Cetirizine

Cetirizine is a second-generation antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria (hives). It is taken by mouth. Effects generally begin within thirty minutes and last for about a day. The degree of benefit is similar to other antihistamines such as diphenhydramine, which is a first-generation antihistamine.

Cetirizine
Clinical data
Pronunciation/sɛˈtɪrɪzn/
Trade namesAllacan, Piriteze, Zyrtec, others
AHFS/Drugs.comMonograph
MedlinePlusa698026
License data
Pregnancy
category
  • AU: B2
Routes of
administration
By mouth
ATC code
Legal status
Legal status
  • AU: Unscheduled
  • CA: OTC
  • NZ: OTC
  • UK: General sales list (GSL, OTC) / P
  • US: OTC / Rx-only
  • OTC / Rx-only
Pharmacokinetic data
BioavailabilityWell-absorbed (>70%)
Protein binding88–96%
MetabolismMinimal (non-cytochrome P450-mediated)
Onset of action20–42 minutes
Elimination half-lifeMean: 8.3 hours
Range: 6.5–10 hours
Duration of action≥24 hours
ExcretionUrine: 70–85%
Feces: 10–13%
Identifiers
  • (±)-[2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.223.545
Chemical and physical data
FormulaC21H25ClN2O3
Molar mass388.89 g·mol−1
3D model (JSmol)
SMILES
  • Clc1ccc(cc1)C(c2ccccc2)N3CCN(CC3)CCOCC(=O)O
  • 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) Y
  • Key:ZKLPARSLTMPFCP-UHFFFAOYSA-N Y
  (verify)

Common side effects include sleepiness, dry mouth, headache, and abdominal pain. The degree of sleepiness that occurs is generally less than with first-generation antihistamines because second-generation antihistamines are more selective for the H1 receptor. Compared to other second-generation anti-histamines, cetirizine can cause drowsiness. Second-generation antihistamines that do not cause drowsiness are fexofenadine, and loratadine.

Use in pregnancy appears safe, but use during breastfeeding is not recommended. The medication works by blocking histamine H1 receptors, mostly outside the brain.

Cetirizine can be used for paediatric patients. The main side effect to be cautious about is somnolence.

It was patented in 1983 and came into medical use in 1987. It is on the World Health Organization's List of Essential Medicines. It is available as a generic medication. In 2021, it was the 49th most commonly prescribed medication in the United States, with more than 13 million prescriptions.

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