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Accession Number
DB00341  (APRD00630)
Small Molecule

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].

  • Cetirizin
  • Cetirizina
  • Cetirizine
  • Cetirizinum
Product Ingredients
IngredientUNIICASInChI Key
Cetirizine hydrochloride64O047KTOA83881-52-1PGLIUCLTXOYQMV-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CetirizineTablet20 mgOralPro Doc Limitee2016-06-13Not applicableCanada
Reactine 20mg TabletTablet20 mgOralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc2002-01-14Not applicableCanada
Rhinaris ReliefTablet20 mgOralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
ZerviateSolution, gel forming / drops2.4 mg/1mLOphthalmicEyevance Pharmaceuticals2019-02-19Not applicableUs
ZyrtecTablet, chewable5 mg/1OralPhysicians Total Care, Inc.2007-03-302007-12-30Us
ZyrtecSyrup1 mg/1mLOralPfizer Laboratories Div Pfizer Inc.1996-09-272009-01-01Us
ZyrtecTablet, film coated5 mg/1OralPfizer Laboratories Div Pfizer Inc.1995-12-082010-12-08Us
ZyrtecTablet, film coated10 mg/1OralPfizer Laboratories Div Pfizer Inc.1995-12-082010-12-08Us
ZyrtecTablet, chewable5 mg/1OralPfizer Laboratories Div Pfizer Inc.2004-03-162010-12-08Us
ZyrtecTablet, chewable10 mg/1OralPfizer Laboratories Div Pfizer Inc.2004-03-162010-12-08Us
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-cetirizineTablet20 mgOralApotex Corporation2016-04-22Not applicableCanada
Cetirizine HydrochlorideSolution1 mg/1mLOralBreckenridge Pharmaceutical, Inc.2013-12-03Not applicableUs
Cetirizine HydrochlorideTablet10 mg/1OralRemedy Repack2010-12-012010-12-02Us
Cetirizine HydrochlorideTablet10 mg/1OralDirectrx2016-12-22Not applicableUs
Cetirizine HydrochlorideSolution1 mg/1mLOralPreferreed Pharmaceuticals Inc.2014-04-02Not applicableUs
Cetirizine HydrochlorideSyrup1 mg/1mLOralTeva2008-05-302015-11-30Us
Cetirizine HydrochlorideSyrup1 mg/1mLOralQualitest2009-09-252014-12-31Us
Cetirizine HydrochlorideSolution1 mg/1mLOralNostrum Laboratories, Inc.2009-11-162017-04-17Us
Cetirizine HydrochlorideSyrup1 mg/1mLOralAurobindo Pharma2009-12-162014-09-22Us
Cetirizine HydrochlorideSyrup1 mg/1mLOralPreferreed Pharmaceuticals Inc.2010-12-202017-12-28Us
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
24 Hour AllergyLiquid5 mg/5mLOralMeijer Distribution2008-04-162017-07-13Us
24 Hour AllergyCapsule10 mg/1OralWalgreens2013-03-012019-12-31Us
24 Hour AllergyCapsule10 mg/1OralWalgreens2018-09-14Not applicableUs
24 Hour AllergyTablet, film coated10 mg/1OralMeijer Distribution1997-07-07Not applicableUs
24 Hour Allergy Lil Drug Store ProductsTablet10 mg/1OralLil' Drug Store Products, Inc.2014-11-01Not applicableUs
24 Hour Allergy Lil Drug Store ProductsTablet10 mg/1OralLil' Drug Store Products, Inc.2018-06-01Not applicableUs
24-Hour All Day AllergyTablet10 mg/1OralMc Kesson2012-04-27Not applicableUs
7 Select All Day AllergyTablet10 mg/1Oral7 Eleven2014-04-29Not applicableUs
7 Select Childrens Allergy ReliefSolution5 mg/5mLOral7 Eleven2014-08-05Not applicableUs
All Day AllergyCapsule10 mg/1OralTopcare (Topco Associates Llc)2018-02-28Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
12 Hour Allergy DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralMeijer Distribution Inc1988-07-15Not applicableUs
All Day Allergy DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralHyvee2008-05-05Not applicableUs
All Day Allergy DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralKroger Company2014-02-19Not applicableUs
All day Allergy dCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralMajor Pharmaceuticals2008-05-06Not applicableUs
all day Allergy Relief DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralH E B2008-05-02Not applicableUs
All Day Allergy-DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralL. Perrigo Company2011-09-06Not applicableUs
Allergy and Congestion Relief D Original Prescription StrengthCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralRite Aid Corporation2008-04-10Not applicableUs
Allergy Relief DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralCVS Health2008-04-10Not applicableUs
Allergy Relief DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralShopko Stores Operating2013-09-07Not applicableUs
Allergy Relief DCetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1)Tablet, extended releaseOralPublix Super Markets Inc2010-03-11Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ZyrtecCetirizine hydrochloride (5 mg/1)TabletOralPhysicians Total Care, Inc.2002-12-162009-01-18Us
ZyrtecCetirizine hydrochloride (10 mg/1)TabletOralPhysicians Total Care, Inc.1996-12-182009-01-18Us
International/Other Brands
Alerlisin / Cetryn / Formistin / Hitrizin / Virlix / Zirtek / Zyrlex
CAS number
Average: 388.888
Monoisotopic: 388.155370383
Chemical Formula
InChI Key
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid



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].

Associated Conditions

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].

Half life

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].


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].

Affected organisms
  • Humans and other mammals
Cetirizine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
1,10-PhenanthrolineThe therapeutic efficacy of Cetirizine can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Cetirizine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Cetirizine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Cetirizine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Cetirizine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Cetirizine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
AbacavirCetirizine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Cetirizine.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.


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 . [PubMed:14680442]
  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. [PubMed:23867423]
  3. Wheatley LM, Togias A: Clinical practice. Allergic rhinitis. N Engl J Med. 2015 Jan 29;372(5):456-63. doi: 10.1056/NEJMcp1412282. [PubMed:25629743]
  4. Church MK, Church DS: Pharmacology of antihistamines. Indian J Dermatol. 2013 May;58(3):219-24. doi: 10.4103/0019-5154.110832. [PubMed:23723474]
  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. [PubMed:9084458]
External Links
Human Metabolome Database
KEGG Compound
PubChem Compound
PubChem Substance
Therapeutic Targets Database
Guide to Pharmacology
GtP Drug Page
RxList Drug Page Drug Page
ATC Codes
R06AE07 — Cetirizine
AHFS Codes
  • 04:08.00 — Second Generation Antihistamines
FDA label
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Clinical Trials

Clinical Trials
0RecruitingBasic ScienceChronic Prostatitis With Chronic Pelvic Pain Syndrome1
1CompletedNot AvailableHealthy Volunteers4
1CompletedNot AvailableRhinitis, Allergic, Perennial and Seasonal1
1CompletedBasic ScienceAllergies1
1CompletedPreventionSkin Inflammation1
1CompletedTreatmentHealthy Volunteers3
1TerminatedBasic ScienceMigraine1
1, 2CompletedTreatmentNeuromyelitis Optica1
2CompletedPreventionHuman Immunodeficiency Virus (HIV) Infections / Pregnancy1
2CompletedTreatmentAllergic Rhinitis (AR)1
2CompletedTreatmentAllergic Rhinitis (AR) / Rhinitis, Allergic, Seasonal1
2CompletedTreatmentAllergic / Rhinitis / Rhinitis, Allergic, Seasonal / Seasonal1
2CompletedTreatmentRhinitis, Allergic, Seasonal1
2CompletedTreatmentSeasonal Allergic Rhinitis (SAR)3
3CompletedNot AvailableAllergic Rhinitis (AR)2
3CompletedTreatmentDermatitis, Eczematous / Skin Inflammation1
3CompletedTreatmentPerennial Allergic Rhinitis (PAR)2
3CompletedTreatmentPerennial Allergic Rhinitis (PAR) / Rhinitis, Allergic, Perennial1
3CompletedTreatmentRhinitis, Allergic, Perennial1
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)2
4CompletedNot AvailableAllergies2
4CompletedNot AvailablePerennial Allergic Rhinitis (PAR) / Seasonal Allergic Rhinitis (SAR)3
4CompletedDiagnosticAsthma Bronchial1
4CompletedOtherAllergic Rhinitis (AR)1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentAllergic Rhinitis (AR) / Asthma Bronchial1
4CompletedTreatmentAllergic Rhinitis (AR) / Pollen Allergy / Rhinitis, Allergic, Seasonal / Severe Acute Respiratory Syndrome1
4CompletedTreatmentDisseminated Sclerosis1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedTreatmentRhinitis, Allergic, Perennial and Seasonal1
4CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
4Enrolling by InvitationTreatmentDiabetic Neuropathy, Painful / Pain, Neuropathic / Type 2 Diabetes Mellitus1
4RecruitingBasic ScienceExercise Intolerance at Altitude1
4RecruitingTreatmentAllergic Rhinitis (AR) / Asthma Bronchial1
4Unknown StatusTreatmentSeasonal Allergic Rhinitis (SAR)1
Not AvailableCompletedNot AvailableCognition / Driving Ability / Seasonal Allergic Rhinitis (SAR)1
Not AvailableCompletedNot AvailableHealthy Volunteers2
Not AvailableCompletedNot AvailableSeasonal Allergic Rhinitis (SAR) / Sinusitis1
Not AvailableCompletedTreatmentActinic Keratosis (AK)1
Not AvailableCompletedTreatmentSeasonal Allergic Rhinitis (SAR)1


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  • Aurobindo Pharma Ltd.
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  • Caraco Pharmaceutical Labs
  • Cardinal Health
  • CVS Pharmacy
  • Cypress Pharmaceutical Inc.
  • Direct Dispensing Inc.
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  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • EZ-EM Inc.
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  • J.B. Chemicals & Pharmaceuticals
  • Kaiser Foundation Hospital
  • L Perrigo Co.
  • Lake Erie Medical and Surgical Supply
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  • Medvantx Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nucare Pharmaceuticals Inc.
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  • PD-Rx Pharmaceuticals Inc.
  • Perrigo Co.
  • Pfizer Inc.
  • Pharmacy Service Center
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  • Wockhardt Ltd.
Dosage forms
CapsuleOral10 mg/1
SyrupOral1 mg/1
TabletOral10.0 mg/1
Tablet, film coated, extended releaseOral
Capsule, liquid filledOral10 mg/1
SolutionOral1 mg/1mL
SolutionOral5 mg/5mL
SyrupOral1 mg/1mL
SyrupOral5 mg/5mL
TabletOral10 mg/1
TabletOral5 mg/1
Tablet, coatedOral10 mg/1
Tablet, film coatedOral10 mg/1
Tablet, film coatedOral5 mg/1
LiquidOral5 mg/5mL
SuspensionOral1 mg/1mL
Tablet, orally disintegratingOral10 mg/1
SyrupOral5 mg
TabletOral10 mg
TabletOral5 mg
TabletOral20 mg
CapsuleOral10 mg
Tablet, chewableOral10 mg
Tablet, chewableOral5 mg
Tablet, extended releaseOral
Tablet, orally disintegratingOral10 mg
Solution, gel forming / dropsOphthalmic2.4 mg/1mL
Tablet, chewableOral10 mg/1
Tablet, chewableOral5 mg/1
Tablet, multilayer, extended releaseOral
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)


Experimental Properties
melting point (°C)110-115°C
boiling point (°C)542.1 °C at 760 mmHg
water solubility101 mg/L
Caco2 permeability1.14
pKa1.52, 2.92 and 8.27
Predicted Properties
Water Solubility0.0658 mg/mLALOGPS
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
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-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
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


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
Diphenylmethane / Chlorobenzene / Halobenzene / N-alkylpiperazine / Aralkylamine / Aryl halide / 1,4-diazinane / Aryl chloride / Piperazine / Amino acid
show 22 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
monocarboxylic acid, ether, monochlorobenzenes, piperazines (CHEBI:3561)


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. [PubMed:12787835]
  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. [PubMed:15286093]
  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. [PubMed:14505791]
  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. [PubMed:10597865]
  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. [PubMed:15942272]
  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 . [PubMed:14680442]
  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. [PubMed:23867423]
  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. [PubMed:27123426]
  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. [PubMed:14502547]
  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. [PubMed:23564211]
  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. [PubMed:17180728]

Drug created on June 13, 2005 07:24 / Updated on April 23, 2019 16:42