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Accession NumberDB00341  (APRD00630)
TypeSmall Molecule

A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects. [PubChem]

CetirizinGermanNot Available
Prescription ProductsNot Available
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cetirizine Hydrochloridesolution5 mg/5mLoralAmneal Pharmaceuticals2009-10-07Not AvailableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cetirizine Hydrochloridetablet10 mgoralRugby Laboratories Inc2012-03-23Not AvailableUs
Cetirizinetablet10 mgoralNcs Health Care Of Ky, Inc Dba Vangard Labs2007-12-27Not AvailableUs
Cetirizine Hydrochloridetablet, film coated10 mgoralNorthstar Rx LLC2009-10-19Not AvailableUs
Cetirizineliquid5 mg/5mLoralRebel Distributors Corp2008-06-17Not AvailableUs
Cetirizine Hydrochloridetablet10 mgoralShopko Stores Operating Co., LLC2007-12-27Not AvailableUs
Leader All Day Allergytablet10 mgoralCardinal Health2007-12-27Not AvailableUs
Zyrtectablet, film coated10 mgoralMc Neil Consumer Healthcare Division Of Mc Neil Ppc, Inc.2008-10-01Not AvailableUs
Zyrtectablet, orally disintegrating10 mgoralMc Neil Consumer Healthcare Div. Mc Neil Ppc, Inc2014-01-20Not AvailableUs
Zyrteccapsule, liquid filled10 mgoralMc Neil Consumer Healthcare Div Mc Neil Ppc, Inc2010-02-08Not AvailableUs
Cetirizinetablet10 mgoralbryant ranch prepack2008-01-16Not AvailableUs
Kirklands Childrens Aller Tecliquid5 mg/5mLoralCostco Wholesale Company2009-08-14Not AvailableUs
Cetirizine Hydrochloridesolution5 mg/5mLoralAmneal Pharmaceuticals2009-10-07Not AvailableUs
Cetirizine Hydrochloridesolution5 mg/5mLoralAmneal Pharmaceuticals2009-10-07Not AvailableUs
Cetirizine Hydrochloridetablet5 mgoralAmneal Pharmaceuticals2010-01-21Not AvailableUs
Cetirizine Hydrochloridetablet10 mgoralAmneal Pharmaceuticals2010-01-21Not AvailableUs
Cetirizine Hydrochloride Hives Relieftablet5 mgoralAmneal Pharmaceuticals2010-01-21Not AvailableUs
Cetirizine Hydrochloride Hives Relieftablet10 mgoralAmneal Pharmaceuticals2010-01-21Not AvailableUs
Cetirizinetablet10 mgoralLife Line Home Care Services, Inc.2012-02-03Not AvailableUs
International Brands
AlerlisinNot Available
CetrynNot Available
FormistinNot Available
HitrizinNot Available
ReactineJohnson & Johnson Inc.
VirlixNot Available
ZirtekNot Available
ZyrlexNot Available
Brand mixtures
Brand NameIngredients
Zyrtec-DCetirizine + pseudoephedrine hydrochloride
SaltsNot Available
CAS number83881-51-0
WeightAverage: 388.888
Monoisotopic: 388.155370383
Chemical FormulaC21H25ClN2O3
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
Mass SpecNot Available
KingdomOrganic Compounds
ClassBenzene and Substituted Derivatives
Direct parentDiphenylmethanes
Alternative parentsChlorobenzenes; Aryl Chlorides; Piperazines; Diazinanes; Tertiary Amines; Enolates; Ethers; Carboxylic Acids; Polyamines; Organochlorides
Substituentschlorobenzene; aryl halide; 1,4-diazinane; piperazine; aryl chloride; tertiary amine; polyamine; carboxylic acid derivative; carboxylic acid; enolate; ether; organohalogen; amine; organonitrogen compound; organochloride
Classification descriptionThis compound belongs to the diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
IndicationFor the relief of symptoms associated with seasonal allergic rhinitis, perennial allergic rhinitis and the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria
PharmacodynamicsCetirizine, the active metabolite of the piperazine H1-receptor antagonist hydroxyzine, is used to treat chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis.
Mechanism of actionCetirizine competes with histamine for binding at H1-receptor sites on the effector cell surface, resulting in suppression of histaminic edema, flare, and pruritus. The low incidence of sedation can be attributed to reduced penetration of cetirizine into the CNS as a result of the less lipophilic carboxyl group on the ethylamine side chain.
Absorptionmean peak plasma concentration (Cmax) of 114 ng/mL at a time (Tmax) of 2.2 hours postdose was observed for cetirizine
Volume of distributionNot Available
Protein bindingVery high (93%) plasma protein binding
Route of eliminationNot Available
Half life8.3 hours
  • 53 mL/min [healthy]
ToxicitySomnolence (sleepiness or unusual drowsiness), restlessness, irritability
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.6863
Blood Brain Barrier + 0.7576
Caco-2 permeable - 0.5879
P-glycoprotein substrate Substrate 0.7862
P-glycoprotein inhibitor I Inhibitor 0.7364
P-glycoprotein inhibitor II Non-inhibitor 0.7624
Renal organic cation transporter Non-inhibitor 0.5232
CYP450 2C9 substrate Non-substrate 0.8408
CYP450 2D6 substrate Non-substrate 0.9116
CYP450 3A4 substrate Non-substrate 0.7
CYP450 1A2 substrate Non-inhibitor 0.9045
CYP450 2C9 substrate Non-inhibitor 0.907
CYP450 2D6 substrate Non-inhibitor 0.8885
CYP450 2C19 substrate Non-inhibitor 0.9025
CYP450 3A4 substrate Non-inhibitor 0.9465
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.6917
Ames test Non AMES toxic 0.7815
Carcinogenicity Non-carcinogens 0.9426
Biodegradation Not ready biodegradable 0.9974
Rat acute toxicity 2.6841 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.866
hERG inhibition (predictor II) Inhibitor 0.6517
  • Banner pharmacaps inc
  • Actavis mid atlantic llc
  • Amneal pharmaceuticals
  • Apotex inc
  • Aurobindo pharma ltd
  • Cypress pharmaceutical inc
  • Dr reddys laboratories ltd
  • Perrigo israel pharmaceuticals ltd
  • Ranbaxy laboratories ltd
  • Sun pharmaceutical industries inc
  • Taro pharmaceutical industries ltd
  • Teva pharmaceuticals usa
  • Vintage pharmaceuticals llc
  • Wockhardt ltd
  • Perrigo r and d co
  • Mcneil consumer healthcare div mcneil ppc inc
  • Caraco pharmaceutical laboratories ltd
  • Sandoz inc
  • Pfizer inc
  • Actavis elizabeth llc
  • Amneal pharmaceuticals ny llc
  • Cadista pharmaceuticals inc
  • Contract pharmacal corp
  • Mylan pharmaceuticals inc
  • Orchid healthcare
  • Torrent pharmaceuticals llc
  • Unichem laboratories ltd
  • Unique pharmaceutical laboratories
Dosage forms
Capsule, liquid filledoral10 mg
Liquidoral5 mg/5mL
Solutionoral5 mg/5mL
Tabletoral10 mg
Tabletoral5 mg
Tablet, film coatedoral10 mg
Tablet, orally disintegratingoral10 mg
Unit descriptionCostUnit
Cetirizine HCl 100 10 mg tablet Bottle259.71USDbottle
Cetirizine HCl 100 5 mg tablet Bottle259.71USDbottle
Zyrtec 10 mg tablet2.66USDtablet
Zyrtec 5 mg tablet2.66USDtablet
Zyrtec itchy eye 0.025% drops2.62USDml
Cetirizine hcl 5 mg chew tablet2.5USDtablet
Cetirizine hcl 10 mg tablet2.49USDtablet
Cetirizine hcl 5 mg tablet2.49USDtablet
Zyrtec-d tablet1.33USDtablet
Child's zyrtec chew tablet0.9USDtablet
CVS Pharmacy allergy relief 10 mg tablet0.74USDeach
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
CountryPatent NumberApprovedExpires (estimated)
United States64555331998-07-022018-07-02
Experimental Properties
melting point112.5 °CPhysProp
water solubility101 mg/LNot Available
logP2.8Not Available
Predicted Properties
Water Solubility0.0658ALOGPS
pKa (Strongest Acidic)3.6ChemAxon
pKa (Strongest Basic)7.79ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area53.01 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity106.87 m3·mol-1ChemAxon
Polarizability41.88 Å3ChemAxon
Number of Rings3ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
SpectraNot Available
Synthesis Reference

Manne Reddy, “Polymorphic forms of dihydrochloride salts of cetirizine and processes for preparation thereof.” U.S. Patent US20040186112, issued September 23, 2004.

General ReferenceNot Available
External Links
KEGG CompoundC07778
PubChem Compound2678
PubChem Substance46508368
Therapeutic Targets DatabaseDAP000323
Guide to Pharmacology1222
ATC CodesR06AE07R06AE09
AHFS Codes
  • 04:08.00
PDB EntriesNot Available
FDA labelshow(54.2 KB)
MSDSNot Available
Drug InteractionsSearched, but no interactions found.
Food InteractionsNot Available


1. Histamine H1 receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist


Name UniProt ID Details
Histamine H1 receptor P35367 Details


  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Christophe B, Carlier B, Gillard M, Chatelain P, Peck M, Massingham R: Histamine H1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kinetics. Eur J Pharmacol. 2003 May 30;470(1-2):87-94. Pubmed
  3. Tashiro M, Sakurada Y, Iwabuchi K, Mochizuki H, Kato M, Aoki M, Funaki Y, Itoh M, Iwata R, Wong DF, Yanai K: Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography. J Clin Pharmacol. 2004 Aug;44(8):890-900. Pubmed
  4. Tillement JP, Testa B, Bree F: Compared pharmacological characteristics in humans of racemic cetirizine and levocetirizine, two histamine H1-receptor antagonists. Biochem Pharmacol. 2003 Oct 1;66(7):1123-6. Pubmed
  5. Cavero I, Mestre M, Guillon JM, Heuillet E, Roach AG: Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans? Drug Saf. 1999;21 Suppl 1:19-31; discussion 81-7. Pubmed
  6. Tamura T, Masaki S, Ohmori K, Karasawa A: Effect of olopatadine and other histamine H1 receptor antagonists on the skin inflammation induced by repeated topical application of oxazolone in mice. Pharmacology. 2005 Dec;75(1):45-52. Epub 2005 Jun 7. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09