Skip to main content

H1- and H2-Receptor Antagonists

  • Chapter
Pharmacology of the Skin II

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 87 / 2))

Abstract

Histamine is a naturally occurring substance found in most, if not all, tissues of the body. Histamine in tissues is stored predominantly in mast cells which are present in particularly large numbers in skin (Kaliner 1979), where they are most evident around small blood vessels and nerves (Cowen et al. 1979; Eady et al. 1979).

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

Access this chapter

Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 129.00
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 169.99
Price excludes VAT (USA)
  • Compact, lightweight 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

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Ahn HS, Barnett A (1986) Selective displacement of [3H]-mepyramine from peripheral vs. central nervous system receptors by loratadine, a non-sedating antihistamine. Eur J Pharmacol 127:153–155

    Article  PubMed  CAS  Google Scholar 

  • Aoyagi T, Adachi K, Halprin KM, Levine V, Woodyard CW (1981) The effect of histamine on epidermal outgrowth: its possible dual role as an inhibitor and stimulator. J Invest Dermatol 76:24–27

    Article  PubMed  CAS  Google Scholar 

  • Arnold AJ, Simpson JG, Jones HE, Ahmed AR (1979) Suppression of histamine-induced pruritis by hydroxyzine and various neuroleptics. Am Acad Dermatol 1:509–512

    Article  CAS  Google Scholar 

  • Bain WA, Hellier FF, Warin RP (1948) Some aspects of the action of histamine antagonists. Lancet 2:964–969

    Article  PubMed  CAS  Google Scholar 

  • Bleehen SS, Thomas SE, Greaves MW, Newton J, Kennedy CTC, Hindley F, Marks R et al. (1987) Cimetidine and chlorpheniramine in the treatment of chronic idiopathic urticaria: a multi-centre randomized double-blind study. Br J Dermatol 117:81–88

    Article  PubMed  CAS  Google Scholar 

  • Boss M, Burton JL (1981) Lack of effect of the antihistamine drug clemastine on the potentiation of itch by prostaglandin E1. Arch Dermatol 117:208–209

    Article  PubMed  CAS  Google Scholar 

  • Boyce MJ, Wareham K (1980) Histamine H1 and H2-receptors in the cardiovascular system of man. In: Torsoli A, Lucchelli PE, Brimblecome RW (eds) H2-antagonists. Ex-cerpta Medica, Amsterdam

    Google Scholar 

  • Boyce MJ, Balasubramanian V, Wareham K (1980) Cardiovascular effects in man of im-promidine, a novel and specific histamine H2-receptor agonist. Br J Pharmacol 70:157P–158P

    CAS  Google Scholar 

  • Brittain RT, Daly MJ (1981) A review of the animal pharmacology of ranitidine — a new, selective histamine H2-antagonist. Glaxo Symposium, London

    Google Scholar 

  • Brown AE, Griffiths R, Harvey CA, Owen DAA (1986) Pharmacological studies with SK&F 93944 (temelastine), a novel histamine H1 -receptor antagonist with negligible ability to penetrate the central nervous system. Br J Pharmacol 87:569–578

    PubMed  CAS  Google Scholar 

  • Bunce KT, Owen DAA, Smith IR, Vickers MR (1979) Histamine. Int Rev Biochem 26:207–256

    CAS  Google Scholar 

  • Carrier EB (1922) Studies on the physiology of capillaries. V. The reaction of the human capillaries to drugs and other stimuli. Am J Physiol 61:528–547

    CAS  Google Scholar 

  • Cerio R, Lessof MH (1984) Treatment of chronic idiopathic urticaria with terfenadine. Clin Allergy 14:139–141

    Article  PubMed  CAS  Google Scholar 

  • Cheng HC, Woodward JK (1982) Antihistaminic effect of terfenadine: a new piperidine-type antihistamine. Drug Dev Res 2:181–196

    Article  CAS  Google Scholar 

  • Cheng HC, Raevis OK, Munro NL, Woodward JK (1979) Cutaneous vascular histamine H1-receptors in the guinea pig: the histamine skin wheal as a cutaneous vascular model. Arch Int Pharmacodyn Ther 249:241

    Google Scholar 

  • Cook LJ, Shuster S (1979) Lack of effect of H2 blockade in chronic urticaria. Br J Dermatol [Suppl 17]101:20–21

    Google Scholar 

  • Cook LJ, Shuster S (1980) Histamine weal formation and absorption in man. Br J Pharmacol 69:579–585

    PubMed  CAS  Google Scholar 

  • Cook LJ, Shuster S (1983) The effect of H1 and H2 receptor antagonists on the demographic response. Acta Derm Venereol (Stockh) 63:260–262

    CAS  Google Scholar 

  • Cowen T, Trigg P, Eady RAJ (1979) Distribution of mast cells in human dermis-develop-ment of a mapping technique. Br J Dermatol 100:635–640

    Article  PubMed  CAS  Google Scholar 

  • Dale HH, Laidlaw PP (1910) The physiological action of β-imidazolyethylamine. J Physiol (Lond) 41:318–344

    CAS  Google Scholar 

  • Dale HH, Laidlaw PP (1911) Further observations on the action of β-imidazolylethyl-amine. J Physiol (Lond) 43:182–195

    CAS  Google Scholar 

  • Davies MG, Greaves MW (1980) Sensory responses of human skin to synthetic histamine analogues and histamine. Br J Clin Pharmacol 9:461–465

    PubMed  CAS  Google Scholar 

  • Davies MG, Marks R, Horton RJ, Storari FE (1979) The efficacy of histamine antagonists as antipruritics in experimentally induced pruritis. Arch Dermatol Res 266:117–120

    Article  PubMed  CAS  Google Scholar 

  • Durant GJ, Ganellin CR, Griffiths R, Harvey CA, Owen DAA, Sach GS (1984) Some newer H1-receptor histamine antagonists. In: Ganellin CR, Schwartz JC (eds) Frontiers in histamine research. Pergamon, Oxford

    Google Scholar 

  • Eady RAJ, Cowen T, Marshall TF, Plumer V, Greaves MW (1979) Mast cell population density, blood vessel density and histamine content in normal human skin. Br J Dermatol 100:623–633

    Article  PubMed  CAS  Google Scholar 

  • Eppinger H (1913) Ãœber eine eigentümliche Hautreaktion hervorgerufen durch Ergamin. Wien Klin Wochenschr 63:1414

    Google Scholar 

  • Fredriksson T, Hersle K, Hjorth N, Mobacken H, Persson T, Saldo L, Salo O et al. (1986) Terfenadine in chronic urticaria: a comparison with clemastine and placebo. Cutis 38:128–130

    PubMed  CAS  Google Scholar 

  • Flynn SB, Owen DAA (1977) The effects of histamine on skeletal muscle vasculature in cats. J Physiol (Lond) 265:795–807

    CAS  Google Scholar 

  • Haddy FJ (1960) Effect of histamine on small and large vessel pressures in dog forelimb. Am J Physiol 198:161–168

    PubMed  CAS  Google Scholar 

  • Hagermark O, Strandberg K, Bronneberg R (1979) Effects of histamine receptor antagonists on histamine-induced responses in human skin. Acta Derm Venereol (Stockh) 59:297–300

    CAS  Google Scholar 

  • Harmer IM, Harris KE (1926) Observations on the vascular reaction in man in response to histamine. Heart 13:381–394

    Google Scholar 

  • Harper RA, Flaskman BA, Chopra DP (1974) Mitotic response of normal and psoriatic keratinocytes in vitro to compounds known to effect intracellular cyclic AMP. J Invest Dermatol 62(4):384–387

    Article  PubMed  CAS  Google Scholar 

  • Harvey RP, Schocket AL (1980) The effect of H1- and H2-blockade on cutaneous histamine response in man. J Allergy Clin Immunol 65:136–139

    Article  PubMed  CAS  Google Scholar 

  • Humphreys F, Krause LB, Shuster S (1987) The effects of astemizole and indomethacin on weal and flare reactions to histamine, 48/80 and house dust mite antigen (Abstr). Br J Dermatol 116:435

    Google Scholar 

  • Hutchcroft BJ, Moore EG, Orange RP (1979) The effects of H1- and H2-receptor antagonism on the response of monkey skin to intradermal histamine, reverse-type anaphylaxis, and passive cutaneous anaphylaxis. J Allergy Clin Immunol 63:376–382

    Article  PubMed  CAS  Google Scholar 

  • Kaliner MA (1979) The mast cell — a fascinating riddle. N Engl J Med 301:498–499

    Article  PubMed  CAS  Google Scholar 

  • Kaliner MJB, Sigler R, Summers R, Shelhamer JH (1981) Effects of infused histamine: analysis of the effects of H1- and H2-receptor antagonists on cardiovascular and pulmonary responses. J Allergy Clin Immunol 68:365–371

    Article  PubMed  CAS  Google Scholar 

  • Krause LB, Shuster S (1983) Mode of action of H1 antihistamines in itch. Br J Dermatol [Suppl 24]109:27

    Article  Google Scholar 

  • Krause LB, Shuster S (1984 a) The effect of terfenadine on dermographic wealing. Br J Dermatol 110:73–79

    Article  PubMed  CAS  Google Scholar 

  • Krause LB, Shuster S (1984 b) H1-receptor-active histamine not sole cause of chronic idiopathic urticaria. Lancet 2:929–930

    Article  PubMed  CAS  Google Scholar 

  • Krause LB, Shuster S (1985 a) A comparison of astemizole and chlorpheniramine in dermographic urticaria. Br J Dermatol 11:447–453

    Article  Google Scholar 

  • Krause LB, Shuster S (1985 b) Minimal effect of complete H1 receptor blockade on urticaria pigmentosa. Acta Derm Venereol (Stockh) 65:338–340

    CAS  Google Scholar 

  • Lewis T (1927) The vessels of the human skin and their responses. Shaw, London

    Google Scholar 

  • Lewis T, Grant RT (1924) Vascular reaction of the skin to injury. Heart 71:209–235

    Google Scholar 

  • Lynn B (1977) Cutaneous hyperalgesia. Br Med Bull 33:103–108

    PubMed  CAS  Google Scholar 

  • Lyons F, Shuster S (1980) The suppression of sebaceous gland activity by H2 receptor agonists. Br J Dermatol 102:730–731

    Google Scholar 

  • Marks R, Greaves MW (1977) Vascular reactions to histamine and compound 48/80 in human skin: suppression by a histamine H2-receptor blocking agent. Br J Clin Pharmacol 4:367–369

    PubMed  CAS  Google Scholar 

  • Mellander S, Johansson B (1968) Control of resistance, exchange, and capacitance functions in the peripheral circulation. Pharmacol Rev 20:117–196

    PubMed  CAS  Google Scholar 

  • Muston H, Felix R, Shuster S (1979) Differential effect of hypnotics and anxiolytics on itch and scratch. J Invest Dermatol 72:283

    Google Scholar 

  • Nathan RA, Segall N, Schocket AL (1981) A comparison of the actions of H1- and H2-antihistamines on histamine-induced bronchoconstriction and cutaneous wheal response in asthmatic patients. J Allergy Clin Immunol 67:171–177

    Article  PubMed  CAS  Google Scholar 

  • Ostoredo M, Arhand A, Vervloet D, Razzouk H, Charpin J (1980) Effets des antihistami-niques (H1 et H2) sur différents types de tests cutanés explorant l’allergie à médiation humorale ou cellulaire. Rev Fr Allergol 20:113–117

    Article  Google Scholar 

  • Owen DAA, Poy E, Woodward DF (1980) Evaluation of the role of histamine H1- and H2-receptors in cutaneous inflammation in the guinea-pig prodcued by histamine and mast cell degranulation. Br J Pharmacol 69:615–623

    PubMed  CAS  Google Scholar 

  • Popielski L (1920) βImidazolylaethylamine und die Organextrakte. I. β-Imidazolylaethyl-amine als mächtiger Erreger der Magendrüsen. Pflügers Arch Gesamte Physiol 178:214–236

    Article  CAS  Google Scholar 

  • Robertson I, Greaves MW (1978) Responses of human skin blood vessels to synthetic histamine analogues. Br J Clin Pharmacol 5:319–322

    CAS  Google Scholar 

  • Smith JA, Mansfield LE, de Shazo RD, Nelson HS (1980) An evaluation of the pharmacologic inhibition of the immediate and late cutaneous reaction to allergen. J Allergy Clin Immunol 65:118–121

    Article  Google Scholar 

  • Thomas SE, Glenny H, Bleehen SS, Greaves MW, Pilgrim J, Rowell N, Fairiss G et al. (1985) Cimetidine and chlorpheniramine in the treatment of chronic urticaria — an interim analysis of the results from a multi-centre randomised double-blind study. In: Champion RH, Greaves MW, Kobza Black A, Pye RJ (eds) The urticarias. Churchill Livingstone, Edinburgh

    Google Scholar 

  • Van Wauwe J, Avouters F, Niemegeers CJE, Janssens F, van Nueten JM, Janssens PAJ (1981) In vivo pharmacology of astemizole, a new type of H1 anti-histaminic compound. Arch Int Pharmacodyn Ther 251(1):39–51

    PubMed  Google Scholar 

  • Williams TJ, Morley J (1973) Prostaglandins as potentiators of increased vascular permeability in inflammation. Nature 246:215–217

    Article  PubMed  CAS  Google Scholar 

  • Williams TJ, Peck MJ (1977) Role of prostaglanin-mediated vasodilatation in inflammation. Nature 270:530–532

    Article  PubMed  CAS  Google Scholar 

  • Woodward DF, Owen DAA (1982) Effect of H1- and H2-receptor antagonists on cutaneous inflammation evoked by histamine analogues and UV radiation. Eur J Pharmacol 77:103–112

    Article  PubMed  CAS  Google Scholar 

  • Wyllie JH, Hesselbo T, Black JW (1972) Effects in man of histamine H2-receptor blockade by burimamide. Lancet 2:1117–1120

    Article  PubMed  CAS  Google Scholar 

Download references

Authors

Editor information

Editors and Affiliations

Rights and permissions

Reprints and permissions

Copyright information

© 1989 Springer-Verlag Berlin Heidelberg

About this chapter

Cite this chapter

Owen, D.A.A. (1989). H1- and H2-Receptor Antagonists. In: Greaves, M.W., Shuster, S. (eds) Pharmacology of the Skin II. Handbook of Experimental Pharmacology, vol 87 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-74054-1_18

Download citation

  • DOI: https://doi.org/10.1007/978-3-642-74054-1_18

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-74056-5

  • Online ISBN: 978-3-642-74054-1

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics