olopatadine hydrochloride

Olopatadine hydrochloride ophthalmic solution, USP 0.1 % is a sterile ophthalmic solution containing olopatadine, a relatively selective H₁-receptor antagonist and inhibitor of histamine release from the mast cell for topical administration to the eyes. Olopatadine hydrochloride is a white, crystalline, water-soluble powder with a molecular weight of 373.88. The chemical structure is presented below:

Chemical Name: 11-[(Z)-3-(Dimethylamino)propylidene]-6-11-dihydrodibenz[b,e] oxepin-2-acetic acid hydrochloride.

Each mL of olopatadine hydrochloride ophthalmic solution, USP 0.1 % contains: Active: 1.11 mg olopatadine hydrochloride equivalent to 1 mg olopatadine. Preservative: benzalkonium chloride 0.01 %. Inactives: dibasic sodium phosphate dodecahydrate; sodium chloride; hydrochloric acid/sodium hydroxide (adjust pH); and water for injection. It has a pH of approximately 7 and an osmolality of approximately 300 mOsm/kg.

Olopatadine is an inhibitor of the release of histamine from the mast cell and a relatively selective histamine H₁-antagonist that inhibits the in vivo and in vitro type 1 immediate hypersensitivity reaction including inhibition of histamine induced effects on human conjunctival epithelial cells. Olopatadine is devoid of effects on alpha-adrenergic, dopamine and muscarinic type 1 and 2 receptors. Following topical ocular administration in man, olopatadine was shown to have low systemic exposure. Two studies in normal volunteers (totaling 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 (<0.5 ng/mL). Samples in which olopatadine was quantifiable were typically found within 2 hours of dosing and ranged from 0.5 to 1.3 ng/mL. The half-life in plasma was approximately 3 hours, and elimination was predominantly through renal excretion. Approximately 60 to 70% of the dose was recovered in the urine as parent drug. Two metabolites, the mono-desmethyl and the N-oxide, were detected at low concentrations in the urine.

Results from an environmental study demonstrated that olopatadine hydrochloride ophthalmic solution, USP 0.1 % was effective in the treatment of the signs and symptoms of allergic conjunctivitis when dosed twice daily for up to 6 weeks. Results from conjunctival antigen challenge studies demonstrated that olopatadine hydrochloride ophthalmic solution, USP 0.1 %, when subjects were challenged with antigen both initially and up to 8 hours after dosing, was significantly more effective than its vehicle in preventing ocular itching associated with allergic conjunctivitis.

Olopatadine hydrochloride ophthalmic solution, USP 0.1 % is indicated for the treatment of the signs and symptoms of allergic conjunctivitis.

Olopatadine hydrochloride ophthalmic solution, USP 0.1 % is contraindicated in persons with a known hypersensitivity to olopatadine hydrochloride or any components of olopatadine hydrochloride ophthalmic solution, USP 0.1 %.

Olopatadine hydrochloride ophthalmic solution, USP 0.1% is for topical use only and not for injection or oral use.

Headaches have been reported at an incidence of 7%. The following adverse experiences have been reported in less than 5% of patients: Asthenia, blurred vision, burning or stinging, cold syndrome, dry eye, foreign body sensation, hyperemia, hypersensitivity, keratitis, lid edema, nausea, pharyngitis, pruritis, rhinitis, sinusitis, and taste perversion. Some of these events were similar to the underlying disease being studied.

To report SUSPECTED ADVERSE REACTIONS, contact ECI Pharmaceuticals, LLC at 1-888-514-4727 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

The recommended dose is one drop in each affected eye two times per day at an interval of 6 to 8 hours.

Olopatadine hydrochloride ophthalmic solution, USP 0.1% is supplied as follows: 5 mL in LDPE bottles.  

         5 mL: NDC 51293-838-85

Storage

Store at 39°F to 77°F (4°C to 25°C)

Rx Only


Manufactured by:
USV Private Limited
H-13,16,16A,17,18,19,20,21,E-22, OIDC, Mahatma
Gandhi Udyog Nagar, Dabhel, Daman - 396210, India


Manufactured for:
ECI Pharmaceuticals, LLC
Ft. Lauderdale, FL 33309

NDC 51293-838-85
Olopatadine HCl Ophthalmic Solution USP, 0.1 %
For Use in the Eyes Only
5 mL
Rx only