Identification
- Summary
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
- Cetirizine
- DrugBank Accession Number
- DB00341
- Background
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.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Cetirizine (DB00341)
- Weight
- Average: 388.888
Monoisotopic: 388.155370383 - Chemical Formula
- C21H25ClN2O3
- Synonyms
- Cetirizin
- Cetirizina
- Cetirizine
- Cetirizinum
Pharmacology
- Indication
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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- 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.
Target Actions Organism AHistamine H1 receptor antagonistHumans - Absorption
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.
- Metabolism
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.
- Clearance
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.
- Pathways
Pathway Category Cetirizine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Cetirizine is combined with 1,2-Benzodiazepine. Abacavir Cetirizine may decrease the excretion rate of Abacavir which could result in a higher serum level. Aceclofenac Aceclofenac may decrease the excretion rate of Cetirizine which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Cetirizine which could result in a higher serum level. Acetazolamide The risk or severity of CNS depression can be increased when Cetirizine is combined with Acetazolamide. Acetophenazine The risk or severity of CNS depression can be increased when Cetirizine is combined with Acetophenazine. Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Cetirizine which could result in a higher serum level. Aclidinium Cetirizine may decrease the excretion rate of Aclidinium which could result in a higher serum level. Acrivastine The risk or severity of QTc prolongation can be increased when Cetirizine is combined with Acrivastine. Acyclovir Acyclovir may decrease the excretion rate of Cetirizine which could result in a higher serum level. 
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- Avoid alcohol.
- Take with or without food. The absorption is unaffected by food.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Cetirizine hydrochloride 64O047KTOA 83881-52-1 PGLIUCLTXOYQMV-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Alerlisin / Cetryn / Formistin / Hitrizin / Virlix / Zirtek / Zyrlex
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cetirizine Tablet 20 mg Oral Pro Doc Limitee 2016-06-13 Not applicable Canada 
Cetirizine Tablet 20 mg Oral Sanis Health Inc 2021-11-30 Not applicable Canada Cetirizine Tablet 20 mg Oral Sivem Pharmaceuticals Ulc 2023-07-20 Not applicable Canada Cetirizine Hydrochloride Tablets Tablet 20 mg Oral Vita Health Products Inc Not applicable Not applicable Canada M-cetirizine Tablet 20 mg Oral Mantra Pharma Inc 2021-04-20 Not applicable Canada Nra-cetirizine Tablet 20 mg Oral Nora Pharma Inc 2022-04-01 2023-07-18 Canada Nra-cetirizine Tablets Tablet 20 mg Oral Nora Pharma Inc 2023-04-13 Not applicable Canada Quzyttir Injection 10 mg/1mL Intravenous Tersera Therapeutics Llc 2019-11-13 Not applicable US 
Reactine 20mg Tablet Tablet 20 mg Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc 2002-01-14 Not applicable Canada Rhinaris Relief Tablet 20 mg Oral Pendopharm Division Of Pharmascience Inc Not applicable Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ag-cetirizine Tablet 20 mg Oral Angita Pharma Inc. 2022-05-11 Not applicable Canada Allergy Relief Tablet 10 mg/1 Oral bryant ranch prepack 2018-12-31 Not applicable US Apo-cetirizine Tablet 20 mg Oral Apotex Corporation 2016-04-22 Not applicable Canada Bio-cetirizine Tablet 20 mg Oral Biomed Pharma 2023-06-19 Not applicable Canada Cetirizine Hydrochloride Solution 1 mg/1mL Oral A-S Medication Solutions 2014-05-01 Not applicable US Cetirizine Hydrochloride Syrup 1 mg/1mL Oral Qualitest 2009-09-25 2014-12-31 US Cetirizine Hydrochloride Solution 1 mg/1mL Oral Torrent Pharma Inc. 2018-07-13 Not applicable US Cetirizine Hydrochloride Solution 1 mg/1mL Oral Preferred Pharmaceuticals Inc. 2023-09-13 Not applicable US Cetirizine Hydrochloride Syrup 1 mg/1mL Oral Caraco Pharmaceutical Laboratories, Ltd. 2009-11-16 Not applicable US Cetirizine Hydrochloride Syrup 5 mg/5mL Oral Lannett Company, Inc. 2012-05-11 2023-11-30 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image 24 Hour Allergy Capsule, liquid filled 10 mg/1 Oral Meijer Distribution Inc 2020-06-02 Not applicable US 24 Hour Allergy Capsule, liquid filled 10 mg/1 Oral MEIJER, INC. 2022-03-08 Not applicable US 24 Hour Allergy Capsule 10 mg/1 Oral Walgreens 2018-09-14 Not applicable US 24 Hour Allergy Tablet, film coated 10 mg/1 Oral Meijer Distribution Inc 1997-07-07 Not applicable US 24 Hour Allergy Liquid 5 mg/5mL Oral Meijer Distribution 2008-04-16 2017-07-13 US 24 Hour Allergy Lil Drug Store Products Tablet 10 mg/1 Oral Lil' Drug Store Products, Inc. 2018-06-01 2024-12-17 US 24 Hour Allergy Lil Drug Store Products Tablet 10 mg/1 Oral Lil' Drug Store Products, Inc 2014-11-01 2023-01-17 US 24-Hour All Day Allergy Tablet 10 mg/1 Oral Strategic Sourcing Services LLC 2012-04-27 2019-10-01 US 7 Select All Day Allergy Tablet 10 mg/1 Oral 7-Eleven 2014-04-29 2021-01-31 US 7 Select Childrens Allergy Relief Solution 5 mg/5mL Oral 7-Eleven 2014-08-05 2016-10-26 US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image 12 Hour Allergy D Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, film coated, extended release Oral Meijer Distribution Inc 2020-04-07 Not applicable US 12 Hour Allergy D Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, extended release Oral Meijer Distribution Inc 1988-07-15 Not applicable US ABSORGEL´S ® Cetirizine hydrochloride (5 mg) + Ibuprofen (200 mg) + Phenylephrine hydrochloride (10 mg) Capsule, liquid filled Oral 2019-05-28 Not applicable Colombia 
ACERADOX® G Cetirizine hydrochloride (5 mg) + Acetaminophen (500 mg) + Caffeine (30 mg) + Phenylephrine hydrochloride (10 mg) Capsule, coated Oral LABORATORIOS DEMAC LTDA. 2019-02-28 Not applicable Colombia ALERCET® D Cetirizine hydrochloride (100 mg) + Phenylephrine hydrochloride (200 mg) Syrup Oral PROCAPS S.A. 2007-11-22 2022-01-31 Colombia All day Allergy d Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, extended release Oral Major Pharmaceuticals 2008-05-06 Not applicable US All Day Allergy D Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, extended release Oral Kroger Company 2014-02-19 Not applicable US All Day Allergy D Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, film coated, extended release Oral Kroger Company 2020-04-02 Not applicable US All Day Allergy D Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, extended release Oral HYVEE INC 2008-05-05 2019-11-01 US all day Allergy Relief D Cetirizine hydrochloride (5 mg/1) + Pseudoephedrine hydrochloride (120 mg/1) Tablet, extended release Oral H E B 2008-05-02 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Zyrtec Cetirizine hydrochloride (5 mg/1) Tablet Oral Physicians Total Care, Inc. 2002-12-16 2009-01-18 US Zyrtec Cetirizine hydrochloride (10 mg/1) Tablet Oral Physicians Total Care, Inc. 1996-12-18 2009-01-18 US
Categories
- ATC Codes
- S01GX12 — Cetirizine
- S01GX — Other antiallergics
- S01G — DECONGESTANTS AND ANTIALLERGICS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Anti-Allergic Agents
- Antihistamines for Systemic Use
- Central Nervous System Depressants
- Decongestants and Antiallergics
- Drugs that are Mainly Renally Excreted
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Histamine H1 Antagonists, Non-Sedating
- Ophthalmologicals
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- Piperazine Derivatives
- Piperazines
- Potential QTc-Prolonging Agents
- QTc Prolonging Agents
- Sensory Organs
- Chemical TaxonomyProvided by Classyfire
- Description
- 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.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Diphenylmethanes
- Direct Parent
- Diphenylmethanes
- Alternative Parents
- N-alkylpiperazines / Chlorobenzenes / Aralkylamines / Aryl chlorides / Trialkylamines / Amino acids / Monocarboxylic acids and derivatives / Dialkyl ethers / Carboxylic acids / Azacyclic compounds show 5 more
- Substituents
- 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
- UNII
- YO7261ME24
- CAS number
- 83881-51-0
- InChI Key
- ZKLPARSLTMPFCP-UHFFFAOYSA-N
- InChI
- InChI=1S/C21H25ClN2O3/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26/h1-9,21H,10-16H2,(H,25,26)
- IUPAC Name
- 2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
- SMILES
- OC(=O)COCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1
References
- Synthesis Reference
Manne Reddy, "Polymorphic forms of dihydrochloride salts of cetirizine and processes for preparation thereof." U.S. Patent US20040186112, issued September 23, 2004.
US20040186112- General References
- 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]
- 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]
- Wheatley LM, Togias A: Clinical practice. Allergic rhinitis. N Engl J Med. 2015 Jan 29;372(5):456-63. doi: 10.1056/NEJMcp1412282. [Article]
- Church MK, Church DS: Pharmacology of antihistamines. Indian J Dermatol. 2013 May;58(3):219-24. doi: 10.4103/0019-5154.110832. [Article]
- 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]
- External Links
- Human Metabolome Database
- HMDB0005032
- KEGG Compound
- C07778
- PubChem Compound
- 2678
- PubChem Substance
- 46508368
- ChemSpider
- 2577
- BindingDB
- 22890
- 20610
- ChEBI
- 3561
- ChEMBL
- CHEMBL1000
- Therapeutic Targets Database
- DAP000323
- PharmGKB
- PA448905
- Guide to Pharmacology
- GtP Drug Page
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Cetirizine
- FDA label
- Download (54.2 KB)
- MSDS
- Download (26.5 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Hypoxia, Altitude 1 4 Completed Diagnostic Asthma 1 4 Completed Other Allergic Reaction 2 4 Completed Other Allergic Rhinitis (AR) 1 4 Completed Other Perennial Allergic Rhinitis (PAR) / Seasonal Allergic Rhinitis 3 4 Completed Treatment Allergic Rhinitis (AR) 2 4 Completed Treatment Allergic Rhinitis (AR) / Allergy to Tree Pollen / Seasonal Allergic Rhinitis 1 4 Completed Treatment Allergic Rhinitis (AR) / Asthma 2 4 Completed Treatment Multiple Sclerosis 1 4 Completed Treatment Neuropathic Pain / Painful Diabetic Neuropathy (PDN) / Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- 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
- Packagers
- 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.
- PCA LLC
- 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
Form Route Strength Tablet Oral Capsule, extended release Oral Solution Oral 1 mg/ml Capsule, liquid filled Oral 10 mg Syrup Oral 100 mg Syrup Oral 0.1 g Capsule, coated Oral 500 mg Capsule Oral 10 mg/1 Syrup Oral 1 mg/1 Tablet Oral 10.0 mg/1 Solution Oral 100 mg Syrup Oral 0.060 g Granule Oral Solution Oral Solution / drops Oral 10 MG/ML Tablet, chewable Oral Tablet, film coated Oral Solution Oral 10 MG/ML Syrup Oral 1 MG/ML Lozenge Oral 10 mg/1 Solution Oral 0.102 g Solution Oral 1 g Capsule Oral Liquid Oral 5 mg/5mL Tablet; tablet, film coated Oral 10 MG Tablet, film coated, extended release Oral Capsule, liquid filled Oral 10 mg/1 Solution Oral 1 mg/1mL Solution Oral 5 mg/5mL Solution / drops; suspension / drops Oral Syrup Oral 1 mg/1mL Syrup Oral 5 mg/5mL Tablet Oral 10 mg/1 Tablet Oral 5 mg/1 Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 5 mg/1 Solution Nasal; Oral Syrup Oral Solution Oral 10 mg Syrup Oral 0.1 % w/v Tablet, coated Oral Tablet, film coated Oral Suspension Oral 1 mg/1mL Tablet, chewable Oral 2.5 mg/1 Tablet Nasal Tablet, coated Oral 10 mg/1 Solution Oral 100.00 mg Solution / drops; suspension / drops 10 MG/ML Tablet Solution / drops; suspension / drops Capsule, liquid filled Oral 5 mg Solution Oral 0.1 g Syrup Oral 0.119 g Capsule, liquid filled Oral 500 mg Capsule, coated Oral 500 mg Tablet Oral Syrup Oral 6.5 g Syrup Oral Capsule, coated Oral Injection Intravenous 10 mg/1mL Solution / drops Oral Syrup Oral 5 mg / 5 mL Tablet Oral 5 mg Tablet Oral 20 mg Tablet, chewable Oral 10 mg Tablet, chewable Oral 5 mg Tablet, effervescent Tablet, orally disintegrating Oral 10 mg Tablet Oral 10 mg Solution Oral 10.000 mg Solution Oral 0.01 g Capsule, liquid filled Oral Tablet, soluble Tablet Transmucosal Solution Oral 100.000 mg Tablet Oral 10.000 mg Syrup Oral 100 mg Solution / drops Ophthalmic 2.4 mg/1mL Powder, for solution Oral Solution Oral 0.100 g Tablet, chewable Oral 10 mg/1 Tablet, chewable Oral 5 mg/1 Solution Oral Solution / drops Kit; tablet, film coated Oral Tablet, orally disintegrating Oral 10 mg/1 Tablet, extended release Oral Tablet, multilayer, extended release Oral Capsule Oral 10 mg Tablet, coated Oral 10 mg Tablet, film coated Oral 10 mg Tablet 10 mg - Prices
Unit description Cost Unit Cetirizine HCl 100 10 mg tablet Bottle 259.71USD bottle Cetirizine HCl 100 5 mg tablet Bottle 259.71USD bottle Zyrtec 10 mg tablet 2.66USD tablet Zyrtec 5 mg tablet 2.66USD tablet Zyrtec itchy eye 0.025% drops 2.62USD ml Cetirizine hcl 5 mg chew tablet 2.5USD tablet Cetirizine hcl 10 mg tablet 2.49USD tablet Cetirizine hcl 5 mg tablet 2.49USD tablet Zyrtec-d tablet 1.33USD tablet Child's zyrtec chew tablet 0.9USD tablet CVS Pharmacy allergy relief 10 mg tablet 0.74USD each DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6469009 No 2002-10-22 2019-07-13 US US7226614 No 2007-06-05 2022-06-10 US US6489329 No 2002-12-03 2016-04-08 US US7014867 No 2006-03-21 2022-06-10 US US6455533 No 2002-09-24 2018-07-02 US US9254286 Yes 2016-02-09 2033-01-09 US US8829005 Yes 2014-09-09 2030-09-15 US US9750684 No 2017-09-05 2030-03-15 US US9993471 No 2018-06-12 2030-03-15 US US9180090 No 2015-11-10 2030-02-11 US US8314083 No 2012-11-20 2030-02-28 US US8513259 No 2013-08-20 2030-02-11 US US8263581 No 2012-09-11 2030-02-28 US US9119771 No 2015-09-01 2030-02-11 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 110-115°C https://www.chemicalbook.com/ChemicalProductProperty_US_CB3440625.aspx boiling point (°C) 542.1 °C at 760 mmHg https://www.lookchem.com/Cetirizine-hydrochloride/ water solubility 101 mg/L https://www.chemicalbook.com/ChemicalProductProperty_US_CB3440625.aspx logP 2.8 http://www.t3db.ca/toxins/T3D2756 Caco2 permeability 1.14 https://core.ac.uk/download/pdf/76975249.pdf pKa 1.52, 2.92 and 8.27 https://www.researchgate.net/publication/42768947_Isolation_and_Characterization_of_Cetirizine_Degradation_Product_Mechanism_of_Cetirizine_Oxidation - Predicted Properties
Property Value Source Water Solubility 0.0658 mg/mL ALOGPS logP 2.98 ALOGPS logP 0.87 Chemaxon logS -3.8 ALOGPS pKa (Strongest Acidic) 3.59 Chemaxon pKa (Strongest Basic) 7.42 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 53.01 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 106.87 m3·mol-1 Chemaxon Polarizability 41.84 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - 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 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.8885 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor 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
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- 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
- HRH1
- Uniprot ID
- P35367
- Uniprot Name
- Histamine H1 receptor
- Molecular Weight
- 55783.61 Da
References
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- Cetirizine FDA label [File]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- 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]
- 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]
- 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]
- 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 September 28, 2023 01:14