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News About Cetirizine

20-September-2008 09:55:57 - Cetirizine Cetirizine Systematic IUPAC name ± - 2- 4- 4-chlorophenylphenylmethyl -1- piperazinyl ethoxyacetic acid, dihydrochloride Identifiers CAS number 83881-51-0 ATC code R06AE07 PubChem 2678 DrugBank APRD00630 Chemical data Formula C21H25ClN2O3 Mol. mass 388.89 SMILES eMolecules PubChem Synonyms Alatrol, Alzene, Cetirizina MERCK, Cetirin, Cetzine Glaxo, Cetirizin, Humex, Letizen, Razene, Reactine, Zyrtec, Zirtec, Zodac, Zirtek, Zynor, Zyrlek, Zyllergy Pharmacokinetic data Bioavailability well absorbed Protein binding 93% avg Metabolism CYP3A4 Cytochrome P450 3A4 Half life 8.3 Hours Excretion Hepatic, urine or excrement Small amounts Therapeutic considerations Licence data US Pregnancy cat. BUS Legal status GSLUK OTCUS OTC in Canada Routes Oral Cetirizine hydrochloride, an antihistamine, pronounced /sɛˈtɪrɨziË?n/ is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. The structural similarity of cetirizine to hydroxyzine, and its derivation from piperazine, attribute similar adverse reactions and properties to other piperazine derivatives. Formerly prescription-only in the US and Canada, cetirizine is now available over the counter in both. Contents 1 Clinical description 1.1 Pharmacology 1.2 Administration method and metabolisation 1.3 Levo version 2 Clinical use 2.1 Kimura's disease 3 References 3.1 Books and journals 3.2 External links Clinical description Pharmacology Cetirizine crosses the blood-brain barrier only slightly, eliminating the sedative side-effect common with older antihistamines.1 Administration method and metabolisation Chewable, non-chewable, and syrup forms of cetirizine are similarly absorbed rapidly and effectively, with absorbed food minutely affecting the absorption rate which yields a peak serum level one hour after administration;2 in a study of healthy volunteers prescribed 10mg tablets, once daily for 10 days, a mean peak serum level of 311 ng/mL was observed.3 The metabolic effects of cetirizine are long acting; remaining in the system for a maximum of 21 hours before being excreted, the average elimination half-life is 8 hours.23 70% of the drug is excreted or eliminated by kidney function within 72 hours, and 10% is removed through urine or excrement;23 of which, half is observed as unchanged cetirizine compound.23 Like many other antihistamine medications, cetirizine is commonly prescribed in combination with pseudoephedrine hydrochloride, a decongestant. These combinations are marketed using the same brand name as the cetirizine with a -D suffix Zyrtec-D, Virlix-D, etc. Additionally, cetirizine HCl not sold in combination with pseudoephedrine, is commonly known and marketed under the brand name, Zyrtec. Formerly only available by a prescription, both Zyrtec and Zyrtec-D are currently available over the counter in the United States. In the Philippines, a leading cetirizine is Aforvir. 4 Levo version The levo, or active enantiomer, version of Cetirizine is known as Levocetirizine. It is marketed under the name of Xyzal and Xusal. It is claimed to have somewhat fewer side effects. Clinical use Kimura's disease Cetirizine is an effective agent in the treatment of Kimura's disease, which mostly occurs in young Asian men, affecting the lymph nodes and soft tissue of the head and neck in the form of tumor-like lesions. Cetirizine's properties of being effective both in the treatment of pruritus and as an anti-inflammatory agent5 make it suitable for the treatment of the pruritus associated with these lesions.5 In a 2005 study, the American College of Rheumatology conducted treatments initially using prednisone, followed by steroid dosages and azathioprine, omeprazole, and calcium and vitamin D supplements over the course of two years.6 The skin condition of the patient began to improve and the skin lesions lessened. However, there were symptoms of cushingoid and hirsutism observed before the patient was removed from the courses of steroids and placed on 10mg/day of cetirizine to prevent skin lesions;6an agent suitable for the treatment of pruritus associated with such lesions.6 Asymptomatically, the patient's skin lesions disappeared after treatment with cetirizine, blood eosinophil counts became normal,6 corticosteroid effects were resolved,6 and a remission began within a period 2 months.6 It is also thought that the inhibition of eosinophils may be the key to treatment of Kimura's disease due to the role of eosinophils, rather than other cells with regards to the lesions of the skin.6 References ^ Gupta, Anubha; Chatelain, Pierre; Massingham, Roy; Jonsson, E. Niclas; Hammarlund-Udenaes, Margareta 2005-11-22. Brain Distribution of Cetirizine Enantiomers: Comparison of Three Different Tissue-to-Plasma Partition Coefficients: Kp, Kp,u, and Kp,uu. Drug Metabolism and Disposition 34: 318. doi:10.1124/dmd.105.007211. PMID 16303872. ^ a b c d Anderson, P. O., Knoben, J. E., et al. 2002, p807 ^ a b c d Pfizer Inc, et al. 2006, p3 -- Note; this appears as Page 2 in online print versions. ^ Payne, January W 2008-01-09. Over-the-Counter Zyrtec Is About to Arrive, U.S. News World Report. ^ a b Chetrit, E. B., Amir, G., Shalit, M. 2005, p1. ^ a b c d e f g Chetrit, E. B., Amir, G., Shalit, M. 2005, p2. Books and journals Anderson, P. O., Knoben, J. E., et al. 2002 Handbook of clinical drug data 10th ed. McGraw-Hill International Pfizer Inc, et al. 2006 ZYRTEC cetirizine hydrochloride Tablets, Chewable Tablets and Syrup For Oral Use Pfizer Incorporated publications Chetrit, E. B., Amir, G., Shalit, M. 2005. Cetirizine: an effective agent in Kimura's Disease Arthritis Rheumatism Arthritis care research Vol 53, p117-118 External links Non-print version of cetirizine fact sheet. List of brand names US FDA approves Zyrtec-D for over the counter sales US FDA approves Zyrtec for over the counter sales v d e Histamine antagonists H1 or non-selective Alkylamines Bepotastine Bamipine Brompheniramine Chlorpheniramine Dexbrompheniramine Dexchlorpheniramine Dimethindene Metron S Pheniramine Pyrrobutamine Talastine Thenaldine Tolpropamine Triprolidine Ethanolamines Aminoalkyl ethers Bietanautine Bromazine/Bromodiphenhydramine Carbinoxamine Chlorphenoxamine Clemastine Diphenylpyraline Diphenhydramine Doxylamine Embramine p-Methyldiphenhydramine Moxastine Orphenadrine Phenyltoloxamine Setastine Ethylenediamines Chloropyramine Chlorothen Histapyrrodine Methafurylene Mepyramine Methapyrilene Pyrilamine Talastine Thenyldiamine Thonzylamine Tripelennamine Pyribenzamine Phenothiazine Tricyclics Ahistan Etymemazine Hydroxyethylpromethazine Isopromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine Thiazinamium Other Tricyclics Azatadine Clobenzepam Cyproheptadine Deptropine Isothipendyl Loratidine Piperazine Buclizine Chlorcyclizine Cinnarizine Clocinizine Hydroxyzine Niaprazine Oxatomide Benzhydryl compounds Cyclizine, Meclizine Others including selective, 2nd gen, 3rd gen Antazoline Astemizole Azatadine Azelastine Bepottastine Bamipine Cetoxine Clemizole Clobenztropine Deptropine Desloratadine Dimebon Ebastine Emedastine Epinastine Ketotifen Levocabastine Loratadine Mebhydrolin Mizolastine Phenindamine Pimethixene Pyrrobutamine Rupatadine Thenalidine Tritoqualine Alkylamine Acrivastine Tricyclic Olopatadine Piperazine Levocetirizine, Cetirizine Benzhydryl compounds Fexofenadine, Terfenadine H2 Cimetidine Famotidine Ranitidine Roxatidine Lafutidine Niperotidine Nizatidine H3 A-349,821 ABT-239 Burimamide Ciproxifan Clobenpropit Conessine Impentamine Iodophenpropit Thioperamide VUF-5681 H4 JNJ 7777120 Thioperamide VUF-6002 Retrieved from http://en..org/wiki/Cetirizine Categories: H1 receptor antagonists | Piperazines Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Dansk Deutsch Français Italiano Magyar Nederlands 日本語 Polski ไทย Türkçe 中文 This page was last modified on 12 August 2008, at 18:56

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