レボセチリジン化学構造式

レボセチリジン

化学名:レボセチリジン

CAS番号.130018-77-8

英語名:Levocetirizine

CBNumberCB5712207

MFC21H25ClN2O3

MW388.89

MOL File130018-77-8.mol

别名

レボセチリジン

(R)-セチリジン

2-[2-[4-[(αR)-α-(4-クロロフェニル)ベンジル]ピペラジノ]エトキシ]酢酸

レボセチリジン物理性質

融点	205-208°C (dec.)
沸点	542.1±45.0 °C(Predicted)
比重(密度)	1.237±0.06 g/cm3(Predicted)
貯蔵温度	Sealed in dry,2-8°C
溶解性	DMSO: 78 mg/mL (200.57 mM);Ethanol: 78 mg/mL (200.57 mM)
酸解離定数(Pka)	3.46±0.10(Predicted)
水溶解度	Water: 78 mg/mL (200.57 mM)
BCS Class	3
CAS データベース	130018-77-8(CAS DataBase Reference)

安全性情報

HSコード

29335990

危険有害性情報のコード(GHS)

レボセチリジン化学特性,用途語,生産方法

効能
抗アレルギー薬, H1受容体拮抗薬
説明
The (R)-enantiomer of the second-generation antihistamine cetirizine, levocetirizine, was first introduced in Germany for seasonal allergic rhinitis (including ocular symptoms), perennial allergic rhinitis and chronic idiopathic urticaria. The dihydrochloride salt can be prepared in four steps from optically active 4-chlorobenzhydrylamine obtained by resolution of its racemate with (+)-tartaric acid. Levocetirizine (eutomer) is a 2-fold more potent H₁ antagonist than cetirizine whereas the other enantiomer (distomer) is 10-fold less potent compared to levocetirizine. Pharmacodynamic studies on healthy volunteers showed that compared to cetirizine, half the dose of levocetirizine (5 mg) was necessary to obtain similar inhibitory effects in the skin test of histamine-induced wheal and flare as well as on histamine-induced nasal congestion and nasal resistance. There was no evidence of chiral inversion of levocetirizine in vivo in several species including human. The daily dose of drug is rapidly and extensively absorbed in human. Interestingly, its volume of distribution (0.41 kg/L) is smaller than that of the distomer (0.60 kg/L). The low volume of distribution is considered as favorable for an antihistamine both in terms of efficacy and safety. Due to its high metabolic stability and lack of effect on the activities of the major CYP isoenzymes, levocetirizine is unlikely to cause interactions with other administered drugs. No clinically relevant effect on electrocardiograms of healthy volunteers was detected.
化学的特性
Off-White Solid
使用
A nonsedating type histamine H1-receptor antagonist. A major metabolite of Hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer. Antihystaminic.

レボセチリジン生産企業

130018-77-8, レボセチリジンキーワード

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レボセチリジン

危険有害性情報のコード(GHS)

レボセチリジン 化学特性,用途語,生産方法

レボセチリジン 生産企業

130018-77-8, レボセチリジン キーワード

レボセチリジン化学特性,用途語,生産方法

レボセチリジン生産企業

130018-77-8, レボセチリジンキーワード