Pataday

Pataday

olopatadine

Manufacturer:

Novartis

Distributor:

DKSH
Full Prescribing Info
Contents
Olopatadine hydrochloride.
Description
Active ingredients: 2.22 mg of olopatadine hydrochloride in one mL solution (0.2%).
Preservative: benzalkonium chloride.
Excipients/Inactive Ingredients: Benzalkonium Chloride, Edetate Disodium, Povidone, Sodium Chloride, Anhydrous Dibasic Sodium Phosphate, Sodium Hydroxide and/or Hydrochloric Acid, Purified Water.
Action
Pharmacotherapeutic group: Ophthalmologicals; decongestant and antiallergics; other antiallergics. ATC code: S01GX09.
Pharmacology: Pharmacodynamics: Olopatadine is a potent selective antiallergic/antihistaminic agent that exerts its effects through multiple distinct mechanisms of actions. It antagonizes histamine (the primary mediator of allergic response in humans) and prevents histamine induced inflammatory cytokine production by human conjunctival epithelial cells. Data from in vitro studies suggest that it may act on human conjunctival mast cells to inhibit the release of pro-inflammatory mediators. In patients with patent nasolacrimal ducts, topical ocular administration of Olopatadine Eye Drops, Solution was suggested to reduce the nasal signs and symptoms that frequently accompany seasonal allergic conjunctivitis. It does not produce a clinically significant change in pupil diameter.
Pharmacokinetics: Absorption: Olopatadine was absorbed into the eye and reached maximal levels (Cmax) within 30 minutes to 2 hours (Tmax) in ocular tissues following bilateral single topical ocular instillation of 1 drop of increasing dose strengths of Olopatadine (0.15%, 0.2% and 0.7%) in Male New Zealand White (NZW) Rabbits. Plasma levels of Olopatadine were low (Cmax <20 ng/mL) following bilateral topical ocular administration of 0.15%/0.2%/0.7% Olopatadine ophthalmic solution to rabbits.
In the humans, plasma levels following topical ocular administration (2 drops of 0.1% in both eyes, four times-daily, 4 days; 2 drops of 0.15% in both eyes, twice daily, 14 days; 2 drops of 0.2% in both eyes, twice daily, 7 days; 1 drop of 0.77% in each eye for 7 days) and oral administration (20 mg, twice daily, 13.5 days) are shown in Table 1. Compared with the oral administration exposure on Day 12, the mean exposure estimates show Olopatadine Cmax (1.64 ng/mL) and AUC0-12 (9.68 ngh/mL) after multiple 0.77% topical ocular doses was 184-fold and 102-fold lower than the Cmax (302 ng/mL) and AUC0-12 (987 ngh/mL) after multiple 20 mg oral doses of Olopatadine. These data indicate that topical ocular doses of 0.77% Olopatadine hydrochloride ophthalmic solution has a wide margin of safety since it resulted in a systemic exposure that is much lower than that after oral doses of 20 mg Olopatadine hydrochloride. (See Table 1.)

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Distribution: Studies in rabbits show ocular tissues associated with the site of dosing i.e., conjunctiva and cornea, had the highest concentrations of Olopatadine after bilateral single topical ocular instillation of 1 drop of increasing dose strengths of Olopatadine (0.15%, 0.2% and 0.7%) in Male New Zealand White (NZW) Rabbits. Olopatadine concentrations in aqueous humor, choroids, ICB and lens increases with increasing concentrations of Olopatadine. Studies conducted in pigmented Dutch belted rabbits indicated a low degree of binding to melanin pigmented tissues.
Biotransformation/Metabolism: Studies have not been conducted to investigate the metabolism of Olopatadine in ocular tissues since toxicology and clinical studies have shown it to be safe and effective. The major metabolites of Olopatadine following oral administration in humans are N-desmethyl Olopatadine (M1) and Olopatadine N-oxide (M3). N-desmethyl Olopatadine (M1) is almost exclusively demethylated by the cytochrome P-450 isozyme 3A4 (CYP3A4). Olopatadine was not an inhibitor of cytochrome P-450 isozymes and therefore drug-drug interactions due to metabolic interactions were not expected.
In the humans after topical ocular administration, N-desmethyl metabolite of Olopatadine (M1) was not quantifiable (≤0.050 ng/mL) in plasma sample in all subjects.
Excretion/Elimination: Studies have not been conducted to investigate the excretion of Olopatadine in the urine or feces after topical ocular instillation. In rats after 14C oral administration, Olopatadine was rapidly eliminated from the body primarily by urinary excretion and biotransformation (metabolism). In humans, urinary excretion of unchanged drug was the major route of elimination.
Studies conducted to investigate the elimination of Olopatadine in rabbits showed concentrations of Olopatadine in various ocular tissues (aqueous humor, choroid, conjunctiva, cornea, and ICB) over the dose strengths (0.1 to 0.7% ophthalmic solution) declined with a half-life of less than 4.65 hours.
In humans, the systemic plasma half-life was less than 3 hours.
Linearity/Non-Linearity: In a single dose study, Olopatadine showed a dose proportional increasing in exposure (Cmax and AUC) in ocular tissues after topical ocular instillation.
Toxicology: Preclinical Safety Data: Non-clinical data reveal no special hazard for humans treated with Olopatadine Hydrochloride Eye Drops, Solution at concentrations up to and including 0.7% based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, and carcinogenic potential.
Effects in non-clinical reproductive and developmental toxicity studies were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use.
Oral doses of up to 400 mg/kg/day (~40,000-fold higher than the prescribed dose in a 50 kg adult treated with the highest concentration of Olopatadine commercially available, 0.7%) resulted in some general toxicity, but had no effect on fertility and general reproductive parameters when either males or females were treated prior to and through mating. No effects were observed on embryo-fetal development in rats or rabbits treated with Olopatadine orally, by gavage, at doses of up to 600 mg/kg/day and 400 mg/kg/day, respectively. Peri- and postnatal toxicity studies in rats demonstrated maternal toxicity, and reduced pup survival and weights at the highest dose of 600 mg/kg/day (~60,000-fold higher than the prescribed dose in a 50 kg adult treated with the highest concentration of Olopatadine commercially available, 0.7%), administered to the dam during late gestation and the lactation period. Pup viability and weight gain were also reduced at dose levels of 60 and 200 mg/kg/day. Olopatadine has been detected in the milk of nursing rats following oral administration.
Indications/Uses
PATADAY is indicated for the temporary prevention of itching of the eye due to allergic conjunctivitis.
Dosage/Direction for Use
Adults: The recommended dose is one drop in each affected eye once a day.
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 3 years have not been established.
Geriatric Use: No overall differences in safety and effectiveness have been observed between elderly and younger patients.
Method of administration: For topical ocular use only. Not for injection or oral use.
To prevent contamination of the dropper tip and solution, care must be taken not to touch the eyelids, surrounding areas, or other surfaces with the dropper tip of the bottle.
Keep the bottle tightly closed when not in use.
In case of concomitant therapy with other topical ocular medicines, an interval of 5 minutes should be allowed between successive applications. Eye ointments should be administered last.
Patients should be advised not to wear a contact lens if their eye is red.
PATADAY should not be used to treat contact lens related irritation.
Overdosage
Due to the characteristics of this preparation, no toxic effects are to be expected with an ocular overdose of this product, nor in the event of accidental ingestion of the contents of one bottle.
Contraindications
Hypersensitivity to the active substance or to any of the excipients.
Special Precautions
PATADAY contains benzalkonium chloride which may cause eye irritation and is known to discolour soft contact lenses. Avoid contact with soft contact lenses. Patients must be instructed to remove contact lenses prior to application of PATADAY and wait at least 15 minutes before reinsertion.
Effects on Ability to Drive and Use Machines: Olopatadine is a non-sedating anti-histamine. Temporary blurred vision after drop use, or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs after instillation, the patient must wait until the vision clears before driving or using machinery.
Use In Pregnancy & Lactation
Fertility: Studies have not been performed to evaluate the effect of administration of Olopatadine on human fertility. Effects in non-clinical fertility studies in male and female animals were observed only at dosages considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use (see Pharmacology: Toxicology: Preclinical Safety Data under Actions).
No effects on human fertility are anticipated since systemic exposure to Olopatadine is negligible by the topical ocular route (AUC0-6 of 9.7 nghr/mL in humans administered 1 drop of 0.77% Olopatadine in both eyes once daily for 6.5 days).
Olopatadine can be used by women of childbearing potential.
Pregnancy: There are no or limited amount of data from the use of Olopatadine in pregnant women. Effects in non-clinical reproduction and developmental toxicity studies were observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use (see Pharmacology: Toxicology: Preclinical Safety Data under Actions).
No effects during pregnancy are anticipated since systemic exposure to Olopatadine is negligible by the topical ocular route (AUC0-6 of 9.7 nghr/mL in humans administered 1 drop of 0.77% Olopatadine in both eyes once daily for 6.5 days).
Before prescribing Olopatadine to a pregnant woman, a physician should weigh the benefit of administration to the woman to the risk of the fetus (see Pharmacology: Pharmacokinetics and Toxicology: Preclinical Safety Data under Actions).
Breast-feeding: Available pharmacodynamic/toxicological data in animals have shown excretion of Olopatadine/metabolites in milk following high dose systemic Olopatadine administration. Radioactivity has been identified in the milk of nursing rats at concentrations of 0.33 to 4.28 times that of plasma concentrations (1,184 nghr/mL AUC0-24 in lactating rat plasma) following a 1 mg/kg oral administration of 14C-Olopatadine.
Based upon the low level of Olopatadine present in human plasma following topical ocular administration (AUC0-6 of 9.7 nghr/mL in humans administered 1 drop of 0.77% Olopatadine in both eyes once daily for 6.5 days), the concentration of Olopatadine potentially present in breast milk is expected to be negligible. However, as there is no data available on the concentration of Olopatadine/metabolites in human milk following topical ocular administration, a risk to the suckling child cannot be excluded.
Patients should be informed that antihistamines may affect the milk production of a nursing mother. Before prescribing Olopatadine to a nursing mother, a physician should weigh the benefit of administration to the mother to the risk of the breastfeeding child (see Pharmacology: Pharmacokinetics and Toxicology: Preclinical Safety Data under Actions).
Adverse Reactions
The following adverse reactions have been reported during clinical studies with Olopatadine hydrochloride ophthalmic solution, 0.1% and 0.2% and are classified according to the subsequent convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000) and very rare (<1/10,000). Within each frequency-grouping, adverse reactions are presented in order of decreasing seriousness. (See Table 2.)

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Post-Marketing Surveillance: Additional adverse reactions identified from post-marketing surveillance include the following. Frequencies cannot be estimated from the available data. Within each System Organ Class adverse reactions are presented in order of decreasing seriousness. (See Table 3.)

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Drug Interactions
No clinically relevant interactions have been described.
Caution For Usage
Incompatibilities: None known.
Storage
Store below 30°C. Discard 28 days after opening.
ATC Classification
S01GX09 - olopatadine ; Belongs to the class of other ophthalmologic antiallergics.
Presentation/Packing
Ophth soln 0.2% (colorless to light yellow solution) x 2.5 mL.
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