Second Generation Antihistamines in Treatment of Urticaria

Samia Elzwi*

Assistant professor, Department of pharmacology. University of Benghazi. Libya

*Correspondence: Samia Elzwi, Department of pharmacology. University of Benghazi, Libya,

Email: Samia.Alzwi@uob.edu.ly

Received: 07 Dec, 2024; Accepted: 25 Dec, 2024; Published: 31 Dec, 2024.

Copyright: © 2025 Samia Elzwi. This is an open-ac cess article distributed under the terms of the Cre ative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited

Abstract

Urticaria is mast cell mediated shin disease characterized by recurrent, transient itchy wheals, angioedema or both. If urticaria lasts less than six weeks, it is categorized as acute urticaria; if it lasts longer than six weeks, it is classified as chronic urticaria. Chronic urticaria is further divided into spontaneous urticaria and inducible urticaria that trigger by specific cause like cold, heat, stress, friction.

Histamine is biogenic amine belongs to group of autocoids and main mediator released from mast cell. Its play’s role in pathogenesis of urticaria, bronchial asthma, allergic rhinitis and many other diseases. However, the first line in the treatment of urticaria is antihistamine drugs especially H1 antagonist which classified into first and second generation, for many years, the first generation has been used to treat urticaria, but its use has decreasedbecause of side effects include sedative, anticholinergic, and various medication interactions.Moreover, the trends towards the use of second generation antihistaminic drugs which plays pivotal role in the treatment of urticaria due to long duration and no sedative side effects.

Introduction:

Urticaria is mast cell mediated shin disease characterized by recurrent, transient itchy wheals, angioedema or both. If urticaria is lasts less than 6 weeks is categized as acute urticaria and chronic urticaria if it last more than 6 weeks [1].Histamine is biogenic amine belongs to group of autocoids and formed by decarboxylation of histidine-by-histidine decarboxylase and main mediator released from mast cell plays role in pathogenesis of urticaria, bronchial asthma, allergic rhinitis and many other diseases. However, the first line in the treatment of urticaria is antihistamine drugs especially H1 antagonist which classified into first and second generation, first generation cross blood brain barrier causes sedative effect and impair congestive function. Furthermore, it classified into different chemical subgroup’s like Alkylamines (chlorpheniramine),Piperazines (hydroxyzine), Piperidines (cyproheptadine), and Ethanolamine (diphenhydramine) [2].

Second generation antihistamine is now most commonly used in the treatment of urticaria Cetirizine, desloratadine, fexofenadine, levocetirizine, and loratadine are examples of second-generation H1 antihistamines that cross the blood-brain barrier considerably less than their predecessors.

However, first H1 receptor antagonist has in non-selective action on H1 receptor so in addition to blocking H1 receptor the drugs have affinity for Muscarinic, Alpha receptors and serotonin receptor this leads to multiple adverse effects when used these drugs in treatment of urticaria and many allergic and non-allergic diseases.

Method: In order to conduct this systematic review, we searched the medical literature for studies that discussed the use of antihistamine especially second generation H1 antagonist in patients from October to December 2024, an English only literature search was conducted utilizing the electronic databases of MEDLINE (via PUBMED), EMBASE, SCOPUS, OVID, and Cochrane Library Only publications that had undergone peer review were used in the final Analysis and key words were employed Urticaria , H1 antagonist , first generation and second generation . Additionally, we looked through the references of the most pertinent review articles for any new research that our original literature search had miss.

According to Literature Review

Findings We found 8 RCTs with 680 patients. Intramuscular first-generation H1-antihistamine was more effective than H2-blockers in reducing pruritus symptoms (SMD, −0.38; 95 percent confidence interval [CI], −0.75 to −0.02) in the ED setting (2 trials, n=118). However, it also had more sedative effects.).Better clinical outcomes had been demonstared with Intravenous second-generation H1-antihistamine (sgAH than intravenous first generation antihistamine in the ED setting, with a lower risk of return to any ED/clinic (OR, 0.31; 95 percent CI, 0.12-0.83) and a lower risk of any adverse event (OR, 0.24; 95 percent CI, 0.09-0.63), while also improving pruritus symptoms to a comparable degree (2 trials, n=295) [3].

The test second generation antihistamine at standard dose showed significant statistical superiority over placebo in all placebo-controlled studies, confirming its efficacy and safety in the treatment of chronic urticaria. Hide and associates. In treating urticaria, found that bilastine 20mg once daily or 10mg once daily significantly improved tolerability and efficacy when compared to a placebo. Levocetirizine 5 mg Once Daily (OD) was shown in two studies to be safer and more effective than a placebo in the treatment of urticaria. Three studies each reported a significant advantage of desloratadine 5 mg Once Daily (OD), and rupatadine 10mg OD over placebo. According to two studies, fexofenadine 180 mg OD significantly outperformed a placebo in terms of tolerability, safety, and effectiveness, Nelson etal, stated that fexofenadine significantly improved their quality of life and sleep [4].

Moreover, in another study the key to determining the causes of treatable acute urticaria is a thorough clinical history. As the first line of treatment, oral second-generation antihistamine ought to be extensively accessible. In cases of moderate-to-severe urticaria or if symptoms continue, it may be helpful to at least double the usual dosage of the low sedative potential second generation antihistamine. In instances of severe acute urticaria, particularly in children experiencing notable or primarily angioedema, the addition of short-term oral corticosteroids may be considered.

For evidence-based recommendations to be supported, clinical trials involving larger pediatric populations are required [5].

All of the reviewed articles agreed that the first line of treatment for chronic urticaria should be low sedating, second-generation antihistamines. However, recommendations for refractory urticaria varied and included leukotriene receptor antagonists or sedating antihistamines as adjunctive treatments, as well as dose escalation of second-generation antihistamines. To guarantee that treatment is founded on clinical evidence, more research into efficacious second-line treatments and uniform application of existing guidelines are required [6, 7].

Included were 51 randomized clinical trials witH14 distinct second-generation antihistamine and various dosage schedules, totaling 7502 participants. Differences in second generation antihistamine treatment comparisons were noted in terms of treatment unacceptability, tolerability, adverse events, and central nervous system side effects, according to the results of network meta-analyses [8]. The outcomes of second-generation antihistamine treatment for serious adverse events and those for anticholinergic side effects did not differ statistically significantly. The top three treatments with unfavorable safety profiles linked to CNS side effects and any adverse events were cetirizine 10 mg, mizolastine 10 mg, and emedastine 4 mg, according to the ranking of safety profiles [9].

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