LEVOCETIRIZINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H25ClN2O3
Molecular Weight	388.888
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC(=O)COCCN1CCN(CC1)[C@H](C2=CC=CC=C2)C3=CC=C(Cl)C=C3

InChI

InChIKey=ZKLPARSLTMPFCP-OAQYLSRUSA-N

InChI=1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26)/t21-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C21H25ClN2O3
Molecular Weight	388.888
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022064s028_022157s012lbl.pdfhttp://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf

Levocetirizine dihydrochloride is the R enantiomer of cetirizine hydrochloride, a racemic compound with antihistaminic properties. Levocetirizine is a third-generation non-sedative antihistamine indicated for the relief of symptoms associated with seasonal and perennial allergic rhinitis and uncomplicated skin manifestations of chronic idiopathic urticaria. It was developed from the second-generation antihistamine cetirizine. Levocetirizine was approved by the United States Food and Drug Administration on May 25, 2007 and is marketed under the brand XYZAL. Its principal effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H1-receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs. 6 nmol/L, respectively). The clinical relevance of this finding is unknown.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 316 Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18336052	Antagonist 2849		3.0 nM [Ki]
Histamine H1 receptor 316 Target ID: CHEMBL231 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022064s028_022157s012lbl.pdf	Inverse Agonist 85		6.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Seasonal allergic rhinitis 64 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf	Palliative	Approved 8583	XYZAL Approved Use Levocetirizine dihydrochloride tablet is a histamine H1-receptor antagonist indicated for: The relief of symptoms associated with seasonal and perennial allergic rhinitis (1.1, 1.2) The treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria (1.3) 1.1 Seasonal Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older. 1.2 Perennial Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with perennial allergic rhinitis in adults and children 6 years of age and older. 1.3 Chronic Idiopathic Urticaria Levocetirizine dihydrochloride tablets are indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older. Launch Date 2007
Perennial allergic rhinitis 47 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf	Palliative	Approved 8583	XYZAL Approved Use Levocetirizine dihydrochloride tablet is a histamine H1-receptor antagonist indicated for: The relief of symptoms associated with seasonal and perennial allergic rhinitis (1.1, 1.2) The treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria (1.3) 1.1 Seasonal Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older. 1.2 Perennial Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with perennial allergic rhinitis in adults and children 6 years of age and older. 1.3 Chronic Idiopathic Urticaria Levocetirizine dihydrochloride tablets are indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older. Launch Date 2007
Chronic idiopathic urticaria 11 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf	Palliative	Approved 8583	XYZAL Approved Use Levocetirizine dihydrochloride tablet is a histamine H1-receptor antagonist indicated for: The relief of symptoms associated with seasonal and perennial allergic rhinitis (1.1, 1.2) The treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria (1.3) 1.1 Seasonal Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with seasonal allergic rhinitis in adults and children 6 years of age and older. 1.2 Perennial Allergic Rhinitis Levocetirizine dihydrochloride tablets are indicated for the relief of symptoms associated with perennial allergic rhinitis in adults and children 6 years of age and older. 1.3 Chronic Idiopathic Urticaria Levocetirizine dihydrochloride tablets are indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 years of age and older. Launch Date 2007
Allergic rhinitis 104 Sources: https://www.drugs.com/monograph/levocetirizine-dihydrochloride.html	Primary	Approved 8583	XYZAL Approved Use For the temporary relief of nasal decongestiom due to the commomn cold, hay fever or other upper respiratpry allergies. Temporarily relieves nasal stuffiness. Decongests nasal passages: shrinks swollen membranes. Temporarily restores freer breathing through the nose. Helps decongest sinus openings and passages; temporarily relieves sinus congestion and pressure. Promotes nasal and/or sinus drainage. temporarily relieves sinus congestion and pressure. Launch Date 2007
Chronic Idiopathic Urticaria 3 Sources: https://www.drugs.com/monograph/levocetirizine-dihydrochloride.html	Primary	Approved 8583	XYZAL Approved Use For the temporary relief of nasal decongestiom due to the commomn cold, hay fever or other upper respiratpry allergies. Temporarily relieves nasal stuffiness. Decongests nasal passages: shrinks swollen membranes. Temporarily restores freer breathing through the nose. Helps decongest sinus openings and passages; temporarily relieves sinus congestion and pressure. Promotes nasal and/or sinus drainage. temporarily relieves sinus congestion and pressure. Launch Date 2007
Dermatitis 10 Sources: https://clinicaltrials.gov/show/NCT00375713	Primary	Phase III 665	XYZAL Approved Use Unknown

C_max

Value	Dose	Analyte	Population
512.25 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11564134	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.27 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.17 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
4136.4 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11564134	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.31 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.97 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
7.76 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11564134	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7.05 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.83 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	LEVOCETIRIZINE blood	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
4.5% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/11758635	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		LEVOCETIRIZINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
20 mg 1 times / day multiple, oral Highest studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1398-9995.2011.02606.x	unhealthy, 18–60 years Health Status: unhealthy Age Group: 18–60 years Sources: https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1398-9995.2011.02606.x	Sources: https://onlinelibrary.wiley.com/doi/epdf/10.1111/j.1398-9995.2011.02606.x
5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21502689 https://pubmed.ncbi.nlm.nih.gov/28081586	unhealthy, 48-64 years Health Status: unhealthy Age Group: 48-64 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21502689 https://pubmed.ncbi.nlm.nih.gov/28081586	Disc. AE: Hepatotoxicity... AEs leading to discontinuation/dose reduction: Hepatotoxicity (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/21502689 https://pubmed.ncbi.nlm.nih.gov/28081586
5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Age Group: > 12 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf	Disc. AE: Somnolence, Fatigue... AEs leading to discontinuation/dose reduction: Somnolence (2.3%) Fatigue (2.3%) Asthenia (2.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf

AEs

AE	Significance	Dose	Population
Hepatotoxicity	2 patients Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/21502689 https://pubmed.ncbi.nlm.nih.gov/28081586	unhealthy, 48-64 years Health Status: unhealthy Age Group: 48-64 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/21502689 https://pubmed.ncbi.nlm.nih.gov/28081586
Asthenia	2.3% Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Age Group: > 12 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf
Fatigue	2.3% Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Age Group: > 12 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf
Somnolence	2.3% Disc. AE	5 mg 1 times / day steady, oral Recommended Dose: 5 mg, 1 times / day Route: oral Route: steady Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf	unhealthy, > 12 years Health Status: unhealthy Age Group: > 12 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	inhibitor 2438 inducer 440	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2C19 2057 CYP2E1 1060 P-gp 1741	P-gp 2052 OATP1A2 67 OAT4 93 OATP1B1 503 OATP1B3 435	CYP1A2 832 UGT1A1 78

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
UGT1A1 303	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no

Drug as victim

Target	Modality	Activity
OAT4 93	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	likely
OATP1A2 67	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	likely
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	weak
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=19 Page: 19.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_PharmR.pdf#page=107 Page: 107.0

Sourcing

Vendor/Aggregator	ID	URL
3B Scientific (Wuhan) Corp	3B2-6286	http://www.3bsc.com/index/pro_info.php?id=115439
Alfa Chemistry	130018-77-8	https://www.alfa-chemistry.com/levocetirizine-cas-130018-77-8-item-289953.htm
Alichem	139002959	http://www.alichem.com/en/products/130018-77-8.html
AvaChem Scientific	1666B	http://www.avachem.com/productSearch.asp?1666B
BenchChem	B532939	https://www.benchchem.com/product/b532939
BLD Pharm	BD136222	http://www.bldpharm.com/products/130018-77-8.html
Boerchem	BC208946	http://www.boerchem.com/?product_35374.html
Capot Chemical	21319	http://www.capotchem.com/en/21319.htm
Capot Chemical	PubChem21319	http://www.capotchem.com/en/21319.htm
Chem Scene	CS-0012812	http://www.chemscene.com/130018-77-8.html
ChemMol	30104496	http://www.chemmol.com/chemmol/30104496.html
ChemMol	44003424	http://www.chemmol.com/chemmol/44003424.html
Chemspace	CSSS00020617386	https://chem-space.com/CSSS00020617386
Hairui	HR101445	http://www.hairuichem.com/en/product/130018-87-0.html
iChemical	EBD7151	http://www.ichemical.com/chemicals/cas-130018-77-8
Lab Network	LN01271259	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01271259
MedChem Express	HY-B0814	https://www.medchemexpress.com/r-cetirizine.html
OChem	6175	http://www.ocheminc.com/index.php?act=psearch&pid=18L778
Selleck Chemicals	S5864	http://www.selleckchem.com/products/levocetirizine.html
Smolecule	S532939	http://www.smolecule.com/products/s532939
THE BioTek	bt-273338	https://www.thebiotek.com/product/inhibitors/bt-273338
TripleBond	CL0022	http://www.triplebond-canada.com/prod/1689/
Yuhao Chemical	RT7047	http://www.chemyuhao.com/130018-77-8.html

PubMed

Title	Date	PubMed
Levocetirizine improves health-related quality of life and health status in persistent allergic rhinitis.	2006-10	16723217
Lichenoid eruption associated with the use of nebivolol.	2006-09	16896017
Stereoselective pharmacokinetics of cetirizine in the guinea pig: role of protein binding.	2006-09	16791848
Pathophysiology of nasal obstruction and meta-analysis of early and late effects of levocetirizine.	2006-08	16911353
Facial thermography is a sensitive tool to determine antihistaminic activity: comparison of levocetirizine and fexofenadine.	2006-08	16842390
Gateways to clinical trials.	2006-06	16845450
Chiral separation of cetirizine by capillary electrophoresis.	2006-06	16786474
Gateways to clinical trials.	2006-05	16801985
Effects of levocetirizine as add-on therapy to fluticasone in seasonal allergic rhinitis.	2006-05	16650054
Levocetirizine is an effective treatment in patients suffering from chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled, parallel, multicenter study.	2006-04	16650180
Levocetirizine in patients with chronic idiopathic urticaria: results of a multicenter clinical practice study.	2006-04	16625989
Gateways to clinical trials.	2006-03-17	16541195
Gateways to clinical trials.	2006-03	16636723
Levocetirizine in the treatment of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study.	2006-03	16445787
Changes in pH differently affect the binding properties of histamine H1 receptor antagonists.	2006-01-20	16388798
Fixed drug eruption due to levocetirizine.	2006-01-06	16394467
A review of the evidence from comparative studies of levocetirizine and desloratadine for the symptoms of allergic rhinitis.	2006-01	16490589
Effect of levocetirizine on the contraction induced by histamine on isolated rabbit bronchioles from precision-cut lung slices.	2006	16943691
Levocetirizine as treatment for symptoms of seasonal allergic rhinitis.	2006	16910288
Levocetirizine for treatment of immediate and delayed mosquito bite reactions.	2006	16874418
Levocetirizine: a review of its use in the management of allergic rhinitis and skin allergies.	2006	16740020
Familial aquagenic urticaria and bernard-soulier syndrome.	2006	16319487
Gateways to clinical trials.	2005-12	16395422
Desloratadine and levocetirizine improve nasal symptoms, airflow, and allergic inflammation in patients with perennial allergic rhinitis: a pilot study.	2005-12	16275616
Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines.	2005-09	16273334
Fixed drug eruption: a novel side-effect of levocetirizine.	2005-09	16135160
Efficacy and safety of levocetirizine on symptoms and health-related quality of life of children with perennial allergic rhinitis: a double-blind, placebo-controlled randomized clinical trial.	2005-08	16136768
A new antihistamine levocetirizine inhibits eosinophil adhesion to vascular cell adhesion molecule-1 under flow conditions.	2005-08	16120090
Levocetirizine: pharmacokinetics and pharmacodynamics in children age 6 to 11 years.	2005-08	16083790
A review of the evidence from comparative studies of levocetirizine and desloratadine for the symptoms of allergic rhinitis.	2005-07	16154477
A treatment for allergic rhinitis: a view on the role of levocetirizine.	2005-07	16004679
Levocetirizine has a longer duration of action on improving total nasal symptoms score than fexofenadine after single administration.	2005-07	15963090
Prediction of genotoxicity of chemical compounds by statistical learning methods.	2005-06	15962942
Potential of levocetirizine in the relief of nasal congestion.	2005-06	15924602
Costs associated with persistent allergic rhinitis are reduced by levocetirizine.	2005-06	15876309
Levocetirizine in children: evidenced efficacy and safety in a 6-week randomized seasonal allergic rhinitis trial.	2005-05	15853959
Bacillus clausii effects in children with allergic rhinitis.	2005-05	15813820
Levocetirizine in 1-2 year old children: pharmacokinetic and pharmacodynamic profile.	2005-04	15966463
Population pharmacokinetics of levocetirizine in very young children: the pediatricians' perspective.	2005-03	15787865
Levocetirizine improves nasal symptoms and airflow in patients with persistent allergic rhinitis: a pilot study.	2005-01	15745374
Retrospective population pharmacokinetics of levocetirizine in atopic children receiving cetirizine: the ETAC study.	2005-01	15606437
[Patient report: allergic rhinitis].	2005	16515333
Quantitative determination of cetirizine enantiomers in guinea pig plasma, brain tissue and microdialysis samples using liquid chromatography/tandem mass spectrometry.	2005	15912525
Pharmacological management of allergic rhinitis in the elderly: safety issues with oral antihistamines.	2005	15839718
Chronic urticaria: clinical aspects and focus on a new antihistamine, levocetirizine.	2004-12-31	15624746
Gateways to clinical trials.	2004-11	15632957
H1 histamine receptor mediates inflammatory responses in human keratinocytes.	2004-11	15536428
Levocetirizine improves quality of life and reduces costs in long-term management of persistent allergic rhinitis.	2004-10	15480324
Modern histamine H1-receptor antagonists in the unified airway.	2004-09	15540371
Chronic urticaria: aetiology, management and current and future treatment options.	2004	15516152

Patents

Sample Use Guides

In Vivo Use Guide

Allergic Rhinitis: 5 mg once daily; alternatively, 2.5 mg once daily may be adequate for some patients. Chronic Idiopathic Urticaria: 5 mg once daily; alternatively, 2.5 mg once daily may be adequate for some patients.

Route of Administration: Oral

In Vitro Use Guide

Equilibrium binding experiments on CHO cells expressing H1 receptor were performed using [3H]mepyramine as a radiolabel ligand.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:02:10 GMT 2025` Edited by `admin` on `Mon Mar 31 18:02:10 GMT 2025`
Record UNII	6U5EA9RT2O
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

XAZAL

Preferred Name

English

LEVOCETIRIZINE

Official Name

English

(R)-CETIRIZINE

Common Name

English

CETIRIZINE (R)-FORM

Common Name

English

CETIRIZINE, (R)-

Common Name

English

Levocetirizine [WHO-DD]

Common Name

English

LEVOCETIRIZINE [VANDF]

Common Name

English

LEVOCETIRIZINE [USAN]

Common Name

English

(-)-CETIRIZINE

Common Name

English

ACETIC ACID, (2-(4-((R)-(4-CHLOROPHENYL)PHENYLMETHYL)-1-PIPERAZINYL)ETHOXY)-

Common Name

English

LEVOCETIRIZINE [MART.]

Common Name

English

CETIRIZINE (R)-FORM [MI]

Common Name

English

ACETIC ACID, (2-(4-((R)-(4-CHLOROPHENYL)PHENYLMETHYL)-1-PIPERAZINYL)ETHOXY)

Common Name

English

CETIRIZINE, (-)-

Common Name

English

levocetirizine [INN]

Common Name

English

(2-{4-[(R)-(4-Chlorophenyl)phenylmethyl]piperazin-1-yl}ethoxy)acetic acid

Systematic Name

English

Classification Tree Code System Code

WHO-ATC

R06AE09