Cetirizine
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|---|---|
| Pronunciation | /sɛˈtɪrɪziːn/ ⓘ |
| Trade names | Zyrtec, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a698026 |
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| Routes of administration | By mouth |
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| Pharmacokinetic data | |
| Bioavailability | Well-absorbed (>70%)[7] |
| Protein binding | 88–96%[7] |
| Metabolism | Minimal (non-cytochrome P450-mediated)[9][8] |
| Onset of action | 20–42 minutes[8] |
| Elimination half-life | Mean: 8.3 hours[9][8] Range: 6.5–10 hours[10] |
| Duration of action | ≥24 hours[10] |
| Excretion | Urine: 70–85%[9] Feces: 10–13%[9] |
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| ECHA InfoCard | 100.223.545 |
| Chemical and physical data | |
| Formula | C21H25ClN2O3 |
| Molar mass | 388.89 g·mol−1 |
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Cetirizine is a second-generation peripherally selective antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria (hives).[11] It is taken by mouth.[12] Effects generally begin within thirty minutes and last for about a day.[12] The degree of benefit is similar to other antihistamines such as diphenhydramine, which is a first-generation antihistamine.[12]
Common side effects include sleepiness, dry mouth, headache, and abdominal pain.[12] 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.[13][11] Compared to other second-generation antihistamines, cetirizine can cause drowsiness.[13] Among second-generation antihistamines, cetirizine is more likely than fexofenadine and loratadine to cause drowsiness.[13]
Use in pregnancy appears safe, but use during breastfeeding is not recommended.[14] The medication works by blocking histamine H1 receptors, mostly outside the brain.[12]
Cetirizine can be used for paediatric patients. The main side effect to be cautious about is somnolence.[15]
It was patented in 1983[16][17] and came into medical use in 1987.[18] It is on the World Health Organization's List of Essential Medicines.[19] It is available as a generic medication.[11] In 2022, it was the 43rd most commonly prescribed medication in the United States, with more than 13 million prescriptions.[20][21]
- ^ "Reactine Product information". Health Canada. 24 January 2007. Retrieved 17 February 2025.
- ^ "Reactine Product information". Health Canada. 4 August 1997. Retrieved 17 February 2025.
- ^ "Zyrtec Product information". Health Canada. 5 July 2001. Retrieved 17 February 2025.
- ^ "Zyrtec Allergy- cetirizine hydrochloride tablet, film coated". DailyMed. 11 February 2025. Retrieved 17 February 2025.
- ^ "Quzyttir- cetirizine hydrochloride injection". DailyMed. 25 October 2022. Retrieved 17 February 2025.
- ^ "Zerviate- cetirizine solution/ drops". DailyMed. 9 October 2023. Retrieved 17 February 2025.
- ^ a b Chen C (2008). "Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine". Current Medicinal Chemistry. 15 (21): 2173–2191. doi:10.2174/092986708785747625. PMID 18781943.
- ^ a b c Cite error: The named reference
pmid10384858was invoked but never defined (see the help page). - ^ a b c d Cite error: The named reference
pmid14680442was invoked but never defined (see the help page). - ^ a b Simons FE (December 2002). "Comparative pharmacology of H1 antihistamines: clinical relevance". The American Journal of Medicine. 113 (Suppl 9A): 38S – 46S. doi:10.1016/s0002-9343(02)01436-5. PMID 12517581.
- ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 279. ISBN 9780857113382.
- ^ a b c d e "Cetirizine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 28 August 2021. Retrieved 3 March 2019.
- ^ a b c Slater JW, Zechnich AD, Haxby DG (January 1999). "Second-generation antihistamines: a comparative review". Drugs. 57 (1): 31–47. doi:10.2165/00003495-199957010-00004. PMID 9951950. S2CID 46984477.
- ^ "Cetirizine Pregnancy and Breastfeeding Warnings". Drugs.com. Archived from the original on 6 March 2019. Retrieved 3 March 2019.
- ^ Zhou P, Jia Q, Wang Z, Zhao R, Zhou W (25 August 2022). "Cetirizine for the treatment of allergic diseases in children: A systematic review and meta-analysis". Frontiers in Pediatrics. 10: 940213. doi:10.3389/fped.2022.940213. PMC 9452751. PMID 36090559.
- ^ Cite error: The named reference
US4525358was invoked but never defined (see the help page). - ^ US4525358A, Baltes, Eugene; Lannoy, Jean de & Rodriguez, Ludovic, "2-[4-(Diphenylmethyl)-1-piperazinyl]-acetic acids and their amides", issued 25 June 1985.
- ^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 549. ISBN 9783527607495. Archived from the original on 8 October 2022. Retrieved 19 September 2020.
- ^ World Health Organization (2023). The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023). Geneva: World Health Organization. hdl:10665/371090. WHO/MHP/HPS/EML/2023.02.
- ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
- ^ "Cetirizine Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.