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All antihistamines cross blood-brain barrier

BMJ 2000; 321 doi: https://doi.org/10.1136/bmj.321.7260.572 (Published 02 September 2000) Cite this as: BMJ 2000;321:572

This article has a correction. Please see:

  1. J G Ramaekers, experimental psychopharmacologist (j.ramaekers@psychology.unimaas.nl),
  2. A Vermeeren, experimental psychologist
  1. Experimental Psychopharmacology Unit, Brain and Behaviour Institute, Maastricht University, 6200 MD Maastricht, Netherlands

    EDITOR—With reference to the paper by Mann et al,1 the dichotomy between antihistamines of the first and second generation was introduced to indicate a big pharmacological difference between these drugs. The second generation antihistamines were less soluble in lipid and thus less readily penetrated the blood-brain barrier. When given to people in therapeutic doses, terfenadine produced about 17% occupancy of histamine H1 receptors in the frontal lobe whereas the first generation antihistamine chlorpheniramine produced about 77% occupancy.2 In …

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