Levocetirizine dihydrochloride

Names

[ Name ]:
Levocetirizine dihydrochloride

[Synonym ]:
Xyzall
EINECS 200-659-6
(R)-Cetirizine Dihydrochloride
Levocetirizine dihydrochloride
(2-{4-[(R)-(4-Chlorphenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)essigsäuredihydrochlorid
MFCD07366507
(-)-Cetirizine dihydrochloride
Levocetirizine 2HCl
Xusal
(2-{4-[(R)-(4-Chlorophenyl)(phenyl)methyl]-1-piperazinyl}ethoxy)acetic acid dihydrochloride
2-[2-[4-[(R)-(4-Chlorophenyl)phenylmethyl]piperazin-1-yl]ethoxy]acetic Acid Dihydrochloride
Xyzal
acide (2-{4-[(R)-(4-chlorophényl)(phényl)méthyl]pipérazin-1-yl}éthoxy)acétique dichlorhydrate
acetic acid, [2-[4-[(R)-(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, dihydrochloride
Acetic acid, 2-[2-[4-[(R)-(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]-, hydrochloride (1:2)
(2-{4-[(R)-(4-Chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid dihydrochloride

Biological Activity

[Description]:

Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Endocrinology

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[In Vivo]

Levocetirizine (0.4 mg/kg; oral administration; male Sprague-Dawley rats) treatment shows that the Cmax, AUC0-t , AUC0-∞ and t1/2 are 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively in Sprague-Dawley rats[1]. Animal Model: 30 male Sprague-Dawley rats (8 weeks old; 200-250 g)[1] Dosage: 0.4 mg/kg Administration: Oral administration (Pharmacokinetic Analysis) Result: The Cmax, AUC0-t , AUC0-∞ and t1/2 were 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively.

[References]

[1]. Lohar P, et al. Simultaneous bioanalysis and pharmacokinetic interaction study of acebrophylline, levocetirizine and pranlukast in Sprague-Dawley rats. Biomed Chromatogr. 2019 Dec;33(12):e4672.

Chemical & Physical Properties

[ Boiling Point ]:
542.1ºC at 760 mmHg

[ Melting Point ]:
215-220ºC

[ Molecular Formula ]:
C₂₁H₂₇Cl₃N₂O₃

[ Molecular Weight ]:
461.810

[ Flash Point ]:
281.6ºC

[ Exact Mass ]:
460.108734

[ PSA ]:
53.01000

[ LogP ]:
4.62800

[ Storage condition ]:
room temp

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H400

[ Precautionary Statements ]:
P273

[ Hazard Codes ]:
Xn,N

[ Risk Phrases ]:
22-50/53

[ Safety Phrases ]:
60-61

[ RIDADR ]:
UN 3077 9 / PGIII

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933599090

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

Rapid chiral separation of racemic cetirizine in human plasma using subcritical fluid chromatography-tandem mass spectrometry.

J. Pharm. Biomed. Anal. 117 , 380-9, (2015)

A method for fast chiral separation of cetirizine and quantitation of levocetirizine in human plasma using subcritical fluid chromatography with tandem mass spectrometry was developed and validated. T...

Development and characterization of pharmacokinetic parameters of fast-dissolving films containing levocetirizine.

Sci. Pharm. 80 , 779-87, (2012)

A fast-dissolving film containing levocetirizine, a non-sedative antihistamine drug, was developed using pullulan, xanthan gum, propylene glycol, and tween 80 as the base materials. The drug content o...