OLOPATADINE HYDROCHLORIDE- olopatadine hydrochloride solution/ drops
Mylan Pharmaceuticals Inc.
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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 USP is a white to yellowish, 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 USP equivalent to 1 mg olopatadine.
Preservative: benzalkonium chloride 0.01%. Inactives: dibasic sodium phosphate anhydrous, sodium chloride, hydrochloric acid and/or sodium hydroxide (to 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 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 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, 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, 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 μL 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.
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, pruritus, 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 in a 5 mL sterile white opaque LDPE bottle with sterile open white opaque LDPE nozzle and sterile HDPE white cap.
5 mL fill
NDC 0378-8023-35
carton of one bottle
Storage
Store at 4° to 25°C (39° to 77°F).
INSTRUCTIONS FOR USE
Olopatadine Hydrochloride Ophthalmic Solution USP 0.1%
Before you use Olopatadine Hydrochloride Ophthalmic Solution USP 0.1% for the first time:
- 1.
- Check to make sure that the tamper evident ring between the bottle and the cap is not broken (See Figure A). If the tamper evident ring is broken or missing, contact your pharmacist.
- 1.
- Tear off the tamper evident ring (See Figure B).
- 1.
- To open the bottle, remove the cap by turning it in the counterclockwise direction (See Figure C).
This Instructions for Use has been approved by the U.S. Food and Drug Administration.
Manufactured for:
Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.
Manufactured by:
Micro Labs Limited
Bangalore – 560 099, INDIA
M.L. No.: KTK/28/357/2006
Revised: 7/2017
MCR:OLOPHOS1:R2
PRINCIPAL DISPLAY PANEL – 0.1%
NDC 0378-8023-35
Olopatadine
HCl
Ophthalmic
Solution, USP
0.1%
For Use in the
Eyes Only
Rx only 5 mL
Sterile
Each mL contains:
Active: Olopatadine
hydrochloride USP 1.11 mg,
equivalent to olopatadine 1 mg.
Preservative: benzalkonium
chloride 0.01%
Inactives: dibasic sodium
phosphate anhydrous, sodium
chloride, hydrochloric acid
and/or sodium hydroxide
(to adjust pH) and water
for injection.
Usual Dosage: See
accompanying prescribing
information.
Store at 4º to 25ºC
(39º to 77ºF).
Keep this and all medication
out of the reach of children.
This package is not child
resistant.
Warning: Do not touch
dropper tip to any surface,
as this may contaminate
the solution.
Manufactured for:
Mylan Pharmaceuticals Inc.
Morgantown, WV 26505 U.S.A.
Made in India
MCR:8023:1C:R2
Mylan.com
M.L. No.: KTK/28/357/2006
| OLOPATADINE HYDROCHLORIDE
olopatadine hydrochloride solution/ drops |
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| Labeler - Mylan Pharmaceuticals Inc. (059295980) |