OLOPATADINE HYDROCHLORIDE- olopatadine hydrochloride solution/ drops 
Teva Pharmaceuticals USA, Inc.

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HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use OLOPATADINE HYDROCHLORIDE OPHTHALMIC SOLUTION safely and effectively. See full prescribing information for OLOPATADINE HYDROCHLORIDE OPHTHALMIC SOLUTION.

OLOPATADINE HYDROCHLORIDE ophthalmic solution 0.2%
Initial U.S. Approval: 1996

INDICATIONS AND USAGE

Olopatadine hydrochloride ophthalmic solution is a mast cell stabilizer indicated for the treatment of ocular itching associated with allergic conjunctivitis. (1)

DOSAGE AND ADMINISTRATION

The recommended dose is one drop in each affected eye once a day. (2)

DOSAGE FORMS AND STRENGTHS

Ophthalmic solution 0.2%: each mL contains 2.22 mg of olopatadine hydrochloride. (3)

WARNINGS AND PRECAUTIONS

For topical ocular use only. Not for injection or oral use. (5.1)

ADVERSE REACTIONS

Symptoms similar to cold syndrome and pharyngitis were reported at an incidence of approximately 10%. (6)

To report SUSPECTED ADVERSE REACTIONS, contact Teva Pharmaceuticals USA, Inc. at 1-866-832-8537 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

See 17 for PATIENT COUNSELING INFORMATION.

Revised: 2/2017

FULL PRESCRIBING INFORMATION: CONTENTS*

1 INDICATIONS AND USAGE

2 DOSAGE AND ADMINISTRATION

3 DOSAGE FORMS AND STRENGTHS

4 CONTRAINDICATIONS

5 WARNINGS AND PRECAUTIONS

5.1 For Topical Ocular Use Only

5.2 Contamination of Tip and Solution

5.3 Contact Lens Use

6 ADVERSE REACTIONS

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

8.3 Nursing Mothers

8.4 Pediatric Use

8.5 Geriatric Use

11 DESCRIPTION

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

12.3 Pharmacokinetics

13 NONCLINICAL TOXICOLOGY

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

14 CLINICAL STUDIES

16 HOW SUPPLIED/STORAGE AND HANDLING

17 PATIENT COUNSELING INFORMATION

17.1 Topical Ophthalmic Use Only

17.2 Sterility of Dropper Tip

17.3 Concomitant Use of Contact Lenses

Olopatadine Hydrochloride Ophthalmic Solution USP 0.2%, 2.5 mL Bottle, Carton Text

*
Sections or subsections omitted from the full prescribing information are not listed.

FULL PRESCRIBING INFORMATION

1 INDICATIONS AND USAGE

Olopatadine hydrochloride ophthalmic solution is indicated for the treatment of ocular itching associated with allergic conjunctivitis.

2 DOSAGE AND ADMINISTRATION

The recommended dose is one drop in each affected eye once a day.

3 DOSAGE FORMS AND STRENGTHS

Ophthalmic solution 0.2%: each mL contains 2.22 mg of olopatadine hydrochloride USP.

4 CONTRAINDICATIONS

None.

5 WARNINGS AND PRECAUTIONS

5.1 For Topical Ocular Use Only

Not for injection or oral use.

5.2 Contamination of Tip and Solution

As with any eye drop, 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.

5.3 Contact Lens Use

Patients should be advised not to wear a contact lens if their eye is red.

Olopatadine hydrochloride ophthalmic solution 0.2% should not be used to treat contact lens related irritation.

The preservative in olopatadine hydrochloride ophthalmic solution, 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 0.2% before they insert their contact lenses.

6 ADVERSE REACTIONS

Symptoms similar to cold syndrome and pharyngitis were reported at an incidence of approximately 10%.

The following adverse experiences have been reported in 5% or less of patients:

Ocular: blurred vision, burning or stinging, conjunctivitis, dry eye, foreign body sensation, hyperemia, hypersensitivity, keratitis, lid edema, pain and ocular pruritus.

Non-ocular: asthenia, back pain, flu syndrome, headache, increased cough, infection, nausea, rhinitis, sinusitis and taste perversion.

Some of these events were similar to the underlying disease being studied.

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Teratogenic Effects

Pregnancy Category C

Olopatadine was found not to be teratogenic in rats and rabbits. However, rats treated at 600 mg/kg/day, or 150,000 times the MROHD and rabbits treated at 400 mg/kg/day, or approximately 100,000 times the MROHD, during organogenesis showed a decrease in live fetuses. In addition, rats treated with 600 mg/kg/day of olopatadine during organogenesis showed a decrease in fetal weight. Further, rats treated with 600 mg/kg/day of olopatadine during late gestation through the lactation period showed a decrease in neonatal survival and body weight. 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.

8.3 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 0.2% is administered to a nursing mother.

8.4 Pediatric Use

Safety and effectiveness in pediatric patients below the age of 2 years have not been established.

8.5 Geriatric Use

No overall differences in safety and effectiveness have been observed between elderly and younger patients.

11 DESCRIPTION

Olopatadine hydrochloride ophthalmic solution USP 0.2% is a sterile ophthalmic solution containing olopatadine for topical administration to the eyes. Olopatadine hydrochloride, USP is a white or whitish, crystalline, water-soluble powder.

The structural formula of olopatadine hydrochloride, USP is:

STRUCTUAL FORMULA

C21H23NO3 • HCl M.W. 373.88

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 for topical ocular use only, contains 2.22 mg olopatadine hydrochloride, USP equivalent to 2 mg olopatadine and has the following inactive ingredients: dibasic sodium phosphate anhydrous, edetate disodium, povidone, sodium chloride; benzalkonium chloride 0.01% (preservative); 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.

12 CLINICAL PHARMACOLOGY

12.1 Mechanism of Action

Olopatadine is a mast cell stabilizer and a histamine H1 antagonist. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.

12.3 Pharmacokinetics

Systemic bioavailability data upon topical ocular administration of olopatadine hydrochloride ophthalmic solution are not available. Following topical ocular administration of olopatadine 0.15% ophthalmic solution in man, olopatadine was shown to have a 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 elimination half-life in plasma following oral dosing was 8 to 12 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.

13 NONCLINICAL TOXICOLOGY

13.1 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 μL drop size and a 50 kg person, these doses were approximately 150,000 and 50,000 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 approximately 100,000 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 approximately 15,000 times the MROHD level.

14 CLINICAL STUDIES

Results from clinical studies of up to 12 weeks duration demonstrate that olopatadine hydrochloride ophthalmic solution when dosed once a day is effective in the treatment of ocular itching associated with allergic conjunctivitis.

16 HOW SUPPLIED/STORAGE AND HANDLING

Olopatadine hydrochloride ophthalmic solution USP 0.2% is a clear, colorless to light yellow solution supplied in a white, low density polyethylene (LDPE) bottle with a white dropper tip, and a high density polyethylene cap.

2.5 mL fill in 5 mL bottle (NDC 0093-7684-32)

Storage

Store at 2° to 25°C (36° to 77°F)

KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.

17 PATIENT COUNSELING INFORMATION

17.1 Topical Ophthalmic Use Only

For topical ophthalmic administration only.

17.2 Sterility of Dropper Tip

Patients should be advised to not touch dropper tip to any surface, as this may contaminate the contents.

17.3 Concomitant Use of Contact Lenses

Patients should be advised not to wear a contact lens if their eyes are red. Patients should be advised that olopatadine hydrochloride ophthalmic solution should not be used to treat contact lens related irritation. Patients should also be advised to remove contact lenses prior to instillation of olopatadine hydrochloride ophthalmic solution. The preservative in olopatadine hydrochloride ophthalmic solution, benzalkonium chloride, may be absorbed by soft contact lenses. Lenses may be reinserted following administration of olopatadine hydrochloride ophthalmic solution.

Manufactured In Israel By:

Teva Pharmaceutical Ind. Ltd.

Jerusalem, 9777402, Israel

Manufactured For:

Teva Pharmaceuticals USA, Inc.

North Wales, PA 19454

Rev. A 2/2017

Package/Label Display Panel

image

Olopatadine Hydrochloride Ophthalmic Solution USP 0.2%, 2.5 mL Bottle, Carton Text

NDC 0093-7684-32

(Once a day)

Olopatadine

Hydrochloride

Ophthalmic

Solution USP

0.2%*

For Topical Application in the Eye

Sterile

Rx only

2.5 mL

TEVA

OLOPATADINE HYDROCHLORIDE 
olopatadine hydrochloride solution/ drops
Product Information
Product TypeHUMAN PRESCRIPTION DRUGItem Code (Source)NDC:0093-7684
Route of AdministrationOPHTHALMIC
Active Ingredient/Active Moiety
Ingredient NameBasis of StrengthStrength
OLOPATADINE HYDROCHLORIDE (UNII: 2XG66W44KF) (OLOPATADINE - UNII:D27V6190PM) OLOPATADINE2 mg  in 1 mL
Inactive Ingredients
Ingredient NameStrength
SODIUM PHOSPHATE, DIBASIC, ANHYDROUS (UNII: 22ADO53M6F)  
EDETATE DISODIUM (UNII: 7FLD91C86K)  
POVIDONE K30 (UNII: U725QWY32X)  
SODIUM CHLORIDE (UNII: 451W47IQ8X)  
BENZALKONIUM CHLORIDE (UNII: F5UM2KM3W7)  
WATER (UNII: 059QF0KO0R)  
Other Ingredients
Ingredient KindIngredient NameQuantity
May containHYDROCHLORIC ACID (UNII: QTT17582CB)  
May containSODIUM HYDROXIDE (UNII: 55X04QC32I)  
Packaging
#Item CodePackage DescriptionMarketing Start DateMarketing End Date
1NDC:0093-7684-321 in 1 CARTON05/04/201803/31/2022
12.5 mL in 1 BOTTLE, DROPPER; Type 0: Not a Combination Product
Marketing Information
Marketing CategoryApplication Number or Monograph CitationMarketing Start DateMarketing End Date
ANDAANDA09084805/04/201803/31/2022
Labeler - Teva Pharmaceuticals USA, Inc. (001627975)

Revised: 2/2017
 
Teva Pharmaceuticals USA, Inc.