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Levocabastine
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.
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).
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. HOW SUPPLIED 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.
Federal law prohibits dispensing
without prescription.
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.
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.
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