A Double Dose of Levocetirizine Leads to Better Control of Histamine-Induced Flare, Wheal and Itch in Healthy Donors

Abstract

Levocetirizine is classified as a nonsedating second-generation antihistamine. This drug is used to treat allergic disorders such as urticaria and pruritus. Thus far, studies have demonstrated an increase in efficacy for refractory urticaria by increasing doses of antihistamines; however, more lines of supportive evidence for these guidelines are required to justify this management strategy. In this study, we found that a double dose of levocetirizine suppressed histamine-induced flare formation more rapidly and sustainably, and wheal and itch more extensively, compared with the conventional dose using both visual and laser Doppler imaging scales in a noninvasive manner. These results suggest that double-dosed levocetirizine treatment suppresses histamine-induced skin symptoms more rapidly, profoundly and sustainably than conventionally dosed levocetirizine treatment.

Efficacy of increased dose of rupatadine up to 20 mg on itching in Japanese patients due to chronic spontaneous urticaria, dermatitis, or pruritus: A post hoc analysis of phase III clinical trial

“…Oral antihistamines such as rupatadine, a dual‐acting selective oral H1 antagonist, are used for alleviating pruritus associated with cutaneous diseases safely and promptly . However, studies on the efficacy of antihistamine updosing for pruritus‐targeting patients other than urticaria are scarce . The current additional subgroup analysis focused on the effect of rupatadine on patients with heterogeneous characteristics such as varied baseline cutaneous conditions and updose timing to 20 mg for the purpose of interpreting the possible influence of the said factors on the improvement of symptoms for patients suffering from itch.…”

“…12 However, studies on the efficacy of antihistamine updosing for pruritus-targeting patients other than urticaria are scarce. 5,6 The current additional subgroup analysis if the baseline score is <4.5 (Table 1). This finding suggests the potential use of the baseline TPS as a pretreatment predictive marker for the necessity of updose to 20 mg. Further investigation on this matter is worth conducting.…”

“…In patients with pruritus, antihistamines are recommended in addition to appropriate skin care and other protective measures in Japan . However, not many studies have focused on the efficacy of updose and its association with baseline conditions and timing of response to the drug prior to updose …”

“…4 However, not many studies have focused on the efficacy of updose and its association with baseline conditions and timing of response to the drug prior to updose. 5,6 Rupatadine is a second-generation antihistamine with minimal anticholinergic and sedative side effects due to its high selective antagonism. 7 Rupatadine mechanism of action is characterized by its unique molecular structure: the lutidinyl group, which antagonizes platelet-activating factor (PAF) receptors, and the piperidinyl group, which antagonizes histamine H1 receptor.…”

Evaluation of the antihistamine effects of olopatadine and levocetirizine during a 24‐h period: A double‐blind, randomized, cross‐over, placebo‐controlled comparison in skin responses induced by histamine iontophoresis

“…These results indicate that adequate antihistamines should be prescribed for patients while considering the efficacy and duration of the antihistamine effect, especially in patients with severe symptoms. Very recently, an article which supports our results has been published. The article, published by Kabashima's group, demonstrated that double dose of levocetirizine inhibited iontophoresis‐induced skin reactions more strongly, more rapidly and more sustainably than a single administration of the drug.…”