PATANOL® (olopatadine hydrochloride ophthalmic solution) 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 PATANOL 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 purified water. It has a pH of approximately 7 and an osmolality of approximately 300 mOsm/kg.

Last updated on RxList: 3/17/2008

PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1 % is indicated for the treatment of the signs and symptoms of allergic conjunctivitis.

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

PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is supplied as follows:

5 mL in plastic DROP-TAINER© dispenser.

5 mL: NDC 0065-0271-05

Storage: Store at 39°F-77°F (4°C-25°C)

ALCON LABORATORIES, INC. Fort Worth, Texas 76134 USA. Revised: August 2002. FDA Rev date: 4/17/2003

Last updated on RxList: 3/17/2008

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.

No information provided.

Last updated on RxList: 3/17/2008

PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% is for topical use only and not for injection or oral use.

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 PATANOL (olopatadine hydrochloride ophthalmic solution) 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.

Last updated on RxList: 3/17/2008

No information provided.

PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1 % is contraindicated in persons with a known hypersensitivity to olopatadine hydrochloride or any components of PATANOL.

Last updated on RxList: 3/17/2008

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 PATANOL 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 PATANOL, 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.

Last updated on RxList: 3/17/2008

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. PATANOL® (olopatadine hydrochloride ophthalmic solution) 0.1 % should not be used to treat contact lens related irritation. The preservative in PATANOL, 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 PATANOL (olopatadine hydrochloride ophthalmic solution) 0.1% before they insert their contact lenses.

Last updated on RxList: 3/17/2008

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

OLOPATADINE - OPHTHALMIC SOLUTION

(oh-low-PAT-uh-deen)

COMMON BRAND NAME(S): Patanol

USES: This medication is an antihistamine used to treat itching and redness in the eyes due to allergies.

This medication is not recommended for the treatment of eye irritation due to wearing contact lenses.

HOW TO USE: Apply this medication in the affected eye(s) usually once or twice a day as directed by your doctor, depending on the brand of eye drops you are prescribed.

Wash your hands before each use. To avoid contamination, do not touch the dropper tip or let it touch your eye or any other surface.

The preservative in this product may be absorbed by contact lenses. If you wear contact lenses, remove them before using this medication and keep them out of your eyes for at least 10 minutes after each dose.

Tilt your head back, look upward and pull down the lower eyelid to make a pouch. Hold the dropper directly over your eye and apply the prescribed number of drops. Look downward and gently close your eye for 1 to 2 minutes. Place one finger at the inside corner of your eye near the nose and apply gentle pressure. This will prevent the medication from draining out. Try not to blink and do not rub your eye.

Do not rinse the dropper. Replace the dropper cap after each use.

Use this medication regularly in order to get the most benefit from it. Remember to use it at the same time(s) each day. Continue using it for the full time prescribed.

Wait at least 5 minutes in between applying this medicine and any other eye medication (e.g., drops or ointments) you may be using. Use eye drops before eye ointments to allow the eye drops to enter the eye.

Inform your doctor if your condition persists or worsens.

SIDE EFFECTS: Headache, blurred vision, burning/stinging/redness/dryness of the eye, eyelid swelling, or a feeling as if something is in your eye may occur. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction include: rash, itching, swelling, dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before taking olopatadine hydrochloride, tell your doctor or pharmacist if you are allergic to it; or to the preservative (benzalkonium chloride); or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: contact lens use.

Use caution engaging in activities requiring clear vision such as driving or using machinery because your vision may be temporarily blurred or unstable after applying this drug.

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.

Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: This medicine may be harmful if swallowed. If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents can call their local poison control center directly.

NOTES: Do not share this medication with others.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store the US product between 39-77 degrees F (4-25 degrees C) away from light and moisture. Do not store in the bathroom.

Store the Canadian product between 39-86 degrees F (4-30 degrees C) away from light and moisture. Do not store in the bathroom.

Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.