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
This list comprises raw data collected from different countries.
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Bold names are the searchable terms, while the gray names that follow are all mapped to the bolded term.
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Albert Heijn Hooikoortstabletten Cetirizine diHCl 10 mg, filmomhulde tabletten · Allergietabletten HTP Cetirizine diHCl 10 mg, filmomhulde tabletten · Cetirizine 2HCl Sandoz 10 mg, filmomhulde tabletten · Cetirizine 2HCl Teva 1 mg/ml, drank · Cetirizine diHCl Aurobindo 10 mg, filmomhulde tabletten · Cetirizine diHCl SAM 10 mg, filmomhulde tabletten · Cetirizine diHCl Sanias 10 mg, filmomhulde tabletten · Cetirizine diHCl Teva 10 mg, filmomhulde tabletten · Cetirizine diHCl Triangle Pharma 10 mg hooikoortstabletten, filmomhulde tablettten · Cetirizine diHCl Viatris 10 mg, filmomhulde tabletten · DA Cetirizine diHCl 10 mg, filmomhulde tabletten · Etos Hooikoortstabletten Cetirizine diHCl 10 mg, filmomhulde tabletten · Jumbo hooikoortstabletten Cetirizine diHCI 10 mg, filmomhulde tabletten · Kruidvat Cetirizine diHCl 10 mg Allergietabletten, filmomhulde tabletten · Kruidvat hooikoortstabletten cetirizine diHCl 10 mg, filmomhulde tabletten · Livsane Hooikoortstabletten Cetirizine diHCl 10 mg, filmomhulde tabletten · Prevalin Allerstop cetirizine 10 mg, filmomhulde tabletten · Reactine 10 mg, filmomhulde tabletten · RXT Cetirizine diHCl 10 mg hooikoortstabletten, filmomhulde tabletten · Trekpleister Cetirizine diHCl 10 mg Allergietabletten, filmomhulde tabletten · Trekpleister hooikoortstabletten cetirizine diHCl 10 mg, filmomhulde tabletten · Zyrtec 1 mg/ml drank · Zyrtec 10 mg filmomhulde tabletten · Zyrtec 10 mg, filmomhulde tabletten 
Cetirizin AB 10 mg compr. pellic. · Cetirizin Aurobindo 10 mg compr. pellic. · Cetirizine EG 10 mg compr. pellic. · Cetirizine Sandoz 1 mg/ml sol. buv. · Cetirizine Sandoz 10 mg compr. pellic. · Cetirizine Teva 10 mg compr. pellic. · Reactine 10 mg compr. pellic. · Zyrtec 10 mg compr. pellic. 
ALERCINA 10 mg COMPRIMIDOS · ALERLISIN 1 mg/ml SOLUCION ORAL · ALERLISIN 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA · ALERLISIN 10 mg/ml GOTAS ORALES EN SOLUCION · Cetirizina · CETIRIZINA ALMUS 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CETIRIZINA ALTER 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CETIRIZINA APOTEX 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CETIRIZINA ARISTO 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Cetirizina Aurovitas 10 mg Comprimidos Recubiertos con Pelicula efg · CETIRIZINA BEXAL 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CETIRIZINA CINFA 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Cetirizina Cipla 1 mg/ml Solucion Oral efg · CETIRIZINA KERN PHARMA 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Cetirizina Mabo 10 mg Comprimidos Recubiertos con Pelicula efg · CETIRIZINA NORMON 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · CETIRIZINA RATIOPHARM 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Cetirizina Sandoz 10 mg Comprimidos Recubiertos con pel?Cula efg · CETIRIZINA SANDOZ 10 mg/ml GOTAS ORALES EN SOLUCION EFG · CETIRIZINA TARBIS 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Cetirizina Tarbis Farma 10 mg Comprimidos Recubiertos con Pelicula efg · CETIRIZINA TEVA 1 mg/ml SOLUCION ORAL EFG · Cetirizina Tevagen 10 mg Comprimidos Recubiertos con Pelicula efg · Cetirizina uxa 10 mg Comprimidos Recubiertos con Pelicula efg · Cetirizina Viatris 10 mg Comprimidos Recubiertos con Pelicula efg · CETIRIZINA ZENTIVA 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG · Zyrtec · ZYRTEC 1 mg/ml SOLUCION ORAL · Zyrtec 10 mg Comprimidos Recubiertos con Pelicula · Zyrtec Comprimidos Recubiertos 
Cerchio · Ceteris · Cetirizina · Formistin · Generit · Prizitec · Sotrizol · Stamidix · Suspiria · Tezastin · Zirtec 
ALLEMAX 10 mg · CELERG 10 mg · CETIRIZINA ARENA 10 mg · CETIRIZINA HELCOR 10 mg · CETIRIZINA LAROPHARM 10 mg · CETIRIZINA PXGPHARMA 10 mg · REACTIN 10 mg · ZYRTEC 10 mg/ml 
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 · Cetirizin Teva · Vialerg · Zyrtec 
Cetimax · Cetirizin Norfri · Cetirizin Sandoz · Cetirizin Viatris · Zyrtec 
Alermed · Alerzina · AlleMax · Allertec · Allertec Kids · Allertec WZF · Amertil · Amertil Bio · CetAlergin · Cetigran · Cetip · Cetirizine Genoptim SPH · Cetoalergedd · Cetririzinum US Pharmacia · Cetrix · Letizen · Zyrtec · Zyrtec UCB 
Cetirizine EG · Reactine · Zyrtec 
Cetirizin STADA · Cetirizine Alvogen · Histas?n · Histasín · Zensitin 
Cetimax · Cetirizin Sandoz · Cetirizin-ratiopharm · Heinix · Histec · Zyrtec 
Aceterin · Alyr · Cetirizin Actavis · Cetirizine Livsane · Cetirizine Siromed · Cetrix · Zyrtec 
Alergosan® · Alergosan® s · Cetirizin SLAVIAMED · Cetirizin Zentiva® · Letizen®
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