OLOPATADINE HYDROCHLORIDE solution/ drops

Olopatadine Hydrochloride by

Drug Labeling and Warnings

Olopatadine Hydrochloride by is a Prescription medication manufactured, distributed, or labeled by Cipla USA Inc., Cipla Limited- Indore. Drug facts, warnings, and ingredients follow.

Drug Details [pdf]

DESCRIPTION

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

SPL UNCLASSIFIED SECTION

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; 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.

CLINICAL PHARMACOLOGY

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 60-70% 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.

INDICATIONS AND USAGE

Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% is indicated for the treatment of the signs and symptoms of allergic conjunctivitis.

CONTRAINDICATIONS

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%.

WARNINGS

Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% is for topical use only and not for injection or oral use.

PRECAUTIONS

Information for Patients:

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.

Patients should be advised not to wear a contact lens if their eye is red. Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% should not be used to treat contact lens related irritation. The preservative in Olopatadine Hydrochloride Ophthalmic Solution USP 0.1%, benzalkonium chloride, may be absorbed by soft contact lenses. Patients who wear soft contact lenses and whose eyes are not red should be instructed to wait at least ten minutes after instilling Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% before they insert their contact lenses.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

Olopatadine administered orally was not carcinogenic in mice and rats in doses up to 500 mg/kg/day and 200 mg/kg/day, respectively. Based on a 40 microliter drop size, these doses were 78,125 and 31,250 times higher than the maximum recommended ocular human dose (MROHD). 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 MROHD 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: Pregnancy Category C.

Olopatadine was found not to be teratogenic in rats and rabbits. However, rats treated at 600 mg/kg/day, or 93,750 times the MROHD and rabbits treated at 400 mg/kg/day, or 62,500 times the MROHD, during organogenesis showed a decrease in live fetuses. 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.

Nursing Mothers:

Olopatadine has been identified in the milk of nursing rats following oral administration. It is not known whether topical ocular administration could result in sufficient systemic absorption to produce detectable quantities in the human breast milk. Nevertheless, caution should be exercised when Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% is administered to a nursing mother.

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 or effectiveness have been observed between elderly and younger patients.

ADVERSE REACTIONS

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.

DOSAGE AND ADMINISTRATION

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

HOW SUPPLIED

Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% is supplied as follows: 5 mL in white opaque low density polyethylene bottle with translucent low density polyethylene dropper and white opaque high density polyethylene cap.

5 mL: NDC 69097-275-35

Storage: Store between 4°C-25°C (39°F-77°F), Protect from light.

Rx Only

Manufactured by:

Cipla Ltd.

Plot 9 & 10, Indore SEZ,

Pithampur, M.P.-454 775,

INDIA

Manufactured for:

Cipla USA, Inc.,

1560, Sawgrass, Suite 130,

Sunrise, FL, 33323

Revised Date: 04/ 2018

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL

NDC: 69097-275-35

0.1%

Olopatadine

Hydrochloride

Ophthalmic Solution, USP

0.1%

Rx ONLY

label

NDC: 69097-275-35  Rx only

Olopatadine Hydrochloride

Ophthalmic

Solution, USP

0.1%

For Topical Application

In the Eye

5ml

Cipla

carton label

INGREDIENTS AND APPEARANCE

OLOPATADINE HYDROCHLORIDE 
olopatadine hydrochloride solution/ drops

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	Item Code (Source)	NDC: 69097-275
Route of Administration	OPHTHALMIC

Active Ingredient/Active Moiety
Ingredient Name	Basis of Strength	Strength
OLOPATADINE HYDROCHLORIDE (UNII: 2XG66W44KF) (OLOPATADINE - UNII:D27V6190PM)	OLOPATADINE	1 mg  in 1 mL

Inactive Ingredients
Ingredient Name	Strength
HYDROCHLORIC ACID (UNII: QTT17582CB)
SODIUM PHOSPHATE, DIBASIC (UNII: GR686LBA74)
SODIUM CHLORIDE (UNII: 451W47IQ8X)
SODIUM HYDROXIDE (UNII: 55X04QC32I)
WATER (UNII: 059QF0KO0R)
BENZALKONIUM CHLORIDE (UNII: F5UM2KM3W7)

Packaging
#	Item Code	Package Description	Marketing Start Date	Marketing End Date
1	NDC: 69097-275-35	5 mL in 1 BOTTLE, DROPPER; Type 0: Not a Combination Product	07/26/2017

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
ANDA	ANDA206046	07/26/2017

Labeler - Cipla USA Inc. (078719707)

Registrant - Cipla USA Inc. (078719707)

Establishment
Name	Address	ID/FEI	Business Operations
Cipla Limited- Indore		918596409	ANALYSIS(69097-275) , MANUFACTURE(69097-275) , LABEL(69097-275) , PACK(69097-275)