Cetirizine is a selective Histamine-1 antagonist drug used in allergic rhinitis and chronic urticaria.

Brand Names
Aller-tec, Aller-tec D, Quzyttir, Reactine, Wal Zyr 24 Hour Allergy, Wal Zyr D, Wal-zyr, Zerviate, Zyrtec, Zyrtec-D
Generic Name
DrugBank Accession Number

Cetirizine, also commonly known as Zyrtec, is an orally active second-generation histamine H1 antagonist proven effective in the treatment of various allergic symptoms, such as sneezing, coughing, nasal congestion, hives, and other symptoms 1, 2.

One of the most common uses for this drug is for a condition called allergic rhinitis. The prevalence of allergic rhinitis in the United States is about 15% according to physician diagnoses, and up to 30%, according to self-reported nasal symptoms. Allergic rhinitis is associated with multiple missed or unproductive days at work and school, problems with sleep, and other difficulties with day to day activities for many individuals 3. Furthermore, some antihistamine agents that are used to treat this condition cause undesirable, sedating effects 4.

Cetirizine is one of the first second-generation H1 antihistamines (SGAHs) formulated to selectively inhibit the H1 receptor without sedating effects 2.

Small Molecule
Average: 388.888
Monoisotopic: 388.155370383
Chemical Formula
  • Cetirizin
  • Cetirizina
  • Cetirizine
  • Cetirizinum



Seasonal Allergic Rhinitis: Indicated for the relief of symptoms associated with seasonal allergic rhinitis caused by allergens such as ragweed, grass and tree pollens in adults and children 2 years of age and above. Symptoms treated effectively include sneezing, rhinorrhea, nasal pruritus, ocular pruritus, tearing, and redness of the eyes Label.

Perennial allergic rhinitis: This drug is indicated for the relief of symptoms associated with perennial allergic rhinitis due to allergens including dust mites, animal dander, and molds in adults and children 6 months of age and older. Symptoms treated effectively include sneezing, rhinorrhea, postnasal discharge, nasal pruritus, ocular pruritus, and tearing Label.

Chronic urticaria: Cetirizine is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older. It markedly reduces the occurrence, severity, and duration of hives and significantly reduces pruritus Label.

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Symptomatic treatment ofChronic idiopathic urticaria••••••••••••
Used in combination for symptomatic treatment ofFlu caused by influenzaCombination Product in combination with: Phenylephrine (DB00388), Acetaminophen (DB00316)••••••••••••••••••• ••• ••••••••
Used in combination for symptomatic treatment ofHay feverMixture Product in combination with: Pseudoephedrine (DB00852)••• •••
Symptomatic treatment ofPerennial allergic rhinitis••••••••••••••••••• •• ••••• •••••••• ••••••• ••••••• •• ••••• •••• ••••
Used in combination for symptomatic treatment ofRespiratory allergyCombination Product in combination with: Pseudoephedrine (DB00852)••• •••
Contraindications & Blackbox Warnings
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General effects and respiratory effects

Cetirizine, the active metabolite of the piperazine H1-receptor antagonist hydroxyzine, minimizes or eliminates the symptoms of chronic idiopathic urticaria, perennial allergic rhinitis, seasonal allergic rhinitis, allergic asthma, physical urticaria, and atopic dermatitis. The clinical efficacy of cetirizine for allergic respiratory diseases has been well established in numerous trials Label.

Effects on urticaria/anti-inflammatory effects

It has anti-inflammatory properties that may play a role in asthma management 1. There is evidence that cetirizine improves symptoms of urticaria. Marked clinical inhibition of a wheal and flare response occurs in infants, children as well as adults within 20 minutes of one oral dose and lasts for 24 h 1. Concomitant use of cetirizine reduces the duration and dose of topical anti-inflammatory formulas used for the treatment of atopic dermatitis 1.

Mechanism of action

Cetirizine, a metabolite of hydroxyzine, is an antihistamine drug. Its main effects are achieved through selective inhibition of peripheral H1 receptors. The antihistamine activity of cetirizine has been shown in a variety of animal and human models. In vivo and ex vivo animal models have shown insignificant anticholinergic and antiserotonergic effects. In clinical studies, however, dry mouth was found to be more frequent with cetirizine than with a placebo. In vitro receptor binding studies have demonstrated no detectable affinity of cetirizine for histamine receptors other than the H1 receptors. Studies with radiolabeled cetirizine administration in the rat have demonstrated insignificant penetration into the brain. Ex vivo studies in the mouse have shown that systemically administered cetirizine does not occupy cerebral H1 receptors significantly Label.

AHistamine H1 receptor

Cetirizine was rapidly absorbed with a time to maximum concentration (Tmax) of about 1 hour after oral administration of tablets or syrup formulation in adult volunteers Label. Bioavailability was found to be similar between the tablet and syrup dosage forms. When healthy study volunteers were given several doses of cetirizine (10 mg tablets once daily for 10 days), a mean peak plasma concentration (Cmax) of 311 ng/mL was measured Label.

Effect of food on absorption

Food had no effect on cetirizine exposure (AUC), however, Tmax was delayed by 1.7 hours and Cmax was decreased by 23% in the fed state Label.

Volume of distribution

Apparent volume of distribution: 0.44 +/- 0.19 L/kg 5.

Protein binding

The mean plasma protein binding of cetirizine is 93% Label.


A mass balance clinical trial comprised of 6 healthy male study volunteers showed that 70% of the administered radioactivity was measured in the urine and 10% in the feces after cetirizine administration. About 50% of the radioactivity was measured in the urine as unchanged cetirizine. Most of the rapid increase in peak plasma radioactivity was related to the parent drug, implying a low level of first pass metabolism. This prevents potential interactions of cetirizine with drugs interacting with hepatic cytochrome enzymes 1.

Cetirizine is metabolized partially by oxidative O-dealkylation to a metabolite with insignificant antihistaminic activity. The enzyme or enzymes responsible for this step in cetirizine metabolism have not yet been identified Label.

Route of elimination

Mainly eliminated in the urine Label, 1.

Between 70 – 85% of an orally administered dose can be found in the urine and 10 – 13% in the feces 1.


Plasma elimination half-life is 8.3 hours Label.


Apparent total body clearance: approximately 53 mL/min Label.

Cetirizine is mainly eliminated by the kidneys 1, Label. Dose adjustment is required for patients with moderate to severe renal impairment and in patients on hemodialysis Label.

Adverse Effects
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Oral LD50 (rat): 365 mg/kg; Intraperitoneal LDLO (mouse): 138 mg/kg; Oral TDLO (rat): 50 mg/kg; Oral TDLO (mouse): 0.1 mg/kg MSDS.

Carcinogenesis and mutagenesis: In a 2-year carcinogenicity study in rats, cetirizine was not shown to be carcinogenic at dietary doses up to 20 mg/kg (approximately 15 times the maximum recommended daily oral dose in adults). In a 2-year carcinogenicity study in mice, cetirizine administration lead to an incidence of benign liver tumors in males at a dietary dose of 16 mg/kg (approximately 6 times the maximum recommended daily oral dose in adults). The clinical significance of these findings during long-term use of cetirizine is unknown at this time Label.

Cetirizine was not mutagenic in the Ames test, and not clastogenic in the human lymphocyte assay, the mouse lymphoma assay, and in vivo micronucleus test in rats Label.

Impairment of fertility

In a fertility and reproduction study in mice, cetirizine did not negatively impact fertility at an oral dose of 64 mg/kg (approximately 25 times the maximum recommended daily oral dose in adults) Label.

Pregnancy Category B:

In mice, rats, and rabbits, cetirizine was not teratogenic at oral doses up to 96, 225, and 135 mg/kg, respectively (approximately 40, 180 and 220 times the maximum recommended daily oral dose in adults). There are no adequate and well-controlled studies in pregnant women. Because animal studies are not always predictive of human response, cetirizine should be used in pregnancy only if clearly needed Label.

Use in breastfeeding/nursing

Cetirizine has been reported to be excreted in human breast milk. The use of cetirizine in nursing mothers is not recommended Label.

Cetirizine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Cetirizine is combined with 1,2-Benzodiazepine.
AbacavirCetirizine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AceclofenacAceclofenac may decrease the excretion rate of Cetirizine which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Cetirizine which could result in a higher serum level.
AcetazolamideThe risk or severity of CNS depression can be increased when Cetirizine is combined with Acetazolamide.
Food Interactions
  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.


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Product Ingredients
IngredientUNIICASInChI Key
Cetirizine hydrochloride64O047KTOA83881-52-1PGLIUCLTXOYQMV-UHFFFAOYSA-N
Product Images
International/Other Brands
Alerlisin / Cetryn / Formistin / Hitrizin / Virlix / Zirtek / Zyrlex
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CetirizineTablet20 mgOralSanis Health Inc2021-11-30Not applicableCanada flag
CetirizineTablet20 mgOralSivem Pharmaceuticals Ulc2023-07-20Not applicableCanada flag
CetirizineTablet20 mgOralPro Doc Limitee2016-06-13Not applicableCanada flag
Cetirizine Hydrochloride TabletsTablet20 mgOralVita Health Products IncNot applicableNot applicableCanada flag
M-cetirizineTablet20 mgOralMantra Pharma Inc2021-04-20Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ag-cetirizineTablet20 mgOralAngita Pharma Inc.2022-05-11Not applicableCanada flag
Apo-cetirizineTablet20 mgOralApotex Corporation2016-04-22Not applicableCanada flag
Bio-cetirizineTablet20 mgOralBiomed Pharma2023-06-19Not applicableCanada flag
Cetirizine HydrochlorideTablet10 mg/1OralDirect Rx2016-12-22Not applicableUS flag
Cetirizine HydrochlorideTablet10 mg/1OralRemedy Repack2010-12-012010-12-02US flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
24 Hour AllergyLiquid5 mg/5mLOralMeijer Distribution2008-04-162017-07-13US flag
24 Hour AllergyTablet, film coated10 mg/1OralMeijer Distribution Inc1997-07-07Not applicableUS flag
24 Hour AllergyCapsule10 mg/1OralWalgreens2018-09-14Not applicableUS flag
24 Hour AllergyCapsule, liquid filled10 mg/1OralMeijer Distribution Inc2020-06-02Not applicableUS flag
24 Hour AllergyCapsule, liquid filled10 mg/1OralMEIJER, INC.2022-03-08Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
12 Hour Allergy DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralMeijer Distribution Inc1988-07-15Not applicableUS flag
12 Hour Allergy DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, film coated, extended releaseOralMeijer Distribution Inc2020-04-07Not applicableUS flag
ACERADOX® GCetirizine hydrochloride (5 mg) + Acetaminophen (500 mg) + Caffeine (30 mg) + Phenylephrine hydrochloride (10 mg)Capsule, coatedOralLABORATORIOS DEMAC LTDA.2019-02-28Not applicableColombia flag
ACIDRINEDJARABE.Cetirizine hydrochloride (0.1 g) + Phenylephrine hydrochloride (0.2 g)SyrupOralC.I. FARMACAPSULAS S.A.S2006-11-102020-10-01Colombia flag
ALCADOL®GRIPACetirizine hydrochloride (5 mg) + Ibuprofen (200 mg) + Phenylephrine hydrochloride (10 mg)Capsule, liquid filledOral2015-12-11Not applicableColombia flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Allexpert 24HR Antihistamine Cetirizine Hydrochloride Oral SolutionCetirizine hydrochloride (1 mg/1mL)SolutionOralBowong Technology (ShenZhen) Co.,Ltd2024-04-17Not applicableUS flag
ZyrtecCetirizine hydrochloride (10 mg/1)TabletOralPhysicians Total Care, Inc.1996-12-182009-01-18US flag
ZyrtecCetirizine hydrochloride (5 mg/1)TabletOralPhysicians Total Care, Inc.2002-12-162009-01-18US flag


ATC Codes
S01GX12 — CetirizineR06AE07 — Cetirizine
Drug Categories
Chemical TaxonomyProvided by Classyfire
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Organic compounds
Super Class
Benzene and substituted derivatives
Sub Class
Direct Parent
Alternative Parents
N-alkylpiperazines / Chlorobenzenes / Aralkylamines / Aryl chlorides / Trialkylamines / Amino acids / Monocarboxylic acids and derivatives / Dialkyl ethers / Carboxylic acids / Azacyclic compounds
show 5 more
1,4-diazinane / Amine / Amino acid / Amino acid or derivatives / Aralkylamine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Carbonyl group
show 22 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
monocarboxylic acid, ether, monochlorobenzenes, piperazines (CHEBI:3561)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

CAS number
InChI Key
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid


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 References
  1. Portnoy JM, Dinakar C: Review of cetirizine hydrochloride for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Jan;5(1):125-35. doi: 10.1517/14656566.5.1.125 . [Article]
  2. Zhang L, Cheng L, Hong J: The clinical use of cetirizine in the treatment of allergic rhinitis. Pharmacology. 2013;92(1-2):14-25. doi: 10.1159/000351843. Epub 2013 Jul 18. [Article]
  3. Wheatley LM, Togias A: Clinical practice. Allergic rhinitis. N Engl J Med. 2015 Jan 29;372(5):456-63. doi: 10.1056/NEJMcp1412282. [Article]
  4. Church MK, Church DS: Pharmacology of antihistamines. Indian J Dermatol. 2013 May;58(3):219-24. doi: 10.4103/0019-5154.110832. [Article]
  5. Spicak V, Dab I, Hulhoven R, Desager JP, Klanova M, de Longueville M, Harvengt C: Pharmacokinetics and pharmacodynamics of cetirizine in infants and toddlers. Clin Pharmacol Ther. 1997 Mar;61(3):325-30. doi: 10.1016/S0009-9236(97)90165-X. [Article]
Human Metabolome Database
KEGG Compound
PubChem Compound
PubChem Substance
Therapeutic Targets Database
Guide to Pharmacology
GtP Drug Page
RxList Drug Page
Drugs.com Drug Page
FDA label
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Clinical Trials

Clinical Trials
4CompletedBasic ScienceHypoxia, Altitude1
4CompletedOtherAllergic Reaction2
4CompletedOtherAllergic Rhinitis (AR)1
4CompletedOtherPerennial Allergic Rhinitis (PAR) / Seasonal Allergic Rhinitis3


  • 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
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • Apotex Inc.
  • Apotheca Inc.
  • AQ Pharmaceuticals Inc.
  • Atlantic Biologicals Corporation
  • Aurobindo Pharma Ltd.
  • Bryant Ranch Prepack
  • Caraco Pharmaceutical Labs
  • Cardinal Health
  • CVS Pharmacy
  • Cypress Pharmaceutical Inc.
  • Direct Dispensing Inc.
  • Direct Pharmaceuticals Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • EZ-EM Inc.
  • H.J. Harkins Co. Inc.
  • J.B. Chemicals & Pharmaceuticals
  • Kaiser Foundation Hospital
  • L Perrigo Co.
  • Lake Erie Medical and Surgical Supply
  • McNeil Laboratories
  • Medvantx Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nucare Pharmaceuticals Inc.
  • Ohm Laboratories Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Perrigo Co.
  • Pfizer Inc.
  • Pharmacy Service Center
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Qualitest
  • Ranbaxy Laboratories
  • Redpharm Drug
  • Resource Optimization and Innovation LLC
  • Sandoz
  • Southwood Pharmaceuticals
  • Teva Pharmaceutical Industries Ltd.
  • US Pharmaceutical Group
  • Vangard Labs Inc.
  • Warner Chilcott Co. Inc.
  • Wockhardt Ltd.
Dosage Forms
Capsule, extended releaseOral
SolutionOral1 mg/ml
SyrupOral100 mg
Capsule, liquid filledOral10 mg
SyrupOral0.1 g
CapsuleOral10 mg/1
SyrupOral1 mg/1
TabletOral10.0 mg/1
SolutionOral100 mg
Tablet, coatedOral
SyrupOral0.060 g
Powder, for solutionOral
SolutionOral0.1 g
Tablet, chewableOral
Tablet, film coatedOral
SolutionOral10 MG/ML
SyrupOral1 MG/ML
LozengeOral10 mg/1
SolutionOral1000000 mg
SolutionOral10 mg
TabletOral1000000 mg
Tablet, coatedOral1000000 mg
SolutionOral0.102 g
SolutionOral1 g
LiquidOral5 mg/5mL
Tablet; tablet, film coatedOral10 MG
Tablet, film coated, extended releaseOral
Capsule, liquid filledOral10 mg/1
SolutionOral1 mg/1mL
SolutionOral5 mg/5mL
Solution / drops; suspension / dropsOral
SyrupOral1 mg/1mL
SyrupOral5 mg/5mL
TabletOral10 mg/1
TabletOral5 mg/1
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
SolutionNasal; Oral
SyrupOral0.1 % w/v
Tablet, film coatedOral
SuspensionOral1 mg/1mL
Tablet, chewableOral2.5 mg/1
Tablet, coatedOral10 mg/1
SolutionOral100.00 mg
Solution / drops; suspension / drops10 MG/ML
TabletOral50000000 mg
Solution / drops; suspension / drops
Capsule, liquid filledOral1000000 mg
SyrupOral0.119 g
Capsule, coatedOral500 mg
Capsule, coatedOral
InjectionIntravenous10 mg/1mL
Solution / dropsOral
SyrupOral5 mg / 5 mL
TabletOral5 mg
TabletOral20 mg
Tablet, chewableOral10 mg
Tablet, chewableOral5 mg
Tablet, effervescent
Tablet, orally disintegratingOral10 mg
TabletOral10 mg
SolutionOral10.000 mg
SolutionOral0.01 g
Capsule, liquid filledOral
Tablet, soluble
SolutionOral100.000 mg
TabletOral10.000 mg
Solution / dropsOphthalmic2.4 mg/1mL
Solution / dropsOral10 MG/ML
SolutionOral0.100 g
Tablet, chewableOral10 mg/1
Tablet, chewableOral5 mg/1
Solution / drops10 mg/ml
Kit; tablet, film coatedOral
Tablet, orally disintegratingOral10 mg/1
Tablet, extended releaseOral
Tablet, multilayer, extended releaseOral
CapsuleOral10 mg
Tablet, coatedOral10 mg
Tablet, film coatedOral10 mg
Tablet10 mg
Unit descriptionCostUnit
Cetirizine HCl 100 10 mg tablet Bottle259.71USD bottle
Cetirizine HCl 100 5 mg tablet Bottle259.71USD bottle
Zyrtec 10 mg tablet2.66USD tablet
Zyrtec 5 mg tablet2.66USD tablet
Zyrtec itchy eye 0.025% drops2.62USD ml
Cetirizine hcl 5 mg chew tablet2.5USD tablet
Cetirizine hcl 10 mg tablet2.49USD tablet
Cetirizine hcl 5 mg tablet2.49USD tablet
Zyrtec-d tablet1.33USD tablet
Child's zyrtec chew tablet0.9USD tablet
CVS Pharmacy allergy relief 10 mg tablet0.74USD each
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6469009No2002-10-222019-07-13US flag
US7226614No2007-06-052022-06-10US flag
US6489329No2002-12-032016-04-08US flag
US7014867No2006-03-212022-06-10US flag
US6455533No2002-09-242018-07-02US flag
US9254286Yes2016-02-092033-01-09US flag
US8829005Yes2014-09-092030-09-15US flag
US9750684No2017-09-052030-03-15US flag
US9993471No2018-06-122030-03-15US flag
US9180090No2015-11-102030-02-11US flag
US8314083No2012-11-202030-02-28US flag
US8513259No2013-08-202030-02-11US flag
US8263581No2012-09-112030-02-28US flag
US9119771No2015-09-012030-02-11US flag


Experimental Properties
melting point (°C)110-115°Chttps://www.chemicalbook.com/ChemicalProductProperty_US_CB3440625.aspx
boiling point (°C)542.1 °C at 760 mmHghttps://www.lookchem.com/Cetirizine-hydrochloride/
water solubility101 mg/Lhttps://www.chemicalbook.com/ChemicalProductProperty_US_CB3440625.aspx
Caco2 permeability1.14https://core.ac.uk/download/pdf/76975249.pdf
pKa1.52, 2.92 and 8.27https://www.researchgate.net/publication/42768947_Isolation_and_Characterization_of_Cetirizine_Degradation_Product_Mechanism_of_Cetirizine_Oxidation
Predicted Properties
Water Solubility0.0658 mg/mLALOGPS
pKa (Strongest Acidic)3.59Chemaxon
pKa (Strongest Basic)7.42Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area53.01 Å2Chemaxon
Rotatable Bond Count8Chemaxon
Refractivity106.87 m3·mol-1Chemaxon
Polarizability41.84 Å3Chemaxon
Number of Rings3Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Human Intestinal Absorption+0.6863
Blood Brain Barrier+0.7576
Caco-2 permeable-0.5879
P-glycoprotein substrateSubstrate0.7862
P-glycoprotein inhibitor IInhibitor0.7364
P-glycoprotein inhibitor IINon-inhibitor0.7624
Renal organic cation transporterNon-inhibitor0.5232
CYP450 2C9 substrateNon-substrate0.8408
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.7
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.8885
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9465
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6917
Ames testNon AMES toxic0.7815
BiodegradationNot ready biodegradable0.9974
Rat acute toxicity2.6841 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.866
hERG inhibition (predictor II)Inhibitor0.6517
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0udr-3292000000-e20abaab20740ce81a18
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000j-0900000000-9801bb859e79fa9922aa
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-014b559d56b0f32984ff
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-213bd47e17d5ab69ad4b
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-004r-9006000000-f496e22c8e0e293fe98c
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-d8a55ab1a7aff0580a91
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-d8a55ab1a7aff0580a91
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-dc957bb6f947575ae4fa
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000b-0900000000-48fc0581ff9fff15e16d
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-04ca95fadd952d0aaeb8
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-000i-0009000000-014b559d56b0f32984ff
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0006-0009000000-26a7769df28c2325ec53
LC-MS/MS Spectrum - LC-ESI-ITFT , negativeLC-MS/MSsplash10-0006-0009000000-284c2e7b25733d7c9875
LC-MS/MS Spectrum - LC-ESI-QFT , negativeLC-MS/MSsplash10-000i-0009000000-04befed283d691217ba2
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0190000000-14715ff4d57580fbb166
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f79-0069000000-431df9c3533b77cf08bc
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0090000000-e042b67e2048318e7dbd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0190000000-b0dfb67717c01fd0c0b9
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0gb9-0970000000-e2810b242fefb4a419e7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0900000000-72f7cddc4ff6d45f98c0
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0900000000-d6044767562f707c8061
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f79-0059000000-15be2621a731a6c2b0ea
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0090000000-01f33b4e54bcb6c8720c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0190000000-f28111ea9c76c1bd27dd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0gb9-0970000000-673301f54b883df73a2a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0900000000-81ab05c275bd28fa3dfb
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0900000000-82d8eb507c79b7342917
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0190000000-0f667566feb3af808386
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0uxr-0690000000-0d4336539c5ebe9050c8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-014i-0900000000-1638816057d01db5eaa1
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0190000000-de2feb9a65604f442606
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0udi-0190000000-58d302681ca058e5706c
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0391000000-7af5014f07bed862bba6
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0491000000-ac48bba9129fe5016c4b
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000i-0009000000-68052b6766ed366c63e4
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0uk9-0079000000-2d34cc42330f30041359
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-000i-6029000000-096a770835329ffdc3ff
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0udl-2590000000-7b8e2450b42ebd6f9a56
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0hj9-5059000000-73fb3a3e16673256f88e
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-7290000000-5274772d061942672254
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)
DarkChem Lite v0.1.0
DeepCCS 1.0 (2019)


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1. Histamine H1 receptor
Pharmacological action
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
Uniprot ID
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
  1. 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. [Article]
  2. 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. [Article]
  3. 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. [Article]
  4. 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. [Article]
  5. 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. [Article]
  6. Portnoy JM, Dinakar C: Review of cetirizine hydrochloride for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Jan;5(1):125-35. doi: 10.1517/14656566.5.1.125 . [Article]
  7. Zhang L, Cheng L, Hong J: The clinical use of cetirizine in the treatment of allergic rhinitis. Pharmacology. 2013;92(1-2):14-25. doi: 10.1159/000351843. Epub 2013 Jul 18. [Article]
  8. Cetirizine FDA label [File]


Pharmacological action
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
Uniprot ID
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
  1. Mesgari Abbasi M, Valizadeh H, Hamishekar H, Mohammadnejad L, Zakeri-Milani P: The Effects of Cetirizine on P-glycoprotein Expression and Function In vitro and In situ. Adv Pharm Bull. 2016 Mar;6(1):111-8. doi: 10.15171/apb.2016.017. Epub 2016 Mar 17. [Article]
  2. Polli JW, Baughman TM, Humphreys JE, Jordan KH, Mote AL, Salisbury JA, Tippin TK, Serabjit-Singh CJ: P-glycoprotein influences the brain concentrations of cetirizine (Zyrtec), a second-generation non-sedating antihistamine. J Pharm Sci. 2003 Oct;92(10):2082-9. doi: 10.1002/jps.10453. [Article]
  3. Conen S, Theunissen EL, Vermeeren A, van Ruitenbeek P, Stiers P, Mehta MA, Toennes SW, Ramaekers JG: The role of P-glycoprotein in CNS antihistamine effects. Psychopharmacology (Berl). 2013 Sep;229(1):9-19. doi: 10.1007/s00213-013-3075-z. Epub 2013 Apr 7. [Article]
  4. Obradovic T, Dobson GG, Shingaki T, Kungu T, Hidalgo IJ: Assessment of the first and second generation antihistamines brain penetration and role of P-glycoprotein. Pharm Res. 2007 Feb;24(2):318-27. doi: 10.1007/s11095-006-9149-4. Epub 2006 Dec 19. [Article]

Drug created at June 13, 2005 13:24 / Updated at April 24, 2024 14:30