Vizallerol

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT VIZALLERGOL (VISALLERGOL)

Composition:

Active substance: olopatadine;

1 ml of solution contains 2.22 mg of olopatadine hydrochloride equivalent to 2.0 mg of olopatadine;

Excipients: benzalkonium chloride, povidone K-29/32, sodium chloride, disodium edetate, anhydrous sodium hydrogen phosphate, hydrochloric acid, sodium hydroxide, water for injections.

Pharmaceutical form. Eye drops.

Main physicochemical properties: clear solution ranging from colorless to light yellow.

Pharmacotherapeutic group.

Ophthalmological agents. Anti-inflammatory and antiallergic agents.

ATC code S01GX09.

Pharmacological Properties.

Pharmacodynamics.

Olopatadine is a potent, selective antiallergic/antihistamine agent with multiple pronounced mechanisms of action. It counteracts 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 mast cells of the human conjunctiva, inhibiting the release of inflammatory mediators. It has been observed that local ophthalmic administration of VizallerGol 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 development in offspring nursed by females that received systemic doses of olopatadine exceeding the maximum recommended for ophthalmic use in humans. Olopatadine was detected in animal milk after oral administration.

Pharmacokinetics.

Olopatadine is systemically absorbed, as with other locally applied medicinal products. However, following topical administration, systemic absorption of olopatadine is minimal, and plasma concentrations range from below the quantifiable limit (< 0.5 ng/mL) to 1.3 ng/mL. These concentrations are 50 to 200 times lower than those achieved with oral administration of well-tolerated doses of the drug.

Since olopatadine is excreted in urine predominantly as unchanged active substance, its pharmacokinetics are altered in renal impairment. Peak plasma concentrations in patients with severe renal insufficiency (mean creatinine clearance – 13 mL/min) are 2 to 3 times higher than those in healthy adult volunteers.

Clinical characteristics.

Indications.

Treatment of seasonal allergic conjunctivitis.

Contraindications.

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

Interaction with other medicinal products and other forms of interaction.

Studies on the interaction of VizallerGol with other medicinal products have not been conducted.

In vitro studies have shown that olopatadine does not inhibit metabolic reactions of the 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

Vizallerhol is an antiallergic/antihistamine agent administered locally but which is systemically absorbed. The drug should be discontinued if any signs of serious reactions or hypersensitivity occur.

Vizallerhol contains benzalkonium chloride, which may cause eye irritation.

There have also been reports that benzalkonium chloride may cause punctate keratopathy and/or toxic ulcerative keratopathy. Patients with dry eye syndrome or corneal damage who use the product frequently or over prolonged periods should be carefully monitored.

Contact lenses

Benzalkonium chloride is known to discolor contact lenses. Contact with soft contact lenses should be avoided. Patients should be advised to remove contact lenses before instilling the drops and to wait at least 15 minutes after instillation before reinserting the contact lenses.

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

Use during pregnancy or breastfeeding

Pregnancy

Data on the ophthalmic use of olopatadine in pregnant women are lacking or limited in quantity. Animal studies have revealed 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 contraceptive measures.

Breastfeeding period

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

Reproductive function

No studies have been conducted on the effect of olopatadine on human reproductive function following topical ophthalmic administration.

Ability to influence reaction rate while driving or operating machinery

Vizallerhol has no effect or has a negligible effect on the ability to drive or operate machinery. However, as with the use of 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, the patient should wait until vision clears before driving or operating machinery.

Administration and Dosage

For ophthalmic use only.

One drop of Vizallerghol should be instilled into the conjunctival sac of the affected eye(s) once daily. If necessary, treatment may continue for up to 4 months.

Use in elderly patients

Dosage adjustment is not required for this patient group.

Use in children and adolescents

Vizallerghol may be used in children aged 3 years and older at the same dosage as in adults. Safety and efficacy of Vizallerghol in children under 3 years of age have not been established. Data in this age group are lacking.

Use in patients with hepatic or renal impairment

Studies with olopatadine in the form of Vizallerghol eye drops in patients with hepatic or renal impairment have not been conducted. However, dosage adjustment is not required in cases of hepatic or renal dysfunction (see section "Pharmacokinetics" for detailed information).

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

To prevent contamination of the dropper tip and the bottle's contents, care should be taken not to touch eyelids, surrounding areas, or other surfaces with the dropper tip. The dropper bottle must be tightly closed after each use.

Children

Vizallerghol may 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 a Vizallerghol bottle 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 animals was observed only at doses substantially exceeding the maximum human dose, suggesting a low likelihood of QT prolongation during clinical use. In a study involving 102 healthy volunteers, including young men and women as well as 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, peak plasma concentrations of olopatadine (ranging from 35 to 127 ng/mL) were at least 70 times higher than those achieved with topical olopatadine administration regarding effects on cardiac repolarization.

In case of overdose, appropriate monitoring and symptomatic treatment should be initiated.

Adverse reactions.

The adverse reactions listed below are classified according to the following criteria: very common (≥1/10), common (>1/100, <1/10), uncommon (>1/1000, ≤1/100), rare (>1/10000, ≤1/1000), very rare (≤1/10000), or 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, very rare cases of corneal calcification have been reported with the use of ophthalmic solutions containing phosphates.

Reporting suspected adverse reactions for registered medicinal products is very important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are requested to report suspected adverse reactions via the system established by current legislation.

Shelf life. 2 years.

Do not use more than 28 days after first opening the bottle.

Storage conditions.

Store at a temperature from 2 °C to 25 °C in the original packaging.

Keep out of the reach of children.

Packaging.

2.5 ml in a plastic bottle with dropper, № 1 in a pack.

Prescription status.

Prescription only.

Manufacturer.

SENTISS PHARMA PVT. LTD., India.

Manufacturer's address.

Village Khera Nihla, Tehsil Nalagarh, Distt. Solan, Himachal Pradesh, 174 101, India.

Marketing Authorization Holder.

SENTISS PHARMA PVT. LTD., India.

Address of the Marketing Authorization Holder.

212/D-1, Ashirwad Commercial Complex, Green Park, New Delhi, 110016, India.