Vizallergol eye drops 0.2% vial 2.5 ml

Olopatadin

Dosage Form:

eye drops 1 ml contains:
active ingredient: olopatadine hydrochloride 2.22 mg (equivalent to 2.0 mg of olopatadin);

excipients: benzalkonium chloride 0.1 mg, povidone K-29/32 18.0 mg, sodium hydrophosphate anhydrous 5.0 mg, sodium chloride 5.5 mg, disodium edetate 0.1 mg, hydrochloric acid and / or sodium hydroxide to pH 7.0, water for injection up to 1 ml. Clear solution from colorless to light yellow color. Antiallergic - H1-histamine receptor blocker

Pharmacodynamics:
Olopatadin is a potent selective anti-allergic / antihistamine drug whose pharmacological effects are developed through several different mechanisms of action. It is an antagonist of histamine (the main mediator of allergic reactions in humans) and prevents histamine-induced release of inflammatory cytokines in the epithelial cells of the conjunctiva. According to the results of in vitro studies it is assumed inhibition of the release of anti-inflammatory mediators by mast conjunctival cells.

In patients with passable nasolacrimal ducts, local use of olopatadine in the form of instillations in the conjunctival sac allowed to reduce the severity of symptoms from the nose, often associated with seasonal allergic conjunctivitis.
Olopatadin has no clinically significant effect on the diameter of the pupil. Suction
Olopatadin undergoes systemic absorption, as well as other drugs intended for topical use. However, plasma concentrations of olopatadin after its topical application in ophthalmology are low and range from a level below the quantitative determination (<0.5 ng / ml) to 1.3 ng / ml. The claimed plasma concentrations are 50–200 times lower than those given by oral administration of therapeutic doses of olopatadin.

Removal
According to pharmacokinetic studies of oral forms of olopatadin, the elimination half-life is from 8 to 12 hours, the drug is eliminated mainly by the kidneys. 60 - 70% of the administered dose is excreted in the urine unchanged, and low concentrations of 2 metabolites, mono-desmethyl and n-oxide, are also detected in the urine.
Due to the fact that olopatadin is excreted by the kidneys mostly unchanged, impaired renal function leads to a change in the pharmacokinetics of olopatadin, leading to a significant (2.3 times) increase in the concentration of olopatadin in patients with severe renal insufficiency (creatinine clearance 13 ml / min)

The concentration of olopatadin in plasma after its topical administration in the form of instillations is 50–200 times lower than with oral administration of therapeutic doses, therefore, there is no need to change the dosing regimen in patients with impaired renal function.
Since the hepatic pathway of elimination is not essential for olopatadine, dose adjustment is not required when used in patients with impaired liver function.
After oral administration of 10 mg of olopatadine by patients on hemodialysis, the concentration of olopatadine in plasma was significantly lower on the day of hemodialysis compared with the days when hemodialysis was not performed. This suggests that elimination of olopatadin using hemodialysis is possible.
According to the results of comparative studies of the pharmacokinetics of the oral dosage form of olopadadine at a concentration of 10 mg in young (mean age 21 years) and elderly patients (average age 74 years), there were no significant differences in plasma concentrations of olopatadin, plasma protein binding and injecting parameters of the drug in unchanged and in the form of metabolites.

Indications and usage

Relief of ocular itching in allergic conjunctivitis.

Contraindications

Hypersensitivity to the drug.
Children age up to 3 years.
Pregnancy and breastfeeding period.
Pregnancy and lactation:
Fertility
Research on the effect of topical olopatadin in ophthalmology on fertilityman was not carried out.

Pregnancy
Information about the local use of olopatadin in ophthalmology in pregnant women is missing or limited. In animal studies, data on the toxic effects of olopatadin on reproductive function in systemic use were obtained. The use of olopatadin during pregnancy and women of childbearing age who do not use contraceptive methods is not recommended.
Excreted olopatadin in breast milk when using the drug in animals. Risk to newborns and infants cannot be excluded. The use of the drug Vizallergol during breastfeeding is not recommended.

Dosage and administration

The drug Vizallergol instilled in 1 drop 1 time a day in the affected eye (s). The duration of the course of therapy, if necessary, can be up to 4 months.
No need to change the dosing regimen in elderly patients.
Use in the pediatric population
The use of Vizallergol is possible in children over 3 years old in the same doses as in adults. The efficacy and safety of olopatadin in children under 3 years of age has not been confirmed.
Use in patients with renal and hepatic failure
The use of olopatadin in the form of eye drops has not been studied in patients with renal or hepatic insufficiency.No dose adjustment is required for the stated category of patients.
Do not touch the tip of the bottle to the eyelids, the skin of the peri-orbital area and other surfaces to avoid microbial contamination of the drug. Tightly close the lid after using the drug.
If necessary, can be used in combination with other drugs for local use in ophthalmology, in this case the interval between their use should be at least 5 minutes.

Adverse reactions

General information about the profile of adverse events
In clinical studies involving 1680 patients, the dosage regimen ranged from 1 to 4 drops per day, the duration of the course of therapy was up to 4 months, the use of olopatadine was carried out both in monotherapy and together with loratadine in a dosage of 10 mg. The overall incidence of adverse events was about 4.5%, while cessation of participation in a clinical study due to the development of adverse reactions was observed only in 1.6% of cases. In clinical studies, no serious adverse events were noted, both from the organ of vision and from the organism as a whole. The most common adverse reaction associated with treatment was pain in the eye, this phenomenon was observed in 0.7% of patients.

Tabular data on adverse events
The following adverse events were observed during clinical trials and post-registration use of the drug and are classified according to the following gradation of the frequency of occurrence of adverse events: very often (> 1/10), often (from> 1/100 to <1/10),infrequently (from> 1 / 1,000 to <1/100), rarely (from> 1 / 10,000 to <1/1000), very rarely (<1 / 10,000), the frequency is unknown (frequency of occurrence cannot be determined based on available data ). Within each group, adverse events are listed in order of severity.

System organ class	Frequency of occurrence	Adverse events
Infectious disorders	Infrequently	Rhinitis
Violations with side of the immune system	Frequency unknown	Hypersensitivity, swelling of the face
Violations nervous system	Often	Headache, dysgeusia
	Infrequently	Dizziness, hypesthesia
	Frequency unknown	Drowsiness
Violations on the part of the organ of vision	Often	Eye pain, eye irritation, syndrome "dry" eyes, unusual sensations in the eye.
	Infrequently	Corneal erosion, corneal epithelium defect, point keratitis, keratitis, accumulation of color pigment in the area of ​​the defect of the cornea with carrying out diagnostic tests, isolation out of sight, photophobia, blurred vision, decreased visual acuity, blepharospasm, discomfort in the eye, itching in the eye, folliculosis conjunctiva conjunctiva, foreign body sensation in the eye, lacrimation, eyelid erythema, eyelid edema, eyelid abnormalities, conjunctival injection.
	Frequency unknown	Corneal edema, conjunctival edema, conjunctivitis, mydriasis, violation of visual functions, crusts on the edges of the eyelids.
Violations from the side respiratory system thoracic organs cells and mediastinum	Often	Dry nose
	Frequency unknown	Dyspnea, sinusitis
Violations from the side gastrointestinal intestinal tract	Frequency unknown	Nausea, vomiting
Violations by skin and subcutaneous adipose tissue	Infrequently	Contact dermatitis, burning sensation of the skin, dry skin.
	Frequency unknown	Dermatitis, erythema.
General violations	Often	Increased fatigue
	Frequency unknown	Asthenia, malaise

In very rare cases, when phosphate-containing drops were used by patients with a concomitant significant corneal damage, corneal calcification developed. There is no information about the development of toxic effects in case of accidental administration of an excess amount of the drug in the conjunctival cavity or in case of accidental ingestion.
With the development of an overdose if accidentally swallowed, treatment is symptomatic. Studies of the interaction of olopatadin with other drugs have not been conducted.
In vitro studies have demonstrated the absence of inhibition of metabolic reactions mediated by the 1A2, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4 cytochrome P-450 isoenzymes.
According to the obtained results, the likelihood of olopatadin entering into metabolic reactions when used together with other drugs is estimated as low. Olopatadina hydrochloride is an antiallergic / antihistamine preparation for topical use in ophthalmology, and, despite topical application, can be absorbed into the systemic circulation. With the appearance of pronounced hypersensitivity reactions should discontinue use of the drug.
Vizallergol should not be used to relieve conjunctival injection caused by the use of contact lenses.
The drug contains benzalkoniya chloride, which can be adsorbed by soft contact lenses and cause eye irritation. It is necessary to remove contact lenses before instillation and install again no earlier than 15 minutes after instillation of the drug.
According to several studies, benzalkonium chloride can provoke the development of punctate keratopathy and / or toxic ulcerative keratopathy.
Requires careful monitoring of the condition of the eyes of patients with frequent or long-term use of Vizallergol with the accompanying syndrome of "dry" eyes, as well as corneal lesions. Vizallergol does not have a significant impact on the ability to drive vehicles, machinery. If there is a blurred vision immediately after instillation, it is necessary to refrain from driving vehicles and mechanisms until the clarity of visual perception is restored.
Form release / dosage:
Eye drops, 0.2%.
Packaging:
On 2,5 ml in a polyethylene bottle with a stopper dropper and the screwing up cap with control of first opening.
On 1 bottle with the application instruction in a cardboard pack.
Storage conditions:
Store at a temperature of from 2 to 25 ° C.

Do not freeze.
Keep out of the reach of children.
Shelf life:
2 years.

Drops to use within 28 days after opening the bottle.

Do not use after the expiration date printed on the package.