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Information @ a Glance

General

  • Loratidine is a new generation antihistamine drug, used for treating various skin and other allergies.
  • Since Loratadine represents a “new generation” of antihistamine, it does not cross the blood-brain barrier and does not cause drowsiness.
  • Loratidine has a much longer lasting effect when compared to other antihistamines in use.
  • It is (H1) receptor antagonist, penetrates very poorly into the central system, hence is devoid of CNS depressant effects. Structurally it is related to azatidine. Loratidine also suppresses mast cell mediator release.
  • Loratadine, a member of the piperidine class of antihistamines, has gotten relatively positive reviews in particular for the treatment of feline itchy skin.

Process

  • Loratadine, a long-acting tricyclic antihistamine, undergoes extensive first-pass metabolism in the liver to form its major metabolite
    desloratadine, which also possesses antihistamine activity and is subject to further metabolism.
  • A gastro retentive controlled release system of loratadine was formulated to increase the residence time in stomach and to modulate the release behaviour of the drug.
  • The preparation of colloidal particles of different morphologies, including spheres, of two drugs, loratadine and danazol, has been described.
  • The synthesis of two contaminants of Loratadine, generated when the product is formulated as a syrup.

Application

  • The combination of montelukast and loratadine, 2 mediator receptor antagonists, should be more efficacious than either used alone in the treatment of allergic rhinitis.
  • The nonsedating antihistamine loratadine has an effect rapidly on activating delayedrectifier K1 channel (Kv1.5) cloned from human heart and stably expressed in HEK 293 cells or mouse Ltk2 cells.
  • Loratadine (LOR) is an orally active H1 receptor antagonist. It has been widely used because of its efficacy in treating allergic disorders without significant central and autonomic nervous side effects such as sedation and anticholinergic properties.

Market

  • India is set to rule the generics market for Loratidine, an anti-allergy drug, in the US.
  • Loratidine sales in the US, at $ 3.2 billion, account for 80 per cent of global sales.
  • According to pharma industry sources, loratidine has been seeing an annual growth of about 31 per cent and its getting into OTC would bring down the prices, while pumping up the volumes.

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