Patolop

Colourless, clear solution practically free from particles.
Each mL contains: Olopatadine hydrochloride, EP equivalent to olopatadine 1 mg, Benzalkonium chloride 0.10 mg equivalent to 0.2 mg Benzalkonium chloride.

Pharmacotherapeutic group: Ophthalmological; decongestant and antiallergics; other antiallergics. ATC code: S01GX 09.
Pharmacology: Pharmacodynamics: Olopatadine is a potent selective antiallergic/antihistaminic agent that exerts its effects through multiple distinct mechanisms of action. 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 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 is absorbed systemically, as are other topically administered medicinal products. However, systemic absorption of topically applied Olopatadine is minimal with plasma concentrations ranging from below the assay quantitation limit (<0.5 ng/mL) up to 1.3 ng/mL. These concentrations are 50-to 200-fold lower than those following well-tolerated oral doses.
Elimination: From oral pharmacokinetic studies, the half-life of Olopatadine in plasma was approximately eight to 12 hours, and elimination was predominantly through renal excretion. Approximately 60-70% of the dose was recovered in the urine as an active substance. Two metabolites, the mono-desmethyl, and the N-oxide, were detected at low concentrations in the urine.
Since olopatadine is excreted in urine primarily as an unchanged active substance, impairment of renal function alters the pharmacokinetics of olopatadine with peak plasma concentrations 2.3-fold greater in patients with severe renal impairment (mean creatinine clearance of 13.0 mL/min) compared to healthy adults. Following a 10 mg oral dose in patients undergoing hemodialysis (with no urinary output), plasma olopatadine concentrations were significantly lower on the hemodialysis day than on the non-hemodialysis day suggesting olopatadine can be removed by hemodialysis.
Studies comparing the pharmacokinetics of 10 mg oral doses of olopatadine in young (mean age 21 years) and elderly (mean age 74 years) showed no significant differences in the plasma concentrations (AUC), protein binding, or urinary excretion of unchanged parent drug and metabolites.
A renal impairment study after oral dosing of olopatadine has been performed in patients with severe renal impairment. The results indicate that a somewhat higher plasma concentration can be expected with olopatadine in this population. Since plasma concentrations following topical ocular dosing of Olopatadine are 50 to 200-fold lower than after well-tolerated oral doses, dose adjustment is not expected to be necessary for the elderly or in the renally impaired population. Liver metabolism is a minor route of elimination. Dose adjustment is not expected to be necessary with hepatic impairment.

It is used in the treatment of ocular signs and symptoms of seasonal allergic conjunctivitis.

The dose is one drop of Olopatadine Hydrochloride in the conjunctival sac of the affected eye or eyes twice daily (8 hourly). Treatment may be maintained for up to four months if considered necessary.
Method of administration: Inspect visually for particulate matter and discoloration prior to administration.
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 the case of concomitant therapy with other topical ocular medicines, an interval of five to ten minutes should be allowed between successive applications.
Additional data about special populations: Kidney/liver failure: Olopatadine in the form of eye drops (Olopatadine Hydrochloride) has not been studied in patients with kidney and liver failure. However, no dosage adjustment is expected to be necessary in patients with kidney and liver failure.
Pediatric population: Olopatadine Hydrochloride may be used in pediatric patients (three years of age and older) at the same dose as in adults.
Geriatric population: No dosage adjustment in elderly patients is necessary.

No data are available in humans regarding overdose by accidental or deliberate ingestion. Olopatadine has a low order of acute toxicity in animals. Accidental ingestion of the entire contents of a bottle of Olopatadine Hydrochloride would deliver a maximum systemic exposure of 5 mg of Olopatadine. This exposure would result in a final dose of 0.5 mg/kg in a 10 kg infant, assuming 100% absorption.
Prolongation of the QTc interval in dogs was observed only at exposures considered sufficiently in excess of the maximum human exposure indicating little relevance to clinical use. A 5 mg oral dose was administered twice daily for 2.5 days to 102 young and elderly male and female healthy volunteers with no significant prolongation of QTc interval compared to placebo. The range of peak steady-state olopatadine plasma concentrations (35 to 127 ng/mL) seen in this study represents at least a 70-fold safety margin for topical olopatadine with respect to effects on cardiac repolarization.
Treatment: In the case of an overdose, appropriate monitoring and follow-up of the patient is necessary.

It is contraindicated in people who have hypersensitivity to olopatadine or any of the excipients of it.

Olopatadine Hydrochloride is an antiallergic/antihistaminic agent and when administered topically, it can be absorbed systemically. If serious reactions or hypersensitivity occur, discontinue the use of this treatment.
Benzalkonium chloride which is generally used as a preservative material in ophthalmic products has been reported to cause punctate keratopathy and/or toxic ulcerative keratopathy. Close monitoring is required frequently and regularly in dry eye patients or in conditions where the cornea is compromised due to Olopatadine Hydrochloride containing benzalkonium chloride, or in conditions where the cornea is compromised.
Contact lenses: It is suitable to wait 10-15 minutes after Olopatadine Hydrochloride instillation before re-inserting contact lenses.
Effects on the ability to drive and use machines: As with other eye drops, temporary blurred vision or other visual disturbances may affect the ability to drive or use machines. If blurred vision occurs after instillation, the patient should wait until the vision clears before driving or using machinery.

General recommendation: Pregnancy category: C.
Women of childbearing potential/Contraception: There is no sufficient data on the use of olopatadine in pregnant women. Women of childbearing potential should have effective contraception during treatment.
Pregnancy period: There are no clinical data obtained from the pregnant patients for olopatadine.
Studies on animals are insufficient in terms of the effects on pregnancy and/or embryonal/fetal development and/or birth and/or post-natal development. The potential risk for humans is unknown.
Olopatadine Hydrochloride should not be used unless it is necessary in the pregnancy period. During pregnancy, it should be used only if the potential benefit is more than the potential fetal risk.
Caution should be exercised when prescribing this product to pregnant women.
Lactation period: Olopatadine Hydrochloride is not recommended for breastfeeding mothers.
Olopatadine has been detected in the milk of lactating rats following oral administration. Studies in animals have shown reduced growth of breastfed pups of she-dogs receiving systemic doses of olopatadine well in excess of the maximum level recommended for human ocular use. It is not known whether or not topical ocular administration in humans will lead to systemic absorption at a level that can be passed into breast milk.
It is not known whether topical olopatadine is excreted in human milk or not. Excretion of topical olopatadine in milk has not been studied on animals. When deciding whether breastfeeding will be stopped or not or whether Olopatadine Hydrochloride treatment will be stopped or not whether to avoid treatment or not, the benefit of breastfeeding for the child and the benefit of Olopatadine Hydrochloride treatment for the mother should be taken into consideration.
Reproductive ability/Fertility: There is no known effect on reproductive ability (fertility).

Summary of the safety profile: In clinical studies involving 1680 patients, olopatadine was administered one to four times daily in both eyes for up to four months as monotherapy or adjunctive therapy to loratadine 10 mg. Approximately 4.5% of patients can be expected to experience adverse reactions associated with the use of olopatadine; however, only 1.6% of patients discontinued the clinical studies due to these adverse reactions. No serious ophthalmic or systemic adverse reactions related to olopatadine were reported in clinical studies. The most frequent treatment-related adverse reaction was eye pain, reported at an overall incidence of 0.7%.
Tabulated list of adverse reactions: The following adverse reactions have been reported during clinical studies and post-marketing data and are classified according to the following convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (<1/10,000) or not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness. (See table.)

Click on icon to see table/diagram/image

Cases of corneal calcification have been reported very rarely in association with the use of phosphate-containing eye drops in some patients with significantly damaged corneas.

No interaction studies with other medicinal products have been performed.
In vitro studies have shown that Olopatadine did not inhibit metabolic reactions that involve cytochrome P-450 isozymes 1A2, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A4. These results indicate that Olopatadine is unlikely to result in metabolic interactions with other concomitantly administered active substances.

Special Precautions for Disposal and Other Handling: Any unused product or waste material should be disposed of in accordance with local requirements.

Store at temperatures not exceeding 30°C. Protect from light.
Product can be used for 28 days upon opening.

Ophthalmic Decongestants, Anesthetics, Anti-Inflammatories

S01GX09 - olopatadine ; Belongs to the class of other ophthalmologic antiallergics.

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