Disease relevance of cetirizine

• Two agents recently marketed in the United States, Ioratidine and cetirizine, appear to lack the ability to prolong repolarization and induce torsades de pointes [1].
• RESULTS: Acute urticaria occurred in 16.2% of the placebo-treated children and in 5.8% of the children treated with cetirizine (P <.001) [2].
• A double-blinded, randomized, placebo-controlled trial of cetirizine in preventing the onset of asthma in children with atopic dermatitis: 18 months' treatment and 18 months' posttreatment follow-up [3].
• Early treatment of perennial rhinitis with budesonide or cetirizine and its effect on long-term outcome [4].
• The ability of cetirizine (and perhaps other antihistamines) to inhibit these responses at usual therapeutic doses may be useful in investigating the late allergic reaction [5].

Psychiatry related information on cetirizine

• Cetirizine is associated with sedation or psychomotor impairment in some studies but not in others [6].
• Binding results indicated that the interaction between cetirizine, its enantiomers, and histamine is compatible with a competitive behavior, in contrast with the noncompetitive profile of cetirizine and levocetirizine observed in isolated organs [7].
• A dose-ranging study of the effects of mequitazine on actual driving, memory and psychomotor performance as compared to dexchlorpheniramine, cetirizine and placebo [8].
• Specific review of the psychometric effects of cetirizine [9].
• A low dose of cetirizine decreased the reaction time, whereas an increase in reaction time was found for the high dose [10].

High impact information on cetirizine

• RESULTS: The cumulative potency of each drug in affecting tumor growth or growth mechanisms in the five in vitro assays ranked as follows: Loratidine and astemizole ranked highest and were equally potent, followed in decreasing order by hydroxyzine, doxylamine, and cetirizine [11].
• Although cetirizine has less potential for causing arrhythmias than other histamine 1 blockers, such an interaction should be considered, especially in patients with renal insufficiency who are receiving pilsicainide [12].
• Comment on severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency [13].
• In vitro studies using Xenopus oocytes with microinjected human organic cation transporter 2 and renal cells transfected with human multidrug resistance protein 1 revealed that the transport of the substrates of these transporters was inhibited by either cetirizine or pilsicainide [12].
• The plasma concentrations of both drugs were significantly increased during the coadministration, and the cetirizine concentration decreased on cessation of pilsicainide despite the fact that treatment with cetirizine was continued, which suggested that the fainting was induced by the pharmacokinetic drug interaction [12].

Chemical compound and disease context of cetirizine

• By reviewing published studies of the effectiveness of terfenadine, cetirizine, and loratadine in clinical asthma, evidence for the relevant effect of the second-generation antihistamines on bronchial asthma can be found [14].
• Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria [15].
• Urticaria: clinical efficacy of cetirizine in comparison with hydroxyzine and placebo [16].
• CONCLUSIONS: Cetirizine produced a significant protective effect against an allergen-induced late allergic reaction in a BPT [17].
• Effect of the H2-antagonist cimetidine on the pharmacokinetics and pharmacodynamics of the H1-antagonists hydroxyzine and cetirizine in patients with chronic urticaria [18].

Biological context of cetirizine

• Pharmacokinetics and pharmacodynamics of cetirizine in infants and toddlers [19].
• The results were confirmed in an ensuing double-blind, placebo-controlled study of 16 healthy subjects and 14 adult patients with atopic dermatitis, where ex vivo monocyte chemotaxis was reduced or abolished during cetirizine therapy [20].
• Neither cetirizine nor albuterol uniformly inhibited exercise-induced bronchoconstriction [21].
• Cetirizine, loratadine, or placebo in subjects with seasonal allergic rhinitis: effects after controlled ragweed pollen challenge in an environmental exposure unit [22].
• The subjects underwent double-blind, crossover pretreatments in randomized order in two separate protocols with (1) three daily oral doses of 20 mg of cetirizine and placebo, followed by allergen inhalation, and (2) single oral doses of cetirizine (5, 10, and 20 mg), albuterol (4 mg), and placebo, followed by exercise with cold-air inhalation [21].

Anatomical context of cetirizine

• In vivo effects of cetirizine on cutaneous reactivity and eosinophil migration induced by platelet-activating factor (PAF-acether) in man [23].
• In the skin, cetirizine has been found to reduce eosinophil and neutrophil late-phase infiltration and prostaglandin D2 release [24].
• OBJECTIVE: This prospective, randomized, parallel-group, double-blind, placebo-controlled study was designed to evaluate the safety of the H(1)-antihistamine cetirizine, particularly with regard to central nervous system and cardiac effects, in infants age 6 to 11 months, inclusive [25].
• We also compared the ability of cetirizine and three antihistamines to cross the blood-brain barrier [26].
• Cetirizine inhibits the in vitro and ex vivo chemotactic response of T lymphocytes and monocytes [20].

Associations of cetirizine with other chemical compounds

• Terfenadine, astemizole, loratadine, and cetirizine produce an incidence of central nervous system and anticholinergic adverse effects similar to that produced by placebo [27].
• The effect of both a single dose (15 mg) and 7 days of treatment (15 mg twice daily) with cetirizine, a potent H1 antagonist on bronchoconstriction induced by histamine and leukotriene D4 (LTD4) has been examined in 10 patients with mild atopic asthma in a placebo-controlled, double-blind, crossover study [28].
• Newly available antihistamine preparations, levocetirizine, the R-enantiomer of racemate cetirizine, and desloratadine, an active metabolite of loratadine, have been recently released for allergic rhinitis [29].
• Cetirizine did not modify significantly the allergen inhalation-challenge test, but it inhibited the recruitment of inflammatory cells, mainly eosinophils [30].
• The new H1-receptor antagonist, cetirizine 2 HCl, orally administered with 10 mg once a day to pollen-sensitive patients in a double-blind, crossover study versus placebo, induced a significant decrease in the wheal-and-flare cutaneous reaction induced by intradermal injection of pollen, histamine, and compound 48/80 [31].

Gene context of cetirizine

• Pre-incubation with cetirizine diminished the IL-8 release from cells activated with TNF-alpha or PMA in a significant manner [32].
• RESULTS: Cetirizine at high concentrations (10(2)-10(3) microM) markedly inhibited IFNgamma-induced expression of membrane ICAM-1, HLA-DR and up-regulation of MHC class I, but had no effect on CD40 expression [33].
• Finally, cetirizine, but not hydrocortisone, inhibited the release of MCP-1 and RANTES from IFNgamma-stimulated keratinocytes [33].
• In contrast, nonsedating H1-antagonists cetirizine, loratadine, and desloratadine are P-gp substrates [34].
• In group A, ICAM-1-positive cells decreased from 75.8 (SE +/- 15.12) to 38.8 (SE +/- 7.57) ICAM-3-positive cells decreased from 61.7 (SE +/- 12.72) to 45.2 (SE +/- 9.44) and LFA-1 decreased from 103.9 (SE +/- 17.34) to 66.5 (SE +/- 8.63) after cetirizine treatment (p = 0.02) [35].

Analytical, diagnostic and therapeutic context of cetirizine

• In a double-blind, crossover study, seven subjects allergic to grass pollen and three nonallergic control subjects received orally either cetirizine, 20 mg/day, or placebo for 4 days [23].
• OBJECTIVE: The protective effect of cetirizine on inflammatory changes after ASCC was assessed in 12 patients with rhinoconjunctivitis caused by Parietaria judaica in a double-blind study [36].
• Comparison between nasal provocation tests and skin tests in patients treated with loratadine and cetirizine [37].
• In traditional clinical trials, cetirizine has been shown to be safe and effective for the treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria [22].
• Pretreatment of subjects with cetirizine reduced the number of sneezes induced by antigen challenge but did not significantly reduce levels of histamine or prostaglandin D2 in a double-blind, placebo-controlled trial with the lavage model [38].

References