Levocetirizine Struktur

Levocetirizine

Bezeichnung:Levocetirizine

CAS-Nr130018-77-8

Englisch Name:Levocetirizine

CBNumberCB5712207

SummenformelC21H25ClN2O3

Molgewicht388.89

MOL-Datei130018-77-8.mol

Levocetirizine physikalisch-chemischer Eigenschaften

Schmelzpunkt	205-208°C (dec.)
Siedepunkt	542.1±45.0 °C(Predicted)
Dichte	1.237±0.06 g/cm3(Predicted)
storage temp.	Sealed in dry,2-8°C
Löslichkeit	DMSO: 78 mg/mL (200.57 mM);Ethanol: 78 mg/mL (200.57 mM)
pka	3.46±0.10(Predicted)
Wasserlöslichkeit	Water: 78 mg/mL (200.57 mM)
BCS Class	3
CAS Datenbank	130018-77-8(CAS DataBase Reference)

Sicherheit

HS Code

29335990

Gefahreninformationscode (GHS)

Levocetirizine Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Chemische Eigenschaften
Off-White Solid
Originator
Sepracor (US)
Verwenden
Labeled cetirizine, intended for use as an internal standard for the quantification of cetirizine by GC- or LC-mass spectrometry.
Verwenden
H1 antihistamine, antiallergic
Verwenden
A nonsedating type histamine H1-receptor antagonist. A major metabolite of Hydroxyzine. Pharmacological activity resides primarily in the (R)-isomer. Antihystaminic.
Definition
ChEBI: 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic acid is a diarylmethane.
Trademarks
Xusal
Clinical Use
Antihistamine:
Symptomatic relief of allergy such as hay fever, urticaria

Levocetirizine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

130018-77-8, Levocetirizine Verwandte Suche:

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