Monograph
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.
Similar drugs
References
| # | Citation details | PMID |
|---|---|---|
| * | Scientific articles | |
| 1. | Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem 2008;15(21):2173-91.
Chen C. |
18781943 |
| 2. | In vitro inhibition of human liver drug metabolizing enzymes by second generation antihistamines. Chem Biol Interact 1999;123(1):63-79.
Nicolas JM, Whomsley R et al. |
10597902 |
| 3. | 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.
Peytavin G, Gautran C et al. |
15889300 |
| 4. | 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.
Simons FER, Sussman GL et al. |
7897151 |
| 5. | The metabolism and pharmacokinetics of 14C-cetirizine in humans. Ann Allergy 1987;59(6 Pt 2):31-4.
Wood SG, John BA et al. |
|
Tradenames
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Cetirizine · Prevalin Allerstop cetirizine · Reactine · Zyrtec 
Cetirizin · Cetirizine · Reactine · Zyrtec 
Alercina · Alerlisin · Cetirizina · Zyrtec 
Cerchio · Ceteris · Cetirizina · Formistin · Generit · Prizitec · Sotrizol · Stamidix · Suspiria · Tezastin · Zirtec 
Allemax · Celerg · Cetirizina · Cetirizina Pxgpharma · Reactin · Zyrtec 
Allacan · AllerTek · BecoAllergy · Bell's · Benadryl · Benadryl Allergy · Benadryl Allergy Children's 6+ · Benadryl One A Day · Benadryl One A Day Relief · Care Hayfever and Allergy · Cetec · Cetirizine · Cetirocol · Galpharm Hayfever and Allergy Relief · Lloydspharmacy Hayfever and Allergy Relief · Numark Hayfever & Allergy Relief · Piriteze Allergy · Pollenshield Hayfever · Pollenshield Hayfever Relief · Sentanase · Ziralton Allergy Relief for Children · Zirtek · Zirtek Allergy · Zirtek Allergy Relief for Children 
Alnok · Benaday · Cetimax · Cetiriva · Cetirizin · Vialerg · Zyrtec 
Cetimax · Cetirizin · Zyrtec 
Alermed · Alerzina · AlleMax · Allertec · Amertil · Amertil Bio · CetAlergin · Cetigran · Cetip · Cetirizine · Cetoalergedd · Cetririzinum · Cetrix · Letizen · Zyrtec 
Cetirizine · Reactine · Zyrtec 
Cetirizin · Cetirizine · Histasín · Zensitin 
Cetimax · Cetirizin · Heinix · Histec · Zyrtec 
Aceterin · Alyr · Cetirizin · Cetirizine · Cetrix · Zyrtec 
Alergosan · Cetirizin · Letizen
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