Livostin () ™ 0.05% (levocabastine hydrochloride ophthalmic suspension) is a selective histamine H-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 (–)--1-[-4-Cyano-4- (p-fluorophenyl)cyclohexyl]-3-methyl-4-phenylisonipecotic acid monohydrochloride, and is represented by the following chemical structure:
Levocabastine is a potent, selective histamine H-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).
SHAKE WELL BEFORE USING.
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 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).
The most frequent adverse experiences reported with the use of Livostin () ™ 0.05% (levocabastine hydrochloride ophthalmic 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.
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 15°to 30°C (59° to 86°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)
Rx Only
Levocabastine hydrochloride is an original product of Janssen Pharmaceutica Inc.
Mfd. by OMJ Pharmaceuticals, Inc.,
San Germán, P.R., 00683 for:
Novartis Ophthalmics, Duluth, GA 30097
5035-E
