Action And Clinical Pharmacology: Olopatadine is a mast cell stabilizer and a potent, selective histamine H1 antagonist that inhibits the in vivo type 1 immediate hypersensitivity reaction. In vitro studies have demonstrated the ability of olopatadine to stabilize rodent basophils and human conjunctival mast cells and inhibit antigen-stimulated release of histamine. In addition, olopatadine inhibits the release of other mast cell inflammatory mediators (i.e., tryptase and prostaglandin D2) as demonstrated in in vitro studies. Olopatadine is a selective histamine H1 receptor antagonist in vitro and in vivo as demonstrated by its ability to inhibit binding and histamine-stimulated vascular permeability in the conjunctiva following topical ocular administration. Olopatadine is devoid of effects on alpha-adrenergic, dopamine, muscarinic type 1 and 2, and serotonin receptors.
Pharmacokinetics: Following topical ocular administration in man, olopatadine was shown to have low systemic exposure. Two studies in normal volunteers (totalling 24 subjects) dosed bilaterally with olopatadine 0.15% ophthalmic solution once every 12 hours for 2 weeks demonstrated plasma concentrations to be generally below the quantitation limit of the assay.
Indications And Clinical Uses: For the treatment of allergic conjunctivitis.
Contra-Indications: Hypersensitivity to any component of this product.
Manufacturers’ Warnings In Clinical States: For topical use only. Not for injection. Patients should be instructed not to instill olopatadine ophthalmic solution while wearing contact lenses, but to wait for 10 minutes after instillation before inserting contact lenses.
Precautions: Information for the Patient: To prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use.
Carcinogenesis, Mutagenesis, Impairment of Fertility: Olopatadine was not carcinogenic in mice and rats of either sex at doses up to 78 000 and 31 000 times the maximum recommended ocular human use level, respectively. No mutagenic potential was observed when olopatadine was tested in an in vitro bacterial reverse mutation (Ames) test, an in vitro mammalian chromosome aberration assay or an in vivo mouse micronucleus test. Olopatadine administered to male and female rats at oral doses of 62 500 times the maximum recommended ocular human use level resulted in a slight decrease in the fertility index and reduced implantation rate; no effects on reproductive function were observed at doses of 7 800 times the maximum recommended ocular human use level.
Pregnancy: Olopatadine was found not to be teratogenic in rats and rabbits at oral doses >90 000 and >60 000 times the maximum recommended ocular human use level, respectively. There are, however, no adequate and well controlled studies in pregnant women. Because animal studies are not always predictive of human responses, this drug should be used in pregnant women only if the potential benefit to the mother justifies the potential risk to the embryo or fetus.
Lactation: Olopatadine has been identified in the milk of nursing rats following oral administration. Rat pups of mothers administered olopatadine orally at greater than 625 times (but not at 312 times) the maximum recommended ocular human use level demonstrated reduced body weight gain during the nursing period. It is not known whether topical ocular administration could result in sufficient systemic absorption to produce detectable quantities in human breast milk. Nevertheless, caution should be exercised when olopatadine ophthalmic solution is administered to a nursing mother.
Children: Safety and effectiveness in pediatric patients between the ages of 3 and 16 have been established.
Adverse Reactions: In clinical studies of olopatadine ophthalmic solution, ocular and nonocular adverse reactions related to therapy were reported at an incidence below 1%.
Ocular: mild transient burning or stinging, pruritus, hyperemia, foreign body sensation, superficial keratitis, lid edema, dry eye, lid dryness, lid spasm, photophobia.
Nonocular: asthenia, headache, taste perversion.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: A topical overdosage may be flushed from the eye(s) with warm tap water.
Dosage: The recommended dose is 1 to 2 drops in each affected eye twice daily.
Availability And Storage: Each mL of ophthalmic solution contains: olopatadine HCl 1.11 mg equivalent to olopatadine 1 mg. Nonmedicinal ingredients: benzalkonium chloride, dibasic sodium phosphate, hydrochloric acid/sodium hydroxide (to adjust pH), purified water and sodium chloride. Plastic Drop-Tainer dispensers of 5 mL. Store at 4 to 30°C.
PATANOL Alcon Olopatadine HCl Antiallergy Agent