Histamine Modulators

  • Michael Yarborough
  • Judy G. Johnson


Histamine modulators, more commonly referred to as antihistamines, have been commonly used in the USA for over half a century. Many of the dangerous side effects of these medications have been minimized due to the development of more advanced formulations with the removal of the more dangerous medications from the US market by the FDA. Knowledge of the potential side effect profiles of the antihistamines is necessary for any provider who is either prescribing or administering these medications. Those negative side effect profiles include the effects on the cardiac system and the central nervous system. In addition, providers must know the effects that occur with the extremes of age and during pregnancy. Potential metabolic effects are also important aspects that must be considered when dealing with antihistamines. Remarkably, only one of the antihistamines has been assigned a boxed warning by the FDA.


Grapefruit Juice Histamine Receptor Inverse Agonist Allergic Symptom Dangerous Side Effect 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Supplementary material


  1. 1.
    Criado PR, Criado RFJ, Maruta CW, et al. Histamine, histamine receptors and antihistamines: new concepts. Braz Annals Dermatol. 2010;85(2):195–210.CrossRefGoogle Scholar
  2. 2.
    Jutel M, Blaser K, Akdis CA. Histamine in chronic allergic responses. J Invest Allergy Clin Immunol. 2005;15:1–8.Google Scholar
  3. 3.
    Leurs R, Church MK, Taglialatela M. H1-antihistamines: inverse agonism, anti-inflammatory actions and cardiac effects. Clin Exp Allergy. 2002;32:489–98.PubMedCrossRefGoogle Scholar
  4. 4.
    Monroe E, Daly A, Shalhoub R M.D. Appraisal of the validity of histamine-induced wheal and flare is used to predict the clinical efficacy of antihistamines. J Allergy Clin Immunol. 1997;99(2):S789–806.CrossRefGoogle Scholar
  5. 5.
    Nicolas JM. The metabolic profile of second-generation antihistamines. Allergy. 2000;55 Suppl 60:46–52.PubMedCrossRefGoogle Scholar
  6. 6.
    Lin S. Antihistamines. In: Sinatra R, Jahr J, Watkins-Pitchford J, editors. The essence of analgesia and analgesics. New York: Cambridge University Press; 2011. p. 391–6.Google Scholar
  7. 7.
    Davila I, Sastre J, Bartra J, del Cuvillo A, Jauregui I, Montoro J, et al. Effect of H1 antihistamines upon the cardiovascular system. J Investig Allergol Clin Immunol. 2006;16 Suppl 1:13–23.PubMedGoogle Scholar
  8. 8.
    Rumore MM, Schlichting DA. Analgesic effects of antihistaminics. Life Sci. 1985;36(5):403–16.PubMedCrossRefGoogle Scholar
  9. 9.
    Kornhuber J, Parson CG, Hartnamm S, et al. Orphenadrine is an uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist: binding and patch clamp studies. J Neural Transm Gen Sect. 1995;102(3):237–46.PubMedCrossRefGoogle Scholar
  10. 10.
    Boustani M, Hall KS, Lane KA, et al. The association between cognition and histamine-2 receptor antagonists in African Americans. J Am Geriatr Soc. 2007;55(8):1248–53.PubMedCentralPubMedCrossRefGoogle Scholar
  11. 11.
    Powell RJ, Du Toit GI, Siddique N, Leech SC, Dixon TA, Clark AT, British Society for Allergy and Clinical Immunology (BSACI), et al. BSACI guidelines for the management of chronic urticaria and angio-oedema. Clin Exp Allergy. 2007;37:631–50.PubMedCrossRefGoogle Scholar
  12. 12.
    Gill SK, O’Brien L, Koren G. The safety of histamine 2 (H2) blockers in pregnancy: a meta-analysis. Dig Dis Sci. 2009;54:1835–8.PubMedCrossRefGoogle Scholar
  13. 13.
    Humphries TJ, Merritt GJ. Review article: drug interactions with agents used to treat acid-related diseases. Aliment Pharmacol Ther. 1999;13 Suppl 3:18–26.PubMedCrossRefGoogle Scholar
  14. 14.
    Kirch W, Hoensch H, Janisch HD. Interactions and non-interactions with ranitidine. Clin Pharmacokinet. 1984;9(6):493–510.PubMedCrossRefGoogle Scholar
  15. 15.
    U.S. Food and Drug Administration[Internet]. Postmarket drug safety information for patients and providers. Information for healthcare professionals – intravenous promethazine and severe tissue injury, including gangrene. (updated 09/16/2009). Available from

Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  • Michael Yarborough
    • 1
  • Judy G. Johnson
    • 2
  1. 1.Department of AnesthesiologyTulane Medical CenterNew OrleansUSA
  2. 2.Department of AnesthesiologyLouisiana State UniversityNew OrleansUSA

Personalised recommendations