Opatadine eco

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT OPATADIN ECO (OPATADIN ECO)

Composition:

Active substance: olopatadine;

1 ml of solution contains olopatadine 1 mg (as olopatadine hydrochloride);

Excipients: disodium hydrogen phosphate dodecahydrate; sodium chloride; polysorbate 80; hydrochloric acid diluted; water for injections.

Pharmaceutical form. Eye drops, solution.

Main physicochemical properties: clear, colorless or almost colorless liquid.

Pharmacotherapeutic group.

Agents for use in ophthalmology. Anti-inflammatory and antiallergic agents.

ATC code S01GX09.

Pharmacological properties.

Pharmacodynamics.

Olopatadine is a potent, selective antiallergic/antihistamine agent with multiple distinct mechanisms of action. It antagonizes the release of histamine (the primary mediator of allergic reactions in humans) and prevents histamine-induced stimulation of cytokine production by human conjunctival epithelial cells. In vitro studies indicate that the drug acts on conjunctival mast cells, inhibiting the release of inflammatory mediators. Clinical observations have shown that topical ophthalmic use of OPATADIN ECO in patients with patent nasolacrimal ducts reduces nasal signs and symptoms commonly associated with seasonal allergic conjunctivitis. The drug does not cause clinically significant changes in pupil diameter.

Preclinical data obtained from standard safety, pharmacology, repeated-dose toxicity, genotoxicity, carcinogenic potential, and reproductive toxicity studies revealed no hazard to humans.

Animal studies showed delayed pup development during lactation in females administered systemic doses of olopatadine exceeding the maximum recommended dose for human ophthalmic use. Olopatadine was detected in the milk of lactating rats following oral administration.

Pharmacokinetics.

Olopatadine is systemically absorbed, as with other topically applied medications. However, systemic absorption following topical application is minimal, and plasma concentrations range from below the limit of quantification (< 0.5 ng/mL) to 1.3 ng/mL. These concentrations are 50–200 times lower than those achieved with orally administered doses that are well tolerated.

Pharmacokinetic studies following oral administration showed that the plasma half-life of olopatadine is approximately 8–12 hours, with the drug being primarily eliminated via the kidneys. Approximately 60–70% of the administered dose was recovered in urine as unchanged active substance. Two metabolites, monodesmethyl and N-oxide, were detected in urine at low concentrations.

Since olopatadine is excreted in urine predominantly as unchanged active substance, its pharmacokinetics are altered in patients with impaired renal function. Peak plasma concentrations in patients with severe renal impairment (mean creatinine clearance of 13 mL/min) are 2–3 times higher than in healthy adult volunteers. In patients undergoing hemodialysis after a 10 mg oral dose, plasma olopatadine concentrations were significantly lower on dialysis days compared to non-dialysis days, suggesting that olopatadine is removed during hemodialysis.

Comparative pharmacokinetic studies following a 10 mg oral dose in young subjects (mean age 21 years) and elderly subjects (mean age 74 years) showed no significant differences in plasma concentrations, protein binding, or urinary excretion of unchanged drug and metabolites.

Studies of olopatadine following oral administration in patients with severe renal impairment have been conducted. Results suggest that somewhat higher plasma concentrations may be expected in this patient group when using OPATADIN ECO. However, since plasma concentrations after topical ophthalmic administration of olopatadine are 50–200 times lower than those achieved with well-tolerated oral doses, dosage adjustment is not required for elderly patients or those with renal impairment. Hepatic metabolism is not a major elimination pathway for the drug; therefore, dosage adjustment is not necessary for patients with hepatic impairment.

Clinical characteristics.

Indications.

Treatment of seasonal allergic conjunctivitis.

Contraindications.

Hypersensitivity to olopatadine or to any excipient of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

No studies on the interaction of OPATADIN ECO with other medicinal products have been conducted.

In vitro studies have shown that olopatadine does not inhibit metabolic reactions of cytochrome P450 isoenzymes 1A2, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4. These results indicate that olopatadine is unlikely to cause metabolic interactions with other active substances when used concomitantly.

Special precautions for use

OPATADIN ECO is a topical antiallergic/antihistamine agent that is subject to systemic absorption. The drug should be discontinued if any signs of serious reactions or increased sensitivity occur.

The effect of the medicinal product on contact lenses has not been studied. Contact lenses should be removed prior to instillation of the drops; lenses may be reinserted 15 minutes after administration.

Use during pregnancy or breastfeeding

Pregnancy

Data on the ophthalmic use of olopatadine in pregnant women are lacking or very limited. Animal studies have shown reproductive toxicity following systemic administration (see section "Pharmacological properties"). Olopatadine is not recommended for use in pregnant women or in women of childbearing potential who are not using contraception.

Breastfeeding period

Animal studies have shown that olopatadine passes into breast milk following oral administration (see section "Pharmacological properties"). A risk to newborns/infants cannot be excluded. OPATADIN ECO should not be used during breastfeeding.

Fertility

There have been no studies on the effect of olopatadine on human fertility following topical ophthalmic administration.

Effect on ability to drive and use machines

OPATADIN ECO has no effect or has a negligible effect on the ability to drive and operate machinery. As with any eye drops, transient blurred vision or other visual disturbances may affect the ability to drive or operate machinery. If blurred vision occurs upon instillation, patients should wait until vision clears before driving or operating machinery.

Method of Administration and Dosage

For ophthalmic use only.

One drop of OPATADIN ECO should be instilled into the conjunctival sac of the affected eye(s) twice daily (with an 8-hour interval). If necessary, treatment may last up to 4 months.

Use in elderly patients

No dosage adjustment is required for this patient group.

Use in children and adolescents

The medicinal product OPATADIN ECO can be used in pediatric practice for children aged 3 years and older at the same dosage as in adults. The safety and efficacy of OPATADIN ECO in children under 3 years of age have not been established. Data regarding this age group are lacking.

Use in hepatic and renal impairment

Studies with olopatadine in the form of ophthalmic drops (OPATADIN ECO) have not been conducted in patients with hepatic or renal impairment. However, no dosage adjustment is necessary in cases of hepatic or renal impairment (see section "Pharmacokinetics").

After the first opening of the bottle, remove the safety ring designed for first-opening control.

The medicinal product OPATADIN ECO is a sterile solution that does not contain preservatives.

Before using the medicinal product:

• Before first use, practice using the dropper bottle by slowly squeezing it to instill one drop into the eye without touching the eye.
• If the patient feels confident about instilling one drop, they should choose the most comfortable position (sitting, lying on the back, or standing in front of a mirror).

Administration of the medicinal product:

1. Wash hands thoroughly before applying the medication.
2. Do not use the drops if the packaging or bottle is damaged.
3. Ensure that the tamper-evident ring on the cap is intact. Before first use, unscrew the cap: slight resistance may be felt when breaking the tamper-evident ring.
4. If the tamper-evident ring is damaged during first opening, remove and discard it to avoid injury.
5. Tilt the head backward and gently pull down the lower eyelid to create a space between the eyeball and the eyelid. Avoid contact between the dropper tip and the eye, eyelids, or fingers.
6. Gently squeeze the bottle walls to allow the drop to enter the eye. Note that there may be a delay of several seconds between squeezing the bottle and the drop falling. Do not squeeze too hard. If the patient is unsure how to administer the drops, they should consult a physician, pharmacist, or nurse.
7. If the physician has prescribed the medication for the other eye, repeat steps 5–7.
8. After use and before subsequent use, shake the bottle once, holding it with the dropper tip facing downward, without touching the dropper tip, to remove residual solution from the tip. This is necessary to ensure proper delivery of subsequent drops. After instillation, screw the cap back onto the bottle.

If more than one ophthalmic agent is used locally, the interval between administrations should be at least 5 minutes. Ophthalmic ointments should be applied last.

Children.

The medicinal product OPATADIN ECO can be used in children aged 3 years and older at the same dosage as in adults.

Overdose.

There are no data on overdose in humans following accidental or intentional ingestion. Olopatadine showed a low level of acute toxicity in animals. Accidental ingestion of the entire contents of one bottle of OPATADIN ECO would result in a maximum systemic exposure of 5 mg of olopatadine. This exposure could occur at a final dose of 0.5 mg/mL in a child weighing 10 kg with 100% absorption.

Prolongation of the QT interval in dogs was observed only at doses significantly exceeding the maximum human dose, indicating a low likelihood of QT prolongation during clinical use. In a study involving 102 healthy volunteers, including young men and women and elderly individuals, who received 5 mg of the drug orally twice daily for 2.5 days, a slight increase in QT interval was observed compared to placebo. In this study, the maximum plasma concentration of olopatadine (ranging from 35 to 127 ng/mL) was at least 70 times higher than the level achieved with topical olopatadine administration regarding its effect on cardiac repolarization.

In case of overdose, appropriate patient evaluation and treatment should be initiated.

Adverse reactions.

During clinical studies involving 1680 patients, the medicinal product OPATADINE ECO was administered once to four times daily in both eyes for up to 4 months, either as monotherapy or as add-on therapy to loratadine 10 mg. Adverse reactions related to the use of OPATADINE ECO were observed in approximately 4.5% of patients; however, only 1.6% of patients discontinued participation in clinical studies due to these adverse reactions. No serious ophthalmological or systemic adverse events related to the use of the medicinal product were reported during clinical studies. The most common adverse effect associated with OPATADINE ECO was ocular pain, occurring at a frequency of 0.7%.

The adverse reactions listed below were reported during clinical studies and in the post-marketing period, and are classified by frequency: very common (≥1/10), common (>1/100, <1/10), uncommon (>1/1000, ≤1/100), rare (>1/10000, ≤1/1000), very rare (≤1/10000), frequency not known (cannot be estimated from available data). Within each group, adverse reactions are listed in order of decreasing severity.

In patients with significant corneal involvement, corneal calcification has very rarely been reported with the use of ophthalmic drops containing phosphates.

Reporting of suspected adverse reactions

Reporting of suspected adverse reactions after registration of the medicinal product is important. This allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are required to report any suspected adverse reactions.

Shelf life. 2 years.

Shelf life after first opening – 90 days.

Storage conditions.

Store at a temperature not exceeding 30 °C.

Keep out of reach and sight of children.

Packaging. 5 ml of solution in a 5 ml polyethylene dropper bottle with a cap equipped with a tamper-evident ring. 1 or 3 bottles with the package leaflet in a cardboard box.

Prescription status. Prescription only.

Marketing Authorization Holder.

Pharmaceutical Works “POLPHARMA” S.A.

Pharmaceutical Works “POLPHARMA” S.A.

Address of the Marketing Authorization Holder and location of its operating site.

19, Pelplinska Str., 83-200 Starogard Gdanski, Poland

19, Pelplinska Str., 83-200 Starogard Gdanski, Poland

Manufacturer.

Rafarm S.A.

Rafarm S.A.

Address of the manufacturer and location of its operating site.

Thesi Pousi Xatzi Agiou Louka, Paiania, 190 02, Greece

Thesi Pousi Xatzi Agiou Louka, Paiania, 190 02, Greece