Cetirizine: Antiallergic therapy beyond traditional H1 antihistamines

Sheffer, Albert L.; Samuels, Lawrence L.

doi:10.1016/s0091-6749(05)80251-9

Cited by 26 publications

(8 citation statements)

References 15 publications

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“…The potential for second‐generation H 1 ‐antihistamines to penetrate across blood‐brain barrier and cause anticholinergic effects is lower but not clinically irrelevant (e.g. cetirizine) …”

Section: Discussionmentioning

confidence: 92%

The use of medications with anticholinergic properties and risk factors for their use in hospitalised elderly patients

Wawruch

Macugova

Kostkova

et al. 2011

Pharmacoepidemiology and Drug

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Section: Discussionmentioning

confidence: 92%

The use of medications with anticholinergic properties and risk factors for their use in hospitalised elderly patients

Wawruch

Macugova

Kostkova

et al. 2011

Pharmacoepidemiology and Drug

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“…A number of studies demonstrate that new antihistamines reduce clinical symptoms of allergic diseases. Several studies support the view that new antihistamines have anti‐inflammatory effects in vivo [5–15]. For instance, new antihistamines such as cetirizine and azelastine attenuate eosinophil recruitment into the site of allergic inflammation [8, 14], and intracellular adhesion molecule‐1 (ICAM‐1) expression on epithelial cells from the site of allergic inflammation [11, 12, 14].…”

mentioning

confidence: 99%

Anti‐inflammatory actions of new antihistamines

Hayashi

Hashimoto

1999

Clin Experimental Allergy

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“…Cetirizine, the carboxylated metabolite of hydroxyzine, is a sgAH of the piperazine family with very low sedating and anticholinergic activities. 29 Cetirizine has a chiral centre and, therefore, exists in two enantiomeric forms, R-and L-cetirizine, of which only L-cetirizine (levocetirizine) is active on H 1 receptors. Levocetirizine has a similar tolerability and a higher potency than the parent racemic form, cetirizine.…”

Section: Cetirizine and Levocetirizinementioning

confidence: 99%

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

Cataldi

Maurer

Taglialatela

et al. 2019

Clin Experimental Allergy

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The symptoms of chronic urticaria, be it chronic spontaneous urticaria (CSU) or chronic inducible urticaria (CindU), are mediated primarily by the actions of histamine on H1 receptors located on endothelial cells (the weal) and on sensory nerves (neurogenic flare and pruritus). Thus, second‐generation H1 antihistamines (sgAHs) are the primary treatment of these conditions. However, many patients are poorly responsive to licensed doses of antihistamines. In these patients, the current EAACI/GA2LEN/EDF/WAO guideline for urticaria suggests updosing of sgAHs up to fourfold. However, such updosing is off‐label and the responsibility resides with the prescribing physician. Therefore, the safety of the drug when used above its licensed dose is of paramount importance. An important aspect of safety is potential cardiotoxicity. This problem was initially identified some 20 years ago with cardiotoxic deaths occurring with astemizole and terfenadine, two early sgAHs. In this review, we discuss the mechanisms and assessments of potential cardiotoxicity of H1 antihistamines when updosed to four times their licensed dose. In particular, we have focused on the potential of H1 antihistamines to block hERG (human Ether‐a‐go‐go‐Related Gene) voltage‐gated K+ channels, also known as Kv11.1 channels according to the IUPHAR classification. Blockade of these channels causes QT prolongation leading to torsade de pointes that may possibly degenerate into ventricular fibrillation and sudden death. We considered in detail bilastine, cetirizine, levocetirizine, ebastine, fexofenadine, loratadine, desloratadine, mizolastine and rupatadine and concluded that all these drugs have an excellent safety profile with no evidence of cardiotoxicity even when updosed up to four times their standard licensed dose, provided that the prescribers carefully consider and rule 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 have direct QT prolonging effects or inhibit sgAH metabolism.

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Cetirizine: Antiallergic therapy beyond traditional H1 antihistamines

Cited by 26 publications

References 15 publications

The use of medications with anticholinergic properties and risk factors for their use in hospitalised elderly patients

The use of medications with anticholinergic properties and risk factors for their use in hospitalised elderly patients

Anti‐inflammatory actions of new antihistamines

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

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Cetirizine: Antiallergic therapy beyond traditional H1 antihistamines

Cited by 26 publications

References 15 publications

The use of medications with anticholinergic properties and risk factors for their use in hospitalised elderly patients

The use of medications with anticholinergic properties and risk factors for their use in hospitalised elderly patients

Anti‐inflammatory actions of new antihistamines

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

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Product

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