LEVOCETIRIZINE DIHYDROCHLORIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H25ClN2O3.2ClH
Molecular Weight	461.81
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure of LEVOCETIRIZINE DIHYDROCHLORIDE

Structure Search

SMILES

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

InChI

InChIKey=PGLIUCLTXOYQMV-GHVWMZMZSA-N

InChI=1S/C21H25ClN2O3.2ClH/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);2*1H/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 315 Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18336052	Antagonist 2778		3.0 nM [Ki]
Histamine H1 receptor 315 Target ID: CHEMBL231 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/022064s028_022157s012lbl.pdf	Inverse Agonist 80		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 8429	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 8429	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 8429	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 100 Sources: https://www.drugs.com/monograph/levocetirizine-dihydrochloride.html	Primary	Approved 8429	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 8429	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 656	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 1737 inhibitor 1587 inducer 781	inhibitor 1767 inducer 389	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2C19 1478 CYP2E1 882 P-gp 1461	P-gp 1537 OATP1A2 62 OAT4 78 OATP1B1 406 OATP1B3 350	CYP1A2 701 UGT1A1 69

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=4 Page: 4.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
UGT1A1 254	inducer 1573 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 78	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	likely
OATP1A2 62	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	likely
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2007/022064s000_ClinPharmR.pdf#page=20 Page: 20.0	weak
CYP3A4 1737	substrate 3367 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 1647	inhibitor 1626 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
Chronic urticaria: aetiology, management and current and future treatment options.	2004	15516152
Gateways to clinical trials.	2004 Nov	15632957
H1 histamine receptor mediates inflammatory responses in human keratinocytes.	2004 Nov	15536428
Chronic urticaria: clinical aspects and focus on a new antihistamine, levocetirizine.	2004 Nov-Dec	15624746
Levocetirizine improves quality of life and reduces costs in long-term management of persistent allergic rhinitis.	2004 Oct	15480324
Modern histamine H1-receptor antagonists in the unified airway.	2004 Sep	15540371
[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
Levocetirizine in 1-2 year old children: pharmacokinetic and pharmacodynamic profile.	2005 Apr	15966463
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
Gateways to clinical trials.	2005 Dec	16395422
Desloratadine and levocetirizine improve nasal symptoms, airflow, and allergic inflammation in patients with perennial allergic rhinitis: a pilot study.	2005 Dec	16275616
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
A review of the evidence from comparative studies of levocetirizine and desloratadine for the symptoms of allergic rhinitis.	2005 Jul	16154477
A treatment for allergic rhinitis: a view on the role of levocetirizine.	2005 Jul	16004679
Levocetirizine has a longer duration of action on improving total nasal symptoms score than fexofenadine after single administration.	2005 Jul	15963090
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
Costs associated with persistent allergic rhinitis are reduced by levocetirizine.	2005 Jun	15876309
Population pharmacokinetics of levocetirizine in very young children: the pediatricians' perspective.	2005 Mar	15787865
Levocetirizine in children: evidenced efficacy and safety in a 6-week randomized seasonal allergic rhinitis trial.	2005 May	15853959
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 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
Levocetirizine is an effective treatment in patients suffering from chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled, parallel, multicenter study.	2006 Apr	16650180
Levocetirizine in patients with chronic idiopathic urticaria: results of a multicenter clinical practice study.	2006 Apr	16625989
Pathophysiology of nasal obstruction and meta-analysis of early and late effects of levocetirizine.	2006 Aug	16911353
Facial thermography is a sensitive tool to determine antihistaminic activity: comparison of levocetirizine and fexofenadine.	2006 Aug	16842390
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 Jan-Feb	16541195
Gateways to clinical trials.	2006 Jun	16845450
Chiral separation of cetirizine by capillary electrophoresis.	2006 Jun	16786474
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
Levocetirizine improves health-related quality of life and health status in persistent allergic rhinitis.	2006 Oct	16723217
Lichenoid eruption associated with the use of nebivolol.	2006 Sep	16896017
Stereoselective pharmacokinetics of cetirizine in the guinea pig: role of protein binding.	2006 Sep	16791848

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 DIHYDROCHLORIDE

Official Name

English

Levocetirizine dihydrochloride [WHO-DD]

Common Name

English

LEVOCETIRIZINE DIHYDROCHLORIDE [USAN]

Common Name

English

LEVOCETIRIZINE HYDROCHLORIDE [MART.]

Common Name

English

CETIRIZINE (R)-FORM DIHYDROCHLORIDE

Common Name

English

LEVOCETIRIZINE DIHYDROCHLORIDE [ORANGE BOOK]

Common Name

English

LEVOCETIRIZINE DIHYDROCHLORIDE [VANDF]

Common Name

English

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

Common Name

English

CETIRIZINE (R)-FORM DIHYDROCHLORIDE [MI]

Common Name

English

LEVOCETIRIZINE HYDROCHLORIDE [JAN]

Common Name

English

LEVOCETIRIZINE DIHYDROCHLORIDE [USP MONOGRAPH]

Common Name

English

UCB-28556

Code

English

XYZAL

Brand Name

English

LEVOCETIRIZINE DIHYDROCHLORIDE [USP-RS]

Common Name

English

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

Systematic Name

English

NSC-758898

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C29578