ロラタジン 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
用途
ロラタジン（Loratadine）は、持続性選択ヒスタミンH1受容体拮抗薬で、アレルギー性鼻炎や蕁麻疹?皮膚湿疹に用いられる。
効能
抗アレルギー薬, H1受容体拮抗薬
商品名
クラリチン (バイエル薬品); クラリチン (バイエル薬品); クラリチン (バイエル薬品); クラリチン (バイエル薬品)
説明
Loratadine is a non-sedating antihistamine indicated for use in allergic rhinitis and chronic
urticaria. Its major advantage over other non-sedating antihistamines such as astemizole
and terfenadine is its very fast onset of action. Loratadine is claimed not to cross the
blood-brain barrier.
化学的特性
White Crystalline Solid
使用
Loratadine, is used as a peripheral histamine H1 receptor agonist. It is also used as an orally active antiallergic agent. It is an important raw material and intermediate used in Organic Synthesis, Pharmaceuticals, Agrochemicals and Dyestuff.
適応症
Loratadine (Claritin) is a long-acting, potent peripheral H1 blocker with minimal
sedative effects. It does not appear to have the same adverse cardiac effects as
the other nonsedating H1 antihistamines. It is indicated for allergic rhinitis and
chronic urticaria.
一般的な説明
Loratadine, 4-(8-chloro-5,6-dihydro-11Hbenzo[5,6]-cyclohepta[1,2-b]pyridin-l 1-ylidene-1-carboxylic acid ethyl ester, is a white to off-white powder insoluble in water but very soluble in acetone, alcohols, and chloroform. Loratadine is structurally related to the antihistamines azatadine and cyproheptadine, and to some tricyclic antidepressants. It differs from azatadine, in that a neutral carbamate group has replaced the basic tertiary amino moiety, and a phenyl ring has been substituted with a chlorine atom. Loratadine is a selective peripheral H1-antihistamine with a receptor-binding profile like that of the other members of this series, except that it has more antiserotonergic activity. Thus, it produces no substantial CNS or autonomic side effects or cardiac toxicity.
Loratadine displays potency comparable with that of astemizole and greater than that of terfenadine. Loratadine is indicated for the relief of nasal and nonnasal symptoms of seasonal allergic rhinitis. In the presence of a CYP3A4 inhibitor ketoconazole, loratadine is metabolized to descarboethoxyloratadine predominantly by CYP2D6.
生物活性
Peripheral histamine H 1 receptor antagonist (K i = 35 nM); devoid of central effects. Orally active antiallergic agent.
臨床応用
Loratadine is related to the first-generation tricyclic antihistamines and to
antidepressants. It is nonsedating, and neither it nor its major metabolite, desloratadine
(descarboethoxyloratadine), is associated with the potentially cardiotoxic effects reported for
terfenadine and astemizole. On chronic dosing, the AUC (plasma concentration–time curve)
for the metabolite is greater than that for the parent drug, and its half-life is longer.
ロラタジン 上流と下流の製品情報
原材料
準備製品