R06AE07 - Cetirizine |
Not porphyrinogenic |
NP |
Rationale
30 reports of uneventful long term or short term use. Little affinity to cytochrome P450 and no known induction or inhibition of CYP 2C9 or 3A4. No inhibition of CYP 2C9 or 3A4 in human liver microsomes.
Chemical description
Piperazine antihistamine
Therapeutic characteristics
Cetirizine is given orally for the treatment of allergic rhinitis, conjunctivitis, pruritus and urticaria.
Metabolism and pharmacokinetics
Cetirizine is mainly eliminated unchanged in urine. Some metabolism occurs, and it is unclear what cytochrome P-450 enzymes are involved. The fact that the CYP inhibitor ritonavir increases the plasma concentrations of cetirizin indicates that CYP is involved in the metabolism (Peytavin G, 2005). However, cetirizine seem to be free from clinically significant pharmacokinetic interactions. Given the widespread use of these drugs any consistent clinically significant interaction might have been expected to be seen by now. One study using human liver microsomes showed that cetirizine had no inhibitory effects on CYP 3A4 or 2C9 in vitro (Nicholas JM 1999).
IPNet drug reports
Uneventful use reported in 31 patients with acute porphyria.
References
- Scientific articles
- Chen C. Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem 2008;15(21):2173-91. PMID 18781943. #3381
- Nicolas JM, Whomsley R et al. In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact 1999;123(1):63-79. PMID 10597902. #3380
- Peytavin G, Gautran C et al. Evaluation of pharmacokinetic interaction between cetirizine and ritonavir, an HIV-1 protease inhibitor, in healthy male volunteers. Eur J Clin Pharmacol 2005;61:267-73. PMID 15889300. #3377
- Simons FER, Sussman GL et al. Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria. J Allergy Clin Immunol 1995;95:685â-93. PMID 7897151. #4718
- Wood SG, John BA et al. The metabolism and pharmacokinetics of 14C-cetirizine in humans. Ann Allergy 1987;59(6 Pt 2):31-4. #3379
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