Antiallergic drug Desloratadine Raw Materials Powder

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Desloratadine Powder Usage and Synthesis.

Including chronic idiopathic urticaria, perennial allergic rhinitis and other allergic diseases. In addition, it can relieve the symptoms of cold urticaria.

1. Treatment of allergic rhinitis (AR) With increasing knowledge of specific mediators such as histamine, prostaglandin D2, leukotriene C4,IL-3,IL-8,ICAM-1 that play a unique role in early and late allergic reactions, many treatment routes targeting the allergic cascade have emerged. Desloratadine can effectively inhibit the release of inflammatory mediators at multiple sites in this cascade, thereby preventing various symptoms of AR (such as nasal congestion, etc.).

2. Clinical trials for the treatment of chronic idiopathic urticaria (CIU) have shown that desloratadine can reduce the frequency of itching in CIU patients by 75% within 6h. The clinical trial of desloratadine on CIU led by the First Affiliated Hospital of Nanjing Medical University and the Dermatology Department of Huashan Hospital Affiliated to Fudan University showed that after 2 and 4 weeks of application of the first dose of desloratadine, patients' scores could be improved by up to 80% in terms of maximum wind mass size, number of wind masses, itching and total symptom score. The results indicated that desloratadine had a good effect on CIU.

Uses and functions of Desloratadine.

1. Anti-allergic effect Desloratadine is highly selective and specifically binds to H1 receptor. Among known antihistamines, desloratadine has the strongest binding ability to H1 receptor and has significant anti-H1 receptor effect. It was 4 times more potent than loratadine in inhibiting histamine-induced foot swelling in mice. Desloratadine inhibits the release of inflammatory cytokines from stimulated human mast cells and basophils at the nanomolar level, including IL-3,IL-6,TNF-α,GM-CSF, etc. The inhibitory effect is stronger than dexamethasone and cetirizine.

2. Desloratadine has its own activity, good absorption, and less than 30 minutes of effective time. The maximum blood concentration was reached about 3h after oral administration, the Cmax was 3.98 ng·mL-1 and the clearance rate was 114 ~ 201L·h-1. A clinical time-of-effect study in patients with allergic rhinitis demonstrated that desloratadine acted faster than existing antihistamines, with an average time of 28.45min, compared with 1h for loratadine and midazolastine and 2h for cetirizine. The half-life is about 24h, and the effect is long-lasting.

In vitro study of Desloratadine.

Desloratadine is a competitive antagonist of carbachocholine-induced iris smooth muscle contraction in isolated rabbits with pA2 of 6.67. Desloratadine binds to the human H1 receptor and has a Ki value of 0.87 nM in tritium-labeled mepiramine. Desloratadine (100 nM to 10 μM) inhibits the production of the cytokines IL-4 and IL-13 in both IGE-mediated and non-IGE-mediated human basophils. Desloratadine (300 nM to 100 μM) inhibits IgE mediated and non-IGE mediated histamine release from human peripheral blood basophils.

In eosinophilic cells taken from patients with allergic rhinitis or allergic asthma, Desloratadine (0.1 μM to 10 μM) inhibited platelet activator induced eosinophilic chemotaxis and TNF-α-induced eosinophilic cell adhesion. Desloratadine (1 μM to 10 μM) dose-dependent inhibited the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μm-10 μM) inhibited IL-13 secretion in basophilic granulocytes in a dose-dependent manner. Desloratadine (10 μM) pretreatment resulted in a substantial reduction of induced cytokines in cultured basophils. In cultured basophilic granulocytes, Desloratadine (10 μM) pretreatment caused an approximately 80% reduction in IL-4 and anti-ige activation. Desloratadine (10 μM) also inhibited histamine and IL-4 protein secretion into the upper clear night of cultured basophils.

Product method of Bulk Desloratadine Powder.

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