User:Mr. Ibrahem/Cetirizine

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Mr. Ibrahem/Cetirizine
Clinical data
Pronunciation/sɛˈtɪrɪziːn/
Trade namesZyrtec, Incidal, others
AHFS/Drugs.comSystemic: Monograph
Eye: Monograph
MedlinePlusa698026
License data
Pregnancy
category
  • AU: B2
Routes of
administration		By mouth
Drug classSecond-generation antihistamine
Legal status
Legal status
Pharmacokinetic data
BioavailabilityWell-absorbed (>70%)[1]
Protein binding88–96%[1]
MetabolismMinimal (non-cytochrome P450-mediated)[3][2]
Onset of action20–42 minutes[2]
Elimination half-lifeMean: 8.3 hours[3][2]
Range: 6.5–10 hours[4]
Duration of action≥24 hours[4]
ExcretionUrine: 70–85%[3]
Feces: 10–13%[3]
Identifiers
  • (±)-[2-[4-[(4-Chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid
Chemical and physical data
FormulaC21H25ClN2O3
Molar mass388.89 g·mol−1
3D model (JSmol)
  • 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) checkY
  • Key:ZKLPARSLTMPFCP-UHFFFAOYSA-N checkY
  (verify)

Cetirizine, sold under the brand name Zyrtec among others, is an antihistamine used to treat allergic rhinitis (hay fever), dermatitis, and urticaria.[6] It is taken by mouth.[7] Effects generally begin within an hour and last for about a day.[7] The degree of benefit is similar to other antihistamines such as diphenhydramine.[7]

Common side effects include sleepiness, dry mouth, headache, and abdominal pain.[7] The degree of sleepiness that occurs is generally less than with first generation antihistamines.[6] Serious side effects may include aggression and angioedema.[6] Use in pregnancy appears safe, but use during breastfeeding is not recommended.[8] It is a second-generation antihistamine and works by blocking histamine H1 receptors, mostly outside the brain.[7]

It was patented in 1981 and came into medical use in 1987.[9] It is available as a generic medication.[6] A month's supply in the United Kingdom costs the NHS about £0.70 as of 2019.[6] In the United States the wholesale cost of this amount is about US$2.50.[10] In 2017, it was the 66th most commonly prescribed medication in the United States, with more than eleven million prescriptions.[11][12]

References[edit]

  1. ^ a b Chen C (2008). "Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine". Curr. Med. Chem. 15 (21): 2173–91. doi:10.2174/092986708785747625. PMID 18781943.
  2. ^ a b c Simons FE, Simons KJ (1999). "Clinical pharmacology of new histamine H1 receptor antagonists". Clin Pharmacokinet. 36 (5): 329–52. doi:10.2165/00003088-199936050-00003. PMID 10384858.
  3. ^ a b c d Portnoy JM, Dinakar C (2004). "Review of cetirizine hydrochloride for the treatment of allergic disorders". Expert Opin Pharmacother. 5 (1): 125–35. doi:10.1517/14656566.5.1.125. PMID 14680442.
  4. ^ a b Simons FE (2002). "Comparative pharmacology of H1 antihistamines: clinical relevance". Am. J. Med. 113 Suppl 9A (9): 38S–46S. doi:10.1016/s0002-9343(02)01436-5. PMID 12517581.
  5. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 7 September 2020.
  6. ^ a b c d e British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 279. ISBN 9780857113382.
  7. ^ a b c d e "Cetirizine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  8. ^ "Cetirizine Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  9. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 549. ISBN 9783527607495.
  10. ^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
  11. ^ "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
  12. ^ "Cetirizine - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
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