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Antihistamines Modulate Functional Activity of Macrophages.

N G Plekhova1, E V Eliseeva2, I N Dubnyak2

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Second-generation antihistamines, like loratadine, induce macrophage apoptosis at lower doses. These drugs also modulate cytokine production, indicating potential immunomodulatory effects in cellular models.

Keywords:
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Area of Science:

  • Immunology
  • Pharmacology
  • Cell Biology

Background:

  • Antihistamines are widely used for allergic conditions.
  • Understanding their cellular effects beyond histamine receptor antagonism is crucial.
  • Macrophage function is central to immune responses.

Purpose of the Study:

  • To compare the in vitro effects of first-, second-, and third-generation antihistamines on macrophage viability, enzyme activity, and cytokine production.
  • To investigate dose-dependent effects of these antihistamines.

Main Methods:

  • In vitro model using macrophages.
  • Assessment of cell viability and apoptosis.
  • Measurement of ATPase and 5'-AMP activity.
  • Quantification of cytokine production (IL-1β, TNFα, IL-10).

Main Results:

  • Decreasing antihistamine dose increased macrophage viability.
  • Second-generation antihistamines (loratadine, desloratadine) predominantly induced macrophage apoptosis.
  • A dose-dependent increase in ATPase and 5'-AMP activity was observed, with less impact from second-generation drugs.
  • Macrophages produced TNFα and IL-10 but not IL-1β under drug influence.

Conclusions:

  • Antihistamines exhibit dose-dependent effects on macrophage viability and apoptosis.
  • Second-generation antihistamines show a distinct profile, inducing apoptosis and modulating cytokine release.
  • These findings suggest immunomodulatory properties of antihistamines, impacting macrophage function beyond histamine blockade.