acuity over 5 letters ETDRS scale (1 line on the Snellen table) ranibizumab treatment is resumed.
Between the introduction of two doses of the drug should be observed interval of at least 1 Months. Before the introduction of ranibizumab should control the quality and color of the dissolution solution. The drug should not be used when changing the color of the solution and the appearance of insoluble visible particles.
Side effect
The study of the safety of the drug was carried out in the course of clinical trials in 1315 patients for 2 years.
Serious adverse events, related to the procedure of administration, included endophthalmitis, rhegmatogenous retinal detachment and cataract due to iatrogenic injury. Other serious adverse events from the eyes, observed at primeneniiranibizumaba, included intraocular inflammation and increased intraocular pressure.
The following adverse events (possibly related to the use of the drug) occurred at a frequency of at least 2% patients, received a dose of ranibizumab 0.5 mg, compared with the control group (simulation of injection or photodynamic therapy).
The incidence of adverse events was estimated as follows:: arise very often (≥1/10), often (≥1/100; <1/10), sometimes (≥1/1000; <1/100), rarely (≥1/10 000; <1/1000), rarely (<1/10 000).
Infections and infestations: Often – nazofaringit; often – flu.
From the hematopoietic system: often – anemia.
CNS: Often – headache; often – alarm.
On the part of the organ of vision: Often – intraocular inflammation, inflammation vitreous, vitreous detachment, retinal hemorrhage, visual impairment, sore eyes, turbidity in the vitreous, increased intraocular pressure, conjunctival hemorrhage, eye irritation, foreign body sensation in the eye, lacrimation, .Aloe, dry eye syndrome, red eyes, itching sensation in the eyes; often – degenerative changes of the retina, retinal damage, retinal disinsertion, retinal tears, detachment of the retinal pigment epithelium, gap pigment epithelium, reduced visual acuity, vitreous hemorrhage, the defeat of the vitreous, uveitis, Irit, iridocyclitis, Cataract, subkapsulyarnaya cataracts, PCO lens, punctate keratitis, corneal erosion, Opalescence cell in the anterior chamber, blurred vision, hemorrhage at the injection site, eye hemorrhage, conjunctivitis, allergic conjunctivitis, discharge from the eyes, photopsia, photophobia, discomfort in the eyes, swelling of the eyelids, soreness century, conjunctival hyperemia; sometimes – blindness, endophthalmitis, gipopion, gifema, keratopathy, adhesions of the iris, deposition in the cornea, corneal edema, corneal striae, pain or irritation at the injection site, abnormal sensation in the eye and irritation century.
The respiratory system: often – cough.
From the digestive system: often – nausea.
Allergic reactions: often – rash, hives, itch.
On the part of the musculoskeletal system: Often – artralgii.
Contraindications
Confirmed or suspected eye infection or infectious processes periocular localization;
Intraocular inflammation;
Children and teens under 18 years (the efficacy and safety of the drug in these patients has not been studied);
Pregnancy;
Lactation;
Hypersensitivity to ranibizumab or any other component of the drug.
Precautions should be administered to patients with known history of hypersensitivity (Only after careful assessment of risk / benefit ratio).
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation (breast-feeding).
During the therapy with women of childbearing age should use reliable methods of contraception.
Cautions
Conduct ranibizumab treatment should only ophthalmologist, having experience in intravitreal injections.
Introduction ranibizumab should always be carried out under aseptic conditions. Besides, during 1 weeks after the injection of the drug should be monitored for patients with a view to identifying possible local infection and timely treatment of. Should inform patients about the need to immediately tell your doctor about all the symptoms, which may indicate the development of endophthalmitis.
When injected into the vitreous inhibitors endothelial growth factor A (VEGF-A) theoretically may develop arterial thromboembolic events. However, in clinical studies in patients, treated with ranibizumab, incidence of thromboembolic events was low and similar to that in the control group.
Effects on ability to drive vehicles and management mechanisms
Against the background of ranibizumab may develop temporary visual impairment, adversely affect the ability to drive vehicles and use machines. If you experience symptoms such patients should not drive vehicles or operate machinery to reduce the severity of temporary visual impairment.
Drug Interactions
Interaction of ranibizumab with other drugs has not been studied.
Ranibizumab should not be mixed with any other drugs or solvents.
