Changbo Qu, Gwenny M. Fuhler, Yihang Pan

Int J Mol Sci . 2021 May 26;22(11):5672. doi: 10.3390/ijms22115672.

The pandemic of COVID-19, caused by SARS-CoV-2, has led to extensive and long-term health issues in those affected by the disease. It is essential to identify new treatments for COVID-19 infection with a better outcome too. The objective of this review is to summarize the use of H1 receptor antagonists in SARS-CoV-2 infection.

One of the common characteristics of severe COVID-19 is unbalanced lung inflammation. Reducing lung inflammation can help improve COVID-19 clinical manifestations. H1 receptor antagonists may inhibit SARS-CoV-2 either via the H1 receptor or via the ACE2 receptor. The virus spike proteins interact with both cellular heparan sulfate and ACE2 through its receptor-binding domain, and H1-antihistamines may disrupt the interaction between heparan sulfate and spike protein, inhibiting the virus entry in the cell.

New-generation H1 receptor antagonists, such as loratadine and desloratadine, may help inhibit SARS-CoV-2 infection by reducing lung inflammation induced by histamine, as well as other inflammatory activities. These antihistamines have also been shown to exert antiviral effects when blocking H1 receptors and, therefore, to affect SARS-CoV-2 replication via the mediation of metabolism and immune responses.

In conclusion, H1 receptor antagonists are relatively inexpensive drugs, ready to use and with the capacity to improve patient outcomes due to their role in reducing inflammation and antiviral effects. They may also be attractive prophylactic candidates for lowering the risk of SARS-CoV-2 infection in the general population.

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