Safety information for pregnancy and breastfeeding
Pregnancy
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).
Breastfeeding
Cetirizine has been reported to be excreted in human breast milk.
Always consult your doctor or midwife before taking any medicine during pregnancy or while breastfeeding. Source: DrugBank (CC BY-NC 4.0).
Official documents, adverse reaction reporting, and safety monitoring
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Yellow Card reports
The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.
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Suspected adverse reactions reported for Cetirizine
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
EudraVigilance
The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.
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Suspected adverse reactions reported for Cetirizine
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EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.
1 branded products available
Part of the Benadryl brand family (generic: Cetirizine)
MHRA licensed products
View all licensed products for Cetirizine on the MHRA register
WHO defined daily dose (DDD)
10 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary BNF/ATC mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Guidelines from the National Institute for Health and Care Excellence
NICE clinical guidance(3)
Chronic urticaria: off-label doses of cetirizine (ESUOM31)
Insect bites and stings: antimicrobial prescribing (NG182)
Difelikefalin for treating pruritus in people having haemodialysis (TA890)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Supply & safety information
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Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. Shortage and safety information sourced from MHRA drug safety updates (gov.uk, Crown Copyright under OGL v3.0).
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing all 29 studies.
Reviews & meta-analyses: 6 · Randomised trials: 1 · 2018–2026
Showing all 29 studies, sorted by most relevant.
Xiaomei Chen, Hongmei Xiang, Ming Yang
Journal of Cosmetic Dermatology, 2022
- Alopecia
- Cetirizine
- Administration, Topical
Karla Pinheiro de Alencar, Daniel Fernandes Peixoto, Fábio do Nascimento Máximo, et al.
Brazilian Oral Research, 2024
- Analysis of Variance
- Dental Plaque
- Hydrogen-Ion Concentration
The aim of this study was to evaluate in vivo dental biofilm acidogenicity induced by nine long-term pediatric oral liquid medications (OLMs). A double-blind crossover randomized clinical trial was conducted with 12 individuals aged 18 to 22 years who had good oral hygiene (OSI < 1.1) and a DMFT index of less than 12. Each participant was exposed to nine OLMs and a 10% sucrose solution (positive control) as part of the crossover design. The pH of the dental biofilm was measured with a Beetrode® microelectrode at 0, 5, 10, 15, 20, 25, and 30 min. Statistical analysis was performed to determine the minimum pH and the area under the curve (AUC). One-way ANOVA was utilized, and the significance level was set at 0.05. Pediatric OLMs caused a sucrose-like decrease in biofilm pH, regardless of therapeutic class (p > 0.05). The mean ± standard deviation of the AUC ranged from 16.26 ± 11.59 (cetirizine) to 39.22 ± 20.81 (azithromycin), with no statistically significant difference compared to sucrose (25.22 ± 6.97) (p > 0.05). The findings suggest that pediatric OLMs contribute to dental biofilm acidogenicity, with a more pronounced effect induced by medications used for respiratory diseases and also by antibiotics.
Abstract licence: CC BY
Suman Ghosh, Ishita Debnath, Sobhanjan Bhunia, et al.
Biomedical and Pharmacology Journal, 2025
Histamine-mediated allergic reactions are central to the pathogenesis of various allergic disorders, involving complex molecular mechanisms. Cetirizine, a second-generation antihistamine, functions as a potent H1 receptor antagonist and is widely utilized for the management of these conditions. This review comprehensively evaluated the molecular mechanisms underlying histamine release, its interaction with H1 receptors, and the subsequent allergic responses. It also analyzed the pharmacokinetics and pharmacodynamics of cetirizine, highlighting its high selectivity for H1 receptors and its minimal sedative effects. The clinical efficacy of cetirizine was demonstrated across several allergic conditions, including food allergies, atopic dermatitis, allergic conjunctivitis, and drug-induced hypersensitivities. In these contexts, cetirizine reduced histamine-mediated symptoms, such as pruritus and inflammation, and improved patient outcomes. Additionally, combination therapies involving cetirizine with other antihistamines, corticosteroids, or biologics were discussed, particularly in refractory or severe allergic cases. Despite its overall safety, this review also highlighted the adverse effects associated with long-term cetirizine use, particularly in special populations such as pediatric, elderly, and patients with renal impairment. Future perspectives emphasize the role of future research on cetirizine in personalized allergy treatment, emerging combination therapies with biologics, and its potential in prophylactic applications.
Abstract licence: CC BY
Mikołaj Turski, Małgorzata Łukasiewicz, Piotr Sajdak, et al.
Alergologia Polska, 2024
A 2-year-old boy with suspected lactose intolerance developed an extensive, itchy rash after using a nasal spray containing dexpanthenol. He was initially treated for a viral upper airway infection with ibuprofen, xylometazoline, and cetirizine. A switch to a drug containing dexpanthenol led to the appearance of the rash and subsequent sleep deprivation. No other possible cause of allergy was found. The withdrawal of all drugs but cetirizine led to full recovery. Dexpanthenol, an alcohol analog of vitamin B5, is present in many drugs for its positive impact on tissue repair. Although generally considered safe, it may rarely cause an allergic reaction, hence we underscore the importance of considering dexpanthenol oversensitivity in patients with unexplained widespread rashes, particularly in pediatric cases.
Abstract licence: CC BY-NC-SA
M. Blaiss, J. Bernstein, A. Kessler, et al.
Advances in Therapy, 2021
- Urticaria
- Cetirizine
- Diphenhydramine
antihistamine, has been safely used over-the-counter for many years. In 2019, IV cetirizine was approved for the treatment of acute urticaria. In light of this approval, this narrative review discusses the changing landscape of IV antihistamines for the treatment of histamine-mediated conditions. Specifically, IV antihistamines will be discussed as a treatment option for acute urticaria and angioedema, as premedication to prevent infusion reactions related to anticancer agents and other biologics, and as an adjunct treatment for anaphylaxis and other allergic reactions. Before the development of IV cetirizine, randomized controlled trials of IV antihistamines for these indications were lacking. Three randomized controlled trials have been conducted with IV cetirizine versus IV diphenhydramine in the ambulatory care setting. A phase 3 trial of IV cetirizine 10 mg versus IV diphenhydramine 50 mg was conducted in 262 adults who presented to the urgent care/emergency department with acute urticaria requiring antihistamines. For the primary efficacy endpoint, defined as change from baseline in a 2-h patient-rated pruritus score, non-inferiority of IV cetirizine to IV diphenhydramine was demonstrated (score - 1.6 vs - 1.5, respectively; 95% CI - 0.1, 0.3). Compared with IV diphenhydramine, IV cetirizine demonstrated fewer adverse effects including less sedation, a significantly shorter length of stay in the treatment center, and fewer returns to the treatment center at 24 and 48 h. Similar findings were demonstrated in another phase 2 acute urticaria trial and in a phase 2 trial assessing IV cetirizine for pretreatment for infusion reactions in the oncology/immunology setting. IV cetirizine is associated with similar patient outcomes, fewer adverse effects, and increased treatment center efficiency than IV diphenhydramine.
Abstract licence: CC BY-NC
G. Parisi, S. Leonardi, G. Ciprandi, et al.
Clinical and Molecular Allergy : CMA, 2020
Cetirizine is a second-generation antihistamine, derived from the metabolism of hydroxyzine, highly specific for the H1 receptors, and with marked antiallergic properties. Although its history began more than 30 years ago, it remains one of the most used drugs in children with a leading role in the medical care of children with allergic diseases. Cetirizine use is licensed for paediatric patients for the treatment of allergic rhinitis, and chronic spontaneous urticaria, in Europe in children older than 2 years old and in the USA in children older than 6 months old. This review provides a practical update on the use of cetirizine in children and adolescents.
Abstract licence: CC BY
A. Corsico, S. Leonardi, A. Licari, et al.
Multidisciplinary Respiratory Medicine, 2019
Antihistamines are currently one of the most commonly administered categories of drugs. They are used to treat symptoms that are secondary to histamine release, which is typical of certain allergic conditions, including rhinitis, conjunctivitis, asthma, urticaria, and anaphylaxis. Cetirizine belongs to the second-generation family, so, it is very selective for peripheral H1 receptors, is potent and quickly relieves symptoms, exerts additional anti-allergic/anti-inflammatory effects, and is usually well-tolerated. It has been marketed 30 years ago. In these years, a remarkable body of evidence has been built. The current review provides a practical update on the use of cetirizine in clinical practice.
Abstract licence: CC BY-NC
Reed B. Hogan II, Reed B. Hogan III, T. Cannon, et al.
Pulmonary Pharmacology & Therapeutics, 2020
- Betacoronavirus
- COVID-19
- SARS-CoV-2
M. Aldawsari, El-Sayed Khafagy, E. Moglad, et al.
Saudi Pharmaceutical Journal : SPJ, 2023
Cetirizine hydrochloride (CTZ), a second-generation anti-histaminic drug, has been recently explored for its effectiveness in the treatment of alopecia. Niosomes are surfactant-based nanovesicular systems that have promising applications in both topical and transdermal drug delivery. The aim of this study was to design topical CTZ niosomes for management of alopecia. Thin film hydration technique was implemented for the fabrication of CTZ niosomes. The niosomes were examined for vesicle size, surface charge, and entrapment efficiency. The optimized niosomal formulation was incorporated into a hydrogel base (HPMC) and explored for physical characteristics, ex vivo permeation, and in vivo dermato-kinetic study. The optimized CTZ-loaded niosomal formulation showed an average size of 403.4 ± 15.6 nm, zeta potential of - 12.9 ± 1.7 mV, and entrapment efficiency percentage of 52.8 ± 1.9%. Compared to plain drug solution, entrapment of CTZ within niosomes significantly prolonged in vitro drug release up to 12 h. Most importantly, ex-vivo skin deposition studies and in vivo dermato-kinetic studies verified superior skin deposition/retention of CTZ from CTZ-loaded niosomal gels, compared to plain CTZ gel. CTZ-loaded niosomal gel permitted higher drug deposition percentage (19.2 ± 1.9%) and skin retention (AUC0-10 h 1124.5 ± 87.9 μg/mL.h) of CTZ, compared to 7.52 ± 0.7% and 646.2 ± 44.6 μg/mL.h for plain CTZ gel, respectively. Collectively, niosomes might represent a promising carrier for the cutaneous delivery of cetirizine for the topical management of alopecia.
Abstract licence: CC BY-NC-ND
Krisztián Pamlényi, K. Kristó, Orsolya Jójárt-Laczkovich, et al.
Pharmaceutics, 2021
Currently, pharmaceutical companies are working on innovative methods, processes and products. Oral mucoadhesive systems, such as tablets, gels, and polymer films, are among these possible products. Oral mucoadhesive systems possess many advantages, including the possibility to be applied in swallowing problems. The present study focused on formulating buccal mucoadhesive polymer films and investigating the physical and physical-chemical properties of films. Sodium alginate (SA) and hydroxypropyl methylcellulose (HPMC) were used as film-forming agents, glycerol (GLY) was added as a plasticizer, and cetirizine dihydrochloride (CTZ) was used as an active pharmaceutical ingredient (API). The polymer films were prepared at room temperature with the solvent casting method by mixed two-level and three-level factorial designs. The thickness, tensile strength (hardness), mucoadhesivity, surface free energy (SFE), FTIR, and Raman spectra, as well as the dissolution of the prepared films, were investigated. The investigations showed that GLY can reduce the mucoadhesivity of films, and CTZ can increase the tensile strength of films. The distribution of CTZ proved to be homogeneous in the films. The API could dissolve completely from all the films. We can conclude that polymer films with 1% and 3% GLY concentrations are appropriate to be formulated for application on the buccal mucosa as a drug delivery system.
Abstract licence: CC BY
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
1 found
Half-life
8.3 hours
Mechanism
Cetirizine, a metabolite of hydroxyzine, is an antihistamine drug.
Food interactions
2 warnings
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
1 hour
Half-life
8.3 hours
Protein binding
93%
Volume of distribution
0.19 L/kg
[A175063]
Metabolism
70%
Elimination
70 – 85%
[A175051]
Between 70 – 85% of an orally administered dose can be found in the urine and 10 – 13% in the feces .
[A175051]…
Clearance
53 mL/min
Cetirizine…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
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 [A175057]. Furthermore, some antihistamine agents that are used to treat this condition cause undesirable, sedating effects [A175060].
Cetirizine is one of the first second-generation H1 antihistamines (SGAHs) formulated to selectively inhibit the H1 receptor without sedating effects [A175054].
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 [FDA 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 [FDA label].
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1622 interactions
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 [FDA 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 [FDA 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) [FDA 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 [FDA 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 [FDA label].
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 [FDA label].
Effects on urticaria/anti-inflammatory effects
It has anti-inflammatory properties that may play a role in asthma management [A175051]. 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 [A175051]. Concomitant use of cetirizine reduces the duration and dose of topical anti-inflammatory formulas used for the treatment of atopic dermatitis [A175051].
How the body processes this drug — absorption, distribution, metabolism, and elimination
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 [FDA label].
[A175063]
This prevents potential interactions of cetirizine with drugs interacting with hepatic cytochrome enzymes .
[A175051]
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 [FDA label].
[A175051]
Between 70 – 85% of an orally administered dose can be found in the urine and 10 – 13% in the feces .
[A175051]
Cetirizine is mainly eliminated by the kidneys [A175051], [FDA label]. Dose adjustment is required for patients with moderate to severe renal impairment and in patients on hemodialysis [FDA label].
Proteins and enzymes this drug interacts with in the body
PMID:33828102 PMID:8280179
Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity)
Proteins that transport this drug across cell membranes
PMID:2897240 PMID:35970996 PMID:8898203 PMID:9038218 PMID:35507548
Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins .
PMID:8898203
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells PMID:2897240 PMID:35970996 PMID:9038218
Involved compounds
ATC S01GX12
ATC R06AE07
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Show
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Cetirizine
Additional database identifiers
Drugs Product Database (DPD)
7942
ChemSpider
2577
BindingDB
22890
Guide to Pharmacology
1222
HUGO Gene Nomenclature Committee (HGNC)
HGNC:5182
GenAtlas
HRH1
GeneCards
HRH1
GenBank Gene Database
Z34897
GenBank Protein Database
510296
Guide to Pharmacology
262
UniProt Accession
HRH1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:40
GenAtlas
ABCB1
GeneCards
ABCB1
GenBank Gene Database
M14758
GenBank Protein Database
307180
Guide to Pharmacology
768
UniProt Accession
MDR1_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q423075), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication. WHO INN from the World Health Organization.