Skip to main content
SpringerLink
Log in

Dermatological Indications of Antihistamines

  • Protocol
  • First Online:
Histamine Receptors as Drug Targets

Part of the book series: Methods in Pharmacology and Toxicology ((MIPT))

  • 797 Accesses

Abstract

Antihistamines are drugs that exert their biological effects inhibiting the action of histamine by occupying its receptors. They are divided into four subclasses depending on their tendency to bond with H1, H2, H3, or H4 histamine receptors. H1 antihistamines are the most commonly used in dermatology for the treatment of urticaria and other pruritic dermatoses.

This is a preview of subscription content, log in via an institution to check access.

Access this chapter

Log in via an institution
Protocol
USD 49.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 89.00
Price excludes VAT (USA)
  • Available as EPUB and PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 119.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info
Hardcover Book
USD 169.99
Price excludes VAT (USA)
  • Durable hardcover edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

References

  1. Panula P, Chazot PL, Cowart M et al (2015) Histamine receptors. Pharmacol Rev 67:601–655

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  2. Smuda C, Bryce PJ (2011) New developments in the use of histamine and histamine receptors. Curr Allergy Asthma Rep 11:94–100

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  3. Ohsawa Y, Hirasawa N (2014) The role of histamine H1 and H4 receptors in atopic dermatitis: from basic research to clinical study. Allergol Int 63:533–542

    Article  CAS  PubMed  Google Scholar 

  4. Thurmond RL, Gelfand EW, Dunford PJ (2008) The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov 7:41–53

    Article  CAS  PubMed  Google Scholar 

  5. Hu WW, Chen Z (2012) Role of histamine and its receptors in cerebral ischemia. ACS Chem Nerosci 3:238–247

    Article  Google Scholar 

  6. Kopic S, Geibel JP (2013) Gastric acid, calcium absorption, and their impact on bone health. Physiol Rev 93:189–268

    Article  CAS  PubMed  Google Scholar 

  7. Ellenbroek BA (2013) Histamine H3 receptors, the complex interaction with dopamine and its implications for addiction. Br J Pharmacol 170:46–57

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  8. Hofstra CL, Desai PJ, Thurmond RL et al (2003) Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells. J Pharmacol Exp Ther 305:1212–1221

    Article  CAS  PubMed  Google Scholar 

  9. Nijmeijer S, de Graaf C, Leurs R et al (2012) Molecular pharmacology of histamine H4 receptors. Front Biosci (Landmark Ed) 17:2089–2106

    Article  Google Scholar 

  10. Gschwandtner M, Rossbach K, Dijkstra D et al (2010) Murine and human Langerhans cells express a functional histamine H4 receptor: modulation of cell migration and function. Allergy 65:840–849

    Article  CAS  PubMed  Google Scholar 

  11. Dib K, Perecko T, Jenei V et al (2014) The histamine H4 receptor is a potent inhibitor of adhesion-dependent degranulation in human neutrophils. J Leukoc Biol 96:411–418

    Article  PubMed  Google Scholar 

  12. Ling P, Ngo K, Nguyen S et al (2004) Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol 142:161–171

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  13. Dunford PJ, O’Donnell N, Riley JP et al (2006) The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells. J Immunol 176:7062–7070

    Article  CAS  PubMed  Google Scholar 

  14. Greaves MW (2005) Antihistamines in dermatology. Skin Pharmacol Physiol 18:220–229

    Article  CAS  PubMed  Google Scholar 

  15. Del Cuvillo A, Sastre J, Montoro J et al (2007) Use of antihistamines in pediatrics. J Investig Allergol Clin Immunol 17(S2):28–40

    CAS  PubMed  Google Scholar 

  16. Simons FE, Simons KJ (2008) H1 antihistamines: current status and future directions. World Allergy Organ J 1:145–155

    Article  PubMed  PubMed Central  Google Scholar 

  17. Richelson E (1979) Tricyclic antidepressants and histamine H1 receptors. Mayo Clin Proc 54:669–674

    CAS  PubMed  Google Scholar 

  18. Singh H, Becker PM (2007) Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs 16:1295–1305

    Article  CAS  PubMed  Google Scholar 

  19. Egan CA, Rallis TM (1997) Treatment of chronic urticaria with ketotifen. Arch Dermatol 133:147–149

    Article  CAS  PubMed  Google Scholar 

  20. Sokol KC, Amar NK, Starkey J et al (2013) Ketotifen in the management of chronic urticaria: resurrection of an old drug. Ann Allergy Asthma Immunol 111:433–436

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  21. Paquette D, Rothe MJ (2000) Unapproved dermatologic indications for H2 receptor antagonists, cromolyn sodium, and ketotifen. Clin Dermatol 18:103–111

    Article  CAS  PubMed  Google Scholar 

  22. Finn DF, Walsh JJ (2013) Twenty-first century mast cell stabilizers. Br J Pharmacol 170:23–37

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  23. Theoharides TC, Valent P, Akin C (2015) Mast cells, mastocytosis, and related disorders. N Engl J Med 373:163–172

    Article  CAS  PubMed  Google Scholar 

  24. Zuberbier T, Aberer W, Asero R et al (2014) The EAACI/GA(2) LEN/EDF/WAO Guideline for the definition, classification, diagnosis, and management of urticaria: the 2013 revision and update. Allergy 69:868–887

    Article  CAS  PubMed  Google Scholar 

  25. Schoepke N, Doumoulakis G, Maurer M (2013) Diagnosis of urticaria. Indian J Dermatol 58:211–218

    Article  PubMed  PubMed Central  Google Scholar 

  26. Sachdeva S, Gupta V, Amin SS et al (2011) Chronic urticaria. Indian J Dermatol 56:622–628

    Article  PubMed  PubMed Central  Google Scholar 

  27. Bernstein JA, Lang DM, Khan DA et al (2014) The diagnosis and management of acute and chronic urticaria: 2014 update. J Allergy Clin Immunol 133:1270–1277

    Article  PubMed  Google Scholar 

  28. Sharma M, Bennett C, Cohen SN et al (2014) H1-antihistamines for chronic spontaneous urticaria. Cochrane Database Syst Rev 11:CD006137

    Google Scholar 

  29. Fedorowicz Z, van Zuuren EJ, Hu N (2012) Histamine H2-receptor antagonists for urticaria. Cochrane Database Syst Rev 3:CD008596

    Google Scholar 

  30. Lee JH, Son SW, Cho SH (2016) A comprehensive review of the treatment of atopic eczema. Allergy Asthma Immunol Res 8:181–190

    Article  PubMed  Google Scholar 

  31. Bannister MJ, Freeman S (2000) Adult-onset atopic dermatitis. Australas J Dermatol 41:225–228

    Article  CAS  PubMed  Google Scholar 

  32. Kanwar AJ, Narang T (2013) Adult onset atopic dermatitis: under-recognized or under-reported? Indian Dermatol Online J 4:167–171

    Article  PubMed  PubMed Central  Google Scholar 

  33. Novak N, Leung DY (2011) Advances in atopic dermatitis. Curr Opin Immunol 23:778–783

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  34. De Benedetto A, Yoshida T, Fridy S et al (2015) Histamine and skin barrier: are histamine antagonists useful for the prevention or treatment of atopic dermatitis? J Clin Med 4:741–755

    Article  PubMed  PubMed Central  Google Scholar 

  35. Nicolaidou E, Katsambas AD (2003) Antihistamines and steroids in pediatric dermatology. Clin Dermatol 21:321–324

    Article  PubMed  Google Scholar 

  36. Savall BM, Chavez F, Tays K et al (2014) Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H4 receptor antagonists. J Med Chem 57:2429–2439

    Article  CAS  PubMed  Google Scholar 

  37. Kollmeier A, Francke K, Chen B et al (2014) The histamine H4 receptor antagonist, JNJ 39758979, is effective in reducing histamine-induced pruritus in a randomized clinical study in healthy subjects. J Pharmacol Exp Ther 350:181–187

    Article  PubMed  Google Scholar 

  38. Ohsawa Y, Hirasawa N (2012) The antagonism of histamine H1 and H4 receptors ameliorates chronic allergic dermatitis via anti-pruritic and anti-inflammatory effects in NC/Nga mice. Allergy 67:1014–1022

    Article  CAS  PubMed  Google Scholar 

  39. O’Donoghue M, Tharp MD (2005) Antihistamines and their role as antipruritics. Dermatol Ther 18:333–340

    Article  PubMed  Google Scholar 

  40. Goutos I, Dziewulski P, Richardson PM (2009) Pruritus in burns: review article. J Burn Care Res 30:221–228

    Article  PubMed  Google Scholar 

  41. Juckett G (2013) Arthropod bites. Am Fam Physician 88:841–847

    PubMed  Google Scholar 

  42. Smith KJ, Skelton HG, Yeager J et al (1997) Pruritus in HIV-1 disease: therapy with drugs which may modulate the pattern of immune dysregulation. Dermatology 195:353–358

    Article  CAS  PubMed  Google Scholar 

  43. Pour-Reza-Gholi F, Nasrollahi A, Firouzan A et al (2007) Low-dose doxepin for treatment of pruritus in patients on hemodialysis. Iran J Kidney Dis 1:34–37

    PubMed  Google Scholar 

  44. Englisch W, Bauer CP (1997) Dimethindene maleate in the treatment of pruritus caused by varicella zoster virus infection in children. Arzneimittelforschung 47:1233–1235

    CAS  PubMed  Google Scholar 

  45. Mamdani FS (1994) Pharmacologic management of herpes zoster and postherpetic neuralgia. Can Fam Physician 40:321–326

    CAS  PubMed  PubMed Central  Google Scholar 

  46. Verma P, Singal A, Sharma S (2012) Idiopathic bullous eosinophilic cellulitis (Wells syndrome) responsive to topical tacrolimus and antihistamine combination. Indian J Dermatol Venereol Leprol 78:378–380

    Article  PubMed  Google Scholar 

  47. Sinno H, Lacroix JP, Lee J et al (2012) Diagnosis and management of eosinophilic cellulitis (Wells’ syndrome): a case series and literature review. Can J Plast Surg 20:91–97

    Article  PubMed  PubMed Central  Google Scholar 

  48. Tripathi T, Shahid M, Khan HM et al (2010) Modulation of in vivo immunoglobulin production by endogenous histamine and H1R and H2R agonists and antagonists. Pharmacol Rep 62:917–925

    Article  CAS  PubMed  Google Scholar 

  49. Sinha S, Relhan V, Garg VK (2015) Immunomodulators in warts: unexplored or ineffective? Indian J Dermatol 60:118–129

    Article  PubMed  PubMed Central  Google Scholar 

  50. Bauman C, Francis JS, Vanderhooft S et al (1996) Cimetidine therapy for multiple viral warts in children. J Am Acad Dermatol 35:271–272

    Article  CAS  PubMed  Google Scholar 

  51. Micali G, Nasca MR, Dall’Oglio F et al (2003) Cimetidine therapy for epidermodysplasia verruciformis. J Am Acad Dermatol 48:S9–10

    Article  PubMed  Google Scholar 

  52. Stashower ME, Yeager JK, Smith KJ et al (1993) Cimetidine as therapy for treatment-resistant psoriasis in a patient with acquired immunodeficiency syndrome. Arch Dermatol 129:848–850

    Article  CAS  PubMed  Google Scholar 

  53. Staevska M, Gugutkova M, Lazarova C et al (2014) Night-time sedating H1-antihistamine increases daytime somnolence but not treatment efficacy in chronic spontaneous urticaria: a randomized controlled trial. Br J Dermatol 171:148–154

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  54. Murota H, Kitaba S, Tani M et al (2010) Impact of sedative and non-sedative antihistamines on the impaired productivity and quality of life in patients with pruritic skin diseases. Allergol Int 59:345–354

    Article  PubMed  Google Scholar 

  55. Nicholson AN (1983) Antihistamines and sedation. Lancet 322:211–212

    Article  Google Scholar 

  56. Chishty M, Reichel A, Siva J et al (2001) Affinity for the P-glycoprotein efflux pump at the blood-brain barrier may explain the lack of CNS side-effects of modern antihistamines. J Drug Target 9:223–228

    Article  CAS  PubMed  Google Scholar 

  57. Hu Y, Sieck DE, Hsu WH (2015) Why are second-generation H1-antihistamines minimally sedating? Eur J Pharmacol 765:100–106

    Article  CAS  PubMed  Google Scholar 

  58. Naicker P, Anoopkumar-Dukie S, Grant GD et al (2013) The effects of antihistamines with varying anticholinergic properties on voluntary and involuntary movement. Clin Neurophysiol 124:1840–1845

    Article  PubMed  Google Scholar 

  59. He M, Deng C, Huang XF (2013) The role of hypothalamic H1 receptor antagonism in antipsychotic-induced weight gain. CNS Drugs 27:423–434

    Article  CAS  PubMed  Google Scholar 

  60. Woosley RL (1996) Cardiac actions of antihistamines. Annu Rev Pharmacol Toxicol 36:233–252

    Article  CAS  PubMed  Google Scholar 

  61. Rico S, Antonijoan R, Barbanoj M (2009) Ebastine in the light of CONGA recommendations for the development of third-generation antihistamines. J Asthma Allergy 2:73–92

    CAS  PubMed  PubMed Central  Google Scholar 

  62. Deepinder F, Braunstein GD (2012) Drug-induced gynecomastia: an evidence-based review. Expert Opin Drug Saf 11:779–795

    Article  CAS  PubMed  Google Scholar 

  63. Van Thiel DH, Gavaler JS, Smith WI Jr et al (1979) Hypothalamic-pituitary-gonadal dysfunction in men using cimetidine. N Engl J Med 300:1012–1015

    Article  CAS  PubMed  Google Scholar 

  64. Schmidt JB (1998) Other antiandrogens. Dermatology 196:153–157

    Article  CAS  PubMed  Google Scholar 

  65. Hafeez ZH (1996) Antihistamines and their role in dermatology. J Pak Med Assoc 46:264–267

    CAS  PubMed  Google Scholar 

  66. Clegg A, Young JB (2011) Which medications to avoid in people at risk of delirium: a systematic review. Age Ageing 40:23–29

    Article  PubMed  Google Scholar 

  67. Tawadrous D, Dixon S, Shariff SZ et al (2014) Altered mental status in older adults with histamine2-receptor antagonists: a population-based study. Eur J Intern Med 25:701–709

    Article  CAS  PubMed  Google Scholar 

  68. Elder JB, Ganguli PC, Gillespie IE (1979) Cimetidine and gastric cancer. Lancet 313:1005–1006

    Article  Google Scholar 

  69. Langman MJ, Dunn JA, Whiting JL et al (1999) Prospective, double-blind, placebo-controlled randomized trial of cimetidine in gastric cancer. British Stomach Cancer Group. Br J Cancer 81:1356–1362

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  70. Jiang CG, Liu FR, Yu M et al (2010) Cimetidine induces apoptosis in gastric cancer cells in vitro and inhibits tumor growth in vivo. Oncol Rep 23:693–700

    Article  CAS  PubMed  Google Scholar 

  71. Tønnesen H, Knigge U, Bülow S et al (1988) Effect of cimetidine on survival after gastric cancer. Lancet 332:990–992

    Article  Google Scholar 

  72. Pompili M, Basso M, Grieco A et al (2004) Recurrent acute hepatitis associated with use of cetirizine. Ann Pharmacother 38:1844–1847

    Article  PubMed  Google Scholar 

  73. Ekiz F, Yüksel I, Ekiz O et al (2011) Levocetirizine induced hepatotoxicity in a patient with chronic urticaria. Ann Hepatol 10:237–238

    PubMed  Google Scholar 

  74. Paton DM, Webster DR (1985) Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet 10:477–497

    Article  CAS  PubMed  Google Scholar 

  75. Zazgornik J, Huang ML, Van Peer A et al (1993) Pharmacokinetics of orally administered levocabastine in patients with renal insufficiency. J Clin Pharmacol 33:1214–1218

    Article  CAS  PubMed  Google Scholar 

  76. Gilboa SM, Strickland MJ, Olshan AF et al (2009) National Birth Defects Prevention Study. Use of antihistamine medications during early pregnancy and isolated major malformations. Birth Defects Res A Clin Mol Teratol 85:137–150

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  77. Gilboa SM, Ailes EC, Rai RP et al (2014) Antihistamines and birth defects: a systematic review of the literature. Expert Opin Drug Saf 13:1667–1698

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  78. FDA Pregnancy Categories. http://www.drugs.com/pregnancy-categories.html. Accessed 26 Apr 2016

  79. Poza J, Caminal P, Vallverdú M et al (2007) Study of the EEG changes during the combined ingestion of alcohol and H1-antihistamines by using the wavelet transform. Conf Proc IEEE Eng Med Biol Soc 2007:23–26

    PubMed  Google Scholar 

  80. Scaglione F (2012) Safety profile of bilastine: 2nd generation H1-antihistamines. Eur Rev Med Pharmacol Sci 16:1999–2005

    CAS  PubMed  Google Scholar 

  81. Montoro J, Bartra J, Sastre J et al (2013) H1 antihistamines and benzodiazepines. Pharmacological interactions and their impact on cerebral function. J Investig Allergol Clin Immunol 23(S1):17–26

    CAS  PubMed  Google Scholar 

  82. Bartra J, Valero AL, del Cuvillo A et al (2006) Interactions of the H1 antihistamines. J Investig Allergol Clin Immunol 16(1):29–36

    PubMed  Google Scholar 

  83. Stahl SM, Felker A (2008) Monoamine oxidase inhibitors: a modern guide to an unrequited class of antidepressants. CNS Spectr 13:855–870

    Article  PubMed  Google Scholar 

  84. Zhou S, Yung Chan S, Cher Goh B et al (2005) Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs. Clin Pharmacokinet 44:279–304

    Article  CAS  PubMed  Google Scholar 

  85. Katz HI (1999) Drug interactions of the newer oral antifungal agents. Br J Dermatol 141(S56):26–32

    Article  PubMed  Google Scholar 

  86. Fourneau E, Bovet D (1933) Recherches sur l’ action sympathicolytique d' un nouveau dérivé du dioxane. Arch Int Pharmacodyn Ther 46:178–191

    CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Dermatology, 401 General Military Hospital of Athens, Athens, Greece

    Chrysovalantis Korfitis

  2. Department of Dermatology, Veterans Administration Hospital of Athens, 10-12 Monis Petraki Street, 11521, Athens, Greece

    Efstathios Rallis

  3. 2nd Department of Dermatology and Venereology, Medical School, National and Kapodistrian University of Athens, University Hospital ‘Attikon’, Athens, Greece

    Dimitrios Rigopoulos

Authors
  1. Chrysovalantis Korfitis
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Efstathios Rallis
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Dimitrios Rigopoulos
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Efstathios Rallis .

Editor information

Editors and Affiliations

  1. Department of Pharmacology Medical School, National and Kapodistrian University of Athens, Athens, Greece

    Ekaterini Tiligada

  2. Centre for Experimental Medicine, School of Medicine, Dentistry and Biomedical Sciences, Queen’s University Belfast, Belfast, Northern Ireland, United Kingdom

    Madeleine Ennis

Rights and permissions

Reprints and permissions

Copyright information

© 2017 Springer Science+Business Media LLC

About this protocol

Cite this protocol

Korfitis, C., Rallis, E., Rigopoulos, D. (2017). Dermatological Indications of Antihistamines. In: Tiligada, E., Ennis, M. (eds) Histamine Receptors as Drug Targets. Methods in Pharmacology and Toxicology. Humana Press, New York, NY. https://doi.org/10.1007/978-1-4939-6843-5_16

Download citation

  • DOI: https://doi.org/10.1007/978-1-4939-6843-5_16

  • Published:

  • Publisher Name: Humana Press, New York, NY

  • Print ISBN: 978-1-4939-6841-1

  • Online ISBN: 978-1-4939-6843-5

  • eBook Packages: Springer Protocols

Publish with us

Policies and ethics

Search

Navigation