Agents and Actions

, Volume 13, Issue 1, pp 16–20 | Cite as

Histamine receptor blocking effects of cimetidine in the airways

  • V. Hartmann
  • H. Magnussen
  • W. OliverJr
  • W. M. Abraham
  • A. Wanner
  • T. Ahmed
Histamine and Kinins


We investigated the modification of histamine-induced bronchoconstriction by the H2-antagonist cimetidine in conscious sheep. One hundred breaths of 5% histamine aerosol increased mean (SD) pulmonary resistance (RL) by 5.6 (1.4) cmH2O/1/sec. This increase inRL was completely blocked by intravenous clemastine (0.5 mg), a specific H1-antagonist, indicating that the histamine-induced bronchoconstriction was mediated by H1-receptors. Intravenous cimetidine caused a dose-dependent enhancement of the histamine response between 1 and 1000 mg with a mean peak ΔRL of 15.3 (5) cmH2O/1/sec (P<0.05) at the 1000 mg dose, while it blocked the histamine response at a dose of 2400 mg [ΔRL=1.9 (2) cmH2O/1/sec,p=NS]. This paradoxic effect was not related to an anticholinergic mechanism as intravenous cimetidine (2400 mg) failed to block carbachol-induced (25 breaths of 1% solution) bronchoconstriction. We conclude that in the ovine airway, cimetidine is a selective H2-histamine receptor blocker at lower tissue concentrations, and a combined H2- and H1-histamine receptor blocker at high tissue concentrations.


Histamine Cimetidine Receptor Blocker Tissue Concentration Blocking Effect 
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Copyright information

© Birkhäuser Verlag 1983

Authors and Affiliations

  • V. Hartmann
    • 2
  • H. Magnussen
    • 2
  • W. OliverJr
    • 1
  • W. M. Abraham
    • 1
  • A. Wanner
    • 1
  • T. Ahmed
    • 1
  1. 1.Division of Pulmonary DiseaseMount Sinai Medical CenterMiami BeachUSA
  2. 2.Medizinische Universitäts-PoliklinikBonnWest Germany

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