Oloridin eye drops 0.1% vial, 5ml

Composition

Per 1 ml:

Active ingredient:

Olopatadine hydrochloride – 1.11 mg in terms of olopatadine 1.0 mg

Auxiliary substances:

Benzalkonium chloride-0.1 mg

Sodium Hydrophosphate Dihydrate-6.0 mg

Sodium chloride-6.0 mg

of hydrochloric acid solution of 5 M or sodium hydroxide solution of 1 M – up to pH 7.0-7.2 Water for injection up to 1 ml

Pharmacological action

Pharmacotherapy group: Anti-allergic agent-H 1-histamine receptor blocker. ATX Code: S01GX09 Pharmacological Properties Pharmacodynamics

Olopatadine is a potent, selective anti-allergic / antihistamine drug whose pharmacological effects develop through several different mechanisms of action.

It is an antagonist of histamine (the main mediator of allergic reactions in humans) and prevents the histamine-induced release of inflammatory cytokines in conjunctival epithelial cells.

The results of in vitro studies suggest inhibition of the release of pro-inflammatory mediators by conjunctival mast cells.

In patients with passable nasolacrimal ducts, topical application of olopatadine in the form of instillations into the conjunctival sac reduced the severity of nasal symptoms often associated with seasonal allergic conjunctivitis.

Olopatadine has no clinically significant effect on pupil diameter.

Pharmacokinetics

Suction

Olopatadine undergoes systemic absorption, like other drugs intended for topical use. However, plasma concentrations of olopatadine after topical application in ophthalmology are low and range from below the level of quantitative determination ( The claimed plasma concentrations are 50-200 times lower than those with oral therapeutic doses of olopatadine.

Deduction

According to pharmacokinetic studies of oral forms of olopatadine, the half-life is from 8 to 12 hours, the drug is excreted mainly by the kidneys. 60-70% of the administered dose is excreted unchanged in the urine, and low concentrations of 2 metabolites – mono-desmethyl and n-oxide-are also detected in the urine.

Due to the fact that olopatadine is mainly excreted unchanged by the kidneys, impaired renal function leads to a change in the pharmacokinetics of olopatadine, leading to a significant (2.3 times) increase in the concentration of olopatadine in plasma in patients with severe renal insufficiency (creatinine clearance 13 ml/min). Due to the fact that the concentration of olopatadine in plasma after its topical application in the form of instillations is 50-200 times lower than with oral use of therapeutic doses, there is no need to change the dosage regimen in elderly patients with impaired renal function. Since the hepatic elimination pathway is not the primary route for olopatadine, no dose adjustment is required when used in patients with impaired liver function.

After oral use of 10 mg of olopatadine to patients on hemodialysis, the plasma concentration of olopatadine was significantly lower on the day of hemodialysis compared to days when hemodialysis was not performed. This indicates that the elimination of olopatadine by hemodialysis is possible.

According to the results of comparative studies of the pharmacokinetics of the oral dosage form of olopatadine at a concentration of 10 mg in young (mean age 21 years) and elderly patients (mean age 74 years), there were no significant differences in plasma concentrations of olopatadine, plasma protein binding, and excretion parameters in unchanged form and in the form of metabolites.

Indications

Treatment of seasonal allergic conjunctivitis symptoms.

Use during pregnancy and lactation

Fertility

Studies on the effect of topical application of olopatadine in ophthalmology on human fertility have not been conducted.

Pregnancy

Information on topical use of olopatadine in ophthalmology in pregnant women is not available or limited. In animal studies, data have been obtained on the toxic effect of olopatadine on reproductive function with systemic use. It is not recommended to use olopatadine during pregnancy and women of childbearing age who do not use contraceptive methods.

Breast-feeding period

The excretion of olopatadine in breast milk was noted when using the drug in animals. The risk for newborns and children cannot be excluded. It is not recommended to use the drug during breastfeeding

Contraindications

Hypersensitivity to the components of the drug, pregnancy and lactation, age up to 3 years.

With caution

In patients with concomitant dry eye syndrome and corneal diseases.

Side effects

General information about the adverse event profile

In clinical trials involving 1,680 patients, the dosage regimen ranged from 1 to 4 drops per day, the duration of therapy was up to 4 months, and olopatadine was used both in monotherapy and in combination with loratadine at a dosage of 10 mg. The overall incidence of adverse events was about 4.5%, while discontinuation of participation in the clinical trial due to the development of adverse reactions was observed only in 1.6% of cases. In the course of clinical studies, no adverse events were observed either on the part of the visual organ or on the part of the body as a whole. The most common treatment-related adverse reaction was eye discomfort, which was reported in 0.7% of patients.

Tabular data about undesirable events

The following adverse events were reported during clinical trials and post-marketing use of the drug and are classified according to the following gradation of the frequency of adverse events: very common (≥ 1/10), common (≥ 1/100, < 1/10), infrequent (≥ 1/1000, < 100), rare (≥ 1/10000, < 1/1000), very rare ( Within each group, adverse events are listed in order of decreasing severity.

In very rare cases, patients with concomitant significant corneal damage have developed corneal calcification when using phosphate – containing drops.

Interaction

Interaction studies of olopatadine with other drugs have not been conducted.

In vitro studies have demonstrated the absence of inhibition of metabolic reactions mediated by cytochrome P 450 isoenzymes 1A2,2C8,2C9,2C19,2D6,2E1AND 3A4. According to the results obtained, the probability of olopatadine entering into metabolic reactions when co-administered with other drugs is estimated as low.

How to take, course of use and dosage

Locally.

Instill 1 drop of the solution into the conjunctival sac of the affected eye 2 times a day (with an interval of 8 hours).

The duration of treatment is up to four months.

If necessary, the drug can be used in combination with other drugs. In this case, the interval between their use should be at least 5 minutes.

Elderly people

There is no need to adjust the dosage for elderly patients.

Children from 3 years of age

The drug can be used in the same doses as in adults.

Kidney or liver failure

No studies have been conducted in patients with renal or hepatic insufficiency regarding the use of olopatadine in the form of eye drops. However, no dose adjustment is expected to be necessary in patients with renal or hepatic insufficiency.

Overdose

There are no data on the development of toxic effects in case of accidental introduction of an excessive amount of the drug into the conjunctival cavity or in case of accidental ingestion, treatment should be supportive.

Description

Clear, colorless or slightly yellowish solution.

Special instructions

Olopatadine hydrochloride is an anti-allergic/antihistamine drug for topical use in ophthalmology, and, despite topical use, can be absorbed into the systemic circulation. If severe hypersensitivity reactions occur, the drug should be discontinued. The drug contains benzalkonium chloride, which can cause eye irritation and discolor soft contact lenses. Contact with soft contact lenses should be avoided. Patients should be instructed to remove their contact lenses before applying the drug and replace them no earlier than 15 minutes after instillation of the drug.

With frequent or prolonged use of the drug, benzalkonium chloride can cause the appearance of pinpoint keratitis or toxic ulcerative keratopathy in patients with dry eye syndrome or corneal pathology.

Effect on the ability to drive vehicles and mechanisms Olopatadine does not significantly affect the ability to drive vehicles and mechanisms. If blurred vision is observed immediately after instillation, it is necessary to wait for the restoration of clear visual perception before driving vehicles and mechanisms.

Form of production

Eye drops 0.1%.

Storage conditions

At a temperature not exceeding 30 °C. Keep out of reach of children.

Shelf

life is 3 years. After opening the bottle – 1 month.

Do not use after the expiration date!

Active ingredient

Olopatadine

Conditions of release from pharmacies

By prescription

Dosage form

eye drops