Levocabastine Synthesis Essay

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.

Structured Indications
Pharmacodynamics

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.

Mechanism of action

Levocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin 2 receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.

Absorption

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

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

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

Route of elimination
Not Available
Half life

36 hours (after oral administration)

Clearance
Not Available
Toxicity

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

Affected organisms
Pathways
Pharmacogenomic Effects/ADRs
Not Available

MDPI and ACS Style

Kang, S.K.; Nam, D.H.; Ahn, J.; Lee, J.; Sim, J.; Lee, J.; Suh, Y.-G. Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist. Molecules2017, 22, 1971.

AMA Style

Kang SK, Nam DH, Ahn J, Lee J, Sim J, Lee J, Suh Y-G. Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist. Molecules. 2017; 22(11):1971.

Chicago/Turabian Style

Kang, Sung K.; Nam, Dong H.; Ahn, Jaeseung; Lee, Jaemin; Sim, Jaehoon; Lee, Jeeyeon; Suh, Young-Ger. 2017. "Practical and Sustainable Synthesis of Optically Pure Levocabastine, a H1 Receptor Antagonist." Molecules 22, no. 11: 1971.

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