Olopatadine Hydrochloride Ophthalmic Solution USP, 0.1% is a sterile ophthalmic solution containing Olopatadine, a relatively selective H 1-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]-6-11dihydrodibenz[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. Inactives: Dibasic Sodium Phosphate; Sodium Chloride; Hydrochloric Acid/Sodium Hydroxide (adjust pH); and Water for Injection. Preservative: Benzalkonium Chloride 0.01%. 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 H 1-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, pruritus, rhinitis, sinusitis, and taste perversion. Some of these events were similar to the underlying disease being studied.

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 in a 10 mL white, low density polyethylene (LDPE) bottle with a dropper tip, and a white polypropylene cap in the following size:

NDC: 60429-957-05 5 mL in 10 mL bottle

Store at 4° to 25°C (39° to 77°F).

Rx only

AKORN



Manufactured by: Akorn, Inc.



Lake Forest, IL 60045

OLPA0N Rev. 01/17

Marketed/Packaged by:

GSMS, Inc.

Camarillo, CA 93012

Principal Display Panel Text for Container Label:

NDC 60429-957-05

Olopatadine HCl

Ophthalmic Solution, USP

0.1%

FOR USE IN THE EYES ONLY

Rx only 5 mL

Principal Display Panel Text for Carton Label:

NDC 60429-957-05

Olopatadine

HCl

Ophthalmic

Solution, USP

0.1%

FOR USE IN THE EYES

ONLY

5 mL

Rx only