Molecule

Drug Groups

approved

Description

Levocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.

Indication

As an ophthalmic for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis. Also used as a nasal spray for allergic rhinitis.

Pharmacology

Levocabastine is a selective histamine H1-receptor antagonist exerting inhibitory effects on the release of chemical mediators from mast cells and on the chemotaxis of polymorphonuclear leukocytes and eosinophils. Both histamine and antigens induced conjunctivitis can be inhibited by levocabastine. Levocabastine can also reduce symptoms of allergic rhinitis by preventing an increase in vascular permeability of nasal mucosa.

Toxicity

Adverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.

Affected Organisms

Biotransformation

Mostly unchanged. 10 to 20% is metabolized to the acylglucuronide of levocabastine.

Absorption

After instillation in the eye, levocabastine is systemically absorbed, albeit at low levels.

Half Life

36 hours (after oral administration)

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