Levocetirizine: A review of its use in the management of allergic rhinitis and skin allergies

Drugs

Volumn 66, Issue 7, 2006, Pages 973-996

  Hair, Philip I ^a   Scott, Lesley J ^a  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

Author keywords

Allergic disorders; Allergic rhinitis; Asthma; Levocetirizine; Pharmacodynamics; Pharmacokinetics; Skin disorders; Therapeutic use; Urticaria

Indexed keywords

ALLERGEN; CETIRIZINE; CROMOGLYCATE DISODIUM; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 2E1; CYTOCHROME P450 3A4; DESLORATADINE; DEXTROCETIRIZINE; EBASTINE; FEXOFENADINE; HISTAMINE H1 RECEPTOR; HISTAMINE H1 RECEPTOR ANTAGONIST; LEVOCETIRIZINE; LORATADINE; MIZOLASTINE; PLACEBO; PREDNISOLONE; UNCLASSIFIED DRUG; XAZAL; XOZAL; XUZAL; XYSAL; XYZALL;

ALLERGIC RHINITIS; ANTIINFLAMMATORY ACTIVITY; AREA UNDER THE CURVE; ASTHENIA; BINDING AFFINITY; CARDIOVASCULAR SYSTEM; CENTRAL NERVOUS SYSTEM; CHRONIC DISEASE; CLINICAL FEATURE; CLINICAL PRACTICE; CLINICAL TRIAL; COGNITION; DOSE RESPONSE; DROWSINESS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG ERUPTION; DRUG EXCRETION; DRUG HALF LIFE; DRUG INHIBITION; DRUG MARKETING; DRUG METABOLISM; DRUG POTENCY; DRUG POTENTIATION; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG TOLERABILITY; DRUG USE; ENANTIOMER; FATIGUE; GASTROINTESTINAL DISEASE; HAY FEVER; HUMAN; IDIOPATHIC DISEASE; IMMUNOPATHOLOGY; IN VITRO STUDY; IN VIVO STUDY; ISOTOPE LABELING; LICENSING; MAXIMUM ALLOWABLE CONCENTRATION; MEDIASTINUM DISEASE; PALLIATIVE THERAPY; PERENNIAL RHINITIS; PRIMARY HEALTH CARE; PSYCHOMOTOR ACTIVITY; QUALITY OF LIFE; RESPIRATORY TRACT DISEASE; REVIEW; SEDATION; SIDE EFFECT; SKIN ALLERGY; SKIN DISEASE; SOMNOLENCE; STEADY STATE; TABLET FORMULATION; THORAX DISEASE; TREATMENT WITHDRAWAL; URTICARIA; WEIGHT GAIN; XEROSTOMIA;

CETIRIZINE; CLINICAL TRIALS; HISTAMINE H1 ANTAGONISTS, NON-SEDATING; HUMANS; HYPERSENSITIVITY; PIPERAZINES; RHINITIS; RHINITIS, ALLERGIC, PERENNIAL; RHINITIS, ALLERGIC, SEASONAL; SKIN DISEASES; TREATMENT OUTCOME;

EID: 33744958406     PISSN: 00126667     EISSN: 00126667     Source Type: Journal    
DOI: 10.2165/00003495-200666070-00017     Document Type: Review

References (91)

1. Bousquet J, van Cauwenberge P, Khaltaev N. Allergic rhinitis and its impact on asthma. ARIA Workshop Group. J Allergy Clin Immunol 2001; 108 (5 Suppl.): S147-334
2. Bellanti JA, Wallerstedt DB. Allergic rhinitis update: epidemiology and natural history. Allergy Asthma Proc 2000; 21: 367-70
3. Tripathi A, Patterson R. Impact of allergic rhinitis treatment on quality of life. Pharmacoeconomics 2001; 19 (9): 891-9
4. van Wijk RG, Canonica GW. Freedom to enjoy life - the ultimate goal in allergy management. Clin Exp Allergy Rev 2006; 6: 15-9
5. Mullol J, Bachert C, Bousquet J. Management of persistent allergic rhinitis: evidence-based treatment with levocetirizine. Ther Clin Risk Manage 2005; 1 (4): 265-71
6. Kapp A, Wedi B. Chronic urticaria: clinical aspects and focus on a new antihistamine, levocetirizine. J Drugs Dermatol 2004; 3 (6): 632-9
7. Baiardini I, Giardini A, Pasquali M, et al. Quality of life and patients' satisfaction in chronic urticaria and respiratory allergy. Allergy 2003; 58 (7): 621-3
8. van Cauwenberge P, Bachert C, Passalacqua G, et al. Consensus statement on the treatment of allergic rhinitis. European Academy of Allergology and Clinical Immunology. Allergy 2000; 55 (2): 116-34
9. Zuberbier T. Urticaria. Allergy 2003; 58 (12): 1224-34
10. Bousquet J, van Cauwenberge P, Khaltaev N, et al. Allergic rhinitis and its impact on asthma (ARIA): in collaboration with the World Health Organization. Allergy 2002; 57 (9): 841-55
11. Kozel MMA, Sabroe RA. Chronic urticaria: aetiology, management and current and future treatment options. Drugs 2004; 64 (22): 2515-36
12. Curran MP, Scott LJ, Perry CM. Cetirizine: a review of its use in allergic disorders. Drugs 2004; 64 (5): 523-61
13. 1-antihistamine for the treatment of allergic rhinitis. Expert Rev Clin Immunol 2005; 1 (4): 495-510
14. 194. Mol Pharmacol 2002; 61: 391-9
15. 1 receptor antagonists. Eur J Pharmacol 2006; 530 (3): 205-14
16. 1 antagonists: receptor affinity versus selectivity. Inflamm Res 2003; 52 Suppl. 1: S49-50
17. Devalia JL, De Vos C, Hanotte F, et al. A randomized, double-blind, crossover comparison among cetirizine, levocetirizine, and ucb 28557 on histamine-induced cutaneous responses in healthy adult volunteers. Allergy 2001; 56 (1): 50-7
18. Popov T, Dimitrov V, Bachvarova A, et al. A comparison of different doses of levocetirizine and desloratadine in the histamine-induced wheal and flare response in the skin of healthy subjects [poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
19. Denham KJ, Boutsiouki P, Clough GF, et al. Comparison of the effects of desloratadine and levocetirizine on histamine-induced wheal, flare and itch in human skin. Inflamm Res 2003; 52 (10): 424-7
20. Grant JA, Riethuisen J-M, Moulaert B, et al. A double-blind, randomized, single-dose, crossover comparison of levocetirizine with ebastine, fexofenadine, loratadine, mizolastine, and placebo: suppression of histamine-induced wheal-and-flare response during 24 hours in healthy male subjects. Ann Allergy Asthma Immunol 2002 Feb; 88 (2): 190-7
21. Purohit A, Melac M, Pauli G, et al. Twenty-four-hour activity and consistency of activity of levocetirizine and desloratadine in the skin. Br J Clin Pharmacol 2003 Oct; 56 (4): 388-94
22. Hindmarch I, Johnson S, Meadows R, et al. The acute and subchronic effects of levocetirizine, cetirizine, loratadine, promethazine and placebo on cognitive function, psychomotor performance, and weal and flare. Curr Med Res Opin 2001; 17 (4): 241-55
23. Klos K, Kruszewski J, Bant A. The effect of various antihistamines after a single and a continuous (over 5 days) administration on the histamine-induced wheal, flare and skin blood flow: a randomised, double-blind, placebo controlled trial [poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
24. Larbig M, Stamm H, Casper A, et al. Twenty-four hour anti-H1 activity of levocetirizine measured by thermography is superior to fexofenadine [poster]. 23rd Congress of the European Academy of Allergology and Clinical Immunology; 2004 Jun 13-16; Amsterdam
25. Wang DY, Hanotte F, De Vos C, et al. Effect of cetirizine, levocetirizine, and dextrocetirizine on histamine-induced nasal response in healthy adult volunteers. Allergy 2001 Apr; 56 (4): 339-43
26. Passalacqua G, Guerra L, Compalati E, et al. Comparison of the effects in the nose and skin of a single dose of desloratadine and levocetirizine over 24 hours. Int Arch Allergy Immunol 2004; 135 (2): 143-7
27. Frossard N, Purohit A, Becker J, et al. Inhibition of allergen-induced wheal and flare reactions by levocetirizine and desloratadine: a double-blind placebo-controlled study [abstract no. P03.87 plus poster]. 14th Congress of the European Academy of Dermatology and Venereology; 2005 Oct 12-16; London
28. Deruaz C, Leimgruber A, Berney M, et al. Levocetirizine better protects than desloratadine in a nasal provocation with allergic gen. J Allergy Clin Immunol 2004 Apr; 113 (4): 669-76
29. Simons FER, Simons KJ. Levocetirizine: pharmacokinetics and pharmacodynamics in children age 6 to 11 years. J Allergy Clin Immunol 2005 Aug; 116 (2): 355-61
30. Cranswick N, Turzíková J, Fuchs M, et al. Levocetirizine in 1-2 year old children: pharmacokinetic and pharmacodynamic profile. Int J Clin Pharmacol Ther 2005 Apr; 43 (4): 172-7
31. 1 receptor antagonism by cetirizine in isolated guinea pig tissues: influence of receptor reserve and dissociation kinetics. Eur J Pharmacol 2003; 470 (1-2): 87-94
32. Michel L, Jean-Louis F, Dubertret L. Pharmacological study of levocetirizine in IgE-dependent hypersensitivity cutaneous reaction in grass pollen allergic volunteers: demonstration of mediator release and eosinophil recruitment modulation by levocetirizine [abstract no. 458 plus poster]. 20th Congress of the European Academy of Allergology and Clinical Immunology; 2001 May 9-13; Berlin
33. Ciprandi G, Cirillo I-G, Vizzaccaro A, et al. Levocetirizine improves nasal obstruction and modulates cytokine pattern in patients with seasonal allergic rhinitis: a pilot study. Clin Exp Allergy 2004; 34 (6): 958-64
34. Lee DKC, Gardiner M, Haggart K, et al. Comparative effects of desloratadine, fexofenadine, and levocetirizine on nasal adenosine monophosphate challenge in patients with perennial allergic rhinitis. Clin Exp Allergy 2004; 34 (4): 650-3
35. Lee DKC, Gray RD, Wilson AM, et al. Single and short-term dosing effects of levocetirizine on adenosine monophosphate bronchoprovocation in atopic asthma. Br J Clin Pharmacol 2004 Jul; 58 (1): 34-9
36. Gandon JM, Allain H. Lack of effect of single and repeated doses of levocetirizine, a new antihistamine drug, on cognitive and psychomotor functions in healthy volunteers. Br J Clin Pharmacol 2002 Jul; 54 (1): 51-8
37. Verster JC, Volkerts ER, van Oosterwijck AWAA, et al. Acute and subchronic effects of levocetirizine and diphenhydramine on memory functioning, psychomotor performance, and mood. J Allergy Clin Immunol 2003 Mar; 111 (3): 623-7
38. Verster JC, de Weert AM, Bijtjes SIR, et al. Driving ability after acute and sub-chronic administration of levocetirizine and diphenhydramine: a randomized, double-blind, placebo-controlled trial. Psychopharmacology (Berl) 2003; 169: 84-90
39. Ciprandi G, Cirillo I, Vizzaccaro A, et al. Desloratadine and levocetirizine improve nasal symptoms, airflow, and allergic inflammation in patients with perennial allergic rhinitis: a pilot study. Int Immunopharmacol 2005 Dec; 5 (13-14): 1800-8
40. Pellet C, Jean-Louis F, Boland S, et al. Levocetirizine decreases VCAM-1 expression induced by TNF-alpha in human dermal endothelial cells through down-regulation of NF-kappaB pathway [abstract no. 268]. 34th Annual Meeting of the European Society for Dermatological Research; 2004 Sep 9-11; Vienna
41. Thomson L, Blaylock MG, Sexton DW, et al. Cetirizine and levocetirizine inhibit eotaxin-induced eosinophil transendothelial migration through human dermal or lung microvascular endothelial cells. Clin Exp Allergy 2002; 32 (8): 1187-92
42. Wu P, Mitchell S, Walsh GM. A new antihistamine levocetirizine inhibits eosinophil adhesion to vascular cell adhesion molecule-1 under flow conditions. Clin Exp Allergy 2005; 35 (8): 1073-9
43. Petecchia L, Serpero L, Silvestri M, et al. Downregulation of vascular adhesion molecule (VCAM)-1 expression by nasal fibroblasts by levocetirizine in vitro [abstract no. P872]. Eur Respir J 2004 Sep; 24 Suppl. 48: 129s
44. Michel L, Jean-Louis F, Boland S, et al. Inhibition by levocetirizine of VCAM-1 production in human dermal endothelial cells in vitro. Blockage of NF-κB and possible mechanism of antiallergic action [poster]. 22nd Congress of the European Academy of Allergology and Clinical Immunology; 2003 Jun 7-11; Paris
45. 14C] levocetirizine, the R enantiomer of cetirizine, in healthy volunteers. Eur J Clin Pharmacol 2001 Oct; 57: 571-82
46. Baltes E, Coupez R, Giezek H, et al. Absorption and disposition of levocetirizine, the eutomer of cetirizine, administered alone or as cetirizine to healthy volunteers. Fundam Clin Pharmacol 2001 Aug; 15 (4): 269-77
47. 1-receptor antagonist, in humans. Fundam Clin Pharmacol 2002 Dec; 16 (6): 471-8
48. 1-antihistamine cetirizine [poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
49. Whomsley R, Gerin B, Brochot A, et al. Transport characteristics of cetirizine and levocetirizine in Caco-2 cell monolayers [poster]. 22nd Congress of the European Academy of Allergology and Clinical Immunology; 2003 Jun 7-11; Paris
50. UCB Pharma Limited. Xyzal 5mg film-coated tablets [online]. Available from URL: http://emc.medicines.org.uk/emc/ industry/default.asp?page=displaydoc. asp&documentid=17193 [Accessed 2006 Feb 10]
51. Whomsley R, Strolin Benedetti M. Development of new H1 antihistamines: the importance of pharmacokinetics in the evaluation of safe and therapeutically effective agents. Curr Med Chem 2005; 4: 451-64
52. Molimard M, Diquet B, Strolin Benedetti M. Comparison of pharmacokinetics and metabolism of desloratadine, fexofenadine, levocetirizine and mizolastine in humans. Fundam Clin Pharmacol 2004 Aug; 18 (4): 399-411
53. Bertrand B, Eloy P. Levocetirizine is highly effective in patients with seasonal allergic rhinitis not responding to treatment with other antihistamines: an open multicentre study in Belgium (Xpoll) [abstract 723 and poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
54. Jorissen M, Hellings P, Bertrand B, et al. Levocetirizine is highly effective on seasonal allergic rhinitis during high pollen counts: an open multicenter study in Belgium [poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
55. Didier A. Efficacy of levocetirizine in perennial allergic rhinitis (PAR) as measured by the number of comfortable days [abstract no. P840]. Eur Respir J 2004; 24 Suppl. 48: 124s. Plus poster presented at the 14th Congress of the European Respiratory Society; 2004 Sep 4-8; Glasgow
56. Bachert C, Demarteau N. Levocetirizine reduces asthma comorbidity in patients with persistent allergic rhinitis: an exploratory analysis of the XPERT™ trial [abstract and poster]. 24th Congress of the European Academy of Allergology and Clinical Immunology; 2005 Jun 26-Jul 1; Munich
57. Kapp A, Danniau A. Levocetirizine reduces significantly the "time to non-compliance" in CIU patients [poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
58. Karppinen A, Brummer-Korvenkontio H, Burri P, et al. Levocetirizine is effective for delayed mosquito-bite reactions [poster]. 14th Congress of the European Academy of Dermatology and Venereology; 2005 Oct 12-16; London
59. Reunala T, Karppinen A, Hervé J-P, et al. Levocetirizine in the treatment of mosquito-bite allergy [poster]. 19th Congress of the World Allergy Organization; 2005 Jun 26-Jul 1; Munich
60. Klimek L, Hundorf I. Levocetirizine in allergic diseases. An open multicentre practice study on efficacy and safety [in German]. Allergologie 2002; 25 (1 Suppl.): S1-7
61. de Blic J, Wahn U, Billard E, et al. Levocetirizine in children: evidenced efficacy and safety in a 6-week randomized seasonal allergic rhinitis trial. Pediatr Allergy Immunol 2005 May; 16 (3): 267-75
62. Leynadier F, Mees K, Arendt C, et al. Efficacy and safety of levocetirizine in seasonal allergic rhinitis. Acta Otorhinolaryngol Belg 2001; 55 (1): 305-12
63. Day JH, Briscoe MP, Rafeiro E, et al. Comparative clinical efficacy, onset and duration of action of levocetirizine and desloratadine for symptoms of seasonal allergic rhinitis in subjects evaluated in the Environmental Exposure Unit (EEU). Int J Clin Pract 2004 Feb; 58 (2): 109-18
64. Stübner P, Zieglmayer R, Horak F. A direct comparison of the efficacy of antihistamines in SAR and PAR: randomised, placebo-controlled studies with levocetirizine and loratadine using an environmental exposure unit. The Vienna Challenge Chamber (VCC). Curr Med Res Opin 2004; 20 (6): 891-902
65. Horak F, Zieglmayer PU, Zieglmayer R, et al. Levocetirizine has a longer duration of action on improving total nasal symptoms score than fexofenadine after single administration. Br J Clin Pharmacol 2005 Jul; 60 (1): 24-31
66. Potter PC, Bailey MJ, Bateman M, et al. Levocetirizine is effective for symptom relief including nasal congestion in adolescent and adult (PAR) sensitized to house dust mites. Allergy 2003; 58 (9): 893-9
67. Potter PC. Efficacy and safety of levocetirizine on symptoms and health-related quality of life of children with perennial allergic rhinitis: a double-blind, placebo-controlled randomized clinical trial. Paediatric Levocetirizine Study Group. Ann Allergy Asthma Immunol 2005 Aug; 95 (2): 175-80
68. Bachert C, Bousquet J, Canonica GW, et al. Levocetirizine improves quality of life and reduces costs in long-term management of persistent allergic rhinitis. J Allergy Clin Immunol 2004 Oct; 114 (4): 838-44
69. Ciprandi G, Cirillo I-G, Vizzaccaro A, et al. Levocetirizine improves nasal symptoms and airflow in patients with persistent allergic rhinitis: a pilot study. Allerg Immunol (Paris) 2005 Jan; 37 (1): 25-9
70. Kapp A, Pichler WJ. Levocetirizine is an effective treatment in patients suffering from chronic idiopathic urticaria: a randomized, double-blind, placebo-controlled, parallel, multicenter study. Int J Dermatol 2006; 45 (4): 469-74
71. Nettis E, Colanardi MC, Barra L, et al. Levocetirizine in the treatment of chronic idiopathic urticaria: a randomised, double-blind, placebo-controlled study. Br J Dermatol 2006 Mar; 154: 533-8
72. Yin R, Hao F, Xiang M-M, et al. A clinical trial of levocetirizine in the treatment of chronic idiopathic urticaria [in Chinese]. J Clin Dermatol 2003 Aug; 32 (8): 477-8
73. Layton D, Wilton LV, Shakir SAW. Safety profile of levocetirizine as used in general practice in England: results of a prescription-event monitoring study [abstract no. 222]. Pharmacoepidemiol Drug Saf 2004 Jul; 13 Suppl. 1: S112
74. Guptha SD, Prabhakar SM, Sacchidanand S. Fixed drug eruption due to levocetirizine [letter]. Indian J Dermatol Venereol Leprol 2005; 71 (5): 361-2
75. Mahajan VK, Sharma NL, Sharma VC. Fixed drug eruption: a novel side-effect of levocetirizine [letter]. Int J Dermatol 2005; 44 (9): 796-8
76. Kränke B, Mayr-Kanhäuser S. Urticarial reaction to the antihistamine levocetirizine dihydrochloride. Dermatology 2005 Jan; 210 (3): 246-7
77. UCB GmbH. Xyzal oral drops. Kerpen, Germany, 2005 Oct 4
78. Data on file. UCB, 2006 Apr 22
79. Sly RM. Changing prevalence of allergic rhinitis and asthma. Ann Allergy Asthma Immunol 1999 Mar; 82 (3): 233-52
80. Linneberg A, Nielsen NH, Madsen F, et al. Increasing prevalence of allergic rhinitis symptoms in an adult Danish population. Allergy 1999; 54 (11): 1194-8
81. Johansson SGO, Haahtela T. World Allergy Organization guidelines for prevention of allergy and allergic asthma: condensed version. Int Arch Allergy Immunol 2004; 135 (1): 83-92
82. Demoly P, Allaert F-A, Lecasble M, et al. Validation of the classification of ARIA (Allergic Rhinitis and its Impact on Asthma). Programme de Recherches Appliquées à la Gestion des Maladies Allergiques. Allergy 2003; 58 (7): 672-5
83. Onrust SV, Lamb HM. Mometasone furoate: a review of its intranasal use in allergic rhinitis. Drugs 1998; 56 (4): 725-45
84. Ring J, Brockow K, Ollert M, et al. Antihistamines in urticaria. Clin Exp Allergy 1999; 29 Suppl. 1: 31-7
85. UCB Pharma. Xyzal® is the first and only antihistamine licensed for persistent allergic rhinitis [media release]. 2004 Dec 23
86. UCB Pharma. UCB Pharma: clash of the titans: world's first head-to-head data on newest antihistamines has implications for hay fever patients [media release]. 2002 Dec 4
87. 1-receptor antagonists. Biochem Pharmacol 2003; 66 (7): 1123-6
88. 2LEN/EDF guideline: definition, classification and diagnosis of urticaria. Allergy 2006; 61 (3): 316-20
89. 1 antihistamines: clinical relevance. Am J Med 2002; 113 (9A): 38-46S
90. Kapp A, Demarteau N. Cost effectiveness of levocetirizine in chronic idiopathic urticaria: a pooled analysis of two randomised controlled trials. Clin Drug Invest 2006; 26 (1): 1-11
91. Bousquet J, Demarteau N, Mullol J, et al. Costs associated with persistent allergic rhinitis are reduced by levocetirizine. Allergy 2005; 60 (6): 788-94