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

Grant, A.; Riethuisen, Jean Michel; Moulaert, Béatrice; Devos, C

doi:10.1016/s1081-1206(10)61995-3

Cited by 142 publications

(82 citation statements)

References 26 publications

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“…When compared to other 2 nd generation AH, such as desloratadine, levocetirizine appears to be more effective in inhibiting wheal and fl are response. 126,127 Ebastine, fexofenadine, cetirizine and mizolastine rank next and have similar skin effects. Superior effi cacy of ebastine (20 mg) was found in comparison to cetirizine (10 mg) or loratadine (10 mg) on the overall skin wheal response after single and multiple doses, 127 with a longer-acting effect than fexofenadine as well.…”

Section: Variability Factorsmentioning

confidence: 99%

Skin prick tests and allergy diagnosis

Antunes

Borrego

Romeira

et al. 2009

Allergologia et Immunopathologia

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Skin testing remains an essential diagnostic tool in modern allergy practice. A signifi cant variability has been reported regarding technical procedures, interpretation of results and documentation. This review has the aim of consolidating methodological recommendations through a critical analysis on past and recent data. This will allow a better understanding on skin prick test (SPT) history; technique; (contra-) indications; interpretation of results; diagnostic pitfalls; adverse reactions; and variability factors. Skin has an important physiological role in the internal balance homeostasis and constitutes a crucial barrier against external aggressions, with well-known immunological properties. 1 It has been used by allergists for decades as an easily assessed laboratory of the immunological status of the individual.The fi rst skin testing technique was developed by Charles H. Blackley in 1865, a Manchester homeopathic physician with allergic rhinitis. He abraded a quarter-inch area of his skin with a lancet and then applied grass pollen grains. 2 The so-called scratch test was later adopted by Schloss for the diagnosis of food allergy in children. 3 Epicutaneous tests can be divided into scratch tests and prick/puncture tests. The fi rst method, proposed by Blackley 2 , implied a linear scratch without drawing blood and could either be performed fi rst, with the extract then dropped on the abraded skin, or be made through a drop of extract. 4 Although it was used extensively in the past, this technique became progressively obsolete due to patient discomfort, poor reproducibility, possible residual lesions and newer and innocuous procedures. 4 Therefore, scratch test is mentioned here for historical purposes only. It was Sir Thomas Lewis who, in 1924, fi rst applied skin prick tests (SPT). 5 Nevertheless, their generalised use in clinical practice only became a reality about 30 years ago, as a result of technique modifi cations proposed by Pepys. 6 For the purpose of this review and for easier comprehension, skin testing will be referred interchangeably as SPT, whatever device is used for its application.In 1966, Ishizaka's work on immunoglobulin E (IgE) and immediate hypersensitivity reactions 7 established the scientifi c corpus to what was done till then on a strictly empiric basis.As written by Dr Walzer in 1974, "the fact that skin testing has not turned out to be a simple and completely reliable technique does not detract from the fact that, when it is intelligently and skilfully performed, it remains the most effective diagnostic procedure in reaginic allergic disorders". 8 The reliability of skin testing and proper documentation of test results are essential in allergy practice. A recent survey to all physician members and fellows of the American College of Allergy, Asthma and Immunology practicing in the

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Section: Variability Factorsmentioning

confidence: 99%

Skin prick tests and allergy diagnosis

Antunes

Borrego

Romeira

et al. 2009

Allergologia et Immunopathologia

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“…It has been chemically proved that the half dosage form of LCD (2.5 mg) has comparable antihistaminic activity to normal amount (5.0 mg) of cetirizine in the treatment of allergic rhinitis and chronic idiopathic urticaria (Devalia et al, 2001;Grant et al, 2002).…”

Section: Levocetirizine Dihydrochloride (Lcd) Chemically Is (2-[4-[(mentioning

confidence: 99%

Bioanalytical Method Development and Validation for the Determination of Levocetirizine in Pharmaceutical Dosage Form and Human Plasma by RP-HPLC

Jain¹,

Jain²,

Jain³

et al. 2016

J App Pharm Sci

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This study describes the development of a rapid, selective, precise and sensitive reverse phase high -performance liquid chromatography method for the quantitative determination of Levocetirizine Dihydrochloride (LCD) in human plasma and pharmaceutical dosage form. Extraction of drug from plasma was done by employing optimized liquid-liquid extraction procedure. The sample was analyzed using Acetonitrile: Methanol: 20mM Ammonium Acetate Buffer pH-5 (25:55:20 % v/v/v) as mobile phase. Chromatographic separation was achieved on Prontosil C-18 column (4.6 x 250mm, 5μ particle size) as stationary phase using isocratic elution (at a flow rate of 1 mL/min). The peak was detected using UV-PDA detector set at 232 nm and retention time was found to be 8 min for LCD. The calibration curve obtained was linear (r 2 = 0.9998) over the concentration range of 2-10 μg/mL. Method was validated for precision, robustness and recovery. The limit of detection (LOD) and limit of quantitation (LOQ) was 0.0057 and 0.174 µg/mL respectively. There was no significant difference between the amount of drug spiked in plasma and the amount recovered and plasma did not interfere in estimation. Thus, the proposed method is suitable for the analysis of LCD in tablet dosage forms and human plasma.

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“…In this study in children,[39] plasma concentrations of drug are near maximum by 30 minutes and yet it takes an additional 1.5 hours for the drug to diffuse into the extravascular space to produce a maximal clinical effect. In adults, the maximal inhibition of the flare response is usually ~4 hours for levocetirizine, fexofenadine, and desloratadine[40-42] but may be longer for drugs, such as loratadine and ebastine, which require metabolism to produce their active moiety[40]. …”

Section: Second-generation H1-antihistaminesmentioning

confidence: 99%

Pharmacology of Antihistamines

Church¹,

Church²

2011

World Allergy Organization Journal

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This article reviews the molecular biology of the interaction of histamine with its H1-receptor and describes the concept that H1-antihistamines are not receptor antagonists but are inverse agonists i.e. they produce the opposite effect on the receptor to histamine. It then discourages the use of first-generation H1-antihistamines in clinical practice today for two main reasons. First, they are less effective than second generation H1-antihistamines. Second, they have unwanted side effects, particularly central nervous system and anti-cholinergic effects, and have the potential for causing severe toxic reactions which are not shared by second-generation H1-antihistamines. There are many efficacious and safe second-generation H1-antihistamines on the market for the treatment of allergic disease. Of the three drugs highlighted in this review, levocetirizine and fexofenadine are the most efficacious in humans in vivo. However, levocetirizine may cause somnolence in susceptible individuals while fexofenadine has a relatively short duration of action requiring twice daily administration for full all round daily protection. While desloratadine is less efficacious, it has the advantages of rarely causing somnolence and having a long duration of action. Lastly, all H1-antihistamines have anti-inflammatory effects but it requires regular daily dosing rather than dosing 'on-demand' for this effect to be clinically demonstrable.

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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

Cited by 142 publications

References 26 publications

Skin prick tests and allergy diagnosis

Skin prick tests and allergy diagnosis

Bioanalytical Method Development and Validation for the Determination of Levocetirizine in Pharmaceutical Dosage Form and Human Plasma by RP-HPLC

Pharmacology of Antihistamines

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