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

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

Levocetirizine is the active enantiomer of cetirizine. It is inverse agonist of H1 receptors. Levocetirizine hydrochloride was approved for treatment of Allergic Rhinitis and Chronic Idiopathic Urticaria.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 313 Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18336052	Antagonist 2760		3.0 nM [Ki]
Histamine H1 receptor 313 Target ID: CHEMBL231 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022064s028_022157s012lbl.pdf	Inverse Agonist 79		6.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Seasonal allergic rhinitis 63 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf	Palliative	Approved 8360	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 1.18005118E12
Perennial allergic rhinitis 47 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf	Palliative	Approved 8360	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 1.18005118E12
Chronic idiopathic urticaria 11 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022064s030,022157s013lbl.pdf	Palliative	Approved 8360	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 1.18005118E12
Allergic rhinitis 100 Sources: https://www.drugs.com/monograph/levocetirizine-dihydrochloride.html	Primary	Approved 8360	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 1.1799648E12
Chronic Idiopathic Urticaria 3 Sources: https://www.drugs.com/monograph/levocetirizine-dihydrochloride.html	Primary	Approved 8360	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 1.18031044E12
Dermatitis 10 Sources: https://clinicaltrials.gov/show/NCT00375713	Primary	Phase III 663	XYZAL Approved Use Unknown

C_max

Value	Dose	Analyte	Population
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
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
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

AUC

Value	Dose	Analyte	Population
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
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
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

T_1/2

Value	Dose	Analyte	Population
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
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
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

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 n = 13 Health Status: unhealthy Condition: severe urticaria Age Group: 18–60 years Population Size: 13 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 n = 2 Health Status: unhealthy Condition: chronic urticaria Age Group: 48-64 years Sex: M Population Size: 2 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 n = 428 Health Status: unhealthy Age Group: > 12 years Sex: M+F Population Size: 428 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 n = 2 Health Status: unhealthy Condition: chronic urticaria Age Group: 48-64 years Sex: M Population Size: 2 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 n = 428 Health Status: unhealthy Age Group: > 12 years Sex: M+F Population Size: 428 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 n = 428 Health Status: unhealthy Age Group: > 12 years Sex: M+F Population Size: 428 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 n = 428 Health Status: unhealthy Age Group: > 12 years Sex: M+F Population Size: 428 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/022064lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709 inhibitor 1579 inducer 768	inhibitor 1752 inducer 383	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 CYP2C19 1463 CYP2E1 876 P-gp 1437	P-gp 1527 OATP1A2 61 OAT4 76 OATP1B1 403 OATP1B3 347	CYP1A2 689 UGT1A1 69

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP1A2 1673	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2E1 964	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
P-gp 1626	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
UGT1A1 254	inducer 1542 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 76	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	likely
OATP1A2 61	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	likely
CYP2D6 1193	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
OATP1B1 403	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
OATP1B3 347	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
P-gp 1527	substrate 3326 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	weak
CYP3A4 1709	substrate 3326 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 1632	inhibitor 1613 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
BLD Pharm	BD136222	http://www.bldpharm.com/products/130018-77-8.html
BenchChem	B532939	https://www.benchchem.com/product/b532939
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
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
iChemical	EBD7151	http://www.ichemical.com/chemicals/cas-130018-77-8

PubMed

Title	Date	PubMed
Blood distribution of levocetirizine, a new non-sedating histamine H1-receptor antagonist, in humans.	2002 Dec	12685505
Comparative pharmacology of H1 antihistamines: clinical relevance.	2002 Dec 16	12517581
Acute allergy reaction after posterior sub-Tenon's triamcinolone injection in the treatment of intermediate uveitis in the asthmatic patient.	2003	15314977
Chronic urticaria: a role for newer immunomodulatory drugs?	2003	12688835
Driving ability after acute and sub-chronic administration of levocetirizine and diphenhydramine: a randomized, double-blind, placebo-controlled trial.	2003 Aug	12721777
Assessing satisfaction with desloratadine and fexofenadine in allergy patients who report dissatisfaction with loratadine.	2003 Aug 13	12917016
[Safety of new antihistamines].	2003 Jun	14524292
[Clinical aspects of anti-inflammatory action of antihistamines].	2003 Jun	14524290
Acute and subchronic effects of levocetirizine and diphenhydramine on memory functioning, psychomotor performance, and mood.	2003 Mar	12642847
Levocetirizine: new preparation. Me-too: simply the active enantiomer of cetirizine.	2003 Oct	14619884
Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists.	2003 Oct 1	14505791
Gateways to clinical trials.	2003 Sep	14571286
Chronic urticaria: aetiology, management and current and future treatment options.	2004	15516152
Levocetirizine better protects than desloratadine in a nasal provocation with allergen.	2004 Apr	15100671
Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans.	2004 Aug	15312146
Antihistamines: do they work? Further well-controlled trials involving larger samples are needed.	2004 Aug	15245363
Comparative clinical efficacy, onset and duration of action of levocetirizine and desloratadine for symptoms of seasonal allergic rhinitis in subjects evaluated in the Environmental Exposure Unit (EEU).	2004 Feb	15055856
Levocetirizine: the allergist's arsenal grows larger.	2004 Jul	15212608
Single and short-term dosing effects of levocetirizine on adenosine monophosphate bronchoprovocation in atopic asthma.	2004 Jul	15206990
Large-scale overproduction, functional purification and ligand affinities of the His-tagged human histamine H1 receptor.	2004 Jul	15206929
Levocetirizine improves nasal obstruction and modulates cytokine pattern in patients with seasonal allergic rhinitis: a pilot study.	2004 Jun	15196286
Antihistamines and driving ability: evidence from on-the-road driving studies during normal traffic.	2004 Mar	15049392
Levocetirizine: a new selective H1 receptor antagonist for use in allergic disorders.	2004 May	15319796
Gateways to clinical trials.	2004 Nov	15632957
Chronic urticaria: clinical aspects and focus on a new antihistamine, levocetirizine.	2004 Nov-Dec	15624746
Comparison of the effects in the nose and skin of a single dose of desloratadine and levocetirizine over 24 hours.	2004 Oct	15345913
[Patient report: allergic rhinitis].	2005	16515333
Pharmacological management of allergic rhinitis in the elderly: safety issues with oral antihistamines.	2005	15839718
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 Aug	16136768
A new antihistamine levocetirizine inhibits eosinophil adhesion to vascular cell adhesion molecule-1 under flow conditions.	2005 Aug	16120090
Levocetirizine: pharmacokinetics and pharmacodynamics in children age 6 to 11 years.	2005 Aug	16083790
Levocetirizine improves nasal symptoms and airflow in patients with persistent allergic rhinitis: a pilot study.	2005 Jan	15745374
Retrospective population pharmacokinetics of levocetirizine in atopic children receiving cetirizine: the ETAC study.	2005 Jan	15606437
Prediction of genotoxicity of chemical compounds by statistical learning methods.	2005 Jun	15962942
Potential of levocetirizine in the relief of nasal congestion.	2005 Jun	15924602
Population pharmacokinetics of levocetirizine in very young children: the pediatricians' perspective.	2005 Mar	15787865
Bacillus clausii effects in children with allergic rhinitis.	2005 May	15813820
Histamine H1 receptor occupancy and pharmacodynamics of second generation H1-antihistamines.	2005 Sep	16273334
Fixed drug eruption: a novel side-effect of levocetirizine.	2005 Sep	16135160
Fixed drug eruption due to levocetirizine.	2005 Sep-Oct	16394467
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 is an effective treatment in patients suffering from chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled, parallel, multicenter study.	2006 Apr	16650180
A review of the evidence from comparative studies of levocetirizine and desloratadine for the symptoms of allergic rhinitis.	2006 Jan	16490589
Changes in pH differently affect the binding properties of histamine H1 receptor antagonists.	2006 Jan 20	16388798
Gateways to clinical trials.	2006 Mar	16636723
Levocetirizine in the treatment of chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled study.	2006 Mar	16445787
Gateways to clinical trials.	2006 May	16801985
Effects of levocetirizine as add-on therapy to fluticasone in seasonal allergic rhinitis.	2006 May	16650054
Lichenoid eruption associated with the use of nebivolol.	2006 Sep	16896017

Patents

Sample Use Guides

In Vivo Use Guide

Adults and children 12 years of age and older: 5 mg once daily in the evening. Children 6 to 11 years of age: 2.5 mg once daily in the evening. Children 6 months to 5 years of age: 1.25 mg (1/2 teaspoon oral solution)[2.5mL] once daily in the evening.

Route of Administration: Oral

In Vitro Use Guide

Eosinophils isolated from normal subjects were pre-incubated with a concentration range of levocetirizine (10(-6)-10(-10) m) or negative dilution control. Levocetirizine significantly inhibited resting eosinophil adhesion to recombinant human vascular cell adhesion molecule-1 (rhVCAM-1) with maximal effect at 10(-8) M with an EC(50) of 10(-9) m.

Name

Type

Language

LEVOCETIRIZINE

Official Name

English

(R)-CETIRIZINE

Common Name

English

CETIRIZINE (R)-FORM

Common Name

English

XAZAL

Brand 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