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Antihistamines

investigacion seguridad cardiaca antihistaminicos

Cardiac safety of second-generation H1-antihistamines when updosed in chronic spontaneous urticaria

By Selected articles

Mauro Cataldi, Marcus Maurer, Maurizio Taglialatela, Martin K. Church2.

(2019) Clin Exp Allergy. 2019 Sep 13. doi: 10.1111/cea.13500. [Epub ahead of print]

This is a review where the mechanisms and assessment of potential cardiotoxicity of H1-antihistamines are discussed when updosed to four-times their licensed dose. Second generation H1-antihistamines are the primary treatment of chronic urticaria, however there are patients who don’t respond to licensed doses of H1-antihistamines. Current EAACI/GA2LEN/EDF/WAO guideline for urticaria suggest updosing of H1-antihistamines up to 4-fold.

Due to the off label use of this updosing, it is important to ensure its safety. An important aspect of safety is potential cardiotoxicity. This review considered in detail H1-antihistamines such as bilastine, cetirizine, levocetirizine, ebastine, fexofenadine, loratadine, desloratadine, mizolastine and rupatadine. Provided that prescribers carefully considered and ruled out potential risk factors for cardiotoxicity, such as the presence of inherited long QT syndrome, older age, cardiovascular disorders, hypokalemia and hypomagnesemia, or the use of drugs that either haver direct QT prolonging effect or inhibit H1-antihistamines metabolism, reviewers were able to conclude that at up to four-fold the standard dose, H1-antihistamines have excellent cardiac safety profiles.

This is a review where the mechanisms and assessment of potential cardiotoxicity of H1-antihistamines are discussed when updosed to four-times their licensed dose. Second generation H1-antihistamines are the primary treatment of chronic urticaria, however there are patients who don’t respond to licensed doses of H1-antihistamines. Current EAACI/GA2LEN/EDF/WAO guideline for urticaria suggest updosing of H1-antihistamines up to 4-fold.

Due to the off label use of this updosing, it is important to ensure its safety. An important aspect of safety is potential cardiotoxicity. This review considered in detail H1-antihistamines such as bilastine, cetirizine, levocetirizine, ebastine, fexofenadine, loratadine, desloratadine, mizolastine and rupatadine. Provided that prescribers carefully considered and ruled out potential risk factors for cardiotoxicity, such as the presence of inherited long QT syndrome, older age, cardiovascular disorders, hypokalemia and hypomagnesemia, or the use of drugs that either haver direct QT prolonging effect or inhibit H1-antihistamines metabolism, reviewers were able to conclude that at up to four-fold the standard dose, H1-antihistamines have excellent cardiac safety profiles.

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Antihistamínicos H1

Antihistamines for Allergic Rhinitis Treatment from the Viewpoint of Nonsedative Properties.

By Articles about Bilastine
Kawauchi H, Yanai K, Wang DY, Itahashi K, Okubo K.

Antihistamines targeting the histamine H₁ receptor play an important role in improving and maintaining the quality of life of patients with allergic rhinitis. For more effective and safer use of second-generation drugs, which are recommended by various guidelines, a classification based on their detailed characteristics is necessary. Antihistamines for first-line therapy should not have central depressant/sedative activities.
Among the non-sedating group, fexofenadine and bilastine are classified into “non-brain-penetrating antihistamines”.
This review summarizes that the non-brain-penetrating antihistamines should be chosen for the first-line therapy of mild allergic rhinitis.

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The long duration of action of the second generation antihistamine bilastine coincides with its long residence time at the histamine H1 receptor

By Articles about Bilastine
Bosma R, van den Bor J, Vischer HF, Labeaga L, Leurs R

Bilastine shows a long drug-target residence time at the H1 receptor (73 ± 5 min) and this results in a prolonged H1 receptor antagonism in vitro (Ca2+ mobilization in Fluo-4 loaded HeLa cells), following a washout of unbound antagonist. Hence, the long residence time of bilastine can explain the observed long duration of drug action in vivo.

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F1 simulador

Bilastine safety in drivers who need antihistamines: new evidence from high-speed simulator driving test on allergic patients

By Articles about Bilastine
Demonte A, Guanti MB, Liberati S, Biffi A, Fernando F, Fainello M, Pepe P

This study is the first done in patients with allergic rhinitis and/or chronic urticaria using a F1-high speed simulator-driving test evaluating subjects’ performance under bilastine treatment.

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Estudio de bilastina en pacientes japoneses

One-year safety and efficacy study of bilastine treatment in Japanese patients with chronic spontaneous urticaria or pruritus associated with skin diseases

By Articles about Bilastine
Yagami A, Furue M, Togawa M, Saito A, Hide M.

A number of second-generation non-sedating antihistamines are used in clinical practices over the world. However, long-term safety and efficacy have not been proved high level evidence based medicine. 
In conclusion, long-term treatment with bilastine 20 mg once daily for 52 weeks is safe and well tolerated in Japanese patients with hronic spontaneous urticaria (CSU) or pruritus associated with skin diseases. Bilastine improved disease symptoms of both conditions early in treatment, and the efficacy was maintained throughout the treatment.

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