Instructions for use Olopatadine Unimed Pharma eye drops solution 1 mg/ml dropper bottle 5 ml
Composition
active ingredient: olopatadine;
1 ml of solution contains olopatadine hydrochloride 1.11 mg equivalent to olopatadine 1.00 mg;
1 ml contains 30 drops;
Excipients: sodium chloride, sodium hydrogen phosphate dodecahydrate, hydrochloric acid or sodium hydroxide, water for injection.
Dosage form
Eye drops, solution.
Main physicochemical properties: transparent, colorless solution without visible mechanical particles.
Pharmacotherapeutic group
Means for use in ophthalmology. Antiedematous and antiallergic agents. ATX code S01G X09.
Pharmacological properties
Pharmacodynamics.
Olopatadine is a potent, selective antiallergic/antihistamine with several distinct mechanisms of action. It antagonizes the release of histamine (a major mediator of allergic reactions in humans) and prevents histamine-induced cytokine production by human conjunctival epithelial cells. In vitro data indicate that the drug acts on human conjunctival mast cells to inhibit the release of inflammatory mediators. Topical ophthalmic administration of the drug to patients with intact nasolacrimal ducts has been shown to reduce the nasal signs and symptoms that often accompany seasonal allergic conjunctivitis. The drug does not cause clinically significant changes in pupil diameter.
No hazard to humans was revealed based on conventional studies of safety, pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential and reproductive toxicity.
Developmental delay has been shown in pups of lactating rats given systemic doses of olopatadine at doses exceeding the maximum recommended human ophthalmic dose. Olopatadine has been detected in the milk of lactating rats following oral administration.
Pharmacokinetics.
Olopatadine is absorbed systemically, like other topical drugs. However, with topical application of olopatadine, systemic absorption is minimal and plasma concentrations are below the level of quantification (<0.5 ng/mL) to 1.3 ng/mL. These concentrations are 50- to 200-fold lower than those achieved with oral administration at well-tolerated doses.
The plasma half-life of olopatadine after oral administration is approximately 8–12 hours, and the drug is excreted primarily by the kidneys. Approximately 60–70% of the dose was recovered in the urine as the active substance. Two metabolites, mono-desmethyl and N-oxide, were detected in the urine at low concentrations.
Since olopatadine is excreted in the urine, mainly as unchanged active substance, the pharmacokinetics of olopatadine are altered in renal impairment, peak plasma concentrations in patients with severe renal insufficiency (mean creatinine clearance 13 ml/min) being 2-3 times higher than in healthy adult volunteers. In patients undergoing hemodialysis after oral administration of 10 mg, plasma olopatadine concentrations were significantly lower on hemodialysis days than on non-hemodialysis days, suggesting that olopatadine was eliminated during hemodialysis.
When a 10 mg oral dose was administered to young and elderly subjects, no significant differences in plasma concentrations, protein binding, or urinary excretion of unchanged drug and metabolites were observed.
When administered orally to patients with severe renal impairment, somewhat higher plasma concentrations can be expected. Since plasma concentrations after topical ophthalmic administration of olopatadine are 50-200 times lower than after oral administration at well-tolerated doses, no dosage adjustment is necessary for the elderly or patients with renal impairment. Hepatic metabolism is not a major route of elimination. Therefore, no dosage adjustment is necessary for patients with hepatic impairment.
Indication
Treatment of seasonal allergic conjunctivitis.
Contraindication
Hypersensitivity to the active substance or to other components of the drug.
Interaction with other medicinal products and other types of interactions
No studies have been conducted to study the interaction of the drug with other drugs.
In vitro studies have shown that olopatadine does not inhibit the metabolic reactions of cytochrome P450 isoenzymes 1A2, 2C8, 2C9, 2C19, 2D6, 2E1 and 3A4. Olopatadine does not cause metabolic interactions with other active substances when used concomitantly.
Application features
Patients with a history of contact hypersensitivity to silver should not use this medicinal product, as the dispersed drops may contain traces of silver from the bottle cap.
Contact lens users
Before using the drug, it is necessary to remove soft contact lenses and reinstall them 15 minutes after instillation.
Use during pregnancy or breastfeeding
Pregnancy.
There are no or limited ophthalmic data on the use of olopatadine in pregnant women. Reproductive toxicity has been shown in animals after systemic administration (see section 5.1). Olopatadine is not recommended for use in pregnant women and women of childbearing potential not using contraception.
Breastfeeding period.
Olopatadine was excreted in breast milk when administered orally to animals (see section 5.1 for details). A risk to the newborn/infants cannot be excluded. The product should not be used during breast-feeding.
Reproductive function.
No studies have been conducted to evaluate the effect of olopatadine on human reproductive function following topical ophthalmic administration.
Ability to influence reaction speed when driving vehicles or other mechanisms
Olopatadine UNIMED PHARMA has no or negligible influence on the ability to drive or operate machinery.
As with any eye drops, temporary blurred vision or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs during instillation, the patient should wait until vision clears before driving or using machines.
Method of administration and doses
For ophthalmic use only.
Instill 1 drop of the drug into the conjunctival sac of the affected eye(s) twice a day (8 hours apart). If necessary, treatment may last up to 4 months.
Use in elderly patients. There is no need for dosage adjustment for this category of patients.
Use in children and adolescents. Can be used in pediatric practice in children from 3 years of age at the same dosage as in adults. The safety and efficacy of the drug in children under 3 years of age have not been studied. Data on this age group are not available.
Use in hepatic and renal impairment: Olopatadine eye drops have not been studied in patients with hepatic or renal impairment. However, no dosage adjustment is necessary in patients with hepatic or renal impairment (see Pharmacokinetics).
To prevent contamination of the dropper tip and contents of the bottle, care should be taken not to touch the eyelids, surrounding areas, or other surfaces with the tip of the dropper cap. The bottle should be tightly closed after each use.
If more than one ophthalmic agent is applied topically, the interval between their applications should be at least 5 minutes. Eye ointments should be applied last.
Children.
The drug can be used in children aged 3 years and older in the same dosage as adults.
Overdose
There are no data on overdose in humans after accidental or intentional ingestion. Olopatadine has shown low acute toxicity in animals. Accidental ingestion of the entire vial would result in a maximum systemic exposure of 5 mg olopatadine. This exposure would occur at a final dose of 0.5 mg/mL in a 10 kg child assuming 100% absorption.
QT prolongation in dogs was observed only at doses significantly in excess of the maximum human dose, indicating that QT prolongation is unlikely to occur in clinical practice. When 5 mg of olopatadine was administered orally twice daily for 2.5 days to healthy volunteers, young adults, and elderly patients, a slight increase in QT interval was observed compared to placebo. Peak plasma concentrations of olopatadine (35 to 127 ng/mg) were at least 70-fold greater than those observed with topical olopatadine for its effects on cardiac repolarization.
In case of overdose, appropriate examination and treatment of the patient is necessary.
Adverse reactions
In clinical studies involving 1680 patients, olopatadine was administered one to four times daily in both eyes for four months as monotherapy or as add-on therapy to loratadine 10 mg.
Approximately 4.5% of patients may experience adverse reactions related to the use of olopatadine; however, only 1.6% of patients discontinued clinical trials due to these adverse reactions. No serious ophthalmic or systemic adverse reactions related to olopatadine were reported in clinical trials. The most common treatment-related adverse reaction was eye pain, with an overall incidence of 0.7%.
(≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10000 to <1/1000), very rare (<1/10000) or not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing incidence.
Organ System - Frequency: Adverse Reactions
Infections and infestations - Uncommon: rhinitis;
Immune system disorders - Not known: hypersensitivity, facial swelling;
Nervous system disorders: Common: headache, dysgeusia; Uncommon: dizziness, hypoaesthesia, hypoaesthesia; Not known: drowsiness;
Ophthalmological disorders - Common: eye pain, eye irritation, dry eye, abnormal eye sensitivity; Uncommon: corneal erosion, corneal epithelial damage, corneal epithelial disorder, punctate keratitis, keratitis, corneal discoloration, eye discharge, photophobia, blurred vision, decreased visual acuity, blepharospasm, ocular discomfort, ocular pruritus, conjunctival follicles, conjunctival disorder, foreign body sensation in eye, lacrimation increased, eyelid erythema, ocular hyperemia, eyelid edema; Not known: eyelid disorder, ocular hyperemia, corneal edema, eye edema, eye swelling, conjunctivitis, mydriasis, visual impairment, eyelid margin scaling, eye edema;
Respiratory, thoracic and mediastinal disorders: Common: nasal dryness; Not known: dyspnoea, sinusitis;
Gastrointestinal - Not known: nausea, vomiting;
Skin and subcutaneous tissue disorders: Uncommon: contact dermatitis, burning sensation on the skin, dry skin; Not known: dermatitis, erythema;
General disorders - Common: fatigue; Not known: asthenia, malaise.
In patients with significant corneal damage, cases of corneal calcification have been reported very rarely with the use of eye drops containing phosphates.
Reporting adverse reactions after registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of a medicinal product via the Automated Pharmacovigilance Information System at the link: https://aisf.dec.gov.ua.
Expiration date
2 years.
After first opening, store for no more than 8 weeks.
Storage conditions
Store out of the reach of children, at a temperature not exceeding 25 °C in the original packaging. Do not freeze.
Packaging
5 ml or 10 ml in a dropper bottle, 1 dropper bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
LLC "UNIMED PHARMA"/"UNIMED PHARMA Ltd".
Location of the manufacturer and address of its place of business.
Orieskova Street 11, 821 05, Bratislava, Slovak Republic/
Orieskova 11, 821 05 Bratislava, Slovak Republic.
