デスロラタジン 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
デスロラタジン (Desloratadine)は、三環系H1-抗ヒスタミン薬で、アレルギーの治療に使いられる。第二世代抗ヒスタミン薬のロラタジンの活性代謝物（英語版）。
デスロラタジンは、アレルギー性鼻炎や鼻詰まりの治療に用いられる。ロラタジンの主な代謝物質で、これらは有効性と安全性において同様である。
新たな適応はにきびで、イソトレチノインの安価な補助剤として、あるいは場合によって維持療法とか、単剤治療で用いられる。
用途
デスロラタジンは、アレルギー性鼻炎や鼻詰まりの治療に用いられる。ロラタジンの主な代謝物質で、これらは有効性と安全性において同様である。
新たな適応はにきびで、イソトレチノインの安価な補助剤として、あるいは場合によって維持療法とか、単剤治療で用いられる。
効能
抗アレルギー薬, 鎮痒薬, H1受容体拮抗薬
商品名
デザレックス (MSD)
説明
Desloratadine is a second generation of tricyclic antihistamine. It is a H1-receptor antagonist which has anti-inflammatory activity. Its affinity to the H1 receptor is higher than most other H1-receptor antagonists. Desloratadine works by blocking a certain natural substance (histamine) which is produced during an allergic reaction. Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.
Desloratadine is used to treat nasal and non-nasal symptoms (watery eyes, runny nose, itching eyes/nose, sneezing, and itching) of seasonal allergic rhinitis. It is also used to relieve chronic itching caused by hives.
化学的特性
Beige Solid
使用
Desloratadine has been used to test its effect on embryoid body development in in vitro gastrulation model of P19C5 stem cells. It has also been used as an antihistamine mimic in rats and to treat lung cancer (A549) and glioblastoma (U87) cells in various cellular studies.
定義
ChEBI: Loratadine in which the ethoxycarbonyl group attached to the piperidine ring is replaced by hydrogen. The major metabolite of loratidine, desloratadine is an antihistamine which is used for the symptomatic relief of allergic conditions including rhinitis
nd chronic urticaria. It does not readily enter the central nervous system, so does not cause drowsiness.
適応症
Desloratadine (Clarinex) is an active metabolite of loratadine. A 5 mg
daily dose has been shown to be effective. There is no evidence that it offers
any advantage over loratadine.
Fexofenadine (like its parent compound terfenadine) may rarely promote
cardiac arrhythmias (24). No significant difference in efficacy has been noted
in the nonsedating H1 blockers. Combinations of nonsedating antihistamines
in the morning and sedating antihistamines in the evening may be more cost
effective than increasing doses of the nonsedating agent.
一般的な説明
Desloratadine, 8-chloro-6,11-dihydro-11-(4-piperdinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine(Clarinex) is a white to off-white powder that is slightlysoluble in water, but very soluble in ethanol and propyleneglycol. It is the proposed active metabolite loratadine and hasa very similar receptor binding and safety profile. It is indicated for the symptomatic relief of pruritus andreduction in the number and size of hives in chronic idiopathicurticaria patients 6 months of age and older and for therelief of the nasal and nonnasal symptoms of perennial allergicrhinitis (in patients 6 months of age and older) and seasonalallergic rhinitis (in patients 2 years of age and older).
Desloratadine is extensively metabolized to 3-hydroxydesloratadine,also an active metabolite, which is subsequentlyglucuronidated . The cytochrome enzymesresponsible for the formation of 3-hydroxydesloratadinehave not been reported. Coadministration ofdesloratadine with CYP3A4 inhibitors results in marginalincreases in plasma concentrations of desloratadine and3-hydroxydesloratadine, but no significant changes in safetyor efficacy. The mean elimination half-life of desloratadineis about 6 hours, and the drug and its metabolites areeliminated in the urine and feces.
参考文献
[1] https://www.drugbank.ca
[2] Raif S. Geha, Eli O. Meltzer (2001) Desloratadine: A new, nonsedating, oral antihistamine, The Journal of Allergy and Clinical Immunology,107, 751-762
デスロラタジン 上流と下流の製品情報
原材料
8-クロロ-6,11-ジヒドロ-11-(1-メチル-4-ピペリジニリデン)-5H-ベンゾ[5,6]シクロヘプタ[1,2-B]ピリジン
水酸化ナトリウム
クロロぎ酸エチル
2H-Pyrano[3,2-b]pyridine,3,4-dihydro-4-methylene-(9CI)
Loratadine ketone
N-TERT-ブチル-3-メチルピコリンアミド
100643-73-0
1-Methylpiperdin-4-ylmagnesium chloride, 0.50 M in THF
ロラタジン
8-Chloro-6,11-dihydro-11-(1-methyl-4-piperidinyl)-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ol
3-[2-(3-CHLORO-PHENYL)-ETHYL]-PYRIDINE-2-CARBOXYLIC ACID TERT-BUTYLAMIDE
3-[2-(3-クロロフェニル)エチル]ピリジン-2-カルボニトリル
8-クロロ-5,6-ジヒドロ-11H-ベンゾ[5,6]シクロヘプタ[1,2-b]ピリジン-11-オン
準備製品