LIVOSTIN™ 0.05% (levocabastine hydrochloride ophthalmic suspension) is a selective histamine H₁- receptor antagonist for topical ophthalmic use. Each mL contains 0.54 mg levocabastine hydrochloride equivalent to 0.5 mg levocabastine; 0.15 mg benzalkonium chloride; propylene glycol; polysorbate 80; dibasic sodium phosphate, anhydrous; monobasic sodium phosphate, monohydrate; disodium edetate; hydroxypropyl methylcellulose; and purified water. It has a pH of 6.0 to 8.0.

The chemical name for levocabastine hydrochloride is (-) trans-1-[cis-4-Cyano-4-(p-fluorophenyl) cyclohexyl]-3-methyl-4-phenylisonipecotic acid monohydrochloride.

Last updated on RxList: 12/8/2004

LIVOSTIN™ 0.05% (levocabastine hydrochloride ophthalmic suspension) is indicated for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis.

SHAKE WELL BEFORE USING.

The usual dose is one drop instilled in affected eyes four times per day.

LIVOSTIN™ 0.05% (levocabastine hydrochloride ophthalmic suspension), 2.5 mL, 5 mL, and 10 mL is provided in white, polyethylene dropper tip squeeze bottles.

Keep tightly closed when not in use. Do not use if the suspension has discolored.

Store at controlled room temperature 15º to 30º C (59º to 86º F). Protect from freezing.

NDC 58768-610-10 (10.0 mL)
NDC 58768-610-05 (5.0 mL)
NDC 58768-610-99 (2.5 mL)

Federal law prohibits dispensing without prescription.

Last updated on RxList: 12/8/2004

The most frequent adverse experiences reported with the use of LIVOSTIN™ 0.05% (levocabastine hydrochloride ophtalmic suspension) were mild, transient stinging and burning (29%) and headache (5%).

Other adverse experiences reported in approximately 1-3% of patients treated with LIVOSTIN™ were visual disturbances, dry mouth, fatigue, pharyngitis, eye pain/dryness, somnolence, red eyes, lacrimation/ discharge, cough, nausea, rash/erythema, eyelid edema, and dyspnea.

Last updated on RxList: 12/8/2004

For topical use only. Not for injection.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Levocabastine was not carcinogenic in male or female rats or in male mice when administered in the diet for up to 24 months. In female mice, levocabastine doses of 5,000 and 21,500 times the maximum recommended ocular human use level resulted in an increased incidence of pituitary gland adenoma and mammary gland adenocarcinoma possibly produced by increased prolactin levels. The clinical relevance of this finding is unknown with regard to the interspecies differences in prolactin physiology and the very low plasma concentrations of levocabastine following ocular administration.

Mutagenic potential was not demonstrated for levocabastine when tested in Ames' Salmonella reversion test or in Escherichia coli, Drosophila melanogaster, a mouse Dominant Lethal Assay or in rat Micronucleus test.

In reproduction studies in rats, levocabastine showed no effects on fertility at oral doses of 20 mg/kg/day (8,300 times the maximum recommended human ocular dose).

Pregnancy

Nursing Mothers

Based on determinations of levocabastine in breast milk after ophthalmic administration of the drug to one nursing woman, it was calculated that the daily dose of levocabastine in the infant was about 0.5 µg.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 12 have not been established.

Last updated on RxList: 12/8/2004

No information provided.

This product is contraindicated in persons with known or suspected hypersensitivity to any of its components. It should not be used while soft contact lenses are being worn.

Last updated on RxList: 12/8/2004

Levocabastine is a potent, selective histamine H₁- antagonist. Antigen challenge studies performed two and four hours after initial drug instillation indicated activity was maintained for at least two hours.

In an environmental study, LIVOSTIN™ 0.05% (levocabastine hydrochloride ophthalmic suspension) instilled four times daily was shown to be significantly more effective than its vehicle in reducing ocular itching associated with seasonal allergic conjunctivitis.

After instillation in the eye, levocabastine is systemically absorbed. However, the amount of systemically absorbed levocabastine after therapeutic ocular doses is low (mean plasma concentrations in the range of 1-2 ng/ mL).

Last updated on RxList: 12/8/2004

SHAKE WELL BEFORE USING.

To prevent contaminating the dropper tip and suspension, 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. Do not use if the suspension has discolored. Store at controlled room temperature. Protect from freezing.

Last updated on RxList: 12/8/2004

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.

LEVOCABASTINE - OPHTHALMIC

(lee-voh-cab-AST-een)

COMMON BRAND NAME(S): Livostin

USES: This medication is used to relieve eye symptoms (itching, redness, eyelid swelling, watering) due to seasonal allergies. Levocabastine belongs to a class of drugs known as antihistamines. It works by preventing the effects of a certain natural chemical (histamine).

This drug is not recommended for use in children younger than 12 years unless directed by the doctor.

HOW TO USE: To apply eye drops, wash your hands first. To avoid contamination, do not touch the dropper tip or let it touch your eye or any other surface.

If you are wearing contact lenses, remove them before using eye drops. Wait at least 15 minutes before replacing your contact lenses.

Use this medication usually 2 times a day or as directed by your doctor. Your doctor may then direct you to use this medication 3 to 4 times a day. Shake the bottle before each application. Tilt your head back, look upward, and pull down the lower eyelid to make a pouch. Hold the dropper directly over your eye and place 1 drop into the pouch. Look downward and gently close your eyes for 1 to 2 minutes. Place one finger at the 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. Repeat these steps for your other eye.

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

If you are using another kind of eye medication (e.g., drops or ointments), wait at least 5 to 10 minutes before applying other medications. Use eye drops before eye ointments to allow the drops to enter the eye.

Tell your doctor if your condition persists or worsens after 3 days.

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 very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any of the following symptoms of a serious allergic reaction: rash, itching, swelling, severe 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 using levocabastine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies.

After you apply this drug, your vision may become temporarily blurred. Use caution while driving, using machinery, or doing any other activity that requires clear vision. Limit alcoholic beverages.

During pregnancy, this medication should be used only when clearly needed. 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.

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 swallowing or 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. Canada residents can call a provincial poison control center.

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 at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Discard the bottle 1 month after first opening. 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.